Hydrochlorides of 1-alkyl-3-methyl-8-piperazino-7-(tiethanyl-3)xanthine showing antithrombotic effect by blocking gp iib-iiia platelets receptors

FIELD: pharmacology.

SUBSTANCE: invention relates to 1-alkyl-3-methyl-8-piperazino-7-(tiethanyl-3)xanthine hydrochlorides of the general formula: Ia-c, where R=CH2-CH=CH2 (Ia), C3H7-iso (Ib), C5H11-h (Ic).

EFFECT: increased antithrombotic effect by blocking the GP IIb-IIIa platelet receptors.

5 cl, 2 tbl, 5 ex

 



 

Same patents:

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention relates to novel N-containing heteroaryl derivatives of formula I or II or their pharmaceutically acceptable salts, which possess properties of JAK kinase, in particular JAK3, and can be applied for treating such diseases as asthma and chronic obstructive pulmonary disease (COPD). In formulae A represents carbon and B represents nitrogen or A represents nitrogen and B represents carbon; W represents CH or N; R1 and R2, independently represent hydrogen, C1-4alkyl, halogenC1-4alkyl, -CN; R3 represents C1-4alkyl, R9-C1-4alkyl, Cy1, where Cy1 is optionally substituted with one or several substituents R10; R4 represents hydrogen, C1-4alkyl, R12R7N-C0alkyl, where one of R7 and R12 represents hydrogen, and the other represents C1-4alkyl or group R13, which is selected from C1-5alkyl, Cy2-C0alkyl; R5 represents hydrogen; R6 represents hydrogen, C1-4alkyl, C1-4alkoxyC1-4alkyl, hydroxyC1-4alkyl, R12R7N-C1-4alkyl, R16CO-C0alkyl, Cy1; R7 represents hydrogen or C1-4alkyl; R9 represents halogen, -CN, -CONR7R12, -COR13, CO2R12, -OR12, -SO2R13, -SO2NR7R12, -NR7R12, -NR7COR12; R10 represents C1-4alkyl or R9-C0-4alkyl; R11 represents C1-4alkyl, halogen, -CN, -NR7R14; R12 represents hydrogen or R13; R13 represents C1-5alkyl, hydroxyC1-4alkyl, cyanoC1-4alkyl, Cy2-C0alkyl or R14R7N-C1-4alkyl; where Cy2 is optionally substituted with one or several constituents R11; R14 represents hydrogen or C1-4alkyl; R16 represents C1-4alkyl, halogenC1-4alkyl, C1-4alkoxyC1-4alkyl, hydroxyC1-4alkyl or cyanoC1-4alkyl; Cy1 represents monocyclic carbocyclic unsaturated or saturated ring, selected from C3-C6cycloalkyl, phenyl, or saturated monocyclic 4-6-membered heterocyclic ring, containing from 1 to 2 heteroatoms, selected from N and S, or partially unsaturated 10-membered bicyclic heterocyclic ring, containing oxygen atom as heteroatom, which can be substituted with group R11, where said ring is bound with the remaining part of molecule via any available C atom, and where one or several ring C or S atoms are optionally oxidised with formation of CO or SO2; and Cy2 represents monocyclic carbocyclic unsaturated ring, selected from C3-C6cycloalkyl, or aromatic monocyclic 4-6-membered heterocyclic ring, containing from 1 to 2 heteroatoms, selected from N and S, or unsaturated 10-membered bicyclic heterocyclic ring, containing oxygen atom as heteroatom, which can be substituted with group R11, where said ring is bound with the remaining part of molecule via any available atom C or N.

EFFECT: obtaining novel heteroaryl derivatives.

27 cl, 41 ex

FIELD: chemistry.

SUBSTANCE: invention relates to novel derivative of purinylpyridinylamino-2,4-difluorophenylsulphonamide of formula 1 and its pharmaceutically acceptable salt. Compounds have properties of inhibiting Raf-kinase super activity and can be applied for prevention and treatment of diseases, mediated by activity of Raf-kinase, such as cancer, in particular melanoma. In formula 1 R stands for methyl; ethyl; propyl; isopropyl, butyl, isobutyl; cyclopropyl; cyclobutyl; cyclopentyl; cyclohexyl; C5-C6aryl, unsubstituted or substituted with one or more substituents, selected from the group, which consists of chlorine, fluorine, bromine, methyl, ethyl, propyl, isopropyl, butyl, isobutyl, methoxy, ethoxy, propoxy, butoxy, trifluoromethoxy, fluoromethoxy, difluorimethoxy and trifluoroethoxy; C5-C12heteroaryl, which consists of one or two rings, non-substituted or substituted with one or more substituents, selected from the group, which consists of chlorine, fluorine, bromine, methyl, ethyl, propyl, isopropyl, butyl, isobutyl, methoxycarbonyl, ethoxycarbonyl, propoxycarbonyl, butoxycarbonyl, tret- butoxycarbonyl and dioxolanyl; C5-C6heterocycloalkyl, non-substituted or substituted with one or more substituents, selected from the group, which consists of chlorine, fluorine, bromine, methyl, ethyl, propyl, isopropyl, butyl, isobutyl; or C5-C6aryl-linear or branched C1-C6alkyl, non-substituted or substituted with one or more substituents, selected from the group, which consists of chlorine, fluorine, bromine, nitro, methyl, ethyl, propyl, isopropyl, butyl and isobutyl, and heteroaryl and heterocycloalkyl contain in ring one or more heteroatoms, selected from the group, which consists of N, O and S. Invention also relates to methods of obtaining formula 1 compounds.

