公开(公告)号：US07057046B2

公开(公告)日：2006-06-06

申请号：US10440851

申请日：2003-05-19

申请人： Philip Sher ,  Gang Wu ,  Terry Stouch ,  Bruce Ellsworth

发明人： Philip Sher ,  Gang Wu ,  Terry Stouch ,  Bruce Ellsworth

IPC分类号： C07D403/12 ,  C07D471/04 ,  C07D491/048 ,  C07D495/04 ,  C07D519/00

CPC分类号： C07D401/12 ,  A61K31/496 ,  A61K31/5377 ,  A61K31/541 ,  A61K45/06 ,  C07D209/42 ,  C07D403/12 ,  C07D403/14 ,  C07D413/12 ,  C07D417/12 ,  C07D471/04 ,  C07D513/04 ,  A61K2300/00

摘要： A compound of formula I wherein W is a bicyclic hetroaryl of the structure X is —O—, —S—, —SO2—, —CHR5—, —CHR5O—, —CHR5S—, —CHR5SO2—, —CHR5CO— or —CH2CHR5—; Y is a bond or —CHR6—; Z is an aryl or heteroaryl group of the following structure: A is —CH— or —N—; B is —O— or —S—; and R1, R2, R3, R4, R5, R6, R7 and R8 are as described herein. Further provided is a method for treating diabetes and related diseases employing a glycogen phosphorylase inhibiting amount of the above compound, either alone or in combination with another therapeutic agent.

摘要翻译： 其中W是结构X的双环杂芳基的式I化合物是-O - ， - S - ， - SO 2 - ， - CHR 5 - ， - CHR 5，O-，-CHR 5 S，-CHR 5 SO 2 - ， - CHR - 5 CO-或-CH 2 CHR 5 - ; Y是键或-CHR 6 - 。 Z是具有以下结构的芳基或杂芳基：A是-CH-或-N-; B是-O-或-S-; 和R 1，R 2，R 3，R 4，R 5， R 6，R 7和R 8如本文所述。 还提供了单独或与另一种治疗剂组合使用上述化合物的糖原磷酸化酶抑制量的糖尿病和相关疾病的治疗方法。

公开(公告)号：US20060128687A1

公开(公告)日：2006-06-15

申请号：US11352867

申请日：2006-02-13

申请人： Philip Sher ,  Gang Wu ,  Terry Stouch ,  Bruce Ellsworth

发明人： Philip Sher ,  Gang Wu ,  Terry Stouch ,  Bruce Ellsworth

IPC分类号： A61K31/554 ,  C07D417/02

CPC分类号： C07D401/12 ,  A61K31/496 ,  A61K31/5377 ,  A61K31/541 ,  A61K45/06 ,  C07D209/42 ,  C07D403/12 ,  C07D403/14 ,  C07D413/12 ,  C07D417/12 ,  C07D471/04 ,  C07D513/04 ,  A61K2300/00

摘要： A compound of formula I wherein W is a bicyclic hetroaryl of the structure X is —O—, —S—, —SO2—, —CHR5—, —CHR5O—, —CHR5S—, —CHR5SO2—, —CHR5CO— or —CH2CHR5—; Y is a bond or —CHR6—; Z is an aryl or heteroaryl group of the following structure: A is —CH— or —N—; B is —O— or —S—; and R1, R2, R3, R4, R5, R6, R7 and R8 are as described herein. Further provided is a method for treating diabetes and related diseases employing a glycogen phosphorylase inhibiting amount of the above compound, either alone or in combination with another therapeutic agent.

公开(公告)号：US07425550B2

公开(公告)日：2008-09-16

申请号：US11352867

申请日：2006-02-13

申请人： Philip Sher ,  Gang Wu ,  Terry Stouch ,  Bruce Ellsworth

发明人： Philip Sher ,  Gang Wu ,  Terry Stouch ,  Bruce Ellsworth

IPC分类号： A61K31/554 ,  C07D267/14 ,  C07D498/02

CPC分类号： C07D401/12 ,  A61K31/496 ,  A61K31/5377 ,  A61K31/541 ,  A61K45/06 ,  C07D209/42 ,  C07D403/12 ,  C07D403/14 ,  C07D413/12 ,  C07D417/12 ,  C07D471/04 ,  C07D513/04 ,  A61K2300/00

摘要： A compound of formula I is provided having the structure wherein W is as defined herein; X is —CHR5O—; Y is a bond; Z is an aryl or heteroaryl group; and R1, and R2, are as described herein. Further provided is a method for treating diabetes and related diseases employing the above compound, either alone or in combination with another therapeutic agent.

