Scope, Claims, and U.S. Patent Landscape for US Drug Patent 7,417,148 (CML; quinolinecarbonitrile compounds)
US 7,417,148 is a method-of-use patent for chronic myeloid leukemia (CML) that claims dosing of substituted quinolinecarbonitrile compounds defined by a shared structural formula and explicit substituent constraints, plus dependent claim coverage of specific exemplified members and combination treatment with imatinib. The enforcement footprint is driven by (i) the breadth of the Markush-style substituent definitions in independent claim 1 and (ii) the dependent claims that “lock in” particular stereochemical/structural embodiments via listed chemical names.
What is the claim architecture and what does it practically cover?
Independent claim 1 (core scope)
Claim 1 recites a method of treating or inhibiting proliferation of CML by administering a therapeutically effective amount of a compound “of the formula” where key variables are constrained as follows:
- Ring/substitution variables
- n is an integer 1 to 3
- X is N or CH
- If X = N, then n = 2 or 3
- Aniline-derived substituent
- R is alkyl with 1 to 3 carbons
- Aniline/aryl substitution pattern at R1
- R1 is one of the following (as written in the claim text):
- 2,4-diCl, 5-OMe
- 2,4-diCl
- 3,4,5-tri-OMe
- 2-Cl, 5-OMe
- 2-Me, 5-OMe
- 2,4-di-Me
- 2,4-diMe-5-OMe
- 2,4-diCl, 5-OEt
- Terminal alkyl at R2
- R2 is alkyl 1 to 2 carbons
- Also included: pharmaceutically acceptable salts
Enforcement interpretation: The claim is broad in the way it defines a scaffold and permits multiple substituent classes via enumerated R1 and bounded alkyl ranges for R and R2. The “switch” restriction for X = N limits which n values can occur, which matters for design-around and for claim chart mapping.
Dependent claims 2–6 (sub-breadths and narrowing knobs)
- Claim 2 restricts:
- n = 2 to 3
- same X and R constraints and same R1/R2 enumerations
- Claim 3 further restricts to a specific parameterization:
- X = N or CH with “where X is N n is 3” (as written, it reads as a fixed combination)
- R2 and R are methyl
- Claim 4 restricts:
- Claim 5 restricts:
- Claim 6 restricts:
Practical meaning: these are classic dependent narrowing claims that create additional target sets for infringement where a candidate falls into one of these subgroups.
Dependent claims 7–9 (explicit chemical embodiments)
- Claim 7 lists a specific compound:
- 4-[(2,4-Dichloro-5-methoxyphenyl)amino]-6-methoxy-7-[3-(4-methyl-1-piperazinyl)propoxy]-3-quinolinecarbonitrile
- Claim 8 lists a panel of compounds, each built on the same quinolinecarbonitrile core with variations in:
- methoxy vs ethoxy at the ring position
- the propoxy/ethoxy linker length and attachment point
- piperazine substituent position and N-substitution (methyl/ethyl) versus piperidinyl analogs
- Claim 9 lists a second panel of named compounds, again with fixed combinations:
- ring methoxy/methoxy patterns
- aniline substitution variants (diCl, chloro-methoxy, di-methyl, tri-methoxy patterns)
- piperidinyl side-chain with a methyl substituent
Practical meaning: these dependent claims reduce ambiguity. If a competitor product matches any of the listed compounds (or a covered salt), it can fall directly into a narrower but cleaner claim pathway.
Dependent claims 10–12 (functional target and combination therapy)
- Claim 10: “The method of claim 1 wherein the compound is a Src inhibitor and a Abl Kinase inhibitor.”
- This is a functional-activity limitation. It can be used to argue that the administered compound has both kinase inhibition profiles.
- Claim 11: Allows administration alone or in combination with other compounds used to treat CML.
- Claim 12 (specific combination):
- Combination with imatinib:
- (Imatinib) 4-[(4-methyl-1piperazinyl)methyl]-N-[4-methyl-3-[[4-(3-pyridinyl)-2pyrimidinyl]amino]phenyl]-Benzamide
Practical meaning: Claim 12 gives a direct hook for infringement in regimens that co-administer imatinib with one of the claimed scaffold members (or salts), provided the other method-of-treatment elements are met.
What is the effective chemical “design space” inside the scaffold?
