IP Library › Granted Patent US 10,005,810
Granted Patent B2
US 10,005,810 · App. 14/442,987 · Granted Jun 26, 2018

Process for preparing nucleoside prodrugs

Inventors: Chirstopher McGuigan (Peterson Super Ely, GB); Fabrizio Pertusati (Cardiff, GB)
Assignee: University College Cardiff Consultants Limited
C07H19/20B01J27/128B82Y20/00C07H1/00C07H19/06C07H19/10C07H19/16H01S5/34326
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Quick Facts
Patent No.
US 10,005,810
App. No.
14/442,987
Granted
Jun 26, 2018
Kind
B2
Abstract

Provided are phosphoramidate nucleoside compounds of Formula (I), or pharmaceutically acceptable salts or esters or solvates thereof, useful in the treatment of cancer, viral infections and other diseases: Also provided is a process for the synthesis of the compounds of Formula (I) 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 (3)

1. A compound represented by:

wherein the ratio of the R P diastereomer to the S P diastereomer is at most 1:20.

2. The compound of claim 1 , wherein the ratio of the R P diastereomer to the S P diastereomer is 0:100.

Assignments (2)
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Jan 21, 2020
From: UNIVERSITY COLLEGE CARDIFF CONSULTANTS LIMITED
To: NUCANA PLC
Reel/Frame 051572/0178 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Aug 3, 2015
From: MCGUIGAN, CHRISTOPHER; PERTUSATI, FABRIZIO
To: UNIVERSITY COLLEGE CARDIFF CONSULTANTS LIMITED
Reel/Frame 036237/0049 →
Priority Claims (2)
GB 1220666.0 · Nov 16, 2012 · national
GB 1307314.3 · Apr 23, 2013 · national
Continuity (1)
Related Publication 20150291650A1 · Oct 15, 2015
Cited By (6)
US 12,226,429 US 12,458,656 US 12,551,499 US 12,686,697 US 12,741,984 US 12,746,251