Merck Sharp & Dohme LLC - IPR2026-00313

Notice filing date accorded

U.S. Patent No. 11,041,149

File History of U.S. Patent No. 11,041,149 Part 1

File History of U.S. Patent No. 11,041,149 Part 2

United States Patent Publication No. 2013/0302275

U.S. Patent No. 7,767,429

Chao, Structure of Human Hyaluronidase-1 (2007)

WO 2010/077297, published 8 July 2010

Stern, The Hyaluronidases: Their Genomics, Structures, & Mechanisms (2006)

Jedzrejas, Structures of Vertebrate Hyaluronidases (2005)

Zhang, Hyaluronidase Activity of Human Hyal1 (2009)

Arming, In vitro Mutagenesis of PH-20 Hyaluronidase from Human Sperm (1997)

Bordoli, Protein Structure Homology Modeling Using SWISSMODEL (2008)

Frost, Recombinant Human Hyaluronidase (rHuPH20) (2007)

Branden & Tooze, Introduction to Protein Structure (1999) Part 1

Branden & Tooze, Introduction to Protein Structure (1999) Part 2

Table Associating Citations from the ’149 Patent to '731 App and US-275

Steipe, Consensus-Based Engineering of Protein Stability (2004)

Green, Computer Graphics, Homology Modeling, and Bioinformatics (2010)

Chica, Semi-rational Approaches to Engineering Enzyme Activity (2005)

Hardy Assessment of Contraceptive Vaccines Based on Recombinant Mouse Sperm

Pomering, Restricted Entry of IgG (2002)

Baba, Mouse Sperm Lacking Cell Surface Hyaluronidase PH-20 (2002)

Primakoff, Reversible Contraceptive Effect of PH-20 Immunization (1997)

Tung, Mechanism of Infertility in Male Guinea Pigs Immunized with Sperm

Rosengren, Recombinant Human PH20 (2018)

U.S. Patent Application No. 13/694,731

2024 Chemistry Nobel Prize Background

Bordier “Phase separation integral membrane proteins Triton X-114" (1981)

Gmachl, The Human Sperm Protein PH-20 Has Hyaluronidase Activity (1993)

Sills, “Retraction,” Science, 319:569 (2008)

Yue, Loss of Protein Structure Stability as a Major Causative Factor (2005)

Wang & Moult, SNPs, Protein Structure, and Disease (2001)

Marković-Housley, Crystal Structure of Hyaluronidase (2000)

“Negative Results,” Nature: Editorials, 453:258 (2008)

Hayden, Chemistry: Designer Debacle (2008)

Alberts, Molecular Biology of the Cell, Chapter 3 (2007)

He, NMR Structures of Two Designed Proteins with High Sequence Identity

Alexander, A Minimal Sequence Code for Switching Protein Structure (2009)

Ruan, Design & Characterization of a Protein Fold Switching Network (2023)

Redline Comparison of the ’731 Application and ’149 Patent Specifications

Beasley & Hecht, Protein Design: The Choice of de Novo Sequences (1997)

Xiong, Periodicity of Polar and Nonpolar Amino Acids (1995)

Hayden, Key Protein-Design Papers Challenged (2009)

U.S. Patent Application No. 61/631,313

U.S. Patent Application No. 61/796,208

Leisola & Turunen, Protein Engineering: Opportunities and Challenges (2007)

Rosengren, Clinical Immunogenicity of rHuPH20 (2015)

Collection of SWISS-MODEL Webpages from the Internet Archive

Declaration of Jeffrey P. Kushan

Hunnicutt, Sperm Surface Protein PH-20 Is Bifunctional (1996)

Bookbinder, A Recombinant Human Enzyme for Enhanced Interstitial Transport

Goldberg, Protein Degradation and Protection (2003)

Vembar & Brodsky, “One Step at a Time: Endoplasmic Reticulum" (2008)

United States Patent Publication No. 2010/0143457

Primakoff “Fully effective contraception in male and female guinea" (1988)

Im, S. “Cryo-EM Structure of Human Hyaluronidase PH20,” (2025)

Melanie Ann Simpson, Ph.D. Deposition Transcript

Gregory Petsko, Ph.D. Deposition Transcript

Dr. Naismith Analysis Spreadsheet

Dobson, “Principles of protein folding, misfolding and aggregation” (2004)

Dobson, “Protein folding and misfolding” Nature. 18;426(6968):884-90 (2003)

Dobson “Experimental investigation protein folding and misfolding” (2004)

Chiti “Protein Misfolding, Functional Amyloid, and Human Disease” (2006)

Dobson, “Protein misfolding, evolution and Disease” (1999)

Goldsmith “Directed enzyme evolution: beyond the low-hanging fruit" (2012)

Ochoa-Leyva “Protein Design through Systematic Catalytic Loop" (2009)

Pal “Comprehensive and Quantitative Mapping of Energy Landscapes" (2006)

van Rossum, “Reporter-based screening and selection of enzymes” (2013)

Reed “Use of Coefficient of Variation in Assessing Variability" (2002)

TenHave “Cloning and characterization of the cDNA encoding the PH20" (1998)

Chowpongpang “Cloning and characterization of the bovine testicular" (2004)

Fowler “High-resolution mapping of protein sequence function" (2010)

Ringe & Petsko “Q&A: What are pharmacological chaperones" (2009)

Calloni “Investigating the Effects of Mutations on Protein" (2005)

Chiti "Studies of aggregation of mutant proteins in vitro insights" (2002)

Chiti “Rationalization of the effects of mutations on peptide" (2003)

Wang “Immunogenicity of protein aggregates-Concerns and Realities” (2012)

Poelwijk, Frank J., "Empirical fitness landscapes reveal" (2007)

MartinDeleon, P. “Epididymal SPAM1 and its Impact on Sperm Function” (2006)

U.S. Food and Drug Administration, Medical Review: Hylenex, (2005)

US Patent No. 12,091,692

Redline of the ’731 App. and US-275 Publication

Petsko & Ringe, Protein Structure and Function (2004) Part 1

Petsko & Ringe, Protein Structure and Function (2004) Part 2

Petsko & Ringe, Protein Structure and Function (2004) Part 3

Petsko & Ringe, Protein Structure and Function (2004) Part 4

Nelson & Cox, Lehninger Principles of Biochemistry (2005)

Halozyme Therapeutics, Inc., Hylenex Label, U.S. FDA: AccessData (2005)

Declaration of Dr. James Naismith

Petition for Inter Partes Review of U.S. Patent No. 11,041,149

Petitioner's Power of Attorney