`Customer No. 6449
`Application No. 13/617,138
`Attorney Docket No. 3850-125
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`IN THE UNITED STATES PATENT AND TRADEMARK OFFICE
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`Appl. No. (cid:9)
`Applicant (cid:9)
`Filed (cid:9)
`TC/A.U. (cid:9)
`Examiner (cid:9)
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`: 13/617,138
`: Roberto VILLA et al.
`: 14 September 2012
`: 1615
`: Susan T. Tran
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`Docket No. (cid:9)
`Customer No. (cid:9)
`Confirmation No. (cid:9)
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`: 3850-125
`: 06449
`: 7811
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`AMENDMENT
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`MAIL STOP AMENDMENT
`Director of the United States Patent
`and Trademark Office
`P.O. Box 1450
`Alexandria, Virginia 22313-1450
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`Dear Sir:
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`In response to the Office Action dated 16 November 2012, please amend this
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`application as follows:
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`Amendments to the Claims begin on page 2.
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`Remarks begin on page 5.
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`Exhibit 1052
`ARGENTUM
`IPR2018-00080
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`000001
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`Application No.: 13/617,138
`Attorney Docket No. 3850-125
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`AMENDMENTS TO THE CLAIMS
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`This listing of claims will replace all prior versions and listings of claims in the
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`application.
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`Listing of Claims
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`1. (Currently amended) (cid:9)
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`A controlled release oral pharmaceutical composition comprising:
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`(1) a tablet core comprising:
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`a) budesonide in an amount effective for treatment of inflammatory bowel
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`disease in the gastrointestinal tract,
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`b) a lipophilic excipient;
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`c) an amphiphilic excipient;
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`d) a hydrogel-forming hydrophilic excipient other than a gum; and
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`(2) a coating on said tablet core, said coating comprising a gastro-resistant film.
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`2. (Currently Amended) (cid:9)
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`The composition of A controlled release oral pharmaceutical
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`composition according to claim 1, comprising wherein said controlled release oral
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`pharmaceutical composition comprises 9 mg of budesonide.
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`3. (New) (cid:9)
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`A controlled release oral pharmaceutical composition according to claim 1,
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`wherein said hydrogel-forming hydrophilic excipient comprises hydroxypropyl cellulose.
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`2
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`Attorney Docket No. 3850-125
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`4. (New) (cid:9)
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`A controlled release oral pharmaceutical composition according to claim 2,
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`wherein said hydrogel-forming hydrophilic excipient comprises hydroxypropyl cellulose.
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`5. (New) (cid:9)
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`A controlled release oral pharmaceutical composition according to claim 1,
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`wherein said gastro-resistant film comprises at least one methacrylic acid polymer or copolymer.
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`6. (New) (cid:9)
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`A controlled release oral pharmaceutical composition according to claim 5,
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`wherein said hydrogel-forming hydrophilic excipient comprises hydroxypropyl cellulose.
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`7. (New) (cid:9)
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`A controlled release oral pharmaceutical composition according to claim 1,
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`wherein said lipophilic excipient and said amphiphilic excipient are present in said controlled
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`release oral pharmaceutical composition in a ratio of about 1 to 1 by weight.
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`8. (New) (cid:9)
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`A controlled release oral pharmaceutical composition according to claim 7,
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`wherein said hydrogel-forming hydrophilic excipient comprises hydroxypropyl cellulose.
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`9. (New) (cid:9)
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`A controlled release oral pharmaceutical composition according to claim 1,
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`wherein said lipophilic excipient comprises stearic acid.
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`10. (New) (cid:9)
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`A controlled release oral pharmaceutical composition according to claim 9,
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`wherein said hydrogel-forming hydrophilic excipient comprises hydroxypropyl cellulose.
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`Application No.: 13/617,138
`Attorney Docket No. 3850-125
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`11. (New) (cid:9)
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`A controlled release oral pharmaceutical composition according to claim 1,
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`wherein said amphiphilic excipient comprises lecithin.
