Prosecution Insights
Last updated: April 19, 2026
Application No. 17/800,049

HETEROCYCLIC DERIVATIVES AS TRMP8 ANTAGONISTS

Final Rejection §103
Filed
Aug 16, 2022
Examiner
CHANDRAKUMAR, NIZAL S
Art Unit
1625
Tech Center
1600 — Biotechnology & Organic Chemistry
Assignee
Givaudan SA
OA Round
2 (Final)
73%
Grant Probability
Favorable
3-4
OA Rounds
2y 4m
To Grant
91%
With Interview

Examiner Intelligence

Grants 73% — above average
73%
Career Allow Rate
1273 granted / 1752 resolved
+12.7% vs TC avg
Strong +18% interview lift
Without
With
+17.9%
Interview Lift
resolved cases with interview
Typical timeline
2y 4m
Avg Prosecution
76 currently pending
Career history
1828
Total Applications
across all art units

Statute-Specific Performance

§101
1.1%
-38.9% vs TC avg
§103
30.0%
-10.0% vs TC avg
§102
12.0%
-28.0% vs TC avg
§112
35.3%
-4.7% vs TC avg
Black line = Tech Center average estimate • Based on career data from 1752 resolved cases

Office Action

§103
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 1-20 are currently pending. Claims 1-6, 12-14, and 19-20 are withdrawn from consideration. Amended claims 7-11 and 15-18 are under Examination. In view of amendments to claims previously presented obviousness rejection is reformatted. Claim Rejections - 35 USC § 103 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. claims 7-11 and 15-18 is/are rejected under 35 U.S.C. 103 as being unpatentable over Kindler US 2831859, Meki, teach US 4837236, Yoshida WO 9013539, Giblin WO2006066968, Jones WO2006067587, Bit WO2006114272 and Kilbourn Nucl. Med. Biol. Vol. 16, No. 7, pp. 681-686, 1989 for reasons of record. See previously action pictured compounds of Kindler, Meki, Yoshida. Giblin, WO2006066968 RN 892663-84-2 PNG media_image1.png 274 428 media_image1.png Greyscale Jones, WO 2006067587 RN 895572-81-3 PNG media_image2.png 273 413 media_image2.png Greyscale B = phenyl R11= halogen, CN; A= phenyl, W= O, R3 =H, m =0, R4 together makes CO, V= N and Z= CH2 Bit, WO 2006114272 RN 913957-36-5 PNG media_image3.png 268 445 media_image3.png Greyscale A = phenyl R1 = H B = furan R11= C(O))C2H5, X= CH2; A= phenyl, W= O, R3 =H, m =0,; p=1. R4 = H makes CO, V= CH and Z= CHR12 R12= H. Applicant argues, that Kindler, Meki, Yoshida references (and the new Giblin, Jones and Bit references do not teach TRPM8 activity). More on this later. The difference between the compounds of Kindler, Meki, Yoshida references and the new Giblin, Jones and Bit references are in the substituents decorating the periphery of the rings, A , B and V containing rings. ((Note in the previous action page 3 with regards to thiophene compounds, it is Kindler (not Werner)) The position taken by the Examiner as noted previously is that the included and excluded substituents are obvious variants of each other. For example, as instantly amended, thiophene is excluded while heterocycles furan and pyridine are included. These heterocycles are obvious variants of each and are suggestive of each other. Previously noted Kilbourn reference with respect to the position taken (conveniently ignored by the Applicant) is now included in the rejection statement. Kilbourn was conveniently ignored by the applicant. Applicant’s compound (claim 9) 1-methyl-4-(2-(4-methyl-2-(thiophen-2-ylmethyl)phenoxy)ethyl)piperazine is replacement of above phenyl group of (benzyl) with a thienyl group. Such isosteric modifications (see Kilbourn Nucl. Med. Biol. Vol. 16, No. 7, pp. 681-686, 1989) are elementary ideas in medicinal chemistry art. Decorating known structural templates with substituents is routinely used in medicinal chemistry for optimization of desired properties to arrive at alternate versions of prior art compounds. The invention is a selective combination of the inventions by the prior arts done in a manner obvious to one of ordinary skill in the art.. There is no indication in the prior arts that such combination would lead one of ordinary skill in the art to doubt that the combination could not be made. Obviousness can be established by combining or modifying the teachings of the prior art to produce the claimed invention where there is some teaching, suggestion, or motivation to do so found either in the references themselves or in the knowledge generally available to one of ordinary skill in the art. Applicants arguments focus on the Amendments to claims (for example the above noted deletion possibility for thiophene) and the absence of teaching with respect to TRPM8 activity in the cited references. Cited compounds are biologically active though not all the inherent properties of these compounds are appreciated in the cited references for these. Disclosure in the specification does not include any comparative study. Further, of the compounds tested at page 130 Table, it is unclear what substituents (that are not obvious variants) provide for predictable TRPM8 activity argued by the Applicant. In addition it is unclear if the possibilities for Y (second and third structures or R1 and R3 making ring, if buried in the said Table) have any TRPM8 activity. The position taken is that the properties of compounds is inherent. In this context it is noted that as per MPEP 2112 Requirements of Rejection Based on Inherency; Burden of Proof [R-10.2019], "[T]he discovery of a previously unappreciated property of a prior art composition, or of a scientific explanation for the prior art’s functioning, does not render the old composition patentably new to the discoverer." As such Applicants arguments are not persuasive. The prior art made of record and not relied upon is considered pertinent to applicant's disclosure. US 20130245068 see Column A page 1. 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. Any inquiry concerning this communication or earlier communications from the examiner should be directed to NIZAL S CHANDRAKUMAR whose telephone number is (571)272-6202. The examiner can normally be reached M-F 8-5 EST. 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 on (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. /NIZAL S CHANDRAKUMAR/Primary Examiner, Art Unit 1625
Read full office action

Prosecution Timeline

Aug 16, 2022
Application Filed
Aug 10, 2025
Non-Final Rejection — §103
Dec 10, 2025
Response Filed
Feb 02, 2026
Examiner Interview (Telephonic)
Feb 02, 2026
Examiner Interview Summary
Feb 08, 2026
Final Rejection — §103 (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

3-4
Expected OA Rounds
73%
Grant Probability
91%
With Interview (+17.9%)
2y 4m
Median Time to Grant
Moderate
PTA Risk
Based on 1752 resolved cases by this examiner. Grant probability derived from career allow rate.

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