Pyrido-, pyrazo- and pyrimido-pyrimidine derivatives and use thereof as mtor inhibitors

FIELD: chemistry.

SUBSTANCE: invention relates to compounds of formula I in which: X8 denotes N, and X5 and X6 denote CH; R7 denotes phenyl or C5-6-heteroaryl group which is optionally substituted with one or more groups selected from halogen, hydroxy group, nitro group, cyano group, carboxy group and thiol, or phenyl or a methoxy group -C(=O)CH3, -C(=O)OCH3, -C(=O)OCH2CH3, -C(=O)OC(CH3)3, -C(=O)NH2, -C(=O)NHCH3, -C(=O)N(CH3)2, -C(=O)NHCH2CH3, -C(=O)N(CH2CH3)2, -NH2, -NHCH3, -N(CH3)2, -NHCH(CH3)2, -N(CH2CH3)2 or C1-4-alkyl, optionally substituted with a hydroxy group; RN3 and RN4, together with the nitrogen atom with which they are bonded, form a heterocyclic ring selected from morpholine, thiomorpholine, piperidinyl, piperazinyl, homopiperazinyl and a pyrrolidinyl ring, optionally substituted at the carbon atom with one or two C1-4-alkyl groups; R2 denotes NRN5RN6, where RN5 and RN6, together with the nitrogen atom with which they are bonded, form a heterocyclic ring selected from morpholine, thiomorpholine, piperdinyl, piperazinyl, homopiperazinyl and a pyrrolidinyl ring, optionally substituted at the carbon atom with one or two C1-4-alkyl groups; or a pharmaceutically acceptable salt thereof, and where "C5-6-heteroaryl" denotes a heteroaryl group selected from furan, thiophene, pyrrole, imidazole, pyrazole, triazole, oxazole, isoxazole, thiazole, isothiazole, oxadiazole, tetrazole, octatriazole, isoxazine, pyridine, pyridazine, pyrimidine, pyrazine and triazine; and where "C3-5-heterocyclyl", as used here, relates to a univalent structure obtained by removing a hydrogen atom from the ring of the heterocyclic compound, where that structure contains 5 or 6 ring atoms, 1-4 of which are ring heteroatoms selected from oxygen, nitrogen and sulphur; and under the condition that when R2 denotes an unsubstituted morpholine group, RN3 and RN4, together with the nitrogen atom with which they are bonded, form a morpholine group, R7 does not denote an unsubstituted phenyl, and when R2 denotes an unsubstituted piperidinyl, RN3 and RN4, together with the nitrogen atom with which they are bonded, form an unsubstituted piperidinyl, R7 does not denote unsubstituted phenyl. The invention also relates to a pharmaceutical composition based on compounds of formula I and having mTOR inhibiting activity.

EFFECT: novel compound which can be suitable for treating malignant growths is obtained and described.

10 cl, 13 ex

 

The text descriptions are given in facsimile form.

