87 results about "Benzamidine" patented technology

A compound of a formula (1) and pharmacologically acceptable salts thereof: wherein R1 represents hydrogen, halogen, alkyl or hydroxyl; R2 represents hydrogen or halogen; R3 represents hydrogen, alkyl, hydroxyl, carboxyalkyl, alkoxycarbonylalkyl, alkylsulfonyl, alkoxycarbonylalkylsulfonyl, craboxyalkylsulfonyl or carboxyalkylcarbonyl; each of R4 and R5 represents hydrogen, halogen, alkyl, carbamoyl, alkoxy, carboxyl, alkoxycarbonyl, monoalkylcarbamoyl or dialkylcarbamoyl; R6 represents a heterocycle, hydrogen, alkyl, cycloalkyl, aralkyl, carboxyalkyl, alkoxycarbonyalkyl, aliphatic or aromatic acyl, carbamoyl, alkylsulfonyl, aryl, formimidoyl, 1-iminoalkyl, N-alkylforminidoyl or iminoarylmethyl; each of R7 and R8 represents hydrogen or alkyl; n represents 0, 1 or 2. The compound exhibits excellent activated blood coagulation factor X inhibitory activity and prevents or treats blood coagulation-related diseases.

Compounds of the formula Iwhere R, R1, R2, R3, R4, R5 and R6, and l, m and n have the meanings stated in the description, and their preparation are described. The novel compounds are suitable for controlling diseases.

The invention relates to a process for preparing a salt of an optionally substituted 4-benzimidazol-2-ylmethylamino)-benzamidine, characterised in that (a) an optionally correspondingly substituted diaminobenzene is condensed with 2-[4-(1,2,4-oxadiazol-5-on-3-yl)-phenylamino]-acetic acid, b) i) the product thus obtained is hydrogenated, ii) optionally the amidino group is carbonylated, without isolating the intermediate product of the hydrogenation beforehand and iii) without prior isolation of the intermediate product of the carbonylation the desired salt is isolated.

Provided is a stabilized thrombin containing a test reagent and the test reagent kit. The test reagent contains thrombin and an inhibitor having thrombin inhibiting effect, the inhibitor is a protease antagonist having thrombin inhibiting effect, and is preferably selected from the group consisting of benzamidine, p-aminobenzamidine, m-aminobenzamidine, phenylguanidine, argatroban, gabexate mesylate and nafamostat mesylate. The test reagent of the present invention can contain one or more compounds with thrombin stabilizing function, selected from the group consisting of a calcium ion, an organic acid, a surfactant and a protein. The test reagent is useful as a solidifying ability test reagent, especially, fibrinogen metering reagent.

The present invention relates to an oral preparation of N-hydroxy-4-{5-[4-(5-isopropyl-2-methyl-1,3-thiazol-4-yl) phenoxy]pentoxyl-benzamidine having improved bioavailability. More particularly, the present invention relates to an oral preparation comprising: N-hydroxy-4-{5-[4-(5-isopropyl-2-methyl-1,3-thiazol-4-yl) phenoxy]pentoxy}-benzamidine or pharmaceutically acceptable salt thereof; and one or more carbonates selected from the group consisting of alkalimetal carbonate, alkalimetal bicarbonate and alkaline earth metal carbonate, and / or one or more disintegrants selected from the group consisting of sodium starch glycolate, carmellose calcium and croscarmellose sodium. The oral preparation according to the present invention inhibits gelation of N-hydroxy-4-{5-[4-(5-isopropyl-2-methyl-1,3-thiazol-4-yl) phenoxy]pentoxy}-benzamidine or pharmaceutically acceptable salt thereof in the early stage of release, which increases dissolution rate and remarkably raises bioavailability.

The invention relates to a process for preparing an optionally substituted 4-benzimidazol-2-ylmethylamino)-benzamidine, characterised in that(a) an optionally correspondingly substituted diaminobenzene is condensed with 2-[4-(1,2,4-oxadiazol-5-on-3-yl)-phenylamino]-acetic acid,(b) i) the product thus obtained is hydrogenated andii) optionally the amidino group is carbonylated, without isolating the intermediate product of the hydrogenation beforehand;as well as a process for preparing a salt of an optionally substituted 4-(benzimidazol-2-ylmethylamino)-benzamidine, wherein(a) an optionally correspondingly substituted diaminobenzene is condensed with 2-[4-(1,2,4-oxadiazol-5-on-3-yl)-phenylamino]-acetic acid,(b) the product thus obtained is hydrogenated, and(c) i) optionally the amidino group is carbonylated andii) without prior isolation of the intermediate product of the carbonylation the desired salt is isolated.

