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 .
Application Status
The amendment filed on 5/21/2026 in response to the Notice of Non-Compliant claim amendment is acknowledged and has been entered.
Claims 64-71 and 81-87 are currently pending
In the response to the restriction requirement filed on 8/11/2025, Applicants elected the following species:
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which was maintained, but expanded to include at least
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(cmpd 163). Applicants have canceled cmpd 167 and 163 from claim 81, but have added new independent claim 87 which is directed towards compound 167. In view of Applicants substantial amendments to the claims including claim 81, the examiner expanded the search. With Compact Prosecution in mind, prior art has been found on the following species encompassed by the compound of formula I
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and
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which reads on claims 64-65, 69-71 and 82-85.
Claims 64-65, 69-71, 82-85 and 87 are currently under consideration as being drawn to the elected species or to the expanded species.
Claims 67-68, 81 and 86 have been withdrawn from examination as being drawn to a non-elected species.
Priority
Receipt is acknowledged of certified copies of papers required by 37 CFR 1.55. The current application claims priority to PCTCN2020099104 filed on 6/30/2020 and PCTCN2021075828 filed on 2/07/2021. A careful review of the priority documents did not lend support for the elected species. Accordingly, Claim 87 has been given an effective filing date of 6/30/2021 consistent with the filing of PCT/CN2021/103372.
Rejections Withdrawn:
The rejection of claims 64-84 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or a joint inventor (or for applications subject to pre-AIA 35 U.S.C. 112, the applicant), regards as the invention is withdrawn in view of Applicants amendment.
The rejection of Claim(s) 64-84 under 35 U.S.C. 102(a)(2) as being anticipated by Han et al. (US2024/0059710A1, 2024-02-22, Priority to at least PCT/CN2021/099750 filed 2021-06-11) is withdrawn in view of the cancellation of compound 163 from the claim 81.
Rejections Maintained, but amended in view of Applicants amendments:
Claim Rejections - 35 USC § 103
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 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.
This application currently names joint inventors. In considering patentability of the claims the examiner presumes that the subject matter of the various claims was commonly owned as of the effective filing date of the claimed invention(s) absent any evidence to the contrary. Applicant is advised of the obligation under 37 CFR 1.56 to point out the inventor and effective filing dates of each claim that was not commonly owned as of the effective filing date of the later invention in order for the examiner to consider the applicability of 35 U.S.C. 102(b)(2)(C) for any potential 35 U.S.C. 102(a)(2) prior art against the later invention.
Claim(s) 87 is/are rejected under 35 U.S.C. 103 as being unpatentable over Han et al. (US2024/0059710A1, 2024-02-22, Priority to at least PCT/CN2021/099750 filed 2021-06-11), as applied to claims 64-84 above.
Han et al. teach KRAS G12D inhibitors of Formula (I), a composition containing the inhibitor and uses thereof, wherein the compounds have the general structure:
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(Abstract). Specifically, Han et al. teach a KRAS G12D inhibitors including, but not limited to,
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(page 637). Moreover, Han et al. teach a pharmaceutical composition comprising the compounds in combination with a pharmaceutically acceptable excipient (paragraph 0147). With regards to the uses thereof, Han et al. teach a method of treating a subject having a disease or condition related to KRAS G12D mutant protein comprising administering to the subject a therapeutically effective amount of a compound of formula (I), wherein the disease or condition is cancer including, but not limited to, pancreatic, colorectal, endometrial and lung cancer (paragraph 0149).
Han et al. does not specifically teach the elected species
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.
It would have been prima facie obvious to one of ordinary skill in the art, prior to the effective filing date of the instantly claimed invention, to modify the compound
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taught by Han et al. to ring walk the methoxy over one carbon atom on the phenyl ring to arrive at
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. One of ordinary skill in the art would have been motivated to make such a modification, with a reasonable expectation of success, because:
Compounds which are position isomers (compounds having the same radicals in physically different positions on the same nucleus) or homologs (compounds differing regularly by the successive addition of the same chemical group, e.g., by -CH2- groups) are generally of sufficiently close structural similarity that there is a presumed expectation that such compounds possess similar properties. In re Wilder, 563 F.2d 457, 195 USPQ 426 (CCPA 1977). See also In re May, 574 F.2d 1082, 197 USPQ 601 (CCPA 1978) (stereoisomers prima facie obvious); Aventis Pharma Deutschland v. Lupin Ltd., 499 F.3d 1293, 84 USPQ2d 1197 (Fed. Cir. 2007) (5(S) stereoisomer of ramipril obvious over prior art mixture of stereoisomers of ramipril.).
