US 9630968B1
· Lapierre
· 2017
[cited by applicant]
US 20170008904A1
· Crew
· 2017
[cited by applicant]
US 20180072711A1
· Crew
· 2018
[cited by applicant]
US 20180194762A1
· Atallah
· 2018
[cited by applicant]
US 20200121684A1
· Crews
· 2020
[cited by applicant]
US 20200297725A1
· Crews
· 2020
[cited by applicant]
US 20250041429A1
· Lee
· 2025
[cited by applicant]
CN 106459002
· 2017
[cited by applicant]
WO 2002020740A2
· 2002
[cited by applicant]
WO 2014064131A2
· 2014
[cited by applicant]
WO 2014108452A1
· 2014
[cited by applicant]
WO 2016146985A1
· 2016
[cited by applicant]
WO 2016149668A1
· 2016
[cited by applicant]
WO 2016149989A1
· 2016
[cited by applicant]
WO 2016197032A1
· 2016
[cited by applicant]
WO 2016197114A1
· 2016
[cited by applicant]
WO 2017011590A1
· 2017
[cited by applicant]
WO 2017030814A1
· 2017
[cited by applicant]
WO 2017079267A1
· 2017
[cited by applicant]
WO 2017182418A1
· 2017
[cited by applicant]
WO 2017197036A1
· 2017
[cited by applicant]
WO 2017197046A1
· 2017
[cited by applicant]
WO 2017197051A1
· 2017
[cited by applicant]
WO 2017197056A1
· 2017
[cited by applicant]
WO 2017201449A1
· 2017
[cited by applicant]
WO 2017211924A1
· 2017
[cited by applicant]
WO 2018033556A1
· 2018
[cited by applicant]
WO 2018035080A1
· 2018
[cited by applicant]
WO 2018071606A1
· 2018
[cited by applicant]
WO 2018102725A1
· 2018
[cited by applicant]
WO 2018191577A1
· 2018
[cited by applicant]
WO 2018237026A1
· 2018
[cited by applicant]
WO 2019127008A1
· 2019
[cited by applicant]
WO 2019140387A1
· 2019
[cited by applicant]
WO 2019148150A1
· 2019
[cited by applicant]
WO 2019177902A1
· 2019
[cited by applicant]
WO 2019186343A1
· 2019
[cited by applicant]
WO 2019186358A1
· 2019
[cited by applicant]
WO 2019201123
· 2019
[cited by applicant]
WO 2019222101A1
· 2019
[cited by applicant]
WO 2020142228A1
· 2020
[cited by applicant]
WO 2020163823A2
· 2020
[cited by applicant]
WO 2020167518
· 2020
[cited by applicant]
WO 2020198711A1
· 2020
[cited by applicant]
WO 2020201080A1
· 2020
[cited by applicant]
WO 2020239103A1
· 2020
[cited by applicant]
WO 2020263935
· 2020
[cited by applicant]
WO 2021053495
· 2021
[cited by applicant]
WO 2021178920A1
· 2021
[cited by applicant]
WO 2021180103
· 2021
[cited by applicant]
WO 2021219070
· 2021
[cited by applicant]
WO 2022268052
· 2022
[cited by applicant]
WO 2023080732A1
· 2023
[cited by applicant]
Ju, Organic Process Research and Development, 2014, vol. 18(6), pp. 827-830.
[cited by examiner]
Bartlett “Exploiting Chemical Diversity for Drug Discovery” Edited by Paul A Bartlett and Michael Entzeroth, The Royal Society of Chemistry, 2006, pp. 113-118.
[cited by examiner]
“Find ETDs Home » Thesis Resources » Find ETDs” Online: “https://ndltd.org/thesis-resources/find-etds/” Accessed Jan. 31, 2023.
[cited by examiner]
Irwin “ZINC—A Free Database of Commercially Available Compounds for Virtual Screening” J. Chem. Inf. Model. 2005, 45, 177-182.
[cited by examiner]
Kim “PubChem in 2021: new data content and improved web interfaces” Nucleic Acids Research, 2021, vol. 49, Database issue Published online Nov. 5, 2020.
[cited by examiner]
Registry/Zregistry (CAS Registrysm) Sep. 2016 2 pages.
