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116 条记录 (耗时 0.012 秒)

    TRIAZA-CYCLOPENTA[CD]INDENE DERIVATIVES
    41.
    发明申请
    TRIAZA-CYCLOPENTA[CD]INDENE DERIVATIVES 审中-公开
    四环素衍生物[CD] INDENE DERIVATIVES

    公开(公告)号：WO2005066178A1

    公开(公告)日：2005-07-21

    申请号：PCT/JP2005/000323

    申请日：2005-01-06

    申请人： TAISHO PHARMACEUTICAL CO., LTD. ,  NAKAZATO, Atsuro ,  OKUBO, Taketoshi ,  NOZAWA, Dai ,  TAMITA, Tomoko ,  KENNIS, Ludo, E.J.

    发明人： NAKAZATO, Atsuro ,  OKUBO, Taketoshi ,  NOZAWA, Dai ,  TAMITA, Tomoko ,  KENNIS, Ludo, E.J.

    IPC分类号： C07D487/16

    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，阿尔茨海默病，帕金森病，亨廷顿舞蹈病，饮食 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。

    PYRIDO- AND PYRIMIDOPYRIMIDINE DERIVATIVES AS ANTI- PROLIFERATIVE AGENTS
    43.
    发明申请
    PYRIDO- AND PYRIMIDOPYRIMIDINE DERIVATIVES AS ANTI- PROLIFERATIVE AGENTS 审中-公开
    作为抗增生剂的吡咯并吡啶并吡啶衍生物

    公开(公告)号：WO2005058913A1

    公开(公告)日：2005-06-30

    申请号：PCT/EP2004/053501

    申请日：2004-12-15

    申请人： JANSSEN PHARMACEUTICA N.V. ,  FREYNE, Eddy, Jean, Edgard ,  WILLEMS, Marc ,  STORCK, Pierre, Henri ,  PONCELET, Virginie, Sophie ,  VAN EMELEN, Kristof ,  BUIJNSTERS, Peter, Jacobus, Johannes, Antonius ,  EMBRECHTS, Werner, Constant, Johan ,  PERERA, Timothy, Pietro, Suren

    发明人： FREYNE, Eddy, Jean, Edgard ,  WILLEMS, Marc ,  STORCK, Pierre, Henri ,  PONCELET, Virginie, Sophie ,  VAN EMELEN, Kristof ,  BUIJNSTERS, Peter, Jacobus, Johannes, Antonius ,  EMBRECHTS, Werner, Constant, Johan ,  PERERA, Timothy, Pietro, Suren

    IPC分类号： C07D498/18

    CPC分类号： C07D498/16 ,  C07D471/04 ,  C07D487/04 ,  C07D487/16 ,  C07D487/22

    摘要： The present invention concerns the compounds of formula (I) the N -oxide forms, the pharmaceutically acceptable addition salts and the stereochemically isomeric forms thereof, wherein a 1 -a 2 =a 3 -a 4 represents a divalent radical selected from N-CH=CH-CH, N-CH N-CH or CH-CH=N-CH; Z represents NH; Y represents -C 3-9 alkyl-, -C l-5 alkyl-NR 13 -C l-5 alkyl-,-C 1 - 6 alkyl-NH-CO- or -CO-NH -C 1-6 alkyl- ; X 1 represents -O- or -NR 11 -; X 2 represents -C 1-2 alkyl-, -O-C 1-2 alkyl, -O- or -O-CH 2 -;R 1 represents hydrogen or halo; R 2 represents hydrogen, cyano, halo, hydroxycarbonyl-C l-4 alkyloxycarbonyl-, Het 16 -carbonyl- or Ar 5 ; R 3 represents hydrogen; R 4 represents hydroxy, C 1-4 alkyloxy-, Ar 4 -C 1-4 alkyloxy or R 4 represents C l-4 alkyloxy substituted with one or where possible two or more substituents selected from C 1-4 alkyloxy- or Het 2 -; R 11 represents hydrogen; R 12 represents hydrogen, C l-4 alkyl- or C l-4 alkyl-oxy-carbonyl-; R 13 represents Het 14 -C l-4 alkyl, in particular morpholinyl-C l-4 alkyl; Het 2 represents a heterocycle selected from morpholinyl or piperidinyl optionally substituted with C 1-4 alkyl-, preferably methyl; Het 14 represents morpholinyl; Het 16 represents a heterocycle selected from morpholinyl or pyrrolidinyl; Ar 4 represents phenyl; Ar 5 represents phenyl optionally substituted with cyano.

