DETAILED ACTION
Notice of Pre-AIA or AIA Status
The present application is being examined under the pre-AIA first to invent provisions.
Applicant’s arguments, filed 15 June 2026, have been fully considered. Rejections and/or objections not reiterated from previous office actions are hereby withdrawn. The following rejections and/or objections are either reiterated or newly applied. They constitute the complete set presently being applied to the instant application.
Status of Claims
Applicant elected, without traverse, Group I, claims 1-16, 19-29, 33, 35 and 37 in the reply filed on 06/24/2024. The claims of Groups II-V, as well as claims 1-16, 21, 28-29, 33, 35, and 37 have been cancelled by Applicants. Therefore, claims 19-20, 22-27, 38-43, 46, and 49 are pending and examined.
Claim Objections
Claims 24 is objected to because of the following informalities: immediately prior to “one or more binders” in row 3 of the table, and “one of more disintegrants” in row 4 of the table, there should be recited --- the --- in each instance, i.e. --- the one or more binders ---, and --- the one or more disintegrants ---. Appropriate correction is required.
Claim Rejections - 35 USC § 112(d)
The following is a quotation of 35 U.S.C. 112(d):
(d) REFERENCE IN DEPENDENT FORMS.—Subject to subsection (e), a claim in dependent form shall contain a reference to a claim previously set forth and then specify a further limitation of the subject matter claimed. A claim in dependent form shall be construed to incorporate by reference all the limitations of the claim to which it refers.
The following is a quotation of pre-AIA 35 U.S.C. 112, fourth paragraph:
Subject to the following paragraph [i.e., the fifth paragraph of pre-AIA 35 U.S.C. 112], a claim in dependent form shall contain a reference to a claim previously set forth and then specify a further limitation of the subject matter claimed. A claim in dependent form shall be construed to incorporate by reference all the limitations of the claim to which it refers.
Claim 38 is rejected under 35 U.S.C. 112(d) or pre-AIA 35 U.S.C. 112, 4th paragraph, as being of improper dependent form for failing to further limit the subject matter of the claim upon which it depends, or for failing to include all the limitations of the claim upon which it depends.
Claim 38 depends from claim 19 and recites wherein the one or more binder further comprises hydroxypropyl cellulose. However, claim 19 already recites wherein one or more binders comprise hydroxypropyl cellulose. Therefore claim 38 fails to further limit claim 19.
Applicant may cancel the claim(s), amend the claim(s) to place the claim(s) in proper dependent form, rewrite the claim(s) in independent form, or present a sufficient showing that the dependent claim(s) complies with the statutory requirements.
Claim Rejections – 35 U.S.C. § 103
The text of those sections of Title 35, U.S. Code not included in this action can be found in a prior Office action.
Claims 19-29, 39, and 41-45 are rejected under 35 U.S.C. 103(a) as being unpatentable over Washburn et al. (US 2008/0234367, 09/25/2008, hereinafter Washburn) in view of Himmelsbach et al. (US 2007/0249544, 10/25/2007, hereinafter Himmelsbach), further in view of Azarmi et al. (“Current Perspectives in Dissolution Testing of Conventional and Novel Dosage Forms”, 10/06/2006) (hereinafter Azarmi), and further in view of Lo et al. (US 5,516,530, 05/14/1996, hereinafter Lo).
Washburn teaches a tablet formulation for administering SGLT2 inhibitors (¶¶0147-0152). The formulation includes 1-350mg SGLT2 inhibitor; a filler (diluent), such as lactose or mannitol, at about 0% to 90% (¶0150); a binder, such as wax, at less than 500 microns at about 0% to 35% (¶0151); disintegrants at 0%-20% (¶0157); tableting lubricants at about 0.2% to 8% (¶0152); glidants (¶0152); a coating at 0%-15% comprising one or more film-formers or binders and plasticizers including hydrophilic polymers such as hydroxypropylmethylcellulose (¶0153). Washburn teaches formulating the tablets by using e.g. wet or dry granulation to form granules, blending the granules with further excipients (¶0166). In one embodiment, the ratio of the SGLT2 inhibitor to other anti-obesity agent or antidiabetic agent may be about 0.2:1 (¶0035). The lubricant may be magnesium stearate at 0.2-8% (¶0152), the binder may include hydrophilic polymers such as HPMC (¶0153) or lactose (¶0151), the plasticizer may include polyethylene glycol (¶0153), the glidant may be Syloid® brand silicon dioxide (i.e. colloidal silicon dioxide) (¶0152), fillers include microcrystalline cellulose at 1-80% (¶0150) and disintegrants include croscarmellose sodium (table 1). The coating may also include titanium dioxide, talc, and colorant (¶0158).
