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1. 发明申请

WO03024395A8 LINKED BIARYL COMPOUNDS 审中-公开
标题翻译：链接的二元化合物
公开(公告)号：WO03024395A8
公开(公告)日：2004-01-22
申请号：PCT/US0229232
申请日：2002-09-13
申请人： TULARIK INC , JAPAN TOBACCO INC , ABE HIROYUKI , HOUZE JONATHAN , KAWASAKI HISASHI , KAYSER FRANK , SHARMA RAJIV , SPERRY SAMUEL
发明人： ABE HIROYUKI , HOUZE JONATHAN , KAWASAKI HISASHI , KAYSER FRANK , SHARMA RAJIV , SPERRY SAMUEL
IPC分类号： C07D215/20 , A61K31/192 , A61K31/216 , A61K31/4184 , A61K31/421 , A61K31/426 , A61K31/4406 , A61K31/47 , A61P1/00 , A61P3/00 , A61P3/04 , A61P3/06 , A61P3/10 , A61P9/00 , A61P9/10 , A61P11/00 , A61P11/06 , A61P13/08 , A61P13/12 , A61P15/00 , A61P19/02 , A61P25/00 , A61P25/06 , A61P29/00 , A61P31/04 , A61P35/00 , A61P37/00 , C07C317/22 , C07C321/30 , C07C323/20 , C07C323/21 , C07D213/65 , C07D215/22 , C07D235/26 , C07D263/40 , C07D277/20 , C07D277/34 , A61K31/415 , A61K31/24 , A61K31/40 , A61K31/42 , A61K31/425 , C07D207/00 , C07D209/02 , C07D215/00 , C07D233/00 , C07D239/02
CPC分类号： C07C317/22 , C07C323/20 , C07C323/21 , C07C2602/10
摘要： Compounds, compositions and methods that are useful for the treatment of metabolic disorders, inflammatory diseases and cancer are provided herein. In particular, the invention provides compounds which modulate the expression and/or function of proteins involved in lipid metabolism, inflammation and cell proliferation. The subject compounds are linked biaryl compounds.
摘要翻译：本文提供了可用于治疗代谢紊乱，炎性疾病和癌症的化合物，组合物和方法。特别地，本发明提供调节参与脂质代谢，炎症和细胞增殖的蛋白质的表达和/或功能的化合物。主题化合物是联芳基化合物。

2. 发明申请

WO2010045258A2 SPIROCYCLIC GPR40 MODULATORS 审中-公开
标题翻译：螺旋GPR40调制器
公开(公告)号：WO2010045258A2
公开(公告)日：2010-04-22
申请号：PCT/US2009/060549
申请日：2009-10-13
申请人： AMGEN INC. , BROWN, Sean P. , DRANSFIELD, Paul , DU, Xiaohui , FU, Zice , HOUZE, Jonathan , JIAO, XianYun , LAI, SuJen , LI, An-Rong , LIU, Jiwen , MA, Zhihua , MEDINA, Julio C. , PATTAROPONG, Vatee , SHEN, Wang , VIMOLRATANA, Marc , WANG, Yingcai , WANG, Zhongyu , YU, Ming , ZHU, Liusheng
发明人： BROWN, Sean P. , DRANSFIELD, Paul , DU, Xiaohui , FU, Zice , HOUZE, Jonathan , JIAO, XianYun , LAI, SuJen , LI, An-Rong , LIU, Jiwen , MA, Zhihua , MEDINA, Julio C. , PATTAROPONG, Vatee , SHEN, Wang , VIMOLRATANA, Marc , WANG, Yingcai , WANG, Zhongyu , YU, Ming , ZHU, Liusheng
IPC分类号： C07C62/34 , C07D249/00 , C07D277/00 , C07D311/00 , C07D231/00 , C07D271/00 , C07D221/00
CPC分类号： C07C62/34 , C07C2601/02 , C07C2601/04 , C07C2601/08 , C07C2601/10 , C07C2601/14 , C07D213/643 , C07D217/24 , C07D253/065 , C07D277/22 , C07D311/04 , C07D401/12
摘要： The present invention provides compounds useful, for example, for treating metabolic disorders in a subject. Such compounds have the general formula IA, IB, I'A or I'B, where the definitions of the variables are provided herein. The present invention also provides compositions that include, and methods for using, the compounds in preparing medicaments and for treating metabolic disorders such as, for example, type II diabetes.
摘要翻译：本发明提供了可用于例如治疗受试者的代谢紊乱的化合物。这些化合物具有通式IA，IB，I'A或I'B，其中本文提供变量的定义。本发明还提供了组合物，其包括化合物在制备药物和用于治疗代谢性疾病例如II型糖尿病中的使用方法。

