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

References

• Vakil E, Tefferi A. BCR-ABL1-negative myeloproliferative neoplasms: a review of molecular biology, diagnosis, and treatment. Clin Lymphoma Myeloma Leuk. 2011;11(S1):S37–S45.
   PubMedGoogle Scholar
• Kiu H, Nicholson SE. Biology and significance of the JAK/STAT signalling pathways. Growth Factors. 2012;30:88–106.
   PubMed Web of Science ®Google Scholar
• Schwartz DM, Bonelli M, Gadina M, et al. Type I/II cytokines, JAKs, and new strategies for treating autoimmune diseases. Nat Rev Rheumatol. 2016;12:25–36.
   PubMed Web of Science ®Google Scholar
• Borden EC, Sen GC, Uze G, et al. Interferons at age 50: past, current and future impact on biomedicine. Nat Rev Drug Discov. 2007;6:975–990.
   PubMed Web of Science ®Google Scholar
• O’Shea JJ, Schwartz DM, Villarino AV, et al. The JAK-STAT pathway: impact on human disease and therapeutic intervention. Annu Rev Med. 2015;66:311–328.
   PubMed Web of Science ®Google Scholar
• Clark JD, Flanagan ME, Telliez JB. Discovery and development of Janus kinase (JAK) inhibitors for inflammatory diseases. J Med Chem. 2014;57:5023–5038.
   PubMed Web of Science ®Google Scholar
• Tan FH, Putoczki TL, Stylli SS, et al. The role of STAT3 signaling in mediating tumour resistance to cancer therapy. Curr Drug Targets. 2014;15:1341–1353.
   PubMed Web of Science ®Google Scholar
• Sansone P, Bromberg J. Targeting the interleukin-6/Jak/Stat pathway in human malignancies. J Clin Oncol. 2012;30:1005–1014.
   PubMed Web of Science ®Google Scholar
• Haura EB, Zheng Z, Song L, et al. Activated epidermal growth factor receptor – Stat-3 signaling promotes tumor survival in vivo in non-small cell lung cancer. Clin Cancer Res. 2005;11:8288–8294.
   PubMed Web of Science ®Google Scholar
• Lam LT, Wright G, Davis RE. Cooperative signaling through the signal transducer and activator of transcription 3 and nuclear factor-κB pathways in subtypes of diffuse large B-cell lymphoma. Blood. 2008;111:3701–3713.
   PubMed Web of Science ®Google Scholar
• Song JI, Grandis JR. STAT signaling in head and neck cancer. Oncogene. 2000;19:2489–2495.
   PubMed Web of Science ®Google Scholar
• Thomas SJ, Snowden JA, Zeidler MP, et al. The role of JAK/STAT signalling in the pathogenesis, prognosis and treatment of solid tumours. Br J Cancer. 2015;113:365–371.
   PubMed Web of Science ®Google Scholar
• Yin Z, Zhang Y, Li Y, et al. Prognostic significance of STAT3 expression and its correlation with chemoresistance of non-small cell lung cancer cells. Acta Histochem. 2012;114:151–158.
   PubMed Web of Science ®Google Scholar
• Gao SP, Mark KG, Leslie K, et al. Mutations in the EGFR kinase domain mediate STAT3 activation via IL-6 production in human lung adenocarcinomas. J Clin Invest. 2007;117:3846–3856.
   PubMed Web of Science ®Google Scholar
• Lee H-J, Zhuang G, Cao Y, et al. Drug resistance via feedback activation of Stat3 in oncogene-addicted cancer cells. Cancer Cell. 2014;26:207–221.
   PubMed Web of Science ®Google Scholar
• O’Shea JJ, Holland SM, Staudt LM. JAKs and STATs in immunity, immunodeficiency, and cancer. N Engl J Med. 2013;368:161–170.
   PubMed Web of Science ®Google Scholar
• Ostojic A, Vrhovac R, Verstovsek S. Ruxolitinib for the treatment of myelofibrosis: its clinical potential. Ther Clin Risk Manag. 2012;8:95–103.
   PubMed Web of Science ®Google Scholar
• Yu H, Kortylewski M, Pardoll D. Crosstalk between cancer and immune cells: role of STAT3 in the tumour microenvironment. Nat Rev Immunol. 2007;7:41–51.
   PubMed Web of Science ®Google Scholar
• Kortylewski M, Yu H. Role of Stat3 in suppressing anti-tumour immunity. Curr Op Immunol. 2008;20:228–233.
