| 主权项 |
1. A compound of formula I wherein X denotes CH, m, n, o independently of each other denote 1, wherein the bicyclic azacycloalkene core structure of formula I annelated with ring A and attached to the carbonyl group is optionally substituted with 3 to 5 substituents independently of each other selected from the group consisting of R11 and R12, A denotes a benzo ring, which is optionally substituted with one to four substituents independently of each other selected from R1 or wherein 2 adjacent C-atoms are optionally substituted with R2 and R3 and one or two carbon atoms are optionally substituted independently with substituents selected from R1;
and B denotes a cyclohexyl group, and
wherein said cyclohexyl B group is substituted with one or more substituents independently of each other selected from L1, and wherein said cyclohexyl B group optionally is substituted with 1 or 2 substituents independently of each other selected from L2, andwherein 2 adjacent C-atoms of said cyclohexyl B group optionally are substituted with L3 and L4, andwherein 2 adjacent C-atoms of said cyclohexyl B group optionally are substituted with L5 and L6, with the proviso that two of L3 to L6 are not attached to the same carbon atom; RN independently of each other denotes hydrogen, C1-6-alkyl, C3-6-alkenyl, C3-6-alkynyl, C3-6-cycloalkyl, (het)aryl, C1-4-alkylcarbonyl, C1 -4-alkyloxycarbonyl, C1-4-alkylaminocarbonyl, di-(C1-3-alkyl)aminocarbonyl, C1-4-alkylsulfonyl, (het)arylcarbonyl, (het)arylaminocarbonyl, or (het)arylsulfonyl,
wherein each alkyl, alkenyl, and alkynyl group optionally is mono- or polysubstituted with fluorine, and optionally is monosubstitued with hydroxy, C1-4-alkoxy, C1-4-alkylsulfanyl, C1-4-alkylsulfinyl, C1-4-alkylsulfonyl, amino, C1-4-alkylamino, di-(C1-4-alkyl)amino, C1-4-alkylcarbonylamino, cyano, carboxy, C1-4-alkoxycarbonyl, aminocarbonyl, C1-4-alkylaminocarbonyl, di-(C1-4-alkyl)aminocarbonyl, or (het)aryl, R1 denotes fluorine, chlorine, bromine, iodine, cyano, nitro, C1-4-alkyl, hydroxy, C1-4-alkyloxy, C3-6-alkenyloxy, difluoromethyl, trifluoromethyl, difluoromethoxy, trifluoromethoxy, 2,2,2-trifluoro-1-hydroxyethyl, 2,2,2-trifluoro-1-hydroxy-1-methylethyl, 2,2,2-trifluoro-1-hydroxy-1-(trifluoromethyl)ethyl, C3-6-cycloalkyl, C3-6-cycloalkyloxy, C3-6-cycloalkyl-C1-3-alkyl, C3-6-cycloalkyl-C1-3-alkyloxy, tetrahydrofuran-3-yloxy, tetrahydropyran-3-yloxy, tetrahydropyran-4-yloxy, tetrahydrofuranyl-C1-3-alkyloxy, tetrahydropyranyl-C1-3-alkyloxy, (het)aryl, (het)aryloxy, (het)aryl-C1-3-alkyl, (het)aryl-C1-3-alkyloxy, (het)aryloxy-C1-3-alkyl, C1-3-alkyl-carbonyl, (het) aryl-carbonyl,
