|
Patent landscape, scope, and claims: |
United States Patent 9,108,973 (Drug Patent): Scope of Claims, Claim Architecture, and Patent Landscape
What is the claim scope of US Drug Patent 9,108,973?
US 9,108,973 claims a family of compounds defined by a single overarching structural formula (Formula (I)), plus dependent claim layers that narrow substitution patterns, and then a final set of embodiments tied to specific named compounds. The claims also cover pharmaceutical compositions and an FGFR inhibition tumor-treatment method.
Independent claim 1: Formula (I) compound and salt
Claim 1 recites a “compound represented by Formula (I) or a salt thereof” with a large set of variable groups:
Core variable groups in Formula (I)
- R1: each occurrence independently represents C1-C6 alkyl.
- X1 and X2: independently N or CH.
- Y: a substituent linked to Formula (A), (B), or (C):
- Formula (A) moiety: includes a divalent moiety that is a nitrogen-containing C3-C10 heterocycloalkylene group.
- Formula (B) moiety: includes a divalent moiety that is a C3-C10 cycloalkylene group.
- Formula (C) moiety: includes a divalent moiety that is a C6-C12 arylene group.
- Connection rule: “the methylene group of Subformulas (A), (B) and (C) is connected to the nitrogen of the bicycle.”
- R2: selected from a broad functional set, including:
- Hydrogen
- C2-C6 alkynyl
- —C(═O)ORx
- —C(═O)N(Rx)(Ry)
- hydroxy-C1-C6 alkyl
- di(C1-C6 alkyl)amino-C1-C6 alkyl
- C2-C9 heteroaryl, optionally having R3
- R3: C1-C6 alkyl or di(C1-C6 alkyl)amino-C1-C6 alkyl
- Z: vinylene/alkenyl or alkynyl substitution pattern:
- —C(R4)═C(R5)(R6) or —C≡C—R7
- R4, R5, R6:
- same or different; each is hydrogen, halogen, C1-C6 alkyl optionally having R8, or Formula (D) group
- Formula (D) monovalent moiety:
- “nitrogen-containing C3-C10 heterocycloalkyl group”
- R7:
- hydrogen, C1-C6 alkyl, or hydroxy-C1-C6 alkyl
- R8:
- R9:
- C1-C6 alkyl, halogen, or —ORx
- l, m, n:
- l = 0 to 3
- m = 1 to 3
- n = 0 to 2
- Rx and Ry:
- same or different; each is hydrogen, C1-C6 alkyl, C3-C10 cycloalkyl, di(C1-C6 alkyl)amino-C1-C6 alkyl, or C1-C6 alkoxy-C1-C6 alkyl
What this means for coverage
Claim 1 is designed to cover:
- Multiple heterocycle classes for Y (heterocycloalkylene, cycloalkylene, and arylene-linked options)
- Binary choices for X1/X2 (N vs CH)
- A large substitution space at Z (alkenyl or alkynyl with defined substitution patterns)
- Multiple nitrogen-containing substituent options (via Formula (A), Formula (D), and Rx/Ry-containing groups)
- Multiple functionalizations at R2 (carbonyls, amides, alkyne handles, aminoalkyl, heteroaryl)
Dependent claim 2: specific (X1, X2) pairing
- If X2 = N, then X1 = N or CH
- If X2 = CH, then X1 = CH
This claim narrows the binary N/CH arrangement to reduce redundant permutations and focus on specific structural series.
Dependent claim 3: l limited
This narrows the numeric degree-of-substitution parameter in Formula (I).
Dependent claim 4: enumerated choices for Y and Z-structure classes
Claim 4 narrows Y and then enumerates the allowed members:
- If Y = Formula (A), then the divalent moiety is:
- azetidinylene
- pyrrolidinylene
- piperidinylene
- piperazinylene
- morpholinylene
- If Y = Formula (B), then the divalent moiety is:
- cyclopropylene
- cyclobutylene
- If Y = Formula (C), then the divalent moiety is:
This is a key narrowing layer: it converts a broad “C3-C10” and “C6-C12” type definition into named rings for the nitrogen-containing and cycloalkylene alternatives.
Dependent claim 5: Z restrictions depending on Y
- If Y = Formula (A):
- Z is —C(R4)═C(R5)(R6) or C≡C—R7
- If Y = Formula (B) or (C):
So alkyne-form Z is allowed with Y in Formula (A), but not in Formula (B)/(C).
