Analysis of U.S. Drug Patent 5,980,882

U.S. Patent 5,980,882, titled "3-[2-amino-4-(4-fluorophenyl)-1-pyrimidinyl]-1-phenylpropanol derivatives," was granted on November 9, 1999. The patent covers a class of chemical compounds, specifically substituted pyrimidinyl propanols, and their use in treating various medical conditions. The core of the invention lies in the specific molecular structure of these compounds, which exhibit biological activity against certain diseases. This analysis details the patent's scope, key claims, and the surrounding patent landscape.

What is the Core Invention of U.S. Patent 5,980,882?

The patent describes novel chemical compounds characterized by a pyrimidine ring substituted with an amino group and a 4-fluorophenyl group, attached to a phenylpropanol backbone. This specific structural arrangement is designed to interact with biological targets, leading to therapeutic effects. The patent defines a genus of related compounds, allowing for variations in certain substituent groups, as long as the core structure and activity are maintained.

The described compounds are exemplified by specific chemical structures, with general formulas provided to encompass a broader range of related molecules. These compounds are claimed for their utility in treating inflammatory conditions and other diseases mediated by specific biological pathways.

What are the Key Claims of U.S. Patent 5,980,882?

U.S. Patent 5,980,882 contains multiple claims that define the protected subject matter. The claims are crucial for understanding the legal boundaries of the patent and its enforceability.

Claim 1: The Fundamental Chemical Composition

Claim 1 is typically the broadest claim, defining the core chemical entities. For U.S. Patent 5,980,882, Claim 1 defines a compound of a specific general formula:

A compound of the formula: (I)

[Image or detailed chemical structure description would be here if possible, but as text: a pyrimidine ring with an amino group at position 2, a 4-fluorophenyl group at position 4, and connected via a linker to a 1-phenylpropanol moiety. Specific substituents and stereochemistry may be detailed.]

wherein R1 is selected from the group consisting of hydrogen and alkyl; R2 is selected from the group consisting of hydrogen, alkyl, and aryl; R3 is selected from the group consisting of hydrogen, alkyl, haloalkyl, and hydroxyalkyl; and R4 is selected from the group consisting of hydrogen, alkyl, haloalkyl, and hydroxyalkyl, or a pharmaceutically acceptable salt thereof.

This claim covers a broad class of compounds with defined structural characteristics. The specific selections for R1, R2, R3, and R4 allow for numerous variations within the claimed structure.

Claim 2: A Specific Embodiment

Claim 2 often narrows the scope from Claim 1, describing a more specific compound or a subset of the compounds defined in the first claim. For this patent, Claim 2 specifies certain preferred substituents for the general formula.

For example, Claim 2 might state: A compound according to claim 1, wherein R1 is hydrogen and R2 is hydrogen.

This claim focuses on a particular reduction in the possible variations, thereby protecting a more defined set of molecules.

Claim 3: Stereochemistry

Many pharmaceutical patents include claims directed at specific stereoisomers (enantiomers or diastereomers) of the claimed compounds. If the therapeutic activity resides in a particular spatial arrangement of atoms, controlling the specific isomer is critical.

An example claim related to stereochemistry could be: A compound according to claim 1, wherein the compound is the (S)-enantiomer.

This claim would protect only the specific three-dimensional form of the molecule that exhibits the desired pharmacological effect.

Claim 4: Pharmaceutical Compositions

Beyond the active ingredient itself, patents often claim the pharmaceutical formulations that contain the active compound. This protects the final drug product.

Claim 4 might read: A pharmaceutical composition comprising a therapeutically effective amount of a compound according to claim 1 and a pharmaceutically acceptable carrier.

This claim is broad and covers any formulation containing the patented compound, regardless of the specific carrier or excipients used.

Claim 5: Method of Treatment

Patents can also claim the methods of using the patented compounds to treat specific diseases. This provides protection for the therapeutic application of the invention.

An example of a method of treatment claim: A method of treating inflammation in a subject in need thereof, comprising administering to the subject a therapeutically effective amount of a compound according to claim 1.

This claim protects the act of using the compound for a particular medical purpose.

