Ex Parte Gerber et al

Patent Trials and Appeals Board

Mar 27, 2019

14240008 - (D) (P.T.A.B. Mar. 27, 2019)

UNITED STA TES p A TENT AND TRADEMARK OFFICE
APPLICATION NO. FILING DATE
14/240,008 02/20/2014
20999 7590 03/29/2019
HAUG PARTNERS LLP
745 FIFTH A VENUE - 10th FLOOR
NEW YORK, NY 10151
FIRST NAMED INVENTOR
Frederic Gerber
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
ATTORNEY DOCKET NO. CONFIRMATION NO.
247004-208 3578
EXAMINER
CHICKOS, SARAH J
ART UNIT PAPER NUMBER
1619
NOTIFICATION DATE DELIVERY MODE
03/29/2019 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):
docket@haugpartners.com
PTOL-90A (Rev. 04/07)
UNITED STATES PATENT AND TRADEMARK OFFICE
BEFORE THE PATENT TRIAL AND APPEAL BOARD
Ex parte FREDERIC GERBER, MARIE GUHMANN,
AND NORBERT POLLINGER1
Appeal 2018-005048
Application 14/240,008
Technology Center 1600
Before RICHARD M. LEBOVITZ, FRANCISCO C. PRATS, and
ROBERT A. POLLOCK, Administrative Patent Judges.
LEBOVITZ, Administrative Patent Judge.
DECISION ON APPEAL
This appeal involves claims directed to a pharmaceutical composition
comprising diclofenac. The Examiner rejected the claims as obvious under
35 U.S.C. § 103. Pursuant to 35 U.S.C. § 134(a), Appellants appeal the
Examiner's determination that the claims are unpatentable. We have
jurisdiction for the appeal under 35 U.S.C. § 6(b ). The Examiner's decision
is affirmed.
STATEMENT OF THE CASE
Claims 1-3 and 5-14 stand rejected by the Examiner under pre-AIA
35 U.S.C. § 103(a) as obvious in view of GB 2 217 598 Al, published Nov.
1 The Appeal Brief ("Br." entered Aug. 31, 2017) lists Glatt AG as the real-
party-in-interest. Br. 3.
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Application 14/240,008
1, 1989 ("Hagemann") and U.S. Patent No. 6,197,348 Bl, issued Mar. 6,
2001 ("Morella"). Ans. 3.
Claim 1, the only independent claim on appeal, is reproduced below:
1. A pharmaceutical composition comprising:
diclofenac, in a free acid form, as an active ingredient;
and
a (meth)acrylic polymer having at least one tertiary
amino group containing component;
wherein a ratio between (meth)acrylic polymer and
diclofenac is from 1 :20 to 1 :8.
DISCUSSION
The Examiner found that Hagemann describes a pharmaceutical
composition comprising diclofenac and Eudragit E, the latter which the
Examiner found is "a (meth)acrylic polymer having at least one tertiary
amino group containing component" as required by claim 1. Final Act. 3.
The Examiner found that Hagemann does not disclose the claimed ratio
"between (meth)acrylic polymer and diclofenac," but that Hagemann does
disclose an example of a pharmaceutical composition comprising a ratio of a
cellulose polymer to diclofenac of about 1: 10 that falls within the claimed
ratio of "1:20 to 1:8." Final Act. 4. The Examiner found that one of
ordinary skill in the art would have used this ratio to make the recited
composition with the claimed polymer. Id. The Examiner also found that
diclofenac is a results-effective variable in its activity in treating pain and
therefore it would be routine to arrive at the claimed ratio of polymer to
diclofenac recited in the claims. Id. The Examiner found that the skilled
worker would also have had reason to adjust the ratio in view of
Hagemann's teaching that "its compositions have excellent palatability and
are free of the irritating effects of the diclofenac active." Final Act. 5.
