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    Troponyl piperazines as dopamine D4 receptor ligands
    44.
    发明授权
    Troponyl piperazines as dopamine D4 receptor ligands 失效
    托膦酰基哌嗪作为多巴胺D4受体配体

    公开(公告)号：US5998414A

    公开(公告)日：1999-12-07

    申请号：US907672

    申请日：1997-08-08

    Applicant: Xin Wang ,  Jian-min Fu ,  Adi M. Treasurywala

    Inventor： Xin Wang ,  Jian-min Fu ,  Adi M. Treasurywala

    IPC: C07D243/38 ,  C07D295/116 ,  C07D317/58 ,  C07D409/12 ,  A61K31/495 ,  C07D295/155 ,  C07D405/06

    CPC classification number: C07D295/116 ,  C07D243/38 ,  C07D317/58 ,  C07D409/12

    Abstract: Described herein are compounds of the general formula: ##STR1## a stereoisomer, solvate, or pharmaceutically acceptable salt thereof, wherein:R.sub.1 is H, halo, aryl or aryl substituted with one or two groups independently selected from halo, C.sub.1-4 alkyl, C.sub.1-4 -alkoxy, nitro, trifluoromethyl, trifluoromethoxy or cyano;R.sub.2 is C.sub.4-9 alkyl; phenyl or phenyl substituted with one or two groups selected independently from OH, cyano, halo, C.sub.1-4 alkoxy, C.sub.1-4 alkyl, trifluoromethyl, trifluoromethoxy, nitro or phenyl; naphthyl;phenyl fused to a 5 or 6-membered heterocycle; the coumarin moiety ##STR2## wherein R.sub.3 and R.sub.4 are selected independently from H, C.sub.1-4 alkyl and C.sub.1-4 alkoxy;or 1,2-methylenedioxy phenyl;with the proviso that R.sub.2 is not phenyl or 3,4-dimethoxyphenyl when R.sub.1 is H.Also described is their use as pharmaceuticals to treat indications in which the D4 receptor is implicated, such as schizophrenia and anxiety.

    Abstract translation: 本文描述的是下列通式的化合物：其立体异构体，溶剂化物或其药学上可接受的盐，其中：R 1是被一个或两个独立地选自卤素，C 1-4烷基，C 1-4 - 烷氧基，硝基，三氟甲基，三氟甲氧基或氰基; R2是C4-9烷基; 苯基或被一个或两个独立地选自OH，氰基，卤素，C 1-4烷氧基，C 1-4烷基，三氟甲基，三氟甲氧基，硝基或苯基的基取代的苯基; 萘基; 与5或6元杂环稠合的苯基; 香豆素部分，其中R 3和R 4独立地选自H，C 1-4烷基和C 1-4烷氧基; 或1,2-亚甲二氧基苯基; 条件是当R 1为H时，R 2不是苯基或3,4-二甲氧基苯基。还描述了它们作为药物治疗其中涉及D4受体的适应症的用途，例如精神分裂症和焦虑症。

    Dopamine receptor ligands
    45.
    发明授权
    Dopamine receptor ligands 失效
    多巴胺受体配体

    公开(公告)号：US5798350A

    公开(公告)日：1998-08-25

    申请号：US642264

    申请日：1996-05-03

    Applicant: Ashok Tehim ,  Jian-Min Fu ,  Sumanas Rakhit

    Inventor： Ashok Tehim ,  Jian-Min Fu ,  Sumanas Rakhit

    IPC: A61K31/00 ,  A61K31/55 ,  A61P25/18 ,  A61P25/20 ,  C07D243/10 ,  C07D405/12 ,  C07D409/12 ,  C07D413/12 ,  C07D417/12 ,  C07D487/12 ,  C07D491/00 ,  A61K31/495 ,  A61K31/435 ,  C07D401/14 ,  C07D403/14

    CPC classification number: C07D405/12 ,  C07D409/12 ,  C07D413/12 ,  C07D417/12

    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--; R.sub.1 represents C.sub.1-4 alkyl; Y is selected from CH and N; n is 0, 1 or 2; q is 1 or 2; R.sub.2 is C.sub.1-6 alkyl optionally incorporating a heteroatom selected from N, O and S; D is cyclohexane or benzene; and E is a saturated or unsaturated 5- or 6-membered heterocycle incorporating 1, 2 or 3 heteroatoms selected from O, N, and S, wherein E is optionally substituted with 1 or 2 substituents selected from halogen, C.sub.1-4 alkyl and halogen-substituted C.sub.1-4 alkyl; 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-; R 1表示C 1-4烷基; Y选自CH和N; n为0,1或2; q为1或2; R2是任选地加入选自N，O和S的杂原子的C 1-6烷基; D是环己烷或苯; 并且E是掺杂有1,2或3个选自O，N和S的杂原子的饱和或不饱和的5-或6-元杂环，其中E任选被1或2个选自卤素，C 1-4烷基和卤素 - 取代的C 1-4烷基; 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
    49.
    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
    50.
    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。

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