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
The office acknowledges Applicants filing of the response on 8/11/2026 to the restriction election requirement dated 5/12/2026. Applicants have elected Group I without traverse. Applicants have elected the following species for examination.
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The elected species have been found free of prior art. Therefore the scope of the subject matter was extended or broadened pursuant to MPEP 803.02. The species selected for examination is a compound of formula I:
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Claims 1, 5-8, 15, 16, 19-24, 26-36, 39-45, 54, 55, 58-62, and 68 are pending. Claims 2-4, 9-14, 17-18, 25, 37-38, 46-53, 56-57, 63-67 have been cancelled. Claims 62, 68 are withdrawn from further consideration pursuant to 37 C.F.R. 1.142(b), as being drawn to non-elected subject matter. The restriction requirement is made final. Claims 1, 5-8, 15, 16, 19-24, 26-36, 39-45, 54, 55, and 58-61 are examined based on the merits herein.
Application Priority
This application filed 05/24/2024, claims foreign priority to PCT/CN2024/091147, filed 05/06/2024, claims foreign priority to PCT/CN2024/073002, filed 01/18/2024, claims foreign priority to PCT/CN2023/096312, filed 05/25/2023.
Information Disclosure Statement
The information disclosure statement(s) (IDS) filed on 8/11/2026 and 9/13/2024 are in compliance with the provisions of 37 CFR 1.97. Accordingly, the IDS is being considered by the Examiner.
Claim Rejections - 35 USC § 112
The following is a quotation of the first paragraph of 35 U.S.C. 112(a):
(a) IN GENERAL.—The specification shall contain a written description of the invention, and of the manner and process of making and using it, in such full, clear, concise, and exact terms as to enable any person skilled in the art to which it pertains, or with which it is most nearly connected, to make and use the same, and shall set forth the best mode contemplated by the inventor or joint inventor of carrying out the invention.
The following is a quotation of the first paragraph of pre-AIA 35 U.S.C. 112:
The specification shall contain a written description of the invention, and of the manner and process of making and using it, in such full, clear, concise, and exact terms as to enable any person skilled in the art to which it pertains, or with which it is most nearly connected, to make and use the same, and shall set forth the best mode contemplated by the inventor of carrying out his invention.
Claims 1, 5-8, 15, 16, 19-24, 26-36, 39-45, 54, 55, and 58-61 are rejected under 35 U.S.C. 112(a) or 35 U.S.C. 112 (pre-AIA ), first paragraph, as failing to comply with the written description requirement. The claim(s) contains subject matter which was not described in the specification in such a way as to reasonably convey to one skilled in the relevant art that the inventor or a joint inventor, or for applications subject to pre-AIA 35 U.S.C. 112, the inventor(s), at the time the application was filed, had possession of the claimed invention.
The rejection is based on the requirement(s), i.e., the guidelines provided by the MPEP 2163.04. These are listed below:
(A) identify the claim(s) limitations at issue, and (B) establish a prima facie case by providing reasons why a person skilled in the art at the time the application was filed would not have recognized that the inventor was in possession of the invention as claimed in view of the disclosure of the application as filed. The MPEP 2163 further provided or expanded the guidelines for the written description requirements.
(A) identify the claim(s) limitations at issue:
Independent claim 1 is drawn to:
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Dependent claims further limit the variables of independent claim with the recited sub-genus species. Claim 60 is to specific compounds of formula A. Based on the claimed variables, thousands of amide compounds can be arrived from Formula A. Claim 61 is to the pharmaceutical composition of the claimed compounds.
The instant specification describes select compounds in Tables I and IA, that include select examples, wherein Ring A is limited to pyridyl, thiophen, pyrimidine, Ring B to phenyl with para substitution, R3 to indolyl ring etc. The data described in regards to the compounds is very limited.
The variables of formula A are rings A, B, R3, R4, R, Ra1, R3b, Rb with numerous substituents. Ring B is C6-C10 aryl, 5-10 membered heteroaryl, or 3-10 membered heterocyclyl. Ring A is C6-C10 aryl, 5-10 membered heteroaryl, or 3-10 membered heterocyclyl. R3 is an optionally substituted C6-C10 aryl, optionally substituted 5- to 10-membered heteroaryl, optionally substituted C3-C8 cycloalkyl, or optionally substituted 3- to 10-membered heterocyclyl. It is noted that the heteroatoms can be N, S, O, P.
