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AR058379A1 - Derivados de arilpropionamida arilacrilamida arilpropinamida o arilmetilurea como inhibidores del factor xia. proceso de obtencion y composiciones farmaceuticas. - Google Patents

Derivados de arilpropionamida arilacrilamida arilpropinamida o arilmetilurea como inhibidores del factor xia. proceso de obtencion y composiciones farmaceuticas.

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Publication number
AR058379A1
AR058379A1 ARP060105500A ARP060105500A AR058379A1 AR 058379 A1 AR058379 A1 AR 058379A1 AR P060105500 A ARP060105500 A AR P060105500A AR P060105500 A ARP060105500 A AR P060105500A AR 058379 A1 AR058379 A1 AR 058379A1
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AR
Argentina
Prior art keywords
substituted
heterocycle
alkyl
independently
nr8r9
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ARP060105500A
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English (en)
Inventor
Donald J Pinto
Joanne M Smallheer
James R Corte
Zilun Hu
Cavallaro L Cullen
Paul Gilligan
Mimi L Quan
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Bristol Myers Squibb Co
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Publication of AR058379A1 publication Critical patent/AR058379A1/es

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Abstract

La presente se refiere a compuestos de la formula (1), y también a composiciones farmacéuticas que comprenden estos compuestos y métodos para tratar trastornos tromboembolicos y/o inflamatorios usando los mismos y procesos de obtencion de los mismos. Reivindicacion 1: Un compuesto caracterizado porque tiene la formula (1), o estereoisomeros, tautomeros, sales farmacéuticamente aceptables, o solvatos de los mismos, caracterizado porque, A es un carbociclo C3-10 substituido con 0-1 R1 y 0- 3 R2, o un heterociclo de 5 hasta 12 miembros que comprende: átomos de carbono y 1-4 heteroátomos seleccionados de N, O, y S(O)p, en donde el heterociclo está substituido con 0-1 R1 y 0-3 R2; con la condicion de que cuando A es un heterociclo que contiene uno o más átomos de nitrogeno, A no se enlaza a L1 por medio de cualquiera de los átomos de nitrogeno en el anillo A; L1 es -CH2CH2-, -CH(NR7R8)CH2-, -CH=CH-, -CsC-, -OCH2-, -CR5R6NH,-CH2O-, -SCH2-, -SO2CH2-, -CH2NR10-, o -NHNH-; con la condicion de que cuando L1 es -CH2O-, luego A es otro diferente a un fenilo no substituido; M es un elemento del grupo de formulas (2); R1 es, independientemente cada que se presenta. F, Cl, Br, I, OCF3, CF3, -(CH2)rORa, -(CH2)rSRa, CN, - (CH2)rNR7R8, -C(=NR8)NR8R9, -C(O)NR8R9, -S(O)pNR8R9, o alquilo C1-6 substituido con 0-1 R1a; R1a es F, OCF3, CF3, ORa, SRa, CN, -NR7R8, -C(O)NR8R9, -NR8C(O)Rc, -S(O)pNR8R9, NR8SO2Rc, o (CF2)rCF3; R2 es, independientemente cada que se presenta, O, F, CI, Br, OCF3, CF3, CHF2, CN, NO2 (CH2)rORa, (CH2)rSRa, -C(O)Ra, -C(O)ORa, -OC(O)Ra, -(CH2)NR7R8, -C(O)NR8R9, NR8C(O)Rc, NR8C(O)ORc, NR8C(O)NR8Rc, -S(O)pNR8R9, -NR8S(O)pRc, -S(O)Rc, -S(O)2Rc, alquilo C1-6 substituido con 0-1 R2a, (CH2)r-carbociclo de 3-7 miembros opcionalmente substituido con 0-2 R2b, o -(CH2)r-heterociclo de 5-7 miembros que comprende átomos de carbono y 1-4 heteroátomos seleccionados de N, O, y S(O)p, en donde el heterociclo está substituido con 0-2 R2b; alternativamente, cuando los grupos R1 y R2 son substituidos en átomos adyacentes los cuales pueden tomarse junto con los átomos a los cuales se enlazan para formar un carbociclo o heterociclo de 5 hasta 7 miembros que comprende átomos de carbono y 0-4 heteroátomos seleccionados de N, O, y S(O)p y substituido con 0-2 Rg; R2a es F, OCF3, CF3, ORa, SRa, CN, -NR7R8, -C(O)NR8R9, -NR8C(O)Rc, - NR8C(O)ORc, -NR8C(O)NR8Rc, S(O)pNR8R9, -NR8SO2Rc, o (CF2)rCF3; R2b es independientemente cada que se presenta, =O, F, Br, CI, OCF3, CF3, -(CH2)rORa, -(CH2)rSRa, -(CH2)rCN, -(CH2)rNR7R8, -(CH2)rC(O)ORa, (CH2)rC(O)NR8R9, -(CH2)rNR8C(O)Rc, -(CH2)rNR8C(O)ORc, -(CH2)rS(O)pNR8R9, -(CH2)rNR8SO2Rc, alquilo C1-4 o (CF2)rCF3; R3 es, independientemente cada que se presenta, - (CH2)r-carbociclo C3-10 substituido con 0-3 R3a y 0-1 R3d, o -(CH2)r-heterociclo de 5 hasta 12 miembros que comprende: átomos de carbono y 1-4 heteroátomos seleccionados de N, O, y S(O)p, en donde el heterociclo está substituido con 0-3 R3a y 0-1 R3d; R3a es, independientemente cada que se presenta, =O, =NR8, F, CI, Br, I, OCF3, CF3, -(CH2)rCN, NO2, -(CH2)rOR3b, -(CH2)rSR3b, -(CH2)rNR7R8, -NHC(O)NR8R9, -(CH2)rC(O)OR3b, -C(O)alquilo C1-4, -SO2NHR3b, -SO2NHCORc, -SO2NHCO2Rc, -CONHSO2R3c, - (CH2)rNR8C(O)R3b, -(CH2)rNR8CO2R3c, (CH2)rS(O)pNR8R9, -(CH2)rNR8S(O)pR3c, -NHSO2CF3, -S(O)R3c, S(O)2R3c, -(CH2)rC(O)NR8R9, -(CH2)rOC(O)NR8R9, -NHCOCF3, -NHSO2R3c, CONHOR3b, haloalquilo C1-4, haloalquiloxi C1-4, alquilo C1-6 substituido por R3e, alquenilo C2-6 substituido por R3e, alquinilo C1-6 substituido por R3e, cicloalquilo C3-6 substituido por 0-1 R3d, (CH2)r-carbociclo C6-10 substituido por 0-3 R3d o -(CH2)r-heterociclo de 5 hasta 10 miembros que comprende: átomos de carbono y 1-4 heteroátomos seleccionados de N, O, y S(O)p, en donde el heterociclo está substituido con 0-3 R3d; alternativamente, cuando dos grupos R3a se substituyen en átomos adyacentes, estos pueden tomarse junto con los átomos a los cuales se enlazan para formar un carbociclo C3-10 substituido con 0-2 R3d, o un heterociclo de 5 hasta 10 miembros que comprende: átomos de carbono y 1-4 heteroátomos seleccionados de N, O, y S(O)p, en donde el heterociclo está substituido con 0-2 R3d; R3b es, independientemente cada que se presenta, H, alquilo C1-6 substituido con 0-2 R3d, alquenilo C2-6 substituido con 0-2 R3d, alquinilo C2-6 substituido con 0-2 R3d, -(CH2)r-carbociclo C3-10 substituido con 0-3 R3d, o -(CH2)r-heterociclo de 5 