09-06-2022 дата публикации
Номер: US20220177468A1
Принадлежит:
Provided herein are integrin inhibitors, compositions thereof, and methods of their uses. Crystalline forms of salts of the inhibitors are also described, along with methods of preparing the crystalline forms. X-ray powder diffraction data, thermogravimetric analysis, and differential scanning calorimetry data are provided for the crystalline forms. The integrin inhibitors are useful for treatment of, inter alia, fibrotic diseases. 1. A crystalline form of a salt of (S)-4-((2-methoxyethyl)(4-(5 ,6 ,7 ,8-tetrahydro-1 ,8-naphthyridin-2-yl)butyl)amino)-2-(quinazolin-4-ylamino)butanoic acid or a solvate thereof.2. The crystalline form of claim 1 , wherein the crystalline form is a crystalline form of a phosphate salt of the (S)-4-((2-methoxyethyl)(4-(5 claim 1 ,6 claim 1 ,7 claim 1 ,8-tetrahydro-1 claim 1 ,8-naphthyridin-2-yl)butyl)amino)-2-(quinazolin-4-ylamino)butanoic acid.3. The crystalline form of claim 2 , wherein the crystalline form is characterized as having an X-ray powder diffraction (XRPD) pattern comprising:a. peaks at angles 2-theta of about 4.31, about 6.76, about 18.89, about 21.29, and about 23.16 degrees,b. peaks at angles 2-theta of about 4.31, about 6.76, about 11.25, about 12.75, about 18.89, about 20.38, about 21.29, about 23.16, about 23.97, and about 24.68 degrees, orc. peaks at angles 2-theta of about 4.31, about 6.76, about 8.55, about 10.04, about 11.25, about 12.75, about 13.76, about 17.20, about 18.02, about 18.89, about 20.38, about 21.29, about 23.16, about 23.97, about 24.68, about 25.50, about 26.18, about 29.88, and about 33.49 degrees.4. The crystalline form of claim 2 , wherein the crystalline form is characterized as having an XRPD pattern comprising peaks at angles 2-theta of about 4.31 and about 6.76 degrees.5. The crystalline form of claim 2 , wherein the crystalline form is characterized as having an XRPD pattern comprising a peak at an angle 2-theta of about 4.31 degrees.6. The crystalline form of claim 2 , wherein the ...
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