US 6500854B1
· Kitamura et al.
· 2002
[cited by applicant]
US 8088764B2
· Menet
· 2012
[cited by examiner]
US 8242274B2
· Menet et al.
· 2012
[cited by applicant]
US 8563545B2
· Menet
· 2013
[cited by examiner]
US 8853240B2
· Menet et al.
· 2014
[cited by applicant]
US 8999979B2
· Menet
· 2015
[cited by examiner]
US 9284311B2
· Van 't Klooster et al.
· 2016
[cited by applicant]
US 9309244B2
· Menet
· 2016
[cited by examiner]
US 9382247B2
· Sabourault et al.
· 2016
[cited by applicant]
US 9415037B2
· Menet et al.
· 2016
[cited by applicant]
US 9707237B2
· Menet
· 2017
[cited by examiner]
US 20050222171A1
· Bold et al.
· 2005
[cited by applicant]
US 20130310340A1
· Payan et al.
· 2013
[cited by applicant]
EP 0132851A1
· 1985
[cited by applicant]
EP 1391211A1
· 2004
[cited by applicant]
WO 2003010167A1
· 2003
[cited by applicant]
WO 2004072072A1
· 2004
[cited by applicant]
WO 2005124342A2
· 2005
[cited by applicant]
WO 2006018735A2
· 2006
[cited by applicant]
WO 2006038116A2
· 2006
[cited by applicant]
WO 2007009773A1
· 2007
[cited by applicant]
WO 2008025821A1
· 2008
[cited by applicant]
WO 2008150015A1
· 2008
[cited by applicant]
WO 2009010530A1
· 2009
[cited by applicant]
WO 2009017954A1
· 2009
[cited by applicant]
WO 2009027283A1
· 2009
[cited by applicant]
WO 2009047514A1
· 2009
[cited by applicant]
WO 2009155565A1
· 2009
[cited by applicant]
WO 2010010184A1
· 2010
[cited by applicant]
WO 2010010186A1
· 2010
[cited by applicant]
WO 2010010187A1
· 2010
[cited by applicant]
WO 2010010188A1
· 2010
[cited by applicant]
WO 2010010189A1
· 2010
[cited by applicant]
WO 2010010190A1
· 2010
[cited by applicant]
WO 2010010191A1
· 2010
[cited by applicant]
WO 2010141796A2
· 2010
[cited by applicant]
WO 2010149769A1
· 2010
[cited by applicant]
WO 2010149771A1
· 2010
[cited by applicant]
WO 2013189771A1
· 2013
[cited by applicant]
Argiles, “Catabolic Proinflammatory Cytokines”, Curr. Opin. Clin. Nutr. Metab. Care, vol. 1, 2009, pp. 245-251.
[cited by applicant]
Asquith, et al., “Autoimmune Disease: Rheumatoid Arthritis—Animal Models of Rheumatoid Arthritis,” Eur. J. Immunol., vol. 39, 2009, pp. 2040-2044.
[cited by applicant]
Bain, J.—“The Specificities of Protein Kinase Inhibitors: An Update”, Biochem J., vol. 371, 2003, pp. 199-204.
[cited by applicant]
Berishaj, et al., “Stat3 is Tyrosine-phosphorylated Through the Interleukin-6/glycoprotein 130/Janus Kinase Pathway in Breast Cancer,” Breast Cancer Res. vol. 9, No. 3, 2007, R32.
[cited by applicant]
Bundgard., “Prodrugs as a Means to Improve the Delivery of Peptide Drugs,” Adv. Drug Del Rev., vol. 8, 1992, pp. 1-38.
[cited by applicant]
Bush, “Reduction of Joint Inflammation and Bone Erosion in Rat Adjuvant Arthritis by Treatment With Interleukin-17 Receptor lgG1 Fe Fusion Protein”, Arthritis Rheum., vol. 46, 2002, pp. 802-805.
[cited by applicant]
Changelian, et al., “The Specificity of JAK3 kinase Inhibitors,” Blood, vol. 111, 2008, pp. 2155-2157.
