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    • 1. 发明公开
    • PEPTIDE ANTAGONISTS OF THE CALCITONIN CGRP FAMILY OF PEPTIDE HORMONES AND THEIR USE
    • PEPTIDANTAGONISTEN AUS DER CALCITONIN-CGRP-FAMILIE VON PEPTIDHORMONEN UND DEREN VERWENDUNG
    • EP2807187A1
    • 2014-12-03
    • EP13703494.8
    • 2013-01-25
    • Soares, Christopher, J.
    • Soares, Christopher, J.
    • C07K14/585A61K38/22
    • C07K14/57527A61K38/00A61K38/225A61K38/23C07K14/585
    • 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.
    • 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(Pro 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。
    • 10. 发明专利
    • Antagonistas peptídicos de la familia calcitonina CGRP de hormonas peptídicas y su uso
    • ES2819825T3
    • 2021-04-19
    • ES17175988
    • 2013-01-25
    • SOARES CHRISTOPHER J
    • SOARES CHRISTOPHER
    • C07K14/585A61K38/00A61K38/22A61K38/23C07K14/575
    • Un antagonista del péptido relacionado con el gen de la calcitonina, o una sal farmacéuticamente aceptable del mismo, teniendo dicho antagonista la estructura de Fórmula I: X1-Y1-Z1 (I) en donde: X1 es X11-X12-X13-X14-X15-X16-X17 (SEQ ID NO: 16), en donde X11 se selecciona del grupo que consiste en Ala, Cys y Gly, y X12 se selecciona del grupo que consiste en Cys y Ser, siempre que uno de X11 y X12 sea Cys, X13 se selecciona del grupo que consiste en Arg, Asn, Asp y Val, X14 se selecciona del grupo que consiste en Leu, Phe y Thr, X15 se selecciona del grupo que consiste en Ala, Gly y Ser, X16 se selecciona del grupo que consiste en Ala, Ile, Leu, Ser y Val, y X17 es Cys; y Y1 se selecciona del grupo que consiste en -Val-Leu-Gly-Arg-Leu-Ser-Gln-Glu-Leu-His-Arg-Leu-Gln-Thr-Tyr-Pro- Arg-Thr-Asn-(SEQ ID NO: 34), -Val-Leu-Gly-Lys-Leu-Ser-Gln-Glu-Leu-His-Lys-Leu-Gln-Thr-Tyr-Pro-Arg-Thr-Asn- (SEQ ID NO: 35), -Val-Leu-Gly-Lys-Leu-Ser-Gln-Glu-Leu-His-Lys-Leu-Gln-Thr-Tyr-Pro-Arg-Thr-Asp-(SEQ ID NO: 37), -Val-Leu-Gly-Lys-Leu-Ser-Gln-Glu-Leu-His-Lys-Leu-Gln-Thr-Phe-Pro-Arg-Thr-Asn-(SEQ ID NO: 38), -Val- Leu-Gly-Lys-Leu-Ser-Gln-Asp-Ile-His-Lys-Leu-Gln-Thr-Tyr-Pro-Arg-Thr-Asn-(SEQ ID NO: 39), -Val-Leu-Gly-Lys- Leu-Ser-Gln-Glu-Leu-His-Lys-Met-Gln-Thr-Tyr-Pro-Arg-Thr-Asp (SEQ ID NO: 40), -Leu-Leu-Gly-Lys-Leu-Ser-Gln- Glu-Leu-His-Arg-Leu-Gln-Thr-Tyr-Thr-Arg-Thr-Asp-(SEQ ID NO: 41), -Val-Leu-Gly-Lys-Leu-Ser-Gln-Asp-Leu-His- Lys-Leu-Gln-Thr-Phe-Pro-Arg-Thr-Asp-(SEQ ID NO: 42), -Met-Leu-Gly-Lys-Leu-Ser-Gln-Asp-Leu-His-Lys-Leu- Gln-Thr-Phe-Pro-Arg-Thr-Asp-(SEQ ID NO: 43) y -Val-Leu-Gly-Lys-Leu-Ser-Gln-Asp-Ile-His-Lys-Leu-Gln-Thr-His- Pro-Arg-Thr-Asp-(SEQ ID NO: 44); y Z1 es Val-Gly-Ser-Lys-Ala-Phe-NH2.