公开(公告)号：US07998995B2

公开(公告)日：2011-08-16

申请号：US12517800

申请日：2007-12-07

Applicant: Brant Clayton Boren ,  Brett B. Busch ,  Xiao-Hui Gu ,  Vasu Jammalamadaka ,  Shao Po Lu ,  Richard Martin ,  Raju Mohan ,  Edwin Schweiger ,  William C. Stevens ,  Tie-Lin Wang ,  Yinong Xie ,  Wei Xu

Inventor： Brant Clayton Boren ,  Brett B. Busch ,  Xiao-Hui Gu ,  Vasu Jammalamadaka ,  Shao Po Lu ,  Richard Martin ,  Raju Mohan ,  Edwin Schweiger ,  William C. Stevens ,  Tie-Lin Wang ,  Yinong Xie ,  Wei Xu

IPC: A61K31/4178 ,  A61K31/4164 ,  C07D233/56 ,  C07D233/58 ,  C07D233/66 ,  C07D233/64

CPC classification number: C07D233/90 ,  C07D231/10

Abstract: Compounds of the invention are disclosed, such as compounds of formulae LX-LXIV, and pharmaceutically acceptable salts, isomers, or prodrugs thereof, which are useful as modulators of the activity of liver X receptors (LXR) and Farnesoid X receptors (FXR), where R00, R200, R400, R500, J11, J21, G1, G21, and Q are defined herein. Pharmaceutical compositions containing the compounds and methods of using the compounds are also disclosed.

Abstract translation: 公开了本发明的化合物，例如式LX-LXIV的化合物及其药学上可接受的盐，异构体或前药，其可用作肝脏X受体（LXR）和法尼斯X受体（FXR）的活性的调节剂， 其中R00，R200，R400，R500，J11，J21，G1，G21和Q在本文中定义。 还公开了含有化合物的药物组合物和使用该化合物的方法。

公开(公告)号：US20100075964A1

公开(公告)日：2010-03-25

申请号：US11993529

申请日：2006-06-26

Applicant: Brett B. Busch ,  Brenton T. Flatt ,  Xiao-Hui Gu ,  Shao-Po Lu ,  Richard Martin ,  Raju Mohan ,  Michael Charles Nyman ,  Edwin Schweiger ,  William C. Stevens, Jr. ,  Tie-Lin Wang ,  Yinong Xie

Inventor： Brett B. Busch ,  Brenton T. Flatt ,  Xiao-Hui Gu ,  Shao-Po Lu ,  Richard Martin ,  Raju Mohan ,  Michael Charles Nyman ,  Edwin Schweiger ,  William C. Stevens, Jr. ,  Tie-Lin Wang ,  Yinong Xie

IPC: A61K31/5377 ,  C07D233/54 ,  A61K31/4164 ,  C07D401/14 ,  A61K31/4439 ,  A61K31/496 ,  C07D413/14 ,  A61P3/06 ,  A61P9/00 ,  A61P25/00 ,  A61P35/00

CPC classification number: C07D233/64 ,  C07D231/12 ,  C07D231/22 ,  C07D233/90 ,  C07D401/04 ,  C07D401/10 ,  C07D401/12 ,  C07D401/14 ,  C07D403/04 ,  C07D403/10 ,  C07D403/12 ,  C07D403/14 ,  C07D405/10 ,  C07D405/12 ,  C07D405/14 ,  C07D409/04 ,  C07D409/10 ,  C07D409/12 ,  C07D409/14 ,  C07D413/12 ,  C07D417/10 ,  C07D417/12 ,  C07D417/14 ,  C07D487/08

Abstract: Compounds of the invention, such as compounds of Formulae IIa, IIb, IIc or IId, and pharmaceutically acceptable salts, isomers, and prodrugs thereof, are useful as modulators of the activity of liver X receptors, where R1, R2, R21, R3 and G are defined herein. Pharmaceutical compositions containing the compounds and methods of using the compounds are also disclosed.

Abstract translation: 本发明的化合物，例如式IIa，IIb，IIc或IId的化合物及其药学上可接受的盐，异构体和前药可用作肝脏X受体活性的调节剂，其中R1，R2，R21，R3和 G在本文中定义。 还公开了含有化合物的药物组合物和使用该化合物的方法。

公开(公告)号：US20090326218A1

公开(公告)日：2009-12-31

申请号：US12362269

申请日：2009-01-29

Applicant: Richard Martin ,  Tie-Lin Wang ,  Brenton T. Flatt ,  Xiao-Hui Gu ,  Ronald Griffith

Inventor： Richard Martin ,  Tie-Lin Wang ,  Brenton T. Flatt ,  Xiao-Hui Gu ,  Ronald Griffith

IPC: C07D487/04 ,  C07D487/20

CPC classification number: C07D471/04 ,  C07D487/10 ,  C07D491/04

Abstract: Compounds, compositions and methods for modulating the activity of receptors are provided. In particular compounds and compositions are provided for modulating the activity of receptors and for the treatment, prevention, or amelioration of one or more symptoms of disease or disorder directly or indirectly related to the activity of the receptors.

