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212 条记录 (耗时 0.025 秒)

    PROCESS FOR DIMETHYLATION OF ACTIVE METHYLENE GROUPS
    102.
    发明申请
    PROCESS FOR DIMETHYLATION OF ACTIVE METHYLENE GROUPS 审中-公开
    活性甲基团二甲基化方法

    公开(公告)号：US20120149895A1

    公开(公告)日：2012-06-14

    申请号：US13262587

    申请日：2010-03-30

    申请人： Branko Jenko ,  Anton Copar

    发明人： Branko Jenko ,  Anton Copar

    IPC分类号： C07C231/14 ,  C07D273/00 ,  C07C253/30

    CPC分类号： C07C253/30 ,  C07C231/12 ,  C07C237/06 ,  C07C255/19

    摘要： The present invention discloses a process for dimethylation of active methylene groups. Specifically, the invention discloses a process for preparing 3-amino-2,2-dimethylpropanamide. Compounds produced by the present dimethylation process such as 3-amino-2,2-dimethylpropanamide can be used as intermediates in the route of synthesis of therapeutic, prophylactic or diagnostic agent, for example aliskiren or cryptophycin. Particularly, the invention relates to embodiments further extending to processes for preparing pharmaceutical dosage form comprising said therapeutic, prophylactic or diagnostic agents. More specifically, the invention relates to the use of compounds produced by the present dimethylation process for the manufacture of therapeutic, prophylactic or diagnostic agents or for the manufacture of pharmaceutical dosage forms comprising said therapeutic, prophylactic or diagnostic agents. The processes according to the present invention can be beneficially applied for the synthesis of various active pharmaceutical ingredients, such as aliskiren or crypthophycin.

    摘要翻译： 本发明公开了一种活性亚甲基二甲基化方法。 具体地说，本发明公开了一种制备3-氨基-2,2-二甲基丙酰胺的方法。 通过本发明的二甲基化方法制备的化合物如3-氨基-2,2-二甲基丙酰胺可用作合成治疗，预防或诊断剂例如阿利吉仑或隐霉素的途径中的中间体。 特别地，本发明涉及进一步扩展到制备包含所述治疗剂，预防剂或诊断剂的药物剂型的方法的实施方案。 更具体地，本发明涉及通过本发明的二甲基化方法制备的化合物在制备治疗，预防或诊断剂中的用途，或用于制备包含所述治疗，预防或诊断剂的药物剂型。 根据本发明的方法可有利地用于合成各种活性药物成分，例如阿利吉仑或crypthophycin。

    PROCESS FOR THE PREPARATION OF A PHARMACEUTICAL COMPOSITION COMPRISING EZETIMIBE
    103.
    发明申请
    PROCESS FOR THE PREPARATION OF A PHARMACEUTICAL COMPOSITION COMPRISING EZETIMIBE 有权
    制备包含EZETIMIBE的药物组合物的方法

    公开(公告)号：US20120135976A1

    公开(公告)日：2012-05-31

    申请号：US13147956

    申请日：2010-02-05

    申请人： Janez Kerc ,  Miha Homar ,  Polona Jurkovic

    发明人： Janez Kerc ,  Miha Homar ,  Polona Jurkovic

    IPC分类号： A61K31/397 ,  A61P7/00

    CPC分类号： A61K9/145 ,  A61K9/2018 ,  A61K9/2095

    摘要： The present invention belongs to the field of pharmaceutical industry and relates to a process for preparing dosage forms containing ezetimibe, comprising the steps of: a) providing a composition comprising ezetimibe, b) sieving a composition comprising a composition of step (a), c) shear mixing of the composition after step (b), preferably the mixing of the composition is carried out by high shear mixing, d) formulation into a dosage form. The present invention also relates to dosage forms containing ezetimibe and ezetimibe and simvastatin, which have been prepared according to the process according to the invention.

