Title:
【発明の名称】抗腫瘍剤としてのドラスタチンのテトラペプチド誘導体
Document Type and Number:
Japanese Patent JP2002512590
Kind Code:
A
Abstract:
The present invention provides anti-tumor peptides of Formula I,A-B-NR3-CHD-CH(OCH3)-CH2CO-E-K(I),and the acid salts thereof. A is an amino acid residue selected from the group consisting of N-methyl-D-prolyl, N-methyl-D-homoprolyl and N,N-dimethyl-2-ethylphenylglycyl, or an amino acid residue of the formula R1R2N-CHX-CO, wherein R1 is a-methyl group or an ethyl group, R2 is a hydrogen atom, a methyl group or an ethyl group, and X is an alkyl group. B is an amino acid residue selected from the group consisting of valyl, isoleucyl, leucyl, and 2-t-butylglycyl. R3 is a hydrogen atom or a methyl group. D is a normal or branched C2-C5-alkyl group. E is an amino acid residue selected from the group consisting of prolyl, homoprolyl, 5-methylprolyl, and phenylalanyl, or E is a residue derived from an amino acid comprising a pyrrolidine group. K is an alkoxy group or an amino group. An additional embodiment of the present invention is a method for treating a malignancy in a mammal, such as a human, comprising administering to the mammal an effective amount of a compound or compounds of Formula I in a pharmaceutically acceptable composition.
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Inventors:
Teresa Burrosa Lee
Andreas Haupt
Bernd Janssen
Christian Griesinger
Daniel Berryk
Michael Boletsky
Andreas Haupt
Bernd Janssen
Christian Griesinger
Daniel Berryk
Michael Boletsky
Application Number:
JP50845798A
Publication Date:
April 23, 2002
Filing Date:
July 21, 1997
Export Citation:
Assignee:
BASF Akchen Gezel Shaft
International Classes:
A61K38/00; A61P35/00; C07K4/00; C07K5/02; (IPC1-7): C07K4/00; A61K38/00; A61P35/00
Attorney, Agent or Firm:
Toshio Yano (2 outside)