Trials@uspto.gov
`571-272-7822
`
`
`
`
`
`
`
`
`
` Paper 17
`
`
`
`
` Entered: September 21, 2017
`
`UNITED STATES PATENT AND TRADEMARK OFFICE
`____________
`
`BEFORE THE PATENT TRIAL AND APPEAL BOARD
`____________
`
`MYLAN PHARMACEUTICALS INC.,
`Petitioner,
`
`v.
`
`COSMO TECHNOLOGIES LIMITED,
`Patent Owner.
`
`
`Case IPR2017-01035
`Patent 9,320,716 B2
`
`
`
`
`Before SUSAN L. C. MITCHELL, ZHENYU YANG, and
`KRISTI L. R. SAWERT, Administrative Patent Judges.
`
`MITCHELL, Administrative Patent Judge.
`
`
`
`
`DECISION
`Institution of Inter Partes Review
`37 C.F.R. § 42.108
`
`
`
`
`
`

`

`IPR2017-01035
`Patent 9,320,716 B2
`
`
`I. INTRODUCTION
`Mylan Pharmaceuticals, Inc. (“Petitioner”) filed a Petition (Paper 1,
`“Pet.”) on March 9, 2017, requesting an inter partes review of claims 1–29
`of U.S. Patent No. 9,320,716 B2 (Ex. 1001, “the ’716 patent”). Cosmo
`Technologies Limited (“Patent Owner”) filed a Preliminary Response
`(Paper 8, “Prelim. Resp.”) on June 22, 2017. Institution of an inter partes
`review is authorized by statute when “the information presented in the
`petition . . . and any response . . . shows that 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); see also 37 C.F.R. §§ 42.4,
`42.108.
`Upon consideration of the information presented in the Petition and
`the Preliminary Response, we conclude that Petitioner has established a
`reasonable likelihood that it would prevail in its challenge to at least one of
`claims 1–29 of the ’716 patent. Accordingly, we institute an inter partes
`review of those claims.
`
`A. Related Proceedings
`The parties list the following cases in which the ’716 has been
`
`asserted by Patent Owner: Cosmo Technologies Limited v. Mylan
`Pharmaceuticals Inc., 16-cv-00152 (D. Del.); Cosmo Technologies Ltd v.
`Lupin Ltd., 15-cv-00669 (D. Del.); Cosmo Technologies Limited v. Alvogen
`Pine Brook, Inc., 15-cv-00193 (D. Del.); Cosmo Technologies Ltd. v. Actavis
`Laboratories FL, Inc., 15-cv-00164 (D. Del.); and Cosmo Technologies
`Limited v. Par Pharmaceutical, Inc. 15-cv-00116 (D. Del.). Pet. 2; Paper 6,
`2. In addition, concurrently with the Petition under consideration here,
`Petitioner has filed a petition challenging the claims of related U.S. Patent
`
`2
`
`

`

`IPR2017-01035
`Patent 9,320,716 B2
`
`No. 8,784,888 B2, Case No. IPR2017-01034. See Pet. 3; Paper 6, 3. The
`parties also identify several related patents. Pet. 2, Paper 6, 2.
`B. The Asserted Grounds of Unpatentability
`Petitioner asserts the challenged claims are unpatentable on the
`
`following grounds. Pet. 8. Petitioner supports its challenge with the
`Declaration of Anthony Palmieri III, Ph.D., R.Ph. (“Palmieri Declaration”)
`(Ex. 1006).
`
`Reference(s)
`
`U.S. Patent No. 5,681,5841
`
`’584 Patent
`U.S. Patent No. 5,811,3882
`’388 Patent
`’388 and ’584 Patents
`
`Basis
`
`§ 102
`§ 103
`§ 102
`§ 103
`§ 103
`
`Claims Challenged
`
`1–29
`1–29
`1–7, 9, 11–17, 19, 21–29
`1–29
`8, 10, 18, and 20
`
`
`
`C. The ’716 Patent (Ex. 1001)
`The ’716 patent, titled “Controlled Release and Taste Masking Oral
`Pharmaceutical Compositions,” describes an oral pharmaceutical
`composition with an active agent, a macroscopically homogeneous structure,
`and a gastro-resistant coating. Ex. 1001, Abst. Specifically, the
`“macroscopically homogenous structure comprises at least one hydrophilic
`compound and at least one lipophilic compound and/or at least one
`
`
`1 U.S. Patent No. 5,681,584, issued October 28, 1997, to Louis Savastano et
`al. (“’584 Patent”) (Ex. 1008).
`2 U.S. Patent No. 5,811,388, issued September 22, 1998 to David R. Friend
`and David Wong (“’388 Patent”) (Ex. 1009).
`
`3
`
`

