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AR039084A1 - Antagonistas nk1 - Google Patents

Antagonistas nk1

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Publication number
AR039084A1
AR039084A1 ARP030100861A ARP030100861A AR039084A1 AR 039084 A1 AR039084 A1 AR 039084A1 AR P030100861 A ARP030100861 A AR P030100861A AR P030100861 A ARP030100861 A AR P030100861A AR 039084 A1 AR039084 A1 AR 039084A1
Authority
AR
Argentina
Prior art keywords
group
alkyl
independently selected
cycloalkyl
nr15r16
Prior art date
Application number
ARP030100861A
Other languages
English (en)
Original Assignee
Schering Corp
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 Schering Corp filed Critical Schering Corp
Publication of AR039084A1 publication Critical patent/AR039084A1/es

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    • C07D207/18—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having one double bond between ring members or between a ring member and a non-ring member
    • C07D207/22—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom 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
    • C07D207/24—Oxygen or sulfur atoms
    • C07D207/26—2-Pyrrolidones
    • C07D207/263—2-Pyrrolidones with only hydrogen atoms or radicals containing only hydrogen and carbon atoms directly attached to other ring carbon atoms
    • C07D207/27—2-Pyrrolidones with only hydrogen atoms or radicals containing only hydrogen and carbon atoms directly attached to other ring carbon atoms with substituted hydrocarbon radicals directly attached to the ring nitrogen atom
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Abstract

Un antagonista de NK1 que tiene la fórmula (1), con las variables aquí definidas, que es útil para el tratamiento de una variedad de desordenes que incluyen émesis, depresión, ansiedad y tos. Reivindicación 1: Un compuesto que tiene la fórmula (1), o sus sales o solvatos farmacéuticamente aceptables, en la cual: Ar1 y Ar2 están cada uno independientemente seleccionados del grupo que consiste en: a) heteroarilo; b) heteroarilo sustituido con (R21)r; y c) un compuesto de fórmula (2); X1 está seleccionado del grupo que consiste en -O-, -S-, -SO-, -SO2-, -NR20-, -N(COR20)- y -N(SO2R17)-; y cuando X1 está seleccionado del grupo que consiste en -SO-, -SO2-, -N(COR20)- y -N(SOR2R17), entonces, R1 y R2 están cada uno independientemente seleccionados del grupo que consiste en H, alquilo C1-6, hidroxi(alquilo C1-3)-, cicloalquilo C3-8, -CH2F, -CHF2 y -CF3; o R1 y R2 conjuntamente con el átomo de carbono al cual están ambos unidos forman un anillo cicloalquilo C3-6; y cuando X1 está seleccionado del grupo que consiste en -O-, -S-, y -NR20-, entonces R1 y R2 están cada uno independientemente seleccionados del grupo que consiste en H, alquilo C1-6, hidroxi(alquilo C1-3)-, cicloalquilo C3-8, -CH2F, -CHF2 y -CF3; o R1 y R2 conjuntamente con el átomo de carbono al cual están ambos unidos, forman un grupo cicloalquilo C3-8, o R1 y R2 conjuntamente con el átomo de carbono al cual están ambos unidos forman un grupo -C(=O); R3 está seleccionado del grupo que consiste en H, alquilo C1-6, hidroxi(alquilo C1-3)-, cicloalquilo C3-8, -CH2F, -CHF2 y -CF3; R4 y R5 están cada uno independientemente seleccionados del grupo que consiste en H, alquilo C1-6, halógeno, -OR20, -O-C(O)NR15R16, -NR15SO2R17, -NR15C(O)R14, -NR20C(O)NR15R16 y -SR20; o R4 y R5 conjuntamente con el átomo de carbono al cual están ambos unidos forman un grupo -C(=O)- o -C(=NR13); R6 es -(CH2)n1-G donde n1, es 0 a 5, donde G está seleccionado