Ex Parte Baek et al

Patent Trial and Appeal Board

Dec 12, 2017

14060989 (P.T.A.B. Dec. 12, 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.
14/060,989 10/23/2013 Myoung-Ki Baek 16682-000008-US-COB 4383
28997 7590 12/14/2017
HARNESS, DICKEY, & PIERCE, P.L.C
7700 Bonhomme, Suite 400
ST. LOUIS, MO 63105
EXAMINER
IVANOVA, SVETLANA M
ART UNIT PAPER NUMBER
1627
NOTIFICATION DATE DELIVERY MODE
12/14/2017 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):
stldocket@hdp.com
PTOL-90A (Rev. 04/07)
UNITED STATES PATENT AND TRADEMARK OFFICE
BEFORE THE PATENT TRIAL AND APPEAL BOARD
Ex parte MYOUNG-KI BAEK, JAE-HOON JO, and
HYE-JIN CHANG1
Appeal 2016-008224
Application 14/060,989
Technology Center 1600
Before ERIC B. GRIMES, FRANCISCO C. PRATS, and RYAN H. FLAX,
Administrative Patent Judges.
GRIMES, Administrative Patent Judge.
DECISION ON APPEAL
This is an appeal under 35U.S.C. § 134 involving claims to an
anticonvulsive pharmaceutical for transnasal administration, which have
been rejected as obvious. We have jurisdiction under 35 U.S.C. § 6(b).
We reverse.
STATEMENT OF THE CASE
The Specification states that “nasal administration has an advantage in
that drugs may be easily and simply administered to achieve systemic or
1 Appellants identify the Real Party in Interest as SK Biopharmaceuticals
Co., Ltd. (Appeal Br. 3.)
Appeal 2016-008224
Application 14/060,989
topical effects.” (Spec. 14.) However, “drugs such as diazepam and
lorazepam are difficult to be developed into a formulation suitable for nasal
spray administration since they have low solubility in water that is widely
used to dissolve drugs.” {Id. 1 5.) “The nasal absorption of drugs may be
augmented by administering the drugs and a chemical aid or a penetration
enhancer at the same time.” {Id. | 6.)
The Specification discloses
an anticonvulsive pharmaceutical composition, which is nasally
sprayed for the purpose of transnasal administration, [that]
contains as an active component a poorly soluble anticonvulsant
selected from the group consisting of diazepam and lorazepam,
and further include[s] diethylene glycol monoethyl ether and
fatty acid ester, wherein the fatty acid ester is selected from the
group consisting of caprylocaproyl polyoxylglyceride, isopropyl
palmitate, oleoyl polyoxylglyceride, sorbitan monolaurate 20,
methyl laurate, ethyl laurate, and polysorbate 20.
{Id. 128.)
Claims 19—23, 26—32, and 34—36 are on appeal. Claim 19 is the only
independent claim and reads as follows (emphasis added):
19. An anticonvulsive pharmaceutical composition for transnasal
administration, comprising:
about 1% to about 20% by weight of at least one poorly soluble
anticonvulsant,
about 40% to about 60% by weight of diethylene glycol monoethyl
ether, and
at least about 30% by weight of fatty acid ester comprising
caprylocaproyl polyoxylglyceride, isopropyl palmitate and sorbitan
monolaurate 20, and
0% to about 5% by weight of water.
2
Appeal 2016-008224
Application 14/060,989
DISCUSSION
The Examiner has rejected all of the claims on appeal under 35 U.S.C.
§ 103(a) as obvious based on Kim,2 Jamieson,3 Hsu,4 Esposito,5 and
Carrara.6 (Ans. 4.) The Examiner finds that Kim describes “a transnasal
anticonvulsive pharmaceutical composition comprising diazepam as an
active ingredient (from about 0.1 to 10.0% by weight), water, a fatty acid
ester (in an amount of more than about 30% by weight. . .), diethylene
glycol monoethyl ether (from about 30 to 45% by weight), ethanol and
sodium glycocholate.” (Id.)
The Examiner finds that the water content of Kim’s composition is
higher than is recited in claim 19, but Jamieson discloses a transnasal
composition of diazepam that includes only a small amount of water. (Id. at
5.) The Examiner finds that Jamieson discloses transnasal compositions
comprising a benzodiazepine (e.g., diazepam) comprising diethylene glycol
monoethyl ether, another solvent in which the benzodiazepine is less
