LG CHEM, LTD.

Patent Trials and Appeals Board

Jul 14, 2020

14913132 - (D) (P.T.A.B. Jul. 14, 2020)

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.
14/913,132 02/19/2016 Heui Sul PARK 1599-0453PUS1 6788
2292 7590 07/14/2020
BIRCH STEWART KOLASCH & BIRCH, LLP
8110 Gatehouse Road
Suite 100 East
Falls Church, VA 22042-1248
EXAMINER
NEAGU, IRINA
ART UNIT PAPER NUMBER
1627
NOTIFICATION DATE DELIVERY MODE
07/14/2020 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):
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PTOL-90A (Rev. 04/07)
UNITED STATES PATENT AND TRADEMARK OFFICE
__________

BEFORE THE PATENT TRIAL AND APPEAL BOARD
__________

Ex parte HEUI SUL PARK, SUN YOUNG KOO, HYOUNG JIN KIM,
SUNG BAE LEE, HYO SHIN KWAK,
VASILY ARTEMOV, and SOON HA KIM
__________

Appeal 2019-006050
Application 14/913,132
Technology Center 1600
__________

Before JEFFREY N. FREDMAN, ULRIKE W. JENKS, and
TAWEN CHANG, Administrative Patent Judges.

FREDMAN, Administrative Patent Judge.

DECISION ON APPEAL
This is an appeal1,2 under 35 U.S.C. § 134(a) involving claims to
indole compounds of Formula I. The Examiner rejected the claims as
obvious. We have jurisdiction under 35 U.S.C. § 6(b). We reverse.

1 We use the word “Appellant” to refer to “applicant” as defined in 37
C.F.R. § 1.42. Appellant identifies the Real Party in Interest as LG CHEM,
LTD. (see App. Br. 1).
2 We have considered and refer to the Specification of Feb. 19, 2016
(“Spec.”); Final Office Action of Sept. 27, 2018 (“Final Action”); Appeal
Brief of Feb. 13, 2019 (“App. Br.”); Examiner’s Answer of June 12, 2019
(“Ans.”); and Reply Brief of Aug. 9, 2019 (“Reply Br.”).
Appeal 2019-006050
Application 14/913,132
2
Statement of the Case
Background
“[N]ecrosis is a cell death which mainly occurs under pathologic
circumstances, and in most cases it is characterized by an accompanying
inflammatory response” (Spec. 1). “[T]ypical diseases caused by necrosis
include ischemic (e.g., myocardial infarction, stroke, renal infarction),
neurodegenerative and inflammatory diseases” (id. 1–2).
The Specification teaches, “the indole derivatives of Formula (I) . . .
show a superior effect for the prevention and treatment of cellular necrosis
and necrosis-associated diseases” (Spec. 3).
The Claims
Claims 1, 2, 5–12, 15, 32, and 33 are on appeal. Claim 1 is
representative and reads as follows:
1. An indole compound of the following Formula (1) or a
pharmaceutically acceptable salt or isomer thereof:

