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    PROCESS FOR PURIFICATION OF APREPITANT
    1.
    发明申请
    PROCESS FOR PURIFICATION OF APREPITANT 审中-公开
    净化方法

    公开(公告)号：US20130345418A1

    公开(公告)日：2013-12-26

    申请号：US13872373

    申请日：2013-04-29

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

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

    IPC分类号： C07D413/06

    CPC分类号： C07D413/06

    摘要： The present invention relates to a process for obtaining pure aprepitant substantially free of undesired diastereomeric isomer, namely 5-[2(S)-[1(RS)-[3,5-bis(trifluoromethyl)-phenypethoxy]-3-(S)-(4-fluorophenyl)-morpholin-4-yl-methyl]-3,4-dihydro-2H-1,2,4-triazol-3-one. The present invention further provides an improved process for preparation of aprepitant crystalline form II. The present invention also relates to novel amorphous form of aprepitant, a process for its preparation and to a pharmaceutical composition comprising it. The present invention further relates to aprepitant having a mean particle size of less than about 11.5 microns, a process for its preparation and to a pharmaceutical composition comprising it. Thus, for example, aprepitant having a content of diastereomeric impurity of 1.1% is dissolved in ethyl acetate at 70° C., the solution is concentrated to half the initial volume by distilling off ethyl acetate, and the resulting solid is collected at 0-5° C. to give pure aprepitant substantially free of its diastereomeric impurity.

    摘要翻译： 本发明涉及一种获得基本上不含不期望的非对映体异构体的纯阿拉曲肽的方法，即5- [2（S） - [1（RS） - [3,5-双（三氟甲基） - 苯乙氧基] -3- ） - （4-氟苯基） - 吗啉-4-基 - 甲基] -3,4-二氢-2H-1,2,4-三唑-3-酮。 本发明进一步提供了制备阿瑞匹坦晶型II的改进方法。 本发明还涉及新型无定形形式的阿瑞匹坦，其制备方法和包含它的药物组合物。 本发明还涉及具有小于约11.5微米的平均粒度的阿瑞匹坦剂，其制备方法和包含其的药物组合物。 因此，例如，将具有1.1％非对映异构体杂质的阿瑞消制剂溶于70℃的乙酸乙酯中，通过蒸馏除去乙酸乙酯将溶液浓缩至初始体积的一半，并将所得固体在0- 5℃，得到基本上不含其非对映异构体杂质的纯制剂。

    Process for erlotinib hydrochloride
    3.
    发明授权
    Process for erlotinib hydrochloride 有权
    盐酸厄洛替尼的方法

    公开(公告)号：US08389531B2

    公开(公告)日：2013-03-05

    申请号：US11994613

    申请日：2007-07-11

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

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

    IPC分类号： A01N43/54 ,  A61K31/517 ,  C07D239/72

    CPC分类号： C07D239/94

    摘要： The present invention provides an improved and commercially viable process for preparation of erlotinib substantially free of N-methoxyethyl impurity, namely N-[(3-ethynylphenyl)-(2-methoxyethyl)]-6,7-bis(2-methoxyethoxy)-4-quinazolinamine, and its pharmaceutically acceptable acid addition salts thereof in high purity and in high yield. According to the present invention, erlotinib or a pharmaceutically acceptable acid addition salt of erlotinib substantially free of N-methoxyethyl impurity is prepared by isolating erlotinib or a pharmaceutically acceptable salt of erlotinib from a solvent medium comprising dimethyl sulfoxide and an alcoholic solvent.

    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不含N-甲氧基乙基杂质的厄洛替尼即N - [（3-乙炔基苯基） - （2-甲氧基乙基）] -6,7-双（2-甲氧基乙氧基） - 4-喹唑啉胺及其药学上可接受的酸加成盐，其纯度高，产率高。 根据本发明，通过从包含二甲基亚砜和醇溶剂的溶剂介质中分离厄洛替尼或埃洛替尼的药学上可接受的盐，来制备基本上不含N-甲氧基乙基杂质的厄洛替尼或其药学上可接受的厄洛替尼的酸加成盐。

    PROCESS FOR PURIFICATION OF APREPITANT
    6.
    发明申请
    PROCESS FOR PURIFICATION OF APREPITANT 审中-公开
    净化方法

    公开(公告)号：US20090149462A1

    公开(公告)日：2009-06-11

    申请号：US11915864

    申请日：2006-08-28

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

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

    IPC分类号： A61K31/5377 ,  C07D413/06

    CPC分类号： C07D413/06

    摘要： The present invention relates to a process for obtaining pure aprepitant substantially free of undesired diastereomeric isomer, namely 5-[2(S)-[1(RS)-[3,5-bis(trifluoromethyl)-phenyl)ethoxy]-3-(S)-(4-fluorophenyl)-morpholin-4-yl-methyl]-3,4-dihydro-2H-1,2,4-triazol-3-one. The present invention further provides an improved process for preparation of aprepitant crystalline form II. The present invention also relates to novel amorphous form of aprepitant, a process for its preparation and to a pharmaceutical composition comprising it. The present invention further relates to aprepitant having a mean particle size of less than about 11.5 microns, a process for its preparation and to a pharmaceutical composition comprising it. Thus, for example, aprepitant having a content of diastereomeric impurity of 1.1% is dissolved in ethyl acetate at 70° C., the solution is concentrated to half the initial volume by distilling off ethyl acetate, and the resulting solid is collected at 0-5° C. to give pure aprepitant substantially free of its diastereomeric impurity.

