Class of seco bis-indolic compounds which can be used as drugs and a
process for the preparation thereof
    1.
    发明授权
    Class of seco bis-indolic compounds which can be used as drugs and a process for the preparation thereof 失效
    可用作药物的分离双吲哚化合物的类别及其制备方法

    公开(公告)号:US4347249A

    公开(公告)日:1982-08-31

    申请号:US167377

    申请日:1980-07-09

    CPC分类号: C07D519/04 Y10S514/908

    摘要: The invention relates to new chemical compounds.They are compounds corresponding to formula Ia. ##STR1## in which: R'.sub.3 represents a hydrogen atom or a hydroxy radical; R'.sub.5 represents a hydrogen atom or a hydroxy radical; or R'.sub.3 and R'.sub.5 together represent an epoxy bridge or a double bond; R".sub.5 represents a hydrogen atom or an ethyl radical; R'.sub.7 and R'.sub.8 are the same or different and represent a hydrogen atom or a methyl, hydroxymethylene, alkoxymethylene, aryloxymethylene, aminomethylene, monoalkyl or dialkyl aminomethylene, acylmethylene, arylaminomethylene, hydroxyethyl aminomethylene, alkylthiomethylene, aryloxythiomethylene or cyanomethylene radical; R.sub.1 represents a hydrogen atom or an alkyl, formyl or acyl radical: R.sub.2 represents a hydrogen atom or an alkoxy radical; R.sub.7 represents an alkanoyloxy radical, the broken line representing an optional double bond.These compounds can be used as drugs.

    摘要翻译: 本发明涉及新的化合物。 它们是对应于式Ia的化合物。 (Ia)其中:R'3表示氢原子或羟基; R'5表示氢原子或羟基; 或R'3和R'5一起表示环氧桥或双键; R“5表示氢原子或乙基; R'7和R'8相同或不同,表示氢原子或甲基,羟基亚甲基,烷氧基亚甲基,芳氧基亚甲基,氨基亚甲基,单烷基或二烷基氨基亚甲基,酰亚胺基,芳基氨基亚甲基,羟乙基氨基亚甲基,烷基亚甲基,芳氧基亚甲基或氰基亚甲基。 R1表示氢原子或烷基,甲酰基或酰基:R2表示氢原子或烷氧基; R 7表示烷酰氧基,虚线表示任选的双键。 这些化合物可以用作药物。

    Nor bis-indole compounds usable as medicaments
    3.
    发明授权
    Nor bis-indole compounds usable as medicaments 失效
    也不能用作药物的双吲哚化合物

    公开(公告)号:US4307100A

    公开(公告)日:1981-12-22

    申请号:US67439

    申请日:1979-08-20

    IPC分类号: C07D519/04 A61K31/475

    CPC分类号: C07D519/04

    摘要: Compounds with antitumoral activity corresponding to the formula (I): ##STR1## wherein R'.sub.1 is a hydrogen atom or an alkoxy, acyl, formyl or haloacyl radical; R'.sub.2 is a hydrogen atom or an alkyl radical; R'.sub.3 and R".sub.3 are a hydrogen atom, hydroxyl radical or an alkanoyloxy radical, and together are a carbonyl group, and R'.sub.3 and R'.sub.5 together are an epoxy bridge or a double bond; R'.sub.4 is a hydrogen atom or an alkyloxycarbonyl, hydroxymethyl, alkanoyloxymethyl or acetamido radical; R'.sub.5 and R".sub.5 are a hydrogen atom or a hydroxyl, alkanoyloxyl, ethyl or 2-hydroxyethyl radical; R'.sub.6 is a hydrogen atom or an ethyl, 2-hydroxyethyl or acetyl radical; R.sub.1 is a hydrogen atom or an alkyl, formyl or acyl radical; R.sub.2 is a hydrogen atom or alkoxy radical; R.sub.3 is a hydrogen atom or a hydroxyl or alkanoyloxyl radical, and together with R.sub.4 is an epoxy bridge or a double bond; R.sub.4 is a hydrogen atom or a hydroxyl, alkanoyloxyl radical, and together with R.sub.5 is an epoxy bridge; R.sub.6 is an alkyloxycarbonyl, hydrazido, acetamido, hydroxymethyl or alkanoyloxymethyl radical; and R.sub.5 and R.sub.7 are a hydrogen atom or a hydroxyl and alkanoyloxyl radical; acid addition and quaternary ammonium salts thereof and 12-chloro derivatives thereof.

    摘要翻译: 具有对应于式(I)的抗肿瘤活性的化合物:其中R'1是氢原子或烷氧基,酰基,甲酰基或卤代酰基; R'2是氢原子或烷基; R'3和R'3是氢原子,羟基或烷酰氧基,并且一起是羰基,R'3和R'5一起是环氧桥或双键; R'4是氢原子或烷氧基羰基,羟甲基,烷酰氧基甲基或乙酰氨基; R'5和R'5是氢原子或羟基,烷酰氧基,乙基或2-羟乙基; R 6是氢原子或乙基,2-羟乙基或乙酰基; R1是氢原子或烷基,甲酰基或酰基; R2是氢原子或烷氧基; R3是氢原子或羟基或烷酰氧基,与R4一起是环氧桥或双键; R4是氢原子或羟基,烷酰氧基,与R5一起是环氧桥; R6是烷氧基羰基,酰肼基,乙酰氨基,羟甲基或烷酰氧基甲基; 并且R 5和R 7是氢原子或羟基和烷酰氧基; 酸加成物及其季铵盐和其12-氯衍生物。

    Process for the synthesis of leurosine and of its derivatives
    5.
    发明授权
    Process for the synthesis of leurosine and of its derivatives 失效
    合成酪氨酸及其衍生物的方法

    公开(公告)号:US4322350A

    公开(公告)日:1982-03-30

    申请号:US895379

    申请日:1978-04-11

    IPC分类号: C07D519/04

    CPC分类号: C07D519/04

    摘要: A process for the preparation of a compound of formula (V) and salts thereof ##STR1## wherein R.sub.1 is selected from the group consisting of a hydrogen atom, an alkyl radical, a formyl radical and an acyl radical;R.sub.2 is selected from the group consisting of an alkoxycarbonyl radical, a hydrazide radical, an acetamido radical, a hydroxymethyl radical, and an alkanoyloxy methyl radicalandR.sub.3 and R.sub.4 are the same or different and each is selected from the group consisting of a hydrogen atom, a hydroxyl radical and an alkanoyloxyl radical;which comprises the step of treating a compound of formula IV ##STR2## wherein R.sub.1, R.sub.2, R.sub.3 and R.sub.4 are as previously defined with at least one oxidising agent selected from the group consisting of oxidising metal salts, air and oxygen.The above compounds are useful due to their antitumoral activity, and to their use as intermediates of other antitumor drugs.

    摘要翻译: 制备式(V)化合物及其盐的方法其中R 1选自氢原子,烷基,甲酰基和酰基; R2选自烷氧基羰基,酰肼基,乙酰氨基,羟甲基和烷酰氧基甲基,R3和R4相同或不同,各自选自氢原子 ,羟基和烷酰氧基; 其包括处理式IV化合物(IV)的步骤,其中R 1,R 2,R 3和R 4如前所定义,与至少一种选自氧化金属盐,空气和氧气的氧化剂组合。 上述化合物由于其抗肿瘤活性而有用,并且用作其它抗肿瘤药物的中间体。