Dr. Reddy's Lab., Inc.v.Pozen Inc.

Patent Trial and Appeal Board

Oct 9, 2015

13215855 (P.T.A.B. Oct. 9, 2015)

Trials@uspto.gov Paper 28
Tel: 571-272-7822 Entered: October 9, 2015

UNITED STATES PATENT AND TRADEMARK OFFICE

BEFORE THE PATENT TRIAL AND APPEAL BOARD

DR. REDDY’S LABORATORIES, INC.,
Petitioner,
v.
POZEN INC.,
Patent Owner.

Case IPR2015-00802
Patent No. 8,557,285 B2

Before SHERIDAN K. SNEDDEN, SUSAN L. C. MITCHELL, ROBERT
A. POLLOCK, Administrative Patent Judges.
MITCHELL, Administrative Patent Judge.

DECISION
Denying Institution of Inter Partes Review
37 C.F.R. § 42.108
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I. INTRODUCTION
A. Background
Petitioner Dr. Reddy’s Laboratories, Inc. (“Petitioner”) filed a petition
(Paper 2, “Pet.”) to institute an inter partes review of claims 1–4 (the
“challenged claims”) of U.S. Patent No. 8,557,285 B2 (Exhibit 1001, “the
’285 patent”). See 35 U.S.C. §§ 311-319. Patent Owner Pozen Inc. (“Patent
Owner”) filed a Preliminary Response. Paper 23 (“Prelim. Resp.”).
We have jurisdiction under 35 U.S.C. § 314, which provides that an
inter partes review may not be instituted “unless . . . there is a reasonable
likelihood that the petitioner would prevail with respect to at least 1 of the
claims challenged in the petition.” 35 U.S.C. § 314(a). Upon considering
the Petition and Preliminary Response, we conclude that Petitioner has not
established a reasonable likelihood that it would prevail in showing the
unpatentability of any challenged claim of the ’285 patent. Therefore, we do
not authorize an inter partes review for any claim of the ’285 patent.
B. Related Proceedings
Petitioner identifies five related district court proceedings in the
United States District Court of New Jersey. Pet. 2.
C. The ’285 Patent (Ex. 1001)
The ’285 patent is directed to drug dosage forms that have a
coordinated release of an agent that raises the pH of a patient’s
gastrointestinal tract to a safe level, followed by a non-steroidal
anti-inflammatory drug (“NSAID”)), to reduce unwanted gastrointestinal
side effects. Ex. 1001, Abs., 1:20–26. Although NSAIDs are effective
agents for controlling pain, their use can cause gastroduodenal lesions, such
as ulcers and erosions, and a major factor for developing these lesions
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appears to be a low pH environment (acid) in the upper small intestine. Id.
at 1:30–36.
D. Illustrative Claim
Claim 1, the sole independent claim of the ’285 patent, is illustrative
of the claimed subject matter. Claim 1 is reproduced below.
1. A pharmaceutical composition in unit dosage form
comprising therapeutically effective amounts of:
(a) esomeprazole, wherein at least a portion of said
esomeprazole is not surrounded by an enteric coating;
and
(b) naproxen surrounded by a coating that inhibits its
release from said unit dosage form unless said dosage
form is in a medium with a pH of 3.5 or higher;
wherein said unit dosage form provides for release of said
esomeprazole such that upon introduction of said unit dosage
form into a medium, at least a portion of said esomeprazole is
released regardless of the pH of the medium.
Id. at 22:8–18.
E. Prior Art Relies Upon
Petitioner challenges the patentability of claims 1–4 on the basis of
the following prior art references:
Plachetka US 2003/0069255 Apr. 10, 2003 (Ex. 1021)
Stephen P. Clissold and Deborah M. Campoli-Richards, (Ex. 1029)
“Omeprazole: A Preliminary Review of its
Pharmacodynamic and Pharmacokinetic Properties,
and Therapeutic Potential in Peptic Ulcer Disease and
Zollinger-Ellison Syndrome, 32 DRUGS 15–47 (1986)

Depui WO 97/125064 July 17, 1997 (Ex. 1030)
Lundberg WO 00/78293 Dec. 28, 2000 (Ex. 1031)
Phillips WO 00.26185 May 11, 2000 (Ex. 1032)

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F. The Asserted Grounds of Unpatentability
Petitioner contends that the challenged claims are unpatentable based
on the following grounds (Pet. 4–11):
References Basis Claims challenged
Plachetka Publication § 102(b) 1–4
Depui, Lundberg, Phillips and/or
Clissold
§ 103(a) 1–4
II. ANALYSIS
A. Claim Construction
In an inter partes review, claim terms in an unexpired patent are given
their broadest reasonable construction in light of the specification of the
patent in which they appear. 37 C.F.R. § 42.100(b); see also In re Cuozzo
Speed Techs., LLC, 793 F.3d 1268, 1279 (Fed. Cir. 2015) (“Congress
implicitly approved the broadest reasonable interpretation standard in
enacting the AIA,”
1
and “the standard was properly adopted by PTO
regulation.”). Significantly, claims are not interpreted in a vacuum but are
part of, and read in light of, the specification. United States v. Adams,
383 U.S. 39, 49 (1966) (“[I]t is fundamental that claims are to be construed
in the light of the specifications and both are to be read with a view to
ascertaining the invention . . . .”). Claim terms are given their ordinary and
customary meaning as would be understood by one of ordinary skill in the
art in the context of the entire disclosure. In re Translogic Tech., Inc., 504
F.3d 1249, 1257 (Fed. Cir. 2007). An inventor may rebut that presumption

