DERIVADOS DE BENZAMIDA CON PROPIEDADES INHIBIDORAS DE TROMBINA

• Main Authors: PATEL, VIPULKUMAR, WATSON, NIGEL, STEPHEN, PASS, MARTIN
• Format: Patent
• Language: Spanish
• Published: 16.12.2003
• Edition: 7
• Subjects: CHEMISTRY; HETEROCYCLIC COMPOUNDS; HUMAN NECESSITIES; HYGIENE; MEDICAL OR VETERINARY SCIENCE; METALLURGY; ORGANIC CHEMISTRY; PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES

Un compuesto representado por la fórmula (I)**fórmula** donde R1 y R2 representan independientemente un grupo o R1 y R2 forman juntos un grupo heterocicloalquilo o heterocicloalquenilo C3-7, que puede estar opcionalmente sustituido con alquilo C1-6, alcoxi C1-4, halógeno, ácido carboxílico o un grupo éster de ácido carboxílico C1-4; R3 representa hidrógeno, alquilo C1-3, halógeno, o alcoxi C1-2; R4, R5 y R6 representan independientemente hidrógeno, o halógeno; R7 representa hidrógeno o alquilo C1-6; R8 representa hidrógeno, cicloalquilo C3-7, cicloalquenilo C3-7, heterocicloalquilo C3-7, heterocicloalquenilo C3-7, fenilo, naftilo, un anillo heterocíclico aromático de 5 ó 6 miembros que contiene uno o más heteroátomos seleccionados de átomos de nitrógeno, azufre y oxígeno, o un sistema bicíclico de anillos condensados que contiene uno o más átomos de nitrógeno, azufre y oxígeno, grupos que opcionalmente están sustituidos con uno o más grupos seleccionados de halógeno, hidroxi, CN, alquilo C1-6, alcoxi C1-6, aciloxi C1-6, NR9R10, NHCOR11, NHSO2R12, COR13, CO2R14, CONR15R16, y SO2NHR17. The invention relates to a novel class of amide derivatives which act as thrombin inhibitors as described by formula (I), where R1 and R2, independently represent a group (a) or R1 and R2 together form a C3-7 heterocycloalkyl or heterocycloalkenyl group which may be optionally substituted by C1-6 alkyl, C1-4 alkoxy, halogen, carboxylic acid or a C1-4 carboxylic acid ester group; R3 represents hydrogen, C1-3 alkyl, halogen, or C1-2 alkoxy; R4, R5 and R6 independently represent hydrogen, or halogen; R7 represents hydrogen or C1-6 alkyl; R8 represents hydrogen, C3-7 cycloalkyl, C3-7 cycloalkenyl, C3-7 heterocycloalkyl, C3-7 heterocycloalkenyl, aryl or heteroaryl, which groups are optionally substituted by one or more groups selected from halogen, hydroxy, CN, C1-6 alkyl, C1-6 alkoxy, C1-6 acyloxy, NR9R10, NHCOR11, NHSO2R12, COR13, CO2R14, CONR15R16, and SO2NHR17; X represents a bond, a C1-6 alkyl chain, or a C3-6 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, C1-6 alkyl, C1-6 alkoxy, C1-6 acyloxy, NR9R10, NHCOR11, NHSO2R12, COR13, CO2R14, CONR15R16, and SO2NHR17; R9-R17 represent hydrogen, C1-6 alkyl, or R9 and R10 or R15 and R16 form a C</PDA