pSivida US.Inc.

Patent Trials and Appeals Board

May 22, 2020

15147198 - (D) (P.T.A.B. May. 22, 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.
15/147,198 05/05/2016 Paul Ashton 047167-171012 1217
24633 7590 05/22/2020
HOGAN LOVELLS US LLP
IP GROUP, COLUMBIA SQUARE
555 THIRTEENTH STREET, N.W.
WASHINGTON, DC 20004
EXAMINER
FAY, ZOHREH A
ART UNIT PAPER NUMBER
1617
NOTIFICATION DATE DELIVERY MODE
05/22/2020 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):
HLUSDocketing@hoganlovells.com
dcptopatent@hoganlovells.com
PTOL-90A (Rev. 04/07)
UNITED STATES PATENT AND TRADEMARK OFFICE
__________

BEFORE THE PATENT TRIAL AND APPEAL BOARD
__________

Ex parte PAUL ASHTON
__________

Appeal 2019-004931
Application1 15/147,198
Technology Center 1600
__________

Before DONALD E. ADAMS, RACHEL H. TOWNSEND, and
JAMIE T. WISZ, Administrative Patent Judges.

TOWNSEND, Administrative Patent Judge.

DECISION ON APPEAL
This is an appeal under 35 U.S.C. § 134 involving claims to an
injectable sustained release composition, which have been rejected as
obvious. We have jurisdiction under 35 U.S.C. § 6(b).
We affirm.
STATEMENT OF THE CASE
“[M]acular degeneration can produce a slow or sudden loss of vision”
and “[a]ge related macular degeneration (“AMD”) is the leading cause of
blindness worldwide.” (Spec. 1) “Two forms of AMD exist: dry AMD and

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 EyePoint
Pharmaceuticals, Inc. (Appeal Br. 1.)
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wet AMD.” (Id.) “[T]reatments for wet AMD exist, such as use of anti-
neovascular agents[, e.g., agents that block the action of vascular endothelial
growth factor (VEGF), thereby slowing angiogenesis,] and photodynamic
therapy (i.e., laser irradiation of the macula).” (Id.) Appellant’s invention is
concerned with compositions that include kinase inhibitors that can be used
to treat macular degeneration. (Id. at 2.)
Claims 1–10 are on appeal. Claim 1 is representative and reads as
follows:
1. An injectable sustained release composition,
comprising a kinase inhibitor dissolved in a water-miscible
organic solvent, wherein:
the concentration of the kinase inhibitor in the
composition is at least 200 μg/mL; and
the concentration of the kinase inhibitor in the
composition is at least 100 times higher than the solubility of
the kinase inhibitor in water at 37°C.
(Appeal Br. 10.)

The prior art relied upon by the Examiner is:
Name Reference Date
Jessen et al. US 2015/0030588 A1 Jan. 29, 2015

The following ground of rejection by the Examiner is before us on
review:2
Claims 1–10 under 35 U.S.C. § 103(a) as unpatentable over Jessen.

