Details for Patent: 10,301,262

Which drugs does patent 10,301,262 protect, and when does it expire?

Patent 10,301,262 protects VELSIPITY and is included in one NDA.

This patent has thirty-one patent family members in twenty countries.

Summary for Patent: 10,301,262

Title:	Crystalline L-arginine salt of (R)-2-(7-(4-cyclopentyl-3-(trifluoromethyl)benzyloxy)-1,2,3,4-tetrahydrocyclo-penta [b]indol-3-yl)acetic acid(Compund1) for use in SIPI receptor-associated disorders
Abstract:	The present invention relates to, inter alia, a novel crystalline free-plate habit or morphology, processes for preparing the crystalline free-plate habit, and uses of the crystalline free-plate habit of the L-arginine salt of (R)-2-(7-(4-cyclopentyl-3-(trifluoromethyl)benzyloxy)-1,2,3,4-tetrahydrocyclo-penta[b]indol-3-yl)acetic acid (Compound 1) in the treatment of S1Preceptor-associated disorders, for example, diseases and disorders mediated by lymphocytes, transplant rejection, autoimmune diseases and disorders, inflammatory diseases and disorders (e.g., acute and chronic inflammatory conditions), cancer, and conditions characterized by an underlying defect in the vascular integrity or that are associated with angiogenesis such as may be pathologic (e.g., as may occur in inflammation, tumor development, and atherosclerosis).
Inventor(s):	Blackburn Anthony C., Castro Ryan O., Hadd Mark Allen, Ma You-An, Montalban Antonio Garrido, Rueter Jaimie Karyn, Selvey Lee Alani, Shakya Sagar Raj, Carlos Marlon
Assignee:	Arena Pharmaceuticals, Inc.
Application Number:	US15738175
Patent Claim Types: see list of patent claims

Detailed Analysis of the Scope and Claims of United States Patent 10,301,262

Introduction

United States Patent 10,301,262, titled "Crystalline L-arginine salt of (R)-2-(7-(4-cyclopentyl-3-(trifluoromethyl)benzyloxy)-1,2,3,4-tetrahydrocyclo-penta [b]indol-3-yl)acetic acid(Compound 1) for use in SIPI receptor-associated disorders," is a significant patent in the pharmaceutical industry. This patent, assigned to Arena Pharmaceuticals, Inc., protects a novel crystalline form of a compound used in treating various disorders.

Patent Overview

• Issuance Date: May 28, 2019[5].
• Inventors: Anthony C. Blackburn, Ryan O. Castro, Mark Allen Hadd, You-An Ma, Antonio Garrido Montalban, Jaimie Karyn Rueter, Lee Alani Selvey, Sagar Raj Shakya, and Marlon Carlos[5].
• Assignee: Arena Pharmaceuticals, Inc.[5].

Scope of the Patent

The patent covers a specific crystalline form of the L-arginine salt of (R)-2-(7-(4-cyclopentyl-3-(trifluoromethyl)benzyloxy)-1,2,3,4-tetrahydrocyclo-penta [b]indol-3-yl)acetic acid, known as Compound 1. This compound is used in the treatment of SIPI receptor-associated disorders, which include a range of autoimmune and inflammatory conditions such as inflammatory bowel disease, multiple sclerosis, and systemic lupus erythematosus[5].

Claims of the Patent

The patent includes several claims that define the scope of protection:

• Claim 1: The crystalline L-arginine salt of Compound 1, characterized by its specific crystal structure and morphology[4].
• Subsequent Claims: These claims cover various aspects such as the processes for preparing the crystalline form, the use of the compound in treating specific disorders, and the pharmaceutical compositions containing the crystalline L-arginine salt[4].

Patent Landscape

Related Patents

The patent is part of a broader portfolio of patents related to Compound 1 and its uses. Other relevant patents include:

• US10676435: Another patent covering the crystalline L-arginine salt of Compound 1, issued on June 9, 2020[5].
• US11007175: A patent covering methods of treating conditions related to the S1P receptor, issued on May 18, 2021[5].
• US8580841 and US9126932: Patents covering substituted 1,2,3,4-tetrahydrocyclopenta[b]indol-3-yl)acetic acid derivatives useful in the treatment of autoimmune and inflammatory disorders[5].

