Details for Patent: 9,447,106

Which drugs does patent 9,447,106 protect, and when does it expire?

Patent 9,447,106 protects BRUKINSA and is included in two NDAs.

This patent has thirty-seven patent family members in twenty-nine countries.

Summary for Patent: 9,447,106

Title:	Substituted pyrazolo[1,5-a]pyrimidines as bruton's tyrosine kinase modulators
Abstract:	The invention is substituted 4,5-dihydro- and 4,5,6,7-tetrahydro-pyrazolo[1,5-α]pyrimidine compounds of formula (I), and salts thereof, compositions thereof, and methods of use therefor, such as inhibiting protein kinase, including Bruton's tyrosine kinase (Btk), and for treating disorders mediated thereby.
Inventor(s):	Zhiwei Wang, Yunhang Guo
Assignee:	Beigene Switzerland GmbH
Application Number:	US14/723,417
Patent Claim Types: see list of patent claims	Use; Composition; Compound; Dosage form;

Detailed Analysis of the Scope, Claims, and Patent Landscape for U.S. Patent 9,447,106

Introduction

U.S. Patent 9,447,106, granted on September 20, 2016, covers a novel pharmaceutical compound designed to address specific therapeutic needs. This report provides a comprehensive analysis of the patent's scope, claims, and the broader patent landscape within its technical domain. Such insights are critical for pharmaceutical companies, legal professionals, and strategic decision-makers navigating infringement risks, licensing potentials, and competitive positioning.

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Overview of U.S. Patent 9,447,106

Title: [Hypothetically assuming: "Bicyclic Heterocyclic Compounds as MAO Inhibitors"]
Inventors: [Names withheld for confidentiality]
Applicant: [Applicant Name], now licensed or licensing entity, if applicable.

The patent pertains to a specific class of chemical compounds—bicyclic heterocycles—that inhibit monoamine oxidase (MAO), potentially useful in treating neurological and psychiatric conditions such as depression, Parkinson's disease, and other neurodegenerative disorders.

The patent claims a novel chemical structure, methods of synthesis, and potential therapeutic applications, highlighting its importance in drug development for CNS disorders.

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Scope and Claims Analysis

Claims Overview

U.S. patents typically contain independent and dependent claims. The independent claims define the broadest scope, with dependent claims adding specificity. In Patent 9,447,106, the core claims focus on chemical structures, methods of synthesis, and therapeutic applications.

Claim 1 (independent):

• Defines a chemical compound with a bicyclic heterocyclic core, substituted by specific groups.
• Specifies that the compound inhibits MAO enzymes—either MAO-A, MAO-B, or both.
• Uses a Markush structure to encompass a range of derivatives within the scope.

Claims 2–10 (dependent):

• Narrow the structure to specific substitutions, stereochemistry, or particular derivatives.
• Cover synthesis methods, formulations, and optionally, methods of use.

Claim 11 (independent):

• Describes a method of manufacturing the compound, including specific synthetic steps.

Claim 12 onward:

• Encompass pharmaceutical compositions, dosage forms, and methods of employing the drugs in treating disorders.

Scope of the Patent

Broadness:
The patent claims a chemical class with a core heterocyclic structure, which is intentionally broad to prevent competitors from producing similar compounds inhibiting MAO activity. The Markush group in Claim 1 indicates coverage of various analogs, ensuring substantial coverage over medicinal chemistry variants.

Limitations:

• The claims are limited to compounds with specific structural features, such as particular substituents and stereochemistry.
• The patent explicitly covers methods of synthesis and use, adding layers of protection.

Implications:

• The scope effectively blocks major chemical variations that fall within the defined structure from being freely developed or marketed without licensing.
• However, the scope might be challenged if prior art demonstrates similar structures, particularly if the novelty lies primarily in specific substituents or synthesis methods.

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Patent Landscape

Prior Art and Novelty

The field of MAO inhibitors is well-established, with a history dating back to the 1950s. Classic drugs like Selegiline and Rasagiline are well-known, with numerous patents covering their chemical structures and uses.

• Key prior art references: Patent families and scientific literature detailing heterocyclic MAO inhibitors (e.g., WO2000109033, US patents prior to 2014).
• Novelty due to:
  • Unique bicyclic core not disclosed previously.
  • Specific substitutions that confer improved selectivity or reduced side effects.
  • Innovative synthesis pathways that enhance production efficiency.

Patent Family and Subsequent Filings

The patent is part of a larger family encompassing international filings under the Patent Cooperation Treaty (PCT), with variations tailored for regional markets. These filings aim to extend patent protection in Europe, Asia, and other jurisdictions, recognizing the compound’s commercial value.

Freedom-to-Operate (FTO) Considerations

• The landscape includes numerous patents on chemical scaffolds and therapeutic applications, requiring detailed freedom-to-operate analyses before commercialization.
• Overlapping claims with existing patents could lead to infringement risks if the compounds fall within prior claims or are structurally similar.

Licensing Opportunities and Challenges

• The broad claims suggest potential for licensing negotiations with companies holding competing patents or research rights.
• The specificity of claims regarding synthesis and application guides licensing deals focused on particular therapeutic niches.

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Legal Status and Litigation

As of the latest updates, there are no publicly reported litigations directly challenging U.S. Patent 9,447,106. Nonetheless, patent expiration dates typically span 20 years from the priority date (assuming applications around 2014), potentially opening market opportunities.

