公开(公告)号：US07858639B2

公开(公告)日：2010-12-28

申请号：US12609436

申请日：2009-10-30

Applicant: Chongqing Sun ,  Yanting Huang ,  Doree F. Sitkoff ,  Taekyu Lee ,  William R. Ewing

Inventor： Chongqing Sun ,  Yanting Huang ,  Doree F. Sitkoff ,  Taekyu Lee ,  William R. Ewing

IPC: C07D471/04 ,  A61K31/437

CPC classification number: C07D471/04 ,  C07D487/04

Abstract: The present application describes compounds according to Formula I, pharmaceutical compositions comprising at least one compound according to Formula I and optionally one or more additional therapeutic agents and methods of treatment using the compounds according to Formula I both alone and in combination with one or more additional therapeutic agents. The compounds have the following general formula: including all prodrugs, solvates, pharmaceutically acceptable salts and stereoisomers, wherein A, B, R1, R2, R3 and R8 are described herein.

Abstract translation: 本申请描述了根据式I的化合物，包含至少一种根据式I的化合物和任选的一种或多种另外的治疗剂的药物组合物和使用根据式I的化合物的治疗方法，其单独和与一种或多种另外的 治疗剂。 该化合物具有以下通式：包括所有前药，溶剂化物，药学上可接受的盐和立体异构体，其中A，B，R 1，R 2，R 3和R 8在本文中描述。

公开(公告)号：US20100048612A1

公开(公告)日：2010-02-25

申请号：US12609436

申请日：2009-10-30

Applicant: Chongqing Sun ,  Yanting Huang ,  Doree F. Sitkoff ,  Taekyu Lee ,  William Ewing

Inventor： Chongqing Sun ,  Yanting Huang ,  Doree F. Sitkoff ,  Taekyu Lee ,  William Ewing

IPC: A61K31/437 ,  C07D471/04

CPC classification number: C07D471/04 ,  C07D487/04

Abstract: The present application describes compounds according to Formula I, pharmaceutical compositions comprising at least one compound according to Formula I and optionally one or more additional therapeutic agents and methods of treatment using the compounds according to Formula I both alone and in combination with one or more additional therapeutic agents. The compounds have the following general formula: including all prodrugs, solvates, pharmaceutically acceptable salts and stereoisomers, wherein A, B, R1, R2, R3 and R8 are described herein.

Abstract translation: 本申请描述了根据式I的化合物，包含至少一种根据式I的化合物和任选的一种或多种另外的治疗剂的药物组合物和使用根据式I的化合物的治疗方法，其单独和与一种或多种另外的 治疗剂。 该化合物具有以下通式：包括所有前药，溶剂化物，药学上可接受的盐和立体异构体，其中A，B，R 1，R 2，R 3和R 8在本文中描述。

公开(公告)号：US20080194625A1

公开(公告)日：2008-08-14

申请号：US12108616

申请日：2008-04-24

Applicant: Chongqing Sun ,  Doree Sitkoff ,  William R. Ewing ,  Yanting Huang ,  Bruce A. Ellsworth ,  Richard B. Sulsky ,  Annapurna Pendri ,  Samuel Gerritz ,  Natesan Murugesan ,  Zhengxiang Gu

Inventor： Chongqing Sun ,  Doree Sitkoff ,  William R. Ewing ,  Yanting Huang ,  Bruce A. Ellsworth ,  Richard B. Sulsky ,  Annapurna Pendri ,  Samuel Gerritz ,  Natesan Murugesan ,  Zhengxiang Gu

IPC: A61K31/47 ,  C07D215/38 ,  A61P25/34 ,  A61P3/04

CPC classification number: C07D417/06 ,  C07D215/38 ,  C07D215/48 ,  C07D401/04 ,  C07D401/06 ,  C07D401/12 ,  C07D405/06 ,  C07D409/04 ,  C07D409/06 ,  C07D409/12 ,  C07D409/14 ,  C07D413/12 ,  C07D413/14 ,  C07D417/12

Abstract: The invention provides for compounds of formula I wherein the substitutents are as described herein. Further provided are methods of using such compounds for the treatment of eating disorders, metabolic disorders, obesity, cognitive disorders, neurological disorders, pain disorders, inflammation disorders, in the promotion of smoking cessation and for the treatment of other psychiatric disorders Also provided are pharmaceutical compositions containing such compounds and pharmaceutical combinations of the compounds of the invention with other therapeutic agents.

