Prosecution Insights
Last updated: April 19, 2026
Application No. 18/076,274

NOVEL IMIDAZOPYRAZINE DERIVATIVES

Non-Final OA §DP
Filed
Dec 06, 2022
Examiner
HSU, GRACE CHING
Art Unit
1627
Tech Center
1600 — Biotechnology & Organic Chemistry
Assignee
Hoffmann-La Roche, Inc.
OA Round
1 (Non-Final)
75%
Grant Probability
Favorable
1-2
OA Rounds
3y 1m
To Grant
99%
With Interview

Examiner Intelligence

Grants 75% — above average
75%
Career Allow Rate
27 granted / 36 resolved
+15.0% vs TC avg
Strong +27% interview lift
Without
With
+27.3%
Interview Lift
resolved cases with interview
Typical timeline
3y 1m
Avg Prosecution
26 currently pending
Career history
62
Total Applications
across all art units

Statute-Specific Performance

§101
1.9%
-38.1% vs TC avg
§103
18.2%
-21.8% vs TC avg
§102
18.2%
-21.8% vs TC avg
§112
42.2%
+2.2% vs TC avg
Black line = Tech Center average estimate • Based on career data from 36 resolved cases

Office Action

§DP
DETAILED ACTION 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 The present office action is in responsive to February 22, 2024 Preliminary Amendment Remarks and Comments and corresponding miscellaneous documents. Claims 1, 3-14, 16-20, 23 and 30 are pending, claim 4 is currently amended, claims 20 and 30 are withdrawn for being directed to non-elected inventions and claims 2, 15, 21-22, 24-29 and 31-34 are cancelled in the above-identified application. Priority U.S. Pat. Appln. Ser. No.: 18076274, Filed: December 6, 2022 is a continuation of WO 2021/249896 A1 (i.e., PCT/EP2021/065088, Intern.’l Filing Date: June 7, 2021; Intern.’l Pub. Date: December 16, 2021), which claims foreign priority to WO 2021/017600 (i.e., PCT/CN2020/095147, Filing Date: June 9, 2020) Information Disclosure Statement Two (2) Information Disclosure Statements (IDS) submitted on June 5, 2024 and October 8, 2025 and are in compliance with the provisions of 37 CFR 1.97. Accordingly, Information Disclosure Statements have been considered by the Examiner. Election/Restriction Applicant’s election without traverse is acknowledged of: [A] Group I: Claims 1, 3-14, 16-19 drawn to compounds of Formula (I) or a pharmaceutically acceptable salt thereof; and Claim 23 drawn to a pharmaceutical compositions comprising compounds of claim 1 or a pharmaceutically acceptable salt thereof and a therapeutically inert carrier; resp., classified in multiple classes/subclasses (inc.,C07D489/00+, etc.); [B] Species Election: Compound 35 PNG media_image1.png 233 333 media_image1.png Greyscale Because Applicants did not distinctly and specifically point out the supposed errors in the species restriction requirement, the election has been treated as an election without traverse (MPEP § 818.01(a)). [C] Claims 1,3-14,16-19 and 23 read on the elected invention. [D] The following claims are withdrawn from further consideration pursuant to 37 CFR 1.142(b), for being drawn to a nonelected inventions, there being no allowable generic or linking claim: Claim 20 is directed to a process for manufacturing the compounds of formula (I); and Claim 30 method for treatment or prevention of infections with resulting diseases caused by ESKAPE group of bacteria (i.e., Enterococcus faecium, Staphylococcus aureus, Klebsiella pneumoniae, Acinetobacter baumannii, Pseudomonas aeruginosa, Enterobacter species or E. coli, or a combination thereof). Therefore this restriction is considered proper and thus made FINAL. Based on the above, the requirement is still deemed proper and is therefore made FINAL Elected Species and Broad Expanded Search A comprehensive search of the patent and non-patent literature was conducted for: elected species Compound 35 identified supra; and that species election of compound 35 was withdrawn; followed by an expanded broad genus scope directed to a compound of Formula (I) or pharmaceutically acceptable salts thereof, i.e. which encompasses the elected species and other species therein. The species compound 35 has been identified in the WO 2021/249896 A1, part of the same patent family associated with U.S. Pat. Pub. 2023/0141600, which corresponds to U.S. Appln. Ser. No. 18/076, 274 to Hoffman-La Roche, Inc. being examiner ; i.e., which is the current patent application now examined. Search of expanded to encompass broad scope of Formula (I) or pharmaceutically acceptable salts thereof, which identified several of Applicants’ patent applications related to the instant patent application under examination identified by relevant overlapping genus, subgenus and/or compound species encompassed by generic or broad scope of Formula (I). See Citation of Prior