DETAILED ACTION
Status of the Application
Receipt is acknowledged of Applicants’ Remarks, filed 21 April 2026, in the matter of Application N° 17/755,832. Said documents have been entered on the record. The Examiner further acknowledges the following:
The present application, filed on or after March 16, 2013, is being examined under the first inventor to file provisions of the AIA .
No additions, amendments, or cancellations have been made to the claims filed 9 October 2025. No new matter has been added.
Thus, claims 1, 5-9, and 11-16 continue to represent all claims currently under consideration.
Information Disclosure Statement
No Information Disclosure Statements (IDS) have been filed for consideration.
Withdrawn Rejections
Rejections under 35 USC 103
Both of the previously maintained rejections based on the teachings of Inoue have been reconsidered in view of Applicants’ filed remarks. The Examiner also notes that Applicants’ remarks are directed primarily at the teachings of Inoue and do not appear to address the references with respect to the lubricant component.
Therein, the remarks are unpersuasive with the exception of the discussion pertaining to the comparison of the results provided in Table 5b (see Spec., pg. 34, ¶[0074]). Here, a comparison of Examples 5-3, 4-2, and 4-4 is provided along with qualitative depiction of the resulting tablet and properties. The compared Examples also depict the structural location of the two claimed lubricants (i.e., internal vs. external addition) as well as a non-numeric assessment of the “tablet property.” The tablet property is defined in the preceding paragraph as being the “balance between the hardness and the disintegration property”. The hardness parameter (not claimed) by which Applicants’ invention is defined ranges from 15-70N and the disintegrating time (not claimed) is 70 seconds or less (see e.g., Spec., pg. 3, lines 30-33). These parameters are understood as defining Applicants’ “tablet property.”
Considering Inoue’s disclosure, as discussed in the newly presented rejection below, the Examiner agrees that Inoue discloses the use of multiple lubricants and that a coating composition may be used on the tablet. However, the reference focuses on, but does not preclude the possibility of two lubricants that are structurally place in the tablet. Further, Inoue’s disclosed tablets do meet the hardness requirement, but do just fail to meet the disintegration time, based on the use of magnesium stearate in the tablet (i.e., internal).
Thus, on reconsideration, the Examiner withdraws both rejections as previously presented in favor of the newly made rejections herein below.
New Rejections
Applicants’ amendments have necessitated the following ground(s) of rejection:
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, 6-9, 11-12 and 14-15 are rejected under 35 U.S.C. 103 as being unpatentable over Inoue (US Pre-Grant Publication Nº 2016/0158227 A1; of record) in view of Fukushima et al. (US Pre-Grant Publication Nº 2011/0105615 A1; of record).
Inoue discloses a tablet comprising an uncoated tablet containing 7-[4-(4-benzo[b]thiophen-4-yl-piperazin-1-yl)butoxy]-1H-quinolin-2-one (aka brexpiprazole) or a salt thereof, excipients, disintegrants such as low-substituted hydroxypropylcellulose, binders, and lubricants; and further comprising a coating layer containing talc (see e.g., Abstract). Suitable excipients include D-mannitol and microcrystalline cellulose. See ¶[0055]. The excipients may be used singly or in a combination of two or more. See ¶[0056]. The excipient (a) content is not particularly limited, and is included at about 30 to 90% by weight. See ¶[0057]. Examples of binders include partially pregelatinized starch. See ¶[0060]. Examples of lubricants include magnesium stearate, talc, and sodium stearyl fumarate, which may be used singly or in a combination of two or more. See ¶[0069]. The tablet of the present invention may be used as an orally disintegrating tablet. See ¶[0049]. The amount of microcrystalline cellulose may be 5 to 20% by weight. See ¶[0113]. Compound (I) (i.e. 7-[4-(4-Benzo[b]thiophen-4-yl-piperazin-1-yl)butoxy]-1H-quinolin-2-one) treats central nervous system diseases (in particular, schizophrenia). See ¶[0003]. The tablet can be produced by a step of forming into a tablet a mixture containing Compound (I) or a salt thereof, an excipient, a binder, a disintegrant, and a lubricant. See ¶[0188]. Examples of the tablet forming methods include tableting, such as direct compression tableting and external lubrication tableting. See ¶[0190]. The coated tablet can be produced by mixing a coating agent, a colorant, and a liquid medium; spraying the obtained liquid mixture on the surface of the uncoated tablet; and successively drying it. See ¶[0191]. The tablet may have a hardness of 4.7 Kp (equivalent to 46.09 N) and a disintegration time of 69 seconds (Table 2). The measurement of disintegration was performed using water as a test liquid according to the disintegration test of the Japanese Pharmacopeia. See ¶[0201]. The hydroxypropoxyl groups content of the hydroxypropylcellulose may be 10.0 to 12.9%. See ¶[0197].
