Hindered esters of rapamycin and their use as pharmaceuticals

Details Hindered esters of rapamycin and their use as pharmaceuticals Hindered esters of rapamycin and their use as pharmaceuticals

C - Chemistry, Metallurgy

07

D

C07D 498/04 (2006.01) A61K 31/436 (2006.01) C07D 498/18 (2006.01) C07H 19/01 (2006.01)

Patent

CA 2176955

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 radical which may be optionally substituted; R5 is alkyl or arylalkyl; R6 and R7 are taken together to form a saturated heterocyclic ring which may be optionally substituted; k=0-1; m=0-1; n=1-6; with the proviso that R and R1 are not both hydrogen, or a pharmaceutically acceptable salt thereof, which is useful as an immunosuppresive, antiinflammatory, antifungal, antiproliferative, and antitumor agent.

Composé de structure (I) dans laquelle R et R?1¿ représentent chacun, indépendamment, (A), (B), ou hydrogène; R?2¿ et R?3¿ représentent chacun, indépendamment alkyle, arylalkyle, ou bien R?2¿ et R?3¿ peuvent être pris ensemble pour former un anneau cycloalkyle; R?4¿ représente un radical hétérocyclique qui peut être facultativement substitué; R?5¿ représente alkyle ou arylalkyle; R?6¿ et R?7¿ sont pris ensemble pour former un anneau hétérocyclique saturé qui peut être facultativement substitué; k=0-1; m=0-1; n=1-6; à condition que R et R?1¿ ne représentent pas tous les deux hydrogène. Ce composé ou un de ses sels pharmaceutiquement acceptables est utile comme agent immunosuppresseur, anti-inflammatoire, antifongique, antiprolifératif et antitumoral.

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