Ex Parte Stefely et al

Board of Patent Appeals and Interferences

Jun 16, 2009

10327200 (B.P.A.I. Jun. 16, 2009)

UNITED STATES PATENT AND TRADEMARK OFFICE
____________

BEFORE THE BOARD OF PATENT APPEALS
AND INTERFERENCES
____________

Ex parte JAMES S. STEFELY and DANIEL C. DUAN
____________

Appeal 2009-003349
Application 10/327,200
Technology Center 1600
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Decided:1 June 16, 2009
____________

Before DONALD E. ADAMS, RICHARD M. LEBOVITZ, and
MELANIE L. McCOLLUM, Administrative Patent Judges.

ADAMS, Administrative Patent Judge.

DECISION ON APPEAL

1 The two-month time period for filing an appeal or commencing a civil
action, as recited in 37 C.F.R. § 1.304, begins to run from the decided date
shown on this page of the decision. The time period does not run from the
Mail Date (paper delivery) or Notification Date (electronic delivery).

Appeal 2009-003349
Application 10/327,200

This appeal under 35 U.S.C. § 134 involves claims 1-5 and 8-13. The
only remaining pending claims, claims 14-31 have been withdrawn from
consideration (App. Br. 3). We have jurisdiction under 35 U.S.C. § 6(b).

STATEMENT OF THE CASE
The claims are directed to a medicinal aerosol. Claims 1 and 4 are
illustrative:
1. A medicinal aerosol composition comprising:
a propellant selected from the group consisting of 1,1,1,2-
tetrafluoroethane, 1,1,1,2,3,3,3-heptafluoropropane, and a mixture
thereof;
an excipient comprising a compound of the structure
R1-(O-CH2-CH2)n-X; wherein X is selected from the group consisting
of: -C(O)OH; -S(O2)OH; -OS(O2)OH; -P(OH)2O; -OP(OH)2O;
-N(R2)(R2); -OC(R2)(R2)-C(O)-Z; -OC(O)-R2-C(O)-Z;
-O-R3-C(O)-Z; and -OC(O)CH(R3)-N(R2)(R2);
Z is selected from -OH; -N(R2)(R2); -NR-R2-NH-; an amino acid
residue; a peptide residue with from 2 to 8 amino acids; or a hydroxy
acid;
n is from 1 to 250;
R1 is methyl or ethyl;
[e]ach R2 is independently selected from hydrogen or linear, branched,
or cyclic hydrocarbon with 1 to 6 carbons; and
R3 is independently selected from hydrogen or linear, branched, or
cyclic hydrocarbon with 1 to 6 carbons, wherein R2 and R3 may
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optionally be connected together to form an alkylene bridge of from 2
to 4 carbons; and
a drug.

4. The medicinal aerosol composition of claim [1 wherein X is
-OC(R2)(R2)-C(O)-Z] wherein Z is an amino acid residue selected
from the group consisting of glycine, glycineamide, alanine, proline,
taurine, and sarcosine.

The Examiner relies on the following evidence:
Lederer et al. US 3,281,377 Oct. 25, 1966
Ono et al. US 5,342,940 Aug. 30, 1994
Duan et al. US 5,725,841 Mar. 10, 1998

The rejections presented by the Examiner are as follows:
1. Claims 1-3, 5, and 8-13 stand rejected under 35 U.S.C. § 103(a) as
unpatentable over the combination of Duan and Lederer.
2. Claim 4 stands rejected under 35 U.S.C. § 103(a) as unpatentable over
the combination of Duan, Lederer, and Ono.
We reverse.

PRINCIPLES OF LAW
“In proceedings before the Patent and Trademark Office, the
Examiner bears the burden of establishing a prima facie case of obviousness
based upon the prior art.” In re Fritch, 972 F.2d 1260, 1265 (Fed. Cir. 1992).
Obviousness requires a teaching or suggestion of all the elements in a claim
(CFMT, Inc. v. Yieldup Int’l Corp., 349 F.3d 1333, 1342 (Fed. Cir. 2003))
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and “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).

ISSUE

Would it have been prima facie obvious to include Lederer’s
polyethylene glycol carboxylic acid in Duan’s suspension aerosol drug
formulation?

