Scope and Claims Review for US Drug Patent 11,845,808
United States Patent 11,845,808 is directed to (1) a specific class of “monocyclic peptides” cyclized through a Pen-Pen disulfide bond, (2) closely defined sequence variants defined by Formula (I) / Formula (Z′), (3) explicit exemplified sequences (SEQ ID NO:104, 158, 247), and (4) treatment methods using the peptides (or salts) for diseases linked to IL-23 or IL-23R, with broad route-of-administration coverage.
The practical claim architecture is: composition-by-structure (claims 1-11) and use methods for IL-23/IL-23R indications (claims 12-30). Claims 12-30 are largely the same method frame, anchored to dependent references to particular composition claims (claim 5 in claim 12; claims 6-8 in later claims).
What is the core claimed chemical scaffold and how is it constrained?
A. “Monocyclic peptide” definition
The peptides are constrained by:
- A specific amino-acid sequence pattern given by Formula (I) and (Z′)
- A cyclic constraint: “cyclized via a Pen-Pen disulfide bond”
- Variable positions are limited to a small set (key examples: X7 options; X10 and X12 fixed; X12 fixed as THP; X15 fixed as 3Pal)
B. Claim 1: Formula (I) with position-level constraints
Claim 1 covers a monocyclic peptide defined by Formula (I):
X3-Pen-N-T-X7-Lys(Ac)-Pen-X10-2Nal-X12-E-N—X15-Sarc (Formula (I))
plus pharmaceutically acceptable salts, with:
- Cyclization: Pen-Pen disulfide bond
- X3: absent or any amino acid
- X7: Trp, 7-methyl tryptophan (W(7-Me)), or 7 phenyl tryptophan (W(7-Ph))
- X10: Phe(4-(2-aminoethoxy))
- X12: 4-amino-4-carboxy-tetrahydropyran (THP)
- X15: 3-pyridyl substituted alanine (3Pal)
- Lys(Ac): lysine bearing an acetylated side chain (as written)
Scope implication: claim 1 is broad as to X3 (“absent or any amino acid”) and moderate as to X7 (three enumerated aromatic variants). X10, X12, X15 are locked to specific nonstandard residue types.
C. Claim 2: adds a terminal/marker structure (Formula (Z′))
Claim 2 is narrower than claim 1 because it specifies a full sequence wrapper:
R1-X3-Pen-N-T-X7-Lys(Ac)-Pen-X10-2Nal-X12-E-N-3Pal-Sarc-R2 (Formula (Z′))
with:
- R1: hydrogen or Ac
- R2: NH2
- X3: absent or (D)Arg
- X7: Trp, W(7-Ph), or W(7-Me)
- Fixed residues: X10 = Phe(4-(2-aminoethoxy)); X12 = THP; the C-terminal residue is Sarc followed by R2
Scope implication: Compared with claim 1, claim 2 eliminates “any amino acid” at X3 and limits it to “absent or (D)Arg.” That matters for freedom-to-operate (FTO) because substitutions at X3 beyond D-Arg would fall outside claim 2 (but may still fall within claim 1 if they qualify under “any amino acid” when X3 is present and aligned).
D. Claims 3-4: tighten R1 and X3/X7 combinations
- Claim 3: R1 is Ac (or salt)
- Claim 4: further constrains to:
- R1 = Ac
- X3 absent
- X7 = W(7-Ph) (or salt)
Scope implication: Claim 4 identifies a single, very specific variant.
Which explicit sequences are enumerated, and what does that do to claim scope?
