Ex Parte Sas et al

Board of Patent Appeals and Interferences

Oct 20, 2008

10861768 (B.P.A.I. Oct. 20, 2008)

UNITED STATES PATENT AND TRADEMARK OFFICE
__________

BEFORE THE BOARD OF PATENT APPEALS
AND INTERFERENCES
__________

Ex parte BENEDIKT SAS, JOHAN VAN DER EYCKEN,
JOHAN VAN HEMEL, PETRA BLOM, JAN VANDENKERCKHOVE,
and BART RUTTENS
__________

Appeal 2008-3813
Application 10/861,768
Technology Center 1600
__________

Decided: October 20, 2008
__________

Before DEMETRA J. MILLS, RICHARD M. LEBOVITZ, and
JEFFREY N. FREDMAN, Administrative Patent Judges.

FREDMAN, Administrative Patent Judge.

DECISION ON APPEAL
This is an appeal under 35 U.S.C. § 134 involving claims to
compounds with antimicrobial and cytostatic activity, which the Examiner
has rejected as failing to comply with the written description requirement.
We have jurisdiction under 35 U.S.C. § 6(b). We affirm-in-part.
Appeal 2008-3813
Application 10/861,768

Background
“The medical community is constantly seeking new drugs with which
to treat a variety of diseases, infections, and other health issues” (Spec. 1:10-
11). The Specification discloses that “[m]acrolide and ketolide
antimicrobials are all chemically related in that they consist of a macrocyclic
lactone, the majority of them also containing amino sugar and/or neutral
sugar moieties.” (Spec. 7:24-26). The Specification also notes that
“macrolides are active mainly against gram-positive bacteria
(Staphylococcus, Streptococcus and Diplococcus) and possess only limited
activity against gram-negative bacteria (e.g. Neisseria gonorrhoea, N.
Meningitis, etc.). In general, polyene macrolides have very low or no impact
on eukaryotic cells” (Spec. 8:2-5).
Appellants teach “synthesized macrolide and ketolide compounds that
have anti-bacterial, anti-fungal, anti-viral, anti-protozoal, or anti-tumor
activities” (Spec. 9:20-22).
Statement of the Case
The Claims
Claims 1, 15, and 19 are on appeal.1 We will focus on claims 1 and
15, which are representative and read as follows:

1 The Appeal Brief states that claims 1, 15, and 17-19 are rejected in the
final rejection, but in fact, only claims 1, 15, and 19 are rejected (see Final
Rejection 2). Claims 17 and 18 are objected to and are therefore not subject
to this appeal (see Final Rejection 3).
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1. A compound of the formula:

wherein
R1 is -H, -Ph, -PhS, -All, or -Bn;
R2 is, -H, -Me, or -Bn;
R3 is, -H, -Me, or -Bn; and
R4 and R5 are each –OH.

15. A compound of the formula:

wherein, R1 is selected from of -H, -aryl, and -thioaryl;
R2 and R3 are selected from the group consisting of -alkyl and -aryl;
R4 is selected from the group consisting of -H, alkyl and functionalised alkyl
groups;
X is selected from the group consisting of O, N3 and NH; and
R5 is selected from the group consisting of alkyl and functionalised alkyl
groups.

