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88 results about "Benzamidine" patented technology
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Benzamidine is a reversible competitive inhibitor of trypsin, trypsin-like enzymes and serine proteases. It is often used as a ligand in protein crystallography to prevent proteases from degrading a protein of interest; the triangular diamine group at the bottom gives it a very obvious 'stick-man' shape which shows up in difference density maps. The benzamidine moiety is also found in some pharmaceuticals, like dabigatran.
Compositions for Regulation of Hair Growth
InactiveUS20080254055A1Reduce frequencyImprove shaving efficiencyBiocideCosmetic preparationsPersonal carePhytic acid
Personal care composition comprising at least one hair growth regulating compound selected from the group consisting of glyceryl dilaurate, apigenin, tetrahydrocurcumin, oleanolic acid, azelaic acid, sulforaphane, canavanine, pyridoxal 5-phosphate, phytic acid, tannic acid, grape seed extract, NG-nitro-L-arginine-methyl ester, benzamidine, sodium butyrate, betulinic acid, polyornithine, polyarginine, fisetin, jasmonates, methyl-jasmonate, cis-jasmone, caffeic acid phenethyl ester, delphinidin, ethyl abietate, esculetin, sorbic acid methyl ester, canaline, N-formyl-methionine, N-formyl-alanine, taurine, palmitoyl carnitine, undecanol, undecylenic acid, rutin, fusidic acid, phenyl pyruvic acid, L-isoleucine, phenyl glycine, silibinin, silymarin, L-ascorbic acid-6-palmitate, N-undecylenoyl-L-phenylalanine, and salts, derivatives and mixtures of any of the foregoing; and a dermatologically-acceptable carrier.
Owner:THE PROCTER & GAMBLE COMPANY
Benzamidine derivatives
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.
Owner:SANKYO CO LTD
Liquid, aqueous, pharmaceutical compositions of factor VII polypeptides
InactiveUS20060063714A1Good storage stabilityPeptide/protein ingredientsInorganic non-active ingredientsFactor VIIaClotting factor deficiency
The invention relates to a liquid, aqueous pharmaceutical composition comprising a Factor VII polypeptide (e.g. human Factor VIIa) and a buffering agent; wherein the molar ratio of non-complexed calcium ions (Ca2+) to the Factor VII polypeptide is lower than 0.5. The composition may further comprise a stabilizing agent (e.g. copper or magnesium ions, benzamidine, or guanidine), a non-ionic surfactant, a tonicity modifying agent, an antioxidant and a preservative. The composition is useful for treating a Factor VII-responsive syndrome, such as bleeding disorders, including those caused by clotting Factor deficiencies (e.g. haemophilia A, haemophilia B, coagulation Factor XI deficiency, coagulation Factor VII deficiency); by thrombocytopenia or von Willebrand's disease, or by clotting Factor inhibitors, and intra cerebral haemorrhage, or excessive bleeding from any cause. The preparations may also be administered to patients in association with surgery or other trauma or to patients receiving anticoagulant therapy.
Owner:NOVO NORDISK AS
Dipeptide benzamidine as a kininogenase inhibitor
InactiveUS6440937B1Enhance pharmacological effectsPrevent adhesion and metastasisFibrinogenDipeptide ingredientsDiseaseBenzamidine
Owner:ABBOTT GMBH & CO KG
Process for the Preparation of the Salts of 4-(Benzimidazolylmethylamino)-Benzamides
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.
Owner:BOEHRINGER INGELHEIM INT GMBH
Methods for producing cyclic benzamidine derivatives
InactiveUS20060058370A1Operational securityQuality improvementBiocideSulfonic acid esters preparationPhenacylMorpholine
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.
Owner:EISIA R&D MANAGEMENT CO LTD
Method of treating or preventing osteoporosis comprising administering to a patient in need thereof an effective amount of pharmacuetical composition comprising benzamidine derivative or it's salt, and bisphosphonate
The present invention provides a method of treating or preventing osteoporosis comprising administering to a patient in need thereof an effective amount of pharmaceutical composition comprising benzamidine derivative or its salt, and bisphosphonate for the purpose of using simultaneously, separately, or sequentially as active ingredients. As a prophylactic or therapeutic composition for osteoporosis, the combination treatment of the benzamidine derivative and the bisphosphonate compound exhibits excellent inhibitory effect on osteoclast differentiation than the total effect of each individual treatment, thereby being used for the prevention or treatment of osteoporosis.
