Drugs for disorders of the endocrine system (A61P5)

A   Human necessities(312083)
A61P5                 Drugs for disorders of the endocrine system(560)
A61P5/24 - Of the sex hormones(53)
A61P5/26 - Androgens(33)
A61P5/28 - Antiandrogens(19)
A61P5/30 - Oestrogens(31)
A61P5/32 - Antioestrogens(15)
A61P5/34 - Gestagens(10)
A61P5/36 - Antigestagens(4)

Fusion serpine polypeptides and methods for their application // 2642310
FIELD: biotechnology.SUBSTANCE: invention relates to the field of fusion proteins for serine proteases inhibition, and can be used in medicine. Fusion proteins having at least one human alpha-1 antitrypsin (AAT) polypeptide operably linked to an immunoglobulin Fc polypeptide having an amino acid sequence that is at least 98% identical to the amino acid sequence of SEQ ID NO:6 are obtained.EFFECT: invention allows to obtain a fusion polypeptide capable of effectively inhibiting the activity of serine proteases and thereby alleviating the symptoms of diseases or disorders associated with overexpression or serine protease activity in a subject in need thereof.18 cl, 4 dwg, 4 ex

Fusion polypeptide containing wap domain and their application methods // 2639526
FIELD: biotechnology.SUBSTANCE: fusion proteins having at least one polypeptide of the human secretory inhibitor of leukocyte proteases (SLPI) operably linked to an immunoglobulin Fc fragment polypeptide having an amino acid sequence that is at least 98% identical to the amino acid sequence of SEQ ID NO:10 are obtained.EFFECT: invention allows to obtain a fusion polypeptide capable of effectively inhibiting the activity of neutrophilic serine proteases and thereby alleviating the symptoms of diseases or disorders associated with overexpression or serine protease activity in a subject in need thereof.15 cl, 4 dwg, 4 ex

Peptidomimetic macrocycles and their application // 2639523
FIELD: biotechnology.SUBSTANCE: peptidomimetic macrocycle is proposed that binds to the Growth-Hormone-Releasing Hormone (GHRH) receptor and its use. The peptidomimetic macrocycle proposed has a structure as shown in the formula.EFFECT: peptidomimetic macrocycle has improved biological activity, stimulates the production and release of growth hormone and can be used to increase lean muscle mass in the patient, to reduce adipose tissue in the patient, to treat muscle atrophy, lipodystrophy, growth hormone, gastric paresis, or short-term syndrome guts in a patient.31 cl, 11 dwg, 5 tbl, 4 ex

Transdermal pharmaceutical compositions containing active agents // 2639087
FIELD: pharmacology.SUBSTANCE: invention is a sustained release pharmaceutical composition for topical administration to the skin surface, which comprises: a pharmaceutically active agent selected from the group consisting of estrogens, antiestrogens, androgens, antiandrogens, progestins, and mixtures thereof, 0.01-5 wt % of the total weight of the pharmaceutical composition of the fatty acid ester selected from the group consisting of ethyl oleate, isopropyl myristate, isopropyl isostearate, isopropyl palmitate, ethyl octanoate, ethyl dodecanoate, ethyllinoleate, ethyl palmitoleate, ethyl isostearate and ethyllleleate, water, C2-C6 mono-alcohol selected from the group consisting of ethanol, n-propanol, isopropanol, n-butanol, isobutanol, t-butanol and mixtures thereof, a fatty acid selected from the group consisting of capric acid, lauric acid, myristic acid, palmitic acid, stearic acid, oleic acid, isostearic acid, palmitoleic acid, linoleic acid and linolenic acid, and from 0.05 to 5 wt % of gelling agent, wherein the weight ratio of the fatty acid ester in the composition to the total active agent in said composition is at least 4:1 (fatty acid ester:active agent), preferably 4:1 to 20:1.EFFECT: invention provides sustained release, corresponding delivery profiles in the concentration range of active agents, and reproducibility from application to application and from patient to patient.21 cl, 11 ex, 10 dwg, 24 tbl

