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 12/15/2023, is a national phase application under 35 U.S.C. § 371 of International Application No. PCT/EP2021/068532, filed on 07/05/2021.
Information Disclosure Statement
The information disclosure statement (IDS) filed on 04/02/2024, 05/08/2024, 06/04/2024, 07/31/2024, 12/23/2024, 03/07/2025, 07/24/2025 and 06/12/2026, 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.
Status of claims
Applicant’s amendments and arguments filed on 06/12/2026 have been received and have been fully considered.
Claims 1-15 and 19-20 were amended, and claims 16-18 were cancelled. Claims 1-15 and 19-20 are pending.
Withdrawn Objection to Abstract
Objection to Abstract for lacking proper abstract language is withdrawn because Applicant replace the Abstract with new Abstract submitted on 06/12/2026.
Withdrawn Claim Objections
Objection to claims 10-20 under 37 CFR 1.75(c) as being in improper form because a multiple dependent claim, is withdrawn in view of Applicant’s amendment filed on 06/12/2026 that amended claims 10-15 and 19-20 to refer to other claims in the alternative only, and cancelled claims 16-18.
Withdrawn Claim Rejections 35 U.S.C. 112(b)
Rejection to claims 1-20 under 35 U.S.C. 112(b) or 35 U.S.C. 112 (pre-AIA ), second paragraph, as being indefinite for reciting use claim, is withdrawn in view of Applicant’s amendment filed on 06/12/2026 that amended the claims by deleting “for use in” and added “a method of treating …”.
Rejection of claims 1-20 under 35 U.S.C. 112(b) or 35 U.S.C. 112 (pre-AIA ), second paragraph for insufficient antecedent basis for reciting the term “the repeated administration”, is withdrawn in view of Applicant’s amendment filed on 06/12/2026 that amended the claims by deleting the term.
Withdrawn Claim Rejections - 35 USC § 112 (a)
Claims 1-20 are rejected under 35 U.S.C. 112(a) or 35 U.S.C. 112 (pre-AIA ), first paragraph, because the specification does not reasonably provide enablement for the treatment of the claimed scope of neurological disorders or neurodegenerative diseases, sleep disorders, neuropsychiatric conditions, etc., is withdrawn in view of Applicant’s amendment filed on 06/12/2026 that amended claim 1 with “a method of treating Progressive Supranuclear Palsy.”
The lack of enablement of claim 15 recitation “wherein the human subject is at increased risk of …”, is withdrawn in view of Applicant’s persuasive argument filed on 06/12/2026 that the specification provide guidance on how to identify subjects at risk of developing PSP, see specification at pages 10, 16 and 68.
Withdrawn Claim Rejections - 35 USC § 103
Rejection of claims 1-20 under 35 U.S.C. 103 as being unpatentable over A. Quattropani et al. (US Patent No. 10336775B2, 07/02/2019), is withdrawn in view of Applicant’s amendment filed on 06/12/2026 that amended claim 1 with “a method of treating Progressive Supranuclear Palsy.”
Rejection New necessitated by the amendment
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.
Claims 1-15 and 19-20 are rejected under 35 U.S.C. 103 as being unpatentable over A. Quattropani et al. (US Patent No. 10,336,775 B2, 07/02/2019 (Priority date 08/27/2015), “Quattropani” cited in the IDS dated 04/02/2024) in view of Y. Zhu, et al. ACS Chem. Neurosci. 2018/06/20, VL - 9, IS - 6, pp. 1366-1379, “Zhu” cited in the PTO-892), A. Shoeibi, et al. Expert Opinion on Investigational Drugs, 2018, 27:4, 349-361, “Shoeibi” cited in the PTO-892), and PSP Blog, 2015, https://psp-blog.org/tag/o-glcnacase/, cited in the PTO-892), and Alectos, 2016, http://alectos.com/alectos-content/index.php/2016/04/20/alectos-therapeutics-announces-fda-orphan-drug-designation-mk-8719-investigational-small-molecule-oga-inhibitor-treatment-progressive-supranuclear-palsy/, cited in the PTO-892).
Quattropani teaches human glycosidase inhibitors of formula (I) and salts thereof, wherein A, R, W, Q, m, and n are defined, [col. 5-8]:
PNG
media_image1.png
168
220
media_image1.png
Greyscale
Quattropani teaches compound N-(5-(4-(1-(Benzo[d][1,3] dioxol-5-yl)ethyl)piperazin-1-yl)-1,3,4-thiadiazol-2-yl)acetamide, as species of formula (I), [col. 39, Table 1, compound 69, col. 186, ln. 35, and claim 1]:
PNG
media_image2.png
200
514
media_image2.png
Greyscale
Quattropani teaches that the enantiomer 69 is more active than 68, with an IC50 of less than 0.05 µM (enantiomer 68 is 1-10 µM) [ending of Table 1, col. 91].
Quattropani teaches a pharmaceutical composition of the compound as medicament in human and veterinary medicine for treating neurodegenerative diseases selected from one or more tauopathies, Alzheimer's disease, Progressive Supranuclear Palsy (PSP), etc. [col. 110, ln. 63- 64, col. 111, ln. 4-6, 63].
With regard to the dosing amount and dosing frequency, Quattropani teaches that “it will be understood that the specific dose level, frequency and period of administration to any particular human will depend upon a variety of factors including the activity of the specific compound employed, the age, body weight, general state of health, route of administration, etc., and the exact dose can be determined by one of skill in the art as a matter of routine experimentation using well-known means and methods,.” [col. 110, ln. 5-14]. Quattropani teaches that the compound is administered in a unit dosage form in doses of 0.5-1000 mg, more preferably 1-700 mg or 5-100 mg per dose unit. [col. 110, ln. 18-27]. Quattropani teaches that “although a therapeutically effective amount of a compound according to the invention has to be ultimately determined by the treating doctor or vet by considering a number of factors, an effective amount of the compound above for the treatment of neurodegenerative diseases, for example tauopathies and Alzheimer's disease, is usually between 70 mg and 700 mg, where this amount can be administered as a single dose per day or usually in a series of part-doses, i.e., two, three, four, five or six per day, so that the total daily dose is the same. Quattropani teaches that the compound administered orally. [col. 108, ln. 62-63].
