Inhibitors of JAK2 and JAK3: an update on the patent literature 2010 – 2012

Randomized Phase 2b Trial of Tofacitinib (CP-690,550) in De Novo Kidney Transplant Patients: Efficacy, Renal Function and Safety at 1 Year

(2012) F. Vincenti et al.   AMERICAN JOURNAL OF TRANSPLANTATION

Low dose CP-690,550 (tofacitinib), a pan-JAK inhibitor, accelerates the onset of experimental autoimmune encephalomyelitis by potentiating Th17 differentiation

(2012) Hideyuki Yoshida et al.   BIOCHEMICAL AND BIOPHYSICAL RESEARCH COMMUNICATIONS

Efficacy and safety of tofacitinib, an oral Janus kinase inhibitor, in the treatment of psoriasis: a Phase 2b randomized placebo-controlled dose-ranging study

(2012) K.A. Papp et al.   BRITISH JOURNAL OF DERMATOLOGY

Selective JAK1 inhibitor and selective Tyk2 inhibitor patents

(2012) Peter Norman   EXPERT OPINION ON THERAPEUTIC PATENTS

Biology and significance of the JAK/STAT signalling pathways

(2012) Hiu Kiu et al.   GROWTH FACTORS

The JAK-STAT Pathway at Twenty

(2012) George R. Stark et al.   IMMUNITY

Phase I Study of a Novel Oral Janus Kinase 2 Inhibitor, SB1518, in Patients With Relapsed Lymphoma: Evidence of Clinical and Biologic Activity in Multiple Lymphoma Subtypes

(2012) Anas Younes et al.   JOURNAL OF CLINICAL ONCOLOGY

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

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

Risk of Tuberculosis Reactivation With Tofacitinib (CP-690550)

(2012) Mamoudou Maiga et al.   JOURNAL OF INFECTIOUS DISEASES

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

Discovery of Potent and Selective Pyrazolopyrimidine Janus Kinase 2 Inhibitors

(2012) Emily J. Hanan et al.   JOURNAL OF MEDICINAL CHEMISTRY

A Selective, Orally Bioavailable 1,2,4-Triazolo[1,5-a]pyridine-Based Inhibitor of Janus Kinase 2 for Use in Anticancer Therapy: Discovery of CEP-33779

(2012) Benjamin J. Dugan et al.   JOURNAL OF MEDICINAL CHEMISTRY

Therapeutic Efficacy of CEP-33779, a Novel Selective JAK2 Inhibitor, in a Mouse Model of Colitis-Induced Colorectal Cancer

(2012) M. M. Seavey et al.   MOLECULAR CANCER THERAPEUTICS

Heterodimeric JAK–STAT activation as a mechanism of persistence to JAK2 inhibitor therapy

(2012) Priya Koppikar et al.   NATURE

Tofacitinib safe and effective in renal transplant recipients

(2012) Helene Myrvang   Nature Reviews Nephrology

Phase III trial results for tofacitinib bring new oral DMARD therapy a step closer for patients with rheumatoid arthritis

(2012) Emma Leah   Nature Reviews Rheumatology

A Double-Blind, Placebo-Controlled Trial of Ruxolitinib for Myelofibrosis

(2012) Srdan Verstovsek et al.   NEW ENGLAND JOURNAL OF MEDICINE

JAK Inhibition with Ruxolitinib versus Best Available Therapy for Myelofibrosis

(2012) Claire Harrison et al.   NEW ENGLAND JOURNAL OF MEDICINE

Tofacitinib, an Oral Janus Kinase Inhibitor, in Active Ulcerative Colitis

(2012) William J. Sandborn et al.   NEW ENGLAND JOURNAL OF MEDICINE

Tofacitinib (CP-690,550), a Janus Kinase Inhibitor for Dry Eye Disease

(2012) Shiao Hui (Melissa) Liew et al.   OPHTHALMOLOGY

TYK2 Kinase Activity Is Required for Functional Type I Interferon Responses In Vivo

