Hepatitis c virus inhibitors

FIELD: medicine, biochemistry.

SUBSTANCE: invention describes compounds that inhibit function of NS3-protease encoded by hepatitis C virus.

EFFECT: valuable medicinal properties of inhibitors.

6 cl, 2 tbl, 472 ex

 

The text descriptions are given in facsimile form.

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Same patents:

The invention relates to compounds of formula (1), where X and Y Is N or O; R1substituted alkyl, substituted arylalkyl or cycloalkyl; R2and R3Is h or alkyl; And a Is-C(O)-, -OC(O)-, -S(O)2-; R4- alkyl, cycloalkyl or (C5-C12)aryl; compounds of the formula (2), where X and Y are O, S or N; R1- alkyl, optionally substituted arylalkyl; R2and R3Is h or alkyl;- C(O)-; R6- Deputy, including the condensed heterocyclic rings; and compounds of the formula (3), where X and Y are O, S or N; R1- alkyl, alkylsilane, (C5-C12)arylalkyl, (C5-C12)aryl; R2and R3Is h or alkyl; R2' and R3' - N; R11, R12and E together form a mono - or bicyclic ring which may contain heteroatoms

The invention relates to new derivatives of Proline, and more specifically to individual forms new derivative of 1-substituted N-[2-methyl-1-(TRIFLUOROACETYL)- propyl]pyrrolidin-2-carboxamide, which are inhibitors of elastase of human leukocytes (ALC), also known as elastase human neutrophils (ANC), which are important, for example, as a means of research work in pharmacological, diagnostic and related studies and in the treatment of diseases of mammals, which also involved ALC

The invention relates to medicine, namely to methods of producing biologically active substances that have immunoregulatory properties, and may find application in medicine, veterinary medicine and experimental biochemistry

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

SUBSTANCE: invention relates to novel isoquinoline compounds of the general formula (I): wherein R1 represents hydrogen atom, halogen atom or alkyl; Y is absent or represents alkylene chain comprising from 1 to 8 carbon atoms wherein arbitrary carbon atom can comprise hydroxyl group as a substitute; R represents the following formula (II): wherein X represents -CH or nitrogen atom under condition that if Y absent in the formula (I) then X must represent -CH; W represents -CH or nitrogen atom under condition that if X represents -CH then W must represents nitrogen atom; s represents a whole number from 1 to 3; t represents a whole number from 1 to 3; if R3 represents hydrogen atom or alkyl then R2 represents hydrogen atom, alkyl, hydroxyl group or hydroxyalkyl, and R2' represents hydroxyl group or hydroxyalkyl, and if R3 represents hydroxyalkyl then R2 and R2' represent hydrogen atom. Also, invention relates to their optically active forms, pharmaceutically acceptable salts, aqueous adducts, hydrates and solvates. Compounds of the formula (I) elicit inhibitory effect on activity of poly-(ADP-ribose)-polymerase and can be used in prophylaxis of diseases associated with cerebral infarction.

EFFECT: valuable medicinal properties of compounds, improved method of synthesis.

40 cl, 4 tbl, 55 ex

FIELD: organic chemistry of natural compounds, medicine, pharmacy.

SUBSTANCE: invention relates to novel compounds of the formula (I): , wherein each R1, R2 and R3 means independently hydrogen atom or (C1-C4)-alkyl; R4 means (C1-C12)-alkyl optionally comprising from one to three substitutes chosen from group including hydroxy-group, (C1-C12)-alkoxycarbonyl, carbamoyl, (C2-C7)-alkenyl, (C6-C10)-aryl optionally comprising from one to three substitutes chosen from group including halogen atom, (C1-C12)-alkyl, (C1-C12)-alkoxy-, hydroxy-, (C1-C12)-alkylcarbonylamino-group, (C6-C10)-aryl-(C1-C12)-alkyl wherein aryl group comprises optionally from one to three substitutes chosen from group comprising halogen atom, (C1-C12)-alkyl, (C1-C12)-alkoxy-group, heterocyclyl-(C1-C12)-alkyl; R5 means hydroxy-, (C3-C7)-cycloalkylamino-group optionally substituted with phenyl, (C6-C10)-arylamino-, (C6-C10)-aryl-(C1-C4)-alkylamino-group optionally comprising from one to three substitutes chosen from group comprising sulfamoyl, (C1-C12)-alkyl, (C1-C12)-alkoxy-, hydroxy-group, heterocyclyl or benzyl, (C1-C4)-alkoxy-, benzhydrazino-group, heterocyclyl optionally comprising from one to three substitutes chosen from group including benzyl, benzhydryl, heterocyclylamino-group wherein heterocyclyl means saturated, unsaturated or aromatic monovalent cyclic radical comprising from 1 to 3 heteroatoms chosen from nitrogen (N), oxygen (O) and sulfur (S) atoms, or to their combination; n means a whole number 0, 1 or 2. Compounds of the formula (I) elicit anti-proliferative activity that allows their using in pharmaceutical composition. Also, invention describes intermediate compounds.

