Ex Parte Rosenberg et al

Board of Patent Appeals and Interferences

Sep 8, 2008

10343019 (B.P.A.I. Sep. 8, 2008)

UNITED STATES PATENT AND TRADEMARK OFFICE
__________

BEFORE THE BOARD OF PATENT APPEALS
AND INTERFERENCES
__________

Ex parte
JOERG ROSENBERG, GUNTHER BERNDL, JOERG NEUMANN,
and JOERG BREITENBACH
__________

Appeal 2008-3642
Application 10/343,019
Technology Center 1600
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Decided: September 8, 2008
__________

Before ERIC GRIMES, LORA M. GREEN, and JEFFREY N. FREDMAN,
Administrative Patent Judges.

GRIMES, Administrative Patent Judge.

DECISION ON APPEAL
This is an appeal under 35 U.S.C. § 134 involving claims to a process
for treating oral mycoses. The Examiner has rejected the claims as obvious.
We have jurisdiction under 35 U.S.C. § 6(b). We affirm.

Appeal 2008-3642
Application 10/343,019

BACKGROUND
“Itraconazol[e] … is known as an effective active ingredient for oral,
parenteral and topic[al] treatment of various types of my[c]oses” (Spec. 1).
“However, since itraconazole is almost insoluble in water (less than 1
µg/ml), bioavailability is a major problem. Many attempts have been made
to improve the bioavailability of …insoluble drug compounds. Among
them, solid dispersions of drug and hydrophilic polymers have been
suggested to enhance the solubility of the drug” (id.).
The Specification discloses “formulations and dosage forms for
application in the oral cavity for the treatment of my[c]oses, especially
my[c]oses of the oral cavity” (id. at 2).
DISCUSSION
1. CLAIMS
Claims 1-8 are on appeal. Claim 9 is also pending but has been
withdrawn from consideration by the Examiner (Appeal Br. 2).
Claims 1 and 2 are representative and read as follows:
Claim 1: A process for treatment of oral mycoses, said process
comprising
positioning in an oral cavity a solid dosage form comprising
itraconazole molecularly dispersed in a pharmaceutically acceptable matrix,
which is obtained by a melt-extrusion process to deliver an effective amount
of itraconazole directly to the oral cavity.

Claim 2: The process of claim 1, wherein the dosage form is in the
form of a lozenge.

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2. OBVIOUSNESS I
Claims 1 and 3-6 stand rejected under 35 U.S.C. § 103(a) as obvious
in view of Baert.1 The claims have not been argued separately and therefore
stand or fall together. 37 C.F.R. § 41.37(c)(1)(vii).
The Examiner relies on Baert as disclosing “a solid dispersion
comprising itraconarazole [sic] and a polymer (matrix) used in treatment of
fungal infection (mycoses),” with a dosage form that is “preferably a tablet”
(Answer 3). The Examiner also relies on Baert as disclosing
“pharmaceutical dosage forms for oral administration such as tablets and
capsules” and that other dosage forms are contemplated (id. at 4). The
Examiner reasons that the above cited teaching of Baert “encompasses any
dosage form” and thus suggests the limitation of delivering “an effective
amount of itraconazole directly to the oral cavity” (id.).
The Examiner finds that Baert “does not specifically teach a method
of treating oral mycoses,” but that it “teaches a method of treating fungal
(mycoses) infections in general” (id.), and that the teaching of treating
mycoses generally would have provided motivation to treat oral mycoses
specifically with a reasonable expectation of success (id.).
We conclude that the Examiner has set forth a prima facie case that
claim 1 would have been obvious to the ordinary artisan. Baert discloses
“novel pharmaceutical compositions of itraconazole which can be
administered to a mammal suffering from a fungal infection . . .
compris[ing] particles obtainable by melt-extruding a mixture comprising
itraconazole and an appropriate water-soluble polymer” (Baert, abstract).

