Phenyl substituted triazoles and their use as selective...

Details Phenyl substituted triazoles and their use as selective... Phenyl substituted triazoles and their use as selective...

C - Chemistry, Metallurgy

07

D

C07D 471/04 (2006.01) A61K 31/41 (2006.01) A61P 3/12 (2006.01) A61P 9/10 (2006.01) A61P 19/00 (2006.01) A61P 25/28 (2006.01) C07D 249/06 (2006.01) C07D 265/36 (2006.01) C07D 285/14 (2006.01)

Patent

CA 2467267

Phenyl substituted triazoles of formula (I) wherein R1 is naphthyl or phenyl optionally substituted with one or more substituents selected from halo, -O-C1- 6alkyl, -S-C1-6alkyl, C1-6alkyl, C1-6haloalkyl, -O-(CH2)n-Ph, -S-(CH2)n-Ph, cyano, phenyl, and CO2R, wherein R is hydrogen or C1-6alkyl, and n is 0, 1, 2 or 3; or R1 is phenyl or pyridyl fused with an aromatic or non-aromatic cyclic ring of 5-7 members wherein said cyclic ring optionally contains up to three heteroatoms, independently selected from N, O and S, and N may be further optionally substituted by C1-6 alkyl, and wherein the cyclic ring may be optionally substituted by =O; R2 and R3 are independently selected from H, C1- 6alkyl, C1-6alkoxy, phenyl, NH(CH2)n-Ph, NH-C1-6alkyl, halo, alkoxy, CN, NO2, CONHR and SO2NHR; two of X1, X2 and X3 are N and the other is NR4 wherein R4 is hydrogen, C1-6alkyl, C3-7cycloalkyl, -(CH2)p-CN, -(CH2)p-CO2H, -(CH2)p- CONHR5R6, -(CH2)pCOR5, -(CH2)q(OR7)2, -(CH2)pOR5, -(CH2)q-CH=CH-CN, -(CH2)q- CH=CH-CO2H, -(CH2)p-CH=CH-CONHR5R6, -(CH2)pNHCOR8 or -(CH2)pNR9R10; R5 and R6 are independently hydrogen or C1-6alkyl; R7 is C1-6alkyl;R8 is C1-7alkyl, or optionally substituted aryl, heteroaryl, arylC1-6alkyl or heteroaryl C1- 6alkyl; R9 and R10 are independently selected from hydrogen, C1-6alkyl, aryl and arylC1-6alkyl; p is 0-4; and q is 1-4 and salts and solvates thereof, are disclosed, as are methods for their preparation, pharmaceutical compositions containing them and their use in medicine.

La présente invention se rapporte à des triazoles à substitution phényle représentés par la formule (I), dans laquelle R<sb>1</sb> est naphthyle ou phényle éventuellement substitué par un ou plusieurs substituants sélectionnésparmi halo, -O-alkyle C<sb>1-6</sb>, -S-alkyle C<sb>1-6</sb>, alkyle C<sb>1-6</sb>, haloalkyle C<sb>1-6</sb>, -O-(CH<sb>2</sb>)<sb>n</sb>-Ph, -S-(CH<sb>2</sb>)<sb>n</sb>-Ph, cyano, phényle et CO<sb>2</sb>R, où R est hydrogène ou alkyle C<sb>1-6</sb>, et n est égal à 0,1, 2 ou 3; ou R<sb>1</sb> est phényle ou pyridyle fusionné avec un noyau cyclique aromatique ou non aromatique ayant de 5 à 7 éléments, ledit noyau cyclique contenant éventuellement jusqu'à 3 hétéroatomes, indépendamment sélectionnés parmi N, O et S, et N peut également être éventuellement substitué par alkyle C<sb>1-6</sb>, le noyau cyclique étant éventuellement substitué par =O; R<sb>2</sb> et R<sb>3</sb> sont indépendamment sélectionnés parmi H, alkyle C<sb>1-6</sb>, alkoxy C<sb>1-6</sb>, phényle, NH(CH<sb>2</sb>)<sb>n</sb>-Ph, NH-alkyle C<sb>1-6</sb>, halo, alkoxy, CN, NO<sb>2</sb>, CONHR et SO<sb>2</sb>NHR; deux des groupes parmi X1, X2 et X3 sont N et l'autre est NR<sb>4</sb> où R<sb>4</sb> est hydrogène, alkyle C<sb>1-6</sb>, cycloalkyle C<sb>3-7</sb>, -(CH<sb>2</sb>)<sb>p</sb>-CN, -(CH<sb>2</sb>)<sb>p</sb>-CO<sb>2</sb>H, -(CH<sb>2</sb>) <sb>p</sb -CONHR<sb>5</sb>R<sb>6</sb>, -(CH<sb>2</sb>)<sb>p</sb>COR<sb>5</sb>, -(CH<sb>2</sb>)<sb>q</sb>(OR<sb>7</sb>)<sb>2</sb>, -(CH<sb>2</sb>)<sb>p</sb>OR<sb>5</sb>, -(CH<sb>2</sb>)<sb>q</sb>-CH=CH-CN, -(CH<sb>2</sb>)<sb>q</sb>-CH=CH-CO<sb>2</sb>H, -(CH<sb>2</sb>)<sb>p</sb>-CH=CH-CONHR<sb>5</sb>R<sb>6</sb>, -(CH<sb>2</sb>)<sb>p</sb>NHCOR<sb>8</sb> ou -(CH<sb>2</sb>)<sb>p</sb>NR<sb>9</sb>R<sb>10</sb>; R<sb>5</sb> et R<sb>6</sb> sont indépendamment hydrogène ou alkyle C<sb>1-6</sb>; R<sb>7</sb> est alkyle C<sb>1-6</sb>; R<sb>8</sb> est alkyle C<sb>1-7</sb>, ou aryle éventuellement substitué, hétéroaryle, aryl-alkyle C<sb>1-6</sb> ou hétéroaryl-alkyle C<sb>1-6</sb>; R<sb>9</sb> et R<sb>10</sb> sont indépendamment sélectionnés parmi hydrogène, alkyle C<sb>1-6</sb>, aryle et aryl-alkyle C<sb>1-6</sb>; p est compris entre 0 et 4; et q est compris entre 1 et 4. L'invention se rapporte également à des sels et à des solvates de ces triazoles ainsi qu'à des procédés permettant leur préparation, à des compositions pharmaceutiques les contenant et à leur utilisation en médecine.

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