Patent ID: 6300334
Filing Date: 2001-10-09
Classification: A61P,C07D

Abstract:
A compound of formula (I): ##STR78##wherein:R represents a group --C(O)Ar.sup.1 or --C(R.sup.4)(R.sup.5)Ar.sup.1 ;Art represents a heterocyclic group comprising a total of from 5 to 10 atoms which include from 1 to 3 heteroatoms independently selected from nitrogen, oxygen and sulfur, which group Ar.sup.1 may be optionally substituted by one or more substituents independently selected from oxo, hydroxyl, C.sub.1-4 alkyl, C.sub.1-4 alkoxy, halogen, trifluoromethyl, amino, nitro, cyano, trifluoromethoxy, phenoxy, --CH.sub.2 N(R.sup.6).sub.2, --NHSO.sub.2 CF.sub.3, C.sub.1-4 alkylsulfonylamino, --NHC(O)R.sup.6a, CO.sub.2 R.sup.7 or --C(O)NR.sup.8 R.sup.8a, with the proviso that Ar.sup.1 does not represent an optionally substituted benzofuranyl, benzothienyl, indolyl, quinolyl or isoquinolyl group; R.sup.4 represents a hydrogen atom or a C.sub.1-4 alkyl group;R.sup.5 represents a hydrogen atom or a hydroxyl group; each R.sup.6 independently represents a hydrogen atom or a C.sub.1-4 alkyl group;R.sup.6a represents a hydrogen atom or C.sub.1-6 alkyl, phenyl, pyridinyl, (phenyl) C.sub.1-4 alkyl or (pyridinyl) C.sub.1-4 akyl, each of which may be optionally substituted by one or more substituents independently selected from C.sub.1-4 alkyl, C.sub.1-4 alkoxy, C.sub.1-4 alkylcarbonylamino, halogen or trifluoromethyl;R.sup.7 represents a hydrogen atom or a C.sub.1-4 alkyl group;R.sup.8 and R.sup.8a each independently represent a hydrogen atom or a C.sub.1-4 alkyl, phenyl or pyridinyl group;R.sup.1 and R.sup.2 each independently represent a hydrogen atom or a C.sub.1-6 alkyl, C.sub.3-6 alkenyl, CH.sub.2 C.sub.3-5 cycloalkyl or C.sub.3-6 cycloalkyl group;R.sup.3 a hydrogen atom or a group X--R.sup.9 or X--Ar.sup.2 ;X represents an oxygen atom, S(O).sub.n, C(O)NR.sup.10, C(O)O, NH(CO)NR.sup.10, NH(CO)O or SO.sub.2 NR.sup.10, with the proviso that when X represents an oxygen atom and R represents a group --C(R.sup.4)(R.sup.5)Ar.sup.1, then R.sup.4 and R.sup.5 both represent a hydrogen atom; n is 0, 1 or 2;R.sup.9 represents a methyl group optionally substituted by one or more substituents independently selected from cyano, carboxyl, C.sub.1-5 alkoxycarbonyl, 5-tetrazolyl or C(O)NR.sup.11 R.sup.12, or R.sup.9 represents a C.sub.2-6 alkyl or C.sub.3-6 alkenyl group, each of which may be optionally substituted by one or more substituents independently selected from hydroxyl, cyano, carboxyl, C.sub.1-5 alkoxy, C.sub.1-5 alkoxycarbonyl, 5-tetrazolyl, azido, phthalimido, SO.sub.2 NH.sub.2, C(O)NR.sup.11 R.sup.12, NR.sup.13 R.sup.14, NHC(O)R.sup.15 or NHSO.sub.2 R.sup.16 where R.sup.11, R.sup.12, R.sup.13 and R.sup.14 each independently represent a hydrogen atom or a C.sub.1-4 alkyl group, R.sup.15 represents a C.sub.1-4 alkyl, C.sub.1-4 alkoxy, amino or (di)C.sub.1-4 alkylamino group or an alkoxyalkylene group containing up to 6 carbon atoms, and R.sup.16 represents a C.sub.1-4 alkyl or trifluoromethyl group; or, additionally, in the case where X represents C(O)NR.sup.10, NH(CO)NR.sup.10 or SO--NR.sup.10, R.sup.9 and R.sup.10 together with the nitrogen atom to which they are attached may form a 4- to 7-membered saturated heterocyclic ring which may be optionally substituted by one or more hydroxyl groups;R.sup.10 represents a hydrogen atom or a C.sub.1-6 alkyl group or is linked to as defined above; andAr.sup.2 is phenyl, pyridinyl, thienyl, pyridone or pyridine N-oxide, each of which may be optionally substituted by one or more substituents independently selected from halogen, hydroxyl, nitro, amino, NHSO.sub.2 CF.sub.3, C.sub.1-4 alkyl, C.sub.1-4 alkoxy, bis-C.sub.1-4 alkanesulfonylamino, C.sub.1-4 alkylcarbonylamino or C.sub.1-4 alkoxycarbonylamino;or a pharmaceutically-acceptable salt or solvate thereof.