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21. 发明申请

US20180185286A1 POROUS MATERIALS CONTAINING COMPOUNDS INCLUDING PHARMACEUTICALLY ACTIVE SPECIES 审中-公开
公开(公告)号：US20180185286A1
公开(公告)日：2018-07-05
申请号：US15301221
申请日：2015-03-31
申请人： NOVARTIS PHARMA AG , MASSACHUSETTS INSTITUTE OF TECHNOLOGY
发明人： Allan Stuart Myerson , Xiaochuan Yang , Marcus O'Mahony , Markus Krumme , Norbert Rasenack , Leia Dwyer
IPC分类号： A61K9/14 , A61K9/20 , A61K9/48 , A61K31/192 , A61K31/216 , A61K31/343 , A61K9/16
CPC分类号： A61K9/143 , A61K9/146 , A61K9/1652 , A61K9/1694 , A61K9/2009 , A61K9/485 , A61K31/192 , A61K31/216 , A61K31/277 , A61K31/343 , A61K31/397 , A61K31/405 , A61K31/4196 , A61K31/4422 , A61K31/496 , A61K31/64
摘要： Materials containing pharmaceutically active species in solid (e.g., crystal) form, and related methods, are provided, allowing for improved stability, solubility, bioavailability, and/or dissolution rates for pharmaceutically active species having poor aqueous solubility.

22. 发明授权

US09993480B2 mTOR/JAK inhibitor combination therapy 有权
公开(公告)号：US09993480B2
公开(公告)日：2018-06-12
申请号：US13399274
申请日：2012-02-17
申请人： Alessandro M. Vannucchi , Costanza Bogani , Paola Guglielmelli
发明人： Alessandro M. Vannucchi , Costanza Bogani , Paola Guglielmelli
IPC分类号： C07D487/04 , A61K31/519 , A61K31/436 , A61K45/06
CPC分类号： A61K31/519 , A61K31/436 , A61K45/06 , A61K2300/00
摘要： Provided herein is a combination therapy comprising an mTOR inhibitor and a JAK inhibitor. The combination therapy is useful for the treatment of a variety of cancers, including myeloproliferative neoplasms. The combination therapy is also useful for the treatment of any number of JAK-associated diseases.

23. 发明授权

US09458240B2 Anti-BAFFR antibody formulations 有权
标题翻译：抗BAFFR抗体制剂
公开(公告)号：US09458240B2
公开(公告)日：2016-10-04
申请号：US13991984
申请日：2011-12-08
申请人： Marta Cosenza , Christoph Heusser , Julia Neugebauer , Eveline Schaadt , Stefanie Urlinger , Maximilian Woisetschlaeger
发明人： Marta Cosenza , Christoph Heusser , Julia Neugebauer , Eveline Schaadt , Stefanie Urlinger , Maximilian Woisetschlaeger
IPC分类号： A61K39/395 , C07K16/18 , C07K16/28 , A61K9/00 , A61K9/08 , A61K9/19 , A61K47/18 , A61K47/26 , C07K14/715 , A61K39/00
CPC分类号： C07K16/2878 , A61K9/0019 , A61K9/08 , A61K9/19 , A61K39/39533 , A61K39/3955 , A61K39/39591 , A61K47/10 , A61K47/183 , A61K47/26 , A61K2039/505 , C07K2317/21 , C07K2317/56 , C07K2317/565 , C07K2317/73
摘要： Anti-BAFFR antibodies are formulated as lyophilisate or liquid formulation. The lyophilisates can be reconstituted to give a solution with a high concentration of the antibody active ingredient for delivery to a patient without high levels of antibody aggregation. The lyophilisate can be reconstituted with an aqueous reconstituent to provide an aqueous composition in which the antibody has a concentration of at least 50 mg/ml. The lyophilisate or aqueous pharmaceutical composition may include one or more of a sugar, a buffering agent, a surfactant, and/or a free amino acid.
摘要翻译：抗BAFFR抗体配制成冻干液或液体制剂。可以重构冻干物以产生具有高浓度抗体活性成分的溶液，用于递送至患者，而不需要高水平的抗体聚集。可以用水重构物重构冻干物，以提供其中抗体具有至少50mg / ml浓度的水性组合物。冻干物或水性药物组合物可以包括糖，缓冲剂，表面活性剂和/或游离氨基酸中的一种或多种。

