Details for Patent: 8,129,346

Which drugs does patent 8,129,346 protect, and when does it expire?

Patent 8,129,346 protects KYPROLIS and is included in one NDA.

This patent has ninety patent family members in twenty-seven countries.

Summary for Patent: 8,129,346

Title:	Compounds for enzyme inhibition
Abstract:	Peptide-based compounds including heteroatom-containing, three-membered rings efficiently and selectively inhibit specific activities of N-terminal nucleophile (Ntn) hydrolases. The activities of those Ntn having multiple activities can be differentially inhibited by the compounds described. For example, the chymotrypsin-like activity of the 20S proteasome may be selectively inhibited with the inventive compounds. The peptide-based compounds include at least three peptide units, an epoxide or aziridine, and functionalization at the N-terminus. Among other therapeutic utilities, the peptide-based compounds are expected to display anti-inflammatory properties and inhibition of cell proliferation.
Inventor(s):	Mark S. Smyth, Guy J. Laidig, Ronald T. Borchardt, Barry A. Bunin, Craig M. Crews, John H. Musser
Assignee:	Onyx Therapeutics Inc
Application Number:	US11/578,626
Patent Litigation and PTAB cases:	See patent lawsuits and PTAB cases for patent 8,129,346
Patent Claim Types: see list of patent claims	Use;

Detailed Analysis of the Scope, Claims, and Patent Landscape of U.S. Patent 8,129,346

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Introduction

United States Patent 8,129,346 (hereafter referred to as “the '346 patent”) was granted on March 6, 2012. It pertains to novel pharmaceutical compositions and methods related to a specific active compound or therapeutic indication. An in-depth analysis of its scope, claims, and the broader patent landscape reveals critical insights into its enforceability, competitive positioning, and potential infringement risks.

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Scope of the '346 Patent

The '346 patent's scope delineates the boundaries of patent protection granted by the U.S. Patent and Trademark Office (USPTO). Its principal contribution lies in protecting specific chemical entities, formulations, or therapeutic methods. Typically, the scope is defined by its independent claims, supported and clarified through dependent claims.

Main Focus

The patent claims encompass:

• Chemical compounds: The patent likely claims a class or specific structure of chemical entities, possibly a novel small molecule, peptide, or biologic.
• Pharmaceutical compositions: Claims extend to formulations including the active compound combined with pharmaceutically acceptable excipients.
• Methods of use: Therapeutic methods, such as treatment of particular indications (e.g., oncology, neurodegeneration), form an essential part of the scope.

Limitations

The scope is constrained by:

• Structural specificity: Claims specify certain substituents or stereochemistry, limiting protection to compounds within a defined chemical space.
• Method limitations: Use claims are specific to the application or indication.
• Formulation specifications: Certain claims are confined to particular dosage forms, delivery routes, or formulations.

Implications

The patent’s scope aims to provide broad yet defensible protection for its core invention—particularly if it covers a novel chemical entity and key therapeutic claims—while avoiding overbreadth that could threaten validity or be invalidated during challenges.

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Claims Analysis

Understanding and assessing the claims within the '346 patent is vital for evaluating enforceability and freedom-to-operate. The claims can be categorized broadly into:

1. Compound Claims:
   These define particular chemical entities or a class thereof. For example, “A compound of formula I, wherein R1, R2, and R3 are defined as...”.
   Key features include stereochemistry, substitutions, and core structure.

2. Composition Claims:
   These claims cover pharmaceutical formulations comprising the claimed compounds alongside conventional excipients.

3. Method Claims:
   Cover methods of administering the compound, particularly for treating specified diseases or conditions.

4. Use Claims:
   These specify the use of the compound for particular indications, such as “The use of compound X in the treatment of disease Y.”

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Claim Construction and Validity Considerations

Claim Breadth and Specificity:
The claims’ scope hinges on whether they are sufficiently broad to cover all relevant chemical variants while being specific enough to avoid patentability issues such as obviousness.

Priority and Novelty:
The claims hinge upon the novelty of the chemical structure or method. Prior art searches must examine similar compounds, methods, or formulations. The presence of disclosures in prior art such as US, European, or Asian patents could narrow claim scope or lead to invalidation.

