ES2670878T3 - Cianometilpirazol carboxamidas como inhibidores de la Janus quinasa - Google Patents

Cianometilpirazol carboxamidas como inhibidores de la Janus quinasa Download PDF

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ES2670878T3
ES2670878T3 ES12834379T ES12834379T ES2670878T3 ES 2670878 T3 ES2670878 T3 ES 2670878T3 ES 12834379 T ES12834379 T ES 12834379T ES 12834379 T ES12834379 T ES 12834379T ES 2670878 T3 ES2670878 T3 ES 2670878T3
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alkyl
oxy
carbonyl
amino
heteroarylalkyl
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Jason Brubaker
Matthew Lloyd CHILDERS
Matthew Christopher
Joshua T. CLOSE
Jason David KATZ
Joon Jung
Scott Peterson
Phieng Siliphaivanh
Tony Siu
Graham Frank SMITH
Luis E. Torres
Hyun Chong Woo
Jonathan R. Young
Hongjun Zhang
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Merck Sharp and Dohme LLC
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Abstract

Un compuesto de fórmula I o una sal farmacéuticamente aceptable o un estereoisómero del mismo:**Fórmula** cada uno de Ra y R4 se selecciona independientemente entre hidrógeno y alquilo C1-4; A se selecciona entre arilo y heteroarilo; n is independientemente 0, 1, 2, 3 o 4; p es 2 o 3; X se selecciona independientemente entre C, N, O y S; cada uno de R3 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 R3 y R7 se sustituyen independientemente con 0, 1, 2, 3 o 4 sustituyentes R5a; R5a se selecciona entre: 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, arilo C0-10 alquil(oxi)0-1(carbonil)0-1alquilo C0-10, arilo C2-10 alquenil(oxi)0-1(carbonil)0-1alquilo C0-10, arilo 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)0-1oxialquilo 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)0-1carbonilalquilo C0-10, heteroalquil (C0-10) amino(oxi)0-1carbonilalquilo C0-10, cicloalquil C3-8 alquil C0-10 amino(oxi)0-1carbonilalquilo C0-10, arilalquil C0-10 amino(oxi)0-1carbonilalquilo C0-10, heteroarilalquil C0-10 amino(oxi)0-1carbonilalquilo C0-10, heterocicloalquil (C3-8) alquil C0-10 amino(oxi)0-1carbonilalquilo 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, arilalquilo 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); alquilsulfonilo C1-10, heteroalquilsulfonilo C1-10, cicloalquilsulfonilo (C3-8), cicloheteroalquilsulfonilo (C3-8), heteroarilsulfonilo, arilsulfonilo, aminosulfonilo, -SO2N(alquilo C1-6)1-2, -SO2alquilo C1-6, -SO2CF3, -SO2CF2H, alquilsulfinilo C1-10, -Si(CH3)3, amino, (alquil C0-10)1-2 amino, acil C1-4aminoalquilo C0-10, hidroxi, (alquilo C1-10)OH, alquilalcoxi C0-10, ciano, (alquilo C1-6 )ciano y haloalquilo C1-6; en donde dos R5a y el átomo al que están unidos pueden formar opcionalmente un sistema de anillo saturado de 4, 5 o 6 miembros; en donde cada R5a está opcionalmente sustituido con 1, 2, 3 o 4 sustituyentes R6 y R6 se selecciona independientemente entre: 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, arilo C0-10 alquil(oxi)0-1(carbonil)0-1alquilo C0-10, arilo C2-10 alquenil(oxi)0-1(carbonil)0-1alquilo C0-10, arilo 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)0-1oxialquilo 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, 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)0-1carbonilalquilo C0-10, cicloalquil C3-8 alquil C0-10 amino(oxi)0-1carbonilalquilo C0-10, arilalquil C0-10 amino(oxi)0-1carbonilalquilo C0-10, heteroarilalquilo C0-10 amino (oxi)0-1carbonilalquilo C0-10, heterocicloalquil (C3-8)alquil C0-10 amino(oxi)0-1carbonilalquilo C0-10, alquil C1-10 (oxi)0-1carbonilaminoalquilo C0-10, cicloalquil C3-8 alquil C0-10 (oxi)0-1carbonilaminoalquilo C0-10, arilalquilo C0-10 (oxi)0-1carbonilaminoalquilo C0-10, heteroarilalquilo C0-10 (oxi)0-1carbonilaminoalquilo C0-10,
ES12834379T 2011-09-22 2012-09-21 Cianometilpirazol carboxamidas como inhibidores de la Janus quinasa Active ES2670878T3 (es)

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