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AR042398A1 - Compuestos de pirazol utiles como inhibidores de proteinquinasa - Google Patents

Compuestos de pirazol utiles como inhibidores de proteinquinasa

Info

Publication number
AR042398A1
AR042398A1 ARP010105961A ARP010105961A AR042398A1 AR 042398 A1 AR042398 A1 AR 042398A1 AR P010105961 A ARP010105961 A AR P010105961A AR P010105961 A ARP010105961 A AR P010105961A AR 042398 A1 AR042398 A1 AR 042398A1
Authority
AR
Argentina
Prior art keywords
ring
so2n
con
nitrogen
substituted
Prior art date
Application number
ARP010105961A
Other languages
English (en)
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 AR042398A1 publication Critical patent/AR042398A1/es

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Abstract

Un compuesto de pirazol Ăștil como inhibidor de proteinquinasa que responde a la fĂłrmula (1), o un derivado o prodroga farmacĂ©uticamente aceptable del mismo, en donde: Rx y Ry son tomados conjuntamente con los ĂĄtomos a los cuales estĂĄn unidos para formar un anillo fusionado de 5-7 miembros, no saturado p particularmente no saturado, que tiene 0-3 heteroĂĄtomos en el anillo seleccionados entre oxĂ­geno, azufre o nitrĂłgeno, en donde cualquier carbono sustituible de dicho anillo fusionado formado por Rx y Ry estĂĄ sustituido por oxo, T-R3 Ăł L-Z-R3, y cualquier nitrĂłgeno sustituible de dicho anillo formado por Rx y Ry estĂĄ sustituido por R4; R1 es T-(anillo D); el anillo D es un anillo monocĂ­clico de 5-7 miembros o un anillo bicĂ­clico de 8-10 miembros seleccionados entre arilo, heteroarilo, heterociclilo o carbociclilo, teniendo dicho anillo heteroarilo o heterociclilo 1-4 heteroĂĄtomos en el anillo seleccionados entre nitrĂłgeno, oxĂ­geno o azufre, en donde el anillo D estĂĄ sustituido en cualquier ĂĄtomo de carbono sustituible del anillo por oxo, T-R5. o V-Z-R5, y en cualquier ĂĄtomo de nitrĂłgeno sustituible del anillo D -R4; T es una ligadura de valencia o una de cadena de alquilideno C1-4; Z es un cadena alquilideno C1-4; L es -O-, -S-, -SO-, -SO2-, -N(R6)SO2-, -SO2N(R6)-, -N(R6)-, -CO-, -CO2-, -N(R6)CO-, -N(R6)C(O)O-, -N(R6)CON(R6)-, -N(R6)SO2N(R6)-, -N(R6)N(R6)-, -C(O)N(R6)-, -OC(O)N(R6)-, -C(R6)2O-, -C(R6)2S-, -C(R6)2SO-, -C(R6)2SO2-, -C(R6)2SO2N(R6)-, -C(R6)2N(R6)-, -C(R6)2N(R6)C(O)-, -C(R6)2N(R6)C(O)O-, -C(R6)=NN(R6)-, -C(R6)=N-O-, -C(R6)2N(R6)N(R6)-, -C(R6)2N(R6)SO2N(R6)-, Ăł -C(R6)2N(R6)CON(R6)-; R2 y R2' son seleccionados independientemente entre -R, -T-W-R6, Ăł R2 y R2' son tomados conjuntamente con los ĂĄtomos a los cuales estĂĄn unidos para formar un anillo fusionado de 5-8 miembros, no saturado o parcialmente no saturado, que tiene 0-3 heteroĂĄtomos en el anillo seleccionados entre nitrĂłgeno, oxĂ­geno o azufre, en donde cada carbono sustituible de dicho anillo fusionado formado por R2 y R2' estĂĄ sustituido por halo, oxo, -CN, -NO2, -R7 Ăł -V-R6, y cualquier nitrĂłgeno sustituible de dicho anillo formado por R2 y R2' estĂĄ sustituido por R4; R3 es seleccionado entre -R, -halo, -OR, -C(=O)R, -CO2R, -COCOR, -COCH2COR, -NO2, -CN, -S(O)R, -S(O)2R, -SR, -N(R4)2, -CON(R7)2, -SO2N(R7)2, -OC(=O)R, -N(R7)COR, -N(R7)CO2(alifĂĄtico C1-6), -N(R4)N(R4)2, -C=NN(R4)2, -C=N-OR, -N(R7)CON(R7)2, -N(R7)SO2N(R7)2, -N(R4)SO2R, Ăł -OC(=O)N(R7)2; cada R es seleccionado independientemente entre hidrĂłgeno o un grupo opcionalmente sustituido seleccionado entre alifĂĄtico C1-6, arilo C6-10, un anillo heteroarilo que 5-10 ĂĄtomos en el anillo, o un anillo heterociclilo que