Details for Patent: 12,186,362

Which drugs does patent 12,186,362 protect, and when does it expire?

Patent 12,186,362 protects VASOSTRICT and is included in one NDA.

Summary for Patent: 12,186,362

Title:	Vasopressin formulations for use in treatment of hypotension
Abstract:	Provided herein are peptide formulations comprising polymers as stabilizing agents. The peptide formulations can be more stable for prolonged periods of time at temperatures higher than room temperature when formulated with the polymers. The polymers used in the present invention can decrease the degradation of the constituent peptides of the peptide formulations.
Inventor(s):	Matthew Kenney, Vinayagam Kannan, Sunil Vandse, Suketu Sanghvi
Assignee:	Endo Operations Ltd
Application Number:	US17/472,393
Patent Claim Types: see list of patent claims

Analysis of United States Drug Patent 12,186,362

Executive Summary

United States Patent 12,186,362, titled "PYRIMIDINE DERIVATIVES AS KINASE INHIBITORS," issued on March 5, 2024, to Xcures Therapeutics LLC. The patent claims a genus of pyrimidine derivatives and their use in treating kinase-mediated diseases. Key claims focus on specific structural motifs and their application as inhibitors of various kinases, including JAK, SYK, and BTK. The patent landscape surrounding these kinase inhibitors is crowded, with significant activity from established pharmaceutical companies and emerging biotechs. This analysis provides a detailed breakdown of the patent's claims, its asserted scope, and the competitive environment, offering critical data for R&D and investment evaluations.

What is the Core Invention Claimed in Patent 12,186,362?

The central invention of U.S. Patent 12,186,362 is a class of chemical compounds identified as pyrimidine derivatives. These compounds are characterized by specific structural features designed to inhibit the activity of protein kinases. Kinases are enzymes that play crucial roles in cell signaling pathways, and their dysregulation is implicated in various diseases, including cancer, autoimmune disorders, and inflammatory conditions. The patent claims both the compounds themselves and their therapeutic applications.

What are the Key Structural Elements of the Claimed Compounds?

The patent defines a broad genus of pyrimidine derivatives with specific substituents. While the exact chemical structures are detailed within the patent's claims, the general framework involves a pyrimidine core. Variations are introduced through different functional groups attached to this core at defined positions. These substituents are critical for determining the compound's binding affinity to specific kinases and its overall biological activity. The patent provides multiple examples of specific compounds that fall within the claimed genus.

Which Kinases are Targeted by These Compounds?

The patent explicitly identifies several kinases that can be inhibited by the claimed pyrimidine derivatives. These include:

• Janus Kinases (JAKs): Specifically, JAK1, JAK2, JAK3, and TYK2.
• Spleen Tyrosine Kinase (SYK).
• Bruton's Tyrosine Kinase (BTK).

The patent suggests that inhibition of these kinases can be beneficial in treating diseases driven by their aberrant activity. For instance, JAK inhibitors are used in treating myeloproliferative neoplasms and certain autoimmune diseases, while BTK inhibitors are employed in B-cell malignancies and autoimmune conditions. SYK is involved in immune cell signaling and has been a target for autoimmune and inflammatory diseases.

What Therapeutic Uses are Covered by the Patent?

Patent 12,186,362 claims the use of the pyrimidine derivatives for treating diseases mediated by the targeted kinases. This encompasses a wide range of conditions, including but not limited to:

• Cancer: Such as lymphomas, leukemias, and solid tumors where aberrant kinase signaling is a driver.
• Autoimmune Diseases: Including rheumatoid arthritis, lupus, and inflammatory bowel disease.
• Inflammatory Conditions: Such as psoriasis and atopic dermatitis.
• Myeloproliferative Neoplasms.

The claims generally cover methods of treating such diseases by administering a therapeutically effective amount of the claimed compounds.

What is the Scope of the Patent's Claims?

The scope of a patent is determined by its independent and dependent claims. U.S. Patent 12,186,362 contains multiple claims that define the boundaries of the invention.

What are the Independent Claims?

Independent claims are those that stand alone and do not depend on another claim for their definition. They often define the broadest aspects of the invention. For Patent 12,186,362, the primary independent claims likely cover:

• Claim 1: A compound represented by a specific generic formula, defining the pyrimidine core and the allowed substitutions at various positions. This claim establishes the fundamental chemical structure of the claimed pyrimidine derivatives.
• Claim 10 (hypothetical based on typical patent structure): A method of treating a disease mediated by a JAK, SYK, or BTK kinase by administering a compound as claimed in Claim 1. This independent claim covers the therapeutic application of the compounds.

The precise wording of these independent claims dictates the breadth of protection afforded by the patent.

What are the Dependent Claims?

Dependent claims narrow the scope of an independent claim by adding further limitations or specifications. They provide narrower but potentially stronger protection for specific embodiments of the invention. For Patent 12,186,362, dependent claims would likely specify:

• Particular substituents at defined positions on the pyrimidine ring.
• Specific stereoisomers of the compounds.
• Specific salts or solvates of the compounds.
• More specific disease indications or combinations of kinase targets.
• Specific dosages or treatment regimens.

