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.: IPR2019-00451
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`U.S. Patent 9,763,876
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`Issue Date: September 19, 2017
`
`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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`IPR2019-00451
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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 ........................................................................................................ v
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`I. 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)) ................................................... 2
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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)) ............................................. 3
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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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`Identification of Challenge and Relief Requested (37 C.F.R. § 42.104(b)
`C.
`and 37 C.F.R. § 42.22(a)(1)) ................................................................................ 5
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`1. Claims for which IPR is Requested
`(37 C.F.R. § 42.104(b)(1)) ................................................................................ 5
`
`2. Specific Statutory Grounds on Which the Challenge is Based (37
`C.F.R. § 42.104(b)(2)) ...................................................................................... 5
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`IPR2019-00451
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`U.S. Patent No. 9,763,876 B2
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`3.
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`35 U.S.C. § 325(d) Should Not Bar the Petition .................................... 8
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`V. 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.
`
`3.
`
`4.
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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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`“about 56.47% (w/v) vitamin E” ..........................................................14
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`VI.
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`‘876 PATENT FAMILY HISTORY CHART .........................................15
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`VII. EARLIEST EFFECTIVE PRIORITY DATE IS NO EARLIER
`THAN MARCH 27, 2009 ......................................................................................18
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`VIII. SUMMARY OF ‘876 PATENT ................................................................21
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`A. Background of ‘876 Patent ........................................................................21
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`B. Prosecution History of ‘876 Patent...........................................................21
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`IX.
`
`PRIOR ART REFERENCES RELIED ON BY PETITIONER ...........23
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`A. Gwozdz et al., WO 2009/120933 (“Gwozdz”, Exhibit 1014) ..................23
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`1. Benzodiazepines/Diazepam ...................................................................23
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`2. Tocopherols/Tocotrienols and Alcohols ...............................................23
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`3.
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`Intranasal Administration, Including Spraying .................................27
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`4. Bioavailability .........................................................................................28
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`IPR2019-00451
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`U.S. Patent No. 9,763,876 B2
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`B. Meezan et al., U.S. Publication No. 2006/0046962
`(“Meezan‘962”, Exhibit 1011)...........................................................................28
`
`1. General Teachings .................................................................................28
`
`2. Combined With Gwozdz .......................................................................30
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`C. Cartt et al., US 2008/0279784 (“Cartt‘784”, Exhibit 1015) ...................31
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`D. Motivation to Combine ..............................................................................33
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`1. Gwozdz Combined With Meezan’962 .................................................33
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`2. Addition of Cartt’784 to Gwozdz and Meezan’962 ............................34
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`X. THERE IS A REASONABLE LIKELIHOOD THAT AT LEAST
`ONE OF THE CHALLENGED CLAIMS OF ‘876 PATENT IS
`UNPATENTABLE .................................................................................................35
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`A. Grounds Chart ...........................................................................................36
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`B. Grounds 1 and 2 .........................................................................................36
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`1.