1
The Leahy-Smith America Invents Act, Pub. L. No. 11229, 125 Stat. 284
(2011) (“AIA”).
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by providing a definition of the term in the specification with reasonable
clarity, deliberateness, and precision. In re Paulsen, 30 F.3d 1475, 1480
(Fed. Cir. 1994). In the absence of such a definition, limitations are not to
be read from the specification into the claims. In re Van Geuns, 988 F.2d
1181, 1184 (Fed. Cir. 1993).
Petitioner proposes constructions for the terms “comprising . . .
naproxen surrounded by a coating,” “inhibit,” and “at least a portion of said
esomeprazole.” Pet. 24–30. Patent Owner proposes a construction for the
three terms defined by Petitioner, as well as the claim terms “enteric
coating” and “unit dosage form.” We address the construction of “enteric
coating” in this section. Because the arguments concerning why the
Plachetka Publication is prior art under 35 U.S.C. 102(b) is so intertwined
with Petitioner’s proposed constructions and Patent Owner’s proposed
construction of “unit dosage form,” we construe the remaining terms as we
address the ground asserting the Plachetka Publication.
“enteric coating”
Petitioner adopted the definition of “enteric coating” from a district
court construction of the term for U.S. Patent No. 6,926,907 (“the ’907
patent) that shares the same specification as the ’285. Pet. 11, n.1, 13
(quoting Patent Owner’s statement that the ’907 patent shares the same
specification of the ’285 patent). The district court interpreted “enteric
coating” to mean “a delayed release coating” and noted that although such
coating is “commonly and perhaps frequently pH-dependent, the evidence
shows that other types of enteric coating are utilized in the field.” Ex. 1019,
12.
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Patent Owner similarly contends that the proper construction of
“enteric coating” means “a delayed release coating,” but agrees with the
district court that the broadest reasonable interpretation of the term “should
not be construed as ‘strictly a pH-dependent form.’” Prelim. Resp. 11.
Petitioner does not appear to disagree with this construction. See Pet. 11,
n.1. On the present record, we conclude that the broadest reasonable
interpretation of “enteric coating” is a delayed release coating that is not
limited to a strictly pH-dependent form. See Ex. 1001, 4:59–64
(“Alternatively, a barrier coating may be employed which controls the
release of NSAID by time, as opposed to pH, with the rate adjusted so that
NSAID is not released until after the pH of the gastrointestinal tract has risen
to at least 3.5, preferably at least 4, and more preferably at least 5.”).
B. Principles of Law
A claim is unpatentable under 35 U.S.C. § 102 if a single prior art
reference expressly or inherently describes each and every limitation set
forth in the claim. See Perricone v. Medicis Pharm. Corp., 432 F.3d 1368,
1375 (Fed. Cir. 2005); Verdegaal Bros., Inc. v. Union Oil Co., 814 F.2d 628,
631 (Fed. Cir. 1987).
A claim is unpatentable under 35 U.S.C. § 103 if the differences
between the claimed subject matter and the prior art are such that the subject
matter, as a whole, would have been obvious at the time the invention was
made to a person having ordinary skill in the art to which said subject matter
pertains. KSR Int’l Co. v. Teleflex Inc., 550 U.S. 398, 406 (2007).
The question of obviousness is resolved on the basis of underlying factual
determinations including: (1) the scope and content of the prior art; (2) any
differences between the claimed subject matter and the prior art; (3) the level
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of ordinary skill in the art; and (4) objective evidence of nonobviousness.
Graham v. John Deere Co., 383 U.S. 1, 17–18 (1966).
A prima facie case of obviousness is established when the prior art
itself would appear to have suggested the claimed subject matter to a person
of ordinary skill in the art. In re Rinehart, 531 F.2d 1048, 1051 (CCPA
1976). The level of ordinary skill in the art is reflected by the prior art of
record. See Okajima v. Bourdeau, 261 F.3d 1350, 1355 (Fed. Cir. 2001);
In re GPAC Inc., 57 F.3d 1573, 1579 (Fed. Cir. 1995); In re Oelrich,
579 F.2d 86, 91 (CCPA 1978).
We analyze the asserted grounds of unpatentability in accordance with
the above-stated principles.
C. Anticipation by or Obviousness Over the Plachetka Publication
Petitioner asserts that the claims of the ’285 patent are not entitled to
an effective filing date earlier than May 16, 2005, because the two
applications filed before this date in the listed chain of priority on the face of
the ’285 patent do not provide written description support for five features of
the claims of the ’285 patent. Pet. 4. This alleged break in the chain of
priority for the claims of the ’285 patent is illustrated in the following figure
provided by Petitioner.
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Id. at 7.
As the above figure shows, the ’285 patent issued from a series of five
applications all of which Petitioner characterizes as addressing
“compositions combining an acid inhibitor and an NSAID and related
methods,” all naming John R. Plachetka as the sole inventor. Id. at 12;