    摘要翻译： 本发明属于制药工业领域，涉及制备含有依泽替米贝的剂型的方法，该方法包括以下步骤：a）提供包含依泽麦布的组合物，b）筛分包含步骤（a），c ）组合物在步骤（b）之后的剪切混合，优选组合物的混合通过高剪切混合进行，d）配制成剂型。 本发明还涉及根据本发明的方法制备的依泽替米贝，依泽替米贝和辛伐他汀的剂型。

    PROCESS FOR THE PREPARATION OR PURIFICATION OF OLMESARTAN MEDOXOMIL
    104.
    发明申请
    PROCESS FOR THE PREPARATION OR PURIFICATION OF OLMESARTAN MEDOXOMIL 有权
    奥美沙芬制剂的制备或纯化方法

    公开(公告)号：US20110263666A1

    公开(公告)日：2011-10-27

    申请号：US12672267

    申请日：2008-08-07

    申请人： Samo Pirc ,  Lovro Selic

    发明人： Samo Pirc ,  Lovro Selic

    IPC分类号： A61K31/4178 ,  A61P9/12 ,  C07D405/14

    CPC分类号： C07D405/14

    摘要： The present invention relates to a process for the preparation and purification of olmesartan medoxomil hydrohalide salts and optionally converting them to olmesartan medoxomil. The invention also relates to products obtainable by the process of the invention, to pharmaceutical compositions comprising the products and to their use in medicine, particularly to treat hypertension.

    摘要翻译： 本发明涉及一种用于制备和纯化奥美沙坦酯的氢卤酸盐的方法，并且任选将其转化为奥美沙坦酯。 本发明还涉及通过本发明的方法获得的产品，包括产品的药物组合物及其在医药中的用途，特别是治疗高血压。

    GRANULATION OF ACTIVE PHARMACEUTICAL INGREDIENTS
    105.
    发明申请
    GRANULATION OF ACTIVE PHARMACEUTICAL INGREDIENTS 审中-公开
    活性药物成分的制备

    公开(公告)号：US20110136883A1

    公开(公告)日：2011-06-09

    申请号：US12937081

    申请日：2009-04-08

    申请人： Rade Injac ,  Sara Cesar

    发明人： Rade Injac ,  Sara Cesar

    IPC分类号： A61K31/4178 ,  A61P9/12

    CPC分类号： A61K9/2013 ,  A61K9/1617 ,  A61K9/1623 ,  A61K9/1641 ,  A61K9/1694 ,  A61K9/2018 ,  A61K9/2031 ,  A61K31/4178 ,  A61K31/54

    摘要： The present invention discloses a dry formulation or granulation comprising, in admixture, more than 50 wt. % of active pharmaceutical ingredient and from 1 to 10 wt. % of each of any nonaqueous excipient selected from liquid substances. In a preferred embodiment no water or lower alcohol has been added in any step of the preparation of the dry formulation or granulation, and the nonaqueous excipient selected from liquid substances is adsorbed to dryness by the active pharmaceutical ingredient and/or by a further solid excipient. Pharmaceutical formulations based on such dry formulation or granulation, and processes for the preparation thereof, are described as well. The dry formulations or granulations reliably and effectively further processed under dry conditions without requiring active drying, including e.g. briquetting, slugging, sieving, milling, tabletting, further fine granulating, direct compression, and the like.

    摘要翻译： 本发明公开了一种干燥制剂或造粒剂，其中混合物含有大于50wt。 ％的活性药物成分和1至10wt。 各种非水性赋形剂中的每一种选自液体物质的％。 在优选的实施方案中，在制备干燥制剂或造粒的任何步骤中不加入水或低级醇，并且通过活性药物成分和/或其它固体赋形剂将选自液体物质的非水性赋形剂吸附至干燥 。 还描述了基于这种干制剂或造粒的药物制剂及其制备方法。 干制剂或颗粒在干燥条件下可靠且有效地进一步处理，而不需要主动干燥，包括例如 压块，压块，筛分，研磨，压片，进一步精细制粒，直接压缩等。

    Method of preparing stabilized pharmaceutical compositions comprising active ingredients susceptible to conversion to alternate polymorph forms
    107.
    发明申请
    Method of preparing stabilized pharmaceutical compositions comprising active ingredients susceptible to conversion to alternate polymorph forms 审中-公开
    制备稳定的药物组合物的方法，其包含易于转化为交替多晶型形式的活性成分

    公开(公告)号：US20110021631A1

    公开(公告)日：2011-01-27

    申请号：US12878562

    申请日：2010-09-09

    申请人： Peter SVETE

    发明人： Peter SVETE

    IPC分类号： A61K31/225 ,  A61P9/10

    CPC分类号： A61K9/1652 ,  A61K31/4184 ,  A61K31/695 ,  C07C67/62 ,  C07C2602/28 ,  C07C69/33

    摘要： A process is described for the preparation of a pharmaceutical comprising an active pharmaceutical ingredient capable of existing in multiple polymorphic forms, wherein the process comprises a step of preparation of a wet phase comprising the active pharmaceutical ingredient and microcrystalline cellulose and a liquid, wherein in the wet phase has a weight ratio of active pharmaceutical ingredient to microcrystalline cellulose above 1.0 or a weight ratio of active pharmaceutical ingredient to liquid above 1.0.

