Nitro derivatives of vinblastine-type bisindoles, and pharmaceutical compositions containing them
US4746665A · kind A · utility
Assignee
Inventors
Key dates
| Filing date | Jun 12, 1986 |
| Grant date | May 24, 1988 |
| Priority date | — |
| Expiry date | Jun 12, 2006 |
Classification
- Technology area (CPC A)Human Necessities
- CPC primaryA61P35/00
- WIPO fieldOrganic fine chemistry
- WIPO sectorChemistry
Abstract
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; PA0 R.sub.2 stands for a hydroxy or ethyl group of .beta.-position; PA0 R.sub.3 means an ethyl group of .alpha.-position; PA0 R.sub.4 represents a hydrogen atom; or PA0 R.sub.3 and R.sub.4 together represent an oxygen bridge or a double bond; PA0 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; and PA0 Y stands for --N.dbd. when R.sub.5 stands for a nitro group; whereas PA0 Y 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.
Source: USPTO / EPO open patent data. Objective bibliographic and citation counts.