ES2640911T3 - Cicloalquilnitrilpirazolcarboxamidas como inhibidores de la quinasa Janus - Google Patents

Cicloalquilnitrilpirazolcarboxamidas como inhibidores de la quinasa Janus Download PDF

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ES2640911T3
ES2640911T3 ES12833410.9T ES12833410T ES2640911T3 ES 2640911 T3 ES2640911 T3 ES 2640911T3 ES 12833410 T ES12833410 T ES 12833410T ES 2640911 T3 ES2640911 T3 ES 2640911T3
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alkyl
carbonyl
oxy
1oxy
cycloalkyl
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Jason Brubaker
Christopher J. Dinsmore
Dawn Marie Hoffman
Joon Jung
Duan Liu
Scott Peterson
Tony Siu
Luis E. Torres
Hongjun Zhang
Zhongyong Wei
Feng Shi
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Merck Sharp and Dohme LLC
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Abstract

Un compuesto de fórmula I o una sal o un estereoisómero farmacéuticamente aceptables del mismo: cada uno de Ra y R4 se selecciona independientemente entre hidrógeno y alquilo C1-4; A se selecciona entre arilo, y heteroarilo; n es 0, 1,2, 3, o 4; p es 2, 3, o 4; cada uno de R2 y R7 se selecciona independientemente entre hidrógeno, halógeno, alquilo C1-10, alquenilo C2-10, heteroalquilo C1-10, arilalquil C0-10 alquilo C0-10, cicloalquil C3-8 alquilo C0-10, heteroarilalquilo C0-10, heterocicloalquil (C3-8) alquilo C0-10, y en donde cada uno de R2 y R7 está independientemente sustituido con 0, 1,2, 3 o 4 sustituyentes R5a; R5a se selecciona de: halógeno, alquil C1-10 (oxi)0-1(carbonil)0-1alquilo C0-10, heteroalquil C1-10 (oxi)0-1(carbonil)0-1alquilo C0-10, alquenil C2-10 (oxi)0-1(carbonil)0-1alquilo C0-10, aril C0-10 alquil(oxi)0-1(carbonil)0-1alquilo C0-10, aril C2-10 alquenil(oxi)0-1(carbonil)0-1alquilo C0-10, aril C2-10 alquinil(oxi)0-1(carbonil)0-1alquilo C0-10, cicloalquil C3-8 alquil C0-10 (oxi)0-1(carbonil)0-1alquilo C0-10, heteroarilalquil C0-10 (oxi)0-1(carbonil)0-1alquilo C0-10, heterocicloalquil (C3-8)alquil C0-10 (oxi)0-1(carbonil)0-1alquilo C0-10, alquil C1-10 (carbonil)0-1oxi alquilo C0-10, heteroalquil C1-10 (carbonil)0-1oxi alquilo C0-10, alquenil C2-10 (carbonil)0-1oxi alquilo C0-10, heteroalquil C1-10 (carbonil)0-1oxi alquilo C0-10, aril C0-10 alquil (carbonil)0-1oxi alquilo C0-10, cicloalquil (C3-8) alquil C0-10 (carbonil)0-1oxi alquilo C0-10, heteroarilalquil C0-10 (carbonil)0-1oxialquilo C0-10, heterocicloalquil (C3-8) alquil C0-10 (carbonil)0-1oxi alquilo C0-10, (alquil (C0-10))1-2aminocarboniloxi, heteroalquil (C0-10)aminocarboniloxi, arilalquil (C0-10) aminocarboniloxi, cicloalquil (C3-8) alquil (C0-10) aminocarboniloxi, heteroarilalquil (C0-10)aminocarboniloxi, heterocicloalquil (C3-8) alquil (C0-10)aminocarboniloxi, alquil C0-10 amino(oxi)0-1(carbonil)0-1 alquenilo C2-10, alquil C1-10 amino(oxi)0-1(carbonil)0-1 alquilo C0-10, heteroalquil (C0-10)amin(oxi)0-1(carbonil)0-1 alquilo C0-10, cicloalquil C3-8 alquil C0-10 amino(oxi)0-1(carbonil)0-1 alquilo C0-10, arilalquil C0-10 amino(oxi)0-1(carbonil)0-1 alquilo C0-10, heteroarilalquil C0-10 amino((oxi)0-1(carbonil)0-1 alquilo C0-10, heterocicloalquil (C3-8) alquil C0-10 amino(oxi)0-1(carbonil)0-1alquilo C0-10, alquil C1-10 (oxi)0-1(carbonil)0-1aminoalquilo C0-10, heteroalquil C1-10 (oxi)0-1(carbonil)0-1aminoalquilo C0-10, cicloalquil C3-8 alquil C0-10 (oxi)0-1(carbonil)0-1aminoalquilo C0-10, arilalquil C0-10 (oxi)0-1(carbonil)0-1aminoalquilo C0-10, heteroarilalquil C0-10 (oxi)0-1(carbonil)0-1aminoalquilo C0-10, heterocicloalquil (C3-8) alquil C0-10 (oxi)0-1(carbonil)0-1aminoalquilo C0-10, -CO2(alquilo C0-10), -(alquil C0-10)CO2H, Oxo (>=O), formilo, sulfonilo , alquilsulfonilo C1-10, heteroalquilsulfonilo C1-10, cicloalquilsulfonilo (C3-8), cicloheteroalquilsulfonilo (C3-8), heteroarilsulfonilo, arilsulfonilo, aminosulfonilo, -SO2N(alquilo C0-6)1-2, -SO2alquilo C1-6, -SO2CF3, -SO2CF2H, -Si(CH3)3 alquilsulfinilo C1-10, amino, (alquil C0-10)1-2 amino, acil C1-4aminoalquilo C0-10, hidroxilo, (alquilo C1-10)OH, alquil C0-10 alcoxilo, iminoalquilo C0-10, (alquilo C0-10)imino, ciano, alquil C1-6ciano, y haloalquilo C1-6; en donde dos R5a y el átomo al que están unidos pueden formar opcionalmente un sistema de anillo saturado de 3, 4, 5, o 6 miembros; en dondecada R5a está opcionalmente sustituido con 1,2, 3 o 4 sustituyentes R6 y R6 se selecciona independientemente entre:
ES12833410.9T 2011-09-22 2012-09-21 Cicloalquilnitrilpirazolcarboxamidas como inhibidores de la quinasa Janus Active ES2640911T3 (es)

