Details for Patent: 9,868,739

Which drugs does patent 9,868,739 protect, and when does it expire?

Patent 9,868,739 protects KISQALI and KISQALI FEMARA CO-PACK (COPACKAGED) and is included in two NDAs.

This patent has forty-four patent family members in twenty-five countries.

Summary for Patent: 9,868,739

Title:	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
Abstract:	This invention relates to (1) process of making 7-Cyclopentyl-2-(5-piperazin-1-yl-pyridin-2-ylamino)-7H-pyrrolo[2,3-d]pyr- imidine-6-carboxylic acid dimethylamide and salt(s) thereof; (2) novel salt(s) of 7-Cyclopentyl-2-(5-piperazin-1-yl-pyridin-2-ylamino)-7H-pyrrolo[2,3-d]pyr- imidine-6-carboxylic acid dimethylamide; (3) pharmaceutical compositions comprising the same; and (4) methods of treatment using the same.
Inventor(s):	Calienni; John Vincent (Cranford, NJ), Chen; Guang-Pei (Livingston, NJ), Gong; Baoqing (Morris Plains, NJ), Kapa; Prasad Koteswara (Parsippany, NJ), Saxena; Vishal (Quincy, MA)
Assignee:	Novartis AG (Basel, CH)
Application Number:	14/887,790
Patent Litigation and PTAB cases:	See patent lawsuits and PTAB cases for patent 9,868,739
Patent Claim Types: see list of patent claims	Use;

United States Patent 9,868,739: A Detailed Analysis of Scope, Claims, and Patent Landscape

Introduction

The United States Patent 9,868,739, 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 significant patent in the pharmaceutical sector, particularly in the treatment of cancer. This analysis will delve into the scope, claims, and the broader patent landscape surrounding this invention.

Background of the Invention

The patent pertains to a specific compound, 7-cyclopentyl-2-(5-piperazin-1-yl-pyridin-2-ylamino)-7H-pyrrolo[2,3-d]pyrimidine-6-carboxylic acid dimethylamide, which is a salt form of the drug ribociclib. Ribociclib is a selective cyclin-dependent kinase inhibitor used in the treatment of certain types of breast cancer[4].

Scope of the Patent

The scope of the patent encompasses the salt forms of the compound, as well as the processes for their manufacture. Here are the key aspects:

Salt Forms

The patent describes various salt forms of the compound, which are crucial for pharmaceutical applications due to their improved stability, solubility, and bioavailability. These salt forms include, but are not limited to, dimethylamide salts[1].

Manufacturing Processes

The patent details the methods for synthesizing these salt forms, including the specific chemical reactions and conditions required. This is vital for ensuring the consistency and quality of the final product[1].

Claims of the Patent

The claims of the patent are the legal boundaries that define what is protected under the patent. Here are some key claims:

Claim 1: Composition

Claim 1 typically describes the composition of the salt forms of the compound, specifying the chemical structure and the types of salts covered[1].

Claim 9: Pharmaceutical Composition

This claim, as mentioned in related litigation documents, pertains to a pharmaceutical composition comprising a therapeutically effective amount of the salt according to the patent. This claim is critical for the commercial use of the drug in medical treatments[2].

Patent Landscape

The patent landscape surrounding US 9,868,739 is complex and involves several related patents and legal disputes.

Related Patents

Several patents are associated with the same class of compounds and their uses:

• US 8,324,225: This patent, issued in 2012, describes pyrrolopyrimidine compounds and their derivatives useful for treating proliferative diseases. It sets a foundational framework for later patents, including US 9,868,739[5].
• US 9,193,732: This patent, also related to ribociclib, is involved in ongoing litigation regarding generic versions of the drug[2].

Patent Expiration Dates

Understanding the expiration dates of these patents is crucial for determining the timeline of exclusivity:

• US 8,324,225: Expires on June 17, 2028[5].
• US 9,193,732: Expires on November 9, 2031[2].
• US 9,868,739: Expires on January 16, 2031[1].

Litigation and Generic Versions

The patent is currently involved in litigation related to generic versions of ribociclib. Companies like Natco Pharma are seeking FDA approval for generic ribociclib tablets, which Novartis and Astex Therapeutics argue would infringe on the claims of US 9,868,739 and other related patents[2].

Impact on Innovation and Competition

The scope and claims of US 9,868,739 have significant implications for innovation and competition in the pharmaceutical industry.

Innovation

The patent's focus on specific salt forms and manufacturing processes encourages innovation in drug development by protecting novel and non-obvious inventions. However, overly broad claims can sometimes stifle innovation by limiting the ability of other researchers to work in the same area[3].

Competition

The litigation surrounding generic versions highlights the competitive landscape. The protection offered by the patent ensures that the original inventors and patent holders can recoup their investment in research and development. However, it also delays the entry of generic competitors, which can affect drug prices and accessibility[2].

Metrics for Patent Scope

To understand the scope of US 9,868,739 better, metrics such as independent claim length and independent claim count can be used. These metrics help in assessing the breadth and clarity of the patent claims:

• Independent Claim Length: Shorter independent claims often indicate narrower and more specific claims, which are associated with a higher probability of grant and shorter examination processes[3].
• Independent Claim Count: A lower number of independent claims can suggest a more focused and less broad patent scope[3].

Conclusion

The United States Patent 9,868,739 is a critical patent in the field of cancer treatment, particularly for the drug ribociclib. Its scope and claims define the legal boundaries for the use and manufacture of specific salt forms of the compound. The patent landscape, including related patents and ongoing litigation, highlights the complex interplay between innovation, competition, and intellectual property protection.

