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 .
Claims Status
Claims 1-11 are pending and under current examination.
Information Disclosure Statement
Information Disclosure Statement (IDS) filed on 02/05/2024 has been considered by the Examiner. A signed copy of the IDS is included with the present Office Action.
Abstract-objection
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.
The abstract of the disclosure is objected to because of the implied phraseology “the disclosed invention relates to” and because of the recitation “more specifically” since the abstract should be clear and concise.
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).
Claim Rejections - 35 USC § 112
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 1-11 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 1 and 11 recite the limitation at least one organic or inorganic basic excipient. The term “basic” in claim 1 renders the scope of the claim indefinite. It is unclear if “basic” refers to an excipient that is a base or if basic refers to common or conventional excipients. The term basic is not defined by the claim, the specification does not provide a standard for ascertaining which excipients are basic and one of ordinary skill in the art would not be appraised of the scope of the invention since basic excipients is not an art recognized term for excipients. Although the instant specification recites basic excipients such as sodium croscarmellose and calcium hydrogen phosphate, the specification does not clearly define which excipients meet a “basic excipient” in the context of the claim. Examples of excipients such as in the instant specification does not require the basic excipient necessarily be the sodium croscarmellose or calcium hydrogen phosphate. Accordingly, the scope of claims 1 and 11 is indefinite. Dependent claims 2-10 do not rectify the deficiency of claims 1 and 11.
Claim 2 recites the stable pharmaceutical composition according to claim 1, further comprises one or more other pharmaceutically acceptable excipients. It is unclear if the further excipients are inclusive of any organic/inorganic basic and/or at least one acid excipients. The scope of the “other pharmaceutically acceptable excipients” is unclear because the instant specification does not define which compounds can comprise another excipient. Although paragraph [0057] recites other excipients such as surfactants and/or binders it is unclear if such excipients are basic or acidic excipients or not since claim 1 is unclear.
Claim 3 recites that wherein at least one organic or inorganic basic excipient include but are not limited to. The phrase include but not limited to renders the claim indefinite because it is unclear what other alternatives are intended to be encompassed by the claim See In re Kiely, 2022 USPQ2d 532 at 2* (Fed. Cir. 2022). A Markush grouping is a closed group of alternatives, i.e., the selection is made from a group "consisting of" (rather than "comprising" or "including") the alternative members. Abbott Labs., 334 F.3d at 1280, 67 USPQ2d at 1196. If a Markush grouping requires a material selected from an open list of alternatives (e.g., selected from the group "comprising" or "consisting essentially of" the recited alternatives), the claim is indefinite because it is unclear what other alternatives are intended to be encompassed by the claim. See In re Kiely, 2022 USPQ2d 532 at 2* (Fed. Cir. 2022) ( see MPEP 2173.05(h). Furthermore, it is unclear if at least one organic or inorganic basic excipient of claim 3 refers back to the at least one organic or inorganic basic excipient of claim 1 or an additional basic excipient because the claim does not recite “the” at least one organic or inorganic basic excipient.
Claim 4 recites wherein at least one organic or basic excipient include. The phrase include is synonymous with comprising and renders the claim indefinite because it is unclear what other alternatives are intended to be encompassed by the claim See In re Kiely, 2022 USPQ2d 532 at 2* (Fed. Cir. 2022). A Markush grouping is a closed group of alternatives, i.e., the selection is made from a group "consisting of" (rather than "comprising" or "including") the alternative members. Abbott Labs., 334 F.3d at 1280, 67 USPQ2d at 1196. If a Markush grouping requires a material selected from an open list of alternatives (e.g., selected from the group "comprising" or "consisting essentially of" the recited alternatives), the claim is indefinite because it is unclear what other alternatives are intended to be encompassed by the claim. See In re Kiely, 2022 USPQ2d 532 at 2* (Fed. Cir. 2022) ( see MPEP 2173.05(h). Furthermore, it is unclear if at least one organic or inorganic basic excipient of claim 3 refers back to the at least one organic or inorganic basic excipient of claim 1 or an additional basic excipient because the claim does not recite “the” at least one organic or inorganic basic excipient.
