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Patent landscape, scope, and claims: |
What is US Patent 8,362,002 and what does it claim?
US Patent 8,362,002 is written as a method-of-treatment patent that covers administration of a large formula I chemical class to treat a defined set of cancers and to inhibit MEK. The operative claim language is largely structural, with downstream narrowing in dependent claims to specific substituent combinations and then to enumerated exemplified compounds.
At the top of the hierarchy, claim 1 covers:
- A method of treating a disease where “treating” is defined as inhibiting the disease.
- The disease is selected from a cancer panel (melanoma, colorectal, pancreatic, breast, non-small cell lung, small cell lung, papillary and anaplastic thyroid, endometrial, ovarian).
- The method comprises administering a therapeutically effective amount of:
- a compound of formula I (including single stereoisomer or mixtures), optionally as a pharmaceutically acceptable salt, or
- a pharmaceutical composition containing that compound plus a pharmaceutically acceptable carrier/excipient/diluent.
- The core scope is then defined by broad substituent variable definitions across Groups A-D for A, X, R1-R7 (and nested definitions for R8, R9, R10, R12, etc.).
Claim 2 is a second independent method track that covers:
- “A method of inhibiting MEK” by administering the same formula I class.
The dependent claims (3-63) provide structured narrowing by:
1) limiting which “Group” applies (A is from Group A, B, C, or D),
2) constraining specific variable choices (examples: halo-only patterns, X halo, R7 halo, R1/R2/R5/R6 set to hydrogen),
3) carving out specific exemplified subsets (“selected from Group A where …”), and
4) listing many named specific compounds in claim 38 and then further narrowing by stereochemistry in claims 39-63.
Independent claim scope summary (structural and therapeutic)
| Claim |
Therapeutic target language |
Indicated disease / target |
Drug identity |
Claiming style |
| 1 |
Treating = inhibiting |
Cancer list (melanoma to ovarian, with thyroid subtypes) |
Formula I compound class (incl. stereoisomers) or salt; composition w/ carrier |
Broad class method + pharma composition |
| 2 |
Inhibiting |
MEK |
Same formula I class |
Broad class method focused on mechanism pathway |
How broad is “formula I” in claim 1?
The breadth is driven by three layers:
1) A variable scaffold (“A” plus defined aromatic/heteroaromatic groups)
Claim 1 defines A in one of Group A, Group B, Group C, or Group D.
- Group A: phenylene (optionally substituted with up to four substituents selected from R10, R12, R14, R16).
- Group B: heteroarylene (options include bicyclic/biaryl hetero frameworks; substitution defined by selected R10/R12/R14/R16/R19).
- Group C: group A defined where R10 is constrained to a different subset and introduces Y1 as either ═CH— or ═N—.
- Group D: group A is simplified further (R40/R40a hydrogen or alkyl), with limited X and variable R1-R6 constraints.
2) A massive substituent universe for R1-R6 and nested substituent variables
For many of the substituent variables, the claim allows:
- Atoms: hydrogen, halo, nitro
- Carbonyl / sulfonyl motifs: C(O)R8, C(O)OR8, C(O)NR8R8’, SO(m)R8, SO2NR8R8’, etc.
- “Heteroatom substituent” families including amines and multiple protected forms
- “Cycloalkyl/heteroaryl/aryl optionally substituted with 1-7 groups” using multiple substitution allowances (halo, alkyl, hydroxy, OR8, NR8R8’, cyano, carboxy derivatives, sulfone/sulfonamide families, etc.)
In other words: claim 1 does not claim a single compound. It claims an administration method for any compound that fits the defined chemical-variable constraints.
3) Stereochemistry inclusion
Claim 1 explicitly includes:
- single stereoisomer or mixture of stereoisomers.
This is relevant to designing around: many dependent claims then narrow to specific stereoisomeric exemplars, but the independent claims remain stereochemically inclusive.
What cancers and what target are covered?
Cancer list in claim 1
The disease is selected from:
- Melanoma
- Colorectal cancer
- Pancreatic cancer
- Breast cancer
- Non-small cell lung cancer
- Small cell lung cancer
- Papillary and anaplastic thyroid cancer
- Endometrial cancer
- Ovarian cancer
MEK inhibition in claim 2
Claim 2 is direct:
- Method of inhibiting MEK by administering the formula I class.
This makes the claim set useful both for indication claims (broad cancer panel) and mechanism claims (MEK inhibition).
