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 .
DETAILED ACTION
Status of the Claims
Claims 167-189 are pending and are examined on their merits.
Priority
Applicant’s claim for the benefit of a prior-filed application under 35 U.S.C. 120 is acknowledged. Applicant has complied with all conditions for receiving the benefit of an earlier filing date under 35 U.S.C. 120 based on the date of the provisional applications 63/607,617 and 63/650,144 filed on December 8th 2023 and May 21st 2024.
Information Disclosure Statement
The Information Disclosure Statements filed on April 21st 2025 and March 27th 2025 are in compliance with the provisions of 37 CFR 1.97 and have been considered in full. A signed copy of references cited from the IDS is included with this Office Action.
Claim Rejections - 35 USC § 112(b)
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 169, 171, 172, and 181, as well as their dependent claims 174 and 177-180 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.
Claims 169, 171, and 172, as well as their dependent claims 174 and 177-180 are indefinite for reciting “an XRPD pattern substantially as shown in FIG. 5,” “a differential scanning calorimetry (DSC) thermogram substantially as shown in FIG. 6,” and “a thermogravimetric analysis (TGA) thermogram substantially as shown in FIG. 7.”
See MPEP 2173.05(s):
Where possible, claims are to be complete in themselves. Incorporation by reference to a specific figure or table "is permitted only in exceptional circumstances where there is no practical way to define the invention in words and where it is more concise to incorporate by reference than duplicating a drawing or table into the claim. Incorporation by reference is a necessity doctrine, not for applicant’s convenience." Ex parte Fressola, 27 USPQ2d 1608, 1609 (Bd. Pat. App. & Inter. 1993) (citations omitted).
Appropriate correction is required.
Claim 181 is indefinite for reciting “the pharmaceutical composition of claim 171…” No pharmaceutical composition is recited in claim 171. For the purpose of examination, claim 181 will be read as “the pharmaceutical composition of claim 177…”
Claim Rejections - 35 USC § 102
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 the appropriate paragraphs of 35 U.S.C. 102 that form the basis for the rejections under this section made in this Office action:
A person shall be entitled to a patent unless –
(a)(1) the claimed invention was patented, described in a printed publication, or in public use, on sale, or otherwise available to the public before the effective filing date of the claimed invention.
Claims 167—172 and 176-179 are rejected under 35 U.S.C. 102(a)(1) as being anticipated by Shanghai Haoyuan (CN116283919A published on March 21st 2023; Google Patents Translation Attached).
Claim 167 is directed towards a crystalline anhydrous form of the anticancer compound, Vimseltinib, wherein the crystal form comprises XRPD peaks at 11.4, 14.7, 17.1, 20.1, 21.3, and 29.1 ± 0.2 degrees 2θ.
Shanghai Haoyuan teaches an anhydrous crystal form of Vimseltinib (Shanghai Haoyuan, Translation, pg. 3), with XRPD peaks at 11.3, 14.6, 17.1, 20.0, 21.3, and 29.5 ± 0.2 degrees 2θ (Shanghai Haoyuan, Translation, pg. 3). As Shanghai Haoyuan’s XRPD peaks are recognized as being identical (within the standard margin of error) to applicant’s XRPD peaks, Shanghai Haoyuan anticipates claim 167.
Claim 168 is directed towards the crystal form of claim 167 comprising peaks at 10.2, 10.5, 11.4, 14.7, 17.1, 20.1, 21.3, and 29.1 ± 0.2 degrees 2θ. Shanghai Haoyuan further teaches peaks at 10.1, 10.4, 11.3, 14.6, 17.1, 20.0, 21.3, and 29.5 ± 0.2 degrees 2θ (Shanghai Haoyuan, Translation, pg. 3). As Shanghai Haoyuan’s XRPD peaks are recognized as being identical to applicant’s XRPD peaks, Shanghai Haoyuan anticipates claim 168.