    摘要翻译： 本发明涉及一种获得基本上不含不需要的非对映体异构体的纯阿拉米特的方法，即5- [2（S） - [1（RS） - [3,5-双（三氟甲基） - 苯基） - 乙氧基] -3- （S） - （4-氟苯基） - 吗啉-4-基 - 甲基] -3,4-二氢-2H-1,2,4-三唑-3-酮。 本发明进一步提供了制备阿瑞匹坦晶型II的改进方法。 本发明还涉及新型无定形形式的阿瑞匹坦，其制备方法和包含它的药物组合物。 本发明还涉及具有小于约11.5微米的平均粒度的阿瑞匹坦剂，其制备方法和包含其的药物组合物。 因此，例如，将具有1.1％非对映异构体杂质的阿瑞消制剂溶于70℃的乙酸乙酯中，通过蒸馏除去乙酸乙酯将溶液浓缩至初始体积的一半，并将所得固体在0- 5℃，得到基本上不含其非对映异构体杂质的纯制剂。

    Polymorphs of sunitinib malate
    7.
    发明授权
    Polymorphs of sunitinib malate 有权
    苹果酸舒尼替尼的多晶型物

    公开(公告)号：US08329740B2

    公开(公告)日：2012-12-11

    申请号：US13120453

    申请日：2009-01-02

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

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

    IPC分类号： A61K31/4015 ,  C07D209/34

    CPC分类号： C07D403/06

    摘要： The present invention provides a novel crystalline form of sunitinib malate, process for its preparation and to pharmaceutical composition containing it. The present invention also provides a process for preparation of sunitinib malate crystal form I. Thus, for example, sunitinib malate was added to water, the mixture was heated to 80 deg C. to obtain a clear solution and stirred for 30 minutes at 80 deg C., slowly cooled to room temperature and the solution was subjected to freeze drying at about −90 deg C. for 8 hours to give sunitinib malate crystalline form III.

    摘要翻译： 本发明提供了一种新型的苹果酸舒尼替尼的结晶形式，其制备方法和含有它的药物组合物。 本发明还提供了制备苹果酸舒尼替尼结晶形式I的方法。因此，例如，将苹果酸舒尼替尼加入水中，将混合物加热至80℃以获得澄清溶液，并在80℃下搅拌30分钟 将其缓慢冷却至室温，并将溶液在约-90℃下冷冻干燥8小时，得到苹果酸舒尼替尼结晶形式III。

    PROCESS FOR ERLOTINIB HYDROCHLORIDE
    8.
    发明申请
    PROCESS FOR ERLOTINIB HYDROCHLORIDE 有权
    ERLOTINIB氢氯化物的方法

    公开(公告)号：US20100130741A1

    公开(公告)日：2010-05-27

    申请号：US11994613

    申请日：2007-07-11

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

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

    IPC分类号： C07D239/94

    CPC分类号： C07D239/94

    摘要： The present invention provides an improved and commercially viable process for preparation of erlotinib substantially free of N-methoxyethyl impurity, namely N-[(3-ethynylphenyl)-(2-methoxyethyl)]-6,7-bis(2-methoxyethoxy)-4-quinazolinamine, and its pharmaceutically acceptable acid addition salts thereof in High purity and in high yield. According to the present invention, erlotinib or a pharmaceutically acceptable acid addition salt of erlotinib substantially free of N-methoxyethyl impurity is prepared by isolating erlotinib or a pharmaceutically acceptable salt of erlotinib from a solvent medium comprising dimethyl sulfoxide and an alcoholic solvent.

    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不含N-甲氧基乙基杂质的厄洛替尼即N - [（3-乙炔基苯基） - （2-甲氧基乙基）] -6,7-双（2-甲氧基乙氧基） - 4-喹唑啉胺及其药学上可接受的酸加成盐，其纯度高，产率高。 根据本发明，通过从包含二甲基亚砜和醇溶剂的溶剂介质中分离厄洛替尼或埃洛替尼的药学上可接受的盐，来制备基本上不含N-甲氧基乙基杂质的厄洛替尼或其药学上可接受的厄洛替尼的酸加成盐。

    NOVEL POLYMORPHS OF SUNITINIB MALATE
    9.
    发明申请
    NOVEL POLYMORPHS OF SUNITINIB MALATE 有权
    新西兰麻黄碱的新型聚合物

    公开(公告)号：US20110306647A1

    公开(公告)日：2011-12-15

    申请号：US13120453

    申请日：2009-01-02

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

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

    IPC分类号： A61K31/404 ,  A61P35/00 ,  C07D403/14

    CPC分类号： C07D403/06

    摘要： The present invention provides a novel crystalline form of sunitinib malate, process for its preparation and to pharmaceutical composition containing it. The present invention also provides a process for preparation of sunitinib malate crystal form I. Thus, for example, sunitinib malate was added to water, the mixture was heated to 80 deg C. to obtain a clear solution and stirred for 30 minutes at 80 deg C., slowly cooled to room temperature and the solution was subjected to freeze drying at about −90 deg C. for 8 hours to give sunitinib malate crystalline form III.

    摘要翻译： 本发明提供了一种新型的苹果酸舒尼替尼的结晶形式，其制备方法和含有它的药物组合物。 本发明还提供了制备苹果酸舒尼替尼结晶形式I的方法。因此，例如，将苹果酸舒尼替尼加入水中，将混合物加热至80℃以获得澄清溶液，并在80℃下搅拌30分钟 将其缓慢冷却至室温，并将溶液在约-90℃下冷冻干燥8小时，得到苹果酸舒尼替尼结晶形式III。