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 1-29 are pending in this application.
Improper amendment of claims 10, 15, 19, and 29
The 7/29/2026 amendments to claims 10, 15, 19, and 29 are improper because they do not show all the changes with markings. For example, in the original claim 10, there was an “and” after 11.9°,” but the 7/29/2026 amendment deleted said “and” without showing a strikethrough, as shown below:
Original claim 10
PNG
media_image1.png
94
610
media_image1.png
Greyscale
Claim 10 as amended on 7/29/2026
PNG
media_image2.png
188
577
media_image2.png
Greyscale
The same issue is found in claims 15, 19, and 29. For the purpose of this Office action, the amended claims as shown above and their scope will be examined.
Terminal Disclaimer
The terminal disclaimer filed on 7/29/2026 disclaiming the terminal portion of any patent granted on this application which would extend beyond the expiration date of U.S. Patent Nos. 12528787, 12447149, 12551483 and 12643883, and any patent granted on Application Numbers 18971846 and 19544595 has been reviewed and is accepted. The terminal disclaimer has been recorded.
Withdrawn grounds of rejection
Nonstatutory double patenting grounds of rejection over U.S. Patent Nos. 12528787, 12447149, 12551483, 12643883, and Application Numbers 18971846 and 19544595 are withdrawn in view of the terminal disclaimer filed on 7/29/2026.
New grounds necessitated by amendment of 7/29/2026
35 U.S.C. 112(a) or 35 U.S.C. 112 (pre-AIA ), first paragraph (written description)
The following is a quotation of the first paragraph of 35 U.S.C. 112(a):
(a) IN GENERAL.—The specification shall contain a written description of the invention, and of the manner and process of making and using it, in such full, clear, concise, and exact terms as to enable any person skilled in the art to which it pertains, or with which it is most nearly connected, to make and use the same, and shall set forth the best mode contemplated by the inventor or joint inventor of carrying out the invention.
The following is a quotation of the first paragraph of pre-AIA 35 U.S.C. 112:
The specification shall contain a written description of the invention, and of the manner and process of making and using it, in such full, clear, concise, and exact terms as to enable any person skilled in the art to which it pertains, or with which it is most nearly connected, to make and use the same, and shall set forth the best mode contemplated by the inventor of carrying out his invention.
Claims 1-26 are rejected under 35 U.S.C. 112(a) or 35 U.S.C. 112 (pre-AIA ), first paragraph, as failing to comply with the written description requirement. The claim(s) contains subject matter which was not described in the specification in such a way as to reasonably convey to one skilled in the relevant art that the inventor or a joint inventor, or for applications subject to pre-AIA 35 U.S.C. 112, the inventor(s), at the time the application was filed, had possession of the claimed invention.
(1) Independent claims 1, 11, 16, and 20 have been amended to recite “lactose or a hydrate thereof.” Although lactose monohydrate and lactose dihydrate were originally disclosed (e.g., specification paragraph 72), there is no disclosure of the broader genus “hydrate thereof.” Said genus was not reasonably conveyed because only two hydrates were actually disclosed with no further disclosure that other hydrates can be included.
(2) The amendatory particle size distribution parameters are recited as “or.” In other words, the claimed dosage form has crystalline dihydrate form of vimseltinib (Formula I), wherein d10 is about 6-8 microns, d50 is about 16-20 microns, or d90 is about 32-40 microns. Thus, the claims currently encompass these parameters, which can be independent of the others. For example, the claims encompass 6 µm (d10), 100 µm (d50), and 200 µm (d90) values. As another example, the claims encompass one single value, e.g., d50, which indicates almost nothing about the width or shape of particle size distribution.
The original specification disclosed d10, d50, and d90 values in combination such that the dihydrate particles of the invention had d10, d50, and d90 values at the same time, i.e., the d10, d50, and d90 values were descriptive of the same underlying particle size distribution curve in the originally filed disclosure. See Example 3, paragraph 1172 and Table 2. Current claim scope, as amended on 7/29/2026, was not reasonably conveyed because the original disclosure only disclosed d10, d50, and d90 values in combination.
