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31. 发明申请

WO2013173198A1 PYRIMIDINYLPIPERIDINYLOXYPYRIDONE ANALOGUES AS GPR119 MODULATORS 审中-公开
标题翻译： PYRIMIDINYLPIPERIDINYLOXYPYRIDONE ANALOGUES作为GPR119调制器
公开(公告)号：WO2013173198A1
公开(公告)日：2013-11-21
申请号：PCT/US2013/040692
申请日：2013-05-13
申请人： BRISTOL-MYERS SQUIBB COMPANY
发明人： BROEKEMA, Matthias , WU, Gang , WACKER, Dean, A.
IPC分类号： C07D401/14 , A61K31/506 , A61P3/00
CPC分类号： C07D401/14 , A61K31/403 , A61K31/506
摘要： Novel compounds of structure Formula I: (I) or an enantiomer, a diastereomer, or a pharmaceutically acceptable salt thereof, wherein R1, R2 and R3 are defined herein, are provided which are GPR119 G protein-coupled receptor modulators. GPR119 G protein-coupled receptor modulators are useful in treating, preventing, or slowing the progression of diseases requiring GPR119 G protein-coupled receptor modulator therapy. Thus, the disclosure also concerns compositions comprising these novel compounds and methods of treating diseases or conditions related to the activity of the GPR119 G protein-coupled receptor by using any of these novel compounds or a composition comprising any of such novel compounds.
摘要翻译：提供结构式I的新型化合物：其中R1，R2和R3在本文中定义的是GPR119G蛋白偶联受体调节剂，其中R 1，R 2和R 3在本文中定义，所述化合物是式（I）或其对映异构体，非对映异构体或其药学上可接受的盐。 GPR119 G蛋白偶联受体调节剂可用于治疗，预防或减缓需要GPR119 G蛋白偶联受体调节剂治疗的疾病进展。因此，本公开还涉及包含这些新化合物的组合物以及通过使用任何这些新化合物或包含任何这些新化合物的组合物来治疗与GPR119G蛋白偶联受体的活性有关的疾病或病症的方法。

32. 发明申请

WO2012149236A1 NOVEL BICYCLIC NITROGEN CONTAINING HETEROARYL TGR5 RECEPTOR MODULATORS 审中-公开
标题翻译：新型双相含氮异氰酸酯TGR5受体调节剂
公开(公告)号：WO2012149236A1
公开(公告)日：2012-11-01
申请号：PCT/US2012/035327
申请日：2012-04-27
申请人： BRISTOL-MYERS SQUIBB COMPANY , ROBL, Jeffrey A. , LI, Jun , KENNEDY, Lawrence J. , WALKER, Steven J. , WANG, Haixia , WASHBURN, William N. , AHMAD, Saleem , NGU, Khehyong
发明人： ROBL, Jeffrey A. , LI, Jun , KENNEDY, Lawrence J. , WALKER, Steven J. , WANG, Haixia , WASHBURN, William N. , AHMAD, Saleem , NGU, Khehyong
IPC分类号： C07D215/08 , C07D401/04 , C07D403/04 , C07D413/04 , C07D417/04 , A61K31/4709 , A61K31/553 , A61K31/554 , A61P3/00 , A61P9/00 , C07D401/14 , C07D413/14
CPC分类号： C07D401/04 , A61K31/47 , A61K31/4709 , A61K31/473 , A61K31/4747 , A61K31/496 , A61K31/506 , A61K31/5377 , A61K31/5415 , A61K31/55 , A61K31/553 , A61K31/554 , A61K31/675 , A61K45/06 , C07D215/08 , C07D221/16 , C07D401/12 , C07D401/14 , C07D403/04 , C07D405/14 , C07D409/14 , C07D413/04 , C07D413/14 , C07D417/04 , C07F9/60
摘要： Novel compounds of Formula I:or an enantiomer, diastereomer, tautomer, prodrug or salt thereof, wherein m, Q, T, U, V, ring A, X, Y, R 3 , R 4 , R 4a , R 5a , R 5b , R 5c , R 5d , R 5e , R 6a , R 6b , and R 6c are defined herein, are provided which are TGR5 G protein-coupled receptor modulators. TGR5 G protein-coupled receptor modulators are useful in treating, preventing, or slowing the progression of diseases requiring TGR5 G protein-coupled receptor modulator therapy. Thus, the disclosure also concerns compositions comprising these novel compounds and methods of treating diseases or conditions related to the activity of the TGR5 G protein-coupled receptor by using any of these novel compounds or a composition comprising any of such novel compounds.
摘要翻译：式I的新型化合物或其对映体，非对映体，互变异构体，前药或其盐，其中m，Q，T，U，V，环A，X，Y，R 3，R 4，R 4a，R 5a，R 5b，R 5c，本文定义的R5e，R6a，R6b和R6c是TGR5G蛋白偶联受体调节剂。 TGR5G蛋白偶联受体调节剂可用于治疗，预防或减缓需要TGR5G蛋白偶联受体调节剂治疗的疾病进展。因此，本公开还涉及包含这些新化合物的组合物和通过使用任何这些新化合物或包含任何这些新化合物的组合物来治疗与TGR5G蛋白偶联受体的活性有关的疾病或病症的方法。

