Publication number: 20060252764
Abstract: This invention concerns HIV replication inhibitors of formula the N-oxides, the pharmaceutically acceptable addition salts, the quaternary amines and the stereochemically isomeric forms thereof, wherein the ring containing -a1=a2-a3=a4- and -b1=b2-b3=b4- represents phenyl, pyridyl, pyrimidinyl, pirazinyl, pyridazinyl;n is 0 to 5; m is 1 to 4; R1 is hydrogen; aryl; formyl; C1-6alkylcarbonyl; C1-6alkyl; C1-6alkyloxycarbonyl; substituted C1-6alkyl, C1-6alkylcarbonyl, C1-6alkyloxycarbonyl, C1-6alkylcarbonyloxy; substituted C1-6alkyloxyC1-6alkylcarbonyl; R2 is hydroxy, halo, optionally substituted C1-6alkyl, C3-7cycloalkyl, optionally substituted C2-6alkenyl, optionally substituted C2-6alkynyl, C1-6alkyloxy, C1-6alkyloxycarbonyl, carboxyl, cyano, nitro, amino, mono- or di(C1-6alkyl)amino, polyhalomethyl, polyhalomethyloxy, polyhalomethylthio, —S(?O)pR6, —NH—S(?O)pR6, —C(?O)R6, —NHC(?O)H, —C(?O)NHNH2, —NHC(?O)R6, —C(?NH)R6 or a 5-membered heterocycle; X1 is —NR5—, —NH—NH—, —N?N—, —O—, —C(?O)—, C1-4alkanediyl,
Type:
Application
Filed:
June 26, 2006
Publication date:
November 9, 2006
Inventors:
Jerome Guillemont, Patrice Palandijian, Marc De Jonge, Lucien Koymans, Hendrik Vinkers, Frederik Daeyaert, Jan Heeres, Koen Van Aken, Paulus Lewi, Paul Janssen, Frank Xavier Arts
Publication number: 20060211724
Abstract: The present invention concerns the compounds having the formula (1), N-oxides, salts, stereoisomeric forms, racemic mixtures, prodrugs, esters and metabolites thereof wherein (a) or (b); A, together with the two carbons of the phenyl ring to which it is attached forms a monocyclic aryl or a monocyclic Het2; R1 is hydrogen, halo, nitro, cyano, sultam, sultim, C3-7cycloalkyl, C(?O)—R5, S(?O)y—R6, OR7, NR8R9, C(?NR8)—R5, optionally polysubstituted C1-6alkyl, optionally polysubstituted C2-6alkenyl or optionally polysubstituted C2-6alkynyl; R2 is hydrogen, C3-7cycloalkyl, aryl, Het1, Het2, C(?O)—R5, S(?)y—R6OR7, NR8R9, C?NR8)—R5, or optionally polysubstituted C1-6alkyl, optionally polysubstituted C2-6alkenyl or optionally polysubstituted C2-6alkynyl. It further relates to their use as HIV integrase inhibitors, processes for their preparation as well as pharmaceutical compositions and diagnostic kits comprising them.
Type:
Application
Filed:
April 27, 2004
Publication date:
September 21, 2006
Inventors:
Gaston Verschueren, Inge Dierynck, Dominique Louis Nestor Surleraux, Frederik Daeyaert