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 .
Priority
This application, filed on 09/22/2023, is a continuation of U.S. Patent Application No. 17/671,714, filed 02/15/2022, which claims priority to U.S. provisional application 63/149,901, filed on 02/16/2021 and 63/275,163 filed on 11/03/2021.
Information Disclosure Statement
The information disclosure statement (IDS) filed on 01/27/2025, complies with the provisions of 37 CFR 1.97, 1.98 and MPEP § 609. Accordingly, it has been placed in the application file and the information therein has been considered as to the merits, except where noted.
Election/Restriction
Applicant’s election of Group II, pending claims 42-57, without traverse in the reply filed on 01/27/2025 to Restriction Requirement filed on 11/25/2024, is acknowledged. Claims 1-41 and 58-109 are withdrawn from further consideration pursuant to 37 CFR 1.142(b) as being drawn to a nonelected invention, there being no allowable generic or linking claim.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 with traverse in the reply filed on 01/27/2025. After careful reconsideration, claims 71-82 are rejoined. Thus, claims 1-41, 58-70, and 83-109 are withdrawn, and claims 42-57 and 71-82 are under consideration.
DETAILED ACTION
Claims 1-109 are pending with claims 1-41, 58-70, and 83-109 are withdrawn and claims 42-57, and 71-82 are under consideration.
Claim Interpretation
Examination requires claim terms first be construed in terms in the broadest reasonable manner during prosecution as is reasonably allowed in an effort to establish a clear record of what applicant intends to claim. See MPEP § 2111. Under a broadest reasonable interpretation, words of the claim must be given their plain meaning, unless such meaning is inconsistent with the specification. See MPEP § 2111.01. It is also appropriate to look to how the claim term is used in the prior art, which includes prior art patents, published applications, trade publications, and dictionaries. MPEP § 2111.01 (III). However, specific embodiments of the specification cannot be imported into the claims, particularly where the subject claim limitation is broader than the embodiment. MPEP § 2111.01(II).
Claim interpretation for “unit dosage”
Claims 42-57 recite “a unit dosage form”. The unit dosage will be interpreted as a pharmaceutical composition, for example a capsule or tablet.
Objection to Specification
The disclosure is objected to because it contains an embedded hyperlink and/or other form of browser-executable code. Applicant is required to delete the embedded hyperlink and/or other form of browser-executable code; references to websites should be limited to the top-level domain name without any prefix such as http:// or other browser-executable code. See MPEP § 608.01. The embedded hyperlinks are on Pages 46, 51 and 52.
The disclosure is objected to because of the following informalities:
The instant specification recites that the instant Application is a continuation of Application No. 17/671,741, which should Application No. 17/671,714. The typographical error should be corrected.
Appropriate correction is required.
Claim Rejections - 35 USC § 103
In the event the determination of the status of the application as subject to AIA 35 U.S.C. 102 and 103 (or as subject to pre-AIA 35 U.S.C. 102 and 103) is incorrect, any correction of the statutory basis for the rejection will not be considered a new ground of rejection if the prior art relied upon, and the rationale supporting the rejection, would be the same under either status.
The following is a quotation of 35 U.S.C. 103 which forms the basis for all obviousness rejections set forth in this Office action:
A patent for a claimed invention may not be obtained, notwithstanding that the claimed invention is not identically disclosed as set forth in section 102, if the differences between the claimed invention and the prior art are such that the claimed invention as a whole would have been obvious before the effective filing date of the claimed invention to a person having ordinary skill in the art to which the claimed invention pertains. Patentability shall not be negated by the manner in which the invention was made.
The factual inquiries for establishing a background for determining obviousness under 35 U.S.C. 103 are summarized as follows:
1. Determining the scope and contents of the prior art.
2. Ascertaining the differences between the prior art and the claims at issue.
3. Resolving the level of ordinary skill in the pertinent art.
4. Considering objective evidence present in the application indicating obviousness or nonobviousness.
35 USC § 103 over Vasbinder
Claims 42-52 and 76-77 are rejected under 35 U.S.C. 103 as being unpatentable over M. Vasbinder et al. (US 20190330194 A1, 10/31/2019, “Vasbinder” cited in the PTO-892).
Vasbinder teaches a pharmaceutical composition comprising a compound of Formula I, or a pharmaceutically acceptable salt thereof, and at least one pharmaceutically acceptable carrier, wherein the claimed compound discloses as a species of Formula I in Table E11 [Pg. 370, Table E11, Ln. 1], and in Vasbinder’s claims 444-451, as Vasbinder document claims the compound and its pharmaceutical compositions:
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Vasbinder teaches pharmaceutical formulations and dosage forms of the above PARP7 inhibitor, [540], wherein the formulation is for oral administration, wherein the composition can be formulated in a unit dosage form, a physically discrete unit suitable as unitary dosages for human subjects and other mammals, each unit containing a predetermined quantity of active material calculated to produce the desired therapeutic effect, in association with a suitable pharmaceutical excipient. [Pg. 30, [542]]. Vasbinder teaches that the unit dosage form is prepared in a solid composition including tablets, pills and capsules containing 0.1 to about 500 mg of the above compound [Pg. 30, [0544]].
