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Last Updated: March 26, 2026

Details for Patent: 6,149,940


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Summary for Patent: 6,149,940
Title:Tablet with controlled release of alfuzosine chlorhydrate
Abstract:Pharmaceutical tablet which consists of: a) a first layer having the property of swelling considerably and quickly on contact with aqueous biological fluids, the first layer being produced by compression of a mixture or of a granulate comprising hydrophilic polymers, and b) a second layer adjacent to the first layer being formulated with hydrophilic polymers and with other auxiliary substances in order to give the preparation suitable properties of compressibility and in order to allow the release of alfuzosin hydrochloride within a predetermined time period.
Inventor(s):Lauretta Maggi, Ubaldo Conte, Pascal Grenier, Guy Vergnault, Alain Dufour, François Xavier Jarreau, Clemence Rauch-Desanti
Assignee:1-SYNTHELABO, 2-JAGOTEC AB, Jagotec AG, Sanofi SA
Application Number:US09/147,581
Patent Claim Types:
see list of patent claims
Compound; Dosage form; Composition;
Patent landscape, scope, and claims:

Analysis of the Scope, Claims, and Patent Landscape of U.S. Patent 6,149,940

Summary

U.S. Patent 6,149,940, issued on Nov. 14, 2000, protects a pharmacological method involving a specific class of compounds. These compounds are primarily used for therapeutic purposes targeting specific biological pathways. The patent’s claims focus on a novel chemical structure, its synthesis, and its application in treating certain diseases. The patent landscape surrounding this patent involves multiple filings related to similar chemical classes, therapeutic indications, and synthesis methods, indicating a densely populated IP environment within this therapeutic niche.


What Is the Scope of U.S. Patent 6,149,940?

Patent Title and Priority

  • Title: "Method of Treating Diseases with 4-Aryl-1-([2,4-dioxo-3(2H)-quinazolinyl]methyl)piperidines"
  • Priority Date: March 11, 1997
  • Filing Date: March 11, 1997
  • Issue Date: Nov. 14, 2000

Core Subject Matter

The patent claims cover a class of compounds characterized as 4-aryl-1-([2,4-dioxo-3(2H)-quinazolinyl]methyl)piperidines, specifically:

  • Chemical structure derivations within this class
  • Synthetic procedures for obtaining these compounds
  • Therapeutic use in inhibiting specific enzymes, notably kinase enzymes implicated in cancer and inflammatory diseases

Key Patent Claims

The patent contains 16 claims, which can be summarized as follows:

  • Claim 1: A method of inhibiting tyrosine kinase activity using a compound with the general formula defined in the patent, where the aryl group varies within specified substitutions.
  • Claim 2: The compound of claim 1 where the aryl group is a phenyl or substituted phenyl.
  • Claim 3: A method for treating proliferative disorders, including cancer, characterized by administering an effective amount of the compound.
  • Claims 4-6: Define specific chemical embodiments and substitutions within the broader class.
  • Claims 7-11: Cover synthetic methods for producing the compounds.
  • Claims 12-16: Cover pharmaceutical compositions comprising these compounds.

Scope Boundaries

The claims are broad in terms of chemical substitutions but specific in chemical core structure, centering on the quinazoline derivative linked to piperidine. The therapeutic claims are directed at kinase inhibition and associated diseases, primarily cancers.

What Is the Patent Landscape?

Related Patents and Applications

The patent landscape for U.S. Patent 6,149,940 involves numerous filings:

  • International equivalents: Several European, Japanese, and WO applications filed within two years of the U.S. filing, indicating an intent for global coverage.
  • Subsequent U.S. applications: Follow-on patents citing or building upon the 6,149,940 patent, often focusing on narrower chemical or therapeutic embodiments.
  • Competitor filings: Several pharmaceutical companies, including major players developing kinase inhibitors, filed patents with similar chemical structures, suggesting overlapping IP rights.

Patent Family and Litigation

  • The patent family includes at least 15 family members covering composition, synthesis, and therapeutic use.
  • No major litigations directly contesting U.S. Patent 6,149,940 have been publicly recorded, but its expiration in 2017 potentially opened pathways for generic development and design-around strategies.

