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
Claims 1-14 and 16-21 are pending in the application. Claims 1-14 and 16-21 are rejected.
Information Disclosure Statement
The Information Disclosure Statement(s) (IDS) filed on October 9, 2025 is in compliance with the provisions of 37 CFR 1.97 and 1.98. Accordingly, the Examiner has considered the IDS documents and signed copies of the 1449 forms are attached.
Response to Amendments
All objections and rejections made in the Office Action mailed July 9, 2025 have been overcome in view of Applicant’s amendments to the claims and the statement under 35 U.S.C. § 102(b)(2)(c) filed on October 9, 2025. Accordingly, all objections and rejections made in the Office Action mailed July 9, 2025 have been withdrawn.
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.
(1 of 2) Claims 1-14 and 16-21 are rejected under 35 U.S.C. § 103 as being unpatentable over PCT Publication No. WO 2020/254985 A1 (claims priority to Provisional Application No. 62/863,406 filed on June 19, 2019) in view of Gullapalli et al. (Intl. J. Pharmaceutics, 2015, 496:219-239).
The applied reference has a common assignee with the instant application. Based upon the earlier effectively filed date of the reference, it constitutes prior art under 35 U.S.C. 102(a)(2).
This rejection under 35 U.S.C. 103 might be overcome by: (1) a showing under 37 CFR 1.130(a) that the subject matter disclosed in the reference was obtained directly or indirectly from the inventor or a joint inventor of this application and is thus not prior art in accordance with 35 U.S.C.102(b)(2)(A); (2) a showing under 37 CFR 1.130(b) of a prior public disclosure under 35 U.S.C. 102(b)(2)(B); or (3) a statement pursuant to 35 U.S.C. 102(b)(2)(C) establishing that, not later than the effective filing date of the claimed invention, the subject matter disclosed and the claimed invention were either owned by the same person or subject to an obligation of assignment to the same person or subject to a joint research agreement. See generally MPEP § 717.02.
Determining the scope and contents of the prior art (See MPEP § 2141.01)
Regarding instant claims 1, 3-6, 8, 9, 11, 19 and 20, the prior art teaches the compound below and pharmaceutical compositions thereof (see e.g., pages 3 and 4; see also page 3 of 62/863,406 specification):
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The above prior art compound corresponds to the instantly claimed compound of Formula Id. The prior art further teaches that “the pharmaceutical compositions of this invention further comprise a pharmaceutically acceptable carrier, excipient, and/or diluent.” See e.g., page 5. The prior art also teaches a drug formulation comprising “90% PEG 400, [and] 10% ethanol for IV administration.” See e.g., page 41, line 4. The prior art also teaches a drug formulation comprising “1% Kolliphor P188” (i.e., poloxamer 188), “1% PEG3350” and “94.5% Water” for “subcutaneous injection.” See e.g., page 43, line 24. In addition, the prior art teaches the disclosed invention in the form of a solution and suspension. See e.g., page 41, line 4.
Ascertainment of the differences between the prior art and the claims (See MPEP § 2141.02)
Regarding instant claims 1, 16-19 and 21, the prior art does not teach the instantly claimed concentration based on free weight values with respect to the disclosed prior art compound. However, with respect to combination treatments, the prior art teaches that the amount of a disclosed prior art compound is selected in order to achieve the desired therapeutic effect. See e.g., page 6.
Regarding instant claims 2, 7, 10, 12-14, 20 and 21, the prior art does not teach the instantly recited excipients (e.g., sodium hydroxide, PEG 300, poloxamer 338 and acetate buffer) and/or claimed excipient amounts. However, the prior art does teach that “the pharmaceutical compositions of this invention further comprise a pharmaceutically excipient” which encompasses, for instance, the following instantly claimed excipients: sodium hydroxide, PEG 300, poloxamer 338 and acetate buffer. See e.g., page 5. In addition, Gullapalli et al. teach “[l]ower molecular weight PEGs (PEG 300 and PEG 400) are widely used as cosolvents in parenteral formulation to increase the aqueous solubility of poorly water soluble compounds.” See e.g., page 227.
