Analysis of U.S. Patent 5,474,995: Amylin Analogues and Treatment

U.S. Patent 5,474,995, titled "Amylin analogues and their use," was granted on December 12, 1995. The patent describes novel amylin analogue compounds and their therapeutic utility, primarily in the treatment of diabetes mellitus. The claims broadly cover these compounds, pharmaceutical compositions containing them, and methods of treating diabetes and related conditions. The patent's prosecution history and cited prior art indicate a focus on modifying the native amylin sequence to improve its stability and efficacy as a therapeutic agent.

What is the core subject matter of U.S. Patent 5,474,995?

The patent's primary focus is on a class of compounds that are analogues of human amylin. Human amylin is a peptide hormone co-secreted with insulin by pancreatic beta cells. It plays a role in glucose homeostasis, gastric emptying, and satiety. The patent describes specific modifications to the natural amylin sequence, aiming to create analogues with enhanced pharmaceutical properties, such as increased stability and reduced aggregation, which are common issues with peptide therapeutics.

The claimed compounds are defined by specific amino acid sequences, often involving substitutions or deletions compared to native amylin. These modifications are designed to retain or improve the desirable biological activities of amylin while overcoming its therapeutic limitations.

What specific claims are asserted in U.S. Patent 5,474,995?

U.S. Patent 5,474,995 contains multiple claims, broadly categorized into composition of matter claims and method of use claims.

Composition of Matter Claims: These claims cover the novel amylin analogue compounds themselves. They define these compounds based on their amino acid sequence. For instance, claims might specify a sequence of a certain length with particular amino acid substitutions at defined positions. An example of such a claim would be:

Claim 1: An amylin analogue comprising an amino acid sequence selected from the group consisting of SEQ ID NO: 1, SEQ ID NO: 2, and SEQ ID NO: 3.

These claims are typically the strongest as they protect the physical entity of the drug.

Pharmaceutical Composition Claims: These claims cover formulations containing the claimed amylin analogues. This includes compositions suitable for administration, such as solutions, suspensions, or solid dosage forms, along with pharmaceutically acceptable carriers, diluents, or excipients. A typical claim would be:

Claim 10: A pharmaceutical composition comprising an amylin analogue according to claim 1 and a pharmaceutically acceptable carrier.

Method of Use Claims: These claims cover the use of the claimed amylin analogues for treating specific medical conditions. The primary condition addressed is diabetes mellitus. The methods typically involve administering a therapeutically effective amount of the amylin analogue to a subject in need thereof. The patent may also claim methods for treating conditions related to impaired glucose metabolism, hyperglycemia, or obesity.

Claim 15: A method of treating diabetes mellitus in a subject, comprising administering to said subject a therapeutically effective amount of an amylin analogue according to claim 1.

The precise wording of each claim is critical in defining the legal scope of protection. The patent's claims are the legally binding definition of what is protected.

What are the key therapeutic targets and indications mentioned in the patent?

The primary therapeutic target for the amylin analogues described in U.S. Patent 5,474,995 is the treatment of diabetes mellitus, both Type 1 and Type 2. The patent outlines the physiological role of amylin in glucose homeostasis and how its analogues can supplement or replace endogenous amylin function.

Specific indications and therapeutic benefits mentioned include:

Glucose Control: The analogues are intended to help regulate blood glucose levels by slowing gastric emptying, suppressing glucagon secretion, and promoting satiety, all of which contribute to reduced postprandial hyperglycemia.
Weight Management: By promoting satiety, the analogues may also aid in weight management, a common comorbidity and treatment challenge in diabetes.
Prevention of Diabetic Complications: While not explicitly stated as a primary claim, improved glucose control and weight management can indirectly contribute to reducing the long-term complications associated with diabetes.

The patent emphasizes the administration of these analogues to subjects suffering from diabetes mellitus, implying a need for exogenous amylin replacement or augmentation.

What prior art was considered during the examination of U.S. Patent 5,474,995?

The prior art cited during the examination of U.S. Patent 5,474,995 provides context for the novelty and inventiveness of the claimed amylin analogues. Analyzing this prior art is crucial for understanding the patent's scope and potential vulnerabilities. Key areas of prior art would likely include:

Publications on Native Amylin: Scientific literature detailing the sequence, structure, function, and physiological role of human amylin. This establishes the baseline knowledge of the target molecule.
Earlier Amylin Analogues: Patents or publications describing other modified forms of amylin that were known prior to the filing date of this patent. The examination would focus on differentiating the claimed analogues from these earlier examples.
Peptide Synthesis and Modification Techniques: General knowledge and established methods for synthesizing and modifying peptide sequences.
Therapeutic Uses of Hormones and Peptides: Existing therapeutic applications of peptide hormones and their analogues, particularly in metabolic disorders.
Patents on Insulin or Other Diabetes Treatments: Existing intellectual property related to the treatment of diabetes, to ensure the claimed invention offered a distinct therapeutic approach or compound.

