abstract |
Thiazolopyridine derivs. of formula (I), mixts. of their isomers and their acid-addn. salts, are new. In the formula, one of X and Y is N and the other is O; R1 is H, lower alkyl, OH, SH, lower alkoxy, lower alkylthio or phenyl; R2 is lower alkyl, 7-8C aralkyl or phenyl opt. mono-,di or trisubstd. by halogen, lower alkyl, lower alkoxy, CF3, COOH, CONH2 and/or lower alkoxycarbonyl; R3 is H, lower alkyl, acyl, lower alkoxycarbonyl, or 7-8C aralkyl opt. mono- or disubstd. by halogen; n = 1-3; m = 1-3; m+n = 2-4. (I) are esp. useful as anorexigenic agents with little effect on motility and little or no cardiovascular side-effects. They also have antiarrhythmic, antiasthmatic, antiinflammatory, antihypertensive, antithrombotic, beta-adrenergic blocking, anxiolytic, bronchodilatory, myorelaxant, hypolipaemic and hypoglycaemic activity. A typical cpd. is 10-phenyl-5,6,7,9-tetrahydro-8H-thiazolo 5',4':5,6 pyrido 3,2-c a- zepine. In an example, this is prepd. from 4-amino-5-benzoylthiazole and hexahydro-4-azepinone. |