IPC classes for russian patent Benzodiazepine compound and pharmaceutical composition (RU 2496775):
Another patents in same IPC classes:
Iap inhibitors / 2491276
Invention relates to compounds of formula: U 1-M-U 2, where U 1 and U 2 have general formula ![]() (I), where: G stands for: ![]() IVb ![]() IVd ![]() ive, and values M, X 1, X 2, R 2, R 3, R 3', R 4, R 4', R 5, R 5', R 6, R 6', R 7, Z 7, Z 2, Z 3, Z 4, Q 2 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, R 1, R 2, R 3 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 R 1 represents -A 11-A 12-; R 2 represents tetrahydrofurylmethyl, tetrahydropyranylmethyl or tetrahydropyranyl; A 11 represents a single bond, methylene or 3,2-ethylene; A 12 represents C 1-6 alkyl, C 3-6 cycloalkyl or C 3-6 cycloalkyl containing methyl; R 3 represents methoxy, cyano, cyclobutyloxymethyl, methoxymethyl or ethoxymethyl; and R 4 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; C 1-C 6-alkyl; halogen- C 1-C 6-alkyl; hydroxy-C 1-C 6-alkyl; C 1-C 6-alkoxy; C 6-C 10-aryl; or a (3-7)-member heteroaryl containing 1-3 oxygen atoms, P is C 1-C 6-alkyl, optionally substituted with a halogen, and R is a group selected from: (i) -C 1-C 6-alkyl-R 1, (ii) -NR 2R 3, (iii) -O-R 4, (iv) -S-R 5, (v) -C (=O))-R 6, (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 R 1, R 2, R 3, R 4, R 3, R 6, 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 C 1-4alkyl, C 3-6cycloalkyl and NH 2; B is phenyl which is unsubstituted or mono- or disubstituted, where the substitutes are independently selected from a group comprising C 1-4alkyl, trifluoromethyl, NHC(O)CH 3 and halogen; and R 1 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 C 1-4alkyl; or R 1 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.
Bicyclosulphonyl acid (bcsa) and use thereof as therapeutic agent / 2472784
Invention relates to bicyclosulphonyl acid (BCSA) compounds of formula: ![]() where: where each of -R pw, -R px, -R PY, and -R PZ independently denotes H or -R RS1; each -R RS1 independently denotes -F, -Cl, -Br, -I, -R A1, -CF 3, -OH, -OCF 3 or -OR A1; where each R A1 independently denotes C 1-4alkyl, phenyl or benzyl; and additionally, two neighbouring -R RS1 groups can together form -OCH 2O-, -OCH 2CH 2O- or -OCH 2CH 2CH 2O-; -R AK independently denotes a covalent bond, -(CH 2)- or -(CH 2) 2-; -R N independently denotes -R NNN, or -L N-R NNN; 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 R 1 and R 2 are hydrogen, C 1-4alkyl or fluorine; R 3 is a phenyl which is unsubstituted, mono- or disubstituted, where the substitutes are independently selected from a group comprising C 1-4alkyl, C 1-4alkoxy 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 C 1- 4alkyl, C 1-4alkoxy group, halogen and trifluoromethyl; A is ![]() or ![]() ; R 4 is C 1-4alkyl or -NR 6R 7; R 6 is hydrogen or C 1-4alkyl; R 7 is hydrogen or C 1-4alkyl; and D is a phenyl which is unsubstituted, mono- or disubstituted, where the substitutes are independently selected from a group comprising C 1-4alkyl, C 1-4alkoxy 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.
