Solid forms containing (+)-2-[1-(3-ethoxy-4-methoxyphenyl)-2-methylsulphonylethyl]-4-acetylaminoisoindoline-1, 3-dione, their compositions and use

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention refers to solid forms of (+)-2-[1-(3-ethoxy-4-methoxyphenyl)-2-methylsulphonylethyl]-4-acetylaminoisoindoline-1,3-dione of formula (I) inhibiting TNF-α or PDE4 production that enables using them in treating psoriasis.

EFFECT: producing an agent for treating psoriasis.

36 cl, 14 tbl, 33 dwg, 14 ex

 

The text descriptions are given in facsimile form.

1. Solid form, containing enantiomerically pure compound of formula (I)

which has a powder x-ray that contains peaks at approximately 8.1, 15,2, 17,4, 23,6 and 25.1 degrees 2θ.

2. Solid form according to claim 1, which has a curve of differential scanning calorimetry, containing an endothermic process with an initial temperature of approximately 155°C.

3. Solid form according to claim 1, which has a curve of thermogravimetric analysis, containing the mass loss of less than about 1% when heated from about 25°C. to about 140°C.

4. Solid form according to claim 1, which has a curve of thermogravimetric analysis, containing the mass loss of less than about 0.05% when heated from about 25°C. to about 140°C.

5. Solid form, containing enantiomerically pure compound of formula (I)

which has a powder x-ray that contains peaks at approximately 10.1, 13,5, 20.7 and 26.9 degrees 2θ.

6. Solid form according to claim 5, which has ochkovuyu x-rays, optionally containing peaks at approximately 12,4, 15,7, 18,1 and 24.7 degrees 2θ.

7. Solid form according to claim 5, which has a curve of differential scanning calorimetry, containing an endothermic process with an initial temperature of about 154°C.

8. Solid form according to claim 5, which has a curve of thermogravimetric analysis, containing the mass loss of less than about 1% when heated from about 25°C. to about 140°C.

9. Solid form according to claim 5, which has a curve of thermogravimetric analysis, containing the mass loss of less than approximately 0.25% when heated from about 25°C. to about 140°C.

10. Solid form according to claim 5, which shows an increase of mass less than about 1%, when exposed to increasing relative humidity from about 0% to about 95% relative humidity.

11. Solid form according to claim 5, which shows a weight increase of less than approximately 0.6%, when exposed to increasing relative humidity from about 0% to about 95% relative humidity.

12. Solid form according to claim 5, which is stable when exposed to approximately 40°C and about 75% relative humidity for about 4 weeks.

13. Solid form, containing enantiomerically pure is Obedinenie formula (I)

which has a powder x-ray that contains peaks at approximately 8,1, 8,6, the 15.6, 17.3 and 25.4 degrees 2θ.

14. Solid form according to item 13, which has a curve of differential scanning calorimetry, containing an endothermic process with an initial temperature of approximately 145°C.

15. Solid form according to item 13, which has a curve of thermogravimetric analysis, containing the mass loss of less than about 1% when heated from about 25°to about 180°C.

16. Solid form according to item 13, which has a curve of thermogravimetric analysis, containing the mass loss of less than approximately 0.1% when heated from about 25°to about 180°C.

17. Solid form according to item 13, which shows an increase of mass less than about 1%, when exposed to increasing relative humidity from about 0% to about 95% relative humidity.

18. Solid form according to item 13, which shows an increase of mass less than about 0.2%when exposed to increasing relative humidity from about 0% to about 95% relative humidity.

19. Pharmaceutical composition for inhibiting production of TNF-α or PDE4 containing solid form according to any one of claims 1 to 18 and a pharmaceutically acceptable rabbanites is, excipient or carrier.

20. Pharmaceutical composition for inhibiting production of TNF-α or PDE4, suitable for oral administration, contains from about 10 mg to about 200 mg of a solid form according to any one of claims 1 to 18 and a pharmaceutically acceptable diluent, excipient or carrier.

21. The pharmaceutical composition according to claim 20 containing from about 10 mg to about 100 mg of a solid form.

22. The pharmaceutical composition according to claim 20, where the pharmaceutical composition is presented in capsule form.

23. The pharmaceutical composition according to item 22, where the capsule contains approximately 10 mg of a solid form.

24. The pharmaceutical composition according to item 22, where the capsule contains approximately 20 mg of a solid form.

25. The pharmaceutical composition according to item 22, where the capsule contains about 25 mg of a solid form.

26. The pharmaceutical composition according to item 22, where the capsule contains approximately 50 mg of a solid form.

27. The pharmaceutical composition according to claim 20, where the pharmaceutical composition is presented in tablet form.

