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1. 发明申请

WO2006055462A1 2-AMINO-4-FUNCTIONALIZED TETRALIN DERIVATIVES AND RELATED GLYCOGEN PHOSPHORYLASE INHIBITORS 审中-公开
标题翻译： 2-氨基-4-功能化四氢萘衍生物和相关的GLYCOGEN磷酸酶抑制剂
公开(公告)号：WO2006055462A1
公开(公告)日：2006-05-26
申请号：PCT/US2005/041096
申请日：2005-11-14
申请人： BRISTOL-MYERS SQUIBB COMPANY , SHER, Philip, M. , NIRSCHL, Alexandra, A. , MENG, Wei , WASHBURN, William, N.
发明人： SHER, Philip, M. , NIRSCHL, Alexandra, A. , MENG, Wei , WASHBURN, William, N.
IPC分类号： C07D209/42 , C07D403/12 , C07D401/12 , C07D401/14 , A61K31/404 , A61K31/435 , A61K31/41 , A61K31/4439 , A61K31/454
CPC分类号： C07D401/12 , C07D209/42 , C07D403/12
摘要： Novel compounds are provided which are glycogen phosphorylase inhibitors which are useful in treating, preventing or slowing the progression of diseases requiring glycogen phosphorylase inhibitor therapy such as diabetes and related conditions (such as hyperglycemia, impaired glucose tolerance, insulin resistance and hyperinsulinemia), the microvascular complications associated with diabetes (such as retinopathy, neuropathy, nephropathy and delayed wound healing), the macrovascular complications associated with diabetes (cardiovascular diseases such as atherosclerosis, abnormal heart function, myocardial ischemia and stroke), as well as Metabolic Syndrome and its component conditions including hypertension, obesity and dislipidemia (including hypertriglyceridemia, hypercholesterolemia and low HDL), and other maladies such as non-cardiac ischemia, infection and cancer. These novel compounds have the structure [INSERT CHEMICAL STRUCTURE HERE] I or stereoisomers or prodrugs or pharmaceutically acceptable salts thereof, wherein W, R1, R2, X and Z are defined herein.
摘要翻译：提供了新型化合物，其是可用于治疗，预防或减缓需要糖原磷酸化酶抑制剂治疗（如糖尿病和相关病症（如高血糖，葡萄糖耐量异常，胰岛素抵抗和高胰岛素血症））的疾病进展的糖原磷酸化酶抑制剂，微血管与糖尿病相关的并发症（如视网膜病变，神经病变，肾病和延迟伤口愈合），与糖尿病相关的大血管并发症（心血管疾病如动脉粥样硬化，心脏功能异常，心肌缺血和中风）以及代谢综合征及其组成条件包括高血压，肥胖和血脂异常（包括高甘油三酯血症，高胆固醇血症和低HDL）以及其他疾病如非心脏缺血，感染和癌症。这些新化合物具有[INSERT CHEMICAL STRUCTURE HERE] I或其立体异构体或前药或其药学上可接受的盐，其中W，R1，R2，X和Z如本文所定义。

