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Patent landscape, scope, and claims: |
United States Drug Patent RE46856: Scope, Claims, and US Patent Landscape
RE46856 is a US reissue claim set built around a single core compound class defined by a highly substituted scaffold with broad substituent permissiveness, plus dependent claim narrowing to specific heteroaryl heads, specific N-substituent closures, explicit exemplified analogs, and downstream claims to formulations, methods, and PI3K inhibition uses. Claim 1 is the economic center of gravity: it is a Markush-style genus with multiple substitution variables (R1-R8), including stereochemical and salt/solvate coverage. Dependent claims then carve narrower embodiments and specific listed species.
What does claim 1 actually cover? (Genus structure and degree of freedom)
Claim 1 preamble
- Covers: a compound of a generic formula (the formula itself is not fully reproduced in your excerpt, but the variable definition block is complete), plus:
- physiologically acceptable salt
- solvate
- hydrate
- stereoisomer
Core connectivity (R1) and embedded ring-closure options
Claim 1 defines R1 as:
- —(CH2)n—(CHR4)—(CH2)m—N(R5)(R5′)
With:
- n: integer 1 to 4
- m: integer 0 to 4
- Constraint: when R4 and R5 are taken together to form a nitrogen ring, n + m ≤ 4
R4 and the N-substituent definition are the key levers for claim breadth:
- R4 is hydrogen, hydroxy, or alkoxy
- R5 and R5′ are independently:
- hydrogen
- alkyl
- cycloalkylalklyl (as written)
- alkoxyalkyl
- or (optionally) taken together with the nitrogen to form a 3–7 member nitrogen-containing ring (optionally with O/N/S) with optional R6′ substitution
- OR R4 and R5 taken together with the attached atoms form a 5–6 member nitrogen-containing ring (optionally with additional N/O/S) with optional R6′ substitution
This means the genus includes:
- open-chain N-substitution (N(R5)(R5′))
- cyclic N-heterocycles via R5/R5′ cyclization
- alternative ring closure that uses R4 + R5 to build a fused/linked nitrogen-containing ring
R2 (heteroaryl head)
- R2 is a heteroaryl optionally substituted with 1, 2, or 3 R6 groups
Downstream dependent claims restrict R2 to specific named heteroaryl types:
- pyridine, pyridazine, pyrimidine, pyrazine, pyrole, oxazole, thiazole, furan, thiophene (and subsets in later claims)
R3 (alkyl/cycloalkyl)
- R3 is alkyl or cycloalkyl
Dependent claims later specify R3 = methyl.
R6 and R6′ (substituent dictionaries controlling heteroaryl patterning)
- Each R6 is independently chosen from a long list including:
- halogen, alkyl, alkenyl, alkynyl, cycloalkyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl
- heterocyclic ring, heterocyclylalkyl, alkyl-OR7, alkyl-SR7, alkyl-N(R7)(R7′), alkyl-COR7
- —CN, —COOR7, —CON(R7)(R7′), —OR7, —SR7, —N(R7)(R7′), —NR7COR7
- each R6 optionally substituted with 1 or more R8 groups
- Each R6′ is independently:
- alkyl
- cycloalkylalklyl (as written)
- or alkyl-OR7
So R6 controls heteroaryl ring substitution, and R6′ controls substitution on the nitrogen-containing ring closure.
R7 and R7′ (tails on OR/S/N substituents)
- R7 and R7′ independently:
- hydrogen
- alkyl, alkenyl, alkynyl
- cycloalkyl, cycloalkylalklyl (as written)
- cycloalkenyl, aryl, arylalkyl
- heteroaryl, heterocyclic ring, heterocyclylalkyl, heteroarylalkyl
R8 (optional extra functionalization on R6 substituents)
- R8 independently chosen from a set including:
- nitro, hydroxy, cyano, formyl, acetyl
- halogen, amino
- alkyl, alkoxy, alkenyl, alkynyl
- cycloalkyl, cycloalkylalklyl, cycloalkenyl, aryl, arylalkyl
- heteroaryl, heterocyclic ring, heterocyclylalkyl, heteroarylalkyl
Practical scope consequence
Claim 1 is not limited to a handful of examples. It reads as a large genus over:
- a substituted scaffold with a flexible N-terminus (open or cyclic)
- wide heteroaryl substitution patterns (1 to 3 R6)
- broad R6 dictionaries enabling many functional groups and nested substituent sets
- ring-closure modes that may significantly change topology while staying within the claim’s variable logic
How narrow are the dependent claims? (Risk segmentation by claim layer)
Claim 2 (R2 is specifically “nitrogen-containing heteroaryl”)
- Narrows R2 to:
- nitrogen-containing heteroaryl (still optionally substituted 1 to 3 R6)
Claims 3–6 (N substituent specificity via R5/R5′ and closure)
- Claim 3: R5 and R5′ independently alkyl
- Claim 4: R5 and R5′ taken together form a 5–6 member nitrogen-containing heterocycle with at least one additional O/N/S
- Claim 5: R4 = hydroxy
- Claim 6: R4 and R5 taken together form the 5–6 member nitrogen-containing heterocycle with optional heteroatoms
Claims 7–9 (R3 and explicit heteroaryl lists)
- Claim 7: R3 = methyl
- Claim 8: R2 is one of:
- pyridine, pyridazine, pyrimidine, pyrazine, pyrole, oxazole, thiazole, furan, thiophene
- unsubstituted or substituted with 1 to 3 R6
- Claim 9: same list but excludes furan and thiophene and includes:
- pyridine, pyridazine, pyrimidine, pyrazine, pyrole, oxazole, thiazole
Claims 10–21 (formula-dependent variants)
Claims 10, 11–12, 13–15, 16–18, 19–21 introduce “compound having the formula” language, which in your excerpt truncates the actual structural formula text. They continue to gate by R2 list subsets.
