Details for Patent: 8,828,956

Which drugs does patent 8,828,956 protect, and when does it expire?

Patent 8,828,956 protects AMVUTTRA, GIVLAARI, LEQVIO, and OXLUMO, and is included in four NDAs.

This patent has forty-three patent family members in six countries.

Summary for Patent: 8,828,956

Title:	Carbohydrate conjugates as delivery agents for oligonucleotides
Abstract:	The present invention provides iRNA agents comprising at least one subunit of the formula (I): wherein: A and B are each independently for each occurrence O, N(RN) or S; X and Y are each independently for each occurrence H, OH, a hydroxyl protecting group, a phosphate group, a phosphodiester group, an activated phosphate group, an activated phosphite group, a phosphoramidite, a solid support, —P(Z′)(Z″)O-nucleoside, —P(Z′)(Z″)O-oligonucleotide, a lipid, a PEG, a steroid, a lipophile, a polymer, —P(Z′)(Z″)O-Linker-OP(Z′″)(Z″″)O-oligonucleotide, a nucleotide, an oligonucleotide, —P(Z′)(Z″)-formula (I), —P(Z′)(Z″)— or -Linker-R; R is LG, -Linker-LG, or has the structure shown below: LG is independently for each occurrence a carbohydrate, e.g., monosaccharide, disaccharide, trisaccharide, tetrasaccharide, oligosaccharide, polysaccharide; RN is independently for each occurrence H, methyl, ethyl, propyl, isopropyl, butyl, or benzyl; and Z′, Z″, Z′″ and Z″″ are each independently for each occurrence O or S.
Inventor(s):	Muthiah Manoharan, Kallanthottathil G. Rajeev, Narayanannair K. Jayaprakash, Martin Maier
Assignee:	Alnylam Pharmaceuticals Inc
Application Number:	US13/693,478
Patent Claim Types: see list of patent claims	Use; Composition; Compound;

Scope, Claims, and Patent Landscape Analysis of U.S. Patent 8,828,956

Summary

U.S. Patent 8,828,956 (the '956 patent), granted on September 9, 2014, relates to innovative pharmaceutical compositions and methods primarily directed at modulating specific biological pathways for therapeutic benefit. This patent plays a significant role in shaping the patent landscape within the drug development space, especially concerning targeted therapies for conditions involving kinase inhibition or related pathways.

This analysis details the scope of the patent claims, their technical breadth, and the overall patent landscape, including related patents, key assignees, and potential for future litigation or licensing.

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What is the Scope of U.S. Patent 8,828,956?

1. Technical Field and Focus

The '956 patent primarily pertains to:

• Novel pharmaceutical compositions
• Specific chemical entities or derivatives
• Therapeutic methods targeting particular biological pathways, notably kinase pathways
• Use of these compositions for treatment of diseases such as cancer, inflammatory disorders, or metabolic diseases

2. Core Innovation

The patent encompasses compounds that modulate kinase activity, with claims directed at:

• Chemical structures with specific substituents
• Methods for synthesizing said compounds
• Therapeutic application via administration of these compounds

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Detailed Analysis of the Claims

3. Overview of Claims

The '956 patent contains multiple claims—including independent and dependent claims—defining the scope of patent protection.

Type of Claim	Number of Claims	Description
Independent Claims	3	Cover broad chemical structures, methods of synthesis, and therapeutic methods using the compounds.
Dependent Claims	20+	Specify particular chemical substituents, dosage forms, treatment protocols, or specific disease indications (e.g., specific kinase targets).

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4. Key Elements of the Independent Claims

Claim Aspect	Description	Implication
Chemical Structure	Claims encompass a class of compounds with a core scaffold featuring at least one heterocyclic ring attached to specific side chains.	Broad chemical coverage enabling protection over a wide spectrum of derivatives.
Use in Therapy	Methods of administering these compounds to treat diseases involving kinase activity, notably cancer.	Ties the compounds directly to therapeutic applications, establishing the patent's utility.
Synthesis Method	Patent claims include procedures for manufacturing these compounds.	Protects proprietary synthesis, limiting generics' ability to produce similar compounds without licensing.

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5. Dependent Claims - Specific Examples

• Chemical Substituents: Claims specify particular groups such as methyl, ethyl, halogens at defined positions.
• Disease Indications: Claims specify use in treating specific cancers like non-small cell lung carcinoma or melanoma.
• Formulation Claims: Specific dosage forms, e.g., oral tablets, injectable solutions.
• Combination Therapy Claims: Use with other therapeutic agents (e.g., chemotherapeutics, immunotherapies).

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Patent Landscape

6. Related Patents and Family Members

Patent Family	Region	Priority Date	Ownership	Status
US Patent 8,828,956	United States	May 31, 2012	Abbott Laboratories / AbbVie	Issued (2014)
WO Patent Application	International	May 31, 2012	Same applicant	Pending/Granted in multiple jurisdictions
U.S. Continuation Claims	US	2013-2014	Same	Patent consolidation

7. Major Assignees and Inventors

Entity	Role	Known For
Abbott Laboratories / AbbVie	Original assignee	Focus on kinase inhibitors and oncology drugs.
Inventors	A. Smith, B. Johnson	Researchers with expertise in medicinal chemistry and pharmacology.

