UNITED STATES PATENT AND TRADEMARK OFFICE
`__________________
`
`BEFORE THE PATENT TRIAL AND APPEAL BOARD
`__________________
`
`Mr. J Kyle Bass and Mr. Erich Spangenberg,
`Petitioners
`
`
`v.
`
`
` ALPEX PHARMA
`Patent Owner
`
`________
`
`Patent No. 8,440,170
`Issued: May 14, 2013
`Filed: PCT January 30, 2009
`Inventors: F. Stroppolo and S. Ardalan
`Title: “Orally Disintegrating Tablets with Speckled Appearance”
`____________________
`
`Inter Parties Review No.— IPR2016-00245
`
`
`
`__________________
`
`
`
`CORRECTED PETITION FOR INTER PARTES REVIEW OF
`U.S. PATENTNO. 8,44,170
`AND MANDATORY NOTICES UNDER 37 C.F.R. § 42.8
`
`
`
`
`
`
`
`
`
`
`
`

`
`U.S. Patent No. 8,440,170
`
`TABLE OF CONTENTS
`
`
`I. INTRODUCTION ............................................................................................. 1
`
`II. GROUNDS FOR STANDING .......................................................................... 1
`
`III. MANDATORY NOTICES ............................................................................... 1
`A. Real Party-In-Interest .............................................................................. 1
`Notice of Related Matters ........................................................................ 2
`B.
`Lead and Backup Counsel ....................................................................... 2
`C.
`Service Information .................................................................................. 2
`D.
`Payment of Fees ........................................................................................ 3
`E.
`
`IV. THRESHOLD REQUIREMENT FOR INTER PARTES REVIEW ........... 3
`
`V. IDENTIFICATION OF CHALLENGE .......................................................... 3
`A. Overview of the ‘170 Patent..................................................................... 3
`The ‘170 Specification ......................................................................... 3
`1.
`The ‘170 Patent Claims ....................................................................... 4
`2.
`Prosecution History of the ‘170 Patent .............................................. 5
`B.
`
`VI. LEVEL OF SKILL IN THE ART ................................................................... 7
`
`VII.
`A.
`B.
`C.
`
`CLAIM CONSTRUCTION ..................................................................... 8
`“speckled appearance” ............................................................................. 8
`“colored granules” .................................................................................... 9
`“pharmaceutically acceptable carrier” .................................................. 9
`
`VIII.
`
`DETAILED EXPLANATION OF THE CHALLENGE .................... 10
`
`IX. GROUND 1: CLAIMS 1-9 OF THE ‘170 PATENT ARE
`UNPATENTABLE AS OBVIOUS OVER THE PREVACID LABEL
`IN VIEW OF STAWSKI UNDER 35 U.S.C. § 103. ...................................... 11
`
`
`
`X. GROUND 2: CLAIMS 1-3, 5, 6, 8, AND 9 OF THE ‘170 PATENT
`ARE UNPATENTABLE AS OBVIOUS OVER THE PREVACID
`LABEL IN VIEW OF SERPELLONI UNDER 35 U.S.C. § 103. ................. 23
`
`XI. SECONDARY CONSIDERATIONS DO NOT REBUT THE
`PRIMA FACIE CASE; THERE ARE NO UNEXPECTED
`RESULTS OVER THE CLOSEST PRIOR ART ........................................ 31
`
`
`
`ii
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`

`
`XII.
`
`CONCLUSION ..................................................................................... 333
`
`TABLE OF EXHIBITS ......................................................................................... 34
`
`U.S. Patent No. 8,440,170
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`
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`
`iii
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`

`
`U.S. Patent No. 8,440,170
`
`
`CASES
`
`TABLE OF AUTHORITIES
`
`Alcon Research, Ltd. v. Apotex Inc.,
`687 F.3d 1362, 1369 (Fed. Cir. 2012), cert denied, 133 S. Ct. 1736 (2013) .......12
`
`Graham v. John Deere Co.,
`383 U.S. 1, 17-18 (1966) ......................................................................................11
`
`In re Cuozzo Speed Techs., LLC,
`No. 2014-1301, 2015 U.S. App. LEXIS 1699, Slip. Op. at 21 (Fed. Cir. Feb. 4,
`2015) ....................................................................................................................... 7
`
`KSR Int'l Co. v. Teleflex Inc.,
`550 U.S. 398, 406-07 (2007) ......................................................................... 11, 26
`
`Par Pharm. Inc. v. TWI Pharms., Inc.,
`773 F.3d 1186, No. 2014-1391, 2014 U.S. App. LEXIS 22737, at *24 (Fed. Cir.
`Dec. 3, 2014) ........................................................................................................12
`
`
`
`
`
`iv
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`

