AR042052A1 - Diaminotriazoles utiles como inhibidores de proteinquinasas - Google Patents

Diaminotriazoles utiles como inhibidores de proteinquinasas

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Publication number
AR042052A1
AR042052A1 ARP030104218A ARP030104218A AR042052A1 AR 042052 A1 AR042052 A1 AR 042052A1 AR P030104218 A ARP030104218 A AR P030104218A AR P030104218 A ARP030104218 A AR P030104218A AR 042052 A1 AR042052 A1 AR 042052A1
Authority
AR
Argentina
Prior art keywords
phenyl
unsubstituted
substituted
optionally substituted
formula
Prior art date
Application number
ARP030104218A
Other languages
English (en)
Inventor
Albert C Pierce
Michael Arnost
Robert J Davies
Cornelia J Forster
Vicent Galullo
Ronald Grey
Mark Ledeboer
Shi-Kai Tian
Jinwang Xu
Hayley Binch
Original Assignee
Vertex Pharma
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Vertex Pharma filed Critical Vertex Pharma
Publication of AR042052A1 publication Critical patent/AR042052A1/es

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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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    • C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/04—Ortho-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D495/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms
    • C07D495/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
    • C07D495/04—Ortho-condensed systems

Abstract

La presente se refiere a diaminotriazoles útiles como inhibidores de proteinazas. También provee composiciones farmacéuticas que comprenden compuestos y métodos para usar dichas composiciones en el tratamiento de varios desórdenes. Reivindicación 1: Un compuesto de fórmula (1) o un sal farmacéutica aceptable de la misma, en la cual R1 es H o Y-R1, donde Y es una cadena de alquilideno opcionalmente sustituida C1-6 en la cual hasta dos unidades metileno están opcionalmente e independientemente reemplazada por -O-, -S-, -NR-, -OCO-, -COO-, o -CO-; cada ocurrencia de R es independientemente H o un grupo alifático C1-6 opcionalmente sustituido; y cada ocurrencia de R´ es independientemente H o un grupo opcionalmente sustituido seleccionado entre un grupo alifático C1-6, un anillo monocíclico de 3-8 miembros, saturado parcialmente insaturado o plenamente insaturado que tiene 0.3 heteroátomos independientemente seleccionados entre N, O, o S, o un anillo bicíclico de 8-12 miembros saturado, parcialmente insaturado plenamente insaturado que tiene 0-5 heteroátomos independientemente seleccionados entre N, O, o S; o R y R¨, son tomadas conjuntamente con el (los) átomo (s) a los cuales están ligada para formar un anillo monocíclico o bicíclico de 3-12 miembros opcionalmente sustituido, saturado, parcialmente insaturado o totalmente insaturado que tiene 0-4 heteroátomos seleccionados independientemente entre N, O, o S; R2 es -(T)nAr1, o -(T)uCy1, donde T es opcionalmente una cadena de alquilideno C14 opcionalmente sustituida donde una unidad metileno de T está opcionalmente reemplazada por -NR-, -S-, -O-, -CS-, -CO2, -OCO-, -CO-, -COCO-, -CONR-, -NRCO, -NRCO2-, SO2NR-, -NRSO2-, -CONRNR-, -NRCONR-, -OCONR-, -NRNR-, -NRSO2NR-, -SO-, -SO2-, -PO-, -PO2-, o -POR-; n es 0 o 1; Ar1 es un grupo arilo opcionalmente sustituido, seleccionado entre un anillo monocíclico de 5-6 miembros o un anillo bicíclico de 8-12 miembros que tienen 0-5 heteroátomos seleccionados independientemente seleccionados entre N, O o S; y Cy1 es un grupo opcionalmente sustituido seleccionado entre un anillo monocíclico de 3-7 miembros que tiene 0-3 heteroátomos seleccionados independientemente entre N, O, o S, o un anillo bicíclico de 8-12 miembros saturado o