3. 发明申请

WO2007106469A2 BICYCLIC CARBOXYLIC ACID DERIVATIVES USEFUL FOR TREATING METABOLIC DISORDERS 审中-公开
标题翻译：用于治疗代谢障碍的双环羧酸衍生物
公开(公告)号：WO2007106469A2
公开(公告)日：2007-09-20
申请号：PCT/US2007/006279
申请日：2007-03-12
申请人： AMGEN INC. , SHARMA, Rajiv , AKERMAN, Michelle , CARDOZO, Mario, G. , HOUZE, Jonathan, B. , LI, An-Rong , LIU, Jinqian , LIU, Jiwen , MA, Zhihua , MEDINA, Julio, C. , SCHMITT, Michael, J. , SUN, Ying , WANG, Yingcai , WANG, Zhongyu , ZHU, Liusheng
发明人： SHARMA, Rajiv , AKERMAN, Michelle , CARDOZO, Mario, G. , HOUZE, Jonathan, B. , LI, An-Rong , LIU, Jinqian , LIU, Jiwen , MA, Zhihua , MEDINA, Julio, C. , SCHMITT, Michael, J. , SUN, Ying , WANG, Yingcai , WANG, Zhongyu , ZHU, Liusheng
IPC分类号： C07D209/08 , C07D209/46 , C07D215/22 , C07D277/24 , C07D311/74 , C07D313/08 , C07D417/12 , C07D498/04 , C07C59/54 , C07C59/72 , A61K31/426 , A61P3/10
CPC分类号： C07C57/62 , C07C59/64 , C07C59/72 , C07D209/08 , C07D209/46 , C07D215/20 , C07D215/227 , C07D277/24 , C07D311/58 , C07D311/74 , C07D311/76 , C07D313/08 , C07D417/12 , C07D498/04
摘要： Compounds having the general formula I and/or the general formula II are useful, for example, for treating metabolic disorders in a subject formula (I) (II) where the variables are provided herein. Compositions and methods for using the compounds for preparing medicaments and for treating metabolic disorders such as, for instance, type II diabetes are disclosed.
摘要翻译：具有通式I和/或通式II的化合物可用于例如本文提供变量的主题式（I）（II）中的代谢紊乱。公开了用于制备药物和用于治疗代谢性疾病例如II型糖尿病的化合物的组合物和方法。

4. 发明申请

WO2005086661A3 COMPOUNDS, PHARMACEUTICAL COMPOSITIONS AND METHODS FOR USE IN TREATING METABOLIC DISORDERS 审中-公开
标题翻译：化合物，药物组合物和用于治疗代谢障碍的方法
公开(公告)号：WO2005086661A3
公开(公告)日：2006-05-04
申请号：PCT/US2005005815
申请日：2005-02-24
申请人： AMGEN INC , AKERMAN MICHELLE , HOUZE JONATHAN , LIN DANIEL C H , LIU JIWEN , LUO JIAN , MEDINA JULIO C , QIU WEI , REAGAN JEFFREY D , SCHMITT MICHAEL J , WANG YINGCAI , SHARMA RAJIV , SHUTTLEWORTH STEPHEN J , SUN YING , ZHANG JIAN , ZHU LIUSHENG
发明人： AKERMAN MICHELLE , HOUZE JONATHAN , LIN DANIEL C H , LIU JIWEN , LUO JIAN , MEDINA JULIO C , QIU WEI , REAGAN JEFFREY D , SCHMITT MICHAEL J , WANG YINGCAI , SHARMA RAJIV , SHUTTLEWORTH STEPHEN J , SUN YING , ZHANG JIAN , ZHU LIUSHENG
IPC分类号： C07D277/24 , C07D277/30 , C07C53/132 , A61K31/19 , A61K31/215 , A61K31/42 , C07C213/00 , C07C277/00
CPC分类号： C07D277/24 , C07D277/30
摘要： The present invention provides compounds useful, for example, for modulating insulin levels in a subject and that have the general formula Q-L 1 -P-L 2 -M-X-L 3 -A wherein the definitions of the variables Q, L 1 , P, L 2 , M, X, L 3 and A are provided herein. The present invention also provides compositions and methods for use of the compounds, for instance, for treatment of type II diabetes.
摘要翻译：本发明提供了可用于例如用于调节受试者中胰岛素水平的化合物，其具有通式QL 1 -PL 2 -MXL 3 / SUP> -A，其中变量Q，L 1，P，L 2，M，X，L 3和A的定义是本文提供。本发明还提供了用于化合物的组合物和方法，例如用于治疗II型糖尿病。

