Prosecution Insights
Last updated: April 19, 2026
Application No. 18/390,137

INHIBITORS OF PLASMA KALLIKREIN AND USES THEREOF

Non-Final OA §DP
Filed
Dec 20, 2023
Examiner
CARCANAGUE, DANIEL R
Art Unit
1621
Tech Center
1600 — Biotechnology & Organic Chemistry
Assignee
Takeda Pharmaceutical Company Limited
OA Round
1 (Non-Final)
81%
Grant Probability
Favorable
1-2
OA Rounds
1y 11m
To Grant
99%
With Interview

Examiner Intelligence

Grants 81% — above average
81%
Career Allow Rate
753 granted / 931 resolved
+20.9% vs TC avg
Strong +24% interview lift
Without
With
+24.3%
Interview Lift
resolved cases with interview
Fast prosecutor
1y 11m
Avg Prosecution
8 currently pending
Career history
939
Total Applications
across all art units

Statute-Specific Performance

§101
1.1%
-38.9% vs TC avg
§103
23.0%
-17.0% vs TC avg
§102
24.4%
-15.6% vs TC avg
§112
31.4%
-8.6% vs TC avg
Black line = Tech Center average estimate • Based on career data from 931 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 . Non-Final Rejection Priority This application was filed 20 December 2023 and is a continuation of application 17/519,013 which was filed November 04, 2021, issued February 20, 2024 as US 11,905,285 and is a continuation of application 16/636,518 which was filed February 04, 2020, issued November 09, 2021 as US 11,168,083 and is a national stage filing under 35 U.S.C. § 371 of International PCT Application, PCT/US2018/045183, filed August 3, 2018, which claims priority to Provisional Application 62/541,403, filed August 4, 2017. Information Disclosure Statement The IDS dated 17 April 2024 has been received, entered and considered, a copy is included herein. PTO-892 Form References from the Examiner’s search of the invention are made of record. Patent application publications sharing inventor and/or applicant and describing subject matter related to that of the examined application are cited for completeness. Status of the claims Applicant’s preliminary claim amendment dated 17 April 2024 is acknowledged. Claims 1-2, 4-5, 7-8, 10, 12, 14-15, 19-20, 23, 26 and 35-40 are pending and are rejected. Claims 3, 6, 9, 11, 13, 16-18, 21-22, 24-25 and 27-34 were cancelled by the Applicant. Claims are Allowable over the Prior Art No prior art rejection of any of the pending claims is set forth herein. Independent claim 1 is drawn to a method of use of a compound, according to a generic Markush formula I, which requires a combination of features that is not disclosed, taught or suggested by the prior art of record. The closest prior art references to the claimed subject matter and the non-obvious differences therefrom are discussed below: Gardelli (J. Med. Chem. 2007, 50, 4953-4975, IDS) teaches a compound which arguably falls into the scope of the genus required by independent claim 1, see the non-final rejection dated 27 November 2020 in application 16/636,518 at pages 3-6. PNG media_image1.png 535 703 media_image1.png Greyscale Compound 89r, shown above, appears in scheme 5 on page 4961 and is described in the experimental part for compound 21 at page 4970. This compound is further converted to a target compound which differs substantially in structure from a compound required by the examined claims. The target compounds of Gardelli are taught as having utility in antiviral methods of use which are completely different from that of the examined claims and there is no reason provided by the reference or the prior art of record why any of the target compounds, much less any synthetic intermediates, would be used in a method as presently claimed. See also the intermediate compound 9v disclosed by Laurent (US20120009141, IDS) on page 39: PNG media_image2.png 423 359 media_image2.png Greyscale The compound lacks the required –C(O)-NH-R3 moiety attached to A but has instead a methyl-substituted variant –C(O)N(CH3)OCH3. Modification of the US20120009141 compound 9v or the Gardelli (J. Med. Chem. 2007, 50, 4953-4975) intermediates cited above would render them unsuitable for their intended purpose. A skilled artisan would find no reason to modify these intermediates to obtain a compound required by the present claims nor to use it as presently claimed. See also WO2017059178 (IDS), which teaches pyrrolidine compounds structurally related to those of the claims, with the same utility. For example, see compound at the bottom left of page 23: PNG media_image3.png 388 336 media_image3.png Greyscale The compounds taught in