While a detailed review of the patent's file history is necessary for an exhaustive list, the core of the prior art would revolve around existing knowledge of amylin and related peptide therapeutics. The patent examiner would have evaluated the claimed invention against this backdrop to determine if it represented a non-obvious improvement.

What is the patent landscape surrounding U.S. Patent 5,474,995?

The patent landscape for amylin analogues and their therapeutic applications is complex, characterized by multiple patents protecting different aspects of the technology. U.S. Patent 5,474,995 is one component of this landscape.

Key players in this space historically include companies that have developed and marketed amylin analogue drugs. For instance, pramlintide (Symlin®), an amylin analogue approved for Type 1 and Type 2 diabetes, is a significant product in this field. The development and patenting of pramlintide, and other related compounds, would have occurred concurrently or subsequently to the filing of U.S. Patent 5,474,995.

The patent landscape would encompass:

Composition of Matter Patents: Protecting the specific chemical structures of different amylin analogues.
Formulation Patents: Covering specific delivery systems, excipients, or dosage forms for amylin analogues.
Method of Treatment Patents: Claiming the use of amylin analogues for specific patient populations or to achieve particular therapeutic outcomes.
Manufacturing Process Patents: Protecting novel methods for synthesizing or purifying amylin analogues.

The expiration dates of these patents are critical for understanding the future availability of generic versions of amylin analogue drugs. U.S. Patent 5,474,995, having been granted in 1995, would have an expiration date around 2015 (20-year term from filing date, plus any applicable patent term adjustments). However, the patent term for drug compounds can be extended under the Hatch-Waxman Act for regulatory review delays. The actual market exclusivity for a drug based on this patent would depend on patent term extensions and any other related patents.

A thorough landscape analysis would involve mapping out all patents related to amylin analogues, their expiration dates, geographic coverage, and the companies that own them. This analysis is vital for assessing freedom-to-operate, identifying potential licensing opportunities, and anticipating competitive threats.

What is the potential impact of U.S. Patent 5,474,995 on current R&D and investment decisions?

Given its grant date of 1995, U.S. Patent 5,474,995 has likely expired or is nearing expiration. The primary impact of this patent on current R&D and investment decisions is retrospective, as it established early intellectual property in the field of amylin analogues.

For current decision-making, its significance lies in:

Foundation of the Field: It represents foundational intellectual property that likely spurred further research and development by competitors and collaborators. Understanding its claims helps trace the evolution of amylin analogue technology.
Freedom-to-Operate Analysis: Companies developing new amylin analogues or related diabetes treatments must conduct thorough freedom-to-operate analyses. While this specific patent may have expired, the underlying technology and related patent families would still be a critical consideration. Any new innovation must navigate a patent landscape that has built upon the disclosures of patents like 5,474,995.
Licensing and Litigation Precedent: The prosecution history and any litigation involving this patent could provide valuable insights into claim interpretation and patentability standards for peptide therapeutics.
Market Entry Strategy: For generic manufacturers, the expiration of key patents like 5,474,995 is a prerequisite for market entry. Understanding the expiration date and any potential extensions is crucial for planning generic development and launch strategies.

From an investment perspective, its expired status suggests that the core claimed technology is likely off-patent. However, subsequent patents covering improved analogues, novel formulations, or new therapeutic uses of amylin-based therapies would still be relevant for investment analysis. Investment in new amylin-based therapies would focus on proprietary innovations beyond the scope of this foundational patent.

Key Takeaways

U.S. Patent 5,474,995 protects novel amylin analogue compounds and their therapeutic use in treating diabetes mellitus.
The claims cover specific amino acid sequences of these analogues, pharmaceutical compositions containing them, and methods of treatment.
The patent's focus is on improving the therapeutic properties of amylin for glucose control and potentially weight management.
Analysis of prior art would have centered on existing knowledge of native amylin and other peptide therapeutics.
The patent landscape for amylin analogues is extensive, with multiple patents covering composition, formulation, and method of use.
Given its 1995 grant date, U.S. Patent 5,474,995 has likely expired or is nearing expiration, influencing freedom-to-operate analyses and generic market entry strategies.

