DETAILED ACTION
Continued Examination Under 37 CFR 1.114
A request for continued examination under 37 CFR 1.114, including the fee set forth in 37 CFR 1.17(e), was filed in this application after final rejection. Since this application is eligible for continued examination under 37 CFR 1.114, and the fee set forth in 37 CFR 1.17(e) has been timely paid, the finality of the previous Office action has been withdrawn pursuant to 37 CFR 1.114. Applicant's submission, filed 01/27/2026, has been entered.
Status of Application
Receipt of the amendments to claims and applicant arguments/remarks, filed 01/14/2026 (Response After Final Office Action), is acknowledged.
Claims 1, 6, 8-12 are pending in this application. Claims 2-5, 7, 13 have been cancelled previously. Claims 1, 8, 12 have been amended. Claims 1, 6, 8-12 are currently under consideration.
Any rejection or objection not reiterated in this action is withdrawn. Applicant's amendments necessitated new ground(s) of objection and rejection presented in this office action.
The present application, filed on or after March 16, 2013, is being examined under the first inventor to file provisions of the AIA . 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 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.
Priority
This application, filed January 30, 2021, claims benefit of foreign priority to IN202041004130, filed January 30, 2020 (in English).
Terminal Disclaimer
The terminal disclaimers, filed 10/08/2024, disclaiming the terminal portion of any patent granted on this application, which would extend beyond the expiration date of the prior Patent No. 11,975,011, and any patent granted on pending reference application No. 17/508,238, have been reviewed and are accepted. The terminal disclaimers have been recorded.
Claim Objections
Claim 6 is objected to because of the following informality: Claim 6 comprises the typographic error “in an amount of 6.0% to 7.0%” that needs to be corrected to “in an amount of from 6.0% to 7.0%”. 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 1, 6, 8-12 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.
Claim 1 discloses “A controlled release composition comprising coated minitablet comprising…” and “wherein the total weight of the controlled release compositions is in the range of 595-650 mg)” that is unclear, because the structure of the claimed product (i.e., controlled release composition) is not clearly delineated. As stated previously, the instant specification discloses composition of minitablets with a core and a rate controlling coating (see Abstract; Para. 0001, 0012-0015). Further, the instant specification teaches that total weight of minitablets is in the range of 595-650 (Examples). Therefore, the examiner maintains the position that the structure of the claimed composition/product is not clearly defined. This limitation was interpreted as best understood as “A controlled release composition of coated minitablet comprising…””. Clarification is required.
Claim 1 discloses the property of the disclosed composition (i.e., in vitro dissolution profile) as measured under specific conditions used by the applicant (i.e., pH buffer, temperature, a paddle speed). As stated previously, said property of the disclosed composition/product depends on user’s choice (i.e., pH buffer, temperature, a paddle speed, etc.). Therefore, said claim is not sufficiently definite, because it refers to a variable. MPEP 2173.05. Given that there is no clear-cut indication of the scope of the subject matter covered by the claim, one of ordinary skill in the art would not be reasonably appraised of the scope of the invention. Similar is applied to claim 12. Clarification is required.
Claim 6 (dependent on claim 1) discloses the core minitablet that includes: 80-90 wt% of 5-ASA and 6.5-10 wt% of glyceryl dibehenate (see claim 1) and further include: 6-7 wt% of binders, 0.5-2 wt% of diluents; 1-10 wt% of disintegrants; 1-3.5 wt% of lubricants, 1-3 wt% of glidants; and 6.5-10 wy% of retarding agents (see claim 6). To this point, it is noted that total amount of recited compounds present in the claimed core minitablet is more than 100 wt%. Clarification is required.
Claim 10 and/or 11 (both dependent on claim 1) recite the limitations “seal coating polymer” (claim 10), and/or “seal coated surface” (claim 11). As stated previously, neither the claims nor specification provide a clear definition for said terms. Therefore, one of ordinary skill in the art would not be reasonably appraised of the scope of the invention. Clarification is required.
In response to applicant’s argument that the instant specification recites said terms in Para. 0026 and/or 0030 and teaches the use of any pharmaceutically known conventional seal coat polymers, it is noted that independent claim 1 discloses coated minitablets providing in vitro release profile as claimed (see claim 1). In the present case, it is unclear what seal coat polymers should be used to providing/controlling said claimed property. Clarification is required.
Claim 12 recites numerical limitations “0.5-2%”, “1-3.5%”, “1-3%” without units of measurements (e.g., mol%, wt%, etc.) that is unclear. Therefore, the metes and bounds of the claim cannot be determined. Clarification is required.
