| 主权项 |
1. A compound of the formula (I): wherein: R1 is phenyl independently substituted from 1 to 5 times with halogen, C1-C3 alkyl, C3-C6 cycloalkyl, OR9, or SR10, wherein C1-C3 alkyl and C3-C6 cycloalkyl are optionally substituted with 1 to 10 times with R7; R2 is H; R3 and R4 are each individually H or CH3; R5 is selected from the group consisting of:
(1) hydrogen,(2) C1-C6 alkyl which is optionally substituted from 1 to 11 times with R7,(3) gem-dialkyl, and(4) gem-dihalo; or two R5 substituents on the same carbon, together with the carbon atom to which they are attached, may form a 3-, 4-, or 5-membered cycloalkyl optionally substituted from 1 to 10 times with R7; or two R5 substituents on adjacent carbons of the ring to which they are attached, together may form a 3-, 4-, 5- or 6-membered cycloalkyl optionally substituted from 1 to 10 times with R7; R6 is wherein E, F, and G are each independently nitrogen or carbon and R6a is C1-C2 alkyl, which is optionally substituted 1 to 5 times with halogen or deuterium; R7 is selected from the group consisting of:
(1) hydrogen,(2) halogen,(3) deuterium,(4) gem-dialkyl,(5) gem-dihalo,(6) —OR9, —NR11R12, —NR11C(O)pR10, —S(O)pR10, —CN, —NO2, —C(O)pR10, — C(O)NR11R12, or —NR11C(S)R10, and(7) oxo or thio; R8 is selected from the group consisting of:
(1) hydrogen,(2) halogen,(3) C1-C6 alkyl, C2-C6 alkenyl, C2-C6 alkynyl, C3-C7 cycloalkyl, or C4-C7 cycloalkylalkyl, wherein each of the C1-C6 alkyl, C2-C6 alkenyl, C2-C6 alkynyl, C3-C7 cycloalkyl, and C4-C7 cycloalkylalkyl is independently and optionally substituted from 1 to 11 times with R7, or(4) —OR9, —NR11R12, —NR11C(O)pR10, —S(O)pR10, —CN, —NO2, —C(O)pR10, —C(O)NR11R12, or —NR11C(S)R10; R9 is selected from the group consisting of hydrogen, C1-C4 alkyl, C3-C7 cycloalkyl, C4-C7 cycloalkylalkyl, —C(O)NR11R12, and —C(O)pR10, wherein each of C1-C4 alkyl, C3-C7 cycloalkyl, and C4-C7 cycloalkylalkyl is optionally substituted from 1 to 11 times with R7; R10 is selected from the group consisting of hydrogen, C1-C4 alkyl, C3-C7 cycloalkyl C4-C7 cycloalkylalkyl, aryl, and heteroaryl, wherein each of C1-C4 alkyl, C3-C7 cycloalkyl, and C4-C7 cycloalkylalkyl is optionally substituted from 1 to 11 times with substituents as defined in R7 and aryl or heteroaryl is optionally substituted from 1 to 10 times with R8; R11 and R12 are each independently selected from the group consisting hydrogen, C1-C4 alkyl, C3-C7 cycloalkyl, C4-C7 cycloalkylalkyl, aryl, and heteroaryl, wherein each of C1-C4 alkyl, C3-C7 cycloalkyl, and C4-C7 cycloalkylalkyl is optionally substituted from 1 to 11 times with substituents as defined in R7 and aryl or heteroaryl is optionally substituted from 1 to 10 times with R8, or R11 and R12 are taken together with the nitrogen to which they are attached to form a saturated or partially saturated monocyclic or fused bicyclic heterocycle optionally substituted from 1 to 11 times with R7; A is X is N; Y is N; p is 1, or 2; and m is 0; with the following provisos that: R6 cannot be (a) 1H-1,2,3-triazol-4-yl, or (b) 5-methylisoxazol-4-yl; or an oxide thereof, a pharmaceutically acceptable salt thereof, or an individual enantiomer or diastereomer thereof. |
