3-substituted-d-homo-1,3,5,(10)-estratriene derivatives

C - Chemistry – Metallurgy – 07 – J

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C07J 73/00 (2006.01) A61K 31/56 (2006.01)

Patent

CA 2266051

Because of having excellent estrone sulfatase inhibitory effects, estratriene derivatives represented by general formula (I) are useful in the prevention and treatment of diseases caused by estrogens such as mammary cancer, uterus cancer, ovarian cancer, endometriosis, uterine adenomyosis and mastopathy, wherein one of A and B represents C=O or CH2 while another represents O or NH; and R represents -SO2NR1R2 or -PO(OM)2 (wherein R1 and R2 each independently represent hydrogen or lower alkyl and M represents hydrogen or an alkali metal), provided that when one of A and B is NH, then another is C=O.

Possédant une remarquable action inhibitrice vis-à-vis de l'oestrone sulfatase, les dérivés d'oestrariène, représentés par la formule générale suivante (I), se révèlent des plus utiles dans la prévention et le traitement d'états pathologiques occasionnés par des oestrogènes, notamment les cancers du sein, de l'utérus et des ovaires, l'endométriose, l'adénomyose utérine et les mastopathies. Dans la formule (I), A ou B représente C=O ou CH¿2?, l'autre représentant alors O ou NH tandis que R représente -SO¿2?NR?1¿R?2¿ ou -PO(OM)¿2? (R?1¿ et R?2¿ représentant chacun, de manière indépendante, un hydrogène ou un alkyle de faible poids moléculaire et M représentant un hydrogène ou un métal alcalin) et ce, à la condition que lorsque A ou B représente NH, l'autre représente C=O.

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