2-saccharinylmethyl and 4,5,6,7-tetrahydro-2-saccharinylmethyl phosphates, phosphonates and phosphinates useful as proteolytic enzyme inhibitors and compositions and method of use thereof
US5187173A · kind A · utility
Assignee
Inventors
Key dates
| Filing date | Dec 27, 1991 |
| Grant date | Feb 16, 1993 |
| Priority date | — |
| Expiry date | Dec 27, 2011 |
Classification
- Technology area (CPC C)Chemistry; Metallurgy
- CPC primaryC07F9/65744
- WIPO fieldOrganic fine chemistry
- WIPO sectorChemistry
Abstract
4-R.sub.1 -R.sub.2 -R.sub.3 -2-Saccharinylmethyl, 4-R.sub.4 -4-R.sub.5 -6-R.sub.6 -4,5,6,7-tetrahydro-2-saccharinylmethyl and 4,7-C-4,5,6,7-tetrahydro-2-saccharinylmethyl phosphates, phosphonates and phosphinates of formulas I, II and IIA respectively herein, useful in the treatment of degenerative diseases, and compositions containing them, methods for using them to treat degenerative diseases, and processes for their preparation by reaction of the corresponding 2-halomethylsaccharins with a phosphate, phosphonate or phosphinic acid of formula III herein in the presence of an acid-acceptor.
Source: USPTO / EPO open patent data. Objective bibliographic and citation counts.