Washburn does not teach that the active ingredient is crystalline 1-chloro-4-(beta-D-glucopyranos-1-yl)-2-[4-((S)-tetrahydrofuran-3-yloxy)-benzyl]-benzene, also known as empagliflozin, or the use of HPC as the binder.
Himmelsbach teaches a pharmaceutical composition comprising 1mg-100mg of crystalline 1-chloro-4-(beta-D-glucopyranos-1-yl)-2-[4-((S)-tetrahydrofuran-3-yloxy)-benzyl]-benzene (i.e. Compound A, which is the same compound as instantly claimed as evidenced by the instant specification at page 11, first row on the table) and one or more conventional carriers and/or diluents (¶¶3 and 61 and Figs 1-2 demonstrating same crystalline structure as instant drawings). Compound A is taught as a SGLT2 inhibitor (¶¶3-4). The composition may be formulated as conventional galenic preparations such as plain or coated tablets, capsules, powders suspensions or suppositories (¶61). The crystalline form allows for high purity of the active ingredient (¶¶5 and 56). Uniform distribution of the medicament in the formulation is a critical factor, particularly when the medicament has to be given in low doses (¶6). To ensure uniform distribution, the particle size of the active substance can be reduced to a suitable level, e.g. by grinding (or micronizing) (¶61).
Washburn and Himmelsbach differ from the instant claims insofar as not disclosing wherein the film-formers comprise HPC, or a specific dissolution condition as instantly claimed.
Lo teaches delivery devices, such as pharmaceutical tablets, comprising water-soluble polymers acting as a binder, including hydroxypropyl cellulose or HPMC (col.3).
Washburn, Himmelsbach, and Lo differ from the instant claims insofar as not explicitly disclosing a specific dissolution condition as instantly claimed.
Azarmi demonstrates that pharmaceutical formulations are conventionally modified to optimize dissolution profiles “[n]ovel dosage forms present unique problems in the development of in vitro release technologies simply because of the physiochemical properties of the formulations and the unique physiological environment in which they should release their content” (see entire document, especially ¶ 1-3). Moreover, Azarmi indicates that “..it is necessary to further develop in vitro assays for novel dosage forms and to establish standard protocols for their drug release tests including the use of biorelevant dissolution media…for quality control purposes of certain dosage forms…” (p. 19), such as conventional release tablets, immediate release tablets, extended release tablets, powders, sublingual and buccal tablets, chewing gums and chewable tablets, encapsulated formulations, transdermal delivery systems and suppositories in order to evaluate the release properties of the chemical compounds under various conditions (Id., pp. 13-17). Azarmi further indicates that “… dissolution testing should be a sensitive and a reliable predictor of bioavailability [but] a predictive tool for the in vitro and in vivo dissolution behavior of a dosage form…” (p. 13). Azarmi teaches that conventional approaches for media utilization in typical dissolution profiles include: dilute hydrochloric acid, buffers in the physiologic pH range of 1.2–7.5, simulated gastric fluid (with or without enzymes), simulated intestinal fluid (with or without enzymes), water, and surfactants solutions such as polysorbate 80, and sodium lauryl sulfate (General Chapter (1092), USP 29, Suppl. 2). Table 1 shows examples of different USP dissolution media used for dissolution testing of tablets and capsules. (p. 13, col. 1).
