Estra-1,3,5(10)-triene derivatives, process of preparing...

Details Estra-1,3,5(10)-triene derivatives, process of preparing... Estra-1,3,5(10)-triene derivatives, process of preparing...

C - Chemistry, Metallurgy

07

J

C07J 41/00 (2006.01) A61K 31/56 (2006.01) C07J 43/00 (2006.01) C07J 51/00 (2006.01) C07J 53/00 (2006.01)

Patent

CA 2196694

The invention concerns novel estra-1,3,5(10)-triene amidosulphamates with an R- SO2-O- group in the 3-position, R being an R1R2N- group in which R1 and R2, independently of each other, are a hydrogen atom, an alkyl group with 1 to 5 C- atoms or, together with the N-atom, a polymethyleneimino group with 4 to 6 C- atoms or a morpholino group. The compounds described are suitable for use in hormonal contraception and in climacteric hormone-replacement therapy (HRT), as well as in the treatment of gynaecological and andrological conditions. The compounds described thus only have a low hepatic oestrogenicity. Also described are methods of preparing the compounds described, plus the preparation of pharmaceutical compositions containing them.

L'invention concerne de nouveaux estra-1,3,5,(10)-triène-amidosulfamates, qui présentent un groupe R-SO¿2?-O- en position 3, R étant un groupe R?1¿R?2¿N où R?1¿ et R?2¿ désignent indépendamment l'un de l'autre un atome d'hydrogène, un reste alkyle ayant entre 1 et 5 atomes de C ou conjointement avec l'atome de N, un reste polyméthylènimino ayant entre 4 et 6 atomes de C ou un reste morpholino. Ces composés s'utilisent dans la contraception hormonale et dans l'hormonothérapie climatérique de substitution, ainsi que dans le traitement de syndromes gynécologiques et andrologiques. Ces composés ne présentent de ce fait qu'une oestrogénicité hépatique réduite. L'invention concerne en outre des procédés de préparation desdits composés, ainsi que des procédés de préparation de compositions pharmaceutiques les contenant.

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