(1 h-indol-5-yl)acrylamide derivatives as inhibitors of TEAD proteins and the hippo-YAP1/TAZ signaling cascade for the treatment of cancer

A compound of formula (I):

• wherein
• n is 0;
• R1 is a single bond;
• R2 is selected from the group consisting of:
• a phenyl group unsubstituted or substituted with one or more R3 groups;
• a (C4-C8) cycloalkyl group unsubstituted or substituted with one or more R5 groups;
• and
• a (C4-C8) heterocyclyl group unsubstituted or substituted with one or more R6 groups;
• R3 is selected from the group consisting of:
• an (C1-C4) alkyl group unsubstituted or substituted with one or more fluorine atoms;
• a cyclopropyl group;
• a halogen atom;
• an (C1-C3) alkoxy group unsubstituted or substituted with one or more fluorine atoms;
• a pentafluorosulfanyl group;
• a nitrile group;
• a (C1-C3) trialkylsilyl group;
• an (C1-C3) alkylsulfonyl group;
• and
• a phenyl group unsubstituted or substituted with a trifluoromethyl group;
• R4 is a hydrogen atom or an (C1-C4) alkyl group;
• R5 is a fluorine atom or a trifluoromethyl group;
• R6 is selected from the group consisting of:
• a phenyl group unsubstituted or substituted with one or more fluorine atoms or one or more CF3 groups;
• an (C1-C4) alkyl group substituted with one or more fluorine atoms;
• and
• a fluorine atom;
• R7 is selected from the group consisting of:
• a hydrogen atom;
• a nitrile group;
• an (C1-C4) alkyl group unsubstituted or substituted with an (C1-C3) alkoxy group or a hydroxy group;
• a COO(C1-C4) alkyl group;
• and
• a CONH2 group;
• R8 is a hydrogen atom or an (C1-C4) alkyl group unsubstituted or substituted with a di(C1-C4) alkylamino group;
• and
• R11 is selected from the group consisting of a hydrogen atom, a fluorine atom, and a chlorine atom;
• or a pharmaceutically acceptable salt thereof.

A compound selected from:

• N-[1-[3-(trifluoromethyl)phenyl]methyl]indol-5-yl]acrylamide;
• N-methyl-N-(1-(3-(trifluoromethyl)benzyl)-1H-indol-5-yl)acrylamide;
• N-(1-(5,5,5-trifluoropentyl)-1H-indol-5-yl)acrylamide;
• N-(1-(1-(3-(trifluoromethyl)phenyl)ethyl)-1H-indol-5-yl)acrylamide;
• N-(1-(3-(pentafluoro-16-sulfanyl)benzyl)-1H-indol-5-yl)acrylamide;
• N-(1-(4-(pentafluoro-16-sulfanyl)benzyl)-1H-indol-5-yl)acrylamide;
• N-(1-(4-(trifluoromethoxy)benzyl)-1H-indol-5-yl)acrylamide;
• N-(1-(3-(trifluoromethoxy)benzyl)-1H-indol-5-yl)acrylamide;
• N-(1-(3-iodobenzyl)-1H-indol-5-yl)acrylamide;
• N-(1-(2-fluoro-5-(trifluoromethyl)benzyl)-1H-indol-5-yl)acrylamide;
