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 .
Status of the Claims
Claims 1-13 are pending. Acknowledgment is made of the amendment of claims 1, 2, 5, 6, 10, and 12 in the reply filed 03/31/2026. Claims 9 and 11 are withdrawn.
Restriction/Election Requirement
Applicant elected, in the reply filed on 09/30/2025, without traverse of Group I, directed to a compound of formula (I) or a composition thereof. Applicant further elected the species compound 58, shown below, which reads on claims 1-8, 10, 12, and 13. Examination has been limited to the elected species below and any 35 U.S.C. 102 prior art discovered in the search.
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Claims 9 and 11 are withdrawn from further consideration pursuant to 37 CFR 1.142(b) as being drawn to a nonelected species, there being no allowable generic or linking claim. Election was made without traverse in the reply filed on 09/30/2025.
Withdrawn Objections/Rejections
Applicant’s amendment to the claims, filed 03/31/2026, overcomes the objection to claim 5 for minor informalities. The objection to claim 5 has been withdrawn.
Applicant’s amendment to the claims, filed 03/31/2026, overcomes the rejection to claims 1-3, 8, and 13 under 35 U.S.C. 112(a) for scope of enablement. The rejection of claims 1-3, 8, and 13 has been withdrawn.
Applicant’s amendment to the claims, filed 03/31/2026, overcomes the rejection to claims 1, 3, 8, and 13 are rejected under 35 U.S.C. 102(a)(2) as being anticipated by Poudel et al. (US 20200038403 A1). The rejection of claims 1, 3, 8, and 13 has been withdrawn.
Maintained Objections
Claim Objections
Claims 10 and 12 are objected to because of the following informalities:
Claim 10 reads “…wherein R3 is: … wherein R5 is selected from:
-CH(CH3)NHCH2CH2CH3, and piperazinyl.” (emphasis added where comma should be removed).
Rule 1.141(a) states:
Two or more independent and distinct inventions may not be claimed in one national application, except that more than one species of an invention, not to exceed a reasonable number, may be specifically claimed in different claims in one national application, provided the application also includes an allowable claim generic to all the claimed species and all the claims to species in excess of one are written in dependent form (§ 1.75) or otherwise include all the limitations of the generic claim.
Claim 12 claims a large number of species of the generic claim, but in independent format. Multiple inventions may not be claimed in a single application unless they are species claims which are dependent upon the larger, generic claim. In the past, the Office has held a “reasonable number” to be five (5) species. The present claim contains well over this number of species. One could envision forty pages of species compounds in a single claim which is not dependent upon any genus claim. This would cause undue burden to the Office in examining such a large claim. Therefore, it is recommended that claim 12 either be dependent from a larger, genus claim, or, that claim 12 incorporate all of the limitations of the genus claim.
Appropriate correction is required.
Applicant Argues:
Applicant argues that claim 12 contains all the limitations of the generic claim.
Examiner Responds:
Claim 12 contains numerous compounds that do not contain all the limitations of the genus claim. For example, all of the compounds shown below (from claim 12) do not read on the genus claim, since claim 1 teaches that:
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(key group circled for emphasis)
and that RC is:
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(key group circled for emphasis)
Therefore, the compounds shown below are missing a -CH2- group required by the genus claim, between the connection of RC and either RA or RB.
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Maintained/Modified Rejections
Claim Rejections - 35 USC § 112
The following is a quotation of 35 U.S.C. 112(d):
(d) REFERENCE IN DEPENDENT FORMS.—Subject to subsection (e), a claim in dependent form shall contain a reference to a claim previously set forth and then specify a further limitation of the subject matter claimed. A claim in dependent form shall be construed to incorporate by reference all the limitations of the claim to which it refers.
The following is a quotation of pre-AIA 35 U.S.C. 112, fourth paragraph:
Subject to the following paragraph [i.e., the fifth paragraph of pre-AIA 35 U.S.C. 112], a claim in dependent form shall contain a reference to a claim previously set forth and then specify a further limitation of the subject matter claimed. A claim in dependent form shall be construed to incorporate by reference all the limitations of the claim to which it refers.
Claims 10 and 11 are rejected under 35 U.S.C. 112(d) or pre-AIA 35 U.S.C. 112, 4th paragraph, as being of improper dependent form for failing to further limit the subject matter of the claim upon which it depends, or for failing to include all the limitations of the claim upon which it depends.
Claim 10 recites a compound of claim 6 where R3 is
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. Claim 11 recites a compound of claim 6 where R3 is
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. However, claim 6 recites that R3 is
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or
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. Therefore, claims 10 and 11 add an additional -CH2- group that is not present in the R3 group of claim 6, and expand the scope of the claim upon which they depend.
