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 .1
Status of Claims
Claims 1-20 are pending.
Election/Restrictions
Claims 7, 11-12 and 15-20 are withdrawn from further consideration pursuant to 37 CFR 1.142(b) as being drawn to a nonelected Group II and species outside of Compound 14, there being no allowable generic or linking claim. Election was made without traverse in the reply filed on June 8, 2026.
Applicant’s election without traverse of Group I (claims 1-14) and species of Formula I, compound 14, in the reply filed on June 8, 2026 is acknowledged. Compound 14 is a compound of formula (I) in which variables are defined as: X1 is CR2, R1 and R2 together with the atoms to which they are attached from a 5- to 6- membered heterocyclyl (specifically
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), R5 is H, R3 is
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, X is OH, R6 is H, R7 is C3-C6 cycloalkyl (specifically cyclopropyl) and R4 is H.
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Claims 1, 3-6, 8-10, 13 and 14 are generic to the species.
Upon further search and examination of the claims, the below species of claim 1 have been searched and considered with elected compound 14. These compounds are compounds of 6a and 7a of WO 2020/219287 as detailed below.
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With the search of compounds 6a and 7a, withdrawn claim 2 has been rejoined and therefore claims 1-6, 8-10, 13 and 14 are under examination.
Priority
Receipt is acknowledged of certified copies of papers required by 37 CFR 1.55.
Information Disclosure Statement
The information disclosure statements (IDSs) submitted on 8/28/2025 are in compliance with the provisions of 37 CFR 1.97. Accordingly, the information disclosure statement is being considered by the examiner.
Relevant Art
Note Application No. 18864884 shares with the invention, the common Applicant HAINAN SIMCERE ZAIMING PHARMACEUTICAL CO., LTD., and several shared Inventors (Li, Zhen; Tang, Feng; Fu, Yayuan; Tang, Renhong). However, the claimed Application is not subject to an obviousness double patenting rejection in view of it.
Application No. 18864884, published as US 20250304717, claims a ligand-drug conjugate of Pc(L-D)n, where Pc is a ligand unit (i.e. a peptide residue that includes 1 to 8 amino acid), L is linker and D is a drug unit of formula D-1.
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. Despite the similarities between formula D-1 and claimed compound of formula I, the presence of the Pc ligand and L linker precludes an obviousness rejection for double patenting of the examined claims.
Claim Objections
Claim 13 is objected to because of the following informalities: Claim 13 discloses about 61 compounds but only the first 40 are numbered from pages 9-11, while the balance remain unnumbered. The balance of unnumbered compounds of claim 13 should be numbered. It is suggested the balance of claims be numbered or, the numbering be removed from the first 40 compounds.
Appropriate correction is required.
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, 3-6, 8-10 and 14 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 Claimed Invention
The claimed invention (claim 1) is directed to a compound of formula I, as detailed above, where X1, (where X1 is either N or CR2), R1, R3, R4 and R5 are broadly claimed as recited therein.
Certain narrower embodiments of the claimed invention are presented in various dependent claims. Some of these claims further limit the claimed groups and substituents as detailed therein. Claim 13 recites the claimed and elected species and other individual species. Claim 13 is NOT rejected for written description.
The Supporting Disclosure
Applicants’ supporting disclosure contains certain descriptions and embodiments of the claimed invention.
In the present case, the important factors leading to a conclusion of inadequate written description is the absence of sufficient working examples of the invention as claimed, and the lack of predictability in the art.
In the present case there is no disclosure of compounds having the broad and full scope definitions of the groups and substituents of claim 1. In fact, the scope of compounds that provide adequate written description are the approximately 60-61 compounds of claim 13, the related chemical synthesis Example schemes of compounds 1-40 starting at page 32 of the specification, as well as Tables 1-6 biological data starting at page 109; (Anti-cell proliferation activity of Table 1; anti-proliferative activity IC50 data of Table 2; liver microsome stability data of Table 3; membrane permeability data of Table 4; plasma binding data of Table 5; drug-drug interaction data of Table 6; hERG potassium ion channel data of Table 7).