WO2017059178 require an amide substituent attached to the pyrrolidine ring at the position where the compounds required by the examined claims have a heterocyclic ring moiety A attached. The reference teaches a significantly different structural template, such that there would be no reason to modify it as claimed and if it was modified so dramatically, there would be no reasonable expectation that the modified compound would have similar or better activity. The examined application is not allowable at this time in view of the below non-statutory double patenting rejections. For clarity it is noted that appropriately filed terminal disclaimers would obviate these rejections and put the application into condition for allowance. 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). The filing of a terminal disclaimer by itself is not a complete reply to a nonstatutory double patenting (NSDP) rejection. A complete reply requires that the terminal disclaimer be accompanied by a reply requesting reconsideration of the prior Office action. Even where the NSDP rejection is provisional the reply must be complete. See MPEP § 804, subsection I.B.1. For a reply to a non-final Office action, see 37 CFR 1.111(a). For a reply to final Office action, see 37 CFR 1.113(c). A request for reconsideration while not provided for in 37 CFR 1.113(c) may be filed after final for consideration. See MPEP §§ 706.07(e) and 714.13. The USPTO Internet website contains terminal disclaimer forms which may be used. Please visit www.uspto.gov/patent/patents-forms. The actual 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/apply/applying-online/eterminal-disclaimer. [1] Claims 1-2, 4-5, 7-8, 10, 12, 14-15, 19-20, 23, 26 and 35-40 are rejected on the ground of nonstatutory double patenting as being unpatentable over claims 1-20 of U.S. Patent No. 11,168,083 in view of Kita (Diabetes 2015, 64, 3588–3599). Reference claims 1-14 are drawn to compounds which fall into the scope of the genus required by examined claims 1-2, 4-5, 7-8, 10, 12, 14-15, 19-20, and 23. The species required by examined claim 26 are identically listed in reference claim 14. Reference claim 18 is drawn to a method of use of the reference claim compounds for treating a plasma kallikrein (pKal)-mediated disease or condition in a subject in need thereof. Reference claim 19 suggests both edema and ocular disorder as the plasma kallikrein (pKal)-mediated disease or condition. The reference claims do not specify: -preventing or reducing edema in the eye of a subject per the examined claims. -diabetic macular edema (DME) as the plasma kallikrein (pKal)-mediated disease or condition. (examined claim 35) -the subject as a human diabetic having DME. (examined claims 36 and 40) -an additional treatment that is a VEGF-pathway targeting agent. (examined claims 37-38) -administration by intravitreal injection. (examined claim 39) Kita teaches each of the missing limitations and provides good reason to carry out the reference claim method with these features. The Kita reference teaches that that DME is a pKal-mediated disease or condition at least in the abstract. A skilled artisan would find reason to select DME as such a disease to treat with the reference method. This disease falls into the scope of the disorder required by all the examined claims. It would be obvious to use the particular compounds listed in the reference dependent claims in a method of treatment of DME, such a method meets the limitations of examined claims 1-2, 4-5, 7-8, 10, 12, 14-15, 19-20, 23, 26 and 35. The Kita reference teaches known treatment of human diabetics with DME through intravitreal injection of therapies that block VEGF actions on page 3588, column 2, paragraph 2. A skilled artisan would find reason to treat human diabetics with DME through a similar administration of an agent that interferes with pKal since both pathways operate in the same body compartment and both are taught as reasonable means to provide a benefit in the disease state. The reference suggests the use of both a VEGF-pathway targeting agent and an agent that interferes with pKal at least at page 3598, column 2, lines 9-12: “Since many individuals are not fully responsive to anti-VEGF DME therapy (10), PKal inhibition in these patients may provide an opportunity to further reduce macular thickness and improve vision”. A skilled artisan would find reason to carry out “combination therapy” using both agents in