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1. 发明申请

WO2008060934A2 FORMULATIONS OF TETRAHYDROPYRIDINE ANTIPLATELET AGENTS FOR PARENTERAL OR ORAL ADMINISTRATION 审中-公开
标题翻译：用于肠胃外或口服给药的四氢吡啶抗血小板药物的制剂
公开(公告)号：WO2008060934A2
公开(公告)日：2008-05-22
申请号：PCT/US2007/084040
申请日：2007-11-08
申请人： ACUSPHERE, INC. , BERNSTEIN, Howard , CARNEIRO, Olinda , JAIN, Rajeev A. , PANDIT, Namrata , RANE, Shveta , STRAUB, Julie Ann
发明人： BERNSTEIN, Howard , CARNEIRO, Olinda , JAIN, Rajeev A. , PANDIT, Namrata , RANE, Shveta , STRAUB, Julie Ann
IPC分类号： A61K9/00 , A61K9/107 , A61K9/16 , A61K31/4365
CPC分类号： A61K31/4365 , A61K9/0019 , A61K9/1075 , A61K9/1617 , A61K9/19
摘要： A pharmaceutical composition for the oral or parenteral administration of a compound of Formula (I) comprising an oil in water emulsion, wherein the oil phase comprises the free base of or a pharmaceutically acceptable salt thereof of a compound of Formula (I), and one or more surfactants which are soluble in the oil phase and/or the aqueous phase. The emulsion optionally contains one or more excipients that are soluble in the oil phase and/or the aqueous phase, such as pH modifying agents such as buffers, osmolality/tonicity modifying agents, emulsifying agents, water-soluble polymers, and preservatives. The compound of Formula (I) can be formulated as a solid material and stored until needed. Kits for forming the emulsion are provided. Prior to administration, the solid material can be reconstituted in an aqueous medium to form the emulsion.
摘要翻译：一种用于口服或肠胃外给药式（I）化合物的药物组合物，其包含水包油乳剂，其中所述油相包含化合物的游离碱或其药学上可接受的盐（I）的化合物和一种或多种可溶于油相和/或水相的表面活性剂。乳剂任选含有一种或多种可溶于油相和/或水相的赋形剂，例如pH调节剂如缓冲剂，渗透压/张力调节剂，乳化剂，水溶性聚合物和防腐剂。式（I）化合物可以配制成固体材料并储存直至需要。提供用于形成乳液的试剂盒。在给药之前，固体材料可以在水性介质中重构以形成乳液。

2. 发明申请

WO2008060934A8 FORMULATIONS OF TETRAHYDROPYRIDINE ANTIPLATELET AGENTS FOR PARENTERAL OR ORAL ADMINISTRATION 审中-公开
标题翻译：用于肠胃外或口服给药的四氢吡啶抗血小板药物的制剂
公开(公告)号：WO2008060934A8
公开(公告)日：2008-07-24
申请号：PCT/US2007084040
申请日：2007-11-08
申请人： ACUSPHERE INC , BERNSTEIN HOWARD , CARNEIRO OLINDA , JAIN RAJEEV A , PANDIT NAMRATA , RANE SHVETA , STRAUB JULIE ANN
发明人： BERNSTEIN HOWARD , CARNEIRO OLINDA , JAIN RAJEEV A , PANDIT NAMRATA , RANE SHVETA , STRAUB JULIE ANN
IPC分类号： A61K9/00 , A61K9/107 , A61K9/16 , A61K31/4365
CPC分类号： A61K31/4365 , A61K9/0019 , A61K9/1075 , A61K9/1617 , A61K9/19
摘要： A pharmaceutical composition for the oral or parenteral administration of a compound of Formula (I) comprising an oil in water emulsion, wherein the oil phase comprises the free base of or a pharmaceutically acceptable salt thereof of a compound of Formula (I), and one or more surfactants which are soluble in the oil phase and/or the aqueous phase. The emulsion optionally contains one or more excipients that are soluble in the oil phase and/or the aqueous phase, such as pH modifying agents such as buffers, osmolality/tonicity modifying agents, emulsifying agents, water-soluble polymers, and preservatives. The compound of Formula (I) can be formulated as a solid material and stored until needed. Kits for forming the emulsion are provided. Prior to administration, the solid material can be reconstituted in an aqueous medium to form the emulsion.
摘要翻译：一种用于口服或肠胃外给药式（I）化合物的药物组合物，其包含水包油乳剂，其中该油相包含式（I）化合物的游离碱或其药学上可接受的盐和一种式或更多可溶于油相和/或水相的表面活性剂。乳剂任选含有一种或多种可溶于油相和/或水相的赋形剂，例如pH调节剂如缓冲剂，渗透压/张力调节剂，乳化剂，水溶性聚合物和防腐剂。式（I）化合物可以配制成固体材料并储存直至需要。提供用于形成乳液的试剂盒。在施用之前，固体材料可以在含水介质中重构以形成乳液。

