Detailed Action
The present office action is in response to the amendments filed on 03 Nov 2025.
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 .
Status
Claims 1, 6, and 11 of the pending application have been examined on the merits. Claims 4-5 and 7-9 remain withdrawn (see “Response to Applicant Amendments” below). Acknowledgement is made of the amendments filed 03 Nov 2025. Acknowledgement is made of the cancellation of claims 2-3 and 10. Acknowledgement is made of the newly added claim 11.
Priority
Applicants identify the instant application, Serial #: 17/771,070, filed 22 Apr 2022, as a National Stage Entry of International Patent Application #: PCT/CN2020/120134, filed 10 Oct 2020, which claims foreign priority from Foreign Application #: CN201911019200.0, filed 24 Oct 2019.
Response to Applicant Amendments
Acknowledgement is made of the amendments filed 03 Nov 2025.
The objection to the title is rendered moot following applicant amendments.
The objection to claim 1 is rendered moot following applicant amendments.
The rejection of claim 1 under 35 U.S.C. § 112(a) is rendered moot following applicant amendments.
The rejection of claim 1 under 35 U.S.C. § 112(b) is rendered moot following applicant amendments.
The rejection of claims 1 and 6 under 35 U.S.C. § 102(a)(1) is rendered moot following applicant amendments. A further search was conducted which found prior art (see rejections below). The new grounds of rejection was necessitated by applicant amendment.
Regarding the anticipatory-type double patenting rejections over copending Application No. 17/771,083 and copending Application No. 18/381,583, the terminal disclaimers filed on 05 Feb 2026 have been received and are pending review. The action is being sent in order to expidite the issues under 35 U.S.C. § 102(a)(1) and 35 U.S.C. § 103. The nonstatutory double patenting rejections are maintained and restated below. Since the previous office action (mailed on 09 Jun 2025), copending Application No. 17/771,083 was issued a Notice of Allowance and is now U.S. Patent No. 12,509,447. The rejection is now directed to the patent and not the application and is no longer a provisional rejection.
In the amendments filed 03 Nov 2025, applicant limited the scope of the generic claim to species that did not include the compound that was part of the expanded Markush search. Accordingly, examiner is extending the Markush search to Example 122 on pg. 16 of the instant specification (reproduced below) which reads on the instant claims under examination.
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Prior art was found for this search and a new grounds of rejection is made below. This rejection is necessitated by applicant amendment.
Examiner notes that the relevant anticipation rejection below is based upon art which was found incidental to the search for the elected species. This is not indicative that the entire scope of the claims has been examined; however, the following art is being applied in an effort to promote compact prosecution of the case.
Claim Objections
Claim 11 is 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 § 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 text of those sections of Title 35, U.S. Code not included in this action can be found in a prior Office action.
Claim(s) 1 is/are rejected under 35 U.S.C. 102(a)(1) as being anticipated by WO 2020/118683, hereinafter ‘683. The following anticipation rejection below is based upon art which was found incidental to the search for the elected species. This is not indicative that the entire scope of the claims has been examined; however, the following art is being applied in an effort to promote compact prosecution of the case. The art is related to the searched species in the following way: the primary reference for the rejection of claims 1 and 6 under 35 U.S.C. § 103 contains species which directly anticipate the instant claims.
Instant claim 1 is drawn to compounds of the following generic formula:
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The phrase, “for use as a JAK1/Tyk2 dual inhibitor” is construed as an intended use. Intended uses are not considered a limitation and therefore the above phrase does not further limit the compounds of instant claim 1. See MPEP § 2111.02(II).
‘683 teaches Compound 92 (pg. 112):
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Compound 92 reads on the generic formula of instant claim 1 when X1 is CH; X2 is N; ring G1 is
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; A1, A2, A3, A4, and A5 are CH; R1 replaces the H of A3; and R1 is substituted amido.
Thus, ‘683 anticipates the instant claims.
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 and 6 is/are rejected under 35 U.S.C. 103 as being unpatentable over ‘683 further in view of Patani et al. (Chem Rev, 1996, 96:3147-3176), hereinafter Patani, and CN 110330484 (provided in IDS 04/22/22), hereinafter ‘484.
Examiner has expanded the search of the instant claims to include the following compound:
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Instant claims 1, 6, and 11 read on the above compound. The phrase, “for use as a JAK1/Tyk2 dual inhibitor” in instant claim 1 is construed as an intended use. Intended uses are not considered a limitation and therefore the above phrase does not further limit the compounds of instant claim 1. See MPEP § 2111.02(II).
‘683 teaches Compound 41 (pg. 102):
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‘683 teaches that Compound 41 has the following inhibitory effect on various JAK and TYK proteins (pg. 135, Table 4):
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However, Compound 41 differs from the instant compound in two ways, first, Compound 41 has a fluorine in place of the respective hydrogen on the instant compound. Second, the amide bond in Compound 41 is reversed compared to the instant compound.
Patani teaches that bioisosterism represents one approach used by the medicinal chemist for the rational modification of lead compounds into safe and more clinically effective agents and the concept of bioisosterism is often considered to be qualitative and intuitive (pg. 3147, columns 1-2). Patani teaches the substitution of hydrogen by fluorine is one of the more commonly employed monovalent isosteric replacements (pg. 3149, column 1). Patani also teaches that the ability of fluorine to replace hydrogen is an effective method of exploring the affinity of an agent to the target site by virtue of its greater electronegativity while other parameters such as steric size and lipophilicity are maintained (pg. 3150, column 1). Patani teaches that included in a list of potential bioisosteres of an amide bond is a reversed amide (pg. 3170, column 2, Table 48). Patani teaches that modifying the amide bond to a reversed amide bond can tell a medicinal chemist whether the location of the hydrogen bond donor and acceptor is important for potency (pg. 3171, column 1).
