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71. 发明授权

US09132125B2 Benzoic acid, benzoic acid derivatives and heteroaryl carboxylic acid conjugates of hydrocodone, prodrugs, methods of making and use thereof 有权
标题翻译：苯酮，苯甲酸衍生物和氢可酮的杂芳基羧酸共轭物，前药，其制备方法和用途
公开(公告)号：US09132125B2
公开(公告)日：2015-09-15
申请号：US14557570
申请日：2014-12-02
申请人： KemPharm, Inc.
发明人： Travis Mickle , Sven Guenther , Christal Mickle , Guochen Chi , Jaroslaw Kanski , Andrea K. Martin , Bindu Bera
IPC分类号： A61K45/06 , A61K31/485 , A61K47/48 , C07D491/08 , C07D489/04 , A61K31/167
CPC分类号： A61K47/545 , A61K9/0019 , A61K9/20 , A61K9/2054 , A61K31/167 , A61K31/485 , A61K45/06 , A61K47/542 , A61K47/55 , A61K47/556 , A61P25/30 , C07D489/02 , C07D489/04 , C07D491/08 , A61K2300/00
摘要： The presently described technology provides compositions comprising aryl carboxylic acids chemically conjugated to hydrocodone (morphinan-6-one, 4,5-alpha-epoxy-3-methoxy-17-methyl) to form novel prodrugs/compositions of hydrocodone, including benzoates and heteroaryl carboxylic acids, which have a decreased potential for abuse of hydrocodone. The present technology also provides methods of treating patients, pharmaceutical kits and methods of synthesizing conjugates of the present technology.
摘要翻译：目前描述的技术提供包含与氢可酮（吗啡喃-6-酮，4,5-α-环氧-3-甲氧基-17-甲基）化学偶联的芳基羧酸的组合物，以形成新的前药/氢可酮组合物，包括苯甲酸酯和杂芳基羧酸，其潜在的潜在滥用氢可酮。本技术还提供了治疗患者的方法，药物试剂盒和本技术合成缀合物的方法。

72. 发明申请

US20150238618A1 FATTY ACID FUMARATE DERIVATIVES AND THEIR USES 有权
标题翻译：脂肪酸的FUMARATE衍生物及其用途
公开(公告)号：US20150238618A1
公开(公告)日：2015-08-27
申请号：US14635567
申请日：2015-03-02
申请人： Catabasis Pharmaceuticals, Inc.
发明人： Jill C. Milne , Michael R. Jirousek , Jean E. Bemis , Chi B. Vu
IPC分类号： A61K47/48 , A61K31/385 , A61K31/495 , A61K31/4015 , A61K31/221 , A61K31/197
CPC分类号： C07C235/76 , A61K31/195 , A61K31/197 , A61K31/221 , A61K31/225 , A61K31/385 , A61K31/4015 , A61K31/495 , A61K47/55 , C07C233/20 , C07C233/38 , C07C233/49 , C07C323/41 , C07D207/14 , C07D207/40 , C07D207/416 , C07D241/04 , C07D295/18 , C07D339/04
摘要： The invention relates to Fatty Acid Fumarate Derivatives; compositions comprising an effective amount of a Fatty Acid Fumarate Derivative; and methods for treating or preventing cancer, a metabolic disorder or neurodegenerative disorder comprising the administration of an effective amount of a Fatty Acid Fumarate Derivative.
摘要翻译：本发明涉及富马酸脂肪酸衍生物; 包含有效量的富马酸脂肪酸衍生物的组合物; 以及用于治疗或预防癌症，代谢紊乱或神经变性疾病的方法，包括施用有效量的富马酸脂肪酸衍生物。

73. 发明申请

US20150202313A1 Macromolecular Prodrugs for Hard Tissue and Methods of Use Thereof 审中-公开
标题翻译：用于硬组织的大分子前药及其使用方法
公开(公告)号：US20150202313A1
公开(公告)日：2015-07-23
申请号：US14424737
申请日：2013-09-03
申请人： New York Society for The Ruptured and Crippled Maintaining The Hospital for Special Surgery , Board of Regents of the University of Nebraska
发明人： Dong Wang , Zhenshan Jia , Yijia Zhang , Steven R. Goldring , Aaron Daluiski
IPC分类号： A61K47/48 , A61K49/00 , A61K31/366
CPC分类号： A61K47/48215 , A61K31/366 , A61K31/74 , A61K47/55 , A61K47/60 , A61K47/6907 , A61K49/00
摘要： Methods and compositions for treating bone disorders are disclosed.
摘要翻译：公开了用于治疗骨骼疾病的方法和组合物。

