UNITED STATES PATENT AND TRADEMARK OFFICE
`_________________________
`
`BEFORE THE PATENT TRIAL AND APPEAL BOARD
`_________________________
`
`SUN PHARMACEUTICAL INDUSTRIES LTD.
`Petitioner,
`v.
`MERCK SHARP & DOHME CORP.
`Patent Owner.
`_________________________
`Case IPR2020-01072
`Patent No. 7,326,708
`_________________________
`DECLARATION OF DR. STEVEN W. BALDWIN, PH.D.
`
`Mail Stop PATENT BOARD
`Patent Trial and Appeal Board
`U.S. Patent and Trademark Office
`P.O. Box 1450
`Alexandria, VA 22313-1450
`Submitted Electronically via the PTAB E2E System
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`IPR2020-01072 (7,326,708)
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`TABLE OF CONTENTS
`
` I.
`
`II.
`
`III.
`
`IV.
`
`A.
`
`B.
`
`V.
`
`VI.
`
`INTRODUCTION ...................................................................................... 1
`
`MY EXPERIENCE AND QUALIFICATIONS ........................................ 3
`
`LIST OF MATERIALS CONSIDERED ................................................... 4
`
`LEGAL STANDARD ................................................................................ 5
`
`Anticipation ................................................................................................ 6
`
`Obviousness ................................................................................................ 7
`
`BACKGROUND ...................................................................................... 10
`
`PERSON OF ORDINARY SKILL IN THE ART (“POSA”) ................. 11
`
`VII.
`
`THE ’708 PATENT .................................................................................. 12
`
`VIII.
`
`CLAIM CONSTRUCTION ..................................................................... 16
`
`IX.
`
`ANTICIPATION ...................................................................................... 18
`
`A.
`
`Ground 1: WO 03/004498 anticipates Claims 1-3, 17, 19, and 21-23 of
`the ’708 patent .......................................................................................... 18
`
`1. Disclosure of WO ’498 ............................................................................. 19
`
`2. Claim 1 of the ’708 Patent ........................................................................ 29
`
`3. Claim 2 of the ’708 Patent ........................................................................ 32
`
`4. Claim 3 of the ’708 Patent ........................................................................ 33
`
`5. Claim 17 of the ’708 Patent ...................................................................... 34
`
`6. Claim 19 of the ’708 Patent ...................................................................... 35
`
`7. Claims 21-22 of the ’708 Patent ............................................................... 36
`
`8. Claim 23 of the ’708 Patent ...................................................................... 38
`
`i
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`IPR2020-01072 (7,326,708)
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`B.
`
`Ground 2: Claims 1-3, 17, 19, and 22-23 Are Anticipated by the ’871
`Patent ........................................................................................................ 39
`
`1. Disclosure of the ’871 Patent ................................................................... 39
`
`2. Claims 1 and 2 .......................................................................................... 39
`
`3. Claim 3 ..................................................................................................... 40
`
`4. Claims 17 and 19 ...................................................................................... 41
`
`5. Claim 21 ................................................................................................... 44
`
`6. Claim 22 ................................................................................................... 45
`
`7. Claim 23 ................................................................................................... 45
`
`X.
`
`OBVIOUSNESS ....................................................................................... 45
`
`A.
`
`Ground 3: Claims 3, 17, 19, and 21-23 Would Have Been Obvious in
`View of WO ’498 ..................................................................................... 46
`
`1. The Level of Ordinary Skill in the Pertinent Art ..................................... 46
`
`2. The Scope and Content of the Prior Art ................................................... 46
`
`B.
`
`Ground 4: Claims 1-3, 17, 19, and 21-23 Would Have Been Obvious in
`View of WO ’498 and Bastin ................................................................... 51
`
`1. The Level of Ordinary Skill in the Pertinent Art ..................................... 51
`
`2. The Scope and Content of the Prior Art ................................................... 51
`
`3. The Differences Between the Claims and Prior Art ................................. 53
`
`C.
`
`Ground 5: Claim 4 Would Have Been Obvious in View of WO ’498,
`Bastin, and Brittain ................................................................................... 60
`
`1. The Level of Ordinary Skill in the Pertinent Art ..................................... 60
`
`2. The Scope and Content of the Prior Art ................................................... 60
`
`ii
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`3. The Differences Between the Claim and Prior Art .................................. 62
`
`D.