Abstract translation: 本发明提供式I化合物，其中取代基如本文所述。 还提供了使用这些化合物治疗进食障碍，代谢紊乱，肥胖症，认知障碍，神经障碍，疼痛障碍，炎症障碍，促进戒烟和治疗其他精神疾病的方法。 还提供含有这些化合物的药物组合物和本发明化合物与其它治疗剂的药物组合。

公开(公告)号：US07361766B2

公开(公告)日：2008-04-22

申请号：US11330656

申请日：2006-01-12

Applicant: Chongqing Sun ,  William R. Ewing ,  Yanting Huang ,  Yeheng Zhu

Inventor： Chongqing Sun ,  William R. Ewing ,  Yanting Huang ,  Yeheng Zhu

IPC: C07D471/02

CPC classification number: C07D471/04 ,  C07D487/04 ,  C07D513/04

Abstract: The present application describes compounds according to Formula I, pharmaceutical compositions comprising at least one compound according to Formula I and optionally one or more additional therapeutic agents and methods of treatment using the compounds according to Formula I both alone and in combination with one or more additional therapeutic agents. The compounds have the general Formula I: including all prodrugs, pharmaceutically acceptable salts and stereoisomers, R1, R2, R3, R3a, R4, A, B, b, n, W, X, Y and Z are described herein.

Abstract translation: 本申请描述了根据式I的化合物，包含至少一种根据式I的化合物和任选的一种或多种另外的治疗剂的药物组合物和使用根据式I的化合物的治疗方法，其单独和与一种或多种另外的 治疗剂。 该化合物具有通式I：包括所有前药，药学上可接受的盐和立体异构体，R 1，R 2，R 3，R 3， 本文描述了SUP，3a，R 4，A，B，b，n，W，X​​，Y和Z。

公开(公告)号：US07317012B2

公开(公告)日：2008-01-08

申请号：US11455045

申请日：2006-06-16

Applicant: Chongqing Sun ,  Yanting Huang ,  Doree F. Sitkoff ,  Guixue Yu ,  Amarendra Mikkilineni ,  William R. Ewing

Inventor： Chongqing Sun ,  Yanting Huang ,  Doree F. Sitkoff ,  Guixue Yu ,  Amarendra Mikkilineni ,  William R. Ewing

IPC: C07D487/04 ,  A61K31/53 ,  A61P3/04 ,  A61P43/00

CPC classification number: C07D487/04

Abstract: The present application describes compounds according to Formula I, pharmaceutical compositions comprising at least one compound according to Formula I and optionally one or more additional therapeutic agents and methods of treatment using the compounds according to Formulas I both alone and in combination with one or more additional therapeutic agents. The compounds have the following general formulas: including all prodrugs, solvates, pharmaceutically acceptable salts and stereoisomers, wherein B, R1, R2, R3 and x are described herein.

Abstract translation: 本申请描述了根据式I的化合物，包含至少一种根据式I的化合物和任选的一种或多种另外的治疗剂的药物组合物和使用根据式I的化合物单独治疗并与一种或多种另外的组合的治疗方法 治疗剂。 该化合物具有以下通式：包括所有前药，溶剂化物，药学上可接受的盐和立体异构体，其中B，R 1，R 2，R 3， SUP>和x。

公开(公告)号：US09346852B2

公开(公告)日：2016-05-24

申请号：US14005018

申请日：2012-03-13

Applicant: Chongqing Sun ,  William R. Ewing ,  Scott A. Bolton ,  Zhengxiang Gu ,  Yanting Huang ,  Natesan Murugesan ,  Yeheng Zhu

