DETAILED ACTION
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 .
In view of the amendment, previous 112(b) rejection on claim 3, previous 112(b) rejection on claim 9, previous 112(b) rejection on claim 13, previous 112(b) rejection on claims 19-22,
In view of applicant’s clarification, previous 112(b) rejection on clams 1-4 is hereby withdrawn. In their REMARKS, applicant state that “a means present in the oral dosage form” specifies that means for achieving stability for 24 months is a feature of the product. Thus, the Examiner interprets “a means present in the oral dosage form for making the oral dosage form substantially stable for 24 months” as a product limitation.
Due to the terminal disclaimers filed, previous double patenting rejections over the claims of U.S. Pat. 12,528,787 B2, U.S. Pat. 12,447,149 B2, U.S. Pat. 12,551,483 B2 and co-pending App. 19/421,407 are hereby withdrawn.
It is to be noted that (i) the effective filing date of independent claims 1 and 14 is not December 8, 2023 (on which the provisional application 63/607,697 was filed) but December 6, 2024 instead: the provisional application does not provide adequate support for instant limitation of claim 1 “a means in the oral dosage form for making the oral dosage form substantially stable for 24 months;” or instant limitation of claim 14 “wherein the oral dosage form is substantially stable for 24 month” (there is support (see [000563]-[000565]) only for the crystalline dihydrate form of the compound of Formula (I) being stable for at least 24 months upon static storage about 25oC at about 97% relative humidity or upon static storage at about 40oC at about 75% relative humidity or upon static storage at about 25oC at about 60% relative humidity). That is, there is no support for the oral dosage form substantially stable for 24 months at any conditions. Also there is no support for “a means present in the original dosage form for making the oral dosage form substantially stable for 24 months.” However, (ii) the effective filing date of independent claim 5 is December 8, 2023.
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.
Claim Rejections - 35 USC § 112
The following is a quotation of the first paragraph of 35 U.S.C. 112(a):
(a) IN GENERAL.—The specification shall contain a written description of the invention, and of the manner and process of making and using it, in such full, clear, concise, and exact terms as to enable any person skilled in the art to which it pertains, or with which it is most nearly connected, to make and use the same, and shall set forth the best mode contemplated by the inventor or joint inventor of carrying out the invention.
The following is a quotation of the first paragraph of pre-AIA 35 U.S.C. 112:
The specification shall contain a written description of the invention, and of the manner and process of making and using it, in such full, clear, concise, and exact terms as to enable any person skilled in the art to which it pertains, or with which it is most nearly connected, to make and use the same, and shall set forth the best mode contemplated by the inventor of carrying out his invention.
Claims 29 is rejected under 35 U.S.C. 112(a) or 35 U.S.C. 112 (pre-AIA ), first paragraph, as failing to comply with the written description requirement. The claim(s) contains subject matter which was not described in the specification in such a way as to reasonably convey to one skilled in the relevant art that the inventor or a joint inventor, or for applications subject to pre-AIA 35 U.S.C. 112, the inventor(s), at the time the application was filed, had possession of the claimed invention.
Applicant amended claim 29 to recite that the one or more disintegrants is lactose monohydrate. Such new limitation is not supported in the originally filed disclosure (besides, lactose monohydrate is already being recited as the one or more fillers – see lines 4-5 of claim 29).
Instant 112(a) rejection can be overcome by changing “the one or more disintegrants is lactose monohydrate;” to --- the one or more disintegrants is cross-linked polyvinylpyrrolidone; ---.
The following is a quotation of 35 U.S.C. 112(f):
(f) Element in Claim for a Combination. – An element in a claim for a combination may be expressed as a means or step for performing a specified function without the recital of structure, material, or acts in support thereof, and such claim shall be construed to cover the corresponding structure, material, or acts described in the specification and equivalents thereof.
