4-(4-bromophenyl)-4-oxo-2-{[3-ethoxycarbonyl)-4,5-dimethylthien-2-yl]amino}-2-butenoic acid, having anti-inflammatory and analgesic activity

FIELD: chemistry.

SUBSTANCE: invention relates to organic chemistry and specifically to novel biologically active substances of the class of 4-aryl-2,4-dioxobutanoic acids. Disclosed is 4-(4-bromophenyl)-4-oxo-2-{[3-ethoxycarbonyl)-4,5-dimethylthien-2-yl]amino}-2-butenoic acid, having anti-inflammatory and analgesic activity, of formula (1): .

EFFECT: obtaining a compound with high output, having marked anti-inflammatory and analgesic activity as well as low toxicity.

1 cl, 1 tbl

 

The invention relates to the field of organic chemistry, new biologically active substances of class 4-aryl-2,4-dioxobutane acids, namely 4-(4-bromophenyl)-4-oxo-2-{[3-(etoxycarbonyl)-4,5-dietitian-2-yl]amino}-2-butenova acid (1) formula:

Possessing anti-inflammatory and analgesic activity, suggesting its use in medicine as a drug with anti-inflammatory and analgesic properties.

Similar to the structure of the claimed compounds is 4-(4-were)-4-oxo-2-[3-etoxycarbonyl-4,5-dimethylthiophene-2-ylamino]but-2-ANOVA acid (2) [4-(4-were)-4-oxo-2-[3-etoxycarbonyl-4,5-dimethylthiophene-2-ylamino]but-2-ENOVIA acid, which has anti-inflammatory and analgesic activity: U.S. Pat. 2389724 Grew. Federation. No. 2008151813/04; Appl. 25.12.08; publ. 20.05.10, bull. No. 14] formula:

The data on anti-inflammatory and analgesic activity:

Connection% inhibition carragenine edema after 4 hoursThe latent period of the defensive reflex, after 2 hours
235,3 23,5

A benchmark comparison of selected ortofen formula:

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

Object of the invention is the finding in a series of derivatives of 4-aryl-2,4-dioxobutane acid substances with pronounced anti-inflammatory and analgesic activity and low toxicity.

This object is achieved by obtaining 4-(4-bromophenyl)-4-oxo-2-{[3-(etoxycarbonyl)-4,5-dietitian-2-yl]amino}-2 - butenova acid, which has anti-inflammatory and analgesic activity. The claimed compound 1 synthesized by the interaction of 4-(4-bromophenyl)-2,4-dioxaborinane acid ethyl ester, 2-amino-4,5-dimethylthiophene-3-carboxylic acid in the environment of ethanol at 60°C, followed by separation of the target product known methods according to the scheme:

An example of retrieving the connection 1. To a solution of 2.7 g (0.01 mol) of 4-(4-bromophenyl)-2,4-dioxaborinane acid in 20 ml of ethyl alcohol was added a solution of 1.85 g (0.01 mol) of ethyl ester of 2-amino-4,5-dimethylthiophene-3-carboxylic acid in 20 ml of the same solvent and incubated at room temperature for 24 hours. See the camping cooled to 0°C, the precipitation is filtered off and recrystallized from acetonitrile. Yield 2.00 g (92.17%). TPL 179-180°C. Found, %: C 49.35; N, 3.69; N, 3.22; 18.23; S 67.29; Br 18.23 C18H16BrNO5S. Calculated, %: 49.33; N, 3.68; N, 3.20; 18.25; S 67.32; Br 18.23. IR spectrum (operation 1201, vaseline oil, ν, cm-1): 3189.39 (NH), 1676.30 (COO). An NMR spectrum1N (Varian Mercury300 (300 MHz), DMSO-d6, GMDS, δ, ppm): of 1.33 (t, J 7.2 Hz, 3H, Me), are 2.19 (s, 3H, Me), 2,24 (s, 3H, Me), 4,33 (kV, J 7.2 Hz, 2H, CH2O), 6,47 (s, 1H, C=CH), 7,72 (d, J 8.7 Hz, 2H, arene.), the 7.43 (d, J 8.7 Hz, 2H, arene.), 12,71 (s, 1H, NH).

The compound obtained 1 represents a bright red crystalline substance, soluble in chloroform, toluene, acetone, insoluble in water and hexane.

