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 .
Foreign Priority
The present application claims priority to the applications, CN2021/10608943.2 and PCT/CN2022/096548, with effective filing dates of 1 June 2021 and 1 June 2022, respectively.
Claim Status
This Office Action is in response to Applicant’s Amendment filed, 30 November 2023, wherein Applicant amended claims 3-5, 7, 8, and 12, canceled claims 6, 9-11, and 13-14, and added new claims 15 and 16.
Claims 1-5, 7-8, 12, and 15-16 are pending.
Information Disclosure Statement
The Information Disclosure Statement filed 30 November 2023 and the references cited therein have been considered, unless indicated otherwise.
Claim Interpretation
For purpose of clarity, the Examiner interprets the recitation of an injectable formulation in claim 8 to be parenteral administration: intravenous, intramuscular, subcutaneous, or intrathecal administration as evidenced by Gao (“Parenteral Route,” Osmosis, 2025, <https://www.osmosis.org/answers/parenteral-route>, accessed 11 February 2026).
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.
1. Claim 5 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.
Claim 5 recites an XRPD pattern is essentially as depicted in Fig. 1. The term “essentially” is not defined by the claim, the specification does not provide a standard for ascertaining the requisite degree, and one of ordinary skill in the art would not be reasonably apprised of the scope of the invention. Additionally, 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). See MPEP § 2173.05(s). Because claim 5 refers to Figure 1 and claims the XRPD pattern is essentially as depicted, it is ambiguous as to which exact peaks of the XRPD diffractogram Applicant considers part of the claimed invention and what degree of similarity would infringe.
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.
(a)(2) the claimed invention was described in a patent issued under section 151, or in an application for patent published or deemed published under section 122(b), in which the patent or application, as the case may be, names another inventor and was effectively filed before the effective filing date of the claimed invention.
2. Claims 1-5, 7-8, 12, 15, and 16 are rejected under 35 U.S.C. 102(a)(1) and 102(a)(2) as anticipated by or, in the alternative, under 35 U.S.C. 103 as obvious over Oh (U.S. Patent Publication No. 2021/0139461, published 13 May 2021) as evidenced by Wikipedia (“Water of crystallization,” Wikipedia, 2021, <https://web.archive.org/web/20210331151644/https://en.wikipedia.org/wiki/Water_of_crystallization>, accessed 11 February 2026) and Gele et al. (J Am Chem Soc Au, 2025, 5, 388-398) (“Gele”).
Oh teaches a crystalline form of the mesylate salt of
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, which is lazertinib as defined by claim 1 (abstract; [0001]).
Oh further teaches the XRPD peaks associated with a crystalline lazertinib mesylate form which has the IUPAC name: N-(5-(4-(4-((dimethylamino)methyl)-3-phenyl-1H-pyrazol-1-yl)pyrimidine-2-ylamino)-4-methoxy-2-morpholinophenyl)acrylamide (abstract; [0001]; [0074]). The XRPD peaks associated with the crystalline lazertinib mesylate are the following: 5.614, 12.394, 14.086, 17.143, 18.020, 19.104, 21.585, 22.131, and 22.487 ± 0.2 2θ ([0041]; [0074]). Oh additionally teaches generation of the lazertinib mesylate crystal via mixing lazertinib with mesylate chloride in water and acetone at 45-55 °C to generate the mesylate salt and then directly crystallizing the mesylate salt via addition of acetone at 40-50 °C and subsequent cooling ([0069]; [0070]). After cooling, the mesylate crystals are filtered under reduced pressure, washed with acetone, and vacuum dried at 55 °C ([0070]). While Oh is silent regarding if the crystals are hydrates, the crystals generated by Oh would be hydrates as evidenced by Wikipedia (“Water of crystallization,” Wikipedia, 2021, <https://web.archive.org/web/20210331151644/https://en.wikipedia.org/wiki/Water_of_crystallization>, accessed 11 February 2026). Wikipedia teaches when water molecules are present inside crystals, water was incorporated in the formation of crystals from aqueous solutions (page 1, paragraph 1). Additionally, Wikipedia teaches crystallization from water or moist solvents results in incorporation of water and that a salt with associated water of crystallization is known as a hydrate (page 1, paragraphs 2 and 5). Further, the manipulations specified in Oh would remove excess water in the vacuum filtration (filtration under reduced pressure; [0070]), but Wikipedia teaches that removal of water from the crystalline framework would require heating the sample (page 1, paragraph 2). As defined in the specification, hydrates of Lazertinib mesylate are stable to 100 °C (see the specification, page 16, lines 13-14). Thus, the manipulation of drying the hydrate of Lazertinib mesylate at 45-55 °C would not remove the water, and the crystals of Oh are hydrates ([0069]-[0070]).
Regarding claim 1, Oh teaches a hydrate of crystal of Lazertinib mesylate having the structure of Formula I:
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and XRPD peaks: 5.614° ± 0.2°, 21.585° ± 0.2°, and 22.487° ± 0.2°, which claim 1 defines as peaks representing Form A ([0041], [0069]-[0074]). The XRPD peaks were measured with Cu-Kα radiation, and the three XRPD peaks overlap with three recited peaks of the claimed invention: 5.68° ± 0.2°, 21.61° ± 0.2°, and 22.71° ± 0.2°. Thus, Oh teaches a hydrate Form A of Lazertinib mesylate having the structure of Formula I:
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and XRPD peaks: 5.614° ± 0.2°, 21.585° ± 0.2°, and 22.487° ± 0.2° ([0041], [0069]-[0074]).
