Prosecution Insights
Last updated: April 19, 2026
Application No. 18/005,952

5-HT2A RECEPTOR INHIBITOR OR INVERSE AGONIST, PREPARATION METHOD THEREFOR, AND APPLICATION THEREOF

Non-Final OA §103§112
Filed
Jan 18, 2023
Examiner
MAHLUM, JONATHAN DAVIS
Art Unit
1625
Tech Center
1600 — Biotechnology & Organic Chemistry
Assignee
Geneora Pharma (Shijiazhuang) Co. Ltd.
OA Round
1 (Non-Final)
54%
Grant Probability
Moderate
1-2
OA Rounds
3y 9m
To Grant
71%
With Interview

Examiner Intelligence

Grants 54% of resolved cases
54%
Career Allow Rate
12 granted / 22 resolved
-5.5% vs TC avg
Strong +17% interview lift
Without
With
+16.7%
Interview Lift
resolved cases with interview
Typical timeline
3y 9m
Avg Prosecution
51 currently pending
Career history
73
Total Applications
across all art units

Statute-Specific Performance

§101
2.9%
-37.1% vs TC avg
§103
33.7%
-6.3% vs TC avg
§102
18.9%
-21.1% vs TC avg
§112
24.5%
-15.5% vs TC avg
Black line = Tech Center average estimate • Based on career data from 22 resolved cases