Dependent claim 6: R1 limited
Dependent claim 7: R2 limited
R2 is narrowed to:
- C2-C6 alkynyl
- —C(═O)ORx
- hydroxy-C1-C4 alkyl
- C2-C9 heteroaryl optionally having R3
Dependent claim 8: explicit compound list (1) to (40)
Claim 8 selects a set of 40 specific named stereoisomeric and regioisomeric compounds within the Formula (I) space. The enumerations include:
- Pyrazolo[3,4-d]pyrimidine and pyrrolo[2,3-d]pyrimidine and related bicyclic core variants
- Substitution at the linker nitrogen-containing ring (pyrrolidine, azetidine, pyrrolidine, etc.)
- Multiple “right-side” amide/alkenyl/alkynyl patterns such as:
- prop-2-en-1-one (enone)
- prop-2-yn-1-one (alkynone)
- but-2-en-1-one / but-2-yn-1-one
- Multiple substituents on the terminal amine-bearing group:
- dimethylamino, diethylamino, tert-butylamino, cyclopropylamino, cyclobutylamino, (fluoro) substituted amino rings, hydroxy-bearing amino rings, etc.
Claim 9: pharmaceutical composition
- A composition comprising:
- the compound (or salt) of claim 1
- plus a pharmacologically acceptable carrier
Claim 10: method for treating tumor by inhibition of FGFR
- “A method for treating a tumor by the inhibition of FGFR”
- Administration of an effective amount of the compound (or salt) of claim 1.
Bottom line: the patent stakes out both (1) structure coverage across a wide chemical space and (2) use coverage tied directly to FGFR tumor inhibition.
How is the claim set structured for enforceability?
Two-tier protection
- Tier 1 (composition and method): claim 9 and claim 10 extend into downstream commercialization:
- Formulation coverage (claim 9)
- Therapeutic utility coverage (claim 10), anchored to FGFR tumor inhibition
- Tier 2 (compound structural coverage):
- claim 1 is the broadest structural anchor
- claims 2-7 provide narrowed structural “islands”
- claim 8 provides a set of explicit exemplars that often become focal points in infringement and invalidity analytics
Tightening logic visible in dependencies
- X1/X2 arrangement constrained (claim 2)
- Numeric parameter l constrained (claim 3)
- Ring identity for Y enumerated (claim 4)
- Z chemistry depends on Y (claim 5)
- Small substituent types constrained (claim 6 for R1)
- R2 function set constrained (claim 7)
- Explicit compound list provides concrete claim interpretation points (claim 8)
In litigation terms, this gives multiple fallbacks. Even if the broadest span is attacked, the narrower dependent claims provide structured containment zones.
What does claim 8’s 40-compound list imply about the practical scope?
Claim 8’s explicit list functions like a “catalog” of preferred members and likely illustrates the patent’s working dataset.
Common chemical themes across the 40 compounds
From the enumerations, the following patterns recur:
- The bicyclic core is based on pyrazolo[3,4-d]pyrimidin-1-yl or pyrrolo[2,3-d]pyrimidin-7-yl (and related fused core systems).
- The linker ring is frequently:
- pyrrolidin-1-yl or azetidin-1-yl
- The “tail” is repeatedly an enone or related carbonyl motif:
- prop-2-en-1-one, prop-2-yn-1-one
- but-2-en-1-one, but-2-yn-1-one
- R2 and Z substitutions correspond to the claim’s vinyl/alkynyl and carbonyl functional sets.
- Terminal amine substituents are varied, including:
- dialkylamino groups (dimethylamino, diethylamino, isopropylamino, cyclopropylamino, cyclobutylamino, tert-butylamino)
- hydroxy-bearing amino rings (hydroxypyrrolidinyl, hydroxypiperidinyl)
- fluorinated stereocenters in certain listed compounds (3-fluoropyrrolidin-1-yl)
Stereochemistry coverage
Multiple entries specify (S), (R), and (2S,4S). This increases the probability that the patent is intended to cover specific stereoisomer populations rather than racemates.
Practical implication for FTO
From a freedom-to-operate perspective, competitors producing:
- the same scaffold family with small ring swaps in the linker domain,
- the same core fused heterocycles,
- and similar vinyl/alkyne enone/alkynone terminal patterns,
are the most likely to collide with this patent’s literal scope.
What is claimed therapeutically (FGFR) and how does it affect landscape mapping?
Claim 10 ties the chemistry to FGFR tumor inhibition
The method claim is explicit:
- “treating a tumor by the inhibition of FGFR”
This is a functional endpoint. In landscape work, the main enforcement risk rises when:
- the compound is an FGFR inhibitor (or is marketed/used as such)
- a competitor’s product label or clinical protocol ties use to FGFR inhibition in tumors
How does the patent likely sit in the broader US FGFR inhibitor landscape?
