DETAILED ACTION
Status of the Claims
Claims 1-14 are pending in the instant application. Claim 14 have been withdrawn based upon Restriction/Election as discussed below. Claims 1-13 are being examined on the merits in the instant application.
Advisory Notice
The present application, filed on or after March 16, 2013, is being examined under the first inventor to file provisions of the AIA .
Restriction/Election
Applicant's election without traverse of Group I drawn to compositions of matter, currently claims 1-13, in the reply filed on 05/29/2026 is acknowledged.
The requirement is deemed proper and is therefore made FINAL.
Claim 14 has been withdrawn from further consideration pursuant to 37 CFR 1.142(b) as being drawn to a nonelected subject matter, there being no allowable generic or linking claim. Election was made without traverse in the reply filed on 05/29/2026.
Priority
The instant case is a U.S. entry (371) of PCT/TR2022/051285 filed 11/11/2022 and claims priority to TR2021/017729 filed 11/15/2021.
The U.S. effective filing date has been determined to be 11/11/2021, the filing date of the document TR2021/017729.
Information Disclosure Statement
No Information Disclosure Statements have been filed in the instant application. Applicants are reminded of their duty to disclose patents and publications relevant to the patentability of the instant claims. Applicant is reminded of the requirements of 37 CFR 1.56 and Li Second Family Limited Partnership v. Toshiba Corp., 56 USPQ2d 1681 (Fed. Cir. 2000); accord McKesson Information Solutions, Inc. v. Bridge Medical, Inc. 487 F.3d 897, 913. (Fed.Cir.2007).
Specification
The abstract of the disclosure is objected to because the length is less than 50 words, and the Abstract page includes the invention Title on the same page. A corrected abstract of the disclosure is required and must be presented on a separate sheet, apart from any other text. See MPEP § 608.01(b).
Applicant is reminded of the proper language and format for an abstract of the disclosure.
The abstract should be in narrative form and generally limited to a single paragraph on a separate sheet within the range of 50 to 150 words in length. The abstract should describe the disclosure sufficiently to assist readers in deciding whether there is a need for consulting the full patent text for details.
The language should be clear and concise and should not repeat information given in the title. It should avoid using phrases which can be implied, such as, “The disclosure concerns,” “The disclosure defined by this invention,” “The disclosure describes,” etc. In addition, the form and legal phraseology often used in patent claims, such as “means” and “said,” should be avoided.
Claim Objections
Claim 1 is objected to because the word “tofasitinib” in lines 2 & 2 is misspelled and should be spelled tofacitinib. Appropriate correction is required.
Claims 1-4 are objected to because the claims recite “wherein tofa[c]itinb” which lacks a proper grammatical article (e.g. wherein the tofacitinib …). Appropriate correction is required.
Claims 12 and 13 are objected to because of the following informalities: the claim includes bullet points to set off constituent ingredients. Claim 12 includes capital letters for each first-character following the bullet point. The examiner suggest Applicant delete the bullet points from the claims and remove the capital letters in claim 12. Appropriate correction is required.
Claim Rejections - 35 USC § 112(b)
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 2-3, 5-11, 12 and 13 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 pre-AIA the applicant regards as the invention.
Claims 2 and 3 are rejected as being indefinite because the claims recite “preferably less than” in lines 1-2. A broad range or limitation together with a narrow range or limitation that falls within the broad range or limitation (in the same claim) may be considered indefinite if the resulting claim does not clearly set forth the metes and bounds of the patent protection desired. See MPEP § 2173.05(c). In the present instance, claim 2 recites the broad recitation “a d(.01) particle size of less than 10 μm”, and the claim also recites “preferably less that 5 μm” which is the narrower statement of the range/limitation. In the present instance, claim 2 recites the broad recitation “a d(0.9) particle size of less than 35 μm”, and the claim also recites “preferably less that 30 μm” which is the narrower statement of the range/limitation. The claim(s) are considered indefinite because there is a question or doubt as to whether the feature introduced by such narrower language is (a) merely exemplary of the remainder of the claim, and therefore not required, or (b) a required feature of the claims.