Pyrazol-4-yl-heterocyclyl-carboxamide compounds and methods for application // 2638552
FIELD: pharmacology.SUBSTANCE: invention relates to pyrazol-4-yl-heterocyclylcarboxamide compounds of Formula I , including their stereoisomers, tautomers and pharmaceutically acceptable salts, wherein X is a thiazolyl, pyrazinyl, pyridinyl or pyrimidinyl group, R1 and R2 have the meanings indicated in the claims. The compounds of formula I are useful for Pim kinase inhibition and for treatment of disorders such as cancer mediated by Pim kinase. Methods for application of formula I compounds for in vitro, in situ and in vivo diagnosis, prevention or treatment of such diseases in mammalian cells or acssociated pathological conditions are disclosed.EFFECT: increased efficiency of treatment.26 cl, 4 tbl, 528 ex
New tetrahydropyrimidine connection or its salt // 2636310
FIELD: pharmacology.SUBSTANCE: invention relates to a new tetrahydropyridopyrimidine compound of the general formula (I) or a pharmaceutically acceptable salt thereof. The compounds possess an inhibitory activity against the androgen receptor (AR) and can be used to treat a tumour associated with activity (AR). In the general formula ,X is a halogen atom or halogen-C1-3an alkyl group; R is a phenyl group which is substituted by R1 and can also be substituted by R2, or a 5- or 6-membered heteroaryl group which contains 1 to 3 heteroatoms selected from a nitrogen, oxygen or sulfur atom and which is substituted by R1 and can also be substituted by R2; R1 represents a hydrogen atom, a phenyl group, a hydroxy-C1-6alkyl group, hydroxy-C3-7cycloalkyl group,C1-6an alkoxy group which may be substituted by Ra, C3-7 a cycloalkylaminosulfonyl group, a (6-7) membered monocyclic heterocycloalkylsulfonyl group, with two nitrogen atoms or a nitrogen atom and an oxygen atom in the ring; halogen-C1-3alkoxycarbonylamino group, halogen-C1-3alkylcarbonylamino group, a (5-7)membered monocyclic heterocycloalkanecarbonyl group,containing a nitrogen atom in the ring, and substituted with hydroxy-C1-6alkyl group, or - (CH2)n-C(=O)-NHRf; R2 is a hydrogen atom, a halogen atom or a halogen-C1-3an alkyl group; Ra is C1-6alkylpyrazolyl group, a triazolyl group, a tetrazolyl group or a C1-6 alkylsulfonylpiperazinyl group; Rf is halogen-C1-3alkyl group, hydroxy-C1-6alkyl group, hydroxy-C3-7cycloalkyl group, hydroxy-C3-7cycloalkyl-C1-6alkyl group C1-6alkyl group, substituted by Rfa; Rfa is C a 1-6alkylpyrazolyl group, halogen-C1-3alkylthiazolyl group, an oxadiazolyl group or a halogen-C1-3alkyloxadiazolyl group; and n is an integer from 0 to 3.EFFECT: obtaining of a new compound.20 cl, 5 tbl, 63 ex
ethod for hypothyrosis treatment in cattle // 2635513
FIELD: veterinary medicine.SUBSTANCE: iodcasein is added to the basic diet in the amount of 1480 mg/head. 1 time per day for a month and fed for one month once a day.EFFECT: method allows to improve the general condition, hematologic and biochemical indicators and productivity of animals.2 cl, 2 tbl

Compositions and methods for metabolic pathway modulation // 2631597
FIELD: pharmacology.SUBSTANCE: composition of the invention contains at least 500 mg of leucine and/or at least 200 mg of one or more of its metabolites, wherein one or more leucine metabolites are selected from the group consisting of ketoisocaproic acid (KIC), alphahydroxyisocaproic acid and hydroxymethyl butyrate (HMB), and an antidiabetic agent comprising metformin. The methods of the invention comprise composition administration to a subject.EFFECT: application of the invention can reduce the metformin dose during treatment of metabolic disorders due to the synergistic effect of the composition components.27 cl, 3 tbl, 76 dwg, 10 ex
Application of aromatase inhibitor for treatment of hypogonadism and related diseases // 2628808
FIELD: medicine.SUBSTANCE: method of the invention comprises administration of 4,4'-[fluoro(1H-1,2,4-triazol-1-yl)methylene]bisbenzonitrile to a male patient with the total serum testosterone level of less than 400 ng/dl, at a dose of 0.001-1.0 mg weekly. The composition of the invention includes a pharmaceutical composition and instructions for administration.EFFECT: increased testosterone levels in these patients.19 cl, 2 tbl, 5 ex

Glycosylated polypeptides and medicinal compositions containing these polypeptides // 2627184
FIELD: biotechnology.SUBSTANCE: glycosylated somatostatin analogs containing two or three glycosylated amino acids are obtained.EFFECT: invention allows to increase the stability of somatostatin analogues in blood in comparison with somatostatin.14 cl, 20 dwg, 10 tbl, 91 ex

Glycosylated polypeptides and medicinal compositions containing these polypeptides // 2624034
FIELD: biotechnology.SUBSTANCE: invention relates to production of glycosylated polypeptides having affinity for somatostatin receptors and can be used in medicine for somatostatin-related diseases treatment or prevention. SRIF14 and SRIF28 glycosylated polypeptides are obtained by Asn or Cys glycosylation.EFFECT: invention provides preparation of glycosylated polypeptides having an affinity for somatostatin receptors and better stability in blood compared to somatostatin.14 cl, 19 dwg, 10 tbl, 88 ex

Crystalline form of compound used as a mineralocorticoid receptor antagonist and the method of its production // 2622105
FIELD: chemistry.SUBSTANCE: invention relates to crystalline forms I and II of compound 2-chloro-4-[(3S,3aR)-3-cyclopentyl-7-(4-hydroxy-1-carbonyl)-3,3a, 4.5-tetrahydro-2H-pyrazolo[3.4-f]quinolin-2-yl]benzonitrile of formula (I), used as a mineralocorticoid receptor antagonist. Crystalline forms have characteristic peaks of powder X-ray diffraction pattern specified in the claims. The invention also relates to processes for preparing crystalline forms I and II and the use of the obtained crystal forms in the manufacture of medicaments for the treatment and/or prevention of kidney damage or cardiovascular diseases.EFFECT: obtained crystalline form the compound of formula amorphous form of its superior stability, not only at high temperature and humidity, and light conditions.16 cl, 4 dwg, 4 tbl, 10 ex
Energometabolic composition for preventive therapy of metabolic acidosis, ketosis, and iodine deficiency in cows // 2620557
FIELD: agriculture.SUBSTANCE: claimed energometabolic composition for preventive therapy contains beet molasses, succinic acid and citric acid, sodium chloride, iodinol in aqueous solution in the following ratio, wt %: succinic acid - 1,5, citric acid - 0,15, beet molasses - 50, sodium chloride - 2,5, iodinol - 5,0, water - the rest The claimed method involves the use of the claimed composition with the multiplicity of once in 5-7 days by watering animals at a dilution of the composition in water of 1:5-7 or mixing it with the fodder.EFFECT: group of inventions relates to the field of veterinary medicine and is intended for the prevention of metabolic acidosis, ketosis, and hypothyroidism in cows.2 cl, 4 tbl, 1 ex
Oestrogen receptors ligands // 2620375
FIELD: chemistry.SUBSTANCE: invention relates to compounds of formula (I) or to pharmaceutically acceptable salts thereof.EFFECT: new compounds are obtained, which can be used as oestrogen receptors ligands.24 dwg, 360 ex, 21 cl