`
`U.S. Patent No. 8,440,170
`
`RULES
`
`35 U.S.C. § 314(a) ..................................................................................................... 3
`
`37 C.F.R. § 42.100(b) ................................................................................................ 7
`
`37 C.F.R. § 42.8(b)(1) ................................................................................................ 1
`
`37 C.F.R. §§ 42.103(a) and 42.15(a) ......................................................................... 3
`
`
`
`
`
`v
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`

`
`U.S. Patent No. 8,440,170
`
`I.
`
`Introduction
`
`Mr. J Kyle Bass and Mr. Erich Spangenberg ("Petitioner") requests inter
`
`partes review (“IPR”) of claims 1 - 9 of U.S. Patent No. 8,440,170 ("the '170
`
`Patent") (Exhibit 1001).1
`
`
`
`II. Grounds for Standing
`
`Petitioner certifies that the patent for which review is sought is available for
`
`inter partes review, and that Petitioner is not barred or estopped from requesting an
`
`inter partes review on the grounds identified in the petition.
`
`
`
`III. Mandatory Notices
`A. Real Party-In-Interest
`
`Pursuant to 37 C.F.R. § 42.8(b)(1), Petitioner certifies that Mr. Erich
`
`Spangenberg and Mr. J Kyle Bass are the real parties in interest (collectively,
`
`“RPI”). No other person has authority to direct or control (i) the timing of, filing
`
`of, content of, or any decisions or other activities relating to this Petition or (ii) any
`
`
`1 The ‘170 Patent supports the US FDA Orange Book listing of Suprenza. The
`
`front page of the Suprenza website states that: “Suprenza is a registered trademark
`
`of Citius Pharmaceuticals, LLC. Marketed by Prenzamax, LLC. Distributed by
`
`Akrimax Pharmaceuticals, LLC.” (Exhibit 1016)
`
`1
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`

`
`U.S. Patent No. 8,440,170
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`timing, future filings, content of, or any decisions or other activities relating to the
`
`future proceedings related to this Petition. All of the costs associated with this
`
`Petition are expected to be borne by Mr. Erich Spangenberg and Mr. J Kyle Bass.
`
`None of the RPI has any financial interest in any securities of Alpex Pharma or
`
`Citius Pharmaceuticals.
`
`
`
`B. Notice of Related Matters
`
`Petitioner is unaware of any other matter related to the ‘170 Patent.
`
`
`
`C. Lead and Backup Counsel
`
`Lead Counsel:
`Dr. Gregory J. Gonsalves
`Reg. No. 43,639
`2216 Beacon Lane
`Falls Church, VA 22043
`(571) 419-7252
`gonsalves@gonsalveslawfirm.com
`
`Backup Counsel:
`Christopher Casieri
`McNeely, Hare & War LLP
`12 Roszel Road, Suite C104
`Princeton, NJ 08540
`Phone: 609 731 3668
`chris@miplaw.com
`
`
`
`
`
`
`
`
`D. Service Information
`
`Please address all correspondence to the lead and backup counsel at the
`
`addresses shown above. Petitioner also consents to electronic service by e-mail at:
`
`gonsalves@gonsalveslawfirm.com and tmeagher@meagheremanuel.com.
`
`
`
`2
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`