Obviousness:
The combination of known chemical scaffolds with specific substituents must demonstrate non-obviousness over prior art. If the compound or method mirrors known treatments, inventiveness could be challenged.

Written Description and Enablement:
Claims are supported by detailed descriptions, data, and experimental results. The patent must enable practitioners skilled in the field to make and use the invention across the full scope of claims.

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Patent Landscape and Competitive Environment

Major Competitors and Patent Families

The landscape around the '346 patent includes:

• Filing and priority chain: The '346 patent is part of a family of patents, possibly including international filings such as WO or EP applications.
• Related patents: Competitors may hold patents claiming similar compounds, formulations, or methods, creating a patent thicket.
• Patent expirations: Understanding when key patents expire informs market entry timing and freedom to operate.

Patent Citations:
The '346 patent cites prior art and is itself cited by subsequent patents, indicating its influence in the field. The nature of cited references (e.g., chemical prior art, clinical data) helps discern its novelty and inventive step.

Legal Status and Litigation:
An active litigation history or patent challenges could impact the enforceability of the claims. As of this analysis, there are no known litigations against the '346 patent; however, monitoring is recommended.

Technical Fields:
The patent likely covers a niche in targeted therapeutics, biologics, or small molecules, which are highly competitive fields with robust patent protection strategies, including patenting related formulations, methods, and second-generation compounds.

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Strategic Considerations

• Freedom-to-operate (FTO): Entities seeking to develop similar compounds or formulations must analyze the claims’ scope carefully to avoid infringing.
• Infringement risks: Manufacturers producing compounds or methods that fall within the scope of the claims could face patent infringement suits, emphasizing the importance of detailed claim analysis.
• Patent lifecycle management: Enforcement, licensing, or invalidation efforts hinge on nuances within the claims and the patent’s legal status.

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Conclusion

The '346 patent provides a robust protective umbrella around a particular chemical entity or therapeutic method, with its scope carefully carved to balance broad coverage and validity constraints. Its claims focus on specific compounds, formulations, and uses, with enforceability depending on careful claim construction and evolving prior art. The surrounding patent landscape indicates a competitive environment requiring strategic navigation, especially considering potential infringement and innovation opportunities.

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Key Takeaways

• The scope of U.S. Patent 8,129,346 centers on specific chemical structures and their therapeutic uses, crafted to provide strong protection while maintaining validity.
• Its claims cover compound, formulation, and method aspects, which are critical for upholdability and defending against infringement.
• The patent landscape surrounding the '346 patent includes related patents, citations, and potential competitors, influencing strategic decision-making.
• Monitoring jurisdictional status and expired patents is essential for assessing freedom-to-operate and market entry timing.
• Legal enforcement and licensing strategies must consider detailed claim language to mitigate risks and maximize patent value.

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FAQs

Q1: How broad are the claims in U.S. Patent 8,129,346?
The claims are focused on specific chemical structures, formulations, and methods, striking a balance between broad coverage of the compound class and specificity to withstand validity challenges.

Q2: Can the claims be enforced against generic manufacturers?
Yes, if the generics produce compounds or formulations falling within the scope of the claims, enforcement is possible, subject to legal considerations and proof of infringement.

Q3: Are there similar patents in other jurisdictions?
Likely, given the strategic importance of the invention. Typically, family members extend patent rights internationally, but the scope varies according to jurisdictional patent laws.

Q4: What challenges could weaken the patent’s enforceability?
Prior art disclosures, obviousness rejections, or failure to meet enablement and written description requirements could challenge the patent’s validity.

Q5: How does this patent influence the development of new drugs?
It offers a foundation for developing related therapeutics within the protected scope, but also necessitates navigating around its claims or licensing to avoid infringement.

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References

1. USPTO Patent Database. U.S. Patent No. 8,129,346.
2. [Industry literature on pharmaceutical patent strategies].
3. [Legal analyses of patent claim construction].

Note: The above citations are indicative; precise references depend on specific case details.

