713145-53-0Relevant articles and documents
Solubility-driven optimization of phosphodiesterase-4 inhibitors leading to a clinical candidate
Press, Neil J.,Taylor, Roger J.,Fullerton, Joseph D.,Tranter, Pamela,McCarthy, Clive,Keller, Thomas H.,Arnold, Nicola,Beer, David,Brown, Lyndon,Cheung, Robert,Christie, Julie,Denholm, Alastair,Haberthuer, Sandra,Hatto, Julia D. I.,Keenan, Mark,Mercer, Mark K.,Oakman, Helen,Sahri, Helene,Tuffnell, Andrew R.,Tweed, Morris,Tyler, John W.,Wagner, Trixie,Fozard, John R.,Trifilieff, Alexandre
, p. 7472 - 7479 (2012)
The solubility-driven optimization of a series of 1,7-napthyridine phosphodiesterase-4 inhibitors is described. Directed structural changes resulted in increased aqueous solubility, enabling superior pharmacokinetic properties with retention of PDE4 inhib
[1,7]NAPHTHYRIDINES AS PDE4 INHIBITORS
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Page 20, (2008/06/13)
Compounds of Formula (I) in free or salt form, wherein R1, R2 and R3 have the meanings as indicated in the specification, are useful for treating conditions mediated by of phosphodiesterase type 4 or the down-regulation or inhibition of TNF-α release, particularly obstructive or inflammatory airways diseases. Pharmaceutical compositions that contain the compounds and processes for preparing the compounds are also described.