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AR041545A1 - Derivados sustituidos de 1,4-di-piperidin-4 il-piperazina y su uso como antagonistas de neuroquininas - Google Patents

Derivados sustituidos de 1,4-di-piperidin-4 il-piperazina y su uso como antagonistas de neuroquininas

Info

Publication number
AR041545A1
AR041545A1 ARP030103649A ARP030103649A AR041545A1 AR 041545 A1 AR041545 A1 AR 041545A1 AR P030103649 A ARP030103649 A AR P030103649A AR P030103649 A ARP030103649 A AR P030103649A AR 041545 A1 AR041545 A1 AR 041545A1
Authority
AR
Argentina
Prior art keywords
alkyl
group
amino
halo
radical
Prior art date
Application number
ARP030103649A
Other languages
English (en)
Original Assignee
Janssen Pharmaceutica Nv
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
Priority claimed from PCT/EP2002/014836 external-priority patent/WO2004056772A1/en
Application filed by Janssen Pharmaceutica Nv filed Critical Janssen Pharmaceutica Nv
Publication of AR041545A1 publication Critical patent/AR041545A1/es

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  • Nutrition Science (AREA)

Abstract

La presente se refiere a derivados sustituidos de 1,4-di-piperidin-4-il-piperazina que tienen actividad antagonista de las neuroquininas, en particular actividad antagonista de NK1, su preparación, composiciones que los comprenden y su uso como medicamento, en particular para el tratamiento de la emesis, ansiedad, depresión, pancreatitis y SCI. Reivindicación 1: Un compuesto de acuerdo con la fórmula (1), las sales de adición con ácidos o bases aceptables para uso farmacéutico del mismo, las formas estereoquímicamente isoméricas del mismo, la forma de N-óxido del mismo y profármaco del mismo, en donde: n es un número entero, igual a 0, 1 ó 2; m es un número entero, igual a 1 ó 2, con la condición de que si m es 2, entonces n sea 1; p es un número entero, igual a 1 ó 2; Q es O o NR3; X es un enlace covalente o un radical bivalente de fórmula -O-, -S-, o -NR3-; cada R3 independientemente uno del otro es hidrógeno o alquilo; cada R1 independientemente uno del otro se selecciona del grupo de Ar1, Ar1-alquilo y di(Ar1)-alquilo; q es un núemro entero igual a 0 ó 1; R2 es alquilo, Ar2, Ar2-alquilo, Het1 o Het1-alquilo; Y es un enlace covalente o un radical bivalente de fórmula -C(=O)- o -SO2-; cada Alk representa, independientemente uno del otro, un enlace covalente; un radical hidrocarbonado saturado o no saturado, lineal o ramificado bivalente C1-6; o un radical hidrocarbonado cíclico saturado o no saturado C3-6; cada radical opcionalmente sustituido en uno o más átomo de carbono con uno o más radicales alquilo, fenilo, halo, ciano, hidroxi, formilo