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 .
DETAILED ACTION
Response to Election/Restriction filed on October 30, 2025. Claims 1-2, 7, 9, 17, 25, 32, 35-36, 39-42, 45, 49-50, 52-53, 55-56, 60-61, 67, 69, 72, 79, 86, 89 are pending in the instant application.
Election/Restrictions
Applicant elected without traverse Group I (drawn to a monocyclic peptide inhibitor) and without traverse SEQ ID NO:1 from List I in the reply filed October 30, 2025.
The restriction is deemed proper and is made FINAL in this office action. Claims 17, 35, 39, 41-42, 49, 52, 55, 72, 89 is withdrawn from consideration as being drawn to a non-elected invention
Claims 1-2, 7, 9, 25, 32, 36, 40, 45, 50, 53, 56, 61, 67, 69, 79, 86 are examined on the merits of this office action.
Claim Objection
Claim 2 is objected to for the following informality: the extra semicolon should be removed following X4 and X9.
Claim Rejections - 35 USC § 112, First Paragraph
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 1-2, 7, 9, 25, 32, 36, 40, 45, 50, 53, 56, 61, 67, 69, 79, 86 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 pre-AIA the inventor(s), at the time the application was filed, had possession of the claimed invention.
MPEP § 2163 states that the written description requirement for a claimed genus may be satisfied through sufficient description of a representative number of species by actual reduction to practice, or by disclosure of relevant, identifying characteristics, i.e., structure or other physical and/or chemical properties, by functional characteristics coupled with a known or disclosed correlation between function and structure, or by a combination of such identifying characteristics, sufficient to show the applicant was in possession of the claimed genus.
Scope of the claims
The claims are directed to a broad genus of IL-23 inhibitory peptides comprising a 16-amino acid sequence in which numerous amino acid positions, including at least nine positions, are defined by alternative amino acids or semi-defined Markush groups. The claims encompass a large number of structurally distinct peptide species possessing IL-23 inhibitory activity. Because multiple amino acid positions permit independent variation, the claims encompass an extensive genus of peptide sequences. The specification therefore must reasonably convey to one of ordinary skill in the art that the inventors were in possession of the full scope of the claimed genus as of the filing date.
Therefore, to meet the written description requirement of 35 U.S.C. § 112, first paragraph, the specification must disclose a representative number of species that meet both the structural and functional limitations of the genus or the specification and/or the prior art must identify the structural elements that correlate to the claimed function in a manner that demonstrates to one of ordinary skill in the art that Applicant was in possession of the claimed genus at the time the application was filed.
Actual Reduction to Practice
MPEP § 2163 states that the written description requirement for a claimed genus may be satisfied through sufficient description of a representative number of species by actual reduction to practice. A “representative number of species” means that the species which are adequately described are representative of the entire genus. Thus, when there is substantial variation within the genus, one must describe a sufficient variety of species to reflect the variation within the genus.
The specification demonstrates that the inventors synthesized and tested approximately 19 peptide species. Experimental data are provide for IL-23 receptor competitive binding, pSTAT3 inhibition, NK cell assays, and stability studies. While these data establish that the disclosed peptide species possess the claimed biological activity, actual reduction to practice of a limited number of individual peptide species does not establish possession of the substantially broader claimed genus encompassing numerous untested peptide variants. The disclosed working examples therefore demonstrate possession of only the specifically exemplified peptides rather than the entire breadth of the claimed genus.
Accordingly, the disclosed examples do not constitute representative species of the claimed genus. Therefore, the instant specification has failed to meet the written description requirement by actual reduction to practice of a representative number of species alone.
Sufficient relevant identifying characteristic
MPEP § 2163 states that the written description requirement for a claimed genus may be satisfied through sufficient description of a representative number of species by actual reduction to practice, or by disclosure of relevant, identifying characteristics, i.e., structure or other physical and/or chemical properties, by functional characteristics coupled with a known or disclosed correlation between function and structure, or by a combination thereof.
The specification discloses the complete amino acid sequences of approximately nineteen representative peptides. However, the claims encompass substantially more peptide sequences than those specifically disclosed. The specification does not identify structural characteristics common to the entire claimed genus that distinguish peptides maintaining IL-23 inhibitory activity from peptides lacking such activity. Instead, the specification merely identifies individual working examples without providing sufficient identifying characteristics demonstrating possession of the full genus. Accordingly, the disclosure does not provide representative species reasonably commensurate with the scope of the claims.
Physical/Chemical Properties
Amino acids differs substantially in their physicochemical properties, including size, charge, hydrophobicity, polarity, aromaticity, steric effects, hydrogen bonding and conformational constraints. Substitutions among amino acids at multiple positions within a peptide may significantly alter peptide folding, receptor recognition, binding affinity, metabolic stability and biological activity. The specification does not disclose that the amino acids recited within the claimed variable positions are functionally interchangeable, nor does it provide experimental evidence demonstrating that substitutions across the claimed alternatives preserve IL-23 inhibitory activity. Accordingly, the disclosure fails to establish that peptides containing the full breadth of claimed amino acid substations possess the claimed functional properties.
Functional characteristics when coupled with a known or disclosed correlation between function and structure:
Although the specification reports biological activity for approximately 19 peptide species, it does not disclose a structure function relationship sufficient to predict activity across the full claimed genus. Specifically, the specification does not demonstrate which amino acid substitutions are tolerated at each variable position, why the claimed alternatives maintain IL-23 inhibition, that amino acids within each semi defined group are functionally equivalent, that substitutions at one position remain effective independent of substitions at the remaining variable positions or any predictive structure activity relationship permitting one of ordinary skill in the art to recognize which members of the claimed genus possess the claimed activity. Instead, the disclosure merely demonstrates that certain specific combinations of amino acids produce active peptides. The functional data therefore establish activity only for the disclosed species and do not reasonably convey possession of the substantially broader claimed genus.
Method of Making
The specification adequately teaches methods for synthesizing peptide inhibitors using conventional peptide synthesis techniques. However, the ability to make peptides throughout the claimed genus does not demonstrate possession of the claimed invention. The written description requirement is distinct from enablement and requires evidence that the inventors were in possession of the claimed genus itself rather than merely providing methods for producing peptides failing within the claim scope. Accordingly, disclosure of peptide synthesis methods does not cure the deficiencies discussed above.
Conclusion
The specification fails to provide an adequate written description of the claimed peptide genus under 35 U.S.C. 112(a). Although the approximately nineteen peptide species are disclosed and experimentally characterized, the claims encompass a substantially broader genus of peptides containing numerous independently variable amino acid positions. The specification neither discloses a sufficient number of representative species commensurate with the breadth of the claims nor identifies structural features or a reliable correlation between peptide structure and IL-23 inhibitory function that would reasonably convey possession of the full claimed genus. Because amino acid substitutions are not inherently predictable due to differences in physicochemical properties and their effects on peptide conformation and receptor binding, one of ordinary skill in the art would not reasonably conclude that the inventors possessed all peptides encompassed by the claimed genus based solely upon the limited disclosed species.
Claim Rejections - 35 USC § 112
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.
Claims 56 and 67, 69 are 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 56 recites “The peptide inhibitor or pharmaceutically acceptable salt or solvate thereof of claim 1, wherein: X11 is 3Quin, 2-Nal, Phe(2-Me), Phe(3-Me), Phe(4-Me), Phe(3,4-dimethoxy), or 1-Nal; X11is 3Quin, 2-Nal or 1-Nal; X11 is 2-Nal; and/or X7 is unsubstituted Trp”.
The claims does not indicate whether the latter limitation is intended to further narrow the former limitation, define an alternative embodiment, or replace the preceding limitation. Because the claim separately assigns multiple definitions to the same variable without clearly expressing their relationship, the metes and bounds of the claimed subject matter cannot be determined with reasonable certainty. The X11 variable cannot be all of these amino acids at the same time (i.e. the “and” in the and/or).
Claim 67 recites that the substituents include “Pegylated versions alone or as spacers of any of the foregoing”. The scope of this limitation is not reasonably certain. Specifically, it is unclear whether the phrase “including PEGylated versions..” is intended to recite additional claim limitations or merely exemplary embodiments. It is further unclear what constitutes a “PEGylated version” of the previously recited substituents, what is meant by “alone”, what structures qualify as PEG “spacers”, and how such PEGylated versions or spacers relate to “any of the foregoing”. The claim does not identify the point of PEG attachment, the scope of permissible PEG modifications, or whether the phrase encompasses all previously recited substituents or only a subset thereof. Accordingly, one of ordinary skill in the art would not be able to determine the metes and bounds of the claimed invention with reasonable certainty. Therefore, claim 67 fails to comply with the requirements of 35 U.S.C. 112(b). Claim 69 is also rejected due to its dependence on claim 67 and not further clarifying this point of confusion.
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 2, 61, 67, 69 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 2 depends from Claim 1 and recites “….the c terminal amino acid is Asn, DLeu, Dlys or Aib”. However, claim 1 limits Formula (I’) by requiring that the C-terminal amino satisfy the negative limitation of not being Aib (amongst other amino acids). Thus, the limitation added by claim 2 encompasses embodiments excluded by claim 1 and therefore broadens, rather than further limits, the scope of claim 1.
Claim 61 is dependent on claim 1 and recites “X7 is unsubstituted Trp, or Trp substituted with substituted or unsubstituted aryl, or substituted or unsubstituted heteroaryl”. Thus, X7 encompasses unsubstituted Trp, Trp substituted with substituted or unsubstituted aryl or heteroaryl. However, claim 61 claims “wherein: a) X7 is aryl…” Thus, the limitation of X7 being an aryl and not Trp substituted or unsubstituted broadens, rather than further limits, the scope of claim 1.
Claim 67 depends from claim 1 and recites that the peptide inhibitor is selected from Formula Ia’, Ib’, Ic’, Id’, Ie’, II, II’, II’’, IIa through formula XIf, or an amino acid sequence set forth in Table E1. Among the recited alternatives is Formula Ia’, which encompasses embodiments having a C-terminal amino acid outside the scope permitted by Formula I’ of claim 1. Because claim 67 expressly recites an alternative that is broader than claim 1, claim 67 encompasses subject matter excluded by claim 1 and therefore fails to further limit the parent claim. Since claim 67 is of improper dependent form because it encompasses embodiments outside the scope of claim 1 by reciting Formula Ia’, claim 69 necessarily incorporate the same improper scope. The additional limitation recited in claim 69 does not remove Formula Ia’ from the scope of the claim or otherwise restrict the claim to embodiments entirely within the scope of claim 1. Accordingly, claim 69 likewise fails to further limit.
