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    Therapeutic 5-HT ligand compounds
    21.
    发明授权
    Therapeutic 5-HT ligand compounds 失效
    治疗性5-HT配体化合物

    公开(公告)号：US06887868B2

    公开(公告)日：2005-05-03

    申请号：US10247756

    申请日：2002-09-19

    Applicant: Jian-Min Fu

    Inventor： Jian-Min Fu

    IPC: A61K31/5383 ,  A61K51/00 ,  A61P3/04 ,  A61P25/00 ,  A61P25/06 ,  A61P25/08 ,  A61P25/18 ,  A61P25/20 ,  A61P25/22 ,  A61P25/24 ,  A61P25/28 ,  A61P25/30 ,  A61P43/00 ,  C07D498/06 ,  C07D491/06 ,  A61K31/542 ,  C07D487/06

    CPC classification number: C07D498/06

    Abstract: The present invention provides compounds of Formula (I): wherein: R1, R2, R3, R4, R5, R6 R7, R8, n, m, and X have any of the values defined in the specification, as well as pharmaceutical compositions comprising the compounds. The invention also provides therapeutic methods as well as processes and intermediates useful for preparing compounds of Formula (I). The compounds are 5-HT ligands and are useful for treating diseases wherein modulation of 5-HT activity is desired.

    Abstract translation: 本发明提供式（I）的化合物：其中：R 1，R 2，R 3，R 4， R S，R 5，R 6，R 7，R 8，N，m和X具有任何 的说明书中定义的值，以及包含该化合物的药物组合物。 本发明还提供治疗方法以及可用于制备式（I）化合物的方法和中间体。 该化合物是5-HT配体，并且可用于治疗其中需要调节5-HT活性的疾病。

    Arylsulphonyl substituted-tetrahydro- and hexahydro-carbazoles
    23.
    发明授权
    Arylsulphonyl substituted-tetrahydro- and hexahydro-carbazoles 失效
    芳基磺酰基取代的四氢 - 咔唑

    公开(公告)号：US06727274B2

    公开(公告)日：2004-04-27

    申请号：US10268627

    申请日：2002-10-08

    Applicant: Jian-Min Fu

    Inventor： Jian-Min Fu

    IPC: C07D20982

    CPC classification number: C07D209/88

    Abstract: The invention provides compounds of formula I for use in treating conditions in which 5-HT6 receptors are involved such as in anxiety, depression, schizophrenia, Alzheimer's disease, stress-related disease, panic, a phobia, obsessive compulsive disorder, obesity, post-traumatic stress syndrome, epilepsy, and other CNS disorders.

    Abstract translation: 本发明提供式I化合物，其用于治疗其中涉及5-HT 6受体的病症，例如焦虑，抑郁，精神分裂症，阿尔茨海默病，紧张相关疾病，恐慌症，恐惧症，强迫症，肥胖症， 创伤性应激综合征，癫痫和其他CNS疾病。

    Alkyl-substituted compounds having dopamine receptor affinity
    25.
    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：US5834459A

    公开(公告)日：1998-11-10

    申请号：US754014

    申请日：1996-04-01

    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, 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. and C(O); 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; and Z 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 D4 receptor stimulation 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，任选取代的不饱和5-或6-元，同 - 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 =，CH2-，CH =和C（O）; 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受体刺激的适应症的药物，例如精神分裂症。

    Heterocyclic Derivatives and Their Use as Stearoyl-Coa Desaturase Inhibitors
    27.
    发明申请
    Heterocyclic Derivatives and Their Use as Stearoyl-Coa Desaturase Inhibitors 失效
    杂环衍生物及其作为硬脂酰辅酶A去饱和酶抑制剂的用途

    公开(公告)号：US20080096895A1

    公开(公告)日：2008-04-24

    申请号：US11575640

    申请日：2005-09-20

    Applicant: Rajender Kamboj ,  Zaihui Zhang ,  Jian-Min Fu

    Inventor： Rajender Kamboj ,  Zaihui Zhang ,  Jian-Min Fu

    IPC: A61K31/496 ,  A61K31/497 ,  A61P1/16 ,  A61P3/04 ,  A61P3/10 ,  C07D401/14 ,  C07D403/14 ,  C12N9/99

    CPC classification number: A61K31/496 ,  A61K31/501

    Abstract: Methods of treating an SCD-mediated disease or condition in a mammal, preferably a human, are disclosed, wherein the methods comprise administering to a mammal in need thereof a compound of formula (I): where x, y, G, J, K, L, M, V R2, R3, R4, R5, R5a, R6, R6a, R7, R7a, R8 and R8a are defined herein. Pharmaceutical compositions comprising the compounds of formula (I) are also disclosed.

    Abstract translation: 公开了在哺乳动物，优选人中治疗SCD介导的疾病或病症的方法，其中所述方法包括向有需要的哺乳动物施用式（I）化合物：其中x，y，G，J，K ，L，M，VR 2，R 3，R 4，R 5，R 5a R 6，R 6，R 6，R 7，R 7a，R 8， ＆lt; 8a＆gt;和＆lt; 8a＆gt;在本文中定义。 还公开了包含式（I）化合物的药物组合物。

    Pyrrolo[1,2b]pyridazine compounds and their uses
    28.
    发明申请
    Pyrrolo[1,2b]pyridazine compounds and their uses 审中-公开
    吡咯并[1,2b]哒嗪化合物及其用途

    公开(公告)号：US20070224636A1

    公开(公告)日：2007-09-27

    申请号：US11388418

    申请日：2006-03-24

    Applicant: Jian-min Fu

    Inventor： Jian-min Fu

    IPC: G01N33/53 ,  A61K31/502

    CPC classification number: G01N33/948 ,  A61K31/502 ,  G01N2500/02 ,  G01N2800/301

    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。

    Pyrrolo[1,2b]pyridazine compounds and their uses
    29.
    发明申请
    Pyrrolo[1,2b]pyridazine compounds and their uses 审中-公开
    吡咯并[1,2b]哒嗪化合物及其用途

    公开(公告)号：US20060148807A1

    公开(公告)日：2006-07-06

    申请号：US11378537

    申请日：2006-03-17

    Applicant: Jian-min Fu

    Inventor： Jian-min Fu

    IPC: A61K31/503 ,  G01N33/53

    CPC classification number: A61K31/503 ,  G01N33/566 ,  G01N2500/00

    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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