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`Independent Claim 1..............................................................................37
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`2. Claim 2 ....................................................................................................41
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`3. Claims 3-4 ...............................................................................................42
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`4. Claims 5-6 ...............................................................................................42
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`5. Claim 7 ....................................................................................................43
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`6. Claims 8 and 15 ......................................................................................44
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`7. Claims 9-10 .............................................................................................46
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`8. Claims 11-12 ...........................................................................................46
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`9. Claims 13-14 ...........................................................................................47
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`IPR2019-00451
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`U.S. Patent No. 9,763,876 B2
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`10. Claim 16 ...............................................................................................48
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`11. Claims 17-18 ........................................................................................49
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`12. Claims 19-22 ........................................................................................51
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`13. Claim 23 ...............................................................................................52
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`14. Claims 24-26 ........................................................................................54
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`15. Claims 27 and 29 .................................................................................55
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`16. Claim 28 ...............................................................................................56
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`17. Claims 30-33 ........................................................................................59
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`18. Claims 34-36 ........................................................................................61
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`XI. GROUNDS AND CLAIM CHART..........................................................64
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`A. Grounds .......................................................................................................64
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`B. Claims Chart ..............................................................................................65
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`1. Ground 1 .................................................................................................65
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`2. Ground 2 .................................................................................................87
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`XII. CONCLUSION ..........................................................................................93
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`XIII. CERTIFICATE OF COMPLIANCE ......................................................94
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`IPR2019-00451
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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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`IPR2019-00451
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`U.S. Patent No. 9,763,876 B2
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`1007
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`
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`1008
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`1009
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`
`1010
`
`
`1011
`
`
`1012
`
`
`1013
`
`
`
`
`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)
`
`vi
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`IPR2019-00451
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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
`
`
`1021
`
`
`1022
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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, Topical Compositions for
`Treatment of 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)
`
`vii
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`IPR2019-00451
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`U.S. Patent No. 9,763,876 B2
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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
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`
`
`
`
`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)
`
`viii
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`U.S. Patent No. 9,763,876 B2
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`1031
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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
`
`
`1038
`
`
`
`Rowe et al., editors, Handbook of Pharmaceutical Excipients,
`Fourth Edition (2003), Monographs for “Alcohol” (i.e.,
`ethanol), “Alpha Tocopherol”, “Benzyl Alcohol”, “Glycerin”,
`“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)
`
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`IPR2019-00451
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`U.S. Patent No. 9,763,876 B2
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`1039
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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
`
`
`1047
`
`
`
`Behl et al., Effects of physicochemical properties and other
`factors on systemic nasal drug delivery, Advanced Drug
`Delivery Reviews 29 (1998) 89–116 (Behl)
`
`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
`
`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).
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`IPR2019-00451
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`U.S. Patent No. 9,763,876 B2
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`1048
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`1049
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`1050
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`
`
`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).
`
`Cartt’784 Assignment, dated March 6, 2012, recorded March
`29, 2012 (Cartt’784 Assignment)
`
`Table of Various Diazepam Solutions Described in or Modified
`From Sonne’s Example 11 (“DS11”)
`
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`IPR2019-00451
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`I.
`
`THE PETITION
`
`
`
`U.S. Patent No. 9,763,876 B2
`
`Petitioner, real party-in-interest, Aquestive Therapeutics, Inc. (“Aquestive”
`
`or “Petitioner”) (formerly Monosol RX, LLC), hereby petitions the Patent Trial
`
`and Appeal Board (“PTAB”) of the USPTO, pursuant to 35 U.S.C. §§ 311-319 and
`
`37 C.F.R. § 42.1 et seq., to institute an inter partes review and to find unpatentable
`
`and cancel Claims 1-36 (“the Challenged Claims”) of U.S. Patent No. 9,763,876
`
`B2, entitled “Administration of Benzodiazepine Compositions,” assigned to Hale
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`Biopharma Ventures, LLC (“Patent Owner” or “PO”). There is a reasonable
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`likelihood that Petitioner will prevail with respect to at least one claim challenged
`
`in this petition.
`
`
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`II. MANDATORY NOTICES (37 C.F.R. § 42.8)
`
`A. Real Party-in-Interest (37 C.F.R. § 42.8(b)(1))
`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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`IPR2019-00451
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`U.S. Patent No. 9,763,876 B2
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`B. Related Matters (37 C.F.R. § 42.8(b)(2))
`Petitioner filed a Petition for Inter Partes Review (“IPR”) against U.S.
`
`Patent No. 9,763,876, under case number IPR2019-00449 on January 28, 2019 and
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`is concurrently filing a Petition for IPR against U.S. Patent No. 9,763,876 under
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`case number IPR2019-00450. Petitioner is not aware of any other matters.
`
`
`
`C. Counsel (37 C.F.R. §§ 42.8(b)(3) and 42.10(a))
`Petitioner designates the following individuals as its lead counsel and back-
`
`up lead counsel:
`
`Lead Counsel:
`
`Back-up Lead Counsel
`
`Daniel A. Scola, Jr.