28. The pharmaceutical composition according to item 27, where the tablet contains about 10 mg of a solid form.

29. The pharmaceutical composition according to item 27, where the tablet contains about 20 mg of a solid form.

30. The pharmaceutical composition according to item 27, where the tablet sod is RIT approximately 25 mg of a solid form.

31. The pharmaceutical composition according to item 27, where the tablet contains about 50 mg of a solid form.

32. A method of treating psoriasis, comprising an introduction orally to a patient having psoriasis, solid form according to any one of claims 1 to 18 in therapeutically effective amounts, and where the solid form is administered in the form of tablets or capsules.

33. The method according to p, where the psoriasis is moderate to severe plaque psoriasis.

34. The method according to p, where the patient reaches 75% reduction on the scale of the Index area of the affected body surface and the intensity of the main symptoms of psoriasis (PASI) relative to the initial state.

35. The method according to p, where the patient reaches 90% reduction on the scale of the Index area of the affected body surface and the intensity of the main symptoms of psoriasis (PASI) relative to the initial state.

36. The method according to p, where the patient reaches 50% reduction on the scale of the Index area of the affected body surface and the intensity of the main symptoms of psoriasis (PASI) relative to the initial state.



 

Same patents:

FIELD: chemistry.

SUBSTANCE: present invention relates to a method of producing 1-cyclohexene-1,2-dicarboxylic acid derivatives of general formula I: where: R1, R2=H, CH3, C6H5; X=O, NH, which involves exposing a molten corresponding cyclohexane-1,2-dicarboxylic acid derivatives to bromine in the presence of a catalyst - carboxylic acid amide: N,N-dimethylformamide or N-methyl-2-pyrrolidone. Bromine in amount of 1.04-1.10 mol per 1 mol of starting compound is added to the molten corresponding cyclohexane-1,2-dicarboxylic acid derivative heated to 100-120°C, containing a catalyst in amount of 0.045-0.051 mol per 1 mol of starting compound, and then holding the reaction mass at 145-200°C.

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2 cl, 5 ex

FIELD: chemistry.

SUBSTANCE: invention relates to novel N-substituted imides of formulae I and II where n stands for 1; m stands for 1; R1 and R2, R4 and R5 together with adjacent group -CO-N-CO- form 5 or 6-member monocyclic ring, optionally saturated and probably substituted with C1-18alkyl, condensed ring system, which in addition to monocyclic core ring, determined above, contains one or two C6aromatic or C6aliphatic rings; R3 stands for NR12R13, where R12 and R13 independently on each other represent C1-18alkyl, C5-12cycloalkyl, each of which can be substituted with C1-4alkyl; R6 represents C6-10aryl, C1-18alkyl, C6-10ar-C1-C18alkyl, C5-C12cycloalkyl, each of which is optionally substituted with C1-C4alkyl; R7 represents C1-C18alkyl, C6-C10aryl, C6-C10ar-C1-C18alkyl, C5-C12cycloalkyl, each of which is optionally substituted with C1-C4alkyl.

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8 cl, 12 ex

FIELD: pharmacology.

SUBSTANCE: invention concerns novel compounds of formula (1a) or (1b) or their pharmaceutically acceptable salts with inhibition effect on matrix metalloproteinases (MMP). In formula

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13 cl, 18 ex

FIELD: chemistry, pharmacology.

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15 cl, 68 ex, 12 tbl

FIELD: chemistry.

SUBSTANCE: invention relates to production of phthalamide N-thyoderivatives which are efficient inhibitors for rubber. The method of producing N-(chrolalyklthyo)phthalamide of structural formula , where R is alkyl, arylalkyl, cycloalkyl, is effected via interaction of imidining agent with monochloride sulphur with subsequent chlorination of the stock by gaseous chlorine. Unsaturated compounds with one or several double bonds are coupled with produced chlorthyo-N-phthalamide in the medium of the solvent, i.e. chlorinated aromatic or aliphatic hydrocarbons. Potassium phthalamide is used as an imidining agent, while the interaction of chrolthyo-N-phthalamide with unsaturated compounds is effected in the presence of catalyst, i.e. aluminium or iron chloride. Target phthalamide N-thyoderivatives are extracted by vacuum azeotropic distillation in the presence of surfactant added in the amount of not over 0.33% relative to the weight of water added to form azeotrop.

