glpg0634 and Arthritis

glpg0634 has been researched along with Arthritis* in 1 studies

Other Studies

1 other study(ies) available for glpg0634 and Arthritis

Article	Year
Triazolopyridines as selective JAK1 inhibitors: from hit identification to GLPG0634. Journal of medicinal chemistry, 2014, Nov-26, Volume: 57, Issue:22 Janus kinases (JAK1, JAK2, JAK3, and TYK2) are involved in the signaling of multiple cytokines important in cellular function. Blockade of the JAK-STAT pathway with a small molecule has been shown to provide therapeutic immunomodulation. Having identified JAK1 as a possible new target for arthritis at Galapagos, the compound library was screened against JAK1, resulting in the identification of a triazolopyridine-based series of inhibitors represented by 3. Optimization within this chemical series led to identification of GLPG0634 (65, filgotinib), a selective JAK1 inhibitor currently in phase 2B development for RA and phase 2A development for Crohn's disease (CD). Topics: Adenosine Triphosphate; Animals; Arthritis; Chemistry, Pharmaceutical; Collagen; Crohn Disease; Crystallography, X-Ray; Cytokines; Dimerization; Disease Models, Animal; Drug Design; Drug Evaluation, Preclinical; Humans; Inhibitory Concentration 50; Janus Kinase 1; Kinetics; Phosphorylation; Protein Kinase Inhibitors; Pyridines; Rats; Recombinant Proteins; Structure-Activity Relationship; Triazoles	2014

Article

Year

Triazolopyridines as selective JAK1 inhibitors: from hit identification to GLPG0634.

Journal of medicinal chemistry, 2014, Nov-26, Volume: 57, Issue:22

Janus kinases (JAK1, JAK2, JAK3, and TYK2) are involved in the signaling of multiple cytokines important in cellular function. Blockade of the JAK-STAT pathway with a small molecule has been shown to provide therapeutic immunomodulation. Having identified JAK1 as a possible new target for arthritis at Galapagos, the compound library was screened against JAK1, resulting in the identification of a triazolopyridine-based series of inhibitors represented by 3. Optimization within this chemical series led to identification of GLPG0634 (65, filgotinib), a selective JAK1 inhibitor currently in phase 2B development for RA and phase 2A development for Crohn's disease (CD).

Topics: Adenosine Triphosphate; Animals; Arthritis; Chemistry, Pharmaceutical; Collagen; Crohn Disease; Crystallography, X-Ray; Cytokines; Dimerization; Disease Models, Animal; Drug Design; Drug Evaluation, Preclinical; Humans; Inhibitory Concentration 50; Janus Kinase 1; Kinetics; Phosphorylation; Protein Kinase Inhibitors; Pyridines; Rats; Recombinant Proteins; Structure-Activity Relationship; Triazoles

2014