[cited by applicant]
Chen, et al., “Janus Kinase Deregulation in Leukemia and Lymphoma,” Immunity, vol. 36, 2012, pp. 529-541.
[cited by applicant]
Chmp, Guideline on Clinical Investigation of Medicinal Products indicated for the treatment of Psoriasis, 2004.
[cited by applicant]
Choy, E. H. S. and G. S. Panayi, “Cytokinpea Thwayasn D Joint Inflammaint Rihoenum Atoid Arthritis”, N Engl J Med vol. 344, No. 12, 2001, pp. 907-916.
[cited by applicant]
Chubinskaya, “Regulation of Osteogenic Proteins by Chondrocytes”, Int. J. Bio Gel Biology, 2003, pp. 1323-1340.
[cited by applicant]
Clegg, D. 0., D. J. Reda, et al., “Glucosamine, Chondroitin Sulfate, and the Two in Combination for Painful Knee Osteoarthritis”, N Engl J Med, vol. 354, No. 8, 2006, pp. 795-808.
[cited by applicant]
Constantinescu, et al. “Mining for JAK-STAT Mutations in Cancer” Trends in Biochemical Sciences, vol. 33, No. B. 2007, pp. 122-131.
[cited by applicant]
Dolgin, “Companies Hope for Kinase Inhibitor JAKpot,” Elie—Nature Reviews, Drug Discovery, vol. 10, Oct. 2011, pp. 717-718.
[cited by applicant]
Drug Discovery and Development, Understanding The R&D Process—Pharmaceutical Research and Manufacturers of America, 2007, pp. 1-14.
[cited by applicant]
Dymock, “Recent News in the Fast-Paced Field of JAK Inhibitors,” J_ Develop Drugs, vol. 2, No. 2, 2013, pp. 1-2.
[cited by applicant]
Fabian—“A small Molecule-kinase Interaction Map for Clinical Kinase Inhibitors”, Nature Biotech, vol. 23, 2005, pp. 629-336.
[cited by applicant]
Firestein, G. S., “Evolving Concepts of Rheumatoid Arthritis”, Nature, vol. 423, No. 6937, 2003, pp. 356-361.
[cited by applicant]
Geron, “Selective Inhibition of JAK2-Driven Erythroid Differentiation of Polycythemia Vera Progenitors” Cancer Cell, vol. 13, No. 4, 2008, pp. 321-330.
[cited by applicant]
Ghangelian, et al., “The Specificity of JAK3 Kinase Inhibitors,” Blood, vol. 111, 2008, pp. 2155-2157.
[cited by applicant]
Ingersoll, et al., “The Impact of Medication Regimen Factors on Adherence to Chronic Treatment: A Review of Literature,” J. Behav. Med., vol. 31, No. 3, Jun. 2008, pp. 213-224.
[cited by applicant]
IP, “Interleukin (IL)-4 and IL-13 up-regulate Monocyte Chemoattractant Protein-1 Expression in Human Bronchial Epithelial Cells: Involvement of p38 Mitogen-activated Protein Kinase, Extracellular Signal-regulated Kinase…
[cited by applicant]
Jou, “Thrombospondin 1 as an Effective Gene Therapeutic Strategy in Collagen-Induced Arthritis”, Arthritis Rheum, vol. 52, 2005, pp. 339-344.
[cited by applicant]
Kachigian—“Collagen antibody-induced arthrisis”, Nature protocols, vol. 1, 2006, pp. 2512-2516.
[cited by applicant]
Kopf, et al., “Averting Inflammation by Targeting the Cytokine Environment,” Nature Reviews, Drug Discovery, 2010, vol. 9, pp. 703-718.
[cited by applicant]
Kudlacz—“The JAK-3 inhibitor CP-690550 is a Potent Anti-inflammatory Agent in a Murine Model of Pulmonary Eosinophilia,” Eur J Pharmaco, 2008, pp. 154-161.
