发明名称 RORgammaT inhibitors
摘要 The present invention relates to compounds according to Formula I; or a pharmaceutically acceptable salt or solvate thereof. Such compounds can be used in the treatment of RORgammaT-mediated diseases or conditions.
申请公布号 US9603838(B2) 申请公布日期 2017.03.28
申请号 US201514752195 申请日期 2015.06.26
申请人 Merck Sharp & Dohme Corp.;Merck Sharp & Dohme B.V. 发明人 Karstens Willem Frederik Johan;Van Der Stelt Mario;Cals Jos;Azevedo Rita Corte Real Goncalves;Barr Kenneth Jay;Zhang Hongjun;Beresis Richard Thomas;Zhang Dongshan;Duan Xiaobang
分类号 C07D209/04;C07D231/56;A61K31/416;C07D401/06;C07D401/12;C07D403/10;C07D409/14;C07D413/12;C07D413/14;C07D471/04;A61K31/4245;A61K31/437;A61K31/4439;A61K31/4709;A61K45/06;A61K31/422 主分类号 C07D209/04
代理机构 Goodwin Procter LLP 代理人 Goodwin Procter LLP
主权项 1. A compound according to Formula I or a pharmaceutically acceptable salt or solvate thereof, wherein X is C(O), Y is N; n=0, 1, 2, 3 or 4; A4 is CR4, A5 is CR5, A6 is CR6, and A7 is CR7; R1 is (i) (C3-7)cycloalkyl or (C3-5)heterocycloalkyl, both optionally substituted with one or more groups selected from halogen, amino, cyano, nitro, hydroxy, H2NC(O)—, (C1-3)alkoxycarbonyl, (di)(C1-6)alkylaminocarbonyl, (C1-4)alkyl or (C1-3)alkoxy, wherein (C1-3)alkoxycarbonyl, (di)(C1-6)alkylaminocarbonyl, (C1-4)alkyl and (C1-3)alkoxy are optionally substituted with one or more halogens; (ii) (C2-9)heteroaryl, optionally substituted with one or more groups selected from halogen, amino, cyano, nitro, hydroxy, H2NC(O)—, (C1-3)alkoxycarbonyl, (di)(C1-6)alkylaminocarbonyl, (C1-4)alkyl or (C1-3)alkoxy, wherein (C1-3)alkoxycarbonyl, (di)(C1-6)alkylaminocarbonyl, (C1-4)alkyl and (C1-3)alkoxy are optionally substituted with one or more halogens; or (iii) (C6-14)aryl, optionally substituted with one or more groups selected from halogen, amino, cyano, nitro, hydroxy, H2NC(O)—, (C1-3)alkoxycarbonyl, (di)(C1-6)alkylaminocarbonyl, (C1-4)alkyl or (C1-3)alkoxy, wherein (C1-3)alkoxycarbonyl, (di)(C1-6)alkylaminocarbonyl, (C1-4)alkyl or (C1-3)alkoxy are optionally substituted with one or more halogens; R2 is C(O)OH, 5-tetrazoylyl, HOC(CF3)2, C(O)O(C1-10)alkyl, (C1-10)alkylsulfoxyaminocarbonyl; or carbamoyl; R3 is hydrogen, halogen, cyano, nitro, hydroxy, (C1-3)alkylC(O)O—, (C1-4)alkyl, or (C1-4)alkoxy, wherein (C1-4)alkyl and (C1-4)alkoxy are optionally substituted with one or more halogen; R4-R7 independently are H, halogen, amino, cyano, hydroxy, (C1-3)alkoxy, (C1-4)alkyl, (C0-10)alkyl)aminocarbonyl, (di)(C1-6)alkylaminocarbonyl or amino(C1-4)alkyl, wherein (C1-3)alkoxy, (C1-4)alkyl, (C0-10)alkyl)aminocarbonyl, (di)(C1-6)alkylaminocarbonyl and amino(C1-4)alkyl are optionally substituted with one or more halogen, hydroxyl or (C1-3)alkoxy; or a group having the formulaoptionally substituted with one or more of the following: (C1-10)alkyl, halogen, amino, cyano, hydroxy, or (C1-3)alkoxy, and wherein m is 1, 2, 3, or 4.
地址 Rahway NJ US