Piperidine urea derivatives

Patent metadata

Field	Value
Publication number	US-9770446-B2
Application number	US-201414909784-A
Country	US
Kind code	B2
Filing date	Jul 9, 2014
Priority date	Aug 7, 2013
Publication date	Sep 26, 2017
Grant date	Sep 26, 2017

Abstract

Compounds of the formula I

in which R 1 -R 3 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 that is

No.
Name

“A1”
4-benzoyl-piperidine-1-carboxylic acid methyl-m-tolyl-amide

“A2”
4-benzoyl-piperidine-1-carboxylic acid methyl-p-tolyl-amide

“A3”
4-benzoyl-piperidine-1-carboxylic acid (3-methoxy-phenyl)-

methyl-amide

“A4”
4-benzoyl-piperidine-1-carboxylic acid (4-methoxy-phenyl)-

methyl-amide

“A5”
4-(4-methyl-benzoyl)-piperidine-1-carboxylic acid (4-

methoxy-phenyl)-methyl-amide

“A6”
4-(4-methoxy-benzoyl)-piperidine-1-carboxylic acid (4-

methoxy-phenyl)-methyl-amide

“A7”
4-(3-fluoro-benzoyl)-piperidine-1-carboxylic acid (4-methoxy-

phenyl)-methyl-amide

“A8”
4-(4-fluoro-benzoyl)-piperidine-1-carboxylic acid (4-methoxy-

phenyl)-methyl-amide

“A9”
4-(4-chloro-benzoyl)-piperidine-1-carboxylic acid (4-

methoxy-phenyl)-methyl-amide

“A10”
4-benzoyl-piperidine-1-carboxylic acid (3-cyano-phenyl)-

methyl-amide

“A11”
4-benzoyl-piperidine-1-carboxylic acid (4-cyano-phenyl)-

methyl-amide

“A12”
4-benzoyl-piperidine-1-carboxylic acid (3-fluoro-phenyl)-

methyl-amide

“A13”
4-benzoyl-piperidine-1-carboxylic acid (4-fluoro-phenyl)-

methyl-amide

“A14”
4-benzoyl-piperidine-1-carboxylic acid ethyl-(4-methoxy-

phenyl)-amide

“A15”
4-benzoyl-piperidine-1-carboxylic acid (2-hydroxy-ethyl)-(4-

methoxy-phenyl)-amide

“A16”
(4-benzoyl-piperidin-1-yl)-(2,3-dihydro-indol-1-yl)-methanone

“A17”
(2,3-dihydro-indol-1-yl)-[4-(4-methyl-benzoyl)-piperidin-1-yl]-

methanone

“A18”
(2,3-dihydro-indol-1-yl)-[4-(4-methoxy-benzoyl)-piperidin-1-

yl]-methanone

“A19”
(2,3-dihydro-indol-1-yl)-[4-(3-fluoro-benzoyl)-piperidin-1-yl]-

methanone

“A20”
(2,3-dihydro-indol-1-yl)-[4-(4-fluoro-benzoyl)-piperidin-1-yl]-

methanone

“A21”
[4-(4-chloro-benzoyl)-piperidin-1-yl]-(2,3-dihydro-indol-1-yl)-

methanone

“A22”
(4-benzoyl-piperidin-1-yl)-(3,4-dihydro-2H-quinolin-1-yl)-

methanone

“A23”
4-(4-methoxy-3-methyl-benzoyl)-piperidine-1-carboxylic acid

(4-methoxy-phenyl)-methyl-amide

“A24”
4-(4-methoxy-3-methyl-benzoyl)-piperidine-1-carboxylic acid

ethyl-(4-methoxy-phenyl)-amide

“A25”
4-(3-methyl-benzoyl)-piperidine-1-carboxylic acid (4-

methoxy-phenyl)-methyl-amide

“A26”
4-(3-methyl-benzoyl)-piperidine-1-carboxylic acid ethyl-(4-

methoxy-phenyl)-amide

“A27”
4-(3-methoxy-benzoyl)-piperidine-1-carboxylic acid (4-

methoxy-phenyl)-methyl-amide

“A28”
4-(3-methoxy-benzoyl)-piperidine-1-carboxylic acid ethyl-(4-

methoxy-phenyl)-amide

“A29”
4-(3-fluoro-4-methoxy-benzoyl)-piperidine-1-carboxylic acid

(4-methoxy-phenyl)-methyl-amide

“A30”
4-{4-[1-(2-methoxy-ethyl)-1H-pyrazol-4-yl]-benzoyl}-

piperidine-1-carboxylic acid (4-methoxy-phenyl)-methyl-

amide

“A31”
4-(4-methoxy-benzoyl)-piperidine-1-carboxylic acid {4-[1-(2-

methoxy-ethyl)-1H-pyrazol-4-yl]-phenyl}-methyl-amide

“A32”
4-{4-[1-(2-methoxy-ethyl)-1H-pyrazol-4-yl]-benzoyl}-

piperidine-1-carboxylic acid {4-[1-(2-methoxy-ethyl)-1H-

pyrazol-4-yl]-phenyl}-methyl-amide

“A33”
4-[4-(1-ethyl-1H-pyrazol-4-yl)-benzoyl]-piperidine-1-

carboxylic acid (4-methoxy-phenyl)-methyl-amide

“A34”
4-(4-methoxy-benzoyl)-piperidine-1-carboxylic acid [4-(1-

ethyl-1H-pyrazol-4-yl)-phenyl]-methyl-amide

“A35”
4-{4-[1-(2-pyrrolidin-1-yl-ethyl)-1H-pyrazol-4-yl]-benzoyl}-

piperidine-1-carboxylic acid (4-methoxy-phenyl)-methyl-

amide

“A36”
4-(4-methoxy-benzoyl)-piperidine-1-carboxylic acid methyl-

{4-[1-(2-pyrrolidin-1-yl-ethyl)-1H-pyrazol-4-yl]-phenyl}-amide

“A37”
4-{4-[1-(2-pyrrolidin-1-yl-ethyl)-1H-pyrazol-4-yl]-benzoyl}-

piperidine-1-carboxylic acid methyl-{4-

Assignees

• Merck Patent Gmbh

Inventors

• Buchstaller Hans-Peter
• Dorsch Dieter

Classifications

• A61P35/00

  Antineoplastic agents · CPC title

• A61P9/00

  Drugs for disorders of the cardiovascular system · CPC title

• A61P37/00

  Drugs for immunological or allergic disorders · CPC title

• A61P43/00

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

• A61P25/28

  for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia · CPC title