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5 cl, 4 tbl, 46 ex

FIELD: chemistry.

SUBSTANCE: invention relates to extraction of M-(chloralkylthyo)phthalimides, which are efficient anti-scorchers for synthetic and natural rubber. N-(chloralkylthyo)phthalimide is extracted from the mix with phenyl chloride by distillation of the latter. The distillation is effected in vacuum in azeotropy with water in the presence of surfactant in the amount of not over 0.33% relative to added water volume.

EFFECT: increase in vacuum azeotropic distillation intensity and higher power saving.

3 tbl, 30 ex

FIELD: organic chemistry, biochemistry, medicine, virology.

SUBSTANCE: invention relates to a compound of the general formula: (R1)-(R2)-N-CH-(CH=CH2)-CH2R3 wherein R1 represents alkoxycarbonyl, arylalkoxycarbonyl, aryloxycarbonyl, benzoyloxycarbonyl; R2 represents hydrogen atom (H), or R1 and R2 in common with nitrogen atom to which they are joined form phthalimido, succinimido or N-diformyl group; R3 represents thioalkyl or thioaryl. Also, invention relates to a method for synthesis of compounds represented by the formula (8): that involves the following steps: (a) treatment of hydroxybutene of the formula (6): with methanesulfonyl chloride in the presence of an amine base in a polar aprotonic solvent to obtain butene mesylate of the formula (7a): wherein R' represents alkyl or aryl, and (b) treatment of butene mesylate (7a) with thiophene oxide wherein thiphene is formed in situ using thiophenol and non-nucleophilic base in polar aprotonic solvent to obtain thiophenylbutene (8). Also, invention relates to a method for stereoselective conversion of compound of the formula (8) to compound of the formula (9): or the formula (10): wherein this method involves treatment of compound of the formula (8) with osmium-containing oxidizing combination of reagents: K2OsO2(OH)4/K3Fe(CN)6, K2CO3, NaHCO3 and CH3SO2NH2 in the presence of DHQD2PHAL as a chiral accessory reagent to obtain compound represented by he formula (9) or the formula (10). Invention provides synthesis of butene and butane compounds that are useful as intermediate compound in synthesis of nelfinavir mesylate relating to a protease inhibitor.

EFFECT: improved methods of synthesis.

8 cl, 8 ex

FIELD: organic chemistry, medicine, biochemistry, pharmacy.

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EFFECT: valuable medicinal and biochemical properties of compounds.

14 cl, 4 sch, 1 tbl, 53 ex

FIELD: organic chemistry, dyes.

SUBSTANCE: invention relates to the dispersed dyes comprising N-methylphthalimide-diazo-component and a coupling aniline component. Invention proposes a dye of the formula (1): wherein R means hydrogen or bromine atom; R1 means hydrogen atom, methyl or -NHCO-(C1-C4)-alkyl; R2 means (C1-C4)-alkyl substituted with (C1-C4)-alkoxy-group; R3 has any value among R2 being independently of R2. Invention proposes a mixture of dyes comprising at least one azo dye of the formula (1) and at least one azo dye of the formula (4): wherein R1 means hydrogen atom, methyl or -NHCO-(C1-C4)-alkyl; R2 means (C1-C4)-alkyl wherein is possible but not obligatory that C2-alkyl chain or comprising more carbon atoms is broken with oxygen atom, and R has any value of R being independently of R2. Also, invention proposes a method for coloring or printing on semisynthetic or synthetic hydrophobic fibrous materials wherein dye of the formula (1) or mixture of dyes of formulae (1) and (4) is applied on such materials or added in them. Invention proposes dispersed dyes providing coloring characterizing by high strength degree in laundry and against sweat.

EFFECT: valuable properties of dyes.

7 cl, 2 tbl, 3 ex

FIELD: organic chemistry, chemical technology.

