- DEUTERATED PHENYLPROPIONIC ACID DERIVATIVE
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A compound corresponding to 3-[4-[(5,6,7,8-tetrahydro-5,5,8,8-tetramethyl-2-naphthalenyl)carbamoyl]phenyl]propionic acid in which a part or all of hydrogen atoms in the ethylene group constituting the propionic acid moiety are replaced with deuterium atoms, a salt thereof, or an ester thereof, and a prodrug for releasing Am80 as an active medicament after being absorbed into a living body, which comprises the aforementioned compound, a salt thereof, or an ester thereof as an active ingredient.
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Paragraph 0044-0045
(2014/05/08)
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- Synthesis of Am80 (tamibarotene) prodrug candidates, congeners and metabolites
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Compound 1 (IT-M-07000) was previously reported as a candidate prodrug of Am80 (Tamibarotene; used to treat acute promyelocytic leukemia), and shown to be efficiently metabolized to Am80 via β-oxidation. Here, we describe in detail the synthesis of 1, together with another tetradeuterated candidate prodrug, IT-YA-00616 (2), as well as two congeners, and several metabolic intermediates of 1 previously detected in mouse plasma.
- Muratake, Hideaki,Amano, Yohei,Toda, Takahiro,Sugiyama, Kiyoshi,Shudo
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p. 846 - 852
(2013/09/12)
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