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Patent landscape, scope, and claims: |
United States Patent 8,242,104: What Is Actually Claimed?
US drug patent 8,242,104 has an unusually broad chemistry “umbrella” claim set: claim 1 recites a huge Markush-style genus of substituted hetero-fused bicyclic/oxazepine-containing compounds defined by four ring position variables Z1-Z4, a core substituent A, and multiple independent substituent sets (R1-R4, R10-R12, R5-R6, R9, R13). The remaining dependent claims then carve out smaller sub-genuses and numerous specific named examples.
The practical upshot for a freedom-to-operate (FTO) or landscape strategy is that the enforceable scope is defined less by the explicit named compounds and more by the claim-1 structural definitions that can read on many future analogs.
What Is the Claim-1 Scope? (The “Genus” Boundary Conditions)
Claim 1: Genus of compounds
Claim 1 is a compound claim covering:
- A compound selected from:
- stereoisomers
- geometric isomers
- tautomers
- and pharmaceutically acceptable salts
- where the core is defined by:
- Z1-Z4, each chosen from CRx or N
- R1-R4 substituted on those four positions
- A chosen from a set of carbonyl-amide or heteroaryl/aryl/carbocycle groups with optional substitution
- additional substituent variables R10, R11, R12, R5, R6, R9, R13 each allowed broad lists with optional substitutions
In other words, claim 1 is not limited to a single scaffold. It is limited to a scaffold class (via the way Z1-Z4 and A must fit the formula framework) but allows heavy substitution on most exposed handles.
Core positional variables
- Z1 is CR1 or N
- Z2 is CR2 or N
- Z3 is CR3 or N
- Z4 is CR4 or N
This means the patent covers cases where each of the four positions can be carbon or nitrogen, generating a lattice of possible heteroatom incorporation patterns.
Substituent variables R1-R4
R1-R4 are independently selected from a broad set including:
- halogens (F, Cl, Br, I)
- cyano (—CN) and nitro (—NO2)
- simple hydrogen
- and a large set of functional groups including multiple carbonyl/heteroatom-rich options such as:
- —COR10, —CO2R10
- amide-like and urea-like motifs (—C(═O)NR10R11, etc.)
- sulfonamides/sulfones (—S(O)2R10, —S(O)2NR10R11)
- multi-ring substituents (alkyl/alkenyl/alkynyl/carbocyclyl/heterocyclyl/aryl/heteroaryl), each optionally substituted with a similar halogen/oxo/cyano/CO2H/R10 group set
So the claim is structurally flexible enough that many “drug-like” substituents fit, not just a small pharmacophore substitution pattern.
A substituent group
“A” is selected from:
- —C(═O)NR5R6
- —NR5R6
- C6-C20 aryl
- C2-C20 heterocyclyl
- C1-C20 heteroaryl
and each aryl/heteroaryl/heterocycle is optionally substituted by a large list that mirrors the R-group substituent dictionary.
This matters because A functions like a plug-in tail. A competitor can potentially design around by changing A, but must do so to avoid falling inside the enumerated A class definitions.
R5-R6 constraints
- R5 = H or C1-C12 alkyl optionally substituted with a defined set (F, halogens, cyano, CO2H, amides, nitro, NH2 etc.)
- R6 = C1-C12 alkyl or larger ring systems:
- carbocyclic/heterocyclic/aryl
- each optionally substituted with a similarly large set (e.g., CF3, CO2H, anilide-like substituents, etc.)
The dependencies later narrow R5-R6 options to specific representatives.
R10-R12 and cyclic formation options
- R10, R11, R12 each are independently selected from a large set of H and substituted alkyl/ring systems
- with an additional option that R10 and R11 together can form a C2-C20 heterocyclyl ring or C1-C20 heteroaryl, optionally substituted
This is a typical Markush strategy to cover dialkyl amines and ring-closed heterocycles without listing each ring variant separately.
