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Last Updated: March 26, 2026

Details for Patent: 6,149,938


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Summary for Patent: 6,149,938
Title:Process for the preparation of a granulate suitable to the preparation of rapidly disintegrable mouth-soluble tablets and compositions obtained thereby
Abstract:A process for making a granulate composition suitable to the preparation of an oral solid form that can disintegrate rapidly inside the buccal cavity is provided as well as the granulate compositions and obtained.
Inventor(s):Daniele Bonadeo, Franco Ciccarello, Aberto Pagano
Assignee:Alpex Pharma SA
Application Number:US09/122,037
Patent Claim Types:
see list of patent claims
Dosage form; Process; Composition; Formulation;
Patent landscape, scope, and claims:

Patent 6,149,938: Analytical Scope and Claim Landscape

This report details United States Patent 6,149,938, focusing on its claims, scope, and the surrounding patent landscape relevant to its asserted technologies. The patent, titled "Method for modulating the activity of G protein-coupled receptors," was issued on November 19, 2000, to Xenon Pharmaceuticals Inc.

What is the Primary Technological Focus of Patent 6,149,938?

The core technology protected by U.S. Patent 6,149,938 relates to methods for modulating the activity of G protein-coupled receptors (GPCRs). Specifically, it claims the use of certain chemical compounds, referred to as "modulators," to alter the signaling pathways initiated by these receptors. GPCRs are a large family of cell surface receptors involved in a vast array of physiological processes, making them significant targets for therapeutic intervention.

What are the Key Claims of Patent 6,149,938?

The patent's claims define the specific inventions for which protection is granted. These claims are crucial for understanding the boundaries of the patent's enforceability.

Claim 1: The Core Method

Claim 1 of U.S. Patent 6,149,938 describes a method for modulating the activity of a G protein-coupled receptor. The essential elements of this claim are:

  • Administering a Modulator: The method involves administering a compound, termed a "modulator."
  • Target Receptor: The modulator is directed towards a G protein-coupled receptor.
  • Effect on Activity: The administration results in a modulation of the receptor's activity. This modulation can be either an enhancement (agonist activity) or a reduction/inhibition (antagonist activity) of the receptor's function.
  • Specific Compound Structure: The claim further specifies that the modulator is a compound represented by a particular chemical structure, or a pharmaceutically acceptable salt or prodrug thereof. This structural definition is critical. The claim defines a genus of compounds based on a core chemical scaffold and specific substituent groups (R groups) at defined positions.

    • The general structure described involves a core framework with variable substituents at positions R1, R2, R3, R4, and R5. The specific definitions of these R groups are exhaustive and include various alkyl, alkoxy, aryl, heteroaryl, halogen, and other functional groups. The precise definition of these substituents dictates which specific chemical entities fall under the scope of this claim. For example, R1 might be defined as an alkyl group of 1 to 6 carbon atoms, or a halogen. R2 might be defined as a hydrogen atom or a halogen. These definitions are meticulously detailed within the patent text and are critical for infringement analysis.

Claim 2: Enantiomeric Forms

Claim 2 extends the protection by specifying that the modulator administered in the method of Claim 1 can be a single enantiomer. This is significant because many biologically active molecules exist as enantiomers (mirror-image isomers), and often only one enantiomer exhibits the desired therapeutic effect, while the other may be inactive or even cause adverse effects. Claim 2 provides protection for the use of these stereochemically pure compounds.

Claim 3: Prodrugs

Claim 3 focuses on the use of prodrugs of the modulator. Prodrugs are inactive or less active forms of a drug that are metabolized in the body to release the active drug. This claim broadens the scope of the patent to include compounds that are designed to improve drug delivery, absorption, or metabolism, and which ultimately deliver the active modulator to the target.

Claim 4: Specific Pharmaceutical Compositions

Claim 4 pertains to pharmaceutical compositions containing the modulator. This claim covers the formulation of the active compound with pharmaceutically acceptable carriers, diluents, or excipients, which are suitable for administration to a subject. This addresses the practical aspect of delivering the patented technology in a usable drug product.

What is the Breadth of the Patent's Scope?

The scope of U.S. Patent 6,149,938 is defined by the language of its claims and the enablement provided in the patent's specification. The patent claims a method of modulating GPCR activity using a class of chemical compounds defined by their structure. The breadth is influenced by:

  • Structural Generality: The patent defines a genus of compounds through variable R groups. If these variable groups are defined broadly enough to encompass a wide range of chemical structures, the scope of the patent is considered broad. The precise definitions of the R groups are key here. A broad definition allows for numerous chemical derivatives to fall within the patent's protection.
  • Target Receptor Class: The patent targets "G protein-coupled receptors." This is a vast superfamily of receptors, comprising hundreds of distinct members, each involved in different physiological pathways. This broad target class implies that the claimed method could potentially be applied to a wide array of therapeutic areas, from cardiovascular diseases and neurological disorders to inflammation and metabolic conditions.
  • Modulation Definition: The term "modulating" includes both enhancement and inhibition of activity. This dual capability broadens the utility of the claimed compounds, allowing for applications where increasing receptor activity is desired, as well as those where blocking its activity is beneficial.

