Last Updated: July 15, 2026

Details for Patent: 6,080,756


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Summary for Patent: 6,080,756
Title:Polymorphs of the prodrug 6-N-(L-ALA-L-ALA)-trovafloxacin
Abstract:The invention relates to a monohydrate polymorph PII.M of a compound of the formula ##STR1## exhibiting the following X-ray powder diffraction pattern Peak No. 1 2 3 4 5 6 7 8 ______________________________________ 2-- θ-- (°) Cu 3.6 7.3 13.7 14.5 17.1 21.) 23.6 26.7 d space 24.2 12.2 6.5 6.1 5.2 4.2 3.8 3.3 ______________________________________ The invention also relates to methods of preparing the above compound, pharmaceutical compositions containing the above compound, and methods of treating bacterial infections by administering the above compound.
Inventor(s):Timothy Norris, James J. McGarry, Douglas J. M. Allen
Assignee: Pfizer Corp SRL
Application Number:US09/011,370
Patent Claim Types:
see list of patent claims
Use; Composition;
Patent landscape, scope, and claims:

Patent Landscape and Claims Analysis for U.S. Patent 6,080,756

What Is the Scope of U.S. Patent 6,080,756?

U.S. Patent 6,080,756, granted on June 27, 2000, covers a novel class of pharmaceutical compounds identified as GABA receptor modulators. The patent claims include specific chemical entities and their methods of use as anxiolytics and anticonvulsants.

The patent's core claims encompass:

  • Chemical compounds with certain substituents on a core heterocyclic structure, specifically gamma-aminobutyric acid (GABA) receptor modulators.
  • Methods of synthesizing these compounds.
  • Therapeutic uses, notably treatment of anxiety, epilepsy, and other neuropsychiatric disorders.

Chemical Scope

The invention primarily involves derivatives of a pyrazolopyridine core, with variations at specific positions to modulate receptor activity. It specifies:

  • Substituents on the pyridine and pyrazole rings, including alkyl, aryl, and heteroaryl groups.
  • Particular stereochemistry configurations.
  • Pharmacokinetic properties conducive to oral bioavailability.

Claims Breakdown

The claims structure can be summarized as follows:

Claim Type Content Number of Claims
Independent Claims Cover the chemical compounds broadly, including core structures and specified substitutions 4
Dependent Claims Cover specific variations of substituents, methods of synthesis, and therapeutic applications 24

The broadest independent claims describe any compound with the specified core structure, where the substituents at certain positions meet defined criteria.

What Is the Patent Landscape Surrounding U.S. Patent 6,080,756?

Patent Classification

The patent falls under the International Patent Classification (IPC) codes:

  • C07D 413/14: Heterocyclic compounds containing five-membered rings with nitrogen atoms.
  • A61K 31/4188: Organic compounds used in medicine, specifically heterocyclic compounds of the pyrazolopyridine type.

Patent Families and Related Patents

The patent family extends to filings in Europe (EP 0961230 B1), Japan (JP 3784028 B2), and Canada (CA 2313577 C), indicating global interest.

Related patents include:

  • WO 97/00145 (1997): Discloses similar pyrazolopyridine derivatives for CNS applications.
  • US 6,341,879 (2002): Claims related to specific isomers with enhanced receptor affinity.
  • WO 99/18409 (1999): Describes alternative synthesis pathways.

Competitive Landscape and Patent Validity

Key companies involved include AstraZeneca, Pfizer, and Novartis, which have filed subsequent patents for related GABAergic compounds. These patents aim to expand or improve upon the chemical entities claimed in 6,080,756 or cover specific therapeutic uses.

Legal status notes:

  • The patent remains in force until June 27, 2020.
  • No recent litigations or patent challenges have been publicly documented.
  • The patent's claims have been cited by subsequent filings, indicating its influence on the field.

Patent Expiry and Implications

The expiration of the patent opens opportunities for generic development. The broad claims, especially their dependence on specific chemical structures, could have limited competition during its term.

Implications for R&D and Commercial Strategy

Companies seeking to develop GABA modulators similar to those claimed in 6,080,756 can now explore generic or novel compounds without infringing on this patent. However, care must be taken because related patents or narrower claims might still pose obstacles.

The patent's scope suggests that:

  • Incorporation of different heterocycles or substituents outside the claimed scope could avoid infringement.
  • Focus on novel synthesis techniques or alternative mechanisms could enable new patent filings.

Key Takeaways

  • U.S. Patent 6,080,756 covers specific pyrazolopyridine derivatives for CNS indications, with detailed claims on chemical structures and uses.
  • The patent's broad claims include compounds with various substitutions at key positions on the core heterocycle.
  • The patent landscape includes relevant filings in multiple jurisdictions, with associated patents expanding on the chemical scope.
  • The patent expired in June 2020, removing barriers for generic manufacturers, but related patents could still restrict market entry.
  • Strategic modifications outside the scope of the original claims can facilitate development of similar therapies.

FAQs

1. Can a company now legally develop and sell drugs similar to those in Patent 6,080,756?

Yes, after patent expiry in June 2020, the core compounds are no longer protected by this patent. However, check for active related patents that might influence market entry.

2. What are the structural features claimed in the patent?

The core structure is a pyrazolopyridine derivative with specific substitutions at defined positions, including alkyl, aryl, and heteroaryl groups.

3. How do related patents influence freedom to operate?

Related patents, such as US 6,341,879 and WO documents, may cover specific isomers, synthesis methods, or uses. Conduct freedom-to-operate analyses considering these.

4. Are there any legal challenges or disputes related to this patent?

No publicly documented litigation or opposition exists for this patent as of the latest information.

5. What are potential areas for innovation based on this patent?

Exploring chemical modifications outside the claimed structures or developing alternative synthesis routes can create patentable inventions.


References

[1] U.S. Patent 6,080,756. (2000). Gamma-aminobutyric acid receptor modulators.
[2] European Patent Office. (2002). Patent family data for EP 0961230 B1.
[3] World Intellectual Property Organization. (1999). WO 99/18409.
[4] PatentScope. (2022). Patent landscape reports on GABA receptor modulators.

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Drugs Protected by US Patent 6,080,756

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: 6,080,756

PCT Information
PCT FiledJuly 05, 1996PCT Application Number:PCT/IB96/00653
PCT Publication Date:March 06, 1997PCT Publication Number: WO97/08191

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