Ex Parte West et al

Patent Trial and Appeal Board

Dec 21, 2016

11761843 (P.T.A.B. Dec. 21, 2016)

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.
11/761,843 06/12/2007 Leslie George West 1410-77481-US 1701
48940 7590 12/21/2016
FITCH EVEN TAB IN & FLANNERY, LLP
120 SOUTH LASALLE STREET
SUITE 1600
CHICAGO, IL 60603-3406
EXAMINER
GREENE, IVAN A
ART UNIT PAPER NUMBER
1619
MAIL DATE DELIVERY MODE
12/21/2016 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 LESLIE GEORGE WEST, NICOLE LEE WINDSOR,
ANILKUMAR GANAPATI GAONKAR,
NATHAN V. MATUSHESKI, NAM-CHEOL KIM,
CATHY JEAN LUDWIG, and LESLIE LEWIS LAWRENCE1
Appeal 2015-005849
Application 11/761,843
Technology Center 1600
Before MELANIE L. McCOLLUM, RYAN H. FLAX, and KRISTI L. R.
SAWERT, Administrative Patent Judges.
McCOLLUM, Administrative Patent Judge.
DECISION ON APPEAL
This is an appeal under 35 U.S.C. § 134 involving claims to an
enteric-coated composition. The Examiner has 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 Kraft Foods Group Brands
LLC (App. Br. 3).
Appeal 2015-005849
Application 11/761,843
STATEMENT OF THE CASE
Claims 15—24 and 30-35 are on appeal (App. Br. 5 & 23).2 Claims 15
and 20 are representative and read as follows:
15. An enteric-coated chemoprotectant precursor composition
comprising:
a chemoprotectant precursor composition including
(1) about 0.5 to about 50 weight percent glucosinolate;
(2) about 0.5 to about 50 weight percent beta-thioglucosidase; and
(3) about 1 to about 99 weight percent composition comprising
coating excipient and optional diluent, and
wherein the chemoprotectant precursor composition is encapsulated
with enteric coating.
20. The enteric-coated chemoprotectant precursor composition of
claim 15, wherein the enteric coating is selected from the group consisting of
shellac, calcium alginate, zein, fatty acids, fats, or a combination thereof.
Claims 15—19, 21—24, and 30-34 stand rejected under 35 U.S.C.
§ 103(a) as obvious over Omary3 in view of Cortesi,4 Fahey,5 Ashurst,6 and
Li7 (Ans. 2-3).
Claims 20 and 35 stand rejected under 35 U.S.C. § 103(a) as obvious
over Omary in view of Cortesi, Fahey, Ashurst, Li, and Patel8 (Ans. 9).
2 Claims 36 and 37 have been canceled (Ans. 2).
3 Omary et al., US 6,436,450 Bl, Aug. 20, 2002.
4 Rita Cortesi et al., Hydroxy Propyl Methyl Cellulose Phthalate (HPMCP)
Microparticles for Enteric Delivery of Glucosinolate Derived Products from
Cruciferous Vegetable, 12 Minerva Biotec 293—300 (2000).
5 Fahey, US 2002/0151505 Al, Oct. 17, 2002.
6 Ashurst, WO 2006/102236 Al, Sept. 28, 2006.
7 Xian Li & Mosbah M. Kushad, Purification and Characterization of
Myrosinase from Horseradish (Armoracia rusticana) Roots, 43 Plant
Physiology and Biochemistry 503-511 (2005).
8 Patel et al., US 2003/0180352 Al, Sept. 25, 2003.
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Application 11/761,843
ISSUE
With regard to both grounds of rejection, the only issue raised by
Appellants is whether the Examiner has set forth a prima facie case that it
would have been obvious to encapsulate Omary’s composition with an
enteric coating?
FINDINGS OF FACT
1. The Specification discloses: “The present invention provides
enteric-coated glucosinolate and beta-thioglucosidase enzyme particles ....
Preferably, the glucosinolates are glucoraphanin and the beta-
thioglucosidase enzymes are myrosinase.” (Spec. 1 8.)
2. In describing the prior art, Omary “discloses a dietary
supplement containing a brassica vegetable and an exogenous source of
myrosinase enzyme” and states that the supplement “contains pre-formed
isothiocyanates such as sulforaphane rather than glucosinolates,” but that
“pre-formed isothiocyanates are not stable compounds” and “can degrade
over time, thereby losing their beneficial biological activity” (Omary, col. 1,
11. 21-29).