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`U.S. Patent No. 8,440,170
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`E. Payment of Fees
`
`
`
`The required fees are submitted herewith in accordance with 37 C.F.R. §§
`
`42.103(a) and 42.15(a). If any additional fees are due during this proceeding, the
`
`Office is authorized to charge such fees to Deposit Account No. 506831.
`
`
`IV. Threshold Requirement for Inter Partes Review
`
`A petition for inter partes review must demonstrate "a reasonable
`
`likelihood that the petitioner would prevail with respect to at least one of the
`
`claims challenged in the petition." 35 U.S.C. § 314(a). This Petition meets that
`
`threshold. All of the elements of claims 1-9 of the ‘170 Patent are taught or
`
`suggested in the prior art, as explained below in the proposed grounds of
`
`unpatentability.
`
`
`
`V.
`
`Identification of Challenge
`
`A. Overview of the ‘170 Patent
`
`1. The ‘170 Specification
`
`The ‘170 Patent is directed “to orally disintegrating tablets with speckled
`
`appearance” (Ex. 1001 abstract; col 1:14-16). The reasons given for patenting a
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`speckled pill are focused on their supposed “identification by physicians, nurses
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`3
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`U.S. Patent No. 8,440,170
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`and patients” (id.) though such is not claimed by the inventors. The ‘170 Patent
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`describes colored granules and excipients used to make the “speckled appearance”
`
`of the tablets (Ex. 1001 col 3:44-46). As explained by Dr. Park, “[t]he ‘170 Patent
`
`makes no claim as to the active pharmaceutical ingredient (API) useful in the so-
`
`called invention, listing hundreds of active ingredients that could be used with the
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`speckled tablet in a laundry list stretching almost four full columns of the patent.”
`
`(Ex. 1002, ¶ 11 citing Ex. 1001 col 3: 48 – col 7:27).
`
`
`
`2. The ‘170 Patent Claims
`
`The ‘170 Patent has nine claims with all of claims 2-8 depending from the
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`only independent claim, claim 1:
`
`1.
`
`An orally disintegrating tablets [sic] with speckled appearance
`
`comprising (a) speckles comprising colored granules of a water-soluble sugar, and
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`(b) a pharmaceutically acceptable carrier.
`
`Claims 2-4 limit the “water soluble sugar” to the well-known sugars sucrose,
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`sorbitol, mannitol, xylitol, or fructose.
`
`Claims 5-7 limit the colored granules to sizes ranging from 10 µm to about
`
`1200 µm.
`
`Claims 8 and 9 limit the colored granules to about 0.1% w/w to about 50%
`
`w/w per tablet.
`
`4
`
`

`
`As will be seen, none of the claims are novel or non-obvious in light of the
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`U.S. Patent No. 8,440,170
`
`prior art.
`
`
`
`B. Prosecution History of the ‘170 Patent
`
`The application that issued as the ‘170 Patent is National Stage Entry
`
`PCT/EP09/51055 filed on January 30, 2009 with 11 original claims. The
`
`application claimed priority to a provisional application (61/026,249) filed on
`
`February 5, 2008.
`
`A Restriction Requirement was mailed on October 19, 2011 which divided
`
`the original claims into two groups: Group I claims 1-9 and Group II claims 10-11.
`
`A Reply to Restriction was filed on November 10, 2011 (Exhibit 1007). The
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`Applicant chose Group I, claims 1-9, which were claims drawn to orally
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`disintegrating tablets with a speckled appearance comprising colored granules of a
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`water-soluble sugar in admixture with a pharmaceutically acceptable carrier.
`
`A non-final Office Action was mailed February 14, 2012 (Exhibit 1008) in
`
`which the Examiner rejected claims 1-4 and 8 as anticipated by and claims 1-4 and
`
`8-9 as obvious over Martino et al. (US 2003/0180357) (Id.). The Examiner also
`
`rejected all of claims 1-9 as obvious over Martino et al. (US 2003/0180357), in
`
`view of Pettersson et al. (US 2004/0213855).
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`5
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`U.S. Patent No. 8,440,170
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`In a response dated May 14, 2012, Applicants argued that Martino does not
`
`teach colored granules of a water soluble sugar and that the speckled appearance of
`
`Martino was due to an “aqueous coating composition comprising gellan gum.” (Ex.
`
`1009)
`
`The Office then issued a Final Rejection on September 12, 2012 for all
`
`claims for essentially the same reasons as before, and emphasized “the claim only
`
`requires a speckled appearance and does not require the speckles to comprise
`
`colored sugar granules” (Ex. 1010 pg. 7) hence “the argument [proferred above by
`
`Applicant] is not material to the instant rejection because, as indicated in the above
`
`rejection, the teachings of Martino et al. are relied upon for the claim 1 limitations
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`of "colored granules of a water-soluble sugar"” (Id.)
`
`The Applicant submitted a Reply to Rejection on December 12, 2012
`
`amending claim 1 to provide “that the speckles are attributable to the colored
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`granules of water-soluble sugar” and stating “Martino is a ‘homogenous mixture of
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`mannitol and dye,’ not colored granules of a water-soluble sugar.” (Ex. 1011 pg. 4)
`
`A Notice of Allowance was issued on March 20, 2013 in which the
`
`Examiner states “[t]he prior art fails to teach or reasonably suggest an orally
`
`disintegrating tablet, wherein colored granules of sugar provide a speckled
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`appearance” and further states that “the speckles [of Martino] comprise solid
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`6
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`U.S. Patent No. 8,440,170
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`particles of dye ([0061]) and not colored granules of a water-soluble sugar.” (Ex.
`
`1012)
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`It is clear from the Reasons for Allowance that the Examiner failed to
`
`consider the claims in comparison to the vast amount of prior art directed to
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`colored sugar particles useful for imparting a speckled appearance in a
`
`pharmaceutical composition. Not only were “colored granules of a water-soluble
`
`sugar” well known in the art, but that they were even commercially available and
`
`known to be useful to add to pharmaceutical compositions to attain “contrasting
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`colors” from the tablet body.
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`
`
`VI. Level of Skill in the Art
`
`The level of skill in the art is apparent from the cited art. As explained by
`
`Dr. Park, “[a] person having ordinary skill in the art would have either a Pharm. D.
`
`or a Ph.D. in organic chemistry, pharmacy, pharmacology, or a related discipline;
`
`or a Bachelor’s or Master’s degree in organic chemistry or a related field with
`
`about four years of experience relating to formulation of compounds. A person of
`
`ordinary skill in the art may have collaborated with others having expertise in, for
`
`example, methods of treating diseases and administering medicines.” (Ex. 1002, ¶
`
`9).
`
`
`
`7
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`

