1232505-77-9Relevant articles and documents
Novel Series of Dihydropyridinone P2X7 Receptor Antagonists
Lopez-Tapia, Francisco,Walker, Keith A. M.,Brotherton-Pleiss, Christine,Caroon, Joanie,Nitzan, Dov,Lowrie, Lee,Gleason, Shelley,Zhao, Shu-Hai,Berger, Jacob,Cockayne, Debra,Phippard, Deborah,Suttmann, Rebecca,Fitch, William L.,Bourdet, David,Rege, Pankaj,Huang, Xiaojun,Broadbent, Scott,Dvorak, Charles,Zhu, Jiang,Wagner, Paul,Padilla, Fernando,Loe, Brad,Jahangir, Alam,Alker, André
, p. 8413 - 8426 (2015/11/24)
Identification of singleton P2X7 inhibitor 1 from HTS gave a pharmacophore that eventually turned into potential clinical candidates 17 and 19. During development, a number of issues were successfully addressed, such as metabolic stability, plasma stability, GSH adduct formation, and aniline mutagenicity. Thus, careful modification of the molecule, such as conversion of the 1,4-dihydropyridinone to the 1,2-dihydropyridinone system, proper substitution at C-5″, and in some cases addition of fluorine atoms to the aniline ring allowed for the identification of a novel class of potent P2X7 inhibitors suitable for evaluating the role of P2X7 in inflammatory, immune, neurologic, or musculoskeletal disorders.
FUSED TRIAZOLE AMINES AS P2X7 MODULATORS
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, (2011/04/18)
Compounds of the formula I: or pharmaceutically acceptable salts thereof, wherein X, Y, R1, R2, and R3 are as defined herein. Also disclosed are methods of making the compounds and using the compounds for treatment of dise
DIHYDROPYRIMIDONE AMIDES AS P2X7 MODULATORS
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Page/Page column 44-45, (2011/02/25)
Compounds of the formula I: or pharmaceutically acceptable salts thereof, wherein m, n, R1, R2, R3, R4, R5, Ra and Rb are as defined herein. Also disclosed are methods of making the compounds and using the compounds for treatment of diseases associated with the P2X7 purinergic receptor.
DIHYDROPYRIDONE UREAS AS P2X7 MODULATORS
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Page/Page column 58, (2010/07/04)
Compounds of the formula I: or pharmaceutically acceptable salts thereof, wherein m, n, R1, R2, R3, R4 and R5 are as defined herein. Also disclosed are methods of making the compounds and using the compounds for treatment of diseases associated with the P2X7 purinergic receptor.
DIHYDROPYRIDONE AMIDESAS P2X7 MODULATORS
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Page/Page column 49, (2010/07/04)
Compounds of the formula I: or pharmaceutically acceptable salts thereof, wherein m, n, R1, R2, R3, R4, R5 and Ra are as defined herein. Also disclosed are methods of making the compounds and using the compounds for treatment of diseases associated with the P2X7 purinergic receptor.