3. 发明申请

WO2008060934A3 FORMULATIONS OF TETRAHYDROPYRIDINE ANTIPLATELET AGENTS FOR PARENTERAL OR ORAL ADMINISTRATION 审中-公开
标题翻译：四氢吡啶类抗坏血酸药物用于住院或口服给药的制剂
公开(公告)号：WO2008060934A3
公开(公告)日：2008-09-12
申请号：PCT/US2007084040
申请日：2007-11-08
申请人： ACUSPHERE INC , BERNSTEIN HOWARD , CARNEIRO OLINDA , JAIN RAJEEV A , PANDIT NAMRATA , RANE SHVETA , STRAUB JULIE ANN
发明人： BERNSTEIN HOWARD , CARNEIRO OLINDA , JAIN RAJEEV A , PANDIT NAMRATA , RANE SHVETA , STRAUB JULIE ANN
IPC分类号： A61K9/00 , A61K9/107 , A61K9/16 , A61K31/4365
CPC分类号： A61K31/4365 , A61K9/0019 , A61K9/1075 , A61K9/1617 , A61K9/19
摘要： A pharmaceutical composition for the oral or parenteral administration of a compound of Formula (I) comprising an oil in water emulsion, wherein the oil phase comprises the free base of or a pharmaceutically acceptable salt thereof of a compound of Formula (I), and one or more surfactants which are soluble in the oil phase and/or the aqueous phase. The emulsion optionally contains one or more excipients that are soluble in the oil phase and/or the aqueous phase, such as pH modifying agents such as buffers, osmolality/tonicity modifying agents, emulsifying agents, water-soluble polymers, and preservatives. The compound of Formula (I) can be formulated as a solid material and stored until needed. Kits for forming the emulsion are provided. Prior to administration, the solid material can be reconstituted in an aqueous medium to form the emulsion.
摘要翻译：一种用于口服或肠胃外给药包含水包油乳液的式（I）化合物的药物组合物，其中所述油相包含式（I）化合物的游离碱或其药学上可接受的盐，和一种或更多的可溶于油相和/或水相的表面活性剂。乳液任选地含有一种或多种可溶于油相和/或水相的赋形剂，如pH调节剂如缓冲液，重量摩尔渗透压浓度/张力调节剂，乳化剂，水溶性聚合物和防腐剂。式（I）的化合物可以配制成固体物质并储存直至需要。提供了用于形成乳液的试剂盒。在施用前，固体材料可以在水性介质中重构以形成乳液。

4. 发明申请

WO1995000535A1 OPTICALLY PURE CALPAIN INHIBITOR COMPOUNDS 审中-公开
标题翻译：光学纯化学抑制剂化合物
公开(公告)号：WO1995000535A1
公开(公告)日：1995-01-05
申请号：PCT/US1994006497
申请日：1994-06-09
申请人： ALKERMES, INCORPORATED , HARBESON, Scott, L. , STRAUB, Julie, Ann
发明人： ALKERMES, INCORPORATED
IPC分类号： C07K05/02
CPC分类号： C07D295/215 , A61K38/00 , C07C271/22 , C07C275/16 , C07C317/40 , C07K5/0202
摘要： Optically pure alpha -ketoamide compounds, and use therefor in treating neurodegenerative pathologies having enhanced Calpain activity, are disclosed. These compounds comprise optically pure alpha -ketoamides, and physiologically acceptable salts thereof, wherein the alpha -ketoamide contains an amino acid isomer which has an L-configuration about the chiral center which is structurally located in the alpha position to the ketone of the alpha -ketoamide, and wherein the amide functionality of the alpha -ketoamide portion of the compound's molecule is derived from an amine of an amino acid or an amine substituted with a sulfone functionality. The method of treating a human neurodegenerative pathology, having enhanced Calpain activity, with a Calpain inhibitor composition while reducing undesirable inhibition of other cysteine proteases andother side effects associated with the racemic Calpain inhibitor composition includes administering an optically pure L-isomer of an alpha -ketoamide compound, wherein the L-isomer is substantially free of its D-isomer. The method of forming an optically pure L- alpha -ketoamide includes mixing an L- beta -amino- alpha -hydroxyamide in a solution containing a free radical catalyst and then mixing an oxydizing agent into said solution under conditions sufficient to form said optically pure L- alpha -ketoamide.
摘要翻译：公开了光学纯的α-酮酰胺化合物，并用于治疗具有增强的钙蛋白酶活性的神经退行性病变。这些化合物包括光学纯的α-酮酰胺及其生理上可接受的盐，其中α-酮酰胺含有氨基酸异构体，该氨基酸异构体在手性中心具有L-构型，其结构上位于α位酮的α位置，酮酰胺，并且其中化合物分子的α-酮酰胺部分的酰胺官能度衍生自氨基酸的胺或被砜官能团取代的胺。使用钙蛋白酶抑制剂组合物治疗具有增强的钙蛋白酶活性的人类神经变性病理学方法同时减少其他半胱氨酸蛋白酶的不期望的抑制和与外消旋钙蛋白酶抑制剂组合物相关的其它副作用的方法包括给予α-酮酰胺的光学纯的L-异构体化合物，其中L-异构体基本上不含其D-异构体。形成光学纯的L-α-酮酰胺的方法包括在含有自由基催化剂的溶液中混合L-β-氨基-α-羟基酰胺，然后在足以形成所述光学纯L的条件下将氧化剂混合到所述溶液中 α-酮酰胺。

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