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 .
DETAILED ACTION
Response to Amendment
Acknowledgment is made of the receipt and entry of the amendment filed on 02/17/2026, wherein independent claim 1 is amended to recite NR4R5 as a optionally substituted piperidinyl ring wherein Q1 is CH2, CHR10c or C(R10c)2, claims 5-11, 18, and 19 are cancelled, and new claims 25- 36 are added.
Election/Restriction
Applicant elected with travers: i) Group I; ii) compound species, Example 6, in the reply filed on 09/23/2025.
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The Restriction Requirement is made FINAL in last office action mailed on 11/14/2025. Claims 20-24 remain withdrawn from further consideration pursuant to 37 CFR 1.142(b), as being drawn to a nonelected invention.
New claims 26, 28, 33 and 35-36 read on the elected compound species.
It’s noted the amended claim 3, 4 and 13 do not read on the elected compound species. New claims 25, 27, 29-32 and 34 do NOT read on the elected compound species. Claims 3, 4, 13, 25, 27, 29-32 and 34 are withdrawn from further consideration pursuant to 37 CFR 1.142(b), as being drawn to a nonelected species.
The elected species, Example 6 ( CAS# 2760428-44-0, entered STN database on Feb 23, 2022) , is free of anticipatory prior art. Claim 1 is amended to recite a optionally substituted piperidinyl ring wherein Q1 is CH2, CHR10c or C(R10c)2. Claim 16 is amended to remove compound species comprising other ring moiety, including the expanded searched non-elected compound species, (3R)-3-cyano-N-[4-(3-cyanophenyl)-5-(2,6-dimethyl-4-pyridyl)thiazol-2-yl ]pyrrolidine- 1-carboxamide (compound 4.10 disclose by instant specification in Table EX 4 ), wherein Rx is methyl, R1 is methyl, R2 and R3 are both hydrogen, R4 and R5 form pyrrolidinyl ring, R10c is CN.
To expedite compact prosecution, the examiner expanded the search/ reconsideration for non-elected compound recited in claim 16 and non-elected compound species, wherein Rx is methyl, R1 is methyl, R2, R3 an d R6 are hydrogen, Q1 is CH2 . It should be noted that prior art search will not be extended unnecessarily to cover all non-elected species. Other non-elected species are withdrawn from further consideration pursuant to 37 CFR 1.142(b) as being drawn to a non-elected species. Claims 1-2, 12, 14-15, 17, 26, 28, 33 and 35-36 are rejected under 35 U.S.C. 103 as being unpatentable over Ohkawa, in view of Press and Bloomfield on the record and made final.
Status of Claims
Claims 1-4, 12-17, and 20-36 are pending in the instant application.
Claims 3, 4, 13, 20-24, 25, 27, 29-32 and 34 are withdrawn.
Claims 1-2, 12, 14-17, 26, 28, 33 and 35-36 are currently under examination in this office action.
Priority
This instant application 18/018,741 filed on 01/30/2023, is a 371 of PCT/GB2021/051984 filed 07/30/2021, which claims the benefit of priority to foreign application of United Kingdom GB 2011996.2 filed on 07/31/2020.
Acknowledgment is made of applicant’s claim for foreign priority under 35 U.S.C. 119 (a)-(d). The certified copy of foreign application GB 2011996.2 is filed on 01/30/2023.
Information Disclosure Statement
The information disclosure statements filed on 11/21/2025 is in compliance with the provisions of 37 CFR1.97. Accordingly, the reference listed in IDS are being considered by the Examiner. Reference written in foreign language is considered to the degree of English abstract or patent family of foreign patent by Examiner. It’s noted that IDS filed 01/30/2023, 02/17/2023, 02/23/2024, 06/20/2024, 10/18/2024, 12/03/2024, 01/06/2025, 02/12/2025, 04/18/2025 lack the appropriate size fee assertion.
Action Summary/ Response to Argument
Applicant’s Remarks filed 02/17/2026 have been fully considered. Any objections and rejections found in the previous Office Action and not repeated herein has been withdrawn in response to amendments and Applicant's remarks. The text of those sections of Title 35 U.S. Code not included in this action can be found in a prior Office action.
Applicant’s arguments with respect to rejections under 35 U.S.C. § 103 have been fully considered. Claim 16 is amended to recite compound species comprising substituted piperidinyl rings as NR4R5 in combination with specified R groups that are supported by instant disclosure (See Table Ex 3-6). The bioisosteric modification from prior art to the compound species of claim 16 based on structural similarity and SAR study might be achievable, but might require higher level than ordinary skill in the art. Instant specification (See Table1) disclosed compounds species with reasonable adenosine receptor A2A activity that are not expected by prior art. Thus, claim 16 is non-obvious in light of prior art.
