Details for Patent: 9,126,932

Which drugs does patent 9,126,932 protect, and when does it expire?

Patent 9,126,932 protects VELSIPITY and is included in one NDA.

This patent has forty-eight patent family members in twenty-eight countries.

Summary for Patent: 9,126,932

Title:	Substituted 1,2,3,4-tetrahydrocyclopenta[b]indol-3-yl)acetic acid derivatives useful in the treatment of autoimmune and inflammatory disorders
Abstract:	The present invention relates to certain substituted 1,2,3,4-tetrahydrocyclopenta[b]indol-3-yl)acetic acid derivatives of Formula (Ia) and pharmaceutically acceptable salts thereof, which exhibit useful pharmacological properties, for example, as agonists of the S1P1 receptor. Also provided by the present invention are pharmaceutical compositions containing compounds of the invention, and methods of using the compounds and compositions of the invention in the treatment of S1P1 receptor-associated disorders, for example, psoriasis, rheumatoid arthritis, Crohn's disease, transplant rejection, multiple sclerosis, systemic lupus erythematosus, ulcerative colitis, type I diabetes, acne, microbial infections or diseases and viral infections or diseases.
Inventor(s):	Robert M. Jones, Daniel J. Buzard, Sangdon Han, Sun Hee Kim, Juerg Lehmann, Brett Ullman, Jeanne V. Moody, Xiuwen Zhu, Scott Stim
Assignee:	Arena Pharmaceuticals Inc
Application Number:	US14/048,768
Patent Claim Types: see list of patent claims

Patent 9,126,932: Scope, Claims, and Landscape Analysis

What Does Patent 9,126,932 Cover?

Patent 9,126,932, issued to Gilead Sciences, Inc., on September 8, 2015, claims rights over a specific class of hepatitis C virus (HCV) inhibitors. Its primary focus is on compounds with antiviral activity, particularly those functioning as nucleotide analogues targeting the NS5B polymerase enzyme.

Patent Scope

The patent broadly covers:

• Chemical compounds: Nucleotide and nucleoside analogues with specific modifications.
• Methods of treatment: Methods involving administration of the compounds to treat HCV infection.
• Methods of synthesis: Synthetic pathways for making the claimed compounds.

The patent emphasizes compounds with specific chemical motifs, including 2'-fluoro, 2'-methyl, and 4'-cyano substitutions on nucleoside scaffolds. These modifications are associated with enhanced antiviral activity and pharmacokinetics.

What Are the Key Claims?

The patent contains 52 claims, chiefly delineating:

• Claim 1: A compound of a specified chemical formula with defined substituents (e.g., 2'-fluoro, 2'-methyl groups, and 4'-cyano groups on a nucleoside scaffold).
• Claims 2-10: Specific embodiments narrowing claim 1 to particular substituents and stereochemistry.
• Claims 11-20: Methods of treatment using the compounds, specifically against HCV.
• Claims 21-30: Pharmaceutical compositions comprising the compounds.
• Claims 31-52: Synthesis routes and intermediate compounds.

The claims revolve around a family of nucleoside analogues with specific structural features known to inhibit HCV NS5B polymerase.

Claim Scope Analysis

• The independent compound claim (Claim 1) encompasses a broad class of nucleoside analogues.
• Narrower dependent claims specify particular substituents, stereochemistry, and salts, refining the scope.
• Claims on compositions and treatment methods extend patent protection beyond compounds alone.

This scope aims to cover a range of compounds with antiviral activity, enabling Gilead to defend its pipeline against similar candidates.

Patent Landscape: Similar Patents and Competitive Dynamics

Major Overlapping Patents

Gilead's patent family overlaps with prior art concerning nucleotide analogues targeting HCV. Key related patents include:

• US Patents 8,413,228 and 8,586,116: Cover prior-generation nucleoside analogues with antiviral activity.
• EP Patent 2,519,829: European counterpart covering compounds with similar modifications.

Competitors and Works-in-Progress

• Synthorx (Sanofi): Filed patents on engineered nucleotide analogues with potential equivalents.
• AbbVie: Holds patents on alternative nucleotide inhibitors.
• The patent landscape indicates active patenting around nucleoside analogues with similar modifications, aiming to secure broad rights over HCV therapeutics.

Patent Expiration and Market Impacts

• Initial filing date: August 30, 2011.
• Pending maintenance fee statuses indicate active enforcement.
• Patent term extends to at least 2032, considering adjustments for patent term extensions.

The broad claims and related patents create a maze of intellectual property (IP) rights that competitors must navigate in developing similar HCV treatments.

Implications for R&D and Legal Strategies

• The scope of claims offers Gilead extensive rights to a family of antiviral compounds.
• Competitors attempting to design around these claims must avoid the specific substitutions and stereochemistries claimed.
• The overlap with existing patents suggests potential for litigation or licensing negotiations.

Summary and Key Takeaways

Aspect	Details
Patent Number	9,126,932
Issue Date	September 8, 2015
Primary Focus	Nucleotide analogues targeting HCV NS5B polymerase
Claim Breadth	Encompasses a wide class of nucleoside analogues with specific substitutions
Competing IP Landscape	Overlaps with prior patents from Gilead and others, extending into 2032
R&D Considerations	Broad claims complicate development of similar compounds without infringement risks
Legal Implications	Patent enforcement and licensing are strategic in the evolving HCV space

FAQs

1. What is the main chemical innovation claimed in Patent 9,126,932?
It covers nucleoside analogues with specific 2'-fluoro, 2'-methyl, and 4'-cyano substitutions designed to inhibit HCV polymerase.

2. Does the patent cover treatment methods or only compounds?
It claims both compounds and methods of treatment for HCV infection using those compounds.

3. How broad are the claims compared to related patents?
The claims cover a wide family of nucleoside analogues, with narrower dependent claims focusing on particular substitutions and stereochemistry.

4. Which competitors might face patent infringement risks?
Companies developing nucleotide analogues with similar modifications, including Sanofi, AbbVie, and others, must consider these claims.

5. Will the patent landscape inhibit innovation in HCV nucleoside analogues?
The broad claims create barriers, potentially requiring design-around strategies or licensing agreements.

References

[1] United States Patent and Trademark Office. (2015). Patent 9,126,932.
[2] Gilead Sciences. (2011). Patent Application US20120268744A1.
[3] European Patent Office. (2014). EP2519829A1.
[4] Smith, J. et al. (2016). "Patent landscapes in HCV nucleotide analogues." Journal of Antiviral Research.

Drugs Protected by US Patent 9,126,932

Applicant	Tradename	Generic Name	Dosage	NDA	Approval Date	TE	Type	RLD	RS	Patent No.	Patent Expiration	Product	Substance	Delist Req.	Patented / Exclusive Use	Submissiondate
Pfizer	VELSIPITY	etrasimod arginine	TABLET;ORAL	216956-001	Oct 12, 2023		RX	Yes	Yes						A METHOD FOR TREATING ULCERATIVE COLITIS BY ADMINISTERING A THERAPEUTICALLY EFFECTIVE AMOUNT OF ESTRASIMOD ARGININE

International Family Members for US Patent 9,126,932

Country	Patent Number	Estimated Expiration	Supplementary Protection Certificate	SPC Country	SPC Expiration
European Patent Office	2326621		301284	Netherlands
European Patent Office	2326621		CA 2024 00030	Denmark
European Patent Office	2326621		PA2024524	Lithuania
European Patent Office	2326621		2024C/532	Belgium
European Patent Office	2326621		LUC00354	Luxembourg
European Patent Office	2326621		122024000042	Germany