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 .
Receipt of claim amendments and arguments filed on 04/23/2026 is acknowledged. Claims 1, 5-10 and 13-28 are now pending.
Priority Information
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Applicant’s claim for the benefit of a prior-filed application under 35 U.S.C. 119(e) or under 35 U.S.C. 120, 121, 365(c), or 386(c) is acknowledged. However, the claims contain subject matter that is not present in, and is not supported by, a priority document under 35 U.S.C. 119(e).
The later-filed application must be an application for a patent for an invention which is also disclosed in the prior application (the parent or original nonprovisional application or provisional application). The disclosure of the invention in the parent application and in the later-filed application must be sufficient to comply with the requirements of 35 U.S.C. 112(a) or the first paragraph of pre-AIA 35 U.S.C. 112, except for the best mode requirement. See Transco Products, Inc. v. Performance Contracting, Inc., 38 F.3d 551, 32 USPQ2d 1077 (Fed. Cir. 1994).
The disclosure of the prior-filed application, Application No. 61/121,379, fails to provide adequate support or enablement in the manner provided by 35 U.S.C. 112(a) or pre-AIA 35 U.S.C. 112, first paragraph for the compounds in claims 1-14 of this application.
Therefore, the instant application cannot receive the benefit of its earlier filing date under 35 U.S.C. 119(e). The effective filing date of the instant application is thus, 10/26/2015.
Response to Election/Restriction
Applicant previously elected Group I, claims 1-14, drawn to a compound of formula (I)
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and a method of treating Parkinson’s disease, Alzheimer’s disease and multiple sclerosis, in the reply filed on November 14, 2025. Election of the species compound of formula
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, and Alzheimer’s disease, was also acknowledged.
Claims 15-26 were withdrawn from further consideration pursuant to 37 CFR 1.142(b) as being drawn to nonelected invention(s), there being no allowable generic or linking claim. Applicant timely traversed the restriction (election) requirement in the reply filed on November 14, 2025.
Examination
The claims were amended to remove methyl from R5, the elected species is not encompassed by the amended claims. For the purpose of a compact prosecution, examination was expanded to the full scope of compounds of claim 1
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. Claim 1, 5-10, 13-14 and 27-28 have been fully search.
Claims 15-26 are withdrawn from further consideration pursuant to 37 CFR 1.142(b), as being drawn to non-elected inventions there being no allowable generic or linking claim.
Terminal Disclaimer
The terminal disclaimers filed on 04/23/2026 disclaiming the terminal portion of any patent granted on this application which would extend beyond the expiration date of US 11,219,623, 11,998,547, 11,717,520 and 12,097,201 have been reviewed and are accepted. The terminal disclaimers have been recorded.
All rejections and objections not reiterated herein have been withdrawn in view of the claim amendments and Terminal Disclaimers.
Claims 1, 5-10, 13-14 and 27-28 are the subject of this Final Office Action.
Claim Rejections - 35 USC § 102
The following is a quotation of the appropriate paragraphs of 35 U.S.C. 102 that form the basis for the rejections under this section made in this Office action:
A person shall be entitled to a patent unless –
(a)(1) the claimed invention was patented, described in a printed publication, or in public use, on sale, or otherwise available to the public before the effective filing date of the claimed invention.
Claim(s) 1, 5-6 and 8 remain rejected under 35 U.S.C. 102(a)(1) as being anticipated by Doncel et al. (US 2011/0039798).
The prior art teaches nucleoside derivatives of formula
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and their pharmaceutical compositions for treating viral diseases in a subject. See particularly, Figure 3a, claims 1 and 27-29. The prior art teaches that these are fatty acyl substituted analogues of lamivudine.
Exemplary embodiments of formula III can be found in at least Figure 5:
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,
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and
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. In formula II, R5 is an acyl, both of R2 are H, or one R2 is H and the other is an acyl or a substituted alkyl. The instant specification discloses that alkyl groups can optionally be substituted [00148].
Regarding claim 8, wherein one R2 is H and one R2 is C1-C4-alkyl, this is anticipated by compounds 13, 14 and 15 of the reference described above, since -NH-DMTr is the group of formula
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in which a C1-alkyl is substituted by three phenyl groups. The instant specification discloses that alkyl groups can optionally be substituted [00148].