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Application 10/861,768

The rejections as presented by the Examiner are as follows:
Claims 1, 15, and 19 stand rejected under 35 U.S.C. § 112, first
paragraph, as failing to comply with the written description requirement
(Ans. 3).
35 U.S.C. § 112, first paragraph Written Description rejection
The Examiner argues that “[t]here is no disclosure of compound
wherein R4 and R5 are alkyls. There is no disclosure for the terminology
‘functionalised alkyl groups’” (Ans. 4). The Examiner contends that “the
disclosure of Bn does not support the term ‘aryl’ and the disclosure of PhS
does not provide support for the term ‘thioaryl’” (Ans. 5).
The Examiner argues that the “claims as originally filed and which
have been patented (see U.S. Pat. No. 7,138,531) are limited to compounds
wherein R4 and R5 form a ring. The compounds of claims 1 and 19 are
directed to compounds wherein R4 and R5 are both hydroxy groups” (Ans.
6). The Examiner further contends regarding claim 15 that “Appellant
argues that the compounds recited in claim 15 are intermediates [o]f
compounds recited in claim 1 as originally filed . . . the disclosure of a final
product does not provide support for the intermediates now claimed, which
have not been specifically disclosed in the specification as originally filed”
(Ans. 6).
Appellants argue that the “Examiner in the present application has
presented no evidence or reasons supporting why persons skilled in the art
would not recognize in the disclosure a description of the invention defined
in the claims. There is only the conclusory statement that there is no
disclosure of some of the claimed compounds in the specification as
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originally filed” (App. Br. 6). Appellants contend that nine compounds were
disclosed which “are intermediates used in the synthesis of the compounds
that were claimed in claim 1 as originally filed” (App. Br. 6).
Appellants also argue that regarding claim 15 that “[o]ne skilled in the
art would certainly be able to use the genus described and claimed by
Appellant [sic], along with the disclosure of how to make examples of the
genus to make each species contained within that genus” (Rep. Br. 5).
In view of these conflicting positions, we frame the written
description issue before us as follows:
Does the Specification provide an adequate written description of the
compounds of claims 1 and 15?
Findings of Fact (FF)
1. The originally filed2 claim 1 is reproduced below:
1. A compound of the formula:

wherein
Rl is -H, -SPh, -Ph, -PhS, -All, or -Bn;
R2 is -H, -Et, -All, -Me, or -Bn;
R3 is -H, -Et, -Me, -All, or-Bn; and
R4 and R5 form a ring and are -carbamate-C6-alkyl-ether-C4-alkenyl-ether-,
-ester-C6-alkenyl-ester-, -ester-C6-alkyl-ester-, -ether-C8-alkenyl-ether-, -

2 A preliminary amendment amending claim 1 was filed on June 4, 2004, but
is not mentioned in the Appellants’ Declaration as per 37 C.F.R.
§ 1.63(d)(1)(iii).
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ester-C6-alkenyl-amide-, -ether-C7- 10-alkenyl-amide-, -ester-C 10-alkenyl-
ester-, or -ester-C18-alkenyl-ester-, or -OCH(Ph)CH20- or a
pharmaceutically active derivative thereof.

2. The Specification teaches macrolides where R4 and R5 are both
–OH groups, in particular KPE00001011 and KPE00001020 (see Spec. 14).
3. The Specification showed that KPE00001011 and
KPE00001020 had anti-bacterial activity (see Spec. 20, Table 4).
4. The Specification showed that KPE00001011 had anti-fungal
activity while KPE00001020 had minimal anti-fungal activity (see Spec. 21,
Table 5).
5. The Specification teaches that “[t]here is a wide range of
possible variations of the different substituents R1, R2 and R3, such as H,
alkyl, aryl, O-aryl, S-aryl, OH, OR, halogens, -OOCR, COOR, -COR etc.”
(Spec. 9:6-8).
6. In Table 1, titled “Examples of Described Molecules,” the
Specification does not teach any compounds with the R4 and R5 groups of
instant claim 15 (see Spec. 11-15).
7. Appellants identify “twelve distinct compounds that fall within
claim 15 in the specification as originally filed” which are “Compounds 2.3,
6.13, 7.3, 7.9, 7.10, 7.25, 7.45, 7.13, 7.14, 7.15, 7.33, and 7.42” (App. Br. 7).
8. The Specification teaches that compound 2.3 is an intermediate
on the pathway to the synthesis of KPE00001056 (see Figs. 4, 5). Similarly,
compounds 6.13, 7.3, 7.9, 7.10, 7.25, 7.45, 7.13, 7.14, 7.15, 7.33 and 7.42
are all intermediates in the synthesis of final products (see Figs. 6-15).
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Discussion of the 35 U.S.C. § 112, first paragraph Written Description
rejection
The first paragraph of 35 U.S.C. § 112 states:
The specification shall contain a written description of the invention, and of
the manner and process of making and using it, in such full, clear, concise,
and exact terms as to enable any person skilled in the art to which it pertains,
or with which it is most nearly connected, to make and use the same.

