Ex Parte Schultz et al

Board of Patent Appeals and Interferences

Apr 29, 2010

10022138 (B.P.A.I. Apr. 29, 2010)

UNITED STATES PATENT AND TRADEMARK OFFICE
__________

BEFORE THE BOARD OF PATENT APPEALS
AND INTERFERENCES
__________

Ex parte THOMAS SCHULTZ,
BRADLEY A. CLARK, and ANGELA FALZONE
__________

Appeal 2009-014705
Application 10/022,138
Technology Center 1600
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Decided: April 29, 2010
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Before ERIC GRIMES, DONALD E. ADAMS, and LORA M. GREEN,
Administrative Patent Judges.

GRIMES, Administrative Patent Judge.

DECISION ON APPEAL
This is an appeal under 35 U.S.C. § 134 involving claims to an oral
steroid hormone product. The Examiner has rejected the claims as obvious.
We have jurisdiction under 35 U.S.C. § 6(b). We reverse.

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STATEMENT OF THE CASE
Claims 1, 6 and 7 are on appeal. Claim 1 is representative and reads
as follows:
1. An oral steroid hormone product having improved dissolution and
release rate properties, said product comprising norgestimate in admixture
with lactose, wherein substantially all of said norgestimate is in non-
crystalline form and wherein said lactose stabilizes said norgestimate in its
non-crystalline form.

I.
Issue
The Examiner has rejected claims 1, 6 and 7 under 35 U.S.C. § 103(a)
as being obvious in view of Gast,1 Morita,2 Merck,3 Jain,4 Sebhatu,5 and
Buckton6 (Ans. 47). The Examiner has also rejected claims 1, 6, and 7 under
35 U.S.C. § 103(a) as being obvious in view of de Haan8 and Merck

1 Gast et al., US 5,858,405, Jan. 12, 1999
2 Masami Morita et al., Physicochemical Properties of Crystalline Lactose.
II. Effect of Crystallinity on Mechanical and Structural Properties, 32
CHEM. PHARM. BULL. 4076-4083 (1984)
3 S. Budavari (Editor) The Merck Index, 12th ed., p. 632 (1996)
4 R. Jain et al., Stability of a Hydrophobic drug in presence of hydrous and
anhydrous lactose, 46 EUROPEAN JOURNAL OF PHARMACEUTICS AND
BIOPHARMACEUTICS 177-182 (1998)
5 Tesfai Sebhatu et al., Assessment of the degree of disorder in crystalline
solids by isothermal microcalorimetry, 104 INTERNATIONAL JOURNAL OF
PHARMACEUTICS 135-144 (1994)
6 Graham Buckton et al., The influence of additives on the recrystallisation
of amorphous spray dried lactose, 121 INTERNATIONAL JOURNAL OF
PHARMACEUTICS 81-87 (1995)
7 The Examiner also cited a reference by “Rialker et al.” as part of the basis
of the rejection (Ans. 4) but did not list a reference by Rialker et al. as part
of the “Evidence Relied Upon” (Ans. 3) or otherwise identify the reference
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(Ans. 5). Because the same issue is dispositive with respect to both
rejections, we will consider them together.
The Examiner finds that Morita, Jain, Sebhatu, and Buckton teach the
use of lactose in pharmaceutical preparations (Ans. 3). The Examiner finds
that Gast discloses “a hormonal product with an excipient in crystalline and
non-crystalline form” (Ans. 4) but does not teach a “non-crystalline steroid
hormone” (id.). The Examiner finds that Merck discloses “that estrone can
be crystallized which means that it was not crystalline before” (id. at 5). The
Examiner concludes that the claimed composition would have been obvious
because Merck “show[s] that estrone exists in both non-crystalline and
crystalline forms” (id. at 5).
With regard to the second ground of rejection, the Examiner finds that
de Haan discloses pharmaceutical preparations containing steroidal agents in
combination with an excipient that can be lactose (Ans. 6). The Examiner
also finds that de Haan discloses a tablet containing progesterone, and finds
that “[n]orgestimate is progesterone” (id.). As before, the Examiner finds
that Merck discloses “that estrone can be crystallized” (id.), and concludes
that this teaching would have made obvious the claimed composition.
Appellants contend that none of the cited references disclose or
suggest a product comprising norgestimate such that substantially all of the
norgestimate is in non-crystalline form (Appeal Br. 9-11).