[cited by examiner]
Venkatesh, J. Pharm. Sci. 89, 145-154 (2000) (p. 146, left column).
[cited by examiner]
J. G. Cannon, Chapter Nineteen in Burger's Medicinal Chemistry and Drug Discovery, Fifth Edition, vol. I: Principles and Practice, Wiley-Interscience 1995, pp. 783-802, 784.
[cited by examiner]
Arthur, Explor Target Antitumor Ther. 2020;1:131-52.
[cited by examiner]
Wang, Acta Pharmaceutica Sinica B 2020;10(2):207e238.
[cited by examiner]
[cited by applicant]
Ardley, H.C. et al., “E3 ubiquitin ligases,” Essays Biochemistry, 41:15-30, 2005.
[cited by applicant]
Bradshaw, J. M., “The Src, Syk, and Tec family kinases: distinct types of molecular switches,” Cell Signalling, 22(8):1175-1184, 2010.
[cited by applicant]
Buhimschi, A. D. et al., “Targeting the C481S Ibrutinib-Resistance Mutation in Bruton's Tyrosine Kinase Using PROTAC-Mediated Degradation,” Biochemistry, 57(26):3564-3575, 2018.
[cited by applicant]
Cermakova, K. et al., “Next-Generation Drugs and Probes for Chromatin Biology: From Targeted Protein Degradation to Phase Separation,” Molecules, 23(1958):26 pages, 2018.
[cited by applicant]
Conley, M. E. et al., “Primary B Cell Immunodeficiencies: Comparisons and Contrasts,” Annu. Rev. Immunol., 27:199-227, 2009.
[cited by applicant]
Crews, Craig M. et al., “Inducing Protein Degradation as a Therapeutic Strategy,” 61(2):403-404, 2018.
[cited by applicant]
Defendants' Memorandum in Support of Motion to Dismiss, citation: Civil Action 1:24-cv-08167 filed on Dec. 19, 2024, 37 pages.
[cited by applicant]
Dobrovolsky, D. et al., “Bruton tyrosine kinase degradation as a therapeutic strategy for cancer,” Blood, 133(9):952-961, 2019.
[cited by applicant]
Grice, G. L. et al., “The Proteasome Distinguishes between Heterotypic and Homotypic Lysine-11-Linked Polyubiquitin Chains,” Cell Rep., 12(4):545-553, 2015.
[cited by applicant]
Gurcan, H. M. et al., “A review of the current use of rituximab in autoimmune diseases,” Int. Immunopharmacol., 9:10-25, 2009.
[cited by applicant]
Humphries, L. A. et al., “Tee Kinases Mediate Sustained Calcium Influx via Site-specific Tyrosine Phosphorylation of the Phospholipase C Src Homology 2-Src Homology 3 Linker,” J. Biol. Chem., 279(36): 37651-37661, 2004.
[cited by applicant]
Khan, W. N., “Regulation of B lymphocyte development and activation by Bruton's tyrosine kinase,” Immunol. Res., 23(213):147-156, 2001.
[cited by applicant]
Komander, D. et al., “The Ubiquitin Code,” Annu. Rev. Biochem., 81:203-229, 2012.
[cited by applicant]
Lebraud, H. et al., “Protein degradation: a validated therapeutic strategy with exciting prospects,” Essays Biochem., 61(5):517-527, 2017.
[cited by applicant]
Liu, S. et al., “Targeted selective degradation of Bruton's tyrosine kinase by PROTACs,” Medicinal Chemistry Research, 29:802-808, 2020.
[cited by applicant]
Lochmuller, C. H. et al., “Chromatographic Resolution of Enantiomers,” Journal of Chromatography, 113:283-302, 1975.
[cited by applicant]
Lu, J. et al., “Hijacking the E3 Ubiquitin ligase cereblon to efficiently target BRD4,” Chemistry and Biology, 22(6):755-763, 2015.
[cited by applicant]
Lu, M. et al., “Discovery of a Keap1-dependent peptide PROTAC to knockdown Tau by ubiquitination-proteasome degradation pathway,” European Journal of Medicinal Chemistry, 146:251-259, 2018.
[cited by applicant]
Neklesa, T. K. et al., “Targeted protein degradation by PROTACs,” Pharmacology & Therapeutics, 174:138-144, 2017.
