申请人:——
公开号:US20030199497A1
公开(公告)日:2003-10-23
The invention concerns compounds of general formula (I) wherein:
1
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 aralkyl sulphonamide 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.
本发明涉及一般式(I)的化合物,其中:1.基团X代表- NR4,-CH═N或-CHR5-NR4基团;基团Y代表氧或硫原子或NR,-CR5,-CHR5-,-CR5=CR6-或-CHR5-CHR6基团,但当基团X表示-CH═N-或-CHR5-NR4基团时,基团Y代表氧或硫原子或NR,-CR5或-CHR基团;基团R代表氢原子或烷基,芳基或芳烷基;基团R1,R5和R6,相同或不同,分别代表氢或卤原子或烷基或烷氧基;基团R2代表氢原子或烷基;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;以及它们在药学上可接受的酸盐形式,以外消旋混合物和其光学纯异构体。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活性调节剂和作为治疗涉及CaSR活性调节干预的疾病或生理紊乱的药物的用途。