-
公开(公告)号:US20110313008A1
公开(公告)日:2011-12-22
申请号:US13145025
申请日:2010-01-21
申请人: Hubert B. Josien , John W. Clader , Andrew Stamford , William J. Greenlee , Michael John Mayer , Jason L. Davis , Ming Min Hsia , Shuangyi Wan
发明人: Hubert B. Josien , John W. Clader , Andrew Stamford , William J. Greenlee , Michael John Mayer , Jason L. Davis , Ming Min Hsia , Shuangyi Wan
IPC分类号: A61K31/426 , A61P3/10 , A61P3/00 , C07D277/04
CPC分类号: C07D417/04 , C07D277/34
摘要: This invention provides for certain pentafluorosulpholane-containing compounds of the formula or a pharmaceutically acceptable salt, ester, solvate or prodrug thereof, wherein the variables are defined herein; the inventive compounds are agonists of the G-protein coupled receptor 40 (GPR40, also known as free fatty acid receptor FFAR). This invention further relates to pharmaceutical compositions containing these compounds, and the use of these compounds to regulate insulin levels in a mammal. The compounds may be used, for example in the prevention and treatment of Type 2 diabetes mellitus and in the prevention and treatment of conditions related to Type 2 diabetes mellitus, such as insulin resistance, obesity and lipid disorders.
摘要翻译: 本发明提供了具有下式的某些五氟丁烷化合物或其药学上可接受的盐,酯,溶剂合物或前药,其中变量在本文中定义; 本发明化合物是G蛋白偶联受体40(GPR40,也称为游离脂肪酸受体FFAR)的激动剂。 本发明还涉及含有这些化合物的药物组合物,以及这些化合物在哺乳动物体内调节胰岛素水平的用途。 该化合物可用于例如预防和治疗2型糖尿病以及预防和治疗与2型糖尿病相关的病症,例如胰岛素抵抗,肥胖症和脂质疾病。
-
公开(公告)号:US20110312995A1
公开(公告)日:2011-12-22
申请号:US13145359
申请日:2010-01-21
申请人: Hubert B. Josien , John W. Clader , William J. Greenlee , Michael John Mayer , Robert Jason Herr , Jason L. Davis , Kai Deng , Ming Min Hsia , Shuangyi Wan
发明人: Hubert B. Josien , John W. Clader , William J. Greenlee , Michael John Mayer , Robert Jason Herr , Jason L. Davis , Kai Deng , Ming Min Hsia , Shuangyi Wan
IPC分类号: A61K31/4545 , C07D417/14 , C07D417/12 , A61K31/4709 , A61P3/00 , A61K31/4439 , A61P5/48 , A61P3/10 , A61P3/04 , A61P3/06 , C07D401/14 , A61K31/454
CPC分类号: C07D417/12 , C07D215/233 , C07D417/14
摘要: This invention provides for certain bridged and fused heterocyclic compounds of the formula (I) or a pharmaceutically acceptable salt, ester solvate or prodrug thereof wherein: L is: (II) and the other variables are defined herein; the inventive compounds are agonists of the G-protein coupled receptor 40 (GPR40, also known as free fatty acid receptor FFAR). This invention further relates to pharmaceutical compositions containing these compounds, and the use of these compounds to regulate insulin levels in a mammal. The compounds may be used, for example in the prevention and treatment of Type 2 diabetes mellitus and in the prevention and treatment of conditions related to Type 2 diabetes mellitus, such as insulin resistance, obesity and lipid disorders.
摘要翻译: 本发明提供了一些式(I)的桥连和稠合杂环化合物或其药学上可接受的盐,酯溶剂合物或前药,其中:L是:(II),其它变量在本文中定义; 本发明化合物是G蛋白偶联受体40(GPR40,也称为游离脂肪酸受体FFAR)的激动剂。 本发明还涉及含有这些化合物的药物组合物,以及这些化合物在哺乳动物体内调节胰岛素水平的用途。 该化合物可用于例如预防和治疗2型糖尿病以及预防和治疗与2型糖尿病相关的病症,例如胰岛素抵抗,肥胖症和脂质疾病。
-
公开(公告)号:US20110312967A1
公开(公告)日:2011-12-22
申请号:US13145152
申请日:2010-01-21
申请人: Hubert B. Josien , John W. Clader , William J. Greenlee , Michael John Mayer , Jason L. Davis , Shuangyi Wan
发明人: Hubert B. Josien , John W. Clader , William J. Greenlee , Michael John Mayer , Jason L. Davis , Shuangyi Wan
IPC分类号: A61K31/501 , C07D417/12 , C07D263/44 , C07D417/04 , A61P3/10 , A61K31/426 , A61K31/421 , A61K31/427 , A61K31/4439 , C07D277/34 , C07D417/14
CPC分类号: C07D417/14 , C07D263/44 , C07D277/34 , C07D417/04 , C07D417/12
摘要: This invention provides for certain bridged and fused compounds of the formula G-L-A I or a pharmaceutically acceptable salt, ester of solvate thereof wherein: A is: (I) and the other variables are defined herein; the inventive compounds are agonists of the G-protein coupled receptor 40 (GPR40, also known as free fatty acid receptor FFAR). This invention further relates to pharmaceutical compositions containing these compounds, and the use of these compounds to regulate insulin levels in a mammal. The compounds may be used, for example in the prevention and treatment of Type 2 diabetes mellitus and in the prevention and treatment of conditions related to Type 2 diabetes mellitus, such as insulin resistance, obesity and lipid disorders.
