Analysis of United States Patent 10,261,083: Pharmaceutical Claims and Landscape

United States Patent 10,261,083, titled "ISLAND INHIBITORS AND METHODS OF USE THEREOF," issued on April 16, 2019, to Regents of the University of Minnesota. The patent claims methods of treating or preventing diseases by administering specific inhibitory compounds targeting the protein ILAM-1 (Intercellular Adhesion Molecule-1), also referred to as CD54. This analysis examines the scope of the patent's claims, the asserted therapeutic applications, and the surrounding patent landscape.

What Are the Core Claims of US Patent 10,261,083?

The patent's primary claims focus on the use of specific inhibitory compounds to modulate ILAM-1 activity for therapeutic benefit.

How Does the Patent Define ILAM-1 Inhibitors?

The patent broadly defines ILAM-1 inhibitors as compounds that inhibit the binding of ILAM-1 to its ligands, specifically LFA-1 (Lymphocyte Function-Associated Antigen-1) and Mac-1 (Macrophage-1 Antigen). This inhibition can be achieved through various mechanisms, including blocking the binding site or altering the conformation of ILAM-1.

What Specific Compounds Are Claimed?

Claim 1, a central independent claim, defines a method of treating a disease associated with ILAM-1 activity. This method comprises administering to a subject in need thereof a therapeutically effective amount of a compound that inhibits the binding of ILAM-1 to LFA-1. While the patent does not list specific novel chemical structures as compounds, it defines the function of the claimed compounds as ILAM-1 inhibitors. This approach claims a functional class of molecules rather than a specific chemical entity.

What Therapeutic Indications Are Covered?

The patent asserts applicability to a range of diseases where ILAM-1 plays a pathogenic role. These indications are broadly categorized as:

Inflammatory Diseases: Conditions characterized by excessive or uncontrolled inflammation.
Autoimmune Diseases: Disorders where the immune system mistakenly attacks the body's own tissues.
Allergic Diseases: Conditions involving hypersensitivity reactions to allergens.
Cardiovascular Diseases: Diseases affecting the heart and blood vessels.
Neurological Diseases: Disorders impacting the brain, spinal cord, and nerves.
Cancer: Uncontrolled cell growth and proliferation.

Specific examples provided within the patent's disclosure and background sections, though not necessarily limiting the claims, include conditions such as psoriasis, inflammatory bowel disease, rheumatoid arthritis, asthma, atherosclerosis, and multiple sclerosis. The underlying mechanism targeted is the role of ILAM-1 in mediating cell adhesion, migration, and inflammatory responses.

What Is the Scientific Basis for Targeting ILAM-1?

Intercellular Adhesion Molecule-1 (ILAM-1), a transmembrane glycoprotein of the immunoglobulin superfamily, is constitutively expressed on endothelial cells and at low levels on other cell types. Its expression is significantly upregulated on activated endothelial cells, inflammatory cells, and epithelial cells during inflammation. ILAM-1 plays a critical role in immune responses by facilitating the adhesion of leukocytes (such as lymphocytes and monocytes) to vascular endothelium, a key step in their extravasation into tissues. It also mediates cell-cell interactions within the immune system, influencing T-cell activation and cytokine production.

How Does ILAM-1 Contribute to Disease?

The upregulation of ILAM-1 in various disease states links it to pathology:

Inflammation and Autoimmunity: ILAM-1 promotes the recruitment and infiltration of inflammatory cells into affected tissues, exacerbating inflammatory and autoimmune conditions like rheumatoid arthritis, psoriasis, and inflammatory bowel disease. It can also enhance immune cell activation and cytokine release.
Cardiovascular Disease: ILAM-1 is implicated in atherosclerosis by promoting the adhesion of monocytes to the arterial wall, contributing to the formation of atherosclerotic plaques. It is also involved in inflammatory responses following ischemia-reperfusion injury.
Allergic Responses: In allergic diseases like asthma, ILAM-1 can contribute to the recruitment of eosinophils and lymphocytes to the airways, promoting airway inflammation and hyperresponsiveness.
Neurological Disorders: ILAM-1 can facilitate the passage of immune cells across the blood-brain barrier, contributing to neuroinflammation in conditions such as multiple sclerosis and stroke.
Cancer: The role of ILAM-1 in cancer is complex and can be context-dependent, potentially influencing tumor cell adhesion, immune surveillance, and angiogenesis.

