Inhibitors of JAK2 and JAK3: an update on the patent literature 2010 - 2012. (Q38077992)

28 August 2017

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title

Inhibitors of JAK2 and JAK3: an update on the patent literature 2010 - 2012. (English)

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28 August 2017

Brian W Dymock

1

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28 August 2017

Cheng Shang See

series ordinal

2

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28 August 2017

language of work or name

English

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publication date

1 February 2013

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Expert Opinion on Therapeutic Patents

28 August 2017

published in

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28 August 2017

volume

23

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28 August 2017

issue

4

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28 August 2017

page(s)

449-501

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BCR-ABL1--negative myeloproliferative neoplasms: a review of molecular biology, diagnosis, and treatment

28 August 2017

cites work

1 reference

https://api.crossref.org/works/10.1517%2F13543776.2013.765862

Biology and significance of the JAK/STAT signalling pathways

21 January 2018

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A unique clonal JAK2 mutation leading to constitutive signalling causes polycythaemia vera

21 January 2018

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A gain-of-function mutation of JAK2 in myeloproliferative disorders

21 January 2018

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Activating mutation in the tyrosine kinase JAK2 in polycythemia vera, essential thrombocythemia, and myeloid metaplasia with myelofibrosis

21 January 2018

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https://api.crossref.org/works/10.1517%2F13543776.2013.765862

A double-blind, placebo-controlled trial of ruxolitinib for myelofibrosis

21 January 2018

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https://api.crossref.org/works/10.1517%2F13543776.2013.765862

JAK inhibition with ruxolitinib versus best available therapy for myelofibrosis

21 January 2018

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https://api.crossref.org/works/10.1517%2F13543776.2013.765862

The JAK-STAT pathway at twenty

21 January 2018

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https://api.crossref.org/works/10.1517%2F13543776.2013.765862

SOCS regulation of the JAK/STAT signalling pathway

21 January 2018

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https://api.crossref.org/works/10.1517%2F13543776.2013.765862

Disruption of the Jak1 gene demonstrates obligatory and nonredundant roles of the Jaks in cytokine-induced biologic responses

21 January 2018

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https://api.crossref.org/works/10.1517%2F13543776.2013.765862

Jak2 deficiency defines an essential developmental checkpoint in definitive hematopoiesis

21 January 2018

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https://api.crossref.org/works/10.1517%2F13543776.2013.765862

Jak2 is essential for signaling through a variety of cytokine receptors

21 January 2018

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https://api.crossref.org/works/10.1517%2F13543776.2013.765862

Janus kinase 2: a critical target in chronic myelogenous leukemia

21 January 2018

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https://api.crossref.org/works/10.1517%2F13543776.2013.765862

Mutations of Jak-3 gene in patients with autosomal severe combined immune deficiency (SCID)

21 January 2018

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https://api.crossref.org/works/10.1517%2F13543776.2013.765862

Mutation of Jak3 in a patient with SCID: essential role of Jak3 in lymphoid development.

21 January 2018

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https://api.crossref.org/works/10.1517%2F13543776.2013.765862

Janus kinase 3 (Jak3) is essential for common cytokine receptor gamma chain (gamma(c))-dependent signaling: comparative analysis of gamma(c), Jak3, and gamma(c) and Jak3 double-deficient mice

21 January 2018

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https://api.crossref.org/works/10.1517%2F13543776.2013.765862

A natural mutation in the Tyk2 pseudokinase domain underlies altered susceptibility of B10.Q/J mice to infection and autoimmunity

21 January 2018

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https://api.crossref.org/works/10.1517%2F13543776.2013.765862

Involvement of tyrosine kinase-2 in both the IL-12/Th1 and IL-23/Th17 axes in vivo.

