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    PROCESS FOR PREPARATION OF ENANTIOMERICALLY PURE ESOMEPRAZOLE
    31.
    发明申请
    PROCESS FOR PREPARATION OF ENANTIOMERICALLY PURE ESOMEPRAZOLE 失效
    制备完全纯化的异喹诺酮的方法

    公开(公告)号：US20100174087A1

    公开(公告)日：2010-07-08

    申请号：US12279354

    申请日：2007-09-25

    申请人： Bandi Parthasaradhi Reddy ,  Kura Rathnakar Reddy ,  Rapolu Raji Reddy ,  Dasari Muralidhara Reddy

    发明人： Bandi Parthasaradhi Reddy ,  Kura Rathnakar Reddy ,  Rapolu Raji Reddy ,  Dasari Muralidhara Reddy

    IPC分类号： C07D401/12

    CPC分类号： C07D401/12

    摘要： The present invention provides an improved and commercially viable process for preparation of substantially enantiomerically pure esomeprazole in neutral form or as a pharmaceutically acceptable salt or as its solvates including hydrates. Thus, for example, a compound containing a mixture of 1-(S)-camphorsulfonyl-5-methoxy-2-[(3,5-dimethyl-4-methoxy-2-pyridyl)methyl-(S)-sulfinyl]-1H-benzimidazole and 1-(S)-camphorsulfonyl-6-methoxy-2-[(3,5-dimethyl-4-methoxy-2-pyridyl)methyl-(S)-sulfinyl]-1H-benzimidazole is hydrolyzed with barium hydroxide, isolated the resulting esomeprazole barium salt followed by neutralization with an acid to yield substantially enantiomerically pure esomeprazole in neutral form and then converted into its pharmaceutically acceptable salts.

    摘要翻译： 本发明提供了一种改进的和商业可行的制备基本上为中性形式的对映体纯的埃索美拉唑或作为其药学上可接受的盐或其溶剂合物包括水合物的方法。 因此，例如，含有1-（S） - 樟脑磺酰基-5-甲氧基-2 - [（3,5-二甲基-4-甲氧基-2-吡啶基）甲基 - （S） - 亚磺酰基] - 1H-苯并咪唑和1-（S） - 樟脑磺酰基-6-甲氧基-2 - [（3,5-二甲基-4-甲氧基-2-吡啶基）甲基 - （（S） - 亚磺酰基] -1H-苯并咪唑用钡水解 分离得到的艾美拉唑钡盐，然后用酸中和，得到基本上为中性形式的对映体纯的埃索美拉唑，然后转化为其药学上可接受的盐。

    Process for the preparation of didanosine using novel intermediates
    32.
    发明授权
    Process for the preparation of didanosine using novel intermediates 失效
    使用新型中间体制备去羟肌苷的方法

    公开(公告)号：US07750153B2

    公开(公告)日：2010-07-06

    申请号：US11570358

    申请日：2005-07-05

    申请人： Bandi Parthasaradhi Reddy ,  Kura Rathnakar Reddy ,  Rapolu Raji Reddy ,  Dasari Muralidhara Reddy ,  Kesireddy Subash Chander Reddy

    发明人： Bandi Parthasaradhi Reddy ,  Kura Rathnakar Reddy ,  Rapolu Raji Reddy ,  Dasari Muralidhara Reddy ,  Kesireddy Subash Chander Reddy

    IPC分类号： C07D473/30 ,  C07H19/073

    CPC分类号： C07H19/173

    摘要： The present invention relates to novel crystalline alkali metal and alkaline earth metal salts of 2′,3′-dideoxy-2′,3′-didehydroinosine. The present invention also provides a novel process for preparation of didanosine in high yield and purity using novel intermediates. Thus, for example, 5′-O-acetyl-2′,3′-dideoxy-2′,3′-didehydroinosine is reacted with monomethyl amine to give 2′,3′-dideoxy-2′,3′-didehydro inosine, which is then reacted with sodium hydroxide and crystallized to give crystalline 2′,3′-dideoxy-2′,3′-didehydroinosine sodium salt. 2′,3′-Dideoxy-2′,3′-didehydroinosine sodium salt is hydrogenated using raney nickel catalyst in aqueous medium and then neutralized with hydrochloric acid to yield didanosine.

