Analysis of U.S. Drug Patent 5,583,122: Scope, Claims, and Landscape

U.S. Patent 5,583,122, granted on December 10, 1996, to The Upjohn Company (now part of Pfizer Inc.), covers a method of treating various conditions by administering a specific chemical compound. The patent's claims define a method for treating or preventing medical conditions characterized by aberrant cell proliferation. The primary focus is on a pharmaceutical composition containing the active ingredient, [1R-(1R,3R,5S*)]-3-[[(1,1-Dimethylethyl)amino]carbonyl]-5-methyl-1-[[2'-methyl-1,1'-biphenyl]-4-yl]-4-oxo-2-thioxo-1,2,3,4-tetrahydro-5H-1,3-diazepin-5-yl]acetic acid. This compound is also known as Atazanavir sulfate, an antiretroviral medication used in the treatment of HIV infection [1, 2].

What is the Primary Invention Claimed in U.S. Patent 5,583,122?

The core of U.S. Patent 5,583,122 lies in its claims for a method of treating medical conditions involving abnormal cell proliferation. This is achieved through the administration of a pharmaceutical composition containing a specific chemical entity.

Claim 1: Method of Treatment

Claim 1, the broadest independent claim, defines the invention as "A method of treating or preventing a medical condition characterized by aberrant cell proliferation, which comprises administering to a subject in need of such treatment an effective amount of a pharmaceutical composition comprising a compound of the formula:"

The patent then provides a detailed chemical structure and definition for the compound. This compound is a diamino acid derivative and its salts. The specification extensively details the synthesis and characterization of this compound [1].

Dependent Claims: Refining the Scope

Several dependent claims further narrow the scope by specifying particular aspects of the composition or its use. These include:

Claim 2: Specifies a pharmaceutical composition containing the compound of Claim 1 and a pharmaceutically acceptable carrier.
Claim 3: Claims a method of treating or preventing a viral infection, specifically mentioning human immunodeficiency virus (HIV) [1]. This directly points to the intended therapeutic application of the patented compound.
Claim 4: Claims a pharmaceutical composition comprising the compound and a pharmaceutically acceptable carrier, for use in treating or preventing a viral infection [1].
Claim 5: Claims a pharmaceutical composition for use in treating or preventing HIV infection, comprising the compound and a pharmaceutically acceptable carrier [1].

These claims collectively establish the patent's focus on a method of using a specific chemical entity as a therapeutic agent, particularly for conditions involving aberrant cell proliferation and viral infections like HIV [1].

What is the Chemical Structure and Mechanism of Action of the Patented Compound?

The compound at the heart of U.S. Patent 5,583,122 is a diamino acid derivative that functions as an HIV protease inhibitor.

Chemical Identification

The chemical name provided in the patent is *[1R-(1R,3R,5S)]-3-[[(1,1-Dimethylethyl)amino]carbonyl]-5-methyl-1-[[2'-methyl-1,1'-biphenyl]-4-yl]-4-oxo-2-thioxo-1,3-diazepin-5-yl]acetic acid**. This complex nomenclature describes a molecule with specific stereochemistry. The compound is widely recognized as Atazanavir [1, 2].

Mechanism of Action

Atazanavir is a potent and selective inhibitor of the HIV-1 protease enzyme. HIV protease is essential for the replication of the virus. It cleaves viral polyproteins into functional proteins required for viral assembly and maturation. By inhibiting this enzyme, Atazanavir prevents the production of infectious viral particles, thus halting viral replication [3, 4].

The drug's structure is designed to mimic the natural substrate of the HIV protease. It binds to the active site of the enzyme, blocking its catalytic activity. This inhibition leads to the production of immature, non-infectious virions [4].

What is the Patent Landscape Surrounding U.S. Patent 5,583,122?

The patent landscape for U.S. Patent 5,583,122 is characterized by a series of patents covering various aspects of Atazanavir, including its synthesis, formulation, and therapeutic uses. These patents were predominantly filed and granted to The Upjohn Company and its successors.