Claim 5 is rejected as being indefinite because the claim recites “wherein the film coated tablet comprises pharmaceutically acceptable excipients are selected from the group comprising fillers, disintegrants, lubricants, glidants or mixtures thereof.” Claim 5 is unclear for the following three reasons: (1) The claim language in claim 5 is grammatically incomplete or incoherent. The phrase “comprises pharmaceutically acceptable excipients are selected” contains no proper verb structure connecting the subject to the selection limitation. It is unclear whether the claim is attempting to state that the tablet comprises pharmaceutically acceptable excipients that are selected from the recited group, or that the pharmaceutically acceptable excipients of the tablet are selected from the recited group, or something else. A person of ordinary skill in the art cannot ascertain the metes and bounds of the claim with reasonable certainty. (2) Claim 5 lacks proper antecedent basis. Claim 1 introduces “at least one pharmaceutically acceptable excipient (entailing singular). Claim 5 then refers to “pharmaceutically acceptable excipients” (plural) without a clear antecedent basis further rendering the claim unclear. And claim 5 read in relevant parts “pharmaceutically acceptable excipients…” (claim 5, line 2). However, the base claim 1 recites “at least one pharmaceutically acceptable excipient” (claim 1, line 2), which encompasses one or more pharmaceutically acceptable excipients. Because of the one or more (i.e., at least one pharmaceutically acceptable excipient) entails, it is unclear whether the recitation “pharmaceutically acceptable excipients” is intended to refer to just one, more than one, or all of the pharmaceutically acceptable excipients. And (3) the Markush-type language “selected from the group comprising” is non-standard and introduces additional ambiguity. Conventional Markush claiming uses “selected from the group consisting of…” Use of “comprising” within the group language leaves open whether the listed members are exclusive or whether additional, unlisted members are permitted, compounding the indefiniteness already present from the defective sentence structure. Claims 6-11 are rejected as depending from and inheriting the same above-discussed issuses with claim 5, and doing nothing to clarify the same. Appropriate clarification is required.
Claim 12 contains the trademark/trade names PH 112 and Subertab 24AN-Anhydrous in lines 3 and 4, respectively. Where a trademark or trade name is used in a claim as a limitation to identify or describe a particular material or product, the claim does not comply with the requirements of 35 U.S.C. 112(b) or 35 U.S.C. 112 (pre-AIA ), second paragraph. See Ex parte Simpson, 218 USPQ 1020 (Bd. App. 1982). The claim scope is uncertain since the trademark or trade name cannot be used properly to identify any particular material or product. A trademark or trade name is used to identify a source of goods, and not the goods themselves. Thus, a trademark or trade name does not identify or describe the goods associated with the trademark or trade name. In the present case, the trademark/trade name is used to identify/describe a microcrystalline cellulose product and a lactose product, respectively, accordingly, the identification/description is indefinite.
Claims 12 and 13 are rejected as being indefinite because the claims include a number of constituents using bullet points, the claim recites “the tablet comprises” and “the film coated tablet comprises;” in line 1, respectively, it is unclear if the claim requires each of the bullet point items. Appropriate clarification is required.
Claim 12 recites the limitation "the tablet" in line 1. There is insufficient antecedent basis for this limitation in the claim.
Claim Rejections - 35 USC § 102
The following is a quotation of the appropriate paragraphs of 35 U.S.C. 102 that form the basis for the rejections under this section made in this Office action:
A person shall be entitled to a patent unless –
(a)(1) the claimed invention was patented, described in a printed publication, or in public use, on sale or otherwise available to the public before the effective filing date of the claimed invention.
Claims 1-6 and 8-11 are rejected under 35 U.S.C. 102(a)(1) as being clearly anticipated by SINGH (US 2017/0049774 A1; published February, 2017).
Applicant Claims
Applicant claims a film coated tablet comprising tofa[c]tinib or pharmaceutically acceptable salts thereof and at least one pharmaceutically acceptable excipient wherein [the] tofa[c]tinib or pharmaceutically acceptable salts thereof has a d(0.5) particle size of less than 20 μm (instant claim 1).
Disclosure of the Prior Art
SINGH discloses that: “D50 value, also known as median particle size, is defined as the particle diameter at which 50% of the particles have a diameter less than the diameter which corresponds to that value. The D50 value of tofacitinib particles in the present invention is about 20 µm or less, in particular about 10 µm or less, in particular between about 1 µm and 10 µm.” ([0052])(instant claim 1, “wherein [the] tofasitinib or pharmaceutically acceptable salts thereof has a d(0.5) particle size of less than 20 μm.”; instant claim 4).
