Smithkline Beecham Corporation

Pfizer Corporation

Beecham Group Plc

Peter Robin Shelley

Geoffrey H Baker

Roderick J Dorgan

Rhona Mary Banks

Simon Edward Blanchflower

David Owen Morgan

Mark E Poulton

3-desmethylrapamycin or derivatives thereof, processes for their preparation and their use as antifungal agents and immunosuppressants

Novel compounds of formula (I): ##STR1## wherein R.sup.1 is hydrogen or optionally protected hydroxy; R.sup.2 is alkoxy, optionally protected hydroxy, oxo or optionally O-substituted oximino; R.sup.3 is hydrogen, optionally protected hydroxy,or a group 4'-(.alpha.-L-oleandrosyl)-.alpha.-L-oleandrosyloxy or .alpha.-L-oleandrosyloxy wherein the terminal hydroxy group is optionally protected; R.sup.4, R.sup.5, R.sup.6 and R.sup.7 are the same or different and each is hydrogen or an organic radical; and R.sup.8 is an optionally substituted amino or imino group such as optionally O-substituted oxyimino, optionally N-substituted hydrazone, or optionally N-substituted semicarbazone; are useful in the treatment of helminthiasis in humans and animals.

Anthelmintic milbemycins and avermectins

Rapamycin derivative

Compounds of formula (I): ##STR1## wherein R.sup.1 is hydrogen or optionally protected hydroxy; R.sup.2 is alkoxy, optionally protected hydroxy, oxo or optionally O-substituted oximino; R.sup.3 is hydrogen, optionally protected hydroxy, or a group 4'-(.alpha.-L-oleandrosyl)-.alpha.-L-oleandrosyloxy or .alpha.-L-oleandrosyloxy wherein the terminal hydroxy group is optionally protected; one or R.sup.4 and R.sup.5 is hydrogen and the other is methyl; and one of R.sup.6 and R.sup.7 is hydrogen and the other is methyl; with the proviso that (a) when R.sup.1 is optionally protected hydroxy, R.sup.3 is hydrogen, and (b) when R.sup.2 is not methoxy or optionally protected hydroxy, R.sup.1 and R.sup.3 are both hydrogen, are new and useful as anthelmintic agents.

Derivatives of avermectin and milbemycin

Growing community of inventors

Betchworth, United Kingdom

Peter Robin Shelley