( 35 U.S.C. § 112, ¶ 1 (1994)). In a written description case, the “primary
consideration is factual and depends on the nature of the invention and the
amount of knowledge imparted to those skilled in the art by the disclosure.”
Union Oil Co. of Cal. v. Atlantic Richfield Co., 208 F.3d 989, 996 (Fed. Cir.
2000) (quoting In re Wertheim, 541 F.2d 257, 262 (CCPA 1976)). The
written description requirement does not dictate that the applicant describe
the invention exactly. Rather, what is required is that, as of the filing date,
the inventor conveys with reasonable clarity to those skilled in the art that
the inventor was in possession of the subject matter claimed. See Vas-Cath
Inc. v. Mahurkar, 935 F.2d 1555, 1563-64 (Fed. Cir. 1991).
Claims 1 and 19
We agree with the Appellants that the instant Specification describes
the genus of compounds of claims 1 and 19. The instant claim 1 recites
Markush groups which differ from the originally filed claim 1 for R1, R2,
and R3 only in that the original claim allowed R1 to be SPh, allowed R2 to
be Et or All, and allowed R3 to be ET or All (FF 1, 2). Claim 19 claims a
smaller subgenus of claim 1 (see Claim 19). The Specification further
specifically discusses a variety of alternatives for R1, R2, and R3 (FF 5).
The Specification describes several macrolides in which R4 and R5 are OH
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groups, including KPE00001011 and KPE00001020 (FF 2). The
Specification tests the anti-bacterial and anti-fungal activity of the
macrolides in which R4 and R5 have OH groups (FF 3, 4).
We are not persuaded by the Examiner’s argument that the
“specification, as originally, filed, fails to disclose the genus now claimed.
Since the compounds originally claimed and now patented are patentably
distinct compounds from those now encompassed by claims 1 and 19, it
cannot be said that the disclosure of a final product provides support for all
the intermediates” (Ans. 6). First, compounds with an OH group at R4 and
R5 were tested as final products (FF 3,4) and the Specification expressly
listed the members of the R1, R2, and R3 groups (FF 1, 5). In our opinion,
an ordinary practitioner, reviewing tables 1, 4, and 5 of the Specification,
would have recognized that Appellants were in possession of the subgenera
disclosed in claims 1 and 19.
We conclude that claims 1 and 19 satisfy “the requirement that the
patent specification set forth enough detail to allow a person of ordinary skill
in the art to understand what is claimed and to recognize that the inventor
invented what is claimed.” University Of Rochester v. G.D. Searle & Co.,
358 F.3d 916, 928 (Fed. Cir. 2004).
Claim 15
The central issue for claim 15 is that the claim is drawn to a subgenus
of intermediates which differ from compounds in the originally filed claim
with entirely different functional groups at positions R2, R3, R4 and R5 and
only one common functional group at position R1. A subissue is the
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absence of any teaching in the Specification of “functionalized alkyl
groups”.
We agree with the Examiner that the instant Specification does not
describe the genus of compounds of claim 15. The instant claim 15
encompasses R1, R2, R3, R4 and R5 members which were not present in the
original claim (FF 1). While the Specification contemplated a variety of R
groups, “functionalyzed alkyl groups” were not included in the disclosure
(FF 5). We find that the genus of compounds contemplated by the inventor
were the final products shown in Table 1. The issue before us is whether a
disclosure of twelve particular intermediates (FF 7, 8) can support claim 15,
which is generic in some substituents and narrow in other substituents.
In Ruschig, the claims were drawn to a compound with three moieties,
R, R1 and R2, with a myriad of different chemical compounds from which
to choose each of the variables. See In re Ruschig, 379 F.2d 990, 993
(CCPA 1967). Ruschig noted that “the general disclosure of the application
encompasses something like half a million possible compounds.” Id.
Ruschig concluded that,
It is not our view that a disclosure such as that to be found in
the formula and words of claim 2, above, amounts to a
disclosure, sufficient to support a specific claim, of every
compound a skilled chemist can see is within the scope of that
claim. Specific claims to single compounds require reasonably
specific supporting disclosure and while we agree with the
appellants, as the board did, that naming is not essential,
something more than the disclosure of a class of 1000, or 100,
or even 48, compounds is required. Surely, given time, a
chemist could name (especially with the aid of a computer) all
of the half million compounds within the scope of the broadest
claim, which claim is supported by the broad disclosure. This
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does not constitute support for each compound individually
when separately claimed.