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The Examiner further cited Morella to meet the limitation in
dependent claim 10, which recites, "pellets with cores containing said
diclofenac, wherein said cores have a coating comprising said (meth)acrylic
polymer." Final Act. 5. The Examiner also found that Morella teaches
Eudragit E. Id.
Appellants state that the ratio of" 1 : 1 O" relied upon by the Examiner
in the rejection is between hydroxypropyl methyl cellulose (HPMC) and
diclofenac. Appeal Br. 11. Appellants state that HPMC is structurally and
functionally different from Eudragit E, which is the claimed polymer. Id.
Appellants argue "the differences of structure, functionality, and
effectiveness, as well as differences in density, make it clear that the mass
ratio of diclofenac to cellulose is not simply interchangeable with the ratio
for diclofenac to Eudragit® E." Id. at 12.
Appellants summarize the nine examples in Hagemann of diclofenac
combined with a polymer, calculating the ratio between the polymer and the
diclofenac for each example. Appeal Br. 15. Appellants argue that one of
ordinary skill in the art would have only have considered polymers in a
similar class to Eudragit E in deriving a teaching from the calculated ratios
of polymer to diclofenac. Id. at 12. Appellants state that the cellulose-type
polymer relied upon by the Examiner in finding the claimed ratio obvious is
not of the same type as Eudragit E. Id. Thus, Appellants argue that such
ratio would not have led one of ordinary skill in the art to claimed ratios
recited in claims 1 and 14.
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Application 14/240,008
Hagemann
Before addressing Appellants' arguments, we begin with a summary
of Hagemann's disclosure.
FF 1. 2 Hagemann describes effervescent tablets for producing an
aqueous solution of diclofenac that produces immediate or delayed release
of the drug. Hagemann 1:2-5.
FF2. Hagemann teaches that diclofenac is used to treat painful
inflammatory conditions. Hagemann 1: 11-15.
FF3. Hagemann also teaches that diclofenac is sparingly water
soluble. Hagemann 1: 14--15.
FF 4. Hagemann discloses that an object of its invention is "to provide
a novel and therapeutically more advantageous formulation for the sparingly
soluble drug diclofenac, which formulation disintegrates rapidly and has
improved taste." Hagemann 2 (last paragraph).
FF5. Hagemann discloses that the formulation "shall effect a uniform
distribution of the active drug in aqueous phase upon disintegration, without
its bitter taste being noticeable." Hagemann 2 (last paragraph).
FF6. Hagemann explains that this object is achieved by adding water
to the effervescent tablet comprising diclofenac to create a suspension
having a "neutral or pleasant taste" which is then ingested. Hagemann 3: 1-
15.
FF7. The diclofenac is coated "with a swellable coating which is
permeable to water." Hagemann 3:1-15.
2 "FF" is a finding of fact.
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FF8. The swellable coating "consists of an elastic film-like material
that is permeable to water or to aqueous body fluid such as gastric acid or
intestinal juice." Hagemann 4 (last paragraph)
FF9. Hagemann teaches that this coating can be made of high
permeability polymers to achieve rapid release of diclofenac, "for example
polyvinylpyrrolidone [PVP] or with a
dimethylaminoethylmethacrylate/methacrylate copolymer of the
EUDRAGIT E type (Rohm Pharma), and of suitable layer thickness, which
coating is soluble in the gastric juice." Hagemann 3: 18-21 ( emphasis
added).
FF 10. Hagemann also teaches that low permeability coatings can be
used "for example an acrylate/methacrylate copolymer of the EUDRAGIT
NE type and, if desired, of greater thickness, makes it possible to delay the
release of the active drug in the stomach with corresponding prolongation of
the duration of action." Hagemann 3 :25-29 ( emphasis added).