Abstract translation: 提供了调节受体活性的化合物，组合物和方法。 特别地提供化合物和组合物用于调节受体的活性和用于治疗，预防或改善与受体活性直接或间接相关的疾病或病症的一种或多种症状。

公开(公告)号：US07485634B2

公开(公告)日：2009-02-03

申请号：US10447302

申请日：2003-05-27

Applicant: Richard Martin ,  Tie-Lin Wang ,  Brenton T Flatt ,  Xiao-Hui Gu ,  Ronald Griffith

Inventor： Richard Martin ,  Tie-Lin Wang ,  Brenton T Flatt ,  Xiao-Hui Gu ,  Ronald Griffith

IPC: A61P3/00 ,  A61K31/55 ,  C07D487/04

CPC classification number: C07D471/04 ,  C07D487/10 ,  C07D491/04

Abstract: Compounds, compositions and methods for modulating the activity of receptors are provided. In particular compounds and compositions are provided for modulating the activity of receptors and for the treatment, prevention, or amelioration of one or more symptoms of disease or disorder directly or indirectly related to the activity of the receptors.

Abstract translation: 提供了调节受体活性的化合物，组合物和方法。 特别地提供化合物和组合物用于调节受体的活性和用于治疗，预防或改善与受体活性直接或间接相关的疾病或病症的一种或多种症状。

公开(公告)号：US07291628B2

公开(公告)日：2007-11-06

申请号：US11029247

申请日：2005-01-04

Applicant: John L. Neumeyer ,  Jean M. Bidlack ,  Xiao-Hui Gu

Inventor： John L. Neumeyer ,  Jean M. Bidlack ,  Xiao-Hui Gu

IPC: A61K31/485

CPC classification number: C07D221/28 ,  A61K31/485 ,  A61K51/0455

Abstract: The invention is based in part on the discovery that nonselective κ agonists that possess μ receptor-mediated effects in addition to their κ agonist effects can decrease cocaine self-administration more effectively and with fewer undesirable side effects than can highly selective κ agonists. The invention includes a number of new compounds having both nonselective κ opioid receptor agonist activity and additional activity at μ opioid receptors. These compounds are useful for the treatment of cocaine abuse, and can also be radiolabeled for use as imaging agents, e.g., the N-fluoroalkyl and iodoalkyl derivatives can be used, respectively, for positron emission tomography (PET) and single photon computed tomography (SPECT) brain imaging.

Abstract translation: 本发明部分地基于以下发现：除了κ受体介导的作用以外，除了其kappa激动剂效应之外，非选择性κ激动剂可以比高选择性κ激动剂更有效地减少可卡因自身给药并且具有更少的不希望的副作用。 本发明包括许多具有非选择性κ阿片受体激动剂活性和在阿片样物质受体的另外活性的新化合物。 这些化合物可用于治疗可卡因滥用，并且也可以放射性标记用作成像剂，例如，N-氟烷基和碘代烷基衍生物可分别用于正电子发射断层摄影（PET）和单光子计算机断层摄影（ SPECT）脑成像。

公开(公告)号：US20070015746A1

公开(公告)日：2007-01-18

申请号：US10565702

申请日：2004-07-23

Applicant: Richard Martin ,  Tie-Lin Wang ,  Brenton Flatt ,  Xiao-Hui Gu

Inventor： Richard Martin ,  Tie-Lin Wang ,  Brenton Flatt ,  Xiao-Hui Gu

IPC: A61K31/55 ,  C07D498/02 ,  C07D491/02 ,  C07D487/02

CPC classification number: C07D495/04 ,  C07D487/04

Abstract: Compounds, compositions and methods are provided for modulating the activity of receptors and for the treatment, prevention, or amelioration of one or more symptoms of disease or disorder related to the activity of the receptors.

Abstract translation: 提供化合物，组合物和方法用于调节受体的活性和用于治疗，预防或改善与受体活性相关的疾病或病症的一种或多种症状。

公开(公告)号：US20050054634A1

公开(公告)日：2005-03-10

申请号：US10895431

申请日：2003-12-02

Applicant: Brett Busch ,  Brenton Flatt ,  Xiao-Hui Gu ,  Richard Martin ,  Raju Mohan ,  Tie-Lin Wang ,  Jason Wu

Inventor： Brett Busch ,  Brenton Flatt ,  Xiao-Hui Gu ,  Richard Martin ,  Raju Mohan ,  Tie-Lin Wang ,  Jason Wu

IPC: A61K31/435 ,  A61K31/55 ,  C07D471/04 ,  C07D487/04 ,  C07D487/10 ,  C07D491/04 ,  C07D491/20 ,  C07D487/02

CPC classification number: C07D487/04 ,  C07D471/04 ,  C07D487/10 ,  C07D491/04

Abstract: Compounds, compositions and methods for modulating the activity of receptors are provided. In particular, compounds and compositions are provided for modulating the activity of receptors and for the treatment, prevention, or amelioration of one or more symptoms of disease or disorder directly or indirectly related to the activity of the receptors.

Abstract translation: 提供了调节受体活性的化合物，组合物和方法。 特别地，提供了化合物和组合物用于调节受体的活性和用于治疗，预防或改善与受体活性直接或间接相关的疾病或病症的一种或多种症状。