2 The Examiner’s rejection of claims 1–10 under 35 U.S.C. § 112, first
paragraph as lacking an adequate written description made in the Final
Action is deemed to have been withdrawn by the Examiner in light of the
Answer, which indicates that only the 103 rejection over Jesse is “applicable
to the appealed claims.” (Ans. 3.)
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DISCUSSION
The Examiner finds that Jessen teaches a sustained release formula of
protein kinase inhibitors. (Final Action 5.) The Examiner also finds that
Jessen teaches (a) the use of the claimed compounds for treating macular
degeneration, (b) liquid formulations, and (c) employing intravitreal or
intraocular injection for treating ophthalmic condition. (Id. (citing Jessen
¶¶ 242 and 247 (macular degeneration); id. ¶ 536 (intravitreal or intraocular
injection for ophthalmic condition); id. ¶ 504 (liquid composition).) The
Examiner finds that the concentration of inhibitor claimed is taught by
Jessen, as is the use of the claimed solvents/solubilizers, such as alcohols.
(Final Action 5; Ans. 5 (indicating that “the concentration of 200 μg/ml [of
the kinase inhibitor], falls between the concentrations of 0.0001%, to 50%”
taught in Jessen ¶ 463 and that Jessen ¶ 495 teaches that “the composition
may include a solubilizer to ensure good solubilization, which is especially
important for non-oral compositions, such as the ones used by injection.”).)
In view of the foregoing, the Examiner concludes that it would have been
obvious to one having ordinary skill in the art to use the claimed protein
kinase inhibitors for the treatment of ophthalmic conditions by injection.
(Final Action 5.)
The Examiner acknowledges that Jessen “does not specifically teach[]
the sustained release for administration by injection.” (Ans. 4.) However,
the Examiner concludes that, in light of Jessen teaching a kinase inhibitor,
which is dissolved in water miscible organic solvent such as, ethanol, at the
concentrations that encompass the claimed concentrations, and that those
two components are the same two components required by Appellant’s
claim, Jessen’s composition would function as sustained release just as
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Appellant’s claimed invention would. (Id. at 4–5; see also Final Action 5,
8.) The Examiner also concludes that the function of the composition “such
as the higher solubility in organic solvent in comparison with water is the
expected property of the prior art composition,” which has the same
concentration claimed of the kinase inhibitor and is present with an organic
solvent and solubilizer. (Final Action 8; Ans. 5.)
We determine that the Examiner has established a prima facie case of
obviousness. In particular, we agree with the Examiner that Jessen teaches
the claimed active ingredient, a kinase inhibitor, (see, e.g., Jessen ¶ 17) may
be used in treating macular degeneration (see id.¶¶ 242, 247), and can be
used in treating ophthalmic conditions via injection (id. ¶ 536).
Furthermore, Jessen teaches that the form of the composition for injection
may be a solution of the claimed compound in an appropriate solvent and
that ethanol is a suitable solubilizer for use in a “composition[] for
injection.” (Id. ¶¶ 494, 503–505.)
Regarding the concentration range claimed, “at least 200 μg/mL” and
“at least 100 times higher than the solubility of the kinase inhibitor in water
at 37 ºC,” we find the following. Appellant’s Specification teaches that “the
solubility of many kinase inhibitors in water is about 1 to about 50 μM
(about 0.5 μg/mL to about 25 μg/mL for small molecules with a molecular
weight of 500 AMU).” (Spec. 2.) In other words, many kinase inhibitors
have a very low solubility in water.
Jessen discloses use of inhibitors of platelet-derived growth factor
receptors (PDGFR), such as sorafenib, a compound that also inhibits
vascular endothelial growth factor receptor (VEGFR), present in an alcohol
diluent such as ethanol so as to be able to administer the active as an
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injectable solution. (Jessen ¶ 254 (disclosing specific inhibitors of PDGFR),
¶¶ 494–495, 503–504 (disclosing an alcohol diluent such as ethanol for
injectable solutions).) Appellant’s Specification exemplifies a composition
that is within the scope of the invention that includes sorafenib as the kinase
inhibitor. (Spec. 16.) Thus, we find Jessen teaches the use of a known
protein kinase inhibitor that is poorly soluble in water.
Furthermore, Jessen teaches a wide concentration range of kinase
inhibitors may be employed including greater than 0.0001% and up to 50%
w/v, with many smaller ranges also being disclosed. (Jessen ¶ 463.)
Appellant does not dispute the Examiner’s position that the disclosed
concentration ranges in Jessen for protein kinase inhibitors overlaps the
claimed range. (Appeal Br. 8; Reply Br. 7.) Rather, Appellant argues that
while
Jessen lists many concentration ranges, nowhere does it (or any
other passage in Jessen) teach or suggest that there are some
concentrations that can be used advantageously to cause
particular kinase inhibitors to precipitate, leading to injectable
sustained release formulations.
(Reply Br. 7; accord Appeal Br. 8 (“there is no recognition that with suitable
concentrations (as recited in Applicant’s claims) one can actually arrive at an
injectable formulation that has a sustained release profile.”).) That argument
is concerned with whether Jessen recognized the use of the range of
concentrations in an injectable composition to achieve sustained release.
However, that Jessen does not describe the injectable compositions as being
sustained release does not establish that Jessen’s injectable compositions
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would not have such a functional characteristic.3 In re Baxter Travenol
Labs., 952 F.2d 388, 392 (Fed. Cir. 1991) (“Mere recognition of latent
properties in the prior art does not render nonobvious an otherwise known
invention.”). We address this in more detail below with respect to whether
Appellant has established that the claimed invention achieves an unexpected
result.
Turning back to the concentration limitation per se, we note that
“where there is a range disclosed in the prior art, and the claimed invention
falls within that range, there is a presumption of obviousness.” Iron Grip
Barbell Co. v. USA Sports, Inc., 392 F.3d 1317, 1322 (Fed. Cir. 2004).
Based on Appellant’s argument directed to whether Jessen recognized the
claimed functional requirement that the composition be sustained release, we
conclude that Appellant concedes that Jessen teaches ranges of protein
kinase for use in injectable compositions that overlap the claimed
concentrations. “[T]he existence of overlapping or encompassing ranges
shifts the burden to the applicant to show that his invention would not have
been obvious.” In re Peterson, 315 F.3d 1325, 1330 (Fed. Cir. 2003). The
presumption can be rebutted by demonstrating “unexpected properties in the
range claimed” or by showing that the art teaches away from the claimed

