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Patent landscape, scope, and claims: |
United States Patent RE42376: Scope, Claims Architecture, and Patent Landscape
What does RE42376 claim, structurally?
RE42376 is a US reissue patent with a core “Formula 1” definition that covers a broad, combinatorial set of quinoline- and quinoline-substituted amide and carbonitrile type compounds, plus downstream method and composition claims. The claim set is dominated by one very large Markush-style genus claim (Claim 1), expanded with multiple dependent claim tiers and multiple species lists.
The scope is built around a substituted heteroaromatic scaffold with:
- Two key ring/hinge regions controlled by X (aryl/cycloalkyl) and Het (heterocycle),
- A linkage system controlled by Z and a “linker” set Y, M, W (and their provisos),
- Terminal functional groups controlled by R (alkyl or carboalkyl) and by G1, G2, R1, R4 on the aromatic system,
- A broad substitution allowance for X (halogen; C1-C6 alkyl; multiple C2-C6 alkenyl and C2-C6 alkynyl; azido; hydroxylalkyl; cyano; nitro; CF3; carboalkoxy; amino/amido motifs; thioethers; etc.),
- Extensive variation on heterocycles: morpholine/thiomorpholine, piperidine/pyrrolidine, piperazine, imidazole/triazoles/thiazoles/tetrazoles, and fused/oxygenated rings,
- Extensive variation on substituents R6 attached to heteroatoms/carbons of Het (H, C1-C6 alkyl, halo-substituted phenyl, amino, nitro, cyano, azido, hydroxyl, and multiple protected or functionalized fragments).
Claim 1 is the binding constraint: a compound “of Formula 1” where X, Z, R, G1/G2/R1/R4, Y/M/W/Het/R6, and auxiliary group parameters (J, Q, a, g, k, n, p, q, r, s, u, v) must satisfy the specified ranges and provisos, and where the final outcome also includes pharmaceutically acceptable salts.
How wide is Claim 1’s genus?
Claim 1 is a large Markush genus constrained by:
- X definition (major breadth):
- Cycloalkyl C3-C7 with optional C1-C6 alkyl substitution, or
- Pyridinyl, pyrimidinyl, or phenyl optionally mono-, di-, tri-substituted by an extremely wide substituent list.
- Z: one of —NH—, —O—, —S—, or —NR—.
- R: alkyl C1-C6 or carboalkyl C2-C7.
- G1, G2, R1, R4: independently selected from a long list (H, halo, alkyl/alkenyl/alkynyl, hydroxymethyl/halomethyl, multiple oxyl groups, sulfonamide/sulfonyl variants, hydroxy, CF3/CF3O, cyano, nitro, carboxy/carboalkoxy/carboalkyl, phenoxy/phenyl/thiophenoxy/benzyl/anilines, carbamoyl patterns, and more), subject to a key proviso that either G1 or G2 (or both) must fall into a designated subset involving the heteroaromatic “R8R9/CH–M–(C(R6)2)k–Y” family.
- Y, M, W and Het:
- Het is limited to a defined heterocycle list (morpholine family, piperidine family, triazoles, thiazoles, tetrazole, piperazine, furan/thiophene, and various O-containing rings).
- Y is a divalent radical that is tightly tied to nitrogen/oxygen attachment patterns:
- Includes R7—(C(R6)2)s—, R7—(C(R6)2)pNR6R6…, R8R9—CH—M—(C(R6)2)k—Y—, Het-(C(R6)2)q—W—(C(R6)2)k—Y— with a proviso that blocks certain morpholine-linked motifs.
- M and W are selected from >NR6, —O—, or defined substituted amide-like nitrogen patterns, with further coupling constraints to k, p, q, and to the nature of Y and W.
- Numerical parameters (ranges rather than fixed):
- k=0-4, p=2-4, q=0-4, r=1-4, s=1-6, g=1-6, a=0 or 1, n=0 or 1, and u+v=2-4 (with each individually 0-4).
- Multiple conditional parameter caps depending on the chosen structural variables:
- If R6 is alkenyl C2-C7 or alkynyl C2-C7, that alkenyl/alkynyl must be bound to N or O via a saturated carbon.
- When Y is —NR6— and R7 is —NR6R6, —N(R6)3+, or —NR6(OR6), then g=2-6.
- When M is —O— and R7 is —OR6, then p=1-4.
- When Y is —NR6—, then k=2-4.
