Method of conservative treatment of children with renal dysplasia
(57) Abstract:The invention relates to medicine, namely to methods of conservative treatment of children with renal dysplasia. For this child along with the traditional comprehensive therapy to introduce thiotriazoline 0.05-0.1 g 2 times a day for 12-16 days. The method allows to increase the efficiency of treatment of renal dysplasia in children and to reduce the treatment time due to the anti-ischemic, membrane stabilizing, antioxidant and immunomodulatory activity thiotriazoline. 1 C.p. f-crystals, 2 tab. The invention relates to medicine and can be used in clinic for the treatment of dysplastic forms of congenital abnormalities in children.Known by the author's certificate N 1143422, class A 61 K 31/71. B. I. N 9, 1989 , page 24 a method of treating acute renal failure in the initial period using minicola, heparin and lasixa.The disadvantage of this method is that it is virtually ineffective in dysplastic forms of congenital abnormalities in children.A known method according to the author's certificate N 1794456, B. I. N 6, 1993 , page 21. and the patent of Ukraine N 2011, class A 61 M 19/00 treatment CLASS="ptx2">This method activates the kidneys, but is unsuitable for the treatment of dysplastic forms of congenital development of the kidneys. Renal dysplasia significant role in the pathogenesis belongs activation of free-radical oxidation (CPO), excessive accumulation of lipid peroxides and the associated process to reduce the activity of the antioxidant system, resulting in functional and structural disturbance of the cell membrane of the nephron.The known method of conservative treatment of renal dysplasia in children with the use of antioxidant tools, in particular - tocopherol, in complex with pyridoxal phosphate, califona, Citycom, piracetam, nifedipine, nicotinic acid and gentamicin (I. C. Kazan, dis. for the degree of doctor honey. Sciences, M, 1987, ch. VII, pp. 283-298).This method was adopted for the prototype.Application in complex treatment of patients with dysplastic forms of congenital malformations of the kidney-tocopherol can improve the results of treatment at 31-32% of patients.Patent Foundation from 1975 to 1996, methods of complex treatment of dysplastic forms of congenital abnormalities not detected.The basis from the dysplasia.This object is achieved in the way of conservative treatment in children with renal dysplasia due to the use in the treatment of antioxidant "Thiotriazoline" greatly retarding the process of lipid peroxidation, for example, in the form of tablets of 0.05-0.1 g, depending on age twice a day for 12-16 days.Research patent and medical information to confirm the novelty of the present combination of features, therefore, the novelty of the proposed method meets the criteria of the invention.The invention is illustrated below by the description.Thiotriazoline as synthetic hepatoprotective, cardioprotective drug that has anti-ischemic, membrane stabilizing, antioxidant and immunomoduliruushimi activity registered 31.05.94, by the order of Ministry of health of Ukraine N 85, registration N 94/85/1 and approved for serial production and use in clinical practice. By the same order in N 94/85/2 and N 94/85/3 and N 94/85/4 registered 1% and 2.5% solution for injections and pills to 0.1 gFor the treatment of children by the proposed method is most convenient to use pills.In accordance with and is 7 years old and 0.1 g after 7 years for 14 days. Such courses may be several during the year depending on the type and prevalence of dysplastic processes.In combination with thiotriazoline, which is an antioxidant, children are pyridoxalphosphate, Califon, ziemak, piracetam, nifedipine, nicotinic acid, gentamicin, quantitative volume, as and when used as an antioxidant-tocopherol, is determined depending on the age of the child and diagnostic results. It is possible to replace the complex of some other drugs, exclusion or addition of other drugs.The course of treatment is 14 days, although the treatment effect is achieved on the fifth day and finally stabilizes after 12-14 days.Therefore, the extension of treatment for more than 16 days is impractical. The above-described method was tested in the clinic of pediatric surgery on the