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    Arylsulphonyl substituted-tetrahydro- and hexahydro-carbazoles
    12.
    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
    13.
    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
    15.
    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。

    N-methyl piperazine compounds having dopamine receptor affinity
    18.
    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
    19.
    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
    20.
    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。

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