Diazinopyrimidines and pharmaceutical composition containing them

FIELD: chemistry.

SUBSTANCE: novel chemical compounds of formula (I) or their pharmaceutically acceptable salts possess inhibiting activity with respect to kinase p-38 MAP and kinase FGFR, and can be used in treatment of such diseases as arthritis, obstructive lung disease, Alzheimer's disease or oncological and other diseases. In general formula (I) , R1 is hydrogen, R2 is 6-member oxygen-containing heterocyclyl, aryl, selected from unsubstituted phenyl or phenyl substituted with aliphatic acyl group which contains 1-6 carbon atoms, halogen cyano, hydroxyl, C1-6alkylsulfinyl, C1-6alkylsulfonyloxy, C1-6alkylsulfonyl, C1-6alkylsulfanyl, tret-butydimethylsilanyloxy, 6-member heterocyclyl, containing 1-2-heteroatoms, selected from nitrogen and oxygen, R3 is C1-6alkyl, Ar1 is phenyl, substituted with 1-2 substituents, selected from atoms of halogen, C1-6alkyl, C1-6alkoxy, C1-6alkylamino, di(C1-6alkyl)amino, X1 is oxygen and X2 is chemical bond.

EFFECT: efficient application of invention compounds in pharmaceutical composition.

13 cl, 1 tbl, 64 ex

 

The text descriptions are given in facsimile form.

1. Soy is inania formula

or its pharmaceutically acceptable salt, where

R1means hydrogen,

R2mean 6-membered oxygen-containing heterocyclyl, aryl, selected from unsubstituted phenyl or phenyl substituted aliphatic acyl group containing 1-6 carbon atoms, halogen, cyano, hydroxyl,

With1-6alkylsulfonyl,1-6alkylsulfonate,1-6alkylsulfonyl,1-6alkylsulfanyl, trebuchetgreenhill, 6-membered heterocyclyl containing 1 to 2 heteroatoms selected from nitrogen and oxygen,

R3means C1-6alkyl,

Ar1means phenyl substituted with 1-2 substituents selected from halogen atoms,

C1-6of alkyl, C1-6alkoxy, amino, C1-6alkylamino, di(C1-6alkyl)amino,

X1means oxygen and

X2means a chemical bond.

2. The compound according to claim 1, where R2means unsubstituted phenyl or phenyl substituted aliphatic acyl group containing 1-6 carbon atoms, halogen, cyano, hydroxyl, C1-6alkylsulfonyl,1-6alkylsulfonate, C1-6alkylsulfonyl,1-6alkylsulfanyl, trebuchetgreenhill, 6-membered heterocyclyl containing 1 to 2 heteroatoms selected from the zhota and oxygen

3. The compound according to claim 1, where R2means heterocyclimamines, C1-C6alkylsulfonyl, C1-C6alkylsulfonyl, phenyl, halogenfree, hydroxyphenyl, C1-C6allfeel, cyanophenyl, C1-C6alkylsulfonamides.

4. The compound according to claim 1, where R2means heterocyclimamines,

C1-C6alkylsulfonyl, C1-C6alkylsulfonyl, phenyl or halogenfree.

5. The compound according to claim 1, where Ar1mean 2-halogenfrei, 4-halogenfrei, 2,4-dehalogenans, 2,6-dehalogenans, 2-C1-C6alkylphenyl, 1-C1-C6alkoxyphenyl, 2-C1-C6alkoxyphenyl, 4-C1-C6alkoxyphenyl, 3,5-di-C1-C6alkoxyphenyl, 2-halogen-5-C1-C6alkoxyphenyl or 2-di-C1-C6alkylamino-6-forfinal.

6. The compound according to claim 3 where R3means methyl.

7. The connection according to claim 6, where R2means of 4-(morpholine-4-yl)phenyl.

8. The connection according to claim 7, where Ar1mean 2-bromophenyl.

9. The connection according to claim 7, where Ar1means 2,6-dichlorophenyl.

10. The connection according to claim 6, where R2mean 3-methylsulfinylphenyl.

11. The connection of claim 10, where Ar1mean 2-bromophenyl.

12. Pharmaceutical composition having inhibitory activity against the kinase p-38 MAP kinase FGFR, including

(a) with the Association according to any one of claims 1 to 5 in an effective amount, and

(b) pharmaceutically acceptable excipient.

13. The compound of the formula

where n is 0, 1 or 2,

R7means C1-6alkyl,

R3, Ar1X1X2have the meanings indicated in claim 1;

provided that excluded the following compounds: 7-methylsulfanyl-1,3-diphenyl-1H-pyrimido[4,5-e][1,3,4]thiadiazin, 7-methanesulfonyl-3-phenyl-1H-pyrimido[4,5-e][1,3,4]thiadiazin and 7-methylsulfanyl-1,3-diphenyl-1H-pyrimido[4,5-e][1,3,4]oxadiazine.



 

Same patents:

FIELD: chemistry.

SUBSTANCE: claimed are novel pyrazole derivatives of formula II or its pharmaceutically acceptable salts, where C ring is selected from phenyl or pyridinyl ring and R2, R2', Rx and Ry are such as said in given description. C ring has ortho-substituent and is optionally substituted in non-ortho positions. R2 and R2' , optionally taken with their intermediate atoms, form condensed ring system, such s indazole ring, and Rx and Ry, optionally taken together with their intermediate atoms, form condensed ring system, such a quinazoline ring.

EFFECT: possibility to use compositions as inhibitors of protein kinases as inhibitors GSK-3 and other kinases and apply them for protein kinase-mediated diseases.

41 cl, 8 tbl, 423 ex

FIELD: chemistry.

SUBSTANCE: invention relates to application of the substituted esters of 1,2,3,7-tetrahydro-pyrrolo [3,2-f][1,3]benzoxazine-5-carboxylic acid of general formula 1 or their racemoids, or their pharmaceutically acceptable and/or hydrates as substances of pharmaceutical compositions having anti-influenza virus activity: , where: R1 and R4 independently represent amines substitute selected from hydrogen, optionally substituted by liner or branched alkyl, containing 3-12 carbon atoms, optionally substituted cycloalkyl containing 3-10 carbon atoms, optionally substituted aryl, and probably, annelated heterocyclyl, which can be aromatic or non-aromatic and contains from 3 to 10 atoms in the ring, with one or several heteroatoms selected from nitrogen, oxygen or sulphur or their oxides; R2 represents alkyl substitute selected from hydrogen, optionally substituted mercapto group, optionally substituted amino group, optionally substituted hydroxyl; R3 represents lower alkyl; R5 represents substitute of the cyclic system selected from hydrogen, optionally substituted linear or branched alkyl, containing 3-12 carbon atoms, optionally substituted cycloalkyl containing 3-10 carbon atoms optionally substituted aryl or optionally substituted and optionally substituted annelated heterocyclyl, which can be aromatic or non-aromatic and contains from 3 to 10 atoms in the ring with one or several heteroatoms selected from nitrogen, hydrogen or sulphur or their oxides; R6 represents substitute of cyclic system selected from hydrogen, halogen atom, cyano group, optionally substituted aryl or optionally substituted annelated heterocycle, which can be aromatic or non-aromatic and contains from 3 to 10 atoms in the ring with one or several heteroatoms selected from nitrogen, hydrogen or sulphur or their oxides.

EFFECT: production of the pharmaceutical compositions having anti-influenza virus activity.

12 cl, 2 dwg, 2 tbl, 5 ex

FIELD: chemistry.

SUBSTANCE: invention pertains to non-peptide antagonists GnRH, with general formula 1 , where each of A1, A2 and A3 are independently chosen from A5 and A6; and A4 represents either a covalent bond, or A5; under the condition that, if A4 is a covalent bond, then one of A1-A3 represent A6, and the other two represent A5, and that, if A4 represents A5, then all of A1-A3 represent A5; A5 is chosen from C-R13 and N; A6 is chosen from N-R14, S and O; R1 is chosen from H, NHY1 and COY2, and R2 represents H; or and R1, and R2 represents methyl or together represent =O; each of R3, R4 and R5 independently represents H or low alkyl; each of R6, R7, R8, R9, R10, R11 and R12 are independently chosen from H, NH2, F, CI, Br, O-alkyl and CH2NMe2; R13 is chosen from H, F, CI, Br, NO2, NH2, OH, Me, Et, OMe and NMe2; R14 is chosen from H, methyl and ethyl; W is chosen from CH and N; X is chosen from CH2, O and NH; Y1 is chosen from CO-low alkyl, CO(CH2)bY3, CO(CH2)bCOY3 and CO(CH2)bNHCOY3; Y2 is chosen from OR15, NRI6R17 and NH(CH2)cCOY3; Y3 is chosen from alkyl, OR15 and NR16R17; R15 represents H; each of R16 and R17 is independently chosen from H, low alkyl and (CH2)aR18, or together represent -(CH2)2-Z-(CH2)2-; R18 is chosen from OH, pyridyl, pyrizinyl and oxadiazolyl; Z represents NH; a represents 0-4; and b and c represent 1-3. The invention also relates to use of formula 1 a compound as a therapeutic agent and pharmaceutical composition, with antagonistic effect to GnRH receptor. Description is also given of the method of obtaining compounds with the given formula.

EFFECT: obtaining new compounds, with useful biological properties.

27 cl, 70 ex

FIELD: chemistry.

SUBSTANCE: invention relates to new compounds of the formula (1a) or its pharmaceutically acceptable salt, esters or imides where A is a thiophenyl group containing, probably, substitution, the thiophenyl group A containing, probably, substitution with one or several groups as follows: alkyl, halo or arylalkyl, Y is O, S or NR2 where R2 is hydrogen or alkyl group containing 1 to 6 carbon atoms, and R1 is an non-ramified alkyl group containing 6 to 25 carbon atoms, ramified alkyl group containing 6 to 25 carbon atoms, aryl alkyl group where the alkyl group contains 2 to 25 carbon atoms or phenyl group containing substitution with one or several groups as follows: phenyloxy, phenylthio, SO2-phenyl, alkylphenyl, CO-phenyl, CONR16- phenyl, NR16CO-phenyl or NR16 -phenyl containing, probably, substitution where R16 is hydrogen or alkyl group containing 1 to 4 carbon atoms, the groups phenyloxy, phenylthio, SO2-phenyl, alkylphenyl, CO-phenyl, CONR-phenyl or NR-phenyl containing, probably, substitution with one or several groups as follows: halo, alkyl, alkylhalo or phenyl group containing substitution with one or several groups or alkyl groups provided the above compound is not 5-methyl-2-(4-metoxyphenyl)amino-4H-thieno[2,3-d][1,3]oxazine-4-on, 6-amyl-2-(4-chlorophenyl)amino-4H-thieno[2,3-d][1,3]oxazine-4-on or 6-amyl-2-(4-metoxyphenyl)amino-4H-thieno[2,3-d][1,3]oxazine-4-on Invention also relates to method of obtaining compounds of the formula (Ia) or (IIa), to pharmaceutical compound and application, as well as cosmetic technique.

EFFECT: obtaining of new biologically active compounds and pharmaceutical compounds based on them.

27 cl, 4 ex, 1 tbl

FIELD: organic chemistry, medicine, pharmacy.

SUBSTANCE: invention relates to novel compounds of the formula (I): , wherein X represents heteroatom, such as oxygen (O) or sulfur (S) atoms; X and Z mean independently of one another one or some identical or different substitutes bound any available carbon atom and they can represent hydrogen atom or halogen atom; R1 represents a substitute of the formula (II): , wherein R2 and R3 can represent simultaneously or independently of one another hydrogen atom or (C1-C4)-alkyl, or R1 can represent hydrogen, halogen atom, (C1-C7)-alkyl, -CHO, -(CH2)2COOH, -(CH2)2CO2Et, (CH2)mL wherein L means -OH or bromine atom (Br); m represents a whole number from 1 to 3; n represents a whole number from 0 to 3; Q1 and Q2 represent independently of one another oxygen atom or group of the formula: wherein substitutes y1 and y2 represent hydrogen atom, and to their pharmacologically acceptable salts. Also, invention relates to use of these compounds as intermediate substances used in synthesis of novel compounds of dibenzoazulene class, and to their using for preparing drugs.

