公开(公告)号：US07919484B2

公开(公告)日：2011-04-05

申请号：US11815739

申请日：2006-02-08

Applicant: Rajender Kamboj ,  Michael D. Winther ,  Robert Fraser ,  Mikhail Chafeev ,  Sultan Chowdhury ,  Jian-Min Fu ,  Duanjie Hou ,  Shifeng Liu ,  Vandna Raina ,  Mehran Seid Bagherzadeh ,  Serguei Sviridov ,  Kashinath Sadalapure ,  Shaoyi Sun ,  Vishnumurthy Kodumuru ,  Nagasree Chakka ,  Zaihui Zhang ,  Melwyn Abreo ,  Mikhail A. Kondratenko ,  Daniel F. Harvey ,  Cindy J. Hudson ,  Wenbao Li ,  Chi Tu ,  Sengen Sun ,  Mark W. Holladay ,  Heinz W. Gschwend

Inventor： Rajender Kamboj ,  Michael D. Winther ,  Robert Fraser ,  Mikhail Chafeev ,  Sultan Chowdhury ,  Jian-Min Fu ,  Duanjie Hou ,  Shifeng Liu ,  Vandna Raina ,  Mehran Seid Bagherzadeh ,  Serguei Sviridov ,  Kashinath Sadalapure ,  Shaoyi Sun ,  Vishnumurthy Kodumuru ,  Nagasree Chakka ,  Zaihui Zhang ,  Melwyn Abreo ,  Mikhail A. Kondratenko ,  Daniel F. Harvey ,  Cindy J. Hudson ,  Wenbao Li ,  Chi Tu ,  Sengen Sun ,  Mark W. Holladay ,  Heinz W. Gschwend

IPC: A61K31/501 ,  C07D211/34

CPC classification number: A61K31/64 ,  A61K31/00 ,  A61K31/4439 ,  A61K38/28 ,  A61K45/06 ,  A61K2300/00

Abstract: This invention is directed to the use of SCD-1 inhibitors of the formula (I): where x, y, V, W, G, J, L, M, R2, R3, R5, R5a, R6, R6a, R7, R7a, R8 and R8a are defined herein, in combination with other drug therapies to treat adverse weight gain.

Abstract translation: 本发明涉及式（I）的SCD-1抑制剂的用途：其中x，y，V，W，G，J，L，M，R2，R3，R5，R5a，R6，R6a，R7， 本文定义R7a，R8和R8a与其他药物治疗组合以治疗不利的体重增加。

公开(公告)号：US07335658B2

公开(公告)日：2008-02-26

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 D Winther ,  Zaihui Zhang ,  Melwyn Abreo ,  Mark W Holladay ,  Wenbao Li ,  Sengen Sun ,  Chi Tu ,  Heinz W 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 D Winther ,  Zaihui Zhang ,  Melwyn Abreo ,  Mark W Holladay ,  Wenbao Li ,  Sengen Sun ,  Chi Tu ,  Heinz W Gschwend

IPC: C07D403/04 ,  C07D403/14 ,  A61K31/497

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 6，R 4， R 6a，R 7，R 7a，R 8，R 8a，R 8，R 7， 本文定义了9和9和9 9。 还公开了包含式（I）化合物的药物组合物。

公开(公告)号：US20080015230A1

公开(公告)日：2008-01-17

申请号：US11575638

申请日：2005-09-20

Applicant: Rajender Kamboj ,  Zaihui Zhang ,  Jian-Min Fu ,  Mehran Seid Bagherzadeh ,  Serguei Sviridov ,  Sultan Chowdhury ,  Shifeng Liu ,  Vishnumurthy Kodumuru

Inventor： Rajender Kamboj ,  Zaihui Zhang ,  Jian-Min Fu ,  Mehran Seid Bagherzadeh ,  Serguei Sviridov ,  Sultan Chowdhury ,  Shifeng Liu ,  Vishnumurthy Kodumuru

IPC: A61K31/44 ,  A61P3/00 ,  A61P3/04 ,  A61P3/10 ,  C07D213/00 ,  C07D401/02

CPC classification number: C07D213/82

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 y, G, K, L, M, W, V, R2, R3, R4, 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y，G，K，L，M， W，V，R 2，R 3，R 4，R 6，R 6a， R 7，R 7，R 8，R 8和R 8 8a在本文中定义。 还公开了包含式（I）化合物的药物组合物。

公开(公告)号：US07151109B2

公开(公告)日：2006-12-19

申请号：US10387159

申请日：2003-03-12

Applicant: Jian-Min Fu

Inventor： Jian-Min Fu

IPC: A61K31/44

CPC classification number: C07D471/04 ,  A61K31/415

Abstract: The present invention relates to novel pyrazolo[1,5-a]pyridine derivatives of general formula I: 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.

