United States Patent 7,262,203: Scope, Claim Coverage, and US Landscape

What does US Patent 7,262,203 claim at the broadest level?

US 7,262,203 is a composition-of-matter patent that claims a family of substituted diamine compounds (and pharmaceutically acceptable salts) defined by four parallel generic formula sets (Formula (I), (II), (III), and (IV)). The patent then adds dependent sub-claims that narrow variable choices and ends with method and composition claims for angiogenesis-linked disorders, specifically including proliferative retinopathy.

The claim architecture is typical of a “core scaffold + permissive substitution” set:

Independent genus claim: claim 1 is the largest scope (Formula (I)).
Three additional independent genus claims: claims 5, 6, and 7 cover Formula (II), (III), and (IV).
Dependent claims 2 to 46: carve out specific sub-classes (mostly by restricting substituents like X1/X2/X3/X4, W, Q1, and the A1/A2 selection).
Formulation and use: claims 47 to 50 add pharmaceutical composition and angiogenesis-related treatment use.

What is the core chemical scaffold?

All independent formula sets share the same “systems chemistry” structure: a substituted aromatic/heteroaromatic diamine motif with a bicyclic/indazole-like region (as reflected in the enumerated examples in claim 46) linked to a pyrimidine core and a substituted aniline/benzenesulfonamide or related group. The variables in claims 1/5/6/7 mainly govern:

substituents on the aromatic rings (X1, X2, X3, X4)
an additional substituent on the aromatic core (W)
a para/meta substituent or ring substituent position (Q1)
a two-part substituent definition (Q2 and Q3) that selects either A1 or A2 on two positions, with mirror/consistent placement depending on which is selected
the specific identity of Z, Z1, and Z2 that define A2’s bridging fragment
side-chain and sulfonamide/carbamoyl-like options on Z2 and through R2/R3/R4/R5

Claim 1 (Formula (I)) variable map (high-level)

Claim 1 defines a compound of Formula (I) or a salt:

X1 = hydrogen, C1-C4 alkyl, C1-C4 haloalkyl, or C1-C4 hydroxyalkyl
X2 = hydrogen, C1-C4 alkyl, C1-C4 haloalkyl, C(O)R1, or aralkyl
X3 = hydrogen or halogen
X4 = hydrogen, C1-C4 alkyl, C1-C4 haloalkyl, heteroaralkyl, cyanoalkyl, “unsaturated” branched substituents, or C3-C7 cycloalkyl
W = C-R where R = hydrogen, halogen, or cyano
Q1 = hydrogen, halogen, C1-C2 haloalkyl, C1-C2 alkyl, C1-C2 alkoxy, or C1-C2 haloalkoxy
Q2 = A1 or A2
Q3 = conditional swap rule: Q3 is A1 when Q2 is A2, and Q3 is A2 when Q2 is A1
A1 = hydrogen, halogen, C1-C3 alkyl, C1-C3 haloalkyl, or -OR1
A2 = -(Z)m-(Z1)-(Z2) where:
- Z = CH2 (m = 0-3), or NR2 (m = 0-1), or oxygen (m = 0-1), or CH2NR2 (m = 0-1)
- Z1 = S(O)2, S(O), or C(O)
- Z2 = C1-C4 alkyl, NR3R4, aryl, arylamino, aralkyl, aralkoxy, or heteroaryl

Side groups in A2 and elsewhere:

R1 = C1-C4 alkyl
R2, R3, R4 each independently = hydrogen, C1-C4 alkyl, C3-C7 cycloalkyl, —S(O)2R5, or —C(O)R5
R5 = C1-C4 alkyl or C3-C7 cycloalkyl

Special conditional logic:

“when Z is oxygen then Z1 is S(O)2”
“when D is then X2 is C1-C4 alkyl, C1-C4 haloalkyl, C(O)R1, or aralkyl”
(the claim text compresses a missing symbol in the prompt, but the conditional constraint is still explicit)

What is the practical claim scope of the genus?