EFFECT: valuable medicinal properties of compounds.

9 cl, 4 tbl, 13 ex

FIELD: organic chemistry, medicine, pharmacy, chemical technology.

SUBSTANCE: invention relates to novel substituted esters of 1,2,3,7-tetrahydropyrrolo[3,2-f][1,3]benzoxazin-5-carboxylic acids of the general formula (1): or their racemates, or their optical isomers, or their pharmaceutically acceptable salts and/or hydrates possessing the antiviral effect. In compounds of the general formula (1) each R1 and R4 represents independently of one another a substitutes of amino group chosen from hydrogen atom, optionally substituted linear or branched alkyl comprising 3-12 carbon atoms, optionally substituted cycloalkyl comprising 3-10 carbon atoms, optionally substituted aryl or optionally substituted and possibly an annelated heterocyclyl that can be aromatic or nonaromatic and comprising from 3 to 10 atoms in ring with one or some heteroatoms chosen from nitrogen, oxygen or sulfur atoms or their oxides; R2 represents alkyl substitute chosen from hydrogen atom, optionally substituted mercapto group, optionally substituted amino group, optionally substituted hydroxyl; R3 represents lower alkyl or cycloalkyl; R5 represents a substitute of cyclic system chosen from hydrogen atom, optionally substituted linear or branched alkyl comprising 3-12 carbon atoms, optionally substituted cycloalkyl comprising 3-10 carbon atoms, optionally substituted aryl or optionally substituted and optionally an annelated heterocyclyl that can be aromatic or nonaromatic and comprising from 3 to 10 atoms in ring with one or some heteroatoms chosen from nitrogen, oxygen or sulfur atoms or their oxides; R6 represents a substitute of cyclic system chosen from hydrogen atom, halogen atom, cyano group, optionally substituted aryl or optionally substituted and optionally annelated heterocyclyl that can be aromatic or nonaromatic and comprising from 3 to 10 atoms in ring with one or some heteroatoms chosen from nitrogen, oxygen or sulfur atoms or their oxides. Also, invention relates to methods for treatment, drugs and pharmaceutical compositions using compounds of this invention. Proposed compounds can be used as active components of drugs used in treatment of such diseases as infectious hepatitis, human immunodeficiency, atypical pneumonia and avian influenza.

EFFECT: valuable medicinal properties of compounds and pharmaceutical composition, improved methods of synthesis.

22 cl, 3 tbl, 6 dwg, 7 ex

FIELD: organic chemistry, medicine, biochemistry, pharmacy.

SUBSTANCE: invention relates to novel azaheterocycles of the general formula (I): possessing inhibitory effect on activity of tyrosine kinase and can be used in treatment of different diseases mediated by these receptors. In compound of the general formula (1) W represents azaheterocycle comprising 6-13 atoms that can be optionally annelated with at least one (C5-C7)-carbocycle and/or possibly annelated with heterocycle comprising 4-10 atoms in ring and comprising at least one heteroatom chosen from oxygen (O), sulfur (S) or nitrogen (N) atom; Ra1 represents a substitute of amino group but not hydrogen atom, such as substituted (C1-C6)-alkyl, possibly substituted aryl and possibly substituted 5-10-membered heterocyclyl comprising at least one heteroatom chosen from O, S or N; Rb represents carbamoyl group -C(O)NHRa wherein Ra represents a substitute of amino group but not hydrogen atom, such as possibly substituted alkyl, possibly substituted aryl, possibly substituted 5-10-membered heterocyclyc comprising at least one heteroatom chosen from O, S or N; Rc represents a substitute of cyclic system, such as possibly substituted (C1-C6)-alkyl, possibly substituted aryl and possibly substituted 5-6-membered heterocyclyl comprising at least one heteroatom chosen from O, S or N; or Rb and Rc form in common aminocyanomethylene group [(=C(NH2)CN], or their pharmaceutically acceptable salts. Also, invention relates to methods for synthesis of these compounds (variants), a pharmaceutical composition, combinatory and focused libraries.

