公开(公告)号：US08759357B2

公开(公告)日：2014-06-24

申请号：US13499135

申请日：2010-10-01

申请人： Gerald W. Shipps, Jr. ,  Clifford C. Cheng ,  Xioahua Huang ,  Abdelghani Achab ,  Peter Orth ,  Johannes H. Voigt

发明人： Gerald W. Shipps, Jr. ,  Clifford C. Cheng ,  Xioahua Huang ,  Abdelghani Achab ,  Peter Orth ,  Johannes H. Voigt

IPC分类号： A01N43/90 ,  A61K31/519 ,  C07D471/00 ,  C07D487/00 ,  C07D491/00

CPC分类号： A61K31/54 ,  A61K45/06 ,  A61K2300/00

摘要： The present invention relates to novel heterocyclic compounds as Fatty Acid Binding Protein (FABP) inhibitors, pharmaceutical compositions comprising the heterocyclic compounds and the use of the compounds for treating or preventing a cardiovascular disease, a metabolic disorder, obesity or an obesity-related disorder, diabetes, dyslipidemia, a diabetic complication, impaired glucose tolerance or impaired fasting glucose. An illustrative compound of the present invention is shown below:

摘要翻译： 本发明涉及作为脂肪酸结合蛋白（FABP）抑制剂的新型杂环化合物，包含杂环化合物的药物组合物和用于治疗或预防心血管疾病，代谢障碍，肥胖或肥胖相关疾病的化合物的用途， 糖尿病，血脂异常，糖尿病并发症，葡萄糖耐量降低或空腹血糖受损。 本发明的说明性化合物如下所示：

公开(公告)号：US20120190696A1

公开(公告)日：2012-07-26

申请号：US13499135

申请日：2010-10-01

申请人： Gerald W. Shipps, JR. ,  Clifford C. Cheng ,  Xioahua Huang ,  Abdelghani Achab ,  Peter Orth ,  Johannes H. Voigt

发明人： Gerald W. Shipps, JR. ,  Clifford C. Cheng ,  Xioahua Huang ,  Abdelghani Achab ,  Peter Orth ,  Johannes H. Voigt

IPC分类号： A61K31/519 ,  A61P9/00 ,  A61P3/00 ,  A61P3/10 ,  A61P3/04 ,  C07D487/04 ,  A61P3/06

CPC分类号： A61K31/54 ,  A61K45/06 ,  A61K2300/00

摘要： The present invention relates to novel heterocyclic compounds as Fatty Acid Binding Protein (FABP) inhibitors, pharmaceutical compositions comprising the heterocyclic compounds and the use of the compounds for treating or preventing a cardiovascular disease, a metabolic disorder, obesity or an obesity-related disorder, diabetes, dyslipidemia, a diabetic complication, impaired glucose tolerance or impaired fasting glucose. An illustrative compound of the present invention is shown below:

摘要翻译： 本发明涉及作为脂肪酸结合蛋白（FABP）抑制剂的新型杂环化合物，包含杂环化合物的药物组合物和用于治疗或预防心血管疾病，代谢障碍，肥胖或肥胖相关疾病的化合物的用途， 糖尿病，血脂异常，糖尿病并发症，葡萄糖耐量降低或空腹血糖受损。 本发明的说明性化合物如下所示：

公开(公告)号：US09351965B2

公开(公告)日：2016-05-31

申请号：US13994224

申请日：2011-12-16

申请人： Gerald W. Shipps, Jr. ,  Xiaohua Huang ,  Yongqi Deng ,  Liang Zhu ,  Alan B. Cooper ,  Binyuan Sun ,  Abdelghani Achab ,  Sie-Mun Lo

发明人： Gerald W. Shipps, Jr. ,  Xiaohua Huang ,  Yongqi Deng ,  Liang Zhu ,  Alan B. Cooper ,  Binyuan Sun ,  Abdelghani Achab ,  Sie-Mun Lo

IPC分类号： C07D231/56 ,  C07D401/04 ,  C07D471/04 ,  C07D401/14 ,  C07D403/14 ,  C07D417/04 ,  A61K31/416 ,  A61K31/4439 ,  A61K45/06 ,  A61K31/437

CPC分类号： A61K31/4439 ,  A61K31/416 ,  A61K31/437 ,  A61K45/06 ,  C07D231/56 ,  C07D401/04 ,  C07D401/14 ,  C07D403/14 ,  C07D417/04 ,  C07D471/04 ,  A61K2300/00

摘要： The present invention provides a compound of the Formula I, or a pharmaceutically acceptable salt, solvate or ester thereof, wherein R, R1, R2, R3, m and are as defined herein. The compounds are ERK inhibitors. Also disclosed are pharmaceutical compositions that comprise the above compounds, and methods of treating cancer using the same.

摘要翻译： 本发明提供式I化合物或其药学上可接受的盐，溶剂化物或酯，其中R，R 1，R 2，R 3，m如本文所定义。 这些化合物是ERK抑制剂。 还公开了包含上述化合物的药物组合物和使用其的癌症治疗方法。

公开(公告)号：US20130261125A1

公开(公告)日：2013-10-03

申请号：US13994224

申请日：2011-12-16

申请人： Gerald W. Shipps, JR. ,  Xiaohua Huang ,  Yongqi Deng ,  Liang Zhu ,  Alan B. Cooper ,  Binyuan Sun ,  Abdelghani Achab ,  Sie-Mun Lo

发明人： Gerald W. Shipps, JR. ,  Xiaohua Huang ,  Yongqi Deng ,  Liang Zhu ,  Alan B. Cooper ,  Binyuan Sun ,  Abdelghani Achab ,  Sie-Mun Lo

IPC分类号： A61K31/4439 ,  C07D471/04 ,  A61K31/437 ,  C07D401/04

CPC分类号： A61K31/4439 ,  A61K31/416 ,  A61K31/437 ,  A61K45/06 ,  C07D231/56 ,  C07D401/04 ,  C07D401/14 ,  C07D403/14 ,  C07D417/04 ,  C07D471/04 ,  A61K2300/00

摘要： The present invention provides a compound of the Formula I, or a pharmaceutically acceptable salt, solvate or ester thereof, wherein R, R1, R2, R3, m and are as defined herein. The compounds are ERK inhibitors. Also disclosed are pharmaceutical compositions that comprise the above compounds, and methods of treating cancer using the same.

