摘要:
The invention relates to new cytostatic compound, process for their preparation and pharmaceutical compositions containing them. More particularly, there are provided new compounds of the general formula ##STR1## in which R.sup.4 is .beta.-hydroxyl andR.sup.3 is .alpha.-ethyl; orR.sup.4 is hydrogen andR.sup.3 is .beta.-ethyl;R" is a straight chained alkyl having from 1 to 10 carbon atoms, or a branched chained alkyl having from 3 to 10 carbon atoms, in which groups the carbon atom attached to the >N.sub.a -CH.sub.2 -O-- group has a primary or secondary configuration or an alkenyl or alkinyl having from 3 to 6 carbon atoms, or an aralkyl having from 1 to 3 carbon atoms in the alkyl moiety;R.sup.1 is methoxy andR.sup.2 is acetyl,provided that if R.sup.3 is .alpha.-ethyl and R.sup.4 .beta.-hydroxyl, R.sup.4 is other than ethyl.These compounds and N-desmethyl-N- ethoxy- methyl -vinblastine can be prepared according to the invention by transetherification of compounds of the compounds of the general formula ##STR2## with a large excess of alcohols of the general formulaR"--OH (III)Pharmaceutical compositions containing compounds of the general formula /I/ as active ingredients are also within the scope of invention.
摘要:
The invention relates to new cytostatic compound, process for their preparation and pharmaceutical compositions containing them. More particularly, there are provided new compounds of the general formula ##STR1## in which R.sup.4 is .beta.-hydroxyl andR.sup.3 is .alpha.-ethyl; orR.sup.4 is hydrogen andR.sup.3 is .beta.-ethyl;R" is a straight chained alkyl having from 1 to 10 carbon atoms, or a branched chained alkyl having from 3 to 10 carbon atoms, in which groups the carbon atom attached to the >N.sub.a --CH.sub.2 --O-- group has a primary or secondary configuration or an alkenyl or alkinyl having from 3 to 6 carbon atoms, or an aralkyl having from 1 to 3 carbon atoms in the alkyl moiety;R.sup.1 is methoxy andR.sup.2 is acetyl, provided that if R.sup.3 is .alpha.-ethyl and R.sup.4 .beta.-hydroxyl,R.sup.4 is other than ethyl.These compounds and N-desmethyl-N-(ethoxymethyl)-vinblastine can be prepared according to the invention by transetherification of compounds of the compounds of the general formula ##STR2## with a large excess of alcohols of the general formulaR"--OH [III]Pharmaceutical compositions containing compounds of the general formula [I] as active ingredients are also within the scope of invention.
摘要翻译:本发明涉及新的细胞生长抑制化合物,其制备方法和含有它们的药物组合物。 更具体地,提供了通式为“IMAGE”/ I /的新化合物,其中R 4是β-羟基和R 3是α-乙基; 或R4是氢,R3是β-乙基; R“是具有1至10个碳原子的直链烷基或具有3至10个碳原子的支链烷基,其中与> Na-CH 2 -O-基团连接的碳原子具有伯或 二级构型或具有3至6个碳原子的烯基或炔基,或在烷基部分具有1至3个碳原子的芳烷基; R1是甲氧基,R2是乙酰基,条件是如果R3是α-乙基和R4β-羟基,R4不是乙基。 这些化合物和N-去甲基-N-(乙氧基甲基) - 长春花碱可以根据本发明通过将通式为“IMAGE”/ II /的化合物的化合物与大量过量的通式R' '-OH [III]含有通式[I]化合物作为活性成分的药物组合物也在本发明的范围内。
摘要:
The invention relates to novel furfuryl derivatives of the general formula (I), ##STR1## wherein R.sub.1 stands for a hydrogen atom or an acetyl group,R.sub.2 stands for a hydroxyl or ethyl group of.beta.-position;R.sub.3 means an ethyl group of .alpha.-position;R.sub.4 represents a hydrogen atom; orR.sub.3 and R.sub.4 together represent an oxygen bridge; andB stands for a hydroxyl of an O-acyl group, as well as their acid addition salts and pharmaceutical preparations containing these compounds. Further on, the invention relates to a process for preparing these compounds and preparations.The compounds of the general formula (I) show a cytostatic activity with less toxicity than that of the commerically available known vinblastine-type bis-indole alkaloid drugs.