• N-(3-methyl-1-(3-(trifluoromethyl)benzyl)-1H-indol-5-yl)acrylamide;
• N-(1-(3-methoxybenzyl)-1H-indol-5-yl)acrylamide;
• N-(2-methyl-1-(3-(trifluoromethyl)benzyl)-1H-indol-5-yl)acrylamide;
• N-(3-cyano-1-(3-(trifluoromethyl)benzyl)-1H-indol-5-yl)acrylamide;
• N-(1-(3-cyclopropylbenzyl)-1H-indol-5-yl)acrylamide;
• N-(2,3-dimethyl-1-(3-(trifluoromethyl)benzyl)-1H-indol-5-yl)acrylamide;
• N-(1-(3-methylbenzyl)-1H-indol-5-yl)acrylamide;
• N-(1-Benzyl-1H-indol-5-yl)-acrylamide;
• N-(1-(3-(trifluoromethyl)benzyl)-1H-indol-4-yl)acrylamide;
• (E)-4-(dimethylamino)-N-(1-(3-(trifluoromethyl)benzyl)-1H-indol-4-yl) but-2-enamide;
• N-(1-(3-(trifluoromethyl)benzyl)-1H-indol-6-yl)acrylamide;
• N-(1-((4,4-difluorocyclohexyl)methyl)-1H-indol-5-yl)acrylamide;
• N-(1-((tetrahydro-2H-pyran-4-yl)methyl)-1H-indol-5-yl)acrylamide;
• N-(1-((4-(trifluoromethyl)cyclohexyl)methyl)-1H-indol-5-yl)acrylamide;
• N-(1-((1,1-difluorospiro[2.3]hexan-5-yl)methyl)-1H-indol-5-yl)acrylamide;
• N-(1-((3-fluorocyclopentyl)methyl)-1H-indol-5-yl)acrylamide;
• N-(1-(cyclohexylmethyl)-1H-indol-5-yl)acrylamide;
• N-(1-((3-(trifluoromethyl)cyclobutyl)methyl)-1H-indol-5-yl)acrylamide;
• N-(1-((3,3-difluorocyclopentyl)methyl)-1H-indol-5-yl)acrylamide;
• N-(1-([1,1′-biphenyl]-4-ylmethyl)-1H-indol-5-yl)acrylamide;
• N-(1-((3′-(trifluoromethyl)-[1,1′-biphenyl]-4-yl)methyl)-1H-indol-5-yl)acrylamide;
• N-(1-((4′-(trifluoromethyl)-[1,1′-biphenyl]-4-yl)methyl)-1H-indol-5-yl)acrylamide;
• N-(1-((trans)-4-(trifluoromethyl)cyclohexyl)-1H-indol-5-yl)acrylamide;
• N-(1-((cis)-4-(trifluoromethyl)cyclohexyl)-1H-indol-5-yl)acrylamide;
• N-(1-((1-(4-(trifluoromethyl)phenyl)piperidin-4-yl)methyl)-1H-indol-5-yl)acrylamide;
• N-(1-(2-(methyl (2,2,2-trifluoroethyl)amino)ethyl)-1H-indol-5-yl)acrylamide;
• N-(1-(2-(2,2,2-trifluoroethoxy)ethyl)-1H-indol-5-yl)acrylamide;
• N-(1-(1-(2,2,2-trifluoroethyl)piperidin-4-yl)-1H-indol-5-yl)acrylamide;
• N-(1-(4,4-difluorocyclohexyl)-1H-indol-5-yl)acrylamide;
• N-(1-(1-(4-(trifluoromethyl)phenyl)piperidin-4-yl)-1H-indol-5-yl)acrylamide;
• N-(1-(3-(3,3-difluoropyrrolidin-1-yl)propyl)-1H-indol-5-yl)acrylamide;
• N-(1-(4-(trimethylsilyl)benzyl)-1H-indol-5-yl)acrylamide;
• N-(1-(3-(trifluoromethyl)phenyl)-1H-indol-5-yl)acrylamide;
• N-(1-(4-(trifluoromethyl)phenyl)-1H-indol-5-yl)acrylamide;
• N-(1-(6-(trifluoromethyl)pyridin-3-yl)-1H-indol-5-yl)acrylamide;
• N-(1-(5-(trifluoromethyl)pyridin-2-yl)-1H-indol-5-yl)acrylamide;
• N-(1-(pyridin-3-yl)-1H-indol-5-yl)acrylamide;
