Ex Parte Gaul et al

Board of Patent Appeals and Interferences

Jan 3, 2012

12043311 (B.P.A.I. Jan. 3, 2012)

UNITED STATES PATENT AND TRADEMARK OFFICE
__________

BEFORE THE BOARD OF PATENT APPEALS
AND INTERFERENCES
__________

Ex parte MICHAEL GAUL, ALEXANDER KIM, LILY LEE SEARLE,
DIONISIOS RENTZEPERIS, and GILLES C. BIGNAN
__________

Appeal 2011-008222
Application 12/043,311
Technology Center 1600
__________

Before DEMETRA J. MILLS, LORA M. GREEN, and
STEPHEN WALSH, Administrative Patent Judges.

WALSH, Administrative Patent Judge.

DECISION ON APPEAL
This is a decision on appeal under 35 U.S.C. § 134(a) from the Patent
Examiner’s final rejection of claims 1-5, 7-13, 17, and 35 for obviousness.
We have jurisdiction under 35 U.S.C. § 6(b). We affirm.
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STATEMENT OF THE CASE
The invention relates to compounds said to be useful as estrogen
related receptor modulators. (Spec. 1, ll. 15-18.) Claim 1 is representative
and it defines a genus of compounds of Formula (I):

wherein X and R1 through R6 have meanings listed in the claim.
The Examiner rejected claims 1-5, 7-13, 17, and 35 under 35 U.S.C.
§ 103(a) as unpatentable over Player et al., US 2006/0014812 A1, published
Jan. 19, 2006.
Appellants state that claims 2-5, 7-13, 17, and 35 will stand or fall
with claim 1. (App. Br. 8.)
OBVIOUSNESS
The Issue
The Examiner’s position is that Player described compounds and
pharmaceutical compositions that were useful as estrogen related receptor
modulators. (Ans. 4.) The Examiner found that (i) the compound shown in
Player’s Example 8 had high bioactivity at low concentrations (id., citing
Player’s Table 1), and (ii) Appellants claim a position isomer of Player’s
Example 8 compound, that is, Appellants’ compounds have a –CF3 group at
the 3rd position in the phenyl ring rather than at the 2nd position as Player’s
Example 8 compound has it (id. at 5). The Examiner found that an “artisan
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interested in such receptors would have found Example 8 compound to be an
appropriate lead on the basis of its known biological activity.” (Id. at 6.)
According to the Examiner, “[i]t is well established that position isomers are
prima facie structurally obvious even in the absence of a teaching to modify”
(id. at 5), and the Examiner reasoned that “[o]nce the artisan identified
[Example 8] as a suitable lead compound, its position isomers and homologs
would have been obvious variants” (id. at 6).
Appellants contend that the rejection must be reversed because it
failed to satisfy two conditions purportedly set out in Takeda Chemical Ind.
Ltd. v. Alphapharma Pty., Ltd., 492 F.3d 1350 (Fed. Cir. 2007). (App. Br.
4.) Specifically, Appellants contend:
the court stated that two conditions must be met for a position isomer
of a prior art compound to be considered obvious. The first condition
is that a person of ordinary skill in the art would have selected the
prior art compound (here the Example 8 compound) as a lead
compound. Id., 429 F.3d at 1357. The second condition is that the
prior art must suggest making the specific molecular modifications to
the lead compound that are necessary to arrive at the claimed
compound. Id., 429 F.3d at 1360.

(Id.)
The issues Appellants raise on appeal are:
whether the evidence relied upon supports the finding that a person of
ordinary skill would have selected Player’s Example 8 compound as a lead
compound; and
whether the evidence is sufficient to show that the prior art suggested
the positional isomer of Player’s Example 8 compound with a –CF3 group at
the 3rd position in the phenyl ring rather than the 2nd position.
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Findings of Fact
1. We adopt the Examiner’s findings concerning the scope and content
of the prior art.
2. Player’s Example 8 compound has the following formula:

(Player 15, [0175] (circle added at position 3 of the phenyl ring.)
3. Player’s Table 1 reads, in part:

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(Id. at 22.)
Analysis
Because Appellants stress the importance of the Takeda case to this
appeal, we begin with a discussion of that case. In Takeda, Alphapharm
contended that Takeda’s patent claim on pioglitazone was invalid due to
obviousness. The district court found that Alphapharm failed to prove
obviousness. The Federal Circuit summarized the district court’s action as
follows:
[t]he court first concluded that there was no motivation in the prior art
to select compound b as the lead compound for antidiabetic research,
and that the prior art taught away from its use. As such, the court
concluded that Alphapharm failed to make a prima facie case of
obviousness. The court continued its analysis and found that even if
Alphapharm succeeded in making a prima facie showing, Takeda
would still prevail because any prima facie case of obviousness was
rebutted by the unexpected results of pioglitazone’s nontoxicity.