amino, C1-3-alkylamino, di-(C1-3-alkyl)amino, pyrrolidin-1-yl, 2-oxo-pyrrolidin-1-yl, piperidin-1-yl, 2-oxo-piperidin-1-yl, morpholin-4-yl, 3-oxo-morpholin-4-yl, piperazin-1-yl, 2-oxo-piperazin-1-yl, 3-oxo-piperazin-1-yl, 4-(C1-3-alkyl)-piperazin-1-yl, 4-(C1-4-alkylcarbonyl)-piperazin-1-yl, 4-(C3-6-cycloalkylcarbonyl)-piperazin-1-yl, 4-(C1-4-alkyloxycarbonyl)-piperazin-1-yl, 4-(C1-4-alkylsulfonyl)-piperazin-1-yl, 2-oxo-4-(C1-3-alkyl)-piperazin-1-yl, 3-oxo-4-(C1-3-alkyl)-piperazin-1-yl,C1-3-alkyl-carbonylamino, (het)aryl-carbonylamino, (het)aryl-C1-3-alkyl-carbonyl-amino, C1-3-alkyloxy-carbonylamino, aminocarbonylamino, C1-3-alkyl-amino-carbonylamino, di-(C1-3-alkyl)aminocarbonylamino, pyrrolidin-1-yl-carbonylamino, piperidin-1-yl-carbonylamino, morpholin-4-yl-carbonylamino, piperazin-1-yl-carbonylamino, 4-(C1-3-alkyl)-piperazin-1-yl-carbonylamino, C1-3-alkyl-sul-fonylamino, aminosulfonylamino, C1-3-alkylamino-sulfonylamino, di-(C1-3-alkyl)-amino-sulfonylamino, pyrrolidin-1-yl-sulfonylamino, piperidin-1-yl-sulfonylamino, morpholin-4-yl-sulfonylamino, piperazin-1-yl-sulfonylamino, 4-(C1-3-alkyl)-piperazin-1-yl-sulfonylamino, (C1-3-alkyloxy-carbonylamino)carbonylamino, (het)arylsulfonylamino, (het)aryl-C1-3-alkyl-sulfonylamino,N—(C1-3-alkyl)-C1-3-alkyl-carbonylamino, N—(C1-3-alkyl)-(het) arylcarbonylamino, N—(C1-3-alkyl)-(het)aryl-C1-3-alkyl-carbonylamino, N—(C1-3-alkyl)-C1-3-alkyloxy-carbonylamino, N-(aminocarbonyl)-C1-3-alkylamino, N—(C1-3-alkyl-aminocarbonyl)-C1-3-alkylamino , N—[di-(C1-3-alkyl) aminocarbonyl]-C1-3-alkylamino,N—(C1-3-alkyl)-C1-3-alkyl-sulfonylamino, N—(C1-3-alkyl)-(het)arylsulfonylamino, N—(C1-3-alkyl)-(het)aryl-C1-3-alkyl-sulfonylamino,oxo-imidazolidin-1-yl, 2,4-dioxo-imidazolidin-1-yl, 2,5-dioxo-imidazolidin-1-yl, 2-oxo-hexahydropyrimidin-1-yl, wherein the nitrogen atom in position 3 of the aforementioned groups is optionally substituted with methyl or ethyl,(hydroxyimino)aminomethyl, (C1-3-alkyloxyimino)aminomethyl, carboxy, C1-3-alkyloxy-carbonyl, aminocarbonyl, C1-3-alkyl-aminocarbonyl, di-(C1-3-alkyl)-aminocarbonyl, pyrrolidin-1-yl-carbonyl, piperidin-1-yl-carbonyl, morpholin-4-yl-carbonyl, piperazin-1-yl-carbonyl, 4-(C1-3-alkyl)-piperazin-1-yl-carbonyl,carboxy-C1-3-alkyl, C1-3-alkyloxy-carbonyl-C1-3-alkyl, cyano-C1-3-alkyl, aminocarbonyl-C1-3-alkyl, C1-3-alkyl-aminocarbonyl-C1-3-alkyl , di-(C1-3-alkyl)-aminocarbonyl-C1-3-alkyl, pyrrolidin-1-yl-carbonyl-C1-3-alkyl, piperidin-1-yl-carbonyl-C1-3-alkyl, morpholin-4-yl-carbonyl-C1-3-alkyl, piperazin-1-yl-carbonyl-C1-3-alkyl, 4-(C1-3-alkyl)-piperazin-1-yl-carbonyl-C1-3-alkyl,carboxy-C1-3-alkyloxy, C1-3-alkyloxy-carbonyl-C1-3-alkyloxy, cyano-C1-3-alkyloxy, aminocarbonyl-C1-3-alkyloxy, C1-3-alkyl-aminocarbonyl-C1-3-alkyloxy, di-(C1-3-alkyl)-aminocarbonyl-C1-3-alkyloxy, pyrrolidin-1-y1-carbonyl-C1-3-alkyl-oxy, piperidin-1-yl-carbonyl-C1-3-alkyloxy, morpholin-4-yl-carbonyl-C1-3-alkyl-oxy, piperazin-1-yl-carbonyl-C1-3-alkyloxy, 