Ex Parte Bakker et al

Patent Trial and Appeal Board

Jun 24, 2015

11085193 (P.T.A.B. Jun. 24, 2015)

UNITED STATES PATENT AND TRADEMARK OFFICE
UNITED STATES DEPARTMENT OF COMMERCE
United States Patent and Trademark Office
Address: COMMISSIONER FOR PATENTS
P.O. Box 1450
Alexandria, Virginia 22313-1450
www.uspto.gov
APPLICATION NO. FILING DATE FIRST NAMED INVENTOR ATTORNEY DOCKET NO. CONFIRMATION NO.
11/085,193 03/22/2005 Cornelis Bakker 01975.0070 5060
22852 7590 06/24/2015
FINNEGAN, HENDERSON, FARABOW, GARRETT & DUNNER
LLP
901 NEW YORK AVENUE, NW
WASHINGTON, DC 20001-4413
EXAMINER
JARRELL, NOBLE E
ART UNIT PAPER NUMBER
1622
MAIL DATE DELIVERY MODE
06/24/2015 PAPER
Please find below and/or attached an Office communication concerning this application or proceeding.
The time period for reply, if any, is set in the attached communication.
PTOL-90A (Rev. 04/07)
UNITED STATES PATENT AND TRADEMARK OFFICE
__________

BEFORE THE PATENT TRIAL AND APPEAL BOARD
__________

Ex parte CORNELIS BAKKER, JEFFREY C. GLENNON,
MAYKE B. HESSELINK, CLAUDIA THAETE, ANDREW MCCREARY,
and GUSTAAF J.M. VAN SCHARRENBURG
__________

Appeal 2012-004062
Application 11/085,193
Technology Center 1600
__________

Before ERIC B. GRIMES, LORA M. GREEN, and ERICA A. FRANKLIN,
Administrative Patent Judges.

FRANKLIN, Administrative Patent Judge.

DECISION ON APPEAL
This is an appeal1 under 35 U.S.C. § 134 involving claims to a method
for treating pain. The Patent Examiner rejected the claims as obvious. We
have jurisdiction under 35 U.S.C. § 6(b). We reverse.
STATEMENT OF THE CASE
The invention relates to the use of known broad spectrum 5-HT
receptor binding compounds to treat pain. Spec. 1:4–16. The compounds of
the invention have functional serotonin receptor activities, including potent
5-HT1A-agonistic activity, and 5-HT1D-antagonistic activity. Id. at 1:6–7.

1 Appellants identify the Real Party in Interest as Solvay Pharmaceuticals
B.V. (App. Br. 3.)
Appeal 2012-004062
Application 11/085,193

2
Claims 13, 15, and 16 are on appeal. Claim 13 is representative and
reads as follows:
13. A method for treating pain, comprising:
administering to a subject in need of said treatment, a
pharmaceutical composition comprising a therapeutically
effective amount of at least one compound having the formula
(1):

or a stereoisomer thereof, or a pharmacologically
acceptable salt thereof,
wherein:
R1 is alkyl(1-4C), alkoxy(1-4C), hydroxyl,
alkoxy(1-4C)alkyl (1-4C), pyrrolidinyl, piperidinyl,
morpholinyl, halogen, cyano, trifluoromethyl, amino, or
mono- or disubstituted amino wherein the substituents
are alkyl(1-4C), or alkyl(1-4C) carbonyl,
m has the value 0, 1 or 2,
R2 is alkyl(1-4C), alkoxy(1-4C), halogen or
trifluoromethyl,
n is 0 or 1, on the understanding that (m + n)
is at least 1,
R3 is hydrogen, alkyl(1-3C) or alkenyl(2-3C),
R4 is alkyl(1-4C), and
p has the value 0,1 or 2,
and a pharmaceutically acceptable carrier.

