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16 条记录 (耗时 0.028 秒)

    DISODIUM SALTS, MONOHYDRATES, AND ETHANOL SOLVATES FOR DELIVERING ACTIVE AGENTS
    8.
    发明申请
    DISODIUM SALTS, MONOHYDRATES, AND ETHANOL SOLVATES FOR DELIVERING ACTIVE AGENTS 有权
    用于递送活性剂的二盐，单酯和乙醇溶剂

    公开(公告)号：US20110251125A1

    公开(公告)日：2011-10-13

    申请号：US13053641

    申请日：2011-03-22

    申请人： William E. Bay ,  Rajesh K. Agarwal ,  Kiran Chaudhary ,  Shingai Majuru ,  Michael M. Goldberg ,  Joanne P. Corvino ,  Moise Azria ,  Joseph M. Ault ,  Simon D. Bateman ,  Subash Patel ,  Joseph Sikora ,  Rebecca F. Yang ,  Joseph L. Zielinski

    发明人： William E. Bay ,  Rajesh K. Agarwal ,  Kiran Chaudhary ,  Shingai Majuru ,  Michael M. Goldberg ,  Joanne P. Corvino ,  Moise Azria ,  Joseph M. Ault ,  Simon D. Bateman ,  Subash Patel ,  Joseph Sikora ,  Rebecca F. Yang ,  Joseph L. Zielinski

    IPC分类号： A61K38/23

    CPC分类号： C07C231/00 ,  A61K9/2013 ,  A61K47/183 ,  C07C235/60 ,  C07D265/26 ,  C07C235/58

    摘要： The inventors have discovered that the disodium salt of certain delivery agents has surprisingly greater efficacy for delivering active agents than the corresponding monosodium salt. Furthermore, the inventors have discovered that the disodium salts of these delivery agents form solvates with ethanol and hydrates with water. The delivery agents have the formula wherein R1, R2, R3, and R4 are independently hydrogen, halogen, C1-C4 alkyl, or C1-C4 alkoxy; and R5 is a substituted or unsubstituted C2-C16alkylene, substituted or unsubstituted C2-C16 alkenylene, substituted or unsubstituted C1-C12 alkyl(arylene), or substituted or unsubstituted aryl(C1-C12 alkylene). The hydrates and solvates of present invention also have surprisingly greater efficacy for delivering active agents, such as heparin and calcitonin, than their corresponding monosodium salts and free acids. The present invention provides an alcohol solvate, such as ethanol solvate, of a disodium salt of a delivery agent of the formula above. The invention also provides a hydrate of a disodium salt of a delivery agent of the formula above. Preferred delivery agents include, but are not limited to, N-(5-chlorosalicyloyl)-8-aminocaprylic acid (5-CNAC), N-(10-[2-hydroxybenzoyl]amino)decanoic acid (SNAD), and sodium N-(8-[2-hydroxybenzoyl]amino)caprylate (SNAC). The invention also provides methods of preparing the disodium salt, ethanol solvate, and hydrate and compositions containing the disodium salt, ethanol solvate, and/or hydrate.

    摘要翻译： 发明人已经发现，某些递送剂的二钠盐比相应的单钠盐具有惊人的更大的递送活性剂的功效。 此外，本发明人已经发现，这些递送剂的二钠盐与乙醇形成溶剂合物并与水合。 递送剂具有下式：其中R 1，R 2，R 3和R 4独立地是氢，卤素，C 1 -C 4烷基或C 1 -C 4烷氧基; 取代或未取代的C 2 -C 16亚烷基，取代或未取代的C 1 -C 12烷基（亚芳基）或取代或未取代的芳基（C 1 -C 12亚烷基）。 本发明的水合物和溶剂合物对于递送活性剂（例如肝素和降钙素）比其相应的单钠盐和游离酸具有惊人的更大的功效。 本发明提供了一种醇溶剂合物，例如乙醇溶剂化物，其具有上式的递送剂的二钠盐。 本发明还提供了上式的递送剂的二钠盐的水合物。 优选的递送剂包括但不限于N-（5-氯水杨酰基）-8-氨基辛酸（5-CNAC），N-（10- [2-羟基苯甲酰基]氨基）癸酸（SNAD）和N - （8- [2-羟基苯甲酰基]氨基）辛酸酯（SNAC）。 本发明还提供了制备二钠盐，乙醇溶剂合物和水合物的方法以及含有二钠盐，乙醇溶剂化物和/或水合物的组合物。

    Disodium salts, monohydrates, and ethanol solvates for delivering active agents
    9.
    发明授权
    Disodium salts, monohydrates, and ethanol solvates for delivering active agents 有权
    用于递送活性剂的二钠盐，一水合物和乙醇溶剂化物

    公开(公告)号：US07659311B2

    公开(公告)日：2010-02-09

    申请号：US12111750

    申请日：2008-04-29

    申请人： William Elliott Bay ,  Rajesh K. Agarwal ,  Kiran Chaudhary ,  Shingai Majuru ,  Michael M. Goldberg ,  JoAnne P. Corvino ,  Moise Azria ,  Joseph Ault ,  Simon D. Bateman ,  Subash Patel ,  Joseph Sikora ,  Rebecca F. Yang ,  Joseph L. Zielinski

    发明人： William Elliott Bay ,  Rajesh K. Agarwal ,  Kiran Chaudhary ,  Shingai Majuru ,  Michael M. Goldberg ,  JoAnne P. Corvino ,  Moise Azria ,  Joseph Ault ,  Simon D. Bateman ,  Subash Patel ,  Joseph Sikora ,  Rebecca F. Yang ,  Joseph L. Zielinski

