| 摘要 |
The use of 4- and/or 5-substituted 4,5-dihydro-thiazol-2-ylamine compounds (I) for the treatment or prophylaxis of diseases involving abnormal production of nitrogen monoxide (NO) due to induction of inducible nitrogen monoxide synthase (NOS-2), is new. Most compounds (I) are new. Also new are some intermediates. The use of 4- and/or 5-substituted 4,5-dihydro-thiazol-2-ylamine compounds of formula (I) (including racemates, enantiomers or diastereomers and mixtures) or their tautomers or salts is claimed in the preparation of pharmaceutical compositions for the treatment or prophylaxis of diseases involving abnormal production of nitrogen monoxide (NO) due to induction of inducible nitrogen monoxide synthase (NOS-2). R1 = H or alkyl; and R2 = alkyl, -A-NH2, -CH2R3 or -CH2SR4, or phenyl substituted by NO2 or -NHC(=NH)Me; or R1 = alkyl; and R2 = H; R3 = 3-6C cycloalkyl, pyridyl, N-oxidized pyridyl, thienyl, thiazolyl, imidazolyl, pyrazinyl, triazolyl or phenyl (optionally substituted by NO2, OH or COOH); R4 = pyridyl or N-oxidized pyridyl, and A = alkylene; alkyl and alkylene moieties have 1-6C. Independent claims are included for the following: (1) new compounds (I) (including racemates, enantiomers or diastereomers and mixtures) and their tautomers and salts, provided that R3 and R4 are other than N-oxidized pyridyl and that (I; R1 = hexyl or methyl; R2 = H), (I; R1, R2 = Me) and racemic (I; R1 = H; R2 =1-3C n-alkyl), are excluded; (2) preparation of the new compounds (I); (3) new intermediates of formulae (II) (provided that R1 = H), (III) and (II'); and (4) preparation of (II; R1 = H). Ra = H or protecting group, e.g. tert. butoxycarbonyl.
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