The invention relates to a process for preparing a salt of an optionally substituted 4-benzimidazol-2-ylmethylamino)-benzamidine, characterised in that(a) an optionally correspondingly substituted diaminobenzene is condensed with 2-[4-(1,2,4-oxadiazol-5-on-3-yl)-phenylamino]-acetic acid,b) i) the product thus obtained is hydrogenated,ii) optionally the amidino group is carbonylated, without isolating the intermediate product of the hydrogenation beforehand andiii) without prior isolation of the intermediate product of the carbonylation the desired salt is isolated.

Benzamidine derivatives of the following formulae or analogs thereof, i.e., pharmaceutically acceptable salts thereof, are provided. These compounds or salts thereof have a blood-coagulation inhibiting effect based on an excellent effect of inhibiting the action of activated blood coagulation factor X, and they are useful as anticoagulants

Mucositis is the result of a complex process of interactive biologic phenomena that take place in both the epitelium and the submucosa, often leading to severe pain and increased risk of dangerous syste f48 mic infections. Mucositis is often a side effect during chemotherapy and radiation therapy. The benzamidine derivatives herein described are particularly effective for treating and preventing mucositis since they are acting simultaneously at the several phases that characterize this disease. Data supplied from the esp@cenet database

The invention relates to a synthetic technology for 3-phenyl-5-(thiophene-2-yl)-1,2,4-oxadiazole. The technology includes following steps: 1) filling a reaction container with 2-thiophenecarboxylic acid and a solvent with stirring and dissolving, adding thionyl chloride with a heating reflux process, wherein the mole ratio of the 2-thiophenecarboxylic acid to the thionyl chloride is 1:2-5 and refluxing reaction time is 3-20h, after the reaction being finished, removing the solvent and excess thionyl chloride in a manner of evaporation and carrying out an underpressure distillation process to obtain 2-thiophenecarbonyl chloride; 2) dissolving N-hydroxy-benzamidine in a solvent, adding 2-thiopheneacetyl chloride in a dropwise manner, carrying out a heating reaction after the dropwise addition. After the reaction being finished, pouring the reaction product into water, carrying out a layering process, carrying out an extracting process to a water layer through a solvent and carrying out a concentrating crystallization process to obtain a product. With improvement of the technology, reaction processes are reduced and reaction time is shortened. Yield of the 3-phenyl-5-(thiophene-2-yl)-1,2,4-oxadiazole is increased from 50% to more than 80% and overall yield of the 3-phenyl-5-(thiophene-2-yl)-1,2,4-oxadiazole is increased.

In the present invention, the methods of producing a fluorinated cyclic benzamidine derivative (A), or a salt thereof, comprise the step of reacting a specific novel compound with ammonia or imide.The methods of this invention for producing a morpholine-substituted phenacyl derivative (B), or a salt thereof, comprise reaction of a specific novel compound with morpholine, reaction of the product with a halogenating reagent, and deketalization of the product.The methods of this invention for a producing cyclic benzamidine derivative (C), or a salt thereof, comprise the step of coupling compound (A), or a salt thereof, with compound (B), or a salt thereof, in the presence of an ether or a hydrocarbon.The methods of this invention for recrystallizing a cyclic benzamidine derivative (C), or a salt thereof, comprise the steps of dissolving compound (C), or the salt thereof, in a mixed solvent comprising an alcohol and water, or a mixed solvent comprising an ether and water, and after dissolution, adding additional water to precipitate crystals of compound (C), or the salt thereof.

A device for transdermally delivering an anticoagulant agent by electrotransport. Preferably, the anticoagulant comprises a benzamidine or a naphthamidine derivative. A particularly preferred benzamidine derivative is a 2-[3-[4-(4-piperidinyloxy) anilino]-1-propenyl]benzamidine derivative. The devices are configured to maintain a plasma concentration of 20-80 ng / mL or providing a flux in the range of approximately 20 - 40 mg / day. Suitable current densities include 0.050 and 0.10 mA / cm<2>. Methods of the invention include delivering the anticoagulants to precisely maintain the desired plasma concentrations. The invention also comprises treating thromboembolic disease and inhibiting Factor Xa.

