Heteroaryl protease inhibitors and diagnostic imaging agents
US6420397B1 · kind B1 · utility
Assignee
Inventors
Key dates
| Filing date | Jul 7, 2000 |
| Grant date | Jul 16, 2002 |
| Priority date | — |
| Expiry date | Jul 7, 2020 |
Classification
- Technology area (CPC C)Chemistry; Metallurgy
- CPC primaryC07D417/12
- WIPO fieldOrganic fine chemistry
- WIPO sectorChemistry
Abstract
Ketothiazole alkoxyguanidine and aminoguanidine analogs are described, including compounds of the Formula I: wherein X is O or NR9 and Het, A, R1, R7, R8, R12, R13, Ra, Rb, Rc, Z, m and n are set forth in the specification, as well as hydrates, solvates or pharmaceutically acceptable salts thereof, that inhibit proteolytic enzymes such as thrombin. Also described are methods for preparing such compounds. The compounds of the 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. 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 are as anticoagulants either embedded in or physically linked to materials used in the manufacture of devices used in blood collection, blood circulation, an…
Source: USPTO / EPO open patent data. Objective bibliographic and citation counts.