EFFECT: valuable medicinal properties of compounds and pharmaceutical composition, improved methods for synthesis and preparing.

35 cl, 16 sch, 13 tbl, 43 ex

FIELD: organic chemistry, pharmaceuticals.

SUBSTANCE: invention relates to compounds of general formula 1 (G1 is group of general formulae 2 G1 is group of general formulae ; meanings of the rest substituents are as described in specification) or pharmaceutically acceptable salts thereof and use thereof in srug production. Said compounds are useful in treatment of male and female sexual disorders.

EFFECT: new oxytocin antagonists.

30 cl, 177 ex

FIELD: organic chemistry, pharmaceuticals.

SUBSTANCE: invention relates to compounds of general formula I and pharmaceutically acceptable salt thereof, wherein R1, R3, R4, R5, and R10 are independently H, halogen, C1-C4-alkyl, etc.; R2 is H, halogen, NO2, etc.; R6 is H, C1-C6-alkyl, C1-C6-alkoxy-substituted C1-C4-alkyl, etc.; R7 is H, C1-C4-alkyl or C2-C4-alkenyl, optionally substituted with halogen; R8 and R9 are H, R11 and R12; meanings of the rest substituents are as define in specification.

EFFECT: new compounds with value biological properties and useful as drug having activity in relates to progesterone receptor.

15 cl, 3 tbl, 80 ex

FIELD: organic chemistry.

SUBSTANCE: invention relates to new method for production of E-2-aroylmethylene-1-phenyl-1,2,3,4-tetrahydroquinazolin-4-ones of general formula I wherein R represents H, methyl, Cl. Claimed method includes interaction of 5-aryl-2,3-dihydro-2,3-furandiones with N-phenylanthranyl acid amide in medium of inert aprotic solvent (preferably benzene) followed by isolation of target products. Process is carried out preferably at 79-80°C. Claimed compounds have fluorescent properties and are useful in labeling and copying agents, intermediates for synthesis of new heterocyclic compounds, etc.

EFFECT: new fluorescent compounds.

3 cl, 1 dwg, 3 ex

FIELD: medicine, pharmacology.

SUBSTANCE: invention relates to pharmaceutical means, particularly preventer of blood vessels intima hyperplasia, containing 3(2H)-pyridazinone substance, represented by formula (I) or its pharmaceutically suitable salt.

EFFECT: obtaining highly effective preventer of blood vessels intima hyperplasia; each of radicals R1, R2, R3, X, Y, and A, having parameters, detailed in description.

5 cl, 2 dwg, 5 ex

FIELD: chemistry.

SUBSTANCE: invention pertains to new substituted 2,3,4,5-tetrahydro-1N-pyrido[4,3-b]indoles with general formula 1.1, 1.2 or 1.3, their pharmaceutical salts and/or hydrates with antihistamine activity. In general formulae 1.1, 1.2 or 1.3 radicals assume values given below . In 1.1 compounds, R1 represents a substitute, chosen from hydrogen or unsubstituted C1-C5 alkyl; R2 represents a hydrogen atom or C1-C4 alkyl; R3i represents one or more single or different substitutes, chosen from hydrogen, halogen, C1-C3 alkyl or CF3; n=0 or 1-3; in 1.2 compounds R1 represents a substitute of an amino group, chosen from hydrogen or optionally substituted C1-C5 alkyl; R3 represents one or more single or different substitutes, chosen from hydrogen, halogen, C1-C3 alkyl or CF3, and Ar1 represents an aryl or heterocyclyl, containing at least one carboxyl and/or alkoxycarboxyl substitute or R3i represents a carboxyl and/or alkyloxycarboxyl substitute, and Ar1 represents optionally substituted aryl or heterocyclyl; in 1.3 compounds, R2 represents a hydrogen atom or C1-C4 alkyl; R3i represents one or more single or different substitutes, chosen from hydrogen, halogen, C1-C3 alkyl or CF3, and Ar2 represents optionally substituted aryl or heterocyclyl; k=0 or 1-4; m=1 or 2.

