Rahul Sareen et al.

Patent Trials and Appeals Board

Sep 20, 2019

15640823 - (D) (P.T.A.B. Sep. 20, 2019)

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.
15/640,823 07/03/2017 Rahul Sareen 2134-1068 A 7071
96056 7590 09/20/2019
Florek & Endres PLLC
1156 Avenue of the Americas
Suite 600
New York, NY 10036
EXAMINER
GHALI, ISIS A D
ART UNIT PAPER NUMBER
1611
MAIL DATE DELIVERY MODE
09/20/2019 PAPER
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.
PTOL-90A (Rev. 04/07)

UNITED STATES PATENT AND TRADEMARK OFFICE
_________________

BEFORE THE PATENT TRIAL AND APPEAL BOARD
_________________

Ex parte RAHUL SAREEN, SHAHIN FESHARAKI, and PARAG SHAH

_________________

Appeal 2019-003436
Application 15/640,823
Technology Center 1600
_________________

Before ERIC B. GRIMES, RAE LYNN P. GUEST, and DEBORAH KATZ,
Administrative Patent Judges.

KATZ, Administrative Patent Judge.

DECISION ON APPEAL

Appellant1 seeks our review, under 35 U.S.C. § 134(a), of the
Examiner’s decision to reject claims 24–39. (Appeal Brief filed November
8, 2018 (“Appeal Br.”) 1.) We have jurisdiction under 35 U.S.C. § 6(b).
We AFFIRM.

1 We use the word “Appellant” as defined in 37 C.F.R. § 1.42. Appellant
identifies the real party-in-interest as Allergan Sales, LLC. (Appeal Brief
filed November 8, 2018, 3.)
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Appellant’s specification is drawn to tablets that allow for immediate
release of a drug at risk of being abused. (Specification (“Spec.”) 1:4–5.)
Appellant’s Specification explains that the claimed compositions deter abuse
by including a gelling agent to make extraction of the drug difficult and by
including an effervescent agent to deter inhalation as a nasal irritant. (See
Spec. 2:18–20.)
Appellant’s claimed tablets consist essentially of a compressed core,
which consists essentially of a drug, a gelling agent, an effervescent agent,
and optionally other ingredients, wherein the tablet is formulated for
immediate release of the drug. Appellant’s claim 24 recites:
A solid pharmaceutical tablet consisting essentially of:
i) a compressed core; and
ii) optionally an aesthetic or seal coating surrounding the
compressed core,
wherein the compressed core is a mixture consisting essentially
of:
a) a therapeutically effective amount of a drug that is subject to
abuse, wherein the drug is selected from the group consisting of
alfentanil, alimemazine, alprazolam, amphetamine, buprenorphine,
butorphanol, clonazepam, codeine, cyclobenzaprine, diazepam,
dihydrocodeine, dihydromorphine, dronabinol, estazolam, ezopiclone,
fentanyl, flurazepam, hydrocodone, hydromorphone, lorazepam,
methobarbital, methylphenidate, methadone, morphine, oxycodone,
oxymorphone, phenobarbital, secobarbital, tempazepam, tramadol,
triazolam, zaleplon, zopiclone, zolpidem and pharmaceutically
acceptable salts thereof;
b) about 1 to about 20 weight percent of a gelling agent selected
from the group consisting of polyhydroalkylcellulose having a
molecular weight greater than 50,000, a
poly(hydroxyalkylmethacrylate) having a molecular weight of from
5,000 to 5,000,000; a poly(vinylpyrrolidone) having a molecular
weight of from 100,000 to 3,000,000; a polysaccharide, a
carboxyvinyl polymer, a polymer of acrylic acid crosslinked with a
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polyallyl ether of sucrose; polyacrylamides; polyethylene oxide
polymers having a molecular weight of 100,000 to 7,000,000 and
combinations thereof;
c) about 1 to about 20 weight percent of an effervescent agent;
d) optionally at least one conventional pharmaceutical
processing excipient; and
e) optionally a second aversive agent selected from the group
consisting of a second nasal irritant, an antagonist agent, a bittering
agent, a visual modifying agent, an emetic agent and combinations of
the forgoing,
wherein the tablet releases 40 - 90% of the drug in 30 minutes
and 70 - 100% of the drug in 45 minutes when measured using a USP
Apparatus Type 2 dissolution test at 50 rpms and 500 ml of purified
water at 37°C.
(Appeal Br. 17–18.)
Claim 36 is similar but recites fewer drugs and is limited to specific
effervescent agents and polyethylene oxide polymer having a molecular
weight of 100,000 to 7,000,000 as the only gelling agent. Claim 36 recites:
A solid pharmaceutical tablet consisting essentially of:
i) a compressed core; and
ii) optionally an aesthetic or seal coating surrounding the
compressed core,
wherein the compressed core is a mixture consisting essentially
of:
a) a therapeutically effective amount of a drug selected from the
group consisting of buprenorphine, codeine, dihydrocodeine,
dihydromorphine, hydrocodone, hydromorphone, morphine,
oxycodone, oxymorphone and pharmaceutically acceptable salts
thereof;
b) about 1 to about 20 weight percent of a polyethylene oxide
polymer having a molecular weight of 100,000 to 7,000,000;
c) about 1 to about 20 weight percent of an effervescent agent
wherein the effervescent agent consists essentially of an alkaline
source selected from the group consisting of a carbonate, bicarbonate
and a mixture thereof and an acid source selected from the group
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consisting of an organic acid, a salt of an organic acid and a mixture
thereof;
d) at least one conventional pharmaceutical processing
excipient selected from the group consisting of fillers, binders,
lubricants, glidants, disintegrants, coloring agents, and mixtures
thereof;
e) optionally a second aversive agent selected from the group
consisting of a second irritating agent, an antagonist agent, a bittering
agent, a visual modifying agent, an emetic agent and combinations of
the forgoing;
and wherein the tablet releases 40 - 90% of the drug in 30
minutes and 70 - 100% of the drug in 45 minutes when measured
using a USP Apparatus Type 2 dissolution test at 50 rpms and 500 ml
of purified water at 37°C.
(Id. at 20–21.)
The Examiner rejected all of Appellant’s claims as being obvious
under 35 U.S.C. § 103(a) over Tygesen2 and McKenna.3 (See Final Office
Action mailed June 13, 2018 (“Final Act.”) 3–11.)
Findings of Fact
1. Tygesen teaches pharmaceutical compositions for oral
administration that are resistant to abuse, particularly when abused by being
released faster, and therefore being absorbed faster, in the presence of
alcohol. (See Tygesen ¶¶ 3 and 4.)
2. Tygesen teaches immediate release compositions that have a
decreased release rate in the presence of ethanol. (See Tygesen ¶ 30.)

