Rapamycin 31-ester with N,N-dimethylglycine derivatives useful as immunosuppressive agents
US5416086A · kind A · utility
Assignee
Inventors
Key dates
| Filing date | Apr 22, 1994 |
| Grant date | May 16, 1995 |
| Priority date | — |
| Expiry date | Apr 22, 2014 |
Classification
- Technology area (CPC C)Chemistry; Metallurgy
- CPC primaryC07D498/18
- WIPO fieldOrganic fine chemistry
- WIPO sectorChemistry
Abstract
A derivative of rapamycin of general formula (1) and (2) ##STR1## wherein ##STR2## R.sup.2 =hydrogen, or lower alkyl having 1 to 6 carbon atoms; ##STR3## wherein X=hydrogen, lower alkyl having 1 to 6 carbon atoms, --CF.sub.3, --NO.sub.2, --OR.sup.2, NR.sup.2, SR.sup.2, or halogen; PA0 R.sup.4 =lower alkyl, alkenyl or alkynyl having 1 to 6 carbon atoms or an aromatic or heterocyclic moiety selected from the group consisting of phenyl, naphthyl, thiophenyl and quinolinyl; PA0 Y.sup.- =halide, methanesulfonate, toluene sulfonate or maleate: and PA0 Z=oxygen or OH and H. which by virtue of its immunosuppressive activity is useful in treating transplantation rejection, host versus graft disease, autoimmune diseases, and diseases of inflammation.
Source: USPTO / EPO open patent data. Objective bibliographic and citation counts.