Ex Parte Drasner et al

Board of Patent Appeals and Interferences

Jun 29, 2010

10174055 (B.P.A.I. Jun. 29, 2010)

UNITED STATES PATENT AND TRADEMARK OFFICE
__________

BEFORE THE BOARD OF PATENT APPEALS
AND INTERFERENCES
__________

Ex parte KENNETH DRASNER and KEVIN T. WEBER
__________

Appeal 2009-012791
Application 10/174,055
Technology Center 1600
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Decided: June 30, 2010
__________

Before LORA M. GREEN, FRANCISCO C. PRATS, and
MELANIE L. McCOLLUM, Administrative Patent Judges.

Opinion for the Board filed by Administrative Patent Judge PRATS.

Concurring Opinion filed by Administrative Patent Judge McCOLLUM.

PRATS, Administrative Patent Judge.

DECISION ON APPEAL
This appeal under 35 U.S.C. § 134 involves claims to a method for
blocking voltage sensitive sodium channels of neuronal cells in a
mammalian subject. The Examiner rejected the claims as obvious.
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We have jurisdiction under 35 U.S.C. § 6(b). We reverse.

STATEMENT OF THE CASE
Claim 96, the only pending claim, reads as follows:
96 A method for blocking voltage-sensitive sodium
channels of neuronal in a mammalian subject in need of
blockage of voltage-sensitive channels of neuronal
mammalian cells comprising administering to said
subject an effective amount of a compound of the
formula

in which
R1 is 4-chlorophenoxymethyl;
R2 is benzyl and R4 is H or a pharmaceutically
acceptable salt thereof.

The sole rejection before us for review is the Examiner’s rejection of
claim 96 as obvious under 35 U.S.C. § 103(a) in view of Goto1 and Berger2
(Ans. 3-5).
OBVIOUSNESS
ISSUE
The Examiner cites Goto as teaching “a compound of formula 1 as an
anti-diabetic agent in rats,” but concedes that “Goto et al. fail to disclose a

1 JP 2002-155060 (published May 28, 2002) (as translated).
2 U.S. Patent No. 5,688,830 (filed Nov. 18, 1997).
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single embodiment of the compound according to claim 96 nor the
relationship with voltage-gated sodium channel blockers” (Ans. 4). The
Examiner finds, however, that “Berger et al. teach that voltage-gated sodium
channel blockers are used to treat diabetic neuropathy” (id.).
Based on the references’ teachings, the Examiner reasons:
A person of ordinary skill in the art would have been
motivated to formulate a compound according to claim 96 to
block a voltage-sensitive sodium channels because: (1) Goto et
al. teach the genus of the compound in claim 96; (2) Goto et al.
teach the use of the compound as an antidiabetic agent; and (3)
Berger et al. teach that voltage-gated sodium channel blockers
are used to treat diabetic neuropathy. Therefore, one of
ordinary skill in the art would have had a reasonable
expectation of success in treating diabetic neuropathy by
blocking voltage-gated sodium channels in a mammal by
administering a compound according to claim 96.

(Id. at 4-5.)

Appellants contend that “[t]he prior art reference (or references when
combined) must teach or suggest all the claim limitations in a proper
obviousness rejection” (App Br. 7 (citing In re Vaeck, 947 F.2d 488 (Fed.
Cir. 1991))).
Thus, among other things, Appellants argue that “the references do
not teach or suggest all the claim limitations. As appreciated by the
examiner, the cited art does not even [sic] the specific compound recited in
claim 96. Accordingly, for this reason alone, the rejection of claim 96
should be reversed” (id.).
In view of the positions advanced by Appellants and the Examiner,
the issue with respect to this rejection is whether the Examiner has shown
that the cited references, in particular Goto, would have rendered the
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compound used in the process in claim 96 obvious to a person of ordinary
skill in the art.
FINDINGS OF FACT (FF”)
1. Goto discloses an imidazole compound useful as a “diabetic medicine
which has the outstanding pharmacological action which improves only a
hyperglycemia condition without critical side effects, such as hypoglycemia”
(Goto [0001]).
2. Goto’s antidiabetic compounds have the basic formula [1]:

(Id. at [0010].)
3. Goto discloses:
R1 [is] among [type C1-6 alkyl group, a C2-6 alkenyl radical, a
C3-7 cycloalkyl radical, An aryl group, a hetero aryl group or a
JI C1-6 alkylamino radical, a C1-6 alkylamino radical, A C1-6
alkyl sulfonyl group, a C3-7 cycloalkyl radical, C1-6 alkoxy
group, A C1-6 alkoxy carbonyl group, a carboxyl group, a
hydroxyl group, a halogen atom, A C1-6 alkylamino carbonyl
group, a C1-6 alkyl carbonyl group, It is the C1-6 alkyl group
permuted by the aryl group or the hetero aryl group . . . .

