Pfizer Corporation

Graham Lunn

Bernard Joseph Banks

Stephen Paul Gibson

Lee Richard Roberts

Alan John Pettman

Michael Stephen Pacey

Robert James Crook

Mark A Haxell

Alan Daniel Brown

Mark Edward Bunnage

John Paul Mathias

Paul Alan Glossop

David Anthony Price

Kim James

Charlotte Alice Louise Lane

Russell Andrew Lewthwaite

Nigel D Walshe

Douglas James Critcher

James John Eshelby

Nathan Anthony Chubb

Ross Sinclair Strang

Paul H Wiedenau

David H Williams

Andrew J Rudge

David Howard Williams

Andrew John Rudge

Nigel Derek Walshe

Paul Heinrich Wiedenau

The invention relates to compounds of formula (1) and to processes for the preparation of, intermediates used in the preparation of, compositions containing and the uses of, such derivatives. The compounds according to the present invention are useful in numerous diseases, disorders and conditions, in particular inflammatory, allergic and respiratory diseases, disorders and conditions.

Compounds useful for the treatment of diseases

The present invention relates to tetrahydronaphthyridine derivatives of the general formula (I): or of the general formula (I') in which A and Rare as defined within, and to processes for the preparation of, intermediates used in the preparation of, compositions containing and the uses of, including the treatment diseases mediated by H3 ligands, in particular inflammatory, allergic and respiratory diseases, disorders and conditions.

Tetrahydronaphthyridine derivatives

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

The invention described herein relates to: the use of an effective inhibitor of a bacterial &#x3b1;-amylase and/or &#x3b1;-glucosidase in the manufacture of a composition for the treatment of acidosis; a method of treatment of rumen acidosis which comprises administration of an effective amount of an effective inhibitor of a bacterial &#x3b1;-amylase and/or &#x3b1;-glucosidase to a ruminant; a formulation suitable for the treatment of acidosis in an animal which comprises an effective inhibitor of a bacterial &#x3b1;-amylase and/or &#x3b1;-glucosidase in admixture with a suitable excipient, diluent or carrier selected with regard to the intended route of administration and standard pharmaceutical/veterinary/farming practice; screening methods useful in the identification of a suitable inhibitor of a bacterial &#x3b1;-amylase and/or &#x3b1;-glucosidase for the treatment of acidosis in a ruminant; a process for improving ruminant milk quality and/or quantity which comprises treatment of a ruminant with an effective amount of an inhibitor of bacterial &#x3b1;-amylase and/or &#x3b1;-glucosidase; a compound of the formula I: or veterinarily acceptable salt, solvate (including hydrate) or prodrug thereof; and processes to make an effective inhibitor of a bacterial &#x3b1;-amylase and/or &#x3b1;-glucosidase useful for the treatment of acidosis in a ruminant.

Treatment of rumen acidosis with &#x3b1;-amylase inhibitors

Compounds of formula (I), their salts and prodrugs thereof, where the substituents are as defined herein are disclosed as opiate binding agents useful in the treatment of opiate-mediated conditions. Also described are processes for making such substances. 

3-azabicyclo[3.1.0]hexane derivatives useful in therapy

The invention described herein relates to: the use of an effective inhibitor of a bacterial &#x3b1;-amylase and/or &#x3b1;-glucosidase in the manufacture of a composition for the treatment of rumen acidosis; a method of treatment of rumen acidosis which comprises administration of an effective amount of an effective inhibitor of a bacterial &#x3b1;-amylase and/or &#x3b1;-glucosidase to a ruminant; a formulation suitable for the treatment of rumen acidosis in an animal which comprises an effective inhibitor of a bacterial &#x3b1;-amylase and/or &#x3b1;-glucosidase in admixture with a suitable excipient, diluent or carrier selected with regard to the intended route of administration and standard pharmaceutical/veterinary/farming practice; screening methods useful in the identification of a suitable inhibitor of a bacterial &#x3b1;-amylase and/or &#x3b1;-glucosidase for the treatment of acidosis in a ruminant; a process for improving ruminant milk quality and/or quantity which comprises treatment of a ruminant with an effective amount of an inhibitor of bacterial &#x3b1;-amylase and/or &#x3b1;-glucosidase; a compound of the formula I:or veterinarily acceptable salt, solvate (including hydrate) or prodrug thereof; and processes to make an effective inhibitor of a bacterial &#x3b1;-amylase and/or &#x3b1;-glucosidase useful for the treatment of acidosis in a ruminant.

Compounds of formula (I), their salts and prodrugs thereof, where the substituents are as defined herein are disclosed as opiate binding agents useful in the treatment of opiate-mediated conditions. Also described are processes for making such substances.

3-Azabicyclo&lsqb;3.1.0&rsqb;hexane derivatives useful in therapy

Growing community of inventors

Sandwich, United Kingdom

Graham Lunn