Benzimidazolones and analogues and their use as progesterone...

C - Chemistry – Metallurgy – 07 – D

Patent

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Details

C07D 235/26 (2006.01) A61K 31/4184 (2006.01) A61K 31/423 (2006.01) A61K 31/429 (2006.01) A61K 31/498 (2006.01) A61K 31/4985 (2006.01) A61K 31/5415 (2006.01) A61P 5/24 (2006.01) C07C 215/76 (2006.01) C07C 229/18 (2006.01) C07D 235/28 (2006.01) C07D 241/44 (2006.01) C07D 263/58 (2006.01) C07D 277/68 (2006.01) C07D 279/16 (2006.01) C07D 409/04 (2006.01) C07D 487/04 (2006.01)

Patent

CA 2366805

The present invention provides compounds and pharmaceutical formulations useful as progesterone receptor agonists and antagonists and having general formula (a): wherein A is O, S, or NR4; B is a bond between A and C=Q, or the moiety CR5R6; R4, R5, R6 are independently selected from H or optionally substituted C1 to C6 alkyl, C2 to C6 alkenyl, C2 to C6 alkynyl, C3 to C8 cycloalkyl, substituted C3 to C8 cycloalkyl, aryl, or heteorcyclic groups, or cyclic alkyl constructed by fusing R4 and R5 to from a 5 to 7 membered ring; R1 is selected from H, OH, NH2, C1 to C6 alkyl, substituted C1 to C6 alkyl, C3 to C6 alkenyl, substituded C1 to C6 alkenyl, alkynyl, substituted alkynyl, - COH, or optionally substituted -CO(C1 to C3 alkyl), -CO(aryl), -CO(C1 to C3 alkoxy), or -CO(C1 toC3 aminoalkyl) groups; R2 is selected from H, halogen, CN, NO2, or optionally substituted C1 to C6 alkyl, C1 to C6 alkoxy, or C1 to C6 aminoalkyl groups; R3 is selected from a trisubstituted benzene ring; or a 5- or 6- membered heteroaromatic ring containing 1 or 2 substituents; Q is O, S, NR8, or CR9R10; or a pharmaceutically acceptable salt thereof. The invention also includes methods of contraception and methods of treating or preventing maladies associated with the progesterone receptor.

La présente invention concerne des composés et des formulations pharmaceutiques utilisés comme agonistes et antagonistes du récepteur de progestérone représentés par la formule (a): dans laquelle: A représente O, S, ou NR?4¿; B représente une liaison entre A et C=Q, ou la fraction CR?5¿R?6¿; R?4¿, R?5¿, R?6¿ sont individuellement sélectionnés à partir de H ou C¿1?-C¿6? alkyle éventuellement substitué, C¿2?-C¿6? alcényle, C¿2?-C¿6? alcynyle, C¿3?-C¿8? cycloalkyle, C¿3?-C¿8? cycloalkyle substitué, aryle, ou des groupes hétérocycliques, ou alkyle cyclique obtenu par condensation de R?4¿ et R?5¿ pour former un noyau comportant entre 5 et 7 éléments; R?1¿ est sélectionné à partir de H, OH, NH¿2?, C¿1?-C¿6? alkyle, C¿1?-C¿6? alkyle substitué, C¿3?-C¿6? alcényle, C¿1?-C¿6? alcényle substitué, alcynyle, alcynyle substitué, -COH, ou -CO(C¿1?-C¿3? alkyle) éventuellement substitué, -CO(aryle), -CO(C¿1?-C¿3? alcoxy), ou groupes -CO(C¿1?-C¿3? aminoalkyle); R?2¿ est sélectionné à partir de H, halogène, CN, NO¿2?, ou C¿1?-C¿6? alkyle éventuellement substitué, C¿1?-C¿6? alcoxy, ou groupes aminoalkyle C¿1?-C¿6?; R?3¿ est sélectionné à partir d'un noyau de benzène trisubstitué; ou un noyau hétéroaromatique comportant entre 5 et 6 éléments et 1 ou 2 substituants; Q représente O, S, NR?8¿, ou CR?9¿R?10¿; ou un sel de ceux-ci acceptable sur le plan pharmaceutique. En outre, cette invention concerne des méthodes contraceptives et des méthodes de traitement ou de prévention de maladies associées au récepteur de progestérone.

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