Title:
VLA-4 INTEGRIN ANTAGONISTS
Document Type and Number:
WIPO Patent Application WO2001042192
Kind Code:
A3
Abstract:
Compounds of formula (I) wherein Ar is carbocyclic or heterocyclic aryl, or biaryl; Q is O, S or N-CN; X is arylene; V is NH, O, NHOH, CH2 or a direct bond; W is NH, O, NHOH, CH2 or a direct bond; Alk is C2-C7-alkylene or C2-C7-alkylene interrupted by O, S, SO, SO2 or NR3; Y is amino, acylamino, mono- or di- (lower alkyl, aryl or aralkyl)-amino, pyrrolidino, perhydroazepino or a group of the formula (II) in which M1 is N; and M2 is CH2, O, NR3, S, SO or SO2; R1, R2 and R3 are independently hydrogen, lower alkyl, lower alkenyl, cycloalkyl, aryl, cycloalkyl-lower alkyl, aryl-lower alkyl or aryl-lower alkenyl; Z is lower alkylene or lower alkylene substituted by one or more of lower alkyl, lower alkenyl, cycloalkyl, aryl, cycloalkyl-lower alkyl, aryl-lower alkyl or aryl-lower alkenyl; or Z is lower alkylene interrupted by O, S, SO, SO2 or NR3; pharmaceutically acceptable esters and amides thereof; and pharmaceutically acceptable salts thereof, which are useful as VLA-4 integrin antagonists.
Inventors:
WATTANASIN SOMPONG (US)
WEIDMANN BEAT (US)
WEIDMANN BEAT (US)
Application Number:
PCT/EP2000/012226
Publication Date:
January 10, 2002
Filing Date:
December 05, 2000
Export Citation:
Assignee:
NOVARTIS AG (CH)
NOVARTIS ERFIND VERWALT GMBH (AT)
WATTANASIN SOMPONG (US)
WEIDMANN BEAT (US)
NOVARTIS ERFIND VERWALT GMBH (AT)
WATTANASIN SOMPONG (US)
WEIDMANN BEAT (US)
International Classes:
C07D295/12; A61K31/197; A61K31/5375; A61K31/5377; A61P11/00; A61P19/02; A61P27/02; A61P37/06; A61P43/00; C07C273/18; C07C275/42; C07C279/28; C07D295/13; C07D295/18; C07D295/185; (IPC1-7): C07C275/38; A61K31/17; A61K31/5375; A61P27/02; C07D295/13
Domestic Patent References:
| WO1999037605A1 | 1999-07-29 | |||
| WO1998004247A1 | 1998-02-05 |
Foreign References:
| US5936065A | 1999-08-10 |
Download PDF: