New compounds

FIELD: pharmacology.

SUBSTANCE: invention relates to a new compound of the formula (I) or a pharmaceutically acceptable salt thereof having interferon α (IFN-α) and tumour necrosis factor α (TNF-α) inducer properties. The compounds may be useful as vaccine adjuvants. In the formula (I) R1 is n-C3-6alkyl; R2 is hydrogen or methyl; R3 is hydrogen or C1-6alkyl; m is an integer having a value of 1 to 4.

EFFECT: compounds can be used for treatment of allergic diseases and inflammatory conditions, for example, allergic rhinitis and asthma, infectious diseases and cancer.

15 cl, 7 ex

 



 

Same patents:

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention relates to methods of obtaining heteroaryl compounds, represented by structural formulae (I) or (II): where R1-R4 have values, given in subcl. 1,14 of the formula.

EFFECT: compounds can be used for treatment or prevention of cancer, inflammatory states, immunological states, etc.

29 cl, 20 ex

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention refers to a compound (I) or its pharmaceutically acceptable salt, which possess properties of selective phosphodiesterase inhibitors, and can be used for treating male erectile dysfunction. In compound (I) R1 represents C1-C6alkyl; R2 represents C1-6alkyl; R3 represents C1-C6alkyl; R4 represents C1-C6 alkyl; R5 means H. The above salt is formed by the compound of formula (I) and an acid specified in citric acid, oxalic acid, hydrochloric acid, sulphuric acid, phosphoric acid, maleic acid, fumaric acid, tartaric acid, hydroxysuccinic acid, succinic acid, methane sulphonic acid or n-toluene sulphonic acid. A preferential compound is 5-[2-ethoxy-5-(4-methyl-1-homopiperazinylsulphonyl)]phenyl-1-methyl-3-n-propyl-1,6-dihydro-7H-pyrazolo[4,3-d]pyrimidin-7-one.

EFFECT: preparing the pharmaceutically acceptable salt that possesses the properties of selective phosphodiesterase inhibitors.

7 cl, 1 tbl, 5 ex

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention relates to novel compounds of formula (I), possessing properties, making it possible to inhibit phosphorylation of AKT (proteinkinase B; PKB), to versions of method of their obtaining, as well as to intermediate products for their obtaining. In particular compounds can be applied in treatment of different tumours and/or metastases, as well as in case parasitic diseases such a malaria. In formula (I), R1 stands for -L-phenyl or -L-heteroaryl, with term "heteroaryl" standing for bicyclic radical, containing from 9 to 12 units, L stands for either linear or branched alkyl, containing 1-6 carbon atoms, optionally substituted with hydroxyl, or CO group, or group L'-X, where L' stands for linear or branched alkyl, containing 1-6 carbon atoms, and X stands for oxygen or sulphur atom; with phenyl and heteroaryl being optionally substituted with one or several radicals, similar or different, selected from halogen atoms, -NRxRy, alkoxy and alkyl; with said alkyl being optionally substituted with one or several halogen atoms; R2 stands for hydrogen atom or alkyl; R3 stands for alkyl, optionally substituted with one or several halogen atoms; R4 stands for hydrogen atom or halogen atom; with NRxRy being such that Rx and Ry form together with nitrogen atom, which they are bound to, cyclic radical, including 3-10 units, and optionally oxygen atom; and all alkyl or alkoxy radicals, mentioned above, are linear or branched and contain 1-6 carbon atoms.

EFFECT: compounds can be applied as active component for obtaining medications, intended for treatment or prevention of disease, characterised by deregulation of protein- or lipidkinase activity.

25 cl, 3 tbl, 43 ex

FIELD: chemistry.

SUBSTANCE: invention relates to compounds of structural formula

,

having Aβ42 secretion inhibiting activity. In formula I , hetaryl I is a five- or six-member heteroaryl group containing 1-3 heteroatoms selected from O, S or N, hetaryl II is a five- or six-member heteroaryl group containing 1-3 heteroatoms as defined above for hetaryl I, or is a bicyclic ring system containing 1-4 heteroatoms selected from S, O or N, where at least one ring is aromatic by nature, R1 is C1-7-alkyl, C1-7-alkoxy, C1-7-alkyl substituted with a halogen, or a halogen; R2 is a halogen, C1-7-alkyl, C1-7-alkoxy, hydroxy, C1-7-alkyl substituted with a halogen, C1-7-alkyl substituted with a hydroxy, or benzo[1,3]dioxolyl or is -(CHR)p-phenyl, optionally substituted with a halogen, C1-7-alkyl, C1-7-alkoxy, S(O)2-C1-7-alkyl, cyano, nitro, C1-7-alkoxy substituted with a halogen, dimethylamino, -(CH2)p-NHC(O)O-C1-7-alkyl or C1-7-alkyl, substituted with a halogen. The values of radicals R, R3, R4,p, n, m, o are given in the claim.

EFFECT: invention relates to a method of producing said compounds, a medicinal agent containing said compounds and a method of treating Alzheimer's disease, cerebral amyloid angiopathy, Hereditary cerebral hemorrhage with amyloidosis-Dutch type (HCHWA-D), vascular dementia, dementia pugilistica or Down syndrome, associated with β amyloid activity.

21 cl, 283 ex

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention relates to 5,5-condensed heteroarylene compounds IIIB, where U2, V1, V2 and W1 are selected from O, N, NH, S or CR3a; U1, W2, X1 and X2 represent C or N; R1 and R2 represents hydrogen, -C(O)CH(NR1bR1c)R1a, -C(O)CH(N(R1c)C(O)OR1b)R1a or -C(O)OR1a; R3a represents hydrogen or R3; R3 represents halogen or -C(O)OR1a; L1 and L2 are such as given in invention formula, each Z1 and Z2 represents bond or -O-; each Rla, R1b and R1c represents hydrogen, C1-6 alkyl or C6-14 aryl; or Rlb and Rlc together with N atom, which they are bound to, form 5-6-membered heterocyclyl; q, r, s, t and u equal 1. Invention also relates to pharmaceutical compositions, containing 5,5-condensed heteroarylene compounds, and methods of treating or preventing HCV infection.

EFFECT: 5,5-condensed heteroarylene derivatives, possessing inhibiting activity with respect to hepatitis C virus.

43 cl, 42 ex

FIELD: chemistry.

SUBSTANCE: invention relates to a method of obtaining a formula compound. The method includes a stage of binding a formula compound with a formula compound in the presence of a base with the formation of the formula (I) compound. In formula (I) stereochemical configurations in the positions, marked with asterisks, are relative; Rb represents hydrogen; R00 represents a C1-10 aliphatic group or a C6-14 aryl group, including one-three rings; Rd, Re, Re', Rf, Rh, Rh', Rk represent hydrogen; Rg represents chlorine, fluorine, iodine or bromine; Rm represents a protective hydroxyl group; values of radicals Ra, R*, Rc are given in the invention formula. In formulas (II) and (III) Ra, Rb, Rc, Rd, Re, Re', Rf, Rg, Rh, Rh', Rj, Rk and Rm are such as determined in formula (I) and R1 represents -CH2CHO. The invention also relates to methods of obtaining compounds of formulae (V), (VI), (VId) and to a compound of the structural formula (IIa). Structural formulae of compounds (V), (VI), (VId), (IIa) are given in the invention formula.

EFFECT: method makes it possible to carry out synthesis in a regioselective way and use the obtained product without purification.

15 cl, 1 tbl, 26 ex

Ethinyl derivatives // 2553461

FIELD: medicine, pharmaceutics.

SUBSTANCE: claimed invention relates to ethinyl derivatives of formula I, where X represents N or C-R1; Y represents N or C-R2; Z represents CH or N; R4 represents 6-membered ring, containing 0, 1 or 2 nitrogen atoms, possibly substituted with 1-2 groups, selected from halogen, lower alkyl, lower alkoxy or NRR'; R1 represents hydrogen, lower alkyl, lower hydroxyalkyl, lower cycloalkyl or represents 5-6-membered heterocycloalkyl, containing 1-2 heteroatoms, selected from O and N; R2 represents hydrogen, CN; R and R' independently on each other represent hydrogen; or their pharmaceutically acceptable salts or acid-addition salts. Invention also relates to pharmaceutical composition, possessing activity of positive allosteric modulator of mGluR5 receptor, including effective quantity of at least one invention compound, and to application of invention compounds for manufacturing medication for treatment or prevention of diseases, associated with positive allosteric modulators of mGluR5 receptor.

EFFECT: obtained are novel compounds, which can be applied as positive allosteric modulator of mGluR5 receptor.

14 cl, 51 ex

FIELD: chemistry.

SUBSTANCE: invention describes a method of producing and a method of purifying dialkyl pemetrexed of formula (I) , having antifolate action. The compound can be used to treat non-small-cell cancer and, coupled with cisplatin, to treat malignant pleural mesothelioma of the lungs. The method includes reacting a carboxylic acid of formula (II) with a diester of glutamic acid of formula (III) or an acid-addition salt thereof. The process is carried out in the presence of a substituted triphenyl phosphate of formula (IV) , a base and a solvent. In formulae (I) and (III) each R1 and R2 independently represents alkyl groups. In formula (IV) X, Y and Z assume values given in the claim.

EFFECT: use of safe, mild, cheap, non-oxidising and easy to handle triphenyl phosphate simplifies the process and enables to obtain, for example, diethyl pemetrexed with purity higher than 99%.

14 cl, 12 ex

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention relates to field of organic chemistry, namely to novel heterocyclic compounds of formula (1) and/or to their pharmaceutically acceptable salts, where A1 represents CH; A4and A5 independently represent CR2 or N; A2 and A3 together with ring B represent 5-membered heteroaryl or heterocycle, with said 5-membered heteroaryl or heterocycle being selected from where t represents 1 or 2; and R3 is independently selected from H, C1-C6 alkyl, C6-aryl, C3-C6-membered cycloalkyl, C(O)NRcRd, -ORb, heteroaryl, representing pyridine, and heterocycle, representing piperidine and tetrahydropyran; and each of said alkyl, aryl, cycloalkyl, heteroaryl and heterocycle can be substituted with one group, independently selected from C1-C6 alkyl, possibly substituted with one substituent, selected from -CONMe2, C3-membered cycloalkyl, -CN, -OMe, -pyridine, tetrahydropyran, -CO-morpholine, -CO-pyrrolidine, (3-methyl)oxetane; -OH; -C(O)Ra; -CN; -C(O)NRcRd; -NRcRd; -ORb; -S(O)nRe; halogen, and substituted with one group -COMe heterocycle, representing piperidine, on condition that when A4 represents CR2, A2 and A3 together with ring B are selected from structure (3), (5) or (6); represents single bond or double bond; R1 represents heteroaryl, representing 6-membered or 9-10-membered aromatic mono- or bicyclic ring, containing 1-3 heteroatoms, selected from nitrogen, oxygen and sulphur; possibly substituted with one or two groups, independently selected from C1alkyl, C2alkinyl, -NRcRd, -NRcS(O)nRe, -ORb, halogen, halogenalkyl; R2 is independently selected from H; each Ra, Rb, Rc, Rd, and Re is independently selected from H; C1-C4alkyl, possibly substituted with one substituent, selected from -OH, -OMe, -CN, -NH2, -NMe2, C3-cycloalkyl; C2-C3alkenyl; C3alkinyl; C6aryl, possibly substituted with one or more substituents, selected from fluorine or methyl group; C3-membered cycloalkyl, possibly substituted with one substituent, selected from -OH and -CN; halogenalkyl; heteroaryl, representing pyridine; and substituted with one methyl group heterocycle, representing piperidine, or Rc and Rd together with atom (atoms) which they are bound to form 5-6-membered heterocyclic ring, representing pyrrolidine or morpholine; and in each case n is independently equal 2. Invention also relates to particular compounds, pharmaceutical composition, based on claimed compounds; method of inhibiting PI3K and/or mTOR activity and to application of claimed compounds.