basis of the 5th multidisciplinary clinical children's hospital, Zaporozhye with positive results, confirming the efficiency of treatment in two times in comparison with the use of a - tocopherol. Course purpose thiotriazoline with dysplastic forms of congenital abnormalities has led to the reduction of free-radical oxidation is Anttonen (TC) 64.7%, malondialdehyde (MDA) 44.6%, increased-tocopherol on 144, 0mm% (P < 0,02),indicating a significant inhibition of the processes of lipid peroxidation.To compare the effectiveness of treatment using the methods of the prototype and the proposed method were compared to the results of the treatment of the main group of children /34/ who thiotriazoline and the control groups /34/ who-tocopherol. The course of treatment for each group of 14 days. The results are shown in table. 1 - change indicators SRO and table. 2 - change the clinical and laboratory parameters.As shown in clinical studies, the use of thiotriazoline in the complex treatment of 34 patients with dysplastic forms of congenital malformations of the kidneys, can improve the results of treatment in 61.8% of patients of the main group compared to 31.2% of patients in the control group treated with a-tocopherol, i.e., the efficiency increased almost twice.As can be seen from the table. 2, in children who received the combined therapy with the inclusion of thiotriazoline significantly faster stoped bladder pain syndrome, normalized body temperature, appetite improved, and disappeared weakness, malaise.Image the history of the disease N 1304, was hospitalized with a diagnosis of abnormality of the urinary system (MVS), hypoplastic right kidney, corticomedullary segmental dysplasia of the right kidney, chronic pyelonephritis. At admission were noted marked changes in the urine in the form of bacteriuria and pyuria, dull pain in the right lumbar region, the rise in body temperature to 37.8 DK - of 1.88 μm/ml, TC - of 0.53 μm/ml, MDA - 0,88 μm/ml-TF - 0,90 µm/mlThe patient received: thiotriazoline (PL. 0.05 x 2 times a day) for 14 days, pyridoxal phosphate, Califon, ziemak, piracetam, nifedipine, nicotinic acid, gentamicin. According to the statement, the condition is satisfactory, no complaints. Clinical laboratory values within normal limits. DK - 1.00 micron/ml, TC - 0,32 μm/ml, MDA - 0,65 µm/ml, MDA - 0,65 µm/ml-TF - 2,03 μm/ml 1. Method of conservative treatment of children with renal dysplasia, including traditional complex therapy, characterized in that it further child enter thiotriazoline 0.05 - 0.1 g 2 times a day for 12 to 16 days.2. The method according to p. 1, characterized in that the thiotriazoline administered in pill form.
FIELD: organic chemistry, pharmaceutical compositions.
SUBSTANCE: 5-aryl-1H-1,2,4-triazole derivatives of general formula I
, pharmaceutically acceptable salts thereof or pharmaceutical composition containing the same are described. In formula R1 is C1-C6-alkyl, C1-C6-haloalkyl or phenyl; R2 is C3-C8-cycloalkyl; phenyl optionally substituted with one or more substituents selected from C1-C4-alkyl; halogen, hydroxyl, C1-C4-alkoxy, nitro, di-(C1-C4)-alkylamino, C1-C4-alkylsulphonyl, C1-C4- alkylsulphonylamino, and methylenedioxy; phenyl-(C1-C4)-alkyl, wherein phenyl is substituted with C1-C4-alkoxy; or pyridil. New compounds are effective and selective cyclooxygenase-2 (COX-2) inhibitors and useful in treatment of inflammations.
EFFECT: new compounds for inflammation treatment.
10 cl, 36 ex, 1 tbl
FIELD: medicine, dermatology.
SUBSTANCE: invention proposes an anti-infectious preparation comprising the combination of active substances with topical and systemic antifungal agents and a water-insoluble film-forming agent. The systemic antifungal agent is taken among the group including intraconazole, terbinafine and fluconazole or their salts. The topical antifungal agent is taken among the group including ciclopirox, 6-(2,4,4-trimethylpentyl)-1-hydroxy-4-methyl-2(1H)-pyridone, amorolfine and butenafine or their salts. The preparation is used as lacquer for nails in therapy of onychomycosis. The lacquer preparation provides high concentration of systemic antifungal agents in nails after its topical applying. The significant advantage of the preparation involves short time in treatment of anychomycosis.
