JAK3 inhibitors for the treatment of inflammatory and autoimmune diseases: a patent review (2016–present)

A phase 2a randomized, placebo-controlled study to evaluate the efficacy and safety of the oral Janus kinase inhibitors ritlecitinib and brepocitinib in alopecia areata: 24-week results

(2021) Brett King et al.   JOURNAL OF THE AMERICAN ACADEMY OF DERMATOLOGY

Selective inhibition of JAK3 signaling is sufficient to reverse alopecia areata

(2021) Zhenpeng Dai et al.   JCI Insight

Phase I study in healthy participants to evaluate safety, tolerability, and pharmacokinetics of inhaled nezulcitinib, a potential treatment for COVID‐19

(2021) Nathan D. Pfeifer et al.   CTS-Clinical and Translational Science

A phase 2 multiple ascending dose study of the inhaled pan-JAK inhibitor nezulcitinib (TD–0903) in severe COVID-19

(2021) Dave Singh et al.   EUROPEAN RESPIRATORY JOURNAL

Novel 1H-pyrazolo[3,4-d]pyrimidin-6-amino derivatives as potent selective Janus kinase 3 (JAK3) inhibitors. Evaluation of their improved effect for the treatment of rheumatoid arthritis

(2020) Yuan Yin et al.   BIOORGANIC CHEMISTRY

Delgocitinib: First Approval

(2020) Sohita Dhillon   DRUGS

Janus kinases (JAKs): The efficient therapeutic targets for autoimmune diseases and myeloproliferative disorders

(2020) Pengfei Xu et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Ruxolitinib for Glucocorticoid-Refractory Acute Graft-versus-Host Disease

(2020) Robert Zeiser et al.   NEW ENGLAND JOURNAL OF MEDICINE

Efficacy and Safety of PF‐06651600 (Ritlecitinib), a Novel JAK3/TEC Inhibitor in Patients with Moderate to Severe Rheumatoid Arthritis and an Inadequate Response to Methotrexate

(2020) Michael F. Robinson et al.   Arthritis & Rheumatology

Fedratinib, a newly approved treatment for patients with myeloproliferative neoplasm-associated myelofibrosis

(2020) Moshe Talpaz et al.   LEUKEMIA

Trial of Upadacitinib or Abatacept in Rheumatoid Arthritis

(2020) Andrea Rubbert-Roth et al.   NEW ENGLAND JOURNAL OF MEDICINE

Filgotinib: First Approval

(2020) Sohita Dhillon et al.   DRUGS

Baricitinib plus Remdesivir for Hospitalized Adults with Covid-19

(2020) Andre C. Kalil et al.   NEW ENGLAND JOURNAL OF MEDICINE

Selective Tyk2 inhibitors as potential therapeutic agents: a patent review (2015-2018)

(2019) Xingrui He et al.   EXPERT OPINION ON THERAPEUTIC PATENTS

PF-06651600, a dual JAK3/TEC family kinase inhibitor

(2019) Hua Xu et al.   ACS Chemical Biology

Peficitinib: First Global Approval

(2019) Anthony Markham et al.   DRUGS

Current Status in the Discovery of Covalent Janus Kinase 3 (JAK3) inhibitors

(2019) Jun Dai et al.   MINI-REVIEWS IN MEDICINAL CHEMISTRY

Therapeutic treatment of a novel selective JAK3/JAK1/TBK1 inhibitor, CS12192, in rat and mouse models of rheumatoid arthritis

(2019) Song Shan et al.   INTERNATIONAL IMMUNOPHARMACOLOGY

Efficacy and safety of upadacitinib in patients with active ankylosing spondylitis (SELECT-AXIS 1): a multicentre, randomised, double-blind, placebo-controlled, phase 2/3 trial

(2019) Désirée van der Heijde et al.   LANCET

Design of a Janus Kinase 3 (JAK3) Specific Inhibitor 1-((2S,5R)-5-((7H-Pyrrolo[2,3-d]pyrimidin-4-yl)amino)-2-methylpiperidin-1-yl)prop-2-en-1-one (PF-06651600) Allowing for the Interrogation of JAK3 Signaling in Humans

