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71. 发明授权

US09481642B2 Biguanide compositions and methods of treating metabolic disorders 有权
公开(公告)号：US09481642B2
公开(公告)日：2016-11-01
申请号：US14451323
申请日：2014-08-04
申请人： Elcelyx Therapeutics, Inc.
发明人： Alain D. Baron , Mark S. Fineman , Nigel R. A. Beeley
IPC分类号： A61P3/10 , C07C279/26 , A61K9/22 , A61K31/155 , C07D317/58 , A61K31/357 , C07D307/52 , A61K31/341 , C07D249/14 , A61K31/4196 , C07D405/12 , C07D251/18 , A61K31/53 , C07D251/10 , C07D255/02 , A61K31/55 , A61K45/06 , A61K9/00 , A61K9/20 , A61K9/24 , A61K9/28 , A61K9/16 , A61K31/36 , A61K31/381 , A61K31/4453 , A61K31/343 , A61K31/40 , A61K31/454 , C07D207/06 , C07D207/34 , C07D211/14 , C07D307/66 , C07D401/04 , C07D409/12
CPC分类号： A61K31/155 , A61K9/00 , A61K9/0053 , A61K9/1623 , A61K9/20 , A61K9/2018 , A61K9/2054 , A61K9/2086 , A61K9/209 , A61K9/2846 , A61K9/2853 , A61K31/137 , A61K31/341 , A61K31/343 , A61K31/357 , A61K31/36 , A61K31/381 , A61K31/40 , A61K31/4196 , A61K31/4453 , A61K31/454 , A61K31/485 , A61K31/53 , A61K31/55 , A61K45/06 , C07C279/26 , C07D207/06 , C07D207/34 , C07D211/14 , C07D249/14 , C07D251/10 , C07D251/18 , C07D255/02 , C07D307/52 , C07D307/66 , C07D317/58 , C07D401/04 , C07D405/12 , C07D409/12
摘要： Provided herein are methods for treating certain conditions, including diabetes, obesity, and other metabolic diseases, disorders or conditions by administrating a composition comprising a biguanide or related heterocyclic compound, e.g., metformin. Also provided herein are biguanide or related heterocyclic compound compositions, and methods for the preparation thereof for use in the methods of the present invention. Also provided herein are compositions comprising metformin and salts thereof and methods of use.

72. 发明申请

US20160303115A1 OXABICYCLOHEPTANES AND OXABICYCLOHEPTENES FOR THE TREATMENT OF DEPRESSIVE AND STRESS DISORDERS 有权
标题翻译：用于治疗抑郁症和紧张症的奥沙利铂和氧化胆碱
公开(公告)号：US20160303115A1
公开(公告)日：2016-10-20
申请号：US15048389
申请日：2016-02-19
申请人： JOHN S. KOVACH , SALVATORE LECCA , MANUEL MAMELI
发明人： JOHN S. KOVACH , SALVATORE LECCA , MANUEL MAMELI
IPC分类号： A61K31/496
CPC分类号： A61K31/496 , A61K31/343 , C07D303/32 , C07D493/08
摘要： A method of treating a depressive or stress disorder in a subject afflicted therewith comprising administering to the subject an effective amount of a compound having the structure:
摘要翻译：一种治疗患有其的受试者的抑郁或应激障碍的方法，其包括向所述受试者施用有效量的具有以下结构的化合物：（I）。

