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AZOLIDINONES DE METHYLENE DE PYRIDINE ET INHIBITEURS DE LA PHOSPHOINOSITIDE
专利权人:
APPLIED RESEARCH SYSTEMS ARS HOLDING N.V.
发明人:
RUECKLE, THOMAS,QUATTROPANI, ANNA,POMEL, VINCENT,DORBAIS, JEROME,COVINI, DAVID,BISCHOFF, ALEXANDER
申请号:
CA2576765
公开号:
CA2576765C
申请日:
2005.09.02
申请国别(地区):
CA
年份:
2013
代理人:
摘要:
The present invention is related to fused pyridine methylene azolidinonederivatives ofFormula (I)(see formula I)wherein R1 is selected from H, halogen, C1-C6-alkyl, C2-C6-alkenyl and C2-C6-alkynyl,C1-C6-alkyl alkoxy, alkoxycarbonyl, acyl, sulfonyl, sulfanyl, sulfinyl, alkoxyand amino;R2 is selected from H, halogen, C1-C6-alkyl, C2-C6-alkenyl, C2-C6-alkynyl;aryl; heteroaryl,C3-C8-cycloalkyl; C3-C8-heterocycloalkyl, aryl C1-C6-alkyl, heteroaryl C1-C6-alkyl,C3-C8-cycloalkyl C1-C6-alkyl, C3-C8-heterocycloalkyl C1-C6-alkyl, C1-C6-alkylalkoxy,alkoxycarbonyl, acyl, sulfonyl, sulfanyl, sulfinyl, alkoxy and amino;X is selected from S, NH and O;Y is selected from O, S and NR3, wherein R3 is selected from H, optionallysubstitutedC1-C6-alkoxy, optionally substituted C1-C6-alkyl, optionally substituted C2-C6-alkenyl,optionally substituted C2-C6-alkynyl, optionally substituted C1-C6-alkyl aryl,cyano andoptionally substituted sulfonyl;A is a heteroaryl group;n is an integer selected from 1 and 2;as well as its geometrical isomers, its optically active forms as enantiomers,diastereomersand its racemate forms, as well as pharmaceutically acceptable salts thereof,in particular for the treatment and/or prophylaxis of autoimmune disordersand/orinflammatory diseases, cardiovascular diseases, neurodegenerative diseases,bacterial orviral infections, kidney diseases, platelet aggregation, cancer,transplantation, graftrejection or lung injuries.
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