Key dependent-claim narrowing routes (3-37, 38-63)
Dependent claims do three main things:
1) Select which “Group” defines A and constrain the remaining variables.
2) Hard-code “example-like” exemplars by listing specific compounds.
3) Refine stereochemistry and specific substituent selections.
Dependent claims 3 and 4: selected subsets
- Claim 3 narrows to compounds “selected from Group A, Group B, and Group C” and introduces narrower examples where:
- Group A includes phenylene with R10/R12/R14/R16 as hydrogen or halo (and X is halo), with R1/R2/R5/R6 fixed to hydrogen.
- Group B sets A to specific heteroarylene scaffolds (examples include thien-3,4-diyl; benzo[d]isoxazol-5,6-diyl; indazol-5,6-diyl; benzo[d]oxazol-5,6-diyl; benzo[d]imidazol-5,6-diyl; benzo[d][1,2,3]triazol-5,6-diyl; imidazo[1,2-c]pyridin-6,7-diyl; cinnolin-6,7-diyl; quinolin-6,7-diyl; pyridin-3,4-diyl; 1-oxido-pyridin-3,4-diyl; triazolo[4,3-a]pyridin-6,7-diyl; and 2,3-dihydroimidazo[1,2-a]pyridin-6,7-diyl).
- Claim 4 is broader than claim 3 in that it narrows R3 and R4 patterns but still relies on the definitions in claim 1.
Dependent claims 6-8: variable “single-parameter” hooks
These claims provide clean “engineering targets” for infringement analysis:
- Claim 6: R7 is halo
- Claim 7: X is halo
- Claim 8: R1, R2, R5, R6 are hydrogen
These can become “must-have” elements for a given claim path.
Dependent claims 12-17: Group A targeted patterns
Several claims focus on Group A phenylene variants and then restrict R3/R4:
- Claim 12: Group A where R10/R12/R14/R16 are hydrogen or halo and A is phenylene optionally substituted at up to two positions.
- Claims 13-17: constrain R3 and R4 to specific chemistry families like halo, alkoxy, hydroxy, and then further limit which substituent positions connect to heterocycles/aryl.
Dependent claims 18-19: specific halogenation pattern examples
- Claim 18: R7 is iodo or bromo, X is fluoro or chloro, and R1/R2/R5/R6 are hydrogen, while R10/R12/R14/R16 are hydrogen or fluoro.
- Claim 19: provides explicit examples of R10/R12/R14/R16 fluoro placements (e.g., “R10 is 3-fluoro and …”, “R10 is 4-fluoro and …”, etc.).
These claims help tie the chemical class to a specific fluoro pattern and halogen at R7.
Where the claim becomes “practically enumerated”: Claim 38
Claim 38 is the turning point: it lists a large set of specific named compounds as:
- “The method of claim 38 wherein the compound of formula I is selected from the group consisting of: …”
The list includes, among others:
- 1-({3,4-difluoro-2-[(2-fluoro-4-iodophenyl)amino]phenyl}carbonyl)azetidin-3-ol
- Several related azetidine-3-one and azetidine-3-ol analogs
- Multiple derivatives with various amine substituents, carbamates, carboxamides, sulfonamides, oximes, and protected moieties
- Numerous examples with stereochemical descriptors (R/S; cis/trans for cyclohexyl)
- Large numbers of alternative substituents on the azetidine nitrogen substituent position (piperidinyl, pyrrolidinyl, morpholinylmethyl, piperazinyl, triazolyl, imidazolyl, benzotriazolyl, cinnolinyl, etc.)
Claims 39-44 then tie claim 38 to additional named exemplars with explicit stereochemical or functional group identity:
- 39: compound named “1-({3,4-difluoro-2-[(2-fluoro-4-iodophenyl)amino]phenyl}carbonyl)-3-pyrrolidin-2-ylazetidin-3-ol”
- 40-41: same scaffold but with (R) or (S)
- 42-44: methanone analog with (R)/(S)
Then claims 45-51 similarly narrow by enumerated exemplars:
- 45: R3/R4 families specified with substituent
- 50-51: (±)-cis and (±)-trans cyclohexyl stereoisomers
Claims 52-57 extend enumeration across aminoethyl/pyrrolidinylmethyl and other substituent classes. Claims 58-63 continue in the same style (including salts as applicable in at least claim 59).
