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

Bibliography

• Vakil E, Tefferi A. BCR-ABL1–negative myeloproliferative neoplasms: a review of molecular biology, diagnosis, and treatment. Clin Lymphoma Myeloma Leuk 2011;11(Suppl 1):S37-45
   Google Scholar
• Kiu H, Nicholson SE. Biology and significance of the JAK/STAT signalling pathways. Growth Factors 2012;30(2):88-106
   PubMed Web of Science ®Google Scholar
• Baxter EJ, Scott LM, Campbell PJ, Acquired mutation of the tyrosine kinase JAK2 in human myeloproliferative disorders. Lancet 2005;365(9464):1054-61
   PubMed Web of Science ®Google Scholar
• James C, Ugo V, Le Couedic JP, A unique clonal JAK2 mutation leading to constitutive signalling causes polycythaemia vera. Nature 2005;434(7037):1144-8
   PubMed Web of Science ®Google Scholar
• Kralovics R, Passamonti F, Buser AS, A gain-of-function mutation of JAK2 in myeloproliferative disorders. N Engl J Med 2005;352(17):1779-90
   PubMed Web of Science ®Google Scholar
• Levine RL, Wadleigh M, Cools J, Activating mutation in the tyrosine kinase JAK2 in polycythemia vera, essential thrombocythemia, and myeloid metaplasia with myelofibrosis. Cancer Cell 2005;7(4):387-97
   PubMed Web of Science ®Google Scholar
• Verstovsek S, Mesa RA, Gotlib J, A double-blind, placebo-controlled trial of ruxolitinib for myelofibrosis. N Engl J Med 2012;366(9):799-807
   PubMed Web of Science ®Google Scholar
• Harrison C, Kiladjian JJ, Al-Ali HK, JAK inhibition with ruxolitinib versus best available therapy for myelofibrosis. N Engl J Med 2012;366(9):787-98
   PubMed Web of Science ®Google Scholar
• Leah E. Clinical trials: phase III trial results for tofacitinib bring new oral DMARD therapy a step closer for patients with rheumatoid arthritis. Nat Rev Rheumatol 2012;8(10):561
   PubMedGoogle Scholar
• Garber K. Pfizer's JAK inhibitor sails through phase 3 in rheumatoid arthritis. Nat Biotechnol 2011;29(6):467-8
   PubMed Web of Science ®Google Scholar
• FDA approves Xeljanz for rheumatoid arthritis. 2012. Available from: http://www.fda.gov/NewsEvents/Newsroom/PressAnnouncements/ucm327152.htm [Last accessed November 2012]
   Google Scholar
• Stark GR, Darnell JE Jr. The JAK-STAT pathway at twenty. Immunity 2012;36(4):503-14
   PubMed Web of Science ®Google Scholar
• Croker BA, Kiu H, Nicholson SE. SOCS regulation of the JAK/STAT signalling pathway. Semin cell Dev Biol 2008;19(4):414-22
   PubMed Web of Science ®Google Scholar
• Rodig SJ, Meraz MA, White JM, Disruption of the Jak1 gene demonstrates obligatory and nonredundant roles of the Jaks in cytokine-induced biologic responses. Cell 1998;93(3):373-83
   PubMed Web of Science ®Google Scholar
• Neubauer H, Cumano A, Muller M, Jak2 deficiency defines an essential developmental checkpoint in definitive hematopoiesis. Cell 1998;93(3):397-409
   PubMed Web of Science ®Google Scholar
• Parganas E, Wang D, Stravopodis D, Jak2 is essential for signaling through a variety of cytokine receptors. Cell 1998;93(3):385-95
   PubMed Web of Science ®Google Scholar
• Samanta AK, Lin H, Sun T, Janus kinase 2: a critical target in chronic myelogenous leukemia. Cancer Res 2006;66(13):6468-72
   PubMed Web of Science ®Google Scholar
• Macchi P, Villa A, Giliani S, Mutations of Jak-3 gene in patients with autosomal severe combined immune deficiency (SCID). Nature 1995;377(6544):65-8
   PubMed Web of Science ®Google Scholar
• Russell SM, Tayebi N, Nakajima H, Mutation of Jak3 in a patient with SCID: essential role of Jak3 in lymphoid development. Science 1995;270(5237):797-800
   PubMed Web of Science ®Google Scholar