However, claim 1 is still directed to variety of compound of Formula I, wherein Q1 is CH2, which is considered as obvious based on the combined teaching of Ohkawa, Press and Bloomfield. Claim 1 reciting R10C is a group of formula L-Z wherein Z is any heterocyclyl or heteroaryl is broad. Applicant is advised to further amend claim 1 to compound species that commensurate with the scope of instant disclosure.
Specification
Acknowledgement is made of amended specification filed on 02/17/2026 wherein multiple “R2a and R2b” are replaced with “R8a and R8b”. Compound of Formula I recite vast variety of numbered groups/moieties, e.g. L, L1, L1a, L1b, Z, Z1, Ra, Ra1, R1A, Ra2, R2a, Rb, Rb1, Rb2, Rc-f, etc. The Applicant is advised to carefully check the typo error in the definition of variety of moieties and R groups.
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 non-obviousness.
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.
Claims 1-2, 12, 14-15, 17, 26, 28, 33 and 35-36 are rejected under 35 U.S.C. 103 as being unpatentable over Ohkawa et al. (US 2005/0080113 A1, hereafter Ohkawa’ 113, Applicant’s IDS dated 01/30/2023), in view of Press et al.( US20090233938A1, family member of WO 2005/070926 A1, Applicant’s IDS dated 01/30/2023) and Bloomfield et al. (US 2011/0124624 A1).
Ohkawa’113 teaches variety of 1,3-thiazole derivatives comprising substituted pyridyl and phenyl moieties as p38 MAP kinase and/or TNF-C inhibitor and method of treating disease/disorder associated with p38 MAP and/or P450 inhibition (e.g. inflammatory disease) (See abstract, [0002], [0045]-[0052], [0086]-[0091], [0220]- [0298] , Examples 1-113, Table 1 to Table 79, claims 1-26). For example,
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Regarding R group on pyridyl moiety of instant claims 2-6, Ohkawa’113 teaches pyridyl group optionally having 1 or 2 substituents, e.g. C1-6 alkyl (e.g. methyl), hydroxy, etc. (See [0352]). The unsubstituted pyridyl moiety would read on instant claims 5 and 6 wherein both R2 and R3 are hydrogen. Ohkawa’113 teaches embodiments comprising methyl pyridyl group(See Example 7-7, 8 in Table 56-57). that would read on instant Rx is Me, R1 and R3 is H or CH3.
Ohkawa’113 teaches R1 could be aryl group, heterocyclic group, amino group, etc. with further substituent (See [0341]-[0347]).
Regarding instant
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, Ohkawa’113 teaches R1 is amino group substituted with carbonyl or carbamoyl groups (See [0347])
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Ohkawa’113 teaches compound species comprising substituted pyridine, phenyl, NHCO-heterocycle or NHCONHAr moieties that are similar to instant compound of Formula I, for example, 23-247, 23-296, 23-297, etc.
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Ohkawa’113 collectively teaches 4-phenyl-5-pyridyl-thiazole derivatives comprising pyridyl, phenyl and NHCONH moiety that are very similar to core structure of instant compound of Formula I.
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Ohkawa’113 is silent about 1,3-thiazole derivatives comprising 3-CN phenyl moiety and R4/R5 moiety wherein R4 and R5 together with the nitrogen atom to which they are attached form a heterocyclic ring.
Press teaches thiazole derivatives, compound of Formula I, as adenosine A2B receptor antagonist for treatment of inflammatory disease or other conditions related to adenosine receptor(See abstract, [0002], [0040]-[0046], Examples 1-12, claims 1-13).
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Press teaches Ar is phenyl preferably substituted with cyano group (See [ 0015]) and compound species comprising 3-cyanophenyl moiety (See Examples 1-12) (which reads on instant claimed 3-cyanophenyl moiety on the thiazole ring).
Regarding instant claimed
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moiety wherein R4 and R5 together with the nitrogen atom to which they are attached forma heterocyclic ring, Press teaches NR1R2 embodiments comprising CONR3R4 as R2, wherein R3 and R4 together with the nitrogen atom to which they are attached form a 5- or 6- membered heterocyclic group (See [0002]).
Regarding Q1. Press explicitly teaches R3 and R4 together with the nitrogen atom to which they are attached may form a 5-membered heterocyclyl group such as pyrrolyl or pyrrolidinyl or a 6-membered heterocyclyl group such as pyridyl, piperidyl, piperazinyl or morpholinyl (See [0018]). Press embodiment NHCONR3R4 where R3 and R4 form a piperidyl group would read on instant elected species wherein R4 and R5 form piperidyl group, and Q2 is CH2.
