C - Chemistry – Metallurgy – 07 – H
Patent
C - Chemistry, Metallurgy
07
H
C07H 19/01 (2006.01) A61K 31/70 (2006.01) C07D 498/18 (2006.01) C07H 23/00 (2006.01)
Patent
CA 2187024
A compound of structure (I) wherein R1 and R2 are each, independently, hydrogen or -CO(CR3R4)b(CR5R6)dCR7R8R9; R3 and R4 are each, independently, hydrogen, alkyl, alkenyle, alkynyl, trifluoromethyl, or -F; R5 and R6 are each, independently, hydrogen, alkyl, alkenyl, alkynyl, -(CR3R4)fOR10, -CF3, - F, or -CO2R11, or R5 and R6 may be taken together to form X or a cycloalkyl ring that is optionally mono-, di-, or tri-substituted with -(CR3R4)fOR10; R7 is hydrogen, alkyl, alkenyl, alkynyl, -(CR3R4)fOR10, -CF3, -F, or -CO2R11; R8 and R9 are each, independently, hydrogen, alkyl, alkenyl, alkynyl, - (CR3R4)fOR10, -CF3, -F, or -CO2R11, or R8 and R9 may be taken together to form X or a cycloalkyl ring that is optionally mono-, di-, or tri-substituted with - (CR3R4)fOR10; R10 is hydrogen, alkyl, alkenyl, alkynyl, tri-(alkyl)silyl, tri- (alkyl)silylethyl, triphenylmethyl, benzyl, alkoxymethyl, tri- (alkyl)silylethoxymethyl, chloroethyl, or tetrahydropyranyl; R11 is hydrogen, alkyl, alkenyl, alkynyl, or phenylalkyl; X is 5-(2,2-dialkyl)[1,3]dioxanyl, 5- (2-spiro-cycloalkyl)[1,3]dioxanyl, 4-(2,2-dialkyl)[1,3]dioxanyl, 4-(2-spiro- cycloalkyl)[1,3]dioxanyl, 4-(2,2-dialkyl)[1,3]-dioxalanyl, or 4-(2-spiro- cycloalkyl)[1,3]dioxalanyl; b = 0-6; d = 0-6; and f = 0-6 with the proviso that R1 and R2 are both not hydrogen and further provided that either R1 or R2 contains at least one -(CR3R4)fOR10, X, or -(CR3R4)fOR10 substituted cycloalkyl group, or a pharmaceutically acceptable salt thereof which is useful as an immunosuppressive, antiinflammatory, antifungal, antiproliferative, and antitumor agent.
Composé de structure (I) dans lequel: R?1¿ et R?2¿ sont chacun indépendamment hydrogène ou -CO(CR?3¿R?4¿)¿b?(CR?5¿R?6¿)¿d?CR?7¿R?8¿R?9¿; R?3¿ et R?4¿ sont chacun indépendamment hydrogène, alkyle, alcényle, alcynyle, trifluorométhyle ou -F; R?5¿ et R?6¿ sont chacun indépendamment hydrogène, alkyle, alcényle, alcynyle, -(CR?3¿R?4¿)¿f?OR?10¿, -CF¿3?, -F ou -CO¿2?R?11¿, ou bien R?5¿ et R?6¿ peuvent être réunis pour former X ou un cycle cycloalkyle pouvant optionnellement être mono, di ou tri-substitué par -(CR?3¿R?4¿)¿f?OR?10¿; R?7¿ est hydrogène, alkyle, alcényle, alcynyle, -(CR?3¿R?4¿)¿f?OR?10¿, -CF¿3?, -F ou CO¿2?R?11¿; R?8¿ et R?9¿ sont chacun indépendamment hydrogène, alkyle, alcényle, alcynyle, -(R?3¿R?4¿)¿f?OR?10¿, -CF¿3?, -F ou CO¿2?R?11¿, ou bien R?8¿ et R?9¿ peuvent être réunis pour former X ou un cycle cycloalkyle pouvant optionnellement être mono, di ou tri-substitué par -(CR?3¿R?4¿)¿f?OR?10¿; R?10¿ est hydrogène alkyle, alcényle, alcynyle, tri-(alkyl)silyle, tri-(alkyl)silyléthyle, triphénylméthyle, benzyle, alcoxyméthyle, tri-(alkyl)silyléthoxyméthyle, chloroéthyle, ou tétrahydropyranyle; R?11¿ est hydrogène alkyle, alcényle, alcynyle ou phénylalkyle; X est 5-(2,2-dialkyl)[1,3]dioxanyle, 5-(2-spiro-cycloalkyl)[1,3]dioxanyle, 4(2,2-dialkyl)[1,3]dioxanyle, 4(2-spiro-cycloalkyl)[1,3]dioxanyle, 4(2,2-dialkyl)[1,3]dioxalamyle, 4(2-spiro-cycloalkyl)[1,3]dioxalamyle; b = 0-6; d = 0-6; et f = 0-6 sous réserve que R?1¿ et R?2¿ ne soient ni l'un ni l'autre hydrogène et que R?1¿ et R?2¿ contiennent au moins un -(CR?3¿R?4¿)¿f?OR?10¿, un X ou un groupe cycloalkyle à substitution -(CR?3¿R?4¿)¿f?OR?10¿ ou un de leurs sels pharmaceutiquement acceptables servant d'immunosuppresseur, d'anti-inflammatoire, d'antifongique, d'antiproliférant, et d'antitumoral.
Leone Christina L.
Schiehser Guy A.
Skotnicki Jerauld S.
American Home Products Corporation
Torys Llp
Wyeth
LandOfFree
Rapamycin hydroxyesters, process for their preparation and... does not yet have a rating. At this time, there are no reviews or comments for this patent.
If you have personal experience with Rapamycin hydroxyesters, process for their preparation and..., we encourage you to share that experience with our LandOfFree.com community. Your opinion is very important and Rapamycin hydroxyesters, process for their preparation and... will most certainly appreciate the feedback.
Profile ID: LFCA-PAI-O-2040503