Patent ID: 6218538
Filing Date: 2001-04-17
Classification: A61P,C07D

Abstract:
A compound of formula (I) ##STR16##including its 3,4-dihydropyrimidine tautomer form wherein:R.sup.1 represents a monocyclic aromatic ring optionally incorporating one to three heteroatoms which may be the same or different and are selected from N, O or S selected from the group consisting of phenyl, 2-pyridyl, 3-pyridyl, 4-pyridyl, pyrimidinyl, 2-thienyl, 3-thienyl, 2-furyl, 3-furyl, oxazolyl, thiazolyl, isoxazolyl, imidazolyl and thiadiazolyl, which ring may be optionally substituted by halogen, C1 to 6 alkyl, C1 to 6 alkoxy or trifluoromethyl;R.sup.2 represents C1 to 6 alkyl or unsaturated C2 to 6 alkyl, either optionally including O or S, and which is substituted by a phenyl or a monocyclic heteroaryl ring selected from the group consisting of 1-naphthyl, 2-naphthyl, 2-pyridyl, 3-pyridyl, 4-pyridyl, 2-thienyl, 3-thienyl, 2-furyl, 3-furyl, quinolyl, isoquinolyl, indolyl, benzothienyl, benzofuryl, oxazolyl, thiazolyl, isoxazolyl, imidazolyl and thiadiazolyl, which aromatic ring is optionally substituted by one or more substituents independently selected from halogen, C1 to 6 alkyl or C1 to 6 alkoxy;R.sup.3 represents a monocyclic or bicyclic aromatic ring optionally incorporating one heteroatom selected from N, O or S, selected from the group consisting of phenyl, 1-naphthyl, 2-naphthyl, 2-pyridyl, 3-pyridyl, 4-pyridyl, 2-thienyl, 3-thienyl, 2-furyl, 3-furyl, quinolyl, isoquinolyl, indolyl, benzothienyl and benzofuryl, optionally substituted by one or more substituents independently selected from halogen, C1 to 6 alkyl, C1 to 6 alkoxy, cyano, benzyloxy, trifluoromethyl, amino, hydroxy, nitro or carbomethoxy;R.sup.4 and R.sup.5 independently represent hydrogen, C1 to 6 alkyl, or benzyl; or the group NR.sup.4 R.sup.5 together represents piperidinyl, morpholinyl, 3,4-dehydropiperidinyl, thiomorpholinyl, perhydroazepinyl, pyrrolidinyl, piperazinyl or piperazinyl further substituted at N-4 by C1 to 6 alkyl;X represents O, S or NR.sup.6 ;R.sup.6 represents hydrogen or alkyl C1 to 6;and n represents an integer 2 to 4;and optical isomers and racemates thereof or pharmaceutically acceptable salts thereof.