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11. 发明申请

US20120052098A1 LIQUID GANAXOLONE FORMULATIONS AND METHODS FOR THE MAKING AND USE THEREOF 有权
标题翻译：液体GANAXOLONE制剂及其制备和使用方法
公开(公告)号：US20120052098A1
公开(公告)日：2012-03-01
申请号：US13217384
申请日：2011-08-25
申请人： Kenneth SHAW , Mingbao Zhang
发明人： Kenneth SHAW , Mingbao Zhang
IPC分类号： A61K9/10 , A61P25/00 , A61P25/20 , A61P3/00 , A61K31/57 , A61P25/08 , B82Y5/00
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。

12. 发明授权

US07531550B2 Pseudobase benzo[c]phenanthridines with improved efficacy, stability, and safety 有权
标题翻译：具有改善功效，稳定性和安全性的假碱性苯并[c]菲啶
公开(公告)号：US07531550B2
公开(公告)日：2009-05-12
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： A61K31/4741 , C07D491/113
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，R1，R2，R3和R4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。

13. 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。

14. 发明申请

US20110236487A1 SOLID GANAXOLONE FORMULATIONS AND METHODS FOR THE MAKING AND USE THEREOF 有权
标题翻译：固体GANAXOLONE配方及其制备和使用方法
公开(公告)号：US20110236487A1
公开(公告)日：2011-09-29
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： A61K9/14 , A61K31/57 , A61P25/08 , B82Y5/00
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，其中所述颗粒的体积加权中位数直径（D50）为约50nm至约500nm。

15. 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。

16. 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。

17. 发明授权

US6054623A Hydroxythiol grignard reaction synthesis 失效
标题翻译：羟基硫醇格氏反应合成
公开(公告)号：US6054623A
公开(公告)日：2000-04-25
申请号：US215691
申请日：1998-12-18
申请人： David Ryckman , Mingbao Zhang , Guohua Chen
发明人： David Ryckman , Mingbao Zhang , Guohua Chen
IPC分类号： C07C319/02 , C07C323/20 , C07F7/18
CPC分类号： C07C319/02 , C07F7/1892 , Y02P20/55
摘要： A method for the preparation of hydroxythiol compounds by reacting a hydroxyl-protected halide compound having the structure:X--R--OPgwith magnesium in a Grignard-suitable solvent to form a hydroxyl-protected magnesium halide compound, wherein R is selected from substituted or unsubstituted aliphatic radicals, substituted or unsubstituted cyclic aliphatic radicals, substituted or unsubstituted aromatic radicals, substituted or unsubstituted araliphatic radicals and substituted or unsubstituted heterocyclic radicals; Pg is a protecting group; and X is selected from the group consisting of F, Cl, Br and I; then reacting said hydroxyl-protected magnesium halide compound with sulfur in the Grignard-suitable solvent to form a hydroxyl-protected thiomagnesium halide compound; and hydrolyzing the protected hydroxyl group to form a hydroxythiomagnesium halide compound and converting the thiomagnesium halide to a thiol; wherein the protecting group is selected so that species formed by the de-protection of the protecting group are inert toward thiols, or the method further includes the step of removing the protecting group species formed by de-protection of the hydroxyl group from the reaction mixture before converting the thiomagnesium halide to a thiol.
摘要翻译：一种通过在格氏合适的溶剂中使具有结构：XR-OPg与羟基保护的卤化合物与镁反应以形成羟基保护的卤化镁化合物来制备羟基硫醇化合物的方法，其中R选自取代或未取代的脂族基团取代或未取代的环脂族基团，取代或未取代的芳族基团，取代或未取代的芳脂族基团和取代或未取代的杂环基团; Pg是保护组; X选自F，Cl，Br和I; 然后使所述羟基保护的卤化镁化合物与格氏合适的溶剂中的硫反应形成羟基保护的卤化卤化镁化合物; 水解保护的羟基以形成羟基卤化镁化合物并将卤化硫化镁转化为硫醇; 其中选择保护基，使得通过保护基去保护形成的物质对硫醇是惰性的，或者该方法还包括从反应混合物中除去由羟基脱保护形成的保护基物种的步骤之前将硫化镁卤化物转化为硫醇。

