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 Status
New claims 39-47 are pending.
Claims 1-38 are cancelled.
Claims 43-47 which are drawn to the free base of compound I are presently withdrawn in view of the species election to the hemifumarate salt in the reply filed on 07/18/2025. Claims 43-47 are withdrawn from further consideration pursuant to 37 CFR 1.142(b) as being drawn to a nonelected invention, there being no allowable generic or linking claim. Election was made without traverse in the reply filed on 07/18/2025.
Examiner notes that should the claims become eligible for rejoinder they may raise potential 112b issues because free base equivalent is in parenthesis. Secondly, claim 43 should be dependent from claim 39 and not claim 42 because claim 42 is the salt form of hemifumarate and not free base.
Claims 39-42 are under current examination directed to the hemifumarate form of compound I.
Applicants' arguments (and amendments and/or declaration), filed 02/12/2026, have been fully considered. Rejections and/or objections not reiterated from previous office actions are hereby withdrawn. The following rejections and/or objections are either reiterated or newly applied. They constitute the complete set presently being applied to the instant application.
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.
Claims 39-42 are rejected under 35 U.S.C. 103 as being unpatentable over Demorin et al. ( WO2020123800-published 6/18/2020-see IDS filed 7/18/2025) in view of Apolo (WO2018064191).
Demorin et al. teach Compound 1 hemifumarate of structure
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(meeting the elected species to hemifumarate), including form B, see paragraph [0011]. The compound I hemifumarate form can comprise a pharmaceutical composition, see paragraphs [0328]-[0329]. The hemifumarate can comprise Form B, see paragraph [00011]. The pharmaceutical composition can comprise excipients including cellulose derivatives as binders and croscarmellose sodium as a disintegrant, see paragraph [0046]. Microcrystalline cellulose and lactose can be present, see paragraphs [00476] and [00479]. The compound I can be present from 1-99% by weight or preferably from 5-75% by weight with the rest being excipients, see paragraph [00482]. The pharmaceutical composition of Demorin can be prepared with coatings, see paragraph [00477]. Suitable excipients include fillers, diluent, lubricants, disintegrants, binders, and wetting agents, see paragraphs [0096] and [0476]. The composition can be in the form of a tablet or capsule. The compound I salt form which includes hemifumarate can be present from 5-75% by weight.
Demorin does not expressly teach the amount of the croscarmellose sodium present, the presence and amount of silicon dioxide, the presence and amount of hydroxypropylcellulose, the amount of microcrystalline cellulose and lactose, and the presence and amount of steric acid lubricant (elected species for excipients).
However, Apolo teaches treating cancer with the kinase inhibitor carbozantinib wherein the pharmaceutical formulation includes tablets comprising at paragraph [0088]:
28-38 percent by weight of carbozantinib (kinase inhibitor) or a pharmaceutically acceptable salt thereof (based on 100% or 100mg this would encompass 28-38mg);
37- 39 percent by weight or microcrystalline cellulose (based on 100% this would encompass 37-39mg); (filler/diluent paragraph [0041] [0083]-[0085].) In another embodiment the microcrystalline cellulose can comprise 30-80% weight (equivalent to 30-80mg), see paragraphs [0072]-[0077].
18 to 20 percent by weight of lactose anhydrous (18-20mg for 100% weight); (filler paragraph [0041] and [0083]-[0085].)
1.5-4.5 percent by weight of hydroxypropyl cellulose (equivalent to 1.5-4.5mg) (binder see paragraphs [0043]-[0044]);
3-9 percent by weight a croscarmellose sodium (equivalent to 3-9mg) (disintegrant see paragraphs [0045]-[0046];
0.1-0.8 percent by weight (0.1-0.8 mg) of colloidal silicon dioxide (glidant see paragraphs [0047]-[0048]; and
0.5-1 percent (equivalent to 0.5-1mg) by weight of magnesium stearate. Stearic acid is taught to be an alternative lubricant to magnesium stearate, see paragraphs ]0049]-[0050]. Fillers are taught to be inert ingredients which adjust the bulk to produce a size for compression , see paragraph [0041]. Binders are added to powders to impart cohesive qualities which allow the compressed tablet to retain its integrity, see paragraph [0043]. A disintegrant is a substance or a mixture of substances added to facilitate breakup or disintegrate after administration, see paragraph [0045]. Glidant is added to contribute to compressibility, improve flowability and homogeneity of the formulation and to minimize segregation, see paragraph [0047]. The pharmaceutical composition can comprise a film coating including Opadry® for tablets. In one embodiment the film coating can comprise 3.9-4.1% by weight (equivalent to 3.9-4.1mg when total weight is 100mg or 100%).
It would have been prima facie obvious to provide the cellulose derivative of Demorin as a hydroxypropyl cellulose binder present from 18-20% by weight, the croscarmellose sodium disintegrant of Demorin from 3-9% by weight, and to further include microcrystalline cellulose present from 37-39% by weight with lactose present from 18-20% as fillers, 0.1-0.8% of colloidal silicon dioxide glidant and from 0.5-1% stearic acid lubricant.