Vasbinder teaches that the therapeutic dosage can vary according to, for example, the particular use for which the treatment is made, the manner of administration of the compound, the health and condition of the patient, and the judgment of the prescribing physician, and the amount can vary depending upon a number of factors including dosage, chemical characteristics, and the route of administration. Some typical dose ranges are from about 1 μg/kg to about 1 g/kg of body weight per day. In some embodiments, the dose range is from about 0.01 mg/kg to about 100 mg/kg of body weight per day. The dosage is likely to depend on the type and extent of progression of the disease or disorder, the overall health status of the particular patient, the relative biological efficacy of the compound selected, formulation of the excipient, and its route of administration. Effective doses can be extrapolated from dose-response curves derived from in vitro or animal model test systems. [Pg. 31, 0550]].
Vasbinder teaches that the active compound can be effective over a wide dosage range and is generally administered in a pharmaceutically effective amount. It will be understood, however, that the amount of the compound actually administered will usually be determined by a physician, according to the relevant circumstances, including the condition to be treated, the chosen route of administration, the actual compound administered, the age, weight, and response of the individual patient, the severity of the patient's symptoms, and the like. [Pg. 31, [0548]].
With regard to claims 76 and 77 Vasbinder teaches that for preparing solid compositions such as tablets, the principal active ingredient is mixed with a pharmaceutical excipient to form a solid pre-formulation composition e.g., unit dosage containing a homogeneous mixture of a PARP7 inhibitor, wherein the unit dosage forms of the type described above containing from, for example, 0.1 to about 500 mg of the active ingredient of the PARP7 inhibitor. Vasbinder teaches that in the unit dosage form, the active compound can be effective over a wide dosage range and is generally administered in a pharmaceutically effective amount. It will be understood, however, that the amount of the compound actually administered will usually be determined by a physician, according to the relevant circumstances, including the age, weight, and response of the individual patient, the severity of the patient's symptoms, and the like. [Pg. 30, [0544]].
As such, Vasbinder teaches dose ranges of about 0.01 mg/kg to about 100 mg/kg, and 0.1 to about 500 mg. Note that Vasbinder does not provide numerical values to the relative term “about”, nevertheless, Vasbinder teaches that the term “about” indicate that the value or range of values may deviate to an extent deemed reasonable to one of ordinary skill in the art. [Pg. 26, [509]].
However, while Vasbinder teaches a dosing range of 0.1 mg to about 500 mg of the PARP7 inhibitor above, Vasbinder does not teach that the dosage form in an amount of about 25 mg to about 500 mg, or the subdivided doses of 50 mg, 75 mg, 100 mg, 150 mg, 200 mg, 250 mg, or 300 mg.
It would have been prima facie obvious to one of ordinary skill in the art prior to the effective failing date of the instant claimed invention to modify Vasbinder’s dosing range of 0.1-500 mg of PARP7 inhibitor to dosages of about 25 mg- about 500 mg or 30%-50% of the PARP7 inhibitor measured as free base in view of the teachings of Vasbinder. One of ordinary skill in the art is motivated to do so with reasonable expectation of success because Vasbinder teaches dosing ranges that encompasses and overlapped with the claims’ ranges and teaches that the administered amount will be determine by the prescribing physician according to many factors including the manner of administration, the type and extent of progression of the disease or disorder, the overall health status of the particular patient, and response of the individual patient and the like. As provided in the 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). "[A] prior art reference that discloses a range encompassing a somewhat narrower claimed range is sufficient to establish a prima facie case of obviousness." In re Peterson, 315 F.3d 1325, 1330, 65 USPQ2d 1379, 1382-83 (Fed. Cir. 2003). See also In re Harris, 409 F.3d 1339, 74 USPQ2d 1951 (Fed. Cir. 2005). Moreover, MPEP 2144.05.II.A explains: “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).” Thus, claims 42-51 and 76-77 are obvious over Vasbinder.
35 USC § 103 over Vasbinder in view of Khadka
Claims 53-57, 71-75, and 78-82 are rejected under 35 U.S.C. 103 as being unpatentable over M. Vasbinder et al. (US 20190330194 A1, 10/31/2019, “Vasbinder” cited in the PTO-892) as applied above to claims 42-52 and 76-77, in view of P. Khadka et al. (Asian Journal of Pharmaceutical Sciences, Volume 9, Issue 6, 2014, Pages 304-316, ISSN 1818-0876, doi.org/10.1016/j.ajps.2014.05.005, “Khadka” cited in the PTO-892).
As discussed above, Vasbinder teaches a unit dosage form comprising 5-[[(2S)-1-(3-oxo-3-[4-[5- (trifluoromethyl)pyrimidin-2-yl]piperazin-1-yl]propoxy)propan-2-yl] amino]-4-(trifluoromethyl)-2,3-dihydropyridazin-3-one, or a pharmaceutically acceptable salt thereof, in an amount of about 25 mg to about 500 mg, measured as the free base, and a solid pharmaceutical formulation comprising the compound 5-[[(2S)-1-(3-oxo-3-[4-[5-(trifluoromethy]l)pyrimidin-2-yl]piperazin-1-yl]propoxy )propan-2-yl]amino]-4-(trifluoromethyl )-2,3-dihydropyridazin-3-one, or a pharmaceutically acceptable salt thereof, in an amount of about 30% to about 50% w/w (e.g., 40%), and at least one pharmaceutically acceptable excipient. Vasbinder also teaches preparation for solid compositions such as tablets, wherein the above compound is mixed with a pharmaceutical excipient to form a solid pre-formulation composition containing a homogeneous mixture of PARP7 inhibitor above. [Pg. 30, 0544].