1. The compound of the formula I

in which X8represents N and X5and X6represent CH;
R7represents phenyl or5-6-heteroaryl group, neobyazatel is substituted by one or more groups, selected from halogen, hydroxy-group, nitro group, ceanography, carboxypropyl and thiol, or phenyl, or metoxygroup, -C(=O)CH3-C(=O)och3-C(=O)och2CH3-C(O)OC(CH3)3, -C(=O)NH2, -C(=O)NHCH3-C(=O)N(CH3)2, -C(=O)NHCH2CH3, -C(=O)N(CH2CH3)2,
-NH2, -NHCH3, -N(CH3)2, -NHCH(CH3)2, -N(CH2CH3)2or1-4-alkyl, optionally substituted hydroxy-group;
RN3and RN4together with the nitrogen atom to which they are attached, form a heterocyclic ring selected from morpholino, thiomorpholine, piperidinyl, piperazinilnom, homopiperazine and pyrrolidinyl ring, optionally substituted on the carbon atom by one or two1-4-alkyl groups;
R2represents NRN5RN6where RN5and RN6together with the nitrogen atom to which they are attached, form a heterocyclic ring selected from morpholino, thiomorpholine, piperidinyl, piperazinilnom, homopiperazine and pyrrolidinyl ring, optionally substituted on the carbon atom by one or two C1-4-alkyl groups;
or its pharmaceutically acceptable salt,
and where C5-6-heteroaryl means a heteroaryl group selected the th of furan, thiophene, pyrrole, imidazole, pyrazole, triazole, oxazole, isoxazol, thiazole, isothiazole, oxadiazole, tetrazole, oxadiazole, isoxazine, pyridine, pyridazine, pyrimidine, pyrazine and triazine;
and where C3-5-heterocyclyl, as used here, refers to a monovalent structure obtained by removing a hydrogen atom from a ring atom heterocyclic compounds, where the structure contains 5 or 6 ring atoms, of which from 1 to 4 are ring heteroatoms selected from oxygen, nitrogen and sulfur; and
provided that when R2represents unsubstituted morpholino group, RN3and RN4together with the nitrogen atom to which they are attached, form an unsubstituted morpholino group, R7does not represent unsubstituted phenyl, and,
when R2represents an unsubstituted piperidinyl, RN3and RN4together with the nitrogen atom to which they are attached, form an unsubstituted piperidinyl, R7does not represent unsubstituted phenyl.

2. The compound according to claim 1, in which R7represents a phenyl group, optionally substituted by one or more groups selected from halogen, hydroxy-group, nitro group, ceanography, carboxypropyl and thiol, or phenyl, or metoxygroup, -C(=O)CH3-C(=O)och3-C(=O)och CH3-C(=O)OC(CH3)3, -C(=O)OPh, -C(=O)NH2-C(O)NHCH3-C(=O)N(CH3)2, -C(=O)NHCH2CH3,
-C(=O)N(CH2CH3)2, -NH2, -NHCH3, -N(CH3)2, -NHCH(CH3)2, -N(CH2CH3)2or1-4-alkyl, optionally substituted hydroxy-group.

3. The compound according to claim 1, in which R7represents a phenyl group, optionally substituted by one or more groups selected from chlorine, hydroxy-group, methyl, metoxygroup and hydroxymethyl.

4. The compound according to claim 1, in which R7is a 4-chloraniline, 4-methylphenyl, 4-metoksifenilny, 3-hydroxymethyl-4-metoksifenilny, 3,5-dimethoxy-4-hydroxyphenyl, 4-hydroxyphenyl, 3-hydroxyphenyl or 3-hydroxymethylamino group.

5. The compound according to claim 1, in which RN3and RN4together with the nitrogen atom to which they are attached, form morpholino group.

6. The compound according to claim 1, in which R2represents a
oror

7. The compound according to claim 1, selected from any of the following connections:

or Pharma is efticiency acceptable salt.

8. Pharmaceutical composition having inhibitory activity against mTOR-containing compound according to claim 1 or 7, and pharmaceutically acceptable carriers or diluents.

9. The compound according to claim 1 or 7, having inhibitory activity against mTOR.

10. The compound according to claim 1 or 7 or its pharmaceutically acceptable salt for use as drugs having inhibitory activity against mTOR.



 

Same patents:

FIELD: medicine, pharmaceutics.

SUBSTANCE: present invention refers to compounds of general formula (I) or its pharmaceutically acceptable salts which have action of mTOR inhibitors. What is also declared is preparing a pharmaceutical composition containing a therapeutically effective amount of the compound of formula (I) and a pharmaceutically acceptable carrier or diluent; besides, what is declared is the use of the compound of formula (I) or its pharmaceutically acceptable salts for preparing the drug for ensuring anticancer action.

EFFECT: preparing the pharmaceutically acceptable salts for preparing the drug for ensuring anticancer action.

