Cyclopropane carboxylate ethers of purine analogues

FIELD: pharmacology.

SUBSTANCE: invention relates to new cyclopropane carboxylate esters of purine analogues of the formula (T) or pharmaceutically acceptable salts thereof, which can be used for treatment of herpesvirus infections. Herpesvirus infection is an infection caused by the herpes simplex virus, infection of herpes zoster, or cytomegalovirus infection. In the compound of the formula (T) each Rx and Rz is independently hydrogen or (C1-C6)alkyl, or Rx is hydrogen and Rz is (C1-C6)alkyl, or Rx is (C1-C6)alkyl and Rz is hydrogen; and Ry is (C1-C6)alkyl, halo (C1-C6)alkyl, C6aryl, haloC6aryl or (C4-C5)heteroaryl with one heteroatom selected from nitrogen and oxygen in the ring.

EFFECT: increased efficiency of compounds application.

7 cl, 5 dwg, 3 tbl, 16 ex



Same patents:

FIELD: chemistry.

SUBSTANCE: invention relates to a method of producing acyclovir 2/3 hydrate, which involves mixing acyclovir with water in weight ratio of 1:5-50, dissolving at 50-100°C, filtering, cooling the filtrate at 0-30° to deposit crystals, collecting crystals by filtering and drying the crystals at 0-150°C for 0.5-24 hours to obtain acyclovir 2/3 hydrate having a stable crystalline structure.

EFFECT: preparation process is simple and suitable for industrial production.

10 cl, 4 dwg, 1 tbl, 15 ex

FIELD: medicine, pharmaceutics.

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


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

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

8 cl, 2 tbl, 264 ex

FIELD: chemistry.

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

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

15 cl, 6 tbl

FIELD: chemistry.

SUBSTANCE: present invention relates to novel compounds - 9-substituted derivatives of 8-oxoadenine of general formula (I) and their pharmaceutically acceptable salts having interferon-inducing effect on viruses. In general formula (I): , ring A is phenyl; n equals 0; Z1 is a C1-C4alkylene group which is not substituted or substituted with a hydroxyl group; X2 is an oxygen atom, a sulphur atom, SO2, NR5, SO2NR5, NR5SO2 or NHCONH (in which R5 is a hydrogen atom, a substituted or unsubstituted C1-C6alkyl group, where the substitutes are selected from a hydroxyl group, C1-C6-alkoxy group, amino, C1-C6-alkylamino, di- C1-C6-alkylamino, 5-6-member saturated cycloamine group containing 1-2 nitrogen atoms, possibly containing an extra oxygen atom and possibly substituted with an oxo-group, and a tetrazolyl group); Y1, Y2 and Y3 each independently denotes a single bond or a C1-C4-alkylene group; X is an oxygen atom; R2 is a hydrogen atom, a C1-C4-alkyl group optionally substituted with an amino group, a C1-C6-alkylamino group or a di- C1-C6-alkylamino group and R1 is a hydrogen atom.

EFFECT: obtaining novel compounds which can be used as an antiviral or antiallergic agent.

14 cl, 32 tbl, 51 ex

FIELD: chemistry.

SUBSTANCE: invention relates to a novel improved method of producing entecavir of formula (I) which has antiviral effect for possible use in a medicinal agent with low content of the active component, for example in treating hepatitis B. The invention also relates to novel intermediate products and their methods of production. The entecavir has general formula (I) . Its method of production involves subjecting a compound of formula 7c or its mixture with a compound of formula 8a, where Rb is C1-C4alkyl, to oxidation, mainly with a peroxidate, such as a sodium carbonate peroxidate, sodium pyrophosphate peroxidate etc. 7c + 8a. Compound of formula 7c or its mixture with a compound of formula 8a is obtained by bringing the compound of formula 7a into contact with at least one acid selected from halogenated methane-sulphonic acid and possibly methane-sulphonic acid, possibly in the presence of a compound of formula 8a, with subsequent treatment with at least one aqueous base. The invention also relates to production of compounds of formulae 7a and 8a.

EFFECT: increased antiviral effect of the compounds.

27 cl, 8 dwg, 19 ex

FIELD: organic chemistry, chemical technology, medicine, pharmacy.