(3) “d90 particle size distribution of about 32 microns to about 40 microns” was not originally disclosed (emphasis added). Paragraph 1172 disclosed “about 33-40 µm (d90) (Table 2).” This reference to Table 2 is instructive, because the lowest d90 there is 32.9 as shown below:
PNG
media_image3.png
430
968
media_image3.png
Greyscale
Given the operation of “about,” the amended claims are changing the particle size distribution. This was not reasonably conveyed by the original disclosure.
(4) As discussed previously in this Office action, the XRPD patten comprising peaks, in terms of 2θ, has been amended so that the peaks are recited in terms of “or.” The consequence of the amendment is that the claims now encompass a crystalline dihydrate form of vimseltinib that has an XRPD pattern that needs to satisfy only one peak, in terms of 2θ, from the list recited in claims 10, 15, 19, and/or 29.
For example, the claims now encompass a dihydrate having an XRPD peak at 27.1°, but not at 5.9°, not at 10.9°, not at 11.9°, not at 16.8°, and not at 13.7°. Such widening of the claim scope was not reasonably conveyed.
For these reasons, the amended claims fail to find adequate descriptive support from the originally filed disclosure.
35 U.S.C. 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.
Claims 1-29 are rejected under 35 U.S.C. 103 as being unpatentable over Ahn et al. (WO 2014/145025; hereinafter, Ahn)1 in view of CN 1162839192, Liu (US 2013/0310357), Yang et al. (US 10,519,152; hereinafter, Yang), Ibrahim et al. (US 2009/0286783), Shi et al., and Gelderblom et al., further in view of Zhang et al. (US 2020/0054560) and Rohrs et al.
Ahn (WO 2014/145025) teaches 2-aminopyrimidine and analogs as kinase inhibitors having anti-cancer and antiproliferative activities through inhibition of, inter alia, CSF-1R (c-FMS). See abstract; paragraphs 3, 8-9, 123, 226-230. Ahn’s compounds include pharmaceutically acceptable salts, enantiomers, stereoisomers, and tautomers thereof (paragraph 11; claim 1). Ahn’s compound as disclosed in paragraph 207 has the same chemical structure as the compound of formula (I) of the instant application claims, i.e., vimseltinib. Ahn discloses synthesis of vimseltinib, wherein reaction mixture is quenched with water, neutralized with sodium bicarbonate, extracted with ethyl acetate, dried over sodium sulfate, treated with acetonitrile, and filtered (page 51).
CN 116283919 discloses crystal form B of vimseltinib, which is an anhydrous form (paragraph 10). The following X-ray powder diffraction pattern using Cu-Kα radiation is disclosed:
PNG
media_image4.png
506
860
media_image4.png
Greyscale
Diffraction angles, inter alia, 2θ of 10.4 ± 0.2°, 12.1 ± 0.2°, 13.0 ± 0.2°, 17.1 ± 0.2°, and 26.6 ± 0.2° are disclosed (paragraph 14). The diffractogram above also shows a peak at 2θ of about 5.9°.
Liu (US 2013/0310357) is cited to establish that hydrates such as dihydrate are known, alternative forms of compounds used as modulators of CSF-1R kinase (paragraphs 11-12, 50, 54, 81).
Yang (10,519,152) is cited to further establish that crystalline hydrates such as dihydrate are known, alternative forms of compounds used as anti-proliferative agents (column 69, lines 13-25; column 84, line 41 to column 85, line 19).
Ibrahim et al. (US 2009/0286783) disclose the known use of lactose such as lactose monohydrate as a carrier, a cross-linked polyvinylpyrrolidone as a disintegrant, magnesium as a lubricant in pharmaceutical oral dose formulations (paragraphs 333-335).
