DETAILED ACTION
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 the Claims and Response to Amendment
The amendments filed on June 9, 2026 have been entered. Claims 1, 2, 5-11, 19, and 21-39 are pending. Claims 3, 4, 12-18, and 20 are cancelled. Note: previously withdrawn claims (i.e., claims 14-18) as a result of a restriction requirement (dated October 24, 2025) are now cancelled.
Withdrawn Rejections/Objections
Applicant is notified that any outstanding rejection/objection that is not expressly maintained in this office action has been withdrawn or rendered moot in view of applicant's amendments and/or remarks.
Status of Priority
The present application claims priority to U.S. Provisional Application No. 63/356,670, filed on June 29, 2022.
Specification - Disclosure
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 errors of which applicant may become aware in the specification.
Claim Objections
Claims 23 and 28 are objected to because of the following informalities:
For consistency and to avoid 112 issues, in claims 23 and 28:
“…substituted with C1-3 alkyl or (C1-3 alkylene)OH” should read“…substituted with 1 or 2 groups selected, independently, from C1-3 alkyl
Appropriate correction is required.
Claim Rejections - 35 USC § 112(d)
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 10, 23, 28, and 38 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.
Regarding claim 10:
Claim 10 recites the following compound:
“
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” wherein R1 of this compound is Et (i.e., a C2 alkyl). Claim 10 is dependent on claim 2 which specifically states that “R1 is H, F, Cl, Br, or C3-7 cycloalkyl.” According to claim 2, R1 cannot be a C2 alkyl group. Therefore, claim 10 is in improper dependent form for failing to further limit the subject matter of the claim upon which it depends and, instead, broadens the scope of claim 2.
Regarding claims 23 and 28:
Claims 23 and 28 state that R2 can be a C3-4 heteroaryl comprising, independently, one or two heteroatoms independently selected from O, S, or N and substituted with C1-3 alkyl or (C1-3 alkylene)OH. Claims 23 and 28 are dependent on claims 22 and 27, respectively, which specifically states that R2 can be a C2-5 heteroaryl comprising, independently, one or two heteroatoms independently selected from O, S, or N and substituted with 1 or 2 groups selected, independently from C1-6 alkyl. Claims 22 and 27 do not state that the substituent(s) can be a (C1-3 alkylene)OH. Therefore, claims 23 and 28 are in improper dependent form for failing to further limit the subject matter of the claim upon which it depends and, instead, broadens the scope of claims 22 and 27, respectively.
Regarding claim 38:
Claim 38 states that R1 is CH3 or CH2CH3. Claim 38 is dependent on claim 1 which explicitly states that R1 is H, CN, halogen, O-(C1-6 alkyl), or C3-7 cycloalkyl. Claim 1 does not state that R1 can be C1-2 alkyl. Therefore, claim 38 is in improper dependent form for failing to further limit the subject matter of the claim upon which it depends and, instead, broadens the scope of claim 1.
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.
Note on 35 USC § 102 and § 103 Rejections
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.
Claim Rejections - 35 USC § 102
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.
(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.
Rejection Part 1:
Claims 1 and 5 are rejected under 35 U.S.C. 102(a)(1) as being anticipated by:
Cai et al. (Cai) (WO 2009/152325 A1; published December 17, 2009).
Cai discloses diamino-pyridine, pyrimidine and pyridazine compounds which may be used as H4 receptor modulators (abstract). One of the compounds disclosed by Cai is the following compound:
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(see Cai, pg. 242, lines 14-15) which is encompassed by instant claims 1 and 5 wherein:
R1 = R4 = R5 = H
R2 = unsubstituted C5 heterocyclyl (i.e., tetrahydropyranyl)
R3 = NH(C1-6 alkyl) (i.e., NHMe).
Rejection Part 2:
Claims 1, 5-7, 11, and 21 are rejected under 35 U.S.C. 102(a)(2) as being anticipated by
Ellis et al. (Ellis) (WO 2023/279105 A1; filed on July 1, 2022; published January 5, 2023; claims priority to U.S. Provisional Application No. 63/217,607, filed on July 1, 2021 – Effective filing date of prior art is July 1, 2021).
