Ex Parte Gobbi et al

Patent Trial and Appeal Board

Mar 26, 2018

14621903 (P.T.A.B. Mar. 26, 2018)

UNITED STA TES p A TENT AND TRADEMARK OFFICE
APPLICATION NO. FILING DATE FIRST NAMED INVENTOR
14/621,903 02/13/2015 Luca Gobbi
9157 7590 03/28/2018
GENENTECH, INC.
1 DNA WAY
SOUTH SAN FRANCISCO, CA 94080
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.
P30653-US 2706
EXAMINER
SONG, JIANFENG
ART UNIT PAPER NUMBER
1613
NOTIFICATION DATE DELIVERY MODE
03/28/2018 ELECTRONIC
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.
Notice of the Office communication was sent electronically on above-indicated "Notification Date" to the
following e-mail address( es):
pair_roche@firsttofile.com
docketing-uspto-d@gene.com
PTOL-90A (Rev. 04/07)
UNITED STATES PATENT AND TRADEMARK OFFICE
BEFORE THE PATENT TRIAL AND APPEAL BOARD
Ex parte LUCA GOBBI, RENNER KNUST, and ANDREAS KOBLET
Appeal2017-002804
Application 14/621,903 1
Technology Center 1600
Before FRANCISCO C. PRATS, RICHARD J. SMITH, and DAVID
COTTA, Administrative Patent Judges.
COTT A, Administrative Patent Judge.
DECISION ON APPEAL
This is an appeal under 35 U.S.C. § 134 relating to imidazo[2, 1-b]
thiazol-3-one derivatives. Spec. 1. The Examiner rejected the claims on
appeal under 35 U.S.C. § 103(a) as obvious.
We reverse.
1 According to Appellants, the real party in interest is Hoffmann-La Roche
Inc. App. Br. 2.
Appeal2017-002748
Application 12/525,568
STATEMENT OF THE CASE
Claims 1, 2, and 22 are on appeal. Claim 1 is illustrative and reads as
follows:
1. A compound of the formula
r\ R1
OH N
Ar)-)-s
~ N :::---
OR R2
0 I
wherein
Ar is phenyl, pyridinyl, 2,3-dihydro-benzo[l,4]dioxinyl, 1,3-
dihydro-indol-2-one, pyrazinyl, isoxazol-3-yl, imidazolyl,
thiophenyl or pyrimidinyl;
R is lower alkyl or lower alkyl substituted by halogen;
R 1 is hydrogen, halogen, hydroxy, lower alkoxy, lower alkyl and
lower alkoxy substituted by halogen;
R2 is hydrogen, lower alkyl;
R3 is hydrogen, halogen, lower alkyl, lower alkyl substituted by
halogen, lower alkoxy, lower alkoxy substituted by halogen,
O(CH2)mO(CH2)mO-lower alkyl substituted by halogen, cyano,
lower alkoxy substituted by hydroxy, lower alkenyloxy,
C(O)OH, heterocycloalkyl selected from morpholinyl,
pyrrolidinyl or pyrrolidin-2-one, or is heteroaryl selected from
imidazolyl substituted by lower alkyl, or is NR'R" and R' /R"
are independently from each other hydrogen or lower alkyl or-
C(O)lower alkyl; or is
-C(O)NR4R5 and
R4 is hydrogen or lower alkyl and
R5 is hydrogen, lower alkyl, lower alkenyl, -(CH2)m0-lower alkyl
substituted by halogen, lower alkyl substituted by halogen, -
(CH2)n-phenyl optionally substituted by halogen, -
CH2)mNHC(O)-lower alkyl, or -(CH2)mNH2, or
R4 and R5 may form together with the N-atom to which they are
attached a piperidine or azetidine ring, which may be substituted by
halogen; or is
-C(O)O-lower alkyl substituted by halogen;
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Application 12/525,568
n islor2;
m is 1, 2 or 3;
or a pharmaceutically acceptable acid addition salt, a racemic mixture
or its corresponding enantiomer and/or optical isomers thereof.
App Br. 9--10.
The Examiner rejected claims 1, 2, and 22 under 35 U.S.C. § 103(a)
as obvious over the combination of Ali 2 and Pyl. 3
ANALYSIS
In rejecting claims 1, 2, and 22 as obvious, the Examiner found that
Ali disclosed a positional isomer of a species of the compounds recited in
claim 1. Final Act. 5. 4 More specifically, the Examiner found that
compound VII of Ali differed from the claimed compound in that compound
VII has a phenyl substituent at position 5 of the imidazo[2, 1-b ]thiazol-
3(2H)-one ring while the species encompassed by claim 1 includes a phenyl
substituent at position 6 of the imidazo[2, 1-b ]thiazol-3(2H)-one ring. Id. at
6. The Examiner concluded that the claimed species would have been
obvious because positional isomers "are generally of sufficiently close
structural similarity that there is a presumed expectation that such
compounds possess similar properties." Id. The Examiner explains, "since
Ali et al. teaches antifungal activity of compound VII, it is obvious that
position isomer compound 1 also has antifungal activity, and the
2 Ali et al., Synthetic and fungicidal studies on some 2-arylidene-5-phenyl-
4H-imidazo[2,l-b]thiazol-3-(2H)-ones and their dibromo products, 58(11)
