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Inhibitors of bmi-1 Reverse substituted pyrimidine
专利权人:
PTC THERAPEUTICS; INC.
发明人:
申请号:
ARP130104300
公开号:
AR093579A1
申请日:
2013.11.21
申请国别(地区):
AR
年份:
2015
代理人:
摘要:
This document introduces pyridine compounds and various forms of pyridine compounds substituted by ammonia, which hinder the action, reduce the protein content at point 1 of specific lymphocyte BMI (Bmi-1) and the method of inhibiting the action of Bmi-1 and reducing the action of Bmi-1. Bmi-1 for the treatment of Bmi-1 intermediate cancer 1. Claim 1: a formula compound (1),Or a form where R1 is heteromorphic or optional heterocyclization, replaced by 1, 2, 3 or 4 r83099 of the ring carbon atom,or in a ring nitrogen atom member with an oxygen atom substituent to form u N-oxide; X is N or N substituted with an oxygen atom substituent to form an N-oxide; R² is hydrogen, cyano, halo, hydroxyl, nitro, C₁₋₈ alkyl,1. Hydroxy hydrocarbon c8321c83318328;C₁₋₈ alkoxy,amino alquil C -amino (alquil C) -amino hidroxil-amino hidroxil-alquil C -amino alcoxi C -alquil C -amino alquil C -tio alquil C -carbonilo alquil C -carbonil-amino amino-carbonilo alquil C -amino-carbonilo (c) 1-chlorodibenzo-p-dioxin and furan substitutes;R3: hydrogen, cyanogen, halogen and alkyl c83318328;amino alquil C -amino o (alquil C) -amino R es cicloalquilo Ca. Arilo, isopropene or isopropene, each replaced by 1, 2, 3 or 4 r8310 substitutes;R⁵ is independently selected from cyano, halo, hydroxyl, nitro, oxo, C₁₋₈ alkyl,cyano-alkyl C₁₋₈,halo-alkyl Cilo,1. Hydroxy hydrocarbon c8321c83318328;C₁₋₈ alkoxy,alcoxi C -alquilo Chalo-C₁₋₈ alkoxy,C₂₋₈ alkenyl,C₁₋₈ alkoxy-C₂₋₈ alkenyl,1. C 83228331 asphalt;C₁₋₈ alkoxy-C₂₋₈ alkynyl,carboxilo amino alquil C -amino (alquil C) -amino amino-alquilo CC₁₋₈-alkyl-C₁₋₈-alkyl,(pitch pitch pitch-c83218c83316c) 832228;hydroxy-C₁₋₈-alkyl-amino, hydroxy-C₁₋₈-alkyl-C--alkyl,a. Hidroxil codil c8321 No. 8321, countdown 8321; 8331;C₁₋₈-alkoxy-carbonyl, C₁₋₈-alkoxy-carbonyl-C₁₋₈-alkyl,alcoxi C -carbonilamino alquil C -sulfonilo cicloalquilo Caryl, aryl-C₁₋₈-alkyl,aril-amino aril-alquil C -amino heteroarilo heteroaril-alquilo C o heterociclilo donde cicloalquilo Ca. Arilo, heatarilo,
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