| abstract |
It relates to imidazole [2,1-b] [3] benzazepine derivatives of the formula (I). N-oxide forms, pharmaceutically acceptable addition salts, and stereochemically isomeric forms thereof, in which the dotted line is an optional bond; n is 1 or 2; R1 is hydrogen, halo, formyl, C1-4 alkyl, C1-4 alkyl substituted with hydroxy C1-4 alkyloxy, C1-4 alkylcarbonyloxy, imidazolyl, thiazolyl or oxazolyl, or a radical of the formula: -X-CO-OR5, - X-CO-NR6R7, or -X-COR10, in which -X- is a direct bond, C1-4 alkaliyl, or C2-6 alkeniyl; R5 is hydrogen, C1-12 alkyl, Ar, Het, C1-C6 alkyl substituted with C1-4 alkyloxy aryl or heteroaryl; each of R6 and R7 independently is hydrogen or C1-C4 alkyl; R 2 is hydrogen, halo, C 1 -C 4 alkyl, C 1-4 hydroxyalkyl, C 1-4 alkyloxycarbonyl, carboxyl, formyl or phenyl; R3 is hydrogen, C1-C4 alkyl or C1-4 alkyloxy; R4 is hydrogen, halo, C1-C4 alkyl, C1-4 alkyloxy or haloc1-4alkyl; Z is -CH2, CH2-CH2- or -CH = CH-, -CHOH-CH2 -, - O-CH2 -, - C (= O) -CH2, or -C (= NOH-CH2; -AB- is a bivalent radical; -A1- is a direct bond, optionally substituted C1-6 alkandiyl, C1-6alkandiyl-C1-6-acandiyl, C1-6 alkaniyloxy, carbonyl, C1-6 alkandiylcarbonyl, optionally substituted C1-6 alkaniyloxy, - A2- is a direct bond or C1-6 alkandiyl; and Q is aryl. Processes for preparing said products, a pharmaceutical composition comprising the same, a process for preparing said pharmaceutical composition, a product and the use of said compounds as medicaments are described. inhibit or reverse the effects of multidrug resistance. |