Claim 169 is directed towards the crystal form of claim 168, wherein the XRPD pattern is substantially as shown in Figure 5. That is, having peaks matching those found in Table 7 of the specification. The XRPD peaks of Figure 5 and Shanghai Haoyuan are compared below:
Applicant’s XRPD Peaks (Claims 167-168 and Specification, Table 7)
Shanghai Haoyun’s XRPD Peaks (Shanghai Haoyun, Translation, pg. 3)
10.1
10.1
10.5
10.4
11.4
11.3
12.2
12.1
13.1
13.0
14.7
14.6
15.0
14.9
15.5
15.5
15.8
15.8
17.1
17.1
17.6
17.6
19.1
19.1
19.8
19.7
20.1
20.0
20.8
20.7
21.3
21.3
21.8
21.8
22.3
22.2
22.7
22.6
22.8
22.8
23.3
23.3
24.5
24.4
25.2
25.2
25.7
25.7
26.0
26.0
26.3
26.2
26.7
26.6
29.1
29.5
29.5
29.5
Shanghai Haoyun’s crystal form would thereby be recognized as having an XRPD pattern substantially as shown in FIG. 5, and Shanghai Haoyun thereby anticipates claim 169.
Claim 170 requires that the form of claim 168 has a DSC thermogram with an endothermic peak at 216 ± 3 degrees Celsius and an endothermic event onset at about 210-220 degrees Celsius. Shanghai Haoyun’s crystal form has an endothermic peak at 213 degrees Celsius (Shanghai Haoyun, Translation, pg. 3) and an endothermic event onset at about 210 degrees Celsius (Shanghai Haoyun, Figure 6). Shanghai Haoyun thereby anticipates claim 170.
Claim 171 is directed to the crystal form of claim 168 having a DSC thermogram substantially as shown in Figure 6.
The DSC thermograms of Figure 6 (left) and Shanghai Haoyun (right) are shown below:
PNG
media_image1.png
460
735
media_image1.png
Greyscale
PNG
media_image2.png
496
668
media_image2.png
Greyscale
The two diagrams share both an endothermic event onset and an endothermic peak, within the standard margin of error. The two diagrams would therefore be recognized as substantially identical and Shanghai Haoyun anticipates claim 171.
Claim 172 is directed towards the crystal form of claim 168 having a TGA thermogram substantially as shown in Figure 7. The TGA thermogram of Figure 7 is indicative of an anhydrate crystal form in which there is little to no meaningful weight loss through the melting of the crystal form, and no substantial weight loss until its decomposition, beginning at about 330 degrees Celsius. Shanghai Haoyun’s Figure 7 shows a TGA thermogram, also indicative of an anhydrate crystal form, wherein throughout the melting, up to 300 degrees Celsius, less than 2% weight loss occurs. Shanghai Haoyun’s TGA diagram thereby shares the same diagnostic features as applicant’s TGA diagram, defined by the absence of weight loss below and through melting. As one of ordinary skill in the art would recognize the TGA diagrams as being substantially similar, Shanghai Haoyun anticipates claim 172.
Claim 176 is directed towards a pharmaceutical composition comprising the crystal form of claim 167 and a pharmaceutically acceptable excipient. Shanghai Haoyun teaches such a composition (Shanghai Haoyun, Translation, pg. 2, claim 10), anticipating claim 176.
Claim 177 is directed towards a pharmaceutical composition comprising the crystal form of claim 169 and a pharmaceutically acceptable excipient. Shanghai Haoyun teaches such a composition (Shanghai Haoyun, Translation, pg. 2, claim 10), anticipating claim 177.
Claim 178 requires that, in the pharmaceutical composition of claim 177, the crystal form present has a d10 particle size distribution of about 2-10 microns. Shanghai Haoyun teaches a d10 particle size distribution of 6.86 microns, anticipating claim 178.
Claim 179 requires that, in the pharmaceutical composition of claim 177, the crystal form present has a d50 particle size distribution of about 12-24 microns. Shanghai Haoyun teaches a d50 particle size distribution of 13.3 microns, anticipating claim 179.
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.
Claims 173-175 and 181 are rejected under 35 U.S.C. 103 as being unpatentable over Shanghai Haoyun.
