# US 11,078,184 B2 · Dexrabeprazole sodium compound and pharmaceutical composition thereof

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- Number: US 11,078,184 B2
- Document ID: US11078184B2
- Status: Granted
- Kind: B2
- Application number: 16/624,740
- Filed: 2018-06-22
- Published: 2020-07-09
- Granted: 2021-08-03
- Earliest claimed: 2017-06-23
- Assignees: Jiangsu Aosaikang Pharmaceutical Co., Ltd.; Nanjing Hairun Pharmaceutical Co., Ltd.
- Applicants: Jiangsu Aosaikang Pharmaceutical Co., Ltd.; Nanjing Hairun Pharmaceutical Co., Ltd.
- Inventors: Xiangfeng Chen; Hongyu Chen; Xiaoxin Li; Xun Pan; Min Sun
- Web page: https://patentgrep.com/patent/US11078184B2

## CPC

- C07D 401/12: linked by a chain containing hetero atoms as chain links
- A61K 31/4439: containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole (nicotine A61K31/465)
- A61P 1/04: for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
- C07B 2200/13: Crystalline forms, e.g. polymorphs
- C07D: HETEROCYCLIC COMPOUNDS (macromolecular compounds C08)
- A61K: PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES (devices or methods specially adapted for bringing pharmaceutical products into particular physical or administering forms A61J3/00; chemical aspects of, or use of materials for deodorisation of air, for disinfection or sterilisation, or for bandages, dressings, absorbent pads or surgical articles A61L; soap compositions C11D)
- A61P: SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- C07B: GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR (preparation of carboxylic acid esters by telomerisation C07C67/47; telomerisation C08F)

## Abstract

A dexrabeprazole sodium compound includes crystal forms B and C. The crystal form B has good stability and flowability. The crystal form C is an anhydrous crystal form and has good stability and low hygroscopicity. The crystal forms are suitable for preparing a dexrabeprazole sodium preparation.

## Claims

### Claim 1

A dexrabeprazole sodium compound of Formula (I), wherein the dexrabeprazole sodium compound is crystal form C, which has an XRPD pattern represented by angle 2θ with characteristic peaks at 6.22±0.2°, 12.14±0.2°, 12.46±0.2°, 15.82±0.2°, 18.90±0.2°, 22.38±0.2°, 26.56±0.2°, and 28.06±0.2° when measured by Cu target radiation having a DSC pattern with an exothermic peak at about 234° C.±5° C.

### Claim 2 (depends on 1)

A method for preparing the dexrabeprazole sodium compound according to claim 1, comprising the following steps:
1) dissolving dexrabeprazole sodium in methanol or ethanol, concentrating the mixture to dryness under reduced pressure, and repeating the step at least once;
2) adding acetonitrile to the residue obtained in step 1), stirring and concentrating the mixture to dryness under reduced pressure; and
3) adding a solvent toluene or xylene to the residue obtained in step 2), and stirring the mixture for crystallization to obtain the desired compound.

### Claim 3 (depends on 2)

The method according to claim 2, comprising one or more of the following features a) to c):
a) wherein in step 1), the dexrabeprazole sodium is dissolved in methanol;
b) wherein in step 1), the step is repeated for one to six times; and
c) wherein in step 3), the stirring the mixture for crystallization is performed under inert gas protection.

### Claim 4 (depends on 1)

A pharmaceutical composition, comprising the dexrabeprazole sodium compound according to claim 1 and a pharmaceutically acceptable carrier.