However, Vasbinder does not teach that the solid PARP7 inhibitor has a particle size diameter of less than 30 µm, or particle size diameter of about 1-20 µm.
Khadka teaches that the particle size reduction is one of the oldest strategies for improving solubility of drugs since solubility of drugs is intrinsically related to drug particle size, and when the particle size is decreased, the larger surface area of the drug allows the increase in the surface area to volume ratio thus increasing the surface area available for solvation. Khadka teaches that the particle size reduction technologies are therefore routinely used to increase the bioavailability of poorly soluble drugs. [Khadka, pg. 306, col. 1].
Khadka teaches that particle size reduction techniques involving powder and particle technology including mechanical micronization such as jet milling, ball milling, homogenization, which can produce particle size range of 5-10 µm. [Pg. 307- 308, col. 1, 1st para.].
It would have been prima facie obvious to one of ordinary skill in the art, prior to the effective filing date of the instantly claimed invention to decrease the particle size of Vasbinder’s compound 664 above to less than 30 µm i.e., 10 µm in view of the teachings of Khadka. One of ordinary skill would have been motivated to do so with reasonable expectation of success because Khadka teaches that particle size reduction improving solubility and increase the bioavailability of drugs, and provide guidance to different particle size reduction technologies that produce drug particle size as low as 5-10 µm. Thus, claims 53-57, 71-75, and 78-82 are obvious over Vasbinder and Khadka.
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 USPTO Internet website contains terminal disclaimer forms which may be used. Please visit www.uspto.gov/patent/patents-forms. The 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/process/file/efs/guidance/eTD-info-I.jsp.
Double Patenting over U.S. Patent No. 10,550,105 B2
Claims 42-52 and 76-77 are rejected on the ground of nonstatutory double patenting as being unpatentable over claims 1-4 of U.S. Patent No. 10,550,105 B2 in view of Filloon TG. Stat Med. 1995 May 15-30;14(9-10):925-32; discussion 933. doi: 10.1002/sim.4780140911., “Filloon” cited in the PTO0892); and Remington's Pharmaceutical science, 18th edition, Gennaro, A.R., ED, Mack Pub. Co.: Easton, PA, 1990, pp 1633-1665, “Remington”, cited in the PTO-892). Although the claims at issue are not identical, they are not patentably distinct from each other because:
Instant claims 42-52 and 76-77 recites “a unit dosage form comprising 5-[[(2S)-1-(3-oxo-3-[4-[5- (trifluoromethyl)pyrimidin-2-yl]piperazin-1-yl]propoxy)propan-2-yl] amino]-4-(trifluoromethyl)-2,3-dihydropyridazin-3-one, or a pharmaceutically acceptable salt thereof, in an amount of about 25 mg to about 500 mg, measured as the free base, and a solid pharmaceutical formulation comprising the compound 5-[[(2S)-1-(3-oxo-3-[4-[5-(trifluoromethy]l)pyrimidin-2-yl]piperazin-1-yl]propoxy )propan-2-yl]amino]-4-(trifluoromethyl )-2,3-dihydropyridazin-3-one, or a pharmaceutically acceptable salt thereof, in an amount of about 30% to about 50% w/w (e.g., 40%), and at least one pharmaceutically acceptable excipient.” The structure of claims 42 compound is shown below:
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US Patent No. 10,550,105 B2 recited in conflicting claims 1-4 “a pharmaceutical composition comprising a compound having the structure below, or a pharmaceutically acceptable salt thereof, and at least one pharmaceutically acceptable carrier:
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US Patent No. 10,550,105 B2 does not recite in claims 1-4 that the amount of the above compound in the pharmaceutical composition is about 25 mg to about 500 mg, or the subdivided doses of 50 mg, 75 mg, 100 mg, 150 mg, 200 mg, 250 mg, or 300 mg.
With respect to preparing a solid pharmaceutical composition of the pharmaceutically active compound above, Remington teaches that pharmaceutical active substances are most frequently administered orally in a solid dosage form including tablets and capsules and teaches the preparation method of the solid dosage form. [Abstract].
With respect to the amount of the pharmaceutically active compound above in the solid dosage form, Filloon teaches detailed description on determining the minimum therapeutically effective dose, the lowest dose level that yields a therapeutic benefit to patients. Thus, the determination of a therapeutically effective dose of a known pharmaceutical active agent is routine in the prior art.
