GRÜNENTHAL GMBH

Patent Trials and Appeals Board

Oct 21, 2020

2020001093 (P.T.A.B. Oct. 21, 2020)

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.
13/645,595 10/05/2012 Anja GEIßLER 107101-113 KGB 8691
27384 7590 10/21/2020
Briscoe, Kurt G.
Norris McLaughlin, PA
7 Times Square, 21st Floor
New York, NY 10036-6524
EXAMINER
YU, HONG
ART UNIT PAPER NUMBER
1612
NOTIFICATION DATE DELIVERY MODE
10/21/2020 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):
jarcher@norris-law.com
nmanfredi@norris-law.com
PTOL-90A (Rev. 04/07)
UNITED STATES PATENT AND TRADEMARK OFFICE
____________

BEFORE THE PATENT TRIAL AND APPEAL BOARD
____________

Ex parte ANJA GEIßLER and LUTZ BARNSCHEID
____________

Appeal 2020-001093
Application 13/645,595
Technology Center 1600
____________

Before ULRIKE W. JENKS, AMEE A. SHAH, and
RACHEL H. TOWNSEND, Administrative Patent Judges.

SHAH, Administrative Patent Judge.

DECISION ON APPEAL
STATEMENT OF THE CASE
Pursuant to 35 U.S.C. § 134(a), the Appellant1 appeals from the
Examiner’s final decision to reject claims 2, 6–11, 14, 15, 17–19, 21, 22, 24,
and 25, which are all of the pending claims. We have jurisdiction under
35 U.S.C. § 6(b).
We AFFIRM IN PART.

1 We use the word “Appellant” to refer to “applicant” as defined in
37 C.F.R. § 1.42. The Appellant identifies the real party in interest as the
Grünenthal GmbH. Appeal Br. 1.
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CLAIMED SUBJECT MATTER
According to the Specification,
[t]he invention relates to a pharmaceutical dosage form for oral
administration having a breaking strength of at least 300 N and
comprising an opioid agonist, an opioid antagonist, and a
polyalkylene oxide having an average molecular weight of at
least 200,000 g/mol, wherein in accordance with Ph. Eur. the in
vitro release profile of the opioid agonist essentially corresponds
to the in vitro release profile of the opioid antagonist, and
wherein the opioid agonist and the opioid antagonist are
intimately mixed with one another and homogeneously dispersed
in the polyalkylene oxide.
Spec 1.
Claims 24 and 25 are the independent claims. Claim 24 is illustrative
of the subject matter on appeal and is reproduced below (with added
paragraphing):
24. A pharmaceutical dosage form for oral administration
having
a breaking strength of at least 300 N and
comprising a homogeneous mixture of (i) oxycodone or a
physiologically acceptable salt thereof; (ii) an opioid antagonist
selected from the group consisting of naloxone and
pharmaceutically acceptable salts thereof; and (iii) a
polyalkylene oxide having a weight average molecular weight of
at least 500,000 g/mol;
wherein in accordance with Ph. Eur. the in vitro release
profile of the opioid agonist from the pharmaceutical
dosage form essentially corresponds to the in vitro release
profile of the opioid antagonist from the pharmaceutical
dosage form; and
wherein said in vitro release profile is not osmotically
driven.

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REFERENCES
The prior art relied upon is:
Name Reference Date
Breder et al. (“Breder”) US 2003/0069263 A1 Apr. 10, 2003
Arkenau-Maric et al.
(“Arkenau-Maric”)
US 2007 /0183979 A1 Aug. 9, 2007
Everaert et al.
(“Everaert”)
US 2008/0317695 A1 Dec. 25, 2008
Brögmann et al.
(“Brögmann”)
EP 1 492 506 B1 Dec. 31, 2008
Arkenau-Maric et al.
(“Arkenau-Maric ‘872”)
US 8,075,872 B2 Dec. 13, 2011
Merriam-Webster Dictionary, http://www.merriam-webster.com/
dictionary/monolithic (“Monolithic”)

REJECTIONS2
Claims 2, 7–11, 17, 18, 21, 22, 24, and 25 stand rejected on the
ground of non-statutory obviousness-type double patenting as being
unpatentable over claims 1, 2, 4, 6, and 13 of Arkenau-Maric ‘872.
Claims 2, 6–11, 14, 15, 17–19, 21, 22, 24, and 25 stand rejected under
35 U.S.C. § 103(a) as being unpatentable over Arkenau-Maric, Monolithic,
Everaert, and Breder.