Claim 5 recites “the stable pharmaceutical composition of claim 1 wherein the weak acids include but are not limited to the organic acid or inorganic acids including but not limited to tartaric, fumaric, citric or adipic acid”. There is insufficient antecedent basis for the limitation “the weak acids” because claim 1 recites at least one organic or inorganic acid and not a weak acid. The limitation “the organic or inorganic acids” in line 2 of claim 5 lacks antecedent basis because claim 1 recites “at least one” organic or inorganic acid (singular). Thus, it is unclear if the organic or inorganic acids refers back to the one or more than one acid of claim 1. Furthermore, the phrase “include but are not limited to” and “including” in claim 5 is improper Markush language for the selection of the weak acid and organic acid or inorganic acid because it is unclear what other alternatives are intended to be encompassed by the claim See In re Kiely, 2022 USPQ2d 532 at 2* (Fed. Cir. 2022). A Markush grouping is a closed group of alternatives, i.e., the selection is made from a group "consisting of" (rather than "comprising" or "including") the alternative members. Abbott Labs., 334 F.3d at 1280, 67 USPQ2d at 1196. If a Markush grouping requires a material selected from an open list of alternatives (e.g., selected from the group "comprising" or "consisting essentially of" the recited alternatives), the claim is indefinite because it is unclear what other alternatives are intended to be encompassed by the claim. See In re Kiely, 2022 USPQ2d 532 at 2* (Fed. Cir. 2022) ( see MPEP 2173.05(h).
Claim 6 recites “wherein the weak acid is” and “wherein the alkaline or basic excipient is selected from”. There is insufficient antecedent basis for the limitation “the weak acid” because claim 1 recites at least one organic or inorganic acid and not a weak acid. Therefore, it is unclear if the weak acid is referring to the at least one organic or inorganic acid of claim 1 or not. Furthermore, “the alkaline or basic excipient” of claim 6 lacks antecedent basis for the alkaline excipient because claim 1 does not recite an alkaline excipient. The phrase alkaline or basic excipient renders the scope of the claim unclear because claim 1 does not recite an alkaline or basic excipient, thus it is unclear which alkaline excipient the claim is referring to since claim 1 recites at least one organic or inorganic basic excipient. Lastly, it is unclear if the selection in claim 6 refers to a selection of closed end or open list of alternatives because the claim recites “selected from” and not “selected from the group consisting of”. A Markush grouping is a closed group of alternatives, i.e., the selection is made from a group "consisting of" (rather than "comprising" or "including") the alternative members. Abbott Labs., 334 F.3d at 1280, 67 USPQ2d at 1196.
Claim 7 recites the stable pharmaceutical composition according to claim 1, wherein the composition comprises varenicline or pharmaceutically acceptable salts thereof and one or more of alkaline or basic excipients. It is unclear if alkaline or basic excipients are the same at least one basic excipient of claim 1 or further excipients than required by claim 1 since claim 1 recites at least one inorganic or organic basic excipient.
Claim 10 lacks antecedent basis for the recitation of weak acid because claim 10 depends from claim 1 which does not require any weak acid, and furthermore it is unclear if alkaline or basic excipient refers to the at least one organic or inorganic basic excipient of claim 1 (i.e. the one or more inorganic or organic basic excipient of claim 1 or not).
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, 7-8 and 11 are rejected under 35 U.S.C. 102(a)(2) as being anticipated by He et al. (United States Patent Publication 20230190762- effective date of 6/25/2021).
He et al. discloses stable solid varenicline compositions comprising croscarmellose cellulose sodium (a cellulose) and anhydrous dibasic calcium phosphate (aka dicalcium phosphate basic excipient) with varenicline tartrate, microcrystalline cellulose (other excipient), and magnesium stearate lubricant see paragraph [0002], see title, Table 1 and formula of final blend. Nitrosamine impurities include less than 6ppm, see paragraphs [0099]-[0100].
Accordingly, He et al. anticipates instant claims 1-4, 7-8 and 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 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.
Claim(s) 1-11 are rejected under 35 U.S.C. 103 as being unpatentable over He et al. (United States Patent Publication 20230190762- effective date of 6/25/2021).