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`12. (New) (cid:9)
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`A controlled release oral pharmaceutical composition according to claim 11,
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`wherein said hydrogel-forming hydrophilic excipient comprises hydroxypropyl cellulose.
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`Application No.: 13/617,138
`Attorney Docket No. 3850-125
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`Amendments
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`REMARKS
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`Claim 1 has been amended to specify that the hydrogel-forming hydrophilic excipient is
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`not a gum. The as-filed specification discloses at paragraph 36 that the hydrophilic excipient can
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`comprise hydrogel compounds, including natural or synthetic gums. As such, there is written
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`description support for amending claim 1 to recite that the hydrogel-forming hydrophilic
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`excipient comprising the presently claimed controlled release oral pharmaceutical compositions
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`is other than a gum. In re Johnson, 558 F.2d 1008 (C.C.P.A. 1977).
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`New claims 3, 4, 6, 8, 10 and 12 have been added to specify that the hydrogel-forming
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`hydrophilic excipient comprises hydroxypropyl cellulose. Support for these claims can be found
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`in the as-filed specification at least in Example 1 (paragraphs [0047] to [0051]) and Example 2
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`(paragraphs [0052] to [0055]).
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`New claim 5 has been added to specify that the gastro resistant film comprises at least
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`one methacrylic acid polymer or copolymer. Support for this claim can be found in the as-filed
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`specification at least in Example 1 (paragraphs [0047] to [0051]) and Example 2 (paragraphs
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`[0052] to [0055]).
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`New claim 7 has been added to specify that the lipophilic excipient and amphiphilic
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`excipient are in a 1:1 ratio. Support for this claim can be found in the as-filed specification at
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`least in Example 1 (paragraphs [0047] to [0051]) and Example 2 (paragraphs [0052] to [0055]).
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`New claim 9 has been added to specify that the lipophilic excipient is stearic acid.
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`Support for this claim can be found in the as-filed specification at least in Example 1 (paragraphs
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`[0047] to [0051]) and Example 2 (paragraphs [0052] to [0055]).
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`Attorney Docket No. 3850-125
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`New claim 11 has been added to specify that the amphiphilic excipient is lecithin.
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`Support for this claim can be found at least in paragraph [0033] in the as-filed specification.
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`Applicants submit that these amendments do not constitute new matter, and their entry is
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`requested.
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`Rejections for obviousness-type double patenting
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`The Examiner has provisionally rejected claims 1-2 for obviousness-type double
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`patenting over claims 1-15 of copending application Serial No. 13/249,389.
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`The Examiner has provisionally rejected claims 1-2 for obviousness-type double
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`patenting over claims 1-3 of copending application Serial No. 13/462,409, which Applicants note
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`is now U.S. Patent No. 8,293,273.
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`The Examiner has rejected claims 1-2 for obviousness-type double patenting over claims
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`1-11 of U.S. Patent No. 7,410,651.
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`The Examiner has rejected claims 1-2 for obviousness-type double patenting over claims
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`1-11 of U.S. Patent No. 7,431,943.
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`The Examiner has rejected claims 1-2 for obviousness-type double patenting over claims
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`1-11 of U.S. Patent No. 8,029,823 which Applicants note is now RE43799.
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`There is no basis for this rejection. However, solely to expedite prosecution, Applicants
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`submit herewith a Terminal Disclaimer which obviates these rejections. Withdrawal of these
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`rejections is requested.
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`Attorney Docket No. 3850-125
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`Rejection under 35 U.S.C. § 102(e)
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`The Examiner has rejected claims 1-2 under 35 U.S.C. § 102(e) as being anticipated by
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`Hallgren et al. (US 6,239,120). The Examiner contends that Hallgren teaches a tablet
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`composition comprising budesonide and pharmaceutically acceptable carriers which may include
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`a hydrogel excipient (e.g., mannitol cellulose derivatives), an amphiphilic excipient (e.g.,
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`polyethylene glycol) and a lipophilic excipient (e.g., waxes). The Examiner also contends that
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`Hallgren discloses that the tablet may be coated with an enteric coating. The Examiner further
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`contends that Hallgren discloses a dosage of active ingredient of 0.5-20 mg and the use of 9 mg
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`budesonide in the Examples. Applicants traverse this rejection.