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 R 2 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; R 1 and R 2 are independently specified in a group of substitutes consisting of H, halogen, C 1-8-alkyl, C 1-8-alkylphenyl, C 2-8-alkenyl, OR 5, CON(R 5) 2, SO 2N(R 5) 2, phenyl, if necessary containing up to three substitutes of C 1-4alkyl, halogen or C 1-4alkoxy-groups; R 3 is specified in a group consisting of H, C 1-8-alkyl, OR 5; R 3a represents H, or R 2 and R 3 together represent a five-merous saturated cycle; R 4 is specified in a group consisting of H, C 1-8-alkyl; R 4a represents H, or R 4 and R 4a together represent the substitute -CH 2CH 2-; R 5 is specified in a group consisting of C 1-8-alkyl, or R 5 together with the atom whereto attached represents pyrrolidinyl; or R 1 represents 4-trifluoromethoxyphenyl or 2-trifluoromethylphenyl, then X represents S, and R 2, R 3, R 3a, R 4 and R 4a 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; C 1-C 6-alkyl; halogen- C 1-C 6-alkyl; hydroxy-C 1-C 6-alkyl; C 1-C 6-alkoxy; C 6-C 10-aryl; or a (3-7)-member heteroaryl containing 1-3 oxygen atoms, P is C 1-C 6-alkyl, optionally substituted with a halogen, and R is a group selected from: (i) -C 1-C 6-alkyl-R 1, (ii) -NR 2R 3, (iii) -O-R 4, (iv) -S-R 5, (v) -C (=O))-R 6, (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 R 1, R 2, R 3, R 4, R 3, R 6, 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.
Piperidine derivative / 2475485
Present invention relates to a piperidine derivative of general formula (I)
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; R 1 and R 2 are independently specified in a group of substitutes consisting of H, halogen, C 1-8-alkyl, C 1-8-alkylphenyl, C 2-8-alkenyl, OR 5, CON(R 5) 2, SO 2N(R 5) 2, phenyl, if necessary containing up to three substitutes of C 1-4alkyl, halogen or C 1-4alkoxy-groups; R 3 is specified in a group consisting of H, C 1-8-alkyl, OR 5; R 3a represents H, or R 2 and R 3 together represent a five-merous saturated cycle; R 4 is specified in a group consisting of H, C 1-8-alkyl; R 4a represents H, or R 4 and R 4a together represent the substitute -CH 2CH 2-; R 5 is specified in a group consisting of C 1-8-alkyl, or R 5 together with the atom whereto attached represents pyrrolidinyl; or R 1 represents 4-trifluoromethoxyphenyl or 2-trifluoromethylphenyl, then X represents S, and R 2, R 3, R 3a, R 4 and R 4a 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
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1. Connection benzodiazepine represented by the General formula (1)
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or its pharmaceutically acceptable salt,
where R1, R2, R3and R4each independently is hydrogen or lower alkyl;
R2and R3may be associated with the formation of the lower alkylene;
And1is the lowest alkylene, optionally substituted by one or more hydroxy; and
