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37 条记录 (耗时 0.024 秒)

    Substantially Pure and a Stable Crystalline Form of Bosentan
    1.
    发明申请
    Substantially Pure and a Stable Crystalline Form of Bosentan 审中-公开
    波斯坦的基本纯度和稳定的结晶形式

    公开(公告)号：US20110021547A1

    公开(公告)日：2011-01-27

    申请号：US12864571

    申请日：2009-01-22

    申请人： Girish Dixit ,  Nandkumar Gaikwad ,  Hima Prasad Naidu ,  Nitin Sharadchandra Pradhan ,  Jon Valgeirsson

    发明人： Girish Dixit ,  Nandkumar Gaikwad ,  Hima Prasad Naidu ,  Nitin Sharadchandra Pradhan ,  Jon Valgeirsson

    IPC分类号： A61K31/513 ,  C07D403/04

    CPC分类号： C07D403/04

    摘要： Described is a highly stable crystalline form of bosentan having a water content in the range of about 3-4% by weight, based on the total weight of the bosentan, (bosentan crystalline form A5), a process for preparation thereof, and pharmaceutical compositions comprising the bosentan crystalline form A5. Provided also herein is a bosentan impurity, p-tert-butyl-N[6-hydroxy-5-(2-methoxyphenoxy)-2-(2-pyrimidinyl)-4-pyrimidinyl]benzenesulfonamide (deshydroxyethyl bosentan impurity), and process for preparing and isolating thereof. Further provided are highly pure bosentan or a pharmaceutically acceptable salt thereof substantially free of deshydroxyethyl bosentan and bosentan dimer impurities, process for the preparation thereof, and pharmaceutical compositions comprising solid particles of highly pure bosentan or a pharmaceutically acceptable salt thereof, wherein 90 volume-percent of the particles (D90) have a size of less than about 300 microns.

    摘要翻译： 描述了基于波生坦总重量（波生坦结晶形式A5），其制备方法和药物组合物的水含量在约3-4重量％范围内的波生坦的高度稳定的结晶形式 包括波生坦晶体A5。 本文还提供了一种波生坦杂质，对叔丁基-N [6-羟基-5-（2-甲氧基苯氧基）-2-（2-嘧啶基）-4-嘧啶基]苯磺酰胺（脱羟乙基波生坦杂质），和 制备和分离。 还提供了高纯度的波生坦或其药学上可接受的盐，其基本上不含脱羟基乙基波生坦和波生坦二聚体杂质，其制备方法以及包含高纯度波生坦固体颗粒或其药学上可接受的盐的药物组合物，其中90体积％ 的颗粒（D90）具有小于约300微米的尺寸。

    Novel aryl ureido benzoic acid derivatives and their use
    3.
    发明申请
    Novel aryl ureido benzoic acid derivatives and their use 失效
    新型芳基脲基苯甲酸衍生物及其用途

    公开(公告)号：US20060069255A1

    公开(公告)日：2006-03-30

    申请号：US10535683

    申请日：2003-11-10

    申请人： Jon Valgeirsson ,  Elsebet Nielsen ,  Dan Peters

    发明人： Jon Valgeirsson ,  Elsebet Nielsen ,  Dan Peters

    IPC分类号： C07D271/06 ,  C07D211/82

    CPC分类号： C07D213/75 ,  C07C275/42 ,  C07C309/51 ,  C07C2603/18 ,  C07D209/40 ,  C07D231/56 ,  C07D257/04 ,  C07D271/07 ,  C07D317/66 ,  C07D333/36

    摘要： This invention relates to novel aryl ureido benzoic acid derivatives useful as selective and non-competitive antagonists of the ionotropic GluR5 receptor. Due to their biological activity, the aryl ureido derivatives of the invention are considered useful for treating diseases that are responsive to modulation of an aspartate or a glutamate receptor. Moreover the invention provides chemical compounds for use according to the invention, as well as pharmaceutical compositions comprising the chemical compounds, and methods of treating diseases or disorders or conditions responsive to modulation of an aspartate or a glutamate receptor.

    摘要翻译： 本发明涉及可用作离子型GluR5受体的选择性和非竞争性拮抗剂的新型芳基脲基苯甲酸衍生物。 由于其生物学活性，本发明的芳基脲基衍生物被认为可用于治疗对天冬氨酸或谷氨酸受体的调节有反应的疾病。 此外，本发明提供了根据本发明使用的化合物，以及包含化合物的药物组合物，以及治疗对天冬氨酸或谷氨酸受体的调节作用的疾病或病症或病症的方法。

    Novel Polymorph of Atorvastatin Calcium and Use Thereof for the Preparation of Amorphous Atorvastatin Calcium
    6.
    发明申请
    Novel Polymorph of Atorvastatin Calcium and Use Thereof for the Preparation of Amorphous Atorvastatin Calcium 审中-公开
    阿托伐他汀钙的新型多态性及其用于制备无定形阿托伐他汀钙的方法

