-
1
-
-
0036228243
-
-
J.A. Pospisilik, S.G. Stafford, H.-U. Demuth, R. Brownsey, H. Parkhouse, D.T. Finegood, C.H.S. McIntosh, and R.A. Pederson Diabetes 51 2002 943
-
(2002)
Diabetes
, vol.51
, pp. 943
-
-
Pospisilik, J.A.1
Stafford, S.G.2
Demuth, H.-U.3
Brownsey, R.4
Parkhouse, H.5
Finegood, D.T.6
McIntosh, C.H.S.7
Pederson, R.A.8
-
8
-
-
84856220688
-
-
http://www.fiercebiotech.com/press-releases/galvus-new-treatment- patients-type-2-diabetes-receives-european-approval.
-
-
-
-
9
-
-
34249280590
-
-
T. Biftu, G. Scapin, S. Singha, D. Fenga, J.W. Becker, G. Eiermann, H. Hea, K. Lyonsa, S. Patela, A. Petrovb, R. Sinha-Royc, B. Zhang, J. Wuc, X. Zhang, G.A. Dossd, N.A. Thornberry, and A.E. Weber Bioorg. Med. Chem. Lett. 17 2007 3384
-
(2007)
Bioorg. Med. Chem. Lett.
, vol.17
, pp. 3384
-
-
Biftu, T.1
Scapin, G.2
Singha, S.3
Fenga, D.4
Becker, J.W.5
Eiermann, G.6
Hea, H.7
Lyonsa, K.8
Patela, S.9
Petrovb, A.10
Sinha-Royc, R.11
Zhang, B.12
Wuc, J.13
Zhang, X.14
Dossd, G.A.15
Thornberry, N.A.16
Weber, A.E.17
-
10
-
-
37349073397
-
-
M. Eckhardt, E. Langkopf, M. Todayyon, L. Thomas, H. Nar, W. Pfrengle, B. Guth, R. Lotz, P. Sieger, H. Fuchs, and F. Himmelsbach J. Med. Chem. 50 2007 6450
-
(2007)
J. Med. Chem.
, vol.50
, pp. 6450
-
-
Eckhardt, M.1
Langkopf, E.2
Todayyon, M.3
Thomas, L.4
Nar, H.5
Pfrengle, W.6
Guth, B.7
Lotz, R.8
Sieger, P.9
Fuchs, H.10
Himmelsbach, F.11
-
12
-
-
44149127222
-
-
E. Matthias, N. Hauel, F. Himmelsbach, E. Langkopf, H. Nar, M. Todayyon, L. Thomas, B. Guth, and R. Lotz Bioorg. Med. Chem. Lett. 18 2008 3158
-
(2008)
Bioorg. Med. Chem. Lett.
, vol.18
, pp. 3158
-
-
Matthias, E.1
Hauel, N.2
Himmelsbach, F.3
Langkopf, E.4
Nar, H.5
Todayyon, M.6
Thomas, L.7
Guth, B.8
Lotz, R.9
-
14
-
-
78449276647
-
-
Pyrrolopyrimidinones with deviating structure have been reported as DPP-4 inhibitors in Nakahira, H., Kimura, H., Hochigai, H. WO2006/068163
-
Pyrrolopyrimidinones with deviating structure have been reported as DPP-4 inhibitors in Nakahira, H., Kimura, H., Hochigai, H. WO2006/068163; Y. Nishio, H. Kimura, S. Tosaki, E. Sugaru, M. Sakai, M. Horiguchi, Y. Masui, M. Ono, T. Nakagawa, and H. Nakahira Bioorg. Med. Chem. Lett. 20 2010 7246
-
(2010)
Bioorg. Med. Chem. Lett.
, vol.20
, pp. 7246
-
-
Nishio, Y.1
Kimura, H.2
Tosaki, S.3
Sugaru, E.4
Sakai, M.5
Horiguchi, M.6
Masui, Y.7
Ono, M.8
Nakagawa, T.9
Nakahira, H.10
-
15
-
-
78649691630
-
-
M.R. Taskinen, J. Rosenstock, I. Tamminen, R. Kubiak, S. Patel, and K.A. Dugi Diabetes Obes. Metab. 13 2011 65
-
(2011)
Diabetes Obes. Metab.
, vol.13
, pp. 65
-
-
Taskinen, M.R.1
Rosenstock, J.2
Tamminen, I.3
Kubiak, R.4
Patel, S.5
Dugi, K.A.6
-
16
-
-
84856229360
-
-
http://www.fda.gov/NewsEvents/Newsroom/PressAnnouncements/ucm253501.
