US 11,999,758 B2
Inhibitors of the YAP/TAZ-TEAD interaction and their use in the treatment of cancer
Martine Barth, Asnieres les Dijon (FR); Sylvie Contal, Pouilley-les-Vignes (FR); Jean-Louis Junien, Paris (FR); Christine Massardier, Dijon (FR); Christian Montalbetti, Fontaine-lès-Dijon (FR); and Anne Soude, Marsannay-la-Côte (FR)
Assigned to INVENTIVA, Daix (FR)
Appl. No. 17/278,429
Filed by INVENTIVA, Daix (FR)
PCT Filed Oct. 2, 2019, PCT No. PCT/EP2019/076681
§ 371(c)(1), (2) Date Mar. 22, 2021,
PCT Pub. No. WO2020/070181, PCT Pub. Date Apr. 9, 2020.
Claims priority of application No. 18306294 (EP), filed on Oct. 2, 2018.
Prior Publication US 2021/0323982 A1, Oct. 21, 2021
Int. Cl. C07F 5/02 (2006.01); A61P 35/00 (2006.01)
CPC C07F 5/025 (2013.01) [A61P 35/00 (2018.01)] 19 Claims
OG exemplary drawing
 
1. A compound of formula (I):

OG Complex Work Unit Chemistry
wherein:

OG Complex Work Unit Chemistry
 is a substituted or unsubstituted N-containing monocyclic, bicyclic or tricyclic heteroraryl;
R1 is H, an alkyl optionally substituted with one or two groups R6 or an aryl optionally substituted with one or more groups R6;
R2 is H or alkyl; or
R1 and R2 are bound together to form a 5- or 6-membered heterocycle;
R3 and R4 are each independently H or an alkyl optionally substituted with one or two groups R6; or
R3 and R4 are bound together to form a 5- to 8-membered heterocycle;
R5 is H, a halogen, an alkyl optionally substituted with 1 or 2 groups R6, or an alkoxy optionally substituted with 1 or 2 groups R6; or
R4 and R5 are bound together to form a 5- to 7-membered heterocyle;
R6 is hydroxy, alkoxy, —NR15R16, —CO—Y—R17, —CN, —CF3, or aryl;
R15 and R16 are each independently H, alkyl, —CO-alkyl or form together with the nitrogen atom a 3- to 6-membered cyclic group;
Y is —O— or —NR18—;
R17 is H or alkyl; and
R18 is H, alkyl or hydroxyalkyl;
provided that when R3 is H and R4 and R5 are bound together to form a 5-membered heterocycle, then R1 is not H;
or a pharmaceutically acceptable salt thereof.