71 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.

The present invention relates to diamine compounds which inhibit activated blood coagulation factor X and exhibit an anticoagulant effect and there uses for treating various diseases based on thromboembolism.

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.

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.

It is desired to provide a pharmaceutical composition containing a compound represented by formula (I) or a pharmaceutically acceptable salt thereof, or a solvate thereof, which exhibits an inhibitory effect on activated blood coagulation factor X, and is useful as an agent for preventing and / or treating thrombosis, wherein the pharmaceutical composition exhibits favorable dissolution properties. The present invention provides a method for producing a pharmaceutical composition containing a compound represented by formula (I), comprising the step of mixing a compound represented by formula (I) or a pharmaceutically acceptable salt thereof, or a solvate thereof, one or more excipients selected from the group consisting of a sugar alcohol and a water-swelling additive, a disintegrant, and a binder under conditions for keeping the maximum water content of the granules during granulation at 10% or less.

The present invention relates to a 5-amidino-2-hydroxybenzenesulfonamide derivative represented by the general formula: wherein R1 is a hydrogen atom or an optionally substituted lower alkyl group; R2 is a di(lower alkyl)amino group, a lower alkyl group, a cycloalkyl group, an optionally substituted aryl group, an optionally substituted heterocycloalkyl group, or an optionally substituted aromatic heterocyclic group; T is an oxygen atom, a sulfur atom, a sulfonyl group etc.; Q is a hydrogen atom or an optionally substituted lower alkyl group; and Z is a hydrogen atom, 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, a pharmaceutical use thereof and an intermediate thereof.

The present invention relates to an improved and industrially advantageous process for the preparation of (1S, 4S, 5S)-4-bromo-6-oxabicyclo[3.2.1]octan-7-one represented by the following formula (I) which is a key intermediate in the synthesis of edoxaban, a compound that exhibits an inhibitory effect on activated blood coagulation factor X (also referred to as activated factor X or FXa), and is useful as a preventive and / or therapeutic drug for thrombotic diseases. The process includes reacting (1S)-cyclohex-3-ene-1-carboxylic acid of formula (II) with a brominating agent selected from the group consisting of N-bromosuccinimide or 1,3-dibromo-5,5-dimethylhydantoin in the presence of a base selected from calcium oxide or calcium hydroxide in a solvent selected from the group comprising of dichloromethane, toluene, tetrahydrofuran, ethy1 acetate, hexanes, cyclopentyl methyl ether (CPME) or a mixture thereof to get (1S, 4S, 5S)-4-bromo-6-oxabicyclo[3.2.1]octan-7-one of formula (I).