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

Abstract

A compound, or a solvate or a salt thereof of formula (I), wherein, Ar is an optionally substituted aryl or a C5-7cycloalkdienyl group, or a C5-7cycloalkyl group or an optionally substituted single or fused ring aromatic heterocyclic group; R is C1-6 alkyl, C3-7cycloalkyl, C3-7cycloalkylalkyl, optionally substituted phenyl or phenylC1-6alkyl, an optionally substituted five-membered heteroaromatic ring comprising up to four heteroatoms selected from O and N, hydroxyC1-6alkyl, amino C1-6 alkyl, C1-6alkylaminoalkyl, di C1-6alkylaminoalkyl, C1-6acylaminoalkyl, C1-6alkoxyalkyl, C1-6alkylcarbonyl, carboxy, C1-6alkoxycarbonyl, C1-6alkoxycarbonylC1-6alkyl, aminocarbonyl, C1-6alkylaminocarbonyl, di C1-6alkylaminocarbonyl, halogenoC1-6alkyl; or R is a group —(CH2)p— wherein p is 2 or 3 which group forms a ring with a carbon atom of Ar; R1 represents hydrogen or up to four optional substituents selected from the list consisting of, C1-6alkyl, C1-6alkenyl, aryl, C1-6alkoxy, hydroxy, halogen, nitro, cyano, carboxy, carboxamido, suphonamido, C1-6 alkoxycarbonyl, trifluoromethyl, acyloxy, phthalimido, amino or mono- and di-C1-6alkylamino; R2 represents a moiety —(CH2)n—NY1Y2, wherein n is an integer in the range of 1 to 9, Y1 and Y2 are independently selected from hydrogen, C1-6alkyl, C1-6alkyl substituted with hydroxy, C1-6 alkylamino or bis (C1-6alkyl)amino, C1-6alkyl 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 C1-6alkyl, C3-7cycloalkyl, C4-7cycloalkylalkyl, optionally substituted aryl, or an optionally substituted single or fused ring aromatic heterocyclic group; and R4 represents hydrogen or C1-6 alkyl; a pharmaceutical composition comprising such a compound, process for preparing such a compound and the use of such a compound in medicine.

Dependencies are inferred from the claim text.