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1. 发明申请

US20080260834A1 VITAMIN D3 ANALOG LOADED POLYMER FORMULATIONS FOR CANCER AND NEURODEGENERATIVE DISORDERS 审中-公开
标题翻译： VITAMIN D3模拟装载聚合物制剂用于癌症和神经损伤性疾病
公开(公告)号：US20080260834A1
公开(公告)日：2008-10-23
申请号：US12165036
申请日：2008-06-30
申请人： Martin Burke , Maria-Christina White , Mark C. Watts , Jae Kyoo Lee , Betty M. Tyler , Gary H. Posner , Henry Brem
发明人： Martin Burke , Maria-Christina White , Mark C. Watts , Jae Kyoo Lee , Betty M. Tyler , Gary H. Posner , Henry Brem
IPC分类号： A61K31/59 , A61K9/10 , A61P35/00 , A61P25/28
CPC分类号： A61K9/0024 , A61K9/0085 , A61K9/1641
摘要： Localized delivery of 1,25 D3 directly to a target area using biodegradable polymeric matrices maximizes the efficacy of this drug while minimizing systemic exposure and toxicity. Anticalcemic analogs of 1,25 D3 have also been incorporated into controlled release polymer formulations to achieve efficacious intracranial concentrations of 1,25 D3 analogs for the treatment of intracranial tumors as well as neurodegenerative disorders such as Alzheimer's disease as well as to maximize the efficacy of these analogs in the treatment of systemic malignancies. The therapeutic efficacy of these formulations was demonstrated through a variety of studies in vitro and in vivo. Hybrid analogs of 1,25 D3 were incorporated into biodegradable polymer wafers composed of a polyanhydride copolymer of 1,3-bis(p-carboxyphenoxy)propane (CPP) and sebacic acid (SA) in a 20:80 molar ratio. In addition to providing improved treatments for malignancies and neurodegenerative disorders, the spatial localization and high reproducibility of this controlled delivery methodology presents a unique opportunity to study in vivo the poorly understood mechanisms of 1,25 D3's antiangiogenic, antiproliferative, and transcriptional regulating activities.
摘要翻译：使用可生物降解的聚合物基质直接向目标区域局部递送1,25 D 3 N使该药物的功效最大化，同时使全身暴露和毒性最小化。 1,25 D 3 N的类似物也被并入控释聚合物制剂中，以实现颅内肿瘤治疗的有效颅内浓度1,25D 3 N 3类似物以及神经变性疾病如阿尔茨海默病，以及使这些类似物在治疗全身性恶性肿瘤中的功效最大化。通过体外和体内的各种研究证实了这些制剂的治疗功效。将1,25 D 3 N的混合类似物掺入到由20重量份的1,3-双（对羧基苯氧基）丙烷（CPP）和癸二酸（SA）的聚酐共聚物组成的可生物降解的聚合物晶片中：80摩尔比。除了为恶性肿瘤和神经变性疾病提供改进的治疗之外，这种受控递送方法的空间定位和高重现性提供了一个独特的机会，可以在体内研究一个不太了解的1,25 D 3 抗血管生成，抗增殖和转录调节活性。

