Hindered n-oxide esters of rapamycin and their use as...

Details Hindered n-oxide esters of rapamycin and their use as... Hindered n-oxide esters of rapamycin and their use as...

C - Chemistry, Metallurgy

07

H

C07H 19/01 (2006.01) A61K 31/70 (2006.01) C07D 498/18 (2006.01)

Patent

CA 2205577

A compound of structure (I), wherein R and R1 are each, independently, (a), (b), or hydrogen; R2 and R3 are each, independently, alkyl, arylalkyl, or R2 and R3 may be taken together to form a cycloalkyl ring; R4 is a heterocyclic N- oxide radical, which may be optionally substituted; R5 is alkyl or arylalkyl; R6 and R7 are taken together to form a saturated N-alkyl-heterocyclic N-oxide, which may be optionally substituted; k = 0-1, m = 0.1; n = 1-6; with the previso that R and R1 are not both hydrogen, which is useful as an immunosuppressive, antiinflammatory, antifungal, antiproliferative, and antitumor agent.

La présente invention concerne un composé de structure présentée par la formule (I), dans laquelle R et R?1¿ désignent chacun, indépendamment, (a), (b), ou l'hydrogène; R?2¿ et R?3¿ désignent chacun, indépendamment, un alkyle, un arylalkyle, ou R?2¿ et R?3¿ peuvent être pris conjointement pour former un noyau cycloalkyle; R?4¿ est un radical N-oxyde hétérocyclique, qui peut éventuellement être substitué; R?5¿ est un alkyle ou un arylalkyle; R?6¿ et R?7¿ sont pris conjointement pour former un N-oxyde N-alkyl-hétérocyclique saturé, qui peut être éventuellement substitué; k = 0-1; m = 0-1; n = 1-6; à condition que R et R?1¿ ne soient pas tous deux de l'hydrogène. Ce composé est utile en tant qu'agent immunosuppresseur, anti-inflammatoire, antifongique, antiprolifératif et antitumoral.

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