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    • 2. 发明申请
    • Modified Corticotropin Releasing Factor Peptides and Uses Thereof
    • 改性促肾上腺皮质激素释放因子肽及其用途
    • US20080167231A1
    • 2008-07-10
    • US11873291
    • 2007-10-16
    • Thomas R. UlichJean-Philippe EstradierKaren Thibaudeau
    • Thomas R. UlichJean-Philippe EstradierKaren Thibaudeau
    • A61K38/00C07K16/00
    • C07K14/57509A61K38/00A61K47/64A61K47/643A61K47/644A61K47/6889
    • The present invention relates to compounds comprising modified corticotrophin releasing factor peptide and specifically urocortin and urocortin-related peptides, modified derivatives thereof, and conjugates of such modified peptides and derivatives to serum components, preferably serum proteins or peptides. The compounds and conjugates of the invention comprise a reactive group, which is covalently attached to a modified peptide or derivative, optionally through a linking group. The present invention also provides methods for the covalent attachment of a modified peptide or derivative to a serum protein or peptide to form a conjugate of the invention. The conjugates of the invention preferably exhibit a longer in vivo circulating half-life compared to the corresponding unconjugated peptides. The conjugates of the invention also retain at least some of the biological activity of the unconjugated peptides, and preferably exhibit increased biological activity compared to the unconjugated peptides. The present invention also provides methods for the treatment and prevention of a disease or disorder comprising the administration of one or more of the compounds or conjugates of the invention to a subject in need of such treatment or prevention.
    • 本发明涉及包含修饰的促肾上腺皮质激素释放因子肽,特别是尿皮质素和尿皮质素相关肽,其修饰的衍生物,以及这些修饰肽和衍生物与血清成分,优选血清蛋白或肽的缀合物的化合物。 本发明的化合物和缀合物包含反应性基团,其任选地通过连接基团共价连接到修饰的肽或衍生物上。 本发明还提供了将修饰的肽或衍生物共价连接到血清蛋白或肽以形成本发明的缀合物的方法。 与相应的未结合的肽相比,本发明的缀合物优选表现出更长的体内循环半衰期。 本发明的缀合物还保留非共轭肽的至少一些生物活性,并且与非共轭多肽相比优​​选表现出增加的生物学活性。 本发明还提供了治疗和预防疾病或病症的方法,包括将本发明的一种或多种化合物或缀合物施用于需要这种治疗或预​​防的受试者。
    • 4. 发明授权
    • Modified corticotropin releasing factor peptides and uses thereof
    • 修饰的促肾上腺皮质激素释放因子肽及其用途
    • US07982018B2
    • 2011-07-19
    • US11873291
    • 2007-10-16
    • Thomas R. UlichJean-Philippe EstradierKaren Thibaudeau
    • Thomas R. UlichJean-Philippe EstradierKaren Thibaudeau
    • A61K38/35A61K38/38C07K14/695C07K14/76C07K14/765
    • C07K14/57509A61K38/00A61K47/64A61K47/643A61K47/644A61K47/6889
    • The present invention relates to compounds comprising modified corticotrophin releasing factor peptide and specifically urocortin and urocortin-related peptides, modified derivatives thereof, and conjugates of such modified peptides and derivatives to serum components, preferably serum proteins or peptides. The compounds and conjugates of the invention comprise a reactive group, which is covalently attached to a modified peptide or derivative, optionally through a linking group. The present invention also provides methods for the covalent attachment of a modified peptide or derivative to a serum protein or peptide to form a conjugate of the invention. The conjugates of the invention preferably exhibit a longer in vivo circulating half-life compared to the corresponding unconjugated peptides. The conjugates of the invention also retain at least some of the biological activity of the unconjugated peptides, and preferably exhibit increased biological activity compared to the unconjugated peptides. The present invention also provides methods for the treatment and prevention of a disease or disorder comprising the administration of one or more of the compounds or conjugates of the invention to a subject in need of such treatment or prevention.
    • 本发明涉及包含修饰的促肾上腺皮质激素释放因子肽,特别是尿皮质素和尿皮质素相关肽,其修饰的衍生物,以及这些修饰肽和衍生物与血清成分,优选血清蛋白或肽的缀合物的化合物。 本发明的化合物和缀合物包含反应性基团,其任选地通过连接基团共价连接到修饰的肽或衍生物上。 本发明还提供了将修饰的肽或衍生物共价连接到血清蛋白或肽以形成本发明的缀合物的方法。 与相应的未结合的肽相比,本发明的缀合物优选表现出更长的体内循环半衰期。 本发明的缀合物还保留非共轭肽的至少一些生物活性,并且与非共轭多肽相比优​​选表现出增加的生物学活性。 本发明还提供了治疗和预防疾病或病症的方法,包括将本发明的一种或多种化合物或缀合物施用于需要这种治疗或预​​防的受试者。