EFFECT: improvement of characteristics.

15 cl, 3 tbl, 51 ex 1 dwg

FIELD: chemistry.

SUBSTANCE: invention relates to compounds or their pharmaceutically acceptable salts, where compound has formula 1-a, in which R1 and R3 are absent, m represents integer number from 1 to 2, n represents integer number from 1 to 3, A represents , B represents or , where X2 represents O or S, R4a is absent, R4b is selected from the group, consisting of: , , , , and ; Rk is selected from C1-6alkyl and C1-6halogenalkyl, L and E are such as given in i.1 of the invention formula; or compound is such as given in b) of i.1 of the invention formula. Invention also relates to pharmaceutical composition, which contains said compounds.

EFFECT: compounds by i1, possessing inhibiting activity with respect to anti-apoptosis protein Bcl-XL.

27 cl, 6 dwg, 2 tbl, 126 ex

FIELD: medicine.

SUBSTANCE: invention refers to medicine, namely to psychiatry and drug addiction, and may be used for detoxification-infusion therapy of the patients used psychotropic cannabis products. That is ensured by the infusion intravenous drop-by-drop sequential administration of drugs. A mixture containing 5% glucose 200 ml, 25% magnesium sulphate 10 ml and 4% potassium chloride 10 ml are administered. That is combined with the additional bolus administration of 5% vitamin B1 2 ml. That is followed by introducing a mixture containing 0.9% normal saline 200 ml and 20% piracetam 10 ml. That is added with the bolus administration of 5% vitamin B6 10 ml. Then, a mixture containing rheopolyglucin 200 ml, 5% ascorbic acid 5 ml and 1% nicotinic acid 1 ml is administered. Then, a mixture containing 0.9% normal saline 200 ml and 2.4% aminophylline 5 ml is administered. The procedure is performed twice a day for 10 days.

EFFECT: method provides the higher therapeutic effectiveness and reduced length of the therapy, as well as the presented method is reproducible easily.

1 ex

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention refers to chemical-pharmaceutical industry, namely to using a purine derivatives for preparing drug preparations for treating chronic lymphocytic leukaemia and polycystic kidneys.

EFFECT: invention provides preparing the compounds possessing higher activity on lymphocytic leukaemia and polycystic kidneys.

8 cl, 3 dwg, 1 ex, 3 tbl

FIELD: medicine.

SUBSTANCE: invention refers to new heteroaryl compounds of general formula (I) and their pharmaceutically acceptable salts possessing the properties of protein kinase inhibitor, such as mTOR, IKK-2, Tyk2, Syk-kinase. In formula (I) R1 represents substituted or unsubstituted C1-8alkyl, substituted or unsubstituted aryl, specified in phenyl, substituted or unsubstituted 5-6-member heteroaryl with 1-3 nitrogen atoms in a cycle specified in pyridine, pyrazole, indole, indazole, triazole, benzimidazole, 2-(1H-imidazo-[4,5-b]pyridine, substituted or unsubstituted 5-7- member cycloalkyl or substituted or unsubstituted heterocycloalkyl specified in pyrrolidinyl; -X-A-B-Y- taken together form -N(R2)CH2C(O)NH-, -N(R2)C(O)CH2NH-, -N(R2)C(O)NH-, -N(R2)C=N- or -C(R2)=CHNH-; L represents a direct bond, NH or O; R2 represents substituted or unsubstituted C1-8alkyl, substituted or unsubstituted aryl specified in phenyl, tetrahydronaphthalene, unsubstituted 5-7- member mono- or 8- member bicycloalkyl; and R3 and R4 independently represent H or C1-8alkyl. The substitutes in the substituted groups are specified in one or more halogen, C1-8alkyl, hydroxyl, amino, nitro, thiol, C1-4alkyl thioether, cyano, carboxyl, C1-4alkyl ester, halogen alkyl, C6cycloalkyl or heteroaryl specified in pyridyl, triazole, O-lower alkyl, aryl specified in phenyl, phenyl-lower alkyl, CO2CH3, CONH2, OCHF2, CF3 or OCF3 groups wherein CONH2 group may be substituted by cyclohexyl.

