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Patent landscape, scope, and claims: |
United States Patent 12,552,836 (IL-23 Receptor Binding Inhibiting Peptide): Scope, Claim Map, and Landscape
What is patented in US 12,552,836?
US 12,552,836 claims a cyclized peptide inhibitor of IL-23 receptor binding, defined by a specific amino-acid scaffold (Formula II) and ring-closure chemistry (X4 to X9). The patent scope is built around four pillars:
- Biological function: inhibits IL-23 binding to an IL-23 receptor.
- Core sequence logic: a defined variable set at positions X5, X7, X8, X10, X11.
- Cyclization rule: peptide is cyclized via a bond between X4 and X9, with Pen (proline analog) at both positions.
- Drug-like expansion: includes salts/solvates, conjugates (lipophilic/polymeric/PEGylation), and formulation claims (composition, enteric coating).
The claims are not limited to a single peptide. They cover:
- the generic peptide scaffold (claim 1),
- multiple constrained sub-sets (claims 2-7, 12-14, 15-19),
- multiple explicit sequence examples (claim 11),
- optional conjugation/modulation (claims 9-10),
- and pharmaceutical compositions (claims 20-21).
How broad is claim 1, the anchor claim?
Claim 1 defines the subject matter as:
- A peptide inhibitor (or pharmaceutically acceptable salt/solvate)
- Sequence of Formula (II):
X4-X5-X6-X7-X8-X9-X10-X11
- Substitutions:
- X4 = Pen
- X5 = Asn or Gln
- X6 = Thr
- X7 = Trp substituted with alkyl (alkyl at unspecified positions in claim 1)
- X8 = Gln, alpha-Me-Lys, alpha-MeLys(Ac), or Lys(Ac)
- X9 = Pen
- X10 = Phe substituted with 2-aminoethoxy or 2-acetylaminoethoxy
- X11 = 2-Nal or 1-Nal
- Cyclization:
- peptide is cyclized via a bond between X4 and X9
- Mechanism / use:
- inhibits IL-23 binding to an IL-23 receptor.
Scope implications
Claim 1 is structurally defined and functionally tethered. It is broad on:
- two-way substitution at X5 (Asn/Gln),
- multiple options at X8 (four chemical classes including acetylated lysine forms),
- multiple options at X10 (two substitution chemistries),
- two options at X11 (1-Nal vs 2-Nal),
- broad alkyl substitution freedom for Trp at X7 (later constrained in dependent claims).
It is narrow on:
- the backbone positions and fixed residues (X4 Pen, X6 Thr, X9 Pen),
- the cyclization requirement (must connect X4 and X9),
- the end functional target (IL-23 binding inhibition).
What do dependent claims do to narrow the sequence?
X5 narrowing
- Claim 2: X5 is Asn (removes the Gln branch).
X8 narrowing
- Claim 3: X8 is Gln or Lys(Ac)
- Claim 4: X8 is alpha-Me-Lys or alpha-MeLys(Ac)
X10 narrowing
- Claim 5: X10 is Phe[4-(2-aminoethoxy)]
(claim 1 also includes 2-acetylaminoethoxy at X10; claim 5 selects one).
X7 narrowing (Trp-alkyl pattern)
- Claim 6: X7 is Trp substituted with methyl, ethyl, n-propyl, or isopropyl.
- Claim 13: alkyl substitution can be at 4-, 6-, or 7-position of the Trp.
- Claim 14: explicit allowed substitutions:
- W(1-Me), W(4-Me), W(6-Me), W(6-Et), W(7-Me), W(7-Et), W(7-n-Pr), W(7-i-Pr)
This creates a layered fence: claim 1 allows “alkyl substituted Trp,” while claims 13-14 impose a positional and enumerated set.
X11 narrowing
- Claim 7: X11 is 2-Nal (removes 1-Nal).
How is cyclization specified, and why it matters
Claim 1 requires cyclization between X4 and X9. Dependent claim 12 tightens the bond:
- Claim 12: the bond between X4 and X9 is a disulfide bond.
The independent language in claim 1 is already cyclization “via a bond between X4 and X9.” Claim 12 makes the chemistry explicit and can be used to:
- differentiate from alternative cyclizations (e.g., amide linking) if competitors design a different closure method.
What explicit compounds are covered (Seq IDs in claim 11)?