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`U.S. Patent No. 8,440,170
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`VII. Claim Construction
`
`In inter partes review, a claim term is given its "broadest reasonable
`
`construction in light of the specification." See 37 C.F.R. § 42.100(b); see also In re
`
`Cuozzo Speed Techs., LLC, No. 2014-1301, 2015 U.S. App. LEXIS 1699, Slip. Op.
`
`at 21 (Fed. Cir. Feb. 4, 2015). Unless otherwise specified, all terms are to be given
`
`their broadest reasonable interpretation as well as their normal and customary
`
`meaning.
`
`
`
`A. “speckled appearance”
`
`“Speckled” is generally meant as “covered or marked with small spots or
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`patches of color” while “appearance” means “the way something looks”, hence a
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`“speckled appearance” should mean, with regard to a pharmaceutical tablet, a
`
`tablet that “has the look of being covered with small spots or patches of color.”
`
`This construction is the broadest reasonable interpretation in light of the
`
`specification. The term “speckled” is defined as “[d]otted or coated with speckles,
`
`esp. flecked with small spots of contrasting colors.” (Ex. 1015, p. 1307).
`
`Similarly, the Specification of the ‘170 Patent describes a speckled appearance as
`
`“a bicolored appearance characterized by the presence of spots of a different color
`
`on their surface can be easily identified by users.” (Ex. 1001, col. 1, l. 65 – col. 2,
`
`l. 1).
`
`
`
`8
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`

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`U.S. Patent No. 8,440,170
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`B. “colored granules”
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`The term “colored” means “having or having been given a color” while the
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`term “granule” means “a small particle”. The ‘170 Patent defines preferable
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`particle sizes of from about 10 µm to about 1200 µm. Therefore, for the purposes
`
`of this IPR, “colored granules” is defined as “small particles of a size from about
`
`10 µm to about 1200 µm having or having been given color.”
`
`This construction is the broadest reasonable interpretation in light of the
`
`specification. The term “colored” is defined as “[h]aving color.” (Ex. 1015, p.
`
`276). The term “granule” is defined as “[a] small grain or pellet, a particle.” (Ex.
`
`1015, p. 593). Similarly, the Specification of the ‘170 Patent explicitly defines
`
`“colored granules” as “granules of a color different from the color of the tablet.”
`
`(Ex. 1001, col. 2, l. 29). The Specification further states that “the colored granules
`
`used in the ODT [orally disintegrating tablet] of the present invention have a
`
`particle size from about 10 μm to about 1200 μm.” (Id., col. 2, ll. 55-56).
`
`C. “pharmaceutically acceptable carrier”
`
`The term “pharmaceutically acceptable carrier” is not described nor defined
`
`in the specification of the ‘170 Patent. However, as explained by Dr. Park, “it is
`
`well known and accepted that a ‘pharmaceutically acceptable carrier’ is generally
`
`known as an excipient that can be included in a pharmaceutical compositions and
`
`that causes no significant adverse toxicological effects to a patient.” (Ex. 1002, ¶
`
`9
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`

