NEW DARA ACTION RECEPTOR ANTAGONISTS (DARA) AGAINST ATI AND ETA RECEPTORS

摘要

1. The compound of the formula! ! where R3 has any of the formulas! ! where R1 is selected from! ! where! R2 each independently means hydrogen, halogen, C1-C8 alkyl, halogen-C1-C8 alkyl, C3-C8 cycloalkyl, C2-C8 alkenyl, C2-C8 alkynyl, C1-C8 alkoxy-C1-C8 alkyl, C1-C8 alkoxy, aryloxy, C1-C8 alkoxy-C1 -C8 alkoxy, cyano, hydroxyl, hydroxy-C1-C8 alkyl, nitro, - (CH2) WNR18R19, where w is 0, 1, 2 or 3, and R18 and R19 independently mean hydrogen, C1-C8 alkyl, aryl, aryl-C1- C8 alkyl, heteroaryl, heteroaryl-C1-C8 alkyl or may together form a five- or six-membered saturated or unsaturated ring structure, optionally containing one to two heteroatoms selected from oxygen, sulfur or nitrogen, and may yt optionally substituted C1-C8 alkylene, hydroxy or oxo; ! R4 means a five- or six-membered mono- or bicyclic ring system having from one to three heteroatoms selected from O, N and S, such as pyridyl, pyrimidyl, pyrazinyl, pyridazinyl, triazinyl, oxazolyl, isoxazolyl, thiazolyl, thiadiazolyl, isothiazolyl, oxadiazolyl, imidazolyl, triazolyl, tetrazolyl and pyridothiazolyl, each of which may optionally be substituted with one or more of the following substituents: hydrogen, halogen, cyano, C1-C8 alkyl, C1-C8 alkoxy, trifluoromethyl and -COR32; ! R5 and R6 independently mean hydrogen, halogen, C1-C8 alkyl, -COOR13, -CO-NR18R19, cyano and -NR18R19, or R5 and R6 may together form a five- or six-membered cycloalkyl, aryl ring or heteroaryl ring structure having one or two heteroatoms selected from O, N and S, which may be further substituted with C1-C8 alkyl, C1-C8 alkoxy or hydroxy; where R18 and R19 are independently selected from hydrogen, C1-C8 alkyl,! aryl-C1-C8 alkyl, heteroaryl-C1-