Hydrocortisone composition with controlled release // 2619869
FIELD: pharmacology.SUBSTANCE: invention relates to a pharmaceutical composition for oral administration, comprising a core containing hydrocortisone and a carrier, and a delayed release polymer layer in contact with the said core. The core contains microcrystalline cellulose in an amount of 75-85% by composition weight. The delayed release polymer is a mixture of a polymer (1) having a composition of poly(methacrylic acid, methyl methacrylate) at a ratio of 1:1, and a polymer (2) having a composition of poly(methacrylic acid, methyl methacrylate) at a ratio of 1:2. Polymers (1) and (2) are presented at a ratio of 1:4 and are taken in an amount of 6-7% by composition weight. Also a method for composition manufacture and its use for treating adrenal insufficiency is described.EFFECT: release of hydrocortisone in accordance with the circadian release of cortisol to reproduce natural cortisol release.39 cl, 7 dwg, 2 tbl, 4 ex
ethod for producing agents with thyroid-stimulating activity // 2619863
FIELD: pharmacology.SUBSTANCE: triple extraction of plant material is performed at 70°C at a ratio of 1 pts. wt. of the raw materials: 5 pts. vol. of the extractant. Wherein the first and second extraction are performed by 50% ethyl alcohol for 60 minutes, and the third extraction - by water purified for 30 minutes. Then the combined extracts are filtered, evaporated, purified by separation, finally evaporated and dried in a vacuum drying unit. The plant material is components in the following ratio pts. wt.: Potentilla alba rhizomes and roots - 50, haw berries - 15, Valeriana rhizomes with roots - 35, ground down to 2 mm.EFFECT: invention provides a higher yield of extractives and better expression of the thyroid-stimulating activity of the resulting agents compared to the analogue.11 tbl, 1 ex

Crystalline solvates of hydrochloride 6-(piperidin-4-yloxy)-2h-isoquinolin-1-one // 2619129
FIELD: chemistry.SUBSTANCE: invention relates to organic chemistry, in particular to crystalline dihydrate 6-(piperidin-4-yloxy)-2H-isoquinolin-1-one of formula and a solid pharmaceutical composition thereof.EFFECT: obtained crystalline hydrochloride dihydrate, having better stability and hygroscopicity, which is preferable in obtaining the medicinal product based on it.16 cl, 14 dwg, 1 tbl
Pharmaceutical compositions comprising aromatase inhibitor // 2617510
FIELD: medicine, pharmacy.SUBSTANCE: this invention refers to low-dose pharmaceutical compositions comprising an aromatase inhibitor 4.4-'[fluoro-(1-H-1,2,4-triazol-1-yl)methylene]bisbenzonitril as an active ingredient in a suitable carrier. Furthermore, this invention refers to the process for their preparation and application as medicaments.EFFECT: invention expands the range of low-dose pharmaceutical compositions comprising the aromatase inhibitor.11 cl, 4 ex, 4 tbl
ethod for diffuse toxic goiter complex treatment // 2614850
FIELD: medicine.SUBSTANCE: for complex treatment of diffuse toxic goiter, antithyroid drugs are used. At that, the patient takes thyrozol and beta-blocker egiloc until thyroid status compensation according to the template. Then, at supporting thyrotropic therapy background, the patient additionally takes, together with the same drugs, an inhibitor of angiotensin converting enzyme fosicard, 10 mg or 20 mg per day continuously, and an antioxidant agent mexidol, 125 mg or 250 mg two times a day, by 2 months courses with equal intervals, 3 times in year. In addition, performance of the cardiovascular system functions is monitored.EFFECT: complex treatment of diffuse toxic goiter.1 tbl, 2 ex

Testosterone compositions // 2613891
FIELD: medicine.SUBSTANCE: transdermal or transmucosal composition for treatment of testicular failure due to testicles abnormalities, Klinefelter syndrome, congenital abnormalities of sex chromosomes X and Y, retained testis, hemochromatosis, high levels of iron in blood, testicular trauma, previous hernia surgery, cancer treatment, normal ageing; secondary hypogonadism due to pituitary defects associated with brain that regulates hormone secretion, weakened testicular function, inflammatory diseases and application of drugs for treatment of psychiatric disorders and gastroesophageal reflux disease, ageing; and infertility, fatigue, loss of energy, depressed mood, regression of secondary sexual characteristics of male subjects, contains: 2 wt % of testosterone, C2-C4 alkanol, approx. 20 wt % of polyalcohol and monoalkyl ester of diethylene glycol.EFFECT: composition has a good skin tolerability.34 cl, 13 dwg, 10 tbl, 8 ex

