PATENT CLAIM ANALYSIS

Application Number: 15554354
Application Type: Utility
Filing Date: 2018-05
Publication Date: 2018-06
Patent Classification: ["514", "211060"]

Abstract:
The present invention relates to bicyclic tetrahydrothiazepine of formula (I), wherein R 1  to R 3 , X 1 , X 2  and R 18  have the meaning as indicated in the description and claims. The invention further relates to pharmaceutical compositions comprising such compounds as well as their use as medicaments, especially in methods for the treatment or prevention of a neoplastic and/or infectious disease and in vitro methods.

Claim (Index 44):
The pharmaceutical composition of  claim 28 , wherein in formula (I) X 1 , X 2 , R 1 , R 2 , R 3 , and R 18  are selected to give:\n (3R)-3-amino-5-[(4-chlorophenyl)methyl]-N-(2,2-difluorocyclopropyl)-8-fluoro-1,1,4-trioxo-2,3,4,5-tetrahydro-1\u03bb 6 ,5-benzothiazepine-7-carboxamide; (3R)-3-amino-N-butyl-5-[(4-tert-butylphenyl)methyl]-4-oxo-2,3,4,5-tetrahydro-1,5-benzothiazepine-7-carboxamide; (3R)-3-amino-N-butyl-4-oxo-5-{[4-(trifluoromethoxy)phenyl]methyl}-2,3,4,5-tetrahydro-1,5-benzothiazepine-7-carboxamide; (3R)-3-amino-5-[(4-tert-butylphenyl)methyl]-4-oxo-N-(propan-2-yl)-2,3,4,5-tetrahydro-1,5-benzothiazepine-7-carboxamide; (3R)-3-amino-N-butyl-8-fluoro-4-oxo-5-{[4-(trifluoromethoxy)phenyl]methyl}-2,3,4,5-tetrahydro-1,5-benzothiazepine-7-carboxamide; (3R)-3-amino-N-benzyl-4-oxo-5-{[4-(trifluoromethoxy)phenyl]methyl}-2,3,4,5-tetrahydro-1,5-benzothiazepine-7-carboxamide; (3R)-3-amino-N-[(4-methoxyphenyl)methyl]-4-oxo-5-{[4-(trifluoromethoxy)-phenyl]methyl}-2,3,4,5-tetrahydro-1,5-benzothiazepine-7-carboxamide; (3R)-3-amino-N-(oxan-4-yl)-4-oxo-5-{[4-(trifluoromethoxy)phenyl]methyl}-2,3,4,5-tetrahydro-1,5-benzothiazepine-7-carboxamide; (3R)-3-amino-N-butyl-4-oxo-5-{[3-(trifluoromethoxy)phenyl]methyl}-2,3,4,5-tetrahydro-1,5-benzothiazepine-7-carboxamide; (3R)-3-amino-N-butyl-5-[(4-chlorophenyl)methyl]-4-oxo-2,3,4,5-tetrahydro-1,5-benzothiazepine-7-carboxamide; (3R)-3-amino-N-{[4-(morpholin-4-yl)phenyl]methyl}-4-oxo-5-{[4-(trifluoromethoxy)-phenyl]methyl}-2,3,4,5-tetrahydro-1,5-benzothiazepine-7-carboxamide; N-(3-{[(3R)-3-amino-4-oxo-5-{[4-(trifluoromethoxy)phenyl]methyl}-2,3,4,5-tetrahydro-1,5-benzothiazepin-7-yl]formamido}propyl)-2,2-dimethylpropanamide; (3R)-3-amino-N-butyl-5-{[4-(morpholin-4-yl)phenyl]methyl}-4-oxo-2,3,4,5-tetrahydro-1,5-benzothiazepine-7-carboxamide; (3R)-3-amino-8-fluoro-N-(oxan-4-yl)-4-oxo-5-{[4-(trifluoromethoxy)phenyl]methyl}-2,3,4,5-tetrahydro-1,5-benzothiazepine-7-carboxamide; (3R)-3-amino-8-fluoro-4-oxo-N-(propan-2-yl)-5-{[4-(trifluoromethoxy)phenyl]-methyl}-2,3,4,5-tetrahydro-1,5-benzothiazepine-7-carboxamide; (3R)-3-amino-N-benzyl-8-fluoro-4-oxo-5-{[4-(trifluoromethoxy)phenyl]methyl}-2,3,4,5-tetrahydro-1,5-benzothiazepine-7-carboxamide; (3R)-3-amino-N-methyl-4-oxo-5-{[4-(trifluoromethoxy)phenyl]methyl}-2,3,4,5-tetrahydro-1,5-benzothiazepine-7-carboxamide; (3R)-3-amino-N-ethyl-4-oxo-5-{[4-(trifluoromethoxy)phenyl]methyl}-2,3,4,5-tetrahydro-1,5-benzothiazepine-7-carboxamide; (3R)-3-amino-N-({4-[(5-acetamidopentyl)oxy]phenyl}methyl)-4-oxo-5-{[4-(trifluoromethoxy)phenyl]methyl}-2,3,4,5-tetrahydro-1,5-benzothiazepine-7-carboxamide; (3R)-3-amino-5-[(4-chlorophenyl)methyl]-N-(2-methoxyethyl)-4-oxo-2,3,4,5-tetrahydro-1,5-benzothiazepine-7-carboxamide; (3R)-3-amino-N-butyl-5-[(4-cyanophenyl)methyl]-4-oxo-2,3,4,5-tetrahydro-1,5-benzothiazepine-7-carboxamide; (3R)-3-amino-5-[(4-chlorophenyl)methyl]-4-oxo-N-(4,4,4-trifluorobutyl)-2,3,4,5-tetrahydro-1,5-benzothiazepine-7-carboxamide; (3R)-3-amino-5-[(4-chlorophenyl)methyl]-N-(oxan-4-ylmethyl)-4-oxo-2,3,4,5-tetrahydro-1,5-benzothiazepine-7-carboxamide; (3R)-3-amino-N-(5-tert-butyl-1,2-oxazol-3-yl)-5-[(4-chlorophenyl)methyl]-4-oxo-2,3,4,5-tetrahydro-1,5-benzothiazepine-7-carboxamide; (3R)-3-amino-4-oxo-N-(pyridin-3-yl)-5-{[4-(trifluoromethoxy)phenyl]methyl}-2,3,4,5-tetrahydro-1,5-benzothiazepine-7-carboxamide; (3R)-3-amino-5-[(4-chlorophenyl)methyl]-N-[(4-fluorophenyl)methyl]-4-oxo-2,3,4,5-tetrahydro-1,5-benzothiazepine-7-carboxamide; (3R)-3-amino-5-[(4-chlorophenyl)methyl]-N-[(1R)-1-(4-methoxyphenyl)ethyl]-4-oxo-2,3,4,5-tetrahydro-1,5-benzothiazepine-7-carboxamide; (3R)-3-amino-5-[(4-chlorophenyl)methyl]-N-(oxan-3-ylmethyl)-4-oxo-2,3,4,5-tetrahydro-1,5-benzothiazepine-7-carboxamide; (3R)-3-amino-4-oxo-N-(4,4,4-trifluorobutyl)-5-{[4-(trifluoromethoxy)phenyl]methyl}2,3,4,5-tetrahydro-1,5-benzothiazepine-7-carboxamide; (3R)-3-amino-N-(oxan-4-ylmethyl)-4-oxo-5-{[4-(trifluoromethoxy)phenyl]-methyl}-2,3,4,5-tetrahydro-1,5-benzothiazepine-7-carboxamide; (3R)-3-amino-N-[(4-fluorophenyl)methyl]-4-oxo-5-{[4-(trifluoromethoxy)phenyl]-methyl}-2,3,4,5-tetrahydro-1,5-benzothiazepine-7-carboxamide; (3R)-3-amino-N-[(4-fluorophenyl)methyl]-4-oxo-5-{[4-(1,2,3-thiadiazol-4-yl)phenyl]-methyl}-2,3,4,5-tetrahydro-1,5-benzothiazepine-7-carboxamide; (3R)-3-amino-5-[(4-chlorophenyl)methyl]-N-(4,4-difluorocyclohexyl)-4-oxo-2,3,4,5-tetrahydro-1,5-benzothiazepine-7-carboxamide; (3R)-3-amino-5-[(4-chlorophenyl)methyl]-N-[1-(4-fluorophenyl)ethyl]-4-oxo-2,3,4,5-tetrahydro-1,5-benzothiazepine-7-carboxamide; (3R)-3-amino-5-[(4-chlorophenyl)methyl]-N-[(1S)-1-(4-methoxyphenyl)ethyl]-4-oxo-2,3,4,5-tetrahydro-1,5-benzothiazepine-7-carboxamide; (3R)-3-amino-4-oxo-N-(4,4,4-trifluorobutyl)-5-{[6-(trifluoromethyl)pyridin-3-yl]methyl}-2,3,4,5-tetrahydro-1,5-benzothiazepine-7-carboxamide; (3R)-3-amino-N-[(4-fluorophenyl)methyl]-4-oxo-5-{[6-(trifluoromethyl)pyridin-3-yl]methyl}-2,3,4,5-tetrahydro-1,5-benzothiazepine-7-carboxamide; (3R)-3-amino-5-[(4-chlorophenyl)methyl]-N-[(1R)-1-(4-fluorophenyl)ethyl]-4-oxo-2,3,4,5-tetrahydro-1,5-benzothiazepine-7-carboxamide; (3R)-3-amino-5-[(4-chlorophenyl)methyl]-8-fluoro-N-[(4-fluorophenyl)methyl]-4-oxo-2,3,4,5-tetrahydro-1,5-benzothiazepine-7-carboxamide; (3R)-3-amino-5-[(4-chlorophenyl)methyl]-8-fluoro-4-oxo-N-(4,4,4-trifluorobutyl)-2,3,4,5-tetrahydro-1,5-benzothiazepine-7-carboxamide; (3R)-3-amino-N-butyl-5-[(4-chlorophenyl)methyl]-8-fluoro-4-oxo-2,3,4,5-tetrahydro-1,5-benzothiazepine-7-carboxamide; (3R)-3-amino-5-[(4-chlorophenyl)methyl]-8-fluoro-N-(oxan-4-yl methyl)-4-oxo-2,3,4,5-tetrahydro-1,5-benzothiazepine-7-carboxamide; (3R)-3-amino-5-[(4-chlorophenyl)methyl]-8-fluoro-N-[(4-methoxyphenyl)methyl]-4-oxo-2,3,4,5-tetrahydro-1,5-benzothiazepine-7-carboxamide; (3R)-3-amino-5-{[4-(5-methyl-1,2,4-oxadiazol-3-yl)phenyl]methyl}-N-(oxan-4-ylmethyl)-4-oxo-2,3,4,5-tetrahydro-1,5-benzothiazepine-7-carboxamide; (3R)-3-amino-5-[(4-fluorophenyl)methyl]-N-(oxan-4-ylmethyl)-4-oxo-2,3,4,5-tetrahydro-1,5-benzothiazepine-7-carboxamide; (3R)-3-amino-N-butyl-4-oxo-5-{[4-(1H-1,2,4-triazol-1-yl)phenyl]methyl}-2,3,4,5-tetrahydro-1,5-benzothiazepine-7-carboxamide; (3R)-3-amino-N-butyl-5-[(4-carbamoyl