33. 发明申请

WO2010009183A1 PYRIDONE AND PYRIDAZONE ANALOGUES AS GPR119 MODULATORS 审中-公开
标题翻译：吡咯烷酮和吡咯烷酮类似物作为GPR119调节剂
公开(公告)号：WO2010009183A1
公开(公告)日：2010-01-21
申请号：PCT/US2009/050618
申请日：2009-07-15
申请人： BRISTOL-MYERS SQUIBB COMPANY , WACKER, Dean, A. , ROSSI, Karen, A. , WANG, Ying , WU, Gang
发明人： WACKER, Dean, A. , ROSSI, Karen, A. , WANG, Ying , WU, Gang
IPC分类号： C07D401/12 , C07D401/14 , C07D413/14 , A61K31/4545 , A61P3/10 , A61P3/00 , A61P3/04 , A61P3/06 , A61P9/10 , A61P9/12 , A61P19/08 , A61P25/02 , A61P25/28 , A61P31/00 , A61P35/00
CPC分类号： C07D403/14 , A61K31/4545 , A61K31/501 , A61K31/506 , A61K45/06 , C07D401/12 , C07D401/14 , C07D403/12 , C07D413/14
摘要： Novel compounds of structure Formula (I) or an enantiomer, a diastereomer, or a pharmaceutically acceptable salt thereof, wherein Z, R 1 , R 2 , R 21 , T 1 , T 2 , T 3 and T 4 are defined herein, are provided which are GPR119 G protein-coupled receptor modulators. GPR119 G protein-coupled receptor modulators are useful in treating, preventing, or slowing the progression of diseases requiring GPR119 G protein-coupled receptor modulator therapy. Thus, the disclosure also concerns compositions comprising these novel compounds and methods of treating diseases or conditions related to the activity of the GPR119 G protein-coupled receptor by using any of these novel compounds or a composition comprising any of such novel compounds.
摘要翻译：其中Z，R1，R2，R21，T1，T2，T3和T4在本文中定义的结构式（I）的新型化合物或其对映异构体，非对映异构体或其药学上可接受的盐是GPR119G蛋白 - 偶联受体调节剂。 GPR119 G蛋白偶联受体调节剂可用于治疗，预防或减缓需要GPR119 G蛋白偶联受体调节剂治疗的疾病进展。因此，本公开还涉及包含这些新化合物的组合物以及通过使用任何这些新化合物或包含任何这些新化合物的组合物来治疗与GPR119G蛋白偶联受体的活性有关的疾病或病症的方法。

34. 发明申请

WO2009015164A2 ACYCLIC DERIVATIVES AS MODULATORS OF CHEMOKINE RECEPTOR ACTIVITY 审中-公开
标题翻译：作为化合物受体活性调节剂的交联衍生物
公开(公告)号：WO2009015164A2
公开(公告)日：2009-01-29
申请号：PCT/US2008/070801
申请日：2008-07-23
申请人： BRISTOL-MYERS SQUIBB COMPANY , GARDNER, Daniel S. , DUNCIA, John V. , HYNES, John , DHAR, T., G., Murali , CARTER, Percy H. , SANTELLA, Joseph B.
发明人： GARDNER, Daniel S. , DUNCIA, John V. , HYNES, John , DHAR, T., G., Murali , CARTER, Percy H. , SANTELLA, Joseph B.
CPC分类号： C07D401/12 , C07D211/52 , C07D405/12
摘要： The present application describes modulators of MIP-1α of formula (I) or stereoisomers or prodrugs or pharmaceutically acceptable salts thereof, wherein m, Q, T, W, Z, R 1, R 3 , R 4 , R 5 , R 5a and R 5b , are as defined herein. In addition, methods of treating and preventing inflammatory diseases such as asthma and allergic diseases, as well as autoimmune pathologies such as rheumatoid arthritis and atherosclerosis using the modulators of formula (I) are disclosed.
摘要翻译：本申请描述了式（I）的MIP-1a或其立体异构体或前药或其药学上可接受的盐的调节剂，其中m，Q，T，W，Z，R 1，R 3，R 4，R 5，R 5a和R 5b如上定义于此。此外，公开了使用式（I）的调节剂治疗和预防炎性疾病如哮喘和过敏性疾病以及类风湿性关节炎和动脉粥样硬化的自身免疫病态的方法。

