1,2,8,8A-tetrahydrocyclopropa(c)pyrrolo(3,2-e)-indol-4-(5H)-ones and
related compounds
    3.
    发明授权
    1,2,8,8A-tetrahydrocyclopropa(c)pyrrolo(3,2-e)-indol-4-(5H)-ones and related compounds 失效
    1,2,8,8-四氢环丙(c)吡咯并(3,2-e) - 吲哚-4-(5H) - 酮和相关化合物

    公开(公告)号:US4912227A

    公开(公告)日:1990-03-27

    申请号:US894314

    申请日:1986-08-07

    摘要: 1,2,8,8a-Tetrahydrocyclopropa[3]pyrrolo(3,2-e)indol-4(5H)-ones, and related compounds of formulas I and intermediate therefor II ##STR1## wherein R.sub.2, R.sub.2 ', R.sub.3, R.sub.5, R.sub.50 and X are as defined in the specification, e.g., (7bR,8aS)-1,2,8,8a-tetrahydro-7-methyl-2-[[5-(((1H-indol-2-yl)carbonyl)amino)-1H-indol-2-yl]carbonyl]cyclopropa[pyrrolo[3,2-e]indol-4(5H)-one (U-71,184), as purified, and its racemic form (U-68,415), and related compounds, are useful as ultraviolet light absorbers and as antibacterials. The lead compounds are useful as antitumor drug compounds in standard laboratory animal tests.

    摘要翻译: 1,2,8,8a-四氢环丙基[3]吡咯并(3,2-e)吲哚-4(5H) - 酮及其相应的式I化合物及其中间体II其中R 2, R2',R3,R5,R50和X如说明书中所定义,例如(7bR,8aS)-1,2,8,8a-四氢-7-甲基-2 - [[5 - (((1H- 吲哚-2-基)羰基)氨基)-1H-吲哚-2-基]羰基]环丙基]吡咯并[3,2-e]吲哚-4(5H) - 酮(U-71,184),纯化,其 外消旋形式(U-68,415)和相关化合物可用作紫外光吸收剂和抗菌剂。 铅化合物在标准实验室动物试验中可用作抗肿瘤药物化合物。

    &bgr;-sulfonyl hydroxamic acids
    5.
    发明授权
    &bgr;-sulfonyl hydroxamic acids 失效
    β-磺酰基异羟肟酸

    公开(公告)号:US06235928B1

    公开(公告)日:2001-05-22

    申请号:US09269185

    申请日:1999-07-26

    IPC分类号: C07C31704

    CPC分类号: C07C317/44 C07D233/72

    摘要: The present invention provides a compound of formula (I) or a pharmaceutically acceptable salt thereof. Such compounds may be incorporated into pharmaceutical compositions which can inhibit various enzymes from the matrix metalloproteinase family.

    摘要翻译: 本发明提供式(I)化合物或其药学上可接受的盐。 这样的化合物可以并入可以抑制基质金属蛋白酶家族的各种酶的药物组合物中。

    1,2,8,8a-tetrahydrocyclopropa (C) pyrrolo [3,2-e)]-indol-4(5H)-ones and
related compounds
    8.
    发明授权
    1,2,8,8a-tetrahydrocyclopropa (C) pyrrolo [3,2-e)]-indol-4(5H)-ones and related compounds 失效
    1,2,8,8a-四氢环丙(C)吡咯并[3,2-e]] - 吲哚-4(5H) - 酮和相关化合物

    公开(公告)号:US4978757A

    公开(公告)日:1990-12-18

    申请号:US444176

    申请日:1989-11-30

    摘要: 1,2,8,8a-Tetrahydrocyclopropa[3]pyrrolo(3,2-e)indol-4(5H)-ones, and related compounds of formulas I and intermediate therefor II ##STR1## wherein R.sub.2, R.sub.2 ', R.sub.3, R.sub.5, R.sub.50 and X are as defined in the specification, e.g., (7bR,8aS)-1,2,8,8a -tetrahydro-7-methyl-2-[[5-(((1H-indol-2-yl)carbonyl)amino)-1H-indol-2-yl]carbonyl]cyclopropa[pyrrolo[3,2-e]indol-4(5H)-one (U-71,184), as purified, and its racemic form (U-68,415), and related compounds, are useful as ultraviolet light absorbers and as antibacterials. The lead compounds are useful as antitumor drug compounds in standard laboratory animal tests.

    摘要翻译: 1,2,8,8a-四氢环丙基[3]吡咯并(3,2-e)吲哚-4(5H) - 酮及其相应的式I化合物及其中间体II其中R 2, R2',R3,R5,R50和X如说明书中所定义,例如(7bR,8aS)-1,2,8,8a-四氢-7-甲基-2 - [[5 - (((1H- 吲哚-2-基)羰基)氨基)-1H-吲哚-2-基]羰基]环丙基]吡咯并[3,2-e]吲哚-4(5H) - 酮(U-71,184)纯化,其 外消旋形式(U-68,415)和相关化合物可用作紫外光吸收剂和抗菌剂。 铅化合物在标准实验室动物试验中可用作抗肿瘤药物化合物。

    Preparing indoline derivatives
    9.
    发明授权
    Preparing indoline derivatives 失效
    制备二氢吲哚衍生物

    公开(公告)号:US4590280A

    公开(公告)日:1986-05-20

    申请号:US712307

    申请日:1985-03-15

    IPC分类号: C07D209/12

    CPC分类号: C07D209/12

    摘要: An improved process for preparing sulfonylated indoline compounds of the formula ##STR1## via reduction of a nitrodiol of the formula ##STR2## where R.sub.1 and R.sub.3 are defined in the specification, to obtain the corresponding aminodiol ##STR3## and then the aminodiol (III) is sulfonylated and cyclized in situ to obtain the sulfonylated indoline compound (I). The substituted indoline compounds (I) are useful in overall processes for making 1,2,8,8a-cyclopropa[c]benzo[1,2-b:4,3-b']dipyrrol-4(5H)-ones which have useful light absorber, anti-bacterial and anti-tumor pharmaceutical use properties.

    摘要翻译: 通过还原式(II)的硝基二醇制备式(I)的磺酰化二氢吲哚化合物的改进方法,其中R 1和R 3在说明书中定义,以获得相应的氨基二醇(IMAGE)( III),然后将氨基二醇(III)磺酰化并原位环化,得到磺酰化二氢吲哚化合物(I)。 取代的二氢吲哚化合物(I)可用于制备1,2,8,8a-环丙并[c]苯并[1,2-b:4,3-b']二吡咯-4(5H)酮的总体方法,其中 具有有用的光吸收剂,抗菌和抗肿瘤药物使用性质。