发明名称 Apoptosis-inducing agents for the treatment of cancer and immune and autoimmune diseases
摘要 Disclosed are compounds which inhibit the activity of anti-apoptotic Bcl-2 proteins, compositions containing the compounds and methods of treating diseases during which is expressed anti-apoptotic Bcl-2 protein.
申请公布号 US9156856(B2) 申请公布日期 2015.10.13
申请号 US201213682603 申请日期 2012.11.20
申请人 AbbVie Inc. 发明人 Kunzer Aaron R.;Elmore Steven W.;Hexamer Laura A.;Park Cheol-Min;Souers Andrew J.;Sullivan Gerard M;Wang Gary T.;Wang Xilu;Wendt Michael D.
分类号 C07C311/00;C07D513/04;C07C311/51;C07D207/36;C07D211/96;C07D231/18;C07D261/10;C07D275/03;C07D277/36;C07D277/60;C07D285/125;C07D285/135;C07D295/155;C07D295/26;C07D333/34;C07D333/36;C07D333/62;C07D409/12;C07D413/04;C07D413/06;C07D417/14;C07D487/04;C07D333/42 主分类号 C07C311/00
代理机构 Jones Day 代理人 Jones Day
主权项 1. A compound having Formula Ior a therapeutically acceptable salt thereof, wherein A1 is furyl, imidazolyl, isothiazolyl, isoxazolyl, pyrazolyl, pyrrolyl, thiadiazolyl, thienyl, triazolyl, piperidinyl, morpholinyl, dihydro-1,3,4-thiadiazol-2-yl, benzothien-2-yl, benzothiazol-2-yl, [1,2,4]triazolo[1,5-a]pyrimidin-2-yl, tetrahydrothien-3-yl or imidazo[2,1-b][1,3]thiazol-5-yl; wherein A1 is unsubstituted or substituted with one or two or three or four or five substituents independently selected from the group consisting of R1, OR1, C(O)OR1, NHR1, N(R1)2, C(N)C(O)R1, C(O)NHR1, NHC(O)R1, NR1C(O)R1, (O), NO2, F, Cl, Br, I, and CF3; R1 is R2, R3, R4 or R5; R2 is phenyl; R3 is heteroaryl; R4 is heterocycloalkyl; R5 is alkyl or alkenyl, each of which is unsubstituted or substituted with a substituent selected from the group consisting of R7, SR7, N(R7)2, NHC(O)R7, F, Cl, Br and I; R7 is R8, R9, R10 or R11; R8 is phenyl; R9 is heteroaryl; R10 is heterocycloalkyl; R11 is alkyl; Z1 is phenylene; Z2 is heterocycloalkylene; Z1A and Z2A are both absent; L1 is alkylene or alkenylene, each of which is unsubstituted or substituted with phenyl; Z3 is R38 or R40; R38 is phenyl; R40 is cycloalkyl, cycloalkenyl; wherein the phenylene represented by Z1 is unsubstituted or substituted with OR41; R41 is R42 or R43; R42 is phenyl, which is unfused or fused with heteroarene; R43 is heteroaryl, which is unfused or fused with heteroarene; wherein each cyclic moiety represented by R2, R3, R4, R8, R9, R10, Z2, R38, R40, R42 and R43 is independently unsubstituted, or substituted with one or more substituents independently selected from the group consisting of R57, OR57, C(O)OR57, F, Cl, Br and I; R57 is R58, or R61; R58 is phenyl; R61 is alkyl; and wherein the phenyl represented by R58 is unsubstituted or substituted with one or more substituents independently selected from the group consisting of F, Cl, B and I.
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