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
Information Disclosure Statement
The information disclosure statements received 03/30/2026 have been considered.
Restriction/Species Election
Newly submitted claim 126 and amended claim 56 directed to invention that is independent or distinct from the invention originally claimed for the following reasons: Amended claim 56 now requires an additional component (one or more pharmaceutically acceptable excipients) and claim 126 specifies that said additional component is a paraben or parabens.
Since applicant has received an action on the merits for the originally presented invention, this invention has been constructively elected by original presentation for prosecution on the merits. Accordingly, claims 56 and 126 have withdrawn from consideration as being directed to a non-elected invention. See 37 CFR 1.142(b) and MPEP § 821.03.
To preserve a right to petition, the reply to this action must distinctly and specifically point out supposed errors in the restriction requirement. Otherwise, the election shall be treated as a final election without traverse. Traversal must be timely. Failure to timely traverse the requirement will result in the loss of right to petition under 37 CFR 1.144. If claims are subsequently added, applicant must indicate which of the subsequently added claims are readable upon the elected invention.
Should applicant traverse on the ground that the inventions are not patentably distinct, applicant should submit evidence or identify such evidence now of record showing the inventions to be obvious variants or clearly admit on the record that this is the case. In either instance, if the examiner finds one of the inventions unpatentable over the prior art, the evidence or admission may be used in a rejection under 35 U.S.C. 103 or pre-AIA 35 U.S.C. 103(a) of the other invention.
Withdrawn Rejection
In view of the arguments made, the 112(b) rejection of the prior office action has been withdrawn.
In view of the amendments made, the 112(b) antecedent basis rejection and the 102 rejection have been withdrawn.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.
KSR Rationales
The MPEP in section 2143, subsection I gives examples of Rationales for supporting a conclusion of obvious. These rationales are non-exhaustive and include (A) Combining prior art elements according to known methods to yield predictable results; (B) Simple substitution of one known element for another to obtain predictable results; (C) Use of known technique to improve similar devices (methods, or products) in the same way; (D) Applying a known technique to a known device (method, or product) ready for improvement to yield predictable results; (E) “Obvious to try” – choosing from a finite number of identified, predictable solutions, with a reasonable expectation of success; (F) Known work in one field of endeavor may prompt variations of it for use in either the same field or a different one based on design incentives or other market forces if the variations are predictable to one of ordinary skill in the art; (G) Some teaching, suggestion, or motivation in the prior art that would have led one of ordinary skill to modify the prior art reference or to combine prior art reference teachings to arrive at the claimed invention.
Claim(s) 1, 4, 7, 12, 18, 23, 24, 30, 37, 45, 50, 79, 124-125, and 127 is/are rejected under 35 U.S.C. 103 as being unpatentable over American Regent (Caffeine and Sodium Benzoate Injection, USP, American Regent Inc, revised 12/2019, herein after AmRegen) in view of Tsuji (US2004/0034042) and Chaudhari (IJAPBC., Vol. 1, 2012) and as supported by Shen (International Journal of Pharmaceutics, 647, 2023, 123520).
Claims 1, 4, and 56, are drawn to compositions comprising caffeine, sodium benzoate, and lactic acid.
Dependent claim 7 specifies lactic acid.
Dependent claims 12, 18, and 23 specify molar ratios between caffeine and sodium benzoate in a range of about 1:1.0 to about 1:1.5 (claim 12), caffeine and lactic acid of about 1:0.1 to about 1:0.3 (claim 18), and sodium benzoate and lactic acid (claim 23) in a range of about 1:0.15 to about 1:0.18.
Dependent claim 24 specifies a composition of claim 2 wherein the pH of the composition is from about 5 to about 6.
Dependent claims 30 specifies that the solubility of the caffeine is 240 mg/mL or greater.
Dependent claim 37 claims a composition comprising about 15% to about 25% caffeine, about 15% to about 25% sodium benzoate, about 1% to about 3% of lactic acid, and about 50% to about 70% water.”
Dependent claim 45 specifies that the composition is an aqueous solution, has specific molar ratios of caffeine to sodium benzoate, sodium benzoate to lactic acid, and wherein the caffeine has a solubility of 250mg/mL.