Study of anti-inflammatory, analgesic activity and acute toxicity was performed in the research laboratory of BAS Science Institute of Perm state national research University

Acute toxicity (LD50(mg/ml) of the compound (1) was determined by the method Hendersen [Pershin GN. Methods experimental chemotherapy // M, P.100, 109-117 (1971)]. The compound (1) was administered intraperitoneally white mice weighing 16-18 g in the form of a suspension in 2% starch mucus. For the compounds (1) LD50is >1500 mg/kg

According to the classification of the toxicity of preparations of compound (1) belong to V class almost natox is cnyh drugs [Izmerov NF, Capocci I., Sidorov, K.K. Settings toxicometric industrial poisons. - M.: Medicine, 1977. - s].

Anti-inflammatory activity was studied on white Wistar rats weighing 170-200 g Antiexudative action of the compounds (I) were evaluated in a model of acute inflammatory swelling of the feet, caused by subplantar injection of 0.1 ml of 1% solution carragenin. The index action of the studied compounds, administered orally in a dose of 50 mg/kg in 2% solution of starch mucus, served as the amount of swelling of the legs, defined ecometrics. About the power antiexudative action judged by the degree of inhibition of the inflammatory response in % of control [Methodical recommendations on experimental preclinical study non-steroidal anti-inflammatory pharmacological substances. - M., 1982. - 17 S. Approved by the Pharmacological Committee of Ministry of health USSR 11 November 1992 Protocol No. 22]. Compared the effect with ortofen in the dose of 10 mg/kg [Neugodova VP, Zaichenko GV, Ryndin S.E. Toxicological evaluation voltaren // Pharmacologist and toxicologist. - 1986. V.49. No. 1. P.123].

Analgesic activity of compound (I studied in outbred mice weighing 18-22 g with test "hot plate" [Radell Z.O., Selitto J.J. A method for measurement of analgesic activity on inflamed tissue. // Arch. Intermat. Pharmacodun. Et ther. 1957. - Vol.11. No. 4 - S.409-419].

The investigated compounds were administered intraperitoneally in the form of 2% starch is mucus in a dose of 50 mg/kg for 0.5 h before the animals on the premises heated to 53.5°C metal plate. Measure of pain sensitivity was the duration of stay of the animal on the hot plate until the licking of the hind paws, measured in seconds.

The results of the tests are presented in table

Anti-inflammatory, analgesic activity and acute toxicity of compounds 1
ConnectionDose, mg/kgLD50mg/kg% inhibition* carragenine edemaThe latent period of the defensive reflex,
4 hours1.5 hours
Control--0,010,0
150>100044,029,5
Ortofen107461,026,2
*compared with control

As can be seen from the table the Itza, the inventive compound (1) exhibits a pronounced anti-inflammatory and analgesic activity and less toxic than the product comparison - ortofen. Therefore, the claimed compounds (I) may find application in medical practice as anti-inflammatory and analgesic drugs.

4-(4-Bromophenyl)-4-oxo-2-{[3-(etoxycarbonyl)-4,5-dietitian-2-yl]amino}-2 - butenova acid

possessing anti-inflammatory and analgesic activity.



 

Same patents:

FIELD: medicine, pharmaceutics.

SUBSTANCE: declared method refers to preparing 4-methyl-3-[2-(N-propylamino)propionylamino]thiophene-2-carboxylic acid methyl ether hydrochloride (articaine) which is implemented by a reaction of 3-(2-chloropropionyl)amino-4-methyl-2-methoxycarbonylthiophene and n-propylamine, transformation of the reaction product into an aqueous solution in the form of hydrochloride which is used to recover 4-methyl-3-[2-(N-propylamino)propionylamino]thiophene-2-carboxylic acid methyl ether hydrochloride by introducing sodium chloride in the amount to provide the concentration of the latter in the reaction mass within the range of 10.0 to 15.0%. The technical effect consists in the fact that there is developed the method for preparing high-yield and high-purity 4-methyl-3-[2-(N-propylamino)propionylamino]thiophene-2-carboxylic acid methyl ether hydrochloride.

EFFECT: prepared product is a local anaesthetic found a wide application in dentistry and surgical practice.

1 cl, 1 ex

FIELD: chemistry.