`
`Ground 6: Claim 4 Would Have Been Obvious in View of WO ’498 and
`Brittain ...................................................................................................... 63
`
`1. The Level of Ordinary Skill in the Pertinent Art ..................................... 63
`
`2. The Scope and Content of the Prior Art ................................................... 63
`
`3. The Differences Between the Claim and Prior Art .................................. 63
`
`SECONDARY CONSIDERATIONS ...................................................... 64
`
`XI.
`
`
`
`iii
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`IPR2020-01072 (7,326,708)
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`I, Steven W. Baldwin, Ph.D., do hereby declare and state as follows:
`
`1.
`
`I have been asked to provide testimony as to what one of ordinary skill
`
`in the art would have understood with respect to the patent at issue and various prior
`
`art discussed herein. I provide this testimony below:
`
`I. INTRODUCTION
`2.
`I am over the age of 18 and otherwise competent to make this
`
`Declaration.
`
`3.
`
`I have been retained on behalf of Petitioner Sun Pharmaceutical
`
`Industries Ltd., for the above-captioned inter partes review (“IPR”). I am being
`
`compensated for my time in connection with this IPR at my standard consulting rate,
`
`which is $500 per hour. My compensation does not depend in any way on the
`
`outcome of the IPR.
`
`4.
`
`It is my understanding that the Petition for Inter Partes Review in this
`
`matter (the “Petition”) involves U.S. Patent No. 7,326,708 (“the ’708 patent”)
`
`(EX1001).
`
`5.
`
`The ’708 patent names Stephen Howard Cypes, Alex Minhua Chen,
`
`Russell R. Ferlita, Karl Hansen, Ivan Lee, Vicky K. Vydra, and Robert M. Wenslow,
`
`Jr. as the purported inventors.
`
`6.
`
`For the purposes of this declaration, I have been told to assume the
`
`relevant priority date of the ’708 patent is June 24, 2003—the filing date of U.S.
`
`1
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`Provisional Application No. 60/482,1611. I further understand that the ’708 patent is
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`assigned to Merck, Sharpe & Dohme Corp. (“Merck,” “Patentee,” or “Patent
`
`Owner”).
`
`7.
`
`As explained below, it is my opinion that Claims 1-4, 17, 19, and 21-
`
`23 of the ’708 patent2 are anticipated or would have been obvious to the skilled
`
`artisan as of the time of the priority date of the ’708 patent. Therefore, these claims
`
`are invalid.
`
`
`1
`I have not been asked to analyze whether this is indeed the correct priority
`
`date but rather assume that it is for the purposes of my declaration. I understand that
`
`Patent Owner has recently contended that the priority date is earlier than June 24,
`
`2003. EX1015, 10. I express no opinion at this time as to whether June 24, 2003 is,
`
`in fact, the correct priority date. However, should this become an issue during the
`
`proceeding, I may be called upon to offer my opinion.
`
`2
`
`I have not been asked to express an opinion about any other claim of the ’708
`
`patent, nor do I express such opinion because I have not undertaken such an analysis.
`
`2
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`II. MY EXPERIENCE AND QUALIFICATIONS3
`8.
`I am a Professor of Chemistry at Duke University and have specific
`
`IPR2020-01072 (7,326,708)
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`expertise in the field of organic chemistry. My education and experience in this field
`
`are set forth in detail below and in my attached curriculum vitae (Exhibit 1003).
`
`9.
`
`I received my Bachelor’s degree in Chemistry from Dartmouth College
`
`in 1964. I earned my Ph.D. in Organic Chemistry from the California Institute of
`
`Technology in 1969.
`
`10. Following my Ph.D., I completed a National Institutes of Health
`
`Postdoctoral Fellowship from 1969 to 1970 at Columbia University.
`
`11.
`
`I started teaching Chemistry at Duke University in 1970. In addition to
`
`my teaching responsibilities, I served as the director of Graduate Studies and the
`
`chairman of the Department of Chemistry for several years. I have directed 46
`
`doctoral dissertations and masters’ theses.
`
`12. My main research focus lies in the area of synthetic organic chemistry
`
`as applied to molecules of biological interest.
`
`13.