Key Patents in the Atazanavir Family

While U.S. Patent 5,583,122 covers the core method of treatment, other patents protect different intellectual property aspects. Examples of related patent families often include:

Composition of Matter Patents: These patents, if granted, would claim the novel chemical compound itself. U.S. Patent 5,583,122 is a method of use patent, not a composition of matter patent for the compound. The original composition of matter patent for Atazanavir is crucial for foundational protection.
Process Patents: Patents covering specific, novel, and non-obvious methods of synthesizing Atazanavir. These can be critical for manufacturing efficiency and cost-effectiveness.
Formulation Patents: Patents protecting specific pharmaceutical formulations of Atazanavir, such as specific salt forms (e.g., Atazanavir sulfate), dosage forms (e.g., capsules, oral solutions), or combinations with other active pharmaceutical ingredients.
Polymorph Patents: Patents claiming specific crystalline forms (polymorphs) of Atazanavir, which can impact stability, bioavailability, and manufacturing [5].

Patent Expirations and Generic Entry

The expiration of key patents, including the primary composition of matter and method of use patents, is a critical event in the lifecycle of any drug. For Atazanavir, the expiration of foundational patents paved the way for generic competition.

U.S. Patent 5,583,122 Expiration: The patent term for U.S. Patent 5,583,122, granted in 1996, would have expired approximately 20 years from its filing date, subject to any patent term extensions. The application for this patent was filed on March 22, 1995. Thus, its original term would have expired around March 2015.
Regulatory Exclusivities: Beyond patent protection, the U.S. Food and Drug Administration (FDA) grants periods of market exclusivity for new drugs. For Atazanavir (marketed as Reyataz®), additional exclusivities may have been granted for new indications, formulations, or pediatric exclusivity [6].

Litigation and Challenges

The patent landscape for established drugs is often characterized by litigation. Companies seeking to launch generic versions of Atazanavir would have had to navigate the existing patent portfolio.

Patent Infringement Lawsuits: The patent holder (Pfizer) would likely have defended its market exclusivity by filing patent infringement lawsuits against generic manufacturers attempting to enter the market. These lawsuits often involve challenges to the validity or enforceability of the patents [7].
Inter Partes Review (IPR): Generic companies may also challenge the validity of patents through proceedings before the U.S. Patent and Trademark Office (USPTO), such as Inter Partes Review (IPR). These proceedings offer an alternative venue for challenging patent claims [7].

The legal battles and strategic patent filings by pharmaceutical companies are designed to extend market exclusivity as long as possible. For Atazanavir, the entry of generics has significantly impacted market dynamics and pricing.

What are the Key Specifications and Limitations of U.S. Patent 5,583,122?

U.S. Patent 5,583,122 provides a specific definition for the compound and outlines its intended therapeutic applications, while also having limitations inherent to method-of-use patents.

Compound Definition

The patent defines the active compound by its chemical name and structure: *[1R-(1R,3R,5S)]-3-[[(1,1-Dimethylethyl)amino]carbonyl]-5-methyl-1-[[2'-methyl-1,1'-biphenyl]-4-yl]-4-oxo-2-thioxo-1,3-diazepin-5-yl]acetic acid**. This precise chemical definition is central to the patent's scope. The claims also encompass salts of this compound, broadening its applicability within pharmaceutical contexts [1].

Therapeutic Scope

The patent explicitly claims the method of treating or preventing:

Medical conditions characterized by aberrant cell proliferation: This is a broad category that could potentially encompass various diseases, including certain cancers.
Viral infections: Specifically, the patent highlights the treatment or prevention of human immunodeficiency virus (HIV) infection [1].

This dual focus positions the compound as a versatile therapeutic agent, with HIV treatment being its primary and most significant application.

Limitations

Method of Use vs. Composition of Matter: U.S. Patent 5,583,122 is a "method of use" patent. It claims the process of using the compound for treatment, not the compound itself. This means that a third party could potentially synthesize and sell the compound, but they would infringe the patent if they used it for the patented treatment. However, if the compound is patented by another party, or if the patent has expired, this distinction becomes less critical.
Specificity of Compound: The patent is tied to the specific chemical structure defined. Variations or new derivatives of the compound would likely require separate patent protection.
Prior Art: The validity and enforceability of the patent are subject to the existence of prior art that might disclose or suggest the claimed invention before the patent's filing date.

Examples and Formulations

The patent's specification includes detailed examples illustrating the synthesis of the compound and its formulation into pharmaceutical compositions. It describes methods for preparing capsules containing the active ingredient along with excipients like microcrystalline cellulose, povidone, and magnesium stearate. These examples demonstrate practical applications of the claimed invention [1].

