3-aroyl-2-(2-arylhydrazono)pyrrolo [1,2-a] quinoxaline,4-(2h,5h)diones possessing analgesic activity

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention refers to 3-aroyl-2-arylhydrazonopyrrolo[1,2-a]quinozaline-1,4(2H,5H)-diones of formula:

Ar=Ph, R=Me, R1=H (a); Ar=4-MeC6H4 R=Me, R1=H (b); Ar=Ph, R=H, R1=COOH (c).

EFFECT: there are produced new compounds possessing analgesic activity that makes them being suggested to be used in medicine as drugs with the analgesic properties.

1 cl, 3 tbl, 4 ex

 

The invention relates to the field of organic chemistry, new biologically active substances of class 3-aroyl-2-arylhydrazonothiocarbamoilacetamides, namely 3-aroyl-2-arylhydrazones[1,2-a]cinoxacin-1,4(2H,5H)-diones of the formula (1):

possessing analgesic activity, suggesting their use in medicine as a drug with analgesic properties (table 1).

Similar to the structure of the claimed range of compounds are 3-koilpillai[1,2-a]cinoxacin-1,2,4-trions (Ia,b) [Mashevsky IV, Makhmudov P.P., Alexandrov G.A., Golovnina O.V., Duvanov A.V., A. N. maslivets. Synthesis, antibacterial and analgesic activity of 3-acyl-1,2,4,5-tetrahydropyrrolo[1,2-and]cinoxacin-1,2,4-trions // Chem-Pharm. Journe. 2001. T.35. No. 4. P.20-21] formula:

A benchmark comparison of selected Metamizole sodium formula:

which is widely used in medical practice and is similar in action [Mashkovsky PPM Medicines.- 15th ed., Rev., Corr. and extra - M.: OOO "New wave", 2005. - s].

Table 1
No. of connectionsDose, mg/kgLD50 mg/kgDefensive reflex at the peak of action (C)
Control 2% krahm. mucus5010,6±1,21
Metamizole sodium9316,3±3,0 ρ<0,1
Ia50>150024,3±9,3 ρ<0,05
IB50>150024,8±9,4 ρ<0,05

Object of the invention is the finding in a series of derivatives of 3-aroyl-2-arylhydrazones-pyrroloquinoline substances with pronounced analgesic effect and low toxicity.

This object is achieved by obtaining the number of 3-aroyl-2-arylhydrazones [1,2-and]cinoxacin-1,4(2H,5H)-diones, which possess analgesic activity.

The claimed compounds IIA-synthesized by the interaction of 3-koilpillai[1,2-a]cinoxacin-1,2,4(5H)-Trion with arylhydrazines in the medium of anhydrous acetonitrile at 80-82°C, followed by separation fawn product known methods according to the scheme:

Example 1. Obtaining compounds IIa

<> (E)-3-Benzoyl-2-(o-tolylhydrazine)pyrrolo[1,2-and]cinoxacin-1,4(2H,5H)-dione (IIa)

To a solution of 3.18 g (1.0 mmol) 3-benzopyrrole[1,2-a]cinoxacin-1,2,4(5H)-trione in 30 ml of absolute acetonitrile is added a solution of 1.22 g (1.0 mmol) of the hydrochloride of o-tolylhydrazine in 10 ml of absolute dimethylformamide (DMF), boiled for 3 min, cooled, the precipitate is filtered off and recrystallized from DMF. Yield 2.41 g of 57%, TPL 246-248°C. Found, %: C, 70.12; H, 4.26; N, 13.21. C25H18N4O3. Calculated, %: C, 71.08; H, 4.30; N, 13.26. IR spectrum (FSM-120, vaseline oil, ν, cm-1): 3200, 3180 (NH), 1673 (C1=0), 1660 (C4=O), 1624 (COPh). An NMR spectrum1H (Braker AM-400 [operation frequency 400 MHz] in DMSO-d6, internal standard TMS. δ, ppm): 2.07 (s, 3H, Me), 7.07-8.03 hrs (11H, Ph+C6H3+H6-8), 8.71 (1H, H9, J 7.3 Hz), 11.26 (1H, N5H), 13.57 (1H,=N-NH).

