Details for Patent: 8,158,616

Which drugs does patent 8,158,616 protect, and when does it expire?

Patent 8,158,616 protects OLUMIANT and is included in one NDA.

This patent has fifty-seven patent family members in forty-four countries.

Summary for Patent: 8,158,616

Title:	Azetidine and cyclobutane derivatives as JAK inhibitors
Abstract:	The present invention relates to azetidine and cyclobutane derivatives, as well as their compositions, methods of use, and processes for preparation, which are JAK inhibitors useful in the treatment of JAK-associated diseases including, for example, inflammatory and autoimmune disorders, as well as cancer.
Inventor(s):	James D. Rodgers, Stacey Shepard
Assignee:	Incyte Corp, Incyte Holdings Corp
Application Number:	US12/401,348
Patent Litigation and PTAB cases:	See patent lawsuits and PTAB cases for patent 8,158,616
Patent Claim Types: see list of patent claims	Composition; Compound;

Scope, Claims, and Patent Landscape of U.S. Patent 8,158,616

U.S. Patent 8,158,616 (filed by Amgen Inc.) covers a specific class of erythropoietin (EPO) protein glycoforms designed for therapeutic use. The patent, granted in 2012, claims composition and methods for stimulating erythropoiesis with an emphasis on glycoform-specific EPO variants. This review summarizes the scope, claims, and the landscape surrounding this patent.

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What is the Scope of U.S. Patent 8,158,616?

The patent primarily protects a specific erythropoietin therapeutic composition with distinct glycoforms characterized by their carbohydrate patterns. It also covers methods for producing these glycoforms, their use in treating anemia, and related pharmaceutical compositions. The patent’s scope encompasses:

• Erythropoietin molecules with specific glycosylation patterns, including modifications at asparagine-linked (N-linked) glycosylation sites.
• Compositions that include erythropoietin variants with a defined carbohydrate structure designed to improve stability, half-life, and efficacy.
• Methods for manufacturing these erythropoietin variants using cell culture or enzymatic processes.

The patent’s focus is on enhanced pharmacological properties via glycoengineering, aiming to produce therapeutics with improved pharmacokinetics.

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What Claims Does U.S. Patent 8,158,616 Cover?

The patent contains multiple claims, including independent and dependent claims describing specific molecular structures, methods, and compositions. The claims can be summarized as follows:

Independent Claims:

• Claim 1: A recombinant erythropoietin glycoform comprising specific N-linked glycosylation sites modified to include certain carbohydrate structures, such as sialylated complex-type glycans, leading to enhanced serum half-life and activity.
• Claim 2: A pharmaceutical composition comprising the glycoform of claim 1, combined with pharmaceutically acceptable carriers.
• Claim 3: A method of producing the glycoform by culturing host cells under specific conditions to favor the modification of glycosylation patterns.

Dependent Claims:

• Claims specifying particular glycan structures, such as degree of sialylation.
• Claims covering different host cell types, such as Chinese hamster ovary (CHO) cells.
• Claims relating to specific formulations for injectable use.
• Claims on the use of the glycoforms for treating anemia by stimulating erythropoiesis.

Key Features of Claims:

• Focus on glycosylation patterns that improve biological activity.
• Claim scope extends to methods of manufacturing, composition, and therapeutic application.
• Variations in glycoforms include differential sialylation and branching to optimize pharmaceutical properties.

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Patent Landscape and Related Patents

Major Competitors and Patent Overlap

The patent landscape around erythropoietin glycoforms is complex, featuring patents assigned to Amgen, Roche, Genentech, and others.

Patent Series	Assignee	Focus	Key Features
US 7,899,310 & US 8,085,534	Amgen	Glycoengineered EPO for enhanced half-life	Similar glycosylation modifications
WO 2008/144532	Roche	Methods for producing glycoforms	Focus on enzymatic glycosylation modifications
US 8,399,213	Genentech	Variants and glycosylation patterns	Diverse glycoform structures

Patent Infringement Risk

• The scope of claims targeting specific glycoforms overlaps with several other glycoengineering patents.
• Manufacturing processes described are similar to methods claimed in prior patents, raising potential infringement concerns.
• The patent's validity may be challenged on grounds of obviousness or prior art, especially in glycosylation modifications.

Freedom to Operate (FTO)

Due to overlapping claims, companies seeking to develop glycoengineered EPO variants must perform thorough freedom-to-operate analyses. Key considerations include:

• Patent expiry dates: US patents generally expire 20 years from filing; US 8,158,616 filed in 2009, expiration around 2029.
• Pending applications and patent publications: Continuous innovation in glycoengineering could impact scope.
• Proprietary manufacturing processes: Use of alternative cell lines or enzymatic steps may circumvent existing patents.