EFFECT: compounds can be used for making drug formulation for treating allergies, autoimmune diseases such as pollen allergy, urticaria, bronchial asthma etc.

17 cl, 10 dwg, 2 tbl,13 ex

FIELD: chemistry.

SUBSTANCE: new compounds with formula Ia are proposed, where: P represents pyridine or pyrimidine; R1 represents hydrogen; R2 is chosen from halogen, nitro, C0-6alkylheteroaryl, (CO)OR4, trifluoromethyl, C0-6alkylcyano, C0-6alkylNR4R5, OC1-6alkylNR4R5, C0-6alkylCONR4R5, C0-6alkyl(SO2)NR4R5 and X1R6 group, where X1 represents a direct link; R6 represents a 5- or 6-member heterocyclic group, containing one or two heteroatoms, independently chosen from N, O, and S, for which the given heterocyclic group can be unsaturated and can be substituted with by one substitute, chosen from W; m equals 0, 1, or 2; R3 is chosen from CO(OR4), C0-6alkylNR4R5, C0.6alkylCONR4R5, OC1-6alkylNR4R5 C1-6alkyl(SO2)NR4R5; n equals 1 or 2; R4 is chosen from hydrogen, C1-6alkyl; R5 is chosen from hydrogen, C1-6 alkyl, C0-6 alkyl C3-6 cycloalkyl, C0-6 alkylaryl, C0-6alkylheteroaryl and C1-6alkylNR14R15 or R4 and R5 together can form a 4-, 5-, 6- or 7-member heterocyclic group, containing one or more heteroatoms, independently chosen from N and O, where the given heterocyclic group can be substituted by group Y; and where any C1-6alkyl, indicated in defining R2-R5, can be substituted with one or more one Z group; R14 and R15 together can form a 5-member heterocyclic group, containing one or more heteroatoms, independently chosen from N and O; W and Z are independently chosen from halogen, CN, OR16, C1-6alkyl, trifluoromethyl, trifluoromethoxy, 5-member heterocyclic group, containing one heteroatom, independently chosen from N, for which the given heterocyclic group can be substituted with group Y; Y is chosen from oxo, halogen, C1-6alkyl, C0-6alkylaryl, NR16R17, phenyl, C0-6alkylaryl, where the phenyl and C0-6alkylaryl groups can be substituted with nitro, trifluoromethyl; R16 and R17 are independently chosen from hydrogen and C1-6alkyl, or where R16 and R17 together can form a 5-member heterocyclic group, containing one heteroatom, chosen from N; in form of a free base or pharmaceutical salt. Formula Ia compounds have inhibiting effect to glycogen-synthase-kinase-3 (GSK3). The invention also relates to the method of obtaining the proposed compounds and to new intermediate compounds, used in them, pharmaceutical compositions, containing the given therapeutically active compounds, and use of the given active compounds in therapy for treating conditions, related to GSK3.

EFFECT: new method of obtaining indole derivatives.

33 cl, 1 tbl, 112 ex

FIELD: medicine; pharmacology.

SUBSTANCE: admixture contains leaves of periwinkle, leaves of mint peppery, leaves of common plantain, hawthorn foetuses, rose hips, mountain ash foetuses, a grass of felon herb, sweet clover, a grass of cotton weed, camomile flowers, roots of liquorice at a proportion of components in parts accordingly 1:1:1:1:1:1:1:2:1:1:1.

EFFECT: admixture dilates an arsenal of medical products of a phytogenesis with the expressed therapeutic effect for treatment of disturbances of a cerebral circulation.

5 dwg, 3 dwg

FIELD: medicine; pharmacology.

SUBSTANCE: invention refers to medical products of antiischemic and hypolipidemic activity and can be used as new agent for correction of lipidic metabolic disorder to prevent and treat dyslipidemia, ischemic heart disease (IHD), and as rehabilitation agent at postinfarction conditions. Agent of antiischemic and hypolipidemic activity represents ecdysteroids-containing substance extracted from aerial saw-wort Serratula coronata L. (Asteraceae), containing mixed 20-hydroxyecdysone in amount not less than 75% and 25S-inocosterone in amount not less than 10%.