73. 发明申请

US20160287554A1 Small Molecule Metal-Activated Protein Inhibition 审中-公开
标题翻译：小分子金属活化蛋白抑制
公开(公告)号：US20160287554A1
公开(公告)日：2016-10-06
申请号：US15088785
申请日：2016-04-01
申请人： Wayne Charles Guida , Robert Pleasants Sparks , Kenyon Gregory Daniel , Rainer Scott Metcalf , Sreya Mukherjee , Wesley Harrell Brooks
发明人： Wayne Charles Guida , Robert Pleasants Sparks , Kenyon Gregory Daniel , Rainer Scott Metcalf , Sreya Mukherjee , Wesley Harrell Brooks
IPC分类号： A61K31/343 , A61K31/27 , G06F19/16 , A61K31/366 , A61K31/353 , A61K31/50 , A61K9/00 , A61K31/192
CPC分类号： A61K31/343 , A61K31/192 , A61K31/27 , A61K31/353 , A61K31/366 , A61K31/50 , G16B15/00 , G16B35/00 , G16C20/50 , G16C20/60
摘要： A cancer treatment comprises the administration of a pro-drug compound identified by an in silico candidate identification screening. The pro-drug candidates are selected from a data base and calculations are carried out on the association of the pro-drug candidates to form a complex with a metal ion and a proteasome active site. The pro-drug inhibits the active site of the proteasome in the presence of the metal ion and has little or no effect in the absence of the metal ion. The pro-drug can be: 3,4-dihydroxybenzoic acid; galloflavin; 2-{[(carbamoylsulfanyl)acetyl]amino}benzoic acid; 6,7-Dihydroxycoumaranone; 3,6-bis(hydroxymethyl)pyridazin-4(1H)-one; and 4′,5,7-trihydroxyisoflavone, for binding with copper ion and proteasome.
摘要翻译：癌症治疗包括给予通过计算机候选物鉴定筛选鉴定的前药化合物。从数据库中选择前药候选物，并且对前药候选物的结合进行计算，以形成与金属离子和蛋白酶体活性位点的复合物。前药在金属离子的存在下抑制蛋白酶体的活性位点，并且在没有金属离子的情况下几乎没有或没有作用。前药可以是：3,4-二羟基苯甲酸; 姜黄素 2 - {[（氨基甲酰基硫烷基）乙酰基]氨基}苯甲酸; 6,7-二羟基香豆酮; 3,6-双（羟甲基）哒嗪-4（1H） - 酮; 和4'，5,7-三羟基异黄酮，用于与铜离子和蛋白酶体结合。

74. 发明授权

US09452107B2 Systems and methods for superdisintegrant-based composite particles for dispersion and dissolution of agents 有权
标题翻译：用于分散和溶解试剂的基于超级崩解剂的复合颗粒的系统和方法
公开(公告)号：US09452107B2
公开(公告)日：2016-09-27
申请号：US13829948
申请日：2013-03-14
申请人： Ecevit Bilgili , Rajesh Dave , Anagha Bhakay , Mohammad Azad
发明人： Ecevit Bilgili , Rajesh Dave , Anagha Bhakay , Mohammad Azad
IPC分类号： A61J3/00 , A61K9/14 , A61K9/51 , B82Y40/00 , A61J3/02
CPC分类号： A61K9/146 , A61J3/00 , A61J3/02 , A61K9/5138 , A61K9/5161 , A61K31/216 , A61K31/343 , B05D7/24 , B82Y40/00
摘要： The present disclosure provides improved systems and methods utilizing colloidal/ultrafine superdisintegrant-based composite particles for dispersion and/or dissolution of active pharmaceutical agents. In general, the present disclosure utilizes a surfactant-free or near surfactant-free formulation by incorporating a wet milled SDI as a dispersant in the formulation. As such, the present disclosure provides for the preparation of surfactant-free or substantially surfactant-free formulations (e.g., nano-composite micro-particle formulations) by incorporating a wet-milled superdisintegrant (SDI) as the dispersant in the formulations. The advantageous SDI particles (e.g., colloidal/ultrafine SDI particles) of the present disclosure can be used to break-up the aggregates (e.g., nanoparticle aggregates) of the active agents (e.g. poorly water-soluble drugs) in the formulations (e.g., micro-particle formulations) and enhance the recovery of the nanoparticles of active agents during aqueous re-dispersion and their dissolution rate in vitro and in vivo.
摘要翻译：本公开提供了改进的利用胶体/超细超级基质复合颗粒用于活性药剂的分散和/或溶解的系统和方法。通常，本公开内容通过在制剂中掺入湿法研磨的SDI作为分散剂来使用无表面活性剂的或接近表面活性剂的制剂。因此，本公开内容通过在制剂中掺入湿磨超级崩解剂（SDI）作为分散剂来提供制备不含表面活性剂的或基本不含表面活性剂的制剂（例如纳米复合微粒子制剂）。本公开的有利的SDI颗粒（例如，胶体/超细SDI颗粒）可用于分解制剂中活性剂（例如水不溶性药物）的聚集体（例如，纳米颗粒聚集体）（例如，微粒子制剂），并且在水分散分散过程中增强活性剂纳米颗粒的回收率及其在体外和体内的溶解速率。