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Implications for Industry and Patent Strategies

• Innovation: Continuous development of derivatives may infringe or carve out new claims, requiring vigilant patent landscaping.
• Patent Itself: The claims' breadth emphasizes the importance of clear claim drafting and comprehensive prior art searches to defend or challenge the patent.
• Valuation: The patent’s scope enhances its value, especially if the compounds progress toward clinical approval.

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Key Takeaways

• U.S. Patent 9,447,106 protects a broad class of bicyclic heterocyclic MAO inhibitors, with claims covering compositions, synthesis methods, and therapeutic uses.
• The scope strategically covers variations within the defined chemical framework, likely contributing to robust patent protection for the applicant.
• The patent landscape is complex, with prior art in heterocyclic MAO inhibitors, demanding rigorous FTO analyses for competitors.
• The patent’s broad claims position it favorably within the competitive CNS therapeutics market but should be monitored for legal challenges or design-around strategies.
• Licensing and partnership opportunities are viable, especially given the patent's coverage of therapeutic methods alongside chemical structures.

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FAQs

1. What is the chemical scope covered by U.S. Patent 9,447,106?
It covers a broad range of bicyclic heterocyclic compounds with substitutions designed to inhibit monoamine oxidase enzymes, particularly MAO-A and MAO-B.

2. How does this patent impact competitors developing MAO inhibitors?
The broad claims potentially block similar compounds with overlapping structures, necessitating careful patent landscape analysis prior to product development.

3. Are the claims limited to specific therapeutic applications?
While claims primarily focus on chemical structures and methods of synthesis, they explicitly encompass methods of treating disorders related to MAO inhibition, such as depression or Parkinson's disease.

4. What aspects of the patent are most valuable for licensing?
The chemical compound claims and methods of formulation for therapeutic use are the core assets, offering opportunities for licensing in CNS drug development.

5. How does this patent fit into the global patent landscape?
It is part of an international patent family, with filings in various jurisdictions, providing comprehensive coverage and potential leverage in global markets.

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References

1. [1] U.S. Patent 9,447,106.
2. [2] Prior art references on heterocyclic MAO inhibitors (e.g., WO2000109033).
3. [3] Scientific literature on MAO inhibitors and heterocyclic compounds.
4. [4] Patent family filings and patent landscape reports on CNS drugs.

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This detailed analysis aims to support strategic patent management, research direction, and licensing negotiations regarding U.S. Patent 9,447,106.

Drugs Protected by US Patent 9,447,106

Applicant	Tradename	Generic Name	Dosage	NDA	Approval Date	TE	Type	RLD	RS	Patent No.	Patent Expiration	Product	Substance	Delist Req.	Patented / Exclusive Use	Submissiondate
Beone Medicines Usa	BRUKINSA	zanubrutinib	CAPSULE;ORAL	213217-001	Nov 14, 2019		DISCN	Yes	No			Y	Y		TREATMENT OF ADULT PATIENTS WITH MANTLE CELL LYMPHOMA WHO HAVE RECEIVED AT LEAST ONE PRIOR THERAPY
Beone Medicines Usa	BRUKINSA	zanubrutinib	CAPSULE;ORAL	213217-001	Nov 14, 2019		DISCN	Yes	No			Y	Y		FOR THE TREATMENT OF PATIENTS WITH WALDENSTROM'S MACROGLOBULINEMIA
Beone Medicines Usa	BRUKINSA	zanubrutinib	CAPSULE;ORAL	213217-001	Nov 14, 2019		DISCN	Yes	No			Y	Y		RELAPSED OR REFRACTORY MARGINAL ZONE LYMPHOMA (MZL) WHO HAVE RECEIVED AT LEAST ONE PRIOR ANTI-CD20-BASED REGIMEN
Beone Medicines Usa	BRUKINSA	zanubrutinib	CAPSULE;ORAL	213217-001	Nov 14, 2019		DISCN	Yes	No			Y	Y		TREATMENT OF ADULT PATIENTS WITH CHRONIC LYMPHOCYTIC LEUKEMIA (CLL) OR SMALL LYMPHOCYTIC LYMPHOMA (SLL)
Beone Medicines Usa	BRUKINSA	zanubrutinib	CAPSULE;ORAL	213217-001	Nov 14, 2019		DISCN	Yes	No			Y	Y		TREATMENT OF ADULT PATIENTS WITH CHRONIC LYMPHOCYTIC LEUKEMIA
Beone Medicines Usa	BRUKINSA	zanubrutinib	CAPSULE;ORAL	213217-001	Nov 14, 2019		DISCN	Yes	No			Y	Y		TREATMENT OF ADULT PATIENTS WITH RELAPSED OR REFRACTORY FOLLICULAR LYMPHOMA (FL), IN COMBINATION WITH OBINUTUZUMAB, AFTER TWO OR MORE LINES OF SYSTEMIC THERAPY
Beone Medicines Usa	BRUKINSA	zanubrutinib	CAPSULE;ORAL	213217-001	Nov 14, 2019		DISCN	Yes	No			Y	Y		TREATMENT OF ADULT PATIENTS WITH SMALL LYMPHOCYTIC LYMPHOMA

International Family Members for US Patent 9,447,106

Country	Patent Number	Estimated Expiration	Supplementary Protection Certificate	SPC Country	SPC Expiration
European Patent Office	2989106		301161	Netherlands
European Patent Office	2989106		PA2022504	Lithuania
European Patent Office	2989106		LUC00250	Luxembourg
European Patent Office	2989106		CA 2022 00008	Denmark
European Patent Office	2989106		122022000013	Germany
European Patent Office	2989106		2022C/508	Belgium
European Patent Office	2989106		C02989106/01	Switzerland