Ellis discloses compounds that are useful as inhibitors of kinases, including JAK proteins (para. 0009). One of the compounds disclosed by Ellis has the following structure (herein, referred to as compound E166; pg. 75, last compound of table):
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.
Compound E166 is encompassed by instant claims 1, 5-7, 11, and 21 wherein:
R1 = C3 cycloalkyl (i.e., cyclopropyl)
R2 = C3 heterocyclyl (i.e., isothiazolyl) substituted with one C1 alkyl group
R3 = (C1-3 alkylene)-CN (i.e., CH2CN)
R4 = R5 = H.
Rejection Part 3:
Claims 31, 33, 34, and 38 are rejected under 35 U.S.C. 102(a)(2) as being anticipated by
Ellis et al. (Ellis) (WO 2023/279105 A1; filed on July 1, 2022; published January 5, 2023; claims priority to U.S. Provisional Application No. 63/217,607, filed on July 1, 2021 – Effective filing date of prior art is July 1, 2021).
Ellis discloses compounds that are useful as inhibitors of kinases, including JAK proteins (para. 0009). One of the compounds disclosed by Ellis has the following structure (herein, referred to as compound E6; pg. 26, first compound of table):
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.
Compound E6 is encompassed by instant claims 31, 33, 34, and 38 wherein:
R1 = C1 alkyl (i.e., Me)
R2 = C3 heterocyclyl (i.e., isothiazolyl) substituted with one C1 alkyl group
R3 = (C1-3 alkylene)-CN (i.e., CH2CN)
R4 = R5 = H.
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.
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.
Rejection Part 1:
Claims 1, 2, 5-9, 11, 19, and 21 are rejected under 35 U.S.C. 103 as being unpatentable over:
Ellis et al. (Ellis) (WO 2023/279105 A1; filed on July 1, 2022; published January 5, 2023; claims priority to U.S. Provisional Application No. 63/217,607, filed on July 1, 2021 – Effective filing date of prior art is July 1, 2021).
Ellis discloses compounds that are useful as inhibitors of kinases, including JAK proteins (para. 0009). One of the compounds disclosed by Ellis has the following structure (herein, referred to as compound E246; see pg. 118, 2nd to last row, 1st compound):
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. E246 is very similar to the structure of a species encompassed by instant claims 1, 2, 5-9, 11, 19, and 21 as shown below:
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wherein:
R1 = Cl,
R2 = C3 heterocyclyl (i.e., pyrazolyl) substituted with a C1 alkyl group,
R3 = a C7 heterocycloalkyl (i.e.,
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),
R4 = (C1-6 alkylene)CN (i.e., CH2CN), and
R5 = H.
The main difference between the two structures is that the -CH2CN group in compound E246 is geminal to the C7 heterocyclic group whereas in the instant species, the -CH2CN group is bonded to the carbon atom that is adjacent to the carbon atom that is bonded to the same C7 heterocyclic group.
Compound E246 and the instant species are position isomers of each other.
According to MPEP 2144.09:
I. REJECTION BASED ON CLOSE STRUCTURAL SIMILARITY IS FOUNDED ON THE EXPECTATION THAT COMPOUNDS SIMILAR IN STRUCTURE WILL HAVE SIMILAR PROPERTIES
A prima facie case of obviousness may be made when chemical compounds have very close structural similarities and similar utilities. "An obviousness rejection based on similarity in chemical structure and function entails the motivation of one skilled in the art to make a claimed compound, in the expectation that compounds similar in structure will have similar properties." In re Payne, 606 F.2d 303, 313, 203 USPQ 245, 254 (CCPA 1979). See In re Papesch, 315 F.2d 381, 137 USPQ 43 (CCPA 1963) (discussed in more detail below) and In re Dillon, 919 F.2d 688, 16 USPQ2d 1897 (Fed. Cir. 1990) (discussed below and in MPEP § 2144) for an extensive review of the case law pertaining to obviousness based on close structural similarity of chemical compounds. See also MPEP § 2144.08, subsection II.A.4.(c).
II. HOMOLOGY AND ISOMERISM ARE FACTS WHICH MUST BE CONSIDERED WITH ALL OTHER RELEVANT FACTS IN DETERMINING OBVIOUSNESS
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.).
