发明名称 Heteroaryl substituted indole compounds useful as MMP-13 inhibitors
摘要 Disclosed are compounds and compositions of the formula I as described herein which are inhibitors of MMP-13. Also disclosed are methods of using and making compounds of the formula I.;
申请公布号 US8785489(B2) 申请公布日期 2014.07.22
申请号 US200913123048 申请日期 2009.10.13
申请人 Boehringer Ingelheim International GmbH 发明人 Abeywardane Asitha;Farmer Bennett;Farrow Neil Alexander;Gao Donghong Amy;Heim-Riether Alexander;Smith Keenan Lana Louise;Mugge Ingo Andreas;Taylor Steven John;Xiong Zhaoming;Yu Yang;Zhang Qiang
分类号 A61K31/5377;A61K31/506;A61K31/497;A61K31/454;A61K31/444;A61K31/4439;A61K31/427;A61K31/422;A61K31/4178;A61K31/4155;A61K31/404;C07D413/14;C07D413/04;C07D409/14;C07D409/04;C07D405/14;C07D405/04;C07D403/14;C07D403/04;C07D401/14;C07D401/04;C07D487/04;C07D405/12;C07D417/14;C07D471/04;C07D209/42 主分类号 A61K31/5377
代理机构 代理人 Morris Michael P.;Bottino Anthony P.
主权项 1. A compound of the formula (I): Het is a ring chosen from phenyl, oxazolyl, isoxazolyl, oxadiazolyl, thiazolyl, isothiazolyl, pyrazolyl, pyrrolyl, imidazolyl, pyridinyl, pyrimidinyl and pyridazinyl each optionally substituted by one to three C1-5 alkyl, C1-5 alkoxy, C1-5 acyl, C1-5 acylamino, amino, cyano, hydroxyl or halogen; X is —N(R3)—; Y is N or CH; Z is H or F; R1 is chosen from C1-5 alkoxyC1-5 alkyl, C1-5 alkoxycarbonyl-(CH2)n—, —C(O)NR4R5 and Ar1; R2 is chosen from Ar2—(CH2)n—, heterocycle and C1-5 alkyl; R3 is chosen from hydrogen and C1-5 alkyl; each R4 and R5 is independently chosen from hydrogen, C1-5 acyl, C1-5 alkyl, C1-5 alkoxy, hydroxyl, carbocycle-(CH2)n—, heteroaryl and heterocycle-(CH2)n—; Ar1 is chosen from carbocycle, heteroaryl and heterocycle wherein Ar1 is optionally substituted by one to three C1-5 alkyl, C1-5 alkoxy, C1-5 acyl, C1-5 acylamino, amino, cyano, hydroxyl or halogen; Ar2 is chosen from carbocycle, heteroaryl and heterocycle wherein Ar2 is optionally substituted by one to three heteroaryl, C1-5 alkyl, C1-5 alkoxy-(CH2)n—, C1-5 alkoxycarbonyl-(CH2)n—, carboxy-(CH2)n—, C1-5 acyl, C1-5 acylamino, amino, cyano, hydroxyl, sulfonyl, sulfoxide, thio, oxo or halogen; each n is independently 0-2; or a pharmaceutically acceptable salt thereof.
地址 Ingelheim am Rhein DE