    IPC分类号： A61K31/195 ,  C07C229/00

    CPC分类号： C07C231/00 ,  A61K9/2013 ,  A61K47/183 ,  C07C235/60 ,  C07D265/26 ,  C07C235/58

    摘要： The inventors have discovered that the disodium salt of certain delivery agents has surprisingly greater efficacy for delivering active agents than the corresponding monosodium salt. Furthermore, the inventors have discovered that the disodium salts of these delivery agents form solvates with ethanol and hydrates with water. The delivery agents have the formula wherein R1, R2, R3, and R4 are independently hydrogen, halogen, C1-C4 alkyl, or C1-C4 alkoxy; and R5 is a substituted or unsubstituted C2-C16 alkylene, substituted or unsubstituted C2-C16 alkenylene, substituted or unsubstituted C1-C12 alkyl(arylene), or substituted or unsubstituted aryl(C1-C12 alkylene). The hydrates and solvates of present invention also have surprisingly greater efficacy for delivering active agents, such as heparin and calcitonin, than their corresponding monosodium salts and free acids. The present invention provides an alcohol solvate, such as ethanol solvate, of a disodium salt of a delivery agent of the formula above. The invention also provides a hydrate of a disodium salt of a delivery agent of the formula above. Preferred delivery agents include, but are not limited to, N-(5-chlorosalicyloyl)-8-aminocaprylic acid (5-CNAC), N-(10-[2-hydroxybenzoyl]amino)decanoic acid (SNAD), and sodium N-(8-[2-hydroxybenzoyl]amino)caprylate (SNAC). The invention also provides methods of preparing the disodium salt, ethanol solvate, and hydrate and compositions containing the disodium salt, ethanol solvate, and/or hydrate.

    摘要翻译： 发明人已经发现，某些递送剂的二钠盐比相应的单钠盐具有惊人的更大的递送活性剂的功效。 此外，本发明人已经发现，这些递送剂的二钠盐与乙醇形成溶剂合物并与水合。 递送剂具有下式：其中R 1，R 2，R 3和R 4独立地是氢，卤素，C 1 -C 4烷基或C 1 -C 4烷氧基; 取代或未取代的C 2 -C 16亚烯基，取代或未取代的C 1 -C 12烷基（亚芳基）或取代或未取代的芳基（C 1 -C 12亚烷基）。 本发明的水合物和溶剂合物对于递送活性剂（例如肝素和降钙素）比其相应的单钠盐和游离酸具有惊人的更大的功效。 本发明提供了一种醇溶剂合物，例如乙醇溶剂化物，其具有上式的递送剂的二钠盐。 本发明还提供了上式的递送剂的二钠盐的水合物。 优选的递送剂包括但不限于N-（5-氯水杨酰基）-8-氨基辛酸（5-CNAC），N-（10- [2-羟基苯甲酰基]氨基）癸酸（SNAD）和N - （8- [2-羟基苯甲酰基]氨基）辛酸酯（SNAC）。 本发明还提供了制备二钠盐，乙醇溶剂合物和水合物的方法以及含有二钠盐，乙醇溶剂合物和/或水合物的组合物。

    Pharmaceutical Compositions of a 5-HT2A Serotonin Receptor Modulator Useful for the Treatment of Disorders Related Thereto
    10.
    发明申请
    Pharmaceutical Compositions of a 5-HT2A Serotonin Receptor Modulator Useful for the Treatment of Disorders Related Thereto 审中-公开
    用于治疗相关疾病的5-HT2A血清素受体调节剂的药物组合物

    公开(公告)号：US20090053306A1

    公开(公告)日：2009-02-26

    申请号：US11992806

    申请日：2006-09-28

    申请人： Rajesh K. Agarwal ,  Rampurna Prasad Gullapalli ,  Michael Martin ,  Michael Morgan ,  Dennis Chapman ,  Joseph Belier Speer ,  Yun Shan

    发明人： Rajesh K. Agarwal ,  Rampurna Prasad Gullapalli ,  Michael Martin ,  Michael Morgan ,  Dennis Chapman ,  Joseph Belier Speer ,  Yun Shan

    IPC分类号： A61K31/415 ,  A61K9/48

    CPC分类号： A61K9/4858 ,  A61K9/4866 ,  A61K31/415 ,  Y02A50/467

    摘要： The present invention relates to certain pharmaceutical compositions of a 5-HT2A serotonin receptor modulator and methods for preparing pharmaceutical composition related thereto. The pharmaceutical compositions are useful in the treatment of platelet aggregation, coronary artery disease, myocardial infarction, transient ischemic attack, angina, stroke, atrial fibrillation, reducing the risk of blood clot formation, asthma or symptoms thereof, agitation or a symptom, behavioral disorders, drug induced psychosis, excitative psychosis, Gilles de la Tourette's syndrome, manic disorder, organic or NOS psychosis, psychotic disorder, psychosis, acute schizophrenia, chronic schizophrenia, NOS schizophrenia and related disorders, sleep disorders, diabetic-related disorders, progressive multifocal leukoencephalopathy and the like.

    摘要翻译： 本发明涉及5-HT2A 5-羟色胺受体调节剂的某些药物组合物及其制备药物组合物的方法。 药物组合物可用于治疗血小板聚集，冠状动脉疾病，心肌梗塞，短暂性脑缺血发作，心绞痛，中风，心房颤动，降低血块形成风险，哮喘或其症状，躁动或症状，行为障碍 ，药物诱发的精神病，精神病，精神病，吉非替尼杜勒特综合征，躁狂症，有机或NOS精神病，精神病，精神病，急性精神分裂症，慢性精神分裂症，精神分裂症，精神分裂症和相关疾病，睡眠障碍，糖尿病相关疾病，进行性多灶性白质脑病 等等。