AR080709A1 - Derivados de triazina disustituidos farmaceuticamente activos - Google Patents

Derivados de triazina disustituidos farmaceuticamente activos

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Publication number
AR080709A1
AR080709A1 ARP110100926A ARP110100926A AR080709A1 AR 080709 A1 AR080709 A1 AR 080709A1 AR P110100926 A ARP110100926 A AR P110100926A AR P110100926 A ARP110100926 A AR P110100926A AR 080709 A1 AR080709 A1 AR 080709A1
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Argentina
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cr62r63
cycle
nhco
cr49r50
cr86r87
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ARP110100926A
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English (en)
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Peter Nussbaumer
Gerd Ruhter
Ulrich Lucking
Axel Choidas
Jan Eickhoff
Carsten Schultz-Fademrecht
Klebl Bert Dr
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Lead Discovery Center Gmbh
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    • C07D251/14—Heterocyclic compounds containing 1,3,5-triazine rings not condensed with other rings having three double bonds between ring members or between ring members and non-ring members with hydrogen or carbon atoms directly attached to at least one ring carbon atom
    • C07D251/16—Heterocyclic compounds containing 1,3,5-triazine rings not condensed with other rings having three double bonds between ring members or between ring members and non-ring members with hydrogen or carbon atoms directly attached to at least one ring carbon atom to only one ring carbon atom
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    • C07D251/22—Heterocyclic compounds containing 1,3,5-triazine rings not condensed with other rings having three double bonds between ring members or between ring members and non-ring members with hydrogen or carbon atoms directly attached to at least one ring carbon atom to two ring carbon atoms
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    • C07D401/04—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings directly linked by a ring-member-to-ring-member bond
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Abstract

La presente se refiere a derivados de triazina disustituidos y/o sales farmacéuticamente aceptables de ellos, el uso de estos derivados como agentes farmacéuticamente activos, en especial para la profilaxis y/o el tratamiento de enfermedades infecciosas, incluyendo enfermedades oportunistas, enfermedades inmunologicas, enfermedades autoinmunes, enfermedades cardiovasculares, enfermedades celulares proliferativas, inflamacion, disfuncion eréctil y apoplejía, y a composiciones farmacéuticas conteniendo al menos uno de dichos derivados de triazina disustituidos y/o las sales farmacéuticamente aceptables de ellos. Además la presente se refiere al uso de dichos derivados de triazina disustituidos como inhibidores de una proteína quinasa. Reivindicacion 1: Compuestos de la formula general (1) en que R1 es como en las formulas (2), L es un enlace