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    5-arylsulfonyl indoles useful for treating disease
    32.
    发明授权
    5-arylsulfonyl indoles useful for treating disease 失效

    公开(公告)号：US06565829B2

    公开(公告)日：2003-05-20

    申请号：US10210377

    申请日：2002-08-01

    Applicant: Jian-Min Fu

    Inventor： Jian-Min Fu

    IPC: A61K5100

    CPC classification number: C07D209/14

    Abstract: The invention provides derivatives of 5-arylsulfonyl indole and 5-arylsulfonyl indoline compounds which may be in the form of pharmaceutical acceptable salts or compositions that are useful in treating central nervous system diseases such as anxiety and depression. The invention also includes intermediates and processes to make the compounds, isotopically-labeled forms of the compounds and the use of the isotopically labeled forms of the compounds to perform nuclear magnetic resonance imaging and positron emission tomography.

    Benzyl-substituted compounds having dopamine receptor affinity
    33.
    发明授权
    Benzyl-substituted compounds having dopamine receptor affinity 失效
    具有多巴胺受体亲和力的苄基取代的化合物

    公开(公告)号：US5602120A

    公开(公告)日：1997-02-11

    申请号：US354766

    申请日：1994-12-12

    Applicant: Jian-Min Fu ,  Ashok Tehim ,  Robert A. Kirby

    Inventor： Jian-Min Fu ,  Ashok Tehim ,  Robert A. Kirby

    IPC: C07D267/20 ,  A61K31/55 ,  C07D413/04 ,  C07D417/04

    CPC classification number: C07D267/20

    Abstract: Described herein are D4 receptor-selective compounds of the general formula: ##STR1## wherein: A and B are independently selected, optionally substituted, saturated or unsaturated 5- or 6-membered, homo- or heterocyclic rings;X.sub.1 is selected from CH.sub.2, O, NH, S, C.dbd.O, CH--OH, CH--N(C.sub.1-4 alkyl).sub.2, C.dbd.CHCl, C.dbd.CHCN, N--C.sub.1-4 alkyl, N-acetyl, SO.sub.2 and SO;X.sub.2 - - - is selected from N.dbd., CH.sub.2 --, CH.dbd., C(O)--, O--, and S--;Y is selected from CH and N;Z is cyanoR.sub.1 represents C.sub.1-4 alkyl;m is 0, 1, 2 or 3;n is 0, 1 or 2;q is 1 or 2; andD is a 5, 6 or 7-membered, saturated or unsaturated, homo- or heterocyclic ring; and acid addition salts, solvates and hydrates thereof. Their use as ligands for dopamine receptor identification and in a drug screening program, and as pharmaceuticals to treat indications in which the D4 receptor is implicated, such as schizophrenia, is also described.

    Abstract translation: 本文描述的是具有以下通式的D4受体选择性化合物：其中：A和B独立选择，任选取代的饱和或不饱和的5-或6-元，杂环或杂环; X 1选自CH 2，O，NH，S，C = O，CH-OH，CH-N（C 1-4烷基）2，C = CHCl，C = CHCN，N-C 1-4烷基，N-乙酰基， 所以; X2 - - - 选自N =，CH 2 - ，CH =，C（O） - ，O-和S-; Y选自CH和N; Z是氰基，R 1表示C 1-4烷基; m为0,1,2或3; n为0,1或2; q为1或2; 且D为5,6或7元饱和或不饱和的均聚或杂环; 及其酸加成盐，溶剂化物和水合物。 还描述了它们作为多巴胺受体鉴定和药物筛选程序的配体的用途，以及用于治疗其中涉及D4受体的适应症的药物，例如精神分裂症。

    Pyrazolo[1,5-a]pyridine derivatives and their use as neurotransmitter modulators
    37.
    发明授权
    Pyrazolo[1,5-a]pyridine derivatives and their use as neurotransmitter modulators 失效
    吡唑并[1,5-a]吡啶衍生物及其作为神经递质调节剂的用途

    公开(公告)号：US07151109B2

    公开(公告)日：2006-12-19

    申请号：US10387159

    申请日：2003-03-12

    Applicant: Jian-Min Fu

    Inventor： Jian-Min Fu

    IPC: A61K31/44

    CPC classification number: C07D471/04 ,  A61K31/415

    Abstract: The present invention relates to novel pyrazolo[1,5-a]pyridine derivatives of general formula I: that bind with high affifnity to CRF1 receptors, including human CRF1 receptors. This invention also relates to methods of using the compounds of the invention to treat a disorder or condition, the treatment of which can be effected or facilitated by antagonizing a CRF receptor, such as CNS disorders or diseases, particularly anxiety disorders, and depression and stress related disorders.

