69 results about "Blood Coagulation Factor X" patented technology

The present inventors succeeded in constructing bispecific antibodies, which bind to both the blood coagulation factor IX/activated blood coagulation factor IX and blood coagulation factor X, and functionally substitute for blood coagulation factor VIII/activated blood coagulation factor VIII which enhances the enzymatic reaction.

Various bispecific antibodies that specifically bind to both blood coagulation factor IX/activated blood coagulation factor IX and blood coagulation factor X and functionally substitute for the cofactor function of blood coagulation factor VIII, that is, the function to promote activation of blood coagulation factor X by activated blood coagulation factor IX, were produced. From these antibodies, multispecific antigen-binding molecules having a high activity of functionally substituting for blood coagulation factor VIII were successfully discovered.

It has been demanded to provide a process for industrially producing an intermediate for a compound that exhibits an inhibitory effect on activated blood coagulation factor X and is useful as a preventive and/or therapeutic agent for thrombotic diseases. The present invention provides a process for producing the (R)-α-phenylethylamine salt of (S)-3-cyclohexene-1-carboxylic acid, comprising reacting 3-cyclohexene-1-carboxylic acid and (R)-α-phenylethylamine using a mixed solvent of water and acetone or a mixed solvent of water and ethyl acetate as a solvent.

The invention provides a method for efficiently extracting and purifying a blood coagulation factor IX and a blood coagulation factor X. The method provided by the invention comprises the following steps: collecting blood, treating, and collecting blood plasma; and extracting an IX crude extract and an X crude extract from the blood plasma, and purifying. The method is characterized in that the purifying step is to use FIX/FX-bp-Sepharose 4B to purify the blood coagulation factor IX crude extract and the blood coagulation factor X crude extract respectively through the affinity chromatography; and the affinity ligand FIX/FX-bp is selected from ACF I, ACF II or AHP. The purified blood coagulation factor IX can be directly used as a medicament and the purified blood coagulation factor X canbe directly used as a reagent.

The present invention relates to a 5-amidino-2-hydroxybenzenesulfonamide derivative represented by the general formula:

wherein R¹ is an optionally substituted lower alkyl group, an optionally substituted lower alkoxy group, an optionally substituted lower alkenyl group, a cycloalkyl group or a lower acyl group etc.;

Q is a hydrogen atom or an optionally substituted lower alkyl group; and Z is a hydrogen atom or a hydroxy group etc., or a pharmaceutically acceptable salt thereof, which exert a potent and selective activated blood coagulation factor X inhibitory activity and is useful as an agent for the prevention or treatment of a disease occurred associating an activated blood coagulation factor X, a pharmaceutical composition comprising the same and an intermediate thereof. These compounds are useful as preventives or remedies for various diseases such as brain infarction, cerebral thrombosis, cerebral embolism, TIA, cerebral vascular jerk, Alzheimer's diseases, myocardial infarction, heart attack, heart failure, thrombosis, pulmonary infarction and pulmonary embolism.

The compound hemostatic originated from venom features the main active components comprising batoxobin and blood coagulation factor X activator in the purity higher than 97 5 and weight ratio of 1-1000. The compound hemostatic has ensured curative effect, lowered proteinase consumption and thus reduced negative immune response probability.

The present invention provides a condensed furan compound of the formula (I):

wherein Ring X is benzene, pyridine, or the like; Y is an optionally substituted amino, an optionally substituted cycloalkyl, an optionally substituted aryl, an optionally substituted saturated heterocyclic group, an optionally substituted unsaturated heterocyclic group; A is a single bond, lower alkylene, lower alkenylidene, lower alkenylene or an oxygen atom; R³ is hydrogen or the like; and, R⁴ is hydrogen, or the like, or pharmaceutically acceptable salts thereof, which is useful as a medicament, particularly, as an activated blood coagulation factor X inhibitor.