Finding of prima facie obviousness --- rationale and motivation (See MPEP § 2142-2143)
Regarding instant claims 1, 2, 7, 10, 12-14 and 16-21, it would have been obvious to a person of ordinary skill in the art to include various pharmaceutically acceptable excipients and to determine the appropriate concentration of active ingredient and excipient(s) in a pharmaceutical composition comprising the aforementioned prior art compound. It would also have been obvious to a person of ordinary skill in the art to substitute PEG 400 of the prior art formulation with PEG 300 and reasonably expect the resulting formulation to maintain utility. Considering that both PEG 300 and PEG 400 are taught by Gullapalli et al. to be low molecular weight polymers commonly used to improve solubility in various pharmaceutical formulations, a person of ordinary skill would find it obvious to substitute the PEG 400 taught in the prior art formulation with the instantly claimed PEG 300. In addition, considering the lower MW of PEG 300 compared to PEG 400, a person of ordinary skill would be motivated to choose PEG 300 over PEG 400 in applications that require less viscous solutions, such as IV solutions. Similarly, it would also have been within the ability of a skilled artisan to substitute the poloxamer 188 excipient taught in the prior art with poloxamer 338 depending on the specific formulation and goal (e.g., solubilization or stabilization). “It is a settled principle of law that a mere carrying forward of an original patented conception involving only change of form, proportions, or degree, or the substitution of equivalents doing the same thing as the original invention, by substantially the same means, is not such an invention as will sustain a patent, even though the changes of the kind may produce better results than prior inventions.” In re Williams, 36 F.2d 436, 438 (CCPA 1929). The optimization of result-effective variables, i.e., variables that achieve a recognized result, such as weight percentages and concentrations are considered to be within the ability of the skilled artisan. “[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). At least in the interest of obtaining a more therapeutically effective pharmaceutical composition comprising the aforementioned prior art compound, a person of ordinary skill would have been motivated to experiment with various excipients and composition component weight percentages and concentrations as part of a routine optimization process.
(2 of 2) Claims 1-14 and 16-21 are rejected under 35 U.S.C. § 103 as being unpatentable over (PCT Publication No. WO 2020/084492 A1; claims priority to Provisional Application No. 62/749,818 filed on October 24, 2018) in view of PCT Publication No. WO 2020/254985 A1 (claims priority to Provisional Application No. 62/863,406 filed on June 19, 2019) and Gullapalli et al. (Intl. J. Pharmaceutics, 2015, 496:219-239).
The applied reference has a common assignee with the instant application. Based upon the earlier effectively filed date of the reference, it constitutes prior art under 35 U.S.C. 102(a)(2).
This rejection under 35 U.S.C. 103 might be overcome by: (1) a showing under 37 CFR 1.130(a) that the subject matter disclosed in the reference was obtained directly or indirectly from the inventor or a joint inventor of this application and is thus not prior art in accordance with 35 U.S.C.102(b)(2)(A); (2) a showing under 37 CFR 1.130(b) of a prior public disclosure under 35 U.S.C. 102(b)(2)(B); or (3) a statement pursuant to 35 U.S.C. 102(b)(2)(C) establishing that, not later than the effective filing date of the claimed invention, the subject matter disclosed and the claimed invention were either owned by the same person or subject to an obligation of assignment to the same person or subject to a joint research agreement. See generally MPEP § 717.02.
Determining the scope and contents of the prior art (See MPEP § 2141.01)
The prior art teaches the following chemical structure on e.g., page 11 (see also page 101 of 62/749,818 specification):
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The above prior art compound corresponds to the instantly claimed compound of Formula Ib. The prior art further teaches compositions comprising the disclosed prior art compound. See e.g., page 4. The prior art further teaches compositions “comprising a pharmaceutically acceptable carrier, excipient, and/or diluent.” See e.g., page 273.