Key Takeaways

• Compound and Salt Forms: The patent covers specific salt forms of ribociclib, a cyclin-dependent kinase inhibitor.
• Manufacturing Processes: Detailed methods for synthesizing these salt forms are provided.
• Claims: Key claims include the composition and pharmaceutical use of the salt forms.
• Patent Landscape: Related patents and litigation impact the exclusivity and competition in the market.
• Metrics for Patent Scope: Independent claim length and count can help assess the breadth and clarity of the patent.

FAQs

Q: What is the primary compound covered by US 9,868,739?

A: The primary compound is 7-cyclopentyl-2-(5-piperazin-1-yl-pyridin-2-ylamino)-7H-pyrrolo[2,3-d]pyrimidine-6-carboxylic acid dimethylamide, a salt form of ribociclib.

Q: What is the therapeutic use of the compound?

A: The compound is used in the treatment of certain types of breast cancer by inhibiting cyclin-dependent kinases.

Q: Are there generic versions of ribociclib available?

A: As of now, there are no therapeutically equivalent generic versions of ribociclib available in the United States due to ongoing patent protection and litigation[5].

Q: What are the key metrics for assessing patent scope?

A: Independent claim length and independent claim count are used to assess the breadth and clarity of patent claims[3].

Q: What is the current status of litigation related to US 9,868,739?

A: The patent is involved in litigation with companies seeking FDA approval for generic versions of ribociclib, which the original patent holders argue would infringe on their patent claims[2].

Sources

1. US9868739B2 - 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 - Google Patents
2. Case 1:24-cv-01033-UNA Document 1 Filed 09/13/24 - Insight.RPXCorp
3. Patent Claims and Patent Scope - Hoover Institution
4. Ribociclib: Uses, Interactions, Mechanism of Action - DrugBank Online
5. Generic Kisqali Availability - Drugs.com

Drugs Protected by US Patent 9,868,739

Applicant	Tradename	Generic Name	Dosage	NDA	Approval Date	TE	Type	RLD	RS	Patent No.	Patent Expiration	Product	Substance	Delist Req.	Patented / Exclusive Use	Submissiondate
Novartis	KISQALI	ribociclib succinate	TABLET;ORAL	209092-001	Mar 13, 2017		RX	Yes	Yes						IN COMBINATION WITH AN AROMATASE INHIBITOR FOR THE TREATMENT OF PRE/PERIMENOPAUSAL OR POSTMENOPAUSAL WOMEN WITH HR-POSITIVE, HER2-NEGATIVE ADVANCED OR METASTATIC BREAST CANCER, AS INITIAL ENDOCRINE-BASED THERAPY
Novartis	KISQALI	ribociclib succinate	TABLET;ORAL	209092-001	Mar 13, 2017		RX	Yes	Yes						IN COMBINATION WITH FULVESTRANT FOR THE TREATMENT OF POSTMENOPAUSAL WOMEN WITH HR-POSITIVE, HER2-NEGATIVE ADVANCED OR METASTATIC BREAST CANCER, AS INITIAL ENDOCRINE BASED THERAPY OR FOLLOWING DISEASE PROGRESSION ON ENDOCRINE THERAPY
Novartis	KISQALI	ribociclib succinate	TABLET;ORAL	209092-001	Mar 13, 2017		RX	Yes	Yes						IN COMBINATION WITH AN AROMATASE INHIBITOR FOR THE ADJUVANT TREATMENT OF ADULTS WITH HORMONE RECEPTOR (HR)-POSITIVE, HUMAN EPIDERMAL GROWTH FACTOR RECEPTOR 2 (HER2)-NEGATIVE STAGE II AND III EARLY BREAST CANCER AT HIGH RISK OF RECURRENCE
Novartis	KISQALI	ribociclib succinate	TABLET;ORAL	209092-001	Mar 13, 2017		RX	Yes	Yes						IN COMBINATION WITH AN AROMATASE INHIBITOR AS INITIAL ENDOCRINE-BASED THERAPY FOR TREATMENT OF POSTMENOPAUSAL WOMEN WITH HORMONE RECEPTOR (HR)-POSITIVE, HUMAN EPIDERMAL GROWTH FACTOR RECEPTOR 2 (HER-2)-NEGATIVE ADVANCED OR METASTATIC BREAST CANCER
Novartis	KISQALI	ribociclib succinate	TABLET;ORAL	209092-001	Mar 13, 2017		RX	Yes	Yes						IN COMBINATION WITH FULVESTRANT AS INITIAL ENDOCRINE-BASED THERAPY OR FOLLOWING DISEASE PROGRESSION ON ENDOCRINE THERAPY, FOR THE TREATMENT OF ADULT PATIENTS WITH HR-POSITIVE, HER2-NEGATIVE ADVANCED OR METASTATIC BREAST CANCER
Novartis	KISQALI	ribociclib succinate	TABLET;ORAL	209092-001	Mar 13, 2017		RX	Yes	Yes						IN COMBINATION WITH AN AROMATASE INHIBITOR AS INITIAL ENDOCRINE-BASED THERAPY FOR THE TREATMENT OF ADULT PATIENTS WITH HORMONE RECEPTOR (HR)-POSITIVE, HUMAN EPIDERMAL GROWTH FACTOR RECEPTOR 2 (HER2)-NEGATIVE ADVANCED OR METASTATIC BREAST CANCER

International Family Members for US Patent 9,868,739

Country	Patent Number	Estimated Expiration	Supplementary Protection Certificate	SPC Country	SPC Expiration
Argentina	083797
Argentina	117799
Australia	2011326620
Australia	2016203534
Australia	2017221805
Australia	2018274883