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 .
Election/Restrictions
Applicant's election with traverse of Group (I) with the addition of compound
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in the reply filed on 02/24/2026 is acknowledged. The traversal is on the ground(s) that the claims are linked by a single general invention concept and share a special technical feature. However, this argument is not persuasive. As set forth in the restriction requirement mailed on 04/30/2025, the claimed inventions are directed to distinct groups that do not share the same or corresponding special technical feature that defined a contribution over the prior art. According, the claims are not linked by a single inventive concept.
The requirement is still deemed proper and is therefore made FINAL.
Claims 1-17, 20-21, and 24-31 are withdrawn from further consideration pursuant to 37 CFR 1.142(b) as being drawn to a nonelected species, there being no allowable generic or linking claim.
Priority
This application is a National Stage Application under 35 U.S.C. § 371 of PCT International Application No. PCT/1B2020/061065, filed on November 24, 2020, which claims priority to Indian Provisional Patent Application Nos. IN 201921047986, filed November 24, 2019 and IN 202021029084, filed July 8, 2020.
Status of Claims
Claims 1-31 are pending. Claims 1-17, 20-21, and 24-31 are withdrawn. Claims 18-19 and 22-23 are examined in accordance to the elected species.
Information Disclosure Statement
The information disclosure statement (IDS) submitted on 09/08/2022, 07/02/2024, and 08/12/2024 has been considered by the examiner.
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 18-19 and 22-23 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 18 recites: R13 are selected from group comprising H; optionally substituted alkyl, aryl. Heteroaryl, heterocycloalkyl, cycloalkyl …” The phrase “selected from group comprising” renders the scope unclear because “comprising” is open-ended, it does not define a closed set of alternatives, and thus, fails to particularly point out the metes and bounds.
Claim 18 further recites “one or more R21 radicals… wherein one or more substitution… selected from…” This is indefinite because it is unclear which moiety is being substituted, no substitution positions are defined, no upper bounds are provided, and the layered substitution language creates uncertain scope.
Claim 19 depends from claim 18 and recites “a compound of formula VIII according to claim 18.” Claim 19 does not independently cure the indefiniteness of claim 18 and instead incorporate the same ambiguous limitations, including improper Markush structure and unclear substitution scope. Thus, claim 19 is indefinite for the same reasons as claim 18.
Claim 22 recites “T is selected from group comprising optinally substituted aryl, heteoaryl, heterocycloalkyl, cycloalkyl, amino….” Wherein one or more substitution is selected from alkyl, alkoxy….” Use of “group comprising” renders the scope open-ended and indefinite. Second, ambiguous substitution language as it is unclear what is substituted, no position or limits defined, and grammatically unclear. Third, the phosphate structures are embedded within the Markush group without clear designation as substituents or alternative members.
Claim 23 depends from claim 22 and incorporate the indefiniteness limitations. As such, claim 23 is indefinite for the same reasons as claim 22.
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 18-19 and 22-23 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.
Claim 18 encompasses:
R13/R14 = H, alkyl, aryl, heteroaryl, heterocycloalkyl, cycloalkyl
Optional formation of heterocycles, and
Extensive substitution via R21.
The specification (Examples 1-16 and claim 23) consistently discloses:
Amine-containing heterocyclic
Piperidine
Piperazine
Bipiperidine
And phosphorylated derivatives thereof.
The specification does not provide representative number of species or guidance for:
Aryl substituents lacking amine functionality
Broad genus heteroaryl classes
Non-heterocyclic cycloalkyl substituents
Full breath of substitution patterns recited.
The specification does not reasonably convey possession of the full scope of R13/R14 in claim 18.
Claims 19, 22, and 23 depend from claim 18 and incorporate the same broad genus.
Thus, claims 19, 22, and 23 fail the written description requirement for the same reasons.
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.
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.
Claims 18-19 and 22-23 are rejected under 35 U.S.C. 103 as being unpatentable over Jiao et al. (US2016/0060288 A1) in view of Long et al. (J. Med. Chem. 2010, 53, 1830-1842) and Sasmal et al. (Bioorganic & Medicinal Chemistry Letters, Volume 22, Issue 9, 1 May 2012, Pages 3157-316).
Pursuant the restriction requirement, the elected compound
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is directed to a compound of the formula VIII
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comprising;
A fulvestrant steroid core,
A phenolic carbamate linkage, and
A piperidine-piperazine-containing substituent.
Jao teaches fulvestrant derivatives having the same steroidal scaffold
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(see Abstract; paragraphs [0020]-0025]). Moreover, Jiao discloses substitution at the phenolic hydroxyl position via ester or carbonate linkage (see paragraph 0034-0040; Examples). Jiao further teaches these compounds are useful as anticancer agents (estrogen receptor activity) (see paragraphs [0003] and [0006]-0010]).
Thus, Jiao teaches the core structure and modification site corresponding to R13/R14 of claim 14.
Jiao does not teach the claimed elected compound.
However, Long teaches compounds comprising carbamate linkages bearing piperidine and piperazine substituents (see Abstract; Scheme1; Table 1) that such piperidine/piperazine carbamates are biologically active and useful scaffolds (see p. 1831-1833) identification of these motifs as “privileged chemical scaffold” (see p. 1830 (Abstract).
Long teaches the specific functional group and substituent motif corresponding to the elected species.
Sasmal teaches compounds comprising piperazine substituents (Table 1) and piperidine substituents (Table 2) that these substituents are systematically varied and interchanged to optimize activity (see Tables 1-2; p. 3178-3179).
