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AR047449A1 - Amino-benzazoles como inhibidores del receptor p2y1, composiciones farmaceuticas y metodos de tratamiento - Google Patents

Amino-benzazoles como inhibidores del receptor p2y1, composiciones farmaceuticas y metodos de tratamiento

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Publication number
AR047449A1
AR047449A1 ARP050100233A ARP050100233A AR047449A1 AR 047449 A1 AR047449 A1 AR 047449A1 AR P050100233 A ARP050100233 A AR P050100233A AR P050100233 A ARP050100233 A AR P050100233A AR 047449 A1 AR047449 A1 AR 047449A1
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Argentina
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substituted
alkyl
nr8r9
crfrf
orc
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ARP050100233A
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Timothy Herpin
George C Morton
Robert P Rehfuss
Michael Lawrence
Timur Gungor
Michael A Poss
Jacques Y Roberge
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Bristol Myers Squibb Co
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Application filed by Bristol Myers Squibb Co filed Critical Bristol Myers Squibb Co
Publication of AR047449A1 publication Critical patent/AR047449A1/es

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Abstract

Reivindicacion 1: Un compuesto de la formula (1) o un estereoisomero o sales farmacéuticamente aceptables, o solvatos del mismo, caracterizado porque: el anillo A es seleccionado del grupo de formulas (2); X1 es R11, O, o S(O)p; X2 es CR11a o N; X3 es CR11a o N; X4 es CR11b o N; X5 es CR11b o N; el anillo E se selecciona de fenilo, piridinilo, pirimidilo, pirazinilo, y piridazinilo y es sustituido con 0-4 R1; el anillo B es fenilo sustituido con 0-4 R7 o un heteroarilo de 5 a 6 miembros que comprende: átomos de C y 1-4 heteroátomos en el anillo seleccionados de O, N, NR6 y S(O)p, y el heteroarilo está sustituido con 0-4 R7; R1 es independientemente cada vez que se presenta, F, Cl, Br, I, OCF3, CF3, -CF2CF3, -(CRfRf)r-ORc, SRc, CN, NO2, -(CRfRf)r-NR8R9, -(CRfRf)r-C(O)Rc, -(CRfRf)r-C(O)ORc, -(CRfRf)r-C(O)NR8R9, -C(O)NR8-(CRfRf)t-NR8R9, NR10-(CRfRf)nC(O)Rd, -NR10CO-(CRfRf)nORc, -S(O)pNR8R9, -NR10S(O)pRd, -S(O)Rd, -S(O)2Rd, N-(C1-4 alquil)3+Cl-, C1-6 alquilo sustituido con 0-2 Ra, C2- 6 alquenilo sustituido con 0-2 Ra, C2-6 alquinilo sustituido con 0-2 Ra, -(CRfRf)r-C3-10 carbociclo sustituido con 0-3 Rb o -(CRfRf)r-heterociclo de 5 a 12 miembros que comprende: átomos de C y 1-4 heteroátomos seleccionados de N, O y S(O)p, y sustituidos con 0-3 Rb; alternativamente, dos R1 en los átomos de C adyacentes se combinan, con los átomos de C a los cuales se enlazan, forman un carbociclo o heterociclo de 5 a 6 miembros que comprende: átomos de C y 0-3 heteroátomos adicionales seleccionados de N, NH, O, y