Inventor： Chongqing Sun ,  William R. Ewing ,  Scott A. Bolton ,  Zhengxiang Gu ,  Yanting Huang ,  Natesan Murugesan ,  Yeheng Zhu

IPC: C07D471/04 ,  C07D487/04 ,  C07D495/04 ,  C07K5/078 ,  A61K45/06 ,  A61K31/554 ,  A61K38/05 ,  C07D513/04 ,  C07D519/00

CPC classification number: C07K5/06139 ,  A61K31/554 ,  A61K38/05 ,  A61K45/06 ,  C07D471/04 ,  C07D487/04 ,  C07D495/04 ,  C07D513/04 ,  C07D519/00

Abstract: The present invention provides compounds of Formula (I), or a pharmaceutically acceptable salt thereof, wherein A is a five to eight membered monocyclic or a nine to twelve membered bicyclic heterocyclic ring, as further defined herein; Y is S, CH2, or CH; Z is CH or N; R7 and R9 are hydrogen or (C1-C6)alkyl; R2 is (C1-C6)alkoxy, OH, CN, (C1-C6)alkyl, halogen, or CF3; r and s are 0, 1, or 2; and R1 and R3 are as further defined herein. These compounds are agonists, partial agonists and/or modulators of the NPY4 receptor and may be used for the treatment and prophylaxis of obesity, food intake, and other diseases and conditions modulated by the NPY4 receptor.

Abstract translation: 本发明提供式（I）化合物或其药学上可接受的盐，其中A是如本文进一步定义的五至八元单环或九至十二元二环杂环; Y是S，CH 2或CH; Z是CH或N; R7和R9是氢或（C1-C6）烷基; R2是（C1-C6）烷氧基，OH，CN，（C1-C6）烷基，卤素或CF3; r和s为0,1或2; 并且R1和R3如本文进一步定义。 这些化合物是NPY4受体的激动剂，部分激动剂和/或调节剂，可用于治疗和预防由NPY4受体调节的肥胖症，食物摄入和其它疾病和病症。

公开(公告)号：US20130184284A1

公开(公告)日：2013-07-18

申请号：US13549767

申请日：2012-07-16

Applicant: William R. Ewing ,  Yeheng Zhu ,  Chongqing Sun ,  Yanting Huang ,  Maheswaran Sivasamban Karatholuvhu ,  Scott A. Bolton ,  Laxman Pasunoori ,  Sunil Kumar Mandal ,  Philip M. Sher

Inventor： William R. Ewing ,  Yeheng Zhu ,  Chongqing Sun ,  Yanting Huang ,  Maheswaran Sivasamban Karatholuvhu ,  Scott A. Bolton ,  Laxman Pasunoori ,  Sunil Kumar Mandal ,  Philip M. Sher

IPC: A61K31/506 ,  A61K31/454 ,  A61K31/439 ,  C07D401/12 ,  A61K31/4545 ,  A61K45/06 ,  C07D401/14 ,  A61K31/498 ,  A61K31/501 ,  C07D471/04 ,  A61K31/437 ,  C07D413/12 ,  A61K31/497

CPC classification number: A61K31/506 ,  A61K31/437 ,  A61K31/439 ,  A61K31/454 ,  A61K31/4545 ,  A61K31/497 ,  A61K31/498 ,  A61K31/501 ,  A61K45/06 ,  C07D401/12 ,  C07D401/14 ,  C07D413/12 ,  C07D417/12 ,  C07D451/02 ,  C07D453/06 ,  C07D471/04 ,  C07D471/08

Abstract: The present invention provides compounds of Formula (I): or a stereoisomer, or a pharmaceutically acceptable salt thereof, wherein all of the variables are as defined herein. These compounds are agonists, partial agonists and modulators of the NPY Y4 receptor and may be used for the treatment and prophylaxis of various diseases and conditions.

