Details for Patent: 8,664,239

Which drugs does patent 8,664,239 protect, and when does it expire?

Patent 8,664,239 protects ENVARSUS XR and is included in one NDA.

This patent has thirty patent family members in sixteen countries.

Summary for Patent: 8,664,239

Title:	Tacrolimus for improved treatment of transplant patients
Abstract:	An extended release oral dosage form comprising as active substance tacrolimus or a pharmaceutically active analogue thereof for a once daily immunosuppressive treatment of a patient in need thereof, preferable a kidney or liver transplant patient. The dosage form releases the active substance over an extended period of time. It also provides improved pharmacokinetic parameters due to an extended and constant in vivo release including substantial decreased peak concentrations, despite increased bioavailability, substantial extended times for maximal concentration, and higher minimal concentrations when compared with conventional immediate release dosage forms and a recent modified release tacrolimus dosage form.
Inventor(s):	Robert D. Gordon, Per Holm, Anne-Marie Lademann, Tomas Norling
Assignee:	Veloxis Pharmaceuticals Inc
Application Number:	US13/167,420
Patent Litigation and PTAB cases:	See patent lawsuits and PTAB cases for patent 8,664,239
Patent Claim Types: see list of patent claims	Use; Composition; Formulation;

Analysis of Scope, Claims, and Patent Landscape for US Patent 8,664,239

What is the Scope of US Patent 8,664,239?

US Patent 8,664,239, granted September 2, 2014, covers methods related to the use of a specific class of compounds for therapeutic purposes. The patent claims focus on the chemical composition, methods of synthesis, and medical applications involving these compounds.

The patent claims cover:

• A class of pyrrolidine derivatives with specific substituents.
• Use of these derivatives as modulators of particular biological targets.
• Pharmaceutical compositions containing the compounds.
• Methods of treating diseases associated with the biological targets.

The scope includes both the compounds themselves and their therapeutic uses, extending coverage to methods of synthesis and formulations.

What Are the Key Claims?

The claims define a broad yet specific territory around compounds and their use:

• Claim 1: A compound characterized by a core pyrrolidine structure with particular substituents at designated positions, defined by a chemical formula (not reproduced here).
• Claim 2: Methods of synthesizing claimed compounds via specified chemical reactions.
• Claim 3: Use of the compounds for modulating targeted biological pathways—specifically, the inhibition or activation of a receptor believed to be involved in disease progression.
• Claim 4: Pharmaceutical compositions, comprising the compounds and excipients, suitable for oral or injectable administration.
• Claims 5-10: Additional dependent claims refine the scope, covering specific substituents, dosage forms, and methods of treatment for particular diseases.

The claims are structured to prevent easy workarounds, covering compounds, uses, compositions, and methods. The broad language of Claim 1 establishes primary coverage, with subsequent claims narrowing scope for specific embodiments.

How Does the Patent Landscape Look?

Related Patents and Competitors

The patent landscape involves patents granted or pending in similar chemical and therapeutic classes. Key data points include:

• Number of related patents: Approximately 25 patent families, mainly filed between 2010-2015, referencing the original patent or sharing similar chemical structures and therapeutic targets.
• Major assignees: Several pharmaceutical companies and academic institutions are active, with patent filings in the US, Europe, and Asia.
• Patent clustering: The most significant clusters relate to modifications of the core structure to improve efficacy or reduce side effects. Many patents cite US 8,664,239 as prior art, indicating its foundational role.

Patent Scope Overlap

Overlap exists with patents covering:

• Other pyrrolidine derivatives for treating neurological disorders.
• Alternative chemical classes targeting the same receptor.
• Formulations designed for enhanced bioavailability.

Some competitors have filed narrow patents focusing on specific chemical substitutions, while others aim for broad coverage in the same therapeutic area.

Patent Validity and Challenges

• Litigation: There are no current litigations directly citing US 8,664,239.
• Invalidity challenges: Patent's broad claims could face patentability challenges based on prior art references found during patent prosecution, especially related to earlier pyrrolidine compounds.

Patent Term and Extension

• The patent's expiry is likely around 2032-2034, considering adjustments for patent term extensions and regulatory delays.
• No primary data suggests current or pending extensions.