SUBSTANCE: invention relates to a method of producing 3-(2-chloropropionyl)amino-4-methyl-2-methoxycarbonylthiophene by acylation of 3-amino-4-methyl-2-methoxycarbonylthiophene with 2-chloropropionyl chloride through simultaneous addition to a reaction mixture containing 3-amino-4-methyl-2-methoxycarbonylthiophene, 2-chloropropionyl chloride and an alkaline component with relative speed which enables to maintain pH of the medium in aqueous phase in the range of 4.0-8.0.

EFFECT: preventing or minimising secondary reactions of alkaline hydrolysis of 2-chloropropionyl chloride during acylation of 3-(2-chloropropionyl)amino-4-methyl-2-methoxycarbonylthiophene and achieving high output and quality of the product, which is used in synthesis of biologically active compounds and is particularly a key intermediate product in synthesis of hydrochloride of methyl ether of 4-methyl-3-[2-(n-propylamin)propionylamino]thiophene-2-carboxylic acid - one of the best local anaesthetics, known as articaine or ultracaine.

1 cl, 1 ex

FIELD: medicine.

SUBSTANCE: invention refers to a compound of formula (I) or to its pharmaceutically acceptable salt: formula (I) wherein; R1 represents hydrogen; R2 represents phenyl, benzothienyl, benzofuranyl or the group -CH2CH2-phenyl; wherein R2 is optionally substituted by 1 or 2 substitutes optionally specified in F, O, Br, I, -CN, -NO2, -OR8, C1-C6alkyl and -N(R9)2; R4 represents phenyl substituted by 1 or 2 substitutes optionally specified in F, CI, Br, I, -CP3, -OH, -OR8 and C1-C6alkyl; each R8 is optionally specified in C1-C6alkyl; and each R9 is optionally specified in H and C1-C6alkyl. The invention also refers to a pharmaceutical composition for activity modulation of depot-controlled calcium channels (SOC-channels) containing such compounds.

EFFECT: there are produced new compounds and based pharmaceutical compositions which can find application in medicine for treating the diseases or conditions, such as rheumatoid arthritis, psoriasis, inflammatory intestinal disease, asthma and multiple sclerosis.

12 cl, 21 dwg, 1 tbl, 14 ex

FIELD: chemistry.

SUBSTANCE: invention relates to novel substituted cyclohexylmethyl derivatives, having serotonin, noradrenaline or opioid receptor inhibiting activity, optionally in form of cis- or trans-diastereomers or mixture thereof in form of bases or salts with physiologically compatible acids. In formula (1): R2 denotes H or OH; R1 and R2 together denote or =N-OH, R3 denotes a phenyl residue which is unsubstituted or monosubstituted with a halogen atom or a heteroaryl residue selected from a five-member sulphur-containing heteroaryl such as a thienyl residue or an unsubstituted phenyl residue bonded through a C1-C4alkyl group, R4 and R5 independently denote an unsubstituted C1-C3alkyl or R4 and R5 together denote (CH2)3-6, R8 denotes a linear saturated C1-C4 alkyl group bonded with an aryl, which is unsubstituted or monosubstituted with halogen atoms, R9 denotes a saturated C1-C8alkyl; values of radicals R1, m, n, R6, R7, R10-R13 are given in the claim. The invention also relates to methods of producing compounds of formula (I), a medicinal agent containing said compounds, use of compounds of formula (I) to prepare a medicinal agent for anaesthetic treatment during sharp, neuropathic or chronic pain and for treating depression, urinary incontinence, diarrhoea and alcoholism.

EFFECT: high efficiency of using the compounds.

32 cl, 501 ex, 21 tbl

FIELD: chemistry.

SUBSTANCE: invention relates to compounds of general formula

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EFFECT: obtaining compounds of formula (I), having fungicidal activity.

9 cl, 3 dwg, 255 ex

FIELD: chemistry.

SUBSTANCE: pharmaceutical compositions containing at least one compound of formula (IIIa) or (IIIb) or (IVa) or (IVb), where -X- and Y are described in the claims, or pharmaceutically acceptable salts, esters or amides thereof and a pharmaceutically acceptable carrier, which can be used in processes with modulation or E- and P-selectin expression.

EFFECT: obtaining low-molecular non-glycoside and non-peptide compounds, capable of creating antagonism to selectin-mediated processes.

11 cl, 38 ex, 3 tbl

FIELD: chemistry.

