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 .
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.
Election/Restrictions
Applicant’s election without traverse in the reply filed on 29 December 2025, is acknowledged.
Applicants provided a compliant species election:
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, which is a species of genus formula I of instant claim 1, wherein: A1 is an oxygen (O) atom; A2 represents -CRCRD wherein RC and RD are each a hydrogen (H) atom; L1 is methylene; R1 is H; X is carbon (C) atom; L2 represents C2alkylene; Z represents -OR7 wherein R7 is C1alkylene formed together with R4, wherein R4 and R7 together with the C atom and the O atom to which they, respectively, are attached, form a 6-membered saturated heterocycle substituted with methyl.
The Applicants’ elected species is free of the prior art.
The Examiner extended the Markush search to the full scope of instant claim 1 but did not find any prior art.
Therefore, the Election of Species Requirement of 30 July 2025, is withdrawn, as all claims are free of the prior art.
All claims have been examined on the merits.
Current Status of 18/026,187
This Office Action is responsive to the amended claims of 14 March 2023.
Claims 1-21 have been examined on the merits. Claims 1-3, 6, 8-9, 12-13, 15, and 21 are original. Claims 4-5, 7, 10-11, 14, and 16-20 are currently amended.
Priority
The effective filing date is 17 September 2021.
Receipt is acknowledged of certified copies of papers required by 37 CFR 1.55.
Information Disclosure Statement
The information disclosure statements (IDS) submitted on 7 July 2025; 5 May 2025; and 16 May 2023, are in compliance with the provisions of 37 CFR 1.97. Accordingly, the information disclosure statements are being considered by the examiner.
Specification
Various illustrations within the Specification, such as illustrations found within pages 4, 6-8, 37, 41, 43, and 45-46 are highly pixelated and hence of poor resolution. This makes it harder to discern the true identity of each atom, bond, and variable. For example, is “I2” really “L2” (from the illustration within page 4)? Applicants are asked to enlarge the illustrations and darken all bonds and variables so as to make every heteroatom, carbon, and variable more discernible.
The title of the invention contains “Novel”. The title of the invention is not descriptive. Words such as “New”, “Novel”, “Improvement”, and “Improvement of” are not permitted in the title. See MPEP 606 for a complete list of prohibited words. A new title is required that is clearly indicative of the invention to which the claims are directed.
The following title is suggested: -- [[Novel]] Amine Derivatives having a DYRK inhibitory effect -- .
Claim Objections
Claim 1 is objected to for having a highly pixelated (hence poor resolution) illustration of genus formula I. This makes it harder to discern the true identity of each atom, bond, and variable. For example, is “I2” really “L2”?
Claim 7 genus formula 1a is plagued with the same high pixelation (poor resolution) illustration. Moreover, claim 11 formula 1b and claim 16 genus formula 1c are each similarly highly pixelated.
Claims 2-21 are similarly objected to as these claims refer back to claim 1 but do not remedy the rationale underpinning the basis for objecting to claim 1.
Applicants are asked to enlarge the illustrations and darken all bonds and variables so as to make every heteroatom, carbon, and variable more discernible.
Claim 17 is objected to for containing “Example #” after the name of each compound. For example:
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(note the circled “Example 7” and “Example 8”). The Examiner is objecting to the “Example #” appearing after each named compound of claim 17 because it could add ambiguity to the claim as one might ask what Applicants mean by “Example 7”. The Examiner also believes it might be an artifact in drafting the claims to show where support is found in the Specification.
To render moot this objection: please remove all “Example #” appearing after each named compound of claim 17.
Claim Rejections - 35 USC § 112
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 20-21 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 treating the claim 21 diseases, does not reasonably provide enablement for (1) treating and/or preventing the undisclosed plethora of claim 20 diseases and (2) preventing the claim 21 diseases. The specification does not enable any person skilled in the art to which it pertains, or with which it is most nearly connected, to use the invention commensurate in scope with these claims.
The Wands Factors used in an (scope of) enablement rejection include (per MPEP 2164.01(a)):
The breadth of the claims:
Claims 20-21 are drafted to include both therapeutic (“therapeutic agent”) and preventive (“prophylactic agent”) properties of the instant claim 1 compound. Furthermore, claim 21 contains alternative embodiments of diseases which the instant claims 20-21 disclose as being both treated and prevented by the instant claim 1 compound.
