35 results about "Coagulation Factor Xa" patented technology

The present invention relates to compounds of the formula I,wherein R1; R2; R3; R4; R5, R13, R16, X and M have the meanings indicated in the claims. The compounds of formula I are valuable pharmacologically active compounds. They exhibit a strong anti-thrombotic effect and are suitable, for example, for the therapy and prophylaxis of cardio-vascular disorders like thromboembolic diseases or restenoses. They are reversible inhibitors of the blood clotting enzymes factor Xa (FXa) and thrombin and can in general be applied in conditions in which an undesired activity of factor Xa and / or thrombin are present or for the cure or prevention of which an inhibition of factor Xa and thrombin are intended. The invention furthermore relates to processes for the preparation of compounds of the formula I, their use, in particular as active ingredients in pharmaceuticals, and pharmaceutical preparations comprising them.

Production of specific anticoagulant substance and its use disclosed. The process is carried out by connecting amino acid sequence into anticoagulant substance, which is recognized and cracked by zymoplasm or blood coagulation factor Xa, or connecting anticoagulant substance with amino acid sequence as oligopeptide to obtain final product.

The present invention relates to compounds of the formula I,wherein R1; R2; R3; R4; R5, R16, X and M have the meanings indicated in the claims. The compounds of formula I are valuable pharmacologically active compounds. They exhibit a strong anti-thrombotic effect and are suitable, for example, for the therapy and prophylaxis of cardio-vascular disorders like thromboembolic diseases or restenoses. They are reversible inhibitors of the blood clotting enzymes factor Xa and thrombin and can in general be applied in conditions in which an undesired activity of factor Xa and / or thrombin are present or for the cure or prevention of which an inhibition of factor Xa and thrombin are intended. The invention furthermore relates to processes for the preparation of compounds of the formula I, their use, in particular as active ingredients in pharmaceuticals, and pharmaceutical preparations comprising them.

Compositions are provided comprising recombinant variants of the human clotting Factor Xa. Such compositions include a wide variety of isoforms and post-translational modifications of FXa and are useful for treating subjects in need of hemostasis.

Provided is a method for preparing (S)-5-chloro-N-((3-(4-(5,6-dihydro-4H-1,2,4-oxadiazin-3-yl)phenyl)-2-oxooxazolidin-5-yl)methyl)thiophene-2-carboxamide derivatives of Formula (I) which are useful as blood coagulation factor Xa inhibitors, and said method using 1-fluoro-4-nitrobenzen as a starting material. According to the method of the present invention, (S)-5-chloro-N-((3-(4-(5,6-dihydro-4H-1,2,4-oxadiazin-3-yl)phenyl)-2-oxooxazolidin-5-yl)methyl)thiophene-2-carboxamide derivatives of Formula (I) which are useful as blood coagulation factor Xa inhibitors can be prepared in a high purity and a high yield.

The invention relates to a preparation method of an antithrombotic drug, belongs to the technical field of medicinal chemistry and in particular relates to a preparation method of a direct coagulationfactor Xa inhibitor, which is shown as the following reaction. Compared with the existing process, the preparation method has the advantages of mild reaction condition in each step, high yield, simplicity and convenience operation, stable process and suitability for large-scale industrial production.

Disclosed are: a method for preparing a 5-chloro-N-({(5S)-2-oxo-3-[4-(5,6-dihydro-4H-[1,2,4]triazin-1-yl)phenyl]-1,3-oxazolidin-5-yl}-methyl)thiophene-2-carboxamide derivative, which is a inhibitor of blood coagulation factor Xa, in a high purity and yield; and a novel intermedicate used therein.

A kit for quantitative detection of heparin by thromboelastography, comprising a buffer, blood coagulation factor Xa, rabbit brain fat coagulation, blood coagulation factor activator, support agent, biological preservative; the preparation method includes: preparing buffer solution, blood coagulation factor Xa stock solution, Blood coagulation factor activator stock solution, biological antiseptic solution, rabbit brain lipid coagulation stock solution; take support agent and add buffer solution to prepare support solution; add coagulation factor Xa, coagulation factor activator, rabbit brain fat coagulation stock solution according to kit specifications In the support solution, add biological preservative solution after mixing, and then add buffer solution to the specified amount, mix and freeze-dry. The invention can quantitatively detect the heparin in the sample by the thromboelastography detection method, the correlation is good in the linear range, meets the detection limit standard of heparin, and the coefficient of variation is not more than 10%. There is also no requirement for the integrity of the protein in the waterfall, which simplifies the inspection process and is convenient for doctors and patients.