2. 发明申请

WO2006055463A2 2-AMINO-3-FUNCTIONALIZED TETRALIN DERIVATIVES AND RELATED GLYCOGEN PHOSPHORYLASE INHIBITORS 审中-公开
标题翻译： 2-氨基-3-功能化的四环素衍生物和相关的GLYCOGEN磷酸酶抑制剂
公开(公告)号：WO2006055463A2
公开(公告)日：2006-05-26
申请号：PCT/US2005/041098
申请日：2005-11-14
申请人： BRISTOL-MYERS SQUIBB COMPANY , SHER, Philip M. , WU, Gang , MENG, Wei , NIRSCHL, Alexandra, A. , WASHBURN, William, N. , STOUCH, Terry
发明人： SHER, Philip M. , WU, Gang , MENG, Wei , NIRSCHL, Alexandra, A. , WASHBURN, William, N. , STOUCH, Terry
IPC分类号： C07D209/42 , C07D493/08 , C07D405/12 , C07D403/12 , C07D401/12 , A61K31/404 , A61K31/435 , A61K31/4439 , A61K31/454 , A61K31/55
CPC分类号： C07D209/42 , C07D235/24 , C07D401/12 , C07D403/12 , C07D405/12 , C07D491/04 , C07D493/08 , C07D495/04
摘要： Novel compounds are provided which are glycogen phosphorylase inhibitors which are useful in treating, preventing or slowing the progression of diseases requiring glycogen phosphorylase inhibitor therapy such as diabetes and related conditions (such as hyperglycemia, impaired glucose tolerance, insulin resistance and hyperinsulinemia), the microvascular complications associated with diabetes (such as retinopathy, neuropathy, nephropathy and delayed wound healing), the macrovascular complications associated with diabetes (cardiovascular diseases such as atherosclerosis, abnormal heart function, myocardial ischemia and stroke), as well as Metabolic Syndrome and its component conditions including hypertension, obesity and dislipidemia (including hypertriglyceridemia, hypercholesterolemia and low HDL), and other maladies such as non-cardiac ischemia, infection and cancer. These novel compounds have the structure [INSERT CHEMICAL STRUCTURE HERE] I or stereoisomers or prodrugs or pharmaceutically acceptable salts thereof, wherein W, R1, R2, X and Z are defined herein.
摘要翻译：提供了新型化合物，其是可用于治疗，预防或减缓需要糖原磷酸化酶抑制剂治疗（如糖尿病和相关病症（如高血糖，葡萄糖耐量异常，胰岛素抵抗和高胰岛素血症））的疾病进展的糖原磷酸化酶抑制剂，微血管与糖尿病相关的并发症（如视网膜病变，神经病变，肾病和延迟伤口愈合），与糖尿病相关的大血管并发症（心血管疾病如动脉粥样硬化，心脏功能异常，心肌缺血和中风）以及代谢综合征及其组成条件包括高血压，肥胖和血脂异常（包括高甘油三酯血症，高胆固醇血症和低HDL）以及其他疾病如非心脏缺血，感染和癌症。这些新化合物具有[INSERT CHEMICAL STRUCTURE HERE] I或其立体异构体或前药或其药学上可接受的盐，其中W，R1，R2，X和Z如本文所定义。

3. 发明申请

WO2003099836A1 C-ARYL GLUCOSIDE SGLT2 INHIBITORS AND METHOD 审中-公开
标题翻译： C-ARYL GLUCOSIDE SGLT2抑制剂和方法
公开(公告)号：WO2003099836A1
公开(公告)日：2003-12-04
申请号：PCT/US2003/015591
申请日：2003-05-15
申请人： BRISTOL-MYERS SQUIBB COMPANY , ELLSWORTH, Bruce , WASHBURN, William, N. , SHER, Philip, M. , WU, Gang , MENG, Wei
发明人： ELLSWORTH, Bruce , WASHBURN, William, N. , SHER, Philip, M. , WU, Gang , MENG, Wei
IPC分类号： C07H7/04
CPC分类号： C07C43/225 , A61K31/70 , A61K31/7034 , A61K45/06 , C07C45/46 , C07C49/84 , C07H7/04 , C07H15/203 , A61K2300/00
摘要： An SGLT2 inhibiting compound is provided having the formula[Chemical structure] A method is also provided for treating diabetes and related diseases employing an SGLT2 inhibiting amount of the above compound alone or in combination with another antidiabetic agent or other therapeutic agent.
摘要翻译：提供了具有下式的SGLT2抑制化合物[化学结构]还提供了一种用于治疗糖尿病和相关疾病的方法，其使用单独的SGLT2抑制量的上述化合物或与另一种抗糖尿病剂或其它治疗剂组合。