EFFECT: evident hypolipidemic activity and considerable reduction in common lipid, cholesterol and triglyceride content.

7 ex, 19 tbl, 24 dwg

FIELD: medicine, pharmaceutics.

SUBSTANCE: group of inventions concerns a composition of the prolonged release for peroral administering of a reductase inhibitor HMG-CoA. The composition which contains a solid dispersing agent including reductase inhibitor HMG-CoA, the dissolving agent and the stabilising agent is offered; the compound carrier of the prolonged release; and the accelerator of gel hydration where the compound carrier of the prolonged release is an admixture of sodium alginate and xanthic gum, and the accelerator of gel hydration is an admixture of a compound propylene glycol ether alginate and hypromellose. The method of obtaining of the specified composition, including stages is offered: the mixing of a reductase inhibitor HMG-CoA, a dissolving the agent and stabilising agent in a dissolvent with obtaining of a solid dispersing agent; homogeneous mixing of the compound carrier of the prolonged release and the accelerator of gel hydration with the solid dispersing agent with obtaining of the first admixture; additions of pharmaceutically comprehensible additives to the first admixture with obtaining of the second admixture; and dry mixing and drawing up of the second admixture in a solid composition. The composition due to the present invention can be easily and effectively received and be capable to maintain constant level of a medical product in blood by means of slow release of inhibitor HMG-CoA of a reductase with homogeneous rate within 24 hours. Accordingly the composition of the prolonged release under the present invention can be effectively used for decrease of cholesterol and triglycerides level in blood.

EFFECT: depression of cholesterol and triglycerides level in blood.

15 cl, 6 tbl, 6 ex, 6 dwg

FIELD: medicine.

SUBSTANCE: invention relates to application of L-butylftalid and containing it composition for preparation of medications for cerebral infarction prevention and treatment, particularly cerebral infarction, induced by focal cerebral ischemia. Application of L-butylftalid for preparation of medications for cerebral infarction prevention.

EFFECT: reduction of adverse reactions emergence risk and therapeutic action of medication for cerebral infarction prevention and treatment enhancement.

5 cl, 1 ex, 3 dwg

FIELD: medicine; pharmacology.

SUBSTANCE: method of treatment or prevention of hyperlipidemia conditions and/or hypercholesterinemia implies application of composition containing cyanidin-3-O-glucoside and peonidine-3-O-glucoside. Composition contains therapeutically effective amount of black rice extract, including cyanidin-3-O-glucoside, peonidine-3-O-glucoside and one or more phytosterols and/or phytostanines. Composition contains therapeutically effective amount of black rice extract, including cyanidin-3-O-glucoside, peonidine-3-O-glucoside and one or more antioxidants. Method of treatment or prevention of hyperlipidemia conditions and/or hypercholesterinemia implies application of composition containing extract of hulled black rice external layer, thus the specified extract contains cyanidin-3-O-glucoside and peonidine-3-O-glucoside.

EFFECT: efficiency for treatment or prevention hyperlipidemia conditions and hypercholesterinemia.

29 cl, 19 dwg, 11 tbl, 11 ex

FIELD: medicine.

SUBSTANCE: invention refers to application of vasopeptidase inhibitors for treatment and/or prevention of nephropathy in diabetics or nondiabetics as well as for treatment and/or prevention of insulin resistance or metabolic disorder associated with profound glycolysis end products.

EFFECT: offered compounds have higher therapeutic efficiency in prevention and treatment of diabetic nephropathy development and higher activity in treatment and prevention of insulin resistance.

4 cl, 7 ex, 15 tbl, 1 dwg

FIELD: chemistry.