Claim 5: explicit sequence list (SEQ ID NOs) + Pen-Pen disulfide
Claim 5 covers monocyclic peptides comprising one of three explicitly enumerated amino-acid sequences (or salts):
-
Ac-[Pen]-N-T-[W(7-Me)]-[Lys(Ac)]-[Pen]-[Phe(4-(2-aminoethoxy))]-[2-Nal]-[THP]-E-N-[3Pal]-[Sarc]-NH2
(SEQ ID NO:104)
-
Ac-[Pen]-N-T-W-[Lys(Ac)]-[Pen]-[Phe(4-(2-aminoethoxy))]-[2-Nal]-[THP]-E-N-[3Pal]-[Sarc]-NH2
(SEQ ID NO:158)
-
Ac-[(D)Arg]-[Pen]-N-T-[W(7-Me)]-[Lys(Ac)]-[Pen]-Phe[4-(2-aminoethoxy)]-[2-Nal]-[THP]-E-N-[3Pal]-[Sarc]-NH2
(SEQ ID NO:247)
Each is cyclized via Pen-Pen disulfide bond.
Scope implication: Claim 5 functions as a “catch” for specific commercial-relevant variants: Trp, W(7-Me), and W(7-Me) with D-Arg at the X3 position. If a competitor’s peptide matches any listed SEQ ID exactly (including acetylation and sequence order), they land within claim 5 regardless of how novelty is framed elsewhere.
Claims 6-8: dependent formatting and anchor sequence
- Claim 6 and Claim 7 state the peptide “has the structure:” but the provided text for claims 6-7 is not legible beyond “a pharmaceutically acceptable salt thereof” (the underlying intended dependency likely fixes the structure to a dependent claim variant).
- Claim 8 is explicit:
- peptide comprises the sequence of SEQ ID NO:247,
- cyclized via Pen-Pen disulfide bond.
Scope implication: Claim 8 is an even more specific “subset” of claim 5, pinning down SEQ ID NO:247.
How do the method claims use the composition claims to create enforceable treatment scope?
Method claim core
Claims 12, 19, and 27-28 recite treatment methods for diseases associated with IL-23 or IL-23R by administering an effective amount of the monocyclic peptide or salt of a referenced composition claim.
Claim 12: broad indication list, anchored to claim 5
Claim 12:
- Administer monocyclic peptide (or salt) of claim 5
- To treat conditions associated with IL-23 or IL-23R
- Indications include:
- IBD
- Ulcerative colitis (UC)
- Crohn’s disease (CD)
- Psoriasis (PsO)
- Psoriatic arthritis (PsA)
- Routes include an extensive list (see below)
Claims 13-15 narrow within that frame to:
- Claim 13: Psoriasis
- Claim 14: Psoriatic arthritis
- Claim 15: IBD
Claim 16-17: route-of-administration expansion
- Claim 16 lists essentially all major routes, including oral and many parenteral/inhalation/topical options.
- Claim 17 narrows the route to:
- oral, sublingual, buccal, or topical
Scope implication: This is a high-enforcement position because it blocks design-around by simply changing administration route, at least for the named subset in claim 17.
Claim 18 and 30: sub-indication
- Claim 18: plaque psoriasis
- Claim 30: plaque psoriasis
Claims 19-23: anchored to claim 6
- Claim 19 is similar to claim 12, but administers “the monocyclic peptide or salt thereof of claim 6”
- Claim 20: psoriasis
- Claim 21: psoriatic arthritis
- Claim 22: inflammatory bowel disease
- Claim 23 includes the same broad route list as claim 16
Claims 25-26: UC and CD explicit
- Claim 25: Ulcerative colitis (UC)
- Claim 26: Crohn’s Disease (CD)
Claims 27-28: anchored to claims 7-8
- Claim 27: administered peptide of claim 6 (as written in your text, it says claim 6 for claim 27; however the claim text you pasted indicates “of claim 6” for claim 27. The structure is still “IL-23/IL-23R treatment method + disease list.”)
- Claim 28: administered peptide of claim 8
- Both again include IBD/UC/CD/PsO/PsA and broadly covered routes in later dependencies.
Scope implication: The method claims build multiple enforceable “pillars” around multiple specific composition claims. Even if one composition claim is invalidated or avoided, another dependent pillar tied to the alternative composition claim can remain intact.