From your excerpt:
- Claim 11 and 12 restrict to R2 in a named heteroaryl list (with oxazole/thiazole included; furan/thiophene included in claim 14/17/20 sets, excluded in narrower sets).
- Claim 15 and 18 and 21 represent further reductions by excluding furan/thiophene and limiting to a subset.
Claims 22–26
- Claim 22: R5′ is alkyl
- Claim 24–26: further “compound having the formula” variants; claim 26 again requires R5′ is alkyl.
Claims 27–28 (explicit listed species coverage)
These two dependent claims list many specific compounds, each being within the claim 1 variable space, covering multiple:
- carboxamides (nicotinamide / pyrimidine- / thiazole- / isonicotinamide / etc. carboxamide variants)
- substituted “morpholine” sidechain topologies (morpholin-2-yl, morpholin-4-yl, dimethylamino propoxy analogs)
- halogenated and CF3 motifs
- different heteroaryl carboxamide ring substitution patterns
- stereochemical designations (“rel-” forms)
- salts and hydrates (e.g., hydrochlorides, trifluoroacetate)
This is how the patent captures “near neighbors” around the genus: it ensures that the company’s specific clinical candidates and the closest structural neighbors are explicitly claimed species.
Claims 29–34 (pharmaceutical compositions)
- Claim 29: composition with diluent/carrier
- Claim 30: therapeutically effective amount
- Claim 31: optionally includes additional active compound
- Claim 32: additional active compound categories include anti-proliferative, anti-inflammatory, analgesic, immunoregulatory, diuretic, anti-arrhythmic, anti-hypercholesterolemic, anti-diabetic, anti-dyslipidemia, anti-viral, etc.
- Claim 33: lists an expansive set of specific drugs (includes PI3K-adjacent and cancer therapeutics, plus many unrelated classes). This creates a broad combination-use claim.
Claims 35–37 (method claims)
- Claim 35: method of inhibiting phosphatidylinositol-3-kinase (PI3K) in cells by contacting with claim 1 compound(s)
- Claim 36: treating disorder mediated by PI3K inhibition in a mammal by administering effective amount of claim 1 compounds
- Claim 37: disorder categories include angiogenic, inflammatory, autoimmune, cardiovascular, neurodegenerative, metabolic, nociceptive, ophthalmic, pulmonary, renal
Subcategories appear in later claims:
- Claim 38: cardiovascular includes thrombosis, pulmonary hypertension, cardiac hypertrophy, atherosclerosis, heart failure
- Claim 39: inflammatory disorder includes COPD
- Claim 40: angiogenic disorder list includes diabetic retinopathy, ischemic retinal-vein occlusion, retinopathy of prematurity, macular degeneration, neovascular glaucoma, psoriasis, restenosis variants, vascular graft restenosis
Claims 41–46 (hyperproliferative disorder and cancer)
- Claim 41: treating hyperproliferative disorder mediated by PI3K inhibition
- Claim 42: cancer
- Claim 43: cancer types include breast, respiratory tract, brain, reproductive organs, digestive tract, urinary tract, eye, liver, skin, head and neck, thyroid, parathyroid, and distant metastasis of solid tumor
- Claim 44: lymphoma, sarcoma, leukemia
- Claim 46: explicitly mentions colorectal cancer for one compound embodiment
Claims 45, 47, 48–54 etc. (further narrowed species and formula-dependent branches)
- Claim 45: imposes:
- —N(R5)(R5′) = morpholinyl
- R2 heteroaryl list (pyridine/pyridazine/pyrimidine/pyrazine/pyrole/oxazole/thiazole)
- R3 = methyl
- Claim 48–50 further constrain via “compound having the formula” and R2 set
- Claim 52–56: method of treating lymphoma with compound of claim 50 (and salts/hydrates)
Claim 57
Truncated in the excerpt; it continues another “compound having the formula” branch.