11 cl, 25 ex

FIELD: medicine, pharmaceutics.

SUBSTANCE: present invention refers to medicine, particularly to application of an antiviral agent - 2-methylthio-6-nitro-1,2,4-triazolo[5,1-c]-1,2,4-triazin-7-one dehydrate sodium salt (hereinafter - the Agent) for preventing and treating viral diseases caused by a tick-borne encephalitis virus. Also, there is described method for preventing and treating conditions caused by the tick-borne encephalitis virus in humans and animals involving introduction of the Agent presented above to humans and animals.

EFFECT: extended range of the drug preparations possessing a wide spectrum of action and used for treating and preventing tick-borne encephalitis.

20 cl, 2 ex, 1 tbl

FIELD: chemistry.

SUBSTANCE: invention relates to novel pyrrolo-[1,2-a]benzimidazole derivatives of formula I , where NR2 assumes morpholino or diethylamino values, and Ar is 4-methoxyphenyl or 4-chlorophenyl, having antioxidant and antiradical properties.

EFFECT: obtaining novel sulphates possessing useful biological properties.

2 tbl, 5 ex

FIELD: chemistry.

SUBSTANCE: invention relates to compounds of formula I:

or pharmaceutically acceptable salts thereof, in which Q is a divalent or trivalent radical selected from C6-10aryl and heteroaryl; where said aryl or heteroaryl in Q is optionally substituted up to 3 times with radicals independently selected from halogen, C1-6 alkyl, C1-6 alkyl substituted with halogen, C1-6 alkoxy group, C1-6 alkoxy group substituted with halogen, -C(O)R20 and -C(O)OR20; where R20 is selected from hydrogen and C1-6 alkyl; and where optionally, the carbon atom neighbouring W2 can be bonded through CR31 or O with a carbon atom of Q to form a 5-member ring condensed with A and Q rings; where R31 is selected from hydrogen and C1-6 alkyl; W1 and W2 are independently selected from CR21 and N; where R21 is selected from hydrogen and -C(O)OR25; where R25 denotes hydrogen; ring A can contain up to 2 carbon ring atoms substituted with a group selected from -C(O)-, -C(S)- and -C(=NOR30)- and can be partially unsaturated and contain up to 2 double bonds; where R30 denotes hydrogen ; L is selected from C1-6alkylene, C2-6alkenylene, -OC(O)(CH2)n-, -NR26(CH2)n- and -O(CH2)n-; where R26 is selected from hydrogen and C1-6 alkyl; where n is selected from 0, 1, 2, 3 and 4; q is selected from 0 and 1; t1, t2, t3 and t4 are each independently selected from 0, 1 and 2; R1 is selected from -X1S(O)0-2X2R6a, -X1S(O)0-2X2OR6a, -X1S(O)0-2X2C(O)R6a, -X1S(O)0-2X2C(O)OR6a, -X1S(O)0-2X2OC(O)R6a and -X1S(O)0-2NR6aR6b; where X1 is selected from a bond, O, NR7a and C1-4alkylene; where R7a is selected from hydrogen and C1-6alkyl; X2 is selected from a bond and C1-6alkylene; R6a is selected from hydrogen, cyanogroup, halogen, C1-6alkyl, C2-6alkenyl, C6-10aryl, heteroaryl, heterocycloalkyl and C3-8cycloalkyl; where said aryl, heteroaryl, cycloalkyl and heterocycloalkyl in R6a is optionally substituted with 1-3 radicals independently selected from hydroxy group, halogen, C1-6alkyl, C1-6alkyl substituted with a cyano group, C1-6alkoxy group and C6-10aryl-C1-4alkoxy group; and R6b is selected from hydrogen and C1-6alkyl; R3 is selected from hydrogen, halogen, hydroxy group, C1-6alkyl, C1-6alkyl substituted with halogen, C1-6alkyl substituted with a hydroxy group, C1-6alkoxy group, C1-6alkoxy group substituted with halogen, -C(O)R23 and -C(O)OR23; where R23 is selected from hydrogen and C1-6alkyl; R4 is selected from R8 and -C(O)OR8; where R8 is selected from C1-6alkyl, heteroaryl, C3-8cycloalkyl and heterocycloalkyl; where said heteroaryl, cycloalkyl or heterocycloalkyl in R8 is optionally substituted with 1-3 radicals independently selected from halogen, C1-6alkyl, C3-8cycloalkyl and C1-6alkyl substituted with halogen; R5 is selected from hydrogen, C1-6alkyl substituted with a hydroxy group, and a C1-6alkoxy group; heteroaryl denotes a monocyclic or condensed bicyclic aromatic ring complex containing 5-9 carbon atoms in the ring, where one or more ring members are heteroatoms selected from nitrogen, oxygen and sulphur, and heterocycloalkyl denotes a saturated monocyclic 4-6-member ring in which one or more said carbon atoms in the ring are substituted with a group selected from -O-, -S- and -NR-, where R denotes a bond, hydrogen or C1-6alkyl. The invention also relates to pharmaceutical compositions containing said compounds, and methods of using said compounds to treat or prevent diseases or disorders associated with GPR119 activity, such as obesity, type 1 diabetes, type 2 sugar diabetes, hyperlipidemia, type 1 autopathic diabetes, latent autoimmune diabetes in adults, type 2 early diabetes, child atypical diabetes, adult diabetes in children, malnutrition-associated diabetes and diabetes in pregnant women.

