Ex Parte Babcock et al

Board of Patent Appeals and Interferences

May 9, 2012

10636834 (B.P.A.I. May. 9, 2012)

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.
10/636,834 08/05/2003 Walter C. Babcock 0003.0616/PC11847A 9891
152 7590 05/09/2012
CHERNOFF, VILHAUER, MCCLUNG & STENZEL, LLP
601 SW Second Avenue
Suite 1600
PORTLAND, OR 97204-3157
EXAMINER
FUBARA, BLESSING M
ART UNIT PAPER NUMBER
1613
MAIL DATE DELIVERY MODE
05/09/2012 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 BOARD OF PATENT APPEALS
AND INTERFERENCES
__________

Ex parte WALTER C. BABCOCK, WILLIAM B. CALDWELL,
MARSHALL D. CREW, DWAYNE T. FRIESEN, RAVI M. SHANKER,
and DANIEL T. SMITHEY
__________

Appeal 2011-011726
Application 10/636,834
Technology Center 1600
__________

Before ERIC GRIMES, FRANCISCO C. PRATS, and
STEPHEN WALSH, Administrative Patent Judges.

WALSH, Administrative Patent Judge.

DECISION ON APPEAL
This is an appeal under 35 U.S.C. § 134(a) from the rejection of
claims directed to a composition comprising a low-solubility drug and a
concentration-enhancing polymer. The Patent Examiner rejected the claims
for obviousness. We have jurisdiction under 35 U.S.C. § 6(b). We reverse.
Appeal 2011-011726
Application 10/636,834

2
STATEMENT OF THE CASE
The invention is related to “pharmaceutical compositions of a drug in
a semi-ordered state and a polymer that improves the stability of the drug
and enhances the concentration of the drug in a use environment.” (Spec. 1,
ll. 5-7.) According to the Specification, the compositions are “formed by
controlling the rate at which drug is converted from a disordered state to a
semi-ordered state. Generally, the mobility of drug in the disordered state is
temporarily increased by providing heat or a mobility-enhancing agent or
both, such that the drug converts relatively rapidly to the semiordered state.”
(Id. at 5, ll. 10-14.)
Claims 1, 2, 4, 6-9, 11, 21, and 23-27 are on appeal. Claim 1 is
representative and reads as follows:
1. A composition comprising:
(a) a solid comprising a low-solubility drug and a concentration-
enhancing polymer;
(b) said concentration-enhancing polymer being present in said
composition in a sufficient amount so that said composition provides
enhanced concentration of said drug in a use environment relative to a first
control composition consisting essentially of a mixture of an equivalent
amount of said drug in crystalline form and an equivalent amount of said
concentration-enhancing polymer;
said composition made by forming a solid amorphous dispersion of
said low solubility drug and said concentration-enhancing polymer followed
by treating said dispersion by a method selected from the group consisting of
(1) heating said dispersion to a temperature T in degrees Kelvin wherein said
dispersion has a glass-transition temperature Tg in degrees Kelvin, and
wherein said heating satisfies the relationship Tg/T ≤1; (2) exposing said
dispersion to a mobility enhancing agent; and (3) a combination of (1) and
(2);
wherein:
at least a portion of said drug is present in drug-rich regions and said
drug-rich regions are interspersed throughout drug-poor, polymer-rich
regions,
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Application 10/636,834

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at least 60 wt% of said drug is in a non-amorphous semi-ordered state
selected from the group consisting of small crystals of said drug having a
size of less than 200 nm in at least one dimension, crystalline drug having
said concentration-enhancing polymer incorporated into said crystals,
crystals containing crystal defects, and semicrystalline structure, and
said drug in said non-amorphous semi-ordered state exhibits at least
one of:
(i) a powder x-ray diffraction pattern that is different from a powder
x-ray diffraction pattern of said first control composition, wherein at least
one peak present in said diffraction pattern of said first control composition
is not present in said diffraction pattern of said drug in said composition;
(ii) a powder x-ray diffraction pattern having at least one peak that has
a full width at half height of at least 1.1-fold that of an equivalent peak
exhibited by said drug in said first control composition;
(iii) an onset in the melt endotherm that is at a lower temperature than
the onset in the melt endotherm of said drug in said first control
composition; or
(iv) a maximum in the melt endotherm that is at a lower temperature
than the maximum in the melt endotherm of said drug in said first control
composition and wherein said composition comprising said polymer and
said drug in said non-amorphous semi-ordered state exhibits a glass
transition temperature that is different than the glass transition temperature
of a second control composition, said second control composition consisting
essentially of a solid amorphous dispersion of an equivalent amount of said
drug and an equivalent amount of said concentration enhancing polymer
wherein said drug in said second control composition is at least 90 wt%
amorphous.

