AR040031A1 - Compuestos de pirazol-pirimidina anilina utiles como inhibidores de cinasa y composiciones farmaceuticas que los contienen - Google Patents

Compuestos de pirazol-pirimidina anilina utiles como inhibidores de cinasa y composiciones farmaceuticas que los contienen

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Publication number
AR040031A1
AR040031A1 ARP030101712A ARP030101712A AR040031A1 AR 040031 A1 AR040031 A1 AR 040031A1 AR P030101712 A ARP030101712 A AR P030101712A AR P030101712 A ARP030101712 A AR P030101712A AR 040031 A1 AR040031 A1 AR 040031A1
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AR
Argentina
Prior art keywords
alkyl
heteroaryl
substituted
heterocycle
hydroxy
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Application number
ARP030101712A
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English (en)
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Bristol Myers Squibb Co
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Publication date
Application filed by Bristol Myers Squibb Co filed Critical Bristol Myers Squibb Co
Publication of AR040031A1 publication Critical patent/AR040031A1/es

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    • 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
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Abstract

Los compuestos que tiene la fórmula (1). Estos compuestos son útiles como inhibidores de la cinasa p38 en un mamífero. También se presentan composiciones farmacéuticas que contienen los compuestos de fórmula (1) y métodos de tratamiento. Reivindicación 1: Un compuesto que tiene la fórmula (1) o sal, profármaco, o solvato farmacéuticamente aceptable del mismo, en donde: Y es -C(=O)NR1-, -NR1C(=O)-, NR1C(=O)NR1-, NR1SO2-, -SO2NR1-,-C(=O)-, -OC(=O)-, o -CO2-; B se selecciona de alquilo, alquilo sustituido, alquenilo, alquenilo sustituido, hidroxi, alcoxi, arilo, cicloalquilo, heteroarilo, y heterociclo; o cuando Y es -C(=O)NR1-, B también puede seleccionarse de -C(=O)R8-, C(=O)NR8R9, y -CO2R8, R1 es H, alquilo C1-4, o alquilo C1-4 sustituido; R2 es H o alquilo C1-4; R3 es H, metilo, perfluorometilo, hidroxi, metoxi, halógeno, ciano, NH2 o NH(CH3);- R4 es H, alquilo, alquilo sustituido, alquenilo, alquenilo sustituido, arilo, cicloalquilo, heteroarilo o heterociclo; R5 se selecciona de H, halógeno, ciano, alquilo, alquilo sustituido, -C(=O)R11, -CO2R11, -S(=O)R12, -SO2R12, -SO3R12, -OR11, -SR11, -NR11R12, -C(=O)NR11R12; NR11C(=O)R12, NR11CO2R12, -NR11SO2R12, -SO2NR11R12, cicloalquilo, arilo, heterociclo y heteroarilo; R6 se selecciona de halógeno, ciano, nitro, A1-R13, -A1-O-A2-R13, -A1-S-A2-R13, -A1-C(=O)-A2-R13, -A1-OC(=O)-A2-R13, -A1-S(=O)-A2-R13, -A1-SO2A2-R13, -A1-CO2-A2-R13, -A1-NR13-A2-R14, -A1-NR15C(=O)-A2-R13, -A1-NR15C(=O)NR16-A2-R13, -A1-NR15CO2-A2-R13, -A1-NR15SO2-A2-R13, -A1-NR15SO2NR16-A2-R13, -A1-SO2NR15-A2-R13, y -A1-C(=O)NR15-A2-R13; A1 es - (CR17R18)r-; A2 es -(CR19R20)s-; R8 y R9 se seleccionan de H, alquilo, alquilo sustituido, arilo, cicloalquilo, heteroarilo, y heterociclo, o cuando se enlazan al mismo átomo de N, pueden formar juntos un anillo heteroarilo o heterociclo; R11, R12, R13 y R14 se seleccionan de H, alquilo, alquilo sustituido, alquenilo, alquenilo sustituido, arilo, cicloalquilo, heteroarilo, y heterociclo, o cuando se enlazan al mismo átomo de N, pueden formar un anillo heteroarilo o heterociclo, con la condición de que cuando R12 o R13 se enlaza a un grupo sulfonilo (como en -S(=O)R12, -SO2R12, -SO3R12, -A1-S(=O)R13, -A1-SO2R13, y -A1-SO3R13), R12 y R13 no son H; R15 y R16 se seleccionan de H, alquilo C1-4, hidroxi, hidroxi alquilo C1-4, y amino alquilo C1-4; R17, R18, R19, y R20 se seleccionan de H, alquilo C1-4, halógeno, ciano, hidroxi, hidroxi alquilo C1-4, halo alquilo C1-4, haloalcoxi C1-4, amino, alquilamino C1-4, y amino alquilo C1-4; m es 0,1, o 2, y r y s se seleccionan de 0, 1, 2, 3, y 4.
ARP030101712A 2002-05-20 2003-05-16 Compuestos de pirazol-pirimidina anilina utiles como inhibidores de cinasa y composiciones farmaceuticas que los contienen AR040031A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US38201402P 2002-05-20 2002-05-20

Publications (1)

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AR040031A1 true AR040031A1 (es) 2005-03-09

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US (1) US6962915B2 (es)
EP (1) EP1507780B1 (es)
JP (1) JP2005531584A (es)
AR (1) AR040031A1 (es)
AU (1) AU2003241561A1 (es)
ES (1) ES2391948T3 (es)
IS (1) IS7534A (es)
MY (1) MY135309A (es)
NO (1) NO20044866L (es)
PE (1) PE20040512A1 (es)
PL (1) PL374218A1 (es)
TW (1) TW200400034A (es)
WO (1) WO2003099820A1 (es)

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KR100844864B1 (ko) 2004-02-27 2008-07-09 에프. 호프만-라 로슈 아게 헤테로아릴-융합 피라졸로 유도체
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