- When Y is —O— and M or W is —O—, then k=1-4.
- When W is not a bond with Het bonded through nitrogen, then q=2-4.
- When W is a bond with Het bonded through nitrogen and Y is —O— or —NR6—, then k=2-4.
Net effect: Claim 1 covers a very large combinatorial space, but it is not “anything goes.” The provisos create structural dependencies that limit some linker-heterocycle combinations and force specific parameter bands.
What does the claim list include as “species” inside Claim 5?
Claim 5 is a species list (still within the Claim 1 genus) that enumerates specific compounds. It uses a, b, c … mmmm style list covering dozens of concrete structures.
Examples from Claim 5 (not exhaustive):
- b) “N-[4-[(3-Bromophenyl)amino]-3-cyano-6-quinolinyl]-4-(N-allyl-N-methylamino)-2-butynamide…”
- c) “N-[4-[(3-Bromophenyl)amino]-3-cyano-6-quinolinyl]-4-(N-methoxyethyl-N-methylamino)-2-butynamide…”
- f) “4-(4-Chloro-2-fluoro-phenylamino)-6-methoxy-7-(2-pyridin-4-yl-ethoxy)-1-quinoline-3-carbonitrile…”
- h) “4-((2S)-2-Methoxymethylpyrrolidin-1-yl)but-2-ynoic acid…”
- i) spirocyclic variant: “4-(1,4-Dioxa-8-azaspiro[4,5]dec-8-yl)but-2-ynoic Acid…”
- l) includes dihydrochloride salt: “(S)-4-(2-Methoxymethyl-pyrrolidin-1-yl)-but-2-enoic acid…dihydrochloride…”
- v) “4-[(E)-2-(2-quinolinyl)ethenyl]aniline…”
- cc) a thiazolium: “3-{3-[4-(3-Chloro-4-fluoro-phenylamino)-3-cyano-7-methoxy-quinolin-6-ylcarbamoyl]-allyl}-4-methyl-thiazol-3-ium bromide…”
- jj) includes “7-methoxy-6-pyrrolidin-1-yl” quinoline carbonitrile style compound.
Implication for enforcement strategy: The presence of explicit species in Claim 5 tightens infringement targets. Even with broad genus language, these species can anchor validity and provide clearer claim-to-structure mapping for known lead molecules.
What are the operative pharmaceutical “use” claims?
Beyond compound claims, RE42376 includes:
- Claim 6: a broad therapeutic method: treating, inhibiting growth of, or eradicating a neoplasm in a mammal using an effective amount of a Formula 1 compound.
- Claim 7: limits neoplasm sites to a list: breast, kidney, bladder, mouth, larynx, esophagus, stomach, colon, ovary, and lung.
- Claim 8: treatment of polycystic kidney disease with the Formula 1 compound.
Claim 9 adds a composition claim: a pharmaceutical composition comprising a Formula 1 compound or pharmaceutically acceptable salt.
Claims 39-43 similarly create composition claim variants tied to narrower subsets, e.g.,:
- Claim 39: composition comprising a compound of Claim 5 or Claims 10-34 or salts thereof.
- Claims 40-43: compositions tied to “compound of Claim 35”, “Claim 36”, “Claim 37”, and “Claim 38” respectively.
How are later compound claims narrowing the genus?
Claims 10-38 are layered structure definitions, each narrowing subsets of Claim 1 (or repackaging subsets with a smaller choice set). The narrowing pattern is consistent:
- Fix X to phenyl or constrain X substituents (e.g., “halogen only”, “methoxy only”, “chloro only”, etc.).
- Fix Z to —NH— and fix R1/R4 to hydrogen in several tiers.
- Constrain G1 (e.g., allow “alkoxy” then “methoxy”).
- Constrain Het to specific heterocycles (or N-substituted piperazine motifs).
- Constrain W and k to specific patterns (e.g., W is a bond; W bonded through N to Het and k=2-4; or k=3).
Selected examples:
- Claim 10: constructs a compound where X is a substituted phenyl ring with Z=—NH—, R1=R4=H, and restricts Het to a smaller set (pyridine; disubstituted morpholine; thiomorpholine derivatives; imidazole derivatives; thiazole/thiazolidine; N-substituted 1,4-piperazine; N-substituted piperidine; dioxane/dioxolane; N-substituted pyrrolidine).
- Claim 13: Het is N-substituted 1,4-piperazine.
