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 .
Claim Rejections - 35 USC § 112 – Indefiniteness
The following is a quotation of 35 U.S.C. 112(b):
(b) CONCLUSION.—The specification shall conclude with one or more claims particularly pointing out and distinctly claiming the subject matter which the inventor or a joint inventor regards as the invention.
The following is a quotation of 35 U.S.C. 112 (pre-AIA ), second paragraph:
The specification shall conclude with one or more claims particularly pointing out and distinctly claiming the subject matter which the applicant regards as his invention.
Claims 12, 13, 17, and 18 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.
Regarding instant claim 12, the transition phrase “selected from” at lines 4, 6, 10 and 12 renders the claim indefinite because it appears to suggest a Markush group, but does not recite “a group consisting of.” MPEP 211.03 (II) states “A claim element defined by selection from a group of alternatives (a Markush grouping; see MPEP §§ 2117 and 2173.05(h)) requires selection from a closed group "consisting of" (rather than "comprising" or "including") the alternative members. Abbott Labs. v. Baxter Pharmaceutical Products Inc., 334 F.3d 1274, 1280, 67 USPQ2d 1191, 1196-97 (Fed. Cir. 2003).” Accordingly, the lack of the closed claim language renders instant claim 12 indefinite. For the purposes of examination, “selected from” will be interpreted as “selected from a group consisting of.” The Examiner is taking this interpretation because the claim also recites the transition phrase “comprising” which indicates that the recitation of “selected from” is meant to provide different limitations than the open claim language of “comprising.”
Regarding claim 17, the phrase in parentheses renders the claim indefinite because it is unclear whether the limitation(s) in parentheses are part of the claimed invention. See MPEP § 2173.05(d).
Claim Rejections - 35 USC § 103
In the event the determination of the status of the application as subject to AIA 35 U.S.C. 102 and 103 (or as subject to pre-AIA 35 U.S.C. 102 and 103) is incorrect, any correction of the statutory basis (i.e., changing from AIA to pre-AIA ) for the rejection will not be considered a new ground of rejection if the prior art relied upon, and the rationale supporting the rejection, would be the same under either status.
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.
This application currently names joint inventors. In considering patentability of the claims the examiner presumes that the subject matter of the various claims was commonly owned as of the effective filing date of the claimed invention(s) absent any evidence to the contrary. Applicant is advised of the obligation under 37 CFR 1.56 to point out the inventor and effective filing dates of each claim that was not commonly owned as of the effective filing date of the later invention in order for the examiner to consider the applicability of 35 U.S.C. 102(b)(2)(C) for any potential 35 U.S.C. 102(a)(2) prior art against the later invention.
1) Claims 1-9, 11-15, 17, 19 and 21 are rejected under 35 U.S.C. 103 as being unpatentable over Din Belle et al. (US 10,717,726 B2, date of patent 07/21/2020; cited in IDS) in view of Allenspach et al. (US 2004/0186105 A1, publication date 09/23/2004).
Regarding instant claims 1-8, 14, 15 and 21, Din Belle relates to pyran derivatives [title] and claims 2-(Isoindolin-2-ylmethyl)-5-((1-(methylsulfonyl)piperidin-4-yl)methoxy)-4H-pyran-4-one and pharmaceutically acceptable salts thereof [claim 26; col. 259, lines 54-55]. According to Din Belle “[t]he compound can be given to a patient as such or in combination with suitable pharmaceutical excipients in the form of tablets” [col. 38, lines 20-23]. Din Belle discloses “the oral route being the preferred way. The contents of the active compound in the composition is from about 0.5 to 100%, preferably from about 0.5 to about 20%, per weight of the total composition” [col. 38, lines 29-34]. “Compounds of the invention may be administered to a patient in therapeutically effective amounts which range usually from about 1 to about 2000 mg” [col. 38, lines 12-15]. Furthermore, Din Belle discloses “[t]he mixture was cooled to RT, water (10 ml) was added and the product was extracted with EtOAc. The combined extracts were washed with water, dried with Na2SO4 filtered and evaporated. The crude product was purified by column chromatography to afford 0.21 g of the title compound” (i.e., 2-(Isoindolin-2-ylmethyl)-5-((1-(methylsulfonyl)piperidin-4-yl)methoxy)-4H-pyran-4-one) [Example 1; col. 101 – col. 102, lines 6-11].
