# US 2022/0033433 A1 · Process for preparing nucleoside prodrugs

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- Number: US 2022/0033433 A1
- Document ID: US20220033433A1
- Status: Published application
- Kind: A1
- Application number: 17/323,367
- Filed: 2021-05-18
- Published: 2022-02-03
- Earliest claimed: 2012-11-16
- Assignees: NuCana plc
- Applicants: NuCana plc
- Inventors: Christopher McGuigan (Deceased); Fabrizio Pertusati
- Web page: https://patentgrep.com/patent/US20220033433A1

## CPC

- C07H 19/20: with the saccharide radical esterified by phosphoric or polyphosphoric acids
- A61P 1/04: for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
- A61P 13/08: of the prostate
- A61P 15/00: Drugs for genital or sexual disorders (for disorders of sex hormones A61P5/24); Contraceptives
- A61P 31/12: Antivirals
- A61P 31/14: for RNA viruses
- A61P 31/18: for HIV
- A61P 31/20: for DNA viruses
- A61P 31/22: for herpes viruses
- A61P 35/00: Antineoplastic agents
- A61P 35/02: specific for leukemia
- B01J 27/128: with iron group metals or platinum group metals
- B82Y 20/00: Nanooptics, e.g. quantum optics or photonic crystals
- C07H 1/00: Processes for the preparation of sugar derivatives
- C07H 19/06: Pyrimidine radicals
- C07H 19/10: with the saccharide radical esterified by phosphoric or polyphosphoric acids
- C07H 19/16: Purine radicals
- H01S 5/34326: {with a well layer based on InGa(Al)P, e.g. red laser}
- C07H: SUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS (derivatives of aldonic or saccharic acids C07C, C07D; aldonic acids, saccharic acids C07C59/105, C07C59/285; cyanohydrins C07C255/16; glycals C07D; compounds of unknown constitution C07G; polysaccharides, derivatives thereof C08B; DNA or RNA concerning genetic engineering, vectors, e.g. plasmids, or their isolation, preparation or purification C12N15/00; sugar industry C13)
- A61P: SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- B01J: CHEMICAL OR PHYSICAL PROCESSES, e.g. CATALYSIS OR COLLOID CHEMISTRY; THEIR RELEVANT APPARATUS
- B82Y: SPECIFIC USES OR APPLICATIONS OF NANOSTRUCTURES; MEASUREMENT OR ANALYSIS OF NANOSTRUCTURES; MANUFACTURE OR TREATMENT OF NANOSTRUCTURES
- H01S: DEVICES USING THE PROCESS OF LIGHT AMPLIFICATION BY STIMULATED EMISSION OF RADIATION [LASER] TO AMPLIFY OR GENERATE LIGHT; DEVICES USING STIMULATED EMISSION OF ELECTROMAGNETIC RADIATION IN WAVE RANGES OTHER THAN OPTICAL

## Abstract

A process for preparing phosphoramidates of nucleosides where a desired enantiomer, having regard to the asymmetric chiral center of the phosphorus atom P, is provided in an enriched amount. The process comprises admixing a nucleoside with a phosphorochloridate in the presence of a catalyst comprising a metal salt selected from the group consisting of salts of Cu, Fe, La and Yb.

## Claims

### Claim at position 1

1-37. (canceled)

### Claim 38

A method of treating cancer, wherein the method comprises administering to a human patient in need thereof a therapeutically effective amount of a composition comprising a compound of the formula:
or a pharmaceutically acceptable salt thereof, wherein the ratio of the RP diastereomer to the Se diastereomer is in the range from 1:20 to 0:100.

### Claim 39 (depends on 38)

The method of treatment of claim 38, wherein the composition further comprises a pharmaceutically acceptable carrier, diluent or excipient.

### Claim 40 (depends on 38)

The method of treatment of claim 38, wherein the cancer is breast cancer.

### Claim 41 (depends on 38)

The method of treatment of claim 38, wherein the cancer is colon cancer.

### Claim 42 (depends on 38)

The method of treatment of claim 38, wherein the cancer is prostate cancer.

### Claim 43 (depends on 38)

The method of treatment of claim 38, wherein the cancer is leukemia.

### Claim 44 (depends on 38)

The method of treatment of claim 38, wherein the composition is administered orally.

### Claim 45 (depends on 38)

The method of treatment of claim 38, wherein the composition is administered parenterally.

### Claim 46 (depends on 45)

The method of treatment of claim 45, wherein the composition is administered intravenously.

### Claim 47 (depends on 38)

The method of treatment of claim 38, wherein the composition is administered topically.