JP-2022512399-A5 -

Dates

Publication Date

20221219

Application Date

20191212

Description

The scope of the present invention should therefore not be determined by reference to the above detailed description, but rather by reference to the appended claims below, in accordance with the entire scope equivalent to that which is granted by such claims. In one embodiment, for example, the following items are provided. (Item 1) Compound 1 or the crystalline solid form of its hydrate or solvate. (Item 2) The crystalline solid form of compound 1 as described in item 1, characterized in that the crystalline solid form of compound 1 is morphology A, morphology B, morphology C, morphology D, morphology E, morphology F, morphology G, morphology H, morphology K, morphology O, or morphology Q. (Item 3) The crystalline solid form described in item 2, characterized as compound form 1A. (Item 4) The compound 1 form A is characterized by one or more peaks in the XRPD pattern at a 2θ scale of ±0.20, and these one or more peaks are located at 5.48, 9.93, 10.83, 10.98, 11.36, 11.79, 12.04, 12.25, 12.62, 14.33, 14.67, 15.33, 16.02, 16.51, 16.77, 18.07, 19.09, 19.34, 19.60, and 20. A crystalline solid form as described in any one of items 2 to 3, selected from 00, 20.46, 20.85, 21.45, 21.55, 21.76, 22.16, 22.35, 22.58, 22.87, 23.79, 24.11, 24.29, 24.35, 24.87, 25.42, 25.81, 26.09, 26.72, 27.04, 27.44, 27.77, 27.98, 28.19, and 28.56. (Item 5) The crystalline solid form of compound 1 form A is characterized by one or more peaks in the XRPD pattern at a 2θ scale of ±0.20, wherein the one or more peaks are selected from 10.83, 10.98, 11.36, 11.79, 12.04, 14.33, 18.07, 19.09, 20.00, 22.58, 24.87, and 28.19, as described in any one of items 2 to 4. (Item 6) The crystalline solid form of compound 1A is characterized by all of the following peaks in the XRPD pattern at a 2θ scale ±0.20, wherein the peaks are 10.83, 10.98, 11.36, 11.79, 12.04, 14.33, 18.07, 19.09, 20.00, 22.58, 24.87, and 28.19, as described in any one of items 2 to 5. (Item 7) The compound 1 form A is characterized by all of the following peaks in the XRPD pattern at a 2θ scale of ±0.20, where the peaks are 5.48, 9.93, 10.83, 10.98, 11.36, 11.79, 12.04, 12.25, 12.62, 14.33, 14.67, 15.33, 16.02, 16.51, 16.77, 18.07, 19.09, 19.34, 19.60, 20 A crystalline solid form according to any one of items 2 to 6, wherein the values are 00, 20.46, 20.85, 21.45, 21.55, 21.76, 22.16, 22.35, 22.58, 22.87, 23.79, 24.11, 24.29, 24.35, 24.87, 25.42, 25.81, 26.09, 26.72, 27.04, 27.44, 27.77, 27.98, 28.19, and 28.56. (Item 8) The crystalline solid form of compound 1 form A is characterized by endothermic activity having a starting temperature of over 200°C in a DSC thermogram, as described in any one of items 2 to 7. (Item 9) The crystalline solid form of compound 1 form A is characterized by weight loss at temperatures above 200°C in a TGA thermogram, as described in any one of items 2 to 8. (Item 10) The crystalline solid form of compound 1 form A described in any one of items 2 to 9, characterized by a weight increase of approximately 0.8 to approximately 1.0 wt% as determined by DVS analysis when sampled in an environment with a relative humidity of 5% to 95%. (Item 11) The crystalline solid form described in item 2, characterized as compound form 1B. (Item 12) The crystalline solid form of compound 1 form B is characterized by one or more peaks in an XRPD pattern at a 2θ scale of ±0.2, wherein the one or more peaks are selected from 9.58, 10.49, 11.27, 12.10, 13.26, 13.52, 15.15, and 16.69, as described in item 11. (Item 13) The crystalline solid form of compound 1 form B is characterized by one or more peaks in an XRPD pattern at a 2θ scale ±0.2, wherein the one or more peaks are selected from 10.49, 12.10, 13.26, and 13.52, as described in any one of items 11 to 12. (Item 14) The crystalline solid form of compound 1 form B is characterized by all of the following peaks in the XRPD pattern at a 2θ scale ±0.2, wherein the peaks are 10.49, 12.10, 13.26, and 13.52, according to any one of items 11 to 13. (Item 15) The crystalline solid form of compound 1 form B is characterized by all of the following peaks in the XRPD pattern at a 2θ scale ±0.2, wherein the peaks are 9.58, 10.49, 11.27, 12.10, 13.26, 13.52, 15.15, and 16.69, as described in any one of items 11 to 14. (Item 16) The crystalline solid form of compound 1 form B is characterized by a first weight loss of approximately 0.3 wt% between temperatures of 38 and 92°C and a second weight loss of approximately 11.2 wt% between temperatures of 92 and 188°C, as shown in the TGA thermogram, according to any one of items 11 to 15. (Item 17) The crystalline solid form described in item 2, characterized as compound form 1C. (Item 18) The crystalline solid form of compound 1 form C is characterized by one or more peaks in an XRPD pattern at a 2θ scale of ±0.2, wherein the one or more peaks are selected from 3.89, 7.95, 9.31, 10.54, 12.96, 16.61, 17.64, and 20.47, as described in item 17. (Item 19) The crystalline solid form of co