The obtained compound IIa is a dark red crystalline substance, soluble in DMF, DMSO, acetonitrile, and insoluble in water and hexane.

Example 2. Obtaining compounds IIB

(E)-3-(4-Methylbenzoyl)-2-(o-tolylhydrazine)pyrrolo[1,2-and]cinoxacin-1,4(2H,5H)-dione (IIA)

To a solution of 3.32 g (1.0 mmol) 3-(4-methylbenzoyl)pyrrolo[1,2a]cinoxacin-1,2,4(5H)-trione in 30 ml of absolute acetonitrile is added a solution of 1.22 g (1.0 mmol) of the hydrochloride of o-tolylhydrazine in 10 ml of absolute dimethylformamide (DMF),boiled for 3 min, cool, the precipitate is filtered off and recrystallized from DMF. Yield 2.14 g of 49%, TPL 260-262°C. Found, %: C, 71.52; H, 4.60; N, 12.80. C26H20N4O3. Calculated, %: C, 71.55; H, 4.62; N, 12.84. IR spectrum (FSM-120, vaseline oil, ν, cm-1): 3180, 3050 (NH), 1671 (C1=O), 1657 (C4=O), 1617 (COTol). An NMR spectrum1H (Bruker AM-400 [operation frequency 400 MHz] in DMSO-d6, internal standard TMS. δ, ppm): 2.38 (s, 3H, Me), 2.51 (s, 3H, Me), 7.09-8.15 hrs (11H, 2C6H4+H6-8), 8.73 (1H, H9, J 7.4 Hz), 11.28 (1H, N5H), 13.57 (1H, =N-NH).

The obtained compound IIB is a dark red crystalline substance, soluble in DMF, DMSO, acetonitrile, and insoluble in water and hexane.

Example 3. For obtaining compounds IIB

(E)-4-(2-(3-Benzoyl-1,4-dioxaborolan)[1,2-and]cinoxacin-2(1H)-ilidene)-hydrazine)benzoic acid (IIB)

To a solution of 3.18 g (1.0 mmol) 3-benzopyrrole[1,2-a]cinoxacin-1,2,4(5H)-trione in 30 ml of absolute acetonitrile is added a solution (1.0 mmol) of the hydrochloride of 4-hydrazinobenzene acid (n-carboxyanhydride) in 10 ml of absolute dimethylformamide (DMF), boiled for 3 min, cooled, the precipitate is filtered off and recrystallized from DMF. Yield 3.12 g 69%, TPL 310°C. Found, %: C 66.35; N, 3.54; N, 12.35. C25H16N4O5. Calculated, %: C 66.37; N, 3.57; N, 12.38. IR spectrum (FSM-120, vaseline oil, ν,cm -1): 3400 (COOH), 3180, 3050 (NH), 1676 (C1=O), 1660 (C4=O), 1633 (COPh). An NMR spectrum1H (Bruker AM-400 [operation frequency 400 MHz] in DMSO-d6, internal standard TMS. δ, ppm): 7.12-7.66 hrs(N, Ph+C6H4+H6-8), 8.68 (1H, H9, J 7.4 Hz), 11.27 (1H, =N5H), 13.28 (1H, =N-NH).

Example 4. Study of the biological activity

Evaluation of the analgesic properties of the compounds (IIA, b) studied in outbred mice weighing 18-22 g by the method of thermal stimulation "hot plate" Eddie and Leimbach (N.B. Eddy, Leimbarh D.J. Pharmacol and.. Gher. 1953., 385-393). The test substance at a dose of 50 mg/kg was administered vnutribruchinno as a suspension in 2%starch solution (table 2)

In the study of analgesic action of the compounds (IIA-b) according to the method of acetic cramps (table 3) compounds were administered at a dose of 50 mg/kg as a suspension in 2%starch mucus for 30 minutes before the intraperitoneal injection of 0.75%aqueous solution of acetic acid (0.1 ml/10 g).

The product comparison - Metamizole sodium (93 mg/kg).

