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 11-21 are pending in the instant application.
Claims 1-10 have been canceled.
Priority
Acknowledgement is made of Applicant’s claim for foreign priority based on the CN2021110305886.0 application filed in the People’s Republic of China on March 23rd, 2021.
Information Disclosure Statement
The Information Disclosure Statement filed August 21st, 2023 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.
Drawings
The drawings are objected to because several labels in the horizontal axes in Figures 1-3 are illegible. Corrected drawing sheets in compliance with 37 CFR 1.121(d) are required in reply to the Office action to avoid abandonment of the application. Any amended replacement drawing sheet should include all of the figures appearing on the immediate prior version of the sheet, even if only one figure is being amended. The figure or figure number of an amended drawing should not be labeled as “amended.” If a drawing figure is to be canceled, the appropriate figure must be removed from the replacement sheet, and where necessary, the remaining figures must be renumbered and appropriate changes made to the brief description of the several views of the drawings for consistency. Additional replacement sheets may be necessary to show the renumbering of the remaining figures. Each drawing sheet submitted after the filing date of an application must be labeled in the top margin as either “Replacement Sheet” or “New Sheet” pursuant to 37 CFR 1.121(d). If the changes are not accepted by the examiner, the applicant will be notified and informed of any required corrective action in the next Office action. The objection to the drawings will not be held in abeyance.
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 11-12 and 17-21 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 an agarofuran-based compound of structural formula (I) as recited at instant Claim 11 in which R2 is unsubstituted C3-C5 alkylene and R4 is either hydrogen or deuterium, does not reasonably provide enablement for compounds of formula (I) as recited at instant Claim 11 where R2 and R4 are otherwise defined. 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.
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 example of any compound in which R2 and R4 were defined as anything other than the options as noted above in the instant application.
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.
The following is a quotation of 35 U.S.C. 112(b):
(b) CONCLUSION.—The specification shall conclude with one or more claims particularly pointing out and distinctly claiming the subject matter which the inventor or a joint inventor regards as the invention.
The following is a quotation of 35 U.S.C. 112 (pre-AIA ), second paragraph:
The specification shall conclude with one or more claims particularly pointing out and distinctly claiming the subject matter which the applicant regards as his invention.
Claims 11 and 13-16 are rejected under 35 U.S.C. 112(b) or 35 U.S.C. 112 (pre-AIA ), second paragraph, as being indefinite for failing to particularly point out and distinctly claim the subject matter which the inventor or a joint inventor (or for applications subject to pre-AIA 35 U.S.C. 112, the applicant), regards as the invention.
Claim 11 recites the limitation “when m=1, R3 is selected from hydrogen atom, carbonyl, or hydroxy; when m=2, R3 is deuterium atom.” This is indefinite, as defining m=1 and R3 as hydroxyl, the carbon labeled number 4 necessarily must additionally have a hydrogen atom bound to it. For example, Claim 13 is drawn to the following compound:
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Defining m as 2, where one R3 is hydrogen and the second R3 is hydroxyl, this raises an issue of a lack of antecedent basis, as Claim 11 requires that R3 is defined as deuterium when m=2. Appropriate correction is required.
Claims 14-16 are rendered indefinite as they are drawn to a “use” of the compound according to Claim 11 without positively reciting any active steps delimiting how this use is actually practiced. Per MPEP 2173.05(q), “Attempts to claim a process without setting forth any steps involved in the process generally raises an issue of indefiniteness under 35 U.S.C. 112(b) or pre-AIA 35 U.S.C. 112, second paragraph.”
Claim Rejections - 35 USC § 101
35 U.S.C. 101 reads as follows:
Whoever invents or discovers any new and useful process, machine, manufacture, or composition of matter, or any new and useful improvement thereof, may obtain a patent therefor, subject to the conditions and requirements of this title.