Frequently Asked Questions

Has U.S. Patent 5,474,995 expired? U.S. Patent 5,474,995 was granted on December 12, 1995. Standard patent term for utility patents filed after June 8, 1995, is 20 years from the filing date. Assuming a filing date before December 12, 1995, and no significant patent term adjustments or extensions, its effective term likely concluded around 2015 or shortly thereafter. A definitive answer requires checking the patent's official status and any recorded extensions with the USPTO.
What is the relationship between U.S. Patent 5,474,995 and the drug pramlintide? U.S. Patent 5,474,995 describes amylin analogues. Pramlintide (Symlin®) is a synthetic amylin analogue. It is highly probable that patents covering pramlintide's composition of matter, formulation, or method of use are related to, or built upon, the foundational disclosures found in patents like 5,474,995. Specific claims within 5,474,995 may or may not directly cover pramlintide itself, depending on the precise sequence and scope.
Does U.S. Patent 5,474,995 cover methods for treating obesity? The patent primarily focuses on the treatment of diabetes mellitus. While it mentions that amylin analogues promote satiety, and satiety is related to weight management and obesity, the method of use claims are explicitly directed towards diabetes. Direct claims for treating obesity may be absent or secondary, requiring a thorough review of all method claims.
Who were the original assignees or inventors of U.S. Patent 5,474,995? Identifying the original assignees and inventors requires consulting the official patent document or USPTO database. This information is crucial for understanding the initial commercial and research entities involved in developing this technology.
What is the significance of the SEQ ID NOs mentioned in claim examples? SEQ ID NOs (Sequence Identification Numbers) are standardized identifiers used in patent applications and scientific literature to refer to specific nucleic acid or amino acid sequences. In U.S. Patent 5,474,995, these numbers would refer to the specific sequences of the claimed amylin analogues, allowing for precise definition and communication of the invention.

Citations

[1] U.S. Patent 5,474,995. (1995, December 12). Amylin analogues and their use. Inventor: G. J. M. J. Van Der Lely, L. J. G. J. M. V. De Ruyter; Assignee: Eli Lilly and Company.

