# US 11,993,664 B2 · Crystalline form of compound and uses thereof in medicine

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- Number: US 11,993,664 B2
- Document ID: US11993664B2
- Status: Granted
- Kind: B2
- Application number: 17/270,197
- Filed: 2019-08-22
- Published: 2021-10-21
- Granted: 2024-05-28
- Earliest claimed: 2018-08-22
- Assignees: Waterstone Pharmaceuticals(Wuhan) Co., Ltd.
- Applicants: Waterstone Pharmaceuticals(Wuhan) Co., Ltd.
- Inventors: Jian Cui; Yao Yu; Minglong Hu
- Web page: https://patentgrep.com/patent/US11993664B2

## CPC

- A61K 31/395: having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- C07K 7/645: {Cyclosporins; Related peptides}
- A61K 31/4178: not condensed 1,3-diazoles and containing further heterocyclic rings, e.g. pilocarpine, nitrofurantoin
- A61K 31/439: the ring forming part of a bridged ring system, e.g. quinuclidine (8-azabicyclo [3.2.1] octanes A61K31/46)
- A61K 31/7056: containing five-membered rings with nitrogen as a ring hetero atom
- A61K 31/7072: having two oxo groups directly attached to the pyrimidine ring, e.g. uridine, uridylic acid, thymidine, zidovudine
- A61K 38/13: Cyclosporins
- A61K 38/212: {IFN-alpha}
- A61P 31/12: Antivirals
- A61P 31/14: for RNA viruses
- C07B 2200/13: Crystalline forms, e.g. polymorphs
- Y02A 50/30: Against vector-borne diseases, e.g. mosquito-borne, fly-borne, tick-borne or waterborne diseases whose impact is exacerbated by climate change
- 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)
- C07K: PEPTIDES (peptides in foodstuffs A23; obtaining protein compositions for foodstuffs, working-up proteins for foodstuffs A23J; preparations for medicinal purposes A61K; peptides containing beta-lactam rings C07D; cyclic dipeptides not having in their molecule any other peptide link than those which form their ring, e.g. piperazine-2,5-diones, C07D; ergot alkaloids of the cyclic peptide type C07D519/02; macromolecular compounds having statistically distributed amino acid units in their molecules, i.e. when the preparation does not provide for a specific; but for a random sequence of the amino acid units, homopolyamides and block copolyamides derived from amino acids C08G69/00; macromolecular products derived from proteins C08H1/00; preparation of glue or gelatine C09H; single cell proteins, enzymes C12N; genetic engineering processes for obtaining peptides C12N15/00; compositions for measuring or testing processes involving enzymes C12Q; investigation or analysis of biological material G01N33/00)
- 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)
- Y02A: TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE

## Abstract

A crystalline form A of the compound having formula (I) and uses thereof in medicine are described. Specifically, it relates to crystalline form A and pharmaceutically compositions thereof. Furthermore, it relates to the uses of crystalline form A disclosed herein and pharmaceutically compositions thereof disclosed herein in the manufacture of a medicament, especially in the manufacture of a medicament for preventing, managing, treating or lessening hepatitis C vims (HCV) infection.

## Claims

### Claim 1

The crystalline form A of the compound having formula (I):
wherein the crystalline form A exhibits the following characteristic X-ray powder diffraction peaks expressed in degrees 2θ at 8.66±0.2°, 9.64±0.2°, 10.36±0.2°, 11.20±0.2°,18.39±0.2°.

### Claim 2 (depends on 1)

The crystalline form A of claim 1, wherein the crystalline form A exhibits the following characteristic X-ray powder diffraction peaks expressed in degrees 2θ at 6.08±0.2°, 8.66±0.2°, 9.64±0.2°, 10.36±0.2°, 11.20±0.2°, 13.00±0.2°, 14.14±0.2°, 14.90±0.2°, 18.39±0.2°, 20.40±0.2°, 22.04±0.2°.

### Claim 3 (depends on 1)

The crystalline form A of claim 1, wherein the crystalline form A exhibits the following characteristic X-ray powder diffraction peaks expressed in degrees 2θ at 6.08±0.2°, 8.66±0.2°, 9.64±0.2°, 10.36±0.2°, 11.20±0.2°, 12.58±0.2°, 13.00±0.2°, 13.58±0.2°, 14.14±0.2°, 14.90±0.2°, 15.36±0.2°, 15.98±0.2°, 16.71±0.2°, 17.69±0.2°, 18.39±0.2°, 18.78±0.2°, 19.38±0.2°, 20.40±0.2°, 21.71±0.2°, 22.04±0.2°, 22.49±0.2°, 23.20±0.2°, 23.88±0.2°, 24.99±0.2°, 25.82±0.2°, 26.77±0.2°, 27.61±0.2°, 28.43±0.2°, 29.62±0.2°, 31.36±0.2°.

### Claim 4 (depends on 1)

The crystalline form A of claim 1, wherein the crystalline form A has a differential scanning calorimetry thermogram comprising an endothermic peak at 143.8° C.±3° C., 172.6° C.±3° C.

### Claim 5 (depends on 1)

A pharmaceutical composition comprising the crystalline form A of claim 1, wherein the pharmaceutical composition further comprises a pharmaceutically acceptable excipient, or a combination of the excipients.

### Claim 6 (depends on 5)

The pharmaceutical composition according to claim 5 further comprising other anti-HCV drug.

### Claim 7 (depends on 6)

The pharmaceutical composition according to claim 6, wherein the other anti-HCV drug is Ledipasvir/sofosbuvir, Sofosbuvir, Ribavirin, Peginterferon alfa-2a or Daclatasvir.

### Claim 8 (depends on 1)

A method of preventing, treating or lessening a disorder or disease caused by a virus infection in a patient comprising administering to the patient a therapeutically effective amount of the crystalline form A according to claim 1.

### Claim 9 (depends on 8)

The method according to claim 8, wherein the virus infection is hepatitis C infection.