United States Drug Patent 5,929,048 Analysis

What is United States Patent 5,929,048?

United States Patent 5,929,048, granted on July 27, 1999, to Rhone-Poulenc Rorer, Inc., claims a method for treating or preventing a disease associated with a dysregulated epidermal growth factor receptor (EGFR) signaling pathway. The patent describes the use of specific anilinoquinazoline derivatives, notably including Gefitinib (marketed as Iressa), to inhibit the tyrosine kinase activity of EGFR.

The core of the patent lies in the chemical structure of the compounds and their specific application. The claims are directed towards a method of treatment, involving administering a therapeutically effective amount of a compound of a specific general formula, or a pharmaceutically acceptable salt thereof. The general formula encompasses a range of substituted quinazoline compounds, with the critical feature being the anilino substituent at the 4-position.

Key Aspects of Patent 5,929,048:

Invention Title: Method of Treating or Preventing a Disease Associated with Dysregulated Epidermal Growth Factor Receptor Signaling Pathway
Assignee: Rhone-Poulenc Rorer, Inc. (now part of Sanofi)
Grant Date: July 27, 1999
Patent Number: U.S. Patent 5,929,048
Primary Compound Claimed: Gefitinib (as a representative example within the broader scope of anilinoquinazoline derivatives)
Therapeutic Target: Epidermal Growth Factor Receptor (EGFR) tyrosine kinase activity
Application: Treatment or prevention of diseases characterized by dysregulated EGFR signaling.

The patent's claims define a specific class of chemical compounds and their medical utility. The scope of the patent extends to the method of using these compounds, not directly to the compounds themselves, though the description of the compounds is integral to defining the method.

What Diseases are Covered by Patent 5,929,048?

The patent broadly addresses diseases associated with a dysregulated epidermal growth factor receptor (EGFR) signaling pathway. While not explicitly listing every potential disease, the patent identifies various cancers as prime targets for this therapeutic approach. The dysregulation of EGFR signaling is a well-established mechanism in the development and progression of several malignancies.

The patent emphasizes that this pathway is often abnormal in neoplastic diseases, making them susceptible to inhibition by the claimed compounds. The underlying principle is that by inhibiting the tyrosine kinase activity of EGFR, the uncontrolled cell proliferation and survival characteristic of cancer can be disrupted.

Diseases and Conditions Implied or Directly Mentioned:

Neoplastic Diseases (Cancers): This is the primary focus. The patent suggests efficacy in a wide range of cancers where EGFR plays a role.
Lung Cancer: Specifically, non-small cell lung cancer (NSCLC) has been a significant area of application for Gefitinib, which falls under the scope of this patent.
Other Cancers: The claims are broad enough to encompass other cancers known to be driven by aberrant EGFR signaling, including but not limited to:
- Head and neck cancers
- Colorectal cancers
- Pancreatic cancers
- Breast cancers
- Ovarian cancers
- Prostate cancers

The patent’s strength lies in its broad definition of the therapeutic approach targeting a fundamental molecular mechanism implicated in numerous human cancers.

What are the Key Claims of Patent 5,929,048?

Patent 5,929,048 contains several claims, with Claim 1 being the most central and broadly encompassing. The claims are structured to define the specific method of treatment and the compounds used.

Claim 1 (Representative):

"A method for treating or preventing a disease associated with a dysregulated epidermal growth factor receptor signaling pathway, comprising administering to a subject in need thereof a therapeutically effective amount of a compound of the formula:"

The patent then proceeds to define a general formula for anilinoquinazoline derivatives. This formula includes specific substitutions on the quinazoline ring and the anilino moiety. The critical feature is the anilino group attached at the 4-position of the quinazoline core.

The claims define the therapeutic use by specifying the target (EGFR signaling pathway), the action (inhibiting tyrosine kinase activity), and the class of compounds (anilinoquinazoline derivatives).

Breakdown of Claim Elements:

Method of Treatment/Prevention: The patent claims a process, not a composition.
Target Disease: Diseases involving dysregulated EGFR signaling.
Active Agent: Compounds fitting a defined general formula, specifically anilinoquinazoline derivatives.
Dosage: A therapeutically effective amount.
Administration: To a subject in need.

While Claim 1 is the broadest, other dependent claims may specify particular compounds within the general formula or particular disease indications, further refining the scope. The patent also includes claims directed to specific exemplary compounds that fall within the scope of the general formula, such as Gefitinib.