The invention provides a novel synthetic method of o-ethoxyl benzamidine hydrochloride, and belongs to the field of medical intermediate synthesis. The method comprises the following steps of: A, based on o-hydroxyl benzonitrile as a raw material, performing a reflux reaction on the o-hydroxyl benzonitrile and an ethylating reagent in acetone containing an acid-binding agent to obtain o-ethoxyl benzonitrile, wherein the yield is 92-97%; and B, performing a reflux reaction on o-ethoxyl benzonitrile and hydroxylamine hydrochloride in ethanol to obtain o-ethoxyl benzamidoxime, removing ethanol and adding hydrochloric acid, and performing hydrogenation reaction by stirring iron powder or zinc power at constant temperature to prepare o-ethoxyl benzamidine, wherein the yield is 85-90%. Compared with synthetic methods in the prior art, the method provided by the invention is simple and convenient in step, low in cost and available in raw materials, low requirements in production equipment and environmental condition and high in yield, and is very suitable for industrial production.

The invention discloses a composition comprising an iodopropinyl compound (I) and a benzamidine compound (II), and application of the composition as a dandruff-dispelling itch-relieving agent. The composition has excellent performances of dispelling dandruff and relieving itch, wherein the optimum weight ratio of the iodopropinyl compound (I) to the benzamidine compound (II) is between 5:95 (percent) and 95:5 (percent). The composition can form uniform dispersoid which is liquid and stable at room temperature and can be conveniently compatible with formulation so as to simplify a production process. The composition can be applied as the dandruff-dispelling itch-relieving agent to hair-use products, and has the optimum dosage of between 0.001 percent and 5 percent. The composition has good effects of inhibiting and killing pityrosporum orbiculare causing dandruff, and has synergistic dandruff dispelling effect.

The present invention relates to a novel benzamidine derivative, a process for the preparation thereof, and a pharmaceutical composition comprising the same. The benzamidine derivative of the present invention effectively inhibits osteoclast differentiation at an extremely low concentration, and greatly increases the trabecular bone volume, and thus it can be advantageously used for the prevention and treatment of osteoporosis.

The present invention is directed to liquid, aqueous pharmaceutical compositions stabilised against chemical and / or physical degradation containing Factor VII polypeptides, and methods for preparing and using such compositions, as well as vials containing such compositions, and the use of such compositions in the treatment of a Factor VII-responsive syndrome. The main embodiment is represented by a liquid, aqueous pharmaceutical composition comprising at least 0.01 mg / mL of a Factor VII polypeptide (i); a buffering agent (ii) suitable for keeping pH in the range of from about 4.0 to about 9.0; and at least one stabilising agent (iii) comprising a —C(═N—Z1—R1)—NH—Z2—R2 motif, e.g. benzamidine compounds and guanidine compounds such as arginine.

The invention relates to a preparation technology of an interventional thrombolytic biological product namely urechis unicinctus plasmin. The technology comprises the following steps: freezing coelomic fluid of urechis unicinctus, then subjecting the fluid to centrifugation and suction filtration, carrying out freeze drying in vacuum to obtain a coarse product, subjecting the coarse product to DEAE (diethyl amino ethanol)-Sepahcel (cellulose glucan gel) anion exchange chromatography, Sephadex (hydroxypropyl glucan gel)G-75 chromatography, benzamidine-Sepharose (agarose gel) chromatography, and freeze drying to further verify that the coarse product is plasmin, and then carrying out an interventional thrombolytic experiment on a rat carotid and cerebral artery embolism model to prove that the urechis unicinctus plasmin can completely dissolve thrombus and does not have any side effect such as allergy, and the like.

The present invention relates to a novel benzamidine derivative, a process for the preparation thereof, and a pharmaceutical composition comprising the same. The benzamidine derivative of the present invention effectively inhibits osteoclast differentiation at an extremely low concentration, and greatly increases the trabecular bone volume, and thus it can be advantageously used for the prevention and treatment of osteoporosis.