1-substituted-3-{[2-(3,5-di-tret-4-hydroxyphenyl)-2-oxoethyl]}-2aminobenzimidazolium bromides with antiplatelet and antioxidant properties

FIELD: pharmacology.

SUBSTANCE: invention relates to new benzimidazole derivatives of the general formula I , where (Ia) R = n-propyl, (Ib) R = allyl, which has antiplatelet and antioxidant properties.

EFFECT: new benzimidazole derivatives are obtained, useful for myocardial infarction and stroke treatment.

2 tbl, 2 ex

 



 

Same patents:

FIELD: chemistry.

SUBSTANCE: invention relates to a method of obtaining 1,2-di(1H-benzimidazolyl-2)-1,3-dialkylguanidines of general formula I χ=(1)nπ2+θ1+θ22+(1)n+1γarcsin(ctgα1+α22tgψ), where R=alkyl C1-C6, consisting in the interaction of 3-alkyl-1,2,4-triazolo[1,5-a]benzimidazole with butylmagnesiumbromide in an aprotic solvent in an inert atmosphere.

EFFECT: method of obtaining guanidine derivatives of formula I, which can be applied in medicine, is elaborated.

3 cl, 2 ex

FIELD: chemistry.

SUBSTANCE: claimed invention relates to novel compound of formula (1) or its pharmaceutically acceptable salt, possessing SNS inhibiting properties. In general formula R1 represents (1) hydrogen atom, (2) halogen atom, (3) C1-6alkyl group or (4) C1-6halogenalkyl group (whereR1 can be present in any substitutable position of benzene or pyridine ring); L represents (1) simple bond, (2) -O- or (3) -CH2O- (where L can be present in position 5 or 6 of condensed cycle); R2 represents (1) C6-10aryl group (C6-10aryl group is optionally condensed with C3-6cycloalkane), optionally substituted with substituent(s), X represents carbon atom or nitrogen atom. Other values of radicals are given in the invention formula.

EFFECT: obtaining compounds which can be used to prepare medication for treatment or prevention of such diseases as neuropathic pain, nociceptive pain, dysuria, disseminated sclerosis, etc.

19 cl, 47 tbl, 237 ex

FIELD: medicine, pharmaceutics.

SUBSTANCE: present invention refers to a crystalline salt of (1R*,2R*,4R*)-2-(2-{[3-(4,7-dimethoxy-1H-benzoimidazol-2-yl)propyl]methylamino}ethyl)-5-phenylbicyclo[2.2.2]oct-5-en-2-yl isobutyric acid ester. Also, the invention refers to a pharmaceutical composition of the above crystalline salt and using the above crystalline salt for preparing the pharmaceutical composition.

EFFECT: what is prepared is the crystalline salt of (1R*,2R*,4R*)-2-(2-{[3-(4,7-dimethoxy-1H-benzoimidazol-2-yl)propyl]methylamino}ethyl)-5-phenylbicyclo[2,2,2]oct-5-en-2-yl isobutyric acid ester that can be effective as a L/T-type calcium channel blocker.

15 cl, 11 dwg, 10 tbl, 6 ex

FIELD: chemistry.

SUBSTANCE: present invention relates to novel 1-ω-aryloxyalkyl- and benzyl-substituted 2-iminobenzimidazolines and pharmacologically acceptable salts thereof of general formula 1 , where R = CH=CH2, R1 = 2-ClC6H4OCH2 (1b); R = CH=CH2, R1 = 4-ClC6H4OCH2 (1c); R = CH=CH2, R1 = 4-BrC6H4OCH2 (1d); R = CH=CH2, R1 = 2,4-Cl2C6H3OCH2 (1e); R = CH=CH2, R1 = 3,4-Cl2C6H3 (1f); R = CH=CH2, R1 = 4-FC6H4OCH2CH2 (1g); R = CH2N(C2H5)2, R1 = 4-C(CH3)3C6H4OCH2 (1h); R = CH2N(C2H5)2, R1 = 3,4-Cl2C6H3 (1i); R = R1 = 4-OCH3C6H4OCH2 (1j); R = 4-BrC6H4, R1 = 4-OCH3C6H4OCH2 (1k); R = 4-BrC6H4, R1 =2-OCH3C6H4OCH2 (1l); R = 4-NO2C6H4, R1 = 4-OCH3C6H4OCH2 (1m); R = 3,4-Cl2C6H3, R1 = 2-OCH3C6H4OCH2 (1n); R = 3,4-Cl2C6H3, R1 = 4-OCH3C6H4OCH2 (1o); R = C6H5OCH2, R1 = 4-OCH3C6H4OCH2 (1p); R = 2-CH3C6H4OCH2, R1 = 2-OCH3C6H4OCH2 (1q); R = 4-CH3C6H4OCH2, R1 = 2-OCH3C6H4OCH2 (1r); R = 4-C(CH3)3C6H4OCH2, R1 = 2-OCH3C6H4OCH2 (1s); R = 2-OCH3C6H4OCH2, R1 = 4-BrC6H4OCH2 (1t), having anti-protist and antibacterial activity.

