Lieven Baert et al.

Patent Trials and Appeals Board

Sep 4, 2020

2019006010 (P.T.A.B. Sep. 4, 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.
12/161,445 04/12/2011 Lieven Elvire Colette Baert TIP0120USPCT 1385
27777 7590 09/04/2020
JOSEPH F. SHIRTZ
JOHNSON & JOHNSON
ONE JOHNSON & JOHNSON PLAZA
NEW BRUNSWICK, NJ 08933-7003
EXAMINER
CHONG, YONG SOO
ART UNIT PAPER NUMBER
1627
NOTIFICATION DATE DELIVERY MODE
09/04/2020 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):
jnjuspatent@corus.jnj.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 LIEVEN ELVIRE COLETTE BAERT, GUENTER KRAUS, and
GERBEN ALBERT ELEUTHERIUS VAN 'T KLOOSTER
____________

Appeal 2019-006010
Application 12/161,445
Technology Center 1600
____________

Before DONALD E. ADAMS, ERIC B. GRIMES, and
RICHARD M. LEBOVITZ, Administrative Patent Judges.

ADAMS, Administrative Patent Judge.

DECISION ON APPEAL
Pursuant to 35 U.S.C. § 134(a), Appellant1 appeals from Examiner’s
decision to reject claims 10, 17–25, and 28–30 (see Appeal Br. 2; see also
Final Act. 2). We have jurisdiction under 35 U.S.C. § 6(b).
We REVERSE.

1 We use the word “Appellant” to refer to “applicant” as defined in 37
C.F.R. § 1.42. Appellant identifies the real party in interest as “Janssen
Sciences Ireland UC, an affiliate of Johnson & Johnson.” (Appellant’s April
3, 2019 Appeal Brief (Appeal Br.) 1).
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STATEMENT OF THE CASE
Appellant’s disclosure “relates to the long term treatment of HIV
infection by intermittently administering a parenteral formulation
comprising the . . . [non-nucleoside reverse transcriptase inhibitor (NNRTI)
4-[[4-[[4-(2-cyanoethenyl)-2,6-dimethylphenyl]-amino]-2-pyrimidinyl]-
amino]-benzonitrile, also referred to as] TMC278 at relatively long time
intervals” (Spec. 1: 5–7, 35–37). Appellant’s claim 10 is reproduced below:
10. A method of treating HIV in a subject comprising
administering to the subject a solution comprising
an amount of 4-[[4-[[4-(2-cyanoethenyl)-2,6-
dimethylphenyl]amino]-2-
pyrimidinyl]amino]benzonitrile (TMC278) or a
pharmaceutically acceptable acid addition salt thereof,
and a carrier,
wherein the solution is administered intermittently by
subcutaneous or intramuscular administration at a time
interval that is once every one month or once every four
weeks,
and
wherein the amount of TMC278, or the pharmaceutically
acceptable acid-addition salt thereof, is effective in
keeping a minimum blood plasma level of TMC278 in
the subject during the time interval.
(Appeal Br. 12.)

Claims 10, 17–25, and 28–30 stand rejected under 35 U.S.C. § 103(a)
as unpatentable over the combination of Buelow2 and Susman.3

2 Buelow et al., US 2004/0127422 A1, published July 1, 2004.
3 Edward Susman, Retroviruses and Opportunistic Infections – 12th
Conference, 8 IDrugs 299–302 (2005).
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ISSUE
Does the preponderance of evidence relied upon by Examiner support
a conclusion of obviousness?
FACTUAL FINDINGS (FF)
FF 1. Buelow “relates to pharmaceutical preparations and methods for
treating HIV and AIDS, and in particular, to novel combinations of
immunomodulatory peptides and anti-retroviral agents” (Buelow ¶ 2; see
Ans. 4).
FF 2. Buelow discloses that its anti-retroviral agent may be a “non-
nucleoside reverse transcriptase inhibitor [(NNRTI)] selected from the group
consisting of Nevirapine, Dlavirdine, and Efavirenz” (Buelow ¶ 16; see Ans.
4).
FF 3. Buelow discloses that its pharmaceutical preparations, i.e.,
compositions, comprise a pharmaceutically acceptable carrier and “may be
formulated as[, inter alia,] solutions” (Buelow ¶ 108; see Ans. 4 (citing
Buelow ¶¶ 64, 100, 108, 110)).
FF 4. Buelow discloses that its pharmaceutical preparation may be
administered “in a variety of ways, including,” subcutaneously and
intramuscularly (Buelow ¶ 130; see Ans. 4–5).
FF 5. Buelow discloses subcutaneous and intramuscular administration is
preferably carried out with peptides and anti-retroviral agents dissolved or
suspended in suitable aqueous medium” (Buelow ¶ 133; see also id. ¶ 130
(Buelow exemplifies the use of “microparticle, microsphere, and
microencapsulate formulations . . . for oral, intramuscular, or subcutaneous
administrations”); see Ans. 4–5, 7).