With regard to human subject, Quattropani teaches that method can be performed either in-vitro or in-vivo, wherein host or patient can belong to any mammalian species, for example a primate species, particularly humans; rodents, including mice, rats and hamsters; rabbits; horses, cows, dogs, cats, etc. Animal models are of interest for experimental investigations, providing a model for treatment of human disease. [col. 106, ln. 40-55].
With regard to the pharmacokinetics, Quattropani teaches that in-vitro liver microsomal assays provide significant improvements in the pharmacokinetic profiles of compounds of the formula (I) in terms of increases in the in vivo half-life (t/2), concentration at maximum therapeutic effect (Cmax), area under the dose response curve (AUC), [col. 112, ln. 1-10].
In view of the foregoing, Quattropani teaches the claimed compound of formula (I) for use in a method of treating a human subject having neurodegenerative diseases, e.g., Progressive Supranuclear Palsy (PSP) by administration of compound of formula (I) two, three, four or five times. However, one of ordinary skill in the art need to specifically pick Quattropani’s compound 69 above from the human glycosidase inhibitors, and Progressive Supranuclear Palsy from the neurodegenerative diseases taught by Quattropani.
Zhu teaches The glycosylation of nucleocytoplasmic proteins with O-linked N-acetylglucosamine residues (O-GlcNAc) is involved in diverse cellular processes and various diseases including neurodegenerative diseases. Pharmacological inhibition of O-GlcNAc, reproducibly slows neurodegeneration in various Alzheimer’s disease (AD) mouse models manifesting tau pathology. O-GlcNAc inhibitors have been used as pharmaceuticals to alter the progression of AD. O-GlcNAc inhibition significantly decreased the toxic protein associated with AD pathogenesis, enhanced of autophagy in the brain, and hindering the progression of AD, and being a feasible therapeutic strategy for hindering other neurodegenerative diseases. [Abstract]. Zhu teaches the claimed compound as one of the potent GlcNAc inhibitor that activate autophagy and show greater autophagic flux in cells, [page 1369, col. 1, 1st para., page S3, figure S2 of Zhu’s Supported Information document]. Zhu teaches that the compound is administered at a concentration of 250 M. [page S3, figure S2 of Zhu’s Supported Information document].
Shoeibi teaches treatment, pathology and mechanism of progressive supranuclear palsy (PSP). Shoeibi teaches that the abnormal modifications of tau protein, and transcellular tau spread are the pathophysiologic mechanisms of PSP [Abstract]. Shoeibi teaches the role of inhibition of O-linked-β-N-acetylglucosamine in the treatment of PSP, see pages 350, col. 2, 2.2; 354, col. 1, 3rd para.; 357, col. 2, 3rd para.; Fig. 1]. Shoeibi teaches that inhibition of O-linked-β-N-acetylglucosamine considered one of the main therapeutic of PSP, and PSP has been targeted by many O-linked-β-N-acetylglucosamine inhibitors, [page 351, Table 2].
PSP Blog teaches treatment of progressive supranuclear palsy using small molecules inhibitors of O-linked-β-N-acetylglucosamine.
Alectos teaches the use of O-linked-β-N-acetylglucosamine inhibitors for treating progressive supranuclear palsy.
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 pick Quattropani’s compound 69 for the treating human subjects having progressive supranuclear palsy. One of ordinary skill in the art would have been motivated to do so with reasonable expectation of success because Quattropani teaches that compound 69 is a very potent O-GlcNAcase inhibitor; [col. 91, ln. 29]; demonstrate adequate properties for use as a drug by showing high solid state stability, high stability in the presence of liver microsome, high oxidation stability, suitable permeability and potent biological activity; and Quattropani’s patent is directed to compound 69, composition of compound 69, and salt of compound 69 which indicates that compound 69 is the most potent compound of Quattropani, and therefore, skilled artisan would have been motivated to also pick compound 69 for use in a method of treating a human subject have progressive supranuclear palsy. Moreover, Zhu teaches that inhibition of O-linked-β-N-acetylglucosamine is associated with treatment of neurodegenerative diseases, and teaches the claimed compound as one of the potent GlcNAc inhibitor that activate autophagy and show greater autophagic flux in cells.
One of ordinary skill in the art would have been motivated to utilize the potent O-linked-β-N-acetylglucosamine inhibitor taught by Quattropani and Zhu, compound 69 above in treating progressive supranuclear palsy with reasonable expectation of success because Quattropani teaches the use of compound 69 above in treating neurodegenerative diseases including progressive supranuclear palsy; Zhu teaches the use of potent and selective O-linked-β-N-acetylglucosamine inhibitor for treating Alzheimer’s and tauopathies, and teaches the beneficial effects on of the compound in tauopathy mouse models (progressive supranuclear palsy model) [page 1367, col. 1, ending of 1st para., 2nd para., and col. 2 2nd para.]; Shoeibi teaches that inhibition of O-linked-β-N-acetylglucosamine considered one of the main therapeutic of progressive supranuclear palsy (PSP), and PSP has been targeted by many O-linked-β-N-acetylglucosamine inhibitors, [page 351, Table 2]; PSP Blog teaches treatment of progressive supranuclear palsy using small molecules inhibitors of O-linked-β-N-acetylglucosamine; and Alectos teaches the use of O-linked-β-N-acetylglucosamine inhibitors for treating progressive supranuclear palsy. Therefore, in view of the cited art above, inhibiting O-linked-β-N-acetylglucosamine is well-known therapeutic target for the treatment of progressive supranuclear palsy, and specifically selecting compound 69 above for treating progressive supranuclear palsy is prima facie obvious.
The pharmacokinetics of the plasma concentration of the compound of formula (I) of at least about 35 ng/mL, 45-2000 ng/mL, at least about 155 ng/mL, 270-2000 ng/mL, 1650-7390 ng/mL, plasma AUC of about 13850-90500 ng*h/mL, plasma Cmax of about 3580-7390 ng/mL is met for the following reasons: the combination of Quattropani, Zhu, Shoeibi, PSP Blog and Alectos teach a method of using the claimed compound in treating progressive supranuclear palsy. The combination of Quattropani, Zhu, Shoeibi, PSP Blog and Alectos are silent on the pharmacokinetics of the compound but otherwise teaches a substantially identical method as claimed. As such, it is reasonable to presume that the resulting plasma concentration, plasma AUC, and plasma Cmax is inherently met. The burden is on Applicant(s) to show that this property is different from those taught by the prior art and to establish patentable differences. See MPEP 2112.
