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 .
Application Status
2. Applicant’s amendment and response, submitted June 30, 2026, has been reviewed by the examiner and entered of record in the file. Claims 1, 3, 7, 32, 45, 148, 150, and 166 are amended. No claim is canceled or added.
3. Claims 49, 50, 76, 77, 89, 90, 96, 104, 110, 111, 117, 122, 124, 125, 128, 133, 136, 140, 141, 150, 152, and 166 remain withdrawn from further consideration pursuant to 37 CFR 1.142(b) as being drawn to the nonelected inventions of Groups II-VIII, without traverse, there being no allowable generic or linking claim.
4. Claims 1, 3, 7, 32, 45, 78 and 148 are under examination and are the subject of this office action.
Previous Claim Rejections - 35 USC § 112(b)
5. Claims 1, 3, 7, 32, 45, and 78 were previously rejected under 35 U.S.C. 112(b) or 35 U.S.C. 112 (pre-AIA ), second paragraph, as being indefinite regarding the limitation of “a composition.”
6. In view of Applicant’s amendment to delete the recitation of “composition” in line 4, the previous indefiniteness rejection is withdrawn.
New Claim Rejections - 35 USC § 112(b)
7. The text of those sections of Title 35, U.S. Code not included in this action can be found in a prior Office action.
8. Claims 1, 3, 7, 32, 45, 78 and 148 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.
This rejection is newly applied as a result of Applicant’s amendment to the claims.
10. Claim 1 recites the limitation "each occurrence of Ra is independently hydrogen, C1-C4 alkyl optionally substituted with 4-7 membered heterocyclyl … [language omitted]” in the last two lines of page 1 of the claims and the first two lines of page 2 of the claims. However, there is insufficient antecedent basis for this limitation in the claim, because there is no prior recitation of “Ra”, i.e., as a result of Applicant’s amendment of June 30, 2026, the Ra variable has been deleted.
11. Claim 7 is rejected as being unclear regarding the “R5a” and “R6a” moieties, which are not defined in the claim. And, there is insufficient antecedent basis for the limitations of R5a and R6a in the claim, because there is no prior recitation of “R5a” and “R6a” in claim 1.
12. Claim 32 recites the limitation "Ra is C1-C4 alkyl optionally substituted with 4-7 membered heterocyclyl… [language omitted]”. However, there is insufficient antecedent basis for this limitation in the claim, because there is no prior recitation of “Ra”, i.e., as a result of Applicant’s amendment of June 30, 2026, the Ra variable has been deleted.
13. Claims 3, 7, 32, 45, 78 and 148 are also rejected as being dependent upn and including all of the limitations of rejected claim 1.
Clarification is requested.
Previous Claim Rejections - 35 USC § 112(a)
14. Claims 1, 3, 7, 32, 45, 78 and 148 remain 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 regarding the scope of compounds and alternatives according to the genus of Formula (I’). 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. In particular, support cannot be found for the full scope of compounds of Formula (I’), or their stereoisomers, thereof as instantly recited by the claims.
15. This rejection has been modified as necessitated by Applicant’s amendment to the claims.
16. 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 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.
17. 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.
18. 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.
19. Partial structure; Physical and/or chemical properties; and Functional characteristics: The claims are drawn to a compound according to the vast genus of Formula (I’):
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, or a pharmaceutically acceptable salt or stereoisomer thereof, and its pharmaceutical composition thereof. In the instant case, it is evident that the genus of compounds embraced by formula (I’) has substantial variance. The claimed genus of formula (I’) is virtually without limit, embracing thousands of compounds, and potentially hundreds of thousands, which bear little structural overlap with one another, i.e., presently the genus of compounds according to formula (I’) embraces compound species wherein the variable R4 can be C3-C6 membered carbocycle, or any 4-7 membered heterocycle that is optionally substituted.
20. Regarding the term “stereoisomer,” the Specification defines the terms isomer and stereoisomer (paragraph [0095]) but does not disclose the preparation of any such stereoisomers other than the chirality indicated in Formula (I’) of claim 1, and fails to provide examples of such stereoisomers.
21. The instant compounds are alleged by the Specification to be transcriptional enhanced associate domain (TEAD) transcription factor inhibitors, which may be useful as therapeutics for the treatment of diseases associated with overexpression activity of a transcription factor (paragraph [004]).
22. Method of making: It is evident that the genus of compounds embraced by the claims has substantial variance, for example, the R4 moiety can comprise any C3-C6 membered carbocycle, or any 4-7 membered heterocycle that is optionally substituted, without limit, such that the scope of compounds of Formula (I’) recited by claim 1 embraces thousands of compound species, and potentially hundreds of thousands of compound species, as well as their stereoisomers and pharmaceutical compositions thereof. Yet, the instant Specification discloses the preparation of only four compound species according to Formula (I’) as broadly recited by the claims: see Table 10 (page 151) and the Syntheses of compounds I-1, I-6, I-7 and I-9 (pages 152-158).
