Prosecution Insights
Last updated: April 19, 2026
Application No. 18/001,222

IMPROVED PROCESS FOR PREPARATION OF SITAGLIPTIN

Non-Final OA §112
Filed
Dec 08, 2022
Examiner
WILLIS, DOUGLAS M
Art Unit
1624
Tech Center
1600 — Biotechnology & Organic Chemistry
Assignee
Aarti Pharmalabs Limited
OA Round
1 (Non-Final)
83%
Grant Probability
Favorable
1-2
OA Rounds
2y 1m
To Grant
99%
With Interview

Examiner Intelligence

Grants 83% — above average
83%
Career Allow Rate
1472 granted / 1781 resolved
+22.7% vs TC avg
Strong +19% interview lift
Without
With
+19.4%
Interview Lift
resolved cases with interview
Fast prosecutor
2y 1m
Avg Prosecution
40 currently pending
Career history
1821
Total Applications
across all art units

Statute-Specific Performance

§101
0.9%
-39.1% vs TC avg
§103
7.8%
-32.2% vs TC avg
§102
16.7%
-23.3% vs TC avg
§112
50.5%
+10.5% vs TC avg
Black line = Tech Center average estimate • Based on career data from 1781 resolved cases

Office Action

§112
DETAILED ACTION Notice of Pre-AIA or AIA Status The inventor or joint inventor should note that the instant invention, filed on or after March 16, 2013, is being examined under the first inventor to file provisions of the AIA . Status of the Claims Claims 1-20 are pending in the instant invention. According to the Amendments to the Claims, filed July 17, 2025, claims 1-20 were presented for prosecution on the merits. Status of Priority This invention is a 35 U.S.C. § 371 National Stage Filing of International Application No. PCT/IN2021/050567, filed June 11, 2021, which claims priority under 35 U.S.C. § 119(a-d) to IN 202021024760, filed June 12, 2020. Restrictions / Election of Species PNG media_image1.png 200 400 media_image1.png Greyscale The inventor’s or joint inventor’s provisional election of the following, without traverse, in the reply filed on July 17, 2025, is acknowledged: Group I - claims 1-11 and 16-18. Affirmation of this election must be made by the inventor or joint inventor in replying to this Office action. Similarly, the inventor or joint inventor should further note that the requirement is still deemed proper and is therefore made FINAL. Moreover, the inventor or joint inventor should further note that claims 12-15, 19 and 20 were withdrawn from further consideration, pursuant to 37 CFR 1.142(b), as being drawn to a nonelected or cancelled invention, there being no allowable generic or linking claim. Thus, a first Office action and prosecution on the merits of claims 1-11 and 16-18 is contained within. Specification Objection - Disclosure The following guidelines illustrate the preferred layout for the specification of a utility application. These guidelines are suggested for the inventor’s or joint inventor’s use. Arrangement of the Specification As provided in 37 CFR 1.77(b), the specification of a utility invention should include the following sections in order. Each of the lettered items should appear in upper case, without underlining or bold type, as a section heading. If no text follows the section heading, the phrase Not Applicable should follow the section heading: (a) TITLE OF THE INVENTION. (b) CROSS-REFERENCE TO RELATED APPLICATIONS. (c) STATEMENT REGARDING FEDERALLY SPONSORED RESEARCH OR DEVELOPMENT. (d) THE NAMES OF THE PARTIES TO A JOINT RESEARCH AGREEMENT. (e) INCORPORATION-BY-REFERENCE OF MATERIAL SUBMITTED ON A COMPACT DISC. (f) BACKGROUND OF THE INVENTION. (1) Field of the Invention. (2) Description of Related Art (including information disclosed under 37 CFR 1.97 and 1.98). (g) BRIEF SUMMARY OF THE INVENTION. (h) BRIEF DESCRIPTION OF THE SEVERAL VIEWS OF THE DRAWING(S). (i) DETAILED DESCRIPTION OF THE INVENTION. (j) CLAIM OR CLAIMS (commencing on a separate sheet). (k) ABSTRACT OF THE DISCLOSURE (commencing on a separate sheet). (l) SEQUENCE LISTING (See MPEP § 2424 and 37 CFR 1.821-1.825). The inventor or joint inventor is advised to format the specification according to 37 CFR 1.77(b) above and 37 CFR 1.77(c). Revisions should particularly include and/or address: a) section headings (b-i), where applicable; and b) bold-type, underline, and/or upper case formatting. Appropriate correction may be required. Specification Objection - Abstract The inventor or joint inventor is reminded of the proper content of an abstract of the disclosure. With regard particularly to chemical patents, for compounds or compositions, the general nature of the compound or composition should be given as well as the use thereof, e.g., The compounds are of the class of alkyl benzene sulfonyl ureas, useful as oral anti-diabetics. Exemplification of a species could be illustrative of members of the class. For processes, the reactions, reagents and process conditions should be stated, generally illustrated by a single example, unless variations are necessary. See MPEP § 608.01(b), Section B. The abstract of the disclosure is objected to because it fails to exemplify any members or formulae illustrative of its class. Correction is required. See MPEP § 608.01(b). The examiner suggests incorporating the structure of Formula (I) into the abstract, to overcome this objection. Claim Objections Claim 1 is objected to because of the following informalities: for clarity and precision, the existing recitation should be replaced with the following recitation: A process for preparing