1) Substitution breadth is large but bounded by size/functional classes

Even with broad ranges (C1-C4, C3-C7), the genus is bounded to:

small alkyl/haloalkyl/hydroxyalkyl
limited ring substituents (halogen, alkoxy types, cyano, sulfonyl-like)
Z1 constrained to three oxidation states/forms: S(O)2, S(O), or C(O)
Z2 limited to a defined set including alkyl, amines, aryl, arylamino, aralkyl/aralkoxy, heteroaryl

2) The “A2” fragment is the main diversity engine

The A2 group is defined by three nested variables:

the “linker/heteroatom pattern” Z and m
the “oxidation/functional center” Z1 (sulfonyl, sulfoxide, or carbonyl)
the “terminal group” Z2

This makes the patent’s effective chemistry landscape closer to a “functionalized sulfonamide/sulfone/sulfoxide/carboxamide domain” rather than an unconstrained substitution manifold.

3) Dependent claims map to specific commercializable substitution patterns

Dependent claims 8 to 46 systematically restrict:

X1: H, C1-C4 alkyl; then methyl and ethyl specific
X2: H, C1-C4 alkyl; then hydrogen and methyl specific
X3: H vs halogen
X4: reduces to cyanoalkyl and a specific propargyl-type option (—(CH2)pC≡C(CH2)tH)
W: restricts R on the “W” substituent (H/F/Cl/CN)
Q1: restricts to H, halogen, C1-C2 alkyl/alkoxy, then specific instances (chlorine/methyl/methoxy)
Q2/Q3 switching: forces particular A1/A2 positional assignment while constraining A1 to H/halogen/alkyl/haloalkyl and A2 with smaller selections of Z and Z2 (often C1-C4 alkyl and limited R3/R4 = H or C1-C4 alkyl)

How do the parallel independent formulas narrow coverage?

Claims 5 to 7 provide alternative independent genus scaffolds (Formula II, III, IV). Each is similar to Formula I but changes which variables are allowed for X2 (and in claim 6, X2 excludes some options and changes the type of allowed substituent on that position).

Quick comparison: claim 1 vs claim 6 (Formula (III)) on X2

Claim 1 (Formula I): X2 can be hydrogen, C1-C4 alkyl, C1-C4 haloalkyl, C(O)R1, or aralkyl.
Claim 6 (Formula III): X2 is hydrogen, C1-C4 alkyl, C1-C4 haloalkyl, or C(O)R1.
The aralkyl option appears absent in claim 6’s X2 definition as pasted.

The net effect: the patent gives multiple overlapping genera so that different substitution positions and allowed functional classes can be captured, even if one formula set omits a category.

Claim 7 (Formula IV) aligns closely with claim 1

Claim 7 has the same X2 set as claim 1 in the pasted text (hydrogen, C1-C4 alkyl, C1-C4 haloalkyl, or C(O)R1, or aralkyl).

What do dependent claims enforce (and where are they highest value)?

A. “Single-variable lock-ins” create sub-ranges for freedom-to-operate design

High-value dependent claim filters include:

X1 specificities: claims 9 and 10 restrict X1 to methyl or ethyl; claim 10: X1 is methyl.
X2 specificities: claims 12-14 restrict X2 to hydrogen or methyl.
X3 split: claim 15 (X3 halogen) and claim 16 (X3 hydrogen).
X4 constrained to hydrogen/methyl/cyanoalkyl/propargyl-like: claim 17 and claim 18 restrict X4 to small set including —(CH2)pC≡C(CH2)tH with p=1, t=0.
W restricted to small set: claim 25 sets R in W to H/F/Cl/CN; claim 26 restricts to C-F or C-H.
Q1 restricted by functional class: claims 27-32 restrict Q1 to hydrogen/halogen/alkyl/alkoxy then specific chlorine/methyl/methoxy.

From an enforcement lens, these dependent claims allow the patentee to pursue:

broad infringement under claim 1 or one of the other independent formulas, and
fallback positions under narrower dependent claims when an accused compound misses a specific feature in claim 1.

B. A1/A2 positional selection is a secondary but strong fallback

Claim 32-41 and beyond:

enforce Q2 is A1 vs A2, and force Q3 to swap accordingly
restrict A1 to smaller class (H/halogen/C1-C3 alkyl/haloalkyl or -OR1)
restrict A2’s Z1 to one of S(O)2/S(O)/C(O), and frequently cap Z2 to C1-C4 alkyl or NR3R4 with R3/R4 restricted to H/C1-C4 alkyl

This means many candidate competitors could land in “near misses” that are still captured by narrower claim sets.

What is the explicit enumerated example set (claim 46)?

Claim 46 lists a large group of specific compounds (about 40+ named structures in the prompt). The enumerations anchor the abstract genus to concrete substitution patterns, and they reveal the chemistry the applicant considered most commercially or biologically relevant.

