Fluorocyclopentenylcytosine methods of use
AssigneeRexahn Pharmaceuticals, Inc.
InventorsYoung Bok Lee, Deog Joong Kim, Reza Mazhari, Godefridus J. Peters, 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 treating a tumor comprising administering to a subject in need thereof an oral dosage form comprising an effective amount of a compound of formula (I)
- or a hydrate, a solvate, or a pharmaceutically acceptable salt thereof, at a dosage of about 300-2,000 mg/day.
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:
- (i) 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 the expression level of UCK2 indicates a likelihood of efficacy of treatment with a compound of formula (I).
A method of sensitizing a cell to an apoptotic signal comprising contacting the cell with an effective amount of a compound of formula (I)
- or a hydrate, a solvate, or a pharmaceutically acceptable salt thereof.
A process for preparing of 4-amino-1-((1S,4R,5S)-2-fluoro-4,5-dihydroxy-3-(hydroxymethyl)cyclopent-2-en-1-yl)pyrimidin-2(1H)-one 1H20 (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]dioxo1-4-yl)oxy)diphenyl silane (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.