-
1
-
-
84881044531
-
-
sixth ed. The Global Burden (accessed 26.12.13)
-
International Diabetes Federation - Diabetes Atlas sixth ed. 2013 The Global Burden 29 50 http://www.idf.org/diabetesatlas/download-book (accessed 26.12.13)
-
(2013)
International Diabetes Federation - Diabetes Atlas
, pp. 29-50
-
-
-
2
-
-
75149130955
-
Diagnosis and classification of diabetes mellitus
-
American Diabetes Association
-
American Diabetes Association Diagnosis and classification of diabetes mellitus Diabetes Care 33 2010 S62 S69
-
(2010)
Diabetes Care
, vol.33
-
-
-
4
-
-
84861389721
-
India's diabetes time bomb
-
P. Shetty India's diabetes time bomb Nat. Outlook: Diabetes 485 2012 S14 S16
-
(2012)
Nat. Outlook: Diabetes
, vol.485
-
-
Shetty, P.1
-
6
-
-
79960262492
-
Management of type 2 diabetes: New and future developments in treatment
-
A.A. Tahrani, C.J. Bailey, S.D. Prato, and A.H. Barnett Management of type 2 diabetes: new and future developments in treatment Lancet 378 2011 182 197
-
(2011)
Lancet
, vol.378
, pp. 182-197
-
-
Tahrani, A.A.1
Bailey, C.J.2
Prato, S.D.3
Barnett, A.H.4
-
8
-
-
0141785429
-
Glucose-dependent insulinotropic polypeptide promotes β-(INS-1) cell survival via cyclic adenosine monophosphate-mediated caspase-3 inhibition and regulation of p38 mitogen-activated protein kinase
-
DOI 10.1210/en.2002-0068
-
J.A. Ehses, V.R. Casilla, and T. Doty et al. Glucose-dependent insulinotropic polypeptide promotes beta-(INS-1) cell survival via cyclic adenosine monophosphate-mediated caspase-3 inhibition and regulation of p38 mitogen-activated protein kinase Endocrinology 144 2003 4433 4445 (Pubitemid 37204843)
-
(2003)
Endocrinology
, vol.144
, Issue.10
, pp. 4433-4445
-
-
Ehses, J.A.1
Casilla, V.R.2
Doty, T.3
Pospisilik, J.A.4
Winter, K.D.5
Demuth, H.-U.6
Pederson, R.A.7
McIntosh, C.H.S.8
-
9
-
-
0345374580
-
Glucagon-Like Peptide 1 Inhibits Cell Apoptosis and Improves Glucose Responsiveness of Freshly Isolated Human Islets
-
DOI 10.1210/en.2003-0323
-
L. Farilla, A. Bulotta, and B. Hirshberg et al. Glucagon-like peptide 1 inhibits cell apoptosis and improves glucose responsiveness of freshly isolated human islets Endocrinology 144 2003 5149 5158 (Pubitemid 37476040)
-
(2003)
Endocrinology
, vol.144
, Issue.12
, pp. 5149-5158
-
-
Farilla, L.1
Bulotta, A.2
Hirshberg, B.3
Li Calzi, S.4
Khoury, N.5
Noushmehr, H.6
Bertolotto, C.7
Di Mario, U.8
Harlan, D.M.9
Perfetti, R.10
-
10
-
-
0034522773
-
Glucagon-like peptide-1 induces cell proliferation and pancreatic-duodenum homeobox-1 expression and increases endocrine cell mass in the pancreas of old, glucose-intolerant rats
-
DOI 10.1210/en.141.12.4600
-
R. Perfetti, J. Zhou, M.E. Doyle, and J.M. Egan Glucagon-like peptide-1 induces cell proliferation and pancreatic- duodenum homeobox-1 expression and increases endocrine cell mass in the pancreas of old, glucose-intolerant rats Endocrinology 141 2000 4600 4605 (Pubitemid 32055138)
-
(2000)
Endocrinology
, vol.141
, Issue.12
, pp. 4600-4605
-
-
Perfetti, R.1
Zhou, J.I.E.2
Doyle, M.E.3
Egan, J.M.4
-
11
-
-
0037312821
-
The influence of GLP-1 on glucose-stimulated insulin secretion: Effects on β-cell sensitivity in type 2 and nondiabetic subjects
-
DOI 10.2337/diabetes.52.2.380
-
L.L. Kjems, J.J. Holst, A. Volund, and S. Madsbad The influence of GLP-1 on glucose-stimulated insulin secretion: effects on beta-cell sensitivity in type 2 and nondiabetic subjects Diabetes 52 2003 380 386 (Pubitemid 36173193)
-
(2003)
Diabetes
, vol.52
, Issue.2
, pp. 380-386
-
-
Kjems, L.L.1
Holst, J.J.2
Volund, A.3
Madsbad, S.4
-
12
-
-
0033766716
-
Degradation of endogenous and exogenous gastric inhibitory polypeptide in healthy and in type 2 diabetic subjects as revealed using a new assay for the intact peptide
-
C.F. Deacon, M.A. Nauck, and J. Meier et al. Degradation of endogenous and exogenous gastric inhibitory polypeptide in healthy and in type 2 diabetic subjects as revealed using a new assay for the intact peptide J. Clin. Endocrinol. Metab. 85 2000 3575 3581
-
(2000)
J. Clin. Endocrinol. Metab.
, vol.85
, pp. 3575-3581
-
-
Deacon, C.F.1
Nauck, M.A.2
Meier, J.3
-
13
-
-
0037241085
-
Similar elimination rates of glucagon-like peptide-1 in obese type 2 diabetic patients and healthy subjects
-
DOI 10.1210/jc.2002-021053
-
T. Vilsboll, H. Agerso, T. Krarup, and J.J. Holst Similar elimination rates of glucagon-like peptide-1 in obese type 2 diabetic patients and healthy subjects J. Clin. Endocrinol. Metab. 88 2003 220 224 (Pubitemid 36115169)
-
(2003)
Journal of Clinical Endocrinology and Metabolism
, vol.88
, Issue.1
, pp. 220-224
-
-
Vilsboll, T.1
Agerso, H.2
Krarup, T.3
Holst, J.J.4
-
14
-
-
1442350411
-
Secretion, Degradation, and Elimination of Glucagon-Like Peptide 1 and Gastric Inhibitory Polypeptide in Patients with Chronic Renal Insufficiency and Healthy Control Subjects
-
DOI 10.2337/diabetes.53.3.654
-
J.J. Meier, M.A. Nauck, and D. Kranz et al. Secretion, degradation, and elimination of glucagon-like peptide 1 and gastric inhibitory polypeptide in patients with chronic renal insufficiency and healthy control subjects Diabetes 53 2004 654 662 (Pubitemid 38270634)
-
(2004)
Diabetes
, vol.53
, Issue.3
, pp. 654-662
-
-
Meier, J.J.1
Nauck, M.A.2
Kranz, D.3
Holst, J.J.4
Deacon, C.F.5
Gaeckler, D.6
Schmidt, W.E.7
Gallwitz, B.8
-
15
-
-
0014155217
-
Purification and characterization of an aminopeptidase hydrolysing glycyl-proline-naphthylamide
-
V.K. Hopsu-Havu, and S.S. Sarimo Purification and characterization of an aminopeptidase hydrolysing glycyl-proline-naphthylamide Hoppe Seylers Z. Physiol. Chem. 384 1967 1540 1550
-
(1967)
Hoppe Seylers Z. Physiol. Chem.
, vol.384
, pp. 1540-1550
-
-
Hopsu-Havu, V.K.1
Sarimo, S.S.2
-
16
-
-
29144522905
-
Rigidity and flexibility of dipeptidyl peptidase IV: Crystal structures of and docking experiments with DPIV
-
DOI 10.1016/j.jmb.2005.11.014, PII S0022283605014002
-
M. Engel, T. Hoffmann, and S. Manhart et al. Rigidity and flexibility of dipeptidyl peptidase IV: crystal structures of and docking experiments with DPIV J. Mol. Biol. 355 2006 768 783 (Pubitemid 41817635)
-
(2006)
Journal of Molecular Biology
, vol.355
, Issue.4
, pp. 768-783
-
-
Engel, M.1
Hoffmann, T.2
Manhart, S.3
Heiser, U.4
Chambre, S.5
Huber, R.6
Demuth, H.-U.7
Bode, W.8
-
17
-
-
84861095436
-
DPP IV inhibitors: Successes, failures and future prospects
-
A.D. Kshirsagar, and A.S. Aggarwal et al. DPP IV inhibitors: successes, failures and future prospects Diabetes Metab. Syndr. 5 2011 105 112
-
(2011)
Diabetes Metab. Syndr.
, vol.5
, pp. 105-112
-
-
Kshirsagar, A.D.1
Aggarwal, A.S.2
-
18
-
-
0027982677
-
Genomic organization, exact localization, and tissue expression of the human CD26 (dipeptidyl peptidase IV) gene
-
C.A. Abbott, E. Baker, and G.R. Sutherland et al. Genomic organization, exact localization, and tissue expression of the human CD26 (dipeptidyl peptidase IV) gene Immunogenetics 40 1994 31 38
-
(1994)
Immunogenetics
, vol.40
, pp. 31-38
-
-
Abbott, C.A.1
Baker, E.2
Sutherland, G.R.3
-
19
-
-
33947705084
-
Molecular recognition of ligands in dipeptidyl peptidase IV
-
DOI 10.2174/156802607780091064
-
B. Kuhn, M. Hennig, and P. Mattei Molecular recognition of ligands in dipeptidyl peptidase IV Curr. Top. Med. Chem. 7 2007 609 619 (Pubitemid 46488283)
-
(2007)
Current Topics in Medicinal Chemistry
, vol.7
, Issue.6
, pp. 609-619
-
-
Kuhn, B.1
Hennig, M.2
Mattei, P.3
-
20
-
-
0033619675
-
Dipeptidyl-peptidase IV (CD26)-role in the inactivation of regulatory peptides
-
DOI 10.1016/S0167-0115(99)00089-0, PII S0167011599000890
-
R. Mentlein Dipeptidyl-peptidase IV (CD26) - role in the inactivation of regulatory peptides Regul. Pept. 85 1999 9 24 (Pubitemid 29505281)
-
(1999)
Regulatory Peptides
, vol.85
, Issue.1
, pp. 9-24
-
-
Mentlein, R.1
-
22
-
-
0037219684
-
Crystal structure of human dipeptidyl peptidase IV/CD26 in complex with a substrate analog
-
DOI 10.1038/nsb882
-
H.B. Rasmussen, S. Branner, F.C. Wiberg, and N. Wagtmann Crystal structure of human dipeptidyl peptidase IV/CD26 in complex with a substrate analog Nat. Struct. Biol. 10 2003 19 25 (Pubitemid 36034172)
-
(2003)
Nature Structural Biology
, vol.10
, Issue.1
, pp. 19-25
-
-
Rasmussen, H.B.1
Branner, S.2
Wiberg, F.C.3
Wagtmann, N.4
-
23
-
-
0042131827
-
Structural basis of proline-specific exopeptidase activity as observed in human dipeptidyl peptidase-IV
-
DOI 10.1016/S0969-2126(03)00160-6
-
R. Thoma, B. Loeffler, M. Stihle, W. Huber, A. Ruf, and M. Hennig Structural basis of proline-specific exopeptidase activity as observed in human dipeptidyl peptidase-IV Structure 11 2003 947 959 (Pubitemid 36966784)
-
(2003)
Structure
, vol.11
, Issue.8
, pp. 947-959
-
-
Thoma, R.1
Loffler, B.2
Stihle, M.3
Huber, W.4
Ruf, A.5
Hennig, M.6
-
24
-
-
10644296948
-
One site mutation disrupts dimer formation in human DPP-IV proteins
-
C.H. Chien, L.H. Huang, C.Y. Chou, and Y.S. Chen et al. One site mutation disrupts dimer formation in human DPP-IV proteins J. Biol. Chem. 279 2004 52338 52345
-
(2004)
J. Biol. Chem.
, vol.279
, pp. 52338-52345
-
-
Chien, C.H.1
Huang, L.H.2
Chou, C.Y.3
Chen, Y.S.4
-
25
-
-
84860480412
-
Long-acting peptidomimetics based DPP-IV inhibitors
-
S.R. Shah, R. Bahekar, P. Jadav, D. Patel, and A. Joharapurkar et al. Long-acting peptidomimetics based DPP-IV inhibitors Bioorg. Med. Chem. Lett. 22 2012 3516 3521
-
(2012)
Bioorg. Med. Chem. Lett.
, vol.22
, pp. 3516-3521
-
-
Shah, S.R.1
Bahekar, R.2
Jadav, P.3
Patel, D.4
Joharapurkar, A.5
-
26
-
-
84877061867
-
A comparative study of the binding modes of recently launched dipeptidyl peptidase IV inhibitors in the active site, Biochem
-
M. Nabeno, F. Akahoshi, and H. Kishida et al. A comparative study of the binding modes of recently launched dipeptidyl peptidase IV inhibitors in the active site, Biochem Biophys. Res. Commun. 434 2013 191 196
-
(2013)
Biophys. Res. Commun.
, vol.434
, pp. 191-196
-
-
Nabeno, M.1
Akahoshi, F.2
Kishida, H.3
-
27
-
-
0038793576
-
High-resolution structure of human apo dipeptidyl peptidase IV/CD26 and its complex with 1-[({2-[(5-iodopyridin-2-yl)amino]-ethyl}amino)- acetyl]-2-cyano-(S)-pyrrolidine
-
DOI 10.1107/S0907444903010059
-
Oefner, A. D'Arcy, and A.M. Sweeney et al. High resolution structure of human apo dipeptidyl peptidase IV/CD26 and its complex with 1-[({2-[(5- iodopyridin-2-yl)amino]-ethyl}-amino)-acetyl]-2-cyano-(S)-pyrrolidine Acta Crystallogr. Sect. D. 59 2003 1206 1212 (Pubitemid 36872357)
-
(2003)
Acta Crystallographica Section D: Biological Crystallography
, vol.59
, Issue.7
, pp. 1206-1212
-
-
Oefner, C.1
D'Arcy, A.2
Mac Sweeney, A.3
Pierau, S.4
Gardiner, R.5
Dale, G.E.6
-
28
-
-
0037966007
-
The crystal structure of dipeptidyl peptidase IV (CD26) reveals its functional regulation and enzymatic mechanism
-
DOI 10.1073/pnas.0230620100
-
M. Engel, T. Hoffmann, L. Wagner, and M. Wermann et al. The crystal structure of dipeptidyl peptidase IV (CD26) reveals its functional regulation and enzymatic mechanism Proc. Natl. Acad. Sci. U.S.A. 100 2003 5063 5068 (Pubitemid 36542658)
-
(2003)
Proceedings of the National Academy of Sciences of the United States of America
, vol.100
, Issue.9
, pp. 5063-5068
-
-
Engel, M.1
Hoffmann, T.2
Wagner, L.3
Wermann, M.4
Heiser, U.5
Kiefersauer, R.6
Huber, R.7
Bode, W.8
Demuth, H.-U.9
Brandstetter, H.10
-
29
-
-
33845339435
-
Protease inhibitors in the clinic
-
G. Abbenante, and D.P. Fairlie Protease inhibitors in the clinic Med. Chem. 1 2005 71 104
-
(2005)
Med. Chem.
, vol.1
, pp. 71-104
-
-
Abbenante, G.1
Fairlie, D.P.2
-
30
-
-
34250206962
-
Docking-based 3D-QSAR study for selectivity of DPP4, DPP8, and DPP9 inhibitors
-
DOI 10.1016/j.bmcl.2007.04.031, PII S0960894X07004519
-
N.S. Kang, J.H. Ahn, S.S. Kim, C.H. Chae, and S. Yoo Docking-based 3D-QSAR study for selectivity of DPP4, DPP8, and DPP9 inhibitors Bioorg. Med. Chem. Lett. 17 2007 3716 3721 (Pubitemid 46901103)
-
(2007)
Bioorganic and Medicinal Chemistry Letters
, vol.17
, Issue.13
, pp. 3716-3721
-
-
Kang, N.S.1
Ahn, J.H.2
Kim, S.S.3
Chae, C.H.4
Yoo, S.-E.5
-
31
-
-
20444390974
-
Glutamic acid analogues as potent dipeptidyl peptidase IV and 8 inhibitors
-
DOI 10.1016/j.bmcl.2005.04.051, PII S0960894X05005330
-
I.L. Lu, S.J. Lee, H. Tsu, and S.Y. Wu et al. Glutamic acid analogues as potent dipeptidyl peptidase IV and 8 inhibitors Bioorg. Med. Chem. Lett. 15 2005 3271 3275 (Pubitemid 40799072)
-
(2005)
Bioorganic and Medicinal Chemistry Letters
, vol.15
, Issue.13
, pp. 3271-3275
-
-
Lu, I.-L.1
Lee, S.-J.2
Tsu, H.3
Wu, S.-Y.4
Kao, K.-H.5
Chien, C.-H.6
Chang, Y.-Y.7
Chen, Y.-S.8
Cheng, J.-H.9
Chang, C.-N.10
Chen, T.-W.11
Chang, S.-P.12
Chen, X.13
Jiaang, W.-T.14
-
32
-
-
33845648469
-
Homology models of dipeptidyl peptidases 8 and 9 with a focus on loop predictions near the active site
-
DOI 10.1002/prot.21138
-
C. Rummey, and G. Metz Homology models of dipeptidyl peptidases 8 and 9 with a focus on loop predictions near the active site Proteins: Struct. Funct. Bioinform. 66 2007 160 171 (Pubitemid 44955988)
-
(2007)
Proteins: Structure, Function and Genetics
, vol.66
, Issue.1
, pp. 160-171
-
-
Rummey, C.1
Metz, G.2
-
33
-
-
3843072211
-
Dipeptidyl peptidase IV inhibitors for the treatment of diabetes
-
DOI 10.1021/jm030628v
-
A.E. Weber Dipeptidyl peptidase IV inhibitors for the treatment of diabetes J. Med. Chem. 47 2004 4135 4141 (Pubitemid 39045417)
-
(2004)
Journal of Medicinal Chemistry
, vol.47
, Issue.17
, pp. 4135-4141
-
-
Weber, A.E.1
-
34
-
-
70350513013
-
Efficacy and safety of incretin based therapies: Clinical trial data
-
J. White Efficacy and safety of incretin based therapies: clinical trial data J. Am. Pharm. Assoc. 49 2009 S30 S40
-
(2009)
J. Am. Pharm. Assoc.
, vol.49
-
-
White, J.1
-
35
-
-
84873852937
-
Choosing between GLP-1 receptor agonists & DPP-4 inhibitors: A pharmacological perspective
-
10.1155/2012/381713
-
D.X. Brown, and M. Evans Choosing between GLP-1 receptor agonists & DPP-4 inhibitors: a pharmacological perspective J. Nutr. Metab. 2012 10.1155/2012/381713
-
(2012)
J. Nutr. Metab.
-
-
Brown, D.X.1
Evans, M.2
-
36
-
-
41149118550
-
(R)-8-(3-amino-piperidin-1-yl)-7-but-2-ynyl-3-methyl-1-(4-methyl- quinazolin-2-ylmethyl)-3,7-dihydro-purine-2,6-dione (BI 1356), a novel xanthine-based dipeptidyl peptidase 4 inhibitor, has a superior potency and longer duration of action compared with other dipeptidyl peptidase-4 inhibitors
-
DOI 10.1124/jpet.107.135723
-
L. Thomas, M. Eckhardt, E. Langkopf, M. Tadayyon, F. Himmelsbach, and M. Mark (R)-8-(3-amino-piperidin-1-yl)-7-but-2-ynyl-3-methyl-1-(4-methylquinazolin- 2-ylmethyl)-3,7-dihydro-purine-2,6-dione (BI 1356), a novel xanthine-based dipeptidyl peptidase 4 inhibitor, has a superior potency and longer duration of action compared with other dipeptidyl peptidase-4 inhibitors J. Pharmacol. Exp. Ther. 325 2008 175 182 (Pubitemid 351439162)
-
(2008)
Journal of Pharmacology and Experimental Therapeutics
, vol.325
, Issue.1
, pp. 175-182
-
-
Thomas, L.1
Eckhardt, M.2
Langkopf, E.3
Tadayyon, M.4
Himmelsbach, F.5
Mark, M.6
-
37
-
-
78649686908
-
Dipeptidyl peptidase-4 inhibitors in the treatment of type 2 diabetes: A comparative review
-
C.F. Deacon Dipeptidyl peptidase-4 inhibitors in the treatment of type 2 diabetes: a comparative review Diabetes Obes. Metab. 13 2011 7 18
-
(2011)
Diabetes Obes. Metab.
