US 6500854B1
· Kitamura et al.
· 2002
[cited by applicant]
US 8088764B2
· Menet et al.
· 2012
[cited by applicant]
US 8242274B2
· Menet et al.
· 2012
[cited by applicant]
US 8563545B2
· Menet et al.
· 2013
[cited by applicant]
US 8853240B2
· Menet et al.
· 2014
[cited by applicant]
US 8999979B2
· Menet et al.
· 2015
[cited by applicant]
US 9284311B2
· van 't Klooster et al.
· 2016
[cited by applicant]
US 9309244B2
· Menet et al.
· 2016
[cited by applicant]
US 9382247B2
· Sabourault et al.
· 2016
[cited by applicant]
US 9415037B2
· Menet et al.
· 2016
[cited by applicant]
US 9707237B2
· Menet et al.
· 2017
[cited by applicant]
US 20050222171A1
· Bold et al.
· 2005
[cited by applicant]
US 20130310340A1
· Payan et al.
· 2013
[cited by applicant]
US 20170173034A1
· Di Paolo
· 2017
[cited by applicant]
US 20180263997A1
· Alonzo et al.
· 2018
[cited by applicant]
EP 1391211A1
· 2004
[cited by applicant]
EP 2305673A1
· 2011
[cited by applicant]
EP 2445911A1
· 2012
[cited by applicant]
EP 2778159A1
· 2014
[cited by applicant]
JP 2011529032A
· 2011
[cited by applicant]
JP 2012530766A
· 2012
[cited by applicant]
JP 2013049632A
· 2013
[cited by applicant]
WO 2003010167A1
· 2003
[cited by applicant]
WO 2004039816A1
· 2004
[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 2010013768A1
· 2010
[cited by applicant]
WO 2010141796A2
· 2010
[cited by applicant]
WO 2010149769A1
· 2010
[cited by applicant]
WO 2010149771A1
· 2010
[cited by applicant]
WO 2013069297A1
· 2013
[cited by applicant]
WO 2013189771A1
· 2013
[cited by applicant]
WO 2015117980A1
· 2015
[cited by applicant]
WO 2016165953A1
· 2016
[cited by applicant]
WO 2019224283A1
· 2019
[cited by applicant]
Bastin R J: “Salt selection and optimisation procedures for pharmaceutical new chemical entities.” Organic Process Research & Development, 4 (5), 2000, pp. 427-435.
[cited by applicant]
Argiles et al., “Catabolic proinflammatory cytokines,” Curr. Opin. Clin. Nutr. Metab. Care, vol. 1, pp. 245-251 (1998).
[cited by applicant]
Bain et al., “The specificities of protein kinase inhibitors: an update,” Biochem. J., 371, pp. 199-204 (2003).
[cited by applicant]
Berge et al., “Pharmaceutical Salts,” Journal of Pharmaceutical Sciences, vol. 66, No. 1, pp. 1-19 (1977).
[cited by applicant]
Berishaj et al., “Stat3 istyrosine-phosphorylated through the interleukin-6/glycoprotein 130/Janus kinase pathway in breast cancer,” Breast Cancer Res., vol. 9(3), R32 (2007).
[cited by applicant]
Bundgard, “Prodrugs as a means to improve the delivery of peptide drugs,” Adv. Drug Del. Rev., vol. 8, pp. 1-38 (1992).
[cited by applicant]
Bush et al., “Reduction of joint inflammation and bone erosion in rat adjuvant arthritis by treatment with interleukin-17 receptor IgGI Fe fusion protein,” Arthritis Rheum., vol. 46, pp. 802-805 (2002).
[cited by applicant]
Changelian et al., “The specificity of JAK3 kinase inhibitors,” Blood, vol. 111, pp. 2155-2157 (2008).
[cited by applicant]
Chen et al., “Janus Kinase Deregulation in Leukemia and Lymphoma,” Immunity, vol. 36, pp. 529-541 (2012).
[cited by applicant]
Chmp, Guideline on Clinical Investigation of Medicinal Products indicated for the treatment of Psoriasis (2004).
[cited by applicant]
Choy et al., “Cytokine Pathways and Joint Inflammation in Rheumatoid Arthritis,” N. Engl. J. Med., vol. 344, pp. 907-916 (2001).
[cited by applicant]
Chubinskaya et al., “Regulation of osteogenic proteins by chondrocytes,” Int'l J. of Biochem. & Cell Bio., vol. 35, pp. 1323-1340 (2003).
[cited by applicant]
Clegg et al., “Glucosamine, Chondroitin Sulfate, and the Two in combination for Painful Knee Osteoarthritis,” N. Engl. J. Med., vol. 354, No. 8, pp. 795-808 (2006).