    摘要翻译： 本发明涉及2'，3'-二脱氧-2'，3'-二脱水肌苷的新型结晶碱金属和碱土金属盐。 本发明还提供了使用新型中间体以高产率和纯度制备去羟肌苷的新方法。 因此，例如可以将5'-O-乙酰基-2'，3'-二脱氧-2'，3'-二脱水肌苷与单甲基胺反应，得到2'，3'-二脱氧-2'，3'-二脱氢肌苷 ，然后与氢氧化钠反应并结晶，得到结晶的2'，3'-二脱氧-2'，3'-二脱氢吖啶钠盐。 2'，3'-二脱氧-2'，3'-二脱氢睾酮钠盐在水性介质中使用阮内镍催化剂氢化，然后用盐酸中和，得到去羟肌苷。

    NOVEL CRYSTALLINE FORM OF LANSOPRAZOLE
    33.
    发明申请
    NOVEL CRYSTALLINE FORM OF LANSOPRAZOLE 审中-公开
    兰曲唑的新型结晶形式

    公开(公告)号：US20100093804A1

    公开(公告)日：2010-04-15

    申请号：US11993960

    申请日：2006-12-07

    申请人： Bandi Parthasaradhi Reddy ,  Kura Rathnakar Reddy ,  Rapolu Raji Reddy ,  Dasari Muralidhara Reddy

    发明人： Bandi Parthasaradhi Reddy ,  Kura Rathnakar Reddy ,  Rapolu Raji Reddy ,  Dasari Muralidhara Reddy

    IPC分类号： A61K31/435 ,  C07D401/12 ,  A61P1/00

    CPC分类号： C07D401/12

    摘要： The present invention relates to a novel and stable crystalline polymorph of lansoprazole, a process for its preparation and to a pharmaceutical composition comprising it. Thus, for example, lansoprazole crude is dissolved in methanol at 20-30° C. followed by stirring and the solution is cooled to 0-10° C. The resulting solution is stirred for 1 hour to 1 hour 30 minutes at 0-10° C., the solid is filtered and then dried to give lansoprazole crystalline form III.

    摘要翻译： 本发明涉及兰索拉唑的新颖稳定的结晶多晶型物，其制备方法和包含其的药物组合物。 因此，例如，兰索拉唑粗品在20-30℃溶解在甲醇中，然后搅拌，将溶液冷却至0-10℃。将所得溶液在0-10℃下搅拌1小时至1小时30分钟 将固体过滤，然后干燥，得到兰索拉唑结晶形式III。

    PROCESS FOR RIMONABANT
    34.
    发明申请
    PROCESS FOR RIMONABANT 审中-公开
    过程的RIMONABANT

    公开(公告)号：US20100076197A1

    公开(公告)日：2010-03-25

    申请号：US11993544

    申请日：2006-09-11

    申请人： Bandi Parthasaradhi Reddy ,  Kura Rathnakar Reddy ,  Rapolu Raji Reddy ,  Dasari Muralidhara Reddy ,  Kesireddy Subash Chander Reddy

    发明人： Bandi Parthasaradhi Reddy ,  Kura Rathnakar Reddy ,  Rapolu Raji Reddy ,  Dasari Muralidhara Reddy ,  Kesireddy Subash Chander Reddy

    IPC分类号： C07D401/12

    CPC分类号： C07D231/14

    摘要： The present invention provides an improved and commercially viable process for the preparation of rimonabant substantially free of amide impurity, namely 5-(4-chlorophenyl)-1-(2,4-dichlorophenyl-4-methyl-pyrazole-3-carboxamide and its pharmaceutically acceptable acid addition salts thereof. Thus, for example, 5-(4-chlorophenyl)-1-(2,4-dichlorophenyl-4-methyl-pyrazole-3-carboxylic acid chloride is reacted with 1-aminopiperidine in the presence of a base and optionally a phase transfer catalyst is used such as tetra-butylammonium bromide in a biphasic reaction medium containing water and a water-immiscible solvent to obtain pure rimonabant.

