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Patent landscape, scope, and claims: |
United States Patent 11,931,350: Scope, Claim Breadth, and US Patent Landscape
What does US Drug Patent 11,931,350 claim at the core?
US 11,931,350 is a chemical-composition patent centered on a broad “compound of formula” claim with nested structural variables (A2, A4, substituents B3/B4/B5 and D1) and a stereoisomer coverage. It is paired with downstream therapeutic method claims focused on pain and, separately, drug abuse. The claims you provided show three layers of claim scope:
1) Primary genus (Claim 1): one compound formula with multiple options for the key linkages and substitution points.
2) Alternate genera/formulas (Claims 10–11 and variants): additional formula recitations and overlapping substituent definitions.
3) Use patents (Claims 12–13, 17–19, 20): administration for pain and drug abuse.
4) Salt-form coverage (Claim 14–15, and implied in use claims): explicit pharmaceutically acceptable acid salts including a fumarate option.
Claim 1: Genus structure and variable definitions (as provided)
Claim 1 recites:
- “A compound, or a pharmaceutically acceptable salt thereof, having a formula of: or a stereoisomer thereof” with the following defining variable logic:
- A2 is one of: CH2, CHR5, CR5R6.
- A4 is one of: CH2, CHR9, CR9R10, or a cycle of the formula C(CH2)n where n = 2–5.
- Constraints tie A2 to A4/C substituents:
- If A4 is CH2, then CR5R6 is not C(CH3)2, C(CH3)CH2CH3, or CHCH2(CH3)2.
- If A2 is CH2, then CR9R10 is not C(CH3)2, C(CH3)CH2CH3, or CHCH2(CH3)2.
- R5, R6, R9, R10 each independently are selected from:
- CH3, CH2CH3, CH2F, CHF2, CF3, n-Pr, n-Bu, i-Bu, sec-Bu, i-Pr, t-Bu, phenyl.
- B3 is selected from:
- H, alkyl, branched alkyl, optionally substituted aryl, optionally substituted arylalkyl, alkoxycarbonyl, alkylsulfonyl.
- B4 is selected from:
- null, CH2, CHR19, CR19R20, CO.
- B5 is selected from:
- alkyl, branched alkyl, optionally substituted carbocycle, carbocycle-substituted alkyl, optionally substituted aryl, optionally substituted arylalkyl.
- D1 is:
- an optionally substituted heteroaryl.
Implication for breadth: Claim 1 is a “variable-rich” genus. The claim is not limited to a single scaffold; instead it spans multiple substitution regimes and structural options at A2 and A4, plus a wide enumerated substituent set at R5/R6/R9/R10 and broad categories for B3/B5 and heteroaryl D1.
Claim 2: substitution depth on heteroaryl/cycle
Claim 2 depends on Claim 1 and limits substitution on each heteroaryl group or cycle group by enumerating a large substitution set:
- F, Cl, Br, CH3, CH2CH3, CH2F, CHF2, CF3, n-Pr, n-Bu, i-Bu, sec-Bu, i-Pr, t-Bu, CN, OH, OMe, OEt, O-iPr, OCF3, methoxycarbonyl, methanesulfonyl, Ph, benzyl, formyl, acetyl.
This is not just “allowable substituents.” It is a positive list that controls what substitution patterns fall within dependent coverage.
Claims 5–7: key connectivity and ring-fusion limitations
- Claim 5: A2 and A4 are connected by a carbon bridge.
- Claim 6: the bridge is —CH2— or —CH2CH2—.
- Claim 7: “the ring containing A2, A4, and the carbon connected to D1 is fused with another ring” selected from:
- benzene, pyridine, pyrimidine, furan, thiophene, pyridazine.
These dependent claims carve out specific topological subclasses (bridge length and ring fusion), which matters for design-around and for determining which competitors might land inside or outside the genus.
Claims 8–9: multi-substitution permissiveness
- Claim 8: each aryl group can be multiply substituted from a large list (cyano, halogens, alkyls, hydroxyl, alkoxy, amino/aminoalkyl, mercaptans, sulfonyls, carbonyls, aryl/arylalkyl, cycle/cycle-alkyl).
- Claim 9: each cycle group has a similarly broad multiply-substituted allowance.
Claims 10–11: additional formula embodiments
Your text includes multiple formula recitations in Claims 10 and 11. The variable logic is similar to Claim 1, but the recited lists show modest differences in B4 and B5 category scope (for example, B5 lists “carbocycle” and “optionally substituted aryl” types, and B4 includes “null/CH2/CHR19/CR19R20/CO”). The practical result is that Claim 1, 10, and 11 overlap strongly, each acting as alternative genus anchors.