parcialmente insaturado que tiene 0-5 heteroátomos independientemente seleccionados entre N, O, o S; o R1 y R2 tomados conjuntamente con el N forman un anillo heterocíclico o heteroarílico de 5-8 miembros que tiene 1-3 heteroátomos independientemente seleccionados entre N, O, y S; donde Ar1, Cy1, o cualquier anillo formado por R1 y R2 tomados conjuntamente, están cada uno independientemente y opcionalmente sustituidos con X ocurrencias independientes de Q-Rx, donde x es de 0-5. Q es un enlace o es una cadena alquilideno C1-6 donde hasta dos unidades metileno de Q están opcionalmente reemplazadas por: -NR-, -S-, -O-, -CS-, -CO2-, -OCO-, -CO-, -COCO-, -CONR-, -NRCO-, -NRCO2-, -SO2NR-, -NRSO2-, -CONRNR-, -NRCONR-, -OCONR-, -NRNR-, -NRSO2NR-, -SO-, -SO2-, -PO-, -PO2-, o -POR-; y cada ocurrencia de Rx es independientemente R´, halógeno, -NO2-, -CN-, -OR-´-SR´-, -N(R´)2, -NR´COR´, -NR´CONR´2-, NR´CO2R´, COR´, -CO2R´, -OCOR´, CON(R´)2, -OCON(R´)2-, SOR´, -SO2R´, -SO2N(R´)2, NR´SO2R´, NR´SO2N(R´)2, COCOR´, o COCH2COR´, R3 está ligado al átomo de N en la posición 1- o 2- del anillo y es (L)mAr2, o (L)mCy2 donde L está opcionalmente reemplazado por -NR-, -S-, -O-, -CS-, -CO2, -OCO-, -CO-, -COCO-, -CONR-, -NRCO, -NRCO2-, SO2NR-, -NRSO2-, -CONRNR-, -NRCONR-, -OCONR-, -NRNR-, -NRSO2NR-, -SO-, -SO2-, -PO-, -PO2-, o -POR-; m es 0+ o 1; Ar2 es un grupo arilo opcionalmente sustituido seleccionado entre un anillo monocíclico de 5-6 miembros o un anillo bicíclico de 8-12 miembros que tiene 0-5 heteroátomos seleccionados independientemente entre N, O, o S; y Cy2 es un grupo opcionalmente sustituido seleccionado entre un anillo monocíclico de 3-7 miembros saturado o parcialmente insaturado que tiene 0-3 heteroátomos seleccionados independientemente entre N, O, o S, donde Ar2 y Cy2 son, cada R´ uno, independientemente y opcionalmente sustituidos con y ocurrencias de Z-Ry, donde Y es 0-5, Z es un enlace o es una cadena alquilideno C1-6 donde hasta dos unidades metileno de Z están opcionalmente reemplazadas por -NR-, -S-, -O-, -CS-, -CO2-, -OCO-, -CO-, -COCO-, -CONR-, -NRCO-, -NRCO2, -SO2NR-, -NRSO2-, -CONRNR-, -NRCONR-, -OCONR-, -NRNR-, -NRSO2NR-, -SO-, -SO2-, -PO-, -PO2-, o -POR-; y cada ocurrencia de Ry es independiente R´, halógeno, -NO2, -CN, -OR-´, -SR´-, -N(R´)2, -NR´COR´, -NR´CONR´2-, NR´CO2R´, COR´, -CO2R´, -OCOR´, CON(R´)2, -OCON(R´)2-, SOR´, -SO2R´, -SO2N(R´)2, NR´SO2R´, NR´SO2N(R´)2, COCOR´, o COCH2COR´; R4 es H o alquilo C1-6 siempre que cuando R5 es H, R4 es también H; R5 es H, o R3 y R5, tomados conjuntamente forman un grupo opcionalmente sustituido seleccionado entre un anillo monocíclico de 5-7 miembros, saturado, parcialmente insaturado o completamente insaturado que tiene 0-3 heteroátomos independientemente seleccionados entre N, O, o S, o un sistema de anillo bicíclico de 8-10 miembros saturado, parcialmente insaturado o completamente insaturado que tiene 0-3 heteroátomos independientemente seleccionados entre N, O, o S; y donde cualquier anillo formado por R3 y R5 tomados conjuntamente, está opcionalmente sustituido con hasta cinco sustituyentes seleccionados entre W-Rw donde W es un enlace o es una cadena alquilideno C1-6 donde hasta dos grupos metileno de W son opcionalmente e independientemente reemplazados por -NR-, -S-, -O-, -CS-, -CO2, -OCO-, -CO-, -COCO-, -CONR-, -NRCO, -NRCO2-, SO2NR-, -NRSO2-, -CONRNR-, -NRCONR-, -OCONR-, -NRNR-, -NRSO2NR-, -SO-, -SO2-, -PO-, -PO2-, o -POR-; y cada ocurrencia de Rw es independientemente R´, halógeno, -NO2, -CN, -OR-´, -SR´-, -N(R´)2, -NR´COR´, -NR´CONR´2-, NR´CO2R´, COR´, -CO2R´, -OCOR´, CON(R´)2, -OCON(R´)2-, SOR´, -SO2R´, -SO2N(R´)2, NR´SO2R´, NR´SO2N(R´)2, COCOR´, o COCH2COR´; siempre que: (a) cuando