Therefore, it would have been prima facie obvious to one of ordinary skill in the art prior to the effective failing date of the instant claimed invention to prepare a solid oral dosage form of the therapeutically active compound taught by US Patent No. 10,550,105 B2 in a therapeutically effective amount e.g., 25mg-500mg in view of the teachings of Remington and Filloon. One of ordinary skill in the art would have been motivated to do so with reasonable expectation of success because US Patent No. 10,550,105 B2 teaches that the compound is used for the treatment of cancer which indicates that the compound is a therapeutically active compound; Remington teaches methods of preparing a solid oral dosage form of pharmaceutically active compounds and provide motivation to prepare them in solid oral dosage form; and Filloon teaches how to determine the minimum therapeutically effective dose. Therefore, one of ordinary skill in the art would have been motivated to utilize the teachings of Remington and Filloon to prepare therapeutic effective amount of the US Patent No. 10,550,105 B2 above compound in an oral dosage form. Moreover, MPEP 2144.05.II.A explains: “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).” Thus, claims 42-51 are obvious over US Patent No. 10,550,105 B2.
Double Patenting over U.S. Patent No. 10,550,105 B2 in view of Khadka
Claims 53-57 and 71-75, 78-82 are rejected on the ground of nonstatutory double patenting as being unpatentable over claims 1-4 of U.S. Patent No. 10,550,105 B2 in view of Filloon TG. Stat Med. 1995 May 15-30;14(9-10):925-32; discussion 933. doi: 10.1002/sim.4780140911., “Filloon” cited in the PTO0892); and Remington's Pharmaceutical science, 18th edition, Gennaro, A.R., ED, Mack Pub. Co.: Easton, PA, 1990, pp 1633-1665, “Remington”, cited in the PTO-892), as applied above to claims 42-52 and 76-77, further, in view of P. Khadka et al. (Asian Journal of Pharmaceutical Sciences, Volume 9, Issue 6, 2014, Pages 304-316, ISSN 1818-0876, doi.org/10.1016/j.ajps.2014.05.005, “Khadka” cited in the PTO-892). Although the claims at issue are not identical, they are not patentably distinct from each other because:
Instant claims 53-57 and 71-75, 78-82 recite that the particle size diameter [d90] of the unit dosage form, is less than about 30 µm. and a solid preparation of the compound above in an amount of about 30% to about 50% w/w (e.g., 40%), and at least one pharmaceutically acceptable excipient.
As discussed above, the combination of U.S. Patent No. 10,550,105 B2, Remington, and Filloon teaches a unit dosage form comprising 5-[[(2S)-1-(3-oxo-3-[4-[5- (trifluoromethyl)pyrimidin-2-yl]piperazin-1-yl]propoxy)propan-2-yl] amino]-4-(trifluoromethyl)-2,3-dihydropyridazin-3-one, or a pharmaceutically acceptable salt thereof, in a therapeutically effective amount, e.g., 25-500 mg. However, the combination of U.S. Patent No. 10,550,105 B2, Remington, and Filloon do not teach that the solid PARP7 inhibitor has a particle size diameter of less than 30 µm, or particle size diameter of about 1-20 µm.
Khadka’s teachings are as discussed above
It would have been prima facie obvious to one of ordinary skill in the art, prior to the effective filing date of the instantly claimed invention to decrease the particle size of the unit dosage form of the combination of U.S. Patent No. 10,550,105 B2, Remington, and Filloon to less than 30 µm i.e., 10 µm in view of the teachings of Khadka. One of ordinary skill would have been motivated to do so with reasonable expectation of success because Khadka teaches that particle size reduction improving solubility and increase the bioavailability of drugs and provide guidance to different particle size reduction technologies that produce drug particle size as low as 5-10 µm. Thus, claims 53-57 and 71-75, 78-82 are obvious.
Double Patenting over U.S. Patent No. 10,870,641 B2
Claims 42-52 and 76-77 are rejected on the ground of nonstatutory double patenting as being unpatentable over claims 1 and 16 of U.S. Patent No. 10,870,641 B2 in view of Filloon TG. Stat Med. 1995 May 15-30;14(9-10):925-32; discussion 933. doi: 10.1002/sim.4780140911., “Filloon” cited in the PTO0892); and Remington's Pharmaceutical science, 18th edition, Gennaro, A.R., ED, Mack Pub. Co.: Easton, PA, 1990, pp 1633-1665, “Remington”, cited in the PTO-892). Although the claims at issue are not identical, they are not patentably distinct from each other because:
Instant claim 42 recites “a unit dosage form comprising 5-[[(2S)-1-(3-oxo-3-[4-[5- (trifluoromethyl)pyrimidin-2-yl]piperazin-1-yl]propoxy)propan-2-yl] amino]-4-(trifluoromethyl)-2,3-dihydropyridazin-3-one, or a pharmaceutically acceptable salt thereof, in an amount of about 25 mg to about 500 mg, measured as the free base and a solid pharmaceutical formulation comprising the compound 5-[[(2S)-1-(3-oxo-3-[4-[5-(trifluoromethy]l)pyrimidin-2-yl]piperazin-1-yl]propoxy )propan-2-yl]amino]-4-(trifluoromethyl )-2,3-dihydropyridazin-3-one, or a pharmaceutically acceptable salt thereof, in an amount of about 30% to about 50% w/w (e.g., 40%), and at least one pharmaceutically acceptable excipient.” The structure of claims 42 compound is shown below:
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U.S. Patent No. 10,870,641 B2 recites in conflicting claims 1 and 16 “a method of treating cancer in a patient in need of treatment comprising administering to said patient a therapeutically effective amount of a compound having the structure:
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US Patent No. 10,870,641 B2 does not recite in claims 1 or 16 that the therapeutically effective amount is an amount of about 25 mg to about 500 mg, or the subdivided doses of 50 mg, 75 mg, 100 mg, 150 mg, 200 mg, 250 mg, or 300 mg.