[cited by applicant]
Constantinescu et al., “Mining for JAK-STAT mutations in cancer,” Trends in Biochem. Sci., vol. 33, No. 3, pp. 122-131 (2008).
[cited by applicant]
Dolgin, “Companies hope for kinase inhibitor JAKpot,” Nature Reviews Drug Discovery, vol. 10, pp. 717-718 (2011).
[cited by applicant]
Drug Discovery and Development, Understanding The R&D Process, Pharmaceutical Research and Manufacturers of America, pp. 1-14 (2007).
[cited by applicant]
Dymock, “Recent News in the Fast-Paced Field of JAK Inhibitors,” J. Develop. Drugs, vol. 2, No. 2, pp. 1-2 (2013).
[cited by applicant]
Fabian et al., “A small molecule-kinase interaction map for clinical kinase inhibitors,” Nature Biotech., vol. 23, No. 3, pp. 329-336 (2005).
[cited by applicant]
Firestein, “Evolving concepts of rheumatoid arthritis,” Nature, vol. 423, pp. 356-361 (2003).
[cited by applicant]
Geron et al., “Selective inhibition of JAK2-driven erythroid diffferentiation of polycythemia . . . ,” Cancer Cell, vol. 13, No. 4, pp. 321-330 (2008).
[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, pp. 213-224 (2008).
[cited by applicant]
Ip, et al., “Interleukin (IL)-4 and IL-13 up-regulate monocyte chemoattractant protein-1 . . . ,” British Society for Immunology: Clinical and Experimental Immunology, vol. 145, pp. 162-172 (2006).
[cited by applicant]
Jou et al., “Thrombospondin 1 as an effective gene therapeutic strategy in collagen-induced arthritis,” Arthritis & Rheum, vol. 1, pp. 339-344 (2005).
[cited by applicant]
Kachigian, “Collagen antibody-induced arthritis,” Nature Protocols, vol. 1, No. 5, pp. 2512-2516 (2006).
[cited by applicant]
Kopf et al., “Averting inflammation by targeting the cytokine environment,” Nature Reviews, Drug Discovery, vol. 9, pp. 703-718 (2010).
[cited by applicant]
Kudlacz et al., “The JAK-3 inhibitor CP-690550 is a potent anti-inflammatory agent in a murine model of pulmonary eosinophilia,” Eur. J. Pharmaco., vol. 582, pp. 154-161 (2008).
[cited by applicant]
Labadie et al., “Design and evaluation novel 8-0x0- pyridopyrimidine JAK 1/2,” Bioorganic & Medicinal Chemistry Letters, vol. 23, pp. 5923-5930 (2013).
[cited by applicant]
Laurence et al., “JAK Kinases in Health and Disease: An Update,” Open Rheum. J., vol. 6, Suppl. 2, pp. 232-244 (2012).
[cited by applicant]
Lee et al., “Rheumatoid Arthritis,” Lancet, vol. 358, pp. 903-911 (2001).
[cited by applicant]
Legendre et al., “JAK/STAT but not ERK1/ERK2 pathway mediates interleuking . . . ,” J. Biol. Chem., vol. 278, No. 5, pp. 2903-2912 (2003).
[cited by applicant]
Levy et al., “STAT3 Signaling and the Hyper-IgE Syndrome,” N. Engl. J. Med., vol. 357, pp. 1655-1658 (2007).
[cited by applicant]
Li et al., “Oncostatin M-induced matrix metalloproteinase and tissue inhibitor of . . . ,” J. of Immun., vol. 166, pp. 3491-3498 (2001).
[cited by applicant]
Lin et al., “Anti-rheumatic activities of histone deacetylase (HDAC) inhibitors in vivo in collagen-induced arthritis in rodents,” The British J. of Pharma., vol. 150, pp. 862-872 (2007).
[cited by applicant]
Lipinski et al., “Experimental and computational approaches to estimate solubility and permeability in drug discovery and development settings,” Adv. Drug Discovery Reviews, vol. 46, pp. 3-26 (2001).
[cited by applicant]
McGinnity et al., “Evaluation of fresh and cryopreserved hepatocytes as in vitro drug metabolism tools for the prediction of metabolic clearance,” Drug Metab Disp., vol. 32, No. 11, pp. 1247-1253 (2004).
[cited by applicant]
Milici et al., “Cartilage preservation by inhibition of Janus Kinase 3 in two rodent models of rheumatoid arthritis,” Arthritis Research & Therapy, vol. 10, pp. R14 (2008).
[cited by applicant]
Mullighan et al., “JAK mutations in high-risk childhood acute lymphoblastic leukemia,” PNAS, vol. 106, No. 23, pp. 9414-9418 (2009).