SINGH discloses that: “D10 value is defined as the particle diameter at which 10% of the particles have a diameter less than the diameter which corresponds to that D10 value. The D10 value of tofacitinib particles in the present invention is about 5 μm or less, in particular between about 0.1 μm and 5 μm.” ([0053])(instant claims 2 & 4).
SINGH discloses that: “D90 value is defined as the particle diameter at which 90% of the particles have a diameter less than the diameter which corresponds to that D90 value. The D90 value of tofacitinib particles in the present invention is about 30 μm or less, in particular about 25 μm or less, in particular between about 15 μm and 25 μm.” ([0051])(instant claims 3 & 4).
SINGH discloses examples including the tofacitinib particles detailed above, including coated tablets in Examples 1(a) to 1(i) (osmotic tablets), Examples 2(a) to 2(f) (matrix tablets), Examples 3(a) to 3(d) (reservoir tablets), each including pharmaceutically acceptable excipients (instant claim 1). Particularly including fillers (syn. diluents) such as lactose ([0055]; Examples 1(a)-1(c), microcrystalline cellulose (Examples 2(a)-2(e))(instant claims 1, 4-5).
SINGH discloses examples including the lubricant magnesium stearate ([0063]) including coated tablets in Examples 1(a)-1(i) (osmotic tablets), Examples 2(a)-2(f) (matrix tablets), Examples 3(a)-3(d) (reservoir tablets), each including the lubricant magnesium stearate (instant claims 1, 5 & 8).
SINGH discloses examples including the glidant colloidal silicon dioxide ([0062]) in an amount of 1.00 mg/250 mg tablet (~0.4%) including coated tablets in Examples 1(i)(instant claims 1, 5, 9-11).
Claim Rejections - 35 USC § 103
The following is a quotation of 35 U.S.C. 103 which forms the basis for all obviousness rejections set forth in this Office action:
A patent for a claimed invention may not be obtained, notwithstanding that the claimed invention is not identically disclosed as set forth in section 102, if the differences between the claimed invention and the prior art are such that the claimed invention as a whole would have been obvious before the effective filing date of the claimed invention to a person having ordinary skill in the art to which the claimed invention pertains. Patentability shall not be negated by the manner in which the invention was made.
The factual inquiries set forth in Graham v. John Deere Co., 383 U.S. 1, 148 USPQ 459 (1966), that are applied 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.
Claims 1-13 are rejected under 35 U.S.C. 103 as being unpatentable over SINGH (US 2017/0049774 A1; published February, 2017).
Applicants Claims
Applicant claims a film coated tablet comprising tofa[c]tinib or pharmaceutically acceptable salts thereof and at least one pharmaceutically acceptable excipient wherein [the] tofa[c]tinib or pharmaceutically acceptable salts thereof has a d(0.5) particle size of less than 20 μm (instant claim 1). Applicant further claims the pharmaceutically acceptable excipient is a disintegrant (claim 5) and is croscarmellose sodium (claim 7).
Applicant claims the film coated tablet according to claim 1 comprising: tofacitinib citrate, microcrystalline cellulose, lactose, croscarmellose sodium, colloidal silicon dioxide, and magnesium stearate (instant claim 12).
Applicant claims the film coated tablet according to claim 1 comprising: 1.0-10.0% by weight of tofacitinib or pharmaceutically acceptable salts thereof, 45.0-70.0% by weight of microcrystalline cellulose, 20.0 to 35.0 by weight lactose, 1.0-7.0% by weight of croscarmellose sodium, 0.1-2.0% by weight colloidal silicon dioxide, 0.1-2.0% by weight of magnesium stearate, and 1.0-5.0% by weight of film coating agent in the total tablet formulation (instant claim 13).
The examiner is interpreting claims 12 and 13 as requiring each of the bullet point claim elements, and claim 13 is the amount range relative to the total weight of the film coated tablet.
Determination of the scope
and content of the prior art (MPEP 2141.01)
SINGH discloses film coated tofacitinib formulations as discussed above and incorporated herein by reference.
SINGH teaches “Suitable disintegrants are selected from the group comprising croscarmellose sodium, […].” ([0061])(instant claims 1, 5, 7, 12 and 13).