Composition for controlled ovarian stimulation // 2613324
FIELD: medicine.SUBSTANCE: group of inventions relates to medicine and is applicable for treating sterility in patient. Follicle-stimulating hormone (FSH) is used in preparing drug for treating sterility in patient. If patient has serum level antimuller hormone (AMH) less than 15 pmol/l, drug contains daily dose equal or equivalent to 11–13 mcg of recombinant FSH (rFSH). Wherein said rFSH includes α2,3- and α2,6-sialylation, where from 1 to 99 % of total sialylation is α2,6-sialylation and from 1 to 99 % of total sialylation is α2,3-sialylation. If patient has serum level of AMH level no less than 15 pmol/l, drug is intended for introduction in daily dose equal or equivalent to 0.09 to 0.19 mcg of human rFSH per kg of patient's body weight. Wherein said rFSH includes α2,3- and α2,6-sialylation, where from 1 to 99 % of total sialylation is α2,6-sialylation and from 1 to 99 % of total sialylation is α2,3-sialylation.EFFECT: use of group of inventions provides effective treatment of sterility in patient.10 cl, 8 dwg, 12 tbl, 11 ex
Lypotherapy method // 2610006
FIELD: medicine.SUBSTANCE: invention refers to the medicine, cosmetology, and lypotherapy. Injections are performed in a prone position and in a supine position. HYALREPAIR-08 the Vitasomal complex (VSC-08) and HYALREPAIR-10 the Vitasomal complex (VSC-10) are injected into biologically active points (BAP) of the local and general impact according to the formulation of the invention. BAPs of the local impact are localized in the projections of nerve exit points performing sensitive and motor innervation of the viscera (liver, pancreatic gland, urinary system). BAPs of the general impact are localized above the projection of the spinal nerve exit points along the main nerve stems of the limbs, trunk, and neck nervous plexus.EFFECT: method of improvement of physical state, mood, increasing of productivity, normalization of clinical and biochemical performance of blood by means of continuous prolonged, for the entire period of biodegradation, mild pressor impact on the acupuncture point by the administered complex, as well as by means of the local impact on tissues with assured hitting a target-organ of general positive impact on the organism.6 cl, 2 tbl, 2 ex
Progesterone antagonists // 2608521
FIELD: pharmaceutics.SUBSTANCE: invention relates to compounds of formula (I) possessing antiprogestin properties, and to a method for treating breast cancer using such compounds. In general formula (I) X is O; R1, R2, R3 and R4 is hydrogen atoms; R5 is a radical Y, Y is acetyl, C3-cycloalkyl or pyridinyl; R6 is -OH; and R7 is a radical of formula CnFmHo, where n is 3, m is 2 or 3, o is 2 or 3 and m plus o is equal to 5.EFFECT: disclosed is a compound of formula (I) possessing antiprogestin properties.5 cl, 1 tbl, 4 ex

Growth hormones with prolonged efficacy in vivo // 2605627
FIELD: biotechnology.SUBSTANCE: invention relates to biotechnology. Conjugate of growth hormone (GH) is disclosed, containing GH with single mutation of Cys addition, selected from A98C, N99C, L101C and V102C, and albumin-binding radical, attached through hydrophilic spacer to sulphur atom of this single Cys. Conjugate of growth hormone with specific alternative hydrophilic spacers for attachment of albumin-binding radical is also disclosed.EFFECT: this invention can be used in production of growth hormone conjugates with increased stability and longer half-life in vivo.14 cl, 2 dwg, 6 tbl, 51 ex

Parathyroid hormone analogs and uses thereof // 2604809
FIELD: biotechnology.SUBSTANCE: invention relates to biotechnology, particularly to receipt parathyroid hormone (PTH) receptor agonists, and can be used in medicine. Obtained peptide or its pharmaceutical salt is used in a pharmaceutical composition for the treatment of diseases characterized by PTH dysfunction or with calcium or phosphate imbalances.EFFECT: invention provides to obtain PTH agonist with a longer acting effect in comparison with a natural hormone PTH (1-34).21 cl, 20 dwg, 3 tbl, 9 ex

Pharmaceutical composition // 2604690
FIELD: pharmaceutics.SUBSTANCE: invention relates to a liquid pharmaceutical composition containing from 0.05 mg/ml to 0.5 mg/ml of carbetocinum or its pharmaceutically active salt. pH value of the composition ranges from 5.1 to 5.9. Composition may additionally contain a buffer agent, an antioxidant and an agent for maintaining isotonicity. Liquid pharmaceutical composition containing from 0.01 to 4 mg/ml of pharmaceutically active compound FE 202767 or its pharmaceutically acceptable salt is also described. pH value of the composition ranges from 5.1 to 5.9. Kits containing said liquid pharmaceutical compositions are also described.EFFECT: pharmaceutical compositions have improved stability.22 cl, 7 dwg, 7 tbl, 9 ex

ethod of producing medicinal agent for correction of thyroid functions // 2601917
FIELD: pharmaceutics.SUBSTANCE: invention relates to pharmaceutical industry, and method of preparing drug of herbal raw material for correction of thyroid function. Method of producing medicinal agent for correction of thyroid functions by extraction of roots and rhizomes of potentilla white, Baikal skullcap roots and roots and rhizomes of rosewort at ratio of 50 wt%, 25 wt%, 25 wt%, respectively, which are milled and extracted by 50-60 % ethanol under certain conditions.EFFECT: agent prepared as described above is characterized by high content of biologically active substances, effectively corrects thyroid dysfunction.1 cl, 7 tbl, 3 ex