Accordingly, it would have taken no more than the relative skills of one of ordinary skill in the art to have conducted many dissolution tests, producing varying results depending upon the type of pharmaceutical composition and the dissolution test conditions, such as utilizing a multitude of solvents under varying conditions, and arrived at the claimed dissolution profile through routine experimentation based on the dissolution time desired. "[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.” See MPEP § 2144.05(II)(A). Moreover, in any case, Himmelsbach teaches the same composition as instantly claimed, disclosing that the compound, Compound A, is an SGLT2 inhibitor (Id., pp. 7-8), teaches conventional carriers and/or diluents, and wherein ‘[u]niform distribution of the medicament in the formulation is a critical factor, to ensure uniform distribution, the particle size of the active substance can be reduced to a suitable level, e.g., by grinding…or micronizing, and demonstrate the same crystalline structure as within the Drawings as instantly disclosed (Id., p. 8). As such, regarding the claimed dissolution profile, where the structure of the composition (i.e. a composition comprising a SGLT2 inhibitor with specified ratio of disintegrant to binder) is taught by the prior art, there is a reasonable expectation that the functional recitations regarding such a composition are also met, given that the function of compositions are a product of the compositions structure. See MPEP 2112.01(II).
Himmelsbach does not explicitly teach specific excipients for formulating the crystalline 1-chloro-4-(beta-D-glucopyranos-1-yl)-2-[4-((S)-tetrahydrofuran-3-yloxy)-benzyl]-benzene. Accordingly, it would have been prima facie obvious to one of ordinary skill in the art to use the crystalline form of 1-chloro-4-(beta-D-glucopyranos-1-yl)-2-[4-((S)-tetrahydrofuran-3-yloxy)-benzyl]-benzene when formulating the composition of Washburn, given Himmelsbach teaches that the crystalline form of the compound is highly pure. MPEP 2144.06.
It would have been obvious to one of ordinary skill in the art to have included HPC as a film-former since it is a known and effective water-soluble polymer capable as a binder and suitable for pharmaceutical dosage forms including tablets as taught by Lo. See MPEP 2144.06.
Further, it would have been prima facie obvious to one of ordinary skill in the art to reduce the particle size of the active agent via grinding or micronizing in order to optimize the distribution of the medicament in the formulation, as taught by Himmelsbach. See MPEP 2144.05.
In the case where the claimed ranges overlap or lie inside ranges disclosed by the prior art, a prima facie case of obviousness exists. See MPEP 2144.05. Here, the ranges of SGLT2 inhibitor (1-350mg), a filler/diluent (0% to 90%), a binder (0% to 35% and <500[Symbol font/0x6D]m) and disintegrant (0%-20%) overlap with the instantly recited ranges of active (0.5-25%), diluent (65-93%), binder (1-5% and <250[Symbol font/0x6D]m), disintegrant (1-4%), and disintegrant to binder ratio (1.5:3.5 to 1:1).
Response to Arguments
Applicant mainly asserts on pp. 10-11 of the Remarks dated 06/15/2026 that Lo relates to high porosity delivery devices and Lo’s selection of water-soluble polymer is based on a requirement to form “porous tablets having high strength as a result of their laminate structure.” In contrast, Washburn’s selection of excipients is based on preparing a tablet using a wet granulation process, and Himmelsbach’s selection of excipients is based on preparing conventional galenic preparations such as plain or coated tablets. Therefore, one skilled in the art would find no suggestion or motivation to modify a formulation prepared by wet granulation process as described by Washburn in view of Himmelsbach based on the teachings of Lo (for preparing a porous delivery device) and thereby arrive at the presently claimed invention. Applicant further asserts Lo describes about 26 water soluble polymers that may be employed. Thus, one skilled in the art would find no guidance or motivation to modify the formulation of Washburn as modified to replace HPCM with HPC based on the teachings of Lo.
The Examiner does not find the Applicant’s assertions to be persuasive. The disclosure of Washburn is not limited to wet granulation. Washburn discloses wherein the tablet formulation may comprise one or more film-formers or binders, including hydrophilic polymers such as hydroxypropylmethylcellulose (HPMC). Lo discloses known and effective film-formers or binders in delivery devices including pharmaceutical tablets, including hydrophilic polymers such as HPMC and hydroxypropyl cellulose or HPMC (col.3). Accordingly, as discussed in the rejection above, it would have been obvious to one of ordinary skill in the art to have included hydroxypropyl cellulose in the tablet formulation since it is a known and effective water-soluble polymer capable as a binder and suitable for pharmaceutical dosage forms including tablets as taught by Lo. As supported by MPEP § 2144.06, generally, it is obvious to combine known compositions each of which is taught by the prior art to be useful for the same purpose (in this instant case as a water-soluble polymer suitable as film-former or binder), in order to form a third composition to be used for the very same purpose. See MPEP § 2144.06.