The following is a quotation of pre-AIA 35 U.S.C. 112, sixth paragraph:
An element in a claim for a combination may be expressed as a means or step for performing a specified function without the recital of structure, material, or acts in support thereof, and such claim shall be construed to cover the corresponding structure, material, or acts described in the specification and equivalents thereof.
The claims in this application are given their broadest reasonable interpretation using the plain meaning of the claim language in light of the specification as it would be understood by one of ordinary skill in the art. The broadest reasonable interpretation of a claim element (also commonly referred to as a claim limitation) is limited by the description in the specification when 35 U.S.C. 112(f) or pre-AIA 35 U.S.C. 112, sixth paragraph, is invoked.
As explained in MPEP § 2181, subsection I, claim limitations that meet the following three-prong test will be interpreted under 35 U.S.C. 112(f) or pre-AIA 35 U.S.C. 112, sixth paragraph:
(A) the claim limitation uses the term “means” or “step” or a term used as a substitute for “means” that is a generic placeholder (also called a nonce term or a non-structural term having no specific structural meaning) for performing the claimed function;
(B) the term “means” or “step” or the generic placeholder is modified by functional language, typically, but not always linked by the transition word “for” (e.g., “means for”) or another linking word or phrase, such as “configured to” or “so that”; and
(C) the term “means” or “step” or the generic placeholder is not modified by sufficient structure, material, or acts for performing the claimed function.
Use of the word “means” (or “step”) in a claim with functional language creates a rebuttable presumption that the claim limitation is to be treated in accordance with 35 U.S.C. 112(f) or pre-AIA 35 U.S.C. 112, sixth paragraph. The presumption that the claim limitation is interpreted under 35 U.S.C. 112(f) or pre-AIA 35 U.S.C. 112, sixth paragraph, is rebutted when the claim limitation recites sufficient structure, material, or acts to entirely perform the recited function.
Absence of the word “means” (or “step”) in a claim creates a rebuttable presumption that the claim limitation is not to be treated in accordance with 35 U.S.C. 112(f) or pre-AIA 35 U.S.C. 112, sixth paragraph. The presumption that the claim limitation is not interpreted under 35 U.S.C. 112(f) or pre-AIA 35 U.S.C. 112, sixth paragraph, is rebutted when the claim limitation recites function without reciting sufficient structure, material or acts to entirely perform the recited function.
Claim limitations in this application that use the word “means” (or “step”) are being interpreted under 35 U.S.C. 112(f) or pre-AIA 35 U.S.C. 112, sixth paragraph, except as otherwise indicated in an Office action. Conversely, claim limitations in this application that do not use the word “means” (or “step”) are not being interpreted under 35 U.S.C. 112(f) or pre-AIA 35 U.S.C. 112, sixth paragraph, except as otherwise indicated in an Office action.
Claims 1-4 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 limitation “a means present in the oral dosage form for making the oral dosage form substantially for 24 months;” invokes 35 U.S.C. 112(f) or pre-AIA 35 U.S.C. 112, sixth paragraph. However, the written description fails to disclose the corresponding structure, material, or acts for performing the entire claimed function and to clearly link the structure, material, or acts to the function: there is insufficient disclosure in the present specification of the corresponding structure, material, or acts for performing the claimed function of stabilizing the oral dosage form for 24 months. Nor is there a clear linkage (explained in the present specification) between the structure, material, or acts and the function. That is, what in the oral dosage form achieves stability for 24 months? Therefore, the claim is indefinite and is rejected under 35 U.S.C. 112(b) or pre-AIA 35 U.S.C. 112, second paragraph.
Applicant may:
(a) Amend the claim so that the claim limitation will no longer be interpreted as a limitation under 35 U.S.C. 112(f) or pre-AIA 35 U.S.C. 112, sixth paragraph;
(b) Amend the written description of the specification such that it expressly recites what structure, material, or acts perform the entire claimed function, without introducing any new matter (35 U.S.C. 132(a)); or
(c) Amend the written description of the specification such that it clearly links the structure, material, or acts disclosed therein to the function recited in the claim, without introducing any new matter (35 U.S.C. 132(a)).
