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 05/03/2024, is a continuation of U.S. provisional application No. 18/371,626 filed on 09/22/2023, which is a continuation of U.S. Patent Application No. 17/671,714, filed on 02/15/2022, which claims priority to U.S. provisional application No. 63/275,163 filed on 11/03/2021 and U.S. provisional application No. 63/149,901, filed on 02/16/2021.
Information Disclosure Statement
The information disclosure statement (IDS) filed on 11/14/2024, 07/02/2025, 12/12/2025 and 05/28/2026, 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.
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and the fee set forth in 37 CFR 1.17(e) has been timely paid, the finality of the previous Office action has been withdrawn pursuant to 37 CFR 1.114.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 on 05/27/2026 has been entered.
DETAILED ACTION
The Applicant’s amendment and arguments filed on 05/27/2026 have been received and have been fully considered. Claim 1 was amended, claim 33 was cancelled, claims 2-4, 7-28, 31-32, 34-39 and 42-109 were previously cancelled, and claims 110-120 were added.
Claims 1, 5-6, 29-30, 40-41 and 110-120 are pending.
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 form”
Claims 35 and 36 recite “a unit dosage form”. The unit dosage will be interpreted as a pharmaceutical composition, for example a capsule or tablet.
Rejections - Withdrawn
Withdrawn Claim Rejections - 35 USC § 103
Rejection to claims 1, 5-6, 29-30, 33 and 40-41 under 35 U.S.C. 103 as being unpatentable over M. Vasbinder et al. (US PG-PUB 2022/0162196 A1, 05/26/2022) in view of P. Khadka et al. (Asian Journal of Pharmaceutical Sciences, Volume 9, Issue 6, 2014, Pages 304-316, ISSN 1818-0876), is withdrawn in view of Applicant’s arguments that Khadka’s document recommends reducing the particle size to below 1 µm and to nanomolar size range, whereas the claimed particle size is 5-15 µm.
Rejections New in view of the Amendments
Claim Rejections - 35 USC § 112 (a)
The following is a quotation of the first paragraph of 35 U.S.C. 112(a):
(a) IN GENERAL.—The specification shall contain a written description of the invention, and of the manner and process of making and using it, in such full, clear, concise, and exact terms as to enable any person skilled in the art to which it pertains, or with which it is most nearly connected, to make and use the same, and shall set forth the best mode contemplated by the inventor or joint inventor of carrying out the invention.
The following is a quotation of the first paragraph of pre-AIA 35 U.S.C. 112:
The specification shall contain a written description of the invention, and of the manner and process of making and using it, in such full, clear, concise, and exact terms as to enable any person skilled in the art to which it pertains, or with which it is most nearly connected, to make and use the same, and shall set forth the best mode contemplated by the inventor of carrying out his invention.
Claims 1, 5-6, 29-30, 40-41 and 110-120 are rejected under 35 U.S.C. 112(a) or 35 U.S.C. 112 (pre-AIA ), first paragraph, because the specification, while being enabling for treating non-small cell lung carcinoma (NSCLC)1, does not reasonably provide enablement for the treatment of head and neck cancer, breast cancer, large intestine cancer, pancreatic cancer, colon cancer, esophageal cancer, prostate cancer, stomach cancer, and a cancer in which PARP7 expression is amplified. The specification does not enable any person skilled in the art to which it pertains, or with which it is most nearly connected, to use the invention commensurate in scope with these claims.
As a general rule, enablement must be commensurate with the scope of claim language. MPEP 2164.08 states, “The Federal Circuit has repeatedly held that “the specification must teach those skilled in the art how to use the full scope of the claimed invention without undue experimentation.” In re Wright, 999 F.2d 1557, 1561, 27 USPQ2d 1510, 1513 (Fed. Cir. 1993)”. The “use the full scope of the invention without undue experimentation” language was repeated in 2005 in Warner-Lambert Co. v. Teva Pharmaceuticals USA Inc., 75 USPQ2d 1865, and Scripps Research Institute v. Nemerson, 78 USPQ2d 1019 asserts: “A lack of enablement for the full scope of a claim, however, is a legitimate rejection.” The principle was explicitly affirmed most recently in Liebel-Flarsheim Co. v. Medrad, Inc. 481 F.3d 1371, 82 USPQ2d 1113; Auto. Tech. Int’l, Inc. v. BMW of N. Am., Inc., 501 F.3d 1274, 84 USPQ2d 1108 (Fed. Cir. 2007), Monsanto Co. v. Syngenta Seeds, Inc., 503 F.3d 1352, 84 U.S.P.Q.2d 1705 (Fed. Cir. 2007), and Sitrick v. Dreamworks, LLC, 516 F.3d 993, 85 USPQ2d 1826 (Fed. Cir. 2008).
By way of background, four cases are of particular relevance to the question of enablement of a method of treating cancers broadly or even generally:
In In re Buting, 57 CCPA 777, 418 F.2d 540, 163 USPQ 689, the claim was drawn to “The method of treating a malignant condition selected from the group consisting of leukemias, sarcomas, adenocarcinomas, lymphosarcomas, melanomas, myelomas, and ascitic tumors” using a small genus of compounds. The Court decided that human testing “limited to one compound and two types of cancer” was not “commensurate with the broad scope of utility asserted and claimed”.
In Ex parte Jovanovics, 211 USPQ 907 the claims were drawn to “the treatment of certain specified cancers in humans” by the use of a genus of exactly two compounds, the N-formyl or N-desmethyl derivative of leurosine. Applicants submitted “affidavits, publications and data” for one of the compounds, and a dependent claim drawn to the use of that species was allowed. For the other, no data was presented, applicants said only that the other derivative would be expected to be less effective; claims to the genus were refused.
In Ex parte Busse, et al., 1 USPQ2d 1908, claims were drawn to “A therapeutic method for reducing metastasis and neoplastic growth in a mammal” using a single species. The decision notes that such utility “is no longer considered to be “incredible””, but that “the utility in question is sufficiently unusual to justify the examiner's requirement for substantiating evidence.” Note also that there is also a dependent claim 5 which specified “wherein metastasis and neoplastic growth is adenocarcinoma, squamous cell carcinoma, melanoma, cell small lung or glioma.” The decision notes that “even within the specific group recited in claim 5 some of the individual terms used actually encompass a relatively broad class of specific types of cancer, which specific types are known to respond quite differently to various modes of therapy.”
In Ex parte Stevens, 16 USPQ2d 1379 a claim to “A method for therapeutic or prophylactic treatment of cancer in mammalian hosts” was refused because there was “no actual evidence of the effectiveness of the claimed composition and process in achieving that utility.”
Pursuant to In re Wands, 858 F.2d 731, 737, 8 USPQ2d 1400, 1404 (Fed. Cir. 1988), one considers the following factors to determine whether undue experimentation is required:
(1) The breadth of the claims
(2) The nature of the invention
(3) The state of the prior art
(4) The level of one of ordinary skill
(5) The level of predictability in the art
(6) The amount of direction provided by the inventor
(7) The existence of working examples
(8) The quantity of experimentation needed to make or use the invention based on the content of the disclosure.
Some experimentation is not fatal; the issue is whether the amount of experimentation is “undue”; see In re Vaeck, 20 USPQ2d 1438, 1444.
The analysis is as follows:
(1) The breadth of the claims:
The presently claimed invention is directed to 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 400 mg to about 600 mg, measured as the free base, wherein the compound, or the pharmaceutically acceptable salt thereof, is administered as an oral unit dosage form in the form of a tablet twice daily; and wherein the particle size diameter [d90] of the compound, or pharmaceutically acceptable salt thereof, is about 5 to about 15 pm; and wherein the cancer is selected from lung cancer, head and neck cancer, breast cancer, large intestine cancer, pancreatic cancer, colon cancer, esophageal cancer, prostate cancer, stomach cancer, and a cancer in which PARP7 expression is amplified.
