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Benzodiazepine compound and pharmaceutical composition |
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IPC classes for russian patent Benzodiazepine compound and pharmaceutical composition (RU 2496775):
Iap inhibitors / 2491276
Invention relates to compounds of formula: U1-M-U2, where U1 and U2 have general formula (I), where: G stands for: IVb IVd ive, and values M, X1, X2, R2, R3, R3', R4, R4', R5, R5', R6, R6', R7, Z7, Z2, Z3, Z4, Q2 are given in item 1 of the formula.
5-substituted indazole as kinase inhibitors / 2487873
Present invention refers to compounds of formula (I) or pharmaceutically acceptable salts thereof wherein A, R1, R2, R3 and m are specified in the patent claim. The present invention also refers to the number of specific compounds, and to a pharmaceutical composition containing the above compounds effective for inhibition of kinases, such as glycogen synthase kinase 3 (GSK-3), Rho kinase (ROCK), Janus kinase (JAK), AKT, PAK4, PLK, CK2, KDR, MK2, JNK1, aurora, pim 1 and nek 2.
3-phenylpyrazolo[5,1-b]thiazole derivative / 2482120
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.
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.
2-aza-bicyclo[3,3,0]octane derivatives / 2478099
Invention 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 / 2476431
Invention refers to a compound of general formula:
Bicyclosulphonyl acid (bcsa) and use thereof as therapeutic agent / 2472784
Invention 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 / 2471796
Invention 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 / 2471795
Invention refers to new antibacterial compounds of formula I
Compositions for activation of lipoprotein lipase containing benzene derivatives / 2466725
Invention 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).
Protein tyrosine kinase activity inhibitors / 2495044
Invention refers to a compound of formula (I): and pharmaceutically acceptable salts, diastereoisomers and enantiomers thereof, wherein D is specified in a group consisting of , and , M is ; Z is -O-; Ar is a 6-member aromatic ring system substituted by 0 to 4 R2 groups; and G is or ; the other radical values are presented in cl.1 of the patent claim, as well as to using them for inhibiting protein tyrosine kinase inhibition.
Thienopyridazine compounds, preparing them, pharmaceutical compositions containing them, and using them / 2494103
Invention refers to thienopyridazine compounds of formula (I) and to pharmaceutically acceptable salts and hydrates thereof, wherein R1 and R2 independently mean H or C1-4 alkyl; R3 means a saturated or unsaturated 5- or 6-members ring containing N, S or O, or optical isomers thereof, R4 means phenyl, monosubstituted or disubstituted halogen. The invention also refers to a method for preparing the above compounds and to a pharmaceutical composition for treating and preventing tumour diseases containing the above compounds.
Substituted azepine derivatives, pharmaceutical composition and method of treating diseases, disorders and/or pathological conditions wherein 5ht2c-receptor function modulation is desirable / 2485125
Present invention refers to organic chemistry, namely azepine derivatives of general formula (I) or pharmaceutically acceptable salts thereof, wherein X represents S; R1 and R2 are independently specified in a group of substitutes consisting of H, halogen, C1-8-alkyl, C1-8-alkylphenyl, C2-8-alkenyl, OR5, CON(R5)2, SO2N(R5)2, phenyl, if necessary containing up to three substitutes of C1-4alkyl, halogen or C1-4alkoxy-groups; R3 is specified in a group consisting of H, C1-8-alkyl, OR5; R3a represents H, or R2 and R3 together represent a five-merous saturated cycle; R4 is specified in a group consisting of H, C1-8-alkyl; R4a represents H, or R4 and R4a together represent the substitute -CH2CH2-; R5 is specified in a group consisting of C1-8-alkyl, or R5 together with the atom whereto attached represents pyrrolidinyl; or R1 represents 4-trifluoromethoxyphenyl or 2-trifluoromethylphenyl, then X represents S, and R2, R3, R3a, R4 and R4a represents hydrogen, provided a derivative is other than 8- phenyl-5,6,7,8-tetrahydro-4H-thieno[2,3-d]azepin-3-ol and 2-bromo-8-phenyl-5,6,7,8-tetrahydro-4H-thieno[2,3-d]azepine-3-ol. Also, the invention refers to a pharmaceutical composition of the compounds of formula (I) and a method treating disorders on the basis of the use of the compound of formula (I).
