abstract |
The 3-substituted 3,4,5,6,7,8-hexahydro-pyrido [4 ', 3': 4,5] thieno [2,3-d] pyrimidine derivatives can be used as medicaments for diseases which have been shown to reduce serotonin concentration, and in which the activity of the presynaptic receptors 5-HT1B-, 5-HT1A-, 5-HT1D- without interfering with other receptors should be blocked within the therapy. An example of such a disease state is depression. The compounds have the formula wherein R 1 is hydrogen, C 1 -C 4 -alkyl, acetyl, benzoyl, phenylalkyl-C 1 -C 4 -alkyl, wherein the aromatic residue is optionally substituted with halogen, C 1 -C 4 -alkyl, trifluoromethyl, , C1-C4-alkoxy-, amino-, cyano- or nitro groups or is a naphthalene-C1-C3-alkyl residue, a phenylalkanone-C2-C3- residue or a phenylcarbamoyl-C2-residue. R 2 is optionally mono-, di- or tri-substituted with halogen atoms, C 1 -C 4 -alkyl, trifluoromethyl, trifluoromethoxy, hydroxy, C 1 -C 4 -alkoxy, amino-, monomethylamino-, dimethylamino-, cyano- or nitro, pyridyl, pyrimidinyl or pyrazinyl residue which may optionally be anionized with a benzene ring which may optionally be mono- or disubstituted by a halogen atom, C1-C4-alkyl, hydroxy, trifluoromethyl, C1-C4-alkoxy -, amino, cyano or nitro group, and may optionally contain one nitrogen atom or be anionized with a 5- or 6- membered ring which may contain one to two oxygen atoms, or |