Ex Parte Virsik et al

Patent Trials and Appeals Board

Apr 17, 2019

14717639 - (D) (P.T.A.B. Apr. 17, 2019)

UNITED STA TES p A TENT AND TRADEMARK OFFICE
APPLICATION NO. FILING DATE
14/717,639 05/20/2015
20786 7590 04/19/2019
KING & SPALDING
1180 PEACHTREE STREET, NE
ATLANTA, GA 30309-3521
FIRST NAMED INVENTOR
Peter A. Virsik
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.
P233022.US.03 (X-0182
R2)
CONFIRMATION NO.
1037
EXAMINER
DECK, JASON A
ART UNIT PAPER NUMBER
1627
NOTIFICATION DATE DELIVERY MODE
04/19/2019 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):
ATLIPDOCKETING@kslaw.com
PTOL-90A (Rev. 04/07)
UNITED STATES PATENT AND TRADEMARK OFFICE
BEFORE THE PATENT TRIAL AND APPEAL BOARD
Ex parte PETER A. VIRSIK, DAVID J. WUSTOW,
THAMIL ANNAMALAI, and SURESH K. MANTHATI 1
Appeal2017-009546
Application 14/717,639
Technology Center 1600
Before DEBORAH KATZ, JOHN G. NEW, and JOHN E. SCHNEIDER,
Administrative Patent Judges.
SCHNEIDER, Administrative Patent Judge.
DECISION ON APPEAL
This is an appeal2 under 35 U.S.C. § 134(a) from the Examiner's
rejection of claims to compounds for treating multiple sclerosis or psoriasis
1 Appellants identify the Real Party in Interest as Xenoport, Inc. Appeal Br.
3.
2 We have considered and herein refer to the Specification of May 20, 2015
("Spec."); Final Office Action of Jan. 26, 2016 ("Final Act."); Appeal Brief
of Nov. 25, 2016 ("Appeal Br."); Examiner's Answer of May 2, 2017
("Ans."); and Reply Brief June 30, 2017 ("Reply Br."). An oral hearing was
held on Apr. 9, 2019. A copy of the transcript of the hearing will be added
to the file when it becomes available. During the hearing, Appellants
referred to various Power Point slides which refer to various part of the
prosecution history and the references of records. That slide presentation
Appeal2017-009546
Application 14/717,639
that have been rejected as obvious and for obviousness-type double
patenting. We have jurisdiction under 35 U.S.C. § 6(b).
We AFFIRM.
STATEMENT OF THE CASE
Fumaric acid esters have been used to treat psoriasis for many years.
Spec. ,r 3. Oral administration of diemthyl fumarate has shown promising
results in reducing symptoms of multiple sclerosis. Id. ,r 8. Oral
administration of these compounds often results in unwanted side effects
such as serious digestive tract irritation with attendant nausea, vomiting,
abdominal pain and diarrhea. Id. ,r,r 7-8. The specification discloses
"improved methods of treating multiple sclerosis and/or psoriasis in human
patients using fumaric acid esters. The methods are able to achieve high
therapeutic levels of [ methyl hydrogen fumarate] in the blood plasma of a
patient without causing significant gastrointestinal irritation." Id. ,r 10.
Claims 1-15 are on appeal. Claim 1 is the sole independent claim and
reads as follows:
1. (Original) A compound of Formula (I):
/oy~
0
(I)
was used solely as a demonstrative and is not part of the record considered
by the panel.
2
Appeal2017-009546
Application 14/717,639
or a pharmaceutically acceptable salt thereof, wherein:
R1 and R2 are each hydrogen;
R3 and R4 together with the nitrogen to which they are
bonded form a ring chosen from C4-10 heterocycloalkyl and
substituted C4-10 heterocycloalkyl;
n is O; and
X is pair of hydrogen atoms, wherein each hydrogen
atom is connected to the carbon to which it is bonded by a
single bond;
wherein each substituent group is =O.
The claims stand rejected as follows:
Claims 1-15 have been rejected under 35 U.S.C. § I03(a) as
unpatentable over Gangakhedkar3 in view of Sagi. 4
Claims 1-15 have been rejected for non-statutory obviousness-type
double patenting over claims 1-I8ofUS 8,952,006 B2.
Claims 1-15 have been rejected for non-statutory obviousness-type
double patenting over claims 32-36 ofUSSN 13/967,283. 5
DOUBLE PATENTING
Appellants have offered no substantive argument regarding this
rejection other than to ask that it be held in abeyance until allowable subject
matter has been found in the present application. Appeal Br. 17. We
therefore summarily affirm this rejection. 37 C.F.R. 4I.37(c)(iv).