    Abstract translation: 本发明涉及通式I的新的吡唑并[1,5-a]吡啶衍生物：其具有高亲和力结合CRF 1 H 1受体，包括人CRF 1受体 。 本发明还涉及使用本发明化合物治疗病症或病症的方法，其治疗可以通过拮抗CRF受体如CNS疾病或疾病，特别是焦虑症，抑郁和应激来实现或促进 相关疾病。

    SUBSTITUTED PYRIMIDINE DERIVATIVES
    38.
    发明申请
    SUBSTITUTED PYRIMIDINE DERIVATIVES 审中-公开
    取代的吡咯烷衍生物

    公开(公告)号：US20060217398A1

    公开(公告)日：2006-09-28

    申请号：US11424073

    申请日：2006-06-14

    Applicant: Jeffrey Corbett ,  Micheal Ennis ,  Kristine Frank ,  Jian-Min Fu ,  Robert Hoffman ,  Patrick Verhoest

    Inventor： Jeffrey Corbett ,  Micheal Ennis ,  Kristine Frank ,  Jian-Min Fu ,  Robert Hoffman ,  Patrick Verhoest

    IPC: A61K31/506 ,  A61K31/4439

    CPC classification number: C07D239/42 ,  C07D213/72

    Abstract: This invention relates to compounds of Formula I, a stereoisomer thereof, a pharmaceutically acceptable salt thereof, a prodrug thereof, or a pharmaceutically acceptable salt of a prodrug thereof. The compounds interact with CRF1 receptors, including human CRF1 receptors. This invention also relates to methods of using the compounds of the invention to treat a disorder or condition, the treatment of which can be effected or facilitated by antagonizing a CRF receptor, such as CNS disorders or diseases, particularly anxiety-related disorders such as anxiety, and mood disorders such as major depression.

    Abstract translation: 本发明涉及式I化合物，其立体异构体，其药学上可接受的盐，其前药或其前药的药学上可接受的盐。 这些化合物与CRF1受体（包括人CRF 1受体）相互作用。 本发明还涉及使用本发明化合物治疗病症或病症的方法，所述疾病或病症的治疗可以通过拮抗CRF受体如CNS疾病或疾病，特别是焦虑相关疾病例如焦虑来实现或促进 ，以及心理障碍如重度抑郁症。

    Substituted pyrimidine derivatives
    39.
    发明授权
    Substituted pyrimidine derivatives 失效
    取代的嘧啶衍生物

    公开(公告)号：US07087617B2

    公开(公告)日：2006-08-08

    申请号：US10839055

    申请日：2004-05-05

    Applicant: Jeffrey W. Corbett ,  Michael Dalton Ennis ,  Kristine E. Frank ,  Jian-Min Fu ,  Robert Louis Hoffman ,  Patrick R. Verhoest

    Inventor： Jeffrey W. Corbett ,  Michael Dalton Ennis ,  Kristine E. Frank ,  Jian-Min Fu ,  Robert Louis Hoffman ,  Patrick R. Verhoest

    IPC: A61K31/505 ,  C07D239/32

    CPC classification number: C07D239/42 ,  C07D213/72

    Abstract: This invention relates to compounds of Formula I, a stereoisomer thereof, a pharmaceutically acceptable salt thereof, a prodrug thereof, or a pharmaceutically acceptable salt of a prodrug thereof. The compounds interact with CRF1 receptors, including human CRF1 receptors. This invention also relates to methods of using the compounds of the invention to treat a disorder or condition, the treatment of which can be effected or facilitated by antagonizing a CRF receptor, such as CNS disorders or diseases, particularly anxiety-related disorders such as anxiety, and mood disorders such as major depression.

    Abstract translation: 本发明涉及式I化合物，其立体异构体，其药学上可接受的盐，其前药或其前药的药学上可接受的盐。 这些化合物与CRF1受体（包括人CRF 1受体）相互作用。 本发明还涉及使用本发明化合物治疗病症或病症的方法，所述疾病或病症的治疗可以通过拮抗CRF受体如CNS疾病或疾病，特别是焦虑相关疾病例如焦虑来实现或促进 ，以及心理障碍如重度抑郁症。

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