Synthelabo

Sanofi-Aventis

Mitsubishi Pharma Corporation

Sanofi-Synthelabo

Jonathan Reid Frost

Patrick Andre Lardenois

Alexander E Wick

Regis Dupont

Jean Bertin

Pascal George

Corinne Rousselle

Patrick Pasau

Gabor I Koletar

Claude C Morel

Bernard Gaudilliere

Jean Rousseau

Jean Claude Muller

Paul Howard Williams

Kazutoshi Watanabe

Philippe Michel Manoury

Henry Najer

Daniel C Obitz

Adrien Tak Li

Ryoichi Ando

Fumiaki Uehara

Aya Shoda

Keiichi Arimoto

Regine Bartsch

R Egine Bartsch

Yannick Evanno

Mireille Sevrin

Jean-Claude Muller

Antonio Almario Garcia

Gihad Dargazanli

Thomas A Purcell

Salomon Z Langer

Daniel J Galtier

Lydia Zard

Michel Peynot

Johannes Schoemaker

Alfred Saarmets

Antonio Almario Carcia

Howard Williams

Maria C Renones

Jean P Thenot

A pyrimidone derivative represented by formula (I) or a salt thereof: Wherein: And a medicament comprising the said derivative or a salt thereof as an active ingredient which is used for preventive and/or therapeutic treatment of a neurodegenerative disease caused by abnormal activity of GSK3&#x3b2; such as Alzheimer's disease.

2-amino-3-(alkyl)-pyrimidone derivatives

The present invention relates to a process for preparing pyridinyl and pyrimidinyl mono-fluorinated beta keto esters of formula (I):  

Process for the preparation of pyridinyl and pyrimidinyl mono-fluorinated beta keto-esters

A pyrimidone derivative represented by formula (I) or a salt thereof: And a medicament comprising the said derivative or a salt thereof as an active ingredient which is used for preventive and/or therapeutic treatment of a neurodegenerative disease caused by abnormal activity of GSK3&#x3b2; such as Alzheimer's disease.

2-amino-3-(alkyl)-pyrimidone derivatives as GSK3.&#x3b2;.inhibitors

5-Naphthalen-1-yl-1,3-dioxane derivatives, preparation and therapeutical

Compounds of the formula: ##STR1## in which R.sub.1 represents a hydrogen or halogen atom or a methyl or C.sub.1 -C.sub.4 alkoxy group, R'.sub.1 represents a hydrogen or halogen atom, R'.sub.1 represents a hydrogen atom or a methoxy group, R.sub.3 represents a C.sub.1 -C.sub.3 alkyl group, R.sub.4 represents a 2,3-dihydro-1H-inden-2-yl, 2,3-dihydro-1H-inden-1-yl or 1,2,3,4-tetrahydronaphthalen-1-yl group, or R.sub.3 and R.sub.4 together form, with the adjacent nitrogen atom, a 1,2,3,4-tetrahydroisoquinol-2-yl, 6,7-dimethoxy-1,2,3,4-tetrahydroisoquinol-2-yl, 5,8-dimethoxy-1,2,3,4-tetrahydroisoquinol-2-yl, 1,2,3,4-tetrahydro-9H-pyrido[3,4-b]indol-2-yl, 1,2,3,4-tetrahydro-9H-pyrido[4,3-b]indol-3-yl, 4,5,6,7-tetrahydrothieno[2,3-c]pyrid-6-yl, 2,3-dihydro-1H-isoindol-2-yl or 2,3,4,5-tetra-hydro-1H-3-benzazepin-3-yl, group are useful in the treatment of cerebral disorders.

N-(3-Aminopropyl)-N-phenyl-5,6,7,8-tetrahydronaphthalene-2-carboxamide

The present invention provides a piperidine derivative of formula (I) ##STR1## in which R represents a straight- or branched-chain (C.sub.1 -C.sub.19)alkyl group, a straight- or branched-chain (C.sub.2 -C.sub.19)alkenyl group, a (C.sub.3 -C.sub.6)cycloalkyl group, a cycloalkylmethyl group in which the cycloalkyl moiety has from three to six carbon atoms, a phenyl group which is optionally substituted by a halogen atom or a phenyl methyl group which is optionally substituted by a halogen atom, or an addition salt thereof, in the form of an optically pure enantiomer or of a mixture of enantiomers, a process for making them and their therapeutic application.

