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AR054088A1 - Triazoles como inhibidores de proteinquinasas. composiciones farmaceuticas - Google Patents

Triazoles como inhibidores de proteinquinasas. composiciones farmaceuticas

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Publication number
AR054088A1
AR054088A1 ARP050104417A ARP050104417A AR054088A1 AR 054088 A1 AR054088 A1 AR 054088A1 AR P050104417 A ARP050104417 A AR P050104417A AR P050104417 A ARP050104417 A AR P050104417A AR 054088 A1 AR054088 A1 AR 054088A1
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AR
Argentina
Prior art keywords
aliphatic
optionally substituted
hydrogen
haloaliphatic
halogen
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Application number
ARP050104417A
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English (en)
Inventor
Robert J Davies
Cornelia J Forster
Michael J Arnost
Jian Wang
Original Assignee
Vertex Pharma
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Publication date
Application filed by Vertex Pharma filed Critical Vertex Pharma
Publication of AR054088A1 publication Critical patent/AR054088A1/es

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    • C07D249/08—1,2,4-Triazoles; Hydrogenated 1,2,4-triazoles
    • C07D249/10—1,2,4-Triazoles; Hydrogenated 1,2,4-triazoles with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
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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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Abstract

Composiciones farmacéuticas que los comprenden. Reivindicacion 1: Un compuesto de triazol util como inhibidor de proteinquinasas, caracterizado por la formula (1), donde: X es CH o N; Y es CH2, NH, NR, O, o S; R1 es hidrogeno o alquilo C1-6; R2 es hidrogeno; R3 es un grupo arilo opcionalmente sustituido seleccionado entre un anillo monocíclico de 5-6 miembros o un anillo bicíclico de 8-12 miembros; teniendo dicho grupo arilo 0-3 heteroátomos seleccionados independientemente entre nitrogeno, oxígeno o azufre; R5 es hidrogeno, -alifáticoC1-6, -CN, -OH, -O(alifáticoC1-6), -CO2H, -CO2(alifáticoC1-6), -CON(R)2, -O(haloalifáticoC1-4), -haloalifático C1-4, -NO2, -halogeno, -NRo2, o -alifáticoC1-6 opcionalmente sustituido con NH2; R4 es hidrogeno, halogeno; -Ro; -ORo; -SRo; 1,2-metiliendioxi; 1,2-etilendioxi; fenilo (Ph) opcionalmente sustituido con Ro; -O(Ph) opcionalmente sustituido con Ro; -(CH2)1-2(Ph) opcionalmente sustituido con Ro; -CH=CH(Ph) opcionalmente sustituido con Ro; -NO2; -CN; -N(Ro)2; -NRoC(O)Ro; -NRoC(S)Ro; -NRoC(O)N(Ro)2; - NRoC(S)N(Ro)2; -NRoCO2Ro; -NRoNRoC(O)Ro; -NRoNRoC(O)N(Ro)2; -NRoNRoCO2Ro; -C(O)C(O)Ro; -C(O)CH2C(O)Ro; -CO2Ro; -C(O)Ro; -C(S)Ro; -C(O)N(Ro)2; -C(S)N(Ro)2; -C(=NH)-N(Ro)2, -OC(O)N(Ro)2; - OC(O)Ro; -C(O)N(ORo)Ro; -C(NORoRo; -S(O)2Ro; -S(O)3Ro; -SO2N(Ro)2; -S(O)Ro; -NRoSO2N(Ro)2; -NRoSO2Ro; -N(ORo)Ro; -C(=NH)-N(Ro)2; -(CH2)0-2NHC(O)Ro, =O, =S, =NNHR*, =NN(R*)2, =NNHC(0)R*, =NNHCO2(alquilo), =NNHSO2(alquilo), o =NR*, donde cada ocurrencia independiente de Ro se selecciona entre hidrogeno, alifático C1-6 opcionalmente sustituido, un anillo heteroarilo o heterocíclico no sustituido de 5-6 miembros, fenilo, -O(Ph), o -CH2(Ph), o, no obstante la definicion precedente, dos ocurrencias independientes de Ro, en el mismo sustituyente o sustituyentes diferentes, tomadas conjuntamente con el átomo (los átomos) al cual (a los cuales) cada grupo Ro está ligado, forman un anillo heterocíclico, arilo o heteroarilo de 5-8 miembros o un anillo cicloalquilo de 3-8 miembros que tiene 0-3 heteroátomos seleccionados independientemente entre nitrogeno, oxígeno o azufre; el grupo alifático de Ro está sustituido opcionalmente con NH2, NH(alifáticoC1-4), N(alifáticoC1-4)2, halogeno, alifático C1-4, OH, O(alifáticoC1-4), NO2, CN, CO2H, CO2(alifáticoC1-4), O(haloalifáticoC1-4), o halo(alifáticoC1-4), donde cada uno de estos grupos alifáticos C1-4 precedentes no está sustituido; cada R* es seleccionado independientemente entre hidrogeno o un alifático C1-6 opcionalmente sustituido con NH2, NH(alifáticoC1-4), N(alifáticoC1-4)2, halogeno, alifático C1-4, OH, O(alifáticoC1-4), NO2, CN, CO2H, CO2(alifáticoC1-4), O(haloalifáticoC1-4), o halo(alifáticoC1-4), donde cada uno de estos grupos alifáticos C1-4 precedentes no está sustituido; y R es hidrogeno o un grupo alifático C1-6, opcionalmente sustituido con =O, =S, -NH2, NH(alifáticoC1-4), N(alifáticoC1-4)2, halogeno, alifático C1-4, OH, O(alifáticoC1-4), NO2, CN, CO2H, CO2(alifáticoC1-4), O(haloalifáticoC1-4), o halo(alifáticoC1-4), donde cada uno de estos grupos alifáticos precedentes C1-4 no está sustituido.
ARP050104417A 2004-10-21 2005-10-21 Triazoles como inhibidores de proteinquinasas. composiciones farmaceuticas AR054088A1 (es)

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US (1) US7645775B2 (es)
EP (1) EP1811998B1 (es)
JP (1) JP5085330B2 (es)
KR (1) KR20070085407A (es)
CN (1) CN101072556A (es)
AR (1) AR054088A1 (es)
AT (1) ATE485042T1 (es)
AU (1) AU2005299816B2 (es)
BR (1) BRPI0517435A (es)
CA (1) CA2584752A1 (es)
CY (1) CY1111197T1 (es)
DE (1) DE602005024293D1 (es)
DK (1) DK1811998T3 (es)
ES (1) ES2352453T3 (es)
HR (1) HRP20100715T1 (es)
IL (1) IL182664A0 (es)
MX (1) MX2007004841A (es)
NO (1) NO20072567L (es)
NZ (1) NZ555088A (es)
PL (1) PL1811998T3 (es)
PT (1) PT1811998E (es)
RU (1) RU2393155C2 (es)
SI (1) SI1811998T1 (es)
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