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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`Case No.: IPR2019-00450
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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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`BEFORE THE PATENT TRIAL AND APPEAL BOARD
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`AQUESTIVE THERAPEUTICS, INC.
`
`Petitioner
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`v.
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`HALE BIOPHARMA VENTURES, LLC
`
`Patent Owner
`
`
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`
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`Case No.: IPR2019-00450
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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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`
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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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`IPR2019-00450
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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. 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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`PAYMENT OF FEES .................................................................................. 3
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`IV.
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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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`1. Claims for Which IPR is Requested (37 C.F.R. § 42.104(b)(1)) .. 5
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`2. Specific Statutory Ground on Which the Challenge is Based (37
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`C.F.R. § 42.104(b)(2)) ...................................................................................... 5
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`3.
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`35 U.S.C. § 325(d) should not bar the Petition ...................................... 6
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`V. CLAIM CONSTRUCTION ..........................................................................11
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`A. Ordinary and Customary Meaning (37 C.F.R. § 42.104(b)(3) .............11
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`B. Claim Construction Summary Chart ......................................................13
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`C. Construction Of ‘876 Patent Claim Terms .............................................14
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`1.
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`2.
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`3.
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`4.
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`“Vitamin E” ............................................................................................14
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`“Bioavailability” .....................................................................................14
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`“% (w/w)” and “% (w/v)” .....................................................................15
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`“about 56.47% (w/v) vitamin E” ..........................................................16
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`VI.
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`‘876 PATENT FAMILY HISTORY CHART .........................................17
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`VII. EARLIEST EFFECTIVE PRIORITY DATE IS NO EARLIER
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`THAN MARCH 27, 2009 ......................................................................................20
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`VIII. SUMMARY OF ‘876 PATENT ................................................................23
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`A. Background of ‘876 Patent ........................................................................23
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`B. Prosecution History of ‘876 Patent...........................................................23
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`IX.
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`PRIOR ART REFERENCES RELIED ON BY PETITIONER ...........25
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`A. Sonne, U.S. Patent No. 6,193,985 (“Sonne”, Exhibit 1013) ....................25
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`1. General Teachings .................................................................................25
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`2. Specific Teachings ..................................................................................26
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`B. Meezan et al., U.S. Publication No. 2006/0046962
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`(“Meezan‘962”, Exhibit 1011) ..........................................................................35
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`1. General Teachings .................................................................................35
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`2. Combined With Sonne ...........................................................................36
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`C. Motivation to Combine Sonne and Meezan’962 .....................................38
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`X. THERE IS A REASONABLE LIKELIHOOD THAT AT LEAST ONE
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`OF THE CHALLENGED CLAIMS IS UNPATENTABLE .............................39
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`A. Grounds Chart ...........................................................................................40
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`B. Discussion of Ground 1 ..............................................................................40
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`1.
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`Independent Claim 1..............................................................................41
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`2. Claim 2 ....................................................................................................46
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`3. Claims 3-4 ...............................................................................................47
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`4. Claims 5-6 ...............................................................................................48
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`5. Claim 7 ....................................................................................................48
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`6. Claims 8 and 15 ......................................................................................49
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`7. Claims 9-10 .............................................................................................50
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`8. Claims 11-12 ...........................................................................................51
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`9. Claims 13-14 ...........................................................................................52
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`10. Claim 16 ...............................................................................................53
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`11. Claims 17-18 ........................................................................................54
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`12. Claims 19-22 ........................................................................................55
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`13. Claim 23 ...............................................................................................57
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`14. Claims 24-26 ........................................................................................58
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`15. Claims 27 and 29 .................................................................................60
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`16. Claim 28 ...............................................................................................60
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`17. Claims 30-31 ........................................................................................61
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`18. Claims 32-33 ........................................................................................62
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`19. Claims 34-36 ........................................................................................64
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`XI. GROUNDS AND CLAIM CHART..........................................................66
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`A. Ground 1 .....................................................................................................66
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`B. Claims Chart ..............................................................................................67
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`XII. CONCLUSION ..........................................................................................94
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`XIII. CERTIFICATE OF COMPLIANCE ......................................................95
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`EXHIBIT LIST
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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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`
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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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`vi
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`IPR2019-00450
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`U.S. Patent No. 9,763,876 B2
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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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`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)
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`vii
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`IPR2019-00450
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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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`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 Composition for
`Treatment of Seborrheic Keratosis, 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
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`1030
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`1031
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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)
`
`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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`“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)
`
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`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
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`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,
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`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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`Cartt’784 Assignment, dated March 6, 2012, recorded March
`29, 2012 (Cartt’784 Assignment)
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`Table of Various Diazepam Solutions Described in or Modified
`From Sonne’s Example 11 (“DS11”)
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`IPR2019-00450
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`I.