SUBSTANCE: invention relates to compounds of formulae (1) and (2), where R1 is H or alkyl with 1-6 carbon atoms, R2 is H, alkyl with 1-6 carbon atoms or R1 and R2 together with a nitrogen atom form a saturated or unsaturated 5-, 6- or 7-member ring which can also include one or two heteroatoms independently selected from N, O or S. Said 5-, 6- or 7-member ring is possibly substituted with one or two OH groups or halogen groups, and said 5-, 6- or 7-member ring is possibly condensed with an aromatic or non-aromatic 5- or 6-member ring; R3 is independently selected from H, alkyl with 1-20 carbon atoms, cycloalkyl with 3-6 carbon atoms, phenyl or phenyl-alkyl, where the alkyl group has 1-4 carbon atoms, phenyl(hydroxy)alkyl, where the alkyl group has 1-4 carbon atoms, wherein said phenyl groups are possibly substituted with 1-3 groups independently selected from a group comprising halogen, alkyl with 1-6 carbon atoms, alkoxy with 1-6 carbon atoms, or R3 is CO-R7 or CO-O-R7, where R7 is H, alkyl with 1-20 carbon atoms, optionally substituted with a NH2 group or NH-CO alkyl group, where the alkyl group has 1-6 carbon atoms, phenyl or phenyl-alkyl, where the alkyl group has 1-4 carbon atoms, wherein said phenyl groups are possibly substituted with 1-3 groups independently selected from a group comprising halogen, alkyl with 1-6 carbon atoms, alkoxy with 1-6 carbon atoms, is H, alkyl with 1-6 carbon atoms or CO-R8, where R8 is alkyl with 1-6 carbon atoms; wavy lines denote bonds with carbon atoms, having an R or S configuration; dotted lines denote a bond or absence of a bond provided that the ring containing dotted lines is aromatic; m, n and q are whole numbers independently selected from 0, 1, 2 or 3, provided that the sum of m, n and q equals 2 or 3; s equals 0 or 1; W, X and Y independently denote CH, CR5, CR6 or a heteroatom independently selected from N, O and S, and R5 and R6 are independently selected from H, halogen, alkyl with 1-6 carbon atoms, halogen-substituted alkyl with 1-6 carbon atoms, alkoxy with 1-6 carbon atoms and thioxy with 1-3 carbon atoms, phenyl, or R5 and R6 together with atoms to which they are bonded form a carbocyclic ring which has 6 atoms in the ring, or a heterocyclic ring which has 5 or 6 atoms in the ring and 1-3 heteroatoms independently selected from N, O and S. Said carbocyclic or heterocyclic ring, formed jointly by R5 and R6, is possibly substituted with 1-6 R9 groups, where R9 is a halogen.

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65 cl, 1 tbl, 256 ex

FIELD: chemistry.

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6 cl, 56 tbl, 231 ex

FIELD: medicine, pharmaceutics.

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23 cl, 3 tbl, 89 ex

FIELD: chemistry.

SUBSTANCE: invention describes N-cycloalkylbenzylamide derivatives of formula

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11 cl, 5 ex

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention refers to organic chemistry, namely a new biologically active compound of indazole: 3-(3,4-dimethoxyphenyl)-4,5,6,7-tetahydroindazole hydrochloride (I) having formula presented above. The declared compound exhibit analgesic activity, twice less than Analgin and having higher action level. Furthermore, it exhibits high bacteriostatic activity on Staphylococcus aureus (3.8 mg/ml) and manifested bacteriostatic activity on Staphylococcus epidermidis (15.6-31.2 g/ml), Staphylococcus saprophyticus (250 mcg/ml) and the fungus Candida albicans (500-1000 mcg/ml) as well as bactericidal activity on these three species of staphylococci (62.5, 500 and 1000 mcg/ml respectively), having higher action level than phenyl salicylate. The compound (I) is referred to low-toxic (LD50=1500 mg/kg).

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3 cl, 2 tbl, 2 ex

FIELD: medicine, pharmaceutics.

