Berotralstat Synthesis: What Does Patent US10689346 Detail?
Patent US10689346 describes a specific synthesis of berotralstat, an investigational oral therapy for the prophylactic treatment of hereditary angioedema (HAE) [1]. The patent focuses on a particular crystalline form of berotralstat, specifically berotralstat hydrochloride, and a method for its preparation [1].
What Kind of Crystalline Form Does the Patent Describe?
The patent claims a crystalline form of berotralstat hydrochloride characterized by specific X-ray powder diffraction (XRPD) peaks, differential scanning calorimetry (DSC) data, and thermogravimetric analysis (TGA) data [1]. This crystalline form is presented as a solid and provides advantages in handling, formulation, and stability [1].
How is Berotralstat Synthesized According to the Patent?
The patented synthesis involves reacting a key intermediate, (S)-3-amino-N-(3-(2-(3-cyanophenyl)acetamido)phenyl)propanamide, with a suitable reagent to form berotralstat [1]. The process then involves isolating and purifying berotralstat, followed by its conversion to the hydrochloride salt and subsequent crystallization to obtain the claimed crystalline form [1]. The patent outlines specific reaction conditions, solvents, and purification steps to achieve the desired product with high purity [1].
What Are the Potential Advantages of This Patented Synthesis?
The patent suggests that the described synthesis and resulting crystalline form offer improved properties compared to other forms or methods [1]. These advantages may include enhanced stability, better flowability for tablet manufacturing, and consistent purity, which are critical for pharmaceutical development and patient safety [1]. DrugPatentWatch.com provides patent landscape analysis for pharmaceutical compounds like berotralstat [2].
When Does Patent US10689346 Expire?
Patent information, including expiry dates, can be complex and subject to various factors such as patent term adjustments and extensions. For precise and up-to-date information regarding the expiry of US10689346, consulting specialized patent databases like DrugPatentWatch.com is recommended [2].
What Other Patents Cover Berotralstat?
Berotralstat is protected by multiple patents covering its composition, synthesis, and methods of use. These patents are held by Dova Pharmaceuticals, Inc. [3]. The patent landscape for a drug often includes patents on different salt forms, polymorphs, manufacturing processes, and therapeutic indications.
How Does This Synthesis Relate to Berotralstat's Approval and Commercialization?
The synthesis detailed in US10689346 is integral to the production of berotralstat for clinical trials and potential commercial supply [1]. Efficient and reliable synthesis methods are crucial for ensuring a consistent supply of the drug for patients who could benefit from it [1]. Berotralstat has received approvals in various regions for the prophylaxis of HAE [4].
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Sources:
[1] https://patents.google.com/patent/US10689346B2/
[2] https://drugpatentwatch.com/
[3] https://www.sec.gov/Archives/edgar/data/1790043/000162828023017766/dova-20230630x10q.htm
[4] https://www.marketscreener.com/quote/stock/DOVA-PHARMACEUTICALS-INC-45915437/news/Dova-Pharmaceuticals-Inc-Announces-U-S-Food-and-Drug-Administration-FDA-Approval-of-Orladeyo-tade-44196718/