发明名称 QUINOLINE-4-CARBOXAMIDE AS NK-2 AND NK-3 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 C<SUB>5-7 </SUB>cycloalkdienyl group, or a C<SUB>5-7 </SUB>cycloalkyl group or an optionally substituted single or fused ring aromatic heterocyclic group,; R is C<SUB>1-6 </SUB>alkyl, C<SUB>3-7 </SUB>cycloalkyl, C<SUB>3-7 </SUB>cycloalkylalkyl, optionally substituted phenyl or phenyl C<SUB>1-6 </SUB>alkyl, an optionally substituted five-membered heteroaromatic ring comprising up to four heteroatoms selected from O and N, hydroxy C<SUB>1-6 </SUB>alkyl, amino C<SUB>1-6 </SUB>alkyl, C<SUB>1-6 </SUB>alkylaminoalkyl, di C<SUB>1-6 </SUB>alkylaminoalkyl, C<SUB>1-6 </SUB>acylaminoalkyl, C<SUB>1-6 </SUB>alkoxyalkyl, C<SUB>1-6 </SUB>alkylcarbonyl, carboxy, C<SUB>1-6 </SUB>alkoxycarbonyl, C<SUB>1-6 </SUB>alkoxycarbonyl C<SUB>1-6 </SUB>alkyl, aminocarbonyl, C<SUB>1-6 </SUB>alkylaminocarbonyl, di C<SUB>1-6 </SUB>alkylaminocarbonyl, halogeno C<SUB>1-6 </SUB>alkyl; or R is a group -(CH<SUB>2</SUB>)<SUB>p</SUB>- wherein p is 2 or 3 which group forms a ring with a carbon atom of Ar; R<SUB>1 </SUB>represents hydrogen or up to four optional substituents selected from the list consisting of: C<SUB>1-6 </SUB>alkyl, C<SUB>1-6 </SUB>alkenyl, aryl, C<SUB>1-6 </SUB>alkoxy, hydroxy, halogen, nitro, cyano, carboxy, carboxamido, sulphonamido, C<SUB>1-6 </SUB>alkoxycarbonyl, trifluoromethyl, acyloxy, phthalimido, amino or mono- and di-C<SUB>1-6 </SUB>alkylamino; R<SUB>2 </SUB>represents a moiety -(CH<SUB>2</SUB>)<SUB>n</SUB>-NY<SUB>1</SUB>Y<SUB>2 </SUB>wherein n is an integer in the range of from 1 to 9, Y<SUB>1 </SUB>and Y<SUB>2 </SUB>are independently selected from hydrogen; C<SUB>1-6</SUB>-alkyl; C<SUB>1-6 </SUB>alkyl substituted with hydroxy, C<SUB>1-6 </SUB>alkylamino or bis (C<SUB>1-6 </SUB>alkyl) amino; C<SUB>1-6</SUB>-alkenyl; aryl or aryl-C<SUB>1-6</SUB>-alkyl or Y<SUB>1 </SUB>and Y<SUB>2 </SUB>together with the nitrogen atom to which they are attached represent an optionally substituted N-linked single or fused ring heterocyclic group; R<SUB>3 </SUB>is branched or linear C<SUB>1-6 </SUB>alkyl, C<SUB>3-7 </SUB>cycloalkyl, C<SUB>4-7 </SUB>cycloalkylalkyl, optionally substituted aryl, or an optionally substituted single or fused ring aromatic heterocyclic group; and R4 represents hydrogen or C<SUB>1-6 </SUB>alkyl; a pharmaceutical composition comprising such a compound, process for preparing such a compound and the use of such a compound in medicine.
申请公布号 US2007197546(A1) 申请公布日期 2007.08.23
申请号 US20070691899 申请日期 2007.03.27
申请人 发明人 GIARDINA GIUSEPPE A.M.;GRUGNI MARIO;GRAZIANI DAVIDE;RAVEGLIA LUCA F.
分类号 A61K31/4709;A61K31/496;C07D401/02 主分类号 A61K31/4709
代理机构 代理人
主权项
地址