4-(C1-3-alkyl)-piperazin-1-yl-carbonyl-C1-3-alkyloxy,hydroxy-C1-3-alkyl, C1-3-alkyloxy-C1-3-alkyl, amino-C1-3-alkyl, C1-3-alkylamino-C1-3-alkyl, di-(C1-3-alkyl)-amino-C1-3-alkyl, pyrrolidin-1-yl-C1-3-alkyl , C1-4-alkylcarbonyl-amino-C1-3-alkyl, N—(C1-3-alkyl)-C1-4-alkylcarbonyl-amino-C1-3-alkyl , 2-oxo-pyrrolidin-1-yl-C1-3-alkyl, piperidin-1-yl-C1-3-alkyl, 2-oxo-piperidin-1-yl-C1-3-alkyl, morpholin-4-yl-C1-3-alkyl, 3-oxo-morpholin-4-yl-C1-3-alkyl, piperazin-1-yl-C1-3-alkyl, 2-oxo-piperazin-1-y1-C1-3-alkyl , 3-oxo-piperazin-1-yl -C1-3-alkyl, 4-(C1-3-alkyl)-piperazin-1-yl-C1-3-alkyl, 2-oxo-4-(C1-3-alkyl)-piperazin-1-yl-C1-3-alkyl, 3-oxo-4-(C1-3-alkyl)-piperazin-1-yl-C1-3-alkyl,hydroxy-C1-3-alkyloxy, C1-3-alkyloxy-C1-3-alkyloxy, C1-3-alkylsulfanyl-C1-3-alkyloxy, C1-3-alkylsulfinyl-C1-3-alkyloxy, C1-3-alkylsulfonyl-C1-3-alkyloxy, amino-C1-3-alkyloxy, C1-3-alkylamino-C1-3-alkyloxy, di-(C1-3-alkyl)-amino-C1-3-alkyloxy, pyrrolidin-1-yl-C1-3-alkyloxy, 2-oxo-pyrrolidin-1-yl-C1-3-alkyloxy, piperidin-1-yl-C1-3-alkyloxy, 2-oxo-piperidin-1-yl-C1-3-alkyloxy, morpholin-4-yl-C1-3-alkyloxy, 3-oxo-morpholin-4-yl -C1-3-alkyloxy, piperazin-1-yl-C1-3-alkyloxy, 2-oxo-piperazin-1-yl-C1-3-alkyloxy, 3-oxo-piperazin-1-yl-C1-3-alkyloxy, 4-(C1-3-alkyl)-piperazin-1-yl-C1-3-alkyloxy, 2-oxo-4-(C1-3-alkyl)-piperazin-1-yl-C1-3-alkyloxy, 3-oxo-4-(C1-3-alkyl)-piperazin-1-yl-C1-3-alkyloxy,C1-3-alkylsulfanyl, C1-3-alkysulfinyl, C1-3-alkylsulfonyl, C1-3-alkylsulfonyloxy, (het)arylsulfonyl, (het)arylsulfonyloxy, trifluoromethylsulfanyl, trifluoromethyl-sulfinyl, trifluoromethylsulfonyl,aminosulfonyl, C1-3-alkyl-aminosulfonyl, di-(C1-3-alkyl)-aminosulfonyl, pyrrolidin-1-yl-sulfonyl, piperidin-1-yl-sulfonyl, morpholin-4-yl-sulfonyl, piperazin-1-yl-sulfonyl, or 4-(C1-3-alkyl)-piperazin-1-yl-sulfonyl,wherein the above-mentioned saturated heterocycles and cycloalkyl-rings are optionally substituted with one or two groups selected independently from fluorine, C1-3-alkyl, C1-3-alkoxy, C1-3-alkoxy-C1-3-alkyl, and hydroxy, R2 and R3 are linked to each other to form a methylenedioxy, ethylenedioxy or C3-5-alkylene bridging group, which optionally is mono- or disubstituted with methyl, and which optionally and independently is mono- or polyfluorinated; or R2 and R3 together, and combined with the carbon atoms to which they are attached, form a benzo, pyrido, pyrazino, pyridazino, pyrimido, pyrrolo, furano, thieno, pyrazolo, imidazo, triazolo, oxazolo, thiazolo, isoxazolo, or isothiazolo ring, wherein each of said rings optionally is substituted with one to three substituents, independently