-
-
-
-
17
-
-
84856229357
-
-
Kataoka, K., Kosugi, T., Ishii, T., Takeuchi, T., Tsutsumi, T., Nakano, A., Unoki, G., Yamamoto, M., Sakai, Y. WO2003/070729
-
Kataoka, K., Kosugi, T., Ishii, T., Takeuchi, T., Tsutsumi, T., Nakano, A., Unoki, G., Yamamoto, M., Sakai, Y. WO2003/070729.
-
-
-
-
18
-
-
84856229361
-
-
note
-
Compounds were tested for their inhibitory potency against human DPP-4. Human DPP-4 (amino acids 39-766) with a C-terminal step-tag was expressed using the baculovirus system and purified to >80%, and stored in a 25 mM Tris buffer, pH 9, containing 300 mM NaCl at -80 °C. The substrate was kept at 5 mM stock solution in DMSO at -20 °C and the assay buffer for the DPP-4 reaction was 25 nM Tris/HCl, pH 7.5, containing 140 mM NaCl, 10 mM KCl and 0.05% (w/v) CHAPS.
-
-
-
-
19
-
-
29144522905
-
-
This observed boost in affinity moving from piperazine to aminopiperidine has been rationalised in terms of an additional hydrogen bonding ability and lower energy conformation
-
This observed boost in affinity moving from piperazine to aminopiperidine has been rationalised in terms of an additional hydrogen bonding ability and lower energy conformation: M. Engel, T. Hoffmann, S. Manhart, U. Heiser, S. Chambre, R. Huber, H.-U. Demuth, and W. Bode J. Mol. Biol. 356 2006 768
-
(2006)
J. Mol. Biol.
, vol.356
, pp. 768
-
-
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
-
20
-
-
84856218341
-
-
Linagliptin was prepared according to Himmelsbach, F., Langkopf, E., Eckhardt, M., Mark, M., Maier, R., Todayyon, M. WO2004/018468
-
Linagliptin was prepared according to Himmelsbach, F., Langkopf, E., Eckhardt, M., Mark, M., Maier, R., Todayyon, M. WO2004/018468.
-
-
-
-
21
-
-
84856220689
-
-
Milton, J., Wren, S., Wang, S., Folkes, A., Chuckowree, I., Hancox, T; Miller, W., Sohal, S. WO2004065389
-
Milton, J., Wren, S., Wang, S., Folkes, A., Chuckowree, I., Hancox, T; Miller, W., Sohal, S. WO2004065389.
-
-
-
-
22
-
-
25844459084
-
-
G.R. Lankas, B. Leiting, R.S. Roy, G.J. Eiermann, M.G. Beconi, T. Biftu, C.-C. Chan, S. Edmondson, W.P. Feeney, H. He, D.E. Ippolito, D. Kim, K.A. Lyons, H.O. Ok, R.A. Patel, A.N. Petrov, K.A. Pryor, X. Qian, L. Reigle, A. Woods, J.K. Wu, D. Zaller, X. Zhang, L. Zhu, A.E. Weber, and N.A. Thornberry Diabetes 54 2005 2988
-
(2005)
Diabetes
, vol.54
, pp. 2988
-
-
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..
-
23
-
-
41149118550
-
-
L. Thomas, M. Eckhardt, E. Langkopf, M. Tadayyon, F. Himmelsbach, and M. Mark J. Pharmacol. Exp. Ther. 325 2008 175
-
(2008)
J. Pharmacol. Exp. Ther.
, vol.325
, pp. 175
-
-
Thomas, L.1
Eckhardt, M.2
Langkopf, E.3
Tadayyon, M.4
Himmelsbach, F.5
Mark, M.6
-
24
-
-
84856218340
-
-
Himmelsbach, F., Mark, M., Tadayyon, M., Thomas, L. WO2009/024542
-
Himmelsbach, F., Mark, M., Tadayyon, M., Thomas, L. WO2009/024542.
-
-
-
-
25
-
-
84856229359
-
-
Baeschlin, D. K., Clark, D. E., Dunsdon, S. J., Fenton, G., Fillmore, A., Harris, N. V., Higgs, C., Hurley, C. A., Krintel, S. L., MacKenzie, R. E., Ostermann, N., Sirockin, F., Sutton, J. M. WO2007/071738
-
Baeschlin, D. K., Clark, D. E., Dunsdon, S. J., Fenton, G., Fillmore, A., Harris, N. V., Higgs, C., Hurley, C. A., Krintel, S. L., MacKenzie, R. E., Ostermann, N., Sirockin, F., Sutton, J. M. WO2007/071738.
-
-
-
|