(Id.)
4. Goto discloses that “R2 are a hydrogen atom, C1-6 alkyl group,
or an aralkyl radical” (id.).
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5. Goto discloses:
R3 are C1-6 alkyl group, a C1-6 alkoxy carbonyl group, a
halogen atom, a hydroxyl group, or [Formula 24].

(Ring A is an aryl group, a hetero aryl group, or a cycloalkyl
radical here.) R10 A hydrogen atom, a halogen atom, a nitro
group, a hydroxyl group, the amino group, a carboxyl group,
C1-6 alkyl group, C1-6 alkoxy group, a JI C1-6 alkylamino
radical, A C1-6 alkylamino radical, halo C1-6 alkyl group, halo
C1-6 alkoxy group, they are a C3-7 cycloalkyl radical, an
aralkyloxy radical, or C1-6 alkylthio group -- it is --;

(Id.)

6. Goto discloses:

X [is] - (CH2) n- - CH2 n-O-, -O-(CH2) n-, -CR11R12-(CH2)
n-, -CR11R12-(CH2) n-O-, -CR11R12-O-(CH2) n-, or -NR11 -
(here) n is the integer of 0 or 1 thru/or 4, becomes together with
the nitrogen atom with which it differs and a hydrogen atom,
those with C1-6 alkyl group, or R11 and R3 adjoin identically
[ R11 and R12 ], and is [Formula 25].

(Id.)
7. Goto discloses that “R4 and R5 are the same -- or -- differing --
a hydrogen atom, C1-6 alkyl group, or a hydroxyl group -- it is -- R4
and R5 -- together -- becoming-- [Formula 26]” which is a carbonyl
moiety (id.).

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8. Goto discloses:
Y is =CHR9- or =N- and; R6, and R7, R8 and R9 are the same -
- or -- differing -- a hydrogen atom, a halogen atom, C1-6 alkyl
group, C1-6 alkoxy group, a C1-6 alkoxy carbonyl group, a
carboxyl group, an aralkyloxy radical, a C1-6 alkyl
carbonylamino radical, or [Formula 27]

(Here, R13 and R14 become identically together with the
nitrogen atom with which it differs, and is a hydrogen atom,
C1-6 alkyl group, and an aryl group, or R13 and R14 adjoin,
and are [Formula 28].)

(Id.)
9. In addition to the numerous compounds encompassed by its generic
formula, Goto presents 18 different tables showing compounds produced
using different synthesis schemes. (See, e.g. id. at [0065] (“The obtained
compound was shown in Tables 2-4.”))
10. Goto’s compound 2-19, cited by the Examiner as disclosing a
4-chlorophenoxymethyl moiety at the position corresponding to that
required in claim 96 (Ans. 5), does not contain a hydroxyl group at the
position corresponding to that required in claim 96, nor does it contain a
benzyl group at the position corresponding to that required in claim 96 (see
Goto at Table 3).
11. While the Examiner urges that “the remaining R substituents (benzyl,
hydroxy, and hydrogen) of the compound disclosed in claim 96 are clearly
disclosed in numerous examples in the Tables of Goto” (Ans. 5), the
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Examiner does not identify those compounds, or explain the differences
between those compounds and the compound recited in claim 96.
12. The Examiner does not contend that Berger teaches or suggests the
compound recited in claim 96.
PRINCIPLES OF LAW
[T]he Examiner bears the burden of establishing a prima
facie case of obviousness based upon the prior art. “[The
Examiner] can satisfy this burden only by showing some
objective teaching in the prior art or that knowledge generally
available to one of ordinary skill in the art would lead that
individual to combine the relevant teachings of the references.”

