1,3-Dihydro-2h-indol-2-one derivative
    3.
    发明申请
    1,3-Dihydro-2h-indol-2-one derivative 失效
    1,3-二氢-2H-吲哚-2-酮衍生物

    公开(公告)号:US20060276449A1

    公开(公告)日:2006-12-07

    申请号:US10569833

    申请日:2004-08-27

    CPC分类号: C07D403/04

    摘要: A 1,3-dihydro-2H-indol-2-one derivative expressed by Formula 1 (wherein R1 is a halogen atom, a C1 to C4 alkyl group, etc., and R2 is a hydrogen atom, a halogen atom, etc., or R2 is in the 6-position of the indol-2-one and R1 and R2 join together to form a C3 to C6 alkylene group, R3 is a halogen atom, a hydroxyl group, etc., and R4 is a hydrogen atom, a halogen atom, a C1 to C4 alkyl group, etc., or R4 is in the 3-position of the phenyl and R3 and R4 join together to form a methylenedioxy group, R5 is a hydrogen atom or a fluorine atom, R6 is an ethylamino group, a dimethylamino group, etc., R7 is a C1 to C4 alkoxy group, and R8 is a C1 to C4 alkoxy group), or a pharmaceutically acceptable salt of this derivative. This is a novel compound that has antagonistic activity against an aruginine-vasopressin V1b receptor.

    摘要翻译: 由式1表示的1,3-二氢-2H-吲哚-2-酮衍生物(其中R 1是卤素原子,C 1至C 1烷基, 4个烷基等,R 2是氢原子,卤原子等,或R 2 2位在6位的 吲哚-2-酮和R 1和R 2连接在一起以形成C 6 -C 6亚烷基, 亚烷基,R 3是卤素原子,羟基等,R 4是氢原子,卤原子,C 1, / SUB→C 4烷基等,或R 4在苯基的3位和R 3和R 3 连接在一起形成亚甲二氧基,R 5是氢原子或氟原子,R 6是乙氨基,二甲基氨基 基团等,R 7是C 1-4烷氧基的C 1至C 8,并且R 8是 C 1至C 4烷氧基),或该衍生物的药学上可接受的盐。 这是一种新的化合物,具有对抗葡萄糖酸加压素V1b受体的拮抗作用。

    1,3-dihydro-2H-indol-2-one derivative
    4.
    发明授权
    1,3-dihydro-2H-indol-2-one derivative 失效
    1,3-二氢-2H-吲哚-2-酮衍生物

    公开(公告)号:US07528124B2

    公开(公告)日:2009-05-05

    申请号:US10569833

    申请日:2004-08-27

    CPC分类号: C07D403/04

    摘要: A 1,3-dihydro-2H-indol-2-one derivative expressed by Formula 1 (wherein R1 is a halogen atom, a C1 to C4 alkyl group, etc., and R2 is a hydrogen atom, a halogen atom, etc., or R2 is in the 6-position of the indol-2-one and R1 and R2 join together to form a C3 to C6 alkylene group, R3 is a halogen atom, a hydroxyl group, etc., and R4 is a hydrogen atom, a halogen atom, a C1 to C4 alkyl group, etc., or R4 is in the 3-position of the phenyl and R3 and R4 join together to form a methylenedioxy group, R5 is a hydrogen atom or a fluorine atom, R6 is an ethylamino group, a dimethylamino group, etc., R7 is a C1 to C4 alkoxy group, and R8 is a C1 to C4 alkoxy group), or a pharmaceutically acceptable salt of this derivative. This is a novel compound that has antagonistic activity against an aruginine-vasopressin V1b receptor.

    摘要翻译: 由式1表示的1,3-二氢-2H-吲哚-2-酮衍生物(其中,R 1为卤素原子,C 1〜C 4烷基等,R 2为氢原子,卤素原子等) ,或R2为吲哚-2-酮的6-位,R 1和R 2连接在一起形成C 3〜C 6亚烷基,R 3为卤素原子,羟基等,R 4为氢原子 卤素原子,C 1〜C 4烷基等,或者R 4在苯基的3-位,R3和R4连接在一起形成亚甲二氧基,R5是氢原子或氟原子,R6是 乙基氨基,二甲基氨基等,R7为C1〜C4烷氧基,R8为C1〜C4烷氧基)或该衍生物的药学上可接受的盐。 这是一种新的化合物,具有对抗葡萄糖酸加压素V1b受体的拮抗作用。

    Process for producing erythromycin derivative
    6.
    发明授权
    Process for producing erythromycin derivative 失效
    红霉素衍生物的制备方法

    公开(公告)号:US06713615B2

    公开(公告)日:2004-03-30

    申请号:US10344529

    申请日:2003-02-12

    IPC分类号: C07H100

    CPC分类号: C07H17/08

    摘要: There is provided a preparation process useful for an efficient synthesis of 6-O-substituted ketolide derivatives by combining a characterized step of introduction of a substituent at the 6-position by selective cleavage of a C—O bond of the cyclic acetal at the 9-position side via 6,9-cyclic acetal 5-O-desosaminyl erythronolide derivative, a step of conversion into carbonyl groups at the 9- and 3-positions, and a step of 11,12-cyclic carbamation to lead to 6-O-substituted ketolide derivatives.

    摘要翻译: 提供了一种用于有效合成6-O-取代的酮内酯衍生物的制备方法,其通过组合在6位上引入取代基的特征性步骤,通过选择性裂解环状缩醛在9位上的CO键 通过6,9-环状缩醛5-O-去氨基酰基红新环素衍生物,在9位和3位转化为羰基的步骤和11,12-环状氨基甲酰化作用以产生6-O-取代的步骤 酮内酯衍生物。