Analogues of cystamine, used for parkinson's disease treatment

FIELD: medicine.

SUBSTANCE: application of a therapeutically effective amount of at least one cysteamine analog, namely cysteamine and cystamine or a pharmaceutically acceptable salt thereof, for Parkinson's disease treatment at stage II, III or IV according to the Hoehn and Yahr classification, and wherein the cystamine analog or a pharmaceutically acceptable salt thereof is used as: a) an agent for functional restoration of damaged neurons; and/or b) an agent for the structural repair of damaged neurons. Application of a combination comprising at least one cystamine analogue and cysteine or salts thereof for treatment of Parkinson's disease in a patient with Parkinson's disease symptoms, and application of a pharmaceutical composition comprising at least one cystamine analogue or pharmaceutically acceptable salts thereof and containing cysteine or pharmaceutically acceptable salt thereof for treatment of Parkinson's disease in a patient with Parkinson's disease symptoms, is proposed.

EFFECT: functional and structural repair of damaged dopaminergic neurons with cysteamine or cystamine and increased number of nerve cells axons in the damaged areas, cysteine significantly increases cysteamine absorption by the brain.

16 cl, 12 dwg

 



 

Same patents:

FIELD: medicine, pharmaceutics.

SUBSTANCE: claimed invention relates to chemical-pharmaceutical industry and represents application of substituted nitrocatechols of formula for prevention or treatment of disorders, associated with central and peripheral nervous system, which obtain use from inhibition of catechol-O-methyltransferase (COMT), in accordance with schedule of dosing in the range from one time per three days to one time per week.

EFFECT: obtaining composition for prevention or treatment of disorders, associated with central and peripheral nervous system.

45 cl, 1 dwg, 3 ex

FIELD: chemistry.

SUBSTANCE: invention relates to novel compounds of formula

,

possessing properties of binding with delta opioid receptors. In formula I R1 is selected from the group, consisting of phenyl, pyridinyl and thiazolyl, with R1 being optionally substituted with one or two substituents, independently selected from the group, consisting of C1-4alkoxy, fluorine atom, chlorine atom, bromine atom and cyanogroup; in addition, R1 is optionally substituted with di(C1-4alkyl)aminocarbonyl; Y represents O, S, H3, vinyl, ethinyl or S(O); R2 represents a substituent, selected from the group, consisting of hydrogen, C1-4alkyl, C1-4alkoxy, C1-4alkylthio, fluorine atom, chlorine atom, bromine atom and hydroxy; Ra represents hydrogen or methyl; R3 is selected from the group, consisting of pyrrolidin-2-ylmethyl; pyrrolidin-3-ylmethyl; piperidin-2-ylmethyl, piperidin-3-ylmethyl, piperidin-4-ylmethyl, piperidin-2-ylethyl, piperidin-3-ylethyl, piperidin-4-ylethyl, pyridine-4-yl-(C1-2)alkyl, azetidin-3-ylmethyl; morpholin-2-ylmethyl, morpholin-3-ylmethyl, imidazolylmethyl, thiazolylmethyl, (amino)-C3-6cycloalkyl, 3-hydroxy-2-aminopropyl, 8-azabicyclo[3.2.1]octanyl, 1-azabicyclo[2.2.2]octanyl, guanidinylethyl, 4-(imidazol-1-yl)phenylmethyl, 2-(methylamino)ethyl, 2-diethylaminoethyl, 4-diethylaminobut-2-yl, piperidin-3-yl, piperidin-4-yl and pyrrolidin-3-yl; with piperidin-3-yl being optionally substituted on a carbon atom with phenyl; with pyrrolidin-2-yl in pyrrolidin-2-yl-methyl, pyrrolidin-3-yl, piperidin-3-yl and piperidin-4-yl being optionally substituted on a nitrogen atom with methyl, phenylmethyl, phenethyl or methylcarbonyl.

EFFECT: compounds can be used in the treatment of pain, induced by diseases or conditions, such as osteoarthritis, rheumatoid arthritis, migraine, burn, fibromyalgia, cystitis, rhinitis, neuropathic pain, idiopathic neuralgia, toothache, etc.

