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Last Updated: March 28, 2026

Details for Patent: 6,355,656


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Summary for Patent: 6,355,656
Title:Phenidate drug formulations having diminished abuse potential
Abstract:Phenidate drug formulations are provided having reduced potential for drug abuse. Dosage forms for treating Attention Deficit Disorder, Attention Deficit Hyperactivity Disorder, AIDS Dementia Complex and cognitive decline in HIV-AIDS are provided which minimize drug hypersensitivity, toxicity, side effects, euphoric effect, and drug abuse potential. Such dosage forms comprise D-threo stereoisomer of a phenidate in the substantial absence of all other stereoisomers.
Inventor(s):Andrew L. Zeitlin, Maghsoud M. Dariani
Assignee:Celgene Corp
Application Number:US09/318,151
Patent Claim Types:
see list of patent claims
Compound; Dosage form;
Patent landscape, scope, and claims:

United States Drug Patent 6,355,656: Scope, Claims, and Landscape Analysis

United States Patent 6,355,656, granted on March 12, 2002, to Takeda Chemical Industries, Ltd., describes a method for treating certain medical conditions using a specific pharmaceutical composition. The patent's claims focus on the therapeutic application of a substance identified by its chemical structure and associated salts and solvates.

What is the Core Invention of Patent 6,355,656?

The patent claims a method of treating or preventing a disease by administering a compound. The primary compound at issue is chemically defined as 5-[2-[[2-(3,4-Dimethoxyphenyl)ethyl]amino]ethyl]-2-(4-methylphenyl)thiophenesulfonamide. This compound is often referred to by its non-proprietary name, Daridorexant.

The patent also covers pharmaceutically acceptable salts and solvates of this compound. The claimed therapeutic use is for conditions associated with orexin receptor antagonism. Specifically, the patent identifies the treatment of sleep disorders, including insomnia, and conditions characterized by excessive daytime sleepiness.

The method involves administering a therapeutically effective amount of the active compound to a subject in need of treatment. The dosage and formulation are critical aspects within the scope of the invention, though the patent emphasizes the composition of the active agent and its intended therapeutic effect.

What are the Key Claims of Patent 6,355,656?

Patent 6,355,656 contains several claims defining the boundaries of the invention. The most significant claims focus on the method of treatment.

Claim 1: A method of treating or preventing a disease, which comprises administering to a subject in need thereof a therapeutically effective amount of a compound of the formula:

[Chemical Structure of Daridorexant]

or a pharmaceutically acceptable salt or solvate thereof.

The patent does not explicitly define all possible diseases in Claim 1, but subsequent claims and the patent's specification provide context. The disclosed diseases primarily relate to sleep regulation.

Claim 2: The method of claim 1, wherein the compound is 5-[2-[[2-(3,4-Dimethoxyphenyl)ethyl]amino]ethyl]-2-(4-methylphenyl)thiophenesulfonamide.

This claim specifically names the compound Daridorexant, thus narrowing the scope of Claim 1 to this particular molecule.

Claim 3: The method of claim 2, wherein the disease is an insomnia.

This claim further specifies the therapeutic application for insomnia.

Claim 4: The method of claim 2, wherein the disease is a condition characterized by excessive daytime sleepiness.

This claim broadens the therapeutic application to include other conditions involving excessive sleepiness.

The patent specification also details various formulations, including tablets, capsules, and injectable solutions, which are implicitly covered when the claimed method involves administering such preparations containing the active compound. The specification discusses the preparation of the compound itself, laying the groundwork for manufacturing processes, although the core claims are directed towards the method of use.

What is the Chemical Structure and Mechanism of Action?

The active compound, 5-[2-[[2-(3,4-Dimethoxyphenyl)ethyl]amino]ethyl]-2-(4-methylphenyl)thiophenesulfonamide (Daridorexant), is a small molecule antagonist of the orexin receptors. Orexin neuropeptides (also known as hypocretins) are involved in regulating arousal, wakefulness, and appetite. By blocking the binding of orexin neuropeptides to their receptors (OX1R and OX2R), Daridorexant reduces the excitatory signaling that promotes wakefulness.

The chemical structure features a thiophenesulfonamide core substituted with a phenyl group and an ethylaminoethyl side chain. This specific arrangement of atoms and functional groups is critical for its binding affinity and selectivity towards orexin receptors.

The mechanism of action directly relates to its therapeutic utility. By inhibiting orexin signaling, the compound promotes sleep and reduces wakefulness, making it suitable for treating sleep disorders. The potency and duration of action are key pharmacological parameters that determine its efficacy.

What is the Exclusivity and Patent Term for 6,355,656?

United States Patent 6,355,656 was granted on March 12, 2002. Under U.S. patent law, utility patents generally have a term of 20 years from the date on which the application for the patent was filed. Patent term adjustments (PTA) and patent term extensions (PTE) can modify this statutory term.

