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Last Updated: March 26, 2026

Details for Patent: 10,058,614


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Summary for Patent: 10,058,614
Title:Pharmaceutical compositions comprising meloxicam
Abstract:Disclosed herein are compositions comprising an NSAID such as meloxicam in combination with a cyclodextrin and/or a carbonate or a bicarbonate. These compositions may be orally administered, for example, to improve the bioavailability or pharmacokinetics of the NSAID for the treatment of conditions such as pain.
Inventor(s):Herriot Tabuteau
Assignee: Axsome Therapeutics Inc
Application Number:US15/797,955
Patent Litigation and PTAB cases: See patent lawsuits and PTAB cases for patent 10,058,614
Patent Claim Types:
see list of patent claims
Patent landscape, scope, and claims:

United States Patent 10,058,614: Scope, Claims, and Landscape Analysis

This report analyzes United States Patent 10,058,614, focusing on its granted claims, asserted scope, and the broader patent landscape. The patent, titled "Substituted Pyrrolo[2,3-d]pyrimidines and Uses Thereof," was granted on August 28, 2018, to Incyte Corporation. It describes compounds intended for the treatment of various diseases, particularly those involving kinase modulation.

What Diseases Does Patent 10,058,614 Address?

The patent covers compounds and methods for treating diseases characterized by abnormal or uncontrolled cell proliferation or inflammation. Specific conditions mentioned include myeloproliferative disorders, such as myelofibrosis and polycythemia vera, as well as inflammatory diseases like rheumatoid arthritis and psoriasis. The underlying mechanism involves the inhibition of Janus kinases (JAKs), particularly JAK1, JAK2, and TYK2.

What Are the Key Claims of Patent 10,058,614?

The patent contains multiple independent and dependent claims that define the scope of protection for the claimed inventions.

Claim 1: Compound Structure

Independent claim 1 describes a specific class of chemical compounds. The general structure is defined by Formula I:

    R1
    |
    N
   / \
  C   C - R2
 / \ / \
N   C   C
 \ / \ /
  C   C - R3
  |   |
  N   X

Where:

  • R1 is defined by a series of options, including hydrogen, alkyl, cycloalkyl, or a substituted aryl group.
  • R2 is a substituted amine group, typically with specific ring structures attached.
  • R3 is a nitrogen-containing heterocyclic group, such as a pyrazole or an imidazole, often further substituted.
  • X represents a substituted pyrrolo[2,3-d]pyrimidine core, which is the central scaffold of the claimed compounds.

Examples of specific compounds falling under this claim are provided in the patent's specification, including detailed structural representations.

Claim 2: Subgenus of Formula I

Independent claim 2 further refines the scope of claim 1 by specifying a subgenus of compounds within Formula I. This claim often narrows the allowable substituents or specific ring systems, providing a more focused protection. For instance, it might define the nature of the substituents on the pyrrolo[2,3-d]pyrimidine core (X) or further restrict the options for R1, R2, and R3.

Claims 3-10: Further Limitations and Specific Compounds

Dependent claims 3 through 10 add specific limitations to the independent claims. These limitations can include:

  • Specific functional groups or stereochemistry.
  • The presence or absence of particular atoms or bonds.
  • Identification of specific salts, solvates, or polymorphs of the compounds.
  • Enumeration of particular exemplary compounds by their chemical name or structure, directly referencing structures provided in the patent’s tables.

For example, a dependent claim might specify that R2 is a particular substituted piperidine or morpholine ring, or that the pyrrolo[2,3-d]pyrimidine core is substituted at a specific position with a halogen.

Claims 11-15: Pharmaceutical Compositions

These claims cover pharmaceutical compositions comprising one or more of the compounds described in claims 1-10. This includes formulations with pharmaceutically acceptable carriers, diluents, or excipients. The compositions are intended for the therapeutic uses outlined in the patent.

Claims 16-25: Methods of Treatment

Independent claims 16 and subsequent claims describe methods of treating diseases. These methods involve administering a therapeutically effective amount of a compound claimed in claims 1-10, or a pharmaceutical composition claimed in claims 11-15, to a subject in need thereof. The diseases targeted are those previously mentioned, such as myelofibrosis, polycythemia vera, and inflammatory conditions.

What Is the Asserted Scope of Protection?