EFFECT: enhanced effectiveness and valuable medicinal properties of preparation.
6 cl, 6 ex
FIELD: medicine, gynecology, surgery.
SUBSTANCE: one should introduce 3.5%-chitosan ascorbate gel into fistulous channel that contains metronidasol at the dosage of 2 mg/ml, at the volume up to 20 ml once/2 d till complete fistula's closing. The present innovation enables to activate reparative processes and fistulous epithelization that favors for closing fistulous channel in earlier terms.
EFFECT: higher efficiency of therapy conducted.
FIELD: medicine, chemical-pharmaceutical industry, pharmacy.
SUBSTANCE: invention relates to a cerebral protective and stress-protective medicinal agent. Agent comprises an active base as a mixture thiotriazoline with piracetam and water for injection as a forming component. The proposed medicinal agent shows the enhanced bioavailability of active medicinal components, and it shows the cerebral protecting, stress-protective and anti-amnestic effect also.
EFFECT: valuable properties of agent.
SUBSTANCE: method involves administering drugs usable for hindering keratoleukoma occurring after carrying out excimer laser keratectomy with an antioxidant agent being added. The agent is used for jet irrigating cornea before setting lens.
EFFECT: enhanced effectiveness in reducing lipid peroxidation products quantity; accelerated cornea epithelialization.
2 cl, 2 tbl
FIELD: organic chemistry, medicine, biochemistry, pharmacy.
SUBSTANCE: invention describes derivatives of substituted triazoldiamine of the formula (I): wherein R1 represents (C1-C4)-alkyl, phenyl possibly substituted with halogen atom, amino-group substituted with -SO2-(C1-C4)-alkyl, imidazolyl, 1,2,4-triazolyl, imidazolidinone, dioxidoisothiazolidinyl, (C1-C4)-alkylpiperazinyl, residue -SO2- substituted with amino-group, (C1-C4)-alkylamino-group, (C1-C4)-dialkylamino-group, pyridinylamino-group, piperidinyl, hydroxyl or (C1-C4)-dialkylamino-(C1-C3)-alkylamino-group; R2 represents hydrogen atom (H); or R1 represents H and R2 means phenyl possibly substituted with halogen atom or -SO2-NH2; X represents -C(O)-, -C(S)- or -SO2-;R3 represents phenyl optionally substituted with 1-3 substitutes comprising halogen atom and nitro-group or 1-2 substitutes comprising (C1-C4)-alkoxy-group, hydroxy-(C1-C4)-alkyl, amino-group or (C1-C4)-alkyl possibly substituted with 1-3 halogen atoms by terminal carbon atom; (C3-C7)-cycloalkyl possibly substituted with 1-2 groups of (C1-C4)-alkyl; thienyl possibly substituted with halogen atom, (C1-C4)-alkyl that is substituted possibly with -CO2-(C1-C4)-alkyl, (C2-C4)-alkenyl that is substituted possibly with -CO2-(C1-C4)-alkyl, (C1-C4)-alkoxy-group, pyrrolyl, pyridinyl or amino-group substituted with -C(O)-C1-C4)-alkyl; (C1-C4)-alkyl substituted with thienyl or phenyl substituted with halogen atom; (C2-C8)-alkynyl substituted with phenyl; amino-group substituted with halogen-substituted phenyl; furyl, isoxazolyl, pyridinyl, dehydrobenzothienyl, thiazolyl or thiadiazolyl wherein thiazolyl and thiadiazolyl are substituted possibly with (C1-C4)-alkyl; to their pharmaceutically acceptable salts, a pharmaceutical composition based on thereof and a method for its preparing. New compounds possess selective inhibitory effect on activity of cyclin-dependent kinases and can be used in treatment of tumor diseases.
EFFECT: improved preparing method, valuable medicinal and biochemical properties of compounds and composition.
16 cl, 3 tbl, 26 ex
FIELD: organic chemistry, medicine.
