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
This application filed 08/30/2022 is a 371 of PCT/JP2021/007790 filed on 03/02/2021 which claims foreign priority to JAPAN 2020-035827 filed on 03/03/2020 and JAPAN 2020-147340 filed on 09/02/2020.
DETAILED ACTION
The Office Action is in response to the Applicant's reply filed December 26, 2025 to the non-final rejection made on October 7, 2025.
Claims 1-18, and 20-27 are herein acted on the merits.
Information Disclosure Statement
The information disclosure statement(s) (IDS) filed on 4/7/26 and 4/23/26, is in compliance with the provisions of S7 CFR 1.97. Accordingly, the IDS is being considered by the Examiner.
Response to Arguments
Applicant's arguments over the 35 U.S.C. 112(b) or 35 U.S.C. 112 (pre-AIA ), second paragraph rejection of claim 16 is persuasive. The rejection is herewith withdrawn.
Applicant's arguments over the 35 U.S.C. 112(b) or 35 U.S.C. 112 (pre-AIA ), second paragraph rejection of claims 13 and 18-19 is persuasive. The rejection is herewith withdrawn.
Applicant's arguments over the 35 U.S.C. 112(b) or 35 U.S.C. 112 (pre-AIA ), second paragraph rejection of claim 15 is not persuasive. The rejection is herewith maintained. The Examiner states the recitation of a single ester formula, R₁COOR₂, is unclear when the claims also encompass a monoester, diester, and triester. Further, because the claim recites "one of R₁ and R₂" is the long chain and "the other" is the shorter chain, it means the structure can be either RlongCOORshort or RshortCOORlong. While chemically this is one ester type, if the "substituted" groups are different, this creates two potential structural isomers.
Applicant's arguments over the 35 U.S.C. 103 rejection over Bodor et al. (WO2017015485A1 – IDS c 11/30/2022) of claims 1-27 is not persuasive. The rejection is herewith maintained. Applicant arguments over Bodor depend on amendments made to the claims. For example, Applicant agues the anhydrous formulation of Bodor does not disclose or suggest low aqueous formulations where decrease in viscosity over time is suppressed.
In response, the Examiner states the specifications does state the low and non- aqueous formulations have suppressed decreased viscosity over time. Furthermore, the Examiner points out that the low aqueous formulations claimed are encompassed by Bodor. Specifically, Bodor teaches the compositions may also contain conventional additives such as solvents, stabilizers, wetting agents, emulsifiers, buffers, binders, disintegrants, fragrances, lubricants, glidants, antiadherents, propellants, and the like, just so long as the additives and compositions are anhydrous, that is, free of water to the extent required to avoid significant negative impact on the storage stability of the composition (by hydrolysis of the ester drug). [0054] Clearly, the reference renders obvious a low aqueous formulation.
The rejections are as 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.
Claim 15 is rejected under 35 U.S.C. 112(b) or 35 U.S.C. 112 (pre-AIA ), second paragraph, as being 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. It is unclear what “the other R1 and R2” is referring to in the claims.
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 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.
Claims 1-18, and 20-27 are rejected under 35 U.S.C. 103 as being unpatentable over Bodor et al. (WO2017015485A1 – IDS c 11/30/2022).
The claims read on a pharmaceutical formulation for applying as an external application to the surface of the human body, wherein the formulation contains: (a) sofpironium bromide, (b) one or more kinds of water-soluble polymers, and (c) ethanol, wherein the formulation has a pH of 5.2 or lower and is a uniformly dispersed, low water content formulation with a water content of 1 w/w% or more and 5 w/w% or lower, and wherein the pH is measured at any one or more time points selected within 6 months after preparation of the formulation, the pH is determined by measuring pH of the formulation stored at room temperature, and the pH is a value obtained after a pH electrode for non- aqueous solvent is immersed in the formulation for 5 minutes.
Bodor et al. teaches a composition comprising the following ingredients: compound having the formula: (sofpironium bromide)
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(2) said compound having the R stereoisomeric configuration at the 2 position and the R, S or RS stereoisomeric configuration at the 1 ' and 3' positions, or being a mixture thereof; being a mixture thereof;
(b) anhydrous ethanol;
(c) optionally, at least one gelling or viscosity-controlling ingredient; and
(d) optionally, at least one additional carrier or excipient; provided that said topical composition is anhydrous and comprises from about 1 % to about 25 % w/w or w/v of the compound of formula (2), said composition having greater storage stability compared to a composition comprising an aqueous solvent or aqueous buffer, said ingredients being present in amounts such that the product of any transesterification is the same as the compound of formula (2). (claim 1) The claims recite the use of a gelling or viscosity-controlling ingredient is hydroxypropyl cellulose and further comprising at least one member selected from the group consisting of dimethicone, cyclomethicone, myristyl propionate, isopropyl myristate and C12-C15 alkyl lactate; wherein the cyclomethicone is cyclomethicone 5-NF and/or where the dimethicone is dimethicone 350 c5t. (claim 17-18) The active ingredient is dissolved in anhydrous ethanol as a solvent, in which the compound is soluble or at least slightly soluble. It is preferred that the apparent pH of the composition be acidic (i.e. apparent pH <7). [0055] Bodor et al. teaches KLUCEL MF hydroxylpropyl cellulose (HPC and DOW CORNING® DIMETHICONOL BLEND 20 is a unique blend of silicone gum (6%) in dimethicone exemplified in formulations [0096]- [0097]. BHT is butylated hydroxytoluene also known as dibutylhydroxytoluene. Table VIII describes a composition GEL 3 comprising: HPC in 1.25 w/w%, BBI-4000 in 5.0%, hexylene glycol, citric acid anhydrous in 0.001%, C12-C15alkyl lactate in 2.5%, ethanol anhydrous qs to 100.
