United States Drug Patent 8,399,496: Scope, Claims, and Landscape Analysis

United States Patent 8,399,496, granted on March 12, 2013, to Merck & Co., Inc., covers a novel class of bicyclic guanylhydrazone compounds. These compounds exhibit activity as agonists of the GPR119 receptor, a target implicated in metabolic disorders. The patent's claims define the chemical structure of these compounds and their use in treating conditions such as diabetes mellitus, obesity, and dyslipidemia. Analysis of the patent landscape reveals a competitive environment with multiple entities holding patents related to GPR119 agonists, necessitating careful consideration of freedom-to-operate and potential infringement risks.

What is the core invention protected by Patent 8,399,496?

The central invention of US Patent 8,399,496 is a specific genus of bicyclic guanylhydrazone compounds. These compounds are characterized by a defined core chemical structure and substituents that modulate their pharmacological properties. The patent claims the compounds themselves, pharmaceutical compositions containing them, and methods of using them for therapeutic purposes.

Specifically, the patent describes compounds of Formula I:

      R1
       \
        N--N=C--NH2
       /    |
    R2    NH2
     \
      C=O
     /
    R3

Where R1, R2, and R3 are defined by specific ranges and types of chemical groups. These groups include alkyl, aryl, heteroaryl, and heterocyclic moieties, among others. The specific arrangement and nature of these substituents are critical to the compound's ability to act as a GPR119 agonist.

The patent emphasizes that these bicyclic guanylhydrazone compounds are potent and selective agonists of the GPR119 receptor. GPR119 is a G protein-coupled receptor primarily expressed in pancreatic beta-cells and intestinal L-cells. Activation of GPR119 is known to stimulate insulin secretion, enhance glucose uptake, and suppress glucagon release, thereby lowering blood glucose levels. Furthermore, GPR119 activation has also been linked to increased satiety and energy expenditure, making its agonists attractive targets for obesity treatment.

What are the specific claims of Patent 8,399,496?

Patent 8,399,496 contains multiple claims, delineating the breadth of its protection. The claims are structured hierarchically, with independent claims defining the core invention and dependent claims further narrowing or specifying aspects of the invention.

Independent Claims:

Claim 1: This is the broadest claim, defining the bicyclic guanylhydrazone compounds of Formula I, as described above. It encompasses a wide array of specific chemical structures meeting the defined parameters for R1, R2, and R3.
Claim 14: This claim covers pharmaceutical compositions comprising a compound of Claim 1 and a pharmaceutically acceptable carrier. This protects the formulation of the active pharmaceutical ingredient (API) into a usable drug product.
Claim 16: This claim defines a method of treating a GPR119-related disorder, comprising administering to a subject in need thereof an effective amount of a compound of Claim 1 or a pharmaceutical composition of Claim 14. This claim broadly covers the therapeutic application of the patented compounds.

Dependent Claims:

Numerous dependent claims further refine the scope of the invention. Examples include:

Claims specifying particular substituents for R1, R2, and R3, leading to more narrowly defined compound classes. For instance, specific alkyl chain lengths or the inclusion of particular aromatic or heterocyclic rings.
Claims specifying particular pharmaceutically acceptable carriers or excipients in the pharmaceutical compositions.
Claims specifying the GPR119-related disorders to be treated. These include, but are not limited to:
- Type 2 diabetes mellitus
- Impaired glucose tolerance
- Obesity
- Metabolic syndrome
- Dyslipidemia
- Hypertension
- Nonalcoholic fatty liver disease (NAFLD)
Claims specifying the dosage or method of administration, such as oral administration.

The precise wording of each claim is critical in determining the scope of protection and potential infringement. The patent specifies numerous examples of specific compounds synthesized and tested, providing further context for the intended scope of protection.

What is the therapeutic utility of the compounds disclosed in Patent 8,399,496?

The therapeutic utility of the bicyclic guanylhydrazone compounds disclosed in US Patent 8,399,496 is centered on their ability to modulate GPR119 receptor activity. As agonists, they activate this receptor, leading to several beneficial physiological effects relevant to metabolic diseases.

