Aminodiesters of rapamycin
US5162333A · kind A · utility
Assignee
Inventors
Key dates
| Filing date | Sep 11, 1991 |
| Grant date | Nov 10, 1992 |
| Priority date | — |
| Expiry date | Sep 11, 2011 |
Classification
- Technology area (CPC C)Chemistry; Metallurgy
- CPC primaryC07D519/00
- WIPO fieldOrganic fine chemistry
- WIPO sectorChemistry
Abstract
A compound of the structure ##STR1## wherein R.sup.1 is ##STR2## R.sup.3 is hydrogen, alkyl, arylalkyl, (CH.sub.2).sub.s NR.sup.4 R.sup.5, aminoalkyl, hydroxyalkyl, guanylalkyl, mercaptoalkyl, alkylthioalkyl, indolylmethyl, hydroxyphenylmethyl, imidazolylmethyl or phenyl which is optionally mono-, di-, or tri-substituted; PA0 R.sup.4 is hydrogen, alkyl, or aralkyl; PA0 R.sup.2 and R.sup.5 are each independently hydrogen, formyl, alkanoyl, arylalkanoyl, aryloyl, or CO.sub.2 R.sup.6 ; PA0 R.sup.6 is alkyl, arylalkyl, allyl, fluorenylmethyl, or phenyl which is optionally mono-, di-, or tri-substituted; PA0 m is 0-4; n is 0-4; p is 0-1; q is 0-4; r is 0-4; and s is 0-4; 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 antifungal activity is useful in treating fungal infections; and by virtue of its antitumor activity is useful in treating tumors.
Source: USPTO / EPO open patent data. Objective bibliographic and citation counts.