11.beta.-benzaldoxime derivatives of...

Details 11.beta.-benzaldoxime derivatives of... 11.beta.-benzaldoxime derivatives of...

C - Chemistry, Metallurgy

07

J

C07J 41/00 (2006.01) A61K 31/565 (2006.01) A61P 5/46 (2006.01)

Patent

CA 2631364

The present patent application relates to 11.beta.-benzaldoxime derivatives of D-homooestra-4,9-dien-3-ones of Formula (I): wherein R1 is a hydrogen atom or a C1-C6-alkyl, C1-C6-acyl, C1-C4-alkoxycarbonyl, C1-C4-alkylthiocarbonyl, C1-C6-alkylaminocarbonyl or arylaminocarbonyl group; and R2 is a hydrogen atom or a C1-C6-alkyl or C1-C6-acyl group. Compounds of Formula (I) bind more strongly to the glucocorticoid receptor than to the progesterone receptor and are effective antiglucocorticoids. According to the invention, they are suitable for the treatment and/or prevention of symptoms and/or diseases that are attributable to an androgen deficiency induced by glucocorticoids, especially cortisol.

La présente invention concerne des dérivés 11ß-benzaldoxime de D-homooestra-4,9-dien-3-ones de formule (I) : dans laquelle R<SUB>1</SUB> est un atome d'hydrogène ou un groupe alkyle en C<SUB>1</SUB>-C<SUB>6</SUB>, acyle en C<SUB>1</SUB>-C<SUB>6</SUB>, alcoxycarbonyle en C<SUB>1</SUB>-C<SUB>4</SUB>, alkylthiocarbonyle en C<SUB>1</SUB>-C<SUB>4</SUB>, alkylaminocarbonyle en C<SUB>1</SUB>-C<SUB>6</SUB> ou arylaminocarbonyle ; et R<SUB>2</SUB> est un atome d'hydrogène ou un groupe alkyle en C<SUB>1</SUB>-C<SUB>6</SUB> ou acyle en C<SUB>1</SUB>-C<SUB>6</SUB>. Les composés de formule (I) se lient plus fortement au récepteur des glucocorticoïdes qu'au récepteur de la progestérone et ce sont des anti-glucocorticoïdes efficaces. Selon l'invention, ils conviennent pour le traitement et/ou la prévention de symptômes et/ou de maladies qui sont attribuables à une carence en androgènes induite par les glucocorticoïdes, spécialement le cortisol.

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