of each other selected from halogen, C1-3-alkyl, trifluoromethyl, amino, C1-3-alkylamino, di-(C1-3-alkyl)amino, C1-3-alkylcarbonylamino, C1-3-alkylsulfonylamino, hydroxy, cyano, carboxy, C1-3-alkyloxycarbonyl and C1-3-alkyloxy, R10 denotes halogen, C1-3-alkyl, difluoromethyl, trifluoromethyl, cyano, nitro, amino, C1-3-alkylamino, di-(C1-3-alkyl)amino, acetylamino, C1-3-alkylsulfonylamino, carboxy, C1-4-alkyloxycarbonyl, aminocarbonyl, C1-3-alkylaminocarbonyl, di-(C1-3-alkyl)-aminocarbonyl, aminosulfonyl, methylsulfanyl, methylsulfinyl, methylsulfonyl, hydroxy, C1-3-alkyloxy, difluoromethoxy, trifluoromethoxy, or phenyl optionally substituted with 1 or 2 substituents independently of each other selected from fluorine, methyl, methoxy, cyano, and hydroxy, R11 denotes fluorine, C1-4-alkyl, (het)aryl, hydroxy, C1-4-alkyloxy, cyano, carboxy, C1-4-alkyloxycarbonyl, aminocarbonyl, C1-4-alkylamino-carbonyl, di-(C1-4-alkyl)-aminocarbonyl, hydroxy-C1-4-alkyl or C1-3-alkyloxy-C1-4-alkyl, R12 denotes fluorine or C1-4-alkyl, and L1 denotes halogen, C1-4-alkyl, trifluoromethyl, hydroxy, C1-4-alkyloxy, or cyano; L2 denotes fluorine, chlorine, bromine, iodine, nitro, cyano, hydroxy, C3-6-cycloalkyl, C3-6-cycloalkyloxy, tetrahydrofuran-3-yloxy, tetrahydropyran-3-yloxy, tetrahydropyran-4-yloxy, tetrahydrofuranyl-C1-3-alkyloxy, tetrahydropyranyl-C1-3-alkyloxy, (het)aryl, (het)aryloxy,
C1-6-alkyl, C2-6-alkenyl, C2-6-alkynyl, C1-6-alkyloxy, C1-6-alkylamino, wherein in each group one CH2 group optionally is replaced by carbonyl or sulfonyl, and wherein each group optionally is mono or polyfluorinated, and wherein each group optionally is additionally substituted with
hydroxy, chlorine, C1-3-alkyl, C3 -6-cycloalkyl, C1-3-alkyloxy, amino, C1-3-alkyl-amino, di-(C1-3-alkyl)-amino, pyrrolidin-1-yl, 2-oxo-pyrrolidin-1-yl, piperidin-1-yl, 2-oxo-piperidin-1-yl, morpholin-4-yl, 3-oxo-morpholin-4-yl, piperazin--yl, 2-oxo-piperazin-1-yl, 3-oxo-piperazin-1-yl, 4-(C1-3-alkyl)-piperazin-1-yl, 2-oxo-4-(C1-3-alkyl)-piperazin-1-yl, 3-oxo-4-(C1-3-alkyl)-piperazin-1-yl, carboxy, C1-3-alkyloxy-carbonyl, cyano, aminocarbonyl, C1-3-alkylamino-carbonyl, di-(C1-3-alkyl)-aminocarbonyl, pyrrolidin-1-yl-carbonyl, piperidin-1-yl-carbonyl, morpholin-4-yl-carbonyl, piperazin-1-yl-carbonyl, 4-(C1-3-alkyl)-piperazin-1-yl-carbonyl, C1-3-alkylcarbonylamino, arylcarbonylamino, C1-3-alkylsulfanyl, C1-3-alkylsulfinyl, C1-3-alkylsulfonyl, C3-6-cycloalkyl, (het)aryl, or (het)aryloxy; or L2 denotes amino, di-(C1-3-alkyl)amino, pyrrolidin-1-yl, 2-oxo-pyrrolidin-1-yl, piperidin-1-yl, 2-oxo-piperidin-1-yl, morpholin-4-yl, 3-oxo-morpholin-4-yl, piperazin-1-yl, 2-oxo-piperazin-1-yl, 3-oxo-piperazin-1-yl, 4-(C1-3-alkyl)-piperazin-1-yl, 4-(C1-4-alkylcarbonyl)-piperazin-1-yl, 4-(C3-6-cycloalkylcarbonyl)-piperazin-1-yl, 4-(C1-4- alkyloxycarbonyl)-piperazin-1-yl, 4-(C1-4-alkylsulfonyl)-piperazin-1-yl, 2-oxo-4-(C1-3-alkyl)-piperazin-1-yl, 3-oxo-4-(C1-3-alkyl)-piperazin-1-yl,