21 January 2018

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https://api.crossref.org/works/10.1517%2F13543776.2013.765862

TYK2 kinase activity is required for functional type I interferon responses in vivo

21 January 2018

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https://api.crossref.org/works/10.1517%2F13543776.2013.765862

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

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F13543776.2013.765862

Selective JAK1 inhibitor and selective Tyk2 inhibitor patents

21 January 2018

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https://api.crossref.org/works/10.1517%2F13543776.2013.765862

Recent developments on JAK2 inhibitors: a patent review.

21 January 2018

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https://api.crossref.org/works/10.1517%2F13543776.2013.765862

Recent patents in the discovery of small molecule inhibitors of JAK3.

21 January 2018

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https://api.crossref.org/works/10.1517%2F13543776.2013.765862

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

21 January 2018

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https://api.crossref.org/works/10.1517%2F13543776.2013.765862

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

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F13543776.2013.765862

Therapeutic efficacy of CEP-33779, a novel selective JAK2 inhibitor, in a mouse model of colitis-induced colorectal cancer

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F13543776.2013.765862

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

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F13543776.2013.765862

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

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F13543776.2013.765862

Discovery of potent and selective pyrazolopyrimidine janus kinase 2 inhibitors

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F13543776.2013.765862

Tofacitinib (CP-690,550), a Janus kinase inhibitor for dry eye disease: results from a phase 1/2 trial

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F13543776.2013.765862

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) [...]

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F13543776.2013.765862

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-like tyrosine kinase-

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F13543776.2013.765862

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), J

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F13543776.2013.765862

TG101209, a small molecule JAK2-selective kinase inhibitor potently inhibits myeloproliferative disorder-associated JAK2V617F and MPLW515L/K mutations

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F13543776.2013.765862

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

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F13543776.2013.765862

The use of structural biology in Janus kinase targeted drug discovery

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F13543776.2013.765862

Random mutagenesis reveals residues of JAK2 critical in evading inhibition by a tyrosine kinase inhibitor

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F13543776.2013.765862

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

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F13543776.2013.765862

Cross-regulation of JAK and Src kinases

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F13543776.2013.765862

FLT3 and its Role in the Pathogenesis of Acute Myeloid Leukaemia

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F13543776.2013.765862

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

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F13543776.2013.765862

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

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F13543776.2013.765862

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

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F13543776.2013.765862

Risk of tuberculosis reactivation with tofacitinib (CP-690550).

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F13543776.2013.765862

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

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F13543776.2013.765862

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

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F13543776.2013.765862

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

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F13543776.2013.765862

Randomized phase 2b trial of tofacitinib (CP-690,550) in de novo kidney transplant patients: efficacy, renal function and safety at 1 year.

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F13543776.2013.765862

Transplantation: Tofacitinib safe and effective in renal transplant recipients

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F13543776.2013.765862

Tofacitinib, an oral Janus kinase inhibitor, in active ulcerative colitis.

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F13543776.2013.765862

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

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F13543776.2013.765862

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

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F13543776.2013.765862

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

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F13543776.2013.765862

Safety and efficacy of TG101348, a selective JAK2 inhibitor, in myelofibrosis

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F13543776.2013.765862

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

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F13543776.2013.765862

Selective inhibition of JAK1 and JAK2 is efficacious in rodent models of arthritis: preclinical characterization of INCB028050.

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F13543776.2013.765862

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

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F13543776.2013.765862

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

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F13543776.2013.765862

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

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F13543776.2013.765862

Antiangiogenic and antimetastatic activity of JAK inhibitor AZD1480.

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F13543776.2013.765862

The JAK2 inhibitor AZD1480 potently blocks Stat3 signaling and oncogenesis in solid tumors

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F13543776.2013.765862

Therapeutic potential of AZD1480 for the treatment of human glioblastoma

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F13543776.2013.765862

SB1578, a novel inhibitor of JAK2, FLT3, and c-Fms for the treatment of rheumatoid arthritis.

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F13543776.2013.765862

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

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F13543776.2013.765862

10.1517/13543776.2013.765862

21 January 2018

Identifiers

DOI

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28 August 2017

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