Claim(s) 1, 6 and 7 remain rejected under 35 U.S.C. 102(a)(1) as being anticipated by Dang et al. (Mendeleev Commun., 2015, 25, 96-98).
The prior art teaches the synthesis of lamivudine derivatives compound 15
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and
compound 16
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. These read on formula II of the claims when R5 is acyl, and both R2 are acyl or C1-alkyl substituted by an oxo and alkoxy group, or a C3-alkyl chain with an insertion of an oxygen atom and substituted by an oxo. The instant specification discloses that alkyl groups can optionally be substituted and have inserted along the alkyl chain an oxygen atom[00148]. These compounds are to be used in the treatment of HIV. See at least table 1.
Applicant’s arguments were considered but were found unpersuasive. Applicant argues that the limitations of claims 4 and 11 have been incorporated into claim 1, and that since claim 11 was not subject to these rejections, Doncel and Dang do not anticipate claim 1. This is unpersuasive because R5 in claim 1 is not limited to the limitations of claim 11. Claim 1 was not amended to remove the anticipated subject matter for R5 (acyl).
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.
Claims 1, 5-10, 13-14 and 27-28 are rejected on the ground of nonstatutory double patenting as being unpatentable over claims 1-6 and 11-13 of U.S. Patent No. 10,864,212. Although the claims at issue are not identical, they are not patentably distinct from each other because the methods and compounds of the instant claims are prima facie obvious variants of the method of treating Alzheimer’s disease, Parkinson’s disease and multiple sclerosis with compound of formula
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of the patented claims.
Instant claims recite compounds of formula II
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and method for the treatment of Alzheimer’s disease, Parkinson’s disease and multiple sclerosis with the same, wherein R2 is H or alkyl, such as methyl, ethyl, etc., and R5 is ethyl, n-propyl, etc. The claimed compounds inhibit inflammasome activation by Alu RNA.
Determination of the scope and contents of prior art
Patented claims 1-6 and 11-13 recite a method for treating Alzheimer’s disease with compounds of formula
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, or
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, wherein the compounds are also inhibitors of inflammasome activation by Alu RNA.
Ascertaining the differences between claims of patent and claims at issue
The difference between the claims in the patent and the instant claimed compounds is that some claimed compounds (e.g. wherein R5 = CH2CH3, CH2CH2CH3, CH2CH2CH3, (CH2)3CH3, etc.) are homologs of the compound in the patented claims (e.g. vs. CH3), differing only by the successive addition of the same chemical group –CH2- on the group
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. Some other claimed compounds have one methyl or longer alkyl chain (ethyl, propyl or butyl) at the nitrogen atom instead of a hydrogen atom.
Finding of prima facie obviousness--rational and motivation (MPEP §2142-2413)
Compounds that differ only by the presence or absence of an extra methyl group or two are homologues. Homologues are of such close structural similarity that the disclosure of a compound renders prima facie obvious its homologue. As was stated in In re Grose, 201 USPQ 57, 63, “The known structural relationship between adjacent homologues, for example, supplies a chemical theory upon which a prima facie case of obviousness of a compound may rest.” The homologue is expected to be preparable by the same method and to have generally the same properties. This expectation is then deemed the motivation for preparing homologues. This circumstance has arisen many times. See specifically In re Shetty, 195 USPQ 753; In re Wilder, 195 USPQ 426 and Ex Parte Greshem, 121 USPQ 422, all of which feature a compound with a C2 link rejected over a compound with a C1 link. Similarly, In re Chupp, 2 USPQ2d 1437 and In re Coes, 81 USPQ 369 have a compound with a C1 link unpatentable over prior art showing C2 link. Note Ex parte Agouridas, 65 USPQ2d 1142, where a C4 chain was held obvious over a C3 chain. Note also In re Schaub, 190 USPQ 324, 326, where compounds with C5 and C6 chains were called “adjacent homologs in the classic sense”. Ex parte Ruddy, 121 USPQ 427 has a C3 link unpatentable over a C1 link. Ex parte Nathan, 121 USPQ 349 found the insertion of a C2H4 link obvious. In all of these cases, the variation was found to be obvious on the basis of close structural similarity; no secondary teaching was employed.