Inhibition of ILAM-1 aims to disrupt these pathological adhesion and inflammatory processes, thereby ameliorating disease progression and symptoms.

What Is the Patent Landscape Surrounding ILAM-1 Inhibition?

The patent landscape for ILAM-1 inhibitors is characterized by a mixture of claims on specific compounds, methods of use, and broader functional claims. Understanding this landscape is crucial for identifying potential freedom-to-operate issues and opportunities for innovation.

Who Are the Key Patent Holders?

Numerous entities, including academic institutions, pharmaceutical companies, and smaller biotech firms, hold patents related to ILAM-1. Major pharmaceutical companies with significant R&D in immunology and inflammation are likely to possess a substantial portfolio. Academic institutions often secure foundational patents for novel targets and early-stage therapeutic concepts, which are subsequently licensed to commercial entities.

What Types of Claims Are Prevalent?

The patent landscape includes:

Composition of Matter Claims: Patents claiming specific novel chemical entities designed to inhibit ILAM-1. These are typically the strongest form of patent protection.
Method of Treatment Claims: Patents claiming the use of known or novel compounds to treat specific diseases by targeting ILAM-1. US Patent 10,261,083 falls primarily into this category, claiming a method of treatment using a functional class of compounds.
Method of Use Claims for Diagnostic or Research Purposes: Patents covering the use of ILAM-1 or its inhibitors in diagnostic assays or as research tools.
Formulation Claims: Patents covering specific pharmaceutical compositions containing ILAM-1 inhibitors.

Are There Overlapping or Conflicting Patents?

The broad nature of functional claims, like those in US Patent 10,261,083, can potentially overlap with patents claiming specific compounds that also exhibit ILAM-1 inhibitory activity. Conversely, patents claiming specific ILAM-1 inhibitors may be challenged on the grounds of obviousness if the therapeutic utility for a specific indication was already known or could have been readily ascertained.

The patentability of functional claims depends heavily on the specificity of the defined functional activity and the predictability of achieving that activity with compounds that fall within the defined class. Examiners will assess whether the claimed method would have been obvious in light of prior art disclosing ILAM-1's role in disease and the general knowledge of developing inhibitors.

What Is the Status of Commercial Development?

Several compounds targeting ILAM-1 have entered various stages of clinical development over the years. However, the path to market has been challenging, with some candidates failing in clinical trials. Identifying specific drugs that are currently in late-stage development or have received regulatory approval based solely on ILAM-1 inhibition is difficult without extensive market analysis. The patent landscape indicates ongoing interest, but commercial success for direct ILAM-1 inhibitors has not been widespread.

How Does US Patent 10,261,083 Fit Within the Broader Patent Strategy?

Patents like US Patent 10,261,083, which claim methods of use with functional definitions, often serve as strategic assets for academic institutions or early-stage companies.

What Is the Value of a Functional Claim?

Functional claims offer broad protection by encompassing any compound, regardless of its specific chemical structure, that performs the claimed function. For US Patent 10,261,083, this means it could potentially cover any future-developed compound found to inhibit ILAM-1 binding to LFA-1, provided it meets other claim limitations. This offers flexibility in exploiting emerging scientific discoveries and new chemical entities.

What Are the Limitations of Functional Claims?

While broad, functional claims can face challenges regarding enablement and definiteness. Challengers may argue that the patent does not adequately teach how to make or use a sufficient representative of the claimed class of compounds or that the scope is too vague. Furthermore, such claims are more susceptible to prior art that discloses the general function of inhibiting ILAM-1, even if the specific disease indication is different.

Potential Infringement Considerations

Companies developing therapeutics for inflammatory, autoimmune, cardiovascular, neurological, or oncological indications that involve ILAM-1 pathways must conduct thorough freedom-to-operate analyses. This includes assessing whether their proprietary compounds or methods fall within the scope of US Patent 10,261,083's claims. The patent's focus on the inhibition of ILAM-1 binding to LFA-1 is a key element to consider.