One of ordinary skill in the art would have been motivate to do so as Apolo teaches such excipients as being advantageous for adjusting the size of the dosage formulation for compression, for facilitating break up of tablets, imparting cohesive qualities, improved flowability and for optionally film coating tablets with Opadry.
There would have been a reasonable expectation of success because both Apolo and Demorin teach kinase inhibitor formulations which further comprise excipients. The excipients of Demorin can be added in a total amount from 1-95% by weight and Demorin’s pharmaceutical formulation is taught to include croscarmellose sodium as a disintegrant and cellulose derivative binders.
In regards to the amount of microcrystalline cellulose filler and lactose filler, hydroxypropyl cellulose binder, croscarmellose sodium, colloidal silicon dioxide and magnesium stearate, Apolo teaches overlapping ranges. With regards to the amount of compound I present, Demorin teaches overlapping ranges as the compound can be present from 1-99% by weight. From MPEP 2144.05, 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).
Response to remarks regarding 103 rejections
Applicants argue that Apollo refers to a different compounds and that a person of ordinary skill in the art would not be motived to modify Demorin formulations. Applicants argue that one of ordinary skill in the art would not have simply utilize excipients suitable for one compound to formulate a different compound with a reasonable expectation of success.
Examiner respectfully submits that both Apollo and Demorin are directed to kinase inhibitors with structural similarity. One of ordinary skill would have utilized the excipients of Apollo because Apollo teaches their use for formulations which do contain kinase inhibitors. The test for obviousness is not whether the features of a secondary reference may be bodily incorporated into the structure of the primary reference; nor is it 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).
Applicants further argue that Apolo discloses magnesium stearate but the Applicant’s claimed composition is to stearic acid because magnesium stearate can cause sticking. Stearic acid causes improved manufacturing robustness and production efficiency. (paragraph 0344 of instant specification).
Examiner respectfully submits that Apolo clearly exemplifies stearic acid in the alternative to magnesium stearate as a lubricant, see paragraphs [0049] and [0072]-[0077] and teaches that the lubricant provides aid in the flow of the powder. Thus, Apolo is not limited to magnesium stearate. Furthermore, paragraph [0344] of the instant specification discloses that the hydroxypropyl cellulose concentration was increased to 5% weight along with the use of stearic acid in order to prevent sticking thus the property of improved production efficiency is not solely the use of stearic acid in the alternative to magnesium stearate.
Applicants argue that the claimed composition exhibits high stability and dissolution performance as can be shown at paragraph [0350]. The stability and dissolution properties were not predictable from the cited art.
Examiner respectfully submits that Demorin expressly teaches that hemifumarate form of compound 1 is physically stable over 15 days, see paragraphs [00434] and [00446]. The compound of formula I did not show signs of decomposition, see paragraph [00405] of Demorin. Furthermore, the instant specification coats the hemifumarate compound I with Opadry which exhibited less than 0.5% decomposition at paragraph [0350] and Table 6. Whether the unexpected results are the result of unexpectedly improved results or a property not taught by the prior art, the "objective evidence of nonobviousness must be commensurate in scope with the claims which the evidence is offered to support." In other words, the showing of unexpected results must be reviewed to see if the results occur over the entire claimed range. In re Clemens, 622 F.2d 1029, 1036, 206 USPQ 289, 296 (CCPA 1980). The instant claims do not require Opadry blue coatings. Nevertheless, Decorin does teach that the composition can be prepared with coatings that are well known in the art, see paragraph [0477].
Double Patenting
The nonstatutory double patenting rejection is based on a judicially created doctrine grounded in public policy (a policy reflected in the statute) so as to prevent the unjustified or improper timewise extension of the “right to exclude” granted by a patent and to prevent possible harassment by multiple assignees. A nonstatutory double patenting rejection is appropriate where the conflicting claims are not identical, but at least one examined application claim is not patentably distinct from the reference claim(s) because the examined application claim is either anticipated by, or would have been obvious over, the reference claim(s). See, e.g., In re Berg, 140 F.3d 1428, 46 USPQ2d 1226 (Fed. Cir. 1998); In re Goodman, 11 F.3d 1046, 29 USPQ2d 2010 (Fed. Cir. 1993); In re Longi, 759 F.2d 887, 225 USPQ 645 (Fed. Cir. 1985); In re Van Ornum, 686 F.2d 937, 214 USPQ 761 (CCPA 1982); In re Vogel, 422 F.2d 438, 164 USPQ 619 (CCPA 1970); In re Thorington, 418 F.2d 528, 163 USPQ 644 (CCPA 1969).
A timely filed terminal disclaimer in compliance with 37 CFR 1.321(c) or 1.321(d) may be used to overcome an actual or provisional rejection based on nonstatutory double patenting provided the reference application or patent either is shown to be commonly owned with the examined application, or claims an invention made as a result of activities undertaken within the scope of a joint research agreement. See MPEP § 717.02 for applications subject to examination under the first inventor to file provisions of the AIA as explained in MPEP § 2159. See MPEP § 2146 et seq. for applications not subject to examination under the first inventor to file provisions of the AIA . A terminal disclaimer must be signed in compliance with 37 CFR 1.321(b).
