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 07/07/2025, that the instant application 18/724,189 filed 06/25/2024 is a 371 of PCT/CN2023/073323 filed 01/20/2023 which claims foreign priority of Chinese application 202210078957.2 filed 01/24/2022.
Acknowledgment is made of applicant's claim for foreign priority. It is noted, however, that applicant has not provided an English translation of the certified copy of Chinese application 202210078957.2 as required by 35 U.S.C. 119(b). Therefore, art published prior to the PCT date, but not before the date of Chinese application 202210078957.2 has been cited against the claims.
Information Disclosure Statement
The Information Disclosure Statements filed on 06/25/2024 and 05/12/2026 are in compliance with the provisions of 37 CFR 1.97 and have been considered in full. A signed copy of list of references cited from the IDS is included with this Office Action.
Claim Objections
Claims 1 and 4 are objected to because of the following informalities:
Claim 1: “halogen;;” should read “halogen;”.
Claim 4: The claim number for claim 4 is crossed out.
Appropriate correction is required.
Drawings
The drawings are objected to because the drawing on page 126 is not labeled by figure number and is located before the first page labeled “Drawings” (page 127). It is unclear whether this figure is part of the Abstract or the Drawings. Corrected drawing sheets in compliance with 37 CFR 1.121(d) are required in reply to the Office action to avoid abandonment of the application. Any amended replacement drawing sheet should include all of the figures appearing on the immediate prior version of the sheet, even if only one figure is being amended. The figure or figure number of an amended drawing should not be labeled as “amended.” If a drawing figure is to be canceled, the appropriate figure must be removed from the replacement sheet, and where necessary, the remaining figures must be renumbered and appropriate changes made to the brief description of the several views of the drawings for consistency. Additional replacement sheets may be necessary to show the renumbering of the remaining figures. Each drawing sheet submitted after the filing date of an application must be labeled in the top margin as either “Replacement Sheet” or “New Sheet” pursuant to 37 CFR 1.121(d). If the changes are not accepted by the examiner, the applicant will be notified and informed of any required corrective action in the next Office action. The objection to the drawings will not be held in abeyance.
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 1-16 and 18-21 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 1 is directed toward “A crystal form or an acidic salt of a compound”. It is unclear whether the scope of the claims requires or encompasses the acidic salt in a crystalline form. Moreover, claim 5 recites “preferably a crystal form of the acidic salt” and claims 11-12 and 14-16 recite “the acidic salt or crystal form thereof”. Claim 1 contains no clear indication that the acidic salt can be in crystalline form, such that these limitations appear to lack antecedent basis. Clarification is required. Claims 2-10, 13, and 18-21 do not clarify the limitation at issue and are similarly rejected.
Claim 1 recites “y is 0, 1, 2, 3, 4, or 5”. However, “y” cannot be 5 as each of the four carbons on the aryl ring substituted by R1 can only be substituted once. Therefore, “y” can be 4 at most. Claims 2-16 and 18-21 do not clarify the limitation at issue and are similarly rejected.
Claims 3-12 and 14 recite, at multiple occurrences, the phrases “preferably” and/or “more preferably” and/or “further preferably” preceded by a broader limitation and followed by a narrower limitation. The scope of the claims is indefinite as it is unclear whether the limitations following the phrases “preferably” and/or “more preferably” and/or “further preferably” are (a) merely exemplary of the remainder of the claim, and therefore not required, or (b) a required feature of the claims. Claim 21 requires the limitations at issue and are also rejected.
Claims 3-4 and 6-10 recite the phrase “for example”. The phrase "for example" renders the claims indefinite because it is unclear whether the limitation(s) following the phrase are part of the claimed invention. See MPEP § 2173.05(d). Claims 5, 11-12, 14, and 21 require the limitation at issue and are also rejected.
Claims 3, 6-10, and 21 recite “the above-mentioned 2Θ”. The term lacks antecedent basis as it is unclear what “above-mentioned 2Θ” refers to. Claims 5, 11-12, 14 require the limitation at issue and are also rejected.
Claims 3 and 6-10 recite the phrase “basically as shown in”. It is unclear to what degree of similarity the XRPD pattern must share to be considered “basically” the same as the figures referred to. Claims 4-5, 11-12, 14, and 21 require the limitation at issue and are also rejected.
Claim 11 recites “wherein the number of the acid is”. It is unclear what this limitation means or what “the number” refers to.