Office Action

§103 §112
Detailed Action The present office action is in response to the response filed on 05 Nov 2025. 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 . Status Claim 8 of the pending application have been examined on the merits. Claims 1-7 and 9-10 are withdrawn (see “Response to Applicant Election” below). Priority Applicants identify the instant application, Serial #: 18/005,952, filed 18 Jan 2023, as a National Stage Entry of International Patent Application #: PCT/CN2021/107774, filed 22 Jul 2021, which claims foreign priority from Foreign Application #s: CN202110364023.0, filed 03 Apr 2021, and CN202010708352.8, filed 22 Jul 2020. Information Disclosure Statement The information disclosure statement(s) (IDS) submitted on 18 Jan 2023, 05 May 2023, and 18 Aug 2025 are in compliance with the provisions of 37 CFR 1.97. Accordingly, the information disclosure statement is being considered by the examiner. Election/Restrictions Applicant’s election of Group I, claims 1-9, and the species of Compound 20 (see below) in the reply filed on 05 Nov 2025 is acknowledged. PNG media_image1.png 148 180 media_image1.png Greyscale Because applicant did not distinctly and specifically point out the supposed errors in the restriction requirement, the election has been treated as an election without traverse (MPEP § 818.01(a)). Claim 10 is withdrawn from further consideration pursuant to 37 CFR 1.142(b) as being drawn to a nonelected group, there being no allowable generic or linking claim. Election was made without traverse in the reply filed on 05 Nov 2025. Claims 1-7 and 9 withdrawn from further consideration pursuant to 37 CFR 1.142(b) as being drawn to a nonelected species, there being no allowable generic or linking claim. Specifically, the elected species of Compound 20 reads on a Compound of Formula (I) (below) when X1 and X4 are both CH, however, in claim 1 it is specified that one of X1 or X4 must be N. Formula (I) Compound 20 PNG media_image2.png 170 243 media_image2.png Greyscale PNG media_image1.png 148 180 media_image1.png Greyscale Thus claim 1 and the claims that depend on claim 1 are withdrawn for being drawn to a non-elected species. Election was made without traverse in the reply filed on 05 Nov 2025. Claim Objections Claim 8 is objected to because of the following informalities: compounds 88-102 of claim 8 have poor image resolution and are verging on unreadable (pg. 15). Applicant may overcome this objection by submitting higher resolution substitute structures. Appropriate correction is required. 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. 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 8 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 8 contains Markush groupings which do not have the coordinating conjunctions “and” or “or” to properly limit the alternatives defined in the list. See MPEP § 2117(I). Applicant may overcome this rejection by adding the proper coordinating conjunction to each Markush group in need of one. 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) 8 is/are rejected under 35 U.S.C. § 103 as being unpatentable over US 2005/0261278, hereinafter ‘278, further in view of Hacksell et al. (Neurochem Res, 2014, 39:2008-2017), hereinafter Hacksell, Patani et al. (Chem Rev, 1996, 96:3147-3176), hereinafter Patani, and Brooks et al. (ACS Med Chem Lett, 2019, 10:1228-1233), hereinafter Brooks. In the response filed 05 Nov 2025, applicant elected Group I, claims 1-9, and the following species which reads on claim 8: PNG media_image3.png 148 180 media_image3.png Greyscale ‘278 teaches compounds of Formula (III) (paragraph [0049]): PNG media_image4.png 85 228 media_image4.png Greyscale , where the Ar groups can be variable with cycles or heterocycles. ‘278 also teaches a compounds of Formula (I) (paragraph [0061]): PNG media_image5.png 150 299 media_image5.png Greyscale Which is a compound of Formula (III) when Ar1 is substituted aryl; Y2 is a bond; Y1 is methylene; Z is PNG media_image6.png 123 72 media_image6.png Greyscale ; R is methylene; n is 1; W is O; X1 is NH; X2 is methylene; and Ar2 is a substituted aryl group (paragraphs [0050]-[0059]). However, '278 does not teach the instantly elected compound. Hacksell teaches that the compound of Formula (I) taught by '278 is pimavanserin, a drug with selectivity of the 5-HT2A receptor with nanomolar potency as an inverse agonist and no meaningful activity at any other G-protein coupled receptor (pg. 2008, column 1). Patani teaches that bioisosterism represents one approach used by the medicinal chemist for the rational modification of lead compounds into safe and more clinically effective agents and the concept of bioisosterism is often considered to be qualitative and intuitive (pg. 3147, columns 1-2). Patani further teaches that substitution of benzene with pyridine is considered one of the classical bioisosteres and the replacement of -CH= with -N= is commonly used in drug design (pg. 3158, column 1; pg. 3159, column 2). Brooks teaches that a phenyl-alkoxy group with a pyridine-alkoxy group reduced clearance and extend mean residence time for a TRPV4 inhibitor (pg. 1231, column 1). Brooks teaches that an extended mean residence time is highly desirable as it minimizes the peak to trough concentrations during a dose, improving therapeutic index and enabling a lower overall dose (pg. 1228, column 2). MPEP 2144.08(II)(A)(4)(c) states that the “closer the physical and/or chemical similarities between the claimed species or subgenus and any exemplary species or subgenus disclosed in the prior art, the greater the expectation that the claimed subject matter will function in an equivalent manner to the genus. See, e.g., Dillon, 919 F.2d at 696, 16 USPQ2d at 1904 (and cases cited therein).” Based on the teachings of '278, Hacksell, Patani, and Brooks, a person having ordinary skill in the art would substitute the phenyl-alkoxy ring of the compound of Formula (I), taught by '278 and Hacksell, with a pyridinyl-alkoxy group, taught by Patani and Brooks, and arrive at the instantly elected compound. It is commonly known that benzene and pyridine are exchanged to rationally modify compounds in medicinal chemistry, as found in Patani, and the artisan would have been motivated to perform the swap of phenyl for pyridinyl in order to reduce clearance and extend the mean residence time, as taught by Brooks. The artisan would have a reasonable expectation of success that the modified compound of Formula (III) would retain the functionality of the compound of Formula (III) because of the similarities between the compound of Formula (III) and the instantly elected compound. A reference is good not only for what it teaches by direct anticipation but also for what one of ordinary skill in the art might reasonably infer from the teachings (In re Opprecht 12 USPQ 2d 1235, 1236 (Fed Cir. 1989); In re Bode 193 USPQ 12 (CCPA) 1976). In light of the foregoing discussion, the examiner concludes that the subject matter defined by the instant claims would have been obvious within the meaning of 35 USC 103. From the teachings of the references, it is apparent that one of ordinary skill in the art would have had a reasonable expectation of success in producing the claimed invention. Therefore, the invention as a whole was prima facie obvious to one of ordinary skill in the art at the time the invention was made, as evidenced by the references, especially in the absence of evidence to the contrary. Conclusion No claim is allowed. Correspondence Any inquiry concerning this communication or earlier communications from the examiner should be directed to Jonathan D. Mahlum whose telephone number is (703)756-4691. The examiner can normally be reached 8:30 AM - 5:00 PM ET, M-F. Examiner interviews are available via telephone, in-person, and video conferencing using a USPTO supplied web-based collaboration tool. To schedule an interview, applicant is encouraged to use the USPTO Automated Interview Request (AIR) at http://www.uspto.gov/interviewpractice. If attempts to reach the examiner by telephone are unsuccessful, the examiner’s supervisor, Andrew Kosar can be reached at (571) 272-0913. The fax phone number for the organization where this application or proceeding is assigned is 571-273-8300. Information regarding the status of published or unpublished applications may be obtained from Patent Center. Unpublished application information in Patent Center is available to registered users. To file and manage patent submissions in Patent Center, visit: https://patentcenter.uspto.gov. Visit https://www.uspto.gov/patents/apply/patent-center for more information about Patent Center and https://www.uspto.gov/patents/docx for information about filing in DOCX format. For additional questions, contact the Electronic Business Center (EBC) at 866-217-9197 (toll-free). If you would like assistance from a USPTO Customer Service Representative, call 800-786-9199 (IN USA OR CANADA) or 571-272-1000. /J.D.M./Examiner, Art Unit 1625 /Andrew D Kosar/Supervisory Patent Examiner, Art Unit 1625
Read full office action

Prosecution Timeline

Jan 18, 2023
Application Filed
Feb 03, 2026
Non-Final Rejection — §103, §112 (current)

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Study what changed to get past this examiner. Based on 5 most recent grants.

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Prosecution Projections

1-2
Expected OA Rounds
54%
Grant Probability
71%
With Interview (+16.7%)
3y 9m
Median Time to Grant
Low
PTA Risk
Based on 22 resolved cases by this examiner. Grant probability derived from career allow rate.

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