2. 发明授权

US6043386A Non-calcemic, antiproliferative, transcriptionally active 24-fluorinated hybrid analogs of 1.alpha.,-25-dihydroxy vitamin D.sub.3 有权
标题翻译： 1α，-25-二羟维生素D3的非钙血症，抗增殖，转录活性的24-氟化杂合类似物
公开(公告)号：US6043386A
公开(公告)日：2000-03-28
申请号：US323106
申请日：1999-06-01
申请人： Gary H. Posner , Jae Kyoo Lee , Qiang Wang
发明人： Gary H. Posner , Jae Kyoo Lee , Qiang Wang
IPC分类号： A61K31/59 , C07C401/00
CPC分类号： A61K31/59
摘要： Fluorinated analogs of 1.alpha.,25-dihydroxyvitamin D.sub.3. These analogs are synthesized in a convergent manner by joining A-ring and C,D-ring fragments. Each hybrid analog, having a calcemia-lowering 1-hydroxymethyl group and a potentiating 16-ene-24,24-difluorinated C,D-ring and side chain, is designed to be lipophilic and inert toward 24-hydroxylase enzyme catabolism. Each hybrid analog with 1.beta.,3.alpha.-substituent stereochemistry shows a pharmacologically desirable combination of high antiproliferative and high transcriptional activities in vitro and also low calcemic activity in vivo.
摘要翻译： 1α，25-二羟基维生素D3的氟化类似物。这些类似物通过连接A环和C，D环片段以收敛方式合成。具有降钙素1-羟甲基和增强的16-烯-2,24,24-二氟化C，D-环和侧链的每种杂合类似物被设计为亲脂性并且对24-羟化酶分解代谢是惰性的。具有1β，3α-取代立体化学的每种杂合类似物在体外显示高度抗增殖和高转录活性的药理学上期望的组合，并且还体内低钙活性。

3. 发明授权

US5403832A Vitamin D.sub.3 analogues 失效
标题翻译：维生素D3类似物
公开(公告)号：US5403832A
公开(公告)日：1995-04-04
申请号：US284209
申请日：1994-08-02
申请人： Gary H. Posner , Maria-Christina White
发明人： Gary H. Posner , Maria-Christina White
IPC分类号： C07C401/00 , C07F9/53
CPC分类号： C07C401/00 , C07F9/532
摘要： A vitamin D.sub.3 analogue which includes a hydroxyalkyl substituent in the 1-position and a modified D-ring side chain is described. This novel compound is a potent anti-proliferative substance with activity comparable to that of calcitriol but with a vitamin D.sub.3 receptor binding rating of approximately 10.sup.-3 compared to that of calcitriol.
摘要翻译：描述了包含1位羟基烷基取代基和改性的D环侧链的维生素D3类似物。这种新型化合物是一种有效的抗增殖物质，其活性与骨化三醇的活性相当，但维生素D3受体结合等级与骨化三醇相比约为10-3。

4. 发明授权

US08106035B2 25-SO2-substituted analogs of 1μ,25-dihydroxyvitamin D3 有权
标题翻译： 25-SO 2取代的1μ，25-二羟基维生素D3的类似物
公开(公告)号：US08106035B2
公开(公告)日：2012-01-31
申请号：US10738248
申请日：2003-12-18
申请人： Gary H. Posner , Jae Kyoo Lee , Qiang Wang , Kenneth R. Crawford , Hong Woon Yang , Steven M. Silverman , Byung-Chul Suh , Jay A. White , Glenville Jones , Uttam Saha , Heung Bae Jeon
发明人： Gary H. Posner , Jae Kyoo Lee , Qiang Wang , Kenneth R. Crawford , Hong Woon Yang , Steven M. Silverman , Byung-Chul Suh , Jay A. White , Glenville Jones , Uttam Saha , Heung Bae Jeon
IPC分类号： A61K31/59 , C07C401/00
CPC分类号： C07C401/00 , C07B2200/07 , C07C2601/02 , C07C2601/04
摘要： The present invention provides novel D-ring and side-chain analogs of 1α,25-dihydroxyvitamin D3, compositions comprising these compounds and methods of using these compounds as selective inhibitors of CYP24. In particular, the compounds of the invention are useful for treating diseases which benefit from a modulation of the levels of 1α,25-dihydroxyvitamin D3, for example, cell-proliferative disorders.
摘要翻译：本发明提供了1α，25-二羟基维生素D 3的新型D环和侧链类似物，包含这些化合物的组合物和使用这些化合物作为CYP24选择性抑制剂的方法。特别地，本发明的化合物可用于治疗受益于1α，25-二羟基维生素D 3水平的调节的疾病，例如细胞增殖性疾病。