5. 发明申请

WO2009111056A1 CONFORMATIONALLY CONSTRAINED CARBOXYLIC ACID DERIVATIVES USEFUL FOR TREATING METABOLIC DISORDERS 审中-公开
标题翻译：适用于治疗代谢障碍的有约束力的羧酸衍生物
公开(公告)号：WO2009111056A1
公开(公告)日：2009-09-11
申请号：PCT/US2009/001435
申请日：2009-03-04
申请人： AMGEN INC. , BROWN, Sean, P. , DRANSFIELD, Paul, J. , HOUZE, Jonathan , KOHN, Todd, J. , LIU, Jiwen , MEDINA, Julio , PATTAROPONG, Vatee , SHEN, Wang , VIMOLRATANA, Marc , WANG, Yingcai , YU, Ming , ZHU, Liusheng
发明人： BROWN, Sean, P. , DRANSFIELD, Paul, J. , HOUZE, Jonathan , KOHN, Todd, J. , LIU, Jiwen , MEDINA, Julio , PATTAROPONG, Vatee , SHEN, Wang , VIMOLRATANA, Marc , WANG, Yingcai , YU, Ming , ZHU, Liusheng
IPC分类号： C07C59/72 , C07D213/64 , A61K31/192 , A61P3/10 , A61P9/00 , A61K31/435
CPC分类号： C07C59/72
摘要： The present invention provides compounds useful, for example, for treating metabolic disorders in a subject. Such compounds have the general formula I or the general formula III: where the definitions of the variables are provided herein. The present invention also provides compositions that include, and methods for using, the compounds in preparing medicaments and for treating metabolic disorders such as, for example, type II diabetes.
摘要翻译：本发明提供了可用于例如治疗受试者的代谢紊乱的化合物。这些化合物具有通式I或通式III：其中本文提供变量的定义。本发明还提供了组合物，其包括化合物在制备药物和用于治疗代谢性疾病例如II型糖尿病中的使用方法。

6. 发明申请

WO2009048527A1 SUBSTITUTED BIPHENYL GPR40 MODULATORS 审中-公开
标题翻译：取代的BIPHENYL GPR40调节器
公开(公告)号：WO2009048527A1
公开(公告)日：2009-04-16
申请号：PCT/US2008/011422
申请日：2008-10-03
申请人： AMGEN INC. , KIM, Yong-Jae , BROWN, Sean, P. , CAO, Qiong , DRANSFIELD, Paul, J. , DU, Xiaohui , HOUZE, Jonathan , JIAO, Xian Yun , KOHN, Todd, J. , LAI, Sujen , LI, An-Rong , LIN, Daniel , LUO, Jian , MEDINA, Julio, C. , REAGAN, Jeffrey, D. , PATTAROPONG, Vatee , SCHWARZ, Margrit , SHEN, Wang , SU, Yongli , SWAMINATH, Gayathri , VIMOLRATANA, Marc , WANG, Xiang , XIONG, Yumei , YANG, Li , YU, Ming , ZHANG, Jie , ZHU, Liusheng
发明人： KIM, Yong-Jae , BROWN, Sean, P. , CAO, Qiong , DRANSFIELD, Paul, J. , DU, Xiaohui , HOUZE, Jonathan , JIAO, Xian Yun , KOHN, Todd, J. , LAI, Sujen , LI, An-Rong , LIN, Daniel , LUO, Jian , MEDINA, Julio, C. , REAGAN, Jeffrey, D. , PATTAROPONG, Vatee , SCHWARZ, Margrit , SHEN, Wang , SU, Yongli , SWAMINATH, Gayathri , VIMOLRATANA, Marc , WANG, Xiang , XIONG, Yumei , YANG, Li , YU, Ming , ZHANG, Jie , ZHU, Liusheng
IPC分类号： C07C59/68 , C07C217/54 , C07C323/19 , C07D213/64 , A61K31/192 , A61K31/4415 , A61P3/10
CPC分类号： C07C323/62 , C07C59/68 , C07C59/72 , C07C217/54 , C07C217/62 , C07C317/22 , C07C323/19 , C07C2601/02 , C07C2601/04 , C07C2601/08 , C07C2601/10 , C07C2601/14 , C07C2601/16 , C07C2601/18 , C07C2602/42 , C07C2603/74 , C07D213/64 , C07D309/12
摘要： The present invention provides compounds useful, for example, for treating metabolic disorders in a subject. Such compounds have the general formula I: where the definitions of the variables are provided herein. The present invention also provides compositions that include, and methods for using, the compounds in preparing medicaments and for treating metabolic disorders such as, for example, type II diabetes.
摘要翻译：本发明提供了可用于例如治疗受试者的代谢紊乱的化合物。这些化合物具有通式I：其中本文提供变量的定义。本发明还提供了组合物，其包括化合物在制备药物和用于治疗代谢性疾病例如II型糖尿病中的使用方法。

