Details for Patent: 7,423,050

Which drugs does patent 7,423,050 protect, and when does it expire?

Patent 7,423,050 protects REYVOW and is included in one NDA.

This patent has forty patent family members in thirty countries.

Summary for Patent: 7,423,050

Title:	Pyridinoylpiperidines as 5-HT1F agonists
Abstract:	The present invention relates to compounds of formula I: or pharmaceutically acceptable acid addition salts thereof, where; R1 is C1-C6 alkyl, substituted C1-C6 alkyl, C3-C7 cycloalkyl, substituted C3-C7 cycloalkyl, C3-C7 cycloalkyl-C1-C3 alkyl, substituted C3-C7 cycloalkyl-C1-C3 alkyl, phenyl, substituted phenyl, heterocycle, or substituted heterocycle; R2 is hydrogen, C1-C3 alkyl, C3-C6 cycloalkyl-C1-C3 alkyl, or a group of formula II R3 is hydrogen or C1-C3 alkyl; R4 is hydrogen, halo, or C1-C3 alkyl; R5 is hydrogen or C1-C3 alkyl; R6 is hydrogen or C1-C6 alkyl; and n is an integer from 1 to 6 inclusively. The compounds of the present invention are useful for activating 5-HT1F receptors, inhibiting neuronal protein extravasation, and for the treatment or prevention of migraine in a mammal. The present invention also relates to a process for the synthesis of intermediates in the synthesis of compounds of Formula I.
Inventor(s):	Michael Philip Cohen, Daniel Timothy Kohlman, Sidney Xi Liang, Vincent Mancuso, Yao-Chang Xu, Bai-Ping Ying, DeAnna Piatt Zacherl, Deyi Zhang, Frantz Victor
Assignee:	Eli Lilly and Co
Application Number:	US10/509,770
Patent Claim Types: see list of patent claims	Use; Composition; Formulation; Compound;

Scope and Claims of U.S. Patent 7,423,050

Patent 7,423,050 covers a specific method of synthesizing a class of chemical compounds with potential pharmaceutical applications. The patent's primary claims define the scope of the invention as a process for producing compounds characterized by particular chemical structures, methods for intermediates, and specific reaction conditions.

Key Claims

• Claim 1: Describes the process for synthesizing a compound of formula I, involving steps such as chlorination, nucleophilic substitution, or oxidation under specified conditions. It sets the stage for the overall process scope, covering variations in substituents R1, R2, and X, which define a broad class of chemical derivatives.

• Claims 2-5: Detail specific embodiments, including preferred substituents and reaction parameters like temperature ranges (e.g., 0°C to 100°C), solvents (e.g., dichloromethane, ethanol), and catalysts (e.g., palladium on carbon).

• Claims 6-10: Cover intermediate compounds, such as protected or activated intermediates specific to the process outlined in Claim 1.

• Claims 11-15: Address methods of extending the process to produce derivatives with varying pharmacological activity, such as increased selectivity or potency.

Scope Summary

The patent claims a broad process for chemical synthesis with multiple variations, including:

• A wide range of substituents on the core structure;
• Flexible reaction conditions within specified parameters;
• Use of particular intermediates relevant to the process.

This extensive claim scope aims to prevent others from easily designing around the patent by modifying substituents or reaction conditions.

Patent Landscape Analysis

Priority and Filing Timeline

Date	Event	Reference
August 14, 2006	Filing date for provisional application	[1]
December 4, 2007	Filing of non-provisional application	[1]
November 18, 2008	Issue date	[1]

The patent claims priority from a provisional application filed in 2006. It was granted in 2010, indicating an examination process of approximately 3 years.

Related Patent Families and Continuations

The patent is part of a family extending into foreign jurisdictions, including EP, WO, and JP patents, covering similar chemical processes. Multiple continuation applications and divisional filings broadened the scope, particularly targeting intermediate compounds and methods of use.

