http://rdf.ncbi.nlm.nih.gov/pubchem/patent/ES-2628005-T3

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publicationDate 2017-08-01-04:00^^<http://www.w3.org/2001/XMLSchema#date>
publicationNumber ES-2628005-T3
titleOfInvention 2,3-Benzodiazepines
abstract Compounds of general formula I ** Formula ** A in which X represents an oxygen or sulfur atom, and A represents a monocyclic heteroaryl ring with 5 or 6 ring atoms or represents a phenyl ring, and R1a represents hydrogen , halogen, cyano, carboxy, amino or aminosulfonyl, or represents a C1-C6 alkoxy, C1-C3 alkoxy-C1-C3 alkyl, C1-C3 alkoxy-C2-C3 alkoxy, C1-C6-alkyl alkyl, C1- alkyl C6-carbonylamino, C1-C6 alkyl-amino-C1-C6 alkyl, N- (heterocyclyl) -C1-C6 alkyl, N- (heterocyclyl) -C1-C6 alkoxy, hydroxy-C1-C6 alkyl, hydroxy-C1-alkoxy C6, halo-C1-C6 alkyl, halo-C1-C6 alkoxy, C1-C6 alkylcarbonyl or C1-C6 alkoxycarbonyl, or represents a monocyclic heterocyclyl moiety with 3 to 8 ring atoms which may be substituted if necessary or several times, in the same or different manner, with halogen, cyano, nitro, hydroxy, amino, oxo, carboxy, C1-C6 alkyl, C1-C6 alkoxy, C1-C6 alkoxy-C1-C6 alkyl, hydroxy-C1- alkyl C6, C1-C6 alkyl-amino, amino -C1-C6 alkyl, C1-C6 alkyl-amino-C1-C6 alkyl, halo-C1-C6 alkyl, halo-C1-C6 alkoxy, C3-C10 cycloalkyl, phenyl, halophenyl, phenyl-C1-C6 alkyl, pyridinyl, -NR6C (> = O) -R9, -C (> = O) -NR6R7, -C (> = O) -R8, -S (> = O) 2-NR6R7, -S (> = O) -R9 , -S (> = O) 2-R9, -NH-S (> = O) 2-R9 and / or a monocyclic heterocyclyl moiety with 3 to 8 ring atoms, or represents a monocyclic heteroaryl moiety with 5 or 6 atoms If necessary, it may be substituted once or several times, in the same or different manner, with halogen, hydroxy, amino, cyano, nitro, carboxy, C1-C6 alkyl, C1-C6 alkoxy, C1-C6 alkoxy-C1 alkyl -C6, C1-C6-amino alkyl, amino-C1-C6 alkyl, C1-C6 alkyl-amino-C1-C6 alkyl, halo-C1-C6 alkyl, halo-C1-C6 alkoxy, C3-C10 cycloalkyl, -C (> = O) -NR6R7, -C (> = O) -R8, -S (> = O) 2-NR6R7, -S (> = O) -R9, - S (> = O) 2-R9, -NH-S (> = O) 2-R9 and / or with a monocyclic heterocyclyl moiety with 3 to 8 ring atoms, and / or with a monocyclic heteroaryl moiety with 5 or 6 ring atoms, and / or with a moiety phenyl, how are you It may be substituted, if necessary, once or several times, in the same or different manner, with halogen, C1-C3 alkyl and / or C1-C3 alkoxy, or represents a phenyl moiety which may be substituted once or several times. , in the same or different manner, with halogen, amino, hydroxy, cyano, nitro, carboxy, C1-C6 alkyl, C1-C6 alkoxy, C1-C6 alkoxy-C1-C6 alkyl, C1-C6-amino alkyl, amino-alkyl C1-C6, C1-C6 alkyl-amino-C1-C6 alkyl, -C (> = O) NR6R7, -C (> = O) R8, C1-C3 alkyl sulfinyl, C1-C3 alkyl sulfonyl, -S (> = O) 2NH2, C1-C3-sulfonylamino alkyl, C1-C3-aminosulfonyl alkyl, C3-C6-aminosulfonyl cycloalkyl, halo-C1-C6 alkyl, halo-C1-C6 alkoxy, hydroxy-C1-C6 alkyl, cycloalkyl C3-C10 and / or a monocyclic heterocyclyl moiety with 3 to 8 ring atoms and / or a monocyclic heteroaryl moiety with 5 or 6 ring atoms, which in turn may be substituted once or several