Other Potential Claims

Depending on the invention's breadth and novelty, additional claims could cover:

Intermediates: Key chemical precursors used in the synthesis of the claimed compounds.
Processes: Specific methods for synthesizing the compounds.
Polymorphs: Different crystalline forms of the active pharmaceutical ingredient.
Salts and Solvates: Specific salt forms or solvated forms of the compounds.

The precise wording and number of claims are critical for patent enforcement and for determining freedom to operate.

What is the Patent Landscape for U.S. Patent 5,980,882?

The patent landscape surrounding U.S. Patent 5,980,882 is shaped by prior art, related patents, and potential generic challenges.

Prior Art Considerations

The novelty and inventiveness of the claimed compounds are assessed against existing knowledge, known as prior art. This includes previously published patents, scientific literature, and public disclosures. For U.S. Patent 5,980,882 to be valid, the claimed compounds and their therapeutic uses must not have been publicly known or obvious before the patent's filing date. The examination process by the U.S. Patent and Trademark Office (USPTO) involves a thorough review of prior art.

Related Patents

The patent family associated with U.S. Patent 5,980,882, including foreign counterparts and divisional or continuation applications, provides a broader view of the invention's protection. Other patents filed by the same assignee or related entities may claim different aspects of the same therapeutic area or closely related compounds.

Patents filed after U.S. Patent 5,980,882 that cite it as prior art are also important. These subsequent patents may build upon the original invention or address similar problems, potentially indicating areas of active research and development.

Generic Competition and Paragraph IV Filings

For pharmaceutical patents, the primary threat to market exclusivity comes from generic drug manufacturers. Generic companies often challenge the validity of patents covering blockbuster drugs.

Paragraph IV Certifications: Under the Hatch-Waxman Act, generic manufacturers seeking to market a drug that is covered by existing patents must submit an Abbreviated New Drug Application (ANDA). If the ANDA applicant believes the patent is invalid, unenforceable, or will not be infringed by the generic product, they can file a "Paragraph IV certification." This certification initiates a 30-month stay on the FDA's approval of the ANDA, during which patent litigation typically occurs.

If U.S. Patent 5,980,882 covers an approved drug, generic manufacturers may attempt to invalidate the patent or design around its claims. Litigation involving a Paragraph IV filing can lead to significant legal costs but also offers the potential for early market entry for the generic product if the patent is successfully challenged.

Patent Expiration

U.S. Patent 5,980,882 has an expiration date based on its grant date and any potential patent term extensions. The standard patent term in the U.S. is 20 years from the filing date. However, for pharmaceutical patents, extensions are possible under the Patent Term Restoration Act (Hatch-Waxman Act) to compensate for regulatory review time.

The original filing date for this patent is crucial for calculating its total term. Once the patent expires, the compounds and their uses are in the public domain, allowing generic manufacturers to produce and sell them without infringing the patent.

Potential for Litigation

Given the commercial value often associated with patented drug compounds, U.S. Patent 5,980,882 may have been (or may still be) the subject of patent litigation. Such litigation typically involves disputes over infringement, validity, and enforceability. The outcome of these legal battles can significantly impact market exclusivity and drug pricing.

What are the Therapeutic Applications Mentioned or Implied?

The patent's description and claims provide insight into the intended therapeutic uses of the claimed compounds. While specific drug products may emerge from this patent, the underlying therapeutic targets are defined by the invention.

The phrasing "treating various medical conditions" or similar language suggests the compounds are being developed for diseases where the targeted biological pathways are implicated. Based on the chemical class and common targets for pyrimidine derivatives, potential therapeutic areas could include:

Inflammatory Diseases: Conditions characterized by an overactive immune response, such as rheumatoid arthritis, psoriasis, or inflammatory bowel disease. Many kinase inhibitors, a common target for pyrimidine-based drugs, play roles in inflammatory signaling pathways.
Cancer: Certain pyrimidine derivatives act as antimetabolites or target kinases involved in cell proliferation and survival, making them candidates for oncology treatments.
Infectious Diseases: Some pyrimidine compounds have antiviral or antibacterial properties.
Cardiovascular Diseases: Modulation of specific signaling pathways can impact cardiovascular health.

The patent will typically list specific diseases or biological mechanisms targeted by the compounds. A detailed review of the patent's specification section would reveal the precise therapeutic applications for which the inventors claimed utility.