Control 2% krahm. mucus
Table 2
Analgesic activity of compounds IIA, b ("hot plate")
No. of connectionsDose, mg/kgDefensive reflex at the peak of action (C)
50of 10.76±1,63
Metamizole sodium9316.3±3.0
IIa5026.11±3.38
IIb5026.00±3.26

Table 3
Analgesic activity of compounds IIA-b ("acetic cramps")
No. of connectionsDose, mg/kg% suppression cramps
Control 2% krahm. mucus50,/b0
Metamizole sodium9358
IIa50, p/o65.34
IIb50, p/o70.14
IIb50, p/o46.6

Studies have shown (table 2, 3)that the organisations (IIA-C) significantly increased the pain threshold in animals as thermal effects, and acetic acid writhing", outperforms active comparator drug - Metamizole sodium.

3-Aroyl-2-(2-arylhydrazones)pyrrolo[1,2-a]cinoxacin-1,4(2H, 5H)-diones of General formula:

possessing analgesic activity.



 

Same patents:

FIELD: chemistry.

SUBSTANCE: invention describes novel, highly crystalline mono(benzenesulphonic acid)besylate salts and polymorphs of the compound of formula (I): , a pharmaceutical composition containing said compounds, methods of producing the salts and use thereof as medicinal agents, particularly for sedative or hypnotic, anxiolytic, muscle relaxation or anticonvulsant purposes.

EFFECT: improved method.

32 cl, 36 dwg, 22 tbl, 10 cl

FIELD: chemistry.

SUBSTANCE: invention relates to a novel tricyclic derivative of chemical formula 1 or pharmaceutically acceptable salts thereof: formula 1, where Y1, Y2 and Y3 independently denote H, C1-C10 alkyl with a straight or branched chain, hydroxy, C1-C10 alkoxy, -CCOR1, -NR2R3 or -A-B; A denotes -O-, -CH2-, -CH(CH3)-, -CH-N- or -CONH-; B denotes -(CH2)n1-Z, -(CH2)n2-NR2R3 or -(CH2)n3-OR1; Z denotes C5-C20 aryl, unsubstituted or substituted with R5 and selectively R6, C3-C10 cycloalkyl, unsubstituted or substituted with R5 and selectively R6, C1-C20 heterocyclic compound, unsubstituted or substituted with R5 and selectively R6; R1 denotes H or C1-C10 alkyl with a straight or branched chain; R2 and R3 independently denote H, C1-C10 alkyl with a straight or branched chain or -(CH2)n4R7; R5 denotes H, C1-C10 alkyl with a straight or branched chain, C5-C20 aryl or C1-C20 heterocyclic compound; R6 denotes H or C1-C10 alkyl with a straight or branched chain; R7 denotes -NR8R9, -COOR1, -OR1, -CF3, -CN, halogen or Z; R8 and R9 independently denote H or C1-C10 alkyl with a straight or branched chain; n1-n4 respectively denote an integer from 0 to 15; Y denotes H or C1-C10 alkyl with a straight or branched chain. The invention also relates to methods of producing a compound of formula 1, compositions containing the described compound and with effective inhibiting activity on poly(ADP-ribose)polymerase (PARP).

EFFECT: obtaining and describing novel compounds which can be suitable for preventing or treating diseases caused by excess PARP activity, especially neuropathic pain, neurodegenerative diseases, cardiovascular diseases, diabetic neuropathy, inflammatory diseases, osteoporosis and cancer.

23 cl, 123 ex, 7 tbl, 2 dwg

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention refers to a compound of formula possessing action on a BH4 sensitive condition.

EFFECT: invention refers to a pharmaceutical composition containing said compound to applying the compound for preparing a drug for treating the BH4 sensitive condition, such as a vascular disease, a psychoneurological disease, hyperphenylalaninemia.

12 cl, 31 dwg, 20 ex

FIELD: medicine, pharmaceutics.

SUBSTANCE: described are novel derivatives of hexahydro pyrazino [2,1-c][1,2,4]triazine of general formula (III) (values of radicals are given in invention formula), their pharmaceutically acceptable salts and application of said compounds for obtaining medication for treatment and prevention of acute myeloid leukemia.

