US 10,294,219 B2 · Ledipasvir crystal form and preparation method thereof

Abstract

The present invention relates to a novel Ledipasvir (LDV) crystal form and a preparation method thereof. Specifically, disclosed is an LDV solvate. The solvate is a solvate formed by LDV and a solvent A and/or a solvent B, wherein the solvent A is acetonitrile or acetone; and the solvent B is methyl tertiary butyl ether (MTBE). Also disclosed are a preparation method and an application of the solvate. The solvate has a high purity, a good crystallization property, and better optical stability. The preparation method is simple and the process is stable. The solvate can significantly improve quality control and industrial applications of LDV-containing drugs.

Claims17

Dependent claims

A Ledipasvir solvate, wherein which is a solvate of LDV formed with component A and component B, wherein the component A is acetonitrile or acetone, and the component B is methyl tert-butyl ether (MTBE);

and the solvate is selected from the group consisting of:
(i-1) LDV-acetonitrile-MTBE ternary solvate (crystal form A);
and
(i-2) LDV-acetone-MTBE ternary solvate (crystal form B).

1 more element

Dependencies are inferred from the claim text.

Facts

Application

15/741,963Filed 24 Jun 2016

Priority

CN 2015 1 03937676 Jul 2015

Published

US 2018/0194752 A112 Jul 2018

Granted

21 May 2019

Term ends

Not estimatedThe source records don’t support an estimate.

Classification8 codes

C07D 403/14
Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group…
A61K 31/4439
Containing further heterocyclic ring systems: containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
A61P 31/14
Antivirals: for RNA viruses
C07B 2200/13
Indexing scheme relating to specific properties of organic compounds: crystalline forms, e.g. polymorphs

Ledipasvir crystal form and preparation method thereof

Life of this patent

Ledipasvir crystal form and preparation method thereof

Life of this patent

Abstract

Claims17