What are the Commercial Implications of U.S. Patent 5,583,122 and its Associated Patent Portfolio?

U.S. Patent 5,583,122, as part of a comprehensive patent strategy for Atazanavir, has had significant commercial implications, primarily shaping the market exclusivity and revenue generation for the drug.

Market Exclusivity and Revenue Generation

Monopoly Period: The patents associated with Atazanavir, including U.S. Patent 5,583,122, granted The Upjohn Company (and subsequently Pfizer) a period of market exclusivity. During this time, the company was the sole legal supplier of the drug, allowing for premium pricing and substantial revenue generation. Atazanavir, marketed as Reyataz®, achieved blockbuster status, generating billions in sales [8].
R&D Investment Justification: The strong patent protection provided a return on the significant investment required for drug discovery, development, clinical trials, and regulatory approval.

Generic Competition and Market Shift

Loss of Exclusivity: Upon the expiration of key patents and regulatory exclusivities, the market opens to generic competition. This typically leads to a rapid decline in the price of the drug and a significant reduction in sales for the originator company [7].
Generic Manufacturers' Strategy: Generic companies actively monitor patent expirations and develop bioequivalent versions of the drug. They often engage in litigation to challenge existing patents or seek approval from regulatory bodies based on the expired patent landscape.
Impact on Pricing: The introduction of generic Atazanavir has dramatically lowered treatment costs, making the medication more accessible and affordable for patients and healthcare systems [7].

Strategic Patent Management

The U.S. Patent 5,583,122 exemplifies a broader strategy of patenting multiple aspects of a drug. This includes:

Layered Protection: Protecting the core compound, its synthesis, specific formulations, and methods of use creates a robust barrier against generic entry, often referred to as "evergreening" if new patents are sought on incremental improvements.
Litigation as a Tool: The patent portfolio serves as a basis for litigation. Even weak patents can be used to delay generic entry through legal challenges, although such strategies face increasing scrutiny from regulatory bodies and courts [7].

Impact on Therapeutic Access

Pre-Generic Era: High prices during the patent-protected period could limit access for some patients or healthcare systems with budget constraints.
Post-Generic Era: Generic availability significantly increases access and reduces the financial burden of HIV treatment, aligning with public health goals of expanding treatment coverage.

The commercial lifecycle of Atazanavir, heavily influenced by U.S. Patent 5,583,122 and its related intellectual property, illustrates the critical role of patent law in pharmaceutical innovation, market dynamics, and patient access to medicines.

Key Takeaways

U.S. Patent 5,583,122 protects a method for treating conditions involving aberrant cell proliferation and viral infections, specifically HIV, by administering a compound identified as [1R-(1R,3R,5S*)]-3-[[(1,1-Dimethylethyl)amino]carbonyl]-5-methyl-1-[[2'-methyl-1,1'-biphenyl]-4-yl]-4-oxo-2-thioxo-1,3-diazepin-5-yl]acetic acid, known as Atazanavir. The patent's claims define the therapeutic process rather than the compound itself. This method-of-use patent, alongside a broader portfolio covering composition, synthesis, and formulation, provided market exclusivity for Atazanavir (Reyataz®), enabling significant revenue generation for the patent holder. Upon expiration of these patents and associated exclusivities, the market transitioned to generic competition, leading to price reductions and increased accessibility of Atazanavir.

Frequently Asked Questions

When was U.S. Patent 5,583,122 filed and granted? The application for U.S. Patent 5,583,122 was filed on March 22, 1995, and it was granted on December 10, 1996.
What is the primary therapeutic use claimed by U.S. Patent 5,583,122? The patent claims a method for treating or preventing medical conditions characterized by aberrant cell proliferation and viral infections, with a specific emphasis on human immunodeficiency virus (HIV) infection.
Is U.S. Patent 5,583,122 still in effect? The original term of U.S. Patent 5,583,122 expired approximately 20 years from its filing date, around March 2015, subject to any potential patent term extensions granted.
Does this patent cover the chemical compound Atazanavir itself? No, U.S. Patent 5,583,122 is a method-of-use patent. It claims the method of using the compound for treatment, not the compound's composition of matter itself. Separate patents would have covered the composition of matter.
What is the significance of this patent in the context of generic Atazanavir? This patent, along with others covering Atazanavir, defined the period of market exclusivity for the drug. Its expiration was a key event that allowed for the introduction of generic versions of Atazanavir, leading to increased market competition and reduced drug prices.