Cancer is not a single disease, or a cluster of closely related disorders. There are hundreds of proliferative diseases, which have in common only some loss of controlled cell growth. Cancers are highly heterogeneous at both the molecular and clinical level, something seen especially in, for example, the cancers of the breast, brain, and salivary glands. They can occur in every part of the body. The specification and the art of record fail to disclose a validated marker or method for predicting a benefit from the instantly claimed compound. Therefore, the scope of the diseases covered is deemed very broad, and cannot be considered enabled by the instant specification. In addition, treating a cancer encompasses thousands of anti-cancer/antitumor agents under the classes such as small molecular chemotherapy, antitumor antibiotic substance, a platinum-based agent etc. is deemed very broad, and cannot be considered enabled by the instant specification.
(2) The nature of the invention:
The present claims describe a method for treating lung cancer, head and neck cancer, breast cancer, large intestine cancer, pancreatic cancer, colon cancer, esophageal cancer, prostate cancer, stomach cancer, and a cancer in which PARP7 expression is amplified. That is, in order to be enabled to practice the present invention, the skilled artisan would have to accept that by administering 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 to a cancer patient that such therapeutic objectives could actually be achieved. However, in light of the fact that the specification fails to provide the skilled artisan with any direction or guidance as to how the treatment of these cancers in general could be achieved, or how the 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 dose or regimen will be selected for treating any particular kind of cancer, the present specification is viewed as lacking an enabling disclosure of the entire scope of the claimed invention.
(3) The state of the Prior Art:
The instant claims are directed to a method for treating cancer in a subject by administering 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, wherein the cancer is selected from lung cancer, head and neck cancer, breast cancer, large intestine cancer, pancreatic cancer, colon cancer, esophageal cancer, prostate cancer, stomach cancer, and a cancer in which PARP7 expression is amplified. However, as taught by Chakraborty (S. Chakraborty, et al. Ecancermedicalscience. 2012, 14;6:ed16. doi: 10.3332/ecancer.2012.ed16), “the cure for cancer is like the Holy Grail since most of the existing treatments are not effective enough to provide full protection from this disease”. Chakraborty teaches that “in recent years the burgeoning of sophisticated genomic, proteomic and bioinformatics techniques has made it possible for us to get a glimpse of the intricate interplay of numerous cellular genes and regulatory genetic elements that are responsible for the manifestation of cancerous phenotypes. With the use of modern genomic technologies, we are now beginning to understand the enormous complexity of cancer, however, there are few success stories as far as the treatment of cancer is concerned, [Abstract]. Chakraborty teaches that the non-specific nature of cancer symptoms makes diagnosis difficult (let alone treatment). Chakraborty teaches examples of cancer with diagnosis difficulties include esophageal cancer, prostate cancer, and pancreatic cancer. [Page 3-4]. Numerous mechanisms have been proposed as methods of treating assorted cancers a selection of which follow. Cytotoxic agents could be applied directly to the tumor’s cells, directly killing them. Immunotherapy to stimulate the patient's immune system to attack cancer cells, either by immunization of the patient, in which case the patient's own immune system is trained to recognize tumor cells as targets, or by the administration of therapeutic antibodies as drugs, so the patient's immune system is recruited to destroy tumor cells by the therapeutic antibodies. Increasing the amount or activity of the body’s tumor suppressor genes, PTEN, APC and CD95, which can, for example, activate DNA repair proteins, suppress the Akt/PKB signaling pathway, or initiate apoptosis of cancer cells. Angiogenesis inhibitor strategies based on cutting off the blood supply that growing tumors need by shutting off the growth of new blood vessels by, for example, suppressing proliferation of endothelial cells or inducing apoptosis of endothelial cells.
A number of these approaches – and others as well – have produced anti-cancer drugs. However, despite high hopes for success, and a plausible theory why these should work for cancers generally, these approaches have yet to produce a drug which can claim such a goal.
Specifically, the prior art demonstrates that there never has been a compound capable of treating cancers generally or multiple mechanistically diverse cancer types. “The cancer therapy art remains highly unpredictable, and no example exists for efficacy of a single product against tumors generally.” A similar statement appears at In re Application of Hozumi et al., 226 USPQ 353: “In spite of the vast expenditure of human and capital resources in recent years, no one drug has been found which is effective in treating all types of cancer. Cancer is not a simple disease, nor is it even a single disease, but a complex of a multitude of different entities, each behaving in a different way”. There are compounds that treat a modest range of cancers, but no one has ever been able to determine how to get a compound to be effective against cancer generally, or even a majority of cancers.
The attempts to find compounds to treat the various cancers arguably constitute the single most massive enterprise in all of pharmacology. This has not resulted in finding any treatment for tumors generally, and the existence of such a single treatment for cancer is contrary to our present understanding in oncology. This is because it is now understood that there is no “master switch” for cancers generally; cancers arise from an exceptionally wide variety of differing mechanisms. Even the most broadly effective antitumor agents are only effective against a small fraction of the vast number of different cancers known. This is true in part because cancers arise from a wide variety of sources, primarily a wide variety of failures of the body's cell growth regulatory mechanisms, but also such external factors such as viruses, exposure to environmental chemicals (e.g. tobacco tars, alcohol, toxins), ionizing radiation, and unknown environment factors.
Accordingly, there is substantive “reason for one skilled in the art to question the objective truth of the statement of utility or its scope” (In re Langer, 183 USPQ 288, 297), specifically, the scope of covering all the claimed cancers.
Similarly, In re Novak, 134 USPQ 335, 337-338, says “unless one with ordinary skill in the art would accept those allegations as obviously valid and correct, it is proper for the examiner to ask for evidence which substantiates them.” There is no such evidence in this case. Likewise, In re Cortright, 49 USPQ2d 1464, states: “Moreover, we have not been shown that one of ordinary skill would necessarily conclude from the information expressly disclosed by the written description that the active ingredient” does what the specification surmises that it does. That is exactly the case here. Moreover, even if applicants’ assertion that cancer in general could be treated with these compounds were plausible, which it is not, that “plausible” would not suffice, as was stated in Rasmusson v. SmithKline Beecham Corp., 75 USPQ2d 1297, 1301: “If mere plausibility were the test for enablement under section 112, applicants could obtain patent rights to “inventions” consisting of little more than respectable guesses as to the likelihood of their success.”
(4) The skill of those in the art:
The skill of those in the art is expected to be high, requiring advanced training in chemistry, medicine, or pharmacology.
(5) The level of predictability in the art:
With specific reference to cancer, Ex parte Kranz, 19 USPQ2d 1216, 1219 notes the “general unpredictability of the field [of] …anti-cancer treatment.” In re Application of Hozumi et al., 226 USPQ 353 notes the “fact that the art of cancer chemotherapy is highly unpredictable”. More generally, the invention is directed toward medicine and is therefore physiological in nature. It is well established that “the scope of enablement varies inversely with the degree of unpredictability of the factors involved,” and physiological activity is generally considered to be an unpredictable factor. See In re Fisher, 427 F.2d 833, 839, 166 USPQ 18, 24 (CCPA 1970).
With this in mind the level of predictability in the art is sufficiently low that even with hundreds of successful examples of chemotherapy there has yet to be shown any single method of treating the vast scope of cancers known. The level of unpredictability in the art renders the scope of instant claim to be not enabled.
