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`UNITED STATES PATENT AND TRADEMARK OFFICE
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`BEFORE THE PATENT TRIAL AND APPEAL BOARD
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`AQUESTIVE THERAPEUTICS, INC.
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`Petitioner
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`v.
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`HALE BIOPHARMA VENTURES, LLC
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`Patent Owner
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`
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`Case No.: IPR2019-00449
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`U.S. Patent 9,763,876
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`Issue Date: September 19, 2017
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`Title: Administration of Benzodiazepine Compositions
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`PETITION FOR INTER PARTES REVIEW
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`UNDER 35 U.S.C. §§ 311-319 AND 37 C.F.R. § 42.1 ET SEQ.
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`IPR2019-00449
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`U.S. Patent No. 9,763,876 B2
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`TABLE OF CONTENTS
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`TABLE OF CONTENTS ........................................................................................... i
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`EXHIBIT LIST ........................................................................................................ vi
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`I.
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`THE PETITION ................................................................................................. 1
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`II. MANDATORY NOTICES (37 C.F.R. § 42.8) ................................................. 1
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`A. Real Party-in-Interest (37 C.F.R. § 42.8(b)(1)) ............................................. 1
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`B. Related Matters (37 C.F.R. § 42.8(b)(2)) ...................................................... 1
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`C. Counsel (37 C.F.R. §§ 42.8(b)(3) and 42.10(a)) ........................................... 2
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`D. Service Information (37 C.F.R. § 42.8(b)(4)) ................................................ 2
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`III.
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`IV.
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`PAYMENT OF FEES .................................................................................... 3
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`ADDITIONAL REQUREMENTS FOR INTER PARTES REVIEW ........... 4
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`A. Grounds For Standing (37 C.F.R. § 42.104(a)) ............................................. 4
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`B. Level Of Ordinary Skill In The Art ............................................................... 4
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`C.
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`Identification of Challenge and Relief Requested
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`(37 C.F.R. § 42.104(b) and 37 C.F.R. § 42.22(a)(1)) ............................................ 5
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`D. Claims for Which IPR is Requested (37 C.F.R. § 42.104(b)(1)) .................. 5
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`1. Specific Statutory Grounds on Which the Challenge is Based (37 C.F.R.
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`§ 42.104(b)(2)) ................................................................................................... 5
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`V. “CLAIM-SUPPORTING DISCLOSURE” AND “CLAIM-ANTICIPATING
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`DISCLOSURE” IN CARTT’865 .............................................................................. 7
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`VI.
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`CLAIM CONSTRUCTION ........................................................................... 9
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`A. Ordinary and Customary Meaning (37 C.F.R. § 42.104(b)(3)) .................... 9
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`B. Claim Construction Summary Chart ............................................................11
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`C. Construction of ‘876 Patent Claim Terms ...................................................11
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`1.
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`2.
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`3.
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`“Vitamin E”..............................................................................................11
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`“Bioavailability” ......................................................................................12
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`“% (w/w)” and “% (w/v)” ........................................................................13
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`VII.
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`‘876 PATENT FAMILY HISTORY CHART ............................................14
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`VIII. EARLIEST EFFECTIVE PRIORITY DATES ...........................................17
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`A. Priority Summary Chart for the Challenged Claims ...................................20
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`B. Claims 8-10 and 15 Alcohol Ranges Not Supported By Cartt’865 or ‘558
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`Provisional ...........................................................................................................21
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`C. Claims 30-33 Not Supported or Enabled by Cartt’865 or ‘558 Provisional
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`
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`24
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`1. Diazepam - Claims 30-31 (“from 5 to 15% (w/v)”) ................................25
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`2. Vitamin E – Claims 30-33 .......................................................................26
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`3. Alcohols – Claims 30-33 .........................................................................27
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`4. The Effective Filing Date for Claims 30-33 is No Earlier Than June 14,
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`2011 ..................................................................................................................28
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`D. Claims 34-36 Not Supported Or Enabled By Cartt’865 or ‘558 Provisional
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`28
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`IX.
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`SUMMARY OF ‘876 PATENT ..................................................................30
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`A.
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`‘876 Patent Background ...............................................................................30
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`B.
