1353570-14-5Relevant articles and documents
Design and synthesis of aminothiazole modulators of the gamma-secretase enzyme
Rynearson, Kevin D.,Buckle, Ronald N.,Barnes, Keith D.,Herr, R. Jason,Mayhew, Nicholas J.,Paquette, William D.,Sakwa, Samuel A.,Nguyen, Phuong D.,Johnson, Graham,Tanzi, Rudolph E.,Wagner, Steven L.
, p. 3928 - 3937 (2016)
The design and construction of a series of novel aminothiazole-derived γ-secretase modulators is described. The incorporation of heterocyclic replacements of the terminal phenyl D-ring of lead compound 1 was conducted in order to align potency with favorable drug-like properties. γ-Secretase modulator 28 displayed good activity for in vitro inhibition of Aβ42, as well as substantial improvement in ADME and physicochemical properties, including aqueous solubility. Pharmacokinetic evaluation of compound 28 in mice revealed good brain penetration, as well as good clearance, half-life, and volume of distribution which collectively support the continued development of this class of compounds.
COMPOUNDS AND USES THEREOF IN MODULATING LEVELS OF VARIOUS AMYLOID BETA PEPTIDE ALLOFORMS
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Page/Page column 71, (2012/01/14)
The invention provides a novel compound having a structure corresponding to Formula (I): (A)-(B)-(C)-(D) or a pharmaceutically acceptable salt or prodrug thereof and methods for using them.