[cited by applicant]
Ottis et al., “Proteolysis-Targeting Chimeras: Induced Protein Degradation as a Therapeutic Strategy,” ACS Chem. Biol., 12(4):892-898, 2017.
[cited by applicant]
Plaintiff AbbVie Inc.'s Opposition to Defendants' Motion to Dismiss, citation: Civil Action 1:24-cv-08167 filed on Jan. 24, 2025, 44 pages.
[cited by applicant]
Sakamoto, Kathleen M., “Chimeric molecules to target proteins for ubiquitination and degradation,” Methods Enzymol., 399:833-847, 2005.
[cited by applicant]
Sakamoto, Kathleen M., “Protacs: chimeric molecules that target proteins to the Skp1-Cullin-F box complex for ubiquitination and degradation,” Proc Natl Acad Sci USA, 98(15):8554-8559, 2001.
[cited by applicant]
Smith, C. I. E. et al., “Expression of Bruton's Agammaglobulinemia Tyrosine Kinase Gene, BTK, Is Selectively Down-Regulated in T Lymphocytes and Plasma Cells,” J. Immunol., 152:557-565, 1994.
[cited by applicant]
Sun, Y. et al., “Degradation of Bruton's tyrosine kinase mutants by PROTAC for potential treatment of ibrutinib-resistant non-Hodgkin lymphomas,” Leukemia, 33:2105-2110, 2019.
[cited by applicant]
Sun, Y et al., “PROTAC-induced BTK degradation as a novel therapy for mutated BTK C481S induced ibrutinib-resistant B-cell malignancies,” Cell Research, 28:779-781, 2018.
[cited by applicant]
Swatek, K. N. et al., “Ubiquitin modifications,” Cell Research, 26(4):399-422, 2016.
[cited by applicant]
Toure, M. et al., “Small-Molecule PROTACS: New Approaches to Protein Degradation,” Angew. Chem. Int. Ed., 55(6):1966-1973, 2016.
[cited by applicant]
Vetrie, D. et al., The gene involved in X-linked agammaglobulinaemia is a member of the src family of protein-tyrosine kinases, Nature, 361:226-233, 1993.
[cited by applicant]
Zhou, P. et al., “Harnessing the ubiquitination machinery to target the degradation of specific cellular proteins,” Mol. Cell., 6(3):751-756, 2000.
[cited by applicant]
Zorba, A. et al., “Delineating the role of cooperativity in the design of potent PROTACs for BTK,” PNAS, 115(31 ):E7285-E7292, 2018.
[cited by applicant]
International Preliminary Report on Patentability issued in International Patent Application No. PCT/CN2022/143837, dated Jul. 11, 2024.
[cited by applicant]
International Search Report issued in International Patent Application No. PCT/CN2022/143837, dated Mar. 8, 2023.
[cited by applicant]
Defendants' reply in support of motion to dismiss, citation: Civil Action No. 1:24-cv-8167, filed Feb. 14, 2025, 27 pages.
[cited by applicant]
Boichenko, I. et al., “Chemical ligand space of cereblon,” ACS Omega, 3:1163-1171, 2018.
[cited by applicant]
Bondenson, D. P. et al., “Lessons in PROTAC design from selective degradation with a promiscuos warhead,” Cell Chemical Biology, 25:15 pages, 2018.
[cited by applicant]
Burslem, G. M. et al., “Efficient synthesis of immunomodulatory drug analogues enables exploration of structure-degradation relationships,” ChemMedChem, 13:1508-1512, 2018.
[cited by applicant]
Caldwell, R. D. et al., “Discovery of Evobrutinib: an oral, potent, and highly selective, covalent Bruton's tyrosine kinase (BTK) inhibitor for the treatment of immunological diseases,” Journal of Medicinal Chemistry, 6…
[cited by applicant]
Casement, R. et al., “Mechanistic and structural features of PROTAC temary complexes,” Chapter 5, Methods in Molecular Biology, 2365:35 pages, 2021.
[cited by applicant]
Crawford, J. J. et al., “Discovery of GDC-0853: a potent, selective, and noncovalent Bruton's tyrosine kinase inhibitor in early clinical development,” Journal of Medicinal Chemistry, 61:2227-2245, 2018.
