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1. 发明申请

WO2013181174A2 SOLID DOSAGE FORMULATIONS OF AN OREXIN RECEPTOR ANTAGONIST 审中-公开
标题翻译： OREXIN受体拮抗剂的固体剂量配方
公开(公告)号：WO2013181174A2
公开(公告)日：2013-12-05
申请号：PCT/US2013/042959
申请日：2013-05-29
申请人： MERCK SHARP & DOHME CORP. , HARMON, Paul, A. , VARIANKAVAL, Narayan
发明人： HARMON, Paul, A. , VARIANKAVAL, Narayan
IPC分类号： A61K47/32 , A61K31/551
CPC分类号： A61K31/551 , A61K9/2013 , A61K9/2018 , A61K9/2027 , A61K9/2054 , A61K47/32 , A61K47/38
摘要： The present invention is directed to a pharmaceutical composition comprising the compound suvorexant, or a pharmaceutically acceptable salt thereof, a concentration-enhancing polymer, and optionally a pharmaceutically acceptable surfactant.
摘要翻译：本发明涉及一种药物组合物，其包含化合物促氧化剂或其药学上可接受的盐，浓度增强聚合物和任选的药学上可接受的表面活性剂。

2. 发明申请

WO2013181174A3 SOLID DOSAGE FORMULATIONS OF AN OREXIN RECEPTOR ANTAGONIST 审中-公开
标题翻译： OREXIN受体拮抗剂的固体剂量配方
公开(公告)号：WO2013181174A3
公开(公告)日：2014-01-30
申请号：PCT/US2013042959
申请日：2013-05-29
申请人： MERCK SHARP & DOHME , HARMON PAUL A , VARIANKAVAL NARAYAN
发明人： HARMON PAUL A , VARIANKAVAL NARAYAN
IPC分类号： A61K31/551
CPC分类号： A61K31/551 , A61K9/2013 , A61K9/2018 , A61K9/2027 , A61K9/2054 , A61K47/32 , A61K47/38
摘要： The present invention is directed to a pharmaceutical composition comprising the compound suvorexant, or a pharmaceutically acceptable salt thereof, a concentration-enhancing polymer, and optionally a pharmaceutically acceptable surfactant. The concentration-enhancing polymer is a polymer that forms an amorphous dispersion with suvorexant, that is insoluble or almost completely insoluble in water by (a) dissolving the suvorexant or (b) interacting with the suvorexant in such a way that the suvorexant does not form crystals or crystalline domains in the polymer. A concentration-enhancing polymer is water soluble or readily disperse in water, so that when the polymer is placed in water or an aqueous environment (e.g. fluids in the gastrointestinal (Gl) tract or simulated Gl fluids), the solubility and/or bioavailability of suvorexant is increased over the solubility or bioavailability in the absence of the polymer.
摘要翻译：本发明涉及一种药物组合物，其包含化合物促氧化剂或其药学上可接受的盐，浓度增强聚合物和任选的药学上可接受的表面活性剂。浓度增强聚合物是通过（a）将suvorexant溶解或（b）与suvorexant相互作用以使得suvorexant不形成的方式形成具有suvorexant的无定形分散体的聚合物，其不溶或几乎完全不溶于水聚合物中的晶体或结晶域。浓度增强聚合物是水溶性的或容易分散在水中，使得当聚合物置于水或水性环境（例如胃肠道（G1）道或模拟的Gl液中的流体）时，溶解度和/或生物利用度在不存在聚合物的情况下，苏维素增加超过溶解度或生物利用度。

