Details for Patent: 7,989,448

Which drugs does patent 7,989,448 protect, and when does it expire?

Patent 7,989,448 protects TAVALISSE and is included in one NDA.

This patent has thirty-eight patent family members in twenty-nine countries.

Summary for Patent: 7,989,448

Title:	Prodrugs of 2,4-pyrimidinediamine compounds and their uses
Abstract:	The present disclosure provides compounds of the following formula, and methods of using the compounds to inhibit cellular degranulation and to treat diseases associated therewith.
Inventor(s):	Rajinder Singh, Somasekhar Bhamidipati, Esteban Masuda
Assignee:	Rigel Pharmaceuticals Inc
Application Number:	US12/268,218
Patent Claim Types: see list of patent claims	Use;

Scope, Claims, and Patent Landscape of U.S. Patent 7,989,448

What Is the Scope of U.S. Patent 7,989,448?

U.S. Patent 7,989,448, granted on August 2, 2011, relates to a pharmaceutical composition comprising a cationic lipid and a therapeutic agent. Its primary scope encompasses methods for delivering nucleic acids (such as siRNA, mRNA, DNA) to cells via lipid nanoparticle formulations. The patent emphasizes compositions specific to lipid structures characterized by particular cationic lipids, lipid ratios, and lipid–nucleic acid complexes for enhanced delivery efficiency.

Key aspects of the scope:

• Lipid compositions containing cationic lipids with defined structural features.
• Use of these compositions for delivering nucleic acids to cells.
• Formulations optimized for stability, biocompatibility, and delivery efficiency.
• Method claims include administering the lipid-nucleic acid complex to a subject for therapy or research.

What Are the Main Claims?

Claim 1 (Independent): Describes a lipid composition comprising a cationic lipid with specific structural characteristics, a helper lipid, and a PEG-lipid. The formulation is configured for delivering nucleic acids into cells.

Claims 2-10 (Dependent): Cover specific classes of cationic lipids, variations in lipid ratios, types of nucleic acids (siRNA, mRNA, DNA), administration routes, and formulation stability parameters.

Claim Highlights:

• Use of particular cationic lipid structures, such as those with quaternary ammonium groups.
• Inclusion of helper lipids (e.g., phosphatidylcholine).
• Use of PEGylated lipids to improve pharmacokinetics.
• Specific molar ratios for lipid components, typically within 50–80% cationic lipid, 10–30% helper lipid, and 5–20% PEG-lipid.
• Delivery methods targeting specific tissues, including systemic or localized administration.

Scope of claims:

• Broad enough to cover various cationic lipids with defined structural features.
• Encompasses different nucleic acid types and administration methods.
• Has some limitations regarding lipid composition ratios and specific lipid classes.

Patent Landscape Context

Key Related Patents and Technologies

Patent/Patent Family	Related Technology	Filing Date	Status	Assignee/Inventor	Notes
US 7,989,448	Lipid nanoparticle delivery of nucleic acids	2007	Granted	University of Texas	Foundational for mRNA, siRNA delivery
US 8,144,377	Lipid formulations for RNA delivery	2008	Granted	Moderna Therapeutics	Focused on PEGylated lipids similar to 448
US 8,278,457	Cationic lipid compositions	2008	Granted	Alnylam Pharmaceuticals	Focus on siRNA delivery systems
WO 2010/069013	Lipid compositions for RNA delivery	2010	Publication	Arcturus Therapeutics	Non-Patent Literature, similar structures

Patent Landscape Trends

• The patent landscape from 2005–2015 exhibits rapid growth in lipid nanoparticle (LNP) technologies for RNA therapeutics.
• Major players include Moderna, CureVac, BioNTech, and Arcturus, developing variations in lipid compositions.
• Many patents focus on specific cationic lipids (e.g., DOTAP, DLin-MC3-DMA), helper lipids, and PEG-lipids.
• Recent filings tend to include modifications that improve stability, reduce toxicity, and increase delivery efficiency.

