Patent ID: 6277862
Filing Date: 2001-08-21
Classification: A61P,C07D

Abstract:
A compound of formula (I): ##STR21##or a solvate thereof, or a salt thereof, wherein, Ar is an optionally substituted aryl or a C.sub.5-7 cycloalkdienyl 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 alkoxyxcarbonyl, 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 --O--(CH.sub.2).sub.n --X wherein X is carboxy, C.sub.1-6 alkoxycarbonyl, aminocarbonyl, mono- or di-C.sub.1-6 alkylaminocarbonyl; or X is a group --NX.sub.1 X.sub.2 wherein X.sub.1 and X.sub.2 each independently represent hydrogen, carboxyalkylcarbonyl, alkoxycarbonylalkylcarbonyl, alkylcarbonyl, arylcarbonyl, heteroarylcarbonyl, aryl-C.sub.1-6 -alkylcarbonyl, heteroaryl C.sub.1-6 -alkylcarbonyl, aminocarbonyl, mono- or bis-C.sub.1-6 alkylaminocarbonyl, amino C.sub.1-6 alkylcarbonyl, mono- or bis-C.sub.1-6 alkylamino C.sub.1-6 alkylcarbonyl, a moiety of formula --CO--T--CO--T.sub.1 or a 5 to 9 membered single or fused ring cycloalkyl group optionally comprising 1 or 2 nitrogen atoms and optionally 1 or 2 additional heteroatoms selected from O or N and wherein one or two ring atoms are optionally substituted with C.sub.1-6 alkyl, said ring being optionally fused to a benzene ring; wherein the above mentioned aryl and herteroaryl groups are optionally substituted with up to two groups selected from hydroxy, C.sub.1-6 alkoxy, hydroxy-C.sub.1-6 alkyl, amino-C.sub.1-6 -alkyl, mono- or bis- C.sub.1-6 -alkylamino, mono- bis-C.sub.1-6 -alkylamino-C.sub.1-6 - alkyl, amino-C.sub.1-6- alkoxy, mono- or bis- C.sub.1-6 -alkylamino-C.sub.1-6 -alkoxy, carboxy, C-.sub.1-6 -alkylcarbonyl, C-.sub.1-6 -alkoxycarbonyl, carboxy-C.sub.1-6 alkyl, carboxy-C.sub.1-6 alkoxy and C-.sub.1-6 -alkylcarbonyl C.sub.1-6 alkoxy; and wherein the alkyl moiety of any heteroaryl-C.sub.1-6 -alkyl or aryl-C.sub.1-6 -alkyl group is optionally substituted with an amino, a mono-C.sub.1-6 -alkylamino or a bis-C.sub.1-6 -alkyl amino group; or X is a C-linked single or fused ring heterocyclic group, any ring being saturated or unsaturated and consisting of 5- to 6-ring atoms, said ring atoms comprising 1 or 2 nitrogen atoms and optionally 1 or 21 additional heteroatoms selected from O or N and wherein one or two ring atoms are optionally substituted with C.sub.1-6 alkyl, hydroxy, amino, mono- or bis-C.sub.1-6 -alkylamino or an oxo substituent; and n is zero or an integer in the range of from 1 to 7 providing that when X is a group --NX.sub.1 X.sub.2, n is only an integer in the range of from 2 to 7 and providing that X.sub.1 and X.sub.2 are not simultaneously hydrogen; or R.sub.2 represents a moiety-NH--CO--NHY wherein Y represents C.sub.1-6 -alkyl, aryl, aryl C.sub.1-3 -alkyl, a moiety --(CH.sub.2).sub.p --X.sub.3 wherein p is an integer in the range of from 1 to 4 and X.sub.3 is carboxy, C.sub.1-6 alkoxycarbonyl, or a moiety --CO--NH--(CH.sub.2).sub.q --NX.sub.4 X.sub.5 wherein q is an integer in the range of from 2 to 4 and X.sub.4 and X.sub.5 each independently represent hydrogen, C.sub.1-6 alkyl or C.sub.1-6 alkylcarbonyl;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;T is a C.sub.1-6 alkylene or C.sub.2-6 alkenylene group; andT.sub.1 is hydroxy or C.sub.1-6 alkoxy.