`

`IPR2017-01035
`Patent 9,320,716 B2
`
`amphiphilic compound. The macroscopically homogeneous structure
`controls the release of the active ingredient, and the gastro-resistant film
`prevents release of the active agent in the stomach.” Id.
`The macroscopically homogeneous structure is further described as “a
`three-component matrix structure, i.e. a structure formed by successive
`amphiphilic, lipophilic or inert matrices and finally incorporated or
`dispersed in hydrophilic matrices.” Id. at 1:25–28. This structure serves the
`dual purposes of modulating the dissolution rate of the active ingredient in
`aqueous or biological fluids to control the release kinetics in the
`gastrointestinal tract, and allows for oral administration of an active agent
`that has an unpleasant taste or irritates the mucosae of the administration
`site. Id. at 29–36. Therefore, “[t]he compositions of the invention are
`characterized by the absence of a first phase in which the medicament
`superficially present on the matrix is quickly solubilized, and by the fact the
`amphiphilic layer compensate the lack of affinity of the aqueous solvent
`with the lipophilic compounds forming the inner matrix.” Id. 2:65–3:4.
`The composition having the three-component matrix structure as
`described in the ’716 Patent can be prepared using the following three steps.
`a)
`the active ingredient is first inglobated by simple
`kneading or mixing in a matrix or coating consisting of
`compounds having amphiphilic properties, which will be further
`specified below. The active principle(s) can be mixed with the
`amphiphilic compounds without the aid of solvents or with small
`amounts of water-alcoholic solvents.
`b)
`The matrix obtained in a) is incorporated in a low
`melting lipophilic excipient or mixture of excipients, while
`heating to soften and/or melt the excipient itself, which thereby
`incorporates the active ingredient by simple dispersion. After
`cooling at room temperature an inert matrix forms, which can be
`
`4
`
`

`

`IPR2017-01035
`Patent 9,320,716 B2
`
`
`reduced in size to obtain inert matrix granules containing the
`active ingredient particles.
`c)
`The inert matrix granules are subsequently mixed
`together with one or more hydrophilic water-swellable
`excipients. The mixture is then subjected to compression or
`tableting. This way, when the tablet is contacted with biological
`fluids, a high viscosity swollen layer is formed, which
`coordinates the solvent molecules and acts as a barrier to
`penetration of the aqueous fluid itself inside the new structure.
`Said barrier antagonizes the starting "burst effect" caused by the
`dissolution of the medicament inglobated inside the inert matrix,
`which is in its turn inside the hydrophilic matrix.
`Id. at 3:47–4:3.
`
`homogenous
`
`D. Illustrative Claim
`Petitioner challenges claims 1–29 of the ’716 patent. Claims 1, 12,
`and 22 are independent claims. Claim 1, reproduced below, is illustrative.
`
`1.
`A
`controlled
`release
`oral
`pharmaceutical
`composition comprising:
`
`(i)
`budesonide in an amount effective to treat intestinal
`inflammatory disease;
`
`(ii)
`a macroscopically
`comprising:
`at least one lipophilic compound and
`(a)
`
`
`at least one hydrophilic compound,
`(b)
`
`
`wherein the macroscopically homogenous structure
`
`
`controls the release of the budesonide; and
`
`(iii) a gastro-resistant coating on the macroscopically
`homogenous structure that prevents release of budesonide in the
`stomach,
`
`wherein the macroscopically homogenous structure is a
`tablet.
`Ex. 1001, 10:13–26. Claim 12 differs from claim 1 in that “at least one
`amphiphilic compound” is substituted for “at least one lipophilic
`
`structure
`
`5
`
`