3 We agree with Appellant that Jessen only explicitly mentions sustained
release in connection with oral formulations. (Appeal Br. 7; Jessen ¶¶ 474,
525.) But we do not rely on the Examiner’s finding that Jessen teaches
sustained release oral composition to determine a prima facie case of
obviousness has been established with respect to sustained release injectable
compositions. Thus, we do not find persuasive Appellant’s argument that
the Examiner’s rejection “is based on nothing more than taking portions of
Jessen’s disclosure completely out of context” (Appeal Br. 7.)
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invention. In re Geisler, 116 F.3d 1465, 1469 (Fed. Cir. 1997). We
conclude Appellant has done neither for the reasons that follow.
No evidence establishing unexpected properties compared to Jessen
Appellant has not demonstrated that sustained release from an
injectable solution suggested by Jessen is an unexpected property in the
broad concentration range claimed.
Appellant’s Specification teaches sustained release is a natural
function of the general low solubility of protein kinase inhibitors in water
and their presence in a diluent such as ethanol. Appellant’s Specification
explains “limited solubility in water is a key factor in achieving extended
release.” (Spec. 5.) Appellant’s Specification discloses that as water
infiltrates the solution of kinase inhibitor dissolved in organic solvent that is
miscible with water, after it is injected, the kinase inhibitor precipitates from
the solution and the water dissolves the kinase inhibitor “to provide
sustained release” of that inhibitor. (Id. at 2.) Thus, because the teachings
of Jessen would have made it obvious to one of ordinary skill in the art to
dissolve a protein kinase inhibitor, such as those recited in the dependent
claims (see, e.g., Jessen ¶ 254 (disclosing use of inhibitors of platelet-
derived growth factor receptors (PDGFR), such as sorafenib, that also
inhibits vascular endothelial growth factor receptor (VEGFR)), in an alcohol
diluent such as ethanol in up to 50% w/v (see id. ¶¶ 463, 494–495, 503–
504), we determine there is sufficient evidence of record to establish a prima
facie case that the sustained release requirement of the claim is met.
“Where . . . the claimed and prior art products are identical or
substantially identical . . . the PTO can require an applicant to prove that the
prior art products do not necessarily or inherently possess the characteristics
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of his claimed product.” In re Best, 562 F.2d 1252, 1254–55, (CCPA 1977).
This is true even where the rejection is one premised on obviousness. Id.
(“Whether the rejection is based on ‘inherency’ under 35 U.S.C. § 102, on
‘prima facie obviousness’ under 35 U.S.C. § 103, jointly or alternatively, the
burden of proof is the same, and its fairness is evidenced by the PTO’s
inability to manufacture products or to obtain and compare prior art
products.”). Appellant has not demonstrated that there are concentrations
disclosed in Jessen that do not result in sustained release injectable solutions
of protein kinase dissolved in alcohol. Thus, we do not find the Examiner’s
position that the sustained release characteristic is an inherent property of the
range of compositions suggested by Jessen has been proven to be erroneous.
Jessen does not teach away from the claimed invention
We also do not find persuasive Appellant’s argument that Jessen
teaches away from the claimed invention because it teaches “that one should
use solubilizers to prevent precipitation” (Reply Br. 7). We understand the
suggestion that precipitation should be prevented in Jessen to be with respect
to “minimiz[ing] precipitation of the compound” out of solution prior to
injection. (See Jessen ¶ 494 (quoted by Appellant at Reply Br. 7).) In
particular, the paragraph relied upon by Appellant teaches the use of a
solubilizer that minimizes precipitation is also “to ensure good solubilization
and/or dissolution of the compound,” both of which are said to be
“especially important for compositions for non-oral use, e.g., compositions
for injection.” (Jessen ¶ 494.) Such is consistent with the later discussion in
the paragraph that the solubilizer is used to “maintain the composition as a
stable or homogeneous solution or dispersion” (id.) and further noting, in a
separate paragraph, the importance of maintaining “the proper fluidity” of
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injectable solutions (id. ¶ 504). Avoiding such precipitation is common
knowledge in the medicinal and formulation arts to ensure that the dosage
amount provided to the patient is the amount indicated to be in the
formulation. Appellant does not provide evidence that one of ordinary skill
in the art would interpret Jessen’s discussion of minimizing precipitation in a
solution passage otherwise; instead, there is only attorney argument.
“Attorneys’ argument is no substitute for evidence.” Johnston v. IVAC
Corp., 885 F.2d 1574, 1581 (Fed. Cir. 1989).
Consequently, we conclude that Appellant has not rebutted the
Examiner’s prima facie case of obviousness.
Claims 2–10 have not been argued separately from claim 1. (Appeal
Br. 8 (“Applicant respectfully submits that these [dependent] claims are
allowable at least for depending from an allowable independent claim.”).)
Consequently, these claims fall with claim 1. 37 C.F.R.
§ 41.37(c)(1)(iv)(2018).
For the reasons discussed above, we affirm the Examiner’s rejection
of claims 1–10 as being obvious over Jessen.
DECISION SUMMARY
In summary:
Claims
Rejected
35 U.S.C.
§
Reference(s)/Basis Affirmed Reversed
1–10 103 Jessen 1–10

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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). See 37 C.F.R.
§ 1.136(a)(1)(iv).
AFFIRMED