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 without traverse of Group I, claims 21, 23-30, 65-67 and 76, and the species of Compound 13:
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in the reply filed on January 10, 2026 is acknowledged with appreciation.
Claim 77, drawn to a method of treatment, is withdrawn from further consideration pursuant to 37 CFR 1.142(b) as being drawn to a nonelected invention, there being no allowable generic or linking claim.
Applicant is reminded that upon the cancelation of claims to a non-elected invention, the inventorship must be corrected in compliance with 37 CFR 1.48(a) if one or more of the currently named inventors is no longer an inventor of at least one claim remaining in the application. A request to correct inventorship under 37 CFR 1.48(a) must be accompanied by an application data sheet in accordance with 37 CFR 1.76 that identifies each inventor by his or her legal name and by the processing fee required under 37 CFR 1.17(i).
Specification
5. The disclosure is objected to for the following reasons:
6. The abstract contains the term “novel,” in line 1 of the abstract. The Specification also contains multiple instances of the term “novel,” e.g., “More particularly, the invention provides novel compounds, e.g., inhibitors of methionine aminopeptidase 2 (MetAP-2) and pharmaceutical compositions thereof,” (see paragraph [0002]). See also paragraphs [0006] and [0051]. It is suggested that the term “novel” be deleted from the language of both the abstract and the Specification. Once the determination of the novelty of a claimed invention has been established and the disclosure of the invention made public and/or patented, the claimed invention is no longer novel, since the scope of the invention no longer embraces what is considered “novel.” Thus, the incorporation of “novel” into the language of the abstract and the Specification is not appropriate. Appropriate correction is required. See MPEP § 608.01.
Claim Rejections - 35 USC § 112
7. 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.
8. Claims 21, 23-25, 66, and 76 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 claims contain 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.
9. In particular, support cannot be found for the full scope of compounds of formula (IIIA), as instantly claimed.
10. The MPEP §2163 states that the purpose of the written description requirement is to ensure that the inventor had possession, as of the filing date of the application, of the specific subject matter later claimed by him. In the case of chemical entities, Applicant's attention is further directed to Regents of the University of California v. Eli Lilly & Co., 119 F.3d 1559 (Fed. Cir. 1997), cert. denied, 523 U.S. 1089, 118 S. Ct. 1548 (1998), which notes that an adequate written description requires a precise definition, such as by structure, formula, chemical name, or physical properties, “not a mere wish or plan for obtaining the claimed chemical invention.” While the court recognizes that, “[i]n claims involving chemical materials, generic formulae usually indicate with specificity what the generic claims encompass” (Id.), it is also recognized that for a broad generic claim, the specification must provide adequate written description to identify the genus of the claim and/or the genus must be sufficiently detailed to show that applicant was in possession of the claimed invention as a whole (see Vas-Cath, Inc. v. Mahurkar, 935 F.2d 1555 (Fed. Cir. 1991)). If a genus has substantial variance, the disclosure must present a sufficient number of representative species that encompass the genus in order to adequately describe the genus (i.e., the disclosure must describe a sufficient variety of species to reflect the variation within that genus). See MPEP § 2163. Otherwise, as stated by the court in Ariad Pharmaceuticals, Inc., v. Eli Lilly and Company (Fed. Cir. 2010), “a generic claim may define the boundaries of a vast genus of chemical compounds, and yet the question may still remain whether the specification, including original claim language, demonstrates that the applicant has invented species sufficient to support a claim to a genus. The problem is especially acute with genus claims that uses open-ended language such as “or an isotope thereof” or “or a derivative thereof.” In such a case, the claim simply recites the generic “derivative,” and may do so without describing species that achieve that result. But the specification must demonstrate that the Applicant has made a generic invention that achieves the claimed result and do so by showing that the Applicant has invented sufficient alternative species to support the claim to the generically-defined genus.
11. The factors considered in the Written Description requirement are:
(1) level of skill and knowledge in the art,
(2) partial structure,
(3) physical and/or chemical properties,
(4) functional characteristics alone or coupled with a known or disclosed
correlation between structure and function, and
(5) the method of making the claimed invention.
12. Level of skill and knowledge in the art: The level of skill to practice the art of the instantly claimed invention is high and requires a variety of skills usually found in institutions and companies that employ highly trained and skilled scientists to carry out these tasks.