摘要翻译： 提供具有其中W如本文所定义的结构的式I化合物; X是-CHR 5 O-; Y是一个债券; Z是芳基或杂芳基; 和R 1，R 2和R 2如本文所述。 还提供了使用上述化合物单独或与其它治疗剂组合治疗糖尿病和相关疾病的方法。

公开(公告)号：US20060111413A1

公开(公告)日：2006-05-25

申请号：US11273167

申请日：2005-11-14

申请人： Philip Sher ,  Gang Wu ,  Wei Meng ,  Alexandra Nirschl ,  William Washburn ,  Terry Stouch

发明人： Philip Sher ,  Gang Wu ,  Wei Meng ,  Alexandra Nirschl ,  William Washburn ,  Terry Stouch

IPC分类号： A61K31/4184 ,  A61K31/407 ,  C07D498/02 ,  C07D407/02

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 or stereoisomers or prodrugs or pharmaceutically acceptable salts thereof, wherein W, R1, R2, X, Y 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。 这些新化合物具有其结构或立体异构体或前药或其药学上可接受的盐，其中W，R 1，R 2，X，Y和Z在本文中定义。

公开(公告)号：US20050143381A1

公开(公告)日：2005-06-30

申请号：US11016135

申请日：2004-12-17

申请人： Guixue Yu ,  William Ewing ,  Amarendra Mikkilineni ,  Annapurna Pendri ,  Philip Sher ,  Samuel Gerritz ,  Bruce Ellsworth ,  Gang Wu ,  Yanting Huang ,  Chongqing Sun ,  Natesan Murugesan ,  Zhengxiang Gu ,  Ying Wang ,  Doree Sitkoff ,  Stephen Johnson ,  Ximao Wu

发明人： Guixue Yu ,  William Ewing ,  Amarendra Mikkilineni ,  Annapurna Pendri ,  Philip Sher ,  Samuel Gerritz ,  Bruce Ellsworth ,  Gang Wu ,  Yanting Huang ,  Chongqing Sun ,  Natesan Murugesan ,  Zhengxiang Gu ,  Ying Wang ,  Doree Sitkoff ,  Stephen Johnson ,  Ximao Wu

IPC分类号： A61K31/5025 ,  C07D487/04 ,  A61K31/503

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.

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 3， 本文描述了SUP 6，R 7，m和n。

公开(公告)号：US07365061B2

公开(公告)日：2008-04-29

申请号：US11273167

申请日：2005-11-14

申请人： Philip M. Sher ,  Gang Wu ,  Wei Meng ,  Alexandra A. Nirschl ,  William N. Washburn ,  Terry Stouch

发明人： Philip M. Sher ,  Gang Wu ,  Wei Meng ,  Alexandra A. Nirschl ,  William N. Washburn ,  Terry Stouch

IPC分类号： A61K31/404 ,  A61K31/454 ,  A61K31/397 ,  C07D209/04 ,  C07D205/04 ,  C07D401/08

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 or stereoisomers or prodrugs or pharmaceutically acceptable salts thereof, wherein W, R1, R2, X, Y 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。 这些新化合物具有其结构或立体异构体或前药或其药学上可接受的盐，其中W，R 1，R 2，X，Y和Z在本文中定义。

公开(公告)号：US20070004772A1

公开(公告)日：2007-01-04

申请号：US11454322

申请日：2006-06-16

申请人： Chongqing Sun ,  Philip Sher ,  Gang Wu ,  William Ewing ,  Yanting Huang ,  Taekyu Lee ,  Natesan Murugesan ,  Richard Sulsky