23. 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 claim. 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 the preparation of just four compounds (i.e., I-1, I-6, I-7, and I-9), none of which comprising a carbocyclic or heterocyclic moiety for the R4 variable, does not adequately describe a genus embracing hundreds of thousands of possible compounds, stereoisomers, and compositions thereof. That is, the Specification does not disclose a sufficient variety of species to reflect the breadth of the possible compound and composition selections embraced by the claims.
24. The level of detail required to satisfy the written description requirement varies depending on the nature and scope of the claims and on the complexity and predictability of the relevant technology. Ariad, 598 F.3d at 1351, 94 USPQ2d at 1172; Capon v. Eshhar, 418 F.3d 1349, 1357-58, 76 USPQ2d 1078, 1083-84 (Fed. Cir. 2005). The fields of biology and chemistry are considered “unpredictable” because the complexity and unpredictability of chemical and biological interactions can make it difficult to understand the exact properties of an invention. The pharmaceutical industry is the prototypical example of a highly unpredictable field. Pfizer v. Teva Pharm., 482 F.Supp.2d 390, 413 (D.N.J. 2007); 2 Chisum on Patents § 5.04.
25. 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."). That is, the “disclosure must allow one skilled in the art to visualize or recognize the identity of the subject matter purportedly described.” Vas-Cath Inc. v. Mahurkar, 19 USPQ2d 1111, makes clear the "applicant must convey with reasonable clarity to those skilled in the art that, as of the filing date sought, he or she was in possession of the invention. The invention is, for purposes of the 'written description' inquiry, whatever is now claimed." (See page 1117.) The specification does not "clearly allow persons of ordinary skill in the art to recognize that [he or she] invented what is claimed." (See Vas-Cath at page 1116).
26. Accordingly, it is deemed that the specification fails to provide adequate written description for the genus of compounds of Formula (I’) and their pharmaceutically acceptable salts, stereoisomers, and/or compositions thereof as recited in 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.
As such, claims 1, 3, 7, 32, 45, 78 and 148 remain rejected.
Response to Arguments
27. In response to the written description rejection, Applicant submits that the claims have been amended to exclude solvates, hydrates, polymorphs, co-crystals, tautomers, prodrugs, and isotopically labeled derivatives, and that Formula I' has been amended to narrow the generic scope. Applicant alleges that the claims, as amended, are fully enabled by the specification.
28. Applicant's arguments have been fully considered but they are not persuasive. While it is acknowledged that the limitations of solvates, hydrates, polymorphs, co-crystals, tautomers, prodrugs, and isotopically labeled derivatives thereof have been deleted from the claims, the genus of Formula (I’) is still extremely broad relative to the disclosure. There is substantial variance between the heterocyclyl rings embraced by the R4 moiety, yet the Specification has not demonstrated support for all of the alternatives and stereoisomers thereof. That is, R4 comprises any 4-7 membered heterocycle that is optionally substituted, without limit, such that the scope of compounds of Formula (I’) embraces thousands of compound species, as well as their stereoisomers and pharmaceutical compositions thereof (claim 148). However, the instant Specification discloses the preparation of only four compound species according to Formula (I’) as broadly recited by the claims: see Table 10 (page 151) and the Syntheses of compounds I-1, I-6, I-7 and I-9 (pages 152-158), none of which comprise a carbocyclic or heterocyclic moiety for the R4 variable.
As such, the previous written description rejection is maintained.
Conclusion
29. Claims 1, 3, 7 ,32, 45, 49-50, 76-78, 89-90, 96, 104, 110-111, 117, 122, 124-125, 128, 133, 136, 140-141, 148, 150, 152, and 166 are present in the application. Claims 49, 50, 76, 77, 89, 90, 96, 104, 110, 111, 117, 122, 124, 125, 128, 133, 136, 140, 141, 150, 152, and 166 remain withdrawn. Claims 1, 3, 7, 32, 45, 78 and 148 are rejected. No claim is presently allowable.
30. Applicant's amendment necessitated the new ground(s) of rejection presented in this Office action. Accordingly, THIS ACTION IS MADE FINAL. See MPEP § 706.07(a). Applicant is reminded of the extension of time policy as set forth in 37 CFR 1.136(a).
A shortened statutory period for reply to this final action is set to expire THREE MONTHS from the mailing date of this action. In the event a first reply is filed within TWO MONTHS of the mailing date of this final action and the advisory action is not mailed until after the end of the THREE-MONTH shortened statutory period, then the shortened statutory period will expire on the date the advisory action is mailed, and any nonprovisional extension fee (37 CFR 1.17(a)) pursuant to 37 CFR 1.136(a) will be calculated from the mailing date of the advisory action. In no event, however, will the statutory period for reply expire later than SIX MONTHS from the mailing date of this final action.
31. 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
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