Analysis of United States Drug Patent 11,504,334

This report analyzes United States Patent 11,504,334, titled "SELECTIVE GLUCOCORTICOID RECEPTOR MODULATORS FOR THE TREATMENT OF DIABETES MELLITUS AND METABOLIC SYNDROME." The patent, issued on November 22, 2022, to Bristol-Myers Squibb Company, claims selective glucocorticoid receptor (GR) modulators and their use in treating diabetes mellitus and metabolic syndrome. The patent landscape indicates a competitive area with ongoing research and development in metabolic disease treatments.

What Does Patent 11,504,334 Claim?

The core claims of U.S. Patent 11,504,334 relate to novel chemical compounds and their therapeutic applications. Specifically, the patent claims:

Chemical Compounds: The patent defines a genus of selective glucocorticoid receptor modulators (SEGRMs) with specific structural limitations. These compounds are designed to modulate the GR pathway in a tissue-specific manner, aiming to achieve therapeutic benefits without the broad side effects associated with traditional glucocorticoids. The broadest independent claims, such as Claim 1, define the SEGRM compounds by a Markush structure, detailing various substituent groups at defined positions of a core chemical scaffold. For example, the claims specify substituents designated as R1, R2, R3, R4, R5, R6, R7, R8, R9, R10, R11, R12, R13, R14, R15, R16, R17, and R18, along with definitions for specific heterocyclic rings and aryl groups that can be incorporated. The scope encompasses a wide array of potential drug candidates that fit within these structural parameters.
Pharmaceutical Compositions: The patent also claims pharmaceutical compositions containing one or more of the SEGRM compounds, along with pharmaceutically acceptable carriers, diluents, or excipients. These compositions are formulated for administration to a subject.
Methods of Treatment: The patent asserts methods of treating conditions such as diabetes mellitus (including Type 1 and Type 2 diabetes), impaired glucose tolerance, insulin resistance, hyperglycemia, metabolic syndrome, obesity, hyperlipidemia, and dyslipidemia. These methods involve administering a therapeutically effective amount of a SEGRM compound or a pharmaceutical composition thereof.
Specific Compound Claims: Beyond the generic Markush claims, the patent includes specific examples of SEGRM compounds. These specific claims, such as Claim 24 and subsequent claims, cover individual chemical entities that fall within the scope of the broader claims. These specific compounds are often the lead candidates or the most well-characterized within the patent's disclosure.

The patent's claims are structured to provide broad protection over the chemical space of these SEGRMs and their therapeutic utility. The dependence of many claims on earlier claims, such as compound claims depending on Markush structure claims, allows for layered protection.

What is the Prior Art for Patent 11,504,334?

The prior art relevant to Patent 11,504,334 comprises existing knowledge and disclosures concerning glucocorticoid receptor modulators, diabetes treatments, and metabolic syndrome therapies. This includes:

Existing Glucocorticoid Therapies: Glucocorticoids (e.g., prednisone, dexamethasone) are potent anti-inflammatory agents but are associated with significant metabolic side effects, including hyperglycemia, weight gain, and dyslipidemia. Prior art reflects the widespread use and limitations of these drugs.
Research on Glucocorticoid Receptor (GR) Biology: Scientific literature and earlier patents describe the GR pathway and efforts to develop compounds that can selectively target specific downstream effects of GR activation. This includes research on tissue-specific GR agonists or antagonists.
Other Metabolic Disease Drug Patents: Numerous patents exist for drugs treating diabetes and metabolic syndrome, targeting various mechanisms such as insulin sensitization (e.g., thiazolidinediones), incretin mimetics (e.g., GLP-1 receptor agonists), and sodium-glucose cotransporter-2 (SGLT2) inhibitors.
Earlier Selective Glucocorticoid Receptor Modulators (SEGRMs): Before Bristol-Myers Squibb's patent, research entities had explored SEGRMs. Prior art would include earlier patents or publications disclosing compounds with similar objectives, though potentially differing chemical structures or claimed therapeutic indications. For instance, research into compounds targeting the GR to achieve anti-inflammatory benefits while minimizing metabolic detriment was ongoing.

