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21. 发明授权

US09365609B2 Process for preparing a crystalline form of halobetasol propionate 有权
公开(公告)号：US09365609B2
公开(公告)日：2016-06-14
申请号：US13735428
申请日：2013-01-07
申请人： Taro Pharmaceutical North America, Inc.
发明人： Daniella Gutman , Shimon Chernyak
IPC分类号： A61K31/56 , C07J5/00 , C07J7/00
CPC分类号： C07J7/0085 , C07J7/00
摘要： The present invention provides a process for preparing a crystalline form of halobetasol propionate, comprising the step of crystallizing halobetasol propionate from absolute ethanol or a mixture of ethanol and water, wherein the crystalline form of halobetasol propionate is characterized by an x-ray powder diffraction pattern having peaks at 10.0, 11.6, 12.9, 13.4, 14.5, 16.4, 17.6, and 23.5±0.2 degrees 2θ.

22. 发明申请

US20150376225A1 NOVEL COMPOUNDS OF 11BETA-HYDROXY-STEROIDS FOR USE IN MITOCHONDRIA BIOGENESIS AND DISEASES ASSOCIATED WITH MITOCHONDRIAL DYSFUNCTION OR DEPLETION 审中-公开
标题翻译：用于麻醉生物制剂和与麻醉药物功能丧失相关的疾病的11BETA-羟基甾体化合物的新化合物
公开(公告)号：US20150376225A1
公开(公告)日：2015-12-31
申请号：US14762425
申请日：2014-01-23
申请人： SPHAERA PHARMA PVTD. LTD.
发明人： Sundeep Dugar , Frederic George Schreiner , Dinesh Mahajan , Amit Sharma , Ishwar Rakesh Patil , Bilash Kuila
IPC分类号： C07J17/00 , C07J3/00 , C07J43/00 , C07J1/00 , C07J21/00 , C07J7/00 , C07J5/00
CPC分类号： C07J17/00 , C07J1/0011 , C07J1/0022 , C07J3/005 , C07J5/0015 , C07J5/0053 , C07J7/0005 , C07J7/002 , C07J7/007 , C07J9/00 , C07J11/00 , C07J21/00 , C07J21/006 , C07J31/006 , C07J41/0011 , C07J41/0016 , C07J41/0038 , C07J41/005 , C07J43/003
摘要： The present invention provides novel compounds of 11β-hydroxy steroids and compositions and their application as pharmaceuticals for preventing or reversing injury to mitochondria, for treating or preventing diseases relating to mitochondrial dysfunction or depletion, and for inducing regeneration or restructuring of mitochondria as a means of treating diseases relating to abnormalities in mitochondrial structure and function in a human or animal subject. Also disclosed herein are methods for diagnosing injury to mitochondria and for diagnosing the success or failure of therapeutics designed to treat, prevent, or reverse injury to or depletion of mitochondria.
摘要翻译：本发明提供11β-羟基类固醇及其组合物的新化合物及其作为用于预防或逆转线粒体损伤的药物的用途，用于治疗或预防与线粒体功能障碍或消耗相关的疾病，以及诱导线粒体再生或重组作为手段治疗与人或动物受试者的线粒体结构和功能异常有关的疾病。本文还公开了用于诊断线粒体损伤和诊断设计用于治疗，预防或逆转线粒体损伤或消耗的治疗剂的成功或失败的方法。

23. 发明授权

US09144613B2 Halogenated phenols for diagnostics, antioxidant protection and drug delivery 有权
标题翻译：用于诊断，抗氧化保护和药物输送的卤化酚
公开(公告)号：US09144613B2
公开(公告)日：2015-09-29
申请号：US14156896
申请日：2014-01-16
申请人： Keith R. Latham
发明人： Keith R. Latham
IPC分类号： A61K49/00 , G01N33/52 , A61K51/04 , A61K49/04 , A61K47/48 , C07C43/295 , C07C217/60 , C07C323/52 , C07C229/36 , C07C233/25 , C07D475/08 , C07D489/02 , C07D499/887 , C07D209/36 , C07J1/00 , C07J5/00
CPC分类号： A61K47/48023 , A61K49/006 , A61K49/0438 , A61K51/0446 , C07C43/295 , C07C217/60 , C07C229/36 , C07C233/25 , C07C323/52 , C07D209/36 , C07D475/08 , C07D489/02 , C07D499/897 , C07J1/0022 , C07J5/0053 , G01N33/52 , Y10T436/145555
摘要： The present invention relates to a composition and method for the detection of a detectable product formed from a compound of the present invention in the body of an individual. The detectable product may include a halide or a benzenetriol-based or benzenetetrol-based product of a dehalogenation reaction in the presence of FROS. In many embodiments, an indigo-like product formed from an indigogenic compound of the present invention may also be a detectable product for diagnostic purposes. This indigo-like product may have a higher residence time in tissues where it is formed, thus providing a detectable product localized to sites of high FROS. An indigogenic compound containing one or more radioactive isotopes is further provided for therapeutic purposes.
摘要翻译：本发明涉及一种用于检测在个体内由本发明化合物形成的可检测产物的组合物和方法。可检测的产物可以包括在FROS存在下脱卤反应的卤化物或基于苯三醇或苯并四氢呋喃的产物。在许多实施方案中，由本发明的靛蓝化合物形成的靛蓝样产物也可以是用于诊断目的的可检测产物。这种靛蓝样产品可以在其形成的组织中具有更高的停留时间，从而提供定位于高FROS位点的可检测产物。进一步提供含有一种或多种放射性同位素的靛蓝化合物用于治疗目的。