Ex. 1001. Petitioner admits that the specifications of these five applications
are similar. Id. As shown in the figure above, US Provisional Application
60/294,588 (“the ’588 application”) and US Application No. 10/158,216
(“the ’216 application”) are two pre-2003 applications in the priority chain
that Petitioner asserts do not provide written description support for five of
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the features of the claims of the ’285 patent. Because the Plachetka
Publication was published more than two years before the earliest effective
filing date, Petitioner asserts, the Plachetka Publication is prior art under 35
U.S.C. 102(b). Id. at 5–6.
Petitioner asserts that under the broadest reasonable construction
standard, the claims of the ’285 patent are broad enough to encompass
formulations that have the following features:
 releases most of its naproxen immediately at any pH;
 release all of its naproxen slowly at any pH;
 delays release of most of its esomeprazole until reaching a particular
pH;
 does not have “coordinated release,” or
 may be administered orally or in any other manner.
Id. at 8.
In contrast, despite admitting that the specifications of the applications
in the priority chain for the ’285 are similar (see id. at 12–13), Petitioner
asserts that the ’588 and ’216 applications disclose naproxen/esomeprazole
formulations that:
 release no naproxen immediately, and delay[] naproxen release until
reaching a pH of 3.5 or 4;
 prevents the release [of] all of their naproxen until reaching a pH of
3.5 or 4 (as opposed to merely slowing it down, i.e., “inhibiting” it);
 releases all their esomeprazole immediately regardless of pH;
 have “coordinated release,” and
 are orally administered.
Id.
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Patent Owner notes that Petitioner has identified no new matter in the
specification of the ’285 patent relevant to priority that is not identical to the
disclosure in the ’216 application. Prelim. Resp. 14; see Ex. 2009
(comparison between the ’216 application and the ’285 patent). Patent
Owner states that despite that lack of substantial differences in the
specifications, Petitioner argues that the ’285 patent claims are not supported
by its priority application. Prelim. Resp. 15.
Petitioner’s arguments are rooted in its overbroad claim
interpretations, and specifically, as to the application of the transitional term
“comprising,” and the claim terms “inhibits” and “portion.” We will address
Petitioner’s proposed constructions in turn as they relate to the five features
that Petitioner asserts are encompassed by the claims of the ’285 patent, but
not supported by the ’588 or the ’216 applications.
1. “comprising therapeutically effective amounts of . . . naproxen
surrounded by a coating . . .” allegedly encompasses
formulations that release most of its naproxen at any pH
Petitioner asserts that the broadest reasonable interpretation of
“‘comprising . . . naproxen surrounded by a coating’ allows additional
naproxen that is not surrounded by a release inhibiting coating in the “unit
dosage.” Pet. 26. Petitioner concludes that because the transitional phrase
“comprising” allows for additional unrecited elements, “[a]s long as a
minimal ‘therapeutically effective’ amount of naproxen in a unit dosage is
surrounded by the claimed inhibition coating, any amount of additional
uncoated naproxen could be incorporated into the unit dosage.” Id. at 27
(citing Ex. 1010, 49–51, in which Patent Owner makes a similar argument in
District Court). Petitioner posits that under this interpretation, a unit dosage
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could have more than 96.5% of its naproxen released immediately at any pH
and not be subject to coordinated release.
2
Pet. 27–28.
Patent Owner relies on the claim phrase “therapeutically effective” to
frame its interpretation. Prelim. Resp. 7. The claim language requires that a
therapeutically effective amount of naproxen be “surrounded by a coating
that inhibits its release from said unit dosage form unless said dosage form is
in a medium with a pH of 3.5 or higher.” Ex. 1001, 22:12–14. Patent
Owner asserts that the specification of the ’285 patent explicitly defines
“therapeutically effective amount” of NSAID to be “an amount effective to
reduce or eliminate pain or inflammation.” Prelim. Resp. 7 (citing Ex. 1001,
3:66–4:1). The specification of the ’285 patent further defines the
therapeutically effective ranges for naproxen, preferably 50 mg to 1500 mg,
and most preferably, 200 mg to 600 mg. Id. (citing Ex. 1001, 4:11–14).
Because a therapeutically effective amount of naproxen must be
surrounded by a coating, Patent Owner asserts that Petitioner’s position that
the transitional phrase “comprising” may be read to include the bulk amount
of naproxen to be uncoated is unreasonable. Patent Owner concludes that
[a]ccordingly, while other components may be present in a unit
dosage form that includes but is not limited to the recited
therapeutically effective amount of coated naproxen, Petitioner
cannot expand this claim term to include uncoated naproxen––
or any other hypothetical additional components that do not
satisfy the expressly recited coated naproxen requirement—
within this claim limitation.