2 Tygesen et al., U.S. Patent Application Publication 2010/0204259 A1,
published August 12, 2010.
3 McKenna et al., U.S. Patent Application Publication 2009/0081290 A1,
published March 26, 2009.
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3. Tygesen teaches matrix compositions that comprise one or
more low molecular weight polyglycols combined with one or more
effervescent agents. (See Tygesen ¶¶ 3, 32, and 54.)
4. Tygesen teaches that polyethylene glycol (“PEG”)/polyethylene
oxide (“PEO”)4 having molecular weight of from about 900 to about 17,000
Daltons should be selected to formulate an immediate release composition of
the drug substance, but with a decreased release rate when in the presence of
alcohol. (See Tygesen ¶ 36 and 61–66.)
5. Tygesen teaches that “mixtures of PEO and/or mixtures of PEG
materials with different average molecular weights can be used in order to
obtain a desired average molecular weight for the polyglycol material
utilized in immediate release compositions described herein.” (See Tygesen
¶ 66.)
6. Tygesen teaches that in addition to polyglycol-type polymers,
other polymers are suitable for the immediate release formulations including
PVP, polyacrylamide, and Eudragit compounds. (See Tygesen ¶ 68.)
7. Tygesen teaches that the compositions can include many of the
drugs recited in Appellant’s claims, for example amphetamine, codeine,
fentanyl, methadone, morphine, and oxycodone. (See Tygesen ¶¶ 45, 103,
121, 122, 126, 127, and 141.)

