N-9-substituted purine compounds, compositions and methods of use

FIELD: chemistry.

SUBSTANCE: present invention relates to novel compounds of formula I-A, having properties of inhibitors of kinase of phosphoinositide-3-kinase family mTOR and PI3K, for use in treating cancer, as well as for preparing drugs for treating cancer. In compounds of formula I-A R1 is selected from a group comprising cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, azetidin-1-yl, azetidin-2-yl, azetidin-3-yl, pyrrolidin-1-yl, pyrrolidin-2-yl, pyrrolidin-3-yl, piperidin-1-yl, piperidin-2-yl, piperidin-3-yl, piperidin-4-yl, oxetan-2-yl, oxetan-3-yl, tetrahydrofuran-2-yl, tetrahydrofuran-3-yl, tetrahydropyran-2-yl, tetrahydropyran-3-yl and tetrahydropyran-4-yl, oxepan-2-yl, oxepan-3-yl, oxepan-4-yl, phenyl pyrrol-2-yl, pyrrol-3-yl, pyrazol-3-yl, pyrazol-4-yl, pyrazol-5-yl, furan-2-yl, furan-3-yl, thien-2-yl, thien-3-yl, thiazol-2-yl, thiazol-3-yl, thiazol-4-yl, imidazol-1-yl, imidazol-4-yl, pyrid-2-yl, pyrid-3-yl, pyrid-4-yl, pyrimidin-1-yl, pyrimidin-2-yl, pyrimidin-3-yl, pyrazin-2-yl, pyridazin-2-yl, pyridazin-3-yl and triazin-2-yl, where R1 substituted by 0-3 substitutes RR1, selected from a group consisting of halogen, F, Cl, Br, I, -ORa, -C(O)Ra, -Rc; where Ra is selected from hydrogen or C1-6alkyl, Rc is C1-6alkyl; R2 is selected from a group comprising hydrogen, C1-6alkyl, C2-6alkenyl, C2-6alkynyl; R3 is a morpholine-4-yl, where group R3 is substituted with 0–3 substitutes RR3, selected from a group consisting of -Ri, halogen, where Ri is selected from C1-6alkyl, C1-6haloalkyl; D is -NR4C(O)NR5R6 or -NR5R6, where R4 and R5 each denotes hydrogen and R6 is C1-6alkyl, C1-6haloalkyl oxetan-3-yl and pyridyl-on.

EFFECT: treatment of cancer.

11 cl, 1 tbl, 26 ex

 



 

Same patents:

FIELD: chemistry.

SUBSTANCE: invention relates to novel compounds of formula I, having cell proliferation inhibitor properties. In formula I , Y1 and Y2 each independently denote N or C(R1), but Y1 and Y2 do not simultaneously denote N or do not simultaneously denote C(R1), where R1 is selected from a group consisting of a hydrogen atom, C1-6alkyl, where R1 is substituted with 0 or 1 substitutes RR1, selected from a group consisting of -ORa; where Ra is selected from a hydrogen atom; R2 is selected from a group consisting of a hydrogen atom, C1-6alkyl; R3 is a 6-7-member monocyclic or bridge heterocycloalkyl ring containing 2 heteroatoms, selected from N and O, where the group R3 is substituted with 0-3 substitutes RR3, selected from a group consisting of -Ri, Ri is selected from C1-6alkyl; A1, A2, A3 and A4 each denote C(H); and D denotes -NR4C(O)NR5R6, where R4 is selected from a group consisting of a hydrogen atom; R5 and R6 are each independently selected from a group consisting of a hydrogen atom, C1-6alkyl, C4-6heterocycloalkyl containing one oxygen heteroatom; and where R5 and R6 are further substituted with RD, where RD is selected from -S(O)2Rm, where Rm is selected from C1-6alkyl.

EFFECT: compounds can be used to produce medicine for treating cancer.

21 cl, 1 tbl, 21 ex

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention refers to new compounds of structural formula I that possess inhibitory activity on phosphatidyl inositol-3-kinase (PI3-kinase). In formula I: B represents group of formula II:, wherein Wc represents 6-10-merous aryl, q is equal to 0, 1, 2, 3 or 4; X is absent or represents -(CH(R9))z-, z is equal to 1; Y represents -N(R9)-; Wd represents R1 and R2 represents C1-6alkyl or halogeno; R3 represents hydrogen or C1-6alkyl; and in each case R9 independently represents hydrogen or C1-6alkyl.

EFFECT: invention refers to a pharmaceutical composition containing the above compounds, and to a method for P3I-kinase inhibition in a subject, wherein the subject suffers a disease representing cancer, a bone disorder, an inflammatory disease, an immune disease, a nervous system disease, a metabolic disease, a respiratory disease, thrombosis or a cardiovascular disease.

24 cl, 11 dwg, 6 tbl, 43 ex

FIELD: chemistry.

