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    STABLE NANOPARTICULATE DRUG SUSPENSION
    3.
    发明申请
    STABLE NANOPARTICULATE DRUG SUSPENSION 审中-公开
    稳定的纳米脂肪酸药物悬浮液

    公开(公告)号：US20100323020A1

    公开(公告)日：2010-12-23

    申请号：US12817640

    申请日：2010-06-17

    申请人： Rajeev Gokhale ,  Kennan C. Marsh ,  Yi Shi

    发明人： Rajeev Gokhale ,  Kennan C. Marsh ,  Yi Shi

    IPC分类号： A61K31/5377 ,  A61K9/14 ,  A61P35/04 ,  A61P35/00 ,  A61P7/00

    CPC分类号： A61K9/10 ,  A61K9/0095 ,  A61K31/5377 ,  A61K47/02 ,  A61K47/10

    摘要： A liquid pharmaceutical composition comprises an aqueous medium having suspended therein a solid particulate Bc1-2 family protein inhibitory compound such as ABT-263, having a D90 particle size not greater than about 3 μm; wherein the aqueous medium further comprises at least one pharmaceutically acceptable surfactant and at least one pharmaceutically acceptable basifying agent such as sodium bicarbonate in amounts that are effective together to inhibit particle size increase. The composition is suitable for oral or parenteral administration to a subject in need thereof for treatment of a disease characterized by overexpression of one or more anti-apoptotic Bc1-2 family proteins, for example cancer.

    摘要翻译： 液体药物组合物包含其中悬浮有固体颗粒Bc1-2家族蛋白质抑制化合物如ABT-263的水性介质，其D90粒度不大于约3μm; 其中所述水性介质还包含至少一种药学上可接受的表面活性剂和至少一种药学上可接受的碱化剂如碳酸氢钠，其量可以一起有效抑制粒度增加。 该组合物适合于需要其的受试者口服或肠胃外给药，用于治疗以一种或多种抗凋亡Bc1-2家族蛋白（例如癌症）过表达为特征的疾病。

    OCTAHYDRO-PYRROLO[3,4-B]PYRROLE N-OXIDES
    4.
    发明申请
    OCTAHYDRO-PYRROLO[3,4-B]PYRROLE N-OXIDES 有权
    OCTAHYDRO-PYRROLO [3,4-B] PYRROLE N-OXIDES

    公开(公告)号：US20090105267A1

    公开(公告)日：2009-04-23

    申请号：US12208604

    申请日：2008-09-11

    申请人： Marlon D. Cowart ,  Kennan C. Marsh ,  Huaqing Liu ,  Jae Y. Lee ,  Maria G. Beconi ,  Jill M. Wetter ,  Lawrence A. Black ,  Thomas C. Custer

    发明人： Marlon D. Cowart ,  Kennan C. Marsh ,  Huaqing Liu ,  Jae Y. Lee ,  Maria G. Beconi ,  Jill M. Wetter ,  Lawrence A. Black ,  Thomas C. Custer

    IPC分类号： A61K31/501 ,  C07D487/04 ,  A61P25/28

    CPC分类号： C07D487/04

    摘要： The invention relates to octahydro-pyrrolo[3,4-b]pyrrole N-oxides as prodrugs of CNS-active compounds, compositions comprising such compounds, methods for making the compounds, salts, and polymorphs, and methods of treating conditions and disorders using such compounds and compositions. Octahydro-pyrrolo[3,4-b]pyrrole N-oxides of formula (I) are prodrugs of histamine-3 antagonists, and are useful in treating conditions or disorders prevented by or ameliorated by histamine-3 receptor ligands. Octahydro-pyrrolo[3,4-b]pyrrole N-oxide compounds, methods for using such compounds, compositions for making them, and processes for preparing such compounds are disclosed herein.

    摘要翻译： 本发明涉及作为CNS活性化合物前药的八氢吡咯并[3,4-b]吡咯N-氧化物，包含这些化合物的组合物，制备化合物，盐和多晶型物的方法，以及使用 这些化合物和组合物。 式（I）的八氢 - 吡咯并[3,4-b]吡咯N-氧化物是组胺-3拮抗剂的前药，可用于治疗组胺-3受体配体预防或改善的病症或病症。 八氢吡咯并[3,4-b]吡咯N-氧化物化合物，使用这些化合物的方法，制备它们的组合物，以及这些化合物的制备方法。