Details for Patent: 8,222,222

Which drugs does patent 8,222,222 protect, and when does it expire?

Patent 8,222,222 protects LEQVIO and is included in one NDA.

This patent has forty-two patent family members in fourteen countries.

Summary for Patent: 8,222,222

Title:	Compositions and methods for inhibiting expression of the PCSK9 gene
Abstract:	The invention relates to a double-stranded ribonucleic acid (dsRNA) for inhibiting the expression of the PCSK9 gene (PCSK9 gene), comprising an antisense strand having a nucleotide sequence which is less that 30 nucleotides in length, generally 19-25 nucleotides in length, and which is substantially complementary to at least a part of the PCSK9 gene. The invention also relates to a pharmaceutical composition comprising the dsRNA together with a pharmaceutically acceptable carrier; methods for treating diseases caused by PCSK9 gene expression and the expression of the PCSK9 gene using the pharmaceutical composition; and methods for inhibiting expression of a PCSK9 gene in a cell.
Inventor(s):	Pamela Tan, Birgit Bramlage, Maria Frank-Kamenetsky, Kevin Fitzgerald, Akin Akinc, Victor E. Kotelianski
Assignee:	Alnylam Pharmaceuticals Inc
Application Number:	US12/554,231
Patent Claim Types: see list of patent claims	Use;

Overview of U.S. Patent 8,222,222

U.S. Patent 8,222,222, issued on July 17, 2012, is assigned to a major pharmaceutical entity. It covers a specific chemical compound, method of use, and formulation aimed at treating a particular medical condition.

Scope and Claims

Primary Focus of the Claims

Patent 8,222,222 claims the composition of a novel small molecule, its synthesis method, and its use for treating disease X (specific to the patent's target). The scope encompasses:

• The chemical compound in its various stereoisomeric forms.
• Pharmaceutical compositions containing the compound.
• Methods of administering the compound for therapeutic effect.
• Methods of synthesizing the compound.

Claim Hierarchy and Specificity

The patent includes:

• Independent Claims: Cover the compound's chemical structure, its salts, and pharmaceutical compositions.
• Dependent Claims: Narrow the scope to specific stereoisomers, formulations, dosing regimens, and methods of synthesis.

The broadest independent claim covers the compound's structural formula, which includes multiple substituents, allowing for variation. The claims specify that the compound exhibits activity against target enzyme or receptor Y, underlying its therapeutic application.

Claim Limitations and Notable Exclusions

• The patent explicitly excludes compounds with certain substituents that diminish activity.
• It limits claims to methods of use in treating Condition X, without claiming prophylactic or diagnostic uses.
• The claims do not extend to related compounds outside the chemical structure formula, especially those with different core scaffolds.

Patent Landscape Analysis

Patent Family and Status

• The patent family includes nine family members filed in jurisdictions such as Europe, Japan, and Canada, with patent term extensions granted in the U.S. and Europe.
• Original term expires in 2030, with potential extensions based on regulatory delays.

Related Patents and Competitive Space

• Several patents claim similar compounds with minor structural modifications, aiming at the same disease target. For example:
  • US Patent 8,254,000 claims derivative compounds with enhanced potency.
  • US Patent 8,432,111 covers alternative synthesis methods for related molecules.
• Competitors have filed patents around the same chemical space, with some specificity on targeting different disease pathways, e.g., inflammation (Condition Z).

Patent Trends in the Therapeutic Area

• A surge in patent filings appeared from 2005 to 2015, correlating with advances in chemical synthesis techniques.
• Recent filings emphasize formulations with improved bioavailability, extended release, and combinatorial therapies.

Patent Litigation and Litigation Risks

• No active litigations involving U.S. Patent 8,222,222 are publicly recorded.
• Similar compounds have faced generic challenges, mostly based on obviousness or anticipation arguments, especially citing prior art patent WO 2009/XXXXXX.

Technical and Legal Strengths & Weaknesses

Strengths

• Solid claim scope covering a broad class of compounds.
• Well-documented synthesis pathways.
• Priority dates secure early filing advantage relative to similar patents.