   PubMed Web of Science ®Google Scholar
• Avalle L, Pensa S, Regis G, et al. STAT1 and STAT3 in tumourigenesis: a matter of balance. Jakstat. 2012;1:65–72.
   PubMedGoogle Scholar
• Pensa S, Regis G, Boselli D, et al. STAT3 and STAT3 in tumourigenesis: two sides of the same coin? JAK-STAT pathway in disease. Landes Biosci. 2009.
   Google Scholar
• Kortylewski M, Kujawski M, Wang T, et al. Inhibiting Stat3 signaling in the hematopoietic system elicits multicomponent antitumour immunity. Nat Med. 2005;11:1314–1321.
   PubMed Web of Science ®Google Scholar
• Niu G, Wright KL, Huang M, et al. Constitutive Stat3 activity up-regulates VEGF expression and tumour angiogenesis. Oncogene. 2002;21:2000–2008.
   PubMed Web of Science ®Google Scholar
• Integrity database: http://thomsonreuters.com/en/products-services/pharma-life-sciences/pharma-competitive-intelligence/cortellis-competitive-intelligence.html. cited 2015 Sep &Jan 2016.
   Google Scholar
• SciFinder: http://www.cas.org/products/scifinder. cited 2015 Sep and 2016 Jan.
   Google Scholar
• Kettle JG, Åstrand A, Catley M, et al. Inhibitors of JAK-family kinases: an update on the patent literature 2013-2015, part 2. Expert Opin Ther Pat. 2016. doi:10.1080/13543776.2017.1252754.
   Google Scholar
• Dymock BW, See CS. Inhibitors of JAK2 and JAK3: an update on the patent literature 2010 – 2012. Expert Opin Ther Patents. 2013;23:449–501.
   PubMed Web of Science ®Google Scholar
• AbbVie Inc. JAK1selective inhibitor and uses thereof. WO2015061665. 2015
   Google Scholar
• Abbott Laboratories. Novel tricyclic compounds. WO2011068881. 2011
   Google Scholar
• AbbVie Inc. Tricyclic compounds useful as protein kinase inhibitors. WO2013043826. 2013
   Google Scholar
• Almirall Prodesfarma SA Pyridin-2(1H)-one derivatives as JAK inhibitors. WO2013017461. 2013
   Google Scholar
• Ioannidis S, Lamb ML, Wang T, et al. 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. J Med Chem. 2011;54:262–276.
   PubMed Web of Science ®Google Scholar
• Almirall Prodesfarma SA Pyrazolopyrimidin-2-yl derivatives as JAK inhibitors. WO2015086693. 2015
   Google Scholar
• Almirall Prodesfarma SA Imidazolopyrimidin-2-yl derivatives as JAK inhibitors. WO2015091531. 2015
   Google Scholar
• Array BioPharma Inc. 5,7-Substituted-imidazo[1,2-c]pyrimidines. WO2013055645. 2013
   Google Scholar
• Arrien Pharmaceuticals LLC. 3,5-(Un)substituted-1H-pyrrolo[2,3-b]pyridine, 1H-pyrazolo[3,4-b]pyridine and 5H-pyrrolo[2-,3-b]pyrazine dual ITK and JAK3 kinase inhibitors. WO2014172513. 2014
   Google Scholar
• Aurigene Discovery Technologies Ltd. Pyrimidine-2,4-diamine derivatives as kinase inhibitors. WO2014091265. 2014
   Google Scholar
• Novartis. Pyrimidine derivatives. WO2006021454. 2006
   Google Scholar
• BioCryst Pharmaceuticals Inc. Heterocyclic compounds as Janus kinase inhibitors. WO2013033093; 2013
   Google Scholar
• Vertex Pharma. Tricyclic heteroaryl compounds useful as inhibitors of Janus kinase. WO2008079521. 2008
   Google Scholar
• Wang T, Duffy JP, Wang J, et al. Janus kinase 2 inhibitors synthesis and characterization of a novel polycyclic azaindole. J Med Chem. 2009;52:7938–7941.
   PubMed Web of Science ®Google Scholar
• Hunt JT, Mitt T, Borzilleri R, et al. Discovery of the pyrrolo[2,1-f][1,2,4]triazine nucleus as a new kinase inhibitor template. J Med Chem. 2004;47:4054–4059.
