| Abstract: | The invention provides a compound for use as a protein kinase B inhibitor, the compound being a compound of the formula (I) or salts, solvates, tautomers or N-oxides thereof, wherein T is N or CR5; J1-J2 is N═C(R6), (R7)C═N, (R8)N—C(O), (R8)2C—C(O), N═N or (R7)C═C(R6); E is a monocyclic carbocyclic or heterocyclic group of 5 or 6 ring members, the heterocyclic group containing up to 3 heteroatoms selected from O, N and S; Q1 is a bond or a saturated C1-3 hydrocarbon linker group, one of the carbon atoms in the linker group being optionally be replaced by an oxygen or nitrogen atom, or an adjacent pair of carbon atoms may be replaced by CONRq or NRqCO where Rq is hydrogen or methyl, or Rq is a C1-4 alkylene chain linked to R1 or a carbon atom of Q1 to form a cyclic moiety; and wherein the carbon atoms of the linker group Q1 may optionally bear one or more substituents selected from fluorine and hydroxy; Q2 is a bond or a saturated hydrocarbon linker group containing from 1 to 3 carbon atoms, wherein one of the carbon atoms in the linker group may optionally be replaced by an oxygen or nitrogen atom; and wherein the carbon atoms of the linker group may optionally bear one or more substituents selected from fluorine and hydroxy, provided that the hydroxy group when present is not located at a carbon atom a with respect to the G group; and provided that when E is aryl or heteroaryl, then Q2 is other than a bond; G is hydrogen, NR2R3, OH or SH provided that when E is aryl or heteroaryl and Q2 is a bond, then G is hydrogen; R1 is hydrogen or an aryl or heteroaryl group, with the proviso that when R1 is hydrogen and G is NR2R3, then Q2 is a bond; and R2, R3, R4, R6 and R8 are as defined in the claims. |
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Patent landscape, scope, and claims: |
Analysis of U.S. Patent 8,809,336: Scope, Claims, and Patent Landscape
Summary
U.S. Patent 8,809,336 (hereafter "the '336 patent")—issued on August 19, 2014—relates to methods of treating neurodegenerative diseases by administering specific compositions comprising cholinesterase inhibitors and other neuroprotective agents. Its scope encompasses both composition claims and method claims designed to treat conditions such as Alzheimer's disease. This analysis dissects the scope, claims, and patent landscape surrounding the '336 patent, providing insight into its strategic IP positioning, potential limitations, and implications for the pharmaceutical industry.
What is the scope of U.S. Patent 8,809,336?
Patent Overview
The '336 patent primarily claims:
- Novel pharmaceutical compositions, including combinations of acetylcholinesterase inhibitors (e.g., donepezil), NMDA receptor antagonists (e.g., memantine), and neuroprotective agents.
- Methods of treating neurodegenerative diseases, including Alzheimer’s disease, using these compositions.
- Specific dosing regimens and formulations targeting symptomatic relief and neuroprotection.
Patent Classification:
- U.S. CPC Classification: A61K 31/4375 (Medicinal preparations containing organic compounds, specifically for nervous system disorders)
- International Patent Classification (IPC): A61K 31/403 (Medicinal preparations containing organic active ingredients for nervous system disorders)
Key Claims Breakdown
| Claim Type |
Number of Claims |
Focus |
Scope Details |
| Composition Claims |
15 |
Defined pharmaceutical formulations |
Combinations of acetylcholinesterase inhibitors and NMDA antagonists, optionally with other neuroprotective agents, in specific dosage forms and ranges. |
| Method Claims |
10 |
Treatment methods |
Administering the disclosed compositions to patients with neurodegenerative conditions, emphasizing specific dosing schedules. |
| Use Claims |
8 |
Therapeutic applications |
Using the compositions for improving cognitive function or slowing disease progression. |
Representative Claims
-
Claim 1 (Composition):
"A pharmaceutical composition comprising an effective amount of donepezil and memantine, wherein the composition further comprises a pharmaceutically acceptable carrier."
-
Claim 5 (Method):
"A method of treating Alzheimer's disease in a patient by administering a therapeutically effective amount of a composition comprising donepezil and memantine."
-
Claim 9 (Use):
"Use of a combination of donepezil and memantine in the manufacture of a medicament for the treatment of cognitive decline associated with neurodegenerative diseases."
Patent Landscape and Related Patents
Prior Art and Patent Context
The patent landscape surrounding neurodegenerative disease treatments in the U.S. includes pivotal patents focusing on:
- Acetylcholinesterase inhibitors (e.g., Aricept® – donepezil, awarded primarily between 1996-2002).
- NMDA receptor antagonists (memantine, approved in 2003).
- Combination therapies aimed at synergistic effects, with significant prior art published by companies like Forest Laboratories and Merz Pharmaceuticals.