Examples in claim 46 include these repeated motif patterns

Across the enumerated compounds, the most repeated features include:

a fluoro substituent at one ring position (e.g., “5-fluoro-” appears repeatedly)
methyl substituents on the indazole-like ring (e.g., “3-methyl-1H-indazol-6-yl” appears frequently)
a pyrimidinediamine core (2,4-pyrimidinediamine appears repeatedly)
sulfonamide/sulfonyl substituents on the aryl ring:
- “methylsulfonyl”,
- “ethylsulfonyl”,
- “isopropylsulfonyl”,
- “isobutylsulfonyl”,
- and sulfonamide linkages (“methanesulfonamide”, “benzenesulfonamide”, “benzenesulfonamide” types)

Some entries also show:

benzenesulfonamide with methoxy substitution (e.g., “2-methoxy-5-(methylsulfonyl)phenyl”)
carbamide/carbonyl alternatives like “benzamide”, “acetamide”, “acetonitrile” substituents in certain named products
alternative heterocycles on Z2 side such as “isoxazole” appears in at least one enumerated compound (“5-methyl-3-isoxazolylymethyl”)

Enforcement value of claim 46

Claim 46 is a “selected group” claim that can be asserted if an accused compound matches any listed species. Its practical value is that it reduces the interpretive burden on claim construction for at least part of the competitor set.

What does the patent claim cover in the pharmaceutical and method space?

Pharmaceutical composition claim

Claim 47: pharmaceutical composition comprising a therapeutically effective amount of a compound of claim 1 (or salt) plus pharmaceutically acceptable carriers/diluents/excipients.
Claim 48: adds at least one additional anti-neoplastic agent.
Claim 49: adds an additional agent that inhibits angiogenesis.

Method-of-treatment claim

Claim 50: treating a disorder characterized by inappropriate angiogenesis; disorder is proliferative retinopathy; administered compound is a compound of claim 1 (or salt).

This ties the asset to the retina/angiogenesis therapeutic area rather than broad oncology alone.

Patent landscape implications (scope-driven, competitive map)

This is the portion of the landscape analysis that is fully determined by the text provided: the scope and claim structure alone.

1) Likely enforcement posture

Given the layered nature of:

independent genera (I-IV),
then dependent fallback restrictions (X1/X2/X3/X4/W/Q1/A1/A2),
then species list (claim 46),
plus composition and method claims (47-50),

the patent supports an enforcement posture that starts with claim 1/5/6/7 genus hits, then pivots to narrower dependent claims if an accused compound deviates on one variable.

2) Competitor design pressure points

A competitor seeking to design around would focus on removing membership in at least one of the following claim-critical “gates”:

Z1 selection gate: avoid all three allowed Z1 types is not feasible because A2’s Z1 is defined broadly (S(O)2, S(O), or C(O)). But competitors can still try to avoid the required connectivity or oxidation state pattern encoded by Z and m.
A2 structure gate (Z/m/Q2-Q3 positional logic): because Q2/Q3 determines whether A1 and A2 occupy two positions, a competitor can attempt to redesign substitution patterns that are positional inversions not covered by the conditional swap logic.
W and Q1 gate: W is restricted to R = H, halogen, or CN; Q1 is limited to H/halogen and small haloalkyl/alkyl/alkoxy classes. Many competitors can avoid by choosing bulkier aromatic substituents or different functional classes at those positions, if the scaffold allows.
X4 gate: X4 includes a fairly wide list but contains specific chemistry forms like cyanoalkyl and the propargyl-type —(CH2)pC≡C(CH2)tH (with allowed p and t values in claim 1). Competitors can avoid by selecting X4 substituents outside the enumerated functional classes and allowed unsaturation patterns.

3) Where the patent is strongest

The enumerated species in claim 46 indicates “strong coverage” in the region of:

5-fluoro substitution
methylated indazole-like ring
pyrimidinediamine core
aryl sulfonyl/sulfonamide substituents (methylsulfonyl/ethylsulfonyl/isopropylsulfonyl variants)
methoxy substitutions on the aryl sulfonamide ring

If an accused compound shares these repeatedly used motifs, it is likely to fall within one of the narrow dependent claims and/or the species claim.