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`‘876 Patent Prosecution History ..................................................................30
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`X. REASONABLE LIKELIHOOD THAT AT LEAST ONE OF THE
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`CHALLENGED CLAIMS OF ‘876 PATENT IS UNPATENTABLE ..................32
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`A. Ground 1 – Claims 8-10, 15, and 30-33 are Anticipated by Cartt’865
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`(Exhibit 1010) ......................................................................................................32
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`1. Claim 1 .....................................................................................................32
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`2. Claims 8-10 and 15 ..................................................................................37
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`3. Claim 9 .....................................................................................................48
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`4. Claim 10 ...................................................................................................49
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`5. Claims 30-33 ............................................................................................50
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`6. Ground I Conclusion ................................................................................60
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`B. Ground 2 – Claims 8-10, 15, and 30-33 are Obvious in View of Cartt’865
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`(Exhibit 1010) Alone or in View of Ueda (Exhibit 1019) ...................................60
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`1. Cartt’865 Alone .......................................................................................60
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`2. Cartt’865 in View of Ueda .......................................................................61
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`C. Ground 3 – Claims 34-36 Are Obvious In View Of Cartt’865, Meezan‘962,
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`And Jamieson .......................................................................................................64
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`1. Cartt’865 ..................................................................................................64
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`2. Meezan‘962 (Exhibit 1011) .....................................................................66
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`3.
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`Jamieson (Exhibit 1012) ..........................................................................69
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`4. Claims 34-36 Are Obvious ......................................................................72
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`XI.
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`GROUNDS AND CLAIM CHART ............................................................73
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`A. Grounds ........................................................................................................73
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`B. Claims Chart – Grounds 1 and 2 ..................................................................74
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`C. Claims Chart – Ground 3 .............................................................................83
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`XII. CONCLUSION ............................................................................................89
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`XIII. CERTIFICATE OF COMPLIANCE ...........................................................90
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`EXHIBIT LIST
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`EXHIBIT NO.
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`1001
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`1002
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`1003
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`1004
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`1005
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`1006
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`U.S. Patent No. 9,763,876 B2
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`EXHIBIT DESCRIPTION
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`U.S. Patent No. 9,763,876, Administration Of Benzodiazepine
`Compositions, filed October 29, 2014 (‘876 Patent)
`
`File History for ‘876 Patent, Ser. No. 14/527,613 (‘876 FH)
`1002 Part 1 - Pages 1-270
`1002 Part 2 - Pages 271-530
`
`U.S. Patent No. 8,895,546, Administration Of Benzodiazepine
`Compositions, filed June 13, 2012 (‘546 Patent)
`
`File History for ‘546 Patent, Ser. No. 13/495,942 (‘546 FH)
`1004 Part 1 – Pages 1-350
`1004 Part 2 – Pages 351-700
`1004 Part 3 – Pages 701-1050
`1004 Part 4 – Pages 1051-1400
`1004 Part 5 – Pages 1401-1750
`1004 Part 6 – Pages 1751-2100
`1004 Part 7 – Pages 2101-2450
`1004 Part 8 – Pages 2451-2681
`
`Provisional Patent Application No. 61/497,017, filed June 14,
`2011 (‘017 Provisional)
`
`Provisional Patent Application No. 61/570,110, filed December
`13, 2011 (‘110 Provisional)
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`vi
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`IPR2019-00449
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`1007
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`1008
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`1009
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`1010
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`1011
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`1012
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`1013
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`
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`File History for Non-Provisional Patent Application Serial No.
`12/413,439, filed March 27, 2009 (‘439 FH)
`1007 Part 1 – Pages 1-400
`1007 Part 2 – Pages 401-800
`1007 Part 3 – Pages 801-1200
`1007 Part 4 – Pages 1201-1600
`1007 Part 5 – Pages 1601-2000
`1007 Part 6 – Pages 2001-2400
`1007 Part 7 – Pages 2401-2800
`1007 Part 8 – Pages 2801-3200
`1007 Part 9 – Pages 3201-3488
`
`Provisional Patent Application No. 61/040,558, filed March 28,
`2008 (‘558 Provisional)
`
`Cartt et al., WO 2009/121039, Administration Of
`Benzodiazepine Compositions, published October 1, 2009,
`International Filing Date March 27, 2009
`(PCT/US2009/038696) (Cartt ‘039)
`
`U.S. Patent Application Publication No. US 2009/0258865,
`Administration of Benzodiazepine Compositions, Serial No.
`12/413,439 (Cartt‘865)
`
`Meezan et al., U.S. Patent Application Publication No. US
`2006/0046962, Absorption Enhancers for Drug Administration,
`Serial No. 11/127,786, published March 2, 2006 (Meezan‘962)
`
`Jamieson et al., U.S. Patent Application Publication No. US
`2008/0070904, Pharmaceutical Compositions of
`Benzodiazepines and Method of Use Thereof, Serial No.
