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
This application is a national stage application under 35 U.S.C. § 371 of International Application No. PCT/TR2021/050144, filed 02/17/2021, which claims the priority benefit of foreign patent TÜRKİYE Application No. 2020/02323, filed 02/17/2020.
Information Disclosure Statement
The information disclosure statements (IDS) submitted on 08/17/2022 was filed in compliance with the provisions of 37 CFR 1.97. Accordingly, the information disclosure statements are being considered by the examiner.
Election/Restrictions
Applicant’s election without traverse of species 1) breast cancer; 2) an antiproliferative agent; and 3) taxanes (cytoskeletal disruptors), in the reply filed on 10/14/2025 is acknowledged.
The requirement for restriction between Group I (claims 1-4 and 12-13), and Group II (5-11) in the restriction dated 05/29/2025, has been withdrawn.
Status of the Application
Claims 1-13 are pending and currently under examination.
Specification
The disclosure is objected to because of the following informalities: the term “%0,5” appears in the specification, page 12, line 5.
Appropriate correction is required.
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.
Claims 1-2, 5-12 are rejected under 35 U.S.C. 102(a)(1) as being anticipated by CAplus Registry Number: RN 1496429-76-5. [Database Registry Chemical Abstracts Service, Columbus, Ohio, Accession No. RN 1496429-76-5, Entered STN: 16 Dec 2013].
CAplus Registry Number: RN 1496429-76-5 discloses the compound of N-[[[(3-Phenyl-1,2,4-oxadiazol-5-yl)methyl]amino]carbonyl]-L-tryptophan which satisfies the structural limitations of the compound of formula I of the instant claims wherein the compound of formula I encompasses a pharmaceutically acceptable hydrate, solvate, prodrug, stereoisomer, salt, ester, tautomer, isotopically labeled derivative thereof, or form thereof compound of formula I that form under physiological conditions of the human body. See MPEP 2112.01 and MPEP 2111.02 (II).
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Registry number 1496429-76-5 is available as prior art as of 16 Dec 2013, the date it was indexed into the REGISTRY database.
Regarding the composition of claim 12, comprising the anticipatory compound and an excipient, the Registry entry for Registry no. 1496429-76-5 discloses a mass solubility of 0.093 g/L, in unbuffered water at pH 3.92. This teaching of water anticipates the claimed composition, wherein the compounds are present with an excipient (i.e., water).
See MPEP § 2128 “Printed Publications” as prior art. An electronic publication, including an on-line database or Internet publication, is considered to be a “printed publication” within the meaning of 35 U.S.C. § 102 (a) and (b) provided the publication was accessible to persons concerned with the art to which the document relates. In re Wyer, 655 F.2d 221, 227, 210 USPQ 790, 795 (CCPA 1981): since this date represents the date that each compound entered the REGISTRY database on STN, this represents the date that each compound was made accessible to the public.
It is further noted that for the purposes of determining if a reference is a “printed publication,” MPEP § 2128 (I) states the following:
A reference is proven to be a "printed publication" "upon a satisfactory showing that such document has been disseminated or otherwise made available to the extent that persons interested and ordinarily skilled in the subject matter or art, exercising reasonable diligence, can locate it." In re Wyer, 655 F.2d 221, 210 USPQ 790 (CCPA 1981) (quoting I.C.E. Corp. v. Armco Steel Corp., 250 F. Supp. 738, 743, 148 USPQ 537, 540 (SDNY 1966)) ("We agree that ‘printed publication’ should be approached as a unitary concept.
where “prior art disclosures…on an on-line database are considered to be publicly available as of the date the item was publicly posted.” Since each of the database entries above lists the date that each compound was entered into the on-line database, the compounds were made publicly available as of that date in each citation.
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 of this title, 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 set forth in Graham v. John Deere Co., 383 U.S. 1, 148 USPQ 459 (1966), that are applied 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.
Claims 1-13 are rejected under 35 U.S.C. 103 as being unpatentable over CAplus Registry Number: RN 1496429-76-5. [Database Registry Chemical Abstracts Service, Columbus, Ohio, Accession No. RN 1496429-76-5, Entered STN: 16 Dec 2013] in view of Tcherkassov (WO 2020/047668 Al).
The instant claims are directed to a pharmaceutical composition comprising a compound of formula I or a pharmaceutically acceptable derivative, hydrate, solvate, prodrug, stereoisomer, salt, ester, tautomer, or isotopically labeled derivative thereof.
