发明名称 QUINOLINE-4-CARBOXAMIDE DERIVATIVES AS NK-3 AND NK-2 RECEPTOR ANTAGONISTS.
摘要 <p>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-NY1Y2 wherein n is an integrer 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.</p>
申请公布号 MXPA01005095(A) 申请公布日期 2002.04.24
申请号 MX2001PA05095 申请日期 1999.11.19
申请人 SMITHKLINE BEECHAM S.P.A. 发明人 FARINA, CARLO
分类号 A61K31/4709;A61K31/496;A61K31/4985;A61K31/506;A61K31/5377;A61P1/00;A61P1/04;A61P1/14;A61P9/00;A61P9/10;A61P11/00;A61P11/02;A61P11/06;A61P11/14;A61P13/00;A61P13/12;A61P17/00;A61P17/04;A61P17/06;A61P19/02;A61P19/04;A61P25/00;A61P25/02;A61P25/04;A61P25/06;A61P25/08;A61P25/14;A61P25/16;A61P25/18;A61P25/22;A61P25/24;A61P25/28;A61P27/02;A61P29/00;A61P37/02;A61P37/04;A61P37/06;A61P37/08;A61P43/00;C07D215/52;C07D401/06;C07D401/12;C07D401/14;C07D413/10;C07D417/12;C07D471/04;C07D471/10;C07D487/04;C07D487/10;C07D491/10;C07D491/113;C07D498/10;(IPC1-7):A61K31/47;C07D209/00;C07D221/00;C07D235/00;C07D241/00;C07D317/00 主分类号 A61K31/4709
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