hasta 10 miembros que comprende: átomos de carbono y 1-4 heteroátomos seleccionados de N, O, y S(O)p, en donde el heterociclo está substituido con 0-3 R3d; R3c es, independientemente cada que se presenta, alquilo C1-6 substituido con 0-2 R3d, alquenilo C2-6 substituido con 0-2 R3d, alquinilo C2-6 substituido con 0-2 R3d, -(CH2)r-carbociclo C3-10 substituido con 0-3 R3d, o -(CH2)r-heterociclo de 5 hasta 10 miembros que comprende: átomos de carbono y 1-4 heteroátomos seleccionados de N, O, y S(O)p, en donde el heterociclo está substituido con 0-3 R3d; R3d es, independientemente cada que se presenta, H, =O, F, CI, Br, CN, NO2, -(CH2)rNR7R8, -(CH2)rORa, -C(O)Ra, -C(O)ORa, -OC(O)Ra, NR8C(O)Rc, -C(O)NR8R9, - S(O)2NR8R9, -NR7R8, NR8S(O)2NR8R9, NR8S(O)2Rc, -S(O)pRc, -(CF2)rCF3, alquilo C1-6 substituido con 0-2 Re, alquenilo C2-6 substituido con 0-2 Re, alquinilo C2-6 substituido con 0-2 Re, -(CH2)r-carbociclo C3-10 substituido con 0-3 Rd, o (CH2)r-heterociclo de 5 hasta 10 miembros que comprende: átomos de carbono y 1-4 heteroátomos seleccionados de N, O, y S(O)p, en donde el heterociclo está substituido con 0-3 Rd; R3e es, independientemente cada que se presenta, H, -(CH2)rORa, F, =O, CN, NO2, -(CH2)rNR7R8, -C(O)Ra, -C(O)ORa, - OC(O)Ra, NR8C(O)Rc, -C(O)NR8R9, -S(O)2NR8R9, NR8S(O)2NR8R9, NR8S(O)2Rc, -S(O)pRc, (CF2)rCF3, (CH2)r-carbociclo C3-10 substituido con 0-3 Rd, o -(CH2)r-heterociclo de 5 hasta 10 miembros que comprende: átomos de carbono y 1-4 heteroátomos seleccionados de N, O, y S(O)p, en donde el heterociclo está substituido con 0-3 Rd; R4 es, independientemente cada que se presenta, H, F, CI, Br, I, OCF3, CF3, CN, NO2, ORa, SRa, -C(O)Ra, -C(O)ORa, -OC(O)Ra, -NR7R8, -C(O)NR8R9, -NR8C(O)Rc, - S(O)pNR8R9, -NR8S(O)pRc, -S(O)2Rc, o alquilo C1-4 substituido con 0-2 R4a; R4a es, independientemente cada que se presenta, H, F, =O, alquilo C1-6, ORa, SRa, CF3, CN, NO2, -C(O)Ra, -C(O)ORa, -NR7R8, -C(O)NR8R9, -NR8C(O)Rc, -S(O)pNR8R9, -NR8S(O)pRc, - S(O)Rc, o -S(O)2Rc; R5 es, independientemente cada que se presenta, H, F, CF3, -(CH2)rORa, =O, - (CH2)r-NR7R8, -S(O)pNR8R9, -(CH2)r-CO2Ra, -(CH2)r-CONR8R9, o alquilo C1-4; R6 es, independientemente cada que se presenta, H, F, o alquilo C1-4; R7 es, independientemente cada que se presenta, H, alquilo C1-6, -(CH2)n-carbociclo C3-10, -(CH2)n-(heteroarilo de 5 hasta 10 miembros), C(O)Rc, -CHO, -C(O)2Rc, -S(O)2Rc, -CONR8Rc, -OCONHRc, -C(O)O-(alquilo C1-4)OC(O)-(alquilo C1-4), o -C(O)O-(alquilo C1- 4)OC(O)-(arilo C6-10); en donde el alquilo, carbociclo, heteroarilo, y arilo son substituidos con 0-2 Rf; en donde el heteroarilo comprende: átomos de carbono y 1-4 heteroátomos seleccionados de N, O, y S(O)p; R8 es, independientemente cada que se presenta, H, alquilo C1-6, -(CH2)n-fenilo, o -(CH2)n-heterociclo de 5 hasta 10 miembros que comprende: átomos de carbono y 1-4 heteroátomos seleccionados de N, O, y S(O)p