Title:
SUBSTITUTED KYNURENINES, A PROCESS FOR THEIR PREPARATION, AND USE AS MEDICAMENTS
Document Type and Number:
WIPO Patent Application WO/1995/004714
Kind Code:
A1
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), wherein R is halogen, C1-C6 alkyl, C5-C7 cycloalkyl, phenyl-C1-C4 alkyl, C1-C6 alkoxy, C6-C10 aryloxy, phenyl-C1-C4 alkoxy or trifluoromethyl, and R1 is hydroxy, C1-C6 alkoxy, amino, mono-C1-C6 alkylamino, di-C1-C6 alkylamino, hydroxylamino, C1-C4 alkoxyamino or benzyloxyamino, with the provisos that: (i) when R1 is hydroxy and, at the same time, R is halogen, then this halogen is not fluorine; and (ii) when R1 is hydroxy and, at the same time, R is C1-C6 alkyl, then this C1-C6 alkyl is not methyl, either as a single isomer or as a mixture of isomers, and the pharmaceutically acceptable salts thereof.
More Like This:
Inventors:
SCHWARCZ ROBERT (US)
VARASI MARIO (IT)
DELLA TORRE ARTURO (IT)
SPECIALE CARMELA (IT)
BIANCHETTI ALBERTO (IT)
VARASI MARIO (IT)
DELLA TORRE ARTURO (IT)
SPECIALE CARMELA (IT)
BIANCHETTI ALBERTO (IT)
Application Number:
PCT/US1994/007804
Publication Date:
February 16, 1995
Filing Date:
July 15, 1994
Export Citation:
Assignee:
UNIV MARYLAND (US)
PHARMACIA SPA (IT)
SCHWARCZ ROBERT (US)
VARASI MARIO (IT)
TORRE ARTURO DELLA (IT)
SPECIALE CARMELA (IT)
BIANCHETTI ALBERTO (IT)
PHARMACIA SPA (IT)
SCHWARCZ ROBERT (US)
VARASI MARIO (IT)
TORRE ARTURO DELLA (IT)
SPECIALE CARMELA (IT)
BIANCHETTI ALBERTO (IT)
International Classes:
A61K31/00; A61K31/165; A61K31/195; A61K31/198; A61K31/215; A61K31/216; C07C229/36; C07C233/43; C07C233/44; C07C235/10; (IPC1-7): C07C229/00
Foreign References:
| EP0501378A1 | 1992-09-02 |
Other References:
CHEMICAL ABSTRACT, Vol. 92(5), issued January 1979, TANZIZAWA et al., "The Mechanism of Kynureine Hydrolysis Catalyzed by Kynurenase", see Abstract No. 36767u, J. Biochem. 86(5), 1199-209, 1979.
CHEMICAL ABSTRACTS, Vol. 85(25), issued January 1976, RIVETT et al., "A Synthesis of Some Model Kynureine Peptides", see Abstract No. 193113a, Aust. J. Chem., 29(9), 2095-100.
CHEMICAL ABSTRACTS, Vol. 85(25), issued January 1976, RIVETT et al., "A Synthesis of Some Model Kynureine Peptides", see Abstract No. 193113a, Aust. J. Chem., 29(9), 2095-100.
Download PDF:
Previous Patent: 2-AMINOINDANS AS SELECTIVE DOPAMINE D3 LIGANDS
Next Patent: 2-OXIMINOMETHYL-1-PHENYL-1,3-PROPANEDIONE DERIVATIVES AS HERBICIDES
Next Patent: 2-OXIMINOMETHYL-1-PHENYL-1,3-PROPANEDIONE DERIVATIVES AS HERBICIDES