(AZA-)isoquinolinone derivatives

Patent metadata

Field	Value
Publication number	US-9376433-B2
Application number	US-201314420578-A
Country	US
Kind code	B2
Filing date	Jul 12, 2013
Priority date	Aug 8, 2012
Publication date	Jun 28, 2016
Grant date	Jun 28, 2016

Abstract

Compounds of the formula I

in which R 1 , X, Y and n have the meanings indicated in claim 1, are inhibitors of Tankyrase, and can be employed, inter alia, for the treatment of diseases such as cancer, cardiovascular diseases, central nervous system injury and different forms of inflammation.

First claim

The invention claimed is:

1. A compound which is

No.
Name

“A3”
3-[4-(1-hydroxy-1-methyl-ethyl)-phenyl]-2H-isoquinolin-1-one

“A5”
6-fluoro-3-[4-(1-hydroxy-1-methyl-ethyl)-phenyl]-2H-

isoquinolin-1-one

“A6”
7-fluoro-3-[4-(1-hydroxy-1-methyl-ethyl)-phenyl]-2H-

isoquinolin-1-one

“A7”
3-[4-(1-hydroxy-1-methyl-ethyl)-phenyl]-7-methyl-2H-

isoquinolin-1-one

“A8”
3-(4-hydroxymethyl-phenyl)-2H-isoquinolin-1-one

“A16”
7-fluoro-3-{4-[1-(2-hydroxy-ethoxy)-1-methyl-ethyl]-

phenyl}-2H-isoquinolin-1-one

“A20”
3-[4-(1-amino-1-methyl-ethyl)phenyl]-7-fluoro-2H-

isoquinolin-1-one

“A23”
3-[4-(1-hydroxy-1-methyl-ethyl)phenyl]-2H-2,6-naphthyridin-1-

one

“A24”
3-[4-(1-hydroxy-1-methyl-ethyl)phenyl]-2H-2,7-naphthyridin-1-

one

“A25”
7-chloro-3-[4-(1-hydroxy-1-methyl-ethyl)phenyl]-2H-

isoquinolin-1-one

“A26”
3-[4-(1-hydroxy-1-methyl-ethyl)phenyl]-5-methoxy-2H-

isoquinolin-1-one

“A27”
8-fluoro-3-[4-(1-hydroxy-1-methyl-ethyl)phenyl]-2H-

isoquinolin-1-one

“A28”
5-fluoro-3-[4-(1-hydroxy-1-methyl-ethyl)phenyl]-2H-

isoquinolin-1-one

or

“A33”
5,7-difluoro-3-[4-(1-hydroxy-1-methyl-ethyl)-phenyl]-2H-

isoquinolin-1-one

or a pharmaceutically acceptable solvate, salt, tautomer or stereoisomer thereof, or a mixture thereof in all ratios.

2. A medicament comprising at least one compound of claim 1 or a pharmaceutically acceptable salt, solvate, tautomer or stereoisomer thereof, or a mixture thereof in all ratios, and optionally a pharmaceutically acceptable carrier, excipient or vehicle.

3. A medicament comprising at least one compound of claim 1 or a pharmaceutically acceptable salt, solvate, tautomer or stereoisomer thereof, or a mixture thereof in all ratios, and at least one further medicament active ingredient.

4. A kit consisting of separate packs of
(a) an effective amount of a compound of claim 1 or a pharmaceutically acceptable salt, solvate, tautomer or stereoisomer thereof, or a mixture thereof in all ratios, and
(b) an effective amount of a further medicament active ingredient.

Assignees

• Merck Patent Gmbh

Inventors

• Dorsch Dieter
• Buchstaller Hans-Peter

Classifications

• A61P37/00

  Drugs for immunological or allergic disorders · CPC title

• A61P35/02

  specific for leukemia · CPC title

• A61P43/00

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

• A61P35/00

  Antineoplastic agents · CPC title

• A61P9/00

  Drugs for disorders of the cardiovascular system · CPC title