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1. 发明申请

WO2016100147A1 (S)-N-(3-(6-ISOPROPOXYPYRIDIN-3-YL)-1H-INDAZOL-5-YL)-1-(2-(4-(4-(1-METHYL-1H-1,2,4-TRIAZOL-3-YL)PHENYL)-3,6-DIHYDROPYRIDIN-1(2H)-YL)-2-OXOETHYL)-3- (METHYLTHIO)PYRROLIDINE-3-CARBOXAMIDE COMPOSITIONS FOR PHARMACEUTICAL PREPARATIONS 审中-公开
标题翻译：（S）-N-（3-（6-异丙氧基吡啶-3-基）-1H-吲唑-5-基）-1-（2-（4-（4-（1-甲基-1H-1,2， 4-三唑-3-基）苯基）-3,6-二氢吡啶-1（2H） - 基）-2-氧代乙基）-3-（甲基）吡咯烷-3-羧酰胺组合物用于药物制备
公开(公告)号：WO2016100147A1
公开(公告)日：2016-06-23
申请号：PCT/US2015/065428
申请日：2015-12-14
申请人： MERCK SHARP & DOHME CORP. , GUPTA, Pranav , WAN, Jason , TRZASKA, Scott, T.
发明人： GUPTA, Pranav , WAN, Jason , TRZASKA, Scott, T.
IPC分类号： C07D401/04
CPC分类号： C07D401/14 , A61K9/4833 , A61K9/4866 , A61K31/444
摘要： A composition comprising (S)-N-(3-(6-isopropoxypyridin-3-yl)-1H-indazol-5-yl)- 1-(2(4-(4-(1-methyl-1H-1,2,4-triazol-3-yl)phenyl)-3,6-dihydropyridin-1(2H)-yl)-2-oxoethyl)-3- (methylthio)pyrrolidine-3-carboxamide and hypromellose acetate succinate for pharmaceutical preparations, especially capsule preparations.
摘要翻译：包含（S）-N-（3-（6-异丙氧基吡啶-3-基）-1H-吲唑-5-基）-1-（2（4-（4-（1-甲基-1H- 2,4-二氢吡啶-1（2H） - 基）-2-氧代乙基）-3-（甲硫基）吡咯烷-3-甲酰胺和用于药物制剂的琥珀酸羟丙甲纤维素，特别是胶囊制剂。

2. 发明申请

WO2014100077A1 GASTRO-RETENTIVE FORMULATIONS 审中-公开
标题翻译：气体保护配方
公开(公告)号：WO2014100077A1
公开(公告)日：2014-06-26
申请号：PCT/US2013/075929
申请日：2013-12-18
申请人： MERCK SHARP & DOHME CORP. , GUPTA, Pranav , SHETH, Ashlesh , SMITH, Ronald, L.
发明人： GUPTA, Pranav , SHETH, Ashlesh , SMITH, Ronald, L.
IPC分类号： A61K9/00
CPC分类号： A61K9/2086 , A61K9/0065 , A61K9/2031 , A61K9/2054 , A61K31/506 , A61K45/06
摘要： The present invention relates to pharmaceutical compositions of the poorly soluble drugs, and pharmaceutically acceptable salts thereof, in a controlled-release gastric retained oral dosage form. Such compositions are formulated so as to deliver the majority of the incorporated drug into the stomach and upper gastrointestinal tract, with restricted drug delivery in the lower gastrointestinal tract. The dosage forms have multiple layers including an active layer with a first swellable polymer with raltegravir incorporated therein and a non-active layer with a second swellable polymer having a similar molecular weight or a higher molecular weight as the swellable polymer in the active layer.
摘要翻译：本发明涉及可溶性药物的药物组合物及其药学上可接受的盐，其在控释胃内保留的口服剂型中。配制这样的组合物以将大部分并入的药物输送到胃和上消化道，并在下胃肠道中限制药物递送。剂型具有多个层，包括具有引入其中的拉尔维那韦的第一可溶胀聚合物的活性层和具有与活性层中的可溶胀聚合物相似的分子量或更高分子量的第二可溶胀聚合物的非活性层。

