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51. 发明申请

US20160031807A1 NITROXYL DONORS WITH IMPROVED THERAPEUTIC INDEX 有权
公开(公告)号：US20160031807A1
公开(公告)日：2016-02-04
申请号：US14880173
申请日：2015-10-09
申请人： Cardioxyl Pharmaceuticals, Inc.
发明人： Vincent Jacob Kalish , Frederick Arthur Brookfield , Stephen Martin Courtney , Lisa Marie Frost , John P. Toscano
IPC分类号： C07C317/14 , A61K31/24 , A61K47/40 , A61K31/222
CPC分类号： A61K31/341 , A61K9/0019 , A61K9/08 , A61K31/18 , A61K31/222 , A61K31/24 , A61K31/255 , A61K31/343 , A61K31/381 , A61K31/404 , A61K31/42 , A61K31/433 , A61K31/4436 , A61K31/5377 , A61K31/538 , A61K47/12 , A61K47/40 , C07C317/14 , C07D307/64
摘要： The disclosed subject matter provides N-substituted hydroxylamine derivative compounds, pharmaceutical compositions and kits comprising such compounds, and methods of using such compounds or pharmaceutical compositions. In particular, the disclosed subject matter provides methods of using such compounds or pharmaceutical compositions for treating heart failure.

52. 发明授权

US09238019B2 Antitussive and bronchodilator uses for enaminone ester 有权
标题翻译：镇咳药和支气管扩张剂用于烯胺酮
公开(公告)号：US09238019B2
公开(公告)日：2016-01-19
申请号：US12662364
申请日：2010-04-13
申请人： Ahmed Z. El-Hashim , Ivan O. Edafiogho , Samuel B. Kombian , Mariam H. Yousif
发明人： Ahmed Z. El-Hashim , Ivan O. Edafiogho , Samuel B. Kombian , Mariam H. Yousif
IPC分类号： A61K31/24 , A61K9/00
CPC分类号： A61K31/24 , A61K9/0019 , A61K9/0073
摘要： The antitussive and bronchodilator use for an enaminone ester relates to the use of ethyl 4-[(4-chlorophenyl)amino]-6-methyl-2-oxocyclohex-3-en-1-oate (also referred to as “enaminone E121”) for treatment of respiratory conditions, and particularly to use of the ester as the active ingredient in a cough suppressant for nonproductive cough. The ester may be used to achieve an antitussive effect, a bronchodilator effect, or both in a patient in need thereof. The ester may be formulated in any desired delivery form (such as a tablet, a capsule, a time-release capsule, a syrup, a liquid, an injection, a spray, or an inhalant), and be combined with any suitable pharmaceutical carrier, vehicles, binders, fillers, disintegrators, lubricants, solubilizers, emulsifiers, surfactants, and other excipients.
摘要翻译：用于烯胺酯的镇咳药和支气管扩张剂涉及使用4 - [（4-氯苯基）氨基] -6-甲基-2-氧代环己-3-烯-1-酸乙酯（也称为“烯胺E121” ），特别是在用于非生产性咳嗽的止咳剂中使用酯作为活性成分。该酯可以用于在有需要的患者中实现止咳作用，支气管扩张剂作用或两者。酯可以以任何期望的递送形式（例如片剂，胶囊，时间释放胶囊，糖浆，液体，注射剂，喷雾剂或吸入剂）配制，并与任何合适的药物载体组合，载体，粘合剂，填充剂，崩解剂，润滑剂，增溶剂，乳化剂，表面活性剂和其它赋形剂。

