发明名称 PYRROLOTRIAZINE KINASE INHIBITORS
摘要 The present disclosure is generally directed to compounds which can inhibit AAK1 (adaptor associated kinase 1), compositions comprising such compounds, and methods for inhibiting AAK1.
申请公布号 US2016243125(A1) 申请公布日期 2016.08.25
申请号 US201415027585 申请日期 2014.10.08
申请人 BRISTOL-MYERS SQUIBB COMPANY 发明人 Dzierba Carolyn Diane;Dasgupta Bireshwar;Macor John E.;Bronson Joanne J.;Rajamani Ramkumar;Karageorge George N.
分类号 A61K31/53;A61K31/5377 主分类号 A61K31/53
代理机构 代理人
主权项 1. A method for treating or managing a disease or a disorder mediated by AAK1 activity, the method comprising administering to a patient in need thereof a therapeutically effective amount of a compound of formula (I)or a pharmaceutically acceptable salt thereof, wherein: n is 0, 1, or 2; R1 is selected from hydrogen, C1-C3alkyl, —CH2NRaRb, —C(O)NRaRb, —CH2OR6, and —CO2R6; R2 is selected from hydrogen and —CO2R6; R3 is selected from hydrogen and Br; when n is 1, R4 is selected from halo, haloalkyl, hydroxyC1-C3alkyl, —OR6; or, when n is 2, the two R4 groups are on adjacent carbon atoms, and together with the atoms to which they are attached, form a five-membered ring selected fromwherein “” indicates the point of attachment to the six-membered aromatic ring; R5 is selected from C2alkenyl, —NHC(O)R7, —C(O)NHR7, each R6 is independently hydrogen or C1-C6 alkyl; R7 is selected from C1-C6alkyl, and aminoC1-C6alkyl; R8 is selected from aminoC1-C6alkyl, C1-C6alkyl, C3-C6cycloalkyl, haloC1-C6alkyl, hydroxyC1-C6alkyl, and phenyl; and Ra and Rb are independently selected from hydrogen, C1-C3alkoxyC1-C3alkyl, C1-C3alkyl, aminoC2-C6alkyl, cyanoC1-C3alkyl, C3-C6cycloalkylC1-C3alkyl,or Ra and Rb, together with the nitrogen atom to which they are attached, form a ring selected from azetidinyl, morpholinyl, piperazinyl, piperidinyl, pyrrolidinyl,wherein the ring is optionally substituted with one or two substituents independently selected from C1-C3acylamino, C1-C3alkyl, amino, aminoC1-C3alkyl, hydroxy, and methylamino.
地址 Princeton NJ US