| 主权项 |
1. A compound of formulae I(A-E) having the following structure: wherein: the carbon atom designated * is in the R or S configuration; X is phenyl, optionally substituted from 1 to 4 times with substituents as defined in R14; R1 is H, methyl, ethyl, or isopropyl; R2 is H, methyl, or gem-dimethyl; R3 is H, methyl, hydroxy, methoxy, fluoro, chloro, cyano, trifluoromethyl, or trifluoromethoxy; R4 is pyrimidinyl, optionally substituted from 1 to 4 times with substituents as defined below in R14; R5 is H, fluoro, chloro, methyl, trifluoromethyl, trifluoromethoxy, cyano, hydroxy or methoxy; R6 is H, fluoro, chloro, methyl, trifluoromethyl, trifluoromethoxy, cyano, hydroxy or methoxy; R7 is H, gem-dimethyl, or C1-C4 alkyl, wherein each of the C1-C4 alkyl is optionally substituted from 1 to 3 times with substituents as defined in R15; R8 is H; R9 is H; R10 and R11 are each independently selected from the group consisting of H, —C(O)R13, C1-C4 alkyl, C3-C6 cycloalkyl, and C4-C7 cycloalkylalkyl, where each of C1-C6 alkyl, C3-C6 cycloalkyl, and C4-C7 cycloalkylalkyl is optionally substituted from 1 to 3 times with substituents as defined below in R15; R10 and R11 are each independently selected from the group consisting of phenyl, benzyl, and other 5- or 6-membered monocyclic heterocycles, where each of the phenyl, benzyl, and 5- or 6-membered monocyclic heterocycle is optionally substituted from 1 to 3 times with substituents as defined below in R14; R10 and R11 are taken together with the nitrogen to which they are attached to form a saturated or partially saturated monocyclic or fused bicyclic heterocycle selected from the group consisting of piperidine, pyrrolidine, morpholine, thiomorpholine, [1,2]oxazinane, isoxazolidine, 2-oxopiperidinyl, 2-oxopyrrolidinyl, 3-oxomorpholino, 3-oxothiomorpholino, 5,6,7,8-tetrahydroimidazo[1,2-a]pyrazine, 5,6,7,8-tetrahydro-[1,2,4]triazolo[4,3-a]pyrazine, and other monocyclic or fused bicyclic heterocycles containing 1-4 heteroatoms selected from oxygen, nitrogen and sulfur, wherein the heterocycle is attached to the benzazepine core via the nitrogen atom, and is optionally substituted from 1 to 3 times with a substituent selected independently at each occurrence thereof from the group consisting of halogen, cyano, —OR12, —NR12R13, —S(O)nR13, —C(O)R13, and C1-C4 alkyl, where each of C1-C4 alkyl is optionally substituted from 1 to 3 times with substituents as defined below in R15; R10 and R11 are taken together with the nitrogen to which they are attached to form a heterocycle selected from the group consisting of piperazine, 2-oxopiperazinyl, 2-oxo-1,4-diazepanyl, 5-oxo-1,4-diazepanyl, 1,4-diazepane, and other heterocycles containing one additional nitrogen atom in the ring, where the heterocycle is optionally substituted on a ring carbon with from 1 to 3 times with a substituent selected independently at each occurrence thereof from the group consisting of halogen, cyano, —OR12, —NR12R13, —S(O)nR13, —C(O)R13, and C1-C4 alkyl, or on the additional nitrogen atom from 1 to 3 times with a substituent selected independently at each occurrence thereof from the group consisting of S(O)nR13, —C(O)R13, and C1-C4 alkyl, wherein each of C1-C4 alkyl is optionally substituted from 1 to 3 times with substituents as defined below in R15; R10 and R11 are taken together with the nitrogen to which they are attached to form a heterocycle selected from the group consisting of piperazine, 2-oxopiperazinyl, 2-oxo-1,4-diazepanyl, 5-oxo-1,4-diazepanyl, 1,4-diazepane, and other heterocycles containing one additional nitrogen atom in the ring, where the heterocycle is optionally substituted on the additional nitrogen atom with a substituent selected independently at each occurrence thereof from the group consisting of phenyl, benzyl, and 5- or 6-membered aromatic heterocycles containing 1-3 heteroatoms selected from the group consisting of oxygen, nitrogen, and sulfur, where each of the phenyl, benzyl, and 5- and 6-membered heterocycle is optionally substituted from 1 to 3 times with substituents as defined below in R14; R12 is selected from the group consisting of H, C1-C4 alkyl, C3-C6 cycloalkyl, C4-C7 cycloalkylalkyl, and —C(O)R13, where each of C1-C6 alkyl, C3-C6 cycloalkyl, and C4-C7 cycloalkylalkyl is optionally substituted from 1 to 3 times with substituents as defined below in R15; R13 is C1-C4 alkyl; R14 is independently selected at each occurrence from a substituent in the group consisting of halogen, —NO2, —OR12, —NR10R11, —NR12C(O)2R13, —NR12C(O)NR12R13, —S(O)nR13, —CN, —C(O)R13, C1-C6 alkyl, C2-C6 alkenyl, C2-C6 alkynyl, C3-C6 cycloalkyl, and C4-C7 cycloalkylalkyl, wherein each of C1-C6 alkyl, C2-C6 alkenyl, C2-C6 alkynyl, C3-C6 cycloalkyl, and C4-C7 cycloalkylalkyl is optionally substituted from 1 to 3 times with substituents as defined below in R15; and R15 is independently selected at each occurrence from a substituent in the group consisting of —CN, halogen, C(O)R13, C1-C3 alkyl, —OR12, —NR10R11, —S(O)nR13, aryl, and heteroaryl, wherein each of the aryl or heteroaryl groups is optionally substituted from 1 to 4 times with substituents as defined above in R14; and n is 0, 1, or 2. |
