Patent · US Expired

Bis-indole derivatives and pharmaceutical compositions containing them

US4757077A · kind A · utility

0Cited by
7References
4Claims
0Family size

Assignee

Inventors

Key dates

Filing dateJun 12, 1986
Grant dateJul 12, 1988
Priority date
Expiry dateJun 12, 2006

Classification

  • Technology area (CPC A)Human Necessities
  • CPC primaryA61P35/00
  • WIPO fieldOrganic fine chemistry
  • WIPO sectorChemistry

Abstract

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; PA0 R.sub.2 stands for a hydrogen atom; PA0 R.sub.3 means an ethyl group of .alpha.-position; or PA0 R.sub.2 and R.sub.3 together represent an oxygen bridge; PA0 R.sub.4 represents an ethyl or hydroxyl group of .beta.-position; and PA0 R.sub.5 stands for a hydrogen atom or a hydroxyl group; PA0 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, and PA0 X 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.

Source: USPTO / EPO open patent data. Objective bibliographic and citation counts.