Ex Parte Schueckler

Board of Patent Appeals and Interferences

Sep 21, 2011

11212907 (B.P.A.I. Sep. 21, 2011)

UNITED STATES PATENT AND TRADEMARK OFFICE
____________

BEFORE THE BOARD OF PATENT APPEALS
AND INTERFERENCES
____________

Ex parte FRITZ SCHUECKLER
____________

Appeal 2010-012385
Application 11/212,907
Technology Center 1600
____________

Before TONI R. SCHEINER, DONALD E. ADAMS, and JEFFREY N.
FREDMAN, Administrative Patent Judges.

ADAMS, Administrative Patent Judge.

DECISION ON APPEAL
This appeal under 35 U.S.C. § 134 involves claims 1-8, 12-14, 17-23,
and 25-31 (App. Br. 2).
1
Claims 9-11, 15, 16, 24, 32, 33, 37, 41, and 42 are
withdrawn from consideration (id.). We have jurisdiction under 35 U.S.C.
§ 6(b).
STATEMENT OF THE CASE
The claims are directed to a composition (claims 1-8, 12-14, 17-22,
28, 34-36, and 38-40); process for preparation of a solid dispersion (claims

1
Appellant includes claims 34-36 and 38-40 in their statement of the claims
on appeal (App. Br. 2). These claims are free from rejection. Accordingly,
we have not included these claims in our deliberation.
Appeal 2010-012385
Application 11/212,907

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23, 25-27); and a method for treatment of hyper-proliferative disorders,
including cancer (claims 29-31). Claims 1 and 28 are representative and are
reproduced in the “APPENDIX OF CLAIMS ON APPEAL” (App. Br. 10
and 12).
Claims 1-8, 12-14, 17-23, and 25-31 stand rejected under 35 U.S.C. §
103(a) as unpatentable over the combination of Lyons,
2
Serajuddin,
3
and
Onyx.
4

We affirm.
ISSUE
Does the preponderance of evidence on this record support a
conclusion of obviousness?
FACTUAL FINDINGS
FF 1. Lyons teaches the use of 4{4-[3-(4-chloro-3-trifluoromethylphenyl)-
ureido]-phenoxy}-pyridine-2-carboxylic acid methyl amide (BAY 43-9006)
to treat cancer (Ans. 5).
FF 2. Onyx teaches that a Phase I Clinical Trial confirmed the antitumor
activity of BAY 43-9006 in human patients (Ans. 6).
FF 3. Lyons teaches compositions comprising BAY 43-9006 and PVP “in
the form of suspensions or dispersions” (Ans. 5).

2
Lyons et al., US 2003/0125359 A1, published July 3, 2003.
3
Abu T. M. Serajuddin, Solid Dispersion of Poorly Water-Soluble Drugs:
Early Promises, Subsequent Problems, and Recent Breakthroughs, 88(10)
J. Pharma. Sci. 1058-1066 (1999).
4
Onyx Pharmaceuticals, NOVEL RAF KINASE INHIBITOR BAY 43-9006
SHOWS EARLY SIGNS OF TOLERABILITY AND ACTIVITY IN PHASE 1B
COMBINATION TRIALS REPORTED AT ASCO, http://
www.onyx-pharm.com/wt/page/pr_1104881222, accessed November 8,
2007.
Appeal 2010-012385
Application 11/212,907

3
FF 4. Lyons does not teach a solid dispersion comprising BAY 43-9006
and PVP (id.).
FF 5. “Serajuddin teaches that solid dispersions provide enhancement of
bioavailability of poorly water soluble drugs” (id.).
FF 6. Serajuddin teaches “that solvent evaporation is a commonly used
method of preparing solid dispersions” (id.).
FF 7. Serajuddin teaches “that PVP is a commonly used carrier in solid
dispersions produced by the solvent evaporation method” (id. at. 6).
FF 8. Leuner5 suggests that PVP is soluble “in a wide variety of organic
solvents, they are particularly suitable for the preparation of solid
dispersions by the solvent method” (Leuner 53: col. 2, ll. 16-19).
ANALYSIS
Based on the combined teachings of Lyons, Serajuddin, and Onyx the
Examiner concludes that at the time of Appellant’s claimed invention, since
“BAY 43-9006 has been found to be effective in treating cancer,” it would
have been prima facie obvious to formulate a composition comprising BAY
43-9006 and PVP into a solid dispersion to “enhance the bioavailability of
the drug and therefore enhance treatment” (Ans. 6). We find no error in the
Examiner’s prima facie case of obviousness.
Appellant provides separate arguments for the following groups of
claims: I. Claims 1-8, 12-14, 17-23, and 25-27; and II. Claims 28-31.
Claims 1 and 28 are representative. 37 C.F.R. § 41.37(c)(1)(vii).