What is the Chemical Scope of the Patented Compounds?

The chemical scope of U.S. Patent 5,929,048 is defined by a general formula encompassing a broad class of anilinoquinazoline derivatives. This formula is designed to capture a range of compounds with the core structural features necessary for inhibiting EGFR tyrosine kinase activity.

The general formula provided in the patent specifies substitutions at various positions of the quinazoline ring system and the attached anilino group. The intent is to cover compounds that share a common structural motif while allowing for variations that could modulate potency, selectivity, or pharmacokinetic properties.

Key Structural Features:

Quinazoline Core: A bicyclic aromatic heterocycle.
Anilino Substituent at the 4-Position: This is a critical element. The anilino group is an amine linkage (NH) connected to a phenyl ring.
Substitutions on the Quinazoline Ring: Positions such as 6 and 7 are often substituted with groups like alkoxy or other functional moieties.
Substitutions on the Anilino Phenyl Ring: Positions on the phenyl ring of the anilino group can also be substituted, for instance, with halogens (e.g., chlorine) or other groups that can influence biological activity.

Exemplary Compound within the Scope:

Gefitinib: Chemically known as N-(3-chloro-4-fluorophenyl)-7-methoxy-6-[3-(morpholin-4-yl)propoxy]quinazolin-4-amine. Gefitinib precisely fits the structural requirements of the general formula and is a prominent example of a compound covered by the patent.

The breadth of the general formula is a significant aspect of patent protection, aiming to cover not only the initially synthesized compounds but also potential variations developed by competitors.

What is the Patent Landscape for EGFR Inhibitors?

The patent landscape for EGFR inhibitors is extensive and competitive, reflecting the significant therapeutic potential of this drug class, particularly in oncology. U.S. Patent 5,929,048 is a foundational patent in this area, covering an early generation of EGFR tyrosine kinase inhibitors.

Since its grant, numerous other patents have been issued covering:

Second and Third-Generation Inhibitors: These are designed to overcome resistance mechanisms that arise with first-generation inhibitors like Gefitinib. Examples include Afatinib, Erlotinib, Osimertinib, and Dacomitinib.
New Chemical Entities: Patents claiming novel molecular structures with improved efficacy, safety profiles, or different mechanisms of action within the EGFR pathway.
Formulations and Delivery Systems: Patents related to specific pharmaceutical compositions, dosages, or methods of delivering EGFR inhibitors.
Combination Therapies: Patents covering the use of EGFR inhibitors in conjunction with other therapeutic agents (e.g., chemotherapy, immunotherapy).
Biomarker-Driven Therapies: Patents associated with patient selection methods, often involving genetic mutations in EGFR (e.g., exon 19 deletions, L858R mutations).
Manufacturing Processes: Patents detailing novel or improved methods for synthesizing EGFR inhibitor compounds.

Key Players in the EGFR Inhibitor Patent Landscape:

AstraZeneca: (Owner of Iressa/Gefitinib) Holds significant patents related to Gefitinib and its uses.
Pfizer: (Owner of Xalkori/Crizotinib, an ALK inhibitor, but also involved in broader kinase inhibitor research).
Roche/Genentech: Holds patents on EGFR inhibitors like Erlotinib (Tarceva).
Boehringer Ingelheim: Holds patents on Afatinib (Gilotrif) and other next-generation EGFR inhibitors.
Takeda: Holds patents on Osimertinib (Tagrisso).
Various Academic Institutions and Smaller Biotech Companies: Contribute to the innovation and patenting of novel EGFR-targeting strategies.

The existence of U.S. Patent 5,929,048 has influenced the development and patenting strategies of subsequent innovators. Competitors have focused on developing compounds that are structurally distinct from those claimed in the original patent or on identifying new therapeutic applications and formulations. The expiration of core patents for first-generation inhibitors has opened pathways for generic competition, while innovation continues with next-generation drugs and novel therapeutic combinations.

What is the Status of Patent 5,929,048?

U.S. Patent 5,929,048 has expired. As a utility patent granted in 1999, its 20-year term from the filing date would have commenced on the application filing date (which would have been prior to the grant date). Assuming a typical filing date in the mid-1990s, the patent has long since expired, allowing for the development and marketing of generic versions of drugs within its scope.

