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 1-2 and 4-10, in the reply filed on 05/20/2026 is acknowledged.
Accordingly, claims 13-15, 17-21, 23-26, 29, and 34-38 are withdrawn from further consideration as being drawn to a nonelected invention.
Status of Claims
Receipt of Remarks/Amendments filed on 05/21/2026 is acknowledged. Claims 1 and 23 are amended and claims 3, 11-22, 27-28, and 30-33 are canceled. Claims 23-26, 29, and 34-38 are withdrawn as discussed above. Claims 1-2 and 4-10 are examined on the merits herein.
Priority
The instant application filed 12/21/2023, claims benefit to Provisional Application No. 63/476,812, filed 12/22/2022.
Information Disclosure Statement
No information disclosure statement (IDS) has been filed at this time.
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 5 and 6 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.
Claims 5 and 6 recite weight percents without reciting the basis for such percents. For instance, are these amounts based on the total weight of the dispersion or are they based on the weight of a solvent?
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.
Claims 1-2 and 8 are rejected under 35 U.S.C. 102(a)(1)/(a)(2) as being anticipated by Wu et al. (US 20140213554 A1, 07/31/2014, PTO-892), hereinafter Wu.
Wu discloses compounds active on c-kit protein kinases or mutant c-kit protein kinases as well as methods of making and using such compounds (abstract).
Regarding claim 1: An active compound is 3,4-dimethyl-N-(2-phenyl-1H-pyrrolo[2,3-b]pyridin-5-yl)-1H-pyrazole-5-carboxamide (P-2007) ([0211]; Example 2), which reads on instantly claimed Compound I. The compounds are complexed to form an amorphous complex via spray-drying of the compound ([0543]). Such methods may also include addition of polymer systems, including hydroxypropyl methyl cellulose acetate succinate (HPMCAS), that further stabilize the amorphous nature of the complex ([0543]). A “spray-dried solid dispersion,” or “spray-dried dispersion” (SDD) is defined by the instant specification as a dispersion comprising a drug and a polymer, wherein the drug is non-crystalline and is amorphous ([0072]). As such, the spray-dried composition of Wu which includes an amorphous complex of the instantly claimed drug and polymer reads on a spray-dried solid dispersion wherein Compound I is dispersed in a polymer matrix.
Regarding claim 2: The compound ([0211]; Example 2) is preferably in the form of an amorphous complex ([0543]).
Regarding claim 8: Compounds can exist in solvated forms. Some examples of solvents include, but are not limited to, methanol, N,N-dimethylformamide, tetrahydrofuran, dimethylsulfoxide, and water ([0083]).
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.
1. Claims 1-2 and 4-10 are rejected under 35 U.S.C. 103 as being unpatentable over Lindemann et al. (US 20210387946 A1, 12/16/2021, PTO-892), hereinafter Lindemann, in view of Wu et al. (US 20140213554 A1, 07/31/2014, PTO-892), hereinafter Wu.
Regarding claim 1: Lindemann discloses solid dispersions comprising a compound of Formula (I) and a pharmaceutically acceptable polymer ([0004]; claims 1 and 6). The solid dispersion is obtained by spray drying ([0007]; [0015]; [0142]; Examples). The compound of Formula (I) is dispersed in a solid matrix that comprises the polymer(s) ([0048]; [0053]; [0081]).
Regarding claim 2: The solid dispersion is amorphous ([0006]).
Regarding claim 4: The polymer is hypromellose acetate succinate (HPMCAS), specifically HPMCAS-H (i.e., grade H) ([0004]; [0084]-[0085]; [0090]; Examples).
Regarding claim 5: The compound of Formula (I) (i.e., the active) is present in an amount of about 25% by weight of the solid dispersion ([0005]; [0093]; Examples).
Regarding claim 6: The polymer is present in an amount of about 75% by weight of the solid dispersion ([0005]; [0096]; Examples).
Regarding claim 7: The weight ratio of the compound of Formula (I) to the polymer is about 25:75 (i.e., 1:3) ([0005]; [0097]; Examples).
Regarding claim 8: The process for preparing a solid dispersion includes providing a solution of Formula (I) and a polymer in a solvent ([0015]; [0140]; claim 94).
