Patent ES-2875329-T3 (ES)
Title: Antagonistas de opioides kappa de tetrahidroisoquinolina
Inventor: CARROLL FRANK
IPC: A61K31/5377
Filed: 2017-09-15
Granted: 2021-11-10
Abstract: (3R)-7-Hidroxi-N-[(1S)-2-metil-1-(piperidin-1-ilmetil)propil]-1,2,3,4-tetrahidroisoquinolin-3-carboxamida, (3R)-7- Hidroxi-N-[(1S)-1-(hidroximetil)-2-metilpropil]-1,2,3,4-tetrahidroisoquinolin-3-carboxamida, (3R)-7-Hidroxi-N-[(1S)-2- metil-1-(morfolin-4-ilmetil)propil]-1,2,3,4-tetrahidroisoquinolin-3-carboxamida, (3R)-N-[(1S)-1-(Azepan-1-ilmetil)-2- metilpropil]-7-hidroxi-1,2,3,4-tetrahidroisoquinolin-3-carboxamida, (3R)-7-Hidroxi-N-{(1S)-2-metil-1-[(4-metilpiperidin- 1-il)metil]propil}-1,2,3,4-tetrahidroisoquinolin-3-carboxamida, (3R)-N-{(1S)-1-[(Dipropilamino)metil]-2-metilpropil}-7- hidroxi-1,2,3,4-tetrahidroisoquinolin-3-carboxamida, (3R)-N-{(1S)-1-[(4,4-Dimetilpiperidin-1-il)metil]-2-metilpropil}-7- hidroxi-1,2,3,4-tetrahidroisoquinolin-3-carboxamida, (3R)-N-{(1S)-1-{[Bis(2-metilpropil)amino]metil}-2-metilpropil]-7- hidroxi-1,2,3,4-tetrahidroisoquinolin-3-carboxamida, (3R)-N-{(1S)-1-[(4,4-Dietilamino)metil]-2-metilpropil]-7-hidroxi- 10 1,2,3,4-tetrahidroisoquinolin-3-carboxamida, (3R)-7-Hidroxi-N-{(1S)-2-metil-1-[(2-metilpiperidin-1-il)metil]propil}- 1,2,3,4-tetrahidroisoquinolin-3-carboxamida, (3R)-7-Hidroxi-N-{(1S)-2-metil-1-[(4-metoxipiperidin-1-il)metil]propil}- 1,2,3,4-tetrahidroisoquinolin-3-carboxamida, (3R)-7-Hidroxi-N-[(1S)-2-metil-1-{[4-(trifluorometil)piperidin-1- il]metil}propil]-1,2,3,4-tetrahidroisoquinolin-3-carboxamida, (3R)-N-{(1S)-1-[(3,5-Dimetilpiperidin-1-il)metil]-2- metilpropil}-7-hidroxi-1,2,3,4 tetrahidroisoquinolin-3-carboxamida, (3S)-7-Hidroxi-N-{(1S)-2-metil-1-[(4-metilpiperidin- 15 1-il)metil]propil}-1,2,3,4-tetrahidroisoquinolin-3-carboxamida, (3R)-7-Hidroxi-N-{(1R)-2-metil-1-[(4-metilpiperidin-1- il)metil]propil}-1,2,3,4-tetrahidroisoquinolin-3-carboxamida, (3S)-7-Hidroxi-N-{(1R)-2-metil-1-[(4-metilpiperidin-1- il)metil]propil}-1,2,3,4-tetrahidroisoquinolin-3-carboxamida, (3R)-7-Hidroxi-N-{(1S)-2-metil-1-[(4-metilpiperizin-1- il)metil]propil}-1,2,3,4-tetrahidroisoquinolin-3-carboxamida, (3R)-N3-{(1S)-2-metil-1-[(4-metilpiperidin-1-il)metil]propil}- 1,2,3,4-tetrahidroisoquinolin-3,7-dicarboxamida, (3R)-7-Hidroxi-N-{(1S)-2-metil-1-[(5-metil-3,6-dihidropiridin-1(2H)- 20 