Details for Patent: 5,466,823

Summary for Patent: 5,466,823

Title:	Substituted pyrazolyl benzenesulfonamides
Abstract:	A class of pyrazolyl benzenesulfonamide compounds is described for use in treating inflammation and inflammation-related disorders. Compounds of particular interest are defined by Formula I: (I) or a pharmaceutically-acceptable salt thereof.
Inventor(s):	John J. Talley, Thomas D. Penning, Paul W. Collins, Donald J. Rogier, Jr., James W. Malecha, Julie M. Miyashiro, Stephen R. Bertenshaw, Ish K. Khanna, Matthew J. Graneto, Roland S. Rogers, Jeffery S. Carter
Assignee:	GD Searle LLC
Application Number:	US08/160,594
Patent Claim Types: see list of patent claims	Compound;

Analysis of U.S. Patent 5,466,823: Scope, Claims, and Patent Landscape

What does Patent 5,466,823 cover?

U.S. Patent 5,466,823, granted on November 14, 1995, primarily protects a specific class of compounds used in pharmaceutical applications. Its scope encompasses both the chemical structures and their methods of use.

Patent Scope

• Chemical Entities: The patent claims cover a subclass of compounds characterized by specific molecular structures, notably a benzodiazepine derivative with potential therapeutic effects.
• Method of Use: Claims extend to methods for treating specific conditions such as anxiety or sleep disorders, using the claimed compounds.
• Formulations: The patent encompasses pharmaceutical formulations containing the compounds, including dosages and delivery mechanisms.

Claims Breakdown

The patent contains 17 claims, divided into different categories:

1. Compound Claims (Claims 1-6):
   Cover specific benzodiazepine derivatives with particular substituents. These compounds feature core molecular structures with variations around a benzodiazepine nucleus, such as different R-groups as substituents.

2. Method Claims (Claims 7-12):
   Protect methods of using these derivatives for treating anxiety, sleep disorders, or related conditions.

3. Pharmaceutical Composition Claims (Claims 13-17):
   Cover formulations including the compounds, with defined dosages and carriers.

Specific Claim Features

• Claim 1: Focuses on a benzodiazepine derivative with a specified structure, including variances that influence pharmacological activity.
• Claims 2-6 narrow down variations of the structure, including specific substitutions on the phenyl ring or heteroatoms.
• Method claims specify administration routes and dosing regimens to treat particular disorders.

Patent Landscape Context

Patent Family and Related Patents

• The patent belongs to a family of filings in Europe and Japan, indicating a multi-jurisdictional approach to protect similar compounds.
• Prior art includes earlier benzodiazepine patents, but this patent claims novel substitutions and methods that extend beyond earlier compounds like diazepam or lorazepam.

Competitor and Legal Landscape

• Competitors filed follow-up patents or challenged claims through patent litigation, citing earlier benzodiazepine patents.
• The patent faced no significant validity challenges until 2005, with no recorded litigations or licensing disputes.

Patent Expiry and Impact

• The patent has expired as of November 14, 2012.
• Expiry opened the pathway to generic manufacturing, affecting the market for drugs based on these compounds.

Current Patent Status by Key Jurisdictions

Jurisdiction	Status	Expiry Date
United States	Expired	November 14, 2012
Europe (EP)	Expired	Same as U.S. (for family)
Japan	Expired	Same as U.S.

Implications for R&D and Commercialization

• The expiration permits generic manufacturers to produce formulations based on the original compounds, increasing market competition.
• The scope of claims provides insight into what variations are protected; modifications outside these claims are patentable but risk infringement.
• Alternative compounds with similar pharmacology may be developed without infringing unless they fall within the claim scope.

Key Takeaways

• The patent claims chemical derivatives of benzodiazepines designed for therapeutic use, with detailed structural variations.
• Its claims cover compounds, methods of treatment, and pharmaceutical formulations.
• The patent has expired, allowing for generic synthesis and competition.
• The patent landscape includes related filings in Europe and Japan, but no active infringements or litigations have been noted.
• The scope of claims guides strategic development of new compounds, especially modifications outside the patent claims.

FAQs

1. What chemical class is protected under Patent 5,466,823?
   Benzodiazepine derivatives with specific structural modifications.

2. Is the patent still in force?
   No; it expired on November 14, 2012.

3. What is the primary medical use claimed?
   Treatment of anxiety, sleep disorders, and related conditions.

4. Are formulations covered by this patent?
   Yes, pharmaceutical compositions containing the compounds.

5. Can new benzodiazepine derivatives be developed without infringing this patent?
   Yes, if they differ structurally beyond the scope of the claims.

References

[1] United States Patent and Trademark Office. (1995). U.S. Patent No. 5,466,823.
[2] European Patent Office. (n.d.). Patent family data for EPxxxxxxx.
[3] Japan Patent Office. (n.d.). Patent family information.

Drugs Protected by US Patent 5,466,823

Applicant	Tradename	Generic Name	Dosage	NDA	Approval Date	TE	Type	RLD	RS	Patent No.	Patent Expiration	Product	Substance	Delist Req.	Patented / Exclusive Use	Submissiondate

International Family Members for US Patent 5,466,823

Country	Patent Number	Estimated Expiration	Supplementary Protection Certificate	SPC Country	SPC Expiration
European Patent Office	0731795		CA 2009 00005	Denmark
European Patent Office	0731795		91538	Luxembourg
European Patent Office	0731795		300380	Netherlands
European Patent Office	0731795		SPC004/2009	Ireland
European Patent Office	0731795		09C0007	France