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    • 4. 发明申请
    • Methods and compositions for studying, imaging, and treating pain
    • 用于研究,成像和治疗疼痛的方法和组合物
    • US20100284913A1
    • 2010-11-11
    • US12800053
    • 2010-05-07
    • Justin Du BoisJohn MulcahyBrian AndresenDavid C. YeomansSandip Biswal
    • Justin Du BoisJohn MulcahyBrian AndresenDavid C. YeomansSandip Biswal
    • A61K51/04C07D487/14C07K16/00C07K14/00C07H21/04A61K31/519A61K47/48A61K38/02A61P1/00A61P13/00A61P25/00A61P25/08A61P29/00A61K49/16A61K49/14A61K49/12A61K49/10A61K38/43A61P17/00A61K31/58C12N9/96
    • C07D487/16A61K8/4953A61K49/0002A61K49/0004A61K49/0032A61K49/0052A61K51/0459A61Q19/02A61Q19/08C07D487/14
    • Saxitoxin analogue compounds, compositions, pharmaceutical compositions, methods of synthesis of saxitoxin analogues, methods of imaging, methods of treatment, including methods of treating pain, are provided. Saxitoxin (STX), gonyautoxin (GTX), and zetekitoxin, and variant STX compounds bind to sodium channels and are effective to reduce or block flow of sodium ions through such channels. Such channel block affects nerve and muscle action, and may be effective to reduce or block pain sensations, relax muscles, reduce muscle spasm, and reduce wrinkles. STX analogue binding to sodium channels may also be useful to locate, image, or mark sodium channels, and so be useful in studying sodium channels and sodium channel disorders, and in the diagnosis and treatment of patients suffering from sodium channel disorders. In embodiments, the variant STX compounds include conjugates having increased serum half-life as compared to STX when administered to a subject.In embodiments, the present disclosure provides a method for alleviating pain in a subject in need of treatment, the method comprising administering to the subject an effective amount of a saxitoxin analogue compound, or a pharmaceutically acceptable salt, isomer, tautomer or prodrug thereof, whereby pain in said subject is alleviated.
    • 提供了类似萨克西汀类似物,组合物,药物组合物,合成硫氧还蛋白类似物的方法,成像方法,治疗方法,包括治疗疼痛的方法。 沙眼毒素(STX),戈毒毒素(GTX)和泽西酮毒素,和变体STX化合物结合钠通道,并有效减少或阻断钠离子通过这些通道的流动。 这种通道阻滞影响神经和肌肉的作用,并且可以有效地减少或阻止疼痛感觉,放松肌肉,减少肌肉痉挛和减少皱纹。 与钠通道的STX类似物结合也可用于定位,成像或标记钠通道,因此可用于研究钠通道和钠通道障碍,以及用于诊断和治疗患有钠通道障碍的患者。 在实施方案中,变体STX化合物包括与施用于受试者时相比于STX相比具有增加的血清半衰期的结合物。 在实施方案中,本公开提供了一种减轻需要治疗的受试者的疼痛的方法,所述方法包括向受试者施用有效量的沙克西毒素类似物化合物或其药学上可接受的盐,异构体,互变异构体或前药,由此 所述受试者的疼痛缓解。
    • 7. 发明授权
    • Methods and compositions for studying, imaging, and treating pain
    • 用于研究,成像和治疗疼痛的方法和组合物
    • US09174999B2
    • 2015-11-03
    • US12800053
    • 2010-05-07
    • Justin Du BoisJohn MulcahyBrian AndresenDavid C. YeomansSandip Biswal
    • Justin Du BoisJohn MulcahyBrian AndresenDavid C. YeomansSandip Biswal
    • C07D487/14
    • C07D487/16A61K8/4953A61K49/0002A61K49/0004A61K49/0032A61K49/0052A61K51/0459A61Q19/02A61Q19/08C07D487/14
    • Saxitoxin analog compounds, compositions, pharmaceutical compositions, methods of synthesis of saxitoxin analogs, methods of imaging, methods of treatment, including methods of treating pain, are provided. Saxitoxin (STX), gonyautoxin (GTX), and zetekitoxin, and variant STX compounds bind to sodium channels and are effective to reduce or block flow of sodium ions through such channels. Such channel block affects nerve and muscle action, and may be effective to reduce or block pain sensations, relax muscles, reduce muscle spasm, and reduce wrinkles. STX analog binding to sodium channels may also be useful to locate, image, or mark sodium channels, and so be useful in studying sodium channels and sodium channel disorders, and in the diagnosis and treatment of patients suffering from sodium channel disorders. In embodiments, the variant STX compounds include conjugates having increased serum half-life as compared to STX when administered to a subject.In embodiments, the present disclosure provides a method for alleviating pain in a subject in need of treatment, the method comprising administering to the subject an effective amount of a saxitoxin analog compound, or a pharmaceutically acceptable salt, isomer, tautomer or prodrug thereof, whereby pain in said subject is alleviated.
    • 提供萨克西汀类似物,组合物,药物组合物,合成沙星毒素类似物的方法,成像方法,治疗方法,包括治疗疼痛的方法。 沙眼毒素(STX),戈毒毒素(GTX)和泽西酮毒素,和变体STX化合物结合钠通道,并有效减少或阻断钠离子通过这些通道的流动。 这种通道阻滞影响神经和肌肉的作用,并且可以有效地减少或阻止疼痛感觉,放松肌肉,减少肌肉痉挛和减少皱纹。 与钠通道的STX类似物结合也可用于定位,成像或标记钠通道,因此可用于研究钠通道和钠通道障碍,以及用于诊断和治疗患有钠通道障碍的患者。 在实施方案中,变体STX化合物包括与施用于受试者时相比于STX相比具有增加的血清半衰期的结合物。 在实施方案中,本公开提供了一种减轻需要治疗的受试者的疼痛的方法,所述方法包括向受试者施用有效量的沙克西毒素类似物化合物或其药学上可接受的盐,异构体,互变异构体或前药,由此 所述受试者的疼痛缓解。