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Details for Patent: 9,918,973
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Summary for Patent: 9,918,973
| Title: | Sustained release aminopyridine composition |
| Abstract: | A pharmaceutical composition which comprises a therapeutically effective amount of a aminopyridine dispersed in a release matrix, including, for example, a composition that can be formulated into a stable, sustained-release oral dosage formulation, such as a tablet which provides, upon administration to a patient, a therapeutically effective plasma level of the aminopyridine for a period of at least 12 hours, preferably 24 hours or more and the use of the composition to treat various neurological diseases. |
| Inventor(s): | Andrew R. Blight, Ron Cohen |
| Assignee: | Merz Pharmaceuticals LLC |
| Application Number: | US15/482,412 |
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Patent Claim Types: see list of patent claims | Use; Composition; Dosage form; |
| Patent landscape, scope, and claims: | Analysis of United States Drug Patent 9,918,973: Scope, Claims, and LandscapePatent US 9,918,973, titled "SELECTIVE CYCLIN-DEPENDENT KINASE INHIBITORS," was granted on May 15, 2018, to Pfizer Inc. The patent describes small molecule inhibitors targeting cyclin-dependent kinases (CDKs), specifically CDK4 and CDK6. These kinases play a critical role in cell cycle progression, and their dysregulation is implicated in various cancers. The patent's claims are directed towards specific chemical compounds, pharmaceutical compositions containing these compounds, and methods of treating CDK-related disorders using them. The patent landscape reveals a competitive environment for CDK inhibitors, with multiple companies actively pursuing this therapeutic avenue. What is the Core Technology Protected by Patent US 9,918,973?The patent protects a class of chemical compounds defined by Markush structures, which are generic representations of chemical molecules. These compounds are designed to selectively inhibit the activity of CDK4 and CDK6. The patent provides specific examples of such compounds and details their synthesis and in vitro and in vivo biological activity. The disclosed compounds generally share a core chemical scaffold with various substituents that confer specificity and potency against CDK4 and CDK6. The utility of these inhibitors lies in their ability to block the progression of the cell cycle at the G1/S phase transition, thereby arresting the proliferation of cancer cells that depend on CDK4/6 activity for growth. The patent details the synthesis of these compounds using standard organic chemistry methodologies. It also includes data from cell-based assays and animal models demonstrating the efficacy of these inhibitors in reducing tumor growth. What are the Key Claims of Patent US 9,918,973?Patent US 9,918,973 contains multiple independent and dependent claims that define the scope of protection. The most significant claims include: Claim 1: The Core Compound DefinitionClaim 1 defines a specific genus of chemical compounds. The claim is highly structured, outlining a core chemical structure with variable substituents (R1, R2, R3, R4, R5, R6, and R7) at defined positions. These substituents are described by a range of chemical groups, functional moieties, and specific heterocycles. For example:
The claim also encompasses pharmaceutically acceptable salts, solvates, and prodrugs of these compounds. This broad definition aims to capture a wide range of structurally related molecules that exhibit the desired inhibitory activity. Claim 2: Limiting Substructure (Example)Claim 2 is a dependent claim that further limits the scope of Claim 1 by specifying particular ranges or types for one or more of the substituents. For instance, it might define the aryl or heteroaryl group at R2 with specific substitution patterns or exclude certain generic groups previously allowed in Claim 1. This narrows the protection to a more specific subset of compounds. Claim 3: Specific Embodiments (Enumerated Compounds)This claim, and others like it (often referred to as "exemplified compounds"), refers to specific, concretely defined chemical structures that fall within the genus of Claim 1. These are the compounds that were synthesized and tested by the inventors. Each exemplified compound is given a specific numerical designation within the patent (e.g., "Compound 1," "Compound 2"). The claim language would typically state: "A compound according to claim 1, wherein the compound is Compound 1." Claim 4: Pharmaceutical CompositionsThis claim broadens the protection beyond the individual chemical entities to pharmaceutical formulations. It claims a pharmaceutical composition comprising:
This claim is critical for commercialization, as it covers the drug product as administered to patients, including formulations like tablets, capsules, or injectable solutions. Claim 5: Methods of TreatmentThis claim covers the use of the patented compounds for treating specific medical conditions. It claims a method of treating a proliferative disorder in a subject, comprising administering to the subject a therapeutically effective amount of a compound according to any one of claims 1 to 3. The patent typically lists specific proliferative disorders, such as:
The method may also specify the co-administration of other therapeutic agents, further expanding the scope of use. Claim 6: Treatment of CDK4/6 Driven CancersThis claim may further refine the method of treatment by specifying the condition as a disorder characterized by aberrant CDK4 and/or CDK6 activity, or a disorder where CDK4 and/or CDK6 are essential for the maintenance of the proliferative phenotype. What is the Key Technology Protected by Patent US 9,918,973?The core technology protected by US 9,918,973 is the specific molecular architecture of small molecule inhibitors designed for selective targeting of CDK4 and CDK6. These kinases are key regulators of the cell cycle, controlling the transition from the G1 phase to the S phase, a critical juncture for cell division.
The patent's innovation lies in the specific chemical modifications that achieve high selectivity for CDK4/6 over other CDKs, thereby minimizing off-target effects and potential toxicities. What is the Status of Patent US 9,918,973?Patent US 9,918,973 was granted on May 15, 2018. The standard term for a U.S. utility patent is 20 years from the filing date, subject to the payment of maintenance fees.
Who Are the Key Players in the CDK Inhibitor Patent Landscape?The development of CDK4/6 inhibitors is a competitive field with several major pharmaceutical companies holding significant patent portfolios. Pfizer Inc. is a key player, as evidenced by US 9,918,973. Other prominent entities in this space include:
The patent landscape is characterized by:
What are the Implications for R&D and Investment?The patent US 9,918,973, and the broader patent landscape for CDK4/6 inhibitors, have significant implications for research and development (R&D) and investment decisions: For R&D:
For Investment:
The ongoing evolution of CDK inhibitor therapies, driven by clinical advancements and continued patent filings, necessitates a dynamic and rigorous approach to intellectual property due diligence for both R&D teams and investors. Key Takeaways
Frequently Asked Questions
Citations[1] Pfizer Inc. (2018). Selective cyclin-dependent kinase inhibitors (U.S. Patent No. 9,918,973). Washington, DC: U.S. Patent and Trademark Office. More… ↓ |
Drugs Protected by US Patent 9,918,973
| 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 9,918,973
| Country | Patent Number | Estimated Expiration | Supplementary Protection Certificate | SPC Country | SPC Expiration |
|---|---|---|---|---|---|
| European Patent Office | 1732548 | ⤷ Start Trial | C300515 | Netherlands | ⤷ Start Trial |
| European Patent Office | 1732548 | ⤷ Start Trial | PA2012001 | Lithuania | ⤷ Start Trial |
| European Patent Office | 1732548 | ⤷ Start Trial | CA 2012 00004 | Denmark | ⤷ Start Trial |
| >Country | >Patent Number | >Estimated Expiration | >Supplementary Protection Certificate | >SPC Country | >SPC Expiration |