in which
m denotes a number of 1 to 3;
n denotes a number of 0 to 2;
R1 represents hydrogen, C1-C6-alkyl, -(CH2)n-C3-C6-
cycloalkyl or -(CH2)n-heterocyclyl, wherein heterocyclyl is a 4-
to 8-membered ring having 1 to 3 heteroatoms selected from N,
O and S;
R2 represents C1-C6-alkyl or -(CH2)n-A-R6, wherein A
represents C4-C8-cycloalkyl, or represents 4- to 8-membered
heterocyclyl or heteroaryl each of which has 1 to 3 heteroatoms
Appeal 2019-006050
Application 14/913,132
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selected from N, O and S, or represents 6- to 10-membered aryl,
R6 represents hydrogen, C1-C6-alkyl, halogen, hydroxy, nitrile,
nitro, -C(O)-R7 or -SO2R7, and R7 represents C1-C6-alkyl or
allyl, or represents 6- to 10-membered aryl, or represents 4- to
8-membered heterocyclyl or heteroaryl each of which has 1 to 3
heteroatoms selected from N and S, and is optionally
substituted with oxo;
R3 represents hydrogen, halogen, hydroxy, -O-R7, -NH-
R7 or -(CH2)n-R7;
R4 represents hydrogen or XR8R9, wherein X represents
CH or N, R8 and R9 independently of one another represent
hydrogen or Z-R10, Z represents -(CH2)n-, -C(O)-,-C(O)(CH2)n-
or -(CH2)nC(O)-, R10 represents hydrogen, amino, C3-C6-
cycloalkyl or -(NH)rC(=NH)NH2, or represents 4- to 8-
membered heteroaryl or heterocyclyl each of which has
1 to 3 heteroatoms selected from N, O and S, and r denotes a
number of 0 or 1;
R5 represents hydroxy or 6- to 10-membered aryl, or
represents -(CH2)n-4- to 9-membered heterocyclyl which has 1
to 4 heteroatoms selected from N, O and S, and optionally
contains oxo; and
where alkyl, alkoxy, aryl, cycloalkyl, heterocycle and
heteroaryl may be optionally substituted, and the substituents
are one or more selected from the group consisting of hydroxy,
halogen, nitrile, amino, C1-C6-alkylamino, di(C1-C6-
alkyl)amino, carboxy, C1-C6-alkyl, halogeno-C1-C6-alkyl, C1-
C6-alkoxy, aryl- C1-C6-alkoxy and oxo.

The Rejections
The Examiner rejected claims 1, 2, 5–12, 15, 32, and 33 under 35
U.S.C. § 103(a) as obvious over Kim ’5333 (Ans. 3–9).
The Examiner rejected claims 1, 2, 5–12, 15, 32, and 33 under 35
U.S.C. § 103(a) as obvious over Kim ’6734 (Ans. 10–13).

3 Kim et al, US 2010/0291533 A1, published Nov. 18, 2010.
4 Kim et al, US 2010/0197673 A1, published Aug. 5, 2010.
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Application 14/913,132
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Because both of these rejections turn on the same issues and rely upon
similar prior art, we will consider them together.
The Examiner finds Kim ’533 teaches a “subgenus of compounds of
formula (Ia)” (Ans. 3; cf. Ans 10 for Kim ’673). The Examiner finds Kim
’533 teaches specific structures such as the compound of Example 1 (Ans.
5–6; cf. Kim ’533 ¶ 521).
The Examiner acknowledges the “difference between the specific
compounds above disclosed by Kim (2010/0291533) and the instantly
claimed compounds is in the substituent at the 2 position of the indole ring”
(Ans. 7). The Examiner further acknowledges “Kim [’533] does not
specifically teach the instant compounds” (id. at 8).
The Examiner finds it obvious to synthesize the elected species, as
well as other compounds of Formula I, “because such compounds are direct
structural homologs (m = 1, 2, 3, 4) of the compounds Examples 1, 2, 3, 9,
35, 37, 36, 51 disclosed by Kim [’533]” (Ans. 9). The Examiner finds:
Compounds which are position isomers (compounds having the
same radicals in physically different positions on the same
nucleus) or homologs (compounds differing regularly by the
successive addition of the same chemical group, e.g., by -CH2-
groups) are generally of sufficiently close structural similarity
that there is a presumed expectation that such compounds
possess similar properties.
(id.; citing In re Wilder, 563 F.2d 457 (CCPA 1977)).
The issue with respect to these rejections is: Does a preponderance of
the evidence of record support the Examiner’s conclusion that either Kim
’533 or Kim ’673 suggests the claimed compound?
Findings of Fact
1. Kim ’533 teaches:
an indole or indazole compound represented by the
Appeal 2019-006050
Application 14/913,132
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following formula (1), or a pharmaceutically acceptable salt or
isomer thereof as an effective ingredient:

wherein X represents C or N,
n is 0 or 1, and n is 1 when X is C and n is 0 when X is
N,
A represents a direct bond, C3-C8-cycloalkyl, phenyl, or
5-6-membered heteroaryl or heterocycle, each of which
includes 1⁓3 heteroatoms selected from N, O and S
atoms, . . .
R2 represents -(CR5R6)m-D-X"—R8.