The prior art differs from the instant claims on two key points with respect to claim 1.
First, while Inoue does teach that the binder is embodied partially pregelatinized starch, it does not expressly disclose that it is a partially pregelatinized starch having a degree of pregelatinization of 70% or less and a water-soluble component content of 10% or less.
Second, despite Inoue’s teaching and suggestion that more than one lubricant may be used in the practiced coated tablet, and that the tablets may be produced by way of external lubricant tableting, the Examiner acknowledges that there is no express structural teaching pertaining to the location of both the lubricants of interest. It is further acknowledged that magnesium stearate is preferably disclosed as being incorporated into the core tablet (i.e., internal lubricant).
The disclosure of Fukushima remedies both of the aforementioned deficiencies.
Regarding the former, Fukushima discloses a tablet which is rapidly disintegrated in an oral cavity containing an active ingredient, mannitol and corn-derived pregelatinized starch mixed with at least one disintegrant such as carmellose and/or crospovidone (see e.g., Abstract). The “corn-derived pregelatinized starch” is a starch wherein a part or all of cornstarch is pregelatinized and the degree of pregelatinization of the partly pregelatinized starch is less than 30%. See ¶[0114]. Specific examples of the partly pregelatinized starch include commercially available PCS-PC-10. See ¶[0016]. The partly pregelatinized starch used in the rapidly disintegrating tablet was trade name: PCS-PC-10, Asahi Kasei Corporation. See ¶[0088]. The tablet is rapidly disintegrated in an oral cavity containing an active ingredient at a high concentration, and having both good disintegrability in the oral cavity and tablet strength. See ¶[0089].
Regarding the latter deficiency, Fukushima, like Inoue, discloses that the lubricant is not particularly limited in both the kind and amount and that examples of suitable lubricants include both magnesium stearate and sodium stearyl fumarate. See ¶[0048]. More critically, however, Fukushima further exemplifies the specific use of both lubricants, not only in the same formulated dosage form, but also in the same locations, or “roles,” as instantly claimed.
Example 1, for instance, discloses the preparation of active ingredient granules (i.e., Table 1), which are then mixed with placebo granules, cornstarch, and sodium stearyl fumarate, and then compressed to form tablets. Following tablet preparation, the tablets are coated with a suspension of magnesium stearate and ethanol.
The tablets prepared in Comparative Example 1 with respect to the lubricant combination and location, are the same as in Example 1. See ¶[0056]-¶[0059].
Both tablets were analyzed and determined to possess fine disintegrability and high hardness, according to the DHB or Disintegrating time-Hardness-Balance Index). See ¶[0049]. Table 2 presents the following results:
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120
512
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Greyscale
Generally, it is prima facie obvious to select a known material for incorporation into a composition, based on its recognized suitability for its intended use. See MPEP §2144.07. Inoue discloses wherein the tablet comprises partially pregelatinized starch and wherein the lubricant may be one or more such species as magnesium stearate and sodium stearyl fumarate. MPEP §2144.06(I) additionally states that “[i]t is prima facie obvious to combine two compositions each of which is taught by the prior art to be useful for the same purpose, in order to form a third composition to be used for the very same purpose.... [T]he idea of combining them flows logically from their having been individually taught in the prior art.” MPEP §2143.01 states that “[o]bviousness can be established by combining or modifying the teachings of the prior art to produce the claimed invention where there is some teaching, suggestion, or motivation to do so.”