74. 发明申请

US20150158869A1 PYRROLOBENZODIAZEPINES AS UNSYMMETRICAL DIMERIC PBD COMPOUNDS FOR INCLUSION IN TARGETED CONJUGATES 有权
标题翻译：作为非对称双极性PBD化合物，用于包含在目标结合物中的吡咯烷酮
公开(公告)号：US20150158869A1
公开(公告)日：2015-06-11
申请号：US14346006
申请日：2012-09-20
申请人： SPIROGEN SÀRL
发明人： Philip Wilson Howard
IPC分类号： C07D487/04 , A61K47/48 , C07K5/062
CPC分类号： C07D487/04 , A61K47/54 , A61K47/55 , A61K47/60 , C07D519/00 , C07K5/06026 , C07K5/06034 , C07K5/06043 , C07K5/06052 , C07K5/06078 , C07K5/06156 , C07K5/06165
摘要： A compound with the formula I wherein: R2 is of formula II where Q is selected from OH, SH and NRN, and RN is selected from H, methyl and ethyl, as well as drug-linkers and drug-conjugates made from this compound.
摘要翻译：具有式I的化合物，其中：R2为式II，其中Q选自OH，SH和NRN，RN选自H，甲基和乙基，以及由该化合物制备的药物接头和药物偶联物。

75. 发明申请

US20150141513A1 COMPOSITIONS AND METHODS FOR THE TREATMENT OF NEUROLOGICAL DEGENERATIVE DISORDERS AND NEUROLOGICAL DISEASES 审中-公开
标题翻译：治疗神经衰弱性疾病和神经病变的组合物和方法
公开(公告)号：US20150141513A1
公开(公告)日：2015-05-21
申请号：US14399172
申请日：2013-04-19
申请人： Mahesh Kandula
发明人： Mahesh Kandula
IPC分类号： A61K47/48 , C07C317/24
CPC分类号： A61K47/481 , A61K31/165 , A61K47/542 , A61K47/543 , A61K47/55 , A61K47/557 , C07C317/24 , C07C317/44
摘要： The invention relates to the compounds of formula I or its pharmaceutical acceptable salts, as well as polymorphs, solvates, enantiomers, stereoisomers and hydrates thereof. The pharmaceutical compositions comprising an effective amount of compounds of formula I, and methods for the treatment of neurological degenerative disorders and neurological diseases may be formulated for oral, buccal, rectal, topical, transdermal, transmucosal, intravenous, parenteral administration, syrup, or injection. Such compositions may be used to treatment of narcolepsy, shift work sleep disorder, and as an adjunct treatment for obstructive sleep apnea/hypopnea, hypersomnias, like idiopathic hypersomnia, Psychiatric/neurodegenerative disorders, ADHD, Psychiatric/neurodegenerative disorders, Depersonalization disorder, Cognitive enhancement, Fatigue, Post-chemotherapy cognitive impairment and weight loss.
摘要翻译：本发明涉及式I化合物或其药学上可接受的盐，以及其多晶型物，溶剂合物，对映体，立体异构体和水合物。包含有效量的式I化合物的药物组合物和治疗神经退行性疾病和神经疾病的方法可以配制用于口服，口腔，直肠，局部，透皮，经粘膜，静脉内，肠胃外给药，糖浆或注射。此类组合物可用于治疗发作性睡病，转移睡眠障碍，以及作为阻塞性睡眠呼吸暂停/呼吸不足的睡眠呼吸障碍，嗜睡症，特发性睡眠过多，精神病/神经退行性疾病，ADHD，精神病/神经变性疾病，非人群化障碍，认知增强，疲劳，化疗后认知障碍和体重减轻。

76. 发明申请

US20150126450A1 MULTIVALENT PEPTOID OLIGOMERS, PHARMACEUTICAL COMPOSITIONS AND METHODS OF USING SAME 审中-公开
标题翻译：多功能磷脂寡聚体，药物组合物及其使用方法
公开(公告)号：US20150126450A1
公开(公告)日：2015-05-07
申请号：US14394996
申请日：2013-04-16
申请人： NEW YORK UNIVERSITY
发明人： Kent Kirshenbaum , Paul Michael Levine , Michael John Garabedian
IPC分类号： A61K47/48 , C07K7/64 , C07K7/08 , C07K14/00 , C07K5/083 , C07K7/06
CPC分类号： A61K47/554 , A61K38/00 , A61K47/55 , A61K47/59 , A61K47/64 , C07K5/0806 , C07K5/1008 , C07K7/06 , C07K7/08 , C07K7/64 , C07K14/001
摘要： Novel peptoid oligomers are disclosed that have a formula represented by the following formula Ia or Ib: The peptoid oligomers are prepared as modulators of androgen receptor (AR), and may be prepared as pharmaceutical compositions and used for the prevention or treatment of a variety of conditions in mammals, including humans, associated with unwanted or aberrant AR activity. The present peptoid oligomers are particularly valuable for the treatment of subjects with cancer.
摘要翻译：公开了具有由下式Ia或Ib表示的式的新型拟肽低聚物：拟肽寡聚体被制备为雄激素受体（AR）的调节剂，并且可以制备为药物组合物并用于预防或治疗各种哺乳动物（包括人类）与不想要的或异常的AR活动有关的病症。本发明的拟肽寡聚体对于治疗患有癌症的受试者是特别有价值的。

