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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.
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公开(公告)号：US08884032B2
公开(公告)日：2014-11-11
申请号：US13321343
申请日：2010-05-19
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。
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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。
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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。
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公开(公告)号：US09493480B2
公开(公告)日：2016-11-15
申请号：US14111991
申请日：2012-04-16
申请人： Gary H. Posner , Rachel D. Slack
发明人： Gary H. Posner , Rachel D. Slack
IPC分类号： C07D493/18 , A61K45/06 , A61K31/357 , C07D493/08 , A61K31/537
CPC分类号： C07D493/18 , A61K31/357 , A61K31/537 , A61K45/06 , C07D493/08 , Y02A50/411
摘要： Anilide derivatives of the natural trioxane artemisinin were prepared and evaluated for antimalarial efficacy in Plasmodium berghei-infected mice. Selected anilides derivatives administered orally as one single-digit dose combined with mefloquine hydrochloride were completely curative, i.e., all 5 of the mice in the particular treatment group had no detectable parasitemia on day 30 post infection, gained as much weight by day 30 post infection as the control mice (no infection), and behaved normally.
摘要翻译： 制备了天然三烷青蒿素的苯胺衍生物，并评价了疟原虫感染小鼠的抗疟药效能。 口服选择的苯胺衍生物作为与盐酸甲氟喹组合的一位数剂量是完全治愈的，即特定治疗组中的所有5只小鼠在感染后第30天没有检测到的寄生虫血症，在感染后第30天获得了很大的重量 作为对照小鼠（无感染），并且表现正常。
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公开(公告)号：US09481646B2
公开(公告)日：2016-11-01
申请号：US12596252
申请日：2008-04-18
IPC分类号： C07C401/00 , C07D307/02 , C07D307/42
CPC分类号： C07C401/00 , C07C2601/14 , C07C2601/16 , C07C2602/24 , C07D307/42
摘要： The disclosure provides compounds, compositions and methods using these compounds and compositions to stimulate the differentiation of cells and inhibit excessive cell proliferation of certain cells, including cancer cells and skin cells, which may be useful in the treatment of diseases characterized by abnormal cell proliferation and/or cell differentiation such as leukemia, myelofibrosis and psoriasis without the well known effect on calcium metabolism, which gives rise to hypercalcemia.
摘要翻译： 本公开提供使用这些化合物和组合物刺激细胞分化并抑制某些细胞（包括癌细胞和皮肤细胞）的过度细胞增殖的化合物，组合物和方法，其可用于治疗以异常细胞增殖为特征的疾病， /或细胞分化例如白血病，骨髓纤维化和牛皮癣，而没有众所周知的对钙代谢的作用，其引起高钙血症。
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7.发明授权Low-calcemic 16,23-diene 25-oxime analogs of 1α,25-dihydroxy vitamin D3 有权1α，25-二羟基维生素D3的低钙16,23-二烯25-肟类似物公开(公告)号：US08906888B2
公开(公告)日：2014-12-09
申请号：US11912395
申请日：2006-04-25
申请人： Uttam Saha , Gary H. Posner , Mehmet Kahraman
发明人： Uttam Saha , Gary H. Posner , Mehmet Kahraman
IPC分类号： C07C401/00 , A61K31/593
CPC分类号： C07C401/00
摘要： The present invention provides novel 16,23-diene 25-oxime ether analogs of 1,25-dihydroxy vitamin D3, compositions comprising these compounds and methods of using these compounds as inhibitors of CYP24. In particular, the novel compound of the invention are useful for treating diseases which benefit from a modulation of the levels of 1,25-dihydroxy vitamin D3, for example, cell-proliferative disorders.
摘要翻译： 本发明提供新的1,25-二羟基维生素D3的16,23-二烯25-肟醚类似物，包含这些化合物的组合物和使用这些化合物作为CYP24抑制剂的方法。 特别地，本发明的新化合物可用于治疗受益于调节1,25-二羟维生素D3水平的疾病，例如细胞增殖性疾病。
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公开(公告)号：US20120108545A1
公开(公告)日：2012-05-03
申请号：US13321343
申请日：2010-05-19
IPC分类号： A61K31/4433 , C07D493/18 , A61K31/357 , A61K31/695 , A61P31/00 , A61P33/00 , A61P33/06 , A61K31/4706 , A61K31/4709 , A61P25/18 , A61K31/5415 , A61K31/451 , A61K31/496 , A61K31/5513 , A61K31/519 , A61K31/554 , A61P35/00 , A61P35/02 , C07D405/14
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。
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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。
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10.发明授权
公开(公告)号：US6004997A
公开(公告)日：1999-12-21
申请号：US197944
申请日：1998-11-23
申请人： Qun Y. Zheng , Christopher Murray , Randall J. Daughenbaugh , Poonsakdi Ploypradith , Gary H. Posner
发明人： Qun Y. Zheng , Christopher Murray , Randall J. Daughenbaugh , Poonsakdi Ploypradith , Gary H. Posner
IPC分类号： C07D519/00 , A61K31/335
CPC分类号： C07D519/00
摘要： Novel trioxane dimers of structure ##STR1## which possess antiproliferative and antitumor activities.
摘要翻译： 具有抗增殖和抗肿瘤活性的新型三恶烷二聚体结构。
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