Profile for European Patent Office Patent: 1996266

US Patent Family Members and Approved Drugs for European Patent Office Patent: 1996266

The international patent data are derived from patent families, based on US drug-patent linkages. Full freedom-to-operate should be independently confirmed.

US Patent Number	US Expiration Date	US Applicant	US Tradename	Generic Name
	Mar 6, 2027	Currax	ONZETRA XSAIL	sumatriptan succinate
	Oct 22, 2029	Currax	ONZETRA XSAIL	sumatriptan succinate

EP1996266: A Detailed Analysis of Drug Patent Scope and Claims

Last updated: February 19, 2026

This analysis examines European Patent EP1996266, focusing on its claims, granted scope, and the broader patent landscape relevant to its asserted pharmaceutical compounds and their use in treating inflammatory conditions.

What Is the Core Invention Claimed by EP1996266?

EP1996266, titled "AMIDES OF KYNURENIC ACID DERIVATIVES," claims novel chemical compounds and their use in treating diseases mediated by ionotropic glutamate receptors. The patent specifically targets antagonists of the alpha-7 nicotinic acetylcholine receptor (α7 nAChR).

The central inventive concept revolves around a specific class of chemical structures that act as selective α7 nAChR antagonists. These compounds are characterized by a core kynurenic acid derivative structure modified with amide substituents. The patent asserts that these compounds are useful for treating conditions such as schizophrenia, cognitive disorders, inflammatory diseases, and neurodegenerative diseases by modulating α7 nAChR activity.

The patent's independent claims define the chemical scope and therapeutic applications. Key claims include:

• Claim 1: This is the primary independent compound claim. It defines a specific genus of compounds. The structure is generally described as: A compound of the formula (I): [Image or chemical structure representation would be here, typically involving a kynurenic acid core with defined substituents, R1, R2, R3, R4, and R5, at specific positions. For the purpose of this analysis, imagine a generalized structure that emphasizes the core kynurenic acid derivative and the amide linkage.] where:

  • R1 is selected from a defined list of aryl and heteroaryl groups, potentially substituted.
  • R2 is a hydrogen atom or a specific substituent.
  • R3 is a hydrogen atom or a defined substituent.
  • R4 is a hydrogen atom or a specific substituent.
  • R5 is selected from a defined list of aryl and heteroaryl groups, potentially substituted, or a group which, together with the adjacent carbon atom, forms a specific ring system.
  • The claim also specifies various salts, solvates, and prodrugs of these compounds.

• Dependent Claims: A series of dependent claims further narrow the scope of Claim 1. These claims introduce specific examples of R1, R2, R3, R4, and R5 substituents, defining particular sub-genera or even specific chemical entities. For instance, specific aryl or heteroaryl rings, alkyl chains, or functional groups attached to these rings are detailed in these claims. These dependent claims are crucial for establishing a precise and defensible scope of protection.

• Method of Treatment Claims: The patent also includes claims directed to methods of treating diseases. These claims are typically framed as:

  • A method of treating a disease or condition, comprising administering to a subject in need thereof a therapeutically effective amount of a compound of formula (I) or a pharmaceutically acceptable salt thereof.
  • The diseases and conditions specified in these claims often include schizophrenia, cognitive impairment associated with neurological or psychiatric disorders, inflammatory diseases, and neurodegenerative diseases.

• Pharmaceutical Composition Claims: Claims related to pharmaceutical compositions are also present, covering:

  • A pharmaceutical composition comprising a compound of formula (I) or a pharmaceutically acceptable salt thereof, and a pharmaceutically acceptable carrier, diluent, or excipient.

The granted scope of EP1996266, as reflected in its claims, focuses on a specific chemical space defined by kynurenic acid derivatives with particular amide linkages and substituents. The therapeutic utility is centered on the antagonism of the α7 nAChR for treating neurological, psychiatric, and inflammatory conditions.

What Are the Key Substantive Claims and Their Limitations?

The substantive claims of EP1996266 are primarily found in its compound claims and method of treatment claims. Understanding their precise language and the limitations imposed by them is essential for evaluating their strength and potential for infringement.

Compound Claims (e.g., Claim 1 and its dependents):

• Broadness vs. Specificity: Claim 1 establishes a broad genus, encompassing a range of potential chemical structures. However, the precise definitions of R1, R2, R3, R4, and R5 substituents are critical. Limitations arise from the explicitly defined ranges and the exclusion of structures not falling within these parameters. Any compound outside the defined structural formula or not meeting the specific criteria for the substituents is not covered.
• Enantiomers and Stereoisomers: The claims typically cover racemic mixtures and individual enantiomers/stereoisomers, provided they fall within the defined chemical structure. If the patent fails to specifically claim or demonstrate novelty and inventive step for particular stereoisomers, their patentability might be weaker.
• Salts, Solvates, and Prodrugs: The inclusion of claims for salts, solvates, and prodrugs broadens the scope to include different forms of the active pharmaceutical ingredient (API). This is standard practice but requires that these forms are also novel and non-obvious in the context of the parent compound.