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 § 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 (i.e., changing from AIA to pre-AIA ) 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.
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.
Claim(s) 1-2, 7, 9, 25, 32, 36, 40, 45, 50, 53, 56, 61, 67, 69, 79, 86 are rejected under 35 U.S.C. 103 as being unpatentable over Patel (WO2016011208, cited in Applicant’s IDS) in view of in view Frese (Cited in Applicant’s IDS).
Regarding claim 1, Patel teaches a monocyclic peptide inhibitor of an interleukin-23 receptor (claim 1; "wherein the peptide inhibitor is cyclized via a bond between X4 and X9, and wherein the peptide inhibitor inhibits the binding of an interleukin-23 (IL-23) to an IL-23 receptor"), wherein the peptide inhibitor comprises an amino acid sequence of Formula (I'): X3-X4-X5-X6-X7-X8-X9-X10-X11-X12-X13-X14-X15-X (I') wherein: X3 is absent or any amino acid (claim 1; "A peptide inhibitor of an interleukin-23 receptor, or a pharmaceutically acceptable salt or solvate thereof, wherein the peptide inhibitor comprises an amino acid sequence of Formula (Xa): XI-X2-X3-X4-X5-X6-X7-X8-X9-X10-XI I-X12- X13-X14-X15-X16-X17-X18-X19-X20 (Xa)": claim 2; "The peptide inhibitor of claim 1, wherein: XI is absent; X2 is absent; X3 is absent"); X4 is Abu, Cys, Pen (Claim 2; X4 is Cys, Abu or Pen); X5 and X6 is any amino acid (claim 2; "X5 is Ala, Gly, Lys, Asn, Orn, Gln, Arg, Ser or Thr; X6 is Asp or Thr"); X7 is unsubstituted Trp (claim 2; "X7 is Trp"); X8 is any amino acid (claim 2; "X8 is Glu, Gin or Val"); X9 is Abu, Cys, Pen, or Pen (claim 2; X9 is Cys, Abu or Pen); X10 is Phe substituted with halo (claim 3; X10 is Phe(3,4-CI2) and X11 is Trp substituted with hydroxy (claim 2; "X11 is 5-HydroxyTrp"); each of X12, X13, and X14 is independently any amino acid (claim 2: "X12 is Glu, His, Lys, Leu, Orn, Arg, Ser, Thr"; claim 2; X13 is "Asn, Orn, Gin, Arg, Thr or Val"; claim 2; "X14 is Asp, Phe, His, Met, Gin, Arg, Tyr"); X15 is any amino acid (claim 1; X15 is any amino acid) X16 is absent or any amino acid (claim 1;" X16 is any amino acid or absent; X17 is any amino acid or absent; X18 is any amino acid or absent; X19 is any amino acid or absent; and X20 is any amino acid or absent") And provided that ii) the C- terminal amino acid is other than Aib, 2Pal, 3Pal, 4Pal, 5Pyal, THP, His, (D)His, substituted His, substituted (D)His, Phe, substituted Phe, substituted (D)Phe, a-MePhe, substituted a-MePhe, Trp, substituted Trp, substituted or unsubstituted Tyr, substituted or unsubstituted (D)Tyr, substituted or unsubstituted aMeTyr, substituted or unsubstituted (D)aMeTyr, b-hPhe, Sarc, bAla, 1-Nal, aMe(1-Nal), substituted 1-Nal, 2-Nal, aMe(2-Na1), substituted 2-Nal, or N-substituted Asn (claim 1; X16-X20 is absent; claim 2; X15 is Ala, pAla, Glu, Gly, Asn, Gln Arg, Ser); and wherein the peptide inhibitor is cyclized via a bond between X4 and X9 (claim 1; "wherein the peptide inhibitor is cyclized via a bond between X4 and X9, and wherein the peptide inhibitor inhibits the binding of an interleukin-23 (IL-23) to an IL-23 receptor"); and the peptide inhibitor inhibits the binding of an interleukin-23 (IL-23) to an IL-23 receptor (claim 1). Although Patel discloses the Trp of X7 or X11 may be derivatized (Claim 2;" X7 is Trp or 6-Chloro-Trp"; Claim 2; X11 is 5- HydroxyTrp "), Patel does not disclose i) at least one of X7 and X11 is Trp substituted with substituted or unsubstituted aryl, or substituted or unsubstituted heteroaryl (see also paragraph 0021).
However, Frese discloses Boc-protected aryl tryptophan derivatives readily available for peptide synthesis including 7-phenyl- tryptophan(abstract; "different Boc-protected aryl tryptophan derivatives are obtained that can, for example, be used for peptide or peptidomimetic synthesis"; pg 1801 table 2; Boc-7-Ph-W [Box-7-phenyl-Trp]). An artisan of ordinary skill in the art would have followed the disclosure of Frese, because it would have enabled more substitutions at the Trp of X7, making the molecule somewhat more nucleophilic, comparative to the 6-Chloro-Trp already disclosed by Protagonist. Consequently, it would have been obvious for an artisan of ordinary skill to combine all claim limitations, with the exception that X7 is Trp substituted by an unsubstituted aryl, as disclosed by Patel, with X7 is Trp substituted by an unsubstituted aryl, as disclosed by Frese, because it would have enabled a monocyclic peptide inhibitor of IL-23R. It would have been obvious to a person of ordinary skill in the art to select 7-Ph-Trp from the finite number of known amino acid alternatives disclosed in the prior art because such amino acids are recognized as suitable residues for peptide analogs. Selecting these known alternatives would have amounted to no more than the routine optimization of a finite number of predictable options with a reasonable expectations of success (see KSR Int’l Co. v. Teleflex Inc, 550 U.S. 398, 421 (2007), see MPEP 2143).
Regarding claims 2 and 7(a), Patel in view of Frese teaches wherein X3 is absent (see claim 1), X4 is Abu, Cys or Pen (see claim 2, X4); X5 and X6 is any amino acid (claim 2, X5 is Ala, Gly, Lys, Asn, Orn, Gln, Arg, Ser or Thr; X6 is Asp or Thr); X7 is Trp substituted with unsubstituted aryl (Friese, Abstract); X8 is any amino acid including Gln (claim 2, “X8 is Glu, Gln or Val”, also paragraph 0021); X9 is Abu, Cys, Pen (claim 2, X9 is Cys, Abu or Pen); X10 is unsubstituted Phe or Phe substituted with halo (claim 3, X10 is Phe(3,4-C12); and X11 is Trp substituted with hydroxy or 2-Nal (claim 2; X11 is 5-hydroxyTrp, paragraph 0021, 2-Nal); each of X12, X13 or X14 is any amino acid (see claim 12, X12 is Glu, His, Lys, Orn, Arg, Ser, Thr”; claim 2; X13 is Asn, Orn, Gln, Arg, Thr or Val”; claim 2; “X14 is Asp, phe, His, Met, Gln, Arg, Tyr”); X15 is any amino acid (claim 1); X16 is absent or any amino acid (claim 1; X16 is any amino acid or absent, X17 is any amino acid or absent; X18 is any amino acid or absent; X19 is any amino acid or absent; and X20 is any amino acid or absent); and provided that at least one of X7 is Trp substituted with unsubstituted aryl (Frese, abstract); and ii) the C-terminal amino is Asn, Dleu, Dlys or Aib (claim 1; X16-X20 is absent; claim 2; X15 is ala, pAla, Glu, Gly, Asn, Gln, Arg, Ser, paragraph 0021); and wherein the peptide inhibitor is cyclized via a bond between X4 and X9 (claim 1) and wherein the peptide inhibits the binding of an IL-23 to an IL-23 receptor (claim 1).
Regarding claims 9 and 25, Patel in view of Frese teach wherein X4 and X9 are Pen (see paragraph 0021) meeting the limitations of claims 9 and 25 ((a) Formula IIa).
Regarding claim 32, Patel in view of Frese teach wherein X8 is Gln (see claim 1, paragraph 0021, claim 16).
Regarding claim 36, Patel in view of Frese teach wherein X10 is Phe (4-(2-aminoethoxy) (see claims 10 and 16).
Regarding claim 40, Patel in view of Frese teaches wherein X3 is absent (see claim 1), X4 is Abu, Cys or Pen (see claim 2, X4); X5 and X6 is any amino acid (claim 2, X5 is Ala, Gly, Lys, Asn, Orn, Gln, Arg, Ser or Thr; X6 is Asp or Thr); X7 is Trp substituted with unsubstituted aryl (Friese, Abstract); X8 is any amino acid including Gln (claim 2, “X8 is Glu, Gln or Val”, also paragraph 0021); X9 is Abu, Cys, Pen (claim 2, X9 is Cys, Abu or Pen); X10 is unsubstituted Phe or Phe substituted with halo (claim 3, X10 is Phe(3,4-C12); and X11 is Trp substituted with hydroxy or 2-Nal (claim 2; X11 is 5-hydroxyTrp, paragraph 0021, 2-Nal); each of X12, X13 or X14 is any amino acid (see claim 12, X12 is alpha-MeLys; claims 2 and 11; X13 is LysAc”; claims 2 and 11; X14 is Asn; X15 is any amino acid and in particular, Asn (claims 1 and 11); X16 is absent or any amino acid (claim 1; X16 is any amino acid or absent, X17 is any amino acid or absent; X18 is any amino acid or absent; X19 is any amino acid or absent; and X20 is any amino acid or absent); and provided that at least one of X7 is Trp substituted with unsubstituted aryl (Frese, abstract); and ii) the C-terminal amino is Asn, Dleu, Dlys or Aib (claim 1; X16-X20 is absent; claim 2; X15 is ala, pAla, Glu, Gly, Asn, Gln, Arg, Ser, paragraph 0021); and wherein the peptide inhibitor is cyclized via a bond between X4 and X9 (claim 1) and wherein the peptide inhibits the binding of an IL-23 to an IL-23 receptor (claim 1).