(2012) Michaela Prchal-Murphy et al.   PLoS One

Random Mutagenesis Reveals Residues of JAK2 Critical in Evading Inhibition by a Tyrosine Kinase Inhibitor

(2012) Michael R. Marit et al.   PLoS One

The oral HDAC inhibitor pracinostat (SB939) is efficacious and synergistic with the JAK2 inhibitor pacritinib (SB1518) in preclinical models of AML

(2012) V Novotny-Diermayr et al.   Blood Cancer Journal

Modulation of Activation-Loop Phosphorylation by JAK Inhibitors Is Binding Mode Dependent

(2012) Rita Andraos et al.   Cancer Discovery

2,7-Pyrrolo[2,1-f][1,2,4]triazines as JAK2 inhibitors: Modification of target structure to minimize reactive metabolite formation

(2011) Linda R. Weinberg et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Optimization of a novel kinase inhibitor scaffold for the dual inhibition of JAK2 and FAK kinases

(2011) Craig A. Zificsak et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Results from a randomized trial of salvage chemotherapy followed by lestaurtinib for patients with FLT3 mutant AML in first relapse

(2011) M. Levis et al.   BLOOD

Inhibitory effects of the JAK inhibitor CP690,550 on human CD4+ T lymphocyte cytokine production

(2011) Kiyoshi Migita et al.   BMC IMMUNOLOGY

Phase I trial of lestaurtinib for children with refractory neuroblastoma: a new approaches to neuroblastoma therapy consortium study

(2011) Jane E. Minturn et al.   CANCER CHEMOTHERAPY AND PHARMACOLOGY

Antiangiogenic and Antimetastatic Activity of JAK Inhibitor AZD1480

(2011) H. Xin et al.   CANCER RESEARCH

BCR-ABL1—Negative Myeloproliferative Neoplasms: A Review of Molecular Biology, Diagnosis, and Treatment

(2011) Erik Vakil et al.   Clinical Lymphoma Myeloma & Leukemia

The Use of Structural Biology in Janus Kinase Targeted Drug Discovery

(2011) Nilda L. Alicea-Velazquez et al.   CURRENT DRUG TARGETS

Tyk2 deficiency protects joints against destruction in anti-type II collagen antibody-induced arthritis in mice

(2011) M. Ishizaki et al.   INTERNATIONAL IMMUNOLOGY

Safety and Efficacy of TG101348, a Selective JAK2 Inhibitor, in Myelofibrosis

(2011) Animesh Pardanani et al.   JOURNAL OF CLINICAL ONCOLOGY

Involvement of Tyrosine Kinase-2 in Both the IL-12/Th1 and IL-23/Th17 Axes In Vivo

(2011) M. Ishizaki et al.   JOURNAL OF IMMUNOLOGY

Strategies to Mitigate the Bioactivation of 2-Anilino-7-Aryl-Pyrrolo[2,1-f][1,2,4]triazines: Identification of Orally Bioavailable, Efficacious ALK Inhibitors

(2011) Eugen F. Mesaros et al.   JOURNAL OF MEDICINAL CHEMISTRY

2,7-Disubstituted-pyrrolo[2,1-f][1,2,4]triazines: New Variant of an Old Template and Application to the Discovery of Anaplastic Lymphoma Kinase (ALK) Inhibitors with in Vivo Antitumor Activity

(2011) Gregory R. Ott et al.   JOURNAL OF MEDICINAL CHEMISTRY

Discovery of Kinase Spectrum Selective Macrocycle (16E)-14-Methyl-20-oxa-5,7,14,26-tetraazatetracyclo[19.3.1.1(2,6).1(8,12)]heptacosa-1(25),2(26),3,5,8(27),9,11,16,21,23-decaene (SB1317/TG02), a Potent Inhibitor of Cyclin Dependent Kinases (CDKs), Janus Kinase 2 (JAK2), and Fms-like Tyrosine Kinase-3 (FLT3) for the Treatment of Cancer