• Suzuki K, Nakajima H, Saito Y, 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. Int Immunol 2000;12(2):123-32
   PubMed Web of Science ®Google Scholar
• Shaw MH, Boyartchuk V, Wong S, A natural mutation in the Tyk2 pseudokinase domain underlies altered susceptibility of B10.Q/J mice to infection and autoimmunity. Proc Nat Acad Sci USA 2003;100(20):11594-9
   PubMed Web of Science ®Google Scholar
• Ishizaki M, Akimoto T, Muromoto R, Involvement of tyrosine kinase-2 in both the IL-12/Th1 and IL-23/Th17 axes in vivo. J Immunol 2011;187(1):181-9
   PubMed Web of Science ®Google Scholar
• Prchal-Murphy M, Semper C, Lassnig C, TYK2 kinase activity is required for functional type I interferon responses in vivo. PLoS One 2012;7(6):e39141
   PubMed Web of Science ®Google Scholar
• Ishizaki M, Muromoto R, Akimoto T, Tyk2 deficiency protects joints against destruction in anti-type II collagen antibody-induced arthritis in mice. Int Immunol 2011;23(9):575-82
   Google Scholar
• Norman P. Selective JAK1 inhibitor and selective Tyk2 inhibitor patents. Expert Opin Ther Pat 2012;22(10):1233-49
   PubMed Web of Science ®Google Scholar
• Kiss R, Sayeski PP, Keseru GM. Recent developments on JAK2 inhibitors: a patent review. Expert Opin Ther Pat 2010;20(4):471-95
   PubMed Web of Science ®Google Scholar
• Wilson LJ. Recent patents in the discovery of small molecule inhibitors of JAK3. Expert Opin Ther Pat 2010;20(5):609-23
   PubMed Web of Science ®Google Scholar
• Ambit Biosciences Corp. Quinoline and isoquinoline compounds and methods of use thereof. WO2012030944; 2012
   Google Scholar
• Ambit Biosciences Corp. Azolopyridine and azolopyrimidine compounds and methods of use thereof. WO2012030924; 2012
   Google Scholar
• Ambit Biosciences Corp. 4-azolylaminoquinazoline derivatives and methods of use thereof. WO2012030914; 2012
   Google Scholar
• Ambit Biosciences Corp. 7-cyclylquinazoline derivatives and methods of use thereof. WO2012030912; 2012
   Google Scholar
• Ambit Biosciences Corp. 2-cycloquinazoline derivatives and methods of use thereof. WO2012030910; 2012
   Google Scholar
• Ambit Biosciences Corp. JAK kinase modulating quinazoline derivatives and methods of use thereof. WO2010099379; 2010
   Google Scholar
• Ambit Biosciences Corp. Thienopyridine and thienopyrimidine compounds and methods of use thereof. WO2012030894; 2012
   Google Scholar
• Ambit Biosciences Corp. JAK kinase modulating compounds and methods of use thereof. WO2010002472; 2010
   Google Scholar
• Array Biopharma, Inc. 5,7-substituted-imidazo[1,2-c]pyrimidines as inhibitors of JAK kinases. WO2011130146; 2011
   Google Scholar
• AstraZeneca AB. Heterocyclic JAK kinase inhibitors. WO2010038060; 2010
   Google Scholar
• AstraZeneca AB. 2-(imidazolylamino)-pyridine derivatives and their use as JAK kinase inhibitors. WO2010020810; 2010
   Google Scholar
• Bristol-Myers Squibb Co. JAK2 inhibitors and their use for the treatment of myeloproliferative diseases and cancer. WO2011028864; 2011
   Google Scholar
• Purandare AV, McDevitt TM, Wan H, Characterization of BMS-911543, a functionally selective small-molecule inhibitor of JAK2. Leukemia 2012;26(2):280-8
   PubMed Web of Science ®Google Scholar
• Clinical Trial of BMS-911543. 2012. Available from: http://clinicaltrials.gov/ct2/show/NCT01236352?term=911543&rank=1 [Last accessed November 2012]
   Google Scholar
• Cephalon, Inc. Preparation and uses of 1,2,4-triazolo[1,5-a]pyridine derivatives. WO2010141796; 2010
   Google Scholar
• Dugan BJ, Gingrich DE, Mesaros EF, 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(11):5243-54
   PubMed Web of Science ®Google Scholar