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`U.S. Patent No. 8,440,170
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`13). Accordingly, the term “pharmaceutically acceptable carrier” should be
`
`construed to mean “a substance that can be included in the compositions of the
`
`invention and that causes no significant adverse toxicological effects to a patient.”
`
`
`
`VIII. Detailed Explanation of the Challenge
`
`Petitioner relies on the following prior art to support its grounds of challenge
`
`to claims 1-9 of the ‘170 Patent in this Petition:
`
`1. PREVACID® (lansoprazole) Delayed-Release Capsules; PREVACID®
`
`(lansoprazole) For Delayed-Release Oral Suspension; PREVACID®
`
`SoluTab™ (lansoprazole) Delayed-Release Orally Disintegrating Tablets
`
`(Ex. 1004 hereafter “the Prevacid Label”) TAP Pharmaceuticals, Lake
`
`Forest Il, 60045 USA, 102-004-R26 June 2007. The Prevacid Label is
`
`prior art to the ‘170 Patent under at least 35 U.S.C. § 102(a) (pre-AIA)
`
`because it was published in June 2007, less than one year prior to
`
`February 5, 2008, the earliest possible effective filing date for the claims
`
`of the ‘170 Patent. The Prevacid Label was not before the examiner
`
`during prosecution of the ‘170 Patent.
`
`2. US 2006/0193909 to Stawski et al. entitled “Breath Freshening Presses
`
`Tablets and Methods of Making and Using Same” Published August 31,
`
`2006. (Ex. 1005 hereafter “Stawski”). Stawski is prior art to the ‘170
`
`10
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`

`
`U.S. Patent No. 8,440,170
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`Patent under at least 35 U.S.C. § 102(b) (pre-AIA) because it was
`
`published in 2006, more than one year prior to February 5, 2008, the
`
`earliest possible effective filing date for the claims of the ‘170 Patent.
`
`Stawski was not before the examiner during prosecution of the ‘170
`
`Patent.
`
`3. US 4,744,991 to Serpelloni entitled “Speckled Sugarless Chewing-Gum
`
`and Process for its Manufacture” issued May 17, 1988. (Ex. 1006
`
`hereafter “Serpelloni”) Serpelloni is prior art to the ‘170 Patent under at
`
`least 35 U.S.C. § 102(b) (pre-AIA) because it was issued in 1988, more
`
`than one year prior to February 5, 2008, the earliest possible effective
`
`filing date for the claims of the ‘170 Patent. Serpelloni was not before the
`
`examiner during prosecution of the ‘170 Patent.
`
`Petitioner requests that claims 1-9 of the ‘170 Patent be held unpatentable
`
`based on the following grounds:
`
`Ground 1. Claims 1-9 of the ‘170 Patent are unpatentable as obvious over
`
`the Prevacid Label in view of Stawski under 35 U.S.C. § 103.
`
`Ground 2. Claims 1-3, 5, 6, 8, and 9 of the ‘170 Patent are unpatentable as
`
`obvious over the Prevacid Label in view of Serpelloni under 35 U.S.C. § 103.
`
`
`
`IX. Ground 1: Claims 1-9 of the ‘170 Patent are unpatentable as
`
`11
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`U.S. Patent No. 8,440,170
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`obvious over the Prevacid Label in view of Stawski under 35 U.S.C.
`§ 103.
`
`The obviousness inquiry is a question of law based on four factual
`
`predicates: (1) "the scope and content of the prior art," (2) the "differences between
`
`the prior art and the claims at issue," (3) "the level of ordinary skill in the pertinent
`
`art," and (4) "secondary considerations" such as "commercial success, long felt but
`
`unsolved needs, failure of others, etc." KSR Int'l Co. v. Teleflex Inc., 550 U.S. 398,
`
`406-07 (2007) (citing Graham v. John Deere Co., 383 U.S. 1, 17-18 (1966)); 35
`
`U.S.C. § 103(a). KSR reaffirmed that "[t]he combination of familiar elements
`
`according to known methods is likely to be obvious when it does no more than
`
`yield predictable results." KSR, 550 U.S. at 416.
`
`"Motivation to combine may be found in many different places and forms."
`
`Par Pharm. Inc. v. TWI Pharms., Inc., 773 F.3d 1186, No. 2014-1391, 2014 U.S.
`
`App. LEXIS 22737, at *24 (Fed. Cir. Dec. 3, 2014) (citations omitted). Thus, for
`
`example, a challenger is not limited to the same motivation that the patentee had.
`
`Id. (citing Alcon Research, Ltd. v. Apotex Inc., 687 F.3d 1362, 1369 (Fed. Cir.
`
`2012), cert denied, 133 S. Ct. 1736 (2013)).
`
`
`
`A. Independent Claim 1.
`i. An orally disintegrating tablets [sic] with speckled
`appearance
`
`12
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`

