DETAILED ACTION
This office action is in response to applicant’s filing dated July 2, 2025.
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 and 28-34 are pending in the instant application. Claims 20-27 and 35-39 were previously canceled.
Election/Restrictions
Applicant’s election of Group I, drawn to a compound of formula (I) in the reply filed on July 2, 2022 is acknowledged. Because applicant did not distinctly and specifically point out the supposed errors in the restriction requirement, the election has been treated as an election without traverse (MPEP § 818.01(a)).
Claims 28-34 are withdrawn from further consideration pursuant to 37 CFR 1.142(b) as being drawn to a nonelected invention, there being no allowable generic or linking claim. Election was made without traverse in the reply filed on July 2, 2025.
Applicant’s election of Example 9, 4-(4-(3,8-diazabicyclo[3.2.1]octan-3-yl)-2-((1-(morpholinomethyl)cyclopropyl)methoxy)-5,8-dihydropyrido[3,4-d]pyrimidin-7(6H)-yl)-5-iodonaphthalen-2-ol:
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in the reply filed on July 2, 2025 is acknowledged. Because applicant did not distinctly and specifically point out the supposed errors in the restriction requirement, the election has been treated as an election without traverse (MPEP § 818.01(a)).
Example 9 is a compound of formula (I), wherein Ring A is an unsubstituted, saturated, 8-membered N-containing bridged ring which further contains a N, a piperazinyl ring-based ring; Ring B is an unsubstituted, saturated 6-membered ring having at least one N, wherein the Ring B is fused with the pyrimidine ring to form a bicyclic ring; n is 0; Y is a substituted 10-membered aromatic hydrocarbon ring, substituted with an I and OH; L is an oxygen atom; m is 1; and Z is a substituted C3 cycloalkyl substituted with a morpholinylmethyl.
Example 9 has been found free of prior art. Thus, examination has been expanded to encompass the compounds of claim 17. The compounds of claim 17 have been found to be free of art. Thus, examination has been expanded to encompass the following compound:
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Claims 1-19 are presently under examination as they relate to the elected species: Example 9:
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the compounds of claim 17, and expanded species Example 45:
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Priority
The present application is a 371 of PCT/JP2020/045146 filed on November 27, 2020, which claims benefit of foreign priority to JAPAN 2019-216165 filed on November 6, 2019 and PCTJP2019049074 filed on December 6, 2019.
Information Disclosure Statement
The information disclosure statements (IDS) submitted on December 3, 2024; December 4, 2024; and July 2, 2025 are in compliance with the provisions of 37 CFR 1.97. Accordingly, the information disclosure statements are being considered by the Examiner.
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 Objections
Claim 17 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.
Claim Rejections – Improper Markush Grouping’
The improper Markush Group Rejection is based on a judicially approved doctrine when the claim contains an improper grouping of alternatively useable species. A Markush claim contains an “improper Markush grouping” if: (1) The species of the Markush group do not share a single structural similarity,” or (2) the species do not share a common use. Members of a Markush group share a "single structural similarity” when they belong to the same recognized physical or chemical class or to the same recognized physical or chemical class or to the same art-recognized class. Members of a Markush group share a common use when they are disclosed in the specification or known in the art to be functionally equivalent (see Federal Register, Vol. 76, No. 27, Wednesday, February 9, 2011, p. 7166, left and middle columns, bridging paragraph).
Claims 1-16, 18, and 19 are rejected on the grounds of containing “improper Markush grouping”, which contains species that fail to share a single structural similarity.
Claims 1-16, 18, and 19 cite numerous compounds which encompass a wide variety of chemical species which are in different recognized physical classes, and would embrace different chemical compounds that do not share any single structural similarity between the species.
For example, Claim 1 is directed to compounds of Formula (I):
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The variables A, B, Y, and Z encompass a myriad of substituents forming heterocycles so diverse, that they will confer the above structure complete different structural and biological properties. Moreover, these variables can be substituted with any substituent which would confer the above structure with completely different structural and biological properties. For example, Ring B represents a substituted or unsubstituted, 5- to 6-membered saturated or unsaturated ring having at least one heteroatom selected from the group consisting of N, S, and 0, a 6-membered aromatic hydrocarbon ring, C3-C6 cycloalkyl ring, C3-C6 cycloalkenyl or an 8- to 10-membered spiro ring, wherein the Ring B is fused with the pyrimidine ring to form a substituted or unsubstituted bicyclic ring. Thus the core ring system in Formula I can be a pyrido[2,3-d]pyrimidine; quinazoline; pyrimido[5,4-c]pyridazine; pyrido[3,2-d]pyrimidine; pteridine; pyrimido[4,5-d]pyrimidine or a pyrimido[4,5-e][1,2,4]triazine ring system. Moreover, the core ring system in Formula (I) can be a:
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This is just a small number of examples of rings encompassed by the instant claims. Clearly, no ‘‘single structural similarity’’ can be seen. These compounds lack unity of invention since they: do not share a common utility and/or they do not share a substantial structural feature essential to that utility: In re Harnisch, 631 F.2d 716, 206 USPQ 300(CCPA 1980); and Ex parte Hozumi, 3 USPQ2d 1059 (Bd. Pat. App. & Int. 1984).
In response to this rejection, Applicant should either amend the claim(s) to recite only individual species or grouping of species that share a substantial structural feature as well as a common use that flows from the substantial structural feature, or present a sufficient showing that the species recited in the alternative of the claims(s) in fact share a substantial structural feature as well as a common use that flows from the substantial structural feature. This is a rejection on the merits and may be appealed to the Board of Patent Appeals and Interferences in accordance with 35 U.S.C. § 134 and 37 CFR41.31 (a) (1) (emphasis provided).