`11/897,028, published March 20, 2008 (Jamieson)
`
`Sonne, U.S. Patent No. 6,193,985, Tocopherol Compositions
`For Delivery Of Biologically Active Agents, issued February 27,
`2001 (Sonne)
`
`vii
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`IPR2019-00449
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`U.S. Patent No. 9,763,876 B2
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`1014
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`1015
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`1016
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`1017
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`1018
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`1019
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`1020
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`1021
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`1022
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`
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`Gwozdz et al., WO 2009/120933, Pharmaceutical Solutions
`And Method For Solubilizing Therapeutic Agents, published
`October 1, 2009, International Filing Date March 27, 2009
`(PCT/US2009/038518) (Gwozdz)
`
`Cartt et al., U.S. Patent Application Publication No. US
`2008/0279784, Nasal Administration Of Benzodiazepines,
`Serial No. 12/116,842, published November 13, 2008 (Cartt
`‘784)
`
`Kee et al., U.S. Patent No. 5,369,095, Compositions And
`Method Comprising Substituted Glycosides As Mucus
`Membrane Permeation Enhancers, issued November 29, 1994
`(Kee)
`
`Cartt et al., WO 2008/137960, Nasal Administration Of
`Benzodiazepines, published November 13, 2008, International
`filing date May 7, 2008 (PCT/US2008/062961) (Cartt ‘960)
`
`Tenta, U.S. Patent No. 3,949,072, Seborrheic Keratosis
`Treatment, issued April 6, 1976 (Tenta)
`
`Ueda et al., U.S. Patent No. 4,657,901, Pharmaceutical
`Composition, issued April 14, 1987 (Ueda)
`
`Meezan et al., U.S. Patent No. 5,661,130, Absorption
`Enhancers For Drug Administration, issued August 26, 1997
`(Meezan‘130)
`
`Merkus, U.S. Patent Application Publication No. US
`2005/0153956, Serial No. 11/034,474, published July 14, 2005
`(Merkus)
`
`Liversidge et al., U.S. Patent Application Publication No. US
`2006/0198896, Serial No. 11/354,249, published September 7,
`2006 (Liversidge)
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`viii
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`1023
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`1024
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`1025
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`1026
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`1027
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`1028
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`1029
`
`
`1030
`
`
`1031
`
`Ritschel, Handbook of Basic Pharmacokinetics, Chapter 36
`(Bioavailability and Bioequivalence), Drug Intelligence
`Publications, Illinois, 1992 (Ritschel)
`
`Osborne et al., Skin Penetration Enhancers Cited in the
`Technical Literature, Pharmaceutical Technology, November
`1997 (Osborne)
`
`Lindhardt et al., Electroencephalographic effects and serum
`concentrations after intranasal and intravenous administration
`of diazepam to healthy volunteers, Blackwell Science Ltd Br J
`Clin Pharmacol, 52, 521-527, 2001 (Lindhardt)
`
`Kibbe, editor, Handbook of Pharmaceutical Excipients, Third
`Edition (2000), American Pharmaceutical Association,
`Washington DC (Kibbe)
`
`Illum, Nasal drug delivery-possibilities, problems and
`solutions, Journal of Controlled Release 87 (2003) 187-198
`(Illum)
`
`Ivaturi et al., Pharmacokinetics and tolerability of intranasal
`diazepam and midazolam in healthy adult volunteers, Acta
`Neurol Scand. 2009 Nov;120(5):353-7. doi: 10.1111/j.1600-
`0404.2009.01170.x. Epub 2009 May 14 (Ivaturi)
`
`O’Dell et al., School nurses’ experience with administration of
`rectal diazepam gel for seizures, J Sch Nurs., June 2007,
`23(3):166-9 (O’Dell)
`
`Gizurarson et al., Intranasal Administration of Diazepam
`Aiming at the Treatment of Acute Seizures: Clinical Trials in
`Healthy Volunteers, Biological and Pharmaceutical Bulletin,
`Volume 22 (1999) Issue 4 Pages 425-427 (Gizurarson)
`
`Rowe et al., editors, Handbook of Pharmaceutical Excipients,
`Fourth Edition (2003), Monographs for “Alcohol” (i.e.,
`ethanol), “Alpha Tocopherol”, “Benzyl Alcohol”, “Glycerin”,
`ix
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`1032
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`1033
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`1034
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`1035
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`1036
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`1037
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`
`1038
`
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`1039
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`
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`“Olive Oil”, “Polyethylene Glycol”, “Propylene Glycol”,
`“Sesame Oil”, and “Triacetin”, American Pharmaceutical
`Association, Washington DC (Rowe)
`
`Edman [II] et al., Microspheres as a nasal delivery system for
`peptide drugs, Journal of Controlled Release, Vol. 21 (1992)
`165-l72 (Edman II)
`
`French et al., Pharmacopeial Standards and Specifications for
`Bulk Drugs and Solid Oral Dosage Forms, Journal of
`Pharmaceutical Sciences, December 1967, Vol. 56(12):1622-
`1641 (French)
`
`Edman [I] et al., (D) Routes of Delivery: Case Studies - (1)
`Nasal delivery of peptide drugs, Advanced Drug Delivery
`Reviews, 8 (1992) 165-177 (Edman I)
`
`Davis, Delivery of peptide and non-peptide drugs through the
`respiratory tract, Pharmaceutical Science & Technology
`Today, Vol. 2, No. 11 November 1999, pages 450-456 (Davis)
`
`Deshmukh et al., Lorazepam in the Treatment of Refractory
`Neonatal Seizures, Am J Dis Child. 1986;140(10):1042-1044
`(Deshmukh)
`
`Colombo, Mucosal Drug Delivery, Nasal, pp. 592-605, Vol 2,
`Encyclopedia of Controlled Drug Delivery (Mathiowitz,
`editor), John Wiley & Sons, 1999 (Colombo)
`
`Bara, U.S. Patent Application Publication No.
