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21. 发明申请

US20050038040A1 Compounds as CRF1 receptor antagonists 失效
标题翻译：化合物作为CRF1受体拮抗剂
公开(公告)号：US20050038040A1
公开(公告)日：2005-02-17
申请号：US10840485
申请日：2004-05-06
申请人： Jeffrey Corbett , Michael Ennis , Kristine Frank , Jian-Min Fu , Robert Hoffman , Patrick Verhoest
发明人： Jeffrey Corbett , Michael Ennis , Kristine Frank , Jian-Min Fu , Robert Hoffman , Patrick Verhoest
IPC分类号： A61P25/00 , C07D401/14 , C07D403/14 , C07D417/14 , A61K31/497 , C07D43/14
CPC分类号： C07D401/14 , C07D403/14 , C07D417/14
摘要： The present invention relates to compounds of Formula I, or a stereoisomer thereof, a pharmaceutically acceptable salt thereof, or a prodrug thereof. The compounds of the inventions are CRF1 receptor antagonists. Compounds of the invention are useful for treating, in a warm-blooded animal, particularly a mammal, and more particularly a human, various disorders that are associated with CRF or CRF1 receptors, or disorders the treatment of which can be effected or facilitated by antagonizing CRF1 receptors.
摘要翻译：本发明涉及式I化合物或其立体异构体，其药学上可接受的盐或其前药。本发明的化合物是CRF1受体拮抗剂。本发明的化合物可用于在温血动物特别是哺乳动物中治疗，特别是治疗与CRF或CRF1受体相关的各种疾病，或其治疗可通过拮抗作用或促进 CRF1受体。

22. 发明授权

US5700445A N-methyl piperazine compounds having dopamine receptor affinity 失效
标题翻译：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
申请人： Jian-Min Fu , Sumanas Rakhit
发明人： Jian-Min Fu , Sumanas Rakhit
IPC分类号： C07D243/38 , C07D267/18 , C07D337/14 , A61K51/00 , A61M36/14
CPC分类号： C07D267/18 , C07D243/38 , C07D337/14
摘要： 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.
摘要翻译：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。

23. 发明授权

US5602121A Alkyl-substituted compounds having dopamine receptor affinity 失效
标题翻译：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
申请人： Jian-Min Fu
发明人： Jian-Min Fu
IPC分类号： C07D267/20 , A61K31/55 , C07D413/04 , C07D417/04
CPC分类号： C07D267/20
摘要： 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.
摘要翻译：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。

24. 发明授权

US5538965A Dopamine receptor ligands 失效
标题翻译：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
申请人： Ashok Tehim , Jian-Min Fu , Sumanas Rakhit
发明人： Ashok Tehim , Jian-Min Fu , Sumanas Rakhit
IPC分类号： 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分类号： C07D405/12 , C07D409/12 , C07D413/12 , C07D417/12
摘要： 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.
摘要翻译：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。

25. 发明申请

US20080207587A1 Pyridazine Derivatives for Inhibiting Human Stearoyl-Coa-Desaturase 失效
标题翻译：用于抑制人类硬脂酰辅酶脱氢酶的哒嗪衍生物
公开(公告)号：US20080207587A1
公开(公告)日：2008-08-28
申请号：US11575642
申请日：2005-09-20
申请人： Rajender Kamboj , Zaihui Zhang , Jian-Min Fu , Serguei Sviridov , Sultan Chowdhury , Vishnumurthy Kodumuru
发明人： Rajender Kamboj , Zaihui Zhang , Jian-Min Fu , Serguei Sviridov , Sultan Chowdhury , Vishnumurthy Kodumuru
IPC分类号： A61K31/501 , C07D237/06 , C07D403/02 , A61P3/00 , A61P3/04 , A61P3/10 , C07D401/02
CPC分类号： C07D401/12 , A61K31/501 , C07D237/24 , C07D403/12
摘要： 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, Q, W, V, R2, R3, R5, R5a, R6, R6a, R7, R7a, R8 and R8a arc defined herein. Pharmaceutical compositions comprising the compounds of formula (I) are also disclosed.
摘要翻译：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，Q，W，V，R2，R3，R5，R5a，R6，R6a，R7，R7a，R8和R8a。还公开了包含式（I）化合物的药物组合物。