SUBSTANCE: invention describes derivatives of 8-phenyl-6,9-dihydro[1,2,4]-triazolo[3,4-I]purine-5-one of the general formula:

wherein R1 means hydrogen atom, group -CH2-R6 wherein R6 means phenyl; R2 means (C1-C5)-alkyl or group -(CH2)n-R6 wherein n= 1 or 2; R6 means (C1-C4)-alkoxy-group or pyridyl group; R3 means (C1-C6)-alkyl; R4 means hydrogen atom or (C1-C4)-alkyl; R5 means -(CH2)n-R7 wherein n = 0-4; R7 means 3-7-membered ring comprising 1-3 heteroatoms taken among nitrogen atom (N) and oxygen atom (O), (C3-C7)-cycloalkyl or phenyl wherein indicated groups can be substituted with different substitutes; or R4 and R5 mean independently hydrogen atom (H), (C2-C6)-alkynyl or (C1-C6)-alkyl that can be substituted possibly; or R4 and R5 in common with nitrogen atom (N) form 4-7-membered ring comprising 1-2 heteroatoms taken among N and O and substituted possibly. Also, invention relates to their pharmaceutically acceptable salts, methods for preparing these compounds, intermediate substances, pharmaceutical composition and a to a method for treatment of different diseases mediated by activity of phosphodiesterase-5 (PDE-5). Described compounds of the formula (I) are inhibitor of PDE-5.

EFFECT: improved preparing method and treatment, valuable properties of compounds.

20 cl, 5 tbl, 149 ex

FIELD: medicine, pharmacy.

SUBSTANCE: invention relates to new acid-additive nitrate salts of compounds taken among salbutamol, cetirizine, loratidine, terfenadine, emedastine, ketotifen, nedocromil, ambroxol, dextrometorphan, dextrorphan, isoniazide, erythromycin and pyrazinamide. Indicated salts can be used for treatment of pathology of respiratory system and elicit an anti-allergic, anti-asthmatic effect and can be used in ophthalmology also. Indicated salts have less adverse effect on cardiovascular and/or gastroenteric systems as compared with their non-salt analogues. Also, invention proposes pharmaceutical compositions for preparing medicinal agents for treatment of pathology of respiratory system and comprising above indicated salts or nitrate salts of metronidazol or aciclovir.

EFFECT: improved and valuable properties of compounds.

6 cl, 5 tbl, 19 ex

New drug substances // 2237657
The invention relates to organic chemistry and can find application in medicine

New drugs // 2237057
The invention relates to organic chemistry and can find application in medicine

The invention relates to novel 2,6,9-triple-substituted purine derivative of General formula I, having the effect of selective inhibitors of kinases of the cell cycle, which can be used, for example, for the treatment of, for example, autoimmune diseases such as rheumatoid arthritis, systemic lupus erythematosus, diabetes type I, multiple sclerosis, and for the treatment of cancer, cardiovascular diseases such as restenosis, etc

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention relates to pharmaceutical industry and represents medication, possessing virucidal activity, for preventive and therapeutic treatment of viral infections, caused by virus of herpesviridae family, characterised by the fact that said medication contains pyroxican in carrier substance.

EFFECT: invention provides extension of arsenal of means, possessing virucidal activity.

7 cl

FIELD: medicine.

SUBSTANCE: treating an active form of Epstein-Barr viral infection in the children with an inactive HIV infection involves conducting high-active antiretroviral therapy accompanying administering inosin pranobex prescribed orally from the first day of treatment in a daily dose of 50 mg/kg of body weight, 3-4 times a day to make three courses of 10 days each, as well as using suppositories of interferon alpha-2b + taurine per rectum according to the schedule: for the first 10 days of treatment - one suppository two times a day - in the morning and in the evening, every 12 hours; further - one suppository at the bedtime every second day for three months. The method enables reducing a rate and an intensity of the Epstein-Barr viral infection symptoms by reducing the lymphocyte, blood plasma, oropharyngeal mucus Epstein-Barr virus content and improving the immunological status presented by normalising CD3+ lymphocyte, CD4+ lymphocyte, CD95+ lymphocyte, annexin-V+ lymphocyte, annexin-V+/propidium+ lymphocyte, CD19+ lymphocyte counts.

EFFECT: reducing the rate and intensity of symptoms.

2 tbl, 2 ex

FIELD: medicine.

SUBSTANCE: pharmaceutical composition contains a viral preparation containing types 1 and 2 herpes simplex viruses inactivated by formalin or gamma radiation, and an immunocompetent substance. The immunocompetent substance is presented by interferon and a combination of at least two independent amino acids in the following proportions: inactivated types 1 and 2 herpes simplex viruses - 5 mln of plaque-forming units per 1 ml of the suspension, interferon - 150-250 thousand International units/ml, amino acids - 0.27 mg/ml.