The filing of a terminal disclaimer by itself is not a complete reply to a nonstatutory double patenting (NSDP) rejection. A complete reply requires that the terminal disclaimer be accompanied by a reply requesting reconsideration of the prior Office action. Even where the NSDP rejection is provisional the reply must be complete. See MPEP § 804, subsection I.B.1. For a reply to a non-final Office action, see 37 CFR 1.111(a). For a reply to final Office action, see 37 CFR 1.113(c). A request for reconsideration while not provided for in 37 CFR 1.113(c) may be filed after final for consideration. See MPEP §§ 706.07(e) and 714.13.
The USPTO Internet website contains terminal disclaimer forms which may be used. Please visit www.uspto.gov/patent/patents-forms. The actual filing date of the application in which the form is filed determines what form (e.g., PTO/SB/25, PTO/SB/26, PTO/AIA /25, or PTO/AIA /26) should be used. A web-based eTerminal Disclaimer may be filled out completely online using web-screens. An eTerminal Disclaimer that meets all requirements is auto-processed and approved immediately upon submission. For more information about eTerminal Disclaimers, refer to www.uspto.gov/patents/apply/applying-online/eterminal-disclaimer.
Claims 39-42 are rejected on the ground of nonstatutory double patenting as being unpatentable over claims 1-2 of U.S. Patent No. 12017995 in view of Apolo (WO2018064191).
Claims 1-3, 5, 24,33-38 are directed to an invention not patentably distinct from claims 1-2 of commonly assigned U.S. Patent No. 12017995.
Both the instant claims and that of Patent ‘995 claim Compound I which is inclusive of hemifumarate (salt versions). The claims of Patent ‘995 can include an excipient as it is part of a pharmaceutical composition. The broader teaching of hemifumarate in the claims of Patent ‘995 is suggested as inclusive of form B from the disclosure (column 11, line 50(. Patent ‘995 does not recite the presence of the diluent, binder, disintegrants, glidants, lubricants and film coating comprising silicon dioxide glidant, hydroxypropyl cellulose binder, croscarmellose sodium disintegrant, microcrystalline cellulose and lactose as the diluents, stearic acid lubricant, Opadry for film coating. The hemifumarate salt is form B.
Apolo teaches treating cancer with the kinase inhibitor carbozantinib wherein the pharmaceutical formulation includes tablets comprising at paragraph [0088]:
28-38 percent by weight of carbozantinib (kinase inhibitor) or a pharmaceutically acceptable salt thereof (based on 100% or 100mg this would encompass 28-38mg);
37- 39 percent by weight or microcrystalline cellulose (based on 100% this would encompass 37-39mg); (filler/diluent paragraph [0041] [0083]-[0085].) In another embodiment the microcrystalline cellulose can comprise 30-80% weight (equivalent to 30-80mg), see paragraphs [0072]-[0077].
18 to 20 percent by weight of lactose anhydrous (18-20mg for 100% weight); (filler paragraph [0041] and [0083]-[0085].)
1.5-4.5 percent by weight of hydroxypropyl cellulose (equivalent to 1.5-4.5mg) (binder see paragraphs [0043]-[0044]);
3-9 percent by weight a croscarmellose sodium (equivalent to 3-9mg) (disintegrant see paragraphs [0045]-[0046];
0.1-0.8 percent by weight (0.1-0.8 mg) of colloidal silicon dioxide (glidant see paragraphs [0047]-[0048]; and
0.5-1 percent (equivalent to 0.5-1mg) by weight of magnesium stearate. Stearic acid is taught to be an alternative lubricant to magnesium stearate, see paragraphs ]0049]-[0050]. Fillers are taught to be inert ingredients which adjust the bulk to produce a size for compression , see paragraph [0041]. Binders are added to powders to impart cohesive qualities which allow the compressed tablet to retain its integrity, see paragraph [0043]. A disintegrant is a substance or a mixture of substances added to facilitate breakup or disintegrate after administration, see paragraph [0045]. Glidant is added to contribute to compressibility, improve flowability and homogeneity of the formulation and to minimize segregation, see paragraph [0047]. The pharmaceutical composition can comprise a film coating including Opadry® for tablets. In one embodiment the film coating can comprise 3.9-4.1% by weight (equivalent to 3.9-4.1mg when total weight is 100mg or 100%).
It would have been obvious to provide a cellulose derivative of as a hydroxypropyl cellulose binder present from 18-20% by weight, the croscarmellose sodium disintegrant from 3-9% by weight, and to further include microcrystalline cellulose present from 37-39% by weight with lactose present from 18-20% as fillers, 0.1-0.8% of colloidal silicon dioxide glidant and from 0.5-1% stearic acid lubricant with film coating as the pharmaceutical composition of Patent ‘995.
One of ordinary skill in the art would have been motivate to do so as Apolo teaches such excipients as being advantageous for adjusting the size of the dosage formulation for compression, for facilitating break up of tablets, imparting cohesive qualities, improved flowability and for optionally film coating tablets with Opadry.