(2011) Anthony D. William et al.   JOURNAL OF MEDICINAL CHEMISTRY

Discovery of the Macrocycle 11-(2-Pyrrolidin-1-yl-ethoxy)-14,19-dioxa-5,7,26-triaza-tetracyclo[19.3.1.1(2,6).1(8,12)]heptacosa-1(25),2(26),3,5,8,10,12(27),16,21,23-decaene (SB1518), a Potent Janus Kinase 2/Fms-Like Tyrosine Kinase-3 (JAK2/FLT3) Inhibitor for the Treatment of Myelofibrosis and Lymphoma

(2011) Anthony D. William et al.   JOURNAL OF MEDICINAL CHEMISTRY

Characterization of BMS-911543, a functionally selective small-molecule inhibitor of JAK2

(2011) A V Purandare et al.   LEUKEMIA

The novel JAK inhibitor CYT387 suppresses multiple signalling pathways, prevents proliferation and induces apoptosis in phenotypically diverse myeloma cells

(2011) K A Monaghan et al.   LEUKEMIA

Kinase domain mutations confer resistance to novel inhibitors targeting JAK2V617F in myeloproliferative neoplasms

(2011) A Deshpande et al.   LEUKEMIA

Therapeutic Potential of AZD1480 for the Treatment of Human Glioblastoma

(2011) B. C. McFarland et al.   MOLECULAR CANCER THERAPEUTICS

Pfizer's JAK inhibitor sails through phase 3 in rheumatoid arthritis

(2011) Ken Garber   NATURE BIOTECHNOLOGY

Development and a Practical Synthesis of the JAK2 Inhibitor LY2784544

(2011) David Mitchell et al.   ORGANIC PROCESS RESEARCH & DEVELOPMENT

Efficacy of NS-018, a potent and selective JAK2/Src inhibitor, in primary cells and mouse models of myeloproliferative neoplasms

(2011) Y Nakaya et al.   Blood Cancer Journal

CYT387, a novel JAK2 inhibitor, induces hematologic responses and normalizes inflammatory cytokines in murine myeloproliferative neoplasms

(2010) J. W. Tyner et al.   BLOOD

Recent developments on JAK2 inhibitors: a patent review

(2010) Róbert Kiss et al.   EXPERT OPINION ON THERAPEUTIC PATENTS

Recent patents in the discovery of small molecule inhibitors of JAK3

(2010) Lawrence J Wilson   EXPERT OPINION ON THERAPEUTIC PATENTS

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

Discovery of 5-Chloro-N2-[(1S)-1-(5-fluoropyrimidin-2-yl)ethyl]-N4-(5-methyl-1H-pyrazol-3-yl)pyrimidine-2,4-diamine (AZD1480) as a Novel Inhibitor of the Jak/Stat Pathway

(2010) Stephanos Ioannidis et al.   JOURNAL OF MEDICINAL CHEMISTRY

Phase 2 study of CEP-701, an orally available JAK2 inhibitor, in patients with primary or post-polycythemia vera/essential thrombocythemia myelofibrosis

(2009) F. P. S. Santos et al.   BLOOD

The JAK2 Inhibitor AZD1480 Potently Blocks Stat3 Signaling and Oncogenesis in Solid Tumors

(2009) Michael Hedvat et al.   CANCER CELL

Enantioselective Synthesis of Janus Kinase Inhibitor INCB018424 via an Organocatalytic Aza-Michael Reaction

(2009) Qiyan Lin et al.   ORGANIC LETTERS

TG101348, a JAK2-selective antagonist, inhibits primary hematopoietic cells derived from myeloproliferative disorder patients with JAK2V617F, MPLW515K or JAK2 exon 12 mutations as well as mutation negative patients

(2008) T L Lasho et al.   LEUKEMIA

SOCS regulation of the JAK/STAT signalling pathway

(2008) Ben A. Croker et al.   SEMINARS IN CELL & DEVELOPMENTAL BIOLOGY