What therapeutic claims does the patent add?
Pain
- Claim 12: method of treating pain by administering a compound of Claim 1 (or salt).
- Claim 13: method of treating pain by administering a compound of Claim 11 (or salt).
- Claim 17: method of treating pain by administering a compound of Claim 14 (or salt).
- Claim 18: method of treating pain by administering a compound of Claim 15 (or salt).
- Claim 19: method of treating pain by administering a compound of Claim 16 (or salt).
These are classic “use” claims layered on the compound genus.
Drug abuse
- Claim 20: method of treating drug abuse by administering a compound of Claim 1 (or salt).
Implication for scope: the presence of both pain and drug abuse therapeutic use increases enforcement leverage across indications, but the compound scope remains the key driver. If a competitor avoids the compound genus, the method claims generally become irrelevant.
What salt forms are explicitly covered?
Claim 14: explicit acid list for pharmaceutically acceptable salts
Claim 14 enumerates an acid source list for forming pharmaceutically acceptable salts, including (non-exhaustive examples from your text):
- acetic, benzoic, fumaric, citric, tartaric, succinic, maleic, lactic, glycolic, oxalic, salicylic, ascorbic, phosphoric, hydrochloric, hydrobromic, sulfuric, nitric, pamoic, toluene sulfonic, benzene sulfonic, methane sulfonic, ethane sulfonic, and many others.
Claim 15: fumaric acid salt
- Claim 15 expressly targets: “The pharmaceutically acceptable salt is a fumaric acid salt.”
Implication for product targeting: any commercial or development material that is a fumarate salt has a direct claim hook.
How broad is the chemical space covered by the genus?
Even without the full structural diagram, the claim language creates a large combinatorial space:
Key degrees of freedom
- A2: 3 options (CH2, CHR5, CR5R6).
- A4: 4 options (CH2, CHR9, CR9R10, and C(CH2)n with n=2–5).
- R5/R6/R9/R10: each independently from a list of 11 substituents (CH3, CH2CH3, CH2F, CHF2, CF3, n-Pr, n-Bu, i-Bu, sec-Bu, i-Pr, t-Bu, phenyl).
- B3/B5: broad functional categories with “optionally substituted aryl/arylalkyl” and “optionally substituted carbocycle/aryl.”
- D1: “optionally substituted heteroaryl” (no explicit heteroaryl list in the excerpt, so the effective scope depends on how the specification defines “heteroaryl”).
- Aryl/cycle substitution: Claims 2, 8, 9 define a large enumerated substitution set including halogens, alkyls, nitrile, OH, alkoxy, sulfonyl/methanesulfonyl, formyl/acetyl, and carbonyl-containing groups.
Built-in exclusions reduce the space in specific corner cases
The claim contains narrow prohibitions when:
- A4 is CH2, then CR5R6 is not one of three substituted tert-butyl-like carbon options: C(CH3)2, C(CH3)CH2CH3, CHCH2(CH3)2.
- A2 is CH2, then CR9R10 is not one of the same three carbon options.
These exclusions are narrow and appear designed to carve out a small set of unwanted embodiments rather than eliminate broad competitors.
What is the patent landscape posture implied by these claim types?
Because the provided content is only the claims and not the complete application family (priority data, prosecution history, cited prior art, or specification-defined embodiments), the landscape can only be assessed at the claim-structure level. The patent posture implied by Claims 1–20 is:
1) Strong first-layer coverage: a compound genus with salts
This is a typical strategy to secure:
- broad coverage over structural variants through formula variables;
- continued enforcement over salt forms via explicit salt claims.
2) Secondary layer: dependent topology claims
Bridge length (CH2 vs CH2CH2) and ring fusion patterns (benzene/pyridine/pyrimidine/furan/thiophene/pyridazine) introduce narrower sub-genuses that can survive invalidity attacks aimed at the broadest genus features.
3) Use-layer claims for multiple therapeutic areas
Pain and drug abuse are covered. If enforcement targets a compound, the patentee can select the most robust indication claim depending on evidence and regulatory posture.
