Fluorocyclopentenylcytosine methods of use
AssigneeRexahn Pharmaceuticals, Inc.
InventorsYoung Bok Lee, Deog Joong Kim, Godefridus J. Peters, Reza Mazhari, Dzjemma Sarkisjan
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Abstract
The disclosed subject matter provides methods using and kits comprising a compound of formula (I) or a hydrate, a solvate, or a pharmaceutically acceptable salt thereof. The disclosed subject matter further provides a method of treating one or more symptoms of cancer comprising administering to a subject in need thereof a compound of formula (I) and a process for preparing such.
Claims20
A method of predicting efficacy of treatment of a subject in need thereof with a compound of formula (I)
- or a hydrate, a solvate, or a pharmaceutically acceptable salt thereof, comprising the steps of:
- collecting a sample of tumor cell or tissue from the subject;
- and
- (ii) measuring the level of UCK2 expression in the tumor cell or tissue;
- wherein an increase in the expression level of UCK2 indicates a likelihood of efficacy of treatment with a compound of formula (I).
A method of predicting efficacy of treatment of a subject in need thereof with a compound of formula (I)
- or a hydrate, a solvate, or a pharmaceutically acceptable salt thereof, by the steps of:
- (i) collecting a sample of tumor cell or tissue from the subject;
- (ii) measuring one of protein kinases or p53 expression level in the sample;
- (iii) contacting the tumor cell or tissue with a compound of formula (I);
- (iv) measuring one of protein kinases or p53 expression level in the tumor cell or tissue after contact with the compound of formula (I), wherein an increase in protein kinases or p53 expression level indicates likelihood of efficacy.
A process for preparing of 4-amino-1-((1 S,4R,5S)-2-fluoro-4,5-dihydroxy-3-(hydroxymethyl)cyclopent-2-en-1-yl)pyrimidin-2(1H)-one 1H2O (RX-3117-MH), comprising
- converting tert-butyl(((3aR,4R,6aR)-5-fluoro-2,2-dimethyl-6-((trityloxy)methyl)-4,6a-dihydro-3aH-cyclopenta[d][1,3]dioxol-4-yl)oxy)diphenylsilane (ASM11) to 4-amino-1-((3aS,4S,6aR)-5-fluoro-2,2-dimethyl-6-((trityloxy)methyl)-4,6a-dihydro-3aH-cyclopenta[d][1,3]dioxol-4-yl)pyrimidin-2(1H)-one (INT14) in a continuous process with more than one step without isolation of any intermediate.
Dependencies are inferred from the claim text.