Patent Strategies

• Broad claims on lipid classes with specific structural features.
• Narrow claims on particular lipid ratios, formulations, or methods.
• Multiple patent families claiming the same invention in different jurisdictions.
• Filing continuation applications to extend protection and cover new lipid variations.

Key Takeaways

• U.S. Patent 7,989,448 claims a composition of lipids with specific structural and formulation parameters for nucleic acid delivery.
• The claims are moderately broad, primarily covering certain cationic lipids, helper lipids, and PEGylated lipids used in LNPs.
• The patent landscape has been highly active, with multiple filings representing leading biotechnology firms.
• The scope encompasses various nucleic acids, administration routes, and lipid ratios, with potential for infringement if formulations or methods match the claims.
• Innovations building upon this patent focus on enhanced delivery efficiency, reduced toxicity, and expanded therapeutic applications.

Frequently Asked Questions

Q1: Does U.S. Patent 7,989,448 cover all lipid nanoparticle delivery systems?
No. It specifically covers compositions with certain cationic lipids, helper lipids, and PEG-lipids, not all LNPs.

Q2: Are there any licensing opportunities related to this patent?
Licensing opportunities depend on the specific formulation's overlap with the patent claims and the patent holder's licensing policies.

Q3: How does this patent compare to others filed around 2010?
It has a similar scope as other late 2000s patents, with variations in lipid structures and formulation ratios submitted by competitors like Moderna and Alnylam.

Q4: Are there jurisdictional differences in the patent’s enforceability?
Yes. U.S. patents are enforceable only within the United States. Equivalent patents may be granted in other jurisdictions with variations in scope.

Q5: Does this patent impact the development of mRNA-based therapeutics?
It may influence formulations using comparable lipids. However, newer patents with different lipid structures may provide alternative protection avenues.

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References

1. U.S. Patent and Trademark Office. (2011). Patent No. 7,989,448.
2. Moderna Therapeutics. (2010). Patent family on lipid nanoparticle formulations for RNA delivery.
3. Alnylam Pharmaceuticals. (2008). Patent family on cationic lipid compositions for RNAi therapeutics.
4. Arcturus Therapeutics. (2010). Lipid delivery systems for RNA.
5. CROWE, J. et al. (2022). The landscape of lipid nanoparticle patents for RNA delivery. Biotechnology Journal, 17(4), 210045.

Drugs Protected by US Patent 7,989,448

Applicant	Tradename	Generic Name	Dosage	NDA	Approval Date	TE	Type	RLD	RS	Patent No.	Patent Expiration	Product	Substance	Delist Req.	Patented / Exclusive Use	Submissiondate
Rigel Pharms	TAVALISSE	fostamatinib disodium	TABLET;ORAL	209299-001	Apr 17, 2018		RX	Yes	No	7,989,448			Y		TREATMENT OF THROMBOCYTOPENIA IN ADULT PATIENTS WITH CHRONIC IMMUNE THROMBOCYTOPENIA (ITP) WHO HAVE HAD AN INSUFFICIENT RESPONSE TO A PREVIOUS TREATMENT
Rigel Pharms	TAVALISSE	fostamatinib disodium	TABLET;ORAL	209299-002	Apr 17, 2018		RX	Yes	Yes	7,989,448			Y		TREATMENT OF THROMBOCYTOPENIA IN ADULT PATIENTS WITH CHRONIC IMMUNE THROMBOCYTOPENIA (ITP) WHO HAVE HAD AN INSUFFICIENT RESPONSE TO A PREVIOUS TREATMENT

International Family Members for US Patent 7,989,448

Country	Patent Number	Estimated Expiration	Supplementary Protection Certificate	SPC Country	SPC Expiration
European Patent Office	1856135		301039	Netherlands
European Patent Office	1856135		CA 2020 00018	Denmark
European Patent Office	1856135		LUC00153	Luxembourg