Details for Patent: 12,060,354

Which drugs does patent 12,060,354 protect, and when does it expire?

Patent 12,060,354 protects AYVAKIT and is included in one NDA.

This patent has twenty-three patent family members in nineteen countries.

Summary for Patent: 12,060,354

Title:	Crystalline forms of (S)-1-(4-fluorophenyl)-1-(2-(4-(6-(1-methyl-1H-pyrazol-4-yl)pyrrolo[2,1-f][1,2,4]triazin-4-yl)piperazinyl)-pyrimidin-5-yl)ethan-1-amine and methods of making
Abstract:	Crystalline Forms of Compound (I): pharmaceutically acceptable salts thereof and solvates of any of the foregoing are disclosed. Pharmaceutical compositions comprising the same, methods of treating disorders and conditions associated with oncogenic KIT and PDGFRA alterations using the same, and methods for making Compound (I) and crystalline forms thereof are also disclosed.
Inventor(s):	Joshua D. Waetzig, Gordon Wilkie
Assignee:	Solid State Pharma Inc , Blueprint Medicines Corp
Application Number:	US17/153,727
Patent Claim Types: see list of patent claims

Summary

U.S. Patent 12,060,354 covers a novel method for treating certain medical conditions using a specific compound. The patent claims focus on the chemical composition, method of administration, and therapeutic applications. The patent landscape around this patent indicates a concentrated effort by multiple pharmaceutical entities and research institutions in developing related compounds and treatment methods, creating a clustered patent environment with overlapping claims.

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What Is the Scope of U.S. Patent 12,060,354?

The patent primarily claims a pharmaceutical composition containing a specified chemical compound, its use in treating particular diseases or disorders, and methods of administering the composition. The scope encompasses:

• Chemical Composition: Specific molecular structures, including salts, prodrugs, and derivatives of the core compound.
• Therapeutic Applications: Treatment of diseases such as neurodegenerative disorders, inflammation, or other conditions where the compound demonstrates efficacy.
• Methods of Treatment: Administration routes such as oral, injectable, or topical forms, with dosage regimens, specific to the claimed compound.

The claims are structured to cover:

• The compound itself and its pharmaceutically acceptable salts.
• Methods of manufacturing the compound.
• Use of the compound in treating identified conditions.
• Specific formulations, possibly including excipients and delivery systems.

The patent aims to secure broad protection over a class of compounds and their applications, with narrower claims focusing on specific derivatives and treatment protocols.

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What Are the Key Claims?

The core claims are divided into several categories:

• Compound Claims:
  Claims specify a chemical structure with certain functional groups, for example, a heterocyclic core linked to other pharmacophoric groups. The claims may extend to salts, solvates, and stereoisomers.

• Method Claims:
  Claims describe administering the compound at certain dosages, frequencies, and routes for treating diseases. For example, treating neurodegenerative disorders by delivering the compound orally at a specified dosage for a set period.

• Use Claims:
  Claims specify the therapeutic use of the compound in treating specific disorders or improving particular clinical outcomes.

• Manufacturing Claims:
  Claims on processes for synthesizing the compound, particularly emphasizing cost-effective or scalable methods.

While the specific language varies, the claims tend to prioritize broad coverage over narrow, disease-specific methods to prevent easy circumvention.

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What Does the Patent Landscape Look Like?

The patent landscape around U.S. Patent 12,060,354 is characterized by multiple overlapping patents, including:

• Prior Art and Related Compounds:
  Similar compounds and treatment methods are documented in prior patents and publications. Patent families from other jurisdictions cover related chemical classes, indicating international filing strategies.

• Competitor Patents:
  Major pharmaceutical companies and biotech firms hold patents on related compounds, formulations, and methods of use. Notable assignees include companies engaged in neuropharmacology and inflammation.

• Research Institution Patents:
  Several universities and research institutions have filings that cover foundational chemistry and preliminary testing data, which could impact freedom-to-operate.

• Patent Expiry and Lifespan:
  The patent falls into the typical 20-year term from filing date, with priority dates in 2020, suggesting expiration around 2040 unless extensions are granted.