4) Where freedom-to-operate is most likely to be challenged

Method and composition coverage anchors the patent to:

proliferative retinopathy as the angiogenesis disorder
administration of a claim 1 compound (not merely any formula I-IV compound)

So, even if a competitor lands in Formula II/III/IV territory, the method claim is still tethered to “compound as claimed in claim 1.” The composition claims similarly tether to claim 1. That creates a split risk profile:

liability risk for actual treated indication likely depends on whether the commercial compound falls under claim 1 specifically, not just other formula sets.

Claim set summary table

Claim	Type	Coverage focus (from prompt text)	Practical enforcement fallback
1	Independent genus	Formula (I) core variable space (X1-X4, W, Q1, Q2/Q3 with A1/A2, A2 via Z/Z1/Z2)	Broadest + most used in compositions/methods
5	Independent genus	Formula (II) similar structure; X4 and Q/A substitutions similar	Genus alternative if Formula I misses
6	Independent genus	Formula (III) with X2 option set changed (aralkyl removed in pasted)	More selective alternative genus
7	Independent genus	Formula (IV) close to Formula I (X2 includes aralkyl in pasted)	Another overlapping coverage point
8-46	Dependent	Narrowing constraints on X1/X2/X3/X4, W, Q1, Q2/Q3 and A1/A2 subspace	Second-line positions if a feature is missed
47	Composition	Composition containing a compound of claim 1	Use in marketed or formulated products
48-49	Composition enhancer	Adds anti-neoplastic or angiogenesis inhibitor co-therapies	Combination claim leverage
50	Method	Treat proliferative retinopathy by administering claim 1 compound	Indication-linked enforcement

Key Takeaways

US 7,262,203 is a large genus patent with four overlapping independent formula claims (I-IV) and a heavy dependent fallback suite that progressively narrows substituent classes.
Claims 47 and 50 tether to claim 1 specifically, so method and composition enforcement risk for proliferative retinopathy depends on whether the product falls within Formula (I) rather than just Formula (II)-(IV).
The A2 fragment is the principal diversity driver via Z (and m), Z1 (S(O)2/S(O)/C(O)), and Z2 (alkyl/amino/aryl/aralkyl/aralkoxy/heteroaryl).
Claim 46 lists concrete covered species dominated by fluorinated, methylated indazole-like and pyrimidinediamine motifs with aryl sulfonyl/sulfonamide substituents, creating strong anchor points for infringement analysis against likely analogs.

FAQs

1) Does US 7,262,203 cover salts?

Yes. Claims 1, 5, 6, and 7 each explicitly claim the compound “or a salt thereof,” and dependent/species/composition claims reference salts as applicable.

2) Is proliferative retinopathy explicitly covered?

Yes. Claim 50 states the disorder is proliferative retinopathy, characterized by inappropriate angiogenesis.

3) Can a competitor avoid method and composition liability by falling under Formula (II)-(IV) but not Formula (I)?

Based on the claim text provided, the method claim (50) and composition claims (47-49) reference compounds “as claimed in claim 1,” so coverage for those claims is tied to Formula (I) membership.

4) Which substituents get the tightest dependent-claim narrowing?

The dependent claims explicitly narrow X1 (often to methyl/ethyl), X2 (often to hydrogen/methyl), W (often to H/F/Cl/CN), Q1 (often to H/chlorine/methyl/methoxy), and X4 (often to hydrogen/methyl/cyanoalkyl/propargyl-like forms), with further narrowing via Q2/Q3 and A2’s Z/Z1/Z2 constraints.

5) Is there an “explicit species” list in the patent?

Yes. Claim 46 enumerates a large set of specific compounds by name, each “or a salt thereof,” which can be asserted directly if a competitor product matches any listed structure.

References

[1] US Patent 7,262,203, claims 1, 5-7, 8-50 (as provided in the prompt).

Country	Patent Number	Estimated Expiration	Supplementary Protection Certificate	SPC Country	SPC Expiration
European Patent Office	1343782	⤷ Start Trial	C300456	Netherlands	⤷ Start Trial
European Patent Office	1343782	⤷ Start Trial	CA 2010 00024	Denmark	⤷ Start Trial
European Patent Office	1343782	⤷ Start Trial	91710	Luxembourg	⤷ Start Trial
>Country	>Patent Number	>Estimated Expiration	>Supplementary Protection Certificate	>SPC Country	>SPC Expiration

Details for Patent: 7,262,203

Summary for Patent: 7,262,203