2
Petitioner bases this statement on the 50 mg to 1500 mg range for naproxen
provided in the specification of the ’285 patent (see Ex. 1001, 4:11–14),
wherein Petitioner asserts that a formulation within the scope of the claims
of the ’285 patent includes a 50 mg minimum amount of naproxen
surrounded by the coating, but 1450 mg outside of the coating.
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Prelim. Resp. 8. Patent Owner concludes that “comprising . . . naproxen
surrounded by a coating” should be interpreted as “a therapeutically
effective amount of naproxen is surrounded by a coating.” Id. at 9.
Both parties acknowledge that the claim requires a therapeutically
effective amount of naproxen must be surrounded by a coating. Pet. 27;
Prelim. Resp. 7. Petitioner’s interpretation, however, turns this requirement
on its head. As Patent Owner notes, using the transitional term
“comprising” means that additional components may be present, but does
not change the elements that are stated in the claim. Prelim. Resp. 8 (citing
Outside the Box Innovations, LLC v. Travel Caddy, Inc., 695 F.3d 1285,
1305 (Fed. Cir. 2012)). Petitioner’s interpretation, however, would
encompass a composition where the vast majority of the naproxen, i.e., a
therapeutically effective amount, would be outside of the coating. This is
not a reasonable interpretation of the claim.
We agree with Patent Owner that the broadest reasonable
interpretation of the term “comprising . . . naproxen surrounded by a
coating” means “a therapeutically effective amount of naproxen is
surrounded by a coating,” but do not agree with Patent Owner’s arguments
that this claim term excludes any uncoated naproxen from the claim.
As Petitioner notes, the Patent Owner has previously addressed the
meaning of this limitation in response to invalidity contentions asserting lack
of written description support and enablement, stating that the specification
of the ’285 patent supports the interpretation “that, in addition to naproxen
surrounded by a coating that inhibits its release unless the surrounding
medium of the unit dosage form is at least 3.5, the disclosed dosage forms
may include additional naproxen outside the coating.” Ex. 1010, 49 (Patent
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Owner’s responses to invalidity contentions for the ’285 patent) (relying on
statements in the specification of the ’285 patent where the combination of
an acid inhibitor and an NSAID may be in multi-layer tablet form and where
the drug combinations may typically be prepared in admixture with
conventional excipients). Patent Owner also has previously stated that the
transitional term “comprising” does not exclude the presence of additional
naproxen outside of the coating. Id. at 51. We agree. Although the claim
term requires that a therapeutically effective amount of naproxen in a unit
dosage form is surrounded by a coating, it does not exclude a unit dosage
form that has an amount of naproxen outside of the coating that is not
therapeutically effective.
Therefore, we do not agree that the claims of the ’285 patent
encompass a formulation that releases most of its naproxen immediately at
any pH as asserted by Petitioner.
2. ”naproxen surrounded by a coating that inhibits its release
from said unit dosage form unless said dosage form is in a
medium with a pH of 3.5 or higher” allegedly encompasses
formulations that release all of its naproxen slowly at any pH
Petitioner asserts that the claim term “inhibits,” which characterizes
the action of the naproxen-release coating, be assigned its ordinary meaning.
Pet. 28–29. Petitioner uses a dictionary definition to define “inhibits” as “to
slow down or stop.” Id. at 29 (citing Ex. 1038 (Merriam Webster’s online
dictionary)).
Although Patent Owner agrees that the term, “inhibits” should be
afforded its ordinary meaning, Patent Owner states that “inhibits” is better
interpreted in light of the specification of the ’285 patent and the claims as
“prevents, hinders, or restrains.” Prelim. Resp. 10.
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We do not discern a significant difference between the definitions
offered by the parties and are not convinced that we need to provide an
explicit definition encompassing the ordinary meaning of the claim term.
Petitioner, however, utilizes its interpretation of the term “inhibits” to
support its assertion that the claims of the ’285 patent encompass
formulations that releases all of its naproxen slowly at any pH, instead of
preventing release until the formulations are in a medium with a pH of 3.5 or
higher. Pet. 8–9. Petitioner admits that the ’216 application discloses eight
composition examples where “[h]alf of them describe a release coating
whose function is to ‘prevent’ the release of naproxen or naproxen sodium
from the unit dosage until it reaches the desired pH.. The other half
describes a release coating that ‘delays’ the release of naproxen or naproxen
sodium from the unit dosage until it reaches a pH [of] 3.5 or 4.” Pet. 32
(citations omitted). Petitioner concludes that
The pre-2003 applications teach that all NSAID release must be
“delayed” or “prevented”—period. Nowhere in the originally
filed pre-2003 applications is there any discussion or even a
suggestion that any of the NSAID in the unit dosage may be
released below a pH of 3.5.
Id. at 37.
We disagree with Petitioner’s interpretation of the difference in
breadth between “inhibit,” “prevent,” and “delay” would lead to the
conclusion that the claims of the ’285 patent encompass a formulation that
releases all of its naproxen slowly at any pH. The distinction between the
ordinary meanings of these terms is not so vast to be able to reach such a
conclusion. Accordingly, we do not accept Petitioner’s argument that the
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claims of the ’285 patent encompass a formulation that releases all of its
naproxen slowly at any pH.
3. “at least a portion of said esomeprazole” allegedly
encompasses formulations that delay release of most of its
esomeprazole until reaching a particular pH
Petitioner proposes an ordinary meaning construction of “portion” as
“a part of any whole.” Pet. 30. Patent Owner agrees that “portion” should
be assigned its ordinary meaning, but offers that “portion” is “a part of a
larger amount.” Again, we do not discern a significant difference between
the definitions offered by the parties and find that we do not need to provide
an explicit definition for the ordinary meaning of this claim term.
Petitioner asserts, however, that the pre-2003 applications disclose
only acid inhibitor or esomeprazole layers that are entirely uncoated and
subject to immediate release. Pet. 9, 36. Patent Owner, however, points to
Example 4 in the ’216 application where the controlled-release core tablet of
naproxen also contains the acid inhibitor famotidine. Prelim. Resp. 18–19;
Ex. 1012, 17–18. This example is also in the specification of the ’285
patent. Ex. 1001, 13:1–14:20.
Both the ’216 application and the specification of the ’285 patent
describe Example 4 as follows:
The controlled-release core tablet of naproxen and
famotidine [acid inhibitor] is film coated with a
pharmaceutically acceptable enteric coating. The function of
the enteric coat is to delay the release of naproxen until the
dosage form reaches an environment where the pH is above
about 4.
. . . .
The outermost [layer] contains an “acid inhibitor” which
is released from the dosage form immediately after
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administration to the patient. The acid inhibitor in the present
example is a proton pump inhibitor or, preferably, the H2
blocker famotidine which consistently raises the pH of the
stomach to above 4.
Ex. 1012, 17:12–14, 18–21; Ex. 1001, 13:18–22, 29–34. In addition to
famotidine, both documents disclose the use of the proton pump inhibitor
esomeprazole as an acid inhibitor to raise gastric pH. See, e.g., Ex. 1012,
4:17–18, 10:5–9; Ex. 1001, 3:44–47; 8:5–15. Therefore, we disagree with