`US/2006/0178290, Serial No. 10/563,967, published August 10,
`2006 (Bara)
`
`Behl et al., Effects of physicochemical properties and other
`factors on systemic nasal drug delivery, Advanced Drug
`Delivery Reviews 29 (1998) 89–116 (Behl)
`
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`U.S. Patent No. 9,763,876 B2
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`1040
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`1041
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`1042
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`1043
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`1044
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`1045
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`1046
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`1047
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`1048
`
`File History for EP 128 01372.9, based on WO 2012/174158
`and PCT/US2012/042311
`1040 Part 1 - Pages 1-250
`1040 Part 2 - Pages 251-500
`1040 Part 3 – Pages 501-662
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`Declaration of Dr. Nicholas A. Peppas
`
`PDR 54th Edition 2000, DIASTAT® (diazepam rectal gel);
`MIACALCIN® (Calcitonin Nasal Spray); VALIUM®
`(diazepam injection), Physicians’ Desk Reference.
`
`Knoester, et al., Pharmacokinetics and pharmacodynamics of
`midazolam administered as a concentrated intranasal spray. A
`study in healthy volunteers, Br J Clin Pharmacol. 2002
`May;53(5):501-7.
`
`USP NF 2003, The United States Pharmacopeia, The National
`Formulary, United States Pharmacopeial Convention, Inc.
`(“USP/NF”)
`
`Maitani, et al., Design of ocular/lacrimal and nasal systems
`through analysis of drug administration and absorption,
`Journal of Controlled Release, Volume 49, Issues 2–3, 15
`December 1997, Pages 185-192.
`
`Provisional Patent Application No. 61/040,281, Pharmaceutical
`Solutions and Method for Solubilizing Therapeutics Agents,
`filed March 28, 2008, Gwozdz, (Gwozdz ‘281 Provisional)
`
`Gwozdz Assignment of Provisional in Non-Provisional Case,
`dated April 21, 2008, recorded September 23, 2010 (Gwozdz
`Assignment).
`
`Kagatani, et al., U.S. Patent No. 4,690,952, Pharmaceutical
`Compositions for Nasal administration Comprising Calcitonin
`and an Absorption-Promoting Substance, issued September 1,
`1987 (Kagatani).
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`I.
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`THE PETITION
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`Petitioner, real party-in-interest, Aquestive Therapeutics, Inc. (“Aquestive”
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`or “Petitioner”) (formerly Monosol RX, LLC), hereby petitions the Patent Trial
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`and Appeal Board (“PTAB”) of the U.S. PTO, pursuant to 35 U.S.C. §§ 311-319
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`and 37 C.F.R. § 42.1 et seq., to institute an inter partes review and find
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`unpatentable and cancel Claims 8-10, 15, and 30-36 (“the Challenged Claims”) of
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`U.S. Patent No. 9,763,876 B2, entitled “Administration of Benzodiazepine
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`Compositions,” assigned to Hale Biopharma Ventures, LLC (“Patent Owner” or
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`“PO”). There is a reasonable likelihood that Petitioner will prevail with respect to
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`at least one claim challenged in this petition. See also SAS Inst., Inc. v. Iancu, 138
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`S.Ct. 1348 (April 24, 2018).
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`
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`II. MANDATORY NOTICES (37 C.F.R. § 42.8)
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`A. Real Party-in-Interest (37 C.F.R. § 42.8(b)(1))
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`Petitioner Aquestive Therapeutics, Inc. (formerly Monosol Rx, LLC), 30
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`Technology Drive, Warren, New Jersey 07059, a Delaware corporation, is the sole
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`real party-in-interest.
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`B. Related Matters (37 C.F.R. § 42.8(b)(2))
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`Petitioner is not aware of any matters.
