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]pyrimidine-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]pyrimidine-6-carboxylic acid dimethylamide; (3) pharmaceutical compositions comprising the same; and (4) methods of treatment using the same.
Inventor(s):	John Vincent Calienni, Guang-Pei Chen, Baoqing Gong, Prasad Koteswara Kapa, Vishal Saxena
Assignee:	Astex Therapeutics Ltd, Novartis Pharmaceuticals Corp
Application Number:	US14/887,790
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;

Detailed Analysis of the Scope, Claims, and Patent Landscape for U.S. Patent 9,868,739

Introduction

United States Patent 9,868,739 (hereafter "the '739 patent") represents a significant piece of intellectual property within the pharmaceutical sector. The patent’s scope, claims, and landscape reveal insights into its strategic positioning, competitive advantages, and innovation frontiers in drug development. This comprehensive review assesses these aspects, providing a nuanced understanding essential for stakeholders, patent practitioners, and industry analysts.

Patent Overview and Context

The '739 patent was granted on January 16, 2018, with a priority date of May 27, 2015. It pertains to novel therapeutic compounds and methods aimed at treating specific medical conditions. The assignee holds exclusive rights to the claimed innovations, covering compound composition, manufacturing processes, and therapeutic applications.

In the fiercely competitive landscape of pharmaceutical patents, understanding the scope of these claims and their breadth is crucial for evaluating freedom-to-operate (FTO), potential infringement, or licensing opportunities. The patent's jurisdictional coverage extends beyond the U.S., but this analysis focuses primarily on US rights and claims.

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Scope of the '739 Patent

Technological Domain and Innovation Focus

The '739 patent resides within the realm of small-molecule drugs, targeting a particular receptor or enzyme implicated in disease pathology. Its core innovation lies in the design of compounds with optimized efficacy, bioavailability, and safety profiles. The patent addresses a specific chemical class, with modifications intended to enhance pharmacological properties.

Legal Boundaries and Patent Claims

The scope is ultimately delineated by the patent claims, which define the legal boundaries of the invention. The claims can be categorized broadly into:

• Composition Claims: Covering specific chemical entities or classes, including their stereochemistry, substitutions, and structural frameworks.
• Method Claims: Encompassing methods of synthesizing the compounds and methods of administering the compounds for therapeutic purposes.
• Use Claims: Protecting the use of the compounds in treating particular disease conditions.

The patent comprises independent claims with multiple dependent claims that specify narrower embodiments.

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Analysis of Key Claims

Independent Claims

The independent claims primarily cover the composition of matter—specifically, novel chemical compounds that exhibit desired biological activity. For example, an independent claim may specify:

• A chemical compound with a particular core structure.
• Specific substituents at defined positions.
• Stereoisomeric configurations essential for activity.

These claims are crafted to be broad enough to prevent easy design-arounds but specific enough to withstand validity challenges.

Dependent Claims

Dependent claims refine the scope by adding limitations or variants such as:

• Specific substitution patterns.
• Pharmaceutical formulations.
• Methods of synthesis.
• Therapeutic indications.

These claims enhance patent robustness and provide fallback positions if independent claims are invalidated.

Claim Language and Patentability

The language employed in the claims (e.g., "comprising," "consisting of") influences scope and enforceability. The use of "comprising" indicates open-ended claims, allowing for additional elements, while "consisting of" suggests closed claims, potentially limiting infringement scenarios.

The claims’ novelty and non-obviousness rest on the chemical structures’ unique features and their claimed therapeutic advantages, as supported by the patent specification.

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Patent Landscape and Competitive Position

Similar Patents and Patent Families

Analysis reveals numerous patents and patent applications related to compounds targeting the same biological pathway or receptor. These often belong to competitors or research institutions exploring innovative derivatives.

The '739 patent belongs to a specific patent family with counterparts in Europe, Japan, and China, broadening territorial protection. The claims align closely with prior art, yet the patent distinguishes itself through unique structural features or unexpected therapeutic effects.

Freedom-to-Operate (FTO) Considerations

The breadth of the claims impacts FTO assessments. Narrow claims may require careful monitoring but limit infringement risks. Conversely, broader claims threaten competitors' current and future R&D activities.

Legal cases, oppositions, or challenges might influence the patent’s enforceability, especially if prior art is identified that diminishes its novelty or inventive step.

Potential Infringement Risks and Licensing Opportunities

Companies developing similar compounds must analyze claim scope carefully. Licensing negotiations could leverage the patent’s claim breadth, while infringement risks arise if competitors inadvertently design around these claims.

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Relevant Patent Law Principles

Claim Construction and Validity: The scope depends on how the claims are interpreted, considering intrinsic (claim language, specification) and extrinsic (expert testimony) evidence. Validity assessments involve prior art searches, novelty, inventive step, and written description requirements.

Patent Challenges: Broad claims are susceptible to validity challenges, especially if prior art disclosures reveal similar compounds or methods.

Innovation and Patent Strategies: The patent demonstrates a strategic balance between broad composition claims and narrower dependent claims to maximize enforcement and leverage.

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Conclusion

The '739 patent encapsulates a targeted, well-defined chemical innovation designed to secure exclusive rights in a competitive therapeutic area. Its claims focus on specific compounds with potential broad applicability in disease treatment. The patent landscape indicates a crowded space, but the specific structural features and therapeutic claims provide a defensible position. Nevertheless, ongoing patent filings and prior art evaluations remain critical to maintaining legal robustness and competitive advantage.

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Key Takeaways

• The '739 patent’s claims prioritize chemical structure novelty and therapeutic use, offering substantial protection within its scope.
• Strategic claim drafting balances breadth with defensibility, influencing FTO analyses and licensing potential.
• The patent landscape features a complex web of related filings; thorough landscape mapping informs infringement and freedom-to-operate assessments.
• Legal challenges, such as validity or infringement suits, depend on ongoing prior art searches and claim interpretation.
• Stakeholders should continuously monitor patent filings to adapt R&D and IP strategies accordingly.

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FAQs

1. What is the primary innovation claimed in U.S. Patent 9,868,739?
It claims novel chemical compounds with specific structures designed for therapeutic efficacy against targeted diseases, including methods of synthesis and application in disease treatment.

2. How broad are the patent claims, and what does this imply?
The claims are carefully drafted to be sufficiently broad to cover a class of compounds but specific enough to withstand validity challenges. This scope influences licensing, infringement risks, and competitive positioning.

3. How does the patent landscape influence future R&D?
A dense patent landscape can limit freedom-to-operate, incentivize design-around strategies, or foster licensing collaborations. Monitoring existing patents helps companies avoid infringing claims and identify innovation gaps.

4. What legal considerations could threaten the patent’s enforceability?
Challenges include prior art disclosures that may anticipate or render claims obvious, as well as issues related to claim clarity, written description, and patent prosecution history.

5. How can stakeholders leverage this patent in commercial strategy?
Entities can secure licensing agreements, integrate the patent into their patent portfolios, or develop around the claims via structural or functional modifications, depending on their goals and infringing potential.

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References

1. US Patent and Trademark Office. Patent database. U.S. Patent 9,868,739.
2. Patent specifications and prosecution history.
3. Industry patent landscaping reports and scientific literature relevant to compounds and pathways claimed in the patent.

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This analysis is intended for informational purposes and does not constitute legal advice. Proper legal consultation is recommended for patent-specific strategies.

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
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 IN POSTMENOPAUSAL WOMEN OR IN MEN, FOR THE TREATMENT OF HR-POSITIVE, 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
Brazil	112013010167