"> Ketals of 3'
    1.
    发明授权
    Ketals of 3'"-dehydrocardenolide tridigitoxosides 失效
    3“ - 脱氢伐内酰氯沙多昔多糖的水分

    公开(公告)号:US4436735A

    公开(公告)日:1984-03-13

    申请号:US439653

    申请日:1982-11-05

    CPC分类号: C07J19/005

    摘要: The present invention provides ketals of 3'"-dehydrocardenolide tridigitoxosides of the general formula: ##STR1## in which R.sub.1 and R.sub.2 are identical alkyl radicals containing up to 3 carbon atoms or together represent a cyclic ketal containing 2 to 6 carbon atoms, R.sub.3 represents two hydrogen atoms, the group ##STR2## or the radical ##STR3## wherein R.sub.1 and R.sub.2 have the above-given meaning, and R.sub.4 is a hydrogen atom or a lower acyl or alkyl radical.The present invention also provides processes for the preparation of these ketals, as well as pharmaceutical compositions containing them, which are useful for the treatment of cardiac insufficiency.

    摘要翻译: 本发明提供了通式为:其中R 1和R 2是含有至多3个碳原子的相同烷基或一起代表含有2至6个碳原子的环状缩酮的3“ - 脱氢伐尼洛德三唑一硫酮的缩酮 原子,R 3表示两个氢原子,基团或基团,其中R 1和R 2具有上述含义,并且R 4是氢原子或低级酰基或烷基。 本发明还提供了制备这些缩酮的方法以及含有它们的药物组合物,其可用于治疗心功能不全。

    "> Oximes of 3'
    2.
    发明授权
    Oximes of 3'"-dehydrocardenolide tridigitoxosides 失效
    3'' - 脱氢山梨醇苷三ox嗪的肟

    公开(公告)号:US4461763A

    公开(公告)日:1984-07-24

    申请号:US439654

    申请日:1982-11-05

    CPC分类号: C07J41/0016

    摘要: The present invention provides 3'"-dehydrocardenolide tridigitoxoside oximes of the general formula: ##STR1## in which R.sub.1 is a hydrogen atom or an alkyl radical containing up to 3 carbon atoms, R.sub.2 is a hydrogen atom or a lower acyl or alkyl radical and R.sub.3 represents two hydrogen atoms, the group ##STR2## or the oximino group .dbd.NOR.sub.1, wherein R.sub.1 has the above-given meaning.The present invention also provides a process for the preparation of these oximes, as well as pharmaceutical compostions containing them which are useful for the treatment of cardiac insufficiency.

    摘要翻译: 本发明提供具有以下通式的3' - 脱氢伐尼德定三叠氮酮肟:其中R 1是氢原子或含有至多3个碳原子的烷基,R 2是氢原子或低级酰基 或烷基,R 3表示两个氢原子,基团肟基或肟基= NOR1,其中R 1具有上述含义。 本发明还提供了制备这些肟的方法,以及含有它们的药物组合物,其可用于治疗心功能不全。

    Cardioactive 12-dehydrodigoxin-oximes
    4.
    发明授权
    Cardioactive 12-dehydrodigoxin-oximes 失效
    心脏活性12脱氢二氧化in肟

    公开(公告)号:US4292314A

    公开(公告)日:1981-09-29

    申请号:US151481

    申请日:1980-05-19

    CPC分类号: C07J41/0016

    摘要: The present invention provides 12-dehydrodigoxin oximes of the general formula: ##STR1## wherein R.sub.1 and R.sub.2, which can be the same or different, are hydrogen atoms, lower acyl radicals or lower alkyl radicals or R.sub.1 and R.sub.2 together can represent an alkylidene radical containing 2 to 6 carbon atoms and R.sub.3 is a hydrogen atom or a lower alkyl or aralkyl radical. The present invention also provides a process for the preparation of these oximes and pharmaceutical compositions containing them and is also concerned with the use of these oximes for the preparation of pharmaceuticals for the treatment of cardiac insufficiency.

    摘要翻译: 本发明提供了以下通式的12-脱氢二氧in肟:其中R 1和R 2可以相同或不同,为氢原子,低级酰基或低级烷基,或者R 1和R 2一起可代表亚烷基 含有2至6个碳原子,且R 3是氢原子或低级烷基或芳烷基。 本发明还提供了制备这些肟和含有它们的药物组合物的方法,并且还涉及这些肟用于制备用于治疗心功能不全的药物的用途。

    Preparation of C22-alkyl derivative of digoxin
    6.
    发明授权
    Preparation of C22-alkyl derivative of digoxin 失效
    地高辛C22烷基衍生物的制备

    公开(公告)号:US3981862A

    公开(公告)日:1976-09-21

    申请号:US558381

    申请日:1975-03-14

    IPC分类号: C07J19/00

    CPC分类号: C07J19/005

    摘要: A process for the preparation of a C22-alkyl-derivative of digoxin of the formula ##SPC1##In whichR.sub.1 is an alkyl radical containing up to 4 carbon atoms,R.sub.2 and R.sub.3 are selected from the group consisting of hydrogen, acyl, benzyl, carbobenzoxy, trimethylsilyl, tetrahydropyranyl or phosphonoacyl radicals or together form an alkylidene radical,Comprising reacting a compound of the formula ##SPC2##With an alkyl iodide of the formula R.sub.1 I in the presence of a strongly polar aprotic solvent and an alkali metal hydride. If R.sub.2 and R.sub.3 are other than hydrogen they can subsequently be replaced by hydrogen by hydrolysis or hydrogenation. The product can be .alpha.- or .beta.-methylated to produce compounds of high resorption and low toxicity.

    摘要翻译: 制备式IN的地高辛的C22-烷基衍生物的方法,其中R1是含有至多4个碳原子的烷基,R2和R3选自氢,酰基,苄基,苄氧羰基,三甲基甲硅烷基 ,四氢吡喃基或膦酰基基团或一起形成亚烷基,在强极性非质子溶剂和碱金属氢化物的存在下,将式I化合物与式Ia化合物反应。 如果R2和R3不是氢,那么它们随后可以通过水解或氢化被氢代替。 该产物可以是α-甲基化或β-甲基化以产生高吸收和低毒性的化合物。