Alkylated rapamycin derivatives
US5922730A · kind A · utility
Assignee
Inventors
Key dates
| Filing date | Jun 24, 1998 |
| Grant date | Jul 13, 1999 |
| Priority date | — |
| Expiry date | Jun 24, 2018 |
Classification
- Technology area (CPC C)Chemistry; Metallurgy
- CPC primaryC07D498/18
- WIPO fieldOrganic fine chemistry
- WIPO sectorChemistry
Abstract
This invention relates to compounds which possess immunosuppressive and/or anti tumor and/or antinflammatory activity in vivo and/or inhibit thymocyte proliferation in vitro. These compounds are therefore useful in the treaiment of transplantation rejection, autoimmune diseases such as lupus, rheumatoid ardiritis, diabetes mellitus, multiple sclerosis and in the treatment of Candida albicans infections and also in treatment of diseases of inflammation. These compounds are represented by the formula below ##STR1## wherein W and Y are OR.sup.1 and X and Z together form a bond or W and X are OR.sup.2 and Y and Z together form a bond, wherein: PA1 R.sup.1 is selected from --(CH.sub.2).sub.n --Ar with a proviso that Ar is not phenyl, PA2 --(CH.sub.2 CH.sub.2 O).sub.n CH.sub.3 with a proviso that n is greater than one, PA2 --CH.sub.2 CH.sub.2 CH.sub.2 O(CH.sub.2 CH.sub.2 O).sub.m --CH.sub.3, PA2 --(CH.sub.2).sub.n --CH.sub.2 CH(OR.sup.3)CH.sub.2 OR.sup.4 where R.sup.3 and R.sup.4 are H, C.sub.1 -C.sub.10 alkyl, or R.sup.3 and R.sup.4 together are ethylene, methylene or dimethylmethylene; PA2 --CH.sub.2 (CH.sub.2).sub.n --OR.sup.3 with a proviso that R.sup.3 is not H, C.sub.1 -C.sub.10 al…
Source: USPTO / EPO open patent data. Objective bibliographic and citation counts.