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 US9085555(B2) 申请公布日期 2015.07.21
申请号 US201213342161 申请日期 2012.01.02
申请人 NOVARTIS AG 发明人 Altmann Eva;Hommel Ulrich;Lorthiois Edwige Liliane Jeanne;Maibaum Juergen Klaus;Ostermann Nils;Quancard Jean;Randl Stefan Andreas;Rogel Olivier;Simic Oliver;Vulpetti Anna
分类号 C07D471/04;C07D487/04;A61K31/437;A61K31/404;C07D403/12;C07D401/14;C07D403/14;C07D405/14;C07D409/14;C07D417/12;C07D417/14 主分类号 C07D471/04
代理机构 代理人 Alexander John B.
主权项 1. A compound or salt thereof represented by one of the formulae (IIIb) or (IVb):wherein Z2 is CH or N; Z5 is CR5 or N; Z6 is CR6 or N; or an N-oxide thereof Z7 is CH, C(CH3) or N, wherein 0 or 1 or 2 of Z5, Z6 and Z7 is N; R3 is hydrogen, methyl, ethyl, iPr, amino, hydroxymethyl, CH2OMe, or mono-, di- and tri-fluoromethyl, NHMe; R5 is hydrogen, halogen, C1-C4alkyl, C1-C4alkoxy, C2-C4alkenyl, C2-C4alkenyloxy, hydroxy, CO2H, tetrazole, C1-C4alkoxycarbonyl, cyano, wherein each alkyl or alkoxy group is unsubstituted or substituted with up to 5 halogen atoms and with 0 or 1 additional substituents selected from the group consisting of hydroxy, cyano, tetrazole, C1-C4alkoxy, CO2H, C1-C4alkoxycarbonyl, tetrahydrofuranyl, optionally substituted phenyl, pyridyl and pyrimidinyl, and wherein the phenyl is unsubstituted or substituted with 1 or 2 substituents independently selected from halogen, hydroxy, methyl, methoxy and CO2H; R6 is hydrogen, halogen, C1-C4alkyl, C1-C4alkoxy, C2-C4alkenyl, C2-C4alkenyloxy, hydroxy, CO2H, C1-C4alkoxycarbonyl, cyano, wherein each alkyl or alkoxy group is unsubstituted or substituted with up to 5 halogen atoms and with 0 or 1 additional substituents selected from the group consisting of hydroxy, NR10R11, tetrazole, cyano, imidazolyl, C1-C4alkoxy, CO2H, C1-C4alkoxycarbonyl, optionally substituted phenyl, pyrrolyl, morpholino, piperidino, piperazino, and pyridyl, and wherein the phenyl is unsubstituted or substituted with 1 or 2 substituents independently selected from halogen, hydroxy, methyl, methoxy, mono- and dimethyl amino, and CO2H; L is CH2 or NH; R15 is hydrogen, fluoro, methyl, hydroxy, methoxy, ethoxy and OCH2CH2OMe, OCH2CH2N(CH3)2, amino or OCH2CH2pyrrolyl; R16 is hydrogen, fluoro, methyl, amino, hydroxymethyl, methoxymethyl, or aminomethyl; R17 is hydrogen, fluoro or methyl; R19 is hydrogen or R19 and R17, taken in combination, form a cyclopropyl ring; or R15 and R16, taken in combination, form a cyclopropyl ring; G is —C(O)N(H)—; and q is 0 or 1; R21 is hydrogen, methyl, or ethyl, which methyl and ethyl are unsubstituted or substituted with hydroxy, methoxy, cyano, amino, mono- or di-methyl amino, morpholinomethyl, optionally substituted azetidinomethyl, which azetidino ring is substituted with 0 or 1 fluoro or methoxy; or R22 is hydrogen; CR21R22, taken in combination, from a cyclopropane ring; Z is phenyl, pyridyl, pyrazinyl or thienyl, each of which is unsubstituted or substituted with 1, 2, or 3 residues independently selected at each occurrence from the group consisting of halogen, methyl, ethyl, isopropyl, cyclopropyl, methoxy, hydroxy, trifluoromethyl, di or trifluoromethoxy, SF5, CO2H, tetrazole, and NR23R24, unsubstituted or substituted phenyl and unsubstituted or substituted pyridinyl, which substituted phenyl and pyridinyl has 1 or 2 substituents independently selected from the group consisting of halogen and methyl.
地址 Basel CH
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