NON-FINAL REJECTION
This application is a 35 U.S.C. 371 (national stage) application of PCT/EP2021/075316, filed Sep. 15, 2021, which claims benefit of foreign priority to EP 20196818.7, filed Sep. 18, 2020.
Claims 1-12, as amended, are pending.
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
Acknowledgment is made of applicant's claim to foreign priority under 35 U.S.C. 119(a)-(d).
Information Disclosure Statement
The information disclosure statement (IDS) submitted on Mar. 16, 2023 is in compliance with the provisions of 37 CFR 1.97. Accordingly, the information disclosure statement has been considered by the examiner.
Election/Restrictions
Applicant's election with traverse of the compound of formula (I) wherein
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and having the structural formula,
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in the reply filed on Oct. 14, 2025 is acknowledged. The elected species, which is not exemplified in the specification, reads on claims 1 and 6-12.
The traversal is on the ground(s) that the claims have been amended to exclude the compound of Example 9 of Bruno et al., cited in the Species Election requirement dated Jul. 17, 2025 (p. 3). Because Bruno et al. no longer reads on formula (I) as recited by the newly amended claims, Applicant contends that claims 1-12 satisfy the requirement of unity of invention (Remarks dated Oct. 14, 2025, pp. 12-13).
This is not found persuasive because it remains that species encompassed by formula (I) do not present a contribution over the prior art, as detailed below.
The requirement is still deemed proper and is therefore made FINAL.
Claims 2-5 are withdrawn from further consideration pursuant to 37 CFR 1.142(b), as being drawn to nonelected species, there being no allowable generic or linking claim. Applicant timely traversed the restriction (election) requirement in the reply filed on Oct. 14, 2025.
Claims 1 and 6-12 are currently pending and under consideration.
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 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.
Claim 12 is rejected under 35 U.S.C. 102(a)(1) as being anticipated by Gmachl et al. (WO 2018/115380, cited on the IDS dated 3/16/2023).
Gmachl et al. exemplify and claim SOS1 inhibitor compounds of formula (I) for use in the treatment and/or prevention of cancer (claims 1-30), which are formulated in pharmaceutical compositions together with one or more pharmaceutically acceptable excipients, e.g., as tablet for oral administration (Examples A-C, pp. 242-243).
Thus, by disclosing a product comprising one or more SOS1 inhibitors for treatment or prophylaxis of a disease, optionally cancer, Gmachl et al. anticipates claim 12.
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 pre-AIA 35 U.S.C. 103(a) which forms the basis for all obviousness rejections set forth in this Office action:
(a) A patent may not be obtained though the invention is not identically disclosed or described as set forth in section 102, if the differences between the subject matter sought to be patented and the prior art are such that the subject matter as a whole would have been obvious at the time the invention was made to a person having ordinary skill in the art to which said subject matter 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 pre-AIA 35 U.S.C. 103(a) 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.
Claims 1 and 6-12 are rejected under pre-AIA 35 U.S.C. 103(a) as being unpatentable over Yuan et al. (WO2011/011522, cited on PTO-892).
Yuan et al. claim methods of treating cancer comprising the step of administering to a subject in need thereof a therapeutically effective amount of a pharmaceutical composition comprising a compound of formulae (I) or (II), and a pharmaceutically acceptable diluent or carrier (claims 40-43), optionally in combination with at least one additional therapeutic agent (claims 50, 51, 55, and 56).
Thus, the compounds of Yuan et al. are disclosed in compositions comprising a pharmaceutically acceptable excipient, as recited by claim 7; in combinations comprising one or more additional active ingredients, as recited by claim 8; and as a product or medicament for the treatment of a hyperproliferative disease, e.g., cancer, as recited by claims 6 and 9-11.
In particular, Yuan et al. claim a compound of formula (II), having the structural formula,
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(second-to-last compound of claim 39), which reads on formula (I) as recited by claim 1, to the extent that R1 is L-M, where L is a single bond and M is C1-alkyl (methyl); y is 1; R2 is C1-haloalkyl (trifluoromethyl); x is 1; and R3 is hydrogen.
The compound of Yuan et al. differs from the instant claims in that the linker between the pyridopyrimidine core and ring A (phenyl) is -NH-CH2-CH2-, rather than -NH-CH(CH3)-.
However, the compound of Yuan et al. is disclosed as a species of formula (II), having the structural formula,
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wherein X is -NH-; R2 and R3 are each hydrogen or methyl, and n can be 0 or 1 (claim 15).
Therefore, it would have been predictable to one of ordinary skill in the art as of the filing date to modify the compound of Yuan et al., by shortening the linker by one carbon atom and substituting the remaining carbon atom with methyl, to arrive at the claimed compounds with a reasonable expectation of success, because Yuan et al. expressly contemplate the modification, and teach all compounds within the scope of formula (II) as interchangeable equivalents for the same use in methods of treating cancer.
As recognized by MPEP § 2144.09, a prima facie case of obviousness may be made when chemical compounds have (1) very close structural similarities and (2) 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).
The closer the chemical similarities between the claimed species or subgenus and any exemplary species or subgenus disclosed in the prior art, the greater the expectation that the claimed subject matter will function in an equivalent manner to the genus. See, e.g., In re Dillon, 919 F.2d at 693, 696, 16 USPQ2d at 1901, 1904 (and cases cited therein); and In re Deuel, 51 F.3d 1552, 1558, 34 USPQ2d 1210, 1214 (Fed. Cir. 1995).