There would have been a reasonable expectation of success Patent ‘995 can comprise further excipients with the kinase inhibitor.
In regards to the amount of microcrystalline cellulose filler and lactose filler, hydroxypropyl cellulose binder, croscarmellose sodium, colloidal silicon dioxide and magnesium stearate, Apolo teaches overlapping ranges and per MPEP 2144.05, 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). It would have been well within the purview of an ordinary skilled artisan to adjust the concentration of each excipient. In regards to the amount of compound 1, since Apolo teaches that the kinase inhibitor is present in an amount of from 28-38, it would have been obvious to provide the kinase inhibitor of Patent ‘995 in amounts suggested by Apolo for the kinase inhibitor being present.
The U.S. Patent and Trademark Office may not institute a derivation proceeding in the absence of a timely filed petition. The USPTO normally will not institute a derivation proceeding between applications or a patent and an application having common ownership (see 37 CFR 42.411). Commonly assigned Patent No. 12017995 discussed above, may form the basis for a rejection of the noted claims under 35 U.S.C. 102 or 103 if the commonly assigned case qualifies as prior art under 35 U.S.C. 102(a)(2) and the patentably indistinct inventions were not commonly owned or deemed to be commonly owned not later than the effective filing date under 35 U.S.C. 100(i) of the claimed invention.
In order for the examiner to resolve this issue the applicant or patent owner can provide a statement under 35 U.S.C. 102(b)(2)(C) and 37 CFR 1.104(c)(4)(i) to the effect that the subject matter and the claimed invention, not later than the effective filing date of the claimed invention, were owned by the same person or subject to an obligation of assignment to the same person. Alternatively, the applicant or patent owner can provide a statement under 35 U.S.C. 102(c) and 37 CFR 1.104(c)(4)(ii) to the effect that the subject matter was developed and the claimed invention was made by or on behalf of one or more parties to a joint research agreement that was in effect on or before the effective filing date of the claimed invention, and the claimed invention was made as a result of activities undertaken within the scope of the joint research agreement; the application must also be amended to disclose the names of the parties to the joint research agreement.
A showing that the inventions were commonly owned or deemed to be commonly owned not later than the effective filing date under 35 U.S.C. 100(i) of the claimed invention will preclude a rejection under 35 U.S.C. 102 or 103 based upon the commonly assigned case. Alternatively, applicant may take action to amend or cancel claims such that the applications, or the patent and the application, no longer contain claims directed to patentably indistinct inventions.
Claims 39-42 are rejected on the ground of nonstatutory double patenting as being unpatentable over claims 1-2 of U.S. Patent No. 11542259 in view of Demorin et al. ( WO2020123800-published 6/18/2020-see IDS filed 7/18/2025) and Apolo (WO2018064191).
Claims 1-3, 5, 24,33-38 are directed to an invention not patentably distinct from claims 1-2 of commonly assigned U.S. Patent No. 11542259.
Both the instant claims and that of Patent ‘259 claim Compound I which is inclusive of salts. Patent ‘259 does not recite the presence of the hemifumarate form B or a diluent, binder, disintegrants, glidants, lubricants and film coating comprising silicon dioxide glidant, hydroxypropyl cellulose binder, croscarmellose sodium disintegrant, microcrystalline cellulose and lactose as the diluents, stearic acid lubricant, Opadry for film coating.
However, Demorin et al. teach Compound 1 hemifumarate Form B of structure
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(meeting the elected species to hemifumarate), see paragraph [0011]. The compound I hemifumarate form can comprise a pharmaceutical composition, see paragraphs [0328]-[0329]. The pharmaceutical composition can comprise excipients including cellulose derivatives as binders and croscarmellose sodium as a disintegrant, see paragraph [0046]. Microcrystalline cellulose and lactose can be present, see paragraphs [00476] and [00479]. The compound I can be present from 1-99% by weight or preferably from 5-75% by weight with the rest being excipients, see paragraph [00482]. The pharmaceutical composition of Demorin can be prepared with coatings, see paragraph [00477]. Suitable excipients include fillers, diluent, lubricants, disintegrants, binders, and wetting agents, see paragraphs [0096] and [0476]. The composition can be in the form of a tablet or capsule.
presence and amount of steric acid lubricant (elected species for excipients). The hemifumarate can comprise Form B, see paragraph [00011].
Apolo teaches treating cancer with the kinase inhibitor carbozantinib wherein the pharmaceutical formulation includes tablets comprising at paragraph [0088]:
28-38 percent by weight of carbozantinib (kinase inhibitor) or a pharmaceutically acceptable salt thereof (based on 100% or 100mg this would encompass 28-38mg);
37- 39 percent by weight or microcrystalline cellulose (based on 100% this would encompass 37-39mg); (filler/diluent paragraph [0041] [0083]-[0085].) In another embodiment the microcrystalline cellulose can comprise 30-80% weight (equivalent to 30-80mg), see paragraphs [0072]-[0077].
