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 . Claims included in prosecution are claims 1 and 29-31.
Previous Rejections
Applicants' arguments, filed 3/20/2026, have been fully considered. Rejections and/or objections not reiterated from previous office actions are hereby withdrawn. The following rejections and/or objections are either reiterated or newly applied. They constitute the complete set presently being applied to the instant application.
Claim Rejections - 35 USC § 103 (New)
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.
1. Claim 1 and 29-31 are rejected under 35 U.S.C. 103 as being unpatentable over Cao et al. (CN 104857517) (hereinafter Cao) in view of Jiang et al. (Drug Design, Development and Therapy, 2016; 10: 2181–2191) (hereinafter Jiang) and Peterson et al. (US 2016/0168646, Jun. 16, 2016) (hereinafter Peterson).
Cao teaches of an enzalutamide soft capsule and a preparation method thereof. The soft capsule can be prepared by mixing caprylic capric acid polyethylene glycol glyceride (i.e., solvent – Labrasol), butylated hydroxyanisole, butylated hydroxytoluene (i.e., antioxidants) and enzalutamide (i.e., androgen receptor inhibitor) to obtain the soft capsule content material (Abstract). Enzalutamide is an androgen receptor inhibitor that acts on different steps on the androgen receptor signaling pathway. It has been demonstrated that enzalutamide can competitively inhibit the binding of androgen to androgen receptor and inhibit nuclear translocation of the androgen receptor and interaction with DNA (Page 3, Paragraph 2). Enzalutamide belongs to insoluble drugs, has relatively low solubility in aqueous solutions and buffer solutions with different pH, and if a common oral solid preparation, such as a tablet or a capsule, is prepared, drug dissolution is slow and incomplete, and the bioavailability is relatively low, thereby limiting the efficacy of the oral preparation thereof. In the present product, the caprylic capric acid polyethylene glycol glyceride is selected as the excipient of the content. The excipient has excellent solubilizing capacity and can improve drug absorption; good compatibility with most active drugs, and improves the dispersion stability of the drug at the same time (Page 3, Paragraph 4). According to an embodiment, in the capsule content, the mass ratio of the enzalutamide, the caprylic capric acid polyethylene glycol glyceride (i.e., Labrasol), the butylated hydroxyanisole and the butylhydroxytoluene is 1: (10-25): (0.002-0.02): (0.002-0.02) (i.e., 100 parts : 1000-2500 parts : 0.2-2 parts : 0.2-2 parts). Therefore, the content is a pale yellow clear solution, the impurity content is relatively low, and the stability of the enzalutamide soft capsule is significantly improved (Page 4, Paragraph 4).
Cao differs from the instant claims insofar as not disclosing wherein the composition specifically comprises HC-1119.
However, Jiang teaches that deuterated enzalutamide (ENT) (N-trideuteromethyl enzalutamide, d3-ENT) (i.e., HC-1119) is a new molecular entity based on the structure of ENT. Deuterium incorporation can significantly alter the metabolic and pharmacokinetic profiles of the nondeuterated compound, thereby increasing the exposure of d3-ENT and reducing the dose requirement (Page 2182, Paragraph 4). The study found that the Cmax and AUC of the d3-ENT compared to ENT were 35% and 102% higher, respectively. This finding led to the conclusion that the d3-ENT dose requirement would need to be reduced appropriately since the AUC of the d3-ENT would increase significantly in humans (Page 2182, Conclusion).
Accordingly, it would have been obvious for one of ordinary skill in the art before the effective filing date of the claimed invention to have formulated Cao’s composition to comprise deuterated enzalutamide (i.e., HC-1119) instead of enzalutamide motivated by the desire to achieve the metabolic and pharmacokinetic profiles of the deuterated compound, thereby increasing the exposure of d3-ENT and reducing the dose requirement as taught by Jiang.
The combined teachings of Cao and Jiang do not disclose wherein the composition comprises 1-100 mg of the active.
However, Peterson teaches methods for treating triple negative breast cancer with an
androgen receptor inhibitor (Abstract). Suitable androgen receptor inhibitors include enzalutamide (¶ [0035]). Suitable dosing includes capsules comprising 40 mg enzalutamide (¶ [0036]).
Accordingly, it would have been obvious to one of ordinary skill in the art, prior to the filing of the instant application, to have formulated Cao’s capsule to comprise 40 mg enzalutamide since this a known and effective amount thereof for treating cancer using capsules as taught by Peterson.
Regarding the weight ratios recited in instant claim 1, in the case where the claimed ranges "overlap or lie inside ranges disclosed by the prior art" a prima facie case of obviousness exists. See MPEP 2144.05(A). As discussed above, in the capsule content of Cao’s soft capsule, the mass ratio of the enzalutamide, the caprylic capric acid polyethylene glycol glyceride, the butylated hydroxyanisole and the butylhydroxytoluene is 1: (10-25): (0.002-0.02): (0.002-0.02). This is interpreted as 100 parts enzalutamide; 1000-2500 parts caprylic capric acid polyethylene glycol glyceride; 0.2-2 parts butylated hydroxyanisole; and 0.2-2 parts butylhydroxytoluene. Accordingly, because the ratios recited in the instant claim overlap with the ranges disclosed by Cao, the ranges disclosed by Cao meets the instantly recited limitations.