While the compounds of Yuan et al. are not explicitly disclosed as SOS1 inhibitors, as recited by claim 12, Yuan et al. nonetheless disclose methods of administering a compound of formulae (I) or (II) to a patient in need of treatment for various cancers, e.g., leukemia, non-small cell lung cancer, colon cancer, central nervous system cancer, melanoma, ovarian cancer, renal cancer, prostate cancer, and breast cancer (claim 43). That SOS1 inhibition is the biochemical mechanism by which these cancers are treated is intrinsic in the methods of Yuan et al., even if that effect, result, or mechanism was not known or recognized.
A novel use of a known compound can be patentable. However, the instant claims do not recite a novel use of a known compound, but rather a previously unknown property of known compounds known to treat the same conditions in the same patient population.
A prima facie case of obviousness based on structural similarity is rebuttable by proof that the claimed compounds possess unexpectedly advantageous or superior properties. In re Papesch, 315 F.2d 381, 137 USPQ 43 (CCPA 1963).
Claims 1 and 6-11 are rejected under pre-AIA 35 U.S.C. 103(a) as being unpatentable over Hackler et al. (USPN 5,034,393, cited on PTO-892).
Hackler et al. disclose compounds of formula (1) having plant fungicidal, insecticidal, and/or miticidal activity. The compounds of Hackler et al. are disclosed in compositions and products, as well as fungicidal, miticidal, and insecticidal methods (col. 1, lines 8-14).
In particular, Hackler et al. exemplify compound 42, N-[[3-(trifluoromethyl)phenyl]-methyl]-pyrido[2,3-d]pyrimidin-4-amine (see table, col. 9), having the structural formula,
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which reads on formula (I) as recited by claim 1, to the extent that R1 is hydrogen and y is 1 or 2; ring A is phenyl; R2 is C1-6-haloalkyl (trifluoromethyl) and x is 1; and R3 is hydrogen.
The compounds of Hackler et al. are disclosed in compositions comprising a disease-inhibiting and phytologically acceptable amount of compound of formula (1), in combination with a phytologically-acceptable carrier, and may optionally contain additional active ingredients (col. 3, lines 53-60). Hackler et al. teach that the composition can be in the form of an aqueous suspension (col. 21, lines 24-26), or in the form of a solution, wherein the carrier is, e.g., water (col. 21, lines 59-68), which is recognized by the instant specification as a pharmaceutically acceptable excipient (p. 51, lines 13-21).
Thus, the compounds of Hackler et al. are disclosed for treatment or prophylaxis of a disease, as recited by claims 6, 9, and 10; in compositions comprising a pharmaceutically acceptable excipient (e.g., water), as recited by claim 7; and in compositions comprising one or more further active ingredients, as recited by claim 8.
Claim 11 recites the product of claim 9, comprising a compound of formula (I) "for treatment or prophylaxis of a disease, wherein the disease is a hyperproliferative disorder, optionally cancer." This limitation is merely intended use language, which adds no structural elements to the claim.
As recognized by MPEP § 2111.02 (II), a recitation of the intended use of the claimed invention must result in a structural difference between the claimed composition and the prior art in order to patentably distinguish the claimed invention from the prior art. If the prior art structure is capable of performing the intended use, then it meets the claim.
Compound 42 of Hackler et al. differs from the instant claims only in that the carbon atom in the linker is unsubstituted (-CH2-) rather than substituted by methyl (-CH(CH3)-).
However, Hackler et al. disclose compound 42 as a species of formula (1a), having the structural formula,
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wherein X is NR3, and Y is a C1-6 alkylene chain, which is optionally substituted by C1-4 alkyl (claims 1, 20, 21, and 31).
Therefore, it would have been predictable to one of ordinary skill in the art as of the filing date to modify compound 42 of Hackler et al. by substituting hydrogen with methyl to arrive at the claimed compounds with a reasonable expectation of success, because Hackler et al. expressly contemplate the modification, and teach all compounds formula (1a) as interchange-able equivalents.
In addition, where a compound is disclosed to have a particular utility, one of ordinary skill in the art would have a reasonable expectation that modifying the compound by the interchange of hydrogen and methyl would yield compounds having similar properties, which have thus been held to be obvious variants. See In re Wood, 582 F.2d 638, 199 USPQ 137 (CCPA, 1978); Ex Parte Bluestone, 135 USPQ 199 (B.P.A.I. 1961); In re Lincoln and Byrkit, 53 USPQ 40 (C.C.P.A. 1942); In re Druey and Schmidt, 138 USPQ 39 (C.C.P.A. 1963); In re Lohr and Spurlin, 137 USPQ 548 (C.C.P.A. 1963); In re Hoeksema, 158 USPQ 596 (C.C.P.A. 1968); In re Hoke, 195 USPQ 148 (C.C.P.A. 1977); Ex parte Fauque, 121 USPQ 425 (B.P.A.I. 1954); Ex parte Henkel, 130 USPQ 474, (B.P.A.I. 1960).
Citation of Additional Prior Art
Additional references made of record are considered pertinent to applicant's disclosure:
WO2012/079079; US Pub. 2007/0219203; USPN 8,022,077; USPN 6,541,481; and USPN 5,654,307 (all cited on PTO-892).
Conclusion
No claims are allowed.
Any inquiry concerning this communication or earlier communications from the examiner should be directed to SARA E. TOWNSLEY whose telephone number is 571-270-7672. The examiner can normally be reached on Mon-Fri from 9:00 am to 6:00 pm (EST). If attempts to reach the examiner by telephone are unsuccessful, the examiner's supervisor, Jeff S. Lundgren, can be reached at 571-272-5541. The fax phone number for the organization where this application or proceeding is assigned is 571-273-8300.
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/SARA ELIZABETH TOWNSLEY/Examiner, Art Unit 1629