DETAILED ACTION
Claims 1-14 are pending and under consideration on the merits.
Notice of Pre-AIA or AIA Status
The present application, filed on or after March 16, 2013, is being examined under the first inventor to file provisions of the AIA .
Information Disclosure Statement
The information disclosure statement (IDS) submitted on 10/08/2025 was filed prior to the mailing date of a Final Office Action. The submission is in compliance with the provisions of 37 CFR 1.97. Accordingly, it was considered by the Examiner.
Status of the Rejections
The claim objection is withdrawn in view of the amendment.
The 112(b) rejection is withdrawn in view of the amendment, but a new rejection was necessitated by the amendment.
The 103 rejections are withdrawn in view of the amendment, but new rejections are applied over new references as detailed below.
Claim Rejections - 35 USC § 112
The following is a quotation of 35 U.S.C. 112(b):
(b) CONCLUSION.—The specification shall conclude with one or more claims particularly pointing out and distinctly claiming the subject matter which the inventor or a joint inventor regards as the invention.
The following is a quotation of 35 U.S.C. 112 (pre-AIA ), second paragraph:
The specification shall conclude with one or more claims particularly pointing out and distinctly claiming the subject matter which the applicant regards as his invention.
Claims 3-4 and 8-14 are rejected under 35 U.S.C. 112(b) or 35 U.S.C. 112 (pre-AIA ), second paragraph, as indefinite for failing to particularly point out and distinctly claim the subject matter which the inventor or a joint inventor (or for applications subject to pre-AIA 35 U.S.C. 112, the applicant), regards as the invention.
Claim 3 recites “does not dissolve under dissolution conditions for at least two hours.” This limitation is indefinite because the metes and bounds of “dissolution conditions” is unknown. The specification does not appear to provide a formal definition of “dissolution conditions,” and while the working examples provide examples of such conditions, e.g., USP dissolution apparatus 2 (Paddle) and 50 rpm at paragraph 288 as published, limitations from the specification are not imported into the claims. MPEP 2111.01 II. Clarification is required. Since dependent claim 4 does not clarify the point of confusion, it is also rejected.
Claims 8 and 13 recites “vivapur112” wherein VIVAPUR is a trademark. Where a trademark or trade name is used in a claim as a limitation to identify or describe a particular material or product, the claim does not comply with the requirements of 35 U.S.C. 112(b) or 35 U.S.C. 112 (pre-AIA ), second paragraph. See Ex parte Simpson, 218 USPQ 1020 (Bd. App. 1982). The claim scope is uncertain since the trademark or trade name cannot be used properly to identify any particular material or product. A trademark or trade name is used to identify a source of goods, and not the goods themselves. Thus, a trademark or trade name does not identify or describe the goods associated with the trademark or trade name. In the present case, the trademark/trade name is used to identify/describe a chemical compound and, accordingly, the identification/description is indefinite. Additionally, while Applicant may intend that “vivapur112” refers to a microcrystalline cellulose, claim 8 already recites “microcrystalline cellulose.” Clarification is required. Since dependent claims 9-12 and 14 fail to clarify the indefiniteness, they are also rejected. For the purpose of examination in view of the prior art, “vivapur112” has been given its broadest reasonable interpretation, which is that this term is synonymous with “microcrystalline cellulose.”
Claim 12 recites that “the hydroxypropyl cellulose and purified water comprise a binding solution.” It is unclear how a solid chemical compound such as hydroxypropyl cellulose can comprise a liquid “binding solution.” Clarification is required. Since dependent claim 13 does not clarify the confusion, it is also rejected. For the purpose of examination, claim 12 has been given its broadest reasonable interpretation, which is that the composition further comprises a binding solution that comprises the hydroxypropyl cellulose and the purified water.
Claim 13 recites an outside layer comprising vivapur112, croscarmellose sodium, and colloidal silicon dioxide, but this limitation is unclear because these ingredients are already recited by claim 8, from which claim 13 depends. Also, claim 8 fails to recite an “outside layer.” Clarification is required. It is suggested that claim 13 recite that the composition “further” comprises an outside layer to make it clear that this is an additional element not recited by claim 8, and also that each of vivapur112, croscarmellose sodium, and colloidal silicon dioxide should be preceded by “the” to make it clear that claim 13 is referring to ingredients that are already present in the composition of the base claim.
Claim 14 recites “does not dissolve under low pH conditions,” which is indefinite because the specification does not provide a clear definition of “low pH conditions.” While the specification states that a low pH condition is “generally pH 1 to 2” (paragraph 892 as published), the use of “generally” implies that in some circumstances a low pH condition may be something other than a range of 1 to 2, and it is unclear what those circumstances are or what the pH range would be in those circumstances. Clarification is required.
Claim Rejections - 35 USC § 103
The following is a quotation of 35 U.S.C. 103 which forms the basis for all obviousness rejections set forth in this Office action:
A patent for a claimed invention may not be obtained, notwithstanding that the claimed invention is not identically disclosed as set forth in section 102, if the differences between the claimed invention and the prior art are such that the claimed invention as a whole would have been obvious before the effective filing date of the claimed invention to a person having ordinary skill in the art to which the claimed invention pertains. Patentability shall not be negated by the manner in which the invention was made.
The factual inquiries for establishing a background for determining obviousness under 35 U.S.C. 103 are summarized as follows:
1. Determining the scope and contents of the prior art.
2. Ascertaining the differences between the prior art and the claims at issue.
3. Resolving the level of ordinary skill in the pertinent art.
4. Considering objective evidence present in the application indicating obviousness or nonobviousness.
This application currently names joint inventors. In considering patentability of the claims the examiner presumes that the subject matter of the various claims was commonly owned as of the effective filing date of the claimed invention(s) absent any evidence to the contrary. Applicant is advised of the obligation under 37 CFR 1.56 to point out the inventor and effective filing dates of each claim that was not commonly owned as of the effective filing date of the later invention in order for the examiner to consider the applicability of 35 U.S.C. 102(b)(2)(C) for any potential 35 U.S.C. 102(a)(2) prior art against the later invention.
Claims 1-12 and 14 are rejected under 35 U.S.C. 103 as unpatentable over Lee et al. (US Pat. Pub. 2018/0338954) in view of Wakeman et al. (US Pat. Pub. 2018/0360761) and Maeda et al. (U.S. Pat. Pub. 2018/0214460; of record).
As to claims 1-12 and 14, Lee discloses pharmaceutical compositions comprising benzimidazole derivatives as actives such as 4-((5,7-difluorochroman-4-yl)oxy)-N,N,2-trimethyl-1H-benzo[d]imidazole-6-carboxamide (i.e., “tegoprazan”)(paragraphs, 13, 15), and discloses embodiments comprising the active along with mannitol, microcrystalline cellulose, sodium croscarmellose, colloidal silicon dioxide, and magnesium stearate (an “immediate release portion” of claim 1)(paragraphs 36-38). Lee further teaches formulating the immediate release portion as granules (claim 12) by adding a binding solution comprising hydroxpropyl cellulose and purified water (claims 8 and 12)(paragraph 37).
Regarding claim 4, the composition may be a single unit dosage form (paragraph 8).
As to claims 1-12 and 14, Lee does not further expressly disclose that the composition further comprises a modified release portion comprising tegoprazan, polyvinyl alcohol, hydroxypropyl methyl cellulose, talc, methyl acrylic acid copolymer, potassium hydroxide, triethyl citrate, purified water, and an inert particle as recited by claim 1 that comprises sucrose (claims 7, 9), or further comprising polyethylene glycol, polysorbate 80, anhydrous ethanol, and a combination of methacrylic acid-ethyl acrylate copolymer and methacrylic acid-methylmethacrylate copolymer as recited by claim 37, and wherein the modified release portion does not dissolve for at least two hours (claims 3 and 14). Nor does Lee expressly teach that the composition comprises a capsule (claim 2). Additionally, Lee teaches that the composition comprises a total of 50-200 mg, which encompasses or overlaps the total amounts recited by claims 5-6 and 10-11, but because Lee does not teach a modified release portion, it follows that Lee does not disclose apportioning the tegoprazan between the immediate release and modified release portions in the amounts recited by these claims.
