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 . Claims 1-7, 13, 18, 22, 28, 34, 40, 44, 49, 55, 61, 65, 68, 74, 78, 82, 87, 91, 97-98, 102, 133, 137-139 and 154-156 filed August 04, 2026 are currently pending.
Election/Restrictions
Applicant’s election without traverse of Group (I), claims 1-7, 13, 18, 22, 28, 34, 40, 44, 49, 55, 61, 65, 68, 74, 78, 82, 87, 91 and 137-138 in the reply filed on 08/04/2026 is acknowledged.
Claims 97-98, 102, 133, 139 and 154-156 are withdrawn from further consideration pursuant to 37 CFR 1.142(b) as being drawn to a nonelected invention, there being no allowable generic or linking claim. Election was made without traverse in the reply filed on 08/04/2026.
Secondly, Applicant’s election of species of a fumarate crystalline form of Compound (I), elected without traverse in the reply filed on 08/04/2026 is acknowledged.
Claims 28, 34, 40, 44, 49, 55, 61, 65, 68, 74, 78, 82, 87, 91 are withdrawn from further consideration pursuant to 37 CFR 1.142(b) as being drawn to a nonelected crystalline species of Formula (I), there being no allowable generic or linking claim. Election was made without traverse in the reply filed on 08/04/2026.
Priority
Acknowledgement is made of the national stage entry of PCT/CN2022/129169 filed 10/19/2022, which claims foreign priority to PCT/CN2021/125016 filed 10/20/2021.
Information Disclosure Statement
The information disclosure statements (IDS) submitted on 07/18/2024 and 08/04/2026 are in compliance with the provisions of 37 CFR 1.97. Accordingly, the information disclosure statement is being considered by the examiner.
Claim Rejections - 35 USC § 112-Paragraph 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.
Claim 4 is 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 4 is directed to the crystalline form according to claim 1, wherein the complex has an acid/base molar ratio of 0.5:1 to 3:1, preferably, 0.5:1 to 2.5:1, more preferably, 1:1 to 1.5:1.
Regarding claim 4, the phrase "preferably" renders the claim indefinite because it is unclear whether the limitation(s) following the phrase are part of the claimed invention. For example, one interpretation of the claims is that an acid/base molar ratio of 0.5:1 reads on the presently claimed. An alternative interpretation of the claim is that said 0.5:1 molar ratio does not read on the claim as it lies outside of the preferred 1:1 to 1.5:1. molar ratio. See MPEP § 2173.05(d).
Accordingly, one of ordinary skill in the art would not have been apprised of the metes and bounds of the subject matter for which Applicant was presently seeking protection.
Claims 7, 13, 18 and 22 is 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 term “substantially” in the phrase “substantially the same X-ray diffraction pattern as Figure 1” in claim 7 is a relative term which renders the claim indefinite. The term “substantially” is not defined by the claim. In addition, the specification does not provide a standard for ascertaining the requisite degree to identify which specific peaks and the specific number of x-ray diffraction peaks an XRPD must have in order to read on the claimed “substantially the same X-ray diffraction pattern as Figure 1”. Further, the specification fails to provide a reference to identify which peaks are outside the boundary of “substantially the same X-ray diffraction pattern as Figure 1”. As recited in MPEP 2173.05 the meaning of every term used in a claim should be apparent from the prior art or from the specification and drawings at the time the application is filed. Claim language may not be "ambiguous, vague, incoherent, opaque, or otherwise unclear in describing and defining the claimed invention." In re Packard, 751 F.3d 1307, 1311, 110 USPQ2d 1785, 1787 (Fed. Cir. 2014). Applicants need not confine themselves to the terminology used in the prior art, but are required to make clear and precise the terms that are used to define the invention whereby the metes and bounds of the claimed invention can be ascertained. In the present case, Applicant has not done so regarding the boundaries of “substantially the same X-ray diffraction pattern as Figure 1” and accordingly, one of ordinary skill in the art would not have been reasonably apprised of the metes and bounds of the subject matter Applicant was seeking protection.
This situation is duplicated in the phrase “substantially the same X-ray diffraction pattern as Figure 6” found in claim 13, “substantially the same X-ray diffraction pattern as Figure 10” found in claim 18 and “substantially the same X-ray diffraction pattern as Figure 11” found in claim 22.
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.
Claim(s) 1-3, 137-138 are rejected under 35 U.S.C. 102(a)(1) as being anticipated by Zhao (WO2020/057511 published 03/26/2020).
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Zhao (WO2020/057511 published 03/26/2020). Zhao teaches compounds of
Formula (I) as potent inhibitors of EGFR tyrosine kinase (abstract, pages 1-3). Embodied within Formula (I) of Zhao is Example 31 or (R)-N-(4-([1,2,4]triazolo[1,5-c]pyrimidin-7-yloxy)-3-methylphenyl)-5-(,3-dioro-1-methylpiperidin-4-y)oxy)-6 methoxyquinazolin-4-amine, shown above, which reads on presently claimed Compound (I) (pages 43, 128, 130-131). Preparation of crystalline forms or polymorphic forms of compounds of Formula (I) is embraced within the teachings of Zhao, either as a free base or acid salt form. Regarding claim 2, solvated forms of said preparations is also taught by Zhao (pages 57, 60-62). As such, one of ordinary skill in the art would immediately envisage a generic crystalline form of each compound disclosed within Zhao, including a generic crystalline form of the compound of claim 31, which reads on the presently claimed invention. Regarding claims 137-138, formulation of said crystalline form with a pharmaceutically acceptable carrier to yield a pharmaceutical dosage form of said crystalline composition is embodied within the teachings of Zhao (pages 76-82).
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.
