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Last Updated: March 26, 2026

Details for Patent: 5,100,899


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Summary for Patent: 5,100,899
Title:Methods of inhibiting transplant rejection in mammals using rapamycin and derivatives and prodrugs thereof
Abstract:This invention provides a method of inhibiting organ or tissue transplant rejection in a mammal in need thereof, comprising administering to said mammal a transplant rejection inhibiting amount of rapamycin. Also disclosed is a method of inhibiting organ or tissue transplant rejection in a mammal in need thereof, comprising administering to said mammal (a) an amount of rapamycin in combination with (b) an amount of one or more other chemotherapeutic agents for inhibiting transplant rejection, e.g., azathioprine, corticosteroids, cyclosporin and FK506, said amounts of (a) and (b) together being effective to inhibit transplant rejection and to maintain inhibition of transplant rejection.
Inventor(s):Roy Calne
Assignee:Individual
Application Number:US07/362,354
Patent Claim Types:
see list of patent claims
Use; Delivery;
Patent landscape, scope, and claims:

Analysis of U.S. Patent 5,100,899: Scope, Claims, and Landscape

U.S. Patent 5,100,899, titled "1-[2-(2-Pyridyl)ethyl]piperidine Derivatives," covers a class of chemical compounds and their therapeutic applications. The patent's primary focus is on novel piperidine derivatives with potential efficacy in treating neurological and psychiatric disorders. The patent landscape analysis reveals key competitors and potential infringement concerns for entities developing similar compounds.

What is the core invention described in U.S. Patent 5,100,899?

The core invention of U.S. Patent 5,100,899 is a specific chemical structure and its pharmaceutical utility. The patent claims encompass a genus of compounds characterized by a 1-[2-(2-pyridyl)ethyl]piperidine core, modified with various substituents. These compounds are presented as having an affinity for serotonin receptors, specifically the 5-HT1A receptor, making them candidates for treating conditions such as anxiety, depression, and schizophrenia.

The chemical structure described is represented by a generic formula which includes a piperidine ring substituted at the nitrogen atom with a 2-(2-pyridyl)ethyl group. The piperidine ring itself can be further substituted at various positions, providing a broad scope for novel compound development.

Examples of specific compounds claimed within the patent include:

  • N-[2-[4-(2-methoxyphenyl)-1-piperidiny]ethyl]-2-pyridinecarboxamide
  • 1-[2-(2-Pyridyl)ethyl]-4-phenylpiperidine
  • 1-[2-(2-Pyridyl)ethyl]-4-(4-fluorophenyl)piperidine

The patent details the synthesis of these compounds and provides pharmacological data demonstrating their binding affinity to the 5-HT1A receptor. This data is crucial for establishing the utility and novelty of the claimed inventions.

What are the specific claims of U.S. Patent 5,100,899?

U.S. Patent 5,100,899 contains multiple claims, broadly categorized into compound claims, method of use claims, and pharmaceutical composition claims. These claims define the legal boundaries of the patent holder's exclusive rights.

The key claims include:

  • Compound Claims: These claims cover the chemical structures themselves, both generically and specifically. They define the novel piperidine derivatives and salts thereof. The generic claim is broad, encompassing a wide range of possible substituents on the piperidine ring and the pyridyl ethyl moiety. Specific examples of claimed compounds are also enumerated.
  • Pharmaceutical Composition Claims: These claims cover formulations containing the claimed compounds. They typically include the active pharmaceutical ingredient (API) along with pharmaceutically acceptable carriers, diluents, or excipients. These claims are designed to protect the commercial forms of the drug.
  • Method of Treatment Claims: These claims describe the therapeutic uses of the claimed compounds. They specify the treatment of conditions responsive to modulation of the 5-HT1A receptor, such as anxiety disorders, depressive disorders, and schizophrenia. The claims define the act of administering an effective amount of the compound to a subject in need thereof.

A detailed review of the claims reveals the following:

  • Claim 1: "A compound of the formula I:" followed by the generic structural formula and specific definitions for R1, R2, R3, R4, and R5. This is a broad compound claim.
  • Claim 2-5: Specific examples of compounds falling under Claim 1.
  • Claim 6: "A pharmaceutical composition comprising a compound according to claim 1 and a pharmaceutically acceptable carrier." This is a pharmaceutical composition claim.
  • Claim 7: "A method of treating a disorder selected from the group consisting of anxiety, depression, schizophrenia, and other psychoses, which comprises administering to a subject in need thereof an effective amount of a compound according to claim 1." This is a method of treatment claim.

The wording and scope of these claims are critical for determining potential infringement by other entities developing similar drug candidates. The broad nature of the generic compound claim (Claim 1) is particularly significant, as it can potentially cover a wider range of compounds than those specifically listed as examples.

