Title:
SERINE PROTEASE INHIBITOR
Document Type and Number:
WIPO Patent Application WO/2001/003740
Kind Code:
A1
Abstract:
A serine protease inhibitor capable of selectively inhibiting the target serine protease activity alone. This serine protease inhibitor binds to the substrate of serine protease competitively with the serine protease to thereby inhibit the reaction between the serine protease and the substrate. This inhibitor specifically binds to the substrate of the target serine protease to thereby inhibit the activity of the serine protease. This serine protease inhibitor is useful as an antithrombotic agent, a fibrinolysin inhibitor, an anti-digestive enzyme agent and a remedy for disseminated intravascular coagulation.
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Inventors:
SHIMA MIDORI (JP)
KOIDE TAKEHIKO (JP)
HOSOKAWA KAZUYA (JP)
SUZUKI TOYOAKI (JP)
NAGATA MASANORI (JP)
KOIDE TAKEHIKO (JP)
HOSOKAWA KAZUYA (JP)
SUZUKI TOYOAKI (JP)
NAGATA MASANORI (JP)
Application Number:
PCT/JP2000/004595
Publication Date:
January 18, 2001
Filing Date:
July 10, 2000
Export Citation:
Assignee:
FUJIMORI KOGYO CO (JP)
SHIMA MIDORI (JP)
KOIDE TAKEHIKO (JP)
HOSOKAWA KAZUYA (JP)
SUZUKI TOYOAKI (JP)
NAGATA MASANORI (JP)
SHIMA MIDORI (JP)
KOIDE TAKEHIKO (JP)
HOSOKAWA KAZUYA (JP)
SUZUKI TOYOAKI (JP)
NAGATA MASANORI (JP)
International Classes:
A61K38/55; A61P1/00; A61P7/02; A61P7/04; A61P43/00; C07K14/81; C12N9/64; A61K38/00; (IPC1-7): A61K45/00; A61K38/36; A61P1/00; A61P7/02; A61P7/04; A61P43/00
Foreign References:
| EP0882789A2 | 1998-12-09 |
Other References:
SUIDAN,HANA S. ET AL.: "The serine protease granzyme A does not induce platelet aggregation but inhibits responses triggered by thrombin", BIOCHEM. J., vol. 315, no. 3, 1996, pages 939 - 945, XP002931775
OLSON,STEVEN T. ET AL.: "Role of the catalytic serine in the interactions of serine proteinases with protein inhibitors of the serpin family. Contribution of a covalent interaction to the binding energy of serpin-proteinase complexes", J. BIOL. CHEM., vol. 270, no. 50, 1995, pages 30007 - 30017, XP002931776
HARMON J.T. AND JAMIESON G.A.: "Activation of platelets by alpha-thrombin is a receptor-mediated event. D-phenylalanyl-L-prolyl-L-arginine chloromethyl ketone-thrombin, but not N alpha-tosyl-L-lysine chloromethyl ketone-thrombin, binds to the high affinity thrombin receptor", J. BIOL. CHEM., vol. 261, no. 34, 1986, pages 15928 - 15933, XP002931777
ASHTON R.E. AND SCHERAGA H.A.: "Preparation and characterization of anhydrothrombin", BIOCHEMISTRY, vol. 34, no. 19, 1995, pages 6454 - 6463, XP002931778
TOMONO T.: "Preparation of anhydrothrombin and its interaction with plasma antithrombin III", NIPPON KETSUEKI GAKKAI ZASSHI (ACTA HAEMATOLOGICA JAPONICA), vol. 49, no. 4, 1986, pages 969 - 979, XP002931779
PEI G. ET AL.: "Expression, isolation and characterization of an active site (serine 528----alanine) mutant of recombinant bovine prothrombin", J. BIOL. CHEM., vol. 266, no. 15, 1991, pages 9598 - 9604, XP002931780
NIKKEI BIO TECH.: "Nikkei bio saishin yougo jiten, the 4th printing", 1995, NIKKEI BP K.K., XP002931781
GOODMAN & GILMAN'S: "The pharmacological basis of therapeutics", MCGRAW-HILL, XP002931782
See also references of EP 1195163A4
OLSON,STEVEN T. ET AL.: "Role of the catalytic serine in the interactions of serine proteinases with protein inhibitors of the serpin family. Contribution of a covalent interaction to the binding energy of serpin-proteinase complexes", J. BIOL. CHEM., vol. 270, no. 50, 1995, pages 30007 - 30017, XP002931776
HARMON J.T. AND JAMIESON G.A.: "Activation of platelets by alpha-thrombin is a receptor-mediated event. D-phenylalanyl-L-prolyl-L-arginine chloromethyl ketone-thrombin, but not N alpha-tosyl-L-lysine chloromethyl ketone-thrombin, binds to the high affinity thrombin receptor", J. BIOL. CHEM., vol. 261, no. 34, 1986, pages 15928 - 15933, XP002931777
ASHTON R.E. AND SCHERAGA H.A.: "Preparation and characterization of anhydrothrombin", BIOCHEMISTRY, vol. 34, no. 19, 1995, pages 6454 - 6463, XP002931778
TOMONO T.: "Preparation of anhydrothrombin and its interaction with plasma antithrombin III", NIPPON KETSUEKI GAKKAI ZASSHI (ACTA HAEMATOLOGICA JAPONICA), vol. 49, no. 4, 1986, pages 969 - 979, XP002931779
PEI G. ET AL.: "Expression, isolation and characterization of an active site (serine 528----alanine) mutant of recombinant bovine prothrombin", J. BIOL. CHEM., vol. 266, no. 15, 1991, pages 9598 - 9604, XP002931780
NIKKEI BIO TECH.: "Nikkei bio saishin yougo jiten, the 4th printing", 1995, NIKKEI BP K.K., XP002931781
GOODMAN & GILMAN'S: "The pharmacological basis of therapeutics", MCGRAW-HILL, XP002931782
See also references of EP 1195163A4
Attorney, Agent or Firm:
Hatta, Mikio (Nibancho Chiyoda-ku Tokyo, JP)
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