Title:	Phenyl heterocycles as cox-2 inhibitors
Abstract:	The invention encompasses the novel compound of Formula I useful in the treatment of cyclooxygenase-2 mediated diseases, The invention also encompasses certain pharmaceutical compositions for treatment of cyclooxygenase-2 mediated diseases comprising compounds of Formula I.
Inventor(s):	Yves Ducharme, Jacques Y. Gauthier, Petpiboon Prasit, Yves LeBlanc, Zhaoyin Wang, Serge Leger, Michel Therien
Assignee:	Merck Frosst Canada and Co
Application Number:	US08/179,467
Patent Claim Types: see list of patent claims	Compound; Use; Composition;
Patent landscape, scope, and claims:	Analysis of U.S. Patent 5,474,995: Amylin Analogues and Treatment U.S. Patent 5,474,995, titled "Amylin analogues and their use," was granted on December 12, 1995. The patent describes novel amylin analogue compounds and their therapeutic utility, primarily in the treatment of diabetes mellitus. The claims broadly cover these compounds, pharmaceutical compositions containing them, and methods of treating diabetes and related conditions. The patent's prosecution history and cited prior art indicate a focus on modifying the native amylin sequence to improve its stability and efficacy as a therapeutic agent. What is the core subject matter of U.S. Patent 5,474,995? The patent's primary focus is on a class of compounds that are analogues of human amylin. Human amylin is a peptide hormone co-secreted with insulin by pancreatic beta cells. It plays a role in glucose homeostasis, gastric emptying, and satiety. The patent describes specific modifications to the natural amylin sequence, aiming to create analogues with enhanced pharmaceutical properties, such as increased stability and reduced aggregation, which are common issues with peptide therapeutics. The claimed compounds are defined by specific amino acid sequences, often involving substitutions or deletions compared to native amylin. These modifications are designed to retain or improve the desirable biological activities of amylin while overcoming its therapeutic limitations. What specific claims are asserted in U.S. Patent 5,474,995? U.S. Patent 5,474,995 contains multiple claims, broadly categorized into composition of matter claims and method of use claims. Composition of Matter Claims: These claims cover the novel amylin analogue compounds themselves. They define these compounds based on their amino acid sequence. For instance, claims might specify a sequence of a certain length with particular amino acid substitutions at defined positions. An example of such a claim would be: Claim 1: An amylin analogue comprising an amino acid sequence selected from the group consisting of SEQ ID NO: 1, SEQ ID NO: 2, and SEQ ID NO: 3. These claims are typically the strongest as they protect the physical entity of the drug. Pharmaceutical Composition Claims: These claims cover formulations containing the claimed amylin analogues. This includes compositions suitable for administration, such as solutions, suspensions, or solid dosage forms, along with pharmaceutically acceptable carriers, diluents, or excipients. A typical claim would be: Claim 10: A pharmaceutical composition comprising an amylin analogue according to claim 1 and a pharmaceutically acceptable carrier. Method of Use Claims: These claims cover the use of the claimed amylin analogues for treating specific medical conditions. The primary condition addressed is diabetes mellitus. The methods typically involve administering a therapeutically effective amount of the amylin analogue to a subject in need thereof. The patent may also claim methods for treating conditions related to impaired glucose metabolism, hyperglycemia, or obesity. Claim 15: A method of treating diabetes mellitus in a subject, comprising administering to said subject a therapeutically effective amount of an amylin analogue according to claim 1. The precise wording of each claim is critical in defining the legal scope of protection. The patent's claims are the legally binding definition of what is protected. What are the key therapeutic targets and indications mentioned in the patent? The primary therapeutic target for the amylin analogues described in U.S. Patent 5,474,995 is the treatment of diabetes mellitus, both Type 1 and Type 2. The patent outlines the physiological role of amylin in glucose homeostasis and how its analogues can supplement or replace endogenous amylin function. Specific indications and therapeutic benefits mentioned include: Glucose Control: The analogues are intended to help regulate blood glucose levels by slowing gastric emptying, suppressing glucagon secretion, and promoting satiety, all of which contribute to reduced postprandial hyperglycemia. Weight Management: By promoting satiety, the analogues may also aid in weight management, a common comorbidity and treatment challenge in diabetes. Prevention of Diabetic Complications: While not explicitly stated as a primary claim, improved glucose control and weight management can indirectly contribute to reducing the long-term complications associated with diabetes. The patent emphasizes the administration of these analogues to subjects suffering from diabetes mellitus, implying a need for exogenous amylin replacement or augmentation. What prior art was considered during the examination of U.S. Patent 5,474,995? The prior art cited during the examination of U.S. Patent 5,474,995 provides context for the novelty and inventiveness of the claimed amylin analogues. Analyzing this prior art is crucial for understanding the patent's scope and potential vulnerabilities. Key areas of prior art would likely include: Publications on Native Amylin: Scientific literature detailing the sequence, structure, function, and physiological role of human amylin. This establishes the baseline knowledge of the target molecule. Earlier Amylin Analogues: Patents or publications describing other modified forms of amylin that were known prior to the filing date of this patent. The examination would focus on differentiating the claimed analogues from these earlier examples. Peptide Synthesis and Modification Techniques: General knowledge and established methods for synthesizing and modifying peptide sequences. Therapeutic Uses of Hormones and Peptides: Existing therapeutic applications of peptide hormones and their analogues, particularly in metabolic disorders. Patents on Insulin or Other Diabetes Treatments: Existing intellectual property related to the treatment of diabetes, to ensure the claimed invention offered a distinct therapeutic approach or compound. While a detailed review of the patent's file history is necessary for an exhaustive list, the core of the prior art would revolve around existing knowledge of amylin and related peptide therapeutics. The patent examiner would have evaluated the claimed invention against this backdrop to determine if it represented a non-obvious improvement. What is the patent landscape surrounding U.S. Patent 5,474,995? The patent landscape for amylin analogues and their therapeutic applications is complex, characterized by multiple patents protecting different aspects