`

`IPR2017-01035
`Patent 9,320,716 B2
`
`compound.” Id. at 11:4–17. Claim 22 differs from claim 1 in that
`“budesonide” and “at least one amphiphilic compound” is added to the
`“macroscopically homogenous structure” of the oral pharmaceutical
`composition. Id. 12:9–25.
`
`II. ANALYSIS
`A. Claim Construction
`In an inter partes review, claim terms in an unexpired patent are
`interpreted according to their broadest reasonable construction in light of the
`specification of the patent in which they appear. 37 C.F.R. § 42.100(b);
`Office Patent Trial Practice Guide, 77 Fed. Reg. 48,756, 48,766 (Aug. 14,
`2012); In re Cuozzo Speed Techs., LLC, 793 F.3d 1268, 1275–79 (Fed. Cir.
`2015). Under that standard, 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).
`Petitioner provides the constructions found by the District Court of
`Delaware to apply to the following terms of the ’716 patent and related
`patents: “matrix,” “macroscopically homogenous composition” or
`“macroscopically homogeneous structure,” “outer hydrophilic matrix,”
`“lipophilic matrix,” “amphiphilic matrix,” “melting point,” and
`“lipophilic/amphiphilic matrix.” Pet. 5–6 (citing Ex. 1012, 2). Petitioner
`argues that the District Court’s construction of these terms is consistent with
`their broadest reasonable interpretation, and “at the very least, the BRI
`should encompass the district court’s constructions.” Id. at 6; see Ex. 1006
`¶ 46.
`
`6
`
`

`

`IPR2017-01035
`Patent 9,320,716 B2
`
`
`Of particular concern to us to resolve issues in this proceeding for
`purposes of our Decision to Institute is the construction of the term
`“macroscopically homogenous structure.” The District Court defined this
`term as “[a] composition of uniform structure throughout, as observed by the
`naked eye.” Pet. 5 (quoting Ex. 1012, 2). Patent Owner agrees that the
`District Court’s interpretation is the broadest reasonable interpretation for
`this term. Prelim. Resp. 18. Patent Owner provides the dictionary
`definitions of “homogenous” and “macroscopic” upon which the District
`Court relied in crafting its interpretation. Id. at 18–19 (citing Ex. 2014, 555
`(defining “homogenous” as “of uniform structure of composition
`throughout”), 698 (defining “macroscopic” as “large enough to be observed
`by the naked eye”); Ex. 2015, 948 (defining “homogenous” as “uniform in
`structure of composition”), 1189 (same as previously provided definition of
`“macroscopic”). Patent Owner also asserts that this claim term was added to
`distinguish “from formulations that controlled release using a layered
`structure.” Prelim. Resp. 19. Finally, Patent Owner asserts that “[a]reas of
`different color or texture, for example due to excipients of different color,
`still fall within the scope of the claim so long as the differences are uniform
`throughout the structure.” Id.
`The ’716 Patent provides the following references to the
`“macroscopically homogeneous structure.” In describing one known
`technique of preparing a modified release form for a pharmaceutical
`composition, the ’716 Patent distinguishes a “reservoir” for an active
`ingredient created by a known technique as “not macroscopically
`homogeneous along all the symmetry axis of the final form.” Ex. 1001,
`
`7
`
`