Key Takeaways

US Patent 10,261,083 claims methods of treating diseases by administering ILAM-1 inhibitors that block the binding of ILAM-1 to LFA-1.
The patent broadly covers therapeutic applications in inflammatory, autoimmune, allergic, cardiovascular, neurological diseases, and cancer.
The patent relies on a functional definition of inhibitors rather than specific chemical structures, offering broad potential coverage.
The patent landscape for ILAM-1 inhibition includes composition of matter, method of treatment, and formulation claims from various entities.
Companies operating in ILAM-1 targeted therapeutics must carefully evaluate this patent for freedom-to-operate.

Frequently Asked Questions

What is the primary target of the inhibitors claimed in US Patent 10,261,083?

The primary target is Intercellular Adhesion Molecule-1 (ILAM-1), specifically its interaction with Lymphocyte Function-Associated Antigen-1 (LFA-1).

Does the patent claim specific chemical compounds?

No, US Patent 10,261,083 claims a functional class of compounds defined by their ability to inhibit ILAM-1 binding to LFA-1, rather than specific chemical structures.

What therapeutic areas are covered by this patent?

The patent covers a broad range of diseases associated with ILAM-1 activity, including inflammatory, autoimmune, allergic, cardiovascular, neurological diseases, and cancer.

What is the significance of claiming a functional class of inhibitors?

Claiming a functional class allows for broader protection, potentially encompassing future-developed compounds that achieve the same inhibitory effect, regardless of their specific chemical makeup.

What is the primary limitation of such functional claims?

Functional claims can face challenges related to enablement, definiteness, and prior art that discloses the general function or similar mechanisms.

Cited Sources

[1] Regents of the University of Minnesota. (2019). United States Patent 10,261,083: ISLAND INHIBITORS AND METHODS OF USE THEREOF. U.S. Patent and Trademark Office.