The Examiner rejected the claims as follows:
 claims 1, 2, 4, 6-9, 11, 21, and 23-27 under 35 U.S.C. § 103(a) as
unpatentable over Curatolo;1 and
 claims 1, 2, 4, 6-9, 11, 21, and 23-27 under 35 U.S.C. § 103(a) as
unpatentable over Appel.2

1 William J. Curatolo et al., US 2002/0006443 A1, published Jan. 17, 2002.
2 Leah Elizabeth Appel et al., EP 1027887 A2, published Aug. 16, 2000.
Appeal 2011-011726
Application 10/636,834

4

OBVIOUSNESS
Appellants present the same issue for review in both obviousness
rejections. Accordingly, the rejections will be reviewed together.
The Issue
The Examiner found that Curatolo disclosed amorphous solid
dispersions of poorly soluble drugs in concentration enhancing polymers.
(Ans. 6.) The Examiner found that claim 1’s recited composition formation
limitations “do not limit the composition but describe[] the process of
making the composition.” (Id. at 7.) The Examiner gave the limitations no
weight because “[t]he composition of Curatolo has the capacity of being
subjected to the treatment recited in claims 1, 25 and 26.” (Id.)
With regard to the rejection over Appel, the Examiner found that
Appel disclosed “spray-coated amorphous solid dispersion of a drug and
ionizable cellulose polymer,” and that “Appel uses concentration enhancing
polymer for forming the solid dispersion of drug.” (Ans. 8.) The Examiner
again gave no weight to claim 1’s recited composition formation limitations
because “subjecting the formed dispersion to either (1) or (2) or combination
of (1) and (2) recited in claims 1, 25 and 26 and the requirement for claim 27
do not limit the composition but describes the process by which the
composition can be formed by subjecting a dispersion to heating or exposing
the dispersion to mobility enhancing agent or combination of heating and
exposure to mobility enhancing agent. The composition of Appel has the
capacity of being subjected to treatment.” (Id. at 10.)
Appellants stress that “independent claims 1 and 25-26 are not
directed to a solid amorphous dispersion per se, but rather to a post-treated
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Application 10/636,834

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solid amorphous dispersion that results in a composition containing at least
60 wt% of a low-solubility [drug] in a non-amorphous semi-ordered state
broadly (claim 26) or which may be small crystals of the drug having a size
of less than 200 nm in at least one dimension (claim 25), or any of the four
forms recited in claim 1.” (App. Br. 5-6.) Appellants state: “It is the
processing steps recited in the claims that result in formation of drug in the
claimed semi-ordered state” (id. at 6); “[t]hus, although the claims are
directed to a composition, the process steps for making the composition are
included to distinguish the claimed composition from other compositions
that do not have these characteristics” (id. at 7). Appellants note that
although the Curatolo compositions “could be subjected to the claimed
treatments, there is absolutely no suggestion in Curatolo to do so, nor any
motivation to do so articulated by the Examiner.” (Id. at 6.) Appellants
make substantially the same contentions regarding the rejection over Appel.
(Id. at 8-10.)
The rejections found that the Curatolo and Appel dispersions had the
capacity to be subjected to the formation treatment recited in the claims, and
concluded that capacity was sufficient to meet the claim requirement for at
least 60% of the drug to be in a non-amorphous semi-ordered state. The
rejection’s claim interpretation is erroneous. The composition defined in the
claims is a composition “made by” either (1) heating a dispersion, or
(2) exposing the dispersion to a mobility enhancing agent, or a combination
of (1) and (2). The rejection explicitly found the dispersion taught by
Curatolo, or Appel, was not subjected to such treatment. However, the
claimed composition is defined as it exists after the treatment, or as
Appellants call it, a “post-treated” composition (App. Br. 5), not the
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Application 10/636,834

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composition before treatment. Put another way, the rejection failed to
account for every limitation claimed because the Curatolo or Appel
composition is, in Appellants’ terms, a pre-treatment composition, not the
post-treatment composition defined in the claims.

SUMMARY
We reverse the rejection of claims 1, 2, 4, 6-9, 11, 21, and 23-27
under 35 U.S.C. § 103(a) as unpatentable over Curatolo.
We reverse the rejection of claims 1, 2, 4, 6-9, 11, 21, and 23-27
under 35 U.S.C. § 103(a) as unpatentable over Appel.

REVERSED

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