77. 发明授权

US08993278B2 Conjugates for cancer therapy and diagnosis 有权
标题翻译：用于癌症治疗和诊断的共轭物
公开(公告)号：US08993278B2
公开(公告)日：2015-03-31
申请号：US13164204
申请日：2011-06-20
申请人： Stela Gengrinovitch , Esther Izakovich
发明人： Stela Gengrinovitch , Esther Izakovich
IPC分类号： C12P13/20 , C12P13/04 , C12P13/14 , G01N33/574 , A61P35/00 , A61K47/48
CPC分类号： A61K47/48038 , A61K47/481 , A61K47/542 , A61K47/55
摘要： The present invention relates to conjugates of a drug and an amino acid or an amino acid derivative or analog, pharmaceutical compositions that include the conjugates and methods of use thereof. In particular, the present invention relates to conjugates of anti-proliferative drugs and asparagine and glutamine and analogs thereof as compositions for treatment of cancer, and conjugates of imaging agent carriers and amino acids for the diagnosis of tumors and metastases.
摘要翻译：本发明涉及药物和氨基酸或氨基酸衍生物或类似物的缀合物，包括缀合物的药物组合物及其使用方法。特别地，本发明涉及抗增殖药物和天冬酰胺和谷氨酰胺及其类似物作为治疗癌症的组合物的缀合物，以及用于诊断肿瘤和转移瘤的成像剂载体和氨基酸的缀合物。

78. 发明授权

US08969377B2 Compounds and methods for inhibiting NHE-mediated antiport in the treatment of disorders associated with fluid retention or salt overload and gastrointestinal tract disorders 有权
标题翻译：用于抑制NHE介导的止痒剂用于治疗与流体保留或盐过载和胃肠道疾病相关的疾病的化合物和方法
公开(公告)号：US08969377B2
公开(公告)日：2015-03-03
申请号：US13804752
申请日：2013-03-14
申请人： Ardelyx, Inc.
发明人： Noah Bell , Christopher Carreras , Dominique Charmot , Jeffrey W Jacobs , Michael Robert Leadbetter , Marc Navre
IPC分类号： A61K31/18 , C07F9/60 , A61K31/472 , A61K31/4725 , A61K31/517 , A61K31/662 , A61K31/675 , A61K45/06 , C07C311/29 , C07D217/04 , C07D217/14 , C07D401/12 , C07F9/38 , C07F9/576 , C07F9/6558 , C07D217/16 , C07D215/14
CPC分类号： A61K31/4725 , A61K31/18 , A61K31/472 , A61K31/517 , A61K31/662 , A61K31/675 , A61K45/06 , A61K47/55 , A61P1/00 , A61P7/10 , A61P9/04 , A61P9/12 , C07C311/29 , C07D215/14 , C07D217/04 , C07D217/14 , C07D217/16 , C07D401/12 , C07F9/3808 , C07F9/3834 , C07F9/3882 , C07F9/5765 , C07F9/60 , C07F9/65583
摘要： The present disclosure is directed to compounds of the structure (X): wherein: n is 2 or 3; NHE has the structure wherein: R1 is H or —SO2—NR7R8—; R2 is selected from H, —NR7(CO)R8, —SO2—NR7R8— and —NR7R8; R3 is hydrogen; R7 is hydrogen; R8 is a bond linking to L; L is a polyalkylene glycol linker; and Core has the following structure: wherein: X is selected from the group consisting of a bond, —O—, —NH—, NHC(═O)—, —NHC(═O)NH— and —NHSO2—; and Y is selected from the group consisting of a bond, optionally substituted C1-6 alkylene, optionally substituted benzene, pyridinyl, a polyethylene glycol linker and —(CH2)1-6O(CH2)1-6—, and methods of using such compounds for the treatment of irritable bowel syndrome, chronic kidney disease and end-stage renal disease.
摘要翻译：本公开涉及结构（X）的化合物：其中：n为2或3; NHE具有以下结构：其中：R1是H或-SO2-NR7R8-; R2选自H，-NR7（CO）R8，-SO2-NR7R8-和-NR7R8; R3是氢; R7是氢; R8是连接L的键; L是聚亚烷基二醇连接体; 和Core具有以下结构：其中：X选自键，-O - ， - NH - ，NHC（= O） - ， - NHC（= O）NH-和-NHSO 2 - ; 和Y选自由以下组成的组：任选取代的C 1-6亚烷基，任选取代的苯，吡啶基，聚乙二醇连接体和 - （CH 2）1-6 O（CH 2）1-6 - 用于治疗肠易激综合征，慢性肾脏疾病和终末期肾病的化合物。