SUBSTANCE: present invention refers to organic chemistry, namely to new 1,2-dihydroquinoline derivatives of general formula , or to a pharmaceutically acceptable salt thereof, wherein R1 represents a lower alkyl group; R2 represents a hydrogen atom; each of R3 and R4 represents a lower alkyl group; R5 represents a lower alkyl group; R6 represents a halogen atom, a lower alkyl group, a lower alkoxy group, a nitro group; X represents -CO-, -C(O)NR8 - or -S(O)2-; each of R7 and/or R8 may be identical or different, and represents a hydrogen atom, a lower alkyl group, a lower alkenyl group, a lower cycloalkyl group, a phenyl or naphthyl group, a saturated or unsaturated monocyclic 5- or 6-member heterocyclyl with one or two heteroatoms specified in nitrogen, oxygen and sulphur atoms, and 3-5 carbon atoms in a cycle, a lower alkoxy group, a phenoxy group; provided R7 and/or R8 represent a lower alkyl group, a lower alkoxy group, the mentioned lower alkyl group and lower alkoxy group may contain one or three groups specified in a halogen atom, a phenyl group, an unsubstituted monocyclic 6-member heterocyclyl with one heteroatom specified in a nitrogen atom, and 5 carbon atoms in a cycle, a lower alkoxy group, and -NRaRb as a substitute (substitutes); provided R7 and/or R8 represent a phenyl group, a saturated or unsaturated monocyclic 5- or 6-member heterocyclyl with one or two heteroatoms specified in nitrogen, oxygen and sulphur atoms, and 3-5 carbon atoms in a cycle, a phenoxy group, the mentioned phenyl group, saturated or unsaturated monocyclic 5- or 6-member heterocyclyl with one or two heteroatoms specified in nitrogen, oxygen and sulphur atoms, and 3-5 carbon atoms in a cycle, phenoxy group may contain one or two groups specified in a halogen atom, a lower alkyl group, a halogen-substituted lower alkyl group, a phenyl group, a hydroxyl group, a lower alkoxy group, a halogen-substituted lower alkoxy group, a lower alkylthio group, a lower alkylcarbonyl group, a lower alkoxycarbonyl group, a lower alkylcarbonyloxy group, -NRaRb, a nitro group and a cyano group as a substitute (substitutes); Ra and Rb may be identical or different, and each of them represents a hydrogen atom, a lower alkyl group, a lower alkoxycarbonyl group; Y represents a lower alkylene group; Z represents an oxygen atom; p is equal to 2, provided p is equal to 2, R6 may be identical or different. The invention also relates to a pharmaceutical composition and a glucocorticoid receptor modulator of the compound of formula (1).

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7 cl, 1 tbl, 4 ex

FIELD: medicine, pharmaceutics.

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EFFECT: invention provides reduced spontaneous thrombocyte aggregation, inflammation inhibition by reducing histamine secretion, cell protection against neurotoxic actions of thrombin.

1 cl, 4 ex

FIELD: medicine, pharmaceutics.

SUBSTANCE: there are presented 3-(2',2'-dimethylpropanoylamino)-tetrahydropyridin-2-one , (S)-3-(2',2'-dimethylpropanoylamino)-tetrahydropyridin-2-one and pharmaceutical compositions prepared with using said compound or its isomer, as well as the use thereof for preparing a therapeutic agent for preventing or treating inflammatory conditions, and a related method of treating. What is shown is the advantage of the compounds as related to the other broad spectrum chemokine inhibitors (BSCI) on anti-inflammatory activity; it possesses the pharmacokinetic, toxicological properties and the pharmaceutical safety parameters: (S)-3-(2',2'-dimethylpropanoylamino)-tetra-hydropyridin-2-one is 5-25 times more active than (R)-isomer.

EFFECT: higher anti-inflammatory activity.

13 cl, 10 dwg, 9 tbl

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention relates to combined antipyretic drug in form of rectal suppositories. Drug contains paracetamol, dimedrol and papaverine hydrochloride as active components, and lipophilic suppository base Suppocire (Suppocire NA-15) as auxiliary substance, with the following component ratio in g per 1 suppository with 2.0 g weight: paracetamol 0.3-0.5; dimedrol 0.03-0.05; papaverine hydrochloride 0.03-0.05; Suppocire (Suppocire NA-15) - the remaining part (to 2.0 g).

EFFECT: increased efficiency of paracetamol suppositories as antipyretic drugs, with absence of narcotic and psychostimulating substances in their composition.

4 tbl, 2 ex

FIELD: medicine, pharmaceutics.

SUBSTANCE: present invention refers to new compounds of general formula I [X]n-Y-ZR1R2, wherein the radicals are specified in the description, effective as heparan sulphate-binding protein inhibitors. The invention also refers to a pharmaceutical or veterinary composition having heparan sulphate-binding protein inhibitory activity for preventing or treating a disorder in a mammal, and to the use of these compounds and compositions for antiangiogenic, antimetastatic, anti-inflammatory, antimicrobial, anticoagulant and/or antithrombotic therapy in a mammal.

