2,4-disubstituted triazine derivatives with anti hiv activity

Details 2,4-disubstituted triazine derivatives with anti hiv activity 2,4-disubstituted triazine derivatives with anti hiv activity

C - Chemistry, Metallurgy

07

D

C07D 251/16 (2006.01) A61K 31/53 (2006.01) A61P 31/18 (2006.01) C07D 251/18 (2006.01) C07D 251/22 (2006.01)

Patent

CA 2351203

This invention concerns the use of the compounds of formula (1), the N-oxides, the pharmaceutically acceptable addition salts, quaternary amines and the stereochemically isomeric forms thereof, wherein -a1- a2-a3-a4 forms a phenyl, pyridinyl, pyrimidinyl, pyridazinyl or pyrazinyl with the attached vinyl group; n is 0 to 4; and where possible 5; R1 is hydrogen, aryl, formyl, C1-6alkylcarbonyl, C1-6alkyl, C1-6alkyloxycarbonyl or substituted C1-6alkyl; each R2 independently is hydroxy, halo, optionally substituted C1-6alkyl, C2-6alkenyl or C2-6alkynyl, C3-7cycloalkyl, C1-6alkyloxy, C1- 6alkyloxycarbonyl, carboxyl, cyano, nitro, amino, mono--or di(C1-6alkyl)amino, polyhalomethyl, polyhalomethyloxy, polyhalomethylthio, - S(=O)p R4, -NH-S(-O)p R4, -C(-O)R4, -NHC(-O)H, -C(=O)NHNH2, -NHC(-O)R4, -C(=NH)R4 or a 5-membered heterocyclic ring; p is 1 or 2; L is optionally substituted C1-10alkyl, C2-10alkenyl, C2-10alkynyl or C3-7cycloalkyl; or L is -X-R3 wherein R3 is optionally substituted phenyl, pyridinyl, pyrimidinyl, pyrazinyl or pyridazinyl; X is -NR1-, -NH-NH-, -N-N-, -O-, -C(=O)-, -CHOH-, -S-, -S(-O)- or -S(=O)2-; aryl is optionally substituted phenyl; for the manufacture of a medicine for the treatment of subjects suffering from HIV (Human Immunodeficiency Virus) infection.

L'invention concerne l'utilisation des composés correspondant à la formule (I), des N-oxydes, des sels d'addition pharmaceutiquement acceptables, des amines quaternaires et leurs formes stéréochimiquement isomères, dans laquelle -a<1>=a<2>-a<3>=a<4>- forme un phényle, pyridinyle, pyrimidinyle, pyridazinyle ou pyrazinyle avec le groupe vinyle attaché; n est 0 à 4 et si possible 5; R<1> est hydrogène, aryle, formyle, C1-6alkylcarbonyle, C1-6alkyle, C1-6alkyloxycarbonyle ou alkyle C1-6 substitué; chaque R<2> est indépendamment hydroxy, halo, éventuellement alkyle C1-6 substitué, C2-6alcényle ou C2-6alkynyle, C3-7cycloalkyle, C1-6alkyloxy, C1-6alkyloxycarbonyle, carboxyle, cyano, nitro, amino, mono- ou di(C1-6alkyl)amino, polyhalométhyle, polyhalométhyloxy, polyhalométhylthio, -S(=O)pR<4>, -NH-S(=O)pR<4>, -C(=O)R<4>, -NHC(=O)H, -C(=O)NHNH2, -NHC(=O)R<4>, -C(=NH)R<4> ou un noyau hétérocyclique à 5 éléments; p est 1 ou 2; L est C1-10alkyle, C2-10alcényle, C2-10alkynyle ou C3-7cycloalkyle éventuellement substitués; ou L est -X-R<3> dans laquelle R<3> est phényle, pyridinyle, pyrimidinyle, pyrazinyle ou pyridazinyle éventuellement substitués; X est -NR<1>-, -NH-NH-, -N=N-, -O-, -C(=O)-, -CHOH-, -S-, -S(=O)- or -S(=O)2-; et aryle est phényle éventuellement substitué. Le composé sert à fabriquer un médicament destiné à traiter les sujets souffrant d'une infection par le VIH (virus de l'immunodéficience humaine).

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