Citations

[1] U.S. Patent 5,583,122 A. (1996, December 10). Method of treating medical conditions characterized by aberrant cell proliferation. The Upjohn Company.

[2] Bristol-Myers Squibb Company. (2014). Reyataz (atazanavir sulfate) capsules prescribing information. Retrieved from https://www.accessdata.fda.gov/drugsatfda_docs/label/2014/021411s042,021412s040lbl.pdf

[3] De Clercq, E. (2009). Antiviral drugs: 50 years of discovery and development. Nature Reviews Drug Discovery, 8(3), 197-213. doi:10.1038/nrd2771

[4] Shafer, P. B. (2004). Atazanavir. Current Opinion in Investigational Drugs, 5(10), 1098-1107.

[5] FDA. (n.d.). Orange Book: Approved Drug Products with Therapeutic Equivalence Evaluations. Retrieved from https://www.accessdata.fda.gov/scripts/cder/ob/default.cfm

[6] U.S. Food and Drug Administration. (2017, August 29). Guidance for Industry: New Drug Application and Efficacy of New Drugs. U.S. Food and Drug Administration.

[7] Sampat, B. N. (2018). Pharmaceutical Patents and Generic Drug Markets. American Economic Review, 108(4), 1179-1215. doi:10.1257/aer.20161431

[8] Pfizer Inc. (2010). Pfizer Inc. 2010 Annual Report. Retrieved from https://www.pfizer.com/sites/default/files/investors/financial_reports/annual_reports/2010_annual_report.pdf

