DETAILED ACTION
Claims 1-47 are currently pending in the instant application. Claims 1-13, 16-22, 24-26, 29, and 31-37 are rejected. Claim 1 is objected. Claims 14, 15, 23, 27, 28, 30, and 38-47 are withdrawn from consideration as being for non-elected subject matter.
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 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)).
According to MPEP 803.02, the examiner has determined whether the elected species is allowable. Applicants’ elected species appears allowable. Therefore, the search and examination has been extended to the compounds:
PNG
media_image2.png
188
326
media_image2.png
Greyscale
,
PNG
media_image3.png
166
288
media_image3.png
Greyscale
,
PNG
media_image4.png
154
296
media_image4.png
Greyscale
, and
PNG
media_image5.png
154
296
media_image5.png
Greyscale
which are not allowable.
Claims 1-13, 16-22, 24-26, 29, 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.
Claim Objections
Claims 1 objected to because of the following informalities: Specifically, variable L links Ring A to the ring containing X1 and X2, therefore, variable L definitions should have two points of attachment, such as seen for:
PNG
media_image6.png
58
586
media_image6.png
Greyscale
, however,
PNG
media_image7.png
58
586
media_image7.png
Greyscale
only have one attachment shown. It is suggested that
PNG
media_image7.png
58
586
media_image7.png
Greyscale
be provided as seen on page 17, paragraph [00127] of the specification:
PNG
media_image8.png
36
654
media_image8.png
Greyscale
Appropriate correction is required.
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 1-9, 11-13, 16-22, 24-26, 29, and 37 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. Specifically, claim 1 defines X and Y as:
PNG
media_image9.png
232
590
media_image9.png
Greyscale
. wherein R16 and R17 are defined as taken together to form a ring. However, it is unclear what R16 and R17 are when X and Y are independently chosen as -C(R16)- or -C(R17)- instead of dependently choses as both -C(R16)- and -C(R17)- as there is no definition for R16 or R17 that is not in relation to the other. For example, there is no definition for R16 when X is choses as -C(R16)- and Y is -N(H)-.
Claim 36 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 must, under modern claim practice, stand alone to define an invention, and incorporation into claims by express reference to the specification is not permitted. Ex parte Fressola, 27 USPQ 2d 1608 (1993). Instant claim 36 has express reference to the Table 1 or Table 1A in the specification. It is suggested that claim 36 be amended to list the compounds from Tables 1 and Tables 1A in the claim.
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.
Claims 4 and 10 are 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 1 has the formula
PNG
media_image10.png
100
336
media_image10.png
Greyscale
wherein
PNG
media_image11.png
258
590
media_image11.png
Greyscale
and s can be 0-2 with t being 0-2. When s is 0, this provides for a ring containing X-Y-Z being a ring of at least 5 ring members up to 8 ring members, with X attached to the X1, X2 ring at the top and a carbon attached to the X1,X2 ring at the bottom. However, the formula in claim 4:
PNG
media_image12.png
108
296
media_image12.png
Greyscale
defines X, Y and Z the same as in claim 1 and defines n as 0-3. In this case, the ring containing X, Y, and Z is a ring of as low as 4 members (when n is 0 and Z is absent) and up to 8 members. A ring of 4 members for the X, Y and Z ring is outside the scope of claim 1 and therefore, claim 4 fails to limit claim 1. While claim 10 has a ring of 5-8 members for the ring containing X, Y, and Z as Z is defined as –(CH)2- or -O- in claim 10, claims 4 and claim 10 also fail to limit parent claim 1 as claim 1 requires X attached to the X1, X2 ring at the top and a carbon attached to the X1,X2 ring at the bottom, however, if n is 0 in instant claims 4 and 10, then Z is directly attached to the ring containing X1 and X2 and Z can be -O-. Z directly attached to the X1, X2 ring when Z is -O- is outside the scope of parent claim 1, and therefore claims 4 and 10 fail to limit claim 1 from which they depend. 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) 1-12, 17-22, 24-26, 31, and 37 is/are rejected under 35 U.S.C. 102(a)(1) as being anticipated by WO 2012/085166 (IDS filed 7/14/2022).
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_image13.png
140
290
media_image13.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_image14.png
92
824
media_image14.png
Greyscale
PNG
media_image15.png
70
812
media_image15.png
Greyscale
which is:
PNG
media_image4.png
154
296
media_image4.png
Greyscale
. Page 74 provides pharmaceutical compositions with solvents, excipients, auxiliary agents and carriers. The compound of example 46 corresponds to the instant formula (VI) of claims 1, 3, 5-9, 11, 12, 17-21, 24-26 :
PNG
media_image16.png
98
310
media_image16.png
Greyscale
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; X1 and X2 are each -N-; R3 is H; X is -C(O)-, Y is -C(H)2; Z is -C(H)2- or absent; t is 0 or 1; s is 0; m is 1; and R1 is C1alkyl. In regards to instant claims 6-9, while these claims further limit specific variables, these variables do not have to be present on the compounds of claims 6-9. The compound of example 46 corresponds to instant claim 2 formula (V):
PNG
media_image17.png
104
302
media_image17.png
Greyscale
wherein p is 1; R2 is C1alkyl; Ring A is (C5-C15)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- or absent; t is 0 or 1; s is 0; m is 1; and R1 is C1alkyl. The compound of example 46 corresponds to instant claims 4, 10, and 22 formula (I):
PNG
media_image18.png
110
250
media_image18.png
Greyscale
wherein p is 1; R2 is C1alkyl; Ring A is (C5-C15)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- or absent; n is 1 or 2; m is 1; and R1 is C1alkyl. The compound of example 46 corresponds to instant claim 31 formula (II):
PNG
media_image19.png
104
312
media_image19.png
Greyscale
wherein p is 1; R2 is C1alkyl; Ring A is (C5-C15)heteroaryl; ; R3 is H; n is 1; m is 1; and R1 is C1alkyl.