Claim(s) 1-6, 137-138 are rejected under 35 U.S.C. 103 as being unpatentable over the combination of Zhao (WO2020/057511 published 03/26/2020) and Ware (Pharmaceutical Research Vol. 21 pages 177-184. Published 2004).
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Zhao teaches compounds of Formula (I) as potent inhibitors of EGFR tyrosine kinase (abstract, pages 1-3). Embodied within Formula (I) of Zhao is Example 31 or (R)-N-(4-([1,2,4]triazolo[1,5-c]pyrimidin-7-yloxy)-3-methylphenyl)-5-(,3-dioro-1-methylpiperidin-4-y)oxy)-6 methoxyquinazolin-4-amine, shown above, which reads on presently claimed Compound (I) (pages 43, 128, 130-131).
Preparation of crystalline forms or polymorphic forms of compounds of Formula (I) is embraced within the teachings of Zhao, either as a free base or acid salt form. Regarding claim 2, solvated forms of said preparations is also taught by Zhao (pages 57, 60-62). Regarding claims 3-6, the fumarate salt form is taught by Zhao as one of 16 suitable pharmaceutically acceptable salt forms for compounds of Formula (I). (pages 60-61). Regarding claims 137-138, formulation of said crystalline form with a pharmaceutically acceptable carrier to yield a pharmaceutical dosage form of said crystalline composition is embodied within the teachings of Zhao (pages 76-82).
The difference between the presently claimed crystalline composition and that taught by Zhao is that Zhao does not explicitly teach the use of a 1:1 molar ratio of acid to free base.
Ware (Pharmaceutical Research Vol. 21 pages 177-184. Published 2004) teaches high-throughput screening of salt forms for pharmaceutical formulation. Ware teaches preparation of salt forms in a 1:1 molar ratio of acid to free base (page 178 left col.).
Therefore, one of ordinary skill in the art prior to the time of the invention would have found it prima facie obvious to formulate the crystalline preparation of Example 31 of Zhao, as a fumarate salt form in view of Zhao in order to arrive at the presently claimed composition.
MPEP 2143 provides rationale for a conclusion of obviousness including (E):
(E) "Obvious to try" – choosing from a finite number of identified, predictable solutions, with a reasonable expectation of success;
In the present case, the fumarate salt form was one of 16 suitable pharmaceutically acceptable salt forms for crystalline compounds of Formula (I) of Zhao (pages 60-62). Accordingly, one of ordinary skill would have selected and applied the fumarate salt teaching of Zhao to Example 31 of Zhao, arriving at the presently claimed with a reasonable expectation of success.
Secondly, one of ordinary skill in the art at the time of the invention would have found it prima facie obvious to employ a 1:1 molar ratio of acid to free base in preparation of salt form above in view of Ware.
MPEP 2143 provides rationale for a conclusion of obviousness including (A): Combining prior art elements according to known methods to obtain predictable results;
In the present case, Ware discloses 1:1 molar ratio of acid to free base is an art-recognized, routine ratio when preparing pharmaceutical salt forms (page 178 left col.). Consistent with this reasoning, it would have been obvious to have selected the 1:1 molar ratio of acid to free base technique from within the prior art of Ware above and apply it to the preparation of a crystalline salt form of Example 31 taught by Zhao above, arriving at the claimed composition yielding no more than one would expect from such an arrangement.
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 1-3 and 137 are rejected on the ground of nonstatutory double patenting as being unpatentable over claims 1, 15 and 28 of U.S. Patent No. 11,723,908.
Although the claims at issue are not identical, they are not patentably distinct from each other because of the following. Claim 1 of U.S Patent 11,723,908 is directed to a compound of Formula (I) or a pharmaceutically acceptable salt thereof. Claim 28 is directed to the following compound of Formula (I), which is the same as that embraced within claim 1 of the present application.
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For double patenting of previously disclosed, but newly claimed utility, please see Sun Pharmaceutical Industries v. Eli Lilly and Co., 611 F.3d 1381, 1389 (2010). The court in In Sun Pharmaceutical Industries v. Eli Lilly and Co., 611 F.3d 1381, 1389 (2010), states that “[W]e have held, however that there are “certain instances” where the specification of an earlier patent may be used in the obvious-type double patenting analysis. In re Basell, 547, F.3d at 1378. Specifically, the specification’s disclosure may be used to determine whether the claim “merely defines an obvious variation of what is earlier disclosed and claimed”, “to learn the meaning of claim terms” and to “interpret the coverage of a claim” (page 12). Specifically, column 73 and column 77 of U.S. Patent 11,723,908 discloses that different crystal forms, polymorphs, solvated forms and pharmaceutically acceptable salts of each of the disclosed compounds are embodied within the genus of Formula (I). As such, one of ordinary skill in the art would immediately envisage a generic crystalline form of each compound disclosed within U.S. Patent 11,723,908, including a generic crystalline form of the compound of claim 28, which reads on the presently claimed invention. Claim 15 of U.S. Patent 11,723,908 is directed to the disclosed compound and a pharmaceutically acceptable carrier, which overlaps with the subject matter of present claim 137.
Conclusion
Claims 1-7, 13, 18, 22 and 137-138 are rejected. No claim is allowed.
Any inquiry concerning this communication or earlier communications from the examiner should be directed to GEORGE W KOSTURKO whose telephone number is (571)270-5903. The examiner can normally be reached M-F 9:00-5:30.
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If attempts to reach the examiner by telephone are unsuccessful, the examiner’s supervisor, CLINTON A BROOKS can be reached at 571-270-7682. The fax phone number for the organization where this application or proceeding is assigned is 571-273-8300.
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/GEORGE W KOSTURKO/Primary Examiner, Art Unit 1621
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