In re Ruschig, 379 F.2d 990, 993, 994 (CCPA 1967).
Ruschig specifically addressed the argument that “one skilled in the art could
see that ‘if n-butylamine is a reactant, then ethylamine, n-propylamine, etc.,
are also possible reactants.’ We do not see that this guides one to the use of
n-propylamine.” Id. at 994.
Applying Ruschig to the instant facts, we are not persuaded by
Appellants’ contention that based upon the compounds in the original claim
1 and the twelve specific intermediates disclosed in the Specification, “those
skilled in the art would certainly recognize that intermediates of those
compounds must also have been in the possession of Applicant” (App. Br.
8). We find that there is simply no guidance in the Specification which
would have led the skilled artisan to recognize the subgenus of claim 15,
with the specific selection of R1, R2, R3, R4, and R5 given, when no
specific blazemarks suggested this subgenus. We think that this situation is
like the metaphor in Ruschig, where
It is no help in finding a trail or in finding one's way through
the woods where the trails have . . . not yet been made . . . 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, 995 (CCPA 1967).
While we recognize that Appellant has shown specific intermediates
in the Specification, there is no indication in the Specification to expand the
specific intermediates to form generic intermediates. Additionally, as we
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have already noted, we find no specific teaching or support in Appellants’
Specification for selecting a specific subgenus of R1, R2, R3, R4, and R5
groups. See Fujikawa v. Wattanasin, 93 F.3d 1559, 1571 (Fed. Cir. 1996)
(“In finding that Wattanasin's disclosure failed to sufficiently describe the
proposed sub-genus, the Board again recognized that the compounds of the
proposed count were not Wattanasin's preferred, and that his application
contained no blazemarks as to what compounds, other than those disclosed
as preferred, might be of special interest. In the absence of such blazemarks,
simply describing a large genus of compounds is not sufficient to satisfy the
written description requirement as to particular species or sub-genuses”).
We conclude that the instant situation is analogous to that in
Fujikawa, since there are no blazemarks to select the specific subgenus
claimed. Appellants’ claim 15 encompasses a large subgenus with a large
number of species, since each of the R groups includes generic side groups
such as “aryl”, “thioaryl”, “alkyl” and “functionalised alkyl groups.”
However, there is no indication in the Specification that any such subgenus
was contemplated as the invention. We conclude that the written description
requirement is not satisfied for the subgenus of intermediates by a showing
of twelve specific intermediates and a broad generic original claim to the
final products.
We are not persuaded by Appellants argument that the “position of the
Examiner is also suspect due to certain erroneous assumptions made in
support of the rejection of claim 15” (App. Br. 8). While we agree with
Appellants that there is clear support for “aryl,” “benzyl,” “thioaryl” and
“alkyl” generically (App. Br. 8), we do not find specific support for a
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subgenus of the intermediate compounds where specific selections of “aryl”
or “alkyl” are made. For example, claim 15 requires R1 to be selected from
the group of H, aryl and thioaryl, while R2 and R3 are selected from the
group of alkyl and aryl (see Claim 15). Appellants have identified no
support in the Specification which would suggest limiting R1 so that it does
not include alkyl or functionalized alkyl groups, or limiting R2 and R3 so
that they do not include thioaryl or H or functionalized alkyl groups. The
Specification does not provide any reason to exclude OR, halogens, -OOCR,
COOR, -COR groups which are also taught (FF 5). We conclude that the
specific subgenus of claim 15 lacks descriptive support from the
Specification.
We also agree with the Examiner that there is not support for
“functionalized alkyl groups”, which Appellant does not seem to traverse
(Ans. 4).
In view of the above we do not find that inventor has conveyed with
reasonable clarity to those skilled in the art that the inventor was in
possession of the subject matter claimed in claim 15. We affirm the
rejection of claim 15 under 35 U.S.C. § 112, first paragraph, written
description.
CONCLUSION
In summary, we affirm the rejection of claim 15 under 35 U.S.C.
§ 112, first paragraph, written description.
We reverse the rejection of claims 1 and 19 under 35 U.S.C. § 112,
first paragraph, written description.
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No time period for taking any subsequent action in connection with
this appeal may be extended under 37 C.F.R. § 1.136(a)(1)(iv)(2006).
AFFIRMED-IN-PART

clj

KENT A. HERINK
THE FINANCIAL CENTER
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