Ex Parte Brown et al

Patent Trial and Appeal Board

Oct 22, 2018

14567554 (P.T.A.B. Oct. 22, 2018)

UNITED STA TES p A TENT AND TRADEMARK OFFICE
APPLICATION NO. FILING DATE
14/567,554 12/11/2014
20462 7590 10/24/2018
GlaxoSmithKline
Global Patents UP4110
1250 South Collegeville Road
Collegeville, PA 19426
FIRST NAMED INVENTOR
Jonathan R. Brown
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.
BMS11265Cl 9920
EXAMINER
SOROUSH, LAYLA
ART UNIT PAPER NUMBER
1627
NOTIFICATION DATE DELIVERY MODE
10/24/2018 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):
US_cipkop@gsk.com
laura.m.mccullen@gsk.com
eofficeaction@appcoll.com
PTOL-90A (Rev. 04/07)
UNITED STATES PATENT AND TRADEMARK OFFICE
BEFORE THE PATENT TRIAL AND APPEAL BOARD
Ex parte JONATHAN R. BROWN, HELEN HUGHES,
ANDREW B. DENNIS, and PETER TIMMINS
Appeal2017-009160
Application 14/567 ,554
Technology Center 1600
Before MICHAEL J. FITZPATRICK, ULRIKE W. JENKS, and
TIMOTHY G. MAJORS, Administrative Patent Judges.
FITZPATRICK, Administrative Patent Judge.
DECISION ON APPEAL
Jonathan R. Brown, Helen Hughes, Andrew B. Dennis, and Peter
Timmins ("Appellants") 1 appeal under 35 U.S.C. § 134(a) from a final
decision rejecting claims 1-19, 21, and 27. We have jurisdiction under 35
U.S.C. § 6(b).
We affirm.
1 The real party in interest is identified as "ViiV Healthcare UK (No.4)
Limited." Appeal Br. 3.
Appeal2017-009160
Application 14/567,554
STATEMENT OF THE CASE
The Specification
According to Appellants, the "present invention relates to a novel
formulation providing an appropriate pharmacokinetic (PK) profile for the
treatment of HIV infection, and more particularly, to a highly stable,
extended release formulation containing an HIV attachment inhibitor and
hydroxypropyl methylcellulose with no enzyme inhibitors that is efficacious
against HIV." Spec. 1: 10-14.
The Rejected Claims
Claims 1-19, 21, and 27 stand rejected. Final Act. 1. Claims 20 and
26 are cancelled, and claims 22-25, 28, and 29 are withdrawn from
consideration. Id.; Appeal Br. 12-13.
Claim 1 is representative and reproduced below.
1. A pharmaceutical composition comprising
the phosphate ester prodrug of an HIV attachment
inhibitor, 1-benzoyl-4-[2-[ 4-methoxy-7-(3-methyl-lH-1,2,4-
triazol-1-yl)-1-[(phosphonooxy)methyl]-1H-pyrrolo[2,3-c
Jpyridin-3-yl]-1,2-dioxoethyl]-piperazine in the form of a tris
salt, and
hydroxypropyl methyl cellulose (HPMC) having a
hydrated viscosity of at least about 100 cP,
microcrystalline cellulose,
silicon dioxide, and
magnesium stearate,
wherein said composition provides a desired extended
absorption of the parent compound when administered to
humans, provides for stability of the prodrug against alkaline
phosphatase while still contained within the dosage form under
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post-administration conditions, and further wherein said
composition does not contain any enzyme inhibitors.
Appeal Br. 10 (paragraphing added).
The Appealed Rejections
The following rejections are before us for review:
1. claims 1-19, 21, and 27 are rejected under 35 U.S.C. § 103 as
unpatentable over Ueda2 and Vergnault3 (Final Act. 5); and
2. claims 1-19, 21, and 27 are rejected under 35 U.S.C. § 103 as
unpatentable over Ueda and Chouinard4 (Final Act. 8).
DISCUSSION
Rejection 1
The Examiner rejects claims 1-19, 21, and 27 under 35 U.S.C. § 103
as unpatentable over Ueda and Vergnault. Final Act. 5.
Ueda "relates to compounds useful for the treatment of HIV and
AIDS." Ueda i-f2. The Examiner finds that Ueda teaches all of the subject
matter of claim 1, save for the HPMC and silicon dioxide components. Final
Act. 5-6. Appellants do not dispute these findings. See, e.g., Appeal Br. 7
("The Examiner is correct that Ueda discloses the prodrug of the current
claims."); see also Ueda ,II028 ("As immediate release tablets, these
compositions may contain microcrystalline cellulose, dicalcium phosphate,
starch, magnesium stearate and lactose and/or other excipients, binders,
2 US 2005/0209246 Al, published Sept. 22, 2005 ("Ueda").
3 US 7,927,624 B2, issued Apr. 19, 2011 ("Vergnault").
4 US 5,885,615, issued Mar. 23, 1999 ("Chouinard").
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extenders, disintegrants, diluents and lubricants known in the art.") ( cited at
Final Act. 6) ( emphasis added).
Vergnault "relates to a dosage formulation or tablet comprising a
mixed matrix of hydrophilic and lipophilic components able to control the
release rate of one or more therapeutically active agents from the
formulation/tablet." Vergnault 1:20-24. The Examiner found that
"Vergnault et al. teaches hydroxypropyl methyl cellulose (HPMC) is capable
of achieving controlled release and other excipients can be included in the
composition, including silicon dioxide (which is a glidant; Col. 9, lines 54-
59; see Examples) in the tablet oral formulation." Final Act. 3; see also id.
at 6 (citing Vergnault 6:17-18, 6:32-35); Vergnault, e.g., 30:41 (Example 19
employing silicon dioxide as a glidant). Vergnault further teaches that the
HPMC may have a viscosity of 100 cP. Vergnault 8:22-24. Appellants do
not dispute the Examiner's findings with respect to Vergnault. See, e.g.,
Appeal Br. 7 ("The Examiner states that Vergnault discloses HPMC. This is
correct.").
The Examiner concludes that it would have been obvious to combine
the teachings of Ueda and Vergnault to form a pharmaceutical composition
within the scope of the claims. Specifically, the Examiner asserts that the
person of skill would have been "motivated to include such an HPMC [and
