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AR044502A1 - Quinazolinas utiles como moduladores de canales ionicos - Google Patents

Quinazolinas utiles como moduladores de canales ionicos

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Publication number
AR044502A1
AR044502A1 ARP040100670A ARP040100670A AR044502A1 AR 044502 A1 AR044502 A1 AR 044502A1 AR P040100670 A ARP040100670 A AR P040100670A AR P040100670 A ARP040100670 A AR P040100670A AR 044502 A1 AR044502 A1 AR 044502A1
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AR
Argentina
Prior art keywords
ring
phenyl
unsubstituted
taken together
optionally substituted
Prior art date
Application number
ARP040100670A
Other languages
English (en)
Inventor
Jesus E Gonzales Iii
Dean Mitchell Wilson
Andreas Peter Termin
Peter Diederik Jan Grootenhuis
Yulian Zhang
Benjamin John Petzsoldt
Lev Tyler Dewey Fanning
Timothy Donald Neubert
Roger D Tung
Original Assignee
Vertex Pharma
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Publication date
Application filed by Vertex Pharma filed Critical Vertex Pharma
Publication of AR044502A1 publication Critical patent/AR044502A1/es

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    • C07D239/72—Quinazolines; Hydrogenated quinazolines
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    • C07D239/86—Quinazolines; Hydrogenated quinazolines with hetero atoms directly attached in position 4
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Abstract

Se provee también composiciones farmacéuticamente aceptables y métodos para usar las composiciones en el tratamiento de varios trastornos. Reivindicación 1: Un compuesto de fórmula (1), o una sal farmacéuticamente aceptable del mismo, caracterizado porque: R1 y R2, tomados conjuntamente con el átomo de nitrógeno al cual están ligados, forman un anillo monocíclico o bicíclico de 3-12 miembros opcionalmente substituido saturado, parcialmente no saturado, o completamente no saturado que tiene de 0-3 heteroátomos adicionales seleccionados independientemente entre nitrógeno, azufre, u oxígeno; donde el anillo formado por R1 y R2 tomados conjuntamente, es opcionalmente substituido en uno o más átomos substituibles de carbono, nitrógeno, o azufre con z ocurrencias independientes de -R4, donde z es 0-5; el anillo A es un anillo arilo monocíclico de 5-7 miembros o un anillo arilo bicíclico de 8-10 miembros que tiene 0-3 heteroátomos seleccionados independientemente entre nitrógeno, oxígeno, o azufre, o es un anillo monocíclico de 3-8 miembros saturado o parcialmente no saturado que tiene 0-3 heteroátomos independientemente seleccionados entre nitrógeno, oxígeno, o azufre, donde el anillo A está opcionalmente substituido con y ocurrencias independientes de -R5, donde y es 0-5, y adicionalmente está opcionalmente substituido con q ocurrencias independientes de R5a, donde q es 0-2; x es 0-4; cada ocurrencia de R3, R4, y R5 es independientemente Q-RX; donde Q es una ligadura o es una cadena de alquilideno C1-6 donde hasta dos unidades de metileno no adyacente de Q están reemplazados opcionalmente e independientemente por -NR-, -S-, -O-, -CS-, -CO2-, -OCO-, -CO-, -COCO-, -CONR-, -NRCO-, -NRCO2-, -SO2NR-, -NRSO2-, -CONRNR- , -NRCONR-, -OCONR-, -NRNR-, -NRSO2NR-, -SO-, -SO2-, -PO-, -PO2-, -OP(O)(OR)-, o -POR-; y cada ocurrencia de Rx es seleccionada independientemente entre -R', halógeno, =O, -NR', -NO2, -CN, -OR', -SR', -N(R')2, -NR'COR', -NR'CON(R')2, -NR'CO2R', - COR', -CO2R', -OCOR', -CON(R')2, -OCON(R')2, -SOR', -SO2R', -SO2N(R')2, -NR'SO2R', -NR'SO2N(R')2, -COCOR', -COCH2COR', -OP(O)(OR')2, -P(O)(OR')2, -OP(O)2OR', -P(O)2OR', -PO(R')2, o -OPO(R')2; y cada ocurrencia de R5a es independientemente un grupo alifático C1-6 opcionalmente substituido, halógeno, -OR', -SR', -N(R')2, -NR'COR', -NR'CON(R')2, -NR'CO2R', -COR', -CO2R', -OCOR', -CON(R')2, -OCON(R')2, -SOR', -SO2R', -SO2N(R')2, -NR'SO2R', -NR'SO2N(R')2, -COCOR', -COCH2COR', -OP(O)(OR')2, - P(O)(OR')2, -OP(O)2OR', -P(O)2OR', -PO(R')2, o -OPO(R')2; y cada ocurrencia de R es independientemente hidrógeno o un grupo alifático C1-6 opcionalmente substituido; y cada ocurrencia de R' es independientemente hidrógeno o un grupo alifático C1-6 opcionalmente substituido, un anillo monocíclico de 3-8 miembros saturado, parcialmente no saturado, o completamente no saturado que tiene de 0-3 heteroátomos independientemente seleccionados entre nitrógeno, oxígeno, o azufre, o un sistema de anillo bicíclico de 8-12 miembros saturado, parcialmente no saturado, o completamente no saturado que tiene de 0-5 heteroátomos independientemente seleccionados entre nitrógeno, oxígeno, o azufre; o R y R', dos ocurrencias de R, o dos ocurrencias de R', son tomados conjuntamente con el átomo (los átomos) al cual (a los cuales) están ligados, forman un anillo monocíclico o bicíclico de 3-12 miembros opcionalmente substituido saturado, parcialmente no saturado, o completamente no saturado que tiene de 0-4 heteroátomos independientemente seleccionados entre nitrógeno, oxígeno, o azufre; con la condición de que: a. cuando R1 y R2, tomados conjuntamente con el átomo de nitrógeno al cual están ligados, forman un anillo monocíclico de 4 miembros opcionalmente substituido saturado o parcialmente no saturado que tiene 0-3 heteroátomos adicionales independientemente seleccionados entre nitrógeno, azufre, u oxígeno; entonces se excluye 2-oxazolidinona, 3-[(3R,4R)-2-oxo-1-(2-fenil-4- quinazolinil)-4-[2-(3-piridinil)etinil]-3-azetidinil]-4-fenil-, (4S)-; b. cuando R1 y R2, tomados conjuntamente con el átomo de nitrógeno al cual están ligados, forman un anillo monocíclico de 5 miembros opcionalmente substituido saturado o parcialmente no saturado que tiene 0-3 heteroátomos adicionales independientemente seleccionados entre nitrógeno, azufre, u oxígeno; entonces: i. el anillo A no es hexahidro-1H-1,4-diazepin-1-ilo opcionalmente substituido; y ii. se excluyen bencensulfonamida, 2-metoxi-5-[2-[[1-(2-fenil-4-quinazolinil)-3-pirrolidinil]amino]etil]-, (R)-, bis(trifluoroacetato), y bencensulfonamida, 2-metoxi-5-[2-[[1-(2-fenil-4-quinazolinil)-3-pirrolidinil]amino]etil]-, (S)-, bis(trifluoroacetato); iii. se excluyen 3-pirrolidinamina, 1-(2-fenil-4-quinazolinil)-, y (R)-3-pirrolidinamina, 1-(2-fenil-4-quinazolinil)-, (S)-; iv. cuando R1 y R2, tomados conjuntamente son pirrolidin-1-ilo no substituido, el anillo A es fenilo no substituido, y x es 1, entonces R3 no es 6-OMe o 6-OH; v. cuando R1 y R2, tomados conjuntamente son pirrolidin-1-ilo, el anillo A es fenilo no substituido, y x es 2, entonces los dos grupos R3 no son 6-OMe y 7-OMe; vi. cuando R1 y R2, tomados conjuntamente son pirrolidin- 1-ilo no substituido, entonces el anillo A no es pirrolidin-1-ilo no substituido, piperazin-1-ilo opcionalmente substituido, morfolin-1-ilo no substituido; o piperidin-1-ilo no substituido; vii. cuando R1 y R2, tomados conjuntamente son pirrolidin-1- ilo, x es 0 y el anillo A es fenilo no substituido, entonces el grupo pirrolidin-1-ilo no está substituido en la posición 3 con -OH o 2-metoxi-fenoxi; viii. cuando R1 y R2, tomados conjuntamente son pirrolidin-1-ilo no substituido, y x es 0, entonces el anillo A no es 2,3-xililo, 3-metilfenilo, fenilo no substituido, 4-bromo-fenilo, 4-cloro-fenilo, 3-nitro-fenilo, pirid-3-ilo no substituido, 2,4-diclorofenilo, 3,4-diclorofenilo, 4-propoxifenilo, 3-metilfenilo, 3,4,5-trimetoxifenilo, 2- clorofenilo, pirid-4-ilo no substituido, 2-hidroxifenilo, o 4-(1,1-dimetiletil)fenilo; c. cuando R1 y R2, tomados conjuntamente con el átomo de nitrógeno al cual están ligados, forman un anillo monocíclico o bicíclico de 6 miembros opcionalmente substituido saturado o parcialmente no saturado que tiene 0-3 heteroátomos adicionales independientemente seleccionados entre nitrógeno, azufre, u