Table III describes
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With respect to viscosity, Bodor et al. teaches a “preferred gelling or viscosity controlling agent can be a modified cellulose, e.g., hydroxypropyl cellulose (HPC), such as the commercially available KLUCEL™, which can preferably provide viscosity of the composition of from about 100 to about 10,000 cps.” [0032] (reads on the visocosity of lcaim 24-25.
The recitation wherein the pH is measured at any one or more time points selected within 6 months after preparation of the formulation, the pH is determined by measuring pH of the formulation stored at room temperature, and the pH is a value obtained after a pH electrode for non- aqueous solvent is immersed in the formulation for 5 minutes are product by process claims. It is well settled in patent law that product-by-process claims are not limited to the manipulations of the recited steps, only the structure implied by the steps. See MPEP § 2123. The court in In re Thorpe held, “even though product-by-process claims are limited by and defined by the process, determination of patentability is based on the product itself. The patentability of a product does not depend on its method of production. If the product in the product-by-process claim is the same as or obvious from a product of the prior art, the claim is unpatentable even though the prior product was made by a different process.” See 777 F.2d 695, 698, 227 USPQ 964, 966 (Fed. Cir. 1985). In this case, the method wherein the pH is measured at any one or more time points selected within 6 months after preparation of the formulation, the pH is determined by measuring pH of the formulation stored at room temperature, and the pH is a value obtained after a pH electrode for non- aqueous solvent is immersed in the formulation for 5 minutes as claimed does not render structural limitations to the claimed composition. Thus, the processes are not given patentable weight. In claim 4, the formulation “are uniformly dissolved” is not given patentable weight. However, the reference teaches the active ingredient is dissolved [0055].
With respect to the viscosity of the formulation is 10 to 1000 mPass at 25°C after storage at room temperature for 36 months from preparation of the formulation or after storage at 40°C for 3 months from preparation of the formulation or purity of sofpironium bromide is 90 w/w% or higher after storage at room temperature for 36 months from preparation of the formulation, or after storage at 40°C for 3 months from preparation of the formulation recited in claims 25 and 27, Applicant is informed that a prior art composition that comprise all elemental components of the instantly created composition would meet all functional characteristics of the created composition, because such characteristics are inseparable from the composition. The recitation “for medical care, therapeutic treatment, or prevention of a disease selected from the group consisting of hyperhidrosis, overactive bladder, chronic obstructive pulmonary disease, cardiac disease, salivation, ocular disease, and bronchial asthma,” is an intended use of the formulation.
Bodor teaches the compositions may also contain conventional additives such as solvents, stabilizers, wetting agents, emulsifiers, buffers, binders, disintegrants, fragrances, lubricants, glidants, antiadherents, propellants, and the like, just so long as the additives and compositions are anhydrous, that is, free of water to the extent required to avoid significant negative impact on the storage stability of the composition (by hydrolysis of the ester drug). [0054]
The prior art does not exemplify a formulation having water content of 1 w/w% or more and 5 w/w% or lower; a pH of 5.2 or lower with the antioxidant and solvent.
It would have been obvious to one of ordinary skill in the art at the time of filing to modify to a formulation having a pH of 5.2 or lower and have a low water content in the amounts claimed. The motivation to modify the formulation is because Bodor et al. teaches the active ingredient is dissolved in anhydrous ethanol as a solvent, in which the compound is soluble or at least slightly soluble. it is preferred that the apparent pH of the composition be acidic (i.e. apparent pH <7) and further that the additives and compositions are anhydrous, that is, free of water to the extent required to avoid significant negative impact on the storage stability of the composition (by hydrolysis of the ester drug). [0054] Hence a skilled artisan would have had reasonable expectation of success in attaining a dissolved anhydrous formulation with an acidic pH range overlapping with the prior art and free of water to the extent required to avoid significant negative impact on the storage stability of the composition (by hydrolysis of the ester drug).
Conclusion
No claims allowed.
The arguments are not persuasive and the rejection is made FINAL.
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 extension fee 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.
Any inquiry concerning this communication or earlier communications from the examiner should be directed to LAYLA SOROUSH whose telephone number is (571)272-5008. The examiner can normally be reached on Monday thru Friday; 8:30 AM to 5:00 PM EST.
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/LAYLA SOROUSH/ Primary Examiner, Art Unit 1622
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