Title:
2-CYANOPYRROLIDINE DERIVATIVES AND THEIR USE AS MEDICAMENTS
Document Type and Number:
WIPO Patent Application WO2001096295
Kind Code:
A3
Abstract:
The present invention relates to certain N-(substituted glycyl)-2-cyanopyrrolidines of formula (I) wherein Y is as defined herein, in free form or in acid addition salt form. Compounds of formula (I) inhibit DPP-IV (dipeptidyl-peptidase-IV) activity. They are therefore indicated for use as pharmaceuticals in inhibiting DPP-IV and in the treatment of conditions mediated by DPP-IV, such as non-insulin-dependent diabetes mellitus, arthritis, obesity, osteoporosis and further conditions of impaired glucose tolerance.
Inventors:
VILLHAUER EDWIN BERNARD (US)
Application Number:
PCT/EP2001/006595
Publication Date:
May 16, 2002
Filing Date:
June 11, 2001
Export Citation:
Assignee:
NOVARTIS AG (CH)
NOVARTIS ERFIND VERWALT GMBH (AT)
VILLHAUER EDWIN BERNARD (US)
NOVARTIS ERFIND VERWALT GMBH (AT)
VILLHAUER EDWIN BERNARD (US)
International Classes:
A61K31/40; A61K31/427; A61K31/428; A61K31/4439; A61K31/454; A61K31/506; A61P3/04; A61P3/08; A61P3/10; A61P19/02; A61P19/10; A61P43/00; C07D207/16; C07D401/12; C07D403/12; C07D409/12; C07D417/12; C07D417/14; (IPC1-7): C07D401/12; C07D207/16; C07D403/12; C07D417/12; C07D409/12; A61K31/40; A61K31/4439; A61K31/506; A61K31/428; A61K31/427; A61P3/10
Domestic Patent References:
| WO1998019998A2 | 1998-05-14 |
Foreign References:
| US6011155A | 2000-01-04 | |||
| EP0419683A1 | 1991-04-03 |
Other References:
T. E. HUGHES ET AL.: "(1-[[[2-[(5-Cyanopyridin-2-yl]amino]- acetyl]-2-cyano-(S)-pyrrolidine), a Slow-Binding Inhibitor of Dipeptidyl Peptidase IV", BIOCHEMISTRY, vol. 38, no. 36, 1999, pages 11597 - 11603, XP002184055
BALKAN B ET AL: "INHIBITION OF DIPEPTIDYL PEPTIDASE IV WITH NVP-DPP728 INCREASES PLASMA GLP-1 (7-36 AMIDE) CONCENTRATIONS AND IMPROVES ORAL GLUCOSE TOLERANCE IN OBESE ZUCKER RATS", DIABETOLOGIA, BERLIN, DE, vol. 42, no. 11, November 1999 (1999-11-01), pages 1324 - 1331, XP000921066, ISSN: 0012-186X
BALKAN B ET AL: "INHIBITION OF DIPEPTIDYL PEPTIDASE IV WITH NVP-DPP728 INCREASES PLASMA GLP-1 (7-36 AMIDE) CONCENTRATIONS AND IMPROVES ORAL GLUCOSE TOLERANCE IN OBESE ZUCKER RATS", DIABETOLOGIA, BERLIN, DE, vol. 42, no. 11, November 1999 (1999-11-01), pages 1324 - 1331, XP000921066, ISSN: 0012-186X
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