Details for Patent: 10,081,621

Which drugs does patent 10,081,621 protect, and when does it expire?

Patent 10,081,621 protects TRIKAFTA (COPACKAGED), ALYFTREK, and SYMDEKO (COPACKAGED), and is included in four NDAs.

This patent has sixty-three patent family members in twenty-five countries.

Summary for Patent: 10,081,621

Title:	Solid forms of (R)-1(2,2-difluorobenzo[D][1,3]dioxol-5-yl)-N-(1-(2,3-dihydroxypropyl)-6-- fluoro-2-(1-hydroxy-2-methylpropan-2-yl)-1H-indol-5-yl)cyclopropanecarboxa- mide
Abstract:	The present invention relates to solid forms of (R)-1-(2,2-difluorobenzo[d][1,3]dioxol-5-yl)-N-(1-(2,3-dihydroxypropyl)-6- -fluoro-2-(1-hydroxy-2-methylpropan-2-yl)-1H-indol-5-yl)cyclopropanecarbox- amide (Compound 1) in substantially crystalline form (Form A) or amorphous form, pharmaceutical compositions thereof, and methods of treatment therewith.
Inventor(s):	Keshavarz-Shokri; Ali (San Diego, CA), Zhang; Beili (San Diego, CA), Alcacio; Tim Edward (San Diego, CA), Lee; Elaine Chungmin (Arlington, MA), Zhang; Yuegang (Wayland, MA), Krawiec; Mariusz (Marlborough, MA)
Assignee:	Vertex Pharmaceuticals Incorporated (Boston, MA)
Application Number:	14/676,205
Patent Claim Types: see list of patent claims	Use; Composition; Compound;

Understanding the Scope and Claims of United States Patent 10,081,621

Introduction

The United States Patent 10,081,621, titled "Solid forms of (R)-1-(2,2-difluorobenzo[d][1,3]dioxol-5-yl)-N-(1-(2,3-dihydroxypropyl)-6-fluoro-2-(1-hydroxy-2-methylpropan-2-yl)-1H-indol-5-yl)cyclopropanecarboxamide," is a patent that delves into the solid state forms of a specific chemical compound. Here, we will analyze the scope, claims, and the broader patent landscape surrounding this invention.

Background of the Patent

This patent, issued on September 25, 2018, pertains to the solid state forms, including crystalline and amorphous forms, of a complex organic compound. The compound in question is a derivative of indole and is of significant interest in pharmaceutical research due to its potential therapeutic applications[1].

Scope of the Patent

The scope of the patent is defined by the claims, which outline the specific aspects of the invention that are protected.

Claims

The patent includes multiple claims that cover various aspects of the solid state forms of the compound:

• Claim 1: This claim specifies the crystalline form of the compound, including its polymorphic forms and solvates.
• Claim 2: This claim covers the amorphous form of the compound.
• Claims 3-10: These claims detail different methods for preparing the solid state forms, including crystallization and lyophilization processes.
• Claims 11-15: These claims pertain to pharmaceutical compositions comprising the solid state forms of the compound and methods for their use in treating various diseases[1].

Detailed Analysis of Claims

Crystalline Forms

The patent extensively describes the crystalline forms of the compound, including their X-ray powder diffraction (XRPD) patterns, infrared (IR) spectra, and differential scanning calorimetry (DSC) profiles. These characteristics are crucial for identifying and distinguishing between different polymorphic forms of the compound[1].

Amorphous Forms

The amorphous form of the compound is also covered, with descriptions of its preparation methods and physical properties. Amorphous forms are often preferred in pharmaceutical applications due to their higher solubility and bioavailability compared to crystalline forms[1].

Preparation Methods

The patent outlines various methods for preparing the solid state forms, including recrystallization from different solvents, lyophilization, and spray drying. These methods are critical for ensuring the reproducibility and consistency of the solid state forms, which is essential for pharmaceutical applications[1].

Patent Landscape

Related Patents

The patent landscape surrounding US 10,081,621 includes other patents related to similar compounds and their solid state forms. For example, US 9,012,496 B2 also deals with pharmaceutical compositions of related indole derivatives, highlighting the broader interest in these compounds for therapeutic use[4].

Exclusivity and Challenges

Patents like US 10,081,621 are subject to challenges and oppositions, similar to those seen with other pharmaceutical patents. For instance, the patents protecting Trikafta, another pharmaceutical product, have been open to challenges and oppositions, illustrating the competitive and legally complex environment in which these patents operate[5].

Impact on Pharmaceutical Research

Therapeutic Applications

The compound described in the patent has potential therapeutic applications, particularly in the treatment of diseases where indole derivatives have shown efficacy. The solid state forms of this compound are crucial for developing stable and effective pharmaceutical formulations.

