CRYSTAL FORM OF GONADOTROPIN RELEASING HORMONE ANTAGONIST, PREPARATION METHOD THEREFOR, AND USE THEREOF

    公开(公告)号:US20220169658A1

    公开(公告)日:2022-06-02

    申请号:US17675576

    申请日:2022-02-18

    IPC分类号: C07D495/04

    摘要: Provided are a crystal form of a gonadotropin releasing hormone antagonist, a preparation method therefor, and use thereof. A crystal form C and a crystal form D have high purity, good illumination stability, high temperature stability, and high humidity stability, and have good solubility and low hygroscopicity; the saturation solubility of the crystal form C and the crystal form D is 101.75 μg/ml and 87.21 μg/ml, respectively; when the relative humidity is increased from 0 to 50% RH, the hygroscopy gain of the crystal form C and the crystal form D is not greater than 1.76% and 0.73%, respectively; and when the relative humidity is increased from 0 to 90% RH, the hygroscopy gain of the crystal form C and the crystal form D is not greater than 3.43% and 1.61%, respectively. Therefore, the control of a production condition is facilitated, the preparation process is simple, the quality is stable, and large-scale industrial production is easy.

    EUTECTIC FORM A OF ELAGOLIX AND PYRIMETHAMINE, PREPARATION METHOD THEREFOR AND USE THEREOF

    公开(公告)号:US20220143019A1

    公开(公告)日:2022-05-12

    申请号:US17586160

    申请日:2022-01-27

    IPC分类号: A61K31/513 A61K31/505

    摘要: Disclosed are eutectic form A of Elagolix and pyrimethamine, a preparation method therefor and a use thereof. Using Cu-Kα radiation, eutectic form A has characteristic peaks represented by a 20 degree at 8.1±0.2°, 12.2±0.2°, 13.3±0.2° and 21.1±0.2° in an X-ray powder diffraction. Eutectic form A has a high purity, a good light radiation stability, a high temperature stability, a high humidity stability and an accelerated stability, is easy to store, and has a slow moisture absorption under the condition of relatively low humidity, wherein the weight gain of eutectic form A by moisture absorption is not more than 1.08% when the relative humidity increases from 0 to 60% RH. Production conditions for eutectic form A are easy to control, same has a simple preparation process and a stable quality, and is easy to industrially produce on a large-scale.