NUEVOS DERIVADOS DE PEPTIDOS

• Main Authors: DEREK EDWARD BRUNDISH, JOHN PETER PRIESTLE, ALBERT SCHMITZ, HANS RINK, MARKUS GRUTTER
• Format: Patent
• Language: Spanish
• Published: 31.05.1994
• Edition: 5
• Subjects: BEER; BIOCHEMISTRY; CHEMISTRY; COMPOSITIONS THEREOF; CULTURE MEDIA; ENZYMOLOGY; FERMENTATION OR ENZYME-USING PROCESSES TO SYNTHESISE A DESIREDCHEMICAL COMPOUND OR COMPOSITION OR TO SEPARATE OPTICAL ISOMERSFROM A RACEMIC MIXTURE; HETEROCYCLIC COMPOUNDS; HUMAN NECESSITIES; HYGIENE; MEDICAL OR VETERINARY SCIENCE; METALLURGY; MICROBIOLOGY; MICROORGANISMS OR ENZYMES; MUTATION OR GENETIC ENGINEERING; ORGANIC CHEMISTRY; PEPTIDES; PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES; PROCESSES USING MICROORGANISMS; PROPAGATING, PRESERVING OR MAINTAINING MICROORGANISMS; SPIRITS; VINEGAR; WINE

La invención se refiere a nuevos derivados de péptidos que tienen una actividad como inhibidores de enzimas, en particular como inhibidores de trobina. La invención se refiere también a métodos para la producción de dichos inhibidores de enzimas, a composiciones farmacéuticas que contienen estos últimos y a su uso como agentes anticoagulantes. PCT No. PCT/EP93/00908 Sec. 371 Date Oct. 20, 1994 Sec. 102(e) Date Oct. 20, 1994 PCT Filed Apr. 15, 1993 PCT Pub. No. WO93/22344 PCT Pub. Date Nov. 11, 1993Novel compounds of the formula I l or are linked to form C3-C7 cycloalkyl and R3, R4 and R5 are the same or different and are hydrogen, C1-C4 alkyl, hydroxy, OR6, SR6, halogen, NR7R8, NO2, CN, CONR7R8 or CO2R9 wherein R6 is C1-C4 alkyl or C7-C10 aralkyl and R7, R8 and R9 are the same or different and are hydrogen, C1-C4 alkyl or C7-C10 aralkyl or R7 and R8 together with the nitrogen atom to which they are bound form 5 or 6 membered azacycloalkyl or oxazacycloalkyl; Arg is arginine [NH-CH(CH2CH2CH2NH-C(=NH)-NH2)-CO]; X is methine CH or nitrogen; n is an integer from 0 to 7; L is a peptide linker, and H is the carboxy terminal end of hirudin, and salts thereof, are provided. The novel compounds are useful for the medical treatment or prevention of thrombosis or diseases caused by thrombosis or can be used for the determination of thrombin in blood as diagnostic reagents.