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41 条记录 (耗时 0.035 秒)

    Triaza-cyclopenta[cd]indene derivatives
    8.
    发明授权
    Triaza-cyclopenta[cd]indene derivatives 失效
    三氮杂 - 环戊二烯并[cd]茚衍生物

    公开(公告)号：US07365078B2

    公开(公告)日：2008-04-29

    申请号：US10584952

    申请日：2005-01-06

    申请人： Atsuro Nakazato ,  Taketoshi Okubo ,  Dai Nozawa ,  Tomoko Tamita ,  Ludo E. J. Kennis

    发明人： Atsuro Nakazato ,  Taketoshi Okubo ,  Dai Nozawa ,  Tomoko Tamita ,  Ludo E. J. Kennis

    IPC分类号： A01N43/54 ,  A61K31/505 ,  C07D239/00 ,  C07D471/00 ,  C07D487/00 ,  C07D491/00

    CPC分类号： C07D487/16

    摘要： An object of the present invention is to provide an antagonist against CRF receptors which is effective as a therapeutic or prophylactic agent for diseases in which CRF is considered to be involved, such as depression, anxiety, Alzheimer's disease, Parkinson's disease, Huntington's chorea, eating disorder, hypertension, gastral diseases, drug dependence, epilepsy, cerebral infarction, cerebral ischemia, cerebral edema, cephalic external wound, inflammation, immunity-related diseases, alpecia, irritable bowel syndrome, sleep disorders, dermatitides, schizophrenia, pain, etc. A triaza-cyclopenta[cd]indene derivative represented by the following formula [I]: has a high affinity for CRF receptors and is effective against diseases in which CRF is considered to be involved

    摘要翻译： 本发明的目的是提供一种抗CRF受体的拮抗剂，其作为治疗或预防药物是有效的，其涉及CRF被认为涉及的疾病，例如抑郁症，焦虑症，阿尔茨海默氏病，帕金森病，亨廷顿氏舞蹈病，进食 疾病，高血压，胃疾病，药物依赖，癫痫，脑梗塞，脑缺血，脑水肿，头部外伤，炎症，免疫相关疾病，特异性，肠易激综合征，睡眠障碍，皮肤病，精神分裂症，疼痛等。 由下式[I]表示的三氮杂 - 环戊二烯并[cd]茚衍生物：对CRF受体具有高亲和力，并且对于CRF被认为涉及的疾病有效

    (6-fluoro-1,2-benzisoxazol-3-yl)-1-piperidinyl-alkyl-(2, 9-disubstituted-4H-pyrido[1,2-a]pyrimidin-4-one) derivatives
    9.
    发明授权
    (6-fluoro-1,2-benzisoxazol-3-yl)-1-piperidinyl-alkyl-(2, 9-disubstituted-4H-pyrido[1,2-a]pyrimidin-4-one) derivatives 失效
    （6-氟-1,2-苯并异恶唑-3-基）-1-哌啶基 - 烷基 - （2,9-二取代-4H-吡啶并[1,2-a]嘧啶-4-酮）衍生物

    公开(公告)号：US5482943A

    公开(公告)日：1996-01-09

    申请号：US676681

    申请日：1991-03-28

    申请人： Ludo E. J. Kennis ,  Jan Vandenberk ,  Albertus H. M. T. Van Heertum

    发明人： Ludo E. J. Kennis ,  Jan Vandenberk ,  Albertus H. M. T. Van Heertum

    IPC分类号： A61K31/445 ,  A61K31/424 ,  A61K31/4523 ,  A61K31/505 ,  A61K31/519 ,  A61P25/18 ,  C07D471/04

    CPC分类号： C07D471/04

    摘要： Novel 2,9-disubstituted-4H-pyrido[1,2-a]pyrimidin-4-ones having the formula ##STR1## the pharmaceutically acceptable acid addition salts thereof, and the stereochemically isomeric forms thereof, whereinAlk represents C.sub.1-4 alkanediyl,D is a bicyclic heterocycle of formula ##STR2## wherein R.sup.1 represents C.sub.1-4 alkyl, hydroxyC.sub.1-4 alkyl, carboxaldehyde, carboxyl, C.sub.1-10 alkylcarbonyloxyC.sub.1-4 alkyl; each R.sup.2 represents hydrogen or C.sub.1-4 alkyl; R.sup.3 represents C.sub.1-4 alkyl, hydroxyC.sub.1-4 alkyl or methyl substituted with phenyl, 5-methyl-2-furanyl or 3-pyridinyl; and R.sup.4 represents C.sub.1-3 alkyl, phenyl, 5-methyl-2-furanyl or 3-pyridinyl.

    摘要翻译： 具有下式的新的2,9-二取代-4H-吡啶并[1,2-a]嘧啶-4-酮其（I）其药学上可接受的酸加成盐及其立体化学异构形式，其中Alk表示C1 （a）其中R 1表示C 1-4烷基，羟基C 1-4烷基，羧醛，羧基，C 1-10烷基羰基氧基C 1-4烷基，C 1-10烷基羰基氧基，C 1-4烷基， 每个R 2表示氢或C 1-4烷基; R 3表示C 1-4烷基，羟基C 1-4烷基或被苯基，5-甲基-2-呋喃基或3-吡啶基取代的甲基; R 4表示C 1-3烷基，苯基，5-甲基-2-呋喃基或3-吡啶基。