3 Gangakhedkar, et al, WO 2010/02217 A2, published Feb. 25, 2010
("Gangakhedkar").
4 Sagi et al., US 2005/0101779 Al, published May 12, 2005 ("Sagi").
5 USSN 13,967,283 was abandoned on Sept. 6, 2017 rendering this rejection
moot.
3
Appeal2017-009546
Application 14/717,639
OBVIOUSNESS
Issue
The issue with respect to this rejection is whether a preponderance of
the evidence supports the Examiner's conclusion that the subject matter of
the claims would have been obvious over Gangakhedkar combined with
Sagi.
The Examiner finds that Gangakhedkar teaches the use of prodrugs of
methyl hydrogen fumarate to treat multiple sclerosis. Final Act. 3. The
Examiner finds that Gangakhedkar exemplifies fumarate prodrugs having
the following structures:
Id. at 4. The Examiner finds that Gangakhedkar teaches that the use of
prodrugs results in "increased gastrointestinal permeability and absorption,
improved solubility, and minimal cleavage in the gut lumen." Id.
The Examiner finds that Sagi teaches a method for treating multiple
sclerosis using prodrugs with carbonyl masking groups. Id. The Examiner
finds that one of the masking groups used in Sagi is identical to one used in
Gangakhedkar and several others, shown below, have high homology to the
prodrug moieties used in Gangakhedkar.
4
Appeal2017-009546
Application 14/717,639
0
I,.,... .. b.·•· .. · .. . o~ ~
Final Act. 4, citing Sagi 28-29.
The Examiner concludes
It would have been obvious to one of ordinary skill in the
art at the time of filing of the instant invention to make and use
methyl hydrogen fumarate prodrugs with the prodrug moieties
of Sagi et al.
One of ordinary skill would have been motivated to make
and use the instantly claimed compounds because
Gangakhedkar et al. teaches that prodrugs of methyl hydrogen
fumarate offer improved features over methyl hydrogen
fumarate, and teaches the general type of prodrug moieties,
while Sagi et al. discloses additional prodrug moieties for
carboxylate groups that are of the same general type. The
skilled artisan would have used the prodrug moieties of Sagi et
al. for the method of Gangakhedkar et al. during the routine
optimization of the properties of the compounds, and would
have done so with a reasonable expectation of success in
making an improved treatment for multiple sclerosis.
Final Act. 5.
Principles of Law
[T]he examiner bears the initial burden, on review of the
prior art or on any other ground, of presenting a prim a f acie
case ofunpatentability. 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.
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Appeal2017-009546
Application 14/717,639
In re Oetiker, 977 F.2d 1443, 1445 (Fed. Cir. 1992).
"[W]hen a patent claims a structure already known in the prior art that
is altered by the mere substitution of one element for another known in the
field, the combination must do more than yield a predictable result." KSR
Int'! Co. v. Teleflex Inc., 550 U.S. 398,416 (2007), citing United States v.
Adams, 383 U.S. 39, 50-51 (1966).
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 Action and
Answer regarding this rejection. We find the Examiner has established that
the subject matter of the claims would have been obvious to one of ordinary
skill in the art at the time the invention was made over Gangakhedkar
combined with Sagi. Appellants have not produced evidence showing, or
persuasively argued, that the Examiner's determinations on obviousness are
incorrect. Only those arguments made by Appellants in the Briefs have been
considered in this Decision. Arguments not presented in the Briefs are
waived. See 37 C.F.R. § 4I.37(c)(l)(iv) (2015). We have identified claim 1
as representative; therefore, all claims fall with claim 1. We address
Appellants' arguments below.
Appellants contend that the references either alone or in combination
do not teach or suggest the claimed compound. Appeal Br. 7. Appellants
argue that the prodrugs disclosed in Gangakhedkar contain an additional
carbonyl group at the carbon alpha to the nitrogen and Sagi is directed to
prodrugs of phenylalanine derivatives and not methyl hydrogen fumarate.
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Id. Appellants argue that Sagi does not teach or suggest that the masking
moieties disclosed therein can be sued with other drug compositions. Id. at
8.
Appellants also argue that even if one skilled in the art were motivated
to use the prodrug moieties of Sagi with the fumarate of Gangakhedkar, it
would not result in the claimed compound but would produce a compound
with the following structure:
See id. at 10.
We have considered Appellants arguments and are not persuaded that
the Examiner's rejection is in error.