4. 发明申请

WO2006055435A1 2-AMINONAPHTHALENE DERIVATIVES AND RELATED GLYCOGEN PHOSPHORYLASE INHIBITORS 审中-公开
标题翻译： 2-氨基萘基衍生物和相关的GLYCOGEN磷酸酶抑制剂
公开(公告)号：WO2006055435A1
公开(公告)日：2006-05-26
申请号：PCT/US2005/040985
申请日：2005-11-14
申请人： BRISTOL-MYERS SQUIBB COMPANY , MENG, Wei , SHER, Philip, M. , ELLSWORTH, Bruce, A. , WASHBURN, William, N.
发明人： MENG, Wei , SHER, Philip, M. , ELLSWORTH, Bruce, A. , WASHBURN, William, N.
IPC分类号： C07D209/42 , A61K31/404 , A61P3/10
CPC分类号： C07D235/24 , C07D209/42 , C07D491/04 , C07D495/04
摘要： Novel compounds are provided which are glycogen phosphorylase inhibitors which are useful in treating, preventing or slowing the progression of diseases requiring glycogen phosphorylase inhibitor therapy such as diabetes and related conditions (such as hyperglycemia, impaired glucose tolerance, insulin resistance and hyperinsulinemia), the microvascular complications associated with diabetes (such as retinopathy, neuropathy, nephropathy and delayed wound healing), the macrovascular complications associated with diabetes (cardiovascular diseases such as atherosclerosis, abnormal heart function, myocardial ischemia and stroke), as well as Metabolic Syndrome and its component conditions including hypertension, obesity and dislipidemia (including hypertriglyceridemia, hypercholesterolemia and low HDL), and other maladies such as non-cardiac ischemia, infection and cancer. These novel compounds have the structure [PLEASE INSERT CHEMICAL STRUCTURE HERE] I or stereoisomers or prodrugs or pharmaceutically acceptable salts thereof, wherein W, R1 and R2 are defined herein.
摘要翻译：提供了新型化合物，其是可用于治疗，预防或减缓需要糖原磷酸化酶抑制剂治疗（如糖尿病和相关病症（如高血糖，葡萄糖耐量异常，胰岛素抵抗和高胰岛素血症））的疾病进展的糖原磷酸化酶抑制剂，微血管与糖尿病相关的并发症（如视网膜病变，神经病变，肾病和延迟伤口愈合），与糖尿病相关的大血管并发症（心血管疾病如动脉粥样硬化，心脏功能异常，心肌缺血和中风）以及代谢综合征及其组成条件包括高血压，肥胖和血脂异常（包括高甘油三酯血症，高胆固醇血症和低HDL）以及其他疾病如非心脏缺血，感染和癌症。这些新型化合物具有本文所定义的结构，即其中W，R 1和R 2的定义如下。

5. 发明申请

WO2004067482A2 SUBSTITUTED ANILIDE LIGANDS FOR THE THYROID RECEPTOR 审中-公开
标题翻译：用于甲状腺受体的替代辅助配体
公开(公告)号：WO2004067482A2
公开(公告)日：2004-08-12
申请号：PCT/US2004/001985
申请日：2004-01-23
申请人： BRISTOL-MYERS SQUIBB COMPANY , KARO BIO AB , WASHBURN, William, N. , MENG, Wei , RYONO, Denis, E. , ELLSWORTH, Bruce, A. , ERICSSON, Thomas , RAHIMI- GHADIM, Mahmoud , GARG, Neeraj , MALM, Johan
发明人： WASHBURN, William, N. , MENG, Wei , RYONO, Denis, E. , ELLSWORTH, Bruce, A. , ERICSSON, Thomas , RAHIMI- GHADIM, Mahmoud , GARG, Neeraj , MALM, Johan
IPC分类号： C07C
CPC分类号： A61K45/06 , A61K31/195 , A61K31/277 , A61K31/44 , C07C233/25 , A61K2300/00
摘要： Novel thyroid receptor ligands are provided having the general formula I wherein X, R 1 , R 2 , R 3 , R 4 , R 5 , R 6 , R 7 , R 8 , R 9 , R 10 , R 11 , R 12 . and R 13 are as defined herein. In addition, a method is provided for preventing, inhibiting or treating diseases or disorders associated with metabolic dysfunction or which are dependent upon the expression of a T 3 regulated gene, wherein a compound as described above is administered in a therapeutically effective amount.
摘要翻译：提供具有通式I的新型甲状腺受体配体，其中X，R 1，R 2，R 3，R 4，R 5，R 6，R 7，R 8，R 9，R 10，R 11，R 12。和R 13如本文所定义。此外，提供了一种用于预防，抑制或治疗与代谢功能障碍相关或依赖于T3调节基因的表达的疾病或病症的方法，其中如上所述的化合物以治疗有效量施用。

