Diaminopyrimidine derivatives and processes for the preparation thereof
US-10227330-B2 · Mar 12, 2019 · US
Processes for preparing a diaminopyrimidine derivative or acid addition salt thereof
US11623925B2 · US · B2
| Field | Value |
|---|---|
| Publication number | US-11623925-B2 |
| Application number | US-202217873966-A |
| Country | US |
| Kind code | B2 |
| Filing date | Jul 26, 2022 |
| Priority date | May 18, 2018 |
| Publication date | Apr 11, 2023 |
| Grant date | Apr 11, 2023 |
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- Title
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- Abstract
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Abstract
Official abstract text for this publication.
The present invention provides a novel process for preparing a diaminopyrimidine derivative or acid addition salt thereof having an activity as a 5-HT4 receptor agonist. And also, the present invention provides novel crystalline forms of a hydrochloride of the diaminopyrimidine derivative and processes for preparing the same.
First claim
Opening claim text (preview).
The invention claimed is: 1. A crystalline form A of a hydrochloride of a compound of Formula 1, having an XRPD pattern with peaks at 7.4, 9.1, 12.0, 12.5, 13.5, 14.1, 15.9, 16.8, 18.3, 19.1, 24.6, 25.3 and 26.8° 2θ±0.2° 2θ: 2. The crystalline form A of a hydrochloride of the compound of Formula 1 according to claim 1 , having a differential scanning calorimetry (DSC) thermogram showing an endothermic peak at between 229° C. and 235° C. 3. A process for preparing the crystalline form A of a hydrochloride of the compound of Formula 1 according to claim 1 , the process comprising (p) refluxing a reaction mixture obtained by adding hydrochloric acid to a compound of Formula 1 in an organic solvent; (q) cooling the reaction mixture obtained from Step (p) to form a precipitate; and (r) isolating the precipitate of Step (q). 4. A crystalline form B of a hydrochloride of a compound of Formula 1, having an XRPD pattern with peaks at 7.3, 8.8, 11.8, 12.5, 13.2, 13.6, 14.5, 17.7, 18.6, 19.6, 22.0, 24.9, 25.2, and 25.9° 2θ±0.2° 2θ: 5. The crystalline form B of a hydrochloride of the compound of Formula 1 according to claim 4 , having a differential scanning calorimetry (DSC) thermogram showing an endothermic peak at between 229° C. and 235° C. 6. A process for preparing the crystalline form B of a hydrochloride of the compound of Formula 1 according to claim 4 , the process comprises exposing a crystalline form A of a hydrochloride of the compound of Formula 1 having an XRPD pattern with peaks at 7.4, 9.1, 12.0, 12.5, 13.5, 14.1, 15.9, 16.8, 18.3, 19.1, 24.6, 25.3 and 26.8° 2θ±0.2° 2θ, to a 40% or more relative humidity condition so as to control the water contents thereof to about 3.5% or more.
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Classifications
Optical isomers · CPC title
Crystalline forms, e.g. polymorphs · CPC title
Drugs for disorders of the alimentary tract or the digestive system · CPC title
- C07D403/04Primary
directly linked by a ring-member-to-ring-member bond · CPC title
One nitrogen atom and one oxygen or sulfur atom, e.g. cytosine · CPC title
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Frequently asked questions
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- What does patent US11623925B2 cover?
- The present invention provides a novel process for preparing a diaminopyrimidine derivative or acid addition salt thereof having an activity as a 5-HT4 receptor agonist. And also, the present invention provides novel crystalline forms of a hydrochloride of the diaminopyrimidine derivative and processes for preparing the same.
- Who is the assignee on this patent?
- Yuhan Corp
- What technology area does this patent fall under?
- Primary CPC classification C07D403/04. Mapped technology areas include Chemistry & Metallurgy.
- When was this patent published?
- Publication date Tue Apr 11 2023 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 3 related publications on this page (citations in our corpus or others sharing the same primary CPC).