DART, MICHAEL J.,CHUNG, SEUNGWON,HUTCHINS, CHARLES W.,TONG, YUNSONG,ZHANG, QINWEI I.,SHI, LEI,SWEIS, RAMZI FARAH,XU, XIANGDONG,BLACK, LAWRENCE A.,FROST, JENNIFER M.,PLIUSHCHEV, MARINA,SIDRAUSKI, CARME
申请号：
ARP170101181
公开号：
AR108393A1
申请日:
2017.05.05
申请国别(地区):
AR
年份:
2018
代理人:
摘要：
1. This document provides useful compounds, compositions, and methods for the regulation of integrated stress response (ISR) and the treatment of related diseases, disorders, and conditions. 1. Claim 1: a formula compound (1),or a pharmaceutically acceptable salt, solvate, hydrate, tautomer or stereoisomer thereof, wherein: D is a monocyclic bridged cycloalkyl, bridged monocyclic heterocycle, where each bridged monocyclic cycloalkyl, bridged monocyclic heterocycle is optionally substituted with 1-4 RX； L¹ and L² are each independently C₁₋₆ alkylene or 2-7 membered heteroalkylene, wherein each C₁₋₆ alkylene or 2-7 membered heteroalkylene is optionally substituted with 1-5 RX； R¹ and R² are each independently hydrogen, C₁₋₆-alkyl,C₁₋₆-alkoxy-C₁₋₆-alkyl,hydroxy-C₁₋₆-alkyl,1. Silicate-c83217c83316262；A and W are independent phenyl or isomers, each of which can be replaced by 1-5 ry, and each Rx is selected from c83321316a and c8326a separately；hydroxy-C₁₋₆-alkyl,halo-alkyl Cilo,C-amino-alkyl,cyano-alkyl C₁₋₆,oxo, halo, cyano, -ORA, -NRBRC, -NRBC (O) RD, -C (O) NRBRC, -C (O) RD, -C (O) OH, -C (O) ORD, -SRE, -S (O) RD and -S (O) ₂RD； each RY is independently selected from the group consisting of hydrogen, C₁₋₆-alkyl,hydroxy-C₁₋₆-alkyl,C₁₋₆-alkoxy-C₁₋₆-alkyl,halo-alkyl Cilo,halo-C₁₋₆ alkoxy,C-amino-alkyl,cyano-alkyl C₁₋₆,oxo, halo, cyano, -ORA, -NRBRC, -NRBC (O) RD, -C (O) NRBRC, -C (O) RD, -C (O) OH, -C (O) ORD, -S ( RF) ₘ,-S (o) rd, - S (o) 8322；； RD and G1；O the two ry groups in the adjacent atoms, together with the atoms to which they are linked, form a cyclopentadiene glycol composed of 3-7 members or selectively substituted by 1-5 RX； each G1 is an independent cyclopentadiene c83231；a. 4-7 members' non bicycles, 5-6 members' non bicycles, c83231 per bicycle；a. 4-7-member heterocycles, 5-6-member arilo or heterocycles can be replaced by 1-3 RZ； each RZ is selected independently from the asphalt group of c83321316cs；hydroxy-C₁₋₆-alkyl,halo-alkyl Cilo,halo, cyano, -ORA,
