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    Dolastatin 15 derivatives
    31.
    发明授权
    Dolastatin 15 derivatives 失效
    Dolastatin 15衍生物

    公开(公告)号：US5985837A

    公开(公告)日：1999-11-16

    申请号：US112249

    申请日：1998-07-08

    申请人： Kurt Ritter ,  Bernd Janssen ,  Andreas Haupt ,  Andreas Kling ,  Teresa Barlozzari ,  Wilhelm Amberg

    发明人： Kurt Ritter ,  Bernd Janssen ,  Andreas Haupt ,  Andreas Kling ,  Teresa Barlozzari ,  Wilhelm Amberg

    IPC分类号： A61K38/00 ,  A61K35/56 ,  A61P35/00 ,  C07K5/103 ,  C07K5/117 ,  C07K7/02 ,  A61K38/04 ,  A61K38/07 ,  A61K38/08 ,  C07K7/04

    CPC分类号： C07K7/02 ,  C07K5/101 ,  C07K5/1024 ,  A61K38/00

    摘要： Compounds of the present invention include cell growth inhibitors which are peptides of Formula IA--B--D--E--F--G (I)and acid salts thereof, wherein A, D, and E are .alpha.-amino acid residues, B is an .alpha.-amino acid residue or an .alpha.-hydroxy acid residue, F is an aminobenzoic acid residue or an aminocycloalkanecarboxylic acid residue, and G is a monovalent radical, such as, for example, a hydrogen atom, an amino group, an alkyl group, an alkylene alkyl ether, an alkylene alkyl thioether, an alkylene aldehyde, an alkylene amide, a .beta.-hydroxylamino group, a hydrazido group, an alkoxy group, a thioalkoxy group, an aminoxy group, an oximato group, an alkylene aryl group, an alkylene ester, an alkylene sulfoxide or an alkylene sulfone. Another aspect of the present invention includes pharmaceutical compositions comprising a compound of Formula I and a pharmaceutically acceptable carrier. An additional embodiment of the present invention is a method for treating cancer in a mammal, such as a human, comprising administering to the mammal an effective amount of a compound of Formula I in a pharmaceutically acceptable composition.

    摘要翻译： 本发明的化合物包括作为式IA-BDEFG（I）的肽及其酸式盐的细胞生长抑制剂，其中A，D和E是α-氨基酸残基，B是α-氨基酸残基或α - 羟酸残基，F是氨基苯甲酸残基或氨基环烷烃羧酸残基，G是一价基团，例如氢原子，氨基，烷基，亚烷基烷基醚，亚烷基烷基 硫醚，亚烷基醛，亚烷基酰胺，β-羟基氨基，酰肼基，烷氧基，硫代烷氧基，氨氧基，肟基，亚烷基芳基，亚烷基酯，亚烷基亚砜或 亚砜。 本发明的另一方面包括包含式I化合物和药学上可接受的载体的药物组合物。 本发明的另一个实施方案是用于治疗哺乳动物（例如人）中的癌症的方法，包括向所述哺乳动物施用有效量的药学上可接受的组合物中的式I化合物。