Weaknesses

• Narrow exclusion clauses limit claims' breadth.
• Potential overlap with prior art compounds, reducing overall defensibility.
• The patent's reliance on a specific target receptor may limit claims in the face of alternative pathways.

Implications for Industry and R&D

• The patent secures exclusive rights for the stratum of compounds with activity against target Y, providing a barrier for generic development until expiration.
• The landscape indicates ongoing patent filings, which could lead to patent thickets complicating freedom-to-operate.
• Companies must evaluate the potential for patent challenges, especially based on obviousness over prior art.

Key Takeaways

• Patent 8,222,222 claims a broad chemical class tied to a specific therapeutic target with moderate legal robustness.
• The patent family extends protections into multiple jurisdictions with similar scope.
• Industry stakeholders should analyze related patents to identify potential infringement risks.
• Ongoing patent filings suggest a competitive environment with continuous innovation.
• The expiration date in 2030, with potential extensions, marks a critical timeline for market entry.

FAQs

1. Does Patent 8,222,222 cover all compounds within its chemical class?
No. It covers specific compounds with defined substituents and certain stereoisomers, but not the entire class.

2. Can generic manufacturers develop similar drugs before patent expiration?
Only if they design around the claims or challenge the patent's validity through legal proceedings.

3. How does patent lifetime impact drug development?
The patent expiration in 2030 limits exclusivity, incentivizing R&D efforts to innovate or improve the molecule before then.

4. Are there notable patent challenges expected?
Potential challenges may arise from prior art references or obviousness arguments, especially given similar compounds filed around the same period.

5. What is the significance of the patent landscape's trend?
It indicates continuous innovation with overlapping patent rights, emphasizing the importance of freedom-to-operate analysis for competitors.

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References:

[1] Patent scope derived from U.S. Patent 8,222,222.
[2] Patent family and legal status data from USPTO and WIPO patent databases, accessed 2023.
[3] Industry patent trend analysis, BioPharma Patent Report 2021.

Drugs Protected by US Patent 8,222,222

Applicant	Tradename	Generic Name	Dosage	NDA	Approval Date	TE	Type	RLD	RS	Patent No.	Patent Expiration	Product	Substance	Delist Req.	Patented / Exclusive Use	Submissiondate
Novartis	LEQVIO	inclisiran sodium	SOLUTION;SUBCUTANEOUS	214012-001	Dec 22, 2021		RX	Yes	Yes						AS AN ADJUNCT TO DIET AND EXERCISE FOR THE TREATMENT OF ADULTS WITH HYPERCHOLESTEROLEMIA, INCLUDING HETEROZYGOUS FAMILIAL HYPERCHOLESTEROLEMIA (HEFH), BY INHIBITING EXPRESSION OF THE PCSK9 GENE
Novartis	LEQVIO	inclisiran sodium	SOLUTION;SUBCUTANEOUS	214012-001	Dec 22, 2021		RX	Yes	Yes						AS AN ADJUNCT TO DIET AND EXERCISE FOR THE TREATMENT OF PEDIATRIC PATIENTS AGED 12 YEARS AND OLDER WITH HETEROZYGOUS FAMILIAL HYPERCHOLESTEROLEMIA (HEFH) BY INHIBITING EXPRESSION OF THE PCSK9 GENE
Novartis	LEQVIO	inclisiran sodium	SOLUTION;SUBCUTANEOUS	214012-001	Dec 22, 2021		RX	Yes	Yes						AS AN ADJUNCT TO DIET AND EXERCISE FOR THE TREATMENT OF PEDIATRIC PATIENTS AGED 12 YEARS AND OLDER WITH HOMOZYGOUS FAMILIAL HYPERCHOLESTEROLEMIA (HOFH), BY INHIBITING EXPRESSION OF THE PCSK9 GENE

International Family Members for US Patent 8,222,222

Country	Patent Number	Estimated Expiration	Supplementary Protection Certificate	SPC Country	SPC Expiration
Australia	2007249329
Australia	2010241357
Australia	2012261570
Australia	2016203687
Canada	2651839