3-substituted pyrido 3',4':4,5 thieno 2,3-d pyrimidine derivatives for treating 5-HT1B/D receptor related disorders which increases serotonin release in the brain

摘要

A 3-substituted 3,4,5,6,7,8-hexahydropyrido[3',4':4,5]thieno-[2,3-d]pyrimidine derivative of the formula described useful for treating pathological states in which the serotonin concentration is reduced by specifically blocking the activity of the presynaptic 5-HT1B, 5-HT1A, 5-HT1D receptors. The compounds are useful for treating mood disorders with a central nervous causation, such as seasonal affective disorders and dysthymia, including anxiety states disorders, sociophobia, obsessive-compulsive neuroses, post traumatic stress symptoms, memory disturbances, age-related memory loss, and psychogenic eating disorders. Wherein; R1 is a hydrogen atom, a C1-4alkyl group, an acetyl group, a phenylalkylC1-4 radical, the aromatic system being unsubstituted or substituted by halogen, C1-4alkyl, trifluoromethyl, hydroxyl, C1-4alkoxy, amino, cyano or nitro groups, or is a phenylalkanone radical, it being possible for the phenyl group to be substituted by halogen; R2 is a phenyl, pyridyl, pyrimidinyl or pyrazinyl group which is unsubstituted or mono- or disubstituted by halogen atoms, C1-4alkyl, trifluoromethyl, trifluoromethoxy, hydroxyl, C1-4alkoxy, amino, monomethylamino, dimethylamino, cyano or nitro groups and which may be fused to a benzene nucleus which can be unsubstituted or mono- or disubstituted by halogen atoms, C1-4alkyl, hydroxyl, trifluoromethyl, C1-4alkoxy, 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, it also being possible for the linkage between Y and Z to be a double bond; and n is 2, 3 or 4.