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1. 发明申请

US20060142363A1 Imidazolidinedione analogs useful as anticoagulants and antithrombotics 失效
公开(公告)号：US20060142363A1
公开(公告)日：2006-06-29
申请号：US11360048
申请日：2006-02-22
申请人： Damian Arnaiz , Yuo-Ling Chou , Brian Griedel , Raju Mohan , Kenneth Shaw
发明人： Damian Arnaiz , Yuo-Ling Chou , Brian Griedel , Raju Mohan , Kenneth Shaw
IPC分类号： A61K31/4166 , C07D233/88
CPC分类号： C07D235/02 , C07D233/76 , C07D233/78 , C07D401/06 , C07D491/04
摘要： A compound is disclosed, which is useful in treating a mammal having a disease-state characterized by thrombotic activity. The compound is of the following formula: wherein A, B, R1, R2, R3 and R4 are as defined herein or an isomer or isomeric mixture thereof or a pharmaceutically acceptable salt thereof.

2. 发明授权

US08367651B2 Solid ganaxolone formulations and methods for the making and use thereof 有权
标题翻译：固体加诺沙酮制剂及其制备和使用方法
公开(公告)号：US08367651B2
公开(公告)日：2013-02-05
申请号：US13052798
申请日：2011-03-21
申请人： Kenneth Shaw , Mingbao Zhang
发明人： Kenneth Shaw , Mingbao Zhang
IPC分类号： A01N43/00 , A61K31/33
CPC分类号： A61K31/573 , A61K9/0019 , A61K9/10 , A61K9/143 , A61K9/145 , A61K9/146 , A61K9/1676 , A61K9/2054 , A61K9/2059 , A61K9/2077 , A61K9/282 , A61K9/2846 , A61K9/2866 , A61K9/4808 , A61K9/4891 , A61K9/5026 , A61K9/5078 , A61K9/5084 , A61K31/57 , A61K47/02 , A61K47/26 , Y10S977/773 , Y10S977/775 , Y10S977/906 , Y10S977/915
摘要： In certain embodiments, the invention is directed to composition comprising stable particles comprising ganaxolone, wherein the volume weighted median diameter (D50) of the particles is from about 50 nm to about 500 nm.
摘要翻译：在某些实施方案中，本发明涉及包含稳定的颗粒的组合物，所述稳定颗粒包含加纳西酮，其中颗粒的体积加权中位数直径（D50）为约50nm至约500nm。

3. 发明申请

US20110137323A1 SURGICAL CLIP APPLIER 有权
标题翻译：手术夹具
公开(公告)号：US20110137323A1
公开(公告)日：2011-06-09
申请号：US12939296
申请日：2010-11-04
申请人： Jaroslaw T. Malkowski , Kenneth Shaw
发明人： Jaroslaw T. Malkowski , Kenneth Shaw
IPC分类号： A61B17/10
CPC分类号： A61B17/105 , A61B17/068 , A61B17/083 , A61B17/128 , A61B2017/00407 , A61B2090/0803 , A61B2090/0807
摘要： A surgical clip applier is provided including a housing; at least one handle pivotably connected to the housing; a channel assembly extending distally from the housing; a plurality of clips loaded in the clip carrier; a drive channel translatably supported in the housing and the channel assembly, the drive channel being translated upon actuation of the at least one handle; and a counter mechanism supported in the housing, the counter mechanism including indicia visible through the housing, wherein the indicia corresponds to a quantity of clips loaded in the clip applier, wherein the indicia decrements upon each firing of the clip applier resulting in a reduction in the quantity of clips remaining of the plurality of clips.
摘要翻译：提供了一种手术夹具，包括壳体; 至少一个手柄，其可枢转地连接到所述壳体; 从壳体向远端延伸的通道组件; 装载在所述夹子载体中的多个夹具; 可移动地支撑在所述壳体和所述通道组件中的驱动通道，所述驱动通道在所述至少一个手柄的致动时被平移; 以及支撑在所述壳体中的计数器机构，所述计数器机构包括通过所述壳体可见的标记，其中所述标记对应于夹在所述施夹器中的一定数量的夹子，其中所述标记在所述施夹器的每次点火时减小，多个剪辑中剩余的剪辑的数量。

