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 .
Status of the Application
Claims 1-20 are pending as of the response filed 03/19/2026. Claims 14-20 are newly added. Claims 1-20 are examined herein.
The 35 U.S.C. § 112(a) rejection of previous record is maintained and updated to reflect the claim amendments.
The nonstatutory double patenting rejection of previous record is maintained and updated to reflect the claim amendments.
Applicant’s arguments have been fully considered and are addressed below.
Information Disclosure Statement
The information disclosure statement submitted on 03/19/2026 is in compliance with the provisions of 37 CFR 1.97. Accordingly, the information disclosure statement is being considered by the examiner.
Claim Rejections - 35 USC § 112 - Written Description – Maintained and updated
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 1-4, 6-15 and 17-20 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 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 1 is drawn to a crystalline form I of a compound of the following formula 1, a pharmaceutically acceptable salt thereof, or a solvate thereof, wherein the X-ray powder diffraction pattern has 5 or more characteristic peaks selected from among peaks with the following diffraction angles (2θ values) of: 7.19±0.2°, 9.58±0.2°, 10.87±0.2°, 12.50±0.2°, 14.73±0.2°, 17.38±0.2°, 18.22±0.2°, 18.59±0.2°, 19.03±0.2°, 20.61±0.2°, 21.14±0.2°, 21.82±0.2°, 22.42±0.2°, 23.18±0.2°, 24.15±0.2°, 24.92±0.2°, 25.55±0.2°, 27.04±0.2°, 28.75±0.2°, and 29.85±0.2°;
PNG
media_image1.png
270
251
media_image1.png
Greyscale
wherein R1 is C2-C5 alkyl.
The claims are drawn to a multitude of compounds of crystalline form I, characterized by a subset of the recited X-ray powder diffraction peaks (5 or more peaks). The compounds include pharmaceutically acceptable salts, or a solvate thereof, of the compound of formula I, wherein R1 can be C2-C5 alkyl. The X-ray diffraction pattern of a pure crystalline substance can be used to identify the compound because the X-ray diffraction pattern is considered to be a "fingerprint" of a compound. The instant specification discloses the preparation and corresponding X-ray diffraction pattern of a single species of compound encompassed by claim 1 in example 1 (compound of formula 4 as in instant claim 5) in Paras [00147]-[00158]. This is not viewed as being reasonably representative of the genus of compounds exhibiting the X-ray diffraction peaks in its claimed scope because no readily apparent combination of identifying characteristics is provided, other than the disclosure of these specific species as examples of the claimed genus. The instant specification does not describe in sufficient detail the preparation of additional species of compounds/conditions of crystallization for the claimed genus of crystalline compounds.
The MPEP lists factors that can be used to determine if sufficient evidence of possession has been furnished in the disclosure of the Application. Whether the specification shows that the inventor was in possession of the claimed invention is not a single, simple determination, but rather is a factual determination reached by considering a number of factors. Factors to be considered in determining whether there is sufficient evidence of possession include the level of skill and knowledge in the art, partial structure, physical and/or chemical properties, functional characteristics alone or coupled with a known or disclosed correlation between structure and function, and the method of making the claimed invention. Disclosure of any combination of such identifying characteristics that distinguish the claimed invention from other materials and would lead one of skill in the art to the conclusion that the applicant was in possession of the claimed species is sufficient. See Eli Lilly, 119 F.3d at 1568, 43 USPQ2d at 1406. See MPEP 2163 (II) 3 (a) (i).
A chemical genus can be adequately described if the disclosure presents a sufficient number of representative species that encompass the genus. If the genus has substantial variance, the disclosure must describe a sufficient number of species to reflect the variation within that genus. The written description requirement for a claimed genus may be satisfied through sufficient description of a representative number of species by actual reduction to practice (see i)(A) above), reduction to drawings (see i)(B) above), or by disclosure of relevant, identifying characteristics, i.e., structure or other physical and/or chemical properties, by functional characteristics coupled with a known or disclosed correlation between function and structure, or by a combination of such identifying characteristics, sufficient to show the inventor was in possession of the claimed genus (see i)(C) above). See Eli Lilly, 119 F.3d at 1568, 43 USPQ2d at 1406. A "representative number of species" means that the species which are adequately described are representative of the entire genus. Thus, when there is substantial variation within the genus, one must describe a sufficient variety of species to reflect the variation within the genus. See AbbVie Deutschland GmbH & Co., KG v. Janssen Biotech, Inc., 759 F.3d 1285, 1300, 111 USPQ2d 1780, 1790 (Fed. Cir. 2014). The disclosure of only one species encompassed within a genus adequately describes a claim directed to that genus only if the disclosure "indicates that the patentee has invented species sufficient to constitute the gen[us]." See Enzo Biochem, 323 F.3d at 966, 63 USPQ2d at 1615. "A patentee will not be deemed to have invented species sufficient to constitute the genus by virtue of having disclosed a single species when … the evidence indicates ordinary artisans could not predict the operability in the invention of any species other than the one disclosed. See MPEP 2163 (II) 3 (a) (ii).
In the instant case, there is no evidence Applicants had possession of the full genus of compounds at the time of filing, because the specification does not provide examples of enough species of compounds that exhibit an X-ray diffraction pattern characterized by 5 or more peaks recited in claim 1. Thus, the written description requirement for the claimed genus of crystalline compounds of form I has not been met.
Claims 2-4, 6-15 and 17-20 depend from claim 1 and are similarly rejected.
In response to this rejection, the Applicant can amend the claim(s) to recite only individual species or grouping of species that are shown to exhibit the recited characteristic X-ray diffraction pattern, or present a sufficient showing that the species recited in the alternative of the claims in fact exhibits an X-ray diffraction pattern characterized by 5 or more peaks recited in claim 1.