(2017) Atli Thorarensen et al.   JOURNAL OF MEDICINAL CHEMISTRY

Design and Synthesis of a Pan-Janus Kinase Inhibitor Clinical Candidate (PF-06263276) Suitable for Inhaled and Topical Delivery for the Treatment of Inflammatory Diseases of the Lungs and Skin

(2017) Peter Jones et al.   JOURNAL OF MEDICINAL CHEMISTRY

Evaluation of JAK3 Biology in Autoimmune Disease Using a Highly Selective, Irreversible JAK3 Inhibitor

(2017) Fiona Elwood et al.   JOURNAL OF PHARMACOLOGY AND EXPERIMENTAL THERAPEUTICS

The emerging safety profile of JAK inhibitors in rheumatic disease

(2017) Kevin L. Winthrop   Nature Reviews Rheumatology

Tofacitinib as Induction and Maintenance Therapy for Ulcerative Colitis

(2017) William J. Sandborn et al.   NEW ENGLAND JOURNAL OF MEDICINE

Discovery of a JAK3-Selective Inhibitor: Functional Differentiation of JAK3-Selective Inhibition over pan-JAK or JAK1-Selective Inhibition

(2016) Jean-Baptiste Telliez et al.   ACS Chemical Biology

Inhibitors of JAK-family kinases: an update on the patent literature 2013-2015, part 1

(2016) Jason G. Kettle et al.   EXPERT OPINION ON THERAPEUTIC PATENTS

Inhibitors of JAK-family kinases: an update on the patent literature 2013-2015, part 2

(2016) Jason G. Kettle et al.   EXPERT OPINION ON THERAPEUTIC PATENTS

Essential biphasic role for JAK3 catalytic activity in IL-2 receptor signaling

(2016) Geoffrey A Smith et al.   Nature Chemical Biology

Janus kinase (JAK) inhibitors in the treatment of inflammatory and neoplastic diseases

(2016) Robert Roskoski   PHARMACOLOGICAL RESEARCH

JAK3 as an Emerging Target for Topical Treatment of Inflammatory Skin Diseases

(2016) Ana Karina Alves de Medeiros et al.   PLoS One

A Randomized, Double-Blind, Placebo-Controlled, Twelve-Week, Dose-Ranging Study of Decernotinib, an Oral Selective JAK-3 Inhibitor, as Monotherapy in Patients With Active Rheumatoid Arthritis

(2015) Roy M. Fleischmann et al.   Arthritis & Rheumatology

VX-509 (Decernotinib), an Oral Selective JAK-3 Inhibitor, in Combination With Methotrexate in Patients With Rheumatoid Arthritis

(2015) Mark C. Genovese et al.   Arthritis & Rheumatology

Tricyclic Covalent Inhibitors Selectively Target Jak3 through an Active Site Thiol

(2015) Eric R. Goedken et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Discovery and Development of Janus Kinase (JAK) Inhibitors for Inflammatory Diseases

(2014) James D. Clark et al.   JOURNAL OF MEDICINAL CHEMISTRY

Tofacitinib versus Methotrexate in Rheumatoid Arthritis

(2014) Eun Bong Lee et al.   NEW ENGLAND JOURNAL OF MEDICINE

Developing Irreversible Inhibitors of the Protein Kinase Cysteinome

(2013) Qingsong Liu et al.   CHEMISTRY & BIOLOGY

Inborn Errors of Human JAKs and STATs

(2012) Jean-Laurent Casanova et al.   IMMUNITY

Ruxolitinib

(2012) Ruben A. Mesa et al.   NATURE REVIEWS DRUG DISCOVERY

Clinical significance of V617F mutation of the JAK2 gene in patients with chronic myeloproliferative disorders

(2009) Ana L. Basquiera et al.   Hematology