A precise cross-patent landscape requires bibliographic and citation data (family members, priority date, continuations, and litigation/office actions) that are not included in the provided record. With the information provided, only the internal claim structure can be mapped accurately.
Landscape placement based on claim architecture alone
- This patent is positioned as a scaffold-range FGFR small-molecule composition + method filing, rather than:
- a narrow single-substitution patent, or
- a biomarker-only utility claim
- It contains multiple structural fallbacks (claims 2-7) and a concrete exemplar slate (claim 8), typical of patents that expect to defend a broad scaffold while anchoring enforceability with narrowed dependent claim targets.
High-level competitive threat categories
Within the chemical class defined by claim 1 and claim 8, the most sensitive competitive overlap vectors are:
- Same core heterocycle families with different ring substituents in the Y-position (azetidinylene, pyrrolidinylene, etc.)
- Same Z-vinylene/alkynyl motif choices with defined conditional behavior (claim 5)
- Same R2 functional set (claim 7) used in FGFR-inhibitor designs
- Same stereochemistry for the listed exemplars (claim 8)
Key claim scope map (compact, infringement-relevant)
Variables and their allowed ranges
| Feature |
Allowed options in claim 1 (selected) |
Narrowing via dependent claims |
| R1 |
C1-C6 alkyl |
R1 = methyl or ethyl (claim 6) |
| X1, X2 |
each N or CH |
enforce pair logic (claim 2) |
| Y |
Formula (A) N-heterocycloalkylene (C3-C10), Formula (B) cycloalkylene (C3-C10), Formula (C) arylene (C6-C12) |
enumerated ring members (claim 4) |
| Z |
alkenyl or alkynyl pattern |
Z allowed in alkyne form only when Y = Formula (A) (claim 5) |
| R2 |
H, alkynyl, carbonyl ester/amides, hydroxyalkyl, aminoalkyl, heteroaryl |
narrowed set (claim 7) |
| R4-R6 |
H/halogen/C1-C6 alkyl or Formula (D) |
constrained by chosen Y/Z (claim 5) |
| l, m, n |
l 0-3; m 1-3; n 0-2 |
l = 0 or 1 (claim 3) |
| Rx, Ry |
H, alkyl, cycloalkyl, aminoalkyl, alkoxyalkyl |
used throughout functional group definitions |
Downstream protection
- Composition: claim 9
- Method of treatment (FGFR inhibition): claim 10
Key Takeaways
- US 9,108,973 claims a large Formula (I) scaffold with flexible substitution at X1/X2, Y, R2, and Z, plus numeric parameters l, m, n.
- Dependent claims narrow the chemistry via:
- ring identity for Y (azetidinylene/pyrrolidinylene/piperidinylene/piperazinylene/morpholinylene; cyclopropylene/cyclobutylene; phenylene),
- Z allowed forms conditional on Y,
- R1 = methyl or ethyl,
- R2 functional set limitation,
- and l = 0 or 1.
- Claim 8 enumerates 40 specific stereoisomeric compounds, making the patent’s practical scope anchored to concrete embodiments.
- Claims 9 and 10 add enforceable downstream coverage for pharmaceutical compositions and FGFR tumor treatment methods.
FAQs
1) Does claim 1 cover salts as well as free base compounds?
Yes. Claim 1 covers “a compound represented by Formula (I) or a salt thereof.”
2) What ring classes are permitted for Y in the independent claim and narrowed claim?
Claim 1 permits Y to be defined via Formula (A) (nitrogen-containing C3-C10 heterocycloalkylene), Formula (B) (C3-C10 cycloalkylene), or Formula (C) (C6-C12 arylene). Claim 4 narrows those to specific ring members (azetidinylene, pyrrolidinylene, piperidinylene, piperazinylene, morpholinylene; cyclopropylene, cyclobutylene; phenylene).
3) Is the Z substitution allowed to be alkynyl for all Y options?
No. Claim 5 allows Z as either alkenyl or alkynyl when Y = Formula (A), but restricts Z to alkenyl when Y = Formula (B) or (C).
4) What therapeutic target is tied to the method claim?
Claim 10 ties treatment to “inhibition of FGFR.”
5) How many specific compounds are enumerated in claim 8?
Claim 8 lists 40 named compounds.
References
[1] Provided claim text for US Drug Patent 9,108,973 (claims 1-10).
More… ↓
⤷ Start Trial
|