`
`THE PETITION
`
`
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`U.S. Patent No. 9,763,876 B2
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`Petitioner, real party-in-interest, Aquestive Therapeutics, Inc. (“Aquestive”
`
`or “Petitioner”) (formerly Monosol RX, LLC), hereby petitions the Patent Trial
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`and Appeal Board (“PTAB”) of the USPTO, pursuant to 35 U.S.C. §§ 311-319 and
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`37 C.F.R. § 42.1 et seq., to institute an inter partes review and find unpatentable
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`and cancel Claims 1-36 (“the Challenged Claims”) of U.S. Patent No. 9,763,876
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`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
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`in this petition.
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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))
`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))
`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 IPR2019-00451. Petitioner is not aware of any other matters.
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`
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`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-
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`up lead counsel:
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`Lead Counsel:
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`Back-up Lead Counsel
`
`Daniel A. Scola, Jr.
`Reg. No. 29,855
`Hoffmann & Baron, LLP
`dscola@hbiplaw.com
`(973) 331-1700
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`
`
`
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`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
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`Service Information (37 C.F.R. § 42.8(b)(4))
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`D.
`Service on Petitioner may be made electronically by using all the following
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`four 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:
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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 $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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`IV. ADDITIONAL REQUREMENTS FOR INTER PARTES REVIEW
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`U.S. Patent No. 9,763,876 B2
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`
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`A. Grounds for Standing (37 C.F.R. § 42.104(a))
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`Petitioner hereby certifies that ‘876 Patent is available for IPR and Petitioner
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`is not barred or estopped from requesting IPR challenging the claims of ‘876
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`Patent on the ground identified herein.
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`
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`B.
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`Level of Ordinary Skill in the Art
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`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 upon 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.
`4
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`U.S. Patent No. 9,763,876 B2
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`IPR2019-00450
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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))
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`
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`The precise relief requested by Petitioner is that Claims 1-36 (“the
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`Challenged Claims”) are found unpatentable and cancelled from ‘876 Patent.
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`
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`1.
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`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
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`also SAS Inst., Inc. v. Iancu, 138 S.Ct. 1348 (April 24, 2018).
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`2.
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`Specific Statutory Ground on Which the Challenge is Based
`(37 C.F.R. § 42.104(b)(2))
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`Ground
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`Reference(s)
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`Basis
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`Claims Challenged
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`1
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`Sonne
`(Exhibit 1013)
`&
`Meezan‘962
`(Exhibit 1011)
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`35 U.S.C. § 103(a)
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`1-36
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`Petitioner also relies on the expert declaration of Nicholas A. Peppas, Sc.D.
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`(Exhibit 1041, hereinafter “Peppas”) and on ‘876 Patent admitted prior art.
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`5
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`Both Sonne and Meezan‘962 qualify as prior art to the Challenged Claims
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`U.S. Patent No. 9,763,876 B2
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`under at least 35 U.S.C. § 102(b) because they were issued/published more than
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`one year prior to ‘876 Patent’s March 27, 2009 earliest effective filing date1:
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`102(b) Reference
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`Publication/Issue Date
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`Exhibit No.
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`Sonne
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`Meezan‘962
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`February 27, 2001
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`March 2, 2006
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`1013
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`1011
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`
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`35 U.S.C. § 325(d) should not bar the Petition
`3.
` When considering a petition for inter partes review, “the Director may take
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`into account whether, and reject the petition or request because, the same or
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`substantially the same prior art or arguments previously were presented to the
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`Office.” 35 U.S.C. § 325(d). Here, the specific combination of subject matter from
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`prior art references relied upon by Petitioner did not form the basis for any of the
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`rejections of ‘876 Patent.
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`Although both Sonne and Meezan‘962 were relied on by the Examiner
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`during prosecution of the parent ‘546 Patent and grandparent ‘439 application, this
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`1
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`The earliest effective filing date is discussed in more detail in Section VII
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`below.
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`6
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`IPR2019-00450
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`Petition applies them in a new light, through arguments not previously presented to
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`U.S. Patent No. 9,763,876 B2
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`
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`the USPTO, and with support of expert opinion from Dr. Peppas (Exhibit 1041).