EFFECT: novel compounds, useful for inhibiting PI3K and/or mTOR activity have been obtained.

15 cl, 16 ex

FIELD: chemistry.

SUBSTANCE: claimed invention relates to a method of obtaining methyl ether of 3-[(4S)-8-bromo-1-methyl-6-(2-pyridinyl)-4H-imidazo[1,2-a][1,4]benzodiazepin-4-yl]propionic acid and benzosulphonate of methyl ether of 3-[(4S)-8-bromo-1-methyl-6-(2-pyridinyl)-4H-imidazo[1,2-a][1,4]benzodiazepin-4-yl]propionic acid, which includes the interaction of methyl ether of 3-[(S)-7-bromo-2-((R and/or S)-2-hydroxypropylamino)-5-pyridin-2-yl-3H-benzo[e][1,4]diazepin-3-yl]propionic acid with an oxidiser and, optionally, processing the reaction product in acidic conditions, as well as to intermediate compounds and .

EFFECT: simplification and reduction of the price of the obtaining method due to the reduction of the number of stages.

13 cl, 8 ex

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention relates to compound, represented by the following formula

,

or its pharmaceutically acceptable salt. In claimed formula each symbol has values, determined in formula of invention. Versions of formula [I] compound and particular compounds are also objects of invention. In addition, invention relates to pharmaceutical composition, ITK inhibitor and means for treatment or prevention of inflammatory diseases, allergic diseases, autoimmune diseases, transplant rejection and other diseases and methods of treating said diseases.

EFFECT: claimed compounds inhibit induced T-cellular kinase (ITK).

32 cl, 86 tbl, 387 ex

Antiallergic agent // 2553354

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention refers to pharmaceutical industry and represents an anti-allergic agent containing polysaccharide containing galactose, glucose and rhamnose as ingredients, wherein polysaccharide contains galactose, glucose and rhamnose in molar ratio 3-5:1-3:1, and polysaccharide has certain structure.

EFFECT: invention provides extending the range of antiallergic agents.

12 cl, 6 ex, 6 dwg, 1 tbl

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention relates to pharmaceutics. A medication represents derivatives of glutarimides of the general formula (I) or their pharmaceutically acceptable salts. The invention also relates to pharmaceutical compositions and a method of treatment.

EFFECT: ensured by the application of non-toxic derivatives of the said glutarimides for the treatment of eosinophilic diseases, mainly of an allergic origin.

16 cl, 12 tbl, 7 ex

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention refers to medicine, particularly to pharmaceutical industry, and describes a tabletted oral dosage form containing desloratadine in an amount of 3 to 15%, processing additives and a pharmaceutically acceptable excipient. The processing additives consist of sodium croscarmellose, magnesium stearate and povidone. The excipient represents a mixture of lactose disaccharide and microcrystalline cellulose polysaccharide in ratio from 2:1 to 8:1. Lactose and microcrystalline cellulose have an average particle size from 30 to 200 mcm. Producing the table involves granulating desloratadine, lactose and microcrystalline cellulose.

EFFECT: invention provides reducing granulate compression force, increasing process capability and maintaining the high quality of the tablets.

9 cl, 4 tbl, 4 ex

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention relates to the field of medicine, namely to immunology and allergology, and can be used for the treatment of allergy to house dust mites. For this purpose an allergotropine is obtained by a method of chemical conjugation of an allergoid and synthetic highly molecular immunomodulator Polyoxidonium. The allergotropine contains 1000±200 PNU of the allergoid of house dust mites Dermatophagoides pteronyssinus or Dermatophagoides farinae and 6.25±1.25 mg of Polyoxidonium.