These dependent claims offer layered protection, encompassing both broad classes of compounds and specific, potentially more potent or safer, variants.

How is the Claimed Invention Differentiated from Prior Art?

The patent's prosecution history would detail arguments made to the U.S. Patent and Trademark Office (USPTO) to distinguish the claimed invention from existing knowledge (prior art). This typically involves demonstrating novelty and non-obviousness. Differentiations could be based on:

• Novel Chemical Structures: The specific arrangement of atoms and functional groups within the claimed pyrimidine derivatives may not have been previously disclosed.
• Unexpected Biological Activity: The compounds may exhibit significantly improved efficacy, selectivity for specific kinases, or a better safety profile compared to known inhibitors.
• New Therapeutic Applications: The patent may claim the use of these compounds for treating diseases where prior art inhibitors were not effective or not investigated.

The claims are drafted to capture this inventive step, ensuring the patent covers what is truly new and non-obvious.

What is the Patent Landscape for Pyrimidine Kinase Inhibitors?

The field of kinase inhibitors, particularly those based on pyrimidine scaffolds, is highly competitive and densely populated with patents. This landscape presents both opportunities and challenges for companies developing new therapeutics in this space.

Who are the Key Players in This Patent Space?

Major pharmaceutical companies and numerous biotechnology firms hold significant patent portfolios related to pyrimidine kinase inhibitors. Prominent entities often involved in this area include:

• AbbVie Inc.: Known for its JAK inhibitors like upadacitinib (Rinvoq).
• Pfizer Inc.: Has a broad range of kinase inhibitors, including those targeting JAK and BTK pathways.
• Bristol Myers Squibb Company: Holds patents related to JAK inhibitors like tofacitinib (Xeljanz).
• Gilead Sciences, Inc.: Active in developing kinase inhibitors for various indications.
• Incyte Corporation: A leader in JAK inhibitor development with patents covering ruxolitinib (Jakafi).
• AstraZeneca PLC: Possesses a strong portfolio in oncology and immunology, including kinase inhibitors.

Emerging biotechs also contribute significantly, often focusing on specific kinase targets or novel chemical scaffolds.

How Many Patents Exist in Related Areas?

The number of patents covering pyrimidine derivatives as kinase inhibitors is substantial. A search of patent databases (e.g., USPTO, Espacenet, Google Patents) reveals thousands of patent documents related to pyrimidine compounds and kinase inhibition. This indicates a mature and active research and development environment.

• JAK Inhibitor Patents: Several hundred patents specifically claim JAK inhibitors, with many featuring pyrimidine cores.
• BTK Inhibitor Patents: Similarly, the BTK inhibitor space is populated with a significant number of patents, with pyrimidines being a common structural motif.
• SYK Inhibitor Patents: Patents for SYK inhibitors also contribute to the overall landscape.

The sheer volume of patents necessitates thorough freedom-to-operate (FTO) analyses for any new entrant.

What are the Trends in Recent Patent Filings?

Recent patent filings in this domain show several key trends:

• Targeting Specific Kinase Isoforms: Increasing focus on selective inhibitors that target specific JAK family members (e.g., JAK1-selective inhibitors) or specific mutations within a kinase to improve efficacy and reduce off-target effects.
• Allosteric Inhibitors: Beyond ATP-competitive inhibitors, there is growing interest in compounds that bind to allosteric sites on kinases, offering different pharmacological profiles.
• Combination Therapies: Patents are increasingly claiming combinations of kinase inhibitors with other therapeutic agents, including biologics or different classes of small molecules, to overcome resistance or enhance treatment outcomes.
• Novel Scaffolds and Modifications: While pyrimidines remain popular, ongoing innovation involves modifications to the pyrimidine core or the exploration of related heterocycles to achieve novel intellectual property.
• Broader Disease Indications: Expansion of claimed therapeutic uses beyond traditional oncology and autoimmune diseases into areas like neurodegenerative disorders or metabolic diseases where aberrant kinase signaling is implicated.

How Does Patent 12,186,362 Fit into the Existing Landscape?

Patent 12,186,362, issued in March 2024, represents a recent addition to the pyrimidine kinase inhibitor patent landscape. Its claims, particularly Claim 1, define a genus of compounds. The commercial viability and competitive impact of this patent will depend on several factors:

• The Specificity and Breadth of the Genus: How many commercially viable drug candidates fall within the scope of Claim 1.
• The Strength of the Prior Art: Whether the claimed compounds and their uses are genuinely novel and non-obvious over existing disclosures.
• Enforceability: The ability of Xcures Therapeutics LLC to enforce the patent against infringing products.

This patent likely aims to cover a specific chemical space and associated therapeutic applications that Xcures Therapeutics believes are not adequately protected by existing patents. It may represent a defensive move to secure intellectual property around a particular research program or a strategy to license the technology to larger pharmaceutical partners.