Crystals of prasugrel hydrobromate / 2484094
Invention describes crystals of 2-acetoxy-5-(α-cyclopropylcarbonyl-2-fluorobenzyl)-4,5,6,7-tetrahydrothieno[3,2-c]pyridine (prasugrel) hydrobromate, comprisions of crystals and pharmaceutical compositions containing them for preventing and treating the diseases associated with thrombus or embolism in an animal.
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.
Thieno[3,2-c]pyridine derivatives as kinase inhibitors for use in cancer treatment / 2480472
Compound is N-(4-{4-amino-7-[1-(2-hydroxyethyl)-1H-pyrazol-4-yl]thieno[3,2-c]pyridin-3-yl}phenyl-N'-(3-fluorophenyl)urea, N-(4-{4-amino-7-[1-(2-hydroxyethyl)-1H-pyrazol-4-yl]thieno[3,2-c]pyridin-3-yl}phenyl-N'-[4-(difluoromethoxy)phenyl]urea, N-[4-(4-amino-7-{l-[(2S)-2-hydroxypropyl)-1H-pyrazol-4-yl}thieno[3,2-c]pyridin-3-yl)phenyl]-N'-(3-methylphenyl)urea, N-(4- {4-amino-7-[1-(2-hydroxy-2-methylpropyl)-1H-pyrazol-4-yl]thieno[3,2-c]pyridin-3-yl}phenyl-N'-(4-methoxyphenyl)urea, N-[4-(4-amino-7-{1-[(2S)-2,3-dihydroxypropyl)-1H-pyrazol-4-yl}thieno[3,2-c]pyridin-3-yl)phenyl]-N'-(4-methoxyphenyl) or therapeutically acceptable salts thereof. A pharmaceutical composition based on said compounds is also disclosed.
N-acylated 3-amino-4,6-dimethylthieno[2,3-b]pyridine-2-carboxamides as antidotes of 2,4-d on sunflower / 2475490
Invention relates to N-acylated 3-amino-4,6-dimethyl-thieno[2,3-b]pyridine-2-carboxamides, which exhibit antidote activity on 2,4-dichlorophenoxyacetic acid on sunflower.
Piperidine derivative / 2475485
Present invention relates to a piperidine derivative of general formula (I)
Therapeutic agent on pyrroline derivates for prevention of tumorous cell death, method for preparing it and method for using it / 2473551
Invention refers to compound presented by Formula
Intracellular calcium modulating compounds / 2472791
Invention relates to compounds of formula (I): where: A, J, R1, R4, X, Z are given in claim 1, and to a pharmaceutical composition containing such compounds, which modulate activity of store-operated calcium (SOC) channels. The present invention also describes methods of using such SOC channel modulators to treat diseases or conditions where inhibition of activity of SOC channels can be beneficial.
Substituted azepine derivatives, pharmaceutical composition and method of treating diseases, disorders and/or pathological conditions wherein 5ht2c-receptor function modulation is desirable / 2485125
Present invention refers to organic chemistry, namely azepine derivatives of general formula (I) or pharmaceutically acceptable salts thereof, wherein X represents S; R1 and R2 are independently specified in a group of substitutes consisting of H, halogen, C1-8-alkyl, C1-8-alkylphenyl, C2-8-alkenyl, OR5, CON(R5)2, SO2N(R5)2, phenyl, if necessary containing up to three substitutes of C1-4alkyl, halogen or C1-4alkoxy-groups; R3 is specified in a group consisting of H, C1-8-alkyl, OR5; R3a represents H, or R2 and R3 together represent a five-merous saturated cycle; R4 is specified in a group consisting of H, C1-8-alkyl; R4a represents H, or R4 and R4a together represent the substitute -CH2CH2-; R5 is specified in a group consisting of C1-8-alkyl, or R5 together with the atom whereto attached represents pyrrolidinyl; or R1 represents 4-trifluoromethoxyphenyl or 2-trifluoromethylphenyl, then X represents S, and R2, R3, R3a, R4 and R4a represents hydrogen, provided a derivative is other than 8- phenyl-5,6,7,8-tetrahydro-4H-thieno[2,3-d]azepin-3-ol and 2-bromo-8-phenyl-5,6,7,8-tetrahydro-4H-thieno[2,3-d]azepine-3-ol. Also, the invention refers to a pharmaceutical composition of the compounds of formula (I) and a method treating disorders on the basis of the use of the compound of formula (I).