    摘要翻译： 描述了一种用于制备包含能够以多种多形态存在的活性药物成分的药物的方法，其中该方法包括制备包含活性药物成分和微晶纤维素和液体的湿相的步骤，其中在 湿相具有大于1.0的活性药物成分与微晶纤维素的重量比或活性药物成分与高于1.0的液体的重量比。

    DULOXETIN COMPOSITION
    108.
    发明申请
    DULOXETIN COMPOSITION 审中-公开
    DULOXETIN组合物

    公开(公告)号：US20110008439A1

    公开(公告)日：2011-01-13

    申请号：US12521410

    申请日：2007-12-21

    申请人： Miha Tomaz Jaklic ,  Rok Jurecic

    发明人： Miha Tomaz Jaklic ,  Rok Jurecic

    IPC分类号： A61K9/14 ,  A61K31/381

    CPC分类号： A61K31/381 ,  A61K9/5078 ,  A61K9/5089 ,  A61K2300/00

    摘要： The present invention relates to a stable pharmaceutical pellet composition comprising duloxetine or a pharmaceutically acceptable salt thereof and a method for making such composition. In particular, the composition comprises duloxetine hydrochloride and a separating layer comprising a water soluble inorganic salt.

    摘要翻译： 本发明涉及包含度洛西汀或其药学上可接受的盐的稳定药物颗粒组合物和制备该组合物的方法。 特别地，组合物包含度洛西汀盐酸盐和包含水溶性无机盐的分离层。

    ACTIVE PHARMACEUTICAL INGREDIENT ON A SOLID SUPPORT, AMORPHOUS AND WITH AN IMPROVED SOLUBILITY
    109.
    发明申请
    ACTIVE PHARMACEUTICAL INGREDIENT ON A SOLID SUPPORT, AMORPHOUS AND WITH AN IMPROVED SOLUBILITY 审中-公开
    活性药物成分在固体支持，无定形和改善溶解度

    公开(公告)号：US20100305087A1

    公开(公告)日：2010-12-02

    申请号：US12809576

    申请日：2008-12-18

    申请人： Rok Grahek ,  Aleksander Resman ,  Andrej Bastarda ,  Martin Crnugelj

    发明人： Rok Grahek ,  Aleksander Resman ,  Andrej Bastarda ,  Martin Crnugelj

    IPC分类号： A61K31/397 ,  A61K31/122

    CPC分类号： A61K31/122 ,  A61K9/143 ,  A61K31/397

    摘要： A combination preparation comprising an active pharmaceutical ingredient (API) and a pharmaceutically acceptable solid support, wherein said solid support is in a water-insoluble particulate form and comprises a material selected from silicic acid, aluminum hydroxide and titanium hydroxide is disclosed. The API is a compound having both, at least one hydrophobic structural moiety causing the API to have a low solubility in water or in an aqueous solution, and multiple hydrophilic groups arranged to form multiple intermolecular interactions to the solid support involving polar or ionic or hydrogen bonding. The hydrophilic groups of the API are independently equal or different and comprise at least one of the groups consisting of OH- and halogen-groups. The API is bound to the solid support by adsorption, and a major proportion of said API is in an amorphous state. Related pharmaceuticals and methods of preparation also are disclosed.

    摘要翻译： 包含活性药物成分（API）和药学上可接受的固体支持物的组合制剂，其中所述固体支持物为水不溶性颗粒形式，并且包含选自硅酸，氢氧化铝和氢氧化钛的材料。 API是具有至少一个引起API在水中或在水溶液中具有低溶解度的至少一个疏水性结构部分的化合物，以及与包含极性或离子或氢的固体支持物形成多个分子间相互作用的多个亲水基团 粘接。 API的亲水基团独立地相同或不同，并且包含由OH-和卤素基团组成的组中的至少一个。 API通过吸附与固体支持物结合，并且所述API的主要比例处于非晶状态。 还公开了相关药物和制备方法。