53. 发明申请

US20160002157A1 NOVEL HIGH PENETRATION DRUGS AND THEIR COMPOSITIONS THEREOF FOR TREATMENT OF PARKINSON DISEASES 有权
标题翻译：新型高渗透药物及其治疗帕金森病的组合物
公开(公告)号：US20160002157A1
公开(公告)日：2016-01-07
申请号：US14854616
申请日：2015-09-15
申请人： SUZHOU TECHFIELDS MEDICAL LTD.
发明人： Chongxi YU , Lina XU
IPC分类号： C07C317/44 , C07C271/22 , C07D211/62 , C07D471/04 , C07D321/12 , A61K31/40 , C07C219/32 , C07C219/06 , C07C327/36 , A61K31/24 , A61K31/197 , A61K31/277 , C07C237/08 , C07D207/16
CPC分类号： C07D471/04 , A61K31/137 , A61K31/195 , A61K31/197 , A61K31/198 , A61K31/24 , A61K31/277 , A61K31/40 , C07C217/60 , C07C219/06 , C07C219/10 , C07C219/14 , C07C219/28 , C07C219/32 , C07C229/12 , C07C229/36 , C07C229/58 , C07C237/06 , C07C237/08 , C07C237/20 , C07C271/16 , C07C271/22 , C07C317/44 , C07C327/30 , C07C327/36 , C07C2602/08 , C07D207/16 , C07D211/62 , C07D321/12 , C07D455/02 , C07K5/0806 , C07K5/0823 , A61K2300/00
摘要： One aspect of the invention provides a composition of novel high penetration compositions (HPC) or a high penetration prodrug (HPP) for treatment of Parkinson's disease. The HPCs/HPPs are capable of being converted to parent active drugs or drug metabolites after crossing the biological barrier and thus can render treatments for the conditions that the parent drugs or metabolites can. Additionally, the HPPs are capable of reaching areas that parent drugs may not be able to access or to render a sufficient concentration at the target areas and therefore render novel treatments. The HPCs/HPPs can be administered to a subject through various administration routes, e.g., locally delivered to an action site of a condition with a high concentration or systematically administered to a biological subject and enter the general circulation with a faster rate.
摘要翻译：本发明的一个方面提供了用于治疗帕金森病的新型高渗透组合物（HPC）或高渗透性前药（HPP）的组合物。 HPC / HPP能够在穿过生物屏障之后转化为亲本活性药物或药物代谢物，因此可以对母体药物或代谢物可以进行的处理。此外，HPP能够达到母体药物可能无法进入或在目标区域提供足够浓度的区域，从而进行新的治疗。 HPC / HPP可以通过各种施用途径施用于受试者，例如局部递送至具有高浓度或系统地施用于生物受试者的病症的作用部位并以更快的速率进入总体循环。

54. 发明授权

US09226901B2 Pharmaceutical compositions 有权
公开(公告)号：US09226901B2
公开(公告)日：2016-01-05
申请号：US14036946
申请日：2013-09-25
申请人： LOCL Pharma, Inc.
发明人： Paul Bosse , John Ameling , Bernard Schachtel , Ray Takigiku
IPC分类号： A61K9/24 , A61K9/48 , A61K9/20 , A61K31/165 , A61K31/167 , A61K31/437 , A61K31/485 , A61K31/5415 , A61K31/24 , A61K31/515
CPC分类号： A61K31/485 , A61K9/0024 , A61K9/0056 , A61K9/1694 , A61K9/2013 , A61K9/2027 , A61K9/2054 , A61K9/2086 , A61K9/209 , A61K9/4808 , A61K9/5084 , A61K31/165 , A61K31/167 , A61K31/24 , A61K31/403 , A61K31/404 , A61K31/4196 , A61K31/422 , A61K31/437 , A61K31/454 , A61K31/515 , A61K31/522 , A61K31/5415 , A61K45/06 , A61K47/36
摘要： Methods and compositions are provided which comprise effective amounts of analgesic to treat a subject, including reducing or eliminating an adverse effect associated with the analgesic.

55. 发明授权

US09198891B2 Method of treating cancer by inhibition of protein kinase-like endoplasmic reticulum protein kinase 有权
标题翻译：通过抑制蛋白激酶样内质网蛋白激酶治疗癌症的方法
公开(公告)号：US09198891B2
公开(公告)日：2015-12-01
申请号：US13111769
申请日：2011-05-19
申请人： Timothy Cardozo , Hong Wang , David Ron
发明人： Timothy Cardozo , Hong Wang , David Ron
IPC分类号： A61K49/00 , A61K31/225 , A61K31/24 , A61K31/4166 , A61K31/4245 , A61K31/428 , A61K31/433 , A61K31/496 , A61K31/519 , A61K31/536 , C07D207/416 , C07D239/42 , C07D249/12 , C07D265/22 , C07D277/44 , C07D277/54 , C07D277/66 , C07D307/54 , C07D317/60 , C07D403/04 , C07D403/06 , C07D403/12 , C07D409/12 , C07D417/14 , C07D487/04 , C12Q1/48 , G06F19/00 , G06F19/16
CPC分类号： A61K31/225 , A61K31/24 , A61K31/4166 , A61K31/4245 , A61K31/428 , A61K31/433 , A61K31/496 , A61K31/519 , A61K31/536 , C07D207/416 , C07D239/42 , C07D249/12 , C07D265/22 , C07D277/44 , C07D277/54 , C07D277/66 , C07D307/54 , C07D317/60 , C07D403/04 , C07D403/06 , C07D403/12 , C07D409/12 , C07D417/14 , C07D487/04 , C12Q1/485 , G06F19/16 , G06F19/706
摘要： The present invention relates to a method of identifying compounds useful in inhibiting protein kinase-like endoplasmic reticulum protein kinase (PERK). The method comprises providing a first model comprising PERK active domains, where the said active domains are selected from the group consisting of the peptide spanning from amino acid residue Asp144 to amino acid residue Ser191 of SEQ ID NO: 1 and a peptide comprising the amino acid residue at position 7 of SEQ ID NO: 1, providing one or more candidate compounds, evaluating contact between the candidate compounds and the first model to determine which of the one or more candidate compounds have an ability to bind to and/or fit in the first model, and identifying the compounds which, based on said evaluating, have the ability to bind to and/or fit in the first model as compounds potentially useful for inhibiting PERK. The present invention further relates to compounds that can be used for inhibition of PERK, for example human PERK, and methods related to treatment of PERK-mediated diseases.
摘要翻译：本发明涉及鉴定可用于抑制蛋白激酶样内质网蛋白激酶（PERK）的化合物的方法。该方法包括提供包含PERK活性结构域的第一模型，其中所述活性域选自跨越SEQ ID NO：1的氨基酸残基Asp144至氨基酸残基Ser191的肽和包含氨基酸的肽提供一种或多种候选化合物，评估候选化合物与第一模型之间的接触，以确定一种或多种候选化合物中的哪一种具有结合和/或适合的能力第一模型，以及鉴定基于所述评估具有结合和/或适合第一模型的能力的化合物，作为潜在地可用于抑制PERK的化合物。本发明还涉及可用于抑制PERK的化合物，例如人PERK，以及与治疗PERK介导的疾病有关的方法。

