MONTSE LLINAS-BRUNET,MURRAY D BAILEY,DALE CAMERON,ANNE-MARIE FAUCHER,ELISE GHIRO,NATHALIE GOUDREAU,TEDDY HALMOS,MARC-ANDRE POUPART,JEAN RANCOURT,YOULA S TSANTRIZOS,DOMINIK M WERNIC,BRUNO SIMONEAU
申请号：
EEP200100081
公开号：
EE05517B1
申请日:
1999.08.09
申请国别(地区):
EE
年份:
2012
代理人:
摘要：
Racemates, diastereoisomers and optical isomers of a compound of formula (I): wherein B is H, a C 6 or C 10 aryl, C 7-16 aralkyl； Het or (lower alkyl)-Het, all of which optionally substituted with C 1-6 alkyl； C 1-6 alkoxy； C 1-6 alkanoyl； hydroxy； hydroxyalkyl； halo； haloalkyl； nitro； cyano； cyanoalkyl； amino optionally substituted with C 1-6 alkyl； amido； or (lower alkyl)amide； or B is an acyl derivative of formula R 4 -C(O)-； a carboxyl of formula R 4 -O-C(O)-； an amide of formula R 4 -N( R 5 )-C(O)-； a thioamide of formula R 4 -N( R 5 )-C(S)-；or a sulfonyl of formula R 4 -SO 2 ； R 5 is H or C 1-6 alkyl； and Y is H or C 1-6 alkyl； R 3 is C 1-8 alkyl, C 3-7 cycloalkyl, or C 4-10 alkylcycloalkyl, all optionally substituted with hydroxy, C 1-6 alkoxy, C 1-6 thioalkyl, amido, (lower alkyl)amido, C 6 or C 10 aryl, or C 7-16 aralkyl； R 2 is CH 2 - R 20 , NH- R 20 , O- R 20 or S- R 20 , wherein R 20 is a saturated or unsaturated C 3-7 cycloalkyl or C 4-10 (alkylcycloalkyl), all of which being optionally mono-, di- or trisubstituted with R 21 , or R 20 is a C 6 or C 10 aryl or C 7-14 aralkyl optionally substituted, or R 20 is Het or (lower alkyl)-Het, both optionally substituted, Het or (lower alkyl)-Het； carboxyl； carboxy(lower alkyl)； C 6 or C 10 aryl, C 7-14 aralkyl or Het, said aryl, aralkyl or Het being optionally substituted； and R 1 is H； C 1-6 alkyl, C 3-7 cycloalkyl, C 2-6 alkenyl, or C 2-6 alkynyl, all optionally substituted with halogen； or a pharmaceutically acceptable salt or ester thereof.