摘要翻译: 本发明提供了一些具有式G-L-A I的桥连和稠合化合物或其药学上可接受的盐,其溶剂合物的酯,其中:A是:(I),其它变量在本文中定义; 本发明化合物是G蛋白偶联受体40(GPR40,也称为游离脂肪酸受体FFAR)的激动剂。 本发明还涉及含有这些化合物的药物组合物,以及这些化合物在哺乳动物体内调节胰岛素水平的用途。 该化合物可用于例如预防和治疗2型糖尿病以及预防和治疗与2型糖尿病相关的病症,例如胰岛素抵抗,肥胖症和脂质疾病。
-
公开(公告)号:US09364555B2
公开(公告)日:2016-06-14
申请号:US14234133
申请日:2012-07-19
申请人: Paul Edward Floreancig , Billy W. Day , Shuangyi Wan , Fanghui Wu
发明人: Paul Edward Floreancig , Billy W. Day , Shuangyi Wan , Fanghui Wu
IPC分类号: A61K47/48 , C07D407/06 , C07D407/12 , C07D407/14
CPC分类号: A61K47/48384 , C07D407/06 , C07D407/12 , C07D407/14
摘要: Compounds that include a pederin, psymberin or pederin/psymberin chimera scaffold. The pederin scaffold includes a substituent at the C10 and/or C13 position that may include a linker that may be conjugated to a targeting moiety. The psymberin scaffold includes a substituent at the C8 and/or C11 positions that may include a linker that may be conjugated to a targeting moiety. The pederin/psymberin chimera scaffold includes a substituent at the C10 and/or C13 position that may include a linker that may be conjugated to a targeting moiety. The pederin, psymberin or pederin/psymberin chimera scaffold may be modified to include substituents at positions other than the C10 or C13 of pederin, or the C8 and C11 of psymberin.
摘要翻译: 化合物包括pederin,psymberin或pederin / psymberin嵌合体支架。 er脚骨架在C10和/或C13位置包含可以与可能与靶向部分缀合的接头的取代基。 精神分裂素支架在C8和/或C11位置包括可以包含可以与靶向部分缀合的接头的取代基。 pederin / psymberin嵌合体支架包括在C10和/或C13位置的取代基,其可以包括可以与靶向部分缀合的连接体。 可以修饰pederin,psymberin或pederin / psymberin嵌合体支架,以在除Pederin的C10或C13之外的位置或psymberin的C8和C11中包含取代基。
-
公开(公告)号:US20140161877A1
公开(公告)日:2014-06-12
申请号:US14234133
申请日:2012-07-19
申请人: Paul Edward Floreancig , Billy W. Day , Shuangyi Wan , Fanghui Wu
发明人: Paul Edward Floreancig , Billy W. Day , Shuangyi Wan , Fanghui Wu
IPC分类号: A61K47/48
CPC分类号: A61K47/48384 , C07D407/06 , C07D407/12 , C07D407/14
摘要: Compounds that include a pederin, psymberin or pederin/psymberin chimera scaffold. The pederin scaffold includes a substituent at the C10 and/or C13 position that may include a linker that may be conjugated to a targeting moiety. The psymberin scaffold includes a substituent at the C8 and/or C11 positions that may include a linker that may be conjugated to a targeting moiety. The pederin/psymberin chimera scaffold includes a substituent at the C10 and/or C13 position that may include a linker that may be conjugated to a targeting moiety. The pederin, psymberin or pederin/psymberin chimera scaffold may be modified to include substituents at positions other than the C10 or C13 of pederin, or the C8 and C11 of psymberin.
摘要翻译: 化合物包括pederin,psymberin或pederin / psymberin嵌合体支架。 er脚骨架在C10和/或C13位置包含可以与可能与靶向部分缀合的接头的取代基。 精神分裂素支架在C8和/或C11位置包括可以包含可以与靶向部分缀合的接头的取代基。 pederin / psymberin嵌合体支架包括在C10和/或C13位置的取代基,其可以包括可以与靶向部分缀合的连接体。 可以修饰pederin,psymberin或pederin / psymberin嵌合体支架,以在除Pederin的C10或C13之外的位置或psymberin的C8和C11中包含取代基。
-
-
-
-