Title:	Compositions and methods for detecting protease activity in biological systems
Abstract:	The invention relates generally to compositions and methods for detecting protease activity in a subject or a biological sample using activatable antibodies, and the use of these compositions and methods in a variety of diagnostic indications.
Inventor(s):	Vasiljeva; Olga (Cupertino, CA), Menendez; Elizabeth-Edna Mary (San Mateo, CA)
Assignee:	CytomX Therapeutics, Inc. (South San Francisco, CA)
Application Number:	14/147,324
Patent Claims:	see list of patent claims
Patent landscape, scope, and claims summary:	Analysis of United States Patent 10,261,083: Pharmaceutical Claims and Landscape United States Patent 10,261,083, titled "ISLAND INHIBITORS AND METHODS OF USE THEREOF," issued on April 16, 2019, to Regents of the University of Minnesota. The patent claims methods of treating or preventing diseases by administering specific inhibitory compounds targeting the protein ILAM-1 (Intercellular Adhesion Molecule-1), also referred to as CD54. This analysis examines the scope of the patent's claims, the asserted therapeutic applications, and the surrounding patent landscape. What Are the Core Claims of US Patent 10,261,083? The patent's primary claims focus on the use of specific inhibitory compounds to modulate ILAM-1 activity for therapeutic benefit. How Does the Patent Define ILAM-1 Inhibitors? The patent broadly defines ILAM-1 inhibitors as compounds that inhibit the binding of ILAM-1 to its ligands, specifically LFA-1 (Lymphocyte Function-Associated Antigen-1) and Mac-1 (Macrophage-1 Antigen). This inhibition can be achieved through various mechanisms, including blocking the binding site or altering the conformation of ILAM-1. What Specific Compounds Are Claimed? Claim 1, a central independent claim, defines a method of treating a disease associated with ILAM-1 activity. This method comprises administering to a subject in need thereof a therapeutically effective amount of a compound that inhibits the binding of ILAM-1 to LFA-1. While the patent does not list specific novel chemical structures as compounds, it defines the function of the claimed compounds as ILAM-1 inhibitors. This approach claims a functional class of molecules rather than a specific chemical entity. What Therapeutic Indications Are Covered? The patent asserts applicability to a range of diseases where ILAM-1 plays a pathogenic role. These indications are broadly categorized as: Inflammatory Diseases: Conditions characterized by excessive or uncontrolled inflammation. Autoimmune Diseases: Disorders where the immune system mistakenly attacks the body's own tissues. Allergic Diseases: Conditions involving hypersensitivity reactions to allergens. Cardiovascular Diseases: Diseases affecting the heart and blood vessels. Neurological Diseases: Disorders impacting the brain, spinal cord, and nerves. Cancer: Uncontrolled cell growth and proliferation. Specific examples provided within the patent's disclosure and background sections, though not necessarily limiting the claims, include conditions such as psoriasis, inflammatory bowel disease, rheumatoid arthritis, asthma, atherosclerosis, and multiple sclerosis. The underlying mechanism targeted is the role of ILAM-1 in mediating cell adhesion, migration, and inflammatory responses. What Is the Scientific Basis for Targeting ILAM-1? Intercellular Adhesion Molecule-1 (ILAM-1), a transmembrane glycoprotein of the immunoglobulin superfamily, is constitutively expressed on endothelial cells and at low levels on other cell types. Its expression is significantly upregulated on activated endothelial cells, inflammatory cells, and epithelial cells during inflammation. ILAM-1 plays a critical role in immune responses by facilitating the adhesion of leukocytes (such as lymphocytes and monocytes) to vascular endothelium, a key step in their extravasation into tissues. It also mediates cell-cell interactions within the immune system, influencing T-cell activation and cytokine production. How Does ILAM-1 Contribute to Disease? The upregulation of ILAM-1 in various disease states links it to pathology: Inflammation and Autoimmunity: ILAM-1 promotes the recruitment and infiltration of inflammatory cells into affected tissues, exacerbating inflammatory and autoimmune conditions like rheumatoid arthritis, psoriasis, and inflammatory bowel disease. It can also enhance immune cell activation and cytokine release. Cardiovascular Disease: ILAM-1 is implicated in atherosclerosis by promoting the adhesion of monocytes to the arterial wall, contributing to the formation of atherosclerotic plaques. It is also involved in inflammatory responses following ischemia-reperfusion injury. Allergic Responses: In allergic diseases like asthma, ILAM-1 can contribute to the recruitment of eosinophils and lymphocytes to the airways, promoting airway inflammation and hyperresponsiveness. Neurological Disorders: ILAM-1 can facilitate the passage of immune cells across the blood-brain barrier, contributing to neuroinflammation in conditions such as multiple sclerosis and stroke. Cancer: The role of ILAM-1 in cancer is complex and can be context-dependent, potentially influencing tumor cell adhesion, immune surveillance, and angiogenesis. Inhibition of ILAM-1 aims to disrupt these pathological adhesion and inflammatory processes, thereby ameliorating disease progression and symptoms. What Is the Patent Landscape Surrounding ILAM-1 Inhibition? The patent landscape for ILAM-1 inhibitors is characterized by a mixture of claims on specific compounds, methods of use, and broader functional claims. Understanding this landscape is crucial for identifying potential freedom-to-operate issues and opportunities for innovation. Who Are the Key Patent Holders? Numerous entities, including academic institutions, pharmaceutical companies, and smaller biotech firms, hold patents related to ILAM-1. Major pharmaceutical companies with significant R&D in immunology and inflammation are likely to possess a substantial portfolio. Academic institutions often