Shi et al. disclose the use of the soluble lactose in tablets for improved wettability and flowability (page 1; page 3, right column; page 5, left column). Lactose is a well-known excipient and filler: approximately 60-70% of pharmaceutical preparations contain lactose (page 2, left column); and lactose monohydrate is the most common form of lactose (page 2, right column). Lactose also provides additional properties in tablets: 65% lactose formulation can show the “best sustained release of the drug,” whereas 80% lactose formulation can delay drug release (page 5, left column).
Gelderblom et al. disclose long-term tolerability of 30 mg or 20 mg once daily as a loading dose and 6, 10, or 30 mg as the maintenance dose of vimseltinib (abstract 475P on page S757-S758).
Rohrs et al. disclose the well-known fact that content uniformity of pharmaceutical dosage units can be affected by particle size and size distribution (abstract). Particle size, distribution width, and dose influence content uniformity, wherein for example, increase in width requires decrease in d50 if dose is held constant, and an increase in d50 requires a decrease in width if the dose is held constant (page 1050, first paragraph of right column; page 1054, Figure 3).
Zhang et al. (US 2020/0054560) disclose a solid formulation of the kinase inhibitor palbociclib, wherein d10 is 1-5 µm, d50 is 5-10 µm, and d90 is less than 20µm (paragraph 17; claims 14, 20-21, 30-31). Reduced size is generally known to improve dissolution (paragraph 6).
The cited prior art references do not explicitly disclose all the claim-recited features in combination, but the ordinary skilled artisan would have found the claimed invention as a whole obvious for the reasons set forth below.
d10 of about 6-8 µm, d50 of about 16-20 µm, or d90 of about 32-40 µm
Individually and independently, a single particle size feature describes little about the particle size distribution of a drug in a dosage form. For example, two batches can share an identical d50 while one can have a narrow, tight distribution and the other can have a broad one with a long tail of either very fine or very coarse particles. It would have been well within the skill of the ordinary skilled artisan to select appropriate particle size distribution and dose to obtain content uniformity of a solid oral dosage form (Rohrs et al.). The ordinary skilled artisan would have recognized the presently claimed particle size “distribution” features (readable on a single value of d10, d50, or d90) as an obvious and very broad particle size feature, particularly in view of teachings of Rohr et al. and Zhang et al. (use of such features with another kinase inhibitor).
Crystalline dihydrate form, including XRPD pattern comprising peaks,
in terms of 2θ, at about 5.9°, 10.9°, 11.9°, 13.7°, 16.8°, and 27.1°
Ahn does not explicitly disclose a dihydrate of vimseltinib. However, hydrates,
including dihydrate, are well known form of the base compound, as evidenced by Liu and Yang. Additionally, the method disclosed by Ahn in providing vimseltinib (Example 9 on page 51) is suggestive of a hydrate or dihydrate because the quenching step introduced water and the remaining steps may not necessarily obtain the anhydrous product only. Also a dihydrate can from the compound absorbing moisture from the air or the compound retaining trace amount of water for stability.
As for the claim-recited XRPD pattern comprising peaks, in terms of 2θ, the Examiner’s position is that (1) the dihydrate would have been obvious, and (2) the XRPD diffractogram characteristics would have been necessarily possessed by the dihydrate. CN 116283919 shows XRPD diffraction pattern of the anhydrous compound that is quite similar, and the ordinary skilled artisan would have obtained the claimed XRPD features from the obvious dihydrate of vimseltinib suggested by the prior art.
about 20-97% or about 70-97% lactose or lactose monohydrate;
about 1-20% or about 1-10% disintegrant such as crosslinked PVP; and
about 0.1-10% or about 0.1-3% lubricant such as magnesium stearate
Lactose, e.g., lactose monohydrate, is a well-known pharmaceutical excipient or filler, used in 60-70% of pharmaceutical preparations for water solubility, flowability, and wettability (Shi et al.). 65% and 80% lactose formulations are known, with 65% being the best for sustained release and 80% for delayed release (Shi et al.). Ibrahim et al. (US 2009/0286783) disclose lactose monohydrate as a carrier, a cross-linked polyvinylpyrrolidone as a disintegrant, magnesium as a lubricant in pharmaceutical oral dose formulations (paragraphs 333-335). Therefore, it would have been well within the skill of the ordinary skilled artisan to arrive at the claimed lactose, disintegrant, and lubricant at the required percentage ranges upon routine optimization to provide a suitable tablet for oral dosage.