2 The Examiner withdraws the rejection of claims 2, 6–11, 14, 15, 17, 18,
21, 22, 24, and 25 under 35 U.S.C. § 102(b) as anticipated by Arkenau-
Maric. Ans. 3. We also consider withdrawn the Examiner’s rejection of
claim 19 as obvious over Arkenau-Maric and Everaert that is based on the
§ 102(b) rejection of claim 18 (see Final Act. 10).
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OPINION
Double-Patenting
The Examiner rejects claims 2, 7–11, 17, 18, 21, 22, 24, and 25 under
the doctrine of non-statutory obvious-type double patenting under 35 U.S.C.
§ 101 over claims 1, 2, 4, 6, and 13 of Arkenau-Maric ‘872.3 Specifically,
the Examiner notes that both the instant appealed claims and those of
Arkenau-Maric ‘872 recite a pharmaceutical dosage comprising an opioid,
naloxone, and polyalkylene oxide. See Final Act. 4. The Examiner notes
that the patented claims “do not claim osmotically driven in vitro release
profile,” but finds that “[a]lthough the patent and instant claims are not
identical, they are not patentably distinct from each other because claims in
both applications are drawn to the same abuse-proofed dosage forms having
a breaking strength of at least 500 N.”4 Id. (underlining omitted).
The Appellant argues that the patented claims are a genus of the
appealed claims, “do not specify a homogeneous mixture, or that the
homogeneous mixture comprises oxycodone, naloxone, and polyalkylene
oxide, or that the dosage form is non-osmotically driven,” and “do[] not
render obvious the instantly claimed dosage form, or the surprising and
unexpected properties exhibited thereby.” Appeal Br. 18. The Appellant
further argues “[w]hile the present claims might technically be a species
within the broader generic claims of the ‘872 patent, Appellant’s species is

3 We note that although the Examiner does not include instant appealed
claim 6 in this rejection, it is not clear how the administration as recited in
claim 6 changes the structure of dosage form.
4 We note that although the Examiner does not include instant appealed
claim 19 in this rejection, it is not clear how patented claim 1’s recital of at
least 500 N does not include appealed claim 19’s recital of at least 1000 N.
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novel and nonobvious with respect to the genus and, thus, separately
patentable in the wake of the unpredictability known in the prior art at the
time of the present invention.” Id. at 19.
If the claimed invention is “merely an obvious variation of an
invention disclosed and claimed in the [reference] patent,” the instant claims
would be invalid for obviousness-type double patenting. See Abbvie Inc. v.
Mathilda & Terence Kennedy Inst. of Rheumatology Tr., 764 F.3d 1366,
1379 (Fed. Cir. 2014) (quoting In re Vogel, 422 F.2d 438, 441 (CCPA
1970). Although “[i]t is well-settled that a narrow species can be non-
obvious and patent eligible despite a patent on its genus[,] . . . not every
species of a patented genus is separately patentable.” Id. (citations omitted).
We first note that we construe appealed claim 24’s recitation of at
least 300 N to be anything above 300 N, including patented claim 1’s and
appealed claimed 25’s recitations of 500 N and appealed claim 19’s
recitation of 1000 N. And we note that the Appellant is correct in the ways
that the patented claims differ from the appealed claims, including not
reciting that the dosage from is non-osmotically driven. Appeal Br. 18. To
the extent the Appellant might be suggesting that the patented claims are not
non-osmotically driven because Arkenau-Maric ‘872 “mentions osmotic
dosage forms” in the Specification (Appeal Br. 18 n. 5, citing col. 13,
ll. 61–62), we disagree because the patented claims are silent as to an
osmotic or non-osmotic delivery system, and we do not read limitations into
the claims from the Specification. See e.g., Bayer AG v. Biovail Corp., 279
F.3d 1340, 1348 (Fed. Cir. 2002)
The Appellant has not shown, and it is not clear, that the claimed
dosage form has unexpected properties. The patented claims include a
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breaking strength within that required by the appealed from claims and
require that the matrix material include a polyalkylene oxide that is within
the molecular weight limitation required by the appealed from claims.
Furthermore, the patented claims recite that they have a controlled release as
a natural result of the matrix material that is the polyalkylene oxide (see
Arkenau-Maric ‘872, claim 1), and the Appellant does not contend that
controlled release cannot be non-osmotically driven. The Appellant has not
established on the record that the elements of patented claim 13 would not
have the same non-osmotic release when it has all of the other elements
required by the appealed claims.
Therefore, we sustain the Examiner’s rejection of claims 2, 7–11, 17,
18, 21, 22, 24, and 25 under the judicial doctrine of non-statutory obvious-
type double patenting over claims 1, 2, 4, 6, and 13 of Arkenau-Maric ‘872.

