主权项 |
1. A compound of formula I: or a pharmaceutically acceptable salt, hydrate, enantiomer or stereoisomer thereof, wherein independently for each occurrence, X is R1 is hydrogen, alkyl, cycloalkyl, alkylcycloalkyl, alkylaryl, haloalkyl, formyl, heterocyclyl, heterocyclylalkyl, or (C2-C4)alkyl substituted with except that when X is R1 is not R10 is hydrogen or alkyl; R11a is hydrogen, alkyl, or alkyl-cycloalkyl; R11b is hydrogen or alkyl; or taken together with R11a and the nitrogen to which it is attached forms a 4- to 8-membered heterocyclyl comprising 0 or 1 additional heteroatoms; R13 is hydrogen, alkyl, aryl, heteroaryl, aralkyl, heteroaralkyl or silyl; R14 is hydrogen, alkyl, aryl, heteroaryl, aralkyl or heteroaralkyl; R15 is alkyl, cycloalkyl or cycloalkylalkyl; R20 is hydrogen, alkyl, cycloalkyl or cycloalkylalkyl; A is R2 is Y is —NH—, —N(alkyl)-, —O—, or —CR62—; R22a is aryl, heteroaryl, aralkyl, heteroaralkyl, fused bicyclyl, biaryl, aryloxyaryl, heteroaryloxyaryl, aryloxyheteroaryl or heteroaryloxyheteroaryl; R22b is hydrogen or alkyl; R24 is hydrogen or alkyl; R25a, R25b, R25c, and R25d independently are -M2-T2, in which M2 is a bond, SO2, SO, S, CO, CO2, O, O—C1-C4 alkyl linker, C1-C4 alkyl linker, NH, or N(Rt), Rt being C1-C6 alkyl, and T2 is H, halo, or RS4, RS4 being C1-C6 alkyl, C2-C6 alkenyl, C2-C6 alkynyl, C3-C8 cycloalkyl, C6-C10 aryl, 4 to 8-membered heterocycloalkyl, or 5 to 10-membered heteroaryl, and each of 0-C1-C4 alkyl linker, C1-C4 alkyl linker, Rt, and RS4 being optionally substituted with one or more substituents selected from the group consisting of halo, hydroxyl, carboxyl, cyano, C1-C6 alkyl, C2-C6 alkenyl, C2-C6 alkynyl, C1-C6 alkoxyl, amino, mono-C1-C6 alkylamino, di-C1-C6 alkylamino, C3-C8 cycloalkyl, C6-C10 aryl, 4 to 6-membered heterocycloalkyl, and 5 to 6-membered heteroaryl; R3 is hydrogen, halogen, hydroxy, alkyloxy, aralkyloxy, alkylcarbonyloxy or silyloxy; R4 is hydrogen, halogen, hydroxy, alkyloxy, aralkyloxy, alkylcarbonyloxy or silyloxy; R41 is hydrogen, alkyl or alkynyl; Z is hydrogen or R5a is hydrogen, alkyl, haloalkyl, alkenyl, alkynyl, carbocyclyl, heterocyclyl, aryl, heteroaryl, biaryl, alkenylalkyl, alkynylalkyl, carbocyclylalkyl, heterocyclylalkyl, aralkyl, heteroaralkyl, alkylcarbonylaminoalkyl, arylcarbonylaminoalkyl, aralkylcarbonylaminoalkyl, aryl sulfonylaminoalkyl, alkylthioalkyl, aralkylthioalkyl or heteroaralkylthioalkyl; or alkyl substituted with 1, 2 or 3 substituents independently selected from the group consisting of hydroxy, halo, carboxy, alkyoxy, aryloxy, aralkyloxy, nitro, amino, amido, aryl and heteroaryl; R5b is hydrogen, alkyl, haloalkyl, alkenyl, alkynyl, carbocyclyl, heterocyclyl, aryl, heteroaryl, biaryl, alkenylalkyl, alkynylalkyl, carbocyclylalkyl, heterocyclylalkyl, aralkyl, heteroaralkyl, alkylcarbonylaminoalkyl, arylcarbonylaminoalkyl, aralkylcarbonylaminoalkyl, aryl sulfonylaminoalkyl, alkylthioalkyl, aralkylthioalkyl or heteroaralkylthioalkyl; or alkyl substituted with 1, 2 or 3 substituents independently selected from the group consisting of hydroxy, halo, carboxy, alkyoxy, aryloxy, aralkyloxy, nitro, amino, amido, aryl and heteroaryl; or taken together with R5a and the nitrogen to which it is attached forms a 4- to 8-membered heterocyclyl comprising 0 or 1 additional heteroatoms; R6 is hydrogen, alkyl or halo; or two geminal R6 taken together are ethylene, propylene or butylene; R7a is hydrogen, lower alkyl, lower haloalkyl, cyano, halo, lower alkoxy, or C3-C5 cycloalkyl, optionally substituted with 1, 2 or 3 substituents independently selected from the group consisting of cyano, lower alkoxy and halo; R7b is hydrogen, lower alkyl, lower haloalkyl, cyano, halo, lower alkoxy, or C3-C5 cycloalkyl, optionally substituted with 1, 2 or 3 substituents independently selected from the group consisting of cyano, lower alkoxy and halo; and R7c is hydrogen, lower alkyl, lower haloalkyl, cyano, halo, lower alkoxy, or C3-C5 cycloalkyl, optionally substituted with 1, 2 or 3 substituents independently selected from the group consisting of cyano, lower alkoxy and halo. |