o -CR5R6-, -CR5R6-CR7R8-, -CR5R6-CR7R8-CR9R10-, CR5R6-CR7R8-CR9R10-CR11 R12-; R5-R12 representan independientemente uno del otro -H, -CH3, -C2H5, -C3H7, -F, -CI, -Br, I; R3 está seleccionado de -H, -NO2, -NH2, -CN, -F, -CI, -Br, -I, -CH3, -C2H5, -Ph, -C3H7, -CH(CH3)2, -C4H9, -CH2-CH(CH3)2, -CH(CH3)-C2H5, -C(CH3)3, -O-CH3, -O-C2H5, -O-C3H7, -O-CH(CH3)2, -O-C4H9, -O-CH2-CH(CH3)2, -O-CH(CH3)-C2H5, -O-C(CH3)3, -CR13R14R21, -CR13R14-CR15R16R21, -O-CR13R14R21, -CR13R14-CR15R16-CR17R18R21, -CR13R14-CR15R16-CR17R18-CR19R20R21, -O-CR13R14-CR15R16R21, -O-CR13R14-CR15R16-CR17R18R21, -SO2R22, -CONR23R24, -NR25COR22, -O-CR13R14-CR15R16-CR17R18-CR19R20R21, -NR25SO2NR23R24, -NR25SO2R22, -NR25CONR23R24, -SO2NR23R24, -SO(NR26)R27, -NH-CO-NH-Ph; R13-R21, R29-R32 y R33-R48 representan independientemente uno del otro -H, -F, -CI, -Br, -I; R26 es -H, -CH3, -C2H5, -C3H7, -CH(CH3)2, -C4H9, -CH2-CH(CH3)2, -CH(CH3)-C2H5, -C(CH3)3, -C5H11, -CH(CH3)-C3H7, -CH2-CH(CH3)-C2H5, -CH(CH3)-CH(CH3)2, -C(CH3)2-C2H5, -CH2-C(CH3)3, -CH(C2H5)2, -C2H4-CH(CH3)2, -C6H13, -C3H6-CH(CH3)2, -C2H4-CH(CH3)-C2H5, -CH(CH3)-C4H9, -CH2-CH(CH3)-C3H7, -CH(CH3)-CH2-CH(CH3)2, -CH(CH3)-CH(CH3)-C2H5, -CH2-CH(CH3)-CH(CH3)2, -CH2-C(CH3)2-C2H5, -C(CH3)2-C3H7, -C(CH3)2-CH(CH3)2, -C2H4-C(CH3)3, -CH(CH3)-C(CH3)3, -CR13R14R21, -COR28, -CR13R14-CR15R16R21, -CR13R14-CR15R16-CR17R18-CR19R20-CR29R30R21, -CR13R14-CR15R16-CR17R18R21, -CR13R14-CR15R16-CR17R18-CR19R20R21, -CR13R14-CR15R16-CR17R18-CR19R20-CR29R30-CR31R32R21, -COOR28, formulas (3) estos grupos cicloalquílicos C3-6 pueden ser sustituidos además por uno, dos, tres, cuatro, cinco o más sustituyentes seleccionados del grupo que consiste de R33-R48; R22, R27 y R28 se seleccionan independientemente de -CR49R50R51, -CR49R50-CR52R53R51, -CR49R50-CR52R53-CR54R55-CR56R57-CR58R59R51, -CR49R50-CR52R53-CR54R55R51, -CR49R50-CR52R53-CR54R55-CR56R57R51, -CR49R50-CR52R53-CR54R55-CR56R57-CR58R59-CR60R61R51, -CH2Ph, -CH2Ph cuyo grupo fenil puede ser sustituido además por uno, dos, tres, cuatro, cinco o más sustituyentes seleccionados del grupo que consiste de R5-R12 grupos cicloalquílicos C3-6 listados para R26, que pueden ser sustituidos por uno, dos, tres, cuatro, cinco o más sustituyentes seleccionados del grupo que consiste de R33-R48; R49-R61 representan independientemente uno del otro -H, -CH3, -C2H5, -C3H7, -C4H9, -F, -CI, -Br, -I, -OH, -NO2, -NH2; R23 y R24 se seleccionan independientemente de -H, -CR49R50R51, -CR49R50-CR52R53R51, -CR49R50-CR52R53-CR54R55-CR56R57-CR58R59R51, - CR49R50-CR52R53-CR54R55R51, -CR49R50-CR52R53-CR54R55-CR56R57R51, -CR49R50-CR52R53-CR54R55-CR56R57-CR58R59-CR60R61R51, -CR49R50-CR52R53-O-R51', -CR49R50-CR52R53-CR54R55-O-R51', -CR49R50-CR52R53-NR51'R51ö, -CR49R50-CR52R53-CR54R55-NR51'R51ö, -CR49R50-CR52R53-CR54R55-CR56R57-NR51'R51ö, -CR49R50-CR52R53-CR54R55-CR56R57-CR58R59-NR51'R51ô, fenil, fenil sustituido, bencil, bencil sustituido, o los dos residuos R23 y R24 juntos forman con el átomo de nitrogeno al que están ligados una acetidina, pirrolidina, piperidina, piperazina, azepana o anillo morfolino; R51' y