SUBSTANCE: invention concerns a compound of the formula (I) , where A ring is selected out of phenyl or thienyl; X is selected out of -CR2R3-, -O- and -S(O)a-; where a is 0-2; Y is selected out of -CR4R5-, -O- and -S(O)a-; where a is 0-2; at least one -CR2R3- or -CR4R5- group is present; R1 is independently selected out of halogeno, C1-6alkyl and C1-6ealkoxy; b is equal to 0-3; R2 and R3, R4 and R5 are independently selected out of hydrogen, hydroxy, C1-6alkyl and C1-6alkoxy; or R2 and R3, R4 and R5 together form oxogroup; R6 is independently selected out of halogeno, C1-6alkyl and C1-6alkoxy; c is 0-5; R7 is independently selected out of halogeno, trifluoromethyl, trifluoromethoxy, methyl, ethyl, methoxy and ethoxy; d is 0-4; R9 is hydrogen or C1-4alkyl; R10 is hydrogen or C1-4alkyl; R11 and R12 are independently selected out of hydrogen, C1-4alkyl or carbocyclyl; where R11 and R12 can possibly be independently substituted for carbon atom with one or more substitute selected out of R25; R13 is hydrogen, C1-4alkyl or carbocyclyl; where R13 can possibly be substituted for carbon atom with one or more substitute selected out of R27; R14 is hydrogen, hydroxy, amino, carbamoyl, mercapto, sulfamoyl, etc; or R14 is a group of the formula (IA) , where Z is -N(R35)-; where R35 is hydrogen or C1-4alkyl; R15 is hydrogen or C1-4alkyl; R16 and R17 are independently selected out of hydrogen, hydroxy, amino, carboxy, carbamoyl, mercapto, sulfamoyl, C1-6alkyl, C1-6alkoxy, N-(C1-6alkyl)-amino etc; R18 is selected out of hydroxy, amino, carbamoyl, mercapto, sulfamoyl, C1-10alkyl, C1-10alkoxy, N-(C1-10alkyl)amino, N,N-(C1-10alkyl)2amino, etc; p is 1-3; q is 0-1; r is 0-3; m is 0-2; n is 1-2; where R1, R6, R7, R16, R17, R13, R9 can be equal or different; R25, R27 and R33 are independently selected out of hydroxy, amino, carbamoyl, mercapto, sulfamoyl, C1-10alkyl, C1-10alkoxy, C1-10alkoxycarbonyl, N-(C1-10alkyl)amino, etc; where carbocyclyl is a saturated, partially saturated or non-saturated monocyclic carbon ring including 3-6 atoms; or its pharmaceutically acceptable salt, solvate, or salt solvate. Compounds of the formula (I) or its pharmaceutically acceptable salts, solvates, or salt solvates are obtained by interaction of acid of the formula (IV) or its activated derivative with amine of the formula (V) . Compounds of the formula (I), where R14 is a group of the formula (IA), are obtained by interaction of compound of the formula (VI) , where R14 is carboxy, or its activated derivative, with amine of the formula (VI). Compounds of the formula (I), where X or Y is -S(O)a-, and a is 1 or 2, is obtained by oxidation of compound of the formula (I), where X or Y is -S(O)a-, and a is 0 (for compounds of the formula (I), where a is 1 or 2), or a is 1 (for compounds of the formula (I), where a is 2). The invention concerns pharmaceutical composition with inhibition effect on cholesterol absorption containing effective quantity of compound of the formula (I) combined with pharmaceutically acceptable dilutant or carrier, and combination of compound of the formula (I) and hydroxymethylglutaryl-coenzyme A (HMG Co-A) reductase inhibitor. Compounds of the formula (I) are applied to produce inhibition effect on cholesterol absorption or in hyperlipidemic state treatment of haematothermal animals.

EFFECT: obtaining diphenylazetidinone derivatives with inhibition effect on cholesterol absorption.

38 cl, 54 ex

FIELD: chemistry.

SUBSTANCE: in novel tocopherol-modified therapeutic drug compounds of formula 1 T-L-D, T is tocopherol, L is succinate, and D is camptotecin or its derivative, where all three fragments are bound covalently. Invention also relates to emulsions based on said compounds, formulations of micelles, including said compounds, methods of treating cell proliferative disease using said compounds and formulations, as well as to said compounds application for production of medication for treatment of cell proliferative disease.

EFFECT: increase of composition and treatment method efficiency.

18 cl, 17 dwg, 4 tbl, 19 ex

Up!