SUBSTANCE: invention relates to chemistry of adamantine derivatives, namely, to a method for preparing N-phthalimidoalkyladamantane or its derivatives of the general formula: wherein X means a single bond; R1 means hydrogen atom (H); R means C6H5, C6H4COOC2H5; R1 means CH3; R means CH3; R1 means COOC2H5; R means CH2CH2SCH3, (CH2)3CH3; X means CH2CH2; R1 = R means COOC2H5; X, R1 mean ; R means COOC2H5 that represent important intermediate products in synthesis of biologically active substances. Method is carried out by adding corresponding N-phthalimidoalkyl or its derivative to a derivative of adamantine. 1,3-Dehydroadamantane is used as a derivative of adamantine, and the following compounds are used as N-phthalimidoalkyl or its derivative: N-benzylphthalimide, N-isopropylphthalimide, ethyl esters of N-phthalyl-D,L-methionine, N-phthalyl-D,L-norleucine, N-phthalyl-4-aminomethyl-1-benzoic acid, N-phthalyl-4-aminocyclohexane 1-carboxylic acid, 2-(N-phthalimido)-ethylmalonic acid ethyl ester. Process is carried out in the mole ratios of reagents = 1:(2-3), respectively, in inert solvent medium, at temperature 80-120oC for 4-6 h.

EFFECT: improved preparing method, enhanced yield of end compounds.

7 ex

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention refers to chemical-pharmaceutical industry and represents a pharmaceutical composition for local application containing fusidic acid within the range of 1 wt % to 5 wt % and mometasone within the range of 0.05 wt % to 2 wt % and a pharmaceutically acceptable carrier to be applied in treating or preventing inflammatory dermatoses caused by a secondary bacterial infection in a patient.

EFFECT: invention provides effective elimination of secondary bacterial infections in dermatologic injuries.

11 cl, 8 ex, 6 tbl

FIELD: medicine, pharmaceutics.

SUBSTANCE: present invention refers to new compounds of formula (I) and its pharmaceutically acceptable salts possessing dihydroorotate dehydrogenase inhibitory ability, to a based pharmaceutical composition, to application thereof in preparing a drug compound and to a combined preparation containing the presented compounds and the other active compound (I) in effective amounts wherein both groups G1 mean CRC, G2 mean a nitrogen atom or group CRd, of the groups G3 and G4 mean a nitrogen atom and the other one means group CH, M means a hydrogen atom or a pharmaceutically acceptable cation, while R1, R2, Ra, Rb, Rc and Rd have the values specified in the patent claim.

EFFECT: preparing pharmaceutically acceptable salts possessing dihydroorotate dehydrogenase inhibitory ability.

25 cl, 115 ex, 2 tbl

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention relates to method of obtaining said salts, to pharmaceutical composition, containing said salts, and to application of salt for preparation of medication for treatment, prevention or relief of one or several symptoms of disease, mediated by CRTH2, associated with eosinophils, basophils, where disease is selected from asthma, allergic asthma, asthma of physical effort, allergic rhinitis, atopic dermatitis, contact hypersensitivity and hyper IgE syndrome.

EFFECT: invention relates to novel pharmaceutically acceptable salts, containing pharmaceutically acceptable amine, selected from ethylenediamine, piperazine, benzathine or choline and {4,6-bis(dimethylamino)-2-(4-(4-(trifluoromethyl)benzamido)benzyl)pyrimidin-5yl}acetic acid.

43 cl, 21 dwg, 4 tbl, 6 ex

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention relates to novel crystalline forms I, II and amorphous form of {4,6-bis(dimethylamino)-2-(4-(4-(trifluoromethyl)benzamido)benzyl)pyrimidin-5-yl}acetic acid.

EFFECT: invention relates to pharmaceutical composition, containing crystalline form I of compound and to application of crystalline form I for treatment, prevention or relief of one or more symptoms of disease, mediated by CRTH2, associated with eosinophils, basophils, where disease is selected from asthma, allergic asthma, asthma, induced by physical effort, allergic rhinitis, perennial allergic rhinitis, seasonal allergic rhinitis, atopic dermatitis, contact hypersensitivity.

16 cl, 11 dwg, 8 tbl,11 ex

FIELD: medicine.

SUBSTANCE: what is described is a composition for topical application which contains a continuous phase and at least one disperse phase with said composition containing at least one polyaphron dispersion, at least one vitamin D or vitamin D analogue.

EFFECT: composition is characterised by better skin penetration or better stability.

27 cl, 3 dwg, 17 ex

FIELD: medicine.

SUBSTANCE: method of treating psoriasis. The invention refers to medicine, specifically to dermatology, and may be used for treating the patients suffering psoriasis. That is ensured by conducting detoxification, hyposensitising therapy, prescribing antihistamine preparations, vitamins, cytostatics, physiotherapeutic therapy, ointment applications. The conducted therapy is combined with additionally prescribed oral 40% alcoholate (1:10) containing herbal phytoecdysteroids in mass fractions 50 drops 3 times a day 15 minutes before meal daily for 30 days: Rhaponticum carthamoides roots and rhinzomes - 3, pot marigold blossom - 1, wild camomile blossom - 1.

