Rhone Poulenc Rorer

Aventis Pharma Limited

May & Baker, Ltd.

Aventis Pharmaceuticals Inc.

Iain M McLay

Frank Halley

Roger J Walsh

Barry Porter

Neil Victor Harris

Peter Charles Astles

Clive McCarthy

Christopher Smith

Andrew David Morley

Andrew James Ratcliffe

Terance W Hart

Malcolm N Palfreyman

David C Cook

Andrew Paul Van Sickle

Paul L Bamborough

Richard A Lewis

David J Lythgoe

Jeffrey M McKenna

Andrew Bridge

Paul A Wallace

Tahir Majid

Alan Collis

Martyn Foster

Alan Roach

Michael L Edwards

Jean-Claude Aloup

Tahir Nadeem Majid

Stephanie Deprets

Paul Joseph Cox

David John Aldous

Bernard Baudoin

Shelley Amendola

Brian L Pedgrift

Christopher D Edlin

Alan John Collis

Mark Francis Harper

Roger John Aitchison Walsh

Richard Alan Lewis

Compounds of formula (I) are described in which Het is a five or six membered heteroaromatic ring of the formula in which one of Rand Ris optionally substituted heteroaryl and the other is optionally substituted heteroaryl or optionally substituted aryl; Xis a bond, Xand Xare each independently N or C and Xand Xare independently CH, N, NH, O or S; or Xand Xare C, one of X, Xand Xis N and the others are N or CH; but excluding compounds in which Xis a bond, one of Xand Xis N and the other is NH and Xand Xare both C; Rrepresents a group -L-R; Rrepresents hydrogen, alkyl or hydroxyalkyl; or Rand R, when attached to the same carbon atom, may form with the said carbon atom a cycloalkyl, cycloalkenyl or heterocycloalkyl ring or a group C&#x2550;CH; Rrepresents hydrogen or alkyl; and m is zero or an integer 1 or 2; and N-oxides thereof, and their prodrugs; and pharmaceutically acceptable salts and solvates of compounds of formula (I) and N-oxides thereof, and their prodrugs. The compounds are TNF inhibitors and are useful as pharmaceuticals. 

Heteroaryl-cyclic acetals

Compounds of the formula and N-oxides, prodrugs, acid bioisosteres, pharmaceutically acceptable salts or solvates of such compounds, or N-oxides, prodrugs, or acid bioisosteres of such salts or solvates, to compositions comprising such compounds, and methods of treatment comprising administering, to a patient in need thereof, such compounds and compositions.

Pyrrolopyrimidines

Compounds of the following backbone structure:which are useful as Tumor necrosis factor (TNF) inhibitors in treating disease related to elevated TNF.

Imidazolyl-cyclic acetals

Substituted phenyl compounds

This invention is directed to compounds of formula I ##STR1## wherein R.sup.1 is CN, CH.sub.2 CN, CH.dbd.CHCN, CHO, or CH.dbd.CHCO.sub.2 H;

Substituted phenyl compounds with a substituent having a thienyl ring

Substituted phenyl compounds with a substituent having A

Oxathiane derivatives

Therapeutically useful thioformamide derivatives of the formula: ##STR1## wherein R represents alkyl, Ar represents optionally substituted phenyl group, Y represents ethylene, methylene or a valency bond, and X represents carbonyl, hydroxymethylene, &gt;C.dbd.NOR.sup.1, &gt;C.dbd.NN(R.sup.1).sub.2 or &gt;C.dbd.NN(R.sup.1)CON(R.sup.1).sub.2 in which R.sup.1 represents hydrogen or optionally substituted alkyl, benzyl, phenethyl, 1-naphthylmethyl, 2-naphthylmethyl or pyrid-3-ylmethyl or two R.sup.1 substituents on the same nitrogen atom may together form optionally substituted alkylene, and salts thereof, processes for their preparation and compositions containing them are described.

Thioformamide derivatives

This invention relates to thioformamide derivatives of the formula: ##STR1## wherein R represents alkyl, Ar represents optionally substituted phenyl, Y represents an ethylene or methylene radical or a valency bond, and n represents 0 or 1, bioprecursors thereof and pharmaceutically acceptable salts thereof which possess useful pharmacological properties, processes for their preparation and compositions containing them.

Growing community of inventors

Loughton, United Kingdom

Iain M McLay