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`C. Counsel (37 C.F.R. §§ 42.8(b)(3) and 42.10(a))
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`Petitioner designates the following individuals as its lead counsel and back-
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`up lead counsel:
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`Lead Counsel:
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`Back-up Lead Counsel
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`Daniel A. Scola, Jr.
`Reg. No. 29,855
`Hoffmann & Baron, LLP
`dscola@hbiplaw.com
`(973) 331-1700
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`Michael I. Chakansky
`Reg. No. 31,600
`Hoffmann & Baron, LLP
`mchakansky@hbiplaw.com
`(973) 331-1700
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`
`James F. Harrington
`Reg. No. 44,741
`Hoffmann & Baron, LLP
`jharrington@hbiplaw.com
`516-822-3550
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`Matthew J. Solow
`Reg. No. 56,878
`Hoffmann & Baron, LLP
`msolow@hbiplaw.com
`(973) 331-1700
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`D.
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`Service Information (37 C.F.R. § 42.8(b)(4))
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`Service on Petitioner may be made electronically by using all the following
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`five e-mail addresses together in providing service: dscola@hbiplaw.com;
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`mchakansky@hbiplaw.com; jharrington@hbiplaw.com; msolow@hbiplaw.com;
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`and 876IPR@hbiplaw.com. Service on Petitioner may be made by Postal Mailing,
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`U.S. Patent No. 9,763,876 B2
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`Hand-Delivery or facsimile addressed to Lead and Back-up Lead Counsel at the
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`address on the following page, but electronic service above is requested:
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`Hoffmann & Baron, LLP
`6 Campus Drive
`Parsippany, New Jersey 07054
`Facsimile: 973-331-1717
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`
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`III. PAYMENT OF FEES
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`Pursuant to 37 C.F.R. §§ 42.103 and 42.15(a), the undersigned authorizes
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`PTO to charge the $30,500 fee for the 11 claims requested for review (request fee
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`of $15,500; and post-institution fee of $15,000) in this IPR Petition to Deposit
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`Account No. 08-2461. The undersigned further authorizes payment from and to
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`the above referenced Deposit Account for any additional fees or refund that may be
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`due in connection with this petition and IPR proceeding.
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`IV. ADDITIONAL REQUREMENTS FOR INTER PARTES REVIEW
`
`U.S. Patent No. 9,763,876 B2
`
`
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`A. Grounds For Standing (37 C.F.R. § 42.104(a))
`
`Petitioner hereby certifies that ‘876 Patent is available for IPR and that
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`Petitioner is not barred or estopped from requesting IPR challenging the claims of
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`‘876 Patent on the grounds identified herein.
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`
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`B.
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`Level Of Ordinary Skill In The Art
`
`As of the earliest priority date that the Challenged Claims of ‘876 Patent are
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`entitled to, a person of ordinary skill in the art (“POSITA”) would have been a
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`medicinal chemist, pharmaceutical chemist, chemist, or biologist involved in the
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`research and development of pharmaceutical formulations and/or delivery. The
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`POSITA would have at least a bachelor’s degree in chemical, biological, or
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`pharmaceutical sciences or a medical degree, and several years of experience in the
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`field of transmucosal (including intranasal, rectal, vaginal, ocular, lacrimal,
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`nasolacrimal, buccal, sublingual, urethral, inhalation, and auricular)
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`pharmaceutical formulation development and/or delivery, the amount of post-
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`graduate experience depending on the level of formal education. The individual
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`would also have some experience in design and testing of formulations for mucosal
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`delivery (and particularly in intranasal formulations) of systemic-acting drugs.
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`U.S. Patent No. 9,763,876 B2
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`C.
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`Identification of Challenge and Relief Requested
`(37 C.F.R. § 42.104(b) and 37 C.F.R. § 42.22(a)(1))
`The precise relief requested by Petitioner is that Claims 8-10, 15, and 30-36
`
`
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`(“the Challenged Claims”) be found unpatentable and cancelled from ‘876 Patent.
`
`
`
`D. Claims for Which IPR is Requested (37 C.F.R. § 42.104(b)(1))
`
`Petitioner requests inter partes review and cancellation of Claims 8-10, 15,
`
`and 30-36 of ‘876 Patent.
`
`
`
`1.
