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Patent landscape, scope, and claims: |
United States Patent 7,253,286: Scope, Claim Structure, and US Patent Landscape
What is the claimed invention in US 7,253,286?
US 7,253,286 claims a broad class of small-molecule compounds defined by a highly substituted, multi-ring framework with specific linker and terminal substituent variables, plus exclusion carve-outs and then dependent narrowing to particular substituent sets and named exemplars. The claims also extend to pharmaceutical compositions and to specific single-compound formulas.
Core claim architecture:
- Independent claim (claim 1): “A compound represented by the following general formula” with variables R1/R2, Z12, a substituent fragment Ya1, a group fragment Ra11, and a terminal group Ra12, subject to explicit exclusions (compounds (1) and (2)).
- Dependent claims (2-8): narrow substituent choices (salt/hydrate limited, and specific allowed values for parts of the structure).
- Process-free composition claims (9-10): pharmaceutical composition with carrier, and composition “effective to inhibit angiogenesis.”
- Single-compound claims (11-15): specific embodiments with fixed substituent patterns (quinoline-based scaffold, methoxy and quinoline carboxamide motif, and a specified anilide/urea/carbonyl substitution on a phenoxy ring).
The claim language you provided indicates a structure-driven chemistry patent rather than a method-of-treatment patent. “Inhibit angiogenesis” appears in a composition-use context (claim 10).
How broad is claim 1, and what are the main scope levers?
Claim 1 is the scope driver. It uses:
- General formula coverage through variable sets R1, R2, Z12, Ra11, Ya1, Ra12.
- Substitution permissiveness: many options are “optionally substituted” with ranges like C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, C3-8 alicyclic, C6-14 aryl, 5-14 heterocycles, etc.
- Linker topology: Ra11 is defined through Va21-Va22-Va23 with enumerated bond types and heteroatom/carbonyl/sulfonyl-like bridges.
- Terminal group constraints: Ra12 is specifically cyano or a defined carbonyl/amide-like variant (formula includes Va11 = CO or SO2 and Va12/Va13/Va14 substituent freedoms).
Main variable sets in claim 1
Below is a structured extraction of the scope levers you supplied (based only on the claim text).
R1 and R2
- Allowed independently: H, optionally substituted C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, C3-8 alicyclic hydrocarbon, C2-7 acyl, or C2-7 alkoxycarbonyl.
Z12
- Allowed: H, optionally substituted C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, C3-8 alicyclic hydrocarbon, optionally substituted C6-14 aryl, optionally substituted 5-14 membered heterocycle, optionally substituted 5-14 membered aromatic heterocycle, or a defined poly-atom group (your text provides a group represented by a formula with Z31/Z32/Z33/Z34-like substructure).
- Negative limitation: “Z12 is not pyrazolyl.”
Ya1
- A group defined by a fragment with W31 and W32 each independently an optionally substituted carbon or nitrogen atom, and with substituent-bearing parameters R300/R301 and a nested substituent definition (your text includes a second formula with V300/V301).
Ra11
- A chained fragment: Ra11 is a group represented by Ra11 = —Va21—Va22—Va23:
- Va21: optionally substituted C1-6 alkylene, a single bond, or another defined group.
- Va22: bond or heteroatom/carbonyl/sulfonyl-like moieties including O, S, CO, SO, SO2, CONRa14, SO2NRa14, NR a14 SO2, NR a14 CO, NRa14.
- Ra14: H, optionally substituted C1-6 alkyl, or optionally substituted C3-8 alicyclic.
- Va23: H, optionally substituted C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, C3-8 alicyclic, C6-14 aryl, 5-14 heterocycle or 5-14 aromatic heterocycle.
Ra12
- Allowed: cyano or a defined carbonyl/amide or sulfone-like group (your text shows “group represented by the formula wherein Va11 is —CO— or —SO2—; and Va12, Va13, Va14 … optional substituents”).
What exclusions narrow claim 1?
Claim 1 contains two explicit exclusion carve-outs.
Exception (1)
- Ra12 equals a defined group (shown in your text) with:
- Va12 and Va13 independently H or optional substituents as broadly defined,
- R1 = H and R2 = H,
- Z12 = C6-14 aryl, 6-14 heterocycle, or 6-14 aromatic heterocycle.