If applicant is of the opinion that the written description of the specification already implicitly or inherently discloses the corresponding structure, material, or acts and clearly links them to the function so that one of ordinary skill in the art would recognize what structure, material, or acts perform the claimed function, applicant should clarify the record by either:
(a) Amending the written description of the specification such that it expressly recites the corresponding structure, material, or acts for performing the claimed function and clearly links or associates the structure, material, or acts to the claimed function, without introducing any new matter (35 U.S.C. 132(a)); or
(b) Stating on the record what the corresponding structure, material, or acts, which are implicitly or inherently set forth in the written description of the specification, perform the claimed function. For more information, see 37 CFR 1.75(d) and MPEP §§ 608.01(o) and 2181.
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)(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) 1-4 are rejected under 35 U.S.C. 102(a)(2) as being anticipated by Kostik et al (US 12,528,787 B2, which is equivalent to WO 2025/122942 A1, US 2025/0206720 A1, US 2025/0243182 A1 and US 2026/0103452 A1) .
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. 102(a)(2) 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) if the same invention is not being claimed; 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 in the reference 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.
Kostik teaches (see claim 13) the following:
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Kostik further teaches (claim 14-16) that the pharmaceutically acceptable composition of claim 13 is in the form of a capsule (Kostik also teaches (col.153, lines 62-64) that its pharmaceutically acceptable composition can be in the form of a tablet as well). Thus, Kostik teaches instant pharmaceutically acceptable oral dosage form of claim 1 comprising instant crystalline dihydrate form of a compound of Formula (I) wherein the crystalline dihydrate form of the compound of Formula (I) has an X-ray powder diffraction (XRPD) pattern comprising peaks, in terms of 2-theta, at about 10.9o, 16.8o and 27.1o as measured by CuKa radiation. Kostik also teaches instant limitation of claim 4 (“wherein the XRPD pattern comprises peaks in terms of 2-theta, at about 5.9o, 11.9o, and 13.7o as measured by CuKa radiation”).
With respect to instant limitation “a means present in the oral dosage form for making the oral dosage form substantially stable for 24 months” (of claim 1), (i) Kostik teaches (col.162, lines 55-58, col.163, lines 26-29) that the crystalline dihydrate form of its compound of Formula (I) is stable upon static storage at about 25oC and about 97% relative humidity for at least 24 months or at about 40oC and about 75% relative humidity for at least 24 months (Kostik also teaches (col.161, lines 41-50, lines 64-67, col.162, lines 1-4) that crystalline solid-state forms of its compound of Formula (I) are highly stable and that the “stability” of particular solid-state form of compound of Formula (I) means that at least 75 wt.%, 80 wt..%, 85 wt.%, 90 wt.%, 95 wt.%, 96 wt.%, 97 wt.%, 98 wt.% or 99 wt.% of said form remains as said form at the end of the storage period without converting to another form of the compound of Formula (I), thus teaching instant limitation “substantially stable”). Kostik teaches (col.8, lines 30-41) that different solid forms (i.e., different polymorphs) of a single compound (a drug compound) may result in differences with respect to stability for formulated pharmaceutical products (due to the variety of solid forms having distinct physical properties). (ii) Furthermore, as shown above, in claim 13, Kostik teaches that the crystalline dihydrate form of the compound of Formula (I) is present in the composition with a D10 particle size distribution of about 2-10 microns; a d50 particle size distribution of about 12 - 24 microns, and a d90 particle size distribution of about 32 - 40 microns. Kostik teaches (col.2, lines 12-18) that particle size is a critical attribute of an active pharmaceutical ingredient and plays a critical role in the development and commercialization of solid dosage forms and teaches that particle size distribution has a crucial impact on several aspects of a drug, such as stability. (iii) Kostik also teaches (col.153, lines 38-42) that preservatives and chelating agents can be added to its pharmaceutical acceptable composition at levels safe for ingestion to improve storage stability. Thus, one skilled in the art would immediately envisage adding preservatives and chelating agents to Kostik’s pharmaceutical acceptable composition (in the form of a capsule or a tablet). Thus, it is the Examiner’s position that (i) the Kostik’s crystalline dihydrate form of its compound of Formula (I) (as a pharmaceutically active ingredient), which is substantially stable upon static storage at about 25oC and about 97% relative humidity for at least 24 months or at about 40oC and about 75% relative humidity for at least 24 months, (ii) the particle size distribution characteristics of the crystalline dihydrate form (as described in Kostik’s claim 13), and (iii) the use of preservatives and chelating agents are all making the oral dosage form (containing the crystalline dihydrate form of the compound of Formula (I)) substantially stable for at least 24 months. Furthermore, the preservative and chelating agents discussed above teaches instant means present in the original dosage form for making the oral dosage form substantially stable for 24 months.
