Process for the synthesis of a phosphoinositide 3-kinase inhibitor
US-2016362426-A1 · Dec 15, 2016 · US
Salts and processes of preparing a PI3K inhibitor
US10336759B2 · US · B2
| Field | Value |
|---|---|
| Publication number | US-10336759-B2 |
| Application number | US-201615054474-A |
| Country | US |
| Kind code | B2 |
| Filing date | Feb 26, 2016 |
| Priority date | Feb 27, 2015 |
| Publication date | Jul 2, 2019 |
| Grant date | Jul 2, 2019 |
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Abstract
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The present application provides processes for preparing (R)-4-(3-((S)-1-(4-amino-3-methyl-1H-pyrazolo[3,4-d]pyrimidin-1-yl)ethyl)-5-chloro-2-ethoxy-6-fluorophenyl)pyrrolidin-2-one, which is useful as an inhibitor phosphoinositide 3-kinase-delta (PI3Kδ), as well as a salt form and intermediates related thereto.
First claim
Opening claim text (preview).
What is claimed is: 1. A salt which is (R)-4-(3-((S)-1-(4-amino-3-methyl-1H-pyrazolo[3,4-d]pyrimidin-1-yl)ethyl)-5-chloro-2-ethoxy-6-fluorophenyl)pyrrolidin-2-one hydrochloric acid salt, that is crystalline, having at least four XRPD peaks, in terms of 2-theta, selected from about 11.3°, about 16.4°, about 21.0°, about 23.0°, about 28.1°, about 31.2°, and about 32.8°. 2. The salt of claim 1 that is a 1:1 stoichiometric ratio of (R)-4-(3-((S)-1-(4-amino-3-methyl-1H-pyrazolo[3,4-d]pyrimidin-1-yl)ethyl)-5-chloro-2-ethoxy-6-fluorophenyl)pyrrolidin-2-one to hydrochloric acid. 3. The salt of claim 1 characterized by a DSC thermogram having an endothermic peak at about 207° C. 4. The salt of claim 1 having a DSC thermogram substantially as shown in FIG. 1 . 5. The salt of claim 1 having a TGA thermogram substantially as shown in FIG. 2 . 6. The salt of claim 1 having at least five XRPD peaks, in terms of 2-theta, selected from about 11.3°, about 16.4°, about 21.0°, about 23.0°, about 28.1°, about 31.2°, and about 32.8°. 7. The salt of claim 1 having an XRPD profile substantially as shown in FIG. 3 . 8. A pharmaceutical composition comprising a salt of claim 1 and a pharmaceutically acceptable carrier.
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Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00 · CPC title
Antiallergic agents (antiasthmatic agents A61P11/06; ophthalmic antiallergics A61P27/14) · CPC title
Immunosuppressants, e.g. drugs for graft rejection · CPC title
Immunomodulators · CPC title
Drugs for immunological or allergic disorders · CPC title
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- What does patent US10336759B2 cover?
- The present application provides processes for preparing (R)-4-(3-((S)-1-(4-amino-3-methyl-1H-pyrazolo[3,4-d]pyrimidin-1-yl)ethyl)-5-chloro-2-ethoxy-6-fluorophenyl)pyrrolidin-2-one, which is useful as an inhibitor phosphoinositide 3-kinase-delta (PI3Kδ), as well as a salt form and intermediates related thereto.
- Who is the assignee on this patent?
- Incyte Corp
- What technology area does this patent fall under?
- Primary CPC classification C07D487/04. Mapped technology areas include Chemistry & Metallurgy.
- When was this patent published?
- Publication date Tue Jul 02 2019 00:00:00 GMT+0000 (Coordinated Universal Time) (B2). Legal status and post-grant events are not shown on this page.
- What related patents are in patentsdb?
- We list 12 related publications on this page (citations in our corpus or others sharing the same primary CPC).