Solid salt forms of alpha-6-mPEG 6-O-hydroxycolone as opioid agonists and uses thereof

文档序号:1655416 发布日期:2019-12-27 浏览:15次 中文

阅读说明:本技术 作为阿片激动剂的α-6-mPEG6-O-羟基可酮的固体盐形式以及其用途 (Solid salt forms of alpha-6-mPEG 6-O-hydroxycolone as opioid agonists and uses thereof ) 是由 P·安德里斯 Y·达塔尔 R·加迪拉胡 B·A·科瓦尔克奇克 G·C·库克里斯 M·米尔梅 于 2013-10-29 设计创作,主要内容包括:本申请中提供了作为阿片激动剂的α-6-mPEG6-O-羟基可酮的固体盐形式以及其用途。本申请中还提供了制备这些固体形式的方法,使用这些固体形式的方法以及包括这些固体形式的药物组合物。(Solid salt forms of alpha-6-mPEG 6-O-hydroxycodone as opioid agonists and uses thereof are provided herein. Also provided herein are methods of making these solid forms, methods of using these solid forms, and pharmaceutical compositions comprising these solid forms.)

1.α-6-mPEG6-O-hydroxycodone in the form of a solid salt.

2. The α -6-mPEG of claim 16-a solid salt form of an O-hydroxycodone, wherein the salt form is a disordered crystalline form.

3. The α -6-mPEG of claim 16A solid salt form of an-O-hydroxycodone, wherein the salt form is a crystalline form.

4. The solid salt form of any one of the preceding claims, wherein the solid salt form is a-6-mPEG6-O-hydroxyketophosphate.

5. The solid salt form of any one of the preceding claims, wherein the a-6-mPEG6the-O-hydroxyketogenic phosphate is a monophosphate.

6. The solid salt form of any one of the preceding claims, wherein the solid salt form has the following X-ray powder diffraction peaks when measured with Cu ka radiation, comprising: 2.0 + -0.2, 15.0 + -0.2 and 17.0 + -0.2 DEG 2 theta.

7. The solid salt form of any one of the preceding claims, wherein the solid salt form has the following X-ray powder diffraction peaks when measured with Cu ka radiation, comprising: 2.0 + -0.2, 5.5 + -0.2, 15.0 + -0.2, 17.0 + -0.2, and 20.5 + -0.2 degrees 2 theta.

8. The solid salt form of any one of the preceding claims, wherein the solid salt form has the following X-ray powder diffraction peaks when measured with Cu ka radiation, comprising: 2.0 +/-0.2, 5.5 +/-0.2, 6.5 +/-0.2, 8.5 +/-0.2, 11.0 +/-0.2, 13.0 +/-0.2, 15.0 +/-0.2, 17.0 +/-0.2, 19.5 +/-0.2, 20.5 +/-0.2, 25.0 +/-0.2, 28.5 +/-0.2 and 29.5 +/-0.2 degrees 2 theta.

9. The solid salt form of any one of the preceding claims, wherein the solid salt form has the following X-ray powder diffraction peaks when measured with Cu ka radiation, comprising: 2.0 +/-0.2, 4.5 +/-0.2, 5.5 +/-0.2, 6.5 +/-0.2, 8.5 +/-0.2, 11.0 +/-0.2, 13.0 +/-0.2, 15.0 +/-0.2, 17.0 +/-0.2, 17.5 +/-0.2, 19.5 +/-0.2, 20.5 +/-0.2, 21.5 +/-0.2, 24.0 +/-0.2, 25.0 +/-0.2, 26.0 +/-0.2, 28.5 +/-0.2 and 29.5 +/-0.2 degrees 2 theta.

10. The solid form of any one of the preceding claims, wherein the solid salt form has at least one X-ray powder diffraction peak selected from the group consisting of: 2.0 +/-0.2, 5.5 +/-0.2, 6.5 +/-0.2, 8.5 +/-0.2, 11.0 +/-0.2, 13.0 +/-0.2, 15.0 +/-0.2, 17.0 +/-0.2, 19.5 +/-0.2, 20.5 +/-0.2, 25.0 +/-0.2, 28.5 +/-0.2 and 29.5 +/-0.2 degrees 2 theta.

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