4 Tygesen explains that PEG refers to polymers chains with molecular
weights below 20,000, while PEO refers to higher molecular weights
polymers. (See Tygesen ¶ 63.)
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8. Tygesen teaches that the effervescent agent used in the
immediate release composition can be an acid and a base that react together
to release carbon dioxide gas. (See Tygesen ¶ 74.)
9. Tygesen teaches that the immediate release compositions can
include plasticizers, such as polyethylene glycols or polyethylene oxides
with a molecular weight of 1,000 – 500,000 Daltons. (See Tygesen ¶ 85.)
10. Tygesen teaches that the immediate release compositions may
include pharmaceutically acceptable excipients, including fillers, binders,
lubricants, glidants, disintegrants, and coloring agents. (See Tygesen ¶¶ 82–
84.)
11. McKenna teaches pharmaceutical compositions that are tamper
resistant because their release profiles do not change in alcohol and because
they are resistant to crushing. (See McKenna ¶¶ 5, 7, and 8.)
12. McKenna teaches extended release (in contrast to immediate
release) compositions comprising at least one PEO with a molecular weight
of at least 1,000,000 Daltons and at least one polyethylene oxide having a
molecular weight of less than 1,000,000. (See McKenna ¶¶ 15, 17–19, and
72–75.)
13. McKenna teaches:
In embodiments wherein the composition further comprises at least
one low molecular weight polyethylene oxide is used[,] polyethylene
oxides having, based on rheological measurements, an approximate
molecular weight of less than 1,000,000, such as polyethylene oxides
having, based on rheological measurements, an approximate
molecular weight of from 100,000 to 900,000 may be used. The
addition of such low molecular weight polyethylene oxides may be
used to specifically tailor the release rate such as [to] enhance the
release rate of a formulation that otherwise provides a release rate
[too] slow for the specific purpose. In such embodiments at least one
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polyethylene oxide having, based on rheological measurements, an
approximate molecular weight of 100,000 may be used.
(McKenna ¶ 238.)
Analysis
Claim 24
Appellant’s claim 24 recites a tablet consisting essentially of a
compressed core, which consists essentially of a drug selected from a list of
possible drugs, a gelling agent selected from a list of possible gelling agents,
and an effervescent agent, wherein the drug is released from the tablet at a
rate within the recited limits. We agree with the Examiner that the tablet of
claim 24 is obvious because Tygesen teaches a tablet with a compressed
core of at least one of the drugs recited in claim 24 (e.g., codeine, morphine,
hydrocodone, oxycodone, or oxymorphone), a gelling agent recited in claim
24 (e.g., polyvinylpyrrolidone (PVP) or polyacrylamide), and an
effervescent agent. (See Final Act. 5, see Ans. 3–4; see FFs 3 and 6–8.)
Although Appellant argues that the Examiner erred in rejecting claim
24 because of the teachings in the prior art regarding polyethylene oxides,
Appellant does not contest the Examiner’s findings and does not argue that
the teachings in Tygesen of other gelling agents fails to render a composition
with the scope of claim 24 obvious.
Accordingly, Appellant fails to persuade us that the Examiner erred in
rejecting claim 24 and we affirm the rejection. Appellant represents that
claims 25–27, 30, 32–53, and 38 stand or fall with claim 24. (See Appeal
Br. 9.) We affirm the rejection of each of these claims as being obvious over
Tygesen and McKenna, as well.
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Claim 36
Like claim 24, Appellant’s claim 36 recites a tablet consisting
essentially of a compressed core, which consists essentially of a drug
selected from a list of possible drugs, an effervescent agent, an excipient,
and a PEO having a molecular weight of 100,000 to 7,000,000. (See Appeal
Br. 21.) In contrast to claim 24, claim 36 is limited to this PEO.
The Examiner bases the rejection of claim 36 on the teachings in
McKenna that abuse-resistant tablets can include PEO of molecular weights
with the range recited in claim 36. (See Final Act. 7–8; see FFs 11–12.) The
Examiner also relies on the teaching in McKenna that one could specifically
tailor the release rate by increasing it with the addition of lower molecular
weight PEOs, when the release rate had been slowed for another, specific
purpose. (See Final Act. 8, citing McKenna ¶ 2385; see FF 13.) Similarly,
the Examiner relies on the teaching in Tygesen that mixtures of PEO and/or
PEG materials with different average molecular weights can be used in order
to obtain a desired average molecular weight for the polyglycol material
utilized in immediate release compositions. (See Final Act. 6, citing
Tygesen ¶ 66.)

