4,6-disubstituted aminopyrimidine derivatives have anti-HIV activity
AssigneeVirostatics Srl
InventorsFranco Lori, James Chafouleas, Davide De Forni, Antonio Solinas, Zoltán Varga, Zoltán Greff, László Õrfi, György Kéri
Life of this patent
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Abstract
Novel 4,6-disubstituted aminopyrimidine derivatives with the following structure (I) have anti-HIV activity.
Claims20
A compound having formula (I):
- where
- X, Y and Z are H, F, or Cl;
- R1 is OR, where R is hydrogen or a group selected from straight or branched C1-C6 alkyl, C2-C6 alkenyl, C2-C6 alkynyl, C3-C6 cycloalkyl, heterocyclyl, CF3, CCl3, and aryl in positions 2, 3 or 4;
- R2 is OH, alkoxy, aryloxy, CH2OR (where R is H, linear or branched aryl, cycloalkyl or alkyl), CH2NR′R″ (where R′ and R″ are independently H, linear or branched aryl, cycloalkyl or alkyl), CHO, OCOW (where W is linear or branched aryl or alkyl or C-(halogen)3), CONR′R″ (where R′ and R″ independently are H, alkyl, cycloalkyl or aryl), COOR (where R is H, alkyl, cycloalkyl or aryl), CH2NHSO2R (where R is H, alkyl, cycloalkyl or aryl), Cl, Br, F, substituted or unsubstituted CH2—N-benzimidazole, CONHNR′R″ (where R′ and R″ independently are H, alkyl, cycloalkyl or aryl), NRCOOR′ (where R and R′ are independently H, alkyl, cycloalkyl or aryl), NH2, NR′R″ (where R′ and R″ independently are alkyl, cycloalkyl or aryl), NHCOR (where R is H, alkyl, cycloalkyl or aryl), nitro, OCH2CH2-heterocyclyl, OCOR (where R is H, alkyl, cycloalkyl or aryl), OCONR′R″ (where R′ and R″ are independently H, alkyl, cycloalkyl or aryl), OCOOR (where R is H, alkyl, cycloalkyl or aryl), NHCOOCH2C-halo3, NRCONR′R″ (where R, R′ and R″ independently are H, alkyl, cycloalkyl or aryl), NHSO2R (where R is H, alkyl, cycloalkyl or aryl), NHSO2NR′R″ (where R′ and R″ independently are H, alkyl, cycloalkyl or aryl),
- and R3 is OH, alkoxy, aryloxy, NR′R″ (where R′ and R″ are H), NHCOR (where R is H, alkyl, cycloalkyl or aryl), and CONR′R″ (where R′ and R″ independently are H, alkyl, cycloalkyl or aryl.
Ethyl 2-chloro-5-(6-(2-methoxyphenyl)pyrimidin-4-ylamino)benzoate.
2-Fluoro-N4-[6-(2-methoxy-phenyl)-pyrimidin-4-yl]-N1,N1-dimethyl-benzene-1,4-diamine.
2-Dimethylamino-5-[6-(2-methoxy-phenyl)-pyrimidin-4-ylamino]-phenol.
2-Dimethylamino-5-[6-(2-methoxy-phenyl)-pyrimidin-4-ylamino]-benzamide.
Ethyl 5-(6-(2-methoxyphenyl)pyrimidin-4-ylamino)-2-morpholinobenzoate.
2-(2-chloro-5-(6-(2-methoxyphenyl)pyrimidin-4-ylamino)benzyl)isoindoline-1,3-dione.
2-chloro-5-(6-(2-methoxyphenyl)pyrimidin-4-ylamino)benzamide.
N-(3-((1H-benzo[d]imidazol-1-yl)methyl)-4-(4-methylpiperazin-1-yl)phenyl)-6-(2-methoxyphenyl)pyrimidin-4-amine.
Dependencies are inferred from the claim text.