| 摘要 |
The present invention relates to compounds of the general formula(I) wherein R1 is phenyl, piperidin-1-yl or morpholinyl; A is-O-and R is-(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")2, (CH2)n-pyridinyl, -(CH2)n-CF3, (CH2)n-2-oxo-pyrrolidinyl or C4-6-cycloalkyl; R" is independently from each other hydrogen or lower alkyl and n is 1 or 2; or A is-N(R')-and R is lower alkyl, C4-6-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" are independently from each other hydrogen or lower alkyl and n is 1 or 2; or A is CH2- and R is-N(R")-(CH2)m-O-lower alkyl, -N(R")2 S-lower alkyl, or is acetidinyl, pyrrolidinyl or piperidinyl, which optionally substituted by hydroxy or lower alkoxy or is morpholinyl, -N(R")-CH2)m-C4-6-cycloalkyl, -N(R")-(CH2m-C(O)O-lower alkyl, -N(R")-(CH2)m-C(O)OH, -2-oxo pyrrolidinyl, -N(R")-C(O)O-lower alkyl, -O(CH2)m-O-lower alkyl or alkoxy; R" is independently from each other hydrogen or lower alkyl and m is 1, 2 or 3; A is S- and R is lower alkyl; or A-R are together piperazinyl, substituted by lower alkyl, -C(O)-lower alkyl or a oxo group, or is piperidinyl, substituted by lower alkoxy or hydroxy, or is morpholinyl, substituted by lower alkyl, or is C4-6-cycloalkyl, -azetidin-1-yl, optionally substituted by hydroxy or lower alkoxy, thiomorpholine-1,1-dioxo, -tetrahydopyran or 2-oxa-5-aza-bicyclo[2.2.1]hept-5-yl; and to pharmaceutically acceptable acid addition salts thereof. It has been found that the compounds of general formula I are adenosine receptor ligands. Specifically, the compounds of the present invention have a good affinity to the A2A-receptor and they are therefore useful in the treatment of diseases related to this receptor.
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