AR064675A1 - Derivados heterociclicos de pirrolo- [2,3-b] piridina, inhibidores de proteinquinasas plk, composiciones farmaceuticas que los contienen, proceso de preparacion y uso de los mismos en trastornos hiperproliferativos - Google Patents

Derivados heterociclicos de pirrolo- [2,3-b] piridina, inhibidores de proteinquinasas plk, composiciones farmaceuticas que los contienen, proceso de preparacion y uso de los mismos en trastornos hiperproliferativos

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AR064675A1
AR064675A1 ARP070105844A ARP070105844A AR064675A1 AR 064675 A1 AR064675 A1 AR 064675A1 AR P070105844 A ARP070105844 A AR P070105844A AR P070105844 A ARP070105844 A AR P070105844A AR 064675 A1 AR064675 A1 AR 064675A1
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Argentina
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groups
optionally substituted
independently
alkyl
ring
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ARP070105844A
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Michael Mortimore
Guy Brenchley
Jean-Damien Charrier
Michael O'donnell
Stephen Clinton Young
Simon Robert Lorrie Everit
Ronald Knegtel
Joanne Louise Pinder
Alistair Peter Rutherford
Steven Durrant
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Vertex Pharma
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    • C07D403/04—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings directly linked by a ring-member-to-ring-member bond
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Abstract