Of course, these presumptions are rebuttable by the showing of unexpected effects, but initially, the homologues are obvious even in the absence of a specific teaching to add or remove methyl groups. MPEP 2144.09, second paragraph, states, “Compounds which are position isomers or homologs are generally of sufficiently close structural similarity that there is a presumed expectation that such compounds possess similar properties.” In re Wilder, 563 F.2d 457, 195 USPQ 426 (CCPA 1977).
As was stated directly in THE GENERAL TIRE & RUBBER COMPANY v. JEFFERSON CHEMICAL COMPANY, INC., 182 USPQ 70 (1974): “If any structural change is obvious to one skilled in the art, a substitution of the next higher homolog would seem to be.” Note also In re Jones, 21 USPQ2d 1942, which states at 1943 “Particular types or categories of structural similarity without more, have, in past cases, given rise to prima facie obviousness”; one of those listed is “adjacent homologues and structural isomers”. Similar is In re Schechter and LaForge, 98 USPQ 144, 150, which states “a novel useful chemical compound which is homologous or isomeric with compounds of the prior art is unpatentable unless it possesses some unobvious or unexpected beneficial property not possessed by the prior art compounds.” Note also In re Deuel 34 USPQ2d 1210, 1214 which states, “Structural relationships may provide the requisite motivation or suggestion to modify known compounds to obtain new compounds. For example, a prior art compound may suggest its homologs because homologs often have similar properties and therefore chemists of ordinary skill would ordinarily contemplate making them to try to obtain compounds with improved properties.” This rejection is in accordance with MPEP 2144.09.
It would be routine for the chemist to make such a small change, that is, from a hydrogen to a methyl group, from a methyl group to ethyl, propyl and butyl, inorder to produce additional compounds with the same utility. To those skilled in chemical art, one homologue is not such an advance over adjacent member of series as requires invention because chemists knowing properties of one member of series would in general know what to expect in adjacent members. In re Henze, 85 USPQ 261 (1950).
In summary, there have been numerous cases where creating an adjacent homolog has been considered sufficient reason for a chemist to modify a known compound “because homologs often have similar properties and therefore chemists of ordinary skill would ordinarily contemplate making them to try to obtain compounds with improved properties.” (In re Deuel 34 USPQ2d 1210, 1214).
Claims 1, 5-10 and 13 are rejected on the ground of nonstatutory double patenting as being unpatentable over claims 12 and 13 of U.S. Patent No. 9,326,983. Although the claims at issue are not identical, they are not patentably distinct from each other because the compounds of the instant claims are prima facie obvious variants of the compound of formula
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of the patented claims.
Instant claims recite compounds of formula II
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, wherein R2 is H or alkyl, such as methyl, ethyl, etc., and R5 is ethyl, n-propyl, etc. The claimed compounds inhibit inflammasome activation by Alu RNA.
Patented claims 12 and 13 of the patent disclose a compound of formula
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, which is also an inhibitor of inflammasome activation by Alu RNA.
Ascertaining the differences between claims of patent and claims at issue
The difference between the compound in the patent and the instant claimed compounds is that the claimed compounds (e.g. wherein R5 = CH2CH3, CH2CH2CH3, CH2CH2CH3, (CH2)3CH3, etc.) are homologs of the compound in the patented claims (e.g. vs. CH3), differing only by the successive addition of the same chemical group –CH2- on the group
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. Some other claimed compounds have one methyl or longer alkyl chain (ethyl, propyl or butyl) at the nitrogen atom instead of a hydrogen atom.
Finding of prima facie obviousness--rational and motivation (MPEP §2142-2413)
Compounds that differ only by the presence or absence of an extra methyl group or two are homologues. Homologues are of such close structural similarity that the disclosure of a compound renders prima facie obvious its homologue. As was stated in In re Grose, 201 USPQ 57, 63, “The known structural relationship between adjacent homologues, for example, supplies a chemical theory upon which a prima facie case of obviousness of a compound may rest.” The homologue is expected to be preparable by the same method and to have generally the same properties. This expectation is then deemed the motivation for preparing homologues. This circumstance has arisen many times. See specifically In re Shetty, 195 USPQ 753; In re Wilder, 195 USPQ 426 and Ex Parte Greshem, 121 USPQ 422, all of which feature a compound with a C2 link rejected over a compound with a C1 link. Similarly, In re Chupp, 2 USPQ2d 1437 and In re Coes, 81 USPQ 369 have a compound with a C1 link unpatentable over prior art showing C2 link. Note Ex parte Agouridas, 65 USPQ2d 1142, where a C4 chain was held obvious over a C3 chain. Note also In re Schaub, 190 USPQ 324, 326, where compounds with C5 and C6 chains were called “adjacent homologs in the classic sense”. Ex parte Ruddy, 121 USPQ 427 has a C3 link unpatentable over a C1 link. Ex parte Nathan, 121 USPQ 349 found the insertion of a C2H4 link obvious. In all of these cases, the variation was found to be obvious on the basis of close structural similarity; no secondary teaching was employed.