Regarding clams 1-4, and 7-8 and 11, He et al. teach stable solid varenicline compositions comprising croscarmellose cellulose sodium (a cellulose) and anhydrous dibasic calcium phosphate (aka dicalcium phosphate basic compound) with varenicline tartrate, microcrystalline cellulose (other excipient), and magnesium stearate lubricant see paragraph [0002], see title Example 1 and formula of final blend at paragraph [0082]. The tablets can comprise a nitrosamine impurity of less than 6ppm, see paragraph [0099]-[0100], or less than 9ppm, see paragraph [0049] rendering obvious having within the daily acceptable limit of 9ppm.
Regarding instant claims 5-6, He et al. teach that pH adjusting agents including but not limited to a selection from tartaric, citric acid or fumaric acid (weak acids) are added to the solid dosage forms to adjust the pH of the drug environment of the final solid dosage form to a desired or optimum pH range, see paragraph [0042]. Example 1 comprises the basic excipient of dibasic calcium phosphate of which He et al. teach are incorporated as fillers in the solid dosage form.
Regarding instant claim 9, Example 1 comprises about 0.855% if varenicline tartarate per dosage form. The varenicline however can comprise about 0.1-5mg or about 0.5 wt percent to about 2.5% by weight, see paragraphs [0033]-[0034]. Therefore, it would have been obvious to adjust the concentration of varenicline tartarate at Example 1 within ranges of about 0.5-2.5% by weight which overlaps and renders obvious the claimed range of 0.4-0.7% by weight. In the case where the claimed ranges "overlap or lie inside ranges disclosed by the prior art" a prima facie case of obviousness exists. In re Wertheim, 541 F.2d 257, 191 USPQ 90 (CCPA 1976); In re Woodruff, 919 F.2d 1575, 16 USPQ2d 1934 (Fed. Cir. 1990). Furthermore, Example 1 teaches 0.855% by weight varenicline tartarate, and a prima facie case of obviousness exists where the claimed ranges or amounts do not overlap with the prior art but are merely close. Titanium Metals Corp. of America v. Banner, 778 F.2d 775, 783, 227 USPQ 773, 779 (Fed. Cir. 1985).
Regarding instant claim 10, the varenicline tartarate is taught in He et al. to comprise from about 0.1-5mg, see paragraph [0033]. The anhydrous dibasic calcium phosphate is present at 69.29 or 34.6% at Table 1. This amount overlaps the weight ratio of 1:2 to 1:90 since the 5mg of varenicline tartarate to 69.29 of anhydrous dibasic calcium is a ratio of 1:13.86. Although He et al. do not teach the weight ratio of acid to varenicline tartarate, He et al. teach that the pH adjusting agents which include one or more weak acids can be optimized to the desired or optimum range, thus He teaches the pH adjusters are an optimizable result effective variable. One of ordinary skill in the art in view of the teachings of He et al. would have been motivated to adjust the concentration of the weak acid including tartaric acid because He et al. teaches tartaric and citric acid or fumaric acid as agents which adjust the pH of the drug environment to the optimum pH range.
He does not teach the selection of the organic acids such as tartaric or the ratio of the varenicline tartarate to acidic and basic compounds with sufficient specificity to anticipate. However, it would have been obvious to select the weak organic acid of tartaric acid as the pH adjuster and to optimize the range in order to provide the optimum pH range of the drug environment. It would have been obvious to provide an overlapping ratio of the basic compound because He expressly teaches an overlapping ratio for dibasic calcium phosphate. Furthermore, generally, differences in concentration will not support the patentability of subject matter encompassed by the prior art unless there is evidence indicating such concentration is critical. "[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." In re Aller, 220 F.2d 454, 456, 105 USPQ 233, 235 (CCPA 1955).
Since this modification of the prior art represents nothing more than “the predictable use of prior art elements according to their established functions” a prima facie case of obviousness exists. See KSR v. Teleflex, 82 USPQ2d 1385, 1396 (2007).
Conclusion
Currently, no claims are allowed and all claims are rejected.
Correspondence
Any inquiry concerning this communication or earlier communications from the examiner should be directed to SARAH ALAWADI whose telephone number is (571)270-7678. The examiner can normally be reached Monday-Friday 10:00am-6:30pm EST.
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/SARAH ALAWADI/Primary Examiner, Art Unit 1619
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