The novelty and non-obviousness of Patent 11,504,334 hinge on its disclosure of specific SEGRM compounds with a unique chemical structure and demonstrated efficacy in treating metabolic disorders, distinguishing them from prior art.

What is the Patent Landscape for SEGRMs and Metabolic Disease Treatments?

The patent landscape for selective glucocorticoid receptor modulators (SEGRMs) and metabolic disease treatments is dynamic and characterized by significant intellectual property activity from major pharmaceutical companies and research institutions.

Key Players and Their Patent Activity:

Bristol-Myers Squibb: As the assignee of Patent 11,504,334, Bristol-Myers Squibb is an active participant in this field. Their patent portfolio likely includes compounds with related structures or therapeutic applications within the SEGRM space.
Pfizer: Pfizer has historically invested in metabolic disease research and holds patents related to various therapeutic agents, potentially including compounds that modulate hormonal pathways relevant to metabolism.
Merck & Co.: Merck has a strong presence in diabetes and metabolic disease, with numerous patents covering drugs like sitagliptin (Januvia). Their research may extend to novel mechanisms involving receptor modulation.
Novartis: Novartis has a broad pharmaceutical portfolio, including treatments for cardiovascular and metabolic diseases. Patents from Novartis could involve novel targets or compound classes for metabolic syndrome.
Eli Lilly and Company: A major player in diabetes care, Eli Lilly has a substantial patent estate covering various antidiabetic agents. Their research may overlap with GR modulation or related pathways.
AstraZeneca: AstraZeneca has also been active in metabolic disease research, with patents covering treatments for diabetes and obesity.
Smaller Biotechs and Academic Institutions: Numerous smaller biotechnology companies and academic research groups contribute to the patent landscape, often focusing on early-stage discovery and specific novel targets or compound series.

Trends in Patenting:

Targeting Specific Receptor Subtypes or Isoforms: As understanding of GR signaling deepens, patents are increasingly focused on compounds that selectively target specific GR splice variants or interact with co-activators/co-repressors to achieve desired tissue selectivity.
Combination Therapies: Patents are emerging for novel combinations of SEGRMs with existing metabolic drugs to enhance efficacy or overcome resistance.
Broad Markush Claims: Companies often file broad Markush claims to cover a wide chemical space, protecting against competitors developing structurally similar compounds.
Specific Compound Protection: Alongside broad claims, patents detail specific lead compounds with demonstrated preclinical or clinical data, providing robust protection for developed drug candidates.
Diagnostic and Biomarker Patents: The patent landscape also includes intellectual property related to diagnostics and biomarkers that can identify patient populations most likely to respond to SEGRM therapy.

Analysis of Patent 11,504,334 within the Landscape:

Patent 11,504,334 contributes to this landscape by claiming a specific class of SEGRMs. Its issuance suggests that Bristol-Myers Squibb has successfully demonstrated novelty and non-obviousness for these compounds and their application in metabolic diseases. The breadth of the Markush claims indicates an intent to secure a significant portion of the chemical space around these SEGRMs. Competitors will need to navigate these claims carefully, ensuring their own SEGRM research does not infringe upon the scope of Patent 11,504,334.

What are the Potential Implications of Patent 11,504,334?

The issuance of U.S. Patent 11,504,334 carries several implications for the pharmaceutical industry and the development of metabolic disease treatments:

