公开(公告)号：US20080207587A1

公开(公告)日：2008-08-28

申请号：US11575642

申请日：2005-09-20

Applicant: Rajender Kamboj ,  Zaihui Zhang ,  Jian-Min Fu ,  Serguei Sviridov ,  Sultan Chowdhury ,  Vishnumurthy Kodumuru

Inventor： Rajender Kamboj ,  Zaihui Zhang ,  Jian-Min Fu ,  Serguei Sviridov ,  Sultan Chowdhury ,  Vishnumurthy Kodumuru

IPC: A61K31/501 ,  C07D237/06 ,  C07D403/02 ,  A61P3/00 ,  A61P3/04 ,  A61P3/10 ,  C07D401/02

CPC classification number: C07D401/12 ,  A61K31/501 ,  C07D237/24 ,  C07D403/12

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, 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.

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，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。

公开(公告)号：US20070219211A1

公开(公告)日：2007-09-20

申请号：US11575643

申请日：2005-09-20

Applicant: Rajender Kamboj ,  Jian-Min Fu ,  Vishnumurthy Kodumuru ,  Shifeng Liu ,  Kashinath Sadalapure ,  Nagasree Chakka ,  Duanjie Hou ,  Shaoyi Sun

Inventor： Rajender Kamboj ,  Jian-Min Fu ,  Vishnumurthy Kodumuru ,  Shifeng Liu ,  Kashinath Sadalapure ,  Nagasree Chakka ,  Duanjie Hou ,  Shaoyi Sun

IPC: A61K31/50 ,  A61K31/497 ,  C07D403/00 ,  C12N9/99

CPC classification number: A61K31/497 ,  A61K31/50 ,  C07D235/08 ,  C07D487/04

Abstract: 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.

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。

公开(公告)号：US07022694B2

公开(公告)日：2006-04-04

申请号：US10192918

申请日：2002-07-11

Applicant: Jian-Min Fu ,  Jeanette Kay Morris ,  Arthur Glenn Romero

Inventor： Jian-Min Fu ,  Jeanette Kay Morris ,  Arthur Glenn Romero

IPC: A61P25/00 ,  A61K31/55 ,  C07D487/00

CPC classification number: C07D487/04

Abstract: 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.

Abstract translation: 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。

公开(公告)号：US07015229B2

公开(公告)日：2006-03-21

申请号：US10370259

申请日：2003-02-20

Applicant: Jian-Min Fu ,  Jeffrey W. Corbett ,  Michael Dalton Ennis ,  Kristine E. Frank ,  Robert Louis Hoffman ,  Patrick R. Verhoest

Inventor： Jian-Min Fu ,  Jeffrey W. Corbett ,  Michael Dalton Ennis ,  Kristine E. Frank ,  Robert Louis Hoffman ,  Patrick R. Verhoest

IPC: C07D239/46 ,  C07D401/04 ,  C07D403/12 ,  A61K31/506

CPC classification number: C07D239/47 ,  C07D401/04 ,  C07D401/14 ,  C07D403/12 ,  C07D417/14 ,  G01N2333/726

Abstract: This invention relates to substituted pyrimidinone and pyrimidithione derivatives that bind with high affifnity to CRF1 receptors, including human CRF1 receptors. This invention also relates to methods of using the compounds of the invention to treat a disorder or condition, the treatment of which can be effected or facilitated by antagonizing a CRF receptor, such as CNS disorders or diseases, particularly anxiety disorders, and depression and stress related disorders.

