Ex Parte Brigandi et al

Patent Trial and Appeal Board

Apr 3, 2017

12094672 (P.T.A.B. Apr. 3, 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.
12/094,672 05/22/2008 Richard Anthony Brigandi PR61734USw 4348
23347 7590 04/05/2017
GLAXOSMITHKLINE
GLOBAL PATENTS UW2220
709 Swedeland Road
P. O. BOX 1539
KING OF PRUSSIA, PA 19406-0939
EXAMINER
FAY, ZOHREH A
ART UNIT PAPER NUMBER
1621
NOTIFICATION DATE DELIVERY MODE
04/05/2017 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):
laura.m.mccullen@gsk.com
US_cipkop @ gsk. com
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PTOL-90A (Rev. 04/07)
UNITED STATES PATENT AND TRADEMARK OFFICE
BEFORE THE PATENT TRIAL AND APPEAL BOARD
Ex parte RICHARD ANTHONY BRIGANDI, MARK LEVICK, and
WILLIAM HENRY MILLER1
Appeal 2016-004806
Application 12/094,672
Technology Center 1600
Before ERIC B. GRIMES, TAWEN CHANG, and JOHN E. SCHNEIDER,
Administrative Patent Judges.
SCHNEIDER, Administrative Patent Judge.
DECISION ON APPEAL
This is an appeal under 35 U.S.C. § 134 involving claims to a method
for treating ocular neovascular disorders, which have been rejected as
obvious. We have jurisdiction under 35 U.S.C. § 6(b).
We affirm.
STATEMENT OF THE CASE
Neovascularization, also known as angiogenesis, is the process of
forming new blood vessels. Spec. 1. While neovascularization is important
1 Appellants identify the Real Party in Interest as SmithKline Beecham
Corporation. Br. 2.
Appeal 2016-004806
Application 12/094,672
in wound healing, it also plays a role in a number of pathological states
including cancer and diseases of the eye such as age-related macular
degeneration (AMD). Id. The present invention is directed to a method for
treating ocular neovascular disorders by administering an effective amount
of pyrimidine derivatives. Spec. 2.
Claims 1—3, 6, 8, 9, 26, 27, 29, 30, 32, 33, 35, 36, and 38 are on
appeal. Claim 1 is representative of the rejected claims and reads as follows:
1. A method of healing or ameliorating a symptom or side effect
of an ocular neovascular disorder in a mammal or decreasing
the rate of advancement of an ocular neovascular disorder in a
mammal, said method comprising administering to said
mammal an effective amount of a compound of formula (I):
or a salt thereof wherein said compound is administered by
topical administration to the eye.
2
Appeal 2016-004806
Application 12/094,672
Claims 1—3, 6, 8, 9, 26, 27, 29, 30, 32, 33, 35, 36, and 38 stand
rejected under 35 U.S.C. § 103(a) as unpatentable over Boloor2 in view of
Shams3 as evidenced by Bingaman.4
DISCUSSION
Issue
The issue is whether a preponderance of evidence supports the
Examiner’s finding that claims 1—3, 6, 8, 9, 26, 27, 29, 30, 32, 33, 35, 36,
and 38 would have been obvious over Boloor combined with Shams as
evidenced by Bingaman.
The Examiner finds that Boloor teaches treating a disorder “mediated
by inappropriate VEGFR2 (vascular endothelial growth factor-2) activity,”
by administering a therapeutically effective amount of a VEGFR2 inhibitor
such as 5-({4-[(2,3-dimethyl-2H-indazol-6-yl)(methyl)amino]]pyrimidin-2-
yl}amino)-2-methylbenzenesulfonamide (i.e., the compound of formula (I)).
Final Act. 3. The Examiner finds that Boloor teaches topical administration
of the compound, specifically in the form of eye drops for ocular
application. Id. at 4. The Examiner finds that Boloor teaches the use of the
composition for treatment of diseases characterized by neovascularization.
Id. The Examiner finds that while Boloor does not teach treatment of
exudative AMD, Shams teaches treatment of exudative AMD using a VEGF
2 Boloor et al., WO 02/059110 Al, published Aug. 1, 2002 (“Boloor”).
3 Naveed Shams, US 2007/0190058 Al, published Aug. 16, 2007
(“Shams”).