3. 发明申请

WO2013055609A1 PHARMACEUTICAL COMPOSITIONS THAT INHIBIT DISPROPORTIONATION 审中-公开
标题翻译：禁止分解的药物组合物
公开(公告)号：WO2013055609A1
公开(公告)日：2013-04-18
申请号：PCT/US2012/059172
申请日：2012-10-08
申请人： MERCK SHARP & DOHME CORP. , JOHN, Christopher, T. , HARMON, Paul, A.
发明人： JOHN, Christopher, T. , HARMON, Paul, A.
IPC分类号： A01N25/00
CPC分类号： A61K47/12 , A61K9/2013 , A61K9/2054 , A61K31/4439
摘要： Pharmaceutical formulations comprising solid pharmaceutically acceptable organic acids, such as maleic acid or tartaric acid, that inhibit the disproportionation of pharmaceutically acceptable acid salts of active pharmaceutical ingredients, and methods of manufacturing such pharmaceutical compositions. The pharmaceutically acceptable acid salt of the active pharmaceutical ingredient has a pKa of less than about 6.0, and wherein the solid pharmaceutically acceptable organic acid has a pKa of less than about 4.0 and an aqueous solubility in the range of about 500 to about 2000 milligrams per milliliter. A pharmaceutical formulation comprising a pharmaceutical acceptable acid salt of pioglitazone, a solid pharmaceutically acceptable organic acid selected from the group consisting of maleic acid or tartaric acid, and an excipient that promotes disproportionation, wherein the ratio by weight of the solid pharmaceutically acceptable organic acid to excipient is from about 1 :6 to about 1: 1.
摘要翻译：包含抑制活性药物成分的药学上可接受的酸盐的歧化的固体药学上可接受的有机酸如马来酸或酒石酸的药物制剂，以及制造这种药物组合物的方法。活性药物成分的药学上可接受的酸盐的pKa小于约6.0，并且其中固体药学上可接受的有机酸的pKa小于约4.0，水溶解度在约500至约2000毫克/ 毫升。一种药物制剂，其包含吡格列酮的药学上可接受的酸性盐，选自马来酸或酒石酸的固体药学上可接受的有机酸和促进歧化的赋形剂，其中所述固体药学上可接受的有机酸的重量比赋形剂为约1:6至约1:1。

4. 发明申请

WO2015119919A1 PHARMACEUTICAL COMPOSITION OF SELECTIVE HCV NS3/4A INHIBITORS 审中-公开
标题翻译：选择性HCV NS3 / 4A抑制剂的药物组合物
公开(公告)号：WO2015119919A1
公开(公告)日：2015-08-13
申请号：PCT/US2015/014195
申请日：2015-02-03
申请人： MERCK SHARP & DOHME CORP. , MAROTA, Melanie, J. , MCKELVEY, Craig , BIRRINGER, Nicholas , KUIPER, Jesse , HARMON, Paul, A. , SOCIA, Adam, J. , MARSAC, Patrick Jules , CONWAY, Stephen, L.
发明人： MAROTA, Melanie, J. , MCKELVEY, Craig , BIRRINGER, Nicholas , KUIPER, Jesse , HARMON, Paul, A. , SOCIA, Adam, J. , MARSAC, Patrick Jules , CONWAY, Stephen, L.
IPC分类号： A61K31/498 , A61P31/12
CPC分类号： A61K38/06 , A61K9/146 , A61K9/1611 , A61K9/1617 , A61K9/1635 , A61K9/1641 , A61K9/1652 , A61K9/2009 , A61K31/5365
摘要： The present invention is directed to compositions comprising the HCV NS3/4A inhibitor, (1aR,5S,8S,10R,22aR)-5-tert-butyl-N-{(1R,2S)-1-[(cyclopropylsulfonyl)carbamoyl]-2-ethenylcyclopropyl}-14-methoxy-3,6-dioxo-1,1a,3,4,5,6,9,10,18,19,20,21,22,22a-tetradecahydro-8H-7,10-methanocyclopropa[18,19][1,10,3,6]dioxadiazacyclononadecino[11,12-b]quinoxaline-8-carboxamide, or a pharmaceutically acceptable salt thererof, an oral absorption enhancing polymer, and, optionally, a surfactant. The present invention is also directed to solid dispersions and pharmaceutical compositions containing or made from these compositions, and the methods for making these solid dispersions and pharmaceutical compositions.
摘要翻译：本发明涉及包含HCV NS3 / 4A抑制剂（1aR，5S，8S，10R，22aR）-5-叔丁基-N - {（1R，2S）-1 - [（环丙基磺酰基）氨基甲酰基] -2- ethenylcyclopropyl} -14-甲氧基-3,6-二氧代1,1A，3,4,5,6,9,10,18,19,20,21,22,22a十四氢8H-7， 10-甲基环丙烷[18,19] [1,10,3,6]二氧杂二氮杂环十二炔[11,12-b]喹喔啉-8-甲酰胺或其药学上可接受的盐，口服吸收增强聚合物和任选的表面活性剂。本发明还涉及含有或由这些组合物制成的固体分散体和药物组合物，以及制备这些固体分散体和药物组合物的方法。

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