# US 10,501,426 B1 · Synthesis of thiazole derivative as anticancer and anti-antibiotics resistant bacteria agent

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- Number: US 10,501,426 B1
- Document ID: US10501426B1
- Status: Granted
- Kind: B1
- Application number: 16/246,047
- Filed: 2019-01-11
- Granted: 2019-12-10
- Earliest claimed: 2019-01-11
- Assignees: King Saud University
- Applicants: King Saud University
- Inventors: Yahia Nasser Mabkhot; Jamal Mohammed Ali Khaled; Naiyf Sultan Helial Alaloi Alharbi; Fahd Ali Nasr Mohammed; Fahd Abdo Almekhlafi; Nael Mahmmoud Abutaha; Salim S. Al-Showiman
- Web page: https://patentgrep.com/patent/US10501426B1

## CPC

- C07D 277/16: Sulfur atoms
- A61P 31/04: Antibacterial agents
- A61P 35/00: Antineoplastic agents
- A01N 25/08: containing solids as carriers or diluents
- A01N 43/78: 1,3-Thiazoles; Hydrogenated 1,3-thiazoles
- C07D: HETEROCYCLIC COMPOUNDS (macromolecular compounds C08)
- A61P: SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A01N: PRESERVATION OF BODIES OF HUMANS OR ANIMALS OR PLANTS OR PARTS THEREOF (preservation of food or foodstuff A23); BIOCIDES, e.g. AS DISINFECTANTS, AS PESTICIDES OR AS HERBICIDES (preparations for medical, dental or toiletry purposes which kill or prevent the growth or proliferation of unwanted organisms A61K); PEST REPELLANTS OR ATTRACTANTS; PLANT GROWTH REGULATORS

## Abstract

A thiazole derivative compound includes a compound having the following structural formula: or a pharmaceutically acceptable salt thereof.

## Claims

### Claim 1

A thiazole derivative compound having the formula:
or a pharmaceutically acceptable salt thereof.

### Claim 2 (depends on 1)

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

### Claim 3 (depends on 2)

A method of treating a disease, comprising:
administering to a patient a therapeutically effective amount of the pharmaceutical composition according to claim 2, wherein the disease is selected from the group consisting of cancer and bacterial infection, wherein the cancer is selected from the group consisting of liver cancer, colon cancer and breast cancer and the bacterial infection is caused by Staphylococcus epidermidis.

### Claim 4 (depends on 3)

The method of claim 3, wherein the bacterial infection is antibiotic resistant to at least one of amoxicillin, ciprofloxacin, clindamycin, daptomycin, erythromycin, fosfomycin, fusidic acid, gentamicin, lmipenem, levofloxacin, linezolid, moxifloxacin, mupirocin, oxacillin, rifampin, synercid, teicoplanin, tetracycline, trimethoprim/sulfamethoxazole and vancomycin.

### Claim 5 (depends on 1)

A larvicidal active composition, comprising the compound according to claim 1 and at least one of a carrier, a diluting agent, a filling agent, and a surface active agent.

### Claim 6 (depends on 5)

A method for inhibiting or preventing mosquito growth, comprising applying the larvicidal active composition of claim 5 to a locus infested by at least one of mosquitoes, mosquito larvae, and mosquito eggs.

### Claim 7

A method of synthesizing a compound, comprising:
mixing diethyl 2,2′-(thiocarbonylbis(sulfanediyl)diacetate with phenyl isothiocyanate in an organic solvent to form a mixture; and
adding K2CO3 to the mixture to form a second mixture; and
adjusting a pH of the second mixture to form a compound having the structure:

### Claim 8 (depends on 7)

The method of claim 7, wherein the second mixture is stirred at room temperature for about 12 hours.

### Claim 9 (depends on 8)

The method of claim 8, wherein the organic solvent is dimethyl formamide.

### Claim 10 (depends on 8)

The method of claim 8, wherein adjusting the pH of the second mixture comprises adding aqueous HCl to the second mixture.

### Claim 11 (depends on 8)

The method of claim 8, wherein the compound is in crystal form.