EFFECT: compounds can find application for treating or preventing cancer, inflammatory pathological conditions, metabolic pathological conditions.

24 cl, 8 dwg, 2 tbl, 169 ex

FIELD: chemistry.

SUBSTANCE: disclosed agent is a xanthine derivative of formula 1

, where R1 denotes CH3, R2 denotes CH3; R3 denotes halogens: F,Cl, Br, I; R4 denotes hydrogen; R1 denotes CH3, R2 denotes CH3; R3 denotes hydrogen, halogens: F, Cl, Br, I; R4 denotes CH2COOH; R1 denotes hydrogen, R2 denotes CH3; R3 denotes halogens: F, Cl, Br, I; R4 denotes CH3. The preferred compounds of the said agent are 8-chlorotheophylline, 8-bromotheophylline and theophylline-7-acetate. The invention also relates to a method of slowing down proliferation of tumour cells and a method of inducing differentiation in mouse melanoma B16-F10 cells. Each of the methods involves addition of an effective amount of the said agent in an effective amount, preferably in amount of 1 mM.

EFFECT: improved properties of the derivatives.

8 cl, 4 tbl, 12 dwg

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention relates to novel compounds, which inhibit HIV replication, of formula (I) , its pharmaceutically acceptable additive salt; or stereochemically isomer form, where -a1=a2-a3=a4-represents bivalent radical of formula -CH=CH-CH=CH- (a-1); -b1=b2-b3=b4 -represents bivalent radical of formula -CH=CH-CH=CH- (b-1); n represents 0; m represents 1, 2; -A-B- represents bivalent radical of formula -CR5=N- (c-1); -N=N- (c-2); -CH2-CH2- (c-3); -CS-NH- (c-4); -CH=CH- (c-6); R1 represents hydrogen; R2a represents cyano; R3 represents cyano-substituted C1-6alkyl; cyano-substituted C2-6lkenyl; each of R4 independently represents halogen or C1-6alkyl; Q represents hydrogen or C1-6alkyl; R5 represents hydrogen, C1-6alkyl, aryl, pyridyl, thienyl, furanyl, amino, mono- or di(C1-4alkyl)amino, where aryl represents phenyl. Invention also relates to pharmaceutical composition, application and method of obtaining compounds.

EFFECT: obtaining novel compounds, which inhibit HIV replication.

5 cl, 25 dwg, 7 tbl, 16 ex

Novel compounds // 2395511

FIELD: chemistry.

SUBSTANCE: present invention relates to novel xanthine derivatives of general formula (I) and their pharmaceutically acceptable salts which have HM74A receptor activity, which can be used in therapy for treating diabetic dyslipidemia, combined dyslipidemia, heart failure, hypercholesteremia, atherosclerosis, arteriosclerosis, hypertriglyceridemia, type II sugar diabetes, type I diabetes, insulin resistance, hyperlipidemia, anorexia nervosa, obesity, coronary artery disease, thrombosis, stenocardia, chronic kidney disease, peripherical vascular disease or stroke. In compounds of formula (I) , R1 is hydrogen or methyl; R2 is unsubstituted H-C4-6 alkyl; and R3 is chlorine.

EFFECT: obtaining novel compounds and a pharmaceutical composition based on the said novel xanthine derivatives.

15 cl, 54 ex

FIELD: medicine, pharmacology, organic chemistry, pharmacy.

SUBSTANCE: invention relates to novel compounds of the formula (I) promoting the defecation. Also, invention relates to a pharmaceutical composition containing these compounds and a method for promoting defecation and a method for treatment or relief of constipation. Proposed compounds possess the enhanced effectiveness.

EFFECT: valuable medicinal properties of pharmaceutical composition.

14 cl, 11 tbl, 55 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.

SUBSTANCE: method involves removing an epithelial layer, exposing a cornea by saturating it through multiple instillations of 0.1% riboflavin followed by the ultraviolet exposure. After the epithelial layer has been removed, a ring made of an ultraviolet-protected contact lens is applied on a surface of the eyeball perilimbally. An outer diameter of the ring covers the limb by no more than 2 mm, whereas an inner diameter of the ring is equal to a basic diameter of the keratoconus. The whole duration of the ultraviolet exposure involves additional instillations of riboflavin on the cornea every 3-4 minutes. The exposure is characterised by wavelength 365 nm, power 3.0 mWt/cm2 at 50 mm for 30 minutes with the ring to be removed after the exposure is completed.

EFFECT: method is easy to implement, involves no difficulties for specialists, providing higher clinical effectiveness by limiting the ultraviolet exposure area, preventing the ultraviolet involvement of the limb and reducing a risk of postoperative complications.

1 ex

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