   PubMed Web of Science ®Google Scholar
• Jin B. Novel compositions, uses and methods for their preparation. WO2015057695. 2015
   Google Scholar
• Bristol-Myers Squibb Co. Imidazopyridazine JAK-3 inhibitors and their use for the treatment of inflammatory and autoimmune diseases. WO2014039595. 2014
   Google Scholar
• Zydus Cadila Healthcare Ltd. N-Cyanomethylamides as inhibitors of Janus kinase. WO2015019365. 2015
   Google Scholar
• Zydus Cadila Healthcare Ltd. Heterocyclic compounds. WO2013054351. 2013
   Google Scholar
• Calitor Sciences Llc. Sunshine Lake Pharma Co Ltd. Substituted heteroaryl compounds and methods of use. WO2015094803. 2015
   Google Scholar
• Calitor Sciences Llc. Sunshine Lake Pharma Co Ltd. Substituted heteroaryl compounds and methods of use. WO2015148867. 2015
   Google Scholar
• Calitor Sciences Llc. Sunshine Lake Pharma Co Ltd. Substituted heteroaryl compounds and methods of use. WO2015073267. 2015
   Google Scholar
• Genentech Inc. Pyrazolopyrimidine JAK inhibitor compounds and methods. WO2011003065. 2011
   Google Scholar
• Vertex Pharmaceuticals Inc. Compounds useful as inhibitors of ATR kinase. WO2014143241. 2014
   Google Scholar
• Infinity Pharmaceuticals Inc. Heterocyclic compounds and uses thereof. WO2015051244. 2015
   Google Scholar
• Cellzome. Pyrazolo[4,3-c]pyridine derivatives as JAK inhibitors. WO2013017479. 2013
   Google Scholar
• Cellzome. Pyrazolo[4,3-c]pyridine derivatives as JAK inhibitors. WO2013017480. 2013
   Google Scholar
• Cellzome. Heterocyclyl pyrazolopyrimidine analogues as jak inhibitors. WO2011048082. 2011
   Google Scholar
• Cellzome. Heterocyclyl pyrazolopyrimidine analogues as selective JAK inhibitors. WO2012022681. 2012
   Google Scholar
• Cellzome. Pyrazolo[4,3-c]pyridine derivatives as kinase inhibitors. WO2013041605. 2013
   Google Scholar
• Cellzome. Heterocyclyl pyrimidine analogues as JAK inhibitors. WO2013014162; 2013
   Google Scholar
• Cellzome. Pyrimidine-2,4-diamine derivatives as kinase inhibitors. WO2013092854. 2013
   Google Scholar
• Cellzome. Heterocyclyl pyrimidine analogs as TYK2 inhibitors. WO2013174895. 2013
   Google Scholar
• Celon Pharma SP. Imidazo[1,2-b]pyridazin-6-amine derivatives as kinase JAK-2 inhibitors. WO2014020531. 2014
   Google Scholar
• Celon Pharma SP. Pyrazolo[1,5-a]pyrimidine derivatives as kinase JAK-2 inhibitors. WO2015118434. 2015
   Google Scholar
• Su Q, Ioannidis S, Chuaqui C, et al. Discovery of 1-methyl-1h-imidazole derivatives as potent jak2 inhibitors. J Med Chem. 2014;57:144–158.
   PubMed Web of Science ®Google Scholar
• AstraZeneca. Pyrazolyl-amino-substituted pyrimidines and their use for the treatment of cancer. WO2008132502. 2008
   Google Scholar
• AstraZeneca. 5-aminopyrazol-3-yl-3h-imidazo [4,5-b] pyridine derivatives and their use for the treatment of cancer. WO2008129255. 2008
   Google Scholar
• Cephalon Inc. Imidazo[4,5-b]pyridine derivatives as Alk and JAK modulators for the treatment of proliferative disorders. WO2013116291. 2013
   Google Scholar
• Cephalon Inc. Treatment of multiple sclerosis with a 1,2,4-triazolo [1,5a] pyridine derivative. WO2015089153. 2015
   Google Scholar
• Cephalon Inc. Preparation and uses of 1,2,4-triazolo[1,5a]pyridine derivatives. WO2010141796. 2010
   Google Scholar
• Dugan BJ, Gingrich DE, Mesaros EF, et al. 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. J Med Chem. 2012;55:5243–5254.
   PubMed Web of Science ®Google Scholar
• CoNCERT Pharmaceuticals Inc. Deuterated pacritinib. WO2014159511. 2014
   Google Scholar
• CoNCERT Pharmaceuticals Inc. Deuterated baricitinib. WO2014028756. 2014
   Google Scholar
• CoNCERT Pharmaceuticals Inc. Deuterated derivatives of ruxolitinib. WO2013188783; 2013
   Google Scholar
• Dana-Farber Cancer Institute, Inc. Janus kinase inhibitors and uses thereof. WO2015164614. 2015
   Google Scholar
• Tan L, Akahane K, McNally R, et al. Development of selective covalent Janus kinase 3 inhibitors. J Med Chem. 2015;58:6589−6606.