    公开(公告)号：US20100260851A1

    公开(公告)日：2010-10-14

    申请号：US12668433

    申请日：2008-07-11

    申请人： Girish Dixit ,  Anil Shahaji Khile ,  Nitin Sharadchandra Pradhan ,  Jon Valgeirsson

    发明人： Girish Dixit ,  Anil Shahaji Khile ,  Nitin Sharadchandra Pradhan ,  Jon Valgeirsson

    IPC分类号： A61K9/14 ,  A61K31/40 ,  C07D207/34 ,  A61P3/06 ,  A61P9/10

    CPC分类号： C07D207/34

    摘要： The present invention provides a novel polymorphic form of atorvastatin calcium, designated as form Al, process for preparation, pharmaceutical compositions, and method of treating thereof. The present invention further provides a process for the preparation of highly pure amorphous atorvastatin calcium using the novel atorvastatin calcium form Al. The present invention also relates to novel amorphous form of atorvastatin tert-butyl ester, chemically known as [R-(R*,R*)]-2-(4-fluorophenyl)-[β],[δ]-dihydroxy -5-(1-methylethyl)-3-phenyl-4-(phenylcarbamoyl-1H-pyrrole-1-heptanoicacid tert-butyl ester, process for the preparation, and its application for preparing highly pure atorvastatin and its pharmaceutically acceptable salts thereof. The present invention also relates to use of the novel amorphous atorvastatin tert-butyl ester and novel atorvastatin calcium form al for preparing amorphous atorvastatin calcium.

    摘要翻译： 本发明提供了一种新型的阿托伐他汀钙多形态，称为形式A1，制备方法，药物组合物及其处理方法。 本发明还提供使用新型阿托伐他汀钙形式Al制备高纯度无定形阿托伐他汀钙的方法。 本发明还涉及化学上称为[R-（R *，R *）] - 2-（4-氟苯基） - [[b]]，[δ] - 二羟基 - 5-（1-甲基乙基）-3-苯基-4-（苯基氨基甲酰基-1H-吡咯-1-庚酸叔丁酯，其制备方法及其制备高纯度阿托伐他汀及其药学上可接受的盐的应用） 本发明还涉及新型无定形阿托伐他汀叔丁酯和新型阿托伐他汀钙形式用于制备无定形阿托伐他汀钙的用途。

    Repaglinide Substantially Free of Dimer Impurity
    8.
    发明申请
    Repaglinide Substantially Free of Dimer Impurity 审中-公开
    瑞格列奈基本上不含二聚体杂质

    公开(公告)号：US20100197732A1

    公开(公告)日：2010-08-05

    申请号：US12663106

    申请日：2008-06-05

    申请人： Sonny Sebastian ,  Sasidhar Venkata Balla ,  Ramamurthy Katikareddy ,  Nitin Sharadchandra Pradhan ,  Jon Valgeirsson

    发明人： Sonny Sebastian ,  Sasidhar Venkata Balla ,  Ramamurthy Katikareddy ,  Nitin Sharadchandra Pradhan ,  Jon Valgeirsson

    IPC分类号： A61K31/4545 ,  C07D211/26 ,  C07D211/32 ,  A61K31/4453 ,  A61P3/10

    CPC分类号： C07D295/135

    摘要： The present invention provides highly pure repaglinide substantially free of dimer impurity, and process for the preparation thereof. The present invention also relates to 2-ethoxy-N-[(1S)-3-methyl-1-[2-(1-piperidinyl)phenyl]butyl]-4-[2-[[(1S)-3-methyl-1-[2-(1-piperidinyl)phenyl]butyl]amino]-2-oxoethyl]benzamide, an impurity of repaglinide, and a process for preparing and isolating thereof. The present invention further relates to pharmaceutical compositions comprising solid particles of pure repaglinide substantially free of dimer impurity or pharmaceutically acceptable salts thereof, wherein 90 volume-percent of the particles (D90) have a size of less than about 400 microns. The present invention also provides an optical resolution method of racemic 3-methyl-1-(2-piperidino-phenyl)-1-butylamine and use thereof for the preparation of repaglinide.

    摘要翻译： 本发明提供了基本上不含二聚体杂质的高纯度瑞格列奈及其制备方法。 本发明还涉及2-乙氧基-N - [（1S）-3-甲基-1- [2-（1-哌啶基）苯基]丁基] -4- [2 - [[（1S）-3-甲基 -1- [2-（1-哌啶基）苯基]丁基]氨基] -2-氧代乙基]苯甲酰胺，瑞格列奈的杂质及其制备和分离方法。 本发明还涉及包含基本上不含二聚体杂质的纯瑞格列奈的固体颗粒或其药学上可接受的盐的药物组合物，其中90体积％的颗粒（D90）具有小于约400微米的尺寸。 本发明还提供外消旋3-甲基-1-（2-哌啶子基 - 苯基）-1-丁胺的光学拆分方法及其在制备瑞格列奈中的应用。