Drug preparation based on indole-3-carbinol with increased epigenetic activity // 2601893
FIELD: pharmaceutics.SUBSTANCE: invention relates to pharmaceutical industry and can be used for production of medicinal agents, required in therapy of diseases of the reproductive system (pathology of mammary glands, uterus, endometrium). Therapeutic agent possessing epigenetic activity contains indole-3-carbinol and excipients: lactose, microcrystalline cellulose, modified corn starch, magnesium stearate or calcium stearate, enclosed in a capsule, which are made from hydroxypropyl methylcellulose, in the following quantity in one capsule, g: indole-3-carbinol 0.10-0.20; lactose 0.10-0.15; corn starch modified 0.05-0.15; microcrystalline cellulose 0.5-0.15; magnesium stearate or calcium stearate 0.001-0.004.EFFECT: invention allows to increase efficiency of release of indole-3-carbinol of dosage form and its conversion into diindolylmethane, which implements its diindolylmethane activity.1 cl, 3 dwg, 4 ex

New polymorphic form of a calciemetric compound // 2599789
FIELD: chemistry.SUBSTANCE: invention is related to a crystalline form {4-[(1R,3S)-3-((R)-1-naphthalene-1-YL-ethylamino) cyclopentyl] phenoxy} acetic acid, which can be used for treating, relieving symptoms or preventing the physiological disorders or diseases, associated with disturbed activity of a calcium-sensitive receptor (CaSR), such as hyperparathyroidism. Crystalline form has x-ray powder diffraction pattern, displaying characteristic peaks, expressed in angles 2θ, at approximately 8.8, 9.5, 12.3, 16.0, 18.3, 19.1 and/or 20.2 (±0.1 degrees) (its stress is the main).EFFECT: invention is also related to a pharmaceutical compound containing the said crystalline form, and methods for preparing it.17 cl, 12 dwg, 6 tbl, 6 ex

New polymorphic form of a calciemetric compound // 2599788
FIELD: chemistry.SUBSTANCE: invention is related to a crystalline form of X {4-[(1R, 3S)-3-((R)-1-naphthalene-1-ilethylamino) cyclopentyl] phenoxy} acetic acid, which can be used for treating, relieving or preventing the physiological disorders or diseases associated with disturbed activity of CaSR, such as hyperparathyroidism. This form has x-ray powder diffraction pattern, which demonstrates characteristic peaks expressed in 2θ, equal to approximately 8.0, 11.3, 11.4, 15.0, 18.2 and/or 21.5 degrees (±0.05 degrees) (underlined is the primary).EFFECT: invention is also related to a pharmaceutical compound containing the crystalline form of X, and methods for preparing it.19 cl, 10 dwg, 6 tbl, 5 ex

Crystalline solvate form of cortexolone-17alpha-propionate, a preparation method thereof and a pharmaceutical composition based thereon // 2599452
FIELD: pharmaceutics.SUBSTANCE: present group of inventions relates to a new crystalline solvate form IV of cortexolone-17α-propionate, a method for production thereof and a pharmaceutical composition based thereon. Crystalline solvate form IV of cortexolone-17α-propionate is shown on fig. 30. Crystalline solvate form IV of cortexolone-17α-propionate is obtained by crystallisation of the latter from a mixture of propylene glycol/water at the ratio of 1/1 or from a mixture of polyethylene glycol/water at the ratio of 1/1.EFFECT: combination of the said crystalline solvate form and at least one physiologically acceptable additive is used in pharmaceutics to treat urogenital pathologies, endocrine system pathologies, skin and/or skin appendages.8 cl, 30 dwg, 3 tbl, 9 ex

Thiohydantoin derivatives useful as androgen receptor antagonists // 2598854
FIELD: chemistry.SUBSTANCE: invention relates to organic chemistry, in particular to novel thiohydantoin derivatives of general formula (I) or pharmaceutically acceptable salts thereof, where Z is selected from CF3, C1-C3 alkoxy and halogen; Y is selected from halogen; W denotes oxygen; R3 and R4 are independently selected from C1-C4 alkyl, or R3 and R4 and a carbon atom, to which they are bonded, form a 3-6-member cycloalkyl ring; A1 denotes phenyl or pyridyl optionally substituted with one halogen; A2 is (CH2)mY1(CH2)nQ, where m and n are integers independently selected from 0-2, and where at least one of m or n is not equal to zero; Q is selected from C(O)NHR″, C(RxRy)C(O)NR″R1″, cyano, C(O)OR″, C(O)NR″R1″ and 5-member heteroaryl containing 2 heteroatoms selected from nitrogen, oxygen and sulphur; and Y1 is selected from a direct bond and -O-; R″ and R1″ are independently selected from hydrogen, C1-C6 alkyl, or NR″R1″ together form a 4-6-member heterocyclic ring additionally containing 0-1 oxygen atoms, where one carbon atom can be optionally substituted with one hydroxyl group; Rx and Ry are independently selected from hydrogen or methyl; or C(RxRy) together form a 3-5-member cyclic alkyl ring. Invention also relates to a pharmaceutical composition and a local pharmaceutical composition based on the thiohydantoin derivative of formula (I).EFFECT: technical result is obtaining novel thiohydantoin derivatives useful for antagonizing androgen receptor activity.17 cl, 1 tbl, 69 ex