Din Belle does not disclose wet granulation, an intragranular and an extragranular portion.
Allenspach discloses “[a]n orally deliverable pharmaceutical composition comprises a drug of low water solubility and a pregelatinized starch” [abstract]. According to Allenspach, “Such a composition has been found to exhibit a surprising and unexpected increase in drug dissolution rate consistency by comparison with otherwise similar compositions comprising a pregelatinized starch other than that specified immediately above [disclosed compositions]” [0014]. Consistent release rates are desirable to maintain regulatory compliance and reduce waste during manufacture [0003-0005]. In one example, “lactose monohydrate NF, pregelatinized starch NF, croscarmellose sodium NF and microcrystalline cellulose NF” formed a premix [0100] and “[t]he premix was granulated with purified water while mixing at high impeller and chopper speeds to form a wet mass” (i.e., intragranular part during wet granulation) [0101]. Once the “wet mass” premix was dried, it was “blended with extra-granular microcrystalline cellulose NF and croscarmellose sodium NF to form a uniform blend. Magnesium stearate was then added and blended to form a lubricated blend” [0102]. “The lubricated blend was charged into a tablet press hopper and compressed into core tablets” (i.e., instant claim 15) [0103]. The amounts and role of each component are discloses at Table 1, paragraph [0099], reproduced below. Valdecoxib is an exemplary active ingredient [0013].
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The components expressed as percents of their respective granular parts (i.e., intragranular and extragranular) can be seen in Table 2 below.
Component
Role
Intragranular Percent (~%)
Valdecoxib
Active
6.0
Lactose Monohydrate
Diluent (i.e., filler)
62.0
Microcrystalline Cellulose
Diluent (i.e., filler; instant claim 7)
18.1
Pregelatinized Starch
Binding agent
12.0
Croscarmellose sodium
Disintegrant (i.e., instant claim 8)
1.8
Extragranular Percent (~%)
Microcrystalline Cellulose
Diluent (i.e., filler)
88.2
Croscarmellose sodium
Disintegrant
8.8
Magnesium Stearate
Lubricant
2.9
Percent intragranular part per total weight
83%
Percent extragranular part per total weight
17%
It would have been obvious to one of ordinary skill in the art, before the effective filling date of the claimed invention, to have combined the pharmaceutical composition of Table 1 exhibiting consistent drug release profile of Allenspach with the active ingredient disclosed by Din Belle. One would have been motivated to make this combination for the advantages of the consistent release composition disclosed by Allenspach, e.g., regulatory compliance, reduced waste. One would have had a reasonable expectation of success because Din Belle discloses the active ingredient is not readily water soluble (i.e., ethyl acetate phase comprising compound 1 was washed with water in synthesis steps) as desired by Allenspach. Additionally, Din Belle discloses the compounds disclosed therein may be delivered in combination with pharmaceutically acceptable excipients and as tablets. Finally, in combining these elements one would have expected nothing more than predictable results because, when combined by known methods, each prior art element would have performed the same function as it had separately. See MPEP 2143, Exemplary Rationale A.
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(I). In the present case, the instantly claimed ranges for 2-(Isoindolin-2-ylmethyl)-5-((1-(methylsulfonyl)piperidin-4-yl)methoxy)-4H-pyran-4-one in the intragranular part (at least 5% of instant claims 2, 4 and 21; 5-20% of instant claim 3) and the mass of the active (0.5-10mg; instant claim 5) overlap with the ranges taught by the prior art of 6.0% 2-(Isoindolin-2-ylmethyl)-5-((1-(methylsulfonyl)piperidin-4-yl)methoxy)-4H-pyran-4-one in the intragranular part and 1-2000mg 2-(Isoindolin-2-ylmethyl)-5-((1-(methylsulfonyl)piperidin-4-yl)methoxy)-4H-pyran-4-one. Therefore a prima facie case of obviousness exist for each range.
