|
Patent landscape, scope, and claims: |
United States Patent 10,000,480: Scope, Claim Structure, and Patent Landscape
What is US 10,000,480 claiming in plain terms?
US Patent 10,000,480 claims a large genus of chemical compounds defined by a core scaffold (Formula I) plus extensive substitution patterns controlled by variables Y, R1-R6, R11, R2a, R3a, R4-R5, Ra-Rf, and ring-fusion options, including:
- Stereoisomers and pharmaceutically acceptable salts
- A pharmaceutical composition containing one or more claimed compounds (Claim 14)
The top-level claim is Claim 1 (genus). Claims 2-13 are sub-genus / narrowing configurations by selecting specific meanings/sets for key variables (notably R2 and R3 and constraints on R4/R5). Claim 14 adds formulation coverage.
What is the core “handle” of Claim 1 (Formula I) and how broad is it?
Claim 1 is defined as a compound “having the following formula I: or a stereoisomer or pharmaceutically-acceptable salt thereof” with variable definitions. While the actual chemical drawing of Formula I is not included in the text supplied, the claim language makes it clear that infringement analysis will hinge on whether the accused compound:
- Matches the backbone of Formula I, including whether Y = N or CR6
- Matches the allowed substituent classes for R1, R2, R3, R4, R5, R6, and R11
- Falls within the permitted substitution multiplicities and permitted heterocycle/carbocycle “types” described for R2a and R3a (and their derivative substituents)
The scope is broad by construction: it allows repeated substitution with large sets of allowed functional groups (halogens, CN, nitro, OCF3/CF3/CHF2, sulfone/sulfonamide-like motifs, ether/thioether/linkers, amides, and multi-heteroatom rings), and it allows fused ring formation using “two R3a together with the atoms to which they are attached.”
How do the independent claim variables map to chemical space?
Y: N vs carbon (CR6)
Claim 1 limits Y to:
This creates at least a two-way fork in scaffold identity. If a product’s corresponding position is an amide-like N (or equivalent scaffold element), it can fall under Y = N; if it is carbon substituted by R6, it falls under Y = CR6.
R1: small substituent with deuterium and heavy halogen options
Claim 1 allows R1 to be:
- hydrogen, or
- C1-3 alkyl, or
- C3-6 cycloalkyl, each optionally substituted by 0-7 R1a
Where R1a can be:
- hydrogen, deuterium, F, Cl, Br, CN
So R1 is effectively a “small hydrophobic handle” with a high degree of permissible substitution if R1 is a methyl/ethyl/propyl or cycloalkyl.
R2: either an acyl/ester-like fragment or a ring-like fragment
Claim 1 defines R2 as either:
- —C(O)R2a, or
- a C1-6 alkyl, or
- —(CH2)r-3-14 membered carbocycle substituted with 0-1 R2a, or
- a 5-14 membered heterocycle containing 1-4 heteroatoms selected from N, O, S, substituted with 0-4 R2a
R2a is extensive: hydrogen, carbonyl-like (═O), halo, OCF3, CN, NO2, and a wide menu including ether/thioether, carboxamide, ester, urea-like fragments, sulfonamide-like fragments, and alkyl/haloalkyl/alkenyl/alkynyl/heterocycle substituents with substitution counts 0-3 depending on which category applies.
This is a major breadth driver: R2 is where accused products can “land” by selecting either a carbonyl-linked substituent or a ring system.
R3: larger hydrophobic/aryl/heteroaryl or fused ring
Claim 1 defines R3 as:
- C3-10 cycloalkyl, or
- C6-10 aryl, or
- a 5-10 membered heterocycle with 1-4 heteroatoms from N, O, S
Each is substituted with 0-4 R3a.