492 F.3d at 1354.
In its review of specifics pertaining to the lead compound question,
the Federal Circuit approved the district court’s findings that the prior art
description that included Alphapharm’s proposed lead compound
(compound b) “did not disclose experimental data or test results” for
compound b, that “compound b was not identified as one of the three most
favorable compounds,” and that “reliable scientific analysis . . . taught away
from compound b” (it had a toxicity problem), among other findings.
492 F.3d at 1357-58.
On the “lead compound” issue, the facts in Takeda make an inapt
comparison to the evidence here because substantial contrasts are evident.
First, the Examiner here identified evidence that Example 8’s compound had
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a low IC50, and found that the low IC50 would have suggested it as a lead
compound. Player’s Table 1 shows that the compound did have a
comparatively low IC50. (FF 3.) Second, Appellants here simply deny that
the Examiner made that finding rather than offer evidence showing an error
in reliance on the IC50. Third, Appellants here identify no teaching away in
the prior art. Appellants argue that a different Player compound would have
been a better choice as lead compound: Example 12. (App. Br. 6.) We find
this argument unpersuasive for the same reason the Examiner found it
unpersuasive: the ordinary artisan would not have picked just one
compound. (Ans. 9.) See, e.g, Merck & Co., Inc. v. Biocraft Labs., Inc.,
874 F.2d 804, 807 (Fed. Cir. 1989) (holding that the prior art’s disclosure of
a multitude of combinations failed to render any particular formulation less
obvious). Thus, we find the evidence taken as whole supports the finding
that Example 8’s compound would have been seen as a lead compound by
those of ordinary skill in the art. As to the lead compound question, we find
Appellants’ reliance on Takeda misplaced and unpersuasive.
As to the obviousness of positional isomers, the Examiner relied on
the principle that “[i]t is well established that position isomers are prima
facie structurally obvious even in the absence of a teaching to modify. The
isomer is expected to be preparable by the same method and to have
generally the same properties.” (Ans. 5, citing cases.) That settled principle
was not disturbed by the Takeda decision. Indeed the Takeda court referred
to the presumption of motivation for positional isomers:
[b]ecause Alphapharm’s obviousness argument rested entirely on the
court making a preliminary finding that the prior art would have led to
the selection of compound b as the lead compound, and Alphapharm
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failed to prove that assertion, the court did not commit reversible error
by failing to apply a presumption of motivation.

492 F.3d at 1360.
In Takeda, there were facts in evidence that rebutted the presumption:
“the process of modifying lead compound was not routine at the time of the
invention,” 492 F.3d at 1360, and “pioglitazone exhibited unexpectedly
superior properties over the prior art compound b,” 492 F.3d at 1361. Thus,
the court found that “Takeda rebutted any presumed expectation that
compound b and pioglitazone would share similar properties.” 492 F.3d at
1362. Here, in contrast, the Examiner found that “the reference (Player et
al.) teaches the generic claim to include position isomers. The substituents in
the phenyl ring may be at any position, while achieving retention of the
compound’s activity as an EER-alpha receptor modulator. . . . Thus Player
indeed suggests making the claimed changes in the compound structure to
arrive at the claimed position isomer compounds with the expectation of
obtaining compounds for the same use.” (Ans. 7.) That evidence “is
sufficient to show that the claimed and prior art compounds possess a
‘sufficiently close relationship . . . to create an expectation,’ in light of the
totality of the prior art, that the new compound will have ‘similar properties’
to the old.’” Eisai Co. Ltd. v. Dr. Reddy’s Labs., Ltd., 533 F.3d 1353, 1357
(Fed. Cir. 2008) (quoting Aventis Pharma Deutschland GmbH v. Lupin, Ltd.,
499 F.3d 1293, 1301 (Fed. Cir. 2007) (quoting In re Dillon, 919 F.2d 688,
692 (Fed. Cir. 1990))). And in further contrast to the Takeda case,
Appellants here offer no evidence of unexpected results.
Appellants argue it was an error for the Examiner to follow the
MANUAL OF PATENT EXAMINING PROCEDURE (MPEP) instruction on
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positional isomers, which the MPEP describes as “generally of sufficiently
close structural similarity that there is a presumed expectation that such
compounds possess similar properties.” (App. Br. 7, quoting MPEP
§ 2144.09 II, first paragraph.) According to Appellants, the Examiner
should have given more weight to the MPEP’s second paragraph in that
section, which states: “[i]somers having the same empirical formula but
different structures are not necessarily considered equivalent by chemists
skilled in the art and therefore are not necessarily suggestive of each other.”
(Id., quoting the same MPEP section, second paragraph.) This argument is
unpersuasive for the reason the Examiner gave: this case involves position
isomers, not the distinct kind of empirical formula isomer referred to in the
second paragraph. (Ans. 11.) The applicable principle is: “[a] prima facie
case of obviousness may be made when chemical compounds have very
close structural similarities and similar utilities.” (MPEP § 2144.09 I., citing
cases). The evidence here is that Appellants’ compounds have both very
close structural similarities to, and the same utility as Player’s compounds.
Appellants have not rebutted the prima facie case of obviousness.
SUMMARY
We affirm the rejection of claims 1-5, 7-13, 17, and 35 under
35 U.S.C. § 103(a) as unpatentable over Player.

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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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