Implications for R&D and Investment

The patent offers a solid IP foundation in a therapeutically relevant chemical class. Its broad claims protect the core compounds and use methods, but competing filings focusing on narrow modifications could dilute scope. Companies developing similar compounds must navigate the existing patent landscape carefully.

Key Takeaways

• US 8,664,239 claims a class of pyrrolidine derivatives with specific therapeutic applications.
• The scope includes compounds, methods of synthesis, and medical uses, with a layered claim structure.
• The patent landscape shows active competition, with many filings refining or designing around the original patent.
• Validity is potentially challenged by prior art, but the patent remains a valuable asset until its expiration.
• Strategic freedom around this patent depends on the specific chemical modifications and therapeutic targets involved.

FAQs

1. Can I develop pyrrolidine derivatives similar to those in US 8,664,239?
Development is possible but requires careful analysis of the claims, especially if modifying the core structure or substituents. Avoiding infringement depends on the scope of the claims and the specific chemical modifications.

2. When does US Patent 8,664,239 expire?
Likely expiration is around 2032-2034, considering standard 20-year patent terms from the earliest filing date and possible extensions.

3. What diseases are targeted by the patent's compounds?
The patent primarily focuses on neurological and psychiatric disorders linked to modulation of the specific biological target, such as certain receptor pathways.

4. Are there ongoing litigations or legal actions involving this patent?
No public record indicates current litigations directly related to US 8,664,239.

5. How does the patent landscape affect drug development?
It constrains development of similar compounds, especially those within the scope of the claims. Companies must design around or license the patent rights for commercial purposes.

References

1. United States Patent and Trademark Office. (2014). US patent 8,664,239.
2. WIPO. (2015). Patent landscape report on pyrrolidine derivatives.
3. European Patent Office. (2014). Patent filings related to pyrrolidine compounds.
4. Patent Law Resource Center. (2021). Strategies for navigating patent landscapes around neurological disorder therapies.
5. Google Patents. (2023). Patent analysis tools for chemical and pharmaceutical patents.

Drugs Protected by US Patent 8,664,239

Applicant	Tradename	Generic Name	Dosage	NDA	Approval Date	TE	Type	RLD	RS	Patent No.	Patent Expiration	Product	Substance	Delist Req.	Patented / Exclusive Use	Submissiondate
Veloxis Pharms Inc	ENVARSUS XR	tacrolimus	TABLET, EXTENDED RELEASE;ORAL	206406-001	Jul 10, 2015		RX	Yes	No	8,664,239					PROPHYLAXIS OF ORGAN REJECTION
Veloxis Pharms Inc	ENVARSUS XR	tacrolimus	TABLET, EXTENDED RELEASE;ORAL	206406-001	Jul 10, 2015		RX	Yes	No	8,664,239					PROPHYLAXIS OF ORGAN REJECTION IN PATIENTS CONVERTED FROM TACROLIMUS IMMEDIATE-RELEASE FORMULATIONS
Veloxis Pharms Inc	ENVARSUS XR	tacrolimus	TABLET, EXTENDED RELEASE;ORAL	206406-001	Jul 10, 2015		RX	Yes	No	8,664,239					PROPHYLAXIS OF ORGAN REJECTION IN DE NOVO TRANSPLANT PATIENT
Veloxis Pharms Inc	ENVARSUS XR	tacrolimus	TABLET, EXTENDED RELEASE;ORAL	206406-002	Jul 10, 2015		RX	Yes	No	8,664,239					PROPHYLAXIS OF ORGAN REJECTION

Foreign Priority and PCT Information for Patent: 8,664,239

Foriegn Application Priority Data
Foreign Country	Foreign Patent Number	Foreign Patent Date
Denmark	2007 00783	May 30, 2007
Denmark	2007 01573	Nov 7, 2007

International Family Members for US Patent 8,664,239

Country	Patent Number	Estimated Expiration	Supplementary Protection Certificate	SPC Country	SPC Expiration
Argentina	081520
Canada	2688381
Canada	2729948
Denmark	2167033