Claim(s) 1, 3, 5-9, 11-13, 16, 18-21, 24, 25, and 37 is/are rejected under 35 U.S.C. 102(a)(1) as being anticipated by Registry No. 1281447-73-1.
Registry No. 1281447-73-1 is:
PNG
media_image20.png
192
358
media_image20.png
Greyscale
. This compound corresponds to the instant formula (VI) of claims 1, 3, 5-9, 11-13, 16, 18-21, 24 and 25 :
PNG
media_image16.png
98
310
media_image16.png
Greyscale
wherein p is 0; Ring A is (C5-C15)heteroaryl (specifically thienyl); L is -O-(CR11R12)q; q is 1; R11 and R12 are each H; X1 and X2 are -C(R21)- and -C(R22)-; R21 and R22 are both H; R3 is H; X is -C(O)-, Y is -C(H)2; Z is -C(H)2- or absent; t is 0 or 1; s is 0; and m is 0. In regards to instant claims 5-9, while these claims further limit specific variables, these variables do not have to be present on the compounds of claims 5-9.
Registry number 1281447-73-1 is available as prior art as of 17 Apr 2011, 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_image21.png
99
480
media_image21.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. 1281447-73-1 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) 1-10, 16-22, 24, 25, and 31-37 is/are rejected under 35 U.S.C. 102(a)(1) as being anticipated by Registry No. 1927481-35-3.
Registry No. 1927481-35-3 is:
PNG
media_image22.png
172
350
media_image22.png
Greyscale
.
This compound corresponds to the instant formula (VI) of claims 1, 3, 5-9, 16-21, 24, 25 :
PNG
media_image16.png
98
310
media_image16.png
Greyscale
wherein p is 0; Ring A is (C56-C15)aryl (specifically phenyl); L is -N(R10)(CR11R12)q; q is 0; R10 is H; X1 and X2 are each -N-; R3 is H; X is -C(O)-, Y is -C(H)2; Z is -C(H)2- and t is 1 or Z is or absent and t is 2; s is 0; and m is 0. In regards to instant claims 5-9, while these claims further limit specific variables, these variables do not have to be present on the compounds of claims 5-9. The compound of Registry No. 1927481-35-3 corresponds to instant claim 2 formula (V):
PNG
media_image17.png
104
302
media_image17.png
Greyscale
wherein p is 0; Ring A is (C56-C15)aryl (specifically phenyl); 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 and t is 1 or Z is absent and t is 2; s is 0; and m is 0. The compound of Registry No. 1927481-35-3 corresponds to instant claims 4, 10, and 22 formula (I):
PNG
media_image18.png
110
250
media_image18.png
Greyscale
wherein p is 0; Ring A is (C56-C15)aryl (specifically phenyl); 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- and n is 2 or Z is absent and n is 3; and m is 0. The compound of Registry No. 1927481-35-3 corresponds to instant claim 31 formula (II):
PNG
media_image19.png
104
312
media_image19.png
Greyscale
wherein p is 0; Ring A is (C56-C15)aryl (specifically phenyl); R3 is H; n is 12; and m is 0. The compound Registry No. 1927481-35-3 corresponds to instant claims 32, 34, and 35 formula (III):
PNG
media_image23.png
104
248
media_image23.png
Greyscale
wherein p is 0; Ring A is (C56-C15)aryl (specifically phenyl); R10 is H; R3 is H; n is 2; and R4 is hydrogen. The compound of Registry no. 1927481-35-3 corresponds to instant claim 33 formula (IV):
PNG
media_image24.png
118
302
media_image24.png
Greyscale
wherein p is 0; Ring A is (C56-C15)aryl (specifically phenyl);and R4 is hydrogen. The compound of Registry no. 1927481-35-3 corresponds to instant claim 36 as Registry no. 1927481-35-3 is:
PNG
media_image25.png
160
310
media_image25.png
Greyscale
which is the same compound as the compound 0021 of Applicant’s instant Table 1A, page 41:
PNG
media_image26.png
114
460
media_image26.png
Greyscale
.
Registry number 1927481-35-3 is available as prior art as of 08 Jun 2016, 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_image21.png
99
480
media_image21.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. 1927481-35-3 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) 29 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_image13.png
140
290
media_image13.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_image14.png
92
824
media_image14.png
Greyscale
PNG
media_image15.png
70
812
media_image15.png
Greyscale
which is:
PNG
media_image4.png
154
296
media_image4.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 (VI):
PNG
media_image16.png
98
310
media_image16.png
Greyscale
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; X1 and X2 are each -N-; R3 is H; X is -C(O)-, Y is -C(H)2; Z is -C(H)2- or absent; t is 0 or 1; s is 0; m is 1; and R1 is C1alkyl. The difference between instant claim 29 and the compound of example no. 46:
PNG
media_image4.png
154
296
media_image4.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 instant claim 29 requires 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.
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_image13.png
140
290
media_image13.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
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, Joseph McKane can be reached on 571-272-0699. 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 ____________________ 5 November 2025
Rebecca Anderson
Primary Examiner
Art Unit 1626, Group 1620
Technology Center 1600