(het)aryl-carbonylamino, C1-4-alkyloxy-carbonylamino, aminocarbonylamino, C1-4-alkyl-aminocarbonylamino, (het)aryl-aminocarbonylamino, di-(C1-3-alkyl)aminocarbonylamino, pyrrolidin-1-yl-carbonylamino, piperidin-1-yl-carbonylamino, morpholin-4-yl-carbonylamino, piperazin-1-yl-carbonylamino, 4-(C1-3-alkyl)-piperazin-1-yl-carbonylamino, aminosulfonylamino, C1-3-alkylamino -sulfonylamino, di-(C1-3-alkyl)amino-sulfonylamino, pyrrolidin-1-yl-sulfonylamino, piperidin-1-yl-sulfonylamino, morpholin-4-yl-sulfonylamino, piperazin-1-yl -sulfonylamino, 4-(C1-3-alkyl)-piperazin-1-yl-sulfonylamino, (C1-3-alkyloxy-carbonylamino)carbonylamino, (het)arylsulfonylamino,N—(C1-3-alkyl)-C1-3-alkyl-carbonylamino, N—(C1-3-alkyl)-(het)arylcarbonylamino, N—(C1-3-alkyl)-(het)aryl-C1-3-alkyl-carbonylamino, N—(C1-3-alkyl)-C1-3-alkyloxy-carbonylamino, N—(aminocarbonyl)-C1-3-alkylamino, N—(C1-3-alkyl-aminocarbonyl)-C1-3-alkylamino, N-[di-(C1-3-alkyl)aminocarbonyl]-C1-3-alkylamino,N—(C1-3-alkyl)-C1-3-alkyl-sulfonylamino, N—(C1-3-alkyl)-(het)arylsulfonylamino, N—(C1-3-alkyl)-(het)aryl-C1-3-alkyl-sulfonylamino,carboxy, C1-3-alkyloxy-carbonyl, aminocarbonyl, C1-3-alkyl-aminocarbonyl, di-(C1-3-alkyl)-aminocarbonyl, azetidin-1-yl-carbonyl, pyrrolidin-1-yl-carbonyl, piperidin-1-yl-carbonyl, morpholin-4-yl-carbonyl, piperazin-1-yl-carbonyl, 4-(C1-3-alkyl)-piperazin-1-yl-carbonyl, (het)arylaminocarbonyl, N—(C1-3-alkyl)-(het)aryl-aminocarbonyl, (het)aryl-C1-3-alkylaminocarbonyl, N—(C1-3-alkyl)-(het)aryl-C1-3-alkylaminocarbonyl,C1-3-alkylsulfanyl, C1-3-alkysulfinyl, (het)arylsulfonyl, trifluoromethylsulfanyl, trifluoromethylsulfinyl,aminosulfonyl, C1-3-alkyl-aminosulfonyl, di-(C1-3-alkyl)-aminosulfonyl, pyrrolidin-1-yl-sulfonyl, piperidin-1-yl-sulfonyl, morpholin-4-yl-sulfonyl, piperazin-1-yl-sulfonyl, 4-(C1-3-alkyl)-piperazin-1-yl-sulfonyl,wherein the saturated heterocycles and cycloalkyl-rings mentioned in the definition of L2 as a single unit or a sub-moiety within another group are optionally substituted with one or two groups selected from fluorine, C1-3-alkyl, C1-3-alkoxy, C1-3-alkoxy-C1-3-alkyl, and hydroxy, and wherein L3 and L4 are linked to each other and wherein L5 and L6 are linked to each other, such that independently of each other and in each case together with the 2 adjacent C-atoms to which either L3 and L4 or L5 and L6 are attached an aryl- or heteroaryl-group is formed which is fused to the cyclic group B and which is optionally substituted with 1, 2, or 3 identical