Prosecution Insights
Last updated: April 19, 2026
Application No. 18/546,116

MACROCYCLIC 1,3-BRIDGED 6-CHLORO-7-PYRAZOL-4-YL-1 H-INDOLE-2-CARBOXYLATE AND 6-CHLORO-7-PYRIMIDIN-5-YL-1H-INDOLE-2-CARBOXYLATE DERIVATIVES AS MCL-1 INHIBITORS FOR THE TREATMENT OF CANCER

Non-Final OA §112
Filed
Aug 11, 2023
Examiner
PECKHAM, RICHARD GRANT
Art Unit
1627
Tech Center
1600 — Biotechnology & Organic Chemistry
Assignee
Janssen Pharmaceutica NV
OA Round
1 (Non-Final)
68%
Grant Probability
Favorable
1-2
OA Rounds
3y 3m
To Grant
99%
With Interview

Examiner Intelligence

Grants 68% — above average
68%
Career Allow Rate
80 granted / 117 resolved
+8.4% vs TC avg
Strong +35% interview lift
Without
With
+35.3%
Interview Lift
resolved cases with interview
Typical timeline
3y 3m
Avg Prosecution
42 currently pending
Career history
159
Total Applications
across all art units

Statute-Specific Performance

§101
3.3%
-36.7% vs TC avg
§103
28.4%
-11.6% vs TC avg
§102
14.2%
-25.8% vs TC avg
§112
29.3%
-10.7% vs TC avg
Black line = Tech Center average estimate • Based on career data from 117 resolved cases

Office Action

§112
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 1-11 and 15-16 are currently pending. Claim Objections Claims 10-11 and 15 are objected to because “a compound as claimed in [or according to] claim 1” should be amended to read “the compound…”. Appropriate correction is required. Claim Rejections - 35 USC § 112(a) The following is a quotation of the first paragraph of 35 U.S.C. 112(a): (a) IN GENERAL—The specification shall contain a written description of the invention, and of the manner and process of making and using it, in such full, clear, concise, and exact terms as to enable any person skilled in the art to which it pertains, or with which it is most nearly connected, to make and use the same, and shall set forth the best mode contemplated by the inventor or joint inventor of carrying out the invention. The following is a quotation of the first paragraph of pre-AIA 35 U.S.C. 112: The specification shall contain a written description of the invention, and of the manner and process of making and using it, in such full, clear, concise, and exact terms as to enable any person skilled in the art to which it pertains, or with which it is most nearly connected, to make and use the same, and shall set forth the best mode contemplated by the inventor of carrying out his invention. Claims 15-16 are rejected under 35 U.S.C. 112(a) or 35 U.S.C. 112 (pre-AIA ), first paragraph, because the specification, while being enabling for the treatment of MCL-1 associated cancers, does not reasonably provide enablement for non-MCL-1 associated cancer. The specification does not enable any person skilled in the art to which it pertains, or with which it is most nearly connected, to practice the invention commensurate in scope with these claims. In In re Wands, 8 USPQ2d 1400 (1988), factors to be considered in determining whether a disclosure meets the enablement requirement of 35 U.S.C. 112, first paragraph, have need described. They are: 1. the nature of the invention, 2. the state of the prior art, 3. the predictability or lack thereof in the art, 4. the amount of direction or guidance present, 5. the presence or absence of working examples, 6. the breadth of the claims, 7. the quantity of experimentation needed, and 8. the level of the skill in the art. The nature of the invention (1) and breadth of the claims (6) The nature of the invention and breadth of Claims 15-16 is the treatment of cancer comprising administering compounds of Formula (I). The state of the prior art (2) and the predictability or lack thereof in the art (3) Xiang (OncoTargets and Therapy, 2018, 7301-7314) teaches that only a limited amount of cancer is associated with MCL-1 dysregulation; “An analysis of 3,131 cancer specimens has revealed that 36% of breast cancer and 54% of lung cancer specimens exhibit elevated levels of MCL-1 expression” (Page 7301, Para 3). It is unclear how cancers as claimed or specific cancers listed in Claim 16 like lung cancer, which include non-MCL-1 associated forms, would be treated by the present compounds which are MCL-1 inhibitors. One would predict that such compounds would have no effect on the 46% of lung cancers or 64% of breast cancers not associated with MCL-1 levels. Applicant does not explicate how such cancers not associated with elevated MCL-1 would be expected to be treated with the claimed compounds. The amount of direction or guidance present (4) and the presence or absence of working examples (5) Applicant demonstrates anti-MCL-1 activity of the claimed compounds (Pages 116-120, Biological Example 2). However, it remains unclear how MCL-1 inhibition would inhibit non-MCL-1-associated cancers embraced by the scope of Claims 15-16. The quantity of experimentation needed (7) The quantity of experimentation needed is extremely difficult, novel, and undue experimentation; the ability of the compounds to treat non-MCL-1 associated cancers, encompassed by the broad genus of cancers, is nearly impossible to determine and not at all enabled by the experiments disclosed in the specifications of the application. The level of the skill in the art (8) The level of skill in the art is high, even among ordinary artisans. However, there is no expectation that MCL-1 inhibition would affect a disease wherein MCL-1 expression is dysregulated, regardless of the skill of the medical professional practicing the scope of the methods as claimed. Allowable Subject Matter The closest art is found in Zhang (US20220041623, cited in 2/08/2024 IDS). Zhang teaches a similar macrocycle to those taught in instant Formula (I) (left). Compound 1 of Zhang (Page 8) (right) differs from Formula (I) in that the alkylenes are attached to the heterobicycle at different points: PNG media_image1.png 313 389 media_image1.png Greyscale vs. PNG media_image2.png 298 298 media_image2.png Greyscale . Zhang does not teach variability in the macrocyclic core at said points of attachment. Further, it is not obvious to form a constitutional isomer of the Zhang compound to yield one of instant Formula (I) because Zhang does not speak to—nor does the art provide guidance regarding—different synthetic routes and kinetics, variable degrees of freedom within the macrocycle, or MCL-1 inhibition potential or activity in vitro or in vivo. Conclusion Claims 1-9 are allowable. Claims 10-11 and 15 are objected to. Claims 15-16 are rejected. Inquiries Any inquiry concerning this communication or earlier communications from the examiner should be directed to Richard G. Peckham whose telephone number is (703)756-4621. The examiner can normally be reached 8:30am - 4:30pm 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, Kortney Klinkel can be reached on (571) 270-5239. 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. /RICHARD GRANT PECKHAM/Examiner, Art Unit 1627 /Kortney L. Klinkel/Supervisory Patent Examiner, Art Unit 1627
Read full office action

Prosecution Timeline

Aug 11, 2023
Application Filed
Jan 27, 2026
Non-Final Rejection — §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
68%
Grant Probability
99%
With Interview (+35.3%)
3y 3m
Median Time to Grant
Low
PTA Risk
Based on 117 resolved cases by this examiner. Grant probability derived from career allow rate.

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