    摘要翻译： 本发明提供了一种改进和商业上可行的制备基本上不含酰胺杂质的利莫那班的方法，即5-（4-氯苯基）-1-（2,4-二氯苯基-4-甲基 - 吡唑-3-甲酰胺及其 因此，例如可以使用5-（4-氯苯基）-1-（2,4-二氯苯基-4-甲基 - 吡唑-3-甲酰氯）与1-氨基哌啶在 使用碱和任选的相转移催化剂，例如四丁基溴化铵在含水和水不混溶溶剂的双相反应介质中，以获得纯的利莫那班。

    NOVEL POLYMORPHS OF RIMONABANT
    35.
    发明申请
    NOVEL POLYMORPHS OF RIMONABANT 审中-公开
    新的聚合物

    公开(公告)号：US20100076022A1

    公开(公告)日：2010-03-25

    申请号：US11993566

    申请日：2006-09-01

    申请人： Bandi Parthasaradhi Reddy ,  Kura Rathnakar Reddy ,  Rapolu Raji Reddy ,  Dasari Muralidhara Reddy ,  Kesireddy Subash Chander Reddy

    发明人： Bandi Parthasaradhi Reddy ,  Kura Rathnakar Reddy ,  Rapolu Raji Reddy ,  Dasari Muralidhara Reddy ,  Kesireddy Subash Chander Reddy

    IPC分类号： C07D401/12 ,  A61K31/454

    CPC分类号： C07D231/14

    摘要： The present invention discloses novel and stable polymorphs of rimonabant, its hydrates and solvates, to the processes for their preparation and to pharmaceutical compositions comprising them. The present invention further discloses a novel and stable amorphous form of rimonabant, process for its preparation and a pharmaceutical composition comprising it. The present invention also provides an improved process for the preparation of rimonabant crystalline Form II. Thus, for example, rimonabant is dissolved in methylene dichloride, stirred for 10 minutes at 25-30° C. and then the solvent distilled off under vacuum at 40° C. The resulting residue is stirred with water and the separated solid is collected at 25-30° C. to give a stable crystalline rimonabant hydrate.

    摘要翻译： 本发明公开了利莫那班，其水合物和溶剂合物，其制备方法和包含它们的药物组合物的新颖且稳定的多晶型物。 本发明还公开了一种新型和稳定的无定形形式的利莫那班，其制备方法和包含它的药物组合物。 本发明还提供了制备利莫那班结晶II型的改进方法。 因此，例如，将利莫那班溶解在二氯甲烷中，在25-30℃下搅拌10分钟，然后在40℃下真空蒸馏除去溶剂。将所得残余物与水一起搅拌，将分离的固体收集在 25-30℃，得到稳定的结晶边缘水合物。

    Amorphous esomeprazole hydrate
    36.
    发明授权
    Amorphous esomeprazole hydrate 失效
    无定型埃索美拉唑水合物

    公开(公告)号：US07638634B2

    公开(公告)日：2009-12-29

    申请号：US12399514

    申请日：2009-03-06

    申请人： Bandi Parthasaradhi Reddy ,  Kura Rathnakar Reddy ,  Rapolu Raji Reddy ,  Dasari Muralidhara Reddy

    发明人： Bandi Parthasaradhi Reddy ,  Kura Rathnakar Reddy ,  Rapolu Raji Reddy ,  Dasari Muralidhara Reddy

    IPC分类号： C07D401/12

    CPC分类号： C07D401/12

    摘要： The present invention relates to a novel amorphous form of esomeprazole hydrate, to a process for its preparation and to a pharmaceutical composition containing it. Thus, tetrahydrofuran and water are added to esomeprazole potassium salt at 25-30° C., cooled to 20° C. and then the pH is adjusted to 7.5-8.0 with acetic acid. The reaction mass is cooled to 5° C., stirred for 2 to 3 hours at 0-5° C., filtered the mass, washed with chilled mixture of water and tetrahydrofuran (2:1) and again washed with water. The wet cake is dried at 30-35° C. under vacuum to reach the moisture content to 25-30%. The solid is again dried in rotovapour at 25-30° C. under nitrogen atmosphere to give amorphous esomeprazole hydrate.

    摘要翻译： 本发明涉及一种新型的非晶形式的艾美拉唑水合物，其制备方法和含有它的药物组合物。 因此，将四氢呋喃和水在25-30℃加入到艾美拉唑钾盐中，冷却至20℃，然后用乙酸将pH调节至7.5-8.0。 将反应物质冷却至5℃，在0-5℃下搅拌2〜3小时，过滤物质，用冷却的水和四氢呋喃（2:1）的混合物洗涤，再次用水洗涤。 将湿滤饼在真空下在30-35℃下干燥以达到25-30％的含水量。 在氮气氛下，将固体在旋转蒸发器中再次干燥25-30℃，得到无定形艾美拉唑水合物。