R3a has a very broad list including:
- hydrogen/halo/OCF3/CF3/CHF2/CN/NO2
- ether/thioether, carbonyl-containing groups, sulfonamide-like groups
- alkyl/haloalkyl/alkenyl/alkynyl
- fused ring formation: “or two R3a, together with the atoms to which they are attached, combine to form a fused ring wherein said ring is selected from phenyl and a heterocycle …”
This fused-ring option adds additional coverage for compounds where the aryl/heteroaryl is fused and where two substitution points effectively “close” into a fused ring system.
R4 and R5: dials controlling terminal polarity/size
Claim 1:
- R4 and R5 are independently hydrogen, or
- C1-4 alkyl substituted by 0-1 Rf, or
- (CH2)r-phenyl substituted by 0-3 Rd, or
- —(CH2)-5-7 membered heterocycle with 1-4 heteroatoms.
This supports a wide variety of terminal groups but keeps them within defined families.
R6: final handle with halo, CN, nitro, OH
Claim 1 allows R6:
- hydrogen
- halo
- C1-4 alkyl
- C1-4 haloalkyl
- OC1-4 haloalkyl
- OC1-4 alkyl
- CN
- NO2
- OH
This is consistent with a scaffold that includes a carbon position that can bear strongly electron-withdrawing or hydrogen-bonding substituents.
R11: small to medium N-substituent-like patterns
R11 (each occurrence independently) is selected from:
- hydrogen
- C1-4 alkyl substituted by 0-3 Rf
- C3-10 cycloalkyl substituted by 0-1 Rf
- (CH)r-phenyl substituted by 0-3 Rd
- (CH2)r-5-7 membered heterocycle containing 1-4 heteroatoms substituted by 0-3 Rd
R11 is used in amide/sulfonamide-like fragments inside R2a and R3a and thus influences the breadth of those fragments.
Ra, Rb, Rc, Rd, Re, Rf, p, r: the combinatorial expansion
Claim 1 contains multiple layered substitution variables:
- Ra and Ra1: include hydrogen, F/Cl/Br/OCF3/CF3/CHF2/CN/NO2, and linker-containing ether/thioether/carbonylamide and sulfonamide-like motifs; plus alkyl/haloalkyl, alkenyl/alkynyl, and carbocycle/heterocycle groups with substitution counts.
- Rb / Rc / Rd / Re / Rf: define substitution patterns on those motifs, including whether substituents include halogens, CN, OH, and heterocycles.
- p is 0-2, r is 0-1-2-3-4 in Claim 1 (later narrowed in dependent claims).
From a landscape perspective, this layered variability means many distinct structures can fall within Claim 1 even if the scaffold is fixed.
What do the dependent claims narrow?
Claim 2: narrows R2 to specific ring classes
Claim 2 states R2 is:
- —C(O)R2a, or
- C1-6 alkyl, C3-6 cycloalkyl, phenyl, or specific heteroaryl types:
- pyrazolyl, thiazolyl, pyridyl, pyrimidinyl, pyridazinyl, pyrazinyl, quinolinyl, pyrrolopyridinyl
- each substituted with 0-4 R2a
This is a narrower subset than Claim 1’s full “5-14 heterocycle with 1-4 heteroatoms” option.
Claim 3: sets R4 and R5
Claim 3: both R4 and R5 are hydrogen.
This is a targeted narrowing to a simpler terminal substitution pattern.