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`It is also notable that during prosecution of the parent ‘546 Patent, PO
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`mislead the Examiner away from a full and fair consideration of Sonne. PO stated
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`that “while Sonne mentions using ethanol as a viscosity-reducing agent [Col. 3,
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`lines 60-67], this teaching appears in the context of introducing the purported
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`benefits of the therein-described colloidal formulations.” ‘546 FH, Exhibit 1004,
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`p. 2149 (footnotes omitted). PO’s statement is incorrect and misleading. In fact,
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`Sonne discussed solutions having a high viscosity, with such viscosity (of
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`solutions) being reduced by using ethanol as a co-solvent. It was only after Sonne
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`finished discussing the use of ethanol to reduce viscosity of solutions that Sonne
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`turned to colloidal formulations (i.e., emulsions) as one alternative to thinning a
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`solution with ethanol, i.e., Sonne simply suggested colloidal formulations as an
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`alternative to using ethanol to lessen a solution’s viscosity. Sonne’s discussion of
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`ethanol was not an introduction to the benefits of emulsions. Rather, Sonne
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`provided two possibilities (solutions with ethanol, and solutions converted into
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`emulsions) but was not teaching away from solutions with ethanol:
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`7
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`IPR2019-00450
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`U.S. Patent No. 9,763,876 B2
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`“The compositions of the invention may be used
`directly as solutions of the bioactive agent in the
`tocopherol solvent. However such solutions are viscous,
`and
`the viscosity may be
`too high for certain
`applications, for example
`to achieve a sprayable
`formulation for nasal application.
`Viscosity can be reduced by addition of co-
`solvents such as ethanol, but this is less desired, since
`solutions of this kind tend to be irritating to certain
`mucosal tissues.
`Alternatively, the tocopherol solutions may be
`emulsified, to obtain formulations of lower viscosity.”
`Sonne, 3:60-4:2, Exhibit 1013, p. 0005 (emphasis added); see also Peppas,
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`Exhibit 1041, ¶176.
`
`
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`PO further mislead the Examiner in the grandparent ‘439 application away
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`from a proper consideration of Sonne in its entirety, and Example 11 specifically.2
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`Sonne’s Example 11 is a diazepam nosedrop solution:
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`2
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`Sonne’s Example 11 is incredibly significant as applied to ‘876 Patent’s
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`claims (discussed in more detail throughout this Petition).
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`U.S. Patent No. 9,763,876 B2
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`Sonne, 11:1-10, Exhibit 1013, p. 0009.
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`In attempting to overcome the Examiner’s reliance on Sonne in an
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`
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`obviousness rejection, PO misleadingly referred to a list of Sonne’s Examples,
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`including Example 11, as being directed to oil-in-water emulsions and stated
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`“[s]uch emulsions are specifically excluded from the instant claims, which recite
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`solutions (not emulsions)”. ‘439 FH, Exhibit 1007, pp. 0501, 0564, 2833
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`(emphasis in original); see also p. 502 (PO describing several Examples, including
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`Example 11, as “an oil-in-water emulsion of a benzodiazepine for nasal
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`administration.”). Contrary to PO’s assertion, Example 11 is clearly a solution.
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`PO further muddied Sonne’s disclosure and mislead the Examiner away
`
`from Example 11: “Example 11 is an oral solution of diazepam, α-tocopherol and
`
`triacetin”. ‘439 FH, Exhibit 1007, p. 0502 (emphasis added). Clearly, Example 11
`
`is a nosedrop, intended for intranasal administration. PO’s direct statement that
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`Example 11 is an oral solution is demonstrably false and misleading.
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`9
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`U.S. Patent No. 9,763,876 B2
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`PO further mislead the Examiner away from considering, inter alia, Sonne’s
`
`Example 11, arguing: a POSITA “would reasonably infer from the teachings of
`
`column 3, lines 65-67 and the various examples that nasal formulations should be
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`oil-in-water formulations, with a high concentration of oil.” ‘439 FH, Exhibit
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`1007, p. 0502 (emphasis added). PO’s statement is highly misleading. In fact,
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`Sonne clearly indicated that nasal formulations could be solutions, as evidenced by
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`Example 11. Sonne did not limit nasal formulations to oil-in-water formulations
`
`(emulsions).
`
`Lastly, the Examiner mistakenly believed that Sonne did not disclose alkyl
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`glycosides. See, e.g., ‘546 FH, Exhibit 1004, p. 2126 (“Sonne does not teach the
`
`addition of an alkyl glycoside.”); see also ‘439 FH, Exhibit 1007, pp. 3071, 3097,
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`3315, 3474 (“Sonne does not teach the surfactant is an alkyl glycoside.”).
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`However, the Examiner was incorrect, and PO never corrected the Examiner.