SUBSTANCE: invention relates to aryl-substituted pyrazoles or triazoles of the general formula (I): and their pharmaceutically acceptable salts, prodrugs or solvates wherein X means oxygen (O) or sulfur atom (S); Het means one of group of the formula wherein R1 means hydrogen atom (H), (C1-C6)-alkyl, aminocarbonyl, -C(O)R10; R2 and R3 mean independently hydrogen atom (H) or aminocarbonyl; R5, R6, R7 and R8 mean independently hydrogen (H), halogen atom, (C1-C6)-alkyl, -NO2; R10 means -OR11 wherein R11 means hydrogen atom (H), (C1-C6)-alkyl. Compounds of the formula (I) are useful for treatment of neuronal damages observing as result of total or focus ischemia, for treatment or prophylaxis of neurodegenerative states, such as amyotrophic lateral sclerosis and for treatment, prophylaxis or reducing intensity of acute or chronic pains, as agents against entotic sound, anticonvulsant agents, and as anti-maniacal depressants, topical analgesic agents, anti-arrhythmic agents and for treatment or prophylaxis of diabetic neuropathy.
EFFECT: valuable medicinal properties of compounds and pharmaceutical composition.
13 cl, 1 dwg
FIELD: organic chemistry, medicine, pharmacy.
SUBSTANCE: invention describes new derivatives of triazole of the general formula (I): wherein X represents group of the general formula (II): wherein R' means halogen atom; R4 means (C1-C6)-alkyl; L means group of the formula: -La-Lb wherein La means a simple bond, oxygen atom, phenyl group that can be optionally substituted with halogen atom, cyano-group, (C1-C6)-alkyl, (C1-C6)-alkoxy-group or (C1-C6)-alkyl substituted with a single group -O-P(=O)(OH)2, naphthyl group, 5-membered heteroaryl group comprising as a heteroatom oxygen (O) or sulfur (S) atom, or (C3-C7)-cycloalkyl group that is substituted with carboxyl group; and Lb means (C1-C5)-alkylene group that can be optionally substituted with (C1-C6)-alkyl, carboxyl group or di-[(C1-C6)-alkyl]-amino-(C1-C6)-alkyl group; R means hydrogen atom, (C1-C6)-alkanoyl that can be optionally substituted with group: -Q-NR2'R3' wherein Q means a simple bond or carbonyl group, and R2' and R3' in common with nitrogen atom with that they are bound form piperazinyl ring substituted with (C1-C6)-alkyl and/or carboxyl group, or group: -O-P(=O)(OH)2; or their pharmacologically acceptable salts, pharmaceutical composition based on thereof, and a method for treatment of fungal infections.
EFFECT: valuable medicinal properties of compounds and composition, improved method for treatment of infections.
24 cl, 14 tbl, 1 dwg, 45 ex
FIELD: medicine, gynecology.
SUBSTANCE: one should carry out intrauterine photohemotherapy with the help of special equipment for 45-50 min, 5 seances. Moreover, for interrupting acute manifestations of vaginal candidosis it is necessary to conduct therapy with antimycotic preparations once daily for 3 d, and since the 3d-4th d one should perform intrauterine photohemotherapy every other day at the mode "II", after photohemotherapy it is useful to continue antimycotic vaginal therapy for 3 d more. For treating chronic, relapsing forms of vaginal candidosis therapy with antimycotic preparations should be fulfilled locally every other day by alternating it with intrauterine photohemotherapy at modes "II" and "III". In 1.5-2 mo after the course of therapy it is suggested to carry out repeated course of intrauterine photohemotherapy at the mode "III", every other day, 5 seances.
EFFECT: higher efficiency of therapy.
1 cl, 1 ex
FIELD: medicine, medicinal agents, pharmacy.
SUBSTANCE: invention relates to a medicinal agent made as ointment, gel, vaginal or rectal suppository and designated for treatment of candidomycosis and comprising ketoconazole or fluconazole (variants) in the dose 0.01-0.4 g/1 g of agent, and recombinant alpha-interferon in the dose 150000-3000000 IU/g (for rectal and vaginal suppository) and 5-50000 IU/g (for ointment and gel). Invention provides the development of agent with prolonged effect as ointment, gel, vaginal or rectal suppository showing good penetrating capacity and possessing an antimycotic effect.