• Seavey MM, Lu LD, Stump KL, Therapeutic efficacy of CEP-33779, a novel selective JAK2 inhibitor, in a mouse model of colitis-induced colorectal cancer. Mol Cancer Ther 2012;11(4):984-93
   PubMed Web of Science ®Google Scholar
• Zificsak CA, Gingrich DE, Breslin HJ, Optimization of a novel kinase inhibitor scaffold for the dual inhibition of JAK2 and FAK kinases. Bioorg Med Chem Lett 2012;22(1):133-7
   PubMed Web of Science ®Google Scholar
• Cephalon, Inc. Pyrrolotriazines as ALK and JAK2 inhibitors. WO2010071885; 2010
   Google Scholar
• Weinberg LR, Albom MS, Angeles TS, 2,7-Pyrrolo[2,1-f][1,2,4]triazines as JAK2 inhibitors: modification of target structure to minimize reactive metabolite formation. Bioorg Med Chem Lett 2011;21(24):7325-30
   PubMed Web of Science ®Google Scholar
• SAR302503 in phase II studies for myelofibrosis. 2012. Available from: http://clinicaltrials.gov/ct2/show/NCT01420770?term=JAK&rank=17 [Last accessed November 2012]
   Google Scholar
• SAR302503 trial for patients previously treated with Ruxolitinib. Available from: http://clinicaltrials.gov/ct2/show/NCT01523171?term=JAK&rank=33 [Last accessed November 2012]
   Google Scholar
• Mesaros EF, Thieu TV, Wells GJ, 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. J Med Chem 2012;55(1):115-25
   Google Scholar
• Ott GR, Wells GJ, Thieu TV, 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. J Med Chem 2011;54(18):6328-41
   PubMed Web of Science ®Google Scholar
• Debiopharm SA. Bicyclic compounds and their uses as dual c-Src/JAK inhibitors. WO2011101806; 2011
   Google Scholar
• Eli Lilly and Co. Amino pyrazole compound. US20100152181; 2010
   Google Scholar
• Mitchell D, Cole KP, Pollock PM, Development and a practical synthesis of the JAK2 inhibitor LY2784544. Org Proc Res Dev 2012;17:70-81
   Google Scholar
• Galapagos NV. Novel compounds useful for the treatment of degenerative and inflammatory diseases (1). WO2010010191; 2010
   Google Scholar
• Galapagos NV. Novel compounds useful for the treatment of degenerative and inflammatory diseases (2). WO2010010190; 2010
   Google Scholar
• Galapagos NV. Novel compounds useful for the treatment of degenerative and inflammatory diseases (3). WO2010010189; 2010
   Google Scholar
• Galapagos NV. Novel compounds useful for the treatment of degenerative and inflammatory diseases (4). WO2010010188; 2010
   Google Scholar
• Galapagos NV. Novel compounds useful for the treatment of degenerative and inflammatory diseases (5). WO2010010187; 2010
   Google Scholar
• Galapagos NV. Novel compounds useful for the treatment of degenerative and inflammatory diseases (6). WO2010010186; 2010
   Google Scholar
• Galapagos NV. [1,2,4]triazolo[1,5-a] pyridines as JAK inhibitors. WO2010010184; 2010
   Google Scholar
• Galapagos NV. 5-phenyl-[1,2,4]triazolo[1,5-a]pyridin-2-yl carboxamides as JAK inhibitors. WO2010149769; 2010
   Google Scholar
• Genentech, Inc. Pyrazolopyrimidine JAK inhibitor compounds and methods. WO2010051549; 2010
   Google Scholar
• Genentech, Inc. Pyrazolopyrimidine JAK inhibitor compounds and methods. WO2011003065; 2011
   Google Scholar
• Hanan EJ, van Abbema A, Barrett K, Discovery of potent and selective pyrazolopyrimidine janus kinase 2 inhibitors. J Med Chem 2012;55(22):10090-107
   PubMed Web of Science ®Google Scholar
• Hutchison MediPharma Ltd. Pyrrolopyrimidine compounds and uses thereof (1). WO2012022045; 2012
   Google Scholar
• Hutchison Medipharma Ltd. Pyrrolopyrimidine compounds and uses thereof (2). WO2012022265; 2012
   Google Scholar
• Incyte Corp. Heterocyclic-substituted pyrrolopyridines and pyrrolopyrimidines as JAK inhibitors. WO2012068440; 2012
   Google Scholar