摘要翻译： 本发明提供式I化合物或其药学上可接受的盐，溶剂化物或酯，其中R，R 1，R 2，R 3，m如本文所定义。 这些化合物是ERK抑制剂。 还公开了包含上述化合物的药物组合物和使用其的癌症治疗方法。

公开(公告)号：US11319283B2

公开(公告)日：2022-05-03

申请号：US16753035

申请日：2018-10-04

申请人： MERCK SHARP & DOHME CORP. ,  Meredeth Ann McGowan ,  Abdelghani Achab ,  Xavier Fradera ,  Yongxin Han ,  Derun Li ,  Jongwon Lim ,  Kun Liu ,  Nunzio Sciammetta ,  Catherine M. White ,  Wensheng Yu ,  Hongjun Zhang ,  Hua Zhou

发明人： Meredeth Ann McGowan ,  Abdelghani Achab ,  Xavier Fradera ,  Yongxin Han ,  Derun Li ,  Jongwon Lim ,  Kun Liu ,  Nunzio Sciammetta ,  Catherine M. White ,  Wensheng Yu ,  Hongjun Zhang ,  Hua Zhou

IPC分类号： C07D205/04 ,  C07C237/42 ,  C07D213/75 ,  C07D213/82 ,  C07D231/14 ,  C07D233/90 ,  C07D237/20 ,  C07D239/28 ,  C07D241/24 ,  C07D263/34 ,  C07D277/56 ,  C07D285/06 ,  C07D307/14 ,  C07D309/14 ,  C07D487/04

摘要： Disclosed herein is a compound of formula (I), or a pharmaceutically acceptable salt thereof: (Formula (I)). Also disclosed herein are uses of a compound disclosed herein in the potential treatment or prevention of an IDO-associated disease or disorder. Also disclosed herein are compositions comprising a compound disclosed herein. Further disclosed herein are uses of a composition in the potential treatment or prevention of an IDO-associated disease or disorder.

公开(公告)号：US11034661B2

公开(公告)日：2021-06-15

申请号：US16495883

申请日：2018-03-23

申请人： Merck Sharp & Dohme Corp. ,  Liangqin Guo ,  Yongxin Han ,  Kun Liu ,  Shuwen He ,  Joseph Kozlowski ,  Ravi Nargund ,  Wensheng Yu ,  Hongjun Zhang ,  Qinglin Pu ,  Derun Li ,  Abdelghani Achab ,  Guoqing Li

发明人： Liangqin Guo ,  Yongxin Han ,  Kun Liu ,  Shuwen He ,  Joseph Kozlowski ,  Ravi Nargund ,  Wensheng Yu ,  Hongjun Zhang ,  Qinglin Pu ,  Derun Li ,  Abdelghani Achab ,  Guoqing Li

IPC分类号： C07D271/08 ,  C07D413/12

摘要： Disclosed herein is a compound of formula (I), or a pharmaceutically acceptable salt thereof. Also disclosed herein are uses of the compounds disclosed herein in the potential treatment or prevention of an IDO-associated disease or disorder. Also disclosed herein are compositions comprising a compound disclosed herein. Further disclosed herein are uses of the compositions in the potential treatment or prevention of an IDO-associated disease or disorder.

公开(公告)号：US20200277252A1

公开(公告)日：2020-09-03

申请号：US16753035

申请日：2018-10-04

申请人： Meredeth Ann McGowan ,  Abdelghani Achab ,  Xavier Fradera ,  Yongxin Han ,  Derun Li ,  Jongwon Lim ,  Kun Liu ,  Nunzio Sciammetta ,  Catherine M. White ,  Wensheng Yu ,  Hongjun Zhang ,  Hua Zhou ,  MERCK SHARP & DOHME CORP.

发明人： Meredeth Ann McGowan ,  Abdelghani Achab ,  Xavier Fradera ,  Yongxin Han ,  Derun Li ,  Jongwon Lim ,  Kun Liu ,  Nunzio Sciammetta ,  Catherine M. White ,  Wensheng Yu ,  Hongjun Zhang ,  Hua Zhou

IPC分类号： C07C237/42 ,  C07D241/24 ,  C07D213/82 ,  C07D233/90 ,  C07D263/34 ,  C07D231/14 ,  C07D277/56 ,  C07D239/28 ,  C07D213/75 ,  C07D309/14 ,  C07D237/20 ,  C07D307/14 ,  C07D205/04 ,  C07D285/06 ,  C07D487/04

摘要： Disclosed herein is a compound of formula (I), or a pharmaceutically acceptable salt thereof: (Formula (I)). Also disclosed herein are uses of a compound disclosed herein in the potential treatment or prevention of an IDO-associated disease or disorder. Also disclosed herein are compositions comprising a compound disclosed herein. Further disclosed herein are uses of a composition in the potential treatment or prevention of an IDO-associated disease or disorder.