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

   
   

A compound, or a solvate or a salt thereof, of formula (I): 1 wherein, Ar is an optionally substituted aryl or a C.sub.5-7 cycloalkdienyl group, or a C.sub.5-7 cycloalkyl group or an optionally substituted single or fused ring aromatic heterocyclic group; R is C.sub.1-6 alkyl, C.sub.3-7 cycloalkyl, C.sub.3-7 cycloalkylalkyl, optionally substituted phenyl or phenyl C.sub.1-6 alkyl, an optionally substituted five-membered heteroaromatic ring comprising up to four heteroatoms selected from O and N, hydroxy C.sub.1-6 alkyl, amino C.sub.1-6 alkyl, C.sub.1-6 alkylaminoalkyl, di C.sub.1-6 alkylaminoalkyl, C.sub.1-6 acylaminoalkyl, C.sub.1-6 alkoxyalkyl, C.sub.1-6 alkylcarbonyl, carboxy, C.sub.1-6 alkoxycarbonyl, C.sub.1-6 alkoxycarbonyl C.sub.1-6 alkyl, aminocarbonyl, C.sub.1-6 alkylaminocarbonyl, di C.sub.1-6 alkylaminocarbonyl, halogeno C.sub.1-6 alkyl; or R is a group --(CH.sub.2).sub.p-- wherein p is 2 or 3 which group forms a ring with a carbon atom of Ar; R.sub.1 represents hydrogen or up to four 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, phthalimido, amino or mono- and di-C.sub.1-6 alkylamino; R.sub.2 represents a moiety --(CH.sub.2).sub.n--NY.sub.1Y.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 hydrogen; C.sub.1-6-alkyl; C.sub.1-6 alkyl substituted with hydroxy, C.sub.1-6 alkylamino or bis(C.sub.1-6 alkyl)amino; 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; a pharmaceutical composition comprising such a compound, process for preparing such a compound and the use of such a compound in medicine.

 
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