`Reg. No. 29,855
`Hoffmann & Baron, LLP
`dscola@hbiplaw.com
`(973) 331-1700
`
`
`
`
`
`
`
`Michael I. Chakansky
`Reg. No. 31,600
`Hoffmann & Baron, LLP
`mchakansky@hbiplaw.com
`(973) 331-1700
`
`James F. Harrington
`Reg. No. 44,741
`Hoffmann & Baron, LLP
`jharrington@hbiplaw.com
`516-822-3550
`
`Matthew J. Solow
`Reg. No. 56,878
`Hoffmann & Baron, LLP
`msolow@hbiplaw.com
`(973) 331-1700
`
`2
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`IPR2019-00451
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`U.S. Patent No. 9,763,876 B2
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`Service Information (37 C.F.R. § 42.8(b)(4))
`
`D.
`Service on Petitioner may be made electronically by using all the following
`
`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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`Hand-Delivery or facsimile addressed to Lead and Back-up Lead Counsel at the
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`following address, but electronic service above is requested:
`
`Hoffmann & Baron, LLP
`6 Campus Drive
`Parsippany, New Jersey 07054
`Facsimile: 973-331-1717
`
`
`
`III. PAYMENT OF FEES
`
`Pursuant to 37 C.F.R. §§ 42.103 and 42.15(a), the undersigned authorizes
`
`PTO to charge the $47,900.00 fee for the 36 claims requested for review (request
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`fee of $15,500.00 plus $4,800.00 excess claims request fee; and post-institution fee
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`of $15,000.00 plus $12,600.00 excess claims post-institution fee) for this IPR
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`Petition to Deposit Account No. 08-2461. The undersigned further authorizes
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`payment from and to the above referenced Deposit Account for any additional fees
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`or refund that may be due in connection with this petition and IPR proceeding.
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`IPR2019-00451
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`IV. ADDITIONAL REQUREMENTS FOR INTER PARTES REVIEW
`
`U.S. Patent No. 9,763,876 B2
`
`
`
`A. Grounds for Standing (37 C.F.R. § 42.104(a))
`Petitioner hereby certifies that ‘876 Patent is available for IPR and that
`
`Petitioner is not barred or estopped from requesting IPR challenging the claims of
`
`‘876 Patent on the grounds identified herein.
`
`
`
`Level of Ordinary Skill in the Art
`
`B.
`As of the earliest priority date that the Challenged Claims of ‘876 Patent are
`
`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,
`
`nasolacrimal, buccal, sublingual, urethral, inhalation, and auricular)
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`pharmaceutical formulation development and/or delivery, the amount of post-
`
`graduate experience depending upon the level of formal education. The individual
`
`would also have some experience in design and testing of formulations for mucosal
`
`delivery (and particularly in intranasal formulations) of systemic-acting drugs.
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`4
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`IPR2019-00451
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`U.S. Patent No. 9,763,876 B2
`
`C.
`
`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 1-36 (“the
`
`Challenged Claims”) are found unpatentable and cancelled from ‘876 Patent.
`
`
`
`1.
`
`Claims for which IPR is Requested
`(37 C.F.R. § 42.104(b)(1))
`Petitioner requests inter partes review of Claims 1-36 of ‘876 Patent. See
`
`also SAS Inst., Inc. v. Iancu, 138 S.Ct. 1348 (April 24, 2018).
`
`
`
`2.
`
`Specific Statutory Grounds on Which the Challenge is
`Based (37 C.F.R. § 42.104(b)(2))
`
`Ground
`
`Reference(s)
`
`Basis
`
`Claims Challenged
`
`Gwozdz
`(Exhibit 1014)
`&
`Meezan‘962
`(Exhibit 1011)
`
`Gwozdz
`(Exhibit 1014)
`&
`Meezan‘962
`(Exhibit 1011)
`&
`Cartt‘784
`(Exhibit 1015)
`
`1
`
`2
`
`
`
`
`
`35 U.S.C. § 103(a)
`
`1-16, 24-36
`
`35 U.S.C. § 103(a)
`
`17-23
`
`5
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`IPR2019-00451
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`U.S. Patent No. 9,763,876 B2
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`Petitioner also relies on the expert declaration of Nicholas A. Peppas, Sc.D.