Therefore, claims 1-6, 8-9, and 11-12 are prima facie obvious over Quattropani.
With regard to claims 19 and 20, Quattropani teaches that the salt is hydrochloric salt. [col. 103, ln. 36].
With regard to claim 7, 10, and 13-14, Quattropani teaches that the compound is administered in doses of 0.5-1000 mg, more preferably 1-700 mg. [col. 110, ln. 25-27]. Quattropani also teaches that the doses can be between 70 mg and 700 mg administered as a single dose per day or usually in a series of part-doses, e.g., two, three per day. [col. 110, ln. 40-60]. Quattropani teaches amounts that encompasses or overlapped with the claimed amounts. 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). Similarly, a prima facie case of obviousness exists where the claimed ranges or amounts do not overlap with the prior art but are merely close. Titanium Metals Corp. of America v. Banner, 778 F.2d 775, 783, 227 USPQ 773, 779 (Fed. Cir. 1985). "[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, "[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). Furthermore, the optimization of known amounts for known active agents is considered well within the competence level of an artisan of ordinary skill in the pharmaceutical sciences; it has been held that the selection of optimal parameters, such as amounts of active agents, to achieve a beneficial effect, is within the skill in the art of an ordinary artisan. See In re Boesch, 205 USPT 215 (CCPA 1980) and MPEP 2144.05. As such, an artisan having ordinary skill in the art would have been motivated to modify the amounts to achieve 150-500 mg, 300-500mg, 240-1500 mg, and therefore, meets claims 7, 10, and 13-14.
With regard to claim 15, Zhu teaches the treatment of tauopathies in TgN-(MAPT)-JNPL3HlmcFemale mice (known to be at high risk of developing tauopathies) [page 1375, col. 2, 2nd para.]; and Shoeibi teaches that inhibition of O-linked-β-N-acetylglucosamine considered one of the main therapeutic of progressive supranuclear palsy (PSP), wherein the treatment mechanism includes genetic mechanisms, abnormal post-translational modifications of tau protein, and transcellular tau spread [Abstract], and in genetic mechanism, subject containing MAPT gene are at high risk of PSP, and STX6, EIF2AK3, and MOBP genes are risk factors for PSP [page 350, col. 1, ending, col. 2, 1st para.]. Thus, one of ordinary skill in the art have access to Zhu and Shoeibi would be have been motivated to treat the subject at risk of developing PSP with the potent O-linked-β-N-acetylglucosamine inhibitor taught by Quattropani and Zhu, compound 69 above. See Shoeibi whole document.
Response to Argument
Applicant argues:
Furthermore, the burden of production falls on the Examiner to provide a basis in fact and/or technical reasoning to reasonably support the determination that the allegedly inherent characteristic necessarily flows from the teachings of the applied prior art. See MPEP § 2112(V). As an initial matter, Quattropani does not administer the compound of Formula (I) to a subject with Progressive Supranuclear Palsy, at all, let alone at the doses and dosing frequency recited in the pending claims. Therefore, Quattropani cannot inherently teach the claimed PK properties. Quattropani discloses a genus of OGA inhibitors and broad dose ranges encompassing hundreds of structurally diverse compounds, extremely broad doses and dosing regimen related to all of the disclosed compounds, but it does not disclose the specific PK properties of Compound (I). The mere fact that a broad dose range may encompass a dose achieving a given PK threshold does not establish that the claimed PK limitations would necessarily result from following the disclosure of Quattropani. The Examiner has provided no evidence demonstrating that the claimed PK parameters would necessarily be achieved by administering Compound (I) according to any specific dose and dosing regimen disclosed in Quattropani. Absent such evidence, the Examiner has not met the burden of establishing inherency, and the rejection cannot be sustained. See MPEP § 2112(V) ("[T]he examiner must provide a basis in fact and/or technical reasoning to reasonably support the determination that the allegedly inherent characteristic necessarily flows from the teachings of the applied prior art."). Quattropani does not disclose, teach, or suggest the claimed Pl-based dosing regimen. The claimed methods are not simply methods of administering any OGA inhibitor at any dose. Rather, the claims are directed to achieving a specific and clinically meaningful steady- state pharmacokinetic profile.
The specification of the instant application discloses that the EC50 for brain OGA occupancy by Compound (I) in humans is 84.1 ng/ml (95% CI: 68.0-100.1 ng/ml) (paragraph [0372]), as determined by a human PET target occupancy study. The claimed trough concentration threshold (at least about 35 ng/ml) was selected to achieve meaningful, sustained brain OGA target occupancy at trough, specifically, to maintain at least a minimum level of occupancy sufficient for therapeutic effect throughout the dosing interval, the results of which are disclosed in the specification of the instant application and which could not have been predicted from Quattropani's preclinical disclosure.