Additionally, the ranges of claim 6 for the intragranular and extra granular components all overlap with the ranges taught by the prior art. Instant claim 6 recites an intragranular part comprising, per the mass of the intragranular part, 5-20% 2-(Isoindolin-2-ylmethyl)-5-((1-(methylsulfonyl)piperidin-4-yl)methoxy)-4H-pyran-4-one, 55-95% filler, 0.5-10% disintegrant and 1-15% binder. The overlapping ranges taught by the prior art are 6% 2-(Isoindolin-2-ylmethyl)-5-((1-(methylsulfonyl)piperidin-4-yl)methoxy)-4H-pyran-4-one, 80% filler (diluent), 1.88% disintegrant, and 12% binder. Instant claim 6 also recites an extragranular part comprising, per the mass of the extragranular part, 50-100% filler, 0-25% disintegrant and 0-25% lubricant. The overlapping amounts taught by the prior art are 88.2% filler (diluent), 8.8% disintegrant and 2.9% lubricant. Therefore a prima facie case of obviousness exists for each range claimed in instant claim 6.
Finally, the instantly claimed range for the percent intragranular part per total weight of the composition (30-95%; instant claim 14) overlaps with the value taught by the prior art (83% w/w) and so a prima facie case of obviousness exist.
Therefore, it would have been obvious to one of ordinary skill in the art, before the effective filling date of the claimed invention, to have formulated a wet granulated pharmaceutical composition comprising 2-(Isoindolin-2-ylmethyl)-5-((1-(methylsulfonyl)piperidin-4-yl)methoxy)-4H-pyran-4-one, a filler, a disintegrant, and a binder in an intragranular part and a filler, disintegrant and a lubricant in an extragranular part. Wherein each component is within the ranges of instant claims 2-6, and 21. Wherein the filler (diluent) comprises microcrystalline cellulose and the disintegrant comprises croscarmellose sodium. Wherein the percent of the intragranular portion is within the range of instant claim 14.
Regarding instant claim 9 and 11, Allenspach discloses the “composition of the invention optionally further comprises one or more pharmaceutically acceptable binding agents or adhesives as excipients, particularly where the composition is in the form of a tablet. Such binding agents and adhesives preferably impart sufficient cohesion to the blend being tableted to allow for normal processing operations such as sizing, lubrication, compression and packaging, but still allow the tablet to disintegrate and the composition to be absorbed upon ingestion. Suitable binding agents and adhesives include, either individually or in combination … hydroxypropylmethyl cellulose … One or more binding agents and/or adhesives, if present, constitute in total about 0.5% to about 25%” [0071].
It would have been obvious to one of ordinary skill in the art, before the effective filling date of the claimed invention, to have combined the hydroxypropylmethyl cellulose (HPMC) of Allenspach with the pharmaceutical composition taught by Din Belle and Allenspach. On would have been motivated to make this combination to impart sufficient cohesion to allow normal processing. One would have had an expectation of success because Allenspach discloses HPMC is a suitable binding agent. Additionally, in combining these elements one would have expected nothing more than predictable results because, when combined by known methods, each prior art element would have performed the same function as it had separately. See MPEP 2143, Exemplary Rationale A.
Furthermore, the claimed range for the binder (1-15%) would have continued to overlap with the range of the prior art after the combination of HPMC and the composition taught by Din Belle and Allenspach. Allenspach teaches amounts of additional binder as low as 0.5 % of the total composition is suitable. Combining 0.5% w/w of the total composition with the composition taught in Table 1 of Allenspach translates to the addition of 1mg of HPMC (200mg total weight) or 0.6% w/w of the intragranular part. This bring the total weight of the binder to 12.6% w/w of the intragranular part.
