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
Claims 1-20 are pending in the instant application.
Claims 1-3, 9-12, 14-17, and 19-20 are amended.
Claims 4-8, 13, and 18 have been cancelled.
Claims 15, 17, and 19-20 are withdrawn from consideration.
Claims 1-3, 9-12, 14 and 16 are examined herein.
Priority
The instant application claims benefit of foreign priority to CN202010183457.6, filed on 16 March 2020, and CN202011279917.1, filed on 16 November 2020 and the benefit of priority to PCT/CN2021/081126, filed on 16 March 2021. The claims to the benefit of priority are acknowledged. As such, the effective filing date of the claims is 16 March 2020.
Information Disclosure Statement
The information disclosure statements (IDS), submitted on 13 September 2022, 11 October 2023, 15 March 2024, 12 June 2024, 04 September 2024, 21 February 2025, are acknowledged and considered. The submissions are in compliance with the provisions of 37 CFR 1.97.
Response to Arguments
The amendment filed on 23 December 2025 has been entered.
In view of applicant amendment to claims 1 and 9, the objections of record are withdrawn.
In view of applicant amendment to claims 1-3, 9-12, 14, and 16 the 112(a)-written description rejection of record is withdrawn.
In view of applicant amendment to claim 3 the 112(b) rejection of record is withdrawn.
With respect to the 103 rejection, the Applicant argues superior inhibitory activity against the compounds of the prior art. To substantiate this the Applicant presents experimental results as a part of their remarks. The Examiner requests the experimental results be submitted as a declaration so they may be considered against the 103 rejection as evidence. As it stands, the experimental results have not been considered. Therefore the rejection is maintained and amended to reflect the claim cancellations.
All rejections and objections not found below have been withdrawn.
MAINTAINED REJECTIONS
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.
The factual inquiries for establishing a background for determining obviousness under 35 U.S.C. 103 are summarized as follows:
1. Determining the scope and contents of the prior art.
2. Ascertaining the differences between the prior art and the claims at issue.
3. Resolving the level of ordinary skill in the pertinent art.
4. Considering objective evidence present in the application indicating obviousness or nonobviousness.
This application currently names joint inventors. In considering patentability of the claims the examiner presumes that the subject matter of the various claims was commonly owned as of the effective filing date of the claimed invention(s) absent any evidence to the contrary. Applicant is advised of the obligation under 37 CFR 1.56 to point out the inventor and effective filing dates of each claim that was not commonly owned as of the effective filing date of the later invention in order for the examiner to consider the applicability of 35 U.S.C. 102(b)(2)(C) for any potential 35 U.S.C. 102(a)(2) prior art against the later invention.
Claim(s) 1-3, 9-12, 14 and 16 is/are rejected under 35 U.S.C. 103 as being unpatentable over Beatty et al. (WO2018136700, cited by applicant on 1449 IDS).
Regarding claims 1 and 12, Beatty discloses a compound of Formula (I) (claim 1) (pictured below) which overlaps with the instant Formula (I) when
G1 is N or CR3a, where R3a is H
G2 is CR3
G3- is N
Ar1 is phenyl or a 5-6 membered heteroaryl, optionally substituted with 1-3 R9; wherein R9 is C1-8 alkyl, halogen, cyano, and C-1-3 alkoxy; wherein each R9 is optionally substituted with 1-3 R11; wherein R11 is hydroxyl, halo, cyano, C alkyl, or C3-8 cycloalkyl
Ar2 is phenyl or 5-6 membered heteroaryl, optionally substituted
R1a is hydrogen, deuterium, or forms a 5-6 membered heterocyclic ring with R1b
R1b is hydrogen, deuterium, or forms a 5-6 membered heterocyclic ring with R1a
R2 is hydrogen
R4 is hydrogen of C1-3 alkyl
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Beatty does not teach that R3, which corresponds to the instant Rc, is fluorine, chlorine, cyano,
C1-3- alkoxyl or C1-8- haloalkyl. Beatty teaches that R3 can be H or C1-3- alkyl.
Patani teaches that fluorine is a bioisostere for hydrogen (page 3149) and demonstrates improved binding affinity with the replacement (Table 4)
It would be prima facie obvious to one of ordinary skill in the art to substitute the hydrogen, taught by Beatty, with fluorine, or to substitute one of the hydrogens in the C1-3- alkyl with hydrogen, as Patani demonstrates the bioisosteric substitution between hydrogen and fluorine. One skilled in the art would be motivated by a shared utility to make this modification with an expectation of success and improved potency.
Regarding claim 2, Beatty teaches that Ar1, which corresponds to the instant A, is phenyl or a 5-6 membered heteroaryl (claim 1). Pyrimidinyl is an explicit example of a heterocycles given (paragraph [0055]).
Regarding claim 3, Beatty teaches that R3, which corresponds to the instant Rc is hydrogen. Patani teaches that fluorine is a bioisosteric substitution for hydrogen. Substituting hydrogen for fluorine would be prima facie obvious and lead to the instant invention.
Regarding claim 9, Beatty teaches Ar2, which corresponds to the instant B, to be phenyl, optionally substituted once or twice with halo, cyano, or C1-8 alkyl (claim 1).
Regarding claim 10, Beatty teaches that R9 can be C1 alkyl, optionally substituted with 1-3 R11 groups, which corresponds to the instant RL1, RL2 and Rp-. If R9 is unsubstituted the instant RL1, RL2 and Rp- are hydrogen. If substituted they can be hydroxyl, halo, cyano, C alkyl, or C3-8 cycloalkyl (claim 1).
Regarding claim 11, Beatty teaches that R9 can be halogen or C1-8 alkyl (claim 1).
Regarding claim 14 and the elected species L-1 (pictured below, right), Beatty teaches the preferred embodiment (pictured below, left) on page 407. Minimal modification is required to arrive at the instant compound. The reference compound has G2 substituted with nitrogen and G3 substituted with CR3c, wherein R3c is H. Modifying this to the opposite, so G3 is nitrogen and G2 is CR3, where R3 is hydrogen then substituted with its bioisostere fluorine leads to non-elected species L-5 (seen in instant claim 15). One more modification, substituting the fluorine depicted on the right phenyl ring with methyl, which is not only an isosteric replacement but also one taught by Beatty for substituent R10, leads to the instant L-1.
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Regarding claim 16, Beatty teaches the pharmaceutical composition comprising a compound of Formula (I) and a pharmaceutically acceptable excipient (claim 25).
Conclusion
Claims 1-3, 9-12, 14 and 16 are rejected.
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 Jerica K Wilson whose telephone number is (703)756-4690. The examiner can normally be reached Monday-Friday 9:00-5:00.
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/J.K.W./Examiner, Art Unit 1621
/CLINTON A BROOKS/Supervisory Patent Examiner, Art Unit 1621