Claim 50 claims a physical property of the composition which is that the composition is heat stable when subject to a temperature of 135oC for 45 minutes.
Dependent claim 79 claims a composition wherein the composition is configured for intramuscular or subcutaneous routes.
Claim 124 specifies a composition excluding alcohol.
Claim 125 specifies that the weight percentage of sodium benzoate is greater than caffeine.
Claim 127 specifies that the solubility of caffeine is 235 mg/mL or greater at a temperature of from 20 oC to 22 oC.
Regarding claims 1, 4, 12, 24, 45, 79, and 124 AmRegen is drawn to the pharmaceutical combination of caffeine and sodium benzoate. AmRegen in sec. Description states “Caffeine and sodium Benzoate Injection, USP is a clear sterile, nonpyrogenic, solution of Caffeine Alkaloid. Each contains: Caffeine (anhydrous) 125 mg; Sodium Benzoate (added to increase the solubility of caffeine) 125 mg; Water for injection, USP q.s. pH (range 6.5 to 8.5) adjusted with hydrochloric acid and/or sodium hydroxide. For intramuscular or slow intravenous administration only.”
In regards to claims 30, 45, and 127, which have the limitations “wherein the solubility of the caffeine is 240 mg/mL or greater” (claim 24), “250 mg/mL or greater” (claim 45), and “235 mg/mL”, AmRegen teaches that the solubility of caffeine can be increased by the addition of sodium benzoate. AmRegen in sec. Dosage and Administration states “the manufacturer of caffeine and sodium benzoate injection recommends intramuscular, or in emergency failure, intravenous injection of 500 mg of the drug (about 250 mg of anhydrous caffeine) or a maximum single dose of 1 gram (about 500 mg of anhydrous caffeine)…”. AmRegen continues “the usual dose is 0.5 g (7 ½ grains) as frequently as directed by the physician. The maximum safe dose is 0.5 g and the total dose in 24 hours should rarely exceed 2.5 g.” AmRegen also teaches the packaging of the its sodium caffeine benzoate drug is in a 2 mL single dose vial.
Taking the teachings of AmRegen above, one of ordinary skill in the art could modify the commercial dose of sodium caffeine benzoate to include 500 mg caffeine per 2 mL dose. This comes out to be 250 mg/mL for a max safe dose. See Shen below for more discussion.
AmRegen does not explicitly discuss lactic acid. This is addressed by the combination of Tsuji and/or Chaudhari.
Regarding claims 1, 4, 7, 37, 45, and 56, Tsuji in para. [0010]-[0015] teaches a composition comprising a compound represented by formula I, a buffer, and at least one other compound selected from sorbic acid or ethylenediaminetetraacetic acid.
Tsuji compound I
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252
340
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Tsuji in para. [0023] specifically mentions “sodium caffeine benzoate” as a compound represented by formula I above.
Tsuji in para. [0186], Tsuji contemplates the addition of “pH adjusters”. Tsuji in para. [0194] defines “pH adjusters” to include organic acids including lactic acid.
Additionally, Tsuji in para. [0200] contemplates pH of its composition ranging between 3-9. Tsuji states that a preferred embodiment has a pH of 5.5 to 8.5.
Alternatively, Chaudhari on p. 21-22, sec. Excipient based on their origin teaches lactic acid as a common synthetic excipient.
Regarding claims 18, 23, 37, 45, and 125, which are drawn to limitations specifying specific ratios or weight percentages (see claim listing above), the adjustment of these ratios and/or weight percentages would be within the skillset of one of ordinary skill in the art. The MPEP section 2144.05, subsection II states:
The adjustment of particular conventional working conditions (e.g., determining result effective amounts of the ingredients beneficially taught by the cited references), is deemed merely a matter of judicious selection and routine optimization which is well within the purview of the skilled artisan. Generally, differences in concentration or temperature will not support the patentability of subject matter encompassed by the prior art unless there is evidence indicating such concentration or temperature is critical.
“[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). Accordingly, this type of modification would have been well within the purview of the skilled artisan and no more than an effort to optimize results.
Therefore, one of ordinary skill would find the adjustment of particular ratios and weight percentages obvious.