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FIELD: medicine, pharmaceutics. SUBSTANCE: there are described new benzodiazepine compounds of general formula , wherein each R1, R2, R3 and R4 independently represent hydrogen or alkyl, or R2 and R3 together represent lower alkylene; A1 is lower alkylene optionally substituted by hydroxy; and R5 is a fragment of formula , wherein each R6 and R7 independently represents hydrogen, lower alkyl, cycloalkyl, phenyl, furyl, thienyl, pyrazolyl, etc.; each XA and XB independently represents a bond, lower alkylene, -CO-, -SO2- etc., a pharmaceutical composition containing them, and using the above compound as the pharmaceutical composition or for preparing the same. EFFECT: new compounds may be used for preventing and treating cardiac arrhythmia. 8 cl, 1047 ex, 78 tbl
The text descriptions are given in facsimile form. 1. Connection benzodiazepine represented by the General formula (1) where R6and R7each is one of (1)to(52): (1) hydrogen, (2) lower alkyl, (3) lower cycloalkyl, (4) phenyl, optionally substituted by one or more substituents selected from the group consisting of (4-1)to(4-25): (4-1) cyano, (4-2) hydroxy, (4-3) halogen, (4-4) lower alkyl, optionally substituted by one or more substituents selected from the group consisting of halogen, imidazolyl and morpholinyl, (4-5) lower alkoxy, optionally substituted by one or more substituents selected from the group consisting of amino and lower alkylamino, (4-6) pyridyl, (4-7) tanila, (4-8) piperazinil, optionally substituted by one or more lower alkyl, (4-9) phenyl, (4-10) pyrazolyl, optionally substituted by one or more lower alkyl, (4-11) pyrimidinyl, optionally substituted by one or more lower alkyl, (4-12) piperidyl, optionally substituted by one or more lower alkyl, (4-13) furil, (4-14) carboxy, (4-15) lower alkoxycarbonyl, (4-16) amino, optionally substituted by one or more substituents selected from the group consisting of lower alkanoyl and lower alkylsulfonyl, (4-17) lower alkylthio, (4-18) triazolyl, (4-19) them is Azolla, (4-20) pyrrolidinyl, optionally substituted by one or more oxo, (4-21) lower alkylsulfonyl, (4-22) lower alkylenedioxy, optionally substituted by one or more halogen, (4-23) nitro, (4-24) oxazolyl, and (4-25) thiazolyl, optionally substituted by one or more lower alkyl, (5) naphthyl, (6) furil, optionally substituted by one or more substituents selected from the group consisting of lower alkyl, optionally substituted with halogen, carboxy, sulfo, pyridyloxy, lower alkoxycarbonyl and phenyl, (7) tanila, optionally substituted by one or more substituents selected from the group consisting of lower alkyl, lower alkylenedioxy, carboxy, halogen, pyridyl, lower alkoxy, lower alkoxycarbonyl, oxazolyl and Furie, (8) imidazolyl, optionally substituted by one or more substituents selected from the group consisting of phenyl, lower alkyl and halogen, (9) pyrazolyl, optionally substituted by one or more substituents selected from the group consisting of lower alkyl, optionally substituted with halogen, halogen, phenyl, optionally substituted lower alkoxy, purile and tanila, (10) oxazolyl, optionally substituted by one or more substituents selected from the group consisting of lower alkyl and phenyl, (11) isoxa olila, optionally substituted by one or more substituents selected from the group consisting of phenyl, lower alkyl, tanila and Furie, (12) thiazolyl, optionally substituted by one or more substituents selected from the group consisting of lower alkyl, optionally substituted lower alkoxy, phenyl and lower alkanolamine, (13) pyrrolyl, optionally substituted by one or more substituents selected from the group consisting of lower alkyl and lower alkoxycarbonyl, (14) triazolyl, optionally substituted by one or more lower alkyl, (15) pyridyl, optionally substituted by one or more substituents selected from the group consisting of lower alkyl, optionally substituted with halogen, oxo, hydroxy, lower alkoxy, halogen, pyrrolidinyl, morpholinyl and tanila, (16) pyrimidinyl, optionally substituted by one or more substituents selected from the group