The teachings of Remington and Filloon are as discussed above.
The obviousness rationale is like the obviousness rationale for the Double Patenting Rejection of claims 42-52 and 76-77 above and is incorporated herein by reference as applied to the rejected claims.
Double Patenting over U.S. Patent No. 10,870,641 B2 in view of Khadka
Claims 53-57 and 71-75, 78-82 are rejected on the ground of nonstatutory double patenting as being unpatentable over claims 1 and 16 of U.S. Patent No. 10,870,641 B2 in view of Filloon TG. Stat Med. 1995 May 15-30;14(9-10):925-32; discussion 933. doi: 10.1002/sim.4780140911., “Filloon” cited in the PTO0892); and Remington's Pharmaceutical science, 18th edition, Gennaro, A.R., ED, Mack Pub. Co.: Easton, PA, 1990, pp 1633-1665, “Remington”, cited in the PTO-892), as applied above to claims 42-52 and 76-77, further, in view of P. Khadka et al. (Asian Journal of Pharmaceutical Sciences, Volume 9, Issue 6, 2014, Pages 304-316, ISSN 1818-0876, doi.org/10.1016/j.ajps.2014.05.005, “Khadka” cited in the PTO-892). Although the claims at issue are not identical, they are not patentably distinct from each other because:
Instant claims 53-57 and 71-75, 78-82 recite that the particle size diameter [d90] of the unit dosage form, is less than about 30 µm. and a solid preparation of the compound above in an amount of about 30% to about 50% w/w (e.g., 40%), and at least one pharmaceutically acceptable excipient.
As discussed above, U.S. Patent No. 10,870,641 B2, Remington, and Filloon teaches a unit dosage form comprising 5-[[(2S)-1-(3-oxo-3-[4-[5- (trifluoromethyl)pyrimidin-2-yl]piperazin-1-yl]propoxy)propan-2-yl] amino]-4-(trifluoromethyl)-2,3-dihydropyridazin-3-one, or a pharmaceutically acceptable salt thereof, in a therapeutically effective amount, e.g., 25-500 mg. However, the combination of U.S. Patent No. 10,870,641 B2, Remington, and Filloon do not teach that the solid PARP7 inhibitor has a particle size diameter of less than 30 µm, or particle size diameter of about 1-20 µm.
Khadka’s teachings are as discussed above and are incorporated herein by reference.
The obviousness rationale is similar to the obviousness rationale of claims 53-57, 71-75, and 78-82 of the Double Patenting Rejection above.
Double Patenting over U.S. Patent No. 11,014,913 B2
Claims 42-52 and 76-77 are rejected on the ground of nonstatutory double patenting as being unpatentable over claims 1 and 13 of U.S. Patent No. 11,014,913 B2 in view of Filloon TG. Stat Med. 1995 May 15-30;14(9-10):925-32; discussion 933. doi: 10.1002/sim.4780140911., “Filloon” cited in the PTO0892); and Remington's Pharmaceutical science, 18th edition, Gennaro, A.R., ED, Mack Pub. Co.: Easton, PA, 1990, pp 1633-1665, “Remington”, cited in the PTO-892). Although the claims at issue are not identical, they are not patentably distinct from each other because:
Instant claims 42-52 and 76-77 recites “a unit dosage form comprising 5-[[(2S)-1-(3-oxo-3-[4-[5- (trifluoromethyl)pyrimidin-2-yl]piperazin-1-yl]propoxy)propan-2-yl] amino]-4-(trifluoromethyl)-2,3-dihydropyridazin-3-one, or a pharmaceutically acceptable salt thereof, in an amount of about 25 mg to about 500 mg, measured as the free base and a solid pharmaceutical formulation comprising the compound 5-[[(2S)-1-(3-oxo-3-[4-[5-(trifluoromethy]l)pyrimidin-2-yl]piperazin-1-yl]propoxy )propan-2-yl]amino]-4-(trifluoromethyl )-2,3-dihydropyridazin-3-one, or a pharmaceutically acceptable salt thereof, in an amount of about 30% to about 50% w/w (e.g., 40%), and at least one pharmaceutically acceptable excipient.” The structure of claims 42 compound is shown below:
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U.S. Patent No. 11,014,913 B2 recites in conflicting claims 1 and 13 “a compound which is 5-[[(2S)-1-(3-oxo-3-[4-[5- (trifluoromethyl)pyrimidin-2-yl]piperazin-1-yl]propoxy)propan-2-yl] amino]-4-(trifluoromethyl)-2,3-dihydropyridazin-3-one, wherein the compound is crystalline, and a pharmaceutical composition comprising a compound of claim 1 and at least one pharmaceutically acceptable carrier:
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US Patent No. 11,014,913 B2 does not recite in claims 1 and 13 that the amount of the above compound in the pharmaceutical composition is about 25 mg to about 500 mg, or the subdivided doses of 50 mg, 75 mg, 100 mg, 150 mg, 200 mg, 250 mg, or 300 mg.
