发明名称 Phenyl-tetrahydroisoquinoline derivatives
摘要 The invention provides novel compounds having the general formula (I); wherein R1, R2, R3, R4, R5, R6, R7, R8, R9, R10, R11, R12, A and n are as described herein, compositions including the compounds and methods of using the compounds.
申请公布号 US9187429(B2) 申请公布日期 2015.11.17
申请号 US201313864889 申请日期 2013.04.17
申请人 HOFFMANN-LA ROCHE INC. 发明人 Aebi Johannes;Amrein Kurt;Hornsperger Benoit;Kuhn Bernd;Liu Yongfu;Maerki Hans P.;Martin Rainer E.;Mayweg Alexander V.;Mohr Peter;Tan Xuefei
分类号 C07D217/22;C07D217/24;A61K31/47;C07D217/14;C07D221/04;C07D405/12;C07D221/16 主分类号 C07D217/22
代理机构 代理人 Hall Robert C.
主权项 1. A compound of formula (I) wherein R1, R2, R3 and R4 are independently selected from H, halogen, cyano, nitro, alkoxycarbonyl, cycloalkoxycarbonyl, substituted aminocarbonyl, substituted aminosulfonyl, alkyl, haloalkyl, cycloalkyl, alkoxy, haloalkoxy and cycloalkoxy, wherein substituted aminocarbonyl and substituted aminosulfonyl are substituted on the nitrogen atom with one to two substituents independently selected from H, alkyl, cycloalkyl, hydroxyalkyl and alkoxyalkyl; R5 is H, halogen, alkyl or cycloalkyl; R6 is H, alkyl, haloalkyl, cycloalkyl, substituted aryl or substituted heteroaryl, wherein substituted aryl or substituted heteroaryl are substituted with R19, R20 and R21; R7, R8, R9, R10, R11 and R12 are independently selected from H, halogen, alkyl and haloalkyl; A is —(CR13R14)p—NR15R16 or —(CR13R14)p—OR16; R13 and R14 are independently selected from H, alkyl, haloalkyl, cycloalkyl and halocycloalkyl; R15 is H, alkyl, haloalkyl, cycloalkyl, hydroxyalkyl, alkoxyalkyl or haloalkoxyalkyl; R16 is H, alkyl, haloalkyl, cycloalkyl, hydroxyalkyl, alkoxyalkyl, haloalkoxyalkyl, oxetanylalkyl, —CH2—C(O)OH, —CH2—C(O)OR17, —CH2—C(O)—NR17R18, —S(O)R17, —S(O)2R17, —S(O)2OR17, —S(O)2NR17R18, —C(O)R17, —C(O)OR17 or —C(O)NR17R18; R17 is alkyl, hydroxyalkyl, haloalkyl, cycloalkyl, alkylcycloalkyl, alkylcycloalkylalkyl, cycloalkylalkyl, cycloalkoxyalkyl, cycloalkylalkoxyalkyl, alkoxyalkyl, haloalkoxyalkyl, alkoxyalkoxyalkyl or substituted heteroaryl, wherein substituted heteroaryl is substituted with R22, R23 and R24; R18 is H, alkyl, haloalkyl, cycloalkyl, alkoxyalkyl, haloalkoxyalkyl or hydroxyalkyl; R19, R20, R21, R22, R23 and R24 are independently selected from H, halogen, alkyl, haloalkyl, cycloalkyl, alkoxy and haloalkoxy; n is zero, 1 or 2; p is zero or 1; or a pharmaceutically acceptable salt or ester thereof.
地址 Nutley NJ US