Conjupro Biotherapeutics, Inc. et al. vs Ascletis Pharma China Co. Ltd. - PGR2025-00057

Patent Owner's Updated Mandatory Notices Under 37 C.F.R. § 42.8

Patent Owner's Preliminary Response

Patent Owner's Updated Exhibit List

Guang Huang et al., Applications of Oxetanes in Drug Discovery and Medicinal Chemistry, European Journal of Medicinal Chemistry (2023), 261

Juan J. Rojas and James A. Bull, Oxetanes in Drug Discovery Campaigns, Journal of Medicinal Chemistry (2023), 66 , 12697-12709

Jonas Boström et al., Oxadiazoles in Medicinal Chemistry, Journal of Medicinal Chemistry (2011), 55, 1817-1830

Yijing Li et al., Thiadiazole—a Promising Structure in Medicinal Chemistry, ChemMedChem (2013), 27-41

Bethany R. Shire and Edward A. Anderson, Conquering the Synthesis and Functionalization of Bicyclo[1.1.1]pentanes, An Open Access Journal of the American Chemical Society (2023), 3, 1539-1553

Edon Vitaku, et al, Analysis of the Structural Diversity, Substitution Patterns, and Frequency of Nitrogen Heterocycles among U.S. FDA Approved Pharmaceuticals, Journal of Medicinal Chemistry (2014), 57, 10257-10274

Marcelo D. Polêto et al., Aromatic Rings Commonly Used in Medicinal Chemistry: Force Fields Comparison and Interactions With Water Toward the Design of New Chemical Entities, Frontiers in Pharmacology (2018), 9, 1-20

Aimee K. Clarke and William P. Unsworth, A happy medium: the synthesis of medicinally important medium-sized rings via ring expansion, The Royal Society of Chemistry (2020), 11, 2876-2881

Alexander S. Harmata, et al., Bridged bicyclic building block upgrading: Photochemical synthesis of bicyclo[3.1.1]heptan-1-amines, Willard Henry Dow Laboratory, Dept. of Chemistry, Univ. of Michigan

Jang Won Son and Soo Lim, Glucagon-Like Peptide-1 Based Therapies: A New Horizon in Obesity Management, Endocrinology and Metabolism (2024), 39, 206-221

Sean Wharton, M.D. et al., Daily Oral GLP-1 Receptor Agonist Orforglipron for Adults with Obesity, The New England Journal of Medicine (2023), 389, 877-888

A Study of Orforlipron (LY3502970) in Adult Participants with Obesity or Overweight With Weight-Related Comorbidities (ATTAIN-1), Lilly Trials

International Publication No. WO 2024/169952 A1

International Publication No. WO 2023/016546 A1

International Publication No. WO 2024/153070 A1

Ascletis Presented Results from Cohorts 1 and 2 of 28-day Multiple Ascending Dose Study of Its Oral Small Molecule GLP-1R Agonist ASC30 at the 61st European Association for the Study of Diabetes (EASD) Annual Meeting, Ascletis

Jinzi Jason Wu and Vanessa Wang, Poster number: 750-P, ASC30, an Oral GLP-1R Biased Small Molecule Agonist in Participants with Obesity -A First-in-Human Single Ascending Dose Study, (June 20, 2025)

Compound Summary for CID 8028, Tetrahydrofuran, National Center for Biotechnology Information, PubChem

Compound Summary for CID 9253, Cyclopentane, National Center for Biotechnology Information, PubChem

Arun K Ghosh and David D Anderson, Tetrahydrofuran, Tetrahydropyran, Triazoles and Related Heterocyclic Derivatives as Hiv Protease Inhibitors, Future Med Chem. (2011), 3, 1181-1197

Seung-Hwa Kwak et al., Evaluation of Manassantin A Tetrahydrofuran Core Region Analogues and Cooperative Therapeutic Effects with EGFR Inhibition, Journal of Medicinal Chemistry (2020), 63, 6821-6833

Pedro de Sena Murteira Pinheiro, Lucas Silva Franco and Carlos Alberto Manssour Fraga, The Magic Methyl and Its Tricks in Drug Discovery and Development, MDPI (2023), 16, 1157

Petitioner's Response to Patent Owner Request for Discretionary Denial

Corrected English Translation of Int. Pub. No. WO 2025/026270A1 (Su)

International Pub. No. WO 2024/169952A1 (Huang)

Patent Owner’s Brief in Support of Discretionary Denial

Patent Owner's Updated Exhibit List

Excerpts of File History of U.S. Patent No. 12,234,236

Excerpts of File History of U.S. Patent Application No. 18/885,065

International Publication No. WO 2025/131043A1

Certified English Translation of International Publication No. WO 2025/131043A1

U.S. Patent No. 12,291,530

Patent Owner’s Notice of Intent to Designate a Provisionally Recognized PTAB Attorney as Back-Up Counsel Pursuant to 37 CFR § 42.10(c)(2)

Declaration of Geoffrey D. Biegler Pursuant to 37 CFR § 42.10(c)(2)

Patent Owner’s Exhibit List

Notice: Mandatory Notice

Notice: Power of Attorney

Notice: Notice filing date accorded

U.S. Patent No. 12,234,236

Kawai, et al., Proc Natl Acad Sci U S A., 117(47):29959-29967 (2020)

International Publication No. WO 2025/026270A1

Chinese Patent Application No. 202311372605.9 (“Su II”)

Certified English Translation of Chinese Patent App. No. 20231137260.9

U.S. Patent No. 10,858,356 to Yoshino, et al (“Yoshino”)

Talele, Journal of Medicinal Chemistry, 59(19):8712–8756 (2016) (“Talele”)

Liu, et al., Expert Opinion on Therapeutic Patents, 30(10):781-794 (2020)

Pratt, et al., Diabetes Obes Metab., 25(9):2642-2649 (2023)

Frias, et al., Lancet, 402(10400):472–483 (2023)

Chinese Patent Application No. 202311371725 (“the ’725 Provisional”)

Certified English Translation of Chinese Patent App. No. 202311371725

Chinese Patent Application No. 202311189557 (“the ’557 Provisional”)

Certified English Translation of Chinese Patent App. No. 202311189557

U.S. Patent Provisional App. No. US 63/538,892 (“the ’892 Provisional")

Chinese Patent Application No. 202410142451 (“the ’451 Provisional”)

Certified English Translation of Chinese Patent App. No. 202410142451

Chinese Patent Application No. 202311582240 (“the ’240 Provisional”)

Certified English Translation of Chinese Patent App. No. 202311582240

Chinese Patent Application No. 202311686034 (“the ’034 Provisional”)

Certified English Translation of Chinese Patent App. No. 202311686034

U.S. Patent Provisional Application No. 63/545,615 (“the ’615 Provisional”)

U.S. Patent Provisional Application No. 63/603,854 (“the ’854 Provisional”)

Patel & Burns, J Am Chem Soc., 144(39):17797-17802 (2022) (“Patel”)

Pennington & Moustakas, J Med Chem., 60(9):3552-3579 (2017)

Chinese Patent Publication No. CN117069743A (“Meng”)

Certified English Translation of Chinese Patent Publication No. CN117069743

U.S. Patent No. 12,037,339 (“Ren”)

Certified English Translation of International Publication No. WO 2025/0262

Certified English Translation of International Pub. No. WO 2025/026272

Excerpts of File History of U.S. Patent No. 12,234,236

Declaration of Michael C. Pirrung, Ph.D.

Petition: as filed

Notice: Power of Attorney