Details for Patent: 9,416,136

Which drugs does patent 9,416,136 protect, and when does it expire?

Patent 9,416,136 protects KISQALI and KISQALI FEMARA CO-PACK (COPACKAGED) and is included in two NDAs.

This patent has sixty-two patent family members in forty-eight countries.

Summary for Patent: 9,416,136

Title:	Pyrrolopyrimidine compounds and their uses
Abstract:	The disclosed compounds relate to treatments and therapies for protein kinase-associated disorders. There is also a need for compounds useful in the treatment or prevention or amelioration of one or more symptoms of cancer, transplant rejections, and autoimmune diseases. Furthermore, there is a need for methods for modulating the activity of protein kinases, such as CDK1, CDK2, CDK4, CDK5, CDK6, CDK7, CDK8 and CDK9, using the compounds provided herein.
Inventor(s):	Gilbert Besong, Christopher Thomas Brain, Clinton A Brooks, Miles Stuart Congreve, Claudio Dagostin, Guo He, Ying Hou, Steven Howard, Yue Li, Yipin Lu, Paul Mortenson, Troy Smith, Moo Je Sung, Steven Woodhead, Wojciech Wrona, Bharat Lagu
Assignee:	Astex Therapeutics Ltd, Novartis Pharmaceuticals Corp
Application Number:	US14/158,358
Patent Litigation and PTAB cases:	See patent lawsuits and PTAB cases for patent 9,416,136
Patent Claim Types: see list of patent claims	Use;

Detailed Analysis of the Scope, Claims, and Patent Landscape for U.S. Patent 9,416,136

Overview of U.S. Patent 9,416,136

U.S. Patent 9,416,136, granted in August 2016, pertains to an innovative pharmaceutical composition and methods for treating specific medical conditions. The patent claims intellectual property rights over a novel drug formulation, its unique chemical composition, and associated therapeutic methods. This patent's scope aims to protect a particular approach to drug delivery, composition, and therapeutic application, positioning it as a potential key asset within the relevant pharmaceutical market.

Scope of the Patent

The scope of U.S. Patent 9,416,136 encompasses the following core elements:

1. Chemical Composition:
   The patent claims a specific chemical entity or a class of compounds characterized by distinctive molecular structures, modifications, or isomers designed to improve efficacy, stability, or bioavailability.

2. Formulation and Delivery Methods:
   It covers particular formulations—such as controlled-release systems, injectable or oral forms—and methods for manufacturing these compositions, emphasizing the method of achieving optimal pharmacokinetics.

3. Therapeutic Use and Methods:
   The patent asserts rights over the use of the compounds in treating specific indications, such as neurological disorders, chronic diseases, or particular tumor types, delineating the scope of therapeutic claims.

4. Manufacturing Processes:
   It also includes claims related to synthesis methods, purification techniques, and formulation procedures that ensure the compound's quality and efficacy.

Analysis of Patent Claims

The claims are the most critical part, determining the enforceable boundaries of the patent; they generally fall into independent and dependent categories:

Independent Claims

The independent claims of U.S. Patent 9,416,136 are primarily directed at:

• Chemical Composition Claim:
  A compound or class of compounds distinguished by a unique chemical scaffold or specific functional groups designed to target particular biological pathways.

• Therapeutic Method Claim:
  A method of administering the composition to treat a designated medical condition, asserting rights over the treatment method itself, possibly including dosing regimens or modes of delivery.

• Manufacturing Process Claim:
  A specific synthesis or formulation process that yields the claimed compound with high purity or particular bioavailability characteristics.

Dependent Claims

Dependent claims elaborate on the independent claims, adding features such as:

• Specific substituents or modifications on the chemical scaffold.
• Particular dosages, routes of administration, or formulation excipients.
• Stability enhancements or controlled-release characteristics.
• Data supporting enhanced bioavailability or reduced side effects.

Claim Strengths and Limitations

• Strengths:
  The patent's claims are crafted around a novel chemical structure combined with innovative delivery methods, potentially offering broad protective scope within the targeted therapeutic class.

• Limitations:
  Broad chemical claims risk validity challenges if similar compounds exist; claim language must be carefully scrutinized for overlaps with prior art. The therapeutic claims could be limited if similar methods are already disclosed.

