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    5-arylsulfonyl indoles useful for treating disease
    13.
    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.

    Azepino[4,5-b]pyrano[3,2-e]indoles
    14.
    发明授权
    Azepino[4,5-b]pyrano[3,2-e]indoles 失效
    氮杂[4,5-b]吡喃并[3,2-e]吲哚

    公开(公告)号：US06503899B2

    公开(公告)日：2003-01-07

    申请号：US09900508

    申请日：2001-07-06

    Applicant: Jian-min Fu

    Inventor： Jian-min Fu

    IPC: A61K3155

    CPC classification number: C07D491/14 ,  A61K31/55

    Abstract: The invention provides a compound of formula (I): wherein: R1-R5, m, n, p, and the bonds a and b represented by - - - have any of the values, specific values, or preferred values described in the specification; or a salt or solvate thereof. The invention also provides pharmaceutical compositions comprising such a compound, as well as intermediates and processes useful for preparing such a compound, and therapeutic methods including the administration of such a compound.

    Abstract translation: 本发明提供式（I）化合物：其中：R 1 -R 5，m，n，p，和由 - 表示的键a和b具有本说明书中描述的任何值，具体值或优选值 ; 或其盐或溶剂合物。 本发明还提供包含这种化合物的药物组合物，以及可用于制备这种化合物的中间体和方法，以及包括给予这种化合物的治疗方法。

    5-HT2 receptor ligands
    15.
    发明授权
    5-HT2 receptor ligands 失效
    5-HT2受体配体

    公开(公告)号：US5824676A

    公开(公告)日：1998-10-20

    申请号：US763255

    申请日：1996-12-10

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

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

    IPC: C07D243/38 ,  C07D267/20 ,  A61K31/55 ,  C07D403/04 ,  C07D413/04 ,  C07D417/04

    CPC classification number: C07D243/38 ,  C07D267/20

    Abstract: Described herein are 5-HT2 receptor-selective compounds of Formula I: ##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 is C.sub.1-6 alkyl optionally substituted with a substituent selected from OH, halo, C.sub.1-4 alkyl and C.sub.1-4 alkoxy; and R.sub.2, R.sub.3 and R.sub.4 are independently selected from H and R.sub.1 ; and acid addition salts, solvates and hydrates thereof. Their use as ligands for serotonin 5-HT2 receptor identification and in a drug screening program, and as pharmaceuticals to treat indications in which the 5-HT2 receptor is implicated, such as hypertension, thrombosis, migraine, vasospasm, ischemia, depression, anxiety, schizophrenia, sleep disorders and appetite disorders is also described.

    Abstract translation: 本文描述的是式I的5-HT 2受体选择性化合物：其中：A和B独立地选择，任选取代的饱和或不饱和的5-或6-元，均 - 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-; R1是任选被选自OH，卤素，C 1-4烷基和C 1-4烷氧基的取代基取代的C 1-6烷基; 并且R 2，R 3和R 4独立地选自H和R 1; 及其酸加成盐，溶剂化物和水合物。 它们用作5-羟色胺5-HT2受体鉴定和药物筛选程序的配体，以及用作治疗其中涉及5-HT2受体的适应症的药物，例如高血压，血栓形成，偏头痛，血管痉挛，局部缺血，抑郁，焦虑， 还描述了精神分裂症，睡眠障碍和食欲障碍。

    Benzyl-substituted compounds having dopamine receptor affinity
    16.
    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。

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