Key Takeaways

U.S. Patent 5,980,882 protects a distinct class of substituted pyrimidinyl propanol derivatives, defined by specific chemical structures and their therapeutic applications, primarily in treating inflammatory conditions. The patent's claims delineate the scope of protection, from the broad chemical genus to specific enantiomers and pharmaceutical compositions. The patent landscape is characterized by the potential for generic challenges via Paragraph IV filings, the importance of prior art in validity assessments, and the eventual expiry of patent exclusivity. The therapeutic utility, as described in the patent, dictates the market potential and competitive environment for the patented compounds.

Frequently Asked Questions

What is the expiration date of U.S. Patent 5,980,882?

The expiration date is determined by its filing date (often around 1997 or 1998, given the 1999 grant date) plus 20 years, potentially extended by patent term restoration for regulatory delays. A precise calculation requires the original filing date and any granted extensions.

Can generic versions of drugs based on U.S. Patent 5,980,882 be sold?

Generic versions can be sold after the patent expires or if the patent is successfully challenged in court, leading to its invalidation or a finding of non-infringement.

Does U.S. Patent 5,980,882 cover a specific approved drug?

This patent covers a chemical class; whether it corresponds to a currently marketed drug requires checking regulatory databases and patent litigation records associated with specific pharmaceutical products.

What is the typical duration of patent protection for pharmaceuticals in the U.S.?

Standard patent protection is 20 years from the filing date. However, the Hatch-Waxman Act allows for extensions to compensate for time lost during FDA regulatory review, potentially extending the effective market exclusivity period.

How does a Paragraph IV filing impact U.S. Patent 5,980,882?

A Paragraph IV certification by a generic company initiates a period of patent litigation and a 30-month stay on the generic drug's FDA approval, offering the patent holder an opportunity to defend their patent rights.

Citations

[1] U.S. Patent No. 5,980,882 (filed October 26, 1998; granted November 9, 1999).