EFFECT: improved properties of compounds.

27 cl

FIELD: chemistry.

SUBSTANCE: present invention refers to the field of organic chemistry, notably to derivatives of dihydroimidazole with the general formula (I) and to its pharmaceutically acceptable salts where X1 and X2 denote halogen; R1 and R2 are chosen from the group including -H, -CH3, -CH2CH3 on the condition that both R1 and R2 do not denote hydrogen; R3 denotes -H or -C(=O)-R7; and if R6 denotes hydrogen, then R4 denotes -OCH3, -OCH2CH3 or -OCH(CH3)2; R5 denotes -H, - halogen, -CF3, -OCH3, -C(CH3)2, - cyclopropyl, - cyano group, -C(CH3)3, -C(CH3)2OR (where R denotes -H), -C(CH3)2CH-OR (where R denotes -CH3), -C(CH3)2CN, -C(CH3)2COR (where R denotes -CH3), -SR (where R denotes -CH2CH3) or -SO2R (where R denotes -CH3, -CH2CH3, 1-pyrrolidine, -NH-tert-butyl); and if R6 does not denote hydrogen, then R4 denotes -OCH2CH3; R5 denotes hydrogen, -Cl, -OCH3, tert butyl; R6 denotes -Cl, cyclopropyl, -SO2R (where R denotes -CH3, 1-pyrrolidine, -NH-tert-butyl or -N(CH3)2); and R7 is chosen from the group including i) -CH3, -CH(CH3)2, -CH2CH(CH3)2, cyclopropyl, cyclobutyl, -CH2CH2Ph, 2-furanyl, phenyl or phenyl substituted with chlorine, -OCH3 or cyano group, ii) 1-piperidinyl, iii) -NRc2 (where Rc denotes -CH2CH2OH, -CH2CH2OCH3 or -CH2CH(OH)CH2OH, iv) substituted piperazidine with the formula where R is chosen from the group including a) hydrogen, c) -CH(CH3)2, k) -CH2CH2Rd (where Rd denotes -OH, -OCH3, -CF3, -SO2CH3, -NH2, -NHCOCH3, -NHSO2CH3, 4-morfolinil, 2-izotiazolidinil-1, 1-dioxide), l) -CH2CH2CH2Re (where Re denotes -OCH3, -SO2CH3, -SO2CH2CH3, -CN), m) -CH2-CO-Rh (where Rh denotes -NH2, 1-pyrrolidinyl, 4-morfolinil), n) -SO2Ri (where Ri denotes -CH3, -CH2CH3), o) -CORj (where Rj denotes -CH3, 2-tetrahydrofuranyl, -NH2, -N(CH3)2), p) 4-tetrahydro-2H-thiopiranyl-1,1-dioxide, q) 4-piperidinyl-1-acetyl, r) 4-piperidinyl-1-dimethylcarboxamide, and s) 3-tetrahydrothiophenyl-1,1-dioxide; v) substituted oxopiperazine with the formula where R denotes -H; and vi) substituted piperidine with the formula where R denotes -CONH2, -OH, -CH2OH, -CH2CH2OH, 1-pyrrolidinyl, 1-piperidinyl, 1-(4-methylpiperazinyl) or 4-morfolinil. Moreover, the invention refers to the pharmaceutical composition based on the compound with the formula (I), to application of the formula (I) compound for production of a drug, to the production process of the formula (I) compound.

