Beecham Group Plc

Pfizer Corporation

Geoffrey H Baker

Merle Beal

Roderick J Dorgan

Rhona Mary Banks

Mark E Poulton

Peter Robin Shelley

David Owen Morgan

Simon Edward Blanchflower

Lee James Beeley

Peter M Newsome

Stephen F Moss

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

Crystalline calcium pseudomonate or a hydrate thereof, in particular the dihydrate. Processes for the preparation of these salts and their use in human and veterinary medicine and as a growth promoter in animals are described.

Method for improving weight gain and feed utilization in livestock

Compounds of formula (I): ##STR1## wherein R.sup.1 is hydrogen or methyl, R.sup.2 is hydrogen or (E)-2-methyl 2-butenoyloxy, and R.sup.3 is hydrogen or hydroxy, with the proviso that when R.sup.3 is hydrogen, R.sup.1 and R.sup.2 are both hydrogen, and when R.sup.2 is (E)-2-methyl 2-butenoyloxy, R.sup.1 is methyl; the compound of formula (II): ##STR2## and the compound of formula (III): ##STR3## are obtainable by the fermentation of Streptomyces E225 NCIB 12310 or Streptomyces E225B NCIB 12509. The compounds have anthelmintic utility.

Parasiticidal milbemycin derivatives

Compounds of formula (I): ##STR1## wherein R.sup.1 is hydrogen or methyl, R.sup.2 is hydrogen or (E)-2-methyl 2-butenoyloxy, and R.sup.3 is hydrogen or hydroxy, with the proviso that when R.sup.3 is hydrogen, R.sup.1 and R.sup.2 are both hydrogen, and when R.sup.2 is (E)-2-methyl 2-butenoyloxy, R.sup.1 is methyl; the compound of formula (II): ##STR2## and the compound of formula (III): ##STR3## are obtainable by the fermentation of Streptomyces E225 NCIB 12310 or Streptomyces E225B NCIB 12509. The compounds have antihelminthic utility.

Process for producing parasiticidal milbemycin derivatives by culturing

Compounds

Processes for the preparation of these salts and their use in human and veterinary medicine and as a growth promoter in animals are described.

Process for preparing crystalline calcium pseudomonate

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

Crystalline calcium pseudomonate

A compound of formula (I): ##STR1## or a salt thereof wherein R.sup.1 is halogen, C.sub.1-4 alkyl or C.sub.1-4 alkoxy

Growing community of inventors

Banstead, United Kingdom

Geoffrey H Baker