del grupo que consiste en: H, -OH, -O-(alquilo C1-6), -O-(cicloalquilo C3-8), -O-C(O)NR15R16, -NR15R16, -NR15SO2R17, -NR15C(O)R14, -NR20C(O)NR15R16, -C(O)NR15R16, -C(O)OR20, cicloalquilo C3-8; y un resto seleccionado del grupo de fórmulas (3); X4 está seleccionado del grupo que consiste en -O-, -S-, y un resto de fórmula (4); R7 es -(CR40R41)n6-J donde R40 y R41 están cada uno independientemente seleccionados del grupo que consiste en H y alquilo C1-2, y n6 es 0 a 5, y J está seleccionado del grupo que consiste en H, -CF3, , -CHF2, -CH2F, -OH, -O-(alquilo C1-6), -SO2R15, -O-(cicloalquilo C3-8), -O-C(O)NR15R16, -NR15R16, -SO2NR15R16, -NR15SO2R17, -NR15C(O)R14, -NR20C(O)NR15R16, -C(O)NR15R16, -C(O)OR20, cicloalquilo C3-8 y un resto seleccionado del grupo de fórmulas (3) o un compuesto de fórmula (5), con la condición de que: a) cuando R6 es -(CH2)n1-G, donde n1 es 0, entonces G está seleccionado del grupo que consiste en -OH, -O-(alquilo C1-6), -O-(cicloalquilo C3-8), -O-C(O)NR15R16, -NR15R16, - NR15SO2R17, -NR15C(O)R14, -NR20C(O)NR15R16 y un resto del grupo de fórmulas (3); b) R7 es -(CR40R41)n6-J, donde n6 es 0, entonces J está seleccionado del grupo que consiste en H, -CF3, -CHF2, -CH2F, -C(O)NR15R16, -C(O)NR15R16, -C(O)OR20 y un compuesto de fórmula (5); c) cuando n1 para R6 es 0, y n6 para R7 es 0, y uno de R6 y R7 están unidos a través de un heteroátomo al carbono del anillo ciclobutano entonces el otro de R6 y R7 está unido a través de un átomo de carbono al carbono del anillo ciclobutano; ó R6 y R7, conjuntamente con el átomo de carbono al cual están ambos unidos forman un grupo; ó R6 y R7 tomados conjuntamente con el átomo de carbono al cual están unidos forman: a) un anillo de carbono de 4 a 7 miembros; b) un anillo heterocicloalquilo de 4 a 7 miembros; ó c) un anillo de heterocicloalquenilos de 4 a 7 miembros; donde dicho heterocicloalquilo o dicho heterocicloalquenilo comprende de 1 a 4 heteroátomos independientemente seleccionados del grupo que consiste en -O-, -S-, -S(O)-, -SO2-, -N=, y -NR20- (donde R20 es tal como se ha definido en lo que sigue), con la condición de que un anillo -S- en dichos anillos heterocicloalquilo y dichos anillos heterocicloalquenilos no están unidos a otro anillo -S- o anillo -S(O)- o anillo -O-, y con la condición de que un anillo -O-; en dichos anillos heterocicloalquilo y heterocicloalquenilo no está ligado a otro anillo -O-; dichos anillos de 4 a 7 miembros están opcionalmente sustituidos con de 1 a 4 sustituyentes R45 en los cuales cada sustituyente R45 está independientemente seleccionado; R8 y R9 están cada uno independientemente seleccionados del grupo que consiste en H, alquilo C1-6, halógeno, -OR20, -O-C(O)NR15R16, -NR15R16,-NR15C(O)R14, -NR20C(O)NR15R16 y -SR20; o R8 y R9, tomados conjuntamente con el átomo de carbono al cual están ambos unidos, forman un grupo -C(=O)-; R10, R11 y R12 están cada uno independientemente seleccionados del grupo que consiste en H, alquilo C1-6, cicloalquilo C3-8, -OR20, halógeno, -CN, -NO2,-CF3, -CHF2, -CH2F, -CH2CF3, -OCF3, -OCHF2, -OCH2CF3, -C(O)OR20, -C(O)NR23R24, -NR23C(O)R20, -NR23CO2R17, -NR23C(O)NR23R24, -NR23SO2R17, -NR23R24, -SO2NR23R24, -S(O)n5R17, arilo, arilo sustituido con (R21)r donde cada sustituyente R21 está independientemente seleccionado, heteroarilo, y heteroarilo sustituido con (R21)r donde cada sustituyente R21 está independientemente seleccionado; cada R13 está independientemente seleccionado del grupo que consiste en -OH y -O-(alquilo C1-6); cada R14 está independientemente seleccionado del grupo que