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1. 发明授权

US07846671B2 Methods of screening for agents that modulate the interaction of RGS and Gαq and urinary incontinence 有权
标题翻译：筛选调节RGS和Gαq与尿失禁相互作用的药剂的方法
公开(公告)号：US07846671B2
公开(公告)日：2010-12-07
申请号：US10352843
申请日：2003-01-27
申请人： Mark Cockett , Chandra S. Ramanathan , Nicholas J. Lodge , Kevin Fitzgerald , Terry Stouch , Lisa Moore , Rachel M. Kindt , Jenny Kopczynski , Stephen Kohl Doberstein
发明人： Mark Cockett , Chandra S. Ramanathan , Nicholas J. Lodge , Kevin Fitzgerald , Terry Stouch , Lisa Moore , Rachel M. Kindt , Jenny Kopczynski , Stephen Kohl Doberstein
IPC分类号： G01N33/53
CPC分类号： G01N33/6893 , G01N2333/726 , G01N2333/916 , G01N2500/00 , G01N2800/341
摘要： The present invention provides methods that are useful for the treatment or prevention of smooth muscle disorders such as urinary incontinence and compounds that are useful in such methods.
摘要翻译：本发明提供了可用于治疗或预防平滑肌疾病如尿失禁的方法和可用于这些方法的化合物。

2. 发明申请

US20070065883A1 Molecules that modulate Galphaq activity and methods of treating urinary incontinence 审中-公开
标题翻译：调节Galphaq活性的分子和治疗尿失禁的方法
公开(公告)号：US20070065883A1
公开(公告)日：2007-03-22
申请号：US11404725
申请日：2006-04-14
申请人： Mark Cockett , Chandra Ramanathan , Nicholas Lodge , Kevin Fitzgerald , Terry Stouch , Lisa Moore , Rachel Kindt , Jenny Kopczynski , Stephen Doberstein
发明人： Mark Cockett , Chandra Ramanathan , Nicholas Lodge , Kevin Fitzgerald , Terry Stouch , Lisa Moore , Rachel Kindt , Jenny Kopczynski , Stephen Doberstein
IPC分类号： C40B30/06 , C40B40/10 , G01N33/53 , G01N33/567
CPC分类号： G01N33/6893 , G01N2333/726 , G01N2333/916 , G01N2500/00 , G01N2800/341
摘要： The present invention provides methods that are useful for the treatment or prevention of smooth muscle disorders such as urinary incontinence and compounds that are useful in such methods.
摘要翻译：本发明提供了可用于治疗或预防平滑肌疾病如尿失禁的方法和可用于这些方法的化合物。

3. 发明申请

US20060128687A1 Lactam glycogen phosphorylase inhibitors and method of use 有权
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.

4. 发明授权

US07057046B2 Lactam glycogen phosphorylase inhibitors and method of use 有权
标题翻译：内酰胺糖原磷酸化酶抑制剂及其使用方法
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。

5. 发明授权

US07365061B2 2-Amino-3-functionalized tetralin derivatives and related glycogen phosphorylase inhibitors 有权
标题翻译： 2-氨基-3-官能化的四氢化萘衍生物和相关的糖原磷酸化酶抑制剂
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。

6. 发明申请

US20060111413A1 2-Amino-3-functionalized tetralin derivatives and related glycogen phosphorylase inhibitors 有权
标题翻译： 2-氨基-3-官能化的四氢化萘衍生物和相关的糖原磷酸化酶抑制剂
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。

7. 发明授权

US07425550B2 Lactam glycogen phosphorylase inhibitors and method of use 有权
标题翻译：内酰胺糖原磷酸化酶抑制剂及其使用方法
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。

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