EFFECT: preparing the new compounds of general formula I [X]n-Y-ZR1R2, wherein the radicals are specified in the description, effective as the heparan sulphate binding protein inhibitors.

10 cl, 31 ex, 11 tbl, 40 dwg

FIELD: medicine, pharmaceutics.

SUBSTANCE: present invention refers to an aminopropylidene derivative presented by formula wherein R1 and R2, which may be identical or different, represent hydrogen or a substitute specified in the following (a)-(c), provided the case of both representing hydrogen is excluded: (a) carbonyl substituted with hydroxy, alkoxy or hydroxy alkylamino, (b) carbonylalkyl substituted by hydroxy or alkoxy, and (c) acrylic acid including its alkyl ester, R3 and R4, which may be identical or different, represent hydrogen, alkyl which may be substituted by phenyl or cycloalkyl, or R3 and R4, which together form a heterocyclic ring with a nitrogen atom bound thereto, represent pyrrolidino, piperidino, which may be substituted by oxo or piperidino, piperazinyl substituted by alkyl or penyl, morpholino or thiomorpholino; A means oxo or is absento, B represents canbon or oxygen; one of X and Y represents carbon, while the other one represents sulphur, a part represented by a dash line represents a single bond or a double bond, and a wavy line represents a cys-form and/or a transform. Also, the invention refers to a pharmaceutical composition exhibiting histamine receptor antagonist activity on the basis of said compounds.

EFFECT: there are produced new compounds and pharmaceutical compositions thereof, which can be used in medicine for treating asthma, allergic rhinitis, pollen allergy, hives and atopic dermatitis.

10 cl, 12 tbl, 58 ex

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention refers to medicine, and concerns a pharmaceutical composition for treating skin diseases. The composition contains a combination of methylprednisolone aceponate and glycoceramides and a glycoceramide complex containing cholesterol in the amount of 1-3%, and phospholipids in the amount of 25-34%, and excipients. A method for preparing the composition consists in the fact that methylprednisolone aceponate is introduced into an emulsion base containing the glycoceramide complex in the form of a solution to form a coagulation structure.

EFFECT: new pharmaceutical composition is characterised by a wide spectrum of pharmacological properties, stability, uniform distribution of the active ingredients.

9 cl, 2 tbl

FIELD: medicine, pharmaceutics.

SUBSTANCE: present invention refers to a compound of formula (I) presented below wherein the radicals and symbols have the values presented in the patent claim, and/or to its racemate, enantiomer, diastereomers or its pharmaceutically acceptable salts and/or esters. The invention also refers to a method for preparing it, using it in preparing a drug preparation and to drug preparations containing the compound of formula (I).

EFFECT: compound of formula has analgesic action and may be used as an active compound for pain management.

20 cl, 3 tbl, 33 ex

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention refers to a compound having formula (I): wherein each of the groups R1, R2, R3 are independently H or C1-4 alkyl group or C2-4 acyl group; each of the groups R4 and R5 are independently H or the group of formula -SO3R6, wherein R6 is H or the C1-4 alkyl group or the C2-4 acyl group; provided at least one of the groups R4 and R5 is a group having formula -SO3R6, or a pharmaceutically acceptable salt thereof. The invention also refers to a method for preparing the specified compounds of formula (I) and a pharmaceutical composition possessing activity in the inhibition of IL-1 anti-inflammatory cytokines based on these compounds.

EFFECT: there are produced new compounds and pharmaceutical composition on their basis which can find application in medicine for treating an inflammatory or autoimmune condition.

17 cl, 4 dwg, 4 ex

Novel methods // 2484821

FIELD: medicine, pharmaceutics.

SUBSTANCE: there are presented: the use of aclidinium for preparing a medicine for treating or preventing a respiratory disease or condition in a patient by inhalation, wherein said patients showed no systemic antimuscarinic actions, where the patient suffers a condition or is susceptible thereto, which may be exacerbated by systemic antimuscarinic activity (versions), and a related method of treating or preventing.

EFFECT: invention provides local therapeutic action of aclidinium in lungs and has no significant systemic antimuscarinic action as it quickly hydrolysed in blood plasma, and its main metabolites are completely deprived of affinity to muscarinic receptors.

13 cl, 3 ex

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