Warner-lambert Company

Synthelabo

Warner Lambert LLC

Metabio Joullie

Bernard Gaudilliere

Jean Rousseau

Jonathan Reid Frost

Regis Dupont

Alexander E Wick

Henry Jacobelli

Henri Jacobelli

Jean Bertin

Charles Andrianjara

Francine Breuzard

Joseph Armand Picard

Catherine R Kostlan

Philippe Michel Manoury

Michael William Wilson

Daniel C Obitz

Salomon Z Langer

Christian J Warolin

Alain A Calvet

Catherine Burnouf

Johannes Schoemaker

Yves Pascal

Pierre Muller

Jack Jie Li

Remi Lavalette

Svein Dahl

Adrian Payne

Wen-Song Yue

Francis E Rose

Paul M Fabiani

A compound selected from those of formula (I):

Alkynylated quinazoline compounds

A compound selected from those of formula (I):wherein:

Oxo-azabicyclic compounds

A compound selected from those of formula (I):in which:

Triazolo compounds as MMP inhibitors

The present invention relates to triazolo&lsqb;4,3-a&rsqb;quinazoline-5-ones and 5-thiones of Formula I and Formula II, whereby I and II are position isomers of group R on nitrogen 3 or 4. Optionally, the invention also relates to the racemic forms, isomers and pharmaceutically acceptable salts thereof. The invention further relates to a method for the production thereof and to compositions containing said derivatives. The compounds act as inhibitors of phosphodiesterase IV (PDE-4) and, as such, have utility in treating asthma, chronic bronchitis, acutte pulmonary attack, atopic dermatitis, pulmonary hypertension, pulmonary insufficiency, cardiac insufficiency, psoriasis, inflammatory conditions of the digestive system such as haemorrhagic rectocolitis and Crohn's disease, acute respiratory distress syndrome, acute pancreatitis, benign hypertrophy of the prostate, rheumatoid arthritis, multiple sclerosis, depression, ischaemia-induced neuronal damage, partial cerebral ischaemia, and cancer such as malignant tumor and chronic lymphoid leukemia.

1-Amino triazoloc4,3-a&excl; quinazoline-5-ones and/or -5-thiones inhibiting phosphodiesterase IV

Phosphodiesterase 4-inhibiting diazepinoindolones

Ifenprodil and its analogues are useful for the treatment of psychoses such as schizophrenia.

Method of treatment of psychotic disorders

A pyrimidinedione derivative which is a compound of formula (I): ##STR1## in which: R1 denotes hydrogen, a halogen, a methyl group or a methoxy group,

6-phenyl-3-(piperazinyalalkyl)-2,4(1H,3H)-pyrimidinedione derivatives,

Compound of general formula I ##STR1## in which R is hydrogen, R.sub.1 is unsubstituted phenyl, 4-methoxy - 3,5-dimethylphenyl or phenyl substituted at one of the 2-, 3- or 4- positions by halogen, C.sub.1-4 alkyl, C.sub.1-4 alkoxy, hydroxy, benzyloxy, trifluoromethyl, cyano, nitro, amino, acetylamino, methylthio, methylsulphonyl or aminosulphonyl and R.sub.2 is unsubstituted phenyl, 2,4,6-trimethoxyphenyl or phenyl substituted at either the 3- or the 4- positions by fluorine, chlorine, methyl or methoxy, or an acid addition salt thereof.

2-(4-benzoyl-1-piperidyl)-1-phenylalkanol derivatives

Compounds of the formula: ##STR1## wherein R.sub.1 is hydrogen, halogen, trifluoromethyl, alkyl, hydroxyl, alkyoxy, benzyloxy, alkanoyloxy, or benzoyloxy, or when R.sub.2 is hydroxyl or methoxy in the 4-position and R.sub.3 is hydrogen, R.sub.1 may also represent hydroxymethyl carbamoyl or alkoxycarbonyl,

Therapeutically useful 1-phenyl-2-piperidinoalkanol derivatives

There are provided compounds of the general formula ##STR1## in which Ar represents a phenyl group which is unsubstituted or substituted by a halogen atom or a lower alkyl group, or represents a thienyl group, R.sub.1 represents a hydrogen or halogen atom or, when the Ar--CO-- grouping is in the meta-position with respect to the nitrogen atom, a lower alkyl group, R.sub.2 represents a hydrogen atom, or a lower alkyl or an acyl group, and R.sub.3 represents a hydrogen atom, a lower alkyl or a phenyl group and a physiologically acceptable salt thereof. The compounds of the general formula I and their salts have therapeutic utility, especially as analgesics.

Therapeutically useful N-phenylaniline derivatives

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Nanterre, France

Bernard Gaudilliere