Regarding claims 50 and 127, which are drawn to a physical property of the composition, the property is tied to the composition comprising the caffeine, sodium benzoate, and lactic acid. Therefore, if the composition is obvious in view of the art, than the property itself is also obvious in view of the art.
Regarding claim 127 and, specifically, the solubility of caffeine in solution, it is known within the art that the solubility of caffeine in water is 2.17 g/100 mL (21.7 mg/mL) at 25o C, 18.0 g/100 mL at 80o C, and 67 g/100 mL at 100o C. AmRegen further teaches that the addition of sodium benzoate to caffeine increases the solubility of caffeine significantly such that 125 mg of caffeine in a 2 mL vial (62.5 mg/mL) does not solidify. This at least indicates that the concentrations of caffeine taught by AmRegen are not limited by the solubility of caffeine within sodium benzoate but rather what is and what is not considered a safe dose.
Further, a 2023 study by Shen teaches the extent of the solubility enhancement of caffeine by sodium benzoate. Shen on p. 8, sec. Conclusion states “The solubility of caffeine at room temperature can be enhanced more than 20 folds by the addition of sodium benzoate as a hydrotrope.” A 20 fold increase in solubility at room temperature amounts to a solubility of 434 mg/mL of caffeine. While this study came out in 2023, the solubility enhancement effect on caffeine via sodium benzoate was known at the time of the effective filing date. The potential to create compositions wherein caffeine is solubilized at concentrations at or above 235 mg/mL was present within the art at the time of the effective filing date and the solubility limitations would be obvious to one of ordinary skill. Additionally, the MPEP section 2112, subsection II and III states:
II.
“There is no requirement that a person of ordinary skill in the art would have recognized the inherent disclosure at the relevant time, but only that the subject matter is in fact inherent in the prior art reference. Schering Corp. v. Geneva Pharm. Inc., 339 F.3d 1373, 1377, 67 USPQ2d 1664, 1668 (Fed. Cir. 2003)”
III.
“Where applicant claims a composition in terms of a function, property or characteristic and the composition of the prior art is the same as that of the claim but the function is not explicitly disclosed by the reference, the examiner may make a rejection under both 35 U.S.C. 102 and 103.”
Regarding the limitation “wherein the pharmaceutical composition is in the form of a solution and is configured for parenteral administration”, the specification is not explicit as to how a solution “configured for parenteral administration” is distinct from a simple solution. Where a beverage or solution intended for oral administration is distinct from a solution intended for parental administration, the specification and the claims do not sufficiently exclude the solutions of AmRegen and Tsuji. Essentially, the limitation “configured for parenteral administration” is an intended use and does not impart patentable weight to the claim.
AmRegen teaches a composition comprising caffeine and sodium benzoate. Tsuji teaches a composition comprising sodium caffeine benzoate, such as the composition of AmRegen, and further contemplates the addition of a pH adjuster including lactic acid. Chaudhari teaches that lactic acid is a common synthetic excipient which one of ordinary skill could predictably use in combination with the composition of AmRegen. Shen affirms that the solubility of caffeine is enhanced by sodium benzoate, a fact well-known at the time of the effective filing date. Shen further indicates that this solubility can be significantly enhanced upwards 20 times from the standard solubility of 21.7 mg/mL at room temperature.
Therefore, it would have been prima facie obvious at the time of the effective filing date for one of ordinary skill in the art to have combined lactic acid with sodium caffeine benzoate to arrive at the instant claims with a reasonable assumption of success. One of ordinary skill would find motivation to make the combination as Tsuji not only contemplates the combination, but also teaches that the combination can lead to a composition with enhanced preservative effects.
Double Patenting
The nonstatutory double patenting rejection is based on a judicially created doctrine grounded in public policy (a policy reflected in the statute) so as to prevent the unjustified or improper timewise extension of the “right to exclude” granted by a patent and to prevent possible harassment by multiple assignees. A nonstatutory double patenting rejection is appropriate where the conflicting claims are not identical, but at least one examined application claim is not patentably distinct from the reference claim(s) because the examined application claim is either anticipated by, or would have been obvious over, the reference claim(s). See, e.g., In re Berg, 140 F.3d 1428, 46 USPQ2d 1226 (Fed. Cir. 1998); In re Goodman, 11 F.3d 1046, 29 USPQ2d 2010 (Fed. Cir. 1993); In re Longi, 759 F.2d 887, 225 USPQ 645 (Fed. Cir. 1985); In re Van Ornum, 686 F.2d 937, 214 USPQ 761 (CCPA 1982); In re Vogel, 422 F.2d 438, 164 USPQ 619 (CCPA 1970); In re Thorington, 418 F.2d 528, 163 USPQ 644 (CCPA 1969).
