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 .
Priority
Examiner acknowledges that, according to the Filing receipt received 02/25/2025, that the instant application 18/836,748 filed 08/07/2024 is a 371 of PCT/CN2023/000038 filed 02/07/2023, which claims foreign priority of Chinese applications CN202210120295.0 filed 02/07/2022 and CN20231008505.1 filed 01/04/2023.
Information Disclosure Statement
The Information Disclosure Statement filed on 08/07/2024 is in compliance with the provisions of 37 CFR 1.97 and has been considered in full. A signed copy of list of references cited from the IDS is included with this Office Action.
Specification
Applicant is reminded of the proper language and format for an abstract of the disclosure.
The abstract should be in narrative form and generally limited to a single paragraph on a separate sheet within the range of 50 to 150 words in length. The abstract should describe the disclosure sufficiently to assist readers in deciding whether there is a need for consulting the full patent text for details.
The language should be clear and concise and should not repeat information given in the title. It should avoid using phrases which can be implied, such as, “The disclosure concerns,” “The disclosure defined by this invention,” “The disclosure describes,” etc. In addition, the form and legal phraseology often used in patent claims, such as “means” and “said,” should be avoided.
The abstract of the disclosure is objected to because it contains phrases which can be implied (i.e., "Disclosed in the present invention"). A corrected abstract of the disclosure is required and must be presented on a separate sheet, apart from any other text. See MPEP § 608.01(b).
Claim Rejections - 35 USC § 101
35 U.S.C. 101 reads as follows:
Whoever invents or discovers any new and useful process, machine, manufacture, or composition of matter, or any new and useful improvement thereof, may obtain a patent therefor, subject to the conditions and requirements of this title.
Claims 22 and 23 are rejected under 35 U.S.C. 101 because the claimed invention is directed to non-statutory subject matter. The claim(s) does/do not fall within at least one of the four categories of patent eligible subject matter because they are directed toward a "use" of a polymorph (claim 22) or a pharmaceutical composition thereof (claim 23). The claims fail to recite any requisite steps to be considered a process, nor do the claims purport to claim a machine, manufacture, or composition of matter.
Claim Rejections - 35 USC § 112(b)
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 21-23 and 25 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 21 is directed toward a pharmaceutical composition comprising a polymorph according to claim 1 and a pharmaceutically acceptable carrier and/or excipient. Paragraph [0114] sets forth exemplary excipients, including diluents and solvents in which the claimed polymorphs may be soluble (e.g., ethanol, water; see paragraph [0100]). It is unclear how the crystalline form of the claimed polymorph would be maintained if the polymorph is dissolved in solution. Claims 23 and 25 do not clarify the limitation at issue and are also rejected.
Claims 22 and 23 are “use” claims that fail to set forward any requisite steps. The scope of the claims is unclear as no guidance is provided as to how such “uses” are practiced.
Claim Rejections - 35 USC § 112(a)
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 and 21-25 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 directed toward a polymorph of a compound of formula I:
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wherein n is 0 to 2 and X is H2O. Claim 1, however, is not supported by adequate description of any polymorph of formula I. A claimed crystalline polymorph is generally considered adequately described when characterized by at least five XRPD peaks. See Brittain (2009), page 334.
Additionally, while claim 1 is directed toward a polymorph of a generic compound of formula I, wherein n is 0 to 2 and X is H2O, the instant specification only sets forth exemplary polymorphs wherein n is 0 or, if X is H2O, n is 2. Specifically, only forms A, C, L, P, and V fall within the scope of the claims. No examples are described for polymorphs wherein n is any number between 0 and 2 (be it 1 or a non-integer).
Vas-Cath Inc. V. Mahurkar, 19 USPQ2d 1111, states that 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, for purposes of the written description inquiry, is whatever is now claimed (see page 1117). A review of the language of the claims indicates that these claims are drawn to a generic formula.
To provide adequate written description and evidence of possession of a claimed genus, the specification must provide sufficient distinguishing characteristics of the genus. The factors to be considered include disclosure of complete or partial structure, physical and/or chemical properties, functional characteristics, structure/function correlation, methods of making the claimed product, or any combination thereof.
Applicant has therefore only provided adequate written description for forms A, C, L, P, and V wherein no other polymorphs within the scope of the claimed invention could be ascertained by one of ordinary skill in the art in view of the instant disclosure. One of ordinary skill in the art would not be apprised that Applicant was in possession of the full scope of the claimed invention at the time of filing. Correction is required.
Claim Rejections - 35 USC § 112(d)
The following is a quotation of 35 U.S.C. 112(d):
(d) REFERENCE IN DEPENDENT FORMS.—Subject to subsection (e), a claim in dependent form shall contain a reference to a claim previously set forth and then specify a further limitation of the subject matter claimed. A claim in dependent form shall be construed to incorporate by reference all the limitations of the claim to which it refers.
The following is a quotation of pre-AIA 35 U.S.C. 112, fourth paragraph:
Subject to the following paragraph [i.e., the fifth paragraph of pre-AIA 35 U.S.C. 112], a claim in dependent form shall contain a reference to a claim previously set forth and then specify a further limitation of the subject matter claimed. A claim in dependent form shall be construed to incorporate by reference all the limitations of the claim to which it refers.
Claims 3-4, 7-8, 11, 14-15, and 18-19 are rejected under 35 U.S.C. 112(d) or pre-AIA 35 U.S.C. 112, 4th paragraph, as being of improper dependent form for failing to further limit the subject matter of the claim upon which it depends, or for failing to include all the limitations of the claim upon which it depends.
