Detailed Analysis of the Scope and Claims of United States Patent 9,193,732
Introduction
The United States Patent 9,193,732, titled "Salt(s) of 7-cyclopentyl-2-(5-piperazin-1-yl-pyridin-2-ylamino)-7H-pyrrolo[2,3-d]pyrimidine-6-carboxylic acid dimethylamide and processes of making thereof," is a critical patent in the pharmaceutical industry, particularly for the drug ribociclib, marketed as Kisqali by Novartis. This patent is central to the production and use of ribociclib, a kinase inhibitor used in the treatment of certain types of cancer.
Background of Ribociclib
Ribociclib is a selective inhibitor of cyclin-dependent kinases 4 and 6 (CDK4/6), which are crucial for cell cycle progression. It is primarily used in combination with other therapies for the treatment of hormone receptor-positive, human epidermal growth factor receptor 2 (HER2)-negative advanced or metastatic breast cancer[4].
Patent Overview
Issuance and Assignee
The patent was issued on November 17, 2015, and is assigned to Novartis AG. It covers the salts of 7-cyclopentyl-2-(5-piperazin-1-yl-pyridin-2-ylamino)-7H-pyrrolo[2,3-d]pyrimidine-6-carboxylic acid dimethylamide, specifically the succinate salt, and the processes for their preparation[4].
Claims
The patent includes several claims that define the scope of the invention. Here are some key claims:
Claim 1
Claim 1 describes the succinate salt of ribociclib, which is characterized by its specific chemical structure and properties. This claim is foundational as it defines the primary compound covered by the patent[4].
Claim 9
Claim 9 is particularly significant as it pertains to pharmaceutical compositions comprising a therapeutically effective amount of the succinate salt of ribociclib. This claim is crucial for the commercial use of the drug, as it covers the formulation and dosage forms of Kisqali[2].
Processes of Preparation
The patent also details the processes for preparing the succinate salt of ribociclib. These processes include various methods for synthesizing the compound, which are essential for ensuring the quality and consistency of the drug[4].
Solid State Forms
The patent emphasizes the importance of solid state forms of ribociclib succinate, including crystalline and solvated forms. These forms are critical for the stability, bioavailability, and efficacy of the drug. For instance, the crystalline form B of ribociclib succinate is characterized by specific X-ray powder diffraction peaks, which ensure its purity and effectiveness[1].
Patent Landscape
Related Patents
Several other patents are related to ribociclib and its uses. For example:
- Patent 8,324,225: This patent describes pyrrolopyrimidine compounds, including ribociclib, and their use in treating proliferative diseases. It expires on June 17, 2028[5].
- Patent 9,868,739: This patent covers additional salts of ribociclib and their processes of preparation, further expanding the patent protection for Novartis[5].
Patent Expiration Dates
The expiration dates of these patents are crucial for understanding the timeline of generic competition. The key patent (US 9,193,732) expires in 2035, but other related patents have different expiration dates, such as June 17, 2028, and November 9, 2031[5].
Litigation and Generic Competition
The patent has been at the center of several legal battles, particularly with generic manufacturers seeking to enter the market before the patent expires. For example, Natco Pharma has filed an Abbreviated New Drug Application (ANDA) with the FDA, which Novartis argues infringes on the claims of the '732 patent and the '739 patent[2].
Impact on Innovation and Competition
The scope and claims of this patent have significant implications for innovation and competition in the pharmaceutical industry. The patent system is designed to balance the need for innovation with the need for competition. However, overly broad or unclear claims can stifle innovation by increasing licensing and litigation costs[3].
Conclusion
The United States Patent 9,193,732 is a pivotal patent in the pharmaceutical landscape, particularly for the treatment of breast cancer. Its claims and scope define the legal boundaries for the production and use of ribociclib, influencing both innovation and generic competition.
Key Takeaways
- The patent covers the succinate salt of ribociclib and its processes of preparation.
- Claim 9 is crucial for pharmaceutical compositions of ribociclib.
- Solid state forms, including crystalline form B, are essential for the drug's stability and efficacy.
- Related patents and their expiration dates shape the patent landscape.
- Litigation with generic manufacturers highlights the patent's significance in protecting Novartis's market position.
FAQs
Q: What is the primary compound covered by US Patent 9,193,732?
A: The primary compound is the succinate salt of 7-cyclopentyl-2-(5-piperazin-1-yl-pyridin-2-ylamino)-7H-pyrrolo[2,3-d]pyrimidine-6-carboxylic acid dimethylamide.
Q: What is the significance of Claim 9 in the patent?
A: Claim 9 pertains to pharmaceutical compositions comprising a therapeutically effective amount of the succinate salt of ribociclib, which is crucial for the commercial use of the drug.
Q: Why are solid state forms important for ribociclib succinate?
A: Solid state forms, including crystalline and solvated forms, are critical for the stability, bioavailability, and efficacy of the drug.
Q: What are the related patents to US 9,193,732?
A: Related patents include US 8,324,225 and US 9,868,739, which cover other aspects of ribociclib and its uses.
Q: When does the key patent (US 9,193,732) expire?
A: The key patent is expected to expire in 2035, although exact dates may vary based on extensions or additional periods of exclusivity.
Sources
- European Patent Office, "SOLID STATE FORM OF RIBOCICLIB SUCCINATE - EP 3672968 B1," November 1, 2023.
- United States District Court, "Case 1:24-cv-01033-UNA Document 1 Filed 09/13/24," September 13, 2024.
- Hoover Institution, "Patent Claims and Patent Scope," August 18, 2024.
- Google Patents, "US9193732B2 - Salt(s) of 7-cyclopentyl-2-(5-piperazin-1-yl-pyridin-2-ylamino)-7H-pyrrolo[2,3-d]pyrimidine-6-carboxylic acid dimethylamide and processes of making thereof."
- Drugs.com, "Generic Kisqali Availability," November 6, 2024.