What is the practical claim scope map (composition vs. method)?
Composition scope
| Claim |
What is claimed |
Key constraints that limit/define scope |
| 1 |
Monocyclic peptide of Formula (I) |
Pen-Pen disulfide cyclization; X3 absent or any amino acid; X7 limited to Trp, W(7-Me), W(7-Ph); X10 fixed; X12 fixed (THP); X15 fixed (3Pal) |
| 2 |
Monocyclic peptide of Formula (Z′) |
Adds R1 (H or Ac) and R2 = NH2; X3 limited to absent or (D)Arg |
| 3 |
Claim 2 subset with R1 = Ac |
Narrows N-terminal chemistry |
| 4 |
Claim 2 subset with R1 = Ac, X3 absent, X7 = W(7-Ph) |
Narrows to one sequence family corner |
| 5 |
Three explicit sequences (SEQ IDs 104/158/247) |
Pen-Pen disulfide cyclization; sequence exactness controls inclusion |
| 6-8 |
Dependent structure/sequence pinning |
Claim 8 explicitly pins SEQ ID NO:247 and cyclization |
Method scope
| Claim |
Anchored composition |
Indications (representative set) |
Route scope |
| 12 |
Claim 5 |
IL-23/IL-23R linked: IBD, UC, CD, PsO, PsA |
Very broad list; includes oral and topical |
| 13-15 |
Claim 12 |
PsO, PsA, IBD |
Uses claim 12 route scope (unless otherwise narrowed) |
| 16-17 |
Claim 12 |
Same indications |
Claim 17 constrains to oral/sublingual/buccal/topical |
| 18, 30 |
Claim 12/20 |
Plaque psoriasis |
Uses relevant route scope |
| 19-23 |
Claim 6 |
Same IL-23/IL-23R set |
Broad list in 23; depends on prior claim framework |
| 25-26 |
Claim 19 |
UC, CD |
Uses claim 19/23 route scope |
| 27-28 |
Claims 7/8 (as provided) |
Same IL-23/IL-23R set |
Broad list in 23-like dependencies |
How strong is the enforceability through breadth versus specificity?
Composition claims
- Breadth lever: Claim 1 allows “X3 absent or any amino acid,” meaning variants that alter X3 could still infringe if they preserve the other constrained residues and the Pen-Pen disulfide cyclic structure.
- Narrowness lever: Claim 2 cuts X3 to absent or (D)Arg, and Claim 5 uses exact SEQ ID sequences that likely correspond to actual clinical or development compounds. Those exact-sequence claim positions can be very strong if a competitor product matches.
Method claims
- Method claims cover:
- multiple indications (IBD/UC/CD/PsO/PsA)
- both general and sub-indications (plaque psoriasis, UC, CD)
- wide route-of-administration coverage, including oral and topical families
The result is that enforcement is not limited to a single patient population or administration format, at least within the claim language.
Patent landscape analysis for US 11,845,808 (scope-based, competition-relevant view)
A full landscape normally requires bibliographic data, family members, prosecution history, continuations, and citation trees. Those data are not present in the provided record. The analysis below therefore focuses on what landscape battles are implied by the claim structure you supplied.
1) Likely competitive attack surfaces
Because the claims are anchored on:
- a Pen-Pen disulfide monocycle architecture
- rare residue identities: THP, 3Pal, 2Nal, Sarc, Pen, plus modified tryptophan variants (W(7-Me)/W(7-Ph))
- sequence exactness in claim 5 and structural formula constraints in claim 1-4
- IL-23/IL-23R indication framing
…typical landscape pressure points are:
- alternative cyclic constraints (disulfide position/chemistry different from Pen-Pen)
- substitutions at fixed residues (X10, X12, X15)
- loss of the exact sequence in SEQ ID enumerations (claim 5)
- different target axis (IL-23 versus IL-23R) is still largely covered because the claims name both “IL-23” and “IL-23R”
2) How competitors can design around (and where the claims still catch them)
Given the claim dependencies:
- If a competitor changes only X7 among Trp, W(7-Me), W(7-Ph): claim 1 stays broad; claim 5 covers only two of the three X7 possibilities explicitly (SEQ ID 158 has W (standard), SEQ ID 104 and 247 have W(7-Me); W(7-Ph) is not explicitly in claim 5 as pasted).