Claim 173 is directed towards the crystal form of claim 167, wherein the crystal form does not have more than about 10% mol%, 3 mol%, or 1 mol% of other solid-state forms of Vimseltinib. For the teachings of Shanghai Haoyun as they are relevant to claim 167, see the above 102 rejection for claim 167.
Regarding the further limitations of claim 173, that the crystal form is of at least 90%, 97%, or 99% purity, in that it does not include other crystal forms, while Shanghai Haoyun does not explicitly state the mol% of the particular crystal form, Shanghai Haoyun does state that this crystal form has the benefit of decreased impurities, and that avoiding mixed crystals (wherein multiple crystal forms of the compound are present) was an explicit goal in the development of their anhydrous crystal form (Shanghai Haoyun, Translation, pg. 4). One of ordinary skill in the art would thereby have had a reasonable expectation of success in purifying the anhydrous crystal form of claim 167 to where not more than about 10% mol%, 3 mol%, or 1 mol% of other solid-state forms of Vimseltinib are present, and claim 173 is prima facie obvious.
Claim 174 is directed towards the crystal form of claim 169, wherein the crystal form does not have more than about 1 mol% of other solid-state forms of Vimseltinib. For the teachings of Shanghai Haoyun as they are relevant to claim 169, see the above 102 rejection for claim 169.
Regarding the further limitations of claim 174, that the crystal form is of at least 99% purity, in that it does not include other crystal forms, while Shanghai Haoyun does not explicitly state the mol% of the particular crystal form, Shanghai Haoyun does state that this crystal form has the benefit of decreased impurities, and that avoiding mixed crystals (wherein multiple crystal forms of the compound are present) was an explicit goal in the development of their anhydrous crystal form (Shanghai Haoyun, Translation, pg. 4). One of ordinary skill in the art would thereby have had a reasonable expectation of success in purifying the anhydrous crystal form of claim 169 to where not more than about 1 mol% of other solid-state forms of Vimseltinib are present, and claim 174 is prima facie obvious.
Claim 175 requires that the crystal form of claim 167 is stable after four weeks of storage at 40 degrees Celsius with 75% relative humidity. For the teachings of Shanghai Haoyun as they are relevant to claim 167, see the above 102 rejection for claim 167.
Shanghai Haoyun’s crystal form exhibits 99.68% stability under these conditions for 16 days (Shanghai Haoyun, pg. 5, Table 1), well within the realm defined by applicant as “stable” (Specification, paragraph [0506]). As Shanghai Haoyun’s crystal form has demonstrated extremely high stability within applicant’s described conditions over a 16-day period, one of ordinary skill in the art would reasonably expect that this stability trend would continue if another 12 days were added, thereby matching the ‘four weeks of storage’ required by the claim. As one of ordinary skill in the art would reasonably expect Shanghai Haoyun’s crystal form to remain stable after 4 weeks of storage, claim 175 is prima facie obvious.
Claim 181 is directed towards the pharmaceutical composition of claim 177 wherein the crystal form is present in an amount of at least 90% by weight based on the total weight percentage of the compound. For the teachings of Shanghai Haoyun as they relate to claim 177, see the above 102 rejection for claim 177. For the teachings of Shanghai Haoyun as they relate to substantially pure crystal forms, see the above 103 rejection for claim 174. One of ordinary skill in the art would therefore have a reasonable expectation of success in developing a pharmaceutical composition of Shanghai Haoyun’s crystal form wherein the crystal form is present in an amount of at least 90% by weight based on the total weight percentage of the compound, and claim 181 is prima facie obvious.
Claims 180, 182, and 186 are rejected under 35 U.S.C. 103 as being unpatentable over Shanghai Haoyun in view of Sun (Sun et al., 2010 Particle size specifications for solid oral dosage forms: A regulatory perspective, American Pharmaceutical Review pg. 68-73; Web Article Attached).
