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    • 17. 发明申请
    • Pegylated L-Asparaginase
    • 聚乙二醇化的L-天冬酰胺酶
    • US20120100121A1
    • 2012-04-26
    • US13382276
    • 2010-07-06
    • Thierry Abribat
    • Thierry Abribat
    • A61K38/50A61P35/02C12N9/96A61P35/00
    • C12N9/82A61K38/50A61K47/60C12N9/96C12Y305/01001Y02A50/473
    • Disclosed is a conjugate of a protein having substantial L-asparagine aminohydrolase activity and polyethylene glycol. In particular, the polyethylene glycol has a molecular weight less than or equal to about 5000 Da and the protein is an L-asparaginase from Erwinia. The conjugate of the invention has shown superior properties such as maintenance of a high level of in vitro activity and an unexpected increase in half-life in vivo. Also disclosed are methods of producing the conjugate and use of the conjugate in therapy. In particular, a method is disclosed for use of the conjugate in the treatment of cancer, particularly Acute Lymphoblastic Leukemia (ALL). More specifically, a method is disclosed for use of the conjugate as a second line therapy for patients who have developed hypersensitivity or have had a disease relapse after treatment with other L-asparaginase preparations.
    • 公开了具有大量L-天冬酰胺氨基水解酶活性的蛋白质和聚乙二醇的缀合物。 特别地,聚乙二醇具有小于或等于约5000Da的分子量,蛋白质是来自欧文氏菌的L-天冬酰胺酶。 本发明的缀合物显示出优异的性质,例如保持高水平的体外活性和体内半衰期的意想不到的增加。 还公开了在治疗中产生缀合物和缀合物的用途的方法。 特别地,公开了用于结合物治疗癌症,特别是急性淋巴细胞性白血病(ALL)的方法。 更具体地说,公开了一种使用缀合物作为二次线治疗患者的方法,该方法已经发展为超敏反应,或者在用其它L-天冬酰胺酶制剂处理后已经发生疾病复发。
    • 18. 发明授权
    • Modified GLP-1 peptides with increased biological potency
    • 具有增加的生物效能的修饰的GLP-1肽
    • US07067488B2
    • 2006-06-27
    • US10671340
    • 2003-09-25
    • Denis GravelKrishna PeriThierry AbribatAbdelkrim Habi
    • Denis GravelKrishna PeriThierry AbribatAbdelkrim Habi
    • A61K38/22C07K14/575
    • C07K14/605A61K38/26
    • The present invention relates to a GLP-1 peptide having the following formula, or a pharmaceutically acceptable salt thereof: X-His-Ala-Glu-Gly-Thr-Phe-Thr-Ser-Asp-Val-Ser-Ser-Tyr-Leu-Glu-Gly-Gln-Ala-Ala-Lys-Glu-Phe-lle-Ala-Trp-Leu-val-Lys-Gly-Arg-Y (SEQ ID NO. 1) wherein X is a rigidifying hydrophobic moiety and wherein Y is selected from the group consisting of OH, NH2 and Gly-OH. Moreover, the present invention relates to pharmaceutical compositions comprising a therapeutically effective amount of a peptide of the present invention, or a pharmaceutically acceptable salt thereof, in association with at least one constituent selected from a pharmaceutically acceptable carrier, diluent, and excipient.
    • 本发明涉及具有下式的GLP-1肽或其药学上可接受的盐:<?in-line-formula description =“In-line formula”end =“lead”?> X-His-Ala- Glu-Gly-Thr-Phe-Thr-Ser-Asp-Val-Ser-Ser-Tyr-Leu-Glu-Gly-Gln-Ala-Ala-Lys-Glu-Phe-Ala-Ala-Trp-Leu-val- Lys-Gly-Arg-Y(SEQ ID NO.1)<?in-line-formula description =“In-line Formulas”end =“tail”?>其中X是刚性疏水部分,其中Y选自 由OH,NH 2和Gly-OH组成的组。 此外,本发明涉及包含治疗有效量的本发明的肽或其药学上可接受的盐与至少一种选自药学上可接受的载体,稀释剂和赋形剂的成分的药物组合物。