Ex Parte Misselwitz et al

Patent Trial and Appeal Board

Jun 1, 2016

11883218 (P.T.A.B. Jun. 1, 2016)

UNITED STA TES p A TENT AND TRADEMARK OFFICE
APPLICATION NO. FILING DATE
111883,218 07/16/2008
21839 7590 06/03/2016
BUCHANAN, INGERSOLL & ROONEY PC
POST OFFICE BOX 1404
ALEXANDRIA, VA 22313-1404
FIRST NAMED INVENTOR
Frank Misselwitz
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
ATTORNEY DOCKET NO. CONFIRMATION NO.
11987-00042 9960
EXAMINER
KAROL, JODY LYNN
ART UNIT PAPER NUMBER
1627
NOTIFICATION DATE DELIVERY MODE
06/03/2016 ELECTRONIC
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.
Notice of the Office communication was sent electronically on above-indicated "Notification Date" to the
following e-mail address( es):
ADIPDOC 1@BIPC.com
PTOL-90A (Rev. 04/07)
UNITED STATES PATENT AND TRADEMARK OFFICE
BEFORE THE PATENT TRIAL AND APPEAL BOARD
Ex parte FRANK MISSEL WITZ, DAGMAR KUBITZA,
SON-MI PARK, and KLAUS WEHLING
Appeal2014-004087
Application 11/883 ,218 1
Technology Center 1600
Before ERIC B. GRIMES, JOHN G. NEW, and RYAN H. FLAX,
Administrative Patent Judges.
FLAX, Administrative Patent Judge.
DECISION ON APPEAL
This is a decision on appeal under 35 U.S.C. § 134(a) involving
claims directed to a method of treating a thromboembolic disorder with
rivaroxaban administered once daily, for five consecutive days, via a rapid-
release oral dosage. Claims 1, 4, 5, 11, and 18 are on appeal as rejected
under the doctrine of non-statutory obviousness type double patenting and
35 U.S.C. § 103(a). We have jurisdiction under 35 U.S.C. § 6(b).
We affirm-in-part.
1 The Real Party in Interest is Bayer Pharma Aktiengesellschaft of Berlin,
Germany. App. Br. 1.
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Application 11/883 ,218
STATEMENT OF THE CASE
The appealed claims can be found in the Claims Appendix of the
Appeal Brief. Claim 1 is the sole independent claim and reads as follows:
1. A method of treating a thromboembolic disorder comprising
administering a direct factor Xa inhibitor that is 5-Chloro-N-
( { (5S)-2-oxo-3-[ 4-(3-oxo-4-morpholinyl)phenyl]-1,3-
oxazolidin-5-yl }methyl)-2-thiophenecarboxamide no more than
once daily for at least five consecutive days in a rapid-release
oral dosage form to a patient in need thereof.
App. Br. 12 (Claims Appendix).
The following grounds of rejection are on appeal:
A. Claims 1, 4, 5, 11, and 18 rejected under the doctrine of
nonstatutory obviousness-type double patenting over claims 13, 24, and 30
of Straub 4562 in view of Kubitza 13 and Kubitza 2.4 Final Action 9.
B. Claims 1, 4, 5, 11, and 18 rejected under the doctrine of
nonstatutory obviousness-type double patenting over claims 1---6 and 17-21
of Straub 3395 in view of Kubitza 1 and Kubitza 2. Final Action 11.
2 U.S. Patent US 7,157,456 B2 (issued Jan. 2, 2007) (hereinafter "Straub
456").
3 Kubitza et al., Oral, Direct Factor Xa Inhibitor- In Healthy Male
Subjects, 102 BLOOD 81 la (Nov. 16, 2003) (hereinafter "Kubitza 1").
4 Kubitza et al., Single Dose Escalation Study Investigating the
Pharmacodynamics, Safety, and Pharmacokinetics of BAY 59-7939 and
Oral, Direct Factor Xa Inhibitor in Healthy Male Subjects, 102 BLOOD
813a, Abstract (Nov. 16, 2003) (hereinafter "Kubitza 2").
