- Spiro aryl phosphorus oxide or sulfide
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The invention discloses a spiro aryl phosphorus oxide or sulfide as ALK inhibitor, and in particular discloses a compound shown in a formula (I) as an ALK inhibitor or a pharmaceutically acceptable salt thereof.
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- Design and synthesis of spirocyclic compounds as HCV replication inhibitors by targeting viral NS4B protein
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Two novel series of spirocyclic piperidine analogs appended to a pyrazolo[1,5-a]pyridine core were designed, synthesized and evaluated for their anti-HCV activity. A series of piperidine ketals afforded dispiro 6p which showed excellent in vitro anti-HCV activities (EC50 of 1.5 nM and 1.2 nM against genotype 1a and 1b replicons, respectively). A series of piperidine oxazolidinones afforded 27c which showed EC50's of 10.9 nM and 6.1 nM against 1a and 1b replicons, respectively. Both compounds 6p and 27c bound directly to non-structural NS4B protein in vitro (IC50's = 10.2 and 30.4 nM, respectively) and exhibited reduced potency in replicons containing resistance mutations encoding changes in the NS4B protein.
- Tai, Vincent W.-F.,Garrido, Dulce,Price, Daniel J.,Maynard, Andrew,Pouliot, Jeffrey J.,Xiong, Zhiping,Seal, John W.,Creech, Katrina L.,Kryn, Luz H.,Baughman, Todd M.,Peat, Andrew J.
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p. 2288 - 2294
(2014/05/20)
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- SUBSTITUTED QUINOLONES III
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The invention relates to substituted quinolones and to methods for their preparation as well as to their use for the production of medicaments for the treatment and/or prophylaxis of diseases, especially for use as antiviral agents, particularly against cytomegaloviruses.
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Page/Page column 25
(2009/07/25)
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