Combination of selective inhibitor of reverse noradrenaline capture and pdev inhibitor

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention concerns medicine drugs, particularly combination for pain mitigation, including synergic dosage of (S,S)-reboxetine or its pharmaceutically acceptable salt or solvate and 5 type phosphodiesterase inhibitor (PDEV), 3-ethyl-5-[5-(4-ethylpiperasine-1-ylsulfonyl)-2-n-propoxyphenyl]-2-(pyridin-2-yl)methyl-2,6-dihydro-7H-pyrasolo[4,3-d]pyrimidine-7-on. In addition, invention concerns composition and kit for pain mitigation, including the claimed compounds, and application of the combination or composition in pain mitigation.

EFFECT: synergic effect of composition.

12 cl, 1 dwg, 1 ex

 

The text descriptions are given in facsimile form.

1. Combination for the treatment of pain, comprising a synergistic dose:

(a) (S,S)-reboxetine, or its pharmaceutically acceptable salt or MES;

(b) an inhibitor of phosphodiesterase type 5 (PDEV), where the inhibitor of phosphodiesterase type 5 (PDEV) is a 3-ethyl-5-[5-(4-ethylpiperazin-1-ylsulphonyl)-2-n-propoxyphenyl]-2-(pyridin-2-yl)methyl-2,6-dihydro-7H-pyrazole is[4,3-d]pyrimidine-7-one or its pharmaceutically acceptable salt or MES.

2. Pharmaceutical composition for treating pain comprising

(a) (S,S)-reboxetine, or its pharmaceutically acceptable salt or MES;

(b) an inhibitor of phosphodiesterase type 5 (PDEV), where the inhibitor of phosphodiesterase type 5 (PDEV) is a 3-ethyl-5-[5-(4-ethylpiperazin-1-ylsulphonyl)-2-n-propoxyphenyl]-2-(pyridin-2-yl)methyl-2,6-dihydro-7H-pyrazolo[4,3-d]pyrimidine-7-one or its pharmaceutically acceptable salt or MES, and

(C) pharmaceutically acceptable excipient, diluent or carrier.

3. The use of a combination according to claim 1 or a composition according to claim 2 in the manufacture of a medicinal product for simultaneous, sequential or separate introduction of both agents in the treatment of pain.

4. The use according to claim 3, where the pain is a sharp pain.

5. The use of a combination according to claim 3, where pain is a chronic pain.

6. The use according to claim 3, where pain is a nociceptive pain.

7. The use according to claim 3, where pain is a neuropathic pain.

8. The use according to claim 7, where neuropathic pain is selected from-herpetic neuralgia and painful diabetic neuropathy.

9. The use according to claim 3, where the pain is the pain of inflammation.

10. The use according to claim 3, where the pain is the result of musculoskeletal disorders.

11. The use of claim 10, where the NEC is to maintain muscle disorder is a fibromyalgia.

12. Set for treatment of pain, essentially consisting of

(a) a combination according to claim 1, and

(b) funds for the content of these compounds.



 

Same patents:

FIELD: medicine, pharmaceutics.

SUBSTANCE: pharmaceutical composition includes fluoroquinolone antibiotic ofloksacin, tissue reparation stimulator methyluracil and local anesthetic lidocain hydrochloride as active components. Composition base part is polyethyleneoxides with mol weight of 400 and 1500, soluble in water. Also composition includes nipagin and nipasol conservation agents at the ratio of 4:1 and propyleneglycol as plasticiser. Composition is produced as soft sterile formulation. Composition shows aseptic properties in the absence of repeated contamination. Composition has antibacterial, anaesthetic, regeneration and wound healing effect.

EFFECT: obtaining composition with antibacterial, anaesthetic, regeneration and wound healing effect.

2 cl, 3 ex

FIELD: medicine.

SUBSTANCE: invention refers to medicine, specifically to otorhinolaryngology, and is intended for determination of indications for differential therapy in sickly children (SC) suffering from lymphoepithelial pharynx ring pathology. Method is implemented as follows. Operating or biopsy material of lymphoepithelial pharynx ring is analysed for system and local immunity indices. If system and local immunity indices are below normal, system and local immune-response modulating agents are introduced. If system immunity indices only are below normal, system immune-response modulating agents only are introduced. If local immunity indices only are below normal, local immune-response modulating agents only are introduced. If system and local immunity indices are within normal limits, antiinflammatory therapy is applied.

