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 one NDA.

This patent has thirty-two patent family members in twenty-six 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-.alpha.]pyrimidine compounds of formula (I), ##STR00001## 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):	Wang; Zhiwei (Beijing, CN), Guo; Yunhang (Beijing, CN)
Assignee:	BeiGene, Ltd. (George Town, KY)
Application Number:	14/723,417
Patent Claim Types: see list of patent claims	Use; Composition; Compound; Dosage form;

Detailed Analysis of the Scope and Claims of United States Patent 9,447,106

Introduction

United States Patent 9,447,106, titled "Substituted pyrazolo[1,5-a]pyrimidines as Bruton's tyrosine kinase modulators," is a significant patent in the field of pharmaceuticals, particularly in the treatment of diseases related to Bruton's tyrosine kinase (BTK). Here, we will delve into the scope, claims, and the broader patent landscape surrounding this invention.

Inventors and Assignees

The patent was invented by Zhiwei Wang and Yunhang Guo, and it is assigned to BeiGene, Ltd., a biotechnology company based in the Grand Cayman Islands[1][4].

Patent Filing and Grant Dates

The patent application was filed on May 27, 2015, and the patent was granted on September 20, 2016[1][4].

Scope of the Invention

The patent covers methods and compositions for inhibiting Bruton's tyrosine kinase (BTK), an enzyme that plays a crucial role in the signaling pathways of B cells. BTK is implicated in various diseases, including certain types of leukemia and autoimmune disorders. The invention specifically involves substituted pyrazolo[1,5-a]pyrimidine compounds, which are designed to modulate BTK activity.

Chemical Compounds

The patent describes a class of compounds with the general formula (I), which includes substituted 4,5-dihydro- and 4,5,6,7-tetrahydro-pyrazolo[1,5-a]pyrimidines. These compounds are characterized by specific substitutions at various positions, such as the presence of a phenoxyphenyl group and an acryloylpiperidinyl group[1][4].

Claims

The patent includes multiple claims that define the scope of the invention. Here are some key aspects:

Independent Claims

• The patent includes independent claims that define the chemical structure of the compounds, their salts, and compositions thereof. For example, Claim 1 describes the general formula of the substituted pyrazolo[1,5-a]pyrimidine compounds[1][4].

Dependent Claims

• Dependent claims further specify the structure and substitutions of the compounds, such as the type of alkyl or aryl groups attached to the core structure. These claims narrow down the scope to specific embodiments of the invention[1][4].

Method Claims

• The patent also includes method claims related to the use of these compounds for treating diseases associated with BTK activity. These methods involve administering the compounds to patients suffering from conditions such as lymphoma, leukemia, and autoimmune diseases[1][4].

Patent Landscape

Related Patents

The patent is part of a larger family of patents related to BTK inhibitors. Other patents, such as those listed in the references cited section, cover similar compounds and methods. For example, patents like US 7,393,848 B2 and US 7,514,444 B2 also relate to BTK modulators, indicating a competitive and evolving field in this area[1].

Patent Expiration Dates

The patent is set to expire on April 22, 2034, which is 20 years from the date of filing. This expiration date is crucial for understanding the timeline for generic versions of the drug to enter the market[2].

Drug Development and Approval

The compounds described in this patent are part of the development process for drugs like Brukinsa (zanubrutinib), which has been approved by regulatory bodies for the treatment of certain lymphomas. The patent protection ensures that BeiGene maintains exclusive rights to the proprietary chemical formulation and manufacturing process until the patent expires[2].

Patent Scope and Quality

The scope of the patent is defined by the claim language, which is a critical aspect of patent quality. Metrics such as independent claim length and independent claim count can be used to measure patent scope. Narrower claims, as seen in this patent, are often associated with a higher probability of grant and a shorter examination process[3].

Impact on Innovation

The patent's scope and claims can influence innovation in the field. While broad patents might stifle innovation by limiting the space for new inventions, well-defined and narrower claims like those in this patent can encourage further research and development by providing clear boundaries[3].

