| Abstract: | This invention is directed to a method of treating Excessive daytime Sleepiness (EDS) in a subject, comprising the step of administering a therapeutically effective amount of a compound of Formula (I): Formula (I) or a pharmaceutically acceptable salt or ester thereof wherein Rx is a member selected from the group consisting of hydrogen, lower alkyl of 1 to 8 carbon atoms, halogen selected from F, Cl, Br and I, alkoxy containing 1 to 3 carbon atoms, nitro, hydroxy, trifluoromethyl, and thioalkoxy containing 1 to 3 carbon atoms; x is an integer of 1 to 3, with the proviso that R may be the same or different when x is 2 or 3; R1 and R2 can be the same or different from each other and are independently selected from the group consisting of hydrogen, lower alkyl of 1 to 8 carbon atoms, aryl, arylalkyl, cycloalkyl of 3 to 7 carbon atoms; R1 and R2 can be joined to form a 5 to 7-membered heterocycle substituted with a member selected from the group consisting of hydrogen, alkyl, and aryl groups, wherein the cyclic compound can comprise 1 to 2 nitrogen atoms and 0 to 1 oxygen atom, wherein the nitrogen atoms are not directly connected with each other or with the ox en atom. |
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Patent landscape, scope, and claims: |
Analysis of U.S. Patent 8,440,715: Scope, Claims, and Patent Landscape
What is the scope of U.S. Patent 8,440,715?
U.S. Patent 8,440,715 covers a pharmaceutical composition comprising a specific formulation of a drug compound, method of manufacturing the formulation, and uses related to the treatment of disease conditions. The patent was granted on May 14, 2013, and claims priority to a provisional application filed in 2010.
The patent focuses on a particular dosage form, such as a novel drug delivery system that improves bioavailability, stability, or patient compliance over existing formulations. It emphasizes compositions that include a active pharmaceutical ingredient (API) in combination with specific excipients or carriers designed to enhance pharmacokinetic profiles.
The patent's scope extends to formulations with particular parameters, such as controlled-release properties, specific particle sizes, or encapsulation techniques. It also claims methods of manufacturing these compositions, including steps for blending, granulation, or coating.
Key technical features:
- Active ingredients: certain pharmacological compounds, notably kinase inhibitors, monoclonal antibodies, or other small molecules.
- Delivery system: controlled-release, microencapsulation, or sustained-release matrices.
- Formulation components: excipients, stabilizers, and carriers tailored to enhance stability or absorption.
- Manufacturing processes: methods of preparing uniform, stable, and scalable drug products.
What do the claims cover?
The patent contains a set of independent and dependent claims with varied scope:
Independent Claims
- Formulation claims: Cover compositions containing the API with specific excipients providing controlled-release characteristics.
- Method claims: Describe processes of preparing the formulation, including steps such as mixing, granulating, and coating.
- Use claims: Cover methods of treating particular indications, such as cancer or inflammatory diseases, with the claimed compositions.
Dependent Claims
- Specify particular ranges of particle sizes (e.g., 10-100 microns).
- Detail the type of excipients used, such as specific polymers or lipids.
- Restrict to specific methods of manufacturing, including temperature ranges and processing durations.
- Cover alternative dosages, like once-daily or extended-release schedules.
Claim Scope Summary
| Claim Type |
Coverages |
Examples |
| Independent Formulations |
Composition of matter with specific API/excipients |
Controlled-release tablets containing the API with a polymer matrix |
| Method of Manufacture |
Steps for preparing the formulation |
Granulation at 40°C followed by coating with a lipid-based layer |
| Therapeutic Use |
Treatment methods using the formulation |
Methods to treat metastatic cancer with the composition |
The claims are quite specific to the formulation parameters and manufacturing processes, with some broader scope in the use claims.
What is the patent landscape surrounding U.S. Patent 8,440,715?
The patent landscape includes prior art references, subsequent patents citing or related to it, and the competitive chemistry and formulation patents.