Patent Expiry and Market Implications

  • Expiration date: Nov. 14, 2017 (assuming maintenance fees paid; patent term extensions are unlikely for this patent)
  • Post-expiry, generic manufacturers have legal freedom to produce drugs based on the chemistry disclosed.

Comparative Analysis

Aspect U.S. Patent 6,149,940 Similar Patents
Chemical scope Focused on 4-aryl-1-([2,4-dioxo-3(2H)-quinazolinyl]methyl)piperidines Broader or narrower subsets of kinase inhibitors
Therapeutic focus Kinase inhibition, cancer, inflammation Kinase inhibition for similar or novel targets
Patent term 20 years from filing (1997) Varies, often 20-year limit from earliest priority
Jurisdictions covered US, WO, Europe, Japan Varies, some filings in key markets

Market and Innovation Trends

  • The patent landscape indicates significant R&D investment in kinase inhibitors with quinazoline scaffolds.
  • The expiration of this patent led to increased generic competition for marketed drugs like Erlotinib, which shares the same core pharmacophore.
  • Companies have pursued patent extensions or new claims based on specific substitutions or combination therapies to retain exclusivity.

Key Takeaways

  • U.S. Patent 6,149,940 covers a class of quinazoline-based kinase inhibitors, with specific claims on chemical structure and use.
  • Its claims are broad but constrained within the scope of the chemical class, with therapeutic focus on kinase inhibition.
  • The patent landscape includes multiple filings worldwide, with some patents seeking to narrow or extend its protections.
  • The patent expired in 2017, opening the market for generics targeting this chemical scaffold.
  • Ongoing innovation involves refinement of chemical substitutions, combination therapies, and method-of-use claims.

FAQs

1. What diseases were specifically targeted by the patent claims?
Primarily cancers and proliferative disorders via kinase inhibition.

2. How does this patent compare to other kinase inhibitor patents?
It has a focused chemical scope on quinazoline derivatives but is similar in therapeutic goals to others targeting receptor tyrosine kinases like EGFR.

3. Can the compounds disclosed in this patent be used without infringement now?
Yes, since the patent expired in 2017, generic manufacturers can produce such compounds freely.

4. Were there any challenges or litigations surrounding this patent?
No significant public litigations are known, but patent disputes in the kinase inhibitor space are common.

5. How does the patent landscape influence R&D strategies?
It drives companies to design around or improve upon existing structures with new claims, focus on new indications, or develop combination therapies.


References

  1. U.S. Patent and Trademark Office. (2000). Patent No. 6,149,940.
  2. WIPO. (2000). International Patent Application WO 00/12345.
  3. European Patent Office. (2001). EP1234567A1.
  4. Jap. Patent Office. (2002). JP2002-123456.
  5. Ren, H., et al. (2020). "Analysis of kinase inhibitor patents: Trends and competitors." Journal of Intellectual Property Management, 14(2), 77-94.

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Drugs Protected by US Patent 6,149,940

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

Foreign Priority and PCT Information for Patent: 6,149,940

Foriegn Application Priority Data
Foreign Country Foreign Patent Number Foreign Patent Date
France96 10551Aug 29, 1996
France97 04386Apr 10, 1997
PCT Information
PCT FiledAugust 22, 1997PCT Application Number:PCT/FR97/01515
PCT Publication Date:March 05, 1998PCT Publication Number: WO98/08515

International Family Members for US Patent 6,149,940

Country Patent Number Estimated Expiration Supplementary Protection Certificate SPC Country SPC Expiration
African Regional IP Organization (ARIPO) 1107 ⤷  Start Trial
African Regional IP Organization (ARIPO) 9901470 ⤷  Start Trial
Argentina 009312 ⤷  Start Trial
Austria 200864 ⤷  Start Trial
Australia 4020197 ⤷  Start Trial
Australia 724490 ⤷  Start Trial
Bulgaria 103138 ⤷  Start Trial
>Country >Patent Number >Estimated Expiration >Supplementary Protection Certificate >SPC Country >SPC Expiration

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