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Title:
改質されたレチノイド化合物及びその使用
Document Type and Number:
Japanese Patent JP4699347
Kind Code:
B2
Abstract:
A method of minimizing or reducing the toxicity of a retinoid having a free carboxyl group and the resulting modified retinoids are described. The method comprises the step of esterifying the carboxyl group of the retinoid with a highly sterically hindered compound, which is preferably a secondary or tertiary alcohol. The resulting retinoid esters are rendered much less toxic than the starting or parent retinoid. This process provides a retinoid ester analog of reduced toxicity so that it may be administered orally with minimal side effects and with a much greater therapeutic window. The modified retinoid compounds are useful in the treatment and prophylaxis of all diseases and disorders where retinoid compounds have been shown effective.

Inventors:
Deluca, Hector Ef
Krugetto-Dahme, Margaret
Goulgari, Smithra
Application Number:
JP2006501027A
Publication Date:
June 08, 2011
Filing Date:
January 16, 2004
Export Citation:
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Assignee:
WISCONSIN ALUMNI RESEARCH FOUNDATION
International Classes:
C07C403/20; A61K8/67; A61K31/203; A61K31/215; A61K31/575; A61P17/00; A61P17/06; A61P17/10; A61P35/00; A61P35/02; A61Q19/00; A61Q19/08; C07C69/76; C07J9/00
Domestic Patent References:
JP9012538A
JP5505401A
JP5025123A
JP1156921A
JP56075424A
JP3500643A
JP50076048A
JP50076047A
JP5502243A
JP51110551A
Foreign References:
WO1998006390A1
Other References:
European Journal of Pharmaceutical Sciences,1995年,3(2),p.71-76
Attorney, Agent or Firm:
Kazuo Shamoto
Tadashi Masui
Yasushi Kobayashi
Akio Chiba
Hiroyuki Tomita
Hiroko Ejiri