Sitagliptin of Formula (I): PNG media_image2.png 200 400 media_image2.png Greyscale (I) wherein the process comprises the following step: reacting a compound of Formula (II): PNG media_image3.png 200 400 media_image3.png Greyscale (II) with a compound of Formula (III): PNG media_image4.png 200 400 media_image4.png Greyscale (III) wherein: R1 is alkyl, alkyl(aryl), or aryl; and R2 is alkyl, alkyl(aryl), or aryl; in the presence of the biocatalyst, pyridoxal-5-phosphate (PLP), and the transaminase enzyme, CDX-036. Appropriate correction is required. See MPEP § 2173.02. Claim 2 is objected to because of the following informalities: for clarity and precision, the existing recitation should be replaced with the following recitation: The process as claimed in claim 1, wherein the process further comprises: (a) adding a co-solvent selected from the group consisting of dimethyl formamide, dimethyl sulfoxide (DMSO), ethanol, isopropanol, isopropyl acetate, methanol, methyl tert-butyl ether (MTBE), and water; and (b) maintaining the temperature in the range of from 35°C to 60°C. Appropriate correction is required. See MPEP § 2173.02. Claim 3 is objected to because of the following informalities: for clarity and precision, the existing recitation should be replaced with the following recitation: The process as claimed in claim 1, wherein the process further comprises preparing a solution of the compound of Formula (II) in a co-solvent selected from the group consisting of acetone, chloroform, dichloromethane (DCM), dimethyl sulfoxide (DMSO), ethanol, ethyl acetate, isopropanol, and methanol. Appropriate correction is required. See MPEP § 2173.02. Claim 4 is objected to because of the following informalities: for clarity, precision and to avoid issues under 35 U.S.C. § 112(b) and/or 35 U.S.C. § 112(d), the existing recitation should be replaced with the following recitation: The process as claimed in claim 3, wherein the process further comprises: (a) preparing a mixture of the solution of the compound of Formula (II) and water in a buffer; and (b) adding the biocatalyst, pyridoxal-5-phosphate (PLP), at a pH in the range of from 8 to 9. Appropriate correction is required. See MPEP § 2173.02. Claim 5 is objected to because of the following informalities: for clarity and precision, the existing recitation should be replaced with the following recitation: The process as claimed in claim 1, wherein the process further comprises a compound of Formula (III) selected from the group consisting of alanine, 3-aminocyclohexa-1,5-dienecarboxylic acid, 1,4- diaminobutane, 1,2-diaminoethane, 1,5-diaminopentane, isopropylamine, 1-phenylethylamine, and ortho-xylenediamine. Appropriate correction is required. See MPEP § 2173.02. Claim 6 is objected to because of the following informalities: for clarity, precision and to avoid issues under 35 U.S.C. § 112(b) and/or 35 U.S.C. § 112(d), the existing recitation should be replaced with the following recitation: The process as claimed in claim 4, wherein the process further comprises the buffer, triethanolamine. Appropriate correction is required. See MPEP § 2173.02. Claim 7 is objected to because of the following informalities: for clarity and precision, the existing recitation should be replaced with the following recitation: The process as claimed in claim 1, wherein the process further comprises reacting the compound of Formula (II) with the compound of Formula (III) optionally in the presence of a surface tension reducing agent or a phase transfer catalyst. Appropriate correction is required. See MPEP § 2173.02. Claim 8 is objected to because of the following informalities: for clarity and precision, the existing recitation should be replaced with the following recitation: The process as claimed in claim 7, wherein the process further comprises adding the surface tension reducing agent or the phase transfer catalyst to a solution of the compound of Formula (III) prior to adding the biocatalyst, pyridoxal-5-phosphate (PLP). Appropriate correction is required. See MPEP § 2173.02. Claim 9 is objected to because of the following informalities: for clarity and precision, the existing recitation should be replaced with the following recitation: The process as claimed in claim 8, wherein the process further comprises a surface tension reducing agent selected from the group consisting of cetyltrimethylammonium bromide (CTAB), cetyltrimethylammonium chloride (CTAC), and didecyldimethylammonium chloride (DDAC). Appropriate correction is required. See MPEP § 2173.02. Claim 10 is objected to because of the following informalities: for clarity and precision, the existing recitation should be replaced with the following recitation: The process as claimed in claim 1, wherein the process further comprises reacting the compound of Formula (II) with the compound of Formula (III) at a temperature in the range of from 35°C to 60°C. Appropriate correction is required. See MPEP § 2173.02. Claim 11 is objected to because of the following informalities: for clarity and precision, the existing recitation should be replaced with the following recitation: The process as claimed in claim 1, wherein the process further comprises preparing Sitagliptin in a purity in the range of from 99.90% to 99.99%. Appropriate correction is required. See MPEP § 2173.02. Claim 16 is objected to because of the following informalities: for clarity, precision and to avoid issues under 35 U.S.C. § 112(b) and/or 35 U.S.C. § 112(d), the existing recitation should be replaced with the following recitation: The process as claimed in claim 4, wherein the process further comprises adding a surface tension reducing agent or a phase transfer catalyst to a solution of the compound of Formula (III) prior to adding the biocatalyst, pyridoxal-5-phosphate (PLP). Appropriate correction is required. See MPEP § 2173.02. Claim 17 is objected to because of the following informalities: for clarity, precision and to avoid issues under 35 U.S.C. § 112(a), 35 U.S.C. § 112(b) and/or 35 U.S.C. § 112(d), the existing recitation should be replaced with the following recitation: The process as claimed in claim 8, wherein the process further comprises a phase transfer catalyst selected from the group consisting of tetrabutylammonium bromide (TBAB), triethylbenzylammonium chloride (TEBA), tetrabutylammonium fluoride (TBAF), and tetrabutylammonium hydroxide (TBAH). Appropriate correction is required. See MPEP § 2173.02. Claim 18 is objected to because of the following informalities: for clarity and precision, the existing recitation should be replaced with the following recitation: The process as claimed in claim 4, wherein the process further comprises the buffer, triethanolamine. Appropriate correction is required. See MPEP § 2173.02. The examiner asserts that if claim 6 is amended as suggested above, then claim 6 and claim 18 would be independently objected to because the claims would be substantially duplicative. See 37 CFR 1.75 and MPEP § 706.03(k). Claim Rejections - 35 U.S.C. § 112(b) The following is a quotation of the second paragraph of 35 U.S.C. § 112: (b) CONCLUSION. The specification shall conclude with one or more claims particularly pointing out and distinctly claiming the subject matter which the inventor or joint inventor regards as the invention. Claims 4 and 16 are rejected under 35 U.S.C. § 112(b) as being indefinite for failing to set forth the subject matter which the inventor or joint inventor regards as the invention. The inventor or joint inventor should note that claim 4 recites the limitation, The process as claimed in claim 1, further comprises preparing a mixture of the amino compound of Formula (II) solution…, in lines 1-2 of the claim. There is insufficient antecedent basis, in claim 1, for this limitation, with respect to the process for preparing Sitagliptin of the Formula (I). According to claim 1, an amino compound of Formula (II) solution is not recited, with respect to the process for preparing Sitagliptin of the Formula (I). Moreover, the inventor or joint inventor should further note that [C]laims which depend from indefinite claims are also indefinite. {See Ex parte Cordova, 10 USPQ 2d 1949, 1952 (PTO Bd. App. 1989)}. The examiner suggests amending the claims, particularly as stated in the section above entitled Claim Objections, to overcome this rejection. Claim 6 is rejected under 35 U.S.C. § 112(b) as being indefinite for failing to set forth the subject matter which the inventor or joint inventor regards as the invention. The inventor or joint inventor should note that claim 6 recites the limitation, The process as claimed in claim 1, wherein the buffer is triethanolamine, in lines 1-2 of the claim. There is insufficient antecedent basis, in claim 1, for this limitation, with respect to the process for preparing Sitagliptin of the Formula (I). According to claim 1, a buffer is not recited, with respect to the process for preparing Sitagliptin of the Formula (I). The examiner suggests amending the claim, particularly as stated in the section above entitled Claim Objections, to overcome this rejection. Allowable Subject Matter No claims are allowed. Conclusion Any inquiry concerning this communication or earlier communications from the examiner should be directed to DOUGLAS M. WILLIS, whose telephone number is 571-270-5757. The examiner may normally be reached on Monday thru Thursday from 8:00-6:00 EST. The examiner is also available on alternate Fridays. If attempts to reach the examiner by telephone are unsuccessful, the examiner’s supervisor, Mr. Jeffrey Murray, may be reached on 571-272-9023. The fax phone number for the organization where this invention or proceeding is assigned is 571-273-8300. Information regarding the status of an invention may be obtained from Patent Center. For more information about Patent Center, see https://www.uspto.gov/patents/apply/patent-center. Should you have questions on access to Patent Center, contact the Patent Electronic Business Center (PEBC) at 866-217-9197 (toll-free) or ebc@uspto.gov. /DOUGLAS M WILLIS/ Primary Examiner, Art Unit 1624
Read full office action

Prosecution Timeline

Dec 08, 2022
Application Filed
Dec 08, 2022
Response after Non-Final Action
Sep 08, 2025
Non-Final Rejection — §112 (current)

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Prosecution Projections

1-2
Expected OA Rounds
83%
Grant Probability
99%
With Interview (+19.4%)
2y 1m
Median Time to Grant
Low
PTA Risk
Based on 1781 resolved cases by this examiner. Grant probability derived from career allow rate.

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