DERIVATIVES OF NICOTINE- OR ISONICOTINE-BENZOTHIAZOLE AND MEDICINAL AGENT

摘要

FIELD: organic chemistry, medicine, pharmacy.;SUBSTANCE: invention relates to derivatives of nicotine- or isonicotine-benzothiazole of general formulas (IA) and (IB) their pharmaceutically acceptable acid-additive salts and a medicinal agent based on thereof. In compounds of general formula (IA) and (IB) R¹ means phenyl, piperidine-1-yl or morpholine; A means -O-; R means -(CH₂)_n-N(R'')-C(O)-lower alkyl, -(CH₂)_n-O-lower alkyl, -(CH₂)_n-O-(CH₂)_n-O-lower alkyl, lower alkyl, -(CH₂)_n-morpholinyl, -(CH₂)_n-phenyl, -(CH₂)_n-N(R''), -(CH₂)_n-pyridinyl, -(CH₂)_n-CF₃, -(CH₂)_n-2-oxopyrrolidinyl or (C₄-C₆)-cycloalkyl; R'' mean(s) independently of one another hydrogen atom or lower alkyl; n= 1 or 2; A means -N(R')-; R means lower alkyl, (C₄-C₆)-cycloalkyl, -(CH₂)_n-O-lower alkyl, -(CH₂)_n-pyridinyl, -(CH₂)_n-piperidinyl, -(CH₂)_n-phenyl, -(CH₂)_n-N(R'')-C(O)-lower alkyl, -(CH₂)_n-morpholinyl or -(CH₂)_n-N(R'')₂; R' and R'' mean independently of one another hydrogen atom or lower alkyl; n = 1 or 2; or A means -CH₂-; R means -N(R'')-(CH₂)_m-O-lower alkyl, -N(R'')₂, S-lower alkyl, or R means azethidinyl, pyrrolidinyl or piperidinyl that are substituted optionally with hydroxy-group or lower alkoxy-group; or R means morpholinyl, -N(R'')-(CH₂)_m-(C₄-C₆)-cycloalkyl, -N(R'')-(CH₂)_m-C(O)-O-lower alkyl, -O-(CH₂)_m-O-lower alkyl or alkoxy-group; R'' mean(s) independently of one another hydrogen atom or lower alkyl; m = 1, 2 or 3; or A means -S-; R means lower alkyl, or A-R mean in common piperazinyl substituted with alkyl, -C(O)-lower alkyl or oxo-group, or group A-R means piperidinyl substituted with lower alkoxy-group or hydroxy-group, or group A-R means morpholinyl substituted with lower alkyl, or group A-R means (C₄-C₆)-cycloalkyl, azethidine-1-yl optionally substituted with hydroxy-group or lower alkoxy-group, or group A-R means thiomorpholinyl-1,1-dioxo-group, tetrahydropyrane or 2-oxa-5-azabicyclo[2.2.1]hept-5-yl. Proposed compounds can be used in treatment of diseases mediated by adenosine A_2A-receptors, for example, Alzheimer disease, some depressive states, toxicomania and Parkinson's disease.;EFFECT: valuable medicinal properties of compounds and agent.;37 cl, 10 sch, 109 ex