March 17, 2014

CAS databases provide millions of journal article references from more than 10,000 major scientific journals worldwide, patent and patent family references from 63 patent authorities around the world, and other reputable web sources.

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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