EFFECT: obtaining medication for treatment and prevention of acute myeloid leukemia

3 cl, 3 ex, 6 tbl

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention refers to substituted tetrahydropyrrolopyrazines of general formula I, wherein R1, R2 and R3 in each case independently mean hydrogen or groups R1 and R2 or R2 and R3 form a common cycle ; R4 and R5 in each case independently mean H; R6 means branched or unbranched saturated, unsubstituted C1-6-alkyl, or unsubstituted heteroaryl wherein heteroaryl is a 5- or 6-member aromatic residue containing 1 heteroatom specified in a group consisting of N, O and S, or means phenyl wherein phenyl is unsubstituted or single-substituted or double-substituted by 1 or 2 substitutes which in each case are independently specified in a group consisting of F, Cl, Br, I, CF3, C1-6-alkyl, O-C1-6-alkyl, and , or means unsubstituted phenyl attached through C1-3-alkyl chain; R4a, R5a and R6a in each case independently mean H; R7 means (CH2)tC(=O)R8, wherein t is equal to 1, (C=O)(CH2)mNR11R12, wherein m is equal to 1 or 2, C(=O)(CH2)n(C=O)R8, wherein n is equal to 1, 2 or 3, (CH2)sNHC(=O)R8, wherein s is equal to 1 or 2; R8 means NR9R10 or saturated, branched or unbranched, unsubstituted C1-6-alkyl; wherein R9 and R10 in each case independently mean H, saturated, branched or unbranched, unsubstituted C1-6-alkyl, or unsubstituted or saturated C3-8-cycloalkyl, or phenyl, or phenyl attached through C1-3-alkyl wherein the alkyl chain is saturated, branched or unbranched, and wherein phenyl in each case is unsaturated or single or double saturated by 1 or 2 substitutes which independently specified in a group consisting of F, Cl, Br, I, CF3, C1-6-alkyl, O-C1-6-alkyl, pyridyl, and , or unsubstituted heteroaryl attached through C1-3-alkyl wherein heteroaryl is a 5-member aromatic residue 1 heteroatom of which are specified in a group consisting of O and S, wherein the alkyl chain is saturated, branched or unbranched, or heterocyclyl, or heterocyclyl attached through C1-3-alkyl wherein the alkyl chain is saturated, branched or unbranched, and wherein heterocyclyl in each case is saturated, unsubstituted or single substituted by benzyl, and heterocyclyl contains cycloalkyl containing 5 to 6 atoms in a cycle wherein 1 or 2 carbon atoms are substituted by 1 or 2 heteroatoms which are specified in a group consisting of N; or both groups R9 and R10 mean (CH2)3-6, CH2CH2OCH2CH2 or CH2CH2NR14CH2CH2; wherein R14 means phenyl or phenyl attached through C1-3-alkyl wherein phenyl in each case is unsaturated or single substituted by a substitute whih is specified in a group consisting of F, Cl, Br, I, O-C1-6-alkyl, and , or R14 means C(=O)R13; wherein R13 means saturated and unbranched C1-6-alkyl or means phenyl condensed with heteroaryl wherein heteroaryl is a 6-member aromatic residue 1 heteroatom of which is specified in a group consisting of N; R11 and R12 in each case independently mean H, saturated, branched or unbranched C1-6-alkyl, or unsubstituted, saturated C3-8-cycloalkyl, C(=O)R20 or S(=O)2R13; wherein R20 means NR21NR22, or R20 means saturated, branched or unbranched C1-6-alkyl, or means saturated C3-8-cycloalkyl, unsubstituted or single substituted by phenyl, or means unsaturated heteroaryl wherein heteroaryl is a 5-member aromatic residue 1 heteroatom of which is specified in a group consisting of O, or means phenyl wherein phenyl is unsubstituted or single substituted by C1-6-alkyl or means phenyl attached through C1-6-alkyl which is unsubstituted or single substituted by a substitute specified in a group consisting of F, Cl, Br, I and CF3, wherein the alkyl chain is saturated or unsaturated, branched or unbranched; wherein R21 and R22 in each case independently mean H or saturated, branched or unbranched, unsubstituted C1-6-alkyl; in the form of bases and salts of physiologically acceptable acids. The invention also refers to methods for preparing them, to drug preparations for treating disorders or diseases related with at least partially KCNQ2/3 K+ canals containing such compounds.

EFFECT: there are prepared new compounds and based drug preparations which can find application in medicine for managing pain, epilepsy, migraine, panic conditions and urinary incontinence.