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3 tbl, 4 ex

FIELD: chemistry; pharmacy.

SUBSTANCE: invention claims novel [1,2,4]triazolo[1,5-a]pyrimidine-2-ylurea derivatives of the general formula (1), or their pharmaceutically acceptable salts: [formula 1] , where Ar is optionally substituted phenyl group, dihydrobenzofuranyl or thiophenyl group. X is O. R is group of formula (2)-(6) or , where values of Cy and R4-R12 radicals are given in the claim, and medicine containing these compounds.

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14 cl, 16 tbl, 333 ex

Kinase inhibitors // 2348635

FIELD: chemistry; pharmacy.

SUBSTANCE: invention concerns new compounds of formula I: , where W is , X is N or C-R1; R is C1-C7alkyl, C3-C7cycloalkyl, (C1-C7alkylene)-(C3-C7cycloalkyl), -SO2-(C1-C7alkyl) or -SO2-NR5R6; R1 is hydrogen, amino, methyl or -N=CH(NMe)2; R is phenyl optionally substituted by one or more substitutes selected independently out of halogen; R3 is hydrogen, C1-C7alkyl, C3-C7cycloalkyl or phenyl optionally substituted by one or more substitutes selected independently out of halogen and trifluoromethyl; R4 is hydrogen or C1-C7alkyl; R5 and R6 are independently selected out of group including C1-C7alkyl; and its pharmaceutically acceptable salts. Also invention concerns pharmaceutical composition and application.

EFFECT: obtaining new bioactive compounds with inhibition effect on kinase p-38.

10 cl, 114 ex

FIELD: chemistry.

SUBSTANCE: invention concerns compound of formula (I) where Ry is , or its pharmaceutically acceptable salts. These compounds have phosphodiesterase (PDE) inhibition effect, particularly for PDE-4. Additionally invention claims application of compound of the formula (I) or its pharmaceutically acceptable salt in manufacturing of medicine for treatment and/or prevention of cognitive ability depression or disorder of humans, e.g. of chronic neurological disorder, such as Alzheimer's disease.

EFFECT: enhanced efficiency of composition and treatment method.

17 cl, 21 tbl, 191 ex

FIELD: chemistry; pharmacy.

SUBSTANCE: invention concerns novel compounds of formula I , where X1 is O; Ar1 is aryl optionally substituted by one or more halogen atoms; R1 is alkoxyalkyl, alkyl, cycloalkyl, cycloalkylalkyl, hydroxyalkyl, tetrahydropyranyl or piperidinyl optionally substituted by -S(O)2 alkyl group; and R2 is hydroxyalkyl or oxoalkyl. Also invention concerns composition for kinase p38 induced disease control or prevention.

EFFECT: obtaining novel bioactive compounds for kinase p38 induced disease control or prevention.

4 cl, 10 ex, 2 tbl

FIELD: chemistry.

SUBSTANCE: compounds of the invention have chemokine antagonistic properties and can be applied in treatment of immunoinflammatory diseases, such as atherosclerosis, allergy diseases. In general formula (I) R1 is hydrogen atom, (C1-C4)-alkyl, (C1-C4)-alkoxyl, cyclopropylmethoxy group, (C1-C4)-alkylthio group; R2 is halogen atom, (C1-C8)-alkyl, perfluoro-(C1-C4)-alkyl, (C3-C10)-cycloalkyl, phenyl, (C1-C8)-alkoxyl, values of the other radicals are indicated in the claim of the invention.

EFFECT: improved properties.

14 cl, 7 tbl, 20 dwg, 17 ex

FIELD: chemistry.

SUBSTANCE: invention concerns new 2-pyridone derivatives of formula (I): where R1, R2, R4, R5, G1, G2, L, Y and n are as specified in the invention formula, and their pharmaceutically acceptable salts, pharmaceutical compositions containing these compounds, and their application in therapy. These compounds have neutrophil elastase inhibition effect.

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7 cl, 1 tbl, 150 ex

FIELD: chemistry.

SUBSTANCE: invention concerns new bioactive compound of 4-aryl-2,4dioxybutane acid class, - 2-(1,2-diphenyl-2-oxoethylidenehydrazino)-4-(4-methoxyphenyl)-4-oxobut-2-ene acid of the formula (I) .

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1 ex, 1 tbl

FIELD: medicine.

