AR045690A1 - Compuestos biaril heterociclicos y metodos para preparar y utilizar los mismos - Google Patents
Compuestos biaril heterociclicos y metodos para preparar y utilizar los mismosInfo
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- AR045690A1 AR045690A1 ARP040101891A ARP040101891A AR045690A1 AR 045690 A1 AR045690 A1 AR 045690A1 AR P040101891 A ARP040101891 A AR P040101891A AR P040101891 A ARP040101891 A AR P040101891A AR 045690 A1 AR045690 A1 AR 045690A1
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- nr4r4
- saturated
- aromatic
- unsaturated
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- C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
- C07D487/04—Ortho-condensed systems
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- C07D263/08—Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings not condensed with other rings having one double bond between ring members or between a ring member and a non-ring member
- C07D263/16—Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings not condensed with other rings having one double bond between ring members or between a ring member and a non-ring member with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
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- C07D263/18—Oxygen atoms
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- C07D263/16—Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings not condensed with other rings having one double bond between ring members or between a ring member and a non-ring member with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
- C07D263/18—Oxygen atoms
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- C07D263/30—Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
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- C07D417/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
- C07D417/10—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings linked by a carbon chain containing aromatic rings
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Abstract
Se refiere en general al campo de los agentes anti-infecciosos, anti-proliferativos, anti-inflamatorios, y procinéticos. Reivindicación 1: Un compuesto que tiene la fórmula (1) o su sal, éster o profármaco aceptable para uso farmacéutico, en el cual: A se selecciona del grupo integrado por : fenilo, piridilo, pirazinilo, pirimidinilo, y piridazinilo ; B se selecciona del grupo integrado por: fenilo, piridilo, pirazinilo, pirimidinilo, y piridazinilo; Het-CH2-R3 se selecciona del grupo integrado por el grupo de fórmulas (2): M se selecciona del grupo integrado por : a) carbociclo C3-14 aromático, saturado o insaturado, y b) heterociclo aromático, saturado o insaturado de 3-14 miembros que contiene uno o más heteroátomos seleccionados del grupo integrado por nitrógeno, oxígeno, y azufre, donde a) o b) está opcionalmente substituido con uno o más grupos R5; M-L se selecciona del grupo integrado por: a) M-X, b) M-L1, c) M-L1-X, d) M-X-L2, e) M-L1-X-L2, f) M-X-L1-X-L2, g) M-L1-X-L2-X, h) M-X-X-, i) M-L1-X-X-, j) M-X-X-L2, y k) M-L1-X-X-L2, en los cuales X, en cada aparición, se selecciona independientemente del grupo integrado por : a) -O-, b) -NR4, c) -N(O)-, d) -N(OR4)-, e) -S(O)p-, f) -SO2NR4-, g) -NR4SO2-, h) - NR4-N=, i) =N-NR4-, j) -O-N=, k)=N-O-, l) -N=, m) =N-, n) -NR4-NR4-, o) -NR4-C(O)-O-, p) -O-C(O)-NR4-, q) -NR4-C(O)-NR4-, r) -NR4-C(NR4)-NR4-, y s) (fórmula (3)); L1 se selecciona del grupo integrado por : a) alquilo