Hiv inhibiting pyrimidines derivatives

Details Hiv inhibiting pyrimidines derivatives Hiv inhibiting pyrimidines derivatives

C - Chemistry, Metallurgy

07

D

C07D 239/46 (2006.01) A61K 31/505 (2006.01) A61P 31/18 (2006.01) C07C 255/42 (2006.01) C07D 239/47 (2006.01) C07D 239/48 (2006.01) C07D 403/12 (2006.01) C07D 403/14 (2006.01) C07D 405/12 (2006.01) C07D 407/12 (2006.01) C07D 409/12 (2006.01) C07D 413/12 (2006.01) C07D 417/12 (2006.01) A61K 31/675 (2006.01)

Patent

CA 2452217

This invention concerns HIV replication inhibitors of formula (I) 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; 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, -CHOH-, -S-, -S(=O)p-, -X2-C1-4alkanediyl- or - C1-4alkanediyl-X2-; R3 is NHR13; NR13R14; -C(=O)-NHR13; -C(=O)-NR13R14; -C(=O)- R15; -CH=N-NH-C(=O)-R16; substituted C1-6alkyl; optionally substituted C1- 6alkyloxyC1-6alkyl; substituted C2-6alkenyl; substituted C2-6alkynyl; C1- 6alkyl substituted with hydroxy and a second substituent; -C(=N-O-R8)-C1- 4alkyl; R7; or -X3-R7; R4 is halo, hydroxy, C1-6alkyl, C3-7cycloalkyl, C1- 6alkyloxy, cyano, nitro, polyhaloC1-6alkyl, polyhaloC1-6alkyloxy, aminocarbonyl, C1-6alkyloxycarbonyl, C1-6alkylcarbonyl, formyl, amino, mono- or di(C1-4alkyl)amino; their use as a medicine, their processes for preparation and pharmaceutical compositions comprising them.

L'invention concerne des inhibiteurs de la réplication du VIH correspondant à la formule (I), leurs <i>N</i>-oxydes, leurs sels d'addition pharmaceutiquement acceptables, les amines quaternaires et leurs formes stéréochimiquement isomères, dans laquelle le noyau contenant -a¿1?=a¿2?-a¿3?=a¿4?- et -b¿1?=b¿2?-b¿3?=b¿4?- représente phényle, pyridyle, pyrimidinyle, pirazinyle, pyridazinyle; n est 0 à 5; m est 1 à 4; R¿1? est hydrogène; aryle; formyle; alkylcarbonyle C?1-6#191; alkyle C?1-6#191; alkyloxycarbonyle C?1-6#191; alkyle C?1-6#191 substitué, alkylcarbonyle C?1-6#191, alkyloxycarbonyle C?1-6#191, alkylcarbonyloxy C?1-6#191; alkyloxy C?1-6#191; alkylcarbonyle substitué C?1-6#191; R¿2? est hydroxy, halo, alkyle C?1-6#191 éventuellement substitué, cycloalkyle C?3-7#191, alcényle C?2-6#191 éventuellement substitué, alkynyle C?2-6#191 éventuellement substitué, alkyloxy C?1-6#191, alkyloxycarbonyle C?1-6#191, carboxyle, cyano, nitro, amino, mono- ou di(C?1-6#191alkyl)amino, polyhalométhyle, polyhalométhyloxy, polyhalométhylthio, -S(=O)?p#191R¿6?, -NH-S(=O)?p#191R¿6?, -C(=O)R¿6?, -NHC(=O)H, -C(=O)NHNH?2#191, -NHC(=O)R¿6?, -C(=NH)R¿6? ou un hétérocycle à 5 éléments; X?1#191 est -NR¿5?-, -NH-NH-, -N=N-, -O-, -C(=O)-, alcanediyle C?1-4#191, -CHOH-, -S-, -S(=O)?p#191-, alcanediyl-X?2#191-C?1-4#191 ou -C?1-4#191alcanediyl-X?2#191-; R¿3? est NHR¿13?; NR¿13?R¿14?; -C(=O)-NHR¿13?; -C(=O)-NR¿13?R¿14?; -C(=O)-R¿15?; -CH=N-NH-C(=O)-R¿16?; alkyle C?1-6#191 substitué; alkyloxy C?1-6#191 éventuellement substitué; alkyle C?1-6#191; alcényle C?2-6#191 substitué; alkynyle C?2-6#191 substitué; alkyle C?1-6#191 substitué avec hydroxy et un deuxième substitutif; alkyle-C(=N-O-R¿8?)-C?1-4#191; R¿7?; ou -X?3#191-R¿7?; R¿4? est halo, hydroxy, alkyle C?1-6#191, cycloalkyle C?3-7#191, alkyloxy C?1-6#191, cyano, nitro, alkyle polyhalo C?1-6#191, alkyloxy polyhalo C?1-6#191, aminocarbonyle, alkyloxycarbonyle C?1-6#191, alkylcarbonyle C?1-6#191, formyle, amino, mono- ou di(C?1-4#191alkyl)amino; leur utilisation en tant que médicaments, les procédés de fabrication correspondants et les compositions pharmaceutiques les comprenant.

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