Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Heterocyclic carbon compounds containing a hetero ring...
Patent
1991-05-20
1992-06-02
Bond, Robert T.
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Heterocyclic carbon compounds containing a hetero ring...
514321, 540456, A61K 31395, C07D49106
Patent
active
051186772
ABSTRACT:
A compound of the structure ##STR1## wherein R.sup.1 and R.sup.2 are each independently, hydrogen or ##STR2## X is --(CH.sub.2).sub.m -- or --Ar--; R.sup.3 and R.sup.4 are each, independently, hydrogen, alkyl, --(CH.sub.2).sub.n --Ar, --(CH.sub.2).sub.p --NR.sup.5 R.sup.6, or --(CH.sub.2).sub.p --N.sup.+ R.sup.5 R.sup.6 R.sup.7 Y.sup.- ; R.sup.5 and R.sup.6 are each, independently, hydrogen, alkyl, or --(CH.sub.2).sub.n --Ar; Ar is an optionally substituted group selected from ##STR3## in which the optional substituents are selected from the group consisting of alkyl, aralkyl, alkoxy, cyano, halo, nitro, carbalkoxy, or perfluoroalkyl; R.sup.7 is alkyl; Y is a halide, sulfate, phosphate, or p-toluenesulfonate anion; m=1-6; n=1-6; p=1-6; with the proviso that R.sup.1 and R.sup.2 are not both hydrogen; or a pharmaceutically acceptable salt thereof, which by virtue of its immunosuppressive activity is useful in treating transplantation rejection, host vs. graft disease, autoimmune diseases and diseases of inflammation; by virtue of its antitumor activity is useful in treating solid tumors; and by virtue of its antifungal activity is useful in treating fungal infections.
REFERENCES:
patent: 3929992 (1975-12-01), Seghah et al.
patent: 3993749 (1976-11-01), Seghal et al.
patent: 4316885 (1982-02-01), Rakhit
patent: 4401653 (1983-08-01), Eng
patent: 4885171 (1989-12-01), Surendra et al.
J. Antibiot. 28, 721-726 (1975).
J. Antibiot. 28, 727-732 (1975).
J. Antibiot. 31, 539-545 (1978).
Can. J. Physiol. Pharmacol. 55, 48(1977).
FASEB 3,3411 (1989).
FASEB 3,5256 (1989).
Lancet 1183 (1978).
Med. Sci Res. 17:877 (1989).
American Home Products Corporation
Bond Robert T.
Milowsky Arnold S.
LandOfFree
Amide esters of rapamycin does not yet have a rating. At this time, there are no reviews or comments for this patent.
If you have personal experience with Amide esters of rapamycin, we encourage you to share that experience with our LandOfFree.com community. Your opinion is very important and Amide esters of rapamycin will most certainly appreciate the feedback.
Profile ID: LFUS-PAI-O-2228482