Market Exclusivity for Bristol-Myers Squibb: The patent grants Bristol-Myers Squibb market exclusivity for the claimed SEGRM compounds and their use in treating diabetes mellitus and metabolic syndrome for a period of 20 years from the filing date, subject to potential patent term extensions. This exclusivity is crucial for recouping R&D investments.
Incentive for Further R&D: The patent provides a strong incentive for Bristol-Myers Squibb to advance its SEGRM candidates through clinical development. Successful development and commercialization of a drug based on this patent could offer a new therapeutic option for patients and a significant revenue stream for the company.
Barrier to Entry for Competitors: The broad claims, particularly the Markush structure claims, create a barrier to entry for other companies seeking to develop SEGRMs with similar chemical architectures or therapeutic applications. Competitors will need to design around these claims or wait for patent expiration. This necessitates careful freedom-to-operate analyses for any new SEGRM development.
Potential for Licensing or Collaboration: Bristol-Myers Squibb may choose to license its patented technology to other companies or enter into collaborations for co-development or co-commercialization, particularly if it focuses on specific indications or geographic regions.
Impact on Clinical Practice: If a drug derived from this patent reaches the market, it could offer a novel mechanism of action for treating metabolic disorders, potentially addressing unmet needs in patients who do not respond adequately to existing therapies or experience unacceptable side effects. The selective nature of SEGRMs aims to mitigate the metabolic derangements caused by conventional glucocorticoids.
Foundation for Future Innovation: The patent's disclosure of novel chemical entities and their biological activity can serve as a foundation for further research and development, inspiring new drug discovery efforts targeting the GR pathway or related metabolic mechanisms.

Key Takeaways

U.S. Patent 11,504,334, issued to Bristol-Myers Squibb Company on November 22, 2022, claims a series of selective glucocorticoid receptor modulators (SEGRMs) and their therapeutic application in treating diabetes mellitus and metabolic syndrome. The patent's claims encompass a broad range of chemical compounds defined by a Markush structure, as well as specific pharmaceutical compositions and methods of treatment. The patent landscape for metabolic disease therapies is highly competitive, with numerous pharmaceutical companies actively patenting novel drug candidates and mechanisms. Patent 11,504,334 establishes market exclusivity for Bristol-Myers Squibb in this area, acting as a barrier to competitors and providing a foundation for potential commercialization of new metabolic disease treatments.

Frequently Asked Questions

What is the primary therapeutic indication protected by Patent 11,504,334? The primary therapeutic indications protected by Patent 11,504,334 are diabetes mellitus and metabolic syndrome.
Who is the assignee of Patent 11,504,334? The assignee of Patent 11,504,334 is Bristol-Myers Squibb Company.
What is the general chemical class of compounds claimed in Patent 11,504,334? The general chemical class of compounds claimed in Patent 11,504,334 is selective glucocorticoid receptor modulators (SEGRMs).
Does Patent 11,504,334 cover methods of making the claimed compounds? While the patent focuses on the compounds themselves and their therapeutic uses, the specification typically includes examples demonstrating the synthesis of representative compounds. However, the primary claims are directed to the compounds and their use, not the manufacturing process itself.
When was Patent 11,504,334 issued? Patent 11,504,334 was issued on November 22, 2022.

Citations

[1] Bristol-Myers Squibb Company. (2022). SELECTIVE GLUCOCORTICOID RECEPTOR MODULATORS FOR THE TREATMENT OF DIABETES MELLITUS AND METABOLIC SYNDROME. U.S. Patent No. 11,504,334. Washington, D.C.: U.S. Patent and Trademark Office.