[cited by applicant]
Labadie, et al., “Design and Evaluation Novel 8-0x0-pyridopyrimidine JAK 1/2,” Bioorganic & Medicinal Chemistry Letters, vol. 23, 2013, pp. 5923-5930.
[cited by applicant]
Labadie, et al., “Design and Evaluation Novel 8-0x0-pyridopyrimidine,” JAK1/2, vol. 23, 2013, pp. 5923-5930.
[cited by applicant]
Laurence, et al., “JAK Kinases in Health and Disease: An Update,” Open Rheum. Journal, vol. 6. No. 2:M4, 2012, pp. 232-244.
[cited by applicant]
Laurence, et al., “JAK Kinases in Health and Disease: An Update,” Open Rheumatology Journal, vol. 6 No. 2:M4, 2012, pp. 232-244.
[cited by applicant]
Lee, D. M. and M. E. Weinblatt, “Rheumatoid Arthritis,” The Lancet, vol. 358, No. 9285, 2001, pp. 903-911.
[cited by applicant]
Legendre, “JAK/STAT but Not ERK1/ERK2 Pathway Mediates Interleukin (IL)-6/ Soluble IL-6R Down-regulation of Type II Collagen, Aggrecan Core, and Link Protein Transcription in Articular Chondrocytes”, J Biol Chem., vol. …
[cited by applicant]
Levy, “STAT3 Signaling and the Hyper-IgE Syndrome”, N Engl L Med, vol. 357, 2007, pp. 1655-1658.
[cited by applicant]
Li, “Oncostatin M-Induced Matrix Metalloproteinase and Tissue Inhibitor of Metalloproteinase-3 Genes Expression in Chondrocytes Requires Janus Kinase/STAT Signaling Pathway”, J Immunol, vol. 166, 2001, pp. 3491-3498.
[cited by applicant]
Lin, et al., “Anti-rheumatic Activities of Histone Deacetylase (HOAG) Inhibitors in Vivo in Collagen-induced Arthritis in Rodents,” The British Journal of Pharma., vol. 150, 2007, pp. 862-872.
[cited by applicant]
Lipinski, et al., “Experimental and Computational Approaches to Estimate Solubility and Permeability in Drug Discovery and Development Settings,” Advanced Drug Discovery Reviews, vol. 46, 2001, pp. 3-26.
[cited by applicant]
McGinnity—“Evaluation of Fresh and Cryopreserved Hepatocytes as in Vitro Drug Metabolism Tools for the Prediction of Metabolic Clearance” Drug Metabolism and Disposition, vol. 32, No. 11, 2004, pp. 1247-1253.
[cited by applicant]
Milici, et al., “Cartilage Preservation by Inhibition of Janus Kinase 3 in Two Rodent Models of Rheumatoid Arthritis,” Arthritis Research & Therapy, 2008, 10:R14.
[cited by applicant]
Milici, et al., “Cartilage Preservation by Inhibition of Janus Kinase 3 in Two Rodent Models of Rheumatoid Arthritis,” Arthritis Reserach & Therapy, vol. 10, R14, 2008.
[cited by applicant]
Mullighan—“JAK Mutations in High-risk Childhood Acute Lymphoblastic Leukemia”, PNAS vol. 106, No. 23, 2009, pp. 9414-9418.
[cited by applicant]
Naka, et al., “The Paradigm of IL-6: From Basic Science to Medicine,” Arthritis Res., vol. 4, No. 3, 2002, pp. S233-S242.
[cited by applicant]
Nettekoven, et al.—“Synthetic Access to 2-Amido-5-aryl-8-methoxy-triazolopyridine and 2-Amido-5-morpholino-8 methoxy-triazolopyridine Derivatives as Potential Inhibitors of the Adenosine Receptor Subtypes”, Synthesis, N…
[cited by applicant]
Nials—“Mouse Models of Allergic Asthma: Acute and Chronic Allergen Challenge,” Disease Models & Mechanisms, 2008, pp. 213-220.