Alpha-(4-chlorophenyl)-4-[(4-fluorphenyl)-methyl]piperidine-1-ethanol

Compounds of the general formula (I) ##STR1## wherein R.sub.1 represents a hydrogen, fluorine or chlorine atom or a methyl, C.sub.1 -C.sub.3 alkoxy or nitro group; R.sub.3 represents a hydrogen atom or a C.sub.1 -C.sub.3 alkyl group; R.sub.4 represents a 2,3-dihydro-1H-inden-2-yl, 2,3-dihydro-1H-inden-1-yl or 1,2,3,4-tetrahydronaphthalen-1-yl group; or alternatively R.sub.3 and R.sub.4 complete, with the nitrogen atom to which they are attached, a 1,2,3,4-tetrahydro-9H-pyrido[3,4-b]indol-2-yl, 1,2,3,4-tetrahydro-9H-pyrido[4,3-b]indol-3-yl, 4,5,6,7-tetrahydrothieno[2,3-c]pyrid-6-yl, 4,5,6,7-tetrahydrothieno[3,2-c]pyrid-6-yl or 2,3-dihydro-1H-isoindol-2-yl group; are useful for the treatment and prevention of cerebral disorders.

3-(2-aminomethyl)-4-[3-trifluoromethyl)benzoyl]-3-4

N-(-3-aminopropyl)-N-phenyl-5,6,7,8-tetrahydro-naphthalene-2-carboxamide

Compounds of the formula ##STR1## in which Y represents hydrogen, fluorine, chlorine, methyl or methoxy, R.sub.1 represents phenyl substituted by fluorine, methyl, methoxy, trifluoromethyl or phenyl, or R.sub.1 represents 2-thienyl, R.sub.2 represents methyl, and R.sub.3 represents (C.sub.1 -C.sub.4)-alkyl, or phenyl-(C.sub.1 -C.sub.2)-alkyl optionally substituted on the ring by 2 to 3 methoxy groups, or 2-(2-pyridyl)ethyl, or R.sub.2 and R.sub.3 form, with the adjacent nitrogen, 4-phenyl(1-piperidyl), 4-phenylmethyl(1-piperidyl), 1,2,3,4-tetrahydro-2-isoquinolyl, 6-methoxy-1,2,3,4-tetrahydro-2-isoquinolyl, 5,8-dimethoxy-1,2,3,4-tetrahydro-2-isoquinolyl, 6,7-dimethoxy 1,2,3,4-tetrahydro-2-isoquinolyl, 2,3,4,5-tetrahydro-1H-3-benzazepin-3-yl, or 7,8-dimethoxy-2,3,4,5-tetrahydro-1H-3-benzazepin-3-yl, and X represents carbonyl or sulphonyl, and their salts are useful as neuroprotective and antiiischaemic agents.

Benzoxazine derivatives and their application in therapy

A compound which is an ethanol or ethanone derivative of general formula (I) ##STR1## in which X represents CO or CHOH, or is an addition salt thereof with an acid, and, when X represents CHOH, is in the form of a pure enantiomer or a mixture of enantiomers, can be used for the treatment and prevention of cerebral disorders.

1-(3,4-dihydro-2-oxo-1H-quinolin-6-yl)-2-[4-(2-phenylethyl)piperidin-1-yl]e

A compound, in the form of a pure optical isomer or a mixture thereof, of formula (I): ##STR1## in which: Z represents a group of formula --CH.sub.2 --, --C(CH.sub.3).sub.2 --, --CH.dbd.CH--, --(CH.sub.2).sub.2 --, --(CH.sub.2).sub.3 --, --NH-- or --N(CH.sub.3)CH.sub.2 --, in which the nitrogen is bonded to the carbonyl group;

Derivatives of (1-hydroxy-2-piperidylalkyl-indol-2-ones, 2-quinolinones,

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

Method of treatment of psychotic disorders

A quinolinone derivative which is a compound of formula (I): ##STR1## in which: R.sub.1 and R.sub.2 are each, independently of one another, a hydrogen or halogen atom or a (C.sub.1-4)alkyl radical;

Quinolinone derivatives and their preparation in therapy

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,

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

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Wissous, France

Jonathan Reid Frost