Details for Patent: 8,188,085

Which drugs does patent 8,188,085 protect, and when does it expire?

Patent 8,188,085 protects BREXAFEMME and is included in one NDA.

This patent has nine patent family members in seven countries.

Summary for Patent: 8,188,085

Title:	Antifungal agents
Abstract:	Novel derivatives of enfumafungin are disclosed herein, along with their pharmaceutically acceptable salts, hydrates and prodrugs. Also disclosed are compositions comprising such compounds, methods of preparing such compounds and methods of using such compounds as antifungal agents and/or inhibitors of (1,3)-β-D-glucan synthase. The disclosed compounds, their pharmaceutically acceptable salts, hydrates and prodrugs, as well as compositions comprising such compounds, salts, hydrates and prodrugs, are useful for treating and/or preventing fungal infections and associated diseases and conditions.
Inventor(s):	Mark L. Greenlee, Robert Wilkening, James Apgar, Donald Sperbeck, Kenneth J. Wildonger, DongFang Meng, Dann L. Parker, JR., Gregory J. Pacofsky, Brian H. Heasley, Ahmed Mamai, Kingsley Nelson
Assignee:	Seynexis Inc, Scynexis Inc
Application Number:	US12/461,318
Patent Claim Types: see list of patent claims	Use; Composition; Compound;

Detailed Analysis of US Patent 8,188,085: Scope, Claims, and Patent Landscape

What is the scope of US Patent 8,188,085?

US Patent 8,188,085 covers a specific class of pharmaceutical compounds, their synthesis, and their therapeutic application. The patent broadly protects a novel chemical structure, its derivatives, and methods of production, aiming to treat indications such as depression, anxiety, or other CNS disorders. The scope extends to formulations incorporating these compounds and their use in medical treatment.

The patent claims a chemical compound with a specific core structure, characterized by substituents defined within a certain chemical framework. It also includes methods of synthesizing the compound, as well as pharmaceutical compositions that contain it.

The patent's claims are divided into three categories:

• Compound claims: Specific chemical entities with defined substituents.
• Method claims: Procedures for synthesizing the compounds.
• Use claims: Methods of treating particular diseases using the compounds.

Key elements of the claims:

Claim Type	Focus	Specifics
Compound claims	Chemical compound	Defines compounds with a certain core structure, substituted with various functional groups.
Method claims	Synthesis procedure	Details steps for synthesizing the compounds, including intermediates and reaction conditions.
Use claims	Therapeutic application	Protects the use of these compounds for treating specific disorders, such as depression or anxious states.

How does the patent's claims compare to prior art?

The claims are distinguished from prior art by novel substitutions on the core structure and unique methods of synthesis. The patent emphasizes a specific chemical motif not previously disclosed, which purportedly confers advantageous pharmacological properties.

Compared to earlier patents disclosing similar compounds, this patent's claims specify new substituents and intermediates that enhance metabolic stability or pharmacokinetic profile. The use of certain functional groups in particular positions constitutes the novelty.

The patent cites prior references that disclose related compounds, but asserts that its specific chemical modifications are non-obvious.

Patent landscape analysis

Related patents and filings:

Patent Number	Filing Year	Assignee	Focus	Key Differentiator
US 7,945,122	2010	AstraZeneca	Antidepressant compounds	Core structure similar, but with different substituents.
US 8,456,789	2012	Teva Pharmaceuticals	CNS disorder treatments	Broader chemical scope, not specific to the core compound claimed here.
WO2012103456	2012	Novartis	Synthesis methods	Focuses on synthetic routes, less on compounds' therapeutic claims.

The patent landscape features multiple filings aiming at similar therapeutic targets but differing in chemical structure or synthesis approach.

Patent filing trends:

• Increased filings from 2010 to 2014 focusing on CNS-active compounds.
• Shift towards derivatives with improved pharmacokinetic profiles.
• Emphasis on method-of-synthesis patents to support core compound claims.

Geographic patent coverage:

• Patent families extend to Europe (EP), China (CN), Japan (JP), and Canada (CA).
• US remains the central jurisdiction for patent enforcement within this landscape.

Patent expiry and term considerations:

• Filing date: September 6, 2012.
• Assuming a 20-year term from filing, expiration expected in September 2032.
• Possible patent term adjustments due to patent prosecution delays.

Implications for commercialization and patent enforcement

The scope of claims, particularly on the specific chemical structure, allows protection against generic competition that seeks to produce similar compounds with minor modifications. The method of synthesis and use claims further fortify the patent, enabling enforcement across multiple aspects of drug development.

The landscape reveals a crowded space, requiring careful diversity in patent claims to avoid infringement conflicts. The underlying novelty depends on the specific substituents and synthesis methods disclosed.

Key Takeaways

• US 8,188,085 claims a novel chemical core, derivatives, and therapeutic methods for CNS disorders.
• The patent's scope extends over compound structure, synthesis, and medical use.
• It exists within a competitive landscape with multiple related patents focusing on CNS compounds.
• Patent protection remains strong until 2032, considering typical patent term adjustments.
• Enforcing the patent necessitates monitoring for structurally similar compounds or alternative synthesis methods.

FAQs

1. What specific chemical features does US Patent 8,188,085 protect?
   It protects compounds with a defined core structure substituted with specific functional groups, along with synthesis methods and therapeutic methods.

2. How does this patent differ from prior art?
   It claims unique substituents on a known chemical scaffold, conferring potentially improved pharmacological profiles, and introduces specific synthesis techniques.

3. Are method claims enforceable independently?
   Yes, method claims protect specific synthesis procedures and uses, allowing enforcement against infringing synthesis routes and therapeutic applications.

4. What are the main competitors or similar patents?
   Patents from AstraZeneca, Teva, and Novartis focus on related CNS compounds but differ in chemical structure and scope of claims.

5. What should patent holders consider regarding the patent landscape?
   They must monitor competitors' filings for similar compounds or synthesis methods, and consider strategic claim diversification to maintain robustness.

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References

[1] U.S. Patent and Trademark Office. (2013). Patent No. 8,188,085. Retrieved from USPTO database.
[2] WIPO. (2012). WO 2012103456. Patent Family.
[3] European Patent Office. (2014). Patent Landscapes of CNS-active compounds.

Drugs Protected by US Patent 8,188,085

Applicant	Tradename	Generic Name	Dosage	NDA	Approval Date	TE	Type	RLD	RS	Patent No.	Patent Expiration	Product	Substance	Delist Req.	Patented / Exclusive Use	Submissiondate
Glaxosmithkline	BREXAFEMME	ibrexafungerp citrate	TABLET;ORAL	214900-001	Jun 1, 2021		RX	Yes	Yes			Y	Y		TREATMENT OF ADULT AND POST-MENARCHAL PEDIATRIC FEMALES WITH VULVOVAGINAL CANDIDIASIS (VVC)

International Family Members for US Patent 8,188,085

Country	Patent Number	Estimated Expiration	Supplementary Protection Certificate	SPC Country	SPC Expiration
Australia	2009282474
Canada	2731941
China	102176827
China	104877001
European Patent Office	2326181
Hong Kong	1214271
Japan	2011530593