(6) The amount of direction provided/ (7) Working examples:
While the treatment of cancers, lung cancer, head and neck cancer, breast cancer, large intestine cancer, pancreatic cancer, colon cancer, esophageal cancer, prostate cancer, stomach cancer, and a cancer in which PARP7 expression is amplified, is discussed in broad terms, the necessary specifics for each cancer type, i.e. dosing, therapeutic index, contraindications, interaction between the claimed compound with other antitumor agents, etc., are completely absent. And while the anti-cancer agent therapy is discussed in board term the, the specification does not provide testing and examples for the claimed compound against each claimed cancer type. There are prophetic studies include dose escalation phase, relative bioavailability, dose expansion phase, on squamous cell carcinoma of the lung (SCCL), head and neck squamous cell carcinoma (HNSCC), HR+ breast cancer, and PARP7 amplified cancer [page 21-24]. The specification provides no results or discussion of the effectiveness of the claimed compound on these cancer types. The majority of examples are directed to dosing, toxicity and pharmacokinetics of compound 1. Note that Example E discussed clinical study on SCCL [page 29-30], however the study is a combination with pembrolizumab. Skilled artisan would not definitively determine the effectiveness of the claimed compound on SCCL. The limited prophetic studies do very little to provide the necessary information, and, in light of the immense diversity of types of cancers and their varied reactions to treatment, the guidance provided is very limited. The exceptional diversity of cancers, and the treatment of them, is not well represented by these examples. It is well known that there is no single treatment that works for all kinds of cancers, so the experimentation required, based on solely limited cell line assays to practice the instant invention would be egregious.
(8) The quantity of experimentation needed:
Given the fact that, historically, the development of new cancer drugs has been difficult and time consuming, and especially in view of the above factors, the quantity of experimentation needed is expected to be great. However, the quantity needed to expand limited cell line assays as a working example provided in the instant specification to a viable treatment for the claimed scope of cancer or tumor is untenable.
MPEP 2164.01(a) states, “A conclusion of lack of enablement means that, based on the evidence regarding each of the above factors, the specification, at the time the application was filed, would not have taught one skilled in the art how to make and/or use the full scope of the claimed invention without undue experimentation. In re Wright, 999 F.2d 1557, 1562, 27 USPQ2d 1510, 1513 (Fed. Cir. 1993).” That conclusion is clearly justified here.
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 non-obviousness.
35 USC § 103 over Vasbinder II in view of Kuriyama, Shyamal and Gil
Claims 1, 5-6, 29-30, 40-41 and 110-120 are rejected under 35 U.S.C. 103 as being unpatentable over M. Vasbinder et al. (US PG-PUB 2022/0162196 A1, 05/26/2022, (effective filing date 04/28/2020) “Vasbinder II” cited in the previous PTO-892 dated 08/13/2025) in view of M. Gil et al. (USPN 9956144B2, 05/01/2018, “Gil” cited in the PTO-892), Kuriyama A, et al. (AAPS PharmSciTech. 2014 Apr;15(2):375-87, “Kuriyama” cited in the PTO-892) and Shyamal C. et al. (Powder Technology, 2013, Volume 249, Pages 297-303, ISSN 0032-5910, “Shyamal” cited in the PTO-892).
Prior art effect of Vasbinder II
The applied reference, Vasbinder II, has a common Assignee and Inventor with the instant application. Based upon the earlier effectively filed date of the reference, it constitutes prior art under 35 U.S.C. 102(a)(2). This rejection under 35 U.S.C. 102 might be overcome by: (1) a showing under 37 CFR 1.130(a) that the subject matter disclosed in the reference was obtained directly or indirectly from the inventor or a joint inventor of this application and is thus not prior art in accordance with 35 U.S.C.102(b)(2)(A); (2) a showing under 37 CFR 1.130(b) of a prior public disclosure under 35 U.S.C. 102(b)(2)(B); or (3) a statement pursuant to 35 U.S.C. 102(b)(2)(C) establishing that, not later than the effective filing date of the claimed invention, the subject matter disclosed and the claimed invention were either owned by the same person or subject to an obligation of assignment to the same person or subject to a joint research agreement. See generally MPEP § 717.02. 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. This will be applied to this 102 and the following103 rejections herein.
Vasbinder II discloses a method of treating cancer in a subject in need thereof, the method comprising administering to the subject a therapeutically effective amount of PARP7 inhibitor, compound 1 (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), [Pg. 7, [0094] and claims 1 and 23 and 24]:
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wherein said cancer is breast cancer, large intestine cancer, lung cancer, esophagus cancer, pancreatic cancer, prostate cancer, stomach cancer, head and neck cancer or colon cancer. [0095, claim 24]. Vasbinder II discloses that the above PARP7 inhibitor is effective in treating non-small lung cancer, [0178], wherein the cancer is associated with abnormal expression or activity of PARP7. [0095].
Vasbinder II discloses that compound 1 or salts and solid forms thereof can be administered in the form of pharmaceutical compositions of Compound 1 or salts and solid forms thereof, and at least one pharmaceutically acceptable carrier, wherein the composition in the form of tablets or pills and can be administered orally, [Pg. 9, [0112]- [0113]]. Vasbinder II discloses examples wherein compound 1 is administered orally once and twice a day at a dose of 500 mg. [Pg. 20, [0180]-[0181]]. Vasbinder II discloses that compound 1 is also administered in doses of 62.5, 125, 250 and 500 mg. [Pg. 20, [0180]].
However, Vasbinder II does not teach that the compound or pharmaceutically acceptable salt has a particle size diameter of about 5 to about 15 µm.
Kuriyama teaches assessment of the size of the micrometer-scale active pharmaceutical ingredients (API). Kuriyama teaches that particle size is a critical parameter for controlling pharmaceutical quality. Kuriyama teaches that the particle size of tablets of National Institute of Standards and Technology is 5, 10, and 15 μm prepared using a commercial tablet formulation. Kuriyama teaches that these three set, 5, 10, and 15 μm showed good agreement between pre- and post-formulation, tablet surface roughness, and good applicability. [Abstract]. Kuriyama teaches that particle size of API controls the dissolution rate, bioavailability, and stability of the final product, and that the size of ingredient particles is a critical process parameter for ensuring product quality. [page 375, col. 1]. Kuriyama teaches that the particle sizes were 98% for the 5 μm PS microspheres, 96% for the 10 μm PS microspheres, and 101% for the 15 μm PS microspheres. [page 381, col. 1, 2nd para.].
Moreover, Shyamal teaches the importance of particle size on de-agglomeration of cohesive powders of pharmaceutical preparation, wherein the packing fraction was dependent on particle size of between 5.4 and 14 μm. [Abstract]. Shyamal teaches that particles less than 14 μm was chosen because a cohesive particle fraction that showed better de-agglomeration previously had 90% of particles less than 14 μm [page 300, col. 1 last para.]. Shyamal teaches the significant advantages of the particle size between 5.4-14 μm. [page 302, col. 2, last para., 303, col. 1].
Furthermore, Gil teaches a process of reducing particle size of pharmaceutical active ingredients [Abstract]. Gil teaches that “the particle size reduction of active pharmaceutical ingredients is a key unit operation in the pharmaceutical industry”. [col. 2, 4th para.]. Gil teaches that particle size reduction produces powders characterized by high particle fraction necessary for drug delivery without the necessity for stabilizing additives, making this method especially suitable for the manufacturing formulation. [col. 2, 2nd para.]. Gil teaches that the particle size is measure by span value of Dv90-Dv10/Dv50 of less than 2.0. [col. 4, 1st para.]. Gil teaches in Example 1 particle size Dv90 of 7.47.