Regarding claims 45 and 50, Patel in view of Frese teaches wherein X13 is Lys(Ac) (see claim 11) and X14 is Asn (see claim 11).
Regarding claim 53, Patel in view of Frese teaches wherein X7 is Trp substituted with unsubstituted aryl (Frese, abstract).
Regarding claim 56, Patel in view of Frese teaches wherein X11 is Trp substituted with hydroxy or 2-Nal (claim 2; X11 is 5-hydroxyTrp, paragraph 0021, 2-Nal, claim 11).
Regarding claim 61, Patel in view of Frese teaches wherein X7 is Trp substituted with unsubstituted aryl (Frese, abstract, 7-Ph).
Regarding claim 67, Patel in view of Frese teaches wherein R1 is Ac, X as Formula I’ (see above), R2 is NH2 (see claims 1, 8-11).
Regarding claim 69, Patel in view of Frese teaches wherein R1 is Ac, X as Formula I’ (see above), R2 is NH2 (see claims 1, 8-11).
Regarding claim 79, Patel in view of Frese teaches Ac-Pen-N-T-[W(7-Ph)-Lys(Ac)-Pen-[Phe 4-(2-aminoethoxyl)]-2-Nal-apha MeLys-Lys(Ac)-N-DLeu-NH2 (see above teachings). Furthermore, regarding X8 being acetylated Lys (claim 2; X8=any amino acid; para [0058]; "The term "amino acid" or "any amino acid" as used here refers to any and all amino acids, including naturally occurring amino acids (e.g., alpha-amino acids), unnatural amino acids, modified amino acids, and non- natural amino acids. It includes both D- and L-amino acids"; para [0060] Table 1A pg 22: Abbreviations of Non-Natural Amino Acids and Chemical Moieties (for amino acid derivatives); Lys(Ac)=N-epsilon-Acetyl-lysine"). Regarding X14=(D)Leu, see claim 1; X14 is any amino acid; para [0058]; "The term "amino acid" or "any amino acid" as used here refers to any and all amino acids, including naturally occurring amino acids (e.g., a-amino acids), unnatural amino acids, modified amino acids, and non-natural amino acids. It includes both D- and L-amino acids"). Thus, it would have been obvious to a person of ordinary skill in the art to select Lys(Ac) for X8 and/or DLeu for X14 from the finite number of known amino acid alternatives disclosed in the prior art because such amino acids are recognized as suitable residues for peptide analogs. Selecting these known alternatives would have amounted to no more than the routine optimization of a finite number of predictable options with a reasonable expectations of success (see KSR Int’l Co. v. Teleflex Inc, 550 U.S. 398, 421 (2007), see MPEP 2143).
Regarding claim 86, Patel in view of Frese teaches pharmaceutical composition comprising the peptide inhibitor (see claims 44-46) and a carrier.
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.
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Claim(s) 1-2, 7, 9, 25, 32, 36, 40, 45, 50, 53, 56, 61, 67, 69, 79, 86 are rejected on the ground of nonstatutory double patenting as being unpatentable over claims 1-21 of U.S. Patent No.12552836 in view of Frese (see above citation). Although the claims at issue are not identical, they are not patentably distinct from each other because:
The instant application claims “A monocyclic peptide inhibitor of an interleukin-23 receptor, or a pharmaceutically acceptable salt or solvate thereof, wherein the peptide inhibitor comprises an amino acid sequence of Formula (I′): X3-X4-X5-X6-X7-X8-X9-X10-X11-X12-X13-X14-X15-X16 (I′) wherein X3 is absent or any amino acid, A4 is Abu, Cys or Pen, X5 or X6 is any amino acid, X7 is Trp or substituted or unsubstituted aryl, X8 is any amino acid, X9 is Abu, Cys or Pen…; X10 is unsubstituted Phe, or Phe substituted with halo, alkyl, haloalkyl, hydroxy, alkoxy, carboxy, carboxamido, 2-aminoethoxy, or 2-acetylaminoethoxy; and X11 is 2 Quin, 3 Quin, 2-Nal, Phe(2-Me), Phe(3-Me), Phe(4-Me), Phe(3,4-dimethoxy), 1-Nal, unsubstituted Trp, or Trp substituted with aryl, unsubstituted or substituted with halo, alkyl, cyano, haloalkyl, hydroxy, alkoxy, haloalkyloxy, phenyl, or substituted phenyl; each of X12, X13, and X14 is independently any amino acid; X15 is absent or any amino acid;
X16 is absent or any amino acid; at least one of X7 and X11 is Trp substituted with substituted or unsubstituted aryl, or substituted or unsubstituted heteroaryl; the C-terminal amino acid is other than Aib, 2 Pal, 3 Pal, 4 Pal, 5 Pyal, THP, His, (D)His, substituted His, substituted (D)His, Phe, substituted Phe, substituted (D)Phe, a-MePhe, substituted a-MePhe, Trp, substituted Trp, substituted or unsubstituted Tyr, substituted or unsubstituted (D)Tyr, substituted or unsubstituted aMeTyr, substituted or unsubstituted (D)aMeTyr, b-hPhe, Sarc, bAla, 1-Nal, aMe(1-Nal), substituted 1-Nal, 2-Nal, aMe(2-Nal), substituted 2-Nal, or N-substituted Asn; wherein the peptide inhibitor is cyclized via a bond between X4 and X9 (see claim 1). The dependent claims further define the variable amion acids with specific residues and SEQ ID Nos:1-19 (claim 79); pharmaceutical formulations thereof (claim 86).
US Patent No. ‘836 claims A peptide inhibitor or pharmaceutically acceptable salt or solvate thereof, wherein the peptide inhibitor comprises the amino acid sequence of Formula (II) (see claim 1). In particular, US Patent No. ‘836 claims many sequences that fall within the scope of instant Formula I’ In particular, US Patent. No. ‘836 claims Ac-[Pen]-NT-[W(7-Me)]-[Lys(Ac)]-[Pen]-Phe[4-(2- aminoethoxy)]-[2-Nal]-[α-MeLys]-[Lys(Ac)]-N- [(D)Leu]-NH2; (SEQ ID NO: 245) which fall within the scope of formula I. US Patent No. ‘836 claims pharmaceutical formulations thereof. The inhibitors of US Patent No. ‘836 fall within Formula I except that X7 is not Trp substituted with an aryl.
However, Frese discloses Boc-protected aryl tryptophan derivatives readily available for peptide synthesis including 7-phenyl- tryptophan(abstract; "different Boc-protected aryl tryptophan derivatives are obtained that can, for example, be used for peptide or peptidomimetic synthesis"; pg 1801 table 2; Boc-7-Ph-W [Box-7-phenyl-Trp]). An artisan of ordinary skill in the art would have followed the disclosure of Frese, because it would have enabled more substitutions at the Trp of X7, making the molecule somewhat more nucleophilic, comparative to the 6-Chloro-Trp already disclosed by Protagonist. Consequently, it would have been obvious for an artisan of ordinary skill to combine all claim limitations, with the exception that X7 is Trp substituted by an unsubstituted aryl, as disclosed by US Patent No. ‘836, with X7 is Trp substituted by an unsubstituted aryl, as disclosed by Frese, because it would have enabled a monocyclic peptide inhibitor of IL-23R. It would have been obvious to a person of ordinary skill in the art to select 7-Ph-Trp from the finite number of known amino acid alternatives disclosed in the prior art because such amino acids are recognized as suitable residues for peptide analogs. Selecting these known alternatives would have amounted to no more than the routine optimization of a finite number of predictable options with a reasonable expectations of success (see KSR Int’l Co. v. Teleflex Inc, 550 U.S. 398, 421 (2007), see MPEP 2143). The combination of US Patent No. ‘836 and Frese render obvious instant SEQ ID NO:1.
Claim(s) 1-2, 7, 9, 25, 32, 36, 40, 45, 50, 53, 56, 61, 67, 69, 79, 86 are rejected on the ground of nonstatutory double patenting as being unpatentable over claims 1-26 of U.S. Patent No.11041000 in view of Frese (see above citation). Although the claims at issue are not identical, they are not patentably distinct from each other because:
The instant application claims “A monocyclic peptide inhibitor of an interleukin-23 receptor, or a pharmaceutically acceptable salt or solvate thereof, wherein the peptide inhibitor comprises an amino acid sequence of Formula (I′): X3-X4-X5-X6-X7-X8-X9-X10-X11-X12-X13-X14-X15-X16 (I′) wherein X3 is absent or any amino acid, A4 is Abu, Cys or Pen, X5 or X6 is any amino acid, X7 is Trp or substituted or unsubstituted aryl, X8 is any amino acid, X9 is Abu, Cys or Pen…; X10 is unsubstituted Phe, or Phe substituted with halo, alkyl, haloalkyl, hydroxy, alkoxy, carboxy, carboxamido, 2-aminoethoxy, or 2-acetylaminoethoxy; and X11 is 2 Quin, 3 Quin, 2-Nal, Phe(2-Me), Phe(3-Me), Phe(4-Me), Phe(3,4-dimethoxy), 1-Nal, unsubstituted Trp, or Trp substituted with aryl, unsubstituted or substituted with halo, alkyl, cyano, haloalkyl, hydroxy, alkoxy, haloalkyloxy, phenyl, or substituted phenyl; each of X12, X13, and X14 is independently any amino acid; X15 is absent or any amino acid;
X16 is absent or any amino acid; at least one of X7 and X11 is Trp substituted with substituted or unsubstituted aryl, or substituted or unsubstituted heteroaryl; the C-terminal amino acid is other than Aib, 2 Pal, 3 Pal, 4 Pal, 5 Pyal, THP, His, (D)His, substituted His, substituted (D)His, Phe, substituted Phe, substituted (D)Phe, a-MePhe, substituted a-MePhe, Trp, substituted Trp, substituted or unsubstituted Tyr, substituted or unsubstituted (D)Tyr, substituted or unsubstituted aMeTyr, substituted or unsubstituted (D)aMeTyr, b-hPhe, Sarc, bAla, 1-Nal, aMe(1-Nal), substituted 1-Nal, 2-Nal, aMe(2-Nal), substituted 2-Nal, or N-substituted Asn; wherein the peptide inhibitor is cyclized via a bond between X4 and X9 (see claim 1). The dependent claims further define the variable amion acids with specific residues and SEQ ID Nos:1-19 (claim 79); pharmaceutical formulations thereof (claim 86).