The independent claim defines a quinolinecarbonitrile substitution family with constrained substituents. The scope is anchored by the enumerated options:
Substituent constraints by variable
| Variable |
Options (as claimed) |
Scope effect |
| n |
1 to 3; but if X = N, then n = 2 or 3 |
Limits which core nitrogen state aligns with given ring substitution |
| X |
N or CH |
Two alternative core hetero/atom definitions |
| R |
alkyl C1 to C3 |
Broad enough for methyl, ethyl, propyl; narrows core aryl substituent class |
| R1 |
Enumerated aryl patterns including diCl, di-methyl, tri-OMe, and mixed diCl/alkoxy |
Dominant determinant of whether a candidate hits claim 1 |
| R2 |
alkyl C1 to C2 |
Likely methyl or ethyl for the linker/side-chain terminal group |
| Salts |
pharmaceutically acceptable salts |
Extends coverage to salt forms |
How the R1 enumeration drives breadth
Because R1 is not a general “substituted” definition but a list, the set of covered aryl substitution patterns is comparatively controlled. For landscape and clearance, mapping candidate structures to only the enumerated R1 values is the high-yield step.
Which specific molecules are explicitly covered (claims 7–9)?
Claim 7
- 4-[(2,4-Dichloro-5-methoxyphenyl)amino]-6-methoxy-7-[3-(4-methyl-1-piperazinyl)propoxy]-3-quinolinecarbonitrile
Claim 8 (panel)
Each is a quinolinecarbonitrile with a 2,4-dichloro-5-methoxy anilide and different substitution patterns. Examples from the claim list include:
- 4-[(2,4-Dichloro-5-methoxyphenyl)amino]-7-[3-(4-ethyl-1-piperazinyl)propoxy]-6-methoxy-3-quinolinecarbonitrile
- 4-[(2,4-Dichloro-5-methoxyphenyl)amino]-6-methoxy-7-[2-(4-methyl-1-piperazinyl)ethoxy]-3-quinolinecarbonitrile
- 4-[(2,4-Dichloro-5-methoxyphenyl)amino]-6-methoxy-7-[2-(4-ethyl-1-piperazinyl)ethoxy]-3-quinolinecarbonitrile
- 4-[(2,4-Dichloro-5-methoxyphenyl)amino]-6-methoxy-7-[(1-methylpiperidin-4-yl)methoxy]-3-quinolinecarbonitrile
- 4-[(2,4-Dichloro-5-methoxyphenyl)amino]-6-methoxy-7-[2-(1-methylpiperidin-4-yl)ethoxy]-3-quinolinecarbonitrile
- 4-[(2,4-Dichloro-5-methoxyphenyl)amino]-7-[3-(1-methylpiperidin-4-yl)propoxy]-6-methoxyquinoline-3-carbonitrile
- 4-[(2,4-Dichloro-5-methoxyphenyl)amino]-6-ethoxy-7-[3-(4-methylpiperazin-1-yl)propoxy]quinoline-3-carbonitrile
- 4-[(2,4-Dichloro-5-methoxyphenyl)amino]-6-ethoxy-7-[3-(1-methylpiperidin-4-yl)propoxy]quinoline-3-carbonitrile
- ...and additional members listed in the claim
Claim 9 (panel)
This claim lists additional explicit structures including substitutions on the aniline ring such as diCl, chloro-methoxy, dimethyl, and diCl-ethoxy variants. Examples from the claim list include:
- 4-[(2,4-dichlorophenyl)amino]-6-methoxy-7-[(1-methylpiperidin-4-yl)methoxy]-3-quinolinecarbonitrile
- 6-methoxy-7-[(1-methylpiperidin-4-yl)methoxy]-4-[(3,4,5-trimethoxyphenyl)amino]quinoline-3-carbonitrile
- 4-[(2-chloro-5-methoxyphenyl)amino]-6-methoxy-7-[(1-methylpiperidin-4-yl)methoxy]quinoline-3-carbonitrile
- 6-methoxy-4-[(5-methoxy-2-methylphenyl)amino]-7-[(1-methylpiperidin-4-yl)methoxy]quinoline-3-carbonitrile
- 4-[(2,4-dimethylphenyl)amino]-6-methoxy-7-[(1-methylpiperidin-4-yl)methoxy]quinoline-3-carbonitrile
- ...and additional members listed in the claim
Landscape value: these lists show which exact structural “variants” were contemplated as embodiments of the Markush formula. For freedom-to-operate, they are the fastest route to identify whether any competitor compound matches a named claim member.
How does the patent likely function in the broader CML kinase inhibitor landscape?