Obviousness
The Appellant contends that the combination of Arkenau-Maric and
Breder does not render obvious the claimed dosage form comprising
oxycodone, opioid antagonist of naloxone, and polyalkylene oxide wherein
the in vitro release profile of the opioid agonist essentially corresponds to
the in vitro release profile of the opioid antagonist and the in vitro release –
profile is not osmotically driven, as recited in independent claims 24 and 25.
See Appeal Br. 7–13.
The Examiner finds that “Arkenau-Maric et al. do not disclose
osmotically driven in vitro release profile,” but finds that “the composition
disclosed by Arkenau-Maric et al. would necessarily (inherently) have the
claimed in vitro release profile of the opioid agonist and the opioid
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antagonist.” Final Act. 6 (underlining omitted). The Examiner further finds
that “the disclosure of Arkenau-Maric et al. is not explicit enough to support
an anticipation determination with regard to the spatial relationship between
the opioid agonist and the opioid antagonist” (Final Act. 12 (underlining
omitted); see also Ans. 3 (withdrawing the anticipation rejection)) and relies
on Breder to cure this deficiency (see Final Act. 12). In particular, the
Examiner finds “Breder specifically discloses (paragraph 0025)
embodiments in which the dissolution rate of naloxone is a[s] low as plus or
minus 5 percent relative to the dissolution rate of oxycodone, which would
be within the scope of Appellants’ preferred values.” Ans. 6. The Examiner
finds
Breder et al. teach dosage forms with reduced abuse
potential in sustained release form comprising oxycodone (the
claimed and elected opioid agonist) and naloxone (the claimed
but not elected opioid antagonist) either together or separated and
excipients such as PAO with MW of 1,500 to 12,000; wherein
the composition provides a dissolution rate of naloxone within
±20% relative to the dissolution rate of oxycodone at 1 hour, 4
hours and 12 hours when tested in-vitro by the USP Apparatus I
(Basket) method of U.S. Pharmacopela XXIV (2000) at 100 rpm
in 900 ml simulated gastric fluid (SGF) at 37oC.
Final Act. 12 (citing Breder ¶¶ 41, 45, 66, 132, 134, 140). The Examiner
determines that it would have been obvious to one skilled in the art to
combine the teachings of Arkenau-Maric and Breder as it “was well known
to a person of ordinary skill in the art at the time of the invention” to do so,
the “motivation”
flow[ing] from both having the opioid agonist and the opioid
antagonist together and spatially separated having been used in
the prior art, and from their being recognized in the prior art as
useful and effective for the same purpose. Absent some
demonstration of unexpected result it would have been obvious
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to one of ordinary skill in the art to having the opioid agonist and
the opioid antagonist with predictable results to one of ordinary
skill in the art at the time of the invention.
Id. at 13.
Arkenau-Maric discloses a dosage form “suitable for preventing abuse
of an opioid active ingredient” including oxycodone. Arkenau-Maric ¶ 17.
To achieve the necessary breaking strength of the dosage form, at least one
polymer is used, the polymer selected from a group including polyalkylene
oxide. Id. ¶ 20. The dosage form can also contain an auxiliary substance
known to be used in the formulation of solid dosage forms. Id. ¶ 24. The
auxiliary substance can comprise an antagonist suitable for preventing
opioid abuse, such as naloxone or pharmaceutically acceptable salts. Id.
¶¶ 26, 30, 34, 57, 59. The antagonist is “preferably spatially separated from
the remaining constituents of the invention dosage according to the form
and, when correctly used, do not exert any effect.” Id. ¶ 57.
Breder discloses “a pharmaceutical composition comprising from 10
to 40 mg of oxycodone or a pharmaceutically acceptable salt thereof
[“oxycodone”] and 0.65 to 0.90 mg naloxone or a pharmaceutically
acceptable salt thereof [“naloxone”].” Breder, Abstract. In some
