Imperial Chemical Industries Limited

Zeneca Limited

Astrazeneca Ab

Astra Zeneca U.k. Limited

David R Brittain

Robin Wood

John Preston

Jeffrey James Morris

Jethro L Longridge

Anthony L Cooper

Steven P Brown

Linda Slater

Edward D Brown

Walter Hepworth

Gilbert J Stacey

George R Brown

Craig Johnstone

Paul Robert Whittamore

Ronald Platt

Geoffrey R Bedford

Michael S Large

Gareth Morse Davies

Kevin Michael Foote

Keith Blakeney Mallion

David J Brown

Michael Howard Block

Craig Samuel Donald

Michael T Cox

Linda Salter

Compounds of formula (I):wherein: Processes for their preparation and their use in the treatment of disorders mediated by the neuropeptide Y5 receptor in a warm-blooded animal, such as a human being are also described.

Amino substituted dibenzothiophene derivatives for the treatment of disorders mediated by NP Y5 receptor

Chemical compounds

Substituted urea derivatives as cell adhesion inhibitors

Heterocyclic derivatives

Quinuclidine derivatives as squalene synthase inhibitors

The invention concerns novel N-phenylacetyl and related acyl derivatives of (4-amino-2,6-dimethylphenylsulphonyl)nitromethane and pharmaceutically acceptable salts thereof which are inhibitors of the enzyme aldose reductase and are of value, for example, in the treatment of certain peripheral effects of diabetes and galactosemia. Also disclosed are pharmaceutical compositions containing one of the derivatives and processes for the manufacture and use of the derivatives.

Acetamide derivatives

The invention concerns novel phenoxy- and phenylthio-acetyl derivatives of (4-amino-2,6-dimethylphenylsulphonyl)nitromethane and pharmaceutically acceptable salts thereof which are inhibitors of the enzyme aldose reductase and are of value, for example, in the treatment of certain peripheral effects of diabetes and galactosemia. Also disclosed are pharmaceutical compositions containing one of the derivatives and processes for the manufacture and use of the derivatives.

Amidobenzene derivatives, compositions and use

The invention concerns novel (oxamido- and ureido-phenylsulfonyl)nitromethane derivatives and pharmaceutically acceptable salts thereof which are inhibitors of the enzyme aldose reductase and are of value, for example, in the treatment of certain peripheral effects of diabetes and galactosemia. Also disclosed are pharmaceutical compositions containing one of the derivatives and processes for the manufacture and use of the derivatives.

Urea derivatives, compositions and use

The invention concerns novel, pharmaceutically useful, benzheterocyclyl sulphones of the formula I: ##STR1## in which ring A may bear optional halogeno, (1-4C)alkyl or fluoro(1-4C)alkyl substituents; X is oxygen, or a group of the formula --S(O).sub.n -- or --NR.sup.1 -- in which n is zero, 1 or 2 and R.sup.1 is hydrogen, (1-4C)alkyl, (1-6C)alkanoyl, benzoyl or phenyl(1-4C)alkyl, the last two optionally substituted; Y is various linking groups defined hereinafter, such as ethylene or trimethylene; and in which the group --SO.sub.2 CH.sub.2 NO.sub.2 is located at position a, b or c in ring A; together with the non-toxic thereof. Other aspects of the invention include the production of the novel compounds by analogy processes and pharmaceutical compositions of the novel compounds for use in the treatment of diabetic complications.

Benzheterocyclyl sulphones

Amide derivatives, compositions and use

The invention concerns a novel process for the racemization of unwanted enantiomeric forms of 1'-substituted spiro[imidazolidine-4,3'-indoline]-2,2',5-triones and 1'-substituted spiro[pyrrolidine-3,3'-indoline]-2,2',5-triones which comprises heating an unwanted enantiomeric form (or a mixture containing an excess of one enantiomer over the other) alone or, more conveniently, in the presence of a solvent or diluent at a temperature in the range 80.degree. to 280.degree. C.

Process for resolving certain spiro compounds

The invention concerns 1'-(4-bromo-2-fluorobenzyl)-7'-chloro-spiro[imidazolidine-4,3'-indoline]-2 ,2',5-trione in racemic or dextrorotatory form; pharmaceutical compositions thereof for use in the treatment or prophylaxis of certain complications of diabetes; and processes for its manufacture.

Aldose reductase inhibition by spiro indoline derivatives

The invention concerns a novel process for the racemisation of unwanted enantiomeric forms of 1'-substituted spiro[imidazolidine-4,3'-indoline]-2,2',5-triones and 1'-substituted spiro[pyrrolidine-3,3'-indoline]-2,2',5-triones which comprises heating an unwanted enantiomeric form (or a mixture containing an excess of one enantiomer over the other) alone or, more conveniently, in the presence of a solvent or diluent at a temperature in the range 80.degree. to 280.degree. C.

Process for racemizing certain spiro compounds

The invention provides novel spiro[oxazolidine-5,3'-indoline]-2,2',4-triones of formula I bearing substituted benzyl or cinnamyl on the indoline nitrogen, together with salts and non-toxic, biodegradable precursors thereof. The compounds are potent inhibitors of the enzyme aldose reductase and are useful in treating or preventing certain diabetic complications. The invention also provides pharmaceutical compositions containing, and processes for the manufacture of, the compounds of formula I and their salts and derivatives.

1'-Substituted-spiro[oxazolidine-5-3'-indoline]-2,2', 4-trione

Growing community of inventors

Macclesfield, United Kingdom

David R Brittain