Appeal 2012-004062
Application 11/085,193

3
The Examiner rejected claims 13 and 15 under 35 U.S.C. § 103(a) as
unpatentable over Van Steen2 and Taverne.3 Claim 16 is objected to as
depending upon a rejected base claim.
OBVIOUSNESS
The Examiner found that Van Steen discloses compounds satisfying
formula (1) of the claimed invention. Ans. 5. The Examiner found also that
Van Steen teaches that these compounds may be used in the treatment of
“diseases of the central nervous system caused by disturbances of
serotonergic transmission.” Id. Specifically, Van Steen teaches that its
compounds act on the nervous system by binding to 5-HT receptors, i.e., 5-
HT1A and 5-HT1D subtype receptors. Van Steen 3. Van Steen explains that
binding to these receptors provides strengthened antidepressant activity. Id.
The Examiner found that Taverne “definitively” links 5-HT1 receptors to
analgesic properties. Ans. 5–6. According to the Examiner, the claimed
method is obvious because it does not recite any new properties for
compounds that are anticipated by the prior art. Id. at 6.
Appellants contend that the Examiner’s fact-finding is wrong. App.
Br. 12. In particular, Appellants assert that “Taverne does not make any
affirmative statements linking 5-HT1A receptor agonists to treatment of
pain.” Id.
We agree with Appellants. Taverne expressly states that “the very
high affinity and selectivity of the compounds of the invention for

2 Patent Application Publication No. EP 0650964 A1 by Bartholomeus
Johannes van Steen et al., published May 3, 1995 (“Van Steen”).
3 US Patent No. 5,225,409 issued to Thierry Taverne et al., July 6, 1993
(“Taverne”).
Appeal 2012-004062
Application 11/085,193

4
serotoninergic receptors 5HT1A renders them usable in the treatment of
diseases of the serotoninergic system, and more especially depression, stress,
anxiety and schizophrenia.” Taverne at 1:20–24. During this discussion,
Taverne does not relate the affinity or selectivity of a compound for 5-HT1A
receptors to analgesia or use in treating pain. Rather, in the following
paragraph of the disclosure, Taverne describes additional properties
observed in “some compounds of the invention,” including good analgesia.
Id. at 1:31–33. By describing analgesia as exhibited by only “some” of the
compounds that bind to serotoninergic receptors, Taverne suggests to
persons of ordinary skill in the art that analgesia is not an inherent property
of compounds known to bind to 5-HT1A receptors. Consequently, a person
of ordinary skill in the art would not have had a reasonable expectation of
treating pain by administering the serotoninergic receptor binding
compounds disclosed by Van Steen.
The Examiner’s rebuttal evidence, Ràdl4 and Cook,5 does not establish
otherwise. The Examiner found that together these references describe
anpirtoline as a selective 5-HT1B agonist used to control pain. Ans. 6.
According to the Examiner, these references establish that the link between
serotonin and pain was established before the instant application was filed.
Id. However, neither reference links analgesia to the compound’s ability to
bind a serotonin receptor. Indeed, regarding a study comparing 5-HT1A and
5-HT1B receptor binding affinities and analgesic activity of various

4 Stanislav Ràdl et al., Synthesis and Analgesic Activity of Some Quinazoline
Analogs of Anpirtoline, 333 ARCH. PHARM. PHARM. MED. CHEM. 381 (2000)
5 David F. Cook & David Wirtshafter, Quinpirole Attenuates the Striatal
Immediate Early Gene Expression, But Not the Hyperactivity, Induced by
the Serotonin Agonist RU-24969, 852 BRAIN RES. 247 (2000).
Appeal 2012-004062
Application 11/085,193

5
compounds, including anpirtoline, Ràdl states, “we do not know the
mechanism of the analgesic activity of these compounds and therefore it is
difficult to draw any conclusion from [our] observations.” Ràdl 383.
Accordingly, we conclude that the Examiner has not established that
the claimed method of treating pain would have been obvious over the
combined prior art.
SUMMARY
We reverse the Examiner’s rejection.

REVERSED
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