, vol.13
, pp. 7-18
-
-
Deacon, C.F.1
-
38
-
-
32844473903
-
Pharmacokinetic and pharmacodynamic properties of multiple oral doses of sitagliptin, a dipeptidyl peptidase-IV inhibitor: A double-blind, randomized, placebo-controlled study in healthy male volunteers
-
DOI 10.1016/j.clinthera.2006.01.015, PII S0149291806000294
-
A.J. Bergman, C. Stevens, and Y. Zhou et al. Pharmacokinetic and pharmacodynamic properties of multiple oral doses of sitagliptin, a dipeptidyl peptidase-IV inhibitor: a double-blind, randomized, placebo-controlled study in healthy male volunteers Clin. Ther. 28 2006 55 72 (Pubitemid 43254990)
-
(2006)
Clinical Therapeutics
, vol.28
, Issue.1
, pp. 55-72
-
-
Bergman, A.J.1
Stevens, C.2
Zhou, Y.3
Yi, B.4
Laethem, M.5
De Smet, M.6
Snyder, K.7
Hilliard, D.8
Tanaka, W.9
Zeng, W.10
Tanen, M.11
Wang, A.Q.12
Chen, L.13
Winchell, G.14
Davies, M.J.15
Ramael, S.16
Wagner, J.A.17
Herman, G.A.18
-
40
-
-
34147208931
-
Pharmacodynamics of vildagliptin in patients with type 2 diabetes during OGTT
-
DOI 10.1177/0091270006299137
-
Y.L. He, Y. Wang, and J.M. Bullock et al. Pharmacodynamics of vildagliptin in patients with type 2 diabetes during OGTT J. Clin. Pharmacol. 47 2007 633 641 (Pubitemid 46632151)
-
(2007)
Journal of Clinical Pharmacology
, vol.47
, Issue.5
, pp. 633-641
-
-
He, Y.-L.1
Wang, Y.2
Bullock, J.M.3
Deacon, C.F.4
Holst, J.J.5
Dunning, B.E.6
Ligueros-Saylan, M.7
Foley, J.E.8
-
41
-
-
0037777695
-
1-[[(3-Hydroxy-1-adamantyl)amino]acetyl]-2-cyano-(S)-pyrrolidine: A potent, selective, and orally bioavailable dipeptidyl peptidase IV inhibitor with antihyperglycemic properties
-
DOI 10.1021/jm030091l
-
E.B. Villhauer, J.A. Brinkman, and G.B. Naderi et al. 1-[[(3-Hydroxy-1-adamantyl)amino]acetyl]-2-cyano-(S)-pyrrolidine: a potent, selective, and orally bioavailable dipeptidyl peptidase IV inhibitor with antihyperglycemic properties J. Med. Chem. 46 2003 2774 2789 (Pubitemid 36702545)
-
(2003)
Journal of Medicinal Chemistry
, vol.46
, Issue.13
, pp. 2774-2789
-
-
Villhauer, E.B.1
Brinkman, J.A.2
Naderi, G.B.3
Burkey, B.F.4
Dunning, B.E.5
Prasad, K.6
Mangold, B.L.7
Russell, M.E.8
Hughes, T.E.9
-
43
-
-
77951702763
-
Safety, tolerability, pharmacokinetics and pharmacodynamics of once daily oral doses of saxagliptin for 2 weeks in type 2 diabetic and healthy subjects (poster 0606-P)
-
D.W. Boulton, and M. Geraldes Safety, tolerability, pharmacokinetics and pharmacodynamics of once daily oral doses of saxagliptin for 2 weeks in type 2 diabetic and healthy subjects (poster 0606-P) Diabetes 56 2007 A161
-
(2007)
Diabetes
, vol.56
, pp. 161
-
-
Boulton, D.W.1
Geraldes, M.2
-
44
-
-
41649083174
-
Pharmacokinetic, pharmacodynamic, and tolerability profiles of the dipeptidyl peptidase-4 inhibitor alogliptin: A randomized, double-blind, placebo-controlled, multiple-dose study in adult patients with type 2 diabetes
-
DOI 10.1016/j.clinthera.2008.03.004, PII S0149291808001173
-
P. Covington, R. Christopher, and M. Davenport et al. Pharmacokinetic, pharmacodynamic, and tolerability profiles of the dipeptidyl peptidase-4 inhibitor alogliptin: a randomized, double-blind, placebo-controlled, multiple-dose study in adult patients with type 2 diabetes Clin. Ther. 30 2008 499 512 (Pubitemid 351483925)
-
(2008)
Clinical Therapeutics
, vol.30
, Issue.3
, pp. 499-512
-
-
Covington, P.1
Christopher, R.2
Davenport, M.3
Fleck, P.4
Mekki, Q.A.5
Wann, E.R.6
Karim, A.7
-
45
-
-
67649998759
-
Pharmacokinetics, pharmacodynamics and tolerability of multiple oral doses of linagliptin, a dipeptidyl peptidase-4 inhibitor in male type 2 diabetes patients
-
T. Heise, E.U. Graefe-Mody, S. Huttner, and A. Ring et al. Pharmacokinetics, pharmacodynamics and tolerability of multiple oral doses of linagliptin, a dipeptidyl peptidase-4 inhibitor in male type 2 diabetes patients Diabetes Obes. Metab. 11 2009 786 794
-
(2009)
Diabetes Obes. Metab.
, vol.11
, pp. 786-794
-
-
Heise, T.1
Graefe-Mody, E.U.2
Huttner, S.3
Ring, A.4
-
46
-
-
25844459084
-
Dipeptidyl peptidase IV inhibition for the treatment of type 2 diabetes: Potential importance of selectivity over dipeptidyl peptidases 8 and 9
-
DOI 10.2337/diabetes.54.10.2988
-
G.R. Lankas, B. Leiting, and R.S. Roy et al. Dipeptidyl peptidase IV inhibition for the treatment of type 2 diabetes: potential importance of selectivity over dipeptidyl peptidases 8 and 9 Diabetes 54 2005 2988 2994 (Pubitemid 41401097)
-
(2005)
Diabetes
, vol.54
, Issue.10
, pp. 2988-2994
-
-
Lankas, G.R.1
Leiting, B.2
Roy, R.S.3
Eiermann, G.J.4
Beconi, M.G.5
Biftu, T.6
Chan, C.-C.7
Edmondson, S.8
Feeney, W.P.9
He, H.10
Ippolito, D.E.11
Kim, D.12
Lyons, K.A.13
Ok, H.O.14
Patel, R.A.15
Petrov, A.N.16
Pryor, K.A.17
Qian, X.18
Reigle, L.19
Woods, A.20
Wu, J.K.21
Zaller, D.22
Zhang, X.23
Zhu, L.24
Weber, A.E.25
Thornberry, N.A.26
more..
-
47
-
-
63849095884
-
Role of dipeptidyl peptidase IV (DP IV)-like enzymes in T lymphocyte activation: Investigations in DP IV/CD26-knockout mice
-
D. Reinhold, A. Goihl, and S. Wrenger et al. Role of dipeptidyl peptidase IV (DP IV)-like enzymes in T lymphocyte activation: investigations in DP IV/CD26-knockout mice Clin. Chem. Lab. Med. 47 2009 268 274
-
(2009)
Clin. Chem. Lab. Med.
, vol.47
, pp. 268-274
-
-
Reinhold, D.1
Goihl, A.2
Wrenger, S.3
-
48
-
-
48049092062
-
Adverse effects of dipeptidyl peptidases 8 and 9 inhibition in rodents revisited
-
B.F. Burkey, P.K. Hoffmann, U. Hassiepen, J. Trappe, M. Juedes, and J.E. Foley Adverse effects of dipeptidyl peptidases 8 and 9 inhibition in rodents revisited Diabetes Obes. Metab. 10 2008 1057 1061
-
(2008)
Diabetes Obes. Metab.
, vol.10
, pp. 1057-1061
-
-
Burkey, B.F.1
Hoffmann, P.K.2
Hassiepen, U.3
Trappe, J.4
Juedes, M.5
Foley, J.E.6
-
49
-
-
65649147246
-
Biochemistry, pharmacokinetics, and toxicology of a potent and selective DPP8/9 inhibitor
-
J. Wu, H. Tang, T. Yeh, and C. Chen et al. Biochemistry, pharmacokinetics, and toxicology of a potent and selective DPP8/9 inhibitor Biochem. Pharmacol. 78 2009 203 210
-
(2009)
Biochem. Pharmacol.
, vol.78
, pp. 203-210
-
-
Wu, J.1
Tang, H.2
Yeh, T.3
Chen, C.4
-
50
-
-
84859172957
-
Potency, selectivity and prolonged binding of saxagliptin to DPP4: Maintenance of DPP4 inhibition by saxagliptin in vitro and ex vivo when compared to a rapidly-dissociating DPP4 inhibitor
-
M.S. Kirby, A. Wang, and C. Dorso et al. Potency, selectivity and prolonged binding of saxagliptin to DPP4: maintenance of DPP4 inhibition by saxagliptin in vitro and ex vivo when compared to a rapidly-dissociating DPP4 inhibitor BMC Pharmacol. 12 2012 2 12
-
(2012)
BMC Pharmacol.
, vol.12
, pp. 2-12
-
-
Kirby, M.S.1
Wang, A.2
Dorso, C.3
-
52
-
-
66649134595
-
In vitro enzymologic characteristics of saxagliptin, a highly potent and selective DPP4 inhibitor with ''slow binding'' characteristic (Abstract)
-
M.S. Kirby, C. Dorso, and A. Wang et al. In vitro enzymologic characteristics of saxagliptin, a highly potent and selective DPP4 inhibitor with ''slow binding'' characteristic (Abstract) Clin. Chem. Lab. Med. 46 2008 A79
-
(2008)
Clin. Chem. Lab. Med.
, vol.46
, pp. 79
-
-
Kirby, M.S.1
Dorso, C.2
Wang, A.3
-
53
-
-
53149100519
-
Seprase: An overview of an important matrix serine protease
-
P. O'Brien, and B.F. O'Connor Seprase: an overview of an important matrix serine protease Biochim. Biophys. Acta 1784 2008 1130 1145
-
(2008)
Biochim. Biophys. Acta
, vol.1784
, pp. 1130-1145
-
-
O'Brien, P.1
O'Connor, B.F.2
-
54
-
-
0035432607
-
Glucagon-like peptide-1 infusion must be maintained for 24 h/day to obtain acceptable glycemia in type 2 diabetic patients who are poorly controlled on sulphonylurea treatment
-
J. Larsen, B. Hylleberg, K. Ng, and P. Damsbo Glucagon-like peptide-1 infusion must be maintained for 24 h/day to obtain acceptable glycemia in type 2 diabetic patients who are poorly controlled on sulphonylurea treatment Diabetes Care 24 2001 1416 1421 (Pubitemid 33716430)
-
(2001)
Diabetes Care
, vol.24
, Issue.8
, pp. 1416-1421
-
-
Larsen, J.1
Hylleberg, B.2
Ng, K.3
Damsbo, P.4
-
55
-
-
61349143225
-
Medicinal chemistry approaches to the inhibition of dipeptidyl peptidase-4 for the treatment of type 2 diabetes
-
M. Pal, and S.H. Havale Medicinal chemistry approaches to the inhibition of dipeptidyl peptidase-4 for the treatment of type 2 diabetes Bioorg. Med. Chem. 17 2009 1783 1802
-
(2009)
Bioorg. Med. Chem.
, vol.17
, pp. 1783-1802
-
-
Pal, M.1
Havale, S.H.2
-
56
-
-
59149106467
-
Medicinal chemistry approaches to the inhibition of dipeptidyl peptidase IV
-
S.L. Gwaltney II Medicinal chemistry approaches to the inhibition of dipeptidyl peptidase IV Curr. Top. Med. Chem. 8 2008 1545 1552
-
(2008)
Curr. Top. Med. Chem.
, vol.8
, pp. 1545-1552
-
-
Gwaltney, I.I.S.L.1
-
57
-
-
84865785890
-
Recent advances in non-peptidomimetic dipeptidyl peptidase 4 inhibitors: Medicinal chemistry and preclinical aspects
-
Y. Liu, Y. Hu, and T. Liu Recent advances in non-peptidomimetic dipeptidyl peptidase 4 inhibitors: medicinal chemistry and preclinical aspects Curr. Med. Chem. 19 2012 3982 3999
-
(2012)
Curr. Med. Chem.
, vol.19
, pp. 3982-3999
-
-
Liu, Y.1
Hu, Y.2
Liu, T.3
-
58
-
-
20444406121
-
Inhibition of dipeptidyl-peptidase IV catalyzed peptide truncation by Vildagliptin ((2S)-{[(3-hydroxyadamantan-1-yl)amino]acetyl}-pyrrolidine-2- carbonitrile)
-
DOI 10.1016/j.bcp.2005.04.009, PII S0006295205002376
-
I. Brandt, J. Joossens, and X. Chen et al. Inhibition of dipeptidyl-peptidase IV catalyzed peptide truncation by vildagliptin ((2S)-{[(3-hydroxyadamantan-1-yl)amino]acetyl}-pyrrolidine-2-carbonitrile) Biochem Pharmacol. 70 2005 134 143 (Pubitemid 40797877)
-
(2005)
Biochemical Pharmacology
, vol.70
, Issue.1
, pp. 134-143
-
-
Brandt, I.1
Joossens, J.2
Chen, X.3
Maes, M.-B.4
Scharpe, S.5
De Meester, I.6
Lambeir, A.-M.7
-
59
-
-
33847613829
-
Vildagliptin displays slow tight-binding to dipeptidyl peptidase (DPP)-4, but not DPP-8 or DPP-9 (Abstract 0788)
-
B.F. Burkey, M. Russell, K. Wang, J. Trappe, and T.E. Hughes Vildagliptin displays slow tight-binding to dipeptidyl peptidase (DPP)-4, but not DPP-8 or DPP-9 (Abstract 0788) Diabetologia 49 2006 477
-
(2006)
Diabetologia
, vol.49
, pp. 477
-
-
Burkey, B.F.1
Russell, M.2
Wang, K.3
Trappe, J.4
Hughes, T.E.5
-
60
-
-
29244449635
-
Mechanism of Gly-Pro-pNA cleavage catalyzed by dipeptidyl peptidase-IV and its inhibition by saxagliptin (BMS-477118)
-
DOI 10.1016/j.abb.2005.11.010, PII S0003986105004819
-
Y.B. Kim, L.M. Kopcho, and M.S. Kirby et al. Mechanism of Gly-Pro-pNA cleavage catalyzed by dipeptidyl peptidase-IV and its inhibition by saxagliptin (BMS-477118) Arch. Biochem Biophys. 445 2006 9 18 (Pubitemid 41821056)
-
(2006)
Archives of Biochemistry and Biophysics
, vol.445
, Issue.1
, pp. 9-18
-
-
Kim, Y.B.1
Kopcho, L.M.2
Kirby, M.S.3
Hamann, L.G.4
Weigelt, C.A.5
Metzler, W.J.6
Marcinkeviciene, J.7
-
61
-
-
84894182216
-
DPP-IV Inhibition: Promising therapy for the treatment of type 2 diabetes
-
W. Paul DPP-IV Inhibition: promising therapy for the treatment of type 2 diabetes Prog. Med. Chem. 45 2007 71 73
-
(2007)
Prog. Med. Chem.
, vol.45
, pp. 71-73
-
-
Paul, W.1
-
62
-
-
67349123804
-
Synthesis and evaluation of structurally constrained imidazolidin derivatives as potent dipeptidyl peptidase IV inhibitors
-
X. Wang, Y. Wu, L. Wang, and B. Zhang et al. Synthesis and evaluation of structurally constrained imidazolidin derivatives as potent dipeptidyl peptidase IV inhibitors Eur. J. Med. Chem. 44 2009 3318 3322
-
(2009)
Eur. J. Med. Chem.
, vol.44
, pp. 3318-3322
-
-
Wang, X.1
Wu, Y.2
Wang, L.3
Zhang, B.4
-
63
-
-
2342565117
-
Synthesis of Novel Potent Dipeptidyl Peptidase IV Inhibitors with Enhanced Chemical Stability: Interplay between the N-Terminal Amino Acid Alkyl Side Chain and the Cyclopropyl Group of α -Aminoacyl-L-cis-4,5- methanoprolinenitrile-Based Inhibitors
-
DOI 10.1021/jm049924d
-
D.R. Magnin, J.A. Robl, R.B. Sulsky, and D.J. Augeri et al. Synthesis of novel potent dipeptidyl peptidase IV inhibitors with enhanced chemical stability: interplay between the N-terminal amino acid alkyl side chain and the cyclopropyl group of α-aminoacyl-l-cis-4,5-methanoprolinenitrile-based inhibitors J. Med. Chem. 47 2004 2587 2598 (Pubitemid 38580095)
-
(2004)
Journal of Medicinal Chemistry
, vol.47
, Issue.10
, pp. 2587-2598
-
-
Magnin, D.R.1
Robl, J.A.2
Sulsky, R.B.3
Augeri, D.J.4
Huang, Y.5
Simpkins, L.M.6
Taunk, P.C.7
Betebenner, D.A.8
Robertson, J.G.9
Abboa-Offei, B.E.10
Wang, A.11
Cap, M.12
Xin, L.13
Tao, L.14
Sitkoff, D.F.15
Malley, M.F.16
Gougoutas, J.Z.17
Khanna, A.18
Huang, Q.19
Han, S.-P.20
Parker, R.A.21
Hamann, L.G.22
more..
-
64
-
-
62149152364
-
Rational design and synthesis of potent and long-lasting glutamic acid-based dipeptidyl peptidase IV inhibitors
-
W.-T. Jiaang, T.-Y. Tsai, T. Hsu, and C.-T. Chen et al. Rational design and synthesis of potent and long-lasting glutamic acid-based dipeptidyl peptidase IV inhibitors Bioorg. Med. Chem. Lett. 19 2009 1908 1912
-
(2009)
Bioorg. Med. Chem. Lett.