`

`IPR2017-01035
`Patent 9,320,716 B2
`
`2:29–31; see Prelim. Resp. 19. In describing the invention of the ’716
`Patent, it is stated that:
`The compression of the mixture [or tabletting] of
`lipophilic and/or amphiphilic matrix, hydrogel-forming
`compound and, optionally, active ingredient not inglobated in the
`lipophilic matrix, yields a macroscopically homogeneous
`structure in all its volume, namely a matrix containing a
`dispersion of the lipophilic granules in a hydrophilic matrix.
`Id. at 5:5–10; see also id. at 3:62–63 (using “compression” and
`“tableting” interchangeably).
`
`The ’716 Patent’s description of a homogenous structure along all of
`the symmetry axis of the final form, in addition to the definitions of
`“macroscopic” and “homogenous,” all support the District Court’s
`interpretation of the claim term “macroscopically homogenous structure.”
`We agree with Petitioner and Patent Owner that, on this record, the broadest
`reasonable interpretation of “macroscopically homogeneous structure” at
`least includes the District Court’s interpretation of “a composition of
`uniform structure throughout, as observed by the naked eye.”
`Patent Owner proffers a construction of the term “to treat intestinal
`inflammatory disease.” Prelim. Resp. 19–21. We determine that this claim
`term requires no construction for purposes of this decision. See Vivid
`Techs., Inc. v. Am. Sci. & Eng’g, Inc., 200 F.3d 795, 803 (Fed. Cir. 1999)
`(“only those terms need be construed that are in controversy, and only to the
`extent necessary to resolve the controversy”).
`B. Principles of Law
`To establish anticipation, each and every element in a claim, arranged
`as recited in the claim, must be found in a single prior art reference. Net
`MoneyIN, Inc. v. VeriSign, Inc., 545 F.3d 1359, 1369 (Fed. Cir. 2008);
`
`8
`
`

`

`IPR2017-01035
`Patent 9,320,716 B2
`
`Karsten Mfg. Corp. v. Cleveland Golf Co., 242 F.3d 1376, 1383 (Fed. Cir.
`2001). “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 re Graves, 69 F.3d 1147, 1152 (Fed. Cir. 1995) (internal citation and
`emphasis omitted). Moreover, “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.” In re Preda,
`401 F.2d 825, 826 (CCPA 1968).
`A patent claim is unpatentable under 35 U.S.C. § 103(a) 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 of ordinary skill in the art; and (4) objective evidence of
`nonobviousness. Graham v. John Deere Co., 383 U.S. 1, 17–18 (1966).
`“Both the suggestion and the expectation of success must be founded in the
`prior art, not in the applicant’s disclosure.” In re Dow Chemical Co., 837
`F.2d 469, 473 (Fed. Cir. 1988).
`In that regard, an obviousness analysis “need not seek out precise
`teachings directed to the specific subject matter of the challenged claim, for
`a court can take account of the inferences and creative steps that a person of
`ordinary skill in the art would employ.” KSR, 550 U.S. at 418; see
`
`9
`
`

`

`IPR2017-01035
`Patent 9,320,716 B2
`
`Translogic, 504 F.3d at 1259. In KSR, the Supreme Court also stated that an
`invention may be found obvious if trying a course of conduct would have
`been obvious to a person having ordinary skill:
`When there is a design need or market pressure to solve a
`problem and there are a finite number of identified, predictable
`solutions, a person of ordinary skill has good reason to pursue
`the known options within his or her technical grasp. If this leads
`to the anticipated success, it is likely the product not of
`innovation but of ordinary skill and common sense. In that
`instance the fact that a combination was obvious to try might
`show that it was obvious under § 103.
`550 U.S. at 421. “KSR affirmed the logical inverse of this statement by
`stating that § 103 bars patentability unless ‘the improvement is more than
`the predictable use of prior art elements according to their established
`functions.’” In re Kubin, 561 F.3d 1351, 1359−60 (Fed. Cir. 2009) (citing
`KSR, 550 U.S. at 417).
`We are mindful that the level of ordinary skill in the art also is
`reflected by the prior art of record.3 See Okajima v. Bourdeau, 261 F.3d
`
`
`3 Petitioner states that the level of skill in the art at the time of the invention
`is a person who has an “education or experience in the field of drug delivery
`systems, including controlled release compositions. The education and
`experience levels may vary between POSAs, with some having a bachelor’s
`degree in the chemical or pharmaceutical arts (e.g., pharmacy or
`pharmaceutics) plus five years of relevant work experience, and others
`holding more advanced degrees—e.g., Ph.D. or Pharm.D—while having
`fewer years of experience.” Pet. 7; Ex. 1006 ¶¶ 34–35. Patent Owner does
`not offer an explicit definition for one of ordinary skill in the art. See
`generally Prelim. Resp. For purposes of this decision, we apply Petitioner’s
`stated level of ordinary skill in the art, which is supported by Dr. Palmieri,
`because of the sophistication of the technology and the educational and
`experiential level of those who work in this area. See In re GPAC, 57 F.3d
`1573, 1579 (Fed. Cir. 1995).
`
`10
`
`