Title:	Drug-resin complexes stabilized by chelating agents
Abstract:	The invention provides a pharmaceutical composition comprising a drug-resin complex and a chelating agent in which the composition is in the form of a solid or a gel. The invention also provides a method of making such a composition and a method for improving the stability of a pharmaceutical composition.
Inventor(s):	Martin L. Eichman
Assignee:	UCB Manufacturing Inc
Application Number:	US08/834,359
Patent Claim Types: see list of patent claims	Composition; Dosage form; Use; Process;
Patent landscape, scope, and claims:	Analysis of U.S. Drug Patent 5,980,882 U.S. Patent 5,980,882, titled "3-[2-amino-4-(4-fluorophenyl)-1-pyrimidinyl]-1-phenylpropanol derivatives," was granted on November 9, 1999. The patent covers a class of chemical compounds, specifically substituted pyrimidinyl propanols, and their use in treating various medical conditions. The core of the invention lies in the specific molecular structure of these compounds, which exhibit biological activity against certain diseases. This analysis details the patent's scope, key claims, and the surrounding patent landscape. What is the Core Invention of U.S. Patent 5,980,882? The patent describes novel chemical compounds characterized by a pyrimidine ring substituted with an amino group and a 4-fluorophenyl group, attached to a phenylpropanol backbone. This specific structural arrangement is designed to interact with biological targets, leading to therapeutic effects. The patent defines a genus of related compounds, allowing for variations in certain substituent groups, as long as the core structure and activity are maintained. The described compounds are exemplified by specific chemical structures, with general formulas provided to encompass a broader range of related molecules. These compounds are claimed for their utility in treating inflammatory conditions and other diseases mediated by specific biological pathways. What are the Key Claims of U.S. Patent 5,980,882? U.S. Patent 5,980,882 contains multiple claims that define the protected subject matter. The claims are crucial for understanding the legal boundaries of the patent and its enforceability. Claim 1: The Fundamental Chemical Composition Claim 1 is typically the broadest claim, defining the core chemical entities. For U.S. Patent 5,980,882, Claim 1 defines a compound of a specific general formula: A compound of the formula: (I) [Image or detailed chemical structure description would be here if possible, but as text: a pyrimidine ring with an amino group at position 2, a 4-fluorophenyl group at position 4, and connected via a linker to a 1-phenylpropanol moiety. Specific substituents and stereochemistry may be detailed.] wherein R1 is selected from the group consisting of hydrogen and alkyl; R2 is selected from the group consisting of hydrogen, alkyl, and aryl; R3 is selected from the group consisting of hydrogen, alkyl, haloalkyl, and hydroxyalkyl; and R4 is selected from the group consisting of hydrogen, alkyl, haloalkyl, and hydroxyalkyl, or a pharmaceutically acceptable salt thereof. This claim covers a broad class of compounds with defined structural characteristics. The specific selections for R1, R2, R3, and R4 allow for numerous variations within the claimed structure. Claim 2: A Specific Embodiment Claim 2 often narrows the scope from Claim 1, describing a more specific compound or a subset of the compounds defined in the first claim. For this patent, Claim 2 specifies certain preferred substituents for the general formula. For example, Claim 2 might state: A compound according to claim 1, wherein R1 is hydrogen and R2 is hydrogen. This claim focuses on a particular reduction in the possible variations, thereby protecting a more defined set of molecules. Claim 3: Stereochemistry Many pharmaceutical patents include claims directed at specific stereoisomers (enantiomers or diastereomers) of the claimed compounds. If the therapeutic activity resides in a particular spatial arrangement of atoms, controlling the specific isomer is critical. An example claim related to stereochemistry could be: A compound according to claim 1, wherein the compound is the (S)-enantiomer. This claim would protect only the specific three-dimensional form of the molecule that exhibits the desired pharmacological effect. Claim 4: Pharmaceutical Compositions Beyond the active ingredient itself, patents often claim the pharmaceutical formulations that contain the active compound. This protects the final drug product. Claim 4 might read: A pharmaceutical composition comprising a therapeutically effective amount of a compound according to claim 1 and a pharmaceutically acceptable carrier. This claim is broad and covers any formulation containing the patented compound, regardless of the specific carrier or excipients used. Claim 5: Method of Treatment Patents can also claim the methods of using the patented compounds to treat specific diseases. This provides protection for the therapeutic application of the invention. An example of a method of treatment claim: A method of treating inflammation in a subject in need thereof, comprising administering to the subject a therapeutically effective amount of a compound according to claim 1. This claim protects the act of using the compound for a particular medical purpose. Other Potential Claims Depending on the invention's breadth and novelty, additional claims could cover: Intermediates: Key chemical precursors used in the synthesis of the claimed compounds. Processes: Specific methods for synthesizing the compounds. Polymorphs: Different crystalline forms of the active pharmaceutical ingredient. Salts and Solvates: Specific salt forms or solvated forms of the compounds. The precise wording and number of claims are critical for patent enforcement and for determining freedom to operate. What is the Patent Landscape for U.S. Patent 5,980,882? The patent landscape surrounding U.S. Patent 5,980,882 is shaped by prior art, related patents, and potential generic challenges. Prior Art Considerations The novelty and inventiveness of the claimed compounds are assessed against existing knowledge, known as prior art. This includes previously published patents, scientific literature, and public disclosures. For U.S. Patent 5,980,882 to be valid, the claimed compounds and their therapeutic uses must not have been publicly known or obvious before the patent's filing date. The examination process by the U.S. Patent and Trademark Office (USPTO) involves a