phenyl)methyl]-4-oxo-2,3,4,5-tetrahydro-1,5-benzothiazepine-7-carboxamide; (3R)-3-amino-5-[(4-chlorophenyl)methyl]-N-(2-hydroxy-2-methylpropyl)-4-oxo-2,3,4,5-tetrahydro-1,5-benzothiazepine-7-carboxamide; (3R)-3-amino-5-[(4-chlorophenyl)methyl]-N-[(1S)-1-(4-fluorophenyl)ethyl]-4-oxo-2,3,4,5-tetrahydro-1,5-benzothiazepine-7-carboxamide; (3R)-3-amino-5-[(4-chlorophenyl)methyl]-8-fluoro-N-(2-hydroxy-2-methylpropyl)-4-oxo-2,3,4,5-tetrahydro-1,5-benzothiazepine-7-carboxamide; (3R)-3-amino-5-[(4-chlorophenyl)methyl]-4-oxo-N-(4,4,4-trifluorobutyl)-2,3,4,5-tetrahydro-1,5-benzothiazepine-7-carboxamide; (3R)-3-amino-5-[(4-chlorophenyl)methyl]-8-fluoro-N\u2032-(4-fluorophenyl)-4-oxo-2,3,4,5-tetrahydro-1,5-benzothiazepine-7-carbohydrazide; (3R)-3-amino-N-butanoyl-5-[(4-chlorophenyl)methyl]-4-oxo-2,3,4,5-tetrahydro-1,5-benzothiazepine-7-carbohydrazide; (3R)-3-amino-N-butyl-5-[(4-chloro-2-fluorophenyl)methyl]-8-fluoro-4-oxo-2,3,4,5-tetrahydro-1,5-benzothiazepine-7-carboxamide; (3R)-3-amino-5-[(4-chloro-2-fluorophenyl)methyl]-8-fluoro-N-(oxan-4-ylmethyl)-4-oxo-2,3,4,5-tetrahydro-1,5-benzothiazepine-7-carboxamide; (3R)-3-amino-5-[(4-chloro-3-fluorophenyl)methyl]-8-fluoro-N-(oxan-4-ylmethyl)-4-oxo-2,3,4,5-tetrahydro-1,5-benzothiazepine-7-carboxamide; (3R)-3-amino-N-butyl-5-[(4-chloro-3-fluorophenyl)methyl]-8-fluoro-4-oxo-2,3,4,5-tetrahydro-1,5-benzothiazepine-7-carboxamide; (3R)-3-amino-5-[(4-chlorophenyl)methyl]-8-fluoro-4-oxo-N-propoxy-2,3,4,5-tetrahydro-1,5-benzothiazepine-7-carboxamide; (3R)-3-amino-5-[(4-chlorophenyl)methyl]-8-fluoro-N-(2-methyl propoxy)-4-oxo-2,3,4,5-tetrahydro-1,5-benzothiazepine-7-carboxamide; (3R)-3-amino-5-[(4-chlorophenyl)methyl]-8-fluoro-N\u2032-(2-methyl propyl)-4-oxo-2,3,4,5-tetrahydro-1,5-benzothiazepine-7-carbohydrazide; (3R)-3-amino-5-[(4-chlorophenyl)methyl]-4-oxo-N-(propan-2-yl)-2,3,4,5-tetrahydro-1,5-benzothiazepine-7-carboxamide; (3R)-3-amino-5-[(4-chlorophenyl)methyl]-N-(2-methylpropoxy)-4-oxo-2,3,4,5-tetrahydro-1,5-benzothiazepine-7-carboxamide; (3R)-3-amino-5-[(4-chlorophenyl)methyl]-N-(3-methyl butan-2-yl)-4-oxo-2,3,4,5-tetrahydro-1,5-benzothiazepine-7-carboxamide; (3R)-3-amino-N-(but-3-en-1-yl)-5-[(4-chlorophenyl)methyl]-4-oxo-2,3,4,5-tetrahydro-1,5-benzothiazepine-7-carboxamide; (3R)-3-amino-5-[(4-chlorophenyl)methyl]-N\u2032-(2-methylpropyl)-4-oxo-2,3,4,5-tetrahydro-1,5-benzothiazepine-7-carbohydrazide; (3R)-3-amino-N-butyl-5-[(4-chlorophenyl)methyl]-1,4-dioxo-2,3,4,5-tetrahydro-1\u03bb 6 ,5-benzothiazepine-7-carboxamide; (3R)-3-amino-N-butyl-1,1,4-trioxo-5-{[4-(trifluoromethoxy)phenyl]methyl}-2,3,4,5-tetrahydro-1\u03bb 6 ,5-benzothiazepine-7-carboxamide; (3R)-3-amino-5-[(4-chlorophenyl)methyl]-8-fluoro-N-[(4-fluorophenyl)methyl]-1,1,4-trioxo-2,3,4,5-tetrahydro-1\u03bb 6 ,5-benzothiazepine-7-carboxamide; (3R)-3-amino-N-butyl-5-[(4-chlorophenyl)methyl]-8-fluoro-1,1,4-trioxo-2,3,4,5-tetrahydro-1\u03bb 6 ,5-benzothiazepine-7-carboxamide; (3R)-3-amino-5-[(4-chlorophenyl)methyl]-8-fluoro-1,1,4-trioxo-N-(4,4,4-trifluoro-butyl)-2,3,4,5-tetrahydro-1\u03bb 6 ,5-benzothiazepine-7-carboxamide; (3R)-3-amino-5-[(4-chlorophenyl)methyl]-8-fluoro-N-(oxan-4-ylmethyl)-1,1,4-trioxo-2,3,4,5-tetrahydro-1\u03bb 6 ,5-benzothiazepine-7-carboxamide; (3R)-3-amino-8-fluoro-N-(oxan-4-yl methyl)-1,1,4-trioxo-5-{[4-(trifluoromethoxy)-phenyl]methyl}-2,3,4,5-tetrahydro-1\u03bb 6 ,5-benzothiazepine-7-carboxamide; (3R)-3-amino-8-fluoro-1,1,4-trioxo-N-(4,4,4-trifluorobutyl)-5-{[4-(trifluoromethoxy)-phenyl]methyl}-2,3,4,5-tetrahydro-1\u03bb 6 ,5-benzothiazepine-7-carboxamide; (3R)-3-amino-8-fluoro-1,1,4-trioxo-N-phenoxy-5-{[4-(trifluoromethoxy)phenyl]methyl}-2,3,4,5-tetrahydro-1\u03bb 6 ,5-benzothiazepine-7-carboxamide; (3R)-3-amino-5-[(4-chlorophenyl)methyl]-8-fluoro-N-(2-methylpropoxy)-1,1,4-trioxo-2,3,4,5-tetrahydro-1\u03bb 6 ,5-benzothiazepine-7-carboxamide; (3R)-3-amino-5-[(4-chlorophenyl)methyl]-8-fluoro-1,1,4-trioxo-N-phenoxy-2,3,4,5-tetrahydro-1\u03bb 6 ,5-benzothiazepine-7-carboxamide; (3R)-3-amino-5-[(4-chlorophenyl)methyl]-8-fluoro-1,1,4-trioxo-N-(propan-2-yl)-2,3,4,5-tetrahydro-1\u03bb 6 ,5-benzothiazepine-7-carboxamide; (3R)-3-amino-5-[(4-chlorophenyl)methyl]-N-({4-[(5-acetamidopentyl)oxy]phenyl}-methyl)-1,1,4-trioxo-2,3,4,5-tetrahydro-1\u03bb 6 ,5-benzothiazepine-7-carboxamide; (3R)-3-amino-5-[(4-chlorophenyl)methyl]-1,1,4-trioxo-N-(propan-2-yl)-2,3,4,5-tetrahydro-1\u03bb 6 ,5-benzothiazepine-7-carboxamide; (3R)-3-amino-5-[(4-chlorophenyl)methyl]-1,1,4-trioxo-N-(4,4,4-trifluorobutyl)-2,3,4,5-tetrahydro-1\u03bb 6 ,5-benzothiazepine-7-carboxamide; (3R)-3-amino-5-[(4-chlorophenyl)methyl]-N-(2-methylpropoxy)-1,1,4-trioxo-2,3,4,5-tetrahydro-1\u03bb 6 ,5-benzothiazepine-7-carboxamide; (3R)-3-amino-5-[(4-chlorophenyl)methyl]-1,1,4-trioxo-N-propoxy-2,3,4,5-tetrahydro-1\u03bb 6 ,5-benzothiazepine-7-carboxamide; (3R)-3-amino-5-[(4-chlorophenyl)methyl]-N-(3-methylbutan-2-yl)-1,1,4-trioxo-2,3,4,5-tetrahydro-1\u03bb 6 ,5-benzothiazepine-7-carboxamide; (3R)-3-amino-N-(but-3-en-1-yl)-5-[(4-chlorophenyl)methyl]-1,1,4-trioxo-2,3,4,5-tetrahydro-1\u03bb 6 ,5-benzothiazepine-7-carboxamide; (3R)-3-amino-5-[(4-chlorophenyl)methyl]-N-cyclopropyl-8-fluoro-1,1,4-trioxo-2,3,4,5-tetrahydro-1\u03bb 6 ,5benzothiazepine-7-carboxamide; (3R)-3-amino-5-[(4-chlorophenyl)methyl]-N-cyclobutyl-8-fluoro-1,1,4-trioxo-2,3,4,5-tetrahydro-1\u03bb 6 ,5-benzothiazepine-7-carboxamide; (3R)-3-amino-5-[(4-chloro-2-fluorophenyl)methyl]-8-fluoro-1,1,4-trioxo-N-(propan-2-yl)-2,3,4,5-tetrahydro-1\u03bb 6 ,5-benzothiazepine-7-carboxamide; (3R)-3-amino-5-[(3,4-dichlorophenyl)methyl]-1,1,4-trioxo-N-(propan-2-yl)-2,3,4,5-tetrahydro-1\u03bb 6 ,5-benzothiazepine-7-carboxamide; (3R)-3-amino-5-[(4-chloro-3-fluorophenyl)methyl]-1,1,4-trioxo-N-(propan-2-yl)-2,3,4,5-tetrahydro-1\u03bb 6 ,5-benzothiazepine-7-carboxamide; (3R)-3-amino-5-[(4-chlorophenyl)methyl]-N-(cyclohexyloxy)-1,1,4-trioxo-2,3,4,5-tetrahydro-1\u03bb 6 ,5-benzothiazepine-7-carboxamide; (3R)-3-amino-5-[(4-chlorophenyl)methyl]-N-(cyclohexylmethoxy)-1,1,4-trioxo-2,3,4,5-tetrahydro-1\u03bb 6 ,5-benzothiazepine-7-carboxamide; (3R)-3-amino-5-[(4-chlorophenyl)methyl]-8-fluoro-1,1,4-trioxo-N-(2,2,2-trifluoro-ethyl)-2,3,4,5-tetrahydro-1\u03bb 6 ,5-benzothiazepine-7-carboxamide; (3R)-3-amino-5-[(4-chlorophenyl)methyl]-8-fluoro-1,1,4-trioxo-N-(3,3,3-trifluoro-propyl)-2,3,4,5-tetrahydro-1\u03bb 6 ,5-benzothiazepine-7-carboxamide; (3R)-3-amino-5-[(4-chlorophenyl)methyl]-8-fluoro-1,1,4-trioxo-N-[(2S)-1,1,1-trifluoropropan-2-yl]-2,3,4,5-tetrahydro-1\u03bb 6 ,5-benzothiazepine-7-carboxamide; (3R)-3-amino-N-(butan-2-yl)-5-[(4-chlorophenyl)methyl]-8-fluoro-1,1,4-trioxo-2,3,4,5-tetrahydro-1\u03bb 6 ,5-benzothiazepine-7-carboxamide; (3R)-3-amino-N-tert-butyl-5-[(4-chlorophenyl)methyl]-8-fluoro-1,1,4-trioxo-2,3,4,5-tetrahydro-1\u03bb 6 ,5-benzothiazepine-7-carboxamide; (3R)-3-amino-N-(tert-butoxy)-5-[(4-chlorophenyl)methyl]-1,1,4-trioxo-2,3,4,5-tetrahydro-1\u03bb 6 ,5-benzothiazepine-7-carboxamide; (3R)-3-amino-5-[(4-chlorophenyl)methyl]-8-fluoro-1,1,4-trioxo-N-[(1S,2R)-2-phenylcyclopropyl]-2,3,4,5-tetrahydro-1\u03bb 6 ,5-benzothiazepine-7-carboxamide; (3R)-3-amino-5-[(4-chlorophenyl)methyl]-8-fluoro-N-(1-methylcyclopropyl)-1,1,4-trioxo-2,3,4,5-tetrahydro-1\u03bb 6 ,5-benzothiazepine-7-carboxamide; (3R)-3-amino-5-[(4-chlorophenyl)methyl]-8-fluoro-N-(1-methylcyclobutyl)-1,1,4-trioxo-2,3,4,5-tetrahydro-1\u03bb 6 ,5-benzothiazepine-7-carboxamide; (3R)-3-amino-5-[(4-chlorophenyl)methyl]-N-(2,2-dimethylcyclopropyl)-8-fluoro-1,1,4-trioxo-2,3,4,5-tetrahydro-1\u03bb 6 ,5-benzothiazepine-7-carboxamide; (3R)-3-amino-5-[(4-chlorophenyl)methyl]-N-(3,3-difluorocyclobutyl)-8-fluoro-1,1,4-trioxo-2,3,4,5-tetrahydro-1\u03bb 6 ,5-benzothiazepine-7-carboxamide; (3R)-3-amino-N-benzyl-5-[(4-chlorophenyl)methyl]-8-fluoro-1,1,4-trioxo-2,3,4,5-tetrahydro-1\u03bb 6 ,5-benzothiazepine-7-carboxamide; (3R)-3-amino-5-[(4-chlorophenyl)methyl]-8-fluoro-N-heptyl-1,1,4-trioxo-2,3,4,5-tetrahydro-1\u03bb 6 ,5-benzothiazepine-7-carboxamide; (3R)-3-amino-5-[(4-chlorophenyl)methyl]-N-(3,3-difluorocyclopentyl)-8-fluoro-1,1,4-trioxo-2,3,4,5-tetrahydro-1\u03bb 6 ,5-benzothiazepine-7-carboxamide; (3R)-3-amino-5-[(4-chlorophenyl)methyl]-N-[(1R)-2,2-difluorocyclopropyl]-8-fluoro-1,1,4-trioxo-2,3,4,5-tetrahydro-1\u03bb 6 ,5-benzothiazepine-7-carboxamide; (3R)-3-amino-5-[(4-chlorophenyl)methyl]-N-[(1S)-2,2-difluorocyclopropyl]-8-fluoro-1,1,4-trioxo-2,3,4,5-tetrahydro-1\u03bb 6 ,5-benzothiazepine-7-carboxamide; (2R,3R)-3-amino-5-[(4-chlorophenyl)methyl]-N-(2,2-difluorocyclopropyl)-2-methyl-1,1,4-trioxo-2,3,4,5-tetrahydro-1\u03bb 6 ,5-benzothiazepine-7-carboxamide; (3R)-3-amino-5-[(4-chlorophenyl)methyl]-8-fluoro-N-hexadecyl-1,1,4-trioxo-2,3,4,5-tetrahydro-1\u03bb 6 ,5-benzothiazepine-7-carboxamide; (3R)-3-amino-5-[(4-chlorophenyl)methyl]-N-(cyclopropylmethyl)-8-fluoro-1,1,4-trioxo-2,3,4,5-tetrahydro-1\u03bb 6 ,5-benzothiazepine-7-carboxamide; (2R,3R)-3-amino-5-[(4-chlorophenyl)methyl]-2-methyl-1,1,4-trioxo-N-(4,4,4-trifluorobutyl)-2,3,4,5-tetrahydro-1\u03bb 6 ,5-benzothiazepine-7-carboxamide; (3R)-3-amino-N-butyl-8-fluoro-4-oxo-5-(quinolin-2-ylmethyl)-2,3,4,5-tetrahydro-1,5-benzothiazepine-7-carboxamide; (3R)-3-amino-5-[(5-cyclopropyl-1,3,4-thiadiazol-2-yl)methyl]-8-fluoro-N-[(4-fluorophenyl)methyl]-4-oxo-2,3,4,5-tetrahydro-1,5-benzothiazepine-7-carboxamide; (3R)-3-amino-N-butyl-5-[(4-chlorophenyl)methyl]-8-(dimethylamino)-1,1,4-trioxo-2,3,4,5-tetrahydro-1\u03bb 6 ,5-benzothiazepine-7-carboxamide; tert-butyl N-(5-{[(3R)-5-[(4-chlorophenyl)methyl]-8-fluoro-7-{[(4-methoxyphenyl)methyl]carbamoyl}-4-oxo-2,3,4,5-tetrahydro-1,5-benzothiazepin-3-yl]amino}pentyl)carbamate; (3R)-3-amino-N-butyl-1-[(4-chlorophenyl)methyl]-2,5,5-trioxo-1H,2H,3H,4H-5\u03bb 6 -pyrido[3,4-b][1,4]thiazepine-8-carboxamide; (3R)-3-amino-N-benzyl-5-[(4-chlorophenyl)methyl]-8-(dimethylamino)-1,1,4-trioxo-2,3,4,5-tetrahydro-1\u03bb 6 , 5-benzothiazepine-7-carboxamide; (3R)-3-amino-N-(2,2-difluorocyclopropyl)-8-fluoro-5-{[4-methoxy-3-(trifluoromethyl)phenyl]methyl}-1,1,4-trioxo-2,3,4,5-tetrahydro-1\u03bb 6 ,5-benzothiazepine-7-carboxamide; (2R,3R)-3-amino-5-[(4-chlorophenyl)methyl]-8-fluoro-2-methyl-1,1,4-trioxo-N-(4,4,4-trifluorobutyl)-2,3,4,5-tetrahydro-1\u03bb 