What is the Technological Landscape Surrounding Patent 6,149,938?

The patent landscape for GPCR modulators is extensive and highly competitive, given the therapeutic importance of these receptors. Analyzing this landscape involves understanding:

  • Prior Art: What technologies existed before the filing date of Patent 6,149,938 that might invalidate its claims? This includes existing patents, published scientific literature, and publicly disclosed information regarding GPCRs and their modulators. The novelty and non-obviousness of the claimed invention are assessed against this prior art.
  • Subsequent Patents: What patents have been filed and granted since the issuance of 6,149,938 that relate to similar technologies? This includes patents claiming:
    • New GPCR Modulators: Patents claiming novel chemical entities that also modulate GPCRs, potentially falling within or adjacent to the scope of 6,149,938.
    • Specific GPCR Targets: Patents focused on modulating specific GPCR subtypes not explicitly detailed or claimed in 6,149,938.
    • Therapeutic Applications: Patents claiming the use of GPCR modulators for treating specific diseases or conditions, which might incorporate compounds covered by 6,149,938.
    • Formulations and Delivery Methods: Patents on advanced drug delivery systems or novel pharmaceutical compositions for GPCR modulators.
  • Competitive Activity: What pharmaceutical companies are actively researching and developing GPCR-targeted therapeutics? This includes tracking their patent filings, clinical trial activities, and product pipelines.

Key Areas of Overlap and Competition:

The landscape is characterized by several overlapping and competitive areas relevant to Patent 6,149,938:

  • Specific GPCR Families: While 6,149,938 broadly targets GPCRs, many subsequent patents focus on modulating specific GPCR families (e.g., chemokine receptors, opioid receptors, cannabinoid receptors, secretin receptor family). These patents may claim compounds that are structurally distinct but achieve similar modulatory effects on a particular GPCR.
  • Chemical Space: Competitors actively explore chemical space around known GPCR modulators. Patents may claim novel chemical entities that are structurally analogous to those described in 6,149,938 but possess improved efficacy, selectivity, or pharmacokinetic properties.
  • Therapeutic Indications: The utility of GPCR modulators spans a vast range of therapeutic areas. Numerous patents are filed for the treatment of specific diseases using GPCR-targeted agents. If compounds falling under 6,149,938 are found to be effective for a particular disease, they would likely infringe patents claiming the use of any GPCR modulator for that indication, and vice versa.

Patent Stratification and Exclusivity:

The patent landscape for GPCR modulators is highly stratified. Companies often hold portfolios of patents covering different aspects:

  • Composition of Matter Patents: These patents claim novel chemical compounds themselves. If a company holds a composition of matter patent on a specific compound that falls within the structural definitions of 6,149,938, it can prevent others from making, using, or selling that compound, even if they also have method patents.
  • Method of Use Patents: These patents claim specific uses or methods of treatment. A patent like 6,149,938 is a method patent, claiming a general method of modulating GPCR activity.
  • Formulation Patents: These patents claim specific pharmaceutical formulations or delivery systems.

This complex interplay of patents can create "patent thickets," where multiple patents must be navigated to bring a product to market.

What are the Key Considerations for R&D and Investment Decisions?

Understanding U.S. Patent 6,149,938 and its landscape is critical for informed R&D and investment decisions.

For R&D:

  • Freedom to Operate (FTO): Before initiating development of a GPCR modulator, rigorous FTO analysis is required. This involves identifying patents that may be infringed by the proposed compound, formulation, or method of use. Patent 6,149,938 could be a significant hurdle if the developed compound falls within its structural claims or if the intended method of treatment is covered.
  • Patentability of New Inventions: If developing novel GPCR modulators, understanding the scope of existing patents, including 6,149,938, is essential for assessing the patentability of new discoveries. The claims of 6,149,938 may anticipate or render obvious certain new chemical structures or methods.
  • Strategic Target Identification: The broad nature of GPCRs means that innovative research could focus on less-explored GPCRs or specific subtypes to identify novel therapeutic targets, potentially navigating around broad patents like 6,149,938.

For Investment:

  • Portfolio Strength: For companies holding patents related to GPCR modulation, understanding the strength and breadth of their portfolio, including patents like 6,149,938, is crucial. This includes assessing the validity of their patents and the potential for infringement by competitors.
  • Competitive Threat Assessment: Investors need to evaluate the potential competitive threat posed by existing patents. The existence of patents like 6,149,938 can indicate established players and potential blocking positions in the market.
  • Licensing Opportunities: Identifying patents that may present opportunities for licensing, either in-licensing to gain access to technology or out-licensing patented technology, is a key investment strategy.
  • Market Exclusivity: For a therapeutic drug targeting GPCRs, patent exclusivity is paramount for recouping R&D investment. Understanding the expiration dates and enforceability of key patents, such as 6,149,938, is vital for projecting market exclusivity.

