Title:
環式オキシグアニジンプロテアーゼインヒビター
Document Type and Number:
Japanese Patent JP2004505956
Kind Code:
A
Abstract:
Cyclic oxyguanidine compounds, including compounds of Formulae I and II: wherein R1, R3-R6, R21-R26, L, Y, Z, and A are 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 Formulae I and II. 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 are as anticoagulants either embedded in or physically linked to materials used in the manufacture of devices used in blood collection, blood circulation, and blood storage, such as catheters, blood dialysis machines, blood collection syringes and tubes, blood lines and stents.
Inventors:
One, ihua
Le, Chambao
Tom Kuzak, Bruce E.
Sol, Richard M.
Sparrino, John Sea.
Bourne, Roger F.
Le, Chambao
Tom Kuzak, Bruce E.
Sol, Richard M.
Sparrino, John Sea.
Bourne, Roger F.
Application Number:
JP2002518184A
Publication Date:
February 26, 2004
Filing Date:
August 02, 2001
Export Citation:
Assignee:
3-Dimensional Pharmaceuticals, Incorporated
International Classes:
A61K31/535; A61L33/00; A61P1/18; A61P7/02; A61P9/10; A61P11/00; A61P29/00; A61P43/00; C07D265/02; C07D273/06; (IPC1-7): C07D265/02; A61K31/535; A61L33/00; A61P1/18; A61P7/02; A61P9/10; A61P11/00; A61P29/00; A61P43/00
Attorney, Agent or Firm:
Hidesaku Yamamoto
Takaaki Yasumura
Natsuki Morishita
Takaaki Yasumura
Natsuki Morishita