DETAILED ACTION
Claims 1, 5-8, 10-24, 26, 27, and 30-47are currently pending in the instant application. Claims 1, 5-8, 10-12, 16-22, 24, 26, 31, 32, 34, and 37 are rejected. Claims 13 and 33 are objected. Claims 14, 15, 23, 27, 30, and 38-47 are withdrawn from consideration as being for non-elected subject matter. Claim 36 is allowed.
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 election of Group I and the species KG-0338:
PNG
media_image1.png
108
450
media_image1.png
Greyscale
in the reply filed on 22 October 2025 has been previously acknowledged.
According to MPEP 803.02, the examiner has previously determined whether the elected species is allowable. Applicants’ elected species appears allowable. Therefore, the search and examination has been extended to the compounds of claim 13 and 33 which also appear allowable, and has previously been extended to the compound:
PNG
media_image2.png
154
296
media_image2.png
Greyscale
which is not allowable and now further to the compounds:
PNG
media_image3.png
160
326
media_image3.png
Greyscale
and
PNG
media_image4.png
194
368
media_image4.png
Greyscale
which are not allowable.
Claims 1, 5-8, 10-13, 16-22, 24, 26, and 31-37 have been examined to the extent that they are readable on the elected embodiment, the elected species and the above mentioned compounds.
Response to Amendment and Arguments
Applicant's amendment and arguments filed 10 April 2026 have been fully considered and entered into the instant application. Applicant’s amendment has overcome the objection to claim 1. Applicant’s amendment has overcome the 35 USC 112(b) rejection of claims 1-9, 11-13, 16-22, 24-26, 29 and 37 as claim 1 has been amended to remove any recitation of R16 and R17 and claims 2-4, 9, 25 and 29 have been canceled. The 35 USC 112(b) rejection of claim 36 is overcome as reference to table 1 or table 1A has been deleted. The 35 USC 112(d) rejection of claim 4 has been overcome as claim 4 has been canceled. The 35 USC 112(d) rejection of claim 10 is modified below as variable p fails to further limit the subject matter of the claim upon which it depends. The 35 USC 102(a)(1) rejection as being anticipated by WO 2012/085166 has been overcome at least as claim 1 has been amended to incorporate the subject matter of now canceled claim 29. The 35 USC 102(a)(1) rejection as being anticipated by Registry No. 1281447-73-1 has been overcome at least as claim 1 has been amended to include the subject matter of now canceled claim 29. The 35 USC 102(a)(1) rejection as being anticipated by Registry No. 1927481-35-3 has been overcome at least as claim 1 has been amended to include the subject matter of now canceled claim 29. In regards to the 35 USC 103 rejection of claim 29 as being unpatentable over WO 2012/085166, as claim 29 is canceled, the rejection is now modified as follows. Applicant argues that the skilled artisan would not be able to reasonably substituted an isomer for another structurally similar isomer and expect similar properties as compound KG-0339 of Table 1 and compound 0001 of Table 1A, which differ by the position of the F atom on the phenyl ring in the instant application have varying IC50 values as compound KG-0339 has an IC50 value of less than 1uM and compound 0001 has an IC50 value of 1uM to less than 1nM demonstrating that structurally similar isomers have different properties. This argument is not persuasive for multiple reasons. First, the rejected compound is not a positional isomer of compound KG-0339 or compound 0001. Secondly, the data provided in tables I and Tables 1A are not specific data, the IC50 values provided by “A” and “B’ are in ranges. As no exact data is provided, it is possible that compound KG-0339 could have an IC50 value of 0.99uM and compound 0001 could have an IC50 value of 1.01uM, which would be similar. Additionally, both compounds KG-039 and compound 0001 have in vitro IC50 values for the same activity which shows they possess similar properties. Compounds KG-0168-0 and KG-0166-0 provided on page 31 of the specification both have IC 50 rating of “B” and are positional isomer. Compounds 0083 and 0082 and 0083 provided on pages 49-50 of the specification both have IC50 ratings of “A” and are positional isomers. The 35 USC 103 rejection is therefore modified and maintained.
Claim Objections
Claims 13 and 33 are 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 - 35 USC § 112
The following is a quotation of 35 U.S.C. 112(d):
(d) REFERENCE IN DEPENDENT FORMS.—Subject to subsection (e), a claim in dependent form shall contain a reference to a claim previously set forth and then specify a further limitation of the subject matter claimed. A claim in dependent form shall be construed to incorporate by reference all the limitations of the claim to which it refers.
The following is a quotation of pre-AIA 35 U.S.C. 112, fourth paragraph:
Subject to the following paragraph [i.e., the fifth paragraph of pre-AIA 35 U.S.C. 112], a claim in dependent form shall contain a reference to a claim previously set forth and then specify a further limitation of the subject matter claimed. A claim in dependent form shall be construed to incorporate by reference all the limitations of the claim to which it refers.