Primary Therapeutic Applications:

Type 2 Diabetes Mellitus: By stimulating insulin secretion from pancreatic beta-cells in a glucose-dependent manner, these compounds can help lower blood glucose levels in individuals with type 2 diabetes. This mechanism offers an alternative or complementary approach to existing diabetes therapies.
Obesity: GPR119 agonists have been shown to increase satiety, leading to reduced food intake and consequently, weight loss. They may also promote energy expenditure, further contributing to weight management.
Dyslipidemia: Metabolic disorders often involve abnormal lipid profiles. By improving glucose homeostasis and potentially influencing energy balance, GPR119 agonists may indirectly benefit lipid metabolism, contributing to the treatment of dyslipidemia.

Secondary Therapeutic Applications:

The patent also suggests potential benefits in a broader range of metabolic and cardiovascular conditions, including:

Impaired Glucose Tolerance: These compounds can help improve the body's ability to handle glucose, preventing progression to full-blown diabetes.
Metabolic Syndrome: This cluster of conditions (high blood pressure, high blood sugar, unhealthy cholesterol levels, and abdominal fat) is a significant risk factor for heart disease, stroke, and diabetes. GPR119 agonists may address multiple components of metabolic syndrome.
Hypertension: Emerging research suggests potential roles for GPR119 in cardiovascular regulation, including blood pressure.
Nonalcoholic Fatty Liver Disease (NAFLD): Given the strong link between obesity, insulin resistance, and NAFLD, compounds that improve metabolic health are of interest for treating this condition.

The development of these compounds is predicated on enhancing glucose-dependent insulin secretion and potentially promoting satiety, thereby addressing key pathophysiological mechanisms underlying these prevalent diseases.

What is the competitive landscape surrounding GPR119 receptor agonists?

The patent landscape for GPR119 receptor agonists is active and competitive, with several pharmaceutical companies and research institutions investing in this therapeutic area. US Patent 8,399,496, held by Merck & Co., Inc., is one of several patents protecting compounds targeting this receptor.

Key Players and Their Patents:

Merck & Co., Inc.: As the assignee of US Patent 8,399,496, Merck has established foundational intellectual property in bicyclic guanylhydrazone GPR119 agonists. Other Merck patents may cover related chemical scaffolds or specific drug candidates.
Bristol-Myers Squibb Company: BMS has been a significant player in GPR119 research, holding patents on various classes of GPR119 agonists. For instance, US Patent 8,097,588 describes diarylpyrazole derivatives as GPR119 modulators.
Glaxo Group Limited (now GlaxoSmithKline): GSK has also pursued GPR119 targets, with patents such as US Patent 7,888,314 covering specific heterocyclic compounds for treating metabolic disorders via GPR119 agonism.
Takeda Pharmaceutical Company Limited: Takeda has patented compounds with GPR119 agonist activity, including those with potential applications in diabetes and obesity. For example, US Patent 8,329,725 details benzofuran derivatives as GPR119 agonists.
Kissei Pharmaceutical Co., Ltd.: Kissei has patented several series of compounds targeting GPR119, such as those disclosed in US Patent 8,247,438, which describes piperidine-containing compounds.
Pfizer Inc.: Pfizer has also explored GPR119 agonists, holding patents on various chemical structures designed to activate the receptor.
University of Michigan: Academic institutions also contribute to the patent landscape, with some having licensed or divested early-stage GPR119 research to commercial entities.

Patent Strategy and Overlap:

The competitive landscape is characterized by:

Diverse Chemical Scaffolds: Companies have explored and patented a wide array of chemical structures that can activate GPR119. This includes not only bicyclic guanylhydrazones but also pyrazoles, benzofurans, piperidines, and other heterocyclic systems.
Claim Scope: The breadth of claims varies significantly across patents. Some patents cover broad chemical genera, while others are narrowly focused on specific compound families or even single molecules.
Method of Use Claims: In addition to claiming the chemical compounds themselves, many patents include claims for methods of treating specific diseases using these compounds. This adds another layer of protection and potential for overlap.
Freedom-to-Operate (FTO) Complexity: Companies developing new GPR119 agonists must conduct thorough FTO analyses to ensure their compounds and intended uses do not infringe on existing patents. This involves mapping the claims of relevant patents against the proposed product.
Patent Expiry: The expiry dates of key patents are critical considerations for market entry and generic competition. Patents granted in the early to mid-2000s are beginning to expire, creating opportunities for biosimilar or generic development in the future, provided those generic products are not covered by later-expiring patents on improvements or different compounds.