FINDINGS OF FACT
FF 1. Duan teaches suspension “aerosol drug formulations” comprising
dispersing aids and “hydrofluorocarbon propellants” (Duan, col. 1, ll. 16-20
and col. 2, ll. 42-43).
FF 2. Duan’s preferred hydrofluorocarbon propellants are 1,1,1,2-
tetrafluoroethane, 1,1,1,2,3,3,3-heptafluoropropane, and a mixture thereof
(Duan, col. 8, ll. 37-42).
FF 3. There is no dispute on this record that Duan teaches
hydrofluorocarbon propellants within the scope of Appellants’ claimed
invention.
FF 4. Appellants’ Specification discloses that the term “drug” in the
claimed invention includes, inter alia, to antiallergics, analgesics,
bronchodilators, antihistamines, and antitussives (Spec. 5: 18-19).
FF 5. Duan teaches that “[s]uitable drugs for use in a formulation of . . .
[Duan’s] invention include any drug suitable for administration by inhalation
. . . include[ing, inter alia,] antiallergics, analgesics, bronchodilators,
antihistamines, [and] antitussives” (Duan, col. 8, ll. 22-25).
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FF 6. There is no dispute on this record that Duan teaches drugs within the
scope of Appellants’ claimed invention.
FF 7. Appellants’ Specification recognizes that “the use of polyethylene
glycol (PEG) as an excipient is known” in the art (Spec. 2: 11).
FF 8. Appellants disclose that “the usefulness of polyethylene glycol can
be improved if it is functionalized” (Spec. 2: 12-13). Specifically,
Appellants’ disclose
an excipient comprising a compound of the structure
R1-(O-CH2-CH2)n-X, and a drug. X is selected from the group
consisting of: -C(O)OH; -S(O2)OH; -OS(O2)OH; -P(OH)2O;
-OP(OH)2O; -N(R2)(R2); -OC(R2)(R2)-C(O)-Z;
-OC(O)-R2-C(O)-Z; -O-R3-C(O)-Z; and
-OC(O)CH(R3)-N(R2)(R2). Z is selected from –OH,
-N(R2)(R2); -NR-R2-NH-; an amino acid residue; a peptide
residue with from 2 to 8 amino acids; or a hydroxy acid. R1 is
methyl or ethyl. Each R2 is independently selected from
hydrogen or linear, branched, or cyclic hydrocarbon with 1 to 6
carbons. R3 is selected from hydrogen or linear, branched, or
cyclic hydrocarbon with 1 to 6 carbons, wherein R2 and R3 may
optionally be connected together to form an alkylene bridge of
from 2 to 4 carbons.

(Spec. 2: 14-23.)
FF 9. Appellants exemplify the use of “carboxylic acid functionalized
polyethyleneglycol” excipient (Spec. 8: 13).
FF 10. Duan teaches the use of polyethylene glycol as a dispersing aid (e.g.,
surfactant or excipient) (Duan, col. 5, ll. 31-34).
FF 11. The Examiner finds that Duan fails to teach a polyethylene glycol
with a carboxylic acid end group (Ans. 5).
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FF 12. Lederer teaches “[t]he polymerization on an industrial scale of vinyl
compounds, especially vinyl chloride, is advantageously carried out in
emulsion or aqueous suspension” (Lederer, col. 1, ll. 17-19).
FF 13. Lederer teaches that it is known to use “polyethers such as
polyethylene glycol carboxylic acid as emulsifiers for the emulsion
polymerization” (Lederer, col. 1, ll. 53-55).
FF 14. Lederer teaches that when pure polyethers are used as dispersants in
suspension polymerization a “strong formation of deposits occurs in the
polymerization vessel” (Lederer, col. 1, ll. 56-58). Lederer teaches that
“[t]he formation of deposits is undesired because it interferes, for example,
with the elimination of heat and leads to a contamination of the polymers”
(Lederer, col. 2, ll. 43-45). Thus Lederer teaches “a new class of
compounds of modified polyethers . . . particularly suitable for use as
dispersants for the suspension polymerization of vinyl compounds”
(Lederer, col. 1, ll. 59-62).
FF 15. Duan teaches that a myriad of “materials are known and disclosed
for use as dispersing aids in aerosol formulations. Suitability of materials,
however, is dependent on the particular drug and the propellant or class of
propellant used in the formulation” (Duan, col. 1, ll. 54-58; see Reply Br. 3).
In this regard, Duan teaches that “[i]t is sometimes difficult to dissolve
sufficient quantities of conventional surfactants in hydrofluorocarbon (HFC)
propellants” (Duan, col. 1, ll. 59-61; see Reply Br. 3).