Therefore, it would have been obvious to one of ordinary skill in the art, before the effective filling date of the claimed invention, to have formulated the pharmaceutical composition taught by Din Belle and Allenspach, which comprises croscarmellose sodium, to further comprise HPMC.
Regarding instant claims 12 and 13, Allenspach discloses that “[i]n addition to at least one drug and a pregelatinized starch selected as described above, a composition of the invention optionally comprises one or more additional pharmaceutically acceptable diluents as excipients. Suitable diluents illustratively include, either individually or in combination, lactose, including anhydrous lactose and lactose monohydrate; mannitol” [0066]. Allenspach also discloses “[s]uch diluents, if present, constitute in total … about 20% to about 80%, by weight of the composition.” [0066] and that “The diluent or diluents selected preferably exhibit suitable flow properties and, where tablets are desired, compressibility” [0066].
It would have been obvious to one of ordinary skill in the art, before the effective filling date of the claimed invention, to have simply substituted mannitol in place of the lactose monohydrate of the composition discloses in Table 1 of Allenspach. One would have been motivated to make this substitution to achieve a composition with acceptable flow and compressibility properties. One would have had an expectation of success in making this substitution because Allenspach discloses lactose monohydrate and mannitol are both suitable diluents. The simple substitution of one known element (e.g., the mannitol of Allenspach) in place of another (e.g., the lactose monohydrate of Allenspach) in order to achieve predictable results (diluent) is prima facie obvious. See MPEP 2143, Exemplary Rationale B.
The composition taught by Din Belle and Allenspach would have therefore comprised components according to Table 3.
Table 3.
Component
Role
Intragranular Percent (~%)
2-(Isoindolin-2-ylmethyl)-5-((1-(methylsulfonyl)piperidin-4-yl)methoxy)-4H-pyran-4-one
Active
6.0
Mannitol
Diluent (i.e., filler)
24.1 – 96.4%; (20-80% of 200/166)
Microcrystalline Cellulose
Diluent (i.e., filler)
18.1
Pregelatinized Starch
Filler according to instant claim 12
12.0
Hydroxypropylmethyl cellulose
Binder
0.6-30.1; (0.5-25% of 200/166)
Croscarmellose sodium
Disintegrant
1.8
Extragranular Percent (~%)
Microcrystalline Cellulose
Diluent (i.e., filler)
88.2
Croscarmellose sodium
Disintegrant
8.8
Magnesium Stearate
Lubricant
2.9
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(I).
Regarding instant claim 12, the instantly claimed ranges, with respect to the intragranular part, for 2-(Isoindolin-2-ylmethyl)-5-((1-(methylsulfonyl)piperidin-4-yl)methoxy)-4H-pyran-4-one (5-20%), a filler of mannitol, pregelatinized starch and microcrystalline cellulose (55-95%), a disintegrant of croscarmellose sodium (0.5-10%) and a binder comprising HMPC (1-15%) overlap with the ranges of the prior art, with respect to the intragranular part, for 2-(Isoindolin-2-ylmethyl)-5-((1-(methylsulfonyl)piperidin-4-yl)methoxy)-4H-pyran-4-one (6.0%), a filler of mannitol and pregelatinized starch (54.2-100%), a disintegrant of croscarmellose sodium (1.8%) and a binder comprising HMPC (0.6-30.1%). Additionally, the instantly claimed ranges, with respect to the extragranular part, for a filler of microcrystalline cellulose (50-100%), a disintegrant of croscarmellose sodium (0-25%) and lubricant comprising sodium stearyl fumarate (0-25%) overlap with the ranges of the prior art, with respect to the extragranular part, for a binder of microcrystalline cellulose (88.2%), a disintegrant of croscarmellose sodium (8.8%) and 0% lubricant comprising sodium stearyl fumarate. Therefore a prima facie case of obviousness exists for each range recited in instant claim 12.