24. 发明申请

US20140023661A1 COMBINATION THERAPY 有权
标题翻译：组合治疗
公开(公告)号：US20140023661A1
公开(公告)日：2014-01-23
申请号：US13799076
申请日：2013-03-13
申请人： Xizhong Huang , Malte Dong Eun Peters , Karl Maria Schumacher , Zhu Alexander Cao , Jennifer Lorraine Gansert , David Dong Eun Chang
发明人： Xizhong Huang , Malte Dong Eun Peters , Karl Maria Schumacher , Zhu Alexander Cao , Jennifer Lorraine Gansert , David Dong Eun Chang
IPC分类号： A61K31/4439 , A61K39/395
CPC分类号： A61K31/4439 , A61K39/3955 , A61K2039/505 , C07K16/2863 , C07K2316/96 , C07K2317/565 , C07K2317/73 , C07K2317/76 , A61K2300/00
摘要： The present invention relates to a pharmaceutical combination comprising an alpha-isoform specific phosphatidylinositol 3-kinase inhibitor compound, such as (S)-Pyrrolidine-1,2-dicarboxylic acid 2-amide 1-({4-methyl-5-[2-(2,2,2-trifluoro-1,1-dimethyl-ethyl)-pyridin-4-yl]-thiazol-2-yl}-amide), or pharmaceutically acceptable salt thereof, and an IGF1R inhibitor (e.g., the IGF1R inhibitor ANTIBODY A, or a variant or derivative thereof), a pharmaceutical composition comprising such combination, methods for treating cancer comprising administration of therapeutically effective amounts of such inhibitors to a subject in need thereof, and uses of such combination for the treatment of cancer.
摘要翻译：本发明涉及药物组合，其包含α-异构体特异性磷脂酰肌醇3-激酶抑制剂化合物，例如（S） - 吡咯烷-1,2-二羧酸2-酰胺1 - （{4-甲基-5- [2 - （2,2,2-三氟-1,1-二甲基 - 乙基） - 吡啶-4-基] - 噻唑-2-基} - 酰胺）或其药学上可接受的盐和IGF1R抑制剂（例如， IGF1R抑制剂抗体A或其变体或衍生物），包含这种组合的药物组合物，用于治疗癌症的方法，包括向有需要的受试者施用治疗有效量的这种抑制剂，以及这种组合用于治疗癌症的用途。

25. 发明授权

US07935723B2 Use of organic compounds 失效
标题翻译：使用有机化合物
公开(公告)号：US07935723B2
公开(公告)日：2011-05-03
申请号：US11628546
申请日：2005-06-03
申请人： Thomas Edward Hughes
发明人： Thomas Edward Hughes
IPC分类号： A61K31/40 , A61K31/155
CPC分类号： A61K31/00 , A61K31/155 , A61K31/40 , Y10S514/866 , Y10T436/144444 , A61K2300/00
摘要： A method for improving glucose control by administering metformin in combination with a DPP-IV inhibitor to a patient in need thereof, in an amount sufficient to control the glucose level over an extended period of time.
摘要翻译：一种通过将二甲双胍与DPP-IV抑制剂组合施用于有需要的患者，以足以在长时间内控制葡萄糖水平的量来改善葡萄糖控制的方法。

26. 发明授权

US07842688B2 Organic compounds 失效
标题翻译：有机化合物
公开(公告)号：US07842688B2
公开(公告)日：2010-11-30
申请号：US12068443
申请日：2008-02-06
申请人： Peter Herold , Robert Mah , Stefan Stutz , Aleksandar Stojanovic , Vincenzo Tschinke , Nathalie Jotterand
发明人： Peter Herold , Robert Mah , Stefan Stutz , Aleksandar Stojanovic , Vincenzo Tschinke , Nathalie Jotterand
IPC分类号： C07D401/12 , A61K31/4427
CPC分类号： C07D211/42 , C07D401/12 , C07D413/12
摘要： Novel substituted piperidines of the general formulae (I) and (II) with the substituent definitions as explained in detail in the description are described. The compounds are suitable in particular as renin inhibitors and are highly potent.
摘要翻译：描述通式（I）和（II）的新颖取代的哌啶与具有如在说明书中详细说明的取代基定义。该化合物特别适合作为肾素抑制剂，并且是非常有效的。

27. 发明申请

US20100272823A1 PULMONARY DELIVERY PARTICLES COMPRISING WATER INSOLUBLE OR CRYSTALLINE ACTIVE AGENTS 审中-公开
标题翻译：包含水不溶性或结晶活性剂的脉冲递送颗粒
公开(公告)号：US20100272823A1
公开(公告)日：2010-10-28
申请号：US12774540
申请日：2010-05-05
申请人： Thomas E. TARARA , Jeffrey G. Weers , Alexey Kabalnov , Ernest G. Schutt , Luis A. Dellamary
发明人： Thomas E. TARARA , Jeffrey G. Weers , Alexey Kabalnov , Ernest G. Schutt , Luis A. Dellamary
IPC分类号： A61K9/14 , A61K38/43 , A61K31/56 , A61K31/7088 , A61K31/713 , A61K38/00 , A61P11/00 , A61P31/00 , A61P37/08 , A61P29/00 , A61P23/00 , A61P9/00 , B29B9/12
CPC分类号： A61K9/008 , A61K9/0073 , A61K9/0075 , A61K9/0078 , A61K9/1611 , A61K9/1617 , A61K9/1635 , A61K9/1641 , A61K9/1652 , A61K9/1694 , A61K31/685 , Y10S514/937 , Y10S977/904 , Y10S977/906 , Y10S977/926
摘要： A pulmonary delivery medicament comprises a plurality of particulates, the particulates comprising a structural matrix and a water insoluble and/or crystalline active agent. The particulates have a geometric diameter of 0.5 to 50 μm. The water insoluble active agent can be a fungicide, antibiotic, budesonide. A method of making the medicament comprises forming a liquid feedstock, and forming a feedstock suspension by suspending in the liquid feedstock, the active agent and an excipient capable of forming a structural matrix, such as a phospholipid. The feedstock suspension is spray dried to produce the particulates.
摘要翻译：肺递送药物包括多个颗粒，所述颗粒包含结构基质和水不溶性和/或结晶活性剂。颗粒的几何直径为0.5至50μm。水不溶性活性剂可以是杀真菌剂，抗生素，布地奈德。制备药物的方法包括形成液体原料，并通过悬浮在液体原料，活性剂和能够形成结构基质如磷脂的赋形剂中形成原料悬浮液。将原料悬浮液喷雾干燥以产生颗粒。

