Inhibitor compounds

Patent metadata

Field	Value
Publication number	US-9834552-B2
Application number	US-201615091980-A
Country	US
Kind code	B2
Filing date	Apr 6, 2016
Priority date	Sep 7, 2012
Publication date	Dec 5, 2017
Grant date	Dec 5, 2017

Abstract

The present invention relates to compounds of formula I

wherein R 1 , R 4 , Ar, W, X and Z are all as defined herein. The compounds of the present invention are known to inhibit the spindle checkpoint function of Monospindle 1 (Mps1—also known as TTK) kinases either directly or indirectly via interaction with the Mps1 kinase itself. In particular, the present invention relates to the use of these compounds as therapeutic agents for the treatment and/or prevention of proliferative diseases, such as cancer. The present invention also relates to processes for the preparation of these compounds, and to pharmaceutical compositions comprising them.

First claim

The invention claimed is:

1. A method of treating a cancer in a patient in need of such treatment, said method comprising administering to said patient a therapeutically effective amount of N2-(2-ethoxy-4-(4-methyl-4H-1,2,4-triazol-3-yl)phenyl)-6-methyl-N8-neopentylpyrido[3,4-d]pyrimidine-2,8-diamine, or a pharmaceutically acceptable salt or solvate thereof, wherein the cancer is selected from lung, colon, breast, ovarian, prostate, liver, pancreas, brain or skin cancer.

2. The method of claim 1 , wherein the cancer is breast cancer.

3. The method of claim 1 , wherein the cancer is lung cancer.

4. The method of claim 1 , wherein the cancer is ovarian cancer.

5. A method of inhibiting Mps1 kinase in a cell, said method comprising contacting the cell with an effective amount of N 2-(2-ethoxy-4-(4-methyl-4H-1,2,4-triazol-3-yl)phenyl)-6-methyl-N8-neopentylpyrido[3,4-d]pyrimidine-2,8-diamine, or a pharmaceutically acceptable salt or solvate thereof.

6. The method of claim 5 , wherein the method is in vitro or in vivo.

7. A method of inhibiting Mps1 kinase activity in a human or animal subject in need of such inhibition, the method comprising administering to said subject an effective amount of N 2-(2-ethoxy-4-(4-methyl-4H-1,2,4-triazol-3-yl)phenyl)-6-methyl-N8-neopentylpyrido[3,4-d]pyrimidine-2,8-diamine, or a pharmaceutically acceptable salt or solvate thereof.

8. The method of claim 1 , wherein the cancer is human cancer.

Assignees

• Cancer Research Tech Ltd

Inventors

• Hoelder Swen
• Blagg Julian
• Solanki Savade
• Woodward Hannah
• Naud Sebastien
• Bavetsias Vassilios
• Sheldrake Peter
• Innocenti Paolo
• Cheung Kwai-Ming J
• Atrash Butrus

Classifications

• A61P43/00

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

• A61P35/00

  Antineoplastic agents · CPC title

• A61K31/4375 Primary

  the heterocyclic ring system containing a six-membered ring having nitrogen as a ring heteroatom, e.g. quinolizines, naphthyridines, berberine, vincamine · CPC title

• A61K31/519

  ortho- or peri-condensed with heterocyclic rings · CPC title

• C07D471/04 Primary

  Ortho-condensed systems · CPC title