Pharmacia & Upjohn S.p.a.

University System of Maryland

Pharmacia S.p.a.

Carmela Speciale

Mario Varasi

Antonio Giordani

Robert Schwarcz

Alberto Bianchetti

Paolo Pevarello

Luca Benatti

Arturo Della Torre

Massimo Cini

Sergio Mantegani

Manuela Villa

Monica Mosca

Etsuo Okuno

Jerome Breton

Tiziano Bandiera

Paolo Cremonesi

Simona Magagnin

Nevie Covini

Amino-benzothiazole derivatives

4-phenyl-4-oxo-butanoic acid derivatives for use in the treatment of the human or animal body by therepy; particularly as kynurenine-3-hydroxylase inhibitors, in the prevention and/or treatment of a neurodegenerative disease wherein the inhibition of such an enyzme is needed. The present invention further comprises a selected class of the above mentioned 4-phenyl-4-oxo-butanoic acid derivatives, their pharmaceutically acceptable salts, a process for their preparation and pharmaceutical compositions containing them.

4-phenyl-4-oxo-butanoic acid derivatives with kynurenine-3-hydroxylase inhibiting activity

An N-substituted-2-amino-4-phenyl-4-oxo-butanoic acid compound of the formula (I):

N-substituted-2-amino-4-phenyl-4-oxo-butanoic acid compounds having kynurenine-3-hydroxy base inhibitory activity

Recombinant KAT enzyme and process for its preparation

5-(3-Phenyl-3-oxo-propyl)-1H-tetrazole derivatives

Recombinant kynurenine-3-hydroxylase enzyme and process for its

4-phenyl-4-oxo-2-butenoic acid derivatives with kynurenine-3-hydroxylase

Fluoro-substituted benzoylpropionic acid derivatives

Disubstituted piperidine derivatives as neuroprotective agents

Disclosed are isolated DNAs encoding a kynurenine aminotransferase selected from the group consisting of: (a) an isolated DNA sequence which encodes rat KAT; (b) an isolated DNA sequence which hybridizes to the isolated DNA sequence of (a) above and which encodes a KAT enzyme; and (c) an isolated DNA sequence differing from the isolated DNA sequences of (a) and (b) above in codon sequence due to the degeneracy of the genetic code, and which encodes a KAT enzyme. Also disclosed are vectors and host cells containing the same; oligonucleotide probes for identifying kynurenine aminotransferase; and isolated and purified kynurenine aminotransferase.

Recombinant kat enzyme from rat

Substituted kynurenines and process for their preparation

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 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

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Nerviano, Italy

Carmela Speciale