Patent · US Expired

Substituted kynurenines and process for their preparation

US5786508A · kind A · utility

1Cited by
1References
4Claims
0Family size

Assignees

Inventors

Key dates

Filing dateApr 6, 1995
Grant dateJul 28, 1998
Priority date
Expiry dateApr 6, 2015

Classification

  • Technology area (CPC C)Chemistry; Metallurgy
  • CPC primaryC07C2601/14
  • WIPO fieldOrganic fine chemistry
  • WIPO sectorChemistry

Abstract

The present invention relates to the use in the treatment of cognitive disorders associated with the aging processes of the brain and perinatal brain disorders of compounds which act as inhibitors of the enzyme kynurenine aminotransferase (KAT). The present invention also provides, as novel compounds, a selected class of KAT inhibitors which are the compounds of formula (IA) ##STR1## wherein R is halogen, C.sub.1 -C.sub.6 alkyl, C.sub.5 -C.sub.7 cycloalkyl, phenyl-C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.6 alkoxy, C.sub.6 -C.sub.10 aryloxy, phenyl-C.sub.1 -C.sub.4 alkoxy or trifluoromethyl, and PA1 R.sub.1 is hydroxy, C.sub.1 -C.sub.6 alkoxy, amino, mono-C.sub.1 -C.sub.6 alkylamino, di-C.sub.1 -C.sub.6 alkylamino, hydroxylamino, C.sub.1 -C.sub.4 alkoxyamino or benzyloxyamino, PA1 with the provisos that: PA2 (i) when R.sub.1 is hydroxy and, at the same time, R is halogen, then this halogen is not fluorine; and PA2 (ii) when R.sub.1 is hydroxy and, at the same time, R is C.sub.1 -C.sub.6 alkyl, then this C.sub.1 -C.sub.6 alkyl is not methyl, PA1 either as a single isomer or as a mixture of isomers, and the pharmaceutically acceptable salts thereof.

Source: USPTO / EPO open patent data. Objective bibliographic and citation counts.