Ring B can be C6-C10 aryl, 5-10 membered heteroaryl, or 3-10 membered heterocyclyl. For example if ring B is C6 aryl, phenyl, the chemical, physical and pharmacological properties of compounds of formula A will be distinct from the compounds of ring B being pyridyl.
Ring A can be C6-C10 aryl, 5-10 membered heteroaryl, or 3-10 membered heterocyclyl. For example if ring A is C6 aryl, phenyl, the chemical, physical and pharmacological and other properties of formula A compounds will be distinct from the compounds of ring A being pyridyl. Further if Ring A is phenyl and Ring B is pyridyl, such compounds will have distinct properties compared to compounds where Ring A is phenyl and Ring B is phenyl for example.
R3 is an optionally substituted C6-C10 aryl, optionally substituted 5- to 10-membered heteroaryl, optionally substituted C3-C8 cycloalkyl, or optionally substituted 3- to 10-membered heterocyclyl. For example compounds having Ring B as phenyl and R3 as phenyl, and Ring A as phenyl will have distinct chemical, physical and pharmacological and other properties compared to compounds with other varying substituents. In a nutshell, there are multi variant subgenus of compounds of formula A based on the substituents, Ring A, Ring B, R3, etc. and in fact Ring A can be aryl or heteroaryl or heterocyclyl compounds with zero to varying heteroatoms selected from N, O, S, P and in combinations. The different substituents in formula A represent an enormous genus that does not share a common core structure among the possible structures that can be made.
Applicants can claim as broadly as possible for the claimed invention. However, if there is a variability in the genus or broadly claimed subject matter, and if the variability expects unpredictability for the claimed subject matter, then specification must describe the genus with divergent species, so that a skilled person in the art can understands claimed invention and can reproduce applicants claimed invention. In this case, synthetic organic chemistry is probably one of the most unpredictable areas of technology and consequently, the effects of dissimilarities upon structure and function cannot be predicted. So, the absence of description with divergent species makes the invention unpredictable, and cannot be envisioned by a skilled person in the art.
The MPEP lists factors that can be used to determine if sufficient evidence of possession has been furnished in the disclosure of the application. These include level of skill and knowledge in the art, partial structure, physical and/or chemical properties, functional characteristics alone or coupled with a known or disclosed correlation between structure and function, and the method of making the claimed invention. Disclosure of any combination of such identifying characteristics that distinguish the claimed invention from other materials and would lead one of skill in the art to the conclusion that the applicant was in possession of the claimed species is sufficient" (MPEP 2163).
A claimed genus may be satisfied through sufficient description of a representative number of species or disclosure of relevant, identifying characteristics such as functional characteristics coupled with a known or disclosed correlation between function and structure. See MPEP 2163 II(A)(3)(a)(ii).
The number of species that describe the genus must be adequate to describe the entire genus. However, if there is substantial variability, a large number of species must be described.
The question is with thousands of possible divergent compounds can be generated based on the claim language, (i) did applicants provide enough description for making all possible compounds with all possible combinations? (ii) will the generated compounds be capable of retain its end property?
(B) establish a prima facie case by providing reasons why a person skilled in the art at the time the application was filed would not have recognized that the inventor was in possession of the invention as claimed in view of the disclosure of the application as filed:
The further analysis for adequate written description considers, see MPEP 2163, the following:
Determine whether the application describes an actual reduction to practice of the claimed invention:
The instant claim 1 is to plethora of compounds of as described by the functional properties as being known to inhibit a mutant EFGR and treat cancer. The instant specification provides examples with specific ring structures and substituents of select exemplified compounds. However claim 1 is very broad in regards to the number of compounds (thousands of compounds), with varying Markush groups/structures and the data described is very limited. It is noted that description or evidence is provided, specifically nexus between shown data and its end property. No description is provide such a way, the data shown can be extrapolated to all possible species for the claimed compounds, and the resulted ones can retain the end property. Accordingly, applicants failed to describe actual reduction to practice of the claimed invention.
