70232-59-6Relevant articles and documents
Design, Synthesis, and Preclinical Evaluation of 3-Methyl-6-(5-thiophenyl)-1,3-dihydro-imidazo[4,5-b]pyridin-2-ones as Selective GluN2B Negative Allosteric Modulators for the Treatment of Mood Disorders
Chrovian, Christa C.,Soyode-Johnson, Akinola,Stenne, Brice,Pippel, Daniel J.,Schoellerman, Jeffrey,Lord, Brian,Needham, Alexandra S.,Xia, Chungfang,Coe, Kevin J.,Sepassi, Kia,Schoetens, Freddy,Scott, Brian,Nguyen, Leslie,Jiang, Xiaohui,Koudriakova, Tatiana,Balana, Bartosz,Letavic, Michael A.
, p. 9181 - 9196 (2020/10/18)
Selective inhibitors of the GluN2B subunit of N-methyl-d-aspartate receptors in the ionotropic glutamate receptor superfamily have been targeted for the treatment of mood disorders. We sought to identify structurally novel, brain penetrant, GluN2B-selective inhibitors suitable for evaluation in a clinical setting in patients with major depressive disorder. We identified a new class of negative allosteric modulators of GluN2B that contain a 1,3-dihydro-imidazo[4,5-b]pyridin-2-one core. This series of compounds had poor solubility properties and poor permeability, which was addressed utilizing two approaches. First, a series of structural modifications was conducted which included replacing hydrogen bond donor groups. Second, enabling formulation development was undertaken in which a stable nanosuspension was identified for lead compound 12. Compound 12 was found to have robust target engagement in rat with an ED70 of 1.4 mg/kg. The nanosuspension enabled sufficient margins in preclinical toleration studies to nominate 12 for progression into advanced good laboratory practice studies.
AMINOQUINOLINE DERIVATIVES AS ANTIVIRAL AGENTS
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Page/Page column 245, (2012/04/04)
Provided are compounds of Formula (I) and Formula (II) and pharmaceutically acceptable salts thereof, their pharmaceutical compositions, their methods of preparation, and their use for treating viral infections mediated by a member of the Flaviviridae family of viruses such as hepatitis C virus (HCV).
INHIBITORS OF HIV REPLICATION
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Page/Page column 89, (2010/11/03)
Compounds of formula (I): wherein R1, R2, A1, A2, A3, A4, X and Y are as defined herein, are useful as inhibitors of HIV replication.