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AR030324A1 - Derivados de 4-fenil-piridina - Google Patents

Derivados de 4-fenil-piridina

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Publication number
AR030324A1
AR030324A1 ARP010103749A ARP010103749A AR030324A1 AR 030324 A1 AR030324 A1 AR 030324A1 AR P010103749 A ARP010103749 A AR P010103749A AR P010103749 A ARP010103749 A AR P010103749A AR 030324 A1 AR030324 A1 AR 030324A1
Authority
AR
Argentina
Prior art keywords
halogen
lower alkyl
trifluoromethyl
cyano
hydroxy
Prior art date
Application number
ARP010103749A
Other languages
English (en)
Inventor
Thierry Godel
Torsten Hoffmann
Patrick Schnider
Heinz Stadler
Original Assignee
Hoffmann La Roche
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Hoffmann La Roche filed Critical Hoffmann La Roche
Publication of AR030324A1 publication Critical patent/AR030324A1/es

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    • C07D213/02—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
    • C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D213/60—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom 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
    • C07D213/72—Nitrogen atoms
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    • C07D213/60—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom 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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    • C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D213/60—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom 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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    • C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D213/60—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom 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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    • C07D231/10—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
    • C07D231/12—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms
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    • C07D233/56—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members with only hydrogen atoms or radicals containing only hydrogen and carbon atoms, attached to ring carbon atoms
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    • C07D401/04—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings directly linked by a ring-member-to-ring-member bond
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Abstract

La presente se refiere a compuestos con formula general (1), donde: R es hidrogeno o halogeno; R1 es -(C:::C)mR1' o -(CR'=CR'')mR1', donde R1' es: (a) halogeno, (b) ciano, o los siguientes grupos, (c) un resto de formula (2), (d) -C(O)NR'R'', (e) -C(O)O(CH2)mR5, (f) -C(O)R5, (g) -N(OH)-(CH2)mR5, (h) -NR'C(O)-(CH2)mR5, (i) -N[C(O)-R']2, (j) -OR6, (k) -(CH2)m-SR6, -(CH2)m-S(O)R6, o -(CH2)m-S(O)2R6, (l) arilo, opcionalmente sustituido por uno o más sustituyentes, seleccionados a partir de halogeno, trifluorometilo, alquilo inferior, alcoxi inferior, ciano, hidroxi, -NR'R'', nitro, -(CH2)nOR', -C(O)NR'R'', -C(O)OR' o C(O)R', (m) es un grupo heteroarilo de cinco o seis miembros, conteniendo de uno a cuatro heteroátomos, seleccionados a partir de N, O o S y puede ser opcionalmente sustituido por uno o más sustituyentes, seleccionados a partir de halogeno, trifluorometilo, alquilo inferior, alcoxi inferior, ciano, hidroxi, -NR'R'', nitro, -(CH2)nOR', -C(O)OR', -C(O)NR'R'' o -C(O)R', o (n) es una amina terciaria cíclica saturada de cinco o seis miembros, del grupo de formula (3) la cual puede contener un heteroátomo adicional, seleccionado entre N, O o S; R' y R'' son, independientemente uno de otro, hidrogeno, hidroxi, alquilo inferior, cicloalquilo o arilo, donde el alquilo inferior, grupos cicloalquilo o arilo pueden ser opcionalmente sustituidos por uno o más sustituyentes, seleccionados a partir de halogeno, trifluorometilo, alquilo inferior, alcoxi inferior, ciano, hidroxi, -NR'''R'''', nitro, -(CH2)nOR''', -C(O)NR'''R'''', -C(O)OR''' o -C(O)R'''; R''' y R'''' son, independientemente uno de otro, hidrogeno, alquilo inferior, cicloalquilo o arilo; R5 es hidrogeno, ciano, hidroxi, halogeno, trifluorometilo, -C(O)OR', -OC(O)R o arilo, opcionalmente sustituidos por uno o más sustituyentes seleccionados a partir de halogeno, trifluorometilo, alquilo inferior, alcoxi inferior, ciano, hidroxi, -NR'R'', nitro, -(CH2)nOR', -C(O)NR'R'', -C(O)OR' o -C(O)R', o es un grupo heteroarilo de cinco o seis miembros, conteniendo de uno a cuatro heteroátomos, seleccionados a partir de N, O o S y puede ser opcionalmente sustituido por uno o más sustituyentes, seleccionados a partir de halogeno, trifluorometilo, alquilo inferior, alcoxi inferior, ciano, hidroxi, -NR'R'', nitro, -(CH2)nOR', -C(O)NR'R'', -C(O)OR' o -C(O)R'; R6 es hidrogeno, alquilo inferior, trifluorometilo, o arilo, donde el alquilo inferior o el grupo arilo pueden ser opcionalmente sustituidos por uno o más sustituyentes seleccionados a partir de halogeno, trifluorometilo, alquilo inferior, alcoxi inferior, ciano, hidroxi, -NR'R'', nitro, -C(O)NR'R'', -(CH2)nOR', -C(O)OR' o -C(O)R', o es un grupo heteroarilo de cinco o seis miembros, conteniendo de uno a cuatro heteroátomos, seleccionados a partir de N, O o S y puede ser opcionalmente sustituido por uno o más sustituyentes, seleccionados a partir de halogeno, trifluorometilo, alquilo inferior, alcoxi inferior, ciano, hidroxi,, -NR'R'', nitro, -(CH2)nOR', -C(O)NR'R'', -C(O)OR' o -C(O)R'; R7 es -C(O)-(CH2)mOH o un grupo oxo; R2 es hidrogeno, alquilo inferior, alcoxi inferior, halogeno o CF3; R3 y R3' son, independientemente uno del otro, hidrogeno, alquilo inferior o forman juntos, con el átomo de C con el que se unen, un grupo cicloalquilo; R4 y R4' son, independientemente uno de otro, hidrogeno, halogeno, CF3, alquilo inferior o alcoxi inferior; R y R2 o R4 y R4' pueden ser juntos -CH=CH-CH=CH-, opcionalmente sustituido por uno o dos sustituyentes seleccionados a partir de alquilo inferior, halogeno o alcoxi inferior; X es -C(O)N(R8)-, (CH2)pO-, -(CH2)pN(R8)-, -N(R8)C(O)- o -N(R8)-(CH2)p-; donde R8 es hidrogeno o alquilo inferior; n es 1 o 2; m es 0, 1, 2, 3 o 4; o es 1 o 2; y p es 1 o 2; y sales de adicion de ácido farmacéuticamente aceptables. Se ha encontrado que los compuestos de la presente son antagonistas del receptor de la Neuroquinina 1 (NK-1, sustancia P), y por lo tanto son utiles para el tratamiento de enfermedades relacionadas con este receptor. Son objeto de la presente, medicamento, procesos para preparar el compuesto y usos.
ARP010103749A 2000-08-08 2001-08-06 Derivados de 4-fenil-piridina AR030324A1 (es)

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EP00117003 2000-08-08

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AR030324A1 true AR030324A1 (es) 2003-08-20

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MXPA03001143A (es) 2003-06-24
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IL154079A (en) 2008-03-20
HUP0301671A3 (en) 2010-03-29
ATE328871T1 (de) 2006-06-15
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