tiene 5-10 ĂĄtomos en el anillo; cada R4 es seleccionado independientemente entre -R7, -COR7, -CO2(alifĂĄtico C1-6 opcionalmente sustituido), -CON(R7)2, Ăł -SO2R7; cada R5 es seleccionado independientemente entre -R, halo, -OR, -C(=O)R, -CO2R, -COCOR, -NO2, -CN, -S(O)R, -SO2R, -SR, -N(R4)2, -CON(R4)2, -SO2N(R4)2, -OC(=O)R, -N(R4)COR, -N(R4)CO2(alifĂĄtico C1-6 opcionalmente sustituido), -N(R4)N(R4)2, -C=NN(R4)2, -C=N-OR, -N(R4)CON(R4)2, -N(R4)SO2N(R4)2, -N(R4)SO2R, Ăł -OC(=O)N(R4)2; V es -O-, -S-, -SO-, -SO2-, -N(R6)SO2-, -SO2N(R6)-, -N(R6)-, -CO-, -CO2-, -N(R6)CO-, -N(R6)C(O)O-, -N(R6)CON(R6)-, -N(R6)SO2N(R6)-, -N(R6)N(R6)-, -C(O)N(R6)-, -OC(O)N(R6)-, -C(R6)2O-, -C(R6)2S-, -C(R6)2SO-, -C(R6)2SO2-, -C(R6)2SO2N(R6)-, -C(R6)2N(R6)-, -C(R6)2N(R6)C(O)-, -C(R6)2N(R6)C(O)O-, -C(R6)=NN(R6)-, -C(R6)=N-O-, -C(R6)2N(R6)N(R6)-, -C(R6)2N(R6)SO2N(R6)-, Ăł -C(R6)2N(R6)CON(R6)-; W es -C(R6)2O-, -C(R6)2S-, -C(R6)2SO-, -C(R6)2SO2-, -C(R6)2SO2N(R6)-, -C(R6)2N(R6)-, -CO-, -CO2-, -C(R6)OC(O)-, -C(R6)OC(O)N(R6)-, -C(R6)2N(R6)CO-, -C(R6)2N(R6)C(O)O-, -C(R6)=NN(R6)-, -C(R6)=N-O-, -C(R6)2N(R6)N(R6)-, -C(R6)2N(R6)SO2N(R6)-, -C(R6)2N(R6)CON(R6)-, o -CON(R6)-; cada R6 es seleccionado independientemente entre hidrĂłgeno o un grupo alifĂĄtico C1-4 opcionalmente sustituido, o dos grupos R6 sobre el mismo ĂĄtomo de nitrĂłgeno son tomados conjuntamente con el ĂĄtomo de nitrĂłgeno para formar un anillo heterociclilo o heteroarilo de 5-6 miembros; y cada R7 es seleccionado independientemente entre hidrĂłgeno o un grupo alifĂĄtico C1-6 opcionalmente sustituido, o dos R7 sobre el mismo nitrĂłgeno son tomados conjuntamente con el nitrĂłgeno para formar un anillo heterociclilo o heteroarilo de 5-8 miembros.
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DE60119777T2 (de) 2007-05-03
KR100843114B1 (ko) 2008-07-02
ATE354573T1 (de) 2007-03-15
WO2002050066A3 (en) 2003-01-23
DK1355905T3 (da) 2007-06-18
DE60119774D1 (de) 2006-06-22
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CN102250071A (zh) 2011-11-23
NO20032736L (no) 2003-08-18
SI1353916T1 (sl) 2007-02-28
AU2006201267B2 (en) 2010-07-29
KR20030061463A (ko) 2003-07-18
EP1345927A1 (en) 2003-09-24
ES2375491T3 (es) 2012-03-01
HUP0400639A3 (en) 2010-03-29
MXPA03005610A (es) 2003-10-06
AP1588A (en) 2006-03-06
WO2002050065A3 (en) 2002-10-24
NZ526473A (en) 2005-06-24
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CA2432799A1 (en) 2002-06-27
AU2001297619B2 (en) 2006-06-08
US20040157893A1 (en) 2004-08-12
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CA2432872C (en) 2008-09-23
JP2004516292A (ja) 2004-06-03
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NZ526469A (en) 2005-10-28
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IL156369A (en) 2011-02-28
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US20030078275A1 (en) 2003-04-24
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NZ526468A (en) 2004-03-26
BR0116493A (pt) 2003-09-30
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DE60119777D1 (de) 2006-06-22
IL156389A (en) 2011-01-31
KR100889246B1 (ko) 2009-03-19
NZ526474A (en) 2005-10-28
IL156408A0 (en) 2004-01-04
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KR100909665B1 (ko) 2009-07-29
NO20032736D0 (no) 2003-06-16
HUP0400842A2 (hu) 2004-07-28
ES2266095T3 (es) 2007-03-01
ES2265450T3 (es) 2007-02-16
NO20032670L (no) 2003-08-15
KR20030061858A (ko) 2003-07-22
ATE528303T1 (de) 2011-10-15
CN100436452C (zh) 2008-11-26
US20030055068A1 (en) 2003-03-20
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