Patent Expiration Dates

• US10301262: Expires on June 21, 2036[5].
• US10676435: Also expires on June 21, 2036[5].
• US11007175 and US11884626: These patents also expire on June 21, 2036, ensuring extended protection for the compound and its uses[5].

Strategic Importance

The extension of patent protection through polymorph patents, as seen in this case, is a common strategy in the pharmaceutical industry. This approach can significantly delay the entry of generic competitors into the market. For example, the polymorph patent for Omaveloxolone extended its protection by about 40 months, and for Nirogacestat Hydrobromide, the extension was approximately 14 years[1].

Impact on Generic Availability

The presence of these patents means that there is currently no therapeutically equivalent generic version of Velsipity (the drug containing Compound 1) available in the United States. This exclusivity period, combined with the patent protection, ensures that Arena Pharmaceuticals, Inc. maintains market exclusivity for the drug until the patents expire[5].

Patent Scope Metrics

The scope of the patent can be measured using metrics such as independent claim length and independent claim count. Narrower claims, as seen in this patent, are often associated with a higher probability of grant and a shorter examination process compared to broader claims[3].

Conclusion and Key Takeaways

• Specific Compound Protection: The patent specifically protects the crystalline L-arginine salt of Compound 1, ensuring exclusivity for its use in treating SIPI receptor-associated disorders.
• Extended Protection: The patent landscape includes multiple related patents that extend the protection period, delaying generic competition.
• Strategic Significance: The use of polymorph patents is a strategic move to extend market exclusivity, a common practice in the pharmaceutical industry.
• Impact on Generics: The absence of generic versions due to patent protection highlights the importance of these patents in maintaining market exclusivity.

Key Takeaways

• The patent covers a specific crystalline form of a compound used in treating autoimmune and inflammatory disorders.
• Multiple related patents extend the protection period, ensuring market exclusivity.
• The use of polymorph patents is a strategic approach to delay generic competition.
• The patent landscape affects the availability of generic versions of the drug.

Frequently Asked Questions (FAQs)

Q: What is the main compound protected by US Patent 10,301,262? A: The main compound is the crystalline L-arginine salt of (R)-2-(7-(4-cyclopentyl-3-(trifluoromethyl)benzyloxy)-1,2,3,4-tetrahydrocyclo-penta [b]indol-3-yl)acetic acid, known as Compound 1.

Q: What disorders is Compound 1 used to treat? A: Compound 1 is used to treat SIPI receptor-associated disorders, including autoimmune and inflammatory conditions such as inflammatory bowel disease and multiple sclerosis.

Q: When does the patent expire? A: The patent expires on June 21, 2036.

Q: Are there any generic versions of the drug available? A: No, there are currently no therapeutically equivalent generic versions of Velsipity available in the United States due to the patent protection.

Q: How does the patent landscape affect the drug's market exclusivity? A: The multiple related patents extend the protection period, ensuring that Arena Pharmaceuticals, Inc. maintains market exclusivity for the drug until the patents expire.

Cited Sources:

1. Crystal PharmaTech. Review of Polymorph Patent Application of 30 Small Molecule New Drugs Approved by the FDA in 2023.
2. Pharsight. Drug Patents containing Etrasimod Arginine.
3. SSRN. Patent Claims and Patent Scope.
4. Google Patents. US10301262B2 - Crystalline L-arginine salt of (R)-2-(7-(4-cyclopentyl-3-(trifluoromethyl)benzyloxy)-1,2,3,4-tetrahydrocyclo-penta [b]indol-3-yl)acetic acid(Compound 1) for use in SIPI receptor-associated disorders.
5. Drugs.com. Generic Velsipity Availability.

Drugs Protected by US Patent 10,301,262

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	10,301,262		Y	Y

International Family Members for US Patent 10,301,262

Country	Patent Number	Estimated Expiration	Supplementary Protection Certificate	SPC Country	SPC Expiration
Australia	2016284162
Australia	2020204164
Australia	2021249972