-
1
-
-
0019513437
-
Maintenance of blood pressure by the renin-angiotensin system in normal man
-
MacGregor, G. A.; Markandu, N. D.; Roulston, J. E.; Jones, J. C.; Morton, J. J. Maintenance of blood pressure by the renin-angiotensin system in normal man Nature 1981, 291, 329-331 10.1038/291329a0
-
(1981)
Nature
, vol.291
, pp. 329-331
-
-
MacGregor, G.A.1
Markandu, N.D.2
Roulston, J.E.3
Jones, J.C.4
Morton, J.J.5
-
2
-
-
0036690114
-
Drugs Targeting the Renin-Angiotensin-Aldosterone System
-
Zaman, M. A.; Oparil, S.; Calhoun, D. A. Drugs Targeting the Renin-Angiotensin-Aldosterone System Nat. Rev. Drug Discovery 2002, 1, 621-636 10.1038/nrd873
-
(2002)
Nat. Rev. Drug Discovery
, vol.1
, pp. 621-636
-
-
Zaman, M.A.1
Oparil, S.2
Calhoun, D.A.3
-
3
-
-
84895070950
-
The effect of RAAS blockade on the progression of diabetic nephropathy
-
Roscioni, S. S.; Lambers Heerspink, H. J.; de Zeeuw, D. The effect of RAAS blockade on the progression of diabetic nephropathy Nat. Rev. Nephrol. 2014, 10, 77-87 10.1038/nrneph.2013.251
-
(2014)
Nat. Rev. Nephrol.
, vol.10
, pp. 77-87
-
-
Roscioni, S.S.1
Lambers Heerspink, H.J.2
De Zeeuw, D.3
-
5
-
-
77955415650
-
Application of direct renin inhibition to chronic kidney diseases
-
Mende, C. W. Application of direct renin inhibition to chronic kidney diseases Cardiovasc. Drugs Ther. 2010, 24, 139-149 10.1007/s10557-010-6232-1
-
(2010)
Cardiovasc. Drugs Ther.
, vol.24
, pp. 139-149
-
-
Mende, C.W.1
-
7
-
-
78149259520
-
Direct renin inhibitors as a new therapy for hypertension
-
Webb, R. L.; Schiering, N.; Sedrani, R.; Maibaum, J. Direct renin inhibitors as a new therapy for hypertension J. Med. Chem. 2010, 53, 7490-7520 10.1021/jm901885s
-
(2010)
J. Med. Chem.
, vol.53
, pp. 7490-7520
-
-
Webb, R.L.1
Schiering, N.2
Sedrani, R.3
Maibaum, J.4
-
8
-
-
46849092364
-
Recent advances in the discovery of non-peptidic direct renin inhibitors as antihypertensives
-
Yokokawa, F.; Maibaum, J. Recent advances in the discovery of non-peptidic direct renin inhibitors as antihypertensives Expert Opin. Ther. Pat. 2008, 18, 581-602 10.1517/13543776.18.6.581
-
(2008)
Expert Opin. Ther. Pat.
, vol.18
, pp. 581-602
-
-
Yokokawa, F.1
Maibaum, J.2
-
9
-
-
84877951910
-
Recent progress on the discovery of non-peptidic direct renin inhibitors for the clinical management of hypertension
-
Yokokawa, F. Recent progress on the discovery of non-peptidic direct renin inhibitors for the clinical management of hypertension Expert Opin. Drug Discovery 2013, 8, 673-690 10.1517/17460441.2013.791279
-
(2013)
Expert Opin. Drug Discovery
, vol.8
, pp. 673-690
-
-
Yokokawa, F.1
-
10
-
-
34848869297
-
Structural modification of the P2′ position of 2,7-dialkyl-substituted 5(S)- amino-4(S)-hydroxy-8-phenyl-octanecarboxamides: The discovery of aliskiren, a potent nonpeptide human renin inhibitor active after once daily dosing in marmosets
-
Maibaum, J.; Stutz, S.; Göschke, R.; Rigollier, P.; Yamaguchi, Y.; Cumin, F.; Rahuel, J.; Baum, H.-P.; Cohen, N.-C.; Schnell, C. R.; Fuhrer, W.; Gruetter, M. G.; Schilling, W.; Wood, J. M. Structural modification of the P2′ position of 2,7-dialkyl-substituted 5(S)- amino-4(S)-hydroxy-8-phenyl-octanecarboxamides: the discovery of aliskiren, a potent nonpeptide human renin inhibitor active after once daily dosing in marmosets J. Med. Chem. 2007, 50, 4832-4844 10.1021/jm070316i
-
(2007)