EFFECT: obtaining novel compounds with useful biological activity.

1 tbl

FIELD: chemistry.

SUBSTANCE: present invention relates to an agent, having antibacterial and anti-protist activity, based on a hydrochloride of formula (1a-k) , where R=C6H5OCH2 (a); 4-CH3C6H4OCH2 (b); 4-OCH3C6H4OCH2 (c); 2-OCH3C6H4OCH2 (d); 4-FC6H4OCH2 (e); 2-ClC6H4OCH2 (f); C10H7OCH2 (g); 2,4-Cl2C6H3OCH2 (h); 4-BrC6H4OCH2 (i); 2-FC6H4 (j); 2-ClC6H4 (k).

EFFECT: obtaining a novel agent, having antibacterial and anti-protist activity, particularly with respect to Staphylococcus aureus and Escherichia coli bacteria, and moderate anti-protist activity with respect to elementary Colpoda steinii.

1 tbl

FIELD: chemistry.

SUBSTANCE: claimed invention relates to method of obtaining 4-{4-amino-2-chloro-5-[(5-chloro-2-methyl-1H- benzimidazol-6-yl)amino]phenoxy}benzoic acid, which includes acylation of 4,5-dichloro-2-nitroaniline with acetic anhydrite, nucleophilic substitution of chlorine atom, in interaction of two molecules of N-acetyl-4,5-dichloro-2-nitroaniline with each other and with 4-hydroxybenzoic acid in DMSO in presence of K2CO3, reduction of 4-{5-[(5-acetamido-2-chloro-4-nitrophenyl)amino]-2-chloro-4-nitrophenoxy}benzoic acid, with acylation of 4,5-dichloro-2-nitroaniline being carried out at temperature 90°C for 1 h and molar ratio of 4,5-dichloro-2-nitroaniline:acetic anhydrite = 1:2.0, nucleophilic substitution of chlorine atom is carried out in DMSO in presence of K2CO3 for 3 hours at temperature 110°C and molar ratio of N-acetyl-4,5-dichloro-2-nitroaniline:4-hydroxybenzoic acid = 2:1, reduction of 4-{5-[(5-acetamido-2-chloro-4-nitrophenyl)amino]-2-chloro-4-nitrophenoxy}benzoic acid is carried out with SnCl2·2H2O at temperature 110°C for 1 h in icy acetic acid and molar ratio 4-{5-[(5-acetamido-2-chloro-4-nitrophenyl)amino]-2-chloro-4-nitrophenoxy}benzoic acid: SnCl2-2H2O = 1:6.5.

EFFECT: highly effective method of obtaining 4-{4-amino-2-chloro-5-[(5-chloro-2-methyl-1H- benzimidazol-6-yl)amino]phenoxy}benzoic acid, characterized by small time consumption on obtaining target product with high output and high purity.

3 ex

FIELD: chemistry.