Regarding instant claim 13, the instantly claimed ranges, with respect to the intragranular part, for 2-(Isoindolin-2-ylmethyl)-5-((1-(methylsulfonyl)piperidin-4-yl)methoxy)-4H-pyran-4-one (5-20%), mannitol and pregelatinized starch (55-95%), croscarmellose sodium (0.5-10%) and HMPC (1-15%) overlap with the ranges of the prior art, with respect to the intragranular part, for 2-(Isoindolin-2-ylmethyl)-5-((1-(methylsulfonyl)piperidin-4-yl)methoxy)-4H-pyran-4-one (6.0%), mannitol and pregelatinized starch (36.1-100%), croscarmellose sodium (1.8%) and HMPC (0.6-30.1%). Additionally, the instantly claimed ranges, with respect to the extragranular part, for microcrystalline cellulose (50-100%), croscarmellose sodium (0-25%) sodium stearyl fumarate (0-25%) overlap with the ranges of the prior art, with respect to the extragranular part, for microcrystalline cellulose (88.2%), croscarmellose sodium (8.8%) and 0% sodium stearyl fumarate. Therefore a prima facie case of obviousness exists for each range recited in instant claim 13.
Regarding instant claim 17, Allenspach discloses that “[e]xcipients, in particular a disintegrant, for immediate release capsule and tablet compositions of the invention are preferably selected to provide a disintegration time of less than about 30 minutes” [0081]. In the context of Allenspach, disintegration time refers to 75-80% active release (i.e., dissolution of active) as measured in a dissolution assay, for example those performed according to USP24 using Apparatus 2 [0064-0065].
Generally, it is prima facie obvious to select a known material based on its suitability for its intended use. See MPEP 2144.07. In the present case, it would have been obvious to one of ordinary skill in the art, before the effective filling date of the claimed invention, to have selected 30 minutes as the disintegration time for the composition taught by Din Belle and Allenspach because Allenspach discloses 30 minutes is a suitable disintegration time for the tablet composition.
"[E]ven though product-by-process claims are limited by and defined by the process, determination of patentability is based on the product itself. The patentability of a product does not depend on its method of production. If the product in the product-by-process claim is the same as or obvious from a product of the prior art, the claim is unpatentable even though the prior product was made by a different process." In re Thorpe, 777 F.2d 695, 698, 227 USPQ 964, 966 (Fed. Cir. 1985) (See MPEP 2113.). In the present case the prior art product appears to be the same or obvious as claimed, despite not teaching the claimed method of measuring disintegration, insofar as the tablet of Allenspach is taught to disintegrate within 30 minutes.
Therefore, it would have been obvious to one of ordinary skill in the art, before the effective filling date of the claimed invention, to have formulated a pharmaceutical composition, as taught by Din Belle and Allenspach and discussed above, to provide a dissolution of at least 80% per weight within 45 minutes as instantly claimed.
Regarding instant claim 19, Allenspach discloses that “[f]or many drugs including valdecoxib, particle size reduction can lead to improved bioavailability when the drug is formulated in a composition of the invention. Illustratively in the case of valdecoxib, the D90 particle size is preferably less than about 75 μm, for example about 1 to about 70 μm, about 1 to about 40 μm or about 1 to about 30 μm” (i.e., 50% of the particles are must be less than 30microns) [0042].
It would have been obvious to one of ordinary skill in the art, before the effective filling date of the claimed invention, to have combined the teaching of particle size of Allenspach with the active, 2-(Isoindolin-2-ylmethyl)-5-((1-(methylsulfonyl)piperidin-4-yl)methoxy)-4H-pyran-4-one, disclosed by Din Belle. One would have been motivated to make this combination because Allenspach discloses particle size effects bioavailability and exemplifies a suitable range for the consistent release compositions disclosed therein. One would have had an expectation of success because Allenspach teaches that particle sizes for the active ingredient, exemplified by the particle sizes taught for valdecoxib, are suitable for the consistent release compositions. Additionally, in combining these elements one would have expected nothing more than predictable results because, when combined by known methods, each prior art element would have performed the same function as it had separately. See MPEP 2143, Exemplary Rationale A.
