Inhibitors of tyk2
US-2024425484-A1 · Dec 26, 2024 · US
US11680055B2 · US · B2
| Field | Value |
|---|---|
| Publication number | US-11680055-B2 |
| Application number | US-201816650106-A |
| Country | US |
| Kind code | B2 |
| Filing date | Sep 27, 2018 |
| Priority date | Sep 28, 2017 |
| Publication date | Jun 20, 2023 |
| Grant date | Jun 20, 2023 |
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A main object of the present invention is to provide new crystals of (S)-N 2 -[1-(4-fluorophenyl)ethyl]-4-(1-methyl-1H-pyrazol-4-yl)-N 6 -(pyrazin-2-yl)pyridine-2,6-diamine maleate (hereinafter, referred to as “compound A”). A Form-I crystal of the compound A, showing diffraction peaks in its X-ray powder diffraction spectrum at least at the following angles of diffraction 2θ: 6.9 degrees, 9.4 degrees, 12.5 degrees, 15.1 degrees, 16.4 degrees, 18.3 degrees, 19.0 degrees, 24.9 degrees, 25.4 degrees, 27.3 degrees, and 27.7 degrees, wherein X-ray powder diffraction spectrum is obtained by using Cu Kα radiation (λ=1.54 Å). A Form-II crystal of the compound A, showing diffraction peaks in its X-ray powder diffraction spectrum at least at the following angles of diffraction 2θ: 6.9 degrees, 9.2 degrees, 12.4 degrees, 14.8 degrees, 16.5 degrees, 18.1 degrees, 18.5 degrees, 19.8 degrees, 23.6 degrees, 24.9 degrees, and 27.7 degrees, wherein X-ray powder diffraction spectrum is obtained by using Cu Kα radiation (λ=1.54 Å).
Opening claim text (preview).
The invention claimed is: 1. A Form-I crystal of (S)-N 2 -[(1-(4-fluorophenyl)ethyl]-4-(1-methyl-1H-pyrazol-4-yl)-N 6 -(pyrazin-2-yl)pyridine-2,6-diamine maleate, showing diffraction peaks in its X-ray powder diffraction spectrum at least at the following angles of diffraction 2θ: 6.9 degrees, 9.4 degrees, 12.5 degrees, 15.1 degrees, 16.4 degrees, 18.3 degrees, 19.0 degrees, 24.9 degrees, 25.4 degrees, 27.3 degrees, and 27.7 degrees, wherein X-ray powder diffraction spectrum is obtained by utilizing Cu Kα radiation (λ=1.54 Å). 2. A Form-I crystal of (S)-N 2 -[1-(4-fluorophenyl)ethyl]-4-(1-methyl -1H-pyrazol-4-yl)-N 6 -(pyrazin-2-yl)pyridine-2,6-diamine maleate, having an endothermic peak at 203±3° C. in differential scanning calorimetry. 3. A pharmaceutical composition containing the crystal according to claim 1 as an active ingredient and a pharmaceutically acceptable carrier. 4. A pharmaceutical composition containing the crystal according to claim 2 as an active ingredient and a pharmaceutically acceptable carrier. 5. The crystal according to claim 1 , having an endothermic peak at 203±3° C. in differential scanning calorimetry. 6. A pharmaceutical composition containing the crystal according to claim 5 as an active ingredient and a pharmaceutically acceptable carrier.
containing three or more hetero rings · CPC title
Crystalline forms, e.g. polymorphs · CPC title
Maleic acid · CPC title
Drugs for disorders of the blood or the extracellular fluid · CPC title
containing further heterocyclic rings · CPC title
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