R51ö representan independientemente uno del otro -H, -CH3, -C2H5, -C3H7, -C4H9, -CH2Ph, -COOC(CH3)3, -COOCH3, -COOCH2CH3, -COOCH2CH2CH3, -COOCH(CH3)2, -COOCH2Ph, -COCH3; y R25 es -H, -CH3, -C2H5, -C3H7, -CH(CH3)2, -C4H9, -CH2-CH(CH3)2, -CH(CH3)-C2H5, -C(CH3)3; R4 se selecciona de -H, -NO2, -NH2, -CN, -F, -CI, -Br, -I, -CR62R63R64, grupo de formulas (4), -CONH2, -SO2CH3, -SO2C2H5, -SO2C3H7, -NH-SO2-CH3, -NH-SO2-C2H5, -NH-SO2-C3H7, -NHCO-CH3, -NHCO-C2H5, -NHCO-C3H7, -SO2NR23R24, -CH2-SO2NR23R24, -C2H4-SO2NR23R24, -C3H6-SO2NR23R24, -SO2NH2, -CH2-SO2NH2, -C2H4-SO2NH2, -C3H6-SO2NH2, -O-CR62R63-CR65R66R64, -O- CR62R63-CR65R66-CR67R68R64, -CR62R63-CR65R66-CR67R68-CR69R70R64, -O-CR62R63-CR65R66-CR67R68-CR69R70R64, -CR62R63-CR65R66-CR67R68R64, -O-CR62R63-CR65R66-CR67R68-CR69R70-CR71R72R64, -CR62R63-CR65R66R64, -O-CR62R63-CR65R66-CR67R68-CR69R70-CR71R72-CR73R74R64, -O-CR62R63R64, -CR62R63-CR65R66-CR67R68-CR69R70-CR71R72R64, --CR62R63-CR65R66-CR67R68-CR69R70-CR71R72-CR73R74R64, -OCH2Ph, grupo de formulas (3) y (5) estos grupos cicloalcoxi C3-6 y grupos cicloalquílicos C3-6 pueden estar sustituidos además por uno, dos, tres, cuatro, cinco o más sustituyentes seleccionados del grupo que consiste de R33-R48, R62-R74 representan independientemente uno del otro -H, -ciclo-C3H5, -ciclo-C4H7, -ciclo-C5H9, -CR75R76R77, -CR75R76-CR78R79R77, -CR75R76-CR78R79-CR80R81R77, -CR75R76-CR78R79-CR80R79-CR82R81R77, -F, -CI, -Br, -I, -Ph; R75-R82 representan independientemente uno del otro -H, -F, -CI, -Br, -I, -NH2; R4 junto con R22, R23, R24 o R25 puede formar un grupo -CH2CH2- o -CH2CH2CH2- si R4 está ligado en orto a -L-R3; R2 es como en formulas (6), R83 se selecciona de -H, -OH, -NO2, -CN, -F, -CI, -Br, -I, -CF3, -NR23'R24', -CR62R63R64, -CR62R63-NR23'R24', -CR62R63-CR65R66R64, -CR62R63-CR65R66-NR23'R24', -CR62R63-CR65R66-CR67R68R64, -CR62R63-CR65R66-CR67R68-NR23'R24', -O-CR62R63R64, -O-CR62R63-CR65R66R64, -O-R62R63-CR65R66-CR67R68R64, -CHO, -CH2OH, -CR23'O, -CH2OR23'; R23' y R24' representan independientemente uno del otro -H, -CH3, -C2H5, -C3H7, -CH(CH3)2, -C4H9, -CH2-CH(CH3)2, -CH(CH3)-C2H5, -C(CH3)3; -(ciclo-C3H5); x es un valor entre 0 y 3; B es un enlace, -CR86R87-, -CR86R87-CR88R89-, -CR86R87-CR88R89-CR90R91-, -CR86R87-CR88R89-CR90R91-CR92R93-, -CR86R87-CR88R89-CR90R91-CR92R93-CR94R95-, -CR86R87-CR88R89-CR90R91-CR92R93-CR94R95-CR96R97-; R86-R97 representan independientemente uno del otro -H, -CH3, C2H5, -C3H7, -C4H9, -F, -CI, -Br, -I; Y es un enlace, -O-, -S-, -SO-, -SO2-, -SO2NH-, -NHSO2-, -CO-, -COO-, -OOC-, -CONH-, -NHCO-, -NH-, -N(CH3)-, -NH-CO-NH-, -O-CO-NH-, -NH-CO-O-; R84 se selecciona de un enlace, -CR86R87-, -CR86R87-CR88R89-CR90R91-, -CR86R87-CR88R89-CR90R91-CR92R93-, -CR86R87-CR88R89-CR90R91-CR92R93-CR94R95-, -CR86R87-CR88R89-, -CR86R87-CR88R89-CR90R91-CR92R93-CR94R95-CR96R97-; R85 se selecciona de (i) -H, -OH, -OCH3, -OC2H5, -OC3H7, -O-ciclo-C3H5, -OCH(CH3)2, -OC(CH3)3, -OC4H9, -Ph, -OPh, -OCH2-Ph, -OCPh3, -SH, -SCH3, -SC2H5, -SC3H7, -S-ciclo-C3H5, -SCH(CH3)2, -SC(CH3)3, -SC4H9, -NO2, -F, -CI, -Br, -I, -P(O)(OH)2, -P(O)(OCH3)2, -P(O)(OC2H5)2, -P(O)(OCH(CH3)2)2, -Si(CH3)2(C(CH3)3), -Si(C2H5)3, -Si(CH3)3, -CN, -CHO, -COCH3, -COC2H5, -COC3H7, -CO-ciclo-C3H5, -COCH(CH3)2, -COC(CH3)3, -COC4H9, -COOH, -COOCH3, -COOC2H5, -COOC3H7, -COOC4H9, -COO-ciclo-C3H5, -COOCH(CH3)2, -COOC(CH3)3, -OOC-CH3, -OOC-C2H5, -OOC-C3H7, -OOC-C4H9, -OOC-ciclo-C3H5, -OOC-CH(CH3)2, -OOC-C(CH3)3, -CONR23'R24', -NHCOCH3, -NHCOC2H5, -NHCOC3H7, -NHCO-ciclo-C3H5, -NHCO-CH(CH3)2, -NHCOC4H9, -NHCO-C(CH3)3, -NHCO-OCH3, -NHCO-OC2H5, -NHCO-OC3H7, -NHCO-O-ciclo-C3H5, -NHCO-OC4H9, -NHCO-OCH(CH3)2, -NHCO-OC(CH3)3, -NHCO-OCH2Ph, -NR23R24, -CF3, -SOCH3, -SOC2H5, -SOC3H7, -SO-ciclo-C3H5, -SOCH(CH3)2, -SOC(CH3)3, -SO2CH3, -SO2C2H5, -SO2C3H7, -SO2-ciclo-C3H5, -SO2CH(CH3)2, -SO2C4H9, -SO2C(CH3)3, -SO3H, -SO2NR23'R24', -OCF3, -OC2F5, -O-COOCH3, -O-COOC2H5, -O-COOC3H7, -O-COO-ciclo-C3H5, -O-COOC4H9, -O-COOCH(CH3)2, -O-COOCH2Ph, -O-COOC(CH3)3, -NH-CO-NH2, -NH-CO-NHCH3, -NH-CO-NHC2H5, -NH-CO-NHC3H7, -NH-CO-NHC4H9, -NH-CO-NH-ciclo-C3H5, -OCH2-ciclo-C3H5, -NH-CO-NH[CH(CH3)2], -NH-CO-NH[C(CH3)3], -NH-CO-N(CH3)2, -NH-CO-N(C2H5)2, -NH-CO-N(C3H7)2, -NH-CO-N(C4H9)2, -NH-CO-N(ciclo-C3H5)2, -NH-CO-N[CH(CH3)2]2, -NH-CO-N[C(CH3)3]2, -NH-C(=NH)-NH2, -NH-C(=NH)-NHCH3, -NH-C(=NH)-NHC2H5, -NH-C(=NH)-NHC3H7, -NH-C(=NH)-NHC4H9, -NH-C(=NH)-NH-ciclo-C3H5, -NH-C(=NH)-NH[CH(CH3)2], -NH-C(=NH)-NH[C(CH3)3], -NH-C(=NH)-N(CH3)2, -NH-C(=NH)-N(C2H5)2, -NH-C(=NH)-N(C3H7)2, -NH-C(NH)-N(ciclo-C3H5)2, -NH-C(=NH)-N(C4H9)2, -NH-C(=NH)-N[CH(CH3)2]2, -NH-C(=NH)-N[C(CH3)3]2, -O-CO-N H2, -O-CO-NHCH3, -O-CO-NHC2H5, -O-CO-NHC3H7, -O-CO-NHC4H9, -O-CO-NH-ciclo-C3H5, -O-CO-NH[CH(CH3)2], -O-CO-NH[C(CH3)3], -O-CO-N(CH3)2, -O-CO-N(C2H5)2, -O-CO-N(C3H7)2, -O-CO-N(C4H9)2, -O-CO-N(ciclo-C3H5)2, -O-CO-N[CH(CH3)2]2, -O-CO-N[C(CH3)3]2, (ii) un anillo aromático o heteroaromático mono- o bicíclico seleccionado de 2-tienil, 3-tienil, 2-furanil, 3-furanil, 2-oxazolil, 3-oxazolil, 4-oxazolil, 2-tiazolil, 3-tiazolil, 4-tiazolil, 1-pirazolil, 3-pirazolil, 4-pirazolil, 5-pirazolil, 1-imidazolil, 2-imidazolil, 4-imidazolil, 5-imidazolil, fenil, 1-naftil, 2-naftil, 2-piridil, 3-piridil, 4-piridil, 2-pirimidinil, 4-pirimidinil, 5-pirimidinil, 2-pirazinil, 3-piridazinil, 4-piridazinil, 1,3,5-triazin-2-iI, compuestos de formulas (7) que opcionalmente puede estar sustituido por uno o dos sustituyentes seleccionados de -F, -CI, -Br, -I, -OCH3, -CH3, -NO2, -CN, -CF3; (iii) un anillo saturado seleccionado de ciclopentil, acetidin-1-il, compuestos de formulas (8); R99 representa -H, -CH3, -CH2Ph, -COOC(CH3)3, -COOCH3, -COOCH2CH3, -COOCH2CH2CH3, -COOCH(CH3)2, -COOCH2Ph, -COCH3; el grupo -B-Y-R-R85 junto con un sustituyente R83 puede formar un grupo -OCH2O- si R83 está ligado en posicion orto a -B-Y-R-R85; a condicion de que R83 no sea -H si el grupo -B-Y-R84-R85 es hidrogeno; R98 se selecciona de -NO2, -CN, -F, -CI, -Br, -I, -NH2, -OH, -CR62R63R64, -CR62R63-CR65R66R64, -CR62R63-R65R66-C67R68R64, -CR62R63-CR65R66-CR67R68-CR69R70R64, -O-CR62R63R64, -O-CR62R63-CR65R66R64, -O-CR62R63-CR65R66-CR67R
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