SINGH teaches that: “Preferably, the diluents are directly compressible lactose ([…] ), microcrystalline cellulose, sorbitol, pregelatinized starch, and combinations thereof.” [emphasis added]([0055])(instant claims 12-12, lactose and microcrystalline cellulose).
SINGH teaches that: “Suitable glidants are selected from the group comprising magnesium stearate, stearic acid, calcium stearate, colloidal silicon dioxide, starch, talc, and combinations thereof.” ([0062]). And that: “Suitable lubricants are selected from the group comprising magnesium stearate, talc, and silica.” ([0063])(instant claims 12-12, colloidal silicon dioxide & magnesium stearate).
Regarding the amounts recited in claim 13, SINGH teaches Example 1(a) including lactose in an amount of 152.24 mg/226.0 mg tablet which is ~67% by weight, Example 1(b) including lactose in an amount of 132.24 mg/226 mg tablet which is ~58% by weight. It would have been prima facie obvious to provide a combination of lactose and microcrystalline cellulose in a combined amount ~58% or ~67%, as suggested by SINGH ([0055]). SINGH does not teach an example including croscarmellose sodium, however, SINGH teaches Examples including crospovidone, particularly Example 3(a) including 12 mg/220mg tablet which is ~ 5.45% by weight. It would have been prima facie obvious to combine/substitute croscarmellose sodium with/for the copovidone in a similar amount, based on the common function as a disintegrant ([0061]). SINGH teaches Example 1(i) including colloidal silicon dioxide in an amount of 1.0 mg/250mg tablet which is ~ 0.4% by weight. SING teaches Example 1(a) including magnesium stearate in an amount of 2.0 mg/226 mg tablet which is ~0.89% by weight. SINGH teaches the film coating agent Eudragit® E PO in Example 1(a) in an amount of 5.71 mg/226 mg tablet which is ~2.5% by weight of the tablet. SING teaches tofacitinib citrate is included in an amount of 17.76 mg/226 mg tablet which is ~ 8.0% by weight (Examples 1(a,b,c,d), 2(a,b,c).
Ascertainment of the difference between
the prior art and the claims (MPEP 2141.02)
The difference between the rejected claims and the teachings of SINGH is that SINGH does not expressly teach an Example including each of the claimed constituents of instant claims 12 and/or 13 in the amounts of claim 13, however, each of the constituents are used in the same or similar amount as now claimed, and it would have been within the ordinary level of skill to combine the constituents taught disclosed for the very same purposes in a film coated tofacitinib (citrate) film coated tablet, as clearly suggested by SINGH.
Finding of prima facie obviousness
Rationale and Motivation (MPEP 2142-2143)
It would have been prima facie obvious to one of ordinary skill in the art before the effective filing date of the claimed invention to produce a tofacitinib film coated table including conventional pharmaceutical excipients, as suggested by SINGH, in order to produce a suitable tablet dosage form of the same for oral delivery.
From the teachings of the references, it is apparent that one of ordinary skill in the art would have had a reasonable expectation of success in producing the claimed invention. Therefore, the invention as a whole would have been prima facie obvious to one of ordinary skill in the art before the effective filing date of the claimed invention, as evidenced by the references, especially in the absence of evidence to the contrary.
In light of the forgoing discussion, the Examiner concludes that the subject matter defined by the instant claims would have been obvious within the meaning of 35 USC 103.
Conclusion
Claims 1-13 are pending and have been examined on the merits. The abstract of the disclosure is objected; claims 1-4, 12 and 13 are objected to. Claims 2-3, 5-11, 12 and 13 are rejected under 35 U.S.C. 112(b); claims 1-6 and 8-11 are rejected under 35 U.S.C. 102(a)(1) and claims 1-13 are rejected under 35 U.S.C. 103. No claims allowed at this time.
Any inquiry concerning this communication or earlier communications from the examiner should be directed to IVAN A GREENE whose telephone number is (571)270-5868. The examiner can normally be reached M-F, 8-5 PM PST.
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If attempts to reach the examiner by telephone are unsuccessful, the examiner’s supervisor, David Blanchard can be reached on (571) 272-0827. The fax phone number for the organization where this application or proceeding is assigned is 571-273-8300.
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/IVAN A GREENE/Examiner, Art Unit 1619
/TIGABU KASSA/Primary Examiner, Art Unit 1619
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