Art before Conclusion Section (i.e., 3rd party patent literature identified related compounds that are distinguished from those compounds of the present invention due to functional group substituents on positions in the instant application that are not substituted). No prior art was found in the patent and non-patent literature Upon above-identified expanded search, prior art was found (i.e., see Citation of Pertinent Prior Art Section herein) Non-Statutory Double Patenting The nonstatutory double patenting rejection is based on a judicially created doctrine grounded in public policy (a policy reflected in the statute) so as to prevent the unjustified or improper timewise extension of the “right to exclude” granted by a patent and to prevent possible harassment by multiple assignees. A nonstatutory double patenting rejection is appropriate where the conflicting claims are not identical, but at least one examined application claim is not patentably distinct from the reference claim(s) because the examined application claim is either anticipated by, or would have been obvious over, the reference claim(s). See, e.g., In re Berg, 140 F.3d 1428, 46 USPQ2d 1226 (Fed. Cir. 1998); In re Goodman, 11 F.3d 1046, 29 USPQ2d 2010 (Fed. Cir. 1993); In re Longi, 759 F.2d 887, 225 USPQ 645 (Fed. Cir. 1985); In re Van Ornum, 686 F.2d 937, 214 USPQ 761 (CCPA 1982); In re Vogel, 422 F.2d 438, 164 USPQ 619 (CCPA 1970); In re Thorington, 418 F.2d 528, 163 USPQ 644 (CCPA 1969). A timely filed terminal disclaimer in compliance with 37 CFR 1.321(c) or 1.321(d) may be used to overcome an actual or provisional rejection based on nonstatutory double patenting provided the reference application or patent either is shown to be commonly owned with the examined application, or claims an invention made as a result of activities undertaken within the scope of a joint research agreement. See MPEP § 717.02 for applications subject to examination under the first inventor to file provisions of the AIA as explained in MPEP § 2159. See MPEP § 2146 et seq. for applications not subject to examination under the first inventor to file provisions of the AIA . A terminal disclaimer must be signed in compliance with 37 CFR 1.321(b). Effective January 1, 1994, a registered attorney or agent of record may sign a terminal disclaimer. A terminal disclaimer signed by the assignee must fully comply with 37 CFR 3.73(b). The USPTO Internet website contains terminal disclaimer forms which may be used. Please visit www.uspto.gov/patent/patents-forms. The filing date of the application in which the form is filed determines what form (e.g., PTO/SB/25, PTO/SB/26, PTO/AIA /25, or PTO/AIA /26) should be used. A web-based eTerminal Disclaimer may be filled out completely online using web-screens. An eTerminal Disclaimer that meets all requirements is auto-processed and approved immediately upon submission. For more information about eTerminal Disclaimers, refer to www.uspto.gov/patents/process/file/efs/guidance/eTD-info-I.jsp. Effective January 1, 1994, a registered attorney or agent of record may sign a terminal disclaimer. A terminal disclaimer signed by the assignee must fully comply with 37 CFR 3.73(b). [A] Claims 1, 3-14, 16-19 and 23 of the Present Invention In particular, claims 1, 3-14, 16-19 and 23 are directed to a compound of formula (I) or pharmaceutically acceptable salt thereof or corresponding pharmaceutical compositions thereof; where the claim 1 is defined as follows: PNG media_image2.png 23 1 media_image2.png Greyscale [AltContent: textbox ()] PNG media_image3.png 1 3 media_image3.png Greyscale PNG media_image4.png 91 115 media_image4.png Greyscale PNG media_image5.png 18 499 media_image5.png Greyscale PNG media_image5.png 18 499 media_image5.png Greyscale PNG media_image5.png 18 499 media_image5.png Greyscale PNG media_image6.png 1 129 media_image6.png Greyscale PNG media_image6.png 1 129 media_image6.png Greyscale PNG media_image6.png 1 129 media_image6.png Greyscale [B] Provisional Nonstatutory Obviousness-Type Double Patenting Rejections [1] Claims 1,13-14,16-19 and 23 are provisionally rejected under the judicially created doctrine of nonstatutory obvious-type double patenting as being unpatentable over claims 1,3-6, 8-10,12-13,15, 51,54-58 and 61 of co-pending U.S. Appln. Ser. No. 17/976,651 (i.e., corresponds to US Pat. Pub.: 2023/0203043A1 Filing Date: October 28, 2022; “U.S. ‘651 Appln.") In particular, Claim 1 and corresponding dependent claims 3-6, 8-10,12-13,15, 51,54-58 and 61 of U.S. ‘651 Appln are directed to a compound of Formula (I): PNG media_image7.png 4 57 media_image7.png