Rapamycin arylcarbonyl and alkoxycarbonyl carbamates as immunosu

Details Rapamycin arylcarbonyl and alkoxycarbonyl carbamates as immunosu Rapamycin arylcarbonyl and alkoxycarbonyl carbamates as immunosu

1992-10-29

1993-11-16

Shah, Mukund J.

Drug, bio-affecting and body treating compositions

Designated organic active ingredient containing

Having -c-, wherein x is chalcogen, bonded directly to...

540456, C07D49816, A61K 31395

Patent

active

052624234

ABSTRACT:
N-arylcarbonyl and N-alkylcarbonyl carbamates of rapamycin of the formula shown below wherein ##STR1## R.sup.1 and R.sup.2 are both ##STR2## and where A is lower alkoxy or aryl or heteroaryl, R.sup.3 is H or methyl and R.sup.4 is C.sub.1 -C.sub.6 alkyl, C.sub.2 -C.sub.6 alkenyl or C.sub.2 -C.sub.6 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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