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CO5261559A1 - Antagonistas de neurokinina selectivos - Google Patents

Antagonistas de neurokinina selectivos

Info

Publication number
CO5261559A1
CO5261559A1 CO00095391A CO00095391A CO5261559A1 CO 5261559 A1 CO5261559 A1 CO 5261559A1 CO 00095391 A CO00095391 A CO 00095391A CO 00095391 A CO00095391 A CO 00095391A CO 5261559 A1 CO5261559 A1 CO 5261559A1
Authority
CO
Colombia
Prior art keywords
alkyl
mfi
jpeg
cycloalkyl
heteroaryl
Prior art date
Application number
CO00095391A
Other languages
English (en)
Inventor
Neng-Yang Shin
Shue Ho-Jane
Gregory Adam Reichard
Paliwal Sunil
David J Blythin
John J Piwinski
Xiao Dong
Chen Xiao
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 CO5261559A1 publication Critical patent/CO5261559A1/es

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    • C07D239/08—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine 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 directly attached in position 2
    • C07D239/10—Oxygen or sulfur atoms
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Abstract

Se describe un compuesto representado por la fórmula estructural <EMI FILE="00095391_1" ID="1" IMF=JPEG >o su sal farmacéuticamente aceptable, en donde Ar1 y Ar2 son heteroarilo optativamente sustituido o fenilo optativamente sustituido; X1 es O-, -S-, -SO-, -SO2-, -NR12-, NCOR12 -o- NR12SO2R15-; <EMI FILE="00095391_2" ID="2" IMF=JPEG >Se seleccionan entre el grupo que consiste en <EMI FILE="00095391_3" ID="3" IMF=JPEG > X2 es -O -, -S -o -NR5-; Y es =O, =S o =NR11; Y1 es H, alquilo C1-C6, -NR17R13, -SCH3, R19-aril(CH2)n6-, R19-heteroaril-(CH2)n6-, -(CH2)n6- heterocicloalquil, -(C1-C3)alquil-NH-C(O)O(C1-C6)alquilo o -NHC(O)R15; R5 es H o -(CH2)n1-G, en donde n1 es 0-5, G es H, -CF3, -CHF2, -CH2F, OH, -O-(alquilo C1-C6), -SO2R13, -O-(cicloalquilo C3-C8), -NR13R14, -SO2NR13R14, -NR13SO2R15, -NR13COR12, -NR12(CONR13R14), -CONR13R14, -COOR12, cicloalquilo C3-C8, R19-arilo, R19-heteroarilo, y siempre y cuando n1 = 0, G no es H; R1, R2, R3 y R7 son H, alquilo, cicloalquilo, -CHF2, -CH2F o -CF3; o R1 y R2, junto con el carbono al cual están unidos, forman un anillo alquileno; o R1 y R2 juntos son =O; R6 es R7 o -OH; y las variables restantes son como se definieron en la memoria descriptiva, también se describen métodos para el tratamiento de enfermedades susceptibles de tratamiento con antagonistas de neurokinina con dichos compuestos, y composiciones farmacéuticas que comprenden a dichos compuestos. También se describen composiciones farmacéuticas que comprenden una cantidad efectiva de un compuesto de acuerdo con la reivindicación 1, por lo menos un portador farmacéuticamente aceptable, y en combinación con una cantidad efectiva de un inhibidor de la recaptación de serotonina selectivo.
CO00095391A 1999-12-17 2000-12-14 Antagonistas de neurokinina selectivos CO5261559A1 (es)

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