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 .
Election/Restrictions and Status of the Claims
Applicant's election with traverse of butylated hydroxytoluene antioxidant; microcrystalline cellulose and in combination pregelatinized starch as filler; crospovidone disintegrant; povidone as binder; magnesium stearate as lubricant; and colloidal silicone dioxide as antisticking agent species in the reply filed on 7/8/2026 is acknowledged. The traversal is on the ground(s) that the subject matter of all [groups of] species is sufficiently related such that there is no undue burden for searching and examining all species. This is not found persuasive because multiple burdensome search queries would be necessary to search all items and/or combinations.
The requirement is still deemed proper and is therefore made FINAL.
Claims 13, 14, and 18 are withdrawn from further consideration pursuant to 37 CFR 1.142(b), as being drawn to nonelected species, there being no allowable generic or linking claim. Applicant timely traversed the restriction (election) requirement in the reply filed on 7/8/2026.
Accordingly, claims 1-12, 15-17, and 19 are pending and under current examination.
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 6/5/2024 and 7/19/2024 have been 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 8-12, 15-17, and 19 are 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. The aforementioned claims use numerous tilde symbols in conjunction with recitations that appear to be various and/or alternate numerical ranges. While a tilde symbol may be used in informal language to indicate ranges, among other uses or expressions of approximation, its meaning and metes and bounds are considered nonstandard and subject to variable interpretation from one artisan to another. Accordingly, the metes and bounds of items modified or indicated by the tilde symbol are considered indefinite. Moreover, a tilde is generally used to mean about or approximately, however as used in the claims it appears to indicate a value within a range, the metes and bounds of which are not defined. Limitations are not imported from the specification into the claims.
A broad range or limitation together with a narrow range or limitation that falls within the broad range or limitation (in the same claim) may be considered indefinite if the resulting claim does not clearly set forth the metes and bounds of the patent protection desired. See MPEP § 2173.05(c). In the present instance, claims 8-12, 15-17, and 19 recites the broad recitation ranges, and the claims also recite, in some instances multiple recitations, of relatively narrow ranges following said relatively broad ranges/limitation. The claim(s) are considered indefinite because there is a question or doubt as to whether the feature introduced by such narrower language is (a) merely exemplary of the remainder of the claim, and therefore not required, or (b) a required feature of the claims.
Claim 19 recites the limitation "the plain tablet of the tablet" in the last two lines. There is insufficient antecedent basis for this limitation in the claim because there is no prior recited or defined “plain tablet”.
Appropriate clarifications is required.
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.
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 1-7 are rejected under 35 U.S.C. 103 as being unpatentable over CN107663177 (Woo et al., hereafter “Woo”) in view of WO2010/027471A2 (Zeitels et al., “Zeitels”).
The instant claims are drawn to a composition characterized by comprising 107 or a pharmaceutically acceptable salt thereof and an antioxidant.
Woo teaches a salt of 3-(4-(dihexylamino)-3-fluorophenyl)-2,6-dimehylpyrimidin-4(3H)-one in a pharmaceutical composition containing said salt for treating a tissue or organ fibrosis disorder condition. Woo’s formulations are said to demonstrate good biological activity, small undesired and/or toxic side effects, and good stability (see [0001] and [0007])(limitations of claim 1). Woo specifies the hydrochloride salt (see Woo claim 1)(limitation of claim 2). Woo specifies also that the pharmaceutically acceptable carriers may include various functional agents including antioxidants (see page 8 of 14 of translation, paragraph starting “Materials that can serve…”, last word of paragraph). Woo specifies oral administration in the form of tablets for instance (page 8 of 14 of translation, third paragraph which begins “Oral administration may be in the form of: tablets…”)(limitation of claim 5).
Woo does not specify an embodiment necessarily including said antioxidant or name antioxidant suggestions.
Zeitels cures this deficiency. Zeitels teaches formulations which may include for instance an active agent which is an anti-fibrotic agent in a carrier formulation (see [0014] and [0015] for instance). Zeitels teaches that antioxidants exemplary include butylated hydroxytoluene (see [0070] lines 3 and 4)(limitation of claims 3 and 4).
Both Woo and Zeitels pertain to formulations including anti-fibrotic active agents for pharmaceutical applications. It would have been prima facie obvious to one of ordinary skill in the art at the time the invention was filed to combine Zeitels’ antioxidant which is butylated hydroxytoluene in place of Woo’s generically disclosed antioxidant component, with a reasonable expectation of success. One would have been motivated to do so to provide desirable antioxidant benefit and in Woo’s absence of particularly suggestion as to how to do so would have looked to Zeitels’ teaching of the state of the art with regard to antioxidant compounds known to be useful in similar formulations.
Regarding the further presence of at least one excipient as in claims 6 and 7, Zeitels teaches at least one of these agents to be desirably included by the following teachings: Zeitels teaches microcrystalline cellulose among exemplary diluents (see [0066]) and celluloses in general as well as pregelatinized starch among exemplary dispersing agents (see [0067]); Zeitels teaches crospovidone among exemplary dispersing agents (see[0067]); Zeitels teaches magnesium stearate may be included for its benefit as a lubricating agent (see[0072])(limitation of claims 6 and 7); and Zeitels teaches colloidal clays including silicates among exemplary surface active agents (see [0068]).