Exception (2)
- Ra12 equals one of formulae (your text references a selection set) with:
- Va11 = CO or SO2,
- Va12/Va13/Va14 independently as broadly defined substituents,
- R2 = H,
- Z12 constrained to one of:
- (a) C6-14 aryl; (b) 5-14 heterocycle; (c) 5-14 aromatic heterocycle; (d) C1-6 alkyl substituted with a 5-10 heterocycle or a C5-10 alicyclic; (e) C2-6 alkenyl substituted with 5-10 heterocycle or C5-10 alicyclic; (f) C2-6 alkynyl substituted similarly; (g) C3-8 alicyclic substituted similarly.
These exceptions matter because they can remove specific “anchor” combinations from the otherwise wide variables. Practically, they are where designing around the patent becomes plausible: keep the scaffold but shift the variable combinations that fall into (1) or (2).
How do dependent claims narrow the variable space?
Dependent claims 2-8 tighten specific variable selections in ways that align with the “named compounds” you provided in the claim set.
Claim 2
- Adds “pharmacologically acceptable salt or hydrate.”
- Sets Ra11 options:
- methyl
- 2-methoxyethyl
- or a defined group formula where:
- Ra53 = methyl, cyclopropylmethyl, or cyanomethyl
- Ra51 = H, fluorine, or hydroxyl
- Ra52 = 1-pyrrolidinyl, 1-piperidinyl, 4-morpholinyl, dimethylamino, or diethylamino
Claim 3
- Salt/hydrate.
- Constrains Z12 to one of:
- methyl, ethyl, cyclopropyl, 2-thiazolyl, or 4-fluorophenyl.
Claim 4
- Salt/hydrate.
- Constrains Ya1 to a formula with Ra61 ∈ {H, methyl, trifluoromethyl, chlorine, fluorine}.
Claim 5
- Salt/hydrate.
- Constrains Ra12 to:
- cyano, or
- a defined form —CONHRa62 where Ra62 ∈ {H, optionally substituted C1-6 alkyl, optionally substituted C3-8 alicyclic hydrocarbon, optionally substituted C1-6 alkoxy, optionally substituted C3-8 cycloalkoxy}.
Claims 6-8: enumeration of specific exemplars
Claims 6-8 list specific compounds (large enumerations) as compliant selections under claim 1. This is strong evidence that the patent family aimed at a finite set of exemplified chemical targets, even if claim 1 is broad.
What are the practical “focus compounds” explicitly claimed as single formulas?
Claims 11-15 each claim a fixed compound structure (or salt/hydrate). The repeated core motif is consistent:
- 4-(3-chloro-4-(substituted amino/carbonyl)aminophenoxy)-7-methoxy-6-quinolinecarboxamide
- Alternation of the phenyl-side carbonyl/amine substituent:
- cyclopropylaminocarbonyl
- ethylaminocarbonyl
- methylaminocarbonyl
- N6 substitution on the quinoline carboxamide ring system (N6-methoxy variants)
- ethylamino vs cyclopropylamino vs methylamino carbonyl linkages
Explicit single-compound claims
| Claim |
Exact structure title provided in your text |
| 11 |
4-(3-chloro-4-(cyclopropylaminocarbonyl)aminophenoxy)-7-methoxy-6-quinolinecarboxamide (or salt/hydrate) |
| 12 |
4-(3-chloro-4-(ethylaminocarbonyl)aminophenoxy)-7-methoxy-6-quinolinecarboxamide (or salt/hydrate) |
| 13 |
N6-methoxy-4-(3-chloro-4-(((cyclopropylamino)carbonyl)amino)phenoxy)-7-methoxy-6-quinolinecarboxamide (or salt/hydrate) |
| 14 |
4-(3-chloro-4-(methylaminocarbonyl)aminophenoxy)-7-methoxy-6-quinolinecarboxamide (or salt/hydrate) |
| 15 |
N6-methoxy-4-(3-chloro-4-(((ethylamino)carbonyl)amino)phenoxy)-7-methoxy-6-quinolinecarboxamide (or salt/hydrate) |
How does the patent handle “angiogenesis”?
Claim 10 states:
- A pharmaceutical composition comprising a claim-1 compound in an amount effective to inhibit angiogenesis.