13. Partial structure; Physical and/or chemical properties; and Functional characteristics: In the instant case, it is evident that the genus of compounds embraced by formula (IIIA) has substantial variance. The claimed genus of formula (IIIA) is virtually without limit, embracing hundreds of thousands of potential compounds bearing little structural resemblance to one another, i.e., presently the genus of compounds according to formula (IIIA) embraces compound species wherein X is CH; Y1 and Y2 are CH; Z1 is NH; Z2 is C=O; and the ring containing R4 and R5 is 6-membered; and compound species wherein X is N; Y1 is N and Y2 is CH; Z1 is NH; Z2 is S=(O)2; and the ring containing R4 and R5 is 3-membered, which bear almost no structural overlap with each other. Regarding the limitation of “isotope derivative thereof” in the last line of claim 21, “derivatives” of those compounds in the claims could read on any analog, prodrug, and/or metabolite thereof, having widely varying groups that can be substituents of these compounds. It is noted that the specification fails to define or limit “derivatives” such that any chemical structures or substituents can be employed as “derivatives” and there is no clear structural limitation showing what substituents/ modifications could be made to the instant compounds of formula (IIIA). The Specification defines “isotope derivative” as:
“a presently disclosed compound including pharmaceutical salts and prodrugs thereof, each as described herein, in which one or more atoms are replaced by an atom having an atomic mass or mass number different from the atomic mass or mass number usually found in nature. Examples of isotopes that can be incorporated into compounds presently disclosed include isotopes of hydrogen, carbon, nitrogen, oxygen, phosphorous, fluorine and chlorine, such as 2H, 3H, 13C, 14C, 15N, 18O, 31P, 32P, 35S, 18F, and 36Cl, respectively.
By isotopically-labeling the presently disclosed compounds, the compounds may be useful in drug and/or substrate tissue distribution assays. Tritiated (3H) and carbon-14 (14C) labeled compounds are particularly preferred for their ease of preparation and detectability. Further, substitution with heavier isotopes such as deuterium (2H) can afford certain therapeutic advantages resulting from greater metabolic stability, for example increased in vivo half-life or reduced dosage requirements and, hence, may be preferred in some circumstances. Isotopically labeled compounds presently disclosed, including pharmaceutical salts, esters, and prodrugs thereof, can be prepared by any means known in the art. Benefits may also be obtained from replacement of normally abundant 12C with 13C.” (see paragraphs [0042]-[0043]). However, the Specification fails to disclose any examples or alternatives thereof. Thus the genus of “isotope derivative thereof” is virtually without limit.
The Specification teaches that the instant compounds are methionine aminopeptidase 2 (MetAP-2) inhibitors which are useful for treating various diseases and conditions including cancer, obesity, diabetes, rheumatoid arthritis and psoriasis (paragraph [0006]).
14. The method of making the claimed invention: The instant Specification discloses the preparation of only approximately 12 compound species that correspond to a compound of formula (IIIA), as recited in claim 65 (also see Examples 12-23 at pages 54-84), and fails to teach any isotopic forms or derivatives thereof.
15. While the MPEP does not define what constitutes a sufficient number of representative species, the courts have indicated what does not constitute a representative number of species to adequately describe a broad generic. For example, in In re Gostelli, the courts determined that the disclosure of two chemical compounds within a subgenus did not describe that subgenus. In re Gostelli, 872 F.2d 1008 (Fed. Cir. 1989). In the instant case, it is similarly determined that the disclosure of 12 structurally related compounds does not adequately describe a subgenus embracing hundreds of millions of additional compound species bearing no structural relationship with those 12 disclosed compounds. That is, the Specification does not disclose a sufficient variety of species to reflect the extreme variance in the genus.
16. The description requirement of the patent statue requires a description of an invention, not an indication of a result that one might achieve if one made that invention. See In re Wilder, 736, F.2d 1516, 1521, 222 USPQ 369, 372-73 (Fed. Cir. 1984) (affirming rejection because the specification does “little more than outlin[e] goals appellants hope the claimed invention achieves and the problems the invention will hopefully ameliorate”). Accordingly, it is deemed that the specification fails to provide adequate written description for the genus of the claims and does not reasonably convey to one skilled in the relevant art that the inventor(s), at the time the application was filed, had possession of the entire scope of the claimed invention.
17. As such, claims 21, 23-25, 66, and 76 are rejected.
Claim Objections
18. Claims 26-30, 65 and 67 are objected to as being dependent upon a rejected base claim, but would be allowable if rewritten in independent form including all of the limitations of the base claim and any intervening claims.
Conclusion
19. Claims 21, 23-30, 65-67, 76 and 77 are present in the application. Claim 77 is presently withdrawn as directed to a non-elected invention. Claims 21, 23-25, 66, and 76
are rejected. Claims 26-30, 65 and 67 are objected to. No claim is presently allowed.
20. Any inquiry concerning this communication or earlier communications from the examiner should be directed to JANET L COPPINS whose telephone number is (571)272-0680. The examiner can normally be reached Monday-Friday 8:30AM-5PM EST.
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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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/JANET L COPPINS/Examiner, Art Unit 1628
/AMY L CLARK/Supervisory Patent Examiner, Art Unit 1628