DERIVATIVES OF BENZOTHIAZOLE AND MEDICAMENT BASED ON THEREOF Russian patent published in 2007 - IPC C07D417/04 C07D417/14 A61K31/5377 

FIELD: organic chemistry, medicine, pharmacy.

SUBSTANCE: invention elates to derivatives of benzothiazole of the general formula (I): wherein R means hydrogen atom, -(CH₂)_n-phenyl optionally substituted with a substitute chosen from the following group: halogen atom, (lower)-alkyl, (lower)-alkoxy-group, trifluoromethyl or -N(R')-C(O)-(lower)-alkyl, -(CH₂)_n-pyridinyl optionally substituted with (lower)-alkyl, -(CH₂)_n-(C₃-C₆)-cycloalkyl optionally substituted with hydroxy-group, -(CH₂)_n-benzo[1,3]dioxolyl, -(CR'₂)-thiophenyl, -(CR'₂)_n-thiazolyl optionally substituted with (lower)-alkyl, -(CH₂)_n-C(O)-thiophenyl optionally substituted with halogen atom, -(CH₂)-furanyl optionally substituted with (lower)-alkyl, -(CHR')_n-benzofuran-1-yl, -(CH₂)n-benzo[b]thiophenyl, -(CH₂)_n-N(R')-C(O)-phenyl optionally substituted with halogen atom or (lower)-alkoxy-group. -(CH₂)_n-C(O)-phenyl optionally substituted with (lower)-alkoxy-group, -(CH₂)_n-C(O)-2,3-dihydrobenzo[1,4]dioxine-6-yl, -(CH₂)_n-N(R')-C(O)-pyridinyl, -(CH₂)_n-tetrahydrofuranyl, -CH-biphenyl, -CH-(phenyl)pyridinyl, -(CH₂)_n-1-oxo-(CH₂)_n-CH-(phenyl)tetrahydropyranyl, -(CH₂)_n-1-oxo-1,2,3,4-tetrahydroquinoline-3-yl or -(CH₂)_n-S-[1,3,4]thiadiazol-2-yl optionally substituted with amino-group; R' means hydrogen atom or (lower)-alkyl and independently of one another in case R'₂; n = 0, 1, 2, 3 or 4. Also, invention relates to a medicament possessing high affinity to adenosine A_2A-receptors and high selectivity with respect to A₁-receptors and comprising one or more derivatives of benzothiazole of the formula (I) and pharmaceutically acceptable excipients. Invention provides using derivatives of benzothiazole as ligands of adenosine receptors.

EFFECT: valuable medicinal properties of compounds and medicament.

13 cl, 2 tbl, 3 ex