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Title:
AMINOPYRIDINYL-, AMINOGUANIDINYL- AND ALKOXYGUANIDINYL- SUBSTITUTED PHENYL ACETAMIDES AS PROTEASE INHIBITORS
Document Type and Number:
WIPO Patent Application WO2002028825
Kind Code:
A3
Abstract:
Phenyl acetamide compounds are described, including compounds of Formula (I): or a solvate, hydrate or pharmaceutically acceptable salt thereof; wherein R<3>-R<6>, R<11>, B, Y and W are set forth in the specification. The compounds of the invention are potent inhibitors of proteases, especially trypsin-like serine proteases, such as thrombin and factor Xa. Compositions for inhibiting loss of blood platelets, inhibiting formation of blood platelet aggregates, inhibiting formation of fibrin, inhibiting thrombus formation, and inhibiting embolus formation are described. Other uses of compounds of the invention are as anticoagulants either embedded in or physically linked to materials used in the manufacture of devices used in blood collection, blood circulation, and blood storage, such as catheters, blood dialysis machines, blood collection syringes and tubes, blood lines and stents. Additionally, the compounds can be detectably labeled and employed for in vivo imaging for thrombi.

Inventors:
PAN WENXI
LU TIANBAO
MARKOTAN THOMAS P
TOMCZUK BRUCE E
Application Number:
US0131249W
Publication Date:
June 13, 2002
Filing Date:
October 05, 2001
Export Citation:
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Assignee:
DIMENSIONAL PHARM INC (US)
International Classes:
A61K31/155; A61K31/165; A61K31/18; A61K31/255; A61K31/44; A61K45/00; A61L31/00; A61P7/02; A61P9/08; A61P9/10; A61P29/00; A61P43/00; C07C279/00; C07C279/04; C07C291/02; C07C309/67; C07C309/73; C07C311/13; C07C311/21; C07D213/73; C07D213/75; (IPC1-7): C07C279/00; C07D213/40; A61K31/155; A61K31/44; C07C317/14
Domestic Patent References:
WO1999026926A11999-06-03
WO1997001338A11997-01-16
WO1996040100A11996-12-19
WO1999051571A11999-10-14
WO1998023565A21998-06-04
Foreign References:
DE19937494A12001-02-08
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