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US 12,528,832 B2Granted
Crystalline or amorphous form of Bcl-2/Bcl-xL inhibitor compound or its salts
AssigneesAscentage Pharma (Suzhou) Co., Ltd., Ascentage Pharma Group Corp Limited
InventorsJianfeng Wen, Yanqiong Lin, Jianpeng Feng, Zhenzhong Shao, Huirong Lu, Weidong Li
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Abstract
Disclosed herein are a crystalline or amorphous form of a Bcl-2/Bcl-xL inhibitor compound or a salt thereof, and a preparation method and application thereof.
Claims21
A crystalline or amorphous form of the compound of formula 1 or its salt:
- wherein the form is selected from the group consisting of:
- a fumarate salt crystalline form I of the compound of formula 1, having an X-ray powder diffraction (XRPD) pattern comprising peaks at angles 2θ of 18.03±0.2°, 28.81±0.2°, and 31.88±0.2°;
- a hydrochloride salt crystalline form II of the compound of formula 1, having an X-ray powder diffraction (XRPD) pattern comprising peaks at angles 2θ of 13.01±0.2°, 21.55±0.2°, 25.95±0.2°, and 31.33±0.2°;
- a nicotinate crystalline form III of the compound of formula 1, having an X-ray powder diffraction (XRPD) pattern comprising peaks at angles 2θ of 15.46±0.2° and 18.06±0.2°;
- a sodium salt crystalline form IV of the compound of formula 1, having an X-ray powder diffraction (XRPD) pattern comprising peaks at angles 2θ of 16.75±0.2°, 32.34±0.2°, 33.48±0.2° and 37.95±0.2°;
- a potassium salt crystalline form V of the compound of formula 1, having an X-ray powder diffraction (XRPD) pattern comprising peaks at angles 2θ of 24.35±0.2°, 30.10±0.2° and 31.41±0.2°;
- a crystalline form VI of the compound of formula 1, having an X-ray powder diffraction (XRPD) pattern comprising peaks at angles 2θ of 3.94±0.2°, 5.09±0.2°, 18.01±0.2°, and 19.08±0.2°, 19.70±0.2°;
- a crystalline form VII of the compound of formula 1, having an X-ray powder diffraction (XRPD) pattern comprising peaks at angles 2θ of 20.18±0.2°, 20.74±0.2°, 29.20±2 0.2°, 29.28±0.2°, and 36.73±0.2°;
- a crystalline form VIII of the compound of formula 1, having an X-ray powder diffraction (XRPD) pattern comprising a peak at angle 2θ of 18.11±0.2°;
- an adipate salt amorphous form IX of the compound of formula 1, wherein the form has a glass transition temperature at 113.4±2.0° C. measured by MDSC;
- an fumarate amorphous form X of the compound of formula 1, wherein the form has a glass transition temperature at 136.6±12.0° C. measured by MDSC;
- a nicotinic acid salt amorphous form XI of the compound of formula 1, wherein the form has a glass transition temperature at 117.9±2.0° C. measured by MDSC;
- an amorphous form XII of the potassium salt of the compound of formula 1, wherein the form has a glass transition temperature at 135.7±2.0° C. measured by MDSC;
- an amorphous form XIII of the sodium salt of the compound of formula 1, wherein the form has a glass transition temperature at 140.9±2.0° C. measured by MDSC;
- an amorphous form XIV of the compound of formula 1, wherein the form has a glass transition temperature at 148.9±2.0° C. measured by MDSC;
- an amorphous form XV of the maleate salt of the compound of formula 1, wherein the form has a glass transition temperature at 91.89±2.0° C. measured by MDSC;
- and
- an amorphous form XVI of the meglumine salt of the compound of formula 1, wherein the form has a glass transition temperature at 66.19±2.0 measured by MDSC.
15 more elements
Dependencies are inferred from the claim text.