Examiner response:
Applicant's arguments have been fully considered but they are not persuasive. The majority of Applicant’s arguments are on the pharmacokinetics and inherency argument. Quattropani teaches a method of treating neurodegenerative diseases, e.g., Progressive Supranuclear Palsy (PSP) in a human subject by administering compound 69 two, three, four or five times, wherein the compound is administered in a unit dosage form preferably 1-700 mg or 5-100 mg per dose unit. [col. 110, ln. 18-27], with treating tauopathies diseases e.g., PSP is usually between 70 mg and 700 mg, and ultimately determined by the treating doctor or vet by considering a number of factors [col. 108, ln. 62-63], wherein the dosing amount and dosing frequency will depend upon a variety of factors including the activity of the specific compound employed, the age, body weight, general state of health, route of administration, etc., and the exact dose can be determined by one of skill in the art as a matter of routine experimentation using well-known means and methods.” [col. 110, ln. 5-14]. The combination of Quattropani, Zhu, Shoeibi, PSP Blog and Alectos teaches a method of treating Progressive Supranuclear Palsy in a human subject in need thereof, comprising administering to the human subject a unit dosage forms comprising the compound of formula (I) or a pharmaceutically acceptable salt, solvate, or tautomer thereof. Thus, one of ordinary skill in the art would reasonably presume that administering the doses of compound 69 would necessarily produce the claimed pharmacokinetics. Because the combination of Quattropani, Zhu, Shoeibi, PSP Blog and Alectos teaches a substantially identical method as claimed. As such, it is reasonable to presume that the resulting plasma concentration, plasma AUC, and plasma Cmax is inherently met. See MPEP 2112. In view of the obviousness of the claimed compound doses, e.g., 150-500 mg, 240-1500 mg/day (claims 7 and 13) and doses listed on instant specification page 19-20, producing the plasma concentration by administering compound 69 is consider a property of compound 69 since the properties of a compound are inseparable. MEPEP 2112 (1), and claiming of a new or unknown property which is inherently present in the prior art does not necessarily make the claim patentable. In re Best, 562 F.2d 1252, 1254, 195 USPQ 430, 433 (CCPA 1977). The burden is on Applicant(s) to show that this property is different from those taught by the prior art and to establish patentable differences. However, Applicant does not provide factual evidences on criticality of the doses and the resulting plasma concentration, plasma AUC, and plasma Cmax as MPEP 2144.05.II.A explains: “Generally, differences in concentration (dose) will not support the patentability of subject matter encompassed by the prior art unless there is evidence indicating such concentration (dose) 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).” Note that the resulting plasma concentration, plasma AUC, and plasma Cmax are directly flow from the administered doses. Applicant provide arguments without evidence, and as provided in MPEP 2145, If a prima facie case of obviousness is established, the burden shifts to the applicant to come forward with arguments and/or evidence to rebut the prima facie case. See, e.g., In re Dillon, 919 F.2d 688, 692, 16 USPQ2d 1897, 1901 (Fed. Cir. 1990) (en banc). Rebuttal evidence and arguments can be presented in the specification, In re Soni, 54 F.3d 746, 750, 34 USPQ2d 1684, 1687 (Fed. Cir. 1995), by counsel, In re Chu, 66 F.3d 292, 299, 36 USPQ2d 1089, 1094-95 (Fed. Cir. 1995), or by way of an affidavit or declaration under 37 CFR 1.132, e.g., Soni, 54 F.3d at 750, 34 USPQ2d at 1687; In re Piasecki, 745 F.2d 1468, 1474, 223 USPQ 785, 789-90 (Fed. Cir. 1984). However, arguments of counsel cannot take the place of factually supported objective evidence. See, e.g., In re Huang, 100 F.3d 135, 139-40, 40 USPQ2d 1685, 1689 (Fed. Cir. 1996); In re De Blauwe, 736 F.2d 699, 705, 222 USPQ 191, 196 (Fed. Cir. 1984).
Applicant argues:
The Examiner contends that the claimed dose amounts overlap with ranges disclosed in Quattropani. Applicant respectfully submits that mere overlap of numerical ranges does not, without more, establish a prima facie case of obviousness. Quattropani discloses broad dose ranges applicable to a large number of structurally diverse OGA inhibitors, but it provides no pharmacological rationale for selecting any particular dose within those ranges, and it makes no reference whatsoever to the PK targets that define the present claims. The specification discloses human PK data from single-dose and multiple-dose clinical studies demonstrating that the specific claimed regimens, for example, about 150 mg TID or about 250 mg BID, and about 300 mg TID or about 500 mg BID, achieve the clinically meaningful steady-state PK profile defined by the claims (trough concentrations, average concentrations, Cmax, and AUC). These regimens were not selected by routine optimization within a known range; rather, they were identified through human clinical investigation guided by PK/PD modeling that related plasma drug concentrations to brain OGA target occupancy, a relationship that Quattropani neither discloses nor suggests. Quattropani provides no human pharmacokinetic data for Compound (I), no PK/PD model, and no basis from which a person of ordinary skill in the art could have predicted the specific PK parameters that would result from any given dosing regimen.
Examiner response:
Applicant's arguments have been fully considered but they are not persuasive. Applicant claimed that the prior art does not teach the dose amounts. However, instant specification provides multiple dosing amounts, for example 150-1500 mg, about 150 mg TID or about 250 mg BID, and about 300 mg TID or about 500 mg BID, 75 mg thrice a day, 125 twice a day, see instant specification pages 19-21, however, applicant does not provide any evidence on criticality of any of these doses. "[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).” Quattropani teaches that the compound is administered in doses of 0.5-1000 mg, more preferably 1-700 mg. [col. 110, ln. 25-27]. Quattropani also teaches that the doses can be between 70 mg and 700 mg administered as a single dose per day or usually in a series of part-doses, e.g., two, three per day. [col. 110, ln. 40-60]. Quattropani teaches amounts that encompasses or overlapped with the claimed amounts. 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). Similarly, a prima facie case of obviousness exists where the claimed ranges or amounts do not overlap with the prior art but are merely close. Titanium Metals Corp. of America v. Banner, 778 F.2d 775, 783, 227 USPQ 773, 779 (Fed. Cir. 1985). "[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, "[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). Furthermore, the optimization of known amounts for known active agents is considered well within the competence level of an artisan of ordinary skill in the pharmaceutical sciences; it has been held that the selection of optimal parameters, such as amounts of active agents, to achieve a beneficial effect, is within the skill in the art of an ordinary artisan. See In re Boesch, 205 USPT 215 (CCPA 1980) and MPEP 2144.05. furthermore, Zhu teaches that the claimed compound is administered at a concentration of 250 nM, Quattropani teaches that “it will be understood that the specific dose level, frequency and period of administration to any particular human will depend upon a variety of factors including the activity of the specific compound employed, the age, body weight, general state of health, route of administration, etc., and the exact dose can be determined by one of skill in the art as a matter of routine experimentation using well-known means and methods.” [col. 110, ln. 5-14].
Double Patenting
The nonstatutory double patenting rejection is based on a judicially created doctrine grounded in public policy (a policy reflected in the statute) so as to prevent the unjustified or improper timewise extension of the “right to exclude” granted by a patent and to prevent possible harassment by multiple assignees. A nonstatutory double patenting rejection is appropriate where the conflicting claims are not identical, but at least one examined application claim is not patentably distinct from the reference claim(s) because the examined application claim is either anticipated by, or would have been obvious over, the reference claim(s). See, e.g., In re Berg, 140 F.3d 1428, 46 USPQ2d 1226 (Fed. Cir. 1998); In re Goodman, 11 F.3d 1046, 29 USPQ2d 2010 (Fed. Cir. 1993); In re Longi, 759 F.2d 887, 225 USPQ 645 (Fed. Cir. 1985); In re Van Ornum, 686 F.2d 937, 214 USPQ 761 (CCPA 1982); In re Vogel, 422 F.2d 438, 164 USPQ 619 (CCPA 1970); In re Thorington, 418 F.2d 528, 163 USPQ 644 (CCPA 1969).