`

`IPR2017-01035
`Patent 9,320,716 B2
`
`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. Overview of Asserted References
`1. ’584 Patent (Ex. 1008)
`
`The ’584 patent, titled “Controlled Release Drug Delivery Device,”
`discloses a controlled-release device for “delivering a drug . . . to a pre-
`selected region of the gastro-intestinal tract, particularly to the colon.”
`Ex. 1008, [57] Abstract. The ’584 patent teaches that controlled release of a
`drug in the colon is “beneficial for a variety of colonic diseases including
`inflammatory bowel disease.” Id. at 1:39–40.
`The ’584 patent teaches that the drug-delivery device contains: (1) a
`solid core comprising an active ingredient; (2) a “delay jacket” coated over
`the core; and (3) a semi-permeable membrane coated over the delay jacket;
`and (4) an optional enteric coating over the semi-permeable membrane. Id.
`at 5:37–44. The ’584 patent teaches that such a drug-delivery device with an
`enteric coating “resists dissolution in gastric fluid” and “thus allows for
`controlled continuous release of the active agent in the pre-selected region of
`the gastro-intestinal tract at a predetermined average rate.” Id. at 5:45–57.
`The ’584 patent explains the function of each component of the drug-
`delivery device. First, the ’584 patent explains, the enteric coating protects
`the drug delivery device from the acidic gastric fluid upon ingestion. Id. at
`11:44–46. “After the stomach pushes the device through the pylorus into the
`duodenum,” the ’584 patent continues, “the device is exposed to fluids of
`
`11
`
`

`

`IPR2017-01035
`Patent 9,320,716 B2
`
`higher pH and the enteric coating dissolves.” Id. at 11:46–48. Then, “[o]nce
`the semi-permeable membrane is exposed to these fluids, the device is
`activated.” Id. at 11:48–50. Once activated:
`Water from the gastro-intestinal tract is imbibed through the
`membrane by diffusion and begins to selectively dissolve the
`delay jacket. As the soluble components of this delay jacket are
`selectively dissolved, they are released either through the
`membrane, or through the release orifice, until they are depleted.
`The delay jacket directly under the membrane prevents water
`from reaching the active drug core, thus providing the delayed
`release of the active agent. Once the delay jacket has been
`exhausted of soluble components, a suspension of insoluble
`material held in place by the membrane, continues to surround
`the active drug core. Eventually, the active core is reached by
`the water, increasing the pressure within the membrane as the
`core osmotic agents imbibe more and more water. As the drug is
`dissolved or suspended, this hydrostatic pressure forces the
`active agent through the membrane and/or through the release
`orifice to deliver the drug at a controlled rate.
`Id. at 11:50–66.
`Turning to the structure of the drug-delivery device, the ’584 patent
`begins with the solid core. The ’584 patent explains that the solid core
`contains the active ingredient, and specifically lists budesonide as an
`example of a suitable active ingredient. Id. at 6:14, 48. The solid core, the
`’584 patent states, may also contain “other pharmaceutically acceptable
`excipients including osmotic agents, lubricants, glidants, wetting agents,
`binders, fillers, and suspending/thickening agents.” Id. at 6:15–18. The
`’584 patent explains that the lubricants, glidants, wetting agents “aid in
`dissolution of the components, binders, and suspending/thickening agents.”
`Id. at 7:48–50. As to lubricants, the ’584 patent identifies, inter alia,
`calcium stearate, magnesium stearate, and stearic acid as suitable. Id. at
`
`12
`
`

