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1. 发明申请

WO2006044362A3 N-SULFONYLPIPERIDINE CANNABINOID RECEPTOR 1 ANTAGONISTS 审中-公开
公开(公告)号：WO2006044362A3
公开(公告)日：2006-04-27
申请号：PCT/US2005/036498
申请日：2005-10-12
申请人： BRISTOL-MYERS SQUIBB COMPANY , SHER, Philip, M. , WU, Gang , EWING, William, R.
发明人： SHER, Philip, M. , WU, Gang , EWING, William, R.
IPC分类号： A61K31/445 , A61K31/535 , C07D211/26 , C07D215/00 , C07D217/00 , C07D401/12 , C07D413/12 , C07D419/12
摘要： The present application describes compounds according to Formula (I), wherein R 1 , R 2 , R 3 , R 4 , X and Y are described herein. Additionally, the present application describes pharmaceutical compositions comprising at least one compound according to Formula I and optionally one or more additional therapeutic agents. Finally, the present application describes methods of treatment using the compounds according to Formula (I) both alone and in combination with one or more additional therapeutic agents.

2. 发明申请

WO2005063761A1 AZABICYCLIC HETEROCYCLES AS CANNABINOID RECEPTOR MODULATORS 审中-公开
标题翻译：作为CANNABINOID受体调节剂的偶氮异构体
公开(公告)号：WO2005063761A1
公开(公告)日：2005-07-14
申请号：PCT/US2004/042820
申请日：2004-12-17
申请人： BRISTOL-MYERS SQUIBB COMPANY , YU, Guixue , EWING, William, R. , MIKKILINENI, Amarendra, B. , PENDRI, Annapurna , SHER, Philip, M. , GERRITZ, Samuel , ELLSWORTH, Bruce, A. , WU, Gang , HUANG, Yanting , SUN, Chongqing , MURUGESAN, Natesan , GU, Zhengxiang , WANG, Ying , SITKOFF, Doree , JOHNSON, Stephen, R. , WU, Ximao
发明人： YU, Guixue , EWING, William, R. , MIKKILINENI, Amarendra, B. , PENDRI, Annapurna , SHER, Philip, M. , GERRITZ, Samuel , ELLSWORTH, Bruce, A. , WU, Gang , HUANG, Yanting , SUN, Chongqing , MURUGESAN, Natesan , GU, Zhengxiang , WANG, Ying , SITKOFF, Doree , JOHNSON, Stephen, R. , WU, Ximao
IPC分类号： C07D487/04
CPC分类号： C07D487/04
摘要： The present application describes compounds according to Formula (I), pharmaceutical compositions comprising at least one compound according to Formula (I) and optionally one or more additional therapeutic agents and methods of treatment using the compounds according to Formula (I) both alone and in combination with one or more additional therapeutic agents. The compounds have the general Formula (I) including all prodrugs, pharmaceutically acceptable salts and stereoisomers, R 1 , R 2 , R 3 , R 6 , R 7 , m and n are described herein.
摘要翻译：本申请描述了根据式（I）的化合物，包含至少一种根据式（I）的化合物和任选的一种或多种另外的治疗剂的药物组合物和使用根据式（I）的化合物单独和与一种或多种另外的治疗剂组合。化合物具有通式（I），其包括所有前药，药学上可接受的盐和立体异构体，R 1，R 2，R 3，R 6，R 7，m和n在本文中描述。

3. 发明申请

WO2005063762A1 AZABICYCLIC HETEROCYCLES AS CANNABINOID RECEPTOR MODULATORS 审中-公开
标题翻译：作为CANNABINOID受体调节剂的偶氮异构体
公开(公告)号：WO2005063762A1
公开(公告)日：2005-07-14
申请号：PCT/US2004/042878
申请日：2004-12-17
申请人： BRISTOL-MYERS SQUIBB COMPANY , GU, Guixue , EWING, William, R. , MIKKILINENI, Amarendra, B. , PENDRI, Annapurna , ELLSWORTH, Bruce, A. , SHER, Philip, M. , GERRITZ, Samuel , SUN, Chongqing , MURUGESAN, Natesan , WU, Ximao
发明人： GU, Guixue , EWING, William, R. , MIKKILINENI, Amarendra, B. , PENDRI, Annapurna , ELLSWORTH, Bruce, A. , SHER, Philip, M. , GERRITZ, Samuel , SUN, Chongqing , MURUGESAN, Natesan , WU, Ximao
IPC分类号： C07D487/04
CPC分类号： C07D487/04
摘要： The present application describes compounds according to Formula I, pharmaceutical compositions comprising at least one compound according to Formula I and optionally one or more additional therapeutic agents and methods of treatment using the compounds according to Formula I both alone and in combination with one or more additional therapeutic agents. The compounds have the general Formula I. including all prodrugs, pharmaceutically acceptable salts and stereoisomers, R 1 , R 2 , R 3 , R 4 , R 5 , m and n are described herein.
摘要翻译：本申请描述了根据式I的化合物，包含至少一种根据式I的化合物和任选的一种或多种另外的治疗剂的药物组合物和使用根据式I的化合物的治疗方法，其单独和与一种或多种另外的治疗剂。该化合物具有通式I.包括所有前药，药学上可接受的盐和立体异构体，R 1，R 2，R 3，R 4，R 5，m和n如本文所述。