Petitioner that the pre-2003 applications only disclose formulations that
release all their esomeprazole immediately regardless of pH, while the ’285
patent claims encompass formulations that delay release of most of its
esomeprazole until reaching a particular pH.
4. “unit dosage form” does not encompass non-oral
administration
Although Petitioner asserts that the claims of the ’285 patent
encompass formulations that may be administered in ways other than orally
(see Pet. 8; Ex. 1036 ¶ 81), only Patent Owner offers an explicit definition of
“unit dosage form” and asserts it means “a unit dosage form suitable for oral
administration to a patient.” Prelim. Resp. 11. To support its interpretation,
Patent Owner relies on the claim language and a statement in the
specification of the ’285 patent that “[a]ll dosage forms are designed for oral
delivery and provide for the coordinated release of therapeutic agents, i.e.,
for the sequential release of acid inhibitor followed by analgesic.” Id. at 11–
12 (citing Ex. 1001, 6:20–23); see also Pet. 14–15 (recognizing that the
specification of the ’285 patent describes a first aspect of the invention
directed to a unit dosage form suitable for oral administration and
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acknowledging the statement that all the dosage forms were designed for
oral delivery).
We agree with Patent Owner that the specification of the ’285 patent
describes only oral dosage forms for administering the claimed formulations.
For instance, in addition to the statement identified by Patent Owner above,
in defining and describing “unit dosage form,” the specification of the ’285
patent states:
The term “unit dosage form” as used herein refers to a
single entity for drug administration. For example, a single
tablet or capsule combining both an acid inhibitor and an
NSAID would be a unit dosage form. A unit dosage form of
the present invention preferably provides for coordinated drug
release in a way that elevates gastric pH and reduces the
deleterious effects of the NSAID on the gastroduodenal
mucosa, i.e., the acid inhibitor is released first and the release of
NSAID is delayed until after the pH of the GI tract has risen.
Ex. 1001, 4:42–51. Moreover, the specification of the ’285 patent describes
a solution to prevent damage caused to the gastrointestinal tract of patients
using NSAIDS, which focuses on the production of tablets and capsules.
See, e.g., Ex. 1001, 1:20–3:7; see also id. at 8:17–21 (“The pharmaceutical
compositions of the invention include tablets, dragees, liquids and
capsules.”). It is hard to imagine how the administration of these dosage
forms could be accomplished in a way other than oral administration.
As Patent Owner notes, Petitioner gives no examples of any
administration of the claimed pharmaceutical composition that could be used
in non-oral administration. Patent Owner also points out that Petitioner does
not explain how any other potential non-oral route of administration “would
expose the unit dosage to the anticipated pH variations described by the
claims and the specification other than the stomach and intestinal tract.”
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Prelim. Resp. 12. We agree with Patent Owner that “[a]ny administration
route other than oral simply makes no sense in the context of the ’285
patent.” See id.
The only explanation offered by Petitioner for its position is that the
’285 patent claims do not require the unit dosage form to be “suitable for
oral administration” is that this limitation is expressly set forth in the
composition claims of the ’907 patent. Pet. 25 (comparing ’907 and ’285
claims), 27. In addition, Petitioner’s declarant, Dr. Kibbe, opined that even
though “[t]he person of ordinary skill in the art would . . . understand that all
of the dosage forms disclosed in the ’285 patent are formulated for oral
administration,” claim 1 of the ‘285 patent allows for formulations that are
suitable for any other type of administration because “there are several other
types of administration for which a dosage may be formulated” including
“rectal, intravenous, intramuscular, topical, nasal, inhaled, ophthalmic,
transdermal, and subcutaneous.” Ex. 1036 ¶ 81. Neither of these
explanations convinces us that the claimed unit dosage form may be suitable
for non-oral administration. Therefore, we construe “unit dosage form” to
mean “a single entity for drug administration that is suitable for oral
administration.”
Because we construe “unit dosage form” to require suitability for oral
administration, we disagree with Petitioner that the pre-2003 applications
require formulations that are orally administered while the claims of the ’285
patent do not.
5. “coordinated release” is required
Finally, Petitioner asserts that the claims of the ’285 patent do not
require coordinated release of naproxen and esomeprazole. Pet.9, 26 (stating
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“’285 patent claims do not require a ‘coordinated release’ of all of naproxen
in the formulation” based on Petitioner’s claim construction for “comprising
. . . naproxen surrounded by a coating”).
Both the ’216 application and the specification of the ’285 patent state
that
The present invention is directed to drug dosage forms
that release an agent that raises the pH of a patient’s
gastrointestinal tract, followed by a non-steroidal anti-
inflammatory drug. The dosage form is designed so that the
NSAID is not released until the intragastric pH has been raised
to a safe level. The invention also encompasses methods of
treating patients by administering this coordinated release,
gastroprotective, antiarthritic/analgesic combination unit dosage
form to achieve pain and symptom relief with a reduced risk of
developing gastrointestinal damage such as ulcers, erosions and
hemorrhages.
Ex. 1012, 36 (Abs.) (emphasis added); Ex. 1001, Abs. (emphasis added).
Petitioner bases its assertion that the claims of the ’285 patent do not
require “coordinated release” on its incorrect construction of the claim
language to encompass a unit dosage form “that releases most of its
naproxen immediately or begins to release all of its naproxen immediately,
but at a slow rate.” Pet. 35, see id. at 35–38. As we have found, neither is a
requirement of the claims of the ’285 patent. See supra Section II.C.1.–3.
The claims of the ’285 patent do require coordinated release of naproxen and
esomeprazole.
For the reasons set forth above, Petitioner fails to convince us that the
claims of the ’285 patent are not supported by at least the ’216 application.
Therefore, the Plachetka Publication does not qualify as prior art under 35
U.S.C. § 102(b). Consequently, Petitioner has failed to establish a
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reasonable likelihood that it would prevail in showing that claims 1–4 are
unpatentable as anticipated by the Plachetka Publication.
D. Obviousness over Depui, Phillips, Lundberg, and Clissold
Petitioner contends that each of claims 1–4 is unpatentable under 35
U.S.C. § 103 as obvious over the combination of Depui, Phillips,
3
Lundberg,
and Clissold. Pet. 43–56. We begin our discussion with a brief summary of
the references before addressing the parties’ contentions.
1. Depui
Depui teaches oral pharmaceutical preparations that comprise an acid
susceptible proton pump inhibitor in combination with one or more
NSAID(s) in a fixed unit dosage form such as a tablet. Ex. 1030, 3:7–9.
Depui observes that
[s]ome anti-ulcer drugs such as proton pump inhibitors are
susceptible to degradation/transformation in acid reacting and
neutral media as mentioned above. In respect of the stability
properties, it is obvious that the one of the active substances
being a proton pump inhibitor must be protected from contact
with acidic gastric juice by an enteric coating layer.
Id. at 5:24–28. Depui teaches that the proton pump inhibitor is protected by
an enteric coating layer. Therefore, Depui teaches that its fixed unit dosage

