Prosecution Insights
Last updated: April 19, 2026
Application No. 17/616,930

ALTERNATIVE PROCESS FOR THE PREPARATION OF 4-PHENYL-5-ALKOXYCARBONYL-2-THIAZOL-2-YL-1,4-DIHYDROPYRIMIDIN-6-YL]METHYL]-3-OXO-5,6,8,8A-TETRAHYDRO-1H-IMIDAZO[1,5-A]PYRAZIN-2-YL]-CARBOXYLIC ACID

Final Rejection §102§103§112
Filed
Dec 06, 2021
Examiner
WILSON, JERICA KATLYNN
Art Unit
1621
Tech Center
1600 — Biotechnology & Organic Chemistry
Assignee
Hoffmann-La Roche, Inc.
OA Round
2 (Final)
61%
Grant Probability
Moderate
3-4
OA Rounds
3y 3m
To Grant
99%
With Interview

Examiner Intelligence

Grants 61% of resolved cases
61%
Career Allow Rate
57 granted / 94 resolved
+0.6% vs TC avg
Strong +40% interview lift
Without
With
+39.5%
Interview Lift
resolved cases with interview
Typical timeline
3y 3m
Avg Prosecution
39 currently pending
Career history
133
Total Applications
across all art units

Statute-Specific Performance

§101
1.8%
-38.2% vs TC avg
§103
34.4%
-5.6% vs TC avg
§102
18.6%
-21.4% vs TC avg
§112
27.4%
-12.6% vs TC avg
Black line = Tech Center average estimate • Based on career data from 94 resolved cases