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(I). In the present case, the instantly claimed range for particle size (Dv50) of not more than 50 microns overlaps with the range of the prior art of 90% of particles between 1 and 30 microns and so a prima facie case of obviousness exists.
Therefore, it would have been obvious to one of ordinary skill in the art, before the effective filling date of the claimed invention, to have formulated a pharmaceutical composition, as taught by Din Belle and Allenspach and discussed above, such that the particle size of 2-(Isoindolin-2-ylmethyl)-5-((1-(methylsulfonyl)piperidin-4-yl)methoxy)-4H-pyran-4-one is within the instantly claimed range.
2) Claims 16 and 18 are rejected under 35 U.S.C. 103 as being unpatentable over Din Belle et al. (US 10,717,726 B2, date of patent 07/21/2020; cited in IDS) in view of Allenspach et al. (US 2004/0186105 A1, publication date 09/23/2004) as applied to claims 1-9, 11-15, 17, 19 and 21 above, and further in view of Holzer et al. (International Journal of Pharmaceutics, 1979, vol. 2, p. 145-153).
Din Belle and Allenspach, which are taught above, differ from the instant claims insofar as they do not disclose sodium stearyl fumarate. Allenspach discloses the lubricant to be magnesium stearate [0099].
Holzer relates to sodium stearyl fumarate as a tablet lubricant and discloses “[s]odium stearyl fumarate reduced the friction and the adhesion to about the same degree as magnesium stearate and had also about the same influence on tablet strength and disintegration … Sodium stearyl fumarate appears to be a good alternative to magnesium stearate” [abstract].
It would have been obvious to one of ordinary skill in the art, before the effective filling date of the claimed invention, to have simply substituted the sodium stearyl fumarate of Holzer in place of the magnesium stearate of Allenspach. One would have been motivated to, and had an expectation of success in making this substitution because Holzer discloses sodium stearyl fumarate is a good alternative to magnesium stearate. The simple substitution of one known element (e.g., the sodium stearyl fumarate of Holzer) in place of another (e.g., the magnesium stearate of Allenspach) in order to achieve predictable results (lubricant) is prima facie obvious. See MPEP 2143, Exemplary Rationale B.
Therefore, it would have been obvious to one of ordinary skill in the art, before the effective filling date of the claimed invention, to have formulated a pharmaceutical composition, as taught by Din Belle and Allenspach and discussed above, to comprise sodium stearyl fumarate as the lubricant.
3) Claims 16 and 18 are rejected under 35 U.S.C. 103 as being unpatentable over Din Belle et al. (US 10,717,726 B2, date of patent 07/21/2020; cited in IDS) in view of Allenspach et al. (US 2004/0186105 A1, publication date 09/23/2004) as applied to claims 1-9, 11-15, 17, 19 and 21 above, and further in view of Bharate (Journal of Drug Delivery Science and Technology, 2021, 66, 102913).
Din Belle and Allenspach, which are taught above, differ from the instant claims insofar as they do not disclose the p-tulenesulfonic acid salt of 2-(Isoindolin-2-ylmethyl)-5-((1-(methylsulfonyl)piperidin-4-yl)methoxy)-4H-pyran-4-one. Din Belle claims 2-(Isoindolin-2-ylmethyl)-5-((1-(methylsulfonyl)piperidin-4-yl)methoxy)-4H-pyran-4-one and pharmaceutically acceptable salts thereof [col. 259, lines 54-55 and col. 260, lines 14-15]. According to Din Belle “[p]harmaceutically acceptable salts are well known in the field of pharmaceuticals” and Non-limiting examples of salts with inorganic or organic acids include chlorides, bromides, sulfates, nitrates, phosphates, sulfonates” [col. 25, lines 13-14 and 20-23].
