| abstract |
"NICOTIN- OR ISONICOTIN-BENZOTIAZOL DERIVATIVES". The present invention relates to compounds of formula (I): wherein: R4 is phenyl, piperidin-1-yl or morpholinyl; A is -O- and R is (CH ~ 2 ~) ~ n ~ -N (R ") -C (O) -lower alkyl, - (CH ~ 2 ~) ~ n ~ -O-lower alkyl, - ( CH ~ 2 ~,) ~ n ~ -O- (CH ~ 2 ~) ~ n ~ O-lower alkyl, lower alkyl, - (CH ~ 2 ~) ~ n ~, morpholinyl, - (CH ~ 2 ~ ) ~ n -phenyl, - (CH ~ 2 ~,) ~ n ~ -N (R ") ~ 2 <39> ~ - (CH ~ 2 ~) ~ n-pyridinyl, - (CH ~ 2 ~) ~ n -CF-3 ', - (CH -2') -N n -2-oxo-pyrrolidinyl or C 4-6 -cycloalkyl; R "is independently hydrogen or lower alkyl; n is 1 or 2; or A is -N (R <R>) -, and R is lower alkyl, C 4-6 -cycloalkyl, - (CH 2 -). ~ n ~ O-lower alkyl, - (CH ~ 2 ~) ~ n ~ pyridinyl, - (CH ~ 2 ~) ~ n ~ piperidinyl, - (CH ~ 2 ~) ~ n ~ phenyl, - ( CH ~ 2 ~) ~ n ~ -N (R ") - C (O) -lower alkyl, - (CH ~ 2 ~) ~ n ~ morpholinyl or - (CH ~ 2 ~) ~ n ~ -N (R" ) R 2 and R 3 are independently from each other hydrogen or lower alkyl; and n is 1 or 2; or A is -CH ~ 2 ~ -, and R is -N (R ") - (CH ~ 2 ~) ~ m -O-lower alkyl, -N (R") ~ 2 ~, S-lower alkyl or is acetidinyl, pyrrolidinyl or piperidinyl which are optionally substituted by hydroxy or lower alkoxy or is morpholinyl, -N (R ') - (CH 2 -) - m -C (O) OH, -2-oxo-pyrrolidinyl -N (R ") -C (O) O-lower alkyl, -O- (CH-2 ~) -M-O-lower alkyl or alkoxy; R "is independently hydrogen or lower alkyl; em is 1, 2 or 3; or A is -S-, and R is lower alkyl; or AR are together: piperazinyl, substituted by lower alkyl, -C (O) -lower alkyl or an oxo group is either piperidinyl, substituted by lower alkoxy or hydroxy, or is morpholinyl, substituted by lower alkyl, or is C 4-6 -cycloalkyl, azetidin-1-yl, optionally substituted by hydroxy or lower alkoxy, thiomorpholine-1,1-dioxo, tetrahydropyran or 2-oxa-5-aza-bicyclo [2.2.1] hept-5-yl, and pharmaceutically acceptable acid addition salts thereof. I are adenosine receptor ligands Specifically, the compounds of the present invention have satisfactory affinity for the A 2A receptor, and are therefore useful in treating diseases related to that receptor. |