申请人:GILEAD SCIENCES, INC.
公开号:US20040157804A1
公开(公告)日:2004-08-12
Tricyclic compounds according to the structure below, protected intermediates thereof, and methods for inhibition of HIV-integrase are disclosed.
1
A
1
and A
2
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 CR
4
. The aryl carbons may be independently substituted with substituents other than hydrogen. The compounds may include prodrug moieties covalently attached at any site.
本发明揭示了以下结构的三环化合物、其保护中间体以及抑制HIV整合酶的方法。其中,1A1和A2是形成五、六或七元环的基团。L是连接Ar环原子和N原子的键或连接器。X为O、S或取代氮。Ar为芳基或杂环芳基。Q为N、+NR或CR4。芳基碳可以独立地被取代为除氢以外的取代基。化合物可以包括共价连接在任何位点的前药基团。