4 Bingaman et al., US 2003/0207941 Al, published Nov. 6, 2003
(Bingaman”).
3
Appeal 2016-004806
Application 12/094,672
(vascular endothelial growth factor) antagonist. Final Act. 4—5. The
Examiner concludes that
a skilled artisan, at the time of the invention, would have
construed the method of healing or ameliorating a symptom or
side effect of an ocular neovascular disorder, e.g., exudative
age-related macular degeneration, by administering 5-({4-[(2,3-
dimethyl-2H-indazol-6-yl)(methyl)amino]]pyrimidin-2-
yl}amino)-2- methylbenzenesulfonamide topically, as disclosed
by Boloor et al., in view of Shams, as evidenced by Bingaman
et al. One of ordinary skill in the art would have been
motivated to combine the teachings of the aforementioned
references when seeking new methods of administering
therapeutic compounds having increased effectiveness on
disorders associated with neo-vascularization. It would have
been obvious to one of ordinary skill in the art, at the time of
the invention, because the combined teachings of the prior art
are suggestive of the claimed invention.
Final Act. 5.
Appellants contend that Boloor contains a long list of potential
compounds and possible methods of administration and that there is nothing
in Boloor which would lead on skilled in the art to use the claimed
compound in a topical formulation for administration to the eye. Br. 9—10.
Appellants argue that the Examiner engaged in inappropriate hindsight in
selecting the claimed compound. Id. at 11. Appellants argue that while
Shams teaches the treatment of ocular neovascular disorders with VEGF
antagonists, there is no teaching to use small molecules such as the claimed
compound. Id. Appellants also argue that one skilled in the art reading
Shams would not use a topical application of the compound. Id.
4
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Application 12/094,672
Findings of Fact
We adopt as our own the Examiner’s findings and analysis. The
following findings are included for emphasis and reference convenience.
FF1. Boloor teaches that “[cjentral to the process of angiogenesis are
vascular endothelial growth factor (VEGF) and its receptors, termed
vascular endothelial growth factor receptor(s) (VEGFRs).” Boloor 2,11. 2—
3.5
FF2. Boloor teaches that “antagonism of the VEGFR[-]2 kinase
domain would block phosphorylation of tyrosine residues and serve[s] to
disrupt initiation of angiogenesis.” Boloor 3,11. 2—3.
FF3. Boloor discloses “novel pyrimidine derivative compounds,
which are inhibitors of VEGFR-2 kinase activity.” Boloor 3,11. 10—11
FF4. 5-({4-[(2,3-dimethyl-2H-indazol-6-
yl)(methyl)amino]pyrimidin-2-yl}amino)-2-methylbenzenesulfonamide is
one of the pyrimidine derivatives disclosed in Boloor. Boloor 29,11. 25—26.
FF5. Example 69 of Boloor discloses the synthesis of 5-({4-[(2,3-
dimethyl-2H-indazol-6-yl)(methyl)amino]pyrimidin-2-yl}amino)-2-
methylbenzenesulfonamide, which has the following structure:
5 We note that two sets of page numbers appear on the copy of Boloor
reference in the record. We use the page numbers appearing at the top of
each page in this opinion.
5
Appeal 2016-004806
Application 12/094,672
Boloor 95,11.7-23.
FF6. Table 1 of Boloor shows the effectiveness of 5-({4-[(2,3-
dimethyl-2H-indazol-6-yl)(methyl)amino]pyrimidin-2-yl}amino)-2-
methylbenzenesulfonamide in inhibiting angiogenesis relative to other
pyrimidine derivatives. Boloor 105—107.
FF7. Boloor teaches that the pyrimidine derivatives can be applied
topically to the eye using eye drops. Boloor 35,11. 1—3.
FF8. Shams teaches a method of treating intraocular neovascular
diseases using a VEGF antagonist. Shams Abstract.
FF9. AMD is among the disorders which can be treated using the
method of Shams. Shams H 12 and 72.
FF10. Shams teaches that the VEGF antagonist may comprise “small
molecule inhibitors of the VEGFR tyrosine kinases.” Shams 128.
FF11. The compositions of Shams may be applied topically. Shams 1
92.
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Application 12/094,672
Principles of Law
The test of obviousness is “whether the teachings of the prior art,
taken as a whole, would have made obvious the claimed invention.” In re
Gorman, 933 F.2d 982, 986 (Fed. Cir. 1991).