18 to 20 percent by weight of lactose anhydrous (18-20mg for 100% weight); (filler paragraph [0041] and [0083]-[0085].)
1.5-4.5 percent by weight of hydroxypropyl cellulose (equivalent to 1.5-4.5mg) (binder see paragraphs [0043]-[0044]);
3-9 percent by weight a croscarmellose sodium (equivalent to 3-9mg) (disintegrant see paragraphs [0045]-[0046];
0.1-0.8 percent by weight (0.1-0.8 mg) of colloidal silicon dioxide (glidant see paragraphs [0047]-[0048]; and
0.5-1 percent (equivalent to 0.5-1mg) by weight of magnesium stearate. Stearic acid is taught to be an alternative lubricant to magnesium stearate, see paragraphs ]0049]-[0050]. Fillers are taught to be inert ingredients which adjust the bulk to produce a size for compression , see paragraph [0041]. Binders are added to powders to impart cohesive qualities which allow the compressed tablet to retain its integrity, see paragraph [0043]. A disintegrant is a substance or a mixture of substances added to facilitate breakup or disintegrate after administration, see paragraph [0045]. Glidant is added to contribute to compressibility, improve flowability and homogeneity of the formulation and to minimize segregation, see paragraph [0047]. The pharmaceutical composition can comprise a film coating including Opadry® for tablets. In one embodiment the film coating can comprise 3.9-4.1% by weight (equivalent to 3.9-4.1mg when total weight is 100mg or 100%).
It would have been obvious to provide the compound of Patent ‘259 as a hemifumarate B form with a cellulose derivative of as a hydroxypropyl cellulose binder present from 18-20% by weight, the croscarmellose sodium disintegrant from 3-9% by weight, and to further include microcrystalline cellulose present from 37-39% by weight with lactose present from 18-20% as fillers, 0.1-0.8% of colloidal silicon dioxide glidant and from 0.5-1% stearic acid lubricant with film coating as the pharmaceutical composition of Patent ‘259.
One of ordinary skill in the art would have been motivate to do so as Apolo teaches such excipients as being advantageous for adjusting the size of the dosage formulation for compression, for facilitating break up of tablets, imparting cohesive qualities, improved flowability and for optionally film coating tablets with Opadry.
There would have been a reasonable expectation of success because Demorin teach kinase inhibitor formulations which further comprise excipients whereas the claims of Patent ‘995 can comprise pharmaceuticals formulations. .
In regards to the amount of microcrystalline cellulose filler and lactose filler, hydroxypropyl cellulose binder, croscarmellose sodium, colloidal silicon dioxide and magnesium stearate, Apolo teaches overlapping ranges and per MPEP 2144.05, 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). It would have been well within the purview of an ordinary skilled artisan to adjust the concentration of each excipient and compound I taught by Apolo and Demorin.
The U.S. Patent and Trademark Office may not institute a derivation proceeding in the absence of a timely filed petition. The USPTO normally will not institute a derivation proceeding between applications or a patent and an application having common ownership (see 37 CFR 42.411). Commonly assigned U.S. Patent No. 11542259 discussed above, may form the basis for a rejection of the noted claims under 35 U.S.C. 102 or 103 if the commonly assigned case qualifies as prior art under 35 U.S.C. 102(a)(2) and the patentably indistinct inventions were not commonly owned or deemed to be commonly owned not later than the effective filing date under 35 U.S.C. 100(i) of the claimed invention.
In order for the examiner to resolve this issue the applicant or patent owner can provide a statement under 35 U.S.C. 102(b)(2)(C) and 37 CFR 1.104(c)(4)(i) to the effect that the subject matter and the claimed invention, not later than the effective filing date of the claimed invention, were owned by the same person or subject to an obligation of assignment to the same person. Alternatively, the applicant or patent owner can provide a statement under 35 U.S.C. 102(c) and 37 CFR 1.104(c)(4)(ii) to the effect that the subject matter was developed and the claimed invention was made by or on behalf of one or more parties to a joint research agreement that was in effect on or before the effective filing date of the claimed invention, and the claimed invention was made as a result of activities undertaken within the scope of the joint research agreement; the application must also be amended to disclose the names of the parties to the joint research agreement.
A showing that the inventions were commonly owned or deemed to be commonly owned not later than the effective filing date under 35 U.S.C. 100(i) of the claimed invention will preclude a rejection under 35 U.S.C. 102 or 103 based upon the commonly assigned case. Alternatively, applicant may take action to amend or cancel claims such that the applications, or the patent and the application, no longer contain claims directed to patentably indistinct inventions.
Claims 39-42 are provisionally rejected on the ground of nonstatutory double patenting as being unpatentable over claims 1, 8, 18,20,21 of copending Application No. 18706757 reference application) in view of Demorin et al. ( WO2020123800-published 6/18/2020-see IDS filed 7/18/2025) and Apolo (WO2018064191).
Claims 1-3, 5, 24,33-38 are directed to an invention not patentably distinct from claims 1, 8, 18,20,21 of commonly assigned Application no. 18706757.