The crystalline dihydrate of vimseltinib is present in the oral dosage form in an amount selected from about 2.2 mg, 10.8 mg, 15.2 mg, 21.7 mg, and 32.5 mg
Gelderblom teaches doses of 6 mg, 10mg, 20 mg, and 30 mg. It would have
been obvious to the ordinary skilled artisan to formulate oral dosage forms of multiple strengths, containing different amounts of the active drug, depending on release characteristics (immediate release vs. extended release) and/or treatment objective, which would allow the healthcare provider to adjust the dosage to a patient’s specific needs.
Therefore, the claimed invention, as a whole, would have been prima facie obvious to one of ordinary skill in the art before the effective filing date of the claimed invention, because every element of the invention and the claimed invention as a whole have been fairly disclosed or suggested by the teachings of the cited references.
Applicant’s arguments filed on 7/29/2026 have been given due consideration but they were deemed unpersuasive for the following reasons.
Applicant argues that Jian’s (CN 116283919) d10, d50, and d90 values disclosed for Form A in Figure 4 is “significantly different from the instantly claimed PSD values.” The Examiner cannot agree. In this art, d10, d50, and d90 of particle size distribution values do not mean what Applicant implies, i.e., particles fall within the stated (or recited) range. For example, Applicant appears to be arguing the d10 particle size distribution of about 6 microns to about 8 microns means that 10% of particles fall within this size range. This is erroneous. d10 particle size distribution of about 6 microns to about 8 microns, as claimed, actually means that 10% of particles are equal to or smaller than this range. Thus, as Applicant noted, Jian’s Figure 4 discloses d10 of 0.0368, which is below 6-8 microns.
Applicant also appears to be arguing that the claimed solid forms have “controlled PSD parameters,” but as explained previously, the particle size distribution features are recited with an “or,” so there is no meaningful control as to size distribution since any single value such as d10, d50, or d90 fails to define by itself the width or shape of size distribution.
Further, Applicant appears to be arguing that the size distribution features are native particle size distributions. However, there is nothing in the claims that would preclude mechanical size adjustments to obtain improved solubility and/or content uniformity.
For these reasons, all claims must be rejected again.
Double patenting
The nonstatutory double patenting rejection is based on a judicially created doctrine grounded in public policy (a policy reflected in the statute) so as to prevent the unjustified or improper timewise extension of the “right to exclude” granted by a patent and to prevent possible harassment by multiple assignees. A nonstatutory double patenting rejection is appropriate where the conflicting claims are not identical, but at least one examined application claim is not patentably distinct from the reference claim(s) because the examined application claim is either anticipated by, or would have been obvious over, the reference claim(s). See, e.g., In re Berg, 140 F.3d 1428, 46 USPQ2d 1226 (Fed. Cir. 1998); In re Goodman, 11 F.3d 1046, 29 USPQ2d 2010 (Fed. Cir. 1993); In re Longi, 759 F.2d 887, 225 USPQ 645 (Fed. Cir. 1985); In re Van Ornum, 686 F.2d 937, 214 USPQ 761 (CCPA 1982); In re Vogel, 422 F.2d 438, 164 USPQ 619 (CCPA 1970); In re Thorington, 418 F.2d 528, 163 USPQ 644 (CCPA 1969).