Office Action

§102 §103 §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 1-29 are pending in the instant application. Claims 1-29 are examined herein. Priority The instant application claims benefit of foreign priority to PCTCN2019090258, filed on 06 June 2019, and the benefit of priority to PCT/ep2020/065424, filed on 04 June 2020. The claims to the benefit of priority are acknowledged. As such, the effective filing date of the claims is 06 June 2019. Information Disclosure Statement No information disclosure statement (IDS) submitted by applicant. 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. Claims 1-29 are 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. Claims 1 and 4 recite the compound of formula (I) as having the structure pictured below. The subsequent preparation steps contain an extra CH2 group between R3 and the hydantoin (circled in pictures below). It is unclear whether Formula (I) is missing the CH2 group, or Formulas (III), (V), (VI), (VIII), (IX), and (X) contain an extra CH2 group, or there is an unrecited elimination step. The dependent claims 2, 3, and 5-29 do not resolve the issue and are therefore subject to the rejection as well. To overcome the rejection Applicant is advised to amend Formula (I) to include the CH2 group or amend Formulas (III), (V), (VI), (VIII), (IX), and (X) to eliminate the extra CH2 group. For examination purposes, the claims have been interpreted based on Formula (I), i.e. Formulas (III), (V), (VI), (VIII), (IX), and (X) are interpreted without the extra CH2 group between the hydantoin and R3 substituent. PNG media_image1.png 108 238 media_image1.png Greyscale PNG media_image2.png 92 198 media_image2.png Greyscale PNG media_image3.png 264 206 media_image3.png Greyscale PNG media_image4.png 156 210 media_image4.png Greyscale PNG media_image5.png 154 214 media_image5.png Greyscale PNG media_image6.png 148 208 media_image6.png Greyscale PNG media_image7.png 140 174 media_image7.png Greyscale Claims 1-29 are 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. Claims 1 and 4 recite the “process comprising ‘one or more’ of the following steps.” The phrase “one or more” renders the claims indefinite as the bounds of the claims are unclear. Any synthetic scheme that shares one process step with the instant invention could be considered infringing, even if the yielded products are different. The dependent claims 2, 3, and 5-29 do not resolve the issue and are therefore subject to the rejection as well. To overcome the rejection Applicant is advised to amend the claim language in a manner that clearly expresses all the steps are required in the process. For examining purposes, and as seen in the rejections below, the claim language has been interpreted to mean that only one step of the process is necessary to be considered an overlap in invention. Claim Rejections - 35 USC § 102 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 the appropriate paragraphs of 35 U.S.C. 102 that form the basis for the rejections under this section made in this Office action: A person shall be entitled to a patent unless – (a)(1) the claimed invention was patented, described in a printed publication, or in public use, on sale, or otherwise available to the public before the effective filing date of the claimed invention. Claim(s) 1-6 and 27 is/are rejected under 35 U.S.C. 102(a)(1) as being anticipated by Guo et al (WO2015132276A1). Regarding claims 1 and 4, Guo discloses synthetic steps for compounds of the instant Formula (I). Example 19 (page 83) discloses the reaction of V → Q corresponding with the instant steps e), f), and g) in the formation of the instant formula X. Scheme 2 (page 63) discloses the reactions B1 → C → 1 (pictured below) which corresponds to the instant steps k) and l). PNG media_image8.png 154 270 media_image8.png Greyscale PNG media_image9.png 176 524 media_image9.png Greyscale Regarding claim 2 and 5, Guo discloses the position corresponding to the instant R1 is chlorofluorophenyl, the position corresponding to the instant R2 is methyl, and the position corresponding to the instant R3 is dimethylethyl as seen in preferred embodiment 42 (pictured below). PNG media_image10.png 256 168 media_image10.png Greyscale Regarding claim 3, Guo discloses preferred embodiment 42 which corresponds to the instant compound of claim 3. Regarding claim 6, Guo discloses compound Q (corresponding to the instant formula X) as a salt (page82). Regarding claim 27, Guo discloses the reaction to yield compound Q is performed in THF (page 84, line 16). Claim(s) 1-6, 12-16, and 25-29 is/are rejected under 35 U.S.C. 102(a)(1) as being anticipated by Chen (WO2017140750A1). Regarding claims 1 and 4, Chen discloses synthetic steps for compounds of the instant Formula (I). Scheme 1 (page 6) shows reaction steps for VII → VIII → IX → X, corresponding to the instant steps d), e), f), and g). Scheme 2 (page 7) shows reaction steps for XVII → XVIII → I, corresponding to the instant steps l) and m). PNG media_image11.png 180 310 media_image11.png Greyscale PNG media_image12.png 182 354 media_image12.png Greyscale PNG media_image13.png 114 286 media_image13.png Greyscale PNG media_image14.png 174 190 media_image14.png Greyscale Regarding claim 2 and 5, Chen discloses R1 is phenyl optionally substituted with 1-3 halogen or C1-6- -alkyl substituents, R2 is C1-6- -alkyl, and R3 is CxH2x where x is 1, 2, 3, 4, 5, 6, or 7. Regarding claim 3, Chen discloses example 10 (page 30) and example 13 (page 35), pictured below, respectively. PNG media_image15.png 250 138 media_image15.png Greyscale PNG media_image16.png 262 226 media_image16.png Greyscale Regarding claim 6, Chen discloses compound X as a hydrochloride salt (page 27). Regarding claims 12, 13, 25 and 26, Chen discloses the formation of a compound of formula VIII was performed in the presence of a Lewis acid and a reducing agent, wherein the Lewis acid is BF3 · Et2O, and the reducing agent is borane (page 25, line 6). Regarding claims 14 and 27, Chen discloses the formation of a compound of formula IX was performed in the presence of methanol mixed with water (page 26, line 6). Regarding claims 15, 16, 28 and 29, Chen discloses the formation of a compound of formula X in the presence of HCl in a solvent, where the solvent is MIBK (page 27, line 6). 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) 1-6 and 27 is/are rejected under 35 U.S.C. 103 as being unpatentable over Guo et al. (cited above) The teachings of Guo are disclosed above and incorporated by reference herein. Regarding claim 3, Guo teaches the second recited compound as example 42, but does not teach the first recited compound (pictured below). PNG media_image17.png 338 412 media_image17.png Greyscale Guo does teach preferred embodiment 44 (pictured below). The difference between the first recited compound of claim 3 and Guo’s example 44 is the instant compound is an ethyl ester, example 44 is a methyl ester. Example 44 is a species of Guo’s formula (ID) (below) where R4 is a C1-6 alkyl. It would be prima facie obvious to one of ordinary skill in the art to modify example 44 to the first recited instant compound of claim 3 as the genus presented by Guo encompasses both the methyl and ethyl ester. PNG media_image18.png 268 154 media_image18.png Greyscale Conclusion Claims 1-29 are rejected. 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. 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, Clinton Brooks can be reached on (571)270-7682. 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.K.W./Examiner, Art Unit 1621 /BRANDON J FETTEROLF/Supervisory Patent Examiner, Art Unit 1600
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Prosecution Timeline

Dec 06, 2021
Application Filed
Mar 26, 2025
Non-Final Rejection — §102, §103, §112
Aug 26, 2025
Response Filed
Dec 12, 2025
Final Rejection — §102, §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

3-4
Expected OA Rounds
61%
Grant Probability
99%
With Interview (+39.5%)
3y 3m
Median Time to Grant
Moderate
PTA Risk
Based on 94 resolved cases by this examiner. Grant probability derived from career allow rate.

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