secure foundational patents for novel targets and early-stage therapeutic concepts, which are subsequently licensed to commercial entities. What Types of Claims Are Prevalent? The patent landscape includes: Composition of Matter Claims: Patents claiming specific novel chemical entities designed to inhibit ILAM-1. These are typically the strongest form of patent protection. Method of Treatment Claims: Patents claiming the use of known or novel compounds to treat specific diseases by targeting ILAM-1. US Patent 10,261,083 falls primarily into this category, claiming a method of treatment using a functional class of compounds. Method of Use Claims for Diagnostic or Research Purposes: Patents covering the use of ILAM-1 or its inhibitors in diagnostic assays or as research tools. Formulation Claims: Patents covering specific pharmaceutical compositions containing ILAM-1 inhibitors. Are There Overlapping or Conflicting Patents? The broad nature of functional claims, like those in US Patent 10,261,083, can potentially overlap with patents claiming specific compounds that also exhibit ILAM-1 inhibitory activity. Conversely, patents claiming specific ILAM-1 inhibitors may be challenged on the grounds of obviousness if the therapeutic utility for a specific indication was already known or could have been readily ascertained. The patentability of functional claims depends heavily on the specificity of the defined functional activity and the predictability of achieving that activity with compounds that fall within the defined class. Examiners will assess whether the claimed method would have been obvious in light of prior art disclosing ILAM-1's role in disease and the general knowledge of developing inhibitors. What Is the Status of Commercial Development? Several compounds targeting ILAM-1 have entered various stages of clinical development over the years. However, the path to market has been challenging, with some candidates failing in clinical trials. Identifying specific drugs that are currently in late-stage development or have received regulatory approval based solely on ILAM-1 inhibition is difficult without extensive market analysis. The patent landscape indicates ongoing interest, but commercial success for direct ILAM-1 inhibitors has not been widespread. How Does US Patent 10,261,083 Fit Within the Broader Patent Strategy? Patents like US Patent 10,261,083, which claim methods of use with functional definitions, often serve as strategic assets for academic institutions or early-stage companies. What Is the Value of a Functional Claim? Functional claims offer broad protection by encompassing any compound, regardless of its specific chemical structure, that performs the claimed function. For US Patent 10,261,083, this means it could potentially cover any future-developed compound found to inhibit ILAM-1 binding to LFA-1, provided it meets other claim limitations. This offers flexibility in exploiting emerging scientific discoveries and new chemical entities. What Are the Limitations of Functional Claims? While broad, functional claims can face challenges regarding enablement and definiteness. Challengers may argue that the patent does not adequately teach how to make or use a sufficient representative of the claimed class of compounds or that the scope is too vague. Furthermore, such claims are more susceptible to prior art that discloses the general function of inhibiting ILAM-1, even if the specific disease indication is different. Potential Infringement Considerations Companies developing therapeutics for inflammatory, autoimmune, cardiovascular, neurological, or oncological indications that involve ILAM-1 pathways must conduct thorough freedom-to-operate analyses. This includes assessing whether their proprietary compounds or methods fall within the scope of US Patent 10,261,083's claims. The patent's focus on the inhibition of ILAM-1 binding to LFA-1 is a key element to consider. Key Takeaways US Patent 10,261,083 claims methods of treating diseases by administering ILAM-1 inhibitors that block the binding of ILAM-1 to LFA-1. The patent broadly covers therapeutic applications in inflammatory, autoimmune, allergic, cardiovascular, neurological diseases, and cancer. The patent relies on a functional definition of inhibitors rather than specific chemical structures, offering broad potential coverage. The patent landscape for ILAM-1 inhibition includes composition of matter, method of treatment, and formulation claims from various entities. Companies operating in ILAM-1 targeted therapeutics must carefully evaluate this patent for freedom-to-operate. Frequently Asked Questions What is the primary target of the inhibitors claimed in US Patent 10,261,083? The primary target is Intercellular Adhesion Molecule-1 (ILAM-1), specifically its interaction with Lymphocyte Function-Associated Antigen-1 (LFA-1). Does the patent claim specific chemical compounds? No, US Patent 10,261,083 claims a functional class of compounds defined by their ability to inhibit ILAM-1 binding to LFA-1, rather than specific chemical structures. What therapeutic areas are covered by this patent? The patent covers a broad range of diseases associated with ILAM-1 activity, including inflammatory, autoimmune, allergic, cardiovascular, neurological diseases, and cancer. What is the significance of claiming a functional class of inhibitors? Claiming a functional class allows for broader protection, potentially encompassing future-developed compounds that achieve the same inhibitory effect, regardless of their specific chemical makeup. What is the primary limitation of such functional claims? Functional claims can face challenges related to enablement, definiteness, and prior art that discloses the general function or similar mechanisms. Cited Sources [1] Regents of the University of Minnesota. (2019). United States Patent 10,261,083: ISLAND INHIBITORS AND METHODS OF USE THEREOF. U.S. Patent and Trademark Office. More… ↓ ⤷ Start Trial

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Patent: 10,261,083

Summary for Patent: 10,261,083