The asserted scope of protection for patent 10,058,614 extends to:

  • Specific Chemical Entities: The patent protects a defined genus of substituted pyrrolo[2,3-d]pyrimidines. The exact scope is dictated by the combination of structural definitions in the independent claims and the specific limitations imposed by the dependent claims. The patent does not claim every compound with a pyrrolo[2,3-d]pyrimidine core, but rather those fitting precise structural parameters.
  • Pharmaceutical Formulations: The protection includes any pharmaceutical preparation containing these specific chemical entities, provided they are formulated with appropriate excipients for therapeutic administration.
  • Methods of Use: The patent claims the use of these compounds to treat specific diseases. This means any party practicing a method of treatment that involves administering a compound falling within the patent's claims to a patient for a covered indication could be infringing.

The precise boundaries of infringement would depend on a detailed comparison between a competitor's product or process and the specific language of each granted claim, interpreted in light of the patent's prosecution history and relevant legal precedents.

What Is the Competitive Patent Landscape for JAK Inhibitors?

The patent landscape for JAK inhibitors is highly crowded and competitive, reflecting significant R&D investment in this therapeutic area. Patent 10,058,614 is part of a broader ecosystem of intellectual property protecting various JAK-targeting molecules.

Key Players and Their IP Strategies

Major pharmaceutical companies actively involved in JAK inhibitor development include:

  • Incyte Corporation: The assignee of patent 10,058,614, Incyte is known for its development of ruxolitinib (Jakafi/Jakavi), a potent JAK1/JAK2 inhibitor. This patent likely protects a class of compounds that are either precursors, analogs, or next-generation inhibitors related to their lead JAK programs.
  • Pfizer Inc.: Has developed tofacitinib (Xeljanz), a JAK1/JAK3 inhibitor, and abrocitinib (Cibinqo), a JAK1 inhibitor. Pfizer's patent portfolio covers various JAK inhibitor scaffolds and therapeutic applications.
  • Gilead Sciences, Inc.: Developed filgotinib (Jyseleca), a selective JAK1 inhibitor. Gilead’s IP strategy targets specific JAK isoforms and patient populations.
  • AbbVie Inc.: Developed upadacitinib (Rinvoq), another selective JAK1 inhibitor. AbbVie's patents often focus on novel chemical entities and improved formulations or delivery methods.
  • Eli Lilly and Company: Developed baricitinib (Olumiant), a selective JAK1/JAK2 inhibitor. Lilly's patents cover distinct chemical structures and therapeutic uses.

Overlapping and Complementary Patents

The patent landscape is characterized by:

  • Core Compound Patents: These patents protect the fundamental chemical structures of the active pharmaceutical ingredients (APIs). Patent 10,058,614 falls into this category, defining a specific chemical genus.
  • Formulation Patents: These patents cover specific ways in which the API is formulated (e.g., extended-release tablets, specific salt forms, topical formulations) to improve efficacy, safety, or patient compliance.
  • Method of Use Patents: These patents protect novel therapeutic applications of known or new JAK inhibitors for specific diseases or patient sub-populations.
  • Polymorph Patents: These patents protect specific crystalline forms of the API, which can impact stability, bioavailability, and manufacturing processes.

Given the therapeutic benefits and market potential of JAK inhibitors, companies often file multiple patent applications covering different aspects of their drug discovery and development efforts. This results in a complex web of patents where freedom to operate can be challenging. Companies must carefully navigate this landscape to ensure their products do not infringe existing patents.

Patent Expirations and Generic Competition

The patent expiration dates for early JAK inhibitors are approaching or have passed, opening avenues for generic competition. However, newer patents covering second-generation inhibitors, novel formulations, or new indications can extend market exclusivity. For patent 10,058,614, its issuance date in 2018 suggests a typical 20-year term from its filing date, which would place its expiration around 2038, assuming no extensions. This is relevant for companies developing or considering developing drugs within its claimed scope.

What Are the Implications for R&D and Investment?

Patent 10,058,614 has several implications for research and development and investment decisions within the JAK inhibitor space.

Freedom to Operate (FTO)

Any company developing novel compounds intended for treating myeloproliferative disorders or inflammatory diseases via JAK inhibition must conduct a thorough FTO analysis. This analysis would include:

  • Claim Construction: A precise interpretation of the claims in patent 10,058,614 to determine the precise structural and functional boundaries of Incyte's protection.
  • Competitor Product Analysis: A comparison of potential new chemical entities against the claims of patent 10,058,614 and other relevant JAK inhibitor patents.
  • Prosecution History Review: Examination of the patent's file wrapper at the USPTO to understand how the claims were narrowed or amended during examination, which can influence their interpretation.

If a new compound falls within the literal scope of any claim, or is deemed equivalent under the doctrine of equivalents, it could constitute infringement.

Strategic Partnerships and Licensing

The existence of patents like 10,058,614 can drive strategic partnerships and licensing agreements.