R3 es fenilo no sustituido y R´ es H, entonces R2 no es i) fenilo no sustituido, ii) piridilo no sustituido, iii) bencilo sustituido con O- OMe; iv) -(C=S)NH (C=O) fenilo; o v) como se muestra en el resto de fórmula (2), vi) -(C=S)NH-naftilo o -(C=O)NH-naftilo; o b) cuando R3 es fenilo sustituido o no sustituido, entonces R3 no es fenilo sustituido en la posición para con oxazol, trazol, tiadiazol, oxadiazol, tetrazol, triazol, diazol, orpirrol; c) cuando R3 es fenilo, piridilo, pirimidineodiona, o ciclohexilo, y R1 es H, entonces R2 no es fenilo simultáneamente sustituido con una ocurrencia de OMe en la posición meta, y una ocurrencia de oxazol en la posición para; d) cuando R3 es p-Cl fenilo, entonces R2 no es p-Cl-fenilo; e) cuando R3 es pirimidinil no sustituido, entonces R2 no es fenilo no sustituido, fenil sustituido con p-OMe, fenil sustituido con p-OEt o fenil sustituido con o-OMe, o cuando R3 es 4-Me pirimidinil o 4,6-dimetil pirimidinil, entonces o 4,6-dimetilpirimidinil, entonces R2 no es fenil no sustituido; f) cuando R2 es 3-piridimil y R1 es H, entonces R3 no es trimetoxibenzoil; g) cuando R3 es opcionalmente fenil sustituido y R1 es H, entonces R2 no es -(C=S)NH(C=O)fenil, -(C=O)NHfenil, -(C=S)NHfenil, o -(C=O)CH2(C=O)fenil; h) cuando R1 es H, R2 es bencilo no sustituido entonces R3 no es triadiazol sustituido con fenilo opcionalmente sustituido; i) cuando R1 es H, R2 es piridil, y R3 es piridil, entonces R2 no está sustituido con uno o más de CD3, Me, OMe, Br, o Cl; j) cuando R1 es H, R2 es piridilo, entonces R3 no es piridil no sustituido, quinolina no sustituida, fenilo no sustituido, o isoquinolina no sustituida; k) cuando R1 es H y R2 es quinolina no sustituida, entonces R3 no es piridilo no sustituido o quinolina no sustituida; e) cuando R1 es H y R2 es quinolina no sustituida o naftilo no sustituido, entonces R1 no es piridilo no sustituido; m) los compuestos de fórmula (1) excluyen aquellos componentes que tienen la fórmula general (3), donde R1, R2, y R3 son como se definió arriba, M y K son 0 o H2 siempre que K y M serán diferentes, A y B son cada uno -CH2, -N-alquilo-, -N-aralquilo-, -NCORa, -NCONHRb, o -NCSNHRb, donde Ra es alquilo o aralquilo inferior y Rb es alquilo, aralquilo o arilo de cadena recta o ramificada que pueden ser o uno sustituidos o con uno o más sustituyentes alquilos o haloalquilo; n) los compuestos de fórmula (1) excluyen aquellos que tienen la estructura general (4), donde R1 y R2 son según se definió arriba y r y s son, cada uno, independientemente 0, 1, 2, 3, o 4 siempre que la suma de s y r sea al menos 1; o) los compuestos de fórmula (1) excluyen uno o más de los siguientes compuestos de fórmulas (5) a (9), donde R2 es NH(CH)(Ph)C=O(Ph); o como se muestra en la fórmula (10) donde R2 es fenilo no sustituido o fenilo sustituido con OMe, Cl, o Me., como se muestra en la fórmula (11) donde R2 es fenilo no sustituido o fenilo sustituido con OMe, Cl, o Me; o R2 es bencilo no sustituido. Como se muestra en la fórmula (12) donde R2 es opcionalmente aralquilo y Rc y Rd son cada uno independiente Me, H, CH2Cl o Cl, como se muestra en el grupo de fórmulas (13) a (16) donde R2 es fenilo opcionalmente sustituido con Me, OMe, Br o Cl, o como se muestra en la fórmula (17) p) los compuestos de fórmula (1) excluyen uno o más, o todos los siguientes compuestos: i) cuando R1 es H y R2 es fenilo o fenilo opcionalmente sustituido y m es 1, entonces L no es (C=O), (C=S), (CO)NR, (CS)NR, SO2, (SO2)NR, (CO)SO2 o (CS)SO2 o q) los compuestos de fórmula (1) excluyen uno o más o todos los siguientes compuestos pertenecientes al grupo de fórmulas (18) a (23).
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