being cited. Since the Examiner has not provided Appellants or us with
adequate notice of the source of the evidence allegedly provided by Rialker
et al., we have not considered it.
8 De Haan, EP 0503521 A1, Sept. 16, 1992
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The issue with respect to each of the rejections is: Does the evidence
of record support the Examiner’s conclusion that the cited references suggest
a product comprising norgestimate such that substantially all of the
norgestimate is in non-crystalline form?
Findings of Fact
1. Gast discloses a “combination progestin/estrogen oral
contraceptive.… Particularly preferred progestins of this invention are
trimegestone, dienogest, and drospirenone. (Gast, abstract).
2. Gast discloses, in the background prior art, that norgestimate is a
known component of contraceptives (id. at col. 2, l. 48; col. 3, ll. 14 and 25).
3. Gast discloses that “[p]referred estrogens include … estrone or a
salt thereof” (id. at col. 7, ll. 10-12).
4. Merck discloses that estrone exists in three crystal phases (Merck
632).
5. De Haan discloses “dry pharmaceutical preparations containing
ultra-low doses of one or more micronized steroidal medicinal agents in
combination with a primary excipient” (de Haan, 3: 21-23).
6. De Haan discloses that “[s]teroids used in the compositions and
processes of the invention are preferably estrogens, progestogens, or both”
(id. at 4: 32-33).
7. De Haan discloses that “[p]referred progestogens for use with the
invention include 3-ketodesogestrel (‘etonogestrel’), desogestrel,
levo-norgestrel, norgestrel, gestodene, and other compounds with similar
progestogenic activity” (id. at 4: 34-35).

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Principles of Law
“In rejecting claims under 35 U.S.C. § 103, the examiner bears the
initial burden of presenting a prima facie case of obviousness. Only if that
burden is met, does the burden of coming forward with evidence or
argument shift to the applicant.” In re Rijckaert, 9 F.3d 1531, 1532 (Fed.
Cir. 1993).
Analysis
Claim 1 is directed to an oral steroid hormone product comprising
norgestimate, where substantially all of the norgestimate is in non-crystalline
form. Appellants contend that the cited references do not disclose or suggest
this limitation (Appeal Br. 9-11).
The Examiner responds that Gast discloses norgestimate as a
progestin, and progestins in combination with estrogen, and that Merck
discloses that estrone, an estrogen, exists in both non-crystalline and
crystalline forms (Ans. 7-8).
Appellants’ arguments are persuasive that the Examiner has not
adequately explained how the cited references suggest the claimed non-
crystalline norgestimate. While Gast discloses that norgestimate has been
used in contraceptive products before, it does not disclose whether the
norgestimate was in crystalline or non-crystalline form. The Examiner has
not pointed to any disclosure of norgestimate in de Haan. Thus, none of the
cited references disclose non-crystalline norgestimate.
The Examiner’s reasoning, as we understand it, is that Merck’s
disclosure of estrone as having a crystalline form suggests that it also has a
non-crystalline form, and therefore so does the different steroid hormone
norgestimate. This reasoning is not persuasive. The Examiner has not
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adequately explained why the existence of a non-crystalline form of a certain
compound would have made obvious the use of a non-crystalline form of a
different compound in the composition disclosed by Gast or de Haan.
Thus, we are compelled to reverse the rejection of claim 1 as being
obvious in view of Gast, Morita, Merck, Jain, Sebhatu, and Buckton, as well
as the rejection of claim 1 as being obvious in view of de Haan and Merck.
The rejections of claims 6 and 7, which depend from claim 1, are also
reversed for the same reason.
Conclusion of Law
The evidence of record does not support the Examiner’s conclusion
that the cited references suggest a product comprising norgestimate such that
substantially all of the norgestimate is in non-crystalline form.
SUMMARY
We reverse both rejections of claim 1, 6 and 7 under 35 U.S.C.
§ 103(a).
REVERSED
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