Claims 13 and 14 recite the term “same”. It is unclear what limitations are referred to using the term “same”.
Claim 14 recites “the free base crystal form” and “the target product”. These limitations lack antecedent basis.
Claims 16 and 19 recite the transitional phrase “includes” followed by a list of alternatives. A Markush grouping is a closed group of alternatives (MPEP 2173.05(h)). The phrase “includes” is open and causes confusion, as it is unclear what other alternatives are encompassed by the claims.
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 1-2, 4-5, 11-16, and 18-20 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.
The claims are directed toward a crystal form or an acidic salt of a compound of formula (I).
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Claim 1, however, is not supported by the instant disclosure for crystal forms or acidic salts of formula (I) generally. 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), the instant disclosure only sets forth one exemplary polymorph of the free base form of Compound 3 (see structure on page 59; see crystal form “a” on page 9) and one crystalline form of each of its hydrochloride, methanesulfonate, nitrate, sulfate, and hydrobromide salts respectively (see pages 10-43 which depict each crystalline salt form). Regarding claim 12, the instant disclosure provides no description of hydrates of acid salts for any of the claimed compounds, let alone Compound 3. The instant disclosure additionally fails to describe any other polymorphs or crystalline salts of Compound 3, nor does the instant disclosure describe any crystal forms or acidic salts of other compounds within the genus of formula (I), including those listed in claim 2. Crystalline forms and their physical properties, such as XRPD peaks, are not predictable and would not be readily envisaged by one of ordinary skill in the art absent adequate disclosure.
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 the crystalline forms listed above (i.e., each of the crystalline forms disclosed on paragraph [0011] page 5 through page 43), 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.
Claims 18-19 are rejected under 35 U.S.C. 112(a) or 35 U.S.C. 112 (pre-AIA ), first paragraph, because the specification, while being enabling for treatment of the claimed NK3 related diseases, does not reasonably provide enablement for prevention of the claimed NK3 related diseases. The specification does not enable any person skilled in the art to which it pertains, or with which it is most nearly connected, to use the invention commensurate in scope with these claims.
As stated in the MPEP 2164.01 (a), “There are many factors to be considered when determining whether there is sufficient evidence to support a determination that a disclosure does not satisfy the enablement requirement and whether any necessary experimentation is “undue.”
In In re Wands, 8 USPQ2d 1400 (1988), factors to be considered in determining whether a disclosure meets the enablement requirement of 35 U.S.C. 112, first paragraph, have been described. They are:
1. the nature of the invention,
2. the state of the prior art,
3. the predictability or lack thereof in the art,
4. the amount of direction or guidance present,
5. the presence or absence of working examples,
6. the breadth of the claims,
7. the quantity of experimentation needed, and
8. the level of the skill in the art.
It is presumed “prevention” of the claimed disease would require a method of identifying those individuals who will develop the claimed diseases before they exhibit symptoms. There is no evidence of record that would guide the skilled clinician to identify those who have the potential of becoming afflicted.
The factors to be considered in making an enablement rejection were summarized above. 1) As discussed above, preventing diseases requires identifying those patients who will acquire the disease before it occurs. This would require extensive and potentially opened ended clinical research on healthy subjects. 2) The scope of the claims is directed to treatment as well as prevention. 3) There is no working example of such a preventive procedure in man or animal in the specification. 4) The claims rejected are drawn to clinical pharmacology and are therefore physiological in nature. 5) The state of the art is that no general procedure is art-recognized for determining which patients generally will suffer from diseases such as cognitive impairment, Alzheimer’s disease, ADHD, or reproductive disorders before the fact. 6) The artisan using Applicants invention would be a Board-Certified physician in oncological diseases with an MD degree. Despite intensive efforts, pharmaceutical science has been unable to find a way of getting a compound to be effective for the prevention of diseases such as cognitive impairment, Alzheimer’s disease, ADHD, or reproductive disorders. Under such circumstances, it is proper for the PTO to require evidence that such an unprecedented feat has actually been accomplished, In re Ferens, 163 USPQ 609. No such evidence has been presented in this case. The failure of skilled scientists to achieve a goal is substantial evidence that achieving such a goal is beyond the skill of practitioners in that art, Genentech vs. Novo Nordisk, 42 USPQ2nd 1001, 1006. This establishes that it is not reasonable to any agent to be able to prevent diseases such as cognitive impairment, Alzheimer’s disease, ADHD, or reproductive disorders. That is, the skill is so low that no compound effective generally against the prevention of such diseases. 7) It is well established that "the scope of enablement varies inversely with the degree of unpredictability of the factors involved" and physiological activity is generally considered to be an unpredictable factor. See In re Fisher, 427 F.2d 833, 839, 166 USPQ 18, 24 (CCPA 1970). 8) The claims broadly read on all patients, not just those undergoing therapy for the claimed diseases.