or different groups selected from R10, while by aryl is meant phenyl or naphthtyl and by heteroaryl is meant pyrrolyl, furanyl, thienyl, pyridyl, indolyl, benzofuranyl, benzothio-phenyl, quinolinyl, isoquinolinyl, or pyrrolyl, furanyl, thienyl, and pyridyl wherein in each 1 or 2 CH groups are replaced by N, or indolyl, benzofuranyl, benzothiophenyl, quinolinyl, and isoquinolinyl wherein in each 1 to 3 CH groups are replaced by N, and where in each >N—H containing heteroaryl all the >N—H groups present are optionally replaced by other groups independently selected from >N—RN, while the (het)aryl mentioned hereinbefore as a single unit or a sub-moiety within another group is an aryl group as defined hereinbefore, or a heteroaryl group as defined hereinbefore, or a ring selected from the group consisting of 1,2-dihydro-2-oxo-pyridinyl, 1,4-dihydro-4-oxo-pyridinyl, 2,3-dihydro-3-oxo-pyridazinyl, 1,2,3,6-tetrahydro-3,6-dioxo-pyridazinyl, 1,2-dihydro-2-oxo-pyrimidinyl, 3,4-dihydro-4-oxo-pyrimidinyl, 1,2,3,4-tetrahydro-2,4-dioxo-pyrimidinyl, 1,2-dihydro-2-oxo-pyrazinyl, 1,2,3,4-tetrahydro-2,3-dioxo-pyrazinyl, 2,3-di-hydro-2-oxo-indolyl, 2,3-dihydrobenzofuranyl, 2,3-dihydro-2-oxo-1H-benzimidazolyl, 2,3-dihydro-2-oxo-benzoxazolyl, 1,2-dihydro-2-oxo-quinolinyl, 1,4-dihydro-4-oxo-quinolinyl, 1,2-dihydro-1-oxo-isoquinolinyl, 1,4-dihydro-4-oxo-cinnolinyl, 1,2-dihydro-2-oxo-quinazolinyl, 1,4-dihydro-4-oxo-quinazolinyl, 1,2,3,4-tetrahydro-2,4-dioxo-quinazolinyl, 1,2-dihydro-2-oxoquinoxalinyl, 1,2,3,4-tetrahydro-3-oxo-quinoxalinyl, 1,2,3,4-tetrahydro-2,3-dioxo-quinoxalinyl, 1,2-dihydro-1-oxo-phthalazinyl, 1,2,3,4-tetrahydro-1,4-dioxo-phthalazinyl, chromanyl, coumarinyl, 2,3-dihydro-benzol[1,4]dioxinyl and 3,4-dihydro-3-oxo-2H-benzol[1,4]oxazinyl, wherein each of said rings is optionally substituted with 1, 2 or 3 substituents independently of each other selected from R10, and wherein each >N—H containing (het)aryl all the >N—H groups present are optionally replaced by other groups independently selected from >N—RN, whilst each of the above-mentioned alkyl or alkylene moieties may be branched or unbranched, a tautomer, stereoisomer thereof, mixture thereof, or salt thereof, while the compounds comprised by the formula II wherein R is hydrogen or R′ O, while R′ is any substituent, M1 is methyl, ethyl, propyl, or phenyl, M2 and M3 independently of each other are hydrogen, methyl, ethyl, or hydroxy, and ring B is
cyclohexyl which is optionally substituted with one or more C1-5-alkyl groups resulting in B having ≦10 carbon atoms in total, or1-(C1-3-alkoxy)-cyclohex-1-yl, 3-hydroxycyclohexyl, 4-hydroxycyclohexyl, 3-acetoxy-cyclohexyl, 4-acetoxy-cyclohexyl, cyclohexanon-4-yl, are excluded. |
