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PROCESS FOR PRODUCING 2,9-DISUBSTITUTED-4H-PYRIDO(1,2-A)PYRIMIDINE-4-ONE DERIVATIVES AND PHARMACEUTICAL COMPOSITIONS COMPRISING SUCH COMPOUNDS AS ACTIVE INGREDIENT
PROCESS FOR PRODUCING 2,9-DISUBSTITUTED-4H-PYRIDO(1,2-A)PYRIMIDINE-4-ONE DERIVATIVES AND PHARMACEUTICAL COMPOSITIONS COMPRISING SUCH COMPOUNDS AS ACTIVE INGREDIENT
Compounds of formula CHEM pharmaceutically acceptable acid addition salts thereof, and stereochemically isomeric forms thereof, wherein Alk is C1-4alkanediyl, and D is CHEM wherein R1 represents C1-4alkyl, hydroxyC1-4alkyl, carboxaldehyde, carboxyl, C1-10alkylcarbonyloxyC1-4alkyl; each R2 represents hydrogen or C1-4alkyl; R3 represents C1-4alkyl, hydroxyC1-4alkyl or methyl substituted with phenyl, 5-methyl-2-furanyl or 3-pyridinyl; and R4 represents C1-3alkyl, phenyl, 5-methyl-2-furanyl or 3-pyridinyl, which compounds are potent antagonists of dopamine and are therapeutically useful in treating patients suffering from acute psychoses. Compositions containing these compounds as active ingredient and processes of preparing said compounds and compositions.
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机译:式的化合物及其药学上可接受的酸加成盐及其立体化学异构体形式,其中Alk为C1-4烷二基,D为,其中R <1>代表C1-4烷基,羟基C1-4烷基,羧醛,羧基, C1-10烷基羰基氧基C1-4烷基;每个R 2代表氢或C 1-4烷基; R 3表示C 1-4烷基,羟基C 1-4烷基或被苯基,5-甲基-2-呋喃基或3-吡啶基取代的甲基; R 4代表C 1-3烷基,苯基,5-甲基-2-呋喃基或3-吡啶基,这些化合物是多巴胺的有效拮抗剂,并且在治疗患有急性精神病的患者中在治疗上有用。包含这些化合物作为活性成分的组合物以及制备所述化合物和组合物的方法。
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