17 cl, 2 tbl, 91 ex

FIELD: chemistry.

SUBSTANCE: present invention relates to fluorinated compounds of formula , where: D, G and L are independently selected from a group consisting of: CH, C and N, and J and M are independently selected from a group consisting of C and N, under the condition that one of J and M denotes C and the other denotes N, wherein at least two of D, G, M, J and L denote N; X denotes CH2; Y is absent; Z denotes NR1R2; R1 and R2 are independently selected from a group consisting of: hydrogen, C1-C10 alkyl, aryl and heteroaryl, which is associated with aromatic radicals having 6 ring atoms, where 1-2 of these ring atoms are N; each of which can be substituted with one or more halogen atoms; or R1 and R2, together with nitrogen to which they are bonded, form a heterocyclic ring having 5 ring members; R3 is selected from a group consisting of: halogen, C1-C10 alkyl; E denotes aryl which can be substituted with one or more fluoro-substitutes or one or more of the following substitutes: C1-C6 alkyl, QC1-C10 alkyl, QC2-C10 alkenyl, each of which can be substituted with one or more fluoro-substitutes, and where Q denotes O; m denotes a number from 1 to 2; under the condition that: R3 is a fluoro-substitute, or group E includes a fluoro-substitute, or group Z includes a fluoro-substitute, with the condition that E does not denote 4-fluorophenyl or a compound of formula , where D, G and L are independently selected from a group consisting of: CH, C and N, and J and M are independently selected from a group consisting of C and N, under the condition that one of J and M denotes C and the other denotes N, wherein at least two of D, G, M, J and L denote N; X denotes CH2; Y is absent; Z denotes NR1R2; R1 and R2 are independently selected from a group consisting of: hydrogen, C1-C10 alkyl, aryl and heteroaryl, which is associated with aromatic radicals having 6 ring atoms, where 1-2 of these ring atoms are N; each of which can be substituted with one or more of the following substitutes: chlorine, bromine, iodine; or R1 and R2, together with nitrogen to which they are bonded, form a heterocyclic ring having 5 ring members; R3 is selected from a group consisting of: chlorine, bromine, iodine, C1-C10 alkyl; E denotes aryl which can be substituted with one or more chlorine, bromine or iodine atoms, and/or one or more of the following substitutes: C1-C6 alkyl, QC1-C10 alkyl, QC2-C10 alkenyl, each of which can be substituted with one or more substitutes selected from chlorine, bromine, iodine or hydroxy, where Q denotes O, wherein when E denotes phenyl, E does not contain, as a substitute, iodine which is directly bonded to it at position 4; m denotes a number from 1 to 2; wherein at least one of Z, E and R3 includes iodine; under the condition that E does not denote 4-iodophenyl and under the condition that said compound is not a compound of formula (Ia), defined in the following table:

The invention also relates to a pharmaceutical composition based on the compound of formula (I) or (Ia), a diagnosis method, a method of treating said disorders, based on use of the compound of formula (I) or (Ia), and use of the compound of formula (I) or (Ia).

EFFECT: obtaining novel compounds useful in treating disorders in mammals, characterised by anomalous density of peripheral benzodiazepine receptors.

24 cl, 13 dwg, 9 tbl, 23 ex

FIELD: medicine.

SUBSTANCE: invention refers to an agent for activation of lipoprotein lipase containing a benzene derivative of general formula (1) which is used for preventing and treating hyperlipidemia and obesity. The invention also refers to the benzene derivatives of general formula (1a).

EFFECT: composition improvement.

8 cl, 6 tbl, 9 ex

FIELD: medicine, pharmaceutics.

SUBSTANCE: present invention refers to new bicyclic heterocyclic derivatives of general formula wherein radicals and symbols are specified in the patent claim. Said compounds are FGFR receptor (fibroblast growth factor receptor) inhibitors. The invention also refers to a method for preparing a preferential group of compounds of formula (I), to a pharmaceutical composition containing said compounds, and to the use of said compounds for treating diseases, e.g. cancer.

EFFECT: preparing the new bicyclic heterocyclic derivatives.

22 cl, 16 tbl, 422 ex

FIELD: chemistry.