26. 发明申请

US20070219211A1 Bicyclic Heterocyclic Derivatives and Their Use as Inhibitors of Stearoyl-Coadesaturase (Scd) 失效
标题翻译：双环杂环衍生物及其作为硬脂酰辅酶S（STD）抑制剂的用途
公开(公告)号：US20070219211A1
公开(公告)日：2007-09-20
申请号：US11575643
申请日：2005-09-20
申请人： Rajender Kamboj , Jian-Min Fu , Vishnumurthy Kodumuru , Shifeng Liu , Kashinath Sadalapure , Nagasree Chakka , Duanjie Hou , Shaoyi Sun
发明人： Rajender Kamboj , Jian-Min Fu , Vishnumurthy Kodumuru , Shifeng Liu , Kashinath Sadalapure , Nagasree Chakka , Duanjie Hou , Shaoyi Sun
IPC分类号： A61K31/50 , A61K31/497 , C07D403/00 , C12N9/99
CPC分类号： A61K31/497 , A61K31/50 , C07D235/08 , C07D487/04
摘要： Methods of treating an SCD-mediated disease or condition in a mammal, preferably a human, are disclosed, wherein the methods comprise, for example, administering to a mammal in need thereof a compound of formula (I): where x, y, J, K, L, M, W, V, R2, R3, R5, R5a, R6, R6a, R7, R7a, R8 and R8a are defined herein. Pharmaceutical compositions comprising the compounds of formula (I) are also disclosed.
摘要翻译：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，其中所述方法包括例如向有需要的哺乳动物施用式（I）化合物：其中x，y，J ，K，L，M，W，V，R 2，R 3，R 5，R 5a， R 6，R 6a，R 7，R 7a，R 8，和R 8a是本文定义的。还公开了包含式（I）化合物的药物组合物。

27. 发明授权

US07022694B2 Indoles and indolines having 5-HT activity 失效
标题翻译：具有5-HT活性的吲哚和中间体
公开(公告)号：US07022694B2
公开(公告)日：2006-04-04
申请号：US10192918
申请日：2002-07-11
申请人： Jian-Min Fu , Jeanette Kay Morris , Arthur Glenn Romero
发明人： Jian-Min Fu , Jeanette Kay Morris , Arthur Glenn Romero
IPC分类号： A61P25/00 , A61K31/55 , C07D487/00
CPC分类号： C07D487/04
摘要： The present invention provides compounds of Formula (I): wherein R1, R2, R3, R4, R5, R6 and --- 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 useful as 5-HT ligands.
摘要翻译：本发明提供式（I）的化合物：其中R 1，R 2，R 3，R 4， >，R 5，R 6和 - 具有说明书中定义的任何值，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。该化合物可用作5-HT配体。

28. 发明申请

US20050119251A1 Nicotinamide derivatives and their use as therapeutic agents 审中-公开
标题翻译：烟酰胺衍生物及其作为治疗剂的用途
公开(公告)号：US20050119251A1
公开(公告)日：2005-06-02
申请号：US10885901
申请日：2004-07-06
申请人： Jian-Min Fu , Vishnumurthy Kodumuru , Shaoyi Sun , Michael Winther , Richard Fine , Daniel Harvey , Boris Klebansky , Mark Gray-Keller , Heinz Gschwend , Wenbao Li
发明人： Jian-Min Fu , Vishnumurthy Kodumuru , Shaoyi Sun , Michael Winther , Richard Fine , Daniel Harvey , Boris Klebansky , Mark Gray-Keller , Heinz Gschwend , Wenbao Li
IPC分类号： A61K31/496 , A61K31/551
CPC分类号： A61K31/496 , A61K31/551 , Y02A50/387
摘要： 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 m, n, p, V, R1, R2, R3, R4, R5 and R6 are defined herein. Pharmaceutical compositions comprising the compounds of formula (I) are also disclosed.
摘要翻译：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m，n，p，V，R ，R2，R3，R4，R5和R6如本文所定义。还公开了包含式（I）化合物的药物组合物。

