United States Patent 6,967,208: Scope, Claim Structure, and US Patent Landscape
What does US 6,967,208 protect?
US Patent 6,967,208 protects a large genus of pyrazolo[3,4-c]pyridine-based small molecules (Formula I), including:
- Free bases and pharmaceutically acceptable salts
- Stereoisomers
- Broad sets of substituents on multiple ring positions (nested definitions of G, A, B, R, R1a/R1b/R1c/R1d, R2/R2a/R2b/R2c, R3/R3a/R3b/R3c/R3d/R3e/R3f, R4/R4a/R4b/R4c, and R5/R5a with constraints)
The patent also includes product-by-process style “compound-of-claim” downstream coverage:
- Pharmaceutical compositions containing a compound of claim 1 (or dependent-claim variants)
- Methods of treating thromboembolic disorders by administering an effective amount of a compound of claim 1 (or dependent variants)
The downstream coverage is broad: thromboembolic disorders include unstable angina, acute coronary syndrome, myocardial infarction variants, stroke, atherosclerosis, DVT, pulmonary embolism, and thrombosis from devices/procedures (e.g., prosthetic valves, stents, hemodialysis, cardiopulmonary bypass, and other blood-contact artificial surfaces) (claims 10-12, 34-36, 52-54, 55-61, 62-68, 69-75, 76-82, 83-89, 90-96, 97-103).
What is the independent claim’s core scaffold and binding logic (Formula I)?
Claim 1 is a genus claim to “a compound of Formula I” with a highly structured definition of substituent placement and allowed chemistry.
1) Macro-structure
The claimed molecule is defined by:
- A core ring system arranged by multiple variables, with ring substitutions at positions governed by:
- Ring M (with P1, P2, M1, M2), substituted with 0-2 occurrences of R1a
- Ring P (with P1, P2, P3) substituted with a group chain including G
- A linker/functional portion containing G and Formula IIa/IIb
- A second ring system including ring D and ring E, with conditional “ring D absent” fallback to broaden heteroaryl scope
2) Key conditional ring logic: ring D present vs absent
Claim 1 uses a branching definition:
-
Option A: ring D present
- Ring D is a 5-6 membered ring with:
- carbon atoms
- 0-2 heteroatoms selected from N, O, S(O)p
- Ring D:
- substituted with 0-2 R
- 0-3 ring double bonds
- Ring E:
- selected from phenyl, pyridyl, pyrimidyl, pyrazinyl, pyridazinyl
- substituted with 1-2 R
-
Option B: ring D absent
- Ring E present and selected from an expanded list:
- phenyl, pyridyl, pyrimidyl, pyrazinyl, pyridazinyl
- pyrrolyl, pyrazolyl, imidazolyl, isoxazolyl, oxazolyl, triazolyl, thienyl, thiazolyl
- Ring E substituted with 1-2 R
- Additional “ring E substituted with a 5-6 membered heterocycle” structure is also permitted:
- ring E can be substituted with 1 R
- the attached 5-6 heterocycle:
- has carbon atoms
- has 1-4 heteroatoms from N, O, S(O)p
- substituted with 0-1 carbonyl and 1-2 R
- 0-3 ring double bonds
3) Substituent freedom is controlled by permitted functional group sets
Claim 1 defines a broad set of permitted substituents with explicit exclusions, especially for reactive/unstable heteroatom connections.
R is one of the biggest “chemical breadth” drivers
R is selected from a long list including:
- simple H and halogens and alkyls
- hydroxy and alkoxy
- nitrile, trifluoromethyl (and variations in R3e/R4 structures)
- many amines/amides and sulfonamide-like fragments
- methylenedioxy/ethylenedioxy when two adjacent R groups combine
Claim 1 also imposes connectivity restrictions on R1a:
- R1a must form “other than” specific bonds (e.g., “R1a forms other than an N-halo, N-S, O-O, or N-CN bond”)
G is a major structural module with large conditional arrays
Claim 1 defines G as a group of Formula IIa or IIb, and within that:
- G1 can be absent or selected from extensive (CR3R3a)u... patterns with:
- carbonyl / ester / ether / thioether / sulfonamide / sulfone options
- amide and thioamide connectivities
- allowed u+w totals: 0, 1, 2, 3, or 4
- A key limitation:
- G1 does not form specific bonds: “N-S, NCH2N, NCH2O, or NCH2S” with either attachment group.