Thus, Kostik teaches instant claims 1 and 4.
With respect to instant claims 2 and 3, Kostik teaches (claims 14-16) that the pharmaceutically acceptable composition of claim 13, which is in the form of a capsule, contains about 15.2 mg, about 21.7 mg or about 32.5 mg of the crystalline dihydrate form. Thus, Kostik teaches instant claims 2 and 3 (Kostik’s “about 15.2 mg” teaches instant about 14 mg of claim 3, Kostik’s “about 21.7 mg” teaches instant about 20 mg of claim 3 and Kostik’s “about 32.5 mg” teaches instant about 30 mg of claim 3).
Claim Rejections - 35 USC § 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 14 and 19-28 is/are rejected under 35 U.S.C. 103 as being obvious over Kostik et al (US 12,528,787 B2, which is equivalent to WO 2025/122942 A1, US 2025/0206720 A1, US 2025/0243182 A1 and US 2026/0103452 A1) in view of Brown et al (US 2021/0002271 A1).
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).
Kostik teaches (see claim 13) the following:
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Kostik further teaches (claim 14-16) that the pharmaceutically acceptable composition of claim 13 is in the form of a capsule (Kostik also teaches (col.153, lines 62-64) that its pharmaceutically acceptable composition can be in the form of a tablet as well). Thus, Kostik teaches instant pharmaceutically acceptable oral dosage form of claim 14 comprising instant crystalline dihydrate form of a compound of Formula (I) wherein the crystalline dihydrate form of the compound of Formula (I) has an X-ray powder diffraction (XRPD) pattern comprising peaks, in terms of 2-theta, at about 10.9o, 16.8o and 27.1o as measured by CuKa radiation. Kostik also teaches instant limitation of claim 28 (“wherein the XRPD pattern comprises peaks in terms of 2-theta, at about 5.9o, 11.9o, and 13.7o as measured by CuKa radiation”).
