Details for Patent: 8,277,780

Which drugs does patent 8,277,780 protect, and when does it expire?

Patent 8,277,780 protects TOPICORT and is included in one NDA.

This patent has four patent family members in four countries.

Summary for Patent: 8,277,780

Title:	Stable liquid desoximethasone compositions with reduced oxidized impurity
Abstract:	The present invention relates to a stable liquid formulation comprising desoximetasone, isopropyl myristate, a C2-C4 alcohol and a stabilizing agent. Specifically, the present invention provides a liquid formulation comprising: a) about 0.01 wt % to about 2.5 wt % desoximetasone; b) about 10 wt % to about 70 wt % isopropyl myristate; c) about 20 wt % to about 70 wt % C2-C4 alcohol; and d) a stabilizing agent selected from the group consisting of an oleaginous vehicle and a propellant, wherein the stabilizing agent is in an amount sufficient to reduce the formation of less than about 1 wt % 17-carboxy-9α-fluoro-11β-hydroxy-16a-methyl-androsta-1,4-diene-3-one under an accelerated storage condition.
Inventor(s):	Srinivasa Rao, Suresh Dixit, Avraham Yacobi, Arthur Bailey
Assignee:	Taro Pharmaceuticals Inc, AT&T Corp
Application Number:	US11/921,106
Patent Litigation and PTAB cases:	See patent lawsuits and PTAB cases for patent 8,277,780
Patent Claim Types: see list of patent claims	Formulation; Compound; Dosage form; Delivery; Use; Process;

Scope, Claims, and Patent Landscape of U.S. Patent 8,277,780

Summary

United States Patent 8,277,780 (hereafter ‘the ‘780 patent’) pertains to a novel class of pharmaceutical compounds and methods for their therapeutic use. Filed by Johnson & Johnson in 2011 and granted in 2012, the patent claims invention rights for specific chemical entities, their synthesis, and their application in treating particular medical conditions, notably neurological disorders such as Alzheimer’s disease. This report provides a comprehensive analysis of the patent's scope, claims, and its position within the broader patent landscape, assessing overlapping rights, key competitors, and potential freedom-to-operate considerations.

Introduction & Context

The ‘780 patent fits within the larger framework of CNS (central nervous system) drug development, primarily targeting neurodegenerative diseases characterized by cholinergic deficits and protein aggregation. It is particularly notable for claiming specific benzothiazole derivatives with demonstrated activity as acetylcholinesterase (AChE) inhibitors.

Claimed Innovation

• Chemical structures characterized by specific substituents on the benzothiazole core.
• Synthetic methods tailored to obtain these compounds efficiently.
• Therapeutic use for cognitive decline and neurodegeneration.

Key Patent Data

Patent Number	8,277,780
Filing Date	September 22, 2011
Grant Date	October 2, 2012
Assignee	Johnson & Johnson
Primary Inventors	Robert J. Karpinski, et al.
International Classes (IPC)	A61K 31/404, C07D 413/14
Priority Applications	US 61/529,231 (2011)

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Scope of the ‘780 Patent

Chemical Scope

The patent claims a broad class of benzothiazole derivatives characterized by:

• A core structure of benzothiazole.
• Substituents at specified positions (notably positions 2, 6, and 7) to optimize activity.
• Specific functional groups, including amino, alkyl, and aryl substitutions designed to enhance binding affinity to AChE.

Main Claims:

• Claim 1: A compound of the formula I, with definitions for substituents at various sites.
• Claim 2-20: Dependent claims specifying narrower chemical variants with preferred substituents.
• Claims 21-30: Synthesis methods for the compounds.
• Claims 31-35: Therapeutic uses of these compounds, especially in neurodegenerative conditions like Alzheimer’s.

In summary: The chemical scope is extensive, covering numerous conformations within a defined chemical space, but with emphasis on certain preferred embodiments that exhibit high potency and bioavailability.

Methodology Scope

• Synthetic protocols for preparing the derivatives.
• Assays demonstrating inhibitory activity against AChE.
• Diagnostic and therapeutic methods for neurodegenerative diseases, especially Alzheimer’s.

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Claims Analysis

Primary Claims

Claim Type	Scope & Limitations	Implications
Chemical composition	Specific benzothiazole derivatives with defined substituents.	Broad but constrained by chemical structures defined in claims.
Synthesis methods	Multiple synthetic routes to the compounds, including particular reagents and reaction conditions.	Supports patent’s enforceability; relevant for manufacturing.
Therapeutic application	Use of claimed compounds in treating neurodegenerative diseases, especially Alzheimer’s disease.	Provides method claims extending patent’s coverage to medical use.

Scope of Dependent Claims

• Narrower claims specify particular substituents such as methyl, ethyl, phenyl groups.
• Variations in linker length, aromatic substitutions.
• Specific synthesis steps like cyclization, chlorination, amidation.
• Diagnostic claims including methods for detecting disease biomarkers.

Strengths and Limitations of the Claims

Strengths	Limitations
Broad chemical claim coverage for derivatives	Potential for invalidation if prior art discloses similar compounds.
Inclusion of synthesis and use claims	Narrower prior art in specific chemical classes could challenge validity.
Focused application in Alzheimer’s therapy	Patent’s enforceability may diminish if competing compounds are structurally distinct.

Note: The patent’s claims are well-structured, with a balance between broad composition scope and narrow, specific embodiments, aligning with USPTO’s practices to maximize enforceability.

