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CAPLUS COPYRIGHT 2014 ACS
||Preparation of macrocyclic compounds as HIV integrase inhibitors
||Reger, Thomas; Walji, Abbas M.; Sanders, John M.; Wai, John S.; Hu, Lihong; Fang, Shunda; Wang, Liping; Yang, Pengyu; Ma, Zonghui; Sun, Liansheng
||Merck Sharp & Dohme Corp., USA
||PCT Int. Appl., 90pp. CODEN: PIXXD2
The invention relates to pyrimidonyl macrocyclic compds. of formula I as HIV integrase inhibitors; their prepn. and use in the treatment of HIV infection. Macrocyclic compds. of formula I wherein G is O and CHR3; Q is CO and SO2; W is a bond, O, NH and derivs.; X is a bond and CO; Y is C3-5 alkylene and C3-5 alkenylene; Z is a bond, O and NHCO and derivs.; each R1 is independently H, C1-6 alkyl, halo, etc.; R2, R3, R4, R5 are independently H, C1-6 alkyl, halo, etc.; R6 is H, C1-6 alkyl, 3- to 7-membered cycloalkyl, etc.; and pharmaceutically acceptable salts and prodrugs thereof, are claimed. Example compd. II was prepd. by a general procedure (procedure given). The invention compds. were evaluated for their HIV integrase inhibitory activity. From the assay, it was detd. that example compd. II exhibited IC95 value of 9 nM.
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