SUBSTANCE: invention relates to organic chemistry and specifically to compounds of formula or a pharmaceutically acceptable salt of such a compound, where - X is a carbon atom and R1a and R2a together form a bond; or - X is a carbon atom, R1a and R2a together form a bond, and R1 and R2 together form a moiety , where the asterisk shows the bonding site of R2; or - X is a carbon atom, R1a is hydrogen or (C1-4)alkoxy, and R2a is hydrogen; and R1 and R2, unless indicated otherwise, independently denote hydrogen; (C1-5)alkyl; aryl, where aryl denotes naphthyl or phenyl, where said aryl is unsubstituted or independently mono- or disubstituted, where the substitutes are independently selected from a group consisting of (C1-4)alkyl, (C1-4) alkoxy and halogen; or heteroaryl, selected from pyridyl, thienyl, oxazolyl or thiazolyl, where said heteroaryl is unsubstituted; under the condition that if R2 is aryl or heteroaryl, R1 cannot be aryl or heteroaryl, where the aryl and heteroaryl are independently unsubstituted or substituted as defined above; R3 is hydrogen or -CO-R31; R31 is (C1-5)alkyl, (C1-3)fluoroalkyl or (C3-6)cycloalkyl; n equals 1, 2, 3 or 4; B is a -(CH2)m- group, where m equals an integer from 1 to 3; A is-(CH2)P-, where p equals 2 or 3; R4 is (C1-5)alkyl; W is , where R5 is hydrogen or (C1-5)alkyl; R8, R9 and R10 is independently hydrogen, halogen, (C1-5)alkyl, hydroxy, -(C1-5)alkoxy, -O-CO-(C1-5)alkyl, (C1-3)fluoroalkyl, (C1-3)fluoroalkoxy, -CO-(C1-5)alkoxy, (C1-2)alkoxy-(C1-4)alkoxy or -NH-CO-(C1-5)alkyl. The invention also relates to a pharmaceutical composition based on a compound of formula (I).

EFFECT: novel compounds which are useful as calcium channel blockers are obtained.

11 cl, 2 tbl, 166 ex

FIELD: chemistry.

SUBSTANCE: present invention relates to compounds of formula (I) or pharmaceutically acceptable salts of such a compound, where R1 is an unsubstituted phenyl; R2 is -CO-R21; R21 is C1-5alkyl; m equals 3; p equals 2 or 3; and R3 is hydrogen. The invention also relates to specific compounds of formula ,

a pharmaceutical composition based on the compound of formula (I) and use of the compound of formula (I).

EFFECT: novel compounds which are useful as T/L channel blockers are obtained.

6 cl, 1 tbl, 8 ex

FIELD: chemistry.

SUBSTANCE: invention relates to organic chemistry and specifically to a method of producing benzimidazole derivatives of formula where X is a single bond, involving reaction of nitriles, selected from: 3-phenoxybenzonitrile, 3-phenoxyphenyl acetonitrile, 3-(3-phenoxyphenyl)acrylonitrile, 3-(3-phenoxyphenyl)-2-butenonitrile, 3-(3- phenoxyphenyl)propionitrile, 3-(3-phenoxybenzylamino)propionitrile, 2-methyl-2-(3-phenoxybenzoate)propionitrile, 3-phenoxyphenyl methoxypropionitrile with ortho-phenylene diamine hydrochloride in a sealed glass bulb. The process is carried out with molar ratio of nitrile to ortho-phenylene diamine hydrochloride of 1:1.2 at temperature 190-200°C.

EFFECT: novel method of producing said compound with good output and high degree of purity.

FIELD: chemistry.

SUBSTANCE: invention describes a method of producing optionally substituted 4-benzimidazol-2-ylmethylamino)-benzamidine of formula (I) with organic or inorganic acids , in which R1, R2 and R3 are as described in claim 1, characterised by that (a) phenyldiamine of formula

in which R1 and R2 assume values indicated for formula (I), are condensed with 2-[4-(1,2,4-oxadiazol-5-on-3-yl)-phenylamino]-acetic acid and (b) i) the obtained product of formula in which R1 and R2 assume values given for formula (I) is hydrogenated, ii) the amidine group is optionally carbonylated without pre-extraction of the hydrogenation intermediate product and iii) the obtained compound of formula (I), in which R3 denotes hydrogen, without pre-extraction of the carbonylation intermediate product, optionally react with a compound of formula (IV) R3-X (IV) in which R3 assumes values given for formula (I), and X denotes a suitable splitting group, and the desired salt is separated.

EFFECT: novel method enables to obtain the desired compound with high output and using cheap auxiliary material.

