March 17, 2014

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The following patent record is from the CAplusSM database.


Patent Number: WO 2014008636
Title: Preparation of macrocyclic compounds as HIV integrase inhibitors
Inventor(s): Reger, Thomas; Walji, Abbas M.; Sanders, John M.; Wai, John S.; Hu, Lihong; Fang, Shunda; Wang, Liping; Yang, Pengyu; Ma, Zonghui; Sun, Liansheng
Patent Assignee(s): Merck Sharp & Dohme Corp., USA
Source: PCT Int. Appl., 90pp. CODEN: PIXXD2
Language: English

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.

Please note:  Abstracts and Titles for patent records in CAplus are routinely enhanced to better describe the claimed invention.

 View the full-text here.

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