(Kim ’533 ¶¶ 10–20).
2. Kim ’533 teaches, in Example 1, a compound that provides
clear direction for positions R1, R2, and R3 of Formula 1 of claim 1.

The compound of Example 1 of Kim ’533, shown above, is named
“cyclopentyl-[2-(4,5-dihydro-thiazol-2-yl)-1H-indol-7-yl]-amine” (Kim ’533
¶ 521).

Principles of Law
Under the lead compound analysis rubric, we must first “determine[]
whether a chemist of ordinary skill would have selected the asserted prior art
compounds as lead compounds, or starting points, for further development
Appeal 2019-006050
Application 14/913,132
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efforts.” Otsuka Pharm. Co. v. Sandoz, Inc., 678 F.3d 1280, 1291 (Fed. Cir.
2012). “The second inquiry in the analysis is whether the prior art would
have supplied one of ordinary skill in the art with a reason or motivation to
modify a lead compound to make the claimed compound with a reasonable
expectation of success.” Id. at 1292.
A prima facie case for obviousness requires “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.” KSR Int’l Co. v.
Teleflex Inc., 550 U.S. 398, 418 (2007).
Analysis
Species election
Appellant contends “the Examiner has not acknowledged that the
elected species is free of the prior art. The elected species alone should be
currently under examination over the cited prior art as required before
extending the search and examination to other members of Formula (1).”
(Appeal Br. 10).
The Examiner responds “the examiner has sole discretion in what is
examined in addition to the elected species. MPEP 803.02, cited by
Appellant, sets no prohibition against examination of additional species,
beyond the elected species. In this case, the examiner has found the elected
species obvious” (Ans. 13).
Appellant is correct that:
If the examiner determines that the elected species is allowable
over the prior art, the examination of the Markush claim will be
extended. If prior art is then found that anticipates or renders
obvious the Markush claim with respect to a nonelected
species, the Markush claim shall be rejected; claims to the
nonelected species would still be held withdrawn from further
consideration. The prior art search will not be extended
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Application 14/913,132
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unnecessarily to cover all nonelected species, and need not be
extended beyond a proper Markush grouping.
MPEP § 803.02(III)(A). However, MPEP § 803.02(III)(A) also states that
“[f]ollowing election, the Markush claim will be examined fully with respect
to the elected species and further to the extent necessary to determine
patentability.” Thus, the MPEP authorizes the Examiner to perform
additional searching beyond the elected species, if the Examiner determines
that the claim requires further search.
Ordinarily, we limit our consideration of the merits of the appealed
rejection to the elected species. See Ex parte Ohsaka, 2 USPQ2d 1460,
1461 (BPAI 1987). Here, where the Examiner has apparently performed
additional searching, we acknowledge the Examiner’s apparent withdrawal
of the species election and address the entire claim.
Obviousness
Appellant contends “the proper analysis for the obviousness of a
chemical compound is well established as the lead compound analysis”
(Appeal Br. 11). Appellant contends “the Examiner has not explained or
provided a justification on when the Examiner has the option to contradict
the case law and USPTO precedent in analyzing the obviousness of chemical
compounds” (id. at 12). Appellant contends
the Examiner does not provide any motivation for selecting a
particular subgenus among the vast alternatives in Formula la of
Kim ’533. . . . the Examiner identifies eight specific compounds
(1, 2, 3, 9, 35, 36, 37 and 51) from among the myriad of
compounds in Kim ’533 . . . [but] does not provide motivation
for selecting these eight specific compounds from the vast
number of compounds.
(id. at 12). Appellant contends
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[t]he Examiner also identifies the compounds of Examples 147,
148 and 149 . . . Examples of 147 (1.08 μM) 148 (2.35 μM) and
149 (1.45 μM) have among the worst activities of all of the
compounds of Kim ’533. Therefore, one of ordinary skill in the
art would clearly be motivated not to select these compounds
(id. at 13).
The Examiner responds:
If the disclosure by Kim ’533 is viewed as “combinatorial prior
art possibilities”, the instant claims, as written, also cover
“combinatorial possibilities”, with the two genera- that of the