Claim 10 is rejected under 35 U.S.C. 112(d) or pre-AIA 35 U.S.C. 112, 4th paragraph, as being of improper dependent form for failing to further limit the subject matter of the claim upon which it depends, or for failing to include all the limitations of the claim upon which it depends. Specifically, claim 10 defines p as 0, 1, 2, 3, or 4. However, claim 1, from which claim 10 depends, defines p as 1 or 2 and each occurrence of R2 is at the position meta to variable L Applicant may cancel the claim(s), amend the claim(s) to place the claim(s) in proper dependent form, rewrite the claim(s) in independent form, or present a sufficient showing that the dependent claim(s) complies with the statutory requirements.
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.
Claim(s) 1, 5-8, 16, 18, 19, 21, 22, 24, 26, and 37 is/are rejected under 35 U.S.C. 102(a)(1) as being anticipated by Registry No. 327981-55-5.
Registry No. 327981-55-5 is:
PNG
media_image5.png
196
344
media_image5.png
Greyscale
. Registry No. 327981-55-5 corresponds to applicant’s instant formula (I):
PNG
media_image6.png
88
248
media_image6.png
Greyscale
wherein, for example, R2 is halo in the position meta to variable L; p is 1; ring A is (C6-15)aryl; L is -C(O)N(R10)-; R10 is H; R3 is H; X is -C(O)-; Y is -C(H)2-; Z is absent; n is 2; m is 2; and R1 is for each occurrence (C1-C6)alkyl.
In regards to instant claims 6-8, while these claims further limit specific variables, these variables do not have to be present on the compounds of claims 6-8.
Registry number 327981-55-5 is available as prior art as of 19 March 2001, the date it was indexed into the CAplus database.
See MPEP 2128: ELECTRONIC PUBLICATIONS AS PRIOR ART Status as a "Printed Publication" An electronic publication, including an on-line database or Internet publication, is considered to be a “printed publication” within the meaning of 35 U.S.C. 102(a) and (b) provided the publication was accessible to persons concerned with the art to which the document relates. See In re Wyer, 655 F.2d 221, 227, 210 USPQ 790, 795 (CCPA 1981) Since this date represents the date that each compound entered the CAPlus database on STN, this represents the date that each compound was made accessible to the public.
The aforementioned compound anticipates the instantly claimed compounds: It is further noted that for the purposes of determining if a reference is a “printed publication” for the purposes of 102(b), MPEP 2128 states the following:
PNG
media_image7.png
99
480
media_image7.png
Greyscale
where “prior art disclosures…on an on-line database are considered to be publicly available as of the date the item was publicly posted.” Since each of the database entries above lists the date that each compound was entered into the on-line database, the compounds were made publicly available as of that date in each citation, and the claims are anticipated.
Regarding the compositions of claim 37 comprising the anticipatory compounds and a carrier, the Registry entry for Registry no. 327981-55-5 discloses a mass solubility in unbuffered water. This teaching in of water anticipates the claimed composition, wherein the compounds are present with a carrier (i.e., water).
Claim(s) 1, 5-8, 10, 11, 17-21, 24, 26, 31, 32, 34, 35, and 37 is/are rejected under 35 U.S.C. 102(a)(1) as being anticipated by Registry No. 511514-67-3 .
Registry No. 511514-67-3 is:
PNG
media_image8.png
176
344
media_image8.png
Greyscale
Registry No. 511514-67-3 corresponds to applicant’s instant formula (I):
PNG
media_image6.png
88
248
media_image6.png
Greyscale
wherein, for example, R2 is (C1-C6)alkyl in the position meta to variable L; p is 1; ring A is (C5-15)heteroaryl; L is -N(R10)(CR11R12)q; q is 0; R10 is H; R3 is H; X is -C(O)-; Y is -C(H)2-; Z is -C(H)2-; n is 1; and m is 0. Registry No. 511514-67-3 corresponds to instant claims 31, formula (II), claim 32, formula (III), and claims 34 and 35 wherein R4 is hydrogen.
In regards to instant claims 6-8, while these claims further limit specific variables, these variables do not have to be present on the compounds of claims 6-8.
Registry number 511514-67-3 is available as prior art as of 07 May 2003, the date it was indexed into the CAplus database.
See MPEP 2128: ELECTRONIC PUBLICATIONS AS PRIOR ART Status as a "Printed Publication" An electronic publication, including an on-line database or Internet publication, is considered to be a “printed publication” within the meaning of 35 U.S.C. 102(a) and (b) provided the publication was accessible to persons concerned with the art to which the document relates. See In re Wyer, 655 F.2d 221, 227, 210 USPQ 790, 795 (CCPA 1981) Since this date represents the date that each compound entered the CAPlus database on STN, this represents the date that each compound was made accessible to the public.
