C - Chemistry – Metallurgy – 07 – D
Patent
C - Chemistry, Metallurgy
07
D
C07D 487/04 (2006.01) A61K 31/445 (2006.01) A61K 31/47 (2006.01) A61K 31/55 (2006.01) C07D 471/04 (2006.01) C07D 487/14 (2006.01) C07D 491/147 (2006.01) C07D 495/14 (2006.01) C07D 498/04 (2006.01) C07D 498/14 (2006.01)
Patent
CA 2237594
This invention concerns the compounds of formula (I), the N-oxide forms, the pharmaceutically acceptable addition salts and the stereochemically isomeric forms thereof, wherein the dotted line is an optional bond; n is 1 or 2; R1 is hydrogen; halo; formyl; C1-4alkyl optionally substituted with hydroxy, C1-4alkyloxy, C1-4alkylcarbonyloxy, imidazolyl, thiazolyl or oxazolyl; or a radical of formula -X-COOR5, -X-CONR6R7 or -X-COR10 wherein -X- is a direct bond, C1-4alkanediyl or C2-6alkenediyl; R5 is hydrogen, C1-12alkyl, Ar, Het, C1-6alkyl substituted with C1-4alkyloxy, aryl or heteroaryl; R6 and R7 each independently are hydrogen or C1-4alkyl; R2 is hydrogen, halo, C1-4alkyl, hydroxyC1-4alkyl, C1-4alkyloxycarbonyl, carboxyl, formyl or phenyl; R3 is hydrogen, C1-4alkyl or C1-4alkyloxy; R4 is hydrogen, halo, C1- 4alkyl, C1-4alkyloxy or haloC1-4alkyl; Z is -CH2-, -CH2-CH2-, CH=CH-, -CHOH-CH2-, -O-CH2-, -C(=O)-CH2- or -C(=NOH)-CH2-; -A-B- is a bivalent radical; A1 is a direct bond, optionally substituted C1-6alkanediyl, 1-6alkanediyl-oxy-C1-6alkanediyl, carbonyl, C1- 6alkanediylcarbonyl, optionally substituted C1-6alkanediyloxy; A2 is a direct bond or C1-6alkanediyl; and Q is aryl. Processes for preparing said products, formulations comprising said products and their use as a medicine are disclosed, in particular for inhibiting or reversing the effects of multidrug resistance.
Janssens Frans Eduard
Leenaerts Joseph Elisabeth
Sommen Francois Maria
Surleraux Dominique Louis Nestor Ghislaine
Gowling Lafleur Henderson Llp
Janssen Pharmaceutica N.v.
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