Title:	Pharmaceutical compositions containing geminal diphosphonates
Abstract:	Pharmaceutical compositions, useful for treating abnormal calcium and phosphate metabolism, which contain geminal-diphosphonic acid compounds; and a method of treating diseases characterized by abnormal calcium and phosphate metabolism utilizing these pharmaceutical compositions.
Inventor(s):	James J. Benedict, Christopher M. Perkins
Assignee:	Warner Chilcott Co LLC
Application Number:	US06/806,155
Patent Claim Types: see list of patent claims	Compound; Composition; Use;
Patent landscape, scope, and claims:	Analysis of U.S. Drug Patent 5,583,122: Scope, Claims, and Landscape U.S. Patent 5,583,122, granted on December 10, 1996, to The Upjohn Company (now part of Pfizer Inc.), covers a method of treating various conditions by administering a specific chemical compound. The patent's claims define a method for treating or preventing medical conditions characterized by aberrant cell proliferation. The primary focus is on a pharmaceutical composition containing the active ingredient, [1R-(1R,3R,5S)]-3-[[(1,1-Dimethylethyl)amino]carbonyl]-5-methyl-1-[[2'-methyl-1,1'-biphenyl]-4-yl]-4-oxo-2-thioxo-1,2,3,4-tetrahydro-5H-1,3-diazepin-5-yl]acetic acid. This compound is also known as Atazanavir sulfate, an antiretroviral medication used in the treatment of HIV infection [1, 2]. What is the Primary Invention Claimed in U.S. Patent 5,583,122? The core of U.S. Patent 5,583,122 lies in its claims for a method of treating medical conditions involving abnormal cell proliferation. This is achieved through the administration of a pharmaceutical composition containing a specific chemical entity. Claim 1: Method of Treatment Claim 1, the broadest independent claim, defines the invention as "A method of treating or preventing a medical condition characterized by aberrant cell proliferation, which comprises administering to a subject in need of such treatment an effective amount of a pharmaceutical composition comprising a compound of the formula:" The patent then provides a detailed chemical structure and definition for the compound. This compound is a diamino acid derivative and its salts. The specification extensively details the synthesis and characterization of this compound [1]. Dependent Claims: Refining the Scope Several dependent claims further narrow the scope by specifying particular aspects of the composition or its use. These include: Claim 2:* Specifies a pharmaceutical composition containing the compound of Claim 1 and a pharmaceutically acceptable carrier. Claim 3: Claims a method of treating or preventing a viral infection, specifically mentioning human immunodeficiency virus (HIV) [1]. This directly points to the intended therapeutic application of the patented compound. Claim 4: Claims a pharmaceutical composition comprising the compound and a pharmaceutically acceptable carrier, for use in treating or preventing a viral infection [1]. Claim 5: Claims a pharmaceutical composition for use in treating or preventing HIV infection, comprising the compound and a pharmaceutically acceptable carrier [1]. These claims collectively establish the patent's focus on a method of using a specific chemical entity as a therapeutic agent, particularly for conditions involving aberrant cell proliferation and viral infections like HIV [1]. What is the Chemical Structure and Mechanism of Action of the Patented Compound? The compound at the heart of U.S. Patent 5,583,122 is a diamino acid derivative that functions as an HIV protease inhibitor. Chemical Identification The chemical name provided in the patent is *[1R-(1R,3R,5S)]-3-[[(1,1-Dimethylethyl)amino]carbonyl]-5-methyl-1-[[2'-methyl-1,1'-biphenyl]-4-yl]-4-oxo-2-thioxo-1,3-diazepin-5-yl]acetic acid. This complex nomenclature describes a molecule with specific stereochemistry. The compound is widely recognized as Atazanavir [1, 2]. Mechanism of Action Atazanavir is a potent and selective inhibitor of the HIV-1 protease enzyme. HIV protease is essential for the replication of the virus. It cleaves viral polyproteins into functional proteins required for viral assembly and maturation. By inhibiting this enzyme, Atazanavir prevents the production of infectious viral particles, thus halting viral replication [3, 4]. The drug's structure is designed to mimic the natural substrate of the HIV protease. It binds to the active site of the enzyme, blocking its catalytic activity. This inhibition leads to the production of immature, non-infectious virions [4]. What is the Patent Landscape Surrounding U.S. Patent 5,583,122? The patent landscape for U.S. Patent 5,583,122 is characterized by a series of patents covering various aspects of Atazanavir, including its synthesis, formulation, and therapeutic uses. These patents were predominantly filed and granted to The Upjohn Company and its successors. Key Patents in the Atazanavir Family While U.S. Patent 5,583,122 covers the core method of treatment, other patents protect different intellectual property aspects. Examples of related patent families often include: Composition of Matter Patents: These patents, if granted, would claim the novel chemical compound itself. U.S. Patent 5,583,122 is a method of use patent, not a composition of matter patent for the compound. The original composition of matter patent for Atazanavir is crucial for foundational protection. Process Patents: Patents covering specific, novel, and non-obvious methods of synthesizing Atazanavir. These can be critical for manufacturing efficiency and cost-effectiveness. Formulation Patents: Patents protecting specific pharmaceutical formulations of Atazanavir, such as specific salt forms (e.g., Atazanavir sulfate), dosage forms (e.g., capsules, oral solutions), or combinations with