The aforementioned compound anticipates the instantly claimed compounds: It is further noted that for the purposes of determining if a reference is a “printed publication” for the purposes of 102(b), MPEP 2128 states the following:
PNG
media_image7.png
99
480
media_image7.png
Greyscale
where “prior art disclosures…on an on-line database are considered to be publicly available as of the date the item was publicly posted.” Since each of the database entries above lists the date that each compound was entered into the on-line database, the compounds were made publicly available as of that date in each citation, and the claims are anticipated.
Regarding the compositions of claim 37 comprising the anticipatory compounds and a carrier, the Registry entry for Registry no. 511514-67-3 discloses a mass solubility in unbuffered water. This teaching in of water anticipates the claimed composition, wherein the compounds are present with a carrier (i.e., water).
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) 1, 5-8, 10-12, 17-22, 24, 26, 31, and 37 is/are rejected under 35 U.S.C. 103 as being unpatentable over WO 2012/085166 (IDS filed 7/14/2022).
Determining the scope and contents of the prior art
WO2012/085166 discloses compounds which are mGluR5 modulators for the treatment of neurological disorders, page 1. Formula I is disclosed on page 6:
PNG
media_image9.png
140
290
media_image9.png
Greyscale
wherein R5 can be a heteroaryl. Page 10 provides wherein R5 may represent pyridyl optionally substituted with substituents such as C1-6alkyl. A specific compound disclosed is the compound 46, page 74:
PNG
media_image10.png
92
824
media_image10.png
Greyscale
PNG
media_image11.png
70
812
media_image11.png
Greyscale
which is:
PNG
media_image12.png
154
296
media_image12.png
Greyscale
. Page 74 provides pharmaceutical compositions with solvents, excipients, auxiliary agents and carriers.
Ascertaining the differences between the prior art and the claims at issue
The compound of example no. 46 of the WO2012/085166 corresponds to the compound of instant claim 1 formula (I):
PNG
media_image6.png
88
248
media_image6.png
Greyscale
, for example, wherein p is 1; R2 is C1alkyl; Ring A is (C5-C15)heteroaryl (specifically pyridinyl); L is -N(R10)(CR11R12)q; q is 0; R10 is H; R3 is H; X is -C(O)-, Y is -C(H)2; Z is absent or -C(H)2-; n is 1 or 2; m is 1; and R1 is C1alkyl. The difference between the instantly rejected claims and the compound of example no. 46:
PNG
media_image12.png
154
296
media_image12.png
Greyscale
is that example no. 46 corresponds to wherein p is 1 and the occurrence of R2 is at the position para to variable L whereas the instant claims require wherein p is 1 or 2, and each occurrence of R2 is at the position meta to variable L. The difference is one of position of the alkyl group on the pyridinyl ring, positional isomerism. In regards to instant claims 6-8, while these claims further limit specific variables, these variables do not have to be present on the compounds of claims 6-8.
Resolving the level of ordinary skill in the pertinent art and Considering objective evidence present in the application indicating obviousness or nonobviousness.
The level of ordinary skill in the art is that nothing unobvious is seen in substituting the known claimed isomer for the structurally similar isomer, as taught by the prior art reference, since such structurally related compounds suggest one another and would be expected to share common properties absent a showing of unexpected results. In re Norris, 84 USPQ 458 (1950). Additionally, please see MPEP 2144.09, Compounds which are position isomers (compounds having the same radicals in physically different positions on the same nucleus) 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). Lastly, WO2012/085166 discloses preferences towards R5 of formula I, disclosed on page 6:
PNG
media_image9.png
140
290
media_image9.png
Greyscale
wherein R5 can be a heteroaryl, to be pyridyl optionally substituted with substituents such as C1-6alkyl, page 10, which would direct one to prepare additional compounds which would be expected to share common properties absent a showing of unexpected results.
Conclusion
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 REBECCA L ANDERSON whose telephone number is (571)272-0696. The examiner can normally be reached Monday-Friday from 6am-2pm.
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, Andrew Kosar can be reached at 571-272-0913. The fax phone number for the organization where this application or proceeding is assigned is 571-273-8300.
Information regarding the status of published or unpublished applications may be obtained from Patent Center. Unpublished application information in Patent Center is available to registered users. To file and manage patent submissions in Patent Center, visit: https://patentcenter.uspto.gov. Visit https://www.uspto.gov/patents/apply/patent-center for more information about Patent Center and https://www.uspto.gov/patents/docx for information about filing in DOCX format. For additional questions, contact the Electronic Business Center (EBC) at 866-217-9197 (toll-free). If you would like assistance from a USPTO Customer Service Representative, call 800-786-9199 (IN USA OR CANADA) or 571-272-1000.
/REBECCA L ANDERSON/Primary Examiner, Art Unit 1626 ____________________ 26 June 2026
Rebecca Anderson
Primary Examiner
Art Unit 1626, Group 1620
Technology Center 1600
Prosecution Insights