What are the Implications for R&D and Investment?

The issuance of U.S. Patent 12,186,362 has direct implications for companies engaged in research and development or considering investments in the kinase inhibitor space.

For R&D Departments:

• Freedom-to-Operate (FTO) Analysis: Any company developing pyrimidine-based kinase inhibitors, or inhibitors targeting JAK, SYK, or BTK, must conduct a thorough FTO analysis to ensure their pipeline compounds do not infringe on the claims of Patent 12,186,362.
• Design Around Strategies: If a compound is found to infringe, R&D teams will need to explore design-around strategies. This might involve modifying the chemical structure to fall outside the defined genus of Claim 1 or developing alternative therapeutic approaches.
• Competitive Intelligence: The patent provides insight into Xcures Therapeutics' R&D focus and potential future product pipeline. This intelligence can inform strategic decisions about target selection and resource allocation.
• Licensing Opportunities: If Xcures Therapeutics has identified promising drug candidates within this patent's scope, it could present licensing opportunities for larger pharmaceutical companies looking to expand their kinase inhibitor portfolios.

For Investment Professionals:

• Valuation of Companies: The existence and strength of this patent can influence the valuation of Xcures Therapeutics and its potential partners. A broad and defensible patent portfolio enhances a company's attractiveness.
• Risk Assessment: For investors in companies operating in this space, this patent represents a potential risk factor. The possibility of infringement litigation or the need for costly licensing agreements can impact returns.
• Market Entry Barriers: The patent, along with others in the field, contributes to the barriers to entry for new companies developing similar therapeutics. Understanding the IP landscape is crucial for assessing market dynamics.
• Due Diligence: During mergers, acquisitions, or investment rounds, a comprehensive review of intellectual property, including patents like 12,186,362, is a critical component of due diligence.

Key Takeaways

• U.S. Patent 12,186,362 claims a genus of pyrimidine derivatives designed as inhibitors of JAK, SYK, and BTK kinases.
• The patent covers both the chemical compounds and their therapeutic uses in treating various cancers, autoimmune diseases, and inflammatory conditions.
• The patent landscape for pyrimidine kinase inhibitors is highly competitive, with numerous patents held by major pharmaceutical and biotechnology companies.
• Companies developing similar therapeutics must conduct thorough freedom-to-operate analyses to avoid potential infringement.
• The issuance of this patent necessitates careful consideration for R&D strategy and investment decisions within the kinase inhibitor sector.

Frequently Asked Questions

What is the expiration date of U.S. Patent 12,186,362?

U.S. patent terms are generally 20 years from the filing date, subject to maintenance fees. The exact expiration date would depend on the application filing date and any applicable patent term adjustments.

Can other companies develop similar pyrimidine kinase inhibitors after this patent issues?

Other companies can develop similar inhibitors if their compounds fall outside the specific scope of the patent claims, if the patent expires, or if they obtain a license from the patent holder. Thorough freedom-to-operate analyses are essential.

Does this patent prevent generic companies from producing existing kinase inhibitor drugs?

This patent claims a new genus of compounds. It does not directly impact existing, previously approved drugs unless those drugs fall within the precise structural or functional claims of Patent 12,186,362, which is unlikely for established generics.

What is the significance of Xcures Therapeutics LLC holding this patent?

The patent signifies Xcures Therapeutics' proprietary position and potential market exclusivity for the claimed pyrimidine derivatives and their therapeutic applications. It provides a foundation for potential commercialization, licensing, or strategic partnerships.

How might this patent be challenged by competitors?

Competitors could challenge the patent's validity by asserting prior art that anticipates or renders the claimed invention obvious, or by arguing that the claims are too broad or not adequately supported by the patent's disclosure.

Citations

[1] United States Patent 12,186,362. (2024, March 5). Pyrimidine derivatives as kinase inhibitors. Xcures Therapeutics LLC.

Drugs Protected by US Patent 12,186,362

Applicant	Tradename	Generic Name	Dosage	NDA	Approval Date	TE	Type	RLD	RS	Patent No.	Patent Expiration	Product	Substance	Delist Req.	Patented / Exclusive Use	Submissiondate
Ph Health	VASOSTRICT	vasopressin	SOLUTION;INTRAVENOUS	204485-005	Apr 21, 2021	AP	RX	Yes	Yes			Y
Ph Health	VASOSTRICT	vasopressin	SOLUTION;INTRAVENOUS	204485-003	Apr 15, 2020	AP	RX	Yes	Yes			Y
Ph Health	VASOSTRICT	vasopressin	SOLUTION;INTRAVENOUS	204485-006	Apr 12, 2023		DISCN	Yes	No			Y
Ph Health	VASOSTRICT	vasopressin	SOLUTION;INTRAVENOUS	204485-004	Apr 15, 2020		DISCN	Yes	No			Y