il)metil]propil}-1,2,3,4-tetrahidroisoquinolin-3-carboxamida, (3R)-N-{(1S)-1-[(4-Carbamoilpiperidin-1-il)metil]-2- metilprolil}-7-hidroxi-1,2,3,4-tetrahidroisoquinolin-3-carboxamida, (3R)-7-Hidroxi-N-{(1S)-2-metil-1-[(3-metilpiperidin-1- il)metil]propil}-1,2,3,4-tetrahidroisoquinolin-3-carboxamida, (3R)-N-{(1S)-1-[(4-Etilpiperidin-1-il)metil]-2-metilpropil}-7- hidroxi-1,2,3,4-tetrahidroisoquinolin-3-carboxamida, (3R)-7-hidroxi-N-{(1S)-2-metil-1-[(4-metil-3,6-dihidropiridin-1(2H)- il)metil]propil}-1,2,3,4-tetrahidroisoquinolin-3-carboxamida, (3R)-N-[(1S)-1-Ciclopropil-2-(4-metilpiperidin-1-il)etil]-7- 25 hidroxi-1,2,3,4-tetrahidroisoquinolin-3-carboxamida, (3R)-7-Fluoro-N-{(1S)-2-metil-1-[(4-metilpiperidin-1- il)metil]propil}-1,2,3,4-tetrahidroisoquinolin-3-carboxamida, (3R)-7-Metoxi-N-{(1S)-2-metil-1-[(4-metilpiperidin-1- il)metil]propil}-1,2,3,4-tetrahidroisoquinolin-3-carboxamida, (3R)-7-Hidroxi-N-metil-N-{(1S)-2-metil-1-[(4-metilpiperidin- 1-il)metil]propil}-1,2,3,4-tetrahidroisoquinolin-3-carboxamida, (3R)-N-{(1S)-1-[(4,5-dimetil-3,6-dihidropiridin-1(2H)- il)metil]-2-metilpropil}-7-hidroxi-1,2,3,4-tetrahidroisoquinolin-3-carboxamida, (3R)-7-Hidroxi-N-[(1S)-2-metil-1- 30 (pirrolidin-1-ilmetil)propil]-1,2,3,4-tetrahidroisoquinolin-3-carboxamida, (3R)-N-[(1S)-1-(3,6-dihidropiridin-1(2H)-ilmetil)- 2-metilpropil]-7-hidroxi-1,2,3,4-tetrahidroisoquinolin-3-carboxamida, (3R)-7-Hidroxi-N-{(1S)-2-metil-1-[(2-oxopiperidin- 1-il)metil]propil}-1,2,3,4-tetrahidroisoquinolin-3-carboxamida, (3R)-7-Hidroxi-N-(2-piperidin-1-iletil)-1,2,3,4- tetrahidroisoquinolin-3-carboxamida, (3R)-N-[(1R)-1-(Ciclohexilmetil)-2-metilpropil]-7-hidroxi-1,2,3,4- tetrahidroisoquinolin-3-carboxamida, (3R)-N3-[(1R)-1-(Ciclohexilmetil)-2-metilpropil]-1,2,3,4-tetrahidroisoquinolin-3,7- dicarboxamida, (3R)-N-{(1S)-1-[(4-Cianopiperidin-1-il)metil]-2-metilprolil}-7-hidroxi-1,2,3,4-tetrahidroisoquinolin-3- carboxamida, (3R)-N-[(1R)-1-(Ciclopentilmetil)-2-metilpropil]-7-hidroxi-1,2,3,4-tetrahidroisoquinolin-3-carboxamida, (3R)-N-[(1R)-1-(Cicloheptilmetil)-2-metilpropil]-7-hidroxi-1,2,3,4-tetrahidroisoquinolin-3-carboxamida, (3R)-N-[(1S)-1- (Ciclohexilmetil)-2-metilpropil]-7-hidroxi-1,2,3,4-tetrahidroisoquinolin-3-carboxamida, (3R)-N-[(1R)-1-(ciclohexilmetil)- 2-metilpropil]-7-metoxi-1,2,3,4-tetrahidroisoquinolin-3-carboxamida, (3R)-N-[(1R)-1-(Ciclohexilmetil)-2-metilpropil]- 40 