KUANG, RONGZE,BLYTHIN, DAVID,SHIH, NENG-YANG,SHUE, HO-JANE,CHEN, XIAO,CAO, JIANHUA,GU, DANLIN,HUANG, YING,SCHWERDT, JOHN H.,TING, PAULINE C.,WONG, SHING-CHUN,XIAO, LI
申请号：
CA2565599
公开号：
CA2565599C
申请日:
2005.05.16
申请国别(地区):
CA
年份:
2012
代理人:
摘要：
The invention claims compounds of the: (formula I)； wherein: (formula II) is a5-membered heteroaryl； X is S or O； R1 is H, alkyl, cycloalkyl,cylcoalkylalkyl-, -CH2F, -CHF2, -CF3, -C(O)alkyl or -C(O)NR18R19； R3 and R4 H,alkyl, hydroxyalkyl or -C(O)Oalkyl； R5 and R6 are H, alkyl, hydroxyalkyl,alkoxyalkyl, mercaptoalkyl, -CH2F, -CHF2, -CF3, -C(O)OH or -C(O)Oalkyl； R7 isH, alkyl, alkenyl, hydroxyalkyl, cycloalkyl, alkoxyalkyl, aminoalkyl, (R17-phenyl)alkyl or -CH2-C(O)-O-alkyl； and R8 comprises alkyl, heteroaryl, phenylor cycloalkyl, or heterocycloalkyl, all optionally substituted, or acycloalkyl- or heterocycloalkyl-substituted amide； or R7 and R8 and thenitrogen to which they are attached together form an optionally substitutedring； and the remaining variables are as defined in the specification. Alsoclaimed are pharmaceutical compositions, the use of the compounds as PDE4inhibitors, and combinations with other actives.
