Abstract: The present invention relates to a compound of following formula (I): or to a pharmaceutically acceptable salt thereof, as well as to pharmaceutical compositions including same and to the use thereof as a drug, in particular for treating a proliferative disease such as cancer.
Type:
Application
Filed:
May 20, 2010
Publication date:
March 29, 2012
Applicants:
CENTRE NATIONAL DE LA RECHERCHE SCIENTIFIQUE (CNRS), PIERRE FABRE MEDICAMENT
Abstract: An object of the present invention is to provide a novel method for producing a steroid compound. The present invention provides a method for producing 3,7-dioxo-5?-cholanic acid or ester derivatives thereof, which uses, as raw materials, sterols having double bonds at positions 5 and 24, such as cholesta-5,7,24-trien-3?-ol, ergosta-5,7,24(28)-trien-3?-ol, desmosterol, fucosterol, or ergosta-5,24(28)-dien-3?-ol, and which comprises the following 4 steps: (I) a step of performing oxidation of a hydroxyl group at position 3 and isomerization of a double bond at position 5 to position 4; (II) a step of converting position 24 to a carboxyl group or an ester derivative thereof by the oxidative cleavage of a side chain; (III) a step of introducing an oxygen functional group into position 7; and (IV) a step of constructing a 5?-configuration by reduction of a double bond at position 4.
Type:
Application
Filed:
June 30, 2010
Publication date:
January 13, 2011
Applicant:
MITSUBISHI CHEMICAL GROUP SCIENCE AND TECHNOLOGY RESEARCH CENTER, INC.
Abstract: It is an object of the present invention to provide a novel method for producing a steroid compound. The present invention provides a method for producing 5?-3,7-dioxocholanic acid or an ester derivative thereof, using, as a raw material, a sterol having double bonds at position 5 and at position 24, such as cholesta-5,7,24-trien-3?-ol, ergosta-5,7,24(28)-trien-3?-ol, desmosterol, fucosterol, or ergosta-5,24(28)-dien-3?-ol, via the following 4 steps: (I) a step involving oxidation of a hydroxyl group at position 3 and isomerization of a double bond at position 5 to position 4; (II) a step involving the oxidative cleavage of a side chain to convert position 24 to a carboxyl group or an ester derivative thereof; (III) a step of introducing an oxygen functional group into position 7; and (IV) a step of constructing a 5? configuration by reductive saturation of a double bond at position 4.
Abstract: It is intended to provide a substance which is efficacious in whitening sun-burnt skin after UV irradiation and preventing, ameliorating and treating skin pigmentation (for example, spots and freckles caused by sunburn, liver spots) and compositions containing the same. Melanogenesis inhibitors and whitening agents comprising an ergosterol derivative represented by formula (1); melanogenesis inhibitors and whitening agents containing the ergosterol derivative represented by the formula (1); melanogenesis inhibitory compositions and whitening compositions containing the ergosterol derivative represented by formula (1); cosmetics, drugs and external skin preparations containing the ergosterol derivative represented by formula (1); and melanogenesis inhibitory foods and whitening foods containing the ergosterol derivative represented by formula (1).
Abstract: 4-amino-unsaturated androstanedione derivatives provided with aromatase inhibitory activity are obtained by hydrolyzation of a corresponding compound of formula II ##STR1##
Type:
Grant
Filed:
May 20, 1992
Date of Patent:
August 31, 1993
Assignee:
Farmitalia Carlo Erba S.R.L.
Inventors:
Fabrizio Orzi, Antonio Longo, Matteo D'Anello, Natale Barbugian