发明名称 THIAZOLOPYRIDINE DERIVATIVES AS ADENOSINE RECEPTOR LIGANDS
摘要 The present invention relates to compounds of the general formula (I) wherei n R1 is morpholin-4-yl, phenyl or tetrahydropyran-4-yl; R2 is -(CH2)n-aryl, unsubstituted or substituted by one or more substituents, selected from the group consisting of halogen, lower alkoxy, lower alkyl, -(CH2)n NR~R", -0 (CH2)n-O -lower alkyl, or -(CH2)n-heterocyclyl, or is heteroaryl, unsubstituted or substituted by one or more substituents, selected from the group consisting of lower alkyl, lower alkoxy, -(CH2)n NR'R", -(CH2)n- heterocyclyl, which is optionally substituted by hydroxy or lower alkoxy, or is -(CH2)n-heterocyclyl, optionally substituted by one or more substituents selected from the group consisting of -(CH2)n,-OH, -(CH2)n-O-lower alkyl or lower alkyl, or is -(CH2)n-cycloalkyl, or is - (CH2)n,-O -lower alkyl, or is NR'R~~, or is benzo[1,3]dioxole, 2-methyl-l-oxo-2,8-diaza-spiro[4,5] decane, 2- oxa-5-aza~bicyclo [2.2.1]heptane or I-oxa-8-aza-spiro[4.5]decane; R',R" are independently from each other lower alkyl, - (CH2)n ,-O -lower alkyl or cycloalkyl, optionally substituted by hydroxy; n is 0, 1 or 2; and to pharmaceutically acceptable acid addition salts thereof. These compounds may be used in the control or prevention of illnesses based on the modulation of the adenosine system, such as Alzheimer's disease, Parkinson's disease, Huntington's disease, neuroprotection, schizophrenia, anxiety, pain, respiration deficits, depression, drug addiction, such as amphetamine, cocaine, opioids, ethanol, nicotine, cannabinoids, or against asthma, allerg ic responses, hypoxia, ischaernia, seizure and substance abuse. Furthermore, compounds of the present invention may be useful as sedatives, muscle relaxants, antipsychotics, antiepileptics, anticonvulsants and cardiaprotective agents for disorders such as coronary artery disease and heart failure. The most preferred indications in accordance with the present invention are those which include disorders of the central nervous system, f or example the treatment or prevention of Alzheimer's disease, certain depressi ve disorders, drug addiction, neuroprotection and Parkinson's disease as well a s ADHD.
申请公布号 CA2539314(A1) 申请公布日期 2005.03.31
申请号 CA20042539314 申请日期 2004.09.11
申请人 F. HOFFMANN-LA ROCHE AG 发明人 NORCROSS, ROGER DAVID
分类号 C07D513/04;A61K31/4353;A61K31/4365 主分类号 C07D513/04
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