Heteroatoms-containing tricyclic compounds

C - Chemistry – Metallurgy – 07 – H

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C07H 17/00 (2006.01) A61K 31/70 (2006.01) C07H 19/01 (2006.01) C07H 23/00 (2006.01)

Patent

CA 2045989

900-9632 A B S T R A C T: HETEROATOMS-CONTAINING TRICYCLIC COMPOUNDS The invention relates to the field of macrolides. It concerns 12-(2'-cyclopentylvinyl)-11,28-dioxa-4-azatricyclo[22.3.1.04,9]octacos- 18-ene or -14,18-diene and 11-(2'-cyclopentylvinyl)-10,27-dioxa- 4-azatricyclo[21.3.1.04,8]heptacos-17-ene or -13,17-diene derivatives, in particular the compounds of formula I Image I wherein the substituents have various significances. They are prepared by a process comprising ring contraction accompanied by appropriate derivatization. They possess interesting pharmacological activity as immunosuppressant and antiproliferative, antiinflammatory, and chemotherapeutic drug resistance reversing agents.

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