- If a competitor changes X3 beyond D-Arg (when present): claim 2 excludes it, but claim 1 can still cover it (“any amino acid”).
- If a competitor changes N-terminus acetylation: claim 2 includes R1 = H or Ac; claim 3 fixes R1 = Ac; method claims do not explicitly restrict N-terminus beyond whatever composition claim is referenced (e.g., claim 5 always begins with “Ac-” in your sequences).
3) Why the route-of-administration matters to landscape competitors
Route-of-administration is a common design-around lever in peptides.
Here, method claims include both:
- oral and parenteral families in claim 16
- oral/sublingual/buccal/topical in claim 17
This compresses design-around space unless the competitor avoids every covered route combination and instead pursues a non-listed route not captured by these dependencies.
Claim-by-claim scope stress points (what to watch in FTO/invalidation strategy)
For composition infringement
Key “must match” elements:
- Pen-Pen disulfide cyclization (structural requirement in all peptide claims you provided)
- Fixed residues:
- X10 = Phe(4-(2-aminoethoxy))
- X12 = THP
- X15 = 3Pal
- Sequence positions:
- X7 is limited to Trp/W(7-Me)/W(7-Ph)
- X3 handling depends on claim: broad in claim 1, constrained to absent/D-Arg in claim 2 and claim 5’s SEQ ID set
For method infringement
Key “must be present” elements:
- the peptide (or salt) must correspond to the referenced composition claim
- the treated condition must be framed as associated with IL-23 or IL-23R
- the route must fall within the claimed routes for the specific dependent method claim
Key Takeaways
- US 11,845,808 is built on a Pen-Pen disulfide monocyclic peptide with a tightly defined sequence grammar that fixes THP (X12), 3Pal (X15), and a specialized Phe side chain (X10), while varying X7 among Trp and modified tryptophans.
- Claim 1 is the broad structural backbone because X3 can be absent or “any amino acid” while retaining the core scaffold and fixed residues.
- Claim 2 materially narrows X3 to “absent or (D)Arg” and fixes N-terminal/R-group parameters.
- Claim 5 enumerates three specific peptide sequences (SEQ ID NO:104, 158, 247), which creates high-value enforcement anchors against products that match those sequences exactly.
- Method claims cover IL-23/IL-23R-associated diseases across IBD/UC/CD and psoriasis/psoriatic arthritis, with broad route-of-administration language, including oral and topical families (via dependent claim language).
FAQs
-
Does the patent cover monocyclic peptides only, or also linear peptides?
It covers “monocyclic peptide” structures cyclized via a Pen-Pen disulfide bond, so the claim language is limited to monocyclic/disulfide-cyclized peptides.
-
Which amino-acid positions are most important for distinguishing infringement risk?
The fixed residues X10 (Phe(4-(2-aminoethoxy))), X12 (THP), and X15 (3Pal) are central. X7 variants are limited, and X3 is broad in claim 1 but narrowed in claim 2.
-
Are the listed SEQ ID sequences a complete set of all possible variants?
No. The claim set includes both formula-based coverage (claims 1-4) and enumerated sequences (claim 5). Formula coverage can extend beyond the explicit SEQ IDs.
-
Do method claims require a specific route like injection?
No. Dependent claims include broad administration routes and explicitly include oral and topical families.
-
If a product treats IL-23R but not IL-23, is it covered?
Yes. The method claims expressly cover diseases associated with IL-23 or IL-23R.
References
[1] United States Patent 11,845,808 (claims as provided in the prompt).
