3-phenylpyrazolo[5,1-b]thiazole derivative. RU patent 2482120.
![3-phenylpyrazolo[5,1-b]thiazole derivative. RU patent 2482120.](http://img.russianpatents.com/997/9975086.gif)
 Condensed heterocyclic compound / 2480473Invention relates to compounds of formula 1 , where X and T are N or C, Q is a (3-7)-member aromatic ring which contains 0-3 nitrogen atoms as ring members, and which is optionally benzo-condensed and is substituted with oxo; C1-C6-alkyl; halogen- C1-C6-alkyl; hydroxy-C1-C6-alkyl; C1-C6-alkoxy; C6-C10-aryl; or a (3-7)-member heteroaryl containing 1-3 oxygen atoms, P is C1-C6-alkyl, optionally substituted with a halogen, and R is a group selected from: (i) -C1-C6-alkyl-R1, (ii) -NR2R3, (iii) -O-R4, (iv) -S-R5, (v) -C (=O))-R6, (vi) optionally substituted (3-7)-member heteroaryl containing 1-4 heteroatoms selected from a nitrogen atom, an oxygen atom and a sulphur atom, (vi) optionally substituted (3-7)-member heteroatom containing 1-4 heteroatoms selected from a nitrogen atom, an oxygen atom and a sulphur atom, (vii) optionally substituted, saturated or partially unsaturated, separate or condensed (3-10)-member heterocyclic ring containing 1-4 heteroatoms selected from a nitrogen atom, an oxygen atom and a sulphur atom, (viii) azido; where each R1, R2, R3, R4, R3, R6, is as described in the claim. The invention also relates to a pharmaceutical composition for preventing and treating a vascular disease, which contains a compound of formula 1. |
![2-aza-bicyclo[3,3,0]octane derivatives](http://img.russianpatents.com/img_data/993/9930718-s.gif) 2-aza-bicyclo[3,3,0]octane derivatives / 2478099Invention relates to a 2-aza-bicyclo[3.3.0]octane derivative of formula , with stereogenic centres in a (1S,3S,5S)-configuration, where A is a thiazolyl which is unsubstituted or monosubstituted, where the substitute is independently selected from a group comprising C1-4alkyl, C3-6cycloalkyl and NH2; B is phenyl which is unsubstituted or mono- or disubstituted, where the substitutes are independently selected from a group comprising C1-4alkyl, trifluoromethyl, NHC(O)CH3 and halogen; and R1 is an imidazo[2,1·b]thiazolyl or benzoisoxazolyl group, where said groups are independently unsubstituted or monosubstituted, where the substitutes are independently selected from a group comprising C1-4alkyl; or R1 is a 2,3-dihydrobenzofuranyl group; or a pharmaceutically acceptable salt. The 2-aza-bicyclo[3.3.0]octane derivative of formula (I) is as a medicinal agent having the activity of orexin receptor antagonists. |
 Condensed aminohydrothiazine derivative / 2476431Invention refers to a compound of general formula: |
 Bicyclosulphonyl acid (bcsa) and use thereof as therapeutic agent / 2472784Invention relates to bicyclosulphonyl acid (BCSA) compounds of formula: where: where each of -Rpw, -Rpx, -RPY, and -RPZ independently denotes H or -RRS1; each -RRS1 independently denotes -F, -Cl, -Br, -I, -RA1, -CF3, -OH, -OCF3 or -ORA1; where each RA1 independently denotes C1-4alkyl, phenyl or benzyl; and additionally, two neighbouring -RRS1 groups can together form -OCH2O-, -OCH2CH2O- or -OCH2CH2CH2O-; -RAK independently denotes a covalent bond, -(CH2)- or -(CH2)2-; -RN independently denotes -RNNN, or -LN-RNNN; the rest of the values of the radicals are given in claim 1, which act as inhibitors of inhibitors of tumor necrosis factor-α converting enzyme (TACE). |
![3-aza-bicyclo[3,3,0]octane compounds](http://img.russianpatents.com/img_data/987/9874745-s.gif) 3-aza-bicyclo[3,3,0]octane compounds / 2471796Invention relates to 3-aza-bicyclo[3.3.0]octane derivatives of formula , where R1 and R2 are hydrogen, C1-4alkyl or fluorine; R3 is a phenyl which is unsubstituted, mono- or disubstituted, where the substitutes are independently selected from a group comprising C1-4alkyl, C1-4alkoxy group, trifluoromethyl, trifluoromethoxy group and halogen; 2,3-dihydrobenzofuranyl; 2,3-dihydrobenzo[1,4]dioxynyl; or isoxazolyl, pyridyl, indazolyl, benzofuranyl, benzoxazolyl, benzoisoxazolyl, benzothiazolyl, benzoisothiazolyl, pyrrolo[2,1b]thiazolyl, imidazo[ 1,2-a]pyridinyl or imidazo[2,1-b]thiazolyl, where said groups are unsubstituted, mono- or disubstituted, where the substitutes are independently selected from a group comprising C1-4alkyl, C1-4alkoxy group, halogen and trifluoromethyl; A is or ; R4 is C1-4alkyl or -NR6R7; R6 is hydrogen or C1-4alkyl; R7 is hydrogen or C1-4alkyl; and D is a phenyl which is unsubstituted, mono- or disubstituted, where the substitutes are independently selected from a group comprising C1-4alkyl, C1-4alkoxy group, trifluoromethyl and halogen; or a pharmaceutically acceptable salt of such a compound. 3-aza-bicyclo[3.3.0]octane derivatives or a pharmaceutically acceptable salt thereof are used as a medicinal agent having the activity of orexin receptor antagonists. |
