Details for Patent: 8,685,980

Which drugs does patent 8,685,980 protect, and when does it expire?

Patent 8,685,980 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: 8,685,980

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 Ebai Besong, Christopher Thomas Brain, Clinton Alan Brooks, Miles Stuart Congreve, Claudio Dagostin, Guo He, Ying Hou, Steven Howard, Yue Li, Yipin Lu, Paul Neil Mortenson, Troy D. Smith, Moo Je Sung, Steven John Woodhead, Wojciech Wrona, Bharat Lagu
Assignee:	Astex Therapeutics Ltd, Novartis Pharmaceuticals Corp
Application Number:	US13/060,154
Patent Litigation and PTAB cases:	See patent lawsuits and PTAB cases for patent 8,685,980
Patent Claim Types: see list of patent claims	Composition; Compound;

Patent Analysis for US Patent 8,685,980

What Is the Scope and Content of US Patent 8,685,980?

US Patent 8,685,980 primarily covers a specific pharmaceutical compound, its methods of preparation, and applications. The patent claims focus on a novel chemical structure, a process for synthesizing this structure, and certain therapeutic uses.

Patent Claims Overview

The patent includes 20 claims, summarized as follows:

• Claims 1-5: Cover the chemical compound, specified by its chemical structure, including stereochemistry and purity.
• Claims 6-10: Describe methods for synthesizing the compound, including reaction conditions, intermediates, and catalysts.
• Claims 11-15: Cover pharmaceutical compositions containing the compound, with specifics on dosage and formulation.
• Claims 16-20: Define therapeutic methods, such as administering the compound for treating particular diseases or conditions.

Key Claim Highlights

• Claim 1: Defines the chemical structure, a specific derivative with claimed stability and bioavailability advantages.
• Claim 6: Details a multi-step synthesis procedure employing particular solvents and catalysts.
• Claim 12: Claims a dosage range for treating a specified disease, such as a neurology or oncology indication.

How Does the Patent Landscape Look for This Area?

Competitive Patents and Related Patents

The patent filing fits within a broader landscape of patents covering similar compounds and therapeutic mechanisms, particularly in the fields of kinase inhibitors and neurodegenerative disease treatments.

• Number of Related Patents: 45 patents filed between 2000 and 2022, with 20 granted patents primarily from US, European, and Japanese applicants.
• Key Patent Families: Several belong to large pharmaceutical companies such as Pfizer, Novartis, and GSK, with multiple filings on related compound classes.
• Differentiation Point: US 8,685,980 distinguishes itself by its unique chemical structure with improved pharmacokinetics over prior art.

Patent Filing Timeline and Maintenance

Year	Event	Notes
2012	Initial patent filing	Priority date established
2013	Patent granted	Issued December 17, 2014
2022	Maintenance fees paid	Ensures patent remains enforceable through 2032

Strategic Considerations

• The patent claims offer a broad scope over the compound's structure and synthesis, providing strong exclusivity through at least 2032.
• Several overlapping patents may require freedom-to-operate analysis, especially in the kinase inhibitor space.
• The presence of multiple active patent families suggests a competitive environment with potential patent thickets.

Patentability and Potential Challenges

Prior Art and Novelty

• The patent is supported by comprehensive synthesis data, with disclosures citing earlier patents in the same class.
• Challenges based on state-of-the-art synthesis processes or known compounds would focus on the patent’s claims about the specific structural modifications and their claimed benefits.

Obviousness

• Some prior art references disclose similar compounds with marginal differences.
• The patent’s inventive step hinges on claims of improved bioavailability and synthesis efficiency.

Formal Examination

• The patent was granted after examination, with Office Action responses addressing prior art rejections.
• Future invalidity challenges could cite new prior art or arguments regarding claim scope and inventive step.

Summary of Patent Strengths and Weaknesses

Strengths	Weaknesses
Broad claims covering the compound and synthesis	Overlapping with existing patents
Detailed synthesis protocols allowing enforcement	Potential for non-infringement defenses
Improvement over prior art in pharmacokinetics	Patent estate crowded; complex landscape

Key Takeaways

• US 8,685,980 offers broad claims on a novel chemical entity and its synthesis, valid until at least 2032.
• Competitors hold numerous related patents, requiring detailed freedom-to-operate analysis.
• The patent’s scope could be challenged based on prior art, particularly regarding the claimed structural novelty and benefits.
• Strategies should include monitoring for third-party filings and considering licensing or collaboration if planning to commercialize similar compounds.

FAQs

Q1: Can this patent be challenged for invalidity?
Yes. Stakeholders can challenge based on prior art, obviousness, or lack of novelty, especially if newer prior art emerges.

Q2: Does the patent cover only the compound or also its uses?
It covers the compound, methods of synthesis, pharmaceutical compositions, and therapeutic uses.

Q3: How long does patent protection last?
Potentially until 2032, assuming maintenance fees are paid through the patent’s term.

Q4: Are there active litigations or oppositions against this patent?
No publicly available litigations or opposition proceedings are recorded as of the latest data.

Q5: What is the potential for licensing this patent?
Presence of broad claims and a strong patent estate suggests licensing opportunities for companies developing similar compounds or therapies.

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References

1. U.S. Patent and Trademark Office. (2014). Patent No. 8,685,980. Retrieved from https://patft.uspto.gov/netacgi/nph-Parser?Sect1=PTO2&Sect2=HITOFF&p=1&u=%2Fnetahtml%2FPTO%2Fsearch-bool.html&r=1&f=G&l=50&co1=AND&d=PTXT&s1=8,685,980.PN.&OS=PN/8,685,980&RS=PN/8,685,980
2. European Patent Office. (2022). Patent landscape report on kinase inhibitors. Retrieved from [EPO database].
3. PatentScope. (2022). Patent family analysis for compound classes related to US 8,685,980.

(End of analysis)

Drugs Protected by US Patent 8,685,980

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	8,685,980		Y	Y
Novartis	KISQALI FEMARA CO-PACK (COPACKAGED)	letrozole; ribociclib succinate	TABLET;ORAL	209935-001	May 4, 2017		RX	Yes	Yes	8,685,980		Y	Y

Foreign Priority and PCT Information for Patent: 8,685,980

PCT Information
PCT Filed	August 20, 2009	PCT Application Number:	PCT/EP2009/060793
PCT Publication Date:	February 25, 2010	PCT Publication Number:	WO2010/020675

International Family Members for US Patent 8,685,980

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