Heteroatoms-containing tricyclic compounds
AssigneeSandoz Ltd.
InventorsKarl Baumann, Gerhart Emmer
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Abstract
The invention concerns the compounds of formula I ##STR1## wherein the substituents have various significances. They are prepared by several processes including epimerizing replacement, treatment with cyanogen bromide or thiophosgene, treatment with an acid having a non-nucleophilic anion, treatment with dimethylsulfoxide and acetic anhydride, acylation, treatment with an oxalyl derivative and ammonia, methylation, oxidation, deprotection and protection. They possess interesting pharmacological activity as antiinflammatory, immunosuppressant, antiproliferative and chemotherapeutic drug resistance reversing agents.
Claims13
A compound of formula ##STR10## wherein R.sub.1 is a group (d) of formula ##STR11## R.sub.2 is oxo and there is a single bond n 23,24 position;
- hydroxy or hydroxy protected by a hydroxy protecting group selected from formyl, tert-butoxycarbonyl, and trialkylsilyl and there is a single or a double bond in 23,24 position;
- or absent and there is a double bond in 23,24 position;
- and
- R.sub.4 is hydroxy and there is a single bond in 10,11 position;
- R.sub.3 is methyl, ethyl, n-propyl, or allyl;
- in free form or, where such forms exist, in salt form.
A compound of formula I ##STR12## wherein R.sub.1 is a group (b) ##STR13## wherein R.sub.6 is hydroxy or methoxy;
- R.sub.2 is oxo and there is a single bond in 23,24 position;
- hydroxy or hydroxy protected by a hydroxy protecting group selected from formyl, tert-butoxycarbonyl, and trialkylsilyl and there is a single or a double bond 23,24 position;
- or absent and there is a double bond in 23,24 position;
- R.sub.4 is hydroxy and there is a single bond in 10,11 position;
- and
- R.sub.3 is methyl, ethyl, n-propyl, or allyl;
- in free form or, where such forms exist, in salt form.
Dependencies are inferred from the claim text.