35. 发明申请

WO2008070496A3 N- ( (3-BENZYL) -2, 2- (BIS-PHENYL) -PROPAN-1-AMINE DERIVATIVES AS CETP INHIBITORS FOR THE TREATMENT OF ATHEROSCLEROSIS AND CARDIOVASCULAR DISEASES 审中-公开
公开(公告)号：WO2008070496A3
公开(公告)日：2008-06-12
申请号：PCT/US2007/085733
申请日：2007-11-28
申请人： BRISTOL-MYERS SQUIBB COMPANY , SALVATI, Mark E. , JOHNSON, James A. , XU, Ningning
发明人： SALVATI, Mark E. , JOHNSON, James A. , XU, Ningning
IPC分类号： C07C211/48 , C07C215/20 , C07C233/18 , C07C275/08 , C07C275/18 , C07C275/26 , C07D213/61 , C07D307/32 , C07D309/14 , A61K31/44 , A61K31/165 , A61K31/17 , A61K31/137 , A61P3/06 , A61P3/04
摘要： This present invention provides for cholesteryl ester transfer protein (CETP) inhibitors, of formula Ia and Ib / pharmaceutical compositions containing such inhibitors and the use of such inhibitors to elevate certain plasma lipid levels, including high density lipoprotein (HDL)-choIesterol and to lower certain other plasma lipid levels, such as low density lipoprotein (LDL)-cholesterol and triglycerides and accordingly to treat diseases which are affected by low levels of HDL cholesterol and/or high levels of LDL-cholesterol and triglycerides, such as atherosclerosis and cardiovascular diseases in certain mammals (i.e., those which have CETP in their plasma), including humans: wherein A, B, C, R 1 and R 14 are described herein.

36. 发明申请

WO2008042925A1 CYCLIC DERIVATIVES AS MODULATORS OF CHEMOKINE RECEPTOR ACTIVITY 审中-公开
标题翻译：作为化合物受体活性的调节剂的循环衍生物
公开(公告)号：WO2008042925A1
公开(公告)日：2008-04-10
申请号：PCT/US2007/080238
申请日：2007-10-03
申请人： BRISTOL-MYERS SQUIBB COMPANY , CARTER, Percy H. , CORNELIUS, Lyndon A., M.
发明人： CARTER, Percy H. , CORNELIUS, Lyndon A., M.
IPC分类号： C07D401/06 , C07D401/14 , C07D417/14 , A61K31/4525 , A61K31/454 , A61K31/4545 , A61P29/00 , A61P37/00 , A61P19/02
CPC分类号： C07D401/14 , C07D401/06 , C07D405/14 , C07D417/14
摘要： The present application describes modulators of MIP-1α of formula (I), or stereoisomers or prodrugs or pharmaceutically acceptable salts thereof, wherein n, A, T, R 1 , R 2 and R 8 , are as defined herein. In addition, methods of treating and preventing inflammatory diseases such as asthma and allergic diseases, as well as autoimmune pathologies such as rheumatoid arthritis and atherosclerosis using the modulators of formula (I) are disclosed.
摘要翻译：本申请描述了式（I）的MIP-1a或其立体异构体或前药或其药学上可接受的盐的调节剂，其中n，A，T，R 1，R 2 和R 8'如本文所定义。此外，公开了使用式（I）的调节剂治疗和预防炎性疾病如哮喘和过敏性疾病以及类风湿性关节炎和动脉粥样硬化的自身免疫病态的方法。