R5is a group represented by
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where R6and R7each independently is hydrogen, lower alkyl, lower cycloalkyl, phenyl, naphthyl, fullam, teinila, pyrazolyl, oxazolyl, isoxazolyl, thiazolyl, pirrallo, triazolam, pyridium, pyrimidinium, pyridazinyl, pyrazinium, imidazo[2,1-b]what iatlian, thieno[2,3-b]pyrazinium, 2,3-dihydroimidazo[2,1-b]thiazolium, benzothiazolium, indolium, imidazo[1,2-a] pyridium, benzothieno, benzimidazolyl, 2,3-dihydrobenzo[b]fullam, benzofuran, indusrial, furo[2,3-C]pyridium, furo[3,2-C]pyridium, thieno[2,3-C]pyridium, thieno[3,2-C]pyridium, thieno[2,3-b]pyridium, benzo[1,3]dioxolan, benzisoxazole, pyrazolo[2,3-a]-pyridium, indolizinyl, 2,3-dihydroindole, ethanolism, 1,2,3,4-tetrahydro-1H-ethanolism, barbastella, 3,4-dihydroorotase, chinaillon, romaniam, 5,6,7,8-tetrahydroisoquinoline, 3,4-dihydro-1H-ethanolism, naphthyridine, 1,4-benzodioxane, cinnoline, khinoksalinona or 2,3-dihydrobenzo-1,4-oxazinyl, each of which is optionally substituted by one or more substituents selected from the group consisting of the following (4-1)to(4-32):
(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, morpholinyl and lower alkoxy,
(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, optionally substituted by one or bol is e lower alkoxy,
(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, lower alkylsulfonyl and lower alkyl,
(4-17) lower alkylthio,
(4-18) triazolyl,
(4-19) imidazolyl,
(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
(4-25) thiazolyl, optionally substituted by one or more lower alkyl,
(4-26) sulfo,
(4-27) pyridyloxy,
(4-28) lower alkylenedioxy,
(4-29) lower alkanolamine,
(4-30) oxo,
(4-31) morpholinyl and
(4-32) lower alkanoyl;
XAand XBeach is independently a bond, lower alkylene, lower Alcanena, -CO-, -SO2-, -SO2-lower alkylene, -CO-lower alkylene, -CO-lower Alcanena, lower alkylene-N(lower alkyl)-CO-lower alkylene, lower alkylene-N(lower alkyl)-, lower alkylene-M(lower alkyl)-CO - or lower alkylene-O-. 2. Connection benzodiazepine represented by the General formula (1) or its pharmaceutically acceptable salt according to claim 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,
where R6and R7each is one of (4A), (6A), (7a), (15A), (30A), (31A), (32A), (33a), (40A) and (44a):
(4A) phenyl, optionally substituted by one or more substituents selected from the group consisting of (4A-1), (4A-4) and (4A-6):
(4A-1) cyano,
(4A-4) lower alkyl, optionally substituted by one or more halogen, and
(4A-6) pyridyl,
(6A) furil,
(7a) tanila,
(15A) pyridyl, optionally substituted by one or more lower alkyl,
(30A) furo[2,3-C]pyridyl, optionally substituted by one or more oxo,
(31A) furo[3,2-C]pyridyl, optionally substituted by one or more substituents selected from the group consisting of oxo and lower alkyl,
