17-side chain alkynyl-and 20-oxopregna-derivatives of...

Details 17-side chain alkynyl-and 20-oxopregna-derivatives of... 17-side chain alkynyl-and 20-oxopregna-derivatives of...

C - Chemistry, Metallurgy

07

C

C07C 401/00 (2006.01) A61K 31/59 (2006.01) A61K 31/695 (2006.01) C07D 309/12 (2006.01) C07F 7/18 (2006.01)

Patent

CA 2241011

1-Hydroxy pregnacalciferol derivatives of formula (I) and their corresponding 5,6-trans isomers wherein R1 is hydroxyl or lower alkoxy and R2 is optionally hydroxylated or lower alkoxylated lower alkynyl or R1 is C(RA) (RB)CH3 where RA is optionally hydroxylated or lower alkoxylated lower alkynyl and RB is hydroxyl or lower alkoxy or RA and RB together represent oxo and R2 is hydrogen, hydroxyl or lower alkoxy, and R3 and R4 represent hydrogen atoms, exhibit anti-progesterone activity and may be useful as antineoplastic, antifertility, antiproliferative, immunosuppressive and/or antiinflammatory agents.

Dérivés de 1-hydroxy pregnacalciferol représentés par la formule (I) et leurs 5,6-trans isomères correspondants, dans laquelle R?1¿ représente hydroxyle ou alcoxy inférieur et R?2¿ représente alkynyle inférieur éventuellement hydroxylé ou alcoxylé inférieur ou R?1¿ représente C(R?A¿) (R?B¿)CH¿3?, où R?A¿ représente alkynyle inférieur éventuellement hydroxylé ou alcoxylé inférieur et R?B¿ représente hydroxyle ou alcoxy inférieur ou R?A¿ et R?B¿ ensemble représentent oxo et R?2¿ représente hydrogène, hydroxyle ou alcoxy inférieur et R?3¿ et R?4¿ représentent des atomes d'hydrogène. Ces dérivés présentent une activité anti-progestérone et peuvent être utiles en tant qu'agents anti-néoplasiques, anti-fertilité, anti-prolifératifs, immunosuppresseurs et/ou anti-inflammatoires.

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