 3-amino-6-(1-aminoethyl)tetrahydropyrane derivatives / 2471795Invention refers to new antibacterial compounds of formula I |
 Compositions for activation of lipoprotein lipase containing benzene derivatives / 2466725Invention refers to an agent for activation of lipoprotein lipase containing a benzene derivative of general formula (1) which is used for preventing and treating hyperlipidemia and obesity. The invention also refers to the benzene derivatives of general formula (1a). |
 Method of producing diamine derivative / 2464271Method is realised by mixing a compound of formula (B) with p-toluenesulphonic acid or a monohydrate of toluenesulphonic acid in less than 1 molar equivalent with respect to the compound of formula (B), in a solvent while heating. An additional amount of p-toluenesulphonic acid or monohydrate of p-toluenesulphonic acid is then added to the mixed solution while cooling in such an amount that their total molar equivalent with p-toluenesulphonic acid or monohydrate of p-toluenesulphonic acid at the mixing step is equal to 1 molar equivalent or more with respect to the compound of formula (B). At the last step, the obtained solution is crystallised to separate a compound of formula (A). |
 Pyrrolo- and thiazolopyridine compounds (versions) and based pharmaceutical composition / 2461557Invention describes the pyrrolo- and thiazolopyridinium compounds and their pharmaceutically acceptable salts covered by general structural formula I: wherein the values A, B, R1, R2, R3, R4, R5, R6, R7 and R8 are those as presented in cl.1, and a pharmaceutical composition based on the given compound for inhibition of hypoxia-inducible factor (HIF) hydroxylase activity. |
 Glucokinase activators / 2457207Invention relates to compounds of formula I , and pharmaceutically acceptable salts thereof, where L denotes O, S, or CH2; Y denotes N or CH; Z denotes CR3; G denotes CH; R1 denotes a heteroaryl ring of formula , where D1 denotes S, O; D2 denotes N or CR12; D3 denotes CR12; R2 denotes (C6-C10)-aryl; 5-9-member mono- or bicyclic heteroaryl with 1 or 2 heteroatoms independently selected from N or S; a saturated or partially saturated (C3-C7)-cycloalkyl; or a saturated 5-6-member heteocyclyl with 1 heteroatom selected from N, where said aryl, heteroaryl, cycloalkyl and heterocyclyl are optionally substituted with one or two groups independently selected from (C1-C6)-alkyl, F, Cl, Br, CF3, CN, NO2, OR6, C(-O)R6, C(=O)OR6, C(=O)NR6R7, saturated 6-member heterocyclyl with 2 heteroatoms independently selected from N or O, and S(O)2R6, and where said alkyl is optionally substituted with one -OR8 group; R3 denotes H; (C1-C6)-alkyl; (C2-C6)-alkenyl; Cl; Br; OR6; SR6; phenyl; or a 6-member heteroaryl with 1 heteroatom selected from N, where said alkyl and alkenyl are optionally substituted with one group selected from C(=O)OR8, -OR8, -NR8R9; or a saturated 6-member heterocyclyl with 1 heteroatom selected from N or O. |
 Method of treating ischemic heart disease with distal or diffuse affection of coronary arteries / 2481839Claimed invention relates to field of medicine, namely to cardiology, and deals with treatment of ischemic heart disease with distal or diffuse affection of coronary arteries. For this purpose 5-oxymethyluracyl in dose 25 mg per kg of weight was introduced 3 times per day during 2 weeks in experiments on male rabbits of Shilshilla breed. |
