Glaxo Group Limited

Martin Pass

Michael D Dowle

Duncan B Judd

Vipulkumar Kantibhai Patel

David Middlemiss

Barry C Ross

Nigel Stephen Watson

David I Scopes

Kevin S Cardwell

Torquil I Jack

John G Montana

The invention relates to a novel class of amide derivatives which act as thrombin inhibitors as described by formula (I), where R,and R,, independently represent a group (a) or R,and R,together form a C,heterocycloalkyl or heterocycloalkenyl group which may be optionally substituted by C,alkyl, C,alkoxy, halogen, carboxylic acid or a C,carboxylic acid ester group; R,represents hydrogen, C,alkyl, halogen, or C,alkoxy; R,, R,and R,independently represent hydrogen, or halogen; R,represents hydrogen or C,alkyl; R,represents hydrogen, C,cycloalkyl, C,cycloalkenyl, C,heterocycloalkyl, C,heterocycloalkenyl, aryl or heteroaryl, which groups are optionally substituted by one or more groups selected from halogen, hydroxy, CN, C,alkyl, C,alkoxy, C,acyloxy, NR,R,, NHCOR,, NHSO,R,, COR,, CO,R,, CONR,R,, and SO,NHR,; X represents a bond, a C,alkyl chain, or a C,alkenyl chain, where one or two nitrogen, oxygen, or sulfur atoms may be optionally contained within each chain, and the chains are optionally substituted by one or more groups selected from halogen, hydroxy, CN, C,alkyl, C,alkoxy, C,acyloxy, NR,R,, NHCOR,, NHSO,R,, COR,, CO,R,, CONR,R,, and SO,NHR,; R,-R,represent hydrogen, C,alkyl, or R,and R,or R,and R,form a C,heterocycloalkyl ring, or R,additionally may represent trifluoromethyl; and pharmaceutically acceptable derivatives or solvates thereof, to processes for their preparation; and their use in the treatment of clinical conditions susceptible to amelioration by administration of a thrombin inhibitor.

Benzamide derivatives as thrombin inhibitors

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

Benzofuran derivatives

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Stevenage, United Kingdom

Martin Pass