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Pirrolopirimidona and pirrolopiridona, tanquirasa inhibitors
专利权人:
F. HOFFMANN-LA ROCHE AG
发明人:
申请号:
ARP130101978
公开号:
AR091271A1
申请日:
2013.06.05
申请国别(地区):
AR
年份:
2015
代理人:
摘要:
The compounds have activity as anticancer agents. Claim 1: A compound of the formula (1) wherein: Q and X independently of each other are at each occurrence N or CH; R¹ is selected from the group consisting of hydrogen, C₁₋₆ alkyl,C₁₋₆ alkenyl,C₁₋₆ hydroxyalkyl,dihydroxy-C₁₋₆ alkyl,C₃₋₇ cycloalkyl;R 2 is the other part selected from the formula group (2);O r 2 is 2.5-diazabiciclo [2.2.1] heptanie;8308y-o -,where R⁵ is hydrogen, C₁₋₆ alkyl;R⁴ is C₁₋₆ alkyl,C₁₋₆ alkylsulfonyl,acyl C₁₋₆,phenyl or heteroaryl, said heteroaryl is selected from pyridinyl, pyrazinyl and pyrimidinyl and said phenyl and said heteroaryl are optionally substituted one to three times by substituents independently selected from the group consisting of halogen, CN, C₁₋₆ alkylsulfonyl,C₁₋₆ haloalkyl,C₁₋₆ hydroxyalkyl,(alcoxi c83218d. 8331233a) - lessor c83218c8312323a;(Alcoxi C) -carbonilo carboxi CONR Rin which R⁴ᵇ and R⁴ᶜ independently of each other are hydrogen or C₁₋₃ alkyl at each occurrence,and OR⁴ᵃ,wherein R⁴ᵃ is selected from the group consisting of (i) hydrogen, (ii) C₁₋₆ alkyl,(Iii) alcoxi C(Iv) (alcoxi C) -alquilo C(V) hidroxialquilo C y (vi) dihidroxi-alquilo CR3: selected from the hydrogen group, tar c832138;C₁₋₆ alkoxy,substituted alkyl, C₁₋₆ haloalkyl,C₁₋₆ hydroxyalkyl,dihydroxy-C₁₋₆ alkyl,(alcoxi c83218d. 8331233a) - lessor c83218c8312323a;halogen, CN, trifluoromethyl, (C₁₋₆) alkoxycarbonyl, C₁₋₆ alkylsulfonyl,Conr8308;]in which R⁴ᵇ and R⁴ᶜ independently of each other are hydrogen or C₁₋₃ alkyl at each occurrence,and OR³,wherein R³ᵃ is chosen from the group consisting of (i) hydrogen, C₁₋₆ alkyl,(Iii) (alcoxi C) -alquilo C(Iv) hidroxialquilo C y (v) dihidroxi-alquilo COr acceptable saltLos compuestos tienen actividad como agentes anticancerosos. Reivindicación 1: Un compuesto de la fórmula (1) en la que: Q y X con independencia entre sí son en cada aparición N o CH; R¹ se elige entre el grupo formado por hidrógeno, alquilo C₁₋₆, alquenilo C₁₋₆, hidroxialquilo C₁₋₆, dihidroxi-alquilo
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