In response to this rejection, Applicants contend:
“As explained by the M.P.E.P., "[t]he key to supporting any rejection under 35 U.S.C. 103 is the clear articulation of the reason(s) why the claimed invention would have been obvious." §2143. And "[s]imply stating the principle (e.g., 'art recognized equivalent,' 'structural similarity') without that providing an explanation of its applicability to the facts of the case at hand is generally not sufficient to establish a prima facie case of obviousness." §2144. “
Moreover, Applicant respectfully submits that Han does not teach or suggest modifying the cited compound to compound 167 by ring walking the methoxy group. If anything, Applicants assert that Han would have taught away from preparing compound 167 of this application since Han discloses a few hundred pages of compounds, but none of these compounds has a substitution pattern similar to that of compound 167.
These arguments have been carefully considered, but are not found persuasive.
In response to Applicants arguments, the Examiner recognizes that as explained by the MPEP, the rationale to modify or combine the prior art does not have to be expressly stated in the prior art; the rationale may be expressly or impliedly contained in the prior art or it may be reasoned from knowledge generally available to one of ordinary skill in the art, established scientific principles, or legal precedent established by prior case law. In re Fine, 837 F.2d 1071, 5 USPQ2d 1596 (Fed. Cir. 1988); In re Jones, 958 F.2d 347, 21 USPQ2d 1941 (Fed. Cir. 1992); see also In re Kotzab, 217 F.3d 1365, 1370, 55 USPQ2d 1313, 1317 (Fed. Cir. 2000) (setting forth test for implicit teachings); In re Eli Lilly & Co., 902 F.2d 943, 14 USPQ2d 1741 (Fed. Cir. 1990) (discussion of reliance on legal precedent); In re Nilssen, 851 F.2d 1401, 1403, 7 USPQ2d 1500, 1502 (Fed. Cir. 1988) (references do not have to explicitly suggest combining teachings); Ex parte Clapp, 227 USPQ 972 (Bd. Pat. App. & Inter. 1985) (examiner must present convincing line of reasoning supporting rejection); and Ex parte Levengood, 28 USPQ2d 1300 (Bd. Pat. App. & Inter. 1993) (reliance on logic and sound scientific reasoning). In the instant case, the Examiner is relying on legal precedent established by prior case law. Moreover, a review of the specification, specifically Table 2, shows that both compounds 163 and 167 inhibit Ba/F3 KRASG12D at an IC50 vale of less than or equal to 500 nM. As such, there does not appear to be some type of unexpected property associated with compound 167 as compared to compound 163 which falls in line with the case law suggesting an expectation that such compounds would possess similar properties.
Accordingly, the rejection is maintained.
New Rejections Necessitated by the Amendment:
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)(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.
Claim(s) 64-65, 69-71, 82-85 and 87 is/are rejected under 35 U.S.C. 102(a)(2) as being anticipated by Kawai et al. (US20230348495A1, 2023-11-02 with Priority to at least 2019-12-06).
Kawai et al. teach compounds having inhibitor activity against KRAS G12D mutation or a salt thereof and pharmaceutical compositions comprising the compound as an active agent (abstract). With regards to the compounds, Kawai et al teach the compounds include, but are not limited to, compounds having the formula
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and
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(Table 1 cmpds 14 and 18). With regards to the pharmaceutical composition, Kawai et al. teach that the pharmaceutical composition comprises the compound and a pharmaceutically acceptable carrier (see claim 19). Moreover, Kawai et al. teach a method of treating a tumor in a subject in need thereof comprising administering a compound, wherein the tumor includes, but is not limited to, cancer of the lung, oral cavity, prostate, stomach and breast (see claims 28-34).
Conclusion
Therefore, No claim is allowed.
Applicant's amendment necessitated the new ground(s) of rejection presented in this Office action. Accordingly, THIS ACTION IS MADE FINAL. See MPEP § 706.07(a). Applicant is reminded of the extension of time policy as set forth in 37 CFR 1.136(a).
A shortened statutory period for reply to this final action is set to expire THREE MONTHS from the mailing date of this action. In the event a first reply is filed within TWO MONTHS of the mailing date of this final action and the advisory action is not mailed until after the end of the THREE-MONTH shortened statutory period, then the shortened statutory period will expire on the date the advisory action is mailed, and any nonprovisional extension fee (37 CFR 1.17(a)) pursuant to 37 CFR 1.136(a) will be calculated from the mailing date of the advisory action. In no event, however, will the statutory period for reply expire later than SIX MONTHS from the mailing date of this final action.
Any inquiry concerning this communication or earlier communications from the examiner should be directed to BRANDON J FETTEROLF whose telephone number is (571)272-2919. The examiner can normally be reached M-F 6AM-4PM.
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 S Lundgren can be reached at 571-272-5541. The fax phone number for the organization where this application or proceeding is assigned is 571-273-8300.
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BRANDON J. FETTEROLF, PHD
Primary Patent Examiner
Art Unit 1626
/BRANDON J FETTEROLF/Primary Examiner, Art Unit 1626
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