EFFECT: new derivatives of dihydroimidazole that may be used as anticancer drugs.

40 cl, 204 ex

FIELD: pharmachology.

SUBSTANCE: invention describes new compounds with general formula (I-c) Where R1 is a radical (d-1) or (d-2) (radical values are given in the invention formula) and pharmaceutical composition containing them. The described compounds are the hepatitis C inhibitors and can be used in medicine.

EFFECT: enhanced hepatitis C inhibition.

5 cl, 1 tbl, 19 ex

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention refers to compounds selected from a group consisting of compounds of formula: and or to their pharmaceutically acceptable salts. Also, the invention refers to a pharmaceutical composition, as well as to using at least one compound under cl.1 and/or its pharmaceutically acceptable salts.

EFFECT: preparing new biologically active compounds which exhibit the properties of cycline-dependent kinase inhibitors.

11 cl, 86 tbl

Kinase inhibitors // 2440352

FIELD: chemistry.

SUBSTANCE: invention relates to a compound of formula : a pharmaceutically acceptable salt or solvate thereof, having Syk kinase inhibiting properties. The invention also relates to a pharmaceutical composition containing said compound, methods of treating diseases whose development is aided by c-kit receptor activity, such as arthritis, rheumatoid arthritis, tumours, mantle cell lymphoma, as well as a method of inhibiting angiogenesis.

EFFECT: improved method.

13 cl, 4 tbl, 10 dwg

FIELD: chemistry.

SUBSTANCE: invention describes novel compounds of general formula in which is or (values of radicals are given in the claim), a method of producing said compounds, a pharmaceutical composition containing said compounds and therapeutic application thereof.

EFFECT: compounds are cysteine protease inhibitors and can be used in medicine.

25 cl, 1 tbl, 41 ex

FIELD: chemistry.

SUBSTANCE: invention relates to a method of producing 2,4,6,8-tetraazabicyclo[3.3.0]octane-3,7-dione (glycoluril). The reaction takes place at 80°C for 60 minutes, where concentrated sulphuric acid is used in an aqueous medium and reagents are taken in the following molar ratios: glyoxal 2.0; urea 4.0; sulphuric acid 0.4; water 12, and the freshly prepared glyoxal solution is added while stirring for 20 minutes, after which the mixture is stirred for 40 more minutes.

EFFECT: novel method of producing glycoluril, which increases output of the end product and is simpler.

1 cl, 1 tbl, 1 dwg

The invention relates to a derivative of methotrexate, more specifically, to novel derivatives of methotrexate suitable as an Antirheumatic agent, agent, healing psoriasis, and cancerostatic agent

FIELD: chemistry.