Regarding the dosage recited in instant claims 30-31, where 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. See MPEP 2144.05(II)(A). As discussed above, enzalutamide is a therapeutic agent for cancer treatment, which makes dosages thereof a result effective variable, since amounts directly impact the therapeutic effect. Accordingly, it would have taken no more than the relative skills of one of ordinary skill in the art through routine experimentation to have arrived at the claimed dosage of enzalutamide to yield the desired therapeutic effect.
Therefore, the combined teachings of Cao, Jiang, and Peterson render obvious claims 1 and 29-31.
Response to Declaration by Xing Wei
Regarding the allegations presented in the Declaration submitted Mar. 20, 2026, Applicant has not submitted any data in the Declaration that would support their alleged finding. The Examiner respectfully reminds Applicant that Arguments presented by applicant cannot take the place of evidence in the record. See also MPEP § 2145(I). Furthermore, objective evidence which must be factually supported by an appropriate affidavit or declaration to be of probative value includes evidence of unexpected results. See, for example, In re De Blauwe, 736 F.2d 699, 705, 222 USPQ 191, 196 (Fed. Cir. 1984) ("It is well settled that unexpected results must be established by factual evidence." "[A]ppellants have not presented any experimental data showing that prior heat-shrinkable articles split. Due to the absence of tests comparing appellant’s heat shrinkable articles with those of the closest prior art, we conclude that appellant’s assertions of unexpected results constitute mere argument."). See also In re Lindner, 457 F.2d 506, 508, 173 USPQ 356, 358 (CCPA 1972); Ex parte George, 21 USPQ2d 1058 (Bd. Pat. App. & Inter. 1991). See also MPEP § 716.01(c).
While Applicant appears to make the assertion that their capsule outperformed that of the prior art, no tests comparing the two capsules were provided and as such, these arguments are not enough to provide evidence of unexpected results.
In light of the foregoing, the Examiner finds that the Declaration is insufficient to overcome the rejection of record and the rejection is maintained.
Response to Arguments
Regarding Applicant’s arguments about the alleged unexpected results recited in the Declaration submitted Aug. 11, 2025, please refer to the Response to Declaration above. The Examiner again notes that no data was provided in the declaration whatsoever, and that unexpected results must be established by factual evidence.
Furthermore, regarding Applicant pointing to Tables 1-3 of the instant specification, any differences between the claimed invention and the prior art may be expected to result in some difference in properties. The issue is whether the properties differ to such an extent that the difference is really unexpected. The burden is on applicant to establish that the results are in fact really unexpected and of statistical and practical significance. Ex parte Gelles, 22 USPQ2d 1318 (Bd. Pat. App. & Inter. 1992). See also MPEP § 716.02.
Applicant does not appear to have discussed same with respect to objective data. Since no comparative experimental data was presented, no detailed explanation of the components of the comparative product was provided, and no comparative data was explained by Applicant, one of ordinary skill in the art would not be able to properly ascertain how the comparative composition actually compares to the examples of the instant specification. In other words, without the comparative data, a meaningful comparison between the capsule of the prior art and the capsule of the instant claims cannot be made. As such, one of ordinary skill in the art cannot make the determination that Applicant’s finding that using HC-1119 of Cao results in a capsule content that doesn’t completely dissolve is truly “unexpected”.
The Examiner further notes, that while Applicant argues that the resulting comparative HC-1119 capsule content could not be completely dissolved, the Declaration discloses “We discovered that, using the formulation in Example 5 of Cao but the active ingredient of HC-1119, the ingredients could completely dissolve in the resulting soft gel formulation”. It appears that to the contrary of Applicant’s arguments, the Declaration discloses that the comparative soft gel content did indeed dissolve completely. As such, it is unclear what the alleged advantage/unexpected results are.
Regarding Applicant’s arguments that neither Jiang nor Peterson cure the alleged deficiencies of Cao, the Examiner submits that Jiang cures any alleged deficiencies of Cao where Jiang provides strong motivation to use deuterated enzalutamide (i.e., HC-1119) such as the improved metabolic and pharmacokinetic profiles. Furthermore, Peterson cures any alleged deficiencies of Cao where Peterson discloses that 40 mg enzalutamide is a known and effective amount of that active ingredient.
Conclusion
Claims 1 and 29-31 are rejected.
No claims are allowed.
THIS ACTION IS MADE FINAL. 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.
Any inquiry concerning this communication or earlier communications from the examiner should be directed to Abdulrahman Abbas whose telephone number is (571)270-0878. The examiner can normally be reached M-F: 8:30 - 5:30.
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/A.A./Examiner, Art Unit 1612
/SAHANA S KAUP/Supervisory Primary Examiner, Art Unit 1612
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