US Patent No. ‘000 claims A peptide inhibitor or pharmaceutically acceptable salt or solvate thereof, wherein the peptide inhibitor comprises the amino acid sequence of Formula Z) (see claim 1). In particular, US Patent No. ‘000 claims many sequences that fall within the scope of instant Formula I’ In particular, US Patent. No. ‘000 claims Ac-[Pen]-NT-[W(7-Me)]-[Lys(Ac)]-[Pen]-Phe[4-(2- aminoethoxy)]-[2-Nal]-[α-MeLys]-[Lys(Ac)]-N- [(D)Leu]-NH2; (SEQ ID NO: 245) which fall within the scope of formula I. US Patent No. ‘000 claims pharmaceutical formulations thereof (claim 1, main utility). The inhibitors of US Patent No. ‘000 fall within Formula I except that X7 is not Trp substituted with an aryl.
However, Frese discloses Boc-protected aryl tryptophan derivatives readily available for peptide synthesis including 7-phenyl- tryptophan(abstract; "different Boc-protected aryl tryptophan derivatives are obtained that can, for example, be used for peptide or peptidomimetic synthesis"; pg 1801 table 2; Boc-7-Ph-W [Box-7-phenyl-Trp]). An artisan of ordinary skill in the art would have followed the disclosure of Frese, because it would have enabled more substitutions at the Trp of X7, making the molecule somewhat more nucleophilic, comparative to the 6-Chloro-Trp already disclosed by Protagonist. Consequently, it would have been obvious for an artisan of ordinary skill to combine all claim limitations, with the exception that X7 is Trp substituted by an unsubstituted aryl, as disclosed by US Patent No. ‘000, with X7 is Trp substituted by an unsubstituted aryl, as disclosed by Frese, because it would have enabled a monocyclic peptide inhibitor of IL-23R. It would have been obvious to a person of ordinary skill in the art to select 7-Ph-Trp from the finite number of known amino acid alternatives disclosed in the prior art because such amino acids are recognized as suitable residues for peptide analogs. Selecting these known alternatives would have amounted to no more than the routine optimization of a finite number of predictable options with a reasonable expectations of success (see KSR Int’l Co. v. Teleflex Inc, 550 U.S. 398, 421 (2007), see MPEP 2143). The combination of US Patent No. ‘000 and Frese render obvious instant SEQ ID NO:1.
Claim(s) 1-2, 7, 9, 25, 32, 36, 40, 45, 50, 53, 56, 61, 67, 69, 79, 86 are rejected on the ground of nonstatutory double patenting as being unpatentable over claims 1-20 of U.S. Patent No.10941183 in view of Frese (see above citation). Although the claims at issue are not identical, they are not patentably distinct from each other because:
The instant application claims “A monocyclic peptide inhibitor of an interleukin-23 receptor, or a pharmaceutically acceptable salt or solvate thereof, wherein the peptide inhibitor comprises an amino acid sequence of Formula (I′): X3-X4-X5-X6-X7-X8-X9-X10-X11-X12-X13-X14-X15-X16 (I′) wherein X3 is absent or any amino acid, A4 is Abu, Cys or Pen, X5 or X6 is any amino acid, X7 is Trp or substituted or unsubstituted aryl, X8 is any amino acid, X9 is Abu, Cys or Pen…; X10 is unsubstituted Phe, or Phe substituted with halo, alkyl, haloalkyl, hydroxy, alkoxy, carboxy, carboxamido, 2-aminoethoxy, or 2-acetylaminoethoxy; and X11 is 2 Quin, 3 Quin, 2-Nal, Phe(2-Me), Phe(3-Me), Phe(4-Me), Phe(3,4-dimethoxy), 1-Nal, unsubstituted Trp, or Trp substituted with aryl, unsubstituted or substituted with halo, alkyl, cyano, haloalkyl, hydroxy, alkoxy, haloalkyloxy, phenyl, or substituted phenyl; each of X12, X13, and X14 is independently any amino acid; X15 is absent or any amino acid;
X16 is absent or any amino acid; at least one of X7 and X11 is Trp substituted with substituted or unsubstituted aryl, or substituted or unsubstituted heteroaryl; the C-terminal amino acid is other than Aib, 2 Pal, 3 Pal, 4 Pal, 5 Pyal, THP, His, (D)His, substituted His, substituted (D)His, Phe, substituted Phe, substituted (D)Phe, a-MePhe, substituted a-MePhe, Trp, substituted Trp, substituted or unsubstituted Tyr, substituted or unsubstituted (D)Tyr, substituted or unsubstituted aMeTyr, substituted or unsubstituted (D)aMeTyr, b-hPhe, Sarc, bAla, 1-Nal, aMe(1-Nal), substituted 1-Nal, 2-Nal, aMe(2-Nal), substituted 2-Nal, or N-substituted Asn; wherein the peptide inhibitor is cyclized via a bond between X4 and X9 (see claim 1). The dependent claims further define the variable amino acids with specific residues and SEQ ID Nos:1-19 (claim 79); pharmaceutical formulations thereof (claim 86).
US Patent No. ‘183 claims A peptide inhibitor or pharmaceutically acceptable salt or solvate thereof, wherein the peptide inhibitor comprises the amino acid sequence of Formula Xa) (see claim 1). In particular, US Patent No. ‘183 claims many sequences that fall within the scope of instant Formula I’ For example, Ac-[Abu]-QTWQC-[Phe[4-(2-aminoethoxy)]]-[2-Nal]-[Aib]-QNG-NH2 (SEQ ID NO:877) which falls with the instant claims and formula Z with N terminal Ac and C-terminal NH2. US Patent. No. ‘183 claims pharmaceutical formulations thereof (claim 1, main utility).
The inhibitors of US Patent No. ‘183 fall within Formula I except that X7 is not Trp substituted with an aryl.
However, Frese discloses Boc-protected aryl tryptophan derivatives readily available for peptide synthesis including 7-phenyl- tryptophan(abstract; "different Boc-protected aryl tryptophan derivatives are obtained that can, for example, be used for peptide or peptidomimetic synthesis"; pg 1801 table 2; Boc-7-Ph-W [Box-7-phenyl-Trp]). An artisan of ordinary skill in the art would have followed the disclosure of Frese, because it would have enabled more substitutions at the Trp of X7, making the molecule somewhat more nucleophilic, comparative to the 6-Chloro-Trp already disclosed by Protagonist. Consequently, it would have been obvious for an artisan of ordinary skill to combine all claim limitations, with the exception that X7 is Trp substituted by an unsubstituted aryl, as disclosed by US Patent No. ‘183, with X7 is Trp substituted by an unsubstituted aryl, as disclosed by Frese, because it would have enabled a monocyclic peptide inhibitor of IL-23R. It would have been obvious to a person of ordinary skill in the art to select 7-Ph-Trp from the finite number of known amino acid alternatives disclosed in the prior art because such amino acids are recognized as suitable residues for peptide analogs. Selecting these known alternatives would have amounted to no more than the routine optimization of a finite number of predictable options with a reasonable expectations of success (see KSR Int’l Co. v. Teleflex Inc, 550 U.S. 398, 421 (2007), see MPEP 2143). The combination of US Patent No. ‘183 and Frese render obvious instant SEQ ID NOs:1-19.
Claim(s) 1-2, 7, 9, 25, 32, 36, 40, 45, 50, 53, 56, 61, 67, 69, 79, 86 are rejected on the ground of nonstatutory double patenting as being unpatentable over claims 1-21 of U.S. Patent No.10023614 in view of Frese (see above citation). Although the claims at issue are not identical, they are not patentably distinct from each other because:
The instant application claims “A monocyclic peptide inhibitor of an interleukin-23 receptor, or a pharmaceutically acceptable salt or solvate thereof, wherein the peptide inhibitor comprises an amino acid sequence of Formula (I′): X3-X4-X5-X6-X7-X8-X9-X10-X11-X12-X13-X14-X15-X16 (I′) wherein X3 is absent or any amino acid, A4 is Abu, Cys or Pen, X5 or X6 is any amino acid, X7 is Trp or substituted or unsubstituted aryl, X8 is any amino acid, X9 is Abu, Cys or Pen…; X10 is unsubstituted Phe, or Phe substituted with halo, alkyl, haloalkyl, hydroxy, alkoxy, carboxy, carboxamido, 2-aminoethoxy, or 2-acetylaminoethoxy; and X11 is 2 Quin, 3 Quin, 2-Nal, Phe(2-Me), Phe(3-Me), Phe(4-Me), Phe(3,4-dimethoxy), 1-Nal, unsubstituted Trp, or Trp substituted with aryl, unsubstituted or substituted with halo, alkyl, cyano, haloalkyl, hydroxy, alkoxy, haloalkyloxy, phenyl, or substituted phenyl; each of X12, X13, and X14 is independently any amino acid; X15 is absent or any amino acid;
X16 is absent or any amino acid; at least one of X7 and X11 is Trp substituted with substituted or unsubstituted aryl, or substituted or unsubstituted heteroaryl; the C-terminal amino acid is other than Aib, 2 Pal, 3 Pal, 4 Pal, 5 Pyal, THP, His, (D)His, substituted His, substituted (D)His, Phe, substituted Phe, substituted (D)Phe, a-MePhe, substituted a-MePhe, Trp, substituted Trp, substituted or unsubstituted Tyr, substituted or unsubstituted (D)Tyr, substituted or unsubstituted aMeTyr, substituted or unsubstituted (D)aMeTyr, b-hPhe, Sarc, bAla, 1-Nal, aMe(1-Nal), substituted 1-Nal, 2-Nal, aMe(2-Nal), substituted 2-Nal, or N-substituted Asn; wherein the peptide inhibitor is cyclized via a bond between X4 and X9 (see claim 1). The dependent claims further define the variable amion acids with specific residues and SEQ ID Nos:1-19 (claim 79); pharmaceutical formulations thereof (claim 86).