the optional silicon dioxide as a glidant] because Vergnault et al. teaches that
HPMC can increase water uptake and aid in gelling, increasing the matrix
viscosity and decreasing the release rate of the drug." Final Act. 7.
Appellants "agree that none of the components in the presently
claimed composition are novel." Appeal Br. 6. Appellants further "agree
that each of the specifically required components have been used in
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Application 14/567,554
pharmaceutical compositions before." Id. at 6-7. But Appellants argue that
the specific combinations recited by the claims are novel and not obvious.
Id. at 7.
Specifically, Appellants argue the following:
[I]t is insufficient for the Examiner to point to long lists of
possible components in the prior art as evidence that it would be
obvious to make a composition comprising 1) a prodrug
disclosed in Ueda, 2) HPMC wherein 3) said HPMC has a
hydrated viscosity of at least about lOOcP, 4) microcrystalline
cellulose, 5) silicon dioxide, 6) magnesium stearate, and wherein
7) said composition does not contain any enzyme inhibitors. In
order to establish a case of prima facie obviousness, the
Examiner needs to show why, without use of hindsight, it would
have been obvious to choose all 4 of the specific 4 ingredients
required by claim 1 and further, why it would also have been
obvious to exclude enzyme inhibitors.
Id. at 8; see also Reply Br. 2 ("It appears that the Examiner is taking the
position that a prior art disclosure that mentions the possible inclusion of
thousands of ingredients makes any specified subset, no matter how large,
obvious. This is not correct.").
We are not persuaded by Appellants' arguments. As discussed above,
Ueda discloses pharmaceutical compositions containing the same pro drug as
recited in the claims, microcrystalline cellulose, and magnesium stearate.
And, as further discussed above, V ergnault teaches the person of ordinary
skill that (1) HPMC at 100 cP can be added to a pharmaceutical composition
to support a controlled release of a drug and (2) silicon dioxide can be added
to serve as a glidant.
With respect to the Reply Brief argument that the rejection requires
too much picking and choosing of individual components from Ueda and
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Application 14/567,554
Vergnault to arrive at the claimed composition, we remain unpersuaded on
the record before us. See Merck & Co., Inc. v. Biocraft Labs., Inc., 874 F.2d
804, 807 (Fed. Cir. 1989) (species claim held obvious where it recited one of
1200 possible combinations of embodiments disclosed by reference and
where reference suggested no preference for claimed embodiment). "That
the [prior art] discloses a multitude of effective combinations does not
render any particular formulation less obvious." Id. "This is especially true
because the claimed composition is used for the identical purpose taught by
the prior art." Id.; see also Ueda at [57] ("treating HIV infection").
With respect to the negative limitation, that "said composition does
not contain any enzyme inhibitors," Appellants point to the Examiner's
statement that "the prior art 'provides motivation to use each ingredient."'
Reply Br. 2 ( quoting Ans. 10). Appellants argue that this statement
demonstrates that a person of ordinary skill in the art would have been
motivated to use an enzyme inhibitor. Reply Br. 2. We are not persuaded
by this argument. Appellants are taking the Examiner's statement out of
context. The Examiner's statement refers to the ingredients of the claims.
Enzyme inhibitors are not ingredients of the claims.
Further, the Examiner's burden to show a prima facie case of
unpatentability does not require the Examiner to prove that a person of
ordinary skill in the art would not have included enzyme inhibitors; it is
Appellants' burden to show the opposite. Cf Upsher-Smith Labs., Inc. v.
Pamlab, LLC, 412 F.3d 1319, 1322 (Fed. Cir. 2005) ("First, Upsher-Smith
[(Plaintiff-Patent Owner)] argues that the district court erred by placing the
burden on Upsher-Smith to prove that the negative limitation was not found
in the prior art rather than on Pamlab [(Defendant-accused infringer)] to
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Application 14/567,554
prove the presence of the negative limitation in the prior art. The district
court did not so err."). Appellants have not shown why a person of ordinary
skill in the art would have included an enzyme inhibitor.
We affirm Rejection 1.
Rejection 2
The Examiner rejects claims 1-19, 21, and 27 under 35 U.S.C. § 103
as unpatentable over Ueda and Chouinard. Final Act. 8.
Rejection 2 is similar to Rejection 1. Id. at 8-10. More specifically,
the Examiner relies on Ueda in the same manner as in Rejection 1 (id. at 8-
9) and relies on Chouinard teaching the HPMC and silicon dioxide
components. Id. at 9-10 (citing Chouinard 2:22-33, 2:35-37, 3:12-22,
4: 13-20, and 4:58-5:-3). The Examiner concludes that it would have been
obvious to combine the identified teachings of Ueda and Chouinard to form
a pharmaceutical composition within the scope of the claims. Final Act. 10.
Appellants present the same arguments in regard to Rejection 2 as
they do for Rejection 1. Appeal Br. 6-8. As discussed above, those
arguments are not persuasive.
We affirm Rejection 2.
SUMMARY
For the reasons discussed, we affirm the Examiner's rejections of
claims 1-19, 21, and 27.
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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