Macrocyclic immunomodulators

Details Macrocyclic immunomodulators Macrocyclic immunomodulators

C - Chemistry, Metallurgy

07

H

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

Patent

CA 2115295

ABSTRACT MACROCYCLIC IMMUNOMODULATORS This invention provides a compound of the structure Image I or a derivative thereof functionalised in the 31 and/or 42 position, wherein X is selected from the group consisting of -NR1CR2R3(CR4R5)mS-, -NR1CR2R3(CR4R5)mO-, -OCR2R3(CR4R5)mO-, -NR1CR2R3(CR4R5)p-, -OCR2R3(CR4R5)p-,-NR1CR2R3(CR4R5)mNR6- ,-OCR2R3(CR4R5)mNR6-, -SCR2R3(CR4R5)mNR6-, -SCR2R3(CR4R5)mS-, -NOR1-, and -NR1-; R1, R2, R3, R4, R5, and R6 are each, independently, hydrogen, alkyl, trifluoromethyl, aryl or arylalkyl, R2, R3, R4 and R5 each also independently represent fluorine or any pair of R1-6 taken together form a 3-6 membered ring; and when more than one R4 or R5 value is present then they may be the same or different; m= 1-6; and p = 0-6 or a pharmaceutically acceptable salt thereof which is useful as an immunosuppressive, antiinflammatory, antifungal, antiproliferative, and antitumor agent. This invention also covers derivatives of I and the use of I in combination with other immunoregulatory agents.

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