SUBSTANCE: present invention relates to organic chemistry and specifically to novel morpholinopurine derivatives of general formula

,

or a pharmaceutically acceptable salt thereof, where R1 and R2, each independent of each other, denote a C1-C6 alkyl group or a hydrogen atom, R3a and R3b, each independent of each other, denote a C1-C6 alkyl group which can contain three substitutes selected from a group A, or a hydrogen atom, R4 denotes a C1-C6 alkyl group or a hydrogen atom, Ra denotes a group of formula -Y-R , where Y denotes a single bond or a C1-C6 alkylene group, R5 is a C1-C6 alkyl group which can contain one, two or three substitutes selected from group A, a tetrahydrofuranyl group, a pyrrolidinyl group which contains one substitute selected from a group D, and Rb and Rc, each independent of each other, denote a C1-C6 alkyl group which contains one substitute selected from a group E, or a hydrogen atom, or Rb and Rc, together with a nitrogen atom to which they are bonded, for a 5-7-member alicyclic nitrogen-containing heterocyclic group, which is pierazine, morpholine, pyrrolidine, piperidine, homopiperazine, which can contain one, two or three substitutes selected from group E; group A: halogen atom, hydroxy group, C3-C8 cycloalkyl group and oxy group; group D: C1-C6 alkylsulphonyl group; and group E: hydroxy group, formyl group, C1-C6 alkyl group, which can contain one substitute selected from said group A, diC1-C6 alkylamino group, C1-C6 alkylsulphonylamino group, C1-C6alkylsulphonyl C1-C6 alkylamino group, C1-C6 alkylsulphonylamino C1-C6alkyl group, C1-C6alkylcarbonyl group, which can contain one substitute selected from said group A, C1-C6 alkylsulphonyl group, C1-C6 alkylamino C1-C6 alkylcarbonyl group, diC1-C6 alkylamino C1-C6alkylcarbonyl group, which can contain one substitute selected from said group A, diC1-C6 alkylaminocarbonyl group, phenylsulphonyl group and hateroaryl C1-C6 alkylcarbonyl group, where the heteroaryl is imidazolyl. The invention also relates to a pharmaceutical composition, an inhibitor of phosphatidylinositol-3-kinase (PI3K), an inhibitor of mammalian target of rapamycin (mTOR) based on the compound of formula (1a), a method of treating cancer and use of the compound of formula (1a).

EFFECT: obtaining novel morpholinopurine derivatives, having useful biological properties.

42 cl, 19 tbl, 138 ex

FIELD: biotechnologies.

SUBSTANCE: invention relates to new compounds of general formula (1), possibly in the form of trans-isomers, or pharmaceutically acceptable salts, having an activating function of angiogenesis, clear space formation and growth of neurons. The compound may find application as an active agent for a medicinal agent for healing of wounds, a therapeutic and prophylactic agent for treatment of Alzheimer's disease, diseases with heart attack and for hair growth. In the general formula X1 is halogen, C1-C4alkylthiogroup or aminogroup; X2 represents halogen, aminogroup, C1-C4alkoxygroup or oxogroup; X3 represents a hydrogen atom, halogen or C1-C4alkoxygroup; R1 and R2 are identical or different, and each independently represents a hydrogen atom, a hydroxymethyl group or C1-C4acyloxyalkyl group; when X1 is aminogroup, X2 and X3, both are atoms of halogen, X2 and X3, are both alkoxygroups, or X2 represents an oxogroup, X3 is halogen or hydrogen, and R1 and R2, both are C1-C4acyloalkyl groups.

EFFECT: improved properties of compounds.

9 cl, 18 dwg, 5 tbl, 26 ex

FIELD: chemistry.

SUBSTANCE: invention relates to novel forms A and B of crystalline adefovir dipivoxil, which have improved properties during use thereof, particularly high rate of dissolution and high stability.

EFFECT: invention also relates to methods of producing forms A and B of crystalline adefovir dipivoxil.

7 cl, 10 dwg, 4 tbl, 11 ex

FIELD: chemistry.

SUBSTANCE: compound, selected from compound given in Table 1 or in Table A correspond to general formulae: or . In Table 1 compounds are selected from compounds, where Y corresponds to NH or O; R2 is selected from H, 2-fluorophenyl, furan-2-yl; group R4-R3- is selected from group =-CH2-, tetrahydrofuran-3-yl, cyclopentyl, group -(CH2)qZ is selected from phenyl, substituted with CH3, CF3, Cl. In compounds, selected from Table A, R is selected from probably substituted phenyl, CH2CH2OBn, where Bn stands for benzyl; X represents O; R9 is selected from propargyl and cyclopentyl.

EFFECT: compounds are selective antagonists of adenosine A2a receptors and are suitable for manufacturing medication, useful in treatment of diseases, which require antagonistic action with respect to activity of said receptors.