Wakemen discloses pharmaceutical compositions comprising a modified release portion and an immediate release portion as multiparticulates/pellets for release of a drug (paragraphs 52, 112), wherein the modified release portion may comprise an erodible matrix that may comprise polyvinyl alcohol, hydroxypropyl methyl cellulose, a methyl acrylic copolymer such as methyl acrylate-methyl methacrylate or copolymers of methyl methacrylate, ethyl acrylate, or methacrylate (paragraphs 54, 56, 67). Wakemen discloses a specific embodiment of a modified release composition comprising polyvinyl alcohol, hydroxypropyl methyl cellulose, methyl acrylic acid copolymer, talc, purified water, and microcrystalline spheres (an “inert particle” of claims 1 and 8)(Example 17, paragraphs 249-250). Wakemen further discloses a specific immediate release embodiment comprising microcrystalline cellulose, croscarmellose sodium, magnesium stearate, and colloidal silicon dioxide (Example 1 and paragraph 161). Wakemen also teaches that sucrose inert cores can be used instead of microcrystalline cellulose inert cores (paragraph 212). Wakemen further teaches that the modified release pellets may comprise triethyl citrate as a plasticizer (paragraphs 98, 102) and further teaches that the composition may comprise a diluent/filler such as mannitol (paragraph 61) and also that potassium hydroxide may be included to form a salt of the active and also that potassium salts may be included as a pH modifier, the skilled artisan recognizing that potassium hydroxide is a potassium salt (paragraphs 43, 65). Wakemen also teaches applying a film forming agent comprising polyethylene glycol and colorants, dispersion aids, or opacifiers (paragraph 77) and discloses that coatings may be applied using a solvent such as water or ethanol or a mixture thereof (paragraph 214). The multiparticulates may be packaged as a capsule (paragraph 92).
Maeda discloses a modified release pharmaceutical composition comprising an inner core comprising acetylsalicylic acid as an active and further comprising an enteric coating over the core comprising an enteric agent, and an outer layer comprising a potassium competitive acid blocker (paragraphs 17-19, 83-84) such as tegoprazan (paragraph 107). Maeda further discloses that the enteric coating may comprise a sustained release agent in addition to the enteric agent (paragraphs 61 and 71). The release modifying agent may comprise a sustained release agent such as polyvinyl alcohol, polyvinylpyrrolidone (“povidone”), hydroxypropylmethyl cellulose, ethyl acrylate-methyl methacrylate copolymer such as Eudragit NE30D, or a methacrylic acid copolymer L, or an enteric agent such as a methacrylic acid copolymer (paragraph 58). Maeda further teaches incorporating a lubricant such as polysorbate 80 (paragraph 52).
As to claims 1-12 and 14, it would have been prima facie obvious to one of ordinary skill in the art at the effective filing date of the present invention to modify the teachings of Lee by incorporating a modified release portion comprising polyvinyl alcohol, hydroxypropyl methyl cellulose, methyl acrylic acid copolymer, talc, purified water, sucrose cores as an inert particle, potassium hydroxide, and triethyl citrate or in the case of claim 8 further comprising polyethylene glycol, polysorbate 80, anhydrous ethanol, and a combination of methacrylic acid-ethyl acrylate copolymer and methacrylic acid-methylmethacrylate copolymer, because Maeda teaches that tegoprazan is a suitable drug for inclusion in a modified release composition such that the skilled artisan would have been motivated to formulate a modified release tegoprazan formulation and further suggests incorporating polysorbate 80 into tegoprazan formulations in order to impart lubricating properties, and because Wakeman teaches that a modified release formulation for providing controlled release of an active can be incorporated into the same single dosage form that also comprises an immediate release portion, wherein the modified release formulation comprises polyvinyl alcohol, hydroxypropyl methyl cellulose, methyl acrylic acid copolymer, talc, purified water, and inert sucrose particles, and because Wakeman further teaches that potassium salts and triethyl citrate are excipients that may be added to the formulation to control pH and impart plasticizing properties to the composition and that polyethylene glycol. The skilled artisan would have been motivated to make this modification in order to obtain the advantage of a single dosage form that when administered to a subject would provide both immediate therapeutic benefit from the immediate release portion while also providing an extended release of the active which would allow for less frequent dosing of the drug. The skilled artisan additionally would have had a reasonable expectation of success in formulating the tegoprazan modified release portion using the same release modifying agents utilized by Wakemen, including polyvinyl alcohol, hydroxypropyl methyl cellulose, and methyl acrylic acid copolymer, because Maeda teaches that these release modifying agents can successfully be used to form a modified release formulation for tegoprazan. The foregoing modifications are merely the combining of known prior art elements according to known methods to obtain predictable results, which is prima facie obvious. MPEP 2143.
Regarding claim 2, it further would have been prima facie obvious to formulate the composition as a capsule, because Wakeman expressly suggests formulating modified release compositions as a capsule.
