JULIEN PAPILLON,MICHAEL LUZZIO,MICHAEL SCOTT VISSER
申请号：
ARP150102513
公开号：
AR101456A1
申请日:
2015.08.05
申请国别(地区):
AR
年份:
2016
代理人:
摘要：
C-protein cyclase inhibitor (PKC) was reported. PKC inhibitors help to treat PKC related diseases, including some cancers. PKC inhibitors are more effective in tumor suppression at lower doses, with higher power, pharmacological characteristics (PK),Absorption, gastrointestinal tolerance and ribbon selectivity 1. Claim 1: a formula compound (1),Or a pharmaceutically acceptable salt characterized by: X is n or Cr； R, R,R3 and r83088 are h, 2h, halogen and hydroxy (- OH), respectively,C₁₋₃ alkoxy,a. Halo Aquilo c83217c83183223 or c83218c83323；this C₁₋₃-alkyl being optionally substituted with hydroxyl, halogen, C₁₋₃-alkoxy or halo-C₁₋₃-alkoxy；R83099 is independent of H, square, ch8323；CH F CHFCF8323,C8322joh, rental c833218331；1. By F, oh, alcoxilo c83218c83218c83237o halo alcoxylo c83218c831238c83123238c83123237c83223238c83238c83238c238c83238c237c83238c83238c33238f2323c33238c83238c33238c33238c8323；R⁵ᵃ and R⁵ᵇ are each independently H, ²H, C₁₋₃ alkyl,this C₁₋₃-alkyl being optionally substituted with F, OH or C₁₋₃-alkoxy,or R⁵ᵃ and R⁵ᵇ are joined together to form a methylene or ethylene bridging group； R⁵ᶜ and R⁵ᵈ are each independently H, ²H, F, -OH, C₁₋₃ alkoxy,1. Apartment c83218331；this C₁₋₃-alkyl being optionally substituted with F, OH or C₁₋₃-alkoxy,O r8309； 758080 and r8309； 74966 constitute a methylene and ethylene o-ch8322o-o -, bridge group；R8310,R⁷ and R⁸ are each independently selected from H, ²H, halogen, C₁₋₃-alkyl,halo-alkyl Cilo,C₁₋₃ alkoxy,halo-C alco alkoxy,cycloalkyl C₃₋₇,and 4- to 7-membered heterocyclyl having 1 to 3 heteroatoms selected from N, O, and S, this C₁₋₃ alkyl being optionally substituted with F, OH, C₁₋₃ alkoxy or C₁₋₃ haloalkoxy；or wherein R⁶ and R⁸ optionally form a carbocyclic ring or a heterobicyclic ring partially saturated with the heteroaryl ring, the carbocyclic ring or the heterobicyclic ring being optionally substituted with 1 to 3 groups selected from: ²H, halogen, halo-alkyl C₁₋₃,C₁₋₃ alkoxy,halo-C alco alkoxy,cycloalkyl C₃₋₇