Sasmal demonstrates that piperidine and piperazine substituents are recognized as functionally interchangeable in medicinal chemistry.
It would have been obvious to one of ordinary skill in the art at the time the invention was filed to modify the fulvestrant derivatives of Jiao to include a carbame-lined piperidine/piperazine substituent as taught by Long motivated by the known utility of carbamate linkages for modifying pharmacokinetic properties, and the recognition of piperidine/piperazine groups are privileged scaffolds as taught by Long (p. 1830). Sasmal further provides motivation by teaching that piperidine and piperazine substituents are routinely interchanged to optimize biological activity (Tables 1-2). One would have had a reasonable expectation of success because Jio provides the same core scaffold and modification site, Long provides the specific substituent and linkage, and Sasmal confirms such substitutions are predictable and routine.
The claimed elected compound species represent a predictable use of known carbamate-linked piperidine/piperazine substituents on a known fulvestrant scaffold, and therefore would have been obvious.
Such substitutions would have been expected to improve solubility and pharmacokinetic properties, as is well known in the art.
Double Patenting
The nonstatutory double patenting rejection is based on a judicially created doctrine grounded in public policy (a policy reflected in the statute) so as to prevent the unjustified or improper timewise extension of the “right to exclude” granted by a patent and to prevent possible harassment by multiple assignees. A nonstatutory double patenting rejection is appropriate where the conflicting claims are not identical, but at least one examined application claim is not patentably distinct from the reference claim(s) because the examined application claim is either anticipated by, or would have been obvious over, the reference claim(s). See, e.g., In re Berg, 140 F.3d 1428, 46 USPQ2d 1226 (Fed. Cir. 1998); In re Goodman, 11 F.3d 1046, 29 USPQ2d 2010 (Fed. Cir. 1993); In re Longi, 759 F.2d 887, 225 USPQ 645 (Fed. Cir. 1985); In re Van Ornum, 686 F.2d 937, 214 USPQ 761 (CCPA 1982); In re Vogel, 422 F.2d 438, 164 USPQ 619 (CCPA 1970); In re Thorington, 418 F.2d 528, 163 USPQ 644 (CCPA 1969).
A timely filed terminal disclaimer in compliance with 37 CFR 1.321(c) or 1.321(d) may be used to overcome an actual or provisional rejection based on nonstatutory double patenting provided the reference application or patent either is shown to be commonly owned with the examined application, or claims an invention made as a result of activities undertaken within the scope of a joint research agreement. See MPEP § 717.02 for applications subject to examination under the first inventor to file provisions of the AIA as explained in MPEP § 2159. See MPEP § 2146 et seq. for applications not subject to examination under the first inventor to file provisions of the AIA . A terminal disclaimer must be signed in compliance with 37 CFR 1.321(b).
The filing of a terminal disclaimer by itself is not a complete reply to a nonstatutory double patenting (NSDP) rejection. A complete reply requires that the terminal disclaimer be accompanied by a reply requesting reconsideration of the prior Office action. Even where the NSDP rejection is provisional the reply must be complete. See MPEP § 804, subsection I.B.1. For a reply to a non-final Office action, see 37 CFR 1.111(a). For a reply to final Office action, see 37 CFR 1.113(c). A request for reconsideration while not provided for in 37 CFR 1.113(c) may be filed after final for consideration. See MPEP §§ 706.07(e) and 714.13.
The USPTO Internet website contains terminal disclaimer forms which may be used. Please visit www.uspto.gov/patent/patents-forms. The actual filing date of the application in which the form is filed determines what form (e.g., PTO/SB/25, PTO/SB/26, PTO/AIA /25, or PTO/AIA /26) should be used. A web-based eTerminal Disclaimer may be filled out completely online using web-screens. An eTerminal Disclaimer that meets all requirements is auto-processed and approved immediately upon submission. For more information about eTerminal Disclaimers, refer to www.uspto.gov/patents/apply/applying-online/eterminal-disclaimer.
Claims 18-19 and 22-23 are rejected on the ground of nonstatutory double patenting as being unpatentable over claims 83-100 of U.S. Patent No. 18/717,086. Although the claims at issue are not identical, they are not patentably distinct from each other.
Claim 83 is directed to a compound comprising fulvestrant-based steroidal scaffold bearing a carbamate linkage to a piperidine/piperazine substituent. The instant claims are directed to closely related compounds encompassing the elected compound species having the same scaffold and substituent framework.
The compounds of the instant claims differ from the compound of the copending application in the steroidal scaffold of the instant claims comprising a hydroxyl (-OH) group at the corresponding position, whereas the copending claims recite a carbonyl (=O) group at that position. Such a difference represents a well-known and routine chemical modification involving oxidation or reduction of a carbonyl group to an alcohol, or vice versa.
One of ordinary skill in the art would have recognized that such redox transformations are conventional and would have reasonably expected that the resulting compounds would retain similar structural and functional properties. Accordingly, the claimed compounds differ from the compound of the copending claims only by an obvious variation and are therefore not patentably distinct.
Conclusion
Claims 18-19 and 22-23 are not allowed.
Any inquiry concerning this communication or earlier communications from the examiner should be directed to JEAN P CORNET whose telephone number is (571)270-7669. The examiner can normally be reached Monday-Thursday from 7.00am-5.30pm.
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If attempts to reach the examiner by telephone are unsuccessful, the examiner’s supervisor, Amy L Clark can be reached at 571-272-1310. The fax phone number for the organization where this application or proceeding is assigned is 571-273-8300.
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/JEAN P CORNET/Primary Examiner, Art Unit 1628
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