Applicant may cancel the claim(s), amend the claim(s) to place the claim(s) in proper dependent form, rewrite the claim(s) in independent form, or present a sufficient showing that the dependent claim(s) complies with the statutory requirements.
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)(2) the claimed invention was described in a patent issued under section 151, or in an application for patent published or deemed published under section 122(b), in which the patent or application, as the case may be, names another inventor and was effectively filed before the effective filing date of the claimed invention.
Claims 1-5, 8, and 13 are rejected under 35 U.S.C. 102(a)(2) as being anticipated by Poudel et al. (U.S. Patent No. 11,400,094 B2), hereinafter referred to as patent ‘094, with an effectively filed date of 08/03/2018.
Patent ‘094 teaches, in claim 1, compounds of formula (II), shown below.
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Patent ‘094 teaches several compounds that read on the instant claims, including compounds IIa-30 to IIa-34, shown below from Table A. For example, compound IIa-32 reads on instant claims 1-5, 8, and 13, where both instances of R1 are H, one instance of R2 is H, the other R2 is n-butyl, R3 is benzyl substituted by two R5 groups, where one R5 is methoxy and the other is -CH2-pyrrolidinyl.
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Claim Rejections - 35 USC § 103
The following is a quotation of 35 U.S.C. 103 which forms the basis for all obviousness rejections set forth in this Office action:
A patent for a claimed invention may not be obtained, notwithstanding that the claimed invention is not identically disclosed as set forth in section 102, if the differences between the claimed invention and the prior art are such that the claimed invention as a whole would have been obvious before the effective filing date of the claimed invention to a person having ordinary skill in the art to which the claimed invention pertains. Patentability shall not be negated by the manner in which the invention was made.
The factual inquiries for establishing a background for determining obviousness under 35 U.S.C. 103 are summarized as follows:
1. Determining the scope and contents of the prior art.
2. Ascertaining the differences between the prior art and the claims at issue.
3. Resolving the level of ordinary skill in the pertinent art.
4. Considering objective evidence present in the application indicating obviousness or nonobviousness.
This application currently names joint inventors. In considering patentability of the claims the examiner presumes that the subject matter of the various claims was commonly owned as of the effective filing date of the claimed invention(s) absent any evidence to the contrary. Applicant is advised of the obligation under 37 CFR 1.56 to point out the inventor and effective filing dates of each claim that was not commonly owned as of the effective filing date of the later invention in order for the examiner to consider the applicability of 35 U.S.C. 102(b)(2)(C) for any potential 35 U.S.C. 102(a)(2) prior art against the later invention.
Claims 6, 7, 10, and 12 are rejected under 35 U.S.C. 103 as being unpatentable over Poudel et al. (U.S. Patent No. 11,400,094 B2), hereinafter referred to as patent ‘094, as applied to claims 1-5, 8, and 13 above.
Patent ‘094 teaches Compound IIa-02 in Table A, shown below.
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Compound IIa-02 differs from the elected species in that it is a homolog of the elected species.
The CCPA has defined a homologous series as a family of chemically related compounds, the composition of which varies from member to member by a -CH2 (one atom of carbon and two hydrogen). In re Coes, Jr. (CCPA 1949) 173 F2d 1012, 81 USPQ 369. The Court of Appeals for the District of Columbia applied a broader definition and defined a homolog (homologue) as a member of a series of compounds in which each member differs from the next member by a constant number of atoms. Carr. Pats.v. Deutsche Gold-und-Sllber, etc. (CADC 1968) 397 F2d 656,157 USPQ 549.
The "Hass-Henze Doctrine" evolved from three CCPA cases, viz., In re Hass et al. (CCPA 1944) 141 F2d 122 and 127, 60 USPQ 544 and 548; and In re Henze (CCPA 1950) 181 F2d 198, 85 USPQ 261. In the Henze decision, the Court said:
"The nature of homologues and the close relationship the physical and chemical properties of one member of a series bears to adjacent members is such that a presumption of unpatentability arises against a claim directed to a composition of matter, the adjacent homologue of which is old in the art. The burden is on the applicant to rebut that presumption by a showing that the claimed compound possesses unobvious or unexpected beneficial properties not actually possessed by the prior art homologue. It is immaterial that the prior art homologue may not be recognized or known to be useful for the same purpose or to possess the same properties as the claimed compound. The CCPA concluded that because the characteristics normally possessed by members of a homologous series are principally the same, varying gradually from member to member, chemists knowing the properties of one member of a series would in general know what to expect in adjacent members so that a mere difference in degree is not the marked superiority which will ordinarily remove the unpatentability of adjacent homologues of old substances. Contra, where no use for the prior art compound is known. In m Stemniski (CCPA 1971) 444 F2d 581, 170 USPQ 343, and cases cited therein. Whether a compound is patentable over a prior art homologue or isomer is a question to be decided in each case. In re Hass et al., supra."
