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 1-20, in the reply filed on May 11, 2026, is acknowledged.
Claims 21-24 (drawn to Groups II and III), are withdrawn from further consideration pursuant to 37 CFR 1.142(b) as being drawn to a nonelected invention, there being no allowable generic or linking claim.
4. Applicant additionally elected the species of Example 3:
(R)-6-Methyl-N-(pyridin-2-yl)-7,8-dihydro-6H-cyclopenta[e][1,24]triazolo1,3- a]pyridine-4-carboxamide or
(S)-6-Methyl-N-(pyridin-2-yl)-7,8-dihydro-6H- cyclopenta[e][1,2,4]triazolo[4,3-a]pyridine-4-carboxamide,
(i.e., Enantiomer 1 and Enantiomer 2).
5. Claims 1-20 are under examination and are the subject of this office action.
Information Disclosure Statement
6. The information disclosure statements (IDS) submitted on November 3, 2023, November 20, 2023, and March 11, 2026, are in compliance with the provisions of 37 CFR 1.97. Accordingly, the information disclosure statements have been considered by the examiner, please refer to the signed copies of Applicant’s PTO-1449 forms, attached herewith.
Specification
7. The disclosure is objected to for the following reasons: The Specification contains multiple instances of the term “novel,” i.e., “The present disclosure relates to novel AHR agonist compounds, [language omitted]”, in line 1, (see also page 108, line 1). It is suggested that the term “novel” be deleted from the language of 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 Specification is not appropriate. Appropriate correction is required. See MPEP § 608.01(b).
Claim Rejections - 35 USC § 112(b)
8. 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.
9. Claims 1-20 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.
10. Claims 1-5, 7-14, 17, 19 and 20 are rejected as being indefinite regarding the recitation of: “… a stereoisomer or mixture of stereoisomers thereof, or a pharmaceutically acceptable salt of each thereof” in the last two lines of each claim(s). It is not clear if the claimed “stereoisomer or mixture of stereoisomers” refers to the compound recited in the claim, or of an additional, as-yet unrecited stereoisomer(s).
11. Claims 1-14 and 17-20 are rejected as being indefinite regarding the recitation of: “or a pharmaceutically acceptable salt of each thereof” because it is not clear if Applicant intends for “each” to refer to just the compound, or the stereoisomer, or the mixture of stereoisomers, or all of the above. Clarification is requested.
12. Claims 6, 15, 16 and 18 are rejected as being dependent upon and including all of the limitations of rejected claim 1.
13. Claim 3 depends from claim 1 and recites the limitation:
"wherein
PNG
media_image1.png
96
113
media_image1.png
Greyscale
is selected from” and goes on to recite pyrazolyl, pyrimidinyl moieties. However, there is insufficient antecedent basis for these limitations in the claim, because claim 1 limits the “B” ring to “a phenyl, or a 5-membered or 6-membered heteroaryl having 1 or 3 heteroatoms… [language omitted],” [emphasis added]. That is, there is no prior recitation of a 5- or 6-membered heteroaryl moiety having 2 heteroatoms (as required by the pyrazolyl and pyrimidinyl rings recited in claim 3), because claim 1 requires that said ring has either 1 OR 3 heteroatoms.
14. Claim 4 depends from claim 1 and recites the limitation:
PNG
media_image2.png
96
96
media_image2.png
Greyscale
for the “B” ring moiety, wherein “W” can be CH or N.
However, there is insufficient antecedent basis for this limitation in the claim, because claim 1 limits the “B” ring to “a phenyl, or a 5-membered or 6-membered heteroaryl having 1 or 3 heteroatoms… [language omitted],” [emphasis added]. That is, there is no prior recitation of a 6-membered heteroaryl moiety having 2 heteroatoms (as required by the pyrimidinyl ring formed when “W” is N), because claim 1 requires that said ring has either 1 OR 3 heteroatoms.
15. Claim 8 depends from claim 1 and recites the limitation:
PNG
media_image2.png
96
96
media_image2.png
Greyscale
for the “B” ring moiety, wherein “W” can be CH or N.
However, there is insufficient antecedent basis for this limitation in the claim, because claim 1 limits the “B” ring to “a phenyl, or a 5-membered or 6-membered heteroaryl having 1 or 3 heteroatoms… [language omitted],” [emphasis added]. That is, there is no prior recitation of a 6-membered heteroaryl moiety having 2 heteroatoms (as required by the pyrimidinyl ring formed when “W” is N), because claim 1 requires that said ring has either 1 OR 3 heteroatoms.
16. Claims 14 and 15 each depend from claim 1 and recite multiple compound species wherein the moiety corresponding to the “B” ring is pyrimidinyl (i.e., 2 heteroatoms, thiazolyl (i.e., 2 heteroatoms), oxazolyl (i.e., 2 heteroatoms).
However, there is insufficient antecedent basis for these limitations in the claims, because claim 1 limits the “B” ring to “a phenyl, or a 5-membered or 6-membered heteroaryl having 1 or 3 heteroatoms… [language omitted],” [emphasis added]. That is, there is no prior recitation of a 5- or 6-membered heteroaryl moiety having 2 heteroatoms (as required by the pyrimidinyl, thiazolyl, and oxazolyl rings required by certain of the compound species in claims 14 and 15), because claim 1 requires that said ring has either 1 OR 3 heteroatoms.