Although the claims at issue are not identical, they are not patentably distinct from each other because both the instant claims and the claims of Application ‘757 arrive at the structure compound 1 instantly claimed including hemifumarate forms. Application ‘757 discloses that the compound encompasses hemifumarate..
Application ‘757 does not teach the composition is present with or a diluent, binder, disintegrants, glidants, lubricants and film coating comprising silicon dioxide glidant, hydroxypropyl cellulose binder, croscarmellose sodium disintegrant, microcrystalline cellulose and lactose as the diluents, stearic acid lubricant, Opadry for film coating as claimed.
However, Demorin et al. teach Compound 1 hemifumarate form B of structure
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(meeting the elected species to hemifumarate), see paragraph [0011]. The compound I hemifumarate form can comprise a pharmaceutical composition, see paragraphs [0328]-[0329]. The pharmaceutical composition can comprise excipients including cellulose derivatives as binders and croscarmellose sodium as a disintegrant, see paragraph [0046]. Microcrystalline cellulose and lactose can be present, see paragraphs [00476] and [00479]. The compound I can be present from 1-99% by weight or preferably from 5-75% by weight with the rest being excipients, see paragraph [00482]. The pharmaceutical composition of Demorin can be prepared with coatings, see paragraph [00477]. Suitable excipients include fillers, diluent, lubricants, disintegrants, binders, and wetting agents, see paragraphs [0096] and [0476]. The composition can be in the form of a tablet or capsule.
presence and amount of steric acid lubricant (elected species for excipients).
Apolo teaches treating cancer with the kinase inhibitor carbozantinib wherein the pharmaceutical formulation includes tablets comprising at paragraph [0088]:
28-38 percent by weight of Carbozantinib (kinase inhibitor) or a pharmaceutically acceptable salt thereof (based on 100% or 100mg this would encompass 28-38mg);
37- 39 percent by weight or microcrystalline cellulose (based on 100% this would encompass 37-39mg); (filler/diluent paragraph [0041] [0083]-[0085].) In another embodiment the microcrystalline cellulose can comprise 30-80% weight (equivalent to 30-80mg), see paragraphs [0072]-[0077].
18 to 20 percent by weight of lactose anhydrous (18-20mg for 100% weight); (filler paragraph [0041] and [0083]-[0085].)
1.5-4.5 percent by weight of hydroxypropyl cellulose (equivalent to 1.5-4.5mg) (binder see paragraphs [0043]-[0044]);
3-9 percent by weight a croscarmellose sodium (equivalent to 3-9mg) (disintegrant see paragraphs [0045]-[0046];
0.1-0.8 percent by weight (0.1-0.8 mg) of colloidal silicon dioxide (glidant see paragraphs [0047]-[0048]; and
0.5-1 percent (equivalent to 0.5-1mg) by weight of magnesium stearate. Stearic acid is taught to be an alternative lubricant to magnesium stearate, see paragraphs ]0049]-[0050]. Fillers are taught to be inert ingredients which adjust the bulk to produce a size for compression , see paragraph [0041]. Binders are added to powders to impart cohesive qualities which allow the compressed tablet to retain its integrity, see paragraph [0043]. A disintegrant is a substance or a mixture of substances added to facilitate breakup or disintegrate after administration, see paragraph [0045]. Glidant is added to contribute to compressibility, improve flowability and homogeneity of the formulation and to minimize segregation, see paragraph [0047]. The pharmaceutical composition can comprise a film coating including Opadry® for tablets. In one embodiment the film coating can comprise 3.9-4.1% by weight (equivalent to 3.9-4.1mg when total weight is 100mg or 100%).
It would have been obvious to provide the compound of Application ‘757 as a hemifumarate form B with a cellulose derivative of as a hydroxypropyl cellulose binder present from 18-20% by weight, the croscarmellose sodium disintegrant of Demorin from 3-9% by weight, and to further include microcrystalline cellulose present from 37-39% by weight with lactose present from 18-20% as fillers, 0.1-0.8% of colloidal silicon dioxide glidant and from 0.5-1% stearic acid lubricant with film coating as the pharmaceutical composition of Application ‘124..
One of ordinary skill in the art would have been motivate to do so as Apolo teaches such excipients as being advantageous for adjusting the size of the dosage formulation for compression, for facilitating break up of tablets, imparting cohesive qualities, improved flowability and for optionally film coating tablets with Opadry. Furthermore, Application ‘757 recites that compound 1 can be present in hemifumarate form with excipients.
There would have been a reasonable expectation of success because Demorin teach kinase inhibitor formulations which further comprise excipients whereas the claims of Patent ‘757 can comprise further excipients with the kinase inhibitor.
In regards to the amount of microcrystalline cellulose filler and lactose filler, hydroxypropyl cellulose binder, croscarmellose sodium, colloidal silicon dioxide and magnesium stearate, Apolo teaches overlapping ranges and per MPEP 2144.05, 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). It would have been well within the purview of an ordinary skilled artisan to adjust the concentration of each excipient taught by Apolo to arrive at the instantly claimed pharmaceutical composition.