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`Sonne specifically discloses cetearyl glucoside (an alkyl glycoside) in certain
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`emulsion formulations. See, e.g., Sonne, 4:50-53, 6:54-59, 10:61, 13:17, Exhibit
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`1013, pp. 0005, 0006, 0008, 0010. While being taught with respect to emulsions
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`and not solutions, Sonne clearly teaches alkyl glycosides (contrary to the
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`Examiner’s understanding).
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`10
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`U.S. Patent No. 9,763,876 B2
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`Thus, with respect to the parent and grandparent applications, any Examiner
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`consideration of Sonne: (1) was tainted by PO’s misleading statements regarding
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`Sonne generally, and Example 11 specifically; (2) was incomplete and did not
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`consider Sonne’s full teachings; (3) inadvertently misunderstood that Sonne
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`actually did disclose alkyl glycosides; (4) involved claim language different from
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`that in ‘876 Patent; (5) did not have the benefit of Dr. Peppas’ expertise; and (6)
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`was limited to a legal theory different from that presented here. Accordingly, 35
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`U.S.C. § 325(d) does not foreclose this Petition. See, e.g., Taro Pharmaceuticals
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`USA, Inc. v. Apotex Technologies, Inc., IPR2017-01446, Paper No. 7 at 18 (PTAB
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`November 28, 2017); Baker Hughes Inc. v. Liquidpower Specialty Products Inc.,
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`IPR2016-01905, Paper No. 10 at 11-13 (PTAB April 10, 2017); Cisco System, Inc.
`
`v. Spherix Portfolio Acquisition II, Inc., IPR2015-00999, Paper No. 11 at 13
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`(PTAB September 22, 2015); Chimei Innolux Corp. v. Semiconductor Energy Lab.
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`Co., Ltd., IPR2013-00066, Paper No. 10 at 7-8 (PTAB April 24, 2013).
`
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`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
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`customary meaning of such claim as understood by a POSITA and the prosecution
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`11
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`IPR2019-00450
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`history pertaining to the patent. 37 C.F.R. § 42.100. See Phillips v. AWH Corp.,
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`U.S. Patent No. 9,763,876 B2
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`
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`415 F.3d 1303 (Fed. Cir. 2005) (en banc).
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`For inventors to act as their own lexicographer, the definition must be set
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`forth in the specification with reasonable clarity, deliberateness, and precision.
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`Renishaw PLC v. Marposs Societa’ per Azioni, 158 F.3d 1243, 1249 (Fed. Cir.
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`1998). If a feature is not necessary to give meaning to what inventors mean by a
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`claim term, it is “extraneous” and should not be read into the claim. Renishaw
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`PLC, 158 F.3d at 1249; E.I. du Pont de Nemours & Co. v. Phillips Petroleum Co.,
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`849 F.2d 1430, 1433 (Fed. Cir. 1988). The construction that stays true to the claim
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`language and most naturally aligns with the inventors’ description is likely the
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`correct interpretation. See Renishaw PLC, 158 F.3d at 1250.
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`Petitioner’s position regarding the scope of ‘876 Patent’s claims should not
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`be taken as an assertion regarding the appropriate claim scope in other adjudicative
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`forums where a different claim interpretation standard may apply. Moreover,
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`Petitioner reserves all rights to further challenge any claim terms herein under 35
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`U.S.C. § 112, including by arguing that the terms are not definite, supported by the
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`written description, and/or enabled. Further, as Petitioner is precluded from
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`presenting challenges under 35 U.S.C. § 112 in an IPR, Petitioner’s arguments in
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`this Petition, or lack thereof on any of these grounds, should not be interpreted as
`12
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`IPR2019-00450
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`waiving or conflicting with arguments available in other forums under 35 U.S.C. §
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`U.S. Patent No. 9,763,876 B2
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`112.
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`B. Claim Construction Summary Chart
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`Claim Term
`
`vitamin E
`
`bioavailability
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`% (w/w)
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`% (w/v)
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`Construed Claim Term
`“any of the natural or synthetic tocopherols,
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`tocotrienols, any isomers thereof, any esters
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`thereof, any analogs or derivatives thereof, or
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`any combinations thereof”
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`“bioavailability, determined by the ratio of
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`([AUC∞(IN) x Dose(IV)] divided by [AUC∞(IV) x
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`Dose(IN)]) times 100%”
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`“% (w/v) or % (w/w)”
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`“% (w/v) or % (w/w)”
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`“about 56.47% (w/v) vitamin E” “53.65% to 59.29% (w/v) vitamin E”
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`13
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`IPR2019-00450
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`C. Construc
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