A timely filed terminal disclaimer in compliance with 37 CFR 1.321(c) or 1.321(d) may be used to overcome an actual or provisional rejection based on nonstatutory double patenting provided the reference application or patent either is shown to be commonly owned with the examined application, or claims an invention made as a result of activities undertaken within the scope of a joint research agreement. See MPEP § 717.02 for applications subject to examination under the first inventor to file provisions of the AIA as explained in MPEP § 2159. See MPEP § 2146 et seq. for applications not subject to examination under the first inventor to file provisions of the AIA . A terminal disclaimer must be signed in compliance with 37 CFR 1.321(b).
The filing of a terminal disclaimer by itself is not a complete reply to a nonstatutory double patenting (NSDP) rejection. A complete reply requires that the terminal disclaimer be accompanied by a reply requesting reconsideration of the prior Office action. Even where the NSDP rejection is provisional the reply must be complete. See MPEP § 804, subsection I.B.1. For a reply to a non-final Office action, see 37 CFR 1.111(a). For a reply to final Office action, see 37 CFR 1.113(c). A request for reconsideration while not provided for in 37 CFR 1.113(c) may be filed after final for consideration. See MPEP §§ 706.07(e) and 714.13.
The USPTO Internet website contains terminal disclaimer forms which may be used. Please visit www.uspto.gov/patent/patents-forms. The actual filing date of the application in which the form is filed determines what form (e.g., PTO/SB/25, PTO/SB/26, PTO/AIA /25, or PTO/AIA /26) should be used. A web-based eTerminal Disclaimer may be filled out completely online using web-screens. An eTerminal Disclaimer that meets all requirements is auto-processed and approved immediately upon submission. For more information about eTerminal Disclaimers, refer to www.uspto.gov/patents/apply/applying-online/eterminal-disclaimer.
Claims 1-29 are rejected on the ground of nonstatutory double patenting as being unpatentable over claims 1-8 of U.S. Patent No. 12,617,775 in view of Ibrahim et al. (US 2009/0286783), Shi et al., and Gelderblom et al., further in view of Rohr et al. and Zhang et al. (US 2020/0054560).3
Patented claims are directed to a dihydrate form of the compound that is vimseltinib (claims 1-8). Pharmaceutical composition comprising the dihydrate and pharmaceutically acceptable excipients is claimed (claim 2).
Ibrahim et al. (US 2009/0286783) disclose the known use of lactose such as lactose monohydrate as a carrier, a cross-linked polyvinylpyrrolidone as a disintegrant, magnesium as a lubricant in pharmaceutical oral dose formulations (paragraphs 333-335).
Shi et al. disclose the use of the soluble lactose in tablets for improved wettability and flowability (page 1; page 3, right column; page 5, left column). Lactose is a well-known excipient and filler: approximately 60-70% of pharmaceutical preparations contain lactose (page 2, left column); and lactose monohydrate is the most common form of lactose (page 2, right column). Lactose also provides additional properties in tablets: 65% lactose formulation can show the “best sustained release of the drug,” whereas 80% lactose formulation can delay drug release (page 5, left column).
Gelderblom et al. disclose long-term tolerability of 30 mg or 20 mg once daily as a loading dose and 6, 10, or 30 mg as the maintenance dose of vimseltinib (abstract 475P on page S757-S758).
Rohrs et al. disclose the well-known fact that content uniformity of pharmaceutical dosage units can be affected by particle size and size distribution (abstract). Particle size, distribution width, and dose influence content uniformity, wherein for example, increase in width requires decrease in d50 if dose is held constant, and an increase in d50 requires a decrease in width if the dose is held constant (page 1050, first paragraph of right column; page 1054, Figure 3).
Zhang et al. (US 2020/0054560) disclose a solid formulation of the kinase inhibitor palbociclib, wherein d10 is 1-5 µm, d50 is 5-10 µm, and d90 is less than 20µm (paragraph 17; claims 14, 20-21, 30-31). Reduced size is generally known to improve dissolution (paragraph 6).