10 cl, 7 ex

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention refers to using dermatan sulphate recovered from sulodexide for treating diseases involving metalloproteinase MMP-9: varicose veins and vascular malformations accompanied by a risk of thrombosis.

EFFECT: reducing and/or inhibiting individual's blood serum and saphena segments MMP-9 has been shown.

4 cl, 3 dwg, 13 tbl

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention relates to the field of biotechnology, namely, to obtaining inhibitors of adhesion and/or aggregation of platelets, and can be used in medicine. A polypeptide, used as a component of a pharmaceutical composition and in sets for screening of the inhibitors of platelet adhesion or aggregation, is obtained in a recombinant way with the application of a matrix of the salivary gland cDNA of Anopheles stephensi.

EFFECT: invention makes it possible to obtain the polypeptide, possessing inhibiting activity with respect to platelet aggregation and/or inhibiting activity with respect to platelet adhesion.

10 cl, 4 dwg, 5 ex

FIELD: medicine.

SUBSTANCE: invention represents a mixture of two structural isomers: 2,6-di(1,7,7-trimethylbicyclo[2.2.1]hept-2-yl)-4-methylphenol and its diastereomers, and 2-(1,7,7-trimethylbicyclo[2.2.1]hept-2-yl)-6-(2,2,1-trimethylbicyclo[2.2.1]hept-5-yl)-4-methylphenol, and their diastereomers with the ratio of the first and second structural isomer isomers from 60:40 wt % to 95:5 wt %.

EFFECT: extension of the arsenal of means, possessing simultaneously haemorheological, anti-aggregate, anti-thrombogenic, retinoprotecting, endothelium-protecting, neuroprotecting, anti-arrhythmia and anti-ischemic activity, enhancing the cerebral blood flow.

4 dwg, 20 tbl, 6 ex

FIELD: medicine.

SUBSTANCE: before operation analysis of patient's haemostasis by means of thrombodynamics is carried out, and 12 hours before beginning operation anticoagulant prophylaxis with enoxaparin in dose 40 mg s/c 1 time per day performed. Analysis of thrombodynamics and coagulogram are repeated one day after operation, In case of detection of hypercoagulation (increase of one or some indices of thrombodynamics - initial speed of clot growth, stationary speed of clot growth, clot density, appearance of spontaneous clots) dose of enoxaparin is increased to 60 mg one time per day, and in case of detection of hypocoagulation (reduction of one or several indices of thrombodynamics - initial speed of clot growth, stationary speed of clot growth, clot density, delay of clot growth) dose of anticoagulant is reduced twice - 20 mg of enoxaparin per day.

EFFECT: method makes it possible to prevent development of post-operative venous thromboembolic complications in patients with colorectal cancer; said regimen of enoxaparin introduction provides prevention of both thromboembolic and hemorrhagic complications in said group of patients.

2 ex

FIELD: chemistry.

SUBSTANCE: thrombocyte aggregation-inhibiting heteromeric peptides based on imidazo[4,5-e]benzo[1,2-c;3,4-c']difuroxane are disclosed: , where R=Phe-Ile-Ala-Asp-Thr; Arg-Tyr-Gly-Asp-Arg; Lys-Ile-Ala-Asp-Asp; His-Ile-Gly-Asp-Asp.

EFFECT: improved properties.

1 dwg, 2 tbl, 4 ex

FIELD: chemistry.

SUBSTANCE: invention relates to N-carb(arginyl)oxymethylimidazo[4,5-e]benzo[1,2-c; 3,4-c']difuroxane of formula .

EFFECT: improved properties of the compound.

1 dwg, 1 tbl

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention relates to the field of pharmaceutics and represents a medication, possessing venomotor and anticoagulant action, which includes a dry extract of vine leaves, a base, preservatives, solvents, and is characterised by the fact that it additionally contains heparin in the form of a pharmaceutically acceptable salt, as the base it contains a hydrophilic gel-generating agent, as the solvents it contains purified water, propyleneglycol, ethyl alcohol rectified 95%, as the preservatives it contains nipagin, nipasol, with the following component ratio, wt %: dry extract of vine leaves with the content of the sum of flavonoides counter per rutin no less than 8% - 0.1-30.0; heparin in the form of a pharmaceutically acceptable salt - 100-1000 Units, hydrophilic gel-generating agent - 0.2-20.0; nipagin - 0.01-0.2; nipasol - 0.01-0.2, propyleneglycol - 3.0-70.0; ethyl alcohol rectified 95% - 3.0-70.0; purified water - the remaining part.