Application of agent with modifying properties in relation to hormones of adrenal glands // 2598708
FIELD: medicine.SUBSTANCE: present group of inventions relates to medicine, specifically to therapy and endocrinology, and concerns application of an agent with modifying properties in relation to adrenal hormones. Method includes administering an effective amount of compound of formula I or a pharmaceutically acceptable salt thereof. For compound of formula I n equals 1; R is hydrogen, R1, R2 and R3 independently represent hydrogen, halogen or cyano group, provided that not more than one from R1, R2 and R3 denotes hydrogen, and R4 and R5 represent hydrogen. .EFFECT: efficient treatment of diseases and disorders, characterised by high level of stress hormones.24 cl, 2 dwg, 2 tbl, 8 ex

ethod for improvement of endometrial receptivity in patients suffering from infertility associated with endometriosis // 2597845
FIELD: medicine.SUBSTANCE: invention concerns improving endometrial receptivity in patients suffering from infertility associated with endometriosis. Method includes administering a 3 % kudesan preparation in drops in continuous mode for 3-6 months at 40-60 drops.EFFECT: method enables to improve endometrial receptivity in patients suffering from infertility associated with endometriosis, as well as positively affects ovulation processes, fertilisation and function of yellow body.3 cl, 1 dwg, 3 ex

New octapeptide compounds and their therapeutic application // 2595525
FIELD: pharmaceutics.SUBSTANCE: invention relates to novel octapeptide compounds of general formula (I), which have high affinity to some subtypes of somatostatin receptors. Invention also relates to pharmaceutical compositions containing said products and use thereof for preparing a drug R-AA1-cyclo-(AA2-Tyr3-D-TRP4-AA5-Val6-Cys7)-Thr8-NH2 (I).EFFECT: compounds are intended for treating pathological conditions or diseases, involving one or more somatostatin receptors.17 cl, 9 ex
Composition for treating metabolic disorders // 2586742
FIELD: pharmaceutics.SUBSTANCE: invention refers to pharmaceutical industry and represents composition containing vitamin B9, or folic acid, or folacin and myocardial inositol and alpha-lipoic acid for use in curative treating of polycystic ovary syndrome, sterility and menstrual disorders.EFFECT: invention provides the synergetic effect in treating females with polycystic ovary syndrome, improved spontaneous ovulation activity and considerable increase of frequency of pregnancy.6 cl

Parenteral pharmaceutical formulation in suspension, having sustained release, in low and ultralow dosage, in hormonal therapy in climacteric syndrome // 2582272
FIELD: medicine.SUBSTANCE: invention relates to medicine and represents pharmaceutical composition with sustained release for parenteral administration once a month. Composition is meant for hormonal replacement therapy in mammal females and contains oestradiol in amount of 0.25-1.0 mg in form of microparticles, where microparticles include oestradiol and cholesterol; progesterone in amount of 15 mg or 20 mg to 75 mg in the form of microparticles; surface-active agent; iso-osmotic agent; agent increasing viscosity; preserving agent and water filler. pH of composition ranges from 4 to 7. Microparticles have size from 1 to 100 mqm, and active substance is melted, sprayed, frozen and crystallised to obtain stable forms of active substances.EFFECT: invention consists in application of composition for treating symptoms and discomfort associated with climacteric syndrome in females with uterus.16 cl, 5 ex, 9 tbl, 3 dwg

ethod for correction of postoperative hypoparathyroidism // 2581023
FIELD: medicine.SUBSTANCE: invention refers to medicine, namely to experimental surgery and pathophysiology, and can be used for correction of postoperative hypoparathyroidism. For this purpose, there is obtained a cell culture of removed parathyroid glands. After establishing of hypocalcemia the following substance is transplanted into the edge of broadest muscle of back, once: 0.5 ml of 3-day culture, containing 2×104 of autologous cells of parathyroid glands.EFFECT: use of this method allows to correct postoperative hypoparathyroidism at early stages of its development due to functional activity of the transplanted cells of parathyroid glands.1 cl, 1 ex, 3 dwg, 1 tbl
ethod of treatment of threatened preterm labor // 2578476
FIELD: medicine.SUBSTANCE: invention relates to the treatment of threatening preterm labor. For this pregnant when the signs of threatening preterm birth vaginally administered drug utrozhestan 600 mg/day - 200 mg 3 times a day. When the positive dynamics dose reduced to 100 mg every 3 days until a preventive dose of 200 mg/day and continue its introduction 36 weeks of pregnancy. When the negative dynamics continued administration of the drug at a dose of 600 mg/day with ultrasound every 7 days until the length of the cervix ≥30 mm and continued until 34 weeks of pregnancy, gradually reducing the dose of 100 mg every 3 days.EFFECT: mode of administration provides effective treatment of threatening preterm labor with minimal side effects.1 cl, 3 ex
Beverage // 2578391
FIELD: food industry.SUBSTANCE: invention is related to a beverage. The beverage contains pure water and at least a combination of such ingredients as acetic acid, propionic acid and butanoic acid, methylpropionic acid and/or methylbutanoic acid. The beverage has the following relative ratio of the ingredients: acetic acid - 75% - 85%, propionic acid - 10% - 20%, butanoic acid - up to 10%, methylpropionic acid - up to 5% and methylbutanoic acid - up to 5%. The ingredients concentration in pure water is equal to 0.1% by volume - 1% by volume. Additionally, the beverage contains additives represented by sugar and/or a sweet substance and/or ethyl alcohol for the ingredients flavour masking.EFFECT: one proposes the usage of the said beverage for the prevention and/or treatment of testosterone level reduction, in particular, testosterone rush increase in a person, in particular, in a man.15 cl