S(O)p, y sustituido con 0-2 Rb; Y es NR12, O, o S(O)p; R5 es un C3-10 carbociclo sustituido con 0-3 Rb o un heterociclo de 5 a 10 miembros que comprende: átomos de C y 1-4 heteroátomos seleccionados de N, O, y S(O)p, y sustituidos con 0-3 Rb; R6 es H, C1-6 alquilo sustituido con 0-2 Ra, C2-6 alquenilo sustituido con 0-2 Ra, C2-6 alquinilo sustituido con 0-2 Ra, (C1-6 alquil)C(O)-, (C3-6 cicloalquil)C1-3 alquil-C(O)-, (C3-6 cicloalquil)C(O)-, fenil-C(O)-, bencil- C(O)-, bencil-S(O)2-, (C1-6 alquil)NHC(O)-, (C1-6 alquil)2NC(O)-, fenil-NHC(O)-, bencil-NHC(O)-, (fenil)(C1-6 alquil)NC(O)-, (bencil)(C1-6 alquil)NC(O)-, (C1-6 alquil)-S(O)2-, fenil-S(O)2-, (CH2)r-C3-10 carbociclo sustituido con 0-3 Rb, o -(CH2)r- heterociclo de 5 a 10 miembros que comprende: átomos de C y 1-4 heteroátomos seleccionados de N, O y S(O)p, y sustituido con 0-3 Rb; R7 es H, F, Cl, Br, I, OCF3, CF3, ORc, SRc, CN, NO2, -NR8R9, C(O)Rc, C(O)ORc, -C(O)NR8R9, NR10C(O)Rd, -S(O)pNR8R9, - S(O)Rd, -S(O)2Rd, C1-6 alquilo sustituido con 0-2 Ra, C2-6 alquenilo sustituido con 0-2 Ra, C2-6 alquinilo sustituido con 0-2 Ra, -(CH2)r-C3-10 carbociclo sustituido con 0-3 Rb o -(CH2)r-heterociclo de 5 a 10 miembros que comprende: átomos de C y 1- 4 heteroátomos seleccionados de N, O y S(O)p, y sustituidos con 0-3 Rb; alternativamente, dos R7 en los átomos de C adyacentes se combinan para formar un anillo carbocíclico o heterocíclico de 5 a 7 miembros que comprende: átomos de C y 0-3 heteroátomos en el anillo seleccionados de O, N, NR6a, y S(O)p, y el anillo carbocíclico o heterocíclico está sustituido con 0-3 R7a; alternativamente, R6 puede combinarse con el R7 en el átomo C adyacente para formar un anillo carbocíclico o heterocíclico de 5 a 7 miembros que comprende: átomos de C y 0-3 heteroátomos en el anillo seleccionados de O, N, NR6, y S(O)p, y el anillo carbocíclico o heterocíclico está sustituido con 0-3 R7a; R6a es H, C1-4 alquilo, (C1-4 alquil)C(O)-, fenilo- C(O)-, bencil-C(O)-, bencil-S(O)2-, (C1-4 alquil)NHC(O)-, (C1-4 alquil)2-NC(O)-, fenil-NHC(O)-; bencil-NHC(O)-, (C1-4 alquil)-S-(O)2, fenil-S(O)2-, fenilo sustituido con 0-3 Rb, o bencilo sustituido con 0-3 Rb; R7a es H, F, Cl, Br, I, OCF3, CF3, ORc, SRc, CN, NO2, -NR8R9, C(O)Rc, C(O)ORc, -C(O)NR8R9, NR10C(O)Rd, -S(O)pNR8R9, -S(O)Rd, -S(O)2Rd, C1-4 alquilo, fenilo sustituido con 0-3 Rb o bencilo sustituido con 0-3 Rb; R8 es independientemente cada vez que se presenta H, C1-6 alquilo sustituido con 0-2 Rj, C(O)Rk, -C(O)ORk, -C(O)NRiRi, -C(O)O(C1-4 alquilo)-C(O)ORk, S(O)2Rk, -(CRfRf)r-C3-10 carbociclo sustituido con 0-3 Rj, o -(CRfRf)r- heterociclo de 5 a 10 miembros que comprende: átomos de C y 1-4 heteroátomos seleccionados de N, O y S(O)p, y sustituido con 0-3Rj; R9 es, independientemente cada vez que se presenta, H, C1-6 alquilo, o -(CH2)n-C3-10 carbociclo sustituido con 0-2 Rj, o -(CH2)r-heterociclo de 5 a 10 miembros que comprende: átomos de C y 1-4 heteroátomos seleccionados de N, O y S(O)p, y sustituido con 0-2 Rj; alternativamente, R8 y R9, cuando se enlazan al mismo N, se combinan para formar un anillo heterocíclico de 5 a 10 miembros que comprende: átomos de C y 0-2 heteroátomos adicionales seleccionados de N, NRi, O, y S(O)p; R10 es independientemente cada vez que se presenta H, C1-6 alquilo sustituido con 0-2 R10a, C2-6 alquenilo sustituido con 0-2 R10a, C2-6 alquinilo sustituido con 0-2 R10a, -(CH2)r-C3-10 carbocíclico sustituido con 0-3 Re, o -(CH2)r-heterociclo de 5 a 10 miembros que comprende: átomos de C y 1-4 heteroátomos seleccionados de N, O y S(O)p, y sustituido con 0-3 Re; R10a es, independientemente cada vez que se presenta, H, C1-4 alquilo, ORc, Cl, F, Br, I, =O, CCN, NO2, -C(O)Rc, -C(O)ORc, -C(O)NR8R9, o -S(O)pRd; R11 es H, C1-6 alquilo sustituido con 0-2 Ra, C2-6 alquenilo sustituido con 0-2 Ra, C2-6 alquinilo sustituido con 0-2 Ra, C(O)Rc, C(O)ORc, -C(O)NR8R9, -C(O)O(C1-4 alquilo)-C(O)ORk, -S(O)2NR8R9, - (CH2)r-C3-10 carbocíclico sustituido con 0-3 Rb o -(CH2)r-heterociclo de 5 a 10 miembros que comprende: átomos de C y 1-4 heteroátomos seleccionados de N, O, y S(O)p, y sustituido con 0-3 Rb; R11a es H, F, Cl, Br, I, OCF3, CF3, ORc, SRc, CN, NO2, - NR8R9, C(O)Rc, C(O)ORc, -C(O)NR8R9, NR10C(O)Rd, -S(O)pNR8R9, -S(O)Rd, -S(O)2Rd, C1-6 alquilo sustituido con 0-2 Ra, C2-6 alquenilo sustituido con 0-2 Ra, C2-6 alquinilo sustituido con 0-2 Ra, -(CH2)r-C3-10 carbociclo sustituido con 0-3 Rb, o -(CH2)r- heterociclo 5 a 10 miembros que comprende: átomos de C y 1-4 heteroátomos seleccionados de N, O y S(O)p, y sustituido con 0-3 Rb; R11b es F, Cl, Br, I, OCF3, CF3, -CF2CF3, -(CRfRf)r-ORc, SRc, CN, NO2, -(CRfRf)r-NR8R9, -(CRfRf)r-C(O)Rc, -(CRfRf)r- C(O)ORc, -(CRfRf)r-C(O)NR8R9, -C(O)NR8-(CRfRf)t-NR8R9, NR10-(CRfRf)nC(O)Rd, -NR10CO-(CRfRf)nORc, -S(O)pNR8R9, -NR10S(O)pRd, -S(O)Rd, -S(O)2Rd, C1-6 alquilo sustituido con 0-2 Ra, C2-6 alquenilo sustituido con 0-2 Ra, C2-6 alquinilo sustituido con 0- 2 Ra, -(CH2)r-C3-10 carbociclo sustituido con 0-3 Rb, o -(CH2)r-heterociclo 5 a 10 miembros que comprenden: átomos de C y 1-4 heteroátomos seleccionados de N, O y S(O)p, y sustituido con 0-3 Rb; R12 es H, C1-6 alquilo sustituido con 0-2 Ra, C2-6 alquenilo sustituido con 0-2 Ra, C2-6 alquinilo sustituido con 0-2 Ra, C(O)Rc, -C(O)ORc, -C(O)NR8R9, -C(O)O(C1-4 alquilo)-C(O)ORk, -S(O)2Rk, -S(O)2NR8R9, -(CH2)r-C3-10 carbocíclico sustituido con 0-3 Rb o -(CH2)r-heterociclo de 5 a 10 miembros que comprende: átomos de C y 1-4 heteroátomos seleccionados de N, O, y S(O)p, y sustituido con 0-3 Rb; R13 es H, C1-6 alquilo sustituido con 0-2 Ra, C2-6 alquenilo sustituido con 0-2 Ra, C2-6 alquinilo sustituido con 0-2 Ra, C(O)Rc, C(O)ORc, -C(O)NR8R9, -S(O)2Rk, -S(O)2NR8R9, -(CH2)r-C3-10 