Rapamycin amidino carbamates and pharmaceutical compositions...

C - Chemistry – Metallurgy – 07 – H

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

Patent

CA 2192972

A compound of the structure (I) wherein R and R1 are each, independently, hydrogen, or (a); R2 and R3 are each, independently, hydrogen, alkyl, alkenyl, alkynyl, -CO2R5, -COR5, -CN, -NO2, -SO2R5, -SO3R5, -OR5, -SR5, or Ar; R4 is hydrogen, alkyl, alkenyl, alkynyl, -CF3, -NR5R6, -CO2R5, -COR5, CONR5R6, -NO2, halogen, -OR5, -SR5, -CN, -SO2R5, -SO3R5, -SO2NR5R6, or Ar; R5 and R6 are each, independently, hydrogen, alkyl, alkenyl, alkynyl, or Ar; Ar is phenyl, naphthyl, or hetaryl, wherein the foregoing may be optionally substituted; with the proviso that R and R1 are both not hydrogen, or a pharmaceutically acceptable salt thereof which is useful as an immunosuppressive, anti- inflammatory, antifungal, antiproliferative, and antitumor agent.

Composé de structure (I), dans laquelle R et R?1¿ représentent chacun, indépendamment, hydrogène, ou (b); R?2¿ et R?3¿ représentent chacun, indépendamment, hydrogène, alkyle, alcényle, alkynyle, -CO¿2?R?5¿, -COR?5¿, -CN, -NO¿2?, -SO¿2?R?5¿, -SO¿3?R?5¿, -OR?5¿, -SR?5¿, ou Ar; R?4¿ représente hydrogène, alkyle, alcényle, alkynyle, -CF¿3?, -NR?5¿R?6¿, -CO¿2?R?5¿, -COR?5¿, -CONR?5¿R?6¿, -NO¿2?, halogène, -OR?5¿, -SR?5¿, -CN, -SO¿2?R?5¿, -SO¿3?R?5¿, -SO¿2?NR?5¿R?6¿, ou Ar; R?5¿ et R?6¿ représentent chacun, indépendamment, hydrogène, alkyle, alcényle, alkynyle, ou Ar; Ar représente phényle, naphtyle ou hétaryle, ces composés pouvant être éventuellement substitués; à condition que R et R?1¿ ne représentent pas tous les deux hydrogène. Ce composé ou un de ses sels acceptable en pharmacologie est utile comme agent immunosuppresseur, anti-inflammatoire, antifongique, antiprolifératif et antitumoral.

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