CAplus Registry Number: RN 1496429-76-5 discloses the compound of N-[[[(3-Phenyl-1,2,4-oxadiazol-5-yl)methyl]amino]carbonyl]-L-tryptophan which satisfies the structural limitations of formula I of the instant claims.
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However, the CAS registry fails to disclose its use in treating the proliferative disease of breast cancer.
However, the CAS registry fails to explicitly disclose CAS RN 1496429-76-5 in its deprotonated or racemic form with such specificity to rise to the level of anticipation of formula Ia, nor does the reference disclose RN 1496429-76-5 in a composition with an additional pharmaceutically active agent.
It is noted that the compound of CAS RN 1496429-76-5 satisfies the structural limitations of the compound of formula I of the instant claims wherein the compound of formula I encompasses a pharmaceutically acceptable hydrate, solvate, prodrug, stereoisomer, salt, ester, tautomer, isotopically labeled derivative thereof, or form thereof compound of formula I that form under physiological conditions of the human body.
Tcherkassov et al. teach Myc-Max inhibitory compounds having the structure of Formula (I) and compositions thereof for use in treating cancer, including breast cancer (Abstract).
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Tcherkassov discloses “(a)lternatively, the compounds of TABLE 5 may be used for treating cancer, or may be combined with a pharmaceutically acceptable carrier for the treatment of cancer. The cancer may be selected from one or more of the following: prostate cancer; breast cancer; colon cancer; cervical cancer; small-cell lung carcinoma; neuroblastomas; osteosarcoma; glioblastoma; melanoma; and myeloid leukaemia” [0032] (sic). Tcherkassov discloses compounds and all different forms thereof (e.g. free forms, salts, solvates, polymorphs) as described herein include isomers such as geometrical isomers, optical isomers based on asymmetric carbon, stereoisomers, tautomers, individual enantiomers, individual diastereomers, racemates, diastereomeric mixtures and combinations thereof, and are not limited by the description of the formulas illustrated for the sake of convenience. [0047]. Tcherkassov also teaches the derivative of formula I as the compound of VPC-70345 on table 5 (page 47) [0098]. Tcherkassov also teaches when M1 is
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and G1 is H, then n3 is 1 wherein the compound may be for use in the treatment of breast cancer (page 6, bottom paragraph). Tcherkassov also teaches M2 is
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wherein L1-5 are H and. Tcherkassov also teaches the methoxy group on the M2 phenyl ring may be H.
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Therefore, it would have been prima facie obvious to a person having ordinary skill in the art, prior to the effective filing date of the instant application, to use the disclosed compound of CAS RN 1496429-76-5 in a pharmaceutical composition for the treatment of breast cancer because Tcherkassov disclosed that Myc-Max inhibitory compounds having the structure of Formula (I) are useful in treating cancer and given that the compound of CAS RN 1496429-76-5 was already known in the art in view of the teachings of VPC-70345 by Tcherkassov, a skilled artisan would have understood that compounds are generally synthesized as racemic mixtures and exist in a equilibrium of protonated and unprotonated forms based on environmental pH. Accordingly, a skilled artisan would have found it prima facie obvious to include I and Ia and would have been motivated to include protonated forms and/or racemic mixtures of VPC-70345 or CASRN 1496429-76-5, see MPEP 2131.02. Furthermore, the shared close structural makeup to the compound of VPC-70345 which has the
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functional group is disclosed as useful in treating breast cancer and is also encompasses the structural limitations of formula I of the prior art, and therefore would have been prima facie obvious to one of ordinary skill to try through routine experimentation. See MPEP 2144.05.
A person of ordinary skill in the art would have been motivated to use the compound of CAS RN 1496429-76-5 as a treatment for breast cancer as taught by Tcherkassov because of the close structural relationship to VPC-70345 which comprises the known
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functional group which is disclosed to be useful in treating breast cancer. A skilled artisan would have had a reasonable expectation of success in treating breast cancer by selecting the compound of CAS RN 1496429-76-5 due to a close structural make up to Tcherkassov’s disclosed compound of VPC-70345 already disclosed to be useful in treating breast cancer and therefore would have expected a compound of similar structure to have similar effects as disclosed in the prior art of record. See MPEP 2144.05 and 2107.03.
Conclusion
Claims 1-13 are rejected, no claims are allowed.
Correspondence
Any inquiry concerning this communication or earlier communications from the examiner should be directed to ERNESTO VALLE JR whose telephone number is (703)756-5356. The examiner can normally be reached 0730-1700 M-F EST, 1st Friday off.
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/E.V./Examiner, Art Unit 1623
/ADAM C MILLIGAN/Supervisory Patent Examiner, Art Unit 1623