Selective JAK inhibitors in development for rheumatoid arthritis

THU0252 Relationship between Lymphocyte Count and Risk of Infection in Rheumatoid Arthritis Patients Treated with Tofacitinib

(2014) R. van Vollenhoven et al.   ANNALS OF THE RHEUMATIC DISEASES

LB0005 12-week results of a phase 2B dose-ranging study of LY3009104 (INCB028050), an oral JAK1/JAK2 inhibitor, in combination with traditional dmards in patients with rheumatoid arthritis

(2014) E. Keystone et al.   ANNALS OF THE RHEUMATIC DISEASES

A1.72 Baricitinib, an oral janus kinase inhibitor, in the treatment of rheumatoid arthritis: safety and efficacy in an open-label, long-term extension study1

(2014) Peter Taylor et al.   ANNALS OF THE RHEUMATIC DISEASES

Novel triazolo-pyrrolopyridines as inhibitors of Janus kinase 1

(2013) Christopher A. Hurley et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Tofacitinib: A Review of its Use in Adult Patients with Rheumatoid Arthritis

(2013) Lesley J. Scott   DRUGS

Lead identification of novel and selective TYK2 inhibitors

(2013) Jun Liang et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Tyk2 is a therapeutic target for psoriasis-like skin inflammation

(2013) M. Ishizaki et al.   INTERNATIONAL IMMUNOLOGY

Erythropoietin: multiple targets, actions, and modifying influences for biological and clinical consideration

(2013) Hal E. Broxmeyer   JOURNAL OF EXPERIMENTAL MEDICINE

A Restricted Role for TYK2 Catalytic Activity in Human Cytokine Responses Revealed by Novel TYK2-Selective Inhibitors

(2013) S. J. Sohn et al.   JOURNAL OF IMMUNOLOGY

Preclinical Characterization of GLPG0634, a Selective Inhibitor of JAK1, for the Treatment of Inflammatory Diseases

(2013) L. Van Rompaey et al.   JOURNAL OF IMMUNOLOGY

Identification of C-2 Hydroxyethyl Imidazopyrrolopyridines as Potent JAK1 Inhibitors with Favorable Physicochemical Properties and High Selectivity over JAK2

(2013) Mark Zak et al.   JOURNAL OF MEDICINAL CHEMISTRY

Inhibition of spleen tyrosine kinase in the treatment of rheumatoid arthritis

(2013) J. S. Nijjar et al.   RHEUMATOLOGY

Profiling of dihydroorotate dehydrogenase, p38 and JAK inhibitors in the rat adjuvant-induced arthritis model: a translational study

(2012) C Balagué et al.   BRITISH JOURNAL OF PHARMACOLOGY

Ruxolitinib, an oral JAK1 and JAK2 inhibitor, in myelofibrosis

(2012) Kris Vaddi et al.   EXPERT OPINION ON PHARMACOTHERAPY

The JAK-STAT Pathway at Twenty

(2012) George R. Stark et al.   IMMUNITY

Structure-based design of oxygen-linked macrocyclic kinase inhibitors: discovery of SB1518 and SB1578, potent inhibitors of Janus kinase 2 (JAK2) and Fms-like tyrosine kinase-3 (FLT3)

(2012) Anders Poulsen et al.   JOURNAL OF COMPUTER-AIDED MOLECULAR DESIGN

SB1578, a Novel Inhibitor of JAK2, FLT3, and c-Fms for the Treatment of Rheumatoid Arthritis

(2012) B. Madan et al.   JOURNAL OF IMMUNOLOGY

Discovery of the Macrocycle (9E)-15-(2-(Pyrrolidin-1-yl)ethoxy)-7,12,25-trioxa-19,21,24-triaza-tetracyclo[18.3.1.1(2,5).1(14,18)]hexacosa-1(24),2,4,9,14(26),15,17,20,22-nonaene (SB1578), a Potent Inhibitor of Janus Kinase 2/Fms-LikeTyrosine Kinase-3 (JAK2/FLT3) for the Treatment of Rheumatoid Arthritis

(2012) Anthony D. William et al.   JOURNAL OF MEDICINAL CHEMISTRY

Identification of Imidazo-Pyrrolopyridines as Novel and Potent JAK1 Inhibitors

(2012) Janusz J. Kulagowski et al.   JOURNAL OF MEDICINAL CHEMISTRY

Kinase inhibitors: a new class of antirheumatic drugs

(2012) Vasileios Kyttaris   Drug Design Development and Therapy

Specific Jak3 Downregulation in Lymphocytes Impairs γc Cytokine Signal Transduction and Alleviates Antigen-driven Inflammation In Vivo

(2012) Alicia G Gómez-Valadés et al.   Molecular Therapy-Nucleic Acids

Role of Spleen Tyrosine Kinase Inhibitors in the Management of Rheumatoid Arthritis

(2011) David L. Scott   DRUGS

New drugs beyond biologics in rheumatoid arthritis: the kinase inhibitors

(2011) M. G. Bonilla-Hernan et al.   RHEUMATOLOGY

Pacritinib (SB1518), a JAK2/FLT3 inhibitor for the treatment of acute myeloid leukemia

(2011) S Hart et al.   Blood Cancer Journal

Kinase inhibitors: a new approach to rheumatoid arthritis treatment

(2010) Stanley Cohen et al.   CURRENT OPINION IN RHEUMATOLOGY

Selective Inhibition of JAK1 and JAK2 Is Efficacious in Rodent Models of Arthritis: Preclinical Characterization of INCB028050

(2010) J. S. Fridman et al.   JOURNAL OF IMMUNOLOGY

Evaluation of the efficacy and safety of pamapimod, a p38 MAP kinase inhibitor, in a double-blind, methotrexate-controlled study of patients with active rheumatoid arthritis

(2009) Stanley B. Cohen et al.   ARTHRITIS AND RHEUMATISM

The safety and efficacy of a JAK inhibitor in patients with active rheumatoid arthritis: Results of a double-blind, placebo-controlled phase IIa trial of three dosage levels of CP-690,550 versus placebo

(2009) Joel M. Kremer et al.   ARTHRITIS AND RHEUMATISM

Selective p38α Inhibitors Clinically Evaluated for the Treatment of Chronic Inflammatory Disorders

(2009) David M. Goldstein et al.   JOURNAL OF MEDICINAL CHEMISTRY

p38MAPK: stress responses from molecular mechanisms to therapeutics

(2009) Lydia R. Coulthard et al.   TRENDS IN MOLECULAR MEDICINE

Examining the Chirality, Conformation and Selective Kinase Inhibition of 3-((3R,4R)-4-methyl-3-(methyl(7H-pyrrolo[2,3-d]pyrimidin-4-yl)amino)piperidin-1-yl)-3-oxopropanenitrile (CP-690,550)

(2008) Jian-kang Jiang et al.   JOURNAL OF MEDICINAL CHEMISTRY

A quantitative analysis of kinase inhibitor selectivity

(2008) Mazen W Karaman et al.   NATURE BIOTECHNOLOGY