MPEP 2164.01(a) states, "A conclusion of lack of enablement means that, based on the evidence regarding each of the above factors, the specification, at the time the application was filed, would not have taught one skilled in the art how to make and/or use the full scope of the claimed invention without undue experimentation. In re Wright, 999 F.2d 1557, 1562, 27 USPQ2d 1510, 1513 (Fed. Cir. 1993)." That conclusion is clearly justified here.
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.
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) 1-2, 4-5, 11-12, 15-16, and 18-20 is/are rejected under 35 U.S.C. 103 as being unpatentable over Su et al. (WO 2022/022680 A1; 2022; IDS filed 06/25/2024) in view of Berge et al. (Journal of Pharmaceutical Sciences; 1977). Examiner has partially relied upon an English translation of Su et al. which is referred to in the rejection below, of which a copy has been attached.
Su et al. discloses the following compounds (p. 54-104).
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The compounds disclosed by Su et al. are identical to those of instant claim 2. Su et al. additionally discloses that the compounds may be in the form of pharmaceutically acceptable salts thereof (p. 13, English translation) or hydrates (p. 7, English translation). Su et al. discloses pharmaceutical compositions comprising a therapeutically effective dose of the compounds and a pharmaceutically acceptable carrier (p. 6 & 12, English translation). Su et al. additionally discloses a method of treating NK3 related diseases selected from psychotic disorders, cognitive disorders, Parkinson's disease, pain, convulsions, obesity, inflammatory diseases, vomiting, preeclampsia, airway related diseases, reproductive disorders, sex hormone dependent diseases or gynecological diseases, as well as menopausal syndrome which includes symptoms such as hot flashes, sweating, palpitations, dizziness and obesity, wherein the method comprises administering a therapeutically effective amount of the compound or composition thereof (p. 6-7, English translation).
Su et al. does not disclose acid salts of the disclosed compounds, or particular amounts of the compound in the pharmaceutical composition. These limitations are obvious over Su et al. in view of Berge et al.
Berge et al. discloses that salt forms allow for the optimization of pharmaceutical properties (p. 1, col. 1) such as solubility and toxicity (p. 2, col. 2; p. 5, col. 1). Berge et al. discloses common commercially marketed salts, such as hydrochloride, hydrobromide, acetate, sulfate, succinate, and salicylate (Table I), wherein hydrochloride salts are the most popular selection due to availability and physiology (p. 2, col. 2).
It would be prima facie obvious for one of ordinary skill in the art to form acid salts of the compounds disclosed by Su et al. One would be motivated to try, with reasonable expectation of success, as Su et al. suggests the formation of pharmaceutical salts (as well as hydrates) of the disclosed compounds. Furthermore, Berge et al. discloses a list of salts commonly used in the formation of salts, including acidic salts wherein hydrochloride salts are most preferred. One of ordinary skill would be apprised that optimization of the pharmaceutical properties of the compounds of Su et al. by forming such salts at optimal stoichiometric ratios would be advantageous for treating NK3 related diseases.
Furthermore, it would be prima facie obvious for one of ordinary skill in the art to arrive at the claimed ranges of a therapeutically effective amount of the compound of Su et al. in a pharmaceutical composition. One would be motivated to do so, with reasonable expectation of success, in order to determine an effective dose of the compounds for treating NK3 related diseases. Per MPEP 2144.05, absent unexpected results, “Generally, differences in concentration or temperature will not support the patentability of subject matter encompassed by the prior art unless there is evidence indicating such concentration or temperature is critical. ‘[W]here the general conditions of a claim are disclosed in the prior art, it is not inventive to discover the optimum or workable ranges by routine experimentation.’ In re Aller, 220 F.2d 454, 456, 105 USPQ 233, 235 (CCPA 1955).”
Claim(s) 1, 4, 11-12, 15-16, and 18-19 is/are rejected under 35 U.S.C. 103 as being unpatentable over Wang et al. (WO 2020/211798 A1; 2020; IDS filed 06/25/2024) in view of Gordinier et al. (Academic Press; 2001) and Berge et al. (Journal of Pharmaceutical Sciences; 1977). Examiner has partially relied upon an English translation of Wang et al. which is referred to in the rejection below, of which a copy has been attached.