3. Omary discloses a “composition includ[ing] at least one
processed dehydrated brassica vegetable containing glucosinolates and
endogenous myrosinase enzyme” {id. at Abstract).
4. Omary also discloses that, “[w]hen the brassica vegetable
powder is introduced to an aqueous environment (for example, when
ingested by humans), the endogenous myrosinase enzyme promotes the
conversion of the glucosinolates (such as glucoraphanin) to biologically
useful isothiocyanates (such as sulforaphane)” {id. at col. 5,11. 3—8).
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Application 11/761,843
5. Cortesi “describes the production and characterization of
biodegradable microparticles containing glucosinolate hydrolysis products,
designed for enteric delivery” (Cortesi, Abstract).
6. Cortesi discloses:
[IJntestinal drug delivery has been proposed since [it] provides a
number of advantages with respect to conventional oral
administration. For instance, colon environment (i.e. pH and
degradative enzymes) is usually less aggressive for labile drugs
than those of stomach and small intestine. Moreover transit time
through the colon is longer with respect to that of other portions
of the gastrointestinal tract. Finally, it should be underlined that
some pathologies require site-specific drug delivery to the colon.
(Id. at 293 (footnote omitted).)
7. Cortesi also discloses that “[mjicroparticles made of enteric
resistant polymers have been used to prevent drug release to the stomach and
to the upper small intestine” (id.).
8. In addition, Cortesi discloses that the “biological activity shown
by glucosinolates (GLs) and their derived products, has recently increased its
importance due to their possible protective activity against intestine cancer”
(id. at 294).
9. Cortesi also discloses:
When myrosinase and GLs react together after cell disruption,
they result in the production of D-glucose and a series of
different compound[s] depending on the substrate and the
reaction condition such as pH, temperature and substrate
structure. In this respect, at neutral pH and temperature above
25°C, the formation of isothiocyanates is favoured; whilst using
a protonation mechanism and low pH, the main degradation
products are nitriles.
(Id. (footnotes omitted).)
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10. In addition, Cortesi discloses that the pH rises to neutral in the
jejunum of the gastrointestinal tract (id. at Fig. 1).
11. Cortesi also discloses that the “antiproliferative activity of GLs
contained in cruciferous vegetables is attributed to their enzymatic
breakdown products such as isothiocyanate and/or nitriles generated after in
vivo metabolization by endogenous or commensal microflora enzymes” (id.
at 295 (footnote omitted)).
12. In addition, Cortesi discloses that “in general nitriles are
considerably less potent than the corresponding isothiocyanates in inhibiting
cancer cell growth” (id.).
13. Li discloses:
Recent clinical studies, using human volunteers and laboratory
animals, have shown that the bioavailability and absorption of
isothiocyanates from raw Brassica vegetables is much greater
than that from cooked ones in which myrosinase has been
inactivated, suggesting that plant myrosinase is more efficient in
breaking down glucosinolates than gastrointestinal microflora
myrosinase.
(Li 503.)
ANALYSIS
Omary discloses a composition comprising glucosinolate and beta-
thioglucosidase (myrosinase enzyme) (Finding of Facts (FF) 1 & 3). Cortesi
“describes the production and characterization of biodegradable
microparticles containing glucosinolate hydrolysis products, designed for
enteric delivery” (FF 5). In view of the above findings of fact, we conclude
that the Examiner has set forth a prima facie case that it would have been
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obvious to encapsulate Omary’s composition with an enteric coating
(Ans. 8; see also Final Act. 13—14).
In particular, Cortesi discloses that the “antiproliferative activity of
GLs contained in cruciferous vegetables is attributed to their enzymatic
breakdown products such as isothiocyanate and/or nitriles generated after in
vivo metabolization by endogenous or commensal microflora enzymes”
(FF 11). However, Li discloses that plant myrosinase may be “more
efficient in breaking down glucosinolates than gastrointestinal microflora
myrosinase” (FF 13). Cortesi also discloses that “in general nitriles are
considerably less potent than the corresponding isothiocyanates in inhibiting
cancer cell growth” (FF 12). In addition, Cortesi discloses:
When myrosinase and GLs react together after cell disruption,
they result in the production of D-glucose and a series of
different compound[s] depending on the substrate and the
reaction condition such as pH, temperature and substrate
structure. In this respect, at neutral pH and temperature above
25°C, the formation of isothiocyanates is favoured; whilst using
a protonation mechanism and low pH, the main degradation
products are nitriles.
