Sanofi

Pharmacia & Upjohn S.p.a.

University System of Maryland

Elf Sanofi

Pierrel Spa

Pharmacia S.p.a.

Alberto Bianchetti

Tiziano Croci

Mario Varasi

Dino Nisato

Carmela Speciale

Paolo Carminati

Luciano Manara

Robert Schwarcz

Arturo Della Torre

Emilio Crisafulli

Antonio Giordani

Philippe Soubrie

Jacques Simiand

Massimo Cini

Robert Boigegrain

Roberto Cecchi

Gerard R Le Fur

Sergio Boveri

Luciano Toscano

Mario Riva

Romeo Roncucci

Antonina Giudice

Elena Poggesi

Peter-Eugene Keane

G Erard Le Fur

Giampiero Grisanti

Silvia Tricerri Zumin

Roberto Sacilotto

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

Fluoro-substituted benzoylpropionic acid derivatives

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 concerns the use of 4-amino-1-(2-pyridyl)piperidines of general formula (I') ##STR1## wherein R' represents hydrogen, a halogen atom, a methyl, methylthio, trifluoromethyl, trifluoromethylthio, (C.sub.1 -C.sub.3)alkoxy, trifluoromethoxy, 2,2,2-trifluoroethoxy, or phenoxy group optionally substituted with a halogen atom, a trifluoromethyl, (C.sub.1 -C.sub.3)alkyl, (C.sub.1 -C.sub.3)alkoxy, (C.sub.1 -C.sub.3)alkylthio, or cyano group, or of a pharmaceutically acceptable salt thereof, for the preparation of a medicament for the treatment or prophylaxis of those conditions deriving from disorders of the serotoninergic systems wherein a serotoninergic action selectively mediated by the 5-HT.sub.3 receptors is required, e.g. affective disorders, anxiety, psychotic troubles, constipation.

Use of 4-amino-1-(2-pyridyl)piperidines for the preparation of a

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

The invention concerns a method of treatment and prophylaxis of depression and stress by means of a phenylethanolaminotetralin of formula (I) ##STR1## wherein A is a (C.sub.1 -C.sub.4)alkylene radical and R represents a hydrogen atom or a (C.sub.1 -C.sub.4)alkyl group, or a pharmaceutically acceptable salts thereof.

Method of treatment or prophylaxis of depression and stress

A method of prophylaxis and/or treatment of intestinal motility disorders, in particular of constipation, in mammals which comprises administering to a mammal in need of such a treatment a prophylactically and/or therapeutically effective amount of a compound of formula (I) ##STR1## wherein Alk represents a straight or branched (C.sub.1 -C.sub.4)alkylene radical, and

Trifluoromethylphenyltetrahydropyridines for the treatment and/or

A method of treatment of anxiety and depression in mammals is described which comprises administering to a mammal in need thereof an effective amount of a trifluoromethylphenyl-tetrahydropyridine derivative of formula I ##STR1## wherein Alk represents a straight or branched (C.sub.1 -C.sub.4)alkylene chain and R is selected from the group consisting of cyano, acetyl, (C.sub.3 -C.sub.7)cycloalkyl, pyridyl, 1-oxide-pyridyl and naphthyl, or of a pharmaceutically acceptable salt thereof.

Method of treatment of anxiety and anxio-depressive disorders

Phenylethanolamine analog active compounds, optionally substituted on the phenyl group with an halogen atom or with an alkyl or trifluoromethyl group and substituted on the amino group with a phenylalkyl or phenoxy alkyl group optionally substituted on the benzene ring, are used for the treatment and/or prophylaxis of gastrointestinal diseases associated with a smooth muscle contraction.

Phenylethanolamine analog active compounds for the treatment of

Methyllevallorphanium salts having peripheral antagonistic activity of formula ##STR1## wherein Y.sup.n(-) represents the anion a pharmaceutically acceptable acid other than halogen and n represents the number of negative charges of said anion; a process for their preparation by exchange of the halogen ion with the Y.sup.n(-) anion; and pharmaceutical compositions containing them as active ingredients.

Methyllevallorphanium salts having peripheral opiate antagonistic

A novel phenylethanolaminotetraline having lipolytic activity of formula ##STR1## wherin X represents hydrogen, halogen, a trifluoromethyl or a lower alkyl group and R represents hydrogen, a lower alkyl group not substituted or substituted by a cycloalkyl group containing 3 to 7 carbon atoms, a hydroxy group, a lower alkoxy, carboxy or lower carbalkoxy group; a cycloalkyl group containing 3 to 7 carbon atoms; or a lower alcanoyl group; or a pharmaceutically acceptable salt thereof; a process for its preparation; and pharmaceutical compositions containing it as active ingredient, useful for the treatment of obesity.

Phenylethanolaminotetralines, a process for their preparation and

The invention relates to 4-(3-trifluoromethylphenyl)-1,2,3,6-tetrahydropyridines of formula ##STR1## in which R represents a cyano, acetyl or cycloalkyl group of from 3 to 7 carbon atoms and Alk represents a straight or branched alkylene of from 1 to 4 carbon atoms, as well as to the salts thereof, having an anorectic acitivity, to a process for preparing same and to pharmaceutical compositions containing said compounds, useful in the treatment of obesity.

Anorectic agent;

The invention relates to 4-(-3-trifluoromethylphenyl)-1,2,3,6-tetrahydropyridines of formula ##STR1## in which R represents a cyano, acetyl or cycloalkyl group of from 3 to 7 carbon atoms and Alk represents a straight or branched alkylene of from 1 to 4 carbon atoms, as well as to the salts thereof, having an anorectic activity, to a process for preparing same and to pharmaceutical compositions containing said compounds, useful in the treatment of obesity.

Growing community of inventors

Milan, Italy

Alberto Bianchetti