`
`I have published broadly in the field of organic synthetic chemistry. I
`
`have authored or co-authored more than 50 publications and am in the process of
`
`
`3
`I reserve the right to explain my background and qualifications during any
`
`deposition or in any subsequent Reply.
`
`3
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`preparing or have submitted for publication eight additional papers. I have also
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`made numerous presentations regarding my research, and I am the named inventor
`
`of five patents.
`
`14.
`
`I am a member of a number of professional affiliations, including the
`
`American Chemical Society, the American Association for the Advancement of
`
`Science, and the American Association of University Professors. I am also a
`
`reviewer for a number of publications and granting agencies, including the Journal
`
`of the American Chemical Society, The Journal of Organic Chemistry, the National
`
`Science Foundation, and the National Institutes of Health.
`
`III. LIST OF MATERIALS CONSIDERED
`15.
`In formulating my opinions, I have considered the materials referenced
`
`in this Declaration and the Exhibit List below. I have also reviewed the ’708 patent
`
`(EX1001) and its prosecution history, as well as each of the documents cited herein
`
`in light of the general knowledge in the state of the art as of June 24, 2003.
`
`Exhibit #
`1001
`1002
`1003
`1004
`1005
`1006
`
`Description
`U.S. Patent No. 7,326,708
`Declaration of Dr. Steven Baldwin
`CV of Dr. Steven Baldwin
`WO 03/004498 to Edmonson
`Brittain, “Polymorphism in Pharmaceutical Solids”
`Bastin et al. “Salt Selection and Optimisation [sic]
`Procedures for Pharmaceutical New Chemical
`Entities”
`
`4
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`
`Exhibit #
`1007
`1008
`1009
`1010
`
`1011
`1012
`
`1013
`1014
`1015
`
`1016
`
`1017
`
`IPR2020-01072 (7,326,708)
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`Description
`U.S. Patent No 6,699,871
`Orange Book Entry for Janumet®
`Orange Book Entry for Januvia®
`Complete copy of the prosecution history of the ’708
`patent as available for download from the USPTO
`website
`U.S. Patent No. 4,572,909
`U.S. Provisional Application No. 60/303,475, filed
`July 6, 2001
`Prescribing Information for Janumet®
`Prescribing Information for Januvia®
`Merck Sharpe & Dohme’s Responses and Objections
`to
`Defendants’ First Set of Joint Interrogatories (1-10)
`Brown et al., Chemistry: The Central Science, 8th
`Revised Edition 615-618 (2002)
`Mylan Pharmaceuticals Inc. v. Merck Sharp &
`Dohme Corp., IPR2020-00040, Ex. 1002, Declaration
`of Dr. Mukund Chorghade, Ph.D. (Oct. 29, 2019)
`
`IV. LEGAL STANDARD
`16. Although I am not a lawyer, I have been informed by counsel and
`
`provide my general understanding of the law of anticipation and obviousness. I used
`
`these principles in conducting my analysis and drawing any conclusions.
`
`17.
`
`I understand that the first step in determining whether a patent claim
`
`would have been anticipated or obvious is to construe the claims to determine claim
`
`scope and meaning. I understand that in IPR proceedings, the claims must generally
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`5
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`be given “the meaning that the term would have to a person of ordinary skill in the
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`art in question at the time of the invention.”
`
`A. Anticipation
`18.
`I understand that anticipation requires that each and every element of
`
`the claimed invention be disclosed expressly or inherently in a single prior art
`
`reference. I also understand that a reference can anticipate a claim even if it does
`
`not expressly spell out all the limitations arranged or combined as in the claim. For
`
`example, I understand that an element may be inherent in the prior art where the
`
`prior art necessarily functions in accordance with or includes the claimed limitations.
`
`I am also informed that inherency may exist even if a POSA would not appreciate
`
`or recognize the inherent characteristics of the prior art, as the discovery of a
`
`previously unappreciated property does not make an old composition patentable.
`
`19. Moreover, a reference anticipates a claim if it discloses the claimed
`
`invention such that a skilled artisan could take its teachings in combination with his
`
`own knowledge of the particular art and be in possession of the invention. In an
`
`anticipation inquiry, it is proper to take into account not only specific teachings of
`
`the reference but also the inferences which one skilled in the art would reasonably
`
`be expected to draw therefrom. It is also my understanding that proof of efficacy is
`
`not required in order for a reference to be enabled for purposes of anticipation, or
`
`for that matter, anticipation does not require actual performance of suggestions in a
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`6
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`disclosure. I also understand that a prior art reference must enable a POSA to make
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`and use a claimed invention in order to anticipate a patent claim, although I
`
`understand that in an IPR, prior art references are presumed to be enabled.