Claims 8-12, 15-17, and 19 are rejected under 35 U.S.C. 103 as being unpatentable over CN107663177 (Woo et al., hereafter “Woo”) in view of WO2010/027471A2 (Zeitels et al., “Zeitels”) as applied to claims 1-7 above, and further in view of WO2005034916 (Becker et al., hereafter “Becker”).
The teachings of Woo and Zeitels have been delineated above. Woo and Zeitels generally do not specify amounts of excipient components. Becker cures this deficiency.
Regarding the antioxidant content as in claim 8, Becker teaches treatment of autoimmune diseases for instance including conditions encompassing fibrosis (see page 18). Becker’s formulations include a stabilized active agent achieved by inclusion of an antioxidant amount up to 1% and more preferably 0.01 to 0.5% and particularly preferred an amount of 0.2% by weight (see page 7 of translation, second full paragraph)(limitation of claim 8).
Regarding claim 10, Becker specifies a filler component in a solid formulation in an amount of 10 to 90%, more preferably 10 to 50%, and most preferably 15 to 35% by weight (see page 15, second to last paragraph)(limitation of claim 10). Microcrystalline cellulose may be this filler component. Similarly, regarding the instant election wherein the filler is a combination of microcrystalline cellulose and pregelled starch, Becker teaches that these equivalently may be combined as extrusion aids (page 3, second paragraph). Components recited as optional are interpreted to be optional and thus not required to be included and/or included within the recited amounts.
Wood and Zeitels particularly pertain to anti-fibrosis compounds or compositions, and Zeitels and Becker pertain to stabilized formulations wherein the active agent may be for a purpose of anti-fibrosis or a similar condition. It would have been prima facie obvious to one of ordinary skill in the art at the time the invention was made to adjust the amounts of functional components taught by Zeitels and Becker to formulate Wood’s known active agent, with a reasonable expectation of success. One would have been motivated to do so to facilitate stable storage and delivery properties in accordance with the state of the art for similarly formulated products as in Zeitels and as further specified in Becker.
As to the formulation components detailed in claim 11, the 3-(4-(dihexylamino)-3-fluorophenyl)-2,6-dimethylpyrimidin-4(3H)-one or a pharmaceutically acceptable salt thereof has been addressed above by Woo. Becker specifies that the solid granules may be dispensed in a capsule for instance (see page 3, line 6). The antioxidant claimed is addressed above by Becker. The claimed filler component has been addressed above by Becker. As to a disintegrant component, Becker teaches this in the last line on page 9. As to an anti-sticking agent, Becker teaches this benefit agent as well (see page 16, third paragraph, item “c”). As to a lubricant, Becker teaches this component (see page 16, second paragraph). As to the optionally recited components of binder and mass ratio, these are considered met by the prior art since the claim language does not require them.
Regarding claim 15, Becker also teaches tablet formulations (see Becker claim 3 for instance). The components of claim 15 have been otherwise addressed above in regard to claim 11.
As to claim 19, Becker teaches an enteric coating may be added (see page 1, item number 1 near bottom of page).
As to the amount of 3-(4-(dihexylamino)-3-fluorophenyl)-2,6-dimethylpyrimidin-4(3H)-one or a pharmaceutically acceptable salt thereof, as in claims 9, 12, 16, and 17, Becker teaches the active agent for instance which may be rapamycin, to be included in a weight percentage of 9.09% of a solid dispersion for instance (see Table 2; see also Becker claim 13 and page 18 list of conditions treatable with Becker’s products).
As to the instantly elected butylated hydroxytoluene antioxidant as in claim 12, Becker embodies this component in an amount of about 0.05 to about 1% (see pager 11, third paragraph, lines 2-3).
As to the instantly elected microcrystalline and pregelatinized starch filler as in claim 12, Becker specifies microcrystalline cellulose and pregelled starch to be included as an extrusion aid (page 3, second paragraph, lines 1-3) and that generally these components function as binders, carriers, or excipients with an embodiment demonstrating microcrystalline cellulose, an equivalent to the elected combination, to be included in an amount of 20%, 25%, or 35% (see page 31, “3. Preparation of pellets”, table entry), a value included within the instantly claimed range of filler.
As to the instantly elected crospovidone disintegrant as in claim 12, Example 11 demonstrates this component in an amount of 6% (table on page 34).
As to the instantly elected povidone binder as in claim 12, Becker demonstrates povidone included at 5% (see page 31, first table on page).
As to the instantly elected magnesium stearate lubricant as in claim 12, Example 11 demonstrates this component in an amount of 1% (table on page 34),
As to the instantly elected colloidal silicone dioxide anti-sticking agent as in claim 12, Becker teaches this component in an amount of 1 to 50% by weight of the total formulation (see page 17, first full paragraph).
Limitations of claims 16 and 17 have been addressed above in regard to claim 12. In the case where the claimed ranges “overlap or lie inside ranges disclosed by the prior art” a prima facie case of obviousness exists. In re Wertheim, 541 F.2d 257, 191 USPQ 90 (CCPA 1976); In re Woodruff, 919 F.2d 1575, 16 USPQ2d 1934 (Fed. Cir. 1990). Moreover, “Generally, differences in concentration or temperature 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).
Conclusion
No claim is allowed.
Any inquiry concerning this communication or earlier communications from the examiner should be directed to AUDREA B CONIGLIO whose telephone number is (571)270-1336. The examiner can normally be reached Monday - Thursday 7:00 a.m. - 5:30 p.m..
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/AUDREA B CONIGLIO/ Primary Examiner, Art Unit 1617
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