Wang et al. discloses the following compounds of generic formula (I) (p. 2) and species thereof (p. 132).
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The compounds are within the scope of instant formula (I) wherein R1 is halogen and R2 is 4- or 5-membered heterocyclyl. However, the phenyl group is not substituted by deuterium.
Wang et al. additionally discloses that R3 is selected from alternatives including hydrogen and deuterium (p. 3, English translation). Wang et al. teaches that the compounds include pharmaceutically acceptable salts and hydrates thereof (p. 16 & 21, English translation). Wang et al. discloses pharmaceutical compositions comprising a therapeutically effective dose of the compounds and a pharmaceutically acceptable carrier (p. 15 & 21, English translation). Wang et al. additionally discloses a method of treating NK3 related diseases selected from psychotic disorders, cognitive disorders, Parkinson's disease, pain, convulsions, obesity, inflammatory diseases, vomiting, preeclampsia, airway related diseases, reproductive disorders, sex hormone dependent diseases or gynecological diseases, as well as menopausal syndrome which includes symptoms such as hot flashes, sweating, palpitations, dizziness and obesity, wherein the method comprises administering a therapeutically effective amount of the compound or composition thereof (p. 15, English translation).
Wang et al. does not disclose acid salts of the disclosed compounds, or particular amounts of the compound in the pharmaceutical composition. These limitations are obvious over Wang et al. in view of Gordinier et al. and Berge et al.
Gordinier et al. discloses that the natural abundance of deuterium in water is 1 deuterium atom per every 6500 hydrogen atoms (p. 689, col. 1).
Berge et al. discloses that salt forms allow for the optimization of pharmaceutical properties (p. 1, col. 1) such as solubility and toxicity (p. 2, col. 2; p. 5, col. 1). Berge et al. discloses common commercially marketed salts, such as hydrochloride, hydrobromide, acetate, sulfate, succinate, and salicylate (Table I), wherein hydrochloride salts are the most popular selection due to availability and physiology (p. 2, col. 2).
It would be prima facie obvious for one of ordinary skill in the art to substitute the hydrogen of the phenyl group in the compounds of Wang et al. with deuterium. One would be motivated to do so, with reasonable expectation of success, as Wang et al. sets forth deuterium in a list of known, predictable alternatives that may be substituents of the disclosed compounds. Moreover, one of ordinary skill in the art would be apprised, based on the natural abundance of deuterium, that a fraction of the compounds disclosed by Wang et al. would be expected to contain deuterium rather than hydrogen as in the instant invention. Examiner further clarifies that the instant invention does not require any particular relative abundance of deuterium for the instantly claimed crystal forms and acid salts.
It would be prima facie obvious for one of ordinary skill in the art to form acid salts of the compounds disclosed by Wang et al. One would be motivated to try, with reasonable expectation of success, as Wang et al. suggests the formation of pharmaceutical salts (as well as hydrates) of the disclosed compounds. Furthermore, Berge et al. discloses a list of salts commonly used in the formation of salts, including acidic salts wherein hydrochloride salts are most preferred. One of ordinary skill would be apprised that optimization of the pharmaceutical properties of the compounds of Wang et al. by forming such salts at optimal stoichiometric ratios would be advantageous for treating NK3 related diseases.
Furthermore, it would be prima facie obvious for one of ordinary skill in the art to arrive at the claimed ranges of a therapeutically effective amount of the compound of Wang et al. in a pharmaceutical composition. One would be motivated to do so, with reasonable expectation of success, in order to determine an effective dose of the compounds for treating NK3 related diseases. Per MPEP 2144.05, absent unexpected results, “Generally, differences in concentration or temperature will not support the patentability of subject matter encompassed by the prior art unless there is evidence indicating such concentration or temperature is critical. ‘[W]here the general conditions of a claim are disclosed in the prior art, it is not inventive to discover the optimum or workable ranges by routine experimentation.’ In re Aller, 220 F.2d 454, 456, 105 USPQ 233, 235 (CCPA 1955).”