 Nitrogen-containing aromatic heterocyclic compound / 2481330Invention refers to compounds of general formula (I), wherein A represents a pyrrole group or a pyrazole group, and X represents a carbon atom or a nitrogen atom; R1 represents a carboxy group; R2 independently represents a group specified in a substitute group α; R3 independently represents phenyl(C1-C6alkyl)group substituted by, phenyl(C1-C6alkyl)group (wherein the substitute(s) represents (represent) 1-4 groups independently specified in the substitute group α); m is equal to 0, 1, 2 or 3, n is equal to 0 or 1; each of R4, R5, R6 and R7 independently represents a hydrogen atom, C1-C6alkyl group or a halogen atom; B represents a substituted naphthyl group (wherein the substitute(s) represents (represent) 1-4 groups independently specified in the substitute group α), or the group represented by formula (II), wherein B1, B2 and α are those as specified in the patent claim. Also, the invention refers to a pharmaceutical composition possessing lipolysis inhibiting activity, to the use of the compounds of formula (I) in preparing a drug preparation for treating hyperlipidemia, dislipidemia, abnormal lipid metabolism, arteriosclerosis or type II diabetes mellitus and to a method of treating or preventing the mentioned diseases. |
 Antioxidant / 2481116Invention refers to an antioxidant containing a cyclolanostan derivative selected from 9,19-cyclolanostan-3-ol and 24-methylene-9,19-cyclolanostan-3-ol, and a lophenol derivative selected from 4-methylcholest-7-en-3-ol, 4-methylergost-7-en-3-ol and 4-methylstigmast-7-en-3-ol, in the concentration of min. 0.0001 wt %, as an active ingredient. The invention also concerns a method for preparing the specified antioxidant. The antioxidant may be used as a drug preparation, a food or a beverage, a food additive, a drug preparation for topical skin application. |
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Condensed heterocyclic compound / 2480473 Invention relates to compounds of formula 1 , where X and T are N or C, Q is a (3-7)-member aromatic ring which contains 0-3 nitrogen atoms as ring members, and which is optionally benzo-condensed and is substituted with oxo; C1-C6-alkyl; halogen- C1-C6-alkyl; hydroxy-C1-C6-alkyl; C1-C6-alkoxy; C6-C10-aryl; or a (3-7)-member heteroaryl containing 1-3 oxygen atoms, P is C1-C6-alkyl, optionally substituted with a halogen, and R is a group selected from: (i) -C1-C6-alkyl-R1, (ii) -NR2R3, (iii) -O-R4, (iv) -S-R5, (v) -C (=O))-R6, (vi) optionally substituted (3-7)-member heteroaryl containing 1-4 heteroatoms selected from a nitrogen atom, an oxygen atom and a sulphur atom, (vi) optionally substituted (3-7)-member heteroatom containing 1-4 heteroatoms selected from a nitrogen atom, an oxygen atom and a sulphur atom, (vii) optionally substituted, saturated or partially unsaturated, separate or condensed (3-10)-member heterocyclic ring containing 1-4 heteroatoms selected from a nitrogen atom, an oxygen atom and a sulphur atom, (viii) azido; where each R1, R2, R3, R4, R3, R6, is as described in the claim. The invention also relates to a pharmaceutical composition for preventing and treating a vascular disease, which contains a compound of formula 1. |
 Oral solid dosage form and method of treating / 2480210Present invention refers to an oral solid dosage form containing a therapeutically effective amount of aliskiren or its pharmaceutically acceptable salt wherein an active ingredient makes more than 46 wt % of total weight of the oral dosage form. The oral dosage form is presented in the form of a tablet or a film-coated tablet, and contains an internal phase containting aliskiren or its pharmaceutically acceptable salt, an excipient, a binding agent and a disintegrant, and an external phase containing a disintegrant, an excipient, a glidant and a lubricant. |
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Method for correction of ischemic disorders caused by reperfusion liver injury / 2479872 Correction of ischemic disorders caused by reperfusion liver injury in experiment in white Wistar male rats involves modelling an ischemic and reperfusion liver injury. 30 Minutes before, L-norvalin arginase blocker 10 mg/kg is introduced intraperitoneally, and distant ischemic pre-conditioning is conducted. Then, another dose of L-norvalin arginase blocker is introduced immediately after liver ischemia. |