发明人： Chongqing Sun ,  Philip Sher ,  Gang Wu ,  William Ewing ,  Yanting Huang ,  Taekyu Lee ,  Natesan Murugesan ,  Richard Sulsky

IPC分类号： C07D471/02 ,  A61K31/4745

CPC分类号： C07D471/04

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 following general formula: including all prodrugs, solvates, pharmaceutically acceptable salts and stereoisomers, wherein R1, R2, R3, R4 and R5 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，以及使用式I化合物单独和与一种或多种 其他治疗剂。 该化合物具有以下通式：包括所有前药，溶剂化物，药学上可接受的盐和立体异构体，其中R 1，R 2，R 3， 本文描述了R 4和R 5。

公开(公告)号：US20050009870A1

公开(公告)日：2005-01-13

申请号：US10889268

申请日：2004-07-12

申请人： Philip Sher ,  Chongqing Sun ,  Richard Sulsky ,  Gang Wu ,  William Ewing

发明人： Philip Sher ,  Chongqing Sun ,  Richard Sulsky ,  Gang Wu ,  William Ewing

IPC分类号： A61K20060101 ,  A61K31/47 ,  A61K31/4709 ,  C07D215/36 ,  C07D215/38 ,  C07D215/48 ,  C07D401/04 ,  C07D401/06 ,  C07D401/12 ,  C07D405/06 ,  C07D409/04 ,  C07D409/06 ,  C07D409/12 ,  C07D409/14 ,  C07D413/12 ,  C07D413/14 ,  C07D417/06 ,  C07D417/12 ,  C07D453/02 ,  C07D453/04

CPC分类号： C07D417/06 ,  C07D215/38 ,  C07D215/48 ,  C07D401/04 ,  C07D401/06 ,  C07D401/12 ,  C07D405/06 ,  C07D409/04 ,  C07D409/06 ,  C07D409/12 ,  C07D409/14 ,  C07D413/12 ,  C07D413/14 ,  C07D417/12

摘要： The invention provides for compounds of formula I wherein the substitutents are as described herein. Further provided are methods of using such compounds for the treatment of eating disorders, metabolic disorders, obesity, cognitive disorders, neurological disorders, pain disorders, inflammation disorders, in the promotion of smoking cessation and for the treatment of other psychiatric disorders Also provided are pharmaceutical compositions containing such compounds and pharmaceutical combinations of the compounds of the invention with other therapeutic agents.

公开(公告)号：US20060287341A1

公开(公告)日：2006-12-21

申请号：US11455083

申请日：2006-06-16

申请人： Gang Wu ,  Amarendra Mikkilineni ,  Philip Sher ,  Natesan Murugesan ,  Zhengxiang Gu

发明人： Gang Wu ,  Amarendra Mikkilineni ,  Philip Sher ,  Natesan Murugesan ,  Zhengxiang Gu

IPC分类号： A61K31/519 ,  C07D487/04

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: including all prodrugs, solvates, pharmaceutically acceptable salts and stereoisomers, wherein R1, R2, R3, R4 and R5 are described herein.

摘要翻译： 本申请描述了根据式I和II的化合物，包含至少一种式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和使用根据式I和II的化合物的治疗方法 单独并与一种或多种另外的治疗剂组合。 该化合物具有以下通式：包括所有前药，溶剂化物，药学上可接受的盐和立体异构体，其中R 1，R 2，R 3， 本文描述了R 4和R 5。

公开(公告)号：US20060111414A1

公开(公告)日：2006-05-25

申请号：US11273445

申请日：2005-11-14

申请人： Gang Wu ,  Philip Sher

发明人： Gang Wu ,  Philip Sher

IPC分类号： A61K31/4184 ,  A61K31/407 ,  C07D407/02 ,  C07D498/02

CPC分类号： C07D235/24 ,  C07D209/42 ,  C07D401/12 ,  C07D403/12 ,  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 or stereoisomers or prodrugs or pharmaceutically acceptable salts thereof, wherein W, R1, R2, Y 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。 这些新化合物具有其结构或立体异构体或前药或其药学上可接受的盐，其中W，R 1，R 2，Y和Z在本文中定义。