(B) If the application does not describe an actual reduction to practice, determine whether the invention is complete as evidenced by a reduction to drawings or structural chemical formulas that are sufficiently detailed to show that applicant was in possession of the claimed invention as a whole:
Tables 1 and 1A provide limited number of compounds with very specific substituent(s) for Ring A, Ring B, R3 and/or other variables and the assay data with select compounds (Tables 15-17).
(C) If the application does not describe an actual reduction to practice or reduction to drawings or structural chemical formula as discussed above, determine whether the invention has been set forth in terms of distinguishing identifying characteristics, such as structure/function correlations, as evidenced by other descriptions of the invention that are sufficiently detailed to show that applicant was in possession of the claimed invention:
It is noted that synthetic organic chemistry is quite unpredictable (See In re Marzocchi and Horton 169 USPQ at 367). From what is known in the art and described in the specification one skilled in the art would not be able to predict from the instant disclosure which compounds would fall under the umbrella of functional description of being known as broadly as EGFR inhibitor. In fact, the courts have made a distinction between mechanical elements function the same in different circumstances, yielding predictable results, chemical and biological compounds often react unpredictably under different circumstances. In addition, large chemical groups present in the definitions of ring A, ring B, R, R5 that includes phenyl rings, heteroaryl rings, heterocyclyl groups can greatly influence the properties. This is evidenced by the data shown in the instant specification as seen by selected biochemical assay data of exemplified compounds in Table 5. The data provided varies from less than single digit to five digit, for e.g. for compound 157, data for A is >10000 and for compound 572, it is 0.2; for compound 376 D is >10000, and for compound 634 the value is 3. whereas for compound Further there is no data for B, C, E, F, G (assays) for a large number of exemplified compounds. This data shows the unpredictability of the properties of the compounds that vary structurally.
In view of above evidences, applicants have claimed unlimited range of compounds and a skilled person in the art can expect unpredictability in the broadly claimed genus. There are no physical/chemical/structural features that applicants have tied to this property in a relevant teaching manner, and so, making it impossible for an individual of ordinary skill in the art to determine which of the very large genus of compounds would retain its end property. Without a correlation between structure and function, the claims do little more than define the claimed invention by function. That is not sufficient to satisfy the written description requirement.
Applicants have failed to provide guidance or data or evidence as to how the skilled artisan would be able to extrapolate from the disclosure species to make and possibly use of the claimed invention. “A description of what a material does, rather than of what it is, usually does not suffice." Rochester, 358 F 3d at 923; Eli Lilly, 119 at 1568. Instead, the “disclosure must allow one skilled in the art to visualize or recognize the identity of the subject matter purportedly described.”
Vas-Cath Inc. Mahurkar, 19 USPQ2d 1111, makes clear the "applicant must convey with reasonable clarity to those skilled in the art that, as of the filing date sought, he or she was in possession of the invention. The invention is, for purposes of the 'written description' inquiry, whatever is now claimed." (See page 1117.) The specification does not "clearly allow persons of ordinary skill in the art to recognize that [he or she] invented what is claimed." (See Vas-Cath at page 1116).
Accordingly, it is deemed that the specification fails to provide adequate written description for the genus of the claimed subject matter and does not reasonably convey to one skilled in the relevant art that the inventors had possession of the entire scope of the claimed invention.
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, 41, 43-44, 58-60 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.
Claim 1 recites the following limitation:
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For example if LA is O, it exceeds the valency. Appropriate correction is required.
Claim 1 in several instances recites the limitation of ‘optionally substituted’. The substituents for such optional substitutions has not been defined. For e.g. R3 is optionally substituted, the question is if substituted, with what substituents? One skilled in the art cannot determine its metes and bounds due to an inability to envision all of the compounds with no definite number or specific substituents.
Claim 41, 43, 44 recites a limitation of,
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Claims 41, 43-44depends on claim 40, which recites a limitation of ‘optionally substituted 5- to 10- membered heteroaryl’. It is not clear ‘wherein the 3-7 membered ring’ refers to. There is insufficient antecedent basis for this limitation in the claim. Appropriate correction is required.