56. 发明申请

US20150320685A1 PHARMACEUTICAL COMPOSITIONS 有权
公开(公告)号：US20150320685A1
公开(公告)日：2015-11-12
申请号：US14789888
申请日：2015-07-01
申请人： LOCL PHARMA, INC.
发明人： Paul BOSSE , John AMELING , Bernard SCHACHTEL , Ray TAKIGIKU
IPC分类号： A61K9/24 , A61K31/485 , A61K31/167 , A61K31/5415
CPC分类号： A61K31/485 , A61K9/0024 , A61K9/0056 , A61K9/1694 , A61K9/2013 , A61K9/2027 , A61K9/2054 , A61K9/2086 , A61K9/209 , A61K9/4808 , A61K9/5084 , A61K31/165 , A61K31/167 , A61K31/24 , A61K31/403 , A61K31/404 , A61K31/4196 , A61K31/422 , A61K31/437 , A61K31/454 , A61K31/515 , A61K31/522 , A61K31/5415 , A61K45/06 , A61K47/36
摘要： Methods and compositions are provided which comprise effective amounts of analgesic to treat a subject, including reducing or eliminating an adverse effect associated with the analgesic.

57. 发明申请

US20150250728A1 PROCESS FOR PRODUCING SOLID PARTICLES 有权
标题翻译：生产固体颗粒的方法
公开(公告)号：US20150250728A1
公开(公告)日：2015-09-10
申请号：US14430956
申请日：2013-09-25
申请人： TAKEDA PHARMACEUTICAL COMPANY LIMITED
发明人： Naoyuki Murata , Shigeo Yanai
IPC分类号： A61K9/16 , A61K31/24
CPC分类号： A61K9/1688 , A61K9/14 , A61K31/18 , A61K31/24
摘要： A method of producing crystal of a poorly water-soluble pharmaceutical compound, including mixing a solution of a poorly water-soluble pharmaceutical compound in a good solvent and nanobubble water or an aqueous nanobubble solution to precipitate crystal of the poorly water-soluble pharmaceutical compound. The crystal of a poorly water-soluble pharmaceutical compound obtained by the method is microparticulate and has more uniform particle size distribution, and is superior in the absorbability and sustainability.
摘要翻译：一种生产水溶性差的药物化合物的方法，包括将难溶于水的药物化合物的溶液与纳米气泡水溶液或纳米气泡水溶液混合，使难溶于水的药物化合物的晶体析出。通过该方法得到的水溶性差的药物的结晶为微粒状，粒径分布更均匀，吸收性和可持续性优异。

58. 发明申请

US20150224108A1 AQUAPORIN MODULATORS AND METHODS OF USING THEM FOR THE TREATMENT OF EDEMA AND FLUID IMBALANCE 审中-公开
标题翻译：水解调节剂及其用于治疗EDEMA和流体不平衡的方法
公开(公告)号：US20150224108A1
公开(公告)日：2015-08-13
申请号：US14678818
申请日：2015-04-03
申请人： THE ARIZONA BOARD OF REGENTS ON BEHALF OF THE UNIVERSITY OF ARIZONA
发明人： Gary A. Flynn , Andrea J. Yool , Elton Rodrigues Migliati , Leslie S. Ritter
IPC分类号： A61K31/54 , A61K31/24 , A61K31/495 , A61K31/5375 , A61K31/341 , A61K31/4402 , A61K31/4409 , A61K31/443 , A61K31/496 , A61K31/196 , A61K31/4406
CPC分类号： A61K31/54 , A61K31/196 , A61K31/24 , A61K31/341 , A61K31/4402 , A61K31/4406 , A61K31/4409 , A61K31/443 , A61K31/495 , A61K31/496 , A61K31/5375 , C07C311/16 , C07C311/39 , C07D213/16 , C07D213/40 , C07D213/75 , C07D239/91 , C07D241/04 , C07D265/30 , C07D279/12 , C07D307/36 , C07D307/52 , C07D405/06 , C07D405/12 , C07D407/12
摘要： Compounds, including 3-carboxy aryl sulfonamide compounds, which agonize or antagonize aquaporin channels and methods of using them to treat disorders or diseases mediated by aquaporins.
摘要翻译：激动或拮抗水通道蛋白通道的化合物，包括3-羧基芳基磺酰胺化合物，以及使用它们治疗由水通道蛋白介导的疾病或疾病的方法。

