- Design of a series of bicyclic HIV-1 integrase inhibitors. Part 1: Selection of the scaffold
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HIV integrase inhibitors based on a novel bicyclic pyrimidinone core is presented. Nine variations of the core scaffold are evaluated leading to optimization of the 6:6 core giving compound 48 with an EC50 of 3 nM against wild type HIV infected T-cells.
- Jones, Eric D.,Vandegraaff, Nick,Le, Giang,Choi, Neil,Issa, William,MacFarlane, Katherine,Thienthong, Neeranat,Winfield, Lisa J.,Coates, Jonathan A.V.,Lu, Long,Li, Xinming,Feng, Xiao,Yu, Changjiang,Rhodes, David I.,Deadman, John J.
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scheme or table
p. 5913 - 5917
(2010/11/18)
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- BICYCLIC PYRIMIDINONES AND USES THEREOF
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The present invention provides a compound of Formula I or a pharmaceutically acceptable derivative, salt or prodrug thereof. Further provided is a method of treatment or prophylaxis of a viral infection in a subject comprising administering to said subject an effective amount of a compound of Formula I or a pharmaceutically acceptable derivative, salt or prodrug thereof. A pharmaceutical composition or medicament comprising a compoundof Formula I is also provided.
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Page/Page column 24-25
(2008/12/06)
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- PREPARATION AND DIELS-ALDER CYCLOADDITIONS OF SUBSTITUTED VINYLENE CARBONATES (1,3-DIOXOL-2-ONES) AND RELATED COMPOUNDS
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Several substituted vinylene carbonates have been prepared by efficient routes and the dienophilicity of these and related compounds in Diels-Alder cycloadditions has been evaluated.
- Jung, Michael E.,Blum, Roberto B.,Gaede, Bruce J.,Gisler, Matthias R.
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- Hydrated Oxocarbons, I. Preparation and Reactions of Tetrakiscyclobutanes
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Octahydroxycyclobutane (1) reacts with various monoorganoboranes to give in high yields the tetrakis derivatives 2a - d.These react with tertiary amines to yield either 1:2 or 1:4 adducts.Depending on the organo substituents at the boron atoms, alcoholyses of 2a - d result in either partial or complete deborylation giving e.g. tetraalkoxybis derivatives of the cyclobutane ring (7b, c), or, with ring-opening, dimethyl dihydroxyfumarate (5).
- Yalpani, Mohamed,Koester, Roland,Wilke, Guenther
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p. 1336 - 1344
(2007/10/02)
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