[cited by applicant]
Cromm, P. M. et al., “Targeted protein degradation: from chemical biology to drug discovery,” Cell Chemical Biology Review, 24:1181-1190, 2017.
[cited by applicant]
Di Paolo, J. A. et al., “Specific Btk inhibition suppresses B cell- and myeloid cell-mediated arthritis,” Nat. Chem. Biol., 7 (1):41-50, 2011.
[cited by applicant]
Feng, Y. et al., “Bruton's tyrosine kinase (BTK) inhibitors in treating cancer: a patent review (2010-2018),” Expert Opinion on Therapeutic Patents, 29(4):217-241, 2019.
[cited by applicant]
Han, X. et al., “Discovery of ARD-69 as a highly potent proteolysis targeting chimera (PROTAC) degrader of androgen receptor (AR) for the treatment of prostate cancer,” J. Med. Chem., 62:941-964, 2019.
[cited by applicant]
Karbo, Robert B., “Protac molecules for the treatment of autoimmune disorders,” ACS Medicinal Chemistry Letters, 10:276-277, 2019.
[cited by applicant]
Kronke, J. et al., “Lenalidomide induces ubiquitination and degradation of CK1alpha in del (95q) MDS,” Nature, 523:20 pages, 2015.
[cited by applicant]
Li, X. et al., “A patent review of the ubiquitin ligase system: 2015-2018,” Expert Opinion on Therapeutic Patents, 28 (12):919-937, 2018.
[cited by applicant]
Min, J. et al., “Phenyl-glutarimides: Alternative cereblon binders for the design of PROTACs,” Angewandte Chemie, 60:26633-26670, 2021.
[cited by applicant]
Moon, S. et al., “Chemically induced cellular proteolysis: an emerging therapeutic strategy for undruggable targets,” Molecules and Cells, 41(11):933-942, 2018.
[cited by applicant]
Nowak, R. P. et al., “Plasticity in binding confers selectivity in ligand-induced protein degradation,” Nature chemical biology, 14:706-714, 2018.
[cited by applicant]
Raina, K. et al., “Targeted protein knockdown using small molecule degraders,” Current Opinion in Chemical Biology, 39:46-53, 2017.
[cited by applicant]
Rankin, A. L et al., “Selective inhibition of BTK prevents murine lupus and antibody-mediated glomerulonephritis,” The Journal of Immunology, 191(9):4540-4550, 2013.
[cited by applicant]
Sainan, A. et al., “Small-molecule PROTACs: An emerging and promising approach for the development of targeted therapy drugs”, EBioMedicine, 36:552-562, 2018.
[cited by applicant]
Shi, Q. et al., “Purine derivatives as potent Bruton's tyrosine kinase (BTK) inhibitors for autoimmune diseases,” Bioorganic and Medicinal Chemistry Letters, 24:2206-2211, 2014.
[cited by applicant]
Tasso, B. et al., “The development of BTK inhibitors: a five-year update,” Molecules, 26:1-31, 2021.
[cited by applicant]
Tinworth, C. P. et al., “PROTAC-mediated degradation of Bruton's tyrosine kinase is inhibited by covalent binding”; ACS Chemical Biology, 14(3):342-347, 2019.
[cited by applicant]
Troup, R. I. et al., “Current strategies for the design of PROTAC linkers: a critical review,” Exploration of Targerted Anti-tumor Therapy, 1:273-312, 2020.
[cited by applicant]
Weng, G. et al., “PROTAC-DB: an online database of PROTACs,” Nucleic Acids Research, 49:D1381-D1387, 2021.
[cited by applicant]
Winter, G. E. et al., “Phthalimide conjugation as a strategy for in vivo target protein degradation,” Science, 348 (6241): 1376-1381, 2015.
[cited by applicant]
Woodhead, Steve, Presentation: “Structure Guided Design and Optimization of Selective Kinase Inhibitors from Fragment Starting Points,” Takeda California, 33 pages, Apr. 14, 2016.
[cited by applicant]
Zhou, B. et al., “Discovery of a small-molecule degrader of bromodomain and extra-terminal (BET) proteins with picomolar cellular potencies and capable of achieving tumor regression,” Journal of Medicinal Chemistry, 61:…
[cited by applicant]