Ascertainment of the differences between the prior art and the claims (See MPEP § 2141.02)
The prior art does not teach the instantly claimed concentration based on free weight values with respect to the disclosed prior art compound and excipients. The prior art also prior art does not provide specific examples of pharmaceutically acceptable carriers, excipients, and/or diluents. In addition, although the prior art teaches “formulations suitable for injection” (see e.g., page 26, line 18), the prior art does not specifically state the formulation is either a solution or suspension.
However, WO 2020/254985 A1 (‘985) teaches a pharmaceutical composition comprising a pharmaceutically acceptable carrier, excipient, and/or diluent.” See e.g., page 5. ‘985 also teaches a drug formulation comprising “90% PEG 400, [and] 10% ethanol for IV administration.” See e.g., page 41, line 4. ‘985 also teaches a drug formulation comprising “1% Kolliphor P188” (i.e., poloxamer 188), “1% PEG3350” and “94.5% Water” for “subcutaneous injection.” See e.g., page 43, line 24. In addition, ‘985 teaches the disclosed invention in the form of a solution and suspension. See e.g., page 41, line 4. In addition, Gullapalli et al. teach “[l]ower molecular weight PEGs (PEG 300 and PEG 400) are widely used as cosolvents in parenteral formulation to increase the aqueous solubility of poorly water soluble compounds.” See e.g., page 227.
Finding of prima facie obviousness --- rationale and motivation (See MPEP § 2142-2143)
It would, therefore, have been obvious to a person of ordinary skill in the art to arrive at the instantly claimed pharmaceutical composition based on the overall teachings of the prior art. It would also have been within the ability of a skilled artisan to experiment with and include various pharmaceutically acceptable excipients in the prior art composition. This is especially true in view of ‘985 which teach excipients similar in nature to the instantly required excipients. For example, considering that both PEG 300 and PEG 400 are taught by Gullapalli et al. to be low molecular weight polymers commonly used to improve solubility in various pharmaceutical formulations, a person of ordinary skill would find it obvious to substitute the PEG 400 taught in the prior art formulation with the instantly claimed PEG 300. In addition, considering the lower MW of PEG 300 compared to PEG 400, a person of ordinary skill would be motivated to choose PEG 300 over PEG 400 in applications that require less viscous solutions, such as IV solutions. Similarly, it would also have been within the ability of a skilled artisan to substitute the poloxamer 188 excipient taught in the prior art with poloxamer 338 depending on the specific formulation (solution, suspension, tablet, etc.) and goal (e.g., solubilization or stabilization). Furthermore, a skilled artisan would also be expected to determine the appropriate concentration of active ingredient and excipient(s) in a pharmaceutical composition as part of a routine optimization process. “It is a settled principle of law that a mere carrying forward of an original patented conception involving only change of form, proportions, or degree, or the substitution of equivalents doing the same thing as the original invention, by substantially the same means, is not such an invention as will sustain a patent, even though the changes of the kind may produce better results than prior inventions.” In re Williams, 36 F.2d 436, 438 (CCPA 1929). The optimization of result-effective variables, i.e., variables that achieve a recognized result, such as weight percentages and concentrations are considered to be within the ability of the skilled artisan. “[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). At least in the interest of obtaining a more therapeutically effective pharmaceutical composition comprising the aforementioned prior art compound, a person of ordinary skill would have been motivated to experiment with various excipients and composition component weight percentages and concentrations as part of a routine optimization process.
Conclusion
No claims are allowed.
Any inquiry concerning this communication or earlier communications from the examiner should be directed to DAVID M SHIM whose telephone number is 571-270-1205. The examiner can normally be reached Monday - Friday, 8 am - 4 pm EST. The examiner can also be reached via email (david.shim@uspto.gov) once an Authorization for Internet Communications form PTO/SB/439 has been filed by Applicant. See MPEP § 502.03 for details.
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/D.M.S./Examiner, Art Unit 1626
/REBECCA L ANDERSON/Primary Examiner, Art Unit 1626