28. 发明授权

US07759348B2 Pyridazine derivatives and their use as therapeutic agents 失效
标题翻译：哒嗪衍生物及其作为治疗剂的用途
公开(公告)号：US07759348B2
公开(公告)日：2010-07-20
申请号：US12036685
申请日：2008-02-25
申请人： Andreas Billich , Michael D. Winther , Yigal Paul Goldberg
发明人： Andreas Billich , Michael D. Winther , Yigal Paul Goldberg
IPC分类号： A61K31/497 , C07D403/14 , C07D403/04
CPC分类号： A61K31/00 , A61K31/501 , A61K31/551 , C07D237/20 , C07D237/24 , C07D401/12 , C07D403/12 , C07D405/12 , C07D413/12 , C07D417/12 , C07D473/00
摘要： Methods of treating an SCD-mediated skin disorder or condition in a mammal, preferably a human include administering to a mammal in need thereof a compound of formula (I): where x, y, W, V, R2, R3, R4, R5, R6, R6a, R7, R7a, R8, R8a, R9 and R9a are defined herein.
摘要翻译：在哺乳动物，优选人中治疗SCD介导的皮肤病症或病症的方法包括向有需要的哺乳动物施用式（I）化合物：其中x，y，W，V，R 2，R 3，R 4，R 5 ，R6，R6a，R7，R7a，R8，R8a，R9和R9a如本文所定义。

29. 发明授权

US07677467B2 Methods and devices for aerosolizing medicament 有权
标题翻译：用于雾化药物的方法和装置
公开(公告)号：US07677467B2
公开(公告)日：2010-03-16
申请号：US11111492
申请日：2005-04-20
申请人： James B. Fink , Nicanor A. Domingo
发明人： James B. Fink , Nicanor A. Domingo
IPC分类号： A62C35/00
CPC分类号： A61M15/0065 , A61M15/0068 , A61M15/0085 , A61M16/0858 , A61M16/125 , A61M2016/0021 , A61M2016/0024
摘要： Methods and devices are provided for aerosolizing medicament to be inhaled by a user. A housing is provided with an aerosol generator contained within the housing. A medicament feed system supplies medicament to the aerosol generator. A mouthpiece has separate medicament and air flow passages. The medicament flow passage provides aerosolized medicament from the aerosol generator to an outlet of the medicament flow passage, and the air flow passage has an inlet in fluid communication with an ambient atmosphere. The outlets of the medicament and air flow passages are provided at an end of the mouthpiece to provide simultaneous flows of medicament and air that mix in the user's mouth upon inhalation by the user at the end of the mouthpiece.
摘要翻译：提供了用于使用户吸入的药物雾化的方法和装置。壳体设置有容纳在壳体内的气溶胶发生器。药物进料系统向药物发生器提供药物。接口具有单独的药物和空气流通道。药物流动通道将气溶胶发生剂的雾化药物提供到药物流动通道的出口，并且空气流动通道具有与环境大气流体连通的入口。药物和空气流动通道的出口设置在接口管的端部，以在使用者在接口的端部吸入时混合在使用者口中的同时流动的药物和空气。

30. 发明申请

US20090308384A1 Apparatus and methods for delivery of medicament to a respiratory system 审中-公开
公开(公告)号：US20090308384A1
公开(公告)日：2009-12-17
申请号：US12583256
申请日：2009-08-17
申请人： John Power , Desmond Regan , Declan Moran
发明人： John Power , Desmond Regan , Declan Moran
IPC分类号： A61M11/00
CPC分类号： A61M16/08 , A61M15/0085 , A61M16/04 , A61M16/049 , A61M16/06 , A61M2205/8206 , A61M2205/8262 , A61M2209/082
摘要： Apparatus and methods are provided for delivery of a medicament to a respiratory system. A reservoir is provided for a liquid medicament with the reservoir having a liquid medicament inlet port and a medicament outlet. An aerosol generator is provided at the medicament outlet of the reservoir for aerosolizing the liquid medicament. A connector entrains the aerosolized medicament from the aerosol generator with a gas.

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