C1-6, b) alquenilo C2-6, y c) alquinilo C2-6, donde cualquiera de a)-c) está opcionalmente substituido con uno o más grupos R5; y L2 se selecciona del grupo integrado por a) alquilo C1-6, b) alquenilo C2-6, y c) alquinilo C2-6, donde cualquiera de a)-c) está opcionalmente substituido con uno o más grupos R5; R1, en cada aparición, se selecciona independientemente del grupo integrado por: a) F, b) Cl, c) Br, d) I, e) -CF3, f) -OR4, g) -CN, h) -NO2,i) -NR4R4, j) -C(O)R4, k) -C(O)OR4, l) -OC(O)R4, m) -C(O)NR4R4, n) - NR4C(O) R4, o) -OC(O)NR4R4, p) -NR4C(O)OR4, q) -NR4C(O)NR4R4, r) -C(S)R4, s) -C(S)OR4, t) -OC(S)R4, u) -C(S)NR4R4, v) -NR4C(S)R4, w) -OC(S)NR4R4, x) -NR4C(S)OR4, y) -NR4C(S)NR4R4, z) -NR4C(NR4)NR4R4, aa) -S(O)pR4, bb) -SO2NR4R4, y cc) R4; R2, en cada aparición, se selecciona independientemente del grupo integrado por : a) F, b) Cl, c) Br, d) I, e) -CF3, f) -OR4,g) -CN, h) -NO2, i) -NR4R4, j) -C(O)R4, k) -C(O)OR4, l) -OC(O)R4, m) -C(O)NR4R4, n) -NR4C(O)R4, o) -OC(O)NR4R4, p) -NR4C(O)OR4, q) - NR4C(O)NR4R4, r) -C(S)R4, s) -C(S)R4, t) -OC(S)R4, u) -C(S)NR4R4, v) -NR4C(S)R4, w) -OC(S)NR4R4, x) -NR4C(S)OR4, y) -NR4C(S)NR4R4, z) -NR4C(NR4)NR4R4, aa) -S(O)pR4, bb) -SO2NR4R4, y cc) R4; R3 se selecciona del grupo integrado por : a) -OR4, b) - NR4R4, c) -C(O)R4, d) -C(O)OR4, e) -OC(O)R4, f) -C(O)NR4R4, g) -NR4C(O)R4, h) -OC(O)NR4R4, i) -NR4C(O)OR4, j) -NR4C(O)NR4R4, k) -C(S)R4, l) -C(S)OR4, m) -OC(S)R4, n) -C(S)NR4R4, o) -NR4C(S)R4, p) -OC(S)NR4R4, q) -NR4C(S)OR4, r) -NR4C(S)NR4R4, s) - NR4C(NR4)NR4R4, t) -S(O)pR4, u) -SO2NR4R4, y v) R4; R4, en cada aparición, se selecciona independientemente del grupo integrado por : a) H, b) alquilo C1-6, c) alquenilo C2-6, d) alquinilo C2-6, e) carbociclo C3-14 aromático, saturado o insaturado, f) heterociclo de 3-14 miembros aromático, saturado o insaturado que contiene uno o más heteroátomos seleccionados del grupo integrado por nitrógeno, oxígeno, y azufre, g) -C(O)-alquilo C1-6, h) -C(O)-alquenilo C2-6, i) -C(O)-alquinilo C2-6, j) - C(O)-carbociclo C3-14 aromático, saturado o insaturado, k) -C(O)-heterociclo de 3-14 miembros aromático, saturado o insaturado que contiene uno o más heteroátomos seleccionados del grupo integrado por nitrógeno, oxígeno, y azufre, l) -C(O)O-alquilo C1-6, m) -C(O)O-alquenilo C2-6, n) -C(O)O-alquinilo C2-6, o) -C(O)O-carbociclo C3-14 aromático, saturado o insaturado, y p) -C(O)O-heterociclo de 3-14 miembros aromático, saturado o insaturado que contiene uno o más heteroátomos seleccionados del grupo integrado por nitrógeno, oxígeno, y azufre, donde cualquiera de b)-p) está opcionalmente substituido con uno o más grupos R5; R5, en cada aparición, se selecciona independientemente del grupo integrado por: a) F, b) Cl, c) Br, d) I, e) =O, f) =S, g) =NR6, h) =NOR6, i) =N-NR6R6, j) -CF3, k) -OR6, l) -CN, m) -NO2, n) -NR6R6, o) -C(O)R6, p) -C(O)OR6, q) -OC(O)R6, r) -C(O)NR6R6, s) -NR6C(O)R6, t) -OC(O)NR6R6, u) -NR6C(O)OR6, v) -NR6C(O)NR6R6, w) -C(S)R6, x) -C(S)OR6, y) -OC(S)R6, z) - C(S)NR6R6, aa) -NR6C(S)R6, bb) -OC(S)NR6R6, cc) -NR6C(S)OR6, dd) -NR6C(S)NR6R6, ee) -NR6C(NR6)NR6R6, ff) -S(O)pR6, gg) -SO2NR6R6, y hh) R6; R6, en cada aparición, se selecciona independientemente del grupo integrado por: a) H, b) alquilo C1-6, c) alquenilo C2-6, d) alquinilo C2-6, e) carbociclo C3-14 aromático, saturado o insaturado,f) heterociclo de 3-14 miembros aromático, saturado o insaturado que contiene uno o más heteroátomos seleccionados del grupo integrado por nitrógeno, oxígeno, y