consisting of lower alkyl and phenyl, (17) pyridazinyl, (18) pyrazinyl, (19) imidazo[2,1-b]thiazolyl, optionally substituted by one or more halogen, (20) thieno[2,3-b]pyrazinyl, (21) 2,3-dihydroimidazo[2,1-b]thiazolyl, optionally substituted by one or more phenyl, (22) benzothiazolyl, optionally substituted by one or more lower alkyl, (23) indolyl, optionally substituted by one who does more substituents, selected from the group consisting of lower alkyl, lower alkanoyl and halogen, (24) imidazo[1,2-a]pyridyl, optionally substituted by one or more lower alkyl, (25) benzothieno, optionally substituted by one or more lower alkyl, (26) benzimidazolyl, optionally substituted by one or more lower alkyl, (27) 2,3-dihydrobenzo[b]Furie, (28) benzofuran, optionally substituted by one or more halogen, (29) indazole, optionally substituted by one or more lower alkyl, (30) furo[2,3-C]pyridyl, optionally substituted by one or more substituents selected from the group consisting of oxo and lower alkyl, (31) furo[3,2-C]pyridyl, optionally substituted by one or more substituents selected from the group consisting of oxo, lower alkyl, optionally substituted with halogen, halogen, furil, pyridyl and phenyl, optionally substituted by one or more lower alkoxy, (32) thieno[2,3-e]pyridyl, optionally substituted by one or more substituents selected from the group consisting of a carbonyl group and lower alkyl, (33) thieno[3,2-C]pyridyl, optionally substituted by one or more substituents selected from the group consisting of oxo and lower alkyl, (34) thieno[2,3-b]pyridyl, (35) benzo[1,3]dioxole, optionally substituted by one or more halogen,br/> (36) benzisoxazole, (37) pyrazolo[2,3-a]pyridyl, (38) indolizinyl, (39) 2,3-dihydroindole, optionally substituted by one or more substituents selected from the group consisting of oxo, lower alkyl and lower alkanoyl, (40) izochinolina, optionally substituted by one or more substituents selected from the group consisting of lower alkyl, halogen and oxo, (41) 1,2,3,4-tetrahydro-1H-izochinolina, optionally substituted by one or more oxo, (42) barbastella, optionally substituted by one or more lower alkoxy, (43) 3,4-dihydroorotase, optionally substituted by one or more lower alkoxy, (44) chinoline, optionally substituted by one or more substituents selected from the group consisting of amino, optionally substituted by one or two lower alkyl, lower alkoxy, lower alkyl and oxo, (45) Romania, optionally substituted by one or more lower alkyl, (46) 5,6,7,8-tetrahydroisoquinoline, optionally substituted by one or more oxo, (47) 3,4-dihydro-1H-izochinolina, optionally substituted by one or more oxo, (48) naphthyridine, (49) 1,4-benzodioxane, (50) cinnoline, (51) khinoksalinona, or (52) 2,3-dihydrobenzo-1,4-oxazinyl, optionally substituted by one or more substituents selected from the group consisting of lower alkyl and the CSR. 3. Connection benzodiazepine represented by the General Formula (1) or its pharmaceutically acceptable salt according to claim 2, 4. Connection benzodiazepine represented by the General formula (1) or its pharmaceutically acceptable salt according to claim 2, which is chosen from the group consisting of the following compounds: 5. Pharmaceutical composition for prevention and/or treatment of arrhythmia, containing the compound of the benzodiazepine represented by the Formula (1), or its pharmaceutically acceptable salt according to claim 1 and a pharmacologically acceptable carrier. 6. Connection benzodiazepine represented by the Formula (1)or its salt according to claim 1 for use in pharmaceutical compositions for the prevention and/or treatment of arrhythmia. 7. Application connection benzodiazepine represented by the Formula (1), or its pharmaceutically acceptable salt according to claim 1 as a pharmaceutical composition for prevention and/or treatment of arrhythmia. 8. Application connection benzodiazepine represented by the Formula (1), or its pharmaceutically acceptable salt according to claim 1 to obtain a pharmaceutical composition for prevention and/or treatment of arrhythmia.
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