Claims 14-16 are rejected under 35 U.S.C. 101 because the claimed invention is directed to non-statutory subject matter. The claim(s) does/do not fall within at least one of the four categories of patent eligible subject matter because the claims are drawn to a “use” without positively reciting any steps to a process thereof.
Per MPEP 2173.05(q), “”Use” claims that do not purport to claim a process, machine, manufacture, or composition of matter fail to comply with 35 U.S.C. 101. In re Moreton, 288 F.2d 708, 709, 129 USPQ 227, 228 (CCPA1961)(“one cannot claim a new use per se, because it is not among the categories of patentable inventions specified in 35 U.S.C. § 101 “).”
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 11-13 and 17-21 are rejected under 35 U.S.C. 103 as being unpatentable over Guo et. al. (WO 00/31058; machine translation provided; hereinafter referred to as Guo) in view of Meanwell (“Fluorine and Fluorinated Motifs in the Design and Application of Bioisosteres for Drug Design,” Journal of Medicinal Chemistry, 61, 5822-5880, 2018; hereinafter referred to as Meanwell).
At Page 21, Guo teaches the following compound:
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This compound reads on a compound of formula (I) as recited at Claim 11 when the variables are defined as follows:
There is a double bond located in the position 2-3 of the ring A.
R2 is C4 alkylene.
m=1; R3 is hydrogen.
R4 is hydrogen.
This compound differs from a compound of structural formula (I) in that R1 is unsubstituted methyl.
This compound differs from the following compound recited at Claim 13 in that the CF3 moiety in the claimed compound is substituted for a methyl group in the compound taught by Guo, above:
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.
At Page 5823, First Column, second paragraph, Meanwell teaches that “Replacing hydrogen atoms with fluorine has been explored extensively in drug design, most commonly to replace those bound to an aromatic ring or in the context of a CF3 for CH3 replacement where these substitutions can modulate potency or interfere with metabolic modification.”
Applying KSR exemplary rationale B, it would have been prima facie obvious to a person having ordinary skill in the art to substitute the terminal methyl group in the compound taught by Guo for the trifluoromethyl group instantly claimed, as fluorine is known in the art to be bioisosteric to hydrogen. Motivated by the potential to modulate potency by such a substitution as taught by Meanwell, Claims 11-13 and 17-21 would have been practiced with reasonable expectation of success.
Claims 11-12 and 17-21 are rejected under 35 U.S.C. 103 as being unpatentable over U.S. Patent No. 11,358,944 (granted for U.S. Application No. 16/687,538, cited on Applicant’s Information Disclosure Statement filed August 21st, 2023; prior art pursuant to 35 U.S.C. 102(a)(2) as a U.S. Patent with a prior filing date of November 18th, 2019; hereinafter referred to as U.S. Patent No. ‘944) in view of Meanwell.
At Column 2, Line 10, U.S. Patent No. ‘944 teaches the following compound:
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This compound reads on a compound of formula (I) as recited at Claim 11 when the variables are defined as follows:
There is a double bond located in the position 2-3 of the ring A.
R2 is C3 alkylene.
m=2; R3 is deuterium.
R4 is hydrogen.
This compound differs from a compound of structural formula (I) in that R1 is unsubstituted methyl.
At Page 5823, First Column, second paragraph, Meanwell teaches that “Replacing hydrogen atoms with fluorine has been explored extensively in drug design, most commonly to replace those bound to an aromatic ring or in the context of a CF3 for CH3 replacement where these substitutions can modulate potency or interfere with metabolic modification.”
Applying KSR exemplary rationale B, it would have been prima facie obvious to a person having ordinary skill in the art to substitute the terminal methyl group in the compound taught by Guo for the trifluoromethyl group instantly claimed, as fluorine is known in the art to be bioisosteric to hydrogen. Motivated by the potential to modulate potency by such a substitution as taught by Meanwell, Claims 11-12 and 17-21 would have been practiced with reasonable expectation of success.
Conclusion
Claims 11-21 are rejected.
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.
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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