As to claims 5-6 and 10-11, it further would have been prima facie obvious to allocate the 50-200 mg dosage taught by Lee between the modified and immediate release portions to arrive at the allocations recited by these claims, because the amount of active in the immediate release portion relative to the modified release is a result effective variable that will affect the blood concentrations, such as the Cmax, of the active over time. Generally, differences in concentration or temperature will not support the patentability of subject matter encompassed by the prior art unless there is evidence indicating such concentration or temperature is critical. “[W]here the general conditions of a claim are disclosed in the prior art, it is not inventive to discover the optimum or workable ranges by routine experimentation.” In re Aller, 220 F.2d 454, 456, 105 USPQ 233, 235 (CCPA 1955). Here, there is no evidence of record of any unexpected criticality of the recited amounts.
The resulting composition of the prior art as combined above will not dissolve under dissolution conditions for at least two hours as recited by claims 3 and 14 because it comprises the same ingredient recited by the claims, and a product cannot be separated from its properties. The U.S. Patent Office is not equipped with analytical instruments to test prior art compositions for the countless ways that an Applicant may present previously unmeasured characteristics. When the prior art appears to contain the same ingredients that are disclosed by Applicants' own specification as suitable for use in the invention, a prima facie case of obviousness has been established, and the burden is properly shifted to Applicants to demonstrate otherwise. See MPEP 2112.01.
Claim 13 is rejected under 35 U.S.C. 103 as unpatentable over Lee et al. (US Pat. Pub. 2018/0338954) in view of Wakeman et al. (US Pat. Pub. 2018/0360761) and Maeda et al. (U.S. Pat. Pub. 2018/0214460; published 8.2.2018) as applied to claims 1-12 and 14 above, and further in view of Turkyilmaz et al. (WO 2019/151966; published 8.8.2019).
The teachings of Lee, Wakemen, and Maeda are relied upon as discussed above, but they do not further expressly disclose that the granule comprises an outside layer comprising the microcrystalline cellulose, croscarmellose sodium and colloidal silicon dioxide (claim 13).
Turkyilmaz discloses pharmaceutical tablet compositions formed from granules and comprising a core and an outer layer comprising a disintegrant such as croscarmellose sodium (page 6, lines 24-25), a glidant such as colloidal silicon dioxide (page 7, lines 12-13), and a filler such as microcrystalline cellulose (page 7, lines 28-29).
As to claim 13, it would have been prima facie obvious to one of ordinary skill in the art at the effective filing date of the present invention to modify the teachings of Lee, Wakemen, and Maeda as combined supra by incorporating an outside layer on the granule comprising the microcrystalline cellulose, croscarmellose sodium and colloidal silicon dioxide, because Turkyilmaz teaches that pharmaceutical tablets formed from granules and comprising croscarmellose sodium as a disintegrant, colloidal silicon dioxide as a glidant, and microcrystalline cellulose as a filler may comprise these ingredients in the form of an outer layer. The structural configuration of claim 13 was known in the prior art with respect to these ingredients as is made clear by the disclosure of Turkyilmaz, and “[w]hen a patent simply arranges old elements with each performing the same function it had been known to perform and yields no more than one would expect from such an arrangement, the combination is obvious.” KSR v. Teleflex, 127 S.Ct. 1727, 1740 (2007) (quoting Sakraida v. A.G. Pro, 425 U.S. 273, 282 (1976)).
Response to Applicant’s Arguments
Applicant’s argument that the cited art does not teach or suggest a composition comprising both an immediate release and a modified release portion as recited by the claims as amended has been considered carefully, but is moot in light of the new grounds of rejection.
Conclusion
Applicant's amendment necessitated the new ground(s) of rejection presented in this Office action. Accordingly, THIS ACTION IS MADE FINAL. See MPEP § 706.07(a). Applicant is reminded of the extension of time policy as set forth in 37 CFR 1.136(a).
A shortened statutory period for reply to this final action is set to expire THREE MONTHS from the mailing date of this action. In the event a first reply is filed within TWO MONTHS of the mailing date of this final action and the advisory action is not mailed until after the end of the THREE-MONTH shortened statutory period, then the shortened statutory period will expire on the date the advisory action is mailed, and any nonprovisional extension fee (37 CFR 1.17(a)) pursuant to 37 CFR 1.136(a) will be calculated from the mailing date of the advisory action. In no event, however, will the statutory period for reply expire later than SIX MONTHS from the mailing date of this final action.
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/GAREN GOTFREDSON/Examiner, Art Unit 1619
/ANNA R FALKOWITZ/Primary Examiner, Art Unit 1600