A timely filed terminal disclaimer in compliance with 37 CFR 1.321(c) or 1.321(d) may be used to overcome an actual or provisional rejection based on nonstatutory double patenting provided the reference application or patent either is shown to be commonly owned with the examined application, or claims an invention made as a result of activities undertaken within the scope of a joint research agreement. See MPEP § 717.02 for applications subject to examination under the first inventor to file provisions of the AIA as explained in MPEP § 2159. See MPEP § 2146 et seq. for applications not subject to examination under the first inventor to file provisions of the AIA . A terminal disclaimer must be signed in compliance with 37 CFR 1.321(b).
The filing of a terminal disclaimer by itself is not a complete reply to a nonstatutory double patenting (NSDP) rejection. A complete reply requires that the terminal disclaimer be accompanied by a reply requesting reconsideration of the prior Office action. Even where the NSDP rejection is provisional the reply must be complete. See MPEP § 804, subsection I.B.1. For a reply to a non-final Office action, see 37 CFR 1.111(a). For a reply to final Office action, see 37 CFR 1.113(c). A request for reconsideration while not provided for in 37 CFR 1.113(c) may be filed after final for consideration. See MPEP §§ 706.07(e) and 714.13.
The USPTO Internet website contains terminal disclaimer forms which may be used. Please visit www.uspto.gov/patent/patents-forms. The actual filing date of the application in which the form is filed determines what form (e.g., PTO/SB/25, PTO/SB/26, PTO/AIA /25, or PTO/AIA /26) should be used. A web-based eTerminal Disclaimer may be filled out completely online using web-screens. An eTerminal Disclaimer that meets all requirements is auto-processed and approved immediately upon submission. For more information about eTerminal Disclaimers, refer to www.uspto.gov/patents/apply/applying-online/eterminal-disclaimer.
Co-pending application 17/784,375
Claims 1, 4, 7, 12, 18, 23, 24, 30, 37, 45, 50, 79, 124-125, and 127 are provisionally rejected on the ground of nonstatutory double patenting as being unpatentable over claims 1-4, 8, 10, 31, 33, 43-45, 64, 67, 70, and 71 of copending Application No. 17/784,375 in view of American Regent (Caffeine and Sodium Benzoate Injection, USP, American Regent Inc, revised 12/2019, herein after AmRegen) in view of Tsuji (US2004/0034042) and Chaudhari (IJAPBC., Vol. 1, 2012) and as supported by Shen (International Journal of Pharmaceutics, 647, 2023, 123520).
Reference claim 1 is drawn to a composition comprising caffeine citrate and one or more co-solvents. Reference claims 10, 67, and 71 further include lactic acid. Tsuji in para. [0023] lists caffeine citrate as an alternative to sodium-caffeine benzoate. One of ordinary skill would find it obvious to replace the caffeine citrate of the reference claims with sodium caffeine benzoate to arrive at the instant claims with a reasonable assumption of success.
This is a provisional nonstatutory double patenting rejection.
Response to Arguments
Applicant argues that the office action of 03/30/2026 uses impressible hindsight to arrive at the instant claims. Applicant states “It not is appropriate in the obviousness analysis to use the pending claims as a blueprint and, after finding deficiencies in a reference, attempt to approximate the claims in hindsight…”.
The applicant has acknowledged the teachings of Tsuji. Specifically that Tsuji teaches a composition comprising a xanthine, a buffer, and at least one member selected from sorbic acid, EDTA, and salts thereof. Applicant states that “Tsuji does not disclose lactic acid as a preservative. The rationale for the proposed combination of Tsuji with American Regent is therefore incorrect. More specifically, Applicant does not agree with the Office Action’s conclusion…that ‘Tsuji…teaches that the combination [of lactic acid with sodium caffeine benzoate] can lead to a composition with enhanced preservative effects’”.