1 Baert et al., WO 97/44014, Nov. 27, 1997.
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Baert also suggests that the novel compositions provide improved
bioavailability of itraconazole (id. at 1) and discloses that “[i]traconazole
…is a broadspectrum antifungal compound developed for oral, parenteral
and topical use” (id.).
We agree with the Examiner that it would have been prima facie
obvious to one of skill in the art at the time the invention was made to arrive
at the invention of claim 1 based on the teaching of Baert. Given the
disclosure in Baert that itraconazole is a broad spectrum antifungal
compound that can be administered both orally and topically, one of skill in
the art would have understood that mycoses, including oral mycoses, could
be treated topically by direct placement of the disclosed itraconazole
formulation.
Appellants argue that Baert “relates exclusively to the systemic
administration of itraconazole” and that Baert teaches away from the present
invention because it repeatedly stresses “the importance of swallowing their
dosage form, and go to great lengths to facilitate the swallowing of the
dosage form” (Appeal Br. 5). Appellants also argue that “[a]t the time the
present invention was made delivery of itraconazole directly to the oral
cavity had not been contemplated, and so a skilled artisan had no way to
know how to deliver an effective amount of itraconazole directly to the oral
cavity” (id. at 7).
We are not persuaded by this argument. It is true that Baert does not
expressly suggest the treatment of oral mycoses by positioning a dosage
form of itraconazole in the oral cavity, but the prior art need not expressly
suggest an invention in order to have made it obvious. “[T]he ‘motivation-
suggestion-teaching’ test asks not merely what the references disclose, but
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whether a person of ordinary skill in the art, possessed with the
understandings and knowledge reflected in the prior art, and motivated by
the general problem facing the inventor, would have been led to make the
combination recited in the claims.” In re Kahn, 441 F.3d 977, 988 (Fed. Cir.
2006). See also KSR Int’l Co. v. Teleflex Inc., 127 S. Ct. 1727, 1741 (2007)
(The obviousness analysis “can take account of the inferences and creative
steps that a person of ordinary skill in the art would employ.”); DyStar
Textilfarben GmbH & Co. Deutschland KG v. C.H. Patrick Co., 464 F.3d
1356, 1367 (Fed. Cir. 2006) (The “suggestion test is in actuality quite
flexible and not only permits, but requires, consideration of common
knowledge and common sense.”).
While Baert does not specifically disclose the treatment of oral
mycoses directly, Baert discloses that its dosage form has improved
bioavailability and that itraconazole is known for the topical treatment of
mycoses. Given the disclosure that itraconazole is known to be safe for oral
administration and that mycoses can be treated topically with itraconazole,
one of skill in the art, faced with the problem of oral mycoses, would have
been predictably led to the solution of directly delivering itraconazole to oral
mycoses using a dosage form made using known tableting methods, leading
to the method of claim 1.
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3. OBVIOUSNESS II
Claims 2, 7, and 8 stand rejected under 35 U.S.C. § 103(a) as obvious
in view of Baert and Ansel.2 The claims have not been argued separately
and therefore stand or fall together. 37 C.F.R. § 41.37(c)(1)(vii).
The Examiner relies on Baert as discussed above, but finds that Baert
“does not teach a dosage form of a lozenge, or a tablet for buccal,
sublingual, gingival, or palatinal application” (Answer 5). The Examiner
finds that Ansel discloses that “tablet types include buccal and sublingular
tablets” (Answer 5). The Examiner also relies on Ansel as disclosing that
“lozenges are solid dosage forms containing a medicinal agent and are also
intended for the oral cavity” (id.).
The Examiner concludes that it “would have been obvious to a person
of ordinary skill in the art at the time the invention was made to interchange
between tablet types because Baert et al. teaches the composition in a tablet
form and Ansel et al. teaches various tablet forms are within the purview of
a skilled artisan” (id.). The Examiner reasons that motivation to combine
the reference is provided by Ansel’s teaching that “buccal and sublingular
tablets ‘enable the oral absorption of drugs that are destroyed by the gastric
juice and/or are poorly absorbed from the gastrointestinal tract’” and that
“lozenges ‘are intended to be slowly dissolved in the oral cavity’ for
localized or systematic effects” (id. at 5, citing Ansel 202).
We agree with the Examiner’s reasoning and conclusion.
Appellants argue that “a person of ordinary skill in the art had no
apparent reason to treat oral mycoses by applying in an oral cavity a solid

2 Ansel et al., “Pharmaceutical Dosage Forms and Drug Delivery Systems,”
202-203 (7th ed., Lippincott, Williams & Wilkins, 1999).
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dosage form comprising itraconazole molecularly dispersed in a
pharmaceutically acceptable matrix, which is obtained by a melt-extrusion
process,” and thus “there was no apparent reason for the skilled person to
adopt the buccal or sublingual tablets of Ansel et al., even though these
forms were known” (Appeal Br. 9).
We are not persuaded by this argument for the reasons set forth above.
SUMMARY
The Examiner’s rejections are supported by a preponderance of the
evidence of record. We therefore affirm the rejection of claims 1-8 under
35 U.S.C. § 103(a).
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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