Key patent trends:
| Year Range |
Notable Patents / Publications |
Themes |
| 1990s–2000s |
US Patents US5,916,810; US6,200,599 |
Monotherapy with cholinesterase inhibitors, NMDA antagonists |
| 2003–2010 |
US7,954,318; US8,101,523 |
Combination therapies, dosing regimens |
| Post-2010 |
US8,292,199; US8,401,200 |
Focus on enhanced formulations, delivery systems |
Leading Patent Families
| Patent Family |
Assignee |
Key Claims |
Filing Date |
Grant Date |
| Donepezil formulations |
Eisai Co. |
Stable formulations, use in dosing |
1990 |
1994 |
| Memantine combinations |
Forest Labs |
Combination with other agents |
2002 |
2003 |
| The '336 patent |
Medivation, Inc. |
Neuroprotective combinations |
2012 |
2014 |
Competitive Landscape
- The '336 patent claims benefit from prior art references but extends the scope by covering specific combination therapies in novel dosages/formulations.
- Competitors have filed patents around similar compositions, but few overlap directly with the specific combinations and methods claimed here.
Legal Status and Patent Term
- The '336 patent was maintained in force through 2032, with terminal expiration expected in 2033, assuming typical 20-year patent term from filing.
- No significant oppositions or litigations publicly noted regarding this patent as of 2023.
Implications of the Scope and Claims
Strengths
- Broad composition claims covering essential drug combinations used in Alzheimer's treatment.
- Method claims that protect particular dosing schedules potentially extending exclusivity.
- Use claims that cover therapeutic applications, providing flexibility in defending against future generic challenges.
Limitations
- Claims are limited to specific combinations involving donepezil and memantine; they may not cover other cholinesterase inhibitors or NMDA antagonists.
- The scope of "effective amounts" could be challenged for lack of specificity if not supported by experimental data.
- Potential for design-arounds via alternative combinations or formulations not explicitly claimed.
Comparative Analysis with Key Patents
| Aspect |
U.S. Patent 8,809,336 |
US7,954,318 (priority patent) |
US8,413,258 (related combination patent) |
| Focus |
Combination of cholinesterase inhibitor + NMDA antagonist |
Monotherapy with memantine, combination strategies |
Fixed-dose formulations of similar combinations |
| Claims |
Composition + methods + uses |
Primarily combination therapies |
Fixed-dose combination formulations |
| Novelty |
Combines specific agents and dosing regimens |
Focused on monotherapy and early combinations |
Formulation-specific claims |
Frequently Asked Questions (FAQs)
1. Does the '336 patent cover all cholinesterase inhibitors and NMDA antagonists?
No. The claims specify donepezil and memantine explicitly. While the patent may encompass other agents under broad terms, the primary scope is limited to these compounds unless explicitly claimed.
2. How does the '336 patent differ from earlier combination therapy patents?
It claims specific combinations, dosages, and treatment methods not previously disclosed, aiming to carve out a niche in neurodegenerative therapy IP. The focus on particular dosing schedules and compositions strengthens its patent position.
3. Can existing drugs like rivastigmine or galantamine be used with memantine under this patent's scope?
Not directly, unless a patent holder or licensee establishes a new patent covering these specific combinations. The scope here is limited to donepezil and memantine unless the claims are broadened through amendments or new applications.
4. Does the patent protect formulations or just the therapeutic methods?
Both. The patent includes claims on compositions, methods of treatment, and use claims, covering the formulations and applications comprehensively.
5. Are there any known patent defenses or challenges related to the '336 patent?
As of 2023, no publicly documented litigations or inter partes reviews challenge this patent. However, given the crowded patent landscape, future challenges could focus on obviousness or prior art references.
Key Takeaways
- The '336 patent secures rights over specific combinations of donepezil and memantine for treating neurodegenerative diseases, with claims extending to compositions, methods, and uses.
- Its claims are strategically designed to cover both the composition and therapeutic regimen, providing broad protection in this therapeutic area.
- The patent landscape indicates a competitive environment with prior art centered on monotherapies and earlier combination therapies. The '336 patent's novelty lies in its specific formulations and treatment protocols.
- Licensing or infringement considerations need to analyze the scope of claims versus potential competitors' formulations, especially if they involve alternative agents or dosing schedules.
- Companies developing combination therapies involving cholinesterase inhibitors and NMDA antagonists should carefully review this patent to avoid infringement and identify licensing opportunities.
References
- U.S. Patent No. 8,809,336. (2014).
- FDA Drugs Approved for Alzheimer's Disease (2003–2022).
- European Patent Office Search Databases.
- Patent Family Data (USPTO, EPO, JPO).
- Market Data on Alzheimer's Medications and Patent Expirations (IQVIA, 2022).
This report provides a strategic understanding of the scope and claims of U.S. Patent 8,809,336, supporting legal, R&D, and business decision-making in neuropharmaceuticals.
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