[cited by applicant]
Naka et al., “The paradigm of IL-6: from basic science to medicine,” Arthritis Res., vol. 4, Supp. 3, pp. S233-S242 (2002).
[cited by applicant]
Nettekoven et al., “Synthetic Access to 2-Amido . . . ,” Synthesis, vol. 11, pp. 1649-1652 (2003).
[cited by applicant]
Nials et al., “Mouse Models of Allergic Asthma: Acute and Chronic Allergen Challenge,” Disease Models & Mechanisms, vol. 1, pp. 213-220 (2008).
[cited by applicant]
Nishida et al., “Histone Deacetylase Inhibitor Suppression . . . ,” Arthritis & Rheum., vol. 50, pp. 3365-3376 (2004).
[cited by applicant]
O'Dell, “Therapeutic Strategies for Rheumatoid Arthritis,” N. Engl. J. Med., vol. 350, pp. 2591-2602 (2004).
[cited by applicant]
Osaki et al., “The TAT A-containing core promoter of the type II collagen gene . . . ,” Biochem J., vol. 369, pp. 103-115 (2003).
[cited by applicant]
O'Shea et al., “Cytokine signaling modules in inflammatory responses,” Immunity, vol. 28, No. 4, pp. 477-487 (2008).
[cited by applicant]
O'Shea et al., “JAKS and STATs in Immunoregulation and Immune-Mediated Disease,” Immunity, vol. 36, No. 4, pp. 542-550 (2012).
[cited by applicant]
O'Shea et al., “A New Modality for Immunosuppression: Targeting the Jak/Stat Pathway,” Nature Reviews, vol. 3, pp. 555-564 (2004).
[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]
O'Sullivan et al., “Cytokine receptor signaling through the Jak-Stat-Socs pathway in disease,” Molecular Immunology, vol. 44, pp. 2497-2506 (2007).
[cited by applicant]
Otero et al., “Signaling pathway involved in nitric oxide synthase type II . . . ,” Arthritis Research & Therapy, vol. 7, No. 3, pp. 581-591 (2005).
[cited by applicant]
Pernis et al., “JAK-STAT signaling in asthma,” J. Clin. Invest., vol. 109, pp. 1279-1283 (2002).
[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, pp. 658-664 (2012).
[cited by applicant]
Rail et al., “Rheumatoid cachexia: metabolic abnormalities, mechanisms and interventions,” Rheumatology, vol. 43, No. 10, pp. 1219-1223 (2004).
[cited by applicant]
Rodig et al., “Disruption of the Jak1 gene demonstrates,” Cell, vol. 93, pp. 373-383 (1998).
[cited by applicant]
Saharinen et al., “Regulation of the Jak2 Tyrosine Kinase by Its Pseudokinase Domain,” Molecular and Cellular Biology, vol. 20, No. 10, pp. 3387-3395 (2000).
[cited by applicant]
Salvemini et al., “Amelioration of Joint Disease in a Rat Model of Collagen-induced Arthritis . . . ,” Arthritis & Rheum., vol. 44, No. 12, pp. 2909-2921 (2001).
[cited by applicant]
Seavey et al., “The many faces of Janus kinase,” Biochemical Pharmacology, vol. 83, pp. 1136-1145 (2012).
[cited by applicant]
Shelton et al., “Nerve growth factor mediates hyperalgesia and cachexia in auto-immune arthritis,” Pain, vol. 116, pp. 8-16 (2005).
[cited by applicant]
Sims et al., “Targeting Osteoclasts with Zoledronic Acid prevents Bone Destruction in Collagen-Induced Arthritis,” Arthritis & Rheumatism, vol. 50, No. 7, pp. 2338-2346 (2004).
[cited by applicant]
Smolen et al., “Therapeutic strategies for rheumatoid arthritis,” Nat. Rev. Drug Discov., vol. 2, No. 6, pp. 473-488 (2003).
[cited by applicant]
Softfocus SKF Directed Libraries; Library SFK 39, “Serine-Threonine and Tyrosine Kinase directed”, BioFocus DPI, Advertising Article (2006).
[cited by applicant]
Stahl et al., eds., “Handbook of pharmaceutical salts,” Properties, selection and use, Wiley-VCH, pp. 265-327 (2008).
[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 J. of Cancer, vol. 97, pp. 378-383 (2007).
[cited by applicant]
Vainchenker et al., “JAKs in pathology: Role of Janus kinases in hematopoietic malignancies and immunodeficiencies,” Seminars in Cell & Developmental Biology, vol. 19, pp. 385-393 (2008).