EFFECT: valuable medicinal and pharmaceutical properties of agent.
14 cl, 4 tbl, 6 ex
FIELD: organic chemistry, medicine, chemical-pharmaceutical industry, pharmacology, pharmacy.
SUBSTANCE: invention relates to a medicinal agent used for prophylaxis and treatment of diseases and disorders associated with dysfunction of benzodiazepine receptors. This medicinal agent comprises compound of the formula (I)
. Compound of the formula (I) elicits high cardioprotective, neurotrophic, renoprotective activity and enhanced bioavailability.
EFFECT: valuable medicinal properties of compounds.
5 cl, 1 tbl, 1 ex
SUBSTANCE: method involves applying dietotherapy of zoosterol as 0.5% of aqueous solution in the amount of 100-200 ml in the morning 30 min before taking meals at a daily dose of 0.5-1.0 g in 21 days long course.
EFFECT: enhanced effectiveness in correcting metabolism disorders.
FIELD: organic chemistry, vitamins, medicine, pharmacy.
SUBSTANCE: invention relates to a new compound of the formula (I): wherein X means hydrogen atom or hydroxy group; R1 and R2 that can be similar or different mean hydrogen atom, (C1-C4)-alkyl; R3 means hydrogen atom, methyl group, fluorine or chlorine atom. Also, invention relates to its esters able to hydrolysis in vivo in combination with pharmaceutically acceptable acids. Also, invention relates to a pharmaceutical composition eliciting the inhibitory activity with respect to proliferation and promoting differentiation of cells and comprising the effective dose of compound of the formula (I) in common with pharmaceutically acceptable carriers and/or excipients. Also, invention relates to applying compound of the formula (I) for preparing a medicine used in treatment and prophylaxis of disease characterizing by abnormal differentiation of cells and/or proliferation of cells.
EFFECT: valuable medicinal properties of compounds.
13 cl, 3 sch, 3 tbl, 6 ex
FIELD: organic chemistry, pharmacy, biochemistry.
SUBSTANCE: invention relates to new substituted 2H-pyrano[2,3-c] of the general formula (1) eliciting ability to inhibit activity of protein kinase. In the general formula (1) X represents oxygen atom or group NR3; R1 represents group -C(O)R4, optionally substituted and optionally condensed azaheterocycle; R2 represents optionally substituted hydroxyl group or optionally substituted amino-group; R3 represents hydrogen atom or inert substitute meaning optionally substituted low- or non-reactive radical including such as (C1-C7)-alkyl, (C2-C7)-alkenyl, (C2-C7)-alkynyl, (C1-C7)-alkoxy-group, (C7-C12)-aralkyl, heterocyclylalkyl, (C7-C12)-alkaryl, (C3-C10)-cycloalkyl, (C3-C10)-cycloalkenyl, phenyl, aryl, (C2-C12)-alkoxyalkyl, (C2-C10)-alkylsulfinyl, (C2-C10)-alkylsulfonyl, -(CH2)-O-(C1-C7-alkyl), -(CH2)m-N(C1-C7-alkyl)n, aryloxyalkyl, heterocyclyl wherein m and n have value from 1 to 7; R4 represents optionally substituted amino-group or hydrogenated optionally substituted azaheterocycle. Also, invention relates to combinatory and focused libraries consisting of compounds of the present invention and designated for the search of compound-hits and compound-leaders prepared by screening of these libraries for using in preparing medicinal agents.
EFFECT: valuable medicinal properties of compounds.
8 cl, 2 tbl, 6 ex
FIELD: medicine, nephrology.
SUBSTANCE: the present innovation deals with introducing mildronate per 0.25 g 4 times daily about 30 min before meals for 3 wk, and then - per 0.25 g thrice daily about 30 min before meals for 4 wk at the background of daily intake of dipiridamol at the dosage of 200 mg/d. If necessary, therapeutic course should be repeated in 6 mo. The innovation improves endothelial function that leads to suppressed inflammatory process in kidneys and their improved functional capacity.