5 The Examiner cites to paragraphs 237 and 240 of McKenna for the
statement that “[t]he low MW [molecular weight] PEO used to specifically
tailor the release rate such as enhance the release rate of a formulation that
otherwise provides a release rate to slow for the specific purpose.” (Final
Act. 8.) Because this language is almost identical to the language of
McKenna paragraph 238, and the Examiner cites to paragraph 238 for
similar language in the Answer (see Ans. 4), we assume that the citation to
paragraph 237 was intended to be to paragraph 238. (See also Reply Brief
filed March 25, 2019, 4.)
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The Examiner reasons that it would have been obvious to one having
ordinary skill in the art at the time of the invention to provide a tablet as
recited in claim 36 because Tygesen teaches including PEO polymers,
opioids, and effervescent agents in compositions for tablets and because
McKenna teaches a mixture of PEO of high and low molecular weight,
including PEOs with the range claimed, can be used to specifically tailor the
drug release rate from a tablet composition. (See Final Act. 8.) The
Examiner finds from the cited references that it would have been reasonable
to expect formulating an immediate release oral dosage in light of these
teachings. (See id.)
In addition, the Examiner finds that Tygesen teaches immediate
release compositions may further include plasticizers, including PEO having
a molecular weight between 1,000 and 500,000 Daltons. (See Final Act. 6,
citing Tygesen ¶ 85; see FF 9; see Ans. 6.)
We are persuaded by the Examiner’s reasoning because “the analysis
[of obviousness] need not seek out precise teachings directed to the specific
subject matter of the challenged claim, for a court can take account of the
inferences and creative steps that a person of ordinary skill in the art would
employ.” KSR Int'l Co. v. Teleflex Inc., 550 U.S. 398, 418 (2007).
In general, Appellant argues that the teachings of Tygesen and
McKenna would not render the compositions recited in claim 36 obvious
because Tygesen and McKenna demonstrate that PEOs with the high
molecular weight would delay and extend the immediate release profile of
the composition of Tygesen. (See Appeal Br. 8.) Appellant argues that
Tygesen teaches that to obtain the desired immediate release properties for
the tablet, PEGs/PEOs with a molecular weight from 900–17,000 should be
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used. (See Appeal Br. 8.) Specifically, Appellant cites to a portion of
Tygesen teaching that PEO of high MW (20,000 Daltons and above) allows
for “controlled” release of drug, which is contrasted with immediate release.
(See Appeal Br. 11, citing Tygesen ¶¶ 34–35, also citing Tygesen ¶¶ 64 and
66.)
Appellant argues further that Examples 22 and 24 of Tygesen show
that increasing the molecular weight of the PEG/PEO slows the release
profile of drug from a matrix. (See Appeal Br. 12–13; see Reply Brief filed
March 25, 2018 (“Reply Br.”) 5–6.) Appellants assert that in Example 22 a
composition with PEG of molecular weight 17,000 Daltons released a drug
more slowly than the same composition using PEG of 6000 Daltons. (See
id., citing Tygesen Figs. 21 and 23.) Appellant asserts that the Examiner
erred because “merely replacing the lower molecular weight PEO of
Tygesen with the higher molecular weight of McKenna would not result in a
similar profile.” (Appeal Br. 13.)
We are not persuaded by Appellant’s argument because the
Examiner’s rejection6 is not based on a simple substitution of the higher
molecular weight PEG/PEOs of McKenna for the lower molecular weight
PEG/PEOs of Tygesen. (See Ans. 9.) Instead, the Examiner’s rejection is
based on the knowledge in the art that the molecular weights of PEG/PEOs
can be tailored to achieve a desired release rate. (See Final Act. 8.) In other
words, the molecular weight of PEG/PEO is a result effective variable that