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FF 6. Buelow discloses the use of delivery systems to administer
a pharmaceutically therapeutic amount of subject compounds
for more than a day, preferably more than a week, and most
preferabl[y] at least about 30 days to 60 days, or longer[,
wherein,] [l]ong term release systems may comprise
implantable solids or gels containing the subject peptide, such
as biodegradable polymers . . .; pumps, including peristaltic
pumps and fluorocarbon propellant pumps; osmotic and mini-
osmotic pumps; and the like.
(Buelow ¶ 134; see Ans. 5.)
FF 7. Examiner finds that Buelow “fails to disclose the specific NNRTI,
TMC278 (also known as rilpivirine)” (Ans. 5).
FF 8. Susman discloses that rilpivirine has “a half-life of 38 [hours]”
(Susman 300; see Ans. 5).
FF 9. Susman observed a “decline in viral load with rilpivirine [that] was
statistically significant at all doses (25, 50, 100 and 150 mg/day; p < 0.001)”
during “a proof-of-principle 7-day clinical trial” (Susman 300; see Ans. 5).
ANALYSIS
Based on the combination of Buelow and Susman, Examiner
concludes that, at the time Appellant’s invention was made, it would have
been prima facie obvious to use Susman’s NNRTI, TMC278, as the NNRTI
in Buelow’s pharmaceutical preparations for the treatment of a patient with
HIV (Ans. 5). According to Examiner, a
person of ordinary skill in the art would have been motivated to
substitute TMC278 for [Buelow’s NNRTI] because of the
functional equivalency of . . . NNRTIs . . . . Therefore, one of
ordinary skill in the art would have had a reasonable
expectation of success in treating a subject with HIV by
administering a composition comprising the NNRTI, TMC278.
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(Id. at 5–6.) We are not persuaded that Examiner has established prima facie
obviousness for the claimed invention.
As Appellant explains, Susman discloses “that the half-life of
TMC278 is only about 38 hours (about 1.5 days)” and Buelow “discloses
that pumps or biodegradable solids or gels are needed to achieve extended
periods of sustained therapeutic blood plasma levels of anti-HIV agents”
(Appeal Br. 10; see FF 6 and 8). Thus, Appellant contends that “[e]ven if
those of ordinary skill in the art would have prepared a TMC278-containing
solution for subcutaneous or intramuscular injection, they would not have
predicted that a single injection would provide for therapeutically effective
plasma levels of TMC278 for at least 4 weeks” (Appeal Br. 9; see also
Reply Br. 3 (Appellant contends that “the record indicates that those of
ordinary skill in the art would not have been able to predict whether or not
an injected TMC278 solution would have exhibited the requisite[, i.e.
Appellant’s claimed pharmacokinetic,] profile”)). We agree.
As Appellant further explains, “there is no art of record that would
even have been relevant to a person seeking to convert a once-daily, oral
treatment regimen to a once-monthly protocol” (Reply Br. 3). To the extent
that Examiner would contend that those of ordinary skill in this art would
administer the composition suggested by the combination of Buelow and
Susman with the aid of a pump, Examiner failed to identify a reasonable
expectation of success that TMC278, with its known short half-life, could be
formulated for administration once every one month or once every four
weeks as required by Appellant’s claimed invention.
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CONCLUSION
The preponderance of evidence relied upon by Examiner fails to
support a conclusion of obviousness. The rejection of claims 10, 17–25, and
28–30 under 35 U.S.C. § 103(a) as unpatentable over the combination of
Buelow and Susman is reversed.

DECISION SUMMARY
In summary:
Claims
Rejected
35 U.S.C. § Reference(s)/Basis Affirmed Reversed
10, 17–25,
28–30
103 Buelow, Susman 10, 17–25,
28–30

REVERSED