• Incyte Corp. Process for preparing JAK inhibitors and related intermediate compounds. WO2010083283; 2010
   Google Scholar
• Lin Q, Meloni D, Pan Y, Enantioselective synthesis of Janus kinase inhibitor INCB018424 via an organocatalytic aza-Michael reaction. Org Lett 2009;11(9):1999-2002
   Google Scholar
• Incyte Corp. Heterocyclic derivatives of pyrazol-4-yl-pyrrolo[2,3-d]pyrimidines as Janus kinase inhibitors. WO2011028685; 2011
   Google Scholar
• Incyte Corp. 3-[4-(7H-Pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl]octane- or heptane-nitrile as JAK inhibitors. WO2010135621; 2010
   Google Scholar
• Incyte Corp. Janus kinase inhibitors for the treatment of dry eye and other eye related diseases. WO2010039939; 2010
   Google Scholar
• Liew SH, Nichols KK, Klamerus KJ, Tofacitinib (CP-690,550), a Janus kinase inhibitor for dry eye disease: results from a phase 1/2 trial. Ophthalmology 2012;119(7):1328-35
   PubMed Web of Science ®Google Scholar
• Incyte Corp. Topical formulation for a JAK inhibitor. WO2011146808; 2011
   Google Scholar
• Incyte Corp. Cyclobutyl substituted pyrrolopyridine and pyrrolopyrimidine derivatives as JAK inhibitors. WO2012068450; 2012
   Google Scholar
• Incyte Corp. Cyclobutane and methylcyclobutane derivatives as janus kinase derivatives. WO2011103423; 2011
   Google Scholar
• Incyte Corp. Hydroxyl, keto, and glucuronide derivatives of 3-(4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl]-3-cyclopentylpropanenitrile. WO2011044481; 2011
   Google Scholar
• Incyte Corp. Macrocyclic compounds and their use as kinase inhibitors. WO2010085597; 2010
   Google Scholar
• F. Hoffmann-La Roche AG. Macrocyclic inhibitors of JAK. WO2011033053; 2011
   Google Scholar
• William AD, Lee AC, Blanchard S, 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. J Med Chem 2011;54(13):4638-58
   PubMed Web of Science ®Google Scholar
• William AD, Lee AC, Poulsen A, 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-3 (JAK2/FLT3) for the treatment of rheumatoid arthritis. J Med Chem 2012;55(6):2623-40
   PubMed Web of Science ®Google Scholar
• William AD, Lee AC, Goh KC, 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)]heptaco sa-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. J Med Chem 2012;55(1):169-96
   PubMed Web of Science ®Google Scholar
• Tragara Pharmaceuticals, Inc. Solid state forms of macrocyclic kinase inhibitors. WO2011097525; 2011
   Google Scholar
• Merck Sharp & Dohme Corp. Inhibitors of Janus kinases (2). WO2010014453; 2010
   Google Scholar
• Merck Sharp & Dohme Corp. Inhibitors of Janus kinases (1). WO2010011375; 2010
   Google Scholar
• Nerviano Medical Sciences. Substituted indazole derivatives active as kinase inhibitors. WO2010069966; 2010
   Google Scholar
• Novartis Pharma AG. mTOR/JAK inhibitor combination therapy. WO2012112847; 2012
   Google Scholar
• Pfizer, Inc. Pyrrolo[2,3-d]pyrimidine urea compounds as JAK inhibitors. WO2011097087; 2011
   Google Scholar
• Pfizer, Inc. Beneficial effects of combination therapy on cholesterol. US20120252825; 2012
   Google Scholar
• Pfizer, Inc. Pyrrolo[2,3-d]pyrimidine compounds. WO2010020905; 2010
   Google Scholar
• Pfizer, Inc. Pyrrolo[2,3-d]pyrimidine compounds (2). WO2011075334; 2011
   Google Scholar
• Pfizer, Inc. Pyrrolo[2,3-d]pyrimidine compounds (1). WO2011045702; 2011
   Google Scholar
• Auspex Pharmaceuticals, LLC. Piperidine inhibitors of Janus Kinase 3. WO2010123919; 2010
   Google Scholar
• Ratiopharm and Teva. Process for preparing tofacitinib salts. WO2012135338; 2012
   Google Scholar
• Pfizer, Inc. Crystalline and non-crystalline forms of tofacitinib, and a pharmaceutical composition comprising tofacitinib and a penetration enhancer. WO2012137111; 2012