`
`B. Obviousness
`20.
`I understand that a patent claim is invalid if the differences between the
`
`claimed invention and prior art are such that the subject matter as a whole would
`
`have been obvious at the time the invention was made to a POSA.
`
`21.
`
`I have been told the following factors (sometimes referred to as the
`
`Graham factors) are used in making an obviousness determination: a) the scope and
`
`content of the prior art; b) the differences between the prior art and the claimed
`
`invention; c) the level of ordinary skill in the pertinent art; and d) any secondary
`
`considerations evidencing non-obviousness. The obviousness analysis looks to the
`
`state of the art that existed at the time the invention was made. Moreover,
`
`obviousness does not require absolute predictability of success; all that is required
`
`is a reasonable expectation of success. Moreover, I have been informed that the
`
`person of ordinary skill need only have a reasonable expectation of success of
`
`developing the claimed invention. Finally, obviousness cannot be avoided simply
`
`by a showing of some degree of unpredictability in the art so long as there was a
`
`reasonable probability of success.
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`7
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`22.
`
`I also understand that obviousness can be established by combining or
`
`modifying the teachings of the prior art. A claimed invention can be obvious when,
`
`for example, there is some teaching, suggestion, or motivation in the prior art that
`
`would have led a POSA to modify the prior art reference or to combine prior art
`
`reference teachings to arrive at the claimed invention.4
`
`23.
`
`I also understand that the prior art references themselves do not have to
`
`provide an explicit teaching, suggestion, or motivation to combine prior art
`
`teachings; rather, the analysis may rely on interrelated teachings, market demands,
`
`the background knowledge possessed by a POSA, and/or common sense. Moreover,
`
`the POSA can also take account of the inferences and creative steps that he or she
`
`would employ. Put another way, the motivation to combine or modify prior art
`
`references can come from any reason to do so and is not limited to the reasons that
`
`may have motivated the patentee.
`
`24.
`
`I am also informed that a combination of familiar elements according
`
`to known methods is likely to be obvious when it does no more than yield predictable
`
`
`4
`As a general matter, in my view in science and technology a POSA would not
`
`view any single disclosure as complete, and thus, look no further. Were that the case,
`
`society would have halted progress long ago. Instead, ordinary artisans always seek
`
`improvement in their respective fields.
`
`8
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`results. I also understand that when a POSA would have reached the claimed
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`invention through routine experimentation, the invention may be deemed obvious.
`
`25.
`
`I understand that various rationales are utilized to determine whether a
`
`claim
`
`is obvious,
`
`including, among others:
`
` (i) simple substitution or
`
`interchangeability of one known element for another to obtain predictable results;
`
`(ii) use of known techniques to improve similar methods or products in the same
`
`way; (iii) applying a known technique to a known method or product ready for
`
`improvement to yield predictable results; (iv) “obvious to try”—choosing from a
`
`finite number of identified, predictable solutions, with a reasonable expectation of
`
`success; and (v) known work in one field of endeavor prompting variations of it for
`
`use in either the same field or a different one based on design incentives or other
`
`market forces if the variations would have been predictable to one of ordinary skill
`
`in the art.
`
`26. As stated above, I understand that secondary considerations of non-
`
`obviousness are part of the obviousness inquiry. I understand that these secondary
`
`considerations may include failure of others, copying, unexpectedly superior results,
`
`perception in the industry, commercial success, and long-felt but unmet need. I also
`
`understand that for secondary considerations of non-obviousness to be applicable,
`
`they must have a nexus to the claimed subject matter. I understand that this nexus
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`9
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`(i.e., link) includes a connection between the subject matter of the claim and the
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`alleged secondary considerations.
`
`27.
`
`I understand that I cannot use hindsight in any obviousness analysis. In
`
`connection with my opinions, I did not use hindsight, nor did I use the claims and/or
`
`the disclosure of the ’708 patent as a blueprint for piecing together the prior art to
`
`arrive at the claimed invention. As part of the obviousness analysis, and to avoid
`
`hindsight, I thought back to the time of invention (i.e., the relevant priority date
`
`(discussed further below)) and considered the thinking of POSA, guided only by the
`
`prior art references and the then-accepted wisdom in the field.