EFFECT: obtaining the allergotropines, based on the allergoid forms of allergens of house dust mites Dermatophagoides pteronyssinus or Dermatophagoides farinae, possessing more expressed immunogenic and hyposensitising properties in comparison with the native allergen, makes it possible to carry out the effective treatment of allergy by ASIT method.

2 ex, 2 tbl, 2 dwg

FIELD: pharmacology.

SUBSTANCE: invention mainly relates to a food composition, including punicalagins.

EFFECT: improved action in respect to health improvement.

8 cl, 1 tbl, 1 ex

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention refers to microbiology. What is presented is using the strain Bifidobacterium longum NCC 2705 (CNCM-I2618) for preparing a complete nutrient composition used for relieving symptoms of allergy to food in the patients suffering allergies caused by ingestant allergens.

EFFECT: composition provides the secondary prevention of allergic reactions caused by the above ingestant allergens.

16 cl, 7 dwg, 1 ex

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention relates to complex injection preparation for treating polynoses by ASIT method. Said preparation is obtained by simple mixing birch pollen allergoid and muramylpeptide without carrying out chemical conjugation of components, with 2 mg of muramylpeptide being added per 1000 PNU dose.

EFFECT: invention provides considerable enhancement of immune response and stimulates high level of production of specific IgG-antibodies, as well as makes it possible to reduce course of treatment of polynoses, which reduces possibility of complications.

1 dwg, 2 tbl

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention relates to field of pharmaceutics and represents composition for reducing injury caused by ultraviolet radiation, which includes one or more compounds selected from the group consisting of D-methionine and its salts.

EFFECT: invention provides creation of stable and safe composition, which can be applied daily.

10 cl, 37 ex, 7 dwg

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention refers to pharmaceutical industry and medicine, namely to manufacturing drug preparations for treating allergic diseases, such as allergic rhinitis and urticaria. According to the first version, the pharmaceutical composition contains an active substance that is desloratadine, and additives, including citric acid, calcium hydrogen phosphate dihydrate, microcrystalline cellulose, starch, lactose, magnesium stearate, and talc. According to the second version, the pharmaceutical composition contains an active substance that is desloratadine, and additives, including Pearlitol 100SD-Mannitol, calcium hydrogen phosphate dihydrate, microcrystalline cellulose, starch, magnesium stearate, and talc. According to the third version, the pharmaceutical composition contains an active substance that is desloratadine, and additives, including sodium carboxymethyl starch, microcrystalline cellulose, colloidal silicone dioxide, and sodium sodium stearyl fumarate. According to the fourth version, the pharmaceutical composition contains an active substance that is desloratadine, and additives, including sodium carboxymethyl starch, microcrystalline cellulose, Pearlitol 100SD-Mannitol, magnesium stearate, and talc. The pharmaceutical composition is presented in the form of a film-coated tablet.

EFFECT: pharmaceutical composition according to the invention is storage-stable and releases the active substance quickly in the gastrointestinal tract.

10 cl, 9 tbl, 20 ex

FIELD: chemistry.

SUBSTANCE: present invention relates to biotechnology and provides a α1,6-glucan-containing compound of Helicobacter pylori. The present invention also discloses a conjugate for inducing immune response against H.pylori, which contains said compound conjugated with a carrier protein. The present invention also discloses an immunogenic composition, use of said composition and a method of inducing immune response against H.pylori using said composition. The present invention also discloses immune serum for neutralising H.pylori in mammals, which is obtained by immunising said mammal with an immunogenic composition containing said immunogenic composition. The present invention discloses an antibody which recognises said α1,6-glucan-containing compound of H.pylori, use of said antibody and a method of inducing complement-mediated bacteriolysis of H.pylori strains which express α1,6-glucan using said antibody.

EFFECT: invention improves the effectiveness of immunogenic compositions against Hpylori.

27 cl, 8 dwg, 21 tbl, 11 ex

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