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 .
Election/Restrictions
Applicant’s response without traverse to the restriction/ election requirement from 2/20/2026 is acknowledged. Applicant has made the following Group election: Group I, drawn to claims 1-21 and 23 drawn to a compound of Formula I. Applicant has designated claims 1, 4-7, 17 and 23 to read on elected Group I. Applicant has further elected the following species.
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It appears that the description pertaining to claims 1, 4-7, 17 and 23 is a description of the claims, which read on the elected species, just placed in a different portion of the response. The restriction/ election requirement is hereby MADE FINAL. Claims 1, 4-7, 17 and 23 are pending, and have been examined herewith to the extent of Applicant’s elected species of compound. Claims 2, 3, 8-16 and 18-21 are withdrawn from consideration as directed a non-elected invention.
Claim Rejections - 35 USC § 112
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 5 is 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.
Claims 5 depends from claim 1, but have no antecedent basis for the limitation R5 from it.
In the interest of compact prosecution, the Examiner determines that the depicted compound is where in the place of G1, the ring depicts CH, and G1 is
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.
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.
Claims 1, 4-7, 17 and 23 are rejected under 35 U.S.C. 103 as being unpatentable over Muñoz et al., Facilitating Compound Entry as a Means to Discover Antibiotics for Gram-Negative Bacteria, Acc Chem Res, 2021 Mar 16;54(6):1322-1333, Epub 2021 Feb 26 (“Muñoz”, of record), further in view of US 2009/0156578 A1 to Pauls et al. (“Pauls”).
Muñoz describes the discovery and successful applications of a promising strategy for enhancing the accumulation of Gram-positive-only antibiotics as a means of imbuing compounds with broad-spectrum activity. Per Muñoz, “we describe a set of important criteria to consider when selecting candidate Gram-positive-only antibiotics for conversion to Gram-negative-active versions via the eNTRy rules. As detailed herein, using this blueprint the spectrum of activity was expanded for three antibiotic classes that engage three different biological targets: DNA gyrase inhibitor 6DNM, FabI inhibitor Debio-1452, and FMN riboswitch inhibitor Ribocil C.” (Abstract). See cf Figure 3.
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Muñoz describes the importance of having a primary amine for accumulation in E. coli, with charge on the amine being a primary factor in accumulating- as in the compound above.
It is noted that Debio-1452-NH3 describes a compound, only charged, as in Applicant’s claim 7.1 However, the description of a primary amine underneath the compound also describes the same compound as in Applicant’s claim 7.2
Muñoz does not specifically disclose a F substitution on the methylbenzofuran ring, as in Applicant’s elected species of compound. It is noted, however, that H versus F substitution is a well known bioisostere substitution in the art. Further, there is art on compounds with the general structure of Formula (I), which are designated to have this F substitution, as further disclosed in Pauls.
Regarding claims 1 and 6, Pauls teaches a fab1 inhibitor (para [0007], [0531]) compound of formula I or a salt thereof, wherein G1 is CH2; Q is CHRa, where Ra is H; X is C=O; R1 is H; R2 is C1-alkyl; R3 is H and R4 is methyl (para [0825], Example 76).
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Regarding claim 23, Pauls further teaches treating a subject with a bacterial illness by way of targeting bacterial enzymes. (Abstract, [0004-5]).3
Pauls further discloses stereoisomers of the compounds. ([0045], [0086]).
Pauls further a broader structure, wherein, as in Applicant’s elected species a F substitution can be made.
Namely, this is Applicant’s elected species with the F depicted.
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This is the broader structure of Pauls:
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Claim 2 recites A, where R8 can be F, and L can be O.
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Accordingly, it would have been obvious to a person of skill in the art before the effective filing date of the claimed invention to combine the teachings of Muñoz and Pauls in order to practice Applicant’s claimed invention with a reasonable expectation of success. The skilled artisan would have been motivated to do so because Applicant’s claimed species is disclosed as nearly the same compound in Muñoz, which further specifically outlines the benefit of a primary amino group in the structure for having antibacterial activity. The skilled artisan would have been further motivated to modify the compound with an F substitution on the methylbenzofuran ring, as in Applicant’s elected species of compound. Motivation to do so is because H versus F substitution is a well-known bioisostere substitution in the art. Further, Pauls further teaches compounds with the general structure of Formula (I), which are designated to have this F substitution.
Other relevant art
The Examiner also notes that references in the various PCT search reports disclose relevant art with compounds within the broader scope of claim 1. As does art from Applicant’s IDS, e.g. WO 2020/099341 A1 to Gerusz et al. (“Gerusz”, of record).
Gerusz relates to antibiotic compounds for the treatment of N. gonorrhoeae infections and related infections of Formula (I). (Abstract).
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Within this formula is also formula IV.
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Per the definition of substituents:
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(p. 4-6).
This encompasses a compound of Applicant’s claim 1.
Any inquiry concerning this communication or earlier communications from the examiner should be directed to SVETLANA M IVANOVA whose telephone number is (571)270-3277. The examiner can normally be reached 8:30-5:00.
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, Kortney L. Klinkel can be reached at (571) 270-5239. The fax phone number for the organization where this application or proceeding is assigned is 571-273-8300.
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/SVETLANA M IVANOVA/ Primary Examiner, Art Unit 1627
1 It is noted that claims 1, 5-7 and 23, although not for Applicant’s elected species for which an obviousness rejection applies, are otherwise rejectable under 35 U.S.C. 102(a)(1) as being anticipated by Muñoz et al., Facilitating Compound Entry as a Means to Discover Antibiotics for Gram-Negative Bacteria, Acc Chem Res, 2021 Mar 16;54(6):1322-1333, Epub 2021 Feb 26 (“Muñoz”, of record).
2 It is further similar to Applicant’s non-elected claim 8, where the individual non-charged isomers have been claimed, further in view of Pauls, which teaches stereoisomers of the compounds.
3 It is noted that claims 1, 6 and 23, although not for Applicant’s elected species for which an obviousness rejection applies, are otherwise rejectable under 35 U.S.C. 102(a)(1) and 35 U.S.C. 102(a)(2) as being anticipated by US 2009/0156578 A1 to Pauls et al. (“Pauls”).
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