Regarding claim 9: The solvent may comprise tetrahydrofuran, water, or a combination thereof ([0005]; [0141]).
Regarding claim 10: The solvent comprises up to 5% water ([0015]), meaning in a water and tetrahydrofuran combination the ratio would be 5:95 or 1:19.
Overall, the compositions of Lindemann have advantageous physical properties, which may provide benefits in processing, formulation, stability, bioavailability, storage, and handling, among other important pharmaceutical characteristics. The methods described allow for large-scale production compliant with good manufacturing practice (GMP) guidelines ([0041]).
The teachings of Lindemann differ from that of the instantly claimed invention in that Lindemann does not explicitly teach Compound (I) of the instant claims nor a specific embodiment wherein water and tetrahydrofuran are used at a ratio of claim 10.
Wu discloses compounds active on c-kit protein kinases or mutant c-kit protein kinases as well as methods of making and using such compounds (abstract). An active compound is 3,4-dimethyl-N-(2-phenyl-1H-pyrrolo[2,3-b]pyridin-5-yl)-1H-pyrazole-5-carboxamide (P-2007) ([0211]; Example 2), which reads on instantly claimed Compound (I). The compounds are complexed to form an amorphous complex via spray-drying of the compound ([0543]). Such methods may also include addition of polymer systems, including hydroxypropyl methyl cellulose acetate succinate (HPMCAS), that further stabilize the amorphous nature of the complex ([0543]). The compound ([0211]; Example 2) is preferably in the form of an amorphous complex ([0543]). Compounds can exist in solvated forms. Some examples of solvents include, but are not limited to, methanol, N,N-dimethylformamide, tetrahydrofuran, dimethylsulfoxide, and water ([0083]). Such amorphous complexes provide several advantages. For example, lowering of the melting temperature relative to the free base, facilitates additional processing, such as hot melt extrusion, to further improve the biopharmaceutical properties of the compound. Also, the amorphous complex is readily friable, which provides improved compression for loading of the solid into capsule or tablet form ([0543]).
It would have been prima facie obvious, prior to the effective filing date of the claimed invention, to one of ordinary skill in the art to replace the active of Lindemann with the active of Wu (i.e., Compound (I)) since the active of Wu is a known and routine active to be incorporated in a spray-dried polymer complex. One of ordinary skill in the art could have performed simple substitution of one known active for another to predictably yield the instant invention. Moreover, one of ordinary skill in the art would have been motivated to make such as substitution since formulating the active of Wu according to Lindemann would have reasonably improved the processing, stability, and biopharmaceutical properties of the active in the same way described by Lindemann. One of ordinary skill in the art would have had a reasonable expectation of success in making such a modification since Wu teaches that Compound (I) can be formulated in a spray-dried amorphous complex with a polymer such as HPMCAS and that solvents such as tetrahydrofuran and water may be used. Such a combination reads on the spray-dried solid dispersion of claims 1-2 and 4-9.
Regarding the ratio of water to tetrahydrofuran in claim 10, it would have been prima facie obvious to use a combination of water and THF at a ratio of 1:19 since this is a known and routine ratio in the art as taught by Lindemann. Lindemann teaches that a combination of water and THF can be utilized as the solvent and that the solvent may comprise up to 5% water. In combination, these two teachings result in a ratio of 1:19. Therefore, one of ordinary skill in the art would have arrived at the instantly claimed ratio by combining embodiments of Lindemann, which involves no more than choosing from a finite number of identified, predictable solutions, with a reasonable expectation of success.
Conclusion
No claims allowed.
Any inquiry concerning this communication or earlier communications from the examiner should be directed to SUSANNAH S ARMSTRONG whose telephone number is (571)272-0112. The examiner can normally be reached Mon-Fri 7:30-5 (Flex).
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If attempts to reach the examiner by telephone are unsuccessful, the examiner’s supervisor, Sue X Liu can be reached at (571)272-5539. The fax phone number for the organization where this application or proceeding is assigned is 571-273-8300.
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/SUSANNAH S ARMSTRONG/Examiner, Art Unit 1616
/SUE X LIU/Supervisory Patent Examiner, Art Unit 1616
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