Quinoline-4-carboxamide derivatives as NK-3 and NK-2 receptor antagonists

   
   

A compound, or a solvate or a salt thereof, of formula (I): ##STR1## wherein, Ar is an optionally substituted aryl or a C.sub.5-7 cycloalkdienyl group, or an optionally substituted C.sub.5-7 cycloalkyl group, or an optionally substituted single or fused ring aromatic heterocyclic group; R is hydrogen, linear or branched C.sub.1-6 alkyl, C.sub.3-7 cycloalkyl, C.sub.3-7 cycloalkylalkyl; R.sub.1 represents hydrogen or up to three optional substituents selected from the list consisting of: C.sub.1-6 alkyl, C.sub.1-6 alkenyl, aryl, C.sub.1-6 alkoxy, hydroxy, halogen, nitro, cyano, carboxy, carboxamido, sulphonamido, C.sub.1-6 alkoxycarbonyl, trifluoromethyl, acyloxy, amino or mono- and di-C.sub.1-6 alkylamino, R.sub.2 represents a moiety --(CH.sub.2).sub.n --NYY.sub.2 wherein n is an integer in the range of from 1 to 9, Y.sub.1 and Y.sub.2 are independently selected from C.sub.1-6 -alkyl; C.sub.1-6 alkyl substituted with hydroxy, alkoxy, C.sub.1-6 alkylamino or bis (C.sub.1-6 alkyl) amino; C3-6 cycloalkyl; C4-6 azacycloalkyl; C.sub.1-6 -alkenyl; aryl or aryl-C.sub.1-6 -alkyl or Y.sub.1 and Y.sub.2 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 is branched or linear C.sub.1-6 alkyl, C.sub.3-7 cycloalkyl, C.sub.4-7 cycloalkylalkyl, optionally substituted aryl, or an optionally substituted single or fused ring aromatic heterocyclic group; and R.sub.4 represents hydrogen or C.sub.1-6 alkyl, R.sub.5 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.

 
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