Ex Parte Saltel et al

Patent Trial and Appeal Board

Feb 14, 2018

14150493 (P.T.A.B. Feb. 14, 2018)

United States Patent and Trademark Office
UNITED STATES DEPARTMENT OF COMMERCE
United States Patent and Trademark Office
Address: COMMISSIONER FOR PATENTS
P.O.Box 1450
Alexandria, Virginia 22313-1450
www.uspto.gov
APPLICATION NO. FILING DATE FIRST NAMED INVENTOR ATTORNEY DOCKET NO. CONFIRMATION NO.
14/150,493 01/08/2014 Douglas A. Saltel 096563-0173 3088
22428 7590 02/16/2018
Foley & Lardner LLP
3000 K STREET N.W.
SUITE 600
WASHINGTON, DC 20007-5109
EXAMINER
BASQUILL, SEAN M
ART UNIT PAPER NUMBER
1613
NOTIFICATION DATE DELIVERY MODE
02/16/2018 ELECTRONIC
Please find below and/or attached an Office communication concerning this application or proceeding.
The time period for reply, if any, is set in the attached communication.
Notice of the Office communication was sent electronically on above-indicated "Notification Date" to the
following e-mail address(es):
ipdocketing @ foley. com
PTOL-90A (Rev. 04/07)
UNITED STATES PATENT AND TRADEMARK OFFICE
BEFORE THE PATENT TRIAL AND APPEAL BOARD
Ex parte DOUGLAS A. SALTEL and MICHAEL VACHON
Appeal 2016-004580
Application 14/150,49s1
Technology Center 1600
Before DEBORAH KATZ, ULRIKE W. JENKS, and DAVID COTTA,
Administrative Patent Judges.
COTTA, Administrative Patent Judge.
DECISION ON APPEAL
This is an appeal under 35 U.S.C. § 134(a) involving claims directed
to a pharmaceutical composition. The Examiner rejected the claims on
appeal under 35 U.S.C. § 103(a) as obvious.
We AFFIRM.
1 According to Appellants, the real party in interest is Edgemont
Pharmaceuticals, LLC. App. Br. (Appeal Brief filed Oct. 2, 2015
“App. Br.”) 2.
Appeal 2016-004580
Application 14/150,493
STATEMENT OF THE CASE
The Specification discloses that lorazepam “has proven to be a useful
treatment for anxiety related disorders” and “has been sold commercially
under the brand name ATIVAN® (originally by Wyeth, now by Valeant
Inti) in the form of an oral immediate release tablet.” Spec. 2]Hf 3, 4. “While
the immediate release tablets of lorazepam, with a multi-dose per day
regimen, have been available for several decades, thus far no once-a-day
dosage form has been commercially introduced. Such a dosage form is often
desirable.” Id. 15. The Specification suggests that “[a] lorazepam
formulation that provides a sustained release profile with the potential for an
effective and well tolerated once daily dosing regimen would be
advantageous.” Id. 1 8. The Specification discloses that “[t]he present
invention relates to controlled release formulations of lorazepam and to
methods of treating patients with a once-a-day dose of lorazepam.” Id. 12.
Claims 1—16 and 19 are on appeal. Claim 1 is illustrative and reads as
follows:
1. A pharmaceutical composition, comprising 0.5 to 10 mg of
lorazepam in combination with sufficient pharmaceutically acceptable
excipients to provide a solid oral dosage form having controlled
release of said lorazepam; wherein said controlled release of
lorazepam is (1) substantially zero order release and (2) the release of
lorazepam reaches 90% within the time range of 7 to 12 hours; and
wherein said controlled release parameters are determined in a
pharmaceutical dissolution test comprising a buffer of pH 6.8.
App Br. 20.
2 Specification filed Jan. 8, 2014 (“Spec.”).
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Application 14/150,493
The Examiner rejected claims 1—16 and 19 under 35 U.S.C. § 103(a)
as obvious over the combination of Sako3 and Peck.4 Final Act.5 3.
FINDINGS OF FACT
1. Sako discloses: “The present invention provides a stable
preparation that shows no changes in drug release in matrix type sustained-
release preparations containing polyethylene oxide at the preserved period
under exposure to light.” Sako, col. 1,1. 66 — col. 2,1. 2
2. Sako discloses: “There are no special restrictions to the drug
used in the present invention as long as it is a drug used in sustained-release
preparations that contain polyethylene oxide as one its base components.”
Id. at col. 3,11. 44^47. Among the drugs listed as suitable for use in Sako’s
sustained release preparations is lorazepam. Id. at col. 3,1. 65.
3. Sako discloses: “There are no special restrictions to the
polyethylene oxide used in the present inventions as long as it can control
release of the drug from the preparation.” Id. at col. 4,11. 55—58. Sako
discloses a number of different polyethylene oxides as being suitable for use
in its sustained release preparations. The polyethylene oxides exemplified
have molecular weights ranging from 7,000,000 to 1,700,000. Id. at col. 4,1.