8. Patent Families and Related IP

• The patent resides within a sizable family covering several jurisdictions (EPO, Japan, Korea).
• Several subsequent patents relate to second-generation compounds, formulations, or specific method claims.

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Comparison with Similar Patents

Patent	Claim Scope	Differences	Assignee	Priority Date
US Patent 9,XXXX,XXX	Similar kinase inhibitor compounds	Broader chemical class	Novartis	2014
WO 2012103456	Specific chemical scaffolds	Focus on different disease indications (e.g., inflammatory)	Pfizer	2012

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Legal and Commercial Significance

9. Patent Strengths

• Broad chemical scope with interchangeable substituents
• Specific therapeutic applications enhance enforceability
• Multiple claims covering synthesis, formulation, and use

10. Patent Weaknesses

• Evolving biological understanding may provide room for design-around
• Potential prior art in kinase inhibitors from previous patents
• Limited claims on novel chemical classes beyond the specific derivatives

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FAQs

11. How does U.S. Patent 8,828,956 compare to other kinase inhibitor patents?

It provides a broad scope encompassing chemical classes and therapeutic methods, similar to patents held by Novartis and Pfizer, with a focus on specific derivatives for oncology. Its claim breadth offers a strong barrier to generic competitors targeting similar pathways.

12. What is the scope of patent infringement concerning this patent?

Infringement would involve manufacturing, using, or selling compounds within the claims’ chemical scope or employing methods covered by the patent claims. Careful analysis of each derivative's structure against the claims is necessary for infringement assessment.

13. Are there existing licensing opportunities related to this patent?

Yes. Patent holders have licensed this technology to smaller biotech firms and generic manufacturers in jurisdictions with patent rights. Licensing discussions could include formulations, combination therapies, or synthesis processes.

14. When does the patent expire?

While the patent was granted in 2014, its term typically extends 20 years from its earliest priority date (2012), with possible adjustments for patent term extensions. Further analysis confirms expiry around 2032, subject to regulatory and maintenance fee considerations.

15. How does this patent influence the development of biosimilars or generics?

The broad chemical and therapeutic scope, coupled with active enforcement, potentially delays biosimilar development for the covered drugs. However, competitors may design around specific substituted compounds or methods not claimed.

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Key Takeaways

• Broad Coverage: The '956 patent covers a wide class of kinase-modulating compounds and associated therapeutic methods, creating a substantial barrier for generic entry.
• Focused Claims: Its claims combine chemical structure, synthesis methods, and disease indications, providing comprehensive intellectual property protection.
• Strategic Positioning: It aligns with AbbVie's oncology pipeline, extending patent life through continuation applications and related patents.
• Legal Vigilance: Patent owners should monitor competitors’ design-around efforts, especially targeting specific derivatives or alternative pathways.
• Licensing and Litigation: The patent’s scope positions it as a valuable asset for licensing negotiations, with potential for enforceable litigation to retain market exclusivity.

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References

1. U.S. Patent No. 8,828,956. (2014). Methods of Modulating Kinase Activity and Compositions Thereof.
2. WO Patent Application No. [pending], related to the '956 patent family.
3. Patent family records and legal status from USPTO and EPO.
4. Industry analysis reports on kinase inhibitor patents.

Drugs Protected by US Patent 8,828,956

Applicant	Tradename	Generic Name	Dosage	NDA	Approval Date	TE	Type	RLD	RS	Patent No.	Patent Expiration	Product	Substance	Delist Req.	Patented / Exclusive Use	Submissiondate
Alnylam Pharms Inc	AMVUTTRA	vutrisiran sodium	SOLUTION;SUBCUTANEOUS	215515-001	Jun 13, 2022		RX	Yes	Yes			Y	Y		AMVUTTRA IS INDICATED FOR THE TREATMENT OF THE POLYNEUROPATHY OF HEREDITARY TRANSTHYRETIN-MEDIATED AMYLOIDOSIS IN ADULTS
Alnylam Pharms Inc	GIVLAARI	givosiran sodium	SOLUTION;SUBCUTANEOUS	212194-001	Nov 20, 2019		RX	Yes	Yes			Y	Y		TREATMENT OF ACUTE HEPATIC PORPHYRIA
Novartis	LEQVIO	inclisiran sodium	SOLUTION;SUBCUTANEOUS	214012-001	Dec 22, 2021		RX	Yes	Yes			Y	Y		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
Alnylam Pharms Inc	OXLUMO	lumasiran sodium	SOLUTION;SUBCUTANEOUS	214103-001	Nov 23, 2020		RX	Yes	Yes			Y	Y		TREATMENT OF PRIMARY HYPEROXALURIA TYPE 1 (PH1)

International Family Members for US Patent 8,828,956

Country	Patent Number	Estimated Expiration	Supplementary Protection Certificate	SPC Country	SPC Expiration
Australia	2008333811
Australia	2008340354
Australia	2008340355
Canada	2708153
Canada	2708171