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 16-26 are pending in the application. Claims 1-14, 16-23, 25 and 26 are rejected. Claim 24 is objected to.
Priority
This application is a 35 U.S.C. § 371 National Stage Filing of International Application No. PCT/IB2021/053046, filed on April 13, 2021, which claims benefit of Provisional Application No. 63/013,576, filed on April 22, 2020, which claims benefit of Provisional Application No. 63/010,196, filed on April 15, 2020.
Information Disclosure Statement
The Information Disclosure Statement(s) (IDS) filed on April 24, 2026 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.
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 25 and 26 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 25 recites the “the invention” and is rejected as indefinite. There is insufficient antecedent basis for this limitation in the claim. It is suggested Applicant cancel the expression “of the invention” from claim 25 to overcome this issue of indefiniteness. Dependent claim 26 does not correct this issue of indefiniteness and is hence rejected.
Response to Arguments - 35 USC § 103
In reply, Applicant traverses the 35 U.S.C. § 103 rejection of claims 1-14 and 16-21 as presented in the Nonfinal Rejection mailed January 27, 2026. The newly applied 35 U.S.C. § 103 rejection of claims 1-14 and 16-23 has been necessitated by Applicant’s amendment filed on April 24, 2026. The previously presented rejection under 35 U.S.C. § 103 in the Office Action mailed January 27, 2026 has been withdrawn and replaced with the rejection(s) below. Applicant’s remarks, dated April 24, 2026, relevant to the newly applied 35 U.S.C. § 103 are addressed below.
Applicant asserts that the Office has not established a prima facie case of obviousness because the Nonfinal Rejection mailed January 27, 2026 “does not identify or explain what the ‘desired therapeutic effect’ is...or how the claimed compound amount relates to achieving that effect [and], [therefore,] the Office Action fails to establish that the claimed concentration parameter was recognized in the cited reference as result effective.” See pages 7-8 of Remarks dated April 24, 2026. As previously indicated and as discussed below in the newly applied rejection under 35 U.S.C. § 103, the prior art (i.e., WO 2020/254985 A1) teaches “[t]he amounts of the compound and salts of the present invention and the other pharmaceutically active agent(s) and the relative timings of administration will be selected in order to achieve the desired combined therapeutic effect”. See e.g., page 6. It appears Applicant is of the position that a person of ordinary skill in the art would not understand what is entailed by the expression “the desired...therapeutic effect” with respect to the prior art reference. This, however, seems unlikely as a person of ordinary skill in the art need only look at the title (i.e., “PYRIDO[2,3-D]PYRIMIDINE DERIVATIVES AS INHIBITORS OF HUMAN IMMUNODEFICIENCY VIRUS REPLICATION”) of the prior art reference to ascertain what is contextually implied by “the desired...therapeutic effect.” Therefore, Applicant’s arguments are not deemed persuasive by the Examiner and, consequently, instant claims 1-14 and 16-23 are rejected under 35 U.S.C. § 103 as being prima facie obvious over the prior art.
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 16-23 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, 20, 22 and 23 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 21-23, 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 combined 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 16-23, 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 16-23 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.
Allowable Subject Matter
Claims 24-26 are objected to as being dependent upon a rejected base claim, but would be allowable if 1) rewritten in independent form including all of the limitations of the base claim and any intervening claims; and 2) amended accordingly- when required- to address the issues described above.
Conclusion
Claims 1-14, 16-23, 25 and 26 are rejected. Claim 24 is objected to.
Applicant’s amendment necessitated the new ground(s) of rejection presented in this Office action. Accordingly, THIS ACTION IS MADE FINAL. See MPEP § 706.07(a). Applicant is reminded of the extension of time policy as set forth in 37 CFR 1.136(a).
A shortened statutory period for reply to this final action is set to expire THREE MONTHS from the mailing date of this action. In the event a first reply is filed within TWO MONTHS of the mailing date of this final action and the advisory action is not mailed until after the end of the THREE-MONTH shortened statutory period, then the shortened statutory period will expire on the date the advisory action is mailed, and any extension fee pursuant to 37 CFR 1.136(a) will be calculated from the mailing date of the advisory action. In no event, however, will the statutory period for reply expire later than SIX MONTHS from the mailing date of this final action.
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/D.M.S./Examiner, Art Unit 1626
/REBECCA L ANDERSON/Primary Examiner, Art Unit 1626
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