75438-77-6Relevant academic research and scientific papers
Discovery of triazolopyrimidine-based PDE8B inhibitors: Exceptionally ligand-efficient and lipophilic ligand-efficient compounds for the treatment of diabetes
Deninno, Michael P.,Wright, Stephen W.,Etienne, John B.,Olson, Thanh V.,Rocke, Benjamin N.,Corbett, Jeffrey W.,Kung, Daniel W.,Dirico, Kenneth J.,Andrews, Kim M.,Millham, Michele L.,Parker, Janice C.,Esler, William,Van Volkenburg, Maria,Boyer, David D.,Houseknecht, Karen L.,Doran, Shawn D.
scheme or table, p. 5721 - 5726 (2012/09/22)
PDE8B is a cAMP-specific isoform of the broader class of phosphodiesterases (PDEs). As no selective PDE8B inhibitors had been reported, a high throughput screen was run with the goal of identifying selective tools for exploring the potential therapeutic utility of PDE8B inhibition. Of the numerous hits, one was particularly attractive since it was amenable to rapid deconstruction leading to inhibitors with very high ligand efficiency (LE) and lipophilic ligand efficiency (LLE). These triazolopyrimidines were optimized for potency, selectivity and ADME properties ultimately leading to compound 42. This compound was highly potent and selective with good bioavailability and advanced into pre-clinical development.
SUBSTITUTED TRIAZOLOPYRIMIDINES AS PDE8 INHIBITORS
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Page/Page column 31, (2011/06/16)
Compounds of Formula (I): wherein R1 , R2, R3, R4, and R5 are as defined herein, are disclosed.
First dual M3 antagonists-PDE4 inhibitors: Synthesis and SAR of 4,6-diaminopyrimidine derivatives
Provins, Laurent,Christophe, Bernard,Danhaive, Pierre,Dulieu, Jacques,Durieu, Véronique,Gillard, Michel,Lebon, Florence,Lengelé, Sébastien,Quéré, Luc,Van Keulen, Berendjan
, p. 1834 - 1839 (2007/10/03)
SAR around 4,6-diaminopyrimidine derivatives allowed the discovery of the first potent dual M3 antagonists and PDE4 inhibitors. Various chemical modulations around that scaffold led to the discovery of ucb-101333-3 which is characterized by the
CHEMICAL COMPOUNDS WITH DUAL ACTIVITY, PROCESSES FOR THEIR PREPARATION AND PHARMACEUTICAL COMPOSITIONS
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Page/Page column 31-32, (2008/06/13)
The present invention concerns chemical compounds combining affinity and antagonism against the human m3 muscarinic receptor with activity as selective phosphodiesterase IV (PDE IV) inhibitors, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals.
Substituted aminopyrimidines
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, (2008/06/13)
The present invention is directed to certain aminopyrimidines of the general formula STR1 wherein R1, R2, and R3 are hydrogen, halogen, alkoxy, alkylthio, or alkyl having 1 to 4 carbon atoms, or cycloalkyl having 3 to 5 carbon atoms and R4 is hydrogen or an aliphatic or aromatic acyl group, as well as physiologically compatible acid addition salts thereof. Compounds of the present invention are useful as blood pressure lowering agents and in the treatment of glaucoma.