37. 发明申请

WO2008006044A2 SUBSTITUTED ACID DERIVATIVES USEFUL AS ANTIDIABETIC AND ANTIOBESITY AGENTS AND METHOD 审中-公开
标题翻译：用作抗糖尿病药和抗衰老药的取代酸衍生物和方法
公开(公告)号：WO2008006044A2
公开(公告)日：2008-01-10
申请号：PCT/US2007/072897
申请日：2007-07-06
申请人： BRISTOL-MYERS SQUIBB COMPANY , CHENG, Peter T.w. , CHEN, Sean , QIAN, Xinhua , DESHPANDE, Rajendra P. , TANG, Erqing
发明人： CHENG, Peter T.w. , CHEN, Sean , QIAN, Xinhua , DESHPANDE, Rajendra P. , TANG, Erqing
IPC分类号： C07D263/32 , A61K31/421 , A61P1/04 , A61P3/10 , A61P9/10 , A61P17/06 , A61P19/10
CPC分类号： C07D263/32
摘要： Compounds are provided which have the structure of Formula (I): wherein R is hydrogen or C1-C4 alkyl; and each of R1 and R2 is independently hydrogen, C1-C4 alkyl, halo or C1-C4 alkoxy, and salts thereof, which compounds are useful as antidiabetic, hypolipidemic, and antiobesity agents.
摘要翻译：提供了具有式（I）结构的化合物：其中R为氢或C 1 -C 4烷基; 并且每个R 1和R 2独立地为氢，C 1 -C 4烷基，卤代或C 1 -C 4烷氧基及其盐，所述化合物可用作抗糖尿病药，降血脂药和抗肥胖症药。

38. 发明申请

WO2008006043A3 1,3-OXAZOLE DERIVATIVES USEFUL AS ANTI-ATHEROSCLEROTIC, ANTI-DYSLIPIDEMIC, ANTI-DIABETIC AND ANTI-OBESITY AGENTS 审中-公开
公开(公告)号：WO2008006043A3
公开(公告)日：2008-01-10
申请号：PCT/US2007/072891
申请日：2007-07-06
申请人： BRISTOL-MYERS SQUIBB COMPANY , TINO, Joseph, A. , CHENG, Peter, T.W. , SHI, Yan , LI, Jun , MUKHERJEE, Ranjan
发明人： TINO, Joseph, A. , CHENG, Peter, T.W. , SHI, Yan , LI, Jun , MUKHERJEE, Ranjan
IPC分类号： C07D263/32 , A61K31/421 , A61P3/00
摘要： Compounds are provided which have the structure of Formula (I): wherein R1 is halogen; and X is hydrogen or halogen, and salts thereof, which compounds are useful as anti-atherosclerotic, anti-dyslipidemic, anti-diabetic, and anti-obesity agents.

39. 发明申请

WO2006113261A2 INHIBITORS OF 11-BETA HYDROXYSTEROID DEHYDROGENASE TYPE I 审中-公开
标题翻译： 11-羟基脱氢酶脱氢酶I型抑制剂
公开(公告)号：WO2006113261A2
公开(公告)日：2006-10-26
申请号：PCT/US2006/013610
申请日：2006-04-12
申请人： BRISTOL-MYERS SQUIBB COMPANY , LI, James, J. , HAMANN, Lawrence, G. , RUAN, Zheming , COOPER, Christopher, B. , WU, Shung, C. , SIMPKINS, Ligaya, M. , WANG, Haixia , NAYEEM, Akbar , KRYSTEK, Stanley, R., Jr.
发明人： LI, James, J. , HAMANN, Lawrence, G. , RUAN, Zheming , COOPER, Christopher, B. , WU, Shung, C. , SIMPKINS, Ligaya, M. , WANG, Haixia , NAYEEM, Akbar , KRYSTEK, Stanley, R., Jr.
IPC分类号： C07D401/12 , C07D401/14 , C07D401/04 , A61K31/444
CPC分类号： C07D213/70 , A61K31/421 , A61K31/426 , A61K31/4439 , A61K31/4965 , A61K31/497 , A61K31/506 , C07D213/71 , C07D213/81 , C07D213/82 , C07D401/04 , C07D401/06 , C07D401/12 , C07D401/14 , C07D405/04 , C07D405/14 , C07D409/04 , C07D413/14 , C07D487/04 , C07D487/08
摘要： Novel compounds are provided which are 11-beta-hydroxysteroid dehydrogenase type I inhibitors. 11-beta-hydroxysteroid dehydrogenase type I inhibitors are useful in treating, preventing, or slowing the progression of diseases requiring 11-beta-hydroxysteroid dehydrogenase type I inhibitor therapy. These novel compounds have the structure: (I) or stereoisomers or prodrugs or pharmaceutically acceptable salts thereof, wherein G, L, Q, Z, R 6 , R 7 , and R 8 are defined herein.
摘要翻译：提供了新的化合物，其为11-β-羟基类固醇脱氢酶I型抑制剂。 11-β-羟基类固醇脱氢酶I型抑制剂可用于治疗，预防或减缓需要11-β-羟基类固醇脱氢酶I型抑制剂治疗的疾病进展。这些新化合物具有以下结构：（I）或其立体异构体或前药或其药学上可接受的盐，其中G，L，Q，Z，R 6，R 7和本文定义R 8。

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