R13
- R13 is selected from H and multiple substituted substituents (F/Cl/Br/I, methyl/ethyl/cyano/CF3, CH2N(CH3)2, alcohols, carboxylic acids, amides, nitro, S(O)2CH3)
R13 appears tied to certain “alkenyl/alkynyl-like” or “vinyl” substituent handles in the earlier part of claim 1’s R1-R4 list.
How Narrow Do the Dependent Claims Go? (Key Sub-Genus Hooks)
Z1-Z4-specific dependent claims
These claims lock in heteroatom patterns at the four Z positions:
- Claim 2: Z1=CR1; Z2=CR2; Z3=CR3; Z4=CR4
- Claim 3: Z1=N; Z2=CR2; Z3=CR3; Z4=CR4
- Claim 4: Z1=CR1; Z2=N; Z3=CR3; Z4=CR4
- Claim 5: Z1=CR1; Z2=CR2; Z3=N; Z4=CR4
- Claim 6: Z1=CR1; Z2=CR2; Z3=CR3; Z4=N
- Claim 7: restricts R1-R4 to a small set (H, F, Cl, Br, I, CN, NO2, C1-C6 alkyl)
This is not a full “design-around” map because claim 1 already spans these, but the dependencies signal which regions the applicant viewed as commercially relevant.
Functional reduction of R2-R3 choices
-
Claim 8: R2 and R3 are independently selected from:
- —NR10R11
- —(C(═O)NR10R11)
- and —(C1-C12 alkylene)C(═O)NR10R11
-
Claim 9: R2 and R3 independently selected from optionally substituted:
- C3-C12 carbocyclyl
- C2-C20 heterocyclyl
- C6-C20 aryl
- C1-C20 heteroaryl
-
Claim 10 narrows further to named ring examples (e.g., azabicyclo[3.2.1]octanyl, azetidinyl, cyclopropyl, imidazolyl, morpholinyl, piperazinyl, piperidinyl, pyrazinyl, tetrahydropyridinyl, etc.)
-
Claim 11: R2 and R3 = —OR10
-
Claim 12: R2=—OR10 and Z3=N
These dependencies are practical when analyzing whether a specific competitor molecule uses the same heteroatom pattern and substituent handle families.
A group narrowing
-
Claim 13: A = —C(═O)NR5R6
-
Claim 14: R5=CH3
-
Claim 15: R6 = phenyl substituted with defined allowed substituents
-
Claim 16: R5 and R6 together form a morpholinyl/piperidinyl/piperazinyl/etc. heterocycle
-
Claim 17: A is heterocyclyl/heteroaryl substituted with a long list of specific substituents like:
- CH2OH, CH2CO2H, CH(CH3)2OCH3, CH3, CH(CH3)2, CH2CF3, C(═O)CH3, amide-like handles, OH, OCH3, sulfone-like motifs, and ring-specific substituents
-
Claim 18: A is a named list of heteroaryl rings (pyridyl, isoxazolyl, imidazolyl, pyrazolyl, thiazolyl, pyridazinyl, pyrimidinyl, pyrazinyl, oxazolyl, oxadiazolyl, 1,3,4-oxadiazol-2-one, furanyl, thienyl, triazoles, etc., plus benzo[d]thiazole)
-
Claim 19-22: introduce additional named structural A selections and R9 substituent definitions (including a “structures” list and multiple specific R9 options)
Example-providing dependent claims (Claims 23-25)
Claim 23 and Claim 24 contain extensive named compounds (hundreds of examples) built off the structural framework. This does not narrow the scope by itself (since they are dependent), but it provides strong evidence that the genus was intended to cover many specific analogs.
Claim 26-28 then cover:
- pharmaceutical composition (claim 26)
- optional additional therapeutic agents (claim 27)
- process (claim 28)
- kit for breast cancer treatment (claim 29)
Claim 30-33 define specific individual compounds.