3
Although Petitioner lists Daneshmend in the heading for this obviousness
ground, Petitioner does not discuss the reference except in the claim chart
relating to the “naproxen surrounded by a coating” limitation, where
Petitioner states that Daneshmend discloses “the pKa [disassociation
constant] of aspirin of 3.5 and explains why stomach acidity is a contributing
factor to NSAID damage.” Pet. 53; Daneshmend et al., Abolition by
Omeprazole of Aspirin Induced Gastric Mucosal Injury in Man,” 31 GUT
514–517 (1990) (Ex. 1046). We observe that its inclusion in the ground is a
clerical error when the Phillips reference that was discussed and relied upon
in supporting the ground was intended.
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form is an enteric coating layered tablet, capsule, or multiple unit tableted
dosage form. Id. at Abs.
2. Lundberg
Lundberg describes a dosage form with a core material coated with a
semipermeable membrane, which changes its permeability after a pre-
determined time, where the core material contains an active ingredient that
may be omeprazole
4
with one or more alkaline additives, and one or more
swelling agents. Ex. 1031, 3:15–19. Lundberg specifically states that the
dosage form is without an enteric coating layer. Id. at 3:12–13, 3:25–27
(“Surprisingly, the formulation according to the present invention is
prepared without an enteric coating, which previously have been almost an
axiom for dosage forms containing omeprazole or any other proton pump
inhibitor compounds.”).
Lundberg describes how the dosage form works as follows.
When the coated pellets pass the stomach small amounts of
gastric fluid will be absorbed through the semipermeable
membrane. The alkalizing agent in the core material will
neutralize the absorbed acidic fluid and protect the active
ingredient against degradation. At the same time the swelling
agent, will be exposed to the penetrating fluid or moisture, and
it will start to expand. After a predetermined time interval this
expansion leads to disruption of the superimposed
semipermeable membrane by the built-up pressure or to a
swelling that will increase the permeability of the membrane.
The time interval is to be determined so that the pellets have
had time to pass the stomach at the very moment, and have
reached the small intestines. The entire dose of the active
ingredient will then start to be released into the small intestine
where absorption can occur.