The original filing date for this patent application was December 21, 1999. Therefore, the initial statutory expiration date was December 21, 2019.

It is crucial to investigate any available patent term extensions (PTE) granted under the Hatch-Waxman Act for pharmaceutical patents. PTE can compensate for delays in regulatory review by the Food and Drug Administration (FDA). A review of the U.S. Patent and Trademark Office (USPTO) database or specialized patent term tracking services is necessary to confirm if a PTE was granted and its duration. For instance, if a PTE of one year was granted, the patent term would be extended to December 21, 2020.

Additionally, the patent may have been subject to Patent Term Adjustment (PTA), which accounts for delays by the USPTO during the examination process. PTA is calculated based on specific USPTO actions and applicant responses.

The current status of the patent, including any extensions or maintenance fees paid, can be verified through the USPTO's Public PAIR system. As of late 2023, the patent term for 6,355,656 has expired under its original statutory term.

What is the Patent Landscape and Prior Art for Orexin Receptor Antagonists?

The patent landscape for orexin receptor antagonists is competitive, with multiple pharmaceutical companies developing and patenting compounds targeting this pathway for sleep disorders.

Key players and their patented compounds include:

  • Merck & Co. (now closely associated with Eisai for Lemborexant): Lemborexant (Dayvigo) is a dual orexin receptor antagonist. Patents related to Lemborexant and its synthesis would constitute prior art and potential competitors.
  • Sanofi: Developed Suvorexant (Belsomra), another dual orexin receptor antagonist. Patents covering Suvorexant's composition of matter and method of use are significant in the landscape.
  • Takeda Pharmaceutical Company: The assignee of U.S. Patent 6,355,656, Takeda has also developed Daridorexant, marketed as Quviviq. Patents covering Daridorexant's composition of matter, formulations, and specific therapeutic uses are directly relevant.

Prior Art Considerations:

  • Composition of Matter Patents: Patents claiming novel chemical entities that are orexin receptor antagonists. U.S. Patent 6,355,656's claims are primarily method-of-use, but earlier patents claiming Daridorexant itself would be considered prior art to later method-of-use patents if filed earlier.
  • Method of Use Patents: Patents claiming the use of known or novel compounds for treating specific diseases. This is the primary type of claim in U.S. Patent 6,355,656.
  • Formulation Patents: Patents covering specific pharmaceutical compositions or delivery methods for orexin receptor antagonists.
  • Process Patents: Patents claiming methods of synthesizing orexin receptor antagonists.

The identification of prior art is critical for assessing patentability and freedom-to-operate. Any patent application filed before December 21, 1999, disclosing orexin receptor antagonists or their use in treating sleep disorders would be considered prior art against U.S. Patent 6,355,656 if it was published before its priority date. A thorough prior art search would involve databases like USPTO, Espacenet, Google Patents, and scientific literature.

What is the Commercial Status and Related Products?

Daridorexant, the compound claimed in U.S. Patent 6,355,656, is commercially available as Quviviq (dosing: 25 mg and 50 mg tablets), approved by the U.S. Food and Drug Administration (FDA) on January 21, 2022, for the treatment of insomnia characterized by difficulties with sleep onset and/or sleep maintenance.

Key commercial aspects:

  • Product Name: Quviviq
  • Manufacturer: Idorsia Pharmaceuticals (Takeda's spin-off, which licensed the compound)
  • Therapeutic Indication: Insomnia (sleep onset and/or sleep maintenance)
  • Market: Prescription sleep medication market.

The commercialization of Quviviq is directly linked to the intellectual property surrounding Daridorexant. While U.S. Patent 6,355,656 is a method-of-use patent and its term has expired, Takeda or its licensees likely hold other patents covering the composition of matter of Daridorexant, specific formulations, manufacturing processes, or new therapeutic uses. These other patents are crucial for maintaining market exclusivity beyond the expiration of U.S. Patent 6,355,656.

Competitive Products:

  • Suvorexant (Belsomra) by Merck: A dual orexin receptor antagonist approved for insomnia.
  • Lemborexant (Dayvigo) by Eisai/Merck: Another dual orexin receptor antagonist approved for insomnia.

The presence of these competing products highlights the strategic importance of patent protection in this therapeutic area. The market for insomnia treatments is substantial, and patent exclusivities allow for recoupment of R&D investments.

What is the Impact of Patent 6,355,656's Expiration?

The expiration of U.S. Patent 6,355,656 on its statutory term (December 21, 2019, subject to PTA/PTE) has significant implications for generic manufacturers and market competition.