“The combination of familiar elements according to known methods
is likely to be obvious when it does no more than yield predictable results.”
KSR Inti Co. v. Teleflex Inc., 550 U.S. 398, 416 (2007). “[W]hen the
question is whether a patent claiming the combination of elements of prior
art is obvious,” the answer depends on “whether the improvement is more
than the predictable use of prior art elements according to their established
functions.” Mat417.
Picking one of a finite number of known solutions to a known
problem is obvious. Id. at 421:
When there is a design need or market pressure to solve a
problem and there are a finite number of identified, predictable
solutions, a person of ordinary skill has good reason to pursue
the known options within his or her technical grasp. If this
leads to the anticipated success, it is likely the product not of
innovation but of ordinary skill and common sense. In that
instance the fact that a combination was obvious to try might
show that it was obvious under § 103.
Any judgment on obviousness is in a sense necessarily a
reconstruction based upon hindsight reasoning, but so long as it
takes into account only knowledge which was within the level
of ordinary skill at the time the claimed invention was made
and does not include knowledge gleaned only from applicant’s
disclosure, such a reconstruction is proper.
In re McLaughlin, 443 F.2d 1392, 1395 (CCPA 1971).
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Application 12/094,672
Analysis
Claim 1 is representative of the rejected claims and is set forth above.
We agree with the Examiner’s finding that the subject matter of claim
1 would have been obvious to one skilled in the art at the time the invention
was made. Boloor teaches the use of pyrimidine derivatives including 5-
({4- [ (2,3 -dimethyl-2H-indazol- 6-yl)(methyl)amino]pyrimidin-2 -yl} amino)-
2-methylbenzenesulfonamide as VEGFR-2 antagonists. FF1 4. Shams
teaches the use of VEGF antagonists to treat ocular neovascular disorders
such as AMD. FF8—9. We agree with the Examiner that it would have been
obvious to substitute the VEGF antagonist of Boloor for the antagonist in
Shams. Ans. 8.
Appellants contend that there is nothing in Boloor to suggest the use
of the specific pyrimidine derivative recited in the claims. Br. 9—10. We are
unpersuaded. As the Examiner points out, 5-({4-[(2,3-dimethyl-2H-indazol-
6- yl)(methyl)amino]pyrimidin-2-yl} amino)-2-methylbenzenesulfonamide is
specifically discussed in Example 69 of Boloor. Ans. 7, FF5. In addition,
the claimed compound is also listed in Boloor as one of the more effective
pyrimidine derivatives. FF6. Finally, the group of pyrimidine derivatives is
finite and it is well within the ability of one skilled in the art to determine
which compounds would be effective. KSR Int 7 Co., 550 U.S. at 421.
We are also unpersuaded by Appellants’ contention that neither
Boloor nor Shams would lead one to create a composition for topical
treatment. Br. 10. As the Examiner points out, Boloor specifically teaches
topical application to the eye. Ans. 7. In addition, Shams teaches topical
application of VEGF antagonists. FF11.
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Application 12/094,672
Appellants contend that Shams does not teach the use of small
molecules or the treatment of ocular neovascular disorders. Br. 11. Again
we are unpersuaded. Shams specifically teaches the use of small molecule
inhibitors of VEGFR tyrosine kinases such as the compound recited in the
claims. SeeFFlO.
With respect to Appellants’ argument regarding the improper use of
hindsight, we find no evidence in the record that the Examiner based the
rejection on anything gleaned from Appellants’ disclosure. Rather we find
that the Examiner has relied upon only such information that was available
to one skilled in the art at the time the invention was made. In re
McLaughlin, 443 F.2d at 1395.
Conclusion of Law
We conclude that a preponderance of the evidence supports the
Examiner’s finding that claim 1 would have been obvious over Boloor
combined with Shams as evidenced by Bingaman under 35 U.S.C. § 103(a).
Claims 2, 3, 6, 8, 9, 26, 27, 29, 30, 32, 33, 35, 36, and 38 have not
been argued separately and therefore fall with claim 1. 37 C.F.R.
§ 41.37(c)(l)(iv).
SUMMARY
We affirm the rejection under 35 U.S.C. § 103(a).
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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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