SUBSTANCE: correction of pain syndrome accompanying severe psoriasis is ensured with skin irradiation within affected region or above inflammatory tissue using low intensity IR rays of CO2 laser. Laser wavelength is 10.6 mcm. Radiation power density in pulse-periodic regime is 0.015-1 Wt/cm2, radiation pulse duration is 0.5-10 mc, pulse window is 10-100 mc, and highly directional IR radiation divergence is 10-2 radians. While radiation, laser beam is moved on skin within affected region during 5-10 minutes, herewith zone exposure duration determined by laser beam diameter is 1-2 sec. Skin is preliminary coated with adenosine triphosphate with daily exposure within course of 10-15 days.

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1 ex

FIELD: medicine.

SUBSTANCE: invention concerns medicine, urology, and can be applied in vesicular prostate complex disease treatment. It involves placing patient into cryothermic chamber and exposed to heat carrier vapour based on liquid nitrogen for 2-3 minutes. Temperature within -140°C to -180°C is maintained inside the chamber. Cryotherapy course includes 10 daily sessions by one per day. Cryotherapy course is applied in conservative complex therapy of disease in decadent exacerbation or instable remission phase.

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5 tbl, 4 ex

FIELD: chemistry.

SUBSTANCE: present invention pertains to crystalline substance for peroral solid medicinal preparation, which is an indoline compound (KMD-3213), which exhibits blocking action to α1-adrinaline receptors, is suitable for use as a therapeutic medium in case of dysuria and is represented by formula (I) . The x-ray diffraction picture of the powder of this compound is characterised by main peaks 5.5°±0.2°, 6.1°±0.2°, 9.8°±0.2°, 11.1°±0.2°, 12.2°±0.2°, 16.4°±0.2°, 19.7°±0.2° and 20.0°±0.2°, as 2θ.

EFFECT: obtaining solid medicinal preparations for treating dysuria, containing this crystalline substance as an active ingredient.

14 cl, 3 dwg, 2 tbl, 9 ex

FIELD: medicine, urology.

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2 ex

FIELD: medicine; pharmacology.

SUBSTANCE: perform extraction by the water purified using the method of fractional maceration of the dried up leaves of garden wild strawberry - Fragaria ananassa, this. Rosaceae which crush till the sizes of particles from >1.0 mm to ≤3 mm. Perform extraction three times for 30 minutes in the ratio 1:10 (raw materials - extracting agent), in a reactor from stainless steel with a false bottom capacity of 100 l, supplied with an anchor mixer, a steam shirt and a sleeve for the thermometer. Aggregate the water extractions. Clearing of incorporated water extraction is performed by filtration through the druk-filter and separation. Evaporation of the incorporated water extraction is performed in circulating vacuum-evaporating device to 0.1 of the initial volume. Drying is performed on the spray-type dryer.

EFFECT: invention allows to realise the specified method.

8 tbl, 1 dwg

FIELD: medicine; pharmacology.

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4 cl, 3 ex, 2 tbl

FIELD: medicine; urology.

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1 ex, 2 tbl

FIELD: medicine; pharmacology.

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20 cl, 10 dwg, 4 ex

FIELD: chemistry.

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124 cl, 52 ex, 17 tbl, 2 dwg

FIELD: medicine.

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FIELD: chemistry.

SUBSTANCE: invention relates to novel substituted indoles of general formula , where: X stands for -S(O)n-, -C(O)-; A stands for C1-C6alkyl, -(CH2)p-NRaRb; R1, R2, R3 and R4 each is independently selected from group including H, halogen, halogen(C1-C6)alkyl, C1-C6alkyl, C1-C6alkoxy, C1-C6alkylthio, C1-C6alkylsulfinyl, C1-C6alkylsulfonyl, NO2, -NRaRb, phenyl, benzyl and benzyloxy, said phenyl cycles are optionally substituted with substituent, selected from group including C1-C6alkyl, halogen, NO2, halogen(C1-C6)alkyl, C1-C6alkoxy; R5 stands for H, C1-C6alkyl, C1-C6alkoxy, C1-C6alkoxy C1-C6alkyl, C1-C6alkylthio, C1-C6alkylsulfinyl, C1-C6alkylsulfonyl, hydroxyl-(C1-C6)alkyl, hydroxy(C1-C6)alkylamino, halogen, halogen(C1-C6)alkyl-NRaRb, -NRc-( C1-C6)alkylene-NRaRb, or R5 and A together form radical C2-C3alkylene; R6 stands for H, C1-C6alkyl; R' and R" each independently stand for H, C1-C6alkyl; Ra, Rb and Rc each is independently chosen from group including H, C1-C6alkyl, hydroxy(C1-C6)alkyl, C2-C6alkenyl, C3-C6cycloalkyl-(C1-C6)alkyl, or Ra and Rb together with nitrogen atom, to which they are attached, form 5-7 member non-aromatic heterocyclic cycle, optionally containing in cycle O as additional heteroatom; m is equal 1 or 2; n is equal 0, 1 or 2 under condition that, if n is equal 0, R5 does not stand for NRaRb, and p is equal 0, 1 or 2; or their pharmaceutically acceptable salts.