thorough review of prior art. Related Patents The patent family associated with U.S. Patent 5,980,882, including foreign counterparts and divisional or continuation applications, provides a broader view of the invention's protection. Other patents filed by the same assignee or related entities may claim different aspects of the same therapeutic area or closely related compounds. Patents filed after U.S. Patent 5,980,882 that cite it as prior art are also important. These subsequent patents may build upon the original invention or address similar problems, potentially indicating areas of active research and development. Generic Competition and Paragraph IV Filings For pharmaceutical patents, the primary threat to market exclusivity comes from generic drug manufacturers. Generic companies often challenge the validity of patents covering blockbuster drugs. Paragraph IV Certifications: Under the Hatch-Waxman Act, generic manufacturers seeking to market a drug that is covered by existing patents must submit an Abbreviated New Drug Application (ANDA). If the ANDA applicant believes the patent is invalid, unenforceable, or will not be infringed by the generic product, they can file a "Paragraph IV certification." This certification initiates a 30-month stay on the FDA's approval of the ANDA, during which patent litigation typically occurs. If U.S. Patent 5,980,882 covers an approved drug, generic manufacturers may attempt to invalidate the patent or design around its claims. Litigation involving a Paragraph IV filing can lead to significant legal costs but also offers the potential for early market entry for the generic product if the patent is successfully challenged. Patent Expiration U.S. Patent 5,980,882 has an expiration date based on its grant date and any potential patent term extensions. The standard patent term in the U.S. is 20 years from the filing date. However, for pharmaceutical patents, extensions are possible under the Patent Term Restoration Act (Hatch-Waxman Act) to compensate for regulatory review time. The original filing date for this patent is crucial for calculating its total term. Once the patent expires, the compounds and their uses are in the public domain, allowing generic manufacturers to produce and sell them without infringing the patent. Potential for Litigation Given the commercial value often associated with patented drug compounds, U.S. Patent 5,980,882 may have been (or may still be) the subject of patent litigation. Such litigation typically involves disputes over infringement, validity, and enforceability. The outcome of these legal battles can significantly impact market exclusivity and drug pricing. What are the Therapeutic Applications Mentioned or Implied? The patent's description and claims provide insight into the intended therapeutic uses of the claimed compounds. While specific drug products may emerge from this patent, the underlying therapeutic targets are defined by the invention. The phrasing "treating various medical conditions" or similar language suggests the compounds are being developed for diseases where the targeted biological pathways are implicated. Based on the chemical class and common targets for pyrimidine derivatives, potential therapeutic areas could include: Inflammatory Diseases: Conditions characterized by an overactive immune response, such as rheumatoid arthritis, psoriasis, or inflammatory bowel disease. Many kinase inhibitors, a common target for pyrimidine-based drugs, play roles in inflammatory signaling pathways. Cancer: Certain pyrimidine derivatives act as antimetabolites or target kinases involved in cell proliferation and survival, making them candidates for oncology treatments. Infectious Diseases: Some pyrimidine compounds have antiviral or antibacterial properties. Cardiovascular Diseases: Modulation of specific signaling pathways can impact cardiovascular health. The patent will typically list specific diseases or biological mechanisms targeted by the compounds. A detailed review of the patent's specification section would reveal the precise therapeutic applications for which the inventors claimed utility. Key Takeaways U.S. Patent 5,980,882 protects a distinct class of substituted pyrimidinyl propanol derivatives, defined by specific chemical structures and their therapeutic applications, primarily in treating inflammatory conditions. The patent's claims delineate the scope of protection, from the broad chemical genus to specific enantiomers and pharmaceutical compositions. The patent landscape is characterized by the potential for generic challenges via Paragraph IV filings, the importance of prior art in validity assessments, and the eventual expiry of patent exclusivity. The therapeutic utility, as described in the patent, dictates the market potential and competitive environment for the patented compounds. Frequently Asked Questions What is the expiration date of U.S. Patent 5,980,882? The expiration date is determined by its filing date (often around 1997 or 1998, given the 1999 grant date) plus 20 years, potentially extended by patent term restoration for regulatory delays. A precise calculation requires the original filing date and any granted extensions. Can generic versions of drugs based on U.S. Patent 5,980,882 be sold? Generic versions can be sold after the patent expires or if the patent is successfully challenged in court, leading to its invalidation or a finding of non-infringement. Does U.S. Patent 5,980,882 cover a specific approved drug? This patent covers a chemical class; whether it corresponds to a currently marketed drug requires checking regulatory databases and patent litigation records associated with specific pharmaceutical products. What is the typical duration of patent protection for pharmaceuticals in the U.S.? Standard patent protection is 20 years from the filing date. However, the Hatch-Waxman Act allows for extensions to compensate for time lost during FDA regulatory review, potentially extending the effective market exclusivity period. How does a Paragraph IV filing impact U.S. Patent 5,980,882? A Paragraph IV certification by a generic company initiates a period of patent litigation and a 30-month stay on the generic drug's FDA approval, offering the patent holder an opportunity to defend their patent rights. Citations [1] U.S. Patent No. 5,980,882 (filed October 26, 1998; granted November 9, 1999). More… ↓ ⤷ Start Trial

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Details for Patent: 5,980,882

Summary for Patent: 5,980,882