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    Pamoate salt of monoamine anti-Parkinson's agents, method of preparation and use thereof
    1.
    发明授权
    Pamoate salt of monoamine anti-Parkinson's agents, method of preparation and use thereof 有权

    公开(公告)号：US11234961B2

    公开(公告)日：2022-02-01

    申请号：US16639170

    申请日：2018-08-17

    申请人： Zi-Qiang Gu

    发明人： Zi-Qiang Gu

    IPC分类号： A61K31/381 ,  A61K9/00 ,  A61K31/404 ,  A61K31/428

    摘要： In various embodiments, provided herein are pamoate salts of monoamine Anti-Parkinsons disease agents including rotigotine, ropinirole, pramipexole, selegiline, rasagiline, and safinamide, pharmaceutical composition comprising the same, methods of preparing the same, and methods of using the same. For example, the pamoate salt herein can be characterized by a molar ratio of rotigotine, ropinirole, pramipexole, selegiline, rasagiline, or safinamide to pamoic acid of about 1:1 or about 2:1. The pamoate salt herein can also be crystalline including anhydrous, hydrate or solvate forms, or their polymorphs, or amorphous. The pamoate salts described herein can provide a long acting and/or extended release profile of the monoamine agents for the treatment of Parkinsons disease (PD). Thus, also provided herein are methods of preparing a long acting and/or extended release injectable formulation of the monoamine agents using their respective pamoate salts. And in some embodiments, provided herein are methods of treating a subject in need thereof comprising administering a pharmaceutical composition comprising a pamoate salt of rotigotine, ropinirole, pramipexole, selegiline, rasagiline, and/or safinamide.

    PAMOATE SALT OF MONOAMINE ANTI-PARKINSON'S AGENTS, METHOD OF PREPARATION AND USE THEREOF
    2.
    发明申请
    PAMOATE SALT OF MONOAMINE ANTI-PARKINSON'S AGENTS, METHOD OF PREPARATION AND USE THEREOF 审中-公开

    公开(公告)号：US20200230103A1

    公开(公告)日：2020-07-23

    申请号：US16639170

    申请日：2018-08-17

    申请人： Zi-Qiang GU

    发明人： Zi-Qiang GU

    IPC分类号： A61K31/381 ,  A61K9/00 ,  A61K31/404 ,  A61K31/428

    摘要： In various embodiments, provided herein are pamoate salts of monoamine Anti-Parkinsons disease agents including rotigotine, ropinirole, pramipexole, selegiline, rasagiline, and safinamide, pharmaceutical composition comprising the same, methods of preparing the same, and methods of using the same. For example, the pamoate salt herein can be characterized by a molar ratio of rotigotine, ropinirole, pramipexole, selegiline, rasagiline, or safinamide to pamoic acid of about 1:1 or about 2:1. The pamoate salt herein can also be crystalline including anhydrous, hydrate or solvate forms, or their polymorphs, or amorphous. The pamoate salts described herein can provide a long acting and/or extended release profile of the monoamine agents for the treatment of Parkinsons disease (PD). Thus, also provided herein are methods of preparing a long acting and/or extended release injectable formulation of the monoamine agents using their respective pamoate salts. And in some embodiments, provided herein are methods of treating a subject in need thereof comprising administering a pharmaceutical composition comprising a pamoate salt of rotigotine, ropinirole, pramipexole, selegiline, rasagiline, and/or safinamide.

    Alkylcarboxy amino acids-modulators of the kainate receptor
    4.
    发明授权
    Alkylcarboxy amino acids-modulators of the kainate receptor 失效
    红藻氨酸受体的烷基羧基氨基酸调节剂

    公开(公告)号：US5731348A

    公开(公告)日：1998-03-24

    申请号：US600330

    申请日：1996-02-13

    申请人： Zi-Qiang Gu

    发明人： Zi-Qiang Gu

    IPC分类号： A61K31/195 ,  A61P25/00 ,  C07C229/24 ,  C07C233/47 ,  C07C271/22 ,  C07C275/16 ,  C07D207/26 ,  C07D207/277 ,  C07D295/15

    CPC分类号： C07D207/26 ,  C07C229/24 ,  C07C233/47 ,  C07C271/22 ,  C07C275/16 ,  C07D207/277 ,  C07D295/15

    摘要： Compounds of a new class of alkyl carboxy amino acid analogs of glutamic acid act as specific regulators of the kainic acid EAA receptor cation channel. These compounds are useful for treating neurological, neuropsychological, neuropsychiatric, neurodegenerative, neuropsychopharmacological and functional disorders associated with excessive or insufficient activation of the kainic acid subtype of the ionotropic EAA receptors; treating cognitive disorders associated with deactivation, suboptimal activation or over-activation of the kainic acid receptor; alleviating pain and improving and enhancing memory, learning, and associated mental processes. A method for designing novel AMPA or kainic acid receptor agonists or antagonists is also disclosed.

    摘要翻译： 新一类谷氨酸的烷基羧基氨基酸类似物的化合物作为红藻氨酸EAA受体阳离子通道的特异性调节剂。 这些化合物可用于治疗与离子型EAA受体的红藻氨酸亚型的过度或不足活化相关的神经精神病学，神经变性学，神经精神药理学和功能障碍; 治疗与失活，次最佳活化或过度活化红藻氨酸受体相关的认知障碍; 减轻痛苦，改善和增强记忆力，学习能力和相关的心理过程。 还公开了设计新的AMPA或红藻氨酸受体激动剂或拮抗剂的方法。

    PAMOATE SALT OF MONOAMINE ANTI-PARKINSON'S AGENTS, METHOD OF PREPARATION AND USE THEREOF
    6.
    发明申请
    PAMOATE SALT OF MONOAMINE ANTI-PARKINSON'S AGENTS, METHOD OF PREPARATION AND USE THEREOF 有权

    公开(公告)号：US20220296568A1

    公开(公告)日：2022-09-22

    申请号：US17586354

    申请日：2022-01-27

    申请人： Zi-Qiang GU

    发明人： Zi-Qiang GU

    IPC分类号： A61K31/381 ,  A61K9/00 ,  A61K31/404 ,  A61K31/428

    摘要： In various embodiments, provided herein are pamoate salts of monoamine Anti-Parkinsons disease agents including rotigotine, ropinirole, pramipexole, selegiline, rasagiline, and safinamide, pharmaceutical composition comprising the same, methods of preparing the same, and methods of using the same. For example, the pamoate salt herein can be characterized by a molar ratio of rotigotine, ropinirole, pramipexole, selegiline, rasagiline, or safinamide to pamoic acid of about 1:1 or about 2:1. The pamoate salt herein can also be crystalline including anhydrous, hydrate or solvate forms, or their polymorphs, or amorphous. The pamoate salts described herein can provide a long acting and/or extended release profile of the monoamine agents tor the treatment of Parkinsons disease (PD). Thus, also provided herein are methods of preparing a long acting and/or extended release injectable formulation of the monoamine agents using their respective pamoate salts. And in some embodiments, provided herein are methods of treating a subject in need thereof comprising administering a pharmaceutical composition comprising a pamoate salt of rotigotine, ropinirole, pramipexole, selegiline, rasagiline, and/or safinamide.