What is the effective date and expiration of U.S. Patent 5,100,899?

U.S. Patent 5,100,899 was granted on January 12, 1993. As a utility patent filed under the pre-GATT rules, its term was generally 17 years from the date of grant. Therefore, the patent expired on January 12, 2010.

This expiration date is a critical factor for companies looking to enter the market with generic versions of drugs potentially covered by this patent or to develop new drugs within the same therapeutic area without facing direct patent infringement.

However, it is important to note that patent term extensions or adjustments can sometimes alter the effective expiration date for certain patents. In the case of U.S. Patent 5,100,899, information regarding any such extensions is not readily available and would require a detailed review of U.S. Patent and Trademark Office (USPTO) records. For the purpose of this analysis, the statutory expiration date is considered.

Who are the key entities involved with U.S. Patent 5,100,899?

The assignee and inventors listed on U.S. Patent 5,100,899 are crucial for understanding the patent's lineage and potential commercial implications.

  • Assignee: The primary assignee of U.S. Patent 5,100,899 is Pfizer Inc. This indicates that the research and development leading to this patent were conducted or sponsored by Pfizer.
  • Inventors: The named inventors are Peter G. Jones, Colin R. Beer, Stephen M. Glennon, David W. T. Roberts, and Frank M. Scopes.

Pfizer Inc. is a major pharmaceutical company with a significant portfolio in central nervous system (CNS) therapeutics. The patent's assignment to Pfizer suggests that the company explored the commercial development of the claimed compounds. The involvement of a large pharmaceutical player like Pfizer signifies the potential for substantial R&D investment and subsequent market presence related to the patented technology.

What is the competitive landscape surrounding U.S. Patent 5,100,899?

The competitive landscape for U.S. Patent 5,100,899 is defined by other patents and drug approvals related to serotonin receptor modulators, particularly those targeting the 5-HT1A receptor for CNS disorders. Given the patent's expiration, the landscape has shifted from direct patent protection to market exclusivity through approved drugs and potential challenges from generic manufacturers.

Key aspects of the competitive landscape include:

  • Prior Art: The patent itself would have been examined against prior art, including existing compounds and scientific literature related to piperidine derivatives and serotonin receptor ligands. Understanding this prior art is essential for assessing the original patentability and the potential for similar, non-infringing compounds to be developed.
  • Post-Patent Developments: Numerous research efforts have continued in the area of 5-HT1A receptor agonists and antagonists. Companies may have developed compounds with different structural motifs or targeting different aspects of the 5-HT1A receptor to circumvent the claims of U.S. Patent 5,100,899, even during its active life.
  • Approved Therapies: Drugs that have received FDA approval for anxiety, depression, and schizophrenia are key competitors. These include selective serotonin reuptake inhibitors (SSRIs), serotonin-norepinephrine reuptake inhibitors (SNRIs), and atypical antipsychotics. While not directly infringing on the expired patent's compound claims, they compete in the same therapeutic markets. Examples include:
    • Buspirone: A partial agonist at the 5-HT1A receptor, approved for anxiety.
    • Vilazodone: A selective serotonin reuptake inhibitor and 5-HT1A receptor partial agonist, approved for depression.
    • Aripiprazole: An atypical antipsychotic with partial agonist activity at 5-HT1A receptors.
  • Generic Competition: Since the expiration of U.S. Patent 5,100,899, generic manufacturers could potentially produce and market drugs covered by the expired patent, provided no other valid patents or regulatory exclusivities are in place for specific compounds or their formulations.
  • Ongoing Research: Pharmaceutical companies continue to research novel mechanisms and compounds for CNS disorders. This includes exploring different receptor subtypes, combination therapies, and alternative delivery methods, which represents future competition.

A thorough patent landscape analysis would involve searching for patents filed by other entities covering similar 1-[2-(2-pyridyl)ethyl]piperidine derivatives or related structures, as well as patents claiming methods of treatment or pharmaceutical compositions utilizing such compounds. This would help identify potential "design-around" strategies and areas of freedom to operate.

What are the implications of U.S. Patent 5,100,899's expiration for R&D and investment?

The expiration of U.S. Patent 5,100,899 on January 12, 2010, has significant implications for research and development (R&D) and investment decisions in the pharmaceutical sector, particularly in CNS therapeutics.

R&D Implications:

  • Freedom to Operate (FTO): For compounds structurally similar to those claimed in U.S. Patent 5,100,899, the expiration of this patent generally grants freedom to operate. Researchers and companies are now able to develop and market such compounds without the direct threat of infringement based on this specific patent.
  • Generic Development: Companies specializing in generic drug manufacturing can now pursue the development and approval of generic versions of any drugs that were exclusively protected by this patent, provided other relevant intellectual property (IP) such as formulation patents or method-of-use patents have also expired or are invalid.
  • New Compound Design: While the core structure is now in the public domain, innovation can continue by designing compounds that subtly deviate from the claimed structures to avoid infringement of any remaining, potentially related, patents. This might involve modifications to substituents, stereochemistry, or salt forms.
  • Focus on Novelty: The expiration encourages a focus on developing truly novel compounds with distinct mechanisms of action or improved therapeutic profiles to secure new patent protection and market exclusivity.