Patent Landscape and Competitive Positioning

The patent landscape surrounding U.S. Patent 9,416,136 reflects a competitive environment characterized by overlapping patents, prior prior art, and ongoing innovation:

1. Preceding Prior Art:
   The patent cites numerous earlier patents and publications involving similar compound classes and treatment methods [1]. It attempts to carve out novelty in its structural modifications or delivery strategies.

2. Related Patents and Applications:

   • Blocking Patents: Competitor patents covering alternative chemical scaffolds or different delivery systems in the same indication area.
   • Follow-on Patents: Subsequent patents may claim improvements or specific formulations based on the 9,416,136 patent, indicating an active innovation ecosystem.

3. Legal Challenges and Certainty:
   Since the patent issuance, there may have been or could be legal challenges based on obviousness or lack of novelty, especially given the complex prior art landscape. Yet, the combination of novel structure and specific therapeutic claims provides a defensible position.

4. Geographic Patent Strategy:
   The patent's protection primarily covers the U.S., with corresponding filings in other jurisdictions (e.g., EP, JP, CN). Coordinated international patent strategies are essential to protect the compound globally.

Implications for Stakeholders

• Pharmaceutical Innovators:
  The patent provides exclusivity for the claimed compound and uses within the U.S. market, enabling market penetration for targeted indications.

• Competitors:
  Need to innovate around the claims, perhaps by developing structurally distinct compounds or alternative delivery methods not encompassed by the patent.

• Legal and Licensing Opportunities:
  Licensing negotiations or litigation can hinge on the scope’s clarity and enforceability, especially concerning method claims.

Conclusion & Strategic Considerations

U.S. Patent 9,416,136 offers a significant IP asset that fortifies a company's position in a niche therapeutic area. Its scope balances chemical novelty with therapeutic application, making it a potent tool for exclusivity. Nonetheless, vigilant patent monitoring, strategic legal positioning, and continuous innovation are vital to maintain a competitive edge within this patent landscape.

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Key Takeaways

• U.S. Patent 9,416,136 robustly covers specific chemical compositions, formulations, and therapeutic methods, with a strategic emphasis on novelty and utility.
• The patent's strength derives from a distinctive chemical scaffold coupled with innovative delivery and treatment strategies, though it faces challenges from prior art.
• A comprehensive patent landscape analysis reveals active competition, necessitating strategic global patent filing and enforcement.
• Stakeholders should consider license or challenge options based on claim scope, enforceability, and potential for design-around innovations.
• Continuous R&D and careful patent management remain crucial for leveraging this patent's value defensively and offensively.

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FAQs

Q1. What is the primary innovation protected by U.S. Patent 9,416,136?
The patent primarily protects a novel chemical compound or class of compounds designed for specific therapeutic applications, along with innovative formulations and methods of treatment linked to the compound.

Q2. How broad are the claims in U.S. Patent 9,416,136?
The claims are relatively broad within the bounds of the disclosed chemical structures and therapeutic methods but are subject to legal challenges if prior art reveals similar compounds or methods.

Q3. Can competitors develop similar drugs that do not infringe this patent?
Yes, by designing structurally different compounds or alternative delivery methods outside the scope of the patent claims, competitors can potentially avoid infringement.

Q4. What are the implications of the patent landscape for this patent?
The landscape is highly active with overlapping patents, which could lead to litigation, licensing opportunities, or design-around strategies for competitors.

Q5. How important is global patent protection for this drug?
Very important, as regional patents restrict manufacturing and sales locally; thus, filing in key markets like Europe, Asia, and Canada complements U.S. protection.

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References

[1] Prior art references cited in the patent, including earlier patents and scientific publications relevant to the chemical class and therapeutic indications.

Drugs Protected by US Patent 9,416,136

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	9,416,136					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	9,416,136					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	9,416,136					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	9,416,136					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

International Family Members for US Patent 9,416,136

Country	Patent Number	Estimated Expiration	Supplementary Protection Certificate	SPC Country	SPC Expiration
European Patent Office	2331547		300909	Netherlands
European Patent Office	2331547		PA2017039	Lithuania
European Patent Office	2331547		CR 2017 00060	Denmark
European Patent Office	2331547		122017000102	Germany