6. 发明申请

WO2004066929A2 CYCLOALKYL CONTAINING ANILIDE LIGANDS FOR THE THYROID RECEPTOR 审中-公开
标题翻译：含有THYROID受体的CYCLOALKYL含有辅助配体
公开(公告)号：WO2004066929A2
公开(公告)日：2004-08-12
申请号：PCT/US2004/001779
申请日：2004-01-23
申请人： BRISTOL-MYERS SQUIBB COMPANY , WASHBURN, William, N. , MENG, Wei
发明人： WASHBURN, William, N. , MENG, Wei
IPC分类号： A61K
CPC分类号： C07C233/60 , C07C2601/02 , C07C2601/04 , C07C2601/08 , C07C2601/14
摘要： Novel thyroid receptor ligands are provided having the general Formula (I) wherein X, R 1 , R 2 , R 3 , R 4 , R 5 , R 6 , R 7 , R 8 , R 9 , R 10 and R 11 , are as defined herein. In addition, a method is provided for preventing, inhibiting or treating diseases or disorders associated with metabolic dysfunction or which are dependent upon the expression of a T 3 regulated gene, wherein a compound as described above is administered in a therapeutically effective amount.
摘要翻译：提供具有通式（I）的新型甲状腺受体配体，其中X，R 1，R 2，R 3，R 4，R 5，R 6，R 7，R 8，R 9，R 10和R 11如本文所定义。此外，提供了一种用于预防，抑制或治疗与代谢功能障碍相关或依赖于T3调节基因的表达的疾病或病症的方法，其中如上所述的化合物以治疗有效量施用。

7. 发明申请

WO2006071762A3 PYRIMIDINE-BASED INHIBITORS OF DIPEPTIDYL PEPTIDASE IV AND METHODS 审中-公开
公开(公告)号：WO2006071762A3
公开(公告)日：2006-07-06
申请号：PCT/US2005/046750
申请日：2005-12-23
申请人： BRISTOL-MYERS SQUIBB COMPANY , MENG, Wei , HAMANN, Lawrence G. , BRIGANCE, Robert Paul
发明人： MENG, Wei , HAMANN, Lawrence G. , BRIGANCE, Robert Paul
IPC分类号： C07D239/26 , A61K31/505 , A61P3/10
摘要： Compounds are provided having the formula (I) wherein R, B, X and Y are as defined herein.

8. 发明申请

WO2011130459A1 NOVEL GLUCOKINASE ACTIVATORS AND METHODS OF USING SAME 审中-公开
标题翻译：新型GLUCOKINASE激活剂及其使用方法
公开(公告)号：WO2011130459A1
公开(公告)日：2011-10-20
申请号：PCT/US2011/032386
申请日：2011-04-14
申请人： BRISTOL-MYERS SQUIBB COMPANY , MENG, Wei , CHENG, Peter T. W.
发明人： MENG, Wei , CHENG, Peter T. W.
IPC分类号： C07D403/12 , C07D417/12 , A61P3/10 , A61P3/04
CPC分类号： C07D403/12 , C07D417/12
摘要： Compounds are provided which are activators of the enzyme glucokinase and thus are useful in treating diabetes and related diseases, which compounds have the structure wherein R 1 , R 2 , R 3 , R 4 , R 5 , R 6 , Y and X are as defined herein or a pharmaceutically acceptable salt thereof. A method for treating diabetes and related disease employing the above compounds is also provided.
摘要翻译：提供了作为葡糖激酶酶的激活剂并因此可用于治疗糖尿病和相关疾病的化合物，该化合物具有其中R 1，R 2，R 3，R 4，R 5，R 6，Y和X如本文所定义或其药学上可接受的结构的盐。还提供了使用上述化合物治疗糖尿病和相关疾病的方法。