J. Med. Chem.
, vol.50
, pp. 4832-4844
-
-
Maibaum, J.1
Stutz, S.2
Göschke, R.3
Rigollier, P.4
Yamaguchi, Y.5
Cumin, F.6
Rahuel, J.7
Baum, H.-P.8
Cohen, N.-C.9
Schnell, C.R.10
Fuhrer, W.11
Gruetter, M.G.12
Schilling, W.13
Wood, J.M.14
-
11
-
-
47049089844
-
Clinical pharmacokinetics and pharmacodynamics of aliskiren
-
Vaidyanathan, S.; Jarugula, V.; Dieterich, H. A.; Howard, D.; Dole, W. P. Clinical pharmacokinetics and pharmacodynamics of aliskiren Clin. Pharmacokinet. 2008, 47, 515-531 10.2165/00003088-200847080-00002
-
(2008)
Clin. Pharmacokinet.
, vol.47
, pp. 515-531
-
-
Vaidyanathan, S.1
Jarugula, V.2
Dieterich, H.A.3
Howard, D.4
Dole, W.P.5
-
12
-
-
84992183957
-
Structure-based design of a new series of N-(piperidin-3-yl)pyrimidine-5-carboxamides as renin inhibitors
-
published online September 13, 2016; DOI
-
Imaeda, Y.; Tawada, M.; Suzuki, S.; Tomimoto, M.; Kondo, M.; Tarui, N.; Sanada, T.; Kanagawa, R.; Snell, G.; Behnke, C. A.; Kubo, K.; Kuroita, T. Structure-based design of a new series of N-(piperidin-3-yl)pyrimidine-5-carboxamides as renin inhibitors. Bioorg. Med. Chem., published online September 13, 2016; DOI: 10.1016/j.bmc.2016.09.030.
-
Bioorg. Med. Chem.
-
-
Imaeda, Y.1
Tawada, M.2
Suzuki, S.3
Tomimoto, M.4
Kondo, M.5
Tarui, N.6
Sanada, T.7
Kanagawa, R.8
Snell, G.9
Behnke, C.A.10
Kubo, K.11
Kuroita, T.12
-
13
-
-
84875712582
-
A novel class of oral direct renin inhibitors: Highly potent 3,5-disubstituted piperidines bearing a tricyclic p3-p1 pharmacophore
-
Ostermann, N.; Ruedisser, S.; Ehrhardt, C.; Breitenstein, W.; Marzinzik, A.; Jacoby, E.; Vangrevelinghe, E.; Ottl, J.; Klumpp, M.; Hartwieg, J. C.; Cumin, F.; Hassiepen, U.; Trappe, J.; Sedrani, R.; Geisse, S.; Gerhartz, B.; Richert, P.; Francotte, E.; Wagner, T.; Krömer, M.; Kosaka, T.; Webb, R. L.; Rigel, D. F.; Maibaum, J.; Baeschlin, D. K. A novel class of oral direct renin inhibitors: highly potent 3,5-disubstituted piperidines bearing a tricyclic p3-p1 pharmacophore J. Med. Chem. 2013, 56, 2196-2206 10.1021/jm301706j
-
(2013)
J. Med. Chem.
, vol.56
, pp. 2196-2206
-
-
Ostermann, N.1
Ruedisser, S.2
Ehrhardt, C.3
Breitenstein, W.4
Marzinzik, A.5
Jacoby, E.6
Vangrevelinghe, E.7
Ottl, J.8
Klumpp, M.9
Hartwieg, J.C.10
Cumin, F.11
Hassiepen, U.12
Trappe, J.13
Sedrani, R.14
Geisse, S.15
Gerhartz, B.16
Richert, P.17
Francotte, E.18
Wagner, T.19
Krömer, M.20
Kosaka, T.21
Webb, R.L.22
Rigel, D.F.23
Maibaum, J.24
Baeschlin, D.K.25
more..