   Google Scholar
• S*BIO Pte Ltd. Oxygen linked pyrimidine derivatives. WO2007058627; 2007
   Google Scholar
• S*BIO Pte Ltd. 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 citrate salt. WO2010068181; 2010
   Google Scholar
• S*BIO Pte Ltd. 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 maleate salt. WO2010068182; 2010
   Google Scholar
• S*BIO Pte Ltd. 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),2,4,9,14,16,18(26),20,22-nonaene citrate salt. WO2011008172; 2010
   Google Scholar
• Rigel Pharmaceuticals, Inc. Compositions and methods for inhibition of the JAK pathway. WO2012015972; 2012
   Google Scholar
• Rigel Pharmaceuticals. Tricyclic carbamate JAK inhibitors. WO2010039518; 2010
   Google Scholar
• Rigel Pharmaceuticals, Inc. Compositions and methods for inhibition of the JAK pathway; 2). WO2010085684; 2010
   Google Scholar
• Rigel Pharmaceuticals, Inc. Compositions and methods for inhibition of the JAK pathway. WO2010075558; 2010
   Google Scholar
• Pardanani A, Hood J, Lasho T, TG101209, a small molecule JAK2-selective kinase inhibitor potently inhibits myeloproliferative disorder-associated JAK2V617F and MPLW515L/K mutations. Leukemia 2007;21(8):1658-68
   PubMed Web of Science ®Google Scholar
• Targegen, Inc. Compositions and methods for treating myelofibrosis. WO2012061833; 2012
   Google Scholar
• Targegen, Inc. Compositions and methods for treating myelofibrosis (2). WO2012060847; 2012
   Google Scholar
• University of Florida Research Foundation, Inc. Kinase inhibitor compounds. WO2010068710; 2010
   Google Scholar
• YM Biosciences Australia Pty Ltd. Multiple myeloma treatment. WO2012149602; 2012
   Google Scholar
• YM Biosciences Australia Pty Ltd. Treatment of JAK2 mediated conditions. WO2012071612; 2012
   Google Scholar
• Biocryst Pharmaceuticals, Inc. Heterocyclic compounds as Janus kinase inhibitors (1). WO2011031554; 2011
   Google Scholar
• Biocryst Pharmaceuticals, Inc. Pyrrolo[1,2-b]pyridazine derivatives as Janus kinase inhibitors. WO2011014817; 2011
   Google Scholar
• Biocryst Pharmaceuticals, Inc. Heterocyclic compounds as Janus kinase inhibitors (2). WO2011150356; 2011
   Google Scholar
• Biocryst Pharmaceuticals, Inc. Heterocyclic compounds as Janus kinase inhibitors (3). WO2011079230; 2011
   Google Scholar
• Bristol-Myers Squibb Co. Pyrrolopyridazine JAK3 inhibitors and their use for the treatment of inflammatory and autoimmune diseases. WO2012125887; 2012
   Google Scholar
• Cellzome Ltd. Heterocyclyl pyrazolopyrimidine analogues as selective JAK inhibitors. WO2012022681; 2012
   Google Scholar
• Cellzome Ltd. Pyrazole compounds as JAK inhibitors. WO2011134831; 2011
   Google Scholar
• Cellzome Ltd. Heterocyclyl pyrazolopyrimidine analogues as JAK inhibitors. WO2011048082; 2011
   Google Scholar
• Cellzome Ltd. Ortho substituted pyrimidine compounds as JAK inhibitors. WO2011029807; 2011
   Google Scholar
• Dainippon Sumitomo Pharma. New azaindole derivatives. JP2012012332; 2012
   Google Scholar
• Kowa Co., Ltd. Pyridine-3-carboxyamide derivative. WO2010061971; 2010
   Google Scholar
• Portola Pharmaceuticals, Inc. Inhibitors of JAK. WO2010129802; 2010
   Google Scholar
• Portola dual SYK-JAK inhibitor. Available from: http://www.portola.com/PRT2070-Dual-SYK-JAK-Inhibitor [Last accessed November 2012]
   Google Scholar
• Portola Pharmaceuticals, Inc. Nicotinamides as JAK kinase modulators. US20120108566; 2012
   Google Scholar
• F. Hoffmann-La Roche AG. Pyrrolopyrazine derivatives as SYK and JAK inhibitors. WO2011144584; 2011
   Google Scholar