, vol.19
, pp. 1908-1912
-
-
Jiaang, W.-T.1
Tsai, T.-Y.2
Hsu, T.3
Chen, C.-T.4
-
65
-
-
22744449063
-
Discovery and preclinical profile of saxagliptin (BMS-477118): A highly potent, long-acting, orally active dipeptidyl peptidase IV inhibitor for the treatment of type 2 diabetes
-
DOI 10.1021/jm050261p
-
D.J. Augeri, J.A. Robl, D.A. Betebenner, and D.R. Magnin et al. Discovery and preclinical profile of saxagliptin (BMS-477118): a highly potent, long-acting, orally active dipeptidyl peptidase IV inhibitor for the treatment of type 2 diabetes J. Med. Chem. 48 2005 5025 5037 (Pubitemid 41033142)
-
(2005)
Journal of Medicinal Chemistry
, vol.48
, Issue.15
, pp. 5025-5037
-
-
Augeri, D.J.1
Robl, J.A.2
Betebenner, D.A.3
Magnin, D.R.4
Khanna, A.5
Robertson, J.G.6
Wang, A.7
Simpkins, L.M.8
Taunk, P.9
Huang, Q.10
Han, S.-P.11
Abboa-Offei, B.12
Cap, M.13
Xin, L.14
Tao, L.15
Tozzo, E.16
Welzel, G.E.17
Egan, D.M.18
Marcinkeviciene, J.19
Chang, S.Y.20
Biller, S.A.21
Kirby, M.S.22
Parker, R.A.23
Hamann, L.G.24
more..
-
66
-
-
41649095697
-
Synthesis and structure-activity relationships of potent 4-fluoro-2-cyanopyrrolidine dipeptidyl peptidase IV inhibitors
-
DOI 10.1016/j.bmc.2008.01.016, PII S0968089608000333
-
H. Fukushima, A. Hiratate, M. Takahashi, and A. Mikami et al. Synthesis and structure-activity relationships of potent 4-fluoro-2-cyanopyrrolidine dipeptidyl peptidase IV inhibitors Bioorg. Med. Chem. 16 2008 4093 4106 (Pubitemid 351484008)
-
(2008)
Bioorganic and Medicinal Chemistry
, vol.16
, Issue.7
, pp. 4093-4106
-
-
Fukushima, H.1
Hiratate, A.2
Takahashi, M.3
Mikami, A.4
Saito-Hori, M.5
Munetomo, E.6
Kitano, K.7
Chonan, S.8
Saito, H.9
Suzuki, A.10
Takaoka, Y.11
Yamamoto, K.12
-
67
-
-
77954218296
-
(2S,4S)-1-[2-(1,1-Dimethyl-3-oxo-3-pyrrolidin-1-yl-propylamino)acetyl] -4-fluoro-pyrrolidine-2-carbonitrile: A potent, selective, and orally bioavailable dipeptide-derived inhibitor of dipeptidyl peptidase IV
-
C.-T. Chen, W.-T. Jiaang, T.-K. Yeh, and T.-Y. Tsai et al. (2S,4S)-1-[2-(1,1-Dimethyl-3-oxo-3-pyrrolidin-1-yl-propylamino)acetyl] -4-fluoro-pyrrolidine-2-carbonitrile: a potent, selective, and orally bioavailable dipeptide-derived inhibitor of dipeptidyl peptidase IV Bioorg. Med. Chem. Lett. 20 2010 3596 3600
-
(2010)
Bioorg. Med. Chem. Lett.
, vol.20
, pp. 3596-3600
-
-
Chen, C.-T.1
Jiaang, W.-T.2
Yeh, T.-K.3
Tsai, T.-Y.4
-
68
-
-
62549138270
-
Novel trans-2-aryl-cyclopropylamine analogues as potent and selective dipeptidyl peptidase IV inhibitors
-
T.-Y. Tsai, T. Hsu, C.-T. Chen, J.-H. Cheng, and T.-K. Yeh et al. Novel trans-2-aryl-cyclopropylamine analogues as potent and selective dipeptidyl peptidase IV inhibitors Bioorg. Med. Chem. 17 2009 2388 2399
-
(2009)
Bioorg. Med. Chem.
, vol.17
, pp. 2388-2399
-
-
Tsai, T.-Y.1
Hsu, T.2
Chen, C.-T.3
Cheng, J.-H.4
Yeh, T.-K.5
-
69
-
-
0038791485
-
-
Jan 9 (2003)WO 2003002531
-
C.D. Haffner, D.L. McDougald, A.S. Randhawa, S.M. Reister, et al., Fluoropyrrolidines as Ddipeptidyl Ppeptidase Iinhibitors, Jan 9 (2003)WO 2003002531.
-
Fluoropyrrolidines As Ddipeptidyl Ppeptidase Iinhibitors
-
-
Haffner, C.D.1
McDougald, D.L.2
Randhawa, A.S.3
Reister, S.M.4
-
70
-
-
47149101243
-
Discovery of conformationally rigid 3-azabicyclo[3.1.0]hexane-derived dipeptidyl peptidase-IV inhibitors
-
J.A. Sattigeri, M.M.S. Andappan, K. Kishore, and S. Thangathirupathy et al. Discovery of conformationally rigid 3-azabicyclo[3.1.0]hexane-derived dipeptidyl peptidase-IV inhibitors Bioorg. Med. Chem. Lett. 18 2008 4087 4091
-
(2008)
Bioorg. Med. Chem. Lett.
, vol.18
, pp. 4087-4091
-
-
Sattigeri, J.A.1
Andappan, M.M.S.2
Kishore, K.3
Thangathirupathy, S.4
-
71
-
-
74649085040
-
Design and synthesis of DPP-4 inhibitor for the treatment of type 2 diabetes
-
P.C. Tang, Z.G. Lin, Y. Wang, F.L. Yang, and Q. Wang Design and synthesis of DPP-4 inhibitor for the treatment of type 2 diabetes Chin. Chem. Lett. 21 2010 253 256
-
(2010)
Chin. Chem. Lett.
, vol.21
, pp. 253-256
-
-
Tang, P.C.1
Lin, Z.G.2
Wang, Y.3
Yang, F.L.4
Wang, Q.5
-
72
-
-
33847650981
-
Design and synthesis of long-acting inhibitors of dipeptidyl peptidase IV
-
DOI 10.1016/j.bmc.2007.01.033, PII S0968089607000594
-
T. Kondo, I. Sugimoto, T. Nekado, and K. Ochi et al. Design and synthesis of long-acting inhibitors of dipeptidyl peptidase IV Bioorg. Med. Chem. 15 2007 2715 2735 (Pubitemid 46367700)
-
(2007)
Bioorganic and Medicinal Chemistry
, vol.15
, Issue.7
, pp. 2715-2735
-
-
Kondo, T.1
Sugimoto, I.2
Nekado, T.3
Ochi, K.4
Ohtani, T.5
Tajima, Y.6
Yamamoto, S.7
Kawabata, K.8
Nakai, H.9
Toda, M.10
-
73
-
-
33745148202
-
Discovery, structure - Activity relationship, and pharmacological evaluation of (5-substituted-pyrrolidinyl-2-carbonyl)-2-cyanopyrrolidines as potent dipeptidyl peptidase IV inhibitors
-
DOI 10.1021/jm051283e
-
Z. Pei, X. Li, K. Longenecker, T.W. Von Geldern, and P.E. Wiedeman et al. Discovery, structure-activity relationship, and pharmacological evaluation of (5-substituted-pyrrolidinyl-2-carbonyl)-2-cyanopyrrolidines as potent dipeptidyl peptidase IV inhibitors J. Med. Chem. 49 2006 3520 3535 (Pubitemid 43902459)
-
(2006)
Journal of Medicinal Chemistry
, vol.49
, Issue.12
, pp. 3520-3535
-
-
Pei, Z.1
Li, X.2
Longenecker, K.3
Von Geldern, T.W.4
Wiedeman, P.E.5
Lubben, T.H.6
Zinker, B.A.7
Stewart, K.8
Ballaron, S.J.9
Stashko, M.A.10
Mika, A.K.11
Beno, D.W.A.12
Long, M.13
Wells, H.14
Kempf-Grote, A.J.15
Madar, D.J.16
McDermott, T.S.17
Bhagavatula, L.18
Fickes, M.G.19
Pireh, D.20
Solomon, L.R.21
Lake, M.R.22
Edalji, R.23
Fry, E.H.24
Sham, H.L.25
Trevillyan, J.M.26
more..
-
74
-
-
30444442517
-
2-[3-[2-[(25)-2-cyano-1-pyrrolidinyl]-2-oxoethylamino] -3-methyl-1-oxobutyl] -1,2,3,4-tetrahydroisoquinoline: A potent, selective, and orally bioavailable dipeptide-derived inhibitor of dipeptidyl peptidase IV
-
DOI 10.1021/jm0507781
-
W.T. Jiaang, H. Tsu, X. Chen, and C.T. Chen et al. 2-[3-[2-[(2S)-2-Cyano- 1-pyrrolidinyl]-2-oxoethylamino]-3-methyl-1-oxobutyl]-1,2,3,4- tetrahydroisoquinoline: a potent, selective, and orally bioavailable dipeptidederived inhibitor of dipeptidyl peptidase IV J. Med. Chem. 49 2006 373 380 (Pubitemid 43077350)
-
(2006)
Journal of Medicinal Chemistry
, vol.49
, Issue.1
, pp. 373-380
-
-
Tsu, H.1
Chen, X.2
Chen, C.-T.3
Lee, S.-J.4
Chang, C.-N.5
Kao, K.-H.6
Coumar, M.S.7
Yeh, Y.-T.8
Chien, C.-H.9
Wang, H.-S.10
Lin, K.-T.11
Chang, Y.-Y.12
Wu, S.-H.13
Chen, Y.-S.14
Lu, I.-L.15
Wu, S.-Y.16
Tsai, T.-Y.17
Chen, W.-C.18
Hsieh, H.-P.19
Chao, Y.-S.20
Jiaang, W.-T.21
more..
-
75
-
-
80655131901
-
Synthesis and pharmacological characterization of potent, selective, and orally bioavailable isoindoline class dipeptidyl peptidase IV inhibitors
-
N. Kato, M. Oka, T. Murase, M. Yoshida, and M. Sakairi et al. Synthesis and pharmacological characterization of potent, selective, and orally bioavailable isoindoline class dipeptidyl peptidase IV inhibitors Org. Med. Chem. Lett. 1 2011 1 7
-
(2011)
Org. Med. Chem. Lett.
, vol.1
, pp. 1-7
-
-
Kato, N.1
Oka, M.2
Murase, T.3
Yoshida, M.4
Sakairi, M.5
-
76
-
-
80655146931
-
Discovery and pharmacological characterization of N-[2-({2-[(2S)-2- cyanopyrrolidin-1-yl]-2-oxoethyl}amino)-2-methylpropyl]-2- methylpyrazolo[1,5-a] pyrimidine-6-carboxamide hydrochloride (anagliptin hydrochloride salt) as a potent and selective DPP-IV inhibitor
-
N. Kato, M. Oka, T. Murase, M. Yoshida, M. Sakairi, and S. Yamashita Discovery and pharmacological characterization of N-[2-({2-[(2S)-2- cyanopyrrolidin-1-yl]-2-oxoethyl}amino)-2-methylpropyl]-2- methylpyrazolo[1,5-a] pyrimidine-6-carboxamide hydrochloride (anagliptin hydrochloride salt) as a potent and selective DPP-IV inhibitor Bioorg. Med. Chem. 19 2011 7221 7227
-
(2011)
Bioorg. Med. Chem.
, vol.19
, pp. 7221-7227
-
-
Kato, N.1
Oka, M.2
Murase, T.3
Yoshida, M.4
Sakairi, M.5
Yamashita, S.6
-
77
-
-
15444376078
-
Fluoro-olefins as peptidomimetic inhibitors of dipeptidyl peptidases
-
DOI 10.1021/jm0495982
-
P. Van der Veken, K. Senten, and I. Kertesz et al. Fluoro-olefins as peptidomimetic inhibitors of dipeptidyl peptidases J. Med. Chem. 48 2005 1768 1780 (Pubitemid 40396310)
-
(2005)
Journal of Medicinal Chemistry
, vol.48
, Issue.6
, pp. 1768-1780
-
-
Van Der Veken, P.1
Senten, K.2
Kertesz, I.3
De Meester, I.4
Lambeir, A.-M.5
Maes, M.-B.6
Scharpe, S.7
Haemers, A.8
Augustyns, K.9
-
78
-
-
0032564474
-
Inhibition of dipeptidyl peptidase IV by fluoroolefin-containing N-peptidyl-O-hydroxylamine peptidomimetics
-
J. Lin, P.J. Toscano, and J.T. Welch Inhibition of dipeptidyl peptidase IV by fluoroolefin-containing N-peptidyl-O-hydroxylamine peptidomimetics Proc. Natl. Acad. Sci. U.S.A. 95 1998 14020 14024
-
(1998)
Proc. Natl. Acad. Sci. U.S.A.
, vol.95
, pp. 14020-14024
-
-
Lin, J.1
Toscano, P.J.2
Welch, J.T.3
-
79
-
-
0037449356
-
Inhibition of dipeptidyl peptidase IV (DPP IV) by 2-(2-amino-1-fluoro- propylidene)-cyclopentanecarbonitrile, a fluoroolefin containing peptidomimetic
-
DOI 10.1016/S0968-0896(02)00384-X, PII S096808960200384X
-
K. Zhao, D.S. Lim, T. Funaki, and J.T. Welch Inhibition of dipeptidyl peptidase IV (DPP IV) by 2-(2-amino-1-fluoro-propylidene)- cyclopentanecarbonitrile, a fluoroolefin containing peptidomimetic Bioorg. Med. Chem. 11 2003 207 215 (Pubitemid 35418263)
-
(2003)
Bioorganic and Medicinal Chemistry
, vol.11
, Issue.2
, pp. 207-215
-
-
Zhao, K.1
Lim, D.S.2
Funaki, T.3
Welch, J.T.4
-
80
-
-
0029946714
-
Structure-activity relationships of boronic acid inhibitors of dipeptidyl peptidase IV. 1. Variation of the P2 position of Xaa-boroPro dipeptides
-
J. Coutts, T.A. Kelly, R.J. Snow, and C.A. Kennedy et al. Structure-activity relationships of boronic acid inhibitors of dipeptidyl peptidase IV. 1. Variation of the P2 position of Xaa-boroPro dipeptides J. Med. Chem. 39 1996 2087 2094
-
(1996)
J. Med. Chem.
, vol.39
, pp. 2087-2094
-
-
Coutts, J.1
Kelly, T.A.2
Snow, R.J.3
Kennedy, C.A.4
-
81
-
-
0033602521
-
Structure-activity relationship of diaryl phosphonate esters as potent irreversible dipeptidyl peptidase IV inhibitors
-
DOI 10.1021/jm981033g
-
Belyaev, X. Zhang, K. Augustyns, and A.-M. Lambeir et al. Structure-activity relationship of diaryl phosphonate esters as potent irreversible dipeptidyl peptidase IV inhibitors J. Med. Chem. 42 1999 1041 1052 (Pubitemid 29153433)
-
(1999)
Journal of Medicinal Chemistry
, vol.42
, Issue.6
, pp. 1041-1052
-
-
Belyaev, A.1
Zhang, X.2
Augustyns, K.3
Lambeir, A.-M.4
De Meester, I.5
Vedernikova, I.6
Scharpe, S.7
Haemers, A.8
-
82
-
-
0141786949
-
Rapid parallel synthesis of dipeptide diphenyl phosphonate esters as inhibitors of dipeptidyl peptidases
-
DOI 10.1021/cc020096o
-
K. Senten, L. Daniels, and P. Van der Veken et al. Rapid parallel synthesis of dipeptide diphenyl phosphonate esters as inhibitors of dipeptidyl peptidases J. Comb. Chem. 5 2003 336 344 (Pubitemid 37140580)
-
(2003)
Journal of Combinatorial Chemistry
, vol.5
, Issue.3
, pp. 336-344
-
-
Senten, K.1
Daniels, L.2
Van Der Veken, P.3
De Meester, I.4
Lambeir, A.-M.5
Scharpe, S.6
Haemers, A.7
Augustyns, K.8
-
83
-
-
79953792552
-
Pro-Soft Val-boroPro: A strategy for enhancing in vivo performance of boronic acid inhibitors of serine proteases
-
W. William, S.E. Bachovchin, J.H. Poplawski, and D.G. Lai et al. Pro-Soft Val-boroPro: a strategy for enhancing in vivo performance of boronic acid inhibitors of serine proteases J. Med. Chem. 54 2011 2022 2028
-
(2011)
J. Med. Chem.
, vol.54
, pp. 2022-2028
-
-
William, W.1
Bachovchin, S.E.2
Poplawski, J.H.3
Lai, D.G.4
-
84
-
-
0001387705
-
Boronic acid inhibitors of dipeptidyl peptidase IV: A new class of immunosuppressive
-
R.J. Snow, and W.W. Bachovchin Boronic acid inhibitors of dipeptidyl peptidase IV: a new class of immunosuppressive Adv. Med. Chem. 3 1995 149 177
-
(1995)
Adv. Med. Chem.