order to more effectively treat DME since both are taught as providing for a benefit. See also MPEP 2144.06 “"It is prima facie obvious to combine two compositions each of which is taught by the prior art to be useful for the same purpose, in order to form a third composition to be used for the very same purpose.... [T]he idea of combining them flows logically from their having been individually taught in the prior art." In re Kerkhoven, 626 F.2d 846, 850, 205 USPQ 1069, 1072 (CCPA 1980)”. [2] Claims 1-2, 4-5, 7-8, 10, 12, 14-15, 19-20, 23, 26 and 35-40 are rejected on the ground of nonstatutory double patenting as being unpatentable over claims 1-20 of U.S. Patent No. 11,905,285 in view of Kita (Diabetes 2015, 64, 3588–3599). Reference claims 1-14 are drawn to compounds which fall into the scope of the genus required by examined claims 1-2, 4-5, 7-8, 10, 12, 14-15, 19-20, and 23. Numerous of the species required by examined claim 26 are identically listed in reference claim 14. Reference claim 16 is drawn to a method of use of the reference claim compounds for treating a plasma kallikrein (pKal)-mediated disease or condition in a subject in need thereof. Reference claim 19 suggests diabetic macular edema (DME) as the plasma kallikrein (pKal)-mediated disease or condition. (examined claim 35). A skilled artisan would find reason, in the reference claims, to select DME as such a disease to treat with the reference method. This disease falls into the scope of the disorder required by all the examined claims. It would be obvious to use the particular compounds listed in the reference dependent claims in a method of treatment of DME, such a method meets the limitations of examined claims 1-2, 4-5, 7-8, 10, 12, 14-15, 19-20, 23, 26 and 35. The reference claims do not specify: -the subject as a human diabetic having DME. (examined claims 36 and 40) -an additional treatment that is a VEGF-pathway targeting agent. (examined claims 37-38) -administration by intravitreal injection. (examined claim 39) Kita teaches each of the missing limitations and provides good reason to carry out the reference claim method with these features. The Kita reference teaches that that DME is a pKal-mediated disease or condition at least in the abstract. The Kita reference teaches known treatment of human diabetics with DME through intravitreal injection of therapies that block VEGF actions on page 3588, column 2, paragraph 2. A skilled artisan would find reason to treat human diabetics with DME through a similar administration of an agent that interferes with pKal since both pathways operate in the same body compartment and both are taught as reasonable means to provide a benefit in the disease state. The Kita reference suggests the use of both a VEGF-pathway targeting agent and an agent that interferes with pKal at least at page 3598, column 2, lines 9-12: “Since many individuals are not fully responsive to anti-VEGF DME therapy (10), PKal inhibition in these patients may provide an opportunity to further reduce macular thickness and improve vision”. A skilled artisan would find reason to carry out “combination therapy” using both agents in order to more effectively treat DME since both are taught as providing for a benefit. See also MPEP 2144.06 “"It is prima facie obvious to combine two compositions each of which is taught by the prior art to be useful for the same purpose, in order to form a third composition to be used for the very same purpose.... [T]he idea of combining them flows logically from their having been individually taught in the prior art." In re Kerkhoven, 626 F.2d 846, 850, 205 USPQ 1069, 1072 (CCPA 1980)”. Conclusion Any inquiry concerning this communication or earlier communications from the examiner should be directed to DANIEL R CARCANAGUE whose telephone number is (571)270-3023. The examiner can normally be reached 9 am to 5 pm 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, 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. /DANIEL R CARCANAGUE/Primary Examiner, Art Unit 1621
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Prosecution Timeline

Dec 20, 2023
Application Filed
Aug 27, 2025
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
81%
Grant Probability
99%
With Interview (+24.3%)
1y 11m
Median Time to Grant
Low
PTA Risk
Based on 931 resolved cases by this examiner. Grant probability derived from career allow rate.

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