Also, the Examiner notes that claim 20 is very broad—the actual diseases being treated or prevented are not disclosed. Thus, under the broadest reasonable interpretation (BRI) Applicants’ claim 20 is really claiming use of the instant claim 1 compound to treat and/or prevent any (emphasis) disease that might be affected by DYRK modulation. Claim 21 then gives a long (exemplary) list of diseases impacted by DYRK modulation.
The nature of the Invention:
The present invention relates to a medicament comprising a compound that Applicants disclose has a DYRK inhibitory effect which can be used to treat a plurality of neuropsychiatric diseases.
The state of the prior art:
The instant genus formula I of claim 1 comprising the required third ring comprising A1-L1-A2 is not anticipated or taught in the prior art.
However, there is a plethora of prior art disclosing treatments using other compounds to treat many of the neuropsychiatric diseases of claim 21.
Moreover, the Examiner notes that many of the claim 21 diseases cannot be prevented. For example, the prior art reference RHEINSCHILD (Rheinschild, Erica. “Experts: One in Three Cases of Dementia Preventable; Nonmedical Therapies Ideal for Dementia.” Keck School of Medicine of USC. Published 20 July 2017. Accessed 31 March 2026. Available from: < https://keck.usc.edu/news/experts-one-in-three-cases-of-dementia-preventable-nonmedical-therapies-ideal-for-dementia/ > ), discloses lifestyle changes that can reduce the risk of dementia, including Alzheimer’s disease, but cannot prevent dementia or Alzheimer’s disease (see first few pages; also note that the title says “One in Three Cases of Dementia are Preventable”, which means that dementia and Alzheimer’s disease are not entirely preventable). The RHEINSCHILD reference is used by the Examiner to show that the limitations of instant claim 21 with “dementia”: frontotemporal dementia, Lewy body dementia, vascular dementia, and dementia syndrome associated therewith cannot be prevented. Also, RHEINSCHILD is used to show that Alzheimer’s disease cannot be prevented. Note, there is a difference between “reducing the risk of” (through lifestyle changes) and “prevention”.
Furthermore, the prior art reference PARKINSON (The Ohio State University. “Farming with Parkinson’s Disease”. Published 26 January 2012. Accessed 31 March 2026. Available from: < https://ohioline.osu.edu/factsheet/AEX-982.5-11 > ), teaches that “Parkinson’s disease cannot be prevented” (see pages 2-3 “How to Prevent Parkinson’s Disease:”).
Moreover, the prior art reference PANCREATIC (Harvard Health Publishing. “Pancreatic cancer: Symptoms, treatment, and prevention.” Published 23 January 2017. Accessed 31 March 2026. Available from: < https://www.health.harvard.edu/cancer/pancreatic-cancer-symptoms-treatment-and-prevention-the-familyhealth-guide > ), reports that “no one knows exactly what causes pancreatic cancer” (see first page). Hence, it cannot be said that use of a medicament is known to prevent pancreatic cancer. Just like the diseases discussed, above, lifestyle changes can reduce the risk of getting pancreatic cancer (see last page of reference), but “reducing the risk of” is not synonymous with “preventing”.
The level of one of ordinary skill:
The level of one of ordinary skill in the art includes knowledge to engage in a reasonable amount of experimentation to make the compound of instant claim 1 and to test its inhibitory effects on DYRK for potential therapeutic uses.
The level of predictability in the art:
The art is predictable with making the compound of instant claim 1, especially in light of the guidance provided in Applicants’ Specification (see, below; includes pages 119-161 of the Specification). Furthermore, the art is predictable in using the claim 1 compound to treat a variety of diseases linked to DYRK modulation, especially in light of Applicants’ guidance within pages 1-3 and 163-169 of the Specification.
However, the art is unpredictable with regards to using the claim 1 compound as a preventive agent (“prophylactic agent” of instant claims 20-21) to prevent any disease (since instant claim 20 is broad/vague as to diseases that the claim 1 compound is used to prevent) and since there are disclosed neuropsychiatric diseases of claim 21 that are known to be difficult to prevent (see, “The State of the Prior Art” above).