FFl 1. Hagemann also teaches the water-permeable elastic film-like
coating can be celluloses, such as "mixtures of water-soluble cellulose
derivatives such as hydroxypropyl methyl cellulose, and water-insoluble
ethyl cellulose," but does not characterize the celluloses' permeability
properties as being high or low. Hagemann 5. Hagemann also discloses
Aquacoat and Pharmacoat as examples of cellulose polymers. Hagemann 6.
FF 12. Hagemann discloses nine examples of pharmaceutical
compositions of polymer and diclofenac. Hagemann 10-16. Appellants
gathered this information into a table and calculated the ratio between the
polymer coating and the diclofenac. The Examiner does not dispute the
accuracy of the calculations. The table, reproduced below, has been
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Application 14/240,008
annotated on the left to identify the name of the polymer utilized in each
example and highlighted to emphasize the grouping of the polymers.
The table provided by Appellants shows that the ratio of the Eudragit
NE 30D, a low permeability polymer (FFlO), varied from 1: 1 to 1:7.14. The
only high permeability polymer used in the examples is PVP (FF9), which
was utilized in a ratio of 1 :4.65, which falls within the range of the low
permeability polymer. The cellulose polymers (Aquacoat and Pharmacoat),
whose relative permeability was not characterized by Hagemann, is present
in one composition with a polymer to diclofenac ratio of (1 :2.5) about the
same as the ratio of the low permeability Eudragit NE 30D (1 :2) and another
outside the lowest ratio of polymer to diclofenac used in the example
(1 :9.09).
Appellants' key argument is that one of ordinary skill in the art would
not have picked a ratio based on the Pharmacoat cellulose polymer
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formulation (1 :9.09) because it is dissimilar to the claimed high permeability
polymer (Eudragit E) in structure, function, and other characteristics, and its
permeability was not described by Hagemann. Appeal Br. 16. Appellants
argue that the other polymer formulations fall outside the claimed ratio of
1:8 to 1:20 (i.e., 1: 1 to 1:7.14 for low permeability Eudragit NE 30D and
1 :4.65 for high permeability PVP) and this would not have guided one of
ordinary skill in the art to have arrived at the claimed invention.
We have considered this argument, but it does not persuade us that the
Examiner erred in rejecting claim 1 as obvious based on Hagemann.
The purpose of Hagemann's invention is make a composition
comprising diclofenac which masks its bitter taste and is either neutral or
even pleasant tasting when ingested by a human. FF4-FF6. To accomplish
this purpose, Hagemann coats the diclofenac with a swellable coating
permeable to gastric acid or intestinal juices that releases the drug after
ingestion. FF7, FF8. Hagemann does not disclose that a specific ratio of
polymer to diclofenac is necessary to improve the taste of diclofenac and
make a pharmaceutical composition "without its bitter taste being
noticeable" (FF5). The examples show a range of 1: 1 to 1 :9.09, but
Appellants have not identified disclosure in Hagemann, which would limit
the ratio between polymer and diclofenac to only those disclosed in the
examples. It is well-established that disclosed examples and preferred
embodiments do not constitute a teaching away from a broader disclosure or
non-preferred embodiments. In re Susi, 440 F .2d 442, 169 USPQ 423
(CCPA 1971); Merck & Co v. Biocraft Laboratories, 874 F.2d 804, 807
(Fed. Cir. 1989) ("[A]ll disclosures of the prior art, including unpreferred
embodiments, must be considered."). Thus, Appellants' premise that the
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claimed ratio falls outside the ratio disclosed in Hagemann is a
misapprehension that the examples in Hagemann are limiting. Indeed,
Hagemann expressly teaches that "[ t ]he invention is illustrated by the
following non-limitative Examples." Hagemann 10.
It is evident from reading Hagemann that both diclofenac and polymer
are "result-effective variables" (Ans. 7-8), namely compounds whose
amounts are known to effect the desired result, which in this case is
alleviating pain and masking the diclofenac' s bitter taste while achieving the
desired release characteristics of the diclofenac upon ingestion, respectively.
