Ex Parte Thon¿

Patent Trial and Appeal Board

Sep 26, 2017

12517665 (P.T.A.B. Sep. 26, 2017)

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.
12/517,665 06/04/2009 Daniel Joseph Christiaan Thon^, TIP0061USPCT 9112
27777 7590 09/28/2017
JOSEPH F. SHIRTZ
JOHNSON & JOHNSON
ONE JOHNSON & JOHNSON PLAZA
NEW BRUNSWICK, NJ 08933-7003
EXAMINER
SOROUSH, LAYLA
ART UNIT PAPER NUMBER
1627
NOTIFICATION DATE DELIVERY MODE
09/28/2017 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):
j nju spatent @ coru s .j nj. com
lhowd@its.jnj.com
pair_jnj @ firsttofile.com
PTOL-90A (Rev. 04/07)
UNITED STATES PATENT AND TRADEMARK OFFICE
BEFORE THE PATENT TRIAL AND APPEAL BOARD
Ex parte DANIEL JOSEPH CHRISTIAAN THONE1
Appeal 2017-002082
Application 12/517,665
Technology Center 1600
Before DONALD E. ADAMS, ERIC B. GRIMES,
and JOHN E. SCHNEIDER, Administrative Patent Judges.
SCHNEIDER, Administrative Patent Judge.
DECISION ON APPEAL
This is an appeal under 35 U.S.C. § 134(a) involving claims to
pharmaceutical composition for treating AIDS which have been rejected as
obvious and for non-statutory obviousness-type double patenting. We have
jurisdiction under 35 U.S.C. § 6(b).
We affirm.
STATEMENT OF THE CASE
Human immunodeficiency virus (HIV) is the agent for causing
acquired immunodeficiency syndrome (AIDS). Spec. 1. “The spread of
HIV has caused and continues to cause serious health problems throughout
1 Appellant identifies the Real Party in Interest as Janssen Sciences Ireland
UC. Appeal Br. 1.
Appeal 2017-002082
Application 12/517,665
the world. Consequently, the search for effective pharmaceutical agents to
treat HIV infection is of vital importance.” Id. “One class of anti-HIV
pharmaceutical agents comprises the non-nucleoside reverse transcriptase
inhibitors (NNRTIs).” Id. One problem with at least some NNRTIs is that
they are poorly soluble in water and have low bioavailability. Id. The
Specification describes a pharmaceutical composition containing an NNRTI
which an improved solubility in water and improved bioavailability. Spec.
3.
Claims 1, 4, 7, 11, 12, and 14 are on appeal. Claims 1 and 11 are the
independent claims and read as follow:
1. A pharmaceutical composition for immediate release
comprising a solid dispersion consisting of a compound of
formula (I):
Bx
A < ; J- . Nl!
' A A'\V
A XA" X,. -X*'
HN, HBf
\V
X
said compound having a degree of crystallinity of about 10% or
less, in a water soluble polymer selected from the group
consisting of hydroxypropylmethyl cellulose, polyvinyl
pyrrolidone, copolyvidone, and vitamin E TGPS; and wherein
the weight : weight ratio of the polymer to compound being in
the range from 3:1 to 1:1.
2
Appeal 2017-002082
Application 12/517,665
11. A pharmaceutical composition for immediate release
comprising a solid dispersion consisting of a compound of
formula (I):
Br
-k ,k
N
m.
k.
BBr
"•-V
kN
(I)
said compound having a degree of crystallinity of about 10% or
less, and microcrystalline cellulose,
in a water soluble polymer selected from the group consisting of
hydroxypropylmethyl cellulose, polyvinyl pyrrolidone,
copolyvidone, and vitamin E TGPS; and wherein the weight :
weight ratio of the polymer to compound being in the range from
3:1 to 1:1.
The claims stand rejected as follows:
Claims 1 and 7 have been rejected under 35 U.S.C. § 103(a) as
unpatentable over Raoof2 in view of Siepmann.3
2 A. Raoof et al., The Pharmacokinetics ofTMC125 in different mouse
strains: impact on carcinogenicity testing strategy, Abstract, 11th Annual
FDA Science Forum (April 1005) (copy of record, submitted June 4, 2009)
(“Raoof’).
