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    NICOTIN-OR ISONICOTIN BENZOTHIAZOLE DERIVATIVES
    4.
    发明授权
    NICOTIN-OR ISONICOTIN BENZOTHIAZOLE DERIVATIVES 有权
    烟酸或ISONICOTIN苯并噻唑衍生物

    公开(公告)号：EP1448198B1

    公开(公告)日：2007-10-31

    申请号：EP02787632.5

    申请日：2002-11-11

    申请人： F. HOFFMANN-LA ROCHE AG

    发明人： FLOHR, Alexander ,  JAKOB-ROETNE, Roland ,  NORCROSS, Roger, David ,  RIEMER, Claus

    IPC分类号： A61K31/4439 ,  C07D417/12 ,  C07D417/14

    CPC分类号： C07D417/12 ,  C07D417/14

    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-(CH¿2?)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.

    BENZOTHIAZOLE DERIVATIVES
    5.
    发明公开
    BENZOTHIAZOLE DERIVATIVES 有权
    苯并噻唑衍生物

    公开(公告)号：EP1450796A1

    公开(公告)日：2004-09-01

    申请号：EP02787718.2

    申请日：2002-11-18

    申请人： F. HOFFMANN-LA ROCHE AG

    发明人： FLOHR, Alexander ,  JAKOB-ROETNE, Roland ,  NORCROSS, Roger, David ,  RIEMER, Claus

    IPC分类号： A61K31/428 ,  A61K31/429 ,  A61K31/44 ,  A61P25/16 ,  A61P25/28 ,  C07D277/82 ,  C07D417/12 ,  C07D409/12 ,  C07D477/12

    CPC分类号： C07D277/68 ,  C07D417/12

    摘要： The invention relates to compounds of the general formula (I) wherein, R is hydrogen, -(CH2)n-phenyl, optionally substituted by halogen, lower alkyl, lower alkoxy, trifluoromethyl or -N(R')-C(O)-lower alkyl, -(CH2)n-pyridinyl, optionally substituted by lower alkyl, -(CH2)n-C3-6-cycloalkyl, optionally substituted by hydroxy, -(CH2)n-N(R')-C3-6-cycloalkyl, -(CH2)n-benzo[1,3]-dioxolyl, -(CR'2)n-thiophenyl, optionally substituted by lower alkyl, -(CR'2)n-thiazolyl, optionally substituted by lower alkyl, -(CH2)n-C(O)-thiophenyl, optionally substituted by halogen, -(CH2)n-furanyl, optionally substituted by lower alkyl, -(CH2)n-C(O)-(CH2)n-thiophenyl, -(CHR')n-benzofuran-2-yl, -(CH2)n-benzo[b]thiophenyl, optionally substituted by lower alkyl, -(CH2)n-N(R')-C(O)-phenyl, optionally substituted by halogen or lower alkoxy, -(CH2)n-C(O)-phenyl, optionally substituted by lower alkoxy, -(CH2)n-C(O)-2,3-dihydro-benzo [1,4]dioxin-6-yl, -(CH2)n-N(R')-C(O)-pyridinyl, -(CH2)n-tetrahydrofuranyl, -CH-bi-phenyl, -CH(phenyl)-pyridinyl, -(CH2)n-1-oxo-1,3-dihydro-isoindol-2-yl, -(CH2)n-1,3-dioxo-1,3-dihydro-isoindol-2-yl, -(CH2)n-CH(phenyl)-tetrahydropyranyl, -(CH2)n-1-oxo-1,2,3,4-tetrahydro-isoquinolin-3-yl or (CH2)n-S-[1,3,4]thiazol-2-yl, optionally substituted by amino; R' is hydrogen or lower alkyl, independently from each other in case R'2; and n is 0, 1, 2, 3 or 4; and pharmaceutically acceptable acid addition salts thereof. The compounds of formula I have a good affinity to the A2A receptor and they are therefore useful for the treatment of diseases, related to this receptor.

    BENZOTHIAZOLE DERIVATIVES AS ADENOSINE RECEPTOR LIGANDS
    10.
    发明公开
    BENZOTHIAZOLE DERIVATIVES AS ADENOSINE RECEPTOR LIGANDS 有权
    苯并噻唑作为腺苷受体配体

    公开(公告)号：EP1448196A1

    公开(公告)日：2004-08-25

    申请号：EP02803360.3

    申请日：2002-11-09

    申请人： F. Hoffmann-La Roche AG

    发明人： FLOHR, Alexander ,  JAKOB-ROETNE, Roland ,  NORCROSS, Roger, David ,  RIEMER, Claus

    IPC分类号： A61K31/4412 ,  C07D417/12 ,  A61P25/16 ,  A61P25/28

    CPC分类号： C07D417/14 ,  C07D417/12

    摘要： The present invention relates to compounds of the general formula (I): wherein R is phenyl, pyridin-2-yl, -C(O)-O-lower alkyl, -C(O)-lower alkyl, -C(O)-morpholinyl, -C(O)-NR'2,-(CH2)N-NR'2or -(CH2)N-O-lower alkyl and R' may be hydrogen or lower alkyl; and to pharmaceutically acceptable acid addition salts thereof. The compounds disclosed in this application have a good affinity to the A2A receptor and therefore they 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, allergic responses, hypoxia, ischaemia, 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.