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公开(公告)号：EP1636223A1
公开(公告)日：2006-03-22
申请号：EP04732950.3
申请日：2004-05-14
IPC分类号： C07D417/14 , C07D491/10 , C07D417/04 , A61K31/428 , A61P25/28
CPC分类号： C07D417/04 , C07D417/14 , C07D491/10
摘要： The invention relates to compounds of the general formula (I) wherein R1 is 1,4-dioxepanyl or tetrahydropyran-4-yl; R 2 is -N(R)-(CH2)n,-5-or 6 membered non aromatic heterocycle, optionally substituted by one or more substituents, selected from the group consisting of lower alkyl or -NR2, or is - (CH2)n-5-or 6 membered non aromatic heterocycle, optionally substituted by -(CH2)n-OH, lower alkyl, lower alkoxy, or is -CH2)n-5-or 6 membered aromatic heterocycle, optionally substituted by lower alkyl, lower alkoxy, halogen, halogen-lower alkyl, -CH2N(R)(CH2)20CH3, -N(R)(CH2)20CH3, -CH2-morpholinyl or -CH2-pyrrolidinyl or is (CH2)n-cycloalkyl, optionally substituted by hydroxy, or is -N(R)-cycloalkyl, optionally substituted by hydroxy or lower alkyl, or is phenyl, optionally substituted by lower alkoxy, halogen, halogen-lower alkyl, lower alkyl, -CH2-pyrrolidin-1-yl, -CH2-morpholinyl, -CH2N(R)(CH2)20CH3 or -CH2-N(R)C(O)-lower alkyl, or is 1,4-dioxa-8-aza-spiro[4,5]decane, or is 2-oxa-5-aza-bicyclo[2.2.1]heptane, or is I-oxa-8-aza-spiro[4,5]decane, or is -N(R)-7-oxa-bicyclo [2.2. 11 hept-2-yl, or is 2-aza-bicyclo[2.2.2]decane; R is hydrogen or lower alkyl; n is 0 or 1; and pharmaceutically acceptable acid addition salts thereof for the treatment of diseases, which relate to the A2A receptor.
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公开(公告)号：EP1456202A1
公开(公告)日：2004-09-15
申请号：EP02805304.9
申请日：2002-12-05
IPC分类号： C07D417/04 , A61K31/428 , A61P25/00
CPC分类号： C07D417/04 , C07D277/84 , C07D417/12 , C07D417/14
摘要： The present invention relates to compounds of the general formula (1), wherein R1 3,6-dihydro-2H-pyran-4-yl, 5,6-dihydro-4H-pyran-3-yl, t,6-dihydro-4H-pyran-2-yl, tetrahydropyran-2,3 or 4-yl, cyclohex-1-enyl, cyclohexyl or is 1,2,3,6-tetrahydro-pyridin-4yl or piperidin-4-yl, which are optionally substituted C(O)CH3in the 1-position of the N-atom; R2 is lower alkyl, piperidin-1yl, optionally substituted by hydroxy, or is phenyl, optionally substituted by (CH2)n-N(R')-C(O)-(CH2)n-NR'2,-(CH2)n-halogen, lower alkyl or (CH2)n-O-lower alkyl, or is morpholinyl or is pyridinyl, which is optionally substituted by halogen, -N(R')-(CH2)n-O-lower alkyl, lower alkyl, lower alkoxy, morpholinyl or (CH2)n-pyrrolidinyl; n is 0, 1 or 2; R' is hydrogen or lower alkyl, 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 may be used in the treatment of diseases, related to this receptor.
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