Remington and Filloon teach as discussed above.
The obviousness rationale is similar to the obviousness rationale for the Double Patenting Rejection of claims 42-52 and 76-77 above.
Double Patenting over U.S. Patent No. 11,014,913 B2 in view of Khadka
Claims 53-57, 71-75, and 78-82 are rejected on the ground of nonstatutory double patenting as being unpatentable over claims 1 and 16 of U.S. Patent No. 11,014,913 B2 in view of Filloon TG. Stat Med. 1995 May 15-30;14(9-10):925-32; discussion 933. doi: 10.1002/sim.4780140911., “Filloon” cited in the PTO0892); and Remington's Pharmaceutical science, 18th edition, Gennaro, A.R., ED, Mack Pub. Co.: Easton, PA, 1990, pp 1633-1665, “Remington”, cited in the PTO-892), as applied above to claims 42-52 and 71-82, further, in view of P. Khadka et al. (Asian Journal of Pharmaceutical Sciences, Volume 9, Issue 6, 2014, Pages 304-316, ISSN 1818-0876, doi.org/10.1016/j.ajps.2014.05.005, “Khadka” cited in the PTO-892). Although the claims at issue are not identical, they are not patentably distinct from each other because:
Instant claims 53-57 and 71-75, 78-82 recite that the particle size diameter [d90] of the unit dosage form, is less than about 30 µm. and a solid preparation of the compound above in an amount of about 30% to about 50% w/w (e.g., 40%), and at least one pharmaceutically acceptable excipient.
As discussed above, U.S. Patent No. 11,014,913 B2 Remington, and Filloon teaches a unit dosage form comprising 5-[[(2S)-1-(3-oxo-3-[4-[5- (trifluoromethyl)pyrimidin-2-yl]piperazin-1-yl]propoxy)propan-2-yl] amino]-4-(trifluoromethyl)-2,3-dihydropyridazin-3-one, or a pharmaceutically acceptable salt thereof, in a therapeutically effective amount, e.g., 25-500 mg. However, the combination of U.S. Patent No. 11,014,913 B2, Remington, and Filloon do not teach that the solid PARP7 inhibitor has a particle size diameter of less than 30 µm, or particle size diameter of about 1-20 µm.
Khadka’s teachings are as discussed above and are incorporated herein by reference.
The obviousness rationale is similar to the obviousness rationale of claims 53-57 and 71-75, 78-82 of the Double Patenting Rejection above.
Double Patenting over U.S. Patent No. 11,566,020 B1
Claims 42-52 and 76-77 are rejected on the ground of nonstatutory double patenting as being unpatentable over claim 1 of U.S. Patent No. 11,566,020 B1 in view of Filloon TG. Stat Med. 1995 May 15-30;14(9-10):925-32; discussion 933. doi: 10.1002/sim.4780140911., “Filloon” cited in the PTO0892); and Remington's Pharmaceutical science, 18th edition, Gennaro, A.R., ED, Mack Pub. Co.: Easton, PA, 1990, pp 1633-1665, “Remington”, cited in the PTO-892). Although the claims at issue are not identical, they are not patentably distinct from each other because:
Instant claim 42-52 and 76-77 recites “a unit dosage form comprising 5-[[(2S)-1-(3-oxo-3-[4-[5- (trifluoromethyl)pyrimidin-2-yl]piperazin-1-yl]propoxy)propan-2-yl] amino]-4-(trifluoromethyl)-2,3-dihydropyridazin-3-one, or a pharmaceutically acceptable salt thereof, in an amount of about 25 mg to about 500 mg, measured as the free base and a solid pharmaceutical formulation comprising the compound 5-[[(2S)-1-(3-oxo-3-[4-[5-(trifluoromethy]l)pyrimidin-2-yl]piperazin-1-yl]propoxy )propan-2-yl]amino]-4-(trifluoromethyl )-2,3-dihydropyridazin-3-one, or a pharmaceutically acceptable salt thereof, in an amount of about 30% to about 50% w/w (e.g., 40%), and at least one pharmaceutically acceptable excipient.” The structure of claims 42 compound is shown below:
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U.S. Patent No. 11,566,020 B1 recites in conflicting claim 1 “a method of treating cancer in a patient in need of treatment comprising administering to said patient a therapeutically effective amount of a compound which is 5-[[(2S)-1-(3-oxo-3-[4-[5-(trifluoromethyl)pyrimidin-2-yl]piperazin-1-yl]propoxy)propan-2-yl]amino]-4-(trifluoromethyl)-2,3-dihydropyridazin-3-one, wherein the compound is crystalline:
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US Patent No. 11,566,020 B1 does not recite in claim 1 that the therapeutically effective amount is an amount of about 25 mg to about 500 mg, or the subdivided doses of 50 mg, 75 mg, 100 mg, 150 mg, 200 mg, 250 mg, or 300 mg.
Remington and Filloon teach as discussed above.
The obviousness rationale is similar to the obviousness rationale for the Double Patenting Rejection of claims 42-52 and 76-77 above.