24 cl, 3 tbl, 19 ex

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention relates to novel compounds of formula I, possessing ability of binding with delta-opioid receptors. In formula R1 is selected from the group, consisting of i) phenyl, optionally substituted with one-two substituents, independently selected from the group, consisting of C1-4alkyl, C1-4alcoxy, C1-4alkylthio, hydroxyl, di(C1-4alkyl), aminocarbonyl, chlorine and fluorine, in such a way that only one di(C1-4alkyl)aminocarbonyl is present; ii) naphthyl; iii) pyridinyl, optionally substituted with one substituent, selected from the group, consisting of C1-4alkyl, C1-4alcoxy, C1-4alkylthio, hydroxy, fluorine, chlorine and cyano; iv) pyrimidin-5-yl; v) furanyl; vi) thienyl; vii) 5-oxo-4,5-dihydro-[1,2,4]oxodiazol-3-yl; and viii) di(C1-2alkyl)aminocarbonyl; Y represents ethyl, vinyl or bond; or Y represents O, when R1 represents optionally substituted phenyl, where substituent represents C1-4alcoxy; R2 represents phenyl, optionally substituted with one-two substituents, independently selected from the group, consisting of C1-4alkyl, C1-4alcoxy, fluorine, chlorine and cyano, trifluoromethoxy and hydroxy; or R2 represents phenyl, substituted with one aminocarbonyl, di(C1-4alkyl)aminocarbonyl, C1-4alcoxycarbonyl or carboxysubstituent; R3 is selected from the group, consisting of i) 3-aminocyclohexyl; ii) 4-aminocyclohexyl; iii) piperidin-3-yl; iv) piperidin-4-yl; v) pyrrolodin-2-yl-methyl, in which pyrrolodin-2-yl is optionally substituted by 3-rd or 4-th position with one or two fluorine-substituents; vi) azetidin-3-yl; vii) 2-(N-methylamino)ethyl; viii) 3-hydroxy-2-aminopropyl; ix) piperidin-3-yl-methyl; x) 1-azabicyclo[2.2.2]octan-3-yl; and xi) 8-azabicyclo[3.2.1]octan-3-yl; or R3 together with Ra and nitrogen atom, which they both are bound to, form piperazinyl, optionally substituted with 4-C1-4alkyl; Ra represents hydrogen, 2-(N-methylamino)ethyl or C1-2alkyl, optionally substituted with azetidin-3-yl.

EFFECT: compounds can be used in treatment of pain in the range from medium to strong, caused by diseases or conditions, such as osteoarthritis, migraine, burn, fibromyalgia, cystitis, rhenite, neuropathic pain, idiopathic neuralgia, toothache, etc.

21 cl, 4 tbl, 26 ex

FIELD: medicine, pharmaceutics.

SUBSTANCE: group of inventions relates to medicine and deals with the application of at least one peptide, selected from the group, including SEFKHG(C), TLHEFRH(C), ILFRHG(C), TSVFRH(C), SQFRHY(C), LMFRHN(C), SPNQFRH(C), ELFKHHL(C), THTDFRH(C), DEHPFRH(C), QSEFKHW(C), ADHDFRH(C), YEFRHAQ(C) and TEFRHKA(C), for the production of a medication for the prevention and/or treating Alzheimer's disease. The group of inventions relates a vaccine, containing at least one said peptide, intended for the induction of immune response aimed against Aβ.

EFFECT: group of invention provides the favourable effect of vaccination with vaccines with mimotopes in the treatment of Alzheimer's disease.

24 cl, 3 ex, 10 dwg, 5 tbl

FIELD: medicine, pharmaceutics.

SUBSTANCE: present invention refers to a storage-stable pharmaceutical composition and a pharmaceutical formulation containing at least one active pharmaceutical ingredient presenting a nitrocatechol derivative, 2,5-dichlor-3-(5-(3,4-dihydroxy-5-nitrophenyl)-1,2,4-oxadiazol-3-yl)-4,6-dimethylpyridine 1-oxide, at least one excipients and at least one binding agent, wherein at least one excipient is other than a phosphate derivative, wherein at least one binding ingredient is other than a polyvinylpyrrolidone compound, and wherein the above active pharmaceutical ingredient is present in the granulated form.

EFFECT: compositions and/or formulations according to the invention are stable for a long period of time and show a high stability if stored in the high temperature and moisture environment.

26 cl, 8 tbl, 4 ex

FIELD: medicine, pharmaceutics.

SUBSTANCE: group of inventions refers to a pharmaceutical composition based on a compound of formula (I) or its pharmaceutically acceptable salt or solvate. wherein X is S or O, and provided X is S, R1 is OH or NH2; and provided X is O, R1 is OH, NH2 or NHMe. The invention also refers to a compound of formula (I) and a based kit.