[cited by applicant]
Nishida, “Histone Deacetylase Inhibitor Suppression of Autoantibody-Mediated Arthritis in Mice via Regulation of p161NK4a and p21WAF1/Cip1 Expression”, Arthritis Rheum, vol. 50, No. 10, 2004, pp. 3365-3376.
[cited by applicant]
O'Dell, J. R, “Therapeutic Strategies for Rheumatoid Arthritis”, N Engl J Med, vol. 350, No. 25, 2004, pp. 591-25602.
[cited by applicant]
Osaki—“The TATA-containing Core Promoter of the Type II Collagen Gene (COL2A 1) is the Target of Interferon-c-Mediated Inhibition in Human Chondrocytes: Requirement for Stat1a, Jak1 and Jak2”, Biochem J, vol. 369, 2003,…
[cited by applicant]
Oshea—“A New Modality for Immunosuppresion: Targeting the JAK/STAT Pathway”, Nature Rev Drug Disc, vol. 3, 2004, pp. 555-546.
[cited by applicant]
O'Shea, et al., “Cytokine Signaling Modules in Inflammatory Responses,” Immunity, vol. 28, No. 4, 2008, pp. 477-487.
[cited by applicant]
O'Shea, et al., “JAKS and STATs in Immunoregulation and Immune-Mediated Disease,” Immunity, vol. 36, No. 4, 2012, pp. 542-550.
[cited by applicant]
Oste, et al.—“A High Throughput Method of Measuring Bone Architectural Disturbance in a Murine CIA Model by Micro-CT Morphometry”, ECTC Montreal, 2007.
[cited by applicant]
Osullivan, “Cytokine Receptor Signaling Through the Jak-Stat-Socs Pathway in Disease,” Mol Immunology, vol. 44, 2007, pp. 2497-2506.
[cited by applicant]
Otero, “Signalling Pathway Involved in Nitric Oxide Synthase Type II Activation in Chondrocytes: Synergistic Effect pf Leptin with Interleukin-1”, Arthritis Res, vol. 7, 2005, pp. R581-R591.
[cited by applicant]
Pernis, “JAK-STAT Signaling in Asthma”, J. Clin. Invest., vol. 109, 2002, pp. 1279-1283.
[cited by applicant]
Punwani, et al., “Preliminary Clinical Activity of a Topical JAK1/2 Inhibitor in the Treatment of Psoriasis,” J. Am. Acad. Dermatol., vol. 67, No. 4, 2012, pp. 658-664.
[cited by applicant]
Rall, “Rheumatoid Cachexia: Metabolic Abnormalities, Mechanisms and Interventions”, Rheumatology, vol. 43, 2004, pp. 1219-1223.
[cited by applicant]
Rodig , “Disruption of the Jak1 Gene Demonstrates Obligatory and Nonredundant Roles of the Jaks in Cytokine-Induced Biologic Responses”, Cell, vol. 93, 1998, pp. 373-383.
[cited by applicant]
Saharinen, et al., “Regulation of the Jak2 Tyrosine Kinase by Its Pseudokinase Domain,” Molecular and Cellular Biology, vol. 20, No. 10, 2000, pp. 3387-3395.
[cited by applicant]
Salvemini, “Amelioration of Joint Disease in a Rat Model of Collagen-Induced Arthritis by M40403, a Superoxide Dismutase Mimetic”, Arthritis Rheum, vol. 44, No. 12, 2001, pp. 2909-2921.
[cited by applicant]
Seavey, et al., “The Many Faces of Janus Kinase,” Biochemical Pharmacology, vol. 83, 2012, pp. 1136-1145.
[cited by applicant]
Shel Ton, “Nerve Growth Factor Mediates Hyperalgesia and Cachexia in Auto-immune Arthritis”, Pain, vol. 116, 2005, pp. 8-16.
