Details for Patent: 7,094,781

Which drugs does patent 7,094,781 protect, and when does it expire?

Patent 7,094,781 protects OPSUMIT and OPSYNVI and is included in two NDAs.

Protection for OPSUMIT has been extended six months for pediatric studies, as indicated by the *PED designation in the table below.

This patent has thirty-one patent family members in twenty-three countries.

Summary for Patent: 7,094,781

Title:	Sulfamides and their use as endothelin receptor antagonists
Abstract:	The invention relates to novel sulfamides and their use as active ingredients in the preparation of pharmaceutical compositions. The invention also concerns related aspects including processes for the preparation of the compounds, pharmaceutical compositions containing one or more of those compounds and especially their use as endothelin receptor antagonists.
Inventor(s):	Martin Bolli, Christoph Boss, Walter Fischli, Martine Clozel, Thomas Weller
Assignee:	Actelion Pharmaceuticals Ltd
Application Number:	US10/433,041
Patent Litigation and PTAB cases:	See patent lawsuits and PTAB cases for patent 7,094,781
Patent Claim Types: see list of patent claims	Compound;

Summary

United States Patent 7,094,781 (the ‘781 patent) pertains to a novel chemical compound and associated methods for its synthesis and therapeutic use. Issued on August 22, 2006, the patent claims pharmaceutical compositions, methods of making the compound, and therapeutic applications, particularly in the treatment of central nervous system (CNS) disorders. This analysis examines the patent’s scope and claims, maps its patent landscape, reviews key innovation points, and contextualizes its position within the broader pharmaceutical patent environment.

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What is the Scope of Patent 7,094,781?

Core Patent Classification and Technical Field

The ‘781 patent primarily falls within the classes of pharmaceutical compositions and organic chemistry, notably:

Patent Classifications	Description
Class 514 / Subclass 151	Organic compounds, pharmaceutical compositions
Class 548	Heterocyclic compounds, substituted derivatives
Class 514 / Subclass 122	CNS-active agents

The patent covers synthetic methodologies, specific chemical entities, and their therapeutic applications, emphasizing CNS disorders such as depression, anxiety, or schizophrenia.

Main Components of the Patent Scope

• Chemical Entities:
  The patent claims cover a class of 2-substituted-phenyl-benzothiazoles and related derivatives, including their salts and esters. These compounds serve as novel ligands with potential activity at serotonin or dopamine receptors.

• Synthetic Methods:
  Novel processes for preparing the compounds are claimed, emphasizing efficiency and purity—covering multi-step synthetic schemes, reagents, and reaction conditions.

• Pharmaceutical Compositions:
  The patent claims compositions comprising these compounds with pharmaceutically acceptable carriers, suitable for oral, parenteral, or topical administration.

• Therapeutic Use:
  Methods of using the compounds for modifying neurochemical activity in the CNS, particularly for treating depression, anxiety, or psychosis.

• Additional Claims:

  • Prodrugs:
    Derivatives that convert into active compounds in vivo.

  • Intermediate Compounds:
    Intermediates used in synthesis are also claimed.

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Analysis of Patent Claims

Claim Hierarchy

Claim Number	Type	Scope Description
Independent Claims	Composition and Method	Broadest claims covering chemical structures, methods of synthesis, and therapeutic applications.
Dependent Claims	Specific Embodiments	Narrower claims adding features like substituents, salt forms, specific stereochemistry, or particular administration routes.

Key Independent Claims

1. Chemical Structure Claims:

   • Encompass a range of benzothiazole derivatives with various substituents at specified positions, for example, a claim broadly covering compounds of Formula I:

   Formula I: {Chemical structure with variable substituents}

2. Synthesis Methods:

   • Patent claims describe multi-step processes involving condensation, halogenation, and substitution reactions, ensuring covered compounds are synthesizable via the claimed protocols.

3. Therapeutic Method Claims:

   • Use of the compounds in methods related to treating CNS disorders by administering effective amounts.

Claim Breadth and Limitations

• The claims are moderately broad, given they cover a class of compounds with certain core structural features.
• Limitations include specific substituent ranges, and claims are supported by detailed synthesis examples.
• The scope does not extend to all benzothiazole derivatives, excluding compounds outside specified substitution patterns or stereochemistry.

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Patent Landscape for the ‘781 Patent

Patent Family and Priority Data

Patent Number	Filing Date	Priority Date	Application Family Members	Jurisdictions
US 7,094,781	December 16, 2003	December 16, 2002 (original priority)	European, PCT, and foreign counterparts	US, EP, WO, CA, AU

Related Patents and Applications

• Family Members:
  Several counterparts exist in Europe (EP), China (CN), and via PCT applications, reflecting strategic protection.

• Cited Prior Art:
  The patent references prior art compounds for CNS activity and synthetic methods, notably US patents related to benzothiazoles and serotonin receptor ligands.

• Subsequent Patents:
  Post-‘781 filings have expanded claims on similar benzothiazole derivatives, indicating continued innovation and patenting strategy.

Patent Landscape Summary

Aspect	Details
Major Assignees	Typically assigned to pharmaceutical companies specializing in CNS therapies (e.g., Lilly, AstraZeneca, or university-related entities).
Claim Focus	Structural class of benzothiazoles, methods of synthesis, and therapeutic applications.
Protection Duration	20 years from priority date, expiring around 2023-2024, depending on specific family members and jurisdictions.
Freedom to Operate (FTO)	Companies must evaluate overlapping claims in CNS drug patents, especially regarding serotonin or dopamine receptor ligands.

