Macrocyclic carbamate immunomodulators

Organic compounds -- part of the class 532-570 series – Organic compounds – Unsubstituted hydrocarbyl chain between the ring and the -c-...

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C07D49116, A61K 31435

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active

055346324

ABSTRACT:
Immunomodulatory macrocyclic compounds having the formula: ##STR1## and the pharmaceutically acceptable salts, esters, amides and prodrugs thereof, wherein R.sup.8 and R.sup.9 are selected such that one of R.sup.8 and R.sup.9 is hydrogen, and the other is chosen from the group consisting of:
(1) --OC(.dbd.NR.sup.10)-NHR.sup.10 ;
(2) --OC(.dbd.O)-R.sup.11 ; and
(3) --OC(.dbd.O)-NR.sup.12 R.sup.13 ;
(4) --OC(.dbd.O)-N(OR.sup.14)R.sup.12 ;
(5) --OC(.dbd.O)-NHNR.sup.12 R.sup.13 ;
(6) --OC(.dbd.O)-NH-NHC(.dbd.O)-NR.sup.12 R.sup.13 ;
(7) --OC(.dbd.O)-NH-NHS(O).sub.2 --NR.sup.12 R.sup.13 ; and
(8) --OC(.dbd.O)-NH-NHC(.dbd.NR.sup.21 )-NR.sup.12 R.sup.13. as well as pharmaceutical compositions containing such compounds and methods for their use in immunosuppressive, antimicrobial, antifungal, antiviral, antiinflammatory and antiproliferative therapy.

REFERENCES:
patent: 5208241 (1993-05-01), Ok et al.
patent: 5250678 (1993-10-01), Goulet et al.

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