3 J. Siepmann & N.A. Peppas, Modeling of drug release from delivery
systems based on hydroxypropyl methylcellulose (HPMC), 48 Adv. Drug
Deliv. Reviews 139-57 (2001) (“Siepmann”).
3
Appeal 2017-002082
Application 12/517,665
Claims 1 and 7 have been rejected under 35 U.S.C. § 103(a) as
unpatentable over Raoof in view of Winston.4
Claims 1 and 7 have been rejected under 35 U.S.C. § 103(a) as
unpatentable over Raoof in view of Scholler.5
Claim 4 has been rejected under 35 U.S.C. § 103(a) as unpatentable
over Raoof in view of Siepmann in further view of Gilis.6
Claim 4 has been rejected under 35 U.S.C. § 103(a) as unpatentable
over Raoof in view of Winston in further view of Gilis.
Claim 4 has been rejected under 35 U.S.C. § 103(a) as unpatentable
over Raoof in view of Scholler in further view of Gilis.
Claims 11, 12, and 14 have been rejected under 35 U.S.C. § 103(a) as
unpatentable over Raoof in view of Siepmann in further view of Reier.7
Claims 11, 12, and 14 have been rejected under 35 U.S.C. § 103(a) as
unpatentable over Raoof in view of Winston in further view of Reier.
Claims 11, 12, and 14 have been rejected under 35 U.S.C. § 103(a) as
unpatentable over Raoof in view of Scholler in further view of Reier.
4 Alan Winston et al., The clinical pharmacology of antiretrovirals in
development, 2 Expert Opin. Drug Metab. Toxicol. 447—58 (2006)
(“Winston”).
5 M. Scholler et al., Substantial improvement of oral bioavailability of
TMC125 using new tablet formulations in healthy volunteers, Poster
Exhibition: The 3rd IAS Conference on HIV Pathogenesis and
Treatment: Abstract No. TuPe3.1Bl 1 (2005) (copy of record by the
Examiner June 16, 2015) (“Scholler”).
6 Gilis et al., US 2005/0142188 Al, published June 30, 2005 (“Gilis”).
7 George E. Reier & Ralph F. Shangraw, Microcrystalline Cellulose in
Tableting, 55 J. Pharm. Sci. 510—14 (1966) (“Reier”).
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Appeal 2017-002082
Application 12/517,665
Claims 1, 4, 5, 7, 11, and 14 have been rejected on the ground of
nonstatutory obviousness-type double patenting as being unpatentable over
claims 1—5 of Lamoureux.8
OBVIOUSNESS
Claims 1, 7, 11, 12, and 14
Issue
The issue with respect to these rejections is whether a preponderance
of the evidence supports the Examiner’s conclusion that claim 1 would have
been obvious over Raoof combined with either Siepmann, Winston, or
Scholler. Appellant does not provide separate arguments for claim 7.
Further, although claims 11, 12, and 14 have been rejected over Raoof
combined with Siepmann, Winston, or Scholler further in view of Reier,
Appellant has not offered any specific arguments with respect to these
claims, but has addressed these claims along with claim 1. Appeal Br. 5.
We interpret Appellant’s argument to be that Reier fails to make up for
Appellant’s alleged deficiency in the combination of Raoof with Siepmann,
Winston, or Scholler. Therefore, we find that claims 7, 11, 12, and 14 stand
or fall with claim 1.
The Examiner finds that Raoof teaches Compound I (TMC125-HBr).
Final Act. 2. The Examiner finds that Siepmann, Winston and Scholler all
teach the addition of HPMC to compound I to improve solubility. Final Act.
3—6. The Examiner concludes that it would have been obvious to one skilled
in the art to combine the teachings of Raoof with Siepmann, Winston, or
Scholler to produce the claimed invention. Id.
8 Lamoureux et al., US 8,722,696 B2, issued May 13, 2014 (“Lamoureux”).
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Appeal 2017-002082
Application 12/517,665
Appellant contends that the references do not teach or suggest that
TMC125-HBr has a crystallinity of less than 10%. Appeal Br. 6—7.
