Ajinomoto Co., Inc. v. AbTis Co., Ltd. - IPR2025-00283

Petitioner’s Opposition to Patent Owner’s Motion to Amend

Tumey et al., Site Selection: a Case Study in the Identification of Optimal Cysteine Engineered Antibody Drug Conjugates, AAPS JOURNAL, 2017, 19(4):1123- 1135

Tumey et al., Optimization of Tubulysin Antibody–Drug Conjugates: A Case Study in Addressing ADC Metabolism, ACS MEDICINAL CHEMISTRY LETTERS, 2016, 7(11): 977-982

Graziani et al., PF-06804103, A Site-specific Anti-HER2 Antibody–Drug Conjugate for the Treatment of HER2- expressing Breast, Gastric, and Lung Cancers, MOLECULAR CANCER THERAPEUTICS, 2020, 19, 10, 2068-2078

Sadiki et al., Site-specific conjugation of native antibodies, ANTIBODY THERAPEUTICS, 2020, 3(4):271- 284

Chau et al., Antibody–drug conjugates for cancer, THE LANCET, 2019, 394(10200): 793-804

Trail et al., Antibody drug conjugates for treatment of breast cancer: Novel targets and diverse approaches in ADC design, PHARMACOLOGY & THERAPEUTICS, 2018, 181: 126-142

Benjamin et al., Thiolation of Q295: Site-Specific Conjugation of Hydrophobic Payloads without the Need for Genetic Engineering, MOLECULAR PHARMACEUTICS, 2019, 16(6): 2795-2807

Lyon et al., Reducing hydrophobicity of homogeneous antibody-drug conjugates improves pharmacokinetics and therapeutic index, NATURE BIOTECHNOLOGY, 2015, 33: 733-735

Staudacher & Brown, Antibody drug conjugates and bystander killing: is antigen-dependent internalisation required?, BRITISH JOURNAL OF CANCER, 2017, 117: 1736-1742

Pickens et al., Practical Considerations, Challenges, and Limitations of Bioconjugation via Azide–Alkyne Cycloaddition, BIOCONJUGATE CHEMISTRY, 2017, 29(3): 686-701

Lyon et al., Self-hydrolyzing maleimides improve the stability and pharmacological properties of antibodydrug conjugates, NATURE BIOTECHNOLOGY, 2014, 32: 1059-1062

Jain et al., Current ADC Linker Chemistry, PHARMACEUTICAL RESEARCH, 2015, 32: 3526-3540

Knight et al., Synthesis and evaluation of an 18Flabaelled norbornene derivative for copper-free click chemistry reaction, ORGANIC & BIOMOLECULAR CHEMISTRY, 2013, 11: 3817-3825

Oller-Salvia et al., Rapid and Efficient Generation of Stable Antibody–Drug Conjugates via an Encoded Cyclopropene and an Inverse‐Electron‐Demand Diels–Alder Reaction, ANGEW CHEM INT ED ENGL., 2018, 57(11): 2831-2834

Oliveira et al., Inverse electron demand Diels–Alder reactions in chemical biology, CHEMICAL SOCIETY REVIEWS, 2017, 46(16): 4895-4950

Chalker et al., Methods for converting cysteine to dehydroalanine on peptides and proteins, CHEMICAL SCIENCE, 2011, 2: 1666-1676

Kirmse et al., Destabilisierte 2-Norbornyl-Kationen, ANGEWANDTE CHEMIE, 1985, 97(1): 51-52

Mullapudi et al., Resin-Supported Site-Specific Antibody Conjugation Method Leads to Antibody-Drug Conjugates with Retained Efficacy and Improved Stability, BIOCONJUGATE CHEMISTRY, 2025, 36: 1956- 1969

Second Declaration of Dr. Lawrence Nathan Tumey

Deposition Transcript of Dr. Zhaohui Sunny Zhou

Petitioner’s Updated Exhibit List

Petitioner’s Notice of Deposition of Zhaohui Sunny Zhou, PH.D.