• F.Hoffman-La Roche AG. Pyrrolo[2,3-b]pyrazine-7-carboxamide derivatives and their uses as JAK and SYK inhibitors. WO2011144585; 2011
   Google Scholar
• F.Hoffman-La Roche AG. Pyrrolopyrazinyl urea kinase inhibitors. WO2010063634; 2010
   Google Scholar
• F.Hoffman-La Roche AG. Janus kinase inhibitor compounds and methods. WO2010142752; 2010
   Google Scholar
• Takeda Pharmaceutical Co. Ltd. Dihydropyrrolonaphthyridinone compounds as inhibitors of JAK. WO2010144486; 2010
   Google Scholar
• Advinus Therapeutics Ltd. Substituted fused tricyclic compounds, compositions and medicinal applications thereof. WO2012127506; 2012
   Google Scholar
• Almirall, SA. Imidazo[1,2-b]pyridazine and imidazo[4,5-b]pyridine derivatives as JAK inhibitors. WO2012069202; 2012
   Google Scholar
• Almirall, SA. Pyrazole derivatives as JAK inhibitors. WO2011101161; 2011
   Google Scholar
• Almirall, SA. Imidazopyridine derivatives as JAK inhibitors. WO2011076419; 2011
   Google Scholar
• Almirall, SA. Heteroaryl imidazole derivatives as JAK inhibitors. WO2011157397; 2011
   Google Scholar
• Almirall, SA. Pyridine and isoquinoline derivatives as SYK- and JAK-kinase inhibitors. WO2012041476; 2012
   Google Scholar
• Astellas Pharma, Inc. Fused pyrrolopyridine derivative. WO2010119875; 2010
   Google Scholar
• Japan Tobacco, Inc. Nitrogen-containing spiro-ring compound and medicinal use of same. WO2011013785; 2011
   Google Scholar
• Jiangsu Simcere. Large ring compound and application thereof. CN102617599; 2012
   Google Scholar
• Leo Pharma A/S. Novel homopiperazine derivatives as protein tyrosine kinase inhibitors and pharmaceutical use thereof. WO2012003829; 2012
   Google Scholar
• Leo Pharma A/S. Heterocyclic compounds as JAK receptor and protein tyrosine kinase inhibitors. WO2011003418; 2011
   Google Scholar
• Merck Sharp & Dohme Corp. Bicyclic diamines as Janus kinase inhibitors. WO2012054364; 2012
   Google Scholar
• Merck Sharp & Dohme Corp. Azaindoles as Janus kinase inhibitors. WO2011137022; 2011
   Google Scholar
• Palau Pharma, SA. N-containing heteroaryl derivatives as JAK3 kinase inhibitors. WO2011051452; 2011
   Google Scholar
• Palau Pharma, SA. Pyrazole[1,5-a]pyridine derivatives. WO2010072823; 2010
   Google Scholar
• Andraos R, Qian Z, Bonenfant D, Modulation of activation-loop phosphorylation by JAK inhibitors is binding mode dependent. Cancer Discov 2012;2(6):512-23
   PubMed Web of Science ®Google Scholar
• Alicea-Velazquez NL, Boggon TJ. The use of structural biology in Janus kinase targeted drug discovery. Curr Drug Targets 2011;12(4):546-55
   PubMed Web of Science ®Google Scholar
• Marit MR, Chohan M, Matthew N, Random mutagenesis reveals residues of JAK2 critical in evading inhibition by a tyrosine kinase inhibitor. PloS One 2012;7(8):e43437
   Google Scholar
• Deshpande A, Reddy MM, Schade GO, Kinase domain mutations confer resistance to novel inhibitors targeting JAK2V617F in myeloproliferative neoplasms. Leukemia 2012;26(4):708-15
   PubMed Web of Science ®Google Scholar
• Ingley E, Klinken SP. Cross-regulation of JAK and Src kinases. Growth Factors 2006;24(1):89-95
   PubMed Web of Science ®Google Scholar
• Reilly JT. FLT3 and its role in the pathogenesis of acute myeloid leukaemia. Leuk Lymphoma 2003;44(1):1-7
   PubMed Web of Science ®Google Scholar
• Younes A, Romaguera J, Fanale M, 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. J Clin Oncol 2012;30(33):4161-7
   PubMed Web of Science ®Google Scholar
• Novotny-Diermayr V, Hart S, Goh KC, The oral HDAC inhibitor pracinostat (SB939) is efficacious and synergistic with the JAK2 inhibitor pacritinib (SB1518) in preclinical models of AML. Blood Cancer J 2012;2(5):e69