Claim 180 is directed towards the pharmaceutical composition of 177 wherein the crystal form has a d90 particle size distribution of about 32-40 microns. For the teachings of Shanghai Haoyun as they are relevant to claim 177, see the above 102 rejection for claim 177. Regarding the d90 particle size distribution, Shanghai Haoyun teaches a d90 value of 28.4 microns (Shanghai Haoyun, Figure 8), and explicitly states the crystal form’s uniform particle size distribution as a benefit of the form (Shanghai Haoyun, Translation, pg. 6). Particle size distribution is recognized in the art as a result-effective variable that can be optimized for particular pharmokinetic properties. See Sun:
The particle size distribution (PSD) of the drug substance may have significant effects on final drug product performance (e.g., dissolution, bioavailability, content uniformity, stability, etc.). Furthermore, the PSDs of both drug substance and excipients can affect drug product manufacturability (e.g., flowability, blend uniformity, compactibility, etc.), which, ultimately, can impact safety, efficacy, and quality of the drug product.
[Sun, Introduction]
One of ordinary skill in the art would therefore recognize the optimization of the d90 distribution from 28.4 microns to within applicant’s range of 32-40 microns as a case of routine optimization. See MPEP § 2144.05(II)(A):
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) (Claimed process which was performed at a temperature between 40°C and 80°C and an acid concentration between 25% and 70% was held to be prima facie obvious over a reference process which differed from the claims only in that the reference process was performed at a temperature of 100°C and an acid concentration of 10%.); see also Peterson, 315 F.3d at 1330, 65 USPQ2d at 1382 ("The normal desire of scientists or artisans to improve upon what is already generally known provides the motivation to determine where in a disclosed set of percentage ranges is the optimum combination of percentages."
One of ordinary skill in the art would thereby have a reasonable expectation of success in optimizing the d90 particle size distribution to be within applicant’s range, and claim 180 is prima facie obvious.
Claim 182 is directed towards a pharmaceutical composition comprising a crystalline anhydrous form of Vimseltinib with an XRPD pattern comprising peaks at 11.4, 14.7, 17.1, 20.1, and 29.1 ± 0.2 degrees 2θ, and wherein the crystal form has a d10 particle size distribution of about 2-10 microns, a d50 particle size distribution of about 12-24 microns, and a d90 particle size distribution of about 32-40 microns, and a pharmaceutically acceptable excipient.
For the teachings of Shanghai Haoyun as they relate to a pharmaceutical composition comprising an anhydrous form of Vimseltinib with the described XRPD pattern, see the above 102 rejection for claim 177. For the teachings of Shanghai Haoyun as they relate to the d10 and d50 particle size distributions, see the above 102 rejections for claims 178 and 179, respectively. For the teachings of Shanghai Haoyun and Sun as they relate to the d90 particle size distribution, see the above 103 rejection for claim 180. As each of the limitations are met, the combination of Shanghai Haoyun and Sun renders claim 182 prima facie obvious.
Claim 186 is directed towards a pharmaceutical composition comprising a crystalline anhydrous form of Vimseltinib with an XRPD pattern comprising peaks at 11.4, 14.7, 17.1, 20.1, and 29.1 ± 0.2 degrees 2θ, and wherein the crystal form has a d10 particle size distribution of about about 4 microns, a d50 particle size distribution of about 8 microns, and a d90 particle size distribution of about 16 microns, and a pharmaceutically acceptable excipient.
For the teachings of Shanghai Haoyun as they relate to a pharmaceutical composition comprising an anhydrous form of Vimseltinib with the described XRPD pattern, see the above 102 rejection for claim 177. For the teachings of Shanghai Haoyun and Sun as they relate to the optimization of the particle size distribution, see the above 103 rejection for claim 180. As the optimization of the particle size distribution is obvious, the combination of Shanghai Haoyun and Sun renders claim 186 prima facie obvious.
Claims 183-185 and 187-189 are rejected under 35 U.S.C. 103 as being unpatentable over Shanghai Haoyun in view of Sun and in further view of Rosenbaum (Rosenbaum et al., A phase 1b study of avelumab plus DCC-3014, a potent and selective inhibitor of colony stimulating factor 1 receptor (CSF1R), in patients with advanced high-grade sarcoma.. J Clin Oncol 39, 11549-11549(2021)).
