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1. 发明授权

US5411986A Chemoprotective isothiocyanates 失效
公开(公告)号：US5411986A
公开(公告)日：1995-05-02
申请号：US030610
申请日：1993-03-12
申请人： Cheon-Gyu Cho , Gary H. Posner , Paul Talalay , Yuesheng Zhang
发明人： Cheon-Gyu Cho , Gary H. Posner , Paul Talalay , Yuesheng Zhang
IPC分类号： A61K31/145 , A61K31/26 , A61K31/66 , C07C331/20 , C07C331/24 , C07C331/26 , C07C331/28 , C07F9/40 , C07C331/04
CPC分类号： C07C331/28 , A61K31/145 , A61K31/26 , A61K31/66 , C07C331/20 , C07C331/24 , C07C331/26 , C07F9/4006
摘要： Sulforaphane has been isolated and identified as a major and very potent phase II enzyme inducer in broccoli (Brassica oleracea italica). Sulforaphane is a monofunctional inducer, inducing phase II enzymes selectively without the induction of aryl hydrocarbon receptor-dependent cytochromes P-450 (phase I enzymes). Analogues differing in the oxidation state of sulfur and the number of methylene groups were synthesized, and their inducer potencies were measured. Sulforaphane is the most potent of these analogues. Other analogues having different substituent groups in place of the methylsulfinyl group of sulforaphane were also synthesized and assessed. Of these, the most potent are 6-isothiocyanato-2-hexanone and exo-2-acetyl-6-isothiocyanatonorbornane.

2. 再颁专利

USRE36784E Chemoprotective isothiocyanates 失效
标题翻译：化学保护异硫氰酸酯
公开(公告)号：USRE36784E
公开(公告)日：2000-07-18
申请号：US850387
申请日：1997-05-02
申请人： Cheon-Gyu Cho , Gary H. Posner , Paul Talalay , Yuesheng Zhang
发明人： Cheon-Gyu Cho , Gary H. Posner , Paul Talalay , Yuesheng Zhang
IPC分类号： A61K31/145 , A61K31/26 , A61K31/66 , C07C331/20 , C07C331/24 , C07C331/26 , C07C331/28 , C07F9/40 , A61K38/43 , C07C331/04
CPC分类号： C07C331/28 , A61K31/145 , A61K31/26 , A61K31/66 , C07C331/20 , C07C331/24 , C07C331/26 , C07F9/4006
摘要： Sulforaphane has been isolated and identified as a major and very potent phase II enzyme inducer in broccoli (Brassica oleracea italica). Sulforaphane is a monofunctional inducer, inducing phase II enzymes selectively without the induction of aryl hydrocarbon receptor-dependent cytochromes P-450 (phase I enzymes). Analogues differing in the oxidation state of sulfur and the number of methylene groups were synthesized, and their inducer potencies were measured. Sulforaphane is the most potent of these analogues. Other analogues having different substituent groups in place of the methylsulfinyl group of sulforaphane were also synthesized and assessed. Of these, the most potent are 6-isothiocyanato-2-hexanone and exo-2-acetyl-6-isothiocyanatonorbornane.
摘要翻译：已经分离出了萝卜硫烷，并将其鉴定为西兰花中的主要且非常有效的II期酶诱导剂（Brassica oleracea italica）。 Sulforaphane是单功能诱导剂，不依赖于芳基受体依赖的细胞色素P-450（I期酶）的诱导而选择性地诱导II期酶。合成了硫的氧化态和亚甲基数的不同的类似物，测定了它们的诱导效力。磺吡烟是这些类似物中最有效的。还合成了具有不同取代基的其他类似物代替萝卜硫代甲基亚磺酰基，并进行了评估。其中最有效的是6-异硫氰酸根合-2-己酮和外-2-乙酰基-6-异硫氰基降冰片烷。

3. 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.