Bharate discloses “69 sulfonate salts are approved by FDA in the last seven decades comprising sulfate, mesylate, besylate, tosylate, methylsulfate, camsylate, isethionate, and edisylate salts” [abstract]. Additionally, “[t]osylate is a para-toluene sulfonic acid” [p. 8, col. 2, para. 2, line 1].
Generally, it is prima facie obvious to select a known material based on its suitability for its intended use. See MPEP 2144.07. In the present case, it would have been obvious to one of ordinary skill in the art, before the effective filling date of the claimed invention, to have to have selected the tosylate of Bharate as the pharmaceutically acceptable sulfonate salt of 2-(Isoindolin-2-ylmethyl)-5-((1-(methylsulfonyl)piperidin-4-yl)methoxy)-4H-pyran-4-one desired by Din Belle because Bharate discloses tosylate is a pharmaceutically acceptable sulfonate salt.
Therefore, it would have been obvious to one of ordinary skill in the art, before the effective filling date of the claimed invention, to have formulated a pharmaceutical composition, as taught by Din Belle and Allenspach and discussed above, wherein the pharmaceutically acceptable salt of 2-(Isoindolin-2-ylmethyl)-5-((1-(methylsulfonyl)piperidin-4-yl)methoxy)-4H-pyran-4-one is p-toluenesulfonic acid salt (tosylate). Wherein, as discussed above, the composition has an 80% dissolution rate within the instantly claimed range.
4) Claims 20 and 22 are rejected under 35 U.S.C. 103 as being unpatentable over Din Belle et al. (US 10,717,726 B2, date of patent 07/21/2020; cited in IDS) in view of Allenspach et al. (US 2004/0186105 A1, publication date 09/23/2004) as applied to claims 1-9, 11-15, 17, 19 and 21 above, and further in view of Barshied (US 20060076536 A1, publication date 04/13/2006).
Din Belle and Allenspach, which are taught above, differ from the instant claims insofar as they do not teach a package comprising an oxygen scavenger. Allenspach does teach packaging the compositions [0071].
Barshied “relates generally to a pharmaceutical packaging for increasing the product shelf life, reducing discoloration, and reducing degradation of pharmaceuticals by reducing the oxygen level present in the pharmaceutical package. The pharmaceutical package comprises a substantially oxygen impermeable container, at least one oxygen scavenging element disposed in the container, and at least one packaged pharmaceutical product disposed in the oxygen impermeable container” [abstract].
It would have been obvious to one of ordinary skill in the art, before the effective filling date of the claimed invention, to have combined the packaging having an oxygen scavenger of Barshied with the pharmaceutical composition taught by Din Belle and Allenspach. One would have been motivated to make this combination for the advantages described in Barshied, e.g., increased shelf life, reducing discoloration etc. One would have had an expectation of success because Allenspach desires a packaged pharmaceutical composition and Barshied discloses a packaging system for pharmaceutical compositions. Additionally, in combining these elements one would have expected nothing more than predictable results because, when combined by known methods, each prior art element would have performed the same function as it had separately. See MPEP 2143, Exemplary Rationale A.
Therefore, it would have been obvious to one of ordinary skill in the art, before the effective filling date of the claimed invention, to have formulated a pharmaceutical composition as taught by Din Belle and Allenspach, and discussed above, comprising 2-(Isoindolin-2-ylmethyl)-5-((1-(methylsulfonyl)piperidin-4-yl)methoxy)-4H-pyran-4-one and at least on excipient, wherein the composition is in a package comprising an oxygen scavenger.
Conclusion
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/C.T.W./ Examiner, Art Unit 1612
/WALTER E WEBB/ Primary Examiner, Art Unit 1612
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