Greyscale PNG media_image7.png 4 57 media_image7.png Greyscale ; Although the conflicting claims are not identical, they are not patentably distinct from each other because: claims of the instant application directed to a broader genus of compounds of formula (I), and claims of U.S. ‘651 Appln., respectively contain overlapping key variables with corresponding functional groups as shown below (i.e., where it is clear that overlapping compound scope exemplifies double patenting between the claims of the instant and US ‘651 Appln.); claimed compounds of the US ‘651 Appln. read on the broader genus of Formula (I) of the instant invention or the broader claimed genus of Formula (I) of the instant invention encompasses the narrower compound scope of the US ‘‘651 Appln. PRESENT INVENTION US PAT. APPLN. 17/976,651 Claims 1,13-14,16-19 and 23 Compound Formula Correlations Claims 1,3-6, 8-10,12-13,15, 51,54-58 and 61 PNG media_image2.png 23 1 media_image2.png Greyscale (I) PNG media_image7.png 4 57 media_image7.png Greyscale (I) The moiety PNG media_image8.png 57 30 media_image8.png Greyscale attached to the phenyl group of the instant invention, where a Rx = PNG media_image3.png 1 3 media_image3.png Greyscale (i.e., RxC(O) = X) encompasses the corresponding moiety PNG media_image7.png 4 57 media_image7.png Greyscale PNG media_image7.png 4 57 media_image7.png Greyscale attached to phenyl group therein of the U.S. ‘651 Appln The R3 and R5 functional groups are attached to the phenyl moiety PNG media_image8.png 57 30 media_image8.png Greyscale i.e., where R3 and R5 of the instant application corresponds to R3 and R9 and R4 and R8 = hydrogen attached to the phenyl moiety PNG media_image7.png 4 57 media_image7.png Greyscale of U.S. ‘651 Appln that is substituted with X is as defined above and R3 and R9 and R4 and R8 = hydrogen The 1R6,3R5,5R7substituted pyrazole R4 moiety as attached to this group PNG media_image2.png 23 1 media_image2.png Greyscale , where PNG media_image3.png 1 3 media_image3.png Greyscale (i.e., R4 = 1,3,5 substituted pyrazole) and corresponds to the 1R6,3R5,5R7substituted pyrazole PNG media_image7.png 4 57 media_image7.png Greyscale of the U.S. ‘651 Appln PNG media_image9.png 303 745 media_image9.png Greyscale PNG media_image10.png 66 702 media_image10.png Greyscale Below is a schematic chart visually showing how each of the functional groups between the claimed invention and the US ‘561 Appln. correlated with each other: PNG media_image11.png 750 1003 media_image11.png Greyscale [2] Claims 1,13-14, 16-19 and 23 are provisionally rejected on the ground of nonstatutory double patenting as being unpatentable over claims 1-8,10,12, 14, 19, 21-25 and 29 of co-pending U.S. Appln. Ser. No. 18/076,383 (i.e., corresponds to U.S. Pat. Pub. 2023/0141403 A1 Filing Date: December 6, 2022; U.S. ‘383 Appln.) PNG media_image12.png 180 174 media_image12.png Greyscale Claims of the U.S. ‘383 recites compounds of formula (I) thereof or a pharmaceutically acceptable salt thereof and corresponding pharmaceutical compositions as defined as shown: where: X = carbonyl, R1 = PNG media_image13.png 118 126 media_image13.png Greyscale A is selected from the group consisting of 3- to 14-membered heterocyclyl, 5- to 14- membered heteroaryl, C6-C14-aryl, and C3-C10-cycloalkyl; L1 = covalent bond R2, R3, R7, R8 and R9 definitions overlap with those of claimed invention; m = 1 and n = 1,2 or 3 Although the conflicting claims are not identical, they are not patentably distinct from each other because: claims of the instant application are directed to a broader genus of compounds of formula (I) of the present invention, while claimed compounds of formula (I) of U.S. ‘.383 Appln., respectively, which have corresponding and overlapping functional group scope as defined by key variables and functional groups as discussed and shown. Claimed compounds of the US ‘383 Appln. read on the broader genus of Formula (I) of the instant invention or the broader claimed genus of Formula (I) of the instant invention encompasses the narrower compound scope of the US ‘383 Appln Formula (I) of Present Invention Formula (I) or US ‘383 Appln Claims 1,13-14, 16-19 and 23 claims 1-8,10,12, 14, 19, 21-25 and 29 PNG media_image2.png 23 1 media_image2.png Greyscale Compound Formula Correlations PNG media_image12.png 180 174 media_image12.png Greyscale The PNG media_image8.png 57 30 media_image8.png Greyscale moiety, Rx = PNG media_image3.png 1 3 media_image3.png Greyscale attached to phenyl group of Formula (I) of the instant invention (i.e., RxC(O) = R1-X- = R1C(O) which encompasses the group