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 .
Detailed Action
Filing Receipt and Priority
The filing receipt mailed 05/07/2025 states that the instant application is a 371 of PCT/CN2021/104090, filed 07/01/2021.
The WO document submitted with the instant disclosure supports the instant claims. The effective filing date is 07/01/2021.
Information Disclosure Statement
The information disclosure statements received 01/02/2025, 02/06/2024, 05/22/2025 have been considered.
Objections
Claims 10, 16, 22, 28, 35, 41, 47 all state “crystalline form” and then refer to a specific form A-D.
Claim 10 refers to claim 5 which states “”The crystalline form of Claim 1 wherein the crystalline form is form B.” Similar wording is used in claim 16 referring to claim 11, claim 22, referring to claim 17, claim 28 referring to claim 23, claim 35 referring to claim 30, claim 41 referring to claim 36, and claim 47 referring to claim 42.
It is understood that when “crystalline form A” is used, it is synonymous with “form A”. However, the parent claims use “form A” or similar language. Claims should be amended for consistency.
Rejections
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.
Scope of Enablement – Method for Treating Cancer
Claim 48 and 56 is 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 treating non-small cell lung cancer, does not reasonably provide enablement for preventing or treating all cancers. 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. The following Wands Factors have been considered if not explicitly stated: (A) The breadth of the claims, (B) The nature of the invention, (C) The state of the prior art, (D) The level of one of ordinary skill, (E) The level of predictability in the art, (F) The amount of direction provided by the inventor, (G) The existence of working examples; and (H) The quantity of experimentation needed to make or use the invention based on the content of the disclosure.
Breadth of the claims
Claim 48 states “A method for treating cancer, comprising administering to a subject in need thereof a therapeutically effective amount of the composition of claim 1.”
Claim 56 states “A method for treating cancer, comprising administering to a subject in need thereof a therapeutically effective amount of the composition of claim 23.”
“Cancer” is not defined in the claims.
“Treating” is defined to include “reversing, alleviating, delaying the onset of, or inhibiting the progress of, a cancer or one or more symptoms thereof, as described herein.”
“Delaying the onset of” in understood to mean “prevention” as the onset of cancer is when the cancer begins to grow.
Nature of the invention
The invention is a clinical method for treating cancers.
State of the art
The compound I adipate is known within the art as Taletrectinib. Papadopoulos (Clin. Cancer Res; 26(18), 2020) on p. 4790, sec. Discussion reports taletrectinib is effective in treating non-small cell lung cancer (NCLC). No other cancers are discussed.
Working examples and guidance
The instant specification does not discuss any working examples of treating cancer.
Level of predictability
Considering the above, there is insufficient data to enable one of ordinary skill in the art to use the instant crystalline forms in methods to treat all cancers and/or prevention of any cancers.
Scope of Enablement – Method of Preparing
Claim 57 is 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 certain combinations of solvents and anti-solvents, does not reasonably provide enablement for all combinations of solvents and anti-solvents. 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.
The following Wands Factors have been considered if not explicitly stated: (A) The breadth of the claims, (B) The nature of the invention, (C) The state of the prior art, (D) The level of one of ordinary skill, (E) The level of predictability in the art, (F) The amount of direction provided by the inventor, (G) The existence of working examples; and (H) The quantity of experimentation needed to make or use the invention based on the content of the disclosure.
Breadth of the claim
Claim 57 states “A method of preparing a crystalline form of claim 1, the method comprising: mixing an amorphous form of Compound 1 adipate with a solvent; and adding an anti-solvent into the mixture to obtain the form A of Compound 1 adipate.
The terms “solvent” and “anti-solvent” are not defined by the specification. Therefore, the broadest reasonable interpretation includes all possible solvents and all possible anti-solvents.
State of the prior art
The closest art is found in Koike (US2020/0062765) which teaches dissolving compound I in a solution of ethanol and water. To this solution, adipic acid is added and the solution is stirred. Seed crystals were fed to the solution and the solution was eventually cooled to -1oC. Resulting crystals were filtered off and dried. These conditions are identical to conditions disclosed on p. 25-26, table 2 of the instant specification, shown below. Koike does not discuss other solvent and anti-solvent combinations.