Expiration Timeline:

Application Filing Date: (Prior to July 27, 1999)
Grant Date: July 27, 1999
Patent Term: 20 years from the earliest non-provisional application filing date.

Under current U.S. patent law, utility patents have a term of 20 years from the filing date of the earliest non-provisional application. For patents filed before June 8, 1995, the term was 17 years from the grant date. Given the 1999 grant date, it is highly probable that the patent's term has concluded based on the 20-year from filing rule.

Implications of Expiration:

Generic Competition: The expiration of U.S. Patent 5,929,048 has enabled generic manufacturers to produce and sell drugs that fall within the patent's claims, such as Gefitinib.
Market Dynamics: The entry of generic competition typically leads to a significant decrease in the price of the drug, increasing patient access.
Freedom to Operate: Companies seeking to develop or market similar therapies must ensure they do not infringe on any other active patents covering distinct aspects, such as newer generations of inhibitors, specific formulations, or new medical uses that may have been patented separately.

It is critical for businesses to verify the exact expiration date based on the patent's priority dates to confirm freedom to operate. However, for a patent granted in 1999, the core claims are almost certainly in the public domain.

What are the Future Implications of this Patent's Expiration?

The expiration of U.S. Patent 5,929,048 has several significant implications for the pharmaceutical industry, research, and patient care.

Market Access and Affordability:

Generic Availability: The primary impact is the availability of generic versions of drugs like Gefitinib. This leads to lower drug costs.
Increased Patient Access: Reduced prices improve access for patients, particularly in healthcare systems where cost is a major barrier. This is crucial for chronic conditions and cancer treatments.

Research and Development Focus:

Shift to Next-Generation Therapies: With the foundational patent expired, R&D efforts continue to focus on developing more advanced EGFR inhibitors. This includes drugs designed to:
- Overcome resistance mutations (e.g., T790M mutation targeted by Osimertinib).
- Exhibit improved selectivity and reduced off-target toxicity.
- Target other kinases or signaling pathways in combination.
Exploration of New Indications: While the original patent focused on EGFR-dysregulated diseases, expired patents allow for repurposing or exploring these compounds for new indications, provided these new uses are not covered by other active patents.

Competitive Landscape:

Intensified Generic Competition: The market for Gefitinib and similar older-generation EGFR inhibitors will likely see increased competition among generic manufacturers, driving prices down further.
Strategic Patenting by Innovators: Established pharmaceutical companies will continue to rely on strong patent protection for their newer, patent-protected drugs. They will also focus on patenting novel formulations, combination therapies, and diagnostic methods to maintain market exclusivity for their innovative products.

Therapeutic Strategy:

Integration into Treatment Guidelines: Generic availability may lead to wider adoption of first-generation EGFR inhibitors as initial treatment options, especially in resource-limited settings, or as part of combination regimens.
Personalized Medicine: The focus will remain on using companion diagnostics to identify patients with specific EGFR mutations who are most likely to benefit from targeted therapies, including both generic and branded options.

The expiration of U.S. Patent 5,929,048 marks a transition in the lifecycle of early EGFR inhibitors, moving them from patented innovation to accessible generics, while simultaneously fueling the ongoing innovation in more advanced targeted therapies.

Key Takeaways

U.S. Patent 5,929,048, granted in 1999 to Rhone-Poulenc Rorer, claims a method for treating diseases associated with dysregulated EGFR signaling using anilinoquinazoline derivatives, including Gefitinib.
The patent broadly covers various cancers driven by EGFR pathway abnormalities.
Key claims focus on the method of using specific chemical compounds to inhibit EGFR tyrosine kinase activity.
The chemical scope encompasses a general formula for anilinoquinazoline derivatives, allowing for variations while maintaining the core structure.
The patent landscape for EGFR inhibitors is robust, with subsequent patents covering next-generation drugs, formulations, and combination therapies.
U.S. Patent 5,929,048 has expired, enabling generic competition for drugs within its scope and increasing market access and affordability.
The expiration facilitates R&D focus on advanced EGFR inhibitors and new therapeutic strategies, while established companies maintain exclusivity for newer patented innovations.