oxígeno; entonces: i. cuando R1 y R2, tomados conjuntamente forman un anillo morfolino no substituido, y el anillo A es fenilo no substituido, entonces x no es 0, o si x es 1 o 2, entonces R3 no es: 6-fluoro, 6,7-dimetoxi, 6-nitro, 6-AcHN-, 6-metox, 6-NH2, 6-OCHN-, 6-OH, 6-AcMeN-, 6-TsHN-, 6-Me2N-, 7-OH, 6-amino-tiazol-2-ilo, 6-NHCOCOOEt, o 6-(4- fenil-amino-tiazol-2-ilo); ii. cuando R1 y R2, tomados conjuntamente forman un anillo morfolino no substituido, y el anillo A es ciclohexilo no substituido, pirid-3-ilo no substituido, 2-furilo no substituido, 2-fluorofenilo, 3-tienilo, benzofurano, piridazina, fenilo substituido en una o más de las posiciones 3, 4, o 5 del anillo fenilo, y x es 1 o 2, entonces R3 no es 6-NH2, 6-OHCHN-, 6-OH, 7-OH, 6-MsHN-, 6-AcHN-, 6-fluoro, o 6-OMe; iii. cuando R1 y R2, tomados conjuntamente, forman piperid-4- ona, piperid-4-ol, o tiomorfolino, o un anillo morfolino dimetil substituido, el anillo A es fenilo no substituido, y x es 1, entonces R3 no es 6-OH; iv. cuando x es 0 y A es fenilo no substituido, 3,4,5-trimetoxifenilo, o 3,4-dimetoxifenilo, entonces R1 y R2, tomados conjuntamente no son piperidinilo opcionalmente substituido o piperazinilo opcionalmente substituido; v. cuando x es 2 o 3, y R3 es 6,7-diOMe, o 6,7,8-triOMe, entonces R1 y R2, tomados conjuntamente no son piperidin-1-ilo opcionalmente substituido, piperazin-1-ilo, o morfolin-1-ilo; vi. cuando x es 0 y el anillo A es fenilo no substituido, entonces R1 y R2 tomados conjuntamente no son piperazinilo opcionalmente substituido o fusionado; vii. cuando x es 0 y el anillo A es fenilo opcionalmente substituido en una o más de las posiciones 3, 4, o 5 del anillo fenilo, entonces R1 y R2, tomados conjuntamente no son piperazin-1-ilo opcionalmente substituido, o morfolin-1-ilo; viii. cuando x es 0 y el anillo A es 2-F- fenilo, entonces R1 y R2, tomados conjuntamente no son 4-(2-Cl-fenil)-piperazin-1-ilo, 4-(3-Cl-fenil)-piperazin-1-ilo, o morfolin-1-ilo no substituido; ix. cuando x es 0 y el anillo A es 2-Cl-fenilo, entonces R1 y R2, tomados conjuntamente no son morfolin-1-ilo no substituido, 4-Me-piperazin-1-ilo, 4-Et-piperazin-1-ilo, 4-fenil-piperazin-1-ilo, o 4-CH2-(fenil)2-piperazin-1-ilo; x. cuando x es 0 y el anillo A es 2-OH-fenilo, entonces R1 y R2, tomados conjuntamente no son morfolin-1-ilo no substituido, 4-(2-OMe-fenil)-piperazin-1-ilo, 4-CH2-fenil-piperazin-1-ilo, 4-Et-piperazin-1-ilo, o 4-Me-piperazin-1-ilo; xi. cuando x es 0, x es 1 y R3 es 6-Br, o x es 2 y R3 es 6-7-diOMe, y el anillo A es 2- o 3-tienilo opcionalmente substituido, entonces R1 y R2, tomados conjuntamente no son 4-fenil-piperazin-1-ilo, 4-(3-CF3-fenil)-piperazin-1-ilo, 4-(2-OEt-fenil)-piperazin-1-ilo, 4-Me-piperazinilo, o morfolin-1-ilo no substituido; xii cuando x es 0, y el anillo A es pirid-3-ilo o pirid-4- ilo no substituido, entonces R1 y R2, tomados conjuntamente no son morfolin-1-ilo opcionalmente substituido, o piperazin-1-ilo opcionalmente substituido; xiii. cuando x es 0, y el anillo A es 1H-imidazol-2-ilo o 1H-imidazol-1-ilo opcionalmente substituido, entonces R1 y R2 tomados conjuntamente no son morfolin-1-ilo no substituido, 4-Me-piperazin-1-ilo, o 4-CH2CH2OH-piperazin-1-ilo; xiv. cuando x es 0 y el anillo A es 5-NO2-tiazol-2-ilo, entonces R1 y R2, tomados conjuntamente no son 4-Me- piperazin-1-ilo; xv. cuando x es 0 y el anillo A es 5-NO2-2-furanilo, entonces R1 y R2, tomados conjuntamente no son 4-CH2CH2OH-piperazin-1-ilo, 4-Me-piperazin-1-ilo, o morfolin-1-ilo no substituido; xvi. cuando x es 1, R3 es 6-OH y el anillo A es fenilo no substituido, entonces R1 y R2, tomados conjuntamente no son morfolin-1-ilo no substituido, o 4-Me-pipe
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EP1608632A1 (en) 2005-12-28
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US8343980B2 (en) 2013-01-01
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