Ring-fused bicyclic pyridyl derivatives as FGFR4 inhibitors

Patent metadata

Field	Value
Publication number	US-9896449-B2
Application number	US-201615357195-A
Country	US
Kind code	B2
Filing date	Nov 21, 2016
Priority date	Oct 25, 2013
Publication date	Feb 20, 2018
Grant date	Feb 20, 2018

Abstract

The present invention provides a compound of formula (I) or a pharmaceutically acceptable salt thereof;

a method for manufacturing said compound, and its therapeutic uses. The present invention further provides a combination of pharmacologically active agents and a pharmaceutical composition comprising said compound.

First claim

The invention claimed is:

1. A compound of formula (IV) or a salt thereof

wherein
V is selected from CH 2 , O and CH(OH);
W is selected from CH 2 , CH 2 CH 2 and a bond;
R 1 is selected from halogen, C 1 -C 3 alkyl, haloC 1 -C 3 alkyl, hydroxyC 1 -C 3 alkyl, C 3 -C 6 cycloalkyl, CH 2 NR 2 R 3 , CH(CH 3 )NR 2 R 3 , C 1 -C 3 alkoxyC 1 -C 3 alkyl, CH 2 CO 2 H and C(O)H;
R 2 is selected from C 1 -C 3 alkyl and di(C 1 -C 3 alkyl)aminoC 1 -C 3 alkyl;
R 3 is selected from C 1 -C 3 alkyl, C(O)C 1 -C 3 alkyl, C(O)—CH 2 —OH, C(O)—CH 2 —O—CH 3 , C(O)—CH 2 —N(CH 3 ) 2 and S(O) 2 CH 3 ;
or
R 2 and R 3 together with the N atom to which they are attached form a saturated 5- or 6-membered ring optionally comprising one additional heteroatom selected from N, N-oxide, O and S, which ring may be substituted once or more than once with R 4 ;
R 4 is independently selected from C 1 -C 3 alkyl, di(C 1 -C 3 alkyl)amino, C(O)CH 3 and hydroxy;
or
two R 4 attached at the same carbon atom form together with the carbon atom to which they are attached form a 4-, 5- or 6-membered non-aromatic heterocyclic ring comprising at least one heteroatom selected from N, O and S;
or
two R 4 attached at the same ring atom form an oxo group;
R 5 is selected from hydrogen and C 1 -C 3 alkyl.

Assignees

• Buschmann Nicole
• Fairhurst Robin Alec
• Furet Pascal
• Knoepfel Thomas
• Leblanc Catherine
• Liao Lv
• Mah Robert
• Nimsgern Pierre
• Ripoche Sebastien
• Xiong Jing
• Han Bo
• Wang Can
• Zhao Xianglin
• Novartis Ag

Inventors

• Buschmann Nicole
• Fairhurst Robin Alec
• Furet Pascal
• Knoepfel Thomas
• Leblanc Catherine
• Liao Lv
• Mah Robert
• Nimsgern Pierre
• Ripoche Sebastien
• Xiong Jing
• Han Bo
• Wang Can
• Zhao Xianglin

Classifications

• A61P35/00

  Antineoplastic agents · CPC title

• A61P43/00

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

• C07D471/04 Primary

  Ortho-condensed systems · CPC title

• A61K31/5383

  ortho- or peri-condensed with heterocyclic ring systems · CPC title

• A61K31/506

  not condensed and containing further heterocyclic rings · CPC title