1,2,3,4-tetrahidroisoquinolin-3-carboxamida, (3S)-N-[(1S)-1-(Ciclohexilmetil)-2-metilpropil]-7-hidroxi-1,2,3,4- tetrahidroisoquinolin-3-carboxamida, (3S)-N-[(1R)-1-(Ciclohexilmetil)-2-metilpropil]-7-hidroxi-1,2,3,4- tetrahidroisoquinolin-3-carboxamida, (3R)-N-[(1R)-1-(Ciclohexilmetil)-2-metilpropil]-7-fluoro-1,2,3,4- tetrahidroisoquinolin-3-carboxamida, (3R)-N-[(1R)-1-(Ciclohexilmetil)-2-metilpropil]-7-hidroxi-2-metil-1,2,3,4- tetrahidroisoquinolin-3-carboxamida, (3R)-N-[(1S)-1-{[(3S,4R)-3,4-Dimetilpiperidin-1-il]metil}-2-metilpropil]-7-hidroxi- 45 1,2,3,4-tetrahidroisoquinolin-3-carboxamida, (3R)-N-[(1S)-1-{[(3S,4R)-3,4-Dimetilpiperidin-1-il]metil}-2-metilpropil]-7- hidroxi-1,2,3,4-tetrahidroisoquinolin-3-carboxamida, (3R)-N-[(1S)-1-(7-Azabiciclo[2.2.1]hept-7-ilmetil)-2-metilpropil]-7- hidroxi-1,2,3,4-tetrahidroisoquinolin-3-carboxamida, (3R)-N-[(1R)-2-Ciclohexil-1-ciclopropiletil]-7-hidroxi-1,2,3,4- tetrahidroisoquinolin-3-carboxamida, (3R)-N-[(1R)-2-Ciclohexil-1-feniletil]-7-hidroxi-1,2,3,4-tetrahidroisoquinolin-3- carboxamida, (3R)-3-[(Metil{(1S)-2-metil-1-[(4-metilpiperidin-1-il)metil]propil}amino)metil]-1,2,3,4-tetrahidroisoquinolin- 0 7-ol, (3R)-N-{[(1S)-1-[4,4-Difluoropiperidin-1-il]metil]-2-metilpropil}-7-hidroxi-1,2,3,4-tetrahidroisoquinolin-3- carboxamida, (3R)-N-(2-Ciclohexiletil)-7-hidroxi-1,2,3,4-tetrahidroisoquinolin-3-carboxamida, (3R)-7-Hidroxi-N-(2- feniletil)-1,2,3,4-tetrahidroisoquinolin-3-carboxamida, (3R)-3-[({(1S)-2-Metil-1-[(4-metilpiperidin-1- il)metil]propil}amino)metil]-1,2,3,4-tetrahidroisoquinolin-7-ol, (3R)-N-[(1S)-1-{[4-(Dimetilamino)piperidin-1-il]metil}-2- metilpropil]-7-hidroxi-1,2,3,4-tetrahidroisoquinolin-3-carboxamida, (3R)-N-[(1S)-1-{[4-(Difluorometil)piperidin-1- 5 il]metil}-2-metilpropil]-7-hidroxi-1,2,3,4-tetrahidroisoquinolin-3-carboxamida, metilpropil]-7-hidroxi-3-metil-1,2,3,4-tetrahidroisoquinolin-3-carboxamida, (3R)-N-[(1R)-1-(Ciclopentilmetil)-2- (3R)-N3-[(1R)-1-(Ciclopentilmetil)-2- metilpropil]-1,2,3,4-tetrahidroisoquinolin-3,7-dicarboxamida, (3R)-N-[(1R)-1-(Ciclobutilmetil)-2-metilpropil]-7-hidroxi- 1,2,3,4-tetrahidroisoquinolin-3-carboxamida, 6-Hidroxi-N-{(1S)-2-metil-1-[(4-metilpiperidin-1-il)metil]propil}naftalen-2- carboxamida, (3R)-N-[(1R)-2-Ciclopentil-1-ciclopropiletil]-7-hidroxi-1,2,3,4-tetrahidroisoquinolin-3-carboxamida, 6- 60 Hidroxi-N-{(1S)-2-metil-1-[(4-metilpiperidin-1-il)metil]propil}-1,2,3,4-tetrahidronaftalen-2-carboxamida o (3R)-7- Hidroxi-N-{(1R)-2-metil-1-[(4-metilciclohexil)metil]propil}-1,2,3,4-tetrahidroisoquinolin-3-carboxamida o una sal de la misma.