Owner:DONG WHA PHARM CO LTD
Combination comprising thrombin agent and examining agent
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.
Owner:SYSMEX CORP
Process for the Preparation of 4-(Benzimidazolylmethylamino)-Benzamides and the Salts Thereof
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 and ii) 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 and ii) without prior isolation of the intermediate product of the carbonylation the desired salt is isolated.
Owner:BOEHRINGER INGELHEIM INT GMBH
Oral Preparation Having Improved Bioavailability
InactiveUS20070254930A1Improve bioavailabilityPowder deliveryBiocideCarmellose CalciumAlkaline earth metal
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.
Owner:DONG WHA PHARM CO LTD
Process for the preparation of 4-(benzimidazolylmethylamino)-benzamides and the salts thereof
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.
Owner:BOEHRINGER INGELHEIM INT GMBH
Process for the preparation of the salts of 4-(benzimidazolylmethylamino)-benzamides
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.
Owner:BOEHRINGER INGELHEIM INT GMBH
Benzamidine derivatives
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
Owner:AJINOMOTO CO INC
System and method for transdermal delivery of an anticoagulant
InactiveUS20050273047A1Precise dose controlOrganic active ingredientsElectrotherapyMedicineBenzamidine
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 / cm2. 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.
Owner:ALZA CORP
Benzamidine Derivatives for Treatment and Prevention of Cancer Therapy Induced Mucositis
InactiveUS20080194877A1Isocyanic acid derivatives preparationOrganic compound preparationCancer preventionSide effect
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
Owner:ROTTAPHARM SPA
Liquid, aqueous pharmaceutical compositions of factor VII polypeptides
InactiveUS20060205648A1Improve stabilityIncrease storage spaceBiocidePeptide/protein ingredientsArginineBenzamidine
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.
Owner:NOVO NORDISK AS
Method, composition and device for sampling natriuretic peptides in a biological fluid
ActiveUS20090215182A1Easy to manufactureInhibiting proteolysisPreparing sample for investigationMass spectrometric analysisAEBSFEnzyme Inhibitor Agent
Disclosed is a composition that synergistically prevents proteolysis or modification of peptides in sampled biological fluids using sulfonyl fluoride family protease inhibitors at high concentrations combined with at least one additional protease inhibitor of a different type, preferably a broad spectrum protease inhibitor, and a chelator. A preferred embodiment uses AEBSF at 10 mM, Benzamidine at 20 mM and EDTA as the chelator. The disclosed composition may be combined with other protease inhibitors to further modulate its specificity, for instance to additionally target acidic proteases. Additional protease inhibitors, reducing agents, stabilizers and buffering agents may be combined with the disclosed compositions in devices for sampling or testing biological fluids for levels of peptides of interest, or methods therefore. The disclosed devices, compositions and methods are of particular use in sampling and testing for the level of natriuretic peptides.
Owner:SCIOS +1
Synthetic technology for 3-phenyl-5-(thiophene-2-yl)-1,2,4-oxadiazole
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.
Owner:WUHAN INSTITUTE OF TECHNOLOGY
Methods for producing cyclic benzamidine derivatives
InactiveUS7375236B2Efficient productionSimple procedureBiocideSulfonic acid esters preparationImidePhenacyl
Owner:EISIA R&D MANAGEMENT CO LTD
Novel synthetic method of o-ethoxyl benzamidine hydrochloride
InactiveCN103086920ASimple processRaw materials are cheap and easy to getOrganic chemistryHydroxylamine HydrochlorideAcetone
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.
Owner:SHANDONG UNIV OF SCI & TECH
Composition and application thereof as scurf-eliminating and itch-stopping agent
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.
Owner:南京枫华投资管理有限公司
Novel benzamidine derivative, process for the preparation thereof and pharmaceutical composition comprising same
InactiveUS20090054642A1Good effectPrevent and treat osteoporosisOrganic active ingredientsBiocideBenzamidineTrabecular bone
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.
Owner:DONG WHA PHARM CO LTD
3-aminobenzo[d]isothiazole and derivatives thereof, and synthetic method thereof
ActiveCN108084110AWide variety of sourcesStable molecular structureOrganic chemistryAir atmosphereBenzene
The invention mainly relates to 3-aminobenzo[d]isothiazole and derivatives thereof and a synthetic method thereof. Benzamidine compounds and elemental sulfur are converted into 3-aminobenzo[d]isothiazole and the derivatives thereof only under the action of an alkali and in an air atmosphere without use of a catalyst during synthesis. The problems that a conventional synthetic method of a functionalized 3-aminobenzo[d]isothiazole compound has complex synthetic steps, requires a multistep synthesis process to complete, and also requires use of metal catalysts or peroxides, as well as has low yield or harsh reaction conditions are overcome. The synthetic method has the characteristics of simple reaction system, mild reaction conditions, less reaction equipment, simple experimental operation,wide sources of used materials, high yield, easy expanding of users and application, high utilization value of products, expectable prospects of commercialization of the market and the like.