`
`V.
`
`BACKGROUND
`28. Medicinal chemistry is a subject that deals with the design, synthesis,
`
`evaluation, and development of chemical compounds which exert beneficial effects
`
`upon living systems. Medicinal chemists must have a firm understanding of organic
`
`and synthetic chemistry as well as knowledge of other disciplines such as biological,
`
`medical, and pharmaceutical sciences.
`
`29. Medicinal chemists study relationships between the structure of a
`
`particular compound or group of compounds and their properties, including their
`
`interactions with biological systems. These relationships are called structure-
`
`activity relationships (“SAR”). The rationale behind SAR is that the structure of a
`
`chemical implicitly determines its physico-chemical and biological properties.
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`30. The goal of the medicinal chemist is to optimize not only the
`
`pharmacological properties, such as potency, but also the drug-like properties of the
`
`molecules in order to identify a compound suitable for therapeutic use.
`
`VI. PERSON OF ORDINARY SKILL IN THE ART (“POSA”)
`31.
`In arriving at my opinions, I have relied on my experience in the
`
`relevant art and have considered the point of view of a POSA as of the relevant
`
`priority date. It is my understanding that a POSA is a hypothetical person who is
`
`presumed to be aware of all pertinent art, thinks along conventional wisdom in the
`
`art, and is a person of ordinary creativity.
`
`32. As of the relevant priority date, a POSA in the relevant field would have
`
`had (i) a Ph.D. in chemistry, biochemistry, medicinal chemistry, pharmacy,
`
`pharmaceutics, or a related field, and at least two years of relevant experience in
`
`drug development, including an understanding of salt selection in drug development;
`
`(ii) a master’s degree in the same fields and at least five years of the same relevant
`
`experience; or (iii) a bachelor’s degree in the same fields and at least seven years of
`
`the same relevant experience.
`
`33. A POSA would also have knowledge of the scientific literature
`
`concerning the same as of the priority date. A POSA may also work as part of a
`
`multidisciplinary team and draw upon not only his or her own skills, but also take
`
`advantage of certain specialized skills of others in the team to solve a given problem.
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`11
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`34.
`
`In determining the qualifications of a POSA, I considered, among other
`
`factors, the field of the alleged invention and use thereof described in the ’708 patent
`
`and my experience with the educational level of practitioners in related fields. In
`
`addition, my opinion is based upon my background, education, and personal
`
`experience.
`
`35. Based on my experience, I had the understanding and capabilities of a
`
`POSA as defined above prior to, and on, the relevant priority date, and all testimony
`
`and opinions provided herein is from that perspective, including that relevant
`
`timeframe.
`
`VII. THE ’708 PATENT
`36.
`I have reviewed and considered the ’708 patent in view of general
`
`knowledge in the relevant field measured from the relevant priority date for the ’708
`
`patent from the perspective of a POSA as defined above. Again, I reviewed the ’708
`
`patent not for the purposes of using any hindsight in my analysis, but so that I could
`
`understand the scope of the claims, the nature of the alleged invention,5and other
`
`
`5
`For example, I have been informed that the second Graham factor requires
`
`evaluation of the “differences between the prior art and the claims at issue.” To
`
`provide such an analysis, an understanding of the “claims at issue” is needed, which
`
`necessitates a review of the patent.
`
`12
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`matters germane to my analysis (e.g., claim construction issues, priority date issues,
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`and determining the definition of a POSA).
`
`37.
`
`I understand Patent Owner contends that the ’708 patent purportedly
`
`covers the Janumet® and Januvia® products by listing it in the Orange Book. See
`
`EX1008 and EX1009.
`
`38. The ’708 patent, entitled “Phosphoric Acid Salt of a Dipeptidyl
`
`Peptidase-IV Inhibitor,” issued on February 5, 2008 from U.S. Appl. No. 10/874,992
`
`(“the ’992 application”), and ultimately claims a benefit of priority from U.S.