6 The Examiner relied on this reasoning in regard to claim 24 as well as
claim 36. (See Final Act. 4–10.) We affirm the rejection of claim 24 as
discussed above, but also on the basis of this reasoning.
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can be adjusted based on a desired immediate release rate. Indeed, Tygesen
teaches that “mixtures of PEO and/or mixtures of PEG materials with
different average molecular weights can be used in order to obtain a desired
average molecular weight for the polyglycol material utilized in immediate
release compositions described herein.” (Tygesen ¶ 66; FF5; see Ans. 4.) In
addition, Tygesen teaches that, even though PEG/PEO contribute to the
release rate, they are not the only determinants. The Examiner cites Tygesen
for teaching that the release rate of a composition is also determined by the
polymer, disintegrant, and effervescent agent present. (See Ans. 9–10, citing
Tygesen ¶ 72.)
Appellant focuses only on the difference between the PEG/PEOs
used, without acknowledging that one of ordinary skill in the art would be
able to tailor release rate by choosing a PEG/PEO that would give the
desired characteristics, in light of the other ingredients present, such as
effervescent agent, disintegrant, etc. (See Reply Br. 6.) Because
Appellant’s arguments do not address the basis for the Examiner’s rejection,
that it was known in the art that release rate can be tailored by choice of
PEG/PEO, we are not persuaded that the Examiner erred.
Accordingly, Appellant’s argument that the Examiner’s reasoning of
merely replacing the lower molecular weight PEO of Tygesen with the
higher molecular weight of McKenna to achieve the claimed release profile
does not address the Examiner’s actual rejection. (See Appeal Br. 13.)
In regard to the teaching in Tygesen of including PEO within the
claimed molecular weight range as a plasticizer in the immediate release
composition, Appellant argues that PEO with a molecular weight of 1,000 to
500,000, within the claimed range, was provided in paragraph 85 only as
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“boilerplate laundry lists of over 100 plasticizers” and that Tygesen fails to
provide any “blaze marks” or suggestions leading one of ordinary skill to
select such ingredients. (Appeal Br. 14.) We are not persuaded by this
argument because the rejection is based on obviousness, not anticipation.
See in re Arkley, 455 F.2d 586 (CCPA 1972) (“Such picking and choosing
may be entirely proper in the making of a 103, obviousness rejection, where
the applicant must be afforded an opportunity to rebut with objective
evidence any inference of obviousness which may arise from the similarity
of the subject matter which he claims to the prior art . . . .”); see also In re
Malagari, 499 F.2d 1297, 1303 (CCPA 1974) (claimed invention is rendered
prima facie obvious by the teachings of a prior art reference that discloses a
range that touches the range recited in the claim). In other words, Tygesen
teaches that one of ordinary skill in the art would have recognized
immediate release properties even with compositions having PEO with a
molecular weight of up to 500,000.
Appellant also argues that a skilled artisan would not be motivated to
select such a PEO because it would extend the release profile of a drug. (See
Appeal Br. 14.) This argument is also unpersuasive because paragraph 85 of
Tygesen demonstrates that it was known that PEO within the claimed range
would not necessarily inhibit immediate release because it is included in a
composition for immediate release.
Appellant argues that the Examiner’s reliance on paragraph 238 of
McKenna is inappropriate because McKenna refers only to PEOs having a
molecular weight of 100,000 to 1,000,000 and 1,000,000 – 8,000,000 to
adjust a controlled release profile. (See Reply Br. 4–5.) Appellant’s claim
36 recites a PEO of 100,000 to 7,000,000 daltons. Tygesen teaches an
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immediate release composition including PEG with a molecular weight up to
500,000, which overlaps both the range recited in the claims and the range
taught by McKenna. Thus, we are not persuaded that paragraph 238 of
McKenna would not have suggested to one of ordinary skill in the art to
tailor the release rate of a drug formulation with a PEO within the claimed
range.
Appellant does not persuade us that the Examiner erred in rejecting
claim 36. Accordingly, we affirm the rejection of claim 36 as being obvious
over Tygesen and McKenna.
Other Dependent Claims
Appellant argues that claims 28, 37, and 39 stand or fall with the
patentability of claim 36. (See Appeal Br. 9.) Because we are not persuaded
that the Examiner erred in rejecting claim 36, we affirm the rejections of
claims 28, 37, and 39 as well.
Appellant argues separately for the patentability of claim 29 and claim
31. (See Appeal Br. 15–16.) Claim 29 depends on claim 28 and recites a
tablet as in claim 24, “wherein the gelling agent is a polyethylene oxide with
an approximate molecular weight of about 900,000 to about 5,000,000.” (Id.
at 19.) Claim 31 depends directly from claim 24 and recites “wherein the
gelling agent comprises at least two different types of polyethylene oxides
wherein the first polyethylene oxide has an approximate molecular weight
between 500,000 and 1,000,000 and the second polyethylene oxide has an
approximate molecular weight between 2,000,000 and 5,000,000.” (Id. at
19.)
Appellant argues only that “for the same reasons” as claim 24, a
skilled artisan would not have been either motivated to combine PEO
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polymers of the recited molecular weights or have reasonably expected them
to result in an immediate release tablet. (Id. at 15–16.)
As explained above, we are persuaded by the Examiner’s findings and
reasoning that it would have been obvious to one of ordinary skill in the art
to provide a tablet with PEO having a molecular weight within the claimed
ranges because Tygesen and McKenna teach that PEO of high MWs and low
MWs can be used to specifically tailor the drug release rate from a tablet
composition. (See Final Act. 8.) Appellant has neither argued nor
demonstrated any unexpected or surprising results commensurate in scope
with the narrower ranges recited in these claims over the lower molecular
weights encompassed in the broader ranges of the other claims, which would
be expected to be equally useful for an immediate release drug composition
according to the general teachings of Tygesen and McKenna discussed
above. Accordingly, we are not persuaded that the Examiner erred in
rejecting these claims.
Conclusion
Upon consideration of the record and for the reasons given, we affirm
the Examiner’s rejection.
In summary:
Claims Rejected Basis Affirmed Reversed
24–39 § 103 Tygesen,
McKenna
24–39

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

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AFFIRMED