DETAILED ACTION
Claims 1-16 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 .
Priority
Receipt is acknowledged of certified copies of papers required by 37 CFR 1.55.
Information Disclosure Statement
The information disclosure statement (IDS) submitted on 11/26/25 was filed prior to the mailing date of a first Action on the merits. The submission is in compliance with the provisions of 37 CFR 1.97. Accordingly, it was considered by the Examiner.
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 6-8 and 11 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 6 recites that the oral solid preparation comprises a binder, but base claim 1 does not recite a binder. Since claim 6 is reciting an additional ingredient not recited by the base claim, claim 6 should recite that the preparation “further” comprises a binder, for clarity. Dependent claims 7-8 do not clarify the point of confusion so are also rejected.
Claim 11 recites that the oral solid preparation comprises an excipient, but base claim 1 does not recite a binder. Since claim 6 is reciting an additional ingredient not recited by the base claim, claim 6 should recite that the preparation “further” comprises an excipient, for clarity.
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 1-16 are rejected under 35 U.S.C. 103 as unpatentable over Dan et al. (US Pat. Pub. 2019/0175600; of record in IDS) in view of Yanagida et al. (US Pat. Pub. 2011/0027362).
As to claims 1-16, Dan discloses an oral solid preparation such as a tablet (claim 14) comprising 3- [2-fluoro-5-(2,3-difluoro-6-methoxybenzyloxy)-4-methoxypheny1]-2,4-dioxo-1.,2,3,4- tetrahydrothieno[3,4-d|pyrimidine-5-carboxylic acid (i.e., “linzagolix”) or a pharmaceutically acceptable salt thereof (paragraphs 15, 27), wherein the composition may comprise an excipient (claim 11) such as lactose, a disintegrant such as carboxymethyl cellulose, and a binder (claim 6) such as hydroxypropyl methyl cellulose (“hypromellose” of claim 7)(paragraph 28).
Regarding claim 2, the salt may be the choline salt (claim 2 of Dan).
Regarding claim 13, the linzagolix may be present in the amount of 75 mg (paragraph 15).
As to claims 1-16 Dan does not further expressly disclose that the disintegrant is among those recited by claim 1 such as carmellose sodium or croscarmellose calcium, that the excipient includes crystalline cellulose as recited by claim 1 and in the amount of claim 10, nor the presence of low-substituted hydroxypropyl cellulose as recited by claim 1, nor that the preparation comprises a granulated material comprising the linzagolix, crystalline cellulose, low-substituted hydroxypropyl cellulose, and disintegrant as recited by claim 2, nor the dissolution ratio of claim 4, nor the total amount of low-substituted hydroxypropyl cellulose and disintegrant (claim 5), nor the amount of binder (claim 8), nor the amount of linzagolix as a weight percent (claim 9), nor that the excipient comprises D-mannitol (claim 12), or that the tablet is a film-coated tablet (claim 15) comprising one of the coating agents of claim 16 such as hypromellose (claim 16).
Yanagida discloses a film-coated tablet comprising a quinazoline active, a binder such as hydroxypropylcellulose, Hypromellose, or polyvinyl alcohol, one or more fillers selected from lactose, crystalline cellulose, and D-mannitol, a cellulose disintegrant such as one or more of carmellose calcium and low-substituted hydroxypropylcellulose (claims 1-8 and 12-14 of Yanagida), wherein the film coating may comprise Hypromellose (paragraph 71). The binder is present in the amount of 0.1-10 wt%, which encompasses the range of claim 8 (paragraph 70), and the amount of the crystalline cellulose is most preferably 30-60 wt%, which is within the range of claim 10 (paragraphs 55 and 58), and the total amount of cellulose disintegrants is most preferably 2-10 wt% (paragraph 64), which is within the range of claim 5. Yanagida teaches that the film coating helps to prevent decomposition from light exposure but results in less favorable dissolution properties, but that the tablet disclosed therein has good dissolution properties even in the presence of the film coating (paragraphs 4-6). Yanagida further teaches that the tablet is formed by mixing granulated particles comprising the ingredients (paragraph 52). Yanagida discloses a working example showing that the tablet has a dissolution rate of 89% after 15 minutes, which is within the range of claim 4 (Table 1).
As to claims 1-16, 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 Dan composition by formulating the tablet composition as a film-coated tablet wherein the film comprises Hypromellose, and by selecting carmellose calcium and low-substituted hydroxypropyl cellulose as the disintegrants, and crystalline cellulose and D-mannitol as excipient fillers as recited by claims 1, 11-12, and 15-16 and in the form of a granulated material comprising the linzagolix as recited by claim 2, because Yanagida teaches that a film coating on the tablet can help protect against degradation from light but can have harmful effects on dissolution properties which can be overcome by use of the disintegrants and fillers discussed above in the form of a granulated material that is mixed together and formed into a tablet, such that the skilled artisan reasonably would have expected that the Dan composition could be formulated in the same manner to advantageously have protection against light degradation while maintaining good dissolution properties.
Regarding claims 5, 8, and 10, it further would have been prima facie obvious to select an amount of the total amount of cellulose disintegrants (i.e., low-substituted hydroxypropyl cellulose and carmellose calcium), binder, and crystalline cellulose that are within the claimed ranges, because Yanagida expressly teaches that they should be used in amounts within the recited range. Additionally, discovering optimum or working ranges involves only routine skill in the art in cases where the general conditions of a claim are disclosed in the prior art. In re Aller, 220 F.2d 454, 456, 105 USPQ 233, 235 (CCPA 1955).
As to claim 9, it further would have been prima facie obvious to select an amount of linzagolix active that is within the recited range, because the amount of an active is a result effective variable that will affect the therapeutic efficacy of the composition and with a reasonable expectation of success because the skilled artisan would be optimizing the same active compound that is recited by the claims. Generally, differences in concentration 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).
The resulting tablet will possess the dissolution ratio of claim 4 because it comprises the same ingredients recited by the claims, and a product cannot be separated from its properties, and further because Yanagida discloses that a tablet comprising the same ingredients recited by the claims possessed a dissolution within the recited range. 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.
Conclusion
Any inquiry concerning this communication or earlier communications from the examiner should be directed to GAREN GOTFREDSON whose telephone number is (571)270-3468. The examiner can normally be reached on M-F 9AM-6PM.
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/GAREN GOTFREDSON/Examiner, Art Unit 1619
/ANNA R FALKOWITZ/ Primary Examiner, Art Unit 1600
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