5 U.S. Patent US 7,592,339 B2 (issued Sept. 22, 2009) (hereinafter "Straub
339").
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Application 11/883 ,218
C. Claims 1, 4, 5, 11, and 18 rejected under 35 U.S.C. § 103(a) over
Straub 610, 6 Kubitza 1, and Kubitza 2. Final Action 14.
FINDINGS OF FACT
FFl. The recited "5-Chloro-N-( { (5S)-2-oxo-3-[ 4-(3-oxo-4-
morpholinyl)phenyl]-1,3-oxazolidin-5-yl} methyl)-2-thiophenecarboxamide"
is called rivaroxaban by those of ordinary skill in the art (hereinafter, we
refer to this as "rivaroxaban"). Final Action, e.g., 5; App. Br., e.g., 3.
FF2. The Specification defines "treatment" as "includ[ing] the
therapeutic and/ or prophylactic treatment of thromboembolic disorders."
Spec. 9, 11. 1-2.
FF3. The Specification defines "oral dosage forms" as
"pharmaceutical products administered orally ... recognized by those
skilled in the art to include such forms as liquid formulations, granules,
gelcaps, hard gelatine capsules or sachets filled with granules, and tablets
releasing the active compound rapidly or in a modified manner." Spec. 10,
11. 3---6.
FF4. The Specification defines "rapid-release tablets" as "those
which, according to the USP release method using apparatus 2 (paddle),
have a Q value (30 minutes) of 75 %." Spec. 10, 11. 7-9.
FF5. The Specification defines "once daily" as "administration of the
drug once a day and includes the administration of one dosage form as well
6 U.S. Patent Application Pub. US 2003/0153610 Al (published Aug. 14,
2003) (hereinafter "Straub 610"). Straub 610 issued as Straub 456.
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Application 11/883 ,218
as administration of two or more dosage forms simultaneously or
consecutively within a short time period." Spec. 10, 11. 18-20.
FF6. Straub 456 recited at claim 13 "treatment of a thromboembolic
disorder comprising administering to a patient in need thereof an effective
amount of a compound of claim 1 [undisputed to comprise rivaroxaban]
wherein the thromboembolic disorder is myocardial infarct, pulmonary
embolism or deep venous thrombosis." Straub 456 claims 1 and 13; see also
Final Action 9-10 (discussing Straub 456).
FF7. Straub 339 recited at claim 1 "[a] method for inhibiting
thrombus formation comprising administering an effective amount of
[rivaroxaban; see App. Br. 3, n.2] or a hydrate thereof, to a patient in need of
said method." Straub 339 claim 1; see also Final Action 11-12 (discussing
Straub 339).
FF8. Kubitza 1 disclosed administration of BAY 59-7939
[rivaroxaban; App. Br. 5] to "healthy male subjects" as a 5 mg once daily
("od"), oral dose on "Day O" and on "Days 4-8." Kubitza left col., first
through fourth paragraphs; see also Final Action 10-13, 16-17 (discussing
Kubitza 1).
FF9. Kubitza 1 disclosed "BAY 59-7939 was safe and well tolerated
after multiple-dose administration at all the doses tested, with no signs of
bleeding. BAY 59-7939 inhibited FXa [factor Xa] activity .... " Kubitza 1
right col., last section (Conclusions).
FFlO. Kubitza 2 disclosed administering BAY 59-7939 to "103
healthy men" as either 1.25-80 mg tablet (under fasting conditions) or a 5-
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Application 11/883 ,218
10 mg dose as oral solution. Kubitza 2 (Abstract); see also Final Action 10-
13, 16-17 (discussing Kubitza 2).
