US 9220265B2
· Hoekstra et al.
· 2015
[cited by applicant]
JP H0995496A
· 1997
[cited by applicant]
JP 2010517931A
· 2010
[cited by applicant]
JP 2017533923A
· 2017
[cited by applicant]
JP 2017535570A
· 2017
[cited by applicant]
JP 2017536379A
· 2017
[cited by applicant]
JP 2020525426A
· 2020
[cited by applicant]
WO WO2002092553
· 2002
[cited by applicant]
WO WO2004078742
· 2004
[cited by applicant]
WO WO2016022809
· 2016
[cited by applicant]
WO WO2016022827
· 2016
[cited by applicant]
Fini et al. (Archiv der Pharmazie, 320(10), 1014-1019). (Year: 1987).
[cited by examiner]
O'Brien (Polymer Engineering and Science, 29(13), 846-849). (Year: 1989).
[cited by examiner]
Extended EP Search Report for EP21747380.0, mailed Mar. 7, 2024, 5 pages.
[cited by applicant]
Wu et al., Phosphoramidate derivatives of hydroxysteroids as inhibitors of prostate-specific membrane antigen. Bioorganic & Medicinal Chemistry Letters, vol. 18, No. 1, Oct. 30, 2007, pp. 281-284.
[cited by applicant]
International Search Report and Written Opinion for PCT/US2021/015732. Mailed Apr. 15, 2021. 10 pages.
[cited by applicant]
Baldwin et al., Neuroinflammation triggered by ß-glucan/dectin-1 signaling enables CNS axon regeneration. Proc Natl Acad Sci U S A. Feb. 24, 2015;112(8):2581-6.
[cited by applicant]
Berge et al., Pharmaceutical salts. J Pharm Sci. Jan. 1977;66(1):1-19.
[cited by applicant]
Calmus et al., Shaping macrophages function and innate immunity by bile acids: mechanisms and implication in cholestatic liver diseases. Clin Res Hepatol Gastroenterol. Oct. 2014;38(5):550-6.
[cited by applicant]
Colombel et al., Adalimumab for maintenance of clinical response and remission in patients with Crohn's disease: the CHARM trial. Gastroenterology. Jan. 2007;132(1):52-65.
[cited by applicant]
Coskun et al., Novel Targeted Therapies for Inflammatory Bowel Disease. Trends Pharmacol Sci. Feb. 2017;38(2):127-142.
[cited by applicant]
Ferraris et al., Structure-Activity Relationships of Glutamate Carboxypeptidase II (GCPII) Inhibitors. Current Medicinal Chemistry, 2012, 19(9), 1282-1294.
[cited by applicant]
Greene et al., Protective Groups in Organic Synthesis, 3rd ed. John Wiley & Sons. 1999. TOC only. 3 pages.
[cited by applicant]
Hamilton et al., Update on biologic pathways in inflammatory bowel disease and their therapeutic relevance. J Gastroenterol. Jan. 2012;47(1):1-8.
[cited by applicant]
Hanauer et al., Maintenance infliximab for Crohn's disease: the Accent I randomised trial. Lancet. May 4, 2002;359(9317):1541-9.
[cited by applicant]
Hazra et al., Bile acid amides derived from chiral amino alcohols: novel antimicrobials and antifungals. Bioorg Med Chem Lett. Feb. 9, 2004;14(3):773-7.
[cited by applicant]
Ho et al., Obeticholic acid, a synthetic bile acid agonist of the farnesoid X receptor, attenuates experimental autoimmune encephalomyelitis. Proc Natl Acad Sci U S A. Feb. 9, 2016;113(6):1600-5.
[cited by applicant]
Jackson et al., Design and pharmacological activity of phosphinic acid based NAALADase inhibitors. J Med Chem. Nov. 22, 2001;44(24):4170-5.
[cited by applicant]
Jackson et al., Design, synthesis, and biological activity of a potent inhibitor of the neuropeptidase N-acetylated alpha-linked acidic dipeptidase. J Med Chem. Jan. 19, 1996;39(2):619-22.
[cited by applicant]
Kaser et al., Inflammatory bowel disease. Annu Rev Immunol. 2010;28:573-621.
[cited by applicant]
Kozuch et al., Treatment of inflammatory bowel disease: a review of medical therapy. World J Gastroenterol. Jan. 21, 2008;14(3):354-77.
[cited by applicant]
Kuehne et al., Steroidal Dihydro-1,3-Oxazines as Antitumor Agents. J Med Pharm Chem. Mar. 1962;5:281-96.
[cited by applicant]
Kull et al., Mixturs of quaternary ammonium compounds and long- chain fatty acids as antifungal agents. Appl Microbiol. Nov. 1961;9(6):538-41.
[cited by applicant]
Laukens et al., Tauroursodeoxycholic acid inhibits experimental colitis by preventing early intestinal epithelial cell death. Lab Invest. Dec. 2014;94(12):1419-30.