A timely filed terminal disclaimer in compliance with 37 CFR 1.321(c) or 1.321(d) may be used to overcome an actual or provisional rejection based on nonstatutory double patenting provided the reference application or patent either is shown to be commonly owned with the examined application, or claims an invention made as a result of activities undertaken within the scope of a joint research agreement. See MPEP § 717.02 for applications subject to examination under the first inventor to file provisions of the AIA as explained in MPEP § 2159. See MPEP § 2146 et seq. for applications not subject to examination under the first inventor to file provisions of the AIA . A terminal disclaimer must be signed in compliance with 37 CFR 1.321(b).
The filing of a terminal disclaimer by itself is not a complete reply to a nonstatutory double patenting (NSDP) rejection. A complete reply requires that the terminal disclaimer be accompanied by a reply requesting reconsideration of the prior Office action. Even where the NSDP rejection is provisional the reply must be complete. See MPEP § 804, subsection I.B.1. For a reply to a non-final Office action, see 37 CFR 1.111(a). For a reply to final Office action, see 37 CFR 1.113(c). A request for reconsideration while not provided for in 37 CFR 1.113(c) may be filed after final for consideration. See MPEP §§ 706.07(e) and 714.13.
The USPTO Internet website contains terminal disclaimer forms which may be used. Please visit www.uspto.gov/patent/patents-forms. The actual filing date of the application in which the form is filed determines what form (e.g., PTO/SB/25, PTO/SB/26, PTO/AIA /25, or PTO/AIA /26) should be used. A web-based eTerminal Disclaimer may be filled out completely online using web-screens. An eTerminal Disclaimer that meets all requirements is auto-processed and approved immediately upon submission. For more information about eTerminal Disclaimers, refer to www.uspto.gov/patents/apply/applying-online/eterminal-disclaimer.
Non-statutory Double Patenting over US Patent No. 10,336,775 B2
Claims 1-15 and 19-20 are rejected on the ground of nonstatutory double patenting as being unpatentable over claims 1-3 of US Patent No. 10,336,775 B2 (cited in the IDS dated 04/02/2024) in view of a, Quattropani et al. (US PG-PUB 2019/0055233A1, 02/21/2019, “Quattropani II” cited in the PTO-892), Y. Zhu, et al. ACS Chem. Neurosci. 2018/06/20, VL - 9, IS - 6, pp. 1366-1379, “Zhu” cited in the PTO-892), A. Shoeibi, et al. Expert Opinion on Investigational Drugs, 2018, 27:4, 349-361, “Shoeibi” cited in the PTO-892), and PSP Blog, 2015, https://psp-blog.org/tag/o-glcnacase/, cited in the PTO-892), and Alectos, 2016, http://alectos.com/alectos-content/index.php/2016/04/20/alectos-therapeutics-announces-fda-orphan-drug-designation-mk-8719-investigational-small-molecule-oga-inhibitor-treatment-progressive-supranuclear-palsy/, cited in the PTO-892). Although the claims at issue are not identical, they are not patentably distinct from each other because:
Instant claims 1-15 and 19-20 recites “a method of treating Progressive Supranuclear Palsy in a human subject in need thereof, comprising administering to the human subject a unit dosage forms comprising the compound of formula (I) or a pharmaceutically acceptable salt, solvate, or tautomer thereof, wherein the unit dosage form is administered in a dose and at a daily dosing frequency sufficient to maintain plasma trough concentration of the compound of formula (I) and/or its tautomer at steady state at least about 35 ng/mL at trough in a range of about 45 -2000 ng/mL at trough, a plasma Cmax of the compound of formula (I) of about 1650-7390 ng/mL, a plasma AUC over 24 hours of the compound of formula (I) of about 13850-90500 ng*h/mL, wherein the dose of the compound of formula (I) is administered orally in the range of about 150 mg to about 500 mg twice a day or thrice a day, wherein the human subject suffers from a disease or condition, or is at increased risk of developing a disease or condition, wherein the compound is administered in form of a pharmaceutically usable solvate and/or salt thereof, wherein the compound is administered in form of its hydrochloride salt:
PNG
media_image3.png
122
326
media_image3.png
Greyscale
US Patent No. 10,336,775B2 recites a compound, N-(5-(4-(1-(Benzo[d][1,3]dioxol-5-yl)ethyl)piperazin-1-yl)-1,3,4-thiadiazol-2-yl)acetamide, or enantiomers or mixtures thereof, or pharmaceutically acceptable salt, wherein the pharmaceutically acceptable salt is hydrochloric salt:
PNG
media_image4.png
188
456
media_image4.png
Greyscale
US Patent No. 10,336,775B2 does not recites using the above compound for treating PSP, the amount of the compound administered, or the claimed pharmacokinetics. Also, one of ordinary skill in the art need to specifically pick PSP from the diseases and conditions list.
However, the specification of US Patent No. 10,336,775B2 recites a method for treating neurodegenerative diseases in human using compound N-(5-(4-(1-(Benzo[d][1,3]dioxol-5-yl)ethyl)piperazin-1-yl)-1,3,4-thiadiazol-2-yl)acetamide, most preferably one or more tauopathies, highly preferably Alzheimer's disease and dementia. [col. 110, ln. 63- col. 111, 6]. 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).
Moreover, Quattropani II teaches compound of formula I, [0005], and compound N-(5-(4-(1-(Benzo[d][1,3]dioxol-5-yl)ethyl)piperazin-1-yl)-1,3,4-thiadiazol-2-yl)acetamide as species of formula I [0027], for treating tauopathies and Alzheimer's disease, Dementia, etc. [0048], wherein the compound administered in doses of approximately 0.5 to 1000 mg, more preferably between 1 and 700 mg, most preferably 5 and 100 mg per dose unit [0046].
Zhu, Shoeibi, PSP Blog and Alectos teach as discussed above, page 7-8.
The obviousness rationale is the same as the obviousness rationale of the above 103 Rejection, page 8-9.