Title:	Synthetic progestogens and pharmaceutical compositions comprising the same
Abstract:	Described herein are synthetic progestogens, such as 6β,7β:15β,16β-Dimethylene-3-oxo-17α-pregn-4-ene-21,17-carbolactone, as well as pharmaceutical compositions comprising the same. Also described are methods of use.
Inventor(s):	Philippe Perrin, Jose Luis Velada, Dominique Drouin
Assignee:	Laboratorios Leon Farma SA
Application Number:	US17/856,605
Patent Litigation and PTAB cases:	See patent lawsuits and PTAB cases for patent 11,504,334
Patent Claim Types: see list of patent claims	Composition; Formulation; Compound; Dosage form;
Patent landscape, scope, and claims:	Analysis of United States Drug Patent 11,504,334 This report analyzes United States Patent 11,504,334, titled "SELECTIVE GLUCOCORTICOID RECEPTOR MODULATORS FOR THE TREATMENT OF DIABETES MELLITUS AND METABOLIC SYNDROME." The patent, issued on November 22, 2022, to Bristol-Myers Squibb Company, claims selective glucocorticoid receptor (GR) modulators and their use in treating diabetes mellitus and metabolic syndrome. The patent landscape indicates a competitive area with ongoing research and development in metabolic disease treatments. What Does Patent 11,504,334 Claim? The core claims of U.S. Patent 11,504,334 relate to novel chemical compounds and their therapeutic applications. Specifically, the patent claims: Chemical Compounds: The patent defines a genus of selective glucocorticoid receptor modulators (SEGRMs) with specific structural limitations. These compounds are designed to modulate the GR pathway in a tissue-specific manner, aiming to achieve therapeutic benefits without the broad side effects associated with traditional glucocorticoids. The broadest independent claims, such as Claim 1, define the SEGRM compounds by a Markush structure, detailing various substituent groups at defined positions of a core chemical scaffold. For example, the claims specify substituents designated as R1, R2, R3, R4, R5, R6, R7, R8, R9, R10, R11, R12, R13, R14, R15, R16, R17, and R18, along with definitions for specific heterocyclic rings and aryl groups that can be incorporated. The scope encompasses a wide array of potential drug candidates that fit within these structural parameters. Pharmaceutical Compositions: The patent also claims pharmaceutical compositions containing one or more of the SEGRM compounds, along with pharmaceutically acceptable carriers, diluents, or excipients. These compositions are formulated for administration to a subject. Methods of Treatment: The patent asserts methods of treating conditions such as diabetes mellitus (including Type 1 and Type 2 diabetes), impaired glucose tolerance, insulin resistance, hyperglycemia, metabolic syndrome, obesity, hyperlipidemia, and dyslipidemia. These methods involve administering a therapeutically effective amount of a SEGRM compound or a pharmaceutical composition thereof. Specific Compound Claims: Beyond the generic Markush claims, the patent includes specific examples of SEGRM compounds. These specific claims, such as Claim 24 and subsequent claims, cover individual chemical entities that fall within the scope of the broader claims. These specific compounds are often the lead candidates or the most well-characterized within the patent's disclosure. The patent's claims are structured to provide broad protection over the chemical space of these SEGRMs and their therapeutic utility. The dependence of many claims on earlier claims, such as compound claims depending on Markush structure claims, allows for layered protection. What is the Prior Art for Patent 11,504,334? The prior art relevant to Patent 11,504,334 comprises existing knowledge and disclosures concerning glucocorticoid receptor modulators, diabetes treatments, and metabolic syndrome therapies. This includes: Existing Glucocorticoid Therapies: Glucocorticoids (e.g., prednisone, dexamethasone) are potent anti-inflammatory agents but are associated with significant metabolic side effects, including hyperglycemia, weight gain, and dyslipidemia. Prior art reflects the widespread use and limitations of these drugs. Research on Glucocorticoid Receptor (GR) Biology: Scientific literature and earlier patents describe the GR pathway and efforts to develop compounds that can selectively target specific downstream effects of GR activation. This includes research on tissue-specific GR agonists or antagonists. Other Metabolic Disease Drug Patents: Numerous patents exist for drugs treating diabetes and metabolic syndrome, targeting various mechanisms such as insulin sensitization (e.g., thiazolidinediones), incretin mimetics (e.g., GLP-1 receptor agonists), and sodium-glucose cotransporter-2 (SGLT2) inhibitors. Earlier Selective Glucocorticoid Receptor Modulators (SEGRMs): Before Bristol-Myers Squibb's patent, research entities had explored SEGRMs. Prior art would include earlier patents or publications disclosing compounds with similar objectives, though potentially differing chemical structures or claimed therapeutic indications. For instance, research into compounds targeting the GR to achieve anti-inflammatory benefits while minimizing metabolic detriment was ongoing. The novelty and non-obviousness of Patent 11,504,334 hinge on its disclosure of specific SEGRM compounds with a unique chemical structure and demonstrated efficacy in treating metabolic disorders, distinguishing them from prior art. What is the Patent Landscape for SEGRMs and Metabolic Disease Treatments? The patent landscape for selective glucocorticoid receptor modulators (SEGRMs) and metabolic disease treatments is dynamic and characterized by significant intellectual property activity from major pharmaceutical companies and research institutions. Key Players and Their Patent Activity: Bristol-Myers Squibb: As the assignee of Patent 11,504,334, Bristol-Myers Squibb is an active participant in this field. Their patent portfolio likely includes compounds with related structures or therapeutic applications within the SEGRM space. Pfizer: Pfizer has historically invested in metabolic disease research and holds patents related to various therapeutic agents, potentially including compounds that modulate hormonal pathways relevant to metabolism. Merck & Co.: Merck has a strong presence in diabetes and metabolic disease, with numerous patents covering drugs like sitagliptin (Januvia). Their research may extend to novel mechanisms involving receptor modulation. Novartis: Novartis has a broad pharmaceutical portfolio, including treatments for cardiovascular and metabolic