Centre National De La Recherche Scientifique

Philippe Marcel Dauban

Martial Ruat

Robert H Dodd

Pierre Jean-Paul Potier

Albane Kessler

Hélène Véronique Faure

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. 

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Sanite-Genevieve-des-Bois, France

Philippe Marcel Dauban