`

`IPR2017-01035
`Patent 9,320,716 B2
`
`6:51–54. And, as to wetting agents, the ’584 patent lists several suitable
`examples, such as lecithin. Id. at 7:57–8:1. Finally, as to binders, the ’584
`patent again identifies several examples, including hydroxyethyl cellulose,
`hydroxypropyl methylcellulose, and methylcellulose. Id. at 8:1–8.
`In the examples describing how the core was made, the ’584 Patent
`states that “[a]ll core components are mixed together and sized. The mixture
`is then pressed into tablet cores using conventional tableting techniques.”
`Id. at 14:54–56, 15:56–58; see also id. at 13:13–17 (describing making of
`core by mixing together metoprolol fumaratic and povidone and granulating
`with an aqueous alcohol solution; drying and sizing the granulation and
`blending with magnesium sterate; and compressing the dried lubricated
`powder into tablet cores using conventional tableting techniques).
`2. ’388 Patent (Ex. 1009)
`The ’388 Patent describes “[p]harmaceutical compositions for orally
`delivering a therapeutically effective amount of a drug to the colon without
`significant release of the drug in the upper GI tract after oral administration,”
`and particularly preparing such a composition as a tablet. Ex. 1009, Abst.
`More particularly, the ’388 Patent states that
`The compositions of this invention are based on the observation
`that by carefully controlling the percentage of a hydrocolloid
`obtainable from a higher plant at a very high level in an orally-
`administered dosage form and combining it with a suitable
`excipient and a particular family of drugs at low concentrations
`(i.e., less than about 10% by weight), a composition can be
`obtained which traverses the upper GI tract without releasing any
`significant amount of drug, but when it reaches the lower GI
`tract, e.g. the colon, the drug is preferentially released due at least
`in part to the action of the enzymatic environment in the lower
`GI tract that attacks the hydrocolloid to release the drug.
`Id. at 4:49–60.
`
`13
`
`

`

`IPR2017-01035
`Patent 9,320,716 B2
`
`
`Such pharmaceutical compositions are described as useful for treating
`lower gastrointestinal disorders, particularly chronic inflammatory diseases
`of the colon. Id. at 2:58–66, 3:10–15; 8:13–17. A specific active ingredient
`deemed useful for such treatment is budesonide. Id. at 8:25–48; 8:54–56
`(stating budesonide is a preferred active ingredient). One such
`pharmaceutical composition is an orally-deliverable tablet having an inner
`composition optionally surrounded by a pharmaceutically-acceptable
`coating. Id. at 5:23–25.
`The solid tablet of this invention is designed to take
`advantage of
`(1) the protective characteristics of
`the
`hydrocolloid obtainable from higher plants in the upper GI and
`(2) the disintegrative characteristics of the hydrocolloid in the
`lower GI. Thus, the inner composition of the tablet may be one
`of several designs: (a) it may be a matrix of a therapeutically
`effective amount of the active ingredient uniformly dispersed
`throughout in combination with a high percentage of the
`hydrocolloid and a generally lesser amount of other excipients;
`(b) it may have a core, in which the active ingredient is
`concentrated, surrounded by a layer of material that is free of the
`active ingredient and that has a high percentage of the
`hydrocolloid and a generally lesser amount of other excipients;
`(c) it may have a concentration gradient of the active ingredient
`such that there is a greater amount in the core of the tablet with
`lesser amounts in multiple layers surrounding the core and very
`little or no active ingredient in the outer layer. Whether the
`design of the tablet is that of (a), (b) or (c) above, the specificity
`for regional delivery to the lower GI, especially the colon, is
`enhanced by enterically coating the tablet with an appropriate
`enteric coating material.
`Ex. 1009, 5:44–65; see also id. at 15:8–11 (describing one design for the
`pharmaceutical composition as a “tablet which is a uniform matrix”).
`
`14
`
`