Claims 8, 9 are rejected as being dependent on rejected independent claim 1 and failing to cure the defect.
Claim Rejections - 35 USC § 103 - MAINTAINED
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.
Claims 1, 6, 8-12 are rejected under 35 U.S.C. 103 as being unpatentable over Bowe et al., US 2015/0056275 (hereinafter referred to as Bowe), Otterbeck, US 2013/0189356; Shukla et al., US 2009/0169622 (hereinafter referred to as Shukla), in view of Valducci et al., WO 2017/125856A1 (hereinafter referred to as Valducci).
Bowe teaches controlled-release solid dosage forms of mesalamine (also known as 5-aminosalicylic acid and/or 5-ASA) for treatment of inflammatory bowel disease, wherein said dosage forms comprise a plurality of coated mini-tablets having a diameter of 2-5 mm (Claim 7; Abstract; Para. 0005-0007 as applied to claims 1, 12), and wherein said mini-tablets may include:
(a) a core comprising mesalamine (5-ASA; e.g., in an amount of 80 wt%) in combination with pharmaceutically acceptable carrier that may include a diluent, a binder, a lubricant, a plasticizer, a filler, etc., and specifically teaches the use of (Para. 0008-0009, 0011, 0014-0017; 0030, 0055, 0071-0072, 0081, 0092-0099 as applied to claim 1, 6, 8): (i) glyceryl behenate, magnesium stearate, polyethylene glycol, e.g., having molecular weight of 100-10,000 Da, or 750 Da (i.e., a lubricant); etc. and a mixture thereof; (ii) ethyl cellulose, calcium stearate, stearic acid (i.e., a retarding agent); (iii) colloidal silicone dioxide, talc (i.e., a glidant); (iv) polyvinylpyrrolidone, hydroxypropyl cellulose, acacia, hydroxypropyl methylcellulose/hypromellose (i.e., a binder); (v) lactose, lactose monohydrate, starches, microcrystalline cellulose, mannitol (i.e., a diluent); (vi) crospovidone (i.e., a disintegrant);
(b) an outer coating comprising ethyl cellulose (i.e., hydrophobic cellulose) and hydroxypropyl methylcellulose (i.e., a hydrophilic polymer), wherein the coating comprises 1-6 wt% of said mini-tablet (Para. 0008, 0012, 0032, 0074, 0101, 0106-0107 as applied to claims 1, 9);
(c) an optional coating (Para. 0008, 0009, 0074, 0104 as applied to claim 10, 11).
Bowe teaches that said coated mini-tablets may include 80-90 wt% of mesalamine/5-ASA by weight of the mini-tablet core (Para. 0112-0113), and further teaches that coated mini-tablets can be aggregated together to provide dosage forms/compositions of 1-2000 mg of active agent (Claim 14; Para. 0068 as applied to claim 1).
Bowe teaches that the core of said mini-tablets may include (based on the weight of the core): 10-40 wt% of a diluent (Para. 0203-0206); 1-10 wt % of a binder (Para. 0207-0209); 0.5-5 wt % of a lubricant (Para. 0210-0213 as applied to claim 6).
Bowe provides examples of using in the outer coating ethyl cellulose (i.e., a hydrophobic cellulose) and hydroxypropyl methylcellulose (i.e., a hydrophilic polymer) at a weight ratio of 0.66 (Para. 0413, 0414), and/or of using ethyl cellulose in an amount of about 1% (Para. 0404 as applied to claims 1, 9).
Bowe teaches a process of manufacturing said coated mini-tablets comprising (i) mixing or granulating a mixture of active pharmaceutical agent and optional excipients; (ii) drying the mixture to a residual amount of water of 0-5% and passing dry granules through mesh screen of size #20-#75; (iii) directly compressing said mixture into mini-tablets; (iv) coating the mini-tablets with an optional undercoat composition comprising a water-soluble polymer; and further (v) coating the mini-tablets with a top-coat with a top-coat composition comprising a polymer that modifies release of the active pharmaceutical agent (Para. 0007; 0069-0073 as applied to claim 12).
