DETAILED ACTION
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 .
Priority
The examiner notes that there is no certified English translation of the foreign CN202111342790.8. If the applicant wants the application to be accorded benefit of the non-English language application, a certified translation is required.
Acknowledgment is made of applicant's claim for foreign priority based on an application filed in CN202211358879.8 on 11/01/2022. It is noted, however, that applicant has not filed a certified copy of the CN202211358879.8 application as required by 37 CFR 1.55.
Information Disclosure Statement
The information disclosure statements (IDS) submitted on 04/09/2026, 11/13/2025, 06/05/2025, 03/21/2025, 09/17/2024 are being considered by the examiner.
Specification
Applicant is reminded of the proper content of an abstract of the disclosure.
In chemical patent abstracts for compounds or compositions, the general nature of the compound or composition should be given as well as its use, e.g., “The compounds are of the class of alkyl benzene sulfonyl ureas, useful as oral anti-diabetics.” Exemplification of a species could be illustrative of members of the class. For processes, the type of reaction, reagents and process conditions should be stated, generally illustrated by a single example unless variations are necessary.
The use of the term Shelxs97 (page 17), Diacel Chiralpak (page 23), Waters XBridge (page 43), Xtimate (page 44), phenomenex luna (page 68), XLFIT5 (page 70), which are a trade names or a marks used in commerce, has been noted in this application. The term should be accompanied by the generic terminology; furthermore the term should be capitalized wherever it appears or, where appropriate, include a proper symbol indicating use in commerce such as ™, SM , or ® following the term.
Although the use of trade names and marks used in commerce (i.e., trademarks, service marks, certification marks, and collective marks) are permissible in patent applications, the proprietary nature of the marks should be respected and every effort made to prevent their use in any manner which might adversely affect their validity as commercial marks.
Claim Objections
Claims 1-16 and 19 are objected to because of the following informalities: when there is only one variable to select from "selected from" should be "is", (for example: Ra is H, not Ra is selected from H). 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 1-16 and 19 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.
Claims 1-16 and 19 are indefinite in scope because they state the C1-3 alkyl is optionally substituted with 1, 2 or 3 halogens, however no C1-3 alkyl is mentioned besides C1-3 alkyl-S02- so it is unclear if this is the alkyl group that is referred too.
Claims 1-16 and 19 are indefinite in scope because of the dotted lines on ring A and B it is unclear if these are meant to be the attachment points on formula IV as this is not specified.
Claim 14 is indefinite in scope because said moiety can be acridinyl, acridine is a tricyclic heteroaryl and it is not clear how it would fit within the confines of the monocyclic ring characterized by claim 14.
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 3-10, 12, 14-16, 19 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. Claims 3, 5-9, 16, 19 improperly broaden the scope of claim 1 from which they depend because ring A and B can at maximum be a 10 remembered ring, however, the dependent claims allow for when n=m=3 which would include an 11 membered ring. Claims 5-10, 12 16, 19 improperly broaden claim 1 from which they depend because ring A and B cannot be optionally substituted with halogens. Claims 14 improperly broadens the scope of claims 1 and 5 as acridinyl does not fit the scope of the allowed rings A or B. Claim 15 improperly broadens the scope of claim 14 because the first group of claim 15 is not included in the scope of claim 14. Claim 4 does not properly further limit 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.
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.
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, 3-17 and 19-20 is/are rejected under 35 U.S.C. 103 as being unpatentable over BOYS (BOYS et al., WO 2011130146 A1, 2011-10-20) in view of Barillari (Barillari et al., Classical Bioisosteres, Bioisosteres in Medicinal Chemistry, First Edition. Edited by Nathan Brown, Published 2012 by Wiley-VCH Verlag GmbH & Co. KGaA, Pages 15-29) further in view of BROWN (BROWN et al., WO-2017144995-A1, 2017).
The reference BOYS teaches example 160 on page 190, wherein Ra and Rb=
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, T2=N, R2=C1 alkyl, R3=H, R1=H.
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The reference BOYS also teaches “Accordingly, this invention further provides a method of treating a disease or disorder selected from an autoimmune disease and an inflammatory disease in a mammal in need thereof, comprising administering to a mammal a therapeutically effective amount of at least one compound of Formula I or a pharmaceutically acceptable salt thereof. [00412] In one embodiment, the autoimmune or inflammatory disease is selected from lupus, psoriasis , psoriatic arthritis, rheumatoid arthritis, multiple sclerosis and inflammatory bowel diseases” [00411-00412] and “The present invention relates to novel compounds, to pharmaceutical compositions comprising the compounds, to processes for making the compounds, and to the use of the compounds in therapy. More particularly, it relates to certain 5,7-substituted- imidazo[l,2-c]pyrimidine compounds which are inhibitors of JAK kinases. In particular, the compounds are inhibitors of Tyk2, JAK1, JAK2, and/or JAK3, and are useful in the treatment of JAK kinase-associated diseases such as autoimmune diseases, inflammatory diseases, organ, tissue and cell transplant rejection, and hematological disorders and malignancies” [0001].
The reference BOYS also teaches
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instead of
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see reference page 29 as an alternative.
This helps to teach claims 1, 3-17 and 19-20.
The only difference between a compound of instant claims 1, 3-16 and 19 and BOYS is a single N position in the fused ring. Claims 17 and 20 differ in the same N and a change from
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instead of
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.
