Rapamycin carbonate esters as immuno-suppressant agents
US5260300A · kind A · utility
Assignee
Inventor
Key dates
| Filing date | Nov 19, 1992 |
| Grant date | Nov 9, 1993 |
| Priority date | — |
| Expiry date | Nov 19, 2012 |
Classification
- Technology area (CPC A)Human Necessities
- CPC primaryA61P37/06
- WIPO fieldPharmaceuticals
- WIPO sectorChemistry
Abstract
Carbonate esters with rapamycin at position 42 or positions 31 and 42 have been shown to have immunosuppressant properties and are useful in the treatment of transplant rejections and autoimmune diseases. These esters are represented by the formula below: ##STR1## wherein: R.sup.1 and R.sup.2 are independently H or --COOR.sup.3 but both R.sup.1 and R.sup.2 cannot be H, and PA1 R.sup.3 is C.sub.1 -C.sub.6 alkyl where 1 to 3 hydrogens may be replaced by fluorine, chlorine, bromine or iodine, C.sub.3 -C.sub.8 cycloalkyl, C.sub.2 -C.sub.6 alkenyl, or Ar--(CH.sub.2).sub.n -- where n is 0 to 6 and Ar is phenyl, phenyl substituted by fluorine, chlorine, bromine, iodine, trifluoromethyl, nitro, cyano, C.sub.1 -C.sub.6 alkyl or C.sub.1 -C.sub.6 alkoxy; pyridinyl, indolyl, quinolyl or furanyl; PA1 or a pharmaceutically acceptable salt thereof.
Source: USPTO / EPO open patent data. Objective bibliographic and citation counts.