Therefore, in view of Kuriyama, Shyamal and Gil, it would have been prima facie obvious to one of ordinary skill in the art prior to the effective filing date of instantly claimed invention to reduce the particle size of Vasbinder II’s compound 1 above to about 5-10 µm. One of ordinary skill would have been motivated to do so with reasonable expectation of success because Kuriyama teaches that particle size is a critical parameter for controlling pharmaceutical quality and ensuring product quality, controls the dissolution rate, bioavailability, and stability of the final product, and that the size of ingredient particles is a critical process parameter for. [page 375, col. 1], Kuriyama selected particle sizes, 5, 10 and 15 µm based on National Institute of Standards and Technology [page 376, col. 2, 1st para.], Kuriyama teaches that reducing particle size to 5, 10, and 15 μm showed good tableting properties and good applicability; Shyamal teaches the advantages of reducing particle size of API to between 5.4 and 14 μm, and teaches that reducing particle size of API to 90% of particles less than 14 μm control packing fraction and showed better de-agglomeration and a cohesive particle fraction, and Gil teaches that the particle size reduction of active pharmaceutical ingredients to Dv90-Dv10/Dv50 of less than 2.0, e.g., Dv90 of 7.47 is a key unit operation in the pharmaceutical industry to produce powders with good particle fraction, drug delivery properties, and stability. One of ordinary skill in the art would have been motivated to reduce the particle size of Vasbinder II’s PARP7 inhibitor, Compound 1 above to 5-15 μm because according to Vasbinder II, Compound 1 is an active compound for the treatment of cancer by inhibiting PARP7 and Kuriyama, Shyamal and Gil provide the motivation to reduce the particle size of active pharmaceutical ingredients.
Therefore, claims 1, 40-41 and 110-120 are prima facie obvious over Vasbinder II, Kuriyama, Shyamal and Gil.
With regard to claims 5, 6, 29, 30, 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 II’s dosing range of 0.1-500 mg of PARP7 inhibitor to about 400 mg, 600 mg, 200 mg, 300 mg daily doses of the PARP7 inhibitor measured as free base in view of the teachings of Vasbinder II. One of ordinary skill in the art is motivated to do so with reasonable expectation of success because Vasbinder II discloses that compound 1 is administered at doses of 125, 250 and 500 mg twice daily [Pg. 20, [0180], [0181]]; Vasbinder II discloses that compound 1 can be subdivided into unit dosage forms containing from 0.1 to about 500 mg [Pg. 9, [0116]]; Vasbinder II discloses that compound 1 can be effective over a wide dosage range; Vasbinder II discloses that compound 1 is administered in a pharmaceutically effective amount that 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. 9, [0115]]. Moreover, Vasbinder II discloses dosing ranges that encompasses and overlapped with the claims’ ranges, and 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 5, 6, 29, 30 are obvious over Vasbinder II.
35 USC § 103 over Vasbinder in view of Kuriyama, Shyamal and Gil
Claims 1, 5-6, 29-30, 40-41 and 110-120 are rejected under 35 U.S.C. 103 as being unpatentable over M. Vasbinder et al. (US PG-PUB 2019/0330194 A1, 10/31/2019, “Vasbinder” cited in the previous PTO-892 dated 08/13/2025) in view of M. Gil et al. (USPN 9956144B2, 05/01/2018, “Gil” cited in the PTO-892), Kuriyama A, et al. (AAPS PharmSciTech. 2014 Apr;15(2):375-87, “Kuriyama” cited in the PTO-892) and Shyamal C. et al. (Powder Technology, 2013, Volume 249, Pages 297-303, ISSN 0032-5910, “Shyamal” cited in the PTO-892).
Vasbinder teaches a method of treating cancer in a subject in need thereof, the method comprising administering to the subject a therapeutically effective amount of an agent that inhibits PARP7 activity, such as a compound of Formula I, or a pharmaceutically acceptable salt thereof. [0013]. Vasbinder teaches the claimed compound as species of Formula I in Table E11 [Pg. 370, Table E11, Ln. 1], and in Vasbinder’s claims 444-451, as Vasbinder’s document claims the compound and its pharmaceutical compositions:
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wherein the cancer is breast cancer, large intestine cancer, lung cancer, esophagus cancer, pancreatic cancer, prostate cancer, stomach cancer, head and neck cancer or colon cancer, wherein the cancer is associated with abnormal expression or activity of PARP7. [[0524]-[0527]]. Vasbinder discloses that the compound is effective in treating is non-small lung cancer, [[2108], Table A-2].
Vasbinder teaches pharmaceutical formulations and dosage forms of the above PARP7 inhibitor and pharmaceutical excipient, wherein the formulation is for oral administration, wherein the composition can be formulated in a unit dosage form, wherein 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, [0540], [542], [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; 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; and 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]].
Vasbinder teaches that the PARP7 inhibitors, i.e., compound 664, are administered once or twice daily. [Pg. 397, [2117]].
As such, Vasbinder teaches a method of treating cancer associated with overexpression of PARP7 comprising administering dose ranges of about 0.01 mg/kg to about 100 mg/kg, and 0.1 to about 500 mg administered once or twice daily. 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 daily dosage is about 400-600 mg, or the subdivided doses of 200 mg, 300 mg, 400 mg or 600 mg. Vasbinder does not teach that the compound of pharmaceutically acceptable salt has a particle size diameter of about 5 to about 15 µm.
Kuriyama, Shyamal and Gil teach as discussed above, pages 6-7.
Therefore, in view of Kuriyama, Shyamal and Gil, it would have been prima facie obvious to one of ordinary skill in the art prior to the effective filing date of instantly claimed invention to reduce the particle size of Vasbinder’s compound 1 above to about 5-10 µm. One of ordinary skill would have been motivated to do so with reasonable expectation of success because Kuriyama teaches that particle size is a critical parameter for controlling pharmaceutical quality and ensuring product quality, controls the dissolution rate, bioavailability, and stability of the final product, and that the size of ingredient particles is a critical process parameter for. [page 375, col. 1], Kuriyama selected particle sizes, 5, 10 and 15 µm based on National Institute of Standards and Technology [page 376, col. 2, 1st para.], Kuriyama teaches that reducing particle size to 5, 10, and 15 μm showed good tableting properties and good applicability; Shyamal teaches the advantages of reducing particle size of API to between 5.4 and 14 μm, and teaches that reducing particle size of API to 90% of particles less than 14 μm control packing fraction and showed better de-agglomeration and a cohesive particle fraction, and Gil teaches that the particle size reduction of active pharmaceutical ingredients to Dv90-Dv10/Dv50 of less than 2.0, e.g., Dv90 of 7.47 is a key unit operation in the pharmaceutical industry to produce powders with good particle fraction, drug delivery properties, and stability. One of ordinary skill in the art would have been motivated to reduce the particle size of Vasbinder’s PARP7 inhibitor, Compound 1 above to 5-15 μm because according to Vasbinder, Compound 1 is an active compound for the treatment of cancer by inhibiting PARP7 and Kuriyama, Shyamal and Gil provide the motivation to reduce the particle size of active pharmaceutical ingredients.
With regard to the claimed daily dosage of about 400-600 mg, or the subdivided doses of 200 mg, 300 mg, 400 mg or 600 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 400-600 mg, or the subdivided doses of 200 mg, 300 mg, 400 mg or 600 mg 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).”
Therefore, claims 1, 5-6, 29-30, 40-41 and 110-120 are prima facie obvious over Vasbinder, Kuriyama, Shyamal and Gil.