`
`Specific Statutory Grounds on Which the Challenge is
`Based (37 C.F.R. § 42.104(b)(2))
`
`
`Basis
`
`
`Claims Challenged
`
`35 U.S.C. § 102(b)
`
`35 U.S.C. § 103(a)
`
`8-10, 15,
`30-33
`
`8-10, 15,
`30-33
`
`
`Reference(s)
`
`Cartt’865
`(Exhibit 1010)
`
`Cartt’865
` (Exhibit 1010)
`Alone or With
`Ueda
`(Exhibit 1019)
`
`
`5
`
`
`
`
`Ground
`
`
` 1
`
`
`
` 2
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`
`
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`IPR2019-00449
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` 3
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`U.S. Patent No. 9,763,876 B2
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`35 U.S.C. § 103(a)
`
`34-36
`
`Cartt’865
` (Exhibit 1010)
`&
`Meezan‘962
`(Exhibit 1011)
`&
`Jamieson
`(Exhibit 1012)
`
`
`
`
`
`Petitioner also relies on the expert declaration of Nicholas A. Peppas, Sc.D.
`
`(Exhibit 1041, hereinafter “Peppas”) and on ‘876 Patent admitted prior art.
`
`
`
`The foregoing art qualify as prior art under 35 U.S.C. § 102(b) for at least
`
`the reason that the references issued or published more than one year prior to the
`
`earliest possible priority date of the Challenged Claims, namely, June 14, 2011:
`
`102(b) Reference
`
`Publication/Issue Date
`
`Exhibit No.
`
`Cartt’865
`(US 2009/0258865)
`
`Ueda
`(US 4,657,901)
`
`Meezan‘962
`(US 2006/0046962)
`
`Jamieson
`(US 2008/007094)
`
`1010
`
`1019
`
`1011
`
`1012
`
`October 15, 2009
`
`April 14, 1987
`
`March 2, 2006
`
`March 20, 2008
`
`6
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`IPR2019-00449
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`
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`As discussed below, various limitations of each of the Challenged Claims
`
`
`
`U.S. Patent No. 9,763,876 B2
`
`are not supported and/or enabled prior to the filing of ‘017 Provisional (Exhibit
`
`1005) on June 14, 2011. Therefore, the earliest effective filing date for the
`
`Challenged Claims is June 14, 2011.
`
`
`
`V.
`
`“CLAIM-SUPPORTING DISCLOSURE” AND “CLAIM-
`ANTICIPATING DISCLOSURE” IN CARTT’865
`Cartt’865 provides sufficient disclosure to anticipate/render obvious the
`
`Challenged Claims while failing to provide sufficient disclosure to support the
`
`Challenged Claims.
`
`There is nothing in patent law that forbids a patent/patent application from
`
`invalidating its continuation-in-part, as the Federal Circuit has recognized. See,
`
`e.g., Santarus, Inc. v. Par Pharm., Inc., 694 F.3d 1344, 1352 (Fed. Cir. 2012)
`
`(finding a parent patent was a legitimate, invalidating reference against its child
`
`continuation-in-part application).
`
`Moreover, for almost fifty years, courts have held that it is possible for a
`
`reference to anticipate a later application while failing to support it for priority
`
`purposes. The C.C.P.A. held:
`
`
`
`7
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`IPR2019-00449
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`U.S. Patent No. 9,763,876 B2
`
`“[T]he description of a single embodiment of broadly
`claimed subject matter constitutes a description of the
`invention for anticipation purposes, whereas the same
`information in a specification might not alone be enough to
`provide a description of that invention for purposes of
`adequate disclosure.” In re Lukach, 442 F.2d 967, 970
`(C.C.P.A. 1971) (internal citations /quotations omitted).
`
`The Federal Circuit still recognizes the importance of In re Lukach:
`
`“The CCPA also recognized a subtle distinction between
`a written description adequate to support a claim under
`§ 112 and a written description sufficient to anticipate its
`subject matter under § 102(b). The difference between
`'claim-supporting disclosures' and
`'claim-anticipating
`disclosures' was dispositive in [In re Lukach].” Vas-Cath
`Inc. v. Sakharam D. Mahurkar, 935 F.2d 1555, 1562
`(Fed. Cir. 1991).
`
`More recently, the Federal Circuit positively cited Vas-Cath Inc. for this
`
`proposition. See In re Gleave, 560 F.3d 1331, 1334 (Fed. Cir. 2009) (quoting Vas-
`
`Cath Inc.’s discussion of the “distinction between a written description adequate
`
`to support a claim under § 112 and a written description sufficient to anticipate its
`
`subject matter under § 102(b).” (emphasis in original)).
`
`8
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`IPR2019-00449
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`U.S. Patent No. 9,763,876 B2
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`Additionally, M.P.E.P. §211.05(I)(B), 5th paragraph, directs the reader to,
`
`inter alia, In re Lukach as a “case[] of interest” with respect to continuations-in-
`
`part, priority dates, and prior art references.
