Ex Parte Flores-Riveros et al

Patent Trial and Appeal Board

Feb 18, 2016

11941934 (P.T.A.B. Feb. 18, 2016)

UNITED STA TES p A TENT AND TRADEMARK OFFICE
APPLICATION NO. FILING DATE
111941,934 11/17/2007
26551 7590
NeurMedix, Inc,
6165 Greenwich Drive
Suite 150
San Diego, CA 92122
02/18/2016
FIRST NAMED INVENTOR
Jaime Flores-Riveros
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
ATTORNEY DOCKET NO. CONFIRMATION NO.
334 1637
EXAMINER
N ANOV A, SVETLANA M
ART UNIT PAPER NUMBER
1627
MAILDATE DELIVERY MODE
02/18/2016 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 JAIME FLORES-RIVEROS, JAMES M. FRINCKE,
CHRISTOPHER READING, DWIGHT STICKNEY,
and CLARENCE AHLEM
Appeal2013-007013
Application 11/941,934
Technology Center 1600
Before RICHARD M. LEBOVITZ, JEFFREY N. FREDMAN, and
JACQUELINE T. HARLOW, Administrative Patent Judges.
FREDMAN, Administrative Patent Judge.
DECISION ON APPEAL
This is an appeal1under35 U.S.C. § 134 involving claims to a
pharmaceutical formulation. The Examiner rejected the claims as obvious.
We have jurisdiction under 35 U.S.C. § 6(b). We affirm.
1 Appellants identify the Real Party in Interest as Harbor
Therapeutics, Inc. (See Br. 1 ).
Appeal2013-007013
Application 11/941,934
Statement of the Case
Background
"The invention relates to methods and compounds such as 4a-fluoro-
l 7 a-ethynylandrost-5-ene-3 B, 7B, l 7B-triol to modulate inflammation,
metabolic disorders and other conditions described herein. The compounds
can be used to treat or slow the progression of conditions such as type 2
diabetes, hyperglycemia and insulin resistance" (Spec. iJ 2).
The Claims
Claims 18-20 are on appeal. Claim 18 is representative and reads as
follows:
18. A pharmaceutical formulation comprising one or more
pharmaceutically acceptable excipients and a compound having the
structure
R15 H
wherein one R1 is-Hor C1-s optionally substituted alkyl and the
other R1 is -OH, an ester or an ether;
one R2 is-Hor C1-s optionally substituted alkyl and the other R2
is -OH or an ester, or both R2 together are =O;
one R3 is-Hand the other R3 is -H, -OH, an ester or an ether;
R4 in the a-configuration is optionally substituted C2-4 alkynyl;
R4 in the B-configuration is -OH or an ester;
R7 is -CH20H; and
R15 is -OH, an ester or an ether
wherein the pharmaceutical formulation is a unit oral dosage
form containing about 5 mg to about 250 mg of the compound.
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Application 11/941,934
The Issues
A. The Examiner rejected claims 18-20 under 35 U.S.C. § 103(a) as
obvious over Ahlem '2992 and Reading3 (Ans. 4-12).
B. The Examiner rejected claims 18-20 under 35 U.S.C. § 103(a) as
obvious over Ahlem '4254 and Reading (Ans. 22-28).
Because the same issues are dispositive for both of these rejections,
we will consider them together.
The issue with respect to these rejection is: Does the evidence of
record support the Examiner's conclusion that either Ahlem '299 or Ahlem
'425, combined with Reading render claim 18 obvious?
Findings of Fact
1. Ahlem '299 teaches a compound of formula 1, reproduced
below:
l
R3
wherein "R1, R2, R3, R4, R5, R6 and R10 independently are-H, -ORPR, ... an
ester, ... an ether, ... an optionally substituted alkynyl group" (Ahlem '299,
col. 4, 11. 45-67). Ahlem '299 teaches "where RPR independently is
hydrogen" (Ahlem '299, col. 9, 1. 1 ).
2 Ahlem et al., US 6,667,299 Bl, issued Dec. 23, 2003.
3 Reading et al., WO 2004/019953 Al, published Mar. 11, 2004.
4 Ahlem et al., US 2003/0060425 Al, published Mar. 27, 2003.
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Appeal2013-007013
Application 11/941,934
2. Ahlem '299 teaches a compound 1.2.5.9 as reproduced below:
tTh
o~··
I l
no~,
(Ahlem '299, col. 66, 11. 30--40).
3. Ahlem '299 teaches that "one can administer the formula 1
compound(s) orally using about 4 to about 40 mg/kg/day, usually about 6-20
mg/kg/day" (Ahlem '299, col. 75, 11. 56-58).
