ALKYL-SUBSTITUTED CYCLIC AMINES AS SELECTIVE LIGANDS OF D3-DOPAMINE Russian patent published in 2002 - IPC

FIELD: organic chemistry. SUBSTANCE: invention relates to alkyl-substituted cyclic amines of the formula (I): where X and Y are in position 5, 6 or 7 where: (i) n = 1; X means where m = 0 or 1 with exception of case that when m = 0 then Y can not mean hydrogen atom, and Y means hydrogen atom or OR₆; (ii) n = 0 or 1 and in this case X and Y are in ortho-position relatively each to other and they in common form: (a) -C(O)NR₁₀C(O)-; (b) -C(O)NR₄(CH₂)_xNR₁₀C(O)- (where x = 0 or 1); (c) -CH₂NR₁₀C(O)-; (d) -(CH₂)₂NR₁₀C(O)-; (e) -CH₂C(O)NR₁₀; (g) -N(R₃)-C(O)-O-; (j) -CH₂N(R₈)CH₂; iii) n = 0 and Y means OR₉ and in this case X means (CH₂)_mCONR₄R₅, (CH₂)_mNHCOR₃ (where m = 0 or 1); R₁ and R₂ mean independently C₁-C₈-alkyl; R₃ means C₁-C₈-alkyl, aryl; R₄ and R₅ mean independently H, C₁-C₈-alkyl, C₁-C₆-alkylaryl or aryl; C₆ means C₁-C₈-alkyl; R₈ means C₁-C₈-alkyl, SO₂R₄ (under condition that R₄ does not mean hydrogen atom); R₁₀ means H, C₁-C₈-alkyl, C₁-C₆--alkylaryl and aryl in all indicated value means phenyl possibly substituted with methyl, nitro-group, chlorine, fluorine, bromine atom, amino-group, CN, carboxamido-group, acetyl; or it means thiophenyl, isoxazolyl, imidazolyl. Compounds of the formula (I) are selective ligands of D3-dopamine that ensures to use their in treatment of disorders of the central nervous system. EFFECT: valuable medicinal properties of compounds. 16 cl, 2 tbl