Aminoguanidines and alkoxyguanidines as protease inhibitors
US6235778A · kind A · utility
Assignee
Inventors
Key dates
| Filing date | Nov 26, 1997 |
| Grant date | May 22, 2001 |
| Priority date | — |
| Expiry date | Nov 26, 2017 |
Classification
- Technology area (CPC C)Chemistry; Metallurgy
- CPC primaryC07C2601/14
- WIPO fieldOrganic fine chemistry
- WIPO sectorChemistry
Abstract
Aminoguanidine and alkoxyguanidine compounds, including compounds of the formula: ##STR1## PA1 wherein X is O or NR.sup.9 and R.sup.1 14 R.sup.4, R.sup.6 -R.sup.9, R.sup.11, R.sup.12, R.sup.a, R.sup.b, R.sup.c, Y, Z, n and mare set forth in the specification, as well as hydrates, solvates or pharmaceutically acceptable salts thereof, that inhibit proteolytic enzymes such as thrombin are described. Also described are methods for preparing the compounds of Formula I. The novel compounds of the present invention are potent inhibitors of proteases, especially trypsin-like serine proteases, such as chymotrypsin, trypsin, thrombin, plasmin and factor Xa. Certain of the compounds exhibit antithrombotic activity via direct, selective inhibition of thrombin, or are intermediates useful for forming compounds having antithrombotic activity. The invention includes a composition for inhibiting loss of blood platelets, inhibiting formation of blood platelet aggregates, inhibiting formation of fibrin, inhibiting thrombus formation, and inhibiting embolus formation in a mammal, comprising a compound of the invention in a pharmaceutically acceptable carrier. Other uses of compounds of the invention…
Source: USPTO / EPO open patent data. Objective bibliographic and citation counts.