4. Ahlem '425 teaches a compound of formula 1, reproduced
below:
wherein "each R1, R2, R3, R4, R5, R6 and R10 independently are -H, -ORPR, .
. . an ester, ... an ether, ... an optionally substituted alkynyl group"
(Ahlem '425 iii! 25-27). Ahlem '425 further teaches that "RPR
independently is-Hor a protecting group" (Ahlem '425 iJ 35).
5. Ahlem '425 teaches a compound 1.2.5.9 as reproduced below:
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Appeal2013-007013
Application 11/941,934
(Ahlem '425 iJ 422).
6. Ahlem '425 teaches "[i]ntermittent dosing embodiments
include administration of a formula 1 compound, e.g., orally ... as follows:
(1) daily dosing for about 3 to about 190 days (e.g., about 3 to about 20
days)" (Ahlem '425 iJ 461 ).
7. Ahlem '425 teaches that "step (1) may comprise daily dosing of
about 20 mg/day to about 1500 mg/day (e.g., about 50, 75, 100, 125, 150,
175, 200, 225, 250, 275, 300, 325, 350 or 400 mg/day) of a formula 1
compound" (Ahlem '425 iJ 462).
8. Reading teaches a compound as shown below:
R5 R4
.... 11\\\R4
Rs
wherein "each R1, R2, R3, R4, R5, R6, ... R10B ... independently are -H, -
OH, ... an ester, ... an ether, ... an optionally substituted alkynyl group"
(Reading iii! 15, 23).
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Appeal2013-007013
Application 11/941,934
Principles of Law
[T]he cases establish that if an examiner considers that he
has found prior art close enough to the claimed invention to
give one skilled in the relevant chemical art the motivation
to make close relatives (homologs, analogs, isomers, etc.) of
the prior art compound(s), then there arises what has been
called a presumption of obviousness or a prim a facie case of
obviousness .... The burden then shifts to the applicant,
who then can present arguments and/or data to show that
what appears to be obvious, is not in fact that, when the
invention is looked at as a whole.
In re Dillon, 919 F.2d 688, 696 (Fed. Cir. 1990).
Analysis
We adopt the Examiner's findings of fact and reasoning regarding the
scope and content of the prior art (Ans. 4-12; 22-28; FF 1-8) and agree that
claim 18 is rendered obvious by either Ahlem '299 or Ahlem '425 and
Reading. We address Appellants' arguments below.
Appellants contend that "the Examiner did not articulate why any
alleged lead compound(s) would in fact be considered a lead under the law"
(Br. 9). Appellants contend that the "Examiner did not explain why one of
ordinary skill in the art would have selected the specific chemical
modifications of the alleged lead compound(s) needed to arrive at a claimed
composition in normal course of research and development" (Br. 9).
We find this argument unpersuasive because the rejected claims do
not fall into the paradigm established by the lead compound analysis. In
Takeda, the court applied the lead compound analysis to a claim to a specific
compound, not a genus of compounds as in instant claim 18, finding that "in
cases involving new chemical compounds, it remains necessary to identify
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Application 11/941,934
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 Industries, Ltd. v. Alphapharm Pty., Ltd.,
492 F.3d 1350, 1357 (Fed. Cir. 2007). That is, the Takeda court was not
analyzing a claim drawn to millions of compounds, like instant claim 18, but
rather was analyzing a claim drawn to a compound with one specific
chemical formula. Id. at 1353. Similarly, Otsuka also applied the lead
compound analysis in the context of a claim to the specific compound,
Ariprazole, and Daiichi to the specific compound Olmesartan, so neither
decision was drawn to a genus claim of millions of compounds as in the
instant fact pattern. Otsuka Pharm. Co., Ltd. v. Sandoz, Inc., 678 F.3d 1280,
1284 (Fed. Cir. 2012); Daiichi Sankyo Co., Ltd. v. Matrix Labs., Ltd., 619
F.3d 1346 (Fed. Cir. 2010). Therefore, the Examiner properly rejected rote
application of the lead compound analysis to a fact pattern for which the
analysis is inappropriate. See KSR. Intern. Col. v. Teleflex Inc., 550 US 398,
419 (2007) ("Helpful insights, however, need not become rigid and
mandatory formulas . . . when a court transforms the general principle into a
rigid rule that limits the obviousness inquiry ... it errs)"
We recognize, but find unpersuasive, Appellants' argument that the
"'close structural similarity' the Examiner alleges is cobbled together from
generic structures that encompass millions of species and many individual
disclosed compound species with no obvious reason to do so and no
pertinent properties to guide the selection process" (Br. 17).
