| abstract |
FIELD: organic chemistry, medicine, pharmacy. n SUBSTANCE: invention elates to derivatives of benzothiazole of the general formula (I): wherein R means hydrogen atom, -(CH 2 ) 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, -(CH 2 ) n -pyridinyl optionally substituted with (lower)-alkyl, -(CH 2 ) n -(C 3 -C 6 )-cycloalkyl optionally substituted with hydroxy-group, -(CH 2 ) n -benzo[1,3]dioxolyl, -(CR' 2 )-thiophenyl, -(CR' 2 ) n -thiazolyl optionally substituted with (lower)-alkyl, -(CH 2 ) n -C(O)-thiophenyl optionally substituted with halogen atom, -(CH 2 )-furanyl optionally substituted with (lower)-alkyl, -(CHR') n -benzofuran-1-yl, -(CH 2 )n-benzo[b]thiophenyl, -(CH 2 ) n -N(R')-C(O)-phenyl optionally substituted with halogen atom or (lower)-alkoxy-group. -(CH 2 ) n -C(O)-phenyl optionally substituted with (lower)-alkoxy-group, -(CH 2 ) n -C(O)-2,3-dihydrobenzo[1,4]dioxine-6-yl, -(CH 2 ) n -N(R')-C(O)-pyridinyl, -(CH 2 ) n -tetrahydrofuranyl, -CH-biphenyl, -CH-(phenyl)pyridinyl, -(CH 2 ) n -1-oxo-(CH 2 ) n -CH-(phenyl)tetrahydropyranyl, -(CH 2 ) n -1-oxo-1,2,3,4-tetrahydroquinoline-3-yl or -(CH 2 ) 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 A 1 -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. n EFFECT: valuable medicinal properties of compounds and medicament. n 13 cl, 2 tbl, 3 ex |