This is a provisional nonstatutory double patenting rejection because the patentably indistinct claims have not in fact been patented.
The U.S. Patent and Trademark Office may not institute a derivation proceeding in the absence of a timely filed petition. The USPTO normally will not institute a derivation proceeding between applications or a patent and an application having common ownership (see 37 CFR 42.411). Commonly assigned Application No. 18706757 discussed above, may form the basis for a rejection of the noted claims under 35 U.S.C. 102 or 103 if the commonly assigned case qualifies as prior art under 35 U.S.C. 102(a)(2) and the patentably indistinct inventions were not commonly owned or deemed to be commonly owned not later than the effective filing date under 35 U.S.C. 100(i) of the claimed invention.
In order for the examiner to resolve this issue the applicant or patent owner can provide a statement under 35 U.S.C. 102(b)(2)(C) and 37 CFR 1.104(c)(4)(i) to the effect that the subject matter and the claimed invention, not later than the effective filing date of the claimed invention, were owned by the same person or subject to an obligation of assignment to the same person. Alternatively, the applicant or patent owner can provide a statement under 35 U.S.C. 102(c) and 37 CFR 1.104(c)(4)(ii) to the effect that the subject matter was developed and the claimed invention was made by or on behalf of one or more parties to a joint research agreement that was in effect on or before the effective filing date of the claimed invention, and the claimed invention was made as a result of activities undertaken within the scope of the joint research agreement; the application must also be amended to disclose the names of the parties to the joint research agreement.
A showing that the inventions were commonly owned or deemed to be commonly owned not later than the effective filing date under 35 U.S.C. 100(i) of the claimed invention will preclude a rejection under 35 U.S.C. 102 or 103 based upon the commonly assigned case. Alternatively, applicant may take action to amend or cancel claims such that the applications, or the patent and the application, no longer contain claims directed to patentably indistinct inventions
Claims 39-42 are provisionally rejected on the ground of nonstatutory double patenting as being unpatentable over claims 142,151-153 of copending Application No. 18657052 reference application) in view of Apolo (WO2018064191).
Claims 1-3, 5, 24,33-38 are directed to an invention not patentably distinct from claims 142,151-153 of commonly assigned Application no. 18657052.
Although the claims at issue are not identical, they are not patentably distinct from each other because both the instant claims and the claims of Application ‘052 arrive at the structure compound 1 instantly claimed including hemifumarate form B.
Application ‘052 does not teach the composition is present with or a diluent, binder, disintegrants, glidants, lubricants and film coating comprising silicon dioxide glidant, hydroxypropyl cellulose binder, croscarmellose sodium disintegrant, microcrystalline cellulose and lactose as the diluents, stearic acid lubricant, Opadry for film coating as claimed.
However, Apolo teaches treating cancer with the kinase inhibitor carbozantinib wherein the pharmaceutical formulation includes tablets comprising at paragraph [0088]:
28-38 percent by weight of Carbozantinib (kinase inhibitor) or a pharmaceutically acceptable salt thereof (based on 100% or 100mg this would encompass 28-38mg);
37- 39 percent by weight or microcrystalline cellulose (based on 100% this would encompass 37-39mg); (filler/diluent paragraph [0041] [0083]-[0085].) In another embodiment the microcrystalline cellulose can comprise 30-80% weight (equivalent to 30-80mg), see paragraphs [0072]-[0077].
18 to 20 percent by weight of lactose anhydrous (18-20mg for 100% weight); (filler paragraph [0041] and [0083]-[0085].)
1.5-4.5 percent by weight of hydroxypropyl cellulose (equivalent to 1.5-4.5mg) (binder see paragraphs [0043]-[0044]);
3-9 percent by weight a croscarmellose sodium (equivalent to 3-9mg) (disintegrant see paragraphs [0045]-[0046];
0.1-0.8 percent by weight (0.1-0.8 mg) of colloidal silicon dioxide (glidant see paragraphs [0047]-[0048]; and
0.5-1 percent (equivalent to 0.5-1mg) by weight of magnesium stearate. Stearic acid is taught to be an alternative lubricant to magnesium stearate, see paragraphs ]0049]-[0050]. Fillers are taught to be inert ingredients which adjust the bulk to produce a size for compression , see paragraph [0041]. Binders are added to powders to impart cohesive qualities which allow the compressed tablet to retain its integrity, see paragraph [0043]. A disintegrant is a substance or a mixture of substances added to facilitate breakup or disintegrate after administration, see paragraph [0045]. Glidant is added to contribute to compressibility, improve flowability and homogeneity of the formulation and to minimize segregation, see paragraph [0047]. The pharmaceutical composition can comprise a film coating including Opadry® for tablets. In one embodiment the film coating can comprise 3.9-4.1% by weight (equivalent to 3.9-4.1mg when total weight is 100mg or 100%).