In contrast to the broad claimed scope of X1, (where X1 is either N or CR2), R1, R3, R4 and R5 of the claims, the supporting disclosure (approximately 60-61 compounds of claim 13; chemical synthesis Example schemes of compounds 1-40 starting at page 32 of the specification; and Tables 1-6 biological data), are limited to the following:
X1, (where X1 is either N or CR2) X1 is N and where R2 is limited to fluoro, chloro; or alternatively, R1 and R2 together with the atoms to which they are attached form a 5-6 membered heterocyclyl, such as methylenedioxy or ethylenedioxy;
R1 is limited to chloro, bromo, methyl, hydroxyl, cyclopropyl and cyano;
R1 and R5 are combined to form a cyclopentyl, and furano, both unsubstituted;
R3 is limited to hydrogen,
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.;
R4 is limited to hydrogen; or where
R3 and R4 are combined with the nitrogen to which they are attached form
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; and
R5 is limited to hydrogen, fluoro, chloro, NO2, NH2.
Applicant’s disclosure of the 60-61 compounds of claim 13 ( and chemical synthesis Example schemes of compounds 1-40 starting at page 32 of the specification; and Tables 1-6 biological data),, is not a sufficient representation of all the claimed compounds of claim 1 (and rejected dependent claims) as presently pending.
Other than the working examples of the specification (Examples synthesis schemes of compounds 1-40 and Tables 1-6 biological data), Applicant has not reasonably described a scientific or “systematic” approach to synthesize the full scope of claim 1 and claims dependent. See MPEP 2163.02, the standard for determining compliance with the written description.2
Although Applicant has written description support for the 60-61 compounds of claim 13 (supported by the specification as detailed above) Applicant has not provided reasonably provided a description the support the broader scope of the claimed compounds of formula I.
Accordingly, Applicants have not adequately described the invention for the breadth that is claimed. It thus appears that Applicants were not in possession of the claimed invention at the time the application was filed, the full scope of compounds of formula I, and that Applicants’ species do not support the claimed genus.
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.
Claims 1-5, 8-10 and 14 are rejected under 35 U.S.C. 102(a)(1) as anticipated by WO 2020/219287. WO 287 has been cited on the IDS dated Feb 16 2024 as Foreign Ref. No. 6.
Claim 1 is directed to a compound of formula I
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wherein R1, X, X1 is CR2 or N, R2, R3, R4, R5 are defined therein.
WO 287 teaches compound 6a (at Table 1a, page 87), anticipating claim 1, where at the equivalent positions to X, X1, R1, R5, R3 and R4, compound 6a teaches equivalent to X1 (CR2), is C-F (i.e., R2 is F); equivalent to R1 is an alkyl, i.e. CH3; equivalent to R3, there is hydrogen; equivalent to R6 there is hydrogen, equivalent to R7 is hydrogen; equivalent to R4 is hydrogen; equivalent to R5 is hydrogen.
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WO 287 teaches compound 7a (at Table 1a, page 87) anticipating claim 1, where at the equivalent positions to X, X1, R1, R5, R3 and R4, compound 7a teaches equivalent to X1 (CR2), is C-F (i.e., R2 is F); equivalent to R1 is an alkyl, i.e. CH3; equivalent to R3 is
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, i.e.,
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; equivalent to X is OH, equivalent to R6 is hydrogen, equivalent to R7 is hydrogen; equivalent to R4 is hydrogen; equivalent to R5 is hydrogen.
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Regarding claim 2, where R1 is C1-C3 alkyl, compounds 6a and 7 of WO 287 disclose methyl at a position equivalent to R1. See above.
Regarding claims 3-4 where R2 is a halogen, compounds 6a and 7a from WO 287 disclose fluoro at a position to R2. See above.
Regarding claim 5 where R3 is equivalent to hydrogen or
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; R6 and R7 are hydrogen; X is OH; R4 is hydrogen, these are taught by WO 287’s compounds 6a and 7a. See above.