6 ,5-benzothiazepine-7-carboxamide; (3R)-3-amino-5-{[4-(5-methyl-1,2,4-oxadiazol-3-yl)phenyl]methyl}-1,1,4-trioxo-N-(4,4,4-trifluorobutyl)-2,3,4,5-tetrahydro-1\u03bb 6 ,5-benzothiazepine-7-carboxamide; (3R)-3-amino-5-[(4-chlorophenyl)methyl]-8-fluoro-N-(2-methoxyethyl)-1,1,4-trioxo-2,3,4,5-tetrahydro-1\u03bb 6 ,5-benzothiazepine-7-carboxamide; (3R)-3-amino-N-(2,2-difluorocyclopropyl)-5-{[4-(5-methyl-1,2,4-oxadiazol-3-yl)phenyl]methyl}-1,1,4-trioxo-2,3,4,5-tetrahydro-1\u03bb 6 ,5-benzothiazepine-7-carboxamide; (1S,3R)-3-amino-5-[(4-chlorophenyl)methyl]-8-fluoro-4-oxo-7-[(4,4,4-trifluorobutyl)carbamoyl]-2,3,4,5-tetrahydro-1H-1,5-benzothiazepin-1-ium-1-olate; (1R,3R)-3-amino-5-[(4-chlorophenyl)methyl]-8-fluoro-4-oxo-7-[(4,4,4-trifluorobutyl)carbamoyl]-2,3,4,5-tetrahydro-1H-1,5-benzothiazepin-1-ium-1-olate; (3R)-3-amino-5-[(4-cyanophenyl)methyl]-N-(2,2-difluorocyclopropyl)-8-fluoro-1,1,4-trioxo-2,3,4,5-tetrahydro-1\u03bb 6 ,5-benzothiazepine-7-carboxamide; (3R)-3-amino-5-[(4-cyanophenyl)methyl]-8-fluoro-1,1,4-trioxo-N-(4,4,4-trifluorobutyl)-2,3,4,5-tetrahydro-1\u03bb 6 ,5-benzothiazepine-7-carboxamide; (3R)-3-amino-5-[(4-chlorophenyl)methyl]-N-(4,4-difluorocyclohexyl-8-fluoro-1,1,4-trioxo-2,3,4,5-tetrahydro-1\u03bb 6 ,5-benzothiazepine-7-carboxamide; (3R)-3-amino-5-[(4-chlorophenyl)methyl]-8-fluoro-1,1,4-trioxo-N-[2-(trifluoromethyl)cyclopropyl]-2,3,4,5-tetrahydro-1\u03bb 6 ,5-benzothiazepine-7-carboxamide; (3R)-3-amino-5-[(4-chlorophenyl)methyl]-N-(3,3-difluorocyclobutyl)-8-fluoro-4-oxo-2,3,4,5-tetrahydro-1,5-benzothiazepine-7-carboxamide; (3R)-3-amino-8-fluoro-5-[(4-fluorophenyl)methyl]-1,1,4-trioxo-N-(4,4,4-trifluorobutyl)-2,3,4,5-tetrahydro-1\u03bb 6 ,5-benzothiazepine-7-carboxamide; (3R)-3-amino-N-(2,2-difluorocyclopropyl)-8-fluoro-5-[(4-fluorophenyl)methyl]-1,1,4-trioxo-2,3,4,5-tetrahydro-1\u03bb 6 ,5-benzothiazepine-7-carboxamide; (3R)-3-amino-N-butyl-8-fluoro-5-[(4-fluorophenyl)methyl]-4-oxo-2,3,4,5-tetrahydro-1,5-benzothiazepine-7-carboxamide; (3R)-3-amino-N-benzyl-8-fluoro-5-[(4-fluorophenyl)methyl]-4-oxo-2,3,4,5-tetrahydro-1,5-benzothiazepine-7-carboxamide; (3R)-3-amino-N-butyl-8-fluoro-5-[(4-fluorophenyl)methyl]-1,1,4-trioxo-2,3,4,5-tetrahydro-1\u03bb 6 ,5-benzothiazepine-7-carboxamide; (3R)-3-amino-N-benzyl-8-fluoro-5-[(4-fluorophenyl)methyl]-1,1,4-trioxo-2,3,4,5-tetrahydro-1\u03bb 6 ,5-benzothiazepine-7-carboxamide; (3R)-3-amino-5-[(4-chlorophenyl)methyl]-8-fluoro-N-[2-(oxan-4-yl)ethyl]-1,1,4-trioxo-2,3,4,5-tetrahydro-1\u03bb 6 ,5-benzothiazepine-7-carboxamide; (3R)-3-amino-5-benzyl-8-fluoro-1,1,4-trioxo-N-(4,4,4-trifluorobutyl)-2,3,4,5-tetrahydro-1\u03bb 6 ,5-benzothiazepine-7-carboxamide; (3R)-3-amino-5-[(4-chlorophenyl)methyl]-8-fluoro-N-[(4-methoxyphenyl)methyl]-1,1,4-trioxo-2,3,4,5-tetrahydro-1\u03bb 6 ,5-benzothiazepine-7-carboxamide; (3R)-3-amino-5-[(5-cyclopropyl-1,3,4-thiadiazol-2-yl)methyl]-8-fluoro-N-[(4-fluorophenyl)methyl]-1,1,4-trioxo-2,3,4,5-tetrahydro-1\u03bb 6 ,5-benzothiazepine-7-carboxamide; (3R)-3-amino-8-fluoro-5-[(4-fluorophenyl)methyl]-N-[(oxan-4-yl)methyl]-1,1,4-trioxo-2,3,4,5-tetrahydro-1\u03bb 6 ,5-benzothiazepine-7-carboxamide; (3R)-3-amino-N-(3,3-difluorocyclobutyl-8-fluoro-5-[(4-fluorophenyl)methyl]-1,1,4-trioxo-2,3,4,5-tetrahydro-1\u03bb 6 ,5-benzothiazepine-7-carboxamide; (3R)-3-amino-8-fluoro-5-[(4-methoxyphenyl)methyl]-1,1,4-trioxo-N-(4,4,4-trifluorobutyl)-2,3,4,5-tetrahydro-1\u03bb 