The amount of direction provided by the inventor:
The Applicants have provided direction to make the compound of instant claim 1 (see, for example, Specification pages 119-161).
Furthermore, Applicants have provided direction to test the DYRK inhibitory effect of exemplary compounds of the genus formula I from instant claim 1 (see Specification pages 1-3 and 162-168).
The existence of working examples; and
The Specification provides working examples to make the compounds of instant claim 1 (see, for example, Specification pages 119-161).
Furthermore, the Specification provides working examples to use the claim 1 compounds to treat various diseases associated with DYRK modulation (see pages 162-168 showing that the claim 1 compounds have inhibitory effects on DYRK; see pages 1-3 explaining how DYRK modulation impacts neuropsychiatric health, including development of many of the claim 21 diseases).
The quantity of experimentation needed to make or use the invention based on the content of the disclosure:
The quantity of experimentation needed to make the claim 1 compound is reasonable, especially in light of the guidance within Applicants’ Specification pages 119-161.
The quantity of experimentation needed to use the claim 1 compound as a medicament/pharmaceutical composition to treat the DYRK diseases of claim 21 is reasonable in light of Applicant-provided guidance within the Specification pages 1-3 and 162-168.
However, the quantity of experimentation needed to: (1) treat or prevent any disease of claim 20 and (2) prevent the diseases of claim 21 is unreasonable. Applicants’ Specification does not provide guidance as to preventing any disease (BRI of claim 20) and/or any one of the diseases of claim 21. Moreover, the prior art RHEINSCHILD, PARKINSON, and PANCREATIC (all discussed, above) are exemplary in that they show that many of the claim 21 diseases are known not to be preventable.
Therefore, claims 20-21 are rejected as lacking scope of enablement under 35 USC 112(a) for “treating or preventing” the undisclosed plethora of diseases of claim 20 and lack scope of enablement for “preventing” the diseases of claim 21.
To render moot this scope of enablement rejection: please strike “prophylactic”, “preventive” and synonymous of “prevent” from the claims AND specify the DYRK diseases that the claim 1 compound is used to treat within claim 20. This can be done by moving the diseases from claim 21 into claim 20 and then canceling claim 21.
Conclusion
Claims 1-19 are objected to for illegible illustrations and/or “Example #” in the claim 17 compound names (see “Objections”, above).
Claims 20-21 are not presently allowable as written.
There is no known prior art reference that either teaches or anticipates a compound of genus formula I of instant claim 1.
The reference ACS (American Chemical Society. Chemical Abstract Service. RN 5268-89-3. Entered into STN: 16 November 1984), discloses the compound:
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(see enclosed ACS reference), which is structurally similar to genus formula I in that R1 is hydrogen (H) atom.
However, ACS is a close art but not a prior art reference as it does not have a third/fused-ring where instant claim 1 requires A1-L1-A2. Moreover, oxo moieties at the locales corresponding to L2 and R4 are not permitted by instant claim 1. Moreover, the ACS reference has a -CH2-CH2-Cl branch where the same locale of instant claim 1 is a H atom. Finally, the same ring of ACS contains a =S moiety where instant claim 1 requires an =O moiety.
These structural differences account for too many differences to make a viable obviousness rejection without running afoul of hindsight reasoning.
Moreover, the reference WO 2010/10797 (provided by Applicants in their IDS of 16 May 2023) is drawn to distinct ringed compounds that lack the instantly claimed A1-L1-A2 fused ring.
Also, the reference WO 2013/26806 (provided by Applicants in their IDS of 16 May 2023) is drawn to distinct ringed compounds that lack the instantly claimed A1-L1-A2 fused ring.
The co-pending 18/292,585 is not a double patent reference as the claims of ‘585 are drawn to distinct subject matter.
Any inquiry concerning this communication or earlier communications from the examiner should be directed to JOHN S KENYON whose telephone number is (571)270-1567. The examiner can normally be reached Monday-Friday 10a-6p.
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If attempts to reach the examiner by telephone are unsuccessful, the examiner’s supervisor, Andrew D Kosar can be reached at (571) 272-0913. The fax phone number for the organization where this application or proceeding is assigned is 571-273-8300.
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/JOHN S KENYON/Primary Patent Examiner, Art Unit 1625
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