, vol.3
, pp. 149-177
-
-
Snow, R.J.1
Bachovchin, W.W.2
-
85
-
-
0027852277
-
Immunosuppressive boronic acid dipeptides: Correlation between conformation and activity
-
T.A. Kelly, J. Adams, W.W. Bachovchin, and R.W. Barton et al. Immunosuppressiveboronic acid dipeptides: correlation between conformation and activity J. Am. Chem. Soc. 115 1993 12637 12638 (Pubitemid 24077513)
-
(1993)
Journal of the American Chemical Society
, vol.115
, Issue.26
, pp. 12637-12638
-
-
Kelly, T.A.1
Adams, J.2
Bachovchin, W.W.3
Barton, R.W.4
Campbell, S.J.5
Coutts, S.J.6
Kennedy, C.A.7
Snow, R.J.8
-
86
-
-
0028566173
-
Studies on proline boronic acid dipeptide inhibitors of dipeptidyl peptidase IV: Identification of a cyclic species containing a B-N bond
-
R.J. Snow, W.W. Bachovchin, R.W. Barton, and S.J. Campbell et al. Studies on proline boronic acid dipeptide inhibitors of dipeptidyl peptidase IV: identification of a cyclic species containing a B-N bond J. Am. Chem. Soc. 116 1994 10860 10869
-
(1994)
J. Am. Chem. Soc.
, vol.116
, pp. 10860-10869
-
-
Snow, R.J.1
Bachovchin, W.W.2
Barton, R.W.3
Campbell, S.J.4
-
87
-
-
0028075874
-
Dipeptide phosphonates as inhibitors of dipeptidyl peptidase IV
-
DOI 10.1021/jm00049a016
-
B. Boduszek, J. Oleksyszyn, C. Kam, and J. Selzler et al. Dipeptide phosphonates as inhibitors of dipeptidyl peptidase IV J. Med. Chem. 37 1994 3969 3976 (Pubitemid 24379686)
-
(1994)
Journal of Medicinal Chemistry
, vol.37
, Issue.23
, pp. 3969-3976
-
-
Boduszek, B.1
Oleksyszyn, J.2
Kam, C.-M.3
Selzler, J.4
Smith, R.E.5
Powers, J.C.6
-
88
-
-
0242267905
-
Design, Synthesis, and SAR of Potent and Selective Dipeptide-Derived Inhibitors for Dipeptidyl Peptidases
-
K. Senten, P. Van der Veken, I. De Meester, and A.-M. Lambeir et al. Design, synthesis, and SAR of potent and selective dipeptide-derived inhibitors for dipeptidyl peptidases J. Med. Chem. 46 2003 5005 5014 (Pubitemid 37352037)
-
(2003)
Journal of Medicinal Chemistry
, vol.46
, Issue.23
, pp. 5005-5014
-
-
Senten, K.1
Van Der Veken, P.2
De Meester, I.3
Lambeir, A.-M.4
Scharpe, S.5
Haemers, A.6
Augustyns, K.7
-
89
-
-
0038791462
-
Dipeptidyl peptidase IV inhibitors
-
D.M. Evans Dipeptidyl peptidase IV inhibitors Idrugs 5 2002 577 585 (Pubitemid 37214117)
-
(2002)
IDrugs
, vol.5
, Issue.6
, pp. 577-585
-
-
Evans, D.M.1
-
90
-
-
0026166647
-
Dipeptidyl peptidase IV in the immune system. Effects of specific enzyme inhibitors on activity of dipeptidyl peptidase IV and proliferation of human lymphocytes
-
E. Schoen, I. Norn, and H.U. Demuth et al. Dipeptidyl peptidase IV in the immune system. Effects of specific enzyme inhibitors on activity of dipeptidyl peptidase IV and proliferation of human lymphocytes Biol. Chem. Hoppe-Seyler 372 1991 305 311
-
(1991)
Biol. Chem. Hoppe-Seyler
, vol.372
, pp. 305-311
-
-
Schoen, E.1
Norn, I.2
Demuth, H.U.3
-
91
-
-
0346252638
-
4-Amino cyclohexylglycine analogues as potent dipeptidyl peptidase IV inhibitors
-
DOI 10.1016/j.bmcl.2003.10.016
-
E.R. Parmee, J. He, A. Mastracchio, S.D. Edmondson, and L. Colwell et al. 4-Amino cyclohexylglycine analogues as potent dipeptidyl peptidase IV inhibitors Bioorg. Med. Chem. Lett. 14 2004 43 46 (Pubitemid 38016208)
-
(2004)
Bioorganic and Medicinal Chemistry Letters
, vol.14
, Issue.1
, pp. 43-46
-
-
Parmee, E.R.1
He, J.2
Mastracchio, A.3
Edmondson, S.D.4
Colwell, L.5
Eiermann, G.6
Feeney, W.P.7
Habulihaz, B.8
He, H.9
Kilburn, R.10
Leiting, B.11
Lyons, K.12
Marsilio, F.13
Patel, R.A.14
Petrov, A.15
Di Salvo, J.16
Wu, J.K.17
Thornberry, N.A.18
Weber, A.E.19
-
92
-
-
38949172401
-
Design and synthesis of DPP-IV inhibitors lacking the electrophilic nitrile group
-
DOI 10.1016/j.bmc.2007.11.031, PII S0968089607010000
-
Y. Kondo, T. Nekado, I. Sugimoto, and K. Ochi et al. Design and synthesis of DPP-IV inhibitors lacking the electrophilic nitrile group Bioorg. Med. Chem. 16 2008 1613 1631 (Pubitemid 351226600)
-
(2008)
Bioorganic and Medicinal Chemistry
, vol.16
, Issue.4
, pp. 1613-1631
-
-
Kondo, T.1
Nekado, T.2
Sugimoto, I.3
Ochi, K.4
Takai, S.5
Kinoshita, A.6
Hatayama, A.7
Yamamoto, S.8
Kishikawa, K.9
Nakai, H.10
Toda, M.11
-
93
-
-
33646033123
-
[(S)-γ-(Arylamino)prolyl]thiazolidine compounds as a novel series of potent and stable DPP-IV inhibitors
-
H. Sakashita, F. Akahoshi, H. Kitajima, R. Tsutsumiuchi, and Y. Hayashi [(S)-γ-(Arylamino)prolyl]thiazolidine compounds as a novel series of potent and stable DPP-IV inhibitors Bioorg. Med. Chem. 14 2006 3662 3671
-
(2006)
Bioorg. Med. Chem.
, vol.14
, pp. 3662-3671
-
-
Sakashita, H.1
Akahoshi, F.2
Kitajima, H.3
Tsutsumiuchi, R.4
Hayashi, Y.5
-
94
-
-
84864436192
-
Fused bicyclic heteroarylpiperazine-substituted L-prolylthiazolidines as highly potent DPP-4 inhibitors lacking the electrophilic nitrile group
-
T. Yoshida, F. Akahoshi, H. Sakashita, and S. Sonda et al. Fused bicyclic heteroarylpiperazine-substituted L-prolylthiazolidines as highly potent DPP-4 inhibitors lacking the electrophilic nitrile group Bioorg. Med. Chem. 20 2012 5033 5041
-
(2012)
Bioorg. Med. Chem.
, vol.20
, pp. 5033-5041
-
-
Yoshida, T.1
Akahoshi, F.2
Sakashita, H.3
Sonda, S.4
-
95
-
-
84866353450
-
Discovery and preclinical profile of teneligliptin (3-[(2S,4S)-4-[4-(3- methyl-1-phenyl-1H-pyrazol-5-yl)piperazin-1-yl]pyrrolidin-2-ylcarbonyl] thiazolidine): A highly potent, selective, long-lasting and orally active dipeptidyl peptidase IV inhibitor for the treatment of type 2 diabetes
-
T. Yoshida, F. Akahoshi, and H. Sakashita et al. Discovery and preclinical profile of teneligliptin (3-[(2S,4S)-4-[4-(3-methyl-1-phenyl-1H- pyrazol-5-yl)piperazin-1-yl]pyrrolidin-2-ylcarbonyl]thiazolidine): a highly potent, selective, long-lasting and orally active dipeptidyl peptidase IV inhibitor for the treatment of type 2 diabetes Bioorganic Med. Chem. 20 2012 5705 5719
-
(2012)
Bioorganic Med. Chem.
, vol.20
, pp. 5705-5719
-
-
Yoshida, T.1
Akahoshi, F.2
Sakashita, H.3
-
96
-
-
84877594042
-
Teneligliptin: A DPP-4 inhibitor for the treatment of type 2 diabetes
-
Miyako Kishimoto Teneligliptin: a DPP-4 inhibitor for the treatment of type 2 diabetes Diab. Metab. Synd. Obes. Target. Ther. 6 2013 187 195
-
(2013)
Diab. Metab. Synd. Obes. Target. Ther.
, vol.6
, pp. 187-195
-
-
Kishimoto, M.1
-
97
-
-
84862829036
-
Design, synthesis and primary activity of thiomorpholine derivatives as DPP-IV inhibitors
-
H.H. Huang, B. Han, J.L. Liu, and Y. Huan et al. Design, synthesis and primary activity of thiomorpholine derivatives as DPP-IV inhibitors Chin. Chem. Lett. 23 2012 297 300
-
(2012)
Chin. Chem. Lett.
, vol.23
, pp. 297-300
-
-
Huang, H.H.1
Han, B.2
Liu, J.L.3
Huan, Y.4
-
98
-
-
10744233045
-
Fluoropyrrolidine amides as dipeptidyl peptidase IV inhibitors
-
DOI 10.1016/j.bmcl.2003.12.040
-
C.G. Caldwell, P. Chen, J. He, and E.R. Parmee et al. Fluoropyrrolidine amides as dipeptidyl peptidase IV inhibitors Bioorg. Med. Chem. Lett. 14 2004 1265 1268 (Pubitemid 38229869)
-
(2004)
Bioorganic and Medicinal Chemistry Letters
, vol.14
, Issue.5
, pp. 1265-1268
-
-
Caldwell, C.G.1
Chen, P.2
He, J.3
Parmee, E.R.4
Leiting, B.5
Marsilio, F.6
Patel, R.A.7
Wu, J.K.8
Eiermann, G.J.9
Petrov, A.10
He, H.11
Lyons, K.A.12
Thornberry, N.A.13
Weber, A.E.14
-
99
-
-
0030965178
-
Pyrrolidides: Synthesis and structure-activity relationship as inhibitors of dipeptidyl peptidase IV
-
DOI 10.1016/S0223-5234(97)89082-4
-
K.J.L. Augustyns, A.M. Lambeir, M. Borloo, and I. De Meester et al. Pyrrolidides: synthesis and structure-activity relationship as inhibitors of dipeptidyl peptidase IV Eur. J. Med. Chem. 32 1997 301 309 (Pubitemid 27220261)
-
(1997)
European Journal of Medicinal Chemistry
, vol.32
, Issue.4
, pp. 301-309
-
-
Augustyns, K.J.L.1
Lambeir, A.M.2
Borloo, M.3
De Meester, I.4
Vedernikova, I.5
Vanhoof, G.6
Hendriks, D.7
Scharpe, S.8
Haemers, A.9
-
100
-
-
33745151060
-
(2S,3S)-3-amino-4-(3,3-difluoropyrrolidin-1-yl)-N,N-dimethyl-4-oxo-2-(4- [1, 2,4]triazolo[1,5-a]-pyridin-6-ylphenyl)butanamide: A selective α-amino amide dipeptidyl peptidase IV inhibitor for the treatment of type 2 diabetes
-
DOI 10.1021/jm060015t
-
S.D. Edmondson, A. Mastracchio, R.J. Mathvink, and J. He et al. (2S,3S)-3-Amino-4-(3,3-difluoropyrrolidin-1-yl)-N,N-dimethyl-4-oxo-2-(4-[1,2,4] triazolo[1,5-a]- pyridin-6-ylphenyl)butanamide: a selective α-amino amide dpeptidyl peptidase IV inhibitor for the treatment of type 2 diabetes J. Med. Chem. 49 2006 3614 3627 (Pubitemid 43902466)
-
(2006)
Journal of Medicinal Chemistry
, vol.49
, Issue.12
, pp. 3614-3627
-
-
Edmondson, S.D.1
Mastracchio, A.2
Mathvink, R.J.3
He, J.4
Harper, B.5
Park, Y.-J.6
Beconi, M.7
Di Salvo, J.8
Eiermann, G.J.9
He, H.10
Leiting, B.11
Leone, J.F.12
Levorse, D.A.13
Lyons, K.14
Patel, R.A.15
Patel, S.B.16
Petrov, A.17
Scapin, G.18
Shang, J.19
Roy, R.S.20
Smith, A.21
Wu, J.K.22
Xu, S.23
Zhu, B.24
Thornberry, N.A.25
Weber, A.E.26
more..
-
101
-
-
34548812342
-
4-Arylcyclohexylalanine analogs as potent, selective, and orally active inhibitors of dipeptidyl peptidase IV
-
DOI 10.1016/j.bmcl.2007.08.049, PII S0960894X07010050
-
D.E. Kaelin, A.L. Smenton, G.J. Eiermann, and H. He et al. 4-Arylcyclohexylalanine analogs as potent, selective, and orally active inhibitors of dipeptidyl peptidase IV Bioorg. Med. Chem. Lett. 17 2007 5806 5811 (Pubitemid 47446228)
-
(2007)
Bioorganic and Medicinal Chemistry Letters
, vol.17
, Issue.21
, pp. 5806-5811
-
-
Kaelin, D.E.1
Smenton, A.L.2
Eiermann, G.J.3
He, H.4
Leiting, B.5
Lyons, K.A.6
Patel, R.A.7
Patel, S.B.8
Petrov, A.9
Scapin, G.10
Wu, J.K.11
Thornberry, N.A.12
Weber, A.E.13
Duffy, J.L.14
-
102
-
-
61849146383
-
(3,3-Difluoro-pyrrolidin-1-yl)-[(2S,4S)-(4-(4-pyrimidin-2-yl-piperazin-1- yl)-pyrrolidin-2-yl] methanone: A potent, selective, orally active dipeptidyl peptidase IV inhibitor
-
M.J. Ammirati, K.M. Andrews, D.D. Boyer, and A.M. Brodeur et al. (3,3-Difluoro-pyrrolidin-1-yl)-[(2S,4S)-(4-(4-pyrimidin-2-yl-piperazin-1-yl) -pyrrolidin-2-yl] methanone: a potent, selective, orally active dipeptidyl peptidase IV inhibitor Bioorg. Med. Chem. Lett. 19 2009 1991 1995
-
(2009)
Bioorg. Med. Chem. Lett.
, vol.19
, pp. 1991-1995
-
-
Ammirati, M.J.1
Andrews, K.M.2
Boyer, D.D.3
Brodeur, A.M.4
-
103
-
-
84872336284
-
Design, synthesis, structure-activity relationships, and docking studies of 1-(γ-1,2,3-triazol substituted prolyl)-(S)-3,3-difluoropyrrolidines as a novel series of potent and selective dipeptidyl peptidase-4 inhibitors
-
L. Zhang, M. Su, J. Li, and X. Ji et al. Design, synthesis, structure-activity relationships, and docking studies of 1-(γ-1,2,3- triazol substituted prolyl)-(S)-3,3-difluoropyrrolidines as a novel series of potent and selective dipeptidyl peptidase-4 inhibitors Chem. Biol. Drug. Des. 81 2013 198 207
-
(2013)
Chem. Biol. Drug. Des.
, vol.81
, pp. 198-207
-
-
Zhang, L.1
Su, M.2
Li, J.3
Ji, X.4
-
104
-
-
5144231567
-
Ketopyrrolidines and ketoazetidines as potent dipeptidyl peptidase IV (DPP IV) inhibitors
-
DOI 10.1016/j.bmcl.2004.08.057, PII S0960894X04010868
-
D. Ferraris, Y.S. Ko, D. Calvin, and T. Chiou et al. Ketopyrrolidines and ketoazetidines as potent dipeptidyl peptidase IV (DPP IV) inhibitors Bioorg. Med. Chem. Lett. 14 2004 5579 5583 (Pubitemid 39346349)
-
(2004)
Bioorganic and Medicinal Chemistry Letters
, vol.14
, Issue.22
, pp. 5579-5583
-
-
Ferraris, D.1
Ko, Y.-S.2
Calvin, D.3
Chiou, T.4
Lautar, S.5
Thomas, B.6
Wozniak, K.7
Rojas, C.8
Kalish, V.9
Belyakov, S.10
-
105
-
-
4544253908
-
Discovery of potent and selective β-homophenylalanine based dipeptidyl peptidase IV inhibitors
-
DOI 10.1016/j.bmcl.2004.06.099, PII S0960894X04008406
-
J. Xu, H.O. Ok, E.J. Gonzalez, and L.F. Colwell Jr. et al. Discovery of potent and selective β-homophenylalanine based dipeptidyl peptidase IV inhibitors Bioorg. Med. Chem. Lett. 14 2004 4759 4762 (Pubitemid 39490304)
-
(2004)
Bioorganic and Medicinal Chemistry Letters
, vol.14
, Issue.18
, pp. 4759-4762
-
-
Xu, J.1
Ok, H.O.2
Gonzalez, E.J.3
Colwell Jr., L.F.4
Habulihaz, B.5
He, H.6
Leiting, B.7
Lyons, K.A.8
Marsilio, F.9
Patel, R.A.10
Wu, J.K.11
Thornberry, N.A.12
Weber, A.E.13
Parmee, E.R.14
-
106
-
-
4544376832
-
Potent and selective proline derived dipeptidyl peptidase IV inhibitors
-
DOI 10.1016/j.bmcl.2004.07.056, PII S0960894X04009576
-
S.D. Edmondson, A. Mastracchio, M. Beconi, and L.F. Colwell Jr. et al. Potent and selective proline derived dipeptidyl peptidase IV inhibitors Bioorg. Med. Chem. Lett. 14 2004 5151 5155 (Pubitemid 39233384)
-
(2004)
Bioorganic and Medicinal Chemistry Letters
, vol.14
, Issue.20
, pp. 5151-5155
-
-
Edmondson, S.D.1
Mastracchio, A.2
Beconi, M.3
Colwell Jr., L.F.4
Habulihaz, B.5
He, H.6
Kumar, S.7
Leiting, B.8
Lyons, K.A.9
Mao, A.10
Marsilio, F.11
Patel, R.A.12
Wu, J.K.13
Zhu, L.14
Thornberry, N.A.15
Weber, A.E.16
Parmee, E.R.17
-
107
-
-
4544373020
-
Substituted piperazines as novel dipeptidyl peptidase IV inhibitors
-
DOI 10.1016/j.bmcl.2004.06.065, PII S0960894X0400839X
-
L.L. Brockunier, J. He, L.F. Colwell Jr., and B. Habulihaz et al. Potent and selective proline derived dipeptidyl peptidase IV inhibitors Bioorg. Med. Chem. Lett. 14 2004 4763 4766 (Pubitemid 39490305)
-
(2004)
Bioorganic and Medicinal Chemistry Letters
, vol.14
, Issue.18
, pp. 4763-4766
-
-
Brockunier, L.L.1
He, J.2
Colwell Jr., L.F.3
Habulihaz, B.4
He, H.5
Leiting, B.6
Lyons, K.A.7
Marsilio, F.8
Patel, R.A.9
Teffera, Y.10
Wu, J.K.11
Thornberry, N.A.12
Weber, A.E.13
Parmee, E.R.14
-
108
-
-
32044465048
-
The reversed binding of β-phenethylamine inhibitors of DPP-IV: X-ray structures and properties of novel fragment and elaborated inhibitors
-
DOI 10.1016/j.bmcl.2005.11.103, PII S0960894X05015441
-
S. Nordhoff, S. Cerezo-Galvez, A. Feurer, and O. Hill et al. The reversed binding of β-phenethylamine inhibitors of DPP-IV: X-ray structures and properties of novel fragment and elaborated inhibitors Bioorg. Med. Chem. Lett. 16 2006 1744 1748 (Pubitemid 43197558)
-
(2006)
Bioorganic and Medicinal Chemistry Letters
, vol.16
, Issue.6
, pp. 1744-1748
-
-
Nordhoff, S.1
Cerezo-Galvez, S.2
Feurer, A.3
Hill, O.4
Matassa, V.G.5
Metz, G.6
Rummey, C.7
Thiemann, M.8
Edwards, P.J.9
-
109
-
-
19944427998
-
(2R)-4-Oxo-4-[3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a] pyrazin-7(8H)-yl]-1-(2,4,5-trifluorophenyl)butan-2-amine: A potent, orally active dipeptidyl peptidase IV inhibitor for the treatment of type 2 diabetes
-
DOI 10.1021/jm0493156
-
D. Kim, L. Wang, M. Beconi, and G.J. Eiermann et al. (2R)-4-Oxo-4-[3- (trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin- 7(8H)-yl]-1-(2,4,5- trifluorophenyl)butan-2-amine: a potent, orally active dipeptidyl peptidase iv inhibitor for the treatment of type 2 Diabetes J. Med. Chem. 48 2005 141 151 (Pubitemid 40105255)
-
(2005)
Journal of Medicinal Chemistry
, vol.48
, Issue.1
, pp. 141-151
-
-
Kim, D.1
Wang, L.2
Beconi, M.3
Eiermann, G.J.4
Fisher, M.H.5
He, H.6
Hickey, G.J.7
Kowalchick, J.E.8
Leiting, B.9
Lyons, K.10
Marsilio, F.11
McCann, M.E.12
Patel, R.A.13
Petrov, A.14
Scapin, G.15
Patel, S.B.16
Roy, R.S.17
Wu, J.K.18
Wyvratt, M.J.19
Zhang, B.B.20
Zhu, L.21
Thornberry, N.A.22
Weber, A.E.23
more..