公开(公告)号：US06964965B2

公开(公告)日：2005-11-15

申请号：US10417867

申请日：2003-04-17

Applicant: Jeffrey W. Corbett ,  Michael Dalton Ennis ,  Kristine E. Frank ,  Jian-Min Fu ,  Robert Louis Hoffman ,  Patrick R. Verhoest

Inventor： Jeffrey W. Corbett ,  Michael Dalton Ennis ,  Kristine E. Frank ,  Jian-Min Fu ,  Robert Louis Hoffman ,  Patrick R. Verhoest

IPC: G01N33/50 ,  A61K31/4965 ,  A61K31/497 ,  A61P1/00 ,  A61P1/14 ,  A61P3/04 ,  A61P3/08 ,  A61P5/00 ,  A61P7/12 ,  A61P9/00 ,  A61P11/06 ,  A61P15/08 ,  A61P17/00 ,  A61P17/06 ,  A61P17/14 ,  A61P21/00 ,  A61P25/00 ,  A61P25/04 ,  A61P25/06 ,  A61P25/08 ,  A61P25/20 ,  A61P25/22 ,  A61P25/24 ,  A61P25/28 ,  A61P25/32 ,  A61P25/34 ,  A61P25/36 ,  A61P29/00 ,  A61P31/18 ,  A61P35/00 ,  A61P37/06 ,  A61P37/08 ,  A61P43/00 ,  C07D241/20 ,  C07D403/12 ,  C12Q1/02 ,  G01N33/15 ,  C07D401/00 ,  C07D403/00 ,  C07D405/00

CPC classification number: C07D403/12 ,  C07D241/20 ,  Y10S206/828

Abstract: The present invention provides substituted pyrazine derivatives of Formula I, that are CRF1 receptor antagonists, including human CRF1 receptors. This invention also relates to use of compounds of the invention for treating a disorder or condition, the treatment of which can be effected or facilitated by antagonizing a CRF receptor, such as CNS disorders, particularly anxiety-related disorders and mood disorders.

Abstract translation: 本发明提供式I的取代吡嗪衍生物，其为CRF 1受体拮抗剂，包括人CRF 1受体。 本发明还涉及本发明化合物用于治疗病症或病症的用途，所述疾病或病症的治疗可以通过拮抗CRF受体（例如CNS病症，特别是焦虑相关疾病和情绪障碍）来实现或促进。

公开(公告)号：US20050119251A1

公开(公告)日：2005-06-02

申请号：US10885901

申请日：2004-07-06

Applicant: Jian-Min Fu ,  Vishnumurthy Kodumuru ,  Shaoyi Sun ,  Michael Winther ,  Richard Fine ,  Daniel Harvey ,  Boris Klebansky ,  Mark Gray-Keller ,  Heinz Gschwend ,  Wenbao Li

Inventor： Jian-Min Fu ,  Vishnumurthy Kodumuru ,  Shaoyi Sun ,  Michael Winther ,  Richard Fine ,  Daniel Harvey ,  Boris Klebansky ,  Mark Gray-Keller ,  Heinz Gschwend ,  Wenbao Li

IPC: A61K31/496 ,  A61K31/551

CPC classification number: A61K31/496 ,  A61K31/551 ,  Y02A50/387

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 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.

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。

公开(公告)号：US20050065143A1

公开(公告)日：2005-03-24

申请号：US10901563

申请日：2004-07-29

Applicant: 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

Inventor： 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: A61K31/00 ,  A61K31/501 ,  A61K31/551 ,  A61P3/06 ,  C07D237/20 ,  C07D237/24

CPC classification number: A61K31/00 ,  A61K31/501 ,  A61K31/551 ,  C07D237/20 ,  C07D237/24

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, 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.

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，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。

公开(公告)号：US20050049257A1

公开(公告)日：2005-03-03

申请号：US10844004

申请日：2004-05-12

Applicant: Patrick Verhoest ,  Jeffrey Corbett ,  Michael Ennis ,  Kristine Frank ,  Jian-Min Fu ,  Robert Hoffman

Inventor： Patrick Verhoest ,  Jeffrey Corbett ,  Michael Ennis ,  Kristine Frank ,  Jian-Min Fu ,  Robert Hoffman

IPC: 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 classification number: 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

Abstract: Substituted aryl 1,4-pyrazine derivatives and their use in treating anxiety disorders, depression and stress related disorders are disclosed.

Abstract translation: 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。

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.

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。