Non-statutory Double Patenting over US Patent No. 10,696,668 B2
Claims 1-15 and 19-20 are rejected on the ground of nonstatutory double patenting as being unpatentable over claims 1-2 of US Patent No. 10,696,668 B2 (cited in the IDS dated 04/02/2024) in view of a, Quattropani et al. (US PG-PUB , 10/19/2017, “Quattropani III” cited in the PTO-892), Y. Zhu, et al. ACS Chem. Neurosci. 2018/06/20, VL - 9, IS - 6, pp. 1366-1379, “Zhu” cited in the PTO-892), A. Shoeibi, et al. Expert Opinion on Investigational Drugs, 2018, 27:4, 349-361, “Shoeibi” cited in the PTO-892), and PSP Blog, 2015, https://psp-blog.org/tag/o-glcnacase/, cited in the PTO-892), and Alectos, 2016, http://alectos.com/alectos-content/index.php/2016/04/20/alectos-therapeutics-announces-fda-orphan-drug-designation-mk-8719-investigational-small-molecule-oga-inhibitor-treatment-progressive-supranuclear-palsy/, cited in the PTO-892). Although the claims at issue are not identical, they are not patentably distinct from each other because:
Instant claims 1-15 and 19-20 recites “a method of treating Progressive Supranuclear Palsy in a human subject in need thereof, comprising administering to the human subject a unit dosage forms comprising the compound of formula (I) or a pharmaceutically acceptable salt, solvate, or tautomer thereof, wherein the unit dosage form is administered in a dose and at a daily dosing frequency sufficient to maintain plasma trough concentration of the compound of formula (I) and/or its tautomer at steady state at least about 35 ng/mL at trough in a range of about 45 -2000 ng/mL at trough, a plasma Cmax of the compound of formula (I) of about 1650-7390 ng/mL, a plasma AUC over 24 hours of the compound of formula (I) of about 13850-90500 ng*h/mL, wherein the dose of the compound of formula (I) is administered orally in the range of about 150 mg to about 500 mg twice a day or thrice a day, wherein the human subject suffers from a disease or condition, or is at increased risk of developing a disease or condition, wherein the compound is administered in form of a pharmaceutically usable solvate and/or salt thereof, wherein the compound is administered in form of its hydrochloride salt:
PNG
media_image3.png
122
326
media_image3.png
Greyscale
US Patent No. 10,696,668 B2recites compound N-(5-(4-(1-(Benzo[d][1,3]dioxol-5-yl)ethyl)piperazin-1-yl)-1,3,4-thiadiazol-2-yl)acetamide mono-hydrochloride, and solid oral dosage form comprising the compound:
PNG
media_image4.png
188
456
media_image4.png
Greyscale
US Patent No. 10,696,668 B2 does not recites using the above compound for treating PSP, the amount of the compound administered, or the claimed pharmacokinetics. Also, one of ordinary skill in the art need to specifically pick PSP from the diseases and conditions list.
However, US Patent No. 10,696,668 B2 specification recites a method for treating PSP using compound N-(5-(4-(1-(Benzo[d][1,3]dioxol-5-yl)ethyl)piperazin-1-yl)-1,3,4-thiadiazol-2-yl)acetamide, [col. 10, ln. 49]. 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).
Moreover, Quattropani III teaches compound of formula I, [0001], and compound N-(5-(4-(1-(Benzo[d][1,3]dioxol-5-yl)ethyl)piperazin-1-yl)-1,3,4-thiadiazol-2-yl)acetamide as species of formula I [0083, Table 1, comp. 69], for treating tauopathies and Alzheimer's disease. [00164], wherein the compound administered in doses of approximately 0.5 to 1000 mg, more preferably between 1 and 700 mg, most preferably 5 and 100 mg per dose unit [0154].
Zhu, Shoeibi, PSP Blog and Alectos teach as discussed above, page 7-8.
The obviousness rationale is the same as the obviousness rationale of the above 103 Rejection, page 8-9.
Non-statutory Double Patenting over US Patent No. 11,046,712 B2
Claims 1-15 and 19-20 are rejected on the ground of nonstatutory double patenting as being unpatentable over claims 1-12 of US Patent No. 11,046,712 B2 (cited in the IDS dated 04/02/2024), in view of a, Quattropani et al. (US PG-PUB , 10/19/2017, “Quattropani III” cited in the PTO-892), Y. Zhu, et al. ACS Chem. Neurosci. 2018/06/20, VL - 9, IS - 6, pp. 1366-1379, “Zhu” cited in the PTO-892), A. Shoeibi, et al. Expert Opinion on Investigational Drugs, 2018, 27:4, 349-361, “Shoeibi” cited in the PTO-892), and PSP Blog, 2015, https://psp-blog.org/tag/o-glcnacase/, cited in the PTO-892), and Alectos, 2016, http://alectos.com/alectos-content/index.php/2016/04/20/alectos-therapeutics-announces-fda-orphan-drug-designation-mk-8719-investigational-small-molecule-oga-inhibitor-treatment-progressive-supranuclear-palsy/, cited in the PTO-892). Although the claims at issue are not identical, they are not patentably distinct from each other because:
Instant claims 1-15 and 19-20 recites “a method of treating Progressive Supranuclear Palsy in a human subject in need thereof, comprising administering to the human subject a unit dosage forms comprising the compound of formula (I) or a pharmaceutically acceptable salt, solvate, or tautomer thereof, wherein the unit dosage form is administered in a dose and at a daily dosing frequency sufficient to maintain plasma trough concentration of the compound of formula (I) and/or its tautomer at steady state at least about 35 ng/mL at trough in a range of about 45 -2000 ng/mL at trough, a plasma Cmax of the compound of formula (I) of about 1650-7390 ng/mL, a plasma AUC over 24 hours of the compound of formula (I) of about 13850-90500 ng*h/mL, wherein the dose of the compound of formula (I) is administered orally in the range of about 150 mg to about 500 mg twice a day or thrice a day, wherein the human subject suffers from a disease or condition, or is at increased risk of developing a disease or condition, wherein the compound is administered in form of a pharmaceutically usable solvate and/or salt thereof, wherein the compound is administered in form of its hydrochloride salt:
PNG
media_image3.png
122
326
media_image3.png
Greyscale
US Patent No. 11,046,712 B2recites in claim 1 a compound of formula (I), and recites in claim 8 compound 44, and recites in claims 9-12, a method of treating a disease by administering therapeutically effective amount of compound of formula (I), wherein the disease Progressive supranuclear palsy:
PNG
media_image4.png
188
456
media_image4.png
Greyscale
US Patent No. 11,046,712 B2does not recites the amount of the compound administered, or the claimed pharmacokinetics. Also, one of ordinary skill in the art need to specifically pick PSP from the diseases and conditions list.
