Salts of morpholine derivative, crystal forms thereof, processes for producing the same, pharmaceutical compositions including the same, and use thereof
US10519150B2 · kind B2 · utility
Assignee
Inventors
Key dates
| Filing date | Dec 29, 2016 |
| Grant date | Dec 31, 2019 |
| Priority date | — |
| Expiry date | Dec 29, 2036 |
Classification
- Technology area (CPC C)Chemistry; Metallurgy
- CPC primaryC07B2200/13
- WIPO fieldPharmaceuticals
- WIPO sectorChemistry
Abstract
The present invention provides novel pharmaceutically acceptable salts of a morpholine derivative, including a malate, a tartrate, a hydrochloride, an acetate, and a naphthalene disulfonate thereof, wherein the tartrate has 3 crystal salt forms: crystal form A, crystal form B and dihydrate; the malate, the hydrochloride, and the acetate each have one crystal salt form; the naphthalene disulfonate is amorphous. When compared to the known morpholine derivative free base, the present invention has one or more improved properties, e.g., a better crystalline state, greatly improved water solubility, light stability and thermal stability, etc. The present invention further provides preparation methods for the salts of morpholine derivative and the crystal forms thereof, pharmaceutical compositions and use thereof.
Source: USPTO / EPO open patent data. Objective bibliographic and citation counts.