发明名称 Non-annulated thiophenylamides
摘要 The invention provides novel compounds having the general formula (I); wherein R1, R2, R3, R4, R5, R6, R7, A, E and n are as described herein, compositions including the compounds and methods of using the compounds.
申请公布号 US9353102(B2) 申请公布日期 2016.05.31
申请号 US201514645012 申请日期 2015.03.11
申请人 Hoffmann-La Roche Inc. 发明人 Buettelmann Bernd;Ceccarelli Simona M.;Kuehne Holger;Kuhn Bernd;Neidhart Werner;Obst Sander Ulrike;Richter Hans
分类号 C07D417/04;C07D417/14;C07D413/04;C07D413/14;C07D333/36 主分类号 C07D417/04
代理机构 代理人
主权项 1. A compound of formula (I) wherein R1 and R2 are independently selected from H, alkyl, haloalkyl, alkoxyalkyl, haloalkoxyalkyl, cycloalkyl, cycloalkylalkyl, halocycloalkyl, halocycloalkylalkyl, substituted aryl, substituted arylalkyl, substituted heterocycloalkyl, substituted heterocycloalkylalkyl, substituted heteroaryl, substituted heteroarylalkyl, substituted aminocarbonyl, alkoxycarbonyl, haloalkoxycarbonyl and carboxy, wherein substituted aryl, substituted arylalkyl, substituted heterocycloalkyl, substituted heterocycloalkylalkyl, substituted heteroaryl and substituted heteroarylalkyl are substituted with R14, R15 and R16, and wherein substituted aminocarbonyl is substituted on the nitrogen atom with one to two substituents independently selected from H, alkyl, cycloalkyl, haloalkyl, alkylcycloalkyl, cycloalkylalkyl, alkylcycloalkylalkyl, hydroxyalkyl and alkoxyalkyl; R3 is pyrrolidinyl, substituted [1,2,4]-oxadiazolyl, oxazolyl, substituted thiazolyl, substituted [1,2,4]thiadiazol-5-yl, or pyrimidinyl, wherein substituted [1,2,4]-oxadiazolyl, substituted [1,2,4]thiadiazol-5-yl and substituted thiazolyl are substituted with R17 R4 is H or alkyl; R5 and R6 are independently selected from H, alkyl and cycloalkyl; R7 is H, alkyl or cycloalkyl; A is NR8 or CR9R10; E is NR11 or CR12R13; R8 and R11 are independently selected from H, alkyl, haloalkyl, cycloalkyl, halocycloalkyl, cycloalkylalkyl or halocycloalkylalkyl; R9, R10, R12 and R13 are independently selected from H, halogen, alkyl, haloalkyl or cycloalkyl; or R5 and R12 together with the carbon atoms to which they are attached form a substituted cycloalkyl, substituted cycloalkenyl, substituted aryl, substituted heterocycloalkyl or substituted heteroaryl, wherein substituted cycloalkyl, substituted cycloalkenyl, substituted aryl, substituted heterocycloalkyl and substituted heteroaryl are substituted with R20 and can be further substituted with R21 and/or R22, wherein in case R5 and R12 together with the carbon atoms to which they are attached form a substituted aryl or substituted heteroaryl, then R6 and R13 are absent; or R8 and R12 together with the nitrogen and carbon atoms to which they are attached form a substituted heterocycloalkyl or substituted heteroaryl, wherein substituted heterocycloalkyl and substituted heteroaryl are substituted with R20 and can be further substituted with R21 and/or R22, wherein in case R8 and R12 together with the carbon atoms to which they are attached form a substituted heteroaryl, then R13 is absent; or R9 and R11 together with the nitrogen and carbon atoms to which they are attached form a substituted heterocycloalkyl or substituted heteroaryl, wherein substituted heterocycloalkyl and substituted heteroaryl are substituted with R20 and can be further substituted with R21 and/or R22, wherein in case R9 and R11 together with the carbon atoms to which they are attached form a substituted heteroaryl, then R10 is absent; or R9 and R12 together with the carbon atoms to which they are attached form a substituted cycloalkyl, substituted cycloalkenyl, substituted aryl, substituted heterocycloalkyl or substituted heteroaryl, wherein substituted cycloalkyl, substituted cycloalkenyl, substituted aryl, substituted heterocycloalkyl and substituted heteroaryl are substituted with R20 and can be further substituted with R21 and/or R22, wherein in case R9 and R12 together with the carbon atoms to which they are attached form a substituted aryl or substituted heteroaryl, then R10 and R13 are absent; or R10 and R13 together with the carbon atoms to which they are attached form a substituted cycloalkyl, substituted cycloalkenyl, substituted aryl, substituted heterocycloalkyl or substituted heteroaryl, wherein substituted cycloalkyl, substituted cycloalkenyl, substituted aryl, substituted heterocycloalkyl and substituted heteroaryl are substituted with R23 and can be further substituted with R24 and/or R25, wherein in case R10 and R13 together with the carbon atoms to which they are attached form a substituted aryl or substituted heteroaryl, then R9 and R12 are absent; or R10 and R13 together with the carbon atoms to which they are attached form a double bond; R14, R15, R16, R17, R20, R21, R23, R24 and R25 are independently selected from H, hydroxy, oxo, halogen, alkyl, haloalkyl, cycloalkyl, halocycloalkyl, alkoxy, haloalkoxy, alkoxyalkyl, haloalkoxyalkyl, alkoxycarbonyl, carboxy and amino substituted on the nitrogen atom with one to two substituents independently selected from H alkyl, cycloalkyl, haloalkyl, alkylcycloalkyl, cycloalkylalkyl, alkylcycloalkylalkyl, hydroxyalkyl and alkoxyalkyl; n is zero or 1; or a pharmaceutically acceptable salt thereof.
地址 Little Falls NJ US