r-1487 and Arthritis--Rheumatoid

r-1487 has been researched along with Arthritis--Rheumatoid* in 1 studies

Other Studies

1 other study(ies) available for r-1487 and Arthritis--Rheumatoid

Article	Year
Discovery of 6-(2,4-difluorophenoxy)-2-[3-hydroxy-1-(2-hydroxyethyl)propylamino]-8-methyl-8H-pyrido[2,3-d]pyrimidin-7-one (pamapimod) and 6-(2,4-difluorophenoxy)-8-methyl-2-(tetrahydro-2H-pyran-4-ylamino)pyrido[2,3-d]pyrimidin-7(8H)-one (R1487) as orally Journal of medicinal chemistry, 2011, Apr-14, Volume: 54, Issue:7 The development of a new series of p38α inhibitors resulted in the identification of two clinical candidates, one of which was advanced into a phase 2 clinical study for rheumatoid arthritis. The original lead, an lck inhibitor that also potently inhibited p38α, was a screening hit from our kinase inhibitor library. This manuscript describes the optimization of the lead to p38-selective examples with good pharmacokinetic properties. Topics: Administration, Oral; Arthritis, Rheumatoid; Biological Availability; Cell Line; Clinical Trials as Topic; Drug Discovery; Humans; Mitogen-Activated Protein Kinase 14; Models, Molecular; Protein Conformation; Protein Kinase Inhibitors; Pyridones; Pyrimidines; Structure-Activity Relationship; Substrate Specificity	2011

Article

Year

Discovery of 6-(2,4-difluorophenoxy)-2-[3-hydroxy-1-(2-hydroxyethyl)propylamino]-8-methyl-8H-pyrido[2,3-d]pyrimidin-7-one (pamapimod) and 6-(2,4-difluorophenoxy)-8-methyl-2-(tetrahydro-2H-pyran-4-ylamino)pyrido[2,3-d]pyrimidin-7(8H)-one (R1487) as orally

Journal of medicinal chemistry, 2011, Apr-14, Volume: 54, Issue:7

The development of a new series of p38α inhibitors resulted in the identification of two clinical candidates, one of which was advanced into a phase 2 clinical study for rheumatoid arthritis. The original lead, an lck inhibitor that also potently inhibited p38α, was a screening hit from our kinase inhibitor library. This manuscript describes the optimization of the lead to p38-selective examples with good pharmacokinetic properties.

Topics: Administration, Oral; Arthritis, Rheumatoid; Biological Availability; Cell Line; Clinical Trials as Topic; Drug Discovery; Humans; Mitogen-Activated Protein Kinase 14; Models, Molecular; Protein Conformation; Protein Kinase Inhibitors; Pyridones; Pyrimidines; Structure-Activity Relationship; Substrate Specificity

2011