321352-52-7Relevant articles and documents
INHIBITORS OF MTOR-MEDIATED INDUCTION OF AUTOPHAGY
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Paragraph 088, (2021/04/30)
The invention provides amides that inhibit apoptosis or induce autophagy through mTOR-mediated induction of autophagy, or inhibit a related disease such as cerebral ischemia/reperfusion or neurodegenerative diseases, including corresponding sulfonamides, and pharmaceutically acceptable salts, hydrates and stereoisomers thereof. The compounds are employed in pharmaceutical compositions, and methods of making and use, including treating a person in need thereof with an effective amount of the compound or composition, and detecting a resultant improvement in the person's health or condition.
Structure based evolution of a novel series of positive modulators of the AMPA receptor
Jamieson, Craig,MacLean, John K.F.,Brown, Christopher I.,Campbell, Robert A.,Gillen, Kevin J.,Gillespie, Jonathan,Kazemier, Bert,Kiczun, Michael,Lamont, Yvonne,Lyons, Amanda J.,Moir, Elizabeth M.,Morrow, John A.,Pantling, John,Rankovic, Zoran,Smith, Lynn
scheme or table, p. 805 - 811 (2011/02/27)
Starting from compound 1, we utilized biostructural data to successfully evolve an existing series into a new chemotype with a promising overall profile, exemplified by 19.
Discovery of N -[(2 s)-5-(6-fluoro-3-pyridinyl)-2,3-dihydro-1 H -inden-2-yl]-2-propanesulfonamide, a novel clinical AMPA receptor positive modulator
Ward, Simon E.,Harries, Mark,Aldegheri, Laura,Andreotti, Daniele,Ballantine, Stuart,Bax, Benjamin D.,Harris, Andrew J.,Harker, Andy J.,Lund, Jesper,Melarange, Rosemary,Mingardi, Anna,Mookherjee, Claudette,Mosley, Julie,Neve, Marta,Oliosi, Beatrice,Profeta, Roberto,Smith, Kathrine J.,Smith, Paul W.,Spada, Simone,Thewlis, Kevin M.,Yusaf, Shahnaz P.
scheme or table, p. 5801 - 5812 (2010/11/05)
A series of AMPA receptor positive allosteric modulators has been optimized from poorly penetrant leads to identify molecules with excellent preclinical pharmacokinetics and CNS penetration. These discoveries led to 17i, a potent, efficacious CNS penetrant molecule with an excellent pharmacokinetic profile across preclinical species, which is well tolerated and is also orally bioavailable in humans.