-
110
-
-
34249330949
-
Triazolopiperazine-amides as dipeptidyl peptidase IV inhibitors: Close analogs of JANUVIA™ (sitagliptin phosphate)
-
DOI 10.1016/j.bmcl.2007.03.098, PII S0960894X07004167
-
D. Kim, J.E. Kowalchick, S.D. Edmondson, and A. Mastracchio et al. Triazolopiperazine-amides as dipeptidyl peptidase IV inhibitors: close analogs of JANUVIA™ (sitagliptin phosphate) Bioorg. Med. Chem. Lett. 17 2007 3373 3377 (Pubitemid 46819031)
-
(2007)
Bioorganic and Medicinal Chemistry Letters
, vol.17
, Issue.12
, pp. 3373-3377
-
-
Kim, D.1
Kowalchick, J.E.2
Edmondson, S.D.3
Mastracchio, A.4
Xu, J.5
Eiermann, G.J.6
Leiting, B.7
Wu, J.K.8
Pryor, K.D.9
Patel, R.A.10
He, H.11
Lyons, K.A.12
Thornberry, N.A.13
Weber, A.E.14
-
111
-
-
79952364204
-
Discovery of potent dipeptidyl peptidase IV inhibitors derived from β-aminoamides bearing substituted [1,2,3]-triazolopiperidines for the treatment of type 2 diabetes
-
Y. Chen, Z. Shan, M. Peng, and H. Fan et al. Discovery of potent dipeptidyl peptidase IV inhibitors derived from β-aminoamides bearing substituted [1,2,3]-triazolopiperidines for the treatment of type 2 diabetes Bioorg. Med. Chem. Lett. 21 2011 1731 1735
-
(2011)
Bioorg. Med. Chem. Lett.
, vol.21
, pp. 1731-1735
-
-
Chen, Y.1
Shan, Z.2
Peng, M.3
Fan, H.4
-
112
-
-
77957837734
-
Synthesis, biological assay in vitro and molecular docking studies of new imidazopyrazinone derivatives as potential dipeptidyl peptidase IV inhibitors
-
P. Lu, G. Song, Y. Zhu, and S. Xia et al. Synthesis, biological assay in vitro and molecular docking studies of new imidazopyrazinone derivatives as potential dipeptidyl peptidase IV inhibitors Eur. J. Med. Chem. 45 2010 4953 4962
-
(2010)
Eur. J. Med. Chem.
, vol.45
, pp. 4953-4962
-
-
Lu, P.1
Song, G.2
Zhu, Y.3
Xia, S.4
-
113
-
-
79957865337
-
Discovery of DA-1229: A potent, long acting dipeptidyl peptidase-4 inhibitor for the treatment of type 2 diabetes
-
B.J. Lee, H.J. Kim, W.Y. Kwak, and J.P. Min et al. Discovery of DA-1229: a potent, long acting dipeptidyl peptidase-4 inhibitor for the treatment of type 2 diabetes Bioorg. Med. Chem. Lett. 21 2011 3809 3812
-
(2011)
Bioorg. Med. Chem. Lett.
, vol.21
, pp. 3809-3812
-
-
Lee, B.J.1
Kim, H.J.2
Kwak, W.Y.3
Min, J.P.4
-
114
-
-
79951722945
-
Discovery of β-aminoacyl containing thiazolidine derivatives as potent and selective dipeptidyl peptidase IV inhibitors
-
J.H. Ahn, S.S. Kim, W.S. Park, and S.K. Kang et al. Discovery of β-aminoacyl containing thiazolidine derivatives as potent and selective dipeptidyl peptidase IV inhibitors Bioorg. Med. Chem. Lett. 21 2011 1366 1370
-
(2011)
Bioorg. Med. Chem. Lett.
, vol.21
, pp. 1366-1370
-
-
Ahn, J.H.1
Kim, S.S.2
Park, W.S.3
Kang, S.K.4
-
115
-
-
20244380466
-
Dipeptidyl peptidase IV inhibitors derived from β- aminoacylpiperidines bearing a fused thiazole, oxazole, isoxazole, or pyrazole
-
DOI 10.1016/j.bmcl.2005.03.012
-
W.T. Ashton, R.M. Sisco, H. Dong, and K.A. Lyons et al. Dipeptidyl peptidase IV inhibitors derived from β-aminoacylpiperidines bearing a fused thiazole, oxazole, isoxazole, or pyrazole Bioorg. Med. Chem. Lett. 15 2005 2253 2258 (Pubitemid 40528402)
-
(2005)
Bioorganic and Medicinal Chemistry Letters
, vol.15
, Issue.9
, pp. 2253-2258
-
-
Ashton, W.T.1
Sisco, R.M.2
Dong, H.3
Lyons, K.A.4
He, H.5
Doss, G.A.6
Leiting, B.7
Patel, R.A.8
Wu, J.K.9
Marsilio, F.10
Thornberry, N.A.11
Weber, A.E.12
-
116
-
-
34548833898
-
Imidazopiperidine amides as dipeptidyl peptidase IV inhibitors for the treatment of diabetes
-
DOI 10.1016/j.bmcl.2007.08.030, PII S0960894X07009717
-
P. Chen, C.G. Caldwell, R.J. Mathvink, and B. Leiting et al. Imidazopiperidine amides as dipeptidyl peptidase IV inhibitors for the treatment of diabetes Bioorg. Med. Chem. Lett. 17 2007 5853 5857 (Pubitemid 47446221)
-
(2007)
Bioorganic and Medicinal Chemistry Letters
, vol.17
, Issue.21
, pp. 5853-5857
-
-
Chen, P.1
Caldwell, C.G.2
Mathvink, R.J.3
Leiting, B.4
Marsilio, F.5
Patel, R.A.6
Wu, J.K.7
He, H.8
Lyons, K.A.9
Thornberry, N.A.10
Weber, A.E.11
-
117
-
-
67649922154
-
Discovery of β-homophenylalanine based pyrrolidin-2-ylmethyl amides and sulfonamides as highly potent and selective inhibitors of dipeptidyl peptidase IV
-
S. Nordhoff, S. Cerezo-Galvez, H. Deppe, and O. Hill et al. Discovery of β-homophenylalanine based pyrrolidin-2-ylmethyl amides and sulfonamides as highly potent and selective inhibitors of dipeptidyl peptidase IV Bioorg. Med. Chem. Lett. 19 2009 4201 4203
-
(2009)
Bioorg. Med. Chem. Lett.
, vol.19
, pp. 4201-4203
-
-
Nordhoff, S.1
Cerezo-Galvez, S.2
Deppe, H.3
Hill, O.4
-
118
-
-
67651087356
-
From lead to preclinical candidate: Optimization of β- homophenylalanine based inhibitors of dipeptidyl peptidase IV
-
S. Nordhoff, M. Lopez-Canet, B. Hoffmann-Enger, and S. Bulat et al. From lead to preclinical candidate: optimization of β-homophenylalanine based inhibitors of dipeptidyl peptidase IV Bioorg. Med. Chem. Lett. 19 2009 4818 4823
-
(2009)
Bioorg. Med. Chem. Lett.
, vol.19
, pp. 4818-4823
-
-
Nordhoff, S.1
Lopez-Canet, M.2
Hoffmann-Enger, B.3
Bulat, S.4
-
119
-
-
71049150927
-
The design of potent and selective inhibitors of DPP-4: Optimization of ADME properties by amide replacements
-
S. Nordhoff, S. Bulat, S. Cerezo-Galvez, and O. Hill et al. The design of potent and selective inhibitors of DPP-4: optimization of ADME properties by amide replacements Bioorg. Med. Chem. Lett. 19 2009 6340 6345
-
(2009)
Bioorg. Med. Chem. Lett.
, vol.19
, pp. 6340-6345
-
-
Nordhoff, S.1
Bulat, S.2
Cerezo-Galvez, S.3
Hill, O.4
-
120
-
-
13944279484
-
Synthesis and evaluation of pyrazolidine derivatives as dipeptidyl peptidase IV (DP-IV) inhibitors
-
DOI 10.1016/j.bmcl.2005.01.020
-
J.H. Ahn, J.A. Kim, H.M. Kim, and H.M. Kwon et al. Synthesis and evaluation of pyrazolidine derivatives as dipeptidyl peptidase IV (DP-IV) inhibitors Bioorg. Med. Chem. Lett. 15 2005 1337 1340 (Pubitemid 40268987)
-
(2005)
Bioorganic and Medicinal Chemistry Letters
, vol.15
, Issue.5
, pp. 1337-1340
-
-
Ahn, J.H.1
Kim, J.A.2
Kim, H.-M.3
Kwon, H.-M.4
Huh, S.-C.5
Rhee, S.D.6
Kim, K.R.7
Yang, S.-D.8
Park, S.-D.9
Lee, J.M.10
Kim, S.S.11
Cheon, H.G.12
-
121
-
-
24944548675
-
Pyrazolidine derivatives with heteroaryl urea as dipeptidyl peptidase IV inhibitors
-
DOI 10.1248/cpb.53.1048
-
J.H. Ahn, S.H. Jung, J.A. Kim, and S.B. Song et al. Pyrazolidine derivatives with heteroaryl urea as dipeptidyl peptidase IV inhibitors Chem. Pharm. Bull. 53 2005 1048 1050 (Pubitemid 41327707)
-
(2005)
Chemical and Pharmaceutical Bulletin
, vol.53
, Issue.8
, pp. 1048-1050
-
-
Ahn, J.H.1
Jung, S.H.2
Kim, J.A.3
Song, S.B.4
Kwon, S.J.5
Kim, K.R.6
Rhee, S.D.7
Park, S.-D.8
Lee, J.M.9
Kim, S.S.10
Cheon, H.G.11
-
122
-
-
34047141757
-
Synthesis, biological evaluation and structural determination of β-aminoacyl-containing cyclic hydrazine derivatives as dipeptidyl peptidase IV (DPP-IV) inhibitors
-
DOI 10.1016/j.bmcl.2007.01.111, PII S0960894X07001680
-
J.H. Ahn, M.S. Shin, M.A. Jun, and S.H. Jung et al. Synthesis, biological evaluation and structural determination of β-aminoacyl-containing cyclic hydrazine derivatives as dipeptidyl peptidase IV (DPP-IV) inhibitors Bioorg. Med. Chem. Lett. 17 2007 2622 2628 (Pubitemid 46509838)
-
(2007)
Bioorganic and Medicinal Chemistry Letters
, vol.17
, Issue.9
, pp. 2622-2628
-
-
Ahn, J.H.1
Shin, M.S.2
Jun, M.A.3
Jung, S.H.4
Kang, S.K.5
Kim, K.R.6
Rhee, S.D.7
Kang, N.S.8
Kim, S.Y.9
Sohn, S.-K.10
Kim, S.G.11
Jin, M.S.12
Lee, J.O.13
Cheon, H.G.14
Kim, S.S.15
-
123
-
-
50949120037
-
Synthesis and biological evaluation of pyrazoline analogues with β-amino acyl group as dipeptidyl peptidase IV inhibitors
-
M.A. Jun, W.S. Park, S.K. Kang, and K.Y. Kim et al. Synthesis and biological evaluation of pyrazoline analogues with β-amino acyl group as dipeptidyl peptidase IV inhibitors Eur. J. Med. Chem. 43 2008 1889 1902
-
(2008)
Eur. J. Med. Chem.
, vol.43
, pp. 1889-1902
-
-
Jun, M.A.1
Park, W.S.2
Kang, S.K.3
Kim, K.Y.4
-
124
-
-
33845683299
-
(3R)-4-[(3R)-3-Amino-4-(2,4,5-trifluorophenyl)butanoyl]-3-(2,2, 2-trifluoroethyl)-1,4-diazepan-2-one, a selective dipeptidyl peptidase IV inhibitor for the treatment of type 2 diabetes
-
DOI 10.1016/j.bmcl.2006.09.099, PII S0960894X06011656
-
T. Biftu, D. Feng, X. Qian, and G.-B. Liang et al. (3R)-4-[(3R)-3-Amino- 4-(2,4,5-trifluorophenyl)butanoyl]-3-(2,2,2-trifluoroethyl)-1,4-diazepan-2-one, a selective dipeptidyl peptidase IV inhibitor for the treatment of type 2 diabetes Bioorg. Med. Chem. Lett. 17 2007 49 52 (Pubitemid 44959987)
-
(2007)
Bioorganic and Medicinal Chemistry Letters
, vol.17
, Issue.1
, pp. 49-52
-
-
Biftu, T.1
Feng, D.2
Qian, X.3
Liang, G.-B.4
Kieczykowski, G.5
Eiermann, G.6
He, H.7
Leiting, B.8
Lyons, K.9
Petrov, A.10
Sinha-Roy, R.11
Zhang, B.12
Scapin, G.13
Patel, S.14
Gao, Y.-D.15
Singh, S.16
Wu, J.17
Zhang, X.18
Thornberry, N.A.19
Weber, A.E.20
more..
-
125
-
-
70350072361
-
Synthesis and biological evaluation of triazepane derivatives as DPP-IV inhibitors
-
J.H. Ahn, W.S. Park, M.A. Jun, M.S. Shin, and S.S. Kim et al. Synthesis and biological evaluation of triazepane derivatives as DPP-IV inhibitors J. Fluor. Chem. 130 2009 1001 1010
-
(2009)
J. Fluor. Chem.
, vol.130
, pp. 1001-1010
-
-
Ahn, J.H.1
Park, W.S.2
Jun, M.A.3
Shin, M.S.4
Kim, S.S.5
-
126
-
-
79952363348
-
Synthesis and evaluation of [(1R)-1-amino-2-(2,5-difluorophenyl)ethyl] cyclohexanes and 4-[(1R)-1-amino-2-(2,5-difluorophenyl)ethyl]piperidines as DPP-4 inhibitors
-
P. Chen, C.G. Caldwell, W. Ashton, and J.K. Wub et al. Synthesis and evaluation of [(1R)-1-amino-2-(2,5-difluorophenyl)ethyl]cyclohexanes and 4-[(1R)-1-amino-2-(2,5-difluorophenyl)ethyl]piperidines as DPP-4 inhibitors Bioorg. Med. Chem. Lett. 21 2011 1880 1886
-
(2011)
Bioorg. Med. Chem. Lett.
, vol.21
, pp. 1880-1886
-
-
Chen, P.1
Caldwell, C.G.2
Ashton, W.3
Wub, J.K.4
-
127
-
-
23544460894
-
-
Sep. 6 (2002)WO 2002/068420 A1
-
F. Himmelsbach, M. Mark, M. Eckhardt, E. Langkopf, R. Maier, R. Lotz, Xanthine dderivative, pproduction and uuse tthereof as a mmedicament. Sep. 6 (2002)WO 2002/068420 A1.
-
Xanthine Dderivative, Pproduction and Uuse Tthereof As A Mmedicament
-
-
Himmelsbach, F.1
Mark, M.2
Eckhardt, M.3
Langkopf, E.4
Maier, R.5
Lotz, R.6
-
128
-
-
84894211534
-
-
Jan 10 (2002)WO 2002/002560 A3R4
-
A.B. Kanstrup, L.B. Christiansen, J.M. Lundbeck, C.K. Sams, M. Kristiansen, Purine 2,6-diones wwhich aare iinhibitors of the eenzyme ddipeptidyl ppeptidase IV (DPP-IVIV). Jan 10 (2002)WO 2002/002560 A3R4.
-
Purine 2,6-diones Wwhich Aare Iinhibitors of the Eenzyme Ddipeptidyl Ppeptidase IV (DPP-IVIV)
-
-
Kanstrup, A.B.1
Christiansen, L.B.2
Lundbeck, J.M.3
Sams, C.K.4
Kristiansen, M.5
-
129
-
-
37349073397
-
8-(3-(R)-aminopiperidin-1-yl)-7-but-2-ynyl-3-methyl-1-(4-methyl- quinazolin- 2-ylmethyl)-3,7-dihydropurine-2,6-dione (BI 1356), a highly potent, selective, long-acting, and orally bioavailable DPP-4 inhibitor for the treatment of type 2 diabetes
-
DOI 10.1021/jm701280z
-
M. Eckhardt, E. Langkopf, M. Mark, and M. Tadayyon et al. 8-(3-(R)-Aminopiperidin-1-yl)-7-but-2-ynyl-3- methyl-1-(4-methyl-quinazolin-2- ylmethyl)-3,7-dihydropurine-2,6-dione (BI 1356), a highly potent, selective, long-acting, and orally bioavailable DPP-4 inhibitor for the treatment of type 2 diabetes J. Med. Chem. 50 2007 6450 6453 (Pubitemid 350309082)
-
(2007)
Journal of Medicinal Chemistry
, vol.50
, Issue.26
, pp. 6450-6453
-
-
Eckhardt, M.1
Langkopf, E.2
Mark, M.3
Tadayyon, M.4
Thomas, L.5
Nar, H.6
Pfrengle, W.7
Guth, B.8
Lotz, R.9
Sieger, P.10
Fuchs, H.11
Himmelsbach, F.12
-
130
-
-
44149127222
-
3,5-Dihydro-imidazo[4,5-d]pyridazin-4-ones: A class of potent DPP-4 inhibitors
-
DOI 10.1016/j.bmcl.2008.04.075, PII S0960894X08004794
-
M. Eckhardt, N. Hauel, F. Himmelsbach, and E. Langkopf et al. 3,5-Dihydro-imidazo[4,5-d]pyridazin-4-ones: a class of potent DPP-4 inhibitors Bioorg. Med. Chem. Lett. 18 2008 3158 3162 (Pubitemid 351718346)
-
(2008)
Bioorganic and Medicinal Chemistry Letters
, vol.18
, Issue.11
, pp. 3158-3162
-
-
Eckhardt, M.1
Hauel, N.2
Himmelsbach, F.3
Langkopf, E.4
Nar, H.5
Mark, M.6
Tadayyon, M.7
Thomas, L.8
Guth, B.9
Lotz, R.10
-
131
-
-
84856210285
-
Novel heterocyclic DPP-4 inhibitors for the treatment of type 2 diabetes
-
J.M. Sutton, D.E. Clark, S.J. Dunsdon, and G. Fenton et al. Novel heterocyclic DPP-4 inhibitors for the treatment of type 2 diabetes Bioorg. Med. Chem. Lett. 22 2012 1464 1468
-
(2012)
Bioorg. Med. Chem. Lett.