SUBSTANCE: invention relates to novel bicyclic heterocyclic derivatives, which are compounds of formula where values of X1-X5, A, B, R1, R2, q are given in claim 1, as well as pharmaceutical compositions containing said compounds, and use of said compounds to treat cancer.

EFFECT: high efficiency of treatment.

22 cl, 43 ex

FIELD: chemistry.

SUBSTANCE: described are novel azolo[1,2,4,5]tetrazine derivatives of general formula I, where Het=3,5-dimethylpyrazol-1-yl, X=N, R=cyclopropylmethylthio or pentylthio; or Het=3,5-dimethylpyrazol-1-yl, X=CH, R=isopropylthil; or Het=imidazol-1-yl, X=CH, R=H, and use of said compounds and additionally compounds of general formula (I), where Het=3,5-dimethylpyrazol-1-yl, X=N, K=cyclopentylthio; or Het=3,5-dimethylpyrazol-1-yl, X=CH, R=H or phenylthio based on disclosed activity as inhibitors of protein kinase PknA, PknB Mycobacterium tuberculosis when treating tuberculosis patients.

EFFECT: high efficiency of treatment.

2 cl, 2 tbl, 10 ex

FIELD: medicine, pharmaceutics.

SUBSTANCE: what is presented is the use of N-vinylpyrrolidone copolymer presented by general formula (I) wherein a monomer link M represents a fragment of 2-methyl-5-vinyltetrazole (MVT) or 2-methyl-5-vinylpyridine (MVP) and the monomer link content n makes 25-90 mole %, while a viscosity-average molecular weight Mµ of the copolymer depends of the M nature: if M represents MVT, then Mµ=100-250 kDa; if M represents MVT, then Mµ=46-150 kDa in a dose of 200 to 2000 mcg/kg (previously known as a phagocytosis activator) as an agent potentiating an analgesic effect of morphine hydrochloride. A reliable increase of a pain threshold combined with the simultaneous introduction of the copolymer and morphine hydrochloride is shown.

EFFECT: invention provides a double reduction of the morphine dose with keeping a level of analgesia.

4 tbl, 4 ex

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention refers to medicine, and concerns a solid or semi-liquid pharmaceutical dosage form containing a non-steroid anti-inflammatory drug, namely a propionic acid derivative - ibuprofen together with a second active ingredient having a shorter period of a therapeutically effective plasma concentration, namely Phenylephrine, and a method for introducing it.

EFFECT: invention provides an intensified therapeutic effects, particularly pain control together with decongestion for a longer period of time.

25 cl, 15 ex, 9 tbl

FIELD: medicine, pharmaceutics.

SUBSTANCE: stable fat emulsion contains prostaglandin as an active ingredient and phospholipids containing phosphatidylcholine and phosphatidyl glycerol in mass ratio 85:15 to 99.7:0.3. The fat emulsion under the invention and its active ingredient (prostaglandin) possess physical and chemical stability thereby increasing shelf life to approximately two years, and/or extended range of storage temperature to 10°C as compared with a commercially available fat prostaglandin emulsion.

EFFECT: fat emulsion under the invention enables satisfactory effectiveness even in the introduction of a low amount.

25 cl, 10 tbl, 12 ex

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention relates to compounds of formula I: where R, R1, R2, R3, R4, x and z are determined in items of the invention formula, useful as inhibitors of voltage-gated sodium channels.

EFFECT: invention claims pharmaceutically acceptable compositions, which contain said compounds and methods of applying such compositions for treatment of various diseases.

76 cl, 3 tbl

FIELD: medicine.

SUBSTANCE: pharmaceutical composition for prevention or treatment of inflammatory intestinal diseases (IID), which contains 7,8-dimethoxy-4(5H),10-dioxo-1H-1,2,3-triasolo[4,5-c][1]-benzazepine, or its prodrug, preferably 2-(1-isopropoxycarbonyloxy-2-methypropyl)-7,8-dimethoxy-4(5H), 10-dioxi-2H-1,2,3-triasolo[4,5-c] [1]benzazepine, or its pharmaceutically acceptable salt; respective method of prevention or IID treatment and application of said compounds for manufacturing preventive or therapeutic substance against IID. Demonstrated is efficiency of claimed pharmaceutical composition, more powerful than sulfasalazine and prednisolon with respect to said purpose, in combination with high safety. Shown are few side effects of compounds, absence of inhibition of IL-2, IL-4, IL-5, IFN-gamma, absence of weight gain restraint resulting from treatment.

