Rapamycin arylcarbonyl and alkoxycarbonyl as...

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 2148247

2148247 9410176 PCTABS00032 N-arylcarbonyl and N-alkylcarbonyl carbamates of rapamycin of formula (I), wherein R1 is (a) and R2 is H or (b) or R1 and R2 are both (a) and where A is lower alkoxy or aryl or heteroaryl, R3 is H or methyl and R4 is C1-C6 alkyl, C2-C6 alkenyl or C2-C6 alkynyl possess immunosuppressive and/or antifungal and/or antitumor and/or antiinflammatory activity in vitro) and/or inhibit thymocyte proliferation in vivo. These compounds are thus expected to be useful in the treatment of transplantation rejection, autoimmune diseases, fungal infections, cancer, and diseases of inflammation.

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