, vol.22
, pp. 1464-1468
-
-
Sutton, J.M.1
Clark, D.E.2
Dunsdon, S.J.3
Fenton, G.4
-
132
-
-
41349100946
-
Structure-based design and synthesis of benzimidazole derivatives as dipeptidyl peptidase IV inhibitors
-
DOI 10.1016/j.bmcl.2008.02.071, PII S0960894X08002527
-
M.B. Wallace, J. Feng, Z. Zhang, and R.J. Skene et al. Structure-based design and synthesis of benzimidazole derivatives as dipeptidyl peptidase IV inhibitors Bioorg. Med. Chem. Lett. 18 2008 2362 2367 (Pubitemid 351447287)
-
(2008)
Bioorganic and Medicinal Chemistry Letters
, vol.18
, Issue.7
, pp. 2362-2367
-
-
Wallace, M.B.1
Feng, J.2
Zhang, Z.3
Skene, R.J.4
Shi, L.5
Caster, C.L.6
Kassel, D.B.7
Xu, R.8
Gwaltney II, S.L.9
-
133
-
-
1542314925
-
5-fold activity increase by optimization of aromatic substituents
-
DOI 10.1016/j.bmcl.2004.01.019, PII S0960894X04000642
-
J.-U. Peters, S. Weber, S. Kritter, and P. Weiss et al. Aminomethylpyrimidines as novel DPP-IV inhibitors: a 105-fold activity increase by optimization of aromatic substituents Bioorg Med. Chem. Lett. 14 2004 1491 1493 (Pubitemid 38299435)
-
(2004)
Bioorganic and Medicinal Chemistry Letters
, vol.14
, Issue.6
, pp. 1491-1493
-
-
Peters, J.-U.1
Weber, S.2
Kritter, S.3
Weiss, P.4
Wallier, A.5
Boehringer, M.6
Hennig, M.7
Kuhn, B.8
Loeffler, B.-M.9
-
134
-
-
2942532819
-
Aminomethylpyridines as DPP-IV inhibitors
-
DOI 10.1016/j.bmcl.2004.04.049, PII S0960894X04005475
-
J.-U. Peters, S. Weber, S. Kritter, and P. Weiss et al. Aminomethylpyridines as DPP-IV inhibitors Bioorg. Med. Chem. Lett. 14 2004 3579 3580 (Pubitemid 38737171)
-
(2004)
Bioorganic and Medicinal Chemistry Letters
, vol.14
, Issue.13
, pp. 3579-3580
-
-
Peters, J.-U.1
Weber, S.2
Kritter, S.3
Weiss, P.4
Wallier, A.5
Zimmerli, D.6
Boehringer, M.7
Steger, M.8
Loeffler, B.-M.9
-
135
-
-
78650192270
-
Design, synthesis, and in vitro evaluation of novel aminomethyl-pyridines as DPP-4 inhibitors
-
K. Kaczanowska, K.-H. Wiesmuller, and A.-P. Schaffner Design, synthesis, and in vitro evaluation of novel aminomethyl-pyridines as DPP-4 inhibitors ACS Med. Chem. Lett. 1 2010 530 535
-
(2010)
ACS Med. Chem. Lett.
, vol.1
, pp. 530-535
-
-
Kaczanowska, K.1
Wiesmuller, K.-H.2
Schaffner, A.-P.3
-
136
-
-
2942624254
-
An aminomethylpyrimidine DPP-IV inhibitor with improved properties
-
DOI 10.1016/j.bmcl.2004.04.048, PII S0960894X04005463
-
J.-U. Peters, D. Hunziker, H. Fischer, and M. Kansy et al. An aminomethylpyrimidine DPP-IV inhibitor with improved properties Bioorg. Med. Chem. Lett. 14 2004 3575 3578 (Pubitemid 38737170)
-
(2004)
Bioorganic and Medicinal Chemistry Letters
, vol.14
, Issue.13
, pp. 3575-3578
-
-
Peters, J.-U.1
Hunziker, D.2
Fischer, H.3
Kansy, M.4
Weber, S.5
Kritter, S.6
Muller, A.7
Wallier, A.8
Ricklin, F.9
Boehringer, M.10
Poli, S.M.11
Csato, M.12
Loeffler, B.-M.13
-
137
-
-
77955367308
-
Synthesis and SAR of azolopyrimidines as potent and selective dipeptidyl peptidase-4 (DPP4) inhibitors for type 2 diabetes
-
R.P. Brigance, W. Meng, A. Fura, and T. Harrity et al. Synthesis and SAR of azolopyrimidines as potent and selective dipeptidyl peptidase-4 (DPP4) inhibitors for type 2 diabetes Bioorg Med. Chem. Lett. 20 2010 4395 4398
-
(2010)
Bioorg Med. Chem. Lett.
, vol.20
, pp. 4395-4398
-
-
Brigance, R.P.1
Meng, W.2
Fura, A.3
Harrity, T.4
-
138
-
-
77955387970
-
Discovery of 6-(aminomethyl)-5-(2,4-dichlorophenyl)-7-methylimidazo[1,2- a]pyrimidine-2-carboxamides as potent, selective dipeptidyl peptidase-4 (DPP4) inhibitors
-
W. Meng, R.P. Brigance, H.J. Chao, and A. Fura et al. Discovery of 6-(aminomethyl)-5-(2,4-dichlorophenyl)-7-methylimidazo[1,2-a] pyrimidine-2-carboxamides as potent, selective dipeptidyl peptidase-4 (DPP4) inhibitors J. Med. Chem. 53 2010 5620 5628
-
(2010)
J. Med. Chem.
, vol.53
, pp. 5620-5628
-
-
Meng, W.1
Brigance, R.P.2
Chao, H.J.3
Fura, A.4
-
139
-
-
78449276647
-
Discovery of new chemotype dipeptidyl peptidase IV inhibitors having (R)-3-amino-3-methyl piperidine as a pharmacophore
-
Y. Nishio, H. Kimura, S. Tosaki, and E. Sugaru et al. Discovery of new chemotype dipeptidyl peptidase IV inhibitors having (R)-3-amino-3-methyl piperidine as a pharmacophore Bioorg Med. Chem. Lett. 20 2010 7246 7249
-
(2010)
Bioorg Med. Chem. Lett.
, vol.20
, pp. 7246-7249
-
-
Nishio, Y.1
Kimura, H.2
Tosaki, S.3
Sugaru, E.4
-
140
-
-
80052571269
-
2-({6-[(3R)-3-amino-3-methylpiperidine-1-yl]-1,3-dimethyl-2,4-dioxo-1,2, 3,4-tetrahydro-5H-pyrrolo[3,2-d]pyrimidine-5 yl}methyl)-4- fluorobenzonitrile(DSR-12727): A potent, orally active dipeptidyl peptidase IV inhibitor without mechanism-based inactivation of CYP3A
-
Y. Nishio, H. Kimura, N. Sawada, E. Sugaru, and M. Horiguchi et al. 2-({6-[(3R)-3-amino-3-methylpiperidine-1-yl]-1,3-dimethyl-2,4-dioxo-1,2,3, 4-tetrahydro-5H-pyrrolo[3,2-d]pyrimidine-5 yl}methyl)-4-fluorobenzonitrile(DSR- 12727): a potent, orally active dipeptidyl peptidase IV inhibitor without mechanism-based inactivation of CYP3A Bioorg Med. Chem. Lett. 19 2011 5490 5499
-
(2011)
Bioorg Med. Chem. Lett.
, vol.19
, pp. 5490-5499
-
-
Nishio, Y.1
Kimura, H.2
Sawada, N.3
Sugaru, E.4
Horiguchi, M.5
-
141
-
-
80054734762
-
7-Oxopyrrolopyridine-derived DPP4 inhibitors - Mitigation of CYP and hERG liabilities via introduction of polar functionalities in the active site
-
W. Wang, P. Devasthale, A. Wang, and T. Harrity et al. 7-Oxopyrrolopyridine-derived DPP4 inhibitors - mitigation of CYP and hERG liabilities via introduction of polar functionalities in the active site Bioorg Med. Chem. Lett. 21 2011 6646 6651
-
(2011)
Bioorg Med. Chem. Lett.
, vol.21
, pp. 6646-6651
-
-
Wang, W.1
Devasthale, P.2
Wang, A.3
Harrity, T.4
-
142
-
-
34249280590
-
Rational design of a novel, potent, and orally bioavailable cyclohexylamine DPP-4 inhibitor by application of molecular modeling and X-ray crystallography of sitagliptin
-
DOI 10.1016/j.bmcl.2007.03.095, PII S0960894X07004088
-
T. Biftu, G. Scapin, S. Singh, D. Feng, J. Becker, and G. Doss et al. Rational design of a novel, potent, and orally bioavailable cyclohexylamine DPP-4 inhibitor by application of molecular modeling and X-ray crystallography of sitagliptin Bioorg. Med. Chem. Lett. 17 2007 3384 3387 (Pubitemid 46819024)
-
(2007)
Bioorganic and Medicinal Chemistry Letters
, vol.17
, Issue.12
, pp. 3384-3387
-
-
Biftu, T.1
Scapin, G.2
Singh, S.3
Feng, D.4
Becker, J.W.5
Eiermann, G.6
He, H.7
Lyons, K.8
Patel, S.9
Petrov, A.10
Sinha-Roy, R.11
Zhang, B.12
Wu, J.13
Zhang, X.14
Doss, G.A.15
Thornberry, N.A.16
Weber, A.E.17
-
143
-
-
34447309570
-
Discovery of 3-aminopiperidines as potent, selective, and orally bioavailable dipeptidyl peptidase IV inhibitors
-
DOI 10.1016/j.bmcl.2007.05.087, PII S0960894X07006671
-
J.M. Cox, B. Harper, A. Mastracchio, B. Leiting, and R.S. Roy et al. Discovery of 3-aminopiperidines as potent, selective, and orally bioavailable dipeptidyl peptidase IV inhibitors Bioorg. Med. Chem. Lett. 17 2007 4579 4583 (Pubitemid 47058943)
-
(2007)
Bioorganic and Medicinal Chemistry Letters
, vol.17
, Issue.16
, pp. 4579-4583
-
-
Cox, J.M.1
Harper, B.2
Mastracchio, A.3
Leiting, B.4
Sinha Roy, R.5
Patel, R.A.6
Wu, J.K.7
Lyons, K.A.8
He, H.9
Xu, S.10
Zhu, B.11
Thornberry, N.A.12
Weber, A.E.13
Edmondson, S.D.14
-
145
-
-
15744378057
-
Sulphostin, a novel inhibitor of dipeptidyl peptidases IV (DPPIV) that stimulates hematopoiesis in mice
-
M. Abe, F. Abe, C. Nishimura, and E. Ichimura et al. Sulphostin, a novel inhibitor of dipeptidyl peptidases IV (DPPIV) that stimulates hematopoiesis in mice J. Antibiot. 58 2005 111 117 (Pubitemid 40410232)
-
(2005)
Journal of Antibiotics
, vol.58
, Issue.2
, pp. 111-117
-
-
Abe, M.1
Abe, F.2
Nishimura, C.3
Ichimura, E.4
Ogasawara, A.5
Ichinei, M.6
Muraoka, Y.7
Saino, T.8
-
146
-
-
33750456573
-
Discovery of ((4R,5S)-5-amino-4-(2,4,5- trifluorophenyl)cyclohex-1-enyl)- (3- (trifluoromethyl)-5,6-dihydro- [1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl) methanone (ABT-341), a highly potent, selective, orally efficacious, and safe dipeptidyl peptidase IV inhibitor for the treatment of type 2 Diabetes
-
Z. Pei, X. Li, T.W. von Geldern, D.J. Madar, and K. Longenecker et al. Discovery of ((4R,5S)-5-amino-4-(2,4,5- trifluorophenyl)cyclohex-1-enyl)-(3- (trifluoromethyl)-5,6-dihydro- [1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl)methanone (ABT-341), a highly potent, selective, orally efficacious, and safe dipeptidyl peptidase IV inhibitor for the treatment of type 2 Diabetes J. Med. Chem. 49 2006 6439
-
(2006)
J. Med. Chem.
, vol.49
, pp. 6439
-
-
Pei, Z.1
Li, X.2
Von Geldern, T.W.3
Madar, D.J.4
Longenecker, K.5
-
147
-
-
33847628449
-
Pyrrolidine-constrained phenethylamines: The design of potent, selective, and pharmacologically efficacious dipeptidyl peptidase IV (DPP4) inhibitors from a lead-like screening hit
-
DOI 10.1016/j.bmcl.2007.01.026, PII S0960894X07000753
-
B.J. Backes, K. Longenecker, G.L. Hamilton, and K. Stewart et al. Pyrrolidine-constrained phenethylamines: the design of potent, selective, and pharmacologically efficacious dipeptidyl peptidase IV (DPP4) inhibitors from a lead-like screening hit Bioorg. Med. Chem. Lett. 17 2007 2005 2012 (Pubitemid 46367663)
-
(2007)
Bioorganic and Medicinal Chemistry Letters
, vol.17
, Issue.7
, pp. 2005-2012
-
-
Backes, B.J.1
Longenecker, K.2
Hamilton, G.L.3
Stewart, K.4
Lai, C.5
Kopecka, H.6
Von Geldern, T.W.7
Madar, D.J.8
Pei, Z.9
Lubben, T.H.10
Zinker, B.A.11
Tian, Z.12
Ballaron, S.J.13
Stashko, M.A.14
Mika, A.K.15
Beno, D.W.A.16
Kempf-Grote, A.J.17
Black-Schaefer, C.18
Sham, H.L.19
Trevillyan, J.M.20
more..
-
148
-
-
34247204289
-
Discovery and structure - Activity relationships of piperidinone- and piperidine-constrained phenethylamines as novel, potent, and selective dipeptidyl peptidase IV inhibitors
-
DOI 10.1021/jm061436d
-
Z. Pei, X. Li, T.W. von Geldern, and K. Longenecker et al. Discovery and Structure-Activity relationships of piperidinone- and piperidine-constrained phenethylamines as novel, potent, and selective dipeptidyl peptidase iv inhibitors J. Med. Chem. 50 2007 1983 1987 (Pubitemid 46626607)
-
(2007)
Journal of Medicinal Chemistry
, vol.50
, Issue.8
, pp. 1983-1987
-
-
Pei, Z.1
Li, X.2
Von Geldern, T.W.3
Longenecker, K.4
Pireh, D.5
Stewart, K.D.6
Backes, B.J.7
Lai, C.8
Lubben, T.H.9
Ballaron, S.J.10
Beno, D.W.A.11
Kempf-Grote, A.J.12
Sham, H.L.13
Trevillyan, J.M.14
-
149
-
-
34548552525
-
(3R,4S)-4-(2,4,5-Trifluorophenyl)-pyrrolidin-3-ylamine inhibitors of dipeptidyl peptidase IV: Synthesis, in vitro, in vivo, and X-ray crystallographic characterization
-
DOI 10.1016/j.bmcl.2007.07.081, PII S0960894X07009018
-
S.W. Wright, M.J. Ammirati, K.M. Andrews, and A.M. Brodeur et al. (3R,4S)-4-(2,4,5-Trifluorophenyl)-pyrrolidin-3-ylamine inhibitors of dipeptidyl peptidase IV: synthesis, in vitro, in vivo, and X-ray crystallographic characterization Bioorg. Med. Chem. Lett. 17 2007 5638 5642 (Pubitemid 47391309)
-
(2007)
Bioorganic and Medicinal Chemistry Letters
, vol.17
, Issue.20
, pp. 5638-5642
-
-
Wright, S.W.1
Ammirati, M.J.2
Andrews, K.M.3
Brodeur, A.M.4
Danley, D.E.5
Doran, S.D.6
Lillquist, J.S.7
Liu, S.8
McClure, L.D.9
McPherson, R.K.10
Olson, T.V.11
Orena, S.J.12
Parker, J.C.13
Rocke, B.N.14
Soeller, W.C.15
Soglia, C.B.16
Treadway, J.L.17
VanVolkenburg, M.A.18
Zhao, Z.19
Cox, E.D.20
more..
-
150
-
-
79952363044
-
1-((3S,4S)-4-Amino-1-(4-substituted-1,3,5-triazin-2-yl) pyrrolidin-3-yl)-5,5-difluoropiperidin-2-one inhibitors of DPP-4 for the treatment of type 2 diabetes
-
K.M. Andrews, D.A. Beebe, J.W. Benbow, and D.A. Boyer et al. 1-((3S,4S)-4-Amino-1-(4-substituted-1,3,5-triazin-2-yl) pyrrolidin-3-yl)-5,5- difluoropiperidin-2-one inhibitors of DPP-4 for the treatment of type 2 diabetes Bioorg. Med. Chem. Lett. 21 2011 1810 1814
-
(2011)
Bioorg. Med. Chem. Lett.
, vol.21
, pp. 1810-1814
-
-
Andrews, K.M.1
Beebe, D.A.2
Benbow, J.W.3
Boyer, D.A.4
-
151
-
-
44849112519
-
Discovery of new binding elements in DPP-4 inhibition and their applications in novel DPP-4 inhibitor design
-
DOI 10.1016/j.bmcl.2008.05.061, PII S0960894X0800557X
-
G.-B. Liang, X. Qian, T. Biftu, and S. Singh et al. Discovery of new binding elements in DPP-4 inhibition and their applications in novel DPP-4 inhibitor design Bioorg. Med. Chem. Lett. 18 2008 3706 3710 (Pubitemid 351794517)
-
(2008)
Bioorganic and Medicinal Chemistry Letters
, vol.18
, Issue.13
, pp. 3706-3710
-
-
Liang, G.-B.1
Qian, X.2
Biftu, T.3
Singh, S.4
Gao, Y.-D.5
Scapin, G.6
Patel, S.7
Leiting, B.8
Patel, R.9
Wu, J.10
Zhang, X.11
Thornberry, N.A.12
Weber, A.E.13
-
153
-
-
34247869769
-
1,3-Disubstituted 4-aminopiperidines as useful tools in the optimization of the 2-aminobenzo[a]quinolizine dipeptidyl peptidase IV inhibitors
-
DOI 10.1016/j.bmcl.2007.03.072, PII S0960894X07003757
-
T. Lubbers, M. Bohringer, L. Gobbi, M. Hennig, and D. Hunziker 1,3-Disubstituted 4-aminopiperidines as useful tools in the optimization of the 2-aminobenzo[a]quinolizine dipeptidyl peptidase IV inhibitors Bioorg. Med. Chem. Lett. 17 2007 2966 2970 (Pubitemid 46702649)
-
(2007)
Bioorganic and Medicinal Chemistry Letters
, vol.17
, Issue.11
, pp. 2966-2970
-
-
Lubbers, T.1
Bohringer, M.2
Gobbi, L.3
Hennig, M.4
Hunziker, D.5
Kuhn, B.6
Loffler, B.7
Mattei, P.8
Narquizian, R.9
Peters, J.-U.10
Ruff, Y.11
Wessel, H.P.12
Wyss, P.13
-
154
-
-
74049162952
-
Discovery of carmegliptin: A potent and long-acting dipeptidyl peptidase IV inhibitor for the treatment of type 2 diabetes
-
P. Mattei, M. Boehringer, P. Di Giorgio, and H. Fischer et al. Discovery of carmegliptin: a potent and long-acting dipeptidyl peptidase IV inhibitor for the treatment of type 2 diabetes Bioorg. Med. Chem. Lett. 20 2010 1109 1113
-
(2010)
Bioorg. Med. Chem. Lett.
, vol.20
, pp. 1109-1113
-
-
Mattei, P.1
Boehringer, M.2
Di Giorgio, P.3
Fischer, H.4
-
155
-
-
74049094489
-
Aryl- and heteroaryl-substituted aminobenzo[a]quinolizines as dipeptidyl peptidase IV inhibitors
-
M. Boehringer, H. Fischer, M. Hennig, and D. Hunziker et al. Aryl- and heteroaryl-substituted aminobenzo[a]quinolizines as dipeptidyl peptidase IV inhibitors Bioorg. Med. Chem. Lett. 20 2010 1106 1108
-
(2010)
Bioorg. Med. Chem. Lett.
