| 主权项 |
1. A compound having the formula (I) or an N-oxide, stereoisomer, tautomer, racemic or salt thereof, wherein R1 is a bivalent chain selected from wherein the sulfonyl group is attached to the remainder of the molecule via the nitrogen atom of the amide group, and the carbon atom of the acetamide moiety is attached to the remainder of the molecule via the nitrogen of the indole ring of the compound of formula (I); X is selected from —CR5aR5b— or —NR5a—; each of g and h is, independently, an integer selected from 0, 1, 2, 3, 4, or 5, with the proviso that the macrocycle formed by the bivalent chain R1, the —C(═O)—NH— moiety to which R1 is attached and the nitrogen and carbon atoms N1, C6, C7, and C7′ of the indole ring, has from 14 to 17 member atoms; each parallel dashed line (represented by ) represents an optional double bond; R2 is hydrogen or C1-6alkyl; R3 is C3-7cycloalkyl; R4 is a group selected from: R5a and R5b are each independently selected from hydrogen; C1-6alkyl; or haloC1-6alkyl; n is 0, 1, or 2; R6 is selected from hydrogen, halo, C1-6alkyl, or C3-7cycloalkyl; R6a is selected from hydrogen, halo, C1-6alkyl, or C3-7cycloalkyl; R7 is phenyl or thiazolyl, wherein each phenyl is optionally substituted with one, two, or three substituents, wherein each thiazolyl is optionally substituted with one or two substituents; wherein the substituents on both phenyl and thiazolyl are each independently selected from halo; cyano; nitro; C1-6alkyl; —OR12; —C(═O)OR12; —C(═O)R13; —C(═O)NR9aR9b; —NR9aR9b; —NR9aC(═O)R13; —NR9aC(═O)—CH2—NR9aR9b; —SR10; —SO2R11; —SO2NR9aR9b; phenyl optionally substituted with one, two or three substituents each independently selected from halo, trifluoromethyl, cyano, C1-6alkyl, C1-6alkoxy, and —C(═O)NR9aR9b; and Het optionally substituted with one or two substituents each independently selected from oxo, C1-6alkylsulfonyl, and C1-6alkyl; R8 is hydrogen, phenyl, or thiazolyl, wherein each phenyl is optionally substituted with one, two, or three substituents, wherein each thiazolyl is optionally substituted with one or two substituents; wherein the substituents on both phenyl and thiazolyl are each independently selected from halo; cyano; nitro; C1-6alkyl; —OR12; —C(═O)OR12; —C(═O)R13; —C(═O)NR9aR9b; —NR9aR9b; —NR9aC(═O)R13; —NR9aC(═O)—CH2—NR9aR9b; —SR10; —SO2R11; —SO2NR9aR9b; phenyl optionally substituted with one, two or three substituents each independently selected from halo, trifluoromethyl, cyano, C1-6alkyl, C1-6alkoxy, and —C(═O)NR9aR9b; and Het optionally substituted with one or two substituents each independently selected from oxo, C1-6alkylsulfonyl, and C1-6alkyl; R9a and R9b are each independently selected from hydrogen, C1-6alkyl, or arylC1-6alkyl; or R9a and R9b, together with the nitrogen to which they are attached, form a saturated, partially unsaturated, or completely unsaturated 5-8 membered monocycle, wherein said monocycle optionally contains one additional heteroatom selected from the group consisting of oxygen, sulfur and nitrogen, and wherein the remaining monocycle members are carbon atoms; wherein said monocycle is optionally substituted on any carbon atom with one or two substituents each independently selected from halo, C1-6alkyl, hydroxy, or oxo, wherein aryl is phenyl or naphthyl; R10 is C1-6alkyl or C3-7cycloalkyl; R11 is C1-6alkyl or C3-7cycloalkyl; R12 is hydrogen, C1-6alkyl, or benzyl; R13 is C1-6alkyl; Het is pyrrolidinyl, piperidinyl, morpholinyl, or piperazinyl. |