Patent landscape implications (what this claim posture means competitively)
1) The independent claims are mechanism-and-indication dual-use
- Claim 1 supports broad cancer-treatment infringement theories across a defined panel.
- Claim 2 supports additional MEK-inhibition infringement theories even if the payer/labeling argument is framed differently.
For enforcement or freedom-to-operate (FTO), this structure reduces the utility of a “we are not for that exact cancer” argument because the second independent claim is target-mechanism anchored.
2) The chemical scope is a class claim, not a single compound claim
The formula I definition plus Groups A-D plus large optional substituent options means:
- A competitor launching a MEK-inhibiting molecule with azetidine-centric chemistry and matching variable constraints could land inside the claim, even if it is not one of the enumerated exemplars.
3) Dependent claims create multiple “subsets” that can matter in litigation
Even if a defendant avoids the broadest formula I match, they can still end up within narrower dependent claim subsets if their lead compound matches:
- X halo and/or R7 halo,
- R1/R2/R5/R6 hydrogen,
- particular Group A patterns,
- or enumerated exemplars listed in claim 38.
4) The claim contains explicit scaffold recognition patterns
The enumerated list and the narrowing claims around fluoro/iodo/bromo patterns and azetidine-3-ol / azetidine-3-one / related motifs provide high-probability anchors for validity and infringement arguments based on:
- structural matching,
- stereochemistry,
- and substituent presence at defined positions.
Actionable “claim-to-portfolio” map for decision-making
A. What product attributes most strongly affect infringement risk
| Attribute bucket |
Claim language hook |
Why it matters |
| Target biology |
claim 2 MEK inhibition |
If a product is positioned as MEK inhibitor, claim 2 is directly relevant |
| Indication |
claim 1 cancer list |
Labeling or compendial use in those cancers supports claim 1 exposure |
| Core scaffold |
formula I A/X/R1-R7 in Groups A-D |
Class scope depends on matching the variable-defined chemical region |
| Halogen constraints |
dependent claims 6-8, 18-19 |
Halogen identity/placement can become “on/off” requirements |
| Stereochemistry |
independent includes single/mixed; dependent enumerates R/S and cis/trans |
Race to match the compound identity, not just gross formula class |
B. How to use the dependent claim ladder
For landscape and FTO work, the dependent claims act like:
- short-form “filters” (e.g., X halo; R7 halo; R1/R2/R5/R6 = H; Group A constraints)
- and then “final-form” exemplars in claim 38 and later.
If a candidate compound matches the chemical class, you then test whether it also matches one or more of these dependent claim filters that can tighten the enforcement path.
Key Takeaways
- US 8,362,002 is a method-of-treatment patent centered on administering a very broad formula I chemical class to treat a defined cancer panel and to inhibit MEK.
- Claim 1 covers cancer-treatment via “treating = inhibiting” and administers formula I (or salt / composition) to a patient with one of ten cancer indications.
- Claim 2 independently covers MEK inhibition using the same formula I administration approach.
- The chemical scope is governed by broad Groups A-D and extensive substituent variability across R1-R9 and nested substituent definitions, with explicit inclusion of stereoisomer mixtures.
- Dependent claims create multiple narrowing routes, culminating in claim 38, which enumerates many specific named azetidine-containing exemplars, followed by stereochemical and substituent-specific refinements in claims 39-63.
FAQs
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Is US 8,362,002 a composition-of-matter patent?
No. The claims are structured as methods of treatment and methods of inhibiting MEK with optional mention of pharmaceutical composition including carriers/excipients.
-
Does the patent cover both indication-based and mechanism-based use?
Yes. It has an indication-focused independent claim (cancer list in claim 1) and a mechanism-focused independent claim (MEK inhibition in claim 2).
-
How critical are stereochemistry issues in this patent?
Independent claim 1 includes single stereoisomer or mixtures. Dependent claims then narrow to specific stereochemical exemplars (claims 39-63), which are important for “exact compound” matching.
-
Does claim 38 matter if a compound does not match the broad formula I class?
Claim 38 matters only if the compound is already within the formula I class framework. It then helps by enumerating specific compounds that correspond to narrower dependent claim paths.
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What variables are most useful for quick infringement screening?
The strongest practical filters in the dependent set include X halo, R7 halo/iodo/bromo, and constraints like R1/R2/R5/R6 = hydrogen, plus Group selection for A.
References
[1] U.S. Patent No. 8,362,002.
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