Claim 183 is directed towards the pharmaceutical composition of claim 182 wherein the composition is in a capsule form and contains about 14 mg of the compound. For the teachings of Shanghai Haoyun and Sun as they relate to claim 182, see the above 103 rejection for claim 182. Regarding the capsule form, capsules are one of the most common oral dosage forms, and one of ordinary skill in the art would find their use obvious. Regarding the particular dosage of 14 mg, one of ordinary skill in the art would reasonably develop a dosage form of this amount, because Vemseltinib is already known in the art to be used in a dosage form of this amount (Rosenbaum, Abstract). Claim 183 is thereby prima facie obvious.
Claim 184 is directed towards the pharmaceutical composition of claim 182 wherein the composition is in a capsule form and contains about 20 mg of the compound. For the teachings of Shanghai Haoyun and Sun as they relate to claim 182, see the above 103 rejection for claim 182. Regarding the capsule form, capsules are one of the most common oral dosage forms, and one of ordinary skill in the art would find their use obvious. Regarding the particular dosage of 20 mg, one of ordinary skill in the art would reasonably develop a dosage form of this amount, because Vemseltinib is already known in the art to be used in a dosage form of this amount (Rosenbaum, Abstract). Claim 184 is thereby prima facie obvious.
Claim 185 is directed towards the pharmaceutical composition of claim 182 wherein the composition is in a capsule form and contains about 30 mg of the compound. For the teachings of Shanghai Haoyun and Sun as they relate to claim 182, see the above 103 rejection for claim 182. Regarding the capsule form, capsules are one of the most common oral dosage forms, and one of ordinary skill in the art would find their use obvious. Regarding the particular dosage of 30 mg, one of ordinary skill in the art would reasonably develop a dosage form of this amount, because Vemseltinib is already known in the art to be used in a dosage form of this amount (Rosenbaum, Abstract). Claim 185 is thereby prima facie obvious.
Claim 187 is directed towards the pharmaceutical composition of claim 186 wherein the composition is in a capsule form and contains about 14 mg of the compound. For the teachings of Shanghai Haoyun and Sun as they relate to claim 186, see the above 103 rejection for claim 186. Regarding the capsule form, capsules are one of the most common oral dosage forms, and one of ordinary skill in the art would find their use obvious. Regarding the particular dosage of 14 mg, one of ordinary skill in the art would reasonably develop a dosage form of this amount, because Vemseltinib is already known in the art to be used in a dosage form of this amount (Rosenbaum, Abstract). Claim 187 is thereby prima facie obvious.
Claim 188 is directed towards the pharmaceutical composition of claim 186 wherein the composition is in a capsule form and contains about 20 mg of the compound. For the teachings of Shanghai Haoyun and Sun as they relate to claim 186, see the above 103 rejection for claim 186. Regarding the capsule form, capsules are one of the most common oral dosage forms, and one of ordinary skill in the art would find their use obvious. Regarding the particular dosage of 20 mg, one of ordinary skill in the art would reasonably develop a dosage form of this amount, because Vemseltinib is already known in the art to be used in a dosage form of this amount (Rosenbaum, Abstract). Claim 188 is thereby prima facie obvious.
Claim 189 is directed towards the pharmaceutical composition of claim 186 wherein the composition is in a capsule form and contains about 30 mg of the compound. For the teachings of Shanghai Haoyun and Sun as they relate to claim 186, see the above 103 rejection for claim 186. Regarding the capsule form, capsules are one of the most common oral dosage forms, and one of ordinary skill in the art would find their use obvious. Regarding the particular dosage of 30 mg, one of ordinary skill in the art would reasonably develop a dosage form of this amount, because Vemseltinib is already known in the art to be used in a dosage form of this amount (Rosenbaum, Abstract). Claim 189 is thereby prima facie obvious.
Conclusion
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/ANTHONY JOSEPH SEITZ/Examiner, Art Unit 1629
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