JOURNAL OF THE INDIAN CHEMICAL SOCIETY, 1117-18 (1981) ("Ali").
3 Pyl et al., Bicyclic heterocyclic compounds with a common nitrogen atom.
IV. Aminoimidazo[2,l-b]thiazoles, 657 JUSTUS LIEBIGS ANNALEN DER
CHEMIE, 113-20 (1962) ("Pyl").
4 Office Action mailed April 22, 2016 ("Final Act.").
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Application 12/525,568
composition comprising compound 1 and a pharmaceutical acceptable
carrier is obvious to one artisan in the art." Id. at 7.
Appellants argue, inter alia, that the Examiner treats compound VII of
Ali as a "lead compound," but "fails to explain why a person of ordinary
skill in the art would select 'compound VII' as a lead compound for
development of the compounds of claims 1, 2 and 22." App. Br. 7.
As stated inin re Oetiker, 977F.2d1443, 1445 (Fed. Cir. 1992):
"[T]he examiner bears the initial burden ... of presenting a prima facie case
ofunpatentability." Appellant has persuaded us that the Examiner has not
carried the burden of establishing that the claimed invention would have
been obvious over the cited art.
Although the Examiner's obviousness analysis does not expressly
identify Ali's compound VII as a "lead compound," in positing that it would
have been obvious to modify compound VII to arrive at the claimed
compound, the Examiner appears to have applied a lead compound analysis.
A lead compound is defined as "'a compound in the prior art that would be
most promising to modify in order to improve upon its ... activity and
obtain a compound with better activity."' Otsuka Pharm. Co., Ltd. v.
Sandoz, Inc., 678 F.3d 1280, 1291 (Fed. Cir. 2012) (citing Takeda Chem.
Indus., Ltd. v. Alphapharm Pty., Ltd., 492 F.3d 1350, 1357 (Fed. Cir. 2007)).
Stated another way, "a lead compound is 'a natural choice for further
development efforts."' Id. (citing Altana Pharma AG v. Teva Pharm. USA,
Inc., 566 F.3d 999, 1008 (Fed. Cir. 2009)). "While the lead compound
analysis must, in keeping with KSR, not rigidly focus on the selection of a
single, best lead compound, ... the analysis still requires the challenger to
demonstrate ... that one of ordinary skill in the art would have had a reason
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Application 12/525,568
to select a proposed lead compound or compounds over other compounds in
the prior art." Daiichi Sankyo Co., Ltd. v. Matrix Laboratories, Ltd., 619
F.3d 1346, 1354 (Fed. Cir. 2010). The analysis of whether a person of
ordinary skill would have chosen the prior art compound as a lead
compound "is guided by evidence of the compound's pertinent properties"
including "positive attributes such as activity and potency," "adverse effects
such as toxicity," "and other relevant characteristics in evidence." Otsuka,
678 F.3d at 1292.
Importantly, "[a ]bsent a reason or motivation based on such prior art
evidence, mere structural similarity between a prior art compound and the
claimed compound does not inform the lead compound selection." Id.; see
also Daiichi, 619 F.3d at 1354 ("[P]roving a reason to select a compound as
a lead compound depends on more than just structural similarity, but also
knowledge in the art of the functional properties and limitations of the prior
art compounds.").
The Examiner contends that all of the compounds disclosed in Ali are
fungicidal. Ans. 10. However, the Examiner does not articulate a reason
why "one of ordinary skill in the art would have had a reason to select a
proposed lead compound or compounds over other compounds in the prior
art." Daiichi, 619 F.3d at 1354; Ans. 11 (responding to Appellants'
argument that the Examiner failed to explain why the skilled artisan would
have selected compound VII as a lead compound by noting - correctly, but
without addressing the lead compound argument - that the tau aggregation
properties relied upon by Appellants are not recited in the claims).
Moreover, as Appellants argue (App. Br. 5---6), it is not clear that compound
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Application 12/525,568
VII is, in fact, fungicidal. Accordingly, we reverse the Examiner's rejection
of claims 1, 2, and 22.
SUMMARY
In summary, we reverse the rejection of claims 1, 2, and 22 under 35
U.S.C. § 103(a) as obvious over the combination of Ali and Pyl.
REVERSED
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