This is a functional limitation tied to the pharmaceutical composition. In enforcement, this typically focuses on:
- Whether an accused product contains a claimed compound (or falls within claim 1 scope), and
- Whether the product is formulated/dosed such that it is used as an angiogenesis inhibitor (or is positioned in labeling/clinical use consistent with that function).
Patent landscape in the United States: what can be concluded from the claim text alone?
Only the claim text was provided. No patent metadata (application number, assignee, filing dates, priority, expiration, CPC/IPC classification, prosecution history, continuations) was included in your input. With no bibliographic record or family identifiers, a complete US landscape analysis (inter-family overlaps, citation network, FTO relevance, terminal disclaimer status, prosecution estoppel, or co-pending continuations) cannot be produced from the information provided.
Claim-scope map for designing around (based strictly on your claim language)
Claim 1 is broad, but two mechanisms create design space:
- Negative limitation: “Z12 is not pyrazolyl.”
- Two explicit exclusions: carve-outs (1) and (2) that remove specific variable combinations involving Ra12, R1/R2, and Z12.
Highest-leverage “design around” levers in claim text
| Lever |
Where it appears |
Why it matters |
| Z12 cannot be pyrazolyl |
claim 1 |
Direct exclusion of a substituent class |
| Exception (1): R1 = H, R2 = H and Z12 is aryl/heteroaryl types, Ra12 matches excluded form |
claim 1 |
Removes “simple” core substitution combos |
| Exception (2): R2 = H with specific Ra12 formula selection and Z12 in a constrained aryl/heteroaryl/substituted pattern |
claim 1 |
Removes another “anchor” set with R2 = H |
Practical implication for compound matching
In an infringement analysis, the first step is mapping a candidate compound onto:
- whether it has the same overall scaffold topology required by claim 1,
- what the candidate’s Z12 is (including whether it is “pyrazolyl”),
- the candidate’s Ra12 type (cyano vs carbonyl-containing variants),
- and whether it falls into exception (1) or exception (2) based on R1/R2 identity and Z12 class.
Key Takeaways
- US 7,253,286 has a broad Markush claim (claim 1) driven by variable sets (R1/R2, Z12, Ya1, Ra11, Ra12) with wide “optionally substituted” ranges.
- The claim includes two explicit exclusions (exceptions (1) and (2)) that remove specific variable combinations, especially where R1/R2 and Z12 classes align with the excluded patterns.
- Dependent claims (2-5) significantly narrow the variable space by fixing common substituent choices (Ra11 options, Z12 set, Ya1 Ra61 set, and Ra12 to cyano vs CONHRa62).
- Claims 6-8 enumerate many compliant exemplars, showing the practical target set of compounds.
- Claims 9-10 cover pharmaceutical compositions, including a composition-use limitation for angiogenesis inhibition.
- Claims 11-15 are dedicated to specific fixed formulas centered on quinolinecarboxamide motifs and substituted aniline/urea/carbonyl linkages with chloro and methoxy patterning.
- A complete US patent landscape (families, continuations, citations, expiry, and enforceability mapping) cannot be derived from claim text alone.
FAQs
1) Does claim 1 cover salts and hydrates?
Yes. Claim 2 and subsequent dependent claims explicitly limit to “pharmacologically acceptable salt or hydrate.” Claim 1 is written to cover compounds as such; dependent claims then add salt/hydrate scope for narrower sub-groups.
2) What is the most important negative limitation in the claims you provided?
“Z12 is not pyrazolyl” appears in claim 1, which excludes that specific heteroaryl class for Z12.
3) How are the exclusions structured in claim 1?
They are two separate carved-outs labeled (1) and (2), each defined by constraints on Ra12, R1/R2, and Z12 class/substitution patterns.
4) Which claims are directed to pharmaceutical compositions?
Claim 9 covers compositions with a carrier; claim 10 covers compositions “in an amount effective to inhibit angiogenesis.”
5) Are any single compounds explicitly claimed beyond the Markush set?
Yes. Claims 11-15 recite specific compound formulas (or salt/hydrates) with fixed substituent sets.
References
[1] United States Patent 7,253,286 (claims 1-15 as provided in the prompt).
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