Cyclocarbamate derivatives as progesterone receptor modulators

Details Cyclocarbamate derivatives as progesterone receptor modulators Cyclocarbamate derivatives as progesterone receptor modulators

C - Chemistry, Metallurgy

07

D

C07D 417/04 (2006.01) A61K 31/5355 (2006.01) A61K 31/536 (2006.01) A61K 31/541 (2006.01) A61P 15/00 (2006.01) A61P 35/00 (2006.01) C07D 265/18 (2006.01) C07D 413/04 (2006.01) C07D 413/10 (2006.01)

Patent

CA 2371726

This invention provides compounds of Formula (I) wherein R1 and R2 may be single substituents or fused to form spirocyclic or heterospirocyclic rings; R3 is H, OH, NH2, C1 to C6 alkyl, substituted C1 to C6 alkyl, C3 to C6 alkenyl, substituted C1 to C6 alkenyl, alkynyl, or substituted alkynyl, CORC; RC is H, C1 to C3 alkyl, substituted C1 to C3 alkyl, aryl, substituted aryl, C1 to C3 alkoxy , substituted C1 to C3 alkoxy, C1 to C3 aminoalkyl, or substituted C1 to C3 aminoalkyl; R4 is H, halogen, CN, NO2, C1 to C6 alkyl, substituted C1 to C6 alkyl, alkynyl, or substituted alkynyl, C1 to C6 alkoxy, substituted C1 to C6 alkoxy, substituted C1 to C6 alkoxy, amino, C1 to C6 aminoalkyl, or substituted C1 to C6 aminoalkyl; and R5 is selected from a trisubstituted benzene ring of a five or six membered ring with 1, 2, or 3 heteroatoms from the group including O, S, SO, SO2 or NR6 and containing one or two independent substituents from the group including H, halogen, CN, NO2, amino, and C1 to C3 alkyl, C1 to C3 alkoxy, C1 to C3 aminoalkyl, CORF, or NRGCORF; or pharmaceutically acceptable salt thereof, as well as pharmaceutical compositions and methods using the compounds as antagonists of the progesterone receptor.

La présente invention concerne des composés de formule (I) dans laquelle R?1¿ et R?2¿ peuvent être des substituants indépendants ou condensés pour former des noyaux spirocyclique ou hétérospirocycliques; R?3¿ représente H, OH, NH2, C¿1?-C¿6? alkyle, C¿1?-C¿6? alkyle substitué, C¿3?-C¿6? alcényle, C¿1?-C¿6? alcényle substitué, alcynyle, ou alcynyle substitué, COR?C¿; R?C¿ représente H, C¿1?-C¿3? alkyle, C¿1?-C¿3? alkyle substitué, aryle, aryle substitué, C¿1?-C¿3? alcoxy, C¿1?-C¿3? alcoxy, C¿1?-C¿3? aminoalkyle, ou C¿1?-C¿3? aminoalkyle substitué; R?4¿ représente H, halogène, CN, NO¿2?, C¿1?-C¿6? alkyle, C¿1?-C¿6? alkyle substitué, alcynyle, ou alcynyle substitué, C¿1?-C¿6? alcoxy, amino, C¿1?-C¿6? aminoalkyle, ou C¿1?-C¿6? aminoalkyle substitué; et R?5¿ est sélectionné parmi un noyau de benzène trisubstitué avec un noyau de 5 à 6 éléments et 1, 2, ou 3 hétéroatomes sélectionnés dans le groupe constitué par O, S, SO, SO¿2? ou NR?6¿ et contenant un ou deux substituants indépendants du groupe constitué de H, halogène, CN, NO¿2?, amino, and C¿1?-C¿3? alkyle, C¿1?-C¿3? alcoxy, C¿1?-C¿3? aminoalkyle, COR?F¿, ou NR?G¿COR?F¿; ou des sels de ceux-ci acceptables sur le plan pharmaceutique; cette invention concernant également des compositions et des méthodes d'utilisation de ces composés comme antagonistes du récepteur de progestérone.

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