It would have been obvious to provide the compound of Application ‘052 as a hemifumarate form with a cellulose derivative of as a hydroxypropyl cellulose binder present from 18-20% by weight, the croscarmellose sodium disintegrant from 3-9% by weight, and to further include microcrystalline cellulose present from 37-39% by weight with lactose present from 18-20% as fillers, 0.1-0.8% of colloidal silicon dioxide glidant and from 0.5-1% stearic acid lubricant with film coating as the pharmaceutical composition of Application ‘052.
One of ordinary skill in the art would have been motivated to do so as Apolo teaches such excipients as being advantageous for adjusting the size of the dosage formulation for compression, for facilitating break up of tablets, imparting cohesive qualities, improved flowability and for optionally film coating tablets with Opadry.
There would have been a reasonable expectation of success because the compound of Application ‘052 can further comprise excipients whereas the claims of with the kinase inhibitor.
In regards to the amount of microcrystalline cellulose filler and lactose filler, hydroxypropyl cellulose binder, croscarmellose sodium, colloidal silicon dioxide and magnesium stearate, Apolo teaches overlapping ranges and per MPEP 2144.05, 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). It would have been well within the purview of an ordinary skilled artisan to adjust the concentration of each excipient taught by Apolo including the kinase inhibitor to arrive at the instantly claimed pharmaceutical composition.
This is a provisional nonstatutory double patenting rejection because the patentably indistinct claims have not in fact been patented.
The U.S. Patent and Trademark Office may not institute a derivation proceeding in the absence of a timely filed petition. The USPTO normally will not institute a derivation proceeding between applications or a patent and an application having common ownership (see 37 CFR 42.411). Commonly assigned Application No. 18657052 discussed above, may form the basis for a rejection of the noted claims under 35 U.S.C. 102 or 103 if the commonly assigned case qualifies as prior art under 35 U.S.C. 102(a)(2) and the patentably indistinct inventions were not commonly owned or deemed to be commonly owned not later than the effective filing date under 35 U.S.C. 100(i) of the claimed invention. In order for the examiner to resolve this issue the applicant or patent owner can provide a statement under 35 U.S.C. 102(b)(2)(C) and 37 CFR 1.104(c)(4)(i) to the effect that the subject matter and the claimed invention, not later than the effective filing date of the claimed invention, were owned by the same person or subject to an obligation of assignment to the same person. Alternatively, the applicant or patent owner can provide a statement under 35 U.S.C. 102(c) and 37 CFR 1.104(c)(4)(ii) to the effect that the subject matter was developed and the claimed invention was made by or on behalf of one or more parties to a joint research agreement that was in effect on or before the effective filing date of the claimed invention, and the claimed invention was made as a result of activities undertaken within the scope of the joint research agreement; the application must also be amended to disclose the names of the parties to the joint research agreement A showing that the inventions were commonly owned or deemed to be commonly owned not later than the effective filing date under 35 U.S.C. 100(i) of the claimed invention will preclude a rejection under 35 U.S.C. 102 or 103 based upon the commonly assigned case. Alternatively, applicant may take action to amend or cancel claims such that the applications, or the patent and the application, no longer contain claims directed to patentably indistinct inventions
Response to remarks regarding Double Patenting
Applicants argue that U.S. Patent 12017995 claims a crystalline hemifumarate salt of compound I however as discussed above, Apolo discloses different formulations and could not render the claimed invention obvious. With regards to the U.S. Patent 11542259, Applicants argue that as discussed above, Demorin and Apolo do not render the claimed composition obvious.
Examiner respectfully submits that for the same reasons as discussed above with regards to Demorin and Apolo in the response to remarks regarding the 103, the claims of Application ‘259 and ‘995 are rendered obvious
Applicants argue that Application 18657052 does not disclose hemifumarate and that as discussed above, Demorin and Apolo do not cure the shortcomings.
Examiner respectfully submits that Demorin teaches and renders obvious hemifumarate Form B and that for the same reasons as discussed above with regards to Demorin and Apolo the claims of Application ‘757 are rendered obvious
Applicants argue with regards to Application 18706757 that Demorin nor Apollo cure the shortcomings.
Examiner respectfully submits that for the same reasons as discussed above with regards to Demorin and Apolo the claims of Application ‘757 are rendered obvious
Conclusion
Applicant’s arguments/remarks are considered unpersuasive and the addition of all new claims necessitated new rejections. Accordingly, THIS ACTION IS MADE FINAL. See MPEP § 706.07(a). Applicant is reminded of the extension of time policy as set forth in 37 CFR 1.136(a).
Currently, no claims are allowed and claims 39-42 are rejected.
A shortened statutory period for reply to this final action is set to expire THREE MONTHS from the mailing date of this action. In the event a first reply is filed within TWO MONTHS of the mailing date of this final action and the advisory action is not mailed until after the end of the THREE-MONTH shortened statutory period, then the shortened statutory period will expire on the date the advisory action is mailed, and any extension fee pursuant to 37 CFR 1.136(a) will be calculated from the mailing date of the advisory action. In no event, however, will the statutory period for reply expire later than SIX MONTHS from the mailing date of this final action.
/SARAH ALAWADI/ Primary Examiner, Art Unit 1619
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