 Method of treating acute ischemic and hemorrhagic cerebrovascular disease / 2477637Invention refers to medicine and concerns methods of treating acute cerebrovascular disease. A method of treating acute ischemic and hemorrhagic cerebrovascular disease consists in administering a pharmaceutical composition containing a protein-polypeptide complex taken as a biologically active substance and prepared of fast-frozen embryo brain of hoofed farm animals of a gestation term from the middle of the first one-third to the middle of the last one-third of pregnancy, in the amount of 0.05-0.8 mg/day subcutaneously, intramuscularly, intravenously, intranasally and intrathecally. Said protein-polypeptide complex contains negative weak acid neutral proteins and polypeptides referring to growth/differentiation factors, signal molecules, intercellular adhesion molecule, of molecular weights 5 to 200 kD with min. 80% of total weight of proteins having molecular weight 10 to 120 kDa, and characterised nu a peak at UV wave length 274-284 nm and bands at the pi values of 4.2 to 8.4 at isoelectric focusing in 5% polyacrylamide gel. |
 Use of quartenary pyridinium compounds for vasoprotection and/or hepatoprotection / 2477132Invention refers to using a compound of formula (I): |
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Method of early postoperative drug-induced correction of central hemodynamic disorders in oncological patients / 2477128 Invention refers to medicine, namely anaesthesiology, and concerns the early postoperative drug-induced correction of central hemodynamic disorders in oncological patients. That is ensured by measuring a cardiac index (CI), an impact index (II), a LV filling pressure (LVFP), a total peripheral vascular resistance (TPVR), a LV mechanical work index (LVMWI), a systolic blood pressure (SBP); the derived relations of these values in a patient are used to prescribe an individual drug-induced therapy. |
 Capsule and drug preparation for preventing cardiovascular diseases / 2477123Invention refers to pharmaceutical industry, particularly a drug preparation for preventing the development of cardiovascular diseases in individuals of a high-risk group. A capsule for preventing the development of cardiovascular diseases in individuals of a high-risk group which contains acetylsalicylic acid tablets coated by partially hydrolised polyvinyl alcohol (PVA), tablets of simvastatin and pravastatin coated by hydroxypropyl methylcellulose (HPMC) and tablets of lisinopril, ramipril or perindopril coated by partially hydrolised polyvinyl chloride. Using the capsule in producing the drug preparation for preventing the development of cardiovascular diseases in individuals of a high-risk group. |
 5-ht2a- and d3-receptor double modulators / 2480466Invention refers to compounds of general formula |
FIELD: medicine, pharmaceutics.
SUBSTANCE: invention refers to compounds of formula (I) and salts thereof wherein R1 represents -A11-A12-; R2 represents tetrahydrofurylmethyl, tetrahydropyranylmethyl or tetrahydropyranyl; A11 represents a single bond, methylene or 3,2-ethylene; A12 represents C1-6 alkyl, C3-6 cycloalkyl or C3-6 cycloalkyl containing methyl; R3 represents methoxy, cyano, cyclobutyloxymethyl, methoxymethyl or ethoxymethyl; and R4 represents methoxy or chlorine. Also, the invention also refers to a pharmaceutical composition possessing corticotrophin-releasing factor (CRF) receptor antagonist activity, containing a compound of formula (I), to a therapeutic/preventive agent, and a method of treating the diseases specified in the patent claim.
EFFECT: there are presented the compounds of formula (I) as corticotropin-releasing factor (CRF) receptor antagonists.
20 cl, 2 dwg, 2 tbl, 51 ex
The text of the description is given in facsimile form.
1. Connection the following formula (I) or its salt
where R-1 is the formula-And 11-And 12 -; R 2 is , or ; And 11 is a simple link, methylene or 1,2-ethylene; And 12 is C 1-6 alkyl or C 3-6 cycloalkyl, or C 3-6 cycloalkyl containing methyl; R 3 is methoxy, cyano, , or ; and R 4 is methoxy or chlorine.
2. Connection or its salt according to claim 1, wherein R 2 is a -4-yl, -3-yl, (-4-yl)methyl or (tetrahydrofuran-3-yl)methyl.
3. Connection or its salt according to claim 1 or 2, where R 1 is an n-propyl-n-butyl-n-pentyl, , , 2-()ethyl or (2-)methyl.