24. 发明申请

US20140235600A1 NEUROACTIVE 19-ALKOXY-17-SUBSTITUTED STEROIDS, PRODRUGS THEREOF, AND METHODS OF TREATMENT USING SAME 有权
标题翻译：神经元19-烷氧基-17-取代的甾体，其制剂及其使用方法
公开(公告)号：US20140235600A1
公开(公告)日：2014-08-21
申请号：US14132386
申请日：2013-12-18
申请人： Sage Therapeutics, Inc. , Washington University
发明人： Douglas Covey , Albert Jean Robichaud
IPC分类号： C07J1/00 , C07J5/00 , C07J7/00 , C07J21/00 , C07J41/00
CPC分类号： A61K31/58 , A61K31/56 , A61K31/565 , A61K31/566 , A61K31/573 , C07J1/0011 , C07J1/0018 , C07J1/0029 , C07J5/0015 , C07J7/002 , C07J9/005 , C07J13/007 , C07J21/00 , C07J21/006 , C07J21/008 , C07J41/0005 , C07J41/0016 , C07J41/0094 , C07J51/00
摘要： The present disclosure is generally directed to neuroactive 19-alkoxy-17-substituted steroids as referenced herein, and pharmaceutically acceptable salts thereof, for use as, for example, an anesthetic, and/or in the treatment of disorders relating to GABA function and activity. The present disclosure is further directed to pharmaceutical compositions comprising such compounds.
摘要翻译：本公开一般涉及本文所提及的神经活性的19-烷氧基-17-取代的类固醇及其药学上可接受的盐，用作例如麻醉剂和/或用于治疗与GABA功能和活性有关的疾病。本公开进一步涉及包含这些化合物的药物组合物。

25. 发明授权

US08791096B2 Heat sterilization of glucocorticosteroids 有权
标题翻译：糖皮质激素加热灭菌
公开(公告)号：US08791096B2
公开(公告)日：2014-07-29
申请号：US10594861
申请日：2005-05-17
申请人： Adrian Ashley , Paul Lamb , Donald MacDonald , John Miller , Martin J. Oliver , Mathew Pollard
发明人： Adrian Ashley , Paul Lamb , Donald MacDonald , John Miller , Martin J. Oliver , Mathew Pollard
IPC分类号： A61K31/56 , A61L2/00 , C07J5/00
CPC分类号： A61K9/1682 , A61K31/56 , A61K31/573 , A61K31/58 , A61L2/0011 , A61L2/0023 , C07J5/00
摘要： The present invention provides a method for the sterilization of a labile glucocorticosteroid, which method comprises heat-treating by moist heat the labile glucocorticosteroid in the form of a suspension for a sterilizing-effective time. The methods and compositions according to the invention are useful as therapeutic tools to prevent, reverse, and/or reduce the symptoms of allergic and/or inflammatory conditions in a mammalian patient. The invention also provides methods and compositions, which may be manipulated and fine-tuned to fit the condition(s) to be treated while producing fewer side effects.
摘要翻译：本发明提供了一种灭活不稳定糖皮质激素的方法，该方法包括以悬浮液的形式将不稳定的糖皮质激素通过湿热加热灭菌有效时间。根据本发明的方法和组合物可用作预防，逆转和/或减少哺乳动物患者的过敏和/或炎症状况的治疗工具。本发明还提供方法和组合物，其可以被操纵和微调以适应待治疗的状况，同时产生更少的副作用。

26. 发明申请

US20140142078A1 NON-HORMONAL STEROID MODULATORS OF NF-kB FOR TREATMENT OF DISEASE 有权
标题翻译： NF-kB用于治疗疾病的非正性甾体调节剂
公开(公告)号：US20140142078A1
公开(公告)日：2014-05-22
申请号：US14164779
申请日：2014-01-27
申请人： ReveraGen Biopharma
发明人： John M. McCall , Eric Hoffman , Kanneboyina Nagaraju
IPC分类号： C07J5/00
CPC分类号： A61K31/573 , A61K31/57 , A61K31/575 , C07J5/0038 , C07J5/0053 , C07J5/0076 , Y02A50/479 , Y10S514/825 , Y10S514/826 , Y10S514/903
摘要： The present invention relates to compounds and methods which may be useful as treatments of neuromuscular diseases such as muscular dystrophy, and as inhibitors of NF-κB for the treatment or prevention of muscular wasting disease, including muscular dystrophy.
摘要翻译：本发明涉及可用作治疗神经肌肉疾病如肌营养不良的化合物和方法，以及作为NF-κB抑制剂用于治疗或预防肌肉萎缩性疾病，包括肌营养不良症的化合物和方法。