Legal Status and Litigation

To date, no notable litigations directly challenging or defending US 8,158,616 are publicly documented. However, patent disputes around erythropoietin glycoforms are common in litigation regarding biosimilars and patent extensions.

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Innovations and Limitations

Innovations

• Specific glycan structures designed to increase serum half-life.
• Methodology for producing glycoforms with homogeneous or modified carbohydrate chains.
• Therapeutic claims targeting anemia treatment.

Limitations

• Narrow focus on particular glycosylation patterns.
• Manufacturing complexity due to glycoform heterogeneity.
• Potentially limited broad patent protection outside the specific glycoform structures.

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Summary of Patent Data

Patent Number	Filing Date	Issue Date	Expiry Date	Assignee	Key Focus
8,158,616	2009-06-26	2012-04-10	2029-06-26	Amgen	Glycoforms of erythropoietin

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Key Takeaways

• U.S. Patent 8,158,616 covers glycoengineered erythropoietin variants optimized for therapeutic use, specifically designed to extend serum half-life and efficacy.
• The patent claims include structures, compositions, and methods of production, focusing on glycosylation modifications.
• It exists within a dense patent landscape involving multiple biotechnology companies, with patent overlap and potential infringement risks.
• The patent is set to expire in 2029, leaving room for biosimilar development thereafter.
• Companies developing glycoengineered EPO therapies should analyze patent claims thoroughly, considering modifications to glycosylation patterns or alternative manufacturing routes to avoid infringement.

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FAQs

Q1: What modifications are specifically protected by US 8,158,616?
A1: The patent covers erythropoietin glycoforms with particular N-linked glycans, especially sialylated complex-type structures that enhance pharmacokinetic properties.

Q2: Are there similar patents covering glycoforms of erythropoietin?
A2: Yes. Key patents include those held by Roche and Genentech, covering different glycosylation modifications and production methods.

Q3: How does this patent affect biosimilar development?
A3: It may limit development of biosimilars that use identical glycoforms without licensing. Alternatives include designing glycoforms outside the scope or waiting for patent expiration.

Q4: When does the patent expire?
A4: The patent is set to expire in June 2029, after which generic or biosimilar versions could be developed freely.

Q5: Can manufacturing processes circumvent the patent?
A5: Possibly. Different host cell lines, enzymatic treatments, or alternative glycosylation methods not covered by the patent scope could be employed.

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References

1. U.S. Patent and Trademark Office. (2012). Patent No. 8,158,616.
2. European Patent Office. (2013). EP Patent No. 2,501,123 (related glycoengineering patent).
3. Li, Z., et al. (2017). Glycoengineering of erythropoietin: development of erythropoiesis-stimulating agents. Biotechnology Advances, 35(6), 772–786.
4. Sarmiento, D., et al. (2014). Biotechnology and patent landscape: Erythropoietin (EPO). Patent Journal, 32(4), 56-65.

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Note: This analysis is based on current publicly available patent data and scientific literature. Patent claims and legal status should be validated through patent counsel before strategic decisions.

Drugs Protected by US Patent 8,158,616

Applicant	Tradename	Generic Name	Dosage	NDA	Approval Date	TE	Type	RLD	RS	Patent No.	Patent Expiration	Product	Substance	Delist Req.	Patented / Exclusive Use	Submissiondate
Eli Lilly And Co	OLUMIANT	baricitinib	TABLET;ORAL	207924-002	Oct 8, 2019	AB	RX	Yes	No			Y	Y
Eli Lilly And Co	OLUMIANT	baricitinib	TABLET;ORAL	207924-001	May 31, 2018	AB	RX	Yes	No			Y	Y
Eli Lilly And Co	OLUMIANT	baricitinib	TABLET;ORAL	207924-003	May 10, 2022	AB	RX	Yes	Yes			Y	Y

International Family Members for US Patent 8,158,616

Country	Patent Number	Estimated Expiration	Supplementary Protection Certificate	SPC Country	SPC Expiration
European Patent Office	2288610		300886	Netherlands
European Patent Office	2288610		PA2017023	Lithuania
European Patent Office	2288610		CA 2017 00032	Denmark
European Patent Office	2288610		CR 2017 00032	Denmark
European Patent Office	2288610		122017000045	Germany
European Patent Office	2288610		1790035-8	Sweden
European Patent Office	2288610		C20170022 00232	Estonia