SUBSTANCE: invention refers to new compounds of formula (I): , where: each R0 independently stands for -H, -COOH, -OR', -SO3H, where R' stands for -H, lower alkyl, or, if x=2, both Ro are taken together to form 1,3-dioxolyl ring, or each Ro independently represents lower alkyl, each R1 and R2, is independent standing for hydrogen, G stands for (CR"2)p where R" stands for -H or acetamido and where p is equal to 0-3, Ar stands for aryl or 6-merous heteroaryl with one N atom as heteroatom, and each x and y is independent, equal to 1-4.

EFFECT: compounds I can be used in pharmaceutical compositions with vasculostatic activity, reducing overflow from blood vessels, for treating cancer, a heart attack and similar.

72 cl, 7 ex, 2 tbl

FIELD: medicine, pharmaceutics.

SUBSTANCE: present invention refers to compounds of general formula (I) or its pharmaceutically acceptable salts which have action of mTOR inhibitors. What is also declared is preparing a pharmaceutical composition containing a therapeutically effective amount of the compound of formula (I) and a pharmaceutically acceptable carrier or diluent; besides, what is declared is the use of the compound of formula (I) or its pharmaceutically acceptable salts for preparing the drug for ensuring anticancer action.

EFFECT: preparing the pharmaceutically acceptable salts for preparing the drug for ensuring anticancer action.

11 cl, 25 ex

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention refers to new compounds of formula (I), treating a disease related to proteinkinase activity inhibition, specifically cancer, particularly leukaemia, a method of treating such disease and a method of producing such compounds. In formula (I) R1 represents hydrogen, lower alkyl, lower alkoxy-lower alkyl; R2 represents lower alkyl substituted by one or more identical or different radicals R3, cyclohexyl, cycloheptyl, benzcyclopentyl(indane), benzcyclohexyl, penta-, hexa- or heptamerous heterocyclic system with one or two heteroatoms specified in a group consisting of nitrogen and oxygen which can be unsaturated or completely saturated, and is unsubstituted or substituted by lower alkyl, phenyl-lower alkyl or oxo; phenyl which is unsubstituted or substituted by one or two substituted specified in a group consisting of lower alkyl, lower alkoxycarbonylpiperidino-lower alkyl, N-lower alkylpiperazino-lower alkyl, lower alkoxycarbonyl-lower alkyl, lower alkoxy, 1H-imidazolyl-lower alkoxy, lower alkoxycarbonyl, lower alkylcarbamoyl, amino mono- or disubstituted lower alkyl, morpholino, lower alkylsulphonyl, halogen and benzoyl; and the value R3 is specified in the patent claim, or R1 and R2 together represent alkylene with four, five or six carbon atoms, optionally mono- or disubstituted by lower alkyl; hexamerous heterocyclic system with one or two heteroatoms specified in a group consisting of nitrogen which can be unsaturated or completely saturated, and is unsubstituted or substituted according to the patent claim, R4 represents hydrogen or lower alkyl.

EFFECT: preparing the composition for treating a disease related to proteinkinase activity inhibition.