[cited by applicant]
Vainchenker et al., “JAK2, the JAK2 V617F mutant and cytokine receptors,” Pathol. Biol., vol. 55, pp. 88-91 (2007).
[cited by applicant]
Van Vollenhoven et al., “Tofacitinib or Adalimumab versus Placebo in Rheumatoid Arthritis,” New Engl. J. Med., vol. 367, pp. 508-519 (2012).
[cited by applicant]
Verstovsek, “Therapeutic potential of JAK2 inhibitors,” Hematology Am. Soc. Hematol. Educ. Program, pp. 636-642 (2009).
[cited by applicant]
Walsmith et al., “Tumor Necrosis Factor-alpha Production is associated with less body cell mass . . . ,” J. of Rheum., vol. 31, pp. 23-29 (2004).
[cited by applicant]
Wernig, et al., “Efficacy of TG1 01348, a selective JAK2 inhibitor, in treatment of a murine . . . ,” Cancer Cell, vol. 13, No. 4, pp. 311-320 (2008).
[cited by applicant]
Wieland et al., “Osteoarthritis-an untreatable disease,” Nat. Rev. Drug Discov., vol. 4, pp. 331-344 (2005).
[cited by applicant]
Wirtz et al., “Mouse models of inflammatory bowel disease,” Adv. Drug Delivery Reviews, vol. 59, No. 11, pp. 1073-1083 (2007).
[cited by applicant]
Xiang et al., “Identification of somatic JAK1 mutations in patients with acute myeloid leukemia,” Blood, vol. 111, pp. 4809-4812 (2008).
[cited by applicant]
Yoshida et al., “Low dose CP-690,550 (tofacitinib, a pan-JAK inhibitor . . . ,” Biochem. & Biophysical Res. Commun., vol. 418, pp. 234-240 (2012).
[cited by applicant]
Yu et al., “Influence of drug release properties of conventional solid dosage forms on the systemic exposure of highly soluble drugs,” AAPS PharmSci, vol. 3, No. 3, pp. 86-92 (2001).
[cited by applicant]
Zenz et al., “Psoriasis-like skin disease and arthritis caused by inducible epidermal deletion of Jun proteins,” Nature, vol. 437, pp. 369-375 (2005).
[cited by applicant]
Zhang et al., “Activation of Jak/ST AT 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., vol. 121, No. 12, pp. 4618-4621 (2011).
[cited by applicant]
Foreign Priority Document GB1402071.3, filed Feb. 7, 2014.
[cited by applicant]
Communication pursuant to Article 94(3) EPC received in Application No. 19 726 950.9-1109 dated May 29, 2024, 5 pages.
[cited by applicant]
Communication received in Australian Application No. 2019273664 dated Mar. 14, 2024, 3 pages.
[cited by applicant]
Mease et al., “Efficacy and safety of filgotinib, a selective Janus kinase 1 inhibitor, in patients with active psoriatic arthritis (Equator): results from a randomised, placebo-controlled, phase 2 trial,” XP-002793289,…
[cited by applicant]
Mease et al., “Filgotinib, an Oral, Selective Janus Kinase 1 Inhibitor, Is Effective in Psoriatic Arthritis Patients with an Inadequate Response to Conventional Disease-Modifying Anti-Rheumatic Drugs: Results from a Ran…
[cited by applicant]
Mease et al., “Tofacitinib or Adalimumab versus Placebo for Psoriatic Arthritis,” The New England Journal of Medicine, Oct. 19, 2017, 14 pages.
[cited by applicant]
Office Action received in Chinese Application No. 201980034599.1 dated Jul. 21, 2023, with translation, 9 pages.
[cited by applicant]
Office Action received in Chinese Application No. 201980034599.1 dated May 8, 2024, with translation, 7 pages.
[cited by applicant]
Office Action received in Japanese Application No. 2020-565417 dated Apr. 25, 2023, with translation 8 pages.
[cited by applicant]
Office Action received in Japanese Application No. 2020-565417 dated Oct. 17, 2023, with translation, 4 pages.
[cited by applicant]
Office Action received in U.S. Appl. No. 17/057,946 dated Aug. 24, 2023, 13 pages.
[cited by applicant]
Office Action received in U.S. Appl. No. 17/057,946 dated Mar. 18, 2024, 15 pages.
[cited by applicant]
Robin-Jagerschmidt et al., “The JAK1 Selective Inhibitor Filgotinib Regulates Both Enthesis and Colon Inflammation in a Mouse Model of Psoriatic Arthritis,” Scientific Abstracts, Jun. 15, 2017, 2 pages.
[cited by applicant]
Search Report and Written Opinion received in International Application No. PCT/EP2019/063283 dated Aug. 22, 2019, with 13 pages.
[cited by applicant]