Rapamycin 42-oximes and hydroxylamines

Details Rapamycin 42-oximes and hydroxylamines Rapamycin 42-oximes and hydroxylamines

C - Chemistry, Metallurgy

07

H

C07H 19/01 (2006.01) A61K 31/70 (2006.01) C07D 498/18 (2006.01) C07F 7/18 (2006.01) C07H 23/00 (2006.01)

Patent

CA 2206965

A compound of structure (I) wherein X-Y is C=NOR1 or CHNHOR2; R1 and R2 are each, independently, hydrogen, alkyl, alkenyl, alkynyl, aminoalkyl, alkylaminoalkyl, dialkylaminoalkyl, cycloalkyl, alkyloxy, alkoxyalkyl, cycloalkylaminoalkyl, cyanoalkyl, fluoroalkyl, trifluoromethylalkyl, trifluoromethyl, ArO-, -(CH2)mAr, or -COR3; R3 is alkyl of 1-6 carbon atoms, - NH2, -NHR4, -NR4R5, or -OR4; R4 and R5 are each, independently, alkyl, Ar or if both are present can be taken together to form a 4-7 membered ring; Ar is an aryl or heteroaryl radical which may be optionally substituted; and m = 0- 6; or a pharmaceutically acceptable salt thereof, which is useful as an immunosuppressive, antiinflammatory, antifungal, antiproliferative, and antitumor agent.

Cette invention concerne un composé pouvant être représenté par la formule (I), où: X-Y est C=NOR?1¿ ou CHNHOR?2¿; R?1¿ et R?2¿ sont chacun indépendamment choisis parmi les éléments suivants: hydrogène, alkyle, alcényle, alcynyle, aminoalkyle, alkylaminoalkyle, dialkylaminoalkyle, cycloalkyle, alkyloxy, alcoxyalkyle, cycloalkylaminoalkyle, cyanoalkyle, fluoroalkyle, trifluorométhylalkyle, trifluorométhyle, ArO-, -(CH¿2?)¿m?Ar ou -COR?3¿; R?3¿ est choisi parmi les éléments suivants: alkyle contenant 1 à 6 atomes de carbone, -NH¿2?, -NHR?4¿, -NR?4¿R?5¿, ou -OR?4¿; R?4¿ et R?5¿ sont chacun indépendamment un alkyle, Ar, ou, si les deux sont présents, peuvent être pris ensemble pour former un cycle de 4 à 7 chaînons; Ar est un aryle ou un radical hétéroaryle pouvant éventuellement être substitué; et enfin m = 0-6. Cette invention concerne également tout sel de ce composé acceptable d'un point de vue pharmaceutique, lequel peut être employé comme agent immunosuppressif, anti-inflammatoire, antifongique, antiproliférateur et antitumoral.

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