Double Patenting over U.S. Patent No. 11566020B1 in view of Khadka
Claims 53-57, 71-75, and 78-82 are rejected on the ground of nonstatutory double patenting as being unpatentable over claim 1 of U.S. Patent No. 11,566,020 B1 in view of Filloon TG. Stat Med. 1995 May 15-30;14(9-10):925-32; discussion 933. doi: 10.1002/sim.4780140911., “Filloon” cited in the PTO0892); and Remington's Pharmaceutical science, 18th edition, Gennaro, A.R., ED, Mack Pub. Co.: Easton, PA, 1990, pp 1633-1665, “Remington”, cited in the PTO-892), as applied above to claims 42-52 and 71-82, further, in view of P. Khadka et al. (Asian Journal of Pharmaceutical Sciences, Volume 9, Issue 6, 2014, Pages 304-316, ISSN 1818-0876, doi.org/10.1016/j.ajps.2014.05.005, “Khadka” cited in the PTO-892). Although the claims at issue are not identical, they are not patentably distinct from each other because:
Instant claims 53-57,71-75, and 78-82 recite that the particle size diameter [d90] of the unit dosage form, is less than about 30 µm, and a solid preparation of the compound above in an amount of about 30% to about 50% w/w (e.g., 40%), and at least one pharmaceutically acceptable excipient.
As discussed above, U.S. Patent No. 11,566,020 B1 Remington, and Filloon teaches a unit dosage form comprising 5-[[(2S)-1-(3-oxo-3-[4-[5- (trifluoromethyl)pyrimidin-2-yl]piperazin-1-yl]propoxy)propan-2-yl] amino]-4-(trifluoromethyl)-2,3-dihydropyridazin-3-one, or a pharmaceutically acceptable salt thereof, in a therapeutically effective amount, e.g., 25-500 mg. However, the combination of U.S. Patent No. 11,566,020 B1, Remington, and Filloon do not teach that the solid PARP7 inhibitor has a particle size diameter of less than 30 µm, or particle size diameter of about 1-20 µm.
Khadka’s teachings are as discussed above and are incorporated herein by reference.
The obviousness rationale is similar to the obviousness rationale of claims 53-57 and 71-75, 78-82 of the Double Patenting Rejection above.
Double Patenting over Copending application 17/607,090
Claims 42-52 and 76-77 are provisionally rejected on the ground of nonstatutory double patenting as being unpatentable over claims 1, 7, 13, and 21 of Copending application 17/607,0901 (US 2022/0162196 A1) in view of Filloon TG. Stat Med. 1995 May 15-30;14(9-10):925-32; discussion 933. doi: 10.1002/sim.4780140911., “Filloon” cited in the PTO0892); and Remington's Pharmaceutical science, 18th edition, Gennaro, A.R., ED, Mack Pub. Co.: Easton, PA, 1990, pp 1633-1665, “Remington”, cited in the PTO-892). Although the claims at issue are not identical, they are not patentably distinct from each other because:
Instant claims 42-52 and 76-77 recites “a unit dosage form comprising 5-[[(2S)-1-(3-oxo-3-[4-[5- (trifluoromethyl)pyrimidin-2-yl]piperazin-1-yl]propoxy)propan-2-yl] amino]-4-(trifluoromethyl)-2,3-dihydropyridazin-3-one, or a pharmaceutically acceptable salt thereof, in an amount of about 25 mg to about 500 mg, measured as the free base and a solid pharmaceutical formulation comprising the compound 5-[[(2S)-1-(3-oxo-3-[4-[5-(trifluoromethy]l)pyrimidin-2-yl]piperazin-1-yl]propoxy )propan-2-yl]amino]-4-(trifluoromethyl )-2,3-dihydropyridazin-3-one, or a pharmaceutically acceptable salt thereof, in an amount of about 30% to about 50% w/w (e.g., 40%), and at least one pharmaceutically acceptable excipient.” The structure of claims 42 compound is shown below:
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Copending application 17/607,090 recites in conflicting claims 1, 7, 13, and 21 “a solid form of compound 1 having the formula below or a benzenesulfonic acid thereof (conflicting claim 13, and a pharmaceutical composition comprising a compound of claim 1 and at least one pharmaceutically acceptable carrier:
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Copending application 17/607,090 does not recite in claims 1, 7, 13, and 21 that the amount of the above compound in the pharmaceutical composition is about 25 mg to about 500 mg, or the subdivided doses of 50 mg, 75 mg, 100 mg, 150 mg, 200 mg, 250 mg, or 300 mg.
Double Patenting over Copending application 17/607,090 in view of Khadka
Claims 53-57, 71-75, and 78-82 are provisionally rejected on the ground of nonstatutory double patenting as being unpatentable over claims 1, 7, 13 and 21 of Copending application 17/607,090 (US20220162196A1) in view of Filloon TG. Stat Med. 1995 May 15-30;14(9-10):925-32; discussion 933. doi: 10.1002/sim.4780140911., “Filloon” cited in the PTO-892); and Remington's Pharmaceutical science, 18th edition, Gennaro, A.R., ED, Mack Pub. Co.: Easton, PA, 1990, pp 1633-1665, “Remington”, cited in the PTO-892), as applied above to claims 42-52 and 71-82, further, in view of P. Khadka et al. (Asian Journal of Pharmaceutical Sciences, Volume 9, Issue 6, 2014, Pages 304-316, ISSN 1818-0876, doi.org/10.1016/j.ajps.2014.05.005, “Khadka” cited in the PTO-892). Although the claims at issue are not identical, they are not patentably distinct from each other because:
Instant claims 53-57, 71-75, and 78-82 recite that the particle size diameter [d90] of the unit dosage form, is less than about 30 µm. and a solid preparation of the compound above in an amount of about 30% to about 50% w/w (e.g., 40%), and at least one pharmaceutically acceptable excipient.
