3.alpha.-hydroxy-3.beta. methoxymethyl-21-heterocycle...

Details 3.alpha.-hydroxy-3.beta. methoxymethyl-21-heterocycle... 3.alpha.-hydroxy-3.beta. methoxymethyl-21-heterocycle...

C - Chemistry, Metallurgy

07

J

C07J 43/00 (2006.01) A61K 31/58 (2006.01)

Patent

CA 2372342

This invention relates to compounds having Formula (I) or a pharmaceutically acceptable salt, prodrug or solvate thereof, wherein; R1 is H or methyl; R2 is 5.alpha.- or 5.beta.- H; R3 is an optionally substituted N-attached heteroaryl group or a group -X-R4; R4 is an optionally substituted carbon-attached heteroaryl group; and X is O, S or N. The invention also is directed to the use of 3.alpha.- hydroxy-3.beta.- methoxymethyl-substituted steroids as sedative/hypnotics and for inducing anesthesia.

La présente invention concerne des composés de la formule (I) ou des sels pharmaceutiquement acceptables, des promédicaments ou des solvats desdits composés. Dans ladite formule, R¿1? est H ou méthyle; R¿2? est 5.alpha. ou 5.beta. H; R¿3? est un groupe hétéroaryle à liaison N éventuellement substitué ou un groupe X-R¿4?; R¿4? est un groupe hétéroaryle à liaison carbone éventuellement substitué; et X est O, S ou N. L'invention concerne en outre l'utilisation de stéroides substitués par 3.alpha. hydroxy 3.beta. méthoxyméthyle comme sédatifs ou hypnotiques, et notamment comme anesthésiques.

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