Pfizer Corporation

Pifzer, Inc.

Nigel D Walshe

Alexander C Goudie

Stephen Paul Gibson

Christopher J Dutton

Douglas James Critcher

Graham Lunn

James John Eshelby

Nathan Anthony Chubb

Andrew J Rudge

Selena J Cambers

Paul H Wiedenau

David H Williams

The present invention relates to novel terpene alkaloids and their use as antiparasitic agents. The present invention also relates to an antiparasitic agent which comprises a terpene alkaloid compound of this invention as an effective ingredient in an antiparasitic formulation. More particularly, the present invention relates to derivatives of the terpene alkaloid (1S,2R,4aS,5R,8R,8aR)-2-(acetyloxy)-8a-hydroxy-3,8-dimethyl-5-(1-methylethenyl)-1,2,4a,5,6,7,8,8a-octahydronaphthalen-1-yl (2S,3aR,9bR)-6-chloro-9b-hydroxy-5-methyl-1,2,3,3a,5,9b-hexahydropyrrolo[2,3-c][2,1]benzoxazine-2-carboxylate. Pharmaceutical compositions comprising the same are also disclosed.

Antiparasitic terpene alkaloids

An improved process for the preparation of the antiparasitic compound 25-cyclohexyl-22,23-dihydro-5-hydroxyiminoavermectin B1 monosaccharide from doramectine and intermediates therefor and crystalline solvates thereof.

Process for antiparasitic agent

Antiparasitic agents

Antiparasitic compounds of formula (I): ##STR1## The broken line at the 22-23 position representing an optional double bond and either R.sup.1 is H or OH and the double bond is absent or the double bond is present and R.sup.1 is absent; R.sup.2 is optionally substituted phenyl, or a group of formula (II): ##STR2## wherein X is O, S or --CH.sub.2 --, abc and d are 0-2 and a+b+c+d.ltoreq.5 R.sup.3 is H or Me

Method for making antiparasitic agents

A new acidic polycyclic antibiotic UK-61,689 has the formula: ##STR1## or a pharmaceutically acceptable cationic salt thereof. The antibiotic and its cationic salts are active against a variety of microorganisms and are effective in controlling coccidiosis, enteritis and swine dysentery as well as being effective in promotion of growth and/or improving efficiency of feed utilization in swine and ruminants.

Process for producing polycyclic ether antibiotics

Antiparasitic compounds of formula (I): ##STR1## The broken line at the 22-23 position representing an optional double bond and either R.sup.1 is H or OH and the double bond is absent or the double bond is present and R.sup.1 is absent; R.sup.2 is optionally substituted phenyl, or a group of formula (II): ##STR2## wherein X is O, S or --CH.sub.2 13 , abc and d are 0-2 and a+b+c+d.ltoreq.5

Antiparastic agents

Polycyclic ether antibiotic

Antiparasitic compound of formula (I): ##STR1## The broken line at the 22-23 position representing an optional double bond and either

A new acidic polycyclic antibiotic UK-61,689 has the formula: ##STR1## or a pharmaceutically acceptable cationic salt thereof. The antiobiotic and its cationic salts are active against a variety of microorganisms and are effective in controlling coccidiosis, enteritis and swine dysentery as well as being effective in promotion of growth and/or improving efficiency of feed utilization in swine and ruminants.

Growing community of inventors

Deal, United Kingdom

Nigel D Walshe