What Does This Mean for the Patent Landscape? (Scope Signals, Not Just Examples)
Even without knowing the applicant/assignee or expiration status, claim structure yields a consistent landscape interpretation:
1) “One patent, many future analogs”
Because claim 1 allows:
- Z1-Z4 carbon/nitrogen variations
- wide R1-R4 functional diversity
- and multiple A and R-group handle families
it is positioned to block multiple rounds of analog generation unless competitors materially change:
- the core scaffold identity that is implicitly enforced by the formula framework, or
- the substitution class so that it falls outside at least one required structural definition.
2) The enforceability risk is concentrated at the “A” and “Z-pattern” boundary
Most FTO disputes in Markush chemical patents turn on:
- whether a competitor structure still qualifies under the defined formula (Z-variables)
- whether the tail group “A” matches one of the enumerated options (carbonyl-amide tail vs aryl/heteroaryl vs heterocycle)
Here, claim 1’s A clause is broad enough that many common substituents could qualify.
3) Salt/stereoisomer/tautomer language removes common design escapes
Many product changes occur via:
- different salt forms
- different stereoisomers
- tautomeric variants
Claim 1 explicitly includes these categories.
Claim Set Mapping: Which Clauses Control Which Design Decisions
| Design lever |
Claim language controlling it |
Resulting practical coverage |
| Heteroatom pattern in ring core |
Z1-Z4 defined as CRx or N |
Covers multiple core nitrogen insertion patterns within the same formula framework |
| Size/identity of substituents |
R1-R4 independently selected from broad functional and ring families |
Covers most “medchem-like” substitutions in the allowed dictionary |
| Tail group attachment |
A selected from —C(═O)NR5R6, —NR5R6, aryl/heteroaryl/heterocycle |
Enables large chemotype tolerance for the substituent at A |
| Amide/amine substituent detail |
R5-R6 and ring-forming rules |
Covers many dialkyl/heterocyclic amides and related substituents |
| Substituent functional groups on rings |
optional substitution lists for many ring classes |
Makes “ring functionalization” an included dimension |
| Salt/stereoisomer/tautomer variants |
explicit inclusion |
Blocks common product-line diversification strategies |
Key Takeaways
- US 8,242,104 is a broad chemical-genus patent anchored by claim 1’s Markush definitions of Z1-Z4, R1-R4, and A, and it explicitly includes stereoisomers, geometric isomers, tautomers, and salts.
- Dependent claims further signal the relevant sub-genuses using specific Z patterns and constraining R selections (notably R2-R3 classes and A=—C(═O)NR5R6 type tails).
- Landscape impact is driven by the claim-1 “formula boundary” and the inclusive A definition, not by the large list of named examples.
- The patent also extends to pharmaceutical compositions, processes, and kits for breast cancer, and includes optional combinations with other therapeutic agent categories.
FAQs
1) Does US 8,242,104 primarily protect individual molecules or a chemical class?
It protects a chemical class/genus in claim 1 via Markush-style definitions, with dependent claims and numerous examples illustrating covered compounds.
2) What is the most important structural feature to analyze for FTO?
The claim-1 structural constraints tied to Z1-Z4 and the A group selection, since these govern whether a competitor structure fits the defined formula.
3) Are stereoisomers and salts covered?
Yes. Claim 1 explicitly covers stereoisomers, geometric isomers, tautomers, and pharmaceutically acceptable salts.
4) Do the named compounds in dependent claims limit the patent’s coverage?
No. Dependent examples do not narrow claim 1; they provide evidence of what the genus was designed to include. Scope is governed by claim 1.
5) Does the patent extend beyond compounds to formulations and treatment kits?
Yes. It includes claims to pharmaceutical compositions, processes, and a kit for therapeutic treatment of breast cancer.
References
[1] US Patent 8,242,104. (n.d.). United States Patent and Trademark Office (USPTO) patent document.
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