Appellant argues that the references do not teach or suggest the recited
weight ratios for TMC125-HBr and HPMC. Id. at 7—8. Appellant also
argues that none of the references teach the preparation of a solid dispersion
for immediate release. Id. at 8.
Principles of Law
[T]he examiner bears the initial burden, on review of the prior art
or on any other ground, of presenting a prima facie case of
unpatentability. If that burden is met, the burden of coming
forward with evidence or argument shifts to the applicant.
After evidence or argument is submitted by the applicant
in response, patentability is determined on the totality of the
record, by a preponderance of evidence with due consideration
to persuasiveness of argument.
In re Oetiker, 977 F.2d 1443, 1445 (Fed. Cir. 1992).
A proper § 103(a) analysis requires “a searching comparison of the
claimed invention—including all its limitations—with the teaching of the
prior art.” In re Ochiai, 71 F.3d 1565, 1572 (Fed. Cir. 1995).
Where ... the claimed and prior art products are identical or
substantially identical ... the PTO can require an applicant to
prove that the prior art products do not necessarily or inherently
possess the characteristics of his claimed product. . . . [The]
fairness [of the burden-shifting] is evidenced by the PTO’s
inability to manufacture products or to obtain and compare prior
art products.
In re Best, 562 F.2d 1252, 1255 (CCPA 1977).
“[T]he discovery of an optimum value of a variable in a known
process is normally obvious.” Exceptions to this rule include (1) the results
of optimizing a variable were unexpectedly good and (2) the parameter
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Appeal 2017-002082
Application 12/517,665
optimized was not recognized in the prior art as one that would affect the
results. In re Antonie, 559 F.2d 618, 620 (CCPA 1977).
Analysis
We adopt the Examiner’s findings of fact, reasoning on scope and
content of the prior art, and conclusions set out in the Final Office Action
and Answer regarding this rejection. We find the Examiner has established
that the claims would have been obvious in view of Raoof combined with
Siepmann, Winston, or Scholler. Appellant has not produced evidence
showing, or persuasively argued, that the Examiner’s determinations on
obviousness are incorrect. Only those arguments made by Appellant in the
Briefs have been considered in this Decision. Arguments not presented in
the Briefs are waived. See 37 C.F.R. § 41.37(c)(l)(iv) (2015). We have
identified claim 1 as representative; therefore, all claims fall with claim 1.
We address Appellant’s arguments below.
Appellant contends that none of the references teach or suggest that
the compound of formula I has a degree of crystallinity of less than 10%.
Appeal Br. 6—7. We are unpersuaded. The present Specification teaches
that it was known in the art that the degree of crystallinity is inversely
proportional to the bioavailability of poorly water soluble pharmaceutical
compositions. Spec. 2. Thus, one skilled in the art would have been
motivated to use an active agent that is low in crystallinity or amorphous to
enhance bioavailability. Moreover, the references teach the same
compounds and adjuvants as those found in the claims. Final Act. 2—6.
Since the compositions in the references are the same as what is instantly
claimed, the burden shifts to Appellant to demonstrate that the prior art
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Application 12/517,665
products do not inherently possess a low crystallinity. Best, 562 F.2d at
1255.
Appellant argues that the references do not teach or suggest the
claimed weight ratios for the active ingredient and polymer. Appeal Br. 7.
Appellant contends that the references do not set forth the general conditions
from which one skilled in the art would be expected to derive the optimal
conditions. Id. Appellant’s argument is not persuasive. We agree with the
Examiner that the references suggest a general condition of a ratio of 1:1 and
that it would have been a matter of routine manipulation of parameters to
discover the optimum ratios. Ans. 21—22. Appellant has offered no
evidence to show that the claimed ratios produced unexpected results or that
the ratio of polymer and active ingredient would not be looked to in order to
optimize the effectiveness of the composition. Antonie, 559 F.2d at 620.
Appellant argues that none of the references teach or suggest a solid
dispersion for immediate release. Appeal Br. 8. We are unpersuaded.
Scholler specifically teaches a tablet of TMC125 with HPMC. Scholler 1.
Siepmann teaches that the surface area of HPMC tablets can be varied to
control the release rate. Siepmann 143. We agree with the Examiner that it
would have been obvious to one skilled in the art to produce a solid
composition containing TMC125 and HPMC and to adjust the surface area
of HPMC tablets to produce a composition which yields immediate release
of the active agent. Ans. 21—22.
