Patent ID: 6462064
Filing Date: 2002-10-08
Classification: A61K,A61P

Abstract:
A method for treating or preventing cancer or precancer sensitive to the formulae below in a subject in need of such treatment or prevention by inducting apoptosis of cancer or precancer cells by the administration of an apoptotic inducing effective amount of an adamantyl retinoid related compound having one of the following generic formulae set forth below or a pharmaceutically acceptable salt, optical and/or geometrical isomer thereof;a compound of generic formula (I): with the proviso that saidretinoid of Formula (I) is not an RAR-&ggr; receptor-specific agonist ligand, and whereinW is independently â€”CH2â€”, â€”Oâ€”, â€”Sâ€”, â€”SOâ€” or â€”SO2â€”, X is a radical selected from among those of the following formulae (i)-(iii): â€ƒwherein Y is a radical â€”COâ€”Vâ€”, â€”CH&boxH;CHâ€”, â€”CH3C&boxH;CHâ€”, â€”CH&boxH;CCH3â€”, â€ƒâ€”CHOHâ€”CH2â€”Oâ€”, V is an oxygen atom (â€”Oâ€”), an aza radical (â€”NHâ€”), a radical â€”CH&boxH;CHâ€” or â€”Câ‰¡Câ€”; Z is a radical â€”CHâ€” and Zâ€² is an oxygen atom, or Z is a nitrogen atom (N) and Zâ€² is an aza radical (â€”NHâ€”); R1 is a hydrogen atom, halogen atom, or a lower alkyl radical; Râ€²1 is a hydrogen atom, halogen atom, or a lower alkyl radical; R2 is a hydroxyl radical, an alkyl radical, optionally substituted by one or more hydroxyl or acyl groups, an alkoxyl radical, optionally substituted by one or more hydroxyl, alkoxyl or aminocarbonyl groups, and/or optionally interrupted by one or more oxygen atoms, an acyl radical, an aminocarbonyl radical or a halogen; R3 is a hydrogen atom, a hydroxyl radical, an alkyl radical, or an alkoxyl radical; R2 and R3 can form together a radical â€”Oâ€”CH2â€”Oâ€”; R4 is a hydrogen atom, an alkyl radical, an alkoxyl radical, or a halogen; R5 is a radical â€”COâ€”R10, an alkyl radical, optionally substituted by one or more hydroxyl groups, or a halogen; R6 is a hydrogen atom, a halogen atom, a hydroxyl group, or an alkoxyl radical; R7 is a hydrogen atom or a halogen; R8 is a hydrogen atom, a halogen atom or an alkyl radical; R9 is a hydrogen atom, a hydroxyl radical or a halogen atom; R10 is a hydroxyl radical, an alkoxy radical, a radical of formula â€”Nrâ€²râ€³, wherein râ€² and râ€³ represent a hydrogen atom, an optionally substituted aminoalkyl radical, a mono- or polyhydroxyalkyl radical, an optionally substituted aryl radical or an amino acid or sugar residue; or a compound having generic formula (III): wherein Râ€²1, R1, R2, R3, R4, R5, R6 and W are as defined for compounds of formula (I) or is a compound of formula (IV) wherein Râ€²1, R1, R2, R3, R4, R5, R6 and W are as defined for compounds of formula (I).