4
Omeprazole is a racemic compound where esomeprazole is its
S-enantiomer. Ex. 1036 ¶ 43.
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Ex. 1031, 4:12–22.
3. Phillips
Phillips describes a pharmaceutical composition, in an aqueous
solution/suspension or dry formulations, of a proton pump inhibitor, such as
omeprazole, in a pharmaceutically acceptable carrier including a bicarbonate
salt. Ex. 1032, 18:2–9. In Phillips’ preferred embodiment, the enteric
coating of omeprazole particles is dissolved by mixing them with a sodium
bicarbonate solution. Id. at 19:19–23.
Phillips describes the following advantages of the omeprazole
solution/suspension over enteric–coated time-release capsules: (1) a
decreased drug absorbance time; (2) the sodium bicarbonate solution
protects the omeprazole from acid degradation prior to absorption; (3) the
sodium bicarbonate acts as an antacid during absorption of the omeprazole;
and (4) the solution suspension can be administered through an existing
indwelling tube without clogging. Id. at 19:23–20:8.
4. Clissold
Clissold describes in vitro and in vivo animal studies demonstrating
that omeprazole produces long lasting inhibition of gastric acid secretion.
Ex. 1029, 17. Clissold describes a single-dose study where “omeprazole has
been administered as an alkaline (sodium bicarbonate) suspension as
uncoated granules in capsules containing sodium bicarbonate or as capsules
of enteric-coated granules.” Id. at 24. Clissold notes that “omeprazole, a
highly acid-labile compound, may increase its own relative bioavailability
by virtue of its antisecretory activity which reduces the acid degradation of
the parent molecule, consequently enhancing the extent of its absorption.”
Id. at 32.
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5. Analysis
When the claims are construed properly, it is clear that the prior art
does not teach the combination of the limitations set forth in the challenged
claims of the ’285 patent. Petitioner focuses on whether the references teach
the first limitation of the challenged claims: “esomeprazole, wherein at least
a portion of said esomeprazole is not surrounded by an enteric coating”—
and ignores the coordinated release of esomeprazole and naproxen that
“inhibits [naproxen] release from said unit dosage form unless said dosage
form is in a medium with a pH of 3.5 or higher.” See Pet. 43–53; Ex. 1001,
22:8–19 (describing a single dosage form that combines non-enteric coated
esomeprazole with naproxen surrounded by a pH sensitive coating that
inhibits its release for coordinated or sequential release of esomeprazole and
naproxen).
In particular, Petitioner’s discussion of the limitation, “naproxen
surrounded by a coating that inhibits its release from said unit dosage form
unless said dosage form is in a medium with a pH of 3.5 or higher,” is
limited to a single entry in a claim chart listing Naprosyn Physicians’ Desk
Reference and Daneshmend to support a teaching of this limitation. Pet. 53
(citing Daneshmend (Ex. 1046, 3) as disclosing the pKa of aspirin of 3.5 and
explaining why stomach acidity is a contributing factor to NSAID damage,
and Naprosyn Physicians’ Desk Reference (Ex. 1063) as disclosing that
“Naprocyn” are “enteric-coated tablets” ). Petitioner, however, does not
discuss these references or explain how one of skill in the art would combine
the teachings from these references with the other cited references to arrive
at the claimed invention.
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We also agree with Patent Owner that Petitioner has not shown from
the cited references a rationale to combine or expectation of success for the
claimed combination of coordinated release of esomeprazole and naproxen.
Id. at 30. Petitioner relies on Pilbrant and testimony of its declarant,
Dr. Kibbe, to show why one of skill in the art would combine the teachings
of the cited references to arrive at the claimed invention. Pet. 47–53.
Petitioner states:
The person of ordinary skill in the art would have had a
reasonable expectation of success because the claimed unit
dosages incorporate commonly prescribed compounds . . . . To
the extent that a correction needed to be made to the PPI dosage
due to a lack of enteric coat, the person of ordinary skill in the
art would have understood from Pilbrant’s estimation that about
half of omeprazole gets degraded, that doubling the dose would
compensate for any degradative loss of esomeprazole. The
person of ordinary skill in the art would have known about the
self-amplification of the omeprazole . . . .
Pet. 47–48 (citing Ex. 1036 ¶¶ 56–60 (Kibbe Declaration)).
Petitioner’s reliance on Pilbrant’s statement that “more than half of
the dose was lost due to degradation in the acidic stomach” to support its
motivation to combine is not supported. For instance, Dr. Kibbe states:
Even though increasing the dosage [of esomeprazole] would be
approaching the maximal FDA-approved daily amount (of the
