| 摘要 |
Provided are 7-azaindole or 4,7-diazaindole derivatives as an IKKε (I-kappa-B kinase epsilon) and TBK1 (TANK-binding kinase 1) inhibitor. The 7-azaindole or 4,7-diazaindole derivative effectively inhibits IKKε and TBK1, and thus is useful not only as an anticancer agent for the treatment of various cancers including colorectal cancer, breast cancer, CNS cancer, colon cancer, non-small cell lung cancer, kidney cancer, prostate cancer, ovarian cancer, uterus cancer, stomach cancer, liver cancer, skin cancer, lung cancer, brain cancer, bladder cancer, esophageal cancer, pancreatic cancer, thyroid cancer, head and neck cancer, squamous cell carcinoma, osteosarcoma, B-cell or T-cell lymphoma, acute or chronic leukemia and multiple myeloma, but as a therapeutic agent for chronic inflammation. |
| 主权项 |
1. A compound selected from the group consisting of a 7-azaindole or 4,7-diazaindole derivative of formula (I) and a pharmaceutically acceptable salt, a hydrate, and a solvate thereof: wherein, X is C or N, ring A is C6-14 aromatic ring, or saturated or unsaturated 5- to 7-membered heterocycle containing at least one N; R1 is H, halogen, substituted or unsubstituted C5-14 aryl, substituted or unsubstituted 5- to 13-membered heteroaryl, or —NHY (wherein, Y is substituted or unsubstituted C5-14 aryl; and said aryl or heteroaryl is optionally substituted with one or more substituents selected from the group consisting of 5- to 10-membered heterocycloalkyl-C1-7 alkyl, C1-7 alkoxy, halogen, C1-7 alkyl, C1-7 alkylamido, C1-7 alkyl-5- to 10-membered heterocycloalkyl-C1-7 alkyl, C3-10 cycloalkyl-5- to 10-membered heterocycloalkyl-C1-7 alkyl, 5- to 10-membered heterocycloalkyl-C1-7 alkyl, C1-7 alkyl-5- to 10-membered heterocycloalkyl-carbonyl, 5- to 10-membered heterocycloalkyl-amino, 5- to 10-membered heterocycloalkyl-oxy, C1-7 alkyl-sulfonyl, C3-10 cycloalkyl-sulfonyl, sulfamoyl, C1-7 alkyl-sulfamoyl, 5- to 10-membered heterocycloalkyl-sulfonyl, amino, oxo, 5- to 13-membered heteroaryl-C1-7 alkyl-carbamoyl, 5- to 10-membered heterocycloalkyl-C1-7 alkoxy, 5- to 10-membered heterocycloalkyl-carbonyl, C1-7 alkoxy-carbonyl-5- to 10-membered heterocycloalkyl-C1-7 alkyl, 5- to 10-membered heterocycloalkyl, C1-7 alkyl-carbonyl, C1-7 alkoxy-carbonyl, cyano, C1-7 alkyl-5- to 13-membered heteroaryl, di C1-7 alkyl-sulfonyl, C1-7 alkyl-amino-sulfonyl, and C1-7 alkyl-sulfonylamido; R2 is H or —NH2; R3 is H or C1-7 alkyl; R4 is C1-7 alkyl, —C(═O)—R7, —C(═O)—O—R8, —C(═O)—N(—R9)—R10, —CH2—C(═O)—NH—R11 or —CH2—C(═O)—R12; R7 to R12 are each independently H, hydroxy, C1-7 alkyl, substituted or unsubstituted C3-10 cycloalkyl, substituted or unsubstituted 5- to 10-membered heterocycloalkyl or substituted or unsubstituted 5- to 13-membered heteroaryl; and each of said cycloalkyl, heterocycloalkyl and heteroaryl is optionally substituted with C1-7 alkyl; R5 and R6 are each independently H, halogen, C1-7 alkyl or substituted or unsubstituted C5-14 aryl; when said R5 and R6 are C1-7 alkyl, said R5 and R6 are optionally connected to each other. |