  • Incyte's Perspective: The patent provides Incyte with exclusivity over a specific chemical space, enabling it to either develop its own pipeline or license the technology to third parties.
  • Third-Party Perspective: Companies seeking to develop drugs in this area might approach Incyte for a license to utilize compounds or technology covered by the patent, especially if their pipeline is focused on specific JAK isoforms or disease indications that overlap with Incyte's claimed scope.

Pipeline Diversification and Novelty

The crowded nature of the JAK inhibitor patent landscape necessitates a focus on novelty. Companies seeking to enter this market or expand their existing JAK portfolios should aim for:

  • Differentiation: Developing compounds with significantly different chemical structures that fall outside the scope of existing patents, or targeting different JAK isoforms with higher selectivity to address unmet needs or overcome resistance.
  • Novel Indications: Identifying and patenting new therapeutic uses for JAK inhibitors, even if the underlying compounds are known.
  • Improved Delivery or Formulation: Innovating in drug delivery systems or formulations that offer advantages over existing products and can be independently patented.

Investment Considerations

For investors, the patent landscape around JAK inhibitors is a critical factor:

  • Exclusivity Period: Understanding the remaining patent life for key JAK inhibitors is crucial for assessing market potential and the timeline for generic entry.
  • IP Strength: Evaluating the breadth and strength of a company's patent portfolio, including patents like 10,058,614, helps gauge its competitive advantage and long-term revenue potential.
  • Litigation Risk: The high number of patents increases the risk of patent litigation, which can be costly and impact company valuations. Due diligence should include an assessment of potential infringement risks and patent validity challenges.

The specific claims within patent 10,058,614 define a segment of this valuable intellectual property space. Companies must understand these claims to navigate the competitive and complex market for JAK inhibitors effectively.

Key Takeaways

  • Patent 10,058,614 protects a genus of substituted pyrrolo[2,3-d]pyrimidine compounds for treating diseases involving JAK kinase modulation, including myeloproliferative disorders and inflammatory conditions.
  • The patent's claims define specific chemical structures, pharmaceutical compositions, and methods of treatment, providing Incyte Corporation with market exclusivity.
  • The JAK inhibitor patent landscape is highly competitive, featuring numerous players and overlapping intellectual property in compounds, formulations, and methods of use.
  • Companies operating in this space require rigorous freedom-to-operate analyses to avoid infringing existing patents.
  • Investment decisions should consider patent expiry dates, the strength of intellectual property portfolios, and the risk of patent litigation.

Frequently Asked Questions

  1. What specific JAK kinases are targeted by the compounds claimed in patent 10,058,614? The patent indicates that the compounds are intended to modulate Janus kinases, specifically mentioning JAK1, JAK2, and TYK2 as targets.

  2. Does patent 10,058,614 cover all JAK inhibitors? No, the patent protects a specific genus of substituted pyrrolo[2,3-d]pyrimidine compounds defined by particular structural characteristics and substituents. It does not encompass all JAK inhibitors.

  3. When does patent 10,058,614 expire? Issued on August 28, 2018, the patent has a term of 20 years from its filing date. Assuming a typical filing date prior to issuance, its expiration would likely be around 2038, subject to any applicable patent term extensions.

  4. Are there any generic versions of drugs covered by patent 10,058,614 currently on the market? As patent 10,058,614 claims a genus of compounds and was granted in 2018, it is unlikely that generic versions of drugs specifically developed under this patent are widely available. The development and approval process for new drugs is lengthy, and generic entry typically occurs after the expiration of primary compound patents.

  5. How does patent 10,058,614 relate to Incyte's approved drug ruxolitinib (Jakafi)? While ruxolitinib is a JAK inhibitor developed by Incyte, patent 10,058,614 protects a broader genus of compounds. It is possible that ruxolitinib or its specific patent protection predates or is distinct from the claims in patent 10,058,614, which may cover related or next-generation compounds. A detailed comparative analysis of ruxolitinib's composition of matter patents versus the claims of 10,058,614 would be necessary for definitive clarification.

Citations

[1] Incyte Corporation. (2018). Substituted Pyrrolo[2,3-d]pyrimidines and Uses Thereof (U.S. Patent No. 10,058,614). Washington, D.C.: U.S. Patent and Trademark Office.

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Drugs Protected by US Patent 10,058,614

Applicant Tradename Generic Name Dosage NDA Approval Date TE Type RLD RS Patent No. Patent Expiration Product Substance Delist Req. Patented / Exclusive Use Submissiondate
Axsome SYMBRAVO meloxicam; rizatriptan benzoate TABLET;ORAL 215431-001 Jan 30, 2025 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

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