[cited by applicant]
Sims, “Targeting Osteoclasts With Zoledronic Acid Prevents Bone Destruction in Collagen-Induced Arthritis” Arthritis Rheum., vol. 50, No. 7, 2004, pp. 2338-2346.
[cited by applicant]
Smolen JS, Steiner G., “Therapeutic Strategies for Rheumatoid Arthris”, Nat Rev Drug Discov., vol. 2, 2003, pp. 473-488.
[cited by applicant]
SoftFocus SFK Directed Libraries; Library SFK 39, “Serine-Threonine and Tyrosine Kinase directed,” BioFocus DPI, Advertising Article, 2006.
[cited by applicant]
Tam, et al., “Expression Levels of the JAK/STAT Pathway in the Transition from Hormone-sensitive to Hormone-refractory Prostate Cancer”, British Journal of Cancer, vol. 97, 2007, pp. 378-383.
[cited by applicant]
Vainchenker, et al., “JAK2, the JAK2 V617F Mutant and Cytokine Receptors,” Pathol Biol., vol. 55, 2007, pp. 88-91.
[cited by applicant]
Van Vollenhoven, et al., “Tofacitinib or Adalimumab Versus Placebo in Rheumatoid Arthritis,” New England Journal of Medicine, 2012, vol. 367, pp. 508-519.
[cited by applicant]
Verstovsek S., “Therapeutic Potential of JAK2 Inhibitors,” Hematology Am_ Soc. Hematol. Educ. Program, 2009, pp. 636-642.
[cited by applicant]
Walsmith, “Tumor Necrosis Factor-a Production Is Associated with Less Body Cell Mass in Women with Rheumatoid Arthritis”, J Rheumatol., vol. 31, 2004, pp. 23-29.
[cited by applicant]
Wernig, “Efficacy of TG101348, a Selective JAK2 Inhibitor, in Treatment of a Murine Model of JAK2V617F-Induced Polycythemia Vera”, Cancer Cell, vol. 13, No. 4, 2008, pp. 311-320.
[cited by applicant]
Wieland, et al., “Osteoarthritis—An Untreatable Disease?,” Nat Rev Drug Discov., vol. 4, No. 4, 2005, pp. 331-344.
[cited by applicant]
Wirtz, “Mouse Models of Inflammatory Bowel Disease”, Advanced Drug Delivery Reviews, vol. 59, 2007, pp. 1073-1083.
[cited by applicant]
Wirtz, S., et al., “Chemically Induced Mouse Models of Intestinal Inflammation,” Nat. Protocols, vol. 2, 2007, pp. 541-546.
[cited by applicant]
Xiang, “Identification of Somatic JAK1 Mutations in Patients with Acute Myeloid Leukemia”, Blood, vol. 111, 2008, pp. 4809-4812.
[cited by applicant]
Yoshida, et al., “Low Dose CP-690, 550 (tofacitinib, a pan-JAJ inhibitor . . . ,” Biochem & Biophysical Res Commun., vol. 418, 2012, pp. 234-240.
[cited by applicant]
Yu, et al., “Influence of Drug Release Properties of Conventional Solid Dosage Forms on the Systemic Exposure of Highly Soluble Drugs,” MPS Pharmsci, vol. 3, No. 3, 2001, E24.
[cited by applicant]
Zenz, et al., “Psoriasis-like Skin Disease and Arthritis Caused by Inducible Epidermal Deletion of Jun Proteins,” Nature, vol. 437, 2005, pp. 369-375.
[cited by applicant]
Zhang, et al., “Activation of Jak/STAT Proteins Involved in Signal Transduction Pathway Mediated by Receptor for Interleukin 2 in Malignant T Lymphocytes Derived from Cutaneous Anaplastic Large T-cell Lymphoma and Sezar…
[cited by applicant]
Zikherman, et al., “Unraveling the Functional Implications of GWAS: How T Cell Protein Tyrosine Phosphatase Drives Autoimmune Disease,” J Clin Invest., 2011, vol. 121, No. 12, pp. 4618-4621.
[cited by applicant]