NOVEL SOLID FORMS OF EPALRESTAT
    1.
    发明申请
    NOVEL SOLID FORMS OF EPALRESTAT 有权
    EPALRESTAT的新型固体形式

    公开(公告)号:US20110275681A1

    公开(公告)日:2011-11-10

    申请号:US13013786

    申请日:2011-01-25

    CPC分类号: C07D277/36 A61K31/426

    摘要: The invention relates to novel crystalline salts of 5-[(1Z,2E)-2-methyl-3-phenylpropenylidene]-4-oxo-2-thioxo-3-thiazolidineacetic acid and a novel betaine cocrystal of 5-[(1Z,2E)-2-methyl-3-phenylpropenylidene]-4-oxo-2-thioxo-3-thiazolidineacetic acid. The preparation and characterization of the novel crystalline salts and cocrystal according to various embodiments of the invention is described. The invention also relates to pharmaceutical compositions containing the novel crystalline salts and cocrystal and the therapeutic use of the novel crystalline salts and cocrystal to treat and/or prevent various conditions, including treating and/or preventing diabetic complications, inhibiting aldose reductase, and affording cardioprotection in patients who may be non-diabetic.

    摘要翻译: 本发明涉及5 - [(1Z,2E)-2-甲基-3-苯基亚丙基] -4-氧代-2-硫代-3-噻唑烷乙酸的新型结晶盐和5 - [(1Z, 2E)-2-甲基-3-苯基亚丙叉基] -4-氧代-2-硫代-3-噻唑烷乙酸。 描述根据本发明的各种实施方案的新型结晶盐和共晶的制备和表征。 本发明还涉及含有新结晶盐和共结晶的药物组合物以及新型结晶盐和共结晶治疗和/或预防各种病症的治疗用途,包括治疗和/或预防糖尿病并发症,抑制醛糖还原酶和提供心脏保护作用 可能患有非糖尿病的患者。

    Choline cocrystal of epalrestat
    2.
    发明授权
    Choline cocrystal of epalrestat 有权
    胆碱共同结晶

    公开(公告)号:US08906948B2

    公开(公告)日:2014-12-09

    申请号:US13062644

    申请日:2009-09-03

    摘要: The invention relates to a novel choline cocrystal of 5-[(1Z,2E)-2-methyl-3-phenylpropenylidene]-4-oxo-2-thioxo-3-thiazolidineacetic acid. The preparation and characterization of the novel choline cocrystal according to various embodiments of the invention is described. The invention also relates to pharmaceutical compositions containing the novel choline cocrystal and the therapeutic use of the novel choline cocrystal to treat and/or prevent various conditions, including treating and/or preventing diabetic complications, treating and/or preventing homocystinuria reducing levels of homocysteine in blood serum, inhibiting aldose reductase, and affording cardioprotection in non-diabetic patients.

    摘要翻译: 本发明涉及5 - [(1Z,2E)-2-甲基-3-苯基亚丙基] -4-氧代-2-硫代-3-噻唑烷乙酸的新型胆碱共结晶。 描述了根据本发明的各种实施方案的新型胆碱共晶体的制备和表征。 本发明还涉及含有新型胆碱共结晶的药物组合物和新型胆碱共结晶治疗和/或预防各种病症的治疗用途,包括治疗和/或预防糖尿病并发症,治疗和/或预防同型半胱氨酸的同型半胱氨酸降低水平 血清,抑制醛糖还原酶,并在非糖尿病患者中提供心脏保护作用。

    Solid forms of epalrestat
    3.
    发明授权
    Solid forms of epalrestat 有权
    epalrestat的固体形式

    公开(公告)号:US08697735B2

    公开(公告)日:2014-04-15

    申请号:US13013786

    申请日:2011-01-25

    IPC分类号: A61K31/426 C07D277/36

    CPC分类号: C07D277/36 A61K31/426

    摘要: The invention relates to novel crystalline salts of 5-[(1Z,2E)-2-methyl-3-phenylpropenylidene]-4-oxo-2-thioxo-3-thiazolidineacetic acid and a novel betaine cocrystal of 5-[(1Z,2E)-2-methyl-3-phenylpropenylidene]-4-oxo-2-thioxo-3-thiazolidineacetic acid. The preparation and characterization of the novel crystalline salts and cocrystal according to various embodiments of the invention is described. The invention also relates to pharmaceutical compositions containing the novel crystalline salts and cocrystal and the therapeutic use of the novel crystalline salts and cocrystal to treat and/or prevent various conditions, including treating and/or preventing diabetic complications, inhibiting aldose reductase, and affording cardioprotection in patients who may be non-diabetic.