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`Hallgren discloses the use of glucocorticoids, including budesonide, for treating
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`glomerulonephritis, a renal disease. Hallgren does not disclose the use of glucocorticoids for
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`treating inflammatory bowel disease or intestinal diseases. Thus, there is no disclosure in
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`Hallgren of the use of 9 mg budesonide for treating inflammatory bowel disease as required by
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`claim 2.
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`Applicant notes that Hallgren discloses using 9 mg of budesonide for treating IgA
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`nephrology. The total of 9 mg of budesonide was administered via the use of Entocort®
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`budesonide capsules. According to the Entocort® EC budesonide prescribing information (copy
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`attached for the convenience of the Examiner), Entocort® budesonide is in the form of a capsule
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`comprising small pellets, each of which comprises micronized budesonide and a controlled-
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`release coating. Each capsule contains enough of the small pellets that the total dose of
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`budesonide in each capsule is 3 mg. Thus, the 9 mg dose of budesonide disclosed in the
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`Examples of Hallgren is arrived at by the administration of three capsules, each comprising
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`coated pellets, and not in a single tablet, comprising a tablet core and a gastro-resistant coating
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`on the tablet core. One of ordinary skill in the art would appreciate that the capsules used in
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`Hallgren are not the same as, and so do not anticipate, the presently claimed controlled release
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`oral dosage form that comprises a tablet core. Applicants submit that Hallgren does not disclose
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`all of the elements of claims 1 and 2 and thus cannot anticipate these claims.
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`In addition, Hallgren does not teach a tablet in which the hydrogel-forming hydrophilic
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`excipient is hydroxypropyl cellulose (claims 3, 4, 6, 8, 10 and 12). Hallgren does not teach a
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`tablet in which the lipophilic excipient and amphiphilic excipient are present in a 1:1 ratio (claim
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`7). Hallgren also does not disclose a tablet that includes stearic acid as the lipophilic excipient
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`(claim 9). In addition, Hallgren does not disclose a tablet that includes lecithin as the
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`amphiphilic excipient (claim 11). Because Hallgren does not disclose all of the elements of the
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`claimed subject matter as amended, Applicants submit that Hallgren cannot anticipate the claims.
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`In view of the above remarks, Applicants submit that the claimed subject matter is not
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`anticipated by Hallgren et al. Withdrawal of this rejection is requested.
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`Rejection under 35 U.S.C. § 102(b)
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`The Examiner has rejected claim 1 under 35 U.S.C. § 102(b) as being anticipated by
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`Friend et al. (US 5,811,388). The Examiner contends that Friend teaches a drug delivery system
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`such as a tablet that comprises a hydrogel gum, a drug such as budesonide, a penetration
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`enhancer (an amphiphilic excipient) and cellulosic excipients (lipophilic excipients). The
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`Examiner also contends that Friend discloses that the tablet may be coated with an enteric
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`coating. Applicants traverse this rejection.
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`Applicants submit that Friend does not disclose all of the elements of the claims as
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`amended. Specifically, Friend discloses the use of a hydrogel gum. Claim 1 as amended
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`excludes a gum as the hydrogel excipient. Since Friend does not disclose other hydrophilic
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`excipients, it does not disclose this element of claim 1 as amended. In addition, Friend does not
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`teach a tablet in which the hydrogel-forming hydrophilic excipient is hydroxypropyl cellulose
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`(claims 3, 4, 6, 8, 10 and 12). Friend does not disclose a tablet containing 9 mg of budesonide
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`(claim 2). Friend does not teach a tablet in which the lipophilic excipient and amphiphilic
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`excipient are present in a 1:1 ratio (claim 7). Friend also does not disclose a tablet that includes
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`stearic acid as the lipophilic excipient (claim 9). In addition, Friend does not disclose a tablet
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`that includes lecithin as the amphiphilic excipient (claim 11). Because Friend does not disclose
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`all of the elements of the claimed subject matter as amended, Applicants submit that Friend
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`cannot anticipate the claims as amended.
