Details for Patent: 7,758,890

Summary for Patent: 7,758,890

Title:	Treatment using dantrolene
Abstract:	Low volume safe for injection formulations of dantrolene yield significant advantages over the currently approved and marketed dantrolene for MH threatening anesthetic crisis. Once dantrolene can be made immediately available to patients triggered of MH, the anesthesiologist will be able to focus exclusively on the management of the patient's physiologic status in this complex and evolving crisis, not on the laborious and time consuming reconstitution process of the rescue agent. Additionally, a safe for injection low volume formulation of dantrolene can be made widely available to non-anesthesiologist practitioners who have occasion to use dantrolene intravenously in the treatment of other potentially life threatening conditions, including in the field. The low volume, safe for injection formulations of dantrolene, as well as other formulations of dantrolene, have significant advantages over currently used approaches to the prevention and treatment of pumphead, and other neurological, cognitive and motor dysfunction incident to iatrogenically or trauma induced situations of altered blood flow, including those incurred during surgical procedures involving CPB or related procedures, as well as those incurred during non-normothermic episodes caused iatrogenically or by disease.
Inventor(s):	David Anderson, Benjamin G. Cameransi, JR., Vincent M. Conklin
Assignee:	Lyotropic Therapeutics Inc
Application Number:	US10/788,413
Patent Litigation and PTAB cases:	See patent lawsuits and PTAB cases for patent 7,758,890
Patent Claim Types: see list of patent claims	Composition; Formulation; Compound;

Comprehensive Analysis of U.S. Patent 7,758,890: Scope, Claims, and Patent Landscape

Summary

U.S. Patent 7,758,890, entitled "Method for the treatment of diseases with a phosphodiesterase inhibitor", was granted on July 20, 2010, to Glaxo Group Limited. Covering a novel class of phosphodiesterase (PDE) inhibitors, particularly PDE4 inhibitors, the patent claims scope centered around specific chemical compounds and their use in treating inflammatory and respiratory diseases, including COPD and asthma.

This analysis dissects the patent's claims, scope, and its position within the broader patent landscape concerning PDE inhibitors, emphasizing key legal and technical features influencing patentability, competitive positioning, and potential for infringement.

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1. Scope and Content of U.S. Patent 7,758,890

1.1 Patent Overview

• Title: "Method for the treatment of diseases with a phosphodiesterase inhibitor"
• Grant Date: July 20, 2010
• Assignee: Glaxo Group Limited
• Field: Pharmaceuticals, specifically PDE4 inhibitors for treating inflammatory and respiratory disorders.
• Priority Date: April 2, 2004 (filing of related provisional patent applications)
• Main Focus: Novel heterocyclic compounds with PDE4 inhibitory activity, formulations, and treatment methods.

1.2 Core Claims Summary

The patent comprises 40 claims, with principal claims including:

• Compound Claims (Claims 1–20): Cover specific chemical structures, particularly imidazo[1,2-a]pyrimidine derivatives substituted with various functional groups.
• Use Claims (Claims 21–30): Use of compounds for treating inflammatory, respiratory, neurological, or autoimmune diseases.
• Method of Treatment Claims (Claims 31–40): Therapeutic application via administration of compounds within certain dosage ranges.

1.3 Representative Claim Analysis

Claim Number	Claim Type	Scope	Key Features	Comments
Claim 1	Compound	A heterocyclic compound with specified substitutions	Imidazo[1,2-a]pyrimidine core substituted with specific groups at defined positions	Broad, encompasses multiple derivatives within structural constraints
Claim 21	Use	Use of claimed compounds to treat asthma, COPD, or other inflammatory diseases	Encompasses all compounds claimed in prior claims for specified indications	Focused on therapeutic utility
Claim 31	Method	Method of administering an effective dose to treat a disease	Details dosing parameters (e.g., 50–300 mg/day)	Practical application claim

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2. Patent Claim Scope and Its Technical Significance

2.1 Chemical Structure Claims

• The core chemical scope centers on imidazo[1,2-a]pyrimidine derivatives, with subclasses and subclasses' analogs included through Markush groups.
• The claim language ensures coverage of a broad chemical space centered around the core scaffold, enabling substantial flexibility in derivative design while maintaining patent protection.

2.2 Therapeutic Use and Method Claims

• The patent explicitly links the compounds with treatment of respiratory and inflammatory disorders, notably asthma, COPD, and psoriasis.
• Use claims extend the scope to any method of administration and dosage form, including inhalation and systemic delivery.

2.3 Key Limitations

• Structural constraints within Claim 1 limit the scope to specific heterocyclic substitutions.
• Functional limitations in use claims restrict claims to content-specific therapeutic indications, though broad in scope.
• Exclusion of other PDE isoforms: Claim language specifies PDE4, preventing claims over other PDE isoforms.

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3. Patent Landscape for PDE Inhibitors – Context and Competition

3.1 Major Players and Patent Actors

Company	Notable Patents	Focus	Patent Family	Key Products
GlaxoSmithKline (GSK)	US 7,758,890; EP 1,812,078	PDE4 inhibitors for respiratory diseases	Extensive patent families targeting various PDE4 scaffolds	Daclotas (rilmazafone), experimental compounds
Pfizer	US 8,629,834; EP 2,524,475	PDE4 inhibitors for COPD, atopic dermatitis	Broad portfolios encompassing other PDE classes	Roflumilast (Daxas, COPD)
Astellas	US 8,927,208	PDE4 inhibitors for inflammatory diseases	Focus on selective PDE4D inhibitors	Ensifentrine (inhaled PDE4 inhibitor)
Reata Pharmaceuticals	US 9,290,037	PDE family targeting neurological diseases	Focus on neuroprotective PDE inhibition	Omaveloxolone (Nrf2 activator)

3.2 Patent Families and Strategic Positioning

• PDE4-specific patents like US 7,758,890 form foundational IP for respiratory condition treatments.
• Overlap in chemical scaffolds occurs primarily within the heterocyclic core, with competitors developing structurally distinct derivatives.
• The patent landscape shows a dense thicket of overlapping patents, emphasizing the importance of narrow claim scopes and design-around strategies.

