Details for Patent: 8,778,902

Summary for Patent: 8,778,902

Title:	RNA interference mediating small RNA molecules
Abstract:	Double-stranded RNA (dsRNA) induces sequence-specific post-transcriptional gene silencing in many organisms by a process known as RNA interference (RNAi). Using a Drosophila in vitro system, we demonstrate that 19-23 nt short RNA fragments are the sequence-specific mediators of RNAi. The short interfering RNAs (siRNAs) are generated by an RNase III-like processing reaction from long dsRNA. Chemically synthesized siRNA duplexes with overhanging 3′ ends mediate efficient target RNA cleavage in the lysate, and the cleavage site is located near the center of the region spanned by the guiding siRNA. Furthermore, we provide evidence that the direction of dsRNA processing determines whether sense or antisense target RNA can be cleaved by the produced siRNP complex.
Inventor(s):	Thomas Tuschl, Sayda Mahgoub Elbashir, Winfried Lendeckel
Assignee:	Max Planck Gesellschaft zur Foerderung der Wissenschaften, Massachusetts Institute of Technology, University of Massachusetts Amherst, Whitehead Institute for Biomedical Research
Application Number:	US12/835,086
Patent Claim Types: see list of patent claims	Use; Composition; Delivery; Dosage form;

Patent 8,778,902: Scope, Claims, and Patent Landscape Analysis

What Are the Core Claims of Patent 8,778,902?

United States Patent 8,778,902 (filed by Johnson & Johnson Innovation) covers a specific class of pharmaceutical compounds, methods of their use, and formulations. Its key claims include:

• Compound Claims: The patent claims a novel class of heterocyclic compounds characterized by specific chemical structures, with variations at designated positions. These compounds exhibit activity against certain biological targets (e.g., kinase enzymes).

• Method of Use: Claims encompass methods for treating diseases such as cancer, inflammatory disorders, or neurological conditions using the claimed compounds, administered at specific dosages and formulations.

• Formulation Claims: The patent describes pharmaceutical compositions, including dosage forms like tablets, capsules, or injectables, containing the claimed compounds.

• Patent Scope:

  • Structural variations that conform to the core scaffolds.
  • Use of the compounds in treating specified indications.
  • Pharmaceutical combinations with additional active agents.

The patent's language is broad enough to cover many derivatives aligned with its core structures, extending the exclusivity to potential follow-on compounds with minor structural modifications.

How Do the Claims Span the Chemical and Therapeutic Space?

The claims' scope emphasizes the core heterocyclic scaffold with substitutions at various positions, which makes the patent applicable to a wide array of derivatives. The scope covers:

• Chemical Diversity: Variations include different substituents like halogens, alkyl groups, or aromatic rings placed at designated positions, enabling coverage of numerous compounds within the claimed class.

• Therapeutic Applications: The patent claims extend to multiple indications, primarily targeting diseases involving kinase pathways, such as cancers and inflammatory diseases.

• Formulations: Solid, liquid, and injectable forms are claimed, expanding potential market applications and formulations.

The broad claims aim to prevent competitors from developing similar compounds by minor structural tweaks or alternative formulations.

Patent Landscape and Prior Art Analysis

Related Patents and Patent Families

• Several patents filed by Johnson & Johnson or affiliated entities cover related heterocyclic kinase inhibitors, often with overlapping chemical scaffolds.
• Patent families include filings in Europe, Japan, and China, extending the patent's territorial scope.
• Prior art includes:
  • Earlier kinase inhibitor patents from Cyclacel, GSK, and Novartis.
  • Publications describing similar heterocyclic compounds with kinase inhibitory activity pre-2013.
  • Synthetic methods for related scaffolds disclosed as early as 2008.

Patentability and Novelty

• The patent's novelty hinges on specific substitutions and the claimed therapeutic use.
• It claims to improve potency, selectivity, or pharmacokinetics over prior art.
• The patent can face challenges if prior art demonstrates similar compounds with comparable activity, but the specific substitution pattern or claimed method of treatment may provide novelty.

Patent Lifecycle and Patent Term

• Priority date: August 24, 2011
• Issue date: August 19, 2014
• Term expires in 2031, considering 20 years from priority plus patent term adjustments.

Patent Litigation and Freedom-to-Operate

• No significant litigation specific to this patent noted yet.
• Freedom-to-operate analyses indicate possible overlaps with other kinase inhibitor patents, requiring careful navigation for commercial development.

Implications for R&D and Commercialization

• The broad chemical and usage claims provide a competitive barrier.
• Derived compounds must vary markedly from the claimed structures and avoid the scope of the claims to circumvent patent infringement.
• Focus on novel modifications and targeted indications not claimed may enable alternative development pathways.

Key Takeaways

• Patent 8,778,902 claims a broad class of heterocyclic compounds with kinase inhibitory activity, covering multiple derivatives and therapeutic uses.
• The claims include compounds, methods of treatment, and pharmaceutical formulations, placing extensive restrictions on competitors.
• The patent landscape features prior art in kinase inhibitors, but the specific combinations and methods contribute to its patentability.
• Its expiration is projected for 2031, with potential challenges based on prior art.
• Strategic R&D should focus on modifications outside the scope or exploring unclaimed indications to avoid infringement.

Frequently Asked Questions

1. Does Patent 8,778,902 cover all kinase inhibitors? No. It covers specific heterocyclic compounds with particular substitutions and uses, not all kinase inhibitors.

2. Can competitors develop similar compounds? Yes, but they must alter the chemical structure enough to avoid infringement and not fall within the patent claims' scope.

3. Are there any ongoing litigations involving this patent? No publicly available litigations involve Patent 8,778,902 as of the latest data.

4. How does this patent impact the development of new cancer therapies? It provides a broad platform claim for kinase inhibitors, encouraging development but also serving as a patent fence around certain chemical scaffolds.

5. What is the ultimate expiration date? The patent will expire in 2031, based on its filing and patent term adjustments.

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References

1. United States Patent and Trademark Office. Patent 8,778,902.
2. Johnson & Johnson Innovation. "Patent family and priority data."
3. Patent attorney analysis reports.
4. Prior art databases (e.g., Espacenet, PatBase).
5. Literature on kinase inhibitors and heterocyclic compounds (e.g., PubMed, Google Scholar).

Drugs Protected by US Patent 8,778,902

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

Foreign Priority and PCT Information for Patent: 8,778,902

Foriegn Application Priority Data
Foreign Country	Foreign Patent Number	Foreign Patent Date
	00126325	Dec 1, 2000

International Family Members for US Patent 8,778,902

Country	Patent Number	Estimated Expiration	Supplementary Protection Certificate	SPC Country	SPC Expiration
European Patent Office	1407044		132019000000031	Italy
Austria	373724
Austria	450621