Response to Arguments
Applicants argue on page 6 of the response dated 03/19/2026, that “Applicant submits that the structural feature wherein the claimed crystalline from I has 5 or more characteristic X-ray powder diffraction peaks is supported by the written description and demonstrates possession of the crystalline form I across the entire claim scope at the time of filing. Applicant respectfully requests reconsideration of the rejection under 35 U.S.C. § 112(a) in view of this amendment.”
Applicant's arguments have been fully considered but they are not persuasive. Applicants have not demonstrated that the written description is adequate to support the multitude of compounds of crystalline form I, characterized by a subset of the recited 5 or more X-ray powder diffraction peaks. Applicants have not explained or pointed to specific support in the specification that adequately describes a “representative number of species” of the claimed genus. Considering the unpredictability in the field of pharmaceutical crystalline forms and since it is known in the art that small changes in structure can cause large changes in the X-ray powder diffraction peaks, it is not readily apparent that the data provided in the instant disclosure can be expanded or generalized to the scope of the genus of compounds of formula I being claimed.
According to MPEP 2145(I), “Arguments presented by applicant cannot take the place of evidence in the record. See In re De Blauwe, 736 F.2d 699, 705, 222 USPQ 191, 196 (Fed. Cir. 1984); In re Schulze, 346 F.2d 600, 602, 145 USPQ 716, 718 (CCPA 1965); In re Geisler, 116 F.3d 1465, 43 USPQ2d 1362 (Fed. Cir. 1997)”.
Thus, the written description rejection is maintained.
Double Patenting – Maintained and updated
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 USPTO Internet website contains terminal disclaimer forms which may be used. Please visit www.uspto.gov/patent/patents-forms. The 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/process/file/efs/guidance/eTD-info-I.jsp.
Claims 1-4 and 11-20 are provisionally rejected on the ground of nonstatutory double patenting as being unpatentable over claims 1-4 and 11-26 of co-pending Application No 18/258,711.
Although the claims at issue are not identical, they are not patentably distinct from each other because both sets of claims are drawn to crystalline form I of a compound of formula 1, wherein R1 is C2-C5 alkyl, a pharmaceutically acceptable salt thereof, or a solvate thereof.
The instant claims are drawn to
PNG
media_image2.png
579
645
media_image2.png
Greyscale
The claims of the co-pending Application No 18/258,711 are drawn to
PNG
media_image3.png
605
654
media_image3.png
Greyscale
Although the X-ray diffraction peaks of the reference application do not exactly coincide with the instant claims, at least 5 of the characteristic peaks are within the ±0.2° 2θ values recited in the instant claim. The reference application’s peak value of 9.363±0.2°, 10.5969±0.2°, 12.841±0.2°, 17.305±0.2° and 18.364±0.2° anticipates the 9.58±0.2°, 10.87±0.2°, 12.50±0.2°, 17.38±0.2° and 18.22±0.2° peaks of the instant claims, respectively. This renders the instant claims (with respect to a crystalline form I, a pharmaceutical composition and a method for agonizing the function of a melanocortin-4 receptor) prima facie obvious, since both claims are drawn to crystalline form I of a compound of formula 1, with at least 5 overlapping characteristic peaks in the X-ray diffraction pattern.
Thus claims 1-4 and 11-26 of co-pending application 18/258,711 and the instant claims 1-4 and 11-20 are not patentably distinct.
This is a provisional nonstatutory double patenting rejection because the patentably indistinct claims have not in fact been patented.
Allowable Subject Matter
The crystalline form I of a compound of formula 1 as in claim 1 has been found to be free of prior art. Except for the 35 U.S.C. 112(a) and nonstatutory double patenting rejection drafted above, all claims would be allowable.
Claim 5 is 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.
The closest prior art of record is Choi et al. (US 2009/298829 A1, 03 December 2009, hereinafter Choi, in the IDS). Choi teaches a compound of formula 1, pharmaceutically acceptable salt and isomer thereof effective as agonist of melanocortin receptor (Abstract; Para. [0009]; Paras. [0013]-[0029]) for use in the prevention and treatment of obesity, diabetes, inflammation or erectile dysfunction (Para. [0012]).
PNG
media_image4.png
147
374
media_image4.png
Greyscale
Choi teaches the following exemplary compound, A96 (Pg. 26, TABLE 4, third compound).
PNG
media_image5.png
288
664
media_image5.png
Greyscale
PNG
media_image6.png
119
643
media_image6.png
Greyscale
Compound A96 of Choi has close structural similarity to the instant compounds of formula 1. Compound A96 of Choi differs from the instant compounds in the 4,4-dimethylcyclohexyl group versus the instantly claimed 4-methylcyclohexyl group and a methyl versus the instantly claimed C2-C5 alkyl group for R1 in instant formula 1.
However, Choi do not disclose crystalline forms of the melanocortin receptor agonist compounds. There is no teaching or suggestion in the prior art regarding specific crystalline forms of the compound of formula 1 of the instant claims or a process of producing the same. Therefore, the instant claims are novel and non-obvious.
Conclusion
Claims 1-4 and 6-20 are rejected.
Claim 5 is objected to.
No claims are allowed.
THIS ACTION IS MADE FINAL. 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.
Any inquiry concerning this communication or earlier communications from the examiner should be directed to PADMAJA S RAO whose telephone number is (571)272-9918. The examiner can normally be reached 9:00-5:30 pm EDT.
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, Kortney L Klinkel can be reached on (571) 270-5239. 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.
/PADMAJA S RAO/Examiner, Art Unit 1627
/SARAH PIHONAK/Primary Examiner, Art Unit 1627
Prosecution Insights