7. 发明申请

WO2006127503A2 COMPOUNDS, PHARMACEUTICAL COMPOSITIONS AND METHODS FOR THEIR USE IN TREATING METABOLIC DISORDERS 审中-公开
标题翻译：化合物，药物组合物及其用于治疗代谢障碍的方法
公开(公告)号：WO2006127503A2
公开(公告)日：2006-11-30
申请号：PCT/US2006/019545
申请日：2006-05-18
申请人： AMGEN INC , HOUZE, Jonathan , LIU, Jiwen , MA, Zhihua , MEDINA, Julio C. , SCHMITT, Michael J. , SHARMA, Rajiv , SUN, Ying , WANG, Yingcai , ZHU, Liusheng
发明人： HOUZE, Jonathan , LIU, Jiwen , MA, Zhihua , MEDINA, Julio C. , SCHMITT, Michael J. , SHARMA, Rajiv , SUN, Ying , WANG, Yingcai , ZHU, Liusheng
CPC分类号： C07D277/24 , C07B2200/07 , C07C235/34 , C07D233/64 , C07D249/08 , C07D257/04 , C07D263/32 , C07D417/12
摘要： The present invention provides compounds useful, for example, for modulating insulin levels in a subject, having the general formula I: wherein Q is an optionally substituted phenyl; L is a bond or O; P is a benzene or an optionally substituted thiazole ring; and R 1 has the values provided herein. The present invention also provides compositions, uses, and methods for use of the compounds, for instance, for treatment of type II diabetes.
摘要翻译：本发明提供了可用于例如用于调节受试者中具有通式I的胰岛素水平的化合物：其中Q是任选取代的苯基; L是一个键或O; P是苯或任选取代的噻唑环; 且R 1具有本文提供的值。本发明还提供了用于治疗II型糖尿病的化合物的组合物，用途和方法。

8. 发明申请

WO2005086661A2 COMPOUNDS, PHARMACEUTICAL COMPOSITIONS AND METHODS FOR USE IN TREATING METABOLIC DISORDERS 审中-公开
标题翻译：化合物，药物组合物和用于治疗代谢障碍的方法
公开(公告)号：WO2005086661A2
公开(公告)日：2005-09-22
申请号：PCT/US2005/005815
申请日：2005-02-24
申请人： AMGEN INC. , AKERMAN, Michelle , HOUZE, Jonathan , LIN, Daniel, C., H. , LIU, Jiwen , LUO, Jian , MEDINA, Julio, C. , QIU, Wei , REAGAN, Jeffrey, D. , SHARMA, Rajiv , SHUTTLEWORTH, Stephen, J. , SUN, Ying , ZHANG, Jian , ZHU, Liusheng
发明人： AKERMAN, Michelle , HOUZE, Jonathan , LIN, Daniel, C., H. , LIU, Jiwen , LUO, Jian , MEDINA, Julio, C. , QIU, Wei , REAGAN, Jeffrey, D. , SHARMA, Rajiv , SHUTTLEWORTH, Stephen, J. , SUN, Ying , ZHANG, Jian , ZHU, Liusheng
IPC分类号： C07D277/24 , C07D277/30
CPC分类号： C07D277/24 , C07D277/30
摘要： The present invention provides compounds useful, for example, for modulating insulin levels in a subject and that have the general formula Q-L 1 -P-L 2 -M-X-L 3 -A wherein the definitions of the variables Q, L 1 , P, L 2 , M, X, L 3 and A are provided herein. The present invention also provides compositions and methods for use of the compounds, for instance, for treatment of type II diabetes.
摘要翻译：本发明提供了可用于例如调节受试者中胰岛素水平并具有通式QL 1 -PL 2 -MXL 3 -A的化合物，其中变量Q，L <1的定义 >，P，L 2，M，X，L 3和A。本发明还提供了用于治疗II型糖尿病的化合物的组合物和方法。

