2,7-SUBSTITUTED DERIVATIVES OF OCTAHYDROPYRROLO[1,2-A]PYRAZINE, METHOD OF TREATMENT, PHARMACEUTICAL COMPOSITION, AND INTERMEDIATES Russian patent published in 2001 - IPC

FIELD: pharmaceutical chemistry. SUBSTANCE: invention provides compounds of formula I: (I), wherein R₁ is phenyl, naphthyl, benzoxazolonyl, indolyl, indolonyl, benzimidazolyl, or quinolyl; R₂ is hydrogen or C1-C4- alkyl; R₃ phenyl, pyridyl, pyrimidinyl, pyrazinyl, or pyridazinyl; each of groups R₁ and R₃, independently from each other, being optionally substituted by one to four substituents independently selected from group including: fluorine, chlorine, bromine, iodine, cyano, nitro, C1-C6-alkoxy, -NR₄R₅,-NR₄COR₅,-CONR₄R₅, phenyl, -COR₄,-COOR₄, C1-C6-alkyl optionally substituted by 1 to 6 halogen atoms, C3-C6-cycloalkyl, and trifluoromethoxy; X denotes oxygen, NR₄, C=O, CH(OH), CHR₄, or group a, b, c or d: ; R₄ and R₅ are hydrogen or C1-C6- alkyl; m = 0, 1 or 2; n = 0, 1 or 2; all stereoisomers of compounds I and their pharmaceutically acceptable salts. Compounds of invention are ligands for subtypes of dopamine receptors, especially dopamine D₄ receptor, and are thereby suitable for treatment of dopamine system malfunction. Invention also describes intermediates, pharmaceutical composition, and treatment methods. EFFECT: extended assortment of biological active preparations. 23 cl, 18 ex