3. 发明申请

WO2016209787A1 SUSTAINED RELEASE FORMULATION AND TABLETS PREPARED THEREFROM 审中-公开
标题翻译：可持续发布的配方和片剂
公开(公告)号：WO2016209787A1
公开(公告)日：2016-12-29
申请号：PCT/US2016/038456
申请日：2016-06-21
申请人： MERCK SHARP & DOHME CORP. , GUPTA, Pranav , MONTEITH, David
发明人： GUPTA, Pranav , MONTEITH, David
IPC分类号： A01N57/00
CPC分类号： A61K47/32 , A61K9/20 , A61K31/519 , A61K47/00 , A61K47/10 , A61K47/12 , A61K47/34 , A61K47/38
摘要： Disclosed are formulations and tablets made therefrom comprising the compound of Formula IA or Formula IB which have sustained-release properties, and the dispersion containing the compounds of Formula IA or IB which facilitates such sustained release: Formula IA, Formula IB.
摘要翻译：公开了由其制备的制剂和片剂，其包含具有缓释性质的式IA或式IB的化合物，和含有促进这种缓释的式IA或IB化合物的分散体：式IA，式IB。

4. 发明申请

WO2017066134A1 PROCESSES FOR PREPARING FORMULATIONS FOR GASTROINTESTINAL-TARGETED THERAPIES 审中-公开
标题翻译：制备用于胃肠靶向治疗的制剂的方法
公开(公告)号：WO2017066134A1
公开(公告)日：2017-04-20
申请号：PCT/US2016/056322
申请日：2016-10-11
申请人： MERCK SHARP & DOHME CORP. , BHAMBHANI, Akhilesh , EVANS, Robert, K. , GUPTA, Pranav , SMITH, Ronald, L. , WILLIAMS, Donna. M.
发明人： BHAMBHANI, Akhilesh , EVANS, Robert, K. , GUPTA, Pranav , SMITH, Ronald, L. , WILLIAMS, Donna. M.
IPC分类号： A61K9/16 , A61K9/19 , A61K9/20 , A61K9/22 , A61K9/24 , A61K9/26
CPC分类号： A61K9/5042 , A61K9/1623 , A61K9/1652 , A61K9/5026
摘要： The present invention provides a process for preparing enterically-coated lyospheres comprising a therapeutic agent comprising: a.) providing lyospheres comprising the therapeutic agent; b.) coating said lyospheres with an enteric polymer coating composition; and c.) isolating said enterically-coated lyospheres. In other embodiments, the invention provides dosage forms comprising a lyosphere comprising an effective amount of a therapeutic agent and an enteric polymer coating. In some embodiments, the therapeutic agent in the process or dosage form is a polypeptide, a protein, a peptide, a lipopeptide, a glycoprotein, a fusion protein, a protein conjugate, a cytokine, an enzyme, an antibody, an oligonucleotide, a vaccine vector, small molecule, a live virus, an inactivated virus, a virus-like particle, a viral protein subunit, an adjuvant, microbiome, a prebiotic, a probiotic, or an ectobiotic. In some embodiments of the present invention, after oral administration the dosage forms containing the enterically-coated lyospheres provide a method of delivering a therapeutic agent to the ileum, ileo-caecal junction, colon or a combination thereof in a subject.
摘要翻译：本发明提供了制备包含治疗剂的肠溶衣包衣球的方法，其包括：a。）提供包含治疗剂的冻干球; b）用肠溶聚合物包衣组合物包衣所述冻球; 和c）分离所述肠溶衣淋球。在其他实施方案中，本发明提供了包含有效量的治疗剂和肠溶聚合物包衣的冻干球的剂型。在一些实施方案中，所述方法或剂型中的治疗剂是多肽，蛋白质，肽，脂肽，糖蛋白，融合蛋白，蛋白缀合物，细胞因子，酶，抗体，寡核苷酸，疫苗载体，小分子，活病毒，灭活病毒，病毒样颗粒，病毒蛋白亚基，佐剂，微生物组，益生元，益生菌或外生菌。在本发明的一些实施方案中，口服给药后，含有肠溶衣包衣的冻干球的剂型提供了将治疗剂递送至受试者的回肠，回盲肠连接处，结肠或其组合的方法。