-
14
-
-
84904330469
-
Structure-based design of substituted piperidines as a new class of highly efficacious oral direct Renin inhibitors
-
Ehara, T.; Irie, O.; Kosaka, T.; Kanazawa, T.; Breitenstein, W.; Grosche, P.; Ostermann, N.; Suzuki, M.; Kawakami, S.; Konishi, K.; Hitomi, Y.; Toyao, A.; Gunji, H.; Cumin, F.; Schiering, N.; Wagner, T.; Rigel, D. F.; Webb, R. L.; Maibaum, J.; Yokokawa, F. Structure-based design of substituted piperidines as a new class of highly efficacious oral direct Renin inhibitors ACS Med. Chem. Lett. 2014, 5, 787-792 10.1021/ml500137b
-
(2014)
ACS Med. Chem. Lett.
, vol.5
, pp. 787-792
-
-
Ehara, T.1
Irie, O.2
Kosaka, T.3
Kanazawa, T.4
Breitenstein, W.5
Grosche, P.6
Ostermann, N.7
Suzuki, M.8
Kawakami, S.9
Konishi, K.10
Hitomi, Y.11
Toyao, A.12
Gunji, H.13
Cumin, F.14
Schiering, N.15
Wagner, T.16
Rigel, D.F.17
Webb, R.L.18
Maibaum, J.19
Yokokawa, F.20
more..
-
15
-
-
0031024171
-
Experimental and computational approaches to estimate solubility and permeability in drug discovery and development settings
-
Lipinski, C. A.; Lombardo, F.; Dominy, B. W.; Feeney, P. J. Experimental and computational approaches to estimate solubility and permeability in drug discovery and development settings Adv. Drug Delivery Rev. 1997, 23, 3-25 10.1016/S0169-409X(96)00423-1
-
(1997)
Adv. Drug Delivery Rev.
, vol.23
, pp. 3-25
-
-
Lipinski, C.A.1
Lombardo, F.2
Dominy, B.W.3
Feeney, P.J.4
-
16
-
-
0037030653
-
Molecular properties that influence the oral bioavailability of drug candidates
-
Veber, D. F.; Johnson, S. R.; Cheng, H.-Y.; Smith, B. R.; Ward, K. W.; Kopple, K. D. Molecular properties that influence the oral bioavailability of drug candidates J. Med. Chem. 2002, 45, 2615-2623 10.1021/jm020017n
-
(2002)
J. Med. Chem.
, vol.45
, pp. 2615-2623
-
-
Veber, D.F.1
Johnson, S.R.2
Cheng, H.-Y.3
Smith, B.R.4
Ward, K.W.5
Kopple, K.D.6
-
17
-
-
0036127307
-
Biotransformation reactions of five-membered aromatic heterocyclic rings
-
Dalvie, D. K.; Kalgutkar, A. S.; Khojasteh-bakht, S. C.; Obach, R. S.; O'Donnell, J. P. Biotransformation reactions of five-membered aromatic heterocyclic rings Chem. Res. Toxicol. 2002, 15, 269-299 10.1021/tx015574b
-
(2002)
Chem. Res. Toxicol.
, vol.15
, pp. 269-299
-
-
Dalvie, D.K.1
Kalgutkar, A.S.2
Khojasteh-Bakht, S.C.3
Obach, R.S.4
O'Donnell, J.P.5
-
18
-
-
18944393300
-
Bioactivation of 4-ipomeanol by CYP4B1: Adduct characterization and evidence for an enedial intermediate
-
Baer, B. R.; Rettie, A. E.; Henne, K. R. Bioactivation of 4-ipomeanol by CYP4B1: adduct characterization and evidence for an enedial intermediate Chem. Res. Toxicol. 2005, 18, 855-864 10.1021/tx0496993
-
(2005)
Chem. Res. Toxicol.