Unlike Takeda 's claim to an antidiabetic composition, Otsuka 's claim
to a schizophrenia treating composition, or Daiichi 's claim to treatment of
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Application 11/941,934
high blood pressure, Appellants' claim 18 does not encompass any particular
"pertinent properties" or functional requirements nor is the formulation in
claim 18 directed to any particular disease. Therefore, even the attempt to
apply the lead compound analysis fails because claim 18 lacks one specific
activity or function to serve as the target for optimization using a lead
compound. See Takeda, 492 F.3d 1353; Otsuka, 678 F.3d at 1285; and
Daiichi, 619 F.3d at 1347. Indeed, the instant Specification recites a laundry
list of possible disease targets that is more than two pages in length
encompassing conditions ranging from pain and graft versus host disease to
sleep disturbance, chemical bums, multiple sclerosis, obesity, and
atherosclerosis (see Spec. iii! 64-69). The Specification states that it
"provides compounds or compositions to treat, prevent, slow the progression
of or ameliorate an unwanted inflammation condition[,] an autoimmune
disease or a metabolic disorder or a symptom thereof' (id. at iJ 20), but
Appellants did not direct us to a common activity or property by which the
compounds exerted their beneficial effect. Therefore neither claim 18 nor
the Specification provide specific limitations that would distinguish a
desirable lead compound from an undesirable lead compound.
Instead, the instant facts are more similar to those in Susi, where the
CCP A determined that a prior art genus reference Knapp rendered the
subgenus claim at issue obvious, finding that "[p ]lacing a simple
representative of each side by side, it is obvious that the subject matter of
appellant's claim 6 is very nearly within the generic teaching of Knapp." In
re Susi, 440 F.2d 442, 444 (CCPA 1971). Susi found unpersuasive "the
position of one who argues that the selection of a relatively small subgenus
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Application 11/941,934
from a genus disclosed in the prior art would have been unobvious at the
time of his invention to one skilled in the art." Id. at 445.
In this case, the genus of compounds encompassed by Appellants'
claim 18 represents a subgenus fully disclosed by each of Ahlem '299,
Ahlem '425, and Reading (FF 1, 4, 8). Ahlem '299 or Ahlem '425 each
teach specific compound species that differ from the genus of compounds of
claim 18 by the presence of a single hydroxyl group (FF 2, 5) that is a
suggested alternative in the generic compound disclosures (FF 1, 4). Thus,
the claimed subgenus is reasonably suggested by the cited prior artWe
further agree with the Examiner's finding that the prior art teaches "'ring
walking' of the -OH substituent, including where it can be in the C-4 (i.e. R-
15, per Appellant's formula) position" (Ans. 24-25). Consistent with
Dillon, the Examiner has identified compound 1.2.5.9 as a species
structurally similar to the claimed genus of compounds, differing only in the
R15 group of claim 18 (FF 2, 5). The Examiner recognized that each of
Ahlem '299, Ahlem '425, and Reading suggest generic structures which
teach the placement of substituents including -OH substituents at that
position (FF 1, 4, 8). In response to the Examiner's position, Appellants
have provided no evidence of secondary considerations.
We recognize, but find unpersuasive, Appellants' argument that
"Examiner also ignored the limitation that the claimed formulations are oral
unit doses" (Br. 9-10). Ahlem '299 and Ahlem '425 specifically teach oral
dosages in amounts that overlap those required by claim 18 (FF 3, 6).
Appellants provide no reason why those overlapping oral dosages do not
render the oral dosages required by claim 18 obvious. See In re Peterson,
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Application 11/941,934
315 F.3d 1325, 1329 (Fed. Cir. 2003) ("In cases involving overlapping
ranges, we and our predecessor court have consistently held that even a
slight overlap in range establishes a prim a facie case of obviousness.")
Conclusion of Law
The evidence of record supports the Examiner's conclusion that either
Ahlem '299 or Ahlem '425, combined with Reading render claim 18
obvious.
SUMMARY
In summary, we affirm the rejection of claim 18 under 35 U.S.C.
§ 103 (a) as obvious over Ahl em '299 and Reading. Claims 19 and 20 fall
with claim 18. 37 C.F.R. § 41.37(c)(l)(iv).
We affirm the rejection of claim 18 under 35 U.S.C. § 103(a) as
obvious over Ahlem '425 and Reading. Claims 19 and 20 fall with claim
18. 37 C.F.R. § 41.37(c)(l)(iv).
No time period for taking any subsequent action in connection with
this appeal may be extended under 37 C.F.R. § l.136(a).
AFFIRMED
cdc
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