US Patent No. ‘614 claims A peptide inhibitor or pharmaceutically acceptable salt or solvate thereof, wherein the peptide inhibitor comprises the amino acid sequence of Formula Xa) (see claim 1). In particular, US Patent No. ‘614 claims many sequences that fall within the scope of instant Formula I’ In particular, US Patent. No. ‘000 claims Ac-[Pen]-NTWQ]-[Pen]-Phe[4-(2- aminoethoxy)]-[2-Nal]-[α-MeLys]-[Lys(Ac)]-N- N-NH2; (SEQ ID NO:639, 666) which fall within the scope of formula I. US Patent No. ‘614 claims pharmaceutical formulations thereof (claim 21, main utility). The inhibitors of US Patent No. ‘614 fall within Formula I except that X7 is not Trp substituted with an aryl.
However, Frese discloses Boc-protected aryl tryptophan derivatives readily available for peptide synthesis including 7-phenyl- tryptophan(abstract; "different Boc-protected aryl tryptophan derivatives are obtained that can, for example, be used for peptide or peptidomimetic synthesis"; pg 1801 table 2; Boc-7-Ph-W [Box-7-phenyl-Trp]). An artisan of ordinary skill in the art would have followed the disclosure of Frese, because it would have enabled more substitutions at the Trp of X7, making the molecule somewhat more nucleophilic, comparative to the 6-Chloro-Trp already disclosed by Protagonist. Consequently, it would have been obvious for an artisan of ordinary skill to combine all claim limitations, with the exception that X7 is Trp substituted by an unsubstituted aryl, as disclosed by US Patent No. ‘614, with X7 is Trp substituted by an unsubstituted aryl, as disclosed by Frese, because it would have enabled a monocyclic peptide inhibitor of IL-23R. It would have been obvious to a person of ordinary skill in the art to select 7-Ph-Trp from the finite number of known amino acid alternatives disclosed in the prior art because such amino acids are recognized as suitable residues for peptide analogs. Selecting these known alternatives would have amounted to no more than the routine optimization of a finite number of predictable options with a reasonable expectations of success (see KSR Int’l Co. v. Teleflex Inc, 550 U.S. 398, 421 (2007), see MPEP 2143). The combination of US Patent No. ‘614 and Frese render obvious instant SEQ ID NO:1-19.
Claim(s) 1-2, 7, 9, 25, 32, 36, 40, 45, 50, 53, 56, 61, 67, 69, 79, 86 are rejected on the ground of nonstatutory double patenting as being unpatentable over claims 1-26 of U.S. Patent No.10035824 in view of Frese (see above citation). Although the claims at issue are not identical, they are not patentably distinct from each other because:
The instant application claims “A monocyclic peptide inhibitor of an interleukin-23 receptor, or a pharmaceutically acceptable salt or solvate thereof, wherein the peptide inhibitor comprises an amino acid sequence of Formula (I′): X3-X4-X5-X6-X7-X8-X9-X10-X11-X12-X13-X14-X15-X16 (I′) wherein X3 is absent or any amino acid, A4 is Abu, Cys or Pen, X5 or X6 is any amino acid, X7 is Trp or substituted or unsubstituted aryl, X8 is any amino acid, X9 is Abu, Cys or Pen…; X10 is unsubstituted Phe, or Phe substituted with halo, alkyl, haloalkyl, hydroxy, alkoxy, carboxy, carboxamido, 2-aminoethoxy, or 2-acetylaminoethoxy; and X11 is 2 Quin, 3 Quin, 2-Nal, Phe(2-Me), Phe(3-Me), Phe(4-Me), Phe(3,4-dimethoxy), 1-Nal, unsubstituted Trp, or Trp substituted with aryl, unsubstituted or substituted with halo, alkyl, cyano, haloalkyl, hydroxy, alkoxy, haloalkyloxy, phenyl, or substituted phenyl; each of X12, X13, and X14 is independently any amino acid; X15 is absent or any amino acid;
X16 is absent or any amino acid; at least one of X7 and X11 is Trp substituted with substituted or unsubstituted aryl, or substituted or unsubstituted heteroaryl; the C-terminal amino acid is other than Aib, 2 Pal, 3 Pal, 4 Pal, 5 Pyal, THP, His, (D)His, substituted His, substituted (D)His, Phe, substituted Phe, substituted (D)Phe, a-MePhe, substituted a-MePhe, Trp, substituted Trp, substituted or unsubstituted Tyr, substituted or unsubstituted (D)Tyr, substituted or unsubstituted aMeTyr, substituted or unsubstituted (D)aMeTyr, b-hPhe, Sarc, bAla, 1-Nal, aMe(1-Nal), substituted 1-Nal, 2-Nal, aMe(2-Nal), substituted 2-Nal, or N-substituted Asn; wherein the peptide inhibitor is cyclized via a bond between X4 and X9 (see claim 1). The dependent claims further define the variable amino acids with specific residues and SEQ ID Nos:1-19 (claim 79); pharmaceutical formulations thereof (claim 86).
US Patent No. ‘824 claims A peptide inhibitor or pharmaceutically acceptable salt or solvate thereof, wherein the peptide inhibitor comprises the amino acid sequence of Formula Xa) (see claim 1). In particular, US Patent No. ‘183 claims many sequences that fall within the scope of instant Formula I’ For example, Ac-[Abu]-QTWQC-[Phe[4-(2-aminoethoxy)]]-[2-Nal]-[Aib]-QNG-NH2 (SEQ ID NO:877, claim 10) which falls with the instant claims and formula Z with N terminal Ac and C-terminal NH2. US Patent. No. ‘824 claims pharmaceutical formulations thereof (claim 26, main utility). The inhibitors of US Patent No. ‘824 fall within Formula I except that X7 is not Trp substituted with an aryl.
However, Frese discloses Boc-protected aryl tryptophan derivatives readily available for peptide synthesis including 7-phenyl- tryptophan(abstract; "different Boc-protected aryl tryptophan derivatives are obtained that can, for example, be used for peptide or peptidomimetic synthesis"; pg 1801 table 2; Boc-7-Ph-W [Box-7-phenyl-Trp]). An artisan of ordinary skill in the art would have followed the disclosure of Frese, because it would have enabled more substitutions at the Trp of X7, making the molecule somewhat more nucleophilic, comparative to the 6-Chloro-Trp already disclosed by Protagonist. Consequently, it would have been obvious for an artisan of ordinary skill to combine all claim limitations, with the exception that X7 is Trp substituted by an unsubstituted aryl, as disclosed by US Patent No. ‘824, with X7 is Trp substituted by an unsubstituted aryl, as disclosed by Frese, because it would have enabled a monocyclic peptide inhibitor of IL-23R. It would have been obvious to a person of ordinary skill in the art to select 7-Ph-Trp from the finite number of known amino acid alternatives disclosed in the prior art because such amino acids are recognized as suitable residues for peptide analogs. Selecting these known alternatives would have amounted to no more than the routine optimization of a finite number of predictable options with a reasonable expectations of success (see KSR Int’l Co. v. Teleflex Inc, 550 U.S. 398, 421 (2007), see MPEP 2143). The combination of US Patent No. ‘824 and Frese render obvious instant SEQ ID NOs:1-19.
Claim(s) 1-2, 7, 9, 25, 32, 36, 40, 45, 50, 53, 56, 61, 67, 69, 79, 86 are rejected on the ground of nonstatutory double patenting as being unpatentable over claims 1-22 of U.S. Patent No10196424 in view of Frese (see above citation). Although the claims at issue are not identical, they are not patentably distinct from each other because:
The instant application claims “A monocyclic peptide inhibitor of an interleukin-23 receptor, or a pharmaceutically acceptable salt or solvate thereof, wherein the peptide inhibitor comprises an amino acid sequence of Formula (I′): X3-X4-X5-X6-X7-X8-X9-X10-X11-X12-X13-X14-X15-X16 (I′) wherein X3 is absent or any amino acid, A4 is Abu, Cys or Pen, X5 or X6 is any amino acid, X7 is Trp or substituted or unsubstituted aryl, X8 is any amino acid, X9 is Abu, Cys or Pen…; X10 is unsubstituted Phe, or Phe substituted with halo, alkyl, haloalkyl, hydroxy, alkoxy, carboxy, carboxamido, 2-aminoethoxy, or 2-acetylaminoethoxy; and X11 is 2 Quin, 3 Quin, 2-Nal, Phe(2-Me), Phe(3-Me), Phe(4-Me), Phe(3,4-dimethoxy), 1-Nal, unsubstituted Trp, or Trp substituted with aryl, unsubstituted or substituted with halo, alkyl, cyano, haloalkyl, hydroxy, alkoxy, haloalkyloxy, phenyl, or substituted phenyl; each of X12, X13, and X14 is independently any amino acid; X15 is absent or any amino acid;
X16 is absent or any amino acid; at least one of X7 and X11 is Trp substituted with substituted or unsubstituted aryl, or substituted or unsubstituted heteroaryl; the C-terminal amino acid is other than Aib, 2 Pal, 3 Pal, 4 Pal, 5 Pyal, THP, His, (D)His, substituted His, substituted (D)His, Phe, substituted Phe, substituted (D)Phe, a-MePhe, substituted a-MePhe, Trp, substituted Trp, substituted or unsubstituted Tyr, substituted or unsubstituted (D)Tyr, substituted or unsubstituted aMeTyr, substituted or unsubstituted (D)aMeTyr, b-hPhe, Sarc, bAla, 1-Nal, aMe(1-Nal), substituted 1-Nal, 2-Nal, aMe(2-Nal), substituted 2-Nal, or N-substituted Asn; wherein the peptide inhibitor is cyclized via a bond between X4 and X9 (see claim 1). The dependent claims further define the variable amion acids with specific residues and SEQ ID Nos:1-19 (claim 79); pharmaceutical formulations thereof (claim 86).
US Patent No. ‘424 claims A peptide inhibitor or pharmaceutically acceptable salt or solvate thereof, wherein the peptide inhibitor comprises the amino acid sequence of Formula Ir) (see claim 1). In particular, US Patent No. ‘424 claims many sequences that fall within the scope of instant Formula I’ For example, Ac-[Pen]-NTWQ-[Pen]-[Phe[4-(2-aminoethoxy)]]-[2-Nal]-[Aib]-[Lys(Ac)]-NN-NH2 (SEQ ID NO:632, claim 15) which falls with the instant claims and formula Z with N terminal Ac and C-terminal NH2. US Patent. No. ‘424 claims pharmaceutical formulations thereof (claim 15, main utility). The inhibitors of US Patent No. ‘424 fall within Formula I except that X7 is not Trp substituted with an aryl.
