Glaxo Group Limited

Glaxo Wellcome Inc.

Biota Scientific Management Pty Ltd

Allen Hanburys Limited

Michael D Dowle

Harry Finch

Ian H Coates

David E Bays

David Middlemiss

Colin F Webb

Barry C Ross

David I Scopes

Martin Redpath Johnson

Kevin S Cardwell

Torquil I Jack

Duncan B Judd

Lee Andrew Harrison

Pritom Shah

Alexander W Oxford

Simon John Fawcett MacDonald

Keith Mills

Colin David Eldred

Brian Evans

Stephen Paul Watson

Graham George Adam Inglis

Darko Butina

John G Montana

Robin Andrew Smith

Graham George Inglis

Simon John MacDonald

Alan Naylor

Diane Mary Coe

John W Clitherow

John Bradshaw

Julie Nicole Hamblin

Lawrence H Lunts

Barry J Price

Paul Spencer Jones

Darryl McConnell

Charlotte Jane Mitchell

Anthony William James Cooper

Mika Lindvall

Betty Jin

Roger Hayes

Wen-Yang Wu

Alison Judith Redgrave

David George Allen

Caroline Mary Cook

Simon J F MacDonald

Stephen E Shanahan

Christopher David Edlin

Van T T Nguyen

Andrew McM Mason

Martin Pass

Peter Clark

The invention relates to a compound of formula (I) or a salt thereof: wherein: Ris Calkyl, Cfluoroalkyl or &#x2014;(CH)OH; Ris a hydrogen atom (H), methyl or Cfluoroalkyl; Ris a hydrogen atom (H) or Calkyl; Ris optionally substituted branched Calkyl, optionally substituted Ccycloalkyl, optionally substituted mono-unsaturated-Ccycloalkenyl, optionally substituted phenyl, or an optionally substituted heterocyclic group of sub-formula (aa), (bb) or (cc): in which nand nindependently are 1 or 2; and Y is O, S, SO, or NR; and wherein Het is of sub-formula (i), (ii), (iii), (iv) or (v): The compounds are phosphodiesterase (PDE) inhibitors, in particular PDE4 inhibitors. Also provided is the use of a compound of formula (I), or a pharmaceutically acceptable salt thereof, in the manufacture of a medicament for the treatment and/or prophylaxis of an inflammatory and/or allergic disease in a mammal such as a human, for example chronic obstructive pulmonary disease (COPD), asthma, or allergic rhinitis.

Pyrazolo[3,4-B]pyridine compounds, and their use as phosphodiesterase inhibitors

The invention relates to compounds of general formula (I); in which R is an amino or guanidino group; Ris acetyl or trifluoroacetyl; X is CONH, SONH, NHCO or NHCONH; m is either 0 or 1; n is an integer from 2 to 6; q is an integer from 0 to 3; and Y is hydrogen or an aromatic substituent, or a pharmaceutically acceptable derivative thereof; methods for their preparation, pharmaceutical formulations containing them or their use in the prevention or treatment of a viral infection 

Dimeric compounds and their use as anti-viral agents

According to the invention are provided compounds of formula (I) (relative stereochemistry indicated) wherein R,, R,and R,are as defined in the specification. Compounds of formula (I) are useful inter alia in the treatment of inflammatory diseases of the respiratory tract.

Pyrrolopyrrolone derivatives as inhibitors of neutrophil elastase

There are described according to the invention, processes for making compounds of formula (XXVIII),(relative stereochemistry indicated), wherein P,is as defined in the specification.

According to the invention there are provided Hexahydro-Pyrrolo&lsqb;3,4-b&rsqb;pyrrol-2-one compounds of formula (1), (relative stereochemistry indicated), wherein R,, R,and R,are as defined in the specification. Compounds of formula (1) are useful inter alia in the treatment or chronic bronchitis.

Pyrrolopyrrolone derivatives

There are described according to the invention, compounds of formula (XXII).sup.a (relative stereochemistry indicated), wherein R.sub.2 is as defined in the specification. Compounds of formula (XXII).sup.a are useful as intermediates in the production of pharmaceuticals useful in the treatment of chronic bronchitis. ##STR1##

The invention provides compounds of formula (I): ##STR1## or a physiologically acceptable salt, solvate or metabolically labile ester thereof wherein the R groups are defined in the specification. The compounds may be used in the treatment or prophylaxis of hypertension and diseases associated with cognitive disorders.

Benzofuran derivatives

The invention provides compounds of the general formula (I) ##STR1## and physiologically acceptable salts, solvates or non-toxic metabolically labile esters thereof where R.sup.1 represents a halogen atom; Ar represents the group ##STR2## R.sup.3 represents a C-linked tetrazolyl group; R.sup.4 and R.sup.5, which may be the same or different, each independently represent a hydrogen atom or a halogen atom or a C.sub.1-6 alkyl group; and

The invention provides compounds of formula (I): ##STR1## or a physiologically acceptable salt, solvate or metabolically labile ester thereof wherein

The invention provides compounds of formula (I): ##STR1## or a physiologically acceptable salt, solvate or metabolically labile ester thereof. The compounds may be used in the treatment or prophylaxis of hypertension and diseases associated with cognitive disorders.

Pyrazole containing benzofuran derivatives and pharmaceutical

The invention provides compounds of the general formula (I) ##STR1## and physiologically acceptable acid addition salts, metabolically labile esters and solvates thereof in which

Amine derivatives

Indole derivatives are disclosed of the general formula (I): ##STR1## wherein R.sub.1 is hydrogen, C.sub.1-6 alkyl or C.sub.3-6 alkenyl; R.sub.2 is a hydrogen, C.sub.1-3 alkyl, C.sub.3-6 alkenyl, phenyl, phen(C.sub.1-4)alkyl or C.sub.5-7 cycloalkyl; R.sub.3 and R.sub.4 are hydrogen, C.sub.1-3 alkyl or propenyl groups or together form an aralkylidene group; Alk is C.sub.2 -C.sub.3 alkylene chain and A is C.sub.2 -C.sub.5 alkylene chain and its physiologically acceptable salts and solvates. The compounds may be prepared, for example, by cyclization of a compound of general formula (II): ##STR2## where Q is the group NR.sub.3 R.sub.4 or a protected derivative thereof or a leaving group and R.sub.1 l, R.sub.2, R.sub.3, R.sub.4, A and Alk are as defined for formula (I). The compounds have a selective vosoconstrictor action and are useful in treating pain such as migraine. The compounds may be formulated as pharmaceutical compositions in conventional manner, preferably for oral administration.

5-substituted-3-aminoalkyl indole derivatives for migraine

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Ware, United Kingdom

Michael D Dowle