`

`IPR2017-01035
`Patent 9,320,716 B2
`
`
`
`The ’388 Patent describes the purpose of adding excipients is to:
`(1)
`impart
`satisfactory
`processing
`and
`compression
`characteristics to the composition (e.g., adjust the flowability,
`cohesion and other characteristics of the composition) and (2)
`give additional desirable physical characteristics to the tablets
`(e.g. color, stability, hardness, disintegration). Mostly the
`excipients aid in the delayed release of the drug from the
`composition to achieve regional delivery to the lower GI.
`Id. at 11:23–31. These excipients may include lubricants, binders, and
`diluents. Id. at 11:33–37.
`D. Asserted Anticipation by or Obviousness Over the ’584 Patent
`Petitioner provides a detailed description and claim charts to show
`where the ’584 Patent discloses each and every limitation of claims 1–29 to
`support its anticipation challenge. Pet. 9–22. Specifically, Petitioner asserts
`that
`
`The ’584 patent teaches a drug delivery device comprising four
`components: (a) a solid core comprising an active agent; (b) a
`delay jacket coated over the core; (c) a semi-permeable
`membrane coated over the delay jacket; and (d) an enteric
`coating over the semi-permeable membrane. Thus, in a single
`disclosure, the ’584 patent described a controlled release drug
`delivery device with certain classes of excipients.
`Pet. 17 (citing Ex. 1008, 5:37–44; Ex. 1006 ¶¶ 57, 163–64). Petitioner
`asserts that one of skill in the art does not have to resort to impermissible
`picking and choosing among the various possibilities to arrive at the claimed
`combination, and the claims are anticipated. See Pet. 17–18.
`
`In support of its obviousness challenge based on the ’584 Patent,
`Petitioner generally contends that controlled-release pharmaceutical
`compositions containing budesonide for the treatment of intestinal
`inflammatory diseases were well known in the art. See generally Pet. 23.
`
`15
`
`

`

`IPR2017-01035
`Patent 9,320,716 B2
`
`Petitioner also generally contends that excipients such as hydrophilic
`compounds, lipophilic compounds, and amphiphilic compounds were also
`well known in the art, as was the use of gastro-resistant coatings and matrix
`compositions. Id. at 23–24. Petitioner then explains how the challenged
`claims also would have been obvious in view of the teachings of the ’584
`patent. Id. at 24–37.
`Petitioner concludes that
`Considering that the teachings of the ’584 patent alone render
`obvious the claims of the ’716 patent, a POSA would have had a
`reasonable expectation of success. A POSA would have been
`able to combine these well-known classes of excipients in
`formulating an oral composition of budesonide according to
`known principles and techniques, and would have expected to
`obtain a usable formulation with a reasonable expectation of
`success. Such a result would have been predictable because of
`the conventional use of the claimed classes of excipients. The
`’716 patent itself admits that these classes of excipients were
`known, which is consistent with what a POSA would have
`expected.
`Id. at 35–37 (citing Ex. 1001, 1:47-2:55; EX1006, ¶ 94).4
`
`4 We disagree with Petitioner’s assertion that the Patent Owner bears
`the initial burden of showing that an ordinarily skilled artisan “would have
`had no reasonable expectation of success.” Pet. 38 n.11 (quotation and
`emphasis omitted). Petitioner is reminded that “[i]n an inter partes review,
`the burden of persuasion is on the petitioner to prove unpatentability by a
`preponderance of the evidence, and that burden never shifts to the patentee.”
`In re Magnum Oil Tools Int’l, 829 F.3d 1364, 1375 (Fed. Cir. 2016)
`(quotation and citation omitted). Petitioner’s assertion that the Board held in
`Par Pharmaceutical, Inc. v. Novartis AG, Case IPR2016-01479, slip op. at
`11 (PTAB. Feb. 15, 2017), that the “Patent Owner bears the burden at the
`initial stage” is not well taken. Pet. 27 n.11. In that case, the Board
`instituted trial because it found that the Petitioner had “set forth sufficient
`evidence that a person of ordinary skill, viewing [the prior art] in
`combination, would have had a reasonable expectation of success.” Par
`
`16
`
`