Quattropani III teaches compound of formula I, [0001], and compound N-(5-(4-(1-(Benzo[d][1,3]dioxol-5-yl)ethyl)piperazin-1-yl)-1,3,4-thiadiazol-2-yl)acetamide as species of formula I [0083, Table 1, comp. 69], for treating tauopathies and Alzheimer's disease. [00164], wherein the compound administered in doses of approximately 0.5 to 1000 mg, more preferably between 1 and 700 mg, most preferably 5 and 100 mg per dose unit [0154].
Zhu, Shoeibi, PSP Blog and Alectos teach as discussed above, page 7-8.
The obviousness rationale is the same as the obviousness rationale of the above 103 Rejection, page 8-9.
Non-statutory Double Patenting over US Patent No. 11,591,327 B2
Claims 1-15 and 19-20 are rejected on the ground of nonstatutory double patenting as being unpatentable over claims 1-4 of US Patent No. 11,591,327 B2 (cited in the IDS dated 04/02/2024), in view of a, Quattropani et al. (US PG-PUB , 10/19/2017, “Quattropani III” cited in the PTO-892), Y. Zhu, et al. ACS Chem. Neurosci. 2018/06/20, VL - 9, IS - 6, pp. 1366-1379, “Zhu” cited in the PTO-892), A. Shoeibi, et al. Expert Opinion on Investigational Drugs, 2018, 27:4, 349-361, “Shoeibi” cited in the PTO-892), and PSP Blog, 2015, https://psp-blog.org/tag/o-glcnacase/, cited in the PTO-892), and Alectos, 2016, http://alectos.com/alectos-content/index.php/2016/04/20/alectos-therapeutics-announces-fda-orphan-drug-designation-mk-8719-investigational-small-molecule-oga-inhibitor-treatment-progressive-supranuclear-palsy/, cited in the PTO-892). Although the claims at issue are not identical, they are not patentably distinct from each other because:
Instant claims 1-15 and 19-20 recites “a method of treating Progressive Supranuclear Palsy in a human subject in need thereof, comprising administering to the human subject a unit dosage forms comprising the compound of formula (I) or a pharmaceutically acceptable salt, solvate, or tautomer thereof, wherein the unit dosage form is administered in a dose and at a daily dosing frequency sufficient to maintain plasma trough concentration of the compound of formula (I) and/or its tautomer at steady state at least about 35 ng/mL at trough in a range of about 45 -2000 ng/mL at trough, a plasma Cmax of the compound of formula (I) of about 1650-7390 ng/mL, a plasma AUC over 24 hours of the compound of formula (I) of about 13850-90500 ng*h/mL, wherein the dose of the compound of formula (I) is administered orally in the range of about 150 mg to about 500 mg twice a day or thrice a day, wherein the human subject suffers from a disease or condition, or is at increased risk of developing a disease or condition, wherein the compound is administered in form of a pharmaceutically usable solvate and/or salt thereof, wherein the compound is administered in form of its hydrochloride salt:
PNG
media_image3.png
122
326
media_image3.png
Greyscale
US Patent No. 11,591,327B2 recites a hydrochloric acid salt of N-(5-(4-(1-(Benzo[d][1,3]dioxol-5-yl)ethyl)piperazin-1-yl)-1,3,4-thiadiazol-2-yl)acetamide mono-hydrochloride, and solid oral dosage form comprising the compound:
PNG
media_image4.png
188
456
media_image4.png
Greyscale
US Patent No. 11,591,327 B2 does not recites using the above compound for treating PSP, the amount of the compound administered, or the claimed pharmacokinetics. Also, one of ordinary skill in the art need to specifically pick PSP from the diseases and conditions list.
However, US Patent No. 11,591,327 B2 specification recites a method for treating PSP using compound N-(5-(4-(1-(Benzo[d][1,3]dioxol-5-yl)ethyl)piperazin-1-yl)-1,3,4-thiadiazol-2-yl)acetamide, [col. 10, ln. 47]. 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).
Moreover, Quattropani III teaches compound of formula I, [0001], and compound N-(5-(4-(1-(Benzo[d][1,3]dioxol-5-yl)ethyl)piperazin-1-yl)-1,3,4-thiadiazol-2-yl)acetamide as species of formula I [0083, Table 1, comp. 69], for treating PSP [00164], wherein the compound administered in doses of approximately 0.5 to 1000 mg, more preferably between 1 and 700 mg, most preferably 5 and 100 mg per dose unit [0154].
Zhu, Shoeibi, PSP Blog and Alectos teach as discussed above, page 7-8.
The obviousness rationale is the same as the obviousness rationale of the above 103 Rejection, page 8-9.