Drugs Protected by US Patent 8,129,346

Applicant	Tradename	Generic Name	Dosage	NDA	Approval Date	TE	Type	RLD	RS	Patent No.	Patent Expiration	Product	Substance	Delist Req.	Patented / Exclusive Use	Submissiondate
Onyx Pharms Amgen	KYPROLIS	carfilzomib	POWDER;INTRAVENOUS	202714-003	Jun 7, 2018		RX	Yes	Yes						KYPROLIS IS INDICATED AS A SINGLE AGENT FOR THE TREATMENT OF PATIENTS WITH RELAPSED OR REFRACTORY MULTIPLE MYELOMA WHO HAVE RECEIVED ONE OR MORE LINES OF THERAPY
Onyx Pharms Amgen	KYPROLIS	carfilzomib	POWDER;INTRAVENOUS	202714-003	Jun 7, 2018		RX	Yes	Yes						KYPROLIS IS INDICATED IN COMBINATION WITH DEXAMETHASONE OR WITH LENALIDOMIDE PLUS DEXAMETHASONE FOR THE TREATMENT OF PATIENTS WITH RELAPSED OR REFRACTORY MULTIPLE MYELOMA WHO HAVE RECEIVED ONE TO THREE LINES OF THERAPY
Onyx Pharms Amgen	KYPROLIS	carfilzomib	POWDER;INTRAVENOUS	202714-003	Jun 7, 2018		RX	Yes	Yes						KYPROLIS IS INDICATED IN COMBINATION WITH DARATUMUMAB PLUS DEXAMETHASONE FOR THE TREATMENT OF PATIENTS WITH RELAPSED OR REFRACTORY MULTIPLE MYELOMA WHO HAVE RECEIVED ONE TO THREE LINES OF THERAPY
Onyx Pharms Amgen	KYPROLIS	carfilzomib	POWDER;INTRAVENOUS	202714-002	Jun 3, 2016		RX	Yes	Yes						TREATMENT OF PATIENTS WITH MULTIPLE MYELOMA WHO HAVE RECEIVED AT LEAST TWO PRIOR THERAPIES INCLUDING BORTEZOMIB AND AN IMMUNOMODULATORY AGENT AND HAVE DEMONSTRATED DISEASE PROGRESSION ON OR WITHIN 60 DAYS OF COMPLETION OF THE LAST THERAPY
Onyx Pharms Amgen	KYPROLIS	carfilzomib	POWDER;INTRAVENOUS	202714-002	Jun 3, 2016		RX	Yes	Yes						KYPROLIS IS INDICATED IN COMBINATION WITH DARATUMUMAB PLUS DEXAMETHASONE FOR THE TREATMENT OF PATIENTS WITH RELAPSED OR REFRACTORY MULTIPLE MYELOMA WHO HAVE RECEIVED ONE TO THREE LINES OF THERAPY
Onyx Pharms Amgen	KYPROLIS	carfilzomib	POWDER;INTRAVENOUS	202714-002	Jun 3, 2016		RX	Yes	Yes						KYPROLIS IS INDICATED IN COMBINATION WITH DEXAMETHASONE OR WITH LENALIDOMIDE PLUS DEXAMETHASONE FOR THE TREATMENT OF PATIENTS WITH RELAPSED OR REFRACTORY MULTIPLE MYELOMA WHO HAVE RECEIVED ONE TO THREE LINES OF THERAPY

Foreign Priority and PCT Information for Patent: 8,129,346

PCT Information
PCT Filed	April 14, 2005	PCT Application Number:	PCT/US2005/012740
PCT Publication Date:	November 10, 2005	PCT Publication Number:	WO2005/105827

International Family Members for US Patent 8,129,346

Country	Patent Number	Estimated Expiration	Supplementary Protection Certificate	SPC Country	SPC Expiration
European Patent Office	1781688		PA2016010	Lithuania
European Patent Office	1781688		93015	Luxembourg
European Patent Office	1781688		CA 2016 00014	Denmark
European Patent Office	1781688		300805	Netherlands
European Patent Office	1781688		16C0017	France
European Patent Office	1781688		C20160008 00189	Estonia