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 . Claims included in the prosecution are claims 1-7.
Claim Rejections - 35 USC § 103
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.
Claims 1-7 are rejected under 35 U.S.C. 103 as being unpatentable over Chen et al. (US 20190210997, Jul. 11, 2019) (hereinafter Chen) in view of Nakashima et al. (US 2022/0409548, Filing Date Mar 3, 2020) (hereinafter Nakashima).
Chen discloses an alkynyl-substituted heterocyclic compound or a pharmaceutically acceptable salt thereof acting as an FGFR inhibitor (abstract). The compound may be
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(page 8, line 21). A pharmaceutical composition may comprise the compound with a pharmaceutically acceptable carrier (¶ [0048]). The pharmaceutical composition may be administered orally (¶ [0052]).
Chen differs from the instant claims insofar as not disclosing an amorphous solid dispersion comprising the compound and hydroxypropylmethylcellulose acetate succinate.
However, Nakashima discloses an amorphous solid dispersion of a pyrazole-amide compound (title). Specifically, a solid dispersion containing a compound of the formula [I] or a pharmaceutically acceptable salt thereof, and a specific pharmaceutically acceptable polymer (¶ [0001]). It has been found that an amorphous solid dispersion of a compound of the formula [I] or a pharmaceutically acceptable salt thereof with improved pharmacokinetics can be obtained by using a specific pharmaceutically acceptable polymer (¶ [0007] and [0006]). Suitable pharmaceutically acceptable polymers include hydropropylmethylcellulose acetate succinate (¶ [0010]). A method of manufacturing the amorphous solid dispersion comprises mixing the compound of the formula [I] or a pharmaceutically acceptable salt thereof with hydroxpropylmethylcellulose acetate succinate in a solvent, granulating the mixture to obtain a granule, and drying the granule (¶ [0029]-[0033]). Suitable solvents include ethanol (i.e., organic solvent) (¶ [0124]). The method may comprise spray-drying or hot melt extrusion (¶ [0122]). A pharmaceutical composition may comprise the amorphous solid dispersion with a pharmaceutically acceptable carrier (¶ [0019]). The pharmaceutical composition can be in various dosage forms such as a tablet or capsule (¶ [0106]). The content of a compound of the formula [I] in the pharmaceutical composition varies depending on the dosage form and administration route (¶ [0130]). When a conventional tablet containing a crystal of a compound of the formula [I] or a pharmaceutically acceptable salt thereof is used, the oral absorbability of the compound of the formula [I] is influenced by the diet, and when administered under fasting conditions, the exposure may be reduced as compared with the administration after a meal. In contrast, an amorphous solid dispersion of the compound of the formula [I] according to the present invention shows high solubility in some embodiments regardless of the presence or absence of bile acid at the time of administration. Thus, it is less susceptible to the influence of the diet and shows high oral absorbability even when administered under fasting conditions (¶ [0066]).
Accordingly, it would have been prima facie obvious to one of ordinary skill in the art to have incorporated the compound of Chen as an amorphous compound into the solid dispersion and pharmaceutical composition of Nakashima motivated by the desire to improve the pharmacokinetics of the compound as taught by Nakashima. One of ordinary skill in the art would have had a reasonable expectation of success since Nakashima teaches a pyrazole-amide compound and the compound of Chen is a pyrazole-amide compound.
In regards to the amount of compound I claimed, Chen discloses wherein the compound is an FGFR inhibitor and Nakashima discloses wherein the content of the compound varies depending on the dosage form and administration route. Therefore, it would have taken no more than the relative skills of one of ordinary skill in the art through routine experimentation to have arrived at the claimed amount of compound I depending the level of therapeutic effect, the dosage form, and the administration route desired.
In regards to the amount of hydroxypropylmethylcellulose acetate succinate claimed, Nakasima discloses wherein the polymer helps improves pharmacokinetics. Therefore, it would have taken no more than the relative skills of one of ordinary skill in the art through routine experimentation to have arrived at the claimed amount of hydroxypropylmethylcellulose acetate succinate claimed based on the level of improvement desired. Where 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. See MPEP 2144.05(II)(A).
Conclusion
Claims 1-7 are rejected.
No claims are allowed.
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/TRACY LIU/Primary Examiner, Art Unit 1614
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