3-Substituted 3,4,5,7-tetrahydropyrrolo[3',4':4,5]thieno[2,3-d]pyrimidine derivatives, their preparation and use as 5HT antagonists

摘要

A 3-substituted 3,4,5,7-tetrahhydropyrrolo[3',4':4,5]-thieno[2,3-d]pyrimidine derivative of the formula I, wherein, R1is a hydrogen atom, a C1-C4 alkyl group, an acetyl group, a phenylalkyl c1-c4 radical where the aromatic ring is unsubstituted or substituted by halogen, C1-C4 alkyl, trifluoromethyl, hydroxyl, C1-C4 alkoxy, amino, cyano or nitro groups, or is a C1-C3 alkyl carboxylate radical, R2 is a phenyl, pyridyl, pyrimidinyl or pyrazinyl group which is unsubstituted or mono or disubstituted by halogen atoms, C1-C4 alkyl, trifluoromethyl, trifluoromethoxy, hydroxyl, C1-C4 alkoxy, amino, monoethylamino, dimethylamino, cyano or nitro groups, and may be fused to a benzene nucleus which may be mono or disubstituted by halogen atoms, C1-C4 alkyl, hydroxyl, trifluoromethyl, C1-C4 alkoxy, amino, cyano or nitro groups and may contain 1 nitrogen atom, or to a 5 or 6 membered ring which may contain 1-2 oxygen atoms, A is NH or an oxygen atom, Y is CH2, CH2-CH2, CH2-CH2-CH2 or CH2-CH, Z is a nitrogen atom, carbon atom or CH, where the linkage between Y and Z may also be a double bond, and n is 2,3 or 4, or a physiologically tolerated salt thereof. These compounds are useful as selective 5HT1B and/or 5HT1A antagonists.