6 ,5-benzothiazepine-7-carboxamide; (3R)-3-amino-8-fluoro-5-[(4-methoxyphenyl)methyl]-N-[(oxan-4-yl)methyl]-1,1,4-trioxo-2,3,4,5-tetrahydro-1\u03bb 6 ,5-benzothiazepine-7-carboxamide; (3R)-3-amino-N-(2,2-difluorocyclopropyl)-8-fluoro-5-[(4-methoxyphenyl)methyl]-1,1,4-trioxo-2,3,4,5-tetrahydro-1\u03bb 6 ,5-benzothiazepine-7-carboxamide; (3R)-3-amino-5-[(4-chlorophenyl)methyl]-8-fluoro-N-(oxan-4-yl)-1,1,4-trioxo-2,3,4,5-tetrahydro-1\u03bb 6 ,5-benzothiazepine-7-carboxamide; (3R)-3-amino-5-[(4-chlorophenyl)methyl]-N-(3,3-difluorocyclobutyl)-1,1,4-trioxo-2,3,4,5-tetrahydro-1\u03bb 6 ,5-benzothiazepine-7-carboxamide; (3R)-3-amino-5-[(4-chlorophenyl)methyl]-N-[(1S)-3,3-difluorocyclopentyl]-8-fluoro-1,1,4-trioxo-2,3,4,5-tetrahydro-1\u03bb 6 ,5-benzothiazepine-7-carboxamide; (3R)-3-amino-5-[(4-chlorophenyl)methyl]-N-[(1R,2S)-2-fluorocyclopropyl]-1,1,4-trioxo-2,3,4,5-tetrahydro-1\u03bb 6 ,5-benzothiazepine-7-carboxamide; (3R)-3-amino-N-(3,3-difluorocyclobutyl)-5-[(2-fluorophenyl)methyl]-1,1,4-trioxo-2,3,4,5-tetrahydro-1\u03bb 6 ,5-benzothiazepine-7-carboxamide; (3R)-3-amino-N-(3,3-difluorocyclobutyl)-5-[(3-methoxyphenyl)methyl]-1,1,4-trioxo-2,3,4,5-tetrahydro-1\u03bb 6 ,5-benzothiazepine-7-carboxamide; (3R)-3-amino-5-[(4-methoxyphenyl)methyl]-1,1,4-trioxo-N-(4,4,4-trifluorobutyl)-2,3,4,5-tetrahydro-1\u03bb 6 ,5-benzothiazepine-7-carboxamide; (3R)-3-amino-N,5-bis[(4-methoxyphenyl)methyl]-1,1,4-trioxo-2,3,4,5-tetrahydro-1\u03bb 6 ,5-benzothiazepine-7-carboxamide; (3R)-3-amino-5-benzyl-N-[(4-methoxyphenyl)methyl]-1,1,4-trioxo-2,3,4,5-tetrahydro-1\u03bb 6 ,5-benzothiazepine-7-carboxamide; (3R)-3-amino-5-[(4-chlorophenyl)methyl]-N-[(4-methoxyphenyl)methyl]-1,1,4-trioxo-2,3,4,5-tetrahydro-1\u03bb 6 ,5-benzothiazepine-7-carboxamide; (3R)-3-amino-N-(4,4-difluorocyclohexyl)-5-[(4-methoxyphenyl)methyl]-1,1,4-trioxo-2,3,4,5-tetrahydro-1\u03bb 6 , 5-benzothiazepine-7-carboxamide; (3R)-3-amino-5-[(4-chlorophenyl)methyl]-1,1,4-trioxo-N-(3,3,3-trifluoropropyl)-2,3,4,5-tetrahydro-1\u03bb 6 ,5-benzothiazepine-7-carboxamide; (3R)-3-amino-5-[(4-chlorophenyl)methyl]-1,1,4-trioxo-N-[(3R)-oxolan-3-yl]-2,3,4,5-tetrahydro-1\u03bb 6 ,5-benzothiazepine-7-carboxamide; (3R)-3-amino-5-[(4-chlorophenyl)methyl]-1,1,4-trioxo-N-[(oxolan-3-yl)methyl]-2,3,4,5-tetrahydro-1\u03bb 6 ,5-benzothiazepine-7-carboxamide; (3R)-3-amino-5-[(4-chlorophenyl)methyl]-N-[(1R)-2,2-difluorocyclopropyl]-1,1,4-trioxo-2,3,4,5-tetrahydro-1\u03bb 6 ,5-benzothiazepine-7-carboxamide; (3R)-3-amino-5-[(4-cyclopropylphenyl)methyl]-N-[(1R)-2,2-difluorocyclopropyl]-1,1,4-trioxo-2,3,4,5-tetrahydro-1\u03bb 6 ,5-benzothiazepine-7-carboxamide; (3R)-3-amino-N-[(1R)-2,2-difluorocyclopropyl]-5-{[4-(difluoromethoxy)phenyl]methyl}-1,1,4-trioxo-2,3,4,5-tetrahydro-1\u03bb 6 ,5-benzothiazepine-7-carboxamide; (3R)-3-amino-N-[(1R)-2,2-difluorocyclopropyl]-5-[(4-methoxyphenyl)methyl]-1,1,4-trioxo-2,3,4,5-tetrahydro-1\u03bb 6 ,5-benzothiazepine-7-carboxamide; (3R)-3-amino-5-benzyl-1,1,4-trioxo-N-(4,4,4-trifluorobutyl)-2,3,4,5-tetrahydro-1\u03bb 6 ,5-benzothiazepine-7-carboxamide; (3R)-3-amino-8-chloro-5-[(4-chlorophenyl)methyl]-1,1,4-trioxo-N-(4,4,4-trifluorobutyl)-2,3,4,5-tetrahydro-1\u03bb 6 ,5-benzothiazepine-7-carboxamide; (3R)-3-amino-5-{[4-(difluoromethoxy)phenyl]methyl}-N-[(oxan-4-yl)methyl]-1,1,4-trioxo-2,3,4,5-tetrahydro-1\u03bb 6 ,5-benzothiazepine-7-carboxamide; (3R)-3-amino-5-[(4-chlorophenyl)methyl]-N-[(4-fluorooxan-4-yl)methyl]-1,1,4-trioxo-2,3,4,5-tetrahydro-1\u03bb 6 ,5-benzothiazepine-7-carboxamide; (3R)-3-amino-5-[(4-chlorophenyl)methyl]-N-[(1R)-1-(oxan-4-yl)ethyl]-1,1,4-trioxo-2,3,4,5-tetrahydro-1\u03bb 6 ,5-benzothiazepine-7-carboxamide; (3R)-3-amino-5-benzyl-N-[(1R)-2,2-difluorocyclopropyl]-1,1,4-trioxo-2,3,4,5-tetrahydro-1\u03bb 6 ,5-benzothiazepine-7-carboxamide; (3R)-3-amino-5-[(4-chlorophenyl)methyl]-N-[(6-methylpyridin-3-yl)methyl]-1,1,4-trioxo-2,3,4,5-tetrahydro-1\u03bb 6 ,5-benzothiazepine-7-carboxamide; (3R)-3-amino-5-[(4-chlorophenyl)methyl]-N-[(1R)-3,3-difluorocyclopentyl]-1,1,4-trioxo-2,3,4,5-tetrahydro-1\u03bb 6 ,5-benzothiazepine-7-carboxamide; (3R)-3-amino-5-[(4-cyanophenyl)methyl]-8-fluoro-N-[(4-fluorophenyl)methyl]-1,1,4-trioxo-2,3,4,5-tetrahydro-1\u03bb 6 ,5-benzothiazepine-7-carboxamide; (3R)-3-amino-5-[(4-chlorophenyl)methyl]-N-[(3,3-difluorocyclobutyl)methyl]-1,1,4-trioxo-2,3,4,5-tetrahydro-1\u03bb 6 ,5-benzothiazepine-7-carboxamide; (3R)-3-amino-5-[(4-chlorophenyl)methyl]-8-fluoro-N-[2-(2-methoxyethoxy)ethyl]-1,1,4-trioxo-2,3,4,5-tetrahydro-1\u03bb 6 ,5-benzothiazepine-7-carboxamide; (3R)-3-amino-N-(but-3-yn-1-yl)-5-[(4-chlorophenyl)methyl]-8-fluoro-1,1,4-trioxo-2,3,4,5-tetrahydro-1\u03bb 6 ,5-benzothiazepine-7-carboxamide; (3R)-3-amino-5-[(4-chlorophenyl)methyl]-8-fluoro-1,1,4-trioxo-N-(pent-4-yn-1-yl)-2,3,4,5-tetrahydro-1\u03bb 6 , 5-benzothiazepine-7-carboxamide; (3R)-3-amino-8-chloro-5-[(4-chlorophenyl)methyl]-N-[(1R)-2,2-difluorocyclopropyl]-1,1,4-trioxo-2,3,4,5-tetrahydro-1\u03bb 6 ,5-benzothiazepine-7-carboxamide; (3R)-3-amino-5-[(4-chlorophenyl)methyl]-N-[2-(morpholin-4-yl)ethyl]-1,1,4-trioxo-2,3,4,5-tetrahydro-1\u03bb 6 ,5-benzothiazepine-7-carboxamide; (3R)-3-amino-5-[(4-chlorophenyl)methyl]-N-[(6-methoxypyridin-3-yl)methyl]-1,1,4-trioxo-2,3,4,5-tetrahydro-1\u03bb 6 ,5-benzothiazepine-7-carboxamide; (3R)-3-amino-5-[(4-chlorophenyl)methyl]-8-fluoro-1,1,4-trioxo-N-{[4-(prop-2-yn-1-yloxy)phenyl]methyl}-2,3,4,5-tetrahydro-1\u03bb 6 ,5-benzothiazepine-7-carboxamide; (3R)-3-amino-N-[(1R)-2,2-difluorocyclopropyl]-1,1,4-trioxo-5-{[4-(trifluoromethyl)phenyl]methyl}-2,3,4,5-tetrahydro-1\u03bb 6 ,5-benzothiazepine-7-carboxamide; (3R)-3-amino-5-[(4-bromophenyl)methyl]-N-(2,2-difluorocyclopropyl)-1,1,4-trioxo-2,3,4,5-tetrahydro-1\u03bb 6 ,5-benzothiazepine-7-carboxamide; (3R)-3-amino-5-[(4-chlorophenyl)methyl]-N-{2-oxaspiro[3.3]heptan-6-yl}-, 1,4-trioxo-2,3,4,5-tetrahydro-1\u03bb 6 ,5-benzothiazepine-7-carboxamide; or (3R)-5-[(4-chlorophenyl)methyl]-3-(ethylamino)-8-fluoro-1,1,4-trioxo-N-(4,4,4-trifluorobutyl)-2,3,4,5-tetrahydro-1\u03bb 6 ,5-benzothiazepine-7-carboxamide.

Metadata:
- Claim Count in Document: 11.0
- Percentile: 93.0
- Lexical Diversity: 1.46154
- Patent Class: 514.0
- Transitional Phrase Type: none
- Component Type: 0
- Foreign Priority: True
- Related Applications: ['12295545', '12096393', '13128726', '12096432', '12096439']

Analysis Scores:
- 35 USC 101 Eligibility (BERT): 0.7830188743739628
- 35 USC 102 Novelty (BERT): 0.5416781983966235
- Combined Prediction Score: 0.7588848067762288
- Mean Citation Score: 343.96614400000016
- Max Citation Score: 368.7808
- Similarity Product: 284.28967177505496

Labels:
- Claim Label 101: 1
- Claim Label 102: 1
- Claim Label 103: 1
- Claim Label 112: 1
- Combined Label: 1
- Label 101 Adjusted: 1

Dataset: test