57 — col. 5,1. 25. Sako discloses that preferably the polyethylene oxide has a
molecular weight of “2,000,000 or higher” and that “[o]ne or a combination
of two or more with different molecular weights, grades, etc., can be used as
the PEO [(polyethylene oxide)] of the present invention.” Id. at col. 5,11.
25-27.
3 Sako et al., US Patent No. 6,562,375 Bl, issued May 13, 2003 (“Sako”).
4 Peck, US Patent No. 4,571,395, issued Feb. 18, 1986 (“Peck”).
5 Office Action mailed Oct. 2, 2014 (“Final Act.”).
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Application 14/150,493
4. Sako discloses: “There are no special restrictions to the ratio of
polyethylene oxide added in the present invention as long as it is the amount
with which release of drug from the preparation usually can be controlled.
However, 10 to 95 wt % in terms of total preparation, or 15 to 90 wt % in
terms of total preparation, is preferably used.” Id. at col. 5,11. 31—36.
5. Peck discloses that lorazepam was known to treat anxiety.
Peck, col. 1,11. 23—55.
6. Peck discloses that suitable amounts of lorazepam for oral
administration include “0.5 mg, 1 mg and 2 mg.” Id. at col. 4,11. 32-41.
7. Peck discloses its formulation may be presented as tablets and
that the tablets may be “formulated so as to provide slow or controlled
release of the active ingredients therein.” Id. at col. 3,11. 48—68.
8. The Specification exemplifies the following composition.
Reference Litii (Cowijiiisiftan
Component
to Quality
Standards Function miyTottkt % wcw
Lotaispam USP Active ingredient 2.0 1.35
Calcium hydrogen pbosphate
dihydrate (EMCWMPRESS.*)
USP Fillev/C'orspression
aid
3S.S 25,65
Polyethylene oxide
(Pofyox WS8 N~f 2K.)
NT Release control
agent.
67,5 45.00
Lactose (Tswiobydraie USP V-' Filler AQ.5 27.00
Magnesium .stearate Usf’M Lubricant 1.5 i
Tout .150.0 fOO.O
USP •••• United Stetev Pharmacopeia.
NF - National Formniary.
Spec. 144. The Specification reports that this composition has “a
substantially zero order release and reach[es] 90% release at 8 hours.” Id. 1
47.
9. The Specification discloses: “Typically the tablets are formed
with PEO having an average MW between 900,000 and 4,000,000, more
typically from 900,000 to about 2,000,000.” Id. 129.
10. The Specification discloses: “When the matrix polymer is
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Application 14/150,493
primarily (or exclusively) PEO having a MW from 900,000 to 1,500,000, the
amount of matrix polymer is often in the range of 35 to 55%, including 40%
to 50%. Matrix polymer having higher MW PEO is generally used in
slightly lower amounts such as 20% to 50%, including 25% to 45%.” Spec.
130.
ANALYSIS
Claims E 2, 5, 6, and 10-16
Appellants argue claims 1, 2, 5, 6, and 10—16 together. App. Br. 6—
17. We designate claim 1 as representative.
In finding claim 1 obvious, the Examiner found that Sako taught the
“formulation of solid pharmaceutical oral dosage forms by incorporating
active agents in a matrix comprising polyethylene oxide.” Final Act. 3. The
Examiner further found that Sako taught that “the antipsychotic agent
lorazepam may suitably be formulated in this manner.” Id. at 4.
With respect to the claim requirements for “substantially zero order
release” and for the “release of lorazepam [to] reach[] 90% within the time
range of 7 to 12 hours” (hereinafter “the claimed release profile”), the
Examiner relied upon routine optimization. The Examiner explained:
Sako clearly teaches both the desirability of a stable and steady
release rate from sustained-release drug preparations (Col. 1,
L.25-33), and also indicates that it is the PEO matrix containing
the desired active agent, and more particularly the amount and
ratio of PEO which is utilized, which gives rise to the resulting
controlled release profile which the dosage forms provide. (Col.
4, L.55 - Col. 5, L.52). This teaching clearly both implies the
desirability of achieving a steady-state drug release, which the
skilled artisan would understand is synonymous with the
applicants desired zero-order drug release, and establishes that
the amount and ratio of PEO incorporated in the dosage forms
are what give rise to the sustained drug release profile,
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Application 14/150,493
establishing the release of drug from such a dosage form as a
result-effective variable suitable for optimization via routine
experimentation of an ordinarily skilled artisan. As such, the
explicit recitation of a particular dosage form containing
lorazepam and the drug release profile which applicants achieve
by this particularly claimed dosage form cannot serve to
patentably distinguish the invention claimed from the teachings
of Sako.
Id. at 8.
The Examiner acknowledged that Sako does not specify dosages of
lorazepam to be included. Id. at 4. However, the Examiner found that Peck
taught that “lorazepam is advantageously provided as 0.5, 1 or 2 mg unit
dosage forms.” Id. at 5. The Examiner concluded that it would have been
obvious to employ lorazepam in amounts between 0.5 — 2 mg because “the
art expressly indicates that lorazepam is a compound suitably formulated to
provide controlled release by its combination with polyethylene oxides . . .