Otterbeck teaches oral controlled release compositions suitable for the treatment of the intestinal tract (e.g., inflammatory intestinal disorders), wherein said compositions comprise pellets that include (i) a core comprising 5-aminosalicylic acid (5-ASA), a salt or a derivative thereof as an active agent and 1-21 wt% of a matrix forming polymer(s) by the weight of the core; (ii) an enteric coating that may include ethyl cellulose (i.e., hydrophobic cellulose) and hydroxypropyl methylcellulose (i.e., hydrophilic polymer) (Claim 1; Abstract; Para. 0021-0024, 0027-0028; 0049); and (iii) also may include additional coatings (Para. 0031). Otterbeck further teaches that the core may include polyvinylpyrrolidone, microcrystalline cellulose, silica, corn starch, magnesium stearate, lactose, polyethylene glycol, talc, etc. (Para. 0033), and wherein said pellets have a size of 0.1-3 mm (Claims 7, 13; Para. 0037). Otterbeck teaches that said approach allows lowering active compound concentrations in the blood with a simultaneously higher concentration of the active compounds in the intestine, as a result of which the side effect potentially caused by the systemically available active compound or its metabolites, is markedly reduced (Para. 0038, 0039).
Shukla teaches delayed release compositions for the treatment of colonic disorders and diseases, wherein said compositions can be in a form of tablet and include (i) a core comprising 50-80 wt% of 5-ASA/mesalamine in combination with pharmaceutically acceptable adjuvants, disintegrants, binders, glidants, lubricants and/or diluents; and (ii) a coating comprising a mixture of ethyl cellulose/hydrophobic polymer and hydroxypropyl methylcellulose/hydrophilic polymer present at a ratio of from 1:0.67 to 1:5.7 (Abstract; Para. 0003, 0004, 0030-0032). To this point, Shukla teaches that the core may include: (i) starch, lactose, calcium phosphate, stearic acid (i.e., diluent; Para. 0023); (ii) polyvinyl pyrrolidine, starch (i.e., binder; Para. 0023, 0024); (iii) crospovidone, sodium starch glycolate, croscarmellose sodium (i.e., disintegrant; Para. 0023); (iv) magnesium stearate, stearic acid, polyethylene glycol, glyceryl behenate (i.e., lubricant; Para. 0023, 0024); (v) silicon dioxide, talc (i.e., glidant; Para. 0024); (vi) ethyl cellulose, calcium stearate, stearic acid, (i.e., retarding agent; Para. 0023, 0024), and (v) may include additional coating layers (Para. 0027-0029).
Though the cited prior art teaches the use of glyceryl behenate as a constituent of the core, said prior art does not teach the use of glyceryl dibehenate (claim 1).
Valducci teaches modified-release high-dosage tablets for treating inflammation in the colon, wherein said tablets consist of a core containing 5-ASA/mesalamine and at least one gastro-resistant coating (Abstract; Page 1). Valducci teaches that the core may include lubricants, e.g., glycerol dibehenate, magnesium stearate, stearic acid, sodium stearyl fumarate; glidants, e.g., colloidal anhydrous silica; binders, e.g., polyvinylpyrrolidone, hydroxypropyl cellulose, and other additives (Claim 2; Pages 3-4). Valducci further teaches the use of the coating that present in an amount of 5-15 wt% of the total weight of the tablet and consists of polymers having pH-dependent features leading to a release of the active ingredient only when the tablet reaches high pH values, i.e. in the colon, e.g., polymers having carboxylic groups, which in acidic environment are hydrogenated and devoid of charge (thus insoluble), but which become soluble when they lose the hydrogen in basic environment, due to the appearance of a negative charge, and also teaches that said polymers are present in a weight ratios in the range of from 1:0.5 to 1:19 (Page 4). Further, Valducci teaches that said tablets may include 500-2000 mg of 5-ASA/mesalamine, i.e., in an amount of 75-96 wt% by weight of the core (Page 3), and/or 70-95% by the total weight of the tablet (Claim 3; Page 3), and wherein said tablets begin to melt once they reach the colon (Page 6).
Therefore, it is the examiner’s position that the claimed invention, as a whole, would have been prima facie obvious to one of ordinary skill in the art at the time the invention was made, because every element of the invention has been collectively taught by the combined teachings of the references. It would have been obvious to one of ordinary skill in the art before the effective filing date of the claimed invention to try such excipient as glyceryl dibehenate as taught by Valducci preparing tablets as taught by Bowe, Otterbeck and Shukla, because it is prima facie obvious to combine compositions each of which is taught by the prior art to be useful for the same purpose, in order to form a new composition to be used for the very same purpose, i.e., delivering of the claimed active agent to the colon. MPEP 2144.06.
