JP-2022515239-A5 -

Dates

Publication Date

20221226

Application Date

20191220

Description

[00326] Numerous embodiments are described, and the scope of this disclosure is defined by the appended claims and not by any particular embodiment shown as an example. All references cited throughout this application (including references to literature, published patents, published patent applications, and concurrently pending patent applications) are incorporated herein by reference in their entirety. Unless otherwise defined, all technical and scientific terms used herein are to have the same meaning as those commonly known to those skilled in the art. The following is a description of the claims as they were at the time of filing the application. [Claim 1] The tris(hydroxymethyl)aminomethane salt of the compound represented by the formula of compound 1. [Claim 2] The tris(hydroxymethyl)aminomethane salt according to claim 1, wherein at least 80% by weight is crystalline. [Claim 3] The tris(hydroxymethyl)aminomethane salt according to claim 2, wherein at least 60% by weight is in single-crystal form, at least 70% by weight is in single-crystal form, at least 80% by weight is in single-crystal form, at least 90% by weight is in single-crystal form, at least 95% by weight is in single-crystal form, or at least 99% by weight is in single-crystal form. [Claim 4] A tris(hydroxymethyl)aminomethane salt according to any one of claims 1 to 3, having a chemical purity of at least 60% by weight, at least 70% by weight, at least 80% by weight, at least 90% by weight, at least 95% by weight, or at least 99% by weight. [Claim 5] A tris(hydroxymethyl)aminomethane salt according to any one of claims 1 to 4, which is a hydrate. [Claim 6] The tris(hydroxymethyl)aminomethane salt according to any one of claims 1 to 5, wherein the crystalline form A is characterized by powder X-ray diffraction peaks at 2θ angles (±0.2°) of 4.4°, 15.6°, and 18.9°. [Claim 7] The tris(hydroxymethyl)aminomethane salt according to claim 6, wherein the crystalline form A is further characterized by powder X-ray diffraction peaks at 2θ angles (±0.2°) of 11.5°, 16.4°, 19.6°, and 25.5°. [Claim 8] The tris(hydroxymethyl)aminomethane salt according to claim 6 or 7, wherein the crystalline morphology A is further characterized by at least one powder X-ray diffraction peak at a 2θ angle (±0.2°) selected from 8.7°, 15.2°, 18.6°, 21.4°, and 25.1°. [Claim 9] The tris(hydroxymethyl)aminomethane salt according to any one of claims 6 to 8, wherein the crystalline form A is characterized by a powder X-ray diffraction pattern substantially similar to that in Figure 7A. [Claim 10] The tris(hydroxymethyl)aminomethane salt according to any one of claims 1 to 5, wherein the crystalline form is crystalline form B characterized by powder X-ray diffraction peaks at 2θ angles (±0.2°) of 6.0°, 7.0°, and 7.2°. [Claim 11] The tris(hydroxymethyl)aminomethane salt according to claim 10, wherein the crystalline form B is further characterized by at least one powder X-ray diffraction peak at a 2θ angle (±0.2°) selected from 9.3° and 12.5°. [Claim 12] The tris(hydroxymethyl)aminomethane salt according to claim 10 or 11, wherein the crystalline morphology B is further characterized by at least one powder X-ray diffraction peak at a 2θ angle (±0.2°) selected from 15.6° and 19.0°. [Claim 13] The tris(hydroxymethyl)aminomethane salt according to any one of claims 10 to 12, wherein the crystalline form B is characterized by a powder X-ray diffraction pattern substantially similar to that in Figure 8A. [Claim 14] The tris(hydroxymethyl)aminomethane salt according to any one of claims 1 to 5, wherein the crystalline form is crystalline form C characterized by powder X-ray diffraction peaks at 2θ angles (±0.2°) of 4.5°, 13.5°, and 18.0°. [Claim 15] The tris(hydroxymethyl)aminomethane salt according to claim 14, wherein the crystalline morphology C is further characterized by at least one powder X-ray diffraction peak at a 2θ angle (±0.2°) selected from 14.3°, 18.3°, and 23.5°. [Claim 16] The tris(hydroxymethyl)aminomethane salt according to claim 13 or 14, wherein the crystalline morphology C is further characterized by at least one powder X-ray diffraction peak at a 2θ angle (±0.2°) selected from 16.3°, 19.0°, 21.2°, 22.5°, and 22.8°. [Claim 17] The tris(hydroxymethyl)aminomethane salt according to any one of claims 13 to 16, wherein the crystalline form C is characterized by a powder X-ray diffraction pattern substantially similar to that in Figure 9A. [Claim 18] The sodium salt of the compound represented by the formula of compound 1. [Claim 19] The crystalline form of the compound represented by the formula of compound 1. [Claim 20] The crystalline form according to claim 19, wherein the compound is an anhydrous. [Claim 21] The crystal morphology according to claim 19 or 20, characterized by powder X-ray diffraction peaks at 2θ angles (±0.2°) of 5.8°, 11.6°, and 12.8°. [Claim 22] The crystal morphology according to claim 21, wherein the crystal morphology A is further characte