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    IMPROVED PROCESS FOR PREPARING PALIPERIDONE, NOVEL POLYMORPHIC FORMS OF THE SAME AND PROCESS THEREOF
    5.
    发明申请
    IMPROVED PROCESS FOR PREPARING PALIPERIDONE, NOVEL POLYMORPHIC FORMS OF THE SAME AND PROCESS THEREOF 审中-公开
    改进的制备哌拉西酮的新方法及其新形式的多晶型物及其加工

    公开(公告)号：WO2009044413A2

    公开(公告)日：2009-04-09

    申请号：PCT/IN2008000642

    申请日：2008-10-06

    申请人： MATRIX LAB LTD ,  TYAGI OM DUTT ,  VELLENKI SIVA RAM PARASAD ,  SAHU ARABINDA ,  BALSU RAJABABU ,  PHADHURI NAVEEN KUMAR ,  JETTI RAMAKOTESWARA RAO ,  GORANTLA ASHA RANI ,  DATTA DEBAHISH

    发明人： TYAGI OM DUTT ,  VELLENKI SIVA RAM PARASAD ,  SAHU ARABINDA ,  BALSU RAJABABU ,  PHADHURI NAVEEN KUMAR ,  JETTI RAMAKOTESWARA RAO ,  GORANTLA ASHA RANI ,  DATTA DEBAHISH

    IPC分类号： C07D471/04

    CPC分类号： C07D471/04

    摘要： Disclosed herein is an improved process for producing paliperidone, wherein the process includes hydrogenating 3-(2-chloroethyl)-2-methyl-9-(hydroxyprotected)-4H- pyrido[1.2-a] pyrimidin-4-one in presence of an acid and a catalyst under hydrogen pressure to give 3-(2-chloroethyl)-6,7,8,9-tetrahydro-9-hydroxy-2-methyl-4H- pyrido[l,2-a]-pyrimidin-4-one and condensing 3-(2-chloroethyl)-6,7,8,9-tetrahydro-9- hydroxy-2-methyl-4H-pyrido[l,2-a] -pyrimidin-4-one with 6-fluoro-3-(4-piperidinyl)- 1,2-benzisoxazole in presence of a base and a solvent to give paliperidone. In addition, the invention discloses novel polymorphic Forms VI and VII of paliperidone. Furthermore the invention discloses processes for producing the novel polymorphic forms and Form I from the novel polymorphic forms thereof.

    摘要翻译： 本文公开了一种用于生产帕潘立酮的改进方法，其中该方法包括在存在下列物质的情况下氢化3-（2-氯乙基）-2-甲基-9-（羟基保护的）-4H-吡啶并[1,2-a]嘧啶-4-酮 （2-氯乙基）-6,7,8,9-四氢-9-羟基-2-甲基-4H-吡啶并[1,2-a] - 嘧啶-4-酮， 并将3-（2-氯乙基）-6,7,8,9-四氢-9-羟基-2-甲基-4H-吡啶并[1,2-a] - 嘧啶-4-酮与6-氟 - 3-（4-哌啶基）-1,2-苯并异恶唑在碱和溶剂存在下反应，得到帕潘立酮。 另外，本发明公开了帕潘立酮的新型多晶型物VI和VII。 此外，本发明公开了由其新多晶型形式制备新型多晶型和晶型I的方法。

    A PROCESS FOR PURIFICATION OF 7-(4-BROMOBUTOXY)-3,4 DIHYDROCARBOSTYRIL, AN INTERMEDIATE FOR MANUFACTURE OF ARIPIRAZOLE
    6.
    发明申请
    A PROCESS FOR PURIFICATION OF 7-(4-BROMOBUTOXY)-3,4 DIHYDROCARBOSTYRIL, AN INTERMEDIATE FOR MANUFACTURE OF ARIPIRAZOLE 审中-公开
    一种用于纯化7-（4-溴甲氧基）-3,4二氢碳二恶烷的方法，用于制备阿维拉唑的中间体

    公开(公告)号：WO2008026220A1

    公开(公告)日：2008-03-06

    申请号：PCT/IN2007/000310

    申请日：2007-07-24

    申请人： LUPIN LIMITED ,  TYAGI, Om, Dutt ,  THAPER, Rajesh ,  PRABHAVAT, Manoj, Devilalji ,  MANE, Narendra, Dattatreya ,  MAHAJAN, Sanjay ,  SRIVASTAVA, Tushar, Kumar

    发明人： TYAGI, Om, Dutt ,  THAPER, Rajesh ,  PRABHAVAT, Manoj, Devilalji ,  MANE, Narendra, Dattatreya ,  MAHAJAN, Sanjay ,  SRIVASTAVA, Tushar, Kumar

    IPC分类号： C07D401/12 ,  A61K31/496

    CPC分类号： C07D401/12 ,  C07D215/227

    摘要： A process for the purification of 7- (4-bromobutoxy)-3,4- dihydrocarbostyril, substantially free of dimer impurity, said process comprising providing a solution of crude 7- (4-bromobutoxy)-3,4- dihydrocarbostyril containing the dimer impurity in an organic solvent selected from the group of halogenated hydrocarbon solvent, aromatic hydrocarbon, alcohols, alkyl esters of C1-C4 alkanoic acids, ethers, diethyl ester and ketones ; converting to a salt by the addition of an inorganic acid; separation of 1,4-bis [3,4-dihydro-2 (1H)-quinolinone-7-oxy] butane salt (dimer impurity salt) from the mixture, based on the difference in at least one physical property of 7- (4-bromobutoxy)-3,4- dihydrocarbostyril salt and the salt of dimer impurity; liberating the 7- (4-bromobutoxy)-3,4- dihydrocarbostyril salt by treating with an inorganic base; precipitating 7- (4-bromobutoxy)-3,4- dihydrocarbostyril by adding an anti-solvent.