EFFECT: adding interferon to the composition as an adjuvant, and also a combination of two irreplaceable amino acids enables creating the high-effective herpes vaccine, preparing a based dosage form in the form of suppositories that makes the vaccine applicable in paediatric practice.

4 cl, 3 ex

FIELD: medicine.

SUBSTANCE: invention provides a stable composition for treating damages associated with herpes-virus infections in a form specified in creams and gels containing low-level trichloroacetic acid. The amount of trichloroacetic acid makes less than 6% (wt / wt) of the cream or gel.

EFFECT: extending the range of products for treating the damages associated with herpes-virus infections.

25 cl, 3 ex

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention refers to pharmaceutical industry and represents using sulphated hyaluronic acid for preparing a therapeutic agent for local administration for treating inflammatory/irritating skin diseases specified in dermatitis, atopic dermatitis, photocontact dermatitis, rash, vitiligo, eczema, psoriasis, all skin irritations related to activation of anti-inflammatory cytokines, such as IL-1, IL-2, IL-7, IL-8, IL-9 and TNF, wherein hyaluronic acid has a molecular weight falling within the ranges of 10000 D to 50000 D, 150000 D to 250000 D and 500000 D to 750000 D, and a sulphatation degree equal to 1.

EFFECT: invention provides stimulating the immune system protein synthesis for eliciting the immune response.

8 cl, 33 ex, 15 dwg, 3 tbl

FIELD: chemistry.

SUBSTANCE: invention relates to A-seco-triterpenoids of general formula (I) , where or , demonstrating inhibiting activity with respect to type I herpes simplex virus (HSV-1, strain 1C) and HIV-1. In addition, compounds (I) can be used as intermediates for other biologically active compounds.

EFFECT: increased efficiency of compound application.

2 cl, 1 tbl, 6 ex

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention refers to the pharmaceutical industry and represents a composition for the external treatment and prevention of infections caused by the type 1, 2 herpes virus and bacterial complications caused by the herpetic infection, containing lysozyme, peroxidase, povyargol as active ingredients, escin and glycyrrhizinic acid or its salts as anti-inflammatory ingredients, liposomes on the basis of high-active hydrated lecithin in a combination with cholesterol as carriers and pharmaceutically acceptable carriers and excipients, with the ingredients of the composition being taken in certain proportions, wt %.

EFFECT: invention provides extending the range of products for treating and preventing the infections caused by type 1, 2 herpes virus and bacterial complications caused by the herpetic infection.

4 ex, 1 tbl

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention refers to medicine, namely to using a polycarboxylic fullerene C60 derivative as a microbiocidal antiviral agent for the herpes simplex virus (HSV) and cytomegalovirus (CMV) inhibition. The polycarboxylic fullerene C60 derivative has the structural formula .

EFFECT: invention provides the agent for the emergency prevention of HSV and CMV sexual transmission.

7 dwg, 2 tbl, 5 ex

FIELD: medicine.

SUBSTANCE: invention refers to a method of treating recurrent skin and mucosal diseases caused by herpes simplex viruses type 1 and type 2 by coating a damaged region with a preparation containing a base including an active substance - (2,6-dichlorophenyl)amide carbopentoxysulphanic acid of the general formula: wherein X is Na, K, NH4, 2 times a day for 3-5 days, and if observing precursory symptoms, a repeated course of coating with the preparation is performed 1-2 times a day for 2-3 days.

EFFECT: invention provides higher clinical effectiveness in recurrent skin and mucosal diseases caused by herpes simplex viruses type one and type two.

2 cl, 4 ex

FIELD: medicine.

SUBSTANCE: invention represents a drug preparation for treating diseases caused by type 1 herpes simplex and cytomegalovirus, containing recombinant human interferon 2α, lisocyme, Licopid, carnitine 20%, vitamin E and a fatty base.

EFFECT: higher clinical effectiveness and reduced length of treatment, prolonged intercurrent periods, lower recurrent rate by prophylactic administration, reduced manifestation of neurotoxic effects of herpes viruses, lower administration of antibiotics for preventing bacterial complications in infectious-inflammatory diseases caused by herpes simplex virus and cytomegalovirus in children.

2 cl, 3 tbl

FIELD: medicine.

SUBSTANCE: what is presented is using H1.3 recombinant histone protein as an eukaryotic cell adenoviral transduction inhibitor. The invention can be used to producing drug preparations for the diseases related to adenoviral infection.

EFFECT: higher clinical effectiveness.

2 dwg, 1 tbl, 2 ex