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`U.S. Patent No. 8,440,170
`
`The preamble to claim 1 claims “An orally disintegrating tablets [sic] with
`
`speckled appearance”. The Prevacid Label specifically discloses an orally
`
`disintegrating tablet with speckled appearance. (Ex. 1004 pg. 10 “PREVACID
`
`SoluTab Delayed-Release Orally Disintegrating Tablets, 15 mg, are white to
`
`yellowish white uncoated tablets with orange to dark brown speckles”)2.
`
`ii. (a) speckles comprising colored granules of a water-
`soluble sugar
`
`Element (a) of claim 1 claims “speckles comprising colored granules of a
`
`water-soluble sugar”. The Prevacid Label teaches speckles comprising colored
`
`granules (Ex. 1004 pg. 10 “with orange to dark brown speckles”) and tablets
`
`containing water soluble sugars (Ex. 1004 e.g. pg. 1 “mannitol”) but does not
`
`specifically disclose speckles comprising colored granules of a water-soluble
`
`sugar. As explained by Dr. Park, however, “speckles comprising colored granules
`
`
`2 For reference, a picture of two Prevacid tablets from the website
`
`http://www.drugs.com/cdi/prevacid-solutab-orally-disintegrating-tablets.html (Ex.
`
`1013) shows the orally disintegrating tablet with a speckled appearance:
`
`
`
`
`
`13
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`U.S. Patent No. 8,440,170
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`of water-soluble sugar were well-known in the art at the time of the invention.”
`
`(Ex. 1002, ¶ 16).
`
`A preferred embodiment disclosed by Stawski teaches granules of a water-
`
`soluble sugar in tablets.
`
`Pressed tablet 70 shown in FIG. 8 does not have distinct
`
`layers, and may be formed all of one composition. The
`
`composition comprises abrasive inclusions 75 to provide
`
`an abrasive surface opposite the generally domed top
`
`surface on the tablet. The abrasive inclusions in this
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`embodiment comprise solid matrices of carbohydrates,
`
`solid matrices of polyols, extruded carbohydrates or
`
`extruded polyols, and also carry a flavor. (Ex. 1005 para
`
`[0063])
`
`
`
`Stawski, goes on to further teach the granules of a water-soluble sugar in the
`
`tablets (“abrasive granules”) further comprise colored granules of a water-soluble
`
`sugar:
`
`The abrasive inclusions may be made from a number of
`
`different materials, including crystalline sugars or polyols;
`
`solid matrices of carbohydrates, polyols or mixtures; or
`
`extruded carbohydrates, polyols, or mixtures; … . On the
`
`one hand, solid matrices (such as from fluid bed coating or
`
`spray drying) and extruded carbohydrates or polyols are
`
`preferred because these inclusions may also contain
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`14
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`U.S. Patent No. 8,440,170
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`flavors and/or colors. When the inclusions include colors,
`
`the abrasive particles may have a contrasting color from
`
`the remainder of the compressible composition into which
`
`they are added. (Ex. 1005 para [0085]; Examples 3 A-H;
`
`emphasis added)
`
`
`
`Stawski specifically states “[t]he abrasive inclusions can include encapsulated or
`
`entrapped favors and colors. They can also be hard crystals of sugars or polyols,
`
`such as crystalline maltitol.” (Ex. 1005 para [0099]) and “[t]he Palatinit inclusions
`
`[hydrogenated isomaltulose] in the above Examples 3 A-H are replaced with blue
`
`colored mannitol inclusions (Roquette Pearlitol 500DC).” (Ex. 1005 para [0105])
`
`As explained by Dr. Park, “the ‘blue colored mannitol inclusions’ mentioned in
`
`Stawski were commercially available at the time of the invention and known to be
`
`useful as claimed as indicated.” (Ex. 1002 ¶ 16).
`
`As explained by Dr. Park, “[i]t would have been readily obvious to one of
`
`ordinary skill in the art that the speckles disclosed by the Prevacid Label could
`
`have been comprised of colored granules of a water-soluble sugar such as mannitol
`
`as taught by Stawski, as Stawski specifically teaches the inclusions as being useful
`
`15
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`