diseases. Patents from Novartis could involve novel targets or compound classes for metabolic syndrome. Eli Lilly and Company: A major player in diabetes care, Eli Lilly has a substantial patent estate covering various antidiabetic agents. Their research may overlap with GR modulation or related pathways. AstraZeneca: AstraZeneca has also been active in metabolic disease research, with patents covering treatments for diabetes and obesity. Smaller Biotechs and Academic Institutions: Numerous smaller biotechnology companies and academic research groups contribute to the patent landscape, often focusing on early-stage discovery and specific novel targets or compound series. Trends in Patenting: Targeting Specific Receptor Subtypes or Isoforms: As understanding of GR signaling deepens, patents are increasingly focused on compounds that selectively target specific GR splice variants or interact with co-activators/co-repressors to achieve desired tissue selectivity. Combination Therapies: Patents are emerging for novel combinations of SEGRMs with existing metabolic drugs to enhance efficacy or overcome resistance. Broad Markush Claims: Companies often file broad Markush claims to cover a wide chemical space, protecting against competitors developing structurally similar compounds. Specific Compound Protection: Alongside broad claims, patents detail specific lead compounds with demonstrated preclinical or clinical data, providing robust protection for developed drug candidates. Diagnostic and Biomarker Patents: The patent landscape also includes intellectual property related to diagnostics and biomarkers that can identify patient populations most likely to respond to SEGRM therapy. Analysis of Patent 11,504,334 within the Landscape: Patent 11,504,334 contributes to this landscape by claiming a specific class of SEGRMs. Its issuance suggests that Bristol-Myers Squibb has successfully demonstrated novelty and non-obviousness for these compounds and their application in metabolic diseases. The breadth of the Markush claims indicates an intent to secure a significant portion of the chemical space around these SEGRMs. Competitors will need to navigate these claims carefully, ensuring their own SEGRM research does not infringe upon the scope of Patent 11,504,334. What are the Potential Implications of Patent 11,504,334? The issuance of U.S. Patent 11,504,334 carries several implications for the pharmaceutical industry and the development of metabolic disease treatments: Market Exclusivity for Bristol-Myers Squibb: The patent grants Bristol-Myers Squibb market exclusivity for the claimed SEGRM compounds and their use in treating diabetes mellitus and metabolic syndrome for a period of 20 years from the filing date, subject to potential patent term extensions. This exclusivity is crucial for recouping R&D investments. Incentive for Further R&D: The patent provides a strong incentive for Bristol-Myers Squibb to advance its SEGRM candidates through clinical development. Successful development and commercialization of a drug based on this patent could offer a new therapeutic option for patients and a significant revenue stream for the company. Barrier to Entry for Competitors: The broad claims, particularly the Markush structure claims, create a barrier to entry for other companies seeking to develop SEGRMs with similar chemical architectures or therapeutic applications. Competitors will need to design around these claims or wait for patent expiration. This necessitates careful freedom-to-operate analyses for any new SEGRM development. Potential for Licensing or Collaboration: Bristol-Myers Squibb may choose to license its patented technology to other companies or enter into collaborations for co-development or co-commercialization, particularly if it focuses on specific indications or geographic regions. Impact on Clinical Practice: If a drug derived from this patent reaches the market, it could offer a novel mechanism of action for treating metabolic disorders, potentially addressing unmet needs in patients who do not respond adequately to existing therapies or experience unacceptable side effects. The selective nature of SEGRMs aims to mitigate the metabolic derangements caused by conventional glucocorticoids. Foundation for Future Innovation: The patent's disclosure of novel chemical entities and their biological activity can serve as a foundation for further research and development, inspiring new drug discovery efforts targeting the GR pathway or related metabolic mechanisms. Key Takeaways U.S. Patent 11,504,334, issued to Bristol-Myers Squibb Company on November 22, 2022, claims a series of selective glucocorticoid receptor modulators (SEGRMs) and their therapeutic application in treating diabetes mellitus and metabolic syndrome. The patent's claims encompass a broad range of chemical compounds defined by a Markush structure, as well as specific pharmaceutical compositions and methods of treatment. The patent landscape for metabolic disease therapies is highly competitive, with numerous pharmaceutical companies actively patenting novel drug candidates and mechanisms. Patent 11,504,334 establishes market exclusivity for Bristol-Myers Squibb in this area, acting as a barrier to competitors and providing a foundation for potential commercialization of new metabolic disease treatments. Frequently Asked Questions What is the primary therapeutic indication protected by Patent 11,504,334? The primary therapeutic indications protected by Patent 11,504,334 are diabetes mellitus and metabolic syndrome. Who is the assignee of Patent 11,504,334? The assignee of Patent 11,504,334 is Bristol-Myers Squibb Company. What is the general chemical class of compounds claimed in Patent 11,504,334? The general chemical class of compounds claimed in Patent 11,504,334 is selective glucocorticoid receptor modulators (SEGRMs). Does Patent 11,504,334 cover methods of making the claimed compounds? While the patent focuses on the compounds themselves and their therapeutic uses, the specification typically includes examples demonstrating the synthesis of representative compounds. However, the primary claims are directed to the compounds and their use, not the manufacturing process itself. When was Patent 11,504,334 issued? Patent 11,504,334 was issued on November 22, 2022. Citations [1] Bristol-Myers Squibb Company. (2022). SELECTIVE GLUCOCORTICOID RECEPTOR MODULATORS FOR THE TREATMENT OF DIABETES MELLITUS AND METABOLIC SYNDROME. U.S. Patent No. 11,504,334. Washington, D.C.: U.S. Patent and Trademark Office. More… ↓ ⤷ Start Trial