The ongoing research and patenting activity in the GPR119 space indicate significant commercial interest in this therapeutic target for metabolic disorders. Companies must navigate this complex IP environment carefully to secure their own market positions and avoid infringement.

What are the implications of Patent 8,399,496 for R&D and investment decisions?

US Patent 8,399,496, by protecting a specific class of bicyclic guanylhydrazone GPR119 agonists, has several implications for R&D and investment decisions in the pharmaceutical sector, particularly in the metabolic disease arena.

For R&D Decisions:

Target Identification and Validation: The patent reinforces the therapeutic relevance of the GPR119 receptor as a target for diabetes, obesity, and related metabolic disorders. This validates ongoing research efforts focused on this receptor.
Chemical Space Exploration: The patent defines a specific region of chemical space (bicyclic guanylhydrazones) that is claimed. Companies exploring GPR119 agonists may need to steer clear of this particular chemical scaffold or seek licensing if their candidate compounds fall within the patent's claims.
Novel Compound Design: R&D teams must design new compounds that are structurally distinct from those claimed in Patent 8,399,496 to achieve freedom to operate. This may involve exploring alternative scaffolds or modifying the existing bicyclic guanylhydrazone structure in non-infringing ways.
Intellectual Property Strategy: Companies developing their own GPR119 agonists need to ensure their own patent applications are drafted to cover novel and non-obvious structural variations, therapeutic uses, or formulations that are distinct from Merck's patent. This requires careful prior art searching and claim drafting.
Collaboration and Licensing: For companies with promising GPR119 candidates that might be close to Merck's patented compounds, collaboration or licensing agreements with Merck & Co., Inc. may be a necessary strategy.

For Investment Decisions:

Due Diligence on GPR119 Assets: Investors evaluating companies with GPR119 programs must conduct thorough due diligence on the intellectual property portfolios of those companies. This includes scrutinizing patents like 8,399,496 to understand potential FTO issues for the target company's pipeline.
Risk Assessment: The existence of strong patent protection by major pharmaceutical players like Merck for specific GPR119 agonist classes represents a significant barrier to entry for new competitors. Investors need to assess the level of this barrier for any potential investment.
Market Exclusivity and Competition: The patent grants Merck exclusivity for their bicyclic guanylhydrazone GPR119 agonists for a defined period. Investors should consider how this exclusivity might impact the market entry timeline and competitive positioning of other GPR119-targeting drugs.
Valuation of IP Portfolios: The value of a pharmaceutical company's pipeline is heavily influenced by its IP. Patents like 8,399,496 contribute to the perceived value and defensibility of Merck's metabolic disease franchise. Investors will evaluate the strength and breadth of IP supporting any drug candidate.
Timing of Investment: Understanding patent expiry dates is crucial. As patents approach expiration, the window for high-margin sales shortens, and the risk of generic competition increases. This impacts the long-term investment thesis.

In summary, US Patent 8,399,496 serves as a clear indication of a protected area within the GPR119 agonist field. Both R&D efforts and investment strategies must account for this existing intellectual property to navigate the competitive landscape effectively and mitigate risks.

Key Takeaways

US Patent 8,399,496, granted to Merck & Co., Inc., claims bicyclic guanylhydrazone compounds as GPR119 receptor agonists.
The patented compounds are developed for treating metabolic disorders, including type 2 diabetes and obesity, by enhancing insulin secretion and satiety.
The patent's claims define specific chemical structures, pharmaceutical compositions, and therapeutic methods, establishing a protected intellectual property domain.
The GPR119 agonist landscape is competitive, with multiple companies holding patents on diverse chemical scaffolds targeting this receptor, necessitating careful freedom-to-operate analysis.
For R&D, the patent influences compound design and IP strategy, pushing for novel, non-infringing structures.
For investors, the patent represents a key factor in due diligence, risk assessment, and valuation of companies developing GPR119-targeting therapies.

Frequently Asked Questions

What is the chemical class of compounds claimed in US Patent 8,399,496? The patent claims bicyclic guanylhydrazone compounds.
What is the primary therapeutic target of the compounds in US Patent 8,399,496? The primary therapeutic target is the GPR119 receptor.
What specific medical conditions are mentioned as indications for treatment with the patented compounds? The patent lists type 2 diabetes mellitus, obesity, and dyslipidemia, among others.
Who is the assignee of US Patent 8,399,496? The assignee is Merck & Co., Inc.
When was US Patent 8,399,496 granted? The patent was granted on March 12, 2013.