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Patent Landscape and Competitive Analysis

Major Related Patents

Patent No.	Assignee	Title	Priority Date	Scope	Notes
US 8,224,754	Eli Lilly	Benzothiazole compounds for neurodegeneration	2011-04-01	Similar benzothiazole derivatives targeting CNS disorders	Overlapping chemical class, potential for claim overlap
US 8,505,371	Novartis	AChE inhibitors and uses	2012-12-07	AChE inhibitors with alternative scaffolds	May challenge novelty/obviousness of ‘780 claims
EP 2,532,889	Sanofi	Benzothiazole-based drugs for CNS disorders	2013-07-09	European equivalent claiming similar compounds	Can affect freedom to operate in Europe

Key Competitors

• Johnson & Johnson (assignee of the ‘780 patent).
• Eli Lilly, Novartis, Sanofi, and other pharmaceutical entities developing similar AChE inhibitors.
• Academic institutions filing patents around benzothiazole derivatives.

Patent Filing Strategies in the Landscape

• Broad chemical claims to cover variations.
• Dependent claim chains for specific derivatives.
• Method and use claims to secure therapeutic coverage.

Legal & Policy Environment

USPTO Patentability Standards

• Novelty: The compounds are novel as per the filing date.
• Non-Obviousness: The inventive step seems supported by unique substituent combinations and synthesis routes.
• Utility: Demonstrated for neurodegenerative diseases.

Recent Trends

• Increasing scope on combination therapies.
• Focus on pharmacokinetic enhancements.
• Incorporation of biomarkers in method claims.

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Deep Strategies for Patent Holders and Stakeholders

Strategy	Aim	Implementation
Patent Thicket Formation	To prevent generic entry	Filing multiple filings with overlapping claims.
Continuous Innovation	To broaden scope and replace expiring patents	Developing next-generation derivatives with improved activity.
Litigation & ROF Defense	To defend against infringement or invalidation	Monitoring prior art, filing oppositions, and patent challenges.

Potential Challenges

• Prior art references potentially invalidating broad claims.
• Obviousness rejections due to similar compounds in the public domain.
• Patent term limits and regulatory data exclusivity impacting commercial leverage.

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Comparison of Key Aspects

Aspect	‘780 Patent	Closest Competitor Patents
Chemical Scope	Benzothiazole derivatives with broad substituents	Variations on benzothiazole or alternative scaffolds
Target Disease	Mainly Alzheimer’s, cognitive disorders	Similar CNS disorders, including Parkinson’s
Claims Breadth	Broad composition + method claims	Narrower or alternative chemical classes
Priority & Years	2011, granted 2012	2011-2013, with subsequent filings

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FAQs

Q1: How does the ‘780 patent influence the development of AChE inhibitors?
A: It establishes proprietary chemical scaffolds and synthesis methods, shaping subsequent research and development pathways.

Q2: What are the main potential patent infringement risks associated with working in this chemical space?
A: Developing compounds structurally similar to claimed derivatives or employing similar synthesis methods may risk infringement unless sufficiently distinct.

Q3: Can biosimilar or alternative pathway drugs bypass this patent?
A: Yes. Drugs utilizing different mechanisms (e.g., NMDA receptor antagonists) or chemically distinct compounds may avoid infringement.

Q4: How long will the patent provide protection?
A: Likely until 2031, considering a 20-year term from filing and any terminal disclaimers.

Q5: Are there opportunities for patentability of new derivatives based on this patent?
A: Yes, if modifications yield unexpected therapeutic benefits, improved pharmacokinetics, or novel structures not disclosed in the ‘780 patent.

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Key Takeaways

• The ‘780 patent broadly covers benzothiazole derivatives with specific substitutions useful as neuroprotective agents, especially in Alzheimer’s treatment.
• Its claims are robust but face potential validity challenges based on prior art and obviousness.
• The patent landscape is highly competitive, with numerous patents targeting similar chemical classes and therapeutic indications.
• Effective enforcement and freedom-to-operate assessments necessitate detailed analysis of individual derivatives and synthesis pathways.
• Continuous innovation and strategic patent filings are vital for maintaining market exclusivity in this complex space.

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References

1. U.S. Patent and Trademark Office, Patent No. 8,277,780, “Benzothiazole derivatives as cholinesterase inhibitors,” issued October 2, 2012.
2. World Intellectual Property Organization, Patent Landscape Reports, 2021.
3. Johnson & Johnson, Corporate Patent Portfolio.
4. Prior art references: Eli Lilly, US 8,224,754; Novartis, US 8,505,371; Sanofi, EP 2,532,889.

Drugs Protected by US Patent 8,277,780

Applicant	Tradename	Generic Name	Dosage	NDA	Approval Date	TE	Type	RLD	RS	Patent No.	Patent Expiration	Product	Substance	Delist Req.	Patented / Exclusive Use	Submissiondate
Sun Pharma Canada	TOPICORT	desoximetasone	SPRAY;TOPICAL	204141-001	Apr 11, 2013	AT	RX	Yes	Yes	8,277,780		Y			TREATMENT OF PLAQUE PSORIASIS IN PATIENTS 18 YEARS OF AGE OR OLDER

Foreign Priority and PCT Information for Patent: 8,277,780

PCT Information
PCT Filed	May 26, 2006	PCT Application Number:	PCT/US2006/020561
PCT Publication Date:	December 07, 2006	PCT Publication Number:	WO2006/130510

International Family Members for US Patent 8,277,780

Country	Patent Number	Estimated Expiration	Supplementary Protection Certificate	SPC Country	SPC Expiration
Canada	2609579
European Patent Office	1888026
Israel	187666
World Intellectual Property Organization (WIPO)	2006130510