4-[[9-[(3R)-3-oxolanyl]-8-(2-4-6-trifluoroanilino)-2-purinyl]amino]-1-cyclohexanol and Idiopathic-Pulmonary-Fibrosis

4-[[9-[(3R)-3-oxolanyl]-8-(2-4-6-trifluoroanilino)-2-purinyl]amino]-1-cyclohexanol has been researched along with Idiopathic-Pulmonary-Fibrosis* in 1 studies

Other Studies

1 other study(ies) available for 4-[[9-[(3R)-3-oxolanyl]-8-(2-4-6-trifluoroanilino)-2-purinyl]amino]-1-cyclohexanol and Idiopathic-Pulmonary-Fibrosis

Article	Year
Discovery of CC-930, an orally active anti-fibrotic JNK inhibitor. Bioorganic & medicinal chemistry letters, 2012, Feb-01, Volume: 22, Issue:3 In this Letter we describe the discovery of potent, selective, and orally active aminopurine JNK inhibitors. Improving the physico-chemical properties as well as increasing the potency and selectivity of a subseries with rat plasma exposure, led to the identification of four structurally diverse inhibitors. Differentiation based on PK profiles in multiple species as well as activity in a chronic efficacy model led to the identification of 1 (CC-930) as a development candidate, which is currently in Phase II clinical trial for IPF. Topics: Administration, Oral; Animals; Catalytic Domain; Cyclohexanols; Dogs; Enzyme Activation; Enzyme Inhibitors; Haplorhini; Idiopathic Pulmonary Fibrosis; Inhibitory Concentration 50; MAP Kinase Kinase 4; Models, Molecular; Molecular Structure; Purines; Rats; Structure-Activity Relationship	2012

Article

Year

Discovery of CC-930, an orally active anti-fibrotic JNK inhibitor.

Bioorganic & medicinal chemistry letters, 2012, Feb-01, Volume: 22, Issue:3

In this Letter we describe the discovery of potent, selective, and orally active aminopurine JNK inhibitors. Improving the physico-chemical properties as well as increasing the potency and selectivity of a subseries with rat plasma exposure, led to the identification of four structurally diverse inhibitors. Differentiation based on PK profiles in multiple species as well as activity in a chronic efficacy model led to the identification of 1 (CC-930) as a development candidate, which is currently in Phase II clinical trial for IPF.

Topics: Administration, Oral; Animals; Catalytic Domain; Cyclohexanols; Dogs; Enzyme Activation; Enzyme Inhibitors; Haplorhini; Idiopathic Pulmonary Fibrosis; Inhibitory Concentration 50; MAP Kinase Kinase 4; Models, Molecular; Molecular Structure; Purines; Rats; Structure-Activity Relationship

2012