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:
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:
Cardioactive cardenolide-bis-digitoxosides of the formula ##STR1## in which R.sub.1 is a hydrogen atom, a hydroxyl group or an acyloxy radical containing up to 3 carbon atoms, andR.sub.2, R.sub.3 and R.sub.4 each independently is a hydrogen atom, an acyl radical containing up to 3 carbon atoms,with the proviso that the compound contains at least one alkyl radical. The compounds exhibit desirable rates of excretion, primarily extrarenally.
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:
New dihydrodigoxin derivatives of the formula ##SPC1##Wherein one of R.sub.1 and R.sub.2 represents a methyl or ethyl radical and the other represents hydrogen, methyl, ethyl or acetyl (i.e. alkanoyl; and R.sub.3 is hydrogen or an acetyl group; are outstandingly effective for therapy of cardiac insufficiencies, particularly via peroral administration.
摘要翻译:式R 1和R 2的新的二氢二磷杂衍生物代表甲基或乙基,另一个表示氢,甲基,乙基或乙酰基(即烷酰基; R 3是氢或乙酰基);对治疗心脏功能不全有显着的效果 ,特别是通过口腔管理。
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.