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`In view of the above remarks, Applicants submit that the claimed subject matter is not
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`anticipated by Friend et al. Withdrawal of this rejection is requested.
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`Rejection under 35 U.S.C. § 103(a)
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`The Examiner has rejected claims 1-2 under 35 U.S.C. § 103(a) as being unpatentable
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`over Friend et al. (US 5,811,388) in view of Hallgren et al. (US 6,239,120). The Examiner notes
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`that Friend does not teach the amount of budesonide and cites Hallgren for teaching a tablet
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`dosage of budesonide from 0.5-20 mg and the use of 9 mg budesonide in the Examples. The
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`Examiner then contends that it would have been obvious to modify the dosage form of Friend to
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`include budesonide in 9 mg per tablet. Applicants traverse this rejection.
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`As described above, Friend does not disclose hydrophilic excipients other than gums; it
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`does not disclose this element of claim 1 as amended. In addition, Friend does not teach a tablet
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`in which the hydrogel-forming hydrophilic excipient is hydroxypropyl cellulose (claims 3, 4, 6,
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`8, 10 and 12). Friend does not disclose a tablet containing 9 mg of budesonide (claim 2). Friend
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`does not teach a tablet in which the lipophilic excipient and amphiphilic excipient are present in
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`a 1:1 ratio (claim 7). Friend also does not disclose a tablet that includes stearic acid as the
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`lipophilic excipient (claim 9). In addition, Friend does not disclose a tablet that includes lecithin
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`as the amphiphilic excipient (claim 11). Hallgren does not cure these deficiencies of Friend.
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`Thus, the combination of Hallgren with Friend does not result in a controlled release oral
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`pharmaceutical composition which has all of the elements set forth in the claims as amended.
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`Accordingly, the combination of Friend and Hallgren does not render obvious the claims as
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`amended.
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`In addition, Friend teaches the use of a hydrocolloid gum to act as delayed release tool
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`inside of a composition aimed to deliver the active ingredients in the colon. Friend also teaches
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`the use of an enzymatic activation of the release mechanism once the tablet is transiting through
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`the colon. Since these mechanisms are important for the compositions of Friend to deliver the
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`active ingredients, Applicant submits that one of ordinary skill in the art would not look to
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`modify Friend by the elements of Hallgren which would change the basic function of the
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`composition of Friend. For this reason, Applicant submits that the combination of Friend and
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`Hallgren is improper and does not render obvious the claimed subject matter.
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`In view of the above remarks, Applicants submit that the claimed subject matter is not
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`rendered obvious by the combination of Friend et al. and Hallgren et al. Withdrawal of this
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`rejection is requested.
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`Application No.: 13/617,138
`Attorney Docket No. 3850-125
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`Conclusion
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`In view of the above amendments and remarks, it is submitted that the claims satisfy the
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`requirements of the patent statutes and are patentable over the prior art of record.
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`Reconsideration of this application and early notice of allowance is requested. The Examiner is
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`invited to telephone the undersigned if it will assist in expediting the prosecution and allowance
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`of the instant application.
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`Respectfully submitted,
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`Dated: 15 January 2013
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`By (cid:9)
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`/Jeffrey L. Ihnen/
`Jeffrey L. Ihnen
`Registration No. 28,957
`Attorney for Applicants
`607 14th Street, N.W., Suite 800
`Washington, D.C. 20005
`Phone: 202-783-6040
`Fax: 202-783-6031
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`Attachment: ENTOCORT® EC (budesonide) Capsules, Prescribing Information
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`11
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`000011
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`(cid:9)
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