Specifically, diclofenac is used to treat painful inflammatory conditions.
FF2. Consequently, one of ordinary skill would understand that its amount
in a composition would be varied depending on the severity of the pain
sought to be treated. With regard to the polymer, Appellants state "the type
of permeability, high or low, directly relates to how much coating one of
ordinary skill in the art would believe is needed to mask the bitter taste of
diclofenac" and thus "the permeability of the coating bears a direct
correlation to the amount that one of ordinary skill in the art would use."
Appeal Br. 16. In other words, the amount of polymer present in the
composition is also a result-effective variable. Therefore, one of ordinary
skill in the art would have had reason to adjust the amounts of both the
diclofenac and the Eudragit E to obtain a composition, which lacked a bitter
taste and possesses the desired drug release characteristics.
Appellants argue that one of ordinary skill in the art would not have
utilized the ratio of a formulation with cellulose (Examples 6 and 7) as
guidance to formulate Eudragit E because the cellulose's permeability is not
characterized. Appeal Br. 16. Appellants also argue the ratio of Eudragit
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NE because it is a low permeability polymer and Eudragit E is a high
permeability polymer (FF9). Id. Moreover, Appellants argue that the only
high permeability polymer used is PVP, has a ratio of 1 :4.65, and thus one of
ordinary skill in the art "would understand that a greater amount of a high
permeability coating-like Eudragit® E-would be needed to obtain the
same results achieved by a low permeability coating." Appeal Br. 15.
This argument is not supported by persuasive evidence. The only
high permeability polymer exemplified in Hagemann is PVP, which is
present in a ratio of polymer to diclofenac of 1 :4.65, a value that falls within
the range of 1: 1 to 1 :7.14 of the low permeability Eudragit NE 30D. Thus,
contrary to Appellants' argument, Hagemann's examples do not establish a
strict demarcation or correlation between the amount of polymer used in the
composition and its permeability. Rather, there are a number of different
suitable ratios for the low permeability polymer Eudragit NE 30D disclosed
by Hagemann, and the high permeability polymer PVP has one example
within the range utilized for the low permeability polymer. In addition, as
explained above, the examples do not limit Hagemann's invention
(Hagemann 10).
As held in In re Peterson, 315 F.3d 1325, 1329--30 (Fed. Cir. 2003),
there is a "normal desire of scientists or artisans to improve upon what is
already generally known." Thus, one of ordinary skill in the art would have
had reason to optimize the ratio between diclofenac and Eudragit E to
produce a composition with the desired release characteristics, while at the
same time having a neutral or pleasant taste. For the reasons described, we
do not find the examples to limit the ratio between diclofenac and polymer
utilized in a pharmaceutical composition.
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It has been long held that
even though applicant's modification results in great
improvement and utility over the prior art, it may still not be
patentable if the modification was within the capabilities of one
skilled in the art, unless the claimed ranges "produce a new and
unexpected result which is different in kind and not merely in
degree from the results of the prior art."
In re Huang, 100 F.3d 135, 139 (Fed. Cir. 1996) (quoting In re Aller, 220
F.2d 454,456 (1955), and citing In re Woodruff, 919 F.2d 1575, 1578 (Fed.
Cir. 1990)). In this case, Appellants disclose that their composition has the
same release properties and improvement in taste as disclosed for the
compositions described in Hagemann (FF4-FF6).
The Specification discloses:
it is an object of the invention to provide a pharmaceutical
composition of diclofenac exhibiting sufficient taste-masking
properties and at the same time being rapidly effective due to
improved release characteristics, i.e. improved disintegration
characteristics of the pharmaceutical composition and
dissolution characteristics of diclofenac.
Spec. 4:7-10 (also in Substitute Spec. at ,r 22). See also Appeal Br. 6 (third
full paragraph).