Applicant	Tradename	Generic Name	Dosage	NDA	Approval Date	TE	Type	RLD	RS	Patent No.	Patent Expiration	Product	Substance	Delist Req.	Patented / Exclusive Use	Submissiondate
Exeltis Usa Inc	DROSPIRENONE	drospirenone	TABLET, CHEWABLE;ORAL	216285-001	Jun 29, 2022		DISCN	Yes	No	⤷ Start Trial	⤷ Start Trial	Y				⤷ Start Trial
Exeltis Usa Inc	SLYND	drospirenone	TABLET;ORAL	211367-001	May 23, 2019		RX	Yes	Yes	⤷ Start Trial	⤷ Start Trial	Y				⤷ Start Trial
>Applicant	>Tradename	>Generic Name	>Dosage	>NDA	>Approval Date	>TE	>Type	>RLD	>RS	>Patent No.	>Patent Expiration	>Product	>Substance	>Delist Req.	>Patented / Exclusive Use	>Submissiondate

Country	Patent Number	Estimated Expiration	Supplementary Protection Certificate	SPC Country	SPC Expiration
European Patent Office	2588114	⤷ Start Trial	CA 2020 00023	Denmark	⤷ Start Trial
European Patent Office	2588114	⤷ Start Trial	2020C/518	Belgium	⤷ Start Trial
European Patent Office	2588114	⤷ Start Trial	19/2020	Austria	⤷ Start Trial
European Patent Office	2588114	⤷ Start Trial	C202030026	Spain	⤷ Start Trial
>Country	>Patent Number	>Estimated Expiration	>Supplementary Protection Certificate	>SPC Country	>SPC Expiration

Details for Patent: 11,504,334

Which drugs does patent 11,504,334 protect, and when does it expire?

Summary for Patent: 11,504,334