DETAILED ACTION
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 .
Priority
The instant application was filed 16 December 2023 and is the national stage entry of PCT/CN2022/140816 filed 21 December 2022. The Applicant claims priority to foreign application CN202210682418.X filed 16 June 2022. An English copy of the foreign document has not been provided. Therefore, the effective filing date of the instant application is 21 December 2022.
Examiner’s Note
The Applicant's amendments and arguments filed 31 March 2026 are acknowledged and have been fully considered. The Examiner has re-weighed all the evidence of record. Rejections
not reiterated from previous office actions are hereby withdrawn. The following rejections are either reiterated or newly applied. They constitute the complete set presently being applied to the instant application. In the Applicant’s response, filed 31 March 2026, it is noted that claims 1, 6, 8, 9, 12, 15 have been amended and claim 16 has been newly added. Support for the amendments and new claims can be found from canceled claims. No new matter has been added.
Claim Rejections - 35 USC § 103
In the event the determination of the status of the application as subject to AIA 35 U.S.C. 102 and 103 (or as subject to pre-AIA 35 U.S.C. 102 and 103) is incorrect, any correction of the statutory basis (i.e., changing from AIA to pre-AIA ) for the rejection will not be considered a new ground of rejection if the prior art relied upon, and the rationale supporting the rejection, would be the same under either status.
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.
Claim(s) 1, 4-6, 8, 9, 12, 15, 16 is/are rejected under 35 U.S.C. 103 as being unpatentable over Okaji et al. (JP 2013253038 A), Ni et al. (CN 114767663 A), and Krekeler (US 2017/0182105 A1), as evidenced by clinpgx.org, and Cambridge.org.
Okaji teaches an oral film that includes 1-50% (entire teaching) of a drug compound 7-[4-(4-benzo[b]thiophene-4-yl-piperazine-1-yl)butoxy]-1H-quinoline-2-one (common name: brexpiprazole; evidenced by clinpgx.org, pg. 1) with a particle size of 5-60 microns and a thickness of 50-100 microns (claim 1), which is interpreted as partially addressing claim 1. The max particle size recited in Okaji is interpreted as 100% of the particles having a particle size within 5-60 microns. The composition may further comprise PEG as a plasticizer (pg. 3, para. 6) and hydroxypropyl cellulose as a water-soluble polymer (pg. 3, para. 4) in an amount of 10-98% (pg. 3, para. 5), addressing claim 9, and partially addressing claim 1. Water may be used as a solvent (pg. 4, para. 4), partially addressing claim 6. The pharmaceutical suspension in claims 6 and 16 are interpreted as the starting component before the film is made (evidenced by Krekeler, para. 106). Therefore, the liquid state of the composition during the processing steps in Okaji’s teaching (Example 1) is interpreted as the suspension component prior to obtaining the film.
Okaji does not specifically teach an amount of plasticizer or the ratios in claims 1, 4, 5, 8, 12, and 15. Okaji also does not teach an exact combination of the components in claim 1. Okaji does not specifically teach a viscosity of larger than 3,500 mPas for the composition in claims 1 and 6.
Ni teaches an oral film comprising aripiprazole, a film-forming agent, and a plasticizer (abs), where brexpiprazole and aripiprazole are both dopamine multifunctional agents used to treat schizophrenia (evidenced by cambridge.org, pgs. 1-2).
Krekeler teaches that a high viscosity for the suspension is preferable to obtain a stable suspension with a preferred viscosity of 1,000-5,000 mPas (para. 114; entire teaching) for orodispersible films.
In regards to selecting the combination of brexpiprazole, a plasticizer, and a film-forming agent, “[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)). “When the question is whether a patent claiming the combination of elements of prior art is obvious,” the relevant question is “whether the improvement is more than the predictable use of prior art elements according to their established functions.” (Id.). Addressing the issue of obviousness, the Supreme Court noted that the analysis under 35 USC 103 “need not seek out precise teachings directed to the specific subject matter of the challenged claim, for a court can take account of the inferences and creative steps that a person of ordinary skill in the art would employ.” KSR at 1741. The Court emphasized that “[a] person of ordinary skill is… a person of ordinary creativity, not an automaton.” Id. at 1742.
Consistent with this reasoning, it would have been obvious to have selected various combinations of various disclosed ingredients from within a prior art disclosure, to arrive at compositions “yielding no more than one would expect from such an arrangement.”
Okaji teaches compositions and methods for an oral film comprising brexpiprazole with a particle size of 5-60 microns, whereas the claimed invention is directed towards a composition comprising brexpiprazole with a diameter between 30 and 50 microns, a plasticizer, and a film-forming material. Since Okaji teaches the individual components of the claimed composition, it is obvious for one of ordinary skill in the art to select the different combinations of ingredients to arrive at the claimed invention with a reasonable expectation of success.
Since Okaji does not specifically teach a viscosity of larger than 3,500 mPas for the composition in claims 1 and 6, one of ordinary skill in the art would have been motivated to use Krekeler’s teaching of a preferred viscosity of 1,000-5,000 mPas for oral films. A skilled artisan would have recognized the added benefit of utilizing a high suspension in order to obtain a stable suspension and better product, as a result of combining the teachings. Generally, it is prima facie obvious to combine or substitute one equivalent component or process for another, each of which is taught by the prior art to be useful for the same purpose (see MPEP 2144.06).