However, Frese discloses Boc-protected aryl tryptophan derivatives readily available for peptide synthesis including 7-phenyl- tryptophan(abstract; "different Boc-protected aryl tryptophan derivatives are obtained that can, for example, be used for peptide or peptidomimetic synthesis"; pg 1801 table 2; Boc-7-Ph-W [Box-7-phenyl-Trp]). An artisan of ordinary skill in the art would have followed the disclosure of Frese, because it would have enabled more substitutions at the Trp of X7, making the molecule somewhat more nucleophilic, comparative to the 6-Chloro-Trp already disclosed by Protagonist. Consequently, it would have been obvious for an artisan of ordinary skill to combine all claim limitations, with the exception that X7 is Trp substituted by an unsubstituted aryl, as disclosed by US Patent No. ‘424 with X7 is Trp substituted by an unsubstituted aryl, as disclosed by Frese, because it would have enabled a monocyclic peptide inhibitor of IL-23R. It would have been obvious to a person of ordinary skill in the art to select 7-Ph-Trp from the finite number of known amino acid alternatives disclosed in the prior art because such amino acids are recognized as suitable residues for peptide analogs. Selecting these known alternatives would have amounted to no more than the routine optimization of a finite number of predictable options with a reasonable expectations of success (see KSR Int’l Co. v. Teleflex Inc, 550 U.S. 398, 421 (2007), see MPEP 2143). The combination of US Patent No. ‘424 and Frese render obvious instant SEQ ID NOs:1-19.
Claim(s) 1-2, 7, 9, 25, 32, 36, 40, 45, 50, 53, 56, 61, 67, 69, 79, 86 are rejected on the ground of nonstatutory double patenting as being unpatentable over claims 1-24 of U.S. Patent No 9624268 in view of Frese (see above citation). Although the claims at issue are not identical, they are not patentably distinct from each other because:
The instant application claims “A monocyclic peptide inhibitor of an interleukin-23 receptor, or a pharmaceutically acceptable salt or solvate thereof, wherein the peptide inhibitor comprises an amino acid sequence of Formula (I′): X3-X4-X5-X6-X7-X8-X9-X10-X11-X12-X13-X14-X15-X16 (I′) wherein X3 is absent or any amino acid, A4 is Abu, Cys or Pen, X5 or X6 is any amino acid, X7 is Trp or substituted or unsubstituted aryl, X8 is any amino acid, X9 is Abu, Cys or Pen…; X10 is unsubstituted Phe, or Phe substituted with halo, alkyl, haloalkyl, hydroxy, alkoxy, carboxy, carboxamido, 2-aminoethoxy, or 2-acetylaminoethoxy; and X11 is 2 Quin, 3 Quin, 2-Nal, Phe(2-Me), Phe(3-Me), Phe(4-Me), Phe(3,4-dimethoxy), 1-Nal, unsubstituted Trp, or Trp substituted with aryl, unsubstituted or substituted with halo, alkyl, cyano, haloalkyl, hydroxy, alkoxy, haloalkyloxy, phenyl, or substituted phenyl; each of X12, X13, and X14 is independently any amino acid; X15 is absent or any amino acid;
X16 is absent or any amino acid; at least one of X7 and X11 is Trp substituted with substituted or unsubstituted aryl, or substituted or unsubstituted heteroaryl; the C-terminal amino acid is other than Aib, 2 Pal, 3 Pal, 4 Pal, 5 Pyal, THP, His, (D)His, substituted His, substituted (D)His, Phe, substituted Phe, substituted (D)Phe, a-MePhe, substituted a-MePhe, Trp, substituted Trp, substituted or unsubstituted Tyr, substituted or unsubstituted (D)Tyr, substituted or unsubstituted aMeTyr, substituted or unsubstituted (D)aMeTyr, b-hPhe, Sarc, bAla, 1-Nal, aMe(1-Nal), substituted 1-Nal, 2-Nal, aMe(2-Nal), substituted 2-Nal, or N-substituted Asn; wherein the peptide inhibitor is cyclized via a bond between X4 and X9 (see claim 1). The dependent claims further define the variable amion acids with specific residues and SEQ ID Nos:1-19 (claim 79); pharmaceutical formulations thereof (claim 86).
US Patent No. ‘268 claims A peptide inhibitor or pharmaceutically acceptable salt or solvate thereof, wherein the peptide inhibitor comprises the amino acid sequence of FormulaIr) (see claim 1). In particular, US Patent No. ‘268 claims many sequences that fall within the scope of instant Formula I’ For example, Ac-[Pen]-NTWQ-[Pen]-[Phe[4-(2-aminoethoxy)]]-[2-Nal]-[Aib]-[Lys(Ac)]-NN-NH2 (SEQ ID NO:632, claim 5) which falls with the instant claims and formula Z with N terminal Ac and C-terminal NH2. US Patent. No. ‘268 claims pharmaceutical formulations thereof (claim 24, main utility). The inhibitors of US Patent No. ‘268 fall within Formula I except that X7 is not Trp substituted with an aryl.
However, Frese discloses Boc-protected aryl tryptophan derivatives readily available for peptide synthesis including 7-phenyl- tryptophan(abstract; "different Boc-protected aryl tryptophan derivatives are obtained that can, for example, be used for peptide or peptidomimetic synthesis"; pg 1801 table 2; Boc-7-Ph-W [Box-7-phenyl-Trp]). An artisan of ordinary skill in the art would have followed the disclosure of Frese, because it would have enabled more substitutions at the Trp of X7, making the molecule somewhat more nucleophilic, comparative to the 6-Chloro-Trp already disclosed by Protagonist. Consequently, it would have been obvious for an artisan of ordinary skill to combine all claim limitations, with the exception that X7 is Trp substituted by an unsubstituted aryl, as disclosed by US Patent No. ‘268 with X7 is Trp substituted by an unsubstituted aryl, as disclosed by Frese, because it would have enabled a monocyclic peptide inhibitor of IL-23R. It would have been obvious to a person of ordinary skill in the art to select 7-Ph-Trp from the finite number of known amino acid alternatives disclosed in the prior art because such amino acids are recognized as suitable residues for peptide analogs. Selecting these known alternatives would have amounted to no more than the routine optimization of a finite number of predictable options with a reasonable expectations of success (see KSR Int’l Co. v. Teleflex Inc, 550 U.S. 398, 421 (2007), see MPEP 2143). The combination of US Patent No. ‘268 and Frese render obvious instant SEQ ID NOs:1-19.
Claim(s) 1-2, 7, 9, 25, 32, 36, 40, 45, 50, 53, 56, 61, 67, 69, 79, 86 are rejected on the ground of nonstatutory double patenting as being unpatentable over claims 1-21 of U.S. Patent No 11884748 in view of Frese (see above citation). Although the claims at issue are not identical, they are not patentably distinct from each other because:
The instant application claims “A monocyclic peptide inhibitor of an interleukin-23 receptor, or a pharmaceutically acceptable salt or solvate thereof, wherein the peptide inhibitor comprises an amino acid sequence of Formula (I′): X3-X4-X5-X6-X7-X8-X9-X10-X11-X12-X13-X14-X15-X16 (I′) wherein X3 is absent or any amino acid, A4 is Abu, Cys or Pen, X5 or X6 is any amino acid, X7 is Trp or substituted or unsubstituted aryl, X8 is any amino acid, X9 is Abu, Cys or Pen…; X10 is unsubstituted Phe, or Phe substituted with halo, alkyl, haloalkyl, hydroxy, alkoxy, carboxy, carboxamido, 2-aminoethoxy, or 2-acetylaminoethoxy; and X11 is 2 Quin, 3 Quin, 2-Nal, Phe(2-Me), Phe(3-Me), Phe(4-Me), Phe(3,4-dimethoxy), 1-Nal, unsubstituted Trp, or Trp substituted with aryl, unsubstituted or substituted with halo, alkyl, cyano, haloalkyl, hydroxy, alkoxy, haloalkyloxy, phenyl, or substituted phenyl; each of X12, X13, and X14 is independently any amino acid; X15 is absent or any amino acid;
X16 is absent or any amino acid; at least one of X7 and X11 is Trp substituted with substituted or unsubstituted aryl, or substituted or unsubstituted heteroaryl; the C-terminal amino acid is other than Aib, 2 Pal, 3 Pal, 4 Pal, 5 Pyal, THP, His, (D)His, substituted His, substituted (D)His, Phe, substituted Phe, substituted (D)Phe, a-MePhe, substituted a-MePhe, Trp, substituted Trp, substituted or unsubstituted Tyr, substituted or unsubstituted (D)Tyr, substituted or unsubstituted aMeTyr, substituted or unsubstituted (D)aMeTyr, b-hPhe, Sarc, bAla, 1-Nal, aMe(1-Nal), substituted 1-Nal, 2-Nal, aMe(2-Nal), substituted 2-Nal, or N-substituted Asn; wherein the peptide inhibitor is cyclized via a bond between X4 and X9 (see claim 1). The dependent claims further define the variable amion acids with specific residues and SEQ ID Nos:1-19 (claim 79); pharmaceutical formulations thereof (claim 86).
US Patent No. ‘748 claims an IL-23 receptor inhibitor (see claim 1). In particular, US Patent No. ‘748 claims many sequences that fall within the scope of instant Formula I’ For example, Ac-[Abu]-QTWQC-[Phe[4-(2-aminoethoxy)]]-[2-Nal]-[Aib]-QNG-NH2 (SEQ ID NO:877, claim 6) which falls with the instant claims and formula Z with N terminal Ac and C-terminal NH2. US Patent. No. ‘748 claims pharmaceutical formulations thereof (claim 6, main utility). The inhibitors of US Patent No. ‘748 fall within Formula I except that X7 is not Trp substituted with an aryl.