4. 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。

5. 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。

6. 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。

7. 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。

8. 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。

9. 发明授权

US07417156B2 Orally active, antimalarial, anticancer, artemisinin-derived trioxane dimers 有权
标题翻译：口服活性，抗疟药，抗癌，青蒿素衍生的三恶烷二聚体
公开(公告)号：US07417156B2
公开(公告)日：2008-08-26
申请号：US10529513
申请日：2003-09-26
申请人： Gary H. Posner , Theresa A. Shapiro , Surojit Sur , Tanzina Labonte , Kristina Borstnik , Ik-Hyeon Paik , Andrew J. McRiner
发明人： Gary H. Posner , Theresa A. Shapiro , Surojit Sur , Tanzina Labonte , Kristina Borstnik , Ik-Hyeon Paik , Andrew J. McRiner
IPC分类号： A61K31/357 , C07D321/10
CPC分类号： C07D493/18
摘要： In only two steps and in 65% overall yield, natural trioxane artemisinin (I) was converted on gram scale into C-10-carba trioxane dimer (3). This new, very stable dimer was then transformed easily in one additional step into four different dimers (4-7). Alcohol and diol dimers (4 and 5) and ketone dimer (7) are 10 times more antimalarially potent in vitro than artemisinin (I), and alcohol and diol dimers (4 and 5) are strongly inhibitory but not cytotoxic toward several human cancer cell lines. Water-soluble carboxylic acid derivatives (8a-10c and 12) were easily prepared from dimers (4-6); they are thermally stable even at 60° C. for 24 hours, are more orally efficacious as antimalarials than either artelinic acid or sodium artesunate, and have potent and selective anticancer activities. Further derivitization of the alcohol dimers (4 and 17), diol dimer (5) and ketone (7) has produced a number of analogs also antimalarially active in vitro at sub-nanomolar concentrations (most notably: pyridine N-oxides (13, 15, 18, 23, 24 and 25), phosphoric acid triesters (26 and 27), sulfonamide (40) and cyclic carbonate (41)). In addition, dimers (13 and 19) are more efficacious (when administered both orally and i.v.) and less toxic (when administered intraperitoneally to mice as a single dose) than clinically-used sodium artesunate, thereby giving them a better antimalarial therapeutic index than sodium artesunate.
摘要翻译：只有两个步骤，65％的总产率，将天然的三恶烷青蒿素（I）按克标度转化为C-10-碳三三烷二聚物（3）。然后将这种新的非常稳定的二聚体在一个额外的步骤中容易地转化成四种不同的二聚体（4-7）。醇和二醇二聚体（4和5）和酮二聚体（7）在体外比青蒿素（I）具有10倍的抗疟药效力，醇和二醇二聚体（4和5）是强烈抑制的，但对几种人类癌细胞没有细胞毒性线条。水溶性羧酸衍生物（8a-10c和12）容易由二聚体（4-6）制备; 它们甚至在60℃下热稳定24小时，作为抗疟药物比阿特金酸或青蒿琥酯钠更具口服效力，并且具有有效和选择性的抗癌活性。醇二聚体（4和17），二醇二聚物（5）和酮（7）的进一步衍生产生了许多在亚纳摩尔浓度下体外抗疟活性的类似物（最引人注目的是：吡啶N-氧化物（13,15 ，18,23,24和25），磷酸三酯（26和27），磺酰胺（40）和环状碳酸酯（41））。此外，二聚体（13和19）比临床使用的青蒿琥酯钠更有效（当口服和静脉内施用）和毒性较小（当以单剂量腹膜内给予小鼠时），从而给予它们更好的抗疟治疗指数青蒿琥酯钠。

10. 发明授权

US07101865B2 24-sulfoximine vitamin D3 compounds 有权
标题翻译： 24-亚磺酰亚胺维生素D3化合物
公开(公告)号：US07101865B2
公开(公告)日：2006-09-05
申请号：US10460656
申请日：2003-06-13
申请人： Gary H. Posner , Mehmet Kahraman , Uttam Saha
发明人： Gary H. Posner , Mehmet Kahraman , Uttam Saha
IPC分类号： A61K31/59 , C07C401/00
CPC分类号： C07C401/00
摘要： The present invention provides novel sulfoximine compounds, compositions comprising these compounds and methods of using these compounds as 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-dihydroxy vitamin D3, for example, cell-proliferative disorders.
摘要翻译：本发明提供了新的磺酰亚胺化合物，包含这些化合物的组合物和使用这些化合物作为CYP24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，25-二羟维生素D 3水平的调节的疾病，例如细胞增殖性疾病。

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