4. 发明申请

US20080076781A1 PSEUDOBASE BENZO[C]PHENANTHRIDINES WITH IMPROVED EFFICACY, STABILITY, AND SAFETY 有权
标题翻译： PSEUDOBASE BENZO [C]具有改善效率，稳定性和安全性的苯并噻唑
公开(公告)号：US20080076781A1
公开(公告)日：2008-03-27
申请号：US11831498
申请日：2007-07-31
申请人： Kenneth Shaw , Mingbao Zhang
发明人： Kenneth Shaw , Mingbao Zhang
IPC分类号： A61K31/44 , A61K31/4965 , A61P43/00 , C07D221/18 , C07D241/00 , C07D487/22
CPC分类号： C07D491/04
摘要： Pseudobase benzo[c]phenanthridines and the pharmaceutically acceptable salts thereof of Formula I are provided herein. The variables R, R1, R2, R3, and R4 are defined herein. Certain pseudobase benzo[c]phenanthridines provided herein act as prodrugs, targeting the parent benzo[c]phenanthridinium alkaloid to hydrophilic or hydrophobic regions in the body. Pharmaceutical compositions comprising a pseudobase benzo[c]phenanthridine and a carrier, excipient, or diluent are provided herein. Methods of treating or preventing microbial, fungal and or viral infections and methods of treating diseases and disorders responsive to protein kinase C modulation, topoisomerase I, and/or topoisomerase II modulation are also provided.
摘要翻译：本文提供了假碱性苯并[c]菲啶及其式I的药学上可接受的盐。变量R 1，R 1，R 2，R 3和R 4在本文中定义。本文提供的某些假碱性苯并[c]菲啶用作前药，将母体苯并[c]菲啶生物碱靶向体内的亲水或疏水区域。本文提供了包含假碱性苯并[c]菲啶和载体，赋形剂或稀释剂的药物组合物。还提供了治疗或预防微生物，真菌和/或病毒感染的方法以及治疗对蛋白激酶C调节，拓扑异构酶I和/或拓扑异构酶II调节的疾病和病症的方法。

5. 发明授权

US07271170B2 Imidazo-pyrimidines and triazolo-pyrimidines: benzodiazepine receptor ligands 有权
标题翻译：咪唑并 - 嘧啶和三唑并嘧啶：苯并二氮杂受体配体
公开(公告)号：US07271170B2
公开(公告)日：2007-09-18
申请号：US10898690
申请日：2004-07-23
申请人： Linghong Xie , Bingsong Han , Yuelian Xu , George Maynard , Bertrand L. Chenard , Kenneth Shaw , Yang Gao
发明人： Linghong Xie , Bingsong Han , Yuelian Xu , George Maynard , Bertrand L. Chenard , Kenneth Shaw , Yang Gao
IPC分类号： C07D487/04 , A61K31/519 , A61P25/24 , A61P25/22 , A61P25/20
CPC分类号： C07D487/04
摘要： Compounds of Formula I are provided, as are methods for their preparation. The variables Z1, Z2, Z3, R4, R5, R6, R7, R8 and Ar in the above formula are defined herein. Such compounds may be used to modulate ligand binding to GABAA receptors in vivo or in vitro, and are particularly useful in the treatment of a variety of central nervous system (CNS) disorders in humans, domesticated companion animals and livestock animals. Compounds provided herein may be administered alone or in combination with one or more other CNS agents to potentiate the effects of the other CNS agent(s). Pharmaceutical compositions and methods for treating such disorders are provided, as are methods for using such ligands for detecting GABAA receptors (e.g., receptor localization studies).
摘要翻译：提供了式I化合物，以及其制备方法。变量Z 1，Z 2，Z 3，R 4，R 5，/或 >，R 6，R 7，R 8和Ar如上所定义。这样的化合物可用于在体内或体外调节配体与GABA A A受体的结合，并且特别可用于治疗人类中的各种中枢神经系统（CNS）紊乱，驯养伴侣动物和牲畜。本文提供的化合物可以单独施用或与一种或多种其它CNS剂组合施用，以增强其它CNS剂的作用。还提供了用于治疗这种病症的药物组合物和方法，以及使用这种配体检测GABA A受体的方法（例如，受体定位研究）。