9. 发明申请

WO2008005964A2 NOVEL GLUCOKINASE ACTIVATORS AND METHODS OF USING SAME 审中-公开
标题翻译：新型GLUCOKINASE激活剂及其使用方法
公开(公告)号：WO2008005964A2
公开(公告)日：2008-01-10
申请号：PCT/US2007/072708
申请日：2007-07-03
申请人： BRISTOL-MYERS SQUIBB COMPANY , RYONO, Dennis E. , CHENG, Peter T.W. , BOLTON, Scott A. , CHEN, Sean S. , SHI, Yan , MENG, Wei , TINO, Joseph A. , ZHANG, Hao , SULSKY, Richard B.
发明人： RYONO, Dennis E. , CHENG, Peter T.W. , BOLTON, Scott A. , CHEN, Sean S. , SHI, Yan , MENG, Wei , TINO, Joseph A. , ZHANG, Hao , SULSKY, Richard B.
IPC分类号： C07F9/32 , C07F9/40 , A61K31/675 , A61P3/00
CPC分类号： C07F9/6539 , C07F9/582 , C07F9/587 , C07F9/65032 , C07F9/650964 , C07F9/650982 , C07F9/65181
摘要： Compounds are provided which are phosphonate and phosphinate activators and thus are useful in treating diabetes and related diseases and have the structure of Formula (I), wherein Formula (II) is a heteroaryl ring; R 4 is -(CH 2 ) n -Z-(CH 2 ) m -PO(OR 7 )(OR 8 ), -(CH 2 ) n Z-(CH 2 ) m -PO(OR 7 )R 9 , -(CH 2 ) n -Z-(CH 2 ) m -OPO(OR 7 )R 9 , -(CH 2 ) n Z-(CH 2 ) m -OPO(R 9 )(R 10 ), or -(CH 2 ) n Z-(CH 2 ) m -PO(R 9 )(R 10 ); R 5 and R6 are independently selected from H, alkyl and halogen; Y is R 7 (CH 2 ) s or is absent; and X, n, Z, m, R 4 , R 5 , R 6 , R 7 , and s are as defined herein; or a pharmaceutically acceptable salt thereof. A method for treating diabetes and related diseases employing the above compounds is also provided.
摘要翻译：提供了膦酸酯和次膦酸酯活化剂的化合物，因此可用于治疗糖尿病和相关疾病，并具有式（I）的结构，其中式（II）是杂芳基环; R 4是 - （CH 2 CH 2）n - （CH 2）n - （OR 7）（OR 8）， - （CH 2 CH 2）n - Z - （ CH 2 OR 2（OR 7）R 9， - （CH 2 CH 2） SUB>）_{名词 -Z-（CH _{2 ）_{米 -OPO（OR _{7 ）R _{9 - （CH 2）n - Z - （CH 2）2 - （O） - （CH 2）n - （R 10），或 - （CH 2）n - Z - （CH 2） 2 ）_{米 -PO（R _{9 ）（R _{10 ）; R 5和R 6独立地选自H，烷基和卤素; Y是R 7（CH 2）2，或不存在; 和X，n，Z，m，R 4，R 5，R 6，R 7，和 s如本文所定义; 或其药学上可接受的盐。还提供了使用上述化合物治疗糖尿病和相关疾病的方法。}}}}}}}}

10. 发明申请

WO2006071752A1 AZOLOPYRIMIDINE-BASED INHIBITORS OF DIPEPTIDYL PEPTIDASE IV AND METHODS 审中-公开
标题翻译：脯氨酸酯酶基于四氢嘧啶基的抑制剂及其方法
公开(公告)号：WO2006071752A1
公开(公告)日：2006-07-06
申请号：PCT/US2005/046706
申请日：2005-12-23
申请人： BRISTOL-MYERS SQUIBB COMPANY , MENG, Wei , HAMANN, Lawrence G. , BRIGANCE, Robert Paul
发明人： MENG, Wei , HAMANN, Lawrence G. , BRIGANCE, Robert Paul
IPC分类号： C07D487/04 , A61K31/437 , A61P3/10
CPC分类号： C07D487/04
摘要： Compounds are provided having the formula (I): Formula (I) wherein R, X, Y, A and n are as defined herein.
摘要翻译：提供具有式（I）的化合物：式（I）其中R，X，Y，A和n如本文所定义。

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