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ANALYSIS
Claim 1:
Claim 1 is drawn to a medicinal aerosol composition. The claimed
composition comprises (1) a propellant, (2) a drug, and (3) an excipient.
There is no dispute on this record that Duan teaches a medicinal
aerosol composition that comprises (1) a propellant and (2) a drug within the
scope of Appellants’ claimed invention (FF 1-6). Further, while Duan
teaches the use of PEG as a dispersing agent, Duan does not teach the use of
polyethylene glycol with a carboxylic acid end group (FF 10-11).
The Examiner relies on Lederer to make up for this deficiency.
Specifically the Examiner states that Lederer “was merely used for the
general teaching that polyethylene glycol carboxylic acids can be used as
emulsifiers or surfactants” (Ans. 7). Stated differently, in the Examiner’s
view, the context in which Lederer used polyethylene glycol carboxylic acid
as an emulsifier or surfactant is unimportant – as long as Lederer teaches
that polyethylene glycol carboxylic acid is an emulsifier or surfactant one of
ordinary skill in the art would necessarily use it as an emulsifier or surfactant
in any composition (Cf. App. Br. 5 (“[t]he disclosure of carboxy
functionalized PEG in Lederer et al. is . . . in a functionally different context
and one skilled in the art would not have combined it with Duan et al. with
any reasonable expectation of success.”)).
According to the Examiner, because Lederer teaches that polyethylene
glycol carboxylic acid is a known emulsifier for the emulsion
polymerization of vinyl compounds (FF 12-13) “it would have been prima
facie obvious to a person of ordinary skill in the art, at the time the claimed
invention was made, to substitute . . . polyethylene glycol carboxylic acid
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[for polyethylene glycol] as the surfactant in” Duan’s suspension aerosol
drug formulations (Ans. 5). Why, because as the Examiner explains both
Lederer and Appellants “disclose the use of surfactants in suspensions” and
recognize that polyethylene glycol carboxylic acid has an effect on particle
size (Ans. 5). We are not persuaded.
The critical question here is why would a person of ordinary skill in
the art look to Lederer’s teaching of vinyl polymerization to determine the
effective constituents in a medicinal fluorocarbon based aerosol
composition? The Examiner failed to provide a satisfactory answer to that
question.
Duan teaches suspension aerosol drug formulations (FF 1). Lederer
describes that it was known to use polyethylene glycol carboxylic acid as a
dispersant for emulsion polymerization, a chemical polymerization process.
Lederer teaches that unsatisfactory results are obtained when polyethylene
glycol carboxylic acid is used in the polymerization of vinyl compounds in
suspension (FF 14). Further, Duan teaches that a myriad of “materials are
known and disclosed for use as dispersing aids in aerosol formulations.
Suitability of materials, however, is dependent on the particular drug and the
propellant or class of propellant used in the formulation” and that
conventional surfactants are sometimes difficult to dissolve in
hydrofluorocarbon propellants (FF 15). The Examiner has not provided
evidence that polyethylene glycol carboxylic acid, which was known to
cause deleterious effects when used as dispersant in a polymerization
process, would have been recognized as useful in aerosol drug formulations.
For the foregoing reasons we disagree with the Examiner’s assertion
that “one of ordinary skill in the art would have a reasonable expectancy of
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successfully producing a medicinal suspension aerosol formulation by
substituting in polyethylene glycol carboxylic acid to the instant
composition” (Ans. 5).

CONCLUSION OF LAW
It would not have been prima facie obvious to include Lederer’s
polyethylene glycol carboxylic acid in Duan’s suspension aerosol drug
formulation?
The rejection of claims 1-3, 5, and 8-13 under 35 U.S.C. § 103(a) as
unpatentable over the combination of Duan and Lederer is reversed.

Claim 4:
ISSUE
Does Ono make up for the deficiency in the combination of Duan and
Lederer?

FINDINGS OF FACT
FF 16. The Examiner relies on Ono to teach “chemically attaching
polyethylene glycol to proteins” (Ans. 6).

ANALYSIS
Claim 4 depends from claim 1 and further limits the Z substituent of
the excipient compound of the medicinal aerosol composition to a
compound selected from the group consisting of glycine, glycineamide,
alanine, proline, taurine, and sarcosine.
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The Examiner’s rationale appears to be that since Ono teaches
chemically attaching PEG to proteins, one of ordinary skill in the art would
have found it obvious to attach Lederer’s polyethylene glycol carboxylic
acid and use this polyethylene glycol carboxylic acid – protein complex in
Duan’s suspension aerosol drug formulation.
Appellants contend that Ono fails to make up for the deficiencies in
the combination of Duan and Lederer (App. Br. 6). For the reasons set forth
above, we agree.

CONCLUSION OF LAW
Ono fails to make up for the deficiency in the combination of Duan
and Lederer.
The rejection of claim 4 under 35 U.S.C. § 103(a) as unpatentable
over the combination of Duan, Lederer, and Ono is reversed.

REVERSED

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