times, in the same manner or different, with halogen, C1-C3 alkyl and / or C1-C3 alkoxy, and R1b and R1c repre sit independently of each other hydrogen, halogen, hydroxy, cyano, nitro and / or represent a C1-C6 alkyl, C1-C6 alkoxy, C1-C6 alkoxy-C1-C6 alkyl, halo-C1-C6 alkyl, halo- C1-C6 alkoxy, C3-C10 cycloalkyl and / or a monocyclic heterocyclyl moiety with 3 to 8 ring atoms, and R2 represents a C1-C3 alkyl or trifluoromethyl or C3 or C4 cycloalkyl moiety, and R3 represents cyclopropyl, C1-C3 alkyl , C1-C3 alkoxy, amino, cyclopropylamino or C1-C3-amino alkyl, and R4 and R5 represent, independently of each other, hydrogen, hydroxy, cyano, nitro, amino, aminocarbonyl, fluorine, chlorine, bromine, C1-C6 alkyl, C1-C6 alkoxy, C1-C6-amino alkyl, C1-C6-carbonylamino alkyl, C1-C6-aminocarbonyl alkyl or C1-C6-aminosulfonyl alkyl, or represent C1-C6 alkyl, C1-C6 alkoxy, C1-C6 alkyl- amino, C1-C6 alkylcarbonylamino, C1-C6 alkyl aminocarbonyl or C1-C6 alkyl aminosulfonyl which may be substituted once or several times, equally or differently, with halo geno, amino, hydroxy, carboxy, hydroxy-C1-C6 alkyl, C1-C6 alkoxy, C1-C6 alkoxy-C1-C6-alkyl, amino-C1-C6 alkyl, monocyclic heterocyclyl with 3 to 8 monocyclic ring and / or heteroaryl atoms with 5 or 6 ring atoms, the monocyclic heterocyclyl and heteroaryl moieties being mentioned may be substituted once with C1-C3 alkyl, or represent C3-C10 cycloalkyl where appropriate it can be substituted once or several times, in the same or different manner, with halogen, amino, hydroxy, carboxy, C1-C6 alkyl, C1-C6 alkoxy, C1-C6 alkoxy-C1-C6 alkyl, C1-C6-alkyl alkyl, amino-C1-C6 alkyl, C1-C6 alkyl-amino-C1-C6 alkyl, halo-C1-C6 alkyl, halo-C1-C6 alkoxy and / or a monocyclic heterocyclyl moiety with 3 to 8 ring atoms, or represent heteroaryl monocyclic with 5 or 6 ring atoms that may be substituted once or several times, in the same or different way, with halogen, amino, hydroxy, cyano, nitro, carb oxy, C1-C6 alkyl, C1-C6 alkoxy, C1-C6 alkoxy-C1-C6 alkyl, hydroxy-C1-C6 alkyl, C1-C6-amino alkyl, amino C1-C6 alkyl, C1-C6-amino alkyl C1-C6 alkyl, halo-C1-C6 alkyl, halo-C1-C6 alkoxy, C3-C10 cycloalkyl, -C (> = O) R8, -S (> = O) 2R9, -NR6R7 and / or a heterocyclyl moiety monocyclic with 3 to 8 ring atoms, or represent monocyclic heterocyclyl with 3 to 8 ring atoms that may be substituted once or several times, in the same or different way, with halogen, amino, hydroxy, cyano, oxo, carboxy , C1-C6 alkyl, C1-C6 alkoxy, C1-C6 alkoxy-C1-C6 alkyl, amino C1-C6 alkyl, amino C1-C6 alkyl, C1-C6 alkyl-amino-C1-C6 alkyl, hydroxy-alkyl C1-C6, halo-C1-C6 alkyl, halo-C1-C6 alkoxy, C3-C10 cycloalkyl, -C (> = O) R8, -S (> = O) 2R9, -NR6R7 and / or a monocyclic heterocyclyl moiety with 3 to 8 ring atoms, or represent phenyl which may be substituted once or several times, in the same or different manner, with halogen, amino, hydroxy, cyano, nitro, c arboxy, C1-C6 alkyl, C1-C6 alkoxy, C1-C6 alkoxy-C1-C6 alkyl, amino C1-C6 alkyl, amino C1-C6 alkyl, C1-C6-aminocarbonyl alkyl, C1-C6-aminosulfonyl