enteric-coated form), the person of ordinary skill in the art
would have known that PPI’s are safe and have minimal side
effects and that such dosing carried little risk.
Ex. 1036 ¶ 114 (relying on references stating side effects from the
administration of omeprazole were not observed). Pilbrant does state that
without buffer protection for omeprazole, “more than half of the dose was
lost due to degradation in the acidic stomach.” Ex. 1064, 117. Instead of
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indicating a doubling of the dose of omeprazole is the answer, Pilbrant
concluded that the results “clearly show that a conventional, non-buffered,
oral dosage form [non-enteric coated] of omeprazole will have a low
systemic bioavailability owing to preabsorption degradation of omeprazole
in the stomach.” Id.
In summarizing the studies’ results, Pilbrant observed
There are two principle options for the formulation of an
oral, solid dosage form of omeprazole:
 A conventional oral dosage form from which omeprazole
is released and absorbed rapidly enough to avoid degradation in
the stomach.
 An enteric-coated dosage form, which releases
omeprazole for absorption in the small intestine.
The first option was ruled out in a pilot bioavailability
study . . . where it was shown that more than half of the
omeprazole in a rapidly dissolving dosage form degrades in the
stomach.
An enteric-coated dosage form, which does not release
the active ingredient for dissolution and absorption until it has
been transported down to the neutral reacting part of the small
intestine, offers the best possibilities. . . .
An enteric-coated dosage form of omeprazole must be
perfectly coated and acid resistant, since, if any drug leaks out
of the dosage form in the stomach, it is almost immediately
degraded. The same is the case if an acidic medium can diffuse
into the dosage form through pin-holes or damage in the
enteric-coating.
We agree with the Patent Owner that Pilbrant teaches away from the
claimed combination. Prelim. Resp. 36 (“Petitioner’s failure to
acknowledge the complete disclosure of Pilbrant, which negates any
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motivation to use the non-enterically coated form of esomeprazole, despite
the testimony of Petitioner’s own expert, is an incurable flaw in the
Petition”). When a prior art reference teaches away from combining known
elements, discovery of a successful means of combining them is more likely
to be nonobvious. See KSR Internat’l Co. v. Teleflex Inc., 550 U.S. 398, 416
(2007). A reference teaches away “when a person of ordinary skill, upon
reading the reference, would be discouraged from following the path set out
in the reference, or would be led in a direction divergent from the path that
was taken by the applicant.” In re Gurley, 27 F.3d 551, 553 (Fed. Cir.
1994), cited in In re Mouttet, 686 F.3d 1322, 1333-34 (Fed. Cir. 2012).
We disagree with Petitioner’s conclusion that although one of skill in
the art “might have believed” that enteric coated esomeprazole was
generally the better option, “that does not exclude the use of non-enteric
coated esomeprazole as still ‘good enough’ to be obvious, at least in a
combination product where all the esomeprazole needs to do is raise the
stomach pH to 3.5.” Pet. 51. Here, the very statement that Petitioner relies
upon from Pilbrant to support its rationale to combine concerning
preabsorption degradation of omeprazole caused Pilbrant to rule out the use
of conventional oral dosage forms without an enteric coating. We agree
with the Patent Owner that Petitioner’s “[m]otivation to combine in the face
of an express teaching away must be found in the prior art itself and reliance
on the teachings of the ’285 patent is impermissible hindsight.” Prelim.
Resp. 37.
III. CONCLUSION
For the foregoing reasons, we are not persuaded that the Petition
establishes a reasonable likelihood that Petitioner would prevail in showing
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any of claims 1–4 of the ’285 patent are unpatentable. Because we are not
instituting an inter partes review for any challenged claim, we need not
reach the real party-in-interest issue raised by Patent Owner. Prelim. Resp.
43–49.
IV. ORDER
Accordingly, it is
ORDERED that the Petition is denied at to all challenged claims of
the ’285 patent.
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PETITIONER:

Alan H. Pollack
Louis H. Weinstein
BUDD LARNER
apollack@buddlarner.com
lweinstein@buddlarner.com

PATENT OWNER:

Pozen Inc.

Dr. Stephen M. Hash
Dr. Margaret J. Sampson
BAKER BOTTS LLP
stephen.hash@bakerbotts.com
margaret.sampson@bakerbotts.com

Jeffrey S. Gritton
VINSON & ELKINS LLP
jgritton@velaw.com

Horizon Pharma USA, Inc.

Ricardo Rodriguez
Dr. Thomas A. Blinka
COOLEY LLP
rr@cooley.com
tblinka@cooley.com

Dennis Bennett
Dr. Lauren L. Stevens
GLOBAL PATENT GROUP, LLC
dennisbennett@globalpatentgroup.com
lstevens@globalpatentgroup.com