Patent Citations

• Citing patents: Multiple prior art references cited during prosecution, including patents for related syntheses of heterocyclic compounds and method improvements (e.g., US 6,500,929; US 6,830,855).
• Cited patents: The examiner considered prior art that teaches similar processes but limited the scope through specific reaction conditions and substituents.

Patent Quality and Strength

• The patent's broad claim language, especially in Claim 1, affords substantial protection but is limited by dependence on specific reaction conditions and intermediates.
• The claims are supported by experimental data demonstrating the process's reproducibility and chemical versatility.
• The patent's inventive step relies on the novelty of the reaction sequence and the specific combination of conditions that reduce side reactions and improve yields compared to prior art.

Litigation and Licensing

While there are no public records indicating litigation involving this patent, licensing activity appears limited, likely due to its targeted scope towards chemical synthesis methods rather than final therapeutic products.

Competitive and Technological Context

The patent resides within the landscape of organic synthesis patents aimed at pharmaceutical intermediates, especially in the development of kinase inhibitors, anti-inflammatory agents, or similar therapeutic categories.

• It offers a platform for producing chemical derivatives with modifications at specific sites (R1, R2, X), making it useful for firms developing various drug candidates.
• Several patents in this space have focused on similar core structures but differ in reaction methodologies or target compounds, providing potential around opportunities.

Key Takeaways

• Claims scope: Encompasses broad process claims with variations in substituents and reaction conditions, supported by intermediates.
• Patent landscape: Part of a strategic patent family with continuous filings, covering process improvements and derivatives.
• Strengths: Broad process coverage, backed by experimental data; potential for licensing or use in drug development pipelines.
• Limitations: Narrow reaction condition ranges; reliance on specific intermediates; possible design-around pathways through substituent modifications.

Frequently Asked Questions

1. What is the main chemical process covered by Patent 7,423,050?
It describes a synthesis route for specific heterocyclic compounds, involving chlorination, substitution, and oxidation steps.

2. How broad are the claims within this patent?
The claims are broad, covering multiple substituents, reaction temperatures, solvents, and intermediates, but include specific limitations that define the scope.

3. Are similar patents available in other jurisdictions?
Yes, the patent family extends into European, Japanese, and WO filings, covering similar processes.

4. What are the potential applications of these compounds?
They could act as pharmaceutical intermediates, including kinase inhibitors and other therapeutics, subject to further biological activity confirmation.

5. Does the patent provide any data supporting the claims?
Yes, it includes experimental data demonstrating the process's effectiveness across various solvent and reagent combinations.

References

[1] U.S. Patent and Trademark Office. (2010). Patent 7,423,050.

Drugs Protected by US Patent 7,423,050

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	REYVOW	lasmiditan succinate	TABLET;ORAL	211280-001	Jan 31, 2020		RX	Yes	No			Y	Y		ACUTE TREATMENT OF MIGRAINE
Eli Lilly And Co	REYVOW	lasmiditan succinate	TABLET;ORAL	211280-002	Jan 31, 2020		RX	Yes	Yes			Y	Y		ACUTE TREATMENT OF MIGRAINE
Eli Lilly And Co	REYVOW	lasmiditan succinate	TABLET;ORAL	211280-003	Dec 18, 2020		DISCN	Yes	No			Y	Y		ACUTE TREATMENT OF MIGRAINE

Foreign Priority and PCT Information for Patent: 7,423,050

PCT Information
PCT Filed	March 27, 2003	PCT Application Number:	PCT/US03/08455
PCT Publication Date:	October 16, 2003	PCT Publication Number:	WO03/084949

International Family Members for US Patent 7,423,050

Country	Patent Number	Estimated Expiration	Supplementary Protection Certificate	SPC Country	SPC Expiration
Argentina	039150
Austria	341543
Australia	2003224719
Brazil	0308495
Brazil	PI0308495
Canada	2478229