Table 2
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534
350
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Direction provided and working examples
The instant specification discloses working combinations of solvent and anti-solvents, above. Note that not all combinations of solvent and anti-solvent give form A.
Level of predictability
Considering the table above, one of ordinary skill in the art would not predictability be able to form crystalline form A of compound I adipate using the combinations of solvent and anti-solvents that leads to the amorphous form, form C, or form D.
Written Description
Claims 1, 5, 10-11, 16-17, 21-23, 28, 30, 35-36, 41-42, 47-48, and 54-57 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 following claims fail to meet the written description requirement with regards to identifying the specific crystalline form of pemetrexed.
Claim 1 states “form B exhibiting an X-ray powder diffraction (XRPD) pattern that comprises at least one diffraction peak…”. This is repeated for forms C, and D. Forms B-D all include overlapping peaks which are 20.9±0.2o (Form B), 21.0±0.2o (Form C), and 20.9±0.2o (Form D). These peaks are all within the same range of each other. The claim also state “at least one” which requires only one peak is required to characterize the forms. Based on the overlapping peaks, one of ordinary skill would not be able to determine which form is which if only one peak is required. Claim 23 has a similar issue for forms B-D.
The x-ray pattern of a pure crystalline substance can be used to identify compounds because the diffraction pattern is considered to be a "fingerprint" of a compound. The d value for the most intense line is found and compared, followed by the next two intense lines, and so on.
Identification of crystal structures is taught by Bhattacharya et al. (Brittain, ed. Polymorphism in Pharmaceutical Solids, 2009, page 334). As noted in the fourth full paragraph, "it is usually convenient to identify the angles of the 10 most intense scattering peaks in a powder pattern" or the last paragraph which states 5 characteristic XRD (X-ray diffraction) scattering peaks of sodium ibandronate was sufficient to determine the difference in the two polymorphic forms.
Thus, one peak, especially one that overlaps on each form, cannot be used to identify an unknown compound.
As all other claims are dependent on claims 1 and 23, they are also rejected.
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.
Indefiniteness
Claims 48 and 56 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 48 states “A method for treating cancer, comprising administering to a subject in need thereof a therapeutically effective amount of the composition of claim 1.”
Claim 56 states “A method for treating cancer, comprising administering to a subject in need thereof a therapeutically effective amount of the composition of claim 23.”
Claims 1 and 23 do not claim a composition.
Art Rejection
Claim Rejections - 35 USC § 102
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) 1, 23, 28, 53 and 57 is/are rejected under 35 U.S.C. 102(a)(1) and (a)(2) as being anticipated by Koike (US2020/0062765).
Koike on p. 5, Examples 5-7 discloses processes of preparing The following compounds:
Formula 10, Koike
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244
340
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Formula 11, Koike
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210
344
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Koike in para. [0061] discloses dissolving compound of Formula 10 above in ethanol and water and then adding sodium hydroxide. This embraces the elements of claim 28.
Koike in para. [0063] discloses crystalizing compound of Formula II in a solvent system comprising ethanol and water. The instant specification on p. 24-31 discloses preparation of crystalline form A of compound 1 adipate. The specification on p. 24 states “A suitable amount of an amorphous form of Compound 1 adipate was dissolved in 0.5 mL of a solvent to form a solution. An anti-solvent was added to the solution thus obtained to obtain a solid, which was confirmed to be the crystalline form A of compound 1 adipate.” Table 2, shown above in the 112(a) rejection, shows that the combination of ethanol and water is suitable to form crystalline form A. Therefore, Koike discloses the same conditions that the instant specification states form crystalline form A. Therefore, while Koike does not disclose XRPD data or tetragonal crystal system, it embraces the elements of the claims.
Conclusion
No claims allowed.
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/L.G./Examiner, Art Unit 1624
/SUSANNA MOORE/Primary Examiner, Art Unit 1624