95629-02-0Relevant articles and documents
Further optimization of the mGlu5 PAM clinical candidate VU0409551/JNJ-46778212: Progress and challenges towards a back-up compound
Zhou, Ya,Malosh, Chrysa,Conde-Ceide, Susana,Martínez-Viturro, Carlos Manuel,Alcázar, Jesus,Lavreysen, Hilde,Mackie, Claire,Bridges, Thomas M.,Daniels, J. Scott,Niswender, Colleen M.,Jones, Carrie K.,Macdonald, Gregor J.,Steckler, Thomas,Conn, P. Jeffrey,Stauffer, Shaun R.,Bartolomé-Nebreda, José Manuel,Lindsley, Craig W.
, p. 3515 - 3519 (2015/08/06)
This Letter describes the progress and challenges in the continued optimization of the mGlu5 positive allosteric modulator (PAM) clinical candidate VU0490551/JNJ-46778212. While many analogs addressed key areas for improvement, no one compound possessed the amalgamation of improvements needed within the (2(phenoxymethyl)-6,7-dihydrooxazolo[5,4-c]pyridine-5(4H)-yl(aryl)methanone scaffold to advance as a back-up clinical candidate. However, many analogs displayed excellent solubility and physiochemical properties, and were active in the amphetamine-induced hyperlocomotion (AHL) model. Moreover, the SAR was robust for this series of PAMs, and both polar and hydrogen-bond donors were found to be tolerated, leading to analogs with overall attractive profiles and good ligand efficiencies. Graphical abstract
SUBSTITUTED SULFONAMIDE DERIVATIVES
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Page/Page column 143, (2009/11/29)
The invention relates to substituted sulfonamide derivatives, processes for the preparation thereof, medicaments containing these compounds and the use of substituted sulfonamide derivatives for the preparation of medicaments.
N-acylamino acid amide compounds and intermediates for preparation thereof
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, (2008/06/13)
The present invention discloses the compound represented by the formula (I): wherein A represents the following formula (a-1) or the following formula (a-2): B represents the following formula (b): (wherein the symbols are each as defined in the specification) or a pharmaceutically acceptable salts thereof, and intermediates for the preparation thereof, which have excellent platelet aggregation inhibitory activity and other properties and useful as prophylactic or therapeutic agents for diseases associated with a fibrinogen receptor, thrombosis, infarction and the like.