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 .
Priority
This application has PRO 63/523,510 (06/27/2023).
Election/Restrictions
Applicant's election without traverse of Group I, claims 1-30, in the reply filed on 8/10/26 is acknowledged.
Applicant also elected the following species:
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stated to read on claims 1, 3, 6, 7, 9-11, 16-30.
As detailed in the following rejections, the generic claim encompassing the elected species was not found patentable. Therefore, the provisional election of species is given effect, the examination is restricted to the elected species only, and claims not reading on the elected species are held withdrawn. MPEP 803.02; Ex parte Ohsaka, 2 USPQ2d 1460, 1461 (Bd. Pat. App. lnt. 1987). Accordingly, claims 2, 4-5, 8, 12-15 are hereby withdrawn.
Should applicant, in response to this rejection of the Markush-type claim, overcome the rejection through amendment, the amended Markush-type claim will be reexamined to the extent necessary to determine patentability of the Markush-type claim. See MPEP 803.02.
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.
Claims 1, 3, 6, 7, 9-11, 16-30 are rejected under 35 U.S.C. 112(a) because the specification, while being enabling for a scope supported by compounds demonstrated as useful, does not reasonably provide enablement for the full scope of the claims. The specification does not enable any person skilled in the art to which it pertains, or with which it is most nearly connected, to make and/or use the invention commensurate in scope with these claims.
Claim 1 is to a compound of the formula
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which are alleged to bind to the p53 Y220C pocket for modulating p53 activity and use for treating cancer (Specification p. 1-2) wherein U,V,W,X are CR5 or N with one being C-Y-R1, where R1, R2, and R5 are to a vast scope of further substituted groups including 10-membered heteroaryl, Y is O, N, S, CH2, NCH2, OCH2; Z is S, O, NR3a, where R3 and R3a are to a vast list of alternatives. The instant disclosure does not contain sufficient information regarding the subject matter of the claims as to enable one skilled in the pertinent art to make and use the claimed invention upon consideration of the factors set forth in In re Wands, 858 F.2d 731, 737, 8 USPQ2d 1400, 1404 (Fed. Cir. 1998), as follows. See also MPEP § 2164.01(a) and § 2164.04.
The breadth of the claims – the claims are to a scope of a large genus of compounds each claim in excess of billions of compounds.
The nature of the invention – the nature of the claimed invention is to modulate p53.
The state of the prior art – Applicant proposes small molecule reactivators targeting p53 mutants including Y220C, but cites no successful demonstration of the approach.
The level of one of ordinary skill – the level of skill in the art is high as evidenced by Vu et al. (WO2021231474).
The level of predictability in the art – the art is highly unpredictable due to the complex nature of the disease and the mode of action of the compounds used. Furthermore, as evidenced by Vu (Tables 10 and 11) after screening hundreds of compounds only a few showed significant levels of pharmacologic activity.
The amount of direction provided by the inventor – the primary guidance provided by the inventor is given in the Example measuring in vitro assay of binding of a limited number of compounds of claim 1’s Formula, where all are primarily Z=S, with 1 O, and 9 N; U,V,W,X are all CH with one selected from C-Y-R1 with R1 as -NR11; R3 are all primarily -CH2CF3 with 3 as -S-CF3, of which only a small number showed significant activity below 100 nM. There is no apparent correlation between the structure of the compounds within the claims and those tested. Each of the compounds evaluated are all of very similar structure and does not map large chemical structure space compared to the scope of the claims. This lack of supporting data and explanation would cause one of skill in the art to question whether the examples support enablement of the full scope of the claims.
The existence of working examples – there are no working examples of the claimed compounds treating disease and as indicated above. The in vitro assay data has very limited scope
The quantity of experimentation needed to make or use the invention based on the content of the disclosure – given the high level of unpredictability in the art, the lack of working examples, and the limited guidance provided in the examples, there would be a tremendous amount of experimentation required before one of skill in the art would consider being enabled to make and use the full scope of the claims for the asserted utility.
In view of the specification and evidence of record, one of skill in the art would be required to perform an undue amount of experimentation to test each of the compounds of the claims using an appropriate model select candidates for further development in vivo, perform testing to determine dosing, and finally efficacy testing. Thus, one of skill in the art would be required to start ab initio and develop any compound within the scope of the claims. Such a level of experimentation is undue. Weighing the above factors by a preponderance of the evidence results in the conclusion that the claims are not enabled for the asserted utility with the full scope of the claims.
Claim Rejections - 35 USC § 102
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.
(a)(2) the claimed invention was described in a patent issued under section 151, or in an application for patent published or deemed published under section 122(b), in which the patent or application, as the case may be, names another inventor and was effectively filed before the effective filing date of the claimed invention.
Claims 1, 3, 9, 16-24, 28, 30 are rejected under 35 U.S.C. 102(a)(1) as being anticipated by Stewart et al. (WO1999062908).
Stewart teaches the compound [(4-methylphenyl)thio]thieno[2,3-c]pyridine-2-carboxaldehyde (claim 7) which anticipates the claims when Z is S; V is N; X is C-Y-R1; Y is S; R1 is 4-methylphenyl; W,U are CH; R3 is H; A is CH=N-O; R2 is CH2-Phenyl. Stewart also teaches the compound in a pharmaceutical composition (p. 32).
Conclusion
No claims allowed.
Any inquiry concerning this communication or earlier communications from the examiner should be directed to ROBERT H HAVLIN whose telephone number is (571)272-9066. The examiner can normally be reached 9am - 6pm.
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/ROBERT H HAVLIN/Primary Patent Examiner, Art Unit 1626