This architecture makes G a flexible chemistry “plug-in” while keeping the attachment topology constrained.
What does the independent claim’s “A-B-Q” portion do?
Claim 1 contains additional structure variables:
- A is C3-10 carbocycle substituted with 0-2 R4
- B attaches to a different atom on A such that the A-X-N moiety forms other than a N-N-N group
- Q1 is C=O
- ring Q is a 6 to 8 membered monocycle with:
- 0-2 double bonds
- substituted with 0-2 R4a
- X is absent
This yields a constrained “macro-ring” environment that can host carbonyl and substituted ring Q.
How broad is claim coverage in practice? (dependent claims narrow by substitutions and G lists)
The later claims (2-7 and 8-20) refine the Formula I universe by restricting which variables can occur.
Claim 2
Claim 2 further narrows ring D/E scope but still retains breadth by allowing multiple heteroaryl substitutions and a wide R set.
Claims 3-4
Claims 3-4 narrow:
- the G1 set (reduced enumerations and u+w totals narrowed in claim 3)
- reduced A scope (Claim 3 limits A to phenyl substituted with 0-2 R4)
- in Claim 4, the allowed G1 substituents are capped to a shorter list (examples: CH2, CH2CH2, CH2O, OCH2, NH, CH2NH, NHCH2, CH2C(O), etc.)
Claims 5-7
Claims 5 and 6 become materially more concrete, listing specific aromatic rings for A, and in claim 6:
- P4 is —G
- includes a narrower set of G definitions
Claim 8 onwards adds exemplified/defined compounds, including specific named molecules.
Which explicit compounds are listed (claim 8 and nearby)?
Claim 8 lists a set of example species and/or narrower claim intermediates (depending on how the dependent chain is structured in the original patent text). Examples include:
- 3-methoxy-1-(4-methoxyphenyl)-6-[4-(2-oxo-1-piperidinyl)phenyl]-1,4,5,6-tetrahydro-7-H-pyrazolo[3,4-c]pyridin-7-one
- 1-(4-methoxyphenyl)-3-[(methylamino)methyl]-6-[4-(2-oxo-1-piperidinyl)phenyl]-1,4,5,6-tetrahydro-7H-pyrazolo[3,4-c]pyridin-7-one
- 1-(3-chloro-4-fluorophenyl)-6-[4-(2-oxo-1-piperidinyl)phenyl]-3-(trifluoromethyl)-1,4,5,6-tetrahydro-7H-pyrazolo[3,4-c]pyridine-7-one
- Several variants changing:
- aromatic substituent patterns (methoxy, chloro, fluoro, cyano)
- substituents on pyrazolopyridine ring positions (carbonitrile, carboxamide, sulfonamide, tetraazolyl, benzamidine)
These listed structures anchor the genus to a consistent chemical series with recurring motifs:
- 4-(2-oxo-1-piperidinyl)phenyl as a common aryl side chain
- pyrazolo[3,4-c]pyridin-7-one-type core
- methoxy-substituted phenyl and related heteroaryl rings
What is the method-of-use claim scope?
All method claims are framed as:
“administering to a patient in need thereof a therapeutically effective amount of a compound of claim X or a pharmaceutically acceptable salt form thereof.”
Thromboembolic disorder definitions
Across claims:
- Arterial cardiovascular thromboembolic disorders
- Venous cardiovascular thromboembolic disorders
- Thromboembolic disorders in the chambers of the heart
Named conditions include:
- unstable angina
- acute coronary syndrome
- first myocardial infarction
- recurrent myocardial infarction
- ischemic sudden death
- transient ischemic attack
- stroke
- atherosclerosis
- peripheral occlusive arterial disease
- venous thrombosis
- deep vein thrombosis
- thrombophlebitis
- arterial embolism
- coronary arterial thrombosis
- cerebral arterial thrombosis
- cerebral embolism
- kidney embolism
- pulmonary embolism
- thrombosis caused by:
- (a) prosthetic valves or other implants
- (b) indwelling catheters
- (c) stents
- (d) cardiopulmonary bypass
- (e) hemodialysis
- (f) other procedures exposing blood to an artificial surface promoting thrombosis
Sub-class method claims
Dependent method claims then fix the disorder to:
- acute coronary syndrome
- stroke
- deep vein thrombosis
- pulmonary embolism
as seen in the later dependent chain (e.g., claims 58-61 and 65-68 and similar patterns 72-75, 79-82, 86-89, 93-96, 100-103).
