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    COMPOSITIONS AND METHODS FOR TREATING ACUTE AND CHRONIC PAIN BY LOCAL ANTAGONISM OF CGRP RECEPTORS, OR COMBINATION WITH SODIUM CHANNEL INHIBITION OR WITH ANTI-INFLAMMATORY AGENTS
    4.
    发明申请
    COMPOSITIONS AND METHODS FOR TREATING ACUTE AND CHRONIC PAIN BY LOCAL ANTAGONISM OF CGRP RECEPTORS, OR COMBINATION WITH SODIUM CHANNEL INHIBITION OR WITH ANTI-INFLAMMATORY AGENTS 审中-公开
    用于通过CGRP受体的局部拮抗剂治疗急性和慢性疼痛的组合物和方法，或与钠通道抑制剂或抗炎药物组合

    公开(公告)号：US20160347810A1

    公开(公告)日：2016-12-01

    申请号：US14727589

    申请日：2015-06-01

    申请人： AfaSci, Inc.

    发明人： Xinmin Xie ,  Conrado Pascual ,  Xi Xie ,  James Xie

    IPC分类号： C07K14/575 ,  A61K45/06 ,  A61K38/23 ,  A61K9/00

    CPC分类号： C07K14/57527 ,  A61K9/0021 ,  A61K38/00 ,  A61K38/10 ,  A61K38/23 ,  A61K45/06 ,  C07K7/08 ,  C07K14/723

    摘要： The present invention provides compositions, and methods for local administration of certain peptides or combination with certain small molecules that produce analgesia and anti-inflammation in a mammal. Exemplary polypeptides provide peripheral analgesia and anti-inflammation when administered via local topical, subcutaneous, intradermal, or intranasal administration, to provide analgesia and anti-inflammation. Through antagonism of peripheral CGRP receptors alone, or in combination with inhibition of sensory sodium channels or anti-inflammation, the compositions of the invention provide local therapeutic pain relief with minimal undesired systemic side effects in a subject. Also provided are improved peptide delivery techniques including microneedle unit dose administering apparatus and methods. Also provided are hydrogel formulations for sustained local delivery to a subject of one or more of the compositions according to the invention in a therapeutically effective amount, thereby providing local pain relief and/or reducing associated inflammation.

    摘要翻译： 本发明提供了用于局部施用某些肽或与在哺乳动物中产生镇痛和抗炎的某些小分子组合的组合物和方法。 当通过局部局部，皮下，皮内或鼻内给药施用时，示例性多肽提供外周镇痛和抗炎，以提供镇痛和抗炎。 通过单独的外周CGRP受体的拮抗作用，或与抑制感觉钠通道或抗炎症的组合，本发明的组合物提供局部治疗性疼痛缓解，并且在受试者中具有最少的不期望的全身副作用。 还提供了改进的肽递送技术，包括微针单位剂量给药装置和方法。 还提供了用于以治疗有效量持续地局部递送至本发明组合物的一种或多种组合物的水凝胶制剂，从而提供局部疼痛缓解和/或减少相关的炎症。

    PEPTIDE ANTAGONISTS OF THE CALCITONIN CGRP FAMILY OF PEPTIDE HORMONES AND THEIR USE
    9.
    发明申请
    PEPTIDE ANTAGONISTS OF THE CALCITONIN CGRP FAMILY OF PEPTIDE HORMONES AND THEIR USE 有权
    肽激素CGRP家族肽肽拮抗剂及其使用

    公开(公告)号：US20140329752A1

    公开(公告)日：2014-11-06

    申请号：US13821936

    申请日：2013-01-25

    申请人： Christopher J. Soares

    发明人： Christopher J. Soares

    IPC分类号： C07K14/575

    CPC分类号： C07K14/57527 ,  A61K38/00 ,  A61K38/225 ,  A61K38/23 ,  C07K14/585

    摘要： The embodiments provide a modified calcitonin gene-related peptide antagonist including an N-terminal fragment of modified calcitonin gene-related peptide or related protein family member where at least two residues of the N-terminal fragment are cysteine (Cys) and at least one amino acid comprises a non-threonine substitution of a threonine (Thr) residue; a central core where the central core comprises an oc-helix; and a C-terminal fragment of modified calcitonin gene-related peptide or related protein family member comprising a C-terminal amide and where at least one amino acid of the C-terminal fragment is phenylalanine (Phe), proline (Pro), tyrosine (Tyr) or hydroxyproline (Hyp) or pharmaceutically acceptable salt thereof, as well as compositions, including pharmaceutical compositions, comprising a subject peptide. The embodiments further provide treatment methods, including methods of treating a migraine, the methods generally involving administering to an individual in need thereof an effective amount of a subject peptide or composition.

    摘要翻译： 实施方案提供了修饰的降钙素基因相关肽拮抗剂，其包括修饰的降钙素基因相关肽或相关蛋白家族成员的N末端片段，其中N-末端片段的至少两个残基是半胱氨酸（Cys）和至少一个氨基 酸包括苏氨酸（Thr）残基的非苏氨酸取代; 中心芯，其中心芯包含α-螺旋; 和包含C-末端酰胺的修饰的降钙素基因相关肽或相关蛋白家族成员的C末端片段，其中C-末端片段的至少一个氨基酸是苯丙氨酸（Phe），脯氨酸（Pro），酪氨酸（ Tyr）或羟脯氨酸（Hyp）或其药学上可接受的盐，以及包含受试肽的组合物，包括药物组合物。 实施方案进一步提供治疗方法，包括治疗偏头痛的方法，所述方法通常涉及向有需要的个体施用有效量的受试肽或组合物。