Title:
ペプチドおよび/またはタンパク質、並びにその治療用および/または予防用医薬成分を調製するための使用
Document Type and Number:
Japanese Patent JP4181874
Kind Code:
B2
Abstract:
Peptides or proteins (I), based on the alpha - and beta -chain sequences of fibrin/fibrinogen, or their salts, amides and/or mixtures with each other or other materials, have therapeutic and/or preventive use in human or veterinary medicine. Peptides or proteins of formula R 1R 2N-CH 2-C(O)-Z 1-Z 2 (I), or their salts, amides and/or mixtures with each other or other materials, have therapeutic and/or preventive use in human or veterinary medicine. R 1, R 2H or up to 10C saturated or unsaturated hydrocarbyl; Z 1histidine or proline residue; and Z 2arginine residue or a peptide or protein residue (preferably of 2-30 aminoacids) having an initial arginine residue. An independent claim is included for medicaments containing (I). ACTIVITY : Antiinflammatory; antibacterial; immunosuppressive; Antirheumatic; Antiarteriosclerotic; vasotropic; Thrombolytic; anticoagulant; cytostatic; antipsoriatic. In tests for inhibition of reperfusion damage after surgically induced ischemia in rat cardiac tissue, intravenous administration of Gly-His-Arg-Pro-Leu-Asp-Lys-Lys-Arg-Glu-Glu-Ala-Pro-Ser-Leu-Arg-Pro-Ala-Pro-Pro-Pro-Ile-Ser-Gly-Gly-Gly-Tyr-Arg (Ia) at 800 Microg/kg reduced the precentage of dead tissue from 46% to 29%. MECHANISM OF ACTION : Fibrin antagonist; inhibition of fibrin-mediated adhesion of cells from the blood-stream onto vascular endothelium and/or migration of such cells into tissue; inhibition of deposition and adhesion of fibrin cleavage fragments on vascular walls.
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Inventors:
Petzelbauer, Peter
Application Number:
JP2002549711A
Publication Date:
November 19, 2008
Filing Date:
December 07, 2001
Export Citation:
Assignee:
Five Brex Medical Research and Development Game Behr
International Classes:
A61K38/17; A61K38/36; A61P7/02; A61P9/10; A61P29/00; A61P37/00; A61P37/06; C07K5/078; C07K5/083; C07K5/097; C07K5/103; C07K5/117; C07K7/00; C07K14/00; C07K14/75; A61K38/00; A61K39/00
Foreign References:
| WO1998025946A1 |
Other References:
BACH,T.L. et al.,Endothelial cell VE-cadherin functions as a receptor for the β15-42 sequence of fibrin,J. Biol. Chem.,1998年,Vol.273, No.46,p.30719-30728
BALE,M.D. et al.,Effects of fibrinogen-binding tetrapeptides on mechanical properties of fine fibrin clots,Proc. Natl. Acad. Sci. U.S.A.,1985年,Vol.82, No.5,p.1410-1413
ALLPORT,J.R. et al.,Monocytes induce reversible focal changes in vascular endothelial cadherin complex during transendothelial migration under flow,J. Cell. Biol.,2000年,Vol.148, No.1,p.203-216
BALE,M.D. et al.,Effects of fibrinogen-binding tetrapeptides on mechanical properties of fine fibrin clots,Proc. Natl. Acad. Sci. U.S.A.,1985年,Vol.82, No.5,p.1410-1413
ALLPORT,J.R. et al.,Monocytes induce reversible focal changes in vascular endothelial cadherin complex during transendothelial migration under flow,J. Cell. Biol.,2000年,Vol.148, No.1,p.203-216
Attorney, Agent or Firm:
Kenzo Hara International Patent Office
Kenzo Hara
Ryuichi Kijima
Ichiro Kaneko
Kenzo Hara
Ryuichi Kijima
Ichiro Kaneko