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.
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 1-16, 18, and 19 are rejected under 35 U.S.C. 112(a) or 35 U.S.C. 112 (pre-AIA ), first paragraph, as failing to comply with the written description requirement. The claim(s) contains subject matter which was not described in the specification in such a way as to reasonably convey to one skilled in the relevant art that the inventor or a joint inventor, or for applications subject to pre-AIA 35 U.S.C. 112, the inventor(s), at the time the application was filed, had possession of the claimed invention. This is a written description rejection.
Claim 1 recites a large genus of compounds encompassed by general formula (I) wherein
Ring A represents a substituted or unsubstituted, saturated or unsaturated 8- to 10- membered N-containing bridged ring which contains at least one further heteroatom selected from the group consisting of N, S and 0; Ring B represents a substituted or unsubstituted, 5- to 6-membered saturated or unsaturated ring having at least one heteroatom selected from the group consisting of N, S, and O, a 6-membered aromatic hydrocarbon ring, C3-C6 cycloalkyl ring, C3-C6 cycloalkenyl or an 8- to 10-membered spiro ring, Y represents a substituted or unsubstituted, 6- to 10-membered unsaturated monocyclic or bicyclic ring which contains at least one heteroatom selected from the group consisting of N, S and 0, or 6- to 10-membered aromatic hydrocarbon ring; and Z represents cyanoalkyl, alkylcarbonylaminoalkyl, alkylaminocarbonyl, alkylaminoalkyl, a substituted or unsubstituted, C3-C6 cycloalkyl, a 5- to 6-membered saturated ring which contains at least one heteroatom selected from the group consisting of N, S and O, or an 8- to 10-membered partially unsaturated ring which contains at least one heteroatom selected from the group consisting of N, S and O.
M.P.E.P. #2163 states: “An applicant shows possession of the claimed invention by describing the claimed invention with all of its limitations using such descriptive means as words, structures, figures, diagrams, and formulas that fully set forth the claimed invention....one must define a compound by ‘whatever characteristics sufficiently distinguish if. A lack of adequate written description issue also arises if the knowledge and level of skill in the art would not permit one skilled in the art to immediately envisage the product claimed from the disclosed process’.
A description of a chemical genus will usually comprise a recitation of structural features common to the members of the genus, which features constitute a substantial portion of the members of the genus, which features constitute substantial portion of the genus. See Univ. of California vs. Eli Lilly, 43 USPQ 2d 1398, 1406 (Fed. Cir. 1997). This is analogous to enablement of a genus under section 112 first, by showing enablement of a representative number of species within the genus. A chemical genus can be adequately described if the disclosure presents a sufficient number of representative species that encompass the genus. If the genus has a substantial variance, the disclosure must describe a sufficient number of species to reflect the variation within that genus.
Applicant has failed to show that he was in possession of all the diverse compounds encompassed by the general structure (I). Applicant discloses the specific structures of a very narrow set of compounds (see specification, pages 10-14, [0024]) with very few diverse set of substituents at positions Ring A, Ring B, Y, and Z, despite claiming that the groups can be substituted without specifying or limiting the type of substitution.
This small set of compounds cannot be viewed as being reasonably representative of the genus in its claimed scope because no readily apparent combination of identifying characteristics is provided, other than the disclosure of those specific species as examples of the claimed genus.
Given the broad scope of the claimed subject matter, Applicant has not provided sufficient written description that would allow the skilled in the art to recognize all the compounds of claim 1 claimed.
Claim Rejections - 35 USC § 102
In the event the determination of the status of the application as subject to AIA 35 U.S.C. 102 and 103 (or as subject to pre-AIA 35 U.S.C. 102 and 103) is incorrect, any correction of the statutory basis (i.e., changing from AIA to pre-AIA ) for the rejection will not be considered a new ground of rejection if the prior art relied upon, and the rationale supporting the rejection, would be the same under either status.
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.
Claims 1, 5-11, 18, and 19 are rejected under 35 U.S.C. 102(a)(1) as being anticipated by Fischer et al (WO 2017/201161, cited in a previous Office Action).
Regarding claims 1 and 5-11, Fischer teaches Example 45 ([ ] and Claim 85):
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Example 45 is a compound of formula (I), wherein Ring A is a substituted, saturated, 8-membered N-containing bridged ring which further contains a N, a piperazinyl ring-based ring; Ring B is an unsubstituted, saturated 6-membered ring having at least one N, wherein the Ring B is fused with the pyrimidine ring to form a bicyclic ring; n is 0; Y is a substituted 10-membered aromatic hydrocarbon ring, substituted with an OH; L is an oxygen atom; m is 0; and Z is an alkyaminoalkyl.
Regarding claim 18, Fischer teaches pharmaceutical compositions containing the compound or pharmaceutically acceptable salt thereof [0144].
Regarding claim 19, Fischer teaches a pharmaceutical composition comprising a therapeutically effective compound of Formula (I) and a pharmaceutically acceptable excipient (claim 86).
Thus, the teachings of Fischer anticipate the compounds of claims 1, 5-11, 18, and 19.
Conclusion
Claims 1-16, 18, and 19 are rejected.
Claim 17 is free of prior art.
Any inquiry concerning this communication or earlier communications from the examiner should be directed to RAYNA B RODRIGUEZ whose telephone number is (571)272-7088. The examiner can normally be reached 8am-5:00pm, Monday - Thursday.
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/Rayna Rodriguez/ Primary Examiner, Art Unit 1628
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