Centre National De La Recherche Scientifique

Other

Assistance Publique-hopitaux De Paris

Université Paris—sud

Université Paris-saclay

Centre National De La Recherche Scientifique-cnrs

Robert H Dodd

Pierre Jean-Paul Potier

Pierre Potier

Martial Ruat

Jean Rossier

Kevin Cariou

Albane Kessler

Philippe Marcel Dauban

Thierry Naas

Werner Sieghart

Frantisek Jursky

Urs Thomet

Roman Furtmuller

Erwin Sigel

Hélène Faure

Gilbert Dorey

Bogdan Iorga

Marie-Claude Potier

Jean-Paul Pierre Potier

Lia P De Carvalho

Bogdan-Iuliu Iorga

Xavier Doisy

Eugénie Romero

Marie-Caude Potier

Hélène Véronique Faure

Benoît Delatour

Saoussen Oueslati

Jérôme Braudeau

Ahmed El Hadri

Laurent Dubois

Yann Herault

Rodolphe Razet

Mohamed Benchekroun

Corinne Minard

Lia Prado De Carvalho

The present application relates to novel 3-imidazolines of formula (I') and (I) below: (I&#x2032;) (I) Wherein Ar, Ar, Ar, and Rto Rare as defined in the claims. The 3-imidazolines of the invention are useful in antibiotic therapies, in particular as inhibitors of carbapenemases. They are also useful as antibiotics themselves. The present invention also concerns a method for preparing more specifically the 3-imidazolines of formula (I). The present invention further relates to conjugates of said compounds with known antibiotics. 

2- or 3-imidazolines as carbapenemases inhibitors

The present application relates to novel azetidinimine of formula (I). Wherein R-Rare as defined in claim. The azetidinimine of the invention are useful as antibiotics and as inhibitors of a carbapenemases. The present invention thus further relates to their use in antibiotic therapies and their methods of synthesis. 

Azetidinimines as carbapenemases inhibitors

Compounds having inverse agonist functional selectivity for GABAreceptors containing the &#x3b1;5 subunit for use as a medicament in the treatment of cognitive impairments in subjects suffering from Down syndrome. The use of these compounds is disclosed. Pharmaceutical compositions for such treatment can comprise these compounds or suitable pharmaceutically acceptable salt thereof, a polyethoxylated castor oil and dimethyl sulfoxide (DMSO). Methods are disclosed for enhancing cognitive function, or treating or lessening the severity of cognitive impairments, in subjects suffering from Down syndrome by administering to a subject in need thereof a pharmaceutically effective amount of one or more of these compounds.

Composition and method for treating cognitive impairments in down syndrom subjects

The invention concerns diamines of general formula (I), wherein: A represents a group A1 or A2 of general formula (II); B represents a group B1 or B2 of general formula (III); X represents a SO, CH, C&#x2550;O or COO; YZ represents a group of formula CH(R25)&#x2014;CH(R26) or CH(R27)&#x2550;(R28), and R1 to R28, identical or different, represent independently of one another, a hydrogen or halogen atom or an alkyl, cycloalkyl, CN, NO, hydroxy, aryl, aralkyl, alkoxy, aryloxy, amino, alkylamino, dialkylamino, cycloalkylamino, arylamino, arylalkylamino, diarylamino diarylalkylamino, trihalogenoalkyl or trihalogenoalkoxy group, provided that in the group A1, at least one of the radicals R1, R2, R3, R4 or R5 represents the hydrogen atom when the other four do not represent the hydrogen atom and in the group B1, at least one of the radicals R13, R14, R15, R16 or R17 represents the hydrogen atom when the other four do not represent the hydrogen atom, and their salts with a pharmaceutically acceptable acid, in the form of racemic mixture or their optically pore isomers. The invention also concerns their preparation, pharmaceutical compositions comprising them and their use as CaSR activity modulator and as medicine particularly designed for the treatment of psychological diseases and disorders involving CaSR activity modulation.

Diamines having a CaSR modulating activity

The invention concerns compounds of general formula (I) wherein: the group X represents a &#x2014;NR4, &#x2014;CH&#x2550;N or &#x2014;CHR5-NR4-group; the group Y represents an oxygen or sulphur atom or a NR, &#x2014;CR5, &#x2014;CHR5-, &#x2014;CR5=CR6- or &#x2014;CHR5-CHR6 group provided that when group X represents the &#x2014;CH&#x2550;N&#x2014; or &#x2014;CHR5-NR4-group, group Y represents an oxygen or a sulphur atom or a Nr, &#x2014;CR5 or &#x2014;CHR group; the group R represents a hydrogen atom or an alkyl, aryl or aralkyl group; the groups R1, R5 and R6, identical or different, represent each a hydrogen or halogen atom or an alkyl or alkoxy group; the group R2 represents a hydrogen atom or an alkyl group; the group R3 represents an aryl group; and the group R4 represents a hydrogen atom, an alkyl, aryl, aralkyl, alkylsulphonamide, arylsulphonamide or aralkylsulphonamide group; and their salt with a pharmaceutically acceptable acid, in the form of a racemic mixture and their optically pure isomer. The invention also concerns their preparation, pharmaceutical compositions containing them and their use as CaSR activity modulator and as medicine for preferably treating diseases or physiological disorders involving the intervention of CaSR activity modulation. 

Calcium receptor active molecules and method for preparing same

The invention concerns compounds represented by general formula (I) wherein: Z represents a sulfur or oxygen atom; the groups R1 and R2, identical or different, represent each a alkyl group or an alkenyl group; X represents a CO, a CO , an SO, or an SO and the group R represents an alkyl, aryl, alkenyl, or aralkyl group, provided that when Z represents an oxygen atom, X an SO and R a group (a), R1 and R2 do not both represent the methyl group. The invention also concerns methods for preparing said compounds, pharmaceutical compositions containing them and their use as promoter of &ggr;-aminobutyric acid and as medicine particularly designed for treating nervous disorders.

N substituted 3-amino-2,2-di-c-alkyl-1,4-butyrolactones and 1,4-thiobutyrolactones for use as promoter of &ggr;-aminobutyric acid activity and for treating nervous disorders and preparation method

The invention concerns compounds of general formula (I) wherein: Z represents a sulphur or oxygen atom, NH, N-alkyl or Nboc; group R&prime;, identical or different, represent each a hydrogen atom, a OCH group or a OCH O group; group R&Prime; represents a hydrogen or a CH group; group X represents a carbonyl, sulphonyl or CO group; and group R represents an alkyl, aryl, alkenyl or aralkyl group. The invention also concerns the preparation of said compounds, pharmaceutical compositions containing them and their use for stimulating &ggr;-amino-butyric acid activity and as medicine for treating nervous disorders.

N-substituted 1-(lactone) isoquinolones for treating nervous disorders

Compounds derived from 6-azaindoles as ligands of the benzodiazepine

The invention relates to novel .beta.-carboline-derived compounds which are benzodiazepine-receptor ligands having an inverse agonist and antagonist effect on benzodiazepines. These compounds are of the formulae: ##STR1## in which: X is O, S, ##STR2## or alternatively, ##STR3## represents the radical --N(R.sub.6)--C(=O)--CH.sub.2 --X, R.sub.1 is a hydroxyl, alkoxy or alkyl radical substituted by a hydroxyl or alkoxy radical,

.beta.-Carboline-derived compounds, lamchart benzodiazepine-receptor

Growing community of inventors

Paris, France

Robert H Dodd