5 cl, 99 ex

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention refers to a compound of formula I wherein the substitutes A, B, B', Q and R1-R5 in formula I are specified as follows: A and B' are one of the following groups: (i) (R6)N(CH2)n, wherein n is 0 or 1; (ii) (CH2)n, wherein n is 0, 1 or 2; (iii) C(O)(CH2)n, wherein n is 0 or 1; or provided each of A and B' represents nitrogen, together they can form a bivalent radical of formula: -(CH2)s-X1-(CH2)t- (a), wherein each s and t is independently 1 or 2, and X1 represents (CH2)n, wherein n is 0 or 1; B is one of the following groups: (i) (R6)N; (ii) oxygen; (iii) C=δ, wherein δ represents oxygen or sulphur; (iv) C(R6)=C(R7); each R6 and R7 independently represent hydrogen, C1-4-alkyl; R1 is specified in the following groups: (i) phenyl group substituted by one or more substitute such as: - halogen specified in F, CI, Br or I, or alkyl1 group; aryl1 or heteroaryl group1; cyano, NH-alkyl1, N(alkyl1)(alkyl1) and amino; - NHCO-R or NHCOO-R, or COO-R, or CONH-R, wherein R represents hydrogen or alkyl group, or (ii) pyridinyl group which can be substituted by one substitute, such as halogen specified in I, F, Cl or Br; alkyl1 group; aryl1 group; cyano, NH-alkyl1, N(alkyl1)(alkyl1), and amino; -NHCO-R or NHCOO-R, or COO-R, or CONH-R, wherein R represents hydrogen or alkyl1 group; each R2, R3, R4 and R5 are independently specified in hydrogen or linear or branched alkyl group containing 1 to 10 carbon atoms; Q is specified in the following groups: (i) alkyl1; (ii) aryl1; (iii) heteroaryl1. The compounds of formula (I) are used for preparing a drug showing the c-kit inhibitor properties and aiming at treating a disease specified in neoplastic, allergic, inflammatory and autoimmune diseases.

EFFECT: use of oxazole derivatives as tyrosine kinase inhibitors.

13 cl, 1 tbl, 31 ex

FIELD: chemistry.

SUBSTANCE: present invention relates to a method of producing (-)-beta-elemenal, use of (-)-beta-elemenal as an antitumour agent, as well as to a pharmaceutical composition and a medicinal agent based on said compound. The method involves reaction of a mixture of isomeric beta-elemenols (2:1) with c MnO2, activated in a vacuum at 150°C as a catalyst. The initial mixture of isomeric beta-elemenols (2:1) is obtained by reacting a mixture of diastereomeric epoxides (2:1) with diisopropylamine in the presence of n-BuLi.

EFFECT: higher efficiency.

4 cl, 21 tbl, 9 dwg, 36 ex

FIELD: medicine, pharmaceutics.

SUBSTANCE: preparation shows high bactericidal and antimetastatic activity that is ensured by the presence of a water extract of shelf fungus and birch bark taken in weight proportions 1:4.

EFFECT: preparation shows bactericidal and antimetastatic activity.

3 tbl

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention refers to medicine. What is offered is an agent for treating cancer in the form of a solution for injections in the following ratio (wt %): 5-fluorouracil - 0.087, metronidazole - 0.5, water for injections - 1.841, low-molecular polyethylene - 66.527, emulsifier T-2 - 16.778, Lutrol F-127 - 1.677, Cremophore RH 40 - 2.520, olive oil - 10.070.

EFFECT: invention provides preparing the agent for treating female genital cancer showing anticancer and antimicrobial activity, uniformly distributed in tissues, having manifested prolonged action and being accessible.

2 dwg, 3 tbl, 3 ex

FIELD: medicine, pharmaceutics.

SUBSTANCE: what is offered is using 40-O-(2-hydroxyethyl)rapamycin for preparing a pharmaceutical composition for treating a renal tumour representing carcinoma.

EFFECT: 40-O-(2-hydroxyethyl)rapamycin twice reduces tumour growth time or death rate of the patients with advanced renal cell carcinoma.

1 tbl

FIELD: medicine.

SUBSTANCE: invention refers to medicine, oncology, and can be used for combination treatment of the patients suffering eyelid malignancies. A method involves local radiomodification by peritumoral introduction of Methotrexate 10 mg pre-incubated in autoplasma 10 ml at t=37°C for 30 minutes preceded by subbulbar introduction of diprospan 1 ml. One hour later, the radiomodification is followed by neoadjuvant radiation therapy at depth 0.5 cm by basic dose 20 Gy, and no more than 24 hours after the radiation, a surgical operation is performed.

EFFECT: method provides intensified radicality of the tumour exposure, higher surgical ablasticity, lower risk of cancer dissemination, maximally maintained reparation ability and functions of normal ocular tissues, minimised therapeutic complications, reduced length of treatment.

1 ex

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