5
Christian Leuner et al., Improving drug solubility for oral delivery using
solid dispersions, 50 European Jour. of Pharm. and Biopharm., 47-60
(2000).
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Claim 1:
Since Serajuddin suggests that solid dispersions enhance the
bioavailability of pharmaceuticals and that PVP is a commonly used carrier
in solid dispersions, we are not persuaded by Appellant’s contention that
there is no showing that a person of ordinary skill in this art would have
reasonably predicted that BAY 43-9006 could have been formulated as a
solid dispersion (App. Br. 5;
6
Reply Br. 2; Cf. 5 and 7). To the contrary, we
find that a person of ordinary skill in this art looking to enhance the
bioavailability of BAY 43-9006 would have reasonably expected that BAY
43-9006 could be formulated as a solid dispersant using PVP, the carrier
commonly used for this purpose (FF 5 and 7).
We are not persuaded by Appellant’s contention that the evidence on
this record fails to suggest that BAY 43-9006 and PVP would be soluble in
the same solvent, which as suggested by Leuner is a requirement for the
solution method of formulating a solid dispersion (App. Br. 6; see also
Reply Br. 3-4). Leuner teaches that since PVP is soluble “in a wide variety
of organic solvents, they are particularly suitable for the preparation of solid
dispersions by the solvent method” (FF 8). Appellant fails to provide an
evidentiary basis to support his contention that a person of ordinary skill in
this art would not have expected BAY 43-9006 to be soluble in any of the
“wide variety of organic solvents” in which PVP was known to be soluble
(see id.).
Because the combination of references relied upon suggest the use of
a BAY 43-9006 -PVP solid dispersant prepared by the solvent method we

6
All references to Appellant’s Appeal Brief (App. Br.) refer to Appellant’s
Amended Brief on Appeal, entered into the record on January 22, 2010.
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are not persuaded by Appellant’s contentions regarding the hot melt method
of formulating a solid dispersant (see App. Br. 6; Cf. 6-7).
We are not persuaded by Appellant’s contention that Craig
7
confirms
“[t]he unpredictability in forming solid dispersions of pharmaceuticals”
(App. Br. 6). As the Examiner explains, contrary to Appellant’s contention,
Craig suggests that the manufacturing methods for forming solid dispersions
of pharmaceuticals are not only predictable, they are indeed simplistic (Ans.
9-10). Accordingly, we are not persuaded by Appellant’s contention that the
evidence relied upon by the Examiner fails to establish that a person of
ordinary skill in this art would have reasonably expected success in
preparing a solid dispersion with the BAY 43-9006 compound and PVP
(App. Br. 7; see also Reply Br. 5 (“There is nothing in the teachings of Craig
which suggests [that] one of ordinary skill in the art would have an
expectation of success in manufacturing solid dispersions”)).

Claim 28:
Appellant contends that “[a]lthough solid dispersions were known to
have tremendous potential to improve drug solubility, the state of the art at
the time of the invention provided no suggestion or direction that if a solid
dispersion of” BAY 43-9006 “could be formed, it would be one which
would provide improvements in solubility or bioavailability over known
dosage forms” (App. Br. 8). We are not persuaded. Claim 28 does not
require the solid dispersion to exhibit improvements in solubility or
bioavailability over known dosage forms (see Claim 28).

7
Duncan Q.M. Craig, The mechanisms of drug release from solid
dispersions in water-soluble polymers, 231 Int. J. Pharma. 131-144 (2002).
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Application 11/212,907

6
Further, since claim 28 does not require any particular release rate or
ratio of BAY 43-9006:PVP, we are not persuaded by Appellant’s
contentions regarding the release/dissolution rate of the solid dispersion set
forth in claim 28 (id.; Cf. Reply Br. 2 and 5). While Appellant contends that
Example 2 of their Specification “is representative of the subject matter
claimed,” Appellant fails to establish that Example 2 is commensurate with
the full scope of claim 28 (Reply Br. 5).
CONCLUSION OF LAW
The preponderance of evidence on this record supports a conclusion
of obviousness. The rejection of claims 1 and 28 under 35 U.S.C. § 103(a)
as unpatentable over the combination of Lyons, Serajuddin, and Onyx is
affirmed. Because they are not separately argued claims 2-8, 12-14, 17-23,
and 25-27 fall together with claim 1; and claims 29-31 fall together with
claim 28. 37 C.F.R. § 41.37(c)(1)(vii).

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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