PNG media_image14.png 37 48 media_image14.png Greyscale attached to the phenyl group, where R1 is defined as PNG media_image15.png 72 299 media_image15.png Greyscale and PNG media_image16.png 266 302 media_image16.png Greyscale R3 and R5 substituents on the PNG media_image8.png 57 30 media_image8.png Greyscale of the instant invention (i.e.,R3 and R5 = (R2)m) encompasses the corresponding phenyl group substituted with (R2)m, where R2 is defined as PNG media_image17.png 83 380 media_image17.png Greyscale and m = 1 to 4 as shown by o PNG media_image14.png 37 48 media_image14.png Greyscale of the US ‘383 Appln; and The R4 group attached to the imidazo(1,2-a)pyrazine PNG media_image2.png 23 1 media_image2.png Greyscale moiety, is defined as PNG media_image3.png 1 3 media_image3.png Greyscale of the instant invention , where F is C6-C10-aryl substituted with R23, R24 or R25 (i.e., R4 = phenyl substituted with (R3)n), which encompasses the phenyl substituted imidazo(1,2-a)pyrazine PNG media_image12.png 180 174 media_image12.png Greyscale of the US ’383 Appln (i.e., where PNG media_image18.png 91 380 media_image18.png Greyscale . Below is a schematic chart visually showing how each of the functional groups between the claimed invention and the US ‘383 Appln. correlated with each other: PNG media_image19.png 656 1198 media_image19.png Greyscale In AbbVie Inc. v. Kennedy Institute of Rheumatology Trust, 764 F.3d 1366, 112 USPQ2d 1001 (Fed. Cir. 2014), the court explained that it is also proper to look at the disclosed utility in the reference disclosure to determine the overall question of obviousness in a non-statutory double patenting context. See also Pfizer, Inc. v. Teva Pharm. USA, Inc., 518 F.3d 1353, 86 USPQ2d 1001 (Fed. Cir. 2008);Geneva Pharmaceuticals Inc. v. GlaxoSmithKline PLC, 349 F3d 1373, 1385-86, 68 USPQ2d 1865, 1875 (Fed. Cir. 2003). However, one skilled in the art would recognize that the claims of U.S. ‘383 Appln One having ordinary skill in the art at the time of the invention would have noted that subject matter exists in both the instant invention and the co-pending applications that is not patentably distinct from each other. It has also been held that a prior art disclosed genus of useful compounds is sufficient to render prima facie obvious a species falling within a genus. In re Susi, 440 F.2d 442, 169 USPQ 423, 425 (CCPA 1971), followed by the Federal Circuit in Merck & Co. v. Biocraft Laboratories, 847 F.2d 804, 10 USPQ 2d 1843, 1846 (Fed. Cir. 1989). Appropriate action is required accordingly. Citation of Pertinent Prior Art The prior art made of record and not relied upon is considered pertinent to applicant's disclosure, because: The references cited below represent close prior art that teach unsubstituted Rx (= B = 3 to 14 membered heterocycle) and unsubstituted R4 (= F= 5 to 14 membered heteroaryl) variable or functional groups, which is distinguished from compounds of the instant invention have substituted Rx and R4 functional group variables at the same positions: PNG media_image20.png 24 54 media_image20.png Greyscale PNG media_image21.png 106 314 media_image21.png Greyscale and PNG media_image22.png 107 171 media_image22.png Greyscale Zeng et al., Bioorg. & Med. Chem. Lett. (2011), 21-5875: PNG media_image23.png 262 810 media_image23.png Greyscale Thakur et al., India Biochem. and Biophys. Res. Comm. (2017), 482 (4), 1289-1295: PNG media_image24.png 191 446 media_image24.png Greyscale PNG media_image25.png 67 853 media_image25.png Greyscale CONCLUSION Any inquiry concerning this communication or earlier communications from the Examiner should be directed to GRACE C HSU whose telephone number is (571) 270-1689. The Examiner can normally be reached Monday-Friday 7:30 am - 6 pm. Examiner interviews are available via telephone, in-person, and video conferencing using a USPTO supplied web-based collaboration tool. To schedule an interview, Applicants 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 L. KLINKEL can be reached on 571-270-5239. 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. /G.C.H./ Examiner, Art Unit 1627 /Kortney L. Klinkel/Supervisory Patent Examiner, Art Unit 1627
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Prosecution Timeline

Dec 06, 2022
Application Filed
Mar 07, 2026
Non-Final Rejection — §DP (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
75%
Grant Probability
99%
With Interview (+27.3%)
3y 1m
Median Time to Grant
Low
PTA Risk
Based on 36 resolved cases by this examiner. Grant probability derived from career allow rate.

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