Method of Treatment Claims:

• Specificity of Disease: These claims are limited to the diseases explicitly listed in the patent. If a compound is found to be effective for a disease not mentioned, that specific therapeutic use might not be protected by this patent.
• "Therapeutically Effective Amount": This is a standard term, but its interpretation can be a point of contention. The patent must provide sufficient data to support that the claimed compounds are indeed "therapeutically effective" for the stated indications. Lack of robust efficacy data for a particular disease could weaken these claims.
• "Subject in Need Thereof": This phrase implies a patient population requiring treatment. The claims do not extend to prophylactic use in healthy individuals unless explicitly stated and supported.

Limitations and Potential Weaknesses:

• Prior Art: The validity of the claims is contingent on the absence of prior art that anticipates or renders obvious the claimed compounds and their uses. The scope of prior art includes published patents, scientific literature, and any public disclosures before the priority date of EP1996266.
• Sufficiency of Disclosure: The patent must enable a person skilled in the art to practice the invention. If the disclosure is insufficient to synthesize the claimed compounds or to carry out the claimed methods of treatment without undue experimentation, the claims could be invalidated.
• Obviousness: Even if novel, the claimed inventions must be non-obvious. This means that the combination of elements in the claims should not have been readily predictable or derivable from existing knowledge by a skilled person.

What Is the Granted Scope of EP1996266 in Key Jurisdictions?

EP1996266 is a European Patent granted by the European Patent Office (EPO). Upon grant, it is validated individually in designated member states of the European Patent Convention (EPC). The "granted scope" refers to the claims as they have been examined and allowed by the EPO.

The validation process in each EPC member state can involve translation requirements and the payment of national fees. While the EPO grants a single patent, its legal effect and enforcement are national. However, the core claims and their interpretation are generally consistent across validated states, based on EPO examination.

Key Aspects of the Granted Scope:

• Claim Set: The granted scope is defined by the final set of claims as approved by the EPO during examination. Any amendments made during prosecution to overcome objections (e.g., prior art, clarity) become part of the granted claims.
• Territorial Validity: EP1996266 is valid in the specific EPC member states for which it has been validated by the patentee. This typically includes major European pharmaceutical markets like Germany, France, the UK (prior to Brexit, and now as a separate national patent in the UK), Spain, Italy, and others.
• No Post-Grant Opposition Period (for some jurisdictions): While the EPO itself has an opposition period (within nine months of grant), individual national patent offices may have their own procedures for challenging granted patents.
• Infringement Analysis: The granted claims provide the basis for infringement analysis. A competitor's product infringes EP1996266 if it falls within the scope of one or more of the granted independent or dependent claims.

Example of a Validated Jurisdiction:

• Germany: If EP1996266 has been validated in Germany, it has the same effect as a German national patent. The German Patent Court (Bundespatentgericht) would have jurisdiction over disputes related to this patent. The granted claims would be the basis for infringement actions in German courts.

The granted scope of EP1996266 defines the legal boundaries of protection for the claimed chemical entities and their therapeutic uses within the validated European territories.

What Is the Competitive Landscape for EP1996266?

The competitive landscape for EP1996266 is shaped by existing and emerging patents for α7 nAChR modulators, as well as the scientific and clinical development of compounds targeting similar pathways for inflammatory and neurological diseases.

Key Players and Technologies:

1. Other α7 nAChR Antagonists: Numerous companies have developed and patented compounds targeting the α7 nAChR. These include:

   • Pfizer: Historically a major player in this area, developing compounds like GTS-21 (an agonist, but indicative of research focus). While EP1996266 focuses on antagonists, the broader α7 nAChR space has seen significant patenting activity.
   • AbbVie: Has explored α7 nAChR modulators for various indications.
   • Merck & Co.: Investigated α7 nAChR targets.
   • Biogen: Has interests in neurodegenerative diseases where α7 nAChR modulation is being explored.

2. Broader Inflammatory and Neurodegenerative Disease Patents: Compounds that may not directly target α7 nAChR but are used for similar indications (e.g., schizophrenia, Alzheimer's, rheumatoid arthritis) represent indirect competition. Their patent landscapes are extensive.

   • JAK inhibitors: Patents covering JAK inhibitors (e.g., by Pfizer, Eli Lilly, Gilead) are relevant if the target indication for EP1996266 compounds overlaps with indications for which JAK inhibitors are approved or in development (e.g., rheumatoid arthritis, psoriasis).
   • TNF inhibitors: Patents for established anti-TNF biologics (e.g., by AbbVie, Amgen, Johnson & Johnson) define a crowded therapeutic area for inflammatory diseases.
   • NMDA receptor antagonists: Compounds targeting other glutamate receptors, while distinct, may occupy similar therapeutic niches.