With respect to instant limitation “wherein the oral dosage form is substantially stable for 24 months” (of claim 14), (i) Kostik teaches (col.162, lines 55-58, col.163, lines 26-29) that the crystalline dihydrate form of its compound of Formula (I) is stable upon static storage at about 25oC and about 97% relative humidity for at least 24 months or at about 40oC and about 75% relative humidity for at least 24 months (Kostik also teaches (col.161, lines 41-50, lines 64-67, col.162, lines 1-4) that crystalline solid-state forms of its compound of Formula (I) are highly stable and that the “stability” of particular solid-state form of compound of Formula (I) means that at least 75 wt.%, 80 wt..%, 85 wt.%, 90 wt.%, 95 wt.%, 96 wt.%, 97 wt.%, 98 wt.% or 99 wt.% of said form remains as said form at the end of the storage period without converting to another form of the compound of Formula (I), thus teaching instant limitation “substantially stable”). Kostik teaches (col.8, lines 30-41) that different solid forms (i.e., different polymorphs) of a single compound (a drug compound) may result in differences with respect to stability for formulated pharmaceutical products (due to the variety of solid forms having distinct physical properties). (ii) Furthermore, as shown above, in claim 13, Kostik teaches that the crystalline dihydrate form of the compound of Formula (I) is present in the composition with a D10 particle size distribution of about 2-10 microns; a d50 particle size distribution of about 12 - 24 microns, and a d90 particle size distribution of about 32 - 40 microns. Kostik teaches (col.2, lines 12-18) that particle size is a critical attribute of an active pharmaceutical ingredient and plays a critical role in the development and commercialization of solid dosage forms and teaches that particle size distribution has a crucial impact on several aspects of a drug, such as stability. (iii) Kostik also teaches (col.153, lines 38-42) that preservatives and chelating agents can be added to its pharmaceutical acceptable composition at levels safe for ingestion to improve storage stability. Thus, it is the Examiner’s position that (i) the Kostik’s crystalline dihydrate form of its compound of Formula (I) (as a pharmaceutically active ingredient), which is substantially stable upon static storage at about 25oC and about 97% relative humidity for at least 24 months or at about 40oC and about 75% relative humidity for at least 24 months, (ii) the particle size distribution characteristics of the crystalline dihydrate form (as described in Kostik’s claim 13), and (iii) the use of preservatives and chelating agents would all make the oral dosage form (containing the crystalline dihydrate form of the compound of Formula (I)) substantially stable for at least 24 months and that Kostik’s oral dosage form containing the at least 24 month-stable crystalline dihydrate form of the compound of Formula (I) together with the specific particle size distribution features and the preservative (and chelating agents) would be stable for at least 24 months.
With respect to instant limitation of claim 14 “about 20% by weight to about 97% by weight of one or more fillers based on the total weight of the oral dosage form; about 1% by weight to about 20% by weight of one or more disintegrants based on the total weight of the oral dosage form; and about 0.1% by weight to about 10% by weight of one or more lubricants based on the total weight of the oral dosage form”, among exemplary excipients to be used as the pharmaceutically acceptable excipient (as mentioned in claim 13), Kostik includes fillers, disintegrating agents and lubricants (col.4, lines 65-67, col.5, lines 1-2). Kostik does not explicitly teach instant ranges for the amounts of fillers, disintegrating agents and lubricants. However, as evidenced by Brown et al ([0190]), it is already known in the art that pharmaceutical compositions in the form of tablets or capsules can contain 0-20 wt.% of disintegrants, 0-5 wt.% lubricants and 0-99 wt.% fillers. It would have been obvious to one skilled in the art to contain fillers, disintegrating agents and lubricants in Kostik’s pharmaceutically acceptable composition in the amounts of 0-99 wt.%, 0-20 wt.% and 0-5 wt.%, respectively, according to the art-known practice with a reasonable expectation of success. These ranges for the amounts of filler, disintegrating agents and lubricants overlap with instant ranges for the amounts of filler (about 20-97 wt.%), disintegrating agents (about 1-20 wt.%) and lubricants (about 0.1-10 wt.%), thus rendering instant ranges prima facie obvious. In the case “where the [claimed] ranges overlap or lie inside ranges disclosed by the prior art,” a prima facie case of obviousness would exist which may be overcome by a showing of unexpected results, In re Wertheim, 541 F.2d 257, 191 USPQ 90 (CCPA 1976).
Thus, Kostik in view of Brown renders obvious instant claims 14 and 28.
With respect to instant claims 23, Kostik teaches (claims 14-16) that the pharmaceutically acceptable composition of claim 13, which is in the form of a capsule, contains about 15.2 mg, about 21.7 mg or about 32.5 mg of the crystalline dihydrate form. Thus, Kostik in view of Brown renders obvious instant claim 23.