`
`These cases recognize that: (i) continuations-in-part can be invalidated by
`
`their parent/grandparent/etc. applications, and (ii) though subtle, there is a definite
`
`distinction between “claim-supporting disclosures” and “claim-anticipating
`
`disclosures.” As Petitioner will prove, PO stepped into a trap of its own making by
`
`providing disclosure in Cartt’865 sufficient to invalidate the Challenged Claims
`
`while failing to provide disclosure sufficient to support the Challenged Claims.
`
`
`
`
`
`VI. CLAIM CONSTRUCTION
`
`A. Ordinary and Customary Meaning (37 C.F.R. § 42.104(b)(3))
`
`A claim of a patent is construed in accordance with the ordinary and
`
`customary meaning of such claim as understood by one of ordinary skill in the art
`
`and the prosecution history pertaining to the patent. 37 C.F.R. § 42.100. See
`
`Phillips v. AWH Corp., 415 F.3d 1303 (Fed. Cir. 2005) (en banc).
`
`For inventors to act as their own lexicographer, the definition must be set
`
`forth in the specification with reasonable clarity, deliberateness, and precision.
`
`Renishaw PLC v. Marposs Societa’ per Azioni, 158 F.3d 1243, 1249 (Fed. Cir.
`9
`
`
`
`
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`IPR2019-00449
`
`
`1998). If a feature is not necessary to give meaning to what inventors mean by a
`
`U.S. Patent No. 9,763,876 B2
`
`
`
`claim term, it would be “extraneous” and should not be read into the claim.
`
`Renishaw PLC, 158 F.3d at 1249; E.I. du Pont de Nemours & Co. v. Phillips
`
`Petroleum Co., 849 F.2d 1430, 1433 (Fed. Cir. 1988). The construction that stays
`
`true to the claim language and most naturally aligns with the inventors’ description
`
`is likely the correct interpretation. See Renishaw PLC, 158 F.3d at 1250.
`
`Petitioner’s position regarding the scope of ‘876 Patent’s claims should not
`
`be taken as an assertion regarding the appropriate claim scope in other adjudicative
`
`forums where a different claim interpretation standard may apply, e.g., in a patent
`
`infringement action. Moreover, Petitioner reserves all rights to further challenge
`
`any claim terms herein under 35 U.S.C. § 112, including by arguing that the terms
`
`are not definite, supported by the written description, and/or enabled. Further, as
`
`Petitioner is precluded from presenting challenges under 35 U.S.C. § 112 in an
`
`IPR, Petitioner’s arguments in this Petition, or lack thereof on any of these
`
`grounds, should not be interpreted as waiving or conflicting with arguments
`
`available in other forums under 35 U.S.C. § 112.
`
`
`
`
`
`
`
`10
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`IPR2019-00449
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`B. Claim Construction Summary Chart
`
`
`
`U.S. Patent No. 9,763,876 B2
`
`Claim Term
`
`Construed Claim Term
`
`vitamin E
`
`“any of the natural or synthetic tocopherols,
`
`tocotrienols, any isomers thereof, any esters
`
`thereof, any analogs or derivatives thereof, or any
`
`combinations thereof”
`
`“bioavailability, determined by the ratio of
`
`bioavailability
`
`([AUC∞(IN) x Dose(IV)] divided by [AUC∞(IV) x
`
`Dose(IN)]) times 100%”
`
`“% (w/v) or % (w/w)”
`
`“% (w/v) or % (w/w)”
`
`% (w/w)
`
`% (w/v)
`
`
`
`C. Construction of ‘876 Patent Claim Terms
`
`1.
`
`“Vitamin E”
`
`Based on the express definition provided in ‘876 Patent, a POSITA would
`
`understand “vitamin E” as meaning “any of the natural or synthetic tocopherols,
`
`tocotrienols, any isomers thereof, any esters thereof, any analogs or derivatives
`
`thereof, or any combinations thereof.” See ‘876 Patent, 33:8-23, Exhibit 1001, p.
`11
`
`
`
`
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`IPR2019-00449
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`0026; see also Peppas, Exhibit 1041, ¶¶90-93.
`
`
`
`
`
`U.S. Patent No. 9,763,876 B2
`
`2.
`
`“Bioavailability”
`
`‘876 Patent defines “bioavailability” as follows:
`
`“it is intended that bioavailability be determined by a
`suitable pharmacodynamics method, such as comparison
`of area under the blood plasma concentration curve
`(AUC) for the nasally and intravenously administered
`drug.
`It
`is
`further understood
`that
`the percent
`bioavailability
`of
`the
`nasally
`administered
`benzodiazepine may be determined by comparing the
`area under the blood plasma concentration curve obtained
`with one dose of the benzodiazepine (e.g. 10 mg of nasal
`diazepam) with another dose of the same benzodiazepine
`administered intravenously (e.g. 5 mg of i.v. diazepam),
`taking into consideration the difference in dose.”