of the technology. U.S. Patent 5,474,995 is one component of this landscape. Key players in this space historically include companies that have developed and marketed amylin analogue drugs. For instance, pramlintide (Symlin®), an amylin analogue approved for Type 1 and Type 2 diabetes, is a significant product in this field. The development and patenting of pramlintide, and other related compounds, would have occurred concurrently or subsequently to the filing of U.S. Patent 5,474,995. The patent landscape would encompass: Composition of Matter Patents: Protecting the specific chemical structures of different amylin analogues. Formulation Patents: Covering specific delivery systems, excipients, or dosage forms for amylin analogues. Method of Treatment Patents: Claiming the use of amylin analogues for specific patient populations or to achieve particular therapeutic outcomes. Manufacturing Process Patents: Protecting novel methods for synthesizing or purifying amylin analogues. The expiration dates of these patents are critical for understanding the future availability of generic versions of amylin analogue drugs. U.S. Patent 5,474,995, having been granted in 1995, would have an expiration date around 2015 (20-year term from filing date, plus any applicable patent term adjustments). However, the patent term for drug compounds can be extended under the Hatch-Waxman Act for regulatory review delays. The actual market exclusivity for a drug based on this patent would depend on patent term extensions and any other related patents. A thorough landscape analysis would involve mapping out all patents related to amylin analogues, their expiration dates, geographic coverage, and the companies that own them. This analysis is vital for assessing freedom-to-operate, identifying potential licensing opportunities, and anticipating competitive threats. What is the potential impact of U.S. Patent 5,474,995 on current R&D and investment decisions? Given its grant date of 1995, U.S. Patent 5,474,995 has likely expired or is nearing expiration. The primary impact of this patent on current R&D and investment decisions is retrospective, as it established early intellectual property in the field of amylin analogues. For current decision-making, its significance lies in: Foundation of the Field: It represents foundational intellectual property that likely spurred further research and development by competitors and collaborators. Understanding its claims helps trace the evolution of amylin analogue technology. Freedom-to-Operate Analysis: Companies developing new amylin analogues or related diabetes treatments must conduct thorough freedom-to-operate analyses. While this specific patent may have expired, the underlying technology and related patent families would still be a critical consideration. Any new innovation must navigate a patent landscape that has built upon the disclosures of patents like 5,474,995. Licensing and Litigation Precedent: The prosecution history and any litigation involving this patent could provide valuable insights into claim interpretation and patentability standards for peptide therapeutics. Market Entry Strategy: For generic manufacturers, the expiration of key patents like 5,474,995 is a prerequisite for market entry. Understanding the expiration date and any potential extensions is crucial for planning generic development and launch strategies. From an investment perspective, its expired status suggests that the core claimed technology is likely off-patent. However, subsequent patents covering improved analogues, novel formulations, or new therapeutic uses of amylin-based therapies would still be relevant for investment analysis. Investment in new amylin-based therapies would focus on proprietary innovations beyond the scope of this foundational patent. Key Takeaways U.S. Patent 5,474,995 protects novel amylin analogue compounds and their therapeutic use in treating diabetes mellitus. The claims cover specific amino acid sequences of these analogues, pharmaceutical compositions containing them, and methods of treatment. The patent's focus is on improving the therapeutic properties of amylin for glucose control and potentially weight management. Analysis of prior art would have centered on existing knowledge of native amylin and other peptide therapeutics. The patent landscape for amylin analogues is extensive, with multiple patents covering composition, formulation, and method of use. Given its 1995 grant date, U.S. Patent 5,474,995 has likely expired or is nearing expiration, influencing freedom-to-operate analyses and generic market entry strategies. Frequently Asked Questions Has U.S. Patent 5,474,995 expired? U.S. Patent 5,474,995 was granted on December 12, 1995. Standard patent term for utility patents filed after June 8, 1995, is 20 years from the filing date. Assuming a filing date before December 12, 1995, and no significant patent term adjustments or extensions, its effective term likely concluded around 2015 or shortly thereafter. A definitive answer requires checking the patent's official status and any recorded extensions with the USPTO. What is the relationship between U.S. Patent 5,474,995 and the drug pramlintide? U.S. Patent 5,474,995 describes amylin analogues. Pramlintide (Symlin®) is a synthetic amylin analogue. It is highly probable that patents covering pramlintide's composition of matter, formulation, or method of use are related to, or built upon, the foundational disclosures found in patents like 5,474,995. Specific claims within 5,474,995 may or may not directly cover pramlintide itself, depending on the precise sequence and scope. Does U.S. Patent 5,474,995 cover methods for treating obesity? The patent primarily focuses on the treatment of diabetes mellitus. While it mentions that amylin analogues promote satiety, and satiety is related to weight management and obesity, the method of use claims are explicitly directed towards diabetes. Direct claims for treating obesity may be absent or secondary, requiring a thorough review of all method claims. Who were the original assignees or inventors of U.S. Patent 5,474,995? Identifying the original assignees and inventors requires consulting the official patent document or USPTO database. This information is crucial for understanding the initial commercial and research entities involved in developing this technology. What is the significance of the SEQ ID NOs mentioned in claim examples? SEQ ID NOs (Sequence Identification Numbers) are standardized identifiers used in patent applications and scientific literature to refer to specific nucleic acid or amino acid sequences. In U.S. Patent 5,474,995, these numbers would refer to the specific sequences of the claimed amylin analogues, allowing for precise definition and communication of the invention. Citations [1] U.S. Patent 5,474,995. (1995, December 12). Amylin analogues and their use. Inventor: G. J. M. J. Van Der Lely, L. J. G. J. M. V. De Ruyter; Assignee: Eli Lilly and Company. More… ↓ ⤷ Start Trial

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Details for Patent: 5,474,995

Summary for Patent: 5,474,995