With respect to instant claims 19-22, Kostik teaches (col.15, lines 15-20) that the crystalline dihydrate form of the compound of Formula (I) has not more than about 10 mol%, not more than about 5 mol%, not more than about 3 mol% or not more than about 1 mol% of other solid-state forms of the compound of Formula (I). Thus, Kostik in view of Brown renders obvious instant claims 19-22.
With respect to instant claims 25-26, Kostik teaches (col.169, lines 49-57) that the DSC (differential scanning calorimetry) thermogram (as shown in Kostik’s Fig.2 which is the same as instant Fig.2) for the crystalline dihydrate form of the compound of Formula (I) in an open pan exhibits a broad endothermic event with onset varying between about 75oC to about 95oC, an exothermic event with onset varying between about 123oC and 150oC and a sharp endotherm with onset at about 214oC. Thus, Kostik in view of Brown renders obvious instant claims 25-26.
With respect to instant claims 24 and 27, Kostik teaches (col.169, lines 41-44) that the crystalline dihydrate form of the compound of Formula (I) has the XRPD pattern of its Fig.1 (which is the same as instant Fig.1) and a TGA thermogram of its Fig.3 (which is the same as instant Fig.3). Thus, Kostik in view of Brown renders obvious instant claims 24 and 27.
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.
Claim(s) 15-18 and 29 are rejected under 35 U.S.C. 103 as being unpatentable over Kostik et al (US 12,528,787 B2, which is equivalent to WO 2025/122942 A1, US 2025/0206720 A1, US 2025/0243182 A1 and US 2026/0103452 A1) in view of Brown et al (US 2021/0002271 A1) as applied to claim 14 above, and further in view of Berner (US 2013/0316002 A1).
With respect to instant claims 15-18, the Examiner established above that Kostik in view of Brown renders it obvious to add fillers, disintegrating agents and lubricants in the amounts of 0-99 wt.%, 0-20 wt.% and 0-5 wt.%, respectively, to Kostik’s pharmaceutically acceptable composition (in the form of a capsule or tablet) according to the art-known practice with a reasonable expectation of success. Kostik furthermore teaches (col.152, lines 60-63) magnesium stearate among examples for the lubricants that can be used in its solid dosage form. Kostik does not teach instant filler (lactose monohydrate) or instant disintegrant (crosslinked polyvinylpyrrolidone). However, as evidenced by Berner (see [0088], [0122]-[0123]), crosslinked polyvinylpyrrolidone and lactose monohydrate are known in the art as commonly used disintegrants and fillers, respectively, in solid oral dosage forms, such as capsules or tablets. It would have been obvious to one skilled in the art to use lactose monohydrate (as the filler), crosslinked polyvinylpyrrolidone (as the disintegrant) and magnesium stearate (as the lubricant) in Kostik’s solid dosage form with a reasonable expectation of success. Thus, Kostik in view of Brown, and further in view of Berner renders obvious instant claims 15-18.
With respect to instant claim 29, as discussed above, Kostik in view of Brown renders it obvious to add fillers, disintegrating agents and lubricants in the amounts of 0-99 wt.%, 0-20 wt.% and 0-5 wt.%, respectively, to Kostik’s pharmaceutically acceptable composition (in the form of a capsule or tablet). Thus, based on the teachings of Kostik in view of Brown, and further in view of Berner, it would be obvious to one skilled in the art to use 0-99 wt.% of lactose monohydrate (as the filler), 0-20 wt.% of crosslinked polyvinylpyrrolidone (as the disintegrant) and 0-5 wt.% of magnesium stearate (as the lubricant) in Kostik’s solid dosage form with a reasonable expectation of success. These ranges overlaps with instant ranges for the amounts of lactose monohydrate (about 80-90 wt.%), crosslinked polyvinylpyrrolidone (about 1-10 wt.%) and lubricant (about 0.1-3 wt.%), thus rendering instant ranges prima facie obvious. In re Wertheim, supra. Current claim language states that the lactose monohydrate acts both as a filler as well as a disintegrant. Thus, 0-99 wt.% of lactose monohydrate as taught by Kostik in view of Brown and Berner also teaches instant one or more disintegrant which is lactose monohydrate, and the range 0-99 wt.% overlaps with instant range about 1-10 wt.% for the one or more disintegrants, thus rendering instant range for the one or more disintegrant prima facie obvious. In re Wertheim, supra. Thus, Kostik in view of Brown, and further in view of Berner renders obvious instant claim 29.