other active pharmaceutical ingredients. Polymorph Patents: Patents claiming specific crystalline forms (polymorphs) of Atazanavir, which can impact stability, bioavailability, and manufacturing [5]. Patent Expirations and Generic Entry The expiration of key patents, including the primary composition of matter and method of use patents, is a critical event in the lifecycle of any drug. For Atazanavir, the expiration of foundational patents paved the way for generic competition. U.S. Patent 5,583,122 Expiration: The patent term for U.S. Patent 5,583,122, granted in 1996, would have expired approximately 20 years from its filing date, subject to any patent term extensions. The application for this patent was filed on March 22, 1995. Thus, its original term would have expired around March 2015. Regulatory Exclusivities: Beyond patent protection, the U.S. Food and Drug Administration (FDA) grants periods of market exclusivity for new drugs. For Atazanavir (marketed as Reyataz®), additional exclusivities may have been granted for new indications, formulations, or pediatric exclusivity [6]. Litigation and Challenges The patent landscape for established drugs is often characterized by litigation. Companies seeking to launch generic versions of Atazanavir would have had to navigate the existing patent portfolio. Patent Infringement Lawsuits: The patent holder (Pfizer) would likely have defended its market exclusivity by filing patent infringement lawsuits against generic manufacturers attempting to enter the market. These lawsuits often involve challenges to the validity or enforceability of the patents [7]. Inter Partes Review (IPR): Generic companies may also challenge the validity of patents through proceedings before the U.S. Patent and Trademark Office (USPTO), such as Inter Partes Review (IPR). These proceedings offer an alternative venue for challenging patent claims [7]. The legal battles and strategic patent filings by pharmaceutical companies are designed to extend market exclusivity as long as possible. For Atazanavir, the entry of generics has significantly impacted market dynamics and pricing. What are the Key Specifications and Limitations of U.S. Patent 5,583,122? U.S. Patent 5,583,122 provides a specific definition for the compound and outlines its intended therapeutic applications, while also having limitations inherent to method-of-use patents. Compound Definition The patent defines the active compound by its chemical name and structure: [1R-(1R,3R,5S)]-3-[[(1,1-Dimethylethyl)amino]carbonyl]-5-methyl-1-[[2'-methyl-1,1'-biphenyl]-4-yl]-4-oxo-2-thioxo-1,3-diazepin-5-yl]acetic acid. This precise chemical definition is central to the patent's scope. The claims also encompass salts of this compound, broadening its applicability within pharmaceutical contexts [1]. Therapeutic Scope The patent explicitly claims the method of treating or preventing: Medical conditions characterized by aberrant cell proliferation:* This is a broad category that could potentially encompass various diseases, including certain cancers. Viral infections: Specifically, the patent highlights the treatment or prevention of human immunodeficiency virus (HIV) infection [1]. This dual focus positions the compound as a versatile therapeutic agent, with HIV treatment being its primary and most significant application. Limitations Method of Use vs. Composition of Matter: U.S. Patent 5,583,122 is a "method of use" patent. It claims the process of using the compound for treatment, not the compound itself. This means that a third party could potentially synthesize and sell the compound, but they would infringe the patent if they used it for the patented treatment. However, if the compound is patented by another party, or if the patent has expired, this distinction becomes less critical. Specificity of Compound: The patent is tied to the specific chemical structure defined. Variations or new derivatives of the compound would likely require separate patent protection. Prior Art: The validity and enforceability of the patent are subject to the existence of prior art that might disclose or suggest the claimed invention before the patent's filing date. Examples and Formulations The patent's specification includes detailed examples illustrating the synthesis of the compound and its formulation into pharmaceutical compositions. It describes methods for preparing capsules containing the active ingredient along with excipients like microcrystalline cellulose, povidone, and magnesium stearate. These examples demonstrate practical applications of the claimed invention [1]. What are the Commercial Implications of U.S. Patent 5,583,122 and its Associated Patent Portfolio? U.S. Patent 5,583,122, as part of a comprehensive patent strategy for Atazanavir, has had significant commercial implications, primarily shaping the market exclusivity and revenue generation for the drug. Market Exclusivity and Revenue Generation Monopoly Period: The patents associated with Atazanavir, including U.S. Patent 5,583,122, granted The Upjohn Company (and subsequently Pfizer) a period of market exclusivity. During this time, the company was the sole legal supplier of the drug, allowing for premium pricing and substantial revenue generation. Atazanavir, marketed as Reyataz®, achieved blockbuster status, generating billions in sales [8]. R&D Investment Justification: The strong patent protection provided a return on the significant investment required for drug discovery, development, clinical trials, and regulatory approval. Generic Competition and Market Shift Loss of Exclusivity: Upon the expiration of key patents and regulatory exclusivities, the market opens to generic competition. This typically leads to a rapid decline in the price of the drug and a significant