However, Frese discloses Boc-protected aryl tryptophan derivatives readily available for peptide synthesis including 7-phenyl- tryptophan(abstract; "different Boc-protected aryl tryptophan derivatives are obtained that can, for example, be used for peptide or peptidomimetic synthesis"; pg 1801 table 2; Boc-7-Ph-W [Box-7-phenyl-Trp]). An artisan of ordinary skill in the art would have followed the disclosure of Frese, because it would have enabled more substitutions at the Trp of X7, making the molecule somewhat more nucleophilic, comparative to the 6-Chloro-Trp already disclosed by Protagonist. Consequently, it would have been obvious for an artisan of ordinary skill to combine all claim limitations, with the exception that X7 is Trp substituted by an unsubstituted aryl, as disclosed by US Patent No. ‘748 with X7 is Trp substituted by an unsubstituted aryl, as disclosed by Frese, because it would have enabled a monocyclic peptide inhibitor of IL-23R. It would have been obvious to a person of ordinary skill in the art to select 7-Ph-Trp from the finite number of known amino acid alternatives disclosed in the prior art because such amino acids are recognized as suitable residues for peptide analogs. Selecting these known alternatives would have amounted to no more than the routine optimization of a finite number of predictable options with a reasonable expectations of success (see KSR Int’l Co. v. Teleflex Inc, 550 U.S. 398, 421 (2007), see MPEP 2143). The combination of US Patent No. ‘748 and Frese render obvious instant SEQ ID NOs:1-19.
Claim(s) 1-2, 7, 9, 25, 32, 36, 40, 45, 50, 53, 56, 61, 67, 69, 79, 86 are rejected on the ground of nonstatutory double patenting as being unpatentable over claims 1-18 of U.S. Patent No 10787490 in view of Frese (see above citation). Although the claims at issue are not identical, they are not patentably distinct from each other because:
The instant application claims “A monocyclic peptide inhibitor of an interleukin-23 receptor, or a pharmaceutically acceptable salt or solvate thereof, wherein the peptide inhibitor comprises an amino acid sequence of Formula (I′): X3-X4-X5-X6-X7-X8-X9-X10-X11-X12-X13-X14-X15-X16 (I′) wherein X3 is absent or any amino acid, A4 is Abu, Cys or Pen, X5 or X6 is any amino acid, X7 is Trp or substituted or unsubstituted aryl, X8 is any amino acid, X9 is Abu, Cys or Pen…; X10 is unsubstituted Phe, or Phe substituted with halo, alkyl, haloalkyl, hydroxy, alkoxy, carboxy, carboxamido, 2-aminoethoxy, or 2-acetylaminoethoxy; and X11 is 2 Quin, 3 Quin, 2-Nal, Phe(2-Me), Phe(3-Me), Phe(4-Me), Phe(3,4-dimethoxy), 1-Nal, unsubstituted Trp, or Trp substituted with aryl, unsubstituted or substituted with halo, alkyl, cyano, haloalkyl, hydroxy, alkoxy, haloalkyloxy, phenyl, or substituted phenyl; each of X12, X13, and X14 is independently any amino acid; X15 is absent or any amino acid;
X16 is absent or any amino acid; at least one of X7 and X11 is Trp substituted with substituted or unsubstituted aryl, or substituted or unsubstituted heteroaryl; the C-terminal amino acid is other than Aib, 2 Pal, 3 Pal, 4 Pal, 5 Pyal, THP, His, (D)His, substituted His, substituted (D)His, Phe, substituted Phe, substituted (D)Phe, a-MePhe, substituted a-MePhe, Trp, substituted Trp, substituted or unsubstituted Tyr, substituted or unsubstituted (D)Tyr, substituted or unsubstituted aMeTyr, substituted or unsubstituted (D)aMeTyr, b-hPhe, Sarc, bAla, 1-Nal, aMe(1-Nal), substituted 1-Nal, 2-Nal, aMe(2-Nal), substituted 2-Nal, or N-substituted Asn; wherein the peptide inhibitor is cyclized via a bond between X4 and X9 (see claim 1). The dependent claims further define the variable amino acids with specific residues and SEQ ID Nos:1-19 (claim 79); pharmaceutical formulations thereof (claim 86).
US Patent No. ‘490 claims an IL-23 receptor inhibitor (see claim 1). In particular, US Patent No. ‘490 claims many sequences that fall within the scope of instant Formula I’ For example, [Pen]-NTWQ-[Pen]-[Phe[4-(2- aminoethoxy)]-[2-Nal]-[Aib]-[Lys(Ac)]-NN-NH2 (SEQ ID NO:1115 claim 1) which falls with the instant claims and formula Z with N terminal Ac and C-terminal NH2. US Patent. No. ‘490 claims pharmaceutical formulations thereof (claim 1, main utility). The inhibitors of US Patent No. ‘490 fall within Formula I except that X7 is not Trp substituted with an aryl.
However, Frese discloses Boc-protected aryl tryptophan derivatives readily available for peptide synthesis including 7-phenyl- tryptophan(abstract; "different Boc-protected aryl tryptophan derivatives are obtained that can, for example, be used for peptide or peptidomimetic synthesis"; pg 1801 table 2; Boc-7-Ph-W [Box-7-phenyl-Trp]). An artisan of ordinary skill in the art would have followed the disclosure of Frese, because it would have enabled more substitutions at the Trp of X7, making the molecule somewhat more nucleophilic, comparative to the 6-Chloro-Trp already disclosed by Protagonist. Consequently, it would have been obvious for an artisan of ordinary skill to combine all claim limitations, with the exception that X7 is Trp substituted by an unsubstituted aryl, as disclosed by US Patent No. ‘490 with X7 is Trp substituted by an unsubstituted aryl, as disclosed by Frese, because it would have enabled a monocyclic peptide inhibitor of IL-23R. It would have been obvious to a person of ordinary skill in the art to select 7-Ph-Trp from the finite number of known amino acid alternatives disclosed in the prior art because such amino acids are recognized as suitable residues for peptide analogs. Selecting these known alternatives would have amounted to no more than the routine optimization of a finite number of predictable options with a reasonable expectations of success (see KSR Int’l Co. v. Teleflex Inc, 550 U.S. 398, 421 (2007), see MPEP 2143). The combination of US Patent No. ‘490 and Frese render obvious instant SEQ ID NOs:1-19.
Claim(s) 1-2, 7, 9, 25, 32, 36, 40, 45, 50, 53, 56, 61, 67, 69, 79, 86 are provisionally rejected on the ground of nonstatutory double patenting as being unpatentable over claims 32-44, 50, 53-56, 75-81 of copending Application No. 19/421560 (reference application). Although the claims at issue are not identical, they are not patentably distinct from each other because:
The instant application claims “A monocyclic peptide inhibitor of an interleukin-23 receptor, or a pharmaceutically acceptable salt or solvate thereof, wherein the peptide inhibitor comprises an amino acid sequence of Formula (I′): X3-X4-X5-X6-X7-X8-X9-X10-X11-X12-X13-X14-X15-X16 (I′) wherein X3 is absent or any amino acid, A4 is Abu, Cys or Pen, X5 or X6 is any amino acid, X7 is Trp or substituted or unsubstituted aryl, X8 is any amino acid, X9 is Abu, Cys or Pen…; X10 is unsubstituted Phe, or Phe substituted with halo, alkyl, haloalkyl, hydroxy, alkoxy, carboxy, carboxamido, 2-aminoethoxy, or 2-acetylaminoethoxy; and X11 is 2 Quin, 3 Quin, 2-Nal, Phe(2-Me), Phe(3-Me), Phe(4-Me), Phe(3,4-dimethoxy), 1-Nal, unsubstituted Trp, or Trp substituted with aryl, unsubstituted or substituted with halo, alkyl, cyano, haloalkyl, hydroxy, alkoxy, haloalkyloxy, phenyl, or substituted phenyl; each of X12, X13, and X14 is independently any amino acid; X15 is absent or any amino acid;
X16 is absent or any amino acid; at least one of X7 and X11 is Trp substituted with substituted or unsubstituted aryl, or substituted or unsubstituted heteroaryl; the C-terminal amino acid is other than Aib, 2 Pal, 3 Pal, 4 Pal, 5 Pyal, THP, His, (D)His, substituted His, substituted (D)His, Phe, substituted Phe, substituted (D)Phe, a-MePhe, substituted a-MePhe, Trp, substituted Trp, substituted or unsubstituted Tyr, substituted or unsubstituted (D)Tyr, substituted or unsubstituted aMeTyr, substituted or unsubstituted (D)aMeTyr, b-hPhe, Sarc, bAla, 1-Nal, aMe(1-Nal), substituted 1-Nal, 2-Nal, aMe(2-Nal), substituted 2-Nal, or N-substituted Asn; wherein the peptide inhibitor is cyclized via a bond between X4 and X9 (see claim 1). The dependent claims further define the variable amino acids with specific residues and SEQ ID Nos:1-19 (claim 79); pharmaceutical formulations thereof (claim 86).
Co-pending Application 19/421560 claims a peptide inhibitor of formula X4-X15 which overlaps with the inhibitor of the instant claims. Co-pending Application 19/421560 claims Pen- Asn-Thr-X7-Gln-Pen-[F(4-2ae)]-X11-[a-MeLeu]-K(Ac)-Asn-Asn (IXa) (claim 44) which falls within the formula of instant claim 1, wherein X7 Trp substituted with alkyl (see claim 32); pharmaceutical formulations thereof (claim 75).
The inhibitors of Co pending 19/421560 fall within Formula I except that X7 is not Trp substituted with an aryl.
However, Frese discloses Boc-protected aryl tryptophan derivatives readily available for peptide synthesis including 7-phenyl- tryptophan(abstract; "different Boc-protected aryl tryptophan derivatives are obtained that can, for example, be used for peptide or peptidomimetic synthesis"; pg 1801 table 2; Boc-7-Ph-W [Box-7-phenyl-Trp]). An artisan of ordinary skill in the art would have followed the disclosure of Frese, because it would have enabled more substitutions at the Trp of X7, making the molecule somewhat more nucleophilic, comparative to the 6-Chloro-Trp already disclosed by Protagonist. Consequently, it would have been obvious for an artisan of ordinary skill to combine all claim limitations, with the exception that X7 is Trp substituted by an unsubstituted aryl, as disclosed by Co pending 19/421560 with X7 is Trp substituted by an unsubstituted aryl, as disclosed by Frese, because it would have enabled a monocyclic peptide inhibitor of IL-23R. It would have been obvious to a person of ordinary skill in the art to select 7-Ph-Trp from the finite number of known amino acid alternatives disclosed in the prior art because such amino acids are recognized as suitable residues for peptide analogs. Selecting these known alternatives would have amounted to no more than the routine optimization of a finite number of predictable options with a reasonable expectations of success (see KSR Int’l Co. v. Teleflex Inc, 550 U.S. 398, 421 (2007), see MPEP 2143). The combination of Co pending 19/421560 and Frese render obvious instant SEQ ID NOs:1-19.