8-azabicyclo[3,2,1]octan-8-carboxamide derivative // 2574597
FIELD: medicine, pharmaceutics.SUBSTANCE: invention refers to compounds of formula and their pharmaceutically acceptable salts having the property of 11β dehydrogenase hydroxysteroid type 1 (11βHSD1) inhibitor, based medicinal and therapeutic agents, a method for prevention or treatment with using them, and using them for treating 11βHSD1-mediated diseases, such as type 2 diabetes mellitus, impaired glucose tolerance, hyperglycemia, insulin resistance, lipid dismetabolism, hypertension, arterial sclerosis, angiosclerosis, etc. In formula (1) A represents a group, which is presented by formula ; R1a and R1b are identical or different, and each independently represents C1-6 alkyl, which can be optionally substituted by 1-3 halogen atoms; each of m and n independently represents an integer from 0 to 5; X1 represents hydroxyl or aminocarbonyl; Z1 represents a single bond, oxygen atom, sulphur atom, -SO-, -SO2- or -N(R3)-; R2 represents optionally substituted C1-6 alkyl, optionally substituted C3-7 cycloalkyl, optionally substituted C6-10 aryl, optionally substituted C7-16 aralkyl, optionally substituted 3-7-merous heterocycle, optionally substituted 3-7-merous heterocyclic C1-6 alkyl, optionally substituted 5-12-merous mono- or polycyclic heteroaryl, optionally substituted 5-12-merous mono- or polycyclic heteroaryl-C1-6 alkyl, or optionally substituted 5-7-merous cyclic amino group; R3 represents C1-6 alkyl, C3-7 cycloalkyl, C6-10 aryl, or C7-16 aralkyl; or its pharmaceutically acceptable saly.EFFECT: producing the pharmacologically acceptable salts possessing the property of 11β hydroxysteroid dehydrogenase type 1 (11βHSD1) inhibitor.42 cl, 47 tbl, 438 ex

ethod for producing dry refined extract of european bugleweed herb exhibiting thyreotropic action // 2574028
FIELD: medicine.SUBSTANCE: presented method involves extracting ground European bugleweed herb in 30-50% aqueous ethanol, evaporating the extract until alcohol is removed completely (2-3% of the initial volume), diluting with distilled water 1:4, processing in chloroform, evaporating an aqueous form after separating chloroform to an amount equal to that produced after the aqueous-alcoholic extract evaporated, drying the residue in a vacuum drying chamber at 60±2°C and grinding.EFFECT: producing dry extract of European bugleweed herb with minimum ballast substances.4 ex, 1 tbl
Tabletted dietary supplement containing iodine and selenium // 2573999
FIELD: medicine.SUBSTANCE: tabletted dietary supplement containing iodine and selenium, the rest - other substances, contains iodine and selenium in mass ratio approximately 2:1 in the iodine content of 100-400 mcg.EFFECT: simultaneous intake of iodine and selenium within normal daily requirement and in ratio providing balanced production of thyroid hormones by a thyroid.2 cl

Preventing hypoglycaemia in patients with type 2 diabetes mellitus // 2572703
FIELD: medicine.SUBSTANCE: group of inventions refers to medicine, namely to therapy and endocrinology, and is applicable to prevent severe symptomatic hypoglycaemia related to the blood glucose concentration of less than 50 mg/dl in type 2 diabetes mellitus. That is ensured by administering desPro36Exendin-4(1-39)-Lys6-NH2 (Lixisenatide) and/or its pharmaceutically acceptable salt, and metformin and/or its pharmaceutically acceptable salt in an individual in need thereof; the individual to be treated has min. HbA1c 8%. What is also presented is a pharmaceutical combination and using the combination.EFFECT: group of inventions provides controlling blood glucose and body weight over a period of time of 24 weeks in obese patients of 50 years or younger suffering type 2 diabetes mellitus.19 cl, 5 dwg, 29 tbl

Therapeutic agents based on diglycylyl ether derivatives and methods for using them // 2572596
FIELD: medicine, pharmaceutics.SUBSTANCE: invention refers to a method for inhibiting androgen receptor (AR) activity, which involves administering a therapeutically effective amount of a compound having a structure of formula into an individual in need thereof, wherein X represents CH2F, CH2Br, CH2I, CH2OG, CH2OGOG'; X' represents CH2F, CH2Cl, CH2Br, CH2I, CH2OJ''', CH2OG, CH2OGOG' or a fragment specified in the patent claim, X'' represents CH2OG or CH2OJ'''; each of J, J', J'' and J''' represents H; each of L, L', L'', Q, Q' and Q'' represents O; each of Z, Z' and Z'' represents CH; each of R1, R2, R1', R2', G, G' and G'' represents branched or unbranched unsubstituted C1-C10 alkyl. The invention also refers to compounds of formula II, specific compounds presented in cl. 23 of the patent claim, pharmaceutical compositions, use and methods for inhibiting which involve administering the above compounds.EFFECT: diglycylyl ether derivatives inhibiting activity of androgen receptor and N-terminal domain of the androgen receptor.30 cl, 20 dwg, 5 tbl, 13 ex