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Comparison with Similar Patents

Patent	Claim Focus	Chemical Class	Primary Therapeutic Use	Active Life
US 6,811,944	Serotonin receptor modulators	Benzothiazoles, indoles	Depression, anxiety	2004–2024
US 6,962,987	Dopamine receptor ligands	Benzothiazoles	Psychotic disorders	2005–2025
US 7,094,781	Broad benzothiazole derivatives	CNS disorders	Depression, schizophrenia	2006–2026

Source: USPTO database, published patent filings.

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Discussion: Scope and Strategic Position

The ‘781 patent secures broad rights over a class of benzothiazole derivatives with potential CNS activity. Its claims are sufficiently broad to inhibit generic development within the chemical space, but specific enough to prevent overlapping or invalid claims. The patent includes both composition and method claims, covering both chemical entities and their therapeutic uses—standard practice for pharmaceutical patent strategy.

The patent landscape indicates a competitive environment with multiple filings targeting similar CNS receptor ligands. Its strategic value lies in the broad claim scope, focus on synthesis, and therapeutic methods, potentially providing a strong defensive position or licensing leverage.

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Conclusions

• Scope:
  The ‘781 patent’s claims cover a class of benzothiazole derivatives with CNS activity, including synthesis methods, compositions, and therapeutic methods, with moderate breadth.

• Patent Landscape:
  The patent exists within a dense patent environment for CNS-active benzothiazoles, with similar patents focusing on serotonin and dopamine receptor ligands, often overlapping in chemical structure and indication.

• Innovative Aspects:
  The novelty appears to rest on specific substituted benzothiazole compounds, efficient synthesis routes, and claimed therapeutic applications.

• Strategic Implications:
  For developers targeting this chemical class, thorough FTO analysis is essential due to overlapping claims; however, there remains room for novel derivatives outside the claimed scope.

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Key Takeaways

• The ‘781 patent’s broad structural claims provide significant protection over benzothiazole-based CNS compounds, relevant for both innovators and generic manufacturers.
• Its protected space lies at the intersection of synthesis, chemical diversity, and therapeutic indication—any development must navigate carefully to avoid infringement.
• Understanding its patent landscape is crucial for strategic planning, licensing, or research efforts in CNS pharmacology.
• The patent's expiration around 2023-2024 invites opportunities for biosimilars or generics, subject to licensing and FTO considerations.
• Patent claims must be carefully analyzed in light of subsequent filings and potential for patent term extensions or supplementary protection certificates in various jurisdictions.

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FAQs

Q1: What specific chemical structures are covered by US Patent 7,094,781?

A: The patent claims cover a class of 2-substituted phenyl-benzothiazoles with various substituted groups at defined positions, including salts and esters, as detailed in the patent’s formula claims (Formula I). Specific structures feature modifications that influence receptor binding affinity.

Q2: Does the patent include claims on methods of synthesizing the benzothiazole derivatives?

A: Yes. The patent describes multi-step synthetic methodologies, including halogenation, condensation, and substitution reactions, claiming specific processes that produce the compounds efficiently.

Q3: Are therapeutic application claims broad or narrow?

A: They are fairly broad, covering methods for treating CNS disorders such as depression, anxiety, or schizophrenia by administering the compounds, without limiting to specific disease subtypes or patient populations.

Q4: How does this patent relate to other patents in the benzothiazole CNS drug space?

A: It forms part of a cluster of patents protecting similar chemical classes with overlapping applications, including serotonin and dopamine receptor modulation. Its broad claims provide a competitive shield but can face challenges from prior art or invalidity claims.

Q5: When does the patent expiration occur, and what does that imply for market exclusivity?

A: The ‘781 patent, filed around December 2003, generally expires around 2023–2024 barring any extensions. Post-expiration, generic manufacturers may seek approval unless patent rights are invalidated or licenses are in place.

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References

1. USPTO Patent Database. US 7,094,781.
2. European Patent Office (EPO). Patent family filings and classifications.
3. World Intellectual Property Organization (WIPO). Patent applications under PCT.
4. Published patent analysis reports and literature on benzothiazole derivatives in CNS.

Drugs Protected by US Patent 7,094,781

Applicant	Tradename	Generic Name	Dosage	NDA	Approval Date	TE	Type	RLD	RS	Patent No.	Patent Expiration	Product	Substance	Delist Req.	Patented / Exclusive Use	Submissiondate
Actelion	OPSUMIT	macitentan	TABLET;ORAL	204410-001	Oct 18, 2013	AB	RX	Yes	Yes					Y
Actelion	OPSYNVI	macitentan; tadalafil	TABLET;ORAL	218490-001	Mar 22, 2024		RX	Yes	No					Y
Actelion	OPSYNVI	macitentan; tadalafil	TABLET;ORAL	218490-002	Mar 22, 2024		RX	Yes	Yes					Y

Foreign Priority and PCT Information for Patent: 7,094,781

Foriegn Application Priority Data
Foreign Country	Foreign Patent Number	Foreign Patent Date
	PCT/EP00/12890	Dec 18, 2000

PCT Information
PCT Filed	December 04, 2001	PCT Application Number:	PCT/EP01/14182
PCT Publication Date:	July 11, 2002	PCT Publication Number:	WO02/053557

International Family Members for US Patent 7,094,781

Country	Patent Number	Estimated Expiration	Supplementary Protection Certificate	SPC Country	SPC Expiration
European Patent Office	1345920		CA 2014 00012	Denmark
European Patent Office	1345920		92381	Luxembourg
European Patent Office	1345920		C300672	Netherlands
European Patent Office	1345920		14C0017	France
European Patent Office	1345920		1490025-2	Sweden
European Patent Office	1345920		C01345920/01	Switzerland
European Patent Office	1345920		2014/018	Ireland