9. 发明申请

WO0220463A3 FXR MODULATORS 审中-公开
标题翻译： FXR调制器
公开(公告)号：WO0220463A3
公开(公告)日：2003-08-21
申请号：PCT/US0127239
申请日：2001-08-31
申请人： TULARIK INC , HOUZE JONATHAN , MCKENDRY SHARON , GERGELY JOSHUA P , XIA YI , SHAN BEI , KAYSER FRANK
发明人： HOUZE JONATHAN , MCKENDRY SHARON , GERGELY JOSHUA P , XIA YI , SHAN BEI , KAYSER FRANK
IPC分类号： A61P35/00 , C07C233/75 , C07C237/22 , C07C311/19 , C07C311/29 , C07D209/48 , C07D241/44 , C07D279/02 , A61K31/16 , C07C311/17 , C07K14/705
CPC分类号： C07D209/48 , C07C233/75 , C07C237/22 , C07C311/19 , C07C311/29 , C07C2601/14 , C07D241/44 , C07D279/02
摘要： The present invention provides compounds, pharmaceutical compositions and methods that are useful in modulating the farnesoid X receptor (FXR). As FXR is involved in negatively controlling the expression level of cholesterol 7 alpha -hydroxylase (cyp7a), the rate-limiting enzyme involved in the oxidative metabolism of cholesterol into bile acids, the compounds described herein find utility in treating diseases associated with abnormally high or low cholesterol levels. In certain aspects, the FXR modulators (e.g., antagonists) described herein block the negative feed-back downregulation of cyp7a expression produced by certain cholic acids, the endogenous ligands for FXR. Moreover, as FXR forms heterodimers with the retinoid X receptor (RXR) in some cell types, modulation of the level of FXR activity in cells has a wide range of effects on a variety of biological processes which are mediated by RXR or other RXR-interacting proteins such as PPAR gamma and PPAR alpha . Thus, compounds described herein are useful in treating other biological activities such as obesity, diabetes, lipid associated disorders, cancer, inflammatory disorders, disorders involving a disrupted or dysfunctional epidermal barrier, and various other metabolic disorders.
摘要翻译：本发明提供了可用于调节法呢酯X受体（FXR）的化合物，药物组合物和方法。由于FXR涉及负调控胆固醇7α-羟化酶（cyp7a）的表达水平，涉及胆固醇胆固醇氧化代谢的限速酶，本文所述的化合物可用于治疗与异常高相关的疾病或低胆固醇水平在某些方面，本文所述的FXR调节剂（例如拮抗剂）阻断某些胆酸（FXR的内源性配体）产生的cyp7a表达的负反馈下调。此外，由于FXR在一些细胞类型中与类视黄醇X受体（RXR）形成异源二聚体，因此细胞中FXR活性水平的调节对由RXR或其他RXR相互作用介导的各种生物过程具有广泛的影响蛋白质如PPARγ和PPARα。因此，本文所述的化合物可用于治疗其它生物活性，例如肥胖症，糖尿病，脂质相关疾病，癌症，炎性疾病，涉及破坏性或功能失调的表皮屏障的疾病以及各种其它代谢紊乱。

10. 发明申请

WO2003024395A3 LINKED BIARYL COMPOUNDS 审中-公开
公开(公告)号：WO2003024395A3
公开(公告)日：2003-03-27
申请号：PCT/US2002/029232
申请日：2002-09-13
申请人： TULARIK INC. , JAPAN TOBACCO, INC. , ABE, Hiroyuki , HOUZE, Jonathan , KAWASAKI, Hisashi , KAYSER, Frank , SHARMA, Rajiv , SPERRY, Samuel
发明人： ABE, Hiroyuki , HOUZE, Jonathan , KAWASAKI, Hisashi , KAYSER, Frank , SHARMA, Rajiv , SPERRY, Samuel
IPC分类号： A61K31/415
摘要： Compounds, compositions and methods that are useful for the treatment of metabolic disorders, inflammatory diseases and cancer are provided herein. In particular, the invention provides compounds which modulate the expression and/or function of proteins involved in lipid metabolism, inflammation and cell proliferation. The subject compounds are linked biaryl compounds.

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