FFl 1. Kubitza 2 disclosed "BAY 59-7939 showed a rapid onset of
action with maximal effects being observed after 2 hours" and "[a]fter
administration of the oral solution, maximal plasma concentrations were
observed after about 0.5 hours ... "and "[l]ower peak concentrations of
approximately 50% were observed 2 hours after administration of the
tablet." Kubitza 2 (Abstract); see also Final Action 10-13, 16-17
(discussing Kubitza 2).
FF12. Kubitza 2 disclosed "BAY 59-7939 offers predictable
anticoagulation with an excellent safety profile." Kubitza 2 (Abstract).
FF 13. Straub 610 disclosed compounds to treat or prevent
thromboembolic disorders. Straub 610 i-fi-19-18; see also Final Action 15
(discussing Straub 610). Straub 610 disclosed that rivaroxaban is
particularly preferred. Straub 610 i-fi-f 145, 617---635 (Example 44). Straub
610 disclosed that oral administration is preferred and states that suitable
formulations include tablets and solutions. Straub 610 i-fi-1366-367.
DISCUSSION
We address both obviousness-type double patenting rejections and the
§ 103(a) rejection together because they hinge on the same facts and
arguments.
The Examiner determined that the claims of Straub 456 and Straub
339 are directed to administering rivaroxaban to a patient in need of
thromboembolic disorder treatment and that Kubitza 1 and Kubitza 2 would
have made it obvious to administer rivaroxaban in the claimed methods, that
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Application 11/883 ,218
is, once daily, for at least five consecutive days, in a rapid-release oral
dosage form. Final Action 10-13; see also FF6-FFI2 (identifying the
teachings of the references).
We agree with the Examiner's determination. Specifically, Kubitza 1
disclosed oral administration of rivaroxaban once daily for five consecutive
days (FF8) was safe and well tolerated (FF9). Kubitza 2 disclosed
administration of rivaroxaban as an oral solution (FF 10) produced maximal
plasma concentrations after 0.5 hours (FFI 1) and showed an excellent safety
profile (FF12). Based on these teachings, it would have been obvious to
practice the methods claimed by Straub 456 and Straub 339 by administering
rivaroxaban once daily, for at least five consecutive days, as an oral solution.
The Specification lists a variety of oral dosages, e.g., liquids and tablets. See
FF3. We find that the oral solution disclosed by Kubitza 2 is a rapid release
oral dosage form as recited by appealed claim 1 because an oral solution is
an oral dosage form, which would rapidly release.
The Examiner determined that Straub 610 disclosed oral
administration of rivaroxaban to patients (in need thereof) to treat or prevent
thromboembolic disorders. Final Action 15; see also FF13 (indicating
Straub 610's relevant disclosure). The Examiner determined that Kubitza 1
disclosed administering rivaroxaban to patients as an oral dosage for five
consecutive days (as a factor Xa inhibitor). Final Action 16; see also FF8-
FF9 (identifying Kubitza 1 's disclosure). The Examiner determined that
Kubitza 2 disclosed administering rivaroxaban to patients as a rapid release
oral dosage. Final Action 16; see also FF10-FF12 (identifying Kubitza 2's
disclosure). The Examiner determined that a person of ordinary skill in the
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Application 11/883 ,218
art would have been motivated to combine Kubitza 1 and Kubitza 2 with
Straub 610 for their teachings how to effectively and safely administer the
same drug of Straub 610 for the same purpose of Straub 610 (that is, to
inhibit Factor Xa and treat a thromboembolic disorder, such as deep vein
thrombosis). Final Action 16-17. These determinations by the Examiner set
forth a prima facie case of obviousness for independent claim 1.
Appellants argue that Kubitza 1 and Kubitza 2 are "irrelevant to the
presently claimed invention because they merely report studies of the
'pharmacodynamics, safety, and pharmacokinetics' of rivaroxaban in
'healthy male subjects."' App. Br. 5, 10. Appellants argue that because
these are not "patients in need of treatment for or at a significantly increased
risk for thromboembolic disorders," their teachings are inapplicable. Id. We
are not persuaded by these arguments.
