公开(公告)号：EP1284963B1

公开(公告)日：2012-05-09

申请号：EP01938319.9

申请日：2001-05-23

申请人： CENTRE NATIONAL DE LA RECHERCHE SCIENTIFIQUE (CNRS)

发明人： RUAT, Martial ,  DODD, Robert ,  FAURE, Hélène, Véronique ,  DAUBAN, Philippe, Marcel ,  KESSLER, Albane ,  POTIER, Pierre, Jean-Paul

IPC分类号： C07D209/14 ,  A61K31/4045 ,  A61P5/18 ,  C07D209/42

CPC分类号： C07D209/42 ,  C07D209/14

摘要： The invention concerns compounds of general formula (I) wherein: the group X represents a -NR4, -CH = N or -CHR5-NR4- group; the group Y represents an oxygen or sulphur atom or a NR, -CR5, -CHR5-, -CR5=CR6- or -CHR5-CHR6 group provided that when group X represents the -CH=N- or -CHR5-NR4- group, group Y represents an oxygen or a sulphur atom or a Nr, -CR5 or -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.

摘要翻译： 本发明涉及通式（I）的化合物，其中：基团X表示-NR 4，-CH = N或-CHR 5 -NR 4 - 基团; 基团Y代表氧或硫原子或NR，-CR 5，-CHR 5 - ， - CR 5 = CR 6 - 或-CHR 5 -CHR 6基团，条件是当基团X代表-CH = N-或-CHR 5 -NR 4 - 基团 基团Y代表氧或硫原子或Nr，-CR 5或-CHR基团; 基团R表示氢原子或烷基，芳基或芳烷基; 基团R1，R5和R6相同或不同，分别代表氢或卤素原子或烷基或烷氧基; 基团R2表示氢原子或烷基; 基团R3代表芳基; 基团R4代表氢原子，烷基，芳基，芳烷基，烷基磺酰胺，芳基磺酰胺或芳烷基磺酰胺基团; 及其与药学上可接受的酸形成的盐，以外消旋混合物及其光学纯的异构体的形式存在。 本发明还涉及它们的制备，含有它们的药物组合物以及它们作为CaSR活性调节剂的用途以及优选用于治疗涉及CaSR活性调节介入的疾病或生理病症的药物。