摘要:
The invention relates to novel bis-indole derivatives of the general formula (I) ##STR1## wherein R.sub.1 stands for a hydrogen atom or an acetyl group;R.sub.2 stands for a hydrogen atom;R.sub.3 means an ethyl group of .alpha.-position; orR.sub.2 and R.sub.3 together represent an oxygen bridge;R.sub.4 represents an ethyl or hydroxyl group of .beta.-position; andR.sub.5 stands for a hydrogen atom or a hydroxyl group;A represents a C.sub.1-10 straight-chain or C.sub.3-10 branched-chain alkyl group, hydroxy-alkyl, acetyl-alkyl, benzyl, C.sub.3-6 alkenyl or alkynyl or C.sub.5-7 cycloalkyl group or an aromatic group or a heteroaromatic group containing one nitrogen or one oxygen atom, andX stands for oxygen or sulphur atom,as well as their acid addition salts and pharmaceutical preparations containing these compounds.Further on, the invention relates to a process for preparing these compounds and preparations.The compounds of the general formula (I) show a cytostatic activity with less toxicity than that of the known vinblastine-type bis-indole alkaloid drugs which are commercially available.
摘要:
The invention relates to novel nitro derivatives of the general formula (I) ##STR1## wherein R.sub.1 stands for a methyl or a formyl group;R.sub.2 stands for a hydroxy or ethyl group of .beta.-position;R.sub.3 means an ethyl group of .alpha.-position;R.sub.4 represents a hydrogen atom; orR.sub.3 and R.sub.4 together represent an oxygen bridge or a double bond;R.sub.5, R.sub.6 and R.sub.7 stand for a nitro group or hydrogen atom, with the proviso that simultaneously only one of them may stand for hydrogen atom; andY stands for --N.dbd. when R.sub.5 stands for a nitro group; whereasY stands for --NH-- when R.sub.5 stands for a hydrogen atom and a valence bond exists between the C.sub.2, and C.sub.7, atoms,as well as their acid addition salts and pharmaceutical preparations containing these compounds.Further on, the invention relates to a process for preparing these compounds and preparations.The compounds of the general formula (I) show a cytostatic activity with less toxicity than that of the known vinblastine-type bis-indole alkaloid drugs which are commercially available.
摘要:
The invention relates to a new process for the preparation of alkoxyvincaminic acid esters of the formula (I) ##STR1## and/or alkoxyapovincaminic acid esters of the formula (II) ##STR2## wherein R.sup.1, R.sup.2 and R.sup.3 independently stand for alkyl groups having from one to 6 carbon atoms.The compounds of the formulae (I) and (II) are pharmaceutically active, thus some of them show psychostimulant activity.
摘要:
A process is disclosed for the preparation of dimeric alkaloids of formula (II) ##STR1## wherein R stands for methyl or formyl, as well as acid addition salts thereof which comprises oxidizing the vinblastine of formula (III) ##STR2## with chromium (VI) oxide or bichromate or chromic acid alcohol ester in an inert solvent, converting the compound of formula (II), wherein R stands for methyl, so obtained to the acid addition salt and optionally further oxidizing the acid addition salt obtained with an oxidizing agent as defined above and optionally converting the compound of formula (II), wherein R stands for formyl, so obtained to the acid addition salt.
摘要:
The invention relates to new halovincamone derivatives of the general formula (I), ##STR1## wherein R is a C.sub.1-6 alkyl group and X is halogen, and pharmaceutically acceptable acid addition salts and optically active isomers thereof. These compounds possess valuable vasodilating effect, and can be applied to advantage in the therapy.The new compounds defined above are prepared according to the invention so that a single epimer or an epimeric mixture of a racemic or optically active halogenated 14-oxo-15-hydroxy-E-homoeburnane derivative of the general formula (II), ##STR2## wherein R and X are as defined above, or an acid addition salt thereof is treated with an oxidizing agent, and, if desired, the resulting compound of the general formula (I) is converted into its pharmaceutically acceptable acid addition salt and/or resolved.
摘要:
A novel process for preparing 10-bromo-vincaminic acid esters and homologous compounds of the general formula ##STR1## wherein R.sup.1 and R.sup.2 each stand for a C.sub.1-6 alkyl group is disclosed.All the intermediate products are new and exhibit valuable therapeutical effect on the blood circulation.
摘要:
The invention relates to new, racemic or optically active, halogenated 15-hydroxy-E-homoeburnane derivatives of the general formula (Ia) and/or (Ib), ##STR1## wherin R is a C.sub.1-6 alkyl group and X is halogen, and acid addition salts thereof. These compounds are biologically active, furthermore they can be applied as intermediates in the synthesis of other pharmaceutically active substances.The compounds of the general formulae (Ia) and (Ib) are prepared by halogenating the respective racemic or optically active 15-hydroxy-E-homoeburnane derivative of the general formula (II), wherein R is as defined above. ##STR2##
摘要翻译:本发明涉及通式(Ia)和/或(Ib)的新的外消旋或光学活性的卤代的羟基 - 均聚乙二醇衍生物,其中R是 C 1-6烷基,X为卤素,及其酸加成盐。 这些化合物是生物活性的,此外它们可以作为其它药物活性物质合成中的中间体使用。 通式(Ia)和(Ib)的化合物通过卤化通式(II)的各自的外消旋或光学活性的15-羟基-E-高硼烷衍生物而制备,其中R定义如上。 (二)