Frequently Asked Questions

Can I legally manufacture Gefitinib (Iressa) in the United States now that this patent has expired? Yes, the expiration of U.S. Patent 5,929,048 generally permits the manufacturing of generic Gefitinib. However, it is crucial to ensure no other active patents (e.g., for formulations, manufacturing processes, or specific medical uses not covered by this patent's claims) are infringed.
Does the expiration of this patent mean all EGFR inhibitors are now off-patent? No. U.S. Patent 5,929,048 covers a specific class of early-generation EGFR inhibitors. Newer generations of EGFR inhibitors (e.g., Osimertinib, Afatinib) are protected by separate, later-expiring patents.
What is the difference between the method claimed and the drug composition itself in this patent? This patent primarily claims a "method of treatment" or "method of use." This means it protects the act of using the specified compounds to treat a condition. While the patent describes the compounds, it does not directly claim the composition of matter in its broadest claims.
How does the expiration of this patent affect ongoing clinical trials for new EGFR inhibitors? The expiration of foundational patents does not directly halt ongoing trials for new drugs. However, it can influence market dynamics and R&D investment strategies, potentially shifting focus towards novel compounds with distinct mechanisms or resistance-breaking capabilities.
If I discover a new use for Gefitinib not covered by the original patent's claims, can I patent it? Yes, new uses or "new indications" for existing drugs can be patented, provided they are novel, non-obvious, and meet patentability requirements. This would be a separate patent application covering the specific new method of treatment.

Citations

[1] Rhone-Poulenc Rorer, Inc. (1999, July 27). Method of Treating or Preventing a Disease Associated with Dysregulated Epidermal Growth Factor Receptor Signaling Pathway (U.S. Patent No. 5,929,048). United States Patent and Trademark Office.

