ES2619610T3 - Moduladores de ROR-gamma-t de quinolinilo enlazado con heteroarilo - Google Patents

Moduladores de ROR-gamma-t de quinolinilo enlazado con heteroarilo Download PDF

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ES2619610T3
ES2619610T3 ES13783196.2T ES13783196T ES2619610T3 ES 2619610 T3 ES2619610 T3 ES 2619610T3 ES 13783196 T ES13783196 T ES 13783196T ES 2619610 T3 ES2619610 T3 ES 2619610T3
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alkyl
pyridyl
optionally substituted
pyridazyl
pyrazinyl
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Kristi A. Leonard
Kent Barbay
James P. Edwards
Kevin D. Kreutter
David A. Kummer
Umar Maharoof
Rachel NISHIMURA
Maud Urbanski
Hariharan Venkatesan
Aihua Wang
Ronald L. Wolin
Craig R. Woods
Anne Fourie
Xiaohua XUE
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Janssen Pharmaceutica NV
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Abstract

Un compuesto de fórmula I **Fórmula** donde: R1 es pirrolilo, pirazolilo, imidazolilo, triazolilo, tiazolilo, piridilo, piridilo N-óxido, pirazinilo, pirimidinilo, piridazilo, piperidinilo, quinazolinilo, cinolinilo, benzotiazolilo, indazolilo, tetrahidropiranilo, tetrahidrofuranilo, furanilo, fenilo, oxazolilo, isoxazolilo, tiofenilo, benzoxazolilo, bencimidazolilo, indolilo, tiadiazolilo, oxadiazolilo o quinolinilo; donde dichos piridilo, piridil-N-óxido, pirazinilo, pirimidinilo, piridazilo, piperidinilo, quinazolinilo, cinolinilo, benzotiazolilo, indazolilo, imidazolilo, fenilo, tiofenilo, benzoxazolilo, bencimidazolilo, indolilo, quinolinilo y pirazolilo están opcionalmente sustituidos con alquilo C(O)C(1-4), C(O)NH2, alquilo C(O)NHC(1-2), C(O)N(alquilo C(1-2))2, alquilo NHC(O)C1-4), alquilo NHSO2C(1-4), alquilo C(1-4), CF3, CH2CF3, Cl, F, -CN, alquilo OC(1-4), N(alquilo C(1-4))2, -(CH2)3OCH3, alquilo SC(1-4), OH, CO2H, alquilo CO2C(1-4), C(O)CF3, SO2CF3, OCF3, OCHF2, SO2CH3, SO2NH2, alquilo SO2NHC(1-2), alquilo SO2N(C(1-2))2, C(O)NHSO2CH3, o OCH2OCH3; y opcionalmente sustituido con hasta dos sustituyentes adicionales seleccionados independientemente del grupo consistente de Cl, alquilo C(1-2), SCH3, alquilo OC(1-2), CF3, -CN, y F; y donde dichos triazolilo, oxazolilo, isoxazolilo, pirrolilo y tiazolilo están opcionalmente sustituidos con hasta dos sustituyentes seleccionados independientemente del grupo consistente de O2CH3, SO2NH2, C(O)NH2, -CN, alquilo OC(1-2), (CH2)(2- 3)OCH3, SCH3, CF3, F, Cl, y alquilo C(1-2); y dichos tiadiazolilo y oxadiazolilo están opcionalmente sustituidos con alquilo C(1-2); y dichos piridilo, piridil-N-óxido, pirimidinilo, piridazilo y pirazinilo están opcionalmente sustituidos con hasta tres sustituyentes adicionales seleccionados independientemente del grupo consistente de alquilo C(O)NHC(1-2), C(O)N(alquilo C(1-2))2, alquilo NHC(O)C(1-4), alquilo NHSO2C(1-4), C(O)CF3, SO2CF3, alquilo SC2NHC(1-2), SO2N(alquilo C(1-2))2, C(O)NHSO2CH3, SO2CH3, SO2NH2, C(O)NH2, -CN, alquilo OC(1-4), (CH2)(2-3)OCH3 (incluyendo -(CH2)3OCH3), alquilo SC(1-4), CF3, F, Cl, y alquilo C(1-4); R2 es triazolilo, piridilo, piridil-N-óxido, pirazolilo, pirimidinilo, oxazolilo, isoxazolilo, N-acetilpiperidinilo, 1-H-piperidinilo, N-Boc-piperidinilo, NC (1-3) alquil- piperidinilo, tiazolilo, piridazilo, pirazinilo , 1-(3-metoxipropil)- imidazolilo, tiadiazolilo, oxadiazolilo o imidazolilo; donde dicho imidazolilo está opcionalmente sustituido con hasta tres sustituyentes adicionales seleccionados independientemente del grupo consistente de alquilo C(1- 2), SCH3, alquilo OC(1-2), CF3, -CN, F, y Cl; y dichos piridilo, piridil-N-óxido, pirimidinilo, piridazilo y pirazinilo, están opcionalmente sustituidos con hasta tres sustituyentes adicionales seleccionados independientemente del grupo consistente de SO2CH3, SO2NH2, C(O)NH2, -CN, alquilo