Detailed Analysis of the Scope and Claims of United States Patent 11,168,058
Introduction
The United States Patent 11,168,058, titled "Manufacture of a crystalline pharmaceutical product," is a significant patent in the pharmaceutical industry, particularly in the development of androgen receptor (AR) modulators. This patent, assigned to Orion Corporation, involves the manufacture and characteristics of crystalline particles of a specific carboxamide derivative.
Patent Overview
Issuance and Assignee
The patent was issued on November 9, 2021, and is assigned to Orion Corporation, a Finnish pharmaceutical company known for its innovative drug development[2].
Compound Description
The patent focuses on crystalline particles of N—((S)-1-(3-(3-chloro-4-cyanophenyl)-1H-pyrazol-1-yl)-propan-2-yl)-5-(1-hydroxyethyl)-1H-pyrazole-3-carboxamide (Compound I). This compound is a potent androgen receptor (AR) modulator, which is useful in the treatment of AR-dependent cancers, such as prostate cancer, and other diseases where AR antagonism is desired[1][2].
Scope of the Patent
Crystalline Particles
The patent describes the specific characteristics of the crystalline particles, including their surface area, shape, and other physical properties. The crystalline particles have a specific surface area (SSA) in the range of about 8 to about 16 m²/g, preferably from about 10 to about 15 m²/g. These particles are characterized by their rounded shape, which can be substantially spherical, elliptical, or potato-like, with curved surfaces lacking sharp or rough edges. The mean aspect ratio of these particles is higher than 0.8, and the mean high sensitivity (HS) circularity is higher than 0.89[1].
Manufacturing Process
The patent details the methods for preparing these crystalline particles. The process involves specific solvents and conditions to achieve the desired crystalline form. The method ensures the production of particles with consistent and optimal physical properties, which are crucial for their pharmaceutical efficacy and stability[1].
Claims of the Patent
Composition Claims
The patent claims cover the crystalline particles of Compound I and their diastereomers. These claims include the specific surface area, shape, and other physical characteristics of the particles. The claims also encompass the pharmaceutical compositions containing these crystalline particles and their use in treating various diseases[1][2].
Method Claims
The patent includes claims related to the methods of preparing the crystalline particles. These method claims describe the specific conditions, solvents, and processes used to manufacture the desired crystalline form of Compound I[1].
Patent Landscape
Related Patents
Several related patents have been issued to Orion Corporation, all of which pertain to the same compound or its diastereomers. These include patents such as US10,010,530, US10,383,853, and US10,835,515, which also describe the crystalline forms of Compound I and methods for their preparation. These patents collectively protect the various aspects of the compound, including its composition, manufacturing process, and pharmaceutical applications[2].
Patent Expiration Dates
The patent US11,168,058 is set to expire on March 25, 2033. Other related patents, such as US10,010,530 and US10,383,853, are set to expire on January 28, 2036. These expiration dates are crucial for understanding the timeline of exclusivity and potential generic competition[2].
Legal and Regulatory Aspects
Drug Patents and Exclusivity
Drug patents, like US11,168,058, assign exclusive legal rights to the patent holder to protect the proprietary chemical formulation. These patents can include claims on the drug's brand name, trademark, product dosage form, ingredient formulation, or manufacturing process. The patent term typically lasts 20 years from the date of filing but can vary due to factors such as new formulations and patent infringement litigation. Additionally, the FDA may grant exclusivity periods that run concurrently with the patent term, providing additional market protection[2].
Obviousness and Nonobviousness
The obviousness of enantiomers, such as those described in this patent, is a complex issue. Courts often engage in detailed factual analyses to determine whether an enantiomer is obvious based on prior art. The "Lead Compound" analysis is crucial in such determinations, where it must be shown that a chemist of ordinary skill would have selected the racemic mixture as a lead compound for further development. The resolution of racemates into their enantiomers must demonstrate unexpected results or significant improvements over the prior art to be considered nonobvious[4].
Industry Impact
Pharmaceutical Applications
The crystalline particles of Compound I have significant implications for the treatment of AR-dependent cancers and other diseases. The specific physical properties and manufacturing process described in the patent ensure the production of a stable and effective pharmaceutical product. This innovation can lead to improved patient outcomes and expanded treatment options in the field of oncology[1].
Competitive Landscape
The patent landscape surrounding US11,168,058 indicates a strong position for Orion Corporation in the development of AR modulators. The multiple patents covering various aspects of Compound I and its manufacturing process provide a robust intellectual property portfolio, protecting the company's innovations and market position until the patents expire[2].
Key Takeaways
- Compound I: The patent focuses on crystalline particles of N—((S)-1-(3-(3-chloro-4-cyanophenyl)-1H-pyrazol-1-yl)-propan-2-yl)-5-(1-hydroxyethyl)-1H-pyrazole-3-carboxamide, a potent AR modulator.
- Physical Properties: The crystalline particles have specific surface areas, shapes, and other physical characteristics crucial for their pharmaceutical efficacy.
- Manufacturing Process: The patent details the methods for preparing these crystalline particles, ensuring consistent and optimal physical properties.
- Patent Landscape: Multiple related patents protect various aspects of Compound I and its manufacturing process, providing a robust intellectual property portfolio.
- Legal and Regulatory Aspects: The patent term and FDA exclusivity periods provide market protection until the patents expire.
- Industry Impact: The innovation has significant implications for the treatment of AR-dependent cancers and other diseases.
FAQs
What is the main compound described in US Patent 11,168,058?
The main compound is N—((S)-1-(3-(3-chloro-4-cyanophenyl)-1H-pyrazol-1-yl)-propan-2-yl)-5-(1-hydroxyethyl)-1H-pyrazole-3-carboxamide (Compound I), a potent androgen receptor (AR) modulator.
What are the specific physical properties of the crystalline particles described in the patent?
The crystalline particles have a specific surface area (SSA) in the range of about 8 to about 16 m²/g, preferably from about 10 to about 15 m²/g, and are characterized by their rounded shape with curved surfaces lacking sharp or rough edges.
What is the manufacturing process for the crystalline particles?
The process involves specific solvents and conditions to achieve the desired crystalline form. The method ensures the production of particles with consistent and optimal physical properties.
Who is the assignee of US Patent 11,168,058?
The patent is assigned to Orion Corporation, a Finnish pharmaceutical company.
When does the patent expire?
The patent is set to expire on March 25, 2033.
Sources
- US11168058B2 - Manufacture of a crystalline pharmaceutical product. Google Patents.
- Generic Nubeqa Availability. Drugs.com.
- Patent Claims and Patent Scope. SSRN.
- Enantiomer Patents: Innovative or Obvious?. Katten Muchin Rosenman LLP.