, vol.18
, pp. 855-864
-
-
Baer, B.R.1
Rettie, A.E.2
Henne, K.R.3
-
19
-
-
84870239487
-
Design and discovery of new (3S,5R)-5-[4-(2-chlorophenyl)-2,2-dimethyl-5-oxopiperazin-1-yl]piperidine-3-carboxamides as potent renin inhibitors
-
Mori, Y.; Ogawa, Y.; Mochizuki, A.; Nakamura, Y.; Sugita, C.; Miyazaki, S.; Tamaki, K.; Matsui, Y.; Takahashi, M.; Nagayama, T.; Nagai, Y.; Inoue, S.; Nishi, T. Design and discovery of new (3S,5R)-5-[4-(2-chlorophenyl)-2,2-dimethyl-5-oxopiperazin-1-yl]piperidine-3-carboxamides as potent renin inhibitors Bioorg. Med. Chem. Lett. 2012, 22, 7677-7682 10.1016/j.bmcl.2012.09.103
-
(2012)
Bioorg. Med. Chem. Lett.
, vol.22
, pp. 7677-7682
-
-
Mori, Y.1
Ogawa, Y.2
Mochizuki, A.3
Nakamura, Y.4
Sugita, C.5
Miyazaki, S.6
Tamaki, K.7
Matsui, Y.8
Takahashi, M.9
Nagayama, T.10
Nagai, Y.11
Inoue, S.12
Nishi, T.13
-
20
-
-
71049126548
-
Escape from Flatland: Increasing Saturation as an Approach to Improving Clinical Success
-
Lovering, F.; Bikker, J.; Humbelt, C. Escape from Flatland: Increasing Saturation as an Approach to Improving Clinical Success J. Med. Chem. 2009, 52, 6752-6756 10.1021/jm901241e
-
(2009)
J. Med. Chem.
, vol.52
, pp. 6752-6756
-
-
Lovering, F.1
Bikker, J.2
Humbelt, C.3
-
21
-
-
34447109128
-
The role of molecular size in ligand efficiency
-
Reynolds, C. H.; Bembenek, S. D.; Tounge, B. A. The role of molecular size in ligand efficiency Bioorg. Med. Chem. Lett. 2007, 17, 4258-4261 10.1016/j.bmcl.2007.05.038
-
(2007)
Bioorg. Med. Chem. Lett.
, vol.17
, pp. 4258-4261
-
-
Reynolds, C.H.1
Bembenek, S.D.2
Tounge, B.A.3
-
22
-
-
35748934487
-
The Influence of Drug-like Concepts on Decision-Making in Medicinal Chemistry
-
Leeson, P. D.; Springthorpe, B. The Influence of Drug-like Concepts on Decision-Making in Medicinal Chemistry Nat. Rev. Drug Discovery 2007, 6, 881-890 10.1038/nrd2445
-
(2007)
Nat. Rev. Drug Discovery
, vol.6
, pp. 881-890
-
-
Leeson, P.D.1
Springthorpe, B.2
-
23
-
-
67649962669
-
2 agonists using parallel synthesis protocols: A Lipophilic Efficiency (LipE) analysis
-
2 agonists using parallel synthesis protocols: A Lipophilic Efficiency (LipE) analysis Bioorg. Med. Chem. Lett. 2009, 19, 4406-4409 10.1016/j.bmcl.2009.05.062
-
(2009)
Bioorg. Med. Chem. Lett.
, vol.19
, pp. 4406-4409
-
-
Ryckmans, T.1
Edwards, M.P.2
Horne, V.A.3
Correia, A.M.4
Owen, D.R.5
Thompson, L.R.6
Tran, I.7
Tutt, M.F.8
Young, T.9
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