The 'Hass-Henze Doctrine" stands for the proposition that, "If that which appears at first blush to be obvious though new is shown by evidence not to be obvious then the evidence prevails over surmise or unsupported contention and rejection based on obviousness must fail." In re Papesch (CCPA 1963) 315 F2d 381, 137 USPQ 43, 48. The presumption that homologues are unpatentably obvious is an inference of fact, viz., that adjacent homologs are expected to have similar properties which places a 'burden of persuasion' on the applicant who asserted a contrary fact. In re Mills (CCPA 1960) 281 F2d 218, 126 USPQ 513.
Compounds that differ only by the presence of an extra methyl group are homologs. Homologs are of such close structural similarity that the disclosure of a compound renders prima facie obvious its homolog. The homolog is expected to be capable of preparation by the same method and to have the same properties. This expectation is then deemed the motivation for preparing homologs. Homologs are obvious even in the absence of a specific teaching to methylate, In re Wood 199 USPQ 137; In re Hoke 195 USPQ 148; In re Lohr 137 USPQ 548; In re Magerlein 202 USPQ 473; In re Wiechert 152 USPQ 249; Ex parte Henkel 130 USPQ 474; In re Fauque 121 USPQ 425; In re Druey 138 USPQ 39. In all of these cases, the close structural similarity of two compounds differing by only one (or two) methyl groups sufficed; no specific teaching to methylate was present or required. None of these cases has been overruled and indeed the examiner is unaware of any post Lohr case in which motivation is required to put a methyl group on an old compound.
Therefore, since the instant elected species is a homolog of a prior art compound, Compound IIa-02, and it is taught to be used for the same purpose as the prior art species, as a TLR7 agonist, the instant elected species is rendered prima facie obvious in view of the prior art.
Applicant Argues:
Applicant states that one would not be motivated to test a homolog of a prior art compound because the prior art does not provide biological data for the compound.
Examiner Responds:
Applicant's arguments filed 03/31/2026 have been fully considered but they are not persuasive. The prior art does in fact provide biological data for compound IIa-02. The prior art teaches the TLR7 EC50 of the compound IIa-02 to be 510 nM (Table A). As recited above in the Hass-Henze Doctrine, “The burden is on the applicant to rebut that presumption by a showing that the claimed compound possesses unobvious or unexpected beneficial properties not actually possessed by the prior art homologue.” Therefore, the instant elected species is rendered prima facie obvious because of the absence of unexpected results not possessed by the prior art homologue.
New Objections
Claims 1 and 2 are objected to because of the following informalities:
Claim 1 reads “R3 is selected from…-(CH2)n-(4- to 7-membered monocyclic heterocycloalkyl), -(CH2)n-(5- or 6-membered monocyclic heteroaryl), wherein…”, and should read “R3 is selected from…-(CH2)n-(4- to 7-membered monocyclic heterocycloalkyl), and -(CH2)n-(5- or 6-membered monocyclic heteroaryl), wherein…” (emphasis added).
Claim 1 reads “R7 is independently selected from C1-C6 alkyl, C1-C6 aminoalkyl, wherein…”, and should read “R7 is independently selected from C1-C6 alkyl and C1-C6 aminoalkyl, wherein…” (emphasis added).
Claim 2 reads “…the phenyl moiety of benzyl group…” and should read “…the phenyl moiety of said benzyl group…” (emphasis added).
Appropriate correction is required.
New Rejections
Necessitated by Claim Amendment
Claim Rejections - 35 USC § 112
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 1-3, 8, and 13 are rejected under 35 U.S.C. 112(a) or 35 U.S.C. 112 (pre-AIA ), first paragraph, as failing to comply with the written description requirement. The claim(s) contains subject matter which was not described in the specification in such a way as to reasonably convey to one skilled in the relevant art that the inventor or a joint inventor, or for applications subject to pre-AIA 35 U.S.C. 112, the inventor(s), at the time the application was filed, had possession of the claimed invention.
