Discovery of MK-0952, a selective PDE4 inhibitor for the treatment of long-term memory loss and mild cognitive impairment.
Gallant, Michel; Aspiotis, Renee; Day, Stephen; Dias, Rebecca; Dubé, Daniel; Dubé, Laurence; Friesen, Richard W; Girard, Mario; Guay, Daniel; Hamel, Pierre; Huang, Zheng; Lacombe, Patrick; Laliberté, Sebastien; Lévesque, Jean-François; Liu, Susana; Macdonald, Dwight; Mancini, Joseph; Nicholson, Donald W; Styhler, Angela; Townson, Karen; Waters, Kerry; Young, Robert N; Girard, Yves.
Bioorg Med Chem Lett
; 20(22): 6387-93, 2010 Nov 15.
Artigo em Inglês | MEDLINE | ID: mdl-20933411
Structural findings of cinnolines as anti-schizophrenic PDE10A inhibitors through comparative chemometric modeling.
Discovery of [¹¹C]MK-8193 as a PET tracer to measure target engagement of phosphodiesterase 10A (PDE10A) inhibitors.
Synthesis and pharmacological characterization of a europium-labelled single-chain antagonist for binding studies of the relaxin-3 receptor RXFP3.
Treatment of chronic obstructive pulmonary disease with roflumilast, a new phosphodiesterase 4 inhibitor.
Preclinical Characterization of the Phosphodiesterase 10A PET Tracer [(11)C]MK-8193.
Discovery of triazines as selective PDE4B versus PDE4D inhibitors.
Synthesis of Peramine, an Anti-insect Defensive Alkaloid Produced by Endophytic Fungi of Cool Season Grasses.
Imidazo[1,2-a]pyridin-6-yl-benzamide analogs as potent RAF inhibitors.
An unusual spinaceamine-bearing pregnane from a soft coral Scleronephthya sp. inhibits the migration of tumor cells.
Identification of pyridazino[4,5-b]indolizines as selective PDE4B inhibitors.