Amorphous form of isoquinoline derivative
AssigneevTv Therapeutics LLC
InventorsDharma Rao POLISETTI, Thomas Scott YOKUM, Yuanqiang SUN, James C. QUADA, Jr.
Life of this patent
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Abstract
The present invention provides an amorphous form of(S)-2-(3S,8S)-3-(4-(3,4-dichlorobenzyloxy)phenyl-7-((S)-1-phenylpropyl)-2,3,6,7,8,9-hexahydro-[1,4]-dioxino[2,3-g]isoquinolin-8-ylformylamino)-3-(4-(2,3-dimethylpyridin-4-yl)phenyl)propionic acid dihydrochloride salt, pharmaceutical compositions comprising the same, methods of preparation and use thereof in treating conditions, such as diabetes, where modulation of the human GLP-1 receptor is beneficial.
Claims22
An amorphous form of(S)-2-(3S,8S)-3-(4-(3,4-dichlorobenzyloxy)phenyl-7-((S)-1-phenylpropyl)-2,3,6,7,8,9-hexahydro-[1,4]-dioxino[2,3-g]isoquinolin-8-ylformylamino)-3-(4-(2,3-dimethylpyridin-4-yl)phenyl)propionic acid dihydrochloride salt (OAD2 dihydrochloride salt) characterized by an XRPD profile substantially as shown in FIG. 1.
An amorphous form of(S)-2-(3S,8S)-3-(4-(3,4-dichlorobenzyloxy)phenyl-7-((S)-1-phenylpropyl)-2,3,6,7,8,9-hexahydro-[1,4]-dioxino[2,3-g]isoquinolin-8-ylformylamino)-3-(4-(2,3-dimethylpyridin-4-yl)phenyl)propionic acid dihydrochloride salt (OAD2 dihydrochloride salt) characterized through an X-ray powder diffraction (XRPD) pattern showing the absence of long-range periodic atomic ordering or by an XRPD profile substantially the same as shown in FIG. 1;
- and
- characterized by a Differential Scanning calorimetry (DSC) profile substantially the same as shown in FIG. 2;
- characterized by a Differential Scanning calorimetry (DSC) profile having an endothermic peak between 85-105° C.;
- characterized by a Thermogravimetric Analysis (TGA) profile substantially the same as shown in FIG. 3;
- characterized by a Thermogravimetric Analysis (TGA) profile having a weight loss of between 2-4% from 25 to 125° C.;
- characterized by an infrared (IR) profile substantially the same as shown in FIG. 4;
- characterized by an infrared (IR) profile having peaks at 1731±2 cm−1, 1625±2 cm-1 1612±2 cm−1, and 1509±2 cm−1;
- or
- characterized by an FTIR profile having peaks at the wavenumbers (cm−1) 3361, 3207, 2977, 2931, 2876, 1731, 1662, 1625, 1612, 1562, 1509, 1473, 1458, 1393, 1292, 1241, 1220, 1171, 1123, 1079, 1050, 1029, 1003, 877, 818, 764, 703, and 668.
Dependencies are inferred from the claim text.