The MPEP states that the purpose of the written description requirement is to ensure that the inventor had possession, as of the filing date of the application, of the specific subject matter later claimed by him. The courts have stated:
"To fulfill the written description requirement, a patent specification must describe an invention and do so in sufficient detail that one skilled in the art can clearly conclude that "the inventor invented the claimed invention." Lockwood v. American Airlines, Inc., 107 F.3d 1565, 1572, 41 USPQ2d 1961, 1966 (Fed. Cir. 1997); In re Gostelli, 872 F.2d 1008, 1012, 10 USPQ2d 1614, 1618 (Fed. Cir. 1989) ("[T]he description must clearly allow persons of ordinary skill in the art to recognize that [the inventor] invented what is claimed."). Thus, an applicant complies with the written description requirement "by describing the invention, with all its claimed limitations, not that which makes it obvious," and by using "such descriptive means as words, structures, figures, diagrams, formulas, etc., that set forth the claimed invention." Lockwood, 107 F.3d at 1572, 41 USPQ2d at 1966." Regents of the University of California v. Eli Lilly & Co., 43 USPQ2d 1398.
The amendment to claim 1 introduces the proviso that R5 is not
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. This proviso is not supported in the instant specification with respect to compounds represented by formula (I), and therefore this limitation introduces new matter.
Applicant is required to cancel the new matter in the reply to this Office Action.
The following is a quotation of 35 U.S.C. 112(b):
(b) CONCLUSION.—The specification shall conclude with one or more claims particularly pointing out and distinctly claiming the subject matter which the inventor or a joint inventor regards as the invention.
The following is a quotation of 35 U.S.C. 112 (pre-AIA ), second paragraph:
The specification shall conclude with one or more claims particularly pointing out and distinctly claiming the subject matter which the applicant regards as his invention.
Claim 1 is rejected under 35 U.S.C. 112(b) or 35 U.S.C. 112 (pre-AIA ), second paragraph, as being indefinite for failing to particularly point out and distinctly claim the subject matter which the inventor or a joint inventor (or for applications subject to pre-AIA 35 U.S.C. 112, the applicant), regards as the invention.
Claim 1 recites the limitation “R7 is …C1-C6 alkyl, C1-C6 aminoalkyl, wherein said 6- to 11- membered spirocyclic bicyclic heterocycloalkyl group…” (emphasis added). There is insufficient antecedent basis for this limitation in the claim. The phrase “wherein said 6- to 11- membered spirocyclic bicyclic heterocycloalkyl group can be optionally substituted with –(C1-C3 alkylene)-(5- to 7- membered monocyclic heterocycloalkyl)” should be removed from the claim.
The following is a quotation of 35 U.S.C. 112(d):
(d) REFERENCE IN DEPENDENT FORMS.—Subject to subsection (e), a claim in dependent form shall contain a reference to a claim previously set forth and then specify a further limitation of the subject matter claimed. A claim in dependent form shall be construed to incorporate by reference all the limitations of the claim to which it refers.
The following is a quotation of pre-AIA 35 U.S.C. 112, fourth paragraph:
Subject to the following paragraph [i.e., the fifth paragraph of pre-AIA 35 U.S.C. 112], a claim in dependent form shall contain a reference to a claim previously set forth and then specify a further limitation of the subject matter claimed. A claim in dependent form shall be construed to incorporate by reference all the limitations of the claim to which it refers.
Claim 2 is rejected under 35 U.S.C. 112(d) or pre-AIA 35 U.S.C. 112, 4th paragraph, as being of improper dependent form for failing to further limit the subject matter of the claim upon which it depends, or for failing to include all the limitations of the claim upon which it depends.
Claim 2 recites that R5 may be (CH2)n-(5- to 7-membered monocyclic heterocycloalkyl). However, claim 1 recites the proviso that R5 may not be (CH2)-piperazinyl, which would be included in the scope of claim 2. Additionally, claim 2 recites that R7 may be -O-(C1-C6 alkyl), halo, or NH2, but claim 1 from which it depends defined R7 as being selected from C1-6 alkyl or C1-6 aminoalkyl. Therefore, claim 2 expands the scope of the claim upon which it is dependent.
Conclusion
Claims 1-8, 10, 12, and 13 are rejected.
THIS ACTION IS MADE FINAL. 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 RILLA M SAMSELL whose telephone number is (703)756-5841. The examiner can normally be reached Monday-Friday, 7-3.
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If attempts to reach the examiner by telephone are unsuccessful, the examiner’s supervisor, Jeffrey Murray can be reached at (571) 272-9023. The fax phone number for the organization where this application or proceeding is assigned is 571-273-8300.
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/R.M.S./Examiner, Art Unit 1624
/JEFFREY H MURRAY/Supervisory Patent Examiner, Art Unit 1624
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