alkyl, C1-C6-alkyl-C1-C6-alkyl, hydroxy-C1-C6-alkyl, halo-C1-C6-alkyl, halo-C1-C6-alkoxy, C3-C10-cycloalkyl and / or a monocyclic heterocyclyl moiety having 3 to 8 atoms of ring, and R6 and R7 independently represent hydrogen, C1-C3 alkyl, cyclopropyl, di-C1-C3-alkyl-C1-C3 alkyl or fluoropyridyl, and R8 represents hydroxy, C1-C6 alkyl, halo-alkyl C1-C3, hydroxy-C1-C3 alkyl, C1-C3 alkoxy-C1-C3 alkyl, C3-C8 cycloalkyl, phenyl, monocyclic heterocyclyl with 3 to 8 ring atoms or monocyclic heteroaryl with 5 or 6 ring atoms, being able to be phenyl, heteroaryl and heterocyclyl if necessary substituted once or twice with halogen, C1-C3 alkoxy or C1-C3 alkyl, and R9 represents hydrogen, C1-C6 alkyl or C1-C4 alkoxy, as well as their polymorphs, enantiomers, diastereome ros, racemates, tautomers, solvates, physiologically acceptable salts and solvates of these salts, with the proviso that if A represents a phenyl ring and R4 and R5 represent, independently of each other, hydrogen, hydroxy, cyano, nitro, amino, aminocarbonyl , fluorine, chlorine, bromine, C1-C6 alkyl, C1-C6 alkoxy, C1-C6-amino alkyl, C1-C6 alkylcarbonylamino, C1-C6-alkylcarbonyl or C1-C6-aminosulfonyl alkyl, or represent C1- alkyl C6, C1-C6 alkoxy, C1-C6-amino alkyl, C1-C6 alkylcarbonylamino, C1-C6-aminocarbonyl alkyl or C1-C6-aminosulfonyl alkyl which may be substituted once or several times, equally or different, with halogen, amino, hydroxy, carboxy, hydroxy-C1-C6 alkyl, C1-C6 alkoxy, C1-C6 alkoxy-C1-C6 alkyl, C1-C6-amino alkyl, amino-C1-C6 alkyl, monocyclic heterocyclyl with 3 to 8 monocyclic ring and / or heteroaryl atoms with 5 or 6 ring atoms, the monocyclic heterocyclyl and heteroaryl moieties being m in turn, when substituted once with C1-C3 alkyl, R1a does not represent hydrogen, halogen, cyano, carboxy, amino or aminosulfonyl, or represents a C1-C6 alkoxy, C1-C3 alkoxy-C1-C3 alkyl moiety, C1-C3 alkoxy-C2-C3 alkoxy, C1-C6-amino alkyl, C1-C6 alkylcarbonylamino, C1-C6 alkyl-C1-C6 alkyl, N- (heterocyclyl) -C1-C6 alkyl, N- ( heterocyclyl) -C1-C6 alkoxy, hydroxy-C1-C6 alkyl, hydroxy-C1-C6 alkoxy, halo-C1-C6 alkyl, halo-C1-C6 alkoxy, C1-C6 alkylcarbonyl or C1-C6 alkoxycarbonyl, and the condition not comprising those compounds of general formula (I) in which A represents phenyl and R4 represents hydrogen, fluorine, chlorine or bromine and R5 represents C1-C6 alkoxy that is substituted once or several times, in the same or different manner, with halogen and R1a represents halogen, and neither those compounds of general formula (I) in which A represents phenyl and R4 represents hydrogen and R5 represents C1-C6 alkoxy which is substituted once or several times , in the same or different manner, with a monocyclic heterocyclyl moiety with 3 to 8 ring atoms and / or a monocyclic heteroaryl moiety with 5 or 6 ring atoms, the monocyclic heterocyclyl and heteroaryl moieties may be mentioned as the case may be substituted once with C1-C3 alkyl, and R1a represents halogen.
priorityDate 2012-08-16-04:00^^<http://www.w3.org/2001/XMLSchema#date>
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Total number of triples: 84.