Title:
【発明の名称】プロテアーゼインヒビターとしてのアミノグアニジンおよびアルコキシグアニジン
Document Type and Number:
Japanese Patent JP2001506606
Kind Code:
A
Abstract:
Aminoguanidine and alkoxyguanidine compounds, including compounds of the formula:wherein X is O or NR<9 >and R<1>-R<4>, R<6>-R<9>, R<11>, R<12>, R, R, R, Y, Z, n and m 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 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 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:
Tom Shook, Bruce E.
Sol, Richard M.
Le, Tian Bao
Fed, Cynthia El.
Irig, Karl Earl.
Marco Tan, Thomas Peas.
Stagnaro, Thomas P.
Sol, Richard M.
Le, Tian Bao
Fed, Cynthia El.
Irig, Karl Earl.
Marco Tan, Thomas Peas.
Stagnaro, Thomas P.
Application Number:
JP52482998A
Publication Date:
May 22, 2001
Filing Date:
November 26, 1997
Export Citation:
Assignee:
"3-Dimensional Pharmaceuticals, Incorporated"
International Classes:
A01N1/02; A61K31/155; A61K31/165; A61K31/18; A61K31/225; A61K31/255; A61K31/305; A61K31/335; A61K31/341; A61K31/36; A61K31/365; A61K31/38; A61K31/381; A61K31/395; A61K31/40; C07D295/22; A61K31/44; A61K31/445; A61K31/4468; A61K31/47; A61K31/472; A61K31/495; A61K31/505; A61K31/506; A61K31/535; A61K33/42; A61L33/00; A61P7/00; A61P7/02; A61P9/10; A61P29/00; C07C69/76; C07C279/00; C07C279/10; C07C281/16; C07C291/04; C07C303/30; C07C303/40; C07C305/00; C07C309/00; C07C309/63; C07C309/73; C07C309/75; C07C309/76; C07C309/77; C07C311/08; C07C311/16; C07C311/18; C07C311/19; C07C311/21; C07C317/14; C07C317/26; C07C323/17; C07D207/14; C07D207/16; C07D207/48; C07D209/04; C07D211/22; C07D211/58; C07D211/64; C07D211/96; C07D213/24; C07D213/42; C07D215/12; C07D215/36; C07D217/12; C07D217/22; C07D229/00; C07D231/04; C07D237/02; C07D239/42; C07D239/72; C07D243/04; C07D245/02; C07D261/02; C07D263/54; C07D265/02; C07D267/04; C07D269/00; C07D285/14; C07D295/12; C07D307/02; C07D307/52; C07D311/66; C07D311/74; C07D317/08; C07D317/14; C07D317/34; C07D317/40; C07D317/64; C07D333/06; C07D333/34; C07D333/54; C07D333/62; C07D403/04; C07D413/04; C07F9/22; C07C311/17; C07D213/74; C07D307/66; A61K; C07C; C07D; (IPC1-7): C07C279/00; A61K31/155; A61P7/02; C07C303/30; C07C309/73; C07C311/18; C07D207/14; C07D211/58; C07D213/42; C07D215/36; C07D217/22; C07D239/42; C07D295/22; C07D307/52; C07D317/40; C07D333/34
Attorney, Agent or Firm:
Shusaku Yamamoto