Steven B Vernon

US Patent:

55040918, Apr 2, 1996

Filed:

Apr 14, 1994

Appl. No.:

8/224206

Inventors:

Timothy D. Ocain - Waltham MA
Steven K. Vernon - Havertown PA
John J. Huang - San Carlos CA

Assignee:

American Home Products Corporation - Madison NJ

International Classification:

C07D51900
A61K 31395

US Classification:

514291

Abstract:

A compound of the structure ##STR1## R. sup. 1 and R. sup. 2 are each, independently, hydrogen or ##STR2## X is ##STR3## Y is ##STR4## Z is --CH. sub. 2 --, --S--S--, or ##STR5## R. sup. 3 is hydrogen, alkyl, arylalkyl, alkenyl, alkynyl, --(CH. sub. 2). sub. q CO. sub. 2 R. sup. 5, --(CH. sub. 2). sub. r NR. sup. 6 R. sup. 7, carbamylalkyl, aminoalkyl, hydroxyalkyl, guanylalkyl, mercaptoalkyl, alkylthioalkyl, indolylmethyl, hydroxyphenylmethyl, imidazoylmethyl, halo, trifluoromethyl, or phenyl which is optionally mono-, di-, or tri-substituted; R. sup. 4, R. sup. 6, and R. sup. 7 are each, independently, hydrogen, alkyl, or arylalkyl; R. sup. 5 is hydrogen, alkyl, arylalkyl, alkenyl, alkynyl, or phenyl which is optionally mono-, di-, or tri-substituted; h=0-1; j=0-1; m=0-6; n=0-6; p=0-10; q=0-10; r=0-6; with the proviso that R. sup. 1 and R. sup. 2 are not both hydrogen, or a pharmaceutically acceptable salt thereof which is useful for inducing immunosuppression; in the treatment of transplantation rejection, host vs. graft disease, autoimmune diseases, diseases of inflammation, solid tumors, fungal infections, adult T-cell leukemia/lymphoma, and hyperproliferative vascular disorders; for measuring levels of rapamycin; for isolating rapamycin-binding proteins; and detecting monoclonal antibodies specific for rapamycin or derivatives thereof.