Of course, these presumptions are rebuttable by the showing of unexpected effects, but initially, the homologues are obvious even in the absence of a specific teaching to add or remove methyl groups. MPEP 2144.09, second paragraph, states, “Compounds which are position isomers or homologs are generally of sufficiently close structural similarity that there is a presumed expectation that such compounds possess similar properties.” In re Wilder, 563 F.2d 457, 195 USPQ 426 (CCPA 1977).
As was stated directly in THE GENERAL TIRE & RUBBER COMPANY v. JEFFERSON CHEMICAL COMPANY, INC., 182 USPQ 70 (1974): “If any structural change is obvious to one skilled in the art, a substitution of the next higher homolog would seem to be.” Note also In re Jones, 21 USPQ2d 1942, which states at 1943 “Particular types or categories of structural similarity without more, have, in past cases, given rise to prima facie obviousness”; one of those listed is “adjacent homologues and structural isomers”. Similar is In re Schechter and LaForge, 98 USPQ 144, 150, which states “a novel useful chemical compound which is homologous or isomeric with compounds of the prior art is unpatentable unless it possesses some unobvious or unexpected beneficial property not possessed by the prior art compounds.” Note also In re Deuel 34 USPQ2d 1210, 1214 which states, “Structural relationships may provide the requisite motivation or suggestion to modify known compounds to obtain new compounds. For example, a prior art compound may suggest its homologs because homologs often have similar properties and therefore chemists of ordinary skill would ordinarily contemplate making them to try to obtain compounds with improved properties.” This rejection is in accordance with MPEP 2144.09.
It would be routine for the chemist to make such a small change, that is, from a hydrogen to a methyl group, methyl to ethyl, propyl and butyl, in order to produce additional compounds with the same utility. To those skilled in chemical art, one homologue is not such an advance over adjacent member of series as requires invention because chemists knowing properties of one member of series would in general know what to expect in adjacent members. In re Henze, 85 USPQ 261 (1950).
In summary, there have been numerous cases where creating an adjacent homolog has been considered sufficient reason for a chemist to modify a known compound “because homologs often have similar properties and therefore chemists of ordinary skill would ordinarily contemplate making them to try to obtain compounds with improved properties.” (In re Deuel 34 USPQ2d 1210, 1214).
Applicant’s arguments were considered but were found unpersuasive.
Applicant argues that a person having ordinary skill would not have had reason to select the R5 position in this molecule for modification out of the multiple options available. Applicant also argues that there would not be motivation to do so because the desired prevention of phosphorylation is achieved by the addition of the methyl group at R5 position and that further homologation at this position would not have been expected to have any further effect, other than potentially disrupt the binding to the desired target. The examiner is not persuaded because as in In re Deuel 34 USPQ2d 1210, 1214, the expectation for homologs is that they will often have similar properties, and therefore chemists of ordinary skill would ordinarily contemplate making them to try to obtain compounds with improved properties. In addition, there is no teaching/suggestion or evidence in the art that doing so would have been expected to disrupt the binding to the desired target.
Conclusion
Claims 1, 5-10, 13-14 and 27-28 are rejected. No claim is in condition for allowance.
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 VALERIE RODRIGUEZ-GARCIA whose telephone number is (571)270-5865. The examiner can normally be reached Monday-Friday 9:30am-5:30pm.
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If attempts to reach the examiner by telephone are unsuccessful, the examiner’s supervisor, Clinton Brooks can be reached at 571-270-7682. The fax phone number for the organization where this application or proceeding is assigned is 571-273-8300.
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/VALERIE RODRIGUEZ-GARCIA/Primary Examiner, Art Unit 1621
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