Antagonistic peptides of prostaglandin E2 receptor subtype EP4
    1.
    发明申请
    Antagonistic peptides of prostaglandin E2 receptor subtype EP4 失效
    前列腺素E2受体亚型EP4拮抗肽

    公开(公告)号:US20050164949A1

    公开(公告)日:2005-07-28

    申请号:US10968872

    申请日:2004-10-19

    IPC分类号: A61K38/00 C07K7/06 A61K38/08

    摘要: Antagonistic peptides of prostaglandin E2 receptor subtype EP4 and their use in the treatment or prevention of medical conditions associated with oligouric nephropathy, bone resorption, abnormal intestinal crypt cell proliferation or patency of the ductus arteriosus and the like are provided herein. The antagonistic peptides of the present invention can include the following formula: X-ARnYm wherein “X” is a hydrogen atom or an amine protecting group producing a carbamate or an amide when reacting with the amine; “A” is L-(4,4′)-biphenylalanine or D-(4,4′)-biphenylalanine; “R” is an amino acid selected from the group consisting of threonine, serine, tyrosine, glutamic acid, alanine, leucine and glycine; “Y” is lysine; “n” is an integer ranging from 5 to 7; and “m” is an integer ranging from 0 to 2.

    摘要翻译: 前列腺素E2受体亚型EP4的拮抗肽及其在治疗或预防与寡尿性肾病相关的医学病症,骨吸收,动脉导管未闭的肠道隐窝细胞增殖或通畅等中的用途。 本发明的拮抗肽可以包括下列公式:<?in-line-formula description =“In-line Formulas”end =“lead”?>XAR > m <?in-line-formula description =“In-line Formulas”end =“tail”?>其中“X”是氢原子,或当产生氨基甲酸酯或酰胺的胺保护基与 胺; “A”是L-(4,4') - 联苯基丙氨酸或D-(4,4') - 联苯基丙氨酸; “R”是选自苏氨酸,丝氨酸,酪氨酸,谷氨酸,丙氨酸,亮氨酸和甘氨酸的氨基酸; “Y”是赖氨酸; “n”为5〜7的整数; “m”为0〜2的整数。

    Glucagon-like peptide-1 analogs with long duration of action
    5.
    发明授权
    Glucagon-like peptide-1 analogs with long duration of action 失效
    具有长期作用的胰高血糖素样肽-1类似物

    公开(公告)号:US07538185B2

    公开(公告)日:2009-05-26

    申请号:US11031851

    申请日:2005-01-07

    IPC分类号: A61K38/26

    CPC分类号: C07K14/605 A61K38/26

    摘要: Novel GLP-1 analogs having improved biological potency as well as extended pharmacological activity are described herein. More specifically, the present invention relates to GLP-1 analogs (28 or 29 aa long) comprising amino acid substitutions at one or more of the following positions: 8, 20, 27, 30 and 33.

    摘要翻译: 本文描述了具有改善的生物学效力以及延长的药理活性的新型GLP-1类似物。 更具体地说,本发明涉及在一个或多个以下位置上包含氨基酸取代的GLP-1类似物(28或29a a long):8,20,27,30和33。

    Compounds that modulate the glucagon response and uses thereof
    6.
    发明申请
    Compounds that modulate the glucagon response and uses thereof 审中-公开
    调节胰高血糖素反应的化合物及其用途

    公开(公告)号:US20050124550A1

    公开(公告)日:2005-06-09

    申请号:US10871885

    申请日:2004-06-18

    申请人: Krishna Peri

    发明人: Krishna Peri

    CPC分类号: C07K7/06 C07K14/723

    摘要: Peptides that modulate the glucagon response in a mammal are provided. The peptides comprise an amino acid sequence of between about 5 and about 10 amino acids in length that corresponds to the sequence of an extracellular membrane insertion region of a mammalian glucagon receptor, wherein at least one amino acid of the peptide has a D-configuration. Methods of preparing the peptides and the use of the peptides in the amelioration, treatment and/or prevention of glucagon-mediated conditions and diseases such as hyperglycemia, diabetes and obesity are also provided.

    摘要翻译: 提供调节哺乳动物胰高血糖素反应的肽。 所述肽包括长度为约5至约10个氨基酸的氨基酸序列,其对应于哺乳动物胰高血糖素受体的细胞外膜插入区的序列,其中该肽的至少一个氨基酸具有D-构型。 还提供了制备肽的方法和肽在改善,治疗和/或预防胰高血糖素介导的病症和疾病如高血糖,糖尿病和肥胖中的用途。