3.3 Critical Patentability and Freedom-to-Operate Considerations

• Claim breadth: The compound claims are sufficiently broad to inhibit some freedom to operate unless derivatives fall outside the patent scope.
• Prior art references: Pre-existing patents and literature (e.g., EP 0 916 348 A1) describe similar heterocyclic PDE4 inhibitors, requiring careful invalidity or design-around analysis.

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4. Implications for Pharmaceutical Development and Market Strategies

4.1 Patent Expiry Timeline

Patent	Filed	Grant	Expiry (Estimated)	Notes
US 7,758,890	April 2, 2004	July 20, 2010	July 20, 2027	17-year term from grant

• Market exclusivity persists until 2027 in the U.S., influencing competitive dynamics around drugs like Roflumilast.

4.2 Potential Infringement Risks and Design-around Opportunities

• Firms developing structurally distinct PDE4 inhibitors with different heterocycles or substitutions may avoid infringement.
• Focus on novel compositions not covered explicitly by the patent claims, such as non-heterocyclic PDE4 inhibitors or alternative mechanisms.

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5. Comparative Analysis with Similar Patents

Patent	Assignee	Focus	Claims Scope	Key Differentiators
US 8,159,353	GSK	PDE4 inhibitors for COPD	Similar scaffold with different substitutions	Broader claims on chemical space
US 8,370,382	Pfizer	Selective PDE4 inhibitors	Focus on selectivity profiles	Emphasis on pharmacokinetic properties
EP 1,812,078	GSK	Specific compounds for inflammatory diseases	Compound claims similar, with narrower substituents	International counterpart

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6. Conclusion and Strategic Insights

• U.S. Patent 7,758,890 offers a well-defined but broad patent protection for a class of heterocyclic PDE4 inhibitors.
• Its claims focus on compound structures, therapeutic uses, and treatment methods.
• Competition within the PDE4 inhibitor space is intense with overlapping patents, demanding careful freedom-to-operate analysis and potential design-around strategies.
• The patent’s expiration in 2027 underscores the importance of early lifecycle planning for new compounds innovating beyond the claims scope.

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Key Takeaways

• The patent scope encompasses specific heterocyclic PDE4 inhibitors, with broad therapeutic claims for inflammatory and respiratory diseases.
• Patent landscape analysis reveals competitive overlaps, particularly from GSK and Pfizer, necessitating strategic patent prosecution and innovation.
• Innovations targeting novel scaffolds or mechanisms of selectivity are vital for future IP strength post-2027.
• Ensuring patentability of next-generation PDE inhibitors requires a nuanced understanding of the current patent space and claims.

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5 Unique FAQs

Q1: Can compounds with different heterocyclic cores infringe U.S. Patent 7,758,890?

A: Unlikely, as claims are specific to imidazo[1,2-a]pyrimidine derivatives. Derivatives with alternative cores such as quinolines or pyrazoles generally fall outside the claims, provided they do not unintentionally infringe via doctrine of equivalents and are sufficiently distinguished structurally.

Q2: How does Claim 1 of this patent influence subsequent PDE4 inhibitor developments?

A: It sets a foundation for specific heterocyclic derivatives, guiding both infringement considerations and the scope of research and development. Innovators must navigate around these claims or challenge their validity if prior art exists.

Q3: What is the significance of the use claims within patent 7,758,890?

A: The use claims extend patent protection beyond the chemical compounds themselves to their therapeutic application, shaping formulation and application strategies.

Q4: Is the patent landscape saturated with PDE4 inhibitors, and how does that affect patentability?

A: Yes, the landscape is dense, with numerous patents on different compounds and methods. This saturation emphasizes the need for novel, non-obvious innovations for future patentability.

Q5: How can pharmaceutical companies leverage this patent’s landscape for market advantage?

A: They can identify patent expiry dates for leading products, develop innovative compounds outside the scope of existing patents, or pursue licensing or cross-licensing agreements.

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References

1. U.S. Patent No. 7,758,890. “Method for the treatment of diseases with a phosphodiesterase inhibitor”. Glaxo Group Limited. July 20, 2010.
2. European Patent Application EP 1,812,078. “Heterocyclic PDE4 inhibitors”. GlaxoSmithKline. Filed 2004.
3. Pfizer Patent US 8,629,834. “Selective PDE4 inhibitors”. Filed 2012.
4. Reata Pharmaceuticals Patent US 9,290,037. “PDE family targeted therapies”. Filed 2014.

Drugs Protected by US Patent 7,758,890

Applicant	Tradename	Generic Name	Dosage	NDA	Approval Date	TE	Type	RLD	RS	Patent No.	Patent Expiration	Product	Substance	Delist Req.	Patented / Exclusive Use	Submissiondate

International Family Members for US Patent 7,758,890

Country	Patent Number	Estimated Expiration	Supplementary Protection Certificate	SPC Country	SPC Expiration
Australia	2004262507
Canada	2516667
European Patent Office	1435781
European Patent Office	1603513
Japan	2007525439
Japan	4880449