EFFECT: invention provides the creation of the medication in the form of a gel with good absorption, fast soaking, storage stability and acceptable organoleptic properties.

4 cl, 8 ex

FIELD: medicine, pharmaceutics.

SUBSTANCE: present invention refers to a citrate of a compound described by formula (II) below, and a pharmaceutical composition containing said citrate.

EFFECT: experimental results of the present inventions prove that said citrate can inhibit activity of phosphodiesterase type 5 and can be used for treating erectile dysfunction, for inhibiting thrombocyte aggregation and treating thrombosis, for reducing pulmonary hypertension and treating cardiovascular diseases, asthma and diabetic gastroparesis.

2 cl

FIELD: medicine.

SUBSTANCE: invention concerns preparing systemic and topical solid and soft dosage forms for external application in the form of a 1.5% hydrophilic gel and rectal capsules containing a 7.5% hydrophilic gel 1.9 g (in terms of the amount of the active substance of 0.14 g/capsule), for preventing and treating chronic venous insufficiency possessing anticoagulant, antithrombotic, anti-inflammatory, antiexudative and antitranssudative, capillary protective activities and improving haemorheology. An active pharmacologically active substance is presented by a substance of a potassium salt of sulphated arabinogalactan; a hydrophilic base is Aerosil, glycerol and pure water; the ingredients of the agent are taken in certain proportions, wt %.

EFFECT: invention provides the effective prevention and treatment of chronic venous insufficiency, has a broad spectrum of therapeutic action, improves haemorheology, tones the vessels and can be used in particular for treating varicose veins, thrombosis and posttraumatic oedema.

5 cl, 7 ex, 8 dwg

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention refers to medicine, particularly to pharmaceutical industry, and describes a dosage form of Clopidogrel presented in the form of a solid gelatine capsule. The dosage form contains Clopidogrel hydrogen sulphate, lactose anhydride, microcrystalline cellulose, sodium croscarmellose, colloidal silicon dioxide and magnesium stearate.

EFFECT: according to the invention, the dosage form of Clopidogrel contains a high amount of the active ingredient; it is prepared without the use of a wet granulation technique, and provides the more accurate dosage of the ingredients and the stability of the substances used.

9 tbl

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention refers to organic chemistry, namely to benzimidazole-4-carboxamide derivatives of formula , wherein X means an alkenyl group C2-C7 substituted by two methyls, nitro-radical mono-substituted thienyl, unsubstituted quinolinyl, unsubstituted indolyl, unsubstituted pyridazinyl, unsubstituted piperazinyl, C1-C6-alkyl disubstituted piperazinyl, unsubstituted piperidinyl, unsubstituted pyrazinyl, unsubstituted imidazolyl, unsubstituted pyrimidinyl, phenyl monosubstituted pyrimidinyl, pyrimidinyl disubstituted by an amine radical and a radical specified in a group containing -F, -Cl, -Br or -I, hydroxyl trisubstituted phenyl, methoxy-radical trisubstituted phenyl, hydroxyl and methoxy-radical disubstituted phenyl, pyrazolyl disubstituted by a radical specified in a group containing a C1-C6-alkyl, and by a radical specified in a group containing -F, -C1, -Br or -I; Y means aminophenyl monosubstituted by a radical of -F, -O, -Br or -I phenyl, hydroxyethyl disubstituted by hydroxymethyl or C1-C6-alkyl and phenyl monosubstituted by a nitro group, an amino group or a halogen atom; Y also means unsubstituted piperazinyl, unsubstituted pyridyl, unsubstituted pyrazinyl, C1-C6-alkyl monosubstituted thiazol, unsubstituted pyrimidinyl, unsubstituted purinyl. The invention also refers to a pharmaceutical composition based on the compound of formula (I), using the compound of formula (I), a method for producing the compound of formula (I).

EFFECT: there are prepared new benzimidazol-4-carboxamide derivatives possessing antiviral activity.

5 cl, 6 dwg, 4 tbl, 688 ex

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