The invention relates to a high purity coagulation factor Xa (FXa or activated coagulation factor X) preparation and an activation and purification process to obtain the FXa of high purity and high degree of activation without the addition of proteinaceous activators during manufacturing.

The invention relates to the field of medicines related to venous thromboembolic diseases, and particularly relates to an FXa inhibitor containing a bicycle-amide structure, a preparation method of the FXa inhibitor and application of the FXa inhibitor in preparation of medicines for treating venous thromboembolic diseases. The inhibitor structure is as shown in the specification.

The invention relates to the field of medicines related to venous thromboembolic diseases, and particularly relates to an FXa inhibitor containing a bicycle-amide structure, a preparation method of the FXa inhibitor and application of the FXa inhibitor in preparation of medicines for treating venous thromboembolic diseases. The inhibitor structure is as shown in the specification.

The present invention relates to novel oxazolidinone derivatives with cyclic amidines, and prodrugs, hydrates, solvates, isomers and pharmaceutically acceptable salts thereof, and processes for preparing the same, and pharmaceutical compositions comprising the same. The oxazolidinone derivatives with cyclic amidines, and prodrugs, hydrates, solvates, isomers and pharmaceutically acceptable salts thereof can be usefully employed as an anticoagulant for treating thromboembolism and tumors via inhibition of coagulation factor Xa.

The invention relates to a polypeptide for inhibiting an activity of bacillus subtilis transglutaminase (BTG) and its screening method and use. The polypeptide has an amino acid sequence shown in the formula of SEQ ID No: 1. The polypeptide provided by the invention can inhibit the activity of BTG by a fusion protein and has an inhibition rate more than 60%. Through the polypeptide, the activity of expressed BTG having strong cytotoxicity is inhibited in a host cell and then is recovered after the inhibitor is removed under the action of a blood coagulation factor Xa.

The present invention relates to compounds of the formula I,wherein R1; R2; R3; R4; R5, R16, X and M have the meanings indicated in the claims. The compounds of formula I are valuable pharmacologically active compounds. They exhibit a strong anti-thrombotic effect and are suitable, for example, for the therapy and prophylaxis of cardio-vascular disorders like thromboembolic diseases or restenoses. They are reversible inhibitors of the blood clotting enzymes factor Xa and thrombin and can in general be applied in conditions in which an undesired activity of factor Xa and / or thrombin are present or for the cure or prevention of which an inhibition of factor Xa and thrombin are intended. The invention furthermore relates to processes for the preparation of compounds of the formula I, their use, in particular as active ingredients in pharmaceuticals, and pharmaceutical preparations comprising them.

The invention relates to a new compound represented by formula (I) or a pharmaceutically acceptable salt thereof. In the formula (I), X is selected from a 3-9-membered carbon ring or a benzo ring thereof and a 4-10-membered heterocyclic ring or a benzo ring thereof; Y and Z are respectively independently selected from 4-9-membered saturated heterocyclic rings; and R1-3 are respectively independently selected from H, F, Cl, Br, I, CN, OH, SH, NH2, CHO and COOH, or are selected from R01 substituted C1-10 alkyl or heteroalkyl groups, C3-C10 cycloalkyl or heterocycloalkyl groups, and C3-10 cycloalkyl or heterocycloalkyl group substituted C1-10 alkyl or heteroalkyl groups. The compound can be used as an anticoagulant for treating and preventing thrombus abnormity diseases. The strong blood coagulation factor Xa inhibitor is provided to meet practical demands of selectivity and the strong inhibitor of the blood coagulation factor Xa.

The invention relates to the field of medicines related to venous thromboembolic diseases, and particularly relates to an FXa inhibitor containing a bicycle-amide structure, a preparation method of the FXa inhibitor and application of the FXa inhibitor in preparation of medicines for treating venous thromboembolic diseases. The inhibitor structure is as shown in the specification.