azufre, g) -C(O)-alquilo C1-6, h) -C(O)-alquenilo C2-6, i) -C(O)-alquinilo C2-6, j) -C(O)-carbociclo C3-14 aromático, saturado o insaturado,k) -C(O)-heterociclo de 3-14 miembros aromático, saturado o insaturado que contiene uno o más heteroátomos seleccionados del grupo integrado por nitrógeno, oxígeno, y azufre, l) -C(O)O-alquilo C1-6, m) -C(O)O-alquenilo C2-6, n) -C(O)O- alquinilo C2-6, o) -C(O)O-carbociclo C3-14 aromático, saturado o insaturado, y p) -C(O)O-heterociclo de 3-14 miembros aromático, saturado o insaturado que contiene uno o más heteroátomos seleccionados del grupo integrado por nitrógeno, oxígeno, y azufre, donde cualquiera de b)-p) está opcionalmente substituido con uno o más grupos R7; R7, en cada aparición, se selecciona independientemente del grupo integrado por: a) F, b) Cl, c) Br, d) I, e) =O, f) =S, g) =NR8, h) =NOR8, i) =N-NR8R8, j) -CF3, k) -OR8, l) -CN, m) -NO2, n) -NR8R8, o) -C(O)R8, p) -C(O)OR8, q) -OC(O)R8, r) -C(O)NR8R8, s) -NR8C(O)R8, t) - OC(O)NR8R8, u) -NR8C(O)OR8, v) -NR8C(O)NR8R8, w) -C(S)R8, x) -C(S)OR8, y) -OC(S)R8, z) -C(S)NR8R8, aa) -NRC(S)R8, bb) -OC(S)NR8R8, cc) -NR8C(S)OR8, dd) -NR8C(S)NR8R8, ee) -NR8C(NR8)NR8R8, ff) -S(O)pR8, gg) -SO2NR8R8, hh) alquilo C1-6, ii) alquenilo C2-6, jj) alquinilo C2-6, kk) carbociclo C3-14 aromático, saturado o insaturado, y ll) heterociclo de 3-14 miembros aromático, saturado o insaturado que contiene uno o más heteroátomos seleccionados del grupo integrado por nitrógeno, oxígeno, y azufre, donde cualquiera de hh)-ll) está opcionalmente substituido con uno o más restos seleccionados del grupo integrado por R8, F, Cl, Br, I, -CF3, -OR8, -SR8, -CN, -NO2, -NR8R8, -C(O)R8, -C(O)OR8, -OC(O)R8, -C(O)NR8R8, -NR8C(O)R8, -OC(O)NR8R8, - NR8C(O)OR8, -NR8C(O)NR8R8, -C(S)R8, -C(S)OR8, -OC(S)R8, -C(S)NR8R8, -NR8C(S)R8, -OC(S)NR8R8, -NR8C(S)OR8, -NR8C(S)NR8R8, -NR8C(NR8)NR8R8, -SO2NR8R8, y -S(O)pR8; R8, en cada aparición, se selecciona independientemente del grupo integrado por: a) H, b) alquilo C1-6, c) alquenilo C2-6, d) alquinilo C2-6, e) carbociclo C3-14 aromático, saturado o insaturado, f) heterociclo de 3-14 miembros aromático, saturado o insaturado que contiene uno o más heteroátomos seleccionados del grupo integrado por nitrógeno, oxígeno, y azufre, g) -C(O)-alquilo C1-6, h) -C(O)-alquenilo C2-6, i) -C(O)-alquinilo C2-6, j) -C(O)-carbociclo C3-14 aromático, saturado o insaturado, k) -C(O)-heterociclo de 3-14 miembros aromático, saturado o insaturado que contiene uno o más heteroátomos seleccionados del grupo integrado por nitrógeno, oxígeno, y azufre, l) -C(O)O-alquilo C1-6, m) -C(O)O-alquenilo C2-6, n) -C(O)O-alquinilo C2-6, o) -C(O)O-carbociclo C3-14 aromático, saturado o insaturado, y p) -C(O)O- heterociclo de 3-14 miembros aromático, saturado o insaturado que contiene uno o más heteroátomos seleccionados del grupo integrado por nitrógeno, oxígeno, y azufre, donde cualquiera de b)-p) está opcionalmente substituido con uno o más restos seleccionados del grupo integrado por F, Cl, Br, I, -CF3, -OH, -OCH3, -SH, -SCH3, -CN, -NO2,-NH2, -NHCH3, -N(CH3)2, -C(O)CH3, -C(O)OCH3, -C(O)NH2, -NHC(O)CH3, -SO2NH2-SO2NHCH3-, -SO2N(CH3)2, y -S(O)pCH3; m, en cada aparición, independientemente es 0, 1, 2, 3 ó 4; n, en cada aparición, independientemente es 0, 1, 2, 3 ó 4; y p, en cada aparición, independientemente es 0, 1 ó 2; y donde el compuesto no tiene la fórmula correspondiente a cualquiera de las estructuras mencionadas en la tabla.
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