发明名称 ARYLPYRIDINONE ITK INHIBITORS FOR TREATING INFLAMMATION AND CANCER
摘要 Disclosed herein are arylpyridinone compounds and compositions useful in the treatment of ITK mediated diseases, such as inflammation, having the structure of Formula (I):;wherein Ar, R2, R4, R5, n and X are as defined in the detailed description. Methods of inhibition of ITK activity in a human or animal subject are also provided.
申请公布号 US2015210671(A1) 申请公布日期 2015.07.30
申请号 US201514603937 申请日期 2015.01.23
申请人 Confluence Life Sciences, Inc. 发明人 Jacobsen Eric Jon;Blinn James Robert
分类号 C07D401/14;A61K31/444;A61K31/497;A61K45/06;C07D405/14;A61K31/5377;C07D401/12;A61K31/4427;A61K31/4545;A61K31/506 主分类号 C07D401/14
代理机构 代理人
主权项 1. A compound, or a pharmaceutically acceptable salt, hydrate or solvate thereof, of Formula (I): wherein: Ar is chosen from aryl and heteroaryl, wherein Ar may be optionally substituted with one or more R6 substituents; R2 is chosen from hydrogen, halo and C1-4 alkyl; R3 is chosen from hydrogen, halo and C1-4 alkyl; R4 is chosen from cyano, C(O)CH2R2, C(O)CF3, C(O)CH═CH2, C(O)CR7═CH2, C(O)CH═CHR7, C(O)CR7═CHR7, C(O)CH═CR7R7, C(O)CH═CHCH2R8, C(O)CH═CHC(O)CH2R8, C(O)C(CN)═CH2, C(O)(C(O)NH2)C═CH2, S(O)2CH═CH2, (CH2)mCR7═CR9C(O)Me, (CH2)mCR7═CR9C(O)NH2, (CH2)mCR7═CR9C(O)NHR7, (CH2)mCR7═CR9C(O)N(R7)2, and (CH2)mCR7═CR9CN; R5 is chosen from hydrogen, —(CH2)nC3-7 cycloalkyl, and C1-4 alkyl; each R6 is independently chosen from hydrogen, C1-4 alkyl, —(CH2)nC3-7 cycloalkyl, OC1-4 alkyl, C1-4 alkylamino, NH2, NHC1-4 alkyl, N(C1-4 alkyl)2, cyano, C(O)NH2, C(O)NHR5, C(O)N(R5)2, C(O)C1-4 alkyl, trifluoromethyl, halo, —(CH2)nC3-7 cycloalkyl, C(O)NHaryl, and C(O)NHheteroaryl, wherein aryl and heteroaryl may be optionally substituted with one or more R9; each R7 is independently chosen from hydrogen, CN, C1-4 alkyl, C3-7 cycloalkyl, C3-7 heterocycle, aryl, and heteroaryl wherein aryl and heteroaryl may be optionally substituted with one or more R9; R8 is chosen from hydrogen, C1-4 alkyl, C1-4alkylaryl, C1-4alkyl-O-aryl, C1-4 alkylheteroarylaryl, C3-7 cycloalkyl, C3-7 heterocycle, OH, OC1-4 alkyl, C1-4 alkylOC1-4 alkyl, NH2, NHC1-4 alkyl, N(C1-4 alkyl)2, heterocycle, aryl and heteroaryl, wherein each aryl and heteroaryl may be optionally substituted with one or more R9; R9 is chosen from hydrogen, C1-4 alkyl, CN, CF3, C(O)Me, C(O)NH2, and aryl; X is chosen from N and CR3; m is chosen from 1, 2 and 3; and n is chosen from 0, 1, 2, and 3.
地址 St. Louis MO US