    摘要翻译： 一种净化7-（4-溴丁氧基）-3,4-二氢喹诺酮的方法，基本上不含二聚体杂质，所述方法包括提供含有二聚体的粗7-（4-溴丁氧基）-3,4-二氢喹诺酮的溶液 选自卤代烃溶剂，芳族烃，醇，C1-C4链烷酸的烷基酯，醚，二乙基酯和酮的有机溶剂中的杂质; 通过加入无机酸转化成盐; 基于七（（（（））的至少一种物理性质的不同，从混合物中分离1,4-双[3,4-二氢-2（1H） - 喹啉酮-7-氧]丁烷盐（二聚体杂质盐） 4-溴丁氧基）-3,4-二氢喹诺酮和二聚体杂质盐; 通过用无机碱处理释放7-（4-溴丁氧基）-3,4-二氢喹诺酮， 通过加入抗溶剂沉淀7-（4-溴丁氧基）-3,4-二氢喹诺酮。

    A CO-SPRAY DRIED COMPOSITION OF CEFEPIME WITH BASE AND PROCESS FOR PREPARATION THEREOF
    7.
    发明申请
    A CO-SPRAY DRIED COMPOSITION OF CEFEPIME WITH BASE AND PROCESS FOR PREPARATION THEREOF 审中-公开
    具有基础的CO喷雾干燥组合物及其制备方法

    公开(公告)号：WO2006106529A1

    公开(公告)日：2006-10-12

    申请号：PCT/IN2006/000114

    申请日：2006-04-03

    申请人： LUPIN LIMITED ,  TYAGI, Om, Dutt ,  CHAUHAN, Yogendra, Kumar ,  MEHARE, Kishor, Gulabrao

    发明人： TYAGI, Om, Dutt ,  CHAUHAN, Yogendra, Kumar ,  MEHARE, Kishor, Gulabrao

    IPC分类号： C07D501/00 ,  A61K31/545

    CPC分类号： C07D501/00

    摘要： Stable and sterile composition of cefepime and a process for preparing the same. Amorphous composition containing cefepime acid addition salt or solvates thereof and organic or inorganic base obtained by spray drying of their aqueous solution. The process comprises dissolving a composition containing mixture of cefepime acid addition salt and a pharmaceutically acceptable non-toxic organic or inorganic base in water to obtain aqueous solution, filtration of aqueous solution through 0.2 micron membrane filter and subjecting the clear aqueous solution to spray drying, or dissolving a cefepime acid addition salt in water, dissolving a pharmaceutically acceptable non-toxic organic or inorganic base in water, addition of solution from operation (v) to solution from operation (iv) at 0-30°C, preferably at 0-10°C to obtain a solution having a pH in the range of 3.0-7.0, filtration of aqueous solution through 0.2 micron membrane filter, and subjecting the clear aqueous solution to spray drying.

    摘要翻译： 头孢吡肟的稳定无菌组合物及其制备方法。 含有头孢吡肟酸加成盐或溶剂合物的无定形组合物和通过其水溶液的喷雾干燥获得的有机或无机碱。 该方法包括将含有头孢吡肟酸加成盐和药学上可接受的无毒有机或无机碱的混合物的组合物溶解在水中以获得水溶液，通过0.2微米膜过滤器过滤水溶液并使透明水溶液喷雾干燥， 或将头孢吡肟酸加成盐溶解在水中，将药学上可接受的无毒有机或无机碱溶解在水中，在操作（v）中加入溶液至0-30℃，优选0〜 10℃，得到pH范围为3.0-7.0的溶液，通过0.2微米膜过滤器过滤水溶液，并对透明水溶液进行喷雾干燥。

    NOVEL CRYSTALLINE FORMS OF DESLORATADINE AND PROCESS FOR PREPARING THE SAME
    10.
    发明申请
    NOVEL CRYSTALLINE FORMS OF DESLORATADINE AND PROCESS FOR PREPARING THE SAME 审中-公开
    新型氯仿的结晶形式及其制备方法

    公开(公告)号：WO2009122430A3

    公开(公告)日：2010-06-10

    申请号：PCT/IN2009000086

    申请日：2009-02-06

    申请人： MATRIX LAB LTD ,  TYAGI OM DUTT ,  JETTI RAMAKOTESWARA RAO ,  GORANTLA ASHNA RANI

    发明人： TYAGI OM DUTT ,  JETTI RAMAKOTESWARA RAO ,  GORANTLA ASHNA RANI

    IPC分类号： C07D401/04

    CPC分类号： C07D401/04

    摘要： The present invention provides novel crystalline polymorphic forms of desloratadine designated as Form (A) and Form (B), wherein said forms are characterized by different solid state techniques such as powder X-ray diffraction, differential scanning calorimetry, thermo gravimetric analysis and moisture content. Further, this invention discloses processes for preparation of said polymorphic forms. In addition, novel processes for preparing Form (I) and Form (II) of desloratadine and mixtures thereof are also disclosed.

    摘要翻译： 本发明提供了命名为形式（A）和形式（B）的地氯雷他定的新型结晶多晶形式，其中所述形式的特征在于不同的固态技术，例如粉末X射线衍射，差示扫描量热法，热重分析和水分含量 。 此外，本发明公开了所述多晶型物的制备方法。 此外，还公开了制备地氯雷他定的形式（I）和形式（II）的新方法及其混合物。