6 cl, 2 tbl, 18 ex

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention refers to new purine derivatives of formula (I) and to their pharmaceutically acceptable salts exhibiting the properties of adenosine receptor A2A agonists. The compounds can find application for preparing a drug for treating an inflammatory or obstructive respiratory disease. In formula

,

R1, R2 and R3 are those as specified in the patent claim.

EFFECT: preparing new purine derivatives of formula (I) or their pharmaceutically acceptable salts showing the properties of adenosine receptor A2A agonists.

8 cl, 2 tbl, 264 ex

FIELD: medicine, pharmaceutics.

SUBSTANCE: present invention refers to new compounds of formula I or their pharmaceutically acceptable salts showing an ability to inhibit sphingosine kinase, to a based pharmaceutical composition, to a method of inhibiting sphingosine kinase and a method of treating diseases specified in breast cancer, diabetic retinopathy, arthritis and colitis. , wherein X represents -C(R3,R4)N(R5)-, -C(O)N(R4)-; R1 represents phenyl unsubstituted or substituted by 1 or 2 halogens. The values of R2, R3, R4, R5 substitutes are such as specified in the patent claim.

EFFECT: preparation of new compounds.

17 cl, 24 dwg, 9 tbl, 26 ex

FIELD: chemistry.

SUBSTANCE: nucleic base (e.g. uracil, cytosine, adenine, guanine, hypoxanthine, xanthine or similar) reacts with perfluoroalkyl halide in the presence of sulphoxide, peroxide and an iron compound to obtain a perfluoroalkyl-substituted nucleic base.

EFFECT: high cost effectiveness as an intermediate compound for producing medicinal agents.

15 cl, 6 tbl

Chemical compounds // 2405780

FIELD: medicine, pharmaceutics.

SUBSTANCE: present invention refers to new compounds of formula (I): , in which: R1 and R2 are independently specified from hydrogen, C1-6alkyl, C1-6alkoxy and cyclopropyl; X1, X2 and X3 independently represent =N- or =CR10; R3 and R10 are independently specified from hydrogen, halogen, nitro, cyano, amino, carboxy, carbamoyl, C1-6alkyl, N-(C1-6alkyl)amino, N,N(C1-6alkyl)2amino, C1-6alkanoylamino, C1-6alkoxycarbonyl; R4 represents hydrogen; R5 and R6 are independently specified from hydrogen, hydroxy and C1-6alkyl where R5 and R6 independently can be optionally substituted in carbon atom with one or more R16 where R16 represents hydroxy; A represents a single link or C1-2alkylene; where specified C1-2alkylene can be optionally substituted with one or more R18; the ring C represents a saturated, partially saturated or unsaturated mono- or bicyclic ring containing 5 or 6 atoms in which at least one atom can be specified from nitrogen, sulphur or oxygen which can be linked with carbon or nitrogen atom where the -CH2- group can be optionally substituted with -C(O)- and ring sulphur atom can be optionally oxidised to produce S-oxide; R7 is specified from halogen and C1-6alkyl where R7 can be optionally substituted in carbon atom with halogen; n is equal to 0.1 or 2; where R7 values can be equal or different; and R18 is independently specified from halogen and hydroxy; or its pharmaceutically acceptable salt. Also the invention refers to their pharmaceutical compositions and methods for preparation and application thereof for cancer treatment.

EFFECT: preparation of new compounds which can find application for cancer treatment.

23 cl, 96 ex

FIELD: medicine, pharmaceutics.

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

EFFECT: obtaining novel heteroaryl derivatives.

27 cl, 41 ex

FIELD: chemistry.

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

EFFECT: improvement of characteristics.

15 cl, 3 tbl, 51 ex 1 dwg

FIELD: chemistry.

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

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

27 cl, 6 dwg, 2 tbl, 126 ex

FIELD: medicine.

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

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

1 ex

FIELD: medicine, pharmaceutics.

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

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

8 cl, 3 dwg, 1 ex, 3 tbl

FIELD: medicine.

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

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

24 cl, 8 dwg, 2 tbl, 169 ex

FIELD: chemistry.

SUBSTANCE: disclosed agent is a xanthine derivative of formula 1

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

EFFECT: improved properties of the derivatives.

8 cl, 4 tbl, 12 dwg

FIELD: medicine, pharmaceutics.

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

EFFECT: obtaining novel compounds, which inhibit HIV replication.

5 cl, 25 dwg, 7 tbl, 16 ex

Novel compounds // 2395511

FIELD: chemistry.

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

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

15 cl, 54 ex

FIELD: medicine, pharmacology, organic chemistry, pharmacy.

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

EFFECT: valuable medicinal properties of pharmaceutical composition.

14 cl, 11 tbl, 55 ex

FIELD: 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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