Fisons Ltd.

Discoverybiomed, Inc.

Astra Pharmaceuticals Limited

John Dixon

Francis Ince

Erik Schwiebert

John Streiff

Hongwu Gao

Roger C Brown

Brian Springthorpe

Roger Victor Bonnert

David R Cheshire

Alan C Tinker

Richard A Appleton

Andrew J Baxter

Thomas McInally

John R Bantick

David N Hardern

Sidney C Burford

David H Robinson

Kenneth J Gould

Rodney A Brown

David J Wilkinson

Joseph P Ritchie

John B Farmer

Eric C Seales

Deborah Mai

Coumarin derivative compounds and methods for the treatment of hyperproliferative diseases, such as cancer, polycystic kidney disease, and fibrosis of different tissues (e.g., idiopathic pulmonary fibrosis), are provided. The methods include administering to a subject a compound as described herein. Also provided are methods for inhibiting the interaction between two or more heat shock protein chaperones in a cell.

Coumarin derivatives and methods of use in treating hyperproliferative diseases

Novel CFTR corrector compounds that are effective in rescuing halide efflux, delF508-CFTR protein processing, and apical functional chloride ion transport in a cell are provided. Also provided are methods for treating protein folding disorders (e.g., cystic fibrosis and chronic obstructive pulmonary diseases). The methods include administering a CFTR corrector compound or pharmaceutically acceptable salt or prodrug thereof. Methods of rescuing halide efflux in a cell, correcting a processing defect of a delF508-CFTR protein in a cell, and correcting functional delF508-CFTR chloride channels in a cell are also provided.

Coumarin derivatives and methods of use in treating cystic fibrosis, chronic obstructive pulmonary disease, and misfolded protein disorders

Novel CFTR corrector compounds that are effective in rescuing halide efflux, delF508-CFTR protein processing, and apical functional chloride ion transport in a cell are provided. Also provided are methods for treating protein folding disorders (e.g., cystic fibrosis). The methods include administering a CFTR corrector compound or pharmaceutically acceptable salt or prodrug thereof. Methods of rescuing halide efflux in a cell, correcting a processing defect of a delF508-CFTR protein in a cell, and correcting functional delF508-CFTR chloride channels in a cell are also provided.

Small molecule CFTR correctors

Small molecule bicyclic and tricyclic CFTR correctors

There are disclosed compounds of formula I,

7-(2-aminoethyl) benzothiazolones

There are disclosed compounds of the formula (I): ##STR1## in which the variables R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5, R.sub.6, and X are defined in the specification. The compounds are useful as pharmaceuticals, especially as anti-inflammatory agents.

Anti-inflammatory 4-aminophenyl derivatives

Phenylethylamine derivatives of the formula ##STR1## wherein D.sub.1 represents a phenylethyl radical which is substituted with hydroxy and/or alkyl groups,

Phenylethylamine derivatives and pharmaceutical use

Compounds of the formula, ##STR1## in which one of R.sub.30 and R.sub.40 represents a substituted phenylalkyl group and the other of R.sub.30 and R.sub.40 represents hydrogen or halogen, and R.sub.50 and R.sub.60 each independently represent hydrogen or alkyl. The compounds of the invention are useful for the treatment or prophylaxis of renal failure or cardiovascular disease.

Substituted 3,4-dihydroxy phenylethylamino compounds

There are described compounds of formula I, ##STR1## in which Y is S, O or NR.sub.9,

1,3,4-thiadiazoles

Novel compounds of the formula ##STR1## in which one of R.sub.30 and R.sub.40 represents a substituted phenylalkyl group,

##STR1## Compounds of formula (I), in which Z represent O, S, SO.sub.2, CO, NR or a single bond, G represents a one or two ring, saturated or unsaturated carbocyclic or heterocyclic group optionally substituted by phenyl thrihalomethyl or at least groups selected from alkoxy C1 to 6 or halogen atoms, provided that when Z represents a single bond G does not represent phenyl, R represents hydrogen or alkyl C1-6, m and n each independently represent 2, 3 or 4, and q represents an integer from 1 to 3 inclusive, and pharmaceutically acceptable derivatives thereof. There are also described processes for producing the compounds and pharmaceutical, e.g. cardiac, compositions containing them.

Aromatic amines

Novel 3,4-dihydroxyphenylethylamine derivatives possess dopaminergic activity in animals and are therefore useful in the treatment of iner alia congestive heart failure, renal failure and reversible obstructive airways disease. The compounds are generally administered in the form of a pharmaceutical composition comprising the active ingredient in admixture with a pharmaceutically acceptable adjuvant, diluent or carrier.

3,4-Dihydroxyphenylethylamine derivatives and their use

There are described compounds of formula I, ##STR1## in which X represents a C2 to 8 alkylene chain optionally interrupted by a double bond or by S(O).sub.n, wherein n is 0, 1 or 2;

Aromatic compounds

There are provided compounds of formula I, ##STR1## and pharmaceutically acceptable derivatives thereof. There are also described the use of the compounds of formula I as pharmaceuticals, methods for making the compounds and pharmaceutical, e.g. cardiac, compositions containing the compounds.

Growing community of inventors

Great Dalby, United Kingdom

John Dixon