`
`Provisional Application No. 60/482,161 filed June 24, 2003. The ’708 patent issued
`
`with 24 claims, although as mentioned above, I am focusing my analysis on Claims
`
`1-4, 17, 19, and 21-23.
`
`39. The ’708 patent is allegedly directed to “dihydrogenphosphate salt of
`
`4-oxo-4-[3-(trifluoromethyl)-5,6-dihydro [1,2,4] triazolo [4,3-a]lpyrazin-7(8H)-
`
`yl)1-(2,4,5-trifluorophenyl)butan-2-amine [which] is a potent inhibitor of dipeptidyl
`
`peptidase-IV and is useful for the prevention and/or treatment of non-insulin
`
`dependent diabetes mellitus, also referred to as type 2 diabetes.” EX1001, Abstract.
`
`According to the ’708 patent, “[i]nhibition of dipeptidyl peptidase-IV (DP-IV), an
`
`enzyme that inactivates both glucose-dependent insulinotropic peptide (GIP) and
`
`glucagon-like peptide 1 (GLP-1), represents a novel approach to the treatment and
`
`13
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`prevention of Type 2 diabetes, also known as non-insulin dependent diabetes
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`mellitus (NIDDM).” EX1001, 1:32-37.
`
`40. At a high level, Claims 1-4 are directed to sitagliptin phosphate “or a
`
`hydrate thereof,” sitagliptin phosphate in the (R) or (S) configuration, or a crystalline
`
`monohydrate of (R)-sitagliptin phosphate. Claim 17 is directed to a pharmaceutical
`
`composition containing (R)-sitagliptin phosphate. Claim 19 is directed to a method
`
`for the treatment of type 2 diabetes using (R)-sitagliptin phosphate. Claims 21-23
`
`depend ultimately from Claim 2 and recite certain process steps for making
`
`(R)sitagliptin phosphate.
`
`41. Below, I have reproduced Claims 1-4, 17, 19, and 21-23:
`
`salt of 4-oxo-4-[3-
`A dihydrogenphosphate
`1.
`(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-
`a]pyrazin-7(8H)-yl]-1-(2,4,5-trifluorophenyl)butan-2-
`amine of structural formula I:
`
`or a hydrate thereof.
`
`
`
`The salt of claim 1 of structural formula II having
`2.
`the (R)-configuration at the chiral center marked with an*
`
`14
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`IPR2020-01072 (7,326,708)
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`The salt of claim 1 of structural formula III having
`3.
`the (S)-configuration at the chiral center marked with an*
`
`
`The salt of claim 2 characterized in being a
`4.
`crystalline monohydrate.
`
`17. A pharmaceutical composition comprising a
`therapeutically effective amount of the salt according to
`claim 2 in association with one or more pharmaceutically
`acceptable carriers.
`
`19. A method for the treatment of type 2 diabetes
`comprising administering to a patient in need of such
`treatment a therapeutically effective amount of the salt
`according to claim 2 or a hydrate thereof.
`
`21. A process for preparing the salt of claim 2 comprising
`the step of contacting one equivalent of (2R)-4-oxo-4-[3-
`(trifluoromethyl)-5,6-
`
`15
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`IPR2020-01072 (7,326,708)
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`dihydro[1,2,4]triazolo[4,3a]pyrazin-7(8H)-yl]-1-(2,4,5-
`trifluorophenyl)butan-2-amine in an organic solvent or
`aqueous organic solvent with about a one equivalent of
`phosphoric acid at a temperature in the range of about 25-
`100° C.
`
`22. The process of claim 21 wherein said organic solvent
`is a C1-C5 linear or branched alkanol.
`
`23. The phosphoric acid salt of (2R)-4-oxo-4-[3-
`(trifluoromethyl)-5,6-
`dihydro[1,2,4]triazolo[4,3a]pyrazin-7(8H)-yl]-1-(2,4,5-
`trifluorophenyl)butan-2-amine prepared according to the
`process of claim 21.
`
`42. As mentioned above, I reviewed the file history of the ’708 patent.
`
`EX1010. From my review, the Examiner never asserted any prior art rejection.
`
`Furthermore, I saw that no declaration or other evidence of unexpected results (or
`
`any other secondary considerations) was presented to the Examiner during
`
`examination.
`
`43.
`
`I will provide further analysis of the ’708 patent later in this
`
`Declaration.
`
`VIII. CLAIM CONSTRUCTION
`44.