EFFECT: valuable medicinal properties of compounds and pharmaceutical composition.

30 cl, 1 tbl, 69 ex

FIELD: organic chemistry, medicine.

SUBSTANCE: invention relates to novel substituted derivatives of cyclohexane of the formula (I): wherein U means a free electron pair; V means a simple bond, -CH2-, -CH=CH-, -CH=CH-CH2-O-, -C≡C-; W means -COO, -CSO or -SO2; m and n mean independently of one another numbers from 0 to 4; m + n = 0-7; A1 means hydrogen atom (H), lower alkyl, hydroxy-(lower)-alkyl or lower alkenyl; A2 means pyrrolyl, pyrimidinyl, optionally substituted (lower)-alkyl or lower alkyl optionally substituted with R2; or A1 and A2 are bound to form ring; -A1-A2- means lower alkylene optionally substituted with R2 wherein one group -CH2- in -A1-A2- can be optionally replaced for -NR3 or oxygen atom (O); A3, A4, A5, A6, A7 and A8 mean H; R9 means H, lower alkyl; R10 means (lower)-alkyl, phenyl wherein phenyl can be substituted with 1-3 substitutes chosen independently from the group comprising halogen atom, -CF3, (lower)-alkyl; p means 0, 1; R2 means H; R3 means H, lower alkyl, and their pharmaceutically acceptable salts. Compounds of the formula (I) possess the inhibitory effect on activity of enzyme oxidosqualene lanosterol cyclase and can be used in pharmaceutical composition. Also, method relates to a method for treatment and/or prophylaxis of hyperlipemia, artheriosclerosis, hypercholesterolemia and others.

EFFECT: valuable medicinal properties of compounds and pharmaceutical composition.

27 cl, 9 sch, 10 tbl, 43 ex

FIELD: organic chemistry, chemical technology.

SUBSTANCE: invention relates to a method for synthesis of 2-(1-methyl-2-(3,4-fullero[60]pyrrolidinyl)phenol of the formula (1): Method involves interaction of fullerene[60] with 2-[(dimethylamino)methyl]phenol of the general formula: (R-CH2-N(CH3)2) wherein R means in taken in the mole ratio C60 : R-CH2-N-(CH3)2 = 0.01:(0.01-0.011) in the presence of Cp2TiCl2 as catalyst taken in the amount 15-25 mole% relatively to fullerene[60] in argon atmosphere, in toluene medium as a solvent, at temperature 140-160°C for 2-4 h. Method provides preparing the novel compound with the yield 78-86%. Compound of the formula (1) can be used as a chelating agent, sorbent and biologically active substance.

EFFECT: improved method of synthesis.

1 tbl, 1 ex

The invention relates to agriculture and veterinary medicine

The invention relates to an improved process for the preparation of CIS-1-{2-[4-(6-methoxy-2-phenyl-1,2,3,4-tetrahydronaphthalen-1-yl] ethyl} pyrrolidine, which is a substance to obtain the (-)CIS-6-phenyl-5-[4-(2-pyrrolidin-1-yl-ethoxy)phenyl-5,6,7,8-tetrahydronaphthalen-2-ol, which is used in the treatment of osteoporosis, as well as to intermediate compounds for this method

The invention relates to new niftystories compounds of formula I, where R1and R2- H, -OH, -O(C1-C4alkyl), -OCOC6H5, -OCO(C1-C6alkyl), -OSO2(C4-C6alkyl); R3- 1-piperidinyl, 1-pyrrolidinyl, methyl-1-pyrrolidinyl, dimethyl-1-pyrrolidinyl, 4-morpholino, dimethylamino, diethylamino, 1 hexamethyleneimino; intermediate compounds, which are suitable for easing symptoms of postmenopausal syndrome, including osteoporosis, hyperlipemia and estrogenzawisimy cancer, and inhibition of uterine fibroids, endometriosis and proliferation of aortic smooth muscle cells

The invention relates to therapeutic tools, specifically setidentityproviderid N-substituted nitrogenous heterocyclic compounds and methods of producing such compounds, intermediate products used in obtaining, compositions containing such compounds and the use of such heterocycles

FIELD: veterinary science.