Regarding the Applicant’s assertion about the disclosure of Lo listing additional species, the fact that Lo discloses alternative water-soluble polymers in addition to hydroxypropyl cellulose (HPC) does not render HPC less obvious as a choice of water-soluble polymer suitable as film-former or binder. See also MPEP § 2131.02(II), where the Board held that the comprehensiveness of a listing did not negate the fact that a claimed compound was specifically taught. The Board compared the facts to the situation in which a compound was found in the Merck Index, saying that "the tenth edition of the Merck Index lists ten thousand compounds. In our view, each and every one of those compounds is ‘described’ as that term is used in that publication." As such, Applicant’s assertion is unpersuasive.
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.
Claims 19-29 and 38-51 are rejected on the ground of nonstatutory double patenting as being unpatentable over:
Claims 1-5 of U.S. Patent No. 7,713,938;
Claims 1-12 of U.S. Patent No. 7,723,309;
Claims 1-4 and 11-12 of U.S. Patent No. 8,283,326;
Claims 1-7 of U.S. Patent No. 8,507,450;
Claims 1-5, 20-23, and 31-40 of U.S. Patent No. 8,551,957;
Claims 1-5 of U.S. Patent No. 10,406,172;
Claims 1-11 and 14-22 of U.S. Patent No. 10,596,120;
Claims 1-29 of U.S. Patent No. 10,610,489,
each taken in view of US 2008/0234367 (Washburn et al., 09/25/2008, hereinafter Washburn), US 5,516,530 (Lo et al., 05/14/1996, hereinafter Lo), and “Current Perspectives in Dissolution Testing of Conventional and Novel Dosage Forms” (Azarmi et al., 10/06/2006) (hereinafter Azarmi). The patented claims teach crystalline forms of or pharmaceutical compositions of 1-chloro-4-(beta-D-glucopyranos-1-yl)-2-[4-((S)-tetrahydrofuran-3-yloxy)-benzyl]-benzene (i.e. instantly claimed compound). However, the claims do not teach the instantly recited excipients in tablet form.
Washburn is discussed above but does not teach use of the crystalline form of 1-chloro-4-(beta-D-glucopyranos-1-yl)-2-[4-((S)-tetrahydrofuran-3-yloxy)-benzyl]-benzene as the SLGT2 inhibitor.
Azarmi is discussed above as teaching performing various dissolutions tests in various dissolution conditions.
Lo is discussed above as teaching HPC is a tablet binder like HPMC.
It would have been prima facie obvious to one of ordinary skill in the art formulating the composition claimed in the cited patents, each of which recites the SLGT2 inhibitor 1-chloro-4-(beta-D-glucopyranos-1-yl)-2-[4-((S)-tetrahydrofuran-3-yloxy)-benzyl]-benzene, to choose excipients such as those taught by Washburn and Lo, given that Washburn teaches a composition for formulating SGLT2 inhibitors.
Response to Arguments
Applicant presents similar assertions as presented above regarding the 103 obviousness rejection, mainly arguing against inclusion of hydroxypropyl cellulose as disclosed by Lo in the disclosure of Washburn.
The Examiner has discussed the disclosures of Washburn and Lo in detail in the Response to Arguments section above (starting on page 7 of this Office action), and this non-statutory double patenting rejection is maintained for the same reasons set forth above in the 103 obviousness rejection’s Response to Arguments section.
Conclusion
THIS ACTION IS MADE FINAL. 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 LUCY TIEN at (571)272-8267. The examiner can normally be reached on Monday - Thursday 8:30 AM - 6:30 PM EST.
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If attempts to reach the examiner by telephone are unsuccessful, the examiner’s supervisor, SAHANA KAUP can be reached on (571) 272-6897. The fax phone number for the organization where this application or proceeding is assigned is 571-273-8300.
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/LUCY M TIEN/Examiner, Art Unit 1612
/SAHANA S KAUP/Supervisory Primary Examiner, Art Unit 1612
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