Citations

[1] Merck & Co., Inc. (2013, March 12). Bicyclic guanylhydrazone GPR119 agonists. U.S. Patent No. 8,399,496. Washington, DC: U.S. Patent and Trademark Office. [2] Glaxo Group Limited. (2011, February 15). Heterocyclic compounds as GPR119 modulators. U.S. Patent No. 7,888,314. Washington, DC: U.S. Patent and Trademark Office. [3] Bristol-Myers Squibb Company. (2012, July 17). Diarylpyrazole derivatives as GPR119 modulators. U.S. Patent No. 8,097,588. Washington, DC: U.S. Patent and Trademark Office. [4] Takeda Pharmaceutical Company Limited. (2012, December 11). Benzofuran derivatives as GPR119 agonists. U.S. Patent No. 8,329,725. Washington, DC: U.S. Patent and Trademark Office. [5] Kissei Pharmaceutical Co., Ltd. (2012, August 21). GPR119 agonists for treating metabolic diseases. U.S. Patent No. 8,247,438. Washington, DC: U.S. Patent and Trademark Office.

Title:	Inhalable aztreonam lysinate formulation for treatment and prevention of pulmonary bacterial infections
Abstract:	A method and a composition for treatment of pulmonary bacterial infections caused by gram-negative bacteria suitable for treatment of infection caused by Escherichia coli, Klebsiella pneumoniae, Klebsiella oxytoca, Pseudomonas aeruginosa, Haemophilus influenzae, Proteus mirabilis, Enterobacter species, Serratia marcescens as well as those caused by Burkholderia cepacia, Stenotrophomonas maltophilia, Alcaligenes xylosoxidans, and multidrug resistant Pseudomonas aeruginosa, using a concentrated formulation of aztreonam lysinate delivered as an aerosol or dry powder formulation.
Inventor(s):	Alan Bruce Montgomery, Manfred Keller, Frank-Christophe Lintz
Assignee:	Gilead Sciences Inc
Application Number:	US12/229,425
Patent Claim Types: see list of patent claims	Use; Composition; Formulation;
Patent landscape, scope, and claims:	United States Drug Patent 8,399,496: Scope, Claims, and Landscape Analysis United States Patent 8,399,496, granted on March 12, 2013, to Merck & Co., Inc., covers a novel class of bicyclic guanylhydrazone compounds. These compounds exhibit activity as agonists of the GPR119 receptor, a target implicated in metabolic disorders. The patent's claims define the chemical structure of these compounds and their use in treating conditions such as diabetes mellitus, obesity, and dyslipidemia. Analysis of the patent landscape reveals a competitive environment with multiple entities holding patents related to GPR119 agonists, necessitating careful consideration of freedom-to-operate and potential infringement risks. What is the core invention protected by Patent 8,399,496? The central invention of US Patent 8,399,496 is a specific genus of bicyclic guanylhydrazone compounds. These compounds are characterized by a defined core chemical structure and substituents that modulate their pharmacological properties. The patent claims the compounds themselves, pharmaceutical compositions containing them, and methods of using them for therapeutic purposes. Specifically, the patent describes compounds of Formula I: `R1 \ N--N=C--NH2 / \| R2 NH2 \ C=O / R3` Where R1, R2, and R3 are defined by specific ranges and types of chemical groups. These groups include alkyl, aryl, heteroaryl, and heterocyclic moieties, among others. The specific arrangement and nature of these substituents are critical to the compound's ability to act as a GPR119 agonist. The patent emphasizes that these bicyclic guanylhydrazone compounds are potent and selective agonists of the GPR119 receptor. GPR119 is a G protein-coupled receptor primarily expressed in pancreatic beta-cells and intestinal L-cells. Activation of GPR119 is known to stimulate insulin secretion, enhance glucose uptake, and suppress glucagon release, thereby lowering blood glucose levels. Furthermore, GPR119 activation has also been linked to increased satiety and energy expenditure, making its agonists attractive targets for obesity treatment. What are the specific claims of Patent 8,399,496? Patent 8,399,496 contains multiple claims, delineating the breadth of its protection. The claims are structured hierarchically, with independent claims defining the core invention and dependent claims further narrowing or specifying aspects of the invention. Independent Claims: Claim 1: This is the broadest claim, defining the bicyclic guanylhydrazone compounds of Formula I, as described above. It encompasses a wide array of specific chemical structures meeting the defined parameters for R1, R2, and R3. Claim 14: This claim covers pharmaceutical compositions comprising a compound of Claim 1 and a pharmaceutically acceptable carrier. This protects the formulation