, vol.20
, pp. 1106-1108
-
-
Boehringer, M.1
Fischer, H.2
Hennig, M.3
Hunziker, D.4
-
156
-
-
0037394499
-
A fully integrated protein crystallization platform for small-molecule drug discovery
-
DOI 10.1016/S1047-8477(03)00051-0
-
D. Hosfield, J. Palan, M. Hilgers, and D. Scheibe et al. A fully integrated protein crystallization platform for small-molecule drug discovery J. Struct. Biol. 142 2003 207 217 (Pubitemid 36457902)
-
(2003)
Journal of Structural Biology
, vol.142
, Issue.1
, pp. 207-217
-
-
Hosfield, D.1
Palan, J.2
Hilgers, M.3
Scheibe, D.4
McRee, D.E.5
Stevens, R.C.6
-
157
-
-
34248999413
-
Discovery of alogliptin: A potent, selective, bioavailable, and efficacious inhibitor of dipeptidyl peptidase IV
-
DOI 10.1021/jm070104l
-
J. Feng, Z. Zhang, M.B. Wallace, and J.A. Stafford et al. Discovery of alogliptin: a potent, selective, bioavailable, and efficacious inhibitor of dipeptidyl peptidase IV J. Med. Chem. 50 2007 2297 2300 (Pubitemid 46799241)
-
(2007)
Journal of Medicinal Chemistry
, vol.50
, Issue.10
, pp. 2297-2300
-
-
Feng, J.1
Zhang, Z.2
Wallace, M.B.3
Stafford, J.A.4
Kaldor, S.W.5
Kassel, D.B.6
Navre, M.7
Shi, L.8
Skene, R.J.9
Asakawa, T.10
Takeuchi, K.11
Xu, R.12
Webb, D.R.13
Gwaltney II, S.L.14
-
158
-
-
0038453836
-
-
Jan 16 (2003)WO 2003/004496 A1
-
A.B. Kanstrup, C.K. Sams, J.M. Lundbeck, L.B. Christiansen, M. Kristiansen, DPP-4 iinhibiting ppurine dderivatives for the ttreatment of ddiabetes. Jan 16 (2003)WO 2003/004496 A1.
-
DPP-4 Iinhibiting Ppurine Dderivatives for the Ttreatment of Ddiabetes
-
-
Kanstrup, A.B.1
Sams, C.K.2
Lundbeck, J.M.3
Christiansen, L.B.4
Kristiansen, M.5
-
159
-
-
84894148484
-
-
World patent (2002)2002068420
-
F. Himmelsbach,; M.Mark; M.Eckhardt; E.Langkopf; R.Maier; R.Lotz, World patent (2002)2002068420.
-
-
-
Himmelsbach, F.1
-
160
-
-
78751651182
-
Design and synthesis of pyrimidinone and pyrimidinedione inhibitors of dipeptidyl peptidase IV
-
Z. Zhang, M.B. Wallace, J. Feng, and J.A. Stafford et al. Design and synthesis of pyrimidinone and pyrimidinedione inhibitors of dipeptidyl peptidase IV J. Med. Chem. 54 2011 510 524
-
(2011)
J. Med. Chem.
, vol.54
, pp. 510-524
-
-
Zhang, Z.1
Wallace, M.B.2
Feng, J.3
Stafford, J.A.4
-
161
-
-
78650513267
-
The highly potent and selective dipeptidyl peptidase IV inhibitors bearing a thienopyrimidine scaffold effectively treat type 2 diabetes
-
J. Deng, L. Peng, G. Zhang, and X. Lan et al. The highly potent and selective dipeptidyl peptidase IV inhibitors bearing a thienopyrimidine scaffold effectively treat type 2 diabetes Eur. J. Med. Chem. 46 2011 71 76
-
(2011)
Eur. J. Med. Chem.
, vol.46
, pp. 71-76
-
-
Deng, J.1
Peng, L.2
Zhang, G.3
Lan, X.4
-
162
-
-
84860342035
-
Novel pyrrolopyrimidine analogues as potent dipeptidyl peptidase IV inhibitors based on pharmacokinetic property-driven optimization
-
H. Xie, L. Zeng, S. Zeng, and X. Lu et al. Novel pyrrolopyrimidine analogues as potent dipeptidyl peptidase IV inhibitors based on pharmacokinetic property-driven optimization Eur. J. Med. Chem. 52 2012 205 212
-
(2012)
Eur. J. Med. Chem.
, vol.52
, pp. 205-212
-
-
Xie, H.1
Zeng, L.2
Zeng, S.3
Lu, X.4
-
163
-
-
79961165720
-
Identification of 3-Aminomethyl-1,2-dihydro-4-phenyl-1-isoquinolones: A new class of potent, selective, and orally active non-peptide dipeptidyl peptidase iv inhibitors that form a unique interaction with Lys554
-
Y. Banno, Y. Miyamoto, M. Sasaki, S. Oi, and T. Asakawa et al. Identification of 3-Aminomethyl-1,2-dihydro-4-phenyl-1-isoquinolones: a new class of potent, selective, and orally active non-peptide dipeptidyl peptidase iv inhibitors that form a unique interaction with Lys554 Bioorg. Med. Chem. 19 2011 4953 4970
-
(2011)
Bioorg. Med. Chem.
, vol.19
, pp. 4953-4970
-
-
Banno, Y.1
Miyamoto, Y.2
Sasaki, M.3
Oi, S.4
Asakawa, T.5
-
164
-
-
79960553998
-
Discovery of potent, selective, and orally bioavailable quinoline-based dipeptidyl peptidase IV inhibitors targeting Lys554
-
H. Maezaki, Y. Banno, Y. Miyamoto, and Y. Moritou et al. Discovery of potent, selective, and orally bioavailable quinoline-based dipeptidyl peptidase IV inhibitors targeting Lys554 Bioorg. Med. Chem. 19 2011 4482 4498
-
(2011)
Bioorg. Med. Chem.
, vol.19
, pp. 4482-4498
-
-
Maezaki, H.1
Banno, Y.2
Miyamoto, Y.3
Moritou, Y.4
-
165
-
-
79851501708
-
Discovery of a 3-pyridylacetic acid derivative (TAK-100) as a potent, selective and orally active dipeptidyl peptidase IV (DPP-4) inhibitor
-
Y. Miyamoto, Y. Banno, T. Yamashita, and T. Fujimoto et al. Discovery of a 3-pyridylacetic acid derivative (TAK-100) as a potent, selective and orally active dipeptidyl peptidase IV (DPP-4) inhibitor J. Med. Chem. 54 2011 831 850
-
(2011)
J. Med. Chem.
, vol.54
, pp. 831-850
-
-
Miyamoto, Y.1
Banno, Y.2
Yamashita, T.3
Fujimoto, T.4
-
166
-
-
78650744466
-
Design and synthesis of 3-pyridylacetamide derivatives as dipeptidyl peptidase IV (DPP-4) inhibitors targeting a bidentate interaction with Arg125
-
Y. Miyamoto, Y. Banno, T. Yamashita, and T. Fujimoto et al. Design and synthesis of 3-pyridylacetamide derivatives as dipeptidyl peptidase IV (DPP-4) inhibitors targeting a bidentate interaction with Arg125 Bioorg. Med. Chem. 19 2011 172 185
-
(2011)
Bioorg. Med. Chem.
, vol.19
, pp. 172-185
-
-
Miyamoto, Y.1
Banno, Y.2
Yamashita, T.3
Fujimoto, T.4
-
167
-
-
84866424769
-
Discovery of 3H-imidazo[4,5-c]quinolin-4(5H)-ones as potent and selective dipeptidyl peptidase IV (DPP-4) inhibitors
-
Y. Ikuma, H. Hochigai, H. Kimura, and N. Nunami et al. Discovery of 3H-imidazo[4,5-c]quinolin-4(5H)-ones as potent and selective dipeptidyl peptidase IV (DPP-4) inhibitors Bioorg. Med. Chem. 20 2012 5864 5883
-
(2012)
Bioorg. Med. Chem.
, vol.20
, pp. 5864-5883
-
-
Ikuma, Y.1
Hochigai, H.2
Kimura, H.3
Nunami, N.4
-
168
-
-
53549098210
-
Thalidomide as a multi-template for development of biologically active compounds
-
Y. Hashimoto Thalidomide as a multi-template for development of biologically active compounds Arch. Pharm. Chem. Life. Sci. 341 2008 536 547
-
(2008)
Arch. Pharm. Chem. Life. Sci.
, vol.341
, pp. 536-547
-
-
Hashimoto, Y.1
-
169
-
-
0036158279
-
Structural development of biological response modifiers based on thalidomide
-
DOI 10.1016/S0968-0896(01)00308-X, PII S096808960100308X
-
Y. Hashimoto Structural development of biological response modifiers based on thalidomide Bioorg. Med. Chem. 10 2002 461 479 (Pubitemid 34112438)
-
(2002)
Bioorganic and Medicinal Chemistry
, vol.10
, Issue.3
, pp. 461-479
-
-
Hashimoto, Y.1
-
170
-
-
0041324659
-
Structural development of synthetic retinoids and thalidomide-related molecules
-
Y. Hashimoto Structural development of synthetic retinoids and thalidomide-related molecules Cancer Chemother. Pharmacol. 52 2003 S16 S23
-
(2003)
Cancer Chemother. Pharmacol.
, vol.52
-
-
Hashimoto, Y.1
-
171
-
-
2642512949
-
Thalidomide as a multitarget drug and its application as a template for drug design
-
DOI 10.1358/dof.2004.029.04.792298
-
Y. Hashimoto, A. Tanatani, K. Nagasawa, and H. Miyachi Thalidomide as a target drug and its application as a template for drug design Drugs Future 29 2004 383 391 (Pubitemid 38724680)
-
(2004)
Drugs of the Future
, vol.29
, Issue.4
, pp. 383-391
-
-
Hashimoto, Y.1
Tanatani, A.2
Nagasawa, K.3
Miyachi, H.4
-
172
-
-
0031837706
-
Novel biological response modifiers derived from thalidomide
-
Y. Hashimoto Novel biological response modifiers derived from thalidomide Curr. Med. Chem. 5 1998 163 178 (Pubitemid 28238487)
-
(1998)
Current Medicinal Chemistry
, vol.5
, Issue.3
, pp. 163-178
-
-
Hashimoto, Y.1
-
173
-
-
0013212945
-
Structural development of biological response modifiers based on retinoids and thalidomide
-
Y. Hashimoto Structural development of biological response modifiers based on retinoids and thalidomide Mini-Rev. Med. Chem. 2 2002 543 551
-
(2002)
Mini-Rev. Med. Chem.
, vol.2
, pp. 543-551
-
-
Hashimoto, Y.1
-
174
-
-
79955551684
-
Non-competitive and selective dipeptidyl peptidase IV inhibitors with phenethylphenylphthalimide skeleton derived from thalidomide-related α-glucosidase inhibitors and liver X receptor antagonists
-
K. Motoshima, K. Sugita, Y. Hashimoto, and M. Ishikawa Non-competitive and selective dipeptidyl peptidase IV inhibitors with phenethylphenylphthalimide skeleton derived from thalidomide-related α-glucosidase inhibitors and liver X receptor antagonists Bioorg. Med. Chem. Lett. 21 2011 3041 3045
-
(2011)
Bioorg. Med. Chem. Lett.
, vol.21
, pp. 3041-3045
-
-
Motoshima, K.1
Sugita, K.2
Hashimoto, Y.3
Ishikawa, M.4
-
175
-
-
80054933500
-
Recent patents of dipeptidyl peptidase IV inhibitors
-
E. Giralt, L. Mendieta, and T. Tarrago et al. Recent patents of dipeptidyl peptidase IV inhibitors Expert Opin. Ther. Pat. 21 2011 1693 1741
-
(2011)
Expert Opin. Ther. Pat.
, vol.21
, pp. 1693-1741
-
-
Giralt, E.1
Mendieta, L.2
Tarrago, T.3
-
177
-
-
85027286054
-
-
Jan 3 (2013)WO 2013/3250 A1
-
M.J. Zacuto, R.F. Dunn, A.J. Moment, J.M. Janey, et al., Process for preparing chiral dipeptidyl peptidase-IV inhibitors, Jan 3 (2013)WO 2013/3250 A1.
-
Process for Preparing Chiral Dipeptidyl Peptidase-IV Inhibitors
-
-
Zacuto, M.J.1
Dunn, R.F.2
Moment, A.J.3
Janey, J.M.4
-
178
-
-
84894162720
-
-
Nippi, DPP-4 inhibitor, May 10 (2013)WO 2013/65832 A1
-
Nippi, DPP-4 inhibitor, May 10 (2013)WO 2013/65832 A1.
-
-
-
-
179
-
-
84902187706
-
-
May 15 (2012)US 8178541
-
F. Himmaelsbach, E. Langkopf, M. Eckhardt, et al., 8-[3-Amino-piperidin- 1-yl]-xanthines, the preparation thereof and their use as pharmaceutical compositions, May 15 (2012)US 8178541.
-
8-[3-Amino-piperidin-1-yl]-xanthines, the Preparation Thereof and Their Use As Pharmaceutical Compositions
-
-
Himmaelsbach, F.1
Langkopf, E.2
Eckhardt, M.3
-
207
-
-
84894200706
-
-
Feb 15 (2011)US 7888343 B2
-
K. Schoenafinger, G. Jaehne, E. Defossa, et al., Substituted, bicyclic 8-pyrrolidinoxanthines, and methods for their use as inhibitors of DPP, Feb 15 (2011)US 7888343 B2.
-
Substituted, Bicyclic 8-pyrrolidinoxanthines, and Methods for Their Use As Inhibitors of DPP
-
-
Schoenafinger, K.1
Jaehne, G.2
Defossa, E.3
-
228
-
-
84894222851
-
-
Apr 19 (2011)US 7928112
-
T. Biftu, P. Chen, D. Feng, A.E. Webner, Substituted 5,6,7,8- tetrahydropyrido[4,3-d]pyrimidines as DPP-4 inhibitors for the treatment or prevention of diabetes, Apr 19 (2011)US 7928112.
-
Substituted 5,6,7,8-tetrahydropyrido[4,3-d]pyrimidines As DPP-4 Inhibitors for the Treatment or Prevention of Diabetes
-
-
Biftu, T.1
Chen, P.2
Feng, D.3
Webner, A.E.4
-
235
-
-
84887817205
-
-
Jul 8 (2010)US 2010/0173916
-
F. Himmelsbach, M. Mark, M. Eckhardt, et al., Xanthine derivatives, the preparation thereof and their use as pharmaceutical compositions, Jul 8 (2010)US 2010/0173916.
-
Xanthine Derivatives, the Preparation Thereof and Their Use As Pharmaceutical Compositions
-
-
Himmelsbach, F.1
Mark, M.2
Eckhardt, M.3
-
236
-
-
84887817205
-
-
Aug 12 (2010)US 2010/0204250
-
F. Himmelsbach, M. Mark, M. Eckhardt, et al., Xanthine derivatives, the preparation thereof and their use as pharmaceutical compositions, Aug 12 (2010)US 2010/0204250.
-
Xanthine Derivatives, the Preparation Thereof and Their Use As Pharmaceutical Compositions
-
-
Himmelsbach, F.1
Mark, M.2
Eckhardt, M.3
-
242
-
-
84894210354
-
-
Nov 2 (2010)US 7825242
-
J. Feng, S.L. Gwaltney, B. Lam, Z. Zhang, et al., DPP inhibitors, Nov 2 (2010)US 7825242.
-
DPP Inhibitors
-
-
Feng, J.1
Gwaltney, S.L.2
Lam, B.3
Zhang, Z.4
-
244
-
-
84894210354
-
-
Aug 24 (2010)US 7781584
-
J. Feng, S.L. Gwaltney, J.A. Stafford, Z. Zhang, et al., DPP inhibitors, Aug 24 (2010)US 7781584.
-
DPP Inhibitors
-
-
Feng, J.1
Gwaltney, S.L.2
Stafford, J.A.3
Zhang, Z.4
-
249
-
-
84894210354
-
-
Mar 30 (2010)US 7687638
-
J. Feng, S.L. Gwaltney, M.B. Wallace, Z. Zhang, et al., DPP inhibitors, Mar 30 (2010)US 7687638.
-
DPP Inhibitors
-
-
Feng, J.1
Gwaltney, S.L.2
Wallace, M.B.3
Zhang, Z.4
-
262
-
-
84894172698
-
-
Mar 30 (2010)US 7687492
-
J. Xu, L. Wei, A. Mastracchio, S.D. Edmondson, 1,2,4-Oxadiazole derivatives as DPP-4 inhibitors for the treatment or prevention of diabetes, Mar 30 (2010)US 7687492.
-
1,2,4-Oxadiazole Derivatives As DPP-4 Inhibitors for the Treatment or Prevention of Diabetes
-
-
Xu, J.1
Wei, L.2
Mastracchio, A.3
Edmondson, S.D.4
-
264
-
-
84894171832
-
-
Oct 12 (2010)US 7812027
-
T. Biftu, P. Chen, D. Feng, A.E. Webner, Substituted [1,2,4]triazolo[1,5- a]pyrazines as DPP-4 inhibitors for the treatment or prevention of diabetes, Oct 12 (2010)US 7812027.
-
Substituted [1,2,4]triazolo[1,5-a]pyrazines As DPP-4 Inhibitors for the Treatment or Prevention of Diabetes
-
-
Biftu, T.1
Chen, P.2
Feng, D.3
Webner, A.E.4
-
270
-
-
0037787851
-
Dipeptidyl-peptidase IV from bench to bedside: An update on structural properties, functions, and clinical aspects of the enzyme DPP IV
-
A.M. Lambeir, C. Durinx, and S. Scharpe et al. Dipeptidylpeptidase IV from bench to bedside: an update on structural properties, functions, and clinical aspects of the enzyme DPP IV Crit. Rev. Clin. Lab. Sci. 40 2003 209 294 (Pubitemid 36775376)
-
(2003)
Critical Reviews in Clinical Laboratory Sciences
, vol.40
, Issue.3
, pp. 209-294
-
-
Lambeir, A.-M.1
Durinx, C.2
Scharpe, S.3
De Meester, I.4
-
271
-
-
34248223285
-
Biology of Incretins: GLP-1 and GIP
-
DOI 10.1053/j.gastro.2007.03.054, PII S001650850700580X
-
L.L. Baggio, and D.J. Drucker Biology of incretins: GLP-1 and GIP Gastroenterology 132 2007 2131 2157 (Pubitemid 46711096)
-
(2007)
Gastroenterology
, vol.132
, Issue.6
, pp. 2131-2157
-
-
Baggio, L.L.1
Drucker, D.J.2
-
272
-
-
0033561659
-
CD26/dipeptidyl-peptidase IV down-regulates the eosinophil chemotactic potency, but not the anti-HIV activity of human eotaxin by affecting its interaction with CC chemokine receptor 3
-
S. Struyf, P. Proost, D. Schols, and E.D. Clercq et al. CD26/Dipeptidyl-peptidase IV down-regulates the eosinophil chemotactic potency, but not the anti-HIV activity of human eotaxin by affecting its interaction with CC chemokine receptor 3 J. Immunol. 162 1999 4903 4909 (Pubitemid 29314895)
-
(1999)
Journal of Immunology
, vol.162
, Issue.8
, pp. 4903-4909
-
-
Struyf, S.1
Proost, P.2
Schols, D.3
De Clercq, E.4
Opdenakker, G.5
Lenaerts, J.-P.6
Detheux, M.7
Parmentier, M.8
De Meester, I.9
Scharpe, S.10
Van Damme, J.11
-
273
-
-
27844453866
-
Dipeptidyl peptidase IV activity and/or structure homologs: Contributing factors in the pathogenesis of rheumatoid arthritis?
