C - Chemistry – Metallurgy – 07 – D
Patent
C - Chemistry, Metallurgy
07
D
C07D 471/22 (2006.01) A61K 31/4985 (2006.01) A61K 31/519 (2006.01) A61K 31/5365 (2006.01) A61P 31/18 (2006.01) C07D 471/14 (2006.01) C07D 498/14 (2006.01)
Patent
CA 2606282
The present invention is to provide a novel compound (I), having the anti- virus activity, particularly the HIV integrase inhibitory activity, and a drug containing the same, particularly an anti-HIV drug, as well as a process and an intermediate thereof. Compound (I) wherein Z1 is NR4; R1 is hydrogen or lower alkyl; X is a single bond, a hetero atom group selected from O, S, SO, SO2 and NH, or lower alkylene or lower alkenylene in which the hetero atom group may intervene; R2 is optionally substituted aryl; R3 is hydrogen, a halogen, hydroxy, optionally substituted lower alkyl etc; and R4 and Z2 part taken together forms a ring, to form a polycyclic compound, including e.g., a tricyclic or tetracyclic compound.
L'invention porte: sur un nouveau composé (I) à activité antivirale et en particulier inhibitrice vis-à-vis de l'intégrase du VIH, et sur un médicament le contenant, en particulier un médicament anti VIH; et sur un procédé et son intermédiaire. Dans le nouveau composé (I): Z1 est NR4; R1 est hydrogène ou alkyle inférieur; X est une liaison simple, un hétéroatome choisi parmi O, S, SO, SO2 et NH, ou alkylène inférieur ou alcénylène inférieur, dans lequel l'hétéroatome peut intervenir; R2 est aryle facultativement substitué; R3 est hydrogène, halogène, hydroxy, alkyle inférieur facultativement substitué, etc; et R4 et Z2 pris ensemble forment un cycle servant à former un composé polycyclique par exemple tricyclique ou tétracyclique.
Johns Brian Alvin
Kawasuji Takashi
Taishi Teruhiko
Taoda Yoshiyuki
Ogilvy Renault Llp/s.e.n.c.r.l.,s.r.l.
Shionogi & Co. Ltd.
Smithkline Beecham Corporation
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