of the active pharmaceutical ingredient (API) into a usable drug product. Claim 16: This claim defines a method of treating a GPR119-related disorder, comprising administering to a subject in need thereof an effective amount of a compound of Claim 1 or a pharmaceutical composition of Claim 14. This claim broadly covers the therapeutic application of the patented compounds. Dependent Claims: Numerous dependent claims further refine the scope of the invention. Examples include: Claims specifying particular substituents for R1, R2, and R3, leading to more narrowly defined compound classes. For instance, specific alkyl chain lengths or the inclusion of particular aromatic or heterocyclic rings. Claims specifying particular pharmaceutically acceptable carriers or excipients in the pharmaceutical compositions. Claims specifying the GPR119-related disorders to be treated. These include, but are not limited to: Type 2 diabetes mellitus Impaired glucose tolerance Obesity Metabolic syndrome Dyslipidemia Hypertension Nonalcoholic fatty liver disease (NAFLD) Claims specifying the dosage or method of administration, such as oral administration. The precise wording of each claim is critical in determining the scope of protection and potential infringement. The patent specifies numerous examples of specific compounds synthesized and tested, providing further context for the intended scope of protection. What is the therapeutic utility of the compounds disclosed in Patent 8,399,496? The therapeutic utility of the bicyclic guanylhydrazone compounds disclosed in US Patent 8,399,496 is centered on their ability to modulate GPR119 receptor activity. As agonists, they activate this receptor, leading to several beneficial physiological effects relevant to metabolic diseases. Primary Therapeutic Applications: Type 2 Diabetes Mellitus: By stimulating insulin secretion from pancreatic beta-cells in a glucose-dependent manner, these compounds can help lower blood glucose levels in individuals with type 2 diabetes. This mechanism offers an alternative or complementary approach to existing diabetes therapies. Obesity: GPR119 agonists have been shown to increase satiety, leading to reduced food intake and consequently, weight loss. They may also promote energy expenditure, further contributing to weight management. Dyslipidemia: Metabolic disorders often involve abnormal lipid profiles. By improving glucose homeostasis and potentially influencing energy balance, GPR119 agonists may indirectly benefit lipid metabolism, contributing to the treatment of dyslipidemia. Secondary Therapeutic Applications: The patent also suggests potential benefits in a broader range of metabolic and cardiovascular conditions, including: Impaired Glucose Tolerance: These compounds can help improve the body's ability to handle glucose, preventing progression to full-blown diabetes. Metabolic Syndrome: This cluster of conditions (high blood pressure, high blood sugar, unhealthy cholesterol levels, and abdominal fat) is a significant risk factor for heart disease, stroke, and diabetes. GPR119 agonists may address multiple components of metabolic syndrome. Hypertension: Emerging research suggests potential roles for GPR119 in cardiovascular regulation, including blood pressure. Nonalcoholic Fatty Liver Disease (NAFLD): Given the strong link between obesity, insulin resistance, and NAFLD, compounds that improve metabolic health are of interest for treating this condition. The development of these compounds is predicated on enhancing glucose-dependent insulin secretion and potentially promoting satiety, thereby addressing key pathophysiological mechanisms underlying these prevalent diseases. What is the competitive landscape surrounding GPR119 receptor agonists? The patent landscape for GPR119 receptor agonists is active and competitive, with several pharmaceutical companies and research institutions investing in this therapeutic area. US Patent 8,399,496, held by Merck & Co., Inc., is one of several patents protecting compounds targeting this receptor. Key Players and Their Patents: Merck & Co., Inc.: As the assignee of US Patent 8,399,496, Merck has established foundational intellectual property in bicyclic guanylhydrazone GPR119 agonists. Other Merck patents may cover related chemical scaffolds or specific drug candidates. Bristol-Myers Squibb Company: BMS has been a significant player in GPR119 research, holding patents on various classes of GPR119 agonists. For instance, US Patent 8,097,588 describes diarylpyrazole derivatives as GPR119 modulators. Glaxo Group Limited (now GlaxoSmithKline): GSK has also pursued GPR119 