Abstract translation: 本发明涉及通式I的新的吡唑并[1,5-a]吡啶衍生物：其具有高亲和力结合CRF 1 H 1受体，包括人CRF 1受体 。 本发明还涉及使用本发明化合物治疗病症或病症的方法，其治疗可以通过拮抗CRF受体如CNS疾病或疾病，特别是焦虑症，抑郁和应激来实现或促进 相关疾病。

公开(公告)号：US20060217398A1

公开(公告)日：2006-09-28

申请号：US11424073

申请日：2006-06-14

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

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

IPC: A61K31/506 ,  A61K31/4439

CPC classification number: C07D239/42 ,  C07D213/72

Abstract: This invention relates to compounds of Formula I, a stereoisomer thereof, a pharmaceutically acceptable salt thereof, a prodrug thereof, or a pharmaceutically acceptable salt of a prodrug thereof. The compounds interact with 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-related disorders such as anxiety, and mood disorders such as major depression.

Abstract translation: 本发明涉及式I化合物，其立体异构体，其药学上可接受的盐，其前药或其前药的药学上可接受的盐。 这些化合物与CRF1受体（包括人CRF 1受体）相互作用。 本发明还涉及使用本发明化合物治疗病症或病症的方法，所述疾病或病症的治疗可以通过拮抗CRF受体如CNS疾病或疾病，特别是焦虑相关疾病例如焦虑来实现或促进 ，以及心理障碍如重度抑郁症。

公开(公告)号：US07087617B2

公开(公告)日：2006-08-08

申请号：US10839055

申请日：2004-05-05

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: A61K31/505 ,  C07D239/32

CPC classification number: C07D239/42 ,  C07D213/72

Abstract: This invention relates to compounds of Formula I, a stereoisomer thereof, a pharmaceutically acceptable salt thereof, a prodrug thereof, or a pharmaceutically acceptable salt of a prodrug thereof. The compounds interact with 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-related disorders such as anxiety, and mood disorders such as major depression.

Abstract translation: 本发明涉及式I化合物，其立体异构体，其药学上可接受的盐，其前药或其前药的药学上可接受的盐。 这些化合物与CRF1受体（包括人CRF 1受体）相互作用。 本发明还涉及使用本发明化合物治疗病症或病症的方法，所述疾病或病症的治疗可以通过拮抗CRF受体如CNS疾病或疾病，特别是焦虑相关疾病例如焦虑来实现或促进 ，以及心理障碍如重度抑郁症。

公开(公告)号：US07041672B2

公开(公告)日：2006-05-09

申请号：US10844004

申请日：2004-05-12

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

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

IPC: A61K31/4965 ,  C07D401/00 ,  C07D403/00 ,  C07D405/00 ,  C07D409/00

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 pyrazine derivatives of the formula I as defined herein, and their use in treating anxiety disorders, depression and stress related disorders are disclosed.

Abstract translation: 公开了本文定义的式I的取代的芳基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：US06930105B2

公开(公告)日：2005-08-16

申请号：US10271349

申请日：2002-10-15

Applicant: Jian-Min Fu

Inventor： Jian-Min Fu

IPC: A61K31/5383 ,  A61K31/554 ,  A61K51/00 ,  A61P3/04 ,  A61P25/00 ,  A61P25/22 ,  A61P25/24 ,  C07D498/22 ,  C07D513/22 ,  C07D265/28

CPC classification number: C07D498/22 ,  C07D513/22

Abstract: The present invention provides compounds of Formula (I): wherein R1, R2, R3, R4, R5, and R6, 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-HT2C 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 5和R 6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。 该化合物是5-HT配体，并且可用于治疗需要调节5-HT 2C活性的疾病。

公开(公告)号：US20050101613A1

公开(公告)日：2005-05-12

申请号：US10839055

申请日：2004-05-05

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

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

IPC: C07D213/72 ,  C07D239/42 ,  A61K31/506 ,  A61K31/4439 ,  C07D43/02

CPC classification number: C07D239/42 ,  C07D213/72

Abstract: This invention relates to compounds of Formula I, a stereoisomer thereof, a pharmaceutically acceptable salt thereof, a prodrug thereof, or a pharmaceutically acceptable salt of a prodrug thereof. The compounds interact with CRF, receptors, including human CRF, 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-related disorders such as anxiety, and mood disorders such as major depression.

Abstract translation: 本发明涉及式I化合物，其立体异构体，其药学上可接受的盐，其前药或其前药的药学上可接受的盐。 该化合物与CRF，受体（包括人类CRF）受体相互作用。 本发明还涉及使用本发明化合物治疗病症或病症的方法，所述疾病或病症的治疗可以通过拮抗CRF受体如CNS疾病或疾病，特别是焦虑相关疾病例如焦虑来实现或促进 ，以及心理障碍如重度抑郁症。

公开(公告)号：US06465495B1

公开(公告)日：2002-10-15

申请号：US09363877

申请日：1999-07-29

Applicant: Arlindo L. Castelhano ,  Jian-Min Fu

Inventor： Arlindo L. Castelhano ,  Jian-Min Fu

IPC: C07D21302

CPC classification number: C07D213/64 ,  A61K31/4412 ,  A61K31/675 ,  C07D409/04 ,  C07F9/58 ,  C07F9/59

Abstract: Novel pyridone mimetics are disclosed which are useful for the treatment of SH2 domain related diseases.

Abstract translation: 公开了可用于治疗SH2结构域相关疾病的新型吡啶酮模拟物。