The Straub 456 and Straub 339 patents claim, and Straub 610
disclosed, the treatment of a thromboembolic disorder (e.g., inhibiting
thrombus in patients that need such treatment) by administering rivaroxaban.
See FF6-FF7, FF13. Having this information in hand, a person of ordinary
skill in the art would reasonably look to and combine with any of these
references the disclosures of Kubitza 1 and Kubitza 2, which teach how one
can safely administer the drug rivaroxaban. See FF8 and FFlO. Whether
Kubitza 1 and Kubitza 2 are directed to healthy or ill individuals is not
significant because Appellants' Specification defines "treatment" as
including "prophylactic treatment" (FF2), i.e., administration to healthy
people to prevent thromboembolic disorders from developing. Moreover,
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Application 11/883 ,218
the Straub references are each directed to treating ill individuals. FF6, FF7,
FF13.
For these reasons, the Examiner's rejections of claim 1 over Straub
456, Straub 339, and/or Straub 610 in view of Kubitza 1 and Kubitza 2 are
affirmed. Claims 4, 11, and 18 fall with claim 1 because they were not
argued separately. 37 C.F.R. § 41.37(c)(l)(iv).
With respect to claim 5, Appellants identify that "[t]he Examiner
acknowledges that Straub does not teach ... 'a rapid release tablet as
claimed in the instant claim 5. "' App. Br. 9.
The Examiner conceded that the Straub 456, Straub 339, and Straub
610 references did not claim or disclose the "rapid release" tablet of claim 5.
Final Action 10, 12, 15-16. For this, the Examiner relied on Kubitza 2,
which disclosed "BAY 59-7939 showed a rapid onset of action with
maximal effects being observed after 2 hours" and "peak concentrations of
approximately 50% were observed 2 hours after administration of the
tablet." Kubitza 2 (Abstract); see also FFl 1; Final Action 16 and Ans. 13
(discussing Kubitza 2).
Appealed claim 5 recites a "rapid-release tablet," which we interpret
in view of the express definition thereof provided in the Specification, which
is "those [tablets] which, according to the USP release method using
apparatus 2 (paddle), have a Q value (30 minutes) of 75 %." FF4. The only
disclosure of Kubitza 2 directed to drug release by tablets is that "[l]ower
peak concentrations of approximately 50% were observed 2 hours after
administration of the tablet." Kubitza 2 (Abstract). Based on the evidence
of record we cannot conclude that this disclosure indicates a "rapid-release
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Application 11/883 ,218
tablet" as defined in the Specification. Moreover, the Examiner has offered
no explanation as to how the disclosure of Kubitza 2 teaches or suggest a
rapid-release tablet in line with the interpretation of this claim language.
Therefore, we find Appellants' argument (see App. Br. 9) concerning the
patentability of claim 5 over the combined references persuasive and reverse
the Examiner's rejections of claim 5 over Straub 456, Straub 339, or Straub
610 in view of or combined with Kubitza 1 and Kubitza 2.
SUMMARY
The rejection of claims 1, 4, 5, 11, and 18 under the doctrine of
nonstatutory obviousness-type double patenting over claims 13, 24, and 30
of Straub 456 in view ofKubitza 1 and Kubitza 2 is affirmed as to claims 1,
4, 11, and 18, and reversed as to claim 5.
The rejection of claims 1, 4, 5, 11, and 18 under the doctrine of
nonstatutory obviousness-type double patenting over claims 1---6 and 17-21
of Straub 339 in view ofKubitza 1 and Kubitza 2 is affirmed as to claims 1,
4, 11, and 18, and reversed as to claim 5.
The rejection of claims 1, 4, 5, 11, and 18 under 35 U.S.C. § 103(a)
over Straub 610, Kubitza 1, and Kubitza 2 is affirmed as to claims 1, 4, 11,
and 18, and reversed as to claim 5.
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-IN-PART
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