EFFECT: higher efficiency of therapy.
1 ex, 1 tbl
FIELD: organic chemistry, medicine, pharmacy.
SUBSTANCE: invention relates to new derivatives of triazaspiro[5,5]undecane of the formula (I):
wherein values of radicals R1-R5 are given in the invention claim, ort o their quaternary ammonium salts, N-oxides or nontoxic salts. Proposed compounds possess inhibitory and regulating activity with respect to chemokine/chemokine receptors and can be useful in prophylaxis and treatment of different inflammatory diseases, such as asthma, atopic dermatitis, nettle rash, allergic diseases, nephritis, hepatitis, arthritis or proliferative arthritis and other similar diseases. Also, invention relates to pharmaceutical compositions based on compounds of the formula (I).
EFFECT: improved control method, valuable medicinal properties of compounds.
9 cl, 5 sch, 36 tbl, 70 ex
FIELD: organic chemistry, medicine, pharmacy.
SUBSTANCE: invention relates to derivative of triazaspiro[5.5]undecane of the formula (I): wherein R1 means compound of the formula (1): or (2): wherein G represents a bond, (C1-C4)-alkylene, (C2-C4)-alkenylene or -CO-; ring A represents: (1) C5-10-membered mono- or bicarbocyclic ring or (2) 5-10-membered mono- or bicyclic heterocycle comprising 1-2 nitrogen atoms and/or 1-2 oxygen atoms; substitute R6 means the following values: (1) (C1-C4)-alkyl, (2) halogen atom, (3) nitrile group, (4) trifluoromethyl group and others; R2 represents: (1) (C1-C4)-alkyl, (2) (C2-C4)alkynyl or (3) (C1-C4)-alkyl substituted with a substitute represented in claim 1 of the invention claim; each R3 and R4 represents independently: (1) hydrogen atom, (2) (C1-C4)-alkyl or (3) (C1-C4)-alkyl substituted with 1-2 substituted taken among: (a) Cyc 2 and (b) hydroxy-group (wherein Cyc 2 represents (1) C5-6-membered monocarbocyclic ring or (2) 5-6-membered monocyclic heterocycle comprising 1-2 nitrogen atoms and/or one oxygen atom), or R3 and R4 form in common group of the formula: wherein R26 represents (C1-C4)-alkyl or Cyc 2; R5 represents hydrogen atom or (C1-C4)-alkyl, its quaternary ammonium salt, its N-oxide or its nontoxic salt. Also, invention relates to pharmaceutical composition inhibiting HIV, regulator of chemokine/chemokine receptor and agent used in treatment and prophylaxis of some diseases, such as inflammatory diseases, asthma, atopic dermatitis, nettle rash, allergic diseases, nephritis, hepatitis, arthritis and other diseases that comprise as an active component above described compound of the formula (I) or its quaternary ammonium salt, its N-oxide or its nontoxic salt. Also, invention relates to (3R)-1-butyl-2,5-dioxo-3-((1R)-1-hydroxy-1-cyclohexylmethyl)-9-(4-(4-carboxyphenyloxy)phenylmethyl)-1,4,9-triazaspiro[5.5]undecane or its pharmaceutically acceptable salt and pharmaceutical composition based on thereof, and to (3R)-1-butyl-2,5-dioxo-3-((1R)-1-hydroxy-1-cyclohexylmethyl)-9-(4-(4-carboxyphenyloxy)phenylmethyl)-1,4,9-triazaspiro[5.5]undecane hydrochloride and pharmaceutical composition based on thereof.
EFFECT: valuable medicinal properties of derivative and composition.
16 cl, 32 ex
FIELD: medicine, in particular experimental biology.
SUBSTANCE: invention relates to method for prophylaxis and treatment of systemic amyloidosis and nephropathic form thereof, induced in experimental animal. In this purpose 10 % mildronate solution is hypodermically administrated to animals every second day in dose of 50 mg/kg during last 14 days of experiment.
EFFECT: effective method for disease treatment due to simultaneous action on different component of pathogenesis, namely amyloid mass formation in kidney.