The instant specification does not provide any in vitro or in vivo data demonstrating that the claimed compounds exhibit properties that are unexpected relative to the structurally similar position isomers disclosed in Ellis. The instant specification only provides a general reaction scheme (see instant Figure 1) and a general procedure for how to conduct ROCK and JAK assays (see instant Example 1). In the absence of evidence indicating unpredictability or a demonstrated difference in activity, it is reasonable to presume that the claimed compounds would be expected to exhibit properties similar to their corresponding position isomers disclosed in Ellis, thus motivating a POSITA to explore such position isomers as disclosed in the instant case. Hence, instant claims 1, 2, 5-9, 11, 19, and 21 are considered obvious.
Rejection Part 2:
Claims 31-39 are rejected under 35 U.S.C. 103 as being unpatentable over:
Ellis et al. (Ellis) (WO 2023/279105 A1; filed on July 1, 2022; published January 5, 2023; claims priority to U.S. Provisional Application No. 63/217,607, filed on July 1, 2021 – Effective filing date of prior art is July 1, 2021).
Ellis discloses compounds that are useful as inhibitors of kinases, including JAK proteins (para. 0009). One of the compounds disclosed by Ellis has the following structure (herein, referred to as compound E111a; see pg. 95):
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. Ellis demonstrates that compound E111a can inhibit TYK2 and JAK1 with an IC50 of less than 10 nM for both. The structure of compound E111a is very similar to the structure of the compound of instant claim 37):
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. The main difference between the two structures is that the -CH2CN group in compound E111a is geminal to the heterocyclic group whereas in the compound of instant claim 37, the -CH2CN group is bonded to the carbon atom that is adjacent to the carbon atom that is bonded to the same heterocyclic group.
Compound E111a and the compound of instant claim 37 are position isomers of each other.
According to MPEP 2144.09:
I. REJECTION BASED ON CLOSE STRUCTURAL SIMILARITY IS FOUNDED ON THE EXPECTATION THAT COMPOUNDS SIMILAR IN STRUCTURE WILL HAVE SIMILAR PROPERTIES
A prima facie case of obviousness may be made when chemical compounds have very close structural similarities and similar utilities. "An obviousness rejection based on similarity in chemical structure and function entails the motivation of one skilled in the art to make a claimed compound, in the expectation that compounds similar in structure will have similar properties." In re Payne, 606 F.2d 303, 313, 203 USPQ 245, 254 (CCPA 1979). See In re Papesch, 315 F.2d 381, 137 USPQ 43 (CCPA 1963) (discussed in more detail below) and In re Dillon, 919 F.2d 688, 16 USPQ2d 1897 (Fed. Cir. 1990) (discussed below and in MPEP § 2144) for an extensive review of the case law pertaining to obviousness based on close structural similarity of chemical compounds. See also MPEP § 2144.08, subsection II.A.4.(c).
II. HOMOLOGY AND ISOMERISM ARE FACTS WHICH MUST BE CONSIDERED WITH ALL OTHER RELEVANT FACTS IN DETERMINING OBVIOUSNESS
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.).
The instant specification does not provide any in vitro or in vivo data demonstrating that the claimed compounds exhibit properties that are unexpected relative to the structurally similar position isomers disclosed in Ellis. The instant specification only provides a general reaction scheme (see instant Figure 1) and a general procedure for how to conduct ROCK and JAK assays (see instant Example 1). In the absence of evidence indicating unpredictability or a demonstrated difference in activity, it is reasonable to presume that the claimed compounds would be expected to exhibit properties similar to their corresponding position isomers disclosed in Ellis, thus motivating a POSITA to explore such position isomers as disclosed in the instant case. Hence, instant claims 31-39 are considered obvious.