‘484 teaches the Compound 27 as a JAK inhibitor:
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‘484 teaches Compound 27 exhibited enzyme inhibition of 50% for JAK1 and 96% for JAK3 at 10 µM of the compound. Compound 27 shows that reversing the orientation of the amide bond relative to Compound 41 (above) maintains the drug’s inhibitory activity against JAK proteins.
Based on the teachings of ‘683 and Patani, a person of ordinary skill in the art would modify Compound 41 in two ways. First, the artisan would modify the fluorine on the pyrimidine moiety to a hydrogen to explore the affinity of Compound 41 to the target site of the JAK and TYK proteins. Second, the artisan would reverse the amide bond of Compound 41 to determine if the location of the hydrogen bond donor and acceptor is important for potency. By making these changes the artisan would arrive at the instant compound. The artisan would have a reasonable expectation of success that making these two changes would maintain the inhibitory activity of the modified Compound 41 against JAK proteins, as taught by ‘484.
A reference is good not only for what it teaches by direct anticipation but also for what one of ordinary skill in the art might reasonably infer from the teachings (In re Opprecht 12 USPQ 2d 1235, 1236 (Fed Cir. 1989); In re Bode 193 USPQ 12 (CCPA) 1976). In light of the foregoing discussion, the examiner concludes that the subject matter defined by the instant claims would have been obvious within the meaning of 35 USC 103. From the teachings of the references, it is apparent that one of ordinary skill in the art would have had a reasonable expectation of success in producing the claimed invention. Therefore, the invention as a whole was prima facie obvious to one of ordinary skill in the art at the time the invention was made, 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.
Claim 1 is rejected on the ground of anticipatory-type nonstatutory double patenting as being unpatentable over claims 1-10 of U.S. Patent No. 12,509,447, hereinafter ‘447. Although the claims at issue are not identical, they are not patentably distinct from each other.
Claim 1 of the instant application is directed to compounds of the following structure:
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where X1 and X2 are selected from carbon or nitrogen; ring G is
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; A1-5 are selected from carbon, nitrogen, oxygen, or sulfur; one or more R1 substituents may be attached to ring G; and R1 is selected from hydrogen, halogen, alkyl, substituted alkyl, amino, amine, substituted amine, carboxyl, amido, substituted amido, ester, substituted carbonyl, cycloalkyl, heterocycloalkyl, substituted heterocycloalkyl, aryl, substituted aryl, heteroaryl, and substituted heteroaryl.
Claim 1 of the reference patent teaches compounds of the following structure:
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where X1 or X2 are selected from carbon or nitrogen (reference claim 1); G1 is selected from
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(reference claim 2); C1-5 are selected from carbon, nitrogen, sulfur, or oxygen (reference claim 2); and G2 is a four-membered alkyl heterocyclic ring (reference claim 1). When G1 is
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, reference claims 1-10 denote species of instant claim 1 where reference variable G2 corresponds to instant variable R1 when R1 is a heterocycloalkyl.
Claims 1 and 6 are provisionally rejected on the ground of anticipatory-type nonstatutory double patenting as being unpatentable over claim 1-10 of copending Application No. 18/681,583 (reference application). Although the claims at issue are not identical, they are not patentably distinct from each other.
Claim 1 of the instant application is directed to compounds of the following structure:
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where X1 and X2 are selected from carbon or nitrogen; ring G is
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; A1-5 are selected from carbon, nitrogen, oxygen, or sulfur; one or more R1 substituents may be attached to ring G; and R1 is selected from hydrogen, halogen, alkyl, substituted alkyl, amino, amine, substituted amine, carboxyl, amido, substituted amido, ester, substituted carbonyl, cycloalkyl, heterocycloalkyl, substituted heterocycloalkyl, aryl, substituted aryl, heteroaryl, and substituted heteroaryl. Instant claim 6 further limits R1 to
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where R13 is selected from hydrogen, alkyl, substituted alkyl, cycloalkyl, substituted cycloalkyl, hydroxyl, ether, aryl, substituted aryl, heteroaryl, and substituted heteroaryl; and R14 is selected from hydrogen, alkyl, substituted alkyl, cycloalkyl, substituted cycloalkyl, hydroxyl, ether, aryl, substituted aryl, heteroaryl, and substituted heteroaryl.
Claim 1 of the reference application is drawn to compounds of Formula (I) (reference claim 1):
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where R1 is C or N (reference claim 1); R2 is selected from
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(reference claim 1); and R3 is selected from
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(reference claim 3). When R1 is C or N; R2 is
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; and R3 is
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, the reference claims are a species of instant claims 1 and 6 and so anticipate the instant claims.
This is a provisional nonstatutory double patenting rejection because the patentably indistinct claims have not in fact been patented.
Conclusion
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.
Correspondence
Any inquiry concerning this communication or earlier communications from the examiner should be directed to Jonathan D. Mahlum whose telephone number is (703)756-4691. The examiner can normally be reached 8:30 AM - 5:00 PM ET, M-F.
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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.
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/J.D.M./Examiner, Art Unit 1625 /Andrew D Kosar/Supervisory Patent Examiner, Art Unit 1625