Claim 11 enumerates multiple peptides (SEQ ID NOs) as selectable members of claim 1’s scaffold. These sequences are structurally consistent with:
- Ac- N-terminus,
- Pen at X4 and X9 (cyclized by a Pen-Pen disulfide bond),
- Trp substituted with alkyl (e.g., W(7-Me), W(7-Et), W(7-n-Pr)),
- X8 = Lys(Ac) with α-Me-Lys variants in the list (as shown),
- X10 = Phe[4-(2-aminoethoxy)],
- X11 = 2-Nal,
- and a variable residue at the C-terminal amide segment (shown as N-[BA]-NH2 or alternatives like N-[(D)Leu], N-H-NH2, N-[(D)Val], N-[(D)Lys], N-[(D)Phe], N-[(D)Cit], etc.).
The claim includes at least these listed members:
- SEQ ID 242: Ac-[Pen]-NT-[W(7-Me)]-[Lys(Ac)]-[Pen]-Phe[4-(2-aminoethoxy)]-[2-Nal]-[α-MeLys]-[Lys(Ac)]-N-[BA]-NH2
- SEQ ID 245: same core but N-[(D)Leu]-NH2
- SEQ ID 248: same core but N-H-NH2
- SEQ ID 249: same core but N-[Cit]-NH2
- SEQ ID 251: same core but N-[(D)Val]-NH2
- SEQ ID 252: same core but N-[(D)Lys]-NH2
- SEQ ID 258: same core but N-[(D)Phe]-NH2
- SEQ ID 284: W(7-Et) variant with N-[(D)Leu]-NH2
- SEQ ID 285: W(7-n-Pr) variant with N-[(D)Leu]-NH2
Claim 11 ends with the requirement that the peptide is cyclized via a Pen-Pen disulfide bond.
Dependent “compound pick” claims
- Claim 15 reproduces the scaffold constraints in an enumerated way:
- X4 Pen; X5 Asn; X6 Thr; X7 Trp-alkyl; X8 Gln or Lys(Ac); X9 Pen; X10 Phe[4-(2-aminoethoxy)]; X11 2-Nal; cyclized between X4 and X9; IL-23 binding inhibition.
- Claims 16-19 identify specific peptide instances:
- Claim 16: recites SEQ ID NO: 6, 284, 285 (with disulfide cyclization).
- Claims 17-19: each narrows to a specific SEQ ID (6, 284, 285), with disulfide cyclization.
This is a classic pattern: broad genus (claim 1) + enumerable exemplars (claim 11) + “fallback” narrow exclusives (claims 16-19).
What expansion does claim 8 introduce (R1-X-R2 format)?
Claim 8 adds a more generic structural framing:
- peptide inhibitor comprises structure of Formula (Z):
R1—X—R2 (Z)
where:
- R1 is a bond, hydrogen, Ac, C1-C6 alkyl, C6-C12 aryl, aryl-C1-6alkyl, C1-C20 alkanoyl, and includes PEGylated versions as alone or as spacers
- X is the amino acid sequence of Formula (II)
- R2 = OH or NH2
This claim broadens how the peptide can be presented at termini and introduces PEGylation as a permissible modification route, without changing the X core.
What does claim 9-10 cover on conjugates?
Claim 9: peptide inhibitor further comprises a conjugated chemical substituent selected from:
- lipophilic substituent
- or polymeric moiety
Claim 10 enumerates the specific conjugates:
- Ac, Palm, gammaGlu-Palm, isoGlu-Palm, PEG (MW 400 to 40,000), PEG2-Ac, PEG4-isoGlu-Palm, (PEG)5-Palm
- acids and linkers: succinic acid, glutaric acid, pyroglutaric acid, benzoic acid
- hydrophobics: IVA, octanoic acid, 1,4 diaminobutane, isobutyl
- targeting: biotin
Strategic read
The independent scaffold is peptide-defined, but claims 9-10 create a conjugate perimeter that can catch many “me-too” delivery and solubility modifications, as long as the core scaffold and IL-23 binding inhibition remain.
What about formulation scope (claims 20-21)?
- Claim 20: pharmaceutical composition comprising the peptide inhibitor (or salt/solvate) + pharmaceutically acceptable carrier, excipient, or diluent.
- Claim 21: composition further comprising an enteric coating.
This is a standard formulation layer that can matter for:
- oral delivery strategies,
- gastro-resistance and release profile,
- and patentability over purely active-ingredient claims.
How does this patent likely sit in the IL-23 peptide landscape?
Core claim theme
Across the claim set, the patent is built around a tight peptide pharmacophore with:
- Pen-Pen cyclization via disulfide
- Trp substituted with alkyl
- Phe[4-(2-aminoethoxy)] substitution
- Nal isomer requirement
- and IL-23 receptor binding inhibition.
