Use of quinolinone derivatives as a research tool
    7.
    发明授权
    Use of quinolinone derivatives as a research tool 有权
    使用喹啉酮衍生物作为研究工具

    公开(公告)号:US08957091B2

    公开(公告)日:2015-02-17

    申请号:US13885098

    申请日:2011-11-15

    摘要: The present invention relates to the use of quinolinone derivatives of general formula (I), ligands of the Smo receptor or of related receptors which target a binding site of the receptor which is different from the known ligand binding sites, as research tools for identifying modulators of the Smo receptor or of related receptors, characterizing the Hedgehog signalling pathway and diagnosis; the invention also relates to kits containing said derivatives of general formula (I).

    摘要翻译: 本发明涉及使用通式(I)的喹啉酮衍生物,Smo受体的配体或靶向与已知配体结合位点不同的受体的结合位点的相关受体作为鉴定调节剂的研究工具 的Smo受体或相关受体,表征Hedgehog信号通路和诊断; 本发明还涉及含有通式(I)的所述衍生物的试剂盒。

    Use Of Quinolinone Derivatives As A Research Tool
    8.
    发明申请
    Use Of Quinolinone Derivatives As A Research Tool 有权
    使用喹啉酮衍生物作为研究工具

    公开(公告)号:US20130236912A1

    公开(公告)日:2013-09-12

    申请号:US13885098

    申请日:2011-11-15

    摘要: The present invention relates to the use of quinolinone derivatives of general formula (I), ligands of the Smo receptor or of related receptors which target a binding site of the receptor which is different from the known ligand binding sites, as research tools for identifying modulators of the Smo receptor or of related receptors, characterizing the Hedgehog signalling pathway and diagnosis; the invention also relates to kits containing said derivatives of general formula (I).

    摘要翻译: 本发明涉及使用通式(I)的喹啉酮衍生物,Smo受体的配体或靶向与已知配体结合位点不同的受体的结合位点的相关受体作为鉴定调节剂的研究工具 的Smo受体或相关受体,表征Hedgehog信号通路和诊断; 本发明还涉及含有通式(I)的所述衍生物的试剂盒。

    Novel diamines having a casr modulating activity
    10.
    发明申请
    Novel diamines having a casr modulating activity 失效
    具有casr调节活性的新型二胺

    公开(公告)号:US20050192317A1

    公开(公告)日:2005-09-01

    申请号:US10344146

    申请日:2001-08-07

    摘要: 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 SO2, CH2, C═O or COO; YZ represents a group of formula CH(R25)—CH(R26) or CH(R27)═(R28), and R1 to R28, identical or different, represent independently of one another, a hydrogen or halogen atom or an alkyl, cycloalkyl, CN, NO2, 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.

    摘要翻译: 本发明涉及通式(I)的二胺,其中:A表示通式(II)的基团A1或A2; B表示通式(III)的基团B1或B2; X表示SO 2,CH 2,C-O或COO; y Z表示式CH(R 25)-CH(R 26)或CH(R 27) - (R 28)的基团,并且R 1至R 28相同或不同,彼此独立地表示氢或 卤素原子或烷基,环烷基,CN,NO 2,羟基,芳基,芳烷基,烷氧基,芳氧基,氨基,烷基氨基,二烷基氨基,环烷基氨基,芳基氨基,芳基烷基氨基,二芳基氨基二芳基烷基氨基,三卤代烷基或三卤代烷氧基, 条件是在组A1中,当其它四个不表示氢原子时,基团R 1,R 2,R 3,R 4或R 5中的至少一个表示氢原子,在基团B1中,基团R 13, R 14,R 15,R 16或R 17表示氢原子,当其它四个不表示氢原子时,它们与药学上可接受的酸的盐以外消旋混合物或其o 分子孔异构体。 本发明还涉及它们的制备,包含它们的药物组合物及其作为CaSR活性调节剂的用途,以及用于治疗涉及CaSR活性调节的心理疾病和病症的药物。