EFFECT: obtaining compounds possessing agonistic activity which allows using them in pharmaceutical composition.

24 cl, 2 tbl, 22 ex

FIELD: chemistry.

SUBSTANCE: present invention pertains to a new derivative of cyclic amine or its salts with the following formula (I): (where symbols stand for the following: A: 5-8-member cyclic amine, which may contain a double bond, a bridged structure and may contain substitutes R7-R11 in the ring, or -NH2, -NH(inferior alkyl), -N(inferior alkyl)2 or ) morpholin-1-yl; ring B: benzole, thiophene, furane, pyrrole, 5-7-member cycloalkane or 5-7-member cycloalkene; X1: a bond or inferior alkylene; X2: -(CR12R13)n-, -N(R14)-, -N(R14)CO-, -CON(R14)-, -CO-, -CH(OH)-, -N(R14)- (CR12R13)n-, (CR12R13)n-N(R14)-, -CON(R14)-(CR12R13)n-, -n(R14)CO-(CR12R13)n-, -(CR12R13)n-N(R14)CO-, -(CR12R13)n-CON(R14)-, -CO-(CR12R13)n- or -(CR12R13)n-CO-; Y1: -OH, -O-inferior alkyl, NH2 or -N3; R1 and R2: are identical or different and stand for a halogen atom, inferior alkyl or inferior alkylene-OH; R3-R6: are identical or different and stand for a hydrogen atom, a halogen atom, inferior alkyl, inferior alkenyl, inferior alkynyl, -O-inferior alkyl, -OH, -NH2, -NH(inferior alkyl), -N(inferior alkyl)2, -NH-CO- inferior alkyl, -N(inferior alkyl)-CO- inferior alkyl, -CN-, -NO2, -CF3, -O-inferior alkylene-OH, -inferior alkylene-OH, -inferior alkylene-halogen, -inferior alkylene-O-inferior alkyl, -CO-5-8-member cyclic amine, -COOH-inferior alkyl, -COO-inferior alkylene-aryl, pyridine, thiophene, -inferior alkylene-morpholine, aryl, which may contain a substitute: -O-inferior alkyl or -CF3; R7: hydrogen atom, inferior alkyl, -inferior alkylene-aryl or -inferior alkylene-pyridine: R7 is substitute on the nitrogen atom of the cyclic amine; R8-R14: are identical or different and stand for a hydrogen atom or inferior alkyl; n: is an integer, equal to 1, 2 or 3; where R5 and R6, R4 and R5 or R3 and R4 can form an inferior alkylene together, -O-inferior alkylene-O-, -O-inferior alkylene-, -inferior alkylene-O-, -C(R15)=C(R16)-O-, -O-C(R15)=C(R16)-, -C(R15)=C(R16)-C(R17)=C(R18)-; R3 and Y1 together can form -O-inferior alkylene-O- or -inferior alkylene-O-; R1 and Y1 together can form -inferior alkylene-O-; and Y1 and a branch on - X1-A together can form -O- or -O-inferior alkylene; R15-R18 stand for a hydrogen atom, under the condition that, 6-chloro-2,2-dimethyl-1-(1-methyl-4-piperidinyl)indan-1-ol is not included in the group of compounds). The invention also pertains to a derivative of cyclic amine or its salts with formula (II), to a derivative of cyclic amine or its salts with formula (III), to pharmaceutical composition, as well as their use.

EFFECT: obtaining new biologically active compounds and pharmaceutical compositions based on these compounds, with antagonist effect on NMDA receptors NMDA.

7 cl, 160 ex, 45 tbl

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