4. 发明申请

WO2006138734A1 TRIAZOLOPYRIMIDINE CANNABINOID RECEPTOR 1 ANTAGONISTS 审中-公开
标题翻译：三氮唑嘧啶卡那霉素受体1拮抗剂
公开(公告)号：WO2006138734A1
公开(公告)日：2006-12-28
申请号：PCT/US2006/023934
申请日：2006-06-19
申请人： BRISTOL-MYERS SQUIBB COMPANY , WU, Gang , MIKKILINENI, Amarendra, B. , SHER, Philip, M. , MURUGESAN, Natesan , GU, Zhengxiang
发明人： WU, Gang , MIKKILINENI, Amarendra, B. , SHER, Philip, M. , MURUGESAN, Natesan , GU, Zhengxiang
IPC分类号： C07D487/04 , A61K31/519 , A61P3/00
CPC分类号： C07D487/04
摘要： The present application describes compounds according to both Formulas (I) and (II), pharmaceutical compositions comprising at least one compound according to either Formula (I) or (II) and optionally one or more additional therapeutic agents, and methods of treatment using the compounds according to Formulas (I) and (II) both alone and in combination with one or more additional therapeutic agents. The compounds have the following general formulas: (I), (II) including all prodrugs, solvates, pharmaceutically acceptable salts and stereoisomers, wherein R 1 , R 2 , R 3 , R 4 and R 5 are described herein.
摘要翻译：本申请描述了根据式（I）和（II）两者的化合物，包含至少一种根据式（I）或（II）的化合物和任选的一种或多种另外的治疗剂的药物组合物，以及使用单独的和与一种或多种另外的治疗剂组合的根据式（I）和（II）的化合物。所述化合物具有以下通式：（I），（II），其包括所有前药，溶剂合物，药学上可接受的盐和立体异构体，其中R 1，R 2，R 2，本文描述了SUP 3，R 4和R 5。