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`U.S. Patent No. 8,440,170
`
`to ‘have a contrasting color from the remainder of the … [tablet]’ into which they
`
`are added.” (Ex. 1002, ¶ 17). As further explained by Dr. Park, “as the Prevacid
`
`Label also teaches water-soluble sugars, including mannitol, as acceptable carriers,
`
`as well as various dyes, the use of a colored mannitol composition would have
`
`been obvious to one of ordinary skill in the art with a reasonable expectation that
`
`such would have been successful in producing a speckled appearance in a tablet as
`
`specifically disclosed by Stawski.” (Id.).
`
`iii. (b) a pharmaceutically acceptable carrier
`
`Element 1(b) of claim 1 further requires “a pharmaceutically acceptable
`
`carrier.” The Prevacid Label teaches pharmaceutically acceptable carriers.
`
`Each delayed-release orally disintegrating tablet contains
`
`enteric-coated microgranules consisting of 15 mg or 30
`
`mg of lansoprazole (active ingredient) and the following
`
`inactive
`
`ingredients:
`
`lactose
`
`monohydrate,
`
`microcrystalline
`
`cellulose, magnesium
`
`carbonate,
`
`hydroxypropyl cellulose, hypromellose, titanium dioxide,
`
`talc, mannitol, methacrylic
`
`acid,
`
`polyacrylate,
`
`polyethylene glycol, glyceryl monostearate, polysorbate
`
`80, triethyl citrate, ferric oxide, citric acid, crospovidone,
`
`aspartamePhenylketonurics: Contains Phenylalanine 2.5
`
`mg per 15 mg Tablet and 5.1 mg per 30 mg Tablet.,
`
`artificial strawberry flavor and magnesium stearate. (Ex.
`
`1004 pg. 1)
`
`16
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`

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`U.S. Patent No. 8,440,170
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`
`
`Moreover, as explained by Dr. Park, “Stawski also teaches pharmaceutically
`
`acceptable carriers.” (Ex. 1002, ¶ 18 citing Ex. 1005 para [0092]-[0106], Examples
`
`1-3).
`
`Therefore, as explained by Dr. Park, “it would have been readily obvious to
`
`one of ordinary skill in the art that an orally disintegrating tablet with speckled
`
`appearance further comprising a pharmaceutically acceptable carrier could have
`
`been reasonably expected to have been successfully derived from the disclosure of
`
`the Prevacid Label in view of Stawski without undue experimentation.” (Ex. 1002,
`
`¶ 18).
`
`B. Dependent Claims 2-4: The orally disintegrating tablets …
`wherein the water-soluble sugar is mannitol.
`
`Claim 2 depends from claim 1 further requires “the water-soluble sugar is
`
`selected from the group consisting of sucrose and polyalcohols”. Claim 3 depends
`
`from claim 2 and further limits the water-soluble sugars to “the group consisting of
`
`sucrose, sorbitol, mannitol, xylitol, and fructose”. Finally, Claim 4 further limits
`
`the choice of water-soluble sugars to “mannitol.” As explained by Dr. Park,
`
`Stawski satisfies the claim limitations of claims 2, 3, and 4 because it specifically
`
`states that the water-soluble sugar is mannitol. (Ex. 1002, ¶ 19, quoting Ex. 1005
`
`para [0105] “The Palatinit inclusions in the above Examples 3 A-H are replaced
`
`with blue colored mannitol inclusions.”).
`
`17
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`

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`U.S. Patent No. 8,440,170
`
`C. Dependent Claims 5-7: The orally disintegrating tablets …
`wherein the colored granules have a particle size from about 10
`μm to about 1200 μm (claim 5); wherein the colored granules
`have a particle size from about 200 μm to about 800 μm (claim
`6); and wherein the colored granules have a particle size from
`about 300 μm to about 500 μm (claim 7).
`
`Claim 5 depends from claim 1 and attempts to define the size range of the
`
`colored granules “from about 10 μm to about 1200 μm.” Claims 6 and 7 depend
`
`ultimately from claim 5, and further restrict the size of the colored granules to
`
`about 200 μm to about 800 μm and about 300 μm to about 500 μm, respectively.
`
`As explained by Dr. Park, “Stawski satisfies the limitations of claims 5, 6, and 7
`
`because it teaches the claimed range of colored granules of a water-soluble sugar
`
`by disclosing that blue, hydrogenated isomaltulose granules are sized to pass
`
`through #20 sieve (~841 μm) but retained on a #40 sieve (~420 μm).” (Ex. 1002, ¶
`
`20, citing Ex. 1005 para [0100]).
`
`D. Dependent Claims 8-9: The orally disintegrating tablets … the
`colored granules are present in an amount from about 0.1%
`w/w to about 50% w/w per tablet (claim 8); are present in an
`amount from about 1% w/w to about 30% w/w (claim 9).
`
`Claim 8 depends from claim 1 and requires that the colored granules are
`
`present in an amount from about 0.1% w/w to about 50% w/w per tablet while
`
`claim 9, which depends from claim 8, further restricts the amount to from about
`
`1% w/w to about 30% w/w. As explained by Dr. Park, “Stawski satisfies the
`
`limitations of claims 8 and 9 because it teaches that the colored granules are
`
`18
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`