With regard to the concentrations/ratios as instantly claimed, it is noted that differences in experimental parameters such as concentration of compounds in a composition will not support the patentability of subject matter encompassed by the prior art unless there is evidence indicating such parameter is critical. The prior art teaches formulations comprising the same components/compounds. The determination of suitable or effective concentration/composition can be determined by one of ordinary skill in the art through the use of routine or manipulative experimentation to obtain optimal results, as these are variable parameters attainable within the art. Where 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.
Regarding the claimed properties of the disclosed compositions (i.e., in vitro dissolution profiles recited in claims 1, 12), it is noted that the cited prior art teaches the compositions that are substantially the same as the compositions recited by the instant claims. Thus, it is expected that since the prior art is comprised of the same components, the same beneficial properties and effects would also be provided. Further, it is noted that the fact that applicant has recognized another advantage, which would flow naturally from following the suggestion of the prior art cannot be the basis for patentability when the differences would otherwise be obvious. Ex parte Obiaya, 227 USPQ 58, 60 (Bd. Pat. App. & Inter. 1985).
Regarding claim 12, it is noted that in product-by-process claims, “once a product appearing to be substantially identical is found and a 35 U.S.C. 103 rejection is made, the burden shifts to the applicant to show an unobvious difference.” MPEP 2113. This rejection under 35 U.S.C. 103 is proper because the “patentability of a product does not depend on its method of production.” In re Thorpe, 227 USPQ 964, 966 (Fed. Cir. 1985). As a practical matter, the Patent Office is not equipped to manufacture products by the myriad number of processes put before it and then obtain prior art products and make physical comparisons therewith.” In re Brown, 459 F.2d 531, 535, 173 USPQ 685, 688 (CCPA 1972). Therefore, with the showing of the reference, the burden of establishing non-obviousness by objective evidence is shifted to the applicants.
Pertinent Prior Art
The prior art made of record and not relied upon is considered pertinent to applicant's disclosure:
US 2019/0105275 - teaches delayed-immediate release compositions/minitablets having a diameter of 1-4 mm and comprising a core comprising at least 85 wt% of 5-ASA (e.g., 0.4-6 g per unit dosage product) and excipients as instantly claimed and a coating comprising ethyl cellulose (i.e., hydrophobic cellulose) and hydroxypropyl methylcellulose (i.e., a hydrophilic polymer).
US 2020/0155461 – teaches controlled release (here as delayed-immediate release) compositions/minitablets having a diameter of 1-4 mm and comprising a core comprising at least 85 wt% of 5-ASA (e.g., 0.4-6 g per unit dosage product) in combination with excipients as instantly claimed and a coating comprising ethyl cellulose (i.e., hydrophobic cellulose) and hydroxypropyl methylcellulose (i.e., a hydrophilic polymer).
US 2014/0141075 A1 - teaches tablets within a capsule, wherein said tablets comprise a core comprising 5-ASA (50-1,800 mg) in combination with excipients as instantly claimed and a coating comprising ethyl cellulose (i.e., hydrophobic cellulose) and hydroxypropyl methylcellulose (i.e., a hydrophilic polymer), and providing controlled, pH-dependent drug-release profile.
Foppoli et al., (cited previously) – teaches tablets comprising 5-ASA, povidone and crospovidone, glyceryl dibehenate, lactose, hydroxypropyl methylcellulose, polyethylene glycol (PEG 6000), and talc.
US 2022/0047515 - teaches controlled release compositions/minitablets comprising a core comprising mesalazine/5-ASA in combination with excipients as instantly claimed and a coating comprising ethyl cellulose (i.e., hydrophobic cellulose).
Response to Arguments
Applicant's arguments, filed 01/14/2026, have been fully considered, but they were not found to be persuasive for the reasons set forth above. New objections and/or rejections have been added to the record to address newly introduced amendments and/or to clarify the position of the examiner. Additional examiner’s comments are set forth next.