Claims 5 and 11-13 are rejected under 35 U.S.C. 103 as being obvious over SOTO et al (WO 2025/096349 A1 which is equivalent to US 2026/0048052 A1) in view of Brown et al (US 2021/0002271 A1).
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).
Soto teaches ([000137]) a capsule comprising 21.7 mg of crystalline dihydrate form of the compound of Formula (I) shown below that is being administered to a patient twice a week
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. Soto teaches ([000135]) that in some embodiments, the crystalline dihydrate form of the compound of Formula (I) has a purity of greater than 99.5 wt.% (i.e., 0.5 wt.% or less of any other solid state form of the compound of Formula (I) is present) as measured by XRPD. This means that the XRPD pattern of the crystalline dihydrate form of Soto’s compound of Formula (I) with such high purity would (i) naturally or inherently comprise peaks, in terms of 2-theta, at about 10.9o, 16.8o and 27.1o as measured by CuKa radiation, as instantly recited in claim 5; (ii) naturally or inherently comprise peaks, in terms of 2-theta, at about 5.9o, 11.9o, and 13.7o as measured by CuKa radiation, as instantly recited in claim 11; and (iii) naturally or inherently have an XRPD pattern substantially as shown in FIG.1, as instantly recited in claim 12 (since applicant teaches that the crystalline dihydrate form of instant compound of Formula (I) is represented by the XRPD pattern of Fig.1, and since Fig.1 shows peaks (2-theta) at about 10.9o, 16.8o, 27.1o, 5.9o, 11.9o and 13.7o).
With respect to instant limitation “about 20% by weight to about 97% by weight of one or more fillers based on the total weight of the oral dosage form; about 1% by weight to about 20% by weight of one or more disintegrants based on the total weight of the oral dosage form; and about 0.1% by weight to about 10% by weight of one or more lubricants based on the total weight of the oral dosage form”, Soto teaches the use of pharmaceutically acceptable carrier(s) together with its compound of Formula (I) but does not give any details. However, as evidenced by Brown et al ([0190]), it is already known in the art that pharmaceutical compositions in the form of tablets or capsules typically contain pharmaceutically acceptable excipients, such as disintegrants (in the amount of 0-20 wt.%), lubricants (in the amount of 0-5 wt.%), and fillers (in the amount of 0-99 wt.%). It would have been obvious to one skilled in the art to contain fillers, disintegrating agents and lubricants in Soto’s pharmaceutical composition in the amounts of 0-99 wt.%, 0-20 wt.% and 0-5 wt.%, respectively, according to the art-known practice with a reasonable expectation of success. These ranges for the amounts of filler, disintegrating agents and lubricants overlap with instant ranges for the amounts of filler (about 20-97 wt.% of claim 5 and about 80-97 wt.% of claim 13), disintegrating agents (about 1-20 wt.% of claim 5 and about 1-10 wt.% of claim 13) and lubricants (about 0.1-10 wt.% of claim 5 and about 0.1-3 wt.% of claim 13), thus rendering instant ranges of claims 5 and 13 prima facie obvious. In re Wertheim, supra. Thus, Soto in view of Brown renders obvious instant claims 5 and 11-13.
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.
