发明名称 Benzimidazole inhibitors of leukotriene production
摘要 The present invention relates to compounds of formula (IA), (IB) and (IC):; and pharmaceutically acceptable salts thereof, wherein R1-R7 are as defined herein. The invention also relates to pharmaceutical compositions comprising these compounds, methods of using these compounds in the treatment of various diseases and disorders, processes for preparing these compounds and intermediates useful in these processes.
申请公布号 US8772304(B2) 申请公布日期 2014.07.08
申请号 US201113281687 申请日期 2011.10.26
申请人 Boehringer Ingelheim International GmbH 发明人 De Lombaert Stephane;Liu Weimin;Lo Ho Yin;Nemoto Peter Allen
分类号 C07D401/14;A61K31/4184 主分类号 C07D401/14
代理机构 代理人 Morris Michael P.;Patel Usha R.
主权项 1. A compound of formula IA wherein: R1 is pyridinyl, pyrimidinyl, pyrazinyl, pyridazinyl, pyrrolopyridinyl, imidazopyridinyl, pyrazolopyridinyl or dihydropyrrolopyridinyl optionally substituted with oxo, wherein each heterocycle is optionally independently substituted with one to three groups selected from Ra, Rb and Rc; R2 is C1-C6 alkyl or C3-6 cycloalkyl optionally substituted with C1-3 alkyl; R3 is H, —OH, halogen, —CN, C1-6 alkoxy, —COOR8, —C(O)NR8R9 or 5-6 membered heteroaryl ring which is optionally substituted with C1-3 alkyl; R4, R5, and R6 are each independently selected from (a) —H,(b) —OH,(c) halogen,(d) —CN,(e) —CF3,(f) C1-6alkyl optionally substituted with one to three —OH, fluorine, C1-6alkoxyl —N(R8)(R9), or —C(O)N(R8)(R9),(g) C3-6cycloalkyl(h) C1-6alkoxy optionally substituted with one to three —OH, fluorine, —OC1-6alkyl, or —OC3-6cycloalkyl(i) —S(O)nC1-6alkyl,(j) —S(O)2aryl(k) —S(O)2heterocycle(l) —CO2R8,(m) —SCF3,(n′) a5-6 membered heterocyclic ring; R8 and R9 are each independently selected from —H, C1-6alkyl, and 5-6 membered heterocyclic ring; Ra is selected from H, —NH2, —NH(C1-C6)alkyl, —NR10R11, —NH—C(O)C1-C6alkyl, NR11—C(O)C1-C6alkyl, —O(C1-C8)alkyl, —O(C3-C6)cycloalkyl, —S—(C1-C6)alkyl, —S(O)—C1-C6alkyl, —S(O)2—C1-C6alkyl, and —CH2—OH; Rb is selected from —H, —(C1-C6)alkyl, —O—(C1-C6)alkyl, —NH2, —CH2—OH, —C≡N, —CH2NH2 and —C(O)OCH3; Rc is selected from —H, —CH3 and —OH; R10and R11 are each independently selected from —H, C1-6alkyl-5-6 membered heterocyclyl, C1-6alkyl-5-6 membered heteroaryl optionally substituted with halogen and C1-6alkyl-aryl; n is 0, 1 or 2; or a pharmaceutically acceptable salt thereof.
地址 Ingelheim am Rhein DE