17. Claims 16-19 each depend from claim 1 and recite a compound having the following “B” ring moiety:
PNG
media_image3.png
62
49
media_image3.png
Greyscale
. However, there is insufficient antecedent basis for this limitation in the claim, because claim 1 limits the “B” ring to “a phenyl, or a 5-membered or 6-membered heteroaryl having 1 or 3 heteroatoms… [language omitted],” [emphasis added]. That is, there is no prior recitation of a 6-membered heteroaryl moiety having 2 heteroatoms (as required by the pyrimidinyl ring required by claims 16-19), because claim 1 requires that said ring has either 1 OR 3 heteroatoms.
18. Claim 20 is indefinite in the following aspects:
(a) Claim 20 depends from claim 1, and also recites that the compound is “selected from Table 2, 2A, and 3,” in the Specification, which is confusing because it is not clear if the claim is reciting a compound of the formula of claim 1, or an additional compound described in Tables 2, 2A, and 3 in the disclosure.
(b) Claim 20 recites the limitation of Table 3 in line 1, however it is not clear which “Table 3” is intended, i.e., the Table 3 at pages 100-104, or the Table 3 at page 107.
(c) In the Specification, Tables 2, 2A and 3 contain multiple compound species wherein the moiety corresponding to the “B” ring is pyrimidinyl (i.e., 2 heteroatoms, thiazolyl (i.e., 2 heteroatoms), oxazolyl (i.e., 2 heteroatoms). There is insufficient antecedent basis for these limitations, because claim 1 limits the “B” ring to “a phenyl, or a 5-membered or 6-membered heteroaryl having 1 or 3 heteroatoms… [language omitted],” [emphasis added]. That is, there is no prior recitation of a 5- or 6-membered heteroaryl moiety having 2 heteroatoms (as required by the pyrimidinyl, thiazolyl, and oxazolyl rings required by certain of the compound species in Tables 2, 2A and 3), because claim 1 requires that said ring has either 1 OR 3 heteroatoms.
Clarification is requested.
Claim Rejections - 35 USC § 112(a)
19. 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.
20. Claims 1-20 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.
21. In particular, support cannot be found for the full scope of compounds of the formula of claim 1.
22. 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.
23. 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.
24. 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.
25. Partial structure; Physical and/or chemical properties; and Functional characteristics: In the instant case, claim 1 is drawn to the genus of compounds of the following formula:
PNG
media_image4.png
139
219
media_image4.png
Greyscale
, i.e., “B” can be any 5- or 6-membered heteroaryl having 1 or 3 heteroatoms selected from N, S, and O; and “Z” can be CH or N. Thus, the genus is extremely broad with substantial variance, embracing hundreds of thousands of potential compounds bearing little structural resemblance to one another. Yet, the instant Specification discloses only approximately 34 compound species within the recited formula, i.e., 68 enantiomeric compounds total, (see Examples 1-68 and Table 1A, 1B, 1C, 2A, and 3 at pages 85-103).
26. The instant specification teaches that the instantly recited compounds are aryl hydrogen receptor (AHR) agonists. AHR is known to regulate immunological function, and AHR agonists as a class are useful for treating certain immune-mediated diseases such as psoriasis and atopic dermatitis. The specification provides in vitro binding affinity for said enantiomers in the Table at page 107.
27. 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. A person of ordinary skill in the art from the specification or from the prior art cannot predict the pharmacological effects of administration of the instant formulation in subjects in regards to prevention of pain. 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.
28. 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 34 compounds (i.e., 68 enantiomeric species) does not adequately describe a subgenus embracing hundreds of thousands of additional compound species bearing little structural relationship with those 34 disclosed compounds. That is, the Specification does not disclose a sufficient variety of species to reflect the extreme variance in the genus.
29. Thus, Applicants have failed to provide guidance or data or evidence as to how the skilled artisan would be able to extrapolate from the disclosure to use the claimed invention. “A description of what a material does, rather than of what it is, usually does not suffice." Rochester, 358 F 3d at 923; Eli Lilly, 119 at 1568. Instead, 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).
30. 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.").
31. Accordingly, it is deemed that the specification fails to provide adequate written description for the claimed invention and does not reasonably convey to one skilled in the relevant art that the inventors had possession of the entire scope of the claimed invention.
Conclusion
32. Claims 1-24 are present in the application, and claims 21-24 are currently withdrawn. Claims 1-20 are rejected. No claim is presently allowed.
33. 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.
Examiner interviews are available via telephone, in-person, and video conferencing using a USPTO supplied web-based collaboration tool. To schedule an interview, applicant is encouraged to use the USPTO Automated Interview Request (AIR) at http://www.uspto.gov/interviewpractice.
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.
Information regarding the status of published or unpublished applications may be obtained from Patent Center. Unpublished application information in Patent Center is available to registered users. To file and manage patent submissions in Patent Center, visit: https://patentcenter.uspto.gov. Visit https://www.uspto.gov/patents/apply/patent-center for more information about Patent Center and https://www.uspto.gov/patents/docx for information about filing in DOCX format. For additional questions, contact the Electronic Business Center (EBC) at 866-217-9197 (toll-free). If you would like assistance from a USPTO Customer Service Representative, call 800-786-9199 (IN USA OR CANADA) or 571-272-1000.
/JANET L COPPINS/Examiner, Art Unit 1628
/Rayna Rodriguez/Primary Examiner, Art Unit 1628
Prosecution Insights