consiste en H, alquilo C1-6, cicloalquilo C3-8, alquilo (C1-6)NH2 y alquilo (C1-6)NHC(O)O-alquilo (C1-6); R15 y R16 están cada uno independientemente seleccionados del grupo que consiste en H, bencilo, alquilo C1-6 y cicloalquilo C3-8; o R15 y R16 conjuntamente con el átomo de nitrógeno al cual están ambos unidos forman un anillo de 4 a 7 miembros que está opcionalmente sustituido con -OR20, y donde uno de los átomos de carbono en dicho anillo de 4 a 7 miembros es opcionalmente reemplazado con un heteroátomo seleccionado del grupo que consiste en -O-, -S- y -NR20-; cada R17 está independientemente seleccionado del grupo que consiste en alquilo C1-6, cicloalquilo (C3-8)-CF3; cada R20 está independientemente seleccionado del grupo que consiste en H, alquilo C1-6, cicloalquilo C3-8, alquilo (C1-6)NH2, alcoxi(C1-6)-alquilo(C2-6), e hidroxi-alquilo C2-6; cada R21 es un sustituyente en el anillo arilo o heteroarilo al cual está unido y está independientemente seleccionado del grupo que consiste en alquilo C1-6, cicloalquilo C3-8, -OH, -halógeno, -CN, -NO2, -CF3, -CHF2, -CH2F, -OCF3, -OCHF2, OCH2F,-O-alquilo C1-6, -O-cicloalquilo C3-8; -C(O)OR20, -C(O)NR23R24, -NR23R24, NR23C(O)R20, -NR23CO2R20, -NR23C(O)NR23R24, -NR23SO2R17 Y -S(O)n5R17; R22 está seleccionado del grupo que consiste en H, alquilo C1-6, cicloalquilo C3-8 y -(CH2)n4-heterociclolaquilo; R23 y R24 están cada uno independientemente seleccionados del grupo que consiste en H, alquilo C1-6, cicloalquilo C3-8 y bencilo; o R23 y R24 conjuntamente con el átomo de nitrógeno al cual están ambos unidos forman un anillo de 4 a 7 miembros que está opcionalmente sustituido con -OR20, donde uno de los átomos de carbono en el anillo está opcionalmente reemplazado con un heteroátomo seleccionado del grupo que consiste en-O-, -S- y -NR20-; R25 y R26 están cada uno independientemente seleccionados del grupo que consiste en H y alquilo C1-6; o R25 y R26 conjuntamente con el átomo de carbono al cual están unidos forman un grupo -C(=O)- o ciclopropilo; R27 y R28 están cada uno independientemente seleccionados del grupo que consiste en H y alquilo C1-6; o R27 y R28 conjuntamente con el átomo de carbono al cual están ambos unidos forman un grupo -C(=O)- o ciclopropilo; cada R29 está independientemente seleccionado del grupo que consiste en H, alquilo C1-6 y cicloalquilo C3-8; R30 y R31 están cada uno independientemente seleccionados del grupo que consiste en H, alquilo C1-6 (por ejemplo alquilo C1-2) -CH2F,-CHF2, CF3, -OH, y -O(alquilo C1-3); o R30 y R31 conjuntamente con el átomo de carbono al cual están unidos forman un grupo -C(=O)-; R38 y R39 están cada uno independientemente seleccionados del grupo que consiste en H y alquilo C1-6; o R38 y R39 conjuntamente con el átomo de carbono al cual están ambos unidos, forman un grupo ciclopropilo; cada R45 está independientemente seleccionado del grupo que consiste en: alquilo C1-6 (por ejemplo alquilo C1-2), -CH2F, -CHF2, -CF3,-OH, y -O(alquilo C1-3); o dos sustituyentes R45 conjuntamente con el átomo de carbono al cual están ambos unidos, forman un grupo -C(=O)-; X2 está seleccionado del grupo que consiste en -CH2-, -NR22-, -N(C(O)NR15R16)-, -N(CO2R17)-, -N(C(O)R20)-, -O-, -S-, -S(O)-, -SO2-, -CF2- y -CR20F-; r es de 1 a 3; n2 es de 1 a 4; n3 es de 0 a 2; n4 es de 0 a 3; n5 es de 0 a 2; n8 es de 0 a 4; y n9 es de 0 a 3; con la condición de que cuando n3 es O, y R27 y R28 son cada uno H, entonces X2 está seleccionado del grupo que consiste en -CH2-, S(O)-, -SO2-, -CF2- y -CR20F-.
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