Protection of endogenous therapeutic peptides from peptidase activity through conjugation to blood components
    12.
    发明授权
    Protection of endogenous therapeutic peptides from peptidase activity through conjugation to blood components 失效
    通过与血液成分缀合,保护内源性治疗肽免受肽酶活性的影响

    公开(公告)号:US07256253B2

    公开(公告)日:2007-08-14

    申请号:US11066697

    申请日:2005-02-25

    IPC分类号: A61K38/00 C07K14/00

    CPC分类号: C07K19/00

    摘要: A secretin or secretin derivative protected against peptidase activity. The secretin or derivative comprises a peptidic sequence and a reactive group selected from the group consisting of succinimidyl and maleimido groups capable of reacting with an amino group, hydroxyl group or thiol group on a blood component to form a stable covalent bond. The reactive group is attached at a position along the peptidic sequence that provides, when conjugated to a blood component, a higher stability against peptidase degradation than the unconjugated secretin or derivative, and therefore an increased maintenance of the therapeutic activity compared to the unconjugated secretin or derivative. Such a compound is thus effective to provide a source of secretin having a high stability against peptidases. A method for synthesizing such a compound is also described.

    摘要翻译: 保护蛋白酶活性的促胰液素或促胰液素衍生物。 分泌素或衍生物包含肽类序列和选自能够与血液成分上的氨基,羟基或硫醇基反应形成稳定的共价键的琥珀酰亚胺基和马来酰亚胺基的反应性基团。 反应性基团连接在沿着肽序列的位置,当与血液成分缀合时,其比非共轭分泌素或衍生物具有比肽酶降解更高的稳定性,因此与未缀合的促胰液素相比,治疗活性的维持得到增加 衍生物。 因此,这样的化合物有效地提供对肽酶具有高稳定性的促胰液素来源。 还描述了合成这种化合物的方法。

    Anti-obesity agents
    15.
    发明授权
    Anti-obesity agents 失效
    抗肥胖剂

    公开(公告)号:US07601691B2

    公开(公告)日:2009-10-13

    申请号:US11067556

    申请日:2005-02-25

    IPC分类号: C07K14/00 A61K38/00

    摘要: The present invention relates to a compound comprising a PYY peptide or a functional derivative thereof, which is coupled to a reactive group. Such a reactive group is capable of reacting on a blood component so as to form a stable covalent bond therewith. The present invention also relates to a conjugate comprising such a compound which is covalently bonded to a blood component. Moreover, the invention also relates to a method of enhancing, in a patient, the anti-obesity activity of a PYY peptide or functional derivative thereof.

    摘要翻译: 本发明涉及包含与反应性基团偶联的PYY肽或其功能性衍生物的化合物。 这样的反应性基团能够对血液成分进行反应,与其形成稳定的共价键。 本发明还涉及包含共价键合到血液成分上的化合物的缀合物。 此外,本发明还涉及在患者中增强PYY肽或其功能性衍生物的抗肥胖活性的方法。

    CYSTEIC ACID DERIVATIVES OF ANTI-VIRAL PEPTIDES
    16.
    发明申请
    CYSTEIC ACID DERIVATIVES OF ANTI-VIRAL PEPTIDES 审中-公开
    抗病毒肽的氨基酸衍生物

    公开(公告)号:US20090088377A1

    公开(公告)日:2009-04-02

    申请号:US12122627

    申请日:2008-05-16

    IPC分类号: A61K38/16 C07K14/00 C07K14/76

    摘要: This invention relates to C34 peptide derivatives having improved aqueous solubility that are inhibitors of viral infection and/or exhibit antifusogenic properties. In particular, this invention relates to C34 derivatives having inhibiting activity against human immunodeficiency virus (HIV), respiratory synctial virus (RSV), human parainfluenza virus (HPV), measles virus (MeV), and simian immunodeficiency virus (SIV) with long duration of action for the treatment of the respective viral infections.

    摘要翻译: 本发明涉及具有改善的水溶性的C34肽衍生物,其是病毒感染的抑制剂和/或表现出抗融合性质。 特别地,本发明涉及具有长期持续时间的针对人类免疫缺陷病毒(HIV),呼吸道合胞病毒(RSV),人副流感病毒(HPV),麻疹病毒(MeV)和猿猴免疫缺陷病毒(SIV))的抑制活性的C34衍生物 的治疗各自病毒感染的作用。

    Affinity markers for human serum albumin
    19.
    发明授权
    Affinity markers for human serum albumin 失效
    人血清白蛋白的亲和标记

    公开(公告)号:US07166695B2

    公开(公告)日:2007-01-23

    申请号:US10934841

    申请日:2004-09-02

    IPC分类号: C07K7/06

    摘要: Methods and compositions are provided for identifying compounds having affinity or complementarity to a target molecule. Compounds according to the invention may be described by the formula E-Ca—R—Cb-A, wherein E is a therapeutic or diagnostic agent, R is a reactive group, Ca and Cb are connector groups between E and R and between R and A, respectively, and A is an affinity group comprising the sequence F-1-Y-E-E. Compounds according to the invention may be used for labeling the target molecule, particularly where the target molecule is naturally found in a complex mixture, such as a physiological fluid, like blood. By affinity labeling in vivo, the lifetime of physiologically active entities can be greatly enhanced by becoming bound to long-lived blood components. The covalently bound entity may also serve as an antagonist or agonist of a particular binding protein or as an enzyme inhibitor.

    摘要翻译: 提供了用于鉴定与靶分子具有亲和力或互补性的化合物的方法和组合物。 根据本发明的化合物可以用下式描述:其中E是治疗剂或诊断剂,R是反应性基团,C < 分别是E和R之间以及R和A之间的连接器组,A是包含序列F-1 -YEE的亲和基团。 根据本发明的化合物可以用于标记靶分子,特别是当目标分子天然存在于复杂混合物如生理液体如血液中时。 通过体内亲和标记,生理活性实体的寿命可以通过与长寿命的血液成分结合而大大增强。 共价结合的实体也可以用作特异性结合蛋白的拮抗剂或激动剂或作为酶抑制剂。