Novartis Ag

Sandoz Gmbh

Gerhard Emmer

Hans Tscherter

Maximilian Grassberger

Michael Morris Dreyfuss

Karl Baumann

Klaus Ruedi

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.

Heteroatoms-containing tricyclic compounds

Pipecolic acid-containing peptolides wherein the peptidic backbone is of at least 9 .alpha.-amino acid residues joined together by peptide bonds, particularly the compounds of formula I ##STR1## wherein the substituents have various significances, are disclosed. They can be prepared by isolation or derivation from an appropriate microorganism strain such as S 42508/F (NRRL 15761). They have interesting pharmacological, e.g. antifungal, chemotherapeutic drug resistance reversing and to some extent immunosuppressant and antiinflammatory properties.

Pipecolic acid-containing peptolides, their preparation and

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Vienna, Austria

Gerhard Emmer