New peptide derivatives

Details New peptide derivatives New peptide derivatives

C - Chemistry, Metallurgy

07

K

C07K 5/06 (2006.01) A61K 31/395 (2006.01) A61K 38/05 (2006.01) A61P 7/02 (2006.01) A61P 29/00 (2006.01) C07C 257/16 (2006.01) C07C 271/64 (2006.01) C07D 205/04 (2006.01) C07D 207/09 (2006.01) C07D 211/26 (2006.01) C07D 211/60 (2006.01) C07D 239/14 (2006.01) C07D 401/06 (2006.01) C07K 5/02 (2006.01) C07K 5/065 (2006.01) C07K 5/078 (2006.01) A61K 31/616 (2006.01)

Patent

CA 2162900

The invention relates to new competitive inhibitors of trypsin-like serine proteases, their synthesis, pharmaceutical compositions contain-ing the compounds as active ingredients, and the use of the compounds as thrombin inhibitors, anticoagulants and anti-inflammatory inhibitors for prophylaxis and treatment of related dis-eases, according to the formulas (I): A1-A2--NH-(CH2)n-B and (V): A1-A2-NH-(CH2)n-B-D wherein A1 represents a structural fragment of formulas (IIa), (IIb), (IIc), (IId), (IIe), A2 rep-resents a structural fragment of formulas (IIIa), (IIIb), (IIIc), B represents a structural fragment of formulas (IVa), (IVb), (IVc), (IVd). Further described are novel compounds, the new use of compounds and especially new structural frag-ment in synthesis of pharmaceutical compounds.

L'invention concerne de nouveaux inhibiteurs compétitifs des sérine protéases du type trypsine, leur synthèse, des préparations pharmaceutiques renfermant ces composés comme principes actifs, et l'utilisation de ces composés comme inhibiteurs de la thrombine, anticoagulants et inhibiteurs anti-inflammatoires pour la prophylaxie et le traitement de maladies apparentées à la thrombose. Lesdits inhibiteurs correspondent aux formules (I): A<1>-A<2>-NH-(CH2)n-B et (V): A<1>-A<2>-NH-(CH2)n-B-D dans lesquelles A<1> représente un fragment structural des formules (IIa), (IIb), (IIc), (IId), (IIe), A<2> représente un fragment structural des formules (IIIa), (IIIb), (IIIc) et B représente un fragment structural des formules (IVa), (IVb), (IVc), (IVd). L'invention décrit en outre des nouveaux composés, une nouvelle utilisation de ceux-ci et particulièrement du nouveau fragment structural dans la synthèse de composés pharmaceutiques.

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