`
`(Exhibit 1041, hereinafter “Peppas”) and on ‘876 Patent admitted prior art.
`
`
`
`Gwozdz qualifies as prior art to the Challenged Claims under at least 35
`
`U.S.C. § 102(e)(1), based on the March 28, 2008 filing date of its U.S. Provisional
`
`Application No. 61/040,281 (“Gwozdz provisional”, Exhibit 1046) and the
`
`Challenged Claims’ effective filing date of no earlier than March 27, 2009. As
`
`required for Gwozdz (Exhibit 1014) to be effective as prior art as of the March 28,
`
`2008 filing date of Gwozdz provisional1, Gwozdz’s (Exhibit 1014) claims are fully
`
`supported by Gwozdz provisional, at least because Gwozdz’s claims are literally
`
`identical to the claims filed in Gwozdz provisional. See Gwozdz, Exhibit 1014, pp.
`
`1014-1015; see also Gwozdz provisional, Exhibit 1046, pp. 0019-0020. In this
`
`regard, Gwozdz’s and (identical) Gwozdz provisional’s claims: (i) are not defined
`
`by functional language, and (ii) are not broad unsupported genus claims. See, e.g.,
`
`
`
`1
`
`See Dynamic Drinkware, LLC v. Nat'l Graphics, Inc., 800 F.3d 1375, 1381
`
`(Fed.Cir. 2015) (“A provisional application's effectiveness as prior art
`
`depends on its written description support for the claims of the issued patent
`
`of which it was a provisional.”).
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`IPR2019-00451
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`Ariad Pharms., Inc. v. Eli Lilly & Co., 598 F.3d 1336, 1349-1350 (Fed.Cir. 2010).
`
`U.S. Patent No. 9,763,876 B2
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`
`
`Therefore, Gwozdz (Exhibit 1014) is effective as prior art to the Challenged
`
`Claims as of Gwozdz provisional’s March 28, 2008 filing date. See, e.g., Gwozdz,
`
`Exhibit 1014, p. 0000 (priority data section); see also Gwozdz provisional, Exhibit
`
`1046, p. 0001 (filing receipt showing filing date). Because this March 28, 2008
`
`date is the effective filing date for a published application and because the date is
`
`earlier than ‘876 Patent’s earliest effective filing date, Gwozdz (Exhibit 1014)
`
`qualifies as prior art under at least 35 U.S.C. § 102(e)(1).
`
`Moreover, Gwozdz (Exhibit 1014) does not fall under the exception codified
`
`at 35 U.S.C. § 103(c) because Gwozdz and the Challenged Claims, at the earliest
`
`effective filing date of the Challenged Claims (March 27, 2009), had different
`
`ownership with no obligation to assign. In particular, at the relevant time, Gwozdz
`
`was owned by “Particle Sciences, Inc.” See Gwozdz, Exhibit 1014, p. 0000
`
`(listing “Particle Sciences, Inc.” as Applicant). Additionally, Gwozdz provisional
`
`was assigned to Particle Sciences, Inc. as of April 21, 2008. See Gwozdz
`
`Assignment, Exhibit 1047, p. 0003-0005. At no time was ‘876 Patent owned by
`
`Particle Sciences, Inc. Therefore, the exception under 35 U.S.C. § 103(c) does not
`
`apply, and Gwozdz (Exhibit 1014) is prior art to ‘876 Patent under at least 35
`
`U.S.C. § 102(e)(1).
