4,5,7,8-TETRAHYDRO-6H-THIAZOLO[5,4-D]AZEPINES, THEIR PREPARATION AND THEIR USE AS PHARMACEUTICALS

摘要

The present invention relates to new 4,5,7,8tetrahydro-6H-thiazolo¢5,4-d!azepines of formula II <IMG> (II) (wherein A represents one of the groups -C(R3)=CH-, -CH=C(R4)-, <IMG> , - C ? C-, -CH=CH-CH2 * . * * -CH(OR5)-CH2- or -(CH2) n * (wherein n represents the number 2, 3 or 4, R3 represents a hydrogen atom or a methyl group, R4 represents a C1-3 alkyl group or a phenyl group, and R5 represents a hydrogen atom or a methyl or ethyl group, and the carbon atom designated * is linked to the group R1), and R1 represents an optionally substituted phenyl group; a pyridyl group optionally substituted by a chlorine atom or by a methyl, methoxy, benzyloxy or hydroxy group; a naphthyl, quinolyl, isoquinolyl, indolyl, furyl, thienyl, (2-indolinon)yl, carbostyryl or 3,4dihydrocarbostyryl group; a thiazolyl group optionally substituted in the 2position by a methyl or amino group; a benzothiophenyl or benzofuranyl group; or a benzothiazolyl, benzoxazolyl or benzimidazolyl group optionally substituted in the 2-position by a methyl, phenyl or amino group; or A represents a carbon-carbon bond, and R1 represents an indenyl or dihydronaphthalenyl group or a benzopyran or benzothiapyran group optionally substituted by one or two methyl groups; and R2 represents a hydrogen atom or an acetyl or propionyl group optionally substituted in the omega-position by a phenyl or 4-methoxyphenyl group, and the acid addition salts thereof. The new compounds have valuable pharmacological properties, namely selective effects on the dopaminergic system which are achieved by stimulating (predominantly D2) dopamine receptors.