In re Fritch, 972 F.2d 1260, 1265 (Fed. Cir. 1992) (citations omitted,
bracketed material in original).
Thus, while the Supreme Court emphasized “an expansive and
flexible approach” to the obviousness question in KSR Int’ l Co. v. Teleflex
Inc., 550 U.S. 398, 415 (2007), the Court nonetheless also reaffirmed that
it can be important to identify a reason that would have
prompted a person of ordinary skill in the relevant field to
combine the elements in the way the claimed new invention
does . . . because inventions in most, if not all, instances rely
upon building blocks long since uncovered, and claimed
discoveries almost of necessity will be combinations of what, in
some sense, is already known.

Id. at 418-419 (emphasis added).
Applying KSR, the Federal Circuit has stated that “in cases involving
new chemical compounds, it remains necessary to identify some reason that
would have led a chemist to modify a known compound in a particular
manner to establish prima facie obviousness of a new claimed compound.”
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Takeda Chemical Industries, Ltd. v. Alphapharm Pty., Ltd., 492 F.3d 1350,
1357 (Fed. Cir. 2007).
ANALYSIS
We agree with Appellants that the Examiner has not shown that the
cited references, in particular Goto, would have rendered the compound used
in the process in claim 96 obvious to a person of ordinary skill in the art.
We note that Goto discloses a compound having a “core” structure
similar to the compound recited in claim 96 (FF 2). However, Goto’s
compound has eight different variable “R” moieties, as well as variable “X”
and “Y” moieties, each of which can be any one of numerous different
substituents varying from different length alkyl groups to cycloalkyl, aryl,
and heterocyclic groups (FF 2-8).
We are not persuaded that the Examiner has adequately explained
why an ordinary artisan would have been prompted by either Goto’s generic
disclosure, or the specific compounds listed in the tables, to arrive at the
compound recited in claim 96.
Specifically, the Examiner urges that the 4-chlorophenoxymethyl
substituent at the position corresponding to that required in claim 96 is
“preferred” (Ans. 5). However, the Examiner does not point to, and we do
not see, any reference to a 4-chlorophenoxymethyl moiety in Goto’s generic
description of its compounds, much less a disclosure that any particular
substituent is preferred.
Moreover, Goto explicitly states that its tables are lists of “obtained
compound[s]” (see e.g., Goto at [0065] (FF 9)); thus it appears the tables are
lists of the compounds actually synthesized by Goto. We are therefore not
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persuaded that Goto’s tables set forth a list of all possible moieties that can
simply be plugged into the core structure, in any combination.
As noted above, even applying KSR’s flexible standard of
obviousness, “in cases involving new chemical compounds, it remains
necessary to identify some reason that would have led a chemist to modify a
known compound in a particular manner to establish prima facie
obviousness of a new claimed compound.” Takeda Chemical v.
Alphapharm, 492 F.3d at 1357.
As also noted above, the only specific compound of Goto pointed to
by the Examiner does not contain a hydroxyl group at the position
corresponding to that required in claim 96, nor does it contain a benzyl
group at the position corresponding to that required in claim 96 (FF 10).
Despite these differences, the Examiner has not explained why an ordinary
artisan would have been led to modify that compound, or any of the others
disclosed by Goto, to arrive at a compound having the structure required in
claim 96.
As we are not persuaded that Goto’s generic disclosure would have
been sufficiently specific to lead an ordinary artisan to the specific
compound recited in claim 96, and as the Examiner has not pointed to any
specific evidence that would have provided an ordinary artisan with a reason
to modify the actual compounds described by Goto to arrive at the structure
recited in claim 96, we are not persuaded that the Examiner has met the
required burden of showing that the claimed compound would have been
obvious based on Goto’s disclosure. Accordingly, we are compelled to
reverse the Examiner’s obviousness rejection of claim 96 over Goto and
Berger.
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REVERSED

alw

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McCOLLUM, Administrative Patent Judge, concurring.

I concur with the decision to reverse the Examiner’s rejection.
However, in deciding to reverse, I considered that, not only would one of
ordinary skill in the art have to select the claimed compound from the
multitude of compounds encompassed by Goto formula 1, he or she would
then need to select diabetics having neuropathy from diabetics generally in
order to meet the recitation in claim 96 of administering to “a mammalian
subject in need of blockage of voltage-sensitive channels of neuronal
mammalian cells.”

CONCURRING

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