`‘876 Patent, 4:57-5:1, Exhibit 1001, pp. 0011-0012.
`
`Moreover, Ritschel (Exhibit 1023), considered to be a bible of the
`
`pharmacokinetic discipline (Peppas, Exhibit 1041, ¶95), provides the following
`
`equation at p. 506:
`
`12
`
`
`
`
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`IPR2019-00449
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`
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`U.S. Patent No. 9,763,876 B2
`
`Based on the definition in ‘876 Patent, which agrees with Ritschel’s formula,
`
`“bioavailability” should be construed as meaning: “bioavailability, determined by
`
`the ratio of ([AUC∞(IN) x Dose(IV)] divided by [AUC∞(IV) x Dose(IN)]) times 100%.”
`
`
`
`See Peppas, Exhibit 1041, ¶96.
`
`
`
`“% (w/w)” and “% (w/v)”
`3.
`‘876 Patent uses these two terms interchangeably. In particular, independent
`
`Claim 1 recites the term “% (w/w)” for the alcoholic element, while dependent
`
`Claim 5, e.g., recites “% (w/v)” for the same exact alcoholic element. Therefore,
`
`the two terms are interpreted as interchangeable. See Peppas, Exhibit 1041,
`
`¶¶102-103.
`
`Additionally, due to the specific gravities of each of the ingredients recited
`
`in the claims, “the differences between measurements of ‘% (w/v)’ and ‘% (w/w)’
`
`(and even % (v/v)) should be small enough as to be insignificant”. Peppas,
`
`Exhibit 1041, ¶103.
`
`
`
`
`
`13
`
`
`
`
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`IPR2019-00449
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`VII. ‘876 PATENT FAMILY HISTORY CHART
`
`
`
`U.S. Patent No. 9,763,876 B2
`
`
`
`A timeline of the ‘876 Patent family history is provided on the following
`
`page, with a more detailed timeline on the page thereafter:
`
`
`
`
`
`14
`
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`IPR2019-00449
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`Provisionals
`
`
`Serial No. 61/040,558
`Filed: March 28, 2008
`‘558 Provisional
`Exhibit 1008
`
`Serial No. 61/497,017
`Filed: June 14, 2011
` ‘017 Provisional
`Exhibit 1005
`
`Serial. No. 61/570,110
`Filed: Dec. 13, 2011
`‘110 Provisional
`Exhibit 1006
`
`
`
`
`
`U.S. Patent No. 9,763,876 B2
`
`Non-Provisionals
`
`
`
`
`
`Non-Provisional
`FIRST DISCLOSURE OF
`ALKYL GLYCOSIDES
`
`Serial No. 12/413,439
`Filed: March 27, 2009
`US 2009/0258865 (abandoned)
`Cartt’865 – Exhibit 1010
`Published: Oct. 15, 2009
`
`
`C-I-P
`Non-Provisional
`Serial No. 13/495,942
`Filed: June 13, 2012
`USP 8,895,546
`Exhibit 1003
`Issued: Nov. 25, 2014
`
`Continuation
`Serial No. 14/527,613
`Filed: October 29, 2014
`USP 9,763,876 – Exhibit 1001
`Issued: Sept. 19, 2017
`
`15
`
`
`
`
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`IPR2019-00449
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`
`
`Serial No. 61/040,558
`Filed: March 28, 2008
`‘558 Provisional
`Exhibit 1008
`
`Serial No. 12/413,439
`Filed: March 27, 2009
`US 2009/0258865
`Cartt’865 – Exhibit 1010
`(abandoned)
`Published: Oct. 15, 2009
`
`• FIRST DISCLOSURE OF ALKYL
`GLYCOSIDES
`• SUFFICIENT DISCLOSURE TO
`INVALIDATE CLAIMS 8-10, 15, 30-
`33 UNDER §§ 102/103 AND
`CLAIMS 34-36 UNDER § 103
`
`
`
`
`U.S. Patent No. 9,763,876 B2
`
`Serial. No. 61/570,110
`Filed: Dec. 13, 2011
`‘110 Provisional
`Exhibit 1006
`
`Serial No. 13/495,942
`Filed: June 13, 2012
`USP 8,895,546
`Exhibit 1003
`Issued: Nov. 25, 2014
`
`Serial No. 14/527,613
`Filed: October 29, 2014
`USP 9,763,876
`Exhibit 1001
`Issued: Sept. 19, 2017
`
`Serial No. 61/497,017
`Filed: June 14, 2011
` ‘017 Provisional
`Exh
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