Legal and Regulatory Aspects

The patent is subject to various legal and regulatory considerations, including patent infringement litigation and FDA exclusivity periods. These factors can affect the duration of the patent's exclusivity and the timing of generic drug entry into the market[2].

Conclusion

United States Patent 9,447,106 is a significant contribution to the field of BTK inhibitors, providing a detailed description of substituted pyrazolo[1,5-a]pyrimidine compounds and their use in treating BTK-related diseases. The patent's scope and claims are well-defined, ensuring that BeiGene maintains exclusive rights to these compounds until the patent expires in 2034.

Key Takeaways

• Inventors and Assignees: Zhiwei Wang and Yunhang Guo, assigned to BeiGene, Ltd.
• Patent Filing and Grant Dates: Filed on May 27, 2015, and granted on September 20, 2016.
• Scope of the Invention: Involves substituted pyrazolo[1,5-a]pyrimidine compounds as BTK modulators.
• Claims: Include independent and dependent claims defining the chemical structure and methods of use.
• Patent Expiration Dates: Set to expire on April 22, 2034.
• Impact on Innovation: Well-defined claims encourage further research and development.

FAQs

What is the main subject of United States Patent 9,447,106?

The main subject is the use of substituted pyrazolo[1,5-a]pyrimidine compounds as Bruton's tyrosine kinase (BTK) modulators.

Who are the inventors of this patent?

The inventors are Zhiwei Wang and Yunhang Guo.

When is the patent set to expire?

The patent is set to expire on April 22, 2034.

What is the significance of this patent in drug development?

This patent is significant for the development of drugs like Brukinsa (zanubrutinib), which are used to treat certain lymphomas.

How does the patent scope affect innovation?

The well-defined and narrower claims in this patent encourage further research and development by providing clear boundaries.

Sources Cited

1. Wang et al., United States Patent 9,447,106 B2, September 20, 2016.
2. Drugs.com, Generic Brukinsa Availability, November 6, 2024.
3. Marco et al., Patent Claims and Patent Scope, Hoover Institution, August 18, 2016.
4. Google Patents, US9447106B2 - Substituted pyrazolo[1,5-a]pyrimidines as bruton's tyrosine kinase modulators.

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
Beigene	BRUKINSA	zanubrutinib	CAPSULE;ORAL	213217-001	Nov 14, 2019		RX	Yes	Yes	9,447,106		Y	Y		TREATMENT OF ADULT PATIENTS WITH MANTLE CELL LYMPHOMA WHO HAVE RECEIVED AT LEAST ONE PRIOR THERAPY
Beigene	BRUKINSA	zanubrutinib	CAPSULE;ORAL	213217-001	Nov 14, 2019		RX	Yes	Yes	9,447,106		Y	Y		FOR THE TREATMENT OF PATIENTS WITH WALDENSTROM'S MACROGLOBULINEMIA
Beigene	BRUKINSA	zanubrutinib	CAPSULE;ORAL	213217-001	Nov 14, 2019		RX	Yes	Yes	9,447,106		Y	Y		RELAPSED OR REFRACTORY MARGINAL ZONE LYMPHOMA (MZL) WHO HAVE RECEIVED AT LEAST ONE PRIOR ANTI-CD20-BASED REGIMEN
Beigene	BRUKINSA	zanubrutinib	CAPSULE;ORAL	213217-001	Nov 14, 2019		RX	Yes	Yes	9,447,106		Y	Y		TREATMENT OF ADULT PATIENTS WITH CHRONIC LYMPHOCYTIC LEUKEMIA (CLL) OR SMALL LYMPHOCYTIC LYMPHOMA (SLL)
Beigene	BRUKINSA	zanubrutinib	CAPSULE;ORAL	213217-001	Nov 14, 2019		RX	Yes	Yes	9,447,106		Y	Y		TREATMENT OF ADULT PATIENTS WITH CHRONIC LYMPHOCYTIC LEUKEMIA
Beigene	BRUKINSA	zanubrutinib	CAPSULE;ORAL	213217-001	Nov 14, 2019		RX	Yes	Yes	9,447,106		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

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