发明名称 Quinoline-4-carboxamide derivatives as NK-3 and NK-2 receptor antagonists
摘要 A compound, or a solvate or a salt thereof, of formula (I):wherein, Ar is an optionally substituted aryl or a C5-7 cycloalkdienyl group, or an optionally substituted C5-7 cycloalkyl group, or an optionally substituted single or fused ring aromatic heterocyclic group;R is hydrogen, linear or branched C1-6 alkyl, C3-7 cycloalkyl, C3-7 cycloalkylalkyl;R1 represents hydrogen or up to three optional substituents selected from the list consisting of: C1-6 alkyl, C1-6 alkenyl, aryl, C1-6 alkoxy, hydroxy, halogen, nitro, cyano, carboxy, carboxamido, sulphonamido, C1-6 alkoxycarbonyl, trifluoromethyl, acyloxy, amino or mono- and di-C1-6 alkylamino,R2 represents a moiety -(CH2)n-NYY2 wherein n is an integer in the range of from 1 to 9, Y1 and Y2 are independently selected from C1-6-alkyl; C1-6 alkyl substituted with hydroxy, alkoxy, C1-6 alkylamino or bis (C1-6 alkyl) amino; C3-6 cycloalkyl; C4-6 azacycloalkyl; C1-6-alkenyl; aryl or aryl-C1-6-alkyl or Y1 and Y2 together with the nitrogen atom to which they are attached represent an optionally substituted N-linked single or fused ring heterocyclic group;R3 is branched or linear C1-6 alkyl, C3-7 cycloalkyl, C4-7 cycloalkylalkyl, optionally substituted aryl, or an optionally substituted single or fused ring aromatic heterocyclic group; and R4 represents hydrogen or C1-6 alkyl, R5 represents hydrogen or halogen; a process for preparing such compounds, a pharmaceutical composition comprising such compounds and the use of such compounds and composition in medicine.
申请公布号 US6780875(B2) 申请公布日期 2004.08.24
申请号 US20030358938 申请日期 2003.02.05
申请人 SMITHKLINE BEECHAM S.P.A.;SMITHKLINE BEECHAM LABORATORIES PHARMACEUTIQUES 发明人 FARINA CARLO;GIARDINA GIUSEPPE;GRUGNI MARIO;MORVAN MARCEL;NADLER GUY MARGUERITE MARIE GERARD;RAVEGLIA LUCA FRANCESCO
分类号 C07D215/52;C07D401/06;C07D401/12;C07D401/14;C07D413/10;C07D417/12;C07D471/10;C07D487/04;C07D487/10;C07D491/10;(IPC1-7):A61K31/470 主分类号 C07D215/52
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