prior art and of the instant claims- overlapping. The examiner’s
position is that a subgenus of a broad genus disclosed in the
prior art, having the very utility as described in the prior art, is
rendered obvious by the teachings of the prior art.
(Ans. 18).
We agree with Appellant. Whether in the context of a lead compound
analysis or in selecting known equivalents, the burden is on the Examiner to
establish a prima facie case.
If we apply the lead compound analysis, the Examiner does not
identify a specific compound as the lead compound (see, e.g., Ans. 14
“obviousness of chemical compounds need not always be evaluated under
the ‘lead compound’ framework.”) To the extent that any compound might
be selected as the lead compound, compound of Example 1 of Kim ’533 is a
reasonable choice. This compound differs from the claimed compounds in
lacking at least one of the branches leading to the R4 and R5 groups recited
in claim 1 where at least a methyl is required at the R4 location. The
Examiner provides no reason to make the particular modification(s) required
to this Example I compound to obtain either the elected species or a
compound within the scope of claim 1.
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Application 14/913,132
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Alternatively, even if we apply the obvious equivalents/overlapping
genus analysis of the Examiner, the Examiner does not establish that the
selections made in the rejection were known, obvious equivalents.
O’Farrell identifies two kinds of error in an “obvious to try” analysis:
In some cases, what would have been “obvious to try” would
have been to vary all parameters or try each of numerous
possible choices until one possibly arrived at a successful
result, where the prior art gave either no indication of which
parameters were critical or no direction as to which of many
possible choices is likely to be successful. . . . In others, what
was “obvious to try” was to explore a new technology or
general approach that seemed to be a promising field of
experimentation, where the prior art gave only general guidance
as to the particular form of the claimed invention.
In re O’Farrell, 853 F.2d 894, 903 (Fed.Cir.1988). The instant situation fits
both of O’Farrell’s error types, since selection of the particular R groups
from the prior art of Kim ’533 and Kim ’673 would require trying a number
of possible choices, without any indication in the prior art identifying the
specific choices as functioning in treatment of necrosis. Moreover, Kim
’533 and Kim ’673 at best provide general guidance for functional
compounds (FF 1).
We also agree with Appellant that this case falls squarely within the
ambit of Ruschig and Baird (see Reply Br. 4), because
[i]n the instant case, the generic . . . formula disclosed in [the
prior art] contains a large number of variables. . . . While the
[prior art] formula unquestionably encompasses [the claimed
species] when specific variables are chosen, there is nothing in
the disclosure of [the prior art] suggesting that one should select
such variables.
In re Baird, 16 F.3d 380, 382 (Fed. Cir. 1994). The disclosure of a genus
does not necessarily implicitly describe every subgenus encompassed by that
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Application 14/913,132
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genus. In re Smith, 458 F.2d 1389, 1395 (CCPA 1972). Ruschig explained
this standard in the written description context by analogizing a genus and
its constituent species to a forest and its trees, noting that,
It is an old custom in the woods to mark trails by making blaze
marks on the trees. It is no help in finding a trail . . . to be
confronted simply by a large number of unmarked trees.
Appellants are pointing to trees. We are looking for blaze
marks which single out particular trees. We see none.
In re Ruschig, 379 F.2d 990, 994–95 (1967). As Appellant correctly notes,
the Examiner has not provided any blaze marks directing the ordinary artisan
to select either the elected species or compounds within the scope of the
instant claim 1.
Conclusion of Law
A preponderance of the evidence of record does not support the
Examiner’s conclusion that either Kim ’533 or Kim ’673 suggests the
claimed compound.
CONCLUSION
In summary:
Claims
Rejected
35 U.S.C. § References/Basis Affirmed Reversed
1, 2, 5–12, 15,
32, 33
103 Kim ’533 1, 2, 5–12,
32, 33
1, 2, 5–12, 15,
32, 33
103 Kim ’673 1, 2, 5–12,
32, 33
Overall
Outcome
1, 2, 5–12,
32, 33

REVERSED