Claim-by-claim scope map (from your text)
| Claim |
Category |
What it covers (per provided text) |
| 1 |
Compound genus |
Formula-based compound or stereoisomer; A2/A4 variable atoms and substituents; broad B3/B4/B5 and optionally substituted heteroaryl D1; specific exclusions when A2 or A4 equals CH2. |
| 2 |
Dependent compound refinements |
Substitution list for heteroaryl and cycle groups (F/Cl/Br, alkyls, halogenated alkyls, CN, OH, OMe/OEt/O-iPr/OCF3, methoxycarbonyl, methanesulfonyl, Ph/benzyl, formyl, acetyl). |
| 5 |
Dependent compound topology |
A2 and A4 are connected by a carbon bridge. |
| 6 |
Dependent topology |
Bridge length is CH2 or CH2CH2. |
| 7 |
Dependent topology |
Ring fusion with benzene/pyridine/pyrimidine/furan/thiophene/pyridazine. |
| 8 |
Dependent aryl substitution |
Multiply substituted aryl scope using broad substituent list. |
| 9 |
Dependent cycle substitution |
Multiply substituted cycle scope using broad substituent list. |
| 10–11 |
Additional formula embodiments |
Compound formula variants anchored on similar A2/A4 and R5/R6/R9/R10 logic; B3/B4/B5 enumerations differ slightly. |
| 12–13 |
Use (pain) |
Administer compound of Claim 1 or Claim 11 (or salt) for pain. |
| 14 |
Salt forms |
Pharmaceutically acceptable acid salt formed from an enumerated acid list (includes fumaric acid). |
| 15 |
Salt forms |
Fumaric acid salt. |
| 17–19 |
Use (pain, via salt variants) |
Pain treatment using salts tied to Claims 14–16 as recited. |
| 20 |
Use (drug abuse) |
Administer compound of Claim 1 (or salt) for drug abuse. |
Design-around and freedom-to-operate signals embedded in the language
Likely “hot spots” for infringement risk
- Hitting A2/A4: Changing either A2 or A4 outside the enumerated options or outside the ring/cycle rule likely moves the compound outside the genus.
- Avoiding the CH2 corner exclusions: The claim excludes specific carbon substitutions only when A2 or A4 is CH2. If competitors use those excluded substituents, they may fall outside the genus; if they avoid them, risk persists.
- Maintaining B4/B5 categories: B4 is sensitive (null, CH2, CHR19, CR19R20, CO). B5 includes carbocycles and arylalkyl options. A competitor can reduce risk by changing these groups into structurally disjoint categories not captured by the lists.
- Salt selection: If a compound is within the genus, salt selection can be a carve-out lever unless the salt is still within the “pharmaceutically acceptable salt” umbrella. Claim 15 makes fumarate a direct target.
Potential “rescue” during validity challenges
- Even if a broadest genus is attacked, dependent claims with specific topology (bridge length and fused rings) can provide fallback claim sets, particularly if the specification supports those substructures.
Key Takeaways
- US 11,931,350 is a high-breadth compound-genus patent built on a formula with multiple structural variables (A2, A4, R5/R6/R9/R10, B3/B4/B5, and optionally substituted heteroaryl D1) plus stereoisomer coverage.
- The claim includes explicit substitution lists for heteroaryl and cycles (Claim 2) and broad multiply-substituted aryl/cycle allowances (Claims 8–9).
- Topology-dependent hooks exist via carbon bridge length (Claims 5–6) and ring fusion patterns (Claim 7), which create narrower sub-genuses inside the broader formula.
- Therapeutic claims cover pain and drug abuse, giving the patent enforcement optionality across indications.
- Salt coverage is explicit, with a broad enumerated acid list (Claim 14) and direct fumaric acid salt coverage (Claim 15).
FAQs
1) Does the patent cover stereoisomers?
Yes. Claim 1 expressly includes “a stereoisomer thereof.”
2) Is fumarate specifically claimed?
Yes. Claim 15 specifically recites a fumaric acid salt.
3) What therapeutic areas are claimed?
Pain (Claims 12–13, 17–19) and drug abuse (Claim 20).
4) Are bridge and ring fusion required for all coverage?
No. Bridge (Claims 5–6) and fused ring topology (Claim 7) are dependent claims that refine Claim 1 scope.
5) How does the claim limit certain carbon substitutions?
It excludes specific carbon options (C(CH3)2, C(CH3)CH2CH3, CHCH2(CH3)2) only under conditions where A4 is CH2 or where A2 is CH2, respectively.
References
[1] United States Patent Application/Patent Claims Provided by User: US Drug Patent 11,931,350 (Claims 1–20 excerpts as supplied).
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