en donde el alquilo, fenilo y heterociclo son opcionalmente substituidos con 0- 2 Rf; alternativamente, R7 y R8, cuando se enlazan al mismo nitrogeno, se combinan para formar un heterociclo de 5 hasta 10 miembros que comprende: átomos de carbono y 0-3 heteroátomos adicionales seleccionados de N, O, y S(O)p, en donde el heterociclo está substituido con 0-2 Rf; R8a es H o alquilo C1-4; R9 es, independientemente cada que se presenta, H, alquilo C1-6, o -(CH2)n-fenilo; en donde el alquilo y fenilo son opcionalmente substituidos con 0-2 Rf; alternativamente, R8 y R9, cuando se enlazan al mismo nitrogeno, se combinan para formar un heterociclo de 5 hasta 10 miembros que comprende: átomos de carbono y 0-2 heteroátomos adicionales seleccionados de N, O, y S(O)p, en donde el heterociclo está substituido con 0-2 Rd; R10 es, independientemente cada que se presenta, H o alquilo C1-6 substituido con 0-3 R10a; R10a es, independientemente cada que se presenta, H, =O, alquilo C1-4, ORa, SRa, F, CF3, CN, NO2, -C(O)Ra, -C(O)ORa, -C(O)NR8R9, -NR8C(O)Rc, -S(O)pNR8R9, - NR8S(O)pRc, o S(O)pRc; R11 es haloalquilo C1-4, -C(O)NR8R9, -CH2C(O)NR8R9, -CH2CH2C(O)NR8R9, -C(O)Ra, -CH2C(O)Ra, -CH2CH2C(O)Ra, -C(O)ORa, -CH2C(O)ORa, -CH2CH2C(O)ORa, alquilo C1-6 substituido con 0-3 R11c, alquenilo C2-6 substituido con 0-3 R11a, alquinilo C2-6 o substituido con 0-3 R11a, -(CH2)r-carbociclo C3-10 substituido con 0-3 R11b, o -(CH2)r-heterociclo de 5 hasta 10 miembros que comprende: átomos de carbono y 1-4 heteroátomos seleccionados de N, O, y S(O)p, en donde el heterociclo está substituido con 0-3 R11b; R11a es, independientemente cada que se presenta H, =O, ORa, SRa, F, CF3, CN, NO2, -C(O)Ra, -C(O)ORa, -NR7R8, -C(O)NR8R9, NR8C(O)Rc, NR8C(O)ORc, -NR8CHO, -S(O)pNR8R9, NR8S(O)pRc, S(O)pRc, alquilo C1-4, cicloalquilo C3- 6, haloalquilo C1-4, haloalquiloxi C1-4, -(CH2)r-carbociclo C3-10 substituido con 0-3 Rd, o -(CH2)r-heterociclo de 5 hasta 10 miembros que comprende átomos de carbono y 1-4 heteroátomos seleccionados de N, O, y S(O)p, y substituidos con 0-3 Rd; R11b es, independientemente cada que se presenta, H, =O, =NR8, ORa, F, CI, Br, CN, NO2, CF3, OCF3, OCHF2, -C(O)Ra, -C(O)ORa, -NR7R8, -C(O)NR8R9, -NR7C(O)Rb, -NR8C(O)2Rc, -S(O)pNR8R9, -NR8S(O)pRc, S(O)pRc, alquilo C1-6, alquenilo C2-6, alquinilo C2-6, cicloalquilo C3-6, haloalquilo C1-4, haloalquiloxi C1-4, -(CH2)r-carbociclo C3-10 substituido con 0-3 Rd, o -(CH2)r-heterociclo de 5 hasta 10 miembros que comprende átomos de carbono y 1-4 heteroátomos seleccionados de N, O, y S(O)p, y substituidos con 0-3 Rd; alternativamente, cuando dos grupos R11b son substituidos en átomos adyacentes los cuales pueden tomarse junto con los át
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EA014245B1 (ru) 2010-10-29
AU2006325754A1 (en) 2007-06-21
ATE511502T1 (de) 2011-06-15

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