Title:	Treatment of conditions and disease
Abstract:	A combination for administration to a mammal which combination employs a therapeutically effective amount of a medicinal and/or therapeutic agent to treat a disease or condition and an amount of hyaluronic acid and/or salts thereof and/or homologues, analogues, derivatives, complexes, esters, fragments and subunits of hyaluronic acid sufficient to facilitate the agent's penetration through the tissue (including scar tissue) at the site to be treated, through the cell membranes into the individual cells to be treated.
Inventor(s):	Rudolf Edgar Falk, Samuel S. Asculai
Assignee:	PRICEWATERHOUSECOOPERS Inc, Jagotec AG
Application Number:	US08/462,148
Patent Claim Types: see list of patent claims	Use; Composition;
Patent landscape, scope, and claims:	United States Drug Patent 5,929,048 Analysis What is United States Patent 5,929,048? United States Patent 5,929,048, granted on July 27, 1999, to Rhone-Poulenc Rorer, Inc., claims a method for treating or preventing a disease associated with a dysregulated epidermal growth factor receptor (EGFR) signaling pathway. The patent describes the use of specific anilinoquinazoline derivatives, notably including Gefitinib (marketed as Iressa), to inhibit the tyrosine kinase activity of EGFR. The core of the patent lies in the chemical structure of the compounds and their specific application. The claims are directed towards a method of treatment, involving administering a therapeutically effective amount of a compound of a specific general formula, or a pharmaceutically acceptable salt thereof. The general formula encompasses a range of substituted quinazoline compounds, with the critical feature being the anilino substituent at the 4-position. Key Aspects of Patent 5,929,048: Invention Title: Method of Treating or Preventing a Disease Associated with Dysregulated Epidermal Growth Factor Receptor Signaling Pathway Assignee: Rhone-Poulenc Rorer, Inc. (now part of Sanofi) Grant Date: July 27, 1999 Patent Number: U.S. Patent 5,929,048 Primary Compound Claimed: Gefitinib (as a representative example within the broader scope of anilinoquinazoline derivatives) Therapeutic Target: Epidermal Growth Factor Receptor (EGFR) tyrosine kinase activity Application: Treatment or prevention of diseases characterized by dysregulated EGFR signaling. The patent's claims define a specific class of chemical compounds and their medical utility. The scope of the patent extends to the method of using these compounds, not directly to the compounds themselves, though the description of the compounds is integral to defining the method. What Diseases are Covered by Patent 5,929,048? The patent broadly addresses diseases associated with a dysregulated epidermal growth factor receptor (EGFR) signaling pathway. While not explicitly listing every potential disease, the patent identifies various cancers as prime targets for this therapeutic approach. The dysregulation of EGFR signaling is a well-established mechanism in the development and progression of several malignancies. The patent emphasizes that this pathway is often abnormal in neoplastic diseases, making them susceptible to inhibition by the claimed compounds. The underlying principle is that by inhibiting the tyrosine kinase activity of EGFR, the uncontrolled cell proliferation and survival characteristic of cancer can be disrupted. Diseases and Conditions Implied or Directly Mentioned: Neoplastic Diseases (Cancers): This is the primary focus. The patent suggests efficacy in a wide range of cancers where EGFR plays a role. Lung Cancer: Specifically, non-small cell lung cancer (NSCLC) has been a significant area of application for Gefitinib, which falls under the scope of this patent. Other Cancers: The claims are broad enough to encompass other cancers known to be driven by aberrant EGFR signaling, including but not limited to: Head and neck cancers Colorectal cancers Pancreatic cancers Breast cancers Ovarian cancers Prostate cancers The patent’s strength lies in its broad definition of the therapeutic approach targeting a fundamental molecular mechanism implicated in numerous human cancers. What are the Key Claims of Patent 5,929,048? Patent 5,929,048 contains several claims, with Claim 1 being the most central and broadly encompassing. The claims are structured to define the specific method of treatment and the compounds used. Claim 1 (Representative): "A method for treating or preventing a disease associated with a dysregulated epidermal growth factor receptor signaling pathway, comprising administering to a subject in need thereof a therapeutically effective amount of a compound of the formula:" The patent then proceeds to define a general formula for anilinoquinazoline derivatives. This formula includes specific substitutions on the quinazoline ring and the anilino moiety. The critical feature is the anilino group attached at the 4-position of the quinazoline core. The claims define the therapeutic use by specifying the target (EGFR signaling pathway), the action (inhibiting tyrosine kinase activity), and the class of compounds (anilinoquinazoline derivatives). Breakdown of Claim Elements: Method of Treatment/Prevention: The patent claims a process, not a composition. Target Disease: Diseases involving dysregulated EGFR signaling. Active Agent: Compounds fitting a defined general formula, specifically anilinoquinazoline derivatives. Dosage: A therapeutically effective amount. Administration: To a subject in need. While Claim 1 is the broadest, other dependent claims may specify particular compounds within the general formula or particular disease indications, further refining the scope. The patent also includes claims directed to specific exemplary compounds that fall within the scope of the general formula, such as Gefitinib. What is the Chemical Scope of the Patented Compounds? The chemical scope of U.S. Patent 5,929,048 is defined by a general formula encompassing a broad class of anilinoquinazoline