![3-aminobenzo[d]isothiazole and derivatives thereof, and synthetic method thereof](https://images-eureka-patsnap-com.libproxy1.nus.edu.sg/patent_img/57dbe7e5-b2b9-4c28-ab61-c223dfab338c/HSA0000156127230000011.png "3-aminobenzo[d]isothiazole and derivatives thereof, and synthetic method thereof")
![3-aminobenzo[d]isothiazole and derivatives thereof, and synthetic method thereof](https://images-eureka-patsnap-com.libproxy1.nus.edu.sg/patent_img/57dbe7e5-b2b9-4c28-ab61-c223dfab338c/HSA0000156127230000012.png "3-aminobenzo[d]isothiazole and derivatives thereof, and synthetic method thereof")
![3-aminobenzo[d]isothiazole and derivatives thereof, and synthetic method thereof](https://images-eureka-patsnap-com.libproxy1.nus.edu.sg/patent_img/57dbe7e5-b2b9-4c28-ab61-c223dfab338c/HSA0000156127230000021.png "3-aminobenzo[d]isothiazole and derivatives thereof, and synthetic method thereof")
Owner:XIANGTAN UNIV
Liquid, Aqueous Pharmaceutical Compositions of Factor VII Polypeptides
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.
Owner:NOVO NORDISK HEALTH CARE AG
Preparation technology of interventional thrombolytic biological product namely urechis unicinctus plasmin
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.
Owner:陈良海
Benzamidine derivative as well as preparation method and application thereof
ActiveCN109761847AOvercome the aggregation quenching problemImprove performanceSolid-state devicesSemiconductor/solid-state device manufacturingReaction rateGreen chemistry
The invention discloses a benzamidine derivative as well as a preparation method and an application thereof. The benzamidine derivative has aggregation-induced emission performance, and has quite highfluorescence quantum efficiency being 50% or higher in a solid thin-film state, and therefore, the common problem of aggregation quenching of a luminescent material at present is solved. An OLED (organic light-emitting device) prepared from the material as a luminescent layer has excellent performance. Besides, by means of photooxidation in the preparation method, the reaction rate and the yieldare high, any catalyst is not needed, and the preparation method accords with the characteristics of green chemistry.
Owner:ZHEJIANG UNIV OF TECH
Method of treating or preventing osteoporosis comprising administering to a patient in need thereof an effective amount of pharmaceutical composition comprising benzamidine derivatives or their salts, and alendronic acid or its salt
InactiveUS20100029595A1Evaluate effectBiocidePhosphorous compound active ingredientsBenzamidineOsteopoikilosis
The present invention relates to a pharmaceutical composition for preventing and treating osteoporosis, comprising N-hydroxy-4-{5-[4-(5-isopropyl-2-methyl-1,3-thiazol-4-yl)phenoxy]pentoxy}benzamidine, 4-{5-[4-(5-isopropyl-2-methyl-1,3-thiazol-4-yl)phenoxy]pentoxy}benzamidine, or salts thereof, and alendronic acid or a salt thereof.As a prophylactic or therapeutic composition for osteoporosis, the combination treatment of N-hydroxy-4-{5-[4-(5-isopropyl-2-methyl-1,3-thiazol-4-yl)phenoxy]pentoxy}benzamidine, 4-{5-[4-(5-isopropyl-2-methyl-1,3-thiazol-4-yl)phenoxy]pentoxy}-benzamidine, or salts thereof and alendronic acid or a salt thereof exhibits excellent inhibitory effect on osteoclast differentiation, as compared to each individual treatment, thereby being useful for the prevention or treatment of osteoporosis.
Owner:DONG WHA PHARM CO LTD
Benzamidine derivative, process for the preparation thereof and pharmaceutical composition comprising same
InactiveUS7943646B2Good effectPrevent and treat osteoporosisBiocideOrganic active ingredientsBenzamidineTrabecular bone
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.
Owner:DONG WHA PHARM CO LTD
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