Response to Arguments
Applicant’s arguments have been considered but are moot because the new ground of rejection does not rely on Khadka reference applied in the prior rejection of record for any teaching or matter specifically challenged in the argument. Applicant’s arguments are directed mainly to 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 1, 5-6, 29-30, 40-41 and 110-120 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, “Filloon” cited in the previous PTO-892 dated 08/13/2025); Remington's Pharmaceutical science, 18th edition, Gennaro, A.R., ED, Mack Pub. Co.: Easton, PA, 1990, pp 1633-1665, “Remington”, cited in the previous PTO-892 dated 08/13/2025), M. Gil et al. (USPN 9956144B2, 05/01/2018, “Gil” cited in the PTO-892), Kuriyama A, et al. (AAPS PharmSciTech. 2014 Apr;15(2):375-87, “Kuriyama” cited in the PTO-892) and Shyamal C. et al. (Powder Technology, 2013, Volume 249, Pages 297-303, ISSN 0032-5910, “Shyamal” cited in the PTO-892). Although the claims at issue are not identical, they are not patentably distinct from each other because:
Instant claims 1, 5-6, 29-30, 40-41 and 110-120 recites “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 400 mg to about 600 mg, measured as the free base, wherein the compound, or pharmaceutically acceptable salt thereof, is administered at a total daily dosage of about 100, 200, 300, 400, 500, 600 mg, measured as the free base, wherein the compound, or the pharmaceutically acceptable salt thereof, is administered as an oral unit dosage form in the form of a tablet twice daily and wherein the particle size diameter [d90] of the compound, or pharmaceutically acceptable salt thereof, is about 5 to about 15 µm, wherein the cancer is a breast cancer, a cancer of the central nervous system, an endometrium cancer, a kidney cancer, a large intestine cancer, a lung cancer:
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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 the use of the above compound for treating cancer; the amount of the above compound in the pharmaceutical composition is about 400 mg to about 600 mg; or particle size diameter of about 5 to about 15 µm.
US Patent No. 10,550,105 B2 specification recite a method of using the above compound in treating cancer, wherein the cancer is associated with abnormal expression or activity of PARP7, wherein the cancers include multiple myeloma, DLBCL, hepatocellular carcinoma, bladder cancer, esophageal cancer, head and neck cancer (upper aerodigestive cancer), kidney cancer, prostate cancer, rectal cancer, stomach cancer, thyroid cancer, uterine cancer, and breast cancer, wherein the lung cancer is non-small cell lung cancer. [Pg. 40, col. 54, ln. 10-45, Table A-2].
MPEP 804 states: The specification can be used as a dictionary to learn the meaning of a term in the claim. Toro Co. v. White Consol. Indus., Inc., 199 F.3d 1295, 1299, 53 USPQ2d 1065, 1067 (Fed. Cir. 1999) ("[W]ords in patent claims are given their ordinary meaning in the usage of the field of the invention, unless the text of the patent makes clear that a word was used with a special meaning."); Renishaw PLC v. Marposs Societa' per Azioni, 158 F.3d 1243, 1250, 48 USPQ2d 1117, 1122 (Fed. Cir. 1998) ("Where there are several common meanings for a claim term, the patent disclosure serves to point away from the improper meanings and toward the proper meanings."). "The Patent and Trademark Office (‘PTO’) determines the scope of the claims in patent applications not solely on the basis of the claim language, but upon giving claims their broadest reasonable construction ‘in light of the specification as it would be interpreted by one of ordinary skill in the art.’ " Phillips v. AWH Corp., 415 F.3d 1303, 1316, 75 USPQ2d 1321, 1329 (Fed. Cir. 2005) (en banc) (quoting In re Am. Acad. of Sci. Tech. Ctr., 367 F.3d 1359, 1364, 70 USPQ2d 1827, 1830 (Fed. Cir. 2004); see also MPEP § 2111.01. Further, those portions of the specification which provide support for the reference claims may also be examined and considered when addressing the issue of whether a claim in the application defines an obvious variation of an invention claimed in the reference patent or application (as distinguished from an obvious variation of the subject matter disclosed in the reference patent or application). In re Vogel, 422 F.2d 438, 441-42, 164 USPQ 619, 622 (CCPA 1970). The court in Vogel recognized "that it is most difficult, if not meaningless, to try to say what is or is not an obvious variation of a claim," but that one can judge whether or not the invention claimed in an application is an obvious variation of an embodiment disclosed in the patent or application which provides support for the claim. According to the court, one must first "determine how much of the patent disclosure pertains to the invention claimed in the patent" because only "[t]his portion of the specification supports the patent claims and may be considered." The court pointed out that "this use of the disclosure is not in contravention of the cases forbidding its use as prior art, nor is it applying the patent as a reference under 35 U.S.C. 103, since only the disclosure of the invention claimed in the patent may be examined." In AbbVie Inc. v. Kennedy Institute of Rheumatology Trust, 764 F.3d 1366, 112 USPQ2d 1001 (Fed. Cir. 2014), the court explained that it is also proper to look at the disclosed utility in the reference disclosure to determine the overall question of obviousness in a nonstatutory double patenting context. See Sun Pharm. Indus., Ltd. v. Eli Lilly & Co., 611 F.3d 1381, 95 USPQ2d 1797 (Fed. Cir. 2010); Pfizer, Inc. v. Teva Pharm. USA, Inc., 518 F.3d 1353, 86 USPQ2d 1001 (Fed. Cir. 2008); Geneva Pharmaceuticals Inc. v. GlaxoSmithKline PLC, 349 F3d 1373, 1385-86, 68 USPQ2d 1865, 1875 (Fed. Cir. 2003).
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.
With respect to the particle size, Kuriyama, Shyamal and Gil teaches as discussed above, pages 15-16.
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., 400mg-600mg 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).”
One of ordinary skill in the art would have been motivated to reduce the particle size of US Patent No 10550105B2 compound of claim 1 to about 5-10 µm with reasonable expectation of success because Kuriyama teaches that particle size is a critical parameter for controlling pharmaceutical quality and ensuring product quality, controls the dissolution rate, bioavailability, and stability of the final product, and that the size of ingredient particles is a critical process parameter for. [page 375, col. 1], Kuriyama selected particle sizes, 5, 10 and 15 µm based on National Institute of Standards and Technology [page 376, col. 2, 1st para.], Kuriyama teaches that reducing particle size to 5, 10, and 15 μm showed good tableting properties and good applicability; Shyamal teaches the advantages of reducing particle size of API to between 5.4 and 14 μm, and teaches that reducing particle size of API to 90% of particles less than 14 μm control packing fraction and showed better de-agglomeration and a cohesive particle fraction, and Gil teaches that the particle size reduction of active pharmaceutical ingredients to Dv90-Dv10/Dv50 of less than 2.0, e.g., Dv90 of 7.47 is a key unit operation in the pharmaceutical industry to produce powders with good particle fraction, drug delivery properties, and stability. One of ordinary skill in the art would have been motivated to reduce the particle size of US Patent No 10550105B2 compound of claim 1 to 5-15 μm because according to US Patent No 10550105B2, compound of claim 1 is an active compound for the treatment of cancer by inhibiting PARP7 and Kuriyama, Shyamal and Gil provide the motivation to reduce the particle size of active pharmaceutical ingredients. Therefore, claims 1, 40-41 and 110-120 are prima facie obvious over US Patent No. 10,550,105 B2, Remington, Filloon, Kuriyama, Shyamal and Gil.