27. 发明授权

US08679512B2 Topical formulation comprising a corticosteroid as active ingredient 失效
标题翻译：包含皮质类固醇作为活性成分的局部制剂
公开(公告)号：US08679512B2
公开(公告)日：2014-03-25
申请号：US13462245
申请日：2012-05-02
申请人： Salvatore Criscione
发明人： Salvatore Criscione
IPC分类号： A61K9/12 , A61K9/14 , A61K9/16 , C07J5/00
CPC分类号： A61K31/573 , A61K9/0014 , A61K9/10 , A61K9/12 , A61K47/10 , A61K47/26 , A61K47/38
摘要： Topically administering a propellant-free formulation as a spray in the form of aqueous suspension of drug particles, wherein said formulation consists essentially of: micronized particles of beclometasone dipropionate (BDP) suspended in an aqueous phase, said aqueous phase comprising: an emulsifying agent selected from the class of polysorbates in an amount of 0.1 to 0.2% w/v, based on the total volume of the formulation; a sugar or a sugar alcohol in an amount of 5.0 to 5.2% w/v, based on the total volume of the formulation; a mixture of microcrystalline cellulose and carboxymethylcellulose sodium in an amount of 0.5 to 1.0% w/v, based on the total volume of the formulation; one or more preservatives; and water up to 100%, is effective for the prophylaxis and/or treatment of a dermatological disease such as atopic dermatitis, acne and psoriasis.
摘要翻译：以药物颗粒的水性悬浮液的形式局部施用无推进剂的制剂作为喷雾，其中所述制剂基本上由以下组成：悬浮在水相中的二丙酸倍氯米松（BDP）的微粉化颗粒，所述水相包含：选择的乳化剂基于制剂的总体积从0.1至0.2％w / v的量的聚山梨酸酯类; 基于制剂的总体积，5.0至5.2％w / v的糖或糖醇; 基于制剂总体积的0.5-1.0％w / v的微晶纤维素和羧甲基纤维素钠的混合物; 一种或多种防腐剂; 和高达100％的水，对于预防和/或治疗皮肤病如特应性皮炎，痤疮和牛皮癣是有效的。

28. 发明授权

US08586770B2 Unsaturated steroid compounds 有权
标题翻译：不饱和类固醇化合物
公开(公告)号：US08586770B2
公开(公告)日：2013-11-19
申请号：US13030326
申请日：2011-02-18
申请人： James M. Frincke
发明人： James M. Frincke
IPC分类号： C07J1/00 , C07J3/00 , C07J5/00 , C07J7/00 , C07J9/00 , C07J41/00 , A61K31/56
CPC分类号： A61K31/56 , A61K31/568 , A61K31/569 , A61K47/6951 , A61K49/0004 , A61K51/00 , B82Y5/00
摘要： The invention relates to methods to manipulate stem cells in vivo and in vitro to treat, e.g., a condition where cell or tissue repair is needed.
摘要翻译：本发明涉及在体内和体外操纵干细胞以治疗例如需要细胞或组织修复的病症的方法。

29. 发明授权

US08518920B2 Glucocorticoids attached to nitrate esters via an aromatic linker in position 21 and their use in ophthalmology 有权
公开(公告)号：US08518920B2
公开(公告)日：2013-08-27
申请号：US13056921
申请日：2009-07-07
申请人： Francesca Benedini , Annalisa Bonfanti , Valerio Chiroli , Rebecca Steele , Ennio Ongini , Stefano Biondi
发明人： Francesca Benedini , Annalisa Bonfanti , Valerio Chiroli , Rebecca Steele , Ennio Ongini , Stefano Biondi
IPC分类号： A61K31/58 , A61K31/573 , C07J5/00 , C07J71/00
CPC分类号： C07J71/0031 , C07J41/005
摘要： The invention relates to nitrooxy derivatives of fluocinolone acetonide, triamcinolone acetonide, betamethasone and beclomethasone, methods for their preparation, pharmaceutical compositions containing these compounds, and methods of using these compounds and compositions for treating diabetic macular edema, diabetic retinopathy, macular degeneration, age-related macular degeneration and other diseases of retina and macula lutea.

30. 发明授权

US08258124B2 Combination medicament 有权
标题翻译：组合药物
公开(公告)号：US08258124B2
公开(公告)日：2012-09-04
申请号：US12973350
申请日：2010-12-20
申请人： Christian Weimar , Klaus Dietzel , Helgert Müller , Degenhard Marx
发明人： Christian Weimar , Klaus Dietzel , Helgert Müller , Degenhard Marx
IPC分类号： A01N45/00 , A61K31/56 , A61K31/58 , C07J71/00 , C07J5/00 , C07J7/00
CPC分类号： A61K31/575
摘要： The subject matter of this application relates to the combination of ciclesonide or an epimer thereof with R,R-formoterol or a salt, or a hydrate of a salt thereof.
摘要翻译：本申请的主题涉及环索奈德或其差向异构体与R，R-福莫特罗或其盐或其盐的水合物的组合。

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