- Claim 15: X is a phenyl ring with halogen (chloro) constraint.
- Claim 16: Het is again N-substituted 1,4-piperazine.
- Claims 35-38: impose constraints like G1=methoxy, W is a bond, Het bonded through nitrogen with k=2-4, and k=3.
This architecture produces a typical “genus plus layered species subsets” profile intended to preserve claim coverage across design-around space.
What is the practical patent landscape around RE42376?
This dataset does not include:
- the original US patent number from which RE42376 reissued,
- application publication numbers,
- prosecution history (e.g., continuation relationships, priority data),
- INPADOC family status,
- licensing or marketing authorizations connected to the covered compounds,
- citations to earlier patent families or later patent families.
Because no patent landscape identifiers (assignee, priority, earlier patent numbers, related publications) are provided, a complete, defensible landscape cannot be produced from the claim text alone.
Scope map: what a competitor must avoid structurally
Even without landscape bibliometrics, the text itself indicates the key design-around pressure points:
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Attachment constraints for the linker (Y-M-W system)
- Several “if-then” parameter restrictions tie k, p, q, g to whether Y is —NR6— vs —O—, whether M or W is —O—, and whether W bonds to Het via nitrogen.
- These constraints limit alternative attachment patterns that would otherwise preserve pharmacophore logic while changing geometry.
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Heterocycle selection (Het set)
- Het must be in the listed set in Claim 1.
- Many design-around attempts that swap morpholine for a different tertiary amine ring not in the list would fall outside.
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Blocked morpholine-linked motif
- The proviso in Claim 1 prohibits at least one R3 group from being a Het-(C(R6)2)q—W—(C(R6)2)r— pattern “where Het is morpholino-N-alkyl” with specified alkyl/azacycloalkyl constraints.
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G1/G2/R1/R4 substituent constraints
- Claim 1 imposes that either G1 or G2 (or both) must be within a restricted subset featuring the R8R9/CH-M-(C(R6)2)k-Y-like radicals.
- A competitor changing substitution positions or omitting that radical class could move out of Claim 1 even if they preserve the overall scaffold.
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Fixed substructures in dependent claims
- Claims 10-18 and 20-34, 35-38 constrain further variables like Z, R1/R4, Het type, G1 identity (methoxy), W being a bond, and k values.
- Even if a design-around escapes the broadest genus, it may still fall into a narrower dependent claim tier if it retains those constraints.
Key Takeaways
- RE42376’s claim scope is driven by a large Markush genus (Claim 1) covering Formula 1 quinoline-linked amide/carbonitrile structures with extensive substituent variation, but with multiple linker-parameter provisos that tightly couple Y/M/W/Het and several integer indices.
- Species coverage is explicit through Claim 5’s long enumerated list, supporting clearer infringement mapping for known exemplified molecules.
- Therapeutic scope is broad: neoplasm treatment by administration (Claim 6), neoplasm site list (Claim 7), and polycystic kidney disease treatment (Claim 8), plus broad composition claims (Claims 9, 39-43).
- A competitor’s strongest design-around pressure points are Y/M/W parameter dependencies, Het selection, the blocked morpholine-linked motif, and the required radical class for G1/G2 (Claim 1 proviso).
- A complete US patent landscape analysis (families, priority chain, related continuations, and competitor overlap) cannot be derived from the claim text provided here, since no bibliographic family identifiers are included.
FAQs
1) Is the RE42376 compound scope dominated by a single claim?
Yes. Claim 1 provides the central Formula 1 genus; most other compound claims narrow subsets or restate constrained versions.
2) Does RE42376 include explicit compound examples in the claims?
Yes. Claim 5 lists many specific compounds (a to mmmm style), each claimed as “a compound of Claim 1” within the genus.
3) What indications does RE42376 cover?
It covers neoplasm treatment (Claim 6) with listed organ/indication categories (Claim 7) and polycystic kidney disease (Claim 8).
4) Are salts covered?
Yes. Multiple claims include “a pharmaceutically acceptable salt thereof.”
5) What structural features are most likely to drive infringement or non-infringement?
The controlling factors are the Het choice, and the Y/M/W linker system with k/p/q/g parameter provisos, plus the G1/G2 required radical class linkage in Claim 1.
References (APA)
- United States Reissue Patent RE42376, “A compound of Formula 1…” (claims as provided in the prompt).
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