embodiments, the naloxone has an in-vitro dissolution rate within ±20%, or
alternately 10%, or 5%, relative to the dissolution rate of oxycodone. Id.
¶ 25. In other embodiments with sustained release of the oxycodone and
naloxone, the in vitro dissolution rate is about equal when measured by
weight release per hour, i.e., from about 20–60%, 30–75%, 40–90%, >60%,
or >70% (by weight) of oxycodone and naloxone per 1 hour, 2 hours, more
than 4 hours, 8 hours, or 12 hours, respectively. Id. ¶ 26; see also id.
¶¶ 41, 46. In sustained release osmotic dosage form embodiments, the
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delivery or push layer comprises an osmopolymer including polyalkylene
oxide as well as one or more osmotically effective compounds. Id. ¶¶ 132,
134–136. Breder provides release data for examples of “[s]ustained release
10 mg oxycodone hydrochloride formulations containing naloxone
hydrochloride” without polyalkylene oxide. Id. ¶¶ 201–224 (Examples 5–7),
Tables 7, 7A, 8, 8A, 9, 9A. Breder also provides data for examples of
osmotic dosage systems comprising oxycodone, naloxone, polyethylene
oxide, and hydroxypropylmethylcellulose (“HPMC”). Id. ¶¶ 171–178
(Example 2).
Claims 24 and 25 require that “the in vitro release profile of the opioid
agonist from the pharmaceutical dosage form essentially corresponds to the
in vitro release profile of the opioid antagonist from the pharmaceutical
dosage form” and that this “in vitro release profile is not osmotically
driven.” The Specification defines the term “essentially corresponds” as
preferably mean[ing] that opioid agonist and opioid antagonist
are released according to same order kinetics, preferably both
according to a prolonged release profile; preferably, however,
“essentially corresponds” does not encompass pharmaceutical
dosage forms where one of the opioid agonist and the opioid
antagonist is released immediately, and the other one is released
in a prolonged fashion.
Spec. 8.
We find supported the Examiner’s finding that Breder teaches that the
in vitro release profile of the opioid agonist essentially corresponds to the in
vitro release profile for the opioid antagonist. However, we agree with the
Appellant that Breder teaches that formulations containing the opioid
agonist, opioid antagonist, and polyalkylene oxide with essentially
corresponding in vitro profiles of the agonist and antagonist where that
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release rate profile is osmotically driven, i.e., from an osmotic dosage form
that includes a displacement layer of polyethylene in addition to containing a
drug layer of agonist, antagonist and polyethylene oxide. See Appeal
Br. 10–12; Reply Br. 7–8; Breder ¶¶ 134–135, 171 (Example 2). The
Examiner does not provide reasoning or evidence that one of ordinary skill
in the art would reasonably expect the same release profile when the osmotic
delivery mechanism provided by a composition containing polyalkylene
displacement layer is absent. Rather, the Examiner simply concludes that
doing so would yield predictable results absent evidence to the contrary. See
Final Act. 12–13.
“A showing of unexpected results can support a conclusion of non-
obviousness. See United States v. Adams, 383 U.S. 39 . . . (1966).” Forest
Labs., LLC v. Sigmapharm Labs., LLC, 918 F.3d 928, 937 (Fed. Cir. 2019).
It is well settled that the Appellant has the burden of showing unexpected
results. In re Freeman, 474 F .2d 1318, 1324 (CCP A 1973); In re Klosak,
455 F.2d 1077, 1080 (CCPA 1972). The burden requires the Appellant to
proffer factual evidence that actually shows unexpected results relative to
the closest prior art (see In re Baxter Travenol Labs., 952 F.2d 388, 392
(Fed. Cir. 1991)), and that is reasonably commensurate in scope with the
protection sought by the claims on appeal (In re Grasselli, 713 F.2d 731,
743 (Fed. Cir. 1983)).
Here, the Appellant argues that the claimed dissolution profiles are
unexpected as evidenced by the Brögmann reference where “it was found
that the release rates of the tilidine and naloxone from a mixture of the two