EFFECT: there are prepared new imidazolidine derivatives effective in treating prostate cancer.

28 cl, 14 tbl, 14 ex

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention refers to new compounds of formula I, wherein R1 and R2 are identical or different and specified in an alkyl or alkenyl hydrocarbon chain; the R3 group values split by lipase are specified in the patient claim. R4 and R5 are independently hydrogen or C1-C7alkyl; R6 represents hydrogen or C1-C7alkyl; and R7 and R8 are independently hydrogen or C1-C7alkyl. The invention also refers to using compounds of formulas ,

which are introduced into the mammalian biological system and increase the cell concentrations of specific sn-2 substituted ethanolamine-plasmalogens.

EFFECT: compounds are applicable in treating or preventing the age-related disorders associated with high membrane cholesterol, high amyloids and low plasmalogens, such as neurodegeneration, cognitive disorder, dementia, cancer, osteoporosis, bipolar disorder and vascular diseases.

11 cl, 18 dwg, 7 ex

FIELD: medicine.

SUBSTANCE: invention represents a drug preparation for Parkinson disease containing micronised L-DOPA (3-hydroxy-L-tyrosine) as an active ingredient, which represent stable particles containing poly(lactic-co-glycolic acid 50/50 (PLGA 50/50), or poly(lactic-co-glycolic acid 75/25 (PLGA 75/25), or poly(lactic-co-glycolic acid 50/50 with carboxyl group (PLGA-COOH 50/50), or lactic acid polymer (PLA) in an amount of 75.0÷79.0 wt %, D-mannitol in an amount of 7.5÷8.0 wt %, as well as either polyvinyl alcohol (PVA) or Tween 80.

EFFECT: treating Parkinson disease more effectively.

2 cl, 4 dwg, 2 ex

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention refers to compounds of formula (I) and their pharmaceutically acceptable salts, wherein A is thiazolyl, oxazolyl, thienyl, furyl, imidazolyl, pyrazolyl or oxadiazolyl (structures of which are presented in cl.1 of the patent claim), R1 represents C1-6alkyl; R2 represents (i) phenyl substituted by halogen; C1-6alkyl optionally substituted by morpholine or C1-6dialkylamino; C1-6alkoxy optionally substituted by halogen; or heterocyclyl, wherein a heterocyclyl substitute is specified in morpholine; pyrazolyl optionally substituted by C1-6alkyl; piperidinyl; pyrrolidinyl; oxadiazolyl substituted by C1-6alkyl; furyl substituted by C1-6alkyl; dioxydoisothiazolidinyl; triazolyl; tetrazolyl substituted by C1-6alkyl, tridiazolyl substituted by C1-6alkyl; thiazolyl substituted by C1-6alkyl; pyridyl; or pyrazinyl; (ii) substituted or unsubstituted heterocyclyl specified in quinolinyl; pyridyl substituted by C1-6alkoxy or morpholinyl; or benzo [d] [1, 2, 3] triazolyl substituted by C1-6alkyl; R3 represents phenyl substituted by 2 or 3 substitutes specified in halogen; C1-6alkyl; C1-6alkoxy optionally substituted by halogen; hydroxy group; cyano; or -C(=O)ORa, wherein Ra represents phenyl; R4 represents hydrogen, C1-6alkyl or C1-6halogenalkyl. The invention also refers to a pharmaceutical composition containing the compounds of formula (I), a method for PDE10 inhibition, a method of treating neurological disorders, and to intermediate compounds: 2-(4-chlor-3,5-dimethoxyphenyl)furan and 4-(5-methyl-1,3,4-thiadiazol-2-yl)benzaldehyde.

EFFECT: compounds of formula (I) as PDE10 inhibitors.

39 cl, 13 ex, 2 tbl, 77 dwg

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention refers to medicine and represents a pharmaceutical composition for treating Parkinson's disease, containing a pharmaceutically acceptable carrier and a combination of flat doses of controlled release pramipexole and controlled release rasagiline; the above combination of flat doses contains pramipexole in an amount of 0.06 mg to less than 1.5 mg and rasagiline in an amount of 0.05 mg to less than 1.0 mg.

EFFECT: invention provides the synergetic action of rasagiline and pramipexole in treating Parkinson's disease.

3 cl, 11 dwg, 3 ex, 1 tbl

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention refers to pharmaceutical industry and represents a combination of leucine source and ω-3 polyunsaturated fatty acid source applicable in therapeutic or preventive treatment of hypercalcemia.

