16-hydroxy-11-(substituted phenyl)-estra-4,9-diene derivatives

Details 16-hydroxy-11-(substituted phenyl)-estra-4,9-diene derivatives 16-hydroxy-11-(substituted phenyl)-estra-4,9-diene derivatives

C - Chemistry, Metallurgy

07

J

C07J 41/00 (2006.01) C07J 1/00 (2006.01) C07J 21/00 (2006.01) C07J 31/00 (2006.01) C07J 51/00 (2006.01) C07J 71/00 (2006.01)

Patent

CA 2277924

The present invention relates to 16-hydroxy-11-(substituted phenyl)-estra-4,9- diene derivatives according to formula (I), wherein R1 is C1-6alkyl, C3- 6cycloalkyl, C1-6alkoxy, triflate, pyridyl or phenyl where the phenyl moiety is optionally substituted by one or more substituents selected from cyano, halogen and C1-4alkyl; R2 is hydrogen, C1-6alkyl, 1-oxo-C1-6alkyl or carboxy-1- oxo-C1-6alkyl; R3 is hydrogen, halogen or C1-6alkyl optionally substituted by one or more substituents selected from C1-6alkoxy and halogen; R4 is hydrogen, C1-6alkyl, 1-oxo-C1-6alkyl or carboxy-1-oxo-C1-6alkyl; and X is (H, OH), O or NOH; or a pharmaceutically acceptable salt or solvate thereof; to processes for their preparation, to pharmaceutical formulations containing them and to their use in medical therapy, particularly in the treatment or prophylaxis of glucocorticoid dependent diseases or symptoms.

L'invention concerne des dérivés de 16-hydroxy-11-(phényle substitué)-estra-4,9-diène représentés par la formule (I) dans laquelle R¿1? représente alkyle C¿1?-C¿6?, cycloalkyle C¿3?-C¿6?, alkoxy C¿1?-C¿6?, triflate, pyridyle ou phényle, la fraction phényle étant éventuellement substituée par un ou plusieurs substituants sélectionnés dans cyano, halogène et alkyle C¿1?-C¿4?; R¿2? représente hydrogène, alkyle C¿1?-C¿6?, 1-oxo-alkyle C¿1?-C¿6? ou carboxy-1-oxo-alkyle C¿1?-C¿6?; R¿3? représente hydrogène, halogène ou alkyle C¿1?-C¿6? éventuellement substitué par un ou plusieurs substituants sélectionnés dans akloxy C¿1?-C¿6? et halogène; R¿4? représente hydrogène, alkyle C¿1?-C¿6?, 1-oxo-alkyle C¿1?-C¿6? ou carboxy-1-oxo-alkyle C¿1?-C¿6?; X représente (H, OH), O ou NOH; ou un de leurs sels ou de leurs solvates acceptables sur le plan pharmaceutique; des procédés servant à les préparer, des compositions pharmaceutiques les contenant et leur utilisation en thérapie médicale, en particulier, afin de traiter ou de prévenir des maladies ou des symptômes dépendants des glucocorticoïdes.

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