75. 发明申请

US20160256552A1 TRANSDERMAL COLLOIDAL SOLUTION AGENT 审中-公开
标题翻译：透皮胶体溶液剂
公开(公告)号：US20160256552A1
公开(公告)日：2016-09-08
申请号：US15156244
申请日：2016-05-16
申请人： MEDRx CO., LTD
发明人： Keiko YAMASAKI
IPC分类号： A61K47/24 , A61K47/10 , A61K9/10 , A61K47/18 , A61K9/00 , A61K31/13 , A61K31/135 , A61K31/405 , A61K31/445 , A61K31/485 , A61K31/4196 , A61K31/55 , A61K31/343
CPC分类号： A61K47/24 , A61K9/0014 , A61K9/10 , A61K9/7069 , A61K31/13 , A61K31/135 , A61K31/343 , A61K31/405 , A61K31/4196 , A61K31/445 , A61K31/473 , A61K31/55 , A61K47/10 , A61K47/18 , A61K2300/00
摘要： Disclosed is a transdermal absorptive liquid preparation in which a medicament or a salt thereof is colloidally dispersed in propylene glycol or a propylene glycol-containing solvent, whose transdermal permeability of the medicament is excellent, problem of skin irritation is reduced. This transdermal absorptive liquid formulation has a mode of particle diameter at around 100 nm, and an average particle size of 50 to 500 nm. This transdermal absorptive liquid formulation makes marked improvement in the transdermal permeability by further containing an absorption promoter such as triethanolamine.
摘要翻译：公开了一种透皮吸收液体制剂，其中药物或其盐被胶体地分散在丙二醇或含丙二醇的溶剂中，其药物的透皮渗透性优异，皮肤刺激性降低。该透皮吸收性液体制剂具有约100nm的粒径模式，平均粒径为50〜500nm。该透皮吸收性液体制剂通过进一步含有吸收促进剂如三乙醇胺来显着改善透皮渗透性。

76. 发明授权

US09439216B2 Relay link HARQ operation 有权
标题翻译：中继链路HARQ操作
公开(公告)号：US09439216B2
公开(公告)日：2016-09-06
申请号：US13649872
申请日：2012-10-11
申请人： BlackBerry Limited
发明人： Yi Yu , Zhijun Cai , James Earl Womack , Andrew Mark Earnshaw
IPC分类号： H04J1/16 , H04W74/00 , H04W72/12
CPC分类号： H04B7/155 , A61K31/00 , A61K31/343 , A61K45/06 , H04B7/2606 , H04L1/16 , H04L1/18 , H04L1/1816 , H04L1/1887 , H04L5/0055 , H04L49/201 , H04L2001/0097 , H04W16/32 , H04W72/1268 , H04W72/1284 , H04W72/1294 , H04W72/14 , H04W74/004 , H04W74/0858 , A61K2300/00
摘要： A method for preventing a first network node from missing a transmission from an second network node. The method includes, when a ten millisecond periodicity is used for Multicast/Broadcast Single Frequency Network (MBSFN) subframes, setting a time between an uplink grant from the second network node to the first network node and an acknowledgement/negative-acknowledgement message (ACK/NACK) from the second network node to the first network node equal to ten milliseconds. The method further includes, when a forty millisecond periodicity is used for MBSFN subframes, the second network node sending the first network node an asynchronous grant for an uplink retransmission when a data packet is missed, and when the first network node receives the grant for the uplink retransmission, the first network node retransmitting the missed data packet.
摘要翻译：一种用于防止第一网络节点丢失来自第二网络节点的传输的方法。该方法包括：当对于组播/广播单频网络（MBSFN）子帧使用10毫秒周期时，设置从第二网络节点到第一网络节点的上行链路许可之间的时间和确认/否定确认消息（ACK / NACK）从第二网络节点到第一网络节点等于十毫秒。该方法还包括：当MBSFN子帧使用四十毫秒周期时，第二网络节点在丢失数据分组时向第一网络节点发送用于上行链路重传的异步许可，并且当第一网络节点接收到针对上行链路重传，第一网络节点重传丢失的数据分组。

77. 发明授权

US09433610B2 Compounds that enhance Atoh1 expression 有权
标题翻译：增强Atoh1表达的化合物
公开(公告)号：US09433610B2
公开(公告)日：2016-09-06
申请号：US14511911
申请日：2014-10-10
申请人： Massachusetts Eye & Ear Infirmary , The Brigham & Women's Hospital, Inc.
发明人： Albert Edge , Sang-Jun Jeon , Kathleen Seyb , Marcie Glicksman , Lixin Qiao , Gregory D. Cuny
IPC分类号： A61K31/4184 , A61K31/341 , A61K31/343 , A61K31/381 , A61K31/415 , A61K31/423 , A61K31/4245 , A61K31/426 , A61K31/428 , A61K9/00 , A61K31/353 , A61K31/4436 , A61K31/496 , A61K31/498 , A61K31/517 , A61K31/519 , A61K31/5377 , A61K35/28 , A61K35/545
CPC分类号： A61K31/5377 , A61K9/0046 , A61K31/341 , A61K31/343 , A61K31/352 , A61K31/353 , A61K31/381 , A61K31/404 , A61K31/415 , A61K31/4155 , A61K31/4184 , A61K31/4192 , A61K31/423 , A61K31/4245 , A61K31/426 , A61K31/428 , A61K31/4365 , A61K31/437 , A61K31/44 , A61K31/4436 , A61K31/4439 , A61K31/496 , A61K31/498 , A61K31/517 , A61K31/519 , A61K35/28 , A61K35/545
摘要： This invention generally provides compounds, pharmaceutical compositions, and methods for their use, which include methods that result in increased expression in an Atoh1 gene (e.g., Hath1) in a biological cell. More specifically, the invention relates to the treatment of diseases and/or disorders that would benefit from increased Atoh1 expression, e.g., a hearing impairment or imbalance disorder associated with a loss of auditory hair cells, or a disorder associated with abnormal cellular proliferation.
摘要翻译：本发明通常提供化合物，药物组合物及其使用方法，其包括导致生物细胞中Atoh1基因（例如Hath1）表达增加的方法。更具体地，本发明涉及可以从Atoh1表达增加中受益的疾病和/或病症的治疗，例如与听觉毛细胞丧失相关的听力损伤或不平衡障碍或与异常细胞增殖相关的病症。