   PubMed Web of Science ®Google Scholar
• Dana-Farber Cancer Institute, Inc. Hydrophobically tagged Janus kinase inhibitors and uses thereof. WO2015164604. 2015
   Google Scholar
• Xie T, Lim SM, Westover KD, et al. Pharmacological targeting of the pseudokinase ​Her3. Nat Chem Biol. 2014;10:1006–1012.
   PubMed Web of Science ®Google Scholar
• Eli Lilly & Co. Lilly Industries Ltd. Inhibitor of JAK1 and JAK2. WO2013188184; 2013
   Google Scholar
• Endo Health Solutions Inc. Endo Pharmaceuticals Solutions Inc. Individual. Pyrimido-pyridazinone compounds and use thereof. WO2013028818. 2013
   Google Scholar
• EP Pharma Inc. Compositions and methods related to inhibitors of JAK kinase. WO2013148638. 2013
   Google Scholar
• Stepkowski SM, Kao J, Wang M-E, et al. The Mannich base NC1153 promotes long-term allograft survival and spares the recipient from multiple toxicities. J Immunol. 2005;175:4236–4246.
   PubMed Web of Science ®Google Scholar
• Galapagos NV Individual. Imidazo[4,5-c]pyridine derivatives useful for the treatment of degenerative and inflammatory diseases. WO2013117645. 2013
   Google Scholar
• Galapagos NV Imidazo [4,5-c] pyridine derivatives useful for the treatment of degenerative and inflammatory diseases. WO2013117649. 2013
   Google Scholar
• Galapagos NV Individual. Aminotriazolopyridine for use in the treatment of inflammation, and pharmaceutical compositions thereof. WO2013189771. 2013
   Google Scholar
• Menet CJ, Fletcher SR, Van Lommen G, et al. Triazolopyridines as selective JAK1 inhibitors: from hit identification to GLPG0634. J Med Chem. 2014;57:9323−9342.
   PubMed Web of Science ®Google Scholar
• Galapagos NV Benzimidazole derivatives and pharmaceutical compositions thereof for the treatment of inflammatory disorders. WO2015110378. 2015
   Google Scholar
• Eli Lilly & Co. Hanmi Pharmaceutical Co Ltd. Triazolopyridine derivatives as a tyrosine kinase inhibitor. WO2013118986. 2013
   Google Scholar
• Pan Z, Scheerens H, Li SJ, et al. Discovery of selective irreversible inhibitors for Bruton’s tyrosine kinase. ChemMedChem. 2007;2:58–61.
   PubMed Web of Science ®Google Scholar
• Eli Lilly & Co. Hanmi Pharmaceutical Co Ltd. Novel imidazopyridine derivatives as a tyrosine kinase inhibitor. WO2013100631. 2013
   Google Scholar
• Beijing Hanmi Pharmaceutical Co Ltd. Compound inhibiting kinase activities of BTK and/or JAK3. WO2015039612. 2015
   Google Scholar
• Beijing Hanmi Pharmaceutical Co Ltd. Compound inhibiting kinase activities of BTK and/or JAK3. WO2015039613. 2015
   Google Scholar
• Incyte Corp. Piperidinylcyclobutyl substituted pyrrolopyridine and pyrrolopyrimidine derivatives as JAK inhibitors. WO2013173720. 2013
   Google Scholar
• Incyte Corp Individual. Cyclohexyl azetidine derivatives as JAK inhibitors. WO2013026025. 2013
   Google Scholar
• Li J, Caulder E, Favata M, et al. Blockade of the IL-6/JAK/STAT3 signaling pathway inhibits pancreatic tumor cell growth in 3D spheroid cultures and in xenograft models. 106th Annu Meet Am Assoc Cancer Res (AACR) 2015(Apr 18-22, Philadelphia), Abst 779
   Google Scholar
• Incyte Corp. Bipyrazole derivatives as JAK inhibitors. WO2014186706. 2014
   Google Scholar
• Incyte Corp. Tricyclic fused thiophene derivatives as JAK inhibitors. WO2014071031. 2014
   Google Scholar
• Incyte Corp. Processes of preparing a JAK1 inhibitor and new forms thereto. WO2015168246. 2015
   Google Scholar