1365887-45-1Relevant articles and documents
9-SUBSTITUTED AMINO TRIAZOLO QUINAZOLINE DERIVATIVES AS ADENOSINE RECEPTOR ANTAGONISTS, PHARMACEUTICAL COMPOSITIONS AND THEIR USE
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, (2020/06/19)
In its many embodiments, the present invention provides certain 9-substituted amino triazolo quinazoline compounds of the structural Formula (I): (I), and pharmaceutically acceptable salts thereof, wherein, ring A, R1 and R2 are as defined herein, pharmaceutical compositions comprising one or more such compounds (alone and in combination with one or more other therapeutically active agents), and methods for their preparation and use, alone and in combination with other therapeutic agents, as antagonists of A2a and/or A2b receptors, and in the treatment of a variety of diseases, conditions, or disorders that are mediated, at least in part, by the adenosine A2a receptor and/or the adenosine A2b receptor.
1,5-Substituted nipecotic amides: Selective PDE8 inhibitors displaying diastereomer-dependent microsomal stability
DeNinno, Michael P.,Wright, Stephen W.,Visser, Michael S.,Etienne, John B.,Moore, Dianna E.,Olson, Thanh V.,Rocke, Benjamin N.,Andrews, Melissa P.,Zarbo, Cynthia,Millham, Michele L.,Boscoe, Brian P.,Boyer, David D.,Doran, Shawn D.,Houseknecht, Karen L.
, p. 3095 - 3098 (2011/06/24)
The first highly potent and selective PDE8 inhibitors are disclosed. The initial tetrahydroisoquinoline hit was transformed into a nipecotic amide series in order to address a reactive metabolite issue. Reduction of lipophilicity to address metabolic liab
