GLAXOSMITHKLINE INTELLECTUAL PROPERTY DEVELOPMENT LIMITED
发明人:
申请号：
ARP160100683
公开号：
AR103934A1
申请日:
2016.03.15
申请国别(地区):
AR
年份:
2017
代理人:
摘要：
It is found that the compounds and their salts in this application hinder the binding of bromine domain bet protein family such as acetyllysine residues, so they can be used for treatment, such as treatment of autoimmunity and inflammation, Such as rheumatoid arthritis and cancer. 1. Claim 1: a formula compound (1) or a salt, wherein R1 and R2 are hydrogen or methyl respectively, provided that at least one R1 and R2 are methyl； R3 is tar c83338326；C₁₋₆ alkoxy,cicloalquilo heterocicloalquilo o -CHR (CH) RR830808 is a formula compound (2), which is at the 5th or 6th position of benzozimidazole；R83099 is hydrogen, c832131；alcoxi C o - (CH) ORR8310s is hydrogen, c832131；C₁₋₃ alkoxy,- (CH) ORHydroxy, 11a. Halo, cycloquilo, heatcoquilo, heatcoquilo, arilo or heateriario, in which c83218331 is leased；C₁₋₃ alkoxy,- (CH) ORcycloalkyl, heterocycloalkyl, aryl or heteroaryl may optionally be substituted with one or two substituents selected independently from the group consisting of C₁₋₃-alkyl,C₁₋₃ alkoxy,halo CH OH -COOH y -COCHR8311811 is hydrogen, c8332131 hydrocarbon 832626,- (CH₂) ᵍ-cycloalkyl, - (CH₂) ₕ-heterocycloalkyl or CR¹³R¹⁴R¹⁵；R831222 is hydrogen, c8332131 hydrocarbon 832626,cycloalkyl, heterocycloalkyl or -CHR¹⁶R¹⁷ where said C₁₋₆ alkyl is optionally substituted with C₁₋₃ alkoxy and where R¹⁶ is hydrogen or C₁₋₃ alkyl and R¹⁷ is cycloalkyl or heterocycloalkyl； R⁹,R830404,R1,R2,R830808,R¹⁵ and R¹⁸ are each independently hydrogen or C₁₋₃ alkyl；R3 is hydrogen, hydroxyl, ch83222； or1 831222；halo -COOH -CONH1h-imidazol-4-ilo -, SH -, SH, sEH, hydrocarbyl c833123；C₁₋₃ alkoxy,phenyl or 4-hydroxyphenyl in which said C₁₋₃ alkyl or C₁₋₃ alkoxy can be optionally substituted with halo, hydroxyl, -NHC (= NH₂) NH₂,-NH832222,-COOH, -CONH₂ or -SCH₃；A is 0, 1, 2 or 3； B is 0 or 1； C is 1, 2 or 3, provided B is 1, C is 2 or 3； D and E are 1 or 2； G and H are 0, 1 or 2.Se ha encontrado que los compuestos de la presente solicitud y sales de los mismos inhiben la unión de la familia B