Claim 4: revised variable constraints (subset of Claim 1 but still broad)
Claim 4 defines compounds with formulae (text shows multiple formula placeholders) and includes:
- R1 hydrogen or C1-3 alkyl substituted by 0-7 R1a where R1a is hydrogen/deuterium/halogen
- R2 constrained to carbonyl form or C1-6 alkyl, C3-6 cycloalkyl, phenyl, or specific heteroaryl types (same list as Claim 2)
- R3 constrained to cycloalkyl (C3-10), aryl (C6-10), or 5-10 membered heterocycle with 1-4 heteroatoms
- R4 and R5 appear unconstrained in Claim 4 as written, but dependent claims later address them (Claim 3)
- R11 and the R3a substitution set are constrained more tightly than Claim 1 in some places
- fused ring limitation in Claim 4: fused ring is phenyl or a 5-7 membered heterocycle with 1-4 heteroatoms from N/O/S (substituted with 0-3 Ra1)
Claim 5: specific R2 heteroaryl selection
Claim 5 narrows R2 to:
- pyrazolyl, thiazolyl, pyridyl, pyrimidinyl, pyridazinyl, pyrazinyl, quinolinyl
each substituted with 0-3 R2a
Claim 6: a smaller R2 menu
Claim 6 narrows R2 to:
- —C(O)R2a, or
- C1-6 alkyl, C3-6 cycloalkyl, phenyl, each substituted with 0-3 R2a
Claim 7: R2 is “:” (incomplete in provided text)
Claim 7 text is cut off in the input (“wherein R2 is:”) and therefore cannot be used to produce a complete accurate narrowing description.
Claim 8: R3 selection
Claim 8 narrows R3 to:
- phenyl, cyclopentyl, cyclohexyl
- triazolyl, oxadiazolyl, pyrimidinyl, tetrazolyl
- pyrazolyl, thiazolyl, furanyl, pyranyl
each substituted with 0-4 R3a
Claim 9: detailed R3a/R11/Ra/Rb/Rd/Rc/Rf constraints and p
Claim 9 sets:
- R3a allowed set (contains CN, NH2, OCF3, ORb, halo, cycloalkyl, carbonyl-containing and sulfone/sulfonamide-like motifs, heterocycles with N/S/O, alkyl)
- “fused 5-7 membered heterocycle” option from two R3a
- R11 allowed set simplified
- Ra includes alkyl, halo(F), ORb
- Rb allowed set includes hydrogen, 5-7 heterocycles with N/S/O, or C1-6 alkyl
- Rd only F/Cl/Br/OH
- Rc is alkyl or cycloalkyl, substituted
- Rf is hydrogen/halo/OH
- p = 2
This is a meaningful technical restriction: it collapses earlier broad substitution lists and fixes p.
Claim 10: alternative R3aa/R3ab… and p = 0-2
Claim 10 defines a more specific scheme for R3 substitution:
- R3 is further split into R3aa and R3ab/R3ac/R3ad classes
- R3aa includes sulfone-like (S(O)pRc), ORb, Cl/F/CN/NH2, carbonylamide-like groups, sulfonamide-like motifs, alkyl substituted, and 5-6 heteroaryl
- R3ab/R3ac/R3ad include halo, ORb, and alkyl substituted, plus specific carbonyl and heterocycle classes
- R11 allowed set includes hydrogen/cyclopropyl (0-3 Rf) or alkyl (0-3 Rf)
- p is 0-2
Claim 11 and 12: narrow R3aa
- Claim 11: R3aa is S(O)pRc or C(O)NR11R11
- Claim 12: R3aa is ORb
Claim 13: narrows R3 further
Claim 13 defines R3 as a restricted set of options and corresponding R3aa/R3ab… patterns with constraints on Ra/Rb/Rc/Rd/Rf and fixed p range (p is 0-2) as written.
Claim 14: formulation
Claim 14: a pharmaceutical composition containing one or more compounds of Claim 1 plus a pharmaceutically acceptable carrier/diluent.
What is the infringement-relevant claim “breadth profile”?
Independent claim 1 is a genus with layered substitution
- Coverage depends on matching Formula I backbone (not fully visible in the text excerpt), plus satisfying the “variable-by-variable” substitution constraints.
- The breadth is dominated by:
- R2: carbonyl/ester-like handle and broad ring classes
- R3: aryl/heteroaryl/cycloalkyl/fused ring options
- substitution multiplicities: notably 0-4 for R3a and 0-4 for R3a-type substituents, and 0-7 for R1a when R1 is C1-3 alkyl or C3-6 cycloalkyl.