soluble, and an optional surfactant. (Id. at 5—7.) The Examiner finds that
“Jamieson also discloses formulations with 5-10% water with high stability
if formulated in an aqueous buffer” and concludes that it would have been
obvious “to combine the teachings of Kim and Jamieson in order to arrive at
the optimal amount of water in the formulation.” (Id. at 7—8.)
2 Kim et al. (US 2008/0113970 Al, pub. May 15, 2008).
3 Jamieson et al. (US 2008/0076761 Al, pub. Mar. 27, 2008).
4 Hsu et al. (US 2008/0262445 Al, pub. Oct. 23, 2008)
5 Esposito et al. (US 2002/0034539 Al, pub. Mar. 21, 2002).
6 Carrara et al. (US 2007/0225379 Al, pub. Sept. 27, 2007).
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Appeal 2016-008224
Application 14/060,989
The Examiner finds that Carrara, Hsu, and Esposito disclose that the
specific fatty acid esters recited in claim 19 were known for use in transnasal
or transdermal compositions. {Id. at 9—12.) The Examiner concludes that it
would have been obvious “to modify the invention of Jamieson, such as to
expand the possible penetration enhancers/surfactants in it to include methyl
laurate, caprylocaproyl polyoxylglyceride, isopropyl palmitate, and sorbitan
monolaurate 20, as disclosed in Carrara, Hsu, and Esposito.” {Id. at 12.)
Appellants argue, among other things, that “Jamieson cannot
supplement the missing feature ‘0% to about 5% by weight of water’ of
Claim 19” because “there is only one example containing ‘a fatty acid ester’
with 0% water, and the other examples are directed to a binary solvent
system which are irrelevant to Kim.” (Appeal Br. 9—10.)
We agree with Appellants that the cited references do not support a
prima facie case of obviousness. In particular, the references do not provide
a reason to reduce the water content of Kim’s composition to an amount of
0% to about 5%, as required by the claims. Kim discloses that its
composition contains “diazepam as an active ingredient, water, a fatty acid
ester, diethylene glycol monoethyl ether, ethanol and sodium glycocholate.”
(Kim 117.) Kim teaches that “[t]he sum of water and ethanol is preferably
from about 20 to 30% by weight, based on the total weight of the
composition.” {Id. 122.) Kim states that, “[i]n one preferred embodiment,”
the composition comprises “from about 8% to 12% by weight of water.”
{Id. 124.) Kim characterizes its composition as containing “a minimized
content of water and ethanol.” {Id. 152.)
The Examiner cites Jamieson as a basis for reducing the amount of
water in Kim’s composition to 5% or less, because “Jamieson also discloses
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Appeal 2016-008224
Application 14/060,989
formulations with 5-10% water with high stability if formulated in an
aqueous buffer. ([0199]).” (Ans. 7.) Jamieson discloses, however, that
[f]ormulations containing 5-10% water also demonstrated some
level of clonazepam instability. Thus, the percent clonazepam
dropped to 63-78% in 6 weeks at 60° C. In contrast to the
formulations containing 5-10% water the formulations
containing 10% aqueous buffer at pH 4 demonstrated relatively
high stability. Thus, the assay of those formulations was in the
90% range after 6 weeks of storage at 60° C.
(Jamieson 1199.) Thus, Jamieson discloses that compositions comprising
the benzodiazepine clonazepam were less stable when they contained less
than 10% water, and were more stable when they contained 10% aqueous
buffer. We therefore do not agree with the Examiner that Jamieson would
have led a person of ordinary skill in the art to modify Kim’s composition,
comprising the benzodiazepine diazepam, to contain 0—5% water, as
required by the claims on appeal.
SUMMARY
We reverse the rejection of claims 19-23, 26—32, and 34—36 under 35
U.S.C. § 103(a) based on Kim, Jamieson, Hsu, Esposito, and Carrara.
REVERSED
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