The reference Barillari teaches “The discovery and development of a candidate for clinical evaluation is a long process that involves small modifications to a lead compound to improve some of its properties, such as pharmacological activity, selectivity, and pharmacokinetics. This is often achieved by the medicinal chemists by replacing a functional group with groups sharing similar physical or chemical properties and maintaining similar activity, which are defined as bioisosteres. We will hereby provide a historical overview of the development and evolution of the concepts of isosterism and bioisosterism, followed by a selection of successful examples of bioisosteric modifications reported in the literature”(page 15).
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The reference BROWN teaches very similar compounds with the right core nitrogen placement (see formula I, abstract) also for the purpose of treating a similar range of diseases including psoriasis(page 11) and that are also “The present invention provides pharmaceutically active pyrazolo[1 ,5-a]pyrazin-4-yl TYK2 ligands and analogues. Such compounds are useful for inhibiting Janus Kinases (JAKs). This invention also is directed to compositions comprising methods for making such compounds, and methods for treating and preventing conditions mediated by JAK”(page 1).
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This would help to teach claims 1, 3-17 and 19-20.
It would have been prima facie obvious to one of ordinary skill in the art before the effective filing date of the instant invention to have modified BOYS with Barillari and BROWN because Barillari teaches that it is common practice to make small modifications to a lead compound for drug design to improve some of its properties, such as pharmacological activity, selectivity, and pharmacokinetics and because BROWN teaches very similar compounds for treating the same diseases (such as psoriasis) that function with alternate ring nitrogen and carbon location which would give the substitution a reasonable expectation of success since the nitrogen to carbon swaps are suggested by the prior art of BOYS and BROWN. It would also be obvious to combine these similar structures with reasonable expectation of success for similar disease as both BOYS and BROWN despite slight differences in structure are all suggested as molecules useful in treating and preventing conditions mediated by JAK. Thus these slight modifications have a reasonable expectation of preserving the core activity. One would be motivated to do so incase small modifications lead to improved properties, such as pharmacological activity, selectivity, and pharmacokinetics.
Claim(s) 1-2 and 17-18 is/are rejected under 35 U.S.C. 103 as being unpatentable over BOYS (BOYS et al., WO 2011130146 A1, 2011-10-20) in view of Barillari (Barillari et al., Classical Bioisosteres, Bioisosteres in Medicinal Chemistry, First Edition. Edited by Nathan Brown, Published 2012 by Wiley-VCH Verlag GmbH & Co. KGaA, Pages 15-29) further in view of BROWN (BROWN et al., WO-2017144995-A1, 2017) further in view of YIN (YIN et al., CN111320633A, 2020-06-23, IDS).
The references BOYS, Brown and Barillari have been discussed supra and do not disclose the structures of claims 2 and 18.
The reference YIN teaches similar structured compounds (reference claim 1) for treating the same diseases including psoriasis [0006] as the instant claims, wherein, Cy can be
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[0042] and R2=CN (page 12) and , wherein the fused rings, fused heterocyclic rings, spirocyclic rings, and spirocyclic rings may optionally be further replaced by one or more R4[0045]
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The reference YIN teaches “Cy is selected from fused rings, fused heterocyclic rings, spirocyclic rings, spirocyclic rings, bridged rings, and bridged heterocyclic rings, wherein the fused rings, fused heterocyclic rings, spirocyclic rings, spirocyclic rings, bridged rings, and bridged heterocyclic rings may be further replaced by one or more R4”[0025] and “Each R4 is independently selected from halogen, amino, nitro, cyano …”[0026]. This helps to teach claim 2.
The reference YIN teaches the compound of the current invention are JAK inhibitors[0282 and abstract] and suggested for the treatment of psoriasis [0074].
It would have been prima facie obvious to one of ordinary skill in the art before the effective filing date of the instant invention to have modified BOYS and Barillari and BROWN with YIN because Barillari teaches that it is common practice to make small modifications to a lead compound for drug design to improve some of its properties, such as pharmacological activity, selectivity, and pharmacokinetics and because BROWN and YIN teach very similar compounds for treating the same diseases (such as psoriasis) that function with alternate ring nitrogen and carbon location which would give the substitution a reasonable expectation of success since the nitrogen to carbon swaps are suggested by the prior art of BOYS and BROWN. YIN teaches bridged rings and well as spiro rings substituted with CN making it obvious modification choices for the position of instant ring B as these rings are suggested for similar placement. It would also be obvious to combine these similar structures with reasonable expectation of success to treat similar disease because all of the references: BOYS, BROWN and YIN teach that despite slight differences in structure the compounds are all suggested as molecules useful in treating and preventing conditions mediated by JAK. Thus these slight modifications have a reasonable expectation of preserving the core activity. One would be motivated to do so incase small modifications lead to improved properties, such as pharmacological activity, selectivity, and pharmacokinetics.
Conclusion
Claims 1-20 are rejected.
Any inquiry concerning this communication or earlier communications from the examiner should be directed to ALISON AZAR HASTINGS whose telephone number is (703)756-4584. The examiner can normally be reached Mon-Thurs 7:30am-5pm EST Friday 7:30-4pm EST (every other Friday off).
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/A.A.H./ Examiner, Art Unit 1627
/Kortney L. Klinkel/ Supervisory Patent Examiner, Art Unit 1627
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