Bloomfield teaches 5-phenyl--thiazol-2-yl-amine derivatives as inhibitors of phosphatidylinositol 3 kinase enzymes (pi3) for the treatment of inflammatory diseases (See abstract, [0002], Tables 1-8, claims 1-3).
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Bloomfield teaches embodiments wherein Ra and Rb together form an azetidine, pyrrolidine ring, etc. which read on instant claimed
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moiety wherein R4 and R5 together with the nitrogen atom to which they are attached forma heterocyclic ring.
Bloomfield teaches compound species wherein Ra and Rb form heterocyclic ring (e.g. pyrrolidine) further substituted with CN, CONH2, that read on instant R10c (See [0150], Table 6).
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According to MPEP 2144.09 (I), 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).
It would have been obvious for one of ordinary skill in the art before the effective filing date to further explore more 1,3-thiazole compounds for treating inflammatory disease based on combined teachings of Ohkawa’113, Press and Bloomfield, together with experimentation/optimization based on general knowledge of structure similarity/ bioisosteric modification of SAR study and treatment for anti-inflammatory disease. A skilled artisan would be motivated to combine the teachings of Ohkawa’113, Press and Bloomfield because all teachings are directed to 4-phenyl-1,3-thiazole compounds for treating inflammatory disease. Further exploration/optimization based on the combined teachings of prior art, together with general knowledge of structure similarity/ bioisosteric modification of SAR would provide more 4-phenyl-1,3-thiazole compounds that are expected to have activity/efficacy for treating inflammatory disease.
One of ordinary skill in the art would have had reasonable expectation of success in producing instant claimed invention based on the combined teaching of prior art, together with general knowledge of structure similarity/ bioisosteric modification for SAR study. Therefore, the invention as a whole is prima facie obvious to one of ordinary skill in the art before the effective filing date of the claimed invention, as evidenced by the references, especially in the absence of evidence to the contrary.
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, 12, 14-15, 17, 26, 28, 33 and 35-36 are provisionally rejected on the ground of nonstatutory double patenting as being unpatentable over claims 1, 6-18 of copending Application No 18/834,185 (reference application) in view of Ohkawa et al. (US 2005/0080113 A1, Ohkawa’ 113). This is a provisional nonstatutory double patenting rejection because the patentably indistinct claims have not in fact been patented.
Reference claims are directed to compound of Formula I
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, where R1 is selected from a variety of moiety, for example,
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Reference claims 6-15 further recite R groups that are very similar to instant claims. Reference claims 8-9 recites R4 and R5 together with the nitrogen atom to which they are attached form a heterocyclic ring, including R10C is
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, R10N is
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and S atom present as S(=O), etc. that are very similar to instant claims. The scope of reference claims reciting R1 is
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overlaps with instant claimed compounds. Ohkawa’ 113 also teaches variety of 5-phenyl-1,3-thiazole derivatives comprising pyridyl, phenyl and NHCONH moiety that are very similar to core structure of instant compound of Formula I.
According to MPEP 2144.09 (I), 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). Please note prior art structures do not have to be true homologs or isomers to render structurally similar compounds prima facie obvious. In re Payne, 606 F.2d 303, 203 USPQ 245 (CCPA 1979) (See MPEP 2144.09 III.)
The instant application shares at least one common inventor and applicant with the reference application. Further, the instant application is not related to the reference application thus no 35 USC 121 shield exists. See MPEP 804.01.
Conclusion
Claims 3, 4, 13, 20-24, 25, 27, 29-32 and 34 are withdrawn.
Claims 1-2, 12, 14-15, 17, 26, 28, 33 and 35-36 are rejected.
Claim 16 is allowable.
The following is a statement of reasons for the indication of allowable subject matter: Claim 16 is amended to recite compound species comprising substituted piperidinyl rings as NR4R5 in combination with specified R groups that are supported by instant disclosure (See Table Ex 3-6). The bioisosteric modification from prior art to the compound species of claim 16 based on structural similarity and SAR study might be achievable, but might require higher level than ordinary skill in the art. Instant specification (See Table1) disclosed compounds species with reasonable adenosine receptor A2A activity that are not expected by prior art. Thus, claim 16 is non-obvious in light of prior art and 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 LIYUAN MOU whose telephone number is (571)270-1791. The examiner can normally be reached Mon-Fri 9:00-5:30.
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If attempts to reach the examiner by telephone are unsuccessful, the examiner’s supervisor, Amy L Clark can be reached on (571)272-1310. The fax phone number for the organization where this application or proceeding is assigned is 571-273-8300.
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/L.M./ Examiner, Art Unit 1628
/JARED BARSKY/Primary Examiner, Art Unit 1628
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