`It is my understanding that in an IPR proceeding the claim terms
`
`ordinarily should be given “the meaning that the term would have to a person of
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`ordinary skill in the art in question at the time of the invention.” I have been
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`IPR2020-01072 (7,326,708)
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`informed that there is no prior claim construction determination concerning the ’708
`
`patent in a civil action or a proceeding before the International Trade Commission.
`
`45. The ’708 patent defines various terms within the specification. See,
`
`e.g., EX1001, 3:60-66; 7:62-67; 14:65-15:5. To the extent the ’708 patent
`
`specification defines any term, I use those definitions if relevant in my analysis. As
`
`to all other claim terms, after reviewing the Specification of the ‘708 patent and the
`
`associated file history, in my opinion, no other claim term needs to be construed.
`
`Therefore, I apply the meaning that the claim term would have to a POSA in question
`
`at the time of the invention; i.e., around June 24, 2003.6
`
`46.
`
`I also understand that the transitional phrase “comprising” as used in
`
`the ’708 patent is open ended, i.e., it can include other components, elements, or
`
`steps. This is in contrast to the term “consisting essentially of,” which limits the
`
`scope of a claim to the specified materials or steps and those that do not materially
`
`
`6
`I understand that in the related district court litigation, Patent Owner has
`
`recently contended that the priority date for Claims 1 and 2 of the ’708 patent is no
`
`later than December 13, 2001, i.e., earlier than June 24, 2003. EX1015, Response
`
`to Interrogatory No. 1. My opinions herein are the same regardless of whether the
`
`priority date is determined to be December 13, 2001 or June 24, 2003.
`
`17
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`affect the basic and novel characteristic(s) of the claimed invention.7 Finally, I have
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`IPR2020-01072 (7,326,708)
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`also been informed that “consisting of” excludes any element, step, or ingredient not
`
`specified in the claim.8
`
`IX. ANTICIPATION
`A. Ground 1:9 WO 03/004498 anticipates Claims 1-3, 17, 19, and 21-
`23 of the ’708 patent
`In my opinion, WO 03/004498 (“WO ’498,” EX1004) anticipates
`
`47.
`
`Claims 1-3, 17, 19, and 21-23 of the ’708 patent.
`
`48. WO ’498 was published January 16, 2003, and is entitled “Beta-amino
`
`tetrahydroimidazo (1, 2-a) pyrazines and tetrahydrotriazolo (4, 3-a) pyrazines as
`
`dipeptidyl peptidase inhibitors for the treatment or prevention of diabetes.” I have
`
`been informed that WO ’498 is prior art to the ’708 patent.
`
`
`7
`To be clear, neither “consisting essentially of” nor “consisting” appear in any
`
`claim term of any challenged claim of the ’708 patent.
`
`8
`
`I note that Claim 15 of the WO ’498 uses the term “consisting of.” Therefore,
`
`so that I fully understand the meaning of “consisting of,” it is provided above.
`
`9
`
`I have been informed that Sun is asserting six grounds (i.e., separate
`
`challenges) in total in its Petition.
`
`18
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`IPR2020-01072 (7,326,708)
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`49. From my review of the file history of the ’708 patent, WO ’498 was not
`
`used by the Examiner to formulate any prior art rejection against any of the allowed
`
`claims. EX1010.
`
`1.
`
`Disclosure of WO ’498
`
`50.
`
`I begin by discussing WO ’498 as it would be understood by a POSA.
`
`WO ’498 teaches compounds that may be used as dipeptidyl peptidase-IV enzyme
`
`inhibitors to treat or prevent diabetes. EX1004, 3:23-26.
`
`51. WO ’498 explains how the dipeptidyl peptidase-IV enzyme inhibitors
`
`impact diabetes:
`
`The usefulness of DP-IV inhibitors in the treatment of type
`2 diabetes is based on the fact that DP-TV in vivo readily
`inactivates glucagon like peptide- 1 (GLP-1) and gastric
`inhibitory peptide (GIP). GLP-1 and GIP are incretins and
`are produced when food is consumed. The incretins
`stimulate production of insulin. Inhibition of DP-TV leads
`to decreased inactivation of the incretins, and this in turn
`results in increased effectiveness of the incretins in
`stimulating production of insulin by the pancr