Claim 58 recites compounds with ring D attached to alkynyl group, for example,
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Claim 58 depends on claim 1. Ring D is not defined in claim 1 or in claim 58. One skilled in the art cannot determine its metes and bounds due to an inability to envision all of the compounds defined by the substituent. Clarification is required. For examination purposes, the claims have been examined based on the interpretation that ring D is R5. The specification as filed in page 31, [00114] disclose, “In one embodiment, R5 is ring D. In one embodiment, ring D is phenyl, C5-C6 cycloalkyl, 5- or 6-membered heteroaryl, or 3 to 10-membered heterocyclyl, wherein the phenyl, cycloalkyl, heteroaryl, or heterocyclyl is optionally substituted with one or more substituents”. It is noted that claim 59 depends on claim 58.
Claim 60 has a limitation of ‘Table 1, Table 1A, or Examples 1 to 1080’ in line 1. Claims must, under modem claim practice, stand alone to define an invention, and incorporation into claims by express reference to the specification is not permitted. See Ex parte Fressola, 27 USPQ 2d 1608 (1993). It is suggested that Applicant incorporate the structure of the compound(s) into the claim to overcome this rejection.
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.
Claim(s) 1, 5-8, 15, 16, 20-22, 26-28, 33, 40, 41, 44, 45, 54, 55, 60, 61 are rejected under 35 U.S.C. 103 as being unpatentable over Kang et al. (IDS: WO 2022245061).
Kang teach benzamide derivative, a method for preparing same, and a pharmaceutical composition containing same as an active ingredient and its therapeutic use (abstract). Kang in particular teach the following compounds of formula 1:
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(see page 4).
X, Y and Z are independently carbon or nitrogen atoms; R1 is H, OH, halogen, C1-C10 alkyl unsubstituted or substituted with one or more halogens; R2 is substituted C 6-10 aryl or substituted 5-10 membered heteroaryl; R3 is halogen; R4 is OH, halogen, or C1-15 alkoxy; R5 is -H, -OH, halogen, C1-4 alkyl, or C1-4 alkoxy; and R6 is -H, -OH, halogen, C1-4 alkyl, or C1-4 alkoxy.
If in the above formula, Z is N, X=Y=C, R1 = methyl; R2 is C6 aryl (phenyl), R3 is F (halogen), R4 is OH, and R5 and R6 is H, the following compound can be arrived.
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If in the instantly claimed Formula A, If Ring A is pyridyl with Rb as methyl (C1-C4 alkyl) and Rb or R is R5 (L1 is absent) is C6 aryl, e.g. phenyl, or Rb or R is R5 (L1 is absent) is C1 alkyl; n = 1 (it is noted that Rb or R5 can be C1 alkyl or C6 aryl or 6 membered ring), Ring B is phenyl with (OH and halogen, e.g. F substitution), R3 is indolyl (5-10 membered heteroaryl), the following compound can be arrived.
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In summary, a compound of formula A of the instant claim 1 (elected species) can be arrived from the teachings of Kang.
A person skilled in the art would have found it obvious to arrive at the elected pyrdinecarboxamide compound and its pharmaceutical composition from Kang. A person skilled in the art would have motivated to make the compound and/or the pharmaceutical composition of instant formula A with a reasonable amount of success and to use it to obtain therapeutic benefits. Thus claims 1, 5-8, 15, 16, 20 (formula I-1), 21 (Formula I-b), 22 (Formula I-1a-1), 26-28, 33, 40, 41, 44, 45, 54, 55, 60, 61 would have been obvious over the teachings of Kang.
Conclusion
Any inquiry concerning this communication or earlier communications from the examiner should be directed to UMAMAHESWARI RAMACHANDRAN whose telephone number is (571)272-9926. The examiner can normally be reached M-F- 8:30-5:00 PM (PST).
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, Kortney Klinkel can be reached at 5712705239. The fax phone number for the organization where this application or proceeding is assigned is 571-273-8300.
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/Umamaheswari Ramachandran/Primary Examiner, Art Unit 1627
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