Double Patenting
The nonstatutory double patenting rejection is based on a judicially created doctrine grounded in public policy (a policy reflected in the statute) so as to prevent the unjustified or improper timewise extension of the “right to exclude” granted by a patent and to prevent possible harassment by multiple assignees. A nonstatutory double patenting rejection is appropriate where the conflicting claims are not identical, but at least one examined application claim is not patentably distinct from the reference claim(s) because the examined application claim is either anticipated by, or would have been obvious over, the reference claim(s). See, e.g., In re Berg, 140 F.3d 1428, 46 USPQ2d 1226 (Fed. Cir. 1998); In re Goodman, 11 F.3d 1046, 29 USPQ2d 2010 (Fed. Cir. 1993); In re Longi, 759 F.2d 887, 225 USPQ 645 (Fed. Cir. 1985); In re Van Ornum, 686 F.2d 937, 214 USPQ 761 (CCPA 1982); In re Vogel, 422 F.2d 438, 164 USPQ 619 (CCPA 1970); In re Thorington, 418 F.2d 528, 163 USPQ 644 (CCPA 1969).
A timely filed terminal disclaimer in compliance with 37 CFR 1.321(c) or 1.321(d) may be used to overcome an actual or provisional rejection based on nonstatutory double patenting provided the reference application or patent either is shown to be commonly owned with the examined application, or claims an invention made as a result of activities undertaken within the scope of a joint research agreement. See MPEP § 717.02 for applications subject to examination under the first inventor to file provisions of the AIA as explained in MPEP § 2159. See MPEP § 2146 et seq. for applications not subject to examination under the first inventor to file provisions of the AIA . A terminal disclaimer must be signed in compliance with 37 CFR 1.321(b).
The filing of a terminal disclaimer by itself is not a complete reply to a nonstatutory double patenting (NSDP) rejection. A complete reply requires that the terminal disclaimer be accompanied by a reply requesting reconsideration of the prior Office action. Even where the NSDP rejection is provisional the reply must be complete. See MPEP § 804, subsection I.B.1. For a reply to a non-final Office action, see 37 CFR 1.111(a). For a reply to final Office action, see 37 CFR 1.113(c). A request for reconsideration while not provided for in 37 CFR 1.113(c) may be filed after final for consideration. See MPEP §§ 706.07(e) and 714.13.
The USPTO Internet website contains terminal disclaimer forms which may be used. Please visit www.uspto.gov/patent/patents-forms. The actual filing date of the application in which the form is filed determines what form (e.g., PTO/SB/25, PTO/SB/26, PTO/AIA /25, or PTO/AIA /26) should be used. A web-based eTerminal Disclaimer may be filled out completely online using web-screens. An eTerminal Disclaimer that meets all requirements is auto-processed and approved immediately upon submission. For more information about eTerminal Disclaimers, refer to www.uspto.gov/patents/apply/applying-online/eterminal-disclaimer.
Claims 1, 2, 5-9, 11, 19, 21, and 31-39 are provisionally rejected on the ground of nonstatutory double patenting as being unpatentable over:
claims 1-4, 7-11, 13, 28-32 of U.S. Patent Application No. 18/573,305 (‘305)
Note: ‘305 claims priority to U.S. Provisional Application No. 63/217,607, filed on July 1, 2021, which is the same U.S. Provisional Application No. that Ellis [reference cited in 102 and 103 rejections above] claims priority to.
Although the claims at issue are not identical, they are not patentably distinct from each other because there is:
overlap between the instant claims and the claim set from the co-pending application (see “Claim Rejections - 35 USC § 102 – Rejection Parts 2 and 3” for an example of a compound encompassed by both claim sets) and
the compounds claimed in the co-pending application are obvious homologs of the compounds claimed in the present application (see “Claim Rejections - 35 USC § 103 – Rejection Parts 1 and 2” for details).
Allowable subject matter
Claims 22, 24-27, 29, and 30 are allowed.
Conclusion
Claims 1, 2, 5-11, 19, 21, 23, 28 and 31-39 are rejected. Claims 22, 24-27, 29, and 30 are allowed.
THIS ACTION IS MADE FINAL. 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 KRISTEN ROMERO whose telephone number is (571)272-6478. The examiner can normally be reached M-F 9:30 AM - 6:00 PM ET.
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If attempts to reach the examiner by telephone are unsuccessful, the examiner’s supervisor, JEFFREY H. MURRAY can be reached at (571) 272-9023. The fax phone number for the organization where this application or proceeding is assigned is 571-273-8300.
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/KRISTEN W ROMERO/Examiner, Art Unit 1624
/JEFFREY H MURRAY/Supervisory Patent Examiner, Art Unit 1624
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