Amide derivatives and their use in treating retinal neurodegenerative disorders

摘要

A medicament for treating retinal neurodegenerative disorder comprising a compound of the given formula wherein, Ar is optionally substituted phenyl or optionally substituted aromatic heterocyclic group; N is 0, 1 or 2; R1 is H, optionally substituted alkyl, optionally substituted alkenyl, alkoxycarbonyl, carbamoyl, alkanoyl or cyano; R2 and R3 are independently optionally substituted alkyl; or any two groups of R1, R2 and R3 may be taken together with the carbon atom adjacent thereto to form cycloalkane or all of R1, R2 and R3 may be taken together with the carbon atom adjacent thereto to form bicycloalkane or tricycloalkane, wherein the cycloalkane, the bicycloalkane and the tricycloalkane may be optionally substituted; R4 and R5 are independently H or optionally substituted alkyl; and R6 is H, hydroxy or alkyl. Compounds of formula (I) wherein Ar2 is a group of formula (II) or a six membered aromatic heterocyclic group substituted by 1 to 3 halogen atoms; R1, R2, R3 and R6 are as defined above; One of R7 and R8 is a fluorine atom; The other is H or a halogen atom; and R9 is a H or halogen atom provided that the compound is not one of the following compounds: N-t-butyl-4-fluorobenzamide, N-t-butyl-2-fluorobenzamide, N-(2-hydroxy-1,1-dimethylethyl)-2,4,5-trifluorobenzamide, N-(2-hydroxy-1,1-dimethylethyl)-2,5-difluorobenzamide, N-(2-hydroxy-1,1-dimethylethyl)-2-fluorobenzamide, N-(2-hydroxy-1,1-dimethylethyl)-5-chloro-2-fluorobenzamide, N-(2-hydroxy-1,1-dimethylethyl)-2-chloro-6-iodobenzamide, N-(2-hydroxy-1,1-dimethylethyl)-2,6-difluorobenzamide, N-(2-hydroxy-1,1-dimethylethyl)-2-chloro-4-fluorobenzamide, N-t-butyl-3-chloro-2-pyridincarboxamide, or N-(2-hydroxy-1,1-dimethylethyl)-6-chloro-2-pyridinecarboxamide.