Dependent claims target specific “design spaces”
- If you want to avoid the broadest reading of Claim 1, the strongest narrowing hooks are:
- Claim 3 (R4=R5=H)
- Claim 5/6 (R2 narrowed to selected heteroaryl or phenyl/alkyl/cycloalkyl)
- Claim 8 (R3 narrowed to a defined set including phenyl and several heteroaryl rings)
- Claims 9-13: fixed/limited p, narrowed R3aa and allowed substituent repertoires
From a landscape standpoint, many competitors can still fall inside even these narrower claims because the lists include common medicinal chemistry motifs and common heteroaryl cores.
Patent landscape implications (scope-to-defense and scope-to-competition)
1) Risk is structural, not functional
The claims are structure-defined with substitution variables rather than a pharmacological function statement. That means:
- A competitor can’t easily “design around” by changing mechanism unless it changes the structure so that R1/R2/R3/Y/R4/R5/R6/R11 no longer match the variable definitions.
2) Design-around must attack claim definitional variables
Common design changes that may or may not work:
- Changing a substituent on the aryl/heteroaryl may still be captured if the substituent is within Ra/Rb/Rd/Rf sets.
- Removing a substitution might move you into a narrower dependent claim or remain within Claim 1 since many lists include hydrogen and “each occurrence independently” patterns.
- Using deuterium or specific halogens does not provide a safe harbor; the claim explicitly includes deuterium under R1a (Claim 1 and Claim 4).
3) Composition claim (Claim 14) expands downstream exposure
Even if a manufacturing intermediate is arguable, finished dosage forms that contain the claimed compound plus a standard carrier may fall under Claim 14.
What can be concluded about the “claim coverage” vs “therapeutic class”?
The provided claim excerpt does not include:
- the disease indication,
- target name,
- activity values,
- examples,
- or the identity of Formula I.
So landscape conclusions must remain at claim-scope level: the patent covers a structural genus and a formulation.
Key Takeaways
- US 10,000,480 Claim 1 is a broad structural genus built on Formula I with Y (N or CR6) and multiple substitution vectors (R1, R2, R3, R4-R6, R11) expanded by layered substitution variables (Ra-Rf) with multiple heteroaryl and carbonyl motifs.
- Dependent claims narrow the genus but still cover common medicinal-chemistry motifs: Claim 3 fixes R4=R5=H; Claims 5-6 restrict R2 to specific heteroaryl or simpler groups; Claims 8 and 9-13 restrict R3 and substituent patterns and fix p in at least Claim 9.
- Design-around must change structural elements that control variable definitions, not only tweak substituents, because many substitution lists include halogens, CN, alkyls, ethers, carbonyls, and heterocycles.
- Claim 14 adds formulation coverage, increasing exposure for finished products using claimed compounds.
FAQs
-
Is Claim 10,000,480 limited to one stereochemical form?
No. Claim 1 explicitly covers “a stereoisomer or pharmaceutically acceptable salt.”
-
Does the patent cover both free base and salts?
Yes. Claim 1 and dependent claims include “pharmaceutically-acceptable salt thereof.”
-
Which variables most strongly determine whether a compound falls in scope?
Y (N vs CR6), R2, and R3 are the highest-impact decision nodes due to the large allowed sets and fused-ring options; R4/R5 can further narrow.
-
Are there dependent claims that materially restrict R2 or R3?
Yes. Claims 5 and 6 restrict R2 to specific menus. Claims 8 and 9-13 restrict R3 and substitution rules (including fixed p in Claim 9 and p ranges in later dependent claims).
-
Does the patent include a drug-product/formulation claim?
Yes. Claim 14 claims a pharmaceutical composition comprising one or more Claim 1 compounds plus a carrier/diluent.
References
[1] United States Patent No. 10,000,480. Claims 1-14 (claim text provided in prompt).
More… ↓
⤷ Start Trial
|