5. 发明申请

WO2010042701A2 CORTICOSTEROID COMPOSITIONS AND METHODS OF TREATMENTS THEREOF 审中-公开
标题翻译：角质形成组合物及其治疗方法
公开(公告)号：WO2010042701A2
公开(公告)日：2010-04-15
申请号：PCT/US2009/059970
申请日：2009-10-08
申请人： SCHERING CORPORATION , WAN, Jiansheng , MONTEITH, David , GUPTA, Pranav , SHAH, Samir, Anupam , BERGER, Robert, L. , SEQUEIRA, Joel
发明人： WAN, Jiansheng , MONTEITH, David , GUPTA, Pranav , SHAH, Samir, Anupam , BERGER, Robert, L. , SEQUEIRA, Joel
IPC分类号： A61K9/00 , A61K9/107 , A61K9/48 , A61K31/58
CPC分类号： A61K9/0043 , A61K9/0078 , A61K9/008 , A61K9/1075 , A61K31/58 , A61K47/6951 , B82Y5/00
摘要： This invention relates to steroidal solutions for the preparation of medicaments and drug products useful for treating diseases of the upper and lower airway passages. Various embodiments of the present invention provide compositions, compositions and dosage forms with mometasone furoate in a dissolved state that are suitable for inhalation and can be used for the treatment of diseases of the upper and/or lower airway passages.
摘要翻译：本发明涉及用于制备用于治疗上，下气道通道疾病的药物和药物产品的甾体溶液。本发明的各种实施方案提供了组合物，组合物和剂型，其具有溶解状态的糠酸莫米他松，其适于吸入并且可用于治疗上部和/或下部气道通道的疾病。

6. 发明申请

WO2011019911A1 INTRAVENOUS FORMULATIONS OF NEUROKININ-1 ANTAGONISTS 审中-公开
标题翻译：神经营养因子-1拮抗剂的静脉制剂
公开(公告)号：WO2011019911A1
公开(公告)日：2011-02-17
申请号：PCT/US2010/045317
申请日：2010-08-12
申请人： OPKO HEALTH, INC. , WAN, Jiansheng , GUPTA, Pranav , MONTEITH, David , BHATTACHARYA, Soumendu
发明人： WAN, Jiansheng , GUPTA, Pranav , MONTEITH, David , BHATTACHARYA, Soumendu
IPC分类号： A01N43/42 , A61K31/44
CPC分类号： C07D471/10 , A61K9/0019 , A61K9/1075 , A61K31/44 , A61K47/14 , A61K47/24 , A61K47/44
摘要： Pharmaceutical compositions for intravenous administration comprising the compound of Formula I, or pharmaceutically acceptable salts, hydrates or prodrugs thereof are described herein. Methods of preparing the pharmaceutical compositions and methods for treating nausea and/or emesis with the pharmaceutical compositions are also described herein.
摘要翻译：本文描述了包含式I化合物或其药学上可接受的盐，水合物或前药的用于静脉内施用的药物组合物。本文还描述了制备药物组合物的方法和用药物组合物治疗恶心和/或呕吐的方法。

7. 发明申请

WO2008096372A3 PROCESS FOR PREPARING HIGHLY PURE EZETIMIBE USING NOVEL INTERMEDIATES 审中-公开
公开(公告)号：WO2008096372A3
公开(公告)日：2008-08-14
申请号：PCT/IN2008/000072
申请日：2008-02-06
申请人： IND-SWIFT LABORATORIES LIMITED , SRINIVASAN, Chidambaram, Venkateswaran , SAXENA, Rahul , GUPTA, Pranav , WADHWA, Lalit
发明人： SRINIVASAN, Chidambaram, Venkateswaran , SAXENA, Rahul , GUPTA, Pranav , WADHWA, Lalit
IPC分类号： C07D205/08 , C07D263/26
摘要： The present invention relates to an industrially advantageous process for the preparation of ezetimibe of formula (I) in high yields by using novel benzyl ester intermediates. The present invention further provides a process for the purification of ezetimibe of formula (I).