5. 发明授权

US06380408B1 Non-calcemic, antiproliferative, transcriptionally active sulfur-containing analogs of 1&agr;, 25-dihydroxy vitamin D3 有权
标题翻译： 1α，25-二羟维生素D3的非钙，抗增殖，转录活性含硫类似物
公开(公告)号：US06380408B1
公开(公告)日：2002-04-30
申请号：US09541060
申请日：2000-03-31
申请人： Gary H. Posner , Jae-Kyoo Lee , Qiang Wang , Kenneth R. Crawford , Gyoonhee Han
发明人： Gary H. Posner , Jae-Kyoo Lee , Qiang Wang , Kenneth R. Crawford , Gyoonhee Han
IPC分类号： C07C40100
CPC分类号： C07C401/00
摘要： Novel sulfur-containing analogs of 1&agr;,25-dihydroxy vitamin D3 are provided. These analogs are synthesized in a convergent manner by joining A-ring and C,D ring fragments. Each analog with 1&agr;,3&bgr;-substituent stereochemistry shows a pharmacologically desirable combination of high antiproliferative and high transcriptional activities in vitro and also low calcemic activity in vivo.
摘要翻译：提供了1α，25-二羟基维生素D3的新型含硫类似物。这些类似物通过连接A环和C，D环片段以收敛方式合成。每个具有1alpha，3beta取代基立体化学的类似物都显示体外高抗增殖和高转录活性以及体内低钙活性的药理学上希望的组合。

6. 发明授权

US09775903B2 1-deoxy analogs of 1,25-dihydroxyvitamin D3 compounds 有权
公开(公告)号：US09775903B2
公开(公告)日：2017-10-03
申请号：US13521980
申请日：2011-01-13
申请人： Gary H. Posner , Lindsey C. Hess , Alvin S. Kalinda , Rachel D. Slack , Uttam Saha , P. Martin Petkovich
发明人： Gary H. Posner , Lindsey C. Hess , Alvin S. Kalinda , Rachel D. Slack , Uttam Saha , P. Martin Petkovich
IPC分类号： A61K45/06 , C07C401/00 , A61K31/593
CPC分类号： A61K45/06 , A61K31/593 , C07C401/00 , C07C2601/14 , C07C2602/24
摘要： This present disclosure is directed to novel prodrugs of activated vitamin D3 compounds. The prodrugs can be designed to have one or more beneficial properties, such as selective inhibition of the enzyme CYP24, low calcemic activity, and anti-proliferative activity. Specifically, these prodrugs are 1-deoxy prohormones of active Vitamin D analogs, e.g. analogs of calcitriol. This disclosure is also directed to pharmaceutical and diagnostic compositions containing the prodrugs of the invention, and to their medical use, particularly as prodrugs in the treatment and/or prevention of diseases.

7. 发明授权

US08884032B2 Trioxane monomers and dimers 有权
标题翻译：三恶烷单体和二聚体
公开(公告)号：US08884032B2
公开(公告)日：2014-11-11
申请号：US13321343
申请日：2010-05-19
申请人： Gary H. Posner , Lauren E. Woodard , David R. Levine , Deuk Kyu Moon , Bryan T. Mott
发明人： Gary H. Posner , Lauren E. Woodard , David R. Levine , Deuk Kyu Moon , Bryan T. Mott
IPC分类号： C07D321/00 , A61K31/335 , C07D493/18 , C07D519/00
CPC分类号： C07D493/18 , C07D519/00
摘要： Monomeric and dimeric trioxane fluoroaryl amides, 5-carbon-linked, C-10 non-acetal trioxane dimer esters; trioxane silylamides; and trioxane dimer orthoesters and methods of their use for treating subjects infected with malaria or other parasitic infectious diseases including, but not limited to, toxoplasmic infection; subjects afflicted with psychiatric conditions associated with toxoplasmic infection; and subjects afflicted with cancer.
摘要翻译：单碳和二聚三恶烷氟芳基酰胺，5-碳连接的C-10非缩醛三恶烷二聚体酯; 三恶烷甲硅烷基酰胺和三恶烷二聚体原生体及其用于治疗感染疟疾或其他寄生传染病的受试者的方法，包括但不限于：弓形虫感染; 患有与弓形虫感染相关的精神病症的受试者; 和患有癌症的受试者。

