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Last Updated: December 23, 2024

Details for Patent: 10,112,942


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Summary for Patent: 10,112,942
Title:Substituted pyrazolo[1,5-A]pyridine compounds as RET kinase inhibitors
Abstract: Provided herein are compounds of the Formula I: ##STR00001## and stereoisomers and pharmaceutically acceptable salts or solvates thereof, in which A, B, X.sup.1, X.sup.2, X.sup.3, X.sup.4, Ring D, and E have the meanings given in the specification, which are inhibitors of RET kinase and are useful in the treatment and prevention of diseases which can be treated with a RET kinase inhibitor, including RET-associated diseases and disorders.
Inventor(s): Andrews; Steven W. (Boulder, CO), Aronow; Sean (Boulder, CO), Blake; James F. (Boulder, CO), Brandhuber; Barbara J. (Boulder, CO), Cook; Adam (Boulder, CO), Haas; Julia (Boulder, CO), Jiang; Yutong (Boulder, CO), Kolakowski; Gabrielle R. (Boulder, CO), McFaddin; Elizabeth A. (Boulder, CO), McKenney; Megan L. (Boulder, CO), McNulty; Oren T. (Boulder, CO), Metcalf; Andrew T. (Boulder, CO), Moreno; David A. (Boulder, CO), Tang; Tony P. (Boulder, CO), Ren; Li (Boulder, CO)
Assignee: Array BioPharma Inc. (Boulder, CO)
Application Number:15/858,240
Patent Claim Types:
see list of patent claims
Composition; Compound;
Patent landscape, scope, and claims:

Detailed Analysis of the Scope and Claims of United States Patent 10,112,942

Introduction

United States Patent 10,112,942, titled "Substituted pyrazolo[1,5-A]pyridine compounds as RET kinase inhibitors," is a significant patent in the field of pharmaceuticals, particularly in the development of cancer therapies. This patent, issued to Array BioPharma Inc., covers a class of compounds designed to inhibit the RET (rearranged during transfection) kinase, which is implicated in various cancers.

Inventors and Assignees

The patent was invented by a team of researchers including Steven W. Andrews, Sean Aronow, James F. Blake, Barbara J. Brandhuber, Adam Cook, Julia Haas, Yutong Jiang, Gabrielle R. Kolakowski, Elizabeth A. McFaddin, Megan L. McKenney, Oren T. McNulty, Andrew T. Metcalf, David A. Moreno, Tony P. Tang, and Li Ren. The assignee of the patent is Array BioPharma Inc.[2].

Patent Issuance and Expiration

The patent was issued on October 30, 2018, and is set to expire on October 10, 2037. This expiration date is typical for patents, which generally have a 20-year term from the date of filing, although various factors can influence this duration[2].

Scope of the Patent

Compounds Covered

The patent describes a series of substituted pyrazolo[1,5-A]pyridine compounds, which are designed to inhibit the RET kinase. These compounds are detailed in the patent's formula I, which outlines the structural requirements and possible substitutions for the compounds. The scope includes stereoisomers and pharmaceutically acceptable salts or solvates of these compounds[1][2].

RET Kinase Inhibition

RET kinase is a protein kinase involved in the signaling pathways that regulate cell growth and division. Mutations or dysregulation of RET can lead to various cancers, including medullary thyroid cancer, non-small cell lung cancer, and other solid tumors. The compounds covered by this patent are specifically designed to inhibit RET kinase activity, thereby providing a therapeutic approach to treating these cancers[1].

Claims

The patent includes multiple claims that define the scope of protection for the invented compounds.

Independent Claims

The independent claims define the broadest scope of the invention, including the general structure of the substituted pyrazolo[1,5-A]pyridine compounds and their use as RET kinase inhibitors. These claims are crucial as they set the boundaries for what is considered novel and non-obvious under patent law[1].

Dependent Claims

Dependent claims further narrow down the scope by specifying particular substitutions, functional groups, and other structural details. These claims provide additional protection for specific embodiments of the invention, ensuring that the patent holder has exclusive rights to these more detailed variations[1].

Chemical Structure and Substitutions

The patent delves into the detailed chemical structure of the compounds, including various substituents such as alkyl groups, alkoxy groups, fluoro groups, and other functional groups. The claims also cover different ring systems and heterocyclic groups, providing a comprehensive description of the chemical space covered by the patent[1].

Pharmaceutical Compositions and Uses

In addition to the chemical compounds themselves, the patent also covers pharmaceutical compositions containing these compounds and their use in treating diseases associated with RET kinase dysregulation. This includes methods of treatment and administration, which are essential for the practical application of these compounds in clinical settings[1].

Patent Landscape

Related Patents

There are several related patents issued to Array BioPharma Inc. that cover similar or complementary aspects of RET kinase inhibitors. For example, patents 10,137,124 and 10,172,851 also describe substituted pyrazolo[1,5-A]pyridine compounds with similar structures and uses. These patents collectively form a robust intellectual property portfolio around RET kinase inhibitors[2].

Generic Availability and Exclusivity

The patent's expiration in 2037 will open the door for generic versions of these compounds. However, until then, the exclusivity granted by the FDA and the patent protection ensure that Array BioPharma Inc. retains exclusive marketing rights for these drugs. This exclusivity period can run concurrently with the patent term and is crucial for the commercial success of the drug[2].

Solid State Forms and Formulations

Other patents, such as 10,584,124 and 10,786,489, cover crystalline forms and specific formulations of these compounds. These patents are important for ensuring the stability, bioavailability, and manufacturability of the drug products[2].

Industry Impact

The development and patenting of these RET kinase inhibitors have significant implications for the treatment of cancer. For instance, selpercatinib, a drug developed based on these patents, has shown promising results in clinical trials and has been approved for use in treating certain types of cancer. This underscores the importance of these patents in advancing medical treatment options[4].

Patent Scope and Quality

The scope of this patent, as with many pharmaceutical patents, is subject to scrutiny regarding its breadth and clarity. Research has shown that narrower claims, such as those seen in this patent, are often associated with a higher probability of grant and a shorter examination process. This suggests that the patent office has carefully evaluated the claims to ensure they are specific and valid[3].

Key Takeaways

  • Compounds Covered: The patent covers substituted pyrazolo[1,5-A]pyridine compounds designed to inhibit RET kinase.
  • RET Kinase Inhibition: These compounds are therapeutic agents for treating cancers associated with RET kinase dysregulation.
  • Claims: The patent includes independent and dependent claims defining the scope of protection for the compounds.
  • Chemical Structure: Detailed descriptions of the chemical structure and possible substitutions are provided.
  • Pharmaceutical Compositions: The patent covers pharmaceutical compositions and methods of treatment.
  • Patent Landscape: Related patents and exclusivity periods are crucial for the commercial and intellectual property strategy.
  • Industry Impact: The patents have led to the development of approved cancer treatments like selpercatinib.

FAQs

What is the main subject of United States Patent 10,112,942?

The main subject of this patent is the description and use of substituted pyrazolo[1,5-A]pyridine compounds as RET kinase inhibitors.

Who are the inventors and assignees of this patent?

The inventors include a team of researchers from Array BioPharma Inc., and the assignee is Array BioPharma Inc.

When does the patent expire?

The patent is set to expire on October 10, 2037.

What is the significance of RET kinase in cancer treatment?

RET kinase is involved in signaling pathways that regulate cell growth and division. Mutations or dysregulation of RET can lead to various cancers, making RET kinase inhibitors a promising therapeutic approach.

Are there related patents covering similar compounds?

Yes, there are several related patents issued to Array BioPharma Inc. that cover similar or complementary aspects of RET kinase inhibitors.

Cited Sources

  1. US10112942B2 - Substituted pyrazolo[1,5-A]pyridine compounds as RET kinase inhibitors - Google Patents
  2. Generic Retevmo Availability - Drugs.com
  3. Patent Claims and Patent Scope - Hoover Institution
  4. Solid state forms of selpercatinib and process for preparation thereof - Google Patents

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Drugs Protected by US Patent 10,112,942

Applicant Tradename Generic Name Dosage NDA Approval Date TE Type RLD RS Patent No. Patent Expiration Product Substance Delist Req. Patented / Exclusive Use Submissiondate
Loxo Oncol Eli Lilly RETEVMO selpercatinib CAPSULE;ORAL 213246-001 May 8, 2020 RX Yes No ⤷  Subscribe ⤷  Subscribe Y Y ⤷  Subscribe
Loxo Oncol Eli Lilly RETEVMO selpercatinib CAPSULE;ORAL 213246-002 May 8, 2020 RX Yes Yes ⤷  Subscribe ⤷  Subscribe Y Y ⤷  Subscribe
Loxo Oncol Eli Lilly RETEVMO selpercatinib TABLET;ORAL 218160-001 Apr 10, 2024 RX Yes No ⤷  Subscribe ⤷  Subscribe Y Y ⤷  Subscribe
Loxo Oncol Eli Lilly RETEVMO selpercatinib TABLET;ORAL 218160-002 Apr 10, 2024 RX Yes No ⤷  Subscribe ⤷  Subscribe Y Y ⤷  Subscribe
Loxo Oncol Eli Lilly RETEVMO selpercatinib TABLET;ORAL 218160-003 Apr 10, 2024 RX Yes No ⤷  Subscribe ⤷  Subscribe Y Y ⤷  Subscribe
Loxo Oncol Eli Lilly RETEVMO selpercatinib TABLET;ORAL 218160-004 Apr 10, 2024 RX Yes Yes ⤷  Subscribe ⤷  Subscribe Y Y ⤷  Subscribe
>Applicant >Tradename >Generic Name >Dosage >NDA >Approval Date >TE >Type >RLD >RS >Patent No. >Patent Expiration >Product >Substance >Delist Req. >Patented / Exclusive Use >Submissiondate

International Family Members for US Patent 10,112,942

Country Patent Number Estimated Expiration Supplementary Protection Certificate SPC Country SPC Expiration
Argentina 109919 ⤷  Subscribe
Argentina 109920 ⤷  Subscribe
Australia 2017342022 ⤷  Subscribe
Australia 2017342027 ⤷  Subscribe
Brazil 112019007143 ⤷  Subscribe
Brazil 112019007144 ⤷  Subscribe
Canada 3039760 ⤷  Subscribe
>Country >Patent Number >Estimated Expiration >Supplementary Protection Certificate >SPC Country >SPC Expiration

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