Epizyme, Inc. vs GlaxoSmithKline LLC

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U.S. Patent No. 9,562,041 ("the '041 patent")

U.S. Patent No. 9,956,210 ("the '210 patent")

U.S. Provisional Application No. 61/647,713 ("GSK's Provisional")

File History of the '041 patent Part 1 of 2

PCT Application No. US2013/041115

Communication regarding entity status for Kuntz's Provisional

U.S. Patent Application No. 13/447,007 and inventor declaration ("Kuntz Application") Part 1 of 2

Assignment information for U.S. Patent No. 8,410,088 ("Kuntz Assignment")

Antonysamy, S. et al., Structural context of disease-associated mutations and putative mechanism of autoinhibition revealed by X-ray crystallographic analysis of the EZH2-SET domain. PLoS ONE 8, e84147 (2013)

File History of the '041 patent Part 2 of 2

File History of the '210 patent

U.S. Patent No. 8,410,088 ("Kuntz")

U.S. Provisional Application No. 61/499,595 ("Kuntz's Provisional")

U.S. Patent Application No. 13/447,007 and inventor declaration ("Kuntz Application") Part 2 of 2

Curriculum Vitae of Jonathan L. Sessler ("Sessler CV")

Declaration of Izidore Lossos ("Lossos")

Curriculum Vitae of Izidore Lossos ("Lossos CV")

Verma and Knight, Recent progress in the discovery of small-molecule inhibitors of the HMT EZH2 for the treatment of cancer, Future Med. Chem. 5, 1661-1670 (2013)

Verma et al., Identification of Potent, Selective, Cell-Active Inhibitors of the Histone Lysine Methyltransferase EZH2, ACS Med. Chem. Lett. 3, 1091-1096 (2012)

Ciferri, Molecular architecture of human polycomb repressive complex 2, eLife 1, e00005 (2012)

Jiao, L. & Liu, X., Structural basis of histone H3K27 trimethylation by an active polycomb repressive complex 2. Science 350, aac4383 (2015)

Knutson, S. K. et al., A selective inhibitor of EZH2 blocks H3K27 methylation and kills mutant lymphoma cells. Nat. Chem. Biol. 8, 890-896 (2012)

Brooun A., Gajiwala K., Deng Y et al., Polycomb repressive complex 2 structure with inhibitor reveals a mechanism of activation and drug resistance, Nature Communications 7:11384 (2016)

Wu H. et al., Structure of the Catalytic Domain of EZH2 Reveals Conformational Plasticity in Cofactor and Substrate Binding Sites and Explains Oncogenic Mutations, PLOS ONE 8, e8737 (Dec. 2013)

Qi, W. et al., Selective inhibition of Ezh2 by a small molecule inhibitor blocks tumor cells proliferation. Proc. Natl Acad. Sci. USA 109, 21360-21365 (2012)

Nasveschuk et al., Discovery and Optimization of Tetramethylpiperidinyl Benzamides as Inhibitors of EZH2, ACS Med. Chem. Lett. 5, 378-383 (2014)

Kalinic M, Zloh M, Eric S., Structural insights into binding of small molecule inhibitors to enhancer of zeste homolog 2. J. Comput. Aided Mol. Des. 28, 1109-1128 (2014)

Yang X., Li F., Konze K. et al., Structure-Activity Relationship Studies for Enhancer of Zeste Homologue 2 (EZH2) and EZH1 Inhibitors, J. Med. Chem. 59, 7616-7633 (2016)

Diaz, E. et al., Development and validation of reagents and assays for EZH2 peptide and nucleosome high-throughput screens, J. Biomolecular Screening 17, 1279-1292 (2012)

Brach et al., EZH2 inhibition by Tazemetostat results in altered dependency on B-cell activation signaling in DLBCL, Molecular Cancer Therapeutics 16, 2586-2597 (2017)

U.S. Patent No. 10,478,426 ("the '426 patent")

McCabe, M. T. et al., Mutation of A677 in histonemethyltransferase EZH2in human B-cell lymphoma promotes hypertrimethylation of histone H3 on lysine 27 (H3K27). Proc. Natl Acad. Sci. USA 109, 2989-2994 (2012)

U.S. Pub. No. 2013/0040906

U.S. Pub. No. 2014/0142083

Brana et al., Reaction of N-(2-Pyridylmethyl)-3,5-dimethylbenzamide and N-(3-Pyridylmethyl)-3,5-dimethylbenzamide N-oxides with acetic anhydride, J Heterocyclic Chem. 19, 1297-1300 (1982)

Soumyanarayanan et al., Recently discovered EZH2 and EHMT2 (G9a) inhibitors, Future Med Chem, 8, 1635-1654 (2016)

Miyaura et al., Palladium-catalyzed cross-coupling reactions of organoboron compounds, Chem Rev 95, 2457-2483 (1995)

File History of U.S. Patent No. 8,876,991 (i.e., patent at issue in US Endodontics v. Gold Standard Instruments, PGR2015-00019)

Excerpt from File History of U.S. Patent No. 9,157,017 (i.e., patent at issue in Arkema Inc. v. Honeywell Int'l Inc., PGR2016-00011)

File History of the '426 patent

Declaration of Jonathan L. Sessler ("Sessler")

Petitioner's Power of Attorney

Petition for Inter Partes Review