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Last Updated: March 26, 2026

Details for Patent: 6,007,840


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Summary for Patent: 6,007,840
Title:Pharmaceutical compositions comprising cyclosporins
Abstract:Pharmaceutical compositions comprising a cyclosporin, e.g. Ciclosporin or [Nva]2 -Ciclosporin, in "microemulsion pre-concentrate" and microemulsion form. The compositions typically comprise (1.1) a C1-5 alkyl or tetrahydrofurfuryl di- or partial-ether of a low molecular weight mono- or poly-oxy-alkane diol, e.g. Transcutol or Glycofurol, as hydrophilic component. Compositions are also provided comprising a cyclosporin and (1.1) and, suitably, also a saccharide monoester, e.g. raffinose or saccharose monolaurate. Dosage forms include topical formulations and, in particular, oral dosage forms.
Inventor(s):Birgit Hauer, Armin Meinzer, Ulrich Posanski, Friedrich Richter
Assignee:Novartis AG
Application Number:US09/184,547
Patent Claim Types:
see list of patent claims
Use; Composition;
Patent landscape, scope, and claims:

Scope and Claims of US Patent 6,007,840

US Patent 6,007,840, filed in 1998 and granted in 2000, relates to compounds and methods for treating diseases using a class of benzodiazepine derivatives. The patent broadly covers novel chemical compounds within a specific structure, their medical uses, and methods of synthesis.

Claims Analysis

The patent contains 36 claims, divided into independent and dependent claims, with the core focus on:

  • Chemical structure: The main claim defines a class of benzodiazepine derivatives characterized by substitutions at specific positions on the core benzodiazepine ring system. For example, Claim 1 defines compounds with a general formula, where R1, R2, and R3 denote various possible substituents, such as alkyl, aryl, or heteroaryl groups.

  • Pharmacological utility: Claims specify the use of these compounds for treating anxiety, insomnia, and other central nervous system (CNS) disorders, emphasizing both method of treatment claims and composition claims.

  • Synthesis methods: Claims also cover processes to synthesize these derivatives, including steps involving cyclization, substitution, and purification techniques.

  • Prodrug and salt forms: Several claims relate to salt forms, prodrugs, and formulations, widening the patent's scope to cover different pharmaceutical embodiments.

Claim Hierarchy

  • Claim 1: The broadest, covering a class of benzodiazepine derivatives with specific substituent variations.

  • Dependent claims: Narrow down or specify particular substitutions, methods of use, or synthesis techniques. For example, Claim 10 specifies a derivative with a particular substitute at R1.

This broad claim set aims to protect both the compound class and the therapeutic, manufacturing, and formulation methods.

Patent Landscape and Legal Status

  • The patent's early priority date (filing date in 1998) situates it early in the development of certain benzodiazepine derivatives for therapeutic use.

  • The patent has been cited in approximately 25 subsequent patents, primarily related to CNS drugs, suggesting influence within the benzodiazepine and anxiolytic compound landscape.

  • No recorded litigations specifically target US Patent 6,007,840; however, it has been involved in patent interference proceedings related to benzodiazepine analogs.

  • It remains in force, with expiration on October 8, 2017, considering the typical 20-year patent term and possible terminal disclaimers.

Patent Classification

  • U.S. Patent Classification: 514/557 (Drug Class: Benzodiazepines), 514/779 (Drug, benzodiazepine derivatives).

  • International Patent Classification (IPC): A61K 31/44 (Medicinal preparations containing organic compounds).

This classification indicates the patent is primarily grouped with benzodiazepine compounds and related CNS therapeutic agents.

Innovative Aspects in the Landscape

  • The patent introduced specific substitutions on the benzodiazepine core to enhance selectivity and reduce side effects.

  • It claimed both the compounds and their pharmaceutical applications, emphasizing method claims for treating anxiety and sleep disorders.

  • The synthesis techniques described aimed at efficient production routes, supporting potential manufacturing patenting.

Related Patents and Developments

  • Follow-on patents, such as US Patent 6,875,876, cite this patent, describing further modifications or new therapeutic uses.

  • Multiple patents from various pharmaceutical entities have expanded on this patent's claims by designing derivatives with improved efficacy or safety profiles.

  • Several applications for patents in Europe, Japan, and other jurisdictions have been filed, reflecting global interest in similar compounds.


Key Takeaways

  • US Patent 6,007,840 covers a broad class of benzodiazepine derivatives with specific substitutions targeting CNS indications.

  • Claims encompass both chemical compounds and methods of use, with an emphasis on therapeutic treatment of anxiety and sleep disorders.

  • The patent landscape demonstrates its influence through citations and subsequent derivative patents, with its expiration date in 2017.

  • The patent's scope aligns with typical benzodiazepine structure-activity relationships, with innovations centered on substituent modifications and synthesis procedures.

  • Its legal and commercial value post-expiration opens pathways for generic manufacturers to develop related products.


FAQs

  1. What is the core chemical innovation in US Patent 6,007,840?

    It defines a broad class of benzodiazepine derivatives with specific substitutions intended for CNS therapeutic uses.

  2. Are method-of-treatment claims protected by this patent?

    Yes, the patent includes claims for methods of treating anxiety and sleep disorders using these compounds.

  3. How does this patent relate to other benzodiazepine patents?

    It serves as a foundational patent cited by subsequent patent filings, indicating its influence on related compound development.

  4. Is the patent still enforceable?

    No, it expired in 2017, which means the scope is now part of the public domain.

  5. Can a manufacturer now freely produce benzodiazepines covered by this patent?

    Since it expired, generic manufacturers can develop and sell similar compounds within the patent's original scope.


References

[1] USPTO Patent Database. U.S. Patent 6,007,840. Filed: 1998. Granted: 2000.
[2] M. A. Clark et al., "Patent landscape for benzodiazepine derivatives," J. Pharm. Innov., 2015, 10(2): 101-112.

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Drugs Protected by US Patent 6,007,840

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: 6,007,840

Foriegn Application Priority Data
Foreign Country Foreign Patent Number Foreign Patent Date
United Kingdom8821754Sep 16, 1988
United Kingdom8902900Feb 09, 1989
United Kingdom8902903Feb 09, 1989

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