EFFECT: method enabled considerably improved therapeutic effect in the patients due to evident immunomodulating, adaptogenic, sedative and anti-inflammatory effects of herbal phytoecdysteroids.

2 ex

FIELD: medicine.

SUBSTANCE: invention relates to medicine, namely to dermatology and can be applied for external treatment of psoriatic onychodystrophy. For this purpose mixture of gel tisol and ointment daivonex is applied on nidus of affection in ratio 1:2 with following keeping under adhesive plaster during 8-10 h two times per day. Course of treatment constitutes not less than 14 days.

EFFECT: method ensures reduction of treatment terms and duration of remission and obtaining high therapeutic effect.

1 tbl, 2 ex

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention relates to chemical-pharmaceutical industry, and concerns preparing an agent for treating various dermatopathies: psoriasis, eczema, atopic dermatitis, ulcers incl. trophic and other diseases accompanied by inflammation or skin flaking. According to the first version, the composition contains ethoxylated alcohol, glycerol monostearate, higher fatty alcohols C16-C18 and cocoglycerides, as well as glycerol, olive oil and water. According to the other versions, it contains naphthalan oil or pentoxifylline or urea. All the versions provide a liposomal form of the composition improving healing, soothing and trophic effects.

EFFECT: composition is hypoallergic, easy-to-use.

12 cl, 8 ex

FIELD: medicine, pharmaceutics.

SUBSTANCE: present invention refers to new benzimidazole derivatives of general formula (I) or to its pharmacologically acceptable salts wherein R1 represents a C6-aryl group which can be substituted by 1-3 groups optionally specified in a group of substitutes (a), or a heterocyclic group which represents pyridyl, dihydrobenzofuranyl, 1,3-benzodioxolyl, tetrahydropyranyl, tetrahydrofuranyl which can be substituted by 1-3 groups optionally specified in a group of substitutes (a), R2 represents a C1-C6 alkyl group, R3 represents a C6-aryl group which can be substituted by 1-2 groups optionally specified in a group of substitutes (a), Q represents a group represented by formula =CH-, or a nitrogen atom and a group of substitutes (a) represents a group consisting of a halogen atom, a C1-C6 alkyl group, a C1-C6 halogenated alkyl group, a carboxyl group, a C2-C7 alkylcarbonyl group, a C2-C7 alkoxycarbonyl group, a C1-C6 alkoxy group, a C1-C6 halogenated alkoxy group, an amino group, a 4-morpholinyl group and a di-C1-C6 alkyl)amino group. Also, the invention refers to a pharmaceutical composition based on a compound of formula (I), to a PPARγ activator/modulator based on the compound of formula (I), to using the compound of formula (I), to a method of reducing blood glucose, to a method of activating PPARγ, a method of treating and/or preventing said pathological conditions.

EFFECT: there are produced new benzimidazole derivatives showing PPARγ modulatory activity.

41 cl, 2 dwg, 6 tbl, 76 ex

FIELD: chemistry.

SUBSTANCE: invention describes a novel useful vitamin D3 derivative, which has excellent vitamin D3 activity, and has relatively low action on system calcium metabolism compared to other traditional vitamin D3 derivatives. The invention includes a 9,10-secopregnane derivative of general formula [1] and a pharmaceutical composition containing said derivative as an active ingredient. [Formula 1]

.

In general formula [1], the next part of the structure between position 16 and position 17 denotes a single bond or a double bond. Y denotes a single bond, alkylene, alkenylene or phenylene; R1 and R2 are identical or different and each denotes hydrogen, alkyl or cycloalkyl; or R1 and R2, taken together with an adjacent carbon atom, form a cycloalkyl; R3 denotes hydrogen or methyl; Z denotes hydrogen, hydroxy or -NR11R12, where R11 and R12 assume values given in the claim.

EFFECT: obtaining a useful D3 derivative.

14 cl, 73 ex, 8 tbl

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention refers to medicine and pharmacology, namely a drug preparation inducing alpha and beta interferon, and may be used for treating acute respiratory viral infections (ARVI). The agent represents 5-hydroxy-4-dimethylaminomethyl-1-cyclohexyl-2methyl-3-ethyloxycarbonylindole hydrochloride.

EFFECT: invention provides intensified antiviral action.

13 tbl

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