carbociclo sustituido con 0-3 Rb o -(CH2)r-heterociclo de 5 a 10 miembros que comprende: átomos de C y 1-4 heteroátomos seleccionados de N, O, y S(O)p, y sustituido con 0-3 Rb; Ra es independientemente cada vez que se presenta H, F, OCF3, CF3, ORc, SRc, CN, NO2, -NR8R9, C(O)Rc, C(O)ORc, -C(O)NR8R9, NR10C(O)Rb, -S(O)pNR8R9, -S(O)Rd, o -S(O)2Rd; Rb es, independientemente cada vez que se presenta, H, F, Cl, Br, I, ORc, SRc, CN, NO2, CF3, OCF3, - C(O)Rc, - C(O)ORc, -C(O)NR8R9, -NR10C(O)Rd, -S(O)pNR8R9, -S(O)pRd, -NR8R9, -Si(Me)3, C1-4 haloalquilo, C1-4 haloalquiloxi, C1-4 alquiloxi, C1-4 alquiltio, C1-4 alquilo-C(O)-, C1-4 alquilo-O-C(O)- C1-4 alquilo-C(O)NH-, C1-6 alquilo sustituido con 0-2Rj, C2-6 alquenilo sustituido con 0-2 Rj, C2-6 alquinilo sustituido con 0-2 Rj, -(CH2)r-C3-10 carbociclo sustituido con 0-3 Rj o -(CH2)r-heterociclo 5 a 10 miembros que comprenden: átomos de C y heteroátomos seleccionados de N, O y S(O)p, en donde el heterociclo es sustituido con 0-3 Rj; alternativamente, dos grupos Rb enlazados a átomos adyacentes, junto con los átomos a los cuales se enlazan, forman un anillo carbocíclico o heterocíclico de 5 a 7 miembros que comprenden: átomos de C y 0-2 heteroátomos seleccionados de N, O y S(O)p, 0-1 carbonilo y 0-3 enlaces dobles; Rc es, independientemente cada vez que se presenta H, C1-6 alquilo sustituido con 0-2 Rj, C2-6 alquenilo sustituido con 0-2 Rj, C2-6 alquinilo sustituido con 0-2 Rj, - (CH2)r-C6-10 arilo sustituido con 0-2 Re, o -(CH2)r-heterociclo de 5 a 10 miembros que comprenden: átomos de C y 1-4 heteroátomos seleccionados de N, O y S(O)p, y sustituido con 0-2 Re; Rd es, independientemente cada vez que se presenta CF3, OH, C1- 4 alcoxi, C1-6 alquilo sustituido con 0-2 Rj, -(CH2)r-C3-10 carbociclo sustituido con 0-2 Re, o (CH2)r-heterociclo de 5 a 10 miembros que comprenden: átomos de C y 1-4 heteroátomos seleccionados de N, O y S(O)p, y sustituido con 0-2 Re; Re es, independientemente cada vez que se presenta, H, =O, ORg, F, Cl, Br, I, CN, NO2, -NR8R9, C(O)Rf, -C(O)ORf, -NR8C(O)Rf, -C(O)NR8R9, -SO2NR8R9, -NR8SO2NR8R9, -NR8SO2-C1-4 alquilo,-NR8SO2CF3, -NR8SO2-fenilo, -S(O)2CF3, -S(O)P-C1-4 alquilo, -S(O)p- fenilo, -(CF2)rCF3, C1-6 alquilo, C2-6 alquenilo, C2-6 alquinilo, o -(CH2)n-fenilo; Rf es, independientemente cada vez que se presenta H, C1-6 alquilo o -(CH2)n-fenilo; Rg es, independientemente cada vez que se presenta, H, =o, ORf, F, Cl, Br, I, CN, NO2, -NR9R9, C(O)Rh, -C(O)ORh, -NR9C(O)Rh, -C(O)NR9R9, -SO2NR9R9, -NR9SO2NR9R9, -NR9SO2-C1-4 alquilo, -NR9SO2CF3, -NR9SO2-fenilo, -S(O)2CF3, -S(O)p-C1-4 alquilo, -S(O)p-fenilo, -(CF2)rCF3, C1-6alquilo,. C2-6 alquenilo, C2-6 alquinilo, o -(CH2)n- fenilo; Rh es, independientemente cada vez que se presenta, H, C1-6 alquilo o -(CH2)n-fenilo, Ri es, independientemen
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