OC(1-2),(CH2)(2-3)OCH3, SCH3, CF3, F, Cl, o alquilo C(1-2); y dichos triazolilo, tiazolilo, oxazolilo e isoxazolilo están opcionalmente sustituidos con hasta dos sustituyentes seleccionados independientemente del grupo consistente de SO2CH3, SO2NH2, C(O)NH2, - CN, alquilo OC(1-2), (CH2)(2-3)OCH3, SCH3, CF3, F, Cl, y alquilo C(1-2); y dichos tiadiazolilo y oxadiazolilo están opcionalmente sustituidos con alquilo C(1-2); y dicho pirazolilo está opcionalmente sustituido con hasta tres grupos CH3; R3 es H, OH, OCH3, o NH2; R4 es H, o F; R5 es H, Cl, -CN, CF3, alquilo SC(1-4), alquilo OC(1-4), OH, alquilo C(1-4), N(CH3)OCH3, NH(alquilo C(1-4)), N(alquilo C(1-4))2, o 4-hidroxi-piperidinilo; R6 es O-fenilo, -NHfenilo, -N(alquilo C(1-3))fenilo, -N(CO2C(CH3)3)fenilo, N(COCH3)fenilo, -O-piridilo, - NHpiridilo, -N(alquilo C(1-3))piridilo, N(CO2C(CH3)3)piridilo, N(COCH3)piridilo, -O-pirimidinilo, -NHpirimidinilo, - N(alquilo C(1-3))pirimidinilo, N(CO2C(CH3)3)pirimidinilo, N(COCH3)pirimidinilo, -O-piridazilo, -NHpiridazilo, - N(alquilo C(1-3))piridazilo, N(CO2C(CH3)3)piridazilo, N(COCH3)piridazilo, -O-pirazinilo, -NHpirazinilo, -N(alquilo C(1-3))pirazinilo, N(CO2C(CH3)3)pirazinilo, o N(COCH3)pirazinilo; donde dichos pirimidinilo, piridazilo o pirazinilo están opcionalmente sustituidos con Cl, F, CHF3, SCH3, alquilo OC(1-4), -CN, CONH2, SO2NH2, o SO2CH3; y donde dicho fenilo o dicho piridilo está opcionalmente sustituido hasta dos veces con OCF3, alquilo SO2C(1-4), CF3, OCHF2, pirazolilo, triazolilo, imidazolilo, tetrazolilo, oxazolilo, tiazolilo, alquilo C(1-4), cicloalquilo C(3-4), alquilo OC(1-4), N(CH3)2, SO2NH2, SO2NHCH3, SO2N (CH3)2, CONH2, CONHCH3, CON(CH3)2, Cl, F, - CN, CO2H, OH, CH2OH, alquilo NHCOC(1-2), alquilo COC(1-2), SCH3, alquilo CO2C(1-4), NH2, alquilo NHC(1-2), o OCH2CF3; donde la selección de cada sustituyente opcional es independiente; y donde dichos pirazolilo, triazolilo, imidazolilo, tetrazolilo, oxazolilo y tiazolilo están opcionalmente sustituidos con CH3; R7 es H, Cl, -CN, alquilo C(1-4), OC(1-4)alquiloCF3, OCF3, OCHF2, alquilo OCH2CH2OC(1-4), CF3, SCH3, C(1- 4)alquiloNA1A2 (incluyendo CH2NA1A2), CH2OC(2-3)alquiloNA1A2, NA1A2, C(O)NA1A2, CH2NHC(2- 3)alquiloNA1A2, CH2N(CH3)C(2-3)alquiloNA1A2,NHC(2-3)alquiloNA1A2, N(CH3)C(2-4)alquiloNA1A2, OC(2- 4)alquiloNA1A2, alquilo OC(1-4), OCH2-(1-metil)-imidazol-2-il, fenilo, tiofenilo, furilo, pirazolilo, imidazolilo, piridilo, piridazilo, pirazinilo o pirimidinilo; en donde dichos grupos fenilo, tiofenilo, furilo, pirazolilo, imidazolilo, piridilo, piridazilo, pirazinilo y pirimidinilo están opcionalmente sustituidos con hasta tres sustituyentes seleccionado independientemente del grupo consistente de F, Cl, CH3, CF3, y SOCH3; A1 es H, o alquilo C(1-4); A2 es H, alquilo C(1-4), alquiloC(1-4) alquilo OC(1-4), alquilo C(1-4) OH, alquilo C(O)C(1-4), o alquilo OC(1-4); o A1 o A2 pueden tomarse junto con su nitrógeno unido para formar un anillo seleccionado del grupo consistente de: **Fórmula** Ra es H, alquilo OC(1-4), CH2OH, NH(CH3), N(CH3)2, NH2, CH3, F, CHF3, SO2CH3, o OH; Rb es H, CO2C(CH3)3, alquilo C(1-4), alquilo C(O)C(1-4), alquilo SO2C(1-4), CH2CH2CF3, CH2CF3, CH2- ciclopropilo, fenol, CH2-fenilo, o cicloalquilo C(3-6); R8 es H, alquilo C(1-3) (incluyendo CH3), alquilo OC(1-3) (incluyendo OCH3), CF3, NH2, NHCH3,-CN, o F; R9 es H, o F; y sales farmacéuticamente aceptables de los mismos.

Claims (1)

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ES13783196.2T 2012-10-16 2013-10-15 Moduladores de ROR-gamma-t de quinolinilo enlazado con heteroarilo Active ES2619610T3 (es)

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PCT/US2013/065007 WO2014062655A1 (en) 2012-10-16 2013-10-15 HETEROARYL LINKED QUINOLINYL MODULATORS OF RORyt

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