Reivindicacion 1: Un compuesto de la formula (1): o una sal farmacéuticamente aceptable del mismo, caracterizado porque: R1 es -H, halogeno, un grupo alifático de C1-6 opcionalmente sustituido con 1-3 R3, un -O(grupo alifático de C1-6) opcionalmente sustituido con 1-3 R3, o -N(H)R; cada R es, independientemente, H, un grupo alifático de C1-6, arilo, heteroarilo, cicloalquilo de C3-8, o anillo heterocíclico de 4-12 miembros que opcionalmente contiene 1-3 grupos seleccionados entre -N(R)17-, -O-, o -S-; donde cada uno de los grupos alifático, arilo, heteroarilo, cicloalquilo, y el anillo heterocíclico están opcionalmente sustituidos con 1-3 grupos Q; cada Q es, independientemente, seleccionado entre halogeno, hidroxi, alquilo de C1-6, hencilo, oxo, -CF3, W, -CN, -NH2, -N(H)-W, -N(W)2, -N(H)-SO2-W, -S(O)2-N(H)-W, -S(O)2-N(W)2, -C(O)-W, -C(O)-N(W)2 , -N(H)-C(O)-W, -O-C(O)-W, -C(O)-O-W. -SO2-W, SW o OW; dos Q pueden estar unidos juntos para formar un anillo carbocíclico o heterocíclico de 4 a 8 miembros opcionalmente sustituido con alquilo de C1-3 o CF3; cada W se selecciona, independientemente, entre -H, alquilo de C1-6, aralquilo, cicloalquilo o un anillo heterocíclico; cada alquilo de C1-6, aralquilo o cicloalquilo o anillo heterocíclico está opcionalmente sustituido con 1-3 halogenos, -OR6, -CN alquilo de C1-6 o NR18R19; o un W, junto con el átomo de nitrogeno al que está ligado y un átomo de carbono de R, forman un anillo de 4 a 8 miembros; o dos W, junto con el mismo o diferente átomo de nitrogeno o carbono al que están unidos, forman un anillo heterocíclico de 4 a 8 miembros; o cada R18 y R19 junto con el átomo de nitrogeno al que están unidos, forman un anillo heterocíclico de 4 a 8 miembros, opcionalmente sustituido con alquilo de C1-3 o CF3; dos W pueden estar unidos juntos para formar un cicloalquilo heterocicloalquilo de 4 a 8 miembros, opcionalmente sustituido con alquilo de C1-3 o CF3; R2 es -NR4R5, -OR6, -SR6, o - NR10R11; cada R3 es, independientemente, halogeno, alquilo de C1-6, arilo, o heteroarilo; cada R4 es, independientemente, -H o un grupo alifático de C1-6 opcionalmente sustituido con 1-3 grupos R7; cada R5 es, independientemente, un grupo alifático de C1-6 opcionalmente sustituido con 1-4 grupos R7 o un anillo monocíclico de 3 a 8 miembros o bicíclico de 6 a 10 miembros opcionalmente sustituido con 1-4 grupos R7, o R4 y R5 pueden unirse juntos para formar un anillo monocíclico o bicíclico opcionalmente sustituido con 1-3 grupos R9; cada R6 es independientemente H, alquilo de C1-6, -L-arilo, o -L-heteroarilo, donde cada uno de alquilo de C1-6, -L-arilo, o -L-heteroarilo está opcional e independientemente sustituido con 1-3 grupos 1-3 R8; L es alquilo de C0-3; cada R7 es, independientemente, oxo, alquilo, halogeno, -CN, -OR9, -N(R9)2, cicloalquilo de C3-8, arilo, heteroarilo o un anillo heterocíclico de 4-8 miembros que contiene 1-3 grupos seleccionados entre -N(R)17-, -O-, o -S- , donde cada alquilo, cicloalquilo, anillo heterocíclico monocíclico o bicíclico de 4-8 miembros, arilo, y heteroarilo está opcional e independientemente sustituido con 1-3 grupos R8, o dos R7 en el mismo átomo o átomos adyacentes está unido para formar anillo carbocíclico o un anillo helerocíclico de 4-8 miembros que contiene 1-3 grupos seleccionados entre -N(R)17-, -O-, o -S-, donde cada uno del anillo carbocíclico y heterocíclico de 4-8 miembros está opcional e independientemente sustituido con 1-3 grupos R8; cada R8 es, independientemente, -R, -Q, -R9, -OR9, -N(R9)2, halogeno, o -CN; cada R9 es, independientemente, -H, -N(R16)2, anillo carbocíclico de C3-6, anillo heterocíclico de C3-6, o grupo alifático de C1-3, donde el anillo carbocíclico de C3-6, el anillo heterocíclico de C3-6 y el grupo alifático de C1-3 están opcionalmente sustituidos con 1-3 grupos Q; o dos grupos R9 junto con el átomo N al que están ligados forman un anillo de 4-8 miembros que contiene 1 o 2 grupos adicionales seIeccionados entre -N(R)17-, -O-, o -S-, donde el anillo de 4-8 miembros está opcional e independientemente sustituido con 1-3 grupos W; cada R16 es, independientemente, hidrogeno o alquilo de C1-6 o dos grupos R16 junto con el átomo N al que están ligados, forman un anillo de 4-8 miembros que contiene 1 o 2 grupos seleccionados entre NR17, O, o S; cada R17 es, independientemente, hidrogeno, Q1 o un grupo alifático o cicloalifático de C1-4, donde cada grupo alifático o cicloalifático de C1-4 está opcionalmente sustituido con 1-3 grupos Q; Q1 es C1-6 alquilo, bencilo, -SO2-W, -S(O)2-N(H)-W, -S(O)2-N(W)2 -C(O)-W, -C(O)-N(W)2, -C(O)-N(H)-W, -N(H)-C(O)-W, -O-C(O)-W, -C(O)-O-W, o -SO2-W; R10 es -H o un grupo alifático de C1-6 opcionalmente sustituido con 1-3 grupos R7; R11 es -C(R12R13)C(=O)NR14R15; cada R12 y R13 es, independientemente, H o un grupo alifático de C1-6 opcionalmente sustituido con 1-3 grupos R7; o R12 y R13 pueden unirse para formar un anillo opcionalmente sustituido con 1-3 grupos R9; o R10 y R12 pueden unirse para formar un anillo opcionalmente sustituido con 1-3 grupos R9; y cada R14 y R15 es, independientemente, H, alquilo de C1-6, un grupo carbocíclico o heterocíclico opcionalmente sustituido con 1-3 grupos R7; o R14 y R15 pueden unirse para formar un anillo opcionalmente sustituido con 1-3 grupos R9.
ARP070105844A 2006-12-21 2007-12-21 Derivados heterociclicos de pirrolo- [2,3-b] piridina, inhibidores de proteinquinasas plk, composiciones farmaceuticas que los contienen, proceso de preparacion y uso de los mismos en trastornos hiperproliferativos AR064675A1 (es)

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US87630706P 2006-12-21 2006-12-21
US92229107P 2007-04-06 2007-04-06
US94770707P 2007-07-03 2007-07-03
US98901407P 2007-11-19 2007-11-19

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JP4705695B2 (ja) 2007-10-11 2011-06-22 アストラゼネカ アクチボラグ プロテインキナーゼｂ阻害剤としてのピロロ［２，３−ｄ］ピリミジン誘導体
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