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`IPR2019-00451
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`U.S. Patent No. 9,763,876 B2
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`Meezan’962 was published March 2, 2006, which is more than one year
`
`before the Challenged Claims’ effective filing date of no earlier than March 27,
`
`2009. Therefore, Meezan’962 qualifies as prior art under at least 35 U.S.C. §
`
`102(b).
`
`Cartt‘784 (Exhibit 1015) qualifies as prior art to the Challenged Claims
`
`under at least 35 U.S.C. § 102(e)(1), based on its May 7, 2008 filing date and also
`
`its November 13, 2008 publication date. See Cartt‘784, Exhibit 1015, p. 0000.
`
`The exception under 35 U.S.C. 103(c) is inapplicable because at the time of the
`
`invention of the Challenged Claims (i.e., March 27, 2009), Cartt’784 was owned
`
`by inventor Edward T. Maggio, possibly with an obligation to assign to Aegis
`
`Therapeutics, LLC. Inventor Maggio did assign his interest to Aegis Therapeutics
`
`on March 6, 2012. See Cartt’784 Assignment, Exhibit 1049. At no time was ‘876
`
`Patent owned by Aegis Therapeutics, LLC. Therefore, the exception under 35
`
`U.S.C. § 103(c) does not apply, and Cartt’784 (Exhibit 1015) is prior art to ‘876
`
`Patent under at least 35 U.S.C. § 102(e)(1).
`
`
`
`35 U.S.C. § 325(d) Should Not Bar the Petition
`3.
` When considering a petition for inter partes review, “the Director may take
`
`into account whether, and reject the petition or request because, the same or
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`IPR2019-00451
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`substantially the same prior art or arguments previously were presented to the
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`U.S. Patent No. 9,763,876 B2
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`
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`Office.” 35 U.S.C. § 325(d). Here, the specific combination of subject matter from
`
`prior art references relied upon by Petitioner did not form the basis for any
`
`rejections of ‘876 Patent.
`
`Although Meezan‘962 was relied on by the Examiner during prosecution of
`
`both the parent ‘546 Patent and grandparent ‘439 application, this Petition applies
`
`it in a new light, in a combination with a different primary reference (Gwozdz)
`
`than considered by an Examiner, through arguments not previously presented to
`
`the Patent Office, and with support of expert opinion from Dr. Peppas (Ex. 1041).
`
`
`V. 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
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`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.
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`IPR2019-00451
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`1998). If a feature is not necessary to give meaning to what inventors mean by a
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`U.S. Patent No. 9,763,876 B2
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`claim term, it would be “extraneous” and should not be read into the claim.
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`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
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`Petitioner is precluded from presenting challenges under 35 U.S.C. § 112 in an
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`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.
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`IPR2019-00451
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`U.S. Patent No. 9,763,876 B2
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`B. Claim Construction Summary Chart
`
`Claim Term
`
`Construed Claim Term
`“any of the natural or synthetic tocopherols,
`
`vitamin E
`
`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
`
`% (w/w)
`
`% (w/v)
`
`Dose(IN)]) times 100%”
`
`“% (w/v) or % (w/w)”
`
`“% (w/v) or % (w/w)”
`
`“about 56.47% (w/v) vitamin E” “53.65% to 59.29% (w/v) vitamin E”
`
`
`
`
`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
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`IPR2019-00451
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`thereof, or any combinations thereof.” See ‘876 Patent, 33:8-23, Exhibit 1001, p.
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`U.S. Patent No. 9,763,876 B2
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`
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`0026; see also Peppas, Exhibit 1041, ¶¶82-85.
`
`
`2.
`‘876 Patent defines “bioavailability” as:
`
`“Bioavailability”
`
`“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 one of the bibles of the
`
`pharmacokinetic discipline (Peppas, Exhibit 1041, ¶87), provides the following
`
`equation at p. 506:
`
`12
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`IPR2019-00451
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`U.S. Patent No. 9,763,876 B2
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`Based on the definition in ‘876 Patent, which agrees with Ritschel’s formula,
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`“bioavailability” should be construed as meaning: “bioavai