Phenyl sulfamate derivatives

Details Phenyl sulfamate derivatives Phenyl sulfamate derivatives

C - Chemistry, Metallurgy

07

C

C07C 307/02 (2006.01) A61K 31/165 (2006.01) A61K 31/18 (2006.01) A61K 31/4196 (2006.01) A61P 15/00 (2006.01) A61P 25/28 (2006.01) A61P 35/00 (2006.01) A61P 37/06 (2006.01) C07D 249/08 (2006.01)

Patent

CA 2377803

Phenyl sulfamate derivatives represented by the following formula or salts thereof have a powerful inhibitory effect on steroid sulfatase and are hence useful for the prophylaxis or treatment of diseases associated with steroids such as estrogens, such as breast cancer, corpus uteri cancer, endometrial hyperplasia, infertility, endometriosis, adenomyosis uteri, autoimmune disease, dementia or Alzheimer's disease. (see formula I) wherein R1 and R2 each independently represent a hydrogen atom or a lower alkyl group; R3 represents a hydrogen atom, a halogen atom, a lower alkyl group, -OSO2NR1R2, a lower alkanoylamino group, a nitro group or a cyano group; and A represents a substituted or unsubstituted phenyl group, a group of the formula -X-NR4R5, or the like.

L'invention concerne des dérivés phényl-sulfamates représentés par la formule générale (I) ci-après, ou des sels desdits dérivés, qui présentent une excellente activité inhibitrice vis-à-vis de la stéroïde sulfatase et qui sont donc efficaces en matière de prévention et de traitement des maladies associées aux stéroïdes hormonaux dont les oestrogènes, notamment le carcinome mammaire,le carcinome du corps de l'utérus, l'hyperplasie de l'endomètre,la stérilité, l'endométriose, l'adénomyose utérine,les maladies auto-immunes, la démence, la maladie d'Alzheimer, etc. Dans la formule (I), R<1> et R<2> représentent chacun indépendamment hydrogène ou un alkyle inférieur ; R<3> représente hydrogène, halogéno, un alkyle inférieur, -OSO2NR<1>R<2>, un alcanoylamino inférieur, nitro, ou cyano ; et A désigne un phényle substitué ou non substitué, -X-NR<4>R<5>, ou analogue.

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