1393809-97-6Relevant academic research and scientific papers
SUBSTRATE SELECTIVE INHIBITORS OF INSULIN-DEGRADING ENZYME (IDE) AND USES THEREOF
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Paragraph 00821, (2016/11/17)
Provided herein are compounds of Formulae (RL), (I), (II), (III), (IV), and (V), and pharmaceutically acceptable salts, solvates, hydrates, polymorphs, co-crystals, tautomers, stereoisomers, prodrugs, and isotopically labeled derivatives thereof. Also provided are pharmaceutical compositions, kits, and methods involving the inventive compounds for the treatment of metabolic disorders (e.g., diabetes, hyperglycemia, impaired glucose tolerance, insulin resistance, obesity). The compound are useful as substrate selective inhibitors of insulin-degrading enzyme (IDE).
Synthesis and profiling of a diverse collection of azetidine-based scaffolds for the development of CNS-focused lead-like libraries
Lowe, Jason T.,Lee, Maurice D.,Akella, Lakshmi B.,Davoine, Emeline,Donckele, Etienne J.,Durak, Landon,Duvall, Jeremy R.,Gerard, Baudouin,Holson, Edward B.,Joliton, Adrien,Kesavan, Sarathy,Lemercier, Berenice C.,Liu, Haibo,Marie, Jean-Charles,Mulrooney, Carol A.,Muncipinto, Giovanni,Welzel-O'Shea, Morgan,Panko, Laura M.,Rowley, Ann,Suh, Byung-Chul,Thomas, Meryl,Wagner, Florence F.,Wei, Jingqiang,Foley, Michael A.,Marcaurelle, Lisa A.
, p. 7187 - 7211 (2012/10/30)
The synthesis and diversification of a densely functionalized azetidine ring system to gain access to a wide variety of fused, bridged, and spirocyclic ring systems is described. The in vitro physicochemical and pharmacokinetic properties of representative library members are measured in order to evaluate the use of these scaffolds for the generation of lead-like molecules to be used in targeting the central nervous system. The solid-phase synthesis of a 1976-membered library of spirocyclic azetidines is also described.
