Crystal forms of octahydropyrrolo[3,4-c]pyrrole derivatives
A crystal form and drug technology, applied in drug combinations, medical preparations containing active ingredients, allergic diseases, etc., can solve problems such as low oral bioavailability, poor water solubility, and poor druggability
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Embodiment 1
[0094] Embodiment 1 Crystal form I of the present invention
[0095] 1. Preparation of Form I
[0096] The compound represented by formula (I) (307 g) was prepared with reference to the method of Example 3 in International Application WO 2017088759 A1, which was dissolved in DMF (614 mL), heated to 80° C. and stirred for 0.5 h to dissolve, and then slowly cooled to room temperature , crystallization, suction filtration, the filter residue was washed with water (50 mL × 2), and air-dried at 70°C to obtain an off-white solid powder.
[0097] 2. Identification of Form I
[0098] (1) Identification by Empyrean X-ray Powder Diffraction (XRPD) analysis: using Cu-Kα radiation, it has the following characteristic peaks represented by angle 2θ: 7.44°, 7.78°, 8.24°, 12.69°, 12.95°, 14.08°, 14.75 °,15.03°,17.75°,19.71°,20.12°,20.81°,21.30°,21.89°,22.18°,23.27°,25.49°,25.85°,26.08°,26.60°,27.21°,27.44°,27.70°, 28.53°, with an error tolerance of ±0.2°.
[0099] (2) Identification b...
Embodiment 2
[0100] Example 2 Crystal form VII of the present invention
[0101] 1. Preparation of Form VII
[0102] The crystalline form I (500 mg) of the compound represented by formula (I) was added to DMF (2.0 mL), heated to 50° C. to dissolve, then cooled to room temperature, and then dropped into water (20 mL), and stirring was continued at room temperature. After 24 h, the reaction was stopped, suction filtration, and drying to obtain an off-white solid powder.
[0103] 2. Identification of Form VII
[0104] (1) Identification by Empyrean X-ray Powder Diffraction (XRPD) analysis: using Cu-Kα radiation, with the following characteristic peaks represented by angles 2θ: 8.81°, 11.01°, 13.19°, 13.68°, 14.29°, 15.02°, 16.07 °,16.69°,17.49°,18.23°,18.89°,19.78°,20.30°,20.80°,21.70°,22.15°,23.06°,23.52°,24.02°,24.67°,25.10°,25.61°,26.11°, 26.56°, 26.87°, 27.48°, 27.90°, 29.10°, 29.69°, 30.33°, 31.13°, 32.03°, 32.53°, 32.96°, 33.80°, 34.49°, 35.19°, 35.87°, 38.22°, 39.14° , there is a...
Embodiment 3
[0106] Example 3 Crystal form XIII of the present invention
[0107] 1. Preparation of Form XIII
[0108] The crystalline form I (50 mg) of the compound represented by formula (I) was added to acetone (1.0 mL), and the mixture was suspended and stirred at 50° C. for 24 h. The reaction was stopped, suction filtration, and drying to obtain off-white solid powder.
[0109] 2. Identification of Form XIII
[0110] (1) Identification by Empyrean X-ray powder diffraction (XRPD) analysis: using Cu-Kα radiation, with the following characteristic peaks represented by angles 2θ: 7.18°, 8.28°, 12.37°, 13.45°, 14.26°, 14.87°, 17.48 °,17.90°,19.35°,19.95°,20.71°,21.23°,21.45°,22.11°,23.16°,24.95°,25.55°,26.82°,27.07°,27.35°,28.40°,28.94°,29.40°, 29.99°, with an error tolerance of ±0.2°.
[0111] (2) Identification by TA Q2000 Differential Scanning Calorimetry (DSC) analysis: the scanning speed is 10°C / min, containing endothermic peaks at 146.79°C and 164.21°C, with an error toleranc...
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