The present invention provides a benzofuran derivative of the formula [1]:

wherein x is a group of the formula: —N═ or —CH═; Y is an optionally substituted amino group, an optionally substituted cycloalkyl group or an optionally substituted saturated heterocyclic group; A is a single bond, a carbon chain optionally having a double bond within or at the end(s) of the chain, or an oxygen atom; R¹ is a hydrogen atom or a halogen atom; Ring B is an optionally substituted benzene ring; and R³ is a hydrogen atom, or a pharmaceutically acceptable salt thereof, which is useful as a medicament, especially as an activated blood coagulation factor X inhibitor.

There have been demands for a pharmaceutical composition, which has good dissolvability and contains a compound represented by formula (I), a pharmaceutically acceptable salt thereof or a solvate of the compound or salt, and which has an inhibitory effect on activated blood coagulation factor X and is useful as a prophylactic and/or therapeutic agent for thrombotic diseases. Disclosed is a method for producing a pharmaceutical composition that contains a compound represented by formula (I), which comprises a step wherein a compound represented by formula (I), a pharmaceutically acceptable salt thereof or a solvate of the compound or salt, one or more excipients selected from the group consisting of sugar alcohols and water-swellable additives, a disintegrant and a binder are mixed under such conditions that the maximum water content in a granulated product is maintained at 10% or less during the granulation.

The invention provides edoxaban tosilate hydrate. Edoxaban is a micromolecule oral anticoagulant drug, and is a blood coagulation factor X(FXa) retarding agent. In the process of blood coagulation, the activated coagulation factor X(FXa) activates prothrombin (FII) into thrombin (FIIa), formation of fibrin is promoted, and thrombus is formed, so that FXa is developed as a main target of a new generation anticoagulant drug. Edoxaban is the oral anticoagulant drug by selectively, reversibly and directly inhibiting FXa in order to inhibit formation of thrombus.

To provide a compound which has an anticoagulation action based upon inhibition of activated blood coagulation factor X and is useful as an anticoagulant or an agent for prevention and treatment of diseases caused by thrombus or embolus. A diazepan derivative such as 4-[(3-carbamimidoylphenylamino)methyl]-3-[4-(4-methyl-1,4-diazepan-1-yl)benzoylamino]benzoic acid and 3-hydroxy-4′-methoxy-2-{[4-(4-methyl-1,4-diazepan-1-yl)benzoyl]amino}benzanilide or a salt thereof is an effective ingredient.

Provided are a novel amidine derivative having an activated blood coagulation factor X inhibitory activity, a production method thereof, a production intermediate therefor, and a pharmaceutical composition containing the amidine derivative. An amidinoaniline derivative represented by the following formula (1-1) or a pharmaceutically acceptable salt thereof:

<in the formula (1-1), each symbol is as defined in the Description>, and a pharmaceutical composition containing the amidinoaniline derivative or a pharmaceutically acceptable salt thereof.

The invention discloses a polyethylene glycol and anticoagulant polypeptide surface modified gold material and a preparation method. The preparation method comprises the following steps: taking gold as a base material, and linking polyethylene glycol and an anticoagulant polypeptide onto the gold surface, thereby obtaining the medical material having excellent antithrombotic property, wherein theanticoagulant polypeptide is ACH11. Researches show that, the surface hydrophilicity of the modified material in the invention is greatly improved, and the material has excellent blood compatibility.The modified material is capable of inhibiting activation of a blood coagulation factor X and resisting adhesion and activation of platelets. According to the method disclosed by the invention, an anticoagulant modified surface with excellent property is obtained, and the blood compatibility problem of the material is solved.

This invention relates to tricyclic compounds having spiro union represented by the following formula (I) or its salt which is useful as a drug, and in particular, as an inhibitor for activated blood coagulation factor X, which can be administered orally and which exhibits strong anticoagulation action. The invention also relates to a pharmacophore which was derived from the compound and is useful in molecular designing of the FXa inhibitor.

A novel hemostatic composition and a hemostatic pharmaceutical preparation are provided. A pharmaceutically stable hemostatic liquid composition comprising a mixed solution of activated blood coagulation factor VII (FVIIa) and blood coagulation factor X (FX) in a single container. The mixed solution is maintained at pH ranging from 5.0 to 6.5.