18. 发明授权

US6054622A Aromatic hydroxythiol synthesis using diazonium salts 失效
标题翻译：使用重氮盐的芳香族羟基硫醇合成
公开(公告)号：US6054622A
公开(公告)日：2000-04-25
申请号：US213144
申请日：1998-12-18
申请人： Mingbao Zhang , David Ryckman , Eric MacMillan
发明人： Mingbao Zhang , David Ryckman , Eric MacMillan
IPC分类号： C07C319/06 , C07C319/22 , C07C319/24 , C07C323/20 , C07C323/29 , C07C319/02
CPC分类号： C07C319/06 , C07C319/22 , C07C319/24
摘要： A method for the preparation of aromatic hydroxythiols including oxidizing an aromatic aminothiol to form an aminodisulfide compound; forming a bis-diazonium salt of the aminodisulfide compound; and reacting the bis-diazonium salt with water to form an aromatic hydroxyldisulfide compound, which is then reduced to the hydroxythiol. New bis-diazonium aromatic disulfide compounds are also disclosed.
摘要翻译：一种制备芳族羟基硫醇的方法，包括使芳族氨基硫醇氧化形成氨基二硫化物; 形成氨基二硫化物的双重重氮盐; 并使双重重氮盐与水反应形成芳族羟基二硫化物，然后将其还原成羟基硫醇。还公开了新的二重氮芳族二硫化物。

19. 发明授权

US08541618B2 Indane acetic acid derivatives and their use as pharmaceutical agents, intermediates, and method of preparation 有权
公开(公告)号：US08541618B2
公开(公告)日：2013-09-24
申请号：US13035625
申请日：2011-02-25
申请人： Derek B. Lowe , Philip L. Wickens , Xin Ma , Mingbao Zhang , William H. Bullock , Philip D. G. Coish , Ingo A. Mugge , Andreas Stolle , Ming Wang , Yamin Wang , Chengzhi Zhang , Hai-Jun Zhang , Lei Zhu , Manami Tsutsumi , James N. Livingston
发明人： Derek B. Lowe , Philip L. Wickens , Xin Ma , Mingbao Zhang , William H. Bullock , Philip D. G. Coish , Ingo A. Mugge , Andreas Stolle , Ming Wang , Yamin Wang , Chengzhi Zhang , Hai-Jun Zhang , Lei Zhu , Manami Tsutsumi , James N. Livingston
IPC分类号： C07C59/00 , C07C62/36 , C07C62/38 , C07C65/30 , C07C65/34 , A01N43/76 , A61K31/42
CPC分类号： C07D277/32 , C07B2200/07 , C07C51/412 , C07C51/44 , C07C59/72 , C07C69/732 , C07C69/734 , C07C69/738 , C07C2602/08 , C07D263/32 , C07D277/24 , C07D277/40 , C07D413/04 , C07D413/10 , C07D413/12
摘要： This invention relates to novel indane acetic acid derivatives which are useful in the treatment of diseases such as diabetes, obesity, hyperlipidemia, and atherosclerotic diseases. The invention also relates to intermediates useful in preparation of indane acetic derivatives and to methods of preparation.

20. 发明授权

US08013166B2 Preparation and use of aryl alkyl acid derivatives for the treatment of obesity 失效
公开(公告)号：US08013166B2
公开(公告)日：2011-09-06
申请号：US12231878
申请日：2008-09-05
申请人： Roger A. Smith , Ann-Marie Campbell , Philip Coish , Miao Dai , Susan Jenkins , Derek Lowe , Stephen J. O'Connor , Ning Su , Gan Wang , Mingbao Zhang , Lei Zhu
发明人： Roger A. Smith , Ann-Marie Campbell , Philip Coish , Miao Dai , Susan Jenkins , Derek Lowe , Stephen J. O'Connor , Ning Su , Gan Wang , Mingbao Zhang , Lei Zhu
IPC分类号： C07D277/42 , C07D277/62 , C07D263/34 , C07D263/58
CPC分类号： C07D263/58 , C07D235/30 , C07D263/60 , C07D277/42 , C07D277/58 , C07D277/82 , C07D405/12 , C07D413/12 , C07D417/12
摘要： This invention relates to certain aryl alkyl acid compounds, compositions, and methods for treating or preventing obesity and related diseases.

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