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 of Claims
Claims 1-19 are pending in the instant application.
Election/Restriction
This action is in response to an election from a restriction requirement filed March 25th, 2026. There are 19 claims pending and 15 claims under consideration. Claims 1-2 and 18-19 have been withdrawn as claims drawn to a non-elected invention.
Applicant did not indicate whether the election was made with or without traverse. As such, this has been construed by the examiner as an election without traverse of Group III, Claims 3-16 and a species election of (S)-5,5-dimethyl-2-(((1-methyl-1H-indol-4-yl)methyl)amino)hexanoic acid as a single species of compound of formula (I) in the reply filed May 26th, 2026 is acknowledged. Therefore this restriction is considered proper and thus made FINAL. As amended, Claim 17 now reads on Group III. Therefore, Claims 3-17 are presently under examination.
The elected species was found to be free of the prior art. Thus, examination was extended to all species of a compound of formula (I).
Priority
Acknowledgement is made of Applicant’s claim for foreign priority based on the EP21194937.5 application filed in the European Union on September 3rd, 2021.
Information Disclosure Statement
The Information Disclosure Statement filed on March 4th, 2024 has been fully considered by the examiner, except where marked with a strikethrough.
Specification
The specification has not been checked to the extent necessary to determine the presence of all possible minor errors. Applicant’s cooperation is requested in correcting any of the errors of which Applicant may become aware of in the specification.
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 3-11 and 13-17 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 a compound of formula (I) in which R1, R2, and R3 are C1-3 alkyl, R4 is hydrogen, C1-3 alkyl, C1-3 haloalkyl, or phenyl, and R5 is 5-10 membered heteroaryl, 5-10 membered heterocyclic ring, or 6-10 membered aryl, optionally substituted with -OH, C1-3 alkyl, C1-3 alkoxy, (C1-3 alkyl)hydroxyl, halogen, or C3 heteroaryl, does not reasonably provide enablement for compounds of formula (I) in which these variables are otherwise defined, nor does it enabling for an N-oxide or prodrug thereof. 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 use the invention commensurate in scope with these claims.
Pursuant to In re Wands, 858 F.2d 731, 737, 8 USPQ2d 1400, 1404 (Fed. Cir. 1988), one considers the following factors to determine whether undue experimentation is required: (1) The breadth of the claims, (2) The nature of the invention, (3) The state of the prior art, (4) The level of one of ordinary skill, (5) The level of predictability in the art, (6) The amount of direction provided by the inventor, (7) The existence of working examples and (8) The quantity of experimentation needed to make or use the invention based on the content of the disclosure.
Nature of the invention:
The invention is drawn to a compound of the formula:
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Breadth of the invention:
The scope of the claimed invention is broad, as it is drawn to any compound of the formula noted above, allowing for myriad combinations of the variables recited thereof.
With respect to prodrugs, at Page 30 of the instant specification, prodrugs are defined as “compounds that may be converted under physiological conditions or by solvolysis to a biologically active compound of the invention.” This includes a broad array of compounds readily envisaged by a person having ordinary skill in the art.
With respect to N-oxides, nitrogen atoms are present in a variety of positions including the nitrogen shown in the core structure, above and nitrogens in the substituent groups that define the variables as recited, for example at Claim 3. This allows for a broad number of compounds that would readily be envisaged by a person having ordinary skill in the art.
State of the prior art and predictability in the art:
The invention is directed toward medicine and is therefore physiological in nature. 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 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 ordinary skill in the art:
An ordinary artisan in the area of drug development would have experience in synthesizing chemical compounds for particular activities. The synthesis 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 be employed, developing a therapeutic method, as claimed, prior to synthesizing and testing compounds is generally not well-known or routine, given the complexity of certain biological systems.
The amount of direction provided and working examples:
The compound core depicted with specific substituents represents a narrow subgenus for which applicant has provided sufficient guidance to make and use; however, the disclosure is not sufficient to allow extrapolation of the limited examples to enable the scope of the compounds instantly claimed.
Applicant has provided no working examples of a compound in which R1, R2, R3 is defined as anything other than methyl. With respect to R4, only examples defining R4 as hydrogen, phenyl, CH3, or CHF2 have been provided. With respect to R5, only examples of 5, 6, 9, and 10-membered heteroaryl, heterocyclic, and 6- and 10-membered aryl substituents have been provided. In terms of substitution of R5, the only examples disclosed include -OH, methyl, -OCH3, -CH2OH, halogens, and C3-heteroaryl have been disclosed.
These limited examples are insufficient to provide enablement for the myriad of compounds that read on a compound of formula (I) as recited at instant Claim 3.
Further, no examples are disclosed such that a person having ordinary skill in the art would readily understand which prodrugs or N-oxides of a compound of formula (I) are suitable for use in the scope of the instant invention, nor would a person having ordinary skill in the art readily understand the motivation for making such prodrugs or N-oxides.
Within the specification, “specific operative embodiments or examples of the invention must be set forth. Examples and description should be of sufficient scope as to justify the scope of the claims.” Markush claims must be provided with support in the disclosure for each member of the Markush group. Where the constitution and formula of a chemical compound is stated only as a probability or speculation, the disclosure is not sufficient to support claims identifying the compound by such composition or formula. See MPEP 608.01(p).
MPEP § 2164.01 (a) states, “A conclusion of lack of enablement means that, based on the evidence regarding each of the above factors, the specification, at the time the application was filed, would not have taught one skilled in the art how to make and/or use the full scope of the claimed invention without undue experimentation. In re Wright, 999 F. 2d 1557, 1562, 27 USPQ2d 1510, 1513 (Fed. Cir. 1993).” That conclusion is clearly justified here that Applicant is not enabled for making these compounds.
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 3-9 and 13-17 is/are rejected under 35 U.S.C. 102(a)(1) as being anticipated by Fetalvero et. al. (WO 2017/070518 A1; hereinafter referred to as Fetalvero).
At Page 78, Fetalvero teaches the following compound:
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This compound reads on a compound of formula (I) as recited at instant Claim 3 when the variables are defined as follows:
R1, R2, and R3 are each halo, wherein halo is fluoro.
R4 is H.
R5 is C6-aryl.
Regarding Claim 17, at Page 79, Paragraph 00220, Fetalvero teaches the above compound was obtained as a solution that reads on the limitations instantly recited.
Claims 3 and 10 are rejected under 35 U.S.C. 102(a)(1) as being anticipated by CAS Registry File (194362-76-0; entered into STN September 23rd, 1997; hereinafter referred to as CAS Registry File).
CAS Registry File teaches the following compound:
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This compound reads on a compound of formula (I) as recited at Claim 3 when the variables are defined as follows:
R1, R2, and R3 are each H.
R4 and R5, together form a tricyclic 14-membered heterocyclic ring.
Allowable Subject Matter
Claim 12 is objected to as being dependent upon a rejected base claim, but would be allowable if rewritten in independent form including all of the limitations of the base claim and any intervening claims.
Conclusion
Claims 3-11 and 13-17 are rejected.
Claim 12 is objected to.
No claim is allowed.
Any inquiry concerning this communication or earlier communications from the examiner should be directed to DANIEL JOHN BURKETT whose telephone number is (703)756-5390. The examiner can normally be reached Monday - Friday.
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, Jeffrey Murray can be reached at (571) 272-9023. The fax phone number for the organization where this application or proceeding is assigned is 571-273-8300.
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/D.J.B./ Examiner, Art Unit 1624
/JEFFREY H MURRAY/ Supervisory Patent Examiner, Art Unit 1624
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