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 .
Request for Continued Examination Under 37 CFR 1.114
A request for continued examination under 37 CFR 1.114, including the fee set forth in 37 CFR 1.17(e), was filed in this application after final rejection. Since this application is eligible for continued examination under 37 CFR 1.114, and the fee set forth in 37 CFR 1.17(e) has been timely paid, the finality of the previous Office action has been withdrawn pursuant to 37 CFR 1.114. Applicant's submission filed on 02/26/2026 has been entered.
Status of the Claims
Claims 1-3, 19, 20, 67, 69-71, 73, 80, 82, and 132 are pending. Acknowledgment is made of the amendment of claims 1, 69, 71, 73, and 80, the cancellation of claims 41 and 42, and the addition of new claim 132 in the reply filed 02/26/2026.
Information Disclosure Statement
The information disclosure statement (IDS) submitted on 02/26/2026 is in compliance with the provisions of 37 CFR 1.97. Accordingly, the information disclosure statement is being considered by the examiner.
Election/Restriction Requirement
Applicant’s election without traverse of Group I, claims 1-3, 19-20, 41-42, 67, 69-71, 73, 80, and 82, drawn to compounds of formula (I), in the reply filed on 06/25/2025 is acknowledged.
Applicant elected the species Compound 251, shown below, which reads on claims 1-3, 19-20, 67, 69-71, 73, 80, 82, and 132.
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As per MPEP 803.02, the examiner will determine whether the entire scope of the claims is patentable. Applicant’s elected species, Compound 251, appears allowable. Therefore, examination of the claims has been extended to include the full scope of the claims.
Withdrawn Objections/Rejections
Applicant’s amendment to the claims, filed 02/26/2026, overcomes the rejection of claim 80 under 35 U.S.C. 112(d) for failing to include the subject matter of the claim upon which it depends. The rejection of claim 80 has been withdrawn.
Maintained Objections
Claim 80 is objected to because of the following informalities:
Claim 80 reads “The compounds according to claim 1, that are selected from… or pharmaceutically acceptable salts thereof” (emphasis added). In order to be in the singular form, the claim should read “A compound according to claim 1 wherein the compound is selected from… or a pharmaceutically acceptable salt thereof” (emphasis added).
Appropriate correction is required.
Modified Rejections
Necessitated by Claim Amendment
Claim Rejections - 35 USC § 103
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.
Claims 1-3, 20, 67, 69-71, 73, 82, and 132 are rejected under 35 U.S.C. 103 as being unpatentable over Gaufreteau et al. (WO 2021086785 A1, with an effective filing date of 28 October 2019, cited by Applicant in the IDS).
Gaufreteau et al. teaches the compound Example 105, shown below.
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Compared to Formula I of the instant claims, in this Example 105, k is 0, X1 is O, L1 is ethylene, m is 0, L2 is
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, L3 is C4-heterocyclene-C7-alkylene substituted with 2 oxo- groups, and the degradation moiety is
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.
Gaufreteau et al. teaches, in claim 16, a pharmaceutical composition comprising Example 105 shown above, as in instant claim 82.
This compound by Gaufreteau et al. differs from the instant compounds in that the phenyl group is meta-substituted (by L1 and L) rather than para-substituted, as in instant Formula I.
It is well known in the art that compounds having the same radical at different positions on the nucleus are position isomers. Their properties are often so nearly alike as to present difficulties in identification or separation. Ex parte Mowry (POBA 1950) 91 USPQ 219. A novel, useful compound which is isomeric with a compound of the prior art is unpatentable unless it possesses some unobvious or unexpected beneficial property not possessed by the prior art compound. In re Norris (CCPA 1950) 179 F2d 970, 84 USPQ 458; In re Finley (CCPA 1949) 174 F2d 130 and 135, 81 USPQ 383 and 387.
A compound need not be an adjacent homolog or position isomer of a prior art compound in order to be susceptible to a rejection based on structural obviousness; the name used to designate the structural relationship between compounds is not controlling, it is the closeness of that relationship. In re Payne et al. (CCPA 1979) 606 F2d 303, 203 USPQ 245. When chemical compounds have “very close” structural similarities…without more, a prima facie case of obviousness may be made. In re Grabiak (CAFC 1985) 769 F2d 729, 226 USPQ 870.
Therefore, the compounds of the instant claims are unpatentable unless they possesses some unobvious or unexpected beneficial property not possessed by the prior art compound.
New Rejections
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 1-3, 19, 20, 67, 69-71, 73, 82, and 132 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 compound of Formula I where k and m are 0; R2 is unsubstituted H or C1-4 alkyl; L1 is unsubstituted C1-6 alkyl; L3 is C1-10 heteroalkylene, -O-, or 4-10 membered heterocycloalkyl optionally substituted with -OH; RB1 is A2; RB2, RB4, RB5, and RB8 are H; RB3 is A2 or unsubstituted C1-6 alkyl; v2 is 0; RB7 is C1-3 alkyl; and RB9 is H or C1-3 alkyl, does not reasonably provide enablement for compounds of Formula I. 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 the invention commensurate in scope with these claims.
To be enabling, the specification of the patent application must teach those skilled in the art how to make and use the full scope of the claimed invention without undue experimentation. In re Wright, 999 F.2d 1557, 1561 (Fd. Cir. 1993). Explaining what is meant by "undue experimentation," the Federal Circuit has stated that:
The test is not merely quantitative, since a considerable amount of experimentation is permissible, if it is merely routine, or if the specification in question provides a reasonable amount of guidance with respect to the direction in which experimentation should proceed to enable the determination of how to practice a desired embodiment of the claimed invention. PPG v. Guardian, 75 F.3d 1558, 1564 (Fed. Cir. 1996). As pointed out by the court in In re Angstadt, 537 F.2d 498 at 504 (CCPA 1976), the key word is "undue", not "experimentation".