The patented claims do not recite d10, d50, and d90 values. However, it would have been well within the skill of the ordinary skilled artisan to select appropriate particle size distribution and dose to obtain content uniformity of a solid oral dosage form (Rohrs et al.). The ordinary skilled artisan would have recognized the presently claimed particle size “distribution” features (readable on a single value of d10, d50, or d90) as an obvious and very broad particle size feature, particularly in view of teachings of Rohr et al. and Zhang et al., who disclose the use of such features with another kinase inhibitor.
Regarding the claim-recited XRPD pattern comprising peaks in terms of 2θ, it is the Examiner’s position that the same XRPD peaks would have been necessarily obtained because the patented claims are directed to the same dihydrate of vimseltinib.
The patented claims do not explicitly disclose all the excipients, their percentages, and dosage strengths. However, lactose, e.g., lactose monohydrate, is a well-known pharmaceutical excipient or filler, used in 60-70% of pharmaceutical preparations for water solubility, flowability, and wettability (Shi et al.). 65% and 80% lactose formulations are known, with 65% being the best for sustained release and 80% for delayed release (Shi et al.). Ibrahim et al. (US 2009/0286783) disclose lactose monohydrate as a carrier, a cross-linked polyvinylpyrrolidone as a disintegrant, magnesium as a lubricant in pharmaceutical oral dose formulations (paragraphs 333-335). Therefore, it would have been well within the skill of the ordinary skilled artisan to arrive at the claimed lactose, disintegrant, and lubricant at the required percentage ranges upon routine optimization to provide a suitable oral dosage form.
Additionally, Gelderblom teaches doses of 6 mg, 10mg, 20 mg, and 30 mg. It
would have been obvious to the ordinary skilled artisan to formulate oral dosage forms of multiple strengths, containing different amounts of the active drug, depending on release characteristics (immediate release vs. extended release) and/or treatment objective, which would allow the healthcare provider to adjust the dosage to a patient’s specific needs.
Therefore, the ordinary skilled artisan would have recognized the instant claimed invention as an obvious variation of the invention set forth in the patented claims.
Applicant argues in the response filed on 7/29/2026 that the patented claims are “not limited by the specific PSDs claimed for the crystalline dihydrate form. Due to at least these distinct differences … Applicant submits that the claimed invention is patentably distinct.” However, as discussed previously, the claims are readable on a single value such as d10, d50, or d90, which is quite broad and does not actually require much in terms of particle size distribution. Nonetheless, the claimed d10, d50, or d90 values are known in this art (Zhang et al.), and moreover, the ordinary skilled artisan would have been motivated to optimize such values as claimed to obtain improved solubility and content uniformity.
For these reasons, all claims must be rejected again. No claim is allowed.
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.
Any inquiry concerning this communication or earlier communications from the Examiner should be directed to JOHN PAK whose telephone number is (571)272-0620. The Examiner can normally be reached on Monday to Friday from 8:30 AM to 5 PM.
If attempts to reach the Examiner by telephone are unsuccessful, the Examiner's SPE, Fereydoun Sajjadi, can be reached on (571)272-3311. The fax phone number for the organization where this application or proceeding is assigned is (571)273-8300.
Information regarding the status of an application may be obtained from Patent Center. Status information for published applications may be obtained from Patent Center. Status information for unpublished applications is available through Patent Center for authorized users only. Should you have questions about access to Patent Center, contact the Electronic Business Center (EBC) at 866-217-9197 (toll-free).
Examiner interviews are available via telephone, in-person, and video conferencing using a USPTO supplied web-based collaboration tool. To schedule an interview, applicant is encouraged to use the USPTO Automated Interview Request (AIR) Form at https://www.uspto.gov/patents/uspto-automated- interview-request-air-form.
/JOHN PAK/Primary Examiner, Art Unit 1699
1 Cited in the parent application by Applicant.
2 Cited in the parent application by Applicant. Machine translation is provided in this Office action.
3 U.S. Patent No. 12,617,775 issued on 5/5/2026 from Application serial no. 19/299,605, which was previously applied in the Office action of 4/29/2026.
Prosecution Insights