Double Patenting over U.S. Patent No. 10,870,641 B2
Claims 1, 5-6, 29-30, 40-41 and 110-120 are rejected on the ground of nonstatutory double patenting as being unpatentable over claims 1-30 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, “Filloon” cited in the previous PTO-892 dated 08/13/2025); Remington's Pharmaceutical science, 18th edition, Gennaro, A.R., ED, Mack Pub. Co.: Easton, PA, 1990, pp 1633-1665, “Remington”, cited in the previous PTO-892 dated 08/13/2025), M. Gil et al. (USPN 9956144B2, 05/01/2018, “Gil” cited in the PTO-892), Kuriyama A, et al. (AAPS PharmSciTech. 2014 Apr;15(2):375-87, “Kuriyama” cited in the PTO-892) and Shyamal C. et al. (Powder Technology, 2013, Volume 249, Pages 297-303, ISSN 0032-5910, “Shyamal” cited in the PTO-892). Although the claims at issue are not identical, they are not patentably distinct from each other because:
Instant claims 1, 5-6, 29-30, 40-41 and 110-120 recites “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 400 mg to about 600 mg, measured as the free base, wherein the compound, or pharmaceutically acceptable salt thereof, is administered at a total daily dosage of about 100, 200, 300, 400, 500, 600 mg, measured as the free base, wherein the compound, or the pharmaceutically acceptable salt thereof, is administered as an oral unit dosage form in the form of a tablet twice daily and wherein the particle size diameter [d90] of the compound, or pharmaceutically acceptable salt thereof, is about 5 to about 15 µm, wherein the cancer is a breast cancer, a cancer of the central nervous system, an endometrium cancer, a kidney cancer, a large intestine cancer, a lung cancer:
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U.S. Patent No. 10,870,641 B2 recites in conflicting claims 1-30 “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 recites that said cancer is breast cancer, cancer of the central nervous system, endometrium cancer, kidney cancer, large intestine cancer, lung cancer, esophagus cancer, ovarian cancer, pancreatic cancer, prostate cancer, stomach cancer, head and neck cancer (upper aerodigestive cancer), urinary tract cancer, or colon cancer.
US Patent No. 10,870,641 B2 does not recite in claims 1-30 that the therapeutically effective amount is an amount of about 400 mg to about 600 mg; or particle size diameter of about 5 to about 15 µm.
The teachings of Remington, Filloon, Kuriyama, Shyamal and Gil teaches as discussed above, pages 15-16 and 26.
The obviousness rationale is like the obviousness rationale for the Double Patenting Rejection of claims 1, 5-6, 29-30, 40-41 and 110-120 above, page 26-27, and is incorporated herein by reference as applied to the rejected claims.
Double Patenting over U.S. Patent No. 11,014,913 B2
Claims 1, 5-6, 29-30, 40-41 and 110-120 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, “Filloon” cited in the previous PTO-892 dated 08/13/2025); Remington's Pharmaceutical science, 18th edition, Gennaro, A.R., ED, Mack Pub. Co.: Easton, PA, 1990, pp 1633-1665, “Remington”, cited in the previous PTO-892 dated 08/13/2025), M. Gil et al. (USPN 9956144B2, 05/01/2018, “Gil” cited in the PTO-892), Kuriyama A, et al. (AAPS PharmSciTech. 2014 Apr;15(2):375-87, “Kuriyama” cited in the PTO-892) and Shyamal C. et al. (Powder Technology, 2013, Volume 249, Pages 297-303, ISSN 0032-5910, “Shyamal” cited in the PTO-892). Although the claims at issue are not identical, they are not patentably distinct from each other because:
Instant claims 1, 5-6, 29-30, 40-41 and 110-120 recites “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 400 mg to about 600 mg, measured as the free base, wherein the compound, or pharmaceutically acceptable salt thereof, is administered at a total daily dosage of about 100, 200, 300, 400, 500, 600 mg, measured as the free base, wherein the compound, or the pharmaceutically acceptable salt thereof, is administered as an oral unit dosage form in the form of a tablet twice daily and wherein the particle size diameter [d90] of the compound, or pharmaceutically acceptable salt thereof, is about 5 to about 15 µm, wherein the cancer is a breast cancer, a cancer of the central nervous system, an endometrium cancer, a kidney cancer, a large intestine cancer, a lung cancer:
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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 the use of the above compound for treating cancer; the amount of the above compound in the pharmaceutical composition is about 400 mg to about 600 mg; or particle size diameter of about 5 to about 15 µm.
US Patent No. 11,014,913 B2 specification recite a method of using the above compound in treating cancer, wherein the cancer is associated with abnormal expression or activity of PARP7, wherein the cancers include lung cancer, large intestine, multiple myeloma, DLBCL, hepatocellular carcinoma, bladder cancer, esophageal cancer, head and neck cancer (upper aerodigestive cancer), kidney cancer, prostate cancer, rectal cancer, stomach cancer, thyroid cancer, uterine cancer, and breast cancer. [Pg. 40, col. 54, ln. 33-64].
MPEP 804 states: The specification can be used as a dictionary to learn the meaning of a term in the claim. Toro Co. v. White Consol. Indus., Inc., 199 F.3d 1295, 1299, 53 USPQ2d 1065, 1067 (Fed. Cir. 1999) ("[W]ords in patent claims are given their ordinary meaning in the usage of the field of the invention, unless the text of the patent makes clear that a word was used with a special meaning."); Renishaw PLC v. Marposs Societa' per Azioni, 158 F.3d 1243, 1250, 48 USPQ2d 1117, 1122 (Fed. Cir. 1998) ("Where there are several common meanings for a claim term, the patent disclosure serves to point away from the improper meanings and toward the proper meanings."). "The Patent and Trademark Office (‘PTO’) determines the scope of the claims in patent applications not solely on the basis of the claim language, but upon giving claims their broadest reasonable construction ‘in light of the specification as it would be interpreted by one of ordinary skill in the art.’ " Phillips v. AWH Corp., 415 F.3d 1303, 1316, 75 USPQ2d 1321, 1329 (Fed. Cir. 2005) (en banc) (quoting In re Am. Acad. of Sci. Tech. Ctr., 367 F.3d 1359, 1364, 70 USPQ2d 1827, 1830 (Fed. Cir. 2004); see also MPEP § 2111.01. Further, those portions of the specification which provide support for the reference claims may also be examined and considered when addressing the issue of whether a claim in the application defines an obvious variation of an invention claimed in the reference patent or application (as distinguished from an obvious variation of the subject matter disclosed in the reference patent or application). In re Vogel, 422 F.2d 438, 441-42, 164 USPQ 619, 622 (CCPA 1970). The court in Vogel recognized "that it is most difficult, if not meaningless, to try to say what is or is not an obvious variation of a claim," but that one can judge whether or not the invention claimed in an application is an obvious variation of an embodiment disclosed in the patent or application which provides support for the claim. According to the court, one must first "determine how much of the patent disclosure pertains to the invention claimed in the patent" because only "[t]his portion of the specification supports the patent claims and may be considered." The court pointed out that "this use of the disclosure is not in contravention of the cases forbidding its use as prior art, nor is it applying the patent as a reference under 35 U.S.C. 103, since only the disclosure of the invention claimed in the patent may be examined." In AbbVie Inc. v. Kennedy Institute of Rheumatology Trust, 764 F.3d 1366, 112 USPQ2d 1001 (Fed. Cir. 2014), the court explained that it is also proper to look at the disclosed utility in the reference disclosure to determine the overall question of obviousness in a nonstatutory double patenting context. See Sun Pharm. Indus., Ltd. v. Eli Lilly & Co., 611 F.3d 1381, 95 USPQ2d 1797 (Fed. Cir. 2010); Pfizer, Inc. v. Teva Pharm. USA, Inc., 518 F.3d 1353, 86 USPQ2d 1001 (Fed. Cir. 2008); Geneva Pharmaceuticals Inc. v. GlaxoSmithKline PLC, 349 F3d 1373, 1385-86, 68 USPQ2d 1865, 1875 (Fed. Cir. 2003).