In the instant case, the teachings of both the references disclose producing coated tablet compositions that have been assessed for both hardness and rapid disintegrability. While Inoue more preferably discloses the use of magnesium stearate in the uncoated tablet, Fukushima discloses using sodium stearyl fumarate in the tablet and magnesium stearate in the coating of the same tablet.
The ordinarily skilled artisan would be motivated to modify the teachings of Inoue with the teachings of Fukushima on the basis that doing so would not only improve the hardness of the resulting tablet, but also reduce the time it takes to orally disintegrate in the given patient’s oral cavity.
Regarding claim 6 reciting wherein the partially pregelatinized starch (C) is a partially pregelatinized starch having a water-soluble component content of 10% or less, the instant specification discloses that PCS PC-10; Asahi Kasei Corporation was the partially pregelatinized starch used in Example 3-1 and has a water-soluble component content of 3% or less. See ¶[0060]-¶0061]. As discussed above, the partly pregelatinized starch used in the rapidly disintegrating tablet of Fukushima was trade name: PCS-PC-10, Asahi Kasei Corporation. Accordingly, the partially pregelatinized starch of Fukushima has a water-soluble component content of 10% or less.
Claims 5 and 16 are rejected under 35 U.S.C. 103 as being unpatentable over Inoue (US Pre-Grant Publication Nº 2016/0158227 A1; of record) in view of Fukushima et al. (US Pre-Grant Publication Nº 2011/0105615 A1; of record), and further in view of Yoshinari et al. (US Pre-Grant Publication Nº 2001/0001106 A1; of record).
The teachings of Inoue and Fukushima are discussed above. Inoue and Fukushima do not teach wherein the D-mannitol has a 50% particle diameter ranging from 10 µm to 100 µm, and the D-mannitol is present in non-needle-like crystalline form in the tablet.
However, Yoshinari teaches a D-mannitol that shows improved compressibility and is useful as an excipient (abstract). When used as an excipient, D-mannitol is preferably in the state of granules of crystalline aggregate, especially whose average size is about 0.05 to about 5.0 mm in diameter (equal to 50 µm to 5000 µm). The forms of the crystalline aggregate are not specifically limited and any form of crystalline aggregate may be used such as net-like or thin plate-like ones. See ¶[0023]. The D-mannitol exhibits excellent compressibility, which can be used as an excipient for direct compression. The mannitol can be used as a good excipient in the fields of pharmaceutical and food products. See ¶[0030].
Generally, it is prima facie obvious to select a known material for incorporation into a composition, based on its recognized suitability for its intended use. See MPEP §2144.07. Inoue discloses wherein the tablet comprises D-mannitol. Accordingly, it would have been obvious to one of ordinary skill in the art to have incorporated the D-mannitol of Yoshinari into the composition of Inoue since it is a known and effective D-mannitol that provides additional benefits such as exhibiting excellent compressibility as taught by Yoshinari.
All claims under consideration remain rejected; no claims are allowed.
Conclusion
Due to the new grounds of rejection, this action is deemed non-final.
Correspondence
Any inquiry concerning this communication or earlier communications from the Examiner should be directed to Jeffrey T. Palenik whose telephone number is (571) 270-1966. The Examiner can normally be reached on 9:30 am - 7:00 pm; M-F (EST).
If attempts to reach the Examiner by telephone are unsuccessful, the Examiner’s supervisor, Robert A. Wax can be reached on (571) 272-0623. The fax phone number for the organization where this application or proceeding is assigned is 571-273-8300.
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/Jeffrey T. Palenik/
Primary Examiner, Art Unit 1615
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