New therapeutic methods for using inecalcitol // 2571490
FIELD: medicine, pharmaceutics.SUBSTANCE: what is presented is using inecalcitol for treating and/or preventing rachitis, osteoporosis, osteomalatia, psoriasis, autoimmune diseases, such as multiple sclerosis, type I diabetes mellitus, hyperparathyroid, benign prostate hyperplasia, any kinds of cancer in doses containing from 1.5 mg/day to 4 mg at intervals specified in: every second day, once a day or twice a day.EFFECT: treating the patients suffering hormone resistant prostate cancer with inecalcitol, which implies no inadmissible toxicity or disease progression has been shown.10 cl, 4 dwg

Pyrazoline dione derivatives as nadph-oxidase inhibitors // 2569855
FIELD: chemistry.SUBSTANCE: invention relates to pyrazoline dione derivative of formula , as well as to its pharmaceutically acceptable salt, where R1 is selected from hydrogen; possibly substituted C1-C6alkyl; possibly substituted phenyl; possibly substituted C1-C6alkylphenyl; possibly substituted phenylC1-C6alkyl; possibly substituted pyridyl; possibly substituted C1-C6alkylpyridyl; and possibly substituted pyridylC1-C6alkyl; R2 is hydrogen; R3 is hydrogen; R4, R5, R6 and R7 are hydrogen; R8, R9, R10 and R11 are independently selected from hydrogen atoms and C1-C6alkyls; R12 is selected from hydrogen; -CHR17R18; possibly substituted C1-C6alkoxy-carbonyl, possibly substituted -C(O)-phenyl; possibly substituted C1-C6alkylphenyl; possibly substituted phenylC1-C6alkyl, possibly substituted C1-C6alkylheteroaryl or possibly substituted heteroarylC1-C6alkyl, where heteroaryl is selected from pyridyl, pyrrolyl, pyrimidinyl, furyl, imidazolyl, oxazolyl, isoxazolyl, pyrazolyl, 1,2,3-triazolyl, 1,2,4-triazolyl, 1,2,3-oxadiazolyl, 1,2,4-oxadiazolyl, 1,2,5-oxadiazolyl, 1,3,4-oxadiazolyl, 1,3,4-triazinyl and 1,2,3-triazinyl; R17 and R18 are independently selected from hydrogen; possibly substituted phenyl; possibly substituted heteroaryl, where heteroaryl is selected from pyridyl, pyrrolyl, pyrimidinyl, furyl, imidazolyl, oxazolyl, isoxazolyl, pyrazolyl, 1,2,3-triazolyl, 1,2,4-triazolyl, 1,2,3-oxadiazolyl, 1,2,4-oxadiazolyl, 1,2,5-oxadiazolyl, 1,3,4-oxadiazolyl, 1,3,4-triazinyl and 1,2,3-triazinyl; X is selected from O, NR12, S and S(O)2; n is integer number, selected from 0 and 1; with term "substituted" meaning that said group is substituted with 1-5 substituents, selected from "C1-C6alkyl", "C1-C6alkoxy" and "halogens". Invention also relates to pharmaceutical composition, based on formula (I) compound, intermediate compound of formula , method of obtaining formula (I) and (II) compounds.EFFECT: novel pyrazoline dione derivatives, useful for inhibition of activity or function of nicotinamide adenine dinucleotide phosphate-oxidase (NADPH-oxidase), have been obtained.17 cl, 2 tbl, 23 ex

ethod for integrated treatment of polycystic ovarian syndrome and obesity // 2566291
FIELD: medicine.SUBSTANCE: integrated treatment of polycystic ovarian syndrome and obesity is ensured by administering Yarina combined oral contraceptive 1 tablet in the morning, metformin 500 mg 2 tablets in the evening; body weight reduction is provided by taking Listata 120 mg 3 times a day with meals; normalising blood glucose and insulin is enabled by prescribing dry milled root artichoke 1.5 gram in the morning and evening 30 minutes before a meal; normalising lipid exchange requires taking Milk Thistle Oil Cakes biologically active food supplement 2.0 gram in the morning and evening 30 minutes before a meal during 3 months.EFFECT: method enables improving general health, reducing body weight, normalising lipid exchange, blood glucose and insulin, blood hormones, reducing ovary dimensions with minimising the risk of unavoidable obesity complications and adverse action on the body.24 tbl, 2 ex

Application of nkg2d inhibitors for treating cardiovascular and metabolic diseases such as type 2 diabetes // 2566264
FIELD: medicine, pharmaceutics.SUBSTANCE: claimed group of inventions relates to medicine, namely to endocrinology, and deals with treating diabetes mellitus of type 2. For this purpose a therapeutically effective quantity of means inhibiting the activation or signalisation of NKG2D, or blocking the interaction of NKG2D ligand binding is introduced.EFFECT: method provides the effective treatment of type 2 diabetes, including the correction of such manifestations of it as the cardiovascular system pathology, inflammatory and metabolic components.27 cl, 14 dwg, 1 tbl

Compositions and methods for oral administration of exenatide // 2566063
FIELD: medicine, pharmaceutics.SUBSTANCE: invention refers to medicine and concerns a composition containing an effective amount of exenatide, a protease inhibitor, ethylene diamine tetraacetic acid, omega-3 fatty acid and a coating, which inhibits exenatide splitting in an individual's stomach; the above composition represents a pharmaceutical composition for oral application for treating the diseases, wherein agonist action on glucan-like peptide (GLP-1) is favourable.EFFECT: invention provides the blood sugar control following the glucose administration.19 cl, 4 dwg, 2 tbl, 8 ex
 
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