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Application 12/517,665
Conclusion of Law
We conclude that claim 1 would have been obvious over Raoof
combined with Siepmann, Winston, or Scholler.
Claims 7, 11, 12, and 14 have not been argued separately and,
therefore, fall with claim 1. 37 C.F.R. § 41.37(c)(l)(iv).
Claim 4
Appellant contends that the references do not teach or suggest that one
skilled in the art would have selected HPMC 2910 5mPa as the specific
HPMC to use in the claimed composition. Appeal Br. 9. Appellant
contends that Gilis is limited to teaching which azoles should be used with
HPMC 2910 5mPa. Id. We are not persuaded. Gilis teaches that HPMC
2910 5mPa is a commercially available form of HPMC suitable for use in
drug compositions containing a lipophilic active agent. Gilis 38-40.
Appellant’s Specification acknowledges that TMC125 was a known
compound and has low water-solubility (Spec. 1); i.e., it is lipophilic rather
than hydrophilic. Gilis also teaches that the addition of HPMC aids in the
bioavailability of the lipophilic active ingredient and teaches a weight ratio
of drug to polymer of from 1:1 to 1:5. Gilis 40-42. We agree with the
Examiner that it would have been obvious to one skilled in the art to use
HPMC 2910 5mPa as the polymer in the claimed composition. Ans. 22—23.
Conclusion of Law
We conclude that a preponderance of evidence supports the
Examiner’s conclusion that claim 4 would have been obvious over Raoof
combined with Siepmann, Winston, or Scholler further combined with Gilis.
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Appeal 2017-002082
Application 12/517,665
OBVIOUSNESS-TYPE DOUBLE PATENTING
Issue
The issue with respect to this rejection is whether a preponderance of
the evidence supports the Examiner’s conclusion that claims 1, 4, 7, 11, 12,
and 14 are not patentably distinct from claims 1—5 of Lamoureux.
The Examiner finds that Lamoureux claims a pharmaceutical
composition comprising the same compound as formula I in the instant
claims with a surface active agent and a hydrophilic polymer. Final Act. 17.
The Examiner finds that the present claims call for the same active
ingredient with a hydrophilic polymer such as HPMC. Id. The Examiner
concludes that the composition recited in the present claims is not patently
distinct from the composition claimed in Lamoureux. Final Act. 17.
Appellant contends that the present claims are patently distinct from
those of Lamoureux in that Lamoureux does not teach or suggest that the
active agent has a degree of crystallinity of less than 10% or the weight ratio
recited in the instant claims. Appeal Br. 9—10.
Principles of Law
The primary inquiry in double patenting cases is therefore
whether the claims in the latter [sic, later] patent are more than a
“slight variant” from the claims in the earlier patent. . . .
Nonetheless, nonstatutory double patenting is sometimes
referred to as “obviousness-type” double patenting . . . and
“prevents the extension of the term of the original patent via the
patenting of an obvious variation.” . . .
Eli Lilly & Co. v. Teva Pharms. USA, Inc., 619 F.3d 1329, 1341—42 (Fed.
Cir. 2010) (internal citations omitted).
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Appeal 2017-002082
Application 12/517,665
Analysis
We agree with the Examiner that the instant claims represent nothing
more than an obvious variant of the claims of Lamoureux. Lamoureux
claims the same active agent combined with a hydrophilic polymer such as
HPMC. Lamoureux claims 1 and 3. While Lamoureux does not claim a
specific range of polymer to active agent weight ratio, nor do the claims
specify the percent crystallinity of the active agent, as discussed above, those
parameters would have been obvious based on the knowledge of a person of
ordinary skill in the art. Thus, the present claims are nothing more than an
obvious variant of those in Lamoureux.
Conclusion of Law
We conclude that a preponderance of the evidence supports the
Examiner’s conclusion that the pending claims are not patentably distinct
from those of Lamoureux.
SUMMARY
We affirm the rejections under 35 U.S.C. § 103(a).
We affirm the rejection for obviousness-type double patenting.
TIME PERIOD LOR 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).
AFFIRMED
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