   PubMedGoogle Scholar
• Panobinostat and Ruxolitinib in MPN clinical trial. 2011. Available from: http://clinicaltrials.gov/ct2/show/NCT01433445?term=ruxolitinib+and+panobinostat&rank=2 [Last accessed November 2012]
   Google Scholar
• Koppikar P, Bhagwat N, Kilpivaara O, Heterodimeric JAK-STAT activation as a mechanism of persistence to JAK2 inhibitor therapy. Nature 2012;489(7414):155-9
   PubMed Web of Science ®Google Scholar
• AZD1480 Phase 1 study in solid tumors. 2010. Available from: http://clinicaltrials.gov/ct2/show/NCT01112397?term=AZD1480&rank=2 [Last accessed November 2012]
   Google Scholar
• Maiga M, Lun S, Guo H, Risk of tuberculosis reactivation with tofacitinib (CP-690550. J Infect Dis 2012;205(11):1705-8
   PubMedGoogle Scholar
• Yoshida H, Kimura A, Fukaya T, Low dose CP-690,550 (tofacitinib), a pan-JAK inhibitor, accelerates the onset of experimental autoimmune encephalomyelitis by potentiating Th17 differentiation. Biochem Biophys Res Commun 2012;418(2):234-40
   PubMed Web of Science ®Google Scholar
• Migita K, Miyashita T, Izumi Y, Inhibitory effects of the JAK inhibitor CP690,550 on human CD4(+) T lymphocyte cytokine production. BMC Immunol 2011;12:51
   PubMed Web of Science ®Google Scholar
• Papp KA, Menter A, Strober B, Efficacy and safety of tofacitinib, an oral Janus kinase inhibitor, in the treatment of psoriasis: a Phase 2b randomized placebo-controlled dose-ranging study. Br J Dermatol 2012;167(3):668-77
   PubMed Web of Science ®Google Scholar
• Vincenti F, Tedesco Silva H, Busque S, Randomized Phase 2b Trial of Tofacitinib (CP-690,550) in De Novo Kidney Transplant Patients: efficacy, Renal Function and Safety at 1 Year. Am J Transplant 2012;12(9):2446-56
   PubMed Web of Science ®Google Scholar
• Myrvang H. Transplantation: tofacitinib safe and effective in renal transplant recipients. Nat Rev Nephrol 2012;8(8):432
   PubMedGoogle Scholar
• Sandborn WJ, Ghosh S, Panes J, Tofacitinib, an oral Janus kinase inhibitor, in active ulcerative colitis. N Engl J Med 2012;367(7):616-24
   PubMed Web of Science ®Google Scholar
• Minturn JE, Evans AE, Villablanca JG, Phase I trial of lestaurtinib for children with refractory neuroblastoma: a new approaches to neuroblastoma therapy consortium study. Cancer Chemother Pharmacol 2011;68(4):1057-65
   PubMed Web of Science ®Google Scholar
• Levis M, Ravandi F, Wang ES, Results from a randomized trial of salvage chemotherapy followed by lestaurtinib for patients with FLT3 mutant AML in first relapse. Blood 2011;117(12):3294-301
   PubMed Web of Science ®Google Scholar
• Santos FP, Kantarjian HM, Jain N, Phase 2 study of CEP-701, an orally available JAK2 inhibitor, in patients with primary or post-polycythemia vera/essential thrombocythemia myelofibrosis. Blood 2010;115(6):1131-6
   PubMed Web of Science ®Google Scholar
• Pardanani A, Gotlib JR, Jamieson C, Safety and efficacy of TG101348, a selective JAK2 inhibitor, in myelofibrosis. J Clin Oncol 2011;29(7):789-96
   PubMed Web of Science ®Google Scholar
• Lasho TL, Tefferi A, Hood JD, 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. Leukemia 2008;22(9):1790-2
   PubMed Web of Science ®Google Scholar
• Targegen, Inc. Biaryl meta pyrimidine inhibitors of kinases. US20110212077; 2011
   Google Scholar
• SB1518 myelofibrosis clinical trial. 2008. Available from: http://clinicaltrials.gov/ct2/show/NCT00745550?term=SB1518&rank=1 [Last accessed November 2012]
   Google Scholar
• SB1518 myelodysplastic Syndrome (MDS) clinical trial. Available from: http://clinicaltrials.gov/ct2/show/NCT01436084?term=SB1518&rank=5 [Last accessed November 2012]
