Ex Parte Bakker

Board of Patent Appeals and Interferences

Nov 18, 2008

11134455 (B.P.A.I. Nov. 18, 2008)

UNITED STATES PATENT AND TRADEMARK OFFICE
__________

BEFORE THE BOARD OF PATENT APPEALS
AND INTERFERENCES
__________

Ex parte CORNELIS BAKKER
__________

Appeal 2008-4280
Application 11/134,455
Technology Center 1600
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Decided: November 18, 2008
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Before TONI R. SCHEINER, ERIC GRIMES, and FRANCISCO C.
PRATS, Administrative Patent Judges.

GRIMES, Administrative Patent Judge.

DECISION ON APPEAL
This is an appeal under 35 U.S.C. § 134 involving claims to the salt
form of a compound and a method of making a composition comprising it.
The Examiner has rejected the claims for obviousness-type double patenting.
We have jurisdiction under 35 U.S.C. § 6(b). We affirm.
Appeal 2008-4280
Application 11/134,455

Statement Of The Case
The Specification describes a phenylpiperazine derivative having the
following structure:

(Spec. 1: 3-6.). As indicated by “CH3SO3H,” the compound is in the
methanesulfonate salt form (id. at 1: 1-2).1 The Specification states that the
“mesylate compound is much better soluable [sic] in water than the free base
resulting in a good bio-availability” (id. at 2: 15-16).
Claims 4-9, 11, and 12 are pending and on appeal. The claims have
not been argued separately and therefore stand or fall together. 37 C.F.R.
§ 41.37(c)(1)(vii). Claim 4 is representative and reads as follows:
4. A method of preparing a pharmaceutical composition
comprising combining an effective amount of at least one compound of the
formula:

with at least one auxiliary substance.

1 Mesylate and methane sulphonate are synonyms of methanesulfonate.
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Application 11/134,455

The Examiner has rejected claims 4-9, 11, and 12 for obviousness-
type double patenting based on claims 1, 2, and 5 of Van Hes.2
Issue
The Examiner’s position is that the instant claims are not patentably
distinct from Van Hes’s claims because Van Hes’s claims encompass the
compound and mesylate salt form recited in the claims on appeal, and Van
Hes’s disclosure specifically names the methanesulfonate salt form among a
short list of salts (Answer 4-5).
Appellant contends that the specific compound of the claims on
appeal would not have been suggested by Van Hes’s claims, considered by
themselves rather than in combination with Van Hes’s disclosure.
The issue to be decided is: Did the Examiner err in concluding that,
to a person skilled in the art, the process of instant claim 4 would have been
an obvious variant of Van Hes’s claims 1, 2, and 5?
Findings of Fact
1. Claim 1 of Van Hes is directed to a compound of the following
formula:

in which X represents a group of the following formula

2 Van Hes et al., U.S. Patent 7,067,513 B1, issued June 27, 2006.
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Application 11/134,455

and the variables R5-R7, S1-S5, Y, m, and n are chosen from specified groups
or values (Van Hes, col. 16, l. 57 to col. 17, l. 28).
2. The compound of the claims on appeal corresponds to that of Van
Hes’s claim 1 in which m is 3; R5 and R6 are H; n is 1; R7 is 5-fluoro; S1, S3,
and S5 are H; S4 is oxo; S2 is CH3; and Y is O (compare instant claim 4 to
Van Hes claim 1).
3. Claim 2 of Van Hes is directed to the compound of Van Hes’s
claim 1 in which “m is 3, R5=R6=H, n is 0 or 1, and R7 is 5-fluoro, an
enantiomer thereof, or a salt of any of the foregoing” (Van Hes, col. 17, ll.
30-32)
4. Van Hes includes a Certificate of Correction stating that claim 2
also includes the limitations that “S1=S3=S5=H, S4=oxo and S2=CH3” (Van
Hes, Certificate of Correction).
5. Van Hes’s claim 2 defines a set of six compounds, which vary in
the constituents at positions R7 (5-fluoro or H) and Y (CH2, O, or S), having
the following structures:

