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    Dolastatin 15 derivatives
    4.
    发明申请
    Dolastatin 15 derivatives 有权
    Dolastatin 15衍生物

    公开(公告)号：US20060270606A1

    公开(公告)日：2006-11-30

    申请号：US11406512

    申请日：2006-04-18

    申请人： Bernd Janssen ,  Teresa Barlozzari ,  Andreas Haupt ,  Thomas Zierke ,  Andreas Kling

    发明人： Bernd Janssen ,  Teresa Barlozzari ,  Andreas Haupt ,  Thomas Zierke ,  Andreas Kling

    IPC分类号： A61K38/08 ,  C07K7/06

    CPC分类号： C07K7/06 ,  A61K38/00 ,  C12P19/34

    摘要： Compounds of the present invention include cell growth inhibitors which are peptides of Formula I, A-B-D-E-F-(G)r-(K)s-L   (I), and acid salts thereof, wherein A, B, D, E, F, G and K are α-amino acid residues, and s and r are each, independently, 0 or 1. L is a monovalent radical, such as, for example, an amino group, an N-substituted amino group, a β-hydroxylamino group, a hydrazido group, an alkoxy group, a thioalkoxy group, an aminoxy group, or an oximato group. The present invention also includes 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I的肽的细胞生长抑制剂，<？in-line-formula description =“In-line Formulas”end =“lead”→> ABDEF-（G）

    Dolastatin 15 derivatives with carbonyl and heterocyclic functionalities at the C-terminus
    5.
    发明授权
    Dolastatin 15 derivatives with carbonyl and heterocyclic functionalities at the C-terminus 失效
    在C-末端具有羰基和杂环官能团的Dolastatin 15衍生物

    公开(公告)号：US5965537A

    公开(公告)日：1999-10-12

    申请号：US814577

    申请日：1997-03-10

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

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

    IPC分类号： A61K38/00 ,  A61P35/00 ,  A61P35/02 ,  C07K5/10 ,  C07K5/103 ,  C07K7/02 ,  C07K5/00

    CPC分类号： C07K5/101 ,  C07K5/1027 ,  C07K7/02 ,  A61K38/00

    摘要： The present invention relates to novel peptides useful as anti-cancer agents. The compounds of the invention are of Formula I,A-B-D-E-F-G (I)A, B, D, and E are .alpha.-amino acid residues. In one embodiment, F is an azacycloalkanecarboxylic acid residue. In this embodiment, G is a monovalent radical, for example, a hydrogen atom, an alkyl group, an aryl group, or a heteroaryl group. In another embodiment, F is an azacycloalkyl group and G is a heteroaryl group connected to F by a carbon-carbon bond.In another embodiment, the invention includes 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： 本发明涉及可用作抗癌剂的新型肽。 本发明的化合物是式I，A-B-D-E-F-G（I）A，B，D和E是α-氨基酸残基。 在一个实施方案中，F是氮杂环烷羧酸残基。 在本实施方案中，G是一价基团，例如氢原子，烷基，芳基或杂芳基。 在另一个实施方案中，F是氮杂环烷基，G是通过碳 - 碳键与F连接的杂芳基。 在另一个实施方案中，本发明包括用于治疗哺乳动物（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。

    Dolastatin 15 derivatives
    6.
    发明授权
    Dolastatin 15 derivatives 有权
    Dolastatin 15衍生物

    公开(公告)号：US07662786B2

    公开(公告)日：2010-02-16

    申请号：US11406512

    申请日：2006-04-18

    申请人： Bernd Janssen ,  Teresa Barlozzari ,  Andreas Haupt ,  Thomas Zierke ,  Andreas Kling

    发明人： Bernd Janssen ,  Teresa Barlozzari ,  Andreas Haupt ,  Thomas Zierke ,  Andreas Kling

    IPC分类号： A61K38/00

    CPC分类号： C07K7/06 ,  A61K38/00 ,  C12P19/34

    摘要： Compounds of the present invention include cell growth inhibitors which are peptides of Formula I, A-B-D-E-F-(G)r-(K)s-L   (I), and acid salts thereof, wherein A, B, D, E, F, G and K are α-amino acid residues, and s and r are each, independently, 0 or 1. L is a monovalent radical, such as, for example, an amino group, an N-substituted amino group, a β-hydroxylamino group, a hydrazido group, an alkoxy group, a thioalkoxy group, an aminoxy group, or an oximato group. The present invention also includes 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I的肽，ABDEF-（G）r-（K）sL（I）及其酸式盐的细胞生长抑制剂，其中A，B，D，E，F，G和K 是α-氨基酸残基，s和r各自独立地为0或1.L为单价基团，例如氨基，N-取代氨基，β-羟基氨基， 酰肼基，烷氧基，硫代烷氧基，氨氧基或肟基。 本发明还包括用于治疗哺乳动物（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。

    Dolastatin 15 derivatives
    8.
    发明授权
    Dolastatin 15 derivatives 有权
    Dolastatin 15衍生物

    公开(公告)号：US07084110B2

    公开(公告)日：2006-08-01

    申请号：US10255118

    申请日：2002-09-25

    申请人： Bernd Janssen ,  Teresa Barlozzari ,  Andreas Haupt ,  Thomas Zierke ,  Andreas Kling

    发明人： Bernd Janssen ,  Teresa Barlozzari ,  Andreas Haupt ,  Thomas Zierke ,  Andreas Kling

    IPC分类号： A61K38/00

    CPC分类号： C07K7/06 ,  A61K38/00 ,  C12P19/34

    摘要： Compounds of the present invention include cell growth inhibitors which are peptides of Formula I, A-B-D-E-F-(G)r-(K)s-L,  (I) and acid salts thereof, wherein A, B, D, E, F, G and K are α-amino acid residues, and s and r are each, independently, 0 or 1. L is a monovalent radical, such as, for example, an amino group, an N-substituted amino group, a β-hydroxylamino group, a hydrazido group, an alkoxy group, a thioalkoxy group, an aminoxy group, or an oximato group. The present invention also includes 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I的肽的细胞生长抑制剂，<？in-line-formula description =“In-line Formulas”end =“lead”→> ABDEF-（G）及其酸式盐，其中A，B D，E，F，G和K是α-氨基酸残基，s和r各自独立地为0或1.L为单价基团，例如氨基，N-取代 氨基，β-羟基氨基，酰肼基，烷氧基，硫代烷氧基，氨氧基或肟基。 本发明还包括用于治疗哺乳动物（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。

    Dolastatin 15 derivatives
    9.
    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。