The teachings of Remington, Filloon, Kuriyama, Shyamal and Gil teaches as discussed above, pages 15-16 and 26.
The obviousness rationale is like the obviousness rationale for the Double Patenting Rejection of claims 1, 5-6, 29-30, 40-41 and 110-120 above, page 26-27, and is incorporated herein by reference as applied to the rejected claims.
Double Patenting over U.S. Patent No. 11,566,020 B1
Claims 1, 5-6, 29-30, 40-41 and 110-120 are rejected on the ground of nonstatutory double patenting as being unpatentable over claims 1-15 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, “Filloon” cited in the previous PTO-892 dated 08/13/2025); Remington's Pharmaceutical science, 18th edition, Gennaro, A.R., ED, Mack Pub. Co.: Easton, PA, 1990, pp 1633-1665, “Remington”, cited in the previous PTO-892 dated 08/13/2025), M. Gil et al. (USPN 9956144B2, 05/01/2018, “Gil” cited in the PTO-892), Kuriyama A, et al. (AAPS PharmSciTech. 2014 Apr;15(2):375-87, “Kuriyama” cited in the PTO-892) and Shyamal C. et al. (Powder Technology, 2013, Volume 249, Pages 297-303, ISSN 0032-5910, “Shyamal” cited in the PTO-892). Although the claims at issue are not identical, they are not patentably distinct from each other because:
Instant claims 1, 5-6, 29-30, 40-41 and 110-120 recites “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 400 mg to about 600 mg, measured as the free base, wherein the compound, or pharmaceutically acceptable salt thereof, is administered at a total daily dosage of about 100, 200, 300, 400, 500, 600 mg, measured as the free base, wherein the compound, or the pharmaceutically acceptable salt thereof, is administered as an oral unit dosage form in the form of a tablet twice daily and wherein the particle size diameter [d90] of the compound, or pharmaceutically acceptable salt thereof, is about 5 to about 15 µm, wherein the cancer is a breast cancer, a cancer of the central nervous system, an endometrium cancer, a kidney cancer, a large intestine cancer, a lung cancer:
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U.S. Patent No. 11,566,020 B1 recites in conflicting claims 1-15 “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, wherein said cancer is breast cancer, cancer of the central nervous system, endometrium cancer, kidney cancer, large intestine cancer, lung cancer, esophagus cancer, ovarian cancer, pancreatic cancer, prostate cancer, stomach cancer, head and neck cancer (upper aerodigestive cancer), urinary tract cancer, or colon cancer:
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US Patent No. 11,566,020 B1 does not recite in claims 1-30 that the therapeutically effective amount is an amount of about 400 mg to about 600 mg; or particle size diameter of about 5 to about 15 µm.
The teachings of Remington, Filloon, Kuriyama, Shyamal and Gil teaches as discussed above, pages 15-16 and 26.
The obviousness rationale is like the obviousness rationale for the Double Patenting Rejection of claims 1, 5-6, 29-30, 40-41 and 110-120 above, page 26-27, and is incorporated herein by reference as applied to the rejected claims.
Double Patenting over U.S. Patent No. 12371421 B2
Claims 1, 5-6, 29-30, 40-41 and 110-120 are rejected on the ground of nonstatutory double patenting as being unpatentable over claims 1 and 17-20 of U.S. Patent No. 12371421 B2 in view of Filloon TG. Stat Med. 1995 May 15-30;14(9-10):925-32; discussion 933, “Filloon” cited in the previous PTO-892 dated 08/13/2025); Remington's Pharmaceutical science, 18th edition, Gennaro, A.R., ED, Mack Pub. Co.: Easton, PA, 1990, pp 1633-1665, “Remington”, cited in the previous PTO-892 dated 08/13/2025), M. Gil et al. (USPN 9956144B2, 05/01/2018, “Gil” cited in the PTO-892), Kuriyama A, et al. (AAPS PharmSciTech. 2014 Apr;15(2):375-87, “Kuriyama” cited in the PTO-892) and Shyamal C. et al. (Powder Technology, 2013, Volume 249, Pages 297-303, ISSN 0032-5910, “Shyamal” cited in the PTO-892). Although the claims at issue are not identical, they are not patentably distinct from each other because:
Instant claims 1, 5-6, 29-30, 40-41 and 110-120 recites “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 400 mg to about 600 mg, measured as the free base, wherein the compound, or pharmaceutically acceptable salt thereof, is administered at a total daily dosage of about 100, 200, 300, 400, 500, 600 mg, measured as the free base, wherein the compound, or the pharmaceutically acceptable salt thereof, is administered as an oral unit dosage form in the form of a tablet twice daily and wherein the particle size diameter [d90] of the compound, or pharmaceutically acceptable salt thereof, is about 5 to about 15 µm, wherein the cancer is a breast cancer, a cancer of the central nervous system, an endometrium cancer, a kidney cancer, a large intestine cancer, a lung cancer:
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U.S. Patent No. 12371421 B2 recites in conflicting claims 1, and 17-20 “A method of treating cancer in a patient in need of treatment comprising administering to said patient a therapeutically effective amount of a solid form of Compound 1, wherein said cancer is breast cancer, cancer of the central nervous system, endometrium cancer, kidney cancer, large intestine cancer, lung cancer, esophagus cancer, ovarian cancer, pancreatic cancer, prostate cancer, stomach cancer, head and neck cancer upper aerodigestive cancer, urinary tract cancer, or colon cancer:
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US Patent No. 12371421 B2 does not recite in claims 1 and 17-20 that the therapeutically effective amount is an amount of about 400 mg to about 600 mg; or particle size diameter of about 5 to about 15 µm.
The teachings of Remington, Filloon, Kuriyama, Shyamal and Gil teaches as discussed above, pages 15-16 and 26.
The obviousness rationale is like the obviousness rationale for the Double Patenting Rejection of claims 1, 5-6, 29-30, 40-41 and 110-120 above, page 26-27, and is incorporated herein by reference as applied to the rejected claims.
Double Patenting over copending Application No. 18/371,626
Claims 1, 5-6, 29-30, 40-41 and 110-120 are rejected on the ground of nonstatutory double patenting as being unpatentable over claims 42-51 and 56-57 of copending Application No. 18/371,626 (US PG-PUB 2024/0325391 A1) in view of Filloon TG. Stat Med. 1995 May 15-30;14(9-10):925-32; discussion 933, “Filloon” cited in the previous PTO-892 dated 08/13/2025). Although the claims at issue are not identical, they are not patentably distinct from each other because:
Instant claims 1, 5-6, 29-30, 40-41 and 110-120 recites “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 400 mg to about 600 mg, measured as the free base, wherein the compound, or pharmaceutically acceptable salt thereof, is administered at a total daily dosage of about 100, 200, 300, 400, 500, 600 mg, measured as the free base, wherein the compound, or the pharmaceutically acceptable salt thereof, is administered as an oral unit dosage form in the form of a tablet twice daily and wherein the particle size diameter [d90] of the compound, or pharmaceutically acceptable salt thereof, is about 5 to about 15 µm, wherein the cancer is a breast cancer, a cancer of the central nervous system, an endometrium cancer, a kidney cancer, a large intestine cancer, a lung cancer:
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copending Application No. 18/371,626 recited in conflicting claims 42-51 and 56-57 “a unit dosage form comprising 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, in an amount of about 25 mg to about 500 mg, measured as the free base, wherein the unit dosage form is in the form of a tablet, and wherein the particle size diameter [d90] of the compound, or pharmaceutically acceptable salt thereof, is about 5 to about 15 um.