In regards to the amounts of components and ratios in claims 1, 4, 5, 8, 12, and 15, Ni teaches plasticizers in an amount of 4-20% (abs). Therefore, 1-50% of brexpiprazole, 10-98% of a film-forming agent, and 4-20% of a plasticizer could result in ratios for brexpiprazole:(film-forming agent and plasticizer) and film-forming agent:plasticizer that is within the ranges of claims 1 and 4. Similarly, Okaji provides an example with 0.5 parts by mass of brexpiprazole and 7.6 parts by mass of the film-forming agent (Example 1). That being said and in lieu of objective evidence of unexpected results, the amounts of components in claims 1, 4, 5, 8, 12, and 15 can be viewed as a variable that achieves the recognized result of successfully making the brexpiprazole composition, which a skilled artisan would have been easily motivated to modify and adjust. The optimum or workable range of amounts and ratios can be accordingly characterized as routine optimization and experimentation (see MPEP 2144.05 (II)B). “[Discovery of an optimum value of a result effective variable in a known process is ordinarily within the skill of the art.” In re Boesch, 617 F.2d 272, 276 (CCPA 1980). Applicants provide no evidence of any secondary consideration such as unexpected results that would render the optimized amounts of structural units of formula (I) as nonobvious.
Response to Arguments
Applicant's arguments filed 31 March 2026 have been fully considered but they are not persuasive.
The Applicant claims a translation of the referenced patent PCT application was previously filed (Remarks, pg. 5).
An English copy of the application cannot be found. Therefore, the effective filing date of the instant application remains as 21 December 2022.
The Applicant argues that Okaji does note teach the three-component combination in amended claim 1 (Remarks, pgs. 6-7).
Applicant’s argument is not found persuasive. Okaji teaches an oral film that includes 1-50% (entire teaching) of a drug compound 7-[4-(4-benzo[b]thiophene-4-yl-piperazine-1-yl)butoxy]-1H-quinoline-2-one (common name: brexpiprazole; evidenced by clinpgx.org, pg. 1) with a particle size of 5-60 microns and a thickness of 50-100 microns (claim 1), which is interpreted as partially addressing claim 1. The composition may further comprise PEG as a plasticizer (pg. 3, para. 6) and hydroxypropyl cellulose as a water-soluble polymer (pg. 3, para. 4) in an amount of 10-98% (pg. 3, para. 5).
The Applicant argues that Okaji does not disclose the D90 particle size range (Remarks, pg. 7).
Applicant’s argument is not found persuasive. Okaji teaches a full particle size range of 5-60 microns for brexpiprazole, where the max particle size recited in Okaji is interpreted as 100% of the particles having a particle size within 5-60 microns.
The Applicant argues that Okaji does not solve the technical problem of controllable dissolution rate of the active ingredient or that there is no motivation to adjust the D90 range for brexpiprazole (Remarks, pgs. 7-8).
Applicant’s argument is not found persuasive. As previously stated, Okaji teaches a full particle size range of 5-60 microns for brexpiprazole, where it is broadly interpreted that the D90 size would also fall within this entire particle size range. Furthermore, Okaji’s formulation may include film-forming agents, such as hydroxypropyl cellulose, which are known in the art for controlling the release of active ingredients (evidenced by xyzchemical.com, pg. 2). Therefore, it is interpreted that Okaji’s formulation would also solve the technical problem of a controlled dissolution rate of the active ingredient.
The Applicant argues unexpected results regarding the D90 range and dissolution rates (Remarks, pgs. 8-9).
Applicant’s argument is not found persuasive. Tables 8 and 9 of the instant specification show a D90 value of 9.6 microns and 60.8 microns. The formulation includes brexpiprazole, along with other ingredients, such as polyethylene glycol. Any evidence of improved dissolution rates does not have a causal relationship with the merits and scope of the claimed invention, which is, broadly, an oral film consisting of brexpiprazole, a film-forming material, and a plasticizer. As such, the data are not commensurate in scope with the claims.
“For objective evidence of secondary considerations to be accorded substantial weight, its proponent must establish a nexus between the evidence and the merits of the claimed invention.” Wyers v. Master Lock Co., 616 F.3d 1231, 1246 [95 USPQ2d 1525] (Fed. Cir. 2010) (quotation omitted). Where the offered secondary consideration actually results from something other than what is both claimed and novel in the claim, there is no nexus to the merits of the claimed invention. Tokai Corp. v. Easton Enters., Inc., 632 F.3d 1358, 1369 [97 USPQ2d 1673] (Fed. Cir. 2011) (“If commercial success is due to an element in the prior art, no nexus exists.”); Ormco Corp., 463 F.3d at 1312 (“[I]f the feature that creates the commercial success was known in the prior art, the success is not pertinent.”); In re Woodruff, 919 F.2d 1575, 1578 [16 USPQ2d 1934] (Fed. Cir. 1990).
The Applicant argues that the viscosity limitation is not disclosed in the prior art (Remarks, pgs. 9-10).
Applicant’s argument is not found persuasive. The Applicant further argues that Krekeler’s teaching has a different active ingredient type, technical purpose, and technical effect (Remarks, pgs. 10-11). Krekeler teaches that a high viscosity for the suspension, in general, is preferable to obtain a stable suspension with a preferred viscosity of 1,000-5,000 mPas (para. 114; entire teaching) for orodispersible films. Furthermore, Krekeler’s composition comprising a film-forming agent is interpreted as controlling the release of active ingredients as well, which is interpreted as addressing the technical problems. Therefore, Krekeler’s teaching is interpreted broadly to include preferred viscosities for the majority of pharmaceutical suspensions. A skilled artisan would have recognized the added benefit of utilizing a high suspension in order to obtain a stable suspension and better product, as a result of combining the teachings. Generally, it is prima facie obvious to combine or substitute one equivalent component or process for another, each of which is taught by the prior art to be useful for the same purpose (see MPEP 2144.06).
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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/D.A.K./Examiner, Art Unit 1613
/ANDREW S ROSENTHAL/Primary Examiner, Art Unit 1613
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