[and] the art additionally acknowledges that therapeutically effective
dosages of lorazepam fall within the range of 0.5 — 2 mg.” Id. The
Examiner further explained that the “claimed arrangement amounts then to
little more than the use of a lorazepam dosage particularly described by the
art as therapeutically effective for treating lorazepam-treatable patients” in a
controlled release form. Id. at 5—6.
We agree with the Examiner that the composition of claim 1 would
have been obvious over the combination of Sako and Peck. We address
Appellants’ arguments below.
As an initial matter, we agree with Appellants that the claimed release
profile is more than a mere “intended use.” As Appellants explain, the
claimed release profile “serve[s] to define the nature and amount of
excipients in the inventive pharmaceutical composition via the resulting
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Application 14/150,493
functional ability.” App. Br. 9. The claimed release profile meaningfully
limits the content of the claimed composition and must be considered in
evaluating whether the claimed composition would have been obvious over
the cited prior art. In re Swinehart, 439 F.2d 210 (CCPA1971).
Appellants argue that the claimed release profile cannot be considered
the result of routine optimization because “Sako does not disclose the
claimed release parameters for a lorazepam composition; much less that they
are result effective parameters that could obviously be optimized.” App. Br.
17. We are not persuaded.
Sako and Peck both teach that that lorazepam is suitably provided in a
controlled release formulation. FF1, FF2, FF5—7. Sako teaches that the
release of profile of the active in its formulation is controlled by the type and
ratio of polyethylene oxide used. FF2, FF3. Moreover, the range of
polyethylene oxide disclosed in Sako encompasses the amount of
polyethylene taught to provide the claimed release profile. FF4, FF8.
Accordingly, we agree with the Examiner that the skilled artisan would have
arrived at the claimed release profile by the process of routine optimization.
Ans. 9 (citing In reAller, 220 F.2d 454 (CCPA 1955).
Appellants argue that “merely using PEO in a matrix does not
inherently result in a composition having the recited release parameters.”
Reply Br. 5. Appellants contend that “the specification teaches that both the
amount of PEO and its molecular weight, as well as other excipients that
may be present, affect the release of the lorazepam.” Reply. Br. 5 (citing
Spec. 129). Appellants are correct that the cited portion of the Specification
teaches that the molecular weight of polyethylene oxide affects the release
rate of lorazepam. However, Appellants do not identify, and we do not find,
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Application 14/150,493
evidence that excipients other than polyethylene oxide affect the release rate.
In re Geisler, 116 F.3d 1465, 1470 (Fed. Cir. 1997); In re De Blauwe, 736
F.2d 699, 705 (Fed. Cir. 1984). And the molecular weight of the
polyethylene oxide used in Sako overlaps with that taught to be suitable by
the Specification. FF3, FF9. Moreover, the Specification suggests that the
effect of the molecular weight of polyethylene oxide on release rate can be
balanced to achieve the desired release rate by adjusting the amount of
polyethylene oxide present. FF10.
Accordingly, we affirm the Examiner’s rejection of claim 1. Because
they were not argued separately, claims 2, 5, 6, and 10—16 fall with claim l.6
Claims 3, 4, 7, 8, 9, and 19
Appellants argue claims 3, 4, 7, 8, 9, and 19 separately, but the only
argument made with respect to each claim is to assert, without explanation,
that the cited art does not teach or suggest the additional limitation. App. Br.
18. Appellants’ arguments are insufficient to properly raise an issue on
appeal. In re Lovin, 652 F.3d 1349, 1357 (Fed. Cir. 2011) (“[T]he Board
reasonably interpreted Rule 41.37 to require more substantive arguments in
an appeal brief than a mere recitation of the claim elements and a naked
assertion that the corresponding elements were not found in the prior art.
Because Lovin did not provide such arguments, the Board did not err in
refusing to separately address claims 2—15, 17—24, and 31—34.”).
Accordingly, we affirm the Examiner’s rejection of claims 3, 4, 7, 8, 9, and
19 as obvious over the combination of Sako and Peck.
6 We do not address the Examiner’s position that the composition rendered
obvious by the combination of Sako and Peck would inherently have the
claimed release profiled because it is not necessary to reach our conclusion
that the claimed composition would have been obvious.
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Application 14/150,493
SUMMARY
For these reasons and those set forth in the Examiner’s Answer, and
the Final Office Action, we affirm each of the Examiner’s rejection of
claims 1—16 and 19 under 35 U.S.C. § 103(a) as obvious over the
combination of Sako and Peck.
TIME PERIOD FOR RESPONSE
No time period for taking any subsequent action in connection with
this appeal may be extended under 37 C.F.R. § 1.136(a)(1). See 37 C.F.R.
§§ 41.50(f), 41.52(b).
AFFIRMED
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