86 results about "Benzamidine" patented technology

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.

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.

Stabilized compositions of natriuretic peptides comprise the peptide and an effective stabilizing amount of (i) an alkyl or aryl sulfonyl fluoride protease inhibitor, or (ii) benzamidine:

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.

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.

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.

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.

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.

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.

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.

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.

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.

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.