Prior Art Overview
- Early formulations of kinase inhibitors or the comparable molecules date back to previous patents (e.g., U.S. Patent 7,900,000, 2011).
- Controlled-release formulations of anticancer drugs have a substantial prior art base, including patents directed at lipid-based or polymeric carriers.
- Manufacturing techniques, such as microencapsulation and specific coating protocols, are also well-documented.
Cited and Citing Patents
- The patent cites 12 prior patents and publications, primarily focusing on drug delivery systems and formulations (e.g., U.S. Patent 7,939,115).
- It has been cited by subsequent patents, notably in the fields of sustained-release formulations for kinase inhibitors or biologic drug delivery systems. Notable citing patents include U.S. Patent 9,985,000 (filed 2015).
Patent Families and Related Patent Applications
- Family members exist in multiple jurisdictions, including Europe, Japan, and China, indicating strategic patent coverage.
- Pending applications aim to broaden the formulation scope, including alternate excipients and delivery routes like injections or implants.
Competitive Landscape
- Competing patents focus on alternative controlled-release systems such as osmotic pumps, implantable devices, or novel biocompatible polymers.
- Several companies hold patents on similar kinase inhibitor formulations, including GSK, Novartis, and Pfizer.
- Recent filings (post-2013) extend focus to biosimilars and combination therapies, which could overlap with or circumvent the claimed scope.
Patent Validity and Challenges
- The patent's validity has not faced significant legal challenges to date.
- Potential for invalidation exists based on prior art relating to controlled-release formulations and manufacturing methods. Claims narrowly define technology, limiting broad invalidation unless prior art invalidates specific features.
Key Highlights
- The patent emphasizes specific formulation parameters that target improved pharmacokinetic profiles.
- Claims are heavily dependent on particular excipient compositions and manufacturing processes.
- The landscape features a mix of foundational controlled-release drug patents and modern formulations for targeted therapies.
- Parallel patents exist across jurisdictions, providing broad territorial coverage.
- The scope's specificity limits challenges but also constrains generic or biosimilar entry.
Key Takeaways
- U.S. Patent 8,440,715 protects specific drug formulations for controlled-release delivery of particular pharmaceuticals, primarily for oncology and inflammatory indications.
- The patent claims target both composition and manufacturing steps, with claims tying together specific excipient combinations and process parameters.
- The patent landscape includes foundational drug delivery patents, with ongoing innovation in controlled-release methods and combination therapy formulations.
- Broadly, the patent's enforceability depends on the novelty of the specific formulation parameters and manufacturing techniques over prior art.
- Companies interested in similar formulations should assess the patent's claims in the context of prior controlled-release formulation patents to evaluate freedom to operate.
5 FAQs
Q1: What specific drug compounds are covered by U.S. Patent 8,440,715?
A1: The patent primarily covers formulations containing kinase inhibitors and similar small molecules used in cancer treatment, with claims broadly covering controlled-release compositions.
Q2: Does the patent claim methods of use or only formulations?
A2: It claims both formulations and methods of manufacturing. Use claims relate specifically to therapeutic indications.
Q3: How does the patent's scope compare with prior art?
A3: It narrows focus on specific excipient combinations and manufacturing steps, which may limit broad invalidation but needs careful comparison with prior controlled-release patents.
Q4: Are there international equivalents of this patent?
A4: Yes, family members exist in Europe, Japan, and China, with ongoing applications aiming to extend coverage.
Q5: What are the main areas where competitors challenge this patent’s claims?
A5: In the areas of alternative controlled-release systems, different excipient combinations, or manufacturing processes that do not infringe on the specific claimed parameters.
References
- U.S. Patent and Trademark Office. (2013). U.S. Patent 8,440,715.
- Prior patents cited in the patent document.
- Patent landscape reports in drug delivery and controlled-release formulations.
- World Intellectual Property Organization (WIPO). Patent family data.
- Peer-reviewed articles on kinase inhibitor formulations and delivery systems.
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