What is the practical claim coverage map? (From genus to species to use)
Layer 1: Claim 1 genus
- Broad chemical space for a single scaffold family
- Controls:
- N-terminus topology (open vs ring closure)
- heteroaryl head type (any heteroaryl in claim 1; restricted lists in dependents)
- substitution count on heteroaryl (1–3 R6)
- broad substituent dictionaries (R6/R8)
Layer 2: Claim 2–26 narrowing
- Restricts:
- R2 to N-heteroaryls and/or named heteroaryls
- R3 to alkyl/cycloalkyl (then methyl)
- N substituent type (alkyl only) or morpholine-type by specific dependent claims
- ring closure modes
- R5′ alkyl
Layer 3: Claims 27–28 explicit enumerations
- Anchors enforceability around:
- multiple morpholine-propoxy substitutions
- carboxamide variants
- halogenated and CF3 analogs
- stereoisomer and salt/hydrate variants
Layer 4: Claims 29–34 compositions
- Enables formulation protection regardless of route (as written, just carrier/diluent and “therapeutically effective amount”)
- Provides combination therapy hooks with a huge “further active compound” list
Layer 5: Claims 35–46 method claims
- PI3K inhibition in cells
- Treating PI3K-mediated disorders
- Broad disease categories plus explicit cancer/cancer subtypes
Layer 6: Lymphoma-specific branch (claims 52–56)
- Ties a narrower compound set (claim 50 and derivatives) to lymphoma treatment
Patent landscape view for RE46856 (US enforcement posture)
RE46856 is a reissue number, which generally indicates the patent family already existed and is now reissued with a revised claim set. Your excerpt contains only the claim text, not prosecution history or cited documents. As a result, the landscape analysis below focuses on the enforcement posture implied by claim drafting rather than external bibliographic structure.
1) Chemical enforcement posture
2) Use enforcement posture
3) Combination therapy posture
- Claim 33 lists a very wide set of known drugs. This can matter for:
- combination trials
- label expansion scenarios
- off-label regimen patterns
- leverage in settlement talks tied to combination regimens
4) Formulation posture
- Claim 29–31 and claim 34 (“packaged pharmaceutical composition” with instructions) provide coverage for commercial packaging and patient-use instructions.
Claim-to-entity targeting: what features investors should map immediately
| Claim layer |
What it targets |
Where it bites |
Key gating variables |
| Claim 1 |
Chemical genus |
Any analog that fits variable logic |
R1 chain/ring closure, R2 heteroaryl and substitution count, R3, R4, R5/R5′ ring formation, R6/R8 dictionaries |
| Claims 2–9 |
Medium tightening |
“Similar” analog series |
R2 type restrictions; R3 = methyl; R2 list subsets |
| Claims 10–26 |
Formula-variant branches |
Specific sub-series |
“compound having the formula” branches plus heteroaryl list constraints; R5′ alkyl |
| Claims 27–28 |
Named species |
One-to-one with known analogs |
Morpholine/propoxy patterns and many exact carboxamide/heteroaryl combinations |
| Claims 29–34 |
Formulations and combos |
Product commercialization and combination regimens |
therapeutically effective amount; optional additional active agents |
| Claims 35–46 |
PI3K inhibition and treatment |
Clinical indication and method infringements |
PI3K-mediated disorder categories, cancer subtypes |
| Claims 52–56 |
Lymphoma branch |
Hematology development |
compound of claim 50 (and salts/hydrates) |
Key Takeaways
- Claim 1 is a broad Markush genus centered on a substituted scaffold with a flexible R1 N-terminus (including open-chain N(R5)(R5′) and ring-closure modes) and a heteroaryl head (R2) optionally substituted with 1–3 R6 groups.
- Dependent claims narrow by selecting specific heteroaryl lists, locking R3 to methyl, and constraining N-terminus features (including morpholinyl embodiments and R5′ alkyl).
- Claims 27 and 28 provide explicit coverage of many named species (including stereoisomers and salts/hydrates), which is critical for enforcement against real-world synthesized compounds.
- Use claims are expansive and PI3K-explicit, spanning PI3K inhibition in cells and treatment of a broad disorder set, including extensive cancer and hematologic malignancy categories.
- Formulation and combination claims broaden commercial reach, including packaged compositions and combination regimens with a long list of alternative active agents.
FAQs
-
Is RE46856 primarily a chemical patent or a method patent?
It is both. Claim 1 is a chemical genus; claims 35–46 add PI3K inhibition and PI3K-mediated treatment methods, plus disease categories.
-
How does the patent cover different ring topologies at the N-terminus?
Claim 1 uses variable definitions that permit either open N(R5)(R5′) or ring closure using R5/R5′ or R4/R5, subject to size constraints and an n+m ≤ 4 condition.
-
What is the role of “R2 optionally substituted with 1, 2 or 3 R6 groups”?
It drives breadth: it allows multiple substitution patterns on the heteroaryl head while remaining within the same compound family.
-
Do the claims include specific drug candidates or just generic structures?
They include both. Claims 27–28 list many specific compounds by name, alongside the genus of claim 1.
-
What disease areas are explicitly claimed?
PI3K-mediated disorders broadly, including angiogenic, inflammatory, autoimmune, cardiovascular, neurodegenerative, metabolic, nociceptive, ophthalmic, pulmonary, renal, and cancer including lymphoma, sarcoma, and leukemia.
References
[1] US Reissue Patent RE46856, claims text provided in prompt.
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