FINAL REJECTION
Receipt is acknowledged of Applicants' Amendments and Remarks, filed Jun. 24, 2026.
Rejections and/or objections not reiterated from previous Office Actions are hereby withdrawn. The rejections and/or objections set forth below are either maintained or newly applied, and constitute the complete set presently applied to the instant claims.
STATUS OF THE CLAIMS
No claims have been canceled, and no new claims have been added.
No claims have been amended.
Claims 6, 7, 9-14, and 18-21 stand withdrawn as drawn to nonelected inventions and/or species.
Thus, claims 1-5 and 15-17 now represent all claims currently pending and under consideration.
INFORMATION DISCLOSURE STATEMENT
The information disclosure statement (IDS) submitted on Jun. 24, 2026 was filed after the mailing date of the non-final action on Mar. 26, 2026. The submission is in compliance with the provisions of 37 CFR 1.97. Accordingly, the information disclosure statement is being considered by the examiner.
MAINTAINED REJECTIONS
The following rejections are maintained from the previous Office Action dated Mar. 26, 2026, on the ground that the references cited therein continue to read on the limitations of the instant claims.
Double Patenting Rejections
Claims 1-5 and 15-17 stand rejected on the ground of nonstatutory double patenting as being unpatentable over claims 1-4 and 6-14 of U.S. Patent No. 12/227,501.
Although the claims at issue are not identical, they are not patentably distinct from each other because the reference compounds and the examined compounds share the identical pyrrolo[3,2-c]pyridinone structural core, as shown side-by-side below for comparison:
Examined Claim 1 (instant application)
Reference Claim 1 ('501 patent)
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L is C-C or C=C,
unsubstituted or substituted by C1-3 alkyl, etc.
R13a and R13b are H, C1-4 alkyl, etc.
R1, R2a, R2b, R2c is
H, -OH, cyano, halo, etc.
R1, R2a, R2b, R2c can be
H, -OH, cyano, halo, etc.
A is selected from
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502
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A is selected from
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X is methylene or ethylene
X is methylene or ethylene
Y is phenyl or heteroaryl
Y is phenyl or heteroaryl
The reference compounds and the examined compounds also share the identical function as casein kinase 1A (CSNK1A) inhibitors.
The reference compounds differ only in that position 7 of the pyrrolo[3,2-c]pyridinone core is unsubstituted; whereas the examined compounds require a substituent at position 7, e.g., C1-3 alkyl.
For example, reference claim 4 recites the compound of Example 61, which differs from compound 10 of examined claim 5 only by a methyl substitution:
Compound 61 (reference claim 4)
Compound 10 (examined claim 5)
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However, where a prior art compound shares the same utility as those claimed, one of ordinary skill in the art would have a reasonable expectation that modifying the compound by the interchange of hydrogen and alkyl would yield compounds having similar properties. Hydrogen and methyl substitutions are known in the art and have been held to be obvious variants of each other. See MPEP § 2144.09 and In re Dillon, 919 F.2d 688, 16 USPQ2d 1897 (Fed. Cir. 1990).
Reference claim 12 recites a pharmaceutical composition comprising a compound of general formula (I) together with at least one pharmaceutically acceptable auxiliary (excipient), as recited by examined claim 15.
Reference claims 6-11 and 13 recite methods of administering a compound of general formula (I) to treat lymphoma, lung cancer, colon cancer, and metastases thereof in a subject, as recited by examined claim 16.
Reference claim 14 recites a combination comprising one or more first active ingredients selected from a compound of general formula (I), and one or more second active ingredients selected from chemotherapeutic anti-cancer agents and target-specific anti-cancer agents, as recited by examined claim 17.
For the foregoing reasons, examined claims 1-5 and 15-17 would be obvious over the claims of USPN 12,227,501.
Claims 1-5 and 15-17 stand provisionally rejected on the ground of nonstatutory double patenting as being unpatentable over claims 1-5, 8-15, and 17 of copending Application No. 18/018,207 (reference application) in view of Graham et al. (WO 2016/120196, of record).
Although the claims at issue are not identical, they are not patentably distinct from each other because reference formula (I) and examined formula (I) are identical with the exception of the -NH- linker to the A-ring, as shown side-by-side below for comparison:
Examined Claim 1 (instant application)
Reference Claim 1 ('207)
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A is phenyl, pyridine, other monocyclic heteroaryl
A is phenyl, pyridine, other monocyclic heteroaryl with no NH linker
R1 is H, C1-4 alkyl, C3-6 cycloalkyl, etc.
R1 is H, C1-4 alkyl, C3-6 cycloalkyl, etc.
L is C-C or C=C
L is C-C or C=C
R2a, R2b, R2c are H, -OH, cyano, halo, etc.
R2a, R2b, R2c are H, -OH, cyano, halo, etc.
X is methylene or ethylene
X is methylene or ethylene
Y is phenyl or heteroaryl
Y is phenyl or heteroaryl
Compounds of formula (I) of reference claims 1-5 differ from the examined claims only in that the reference compounds lack the -NH- linker between the A ring and the pyrrole ring.
However, Graham et al. disclose compounds of formula (I) (claim 1), having the structural formula,
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wherein E is, e.g., pyridine; and A is phenyl or pyridine.
Thus, Graham et al. explicitly disclose, teach, and suggest that compounds of formula (I) may be substituted on the pyrrole ring by NH-aryl or NH-heteroaryl for use in treating various types of hyperproliferative disorders, including solid tumors, such as cancers of the breast, respiratory tract, brain, reproductive organs, digestive tract, urinary tract, eye, liver, skin, head and neck, thyroid, parathyroid, and their distant metastases; as well as lymphomas, sarcomas, and leukemias (p. 72, line 7 to p. 73, line 28).