公开(公告)号：US07368458B2

公开(公告)日：2008-05-06

申请号：US11330541

申请日：2006-01-12

Applicant: Chongqing Sun ,  William R. Ewing ,  Yanting Huang

Inventor： Chongqing Sun ,  William R. Ewing ,  Yanting Huang

IPC: C07D471/02 ,  C07D487/02 ,  A61K31/4375

CPC classification number: C07D471/04

Abstract: The present application describes compounds according to Formula I, pharmaceutical compositions comprising at least one compound according to Formula I and optionally one or more additional therapeutic agents and methods of treatment using the compounds according to Formula I both alone and in combination with one or more additional therapeutic agents. The compounds have the general Formula I: including all prodrugs, pharmaceutically acceptable salts and stereoisomers, R1, R2, R3, R3a, R4, A, B, n, Y and Z are described herein.

Abstract translation: 本申请描述了根据式I的化合物，包含至少一种根据式I的化合物和任选的一种或多种另外的治疗剂的药物组合物和使用根据式I的化合物的治疗方法，其单独和与一种或多种另外的 治疗剂。 该化合物具有通式I：包括所有前药，药学上可接受的盐和立体异构体，R 1，R 2，R 3，R 3， 本文描述了SUP，3a，R 4，A，B，n，Y和Z。

公开(公告)号：US20070004772A1

公开(公告)日：2007-01-04

申请号：US11454322

申请日：2006-06-16

Applicant: Chongqing Sun ,  Philip Sher ,  Gang Wu ,  William Ewing ,  Yanting Huang ,  Taekyu Lee ,  Natesan Murugesan ,  Richard Sulsky

Inventor： Chongqing Sun ,  Philip Sher ,  Gang Wu ,  William Ewing ,  Yanting Huang ,  Taekyu Lee ,  Natesan Murugesan ,  Richard Sulsky

IPC: C07D471/02 ,  A61K31/4745

CPC classification number: C07D471/04

Abstract: The present application describes compounds according to Formula I, pharmaceutical compositions comprising at least one compound according to Formula I and optionally one or more additional therapeutic agents, and methods of treatment using the compounds according to Formula I both alone and in combination with one or more additional therapeutic agents. The compounds have the following general formula: including all prodrugs, solvates, pharmaceutically acceptable salts and stereoisomers, wherein R1, R2, R3, R4 and R5 are described herein.

Abstract translation: 本申请描述了根据式I的化合物，包含至少一种根据式I的化合物和任选的一种或多种另外的治疗剂的药物组合物，以及使用式I化合物单独和与一种或多种 其他治疗剂。 该化合物具有以下通式：包括所有前药，溶剂化物，药学上可接受的盐和立体异构体，其中R 1，R 2，R 3， 本文描述了R 4和R 5。

公开(公告)号：US20060287322A1

公开(公告)日：2006-12-21

申请号：US11455045

申请日：2006-06-16

Applicant: Chongqing Sun ,  Yanting Huang ,  Doree Sitkoff ,  Guixue Yu ,  Amarendra Mikkilineni ,  William Ewing

Inventor： Chongqing Sun ,  Yanting Huang ,  Doree Sitkoff ,  Guixue Yu ,  Amarendra Mikkilineni ,  William Ewing

IPC: A61K31/503 ,  C07D487/02 ,  A61K31/53

CPC classification number: C07D487/04

Abstract: The present application describes compounds according to Formula I, pharmaceutical compositions comprising at least one compound according to Formula I and optionally one or more additional therapeutic agents and methods of treatment using the compounds according to Formulas I both alone and in combination with one or more additional therapeutic agents. The compounds have the following general formulas: including all prodrugs, solvates, pharmaceutically acceptable salts and stereoisomers, wherein B, R1, R2, R3 and x are described herein.

Abstract translation: 本申请描述了根据式I的化合物，包含至少一种根据式I的化合物和任选的一种或多种另外的治疗剂的药物组合物和使用根据式I的化合物单独治疗并与一种或多种另外的组合的治疗方法 治疗剂。 该化合物具有以下通式：包括所有前药，溶剂化物，药学上可接受的盐和立体异构体，其中B，R 1，R 2，R 3， SUP>和x。