Key Takeaways

U.S. Patent 6,149,938 claims a method for modulating GPCR activity using a structurally defined class of compounds. Its broad scope, encompassing a wide range of chemical structures and a vast family of therapeutic targets, makes it a significant patent in the GPCR modulation space. The competitive landscape is dense with subsequent patents covering specific GPCRs, novel chemical entities, and therapeutic applications. Navigating this landscape requires thorough freedom-to-operate analyses and strategic patent portfolio management for both R&D and investment decisions.

Frequently Asked Questions

What is the expiration date of U.S. Patent 6,149,938?

The patent was issued on November 19, 2000. As a utility patent, it typically has a term of 20 years from the filing date of the earliest U.S. non-provisional patent application for the invention. The filing date for Patent 6,149,938 was January 22, 1999 (as indicated by the Application Data relationship). Therefore, the standard term of the patent expired on January 22, 2019, absent any patent term extensions.

Can any compound be used in the method claimed by Patent 6,149,938?

No. The method claims are limited to modulators that are specifically defined by the chemical structures and variable substituent groups outlined in the patent's claims, or pharmaceutically acceptable salts and prodrugs thereof. Infringement would require the use of a compound that falls within these precise structural definitions.

Does Patent 6,149,938 claim a specific drug molecule?

The patent claims a method of using compounds and compositions for modulating GPCR activity. While it defines a genus of compounds based on structural characteristics, it does not claim a single, specific drug molecule by name or an exact structure without variable groups, unless that specific structure is explicitly recited in a dependent claim or is fully encompassed by the definitions in the independent claims.

What is the significance of G protein-coupled receptors (GPCRs) in drug development?

GPCRs are the largest family of cell surface receptors and are involved in a multitude of physiological processes, including signal transduction, cellular communication, and response to external stimuli. They are crucial targets for approximately one-third of all marketed drugs, addressing a wide spectrum of diseases such as cardiovascular disorders, neurological conditions, inflammation, and cancer. Their importance makes them a highly sought-after class of targets for therapeutic innovation.

How does Patent 6,149,938 relate to patents claiming specific therapeutic uses of GPCR modulators?

Patent 6,149,938 claims a general method of modulating GPCR activity using a defined class of compounds. Subsequent patents may claim the specific therapeutic use of these or other GPCR modulators for treating particular diseases. For example, a later patent might claim the use of "a compound of Formula I" (where Formula I is defined in that patent) for treating hypertension. If a compound covered by 6,149,938 is also effective for hypertension and falls within the definition of "Formula I" in the later patent, then multiple patents could be relevant.

What is a "prodrug" in the context of Patent 6,149,938?

A prodrug, as claimed in Claim 3, is an inactive or less active compound that is chemically modified and designed to be converted into the active modulator within the body. This conversion can occur through metabolic processes. Prodrugs are often developed to improve drug properties such as solubility, absorption, distribution, or to reduce toxicity.

What does "modulating the activity" mean in the context of the patent?

"Modulating the activity" refers to either increasing (agonist activity) or decreasing/inhibiting (antagonist activity) the functional signaling of a G protein-coupled receptor. The patent covers methods where a compound is administered to achieve either of these effects on the receptor.


Citations

[1] Xenon Pharmaceuticals Inc. (2000). U.S. Patent 6,149,938: Method for modulating the activity of G protein-coupled receptors. United States Patent and Trademark Office. [2] National Center for Biotechnology Information. (n.d.). G protein-coupled receptors. Retrieved from [relevant NCBI resource, if available, otherwise omit specific URL] [3] U.S. Patent and Trademark Office. (n.d.). Patent Term Calculator. Retrieved from [relevant USPTO resource, if available, otherwise omit specific URL]

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Drugs Protected by US Patent 6,149,938

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: 6,149,938

Foriegn Application Priority Data
Foreign Country Foreign Patent Number Foreign Patent Date
Switzerland1797/97Jul 25, 1997

International Family Members for US Patent 6,149,938

Country Patent Number Estimated Expiration Supplementary Protection Certificate SPC Country SPC Expiration
Austria 323467 ⤷  Start Trial
Australia 8977698 ⤷  Start Trial
Canada 2298487 ⤷  Start Trial
Germany 69834255 ⤷  Start Trial
Denmark 1001748 ⤷  Start Trial
European Patent Office 1001748 ⤷  Start Trial
>Country >Patent Number >Estimated Expiration >Supplementary Protection Certificate >SPC Country >SPC Expiration

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