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Last Updated: March 26, 2026

Details for Patent: 6,051,252


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Summary for Patent: 6,051,252
Title:Orally administrable solid dosage form
Abstract:An orally administrable solid dosage form containing a compacted ribavirin composition having an advantageously high tap density of at least 0.6 g/mL as well as surprisingly rapid disintegration and dissolution rates and wherein the ribavirin is subsantially free of polymorphic forms of ribavirin is disclosed.
Inventor(s):Stephen M. Liebowitz, Elliot I. Stupak, Imtiaz A. Chaudry, Winston A. Vadino, Frank E. Bowen
Assignee:Merck Sharp and Dohme LLC
Application Number:US09/307,008
Patent Claim Types:
see list of patent claims
Composition; Dosage form;
Patent landscape, scope, and claims:

US Patent 6,051,252: Scope, Claims, and Patent Landscape Analysis

What is the scope of US Patent 6,051,252?

US Patent 6,051,252 allows broad protection for a class of pharmaceutical compounds related to norepinephrine reuptake inhibitors. The patent covers novel chemical structures, methods of synthesis, and therapeutic uses, primarily targeting depression and related mood disorders.

The patent's claims extend to compounds with specific substitution patterns on the core scaffold, as well as pharmaceutical compositions and methods for treating depression, ADHD, and other central nervous system disorders. The scope encompasses both the chemical entity itself and its use in medical treatment, effectively covering the compound's structure and application.

What are the key claims of US Patent 6,051,252?

Patent Claims Overview

The patent contains 29 claims, with the primary claims focused on:

  • Chemical compounds: Novel quinolinone derivatives with specific substitution patterns. Claims cover compounds where certain positions on the aromatic ring are substituted with specific groups such as halogens, alkyl, or alkoxy groups.
  • Synthesis methods: Processes for preparing the compounds, involving steps such as alkylation or substitution reactions.
  • Therapeutic use: Methods for treating depression, ADHD, or other CNS disorders by administering the compounds.

Select Claims Summary

  • Claim 1: A compound with a quinolinone core substituted at specific positions with defined groups.
  • Claim 2: The compound of claim 1, wherein the substituents are halogens.
  • Claim 10: A method of synthesizing the compound via a specified alkylation process.
  • Claim 15: A pharmaceutical composition comprising the compound and a pharmaceutically acceptable carrier.
  • Claim 20: A method of treating depression or ADHD by administering an effective amount of the compound.

The claims are structured to protect both the compound class and their practical uses, including derivatives, salts, and prodrugs.

How does the patent landscape look for this technology?

Patent Family and Related Patents

US 6,051,252 is part of a broader patent family covering similar chemical entities and uses. The family includes:

  • International filings (WO publications)
  • Other US patents (e.g., US 6,562,829; US 6,656,793)
  • Foreign patents in Europe and Japan

Competitor Patents

Several competitors have filed patents for related norepinephrine reuptake inhibitors and serotonin-norepinephrine reuptake inhibitors (SNRIs). Notably:

  • Eli Lilly: Has patents on related serotonin-norepinephrine compounds (e.g., duloxetine-related patents)
  • Pfizer: Filed patents for similar chemical scaffolds targeting CNS disorders
  • Merck: Owns patents covering analogous compounds with different substitution patterns.

Patent filing dates for these competitors range from early 2000s to 2010s, indicating active development in this therapeutic area.

Legal Status & Litigation

US 6,051,252 has expired due to its 20-year patent term, which started from the filing date in 1994 and expired in 2014. No recent litigation or patent disputes are publicly associated with this patent, implying freedom to operate for compounds based on its disclosures.

Market Implications

The expiration opens the pathway for generic development and commercialization of drugs based on the covered compounds. Companies seeking to develop new norepinephrine reuptake inhibitors can reference the patent's disclosures but must avoid infringing active claims.

Summary of the chemical scope

Aspect Details
Core structure Quinolinone derivatives
Substitutions Halogens, alkyl, alkoxy groups at specific positions
Salts, derivatives, prodrugs Included in the scope
Therapeutic methods Treatment of depression, ADHD, CNS disorders

Summary of the patent landscape

Patent/Issuer Key features Filing/Expiration
US Patent 6,051,252 Quinolinone derivatives, methods of synthesis and use Filed 1994, expired 2014
US Patent 6,562,829 Similar compounds, related indications Filed 1998, expired 2018
WO Publications Broad chemical and use disclosures Filed 1996–1997
Eli Lilly SNRI compounds, related chemical scaffolds Filed early 2000s
Pfizer Reuptake inhibitors, similar chemical classes Filed late 1990s–2000s

Key Takeaways

  • US Patent 6,051,252 provides broad coverage of quinolinone derivatives for CNS treatment, focusing on specific substitution patterns.
  • Its claims extend to compounds, synthesis methods, and therapeutic use.
  • The patent has expired, allowing generic development of similar compounds.
  • The patent landscape features numerous filings from major pharma companies around related chemical scaffolds, indicating ongoing competitive activity.
  • Patent expiration reduces barriers for new entrants but also highlights the importance of methyl/structural modifications to avoid patent infringement.

FAQs

1. Can a company develop drugs based on compounds disclosed in US 6,051,252 now that it is expired?
Yes. The patent's expiration means the compounds are no longer protected by patent rights, enabling development and commercialization without infringement concerns, provided no other active patents cover specific modifications or uses.

2. Are there existing patents that still protect similar compounds?
Yes. Companies like Eli Lilly and Pfizer hold patents on related reuptake inhibitors, which may still be active depending on filing and expiration dates.

3. What are the key structural features protected by the patent?
The patent covers quinolinone cores with specific substitutions at defined positions, including halogen substitutions and alkyl groups.

4. How does this patent landscape influence R&D strategies?
The expiration of US 6,051,252 opens opportunities for generic manufacturers. Innovators can focus on novel chemical modifications or new therapeutic uses that do not infringe remaining active patents.

5. What are the primary therapeutic indications protected or covered in relation to these compounds?
Depression, ADHD, and other CNS disorders are the main indications associated with the compounds and methods disclosed.


References

  1. U.S. Patent and Trademark Office. (2022). Patent file wrappers and issued patents.
  2. WIPO. (1996-1997). WO Publications.
  3. Eli Lilly and Company. (2000s). Patent filings related to SNRI compounds.
  4. Pfizer Inc. (Late 1990s–2000s). Patent filings on reuptake inhibitors.
  5. U.S. Patent No. 6,051,252. (Issued 2000).

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Drugs Protected by US Patent 6,051,252

Applicant Tradename Generic Name Dosage NDA Approval Date TE Type RLD RS Patent No. Patent Expiration Product Substance Delist Req. Patented / Exclusive Use Submissiondate
>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 6,051,252

Country Patent Number Estimated Expiration Supplementary Protection Certificate SPC Country SPC Expiration
Argentina 008977 ⤷  Start Trial
Austria 234103 ⤷  Start Trial
Australia 1668301 ⤷  Start Trial
Australia 2199199 ⤷  Start Trial
Australia 742943 ⤷  Start Trial
Australia 762826 ⤷  Start Trial
>Country >Patent Number >Estimated Expiration >Supplementary Protection Certificate >SPC Country >SPC Expiration

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