Dioxolane analogues of uridine for the treatment of cancer

Patent metadata

Field	Value
Publication number	US-10336780-B2
Application number	US-201816208083-A
Country	US
Kind code	B2
Filing date	Dec 3, 2018
Priority date	Aug 25, 2014
Publication date	Jul 2, 2019
Grant date	Jul 2, 2019

Abstract

which are of use in the treatment of cancer, and related aspects.

First claim

The invention claimed is:

1. A compound represented by formula Ia:

wherein:
R 1 is NH 2 ;
R 2 is H;
R 13 is phenyl or naphthyl any of which is optionally substituted with 1, 2 or 3 R 22 ;
R 15 is methyl;
R 16 is C 3 -C 7 cycloalkyl;
each R 22 is independently selected from halo, C 1 -C 6 alkyl, C 2 -C 6 alkenyl, C 1 -C 6 haloalkyl, C 1 -C 6 alkoxy, C 1 -C 6 haloalkoxy, phenyl, hydroxyC 1 -C 6 alkyl, C 3 -C 6 cycloalkyl, C 1 -C 6 alkylcarbonyl, C 3 -C 6 cycloalkylcarbonyl, carboxyC 1 -C 6 alkyl, hydroxy, amino CN, and NO 2 , or any two R 22 groups attached to adjacent ring carbon atoms can combine to form —O—(CR 23 R 23′ ) 1-6 —O—;
R 23 and R 23′ are independently H or C 1 -C 3 alkyl;
or a pharmaceutically acceptable salt and/or solvate thereof.

2. A compound according to claim 1 wherein R 13 is substituted with one or two R 22 .

3. A compound according to claim 1 , wherein R 13 is unsubstituted phenyl.

4. The compound of claim 1 , that is

5. The compound of claim 1 , that is

6. The compound of claim 1 that is

7. The compound of claim 1 that is

8. A pharmaceutical composition comprising a therapeutically effective amount of a compound according to claim 1 in association with a pharmaceutically acceptable adjuvant, diluent or carrier.

9. A pharmaceutical combination comprising a therapeutically effective amount of compound according to claim 1 , further comprising one or more additional therapeutic agent(s) selected from the group consisting of chemotherapeutical agent, multi-drug resistance reversing agent and biological response modifier.

10. The pharmaceutical combination according to claim 9 , wherein the further therapeutic agent is a chemotherapeutical agent.

Assignees

• Medivir Ab

Inventors

• Bethell Richard
• Eneroth Anders
• Klasson Bjorn
• Oberg Fredrik

Classifications

• A61P43/00

  Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00 · CPC title

• A61P35/00

  Antineoplastic agents · CPC title

• A61P1/16

  for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics · CPC title

• C07F9/65586 Primary

  at least one of the hetero rings does not contain nitrogen as ring hetero atom · CPC title

• C07D405/04 Primary

  directly linked by a ring-member-to-ring-member bond · CPC title