This is a provisional nonstatutory double patenting rejection because the patentably indistinct claims have not in fact been patented.
Claim(s) 1-2, 7, 9, 25, 32, 36, 40, 45, 50, 53, 56, 61, 67, 69, 79, 86 are provisionally rejected on the ground of nonstatutory double patenting as being unpatentable over claims 1-54 of copending Application No. 19/695916 (reference application). Although the claims at issue are not identical, they are not patentably distinct from each other because:
The instant application claims “A monocyclic peptide inhibitor of an interleukin-23 receptor, or a pharmaceutically acceptable salt or solvate thereof, wherein the peptide inhibitor comprises an amino acid sequence of Formula (I′): X3-X4-X5-X6-X7-X8-X9-X10-X11-X12-X13-X14-X15-X16 (I′) wherein X3 is absent or any amino acid, A4 is Abu, Cys or Pen, X5 or X6 is any amino acid, X7 is Trp or substituted or unsubstituted aryl, X8 is any amino acid, X9 is Abu, Cys or Pen…; X10 is unsubstituted Phe, or Phe substituted with halo, alkyl, haloalkyl, hydroxy, alkoxy, carboxy, carboxamido, 2-aminoethoxy, or 2-acetylaminoethoxy; and X11 is 2 Quin, 3 Quin, 2-Nal, Phe(2-Me), Phe(3-Me), Phe(4-Me), Phe(3,4-dimethoxy), 1-Nal, unsubstituted Trp, or Trp substituted with aryl, unsubstituted or substituted with halo, alkyl, cyano, haloalkyl, hydroxy, alkoxy, haloalkyloxy, phenyl, or substituted phenyl; each of X12, X13, and X14 is independently any amino acid; X15 is absent or any amino acid;
X16 is absent or any amino acid; at least one of X7 and X11 is Trp substituted with substituted or unsubstituted aryl, or substituted or unsubstituted heteroaryl; the C-terminal amino acid is other than Aib, 2 Pal, 3 Pal, 4 Pal, 5 Pyal, THP, His, (D)His, substituted His, substituted (D)His, Phe, substituted Phe, substituted (D)Phe, a-MePhe, substituted a-MePhe, Trp, substituted Trp, substituted or unsubstituted Tyr, substituted or unsubstituted (D)Tyr, substituted or unsubstituted aMeTyr, substituted or unsubstituted (D)aMeTyr, b-hPhe, Sarc, bAla, 1-Nal, aMe(1-Nal), substituted 1-Nal, 2-Nal, aMe(2-Nal), substituted 2-Nal, or N-substituted Asn; wherein the peptide inhibitor is cyclized via a bond between X4 and X9 (see claim 1). The dependent claims further define the variable amino acids with specific residues and SEQ ID Nos:1-19 (claim 79); pharmaceutical formulations thereof (claim 86).
Copending Application No. 19/695916 claims a peptide inhibitor of formula Xa which overlaps with the inhibitor of the instant claims. Co-pending Application 19/695916 claims Pen-NTWQ-Pen-Phe[4-2(aminoethoxy-2-Nal-Aib-LysAc-NN-NH2 which falls within the formula of instant claim 1, wherein X7 Trp (see claim 11); pharmaceutical formulations thereof (claim 44).
The inhibitors of copending Application No. 19/695916 fall within Formula I except that X7 is not Trp substituted with an aryl.
However, Frese discloses Boc-protected aryl tryptophan derivatives readily available for peptide synthesis including 7-phenyl- tryptophan(abstract; "different Boc-protected aryl tryptophan derivatives are obtained that can, for example, be used for peptide or peptidomimetic synthesis"; pg 1801 table 2; Boc-7-Ph-W [Box-7-phenyl-Trp]). An artisan of ordinary skill in the art would have followed the disclosure of Frese, because it would have enabled more substitutions at the Trp of X7, making the molecule somewhat more nucleophilic, comparative to the 6-Chloro-Trp already disclosed by Protagonist. Consequently, it would have been obvious for an artisan of ordinary skill to combine all claim limitations, with the exception that X7 is Trp substituted by an unsubstituted aryl, as disclosed by Copending Application No. 19/695916 with X7 is Trp substituted by an unsubstituted aryl, as disclosed by Frese, because it would have enabled a monocyclic peptide inhibitor of IL-23R. It would have been obvious to a person of ordinary skill in the art to select 7-Ph-Trp from the finite number of known amino acid alternatives disclosed in the prior art because such amino acids are recognized as suitable residues for peptide analogs. Selecting these known alternatives would have amounted to no more than the routine optimization of a finite number of predictable options with a reasonable expectations of success (see KSR Int’l Co. v. Teleflex Inc, 550 U.S. 398, 421 (2007), see MPEP 2143). The combination of Copending Application No. 19/695916 and Frese render obvious instant SEQ ID NOs:1-19.
This is a provisional nonstatutory double patenting rejection because the patentably indistinct claims have not in fact been patented.
Claim(s) 1-2, 7, 9, 25, 32, 36, 40, 45, 50, 53, 56, 61, 67, 69, 79, 86 are provisionally rejected on the ground of nonstatutory double patenting as being unpatentable over claims 1-2, 7-11, 14-15, 20-23 of copending Application No. 18/579062 (reference application). Although the claims at issue are not identical, they are not patentably distinct from each other because:
The instant application claims “A monocyclic peptide inhibitor of an interleukin-23 receptor, or a pharmaceutically acceptable salt or solvate thereof, wherein the peptide inhibitor comprises an amino acid sequence of Formula (I′): X3-X4-X5-X6-X7-X8-X9-X10-X11-X12-X13-X14-X15-X16 (I′) wherein X3 is absent or any amino acid, A4 is Abu, Cys or Pen, X5 or X6 is any amino acid, X7 is Trp or substituted or unsubstituted aryl, X8 is any amino acid, X9 is Abu, Cys or Pen…; X10 is unsubstituted Phe, or Phe substituted with halo, alkyl, haloalkyl, hydroxy, alkoxy, carboxy, carboxamido, 2-aminoethoxy, or 2-acetylaminoethoxy; and X11 is 2 Quin, 3 Quin, 2-Nal, Phe(2-Me), Phe(3-Me), Phe(4-Me), Phe(3,4-dimethoxy), 1-Nal, unsubstituted Trp, or Trp substituted with aryl, unsubstituted or substituted with halo, alkyl, cyano, haloalkyl, hydroxy, alkoxy, haloalkyloxy, phenyl, or substituted phenyl; each of X12, X13, and X14 is independently any amino acid; X15 is absent or any amino acid;
X16 is absent or any amino acid; at least one of X7 and X11 is Trp substituted with substituted or unsubstituted aryl, or substituted or unsubstituted heteroaryl; the C-terminal amino acid is other than Aib, 2 Pal, 3 Pal, 4 Pal, 5 Pyal, THP, His, (D)His, substituted His, substituted (D)His, Phe, substituted Phe, substituted (D)Phe, a-MePhe, substituted a-MePhe, Trp, substituted Trp, substituted or unsubstituted Tyr, substituted or unsubstituted (D)Tyr, substituted or unsubstituted aMeTyr, substituted or unsubstituted (D)aMeTyr, b-hPhe, Sarc, bAla, 1-Nal, aMe(1-Nal), substituted 1-Nal, 2-Nal, aMe(2-Nal), substituted 2-Nal, or N-substituted Asn; wherein the peptide inhibitor is cyclized via a bond between X4 and X9 (see claim 1). The dependent claims further define the variable amino acids with specific residues and SEQ ID Nos:1-19 (claim 79); pharmaceutical formulations thereof (claim 86).
Copending Application No.18/579062 claims a peptide inhibitor of formula I which overlaps with the inhibitor of the instant claims. Co-pending Application 18/579062 claims wherein X4 is Pen, X5-6 are amino acids, X7 is Trp substituted, X8 is amino acid, X9 is Pen, X10 is F, X11 is Quin3, Nal, X12-16 are amino acids and the C-terminal can be dL which falls within the formula of instant claim 1; pharmaceutical formulations thereof (claim 15).
The inhibitors of copending Application No. 18/579062 fall within Formula I except that X7 is not Trp substituted with an aryl.
However, Frese discloses Boc-protected aryl tryptophan derivatives readily available for peptide synthesis including 7-phenyl- tryptophan(abstract; "different Boc-protected aryl tryptophan derivatives are obtained that can, for example, be used for peptide or peptidomimetic synthesis"; pg 1801 table 2; Boc-7-Ph-W [Box-7-phenyl-Trp]). An artisan of ordinary skill in the art would have followed the disclosure of Frese, because it would have enabled more substitutions at the Trp of X7, making the molecule somewhat more nucleophilic, comparative to the 6-Chloro-Trp already disclosed by Protagonist. Consequently, it would have been obvious for an artisan of ordinary skill to combine all claim limitations, with the exception that X7 is Trp substituted by an unsubstituted aryl, as disclosed by Copending Application No.18/579062 with X7 is Trp substituted by an unsubstituted aryl, as disclosed by Frese, because it would have enabled a monocyclic peptide inhibitor of IL-23R. It would have been obvious to a person of ordinary skill in the art to select 7-Ph-Trp from the finite number of known amino acid alternatives disclosed in the prior art because such amino acids are recognized as suitable residues for peptide analogs. Selecting these known alternatives would have amounted to no more than the routine optimization of a finite number of predictable options with a reasonable expectations of success (see KSR Int’l Co. v. Teleflex Inc, 550 U.S. 398, 421 (2007), see MPEP 2143). The combination of Copending Application No.18/579062 and Frese render obvious instant SEQ ID NOs:1-19.
This is a provisional nonstatutory double patenting rejection because the patentably indistinct claims have not in fact been patented.
Conclusion
No claims are allowed.
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/ERINNE R DABKOWSKI/Primary Examiner, Art Unit 1654
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