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US201161537978P 2011-09-22 2011-09-22
US201161537978P 2011-09-22
PCT/CN2012/001291 WO2013040863A1 (en) 2011-09-22 2012-09-21 Cycloalkylnitrile pyrazole carboxamides as janus kinase inhibitors

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ES12833410.9T Active ES2640911T3 (es) 2011-09-22 2012-09-21 Cicloalquilnitrilpirazolcarboxamidas como inhibidores de la quinasa Janus
ES12834379T Active ES2670878T3 (es) 2011-09-22 2012-09-21 Cianometilpirazol carboxamidas como inhibidores de la Janus quinasa
ES12834277.1T Active ES2633793T3 (es) 2011-09-22 2012-09-21 Pirazol carboxamidas como inhibidores de quinasa Janus

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ES12834379T Active ES2670878T3 (es) 2011-09-22 2012-09-21 Cianometilpirazol carboxamidas como inhibidores de la Janus quinasa
ES12834277.1T Active ES2633793T3 (es) 2011-09-22 2012-09-21 Pirazol carboxamidas como inhibidores de quinasa Janus

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US (4) US9493441B2 (es)
EP (4) EP2758389B1 (es)
JP (4) JP6034869B2 (es)
AU (4) AU2012313094B2 (es)
CA (4) CA2849168A1 (es)
ES (3) ES2640911T3 (es)
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WO (4) WO2013043964A1 (es)

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CA2849168A1 (en) * 2011-09-22 2013-03-28 Merck Sharp & Dohme Corp. Cycloalkylnitrile pyrazole carboxamides as janus kinase inhibitors
WO2014146249A1 (en) * 2013-03-19 2014-09-25 Merck Sharp & Dohme Corp. Geminally substituted cyanoethylpyrazolo pyridones as janus kinase inhibitors
WO2014146492A1 (en) * 2013-03-19 2014-09-25 Merck Sharp & Dohme Corp. N-(2-cyano heterocyclyl)pyrazolo pyridones as janus kinase inhibitors
HUE033587T2 (hu) 2013-05-17 2017-12-28 Incyte Corp Bipirazol-származékok mint JAK inhibitorok
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