29. 发明申请

US20050065143A1 Pyridazine derivatives and their use as therapeutic agents 有权
标题翻译：哒嗪衍生物及其作为治疗剂的用途
公开(公告)号：US20050065143A1
公开(公告)日：2005-03-24
申请号：US10901563
申请日：2004-07-29
申请人： Nagasree Chakka , Mikhail Chafeev , Sultan Chowdhury , Jian-Min Fu , Duanjie Hou , Rajender Kamboj , Vishnumurthy Kodumuru , Shifeng Liu , Vandna Raina , Shaoyi Sun , Serguei Sviridov , Michael Winther , Zaihui Zhang , Melwyn Abreo , Mark Holladay , Wenbao Li , Sengen Sun , Chi Tu , Heinz Gschwend
发明人： Nagasree Chakka , Mikhail Chafeev , Sultan Chowdhury , Jian-Min Fu , Duanjie Hou , Rajender Kamboj , Vishnumurthy Kodumuru , Shifeng Liu , Vandna Raina , Shaoyi Sun , Serguei Sviridov , Michael Winther , Zaihui Zhang , Melwyn Abreo , Mark Holladay , Wenbao Li , Sengen Sun , Chi Tu , Heinz Gschwend
IPC分类号： A61K31/00 , A61K31/501 , A61K31/551 , A61P3/06 , C07D237/20 , C07D237/24
CPC分类号： A61K31/00 , A61K31/501 , A61K31/551 , C07D237/20 , C07D237/24
摘要： 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, W, V, R2, R3, R4, R5, R6, R6a, R7, R7a, R8, R8a, R9 and R9a are defined herein. Pharmaceutical compositions comprising the compounds of formula (I) are also disclosed.
摘要翻译：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，W，V，R R 2，R 3，R 4，R 5，R 6，R 6a，R 7，R 7a，R 8，R 8a，R 本文定义<9>和R 9a。还公开了包含式（I）化合物的药物组合物。

30. 发明申请

US20050049257A1 Substituted aryl 1, 4-pyrazine derivatives 失效
标题翻译：取代的芳基1,4-吡嗪衍生物
公开(公告)号：US20050049257A1
公开(公告)日：2005-03-03
申请号：US10844004
申请日：2004-05-12
申请人： Patrick Verhoest , Jeffrey Corbett , Michael Ennis , Kristine Frank , Jian-Min Fu , Robert Hoffman
发明人： Patrick Verhoest , Jeffrey Corbett , Michael Ennis , Kristine Frank , Jian-Min Fu , Robert Hoffman
IPC分类号： C07D241/18 , C07D241/20 , C07D241/26 , C07D401/04 , C07D401/12 , C07D401/14 , C07D403/12 , C07D405/12 , C07D409/12 , C07D491/04 , G01N33/74 , A61K31/4965 , C07D43/02
CPC分类号： C07D241/18 , C07D241/20 , C07D241/26 , C07D401/04 , C07D401/12 , C07D401/14 , C07D403/12 , C07D405/12 , C07D409/12 , C07D491/04 , G01N33/74 , G01N2333/5751 , G01N2500/02 , Y10S206/828
摘要： Substituted aryl 1,4-pyrazine derivatives and their use in treating anxiety disorders, depression and stress related disorders are disclosed.
摘要翻译：公开了取代的芳基1,4-吡嗪衍生物及其在治疗焦虑症，抑郁症和应激相关疾病中的用途。

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