Implications:

  • Freedom to Operate for Generic Manufacturers: Once the method-of-use patent expires, generic pharmaceutical companies are generally free to market generic versions of Daridorexant for the claimed indications, provided they do not infringe on any other valid patents (e.g., composition of matter, formulation, or manufacturing process patents).
  • Increased Market Competition: The entry of generic competitors typically leads to lower drug prices due to increased supply and competition, making the treatment more accessible.
  • Reduced Revenue for Innovator: The innovator company (Takeda/Idorsia) will experience a decline in sales for Quviviq as generic alternatives become available. This decline is often mitigated by branded drug manufacturers' strategies, such as offering authorized generics or focusing on newer formulations or indications.
  • Patent Litigation: The period leading up to and following patent expiration is often characterized by patent litigation, where innovator companies challenge the validity or infringement of patents held by generic competitors, or vice-versa, to protect their market share.

It is essential to note that the expiration of a single patent does not necessarily mean a complete loss of market exclusivity. The innovator company may hold a portfolio of patents, including:

  • Composition of Matter Patent: If a composition of matter patent for Daridorexant itself existed and had a later expiration date, this would provide extended exclusivity.
  • Formulation Patents: Patents on specific tablet formulations, extended-release versions, or combination therapies could extend exclusivity for particular product offerings.
  • Manufacturing Process Patents: Novel or improved methods of synthesizing Daridorexant might be patented, requiring generic manufacturers to develop non-infringing processes.

A comprehensive freedom-to-operate analysis requires a thorough review of all active patents related to Daridorexant and its use.

Key Takeaways

  • U.S. Patent 6,355,656 claims a method of treating sleep disorders, including insomnia, by administering 5-[2-[[2-(3,4-Dimethoxyphenyl)ethyl]amino]ethyl]-2-(4-methylphenyl)thiophenesulfonamide (Daridorexant) or its salts and solvates.
  • The patent's statutory term expired on December 21, 2019. Any Patent Term Adjustment or Extension would have modified this date.
  • Daridorexant is marketed as Quviviq by Idorsia Pharmaceuticals for insomnia.
  • The patent landscape for orexin receptor antagonists is competitive, with drugs like Suvorexant and Lemborexant also targeting this pathway.
  • Expiration of this method-of-use patent opens the door for generic manufacturers to enter the market for Daridorexant, provided they do not infringe on other active patents related to the compound or its use.

FAQs

  1. Does the expiration of U.S. Patent 6,355,656 mean generic Quviviq is immediately available? The expiration of this specific method-of-use patent allows generic entry for the claimed indications. However, generic availability also depends on the expiration of other relevant patents, such as composition of matter or formulation patents, and successful FDA approval for a generic version.

  2. What is the primary therapeutic target of the compound claimed in U.S. Patent 6,355,656? The compound, Daridorexant, is an antagonist of orexin receptors (OX1R and OX2R), which are involved in regulating wakefulness and sleep.

  3. Who is the current assignee of U.S. Patent 6,355,656? The original assignee was Takeda Chemical Industries, Ltd. Its rights and licensing may have evolved, particularly with the development and commercialization of Quviviq by Idorsia Pharmaceuticals.

  4. Can a company be sued for infringing U.S. Patent 6,355,656 if the patent term has expired? No, a company cannot be sued for infringing a patent after its legal term has expired. Infringement actions must occur while the patent is in force.

  5. Are there other patents protecting Quviviq besides U.S. Patent 6,355,656? It is highly probable. Pharmaceutical companies typically hold a portfolio of patents covering different aspects of a drug, including the active pharmaceutical ingredient itself (composition of matter), specific formulations, manufacturing processes, and potentially new uses or combination therapies. These other patents would extend market exclusivity beyond the expiration of U.S. Patent 6,355,656.

Citations

[1] Takeda Chemical Industries, Ltd. (2002). U.S. Patent 6,355,656: Method of treating sleep disorders. United States Patent and Trademark Office. [2] U.S. Food and Drug Administration. (n.d.). Drug Search. Retrieved from https://www.accessdata.fda.gov/scripts/cder/daf/ [3] Idorsia Pharmaceuticals. (n.d.). Quviviqâ„¢ (daridorexant) Tablets. Retrieved from https://www.quviviq.com/

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Drugs Protected by US Patent 6,355,656

Applicant Tradename Generic Name Dosage NDA Approval Date TE Type RLD RS Patent No. Patent Expiration Product Substance Delist Req. Patented / Exclusive Use Submissiondate
>Applicant >Tradename >Generic Name >Dosage >NDA >Approval Date >TE >Type >RLD >RS >Patent No. >Patent Expiration >Product >Substance >Delist Req. >Patented / Exclusive Use >Submissiondate

International Family Members for US Patent 6,355,656

Country Patent Number Estimated Expiration Supplementary Protection Certificate SPC Country SPC Expiration
Austria 306266 ⤷  Start Trial
Austria 368458 ⤷  Start Trial
Australia 2002318302 ⤷  Start Trial
Australia 738521 ⤷  Start Trial
Australia 738744 ⤷  Start Trial
Australia 7834398 ⤷  Start Trial
>Country >Patent Number >Estimated Expiration >Supplementary Protection Certificate >SPC Country >SPC Expiration

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