79. 发明授权

US08969354B2 Fatty acid fumarate derivatives and their uses 有权
标题翻译：富马酸脂肪酸衍生物及其用途
公开(公告)号：US08969354B2
公开(公告)日：2015-03-03
申请号：US13673588
申请日：2012-11-09
申请人： Jill C. Milne , Michael R. Jirousek , Jean E. Bemis , Chi B. Vu
发明人： Jill C. Milne , Michael R. Jirousek , Jean E. Bemis , Chi B. Vu
IPC分类号： A61K31/4965 , A61K31/40 , C07C233/00 , C07D295/00 , C07D207/00 , C07D339/02 , C07C233/49 , C07D295/18 , C07C233/38 , C07D207/40 , A61K47/48 , C07D241/04 , C07D339/04 , C07C323/41 , C07C233/20
CPC分类号： C07C235/76 , A61K31/195 , A61K31/197 , A61K31/221 , A61K31/225 , A61K31/385 , A61K31/4015 , A61K31/495 , A61K47/55 , C07C233/20 , C07C233/38 , C07C233/49 , C07C323/41 , C07D207/14 , C07D207/40 , C07D207/416 , C07D241/04 , C07D295/18 , C07D339/04
摘要： The invention relates to Fatty Acid Fumarate Derivatives; compositions comprising an effective amount of a Fatty Acid Fumarate Derivative; and methods for treating or preventing cancer, a metabolic disorder or neurodegenerative disorder comprising the administration of an effective amount of a Fatty Acid Fumarate Derivative.
摘要翻译：本发明涉及富马酸脂肪酸衍生物; 包含有效量的富马酸脂肪酸衍生物的组合物; 以及用于治疗或预防癌症，代谢紊乱或神经变性疾病的方法，包括施用有效量的富马酸脂肪酸衍生物。

80. 发明申请

US20150050313A1 NOVEL IMMUNOSTIMULANTS AND SYNTHESIS THEREOF 审中-公开
标题翻译：新型免疫球蛋白及其合成
公开(公告)号：US20150050313A1
公开(公告)日：2015-02-19
申请号：US14458988
申请日：2014-08-13
申请人： The Regents of the University of California
发明人： Rock J. Mancini , Janine K. Tom , Aaron P. Esser-Kahn
IPC分类号： C07H21/04 , A61K31/80 , C08G65/335
CPC分类号： A61K31/80 , A61K47/549 , A61K47/55 , A61K47/64 , C08G65/329 , C08G65/331 , C08G65/3311 , C08G65/333 , C08G65/33303 , C08G65/33331 , C08G65/334 , C08G65/3342 , C08G65/3356 , C08G65/3358
摘要： Disclosed herein are heteromeric molecules comprising two or more different pathogen associated molecular patterns (PAMPs), wherein the two or more PAMPs are linked together with discrete, linear inter-PAMP spacing. Also disclosed are immunogenic compositions comprising the heteromeric molecules and related methods of stimulating an immune response in vivo in a subject or ex vivo comprising administering the immunogenic composition to cells. Also disclosed is a method of synthesizing an immunostimulant comprising: identifying 2 or more different PAMPS, covalently linking the 2 or more different PAMPS together, varying spacing between the 2 or more different PAMPs, and testing the effect of spacing between the 2 or more different PAMPS to identify an optimal spacing that results in immune stimulation.
摘要翻译：本文公开了包含两种或更多种不同的病原体相关分子模式（PAMP）的异聚分子，其中两个或更多个PAMP通过离散的线性间隔间隔间隔连接在一起。还公开了包含异源分子的免疫原性组合物和在受试者体内刺激免疫应答或离体的相关方法，包括向细胞施用免疫原性组合物。还公开了合成免疫刺激剂的方法，其包括：鉴定2种或更多种不同的PAMPS，将2种或更多种不同PAMPS共价连接在一起，改变2种或更多种不同PAMP之间的间隔，并测试2种或更多种不同PAMP之间的间隔效应 PAMPS识别导致免疫刺激的最佳间距。

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