in hydroxypropylmethylcellulose differed significantly and, thus, did not
‘essentially correspond’ to one another, as required by the present claims.”
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Appeal Br. 6 (emphasis omitted); see also id. at 14–15. Specifically, the
Appellant directs attention to paragraph 26 of Brögmann that describes the
prior art as “a tilidine/naloxone-combination” that “is a formulation from
which both active compounds are released in a sustained manner” and where
“[t]he matrix used comprises a relevant part of water-swellable material
(hydroxypropylmethylcellulose (HPMC)) and has therefore to be considered
as a swellable (and possibly partially erosive) diffusion matrix.” Appeal
Br. 6 n. 2. “Accordingly, Appellant had serious doubts whether, and indeed
expressed ‘surprise’ in the paragraph bridging pages 3-4 of the application,
that the combination of properties here sought and claimed could be
simultaneously achieved.” Id. at 6.
The Examiner does not dispute these assertions but contends that
Brögmann “is not the closest prior art of record - Arkenau-Maric is.”
Ans. 7. However, the Examiner does not fully explain why Arkenau-Maric
is the closest prior art of record, particularly when the Examiner
acknowledges that Arkenau-Maric does not teach that the claimed release
profile is not osmotically driven. See Final Act. 12; Ans. 3 (acknowledging
that Arkenau-Maric does not explicitly teach the limitation); see also Ans. 6
(acknowledging it is the combination of Arkenau-Maric and Breder that
teaches the limitation). We find persuasive the Appellant’s argument that
Brögmann is the closest prior art as “Arkenau-Maric does not discuss any
desired release profile relationship between opioid and naloxone,” its “sole
working example does not even contain an antagonist” such as naloxone,
and Brögmann’s “tilidine/naloxone/HPMC construct is most certainly closer
to the instant claims than is Arkenau-Maric since [Brögmann] has an
opioid/naloxone/matrix polymer combination arguably similar to
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Appellant’s oxycodone/naloxone/polyalkylene oxide whereas Arkenau-
Maric does not.” Reply Br. 6.
Thus, the Appellant provides sufficient argument and reasoning of
“the surprising and unexpected nature of Applicant’s showing that
combining a homogeneous mixture of oxycodone, naloxone, and
polyalkylene oxide in a non-osmotically-driven dosage form, as instantly
claimed, is capable of providing similar release rates of oxycodone and
naloxone, as claimed, with all the benefits attendant thereto” (Appeal Br. 14)
that is reasonably commensurate in scope with the protection sought by the
claims on appeal to rebut the Examiner’s prima facie finding of obviousness.
The Examiner errs in not considering the Appellant’s evidence of
unexpected results.
The Examiner fails to rely on the teachings of Monolithic or Everaert
in any manner that would remedy the deficiencies in the Examiner’s
rejection as discussed above. Therefore, we do not sustain the Examiner’s
rejection of independent claims 24 and 25 and of dependent claims 2, 6–11,
14, 15, 17–19, 21, and 22 under 35 U.S.C. § 103(a) as obvious over
Arkenau-Maric, Monolithic, Everaert, and Breder.
CONCLUSIONS
The Examiner’s decision to reject claims 2, 7–11, 17, 18, 21, 22, 24,
and 25 under the judicial doctrine of non-statutory obvious-type double
patenting is sustained.
The Examiner’s decision to reject claims 2, 6–11, 14, 15, 17–19, 21,
22, 24, and 25 under 35 U.S.C. § 103(a) is not sustained.
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In summary:
Claims
Rejected
35 U.S.C. § Reference(s)/
Basis 
Affirmed Reversed
2, 7–11, 17,
18, 21, 22,
24, 25
Double
patenting
Arkenau-Maric
‘872
2, 7–11,
17, 18, 21,
22, 24, 25

2, 6–11, 14,
15, 17–19,
21, 22, 24, 25
103(a) Arkenau-Maric,
Monolithic,
Everaert, Breder
2, 6–11, 14,
15, 17–19,
21, 22, 24, 25
Overall
Outcome
2, 7–11,
17, 18, 21,
22, 24, 25
6, 14, 15, 19

No time period for taking any subsequent action in connection with
this appeal may be extended under 37 C.F.R. § 1.136(a). See 37 C.F.R.
§ 1.136(a)(1)(iv).

AFFIRMED IN PART