59. 发明申请

US20150165047A1 COMPOSITIONS AND METHODS OF DELIVERY OF PHARMACOLOGICAL AGENTS 审中-公开
标题翻译：药物代谢物的组合物和方法
公开(公告)号：US20150165047A1
公开(公告)日：2015-06-18
申请号：US14626678
申请日：2015-02-19
申请人： Abraxis BioScience, LLC
发明人： Neil P. DESAI , Patrick SOON-SHIONG , Vuong TRIEU
IPC分类号： A61K47/42 , A61K31/343 , A61K31/24 , A61K31/436 , A61K31/427 , A61K31/164 , A61K31/4745 , A61K38/13 , A61K31/7048 , A61K31/05 , A61K9/107 , A61K31/337 , A61K31/165
CPC分类号： A61K47/42 , A61K9/0019 , A61K9/0078 , A61K9/107 , A61K9/1075 , A61K9/146 , A61K9/19 , A61K31/00 , A61K31/05 , A61K31/16 , A61K31/164 , A61K31/165 , A61K31/198 , A61K31/24 , A61K31/337 , A61K31/343 , A61K31/355 , A61K31/427 , A61K31/436 , A61K31/4745 , A61K31/7048 , A61K38/13 , A61K47/18 , B82Y5/00 , Y10S977/705 , Y10S977/773 , Y10S977/779 , Y10S977/906 , Y10S977/911 , A61K2300/00
摘要： The present invention relates to a pharmaceutical composition comprising a pharmaceutical agent and a pharmaceutically acceptable carrier, which carrier comprises a protein, for example, human serum albumin and/or deferoxamine. He human serum albumin is present in an amount effective to reduce one or more side effects associated with administration of the pharmaceutical composition. The inventor also provides methods for reducing on or more side effects of administration of the pharmaceutical composition, and methods for enhancing transport and binding of a pharmaceutical agent to a cell.
摘要翻译：本发明涉及包含药剂和药学上可接受的载体的药物组合物，该载体包含蛋白质，例如人血清白蛋白和/或去铁胺。他人血清白蛋白以有效降低与药物组合物的给药相关的一种或多种副作用的量存在。本发明人还提供减少药物组合物施用的副作用的方法以及用于增强药剂与细胞的转运和结合的方法。

60. 发明申请

US20150031688A1 COMPOSITIONS OF DUAL THYROINTEGRIN ANTAGONISTS AND USE IN VASCULAR-ASSOCIATED DISORDERS 有权
标题翻译：双重THYROINTEGRIN拮抗剂的组合物和用于血管相关疾病的组合物
公开(公告)号：US20150031688A1
公开(公告)日：2015-01-29
申请号：US14510506
申请日：2014-10-09
申请人： Vascular Vision Pharmaceutical Company
发明人： Shaker A. Mousa
IPC分类号： C07D279/12 , C07D213/55 , C07C271/22
CPC分类号： C07D279/12 , A61K31/195 , A61K31/24 , A61K31/27 , A61K31/4406 , A61K31/54 , C07C217/20 , C07C239/12 , C07C271/16 , C07C271/22 , C07C275/24 , C07C279/08 , C07D213/36 , C07D213/55 , C07D295/155
摘要： A dual thyrointegrin antagonist and a method for treating an angiogenesis-mediated disorder and/or a hyperthyroidism disorders by introducing the dual thyrointegrin antagonist into animals (e.g., mammals, human beings). The dual thyrointegrin antagonist includes a chemical structure having a thyroid hormone antagonist and αvβ3 integrin antagonist in the same molecule.
摘要翻译：双重甲状腺整合素拮抗剂和通过将双重甲状腺整合素拮抗剂引入动物（例如哺乳动物，人）中来治疗血管生成介导的病症和/或甲状腺功能亢进症的方法。双重甲状腺整合素拮抗剂包括在同一分子中具有甲状腺激素拮抗剂和αv＆bgr 3整合素拮抗剂的化学结构。

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