Title:
エピポドフィロトキシンの(ポリ)アミノアルキルアミノアセトアミド誘導体、その調製方法及び諸療法における抗癌剤としてのその応用
Document Type and Number:
Japanese Patent JP2007532628
Kind Code:
A
Abstract:
Aminoacetamido epipodophyllotoxin derivatives (I) are new. Aminoacetamido epipodophyllotoxin derivatives of formula (I) and their salts are new: R 1, R 2H or Me; R3, A : H, 1-4C alkyl or benzyl, or A is (CH 2) aNR4B, or R3+A forms a 3-8C ring; a : 2-5; R4, B : H, 1-4C alkyl or benzyl, or B is (CH 2) bNR5(CH 2) cNR6R7 or (CH 2) cNR8R9, or R4+B forms a 3-8C ring; b, c : 2-5; R5-R7 : H, 1-4C alkyl or benzyl; R8, R9 : H or 1-5C alkyl, or together form a 3-8C ring or 4- to 8-membered heterocycle; R3+R4, R4+R5, R5+R6, R6+R7, R4+R8 : can also be 2-3C alkylene. An independent claim is also included for a process for preparing (I). [Image] ACTIVITY : Cytostatic. 2-(2-Dimethylaminoethylamino)-N-(9-(4-hydroxy-3,5-dimethoxyphenyl)-8-oxo-5,5a,6,8,8a,9-hexahydro-furo[3',4':6,7]naphtho[2,3-d][1,3]dioxol-5-yl)acetamide gave a 57% increase in survival time at a dose of 10 mg/kg in mice with P388 leukemia. MECHANISM OF ACTION : None given.
Inventors:
Amber, Thierry
Guminski, Eve
Barre, Jean-Marc
Anna Kryukzinki
Guminski, Eve
Barre, Jean-Marc
Anna Kryukzinki
Application Number:
JP2007507869A
Publication Date:
November 15, 2007
Filing Date:
April 14, 2005
Export Citation:
Assignee:
PIERRE FABRE MEDICAMENT
International Classes:
C07D493/04; A61K31/337; A61K31/343; A61K31/4375; A61K31/4525; A61K31/496; A61K31/513; A61K31/5377; A61K33/24; A61K45/00; A61P35/00; A61P35/02; A61P43/00
Attorney, Agent or Firm:
Keiichi Ota