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`U.S. Patent No. 8,440,170
`
`present in an amount from about 0.1% w/w to about 50% w/w per tablet, (Ex. 1005
`
`at para [0100] ‘Palatinit Inclusions 32.97%’) as well as an amount from about
`
`0.1% w/w to about 30% w/w per tablet. (Ex. 1005 at para [0106] ‘Palatinit
`
`Inclusions 16.49%’).” (Ex. 1002, ¶ 21).
`
`
`
`E. Summary of Obviousness Arguments for Ground 1.
`
`The obviousness arguments are summarized for each claim limitation in the
`
`following chart:
`
`
`
`U.S. 8440170
`
`An orally disintegrating tablets
`[sic] with speckled appearance
`comprising
`
`
`
`Suprenza 37.5 mg3
`
`Prevacid and Stawski
`
`The Prevacid Label teaches an orally
`disintegrating tablet with speckled appearance.
`(Ex. 1004 pg. 10 “PREVACID SoluTab
`Delayed-Release Orally Disintegrating
`Tablets, 15 mg, are white to yellowish white
`uncoated tablets with orange to dark brown
`speckles”)
`
`
`
`3 The ‘170 Patent supports the US FDA Orange Book listing of Suprenza
`
`http://www.accessdata.fda.gov/scripts/cder/ob/docs/patexclnew.cfm?Appl_No=20
`
`2088&Product_No=001&table1=OB_Rx. (Exhibit 1003). Image of orally
`
`disintegrating speckled Suprenza tablet available at Exhibit 1014,
`
`http://images.medscape.com/pi/features/drugdirectory/octupdate/AKR07220.jpg.
`
`
`
`19
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`

`
`
`
`1a. (a) speckles comprising
`colored granules of a water-
`soluble sugar, and
`
`U.S. Patent No. 8,440,170
`
`
`
`
`
`
`The Prevacid Label teaches speckles
`comprising colored granules (Ex. 1004 pg. 10
`“with orange to dark brown speckles”) and
`water soluble sugar (pg. 1 mannitol) but does
`not specifically disclose speckles comprising
`colored granules of a water-soluble sugar.
`
`
`Speckles comprising colored granules of water-
`soluble sugar were well-known in the art at the
`time of the invention as disclosed, for example
`by Stawski that teaches tablets (Ex. 1005
`Examples 3 A-H) comprising granules of a
`water-soluble sugar. (Ex. 1005 para [0063]
`“Pressed tablet 70 shown in FIG. 8 does not
`have distinct layers, and may be formed all of
`one composition. The composition comprises
`abrasive inclusions 75 to provide an abrasive
`surface opposite the generally domed top
`surface on the tablet. The abrasive inclusions in
`this embodiment comprise solid matrices of
`carbohydrates, solid matrices of polyols,
`extruded carbohydrates or extruded polyols,
`and also carry a flavor.”). Stawski further
`teaches the granules of water-soluble sugar are
`colored granules of a water-soluble sugar (Ex.
`1005 para [0085] The abrasive inclusions may
`be made from a number of different materials,
`including crystalline sugars or polyols; solid
`matrices of carbohydrates, polyols or mixtures;
`or extruded carbohydrates, polyols, or mixtures;
`… . On the one hand, solid matrices (such as
`from fluid bed coating or spray drying) and
`
`20
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`U.S. Patent No. 8,440,170
`
`extruded carbohydrates or polyols are preferred
`because these inclusions may also contain
`flavors and/or colors. When the inclusions
`include colors, the abrasive particles may
`have a contrasting color from the remainder
`of the compressible composition into which
`they are added.”; para [0098] “The abrasive
`inclusions can include encapsulated or
`entrappe