    摘要翻译： 本发明涉及式（I）化合物的N-氧化物形式，其药学上可接受的加成盐和立体化学异构形式，其中a 1 -a 2 = a 3 -a 4表示 选自N-CH = CH-CH，N-CHN-CH或CH-CH = N-CH的二价基团; Z表示NH; Y表示-C3-9烷基 - ， - C1-5烷基-NR13-C1-5烷基 - ，C1-6烷基-NH-CO-或-CO-NH-C 1-6烷基 - ; X 1表示-O-或-NR 11 - ; X 2表示-C 1-2烷基 - ， - O-C 1-2烷基，-O-或-O-CH 2 - ; R 1表示氢或卤素; R 2代表氢，氰基，卤素，羟基羰基-C 1-4烷基氧基羰基，Het 16 - 羰基 - 或Ar 5。 R 3表示氢; R 4表示羟基，C 1-4烷氧基 - ，Ar 4 -C 1-4烷氧基或R 4表示被一个或多个可能的两个或多个选自C 1-4烷氧基或Het 2的取代基取代的C 1-4烷氧基。 - ; R 11表示氢; R 12表示氢，C 1-4烷基 - 或C 1-4烷基 - 氧 - 羰基 - ; R 13代表Het 14 -Cl-4烷基，特别是吗啉基-C 1-4烷基; Het 2表示选自被C 1-4烷基，优选甲基取代的吗啉基或哌啶基的杂环; Het <14>代表吗啉基; Het 16表示选自吗啉基或吡咯烷基的杂环; Ar 4表示苯基; Ar 5表示任选被氰基取代的苯基。

    TRICYCLIC CRF RECEPTOR ANTAGONISTS
    44.
    发明申请
    TRICYCLIC CRF RECEPTOR ANTAGONISTS 审中-公开
    TRICYCLIC CRF受体拮抗剂

    公开(公告)号：WO2002064592A1

    公开(公告)日：2002-08-22

    申请号：PCT/US2001/049906

    申请日：2001-12-21

    申请人： NEUROCRINE BIOSCIENCES, INC. ,  HADDACH, Mustapha

    发明人： HADDACH, Mustapha

    IPC分类号： C07D471/16

    CPC分类号： C07D471/16 ,  A61K31/53 ,  C07D487/16

    摘要： CRF receptor antagonists are disclosed which have utility in the treatment of a variety of disorders, including the treatment of disorders manifesting hypersecretion of CRF in a warm-blooded animals, such as stroke. The CRF receptor antagonists of this invention have the following structure: including stereoisomers, prodrugs and pharmaceutically acceptable salts thereof, wherein R1, R2, R5, R6, X and Y are as defined herein. Compositions containing a CRF receptor antagonist in combination with a pharmaceutically acceptable carrier are also disclosed, as well as methods for use of the same.

    摘要翻译： 公开了CRF受体拮抗剂，其可用于治疗各种疾病，包括治疗在温血动物（例如中风）中表现出CRF过度分泌的病症。 本发明的CRF受体拮抗剂具有以下结构：包括其立体异构体，前药和药学上可接受的盐，其中R 1，R 2，R 5，R 6，X和Y如本文所定义。 还公开了含有CRF受体拮抗剂与药学上可接受的载体的组合物，以及其用途的方法。

    CYTOTOXIC ALKALOID DERIVATIVES INCLUDING ASMARINE A AND B ISOLATED FROM A SPONGE
    46.
    发明申请
    CYTOTOXIC ALKALOID DERIVATIVES INCLUDING ASMARINE A AND B ISOLATED FROM A SPONGE 审中-公开
    细胞毒素碱性衍生物，包括从海绵中分离的阿斯马林A和B

    公开(公告)号：WO99033832A1

    公开(公告)日：1999-07-08

    申请号：PCT/GB1998/003884

    申请日：1998-12-23

    IPC分类号： A61K31/52 ,  A61K31/551 ,  A61P35/00 ,  C07D487/16 ,  C07D487/06 ,  A61K31/505

    CPC分类号： C07D487/16

    摘要： Asmarine A and B, novel cytotoxic diterpene-alkaloids, have been isolated from the sponge Raspailia sp. The structure of these compounds have been established on the basis of NMR data and confirmed by X-ray analysis. Also claimed are compounds (I) or (II), wherein R represents hydrogen or lower alkyl or lower alkanoyl; R represents hydrogen or lower alkyl; R is either an alkyl or a cycloalkyl group containing one or more isopreneunits, or a monoterpene or a sesquiterpene or a sesquiterpene or a diterpene group; R or R represent hydrogen or lower alkyl; R represents lower alkyl; X represents F or Cl or Br or (I).

    摘要翻译： Asmarine A和B，新型细胞毒二萜生物碱已从海绵Raspailia sp。 这些化合物的结构已经建立在NMR数据的基础上，并通过X射线分析证实。 还要求的是化合物（I）或（II），其中R 1表示氢或低级烷基或低级烷酰基; R 2表示氢或低级烷基; R 3是含有一个或多个异戊二烯单元或单萜或倍半萜烯或倍半萜烯或二萜烯基团的烷基或环烷基; R 4或R 5表示氢或低级烷基; R 6表示低级烷基; X表示F或Cl或Br或（I）。