As discussed above, Copending application 17/607,090, Remington, and Filloon teaches a unit dosage form comprising 5-[[(2S)-1-(3-oxo-3-[4-[5- (trifluoromethyl)pyrimidin-2-yl]piperazin-1-yl]propoxy)propan-2-yl] amino]-4-(trifluoromethyl)-2,3-dihydropyridazin-3-one, or a pharmaceutically acceptable salt thereof, in a therapeutically effective amount, e.g., 25-500 mg. However, the combination of U.S. Patent No. 11,566,020 B1, Remington, and Filloon do not teach that the solid PARP7 inhibitor has a particle size diameter of less than 30 µm, or particle size diameter of about 1-20 µm.
Khadka’s teachings are as discussed above and are incorporated herein by reference.
The obviousness rationale is similar to the obviousness rationale of claims 53-57 and 71-75, 78-82 of the Double Patenting Rejection above.
This is a provisional nonstatutory double patenting rejection because the patentably indistinct claims have not in fact been patented.
Double Patenting over Copending application 18/654,312
Claims 42-57 and 71-82 are provisionally rejected on the ground of nonstatutory double patenting as being unpatentable over claims 1-7, 27-32, and 34-41 of Copending application 18/654,312 (US 2025/0064803 A1). Although the claims at issue are not identical, they are not patentably distinct from each other because:
Instant claims 42-52 and 76-77 recites “a unit dosage form comprising 5-[[(2S)-1-(3-oxo-3-[4-[5- (trifluoromethyl)pyrimidin-2-yl]piperazin-1-yl]propoxy)propan-2-yl] amino]-4-(trifluoromethyl)-2,3-dihydropyridazin-3-one, or a pharmaceutically acceptable salt thereof, in an amount of about 25 mg to about 500 mg, measured as the free base and a solid pharmaceutical formulation comprising the compound 5-[[(2S)-1-(3-oxo-3-[4-[5-(trifluoromethy]l)pyrimidin-2-yl]piperazin-1-yl]propoxy )propan-2-yl]amino]-4-(trifluoromethyl )-2,3-dihydropyridazin-3-one, or a pharmaceutically acceptable salt thereof, in an amount of about 30% to about 50% w/w (e.g., 40%), and at least one pharmaceutically acceptable excipient, wherein the particle size diameter [d90] of the unit dosage form, is less than about 30 µm, and a solid preparation of the compound above in an amount of about 30% to about 50% w/w (e.g., 40%), and at least one pharmaceutically acceptable excipient.” The structure of claims 42 compound is shown below:
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Copending application 18/654,312 recites in conflicting claims 1 and 21 “a method for treating cancer in a subject, wherein the method comprises administering to the subject the compound 5-[[(2S)-1-(3-oxo-3-[4-[5-(trifluoromethyl)pyrimidin- 2-yl]piperazin- 1 -yl]propoxy)propan-2-yl]amino] -4-(trifluoromethyl)-2,3-dihydropyridazin-3- one, or a pharmaceutically acceptable salt thereof, at a total daily dosage of about 50 mg to about 1000 mg, measured as the free base, wherein the compound, or pharmaceutically acceptable salt thereof, is administered at a total daily dosage of about 50 mg, 100 mg, 200 mg, 400 mg, or 600 mg measured as the free base, wherein the compound, or a pharmaceutically acceptable salt thereof, is administered orally, wherein the compound, or a pharmaceutically acceptable salt thereof, is administered as an oral unit dosage form, wherein the oral unit dosage form is in the form of a capsule or tablet, wherein the compound, or a pharmaceutically acceptable salt thereof, has a particle diameter [d90] of less than about 30 pm, about 1 to about 20 pm, about 5 to about 15 pm, about 7 to about 12 pm, of about 8, 9, 10, or 11 pm:
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Copending application 18/654,312 dosage anticipates claims 42-57 and 71-82. Please note that Copending application 18/654,312 teaches therapeutic effective amount of the same compound for treating the same conditions, for example, instant claimed compound and Copending application 18/654,312 compound are directed to treating cancer.
This is a provisional nonstatutory double patenting rejection because the patentably indistinct claims have not in fact been patented.
Conclusion
Claims 42-57 and 71-82 are rejected.
Any inquiry concerning this communication or earlier communications from the examiner should be directed to MANAHIL MIRGHANI ALI ABDALHAMEED whose telephone number is (571)272-1242. The examiner can normally be reached M-F 7:30 am - 5:00 pm.
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/M.M.A./Examiner, Art Unit 1622
/JAMES H ALSTRUM-ACEVEDO/Supervisory Patent Examiner, Art Unit 1622
1 A notice of allowance in this co-pending application was mailed on March 18, 2025. This rejection will become non-provisional when this application issues as a US Patent.