Downstream product coverage: compositions
The composition claims mirror the method claims:
- each includes a pharmaceutically acceptable carrier
- and a “therapeutically effective amount” of a compound of a specified claim.
This gives the patent value for:
- unit-dose forms, oral solids, injectables, etc. (not specified in the claim text you provided, but composition claims are broad)
Patent landscape analysis (US)
Claim-structure-driven landscape implications
Even without analyzing other patents in the dataset, this document’s claim drafting drives the landscape question in a predictable way:
- Genus claim strategy (Formulas I/II)
- Broad chemical variable sets plus explicit exclusions make it harder to design around by small changes in ring substitution or heteroatom functionalization.
- Multiple “escape hatches” for structural substitutions
- The “ring D absent” branch plus expanded E lists create alternative chemical embodiments.
- Broad downstream use claims
- Once you fall within claim 1 (or narrower dependent compounds), the patent covers:
- composition
- method of treating thromboembolism across arterial/venous/cardiac chambers and many specific clinical events
Design-around pressure points
For competitors, the most relevant technical “knobs” are:
- whether the molecule keeps the pyrazolo[3,4-c]pyridin-7-one-like core topology and the specific ring connectivity implied by Formula I
- whether the substituent choices comply with R, R1a, G1 bond restrictions
- whether the substituent pattern falls into one of the allowed ring D/E conditional templates
Family and prosecution signals
The breadth of claim 1 and the heavy use of dependent claims to narrow specific modules (G1, R1a sets, A/B selections) is typical of a strategy to:
- secure a wide independent genus early
- then preserve narrower fallback positions tied to described species (the long list in claim 8 and the named structures in claims later)
That structure is consistent with a strong “coverage ladder”:
- broad genus for litigation leverage
- narrowed sub-genus for validity defense and settlement value
- explicit exemplified compounds as evidentiary anchor points
Key Takeaways
- US 6,967,208 is an expansive genus claim to Formula I compounds built on a pyrazolo[3,4-c]pyridine scaffold with multiple conditional ring modules (notably ring D present/absent and ring E expanded heteroaryl scope).
- Coverage extends beyond compounds to pharmaceutical compositions and broad thromboembolic treatment methods, listing specific clinical indications including ACS, MI, stroke, DVT, and pulmonary embolism, plus thrombosis linked to devices and procedures.
- The claim set uses nested variable definitions for chemical breadth while maintaining topology and connectivity constraints (e.g., explicit bond prohibitions for G1 and R1a).
- The likely competitive risk is high for any program that lands in the same scaffold and substitution topology because downstream method-of-use claims are also broad once the compound claim is met.
FAQs
1) Is claim 1 limited to a single ring system or does it allow multiple ring configurations?
It allows multiple configurations via conditional definitions, especially the “ring D present vs ring D absent” branches and expanded ring E lists.
2) Does the patent only cover free-base compounds or also salts and stereoisomers?
It covers stereoisomers and pharmaceutically acceptable salts alongside free bases.
3) What diseases does the method claims cover?
Thromboembolic disorders broadly, including unstable angina, acute coronary syndrome, myocardial infarction, stroke/TIA, atherosclerosis/PAD, DVT, pulmonary embolism, and thrombosis linked to implants, catheters, stents, cardiopulmonary bypass, hemodialysis, and other blood-contact artificial surfaces.
4) Are compositions claimed in the patent?
Yes. There are pharmaceutical composition claims that include a pharmaceutically acceptable carrier and a therapeutically effective amount of the claimed compound.
5) Where is the main design-around risk: compound scope or use scope?
The main risk is compound scope under claim 1 (Formula I). If a product falls inside, the use scope is already broadly covered for thromboembolic indications.
References
[1] US Patent 6,967,208 (claims provided in prompt text).
