Patent · US Expired

Carbamates of rapamycin

US5489680A · kind A · utility

100Cited by
32References
9Claims
0Family size

Assignee

Inventors

Key dates

Filing dateAug 2, 1994
Grant dateFeb 6, 1996
Priority date
Expiry dateAug 2, 2014

Classification

  • Technology area (CPC A)Human Necessities
  • CPC primaryA61K31/70
  • WIPO fieldPharmaceuticals
  • WIPO sectorChemistry

Abstract

A compound of the structure ##STR1## wherein R.sup.1 and R.sup.2 are each, independently, hydrogen, or --CONH--O--(CR.sup.3 R.sup.4).sub.m Z; PA1 R.sup.3 and R.sup.4 are each, independently, hydrogen, alkyl, cycloalkyl, --CF.sub.3, or F; PA1 Z is hydrogen, alkyl, --OR.sup.5, --SR.sup.5, --NRSR.sup.6, --CN, --CF3, --OAr, --Ar, or R.sup.7 ; PA1 R.sup.5 and R.sup.6 are each, independently, hydrogen, alkyl, arylalkyl, alkenyl, alkynyl, alkoxyalkyl, alkylthioalkyl, alkylaminoalkyl, dialkylaminoalkyl, cycloalkyl, or Ar; PA1 R.sup.7 ##STR2## or --C.tbd.C--R.sup.11 ; R.sup.8, R.sup.9, R.sup.10, and R.sup.11 are each, independently, hydrogen, alkyl of 1-6 carbon atoms, halogen, or phenyl, wherein the phenyl group may be optionally mono-, di-, or tri-substituted; PA1 Ar is an aryl radical that may be optionally mono-, di-, or tri-substituted; and m=1-6; with the proviso that R.sup.1 and R.sup.2 are both not hydrogen, or a pharmaceutically acceptable salt thereof which is useful as an immunosuppressive, antiinflammatory, antifungal, antiproliferative, and antitumor agent.

Source: USPTO / EPO open patent data. Objective bibliographic and citation counts.