Modifying the reference compounds by including an NH linker to ring A (aryl or heteroaryl), as taught by Graham et al., yields compounds which fall within the scope of formula (I) as recited by the examined claims.
It would have been predictable to one of ordinary skill in the art as of the filing date to modify the reference compounds by adding an -NH- linker between the A ring substituent (aryl or heteroaryl) and the pyrrole ring to arrive at the compounds of the examined claims with a reasonable expectation of success, because both the reference compounds and the compounds of Graham et al. are disclosed to be useful for treating the same diseases, such as cancer, tumors, and neoplasms, in the same patient populations.
As recognized by MPEP § 2144.09, a prima facie case of obviousness may be made when chemical compounds have (1) very close structural similarities and (2) similar utilities. "An obviousness rejection based on similarity in chemical structure and function entails the motivation of one skilled in the art to make a claimed compound, in the expectation that compounds similar in structure will have similar properties." In re Payne, 606 F.2d 303, 313, 203 USPQ 245, 254 (CCPA 1979).
Reference claim 15 recites a pharmaceutical composition comprising a compound of general formula (I) together with at least one pharmaceutically acceptable auxiliary (excipient), as recited by examined claim 15.
Reference claims 8-14 recite methods of treating or preventing hematological tumors, solid tumors and/or metastases thereof by administering a compound of general formula (I), as recited by examined claim 16.
Reference claim 17 recites a combination comprising one or more first active ingredients selected from a compound of general formula (I), and one or more second active ingredients selected from chemotherapeutic anti-cancer agents and target-specific anti-cancer agents, as recited by examined claim 17.
For the foregoing reasons, examined claims 1-5 and 15-17 would have been prima facie obvious over US Application No. 18/018,207 in view of Graham et al.
This is a provisional nonstatutory double patenting rejection because the patentably indistinct claims have not in fact been patented.
RESPONSE TO ARGUMENTS
With respect to the rejection of claims 1-4 and 15-17 under 35 U.S.C. 103 over Graham et al. in view of Vernier et al., Applicant’s arguments, see Remarks, pp. 25-29, filed Jun. 24, 2026, have been fully considered and are persuasive. Therefore, this rejection is withdrawn.
With respect to the rejection of claims 1-5 and 15-17 on the ground of nonstatutory double patenting over claims 1-4 and 6-14 of U.S. Patent No. 12/227,501, Applicant's arguments filed Jun. 24, 2026 have been fully considered but they are not persuasive.
Applicant contends that in claimed formula (I),
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,
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and R17 excludes hydrogen. Hence, L does not encompass an unsubstituted single C-C bond. Thus, the claimed genus of the '501 patent does not overlap the pending claims at least because the reference patent requires this position to be unsubstituted (Remarks, pp. 23-24).
Further, Applicant argues that the rejection does not explain why a person of ordinary skill in the art would have chosen to focus on this specific position in the structure of claim 1 of the '501 patent (out of the multiple options available) for modification, absent impermissible hindsight knowledge of the claimed invention (Remarks, p. 24).
Beyond this, the data in the specification of the present application experimentally
demonstrate that numerous compounds within the claim scope are potent inhibitors of casein kinase 1A (CSNK1A) (below 100 nM) whilst showing selectivity over the wild-type EGFR kinase (thus reducing potential toxicity). Specification p. 198 and Tables 1-4. Applicants respectfully submit that a person having ordinary skill in the art would not have been able to predict these beneficial properties in light of the claims of the '501 patent (Remarks, p. 25).
However, as recognized by MPEP § 2143, the lead compound cases do not stand for the proposition that identification of a single lead compound is necessary in every obviousness rejection of a chemical compound.
MPEP § 2144.09 recognizes situations when a prima facie case of obviousness may be made when chemical compounds have very close structural similarities and similar utilities. "An obviousness rejection based on similarity in chemical structure and function entails the motivation of one skilled in the art to make a claimed compound, in the expectation that compounds similar in structure will have similar properties." In re Payne, 606 F.2d 303, 313, 203 USPQ 245, 254 (CCPA 1979). Close structural similarity between chemical compounds (e.g., homologs, analogues, and isomers) is enough, with no need for lead compound analysis.
Further, the compounds of the ‘501 patent are disclosed to have the same function as the claimed compounds, as casein kinase 1A (CSNK1A) inhibitors. As noted in the rejection set forth above, the reference compounds and the examined compounds differ by only an alkyl (methyl) substitution at position 7. Hydrogen and methyl substitutions are known in the art and have been held to be obvious variants of each other. The interchange of an alkyl group and hydrogen, in and of itself, is obvious. See MPEP § 2144.09 and In re Dillon, 919 F.2d 688, 16 USPQ2d 1897 (Fed. Cir. 1990). Therefore, the rejection is maintained.
Applicant's arguments do not address the rejection of claims 1-5 and 15-17 on the ground of nonstatutory double patenting over co-pending application 18/018,207 (reference application) in view of Graham et al. Therefore, the rejection is maintained.
CONCLUSION
No claims are allowed.
THIS ACTION IS MADE FINAL. 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.
CORRESPONDENCE
Any inquiry concerning this communication or earlier communications from the examiner should be directed to SARA E. TOWNSLEY whose telephone number is 571-270-7672. The examiner can normally be reached on Mon-Fri from 10:00 am to 6:00 pm (EST). If attempts to reach the examiner by telephone are unsuccessful, the examiner's supervisor, Jeff S. Lundgren, can be reached at 571-272-5541. The fax phone number for the organization where this application or proceeding is assigned is 571-273-8300.
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/SARA E. TOWNSLEY/Examiner, Art Unit 1629
