C - Chemistry – Metallurgy – 07 – D
Patent
C - Chemistry, Metallurgy
07
D
C07D 471/04 (2006.01) C07D 207/404 (2006.01) C07D 487/04 (2006.01) C07D 498/20 (2006.01) C07D 513/00 (2006.01)
Patent
CA 2501881
Tricyclic compounds according to the structure below, protected intermediates thereof, and methods for inhibition of HIV-integrase are disclosed. Formula (I). Al and A2 are moieties forming a five, six, or seven membered ring. L is a bond or a linker connecting a ring atom of Ar to N. X is O, S, or substituted nitrogen. Ar is aryl or heteroaryl. Q is N, +NR, or CR4. The aryl carbons may be independently substituted with substituents other than hydrogen. The compounds may include prodrug moieties covalently attached at any site.
L'invention concerne des composés tricycliques de formule (I), des intermédiaires protégés de ceux-ci, et des méthodes pour inhiber l'intégrase du VIH. Formule (I), où A?1¿ et A?2¿ sont des fractions formant un noyau de cinq, six ou sept éléments, L est une liaison ou un lieur liant un atome cyclique de Ar à N, X signifie O, S ou de l'azote substitué, Ar désigne aryle ou hétéroaryle, Q représente N, ?+¿NR ou CR?4¿. Les carbones aryle peuvent être indépendamment substitués par des substituants autres que l'hydrogène. Ces composés peuvent comprendre des fractions de promédicaments liées par covalence à un site quelconque.
Chen James M.
Chen Xiaowu
Fardis Maria
Jin Haolun
Kim Choung U.
Gilead Sciences Inc.
Robic
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