13-05-2021 дата публикации
Номер: US20210139511A1
Принадлежит:
This application relates to solid forms and salt forms of the PD-1/PD-L1 inhibitor 4,4′-(((((2,2′-dichloro-[1,1′-biphenyl]-3,3′-diyl)bis(azanediyl))bis(carbonyl))bis(1-methyl-1,4,6,7-tetrahydro-5H-imidazo[4,5-c]pyridine-2,5-diyl))bis(ethane-2,1-diyl))bis(bicyclo[2.2.1]heptane-1-carboxylic acid), including processes of preparation thereof, where the solid forms and salt forms are useful in the treatment of various diseases including infectious diseases and cancer. 1. A salt , which is 4 ,4′-(((((2 ,2′-dichloro-[1 ,1′-biphenyl]-3 ,3′-diyl)bis(azanediyl))bis(carbonyl))bis(1-methyl-1 ,4 ,6 ,7-tetrahydro-5H-imidazo[4 ,5-c]pyridine-2 ,5-diyl))bis(ethane-2 ,1-diyl))bis(bicyclo[2.2.1]heptane-1-carboxylic acid) di-hydrochloric acid salt.2. The salt of claim 1 , having Form I.3. The salt of claim 2 , having an X-ray powder diffraction pattern as substantially shown in .4. The salt of claim 2 , having a DSC thermogram substantially as depicted in .5. The salt of claim 2 , having a thermogravimetric analysis (TGA) thermogram substantially as depicted in .6. The salt of claim 2 , having at least one X-ray powder diffraction (XRPD) peak claim 2 , in terms of 2-theta (±0.2 degrees) claim 2 , selected from 5.7 claim 2 , 8.5 claim 2 , 9.6 claim 2 , 9.9 claim 2 , 11.8 claim 2 , 12.3 claim 2 , 13.1 claim 2 , 13.4 claim 2 , 13.8 claim 2 , 14.2 claim 2 , 14.5 claim 2 , 15.4 claim 2 , 15.8 claim 2 , 16.8 claim 2 , 17.3 and 17.6 degrees.7. The salt of claim 2 , having at least two X-ray powder diffraction (XRPD) peaks claim 2 , in terms of 2-theta (±0.2 degrees) claim 2 , selected from 5.7 claim 2 , 8.5 claim 2 , 9.6 claim 2 , 9.9 claim 2 , 11.8 claim 2 , 12.3 claim 2 , 13.1 claim 2 , 13.4 claim 2 , 13.8 claim 2 , 14.2 claim 2 , 14.5 claim 2 , 15.4 claim 2 , 15.8 claim 2 , 16.8 claim 2 , 17.3 and 17.6 degrees.8. The salt of claim 2 , having at least three X-ray powder diffraction (XRPD) peaks claim 2 , in terms of 2-theta (±0.2 degrees) claim 2 , selected from 5.7 claim 2 , 8.5 claim 2 , ...
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