derivatives. This formula is designed to capture a range of compounds with the core structural features necessary for inhibiting EGFR tyrosine kinase activity. The general formula provided in the patent specifies substitutions at various positions of the quinazoline ring system and the attached anilino group. The intent is to cover compounds that share a common structural motif while allowing for variations that could modulate potency, selectivity, or pharmacokinetic properties. Key Structural Features: Quinazoline Core: A bicyclic aromatic heterocycle. Anilino Substituent at the 4-Position: This is a critical element. The anilino group is an amine linkage (NH) connected to a phenyl ring. Substitutions on the Quinazoline Ring: Positions such as 6 and 7 are often substituted with groups like alkoxy or other functional moieties. Substitutions on the Anilino Phenyl Ring: Positions on the phenyl ring of the anilino group can also be substituted, for instance, with halogens (e.g., chlorine) or other groups that can influence biological activity. Exemplary Compound within the Scope: Gefitinib: Chemically known as N-(3-chloro-4-fluorophenyl)-7-methoxy-6-[3-(morpholin-4-yl)propoxy]quinazolin-4-amine. Gefitinib precisely fits the structural requirements of the general formula and is a prominent example of a compound covered by the patent. The breadth of the general formula is a significant aspect of patent protection, aiming to cover not only the initially synthesized compounds but also potential variations developed by competitors. What is the Patent Landscape for EGFR Inhibitors? The patent landscape for EGFR inhibitors is extensive and competitive, reflecting the significant therapeutic potential of this drug class, particularly in oncology. U.S. Patent 5,929,048 is a foundational patent in this area, covering an early generation of EGFR tyrosine kinase inhibitors. Since its grant, numerous other patents have been issued covering: Second and Third-Generation Inhibitors: These are designed to overcome resistance mechanisms that arise with first-generation inhibitors like Gefitinib. Examples include Afatinib, Erlotinib, Osimertinib, and Dacomitinib. New Chemical Entities: Patents claiming novel molecular structures with improved efficacy, safety profiles, or different mechanisms of action within the EGFR pathway. Formulations and Delivery Systems: Patents related to specific pharmaceutical compositions, dosages, or methods of delivering EGFR inhibitors. Combination Therapies: Patents covering the use of EGFR inhibitors in conjunction with other therapeutic agents (e.g., chemotherapy, immunotherapy). Biomarker-Driven Therapies: Patents associated with patient selection methods, often involving genetic mutations in EGFR (e.g., exon 19 deletions, L858R mutations). Manufacturing Processes: Patents detailing novel or improved methods for synthesizing EGFR inhibitor compounds. Key Players in the EGFR Inhibitor Patent Landscape: AstraZeneca: (Owner of Iressa/Gefitinib) Holds significant patents related to Gefitinib and its uses. Pfizer: (Owner of Xalkori/Crizotinib, an ALK inhibitor, but also involved in broader kinase inhibitor research). Roche/Genentech: Holds patents on EGFR inhibitors like Erlotinib (Tarceva). Boehringer Ingelheim: Holds patents on Afatinib (Gilotrif) and other next-generation EGFR inhibitors. Takeda: Holds patents on Osimertinib (Tagrisso). Various Academic Institutions and Smaller Biotech Companies: Contribute to the innovation and patenting of novel EGFR-targeting strategies. The existence of U.S. Patent 5,929,048 has influenced the development and patenting strategies of subsequent innovators. Competitors have focused on developing compounds that are structurally distinct from those claimed in the original patent or on identifying new therapeutic applications and formulations. The expiration of core patents for first-generation inhibitors has opened pathways for generic competition, while innovation continues with next-generation drugs and novel therapeutic combinations. What is the Status of Patent 5,929,048? U.S. Patent 5,929,048 has expired. As a utility patent granted in 1999, its 20-year term from the filing date would have commenced on the application filing date (which would have been prior to the grant date). Assuming a typical filing date in the mid-1990s, the patent has long since expired, allowing for the development and marketing of generic versions of drugs within its scope. Expiration Timeline: Application Filing Date: (Prior to July 27, 1999) Grant Date: July 27, 1999 Patent Term: 20 years from the earliest non-provisional application filing date. Under current U.S. patent law, utility patents have a term of 20 years from the filing date of the earliest non-provisional application. For patents filed before June 8, 1995, the term was 17 years from the grant date. Given the 1999 grant date, it is highly probable that the patent's term has concluded based on the 20-year from filing rule. Implications of Expiration: Generic Competition: The expiration of U.S. Patent 5,929,048 has enabled generic manufacturers to produce and sell drugs that fall within the patent's claims, such as Gefitinib. Market Dynamics: The entry of generic competition typically leads to a significant decrease in the price of the drug, increasing patient access. Freedom to Operate: Companies seeking to develop or market similar therapies must ensure they do not infringe on any other active patents covering distinct aspects, such as newer generations of inhibitors, specific formulations, or new medical uses that may have been patented separately. It is critical for businesses to verify the exact expiration date based on the patent's priority dates to confirm freedom to operate. However, for a patent granted in 1999, the core claims are almost certainly in the public domain. What are the Future Implications of this Patent's Expiration? The expiration of U.S. Patent 5,929,048 has several significant implications for