-
DOI 10.1186/ar1852
-
Sedo, J.S. Duke-Cohan, and E. Balaziova et al. Dipeptidyl peptidase IV activity and/or structure homologs: contributing factors in the pathogenesis of rheumatoid arthritis? Arthritis Res. Ther. 7 2005 253 269 (Pubitemid 41646256)
-
(2005)
Arthritis Research and Therapy
, vol.7
, Issue.6
, pp. 253-269
-
-
Sedo, A.1
Duke-Cohan, J.S.2
Balaziova, E.3
Sedova, L.R.4
-
274
-
-
84866988553
-
Is dipeptidyl peptidase IV (DPP IV) associated with inflammation present in human spondyloarthritides and rheumatoid arthritis
-
D. Detel, T. Kehler, and S. Buljevic et al. Is dipeptidyl peptidase IV (DPP IV) associated with inflammation present in human spondyloarthritides and rheumatoid arthritis Croat. Chem. Acta 85 2012 231 238
-
(2012)
Croat. Chem. Acta
, vol.85
, pp. 231-238
-
-
Detel, D.1
Kehler, T.2
Buljevic, S.3
-
275
-
-
0024346019
-
Activities of dipeptidyl peptidase II and dipeptidyl peptidase IV in synovial fluid from patients with rheumatoid arthritis and osteoarthritis
-
H. Gotoh et al. Activities of dipeptidyl peptidase II and dipeptidyl peptidase IV in synovial fluid from patients with rheumatoid arthritis and osteoarthritis Clin. Chem. 35 1989 1016 1018 (Pubitemid 19161276)
-
(1989)
Clinical Chemistry
, vol.35
, Issue.6
, pp. 1016-1018
-
-
Gotoh, H.1
Hagihara, M.2
Nagatsu, T.3
Iwata, H.4
Miura, T.5
-
276
-
-
77951725805
-
Inhibition of fibroblast activation protein and dipeptidylpeptidase 4 increases cartilage invasion by rheumatoid arthritissynovial fibroblasts
-
C. Ospelt, J.C. Mertens, and A. Jungel et al. Inhibition of fibroblast activation protein and dipeptidylpeptidase 4 increases cartilage invasion by rheumatoid arthritissynovial fibroblasts Arthritis Rheum. 62 2010 1224 1235
-
(2010)
Arthritis Rheum.
, vol.62
, pp. 1224-1235
-
-
Ospelt, C.1
Mertens, J.C.2
Jungel, A.3
-
277
-
-
38449100190
-
The role of CD26/dipeptidyl peptidase IV in cancer
-
DOI 10.2741/2787
-
P.A. Havre, M. Abe, Y. Urasaki, and K. Ohnuma et al. The role of CD26/dipeptidyl peptidase IV in cancer Front. Biosci. 13 2008 1634 1645 (Pubitemid 351599721)
-
(2008)
Frontiers in Bioscience
, vol.13
, Issue.5
, pp. 1634-1645
-
-
Havre, P.A.1
Abe, M.2
Urasaki, Y.3
Ohnuma, K.4
Morimoto, C.5
Dang, N.H.6
-
278
-
-
69049119483
-
Duke-Cohan. Dipeptidyl peptidase-IV and related molecules: Markers of malignancy?
-
J. Sedo, P. Stremenova, and J. Busek Duke-Cohan. Dipeptidyl peptidase-IV and related molecules: markers of malignancy? Expert Opin. Med. Diag. 2 2008 677 689
-
(2008)
Expert Opin. Med. Diag.
, vol.2
, pp. 677-689
-
-
Sedo, J.1
Stremenova, P.2
Busek, J.3
-
280
-
-
33646416468
-
The protease complex consisting of dipeptidyl peptidase IV and seprase plays a role in the migration and invasion of human endothelial cells in collagenous matrices
-
G. Ghersi, Q. Zhao, M. Salamone, and Y. Yeh et al. The protease complex consisting of dipeptidyl peptidase IV and seprase plays a role in the migration and invasion of human endothelial cells in collagenous matrices Cancer Res. 66 2006 4652 4661
-
(2006)
Cancer Res.
, vol.66
, pp. 4652-4661
-
-
Ghersi, G.1
Zhao, Q.2
Salamone, M.3
Yeh, Y.4
-
281
-
-
59149096596
-
Suppression of neuroblastoma growth by dipeptidyl peptidase IV: Relevance of chemokine regulation and caspase activation
-
W.T. Arscott, A.E. LaBauve, V. May, and U.V. Wesley Suppression of neuroblastoma growth by dipeptidyl peptidase IV: relevance of chemokine regulation and caspase activation Oncogene 28 2009 479 491
-
(2009)
Oncogene
, vol.28
, pp. 479-491
-
-
Arscott, W.T.1
Labauve, A.E.2
May, V.3
Wesley, U.V.4
-
282
-
-
6344253102
-
CD26/dipeptidyl peptidase IV and its role in cancer
-
B. Pro, and N.H. Dang CD26/dipeptidyl peptidase IV and its role in cancer Histol. Histopathol. 19 2004 1345 1351 (Pubitemid 39386791)
-
(2004)
Histology and Histopathology
, vol.19
, Issue.4
, pp. 1345-1351
-
-
Pro, B.1
Dang, N.H.2
-
283
-
-
77952814507
-
Inhibition of multifunctional dipeptidyl peptidase-IV: Is there a risk of oncological and immunological adverse effects?
-
T. Stulc, and A. Sedo Inhibition of multifunctional dipeptidyl peptidase-IV: is there a risk of oncological and immunological adverse effects? Diabetes Res. Clin. Pr. 88 2010 125 131
-
(2010)
Diabetes Res. Clin. Pr.
, vol.88
, pp. 125-131
-
-
Stulc, T.1
Sedo, A.2
-
284
-
-
84886587432
-
Prescribing gliptins: Enthusiasm should be coupled with caution
-
M.K. Garg, S. Kharb, and A. Pandit Prescribing gliptins: enthusiasm should be coupled with caution Ind. J. Endocrinol. Metab. 16 2012 324 325
-
(2012)
Ind. J. Endocrinol. Metab.
, vol.16
, pp. 324-325
-
-
Garg, M.K.1
Kharb, S.2
Pandit, A.3
-
285
-
-
84860638209
-
The cardiovascular effects of GLP-1 receptor agonists
-
T. Okerson, and R.J. Chilton The cardiovascular effects of GLP-1 receptor agonists Cardiovasc. Ther. 30 2012 e146 e155
-
(2012)
Cardiovasc. Ther.
, vol.30
-
-
Okerson, T.1
Chilton, R.J.2
-
286
-
-
79951884751
-
Glucagon-like peptide-1-based therapies and cardiovascular disease: Looking beyond glycaemic control
-
P. Anagnostis, V.G. Athyros, F. Adamidou, and A. Panagiotou et al. Glucagon-like peptide-1-based therapies and cardiovascular disease: looking beyond glycaemic control Diabetes Obes. Metab. 13 2011 302 312
-
(2011)
Diabetes Obes. Metab.
, vol.13
, pp. 302-312
-
-
Anagnostis, P.1
Athyros, V.G.2
Adamidou, F.3
Panagiotou, A.4
-
287
-
-
80051795160
-
Cardiovascular effects of DPP-4 inhibition: Beyond GLP-1
-
G.P. Fadini, and A. Avogaro Cardiovascular effects of DPP-4 inhibition: beyond GLP-1 Vasc. Pharmacol. 55 2011 10 16
-
(2011)
Vasc. Pharmacol.
, vol.55
, pp. 10-16
-
-
Fadini, G.P.1
Avogaro, A.2
-
288
-
-
62949195390
-
Synergy between CD26/DPP IV inhibition and G-CSF improves cardiac function after acute myocardial infarction
-
M.M. Zaruba, H.D. Theiss, M. Vallaster, and U. Mehl et al. Synergy between CD26/DPP IV inhibition and G-CSF improves cardiac function after acute myocardial infarction Cell. Stem Cell. 4 2009 313 323
-
(2009)
Cell. Stem Cell.
, vol.4
, pp. 313-323
-
-
Zaruba, M.M.1
Theiss, H.D.2
Vallaster, M.3
Mehl, U.4
-
289
-
-
36448936053
-
Common pathological processes in Alzheimer disease and type 2 diabetes: A review
-
DOI 10.1016/j.brainresrev.2007.09.001, PII S0165017307001907
-
L. Li, and C. Holscher Common pathological processes in Alzheimer disease and type 2 diabetes: a review Brain Res. Rev. 56 2007 384 402 (Pubitemid 350166529)
-
(2007)
Brain Research Reviews
, vol.56
, Issue.2
, pp. 384-402
-
-
Li, L.1
Holscher, C.2
-
290
-
-
76749116176
-
Long-term inhibition of dipeptidyl peptidase-4 in Alzheimer's prone mice
-
M.D. Amico, C.D. Filippo, and R. Marfella et al. Long-term inhibition of dipeptidyl peptidase-4 in Alzheimer's prone mice Exp. Gerontol. 45 2010 202 207
-
(2010)
Exp. Gerontol.
, vol.45
, pp. 202-207
-
-
Amico, M.D.1
Filippo, C.D.2
Marfella, R.3
-
293
-
-
49849094738
-
Physiochemical drug properties associated with in vivo toxicological outcomes
-
J.D. Hughes, J. Blagg, D.A. Price, and S. Bailey et al. Physiochemical drug properties associated with in vivo toxicological outcomes Bioorg. Med. Chem. Lett. 18 2008 4872 4875
-
(2008)
Bioorg. Med. Chem. Lett.
, vol.18
, pp. 4872-4875
-
-
Hughes, J.D.1
Blagg, J.2
Price, D.A.3
Bailey, S.4
-
294
-
-
78650915884
-
RBx-0597, a potent, selective and slow-binding inhibitor of dipeptidyl peptidase-IV for the treatment of type 2 diabetes
-
S. Singh, S. Sethi, V. Khanna, and B. Benjamin et al. RBx-0597, a potent, selective and slow-binding inhibitor of dipeptidyl peptidase-IV for the treatment of type 2 diabetes Eur. J. Pharmacol. 652 2011 157 163
-
(2011)
Eur. J. Pharmacol.
, vol.652
, pp. 157-163
-
-
Singh, S.1
Sethi, S.2
Khanna, V.3
Benjamin, B.4
-
295
-
-
77955456705
-
Pharmacokinetics of dipeptidylpeptidase-4 inhibitors
-
A.J. Scheen Pharmacokinetics of dipeptidylpeptidase-4 inhibitors Diabetes Obes. Metab. 12 2010 648 658
-
(2010)
Diabetes Obes. Metab.
, vol.12
, pp. 648-658
-
-
Scheen, A.J.1
-
296
-
-
84861683713
-
Clinical pharmacokinetics and pharmacodynamics of linalglitin
-
U. Graefe-Mody, S. Retlich, and C. Friedrich Clinical pharmacokinetics and pharmacodynamics of linalglitin Clin. Pharmacokinet. 51 2012 411 427
-
(2012)
Clin. Pharmacokinet.
, vol.51
, pp. 411-427
-
-
Graefe-Mody, U.1
Retlich, S.2
Friedrich, C.3
-
297
-
-
84863735141
-
Modulation of cytochrome-P450 inhibition (CYP) in drug discovery: A medicinal chemistry perspective
-
S. Kumar, R. Sharma, and A. Roychowdhury modulation of cytochrome-P450 inhibition (CYP) in drug discovery: a medicinal chemistry perspective Curr. Med. Chem. 19 2012 3605 3621
-
(2012)
Curr. Med. Chem.
, vol.19
, pp. 3605-3621
-
-
Kumar, S.1
Sharma, R.2
Roychowdhury, A.3
-
298
-
-
33745413284
-
Quantitative structure - Activity relationship studies on inhibition of HERG potassium channels
-
DOI 10.1021/ci050450g
-
K. Yoshida, and T. Niwa Quantitative structure-activity relationship studies on inhibition of hERG potassium channels J. Chem. Inf. Model 46 2006 1371 1378 (Pubitemid 43999180)
-
(2006)
Journal of Chemical Information and Modeling
, vol.46
, Issue.3
, pp. 1371-1378
-
-
Yoshida, K.1
Niwa, T.2
-
299
-
-
78049442434
-
In silico binary classification QSAR models based on 4D-fingerprints and MOE descriptors for prediction of hERG blockage
-
B.-H. Su, M.-Y. Shen, E.X. Esposito, and A.J. Hopfinger et al. In silico binary classification QSAR models based on 4D-fingerprints and MOE descriptors for prediction of hERG blockage J. Chem. Inf. Model 50 2010 1304 1318
-
(2010)
J. Chem. Inf. Model
, vol.50
, pp. 1304-1318
-
-
Su, B.-H.1
Shen, M.-Y.2
Esposito, E.X.3
Hopfinger, A.J.4
-
300
-
-
0038487659
-
Prediction of hERG potassium channel affinity by traditional and hologram QSAR methods
-
DOI 10.1016/S0960-894X(03)00492-X
-
G. Keseru Prediction of hERG potassium channel affinity by traditional and hologram qSAR methods Bioorg. Chem. Med. Lett. 13 2003 2773 2775 (Pubitemid 36851568)
-
(2003)
Bioorganic and Medicinal Chemistry Letters
, vol.13
, Issue.16
, pp. 2773-2775
-
-
Keseru, G.M.1
-
301
-
-
33244474244
-
Development and evaluation of an in silico model for hERG binding
-
M. Song, and M. Clark Development and evaluation of an in silico model for hERG binding J. Chem. Inf. Model 46 2005 392 400
-
(2005)
J. Chem. Inf. Model
, vol.46
, pp. 392-400
-
-
Song, M.1
Clark, M.2
-
302
-
-
33644971220
-
Prediction of hERG potassium channel affinity by the CODESSA approach
-
Coi, I. Massarelli, L. Murgia, and M. Saraceno et al. Prediction of hERG potassium channel affinity by the CODESSA approach Bioorg. Med. Chem. 14 2006 3153 3159
-
(2006)
Bioorg. Med. Chem.
, vol.14
, pp. 3153-3159
-
-
Coi1
Massarelli, I.2
Murgia, L.3
Saraceno, M.4
-
303
-
-
82355160734
-
A critical assessment of combined ligand- and structure-based approaches to hERG channel blocker modeling
-
L. Du-Cuny, L. Chen, and S. Zhang A critical assessment of combined ligand- and structure-based approaches to hERG channel blocker modeling J. Chem. Inf. Model 51 2011 2948 2960
-
(2011)
J. Chem. Inf. Model
, vol.51
, pp. 2948-2960
-
-
Du-Cuny, L.1
Chen, L.2
Zhang, S.3
-
304
-
-
0037194634
-
+ channel blockers
-
DOI 10.1021/jm0208875
-
Cavalli, E. Poluzzi, F. De Ponti, and M. Recanatini Toward a pharmacophore for drugs inducing the long QT syndrome: insights from a CoMFA study of hERG K+ channel blockers J. Med. Chem. 45 2002 3844 3853 (Pubitemid 35024289)
-
(2002)
Journal of Medicinal Chemistry
, vol.45
, Issue.18
, pp. 3844-3853
-
-
Cavalli, A.1
Poluzzi, E.2
De Ponti, F.3
Recanatini, M.4
-
305
-
-
0036229805
-
Three-dimensional quantitative structure-activity relationship for inhibition of human ether-a-go-go-related gene potassium channel
-
DOI 10.1124/jpet.301.2.427
-
S. Ekins, W.J. Crumb, R.D. Sarazan, and J.H. Wikel et al. A three-dimensional quantitative stucture-activity relationship for inhibition of human ether-a-go-go-related gene potassium channel J. Pharmacol. Exp. Ther. 301 2002 427 434 (Pubitemid 34429951)
-
(2002)
Journal of Pharmacology and Experimental Therapeutics
, vol.301
, Issue.2
, pp. 427-434
-
-
Ekins, S.1
Crumb, W.J.2
Dustan Sarazan, R.3
Wikel, J.H.4
Wrighton, S.A.5
-
307
-
-
33750998518
-
Common pharmacophores for uncharged human ether-a-go-go-related gene (hERG) blockers
-
DOI 10.1021/jm060500o
-
A.M. Aronov Common pharmacophores for uncharged human ether-a-go-go-related gene (hERG) blockers J. Med. Chem. 49 2006 6917 6921 (Pubitemid 44749757)
-
(2006)
Journal of Medicinal Chemistry
, vol.49
, Issue.23
, pp. 6917-6921
-
-
Aronov, A.M.1
-
308
-
-
0038743107
-
Characterization of HERG potassium channel inhibition using CoMSiA 3D QSAR and homology modeling approaches
-
DOI 10.1016/S0960-894X(03)00196-3
-
R.A. Pearlstein, R.J. Vaz, J. Kang, and X.-L. Chen et al. Characterization of hERG potassium channel inhibition using CoMSIA 3D QSAR and homology modeling approaches Bioorg. Chem. Med. Lett. 13 2003 1829 1835 (Pubitemid 36561175)
-
(2003)
Bioorganic and Medicinal Chemistry Letters
, vol.13
, Issue.10
, pp. 1829-1835
-
-
Pearlstein, R.A.1
Vaz, R.J.2
Kang, J.3
Chen, X.-L.4
Preobrazhenskaya, M.5
Shchekotikhin, A.E.6
Korolev, A.M.7
Lysenkova, L.N.8
Miroshnikova, O.V.9
Hendrix, J.10
Rampe, D.11
-
309
-
-
79952124934
-
Combined receptor and ligand-based approach to the universal pharmacophore model development for studies of drug blockade to the hERG pore domain
-
S. Durdagi, H.J. Duff, and S.Y. Noskov Combined receptor and ligand-based approach to the universal pharmacophore model development for studies of drug blockade to the hERG pore domain J. Chem. Inf. Model. 51 2011 463 474
-
(2011)
J. Chem. Inf. Model.
, vol.51
, pp. 463-474
-
-
Durdagi, S.1
Duff, H.J.2
Noskov, S.Y.3
-
311
-
-
84860310064
-
Computational design and discovery of "minimally structured" hERG blockers
-
A. Cavalli, R. Buonfiglio, and C. Ianni et al. Computational design and discovery of "minimally structured" hERG blockers J. Med. Chem. 55 2012 4010 4014
-
(2012)
J. Med. Chem.
, vol.55
, pp. 4010-4014
-
-
Cavalli, A.1
Buonfiglio, R.2
Ianni, C.3
-
312
-
-
13844254976
-
Predictive in silico modeling for hERG channel blockers
-
DOI 10.1016/S1359-6446(04)03278-7, PII S1359644604032787
-
A.M. Aronov Predictive in-silico modelling for hERG channel blockers Drug. Discov. Today 10 2005 149 155 (Pubitemid 40247813)
-
(2005)
Drug Discovery Today
, vol.10
, Issue.2
, pp. 149-155
-
-
Aronov, A.M.1
|