   Google Scholar
• Fridman JS, Scherle PA, Collins R, Selective inhibition of JAK1 and JAK2 is efficacious in rodent models of arthritis: preclinical characterization of INCB028050. J Immunol 2010;184(9):5298-307
   PubMed Web of Science ®Google Scholar
• Baricitinib in participants with diabetic kidney disease. 2012. Available from: http://clinicaltrials.gov/ct2/show/NCT01683409?term=baricitinib&rank=1 [Last accessed November 2012]
   Google Scholar
• Monaghan KA, Khong T, Burns CJ, Spencer A. The novel JAK inhibitor CYT387 suppresses multiple signalling pathways, prevents proliferation and induces apoptosis in phenotypically diverse myeloma cells. Leukemia 2011;25(12):1891-9
   PubMed Web of Science ®Google Scholar
• Tyner JW, Bumm TG, Deininger J, CYT387, a novel JAK2 inhibitor, induces hematologic responses and normalizes inflammatory cytokines in murine myeloproliferative neoplasms. Blood 2010;115(25):5232-40
   PubMed Web of Science ®Google Scholar
• Ioannidis S, Lamb ML, Wang T, Discovery of 5-chloro-N2-[(1S)-1-(5-fluoropyrimidin-2-yl)ethyl]-N4-(5-methyl-1H-pyrazol-3-yl)p yrimidine-2,4-diamine (AZD1480) as a novel inhibitor of the Jak/Stat pathway. J Med Chem 2011;54(1):262-76
   PubMed Web of Science ®Google Scholar
• Xin H, Herrmann A, Reckamp K, Antiangiogenic and antimetastatic activity of JAK inhibitor AZD1480. Cancer Res 2011;71(21):6601-10
   PubMed Web of Science ®Google Scholar
• AZD1480 clinical trial. 2010. Available from: http://clinicaltrials.gov/ct2/show/NCT01112397?term=AZD1480&rank=2 [Last accessed November 2012]
   Google Scholar
• Hedvat M, Huszar D, Herrmann A, The JAK2 inhibitor AZD1480 potently blocks Stat3 signaling and oncogenesis in solid tumors. Cancer Cell 2009;16(6):487-97
   PubMed Web of Science ®Google Scholar
• McFarland BC, Ma JY, Langford CP, Therapeutic potential of AZD1480 for the treatment of human glioblastoma. Mol Cancer Ther 2011;10(12):2384-93
   PubMed Web of Science ®Google Scholar
• Madan B, Goh KC, Hart S, SB1578, a Novel Inhibitor of JAK2, FLT3, and c-Fms for the Treatment of Rheumatoid Arthritis. J Immunol 2012;189(8):4123-34
   PubMed Web of Science ®Google Scholar
• SB1578 clinical trial. 2011. Available from: http://clinicaltrials.gov/ct2/show/NCT01235871?term=1578&rank=1 [Last accessed November 2012]
   Google Scholar
• LY2784544 myeloproliferative neoplasms clinical trial. 2012. Available from: http://clinicaltrials.gov/ct2/show/NCT01594723?term=LY2784544&rank=3 [Last accessed November 2012]
   Google Scholar
• Nakaya Y, Shide K, Niwa T, Efficacy of NS-018, a potent and selective JAK2/Src inhibitor, in primary cells and mouse models of myeloproliferative neoplasms. Blood Cancer J 2011;1(7):e29
   PubMed Web of Science ®Google Scholar
• NS-018 oral clinical trial in MPN patients. 2011. Available from: http://clinicaltrials.gov/ct2/show/NCT01423851?term=NS-018&rank=1 [Last accessed November 2012]
   Google Scholar
• VX-509 clinical trial in RA in subject taking methotrexate. 2012. Available from: http://clinicaltrials.gov/ct2/show/NCT01590459?term=VX-509&rank=2 [Last accessed November 2012]
   Google Scholar
• GSK2586184 Phase 1 trial. 2012. Available from: http://clinicaltrials.gov/ct2/show/NCT01687309?term=GSK2586184&rank=1 [Last accessed November 2012]
   Google Scholar
• GLPG0634 in methotrexate-refractory rheumatoid arthritis patients. 2011. Available from: http://clinicaltrials.gov/ct2/show/NCT01384422?term=GLPG-0634&rank=5 [Last accessed November 2012]
   Google Scholar
• Two clinical posters on GLPG-0634. 2012. Available from: http://www.glpg.com/index.php/randd/pipeline/glpg0634-ra/ [Last accessed November 2012]
   Google Scholar