In response to applicant's arguments against the references individually, the examiner maintains the position that one cannot show nonobviousness by attacking references individually where the rejections are based on combinations of references. In re Keller, 642 F.2d 413, 208 USPQ 871 (CCPA 1981); In re Merck & Co., 800 F.2d 1091, 231 USPQ 375 (Fed. Cir. 1986). As state previously (see Non-Final Office Action, filed 05/05/2025), the test for obviousness is not that the claimed invention must be expressly suggested in any one or all of the references. Rather, the test is what the combined teachings of the references would have suggested to those of ordinary skill in the art. See In re Keller, 642 F.2d 413, 208 USPQ 871 (CCPA 1981). The reason or motivation to modify the reference may often suggest what the inventor has done, but for a different purpose or to solve a different problem. It is not necessary that the prior art suggest the combination to achieve the same advantage or result discovered by applicant. Cross Med. Prods., Inc. v. Medtronic Sofamor Danek, Inc., 424 F.3d 1293, 1323, 76 USPQ2d 1662, 1685 (Fed. Cir. 2005) (“One of ordinary skill in the art need not see the identical problem addressed in a prior art reference to be motivated to apply its teachings.”); In re Linter, 458 F.2d 1013, 173 USPQ 560 (CCPA 1972); In re Dillon, 919 F.2d 688, 16 USPQ2d 1897 (Fed. Cir. 1990), cert. denied, 500 U.S. 904 (1991). Further, it has been held that a prior art reference must either be in the field of applicant’s endeavor or, if not, then be reasonably pertinent to the particular problem with which the applicant was concerned, in order to be relied upon as a basis for rejection of the claimed invention. In re Oetiker, 977 F.2d 1443, 24 USPQ2d 1443 (Fed. Cir. 1992).
In the present case, all cited references are reasonably drawn to the same field of endeavor that is controlled release minitablets/tablets comprising mesalamine/5-ASA as the active agent in combination with other compounds as instantly claimed, wherein said minitablets/tablets are coated with coating(s) comprising compounds as instantly claimed for providing desired/controllable dissolution and/or drug release profile. Therefore, the examiner maintains the positions that the claimed invention, as a whole, would have been prima facie obvious to one of ordinary skill in the art at the time the invention was made, because every element of the invention has been collectively taught by the combined teachings of the references. To this point, it is noted that the Supreme Court decided (KSR International Co. v. Teleflex Inc., 550 U.S. 398 (2007)) that: (i) The obviousness analysis needs not seek out precise teachings directed to the subject matter of the challenged claim and can take into account the inferences and creative steps that one of ordinary skill in the art would employ; (ii) The obviousness analysis cannot be confined by a formalistic conception of the words teaching, suggestion and motivation, or by overemphasis on the importance of published articles and the explicit content of issued patents; (iii) It is error to look only the problem the patentee was trying to solve. Any need or problem known in the field of endeavor at the time of invention and addressed by the prior art can provide a reason for combining the elements in the manner claimed; (iv) It is error to assume that one of ordinary skill in the art in attempting to solve a problem will be led only to those elements of prior art designed to solve the same problem. Common sense teaches that familiar items may have obvious uses beyond their primary purposes, and in many cases one of ordinary skill in the art will be able to fit the teachings of multiple patents together like pieces of a puzzle (one of ordinary skill in the art is not automaton); (v) It is error to assume that a patent claim cannot be proved obvious merely by showing that the combination of elements was “obvious to try”.
In response to applicant’s argument regarding the concentrations and/or ratios as instantly claimed, as stated previously, one skilled in the art would have understood that properties of multicomponent systems depend on compounds included as well as on concentrations and/or distributions of said compounds that define the network of intermolecular interactions, and thereby physical and chemical properties of the system/composition. Therefore, it is expected that different compositions might have different properties. The determination of suitable or effective concentrations/ratios (for providing/controlling properties of compositions) can be and usually is determined by one of ordinary skill in the art through the use of routine or manipulative experimentation to obtain optimal/desired results, as these are variable parameters attainable within the art. Where 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. Regarding the dissolution profiles as instantly claimed, it is noted that since the prior art is comprised of the same components it is expected that the same beneficial properties and effects would also be provided. Further, it is noted that the fact that applicant has recognized another advantage, which would flow naturally from following the suggestion of the prior art cannot be the basis for patentability when the differences would otherwise be obvious. Ex parte Obiaya, 227 USPQ 58, 60 (Bd. Pat. App. & Inter. 1985). Applicant is advised to clarify the claim language, the structure of the claimed compositions/minitablets and clearly point out the patentable novelty, which the applicant thinks the claims present in view of the state of the art disclosed by the references cited, to place the application in condition for allowance.
Conclusion
No claim is allowed at this time.
Any inquiry concerning this communication or earlier communications from the examiner should be directed to OLGA V. TCHERKASSKAYA whose telephone number is (571)270-3672. The examiner can normally be reached 9 am - 6 pm, Monday - Friday.
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/OLGA V. TCHERKASSKAYA/
Examiner, Art Unit 1615
/Robert A Wax/Supervisory Patent Examiner, Art Unit 1615