(32A) thieno[2,3-C]pyridyl, optionally substituted by one or more oxo,
(33a) thieno[3,2-C]pyridyl, optionally substituted by one or more oxo,
(40A) izochinolina, optionally substituted by one or more oxo, and
(44a) chinoline, optionally substituted by one or more oxo.
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:
trihydrochloride 1-ethyl-3,3,5-trimethyl-7-{3-[(2-pyridin-3-retil)pyridine-4-ylmethylamino]propoxy}-15-dihydrobenzo[b][1,4]diazepin-2,4-dione,
trihydrochloride 3,3,5-trimethyl-1-propyl-7-{3-[(2-pyridin-3-retil)pyridine-4-ylmethylamino]propoxy}-1,5-dihydrobenzo[b][1,4]diazepin-2,4-dione,
trihydrochloride 1,5 - diethyl-3,3-dimethyl-7-{3-[(2-pyridin-3-retil)pyridine-4-ylmethylamino]propoxy}-1,5-dihydrobenzo[b][1,4]diazepin-2,4-dione,
trihydrochloride 1,3,3,5-tetramethyl-7-{3-[(2-pyridin-3-retil)pyridine-4-ylmethylamino]propoxy}-1,5-dihydrobenzo[b][1,4]diazepin-2,4-dione,
the dihydrochloride of 1-ethyl-3,3,5-trimethyl-7-(3-{[2-(1-oxo-1H-isoquinoline-2-yl)ethyl]pyridine-4-ylmethylamino}propoxy)-1,5-dihydrobenzo[b][1,4]diazepin-2,4-dione,
the dihydrochloride of 1-ethyl-3,3,5-trimethyl-7-(3-{[2-(7-oxo-7H-furo[2,3-C]pyridine-6-yl)ethyl]pyridine-4-ylmethylamino}propoxy)-1,5-dihydrobenzo[b][1,4]diazepin-2,4-dione,
the dihydrochloride of N-methyl-N-(2-{pyridin-4-ylmethyl-[3-(1,3,3,5-tetramethyl-2,4-dioxo-2,3,4,5-tetrahydro-1H-benzo[b][1,4]diazepin-7-yloxy)propyl]amino}ethyl)benzamide,
the dihydrochloride 1,3,3,5-tetramethyl-7-{3-[(2-methylbenzyl)-(2-pyridin-3-retil)amino]propoxy}-1,5-dihydrobenzo[b][1,4]diazepin-2,4-dione,
trihydrochloride 1,3,3,5-tetramethyl-7-{3-[(2-pyridin-3-retil)-(quinoline-4-ylmethyl)amino]propoxy}-1,5-dihydrobenzo[b][1,4]diazepin-2,4-dione,
trihydrochloride 1-ethyl-3,3,5-trimethyl-7-{3-[(3-methylpyridin-4-ylmethyl)-(2-pyridin-3-retil)amino]propoxy}-1,5-dihydrobenzo[b][1,4]diazepin-2,4-dione,
the dihydrochloride of 1-ethyl-3,3,5-trimethyl-7-(3-{[2-(2-oxo-2H-quinoline-1-yl)ethyl]pyridine-4-ylmethylamino}propoxy)-1,5-Digue is drobenko[b][1,4]diazepin-2,4-dione,
the dihydrochloride of 1-ethyl-3,3,5-trimethyl-7-(3-{[2-(7-oxo-7H-thieno[2,3-C] pyridine-6-yl)ethyl] pyridine-4-ylmethylamino}propoxy)-1,5-dihydrobenzo[b][1,4]diazepin-2,4-dione,
4-({[3-(1-ethyl-3,3,5-trimethyl-2,4-dioxo-2,3,4,5-tetrahydro-1H-benzo[b][1,4] diazepin-7-yloxy)propyl]-[2-(1-oxo-1H-isoquinoline-2-yl)ethyl]amino}methyl)benzonitrile,
1-ethyl-3,3,5-trimethyl-7-(3-{[2-(1-oxo-1H-isoquinoline-2-yl)ethyl]thiophene-3-ylmethylamino}propoxy)-1,5-dihydrobenzo[b][1,4]diazepin-2,4-dione,
1-ethyl-7-(3-{furan-2-ylmethyl-[2-(1-oxo-1H-isoquinoline-2-yl)ethyl]amino}propoxy)-3,3,5-trimethyl-1,5-dihydrobenzo[b][1,4]diazepin-2,4-dione,
7-{3-[benzyl-(2-pyridin-3-retil)amino]propoxy}-1-ethyl-3,3,5-trimethyl-1,5-dihydrobenzo[b][1,4]diazepin-2,4-dione,
3-{[[3-(1-ethyl-3,3,5-trimethyl-2,4-dioxo-2,3,4,5-tetrahydro-1H-benzo[b][1,4]diazepin-7-yloxy)propyl]-(2-pyridin-3-retil)amino]methyl}benzonitrile,