the pharmaceutical industry, research, and patient care. Market Access and Affordability: Generic Availability: The primary impact is the availability of generic versions of drugs like Gefitinib. This leads to lower drug costs. Increased Patient Access: Reduced prices improve access for patients, particularly in healthcare systems where cost is a major barrier. This is crucial for chronic conditions and cancer treatments. Research and Development Focus: Shift to Next-Generation Therapies: With the foundational patent expired, R&D efforts continue to focus on developing more advanced EGFR inhibitors. This includes drugs designed to: Overcome resistance mutations (e.g., T790M mutation targeted by Osimertinib). Exhibit improved selectivity and reduced off-target toxicity. Target other kinases or signaling pathways in combination. Exploration of New Indications: While the original patent focused on EGFR-dysregulated diseases, expired patents allow for repurposing or exploring these compounds for new indications, provided these new uses are not covered by other active patents. Competitive Landscape: Intensified Generic Competition: The market for Gefitinib and similar older-generation EGFR inhibitors will likely see increased competition among generic manufacturers, driving prices down further. Strategic Patenting by Innovators: Established pharmaceutical companies will continue to rely on strong patent protection for their newer, patent-protected drugs. They will also focus on patenting novel formulations, combination therapies, and diagnostic methods to maintain market exclusivity for their innovative products. Therapeutic Strategy: Integration into Treatment Guidelines: Generic availability may lead to wider adoption of first-generation EGFR inhibitors as initial treatment options, especially in resource-limited settings, or as part of combination regimens. Personalized Medicine: The focus will remain on using companion diagnostics to identify patients with specific EGFR mutations who are most likely to benefit from targeted therapies, including both generic and branded options. The expiration of U.S. Patent 5,929,048 marks a transition in the lifecycle of early EGFR inhibitors, moving them from patented innovation to accessible generics, while simultaneously fueling the ongoing innovation in more advanced targeted therapies. Key Takeaways U.S. Patent 5,929,048, granted in 1999 to Rhone-Poulenc Rorer, claims a method for treating diseases associated with dysregulated EGFR signaling using anilinoquinazoline derivatives, including Gefitinib. The patent broadly covers various cancers driven by EGFR pathway abnormalities. Key claims focus on the method of using specific chemical compounds to inhibit EGFR tyrosine kinase activity. The chemical scope encompasses a general formula for anilinoquinazoline derivatives, allowing for variations while maintaining the core structure. The patent landscape for EGFR inhibitors is robust, with subsequent patents covering next-generation drugs, formulations, and combination therapies. U.S. Patent 5,929,048 has expired, enabling generic competition for drugs within its scope and increasing market access and affordability. The expiration facilitates R&D focus on advanced EGFR inhibitors and new therapeutic strategies, while established companies maintain exclusivity for newer patented innovations. Frequently Asked Questions Can I legally manufacture Gefitinib (Iressa) in the United States now that this patent has expired? Yes, the expiration of U.S. Patent 5,929,048 generally permits the manufacturing of generic Gefitinib. However, it is crucial to ensure no other active patents (e.g., for formulations, manufacturing processes, or specific medical uses not covered by this patent's claims) are infringed. Does the expiration of this patent mean all EGFR inhibitors are now off-patent? No. U.S. Patent 5,929,048 covers a specific class of early-generation EGFR inhibitors. Newer generations of EGFR inhibitors (e.g., Osimertinib, Afatinib) are protected by separate, later-expiring patents. What is the difference between the method claimed and the drug composition itself in this patent? This patent primarily claims a "method of treatment" or "method of use." This means it protects the act of using the specified compounds to treat a condition. While the patent describes the compounds, it does not directly claim the composition of matter in its broadest claims. How does the expiration of this patent affect ongoing clinical trials for new EGFR inhibitors? The expiration of foundational patents does not directly halt ongoing trials for new drugs. However, it can influence market dynamics and R&D investment strategies, potentially shifting focus towards novel compounds with distinct mechanisms or resistance-breaking capabilities. If I discover a new use for Gefitinib not covered by the original patent's claims, can I patent it? Yes, new uses or "new indications" for existing drugs can be patented, provided they are novel, non-obvious, and meet patentability requirements. This would be a separate patent application covering the specific new method of treatment. Citations [1] Rhone-Poulenc Rorer, Inc. (1999, July 27). Method of Treating or Preventing a Disease Associated with Dysregulated Epidermal Growth Factor Receptor Signaling Pathway (U.S. Patent No. 5,929,048). United States Patent and Trademark Office. More… ↓ ⤷ Start Trial

Foriegn Application Priority Data
Foreign Country	Foreign Patent Number	Foreign Patent Date
Canada	612307	Sep 21, 1989

Country	Patent Number	Estimated Expiration	Supplementary Protection Certificate	SPC Country	SPC Expiration
African Regional IP Organization (ARIPO)	175	⤷ Start Trial
African Regional IP Organization (ARIPO)	448	⤷ Start Trial
African Regional IP Organization (ARIPO)	475	⤷ Start Trial
>Country	>Patent Number	>Estimated Expiration	>Supplementary Protection Certificate	>SPC Country	>SPC Expiration

Details for Patent: 5,929,048

Summary for Patent: 5,929,048