Ex Parte Ettema et al

Patent Trial and Appeal Board

Apr 29, 2013

11377400 (P.T.A.B. Apr. 29, 2013)

UNITED STATES PATENT AND TRADEMARK OFFICE
__________

BEFORE THE PATENT TRIAL AND APPEAL BOARD
__________

Ex parte GERRIT J. B. ETTEMA, RAYMOND J. H. WESTHEIM,
FAYSAL KALMOUA, KORINDE ANNEMARIE JANSEN, and
FARID ABEDIN DORKOOSH
__________

Appeal 2011-007931
Application 11/377,400
Technology Center 1600
__________

Before DONALD E. ADAMS, ERIC GRIMES, and
GEORGIANNA W. BRADEN, Administrative Patent Judges.

GRIMES, Administrative Patent Judge.

DECISION ON APPEAL
This is an appeal under 35 U.S.C. § 134 involving claims to a
pharmaceutical formulation, which have been rejected for anticipation and
obviousness. We have jurisdiction under 35 U.S.C. § 6(b). We reverse.
STATEMENT OF THE CASE
Claims 1-17 are on appeal. Claim 1 is representative:
1. A pharmaceutical composition in the form of a tablet, comprising 1
to 50 mg of aripiprazole Type II and pharmaceutically acceptable excipients,
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said excipients including (a) one or more polyol fillers, (b) one or more
binders, (c) one or more disintegrants, and (d) a lubricant.

The claims stand rejected as follows:
• Claims 1 and 5 under 35 U.S.C. § 102(e) as anticipated by
Aronhime1 (Answer 3);
• Claims 1-8, 11, 12, and 14 under 35 U.S.C. § 103(a) as obvious
based on Aronhime and Bando2 (Answer 4); and
• Claims 9, 10, 13, and 15-17 under 35 U.S.C. § 103(a) as obvious
based on Aronhime, Bando, and Kothari3 (Answer 4).
All of the rejections on appeal depend on the Examiner’s finding that
the “Form II” aripiprazole disclosed by Aronhime is the same as the “Type
II” aripiprazole recited in the claims (Answer 3-4). The Examiner also finds
that Aronhime discloses tablets containing Form II aripiprazole and the
specific types of excipients recited in claim 1 (id. at 3), or alternatively that
it would have been obvious to formulate tablets containing Form II
aripiprazole and the recited excipients based on the cited references (id. at 4-
5).
Appellants argue that Aronhime recognized that crystalline
aripiprazole Type II was known in the art, and presented its inventive
crystalline “Forms” of aripiprazole, including Form II, as “new, ‘alternate’
crystalline structures” (Appeal Br. 5). Appellants argue that “the inventive

1 Aronhime et al., US 2005/0203299 A1, Sept. 15, 2005.
2 Bando et al, WO 03/026659 A1, Apr. 3, 2003.
3 Kothari et al., US 2002/0076437 A1, June 20, 2002
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Forms of Aronhime were taught to be different from prior art Type I and
Type II polymorphs of aripiprazole” (id.).
We agree with Appellants that a preponderance of the evidence does
not support the Examiner’s finding that Aronhime’s Form II aripiprazole is
the same as the Type II aripiprazole required by the claims. Aronhime states
that the “Proceedings of the 4th Japanese-Korean Symposium on Separation
Technology (Oct. 6-8, 1996) disclosed that aripiprazole anhydride crystals
may exist as Type-I and Type-II crystals” (Aronhime 1, ¶ 5) and that
“[a]lternate crystalline structures possessing the stability and manufacturing
advantages of anhydrous aripiprazole are highly desired” (id. at 1, ¶ 8).
Aronhime discloses that its “invention encompasses anhydrous
aripiprazole crystalline forms which are non-hygroscopic and which
maintain compound stability during storage” (id. at 1, ¶ 9), and that one
“embodiment of the invention encompasses aripiprazole Form II” (id. at 1,
¶ 11). Aronhime specifically claims “[a]n aripiprazole crystalline Form II”
as part of its invention (id. at 13, ¶ 80).
As evidence that Type II and Form II are identical, the Examiner
points to Aronhime’s Figure 2, which shows the powder X-ray diffraction
pattern for Form II (Aronhime 2, ¶ 33), and the Specification’s Figure 1,
which shows the XRPD pattern for Type II (Spec. 5:7). The Examiner finds
that the pattern shown in Aronhime’s Figure 2 is “the exact image of the
claimed Type II aripiprazole image disclosed in the present Figure 1. . . .
Two compounds that have identical X-ray diffraction patterns must be the
same.” (Answer 8.)
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We acknowledge that the patterns shown in Aronhime’s Figure 2 and
the Specification’s Figure 1 are very similar, although it is an exaggeration
to say that they are “identical”: for example, in Aronhime, the peak centered
at about 26.1 is higher than the one centered at about 27.3, while that pattern
is reversed in the Specification’s pattern, and Aronhime’s pattern shows a
single broad peak centered at about 20.0, while the Specification’s pattern
shows a pair of narrow peaks centered at 19.9 and 20.1.
More importantly, however, Aronhime’s disclosure demonstrates that
the Aronhime inventors were aware that Type II aripiprazole had been
disclosed in the prior art (Aronhime 1, ¶ 5). The present Specification cites
the same reference (“Aoki”) as disclosing Type II aripiprazole (Spec. 1:20 to
2:4). The Specification also states that its Figure 1 shows “[a]n example of
an XRPD of the Type II aripiprazole, and which thus substantially
corresponds to the XRPD in Aoki” (id. at 7:9-10).
Thus, the evidence shows that the Aronhime inventors – who can be
presumed to have at least ordinary skill in the relevant art – were aware of
Aoki’s disclosure of Type II aripiprazole, including an XRPD pattern that
substantially corresponds to that of the Specification’s Figure 1, and also
were aware of the XRPD pattern of their own Form II aripiprazole. The
Aronhime inventors nevertheless concluded that Form II was an inventive
contribution to the field; and necessarily, therefore, different from the prior
art Type II. The evidence of record does not support the Examiner’s finding
that a person of ordinary skill in the art would conclude that Aronhime’s
Form II aripiprazole is identical to the prior art Type II aripiprazole based on
their XRPD patterns.
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SUMMARY
We reverse all of the rejections on appeal.

REVERSED

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