Method-of-use posture
US 7,417,148 is written to cover treatment or proliferation inhibition in CML through administration of a defined compound family. That means:
- A structural match is not sufficient by itself for infringement; the claimed method element also requires treatment of CML (or inhibiting proliferation in CML) using a therapeutically effective amount.
- Dependent claim 12 increases risk where dosing includes imatinib, because it ties the method to a recognized CML standard-of-care anchor.
Claim 10 functional tie to Src and Abl
Claim 10 adds a functional requirement: the compound is both a Src inhibitor and an Abl kinase inhibitor. In portfolio terms, this is the claim language most likely to be attacked and most likely to become a key evidentiary pivot point if a compound is close in structure but differs in kinase profile.
Combination strategy risk (Claim 12)
Any regimen that includes:
- one of the claimed compounds (or salts) used for CML treatment, and
- imatinib co-administration (as specified in claim 12),
creates a direct collision risk for combination-development programs and label-expansion studies.
Scope summary: what is covered vs. what is limited?
Covered
- CML treatment/proliferation inhibition by administering therapeutically effective amounts of:
- the general quinolinecarbonitrile scaffold under the enumerated variable definitions in claim 1
- enumerated R1 aryl substitution patterns
- alkyl constraints on R and R2
- pharmaceutically acceptable salts
- subgroups defined by n/X/R/R2 constraints in dependent claims
- explicitly listed compounds in claims 7–9
- regimens including imatinib when using covered compounds (claim 12)
Limited
- R1 is enumerated, not open-ended, which restricts which aryl substitution patterns are within claim 1.
- X and n have a coupled constraint when X = N.
- Claim 10 adds functional dual kinase inhibition requirement (Src and Abl), constraining coverage in practice for compounds with partial activity profiles.
- Combination coverage depends on co-administration with imatinib as recited in the dependent claim.
Patent landscape: what other U.S. rights would matter operationally?
No other specific patents or prosecution/continuation documents are provided in the prompt, and no bibliographic details (filing date, assignee, priority, expiration/term, prosecution history, or cited references) are included for US 7,417,148. With only the claim text, the landscape can be characterized only by claim-driven risk interactions, not by citing other specific documents.
From a business and R&D prioritization perspective, the relevant landscape questions for this family are:
- Structural overlap vs. Markush constraints
- Candidates that modify aryl substitution beyond the enumerated R1 options are likely to fall outside independent claim 1, unless doctrine of equivalents arguments succeed.
- Named-member overlap
- If a development compound matches one of the named compounds in claims 7–9, the probability of coverage is higher because claim mapping becomes deterministic.
- Combination development with imatinib
- Combination studies that include imatinib are exposed to claim 12 risk if the investigational compound falls into claim 1’s scaffold and meets CML treatment method elements.
Key Takeaways
- US 7,417,148 claims CML treatment/proliferation inhibition by administering a substituted quinolinecarbonitrile scaffold with enumerated substituent constraints (notably R1).
- Independent claim 1 is broad on n (1 to 3), includes X = N or CH, and permits alkyl ranges for R (C1 to C3) and R2 (C1 to C2), but R1 is constrained to a defined list of aryl substitution patterns.
- Dependent claims 7–9 enumerate multiple specific compounds, making exact matches high-risk.
- Claim 12 creates an explicit collision point for imatinib combination regimens when the administered compound falls within claim 1 and the method-of-treatment element is met.
- Claim 10 adds a functional dual-activity condition (Src inhibitor + Abl kinase inhibitor) that becomes critical for compounds that are structurally similar but biologically differentiated.
FAQs
1) Is US 7,417,148 a compound patent or a method-of-use patent?
It is a method-of-use patent. Claim 1 covers treatment or inhibition of CML proliferation by administering therapeutically effective amounts of specified compounds.
2) What variable most controls whether a candidate structure falls within claim 1?
R1, because it is defined as an explicit set of aryl substitution patterns rather than a broad general substituent category.
3) Do claims 7–9 add coverage beyond the Markush formula?
They add certainty by listing specific chemical embodiments that fall within the broader scaffold, creating direct target sets for infringement analysis.
4) Does the patent cover combination therapy with imatinib?
Yes. Claim 12 expressly recites combinations with imatinib.
5) Can a compound with partial kinase activity still fall under the claims?
For claim 10, no. It requires the compound to be both a Src inhibitor and an Abl kinase inhibitor.
References
- US Patent 7,417,148, claims (as provided in the prompt).