Regarding claim 8 where equivalent to R5 is hydrogen this is taught per WO 287’s compounds 6a and 7a. See above.
Regarding claim 9 wherein, equivalent to R3 is
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, i.e.,
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; i.e. equivalent to X is OH, where R6 is hydrogen, where to R7 hydrogen, these are taught by compound 71 of WO 287. See above.
Regarding claim 10 and the limitation of a compound of formula Ia,
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wherein R1, R2, R3 , R4 and R5 are as defined in claim 1, as detailed above, compounds 6a and 7a disclose substitutions groups at R1-5 as detailed above in the rejection of claim 1.
Regarding claim 14 and the limitation of a pharmaceutical composition comprising a compound of claim 1, WO 287 teaches a pharmaceutical composition comprising its claimed compounds and a pharmaceutically acceptable carrier. See claim 114.
Conclusion and Correspondence
In summary no claims are allowed. Any inquiry concerning this communication or earlier communications from the examiner should be directed to WILLIAM LEE whose telephone number is (571)270-3876. The examiner can normally be reached M-F.
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, Adam C. Milligan can be reached at (571) 270-7674. The fax phone number for the organization where this application or proceeding is assigned is 571-273-8300.
Information regarding the status of published or unpublished applications may be obtained from Patent Center. Unpublished application information in Patent Center is available to registered users. To file and manage patent submissions in Patent Center, visit: https://patentcenter.uspto.gov. Visit https://www.uspto.gov/patents/apply/patent-center for more information about Patent Center and https://www.uspto.gov/patents/docx for information about filing in DOCX format. For additional questions, contact the Electronic Business Center (EBC) at 866-217-9197 (toll-free). If you would like assistance from a USPTO Customer Service Representative, call 800-786-9199 (IN USA OR CANADA) or 571-272-1000.
/WILLIAM Y LEE/Examiner, Art Unit 1623
/GEORGE W KOSTURKO/Primary Examiner, Art Unit 1621
1 CONTINUING DATA
This application is a 371 of PCT/CN2022/113499 08/19/2022
FOREIGN APPLICATIONS
CHINA 202110955364.5 08/19/2021
CHINA 202111515247.3 12/13/2021
CHINA 202210515797.3 05/12/2022
2 Whenever the issue arises, the fundamental factual inquiry is whether the specification conveys with reasonable clarity to those skilled in the art that, as of the filing date sought, inventor was in possession of the invention as now claimed. See, e.g., Vas-Cath, Inc. v. Mahurkar, 935 F.2d 1555, 1563-64, 19 USPQ2d 1111, 1117 (Fed. Cir. 1991). An applicant shows that the inventor was in possession of the claimed invention by describing the claimed invention with all of its limitations using such descriptive means as words, structures, figures, diagrams, and formulas that fully set forth the claimed invention. Lockwood v. Am. Airlines, Inc., 107 F.3d 1565, 1572, 41 USPQ2d 1961, 1966 (Fed. Cir. 1997). Possession may be shown in a variety of ways including description of an actual reduction to practice, or by showing that the invention was "ready for patenting" such as by the disclosure of drawings or structural chemical formulas that show that the invention was complete, or by describing distinguishing identifying characteristics sufficient to show that the inventor was in possession of the claimed invention. See, e.g., Pfaff v. Wells Elecs., Inc., 525 U.S. 55, 68,119 S.Ct. 304,312, 48 USPQ2d 1641, 1647 (1998); Regents of the Univ. of Cal. v. Eli Lilly, 119 F.3d 1559, 1568, 43 USPQ2d 1398, 1406 (Fed. Cir. 1997); Amgen, Inc. v. Chugai Pharm., 927 F.2d 1200, 1206, 18 USPQ2d 1016, 1021 (Fed. Cir. 1991) (one must define a compound by "whatever characteristics sufficiently distinguish it"
Prosecution Insights