Appellants' arguments about the teachings of the individual references
is not persuasive as it is the combined teachings of the references that serves
as the basis for this rejection. "Non-obviousness cannot be established by
attacking references individually where the rejection is based upon the
teachings of a combination of references. . . . [The reference] must be read,
not in isolation, but for what it fairly teaches in combination with the prior
art as a whole." In re Merck & Co., 800 F.2d 1091, 1097 (Fed. Cir. 1986).
Gangakhedkar teaches the preparation of prodrugs of methyl
hydrogen fumarate and the benefits of such prodrugs. Gangakhedkar, 3--4.
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Both Gangakhedkar and Sagi teach the use of carboxyl masking groups
including those which are structurally the same or similar. Compare,
Gangakhedkar, 63, example 3 and 65, example 9 with Sagi, 28-29, Table A.
It is prima facie obvious to substitute structurally similar compounds where
there is evidence that the compounds share similar properties. In re Dillon,
919 F.2d 688, 691 (Fed. Cir. 1990). Given the teaching of the use of the
same or structurally similar prodrug moieties, we agree with the Examiner
that "[t]he skilled artisan would have understood that the carbonyl masking
utility espoused by Sagi et al. for the taught prodrug moieties could be
successfully used with additional carboxylates, including those of
Gangakhedkar et al." Ans. 9-10.
The lack of any teaching in Sagi that the prodrug moieties disclosed
therein can be used for other active compounds does not negate the
combined teachings of the references. As the Examiner points out
Id.
the disclosure of Gangakhedkar et al. is directed to carboxylate
prodrugs of monomethyl fumarate, wherein the carboxylate was
the site of prodrug-moiety functionalization, and Sagi et al.
similarly taught prodrug functionalization of carboxylates. The
skilled artisan would have understood that the carboxylate of
monomethyl fumarate was a beneficial location to append a
prodrug-moiety, and would have used additional prodrug
moieties, including those of Sagi et al.
Appellants' argument that the combination of Gangakhedkar and Sagi
would result in a structure different from what is claimed is also not
persuasive. Appellants offer no evidence, other than attorney argument, to
support their contention that combining monomethyl fumarate with the
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prodrug moieties of Sagi would result in a peroxy-ester or per-ester. See,
Appeal Br. 11-12. "Attorney's argument in a brief cannot take the place of
evidence." In re Pearson, 494 F.2d 1399, 1405 (CCPA 1974).
Appellants contend that one skilled in the art would not have has a
reasonable expectation of success in creating the claimed compound
following the teachings of Gangakhedkar and Sagi. Appeal Br. 15.
Appellants contend that given the structural dissimilarities of the drug cores
of Gangakhedkar and Sagi and the lack of any teaching in Sagi that the
prodrug moieties could be used with other drug cores, one skilled in the art
would not expect the prodrug moieties of Sagi to work with the monomethyl
fumarate of Gangakhedkar. Id. at 15-16.
We are not persuaded by Appellants' argument. "Obviousness does
not require absolute predictability of success .... For obviousness under
§ 103, all that is required is a reasonable expectation of success." In re
O'Farrell, 853 F.2d 894, 903---04 (Fed. Cir. 1988).
We agree with the Examiner that Gangakhedkar and Sagi teach the
use of prodrug moieties to improve the effectiveness of carboxylic-acid-
based drugs. Ans. 16. As discussed above, Gangakhedkar and Sagi teach
the use of the same or structurally similar prodrug moieties. Compare,
Gangakhedkar, 63, example 3 and 65, example 9 with Sagi, 28-29, Table A.
We agree with the Examiner's conclusion that:
The skilled artisan would have been aware of both the
disclosures of Gangakhedkar et al. and Sagi et al., would have
been aware that carboxylate-prodrugs were useful and known,
would have been aware that the prodrug-moieties could be
successfully substituted in the same drug-core, would have been
aware that the prodrug-moieties could be successfully used in
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differing drug-cores, and would have combined the teachings of
the successful use of carboxylate-promoieties and would have
done so with a reasonable expectation of success.
Ans. 16.
Conclusion of Law
We conclude that a preponderance of the evidence supports the
Examiner's conclusion that the subject matter of claim 1 would have been
obvious over Gangakhedkar combined with Sagi.
Claims 2-15 have not been argued separately and therefore fall with
claim 1. 37 C.F.R. § 4I.37(c)(l)(iv).
SUMMARY
We affirm the rejection for non-statutory obviousness-type double
patenting.
We affirm the rejection under 35 U.S.C. § 103(a).
TIME PERIOD FOR 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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