Patent Owner's Non-Contingent Motion to Amend Under 37 C.F.R. § 42.121

Ex. 2002 - U.S. Patent App. No. 18/154,998

Ex. 2003 - U.S. Patent App. No. 16/980,503

Ex. 2004 - Declaration of Dr. Zhaohui Sunny Zhou

Ex. 2005 - Curriculum Vitae of Dr. Zhaohui Sunny Zhou

Ex. 2006 - Deposition Transcript of Dr. Tumey

Patent Owner's Updated Mandatory Notices

Patent Owner's Notice of Remote Deposition of Dr. Lawrence N. Tumey

ORDER Granting-in-Part and Denying-in-Part Patent Owner’s Motion for Withdrawal and Substitution of Counsel 37 C.F.R. § 42.10

Petitioner's Updated Mandatory Notices

General Order: Related Matters Updates

EXPUNGED

EXPUNGED

Institution Decision: Grant

Order: Scheduling Order

Director Discretionary Decision: Refer

Opposition to Patent Owner’s Argument for Discretionary Denial

Patent Owner's Motion for Withdrawal and Substitution of Counsel

Patent Owner's Updated Mandatory Notices

Patent Owner's Argument for Discretionary Denial

Ex. 2001 - Statutory Disclaimer of U.S. Patent No. 11,896,675

Patent Owner's Preliminary Response

Notice: Extending Deadline for Discretion Briefing

Patent Owner's Updated Power of Attorney

Patent Owner's Updated Mandatory Notices

NOTICE OF FILING DATE ACCORDED TO PETITION AND TIME FOR FILING PATENT OWNER PRELIMINARY RESPONSE

Notice: Mandatory Notice

U.S. Patent No. 11,896,675 (the ’675 patent)

Yamada et al., Dev. a Novel Chemical Site-Specific Conjugation Poster

Okuzumi, Technology of Site Specific Conjugation (PepTalk Presentation)

WO 2018/199337 (Yamada)

WO 2019/240288 (Matsuda)

Clarivate Analytics, PepTalk 2019 - CHI's 18th Annual Meeting

PepTalk 2019 Conference Program

Croasdell, 18th Annual PepTalk: DRUGS OF THE FUTURE

Photographs from Luncheon Presentation

Photographs from Poster Presentation

Email exch. with Dr. Igor D'Angelo providing copy of PepTalk Presentation

Email exch. Dr. Bernhard Valldorf providing a copy of PepTalk Presentation

Email exch. Dr. Michael Szardenings providing copy of PepTalk Presentation

Email exchange with Susan Lee providing a copy of PepTalk Presentation

Email exch. Professor Rolf G. Werner providing copy of PepTalk Presentation

LinkedIn profile of Dr. Igor D'Angelo

LinkedIn profile of Dr. Bernhard Valldorf

LinkedIn profile of Dr. Michael Szardenings

LinkedIn profile of Susan Lee

Lambert and Berkenblit, Antibody–Drug Conjugates for Cancer Treatment

Birrer et al. Antibody-Drug Conjugate-Based Therap.: State of the Science

Schumacher et al., Current Status: Site-Specific Antibody Drug Conjugates

Nejadmoghaddam et al. Antibody-Drug Conjugates Possibilities and Challenges

9th Annual World ADC Conference Program, November 12-15, 2018

Mendelsohn, Technology of Site Specific Conjugation for Next Generation ADC

Oxford English Dictionary definition of “terminal”

Tam et al. Functional, Biophysical and Structural Characterization of Human

Lu et al. Beyond binding antibody effector functions in infectious diseases

Prosecution History for U.S. Patent No. 11,896,675 (the ’675 patent)

Amblard et al. The CuI-catalyzed Huisgen 1,3-dipolar cycloaddition of azide

U.S. 2023/0158167 U.S. pre-grant publication of U.S. Application 16/980,503

WO 2020/184944

U.S. 2023/0158167 (U.S. National Stage of WO 2020/184944)

Declaration of Dr. Tatsuya Okuzumi

Japanese Patent Application No. 2018-113962

Petitioner's Power of Attorney

Declaration of Dr. Lawrence Nathan Tumey

U.S. 2020/0190165 (U.S. National Stage of Yamada)

U.S. 2021/0139541 (U.S. National Stage of Matsuda)

Verified English Translation of Japanese Pat. App. No. 2018-113962

Verified English translation of application US Ser. No. 62/815,557

Petition For Inter Partes Review