Double Patenting
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 filing of a terminal disclaimer by itself is not a complete reply to a nonstatutory double patenting (NSDP) rejection. A complete reply requires that the terminal disclaimer be accompanied by a reply requesting reconsideration of the prior Office action. Even where the NSDP rejection is provisional the reply must be complete. See MPEP § 804, subsection I.B.1. For a reply to a non-final Office action, see 37 CFR 1.111(a). For a reply to final Office action, see 37 CFR 1.113(c). A request for reconsideration while not provided for in 37 CFR 1.113(c) may be filed after final for consideration. See MPEP §§ 706.07(e) and 714.13.
The USPTO Internet website contains terminal disclaimer forms which may be used. Please visit www.uspto.gov/patent/patents-forms. The actual 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/apply/applying-online/eterminal-disclaimer.
Claims 1-2, 4-5, 11, 15-16, and 18-20 are provisionally rejected on the ground of nonstatutory double patenting as being unpatentable over claims 1, 10, 11, and 14 of copending Application No. 18/017,666 (“the ‘666 application”) further in view of Berge et al. (Journal of Pharmaceutical Sciences; 1977).
The claims of the ‘666 application are drawn to compounds of formula (I) (claim 1) and further to compounds of formula (II) (claim 10) as below, as well as pharmaceutically acceptable salts thereof, which substantially overlap with the instantly claimed compounds of formula (I).
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Claim 11 is further directed toward particular species that are identical to the compounds of instant claim 2, and pharmaceutically acceptable salts thereof, as below.
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Claim 14 is directed toward compositions comprising the compounds of claim 1 and a pharmaceutically acceptable carrier.
When making obviousness-type double patenting decisions, the Federal Circuit has stated, “[O]bviousness-type double patenting encompasses any use for a compound that is disclosed in the specification of an earlier patent claiming the compound and is later claimed as a method of using that compound”. Sun Pharm. Indus., Ltd. v. Eli Lilly & Co., 611 F.3d 1381 (Fed. Cir. 2010).
The specification of the ‘666 application further discloses a method of treating NK3 related diseases selected from psychotic disorders, cognitive disorders, Parkinson's disease, pain, convulsions, obesity, inflammatory diseases, vomiting, preeclampsia, airway related diseases, reproductive disorders, sex hormone dependent diseases or gynecological diseases, as well as menopausal syndrome which includes symptoms such as hot flashes, sweating, palpitations, dizziness and obesity, wherein the method comprises administering a therapeutically effective amount of the compound or composition thereof (p. 9-10, as filed 01/23/2023).
The claims of the ‘666 application do not disclose acid salts of the disclosed compounds, or particular amounts of the compound in the pharmaceutical composition. These limitations are obvious in view of Berge et al.
Berge et al. discloses that salt forms allow for the optimization of pharmaceutical properties (p. 1, col. 1) such as solubility and toxicity (p. 2, col. 2; p. 5, col. 1). Berge et al. discloses common commercially marketed salts, such as hydrochloride, hydrobromide, acetate, sulfate, succinate, and salicylate (Table I), wherein hydrochloride salts are the most popular selection due to availability and physiology (p. 2, col. 2).
It would be prima facie obvious for one of ordinary skill in the art to form acid salts of the compounds of the ‘666 application. One would be motivated to try, with reasonable expectation of success, as Wang et al. suggests the formation of pharmaceutical salts of the disclosed compounds. Furthermore, Berge et al. discloses a list of salts commonly used in the formation of salts, including acidic salts wherein hydrochloride salts are most preferred. One of ordinary skill would be apprised that optimization of the pharmaceutical properties of the compounds by forming such salts at optimal stoichiometric ratios would be advantageous for treating NK3 related diseases.
Furthermore, it would be prima facie obvious for one of ordinary skill in the art to arrive at the claimed ranges of a therapeutically effective amount of the compounds of the ‘666 application in a pharmaceutical composition. One would be motivated to do so, with reasonable expectation of success, in order to determine an effective dose of the compounds for treating NK3 related diseases. Per MPEP 2144.05, absent unexpected results, “Generally, differences in concentration or temperature will not support the patentability of subject matter encompassed by the prior art unless there is evidence indicating such concentration or temperature is critical. ‘[W]here the general conditions of a claim are disclosed in the prior art, it is not inventive to discover the optimum or workable ranges by routine experimentation.’ In re Aller, 220 F.2d 454, 456, 105 USPQ 233, 235 (CCPA 1955).”
This is a provisional nonstatutory double patenting rejection because the patentably indistinct claims have not in fact been patented.
Conclusion
No claims are allowed.
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 07/10/2026
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