4. Medicinal and preventive remedy for depression, symptoms of depression, anxiety, irritable syndrome bowel, sleep disorders, insomnia, alcohol dependence, withdrawal symptoms of alcohol, drug dependence, withdrawal symptoms of medicines, functional disorders of the gastrointestinal tract associated with stress, anorexia nervosa, a breach of meal, postoperative , ischemic neuropathy, apoplexy, neuropathy, seizures, epilepsy, hypertension, schizophrenia, bipolar disorder and dementia, containing the connection or its salt according to claim 1.
5. N-Butyl-3-[2,6-dimethoxy-4-()phenyl]-6-methoxy-N-(tetrahydro-2H-PYRAN-4-yl)pyrazolo[5,1-b][1,3]-7-Amin or salt.
6. N-Butyl-3-[4-()-2,6-dimethoxy-phenyl]-6-methoxy-N-(tetrahydro-2H-PYRAN-4-yl)pyrazolo[5,1-b][1,3]-7-Amin or salt.
7. N-(2-)-3-[4-()-2,6-dimethoxy-phenyl]-6-methoxy-N-(tetrahydro-2H-PYRAN-4-yl)pyrazolo[5,1-b][1,3]-7-Amin or salt.
8. 3-[4-()-2,6-dimethoxy-phenyl]-6-methoxy-N-propyl-N-(tetrahydro-2H-PYRAN-3-yl)pyrazolo[5,1-b][1,3]-7-Amin or salt.
9. N-()-3-[2,6-dimethoxy-4-()phenyl]-6-methoxy-N-(tetrahydro-2H-PYRAN-4-yl)pyrazolo[5,1-b][1,3]--7-Amin or salt.
10. N-()-3-[2,6-dimethoxy-4-()phenyl]-6-methoxy-N-(tetrahydro-2H-PYRAN-4-yl)pyrazolo[5,1-b][1,3]-7-Amin or salt.
11. 3-[2,6-Dimethoxy-4-()phenyl]-6-methoxy-N-propyl-N-(tetrahydro-2H-PYRAN-4-yl)pyrazolo[5,1-b][1,3]-7-Amin or salt.
12. 3-[2-Chloro-6-methoxy-4-()phenyl]-6-methoxy-N-propyl-N-(tetrahydro-2H-PYRAN-4-yl)pyrazolo[5,1-b][1,3]-7-Amin or salt.
13. 4-{7-[()(tetrahydrofuran-3-)amino]-6-[5,1-b][1,3]-3-yl}-3,5- or salt.
14. N-()-6-methoxy-N-(tetrahydro-2H-PYRAN-4-)-3-(2,4,6-)pyrazolo[5,1-b][1,3]-7-Amin or salt.
15. Pharmaceutical composition, possessing antagonistic activity against receptor kortikotropin-releasing factor (CRF), which contains connection or its salt on one of claims 1 to 3 as the active ingredient and appropriate supplements.
16. Medicinal and preventive remedy for depression, symptoms of depression, anxiety, or irritable bowel syndrome, containing the connection or its salt on one of claims 1 to 3.
17. Method of treatment or prevention of depression, symptoms of depression, anxiety, irritable bowel syndrome, sleep disorders, insomnia, alcohol dependence, withdrawal symptoms of alcohol, drug dependence, withdrawal symptoms of medicines, functional disorders of the gastrointestinal tract associated with stress, anorexia nervosa, a violation of the meal, postoperative , ischemic neuropathy, apoplexy, neuropathy, seizures, epilepsy, hypertension, schizophrenia, bipolar disorder and dementia, comprising an introduction to the patient compound or its salts one of claims 1 to 3.
18. Method of treatment or prevention of depression, symptoms of depression, anxiety, or irritable bowel syndrome, comprising an introduction to the patient compound or its salts one of claims 1 to 3.
19. Connection or its salt on one of claims 1 and 2 for the treatment or prevention of depression, symptoms of depression, anxiety, irritable bowel syndrome, sleep disorders, insomnia, alcohol dependence, withdrawal symptoms of alcohol, drug dependence, withdrawal symptoms of medicines, functional disorders of the gastrointestinal tract associated with stress, anorexia nervosa, violations of the meal, postoperative , ischemic neuropathy, apoplexy, neuropathy, seizures, epilepsy, hypertension, schizophrenia, bipolar disorder and dementia.
20. Connection or its salt on one of claims 1 and 2 for the treatment or prevention of depression, symptoms of depression, anxiety, or irritable bowel syndrome.