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copending Application No. 18/371,626 does not recite in claims 42-51 and 56-57 the use of the above compound for treating cancer; the amount of the above compound in the pharmaceutical composition is about 400 mg to about 600 mg administered twice daily.
copending Application No. 18/371,626 specification recite a method of using the above compound in treating cancer, wherein the cancer is associated with abnormal expression or activity of PARP7, wherein the cancers include lung cancer, large intestine cancer, multiple myeloma, DLBCL, hepatocellular carcinoma, bladder cancer, esophageal cancer, head and neck cancer (upper aerodigestive cancer), kidney cancer, prostate cancer, rectal cancer, stomach cancer, thyroid cancer, uterine cancer, and breast cancer. [pg. 14, ln. 15-19].
MPEP 804 states: The specification can be used as a dictionary to learn the meaning of a term in the claim. Toro Co. v. White Consol. Indus., Inc., 199 F.3d 1295, 1299, 53 USPQ2d 1065, 1067 (Fed. Cir. 1999) ("[W]ords in patent claims are given their ordinary meaning in the usage of the field of the invention, unless the text of the patent makes clear that a word was used with a special meaning."); Renishaw PLC v. Marposs Societa' per Azioni, 158 F.3d 1243, 1250, 48 USPQ2d 1117, 1122 (Fed. Cir. 1998) ("Where there are several common meanings for a claim term, the patent disclosure serves to point away from the improper meanings and toward the proper meanings."). "The Patent and Trademark Office (‘PTO’) determines the scope of the claims in patent applications not solely on the basis of the claim language, but upon giving claims their broadest reasonable construction ‘in light of the specification as it would be interpreted by one of ordinary skill in the art.’ " Phillips v. AWH Corp., 415 F.3d 1303, 1316, 75 USPQ2d 1321, 1329 (Fed. Cir. 2005) (en banc) (quoting In re Am. Acad. of Sci. Tech. Ctr., 367 F.3d 1359, 1364, 70 USPQ2d 1827, 1830 (Fed. Cir. 2004); see also MPEP § 2111.01. Further, those portions of the specification which provide support for the reference claims may also be examined and considered when addressing the issue of whether a claim in the application defines an obvious variation of an invention claimed in the reference patent or application (as distinguished from an obvious variation of the subject matter disclosed in the reference patent or application). In re Vogel, 422 F.2d 438, 441-42, 164 USPQ 619, 622 (CCPA 1970). The court in Vogel recognized "that it is most difficult, if not meaningless, to try to say what is or is not an obvious variation of a claim," but that one can judge whether or not the invention claimed in an application is an obvious variation of an embodiment disclosed in the patent or application which provides support for the claim. According to the court, one must first "determine how much of the patent disclosure pertains to the invention claimed in the patent" because only "[t]his portion of the specification supports the patent claims and may be considered." The court pointed out that "this use of the disclosure is not in contravention of the cases forbidding its use as prior art, nor is it applying the patent as a reference under 35 U.S.C. 103, since only the disclosure of the invention claimed in the patent may be examined." In AbbVie Inc. v. Kennedy Institute of Rheumatology Trust, 764 F.3d 1366, 112 USPQ2d 1001 (Fed. Cir. 2014), the court explained that it is also proper to look at the disclosed utility in the reference disclosure to determine the overall question of obviousness in a nonstatutory double patenting context. See Sun Pharm. Indus., Ltd. v. Eli Lilly & Co., 611 F.3d 1381, 95 USPQ2d 1797 (Fed. Cir. 2010); Pfizer, Inc. v. Teva Pharm. USA, Inc., 518 F.3d 1353, 86 USPQ2d 1001 (Fed. Cir. 2008); Geneva Pharmaceuticals Inc. v. GlaxoSmithKline PLC, 349 F3d 1373, 1385-86, 68 USPQ2d 1865, 1875 (Fed. Cir. 2003).
With respect to administering the above compound twice daily, Filloon teaches detailed description on determining the minimum therapeutically effective dose, the lowest dose level that yields a therapeutic benefit to patients.
With regard to the total daily dose of 400-600 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 copending Application No. 18/371,626 dose range of about 25 mg to about 500 mg of PARP7 inhibitor to about 400-600 mg (e.g., 200 mg, 300 mg twice daily) of the PARP7 inhibitor measured as free base. One of ordinary skill in the art is motivated to do so with reasonable expectation of success because copending Application No. 18/371,626 range encompasses and overlapped with the claims’ ranges, and 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).”
One of ordinary skill in the art would have been motivated to administer copending Application No. 18/371,626 compound twice daily because Filloon teaches how to determine the therapeutically effective dose, Filloon teaches that one or two doses are administer during and twice a day (BID) dosing is administered in all Filloon’s studies, wherein all the treatments were taken twice daily during determining the therapeutically effective dose and tolerance analysis, [pg. 928, Figures 1-4]. Copending Application No. 18/371,626 is silent with respect to dosing frequency of the 25-500 mg e.g., twice daily, thus, Filloon would reasonably provide motivation to skill artisan practicing copending Application No. 18/371,626 above compound to admonishing the compound twice daily. Thus, claims 1, 5-6, 29-30, 33 and 40-41 are obvious over copending Application No. 18/371,626 in view of Filloon.
Response to Arguments
Applicant argues:
The claims as amended are nonobvious over U.S. Patent No. 10,550,105 B2 for at least the reasons discussed above. the claims as amended are nonobvious over U.S. Patent No. 10,870,641 B2 for at least the reasons discussed above. Thus, the claims as amended are nonobvious over U.S. Patent No. 11,014,913 B2 for at least the reasons discussed above. Thus, the claims as amended are nonobvious over U.S. Patent No. 11,566,020 B1 for at least the reasons discussed above. The claims as amended are nonobvious over U.S. Patent No. 12,371,421 B2 for at least the reasons discussed above. Where the reference application has not matured to a patent and the provisional double patenting rejection over co-pending Application No. 18/371,626 is the only remaining rejection in the application, the examiner should withdraw the provisional rejection.
Examiner response:
Applicant’s arguments have been fully considered but they are not persuasive for the following reasons. The non-statutory double patenting rejections above have been modified, and the secondary prior arts now are Kuriyama, Shyamal and Gil instead of Khadka, see reasons for withdrawn Khadka above. Thus, Applicant’s arguments are moot because the modified rejections do not rely on Khadka reference applied in the prior rejection of record for any teaching or matter specifically challenged in the argument. With respect to the non-statutory double patenting rejection over co-pending Application No. 18/371,626, the rejection is maintained because Applicant’s arguments are not persuasive.
Conclusion
Claims 1, 5-6, 29-30, 40-41 and 110-120 are rejected. No claim is allowed.
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 Examiner conducted search to determine the enablement of treating NSCLC by the claimed compound and the connection between PARP7 inhibition and treatment of NSCLC, and considered that one of skill in the art could practice this subject matter, upon the filing date of the instant application, without undue experimentation in view of instant specification, Spigel and Barber. MPEP § 2164.02; In re Brana, 51 F.3d 1560, 1566, 34 USPQ2d 1486, 1441 (Fed. Cir. 1995). D. Spigel (Journal of Thoracic Oncology, Volume 7, Issue 12, Supplement 5, 2012, Pages S392-S393, “Spigel” cited in the PTO-892), and J. Barber (FirstWord PHARMA, 2013, Study finds PARP inhibitors may be useful against NSCLC, https://firstwordpharma.com/story/968335, “Barber” cited in the PTO-892).
Prosecution Insights