# US 11,299,482 B2 · Salt and crystal form of modified andrographolide compound and preparation method thereof

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- Number: US 11,299,482 B2
- Document ID: US11299482B2
- Status: Granted
- Kind: B2
- Application number: 16/616,300
- Filed: 2018-05-24
- Published: 2021-09-16
- Granted: 2022-04-12
- Earliest claimed: 2017-05-24
- Assignees: Medshine Discovery Inc.; Heilongjiang Zhenbaodao Pharmaceutical Co., Ltd.
- Applicants: Heilongjiang Zhenbaodao Pharmaceutical Co, Ltd; Medshine Discovery Inc.
- Inventors: Jianhua Xia; Zhigan Jiang; Haiying He; Jing Wang
- Web page: https://patentgrep.com/patent/US11299482B2

## CPC

- C07D 405/12: linked by a chain containing hetero atoms as chain links
- A61P 11/00: Drugs for disorders of the respiratory system
- C07B 2200/13: Crystalline forms, e.g. polymorphs
- C07D: HETEROCYCLIC COMPOUNDS (macromolecular compounds C08)
- 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

The present invention provides a salt and crystal form of a modified andrographolide compound and a preparation method and pharmaceutical use thereof.

## Claims

### Claim 1

A crystal Form A of a compound of Formula (II);
having an X-ray powder diffraction pattern comprising characteristic diffraction peaks at 2θ angles of: 10.00±0.2°, 12.91±0.2°, and 16.27±0.2°.

### Claim 2 (depends on 1)

The Crystal Form A according to claim 1, which has an X-ray powder diffraction pattern comprising characteristic diffraction peaks at 2θ angles of: 5.05±0.2°, 10.00±0.2°, 12.91±0.2°, 13.42±0.2°, 14.51±0.2°, 14.94±0.2°, 16.27±0.2°, and 18.36±0.2°.

### Claim 3 (depends on 2)

The Crystal Form A according to claim 2, which has an XRPD pattern as shown in FIG. 1.

### Claim 4 (depends on 1)

The Crystal Form A according to claim 1, which has a differential scanning calorimetry curve comprising endothermic peaks at 119.27° C.±3° C. and 144.42° C.±3° C.

### Claim 5 (depends on 4)

The Crystal Form A according to claim 4, which has a DSC pattern as shown in FIG. 2.

### Claim 6 (depends on 1)

The Crystal Form A according to claim 1, which has a thermogravimetric analysis curve showing a weight loss of 0.1268%±0.1% at 120.00° C. ±3° C.

### Claim 7 (depends on 6)

The Crystal Form A according to claim 6, which has a TGA pattern as shown in FIG. 3.