发明名称 Novel Alkene Oxindole Derivatives
摘要 The present invention provides compounds of formula (I),;;as well as pharmaceutically acceptable salt thereof, wherein R1 to R7 have the significance given herein. The compounds are useful in the treatment of prophylaxis of diseases that are related to AMPK regulation.
申请公布号 US2014288127(A1) 申请公布日期 2014.09.25
申请号 US201414294213 申请日期 2014.06.03
申请人 Hoffmann-La Roche Inc. 发明人 Chen Li;Feng Lichun;Huang Mengwei;Li Jia;Nan Fajun;Pang Tao;Yu Lifang;Zhang Mei
分类号 C07D417/06;C07D409/06;C07D401/06;C07D209/34 主分类号 C07D417/06
代理机构 代理人
主权项 1. A method of treatment or prophylaxis of a disease or disorder related to AMPK regulation, said method comprising administering to a patient in need thereof an effective amount of a compound of formula (I), wherein R1 is selected from the group consisting of: hydrogen, halogen, alkoxy, cyano, haloalkyl, alkylsulfanyl, aminosulfonyl, alkylsulfonyl, haloalkoxy and alkylcarbonyl; R2 is selected from the group consisting of: hydrogen, halogen, alkoxy, cyano, haloalkyl, alkylsulfanyl, aminosulfonyl, alkylsulfonyl, haloalkoxy and alkylcarbonyl; R3 is selected from the group consisting of: hydrogen, halogen, alkoxy, cyano, haloalkyl, alkylsulfanyl, aminosulfonyl, alkylsulfonyl, haloalkoxy and alkylcarbonyl; R4 is selected from the group consisting of: hydrogen, halogen, alkoxy, cyano, haloalkyl, alkylsulfanyl, aminosulfonyl, alkylsulfonyl, haloalkoxy and alkylcarbonyl; R5 is selected from the group consisting of: alkyl, hydroxyalkyl, cycloalkyl, phenylalkyl, halophenylalkyl, phenyl, substituted phenyl, thiophenyl and pyridinyl, wherein said substituted phenyl is phenyl substituted with one to three substituents independently selected from the group consisting of alkyl, alkoxy, halogen, cyano, haloalkyl, alkylsulfanyl, aminosulfonyl, alkylsulfonyl, haloalkoxy and alkylcarbonyl; R6 is selected from the group consisting of: alkyl, hydroxyalkyl, cycloalkyl, phenylalkyl, halophenylalkyl, phenyl, substituted phenyl, thiophenyl and pyridinyl, wherein said substituted phenyl is phenyl substituted with one to three substituents independently selected from the group consisting of alkyl, alkoxy, halogen, cyano, haloalkyl, alkylsulfanyl, aminosulfonyl, alkylsulfonyl, haloalkoxy and alkylcarbonyl; R7 is selected from the group consisting of: substituted phenyl, pyridinyl, substituted pyridinyl, thiazolyl, substituted thiazolyl and carboxy, wherein said substituted phenyl is phenyl substituted with one to three substituents independently selected from the group consisting of alkyl, hydroxy, alkoxy, carboxy, alkoxycarbonylalkyl, alkylaminocarbonyl, carboxyalkoxy, alkoxycarbonyl, alkoxycarbonylalkoxy and alkylsulfonylaminocarbonyl, and said substituted pyridinyl and said substituted thiazolyl are, respectively, pyridinyl and thiazolyl substituted with alkoxycarbonyl or carboxy; and n is 0 or 1; or a pharmaceutically acceptable salt or ester thereof; with the provisos that: R5 and R6 are not both methoxyphenyl at the same time; and when one of R5 and R6 is phenyl and the other one is phenyl, methylphenyl or alkoxyphenyl, R7 is alkoxycarbonylphenyl.
地址 Nutley NJ US