Regarding claim 2, Oh teaches the XRPD pattern further has a characteristic peak at 17.143° ± 0.2°, which overlaps with the claimed invention at 17.21° ± 0.2°, ([0041], [0074]).
Regarding claim 3, Oh teaches the XRPD pattern further has a characteristic peak at 18.020° ± 0.2°, which overlaps with the claimed invention at 18.17° ± 0.2°, ([0041], [0074]).
Regarding claim 4, Oh teaches the XRPD pattern has peaks at the following: 5.614, 12.394, 14.086, 17.143, 18.020, 19.104, 21.585, 22.131, and 22.487 ± 0.2 2θ, which overlaps significantly with the claimed invention ([0041]; [0074]). It is unclear if the differences between the peaks of Oh and the peaks of the claimed invention are a result of the differences in the XRPD collection set-up or in the crystalline polymorph itself, as evidenced by Gele (J Am Chem Soc Au, 2025, 5, 388-398). Gele describes parameters in the XRPD collection set-up that affect the XRPD pattern, such as domain size, collection time, and structural elucidation methods (page 388, column 2, paragraph 3; page 389, column 1, paragraph 1; page 391, column 2, paragraph 4; page 392, column 1, paragraph 1; page 395, column 2, paragraph 7). Thus, it is reasonable to infer that the differences in the peaks of Oh and the claimed invention are from differences in XRPD set-up. Thus, Oh teaches the XRPD pattern has the peaks of claim 4.
Regarding claim 5, Oh teaches the XRPD pattern has peaks at the following: 5.614, 12.394, 14.086, 17.143, 18.020, 19.104, 21.585, 22.131, and 22.487 ± 0.2 2θ, which overlaps significantly with the claimed invention ([0041]; [0074]). It is unclear if the differences between the peaks of Oh and the peaks of the claimed invention are a result of the differences in the XRPD collection set-up or in the crystalline polymorph itself, as evidenced by Gele (J Am Chem Soc Au, 2025, 5, 388-398). Gele describes parameters in the XRPD collection set-up that affect the XRPD pattern, such as domain size, collection time, and structural elucidation methods (page 388, column 2, paragraph 3; page 389, column 1, paragraph 1; page 391, column 2, paragraph 4; page 392, column 1, paragraph 1; page 395, column 2, paragraph 7). Thus, it is reasonable to infer that the differences in the peaks of Oh and the claimed invention are from differences in XRPD set-up. Because Oh teaches a hydrate Form A of Lazertinib mesylate having peaks of the claimed invention, the hydrate Form A of Lazertinib mesylate of Oh would have the same the XRPD diffractogram, as evidenced by Gele (page 388, column 1, paragraph 2). Thus, Oh teaches an XRPD pattern that is essentially as depicted in Figure 1.
Regarding claim 7, Oh teaches that the hydrate Form A of Lazertinib mesylate is a pharmaceutical composition having at least one pharmaceutically acceptable additive ([0060]).
Regarding claim 8, Oh teaches hydrate Form A of Lazertinib mesylate is administered orally, topically, intravenously, intramuscularly, or subcutaneously ([0060]).
Regarding claim 12, Oh teaches inhibiting epidermal growth factor receptor (EGFR) having one or more mutations via hydrate Form A of Lazertinib mesylate ([0056]), which Oh teaches that EGFR mutations play a role in protein kinase-mediated disorders ([0004]). Thus, Oh teaches treating a protein kinase-mediated disorder via hydrate Form A of Lazertinib mesylate ([0055]).
Regarding claim 15, Oh teaches inhibiting epidermal growth factor receptor (EGFR) having one or more mutations via hydrate Form A of Lazertinib mesylate ([0056]), which Oh teaches that EGFR mutation positive is one of the mutations responsible for advanced non-small cell lung cancer ([0002]). Thus, Oh teaches treating non-small cell lung cancer hydrate Form A of Lazertinib mesylate ([0056]).
Regarding claim 16, Oh teaches inhibiting epidermal growth factor receptor (EGFR) having one or more mutations via hydrate Form A of Lazertinib mesylate ([0056]), which Oh teaches that EGFR mutation positive is one of the mutations responsible for advanced non-small cell lung cancer ([0002]). Thus, Oh teaches treating EGFR-mutation-positive non-small cell lung cancer via hydrate Form A of Lazertinib mesylate ([0056]).
Conclusion
No claim is allowed.
Any inquiry concerning this communication or earlier communications from the examiner should be directed to Madeline M Dekarske whose telephone number is (571)272-1789. The examiner can normally be reached Monday - Thursday 10am - 4pm.
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/MADELINE M. DEKARSKE/Examiner, Art Unit 1622
/JAMES H ALSTRUM-ACEVEDO/Supervisory Patent Examiner, Art Unit 1622