SUBSTANCE: invention proposes using disinfecting preparation "Lesiptik" as a preparation for prophylaxis or respiratory diseases in calves. Invention provides enhancing safety of claves to 100% and increasing daily average gains by 24.5%.

EFFECT: valuable properties of preparation.

1 tbl, 3 ex

FIELD: medicine, virology, pharmacy.

SUBSTANCE: invention relates to using derivatives of dithiocarbamate of the formula: R1R2NCS2H and oxidized forms of these compounds, in particular, their dimmers and their pharmaceutically compatible salts for preparing an agent used in treatment or prophylaxis of infection caused by RNA-containing viruses that damage respiratory tract and inducing disease. Also, invention relates to a disinfecting agent containing dithiocarbamate compound and a method for disinfection of surfaces, media and cell cultures.

EFFECT: valuable medicinal properties of compounds.

19 cl, 14 dwg, 14 ex

FIELD: medicine.

SUBSTANCE: method involves making patient contact with effective quantity of one or several compounds. Pharmaceutical composition comprises one or several compounds applicable in absence of exogenous antigen for treating or alleviating the cases of infectious, autoimmune diseases and allergy.

EFFECT: enhanced effectiveness of treatment or prophylaxis.

52 cl

FIELD: virology, biotechnology, medicine, pharmacy.

SUBSTANCE: invention proposes the envelope HCV protein (hepatitis C virus). Protein comprises 80% of glycosylated sites. Such protein is more preferable for diagnostic, prophylactic and therapeutic using. Also, invention proposes a method for preparing such protein, and a drug, vaccine and different pharmaceutical compositions also comprising such protein. Proposed group of inventions can be used in medicine for diagnosis, treatment and prophylaxis of HCV infection and to prediction of clinical effectiveness of treatment.

EFFECT: improved preparing method, valuable medicinal properties of protein.

37 cl, 77 dwg, 16 tbl, 29 ex

FIELD: genetic engineering, virology, pharmacy.

SUBSTANCE: invention proposes the recombinant modified virus OF VACCINE Ankara able to express structural antigens of hepatitis C virus. Virus comprises DNA sequences encoding structural antigens of hepatitis C virus or their functional regions or epitopes of hepatitis C virus structural antigens. Also, invention proposes a pharmaceutical composition comprising such virus, eucaryotic cell infected with such virus, a method for preparing such virus and a method for preparing hepatitis C virus structural polypeptides. Invention can be used in virology and medicine for preparing hepatitis C virus antigen.

EFFECT: valuable properties of virus.

20 cl, 14 dwg, 1 tbl

FIELD: medicine, obstetrics, gynecology.

SUBSTANCE: uterine cavity should be drained in the course of operation, moreover, irrigator's distal end should be withdrawn through operation wound at anterior abdominal wall, and 2 h after the end of operation uterine cavity should be washed through irrigator with 400 ml of cooled 0.06%-sodium hypochlorite solution at perfusion rate being 200 ml/h, 6 times every 12 h up to 3-4 d; after each perfusion one should introduce 1 g kanamycin directly into uterine cavity, moreover, in case of availability of bacterioid and/or anaerobic flora in uterine cavity according to the results obtained due to pre-operational antibioticogram one should add 100 ml 3%-hydrogen peroxide solution into perfusion solution. The present innovation enables to efficiently sanitize uterine cavity due to intrauterine injection of antibiotics by taking into account antibioticogram performed at all stages of operative treatment.

EFFECT: higher efficiency of prophylaxis.

1 cl, 2 ex

FIELD: medicine.

SUBSTANCE: method involves administering 1-methyl-2-phenylthiomethyl-3-carbetoxi-4-dimethyl-aminomethyl-5-oxibromoindol or its salts selected from a group containing hydrochloride monohydrate (arbidol) earlier known as immunomodulator, besilate, fumarate, maleate, citrate or their hydrates.

EFFECT: enhanced effectiveness in healing organism from rotavirus.

4 cl, 8 tbl

FIELD: organic chemistry, biochemistry, medicine, virology.

SUBSTANCE: invention relates to derivatives of 2'=amino-2'-deoxynucleosides of the formula:

wherein R means hydrogen atom (H), alkyl, aminoalkyl; R1 means -(R2NR3) wherein R2 and/or R3 means H, -OH, -NH2, alkyl, benzyl under condition that R doesn't represent H or methyl when R2 and R3 mean H. Compounds elicit an antiviral activity with respect to measles and Marburg viruses exceeding that of ribavirin.

EFFECT: valuable properties of compounds.

4 tbl, 2 dwg, 18 ex

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