EFFECT: pharmaceutical composition in accordance with claimed invention can demonstrate powerful preventive and therapeutic action, even in case of severe form of disease with resistance to conventional therapeutic agents.

28 cl, 3 dwg, 9 tbl

FIELD: medicine.

SUBSTANCE: invention is related to a two-layer composition for acetaminophen and tramadol delivery for at least twelve-month period after the initial introduction. A first layer determines fast release of a part of the composition and contains acetaminophen. A second layer determines continuous release of a part of the composition and contains acetaminophen, tramadol and cross-linked high-amylose starch. The single introduction of the two-layer composition may provide an anaesthising effect for a period of time within the range of a half an hour to approximately one hour after the introduction making at least twelve hours after the initial introduction.

EFFECT: two-layer compositions under the invention may be used for providing both fast, and continuous anaesthising effect in a patient in need thereof.

24 cl, 10 dwg, 5 tbl, 5 ex

FIELD: medicine.

SUBSTANCE: present group of inventions refers to medicine, namely therapy and paediatrics, and concerns treating or preventing systemic inflammation. That is ensured by a food formulation and a diet containing the food formulation containing inactivated Lactobacillus rhamnosus GG in the amount effective to provide 1×104-1×1010 cell equivalents of inactivated Lactobacillus rhamnosus GG per one kg of body weight a day.

EFFECT: introduction of such composition provides effective reduction of the body level of proinflammatory cytokines.

12 cl, 2 ex, 1 tbl, 6 dwg

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention refers to pharmaceutical industry and represents a nutrient formulation for infant or baby for prevention or relief of systemic inflammation, containing: a lipid source, a carbohydrate source, a protein source, vitamins, mineral substances and at least one thermally inactivated Lactobacillus rhamnosus GG, with the nutrient formulation providing delivery of approximately 1×104 to approximately 1×1010 cell equivalents of inactivated Lactobacillus rhamnosus GG per one kg of body weight a day to an infant or baby.

EFFECT: invention provides preservation of the cell and molecular-biological reaction properties of the living probiotic which are effective in treating, relieving or preventing systemic inflammation.

10 cl, 2 ex, 1 tbl, 6 dwg

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention refers to chemical-pharmaceutical industry and represents the use of sodium metaarsenite in preparing an oral dosage form of a pharmaceutical composition for inflammation treatment in a mammal.

EFFECT: use of sodium metaarsenite in preparing the oral dosage form of the pharmaceutical composition for inflammation treatment in a mammal.

6 cl, 7 ex, 1 dwg

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention relates to homogenous pharmaceutical composition for treatment of inflammatory disorders, which contains mixture of steroid anti-inflammatory or anti-histamine active ingredient in pharmaceutically acceptable water carrier with liposome. As steroid anti-inflammatory ingredient used is budesonide or fluticasone or their pharmaceutically acceptable salt, and antihistamine preparation is represented by azelastine or its pharmaceutically acceptable salt, concentration of active ingredient in water carrier is, in fact, equal inside and outside liposomic structures and varies ±20% when concentration of active ingredient inside and outside liposomic structures is compared. Polar lipid is swellable in water and represents phospholipid or glycosphingolipid. Invention also relates to method of composition obtaining, which lies in joint mixing of polar lipid, water phase and said active ingredient and mixture homogenising. Invention also relates to method of treating inflammatory disorders, including introduction of claimed composition to individuum, suffering from or sensitive to said disorders.

EFFECT: invention ensures reduction of irritation, for instance, in case of nasal introduction of composition.

52 cl, 9 ex

FIELD: medicine, pharmaceutics.

SUBSTANCE: described are novel derivatives of hexahydro pyrazino [2,1-c][1,2,4]triazine of general formula (III) (values of radicals are given in invention formula), their pharmaceutically acceptable salts and application of said compounds for obtaining medication for treatment and prevention of acute myeloid leukemia.

EFFECT: obtaining medication for treatment and prevention of acute myeloid leukemia

3 cl, 3 ex, 6 tbl

Up!