- NOVEL HEPATITIS C VIRUS INHIBITORS
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The invention provides compounds of formula (I): wherein Rings A and A' are independently 5-membered optionally substituted aromatic heterocycles; Q is C(=O)NR1R1' or formula U is C(R4)2, O, S, S(=O)2, C(R4)2C(R4)2, CH2O, OCH2, CH2S, SCH2, CH2S(=O)2, S(=O)CH2 or C=C(Ru )2; X is CH2, CHR12, CR12R12, O, S, S(=O)2 or NRx; m is 0, 1, 2 or 3; n is 0, 1, 2 or 3; the other variables are as defined in the claims, which are of use in the treatment or prophylaxis of hepatitis C virus infection, and related aspects.
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- Total synthesis of (+)-brefeldin C, (+)-nor-Me brefeldin A and (+)-4-epi-nor-Me brefeldin A
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A total synthesis of (+)-brefeldin C (BFC) and two brefeldin A (BFA) analogues - (+)-nor-Me BFA and (+)-4-epi-nor-Me BFA - has been developed. Key features of the syntheses include desymmetrization of meso anhydrides, a Carreira reaction to control the ab
- Archambaud, Sylvie,Legrand, Frederic,Aphecetche-Julienne, Karine,Collet, Sylvain,Guingant, Andre,Evain
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experimental part
p. 1364 - 1380
(2010/05/03)
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- α,β-Cyclic-β-benzamido hydroxamic acids: Novel templates for the design, synthesis, and evaluation of selective inhibitors of TNF-α converting enzyme (TACE)
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Selective inhibitors of TNF-α Converting Enzyme (TACE) based on (1R,2S)-cyclopentyl, (3S,4S)-pyrrolidinyl, and (3R,4S)-tetrahydrofuranyl β-benzamido hydroxamic acids have been synthesized and evaluated. This study has led to the discovery of novel inhibitors whose profiles include activity against TACE in an enzyme assay, potency in the suppression of LPS-stimulated TNF-α in human whole blood, selectivity against a panel of MMPs and oral bioavailability.
- Ott, Gregory R.,Asakawa, Naoyuki,Lu, Zhonghui,Liu, Rui-Qin,Covington, Maryanne B.,Vaddi, Krishna,Qian, Mingxin,Newton, Robert C.,Christ, David D.,Traskos, James M.,Decicco, Carl P.,Duan, James J.-W.
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p. 694 - 699
(2008/09/17)
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- Enantioselective synthesis of an advanced intermediate for the synthesis of brefeldin A and analogues
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A synthesis of methyl (1R,2R,4S)-2-[(E)-2-iodovinyl]-4-(methoxymethoxy) cyclopentanecarboxylate is described in nine steps from a prochiral anhydride. A desymmetrization reaction followed by an epimerization and a Takai reaction are the key steps of the t
- Legrand, Frédéric,Archambaud, Sylvie,Collet, Sylvain,Aphecetche-Julienne, Karine,Guingant, André,Evain, Michel
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p. 389 - 393
(2008/09/17)
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