5. 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。

6. 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。

7. 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。

8. 发明申请

WO1997037646A1 CATECHOLAMINE SURROGATES USEFUL AS 'beta'3 AGONISTS 审中-公开
标题翻译： CATECHOLAMINE SURROGATES有用作β3激动剂
公开(公告)号：WO1997037646A1
公开(公告)日：1997-10-16
申请号：PCT/US1997005324
申请日：1997-04-01
申请人： BRISTOL-MYERS SQUIBB COMPANY
发明人： BRISTOL-MYERS SQUIBB COMPANY , CHENG, Peter, T., W. , BISACCHI, Gregory, S. , GAVAI, Ashvinikumar, V. , POSS, Kathleen, M. , RYONO, Denis, E. , SHER, Philip, M. , SUN, Chong-Qing , WASHBURN, William, N.
IPC分类号： A61K31/18
CPC分类号： C07C311/46 , C07C311/08 , C07C311/39 , C07D263/32 , C07D277/28 , C07F9/4056
摘要： Compounds of formula (I) and pharmaceutically acceptable salts thereof. As used in formula (I), and throughout the specification, the symbols have the following meanings: R is lower alkyl, aryl or arylalkyl; R is hydrogen, hydroxyl, hydroxymethyl or halogen; R is hydrogen or alkyl; R and R are independently hydrogen, alkoxy, alkoxymethyl, hydroxyl, -CN, -CON(R )R 2 , -N(R )R , -NR COR , -NR SO2R ; or R and R may together with the carbon atoms to which they are bonded form a heterocycle; R , R and R are independently A or B, wherein A is hydrogen, alkyl, cylcoalkyl, halogen, hydroxyl, aryl, alkoxy, cyano, -SR , -SOR , -SO2R , -N(R )R , -NR COR , -OCH2CON(R )R , -OCH2CO2R , CON(R )R , -CO2R ; and B is -(CH2)nN(R )R , -(CH2)mPO(OR )OR , -(CH2)nNR COR , -O-aryl, -OCH2CH2N(R )R , -COR , -SO2N(R )R , -NR CO2R , -NR CO(N(R )R ), heterocycle or -R and R may together with the carbon atoms to which they are bonded form a heterocycle, provided that at least one of R , R and R is B; R and R are independently hydrogen or lower alkyl; R is lower alkyl; R is hydrogen, lower alkyl, aryl or arylalkyl; m is an integer of 0 to 6; and n is an integer of 1 to 6. These compounds are beta three adrenergic receptor agonists and are useful, therefore for example, in the treatment of diabetes, obesity and gastrointestinal diseases.
摘要翻译：式（I）化合物及其药学上可接受的盐。在式（I）中使用，并且在整个说明书中，符号具有以下含义：R 1是低级烷基，芳基或芳基烷基; R 2是氢，羟基，羟甲基或卤素; R 3是氢或烷基; R 4和R 4独立地是氢，烷氧基，烷氧基甲基，羟基，-CN，-CON（R 6）R 6'，-CO 2，R 6， R 6）R 6，-NR 6 COR 8，-NR 6 SO 2 R 1; 或R 4和R 4'可以与它们所键合的碳原子一起形成杂环; R 5，R 5和R 5独立地是A或B，其中A是氢，烷基，环烷基，卤素，羟基，芳基，烷氧基，氰基，-SR 7，-SOR -SO 2 R 7，-N（R 6）R 6'，-NR 6 COR 8，-OCH 2 CON（R 6）R 6，-OCH 2 CO 2 R CON（R 6）R 6，-CO 2 R 6; 并且B是 - （CH 2）n N（R 6）R 6'， - （CH 2）m PO（OR 6）OR 6， - （CH 2）n NR 6 COR 8， -O-芳基，-OCH 2 CH 2 N（R 6）R 6'，-COR 7，-SO 2 N（R 6）R 6'，-NR 6 CO 2 R 7， NR 6 CO（N（R 6）R 6'），杂环或-R 5和R 5可以与它们所键合的碳原子一起形成杂环，条件是 R 5，R 5'和R 5“中的至少一个是B; R 6和R 6独立地是氢或低级烷基; R 7是低级烷基; R 8是氢，低级烷基，芳基或芳基烷基; m为0〜6的整数。并且n是1至6的整数。这些化合物是β三肾上腺素能受体激动剂，因此可用于例如糖尿病，肥胖症和胃肠道疾病的治疗。

9. 发明授权

EP1268502B1 O-ARYL GLUCOSIDE SGLT2 INHIBITORS AND METHOD 有权
标题翻译： O-葡萄糖苷SGLT2抑制剂和方法芳
公开(公告)号：EP1268502B1
公开(公告)日：2006-02-01
申请号：EP01922840.2
申请日：2001-03-29
申请人： Bristol-Myers Squibb Company
发明人： WASHBURN, William, N. , SHER, Philip, M. , WU, Gang
IPC分类号： C07H15/203 , A61K31/7034 , A61P7/12
CPC分类号： C07H15/203 , C40B40/00
摘要： Formula (I) wherein Y is formula (a) or heteroaryl; A is -O(CH2)m, S, -NH(CH2)m, or (CH2)n where n is 0-3 and m is 0-2; and R1 to R6 are as defined herein. 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 one, two or more other antidiabetic agents, and/or one, two or more hypolipidemic agents.

10. 发明授权

EP1697370B1 AZABICYCLIC HETEROCYCLES AS CANNABINOID RECEPTOR MODULATORS 有权
标题翻译：氮杂双环杂环做大麻素受体调节剂
公开(公告)号：EP1697370B1
公开(公告)日：2007-04-25
申请号：EP04814952.0
申请日：2004-12-17
申请人： Bristol-Myers Squibb Company
发明人： YU, Guixue , EWING, William, R. , MIKKILINENI, Amarendra, B. , PENDRI, Annapurna , SHER, Philip, M. , GERRITZ, Samuel , ELLSWORTH, Bruce, A. , WU, Gang , HUANG, Yanting , SUN, Chongqing , MURUGESAN, Natesan , GU, Zhengxiang , WANG, Ying , SITKOFF, Doree , JOHNSON, Stephen, R. , WU, Ximao
IPC分类号： C07D487/04 , A61K31/5025 , A61P37/02 , A61P25/16
CPC分类号： C07D487/04
摘要： The present application describes compounds according to Formula (I), pharmaceutical compositions comprising at least one compound according to Formula (I) and optionally one or more additional therapeutic agents and methods of treatment using the compounds according to Formula (I) both alone and in combination with one or more additional therapeutic agents. The compounds have the general Formula (I) including all prodrugs, pharmaceutically acceptable salts and stereoisomers, R1, R2, R3, R6, R7, m and n are described herein.

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