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(Van Hes, col. 16, l. 16 to col. 17, l. 32; Certificate of Correction.)
7. The compound of Van Hes’s claim 2 in which R7 is 5-fluoro and Y
is O has the structure shown in claim 4 on appeal.
8. Claim 5 of Van Hes defines a “method of preparing a
[pharmaceutical composition comprising at least one compound as claimed
in claim 1 . . . and at least one auxiliary substance], comprising mixing the at
least one compound, an enantiomer thereof, or a salt of any of the foregoing
with the at least one auxiliary substance” (Van Hes, col. 18, ll. 23-26).
9. The instant Specification states that the mesylate salt form of the
compound recited in the claims on appeal can be made by converting the
free base “into the mesylate according to processes known per se for salt
formation” (Spec. 2: 27-28).
10. The instant Specification provides an example in which the free
base of the compound recited in the claims on appeal is suspended in
methanol, mixed with methane sulfonic acid (in methanol), allowed to
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crystallize, isolated and dried to yield the mesylate salt form of the
compound (Spec. 2: 32 to 3: 3).
11. The Examiner finds that the “scope of salts is a very finite list”
(Answer 6).
12. The Examiner finds that the “methanesulfonate salt forms . . . are
reasonably expected to share the same properties as the free forms given the
express equivalency teaching recited in the claims” (Answer 6).
Principles of Law
“Obviousness-type double patenting is a judicially created doctrine
grounded in public policy, which prevents the extension of the term of the
original patent via the patenting of an obvious variation.” Georgia-Pacific
Corp. v. U.S. Gypsum Co., 195 F.3d 1322, 1326 (Fed. Cir. 1999).
“Obviousness [under 35 U.S.C. § 103] requires inquiry into a
motivation to modify the prior art; nonstatutory double patenting does not.”
Geneva Pharms., Inc. v. GlaxoSmithKline PLC, 349 F.3d 1373, 1378 n.1
(Fed. Cir. 2003).
“Because nonstatutory double patenting compares earlier and later
claims, an earlier patent’s disclosure is not available to show nonstatutory
double patenting. Of course, the earlier patent’s disclosure may register on
the patentability scale if that patent qualifies as prior art under 35 U.S.C.
§ 102, which is generally not the case.” Id. at 1385 (citation omitted).
A disclosure that allows one skilled in the art to “at once envisage
each member of [a] limited class” describes each member of the class “as
fully as if [it] had drawn each structural formula or had written each name.”
In re Petering, 301 F.2d 676, 681-82 (CCPA 1962).
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Analysis
Claim 4 on appeal differs from claim 5 of Van Hes in two ways: (1)
instant claim 4 is limited to a method of making a single compound within
the genus of compounds encompassed by Van Hes’s claim 5, and (2) instant
claim 4 is limited to a method of making the mesylate salt form of the
compound while Van Hes’s claim 5 encompasses making “a salt”
generically.
Neither of these differences would have made the process of claim 4
nonobvious to a person of ordinary skill in the art. Van Hes’s claim 2
defines a set of six compounds, one of which is the specific compound
recited in instant claim 4. Van Hes’s group of compounds is so limited that
it allows those skilled in the art to immediately envisage each member of the
group, and therefore discloses the members of the group as fully as if each
structural formula had been written out. Van Hes’s claim 2 thus would have
made obvious the compound recited in instant claim 4.
Van Hes’s claim to “a salt” generically also would have made obvious
the mesylate salt of the claims on appeal. The Examiner has found that there
are “a very finite” number of pharmaceutically acceptable salts, and
Appellant has not challenged this finding. Those of skill in the art would
have recognized that only a limited number of salts have been approved by
the Food and Drug Administration. See Pfizer, Inc. v. Apotex, Inc., 480 F.3d
1348, 1366 (Fed. Cir. 2007) (as of 1974, only 53 pharmaceutically
acceptable anions known). Those skilled in the art would also have
recognized that the FDA-approved salts include mesylate. See id. at 1354
(pharmaceutically acceptable anions include “hydrochloride, methane
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sulphonate, benzene sulphonate, lactate, succinate, and acetate” (emphasis
added)).
Van Hes’s claims support the Examiner’s finding that those skilled in
the art would have expected the salt form of the compounds claimed by Van
Hes to be functionally equivalent to the free base form of the compounds.
That is, Van Hes’s claim to certain compounds, “an enantiomer thereof, or a
salt of any of the foregoing” is evidence that those skilled in the art would
have expected enantiomers and salts of the claimed compounds to have
functional activity equivalent to that of the free base form. Appellant has
provided no evidence to support a contrary conclusion.
In summary, the mesylate salt form of the compounds claimed in Van
Hes would have been an obvious variant of the free base form of the
compounds because (1) those skilled in the art would have recognized that
the mesylate salt form is one of only a limited number of pharmaceutically
acceptable salts and (2) those skilled in the art would have expected the
mesylate salt form of the compound to have functional activity equivalent to
that of the free base form.
Appellant has argued that the Examiner erred in relying on the
specification of Van Hes as evidence that the specific compound and
mesylate salt form would have been obvious variants of Van Hes’s claims
(App. Br. 9-10; Reply Br. 9-10).
We agree with Appellant that the disclosure of a patent cannot be
relied on in the context of a double patenting rejection unless the patent
qualifies as prior art, which the Examiner has not shown to be the case here.
The Examiner’s error, however, is harmless because, for the reasons
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discussed above, the process of claim 4 on appeal would have been an
obvious variant of the Van Hes’s claims 1, 2, and 5 even without Van Hes’s
specification.
Conclusions of Law
The Examiner did not err in concluding that, to a person skilled in the
art, the process of instant claim 4 would have been an obvious variant of
Van Hes’s claims 1, 2, and 5.
Summary
We affirm the rejection of claim 4. Claims 5-9, 11, and 12 fall with
claim 4.

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

dm

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