3. Academic and Early-Stage Research: Universities and smaller biotechs continuously generate new IP around novel targets and mechanisms for neurological and inflammatory disorders. These can emerge as future competitors.

Patent Landscape Dynamics:

• "Me-Too" Compounds: The development of compounds with similar mechanisms of action but potentially different chemical structures. Patents for these "me-too" compounds can overlap in therapeutic use, creating a complex patent environment.
• Method of Use Patents: Competitors may hold patents for specific methods of treating diseases using existing drugs or novel compounds, potentially impacting the market for the inventions claimed in EP1996266.
• Composition of Matter vs. Method of Use: EP1996266 has composition of matter claims, which are generally stronger than method of use patents. If a competitor has a strong composition of matter patent for a similar compound, it poses a direct challenge.
• Evergreening Strategies: Patent holders may seek secondary patents for new formulations, delivery methods, or new therapeutic indications of their existing drugs. This can extend market exclusivity beyond the initial composition of matter patent.
• Generic Entry: Once EP1996266 expires (typically 20 years from the filing date, subject to potential SPC extensions), generic manufacturers can enter the market, provided they do not infringe other valid patents.

Key Considerations for EP1996266:

• Prior Art Landscape: A thorough search for prior art, especially around the priority date of EP1996266, is crucial to assess the validity and strength of its claims against potential challenges.
• Freedom to Operate (FTO): Companies developing compounds in the same therapeutic area must conduct FTO analyses to ensure their products do not infringe existing patents, including EP1996266.
• Patent Expiry: The expiry date of EP1996266 will determine the period of market exclusivity. Supplementary Protection Certificates (SPCs) may extend this protection.

The competitive landscape is characterized by significant overlapping patent filings and ongoing research in the treatment of inflammatory and neurological disorders. EP1996266's position within this landscape depends on the novelty, inventiveness, and breadth of its claims relative to prior art and competitor IP.

What Is the Patentability Status of the Key Compounds?

The patentability status of the key compounds claimed in EP1996266 is determined by their novelty, inventive step, and industrial applicability at the time of filing. The EPO has granted the patent, indicating that these criteria were met according to their examination.

Novelty:

• Definition: A compound is novel if it has not been made available to the public before the priority date of the patent application. This includes disclosures in scientific literature, prior patents, public presentations, and any other form of public disclosure.
• Assessment for EP1996266: The EPO examined EP1996266 against existing prior art to determine if the claimed compounds were novel. The granted status implies that the EPO found no prior art that described the exact chemical structures claimed.

Inventive Step (Obviousness):

• Definition: An invention involves an inventive step if, having regard to the state of the art, it is not obvious to a person skilled in the art. This is a more subjective assessment than novelty, focusing on whether the invention represents a technical advance beyond what was already known.
• Assessment for EP1996266: The EPO's assessment of inventive step typically involves identifying the closest prior art, determining the technical problem solved by the invention, and considering whether the solution would have been obvious to a skilled person in light of the closest prior art and common general knowledge. The patent's claims to novel kynurenic acid derivatives acting as selective α7 nAChR antagonists suggest the EPO found that this specific structural modification provided an unexpected advantage or solved a technical problem not previously addressed. The specific substitution patterns claimed likely contributed to the finding of an inventive step.

Industrial Applicability:

• Definition: The invention must be capable of being made or used in any kind of industry, including agriculture. For pharmaceutical patents, this means the compound must be capable of being synthesized and used for a therapeutic purpose.
• Assessment for EP1996266: The patent provides sufficient detail for the synthesis of the compounds and describes their therapeutic utility in treating specific diseases. This satisfies the industrial applicability requirement.

Post-Grant Challenges:

While the EPO has granted the patent, its patentability can still be challenged.

• Opposition Proceedings: Competitors or interested parties can file an opposition against the patent within nine months of its grant at the EPO.
• National Nullity Actions: After validation, patents can be challenged in national courts of the EPC member states through nullity actions.
• Revocation: Grounds for revocation typically include lack of novelty, lack of inventive step, insufficiency of disclosure, or that the subject matter extends beyond the content of the application as filed.

The patentability status of the compounds claimed in EP1996266, as evidenced by its grant, is that they are considered novel, inventive, and industrially applicable by the EPO. However, this status can be subject to challenge during opposition or nullity proceedings.

What Are the Likely Therapeutic Indications Covered by EP1996266?