8. 发明授权

US5817692A Endoperoxides useful as antiparasitic agents 失效
标题翻译：内过氧化物可用作抗寄生虫剂
公开(公告)号：US5817692A
公开(公告)日：1998-10-06
申请号：US701423
申请日：1996-08-22
申请人： Gary H. Posner
发明人： Gary H. Posner
IPC分类号： A61K31/357 , C07D493/08 , C07D493/10 , C07D497/08 , A61K31/335 , C07D321/10 , C07D323/04
CPC分类号： A61K31/357 , C07D493/08 , C07D493/10 , C07D497/08
摘要： The present invention relates to novel biologically-active organic peroxides and to novel uses of both known and new organic peroxides. More specifically, this invention details organic endoperoxides having antiparasitic activity, methods for their preparation and methods for treating malaria and cerebral toxoplasmic encephalitis with the organic endoperoxides.
摘要翻译：本发明涉及新颖的生物活性有机过氧化物和新型有机过氧化物的新用途。更具体地，本发明详述了具有抗寄生虫活性的有机内过氧化物，其制备方法和用有机内过氧化物治疗疟疾和脑弓形虫脑炎的方法。

9. 发明授权

US5274142A Vitamin D.sub.3 analogues 失效
标题翻译：维生素D3类似物
公开(公告)号：US5274142A
公开(公告)日：1993-12-28
申请号：US849716
申请日：1992-03-12
申请人： Gary H. Posner , Todd D. Nelson
发明人： Gary H. Posner , Todd D. Nelson
IPC分类号： C07C401/00 , C07F9/53
CPC分类号： C07C401/00 , C07F9/532
摘要： A vitamin D.sub.3 analogue which includes at least one hydroxyalkyl substituent on the A-ring, preferably the 1-position thereof.
摘要翻译：维生素D3类似物，其在A环上包括至少一个羟烷基取代基，优选其1-位。

10. 发明申请

US20130157987A1 1-DEOXY ANALOGS OF 1,25-DIHYDROXYVITAMIN D3 COMPOUNDS 有权
标题翻译： 1,25-二羟基维生素D3化合物的1-去氧模拟物
公开(公告)号：US20130157987A1
公开(公告)日：2013-06-20
申请号：US13521980
申请日：2011-01-13
申请人： Gary H. Posner , Lindsey C. Hess , Alvin S. Kalinda , Rachel D. Slack , Uttam Saha , P. Martin Petkovich
发明人： Gary H. Posner , Lindsey C. Hess , Alvin S. Kalinda , Rachel D. Slack , Uttam Saha , P. Martin Petkovich
IPC分类号： A61K45/06 , A61K31/593 , C07C401/00
CPC分类号： A61K45/06 , A61K31/593 , C07C401/00 , C07C2601/14 , C07C2602/24
摘要： This present disclosure is directed to novel prodrugs of activated vitamin D3 compounds. The prodrugs can be designed to have one or more beneficial properties, such as selective inhibition of the enzyme CYP24, low calcemic activity, and anti-proliferative activity. Specifically, these prodrugs are 1-deoxy prohormones of active Vitamin D analogs, e.g. analogs of calcitriol. This disclosure is also directed to pharmaceutical and diagnostic compositions containing the prodrugs of the invention, and to their medical use, particularly as prodrugs in the treatment and/or prevention of diseases.
摘要翻译：本公开内容涉及活化的维生素D3化合物的新型前药。前药可以被设计为具有一种或多种有益的性质，例如CYP24酶的选择性抑制，低钙血症活性和抗增殖活性。具体来说，这些前药是活性维生素D类似物的1-脱氧激素。骨化三醇的类似物。本公开还涉及含有本发明前药的药物和诊断组合物及其医疗用途，特别是作为前药治疗和/或预防疾病。

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