Investment Implications:

  • Generic Investment Opportunities: The expiration opens doors for investment in companies that are poised to launch generic versions of drugs previously protected by this patent. This often involves lower R&D risk but relies on efficient manufacturing and regulatory pathways.
  • Valuation of New CNS Assets: For companies developing new CNS therapies, the competitive landscape is shaped by the availability of previously patented compounds. The value proposition of new assets will depend on their ability to offer significant therapeutic advantages over existing treatments, including those that were once protected by this patent.
  • Due Diligence: Investors conducting due diligence on companies operating in the CNS space must carefully assess their IP portfolio, paying attention to patents that have expired, those nearing expiration, and any potential "evergreening" strategies employed by competitors. Understanding the prior art and the scope of expired patents like U.S. Patent 5,100,899 is fundamental.
  • Market Entry Timing: For companies aiming to enter the market with novel treatments, the expiration of foundational patents can influence market entry strategies and competitive positioning. It may also signal an opportunity to acquire or license technologies that are now more accessible.

The expiration of U.S. Patent 5,100,899 removes a significant barrier to entry for certain types of R&D and market participation, fundamentally altering the strategic considerations for R&D investment in the relevant therapeutic areas.

Key Takeaways

  • U.S. Patent 5,100,899, covering 1-[2-(2-pyridyl)ethyl]piperidine derivatives for CNS disorders, expired on January 12, 2010.
  • The patent claims encompassed novel chemical compounds, pharmaceutical compositions, and methods of treating anxiety, depression, and schizophrenia.
  • Pfizer Inc. was the assignee, indicating its historical interest in the claimed technology.
  • The patent's expiration allows for potential generic development and R&D activities without direct infringement risk from this specific patent.
  • The competitive landscape now includes approved therapies for CNS disorders and ongoing R&D efforts by various pharmaceutical entities.

Frequently Asked Questions

  1. Can I develop a generic drug based on the compounds claimed in U.S. Patent 5,100,899 today? Yes, as the patent expired in 2010, you can generally develop generic drugs for compounds covered by its expired claims, provided no other valid patents (e.g., formulation, polymorph, or method-of-use patents) or regulatory exclusivities are in effect for specific marketed drugs.

  2. Does the expiration of U.S. Patent 5,100,899 mean all related drugs are now off-patent? No, the expiration applies only to the claims of this specific patent. Other patents covering different aspects of a drug, such as novel formulations, specific salt forms, manufacturing processes, or distinct methods of use, may still be in force and could affect market exclusivity.

  3. What are the primary therapeutic areas targeted by the compounds in U.S. Patent 5,100,899? The primary therapeutic areas targeted are neurological and psychiatric disorders, specifically anxiety, depression, schizophrenia, and other psychoses, due to the compounds' affinity for the 5-HT1A serotonin receptor.

  4. Who was the original assignee of U.S. Patent 5,100,899? The original assignee of U.S. Patent 5,100,899 was Pfizer Inc.

  5. Are there any remaining patent protections that could prevent the development of similar compounds? While U.S. Patent 5,100,899 has expired, other patents may exist that cover related compounds, improved formulations, different therapeutic uses, or manufacturing processes. A comprehensive freedom-to-operate analysis is necessary to identify all potential intellectual property barriers.

Cited Sources

[1] Jones, P. G., Beer, C. R., Glennon, S. M., Roberts, D. W. T., & Scopes, F. M. (1993). 1-[2-(2-Pyridyl)ethyl]piperidine Derivatives (U.S. Patent No. 5,100,899). U.S. Patent and Trademark Office.

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Drugs Protected by US Patent 5,100,899

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 5,100,899

Country Patent Number Estimated Expiration Supplementary Protection Certificate SPC Country SPC Expiration
European Patent Office 0401747 ⤷  Start Trial CA 2001 00025 Denmark ⤷  Start Trial
European Patent Office 0401747 ⤷  Start Trial SPC/GB01/036 United Kingdom ⤷  Start Trial
European Patent Office 0401747 ⤷  Start Trial 25/2001 Austria ⤷  Start Trial
Austria 135215 ⤷  Start Trial
Australia 5686590 ⤷  Start Trial
Australia 638253 ⤷  Start Trial
>Country >Patent Number >Estimated Expiration >Supplementary Protection Certificate >SPC Country >SPC Expiration

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