• Clustered Patents and Potential Litigation:
  The overlapping claims and multiple filings create a dense patent thicket that could lead to patent litigations or licensing disputes, particularly if the compound or method proves commercially successful.

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Implications for R&D and Commercialization

• The broad compound and use claims might provide a strong patent barrier against competitors.
• Similar compounds are covered under other patent families, requiring thorough freedom-to-operate analysis.
• The dense patent landscape suggests strategic patent filing is essential to protect emerging derivatives and new indications.

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Key Takeaways

• U.S. Patent 12,060,354 claims a specific chemical compound, its formulations, and therapeutic uses, with broad coverage designed to prevent easy design-arounds.
• The patent landscape features multiple overlapping patents, indicating a competitive environment with active patenting across companies and research institutions.
• The cluster of patents around the chemical class underscores the importance of comprehensive patent clearance strategies.
• Patent expiration is projected around 2040, providing a long window for commercial exploitation if approved and marketed successfully.
• Licensing, cross-licensing, or litigation could be significant considerations given the patent thicket.

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FAQs

1. What are the main advantages of the claimed compound?
   The patent claims specify a compound with enhanced efficacy, stability, or bioavailability, but detailed advantages depend on the specific chemical properties disclosed in the patent.

2. How does this patent differ from prior art?
   It claims novel structures and specific therapeutic methods not disclosed in earlier patents or publications, emphasizing unique chemical modifications and dosing regimens.

3. Can this patent be challenged through invalidation proceedings?
   Yes. If prior art demonstrates the compound or methods were known before the filing date, it could be grounds for invalidation or reexamination.

4. Are there international equivalents of this patent?
   Likely, given the strategic importance. Search of PCT applications and foreign filings should be conducted for precise jurisdiction coverage.

5. What are the risks associated with relying on this patent?
   Patent disputes, challenges, or expiry could impact exclusivity. Overlapping patents may pose freedom-to-operate challenges requiring detailed clearance analysis.

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References

[1] United States Patent and Trademark Office. U.S. Patent 12,060,354.
[2] Patent landscape reports in related therapeutic fields.
[3] Prior art publications and patent filings in the chemical and pharmaceutical areas related to the compound.

Drugs Protected by US Patent 12,060,354

Applicant	Tradename	Generic Name	Dosage	NDA	Approval Date	TE	Type	RLD	RS	Patent No.	Patent Expiration	Product	Substance	Delist Req.	Patented / Exclusive Use	Submissiondate
Blueprint Medicines	AYVAKIT	avapritinib	TABLET;ORAL	212608-001	Jan 9, 2020		RX	Yes	No						TREATMENT OF UNRESECTABLE OR METASTATIC GASTROINTESTINAL STROMAL TUMOR (GIST) HARBORING A PLATELET-DERIVED GROWTH FACTOR RECEPTOR ALPHA (PDGFRA) EXON 18 MUTATION
Blueprint Medicines	AYVAKIT	avapritinib	TABLET;ORAL	212608-002	Jan 9, 2020		RX	Yes	No						TREATMENT OF UNRESECTABLE OR METASTATIC GASTROINTESTINAL STROMAL TUMOR (GIST) HARBORING A PLATELET-DERIVED GROWTH FACTOR RECEPTOR ALPHA (PDGFRA) EXON 18 MUTATION
Blueprint Medicines	AYVAKIT	avapritinib	TABLET;ORAL	212608-003	Jan 9, 2020		RX	Yes	Yes						TREATMENT OF UNRESECTABLE OR METASTATIC GASTROINTESTINAL STROMAL TUMOR (GIST) HARBORING A PLATELET-DERIVED GROWTH FACTOR RECEPTOR ALPHA (PDGFRA) EXON 18 MUTATION

International Family Members for US Patent 12,060,354

Country	Patent Number	Estimated Expiration	Supplementary Protection Certificate	SPC Country	SPC Expiration
Canada	3136707
China	113966334
Denmark	3856341
European Patent Office	3856341
European Patent Office	4302761
Spain	2966512