Title:
【発明の名称】NK-3およびNK-2受容体アンタゴニストとしてのキノリン-4-カルボキシアミド誘導体
Document Type and Number:
Japanese Patent JP2002530377
Kind Code:
A
Abstract:
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.
Inventors:
Carlo Farina
Giuseppe Giardina
Mario gruni
Marcel Morvan
Guy Marguerite Marie Gerard Nadre
Luca Francesco Laveria
Giuseppe Giardina
Mario gruni
Marcel Morvan
Guy Marguerite Marie Gerard Nadre
Luca Francesco Laveria
Application Number:
JP2000583865A
Publication Date:
September 17, 2002
Filing Date:
November 19, 1999
Export Citation:
Assignee:
SmithKline Beecham S.p.A.
SmithKline Beecham Laboratoire Pharmacy
SmithKline Beecham Laboratoire Pharmacy
International Classes:
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): C07D215/52; 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; C07D401/06; C07D401/12; C07D401/14; C07D417/12; C07D471/04; C07D471/10; C07D487/10; C07D491/113; C07D498/10
Attorney, Agent or Firm:
Aoyama Ryo (1 person outside)