78. 发明授权

US09422304B2 Synthesis of isohexide dicarbamates and derivatives thereof 有权
标题翻译：异己二烯二碳酸酯及其衍生物的合成
公开(公告)号：US09422304B2
公开(公告)日：2016-08-23
申请号：US14781362
申请日：2014-05-07
申请人： ARCHER DANIELS MIDLAND COMPANY
发明人： Kenneth Stensrud
IPC分类号： A61K31/34 , C07D493/04 , A61K31/40 , C07D307/12 , C07D307/42 , C08G71/04 , C08G73/00 , A61K47/26 , A61K31/428 , A61K31/343
CPC分类号： C07D307/42 , A61K31/343 , A61K31/40 , A61K31/428 , A61K47/26 , C07D307/12 , C07D493/04 , C08G12/26 , C08G71/04 , C08G73/00
摘要： Isohexide dicarbamates and a method of preparing the same are described. The method involves reacting a mixture of an isohexide and a cynate salt in a non-aqueous solvent, with a miscible acid having a pKa of about 3.7 or less. The isohexide dicarbamates can serve as precursor materials from which various derivative compounds can be synthesized.
摘要翻译：描述了异己二烯二羧酸酯及其制备方法。该方法包括使非水溶剂中的异癸酸酯和己酸盐的混合物与pKa为约3.7或更低的可混溶的酸反应。异己二烯二碳酸酯可以作为前体材料，可以从其中合成各种衍生化合物。

79. 发明申请

US20160222388A1 CHEMICAL INHIBITION OF FERROCHELATASE AS AN ANTIANGIOGENIC THERAPY 审中-公开
标题翻译：作为抗生素治疗的化学抑制作用
公开(公告)号：US20160222388A1
公开(公告)日：2016-08-04
申请号：US15009339
申请日：2016-01-28
申请人： Indiana University Research and Technology Corporation
发明人： Timothy Corson , Halesha Basavarajappa
IPC分类号： C12N15/113 , A61K31/353 , A61K39/395 , C07K16/22 , A61K31/343 , A61K9/00
CPC分类号： C12N15/1137 , A61K9/0019 , A61K31/343 , A61K31/409 , A61K31/713 , A61K45/06 , C12N2310/14 , C12Y499/01001
摘要： Methods for treating angiogenesis-mediated diseases are disclosed. More particularly, the present disclosure relates to methods of inhibiting ferrochelatase as an antiangiogenic therapy.
摘要翻译：公开了治疗血管生成介导的疾病的方法。更具体地，本公开涉及抑制铁螯合酶作为抗血管生成疗法的方法。

80. 发明申请

US20160213569A1 PHARMACEUTICAL COMPOSITIONS OF RANOLAZINE AND DRONEDARONE 审中-公开
公开(公告)号：US20160213569A1
公开(公告)日：2016-07-28
申请号：US15092126
申请日：2016-04-06
申请人： Gilead Sciences, Inc.
发明人： Michael Gerber , Neal Huang , Joanna M. Koziara , Feng Zhang
IPC分类号： A61J3/10 , A61K9/24 , A61K9/20 , A61K31/495 , A61K31/343
CPC分类号： A61J3/10 , A61K9/146 , A61K9/2027 , A61K9/2054 , A61K9/209 , A61K9/2095 , A61K31/343 , A61K31/495 , A61K47/38 , A61K2300/00
摘要： The present disclosure relates to a solid composition comprising ranolazine and a spray-dried phosphoric acid salt of dronedarone in a bilayer tablet.

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