- INDOLE DERIVATIVES AND THEIR USE AS THYROID RECEPTOR LIGANDS
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The invention provides compounds of formula (I) or pharmaceutically acceptable esters, amides, solvates or salts thereof, including salts of such esters or amides, and solvates of such esters, amides or salts, (I) wherein R1, R2, R3, R4, R5, R6, Y and W are as defined in the specification. The invention also provides the use of such compounds in the treatment or prophylaxis of a condition that may be treated with a thyroid receptor agonist or partial agonist.
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Page/Page column 33
(2008/06/13)
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- Thyroid receptor ligands. Part 4: 4′-amido bioisosteric ligands selective for the thyroid hormone receptor beta
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Based on the examination of the X-ray crystallographic structures of the LBD of TRα and TRβ in complex with KB-141 (2), a number of novel 4′-hydroxy bioisosteric thyromimetics were prepared. Optimal affinity and β-selectivity (33 times), was found with a medium-sized alkyl-substituted amido group; iso-butyl (12c). It can be concluded that bioisosteric replacements of the 4′-hydroxy position represent a new promising class of TRβ-selective synthetic thyromimetics.
- Li, Yi-Lin,Litten, Chris,Koehler, Konrad F.,Mellstroem, Karin,Garg, Neeraj,Garcia Collazo, Ana Maria,Faernegard, Mathias,Grynfarb, Marlena,Husman, Bolette,Sandberg, Johnny,Malm, Johan
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p. 884 - 886
(2007/10/03)
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