EFFECT: invention provides extending the range of products applicable in the therapeutic or preventive treatment of hypercalcemia.

19 cl, 8 dwg, 2 tbl, 4 ex

FIELD: medicine, pharmaceutics.

SUBSTANCE: group of inventions relates to medicine and deals with stable composition for provision of subject with therapeutically or prophylactically effective amount of alpha-1 protease inhibitor (API), containing alpha-1 protease inhibitor (API) and at least one amino acid, selected from alanine, threonine, serine or hydroxyproline, where said composition includes one or more auxiliary substances, where at least one amino acid is present in composition in the total amount of amino acid from approximately 0.01 M to approximately 3 M. Group of inventions also deals with set for treatment or prevention of API-associated disease or condition, which includes said composition; application of at least one amino acid, selected from alanine, threonine, serine or hydroxyproline, for stabilisation of composition, containing alpha-1 protease inhibitor (API).

EFFECT: group of inventions provides stability of API composition.

15 cl, 27 dwg, 5 tbl, 8 ex

FIELD: veterinary medicine.

SUBSTANCE: composition comprises succinic acid, trace elements in the form of sulphates of iron, copper, cobalt, zinc and additionally comprises methionine and beet-root molasses at the following content of components in 1000 ml of an aqueous solution: succinic acid - 5.0 g, beet-root molasses - 150.0 ml, methionine - 2.0 g, ferrous sulphate - 10.0 g, copper sulphate - 0.1 g, cobalt sulphate - 0.5 g, zinc sulphate - 0.5 g.

EFFECT: use of the claimed composition has a positive effect on the immune-metabolic status and growth activity of piglets.

3 tbl, 2 ex

FIELD: medicine, pharmaceutics.

SUBSTANCE: group of inventions refers to medicine, namely to dermatology, and can be used for preventing and/or treating skin itching. It involves using L-serine as a therapeutic agent, a pharmaceutical composition containing L-serine, as well as a dermato-cosmetic composition containing L-serine as a single active agent, Avene Thermal Spring Water, glycerine and a cosmetically acceptable carrier. The L-serine concentration in the composition makes from 0.01 wt % to 10 wt % in relation to the total weight of the composition. More preferentially, the concentration makes 0.5 wt % to 3 wt % in relation to the total weight of the composition.

EFFECT: group of inventions provides the effectiveness of application.

8 cl, 2 tbl, 3 ex

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention refers to the chemical-pharmaceutical industry and represents an agent for preventing or reducing pigmentation, containing a compound presented by the following formula (1) its stereoisomer and/or its pharmacologically acceptable salt, wherein: R1 represents a hydrogen atom or an alkyl group with a linear or branched chain having 1-4 carbon atoms; R2 represents a hydrogen atom or an unsubstituted aliphatic hydrocarbon group having 1-4 carbon atoms; R3 represents an unsubstituted aromatic group having 5-15 carbon atoms, substituted by an alkyl group having 1-6 carbon atoms, by an alkoxy group containing an alkyl chain having 1-6 carbon atoms, or by a phenyl group; R3 also represents an aromatic group having 5-15 carbon atoms; n is equal to 1 or 2, and m represents an integer falling within 0 to 3.

EFFECT: preparing the agent for preventing or reducing pigmentation.

10 cl, 10 ex, 6 tbl

FIELD: biotechnology.

SUBSTANCE: invention relates to a biodegradable synthetic polymer, namely to the polymer of the general formula (I) , where NA has the structure: , AN has the structure: , where n is an integer >2; Z is either absent or is an amino acid residue -NH-(CH2)i-CO-, where i - is an integer from 1 to 5; D represents a linear or branched alkyl C1-C5 or benzyl; B represents a residue of aliphatic diamine -NH-(CH2)k-NH-, where k is an integer from 2 to 6; X and Y can simultaneously have the following meanings: X=H-B, Y=H, or X=Nα-(D-OCO)-L-arginyl-Z-B, Y=Nα-(D-OCO)-L-arginyl-Z, or X=R1-AN-B, Y=NA-R1, where R1 is carboxamide-alkyl of the type H2NCO-CH2- or H2NCO-CH2CH2-. Such a polymer is capable of delivering the natural L-arginine into the tissues of human, animals, through biological membranes and can be used alone or in a combination with other active compounds.

EFFECT: invention enables to obtain the polymer soluble in water, which has no cytotoxicity and enhances the level of nitrogen oxide in the tissues of humans and animals.

2 tbl, 7 ex

FIELD: medicine.

