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 30 March 2023 and is the national stage entry of PCT/EP2021/076996 filed 30 September 2021. The Applicant claims priority to provisional application 63/086,691 filed 02 October 2020 and several foreign documents with the earliest priority date of 08 October 2020. The earliest priority date for the limitation including water in claim 21 appears to be 11 January 2021. Claims 1-14, 16-21 have an effective filing date of 08 October 2020.
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 Rejections not reiterated from previous office actions are hereby withdrawn.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 claim 1 has been amended and no new claims have been added or canceled. Support for the amendment can be found on pg. 11 of the specification. 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) 1-14, 16-21 is/are rejected under 35 U.S.C. 103 as being unpatentable over Bittorf (US 2009/0247468 A1), Friesen (Hydroxypropyl Methylcellulose Acetate Succinate-Based Spray-Dried Dispersions: An Overview, Molecular Pharmaceutics, 2008), and Schade (Dasatinib, a small-molecule protein tyrosine kinase inhibitor, inhibits T-cell activation and proliferation, Blood, 2007), as evidenced by go.drugbank.com.
Bittorf teaches methods of spray drying (entire teaching; abs) dispersions (para. 7) comprising an active ingredient (para. 199), 5-30% (para. 104) HPMCAS (para. 153), water (para. 16), alcohols (para. 141), acetic acid (para. 16), wherein the amounts of solvents may have a wide range, such as 0.1-15% acetic acid and 40-80% of a volatile solvent, such as an alcohol (paras. 18, 141). The composition may be a solution, which is interpreted as a single-phase solution (para. 8), thus far partially addressing claim 1. The compound of interest possibly becoming supersaturated (para. 165), as well as the use of a non-volatile solvent, such as acetic acid (paras. 140, 142), to increase the solubility of the drug is interpreted as addressing the solubility limitation in claim 2. The amount of active ingredient may have about 5-95% (para. 199), addressing claims 3, 9, and 11. The composition comprising 0.1-15% acetic acid (para. 18) addresses claim 5. The composition comprising about 0.1-15% (para. 22) water as a solvent and 5-30% of HPMCAS addresses claims 7 and 10. The drugs or active agent may be any beneficial therapeutic agent (para. 107), which is interpreted as a biologically active compound in claim 12 and also addressing the drug limitation in claim 13. Bittorf’s uses Telaprevir as an example of an active agent suitable in this composition. Telaprevir has a predicted pKa of 11.86 (go.drugbank.com, pg. 9), addressing claim 14. The composition comprising HPMCAS, Applicant’s election, is interpreted as addressing the pharmaceutically acceptable dispersion polymer limitation in claim 16, as well as claims 17 and 18. The composition may comprise residual solvents (para. 279), which includes acetic acid, and the residual solvents may be evaporated, which is interpreted as being below 5,000 ppm in claims 19 and 20. The composition comprising water and an alcohol as solvents is interpreted as addressing the limitation in claim 21.
In regards to the amendments in claim 1, Bittorf teaches the formation of a solution by solubilizing a polymer (para. 7). The preparation to be spray dried includes a therapeutic agent and may form a slurry (para. 115). Solvents, such as acetic acid (para. 16), are used to dissolve the drug (para. 15).
Bittorf does not teach Dasitinib or a specific alcohol in claims 1 and 6. Bittorf does not teach specific molar equivalents of acetic acid in claim 4 or weight ratios of the alcohol to water in claim 8.
Friesen teaches that solid dispersions with HPMCAS are very soluble in solvents, such as methanol, and also provides an economical advantage for the spray drying process (pg. 1009).
Schade teaches that Dasatinib is an oral small molecule and tyrosine kinase inhibitor used to treat certain cancers (abs).
In regards to selecting the combination of an active agent, an alcohol, water, HPMCAS, and acetic acid in Bittorf’s teaching, “[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.”
Since Bittorf does not teach Dasitinib or a specific alcohol in claims 1 and 6, one of ordinary skill in the art would have been led to use Friesen and Schade’s teachings of methanol and Dasatinib, as Friesen teaches that HPMCAS and methanol provide economical and solubility advantages when used together and Bittorf teaches that the drug used in their composition may be a small molecule drug (para. 10). A person of ordinary skill in the art would have been motivated to combine the teachings depending on what the skilled artisan intended to treat, such as certain cancers where a small molecule drug, such as Dasatinib would be desirable to use. Applicant’s election of Dasatinib is interpreted as addressing the pKa, solubility, and Bronstedt base limitations in claim 1.
In regards to specific molar equivalents of acetic acid in claim 4 or weight ratios of the alcohol to water in claim 8, Bittorf teaches 0.1-15% acetic acid (para. 18), 40-80% of a volatile solvent, such as an alcohol (paras. 18, 141), and 1-15% (para. 22) water. That being said and in lieu of objective evidence of unexpected results, the molar equivalence and weight ratios of solvents can be viewed as a variable that achieves the recognized result of successfully performing the method of spray drying a solid dispersion of an active agent. 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 solvents as nonobvious.
Response to Arguments
Applicant's arguments filed 31 March 2026 have been fully considered but they are not persuasive.
The Applicant argues that the art does not teach the amendments in claim 1 (Remarks, pgs. 6-7).
The Applicant argues that Bittorf does not teach or suggest dissolving the dispersion polymer in a solvent, then adding the active agent to form a slurry, and then adding acetic acid to the slurry (Remarks, pg. 7). Applicant’s argument is not found persuasive. In regards to the amendments in claim 1, Bittorf teaches the formation of a solution by solubilizing a polymer (para. 7). The preparation to be spray dried includes a therapeutic agent and may form a slurry (para. 115). Solvents, such as acetic acid (para. 16), are used to dissolve the drug (para. 15). Therefore, Bittorf broadly teaches the method steps recited in instant claim 1.
The Applicant argues that Bittorf does not use acetic acid in any examples (Remarks, pgs. 7-8).
Applicant’s argument is not found persuasive. The Applicant is erroneously pointing to narrow embodiments expressly disclosed within the prior art reference as representing the sum total of information conveyed by each. Art is art, not only for what it expressly teaches, but also for what it would reasonably suggest to the skilled artisan, including alternative or non-preferred embodiments (see MPEP § 2123).
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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