Non-statutory Double Patenting over co-pending Application No 18/062,295
Claims 1-15 and 19-20 are provisionally rejected on the ground of nonstatutory double patenting as being unpatentable over claims 15-39 of co-pending Application No 18/062,295 (US PG-PUB 2023/0120169 A1 cited in the IDS dated 04/02/2024, now US Patent No 12,398,130 B2 (not published yet)) in view of Quattropani et al. (US PG-PUB , 10/19/2017, “Quattropani III” cited in the PTO-892), Y. Zhu, et al. ACS Chem. Neurosci. 2018/06/20, VL - 9, IS - 6, pp. 1366-1379, “Zhu” cited in the PTO-892), A. Shoeibi, et al. Expert Opinion on Investigational Drugs, 2018, 27:4, 349-361, “Shoeibi” cited in the PTO-892), and PSP Blog, 2015, https://psp-blog.org/tag/o-glcnacase/, cited in the PTO-892), and Alectos, 2016, http://alectos.com/alectos-content/index.php/2016/04/20/alectos-therapeutics-announces-fda-orphan-drug-designation-mk-8719-investigational-small-molecule-oga-inhibitor-treatment-progressive-supranuclear-palsy/, cited in the PTO-892). Although the claims at issue are not identical, they are not patentably distinct from each other because:
Instant claims 1-15 and 19-20 recites “a method of treating Progressive Supranuclear Palsy in a human subject in need thereof, comprising administering to the human subject a unit dosage forms comprising the compound of formula (I) or a pharmaceutically acceptable salt, solvate, or tautomer thereof, wherein the unit dosage form is administered in a dose and at a daily dosing frequency sufficient to maintain plasma trough concentration of the compound of formula (I) and/or its tautomer at steady state at least about 35 ng/mL at trough in a range of about 45 -2000 ng/mL at trough, a plasma Cmax of the compound of formula (I) of about 1650-7390 ng/mL, a plasma AUC over 24 hours of the compound of formula (I) of about 13850-90500 ng*h/mL, wherein the dose of the compound of formula (I) is administered orally in the range of about 150 mg to about 500 mg twice a day or thrice a day, wherein the human subject suffers from a disease or condition, or is at increased risk of developing a disease or condition, wherein the compound is administered in form of a pharmaceutically usable solvate and/or salt thereof, wherein the compound is administered in form of its hydrochloride salt:
PNG
media_image3.png
122
326
media_image3.png
Greyscale
Co-pending Application No 18/062,295 recites in claim 15 a compound of formula (I), and recites in claim 25 compound N-(5-(4-(1-(Benzo[d][1,3]dioxol-5-yl)ethyl)piperazin-1-yl)-1,3,4-thiadiazol-2-yl)acetamide as species of formula (I), recites in claim 26 the hydrochloric acid salt of the compound, recites in claim 19 an oral solid dosage of the compound, and recites in claims 20-21, a method of treating a disease by administering the compound of formula (I), wherein the disease is PSP:
PNG
media_image5.png
122
271
media_image5.png
Greyscale
Co-pending Application No 18/062,295 does not recites the amount of the compound administered, or the claimed pharmacokinetics. Also, one of ordinary skill in the art need to specifically pick PSP from the diseases and conditions list.
Quattropani teaches compound of formula I, [0001], and compound N-(5-(4-(1-(Benzo[d][1,3]dioxol-5-yl)ethyl)piperazin-1-yl)-1,3,4-thiadiazol-2-yl)acetamide as species of formula I [0083, Table 1, comp. 69], for treating Progressive Supranuclear Palsy, etc. [00164], wherein the compound administered in doses of approximately 0.5 to 1000 mg, more preferably between 1 and 700 mg, most preferably 5 and 100 mg per dose unit [0154].
Zhu, Shoeibi, PSP Blog and Alectos teach as discussed above, page 7-8.
The obviousness rationale is the same as the obviousness rationale of the above 103 Rejection, page 8-9.
Response to Arguments
Applicant argues:
As an initial matter, the claims of US Patent No. 10,336,775 B2 are directed to compounds and/or pharmaceutical compositions comprising OGA inhibitors, as opposed to being directed to methods of treatment, let alone methods defined by specific pharmacokinetic parameters. By contrast, the claims of the present application are directed to methods of treating Progressive Supranuclear Palsy defined by specific and clinically significant steady-state pharmacokinetic parameters. The present claims thus differ fundamentally in statutory category, scope, and substance from the claims of the reference patent. A claim to a method of treatment defined by specific PK endpoints is not merely an obvious variant of a claim to a compound or composition; it represents a fundamentally different invention.
Examiner response:
Applicant's arguments have been fully considered but they are not persuasive. Applicant argues that “in a nonstatutory double patenting analysis, the specification of the reference patent may be used only as a dictionary to construe the meaning of terms appearing in the reference claims and it cannot be used to import unclaimed subject matter into the scope of those claims, however, 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). US Patent No. 10,696,668B2 specification recites a method for treating PSP using compound N-(5-(4-(1-(Benzo[d][1,3]dioxol-5-yl)ethyl)piperazin-1-yl)-1,3,4-thiadiazol-2-yl)acetamide, [col. 10, ln. 49], and the combination of Zhu, Shoeibi, PSP Blog and Alectos provide support to skilled artisan to pick PSP from the diseases and conditions listed in the patent No. 10,696,668B2, see the obviousness rationale at pages 8-9. With regard to Applicant arguments on the pharmacokinetics of the claimed compound, see the response above, page 12-13.
Conclusion
Claims 1-15 and 19-20 are rejected. No claim is allowed.
Applicant's amendment necessitated the new ground(s) of rejection presented in this Office action. Accordingly, THIS ACTION IS MADE FINAL. See MPEP § 706.07(a). Applicant is reminded of the extension of time policy as set forth in 37 CFR 1.136(a).
A shortened statutory period for reply to this final action is set to expire THREE MONTHS from the mailing date of this action. In the event a first reply is filed within TWO MONTHS of the mailing date of this final action and the advisory action is not mailed until after the end of the THREE-MONTH shortened statutory period, then the shortened statutory period will expire on the date the advisory action is mailed, and any nonprovisional extension fee (37 CFR 1.17(a)) pursuant to 37 CFR 1.136(a) will be calculated from the mailing date of the advisory action. In no event, however, will the statutory period for reply expire later than SIX MONTHS from the mailing date of this final action.
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.
Examiner interviews are available via telephone, in-person, and video conferencing using a USPTO supplied web-based collaboration tool. To schedule an interview, applicant is encouraged to use the USPTO Automated Interview Request (AIR) at http://www.uspto.gov/interviewpractice.
If attempts to reach the examiner by telephone are unsuccessful, the examiner’s supervisor, James H Alstrum-Acevedo can be reached at 571-272-5548. The fax phone number for the organization where this application or proceeding is assigned is 571-273-8300.
Information regarding the status of published or unpublished applications may be obtained from Patent Center. Unpublished application information in Patent Center is available to registered users. To file and manage patent submissions in Patent Center, visit: https://patentcenter.uspto.gov. Visit https://www.uspto.gov/patents/apply/patent-center for more information about Patent Center and https://www.uspto.gov/patents/docx for information about filing in DOCX format. For additional questions, contact the Electronic Business Center (EBC) at 866-217-9197 (toll-free). If you would like assistance from a USPTO Customer Service Representative, call 800-786-9199 (IN USA OR CANADA) or 571-272-1000.
/M.M.A./Examiner, Art Unit 1622
/JAMES H ALSTRUM-ACEVEDO/Supervisory Patent Examiner, Art Unit 1622
Prosecution Insights