SUBSTANCE: invention represents a balanced infusion solution containing sodium, potassium and magnesium chlorides, a solvent and sodium L-arginine succinate of formula: Na+[NH=C(NH2)NH(CH2)3CH(NH2)COOH]+[OOC(CH2)2COO]2-. The ingredients in the solution are found in certain proportions, wt %.

EFFECT: invention provides enhanced detoxification activity, low toxicity and wide range of clinical applications.

11 tbl, 6 ex

FIELD: medicine.

SUBSTANCE: invention relates to a method of treating a mammal with endometriosis. The claimed method includes the pulse or interrupted peroral introduction of an N-acetyl-L-cysteine-containing pharmaceutical composition for 3-5 successive days with the following 2-4-day break or for 1-3 successive days with the following 1-2-day break, for at least a two-month time period. N-acetyl-L-cysteine in the said method is introduced in a dose, constituting from 20 to 90 mg/kg/day.

EFFECT: claimed method provides the more significant effect with respect to endometriosis symptoms in comparison with the traditional daily introduction of N-acetyl-L-cycteine.

11 cl, 7 dwg, 2 tbl, 3 ex

FIELD: medicine.

SUBSTANCE: invention refers to medicine, namely to traumatology and orthopaedics, and can be used for treating proximal humeral injuries. That is ensured by three-staged complex therapeutic actions. At the first stage, setting of fracture and reduction of humeral head dislocation is followed by immobilising an extremity by continuous twenty-four hour brace fixation of the proximal humerus with Desault's bandage for the period of 4 weeks. From the first therapeutic day, the patient does daily 30-minute therapeutic exercises, including isometric, static and ideomotor exercises to strengthen his/her arm muscles and to improve the circulation. That is combined with a complex reparative drug therapy. At the first stage, the anti-inflammatory preparation Arthrofoon is administered orally, while vasodilators improving nicotinic acid, trental or complamin microcirculation are injected intramuscularly daily for 10 days. The enzymatic preparations Wobenzyme or Flogenzyme are also administered in a dose of 3 tablets three times a day for 3-4 weeks. The second stage starting two weeks after the beginning of the treatment involves electric stimulation (ES) by exposing the collar and shoulder muscles from the involved side for 30 minutes to electric signals generated by an electric myostimulation device. The ES procedure requires the patient to perform 15-minute active motions by a healthy arm, and for the following 15 minutes the patient is expected to tense and relax alternatively the muscles from involved side. The therapeutic exercises are also done. The drug treatment regimen of the second stage implies administering the preparations Calcemin or Calcemin Advance for six months. That is combined with 10 daily intramuscular injections of the preparation Milgamma 2 ml. At the third stage 4 weeks after the beginning of the treatment, control X-ray imaging is followed by removing the brace. Accompanied by the reparative drug therapy continued, the complex therapeutic actions provide local injection therapy in number of 8-10 daily procedures. The biologically active reflex areas nearby the involved joint are pre-exposed to focused red laser light, and the mixed preparations Alflutop, or other chondroprotector, vitamin B12, Contrykal or Lidase, Lidocaine are injected in the same areas. Two weeks after the brace has been taken off, the patient keeps doing the therapeutic exercises twice a week continuously. The drug therapy and local injections are repeated six months later. The brace is further required for the following year if the patient is supposed to bear occupational or sports physical loads.

EFFECT: method provides faster recovery of the extremity functionality, prevents posttraumatic degenerative process in the humeral joint, recurred dislocation formation, humeral instability and contractures by optimising the humeral para-articular tissue health, improving the quality of bone tissues, first of all, of the subchondral plate and humeral head.

2 cl, 1 dwg, 2 ex

FIELD: medicine.

SUBSTANCE: composition has an action of the central nervous system; it is presented in the form of a solution, contains glycine, glycerol, a preserving agent and water. The invention also concerns a therapeutic agent and a biologically active addition based on the above composition.

EFFECT: group of inventions provides high bioavailability as the composition is presented in the liquid and ease of dosing.

12 cl, 2 tbl, 3 ex

FIELD: medicine.

SUBSTANCE: invention represents a dietary supplement for preventing alcoholic intoxication and relieving alcohol withdrawal syndrome presented in the form of a tablet containing silicone dioxide, taurine, succinic acid and excipients; the ingredients in the tablet are taken in certain ratio, in grams.

EFFECT: extending the range for preventing alcoholic intoxication and relieving alcohol withdrawal syndrome.

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