The factors that may be considered in determining whether a disclosure would require undue experimentation are set forth In re Wands, 8 USPQ2d 1400 (CAFC 1988) at 1404 wherein, citing Ex parte Forman, 230 USPQ 546 (Bd. Apls. 1986) at 547 the court recited eight factors:
1- the quantity of experimentation necessary,
2- the amount of direction or guidance provided,
3- the presence or absence of working examples,
4- the nature of the invention,
5- the state of the prior art,
6- the relative skill of those in the art,
7- the predictability of the art, and
8- the breadth of the claims
These factors are always applied against the background understanding that scope of enablement varies inversely with the degree of unpredictability involved. In re Fisher, 57 CCPA 1099, 1108, 427 F.2d 833, 839, 166 USPQ 18, 24 (1970). Keeping that in mind, the Wands factors are relevant to the instant fact situation for the following reasons:
The nature of the invention
The nature of the invention relates to compounds of formula (I) in claim 1. Such compounds are useful for modulating BRG1- or BRM-associated factors. This invention is also directed to compositions comprising said compounds.
Predictability of the art
The compounds synthesized in the instant specification appear novel. However, the hypothetical compounds in claim 1 would be unpredictable in terms of one skilled in the art being able to synthesize every possible compound claimed in instant claim 1. It is well established that “the scope of enablement varies inversely with the degree of unpredictability of the factors involved,” and physiological activity is generally considered to be an unpredictable factor. See In re Fisher, 427 F.2d 833, 839, 166 USPQ 18, 24 (CCPA 1970).
In terms of the law, MPEP 2107.03 states “evidence of pharmacological or other biological activity of a compound will be relevant to an asserted therapeutic use if there is a reasonable correlation between the activity in question and the asserted utility. Cross v. Iizuka, 753 F.2d 1040, 224 USPQ 739 (Fed. Cir. 1985); In re Jolles, 628 F.2d 1322, 206 USPQ 885 (CCPA 1980); Nelson v. Bowler, 626 F.2d 853, 206 USPQ 881 (CCPA 1980).” If correlation is lacking, it cannot be relied upon, Ex parte Powers, 220 USPQ 924; Rey-Bellet and Spiegelberg v. Engelhardt v. Schindler, 181 USPQ 453; Knapp v. Anderson, 177 USPQ 688. Indeed, the correlation must have been established “at the time the tests were performed”, Hoffman v. Klaus, 9 USPQ2d 1657.
Level of skill in the art
An ordinary artisan in the area of drug development would have experience in synthesizing and screening chemical compounds for particular activities, such as a medical doctor or chemist. Screening of new drug candidates, while complex, is routine in the art. The process of finding new drugs that have in vitro activity against a particular biological target, (i.e., receptor, enzyme, etc.) is well known. Additionally, while high throughput screening assays can often be employed, developing a therapeutic method, as claimed, is generally not well-known or routine, given the complexity of certain biological systems.
4. The breadth of the claims
The scope of the claims involves compounds of formula (I), shown below.
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Claim 1 is very broad in the number of variables and the options of substituents for each variable. There is an extremely large amount of hypothetical compounds included in claim 1.
5. The amount of direction provided, the presence or absence of working examples, and the quantity of experimentation necessary
The specification only provides the synthesis of about 110 compounds which read on Formula (I). In all of the compounds synthesized, k and m are 0; R2 is unsubstituted H or C1-4 alkyl; L1 is unsubstituted C1-6 alkyl; L3 is C1-10 heteroalkylene, -O-, or 4-10 membered heterocycloalkyl optionally substituted with -OH; RB1 is A2; RB2, RB4, RB5, and RB8 are H; and v2 is 0. Additionally, examples are only provided where RB7 is methyl, RB9 is H or methyl, and RB3 is C3-4 alkyl. However, it would be assumed that the inventors are also enabled for RB7 and RB9 being C2-3 alkyl, and RB3 being C1-6 alkyl, since these substituents are similar in size and reactivity.
Synthesis methods are not taught in the specification to provide for the aforementioned variables to include all of the possible substituents listed in the claims. It would be expected that the varying size, electronegativity, and aromaticity of the substituents (e.g., R2, L1, L3, and RB1 to RB9) would change the reactivity of the compounds, and therefore would require alternate synthesis methods. It could also be possible that some combinations of compounds may not be able to be synthesized due to their instability (e.g., RB1 to RB9 are all substituted with large cyclic groups). It would require one skilled in the art, such as a chemist, to perform thousands of reactions to determine which compounds of formula (I) can be prepared and would require synthesis methods other than those provided in the specification. This is undue experimentation given the limited guidance and direction provided by Applicants.
Accordingly, the instant claims do not comply with the enablement requirement of 35 U.S.C. 112(a), since to practice the claimed invention a person of ordinary skill in the art would have to engage in undue experimentation, with no assurance of success.
Conclusion
Claims 1-3, 19, 20, 67, 69-71, 73, 82, and 132 are rejected.
Claim 80 is objected to.
Any inquiry concerning this communication or earlier communications from the examiner should be directed to RILLA M SAMSELL whose telephone number is (703)756-5841. The examiner can normally be reached Monday-Friday, 7-3.
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/R.M.S./Examiner, Art Unit 1624
/JEFFREY H MURRAY/Supervisory Patent Examiner, Art Unit 1624