(FF 9.) Cortesi also discloses that the pH rises to neutral in the jejunum of
the gastrointestinal tract (FF 10). In view of these teachings, we conclude
that the Examiner has set forth a prima facie case that “the reaction of the
myrosinase and glucosinolate in the colon would have favored the
production of more potent anti-cancer isothiocyanates (over the nitriles)”
(Ans. 8).
In addition, Cortesi discloses that the “biological activity shown by
the glucosinolates . . . and their derived products, has recently increased its
importance due to their possible protective activity against intestine cancer”
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(FF 8). Moreover, Cortesi discloses that “intestinal drug delivery . . .
provides a number of advantages with respect to conventional oral
administration,” including “site-specific drug delivery to the colon” (FF 6).
Cortesi also discloses that “[mjicroparticles made of enteric resistant
polymers have been used to prevent drug release to the stomach and to the
upper small intestine” (FF 7). In view of these teachings, we conclude that
the Examiner has set forth a prima facie case that “an enteric composition
comprising glucoraphanin and myrosinase would have delivered the active
agent (the isothiocyanate sulforaphane) to the site of action (the intestine)
increasing the efficacious action of the drug” (Ans. 8).
Appellants argue:
Cortesi et al. describe compositions containing the reaction end
products (not a precursor (e.g., glucosinolate) and enzyme (e.g.,
beta-thioglucosidase)). The Examiner utilizes Cortesi et al. to
provide motivation to deliver a substrate and enzyme in an
enteric-coating even though this is exactly what Cortesi et al. do
not do. If in view of all of Cortesi et al.’s teachings it was so
obvious that providing an enteric composition comprising both
glucosinolates and beta-thioglucosidases would have been
advantageous, then it is very surprising that Cortesi et al. took
the very opposite approach and prepared compositions with
enteric-coated reaction end products.
(App. Br. 17.) We are not persuaded.
We understand that Cortesi “describes the production and
characterization of biodegradable microparticles containing glucosinolate
hydrolysis products” (FF 5). However, Omary discloses a composition
comprising glucosinolate and beta-thioglucosidase (myrosinase enzyme)
(FF 1 & 3). In addition, for the reasons discussed above, we agree with the
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Examiner that Cortesi provides reasons for encapsulating Omary’s
composition with an enteric coating.
Appellants also argue that “one of ordinary skill in the art would have
no reason to look to Cortesi et al. when considering any modification of
Omary et al. because Omary et al. already allegedly solves the problem that
the Final Action suggests is the reason to look to Cortesi et al. in the first
place” (App. Br. 18). We are not persuaded.
The Examiner does state that it “would have been prima facie obvious
. . . to produce an enteric release formulation comprising a glucosinolate
substrate and a myrosinase enzyme because the glucosinolate-myrosinase
product would have been more stable than a product containing pre-formed
isothiocyanates, as suggested by OMARY” (Ans. 8). However, it is clear
that this statement reflects a reason one of ordinary skill in the art would
have used the composition of Omary rather than the end products of Cortesi.
As discussed above, the Examiner provides other persuasive reasons why
one of ordinary skill in the art would have encapsulated Omary’s
composition with an enteric coating (id.).
In addition, Appellants argue that “it can only be concluded that
improper hindsight was used to render the pending claims obvious” (App.
Br. 20). We are not persuaded. Instead, for the reasons discussed above, we
conclude that the Examiner has provided reasons, from the prior art, that one
of ordinary skill in the art would have encapsulated Omary’s composition
with an enteric coating (Ans. 8).
With regard to claim 20, Appellants additionally argue that “Patel et
al. do not describe the combination of an enzyme and its substrate in an
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enteric-coated composition” (App. Br. 22). However, Appellants fail to
adequately explain why the other applied references fail to suggest this.
CONCLUSION
The evidence supports the Examiner’s conclusion that the applied
references suggest encapsulating Omary’s composition with an enteric
coating. We therefore affirm the obviousness rejections of claims 15 and 20.
Claims 16—19, 21—24, and 30-34 fall with claim 15 and claim 35 falls with
claim 20. 37 C.F.R. § 41.37(c)(l)(iv).
TIME PERIOD FOR RESPONSE
No time period for taking any subsequent action in connection with
this appeal may be extended under 37 C.F.R. § 1.136(a).
AFFIRMED
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