• N-(1-(4-fluorophenyl)-1H-indol-5-yl)acrylamide;
• N-(1-(3,4-difluorophenyl)-1H-indol-5-yl)acrylamide;
• N-(1-(3-(methylsulfonyl)phenyl)-1H-indol-5-yl)acrylamide;
• N-(1-(4-cyanophenyl)-1H-indol-5-yl)acrylamide;
• N-(1-(3,5-difluorobenzyl)-1H-indol-5-yl)acrylamide;
• N-(1-(3,4-difluorobenzyl)-1H-indol-5-yl)acrylamide;
• N-(1-(3-cyanobenzyl)-1H-indol-5-yl)acrylamide;
• N-(1-((5-(trifluoromethyl)furan-2-yl)methyl)-1H-indol-5-yl)acrylamide;
• N-(1-(thiazol-4-ylmethyl)-1H-indol-5-yl)acrylamide;
• N-(1-((2-(trifluoromethyl) thiazol-4-yl)methyl)-1H-indol-5-yl)acrylamide;
• N-(1-(3-(trifluoromethyl)benzyl)-1H-indol-7-yl)acrylamide;
• N-(1-(3-(methylsulfonyl)benzyl)-1H-indol-5-yl)acrylamide;
• N-(3-(methoxymethyl)-1-(3-(trifluoromethyl)benzyl)-1H-indol-5-yl)acrylamide;
• methyl 5-acrylamido-1-(3-(trifluoromethyl)benzyl)-1H-indole-3-carboxylate;
• N-(1-(3-(trifluoromethyl)phenyl)-1H-indol-6-yl)acrylamide;
• N-(1-(4-(pentafluoro-16-sulfanyl)phenyl)-1H-indol-5-yl)acrylamide;
• N-(1-(4-(trifluoromethyl)phenyl)-1H-indol-6-yl)acrylamide;
• N-(1-(2-methyl-4-(trifluoromethyl)phenyl)-1H-indol-5-yl)acrylamide;
• N-(1-(3,5-difluorophenyl)-1H-indol-5-yl)acrylamide;
• N-(1-(5-fluoropyridin-3-yl)-1H-indol-5-yl)acrylamide;
• N-(1-(2-(trifluoromethyl)pyridin-4-yl)-1H-indol-5-yl)acrylamide;
• N-[3-methyl-1-[4-(trifluoromethyl)phenyl]indol-5-yl]acrylamide;
• N-[2-methyl-1-[4-(trifluoromethyl)phenyl]indol-5-yl]acrylamide;
• N-methyl-N-[2-methyl-1-[4-(trifluoromethyl)phenyl]indol-5-yl]acrylamide;
• N-(3-(methoxymethyl)-1-(4-(trifluoromethyl)phenyl)-1H-indol-5-yl)acrylamide;
• N-(6-fluoro-1-(4-(trifluoromethyl)phenyl)-1H-indol-5-yl)acrylamide;
• N-methyl-N-(1-(4-(trifluoromethyl)phenyl)-1H-indol-5-yl)acrylamide;
• (E)-N-(1-(4-(trifluoromethyl)phenyl)-1H-indol-5-yl) but-2-enamide;
• (E)-4-(dimethylamino)-N-(1-(4-(trifluoromethyl)phenyl)-1H-indol-5-yl) but-2-enamide;
• N-(6-chloro-1-(4-(trifluoromethyl)phenyl)-1H-indol-5-yl)acrylamide;
• N-(6-chloro-1-(3-(trifluoromethyl)benzyl)-1H-indol-5-yl)acrylamide;
• N-(7-chloro-1-(3-(trifluoromethyl)benzyl)-1H-indol-5-yl)acrylamide;
• N-(6-fluoro-1-(3-(trifluoromethyl)benzyl)-1H-indol-5-yl)acrylamide;
• N-(7-chloro-1-(4-(trifluoromethyl)phenyl)-1H-indol-5-yl)acrylamide;
• N-(3-(hydroxymethyl)-1-(4-(trifluoromethyl)phenyl)-1H-indol-5-yl)acrylamide;
• 5-acrylamido-1-(3-(trifluoromethyl)benzyl)-1H-indole-3-carboxamide;
• and
• 5-acrylamido-1-(4-(trifluoromethyl)phenyl)-1H-indole-3-carboxamide;
• and a pharmaceutically acceptable salt thereof.