Applicant, regarding Chaudhari, argues that Chaudhari “does not lead one skilled in the art to include lactic acid in the American Regent injection” and that “The Chaudhari disclosure does not suggest the use of lactic acid in all pharmaceutical compositions, and particularly does not suggest incorporating lactic acid into the American Regent injection. Instead, it notes that excipient selection can depend on a number of factors including dosage form, potential detrimental interactions, and route of administration”.
Regarding Shen, Applicant argues that “[Shen] does not combine with the references discussed above to support the rejection.” Applicant states “the Shen paper indicates on the bottom of its first page that it became ‘available online’ on October 17, 2023, after the effective filing date of the pending claims. As a result, Shen is not prior art to this application. Applicant acknowledges the inherency argument made and states “the pending claims are not simply the same composition as the prior art but with a newly discovered property.”
The MPEP section 2112 includes sections I and II, titled “Something which is old does not become patentable upon the discovery a new property” and “Inherent features need not be recognized at the relevant time” (see 103 rejection above for the underlying text of these sections).
Therefore, applicant’s assertion that Shen is not considered prior art does not disqualify Shen’s teachings which show that the combination of sodium benzoate and caffeine leads to enhanced solubility of caffeine. Whether the art recognized this property at the time of the effective filing date or not is irrelevant.
Regarding Tsuji, the prior and current office action state “One of ordinary skill would find motivation to make the combination as Tsuji not only contemplates the combination, but also teaches that the combination can lead to a composition with enhanced preservative effects.” AmRegen teaches caffeine sodium benzoate. Tsuji adds to this combination a number of other components but also contemplates the addition of lactic acid as a pH adjuster. The prior office action acknowledged lactic acid as a pH adjuster, which applicant also acknowledges, (p. 10, para. 4).
Additionally, Chaudhari is relied upon as a general teaching to indicate that lactic acid is a well known excipient within the art. Essentially, a known limitation which can be added to give a predictable result (KSR A).
Tsuji can be viewed as an extension of this principle (KSR A) in that Tsuji shares the combination of caffeine and sodium benzoate (caffeine sodium benzoate) with AmRegen. Tsuji contemplates the addition of lactic acid which makes obvious the instant claims.
New 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) 4 is/are rejected under 35 U.S.C. 102(a)(1) a as anticipated by or, in the alternative, under 35 U.S.C. 103 as obvious over Tsuji (US2004/0034042) and as supported by Shen (International Journal of Pharmaceutics, 647, 2023, 123520).
Tsuji in para. [0253], Example 8 discloses a composition comprising caffeine-sodium benzoate and purified water.
Claim 4 states “means for increasing the solubility of caffeine in aqueous solution…”. The instant specification in para. [0025] states “An exemplary means for increasing the solubility of caffeine in the aqueous solution of caffeine and sodium benzoate is lactic acid. Additional exemplary means for increasing the solubility of caffeine in the aqueous solution of caffeine and sodium benzoate are acetic acid, aspartic acid and glutamic acid.”
Note that the specification is non-limiting in regards to the definition of “means for increasing the solubility of caffeine in the aqueous solution”. Therefore, the broadest reasonable interpretation includes sodium benzoate which Shen teaches increases the solubility of caffeine in aqueous solution (see discussion in the 103 rejection above).
This new rejection has been necessitated by amendments made to the claims and clarifying arguments made in the remarks submitted 03/30/2026.
Conclusion
No claims allowed.
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 nonprovisional extension fee (37 CFR 1.17(a)) 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.
Any inquiry concerning this communication or earlier communications from the examiner should be directed to LUISALBERTO GONZALEZ whose telephone number is (571)272-1154. The examiner can normally be reached M-F 8:30-5:30.
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If attempts to reach the examiner by telephone are unsuccessful, the examiner’s supervisor, Jeffrey Murray can be reached at (571) 272-9023. The fax phone number for the organization where this application or proceeding is assigned is 571-273-8300.
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/L.G./Examiner, Art Unit 1624
/JEFFREY H MURRAY/Supervisory Patent Examiner, Art Unit 1624
Prosecution Insights