targets, with patents such as US Patent 7,888,314 covering specific heterocyclic compounds for treating metabolic disorders via GPR119 agonism. Takeda Pharmaceutical Company Limited: Takeda has patented compounds with GPR119 agonist activity, including those with potential applications in diabetes and obesity. For example, US Patent 8,329,725 details benzofuran derivatives as GPR119 agonists. Kissei Pharmaceutical Co., Ltd.: Kissei has patented several series of compounds targeting GPR119, such as those disclosed in US Patent 8,247,438, which describes piperidine-containing compounds. Pfizer Inc.: Pfizer has also explored GPR119 agonists, holding patents on various chemical structures designed to activate the receptor. University of Michigan: Academic institutions also contribute to the patent landscape, with some having licensed or divested early-stage GPR119 research to commercial entities. Patent Strategy and Overlap: The competitive landscape is characterized by: Diverse Chemical Scaffolds: Companies have explored and patented a wide array of chemical structures that can activate GPR119. This includes not only bicyclic guanylhydrazones but also pyrazoles, benzofurans, piperidines, and other heterocyclic systems. Claim Scope: The breadth of claims varies significantly across patents. Some patents cover broad chemical genera, while others are narrowly focused on specific compound families or even single molecules. Method of Use Claims: In addition to claiming the chemical compounds themselves, many patents include claims for methods of treating specific diseases using these compounds. This adds another layer of protection and potential for overlap. Freedom-to-Operate (FTO) Complexity: Companies developing new GPR119 agonists must conduct thorough FTO analyses to ensure their compounds and intended uses do not infringe on existing patents. This involves mapping the claims of relevant patents against the proposed product. Patent Expiry: The expiry dates of key patents are critical considerations for market entry and generic competition. Patents granted in the early to mid-2000s are beginning to expire, creating opportunities for biosimilar or generic development in the future, provided those generic products are not covered by later-expiring patents on improvements or different compounds. The ongoing research and patenting activity in the GPR119 space indicate significant commercial interest in this therapeutic target for metabolic disorders. Companies must navigate this complex IP environment carefully to secure their own market positions and avoid infringement. What are the implications of Patent 8,399,496 for R&D and investment decisions? US Patent 8,399,496, by protecting a specific class of bicyclic guanylhydrazone GPR119 agonists, has several implications for R&D and investment decisions in the pharmaceutical sector, particularly in the metabolic disease arena. For R&D Decisions: Target Identification and Validation: The patent reinforces the therapeutic relevance of the GPR119 receptor as a target for diabetes, obesity, and related metabolic disorders. This validates ongoing research efforts focused on this receptor. Chemical Space Exploration: The patent defines a specific region of chemical space (bicyclic guanylhydrazones) that is claimed. Companies exploring GPR119 agonists may need to steer clear of this particular chemical scaffold or seek licensing if their candidate compounds fall within the patent's claims. Novel Compound Design: R&D teams must design new compounds that are structurally distinct from those claimed in Patent 8,399,496 to achieve freedom to operate. This may involve exploring alternative scaffolds or modifying the existing bicyclic guanylhydrazone structure in non-infringing ways. Intellectual Property Strategy: Companies developing their own GPR119 agonists need to ensure their own patent applications are drafted to cover novel and non-obvious structural variations, therapeutic uses, or formulations that are distinct from Merck's patent. This requires careful prior art searching and claim drafting. Collaboration and Licensing: For companies with promising GPR119 candidates that might be close to Merck's patented compounds, collaboration or licensing agreements with Merck & Co., Inc. may be a necessary strategy. For Investment Decisions: Due Diligence on GPR119 Assets: Investors evaluating companies with GPR119 programs must conduct thorough due diligence on the intellectual property portfolios of those companies. This includes scrutinizing patents like 8,399,496 to understand potential FTO issues for the target company's pipeline. Risk Assessment: The existence of strong patent protection by major pharmaceutical players like Merck for specific GPR119 agonist classes represents a significant barrier to entry for new competitors. Investors need to assess the level of this barrier for any potential investment. Market Exclusivity and Competition: The patent grants Merck exclusivity for their bicyclic guanylhydrazone GPR119 agonists for a defined period. Investors should consider how this exclusivity might impact the market entry timeline and competitive positioning of other GPR119-targeting drugs. Valuation of IP Portfolios: The value of a pharmaceutical company's pipeline is heavily influenced by its IP. Patents like 8,399,496 contribute to the perceived value and defensibility of Merck's metabolic disease franchise. Investors will evaluate the strength and breadth of IP supporting any drug candidate. Timing of Investment: Understanding patent expiry dates is crucial. As patents approach expiration, the window for high-margin sales shortens, and the risk of generic competition increases. This impacts the long-term investment thesis. In summary, US Patent 8,399,496 serves as a clear indication of a protected area within the GPR119 agonist field. Both R&D efforts and investment strategies must account for this existing intellectual property to navigate the competitive landscape effectively and mitigate risks. Key Takeaways US Patent 8,399,496, granted to Merck & Co., Inc., claims bicyclic guanylhydrazone compounds as GPR119 receptor agonists. The patented compounds are developed for treating metabolic disorders, including type 2 diabetes and obesity, by enhancing insulin secretion and satiety. The patent's claims define specific chemical structures, pharmaceutical compositions, and therapeutic methods, establishing a protected intellectual property domain. The GPR119 agonist landscape is competitive, with multiple companies holding patents on diverse chemical scaffolds targeting this receptor, necessitating careful freedom-to-operate analysis. For R&D, the patent influences compound design and IP strategy, pushing for novel, non-infringing structures. For investors, the patent represents a key factor in due diligence, risk assessment, and valuation of companies developing GPR119-targeting therapies. Frequently Asked Questions What is the chemical class of compounds claimed in US Patent 8,399,496? The patent claims bicyclic guanylhydrazone compounds. What is the primary therapeutic target of the compounds in US Patent 8,399,496? The primary therapeutic target is the GPR119 receptor. What specific medical conditions are mentioned as indications for treatment with the patented compounds? The patent lists type 2 diabetes mellitus, obesity, and dyslipidemia, among others. Who is the assignee of US Patent 8,399,496? The assignee is Merck & Co., Inc. When was US Patent 8,399,496 granted? The patent was granted on March 12, 2013. Citations [1] Merck & Co., Inc. (2013, March 12). Bicyclic guanylhydrazone GPR119 agonists. U.S. Patent No. 8,399,496. Washington, DC: U.S. Patent and Trademark Office. [2] Glaxo Group Limited. (2011, February 15). Heterocyclic compounds as GPR119 modulators. U.S. Patent No. 7,888,314. Washington, DC: U.S. Patent and Trademark Office. [3] Bristol-Myers Squibb Company. (2012, July 17). Diarylpyrazole derivatives as GPR119 modulators. U.S. Patent No. 8,097,588. Washington, DC: U.S. Patent and Trademark Office. [4] Takeda Pharmaceutical Company Limited. (2012, December 11). Benzofuran derivatives as GPR119 agonists. U.S. Patent No. 8,329,725. Washington, DC: U.S. Patent and Trademark Office. [5] Kissei Pharmaceutical Co., Ltd. (2012, August 21). GPR119 agonists for treating metabolic diseases. U.S. Patent No. 8,247,438. Washington, DC: U.S. Patent and Trademark Office. More… ↓ ⤷ Start Trial

Country	Patent Number	Estimated Expiration	Supplementary Protection Certificate	SPC Country	SPC Expiration
European Patent Office	1353647	⤷ Start Trial	C300492	Netherlands	⤷ Start Trial
European Patent Office	1353647	⤷ Start Trial	91851	Luxembourg	⤷ Start Trial
European Patent Office	1353647	⤷ Start Trial	CA 2011 00021	Denmark	⤷ Start Trial
European Patent Office	1353647	⤷ Start Trial	365	Finland	⤷ Start Trial
European Patent Office	1353647	⤷ Start Trial	11C0030	France	⤷ Start Trial
European Patent Office	1353647	⤷ Start Trial	1190027-1	Sweden	⤷ Start Trial
European Patent Office	1353647	⤷ Start Trial	C01353647/01	Switzerland	⤷ Start Trial
>Country	>Patent Number	>Estimated Expiration	>Supplementary Protection Certificate	>SPC Country	>SPC Expiration

Details for Patent: 8,399,496

Summary for Patent: 8,399,496