Hagemann teaches that Eudragit E can be used to mask the bitter taste
of diclofenac (FF9), the same discovery said to be made by Appellants. The
results obtained by Appellants may be a difference in degree, but not in kind,
because, at best, the inventors merely found that an even smaller ratio than
exemplified in Hagemann's examples could be used to achieve the same task
masking effect.
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For the foregoing reasons, the obviousness rejection of claim 1 is
affirmed. Claims 2, 3, 8-13 were not argued separately and therefore fall
with claim 1. 37 C.F.R. § 4I.37(c)(l)(iv).
Claims 5-7
Claims 5-7 further specify characteristics of the (meth)acrylic
polymer of claim 1. The Examiner found that such limitations were met by
Hagemann's disclosure of Eudragit E. Final Act. 4. Appellants contend
that it is not "clear" that Hagemann's Eudragit Eis the same as the current
version because the company has changed the name in the past. Appeal Br.
17-18. Appellants have not provided objective evidence to substantiate their
assertion. The Examiner reasonably found that the Eudragit E described in
Hagemann was the same Eudragit E from Evonik used in the Specification
and having the characteristics of the polymer of claims 5-7 because of the
name identity. The burden thus reasonably shifted to Appellants to
demonstrate that the Eudragit E disclosed in Hagemann does not possess the
claimed characteristics.
Claim 14
Claim 14 depends from claim 1 and further recites, "wherein a ratio
between (meth)acrylic polymer and diclofenac is from 1:20 to 1: 1 O."
The ratio between (meth)acrylic polymer and diclofenac recited in
claim 14 is outside the ratios disclosed in Examples 1-9 of Hagemann.
However, as discussed above, Hagemann does not limit the ratio to a
specific range or value. Hagemann specifically states, with respect to the
Examples 1-9, that "invention is illustrated by the following non-limitative
Examples." Hagemann 10. Appellants' attempt to limit Hagemann to the
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specific working examples and ratios thereof ignores Hagemann's own view
of the Examples as "non-limitative." As explained in the findings of fact,
Hagemann' s invention is "to provide a novel and therapeutically more
advantageous formulation for the sparingly soluble drug diclofenac, which
formulation disintegrates rapidly and has improved taste." FF4. Hagemann
accomplishes this by coating the diclofenac with a swellable polymer. FF7.
One of the polymers disclosed by Hagemann is Eudragit E (FF9), which the
Examiner found to meet the limitations of claims 1 and 14. Appellants seek
to patent the same combination suggested by Hagemann, namely diclofenac
and Eudragit E, combined for the same purpose in masking the bitter taste of
diclofenac (FF4-FF6; Appeal Br. 6). The only difference between
Hagemann and the claims is that the claims are directed to specific ratio
between the two components not expressly disclosed in Hagemann.
Appellants have not shown that this ratio between the polymer and
diclofenac has any property or characteristic that differs in kind from those
disclosed in Hagemann's examples. Appellants have simply found that even
less polymer is necessary to mask the taste of diclofenac than disclosed in
Hagemann's examples. But these examples were not considered to be
limiting by Hagemann, and Appellants have not done anything more than
routinely optimize the amounts of diclofenac and Eudragit E to have arrived
at the claimed ratio.
The law is replete with cases in which the difference between the
claimed invention and the prior art is some range or other
variable within the claims ... in such a situation, the applicant
must show that the particular range is critical, generally by
showing that the claimed range achieves unexpected results
relative to the prior art range.
In re Woodruff, 919 F.2d 1575, 1578 (Fed. Cir. 1990).
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As Appellants have not shown the claimed range in claim 14 ( or
claims 1) is critical, we affirm the rejection.
For the foregoing reasons, the obviousness rejection of claims 1-3 and
5-14 are affirmed. 37 C.F.R. 4I.37(c)(l)(iv).
TIME PERIOD
No time period for taking any subsequent action in connection with
this appeal may be extended under 37 C.F.R. § 1.136(a)(l )(iv).
AFFIRMED
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