Claims 3-4 depend on claim 2, wherein claim 2 is directed toward a polymorph of Form A. Claims 7-8 depend on claim 6, wherein claim 6 is directed toward a polymorph of Form C. Claim 11 depends on claim 10, wherein claim 10 is directed toward a polymorph of Form L. Claims 14-15 depend on claim 13, wherein claim 13 is directed toward a polymorph of Form P. Claims 18-19 depend on claim 17, wherein claim 17 is directed toward a polymorph of Form V. While claims 3-4, 7-8, 11, 14-15, and 18-19 set forth additional peaks and/or patterns (XRPD, DSC, TGA) associated with the polymorphic forms of the claims from which they depend, these claims set forth details which are inherent to the scope of their respective polymorphic forms as set forth in the specification. Therefore, claims 3-4 set forth limitations that are necessarily within the scope of claim 2; claims 7-8 set forth limitations that are necessarily within the scope of claim 6; claim 11 sets forth limitations that are necessarily within the scope of claim 10; claims 14-15 set forth limitations that are necessarily within the scope of claim 13; and claims 18-19 set forth limitations that are necessarily within the scope of claim 17; therefore failing to further limit the subject matter from the claims upon which they depend.
Applicant may cancel the claim(s), amend the claim(s) to place the claim(s) in proper dependent form, rewrite the claim(s) in independent form, or present a sufficient showing that the dependent claim(s) complies with the statutory requirements.
Claim Rejections - 35 USC § 102
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 the appropriate paragraphs of 35 U.S.C. 102 that form the basis for the rejections under this section made in this Office action:
A person shall be entitled to a patent unless –
(a)(1) the claimed invention was patented, described in a printed publication, or in public use, on sale, or otherwise available to the public before the effective filing date of the claimed invention.
(a)(2) the claimed invention was described in a patent issued under section 151, or in an application for patent published or deemed published under section 122(b), in which the patent or application, as the case may be, names another inventor and was effectively filed before the effective filing date of the claimed invention.
Claim(s) 21 is/are rejected under 35 U.S.C. 102(a)(1) and (a)(2) as being anticipated by Jin et al. (WO 2019/240938 A1; IDS filed 08/07/2024).
Jin et al. discloses the following compound, Example 51 (p. 142).
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Example 51 is identical to a compound of formula I wherein n is 0. Jin et al. discloses Example 51 in solution with acetic acid prior to purification (p. 144, par. [00471]). As in the above rejection under 35 U.S.C. 112(b), the scope of claim 21 includes compounds of formula I wherein the polymorphic form is in solution, in which the crystalline structure would not be maintained.
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.
This application currently names joint inventors. In considering patentability of the claims the examiner presumes that the subject matter of the various claims was commonly owned as of the effective filing date of the claimed invention(s) absent any evidence to the contrary. Applicant is advised of the obligation under 37 CFR 1.56 to point out the inventor and effective filing dates of each claim that was not commonly owned as of the effective filing date of the later invention in order for the examiner to consider the applicability of 35 U.S.C. 102(b)(2)(C) for any potential 35 U.S.C. 102(a)(2) prior art against the later invention.
Claim(s) 1 and 22-25 is/are rejected under 35 U.S.C. 103 as being unpatentable over Jin et al. (WO 2019/240938 A1; IDS filed 08/07/2024).
Jin et al. discloses as in the above rejection under 35 U.S.C. 102(a)(1) and (a)(2).
While Jin et al. does not explicitly teach a polymorph of Example 51, the use of Example 51 or a composition thereof for manufacturing a medicament for treating primary hypercholesterolemia, or a method of treating primary hypercholesterolemia comprising administering a polymorph of Example 51 or a composition thereof, these limitations are obvious over Jin et al.
Jin et al. additionally teaches that the disclosed compounds and compositions can be used to treat hypercholesterolemia1 (par. [00237]) and methods of treatment thereof (par. [00236]). Jin et al. discloses purifying Example 51 which affords a white solid (par. [00471]) and additionally suggests crystallizing the disclosed compounds, including crystallizing with pharmaceutically acceptable solvents such as water (par. [00223]).
As such, it would be prima facie obvious for one of ordinary skill in the art to crystallize the compound of Example 51. One would be motivated to do so, with reasonable expectation of success, as Jin et al. suggests that the solvated and unsolvated forms can be formed during the process of preparing the compounds (par. [00223]). One of ordinary skill in the art would be apprised that pursuing crystallized forms of Example 51 would provide additional avenues for treating diseases such as hypercholesterolemia.
It would be prima facie obvious to use the crystallized form of Example 51 for manufacture of a medicament or method of treating hypercholesterolemia. One would be motivated to do so, with reasonable expectation of success, as Jin et al. discloses that the compounds are thyroid hormone receptor agonists preferably for treatment of hypercholesterolemia, wherein Example 51 is particularly efficacious in its binding activity compared to other compounds (see Table 2, pages 153-154).
Allowable Subject Matter
Claims 2, 6, 10, 13, and 17 are objected to as being dependent upon a rejected base claim, but are free of the art. The closest prior art is Jin et al. (WO 2019/240938 A1; IDS filed 08/07/2024) as cited above. However, Jin et al. does not teach or suggest the particular polymorphs of claims 2, 6, 10, 13, and 17 and their requisite peaks, nor would any of the polymorphs be readily predicted or ascertained from the disclosure of Jin et al.
Conclusion
Claims 1, 3-4, 7-8, 11, 14-15, 18-19, and 21-25 are rejected. Claims 2, 6, 10, 13, and 17 are objected to.
Any inquiry concerning this communication or earlier communications from the examiner should be directed to MADELINE E BRAUN whose telephone number is (703)756-4533. The examiner can normally be reached M-F 8:30am-5:00pm ET.
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/MADELINE E BRAUN/Examiner, Art Unit 1624 06/24/2026
1 Examiner notes that this teaching is additionally admitted by Applicant on page 2 of the instant specification (par. [0004]).
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