[cited by applicant]
Lawrance. What is left when anti-tumour necrosis factor therapy in inflammatory bowel diseases fails? World J Gastroenterol. Feb. 7, 2014;20(5):1248-58.
[cited by applicant]
Li et al., Synthesis, Anticancer Activities, Antimicrobial Activities and Bioavailability of Berberine-Bile Acid Analogues. Lett. Drug Des. Discov. 2012, 9(6), 573-580.
[cited by applicant]
Mesters et al, Structure of glutamate carboxypeptidase II, a drug target in neuronal damage and prostate cancer. The EMBO Journal. 2006;25,1375-1384.
[cited by applicant]
Mostarda et al., Glucuronidation of bile acids under flow conditions: design of experiments and Koenigs-Knorr reaction optimization. Org Biomol Chem. Dec. 21, 2014;12(47):9592-600.
[cited by applicant]
Nedelcovych et al., Enhanced Brain Delivery of 2-(Phosphonomethyl)pentanedioic Acid Following Intranasal Administration of Its γ-Substituted Ester Prodrugs. Mol Pharm. Oct. 2, 2017;14(10):3248-3257.
[cited by applicant]
Nedelcovych et al., Glutamine Antagonist JHU083 Normalizes Aberrant Glutamate Production and Cognitive Deficits in the EcoHIV Murine Model of HIV-Associated Neurocognitive Disorders. J Neuroimmune Pharmacol. Sep. 2019;1…
[cited by applicant]
Pellicciari et al., Bile acid derivatives as ligands of the farnesoid X receptor. Synthesis, evaluation, and structure-activity relationship of a series of body and side chain modified analogues of chenodeoxycholic acid…
[cited by applicant]
Rais et al., FOLH1/GCPII is elevated in IBD patients, and its inhibition ameliorates murine IBD abnormalities. JCI Insight. Aug. 4, 2016;1(12):e88634. 11 pages.
[cited by applicant]
Regueiro et al., Infliximab dose intensification in Crohn's disease. Inflamm Bowel Dis. Sep. 2007;13(9):1093-9.
[cited by applicant]
Robinson et al., Hydrolysis of the brain dipeptide N-acetyl-L-aspartyl-L-glutamate. Identification and characterization of a novel N-acetylated alpha-linked acidic dipeptidase activity from rat brain. J Biol Chem. Oct. …
[cited by applicant]
Rojas et al., Kinetics and inhibition of glutamate carboxypeptidase II using a microplate assay. Anal Biochem. Nov. 1, 2002;310(1):50-4.
[cited by applicant]
Rubin and Farber, Pathology. J.B. Lippincott Company. 1994. TOC only. 4 pages.
[cited by applicant]
Sartor et al., Mechanisms of disease: pathogenesis of Crohn's disease and ulcerative colitis. Nat Clin Pract Gastroenterol Hepatol. Jul. 2006;3(7):390-407.
[cited by applicant]
Schmidt et al., Predictive value of mucosal TNF-alpha transcripts in steroid-refractory Crohn's disease patients receiving intensive immunosuppressive therapy. Inflamm Bowel Dis. Jan. 2007;13(1):65-70.
[cited by applicant]
Schreiber et al., Maintenance therapy with certolizumab pegol for Crohn's disease. N Engl J Med. Jul. 19, 2007;357(3):239-50.
[cited by applicant]
Sievanen. Exploitation of Bile Acid Transport Systems in Prodrug Design. Molecules, 2007, 12, 1859-1889.
[cited by applicant]
Sipka et al., The immunomodulatory role of bile acids. Int Arch Allergy Immunol. 2014;165(1):1-8.
[cited by applicant]
Slusher et al, Glutamate Carboxypeptidase II. Handbook of Proteolytic Enzymes vol. 2, 2013, pp. 1620-1627.
[cited by applicant]
Strober et al., The fundamental basis of inflammatory bowel disease. J Clin Invest. Mar. 2007;117(3):514-21.
[cited by applicant]
Tang et al., Prostate targeting ligands based on N-acetylated alpha-linked acidic dipeptidase. Biochem Biophys Res Commun. Jul. 18, 2003;307(1):8-14.
[cited by applicant]
Van Assche et al., Progressive multifocal leukoencephalopathy after natalizumab therapy for Crohn's disease. N Engl J Med. Jul. 28, 2005;353(4):362-8.
[cited by applicant]
Vitharana et al., Synthesis and biological evaluation of (R)- and (S)-2-(phosphonomethyl)pentanedioic acids as inhibitors of glutamate carboxypeptidase II., Tetrahedron: Asymmetry., 2002; vol. 13(15), pp. 1609-1614.
[cited by applicant]
Xavier et al., Unravelling the pathogenesis of inflammatory bowel disease. Nature. Jul. 26, 2007;448(7152):427-34.
[cited by applicant]
Yadav et al., Inflammatory bowel disease: exploring gut pathophysiology for novel therapeutic targets. Transl Res. Oct. 2016;176:38-68.
[cited by applicant]