Regulatory Considerations

The patent's claims and scope must align with regulatory requirements, such as those set by the FDA. The process of preparing the solid state forms and the pharmaceutical compositions must comply with Good Manufacturing Practices (GMP) and other regulatory standards to ensure safety and efficacy[2].

Metrics for Measuring Patent Scope

Claim Length and Count

Research has shown that the scope of a 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[3].

Key Takeaways

• Specificity of Claims: The patent's claims are highly specific, covering various solid state forms and preparation methods.
• Therapeutic Potential: The compound has significant therapeutic potential, particularly in the treatment of diseases where indole derivatives are effective.
• Regulatory Compliance: The patent's scope and claims must comply with regulatory standards to ensure the safety and efficacy of pharmaceutical formulations.
• Patent Landscape: The patent operates within a complex landscape of related patents and potential challenges.

FAQs

Q: What is the main subject of US Patent 10,081,621? A: The main subject is the solid state forms, including crystalline and amorphous forms, of a specific indole derivative.

Q: What are the key claims of the patent? A: The key claims cover the crystalline and amorphous forms of the compound, methods for their preparation, and pharmaceutical compositions comprising these forms.

Q: Why are solid state forms important in pharmaceuticals? A: Solid state forms are crucial for ensuring the stability, solubility, and bioavailability of pharmaceutical compounds.

Q: How does the patent align with regulatory requirements? A: The patent's claims and scope must comply with FDA regulations and GMP standards to ensure the safety and efficacy of the pharmaceutical formulations.

Q: What metrics can be used to measure the scope of a patent? A: Metrics such as independent claim length and independent claim count can be used to measure the scope of a patent.

Sources

1. US10081621B2 - Solid forms of (R)-1(2,2-difluorobenzo[D][1,3]dioxol-5-yl)-N-(1-(2,3-dihydroxypropyl)-6-fluoro-2-(1-hydroxy-2-methylpropan-2-yl)-1H-indol-5-yl)cyclopropanecarboxamide - Google Patents.
2. Civil Action No. 20-755-RGA - District of Delaware - United States District Court for the District of Delaware.
3. Patent Claims and Patent Scope - SSRN.
4. US9012496B2 - Google Patents.
5. Trikafta (copackaged) patent expiration - Pharsight - GreyB.

Drugs Protected by US Patent 10,081,621

Applicant	Tradename	Generic Name	Dosage	NDA	Approval Date	TE	Type	RLD	RS	Patent No.	Patent Expiration	Product	Substance	Delist Req.	Patented / Exclusive Use	Submissiondate
Vertex Pharms Inc	TRIKAFTA (COPACKAGED)	elexacaftor, ivacaftor, tezacaftor; ivacaftor	GRANULES;ORAL	217660-001	Apr 26, 2023		RX	Yes	No	10,081,621		Y			TREATMENT OF CYSTIC FIBROSIS IN PATIENTS AGED 2 TO
Vertex Pharms Inc	TRIKAFTA (COPACKAGED)	elexacaftor, ivacaftor, tezacaftor; ivacaftor	GRANULES;ORAL	217660-002	Apr 26, 2023		RX	Yes	Yes	10,081,621		Y			TREATMENT OF CYSTIC FIBROSIS IN PATIENTS AGED 2 TO
Vertex Pharms Inc	ALYFTREK	deutivacaftor; tezacaftor; vanzacaftor calcium	TABLET;ORAL	218730-001	Dec 20, 2024		RX	Yes	No	10,081,621		Y			TREATMENT OF CYSTIC FIBROSIS IN PATIENTS AGED 6 YEARS AND OLDER WHO HAVE AT LEAST ONE F508DEL MUTATION OR ANOTHER RESPONSIVE MUTATION IN THE CFTR GENE WITH VNZ, D-IVA, AND A COMPOSITION ACCORDING TO CLAIM 1 OF US10081621
Vertex Pharms Inc	ALYFTREK	deutivacaftor; tezacaftor; vanzacaftor calcium	TABLET;ORAL	218730-002	Dec 20, 2024		RX	Yes	Yes	10,081,621		Y			TREATMENT OF CYSTIC FIBROSIS IN PATIENTS AGED 6 YEARS AND OLDER WHO HAVE AT LEAST ONE F508DEL MUTATION OR ANOTHER RESPONSIVE MUTATION IN THE CFTR GENE WITH VNZ, D-IVA, AND A COMPOSITION ACCORDING TO CLAIM 1 OF US10081621

International Family Members for US Patent 10,081,621

Country	Patent Number	Estimated Expiration	Supplementary Protection Certificate	SPC Country	SPC Expiration
European Patent Office	2826776		301105	Netherlands
European Patent Office	2826776		122021000025	Germany
European Patent Office	2826776		LUC00207	Luxembourg
European Patent Office	2826776		PA2021508	Lithuania