1-ethyl-3,3,5-trimethyl-7-{3-[(2-pyridin-3-ylbenzyl)-(2-pyridin-3-retil)amino]propoxy}-1,5-dihydrobenzo[b][1,4]diazepin-2,4-dione,
4-({[3-(1-ethyl-3,3,5-trimethyl-2,4-dioxo-2,3,4,5-tetrahydro-1H-benzo[b][1,4]diazepin-7-yloxy)propyl]-[2-(7-oxo-7H-furo[2,3-C]pyridine-6-yl)ethyl]amino}methyl)benzonitrile,
1-ethyl-3,3,5-trimethyl-7-{3-[[2-(7-oxo-7H-furo[2,3-C]pyridine-6-yl)ethyl]-(4-trifloromethyl)amino]propoxy}-1,5-dihydrobenzo[b][1,4]diazepin-2,4-dione,
1-ethyl-3,3,5-trimethyl-7-(3-{(2-methylbenzyl)-[2-(7-oxo-7H-furo[2,3-C]pyridine-6-yl)ethyl]amino}propoxy)-1,5-dihydrobenzo[b][1,4]diazepin-2,4-dione,
1-ethyl-3,3,5-t is imethyl-7-(3-{[2-(7-oxo-7H-furo[2,3-C]pyridine-6-yl)ethyl]thiophene-2-ylmethylamino}propoxy)-1,5-dihydrobenzo[b][1,4]diazepin-2,4-dione,
the dihydrochloride of 1-ethyl-3,3,5-trimethyl-7-(3-{[2-(2-methyl-4-oxo-4H-furo[3,2-C]pyridine-5-yl)ethyl]pyridine-4-ylmethylamino}propoxy)-1,5-dihydrobenzo[b][1,4]diazepin-2,4-dione,
1-ethyl-3,3,5-trimethyl-7-(3-{[2-(4-oxo-4H-furo[3,2-C]pyridine-5-yl)ethyl]pyridine-3-ylmethylamino}propoxy)-1,5-dihydrobenzo[b][1,4]diazepin-2,4-dione,
1-ethyl-3,3,5-trimethyl-7-(3-{[2-(4-oxo-4H-thieno[3,2-C]pyridine-5-yl)ethyl]pyridine-3-ylmethylamino}propoxy)-1,5-dihydrobenzo[b][1,4]diazepin-2,4-dione,
1-ethyl-3,3,5-trimethyl-7-{3-[[2-(2-methyl-4-oxo-4H-furo[3,2-C]pyridine-5-yl)ethyl]-(4-methylpyridin-3-ylmethyl)amino]propoxy}-1,5-dihydrobenzo[b][1,4]diazepin-2,4-dione,
1-ethyl-3,3,5-trimethyl-7-(3-{(2-methylpyridin-3-ylmethyl)-[2-(4-oxo-4H-furo[3,2-C]pyridine-5-yl)ethyl]amino}propoxy)-1,5-dihydrobenzo[b][1,4]diazepin-2,4-dione,
1-ethyl-3,3,5-trimethyl-7-(3-{(4-methylpyridin-3-ylmethyl)-[2-(4-oxo-4H-furo[3,2-e]pyridine-5-yl)ethyl]amino}propoxy)-1,5-dihydrobenzo[b][1,4]diazepin-2,4-dione,
1-ethyl-3,3,5-trimethyl-7-(3-{(2-methylpyridin-3-ylmethyl)-[2-(4-oxo-4H-thieno[3,2-C]pyridine-5-yl)ethyl]amino}propoxy)-1,5-dihydrobenzo[b][1,4]diazepin-2,4-dione,
the dihydrochloride of 1-ethyl-3,3,5-trimethyl-7-{3-[[2-(2-methyl-4-oxo-4H-furo[3,2-C]pyridine-5-yl)ethyl]-(2-propylpyridine-3-ylmethyl)amino]propoxy}-1,5-dihydrobenzo[b][1,4]diazepin-2,4-dione,
the hydrochloride of N-[3-(1-ethyl-3,3,5-trimethyl-2,4-dioxo-2,3,4,5-tetrahydro-1H-benzo[b][1,4]diazepin-7-yloxy)propyl]-N-(2-pyridin-3-retil)benzosulfimide,
the dihydrochloride of 7-(3-{(2,6-dimethylpyridin the n-3-ylmethyl)-[2-(4-oxo-4H-furo[3,2-C]pyridine-5-yl)ethyl]amino}propoxy)-1-ethyl-3,3,5-trimethyl-1,5-dihydrobenzo[b][1,4]diazepin-2,4-dione,
the hydrochloride of N-[3-(1-ethyl-3,3,5-trimethyl-2,4-dioxo-2,3,4,5-tetrahydro-1H-benzo[b][1,4]diazepin-7-yloxy)propyl]-N-(2-pyridin-3-retil)benzamide and
N-[3-(1-ethyl-3,3,5-trimethyl-2,4-dioxo-2,3,4,5-tetrahydro-1H-benzo[b][1,4]diazepin-7-yloxy)propyl]-N-[2-(1-oxo-1H-isoquinoline-2-yl)ethyl]benzosulfimide.
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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