Title:
STILBENE DERIVATIVE AND CARCINOSTATIC AGENT CONTAINING THE SAME
Document Type and Number:
Japanese Patent JP3163391
Kind Code:
B2
Abstract:
PURPOSE: To obtain a readily synthesized combretastatin derivative useful as a carcinostatic agent having low toxicity and high therapeutic effects.
CONSTITUTION: This stilbene derivative of formula I (X is H or nitrile; Y is an L-α-amino acid acyl), e.g. (Z)-1-(3-amino-4-methoxyphenyl)-2(3,4,5- trimethoxyphenyl)-ethene-glycinamide. The derivative of formula I is obtained by reacting (Z)-1-(3-amino-4-methoxyphenyl)2-(3,4,5-trimethoxyphenyl)-ethene of formula II with an N-α-9-fluorenylmethoxycarbonylamino acid derivative of formula III (Fmoc is N-α-9-fluorenylmethoxycarbonyl; AA is an amino acid acyl) in the presence of dicyclohexylcarbodiimide and 1-hydroxybenzotriazole in dimethylformamide at ambient temperature for 6-12hr, purifying the resultant compound and then deprotecting the purified compound with aqueous sodium hydroxide. The compound of formula I as a carcinostatic agent is usually used in a dose of 1-3000mg for an adult and daily 1-9000mg divided into several portions.
Inventors:
Toshihiro Hatanaka
Koji Ohsumi
Hisashi Tsuji
Yukio Nihei
Ryusuke Nakagawa
Kazuo Ohishi
Koji Ohsumi
Hisashi Tsuji
Yukio Nihei
Ryusuke Nakagawa
Kazuo Ohishi
Application Number:
JP7087696A
Publication Date:
May 08, 2001
Filing Date:
March 04, 1996
Export Citation:
Assignee:
AJINOMOTO CO.,LTD.
International Classes:
C07D207/16; A61K31/165; A61K31/167; A61K31/275; A61K31/277; A61K31/40; A61K31/401; A61P35/00; C07C231/12; C07C237/04; C07C255/44; (IPC1-7): C07C237/04; A61K31/167; A61P35/00; C07C255/44; C07D207/16
Domestic Patent References:
| JP7228558A |
Attorney, Agent or Firm:
Hiroshi Nakamoto (2 outside)
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