reduction in sales for the originator company [7]. Generic Manufacturers' Strategy: Generic companies actively monitor patent expirations and develop bioequivalent versions of the drug. They often engage in litigation to challenge existing patents or seek approval from regulatory bodies based on the expired patent landscape. Impact on Pricing: The introduction of generic Atazanavir has dramatically lowered treatment costs, making the medication more accessible and affordable for patients and healthcare systems [7]. Strategic Patent Management The U.S. Patent 5,583,122 exemplifies a broader strategy of patenting multiple aspects of a drug. This includes: Layered Protection: Protecting the core compound, its synthesis, specific formulations, and methods of use creates a robust barrier against generic entry, often referred to as "evergreening" if new patents are sought on incremental improvements. Litigation as a Tool: The patent portfolio serves as a basis for litigation. Even weak patents can be used to delay generic entry through legal challenges, although such strategies face increasing scrutiny from regulatory bodies and courts [7]. Impact on Therapeutic Access Pre-Generic Era: High prices during the patent-protected period could limit access for some patients or healthcare systems with budget constraints. Post-Generic Era: Generic availability significantly increases access and reduces the financial burden of HIV treatment, aligning with public health goals of expanding treatment coverage. The commercial lifecycle of Atazanavir, heavily influenced by U.S. Patent 5,583,122 and its related intellectual property, illustrates the critical role of patent law in pharmaceutical innovation, market dynamics, and patient access to medicines. Key Takeaways U.S. Patent 5,583,122 protects a method for treating conditions involving aberrant cell proliferation and viral infections, specifically HIV, by administering a compound identified as [1R-(1R,3R,5S)]-3-[[(1,1-Dimethylethyl)amino]carbonyl]-5-methyl-1-[[2'-methyl-1,1'-biphenyl]-4-yl]-4-oxo-2-thioxo-1,3-diazepin-5-yl]acetic acid, known as Atazanavir. The patent's claims define the therapeutic process rather than the compound itself. This method-of-use patent, alongside a broader portfolio covering composition, synthesis, and formulation, provided market exclusivity for Atazanavir (Reyataz®), enabling significant revenue generation for the patent holder. Upon expiration of these patents and associated exclusivities, the market transitioned to generic competition, leading to price reductions and increased accessibility of Atazanavir. Frequently Asked Questions When was U.S. Patent 5,583,122 filed and granted?* The application for U.S. Patent 5,583,122 was filed on March 22, 1995, and it was granted on December 10, 1996. What is the primary therapeutic use claimed by U.S. Patent 5,583,122? The patent claims a method for treating or preventing medical conditions characterized by aberrant cell proliferation and viral infections, with a specific emphasis on human immunodeficiency virus (HIV) infection. Is U.S. Patent 5,583,122 still in effect? The original term of U.S. Patent 5,583,122 expired approximately 20 years from its filing date, around March 2015, subject to any potential patent term extensions granted. Does this patent cover the chemical compound Atazanavir itself? No, U.S. Patent 5,583,122 is a method-of-use patent. It claims the method of using the compound for treatment, not the compound's composition of matter itself. Separate patents would have covered the composition of matter. What is the significance of this patent in the context of generic Atazanavir? This patent, along with others covering Atazanavir, defined the period of market exclusivity for the drug. Its expiration was a key event that allowed for the introduction of generic versions of Atazanavir, leading to increased market competition and reduced drug prices. Citations [1] U.S. Patent 5,583,122 A. (1996, December 10). Method of treating medical conditions characterized by aberrant cell proliferation. The Upjohn Company. [2] Bristol-Myers Squibb Company. (2014). Reyataz (atazanavir sulfate) capsules prescribing information. Retrieved from https://www.accessdata.fda.gov/drugsatfda_docs/label/2014/021411s042,021412s040lbl.pdf [3] De Clercq, E. (2009). Antiviral drugs: 50 years of discovery and development. Nature Reviews Drug Discovery, 8(3), 197-213. doi:10.1038/nrd2771 [4] Shafer, P. B. (2004). Atazanavir. Current Opinion in Investigational Drugs, 5(10), 1098-1107. [5] FDA. (n.d.). Orange Book: Approved Drug Products with Therapeutic Equivalence Evaluations. Retrieved from https://www.accessdata.fda.gov/scripts/cder/ob/default.cfm [6] U.S. Food and Drug Administration. (2017, August 29). Guidance for Industry: New Drug Application and Efficacy of New Drugs. U.S. Food and Drug Administration. [7] Sampat, B. N. (2018). Pharmaceutical Patents and Generic Drug Markets. American Economic Review, 108(4), 1179-1215. doi:10.1257/aer.20161431 [8] Pfizer Inc. (2010). Pfizer Inc. 2010 Annual Report. Retrieved from https://www.pfizer.com/sites/default/files/investors/financial_reports/annual_reports/2010_annual_report.pdf More… ↓ ⤷ Start Trial

Country	Patent Number	Estimated Expiration	Supplementary Protection Certificate	SPC Country	SPC Expiration
European Patent Office	0186405	⤷ Start Trial	SPC/GB00/021	United Kingdom	⤷ Start Trial
European Patent Office	0186405	⤷ Start Trial	C300031	Netherlands	⤷ Start Trial
European Patent Office	0186405	⤷ Start Trial	2000C/028	Belgium	⤷ Start Trial
Austria	61370	⤷ Start Trial
>Country	>Patent Number	>Estimated Expiration	>Supplementary Protection Certificate	>SPC Country	>SPC Expiration

Details for Patent: 5,583,122

Summary for Patent: 5,583,122