This combination suggests the patent is targeting a specific IL-23 axis neutralization mechanism using a constrained peptide design rather than antibodies.
Design-around pressure points
Competitors can attempt to avoid literal infringement by altering one of the claim-essential elements, such as:
- cyclization chemistry (avoiding a disulfide bond, if claim 12 is asserted),
- changing Pen residues or the X4-X9 linkage rule,
- altering the IL-23 binding inhibition claim element (harder because assays determine function),
- changing X10 substitution pattern (switching away from 2-aminoethoxy / 2-acetylaminoethoxy),
- changing the Nal isomer requirement (1-Nal vs 2-Nal).
However, because claim 1 is a genus with several enumerated options, the design space for “safe” variants is narrower than it would be for a single fixed sequence patent.
Claim coverage map (what to watch for in competitor products)
Must-have elements from claim 1
- Cyclized peptide: X4 to X9 bond where X4 and X9 are both Pen
- Sequence positions:
- X5 is Asn or Gln
- X6 is Thr
- X7 is Trp substituted with alkyl
- X8 is one of: Gln, α-Me-Lys, α-MeLys(Ac), Lys(Ac)
- X10 is Phe substituted with 2-aminoethoxy or 2-acetylaminoethoxy
- X11 is 2-Nal or 1-Nal
- Function: inhibits IL-23 binding to IL-23 receptor
Additional fences from dependent claims
- Disulfide cyclization: claim 12
- Enteric coating: claim 21
- Specific Trp substitution list: claims 13-14
- Specific X10 choice: claim 5
- Specific X11 choice: claim 7
- Conjugate types: claims 9-10
- Explicit exemplar sequences: claim 11 and narrower claims 16-19
Practical patent landscape implications for R&D and partnering
1) The patent has both breadth and “fallback” depth
- Claim 1 gives broad genus coverage across key side-chain variants.
- Claim 11 enumerates multiple embodiments, reducing the odds that an accused product falls outside all listed examples.
- Claims 16-19 offer narrow anchors tied to specific SEQ IDs, useful for enforcement if a competitor shifts only some side-chain substitutions.
2) Conjugation and PEGylation are integrated into scope
- Claims 8 and 9-10 allow multiple termini/conjugate modifications.
- A competitor cannot simply swap delivery format (PEGylation, lipophilic conjugates) without re-checking that the core X scaffold still reads on claim 1.
3) Formulation IP matters for oral strategies
- Enteric coating in claim 21 creates a narrow but relevant hook for oral delivery.
Key Takeaways
- US 12,552,836 is a sequence-and-chemistry defined IL-23 receptor binding inhibitor patent centered on a cyclized Pen-Pen peptide scaffold with specific variable residues (X5, X7, X8, X10, X11).
- Claim 1 is the controlling genus: cyclization between X4 and X9, where X4 and X9 are Pen, and the peptide inhibits IL-23 binding to the IL-23 receptor.
- The patent has multi-layer narrowing through dependent claims (disulfide cyclization; enumerated Trp alkyl substitution positions; specific side-chain options; explicit SEQ IDs).
- Conjugates and PEGylation are expressly covered (claims 8, 9-10), increasing capture risk for “delivery-only” variants that keep the same peptide pharmacophore.
- Formulation claims include enteric coatings, relevant for oral product development.
FAQs
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Is infringement controlled by sequence alone or by biological function too?
Claim 1 requires both: the peptide must match the Formula (II)/cyclization scaffold and it must inhibit IL-23 binding to an IL-23 receptor.
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Does the patent require disulfide cyclization?
Claim 1 requires cyclization between X4 and X9; claim 12 specifically limits the bond to a disulfide bond.
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Can changes to Trp-alkyl substitution avoid coverage?
Claim 1 allows alkyl substitution; dependent claims (13-14) enumerate specific positions/substitutions. A safe variant must avoid the claim’s allowed substitution set and still remain outside the genus.
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Are PEGylated versions covered?
Yes. Claim 8 explicitly includes PEGylated versions (alone or as spacers), and claim 10 enumerates PEG molecular weight ranges.
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Do the claims cover specific named peptides?
Yes. Claim 11 lists multiple SEQ ID NOs as covered peptide inhibitors, and claims 16-19 further narrow to specific exemplars (including SEQ ID 6, 284, 285).
References
- United States Patent No. 12,552,836. (Claims as provided in the user prompt).
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