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    N-methyl piperazine compounds having dopamine receptor affinity
    32.
    发明授权
    N-methyl piperazine compounds having dopamine receptor affinity 失效
    具有多巴胺受体亲和力的N-甲基哌嗪化合物

    公开(公告)号：US5700445A

    公开(公告)日：1997-12-23

    申请号：US354905

    申请日：1994-12-12

    Applicant: Jian-Min Fu ,  Sumanas Rakhit

    Inventor： Jian-Min Fu ,  Sumanas Rakhit

    IPC: C07D243/38 ,  C07D267/18 ,  C07D337/14 ,  A61K51/00 ,  A61M36/14

    CPC classification number: C07D267/18 ,  C07D243/38 ,  C07D337/14

    Abstract: Described herein are D4 receptor-selective compounds of the general formula: ##STR1## wherein X.sub.1 is selected from CH.sub.2, NH, O and S; X.sub.2 - - is selected from CH.dbd., CH.sub.2 13 , and N.dbd.; R.sub.1 to R.sub.8 are each independently selected from H, C.sub.1-4 alkyl, halo, cyano, nitro and halo-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X 1选自CH 2，NH，O和S; X2 + E，uns - + EE选自CH =，CH213和N =; R 1至R 8各自独立地选自H，C 1-4烷基，卤素，氰基，硝基和卤素取代的C 1-4烷基及其酸加成盐，溶剂合物和水合物。 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，如精神分裂症。

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

    公开(公告)号：US5602121A

    公开(公告)日：1997-02-11

    申请号：US354793

    申请日：1994-12-12

    Applicant: Jian-Min Fu

    Inventor： Jian-Min Fu

    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 N and CH;R.sub.1 represents C.sub.1-4 alkyl;n is 0, 1 or 2;q is 1 or 2; andZ is C.sub.5-10 alkyl optionally substituted with OH, halo, C.sub.1-4 alkyl or C.sub.1-4 alkoxy and optionally incorporating a heteroatom selected from O, N and S;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N和CH; R 1表示C 1-4烷基; n为0,1或2; q为1或2; 并且Z是任选地被OH，卤素，C 1-4烷基或C 1-4烷氧基取代并任选地引入选自O，N和S的杂原子的C 5-10-10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。

    Dopamine receptor ligands
    34.
    发明授权
    Dopamine receptor ligands 失效
    多巴胺受体配体

    公开(公告)号：US5538965A

    公开(公告)日：1996-07-23

    申请号：US355297

    申请日：1994-12-12

    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 ,  C07D413/14 ,  C07D417/14

    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; andE 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-; R1表示C1-4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。

    Therapeutic compounds
    36.
    发明授权
    Therapeutic compounds 失效
    治疗化合物

    公开(公告)号：US07291738B2

    公开(公告)日：2007-11-06

    申请号：US10375687

    申请日：2003-02-27

    Applicant: Jian-Min Fu

    Inventor： Jian-Min Fu

    IPC: C07D215/38

    CPC classification number: C07D401/14 ,  C07D213/65 ,  C07D487/04

    Abstract: The present invention provides compounds, for example, of formula (I): wherein R1, R2, and R3 have any of the values defined in the specification, as well as pharmaceutical compositions comprising the compounds. The invention also provides therapeutic methods, and processes and intermediates useful for preparing compounds of formula I.

    Abstract translation: 本发明提供了化合物，例如式（I）化合物：其中R 1，R 2，R 3和R 3具有 本说明书中定义的值，以及包含该化合物的药物组合物。 本发明还提供了可用于制备式I化合物的治疗方法，方法和中间体。

    Pyrrolo[1,2-b]pyridazine compounds and their uses
    37.
    发明授权
    Pyrrolo[1,2-b]pyridazine compounds and their uses 失效
    吡咯并[1,2-b]哒嗪化合物及其用途

    公开(公告)号：US07074791B2

    公开(公告)日：2006-07-11

    申请号：US10682691

    申请日：2003-10-09

    Applicant: Jian-Min Fu

    Inventor： Jian-Min Fu

    IPC: C07D487/04 ,  A61K31/5025 ,  A61P25/22 ,  A61P25/24

    CPC classification number: C07D487/04

    Abstract: Disclosed are novel CRF receptor antagonists and their use as treatment of a variety of disorders, including disorders manifesting hypersecretion of CRF or associated with CRF or CRF receptors, such as anxiety, and depression. CRF receptor antagonists of the invention have the structure of formula (I): including stereoisomers or mixture of stereoisomers, pharmaceutically acceptable prodrugs, or pharmaceutically acceptable salts thereof, wherein in formula (I) R1 and R2 are independently selected from H, Me or OMe.

    Abstract translation: 公开了新的CRF受体拮抗剂及其用于治疗多种疾病的用途，包括表现出CRF过度分泌或与CRF或CRF受体如焦虑和抑郁症相关的疾病。 本发明的CRF受体拮抗剂具有式（I）的结构：包括立体异构体或立体异构体的混合物，药学上可接受的前药或其药学上可接受的盐，其中在式（I）中R 1和R 2， SUP> 2 独立地选自H，Me或OMe。

    Pyrrolo[1,2-B]pyridazine compounds and their uses
    38.
    发明授权
    Pyrrolo[1,2-B]pyridazine compounds and their uses 失效
    吡咯并[1,2-B]哒嗪化合物及其用途

    公开(公告)号：US07034023B2

    公开(公告)日：2006-04-25

    申请号：US10799404

    申请日：2004-03-12

    Applicant: Jian-min Fu

    Inventor： Jian-min Fu

    IPC: C07D487/04 ,  A61K31/5025 ,  A61P25/22 ,  A61P25/24

    CPC classification number: C07D487/04

    Abstract: Disclosed are novel CRF receptor antagonists and their use as treatment of a variety of disorders, including disorders manifesting hypersecretion of CRF or associated with CRF or CRF receptors, such as anxiety, and depression. CRF receptor antagonists of the invention have the structure of formula (I): including stereoisomers or mixture of stereoisomers, pharmaceutically acceptable prodrugs, or pharmaceutically acceptable salts thereof, wherein in formula (I) R is H or Me.

    Abstract translation: 公开了新的CRF受体拮抗剂及其用于治疗多种疾病的用途，包括表现出CRF过度分泌或与CRF或CRF受体如焦虑和抑郁症相关的疾病。 本发明的CRF受体拮抗剂具有式（I）的结构：包括立体异构体或立体异构体的混合物，药学上可接受的前药或其药学上可接受的盐，其中在式（I）中R是H或Me。

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