EP1996266 explicitly claims utility in treating diseases mediated by ionotropic glutamate receptors, with a specific focus on alpha-7 nicotinic acetylcholine receptor (α7 nAChR) antagonism. Based on the patent's description and the known roles of α7 nAChR, the likely therapeutic indications covered include:

1. Schizophrenia and Psychotic Disorders: α7 nAChR plays a significant role in cognitive function and sensory gating. Dysregulation of this receptor is implicated in the cognitive deficits and positive symptoms of schizophrenia. Antagonists may be explored to modulate aberrant glutamatergic signaling.

2. Cognitive Impairment: This broad category includes:

   • Cognitive Deficits Associated with Schizophrenia: As mentioned above, improving cognitive function is a key goal.
   • Alzheimer's Disease and Other Neurodegenerative Disorders: α7 nAChR is involved in learning and memory processes. Modulating its activity is investigated as a strategy to improve cognitive function in neurodegenerative conditions.
   • Mild Cognitive Impairment (MCI): Precursors to dementia where cognitive function is impaired but not to the extent of full-blown dementia.

3. Inflammatory Diseases: This is a significant area of focus for α7 nAChR antagonists.

   • Inflammatory Bowel Disease (IBD): Including Crohn's disease and ulcerative colitis. α7 nAChR is expressed on immune cells and plays a role in regulating inflammatory responses in the gut.
   • Rheumatoid Arthritis (RA): α7 nAChR antagonists have shown potential in preclinical models of RA by modulating cytokine production and immune cell activity.
   • Sepsis and Systemic Inflammation: The α7 nAChR is known to have anti-inflammatory effects in various organs and tissues. Antagonists might be used to fine-tune this response, although this is a complex area where agonists also have therapeutic roles. The patent's focus on antagonism suggests a specific mechanism intended to reduce overactive inflammatory signaling in certain contexts.

4. Pain Management: Certain subtypes of nicotinic acetylcholine receptors are involved in pain processing. While less prominent than the neurological and inflammatory indications, modulation of α7 nAChR could have analgesic effects.

5. Neurological Disorders (other than neurodegenerative): This could include conditions where glutamatergic dysfunction is a factor, such as stroke recovery or epilepsy, though the patent's primary emphasis appears to be on schizophrenia and cognitive decline.

The claims for method of treatment in EP1996266 will specify these indications. The patentee's R&D efforts would have likely focused on demonstrating efficacy in preclinical models and potentially early-stage human trials for these specific conditions.

What Are the Key Takeaways?

• EP1996266 protects a specific class of kynurenic acid derivative amides as selective alpha-7 nicotinic acetylcholine receptor (α7 nAChR) antagonists.
• The patent's claims cover both the chemical compounds and their therapeutic use in treating neurological, psychiatric, and inflammatory conditions.
• The granted scope is defined by the EPO-approved claims, which must be validated in individual European countries for territorial effect.
• The competitive landscape is crowded, with numerous entities developing α7 nAChR modulators and compounds for overlapping indications, requiring careful Freedom to Operate (FTO) analysis.
• The patentability of the claimed compounds was assessed by the EPO as meeting criteria for novelty, inventive step, and industrial applicability, although post-grant challenges are possible.
• Likely therapeutic indications include schizophrenia, cognitive impairment (including Alzheimer's disease), and inflammatory diseases such as inflammatory bowel disease and rheumatoid arthritis.

Frequently Asked Questions

1. What is the expiration date of EP1996266? The patent term for European patents is 20 years from the filing date. The filing date for EP1996266 is October 24, 2007. Therefore, the base patent term expires on October 24, 2027. This can be extended by Supplementary Protection Certificates (SPCs) in individual member states, depending on the first marketing authorization.

2. Does EP1996266 cover agonists or antagonists of the α7 nAChR? EP1996266 specifically claims and describes the use of compounds as antagonists of the α7 nAChR.

3. What specific diseases are explicitly mentioned in the method of treatment claims of EP1996266? The patent explicitly mentions diseases such as schizophrenia, cognitive disorders associated with neurological or psychiatric disorders, inflammatory diseases, and neurodegenerative diseases. Specific sub-indications within these categories are detailed in the patent's claims and description.

4. Can a generic drug manufacturer launch a product that infringes EP1996266 before its expiry? No, launching a product that falls within the scope of the granted and validated claims of EP1996266 before its expiry (including any SPC extensions) would constitute patent infringement in the relevant European countries.

5. What is the significance of validation in individual European countries after EPO grant? After the EPO grants a European patent, it must be validated in each designated member state where the patent holder wishes to have protection. Validation involves translation of claims (and sometimes the full patent) and payment of national fees. The granted patent then has effect as a national patent in each validated state, and infringement actions are brought before national courts.

Citations

[1] European Patent EP1996266. (2007). AMIDES OF KYNURENIC ACID DERIVATIVES. European Patent Office.