Claim(s) 7-10 are rejected under 35 U.S.C. 103 as being unpatentable over SOTO et al (WO 2025/096349 A1 which is equivalent to US 2026/0048052 A1) in view of Brown et al (US 2021/0002271 A1) as applied to claim 5 above, and further in view of Berner (US 2013/0316002 A1).
With respect to instant claims 7-10, the Examiner established above that Soto in view of Brown renders it obvious to add fillers, disintegrating agents and lubricants in the amounts of 0-99 wt.%, 0-20 wt.% and 0-5 wt.%, respectively, to Soto’s pharmaceutical composition (in the form of a capsule) according to the art-known practice with a reasonable expectation of success. Brown does not teach instant filler (lactose monohydrate), instant disintegrant (crosslinked polyvinylpyrrolidone) or instant lubricant (magnesium stearate). However, as evidenced by Berner (see [0088], [0116], [0122]-[0123]), crosslinked polyvinylpyrrolidone, lactose monohydrate and magnesium stearate are known in the art as commonly used disintegrants, fillers and lubricants, respectively, in solid oral dosage forms such as capsules or tablets. It would have been obvious to one skilled in the art to use lactose monohydrate (as the filler), crosslinked polyvinylpyrrolidone (as the disintegrant) and magnesium stearate (as the lubricant) in Soto’s solid dosage form (capsule) with a reasonable expectation of success. Thus, Soto in view of Brown, and further in view of Berner renders obvious instant claims 7-10.
Claim(s) 6 is rejected under 35 U.S.C. 103 as being unpatentable over SOTO et al (WO 2025/096349 A1 which is equivalent to US 2026/0048052 A1) in view of Brown et al (US 2021/0002271 A1) as applied to claim 5 above, and further in view of MISIC (US 2022/0096519 A1).
Soto in view of Brown does not teach instant limitation of claim 6. Misic teaches ([0039]) that uniformity of content ensures that a consistent dose of an active pharmaceutical ingredient is maintained in each individual dosage form (e.g., in each capsule or in each tablet) of a batch. In order to determine uniformity of content, multiple capsules or tablets are selected at random and a suitable analytical method is applied to assay the individual content of the API in each capsule or tablet. According to European and US pharmacopoeia, from the obtained assay analyses, a relative standard deviation (RSD) and an acceptance value (AV) are calculated. The calculated AV should be lower than 15 for content uniformity. The RSD and AV are preferably calculated as set out in “The United States pharmacopeia”, 37th version, physical tests, <905> Uniformity of Dosage Units, May 1, 2014. It would have been obvious to one skilled in the art to provide Soto’s uniform dosage form (i.e., a capsule comprising crystalline dihydrate form of the compound of Formula (I)) to have an acceptance value less than 15 according to USP <905> in order to ensure that a consistent dose of API is maintained in each capsule in a batch. Thus, Soto in view of Brown, and further in view of Misic renders obvious instant claim 6.
Response to Arguments
Applicant argue that Kostik et al does not qualify as prior art over instant application because Kostik has the same effective filing date (December 8, 2023) as the instant application. However, for the reasons explained in detail in in Paragraph 5 above, the effective filing date of instant claims (except for claims 5-13) is December 6, 2024, not December 8, 2023. Thus, currently, based upon the earlier effectively filed date of the reference, Kostik constitutes prior art under 35 U.S.C. 102(a)(2).
Applicant also argue that in view of Hamed’s 130(b) declaration filed on August 3, 2026, instant 103 rejections over SOTO et al (WO 2025/096349 A1 which is equivalent to US 2026/0048052 A1) in view of Brown et al (US 2021/0002271 A1) should be withdrawn, however, the 130(b) declaration should show that the prior art subject matter was preceded by an inventor-originated disclosure of the same subject matter. However, no such showing was made in the 130(b) declaration filed. Thus, instant 103 rejections over SOTO in view of Brown still stand.
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/SIN J LEE/
Primary Examiner, Art Unit 1613
August 24, 2026
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