`

`IPR2017-01035
`Patent 9,320,716 B2
`
`
`Patent Owner responds that the ’584 Patent does not disclose every
`claim limitation of each challenged claim to render any challenged claim
`anticipated or obvious. Prelim. Resp. 21–48.
`We have reviewed the parties’ contentions and supporting evidence.
`Given the evidence on this record, we determine that Petitioner has
`demonstrated a reasonable likelihood of prevailing on its assertion that at
`least independent claims 1, 12, and 22 are unpatentable as anticipated by or
`would have been obvious over the ’584 patent.
`We find that Petitioner has shown sufficiently that all of the
`limitations of these claims are taught by the ’584 Patent. We also find on
`this record that Petitioner has shown sufficiently that the ’584 Patent teaches
`these limitations arranged as in the claim because the ’584 Patent teaches
`that all of the claimed compounds may be used in its core component.
`Patent Owner’s argument that the ’584 Patent does not specifically disclose
`the claimed combination of compounds in a particular example is not
`persuasive on this record because we do not find that the number of
`categories and components disclosed in the ’584 Patent is so large that the
`claimed combination would not be immediately apparent to a skilled artisan,
`especially in light of the broad categories of components claimed. See
`Kennametal, Inc. v. Ingersoll Cutting Tool Co., 780 F.3d 1376, 1381–83
`(Fed. Cir. 2015).
`
`
`Pharm. slip op. at 11. That the Board could not conclude that a person of
`ordinary skill would have had no reasonable expectation of success at that
`point in the proceeding does not equate to placing an initial burden on the
`Patent Owner.
`
`17
`
`

`

`IPR2017-01035
`Patent 9,320,716 B2
`
`
`Our analysis focuses on the deficiencies alleged by Patent Owner as to
`independent claims 1, 12, and 22.
`
`Patent Owner asserts that the novel feature of its claimed
`formulation—“a ‘macroscopically homogenous structure’ comprising a
`hydrophilic, lipophilic and/or amphiphilic compound ‘wherein the
`macroscopically homogenous structure controls the release of the
`budesonide’”—creates an “extraordinary drug-release profile” where
`budesonide is delivered throughout the whole colon. Prelim. Resp. 2–3.
`Patent Owner posits that the ’584 Patent does not teach this claimed feature.
`Id. at 3, 22.
`
`1. Macroscopically Homogenous Structure
`Patent Owner asserts that Petitioner’s reliance on the ’584 disclosure
`alone, specifically Example 1 of the ’584 Patent, to show that it teaches a
`macroscopically homogenous structure is insufficient. Prelim. Resp. 26.
`Patent Owner provides a list of factors that may influence homogeneity
`including mixing time, particle size and density, interactions between
`different particles, the type of mixing equipment, whether a mixture is
`moved to different equipment during processing, the relative quantities of
`ingredients, or that some materials may require further steps to obtain a
`homogenous blend such as “geometric dilution” or comilling. Id. at 27–32.
`Patent Owner concludes that “[u]ltimately, determining whether a resulting
`tablet is macroscopically homogenous requires a detailed review of the
`manufacturing process and excipients involved, as for example might be
`found in an FDA-approval application.” Id. at 30.
`Petitioner relies on statements in the ’584 Patent that “[a]ll core
`components are mixed together,” in addition to its ref