8. 发明申请

WO2012077134A1 PROCESS FOR PREPARING ARIPIPRAZOLE POLYMORPHS 审中-公开
标题翻译：制备阿维拉唑多聚物的方法
公开(公告)号：WO2012077134A1
公开(公告)日：2012-06-14
申请号：PCT/IN2011/000830
申请日：2011-12-05
申请人： IND-SWIFT LABORATORIES LIMTED , BHIRUD SHEKHAR, Bhaskar , SARIN GURDEEP, Singh , AAVULA, Sivaji , GUPTA, Pranav , NAIK RAJESH, Vinodrai
发明人： BHIRUD SHEKHAR, Bhaskar , SARIN GURDEEP, Singh , AAVULA, Sivaji , GUPTA, Pranav , NAIK RAJESH, Vinodrai
IPC分类号： C07D215/22
CPC分类号： C07D215/22
摘要： Disclosed is a process for preparing aripiprazole polymorph hydrate A, form B and type II. Also provided is a process for preparing aripiprazole polymorph having an average particle size less than 100 μιη using a specific solvent system and reaction condition for inducing precipitation.
摘要翻译：公开了制备阿立哌唑多晶型水合物A，B型和II型的方法。还提供了制备平均粒度小于100μΩ的阿立哌唑多晶型物的方法使用特定的溶剂体系和反应条件诱导沉淀。

9. 发明申请

WO2009157019A2 PROCESS FOR PREPARING EZETIMIBE USING NOVEL ALLYL INTERMEDIATES 审中-公开
标题翻译：使用全新的中间体制备EZETIMIBE的方法
公开(公告)号：WO2009157019A2
公开(公告)日：2009-12-30
申请号：PCT/IN2009/000358
申请日：2009-06-23
申请人： IND-SWIFT LABORATORIES LIMITED , CHIDAMBARAM VENKATESWARAN, Srinivasan , SARIN GURDEEP, Singh , GUPTA, Pranav , WADHWA, Lalit
发明人： CHIDAMBARAM VENKATESWARAN, Srinivasan , SARIN GURDEEP, Singh , GUPTA, Pranav , WADHWA, Lalit
IPC分类号： C07D205/08 , C07D263/26 , C07C251/24 , C07C403/12
CPC分类号： C07D205/08 , C07D263/26
摘要： The present invention provides an efficient and industrially advantageous process for the preparation of ezetimibe of formula (I), using novel intermediates.
摘要翻译：本发明提供了使用新型中间体制备式（I）的依泽麦布的有效和工业上有利的方法。

10. 发明申请

WO2008073282A2 PH SENSITIVE MATRIX FORMULATION 审中-公开
标题翻译： PH敏感矩阵制剂
公开(公告)号：WO2008073282A2
公开(公告)日：2008-06-19
申请号：PCT/US2007/025025
申请日：2007-12-06
申请人： SCHERING CORPORATION , WAN, Jiansheng , CHEN, Xiaoming , GUPTA, Pranav , MONTEITH, David
发明人： WAN, Jiansheng , CHEN, Xiaoming , GUPTA, Pranav , MONTEITH, David
IPC分类号： A61K9/20 , A61K31/155
CPC分类号： A61K31/155 , A61K9/0065 , A61K9/2027 , A61K9/2054 , A61K9/2077
摘要： The present invention provides formulations of therapeutic agents that benefit from a prolonged time of controlled release in the stomach and upper gastrointestinal (GI) tract, and from an enhanced drug exposure to the upper GI tract. The formulations of the invention comprise a therapeutic agent and one or more pH sensitive polymers that are designed for accelerated hydration, expansion, disintegration and dissolution at the higher pH of the upper GI tract, thereby, ensuring that any therapeutic agent that has not been released in the stomach is released in the upper GI tract, thus maximizing absorption of therapeutic agent that has a window of absorption located at the upper GI tract.
摘要翻译：本发明提供了受益于在胃和上胃肠（GI）道中控制释放时间延长以及来自增强的药物暴露于上胃肠道的治疗剂的制剂。本发明的制剂包含治疗剂和一种或多种pH敏感聚合物，其被设计用于在上胃肠道的较高pH下加速水合，扩张，崩解和溶解，从而确保任何尚未释放的治疗剂在上胃肠道释放胃，从而最大程度地吸收位于上胃肠道的具有吸收窗口的治疗剂。

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