6. 发明申请

US20070148252A1 Solid ganaxolone formulations and methods for the making and use thereof 有权
标题翻译：固体加诺沙酮制剂及其制备和使用方法
公开(公告)号：US20070148252A1
公开(公告)日：2007-06-28
申请号：US11606222
申请日：2006-11-28
申请人： Kenneth Shaw , Mingbao Zhang
发明人： Kenneth Shaw , Mingbao Zhang
IPC分类号： A61K31/57 , A61K9/14
CPC分类号： A61K31/573 , A61K9/0019 , A61K9/10 , A61K9/143 , A61K9/145 , A61K9/146 , A61K9/1676 , A61K9/2054 , A61K9/2059 , A61K9/2077 , A61K9/282 , A61K9/2846 , A61K9/2866 , A61K9/4808 , A61K9/4891 , A61K9/5026 , A61K9/5078 , A61K9/5084 , A61K31/57 , A61K47/02 , A61K47/26 , Y10S977/773 , Y10S977/775 , Y10S977/906 , Y10S977/915
摘要： In certain embodiments, the invention is directed to composition comprising stable particles comprising ganaxolone, wherein the volume weighted median diameter (D50) of the particles is from about 50 nm to about 500 nm.
摘要翻译：在某些实施方案中，本发明涉及包含稳定的颗粒的组合物，所述稳定颗粒包含加纳西酮，其中颗粒的体积加权中值直径（D 50）为约50nm至约500nm。

7. 发明申请

US20060135487A1 Piperazine derivatives and their use as anti-inflammatory agents 失效
公开(公告)号：US20060135487A1
公开(公告)日：2006-06-22
申请号：US11248618
申请日：2005-10-13
申请人： John Bauman , Brad Buckman , Ameen Ghannam , Joseph Hesselgesser , Richard Horuk , Imadul Islam , Meina Liang , Karen May , Sean Monahan , Michael Morrissey , Howard Ng , Kenneth Shaw , Guo Wei , Wei Xu , Zuchun Zhao , Wei Zheng
发明人： John Bauman , Brad Buckman , Ameen Ghannam , Joseph Hesselgesser , Richard Horuk , Imadul Islam , Meina Liang , Karen May , Sean Monahan , Michael Morrissey , Howard Ng , Kenneth Shaw , Guo Wei , Wei Xu , Zuchun Zhao , Wei Zheng
IPC分类号： A61K31/655 , A61K31/496 , A61K31/495
CPC分类号： C07D295/185 , C07D215/18 , C07D241/04 , C07D241/38 , C07D261/14 , C07D295/192 , C07D307/52 , C07D403/06 , C07D403/12 , C07D405/12 , C07D413/12
摘要： This invention is directed to acyl piperazine derivatives which are useful as anti-inflammatory agents. This invention is also directed to pharmaceutical compositions containing the compounds of the invention, and methods of using the compounds to treat inflammatory disorders in humans.

8. 发明授权

US07060451B2 Methods for screening GABA-modulatory compounds for specified pharmacological activities 失效
标题翻译：筛选用于规定药理活性的GABA调节化合物的方法
公开(公告)号：US07060451B2
公开(公告)日：2006-06-13
申请号：US10045396
申请日：2001-11-09
申请人： John Tallman , Dorothy Gallager , Kenneth Shaw , Geoffrey White , Marci Crandall , James Cassella , Lavanya Rajachandran , Pamela Albaugh
发明人： John Tallman , Dorothy Gallager , Kenneth Shaw , Geoffrey White , Marci Crandall , James Cassella , Lavanya Rajachandran , Pamela Albaugh
IPC分类号： G01N33/567 , C07K1/00 , C07H21/04 , C12N1/20 , C12P21/02
CPC分类号： G01N33/9426 , G01N2333/70571 , G01N2500/00
摘要： Methods are provided that are useful in assaying compounds for cognitive enhancing properties, anxiolytic properties, hypnotic properties, or antidepressant properties. These methods involve determining the in vitro efficacy and EC50 of the compounds at defined series of cloned GABAA subtype receptors composed of specific variants of α, β, and γ subunits in order to develop and an activity profile for each compound. Optionally, the binding affinities of the compounds at GABAA receptors are also determined. As an additional step the in vivo effects of the compounds may be tested in animal models.
摘要翻译：提供了可用于测定化合物的认知增强性质，抗焦虑性质，催眠性质或抗抑郁药性质的方法。这些方法包括确定在由α，β和γ亚基的特异性变体组成的限定的克隆的GABA亚型亚型受体系列中的化合物的体外功效和EC 50 为每个化合物开发和活动资料。任选地，还测定了化合物在GABA A A受体上的结合亲和力。作为附加步骤，可以在动物模型中测试化合物的体内作用。

9. 发明授权

US06268496B1 Certain imidazoquinoxalines: a new class of GABA brain receptor ligands 失效
标题翻译：某些咪唑喹啉酮：一类新的GABA脑受体配体
公开(公告)号：US06268496B1
公开(公告)日：2001-07-31
申请号：US09400060
申请日：1999-09-21
申请人： Kenneth Shaw
发明人： Kenneth Shaw
IPC分类号： C07D48704
CPC分类号： C07D487/04
摘要： This invention encompasses compounds of the formula: and the pharmaceutically acceptable non-toxic salts thereof wherein R1, R2, R3, R4, X, and W are variables. These compounds are highly selective agonists, antagonists or inverse agonists for GABAa brain receptors or prodrugs thereof and are useful in the diagnosis and treatment of anxiety, sleep, and seizure disorders, overdose with benzodiazepine drugs, and enhancement of memory.
摘要翻译：本发明包括下式的化合物及其药学上可接受的无毒盐，其中R 1，R 2，R 3，R 4，X和W是变量。这些化合物是GABAa脑受体或其前药的高度选择性激动剂，拮抗剂或反向激动剂，并且可用于诊断和治疗焦虑，睡眠和癫痫发作，用苯二氮卓类药物过量和记忆增强。

10. 发明授权

US5908932A Certain pyrroloquinolinones; a new class of GABA brain receptor 失效
标题翻译：某些吡咯喹啉酮; 一类新的GABA脑受体
公开(公告)号：US5908932A
公开(公告)日：1999-06-01
申请号：US799446
申请日：1997-02-13
申请人： Kenneth Shaw , Jun Yuan
发明人： Kenneth Shaw , Jun Yuan
IPC分类号： C07D471/04 , A61K31/44 , C07D471/06
CPC分类号： C07D471/04
摘要： This invention encompasses compounds of formula (I), and pharmaceutically acceptable non-toxic salts thereof wherein X and Y are the same or different and represent oxygen or H.sub.2 with the proviso that not both X and Y are H.sub.2 ; W represents phenyl, thienyl, or pyridyl, each of which may be unsubstituted or mono or disubstituted with organic or inorganic substituents; and R.sub.1, R.sub.2, R.sub.3, and R.sub.4 are variables representing organic and inorganic substituents. These compounds are highly selective agonists, antagonists or inverse agonists for GABAs brain receptors or prodrugs thereof and are useful in the diagnosis and treatment of anxiety, sleep, and seizure disorders, overdose with benzodiazepine drugs, and enhancement of memory.
摘要翻译：本发明包括式（I）的化合物及其药学上可接受的无毒盐，其中X和Y相同或不同，代表氧或H 2，条件是X和Y都不是H 2; W代表苯基，噻吩基或吡啶基，它们各自可以是未被取代的或被有机或无机取代基单取代或二取代; 并且R1，R2，R3和R4是表示有机和无机取代基的变量。这些化合物是用于GABA脑受体或其前药的高选择性激动剂，拮抗剂或反向激动剂，并且可用于诊断和治疗焦虑，睡眠和癫痫发作障碍，用苯并二氮杂药物过量和增强记忆。

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