- Design and campaign synthesis of piperidine- and thiazole-based histone deacetylase inhibitors
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A lead benzamide, 3, was identified as a potent and low molecular weight histone deacetylase (HDAC) inhibitor. Optimization led to 16d, demonstrating an excellent balance of efficacy and non-efficacy properties, along with very desirable in vivo DMPK. The
- Andrews, David M.,Stokes, Elaine S.E.,Carr, Greg R.,Matusiak, Zbigniew S.,Roberts, Craig A.,Waring, Michael J.,Brady, Madeleine C.,Chresta, Christine M.,East, Simon J.
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p. 2580 - 2584
(2008/12/21)
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- BENZAMIDE DERIVATIVES USEFUL AS HISTONE DEACETYLASE INHIBITORS
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The invention concerns a compound of the formula (I) wherein Ring A is heterocyclyl; m is 0-4 and each R1 is a group such as hydroxy, halo, trifluoromethyl and cyano; R2 is halo and n is 0-2; and each R4 is a group such as hydroxy, halo, trifluromethyl and cyano; p is 0-4; and R3 is amino or hydroxy; or pharmaceutically-acceptable salts or in-vivo-hydrolysable ester or amide thereof processes for their preparation, pharmaceutical compositions containing them and their use in the treatment of diseases or medical condions mediated by histone deacetylase
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Page/Page column 31-32
(2008/06/13)
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