    摘要翻译: 本发明涉及5 - [(1Z,2E)-2-甲基-3-苯基亚丙基] -4-氧代-2-硫代-3-噻唑烷乙酸的新型结晶盐和5 - [(1Z, 2E)-2-甲基-3-苯基亚丙叉基] -4-氧代-2-硫代-3-噻唑烷乙酸。 描述根据本发明的各种实施方案的新型结晶盐和共晶的制备和表征。 本发明还涉及含有新结晶盐和共结晶的药物组合物以及新型结晶盐和共结晶治疗和/或预防各种病症的治疗用途,包括治疗和/或预防糖尿病并发症,抑制醛糖还原酶和提供心脏保护作用 可能患有非糖尿病的患者。

    NOVEL FORMS OF EPERISONE
    4.
    发明申请
    NOVEL FORMS OF EPERISONE 审中-公开
    EPERISONE的新形式

    公开(公告)号:US20120196895A1

    公开(公告)日:2012-08-02

    申请号:US13144292

    申请日:2010-01-11

    CPC分类号: C07D295/108 A61K31/445

    摘要: The invention relates to novel crystalline forms of (2RS)-1-(4-ethylphenyl)-2-methyl-3-piperidin-1-yl-propan-1-one. The preparation and characterization of the novel crystalline forms according to various embodiments of the invention is described. The invention also relates to pharmaceutical compositions containing the novel crystalline forms, which are useful to treat and/or prevent various conditions such as pathological muscle contracture, myotonic conditions, and spastic paralysis or spasticity caused by various neurologic conditions, and are also useful for the treatment and/or prevention of various types of pain and pathological muscle tension.

    摘要翻译: 本发明涉及(2RS)-1-(4-乙基苯基)-2-甲基-3-哌啶-1-基 - 丙-1-酮的新型结晶形式。 描述根据本发明的各种实施方案的新型结晶形式的制备和表征。 本发明还涉及含有新型结晶形式的药物组合物,其可用于治疗和/或预防各种病症如病理性肌肉挛缩,强直条件和由各种神经病症引起的痉挛性麻痹或痉挛状态,并且还可用于 治疗和/或预防各种类型的疼痛和病理性肌肉紧张。

    NOVEL FORMS OF EPERISONE
    5.
    发明申请
    NOVEL FORMS OF EPERISONE 审中-公开
    EPERISONE的新形式

    公开(公告)号:US20110281911A1

    公开(公告)日:2011-11-17

    申请号:US13057542

    申请日:2009-08-03

    CPC分类号: C07D295/108

    摘要: The invention relates to substantially enantiopure crystalline salt forms of (2RS)-I-(4-Ethylphenyl)-2-methyl-3-piperidin-1-ylpropan-1-one. The preparation and characterization of the substantially enantiopure crystalline salt forms according to various embodiments of the invention is described. The invention also relates to pharmaceutical compositions containing the substantially enantiopure crystalline salt forms, which are useful to treat and/or prevent various conditions such as pathological muscle contracture, myotome conditions, and spastic paralysis or spasticity caused by various neurologic conditions, and are also useful for the treatment and/or prevention of various types of pain and pathological muscle tension.

    摘要翻译: 本发明涉及(2RS)-1-(4-乙基苯基)-2-甲基-3-哌啶-1-基丙-1-酮的基本对映体纯的结晶盐形式。 描述了根据本发明的各种实施方案的基本对映体纯的结晶盐形式的制备和表征。 本发明还涉及含有基本上对映体纯的结晶盐形式的药物组合物,其可用于治疗和/或预防各种病症如病理性肌肉挛缩,肌肉破裂症状,以及由各种神经病症引起的痉挛性麻痹或痉挛状态,并且也是有用的 用于治疗和/或预防各种类型的疼痛和病理性肌肉紧张。

    NOVEL FORMS OF REBOXETINE
    7.
    发明申请
    NOVEL FORMS OF REBOXETINE 审中-公开
    新形式的复方

    公开(公告)号:US20100069389A1

    公开(公告)日:2010-03-18

    申请号:US12553564

    申请日:2009-09-03

    CPC分类号: C07D265/30

    摘要: The invention relates to novel crystalline forms of (2R)-2-[(R)-(2-ethoxyphenoxy)-phenylmethyl]morpholine hydrochloride. In various embodiments, the novel crystalline forms may be substantially enantiopure. The preparation and characterization of the novel crystalline forms of (2R)-2-[(R)-(2-ethoxyphenoxy)-phenylmethyl]morpholine hydrochloride is also described. The invention also relates to pharmaceutical compositions containing novel crystalline forms of (2R)-2-[(R)-(2-ethoxyphenoxy)-phenylmethyl]morpholine hydrochloride, which are useful to treat and/or prevent various conditions such as nervous system and pain disorders.

    摘要翻译: 本发明涉及(2R)-2 - [(R) - (2-乙氧基苯氧基) - 苯基甲基]吗啉盐酸盐的新结晶形式。 在各种实施方案中,新的结晶形式可以是基本上对映体纯的。 还描述了(2R)-2 - [(R) - (2-乙氧基苯氧基) - 苯基甲基]吗啉盐酸盐的新结晶形式的制备和表征。 本发明还涉及包含(2R)-2 - [(R) - (2-乙氧基苯氧基) - 苯基甲基]吗啉盐酸盐的新结晶形式的药物组合物,其可用于治疗和/或预防各种病症如神经系统和 疼痛障碍