发明名称 Complement pathway modulators and uses thereof
摘要 The present invention provides a compound of formula I:; a method for manufacturing the compounds of the invention, and its therapeutic uses. The present invention further provides a combination of pharmacologically active agents and a pharmaceutical composition.
申请公布号 US9056874(B2) 申请公布日期 2015.06.16
申请号 US201313826725 申请日期 2013.03.14
申请人 NOVARTIS AG 发明人 Adams Christopher Michael;Babu Charles;Capparelli Michael Paul;Ding Jian;Ehara Takeru;Jendza Keith;Ji Nan;Karki Rajeshri Ganesh;Kawanami Toshio;Xue Liang;Mainolfi Nello;Powers James J.;Serrano-Wu Michael H.;Zhang Chun
分类号 C07D403/06;C07D403/04;C07D403/08;C07D403/14;C07D401/14;C07D413/14;C07D487/04;C07D491/048;A61K31/4184;C07D413/06;A61K31/423;A61K31/4439;A61K45/06 主分类号 C07D403/06
代理机构 代理人 Alexander John B.
主权项 1. A compound, or salt or a tautomer thereof, according to Formula (I): Wherein is a single or double bond; X is N; Y is N(H); one occurrence of R is cyano and the other occurrence of R is hydrogen or R4; R1 is halogen, hydroxyl, C1-C6alkyl, C2-C6alkenyl, C3-C6cycloalkyl, C1-C6alkoxy, haloC1-C6alkyl, hydroxyC1-C6alkyl, aminoC1-C6alkyl, C1-C6alkoxyC1-C6alkyl, C1-C6alkoxyC1-C6alkoxy, C3-C6cycloalkylC1-C6alkoxy, haloC1-C6alkoxy, S(O)pC1-C6alkyl, CH2NHC(O)C1-C4alkyl or OCH2C(O)R7; p is 0, 1, or 2; R2 is C1-C6alkyl, C1-C6alkoxy, hydroxyC1-C6alkyl or halogen; R3 is hydrogen, halogen, cyano, C1-C4alkyl, haloC1-C4alkyl, CH2C(O)R7, phenyl or 5 or 6 member heteroaryl having 1, 2 or 3 ring heteroatoms independently selected from N, O or S, wherein the phenyl or heteroaryl is optionally substituted with 0, 1, or 2 C1-C4alkyl groups, and wherein the alkyl and haloalkyl is optionally substituted with 0 or 1 hydroxy groups; R4 is 0, 1, or 2 substitutents independently selected at each occurrence from halogen and C1-C6alkyl; R5 is hydrogen, C1-C6alkyl, haloC1-C6alkyl, C3-C6cycloalkyl, phenyl or 5 or 6 member heteroaryl having 1, 2 or 3 ring heteroatoms independently selected from N, O or S; or R3 and R5 taken in combination form a divalent —CH2—CH2— or —CH2—N(H)— group; R6 is hydrogen, hydroxy, amino, C1-C6alkyl, C1-C6alkoxy, C1-C6alkoxyC1-C6alkoxy, mono- and di-C1-C4alkylamino, amino C1-C6alkylamino, [CRA2]nR7, [CRA2]nC(O)R7, O[CRA2]nR7, NHC(O)C1-C6alkyl, NHS(O2)C1-C6alkyl, (CH2)nR9, O(CH2)nR9, C(O)R7, N(H)[CRA2]nR7, O[CRA2]nC(O)R7, N(H)[CRA2]nC(O)R7 or tetrazolyl; or CR5R6, taken in combination, form a divalent carbonyl group, a divalent ═CH2 group or cyclopropyl which cyclopropyl is optionally substituted by CO2H or CH2OH; n is 1, 2, 3 or 4; RA is independently selected at each occurrence from hydrogen, halogen or C1-C4alkyl; R7 is hydroxy, C1-C4alkoxy, amino or mono- and di-C1-C4alkylamino; R8 is hydrogen or halogen; and R9 is a 5 member heteroaryl having 1 to 4 ring heteroatoms selected from N, O or S and optionally substituted with 0, 1, or 2 C1-C4alkyl groups.
地址 Basel CH