Salts and crystalline forms of activin receptor-like kinase inhibitors
By forming stable salt crystal forms with different acids, the problem of unstable free base of compound (I) in humid environment is solved, the physical stability and high solubility of compound (I) are achieved, and the production and separation process is simplified.
CN114222745BActive Publication Date: 2025-03-25BLUEPRINT MEDICINES CORP
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Patent Information
- Application Number
- CN202080057092.0
- Authority / Receiving Office
- CN · China
- Patent Type
- Patents(China)
- Current Assignee / Owner
- Priority Date
- 2019-08-13
- Filing Date
- 2020-08-12
- Publication Date
- 2025-03-25
- Estimated Expiration
- 2040-08-12
AI Technical Summary
Technical Problem
The free base of compound (I) is unstable in humid environments and is prone to stick to water, resulting in difficulty in production and separation.
Method used
By forming salts with different acids, such as 1.5:1 succinate, 1:1 hydrochloric acid and 1:1 fumarate, a stable non-hygroscopic crystal form is provided, improving the crystallinity and solubility of compound (I).
Benefits of technology
The physical stability and high solubility of compound (I) are achieved, the large-scale production and separation process is simplified, and the stability and effectiveness of the drug are ensured.
✦ Generated by Eureka AI based on patent content.
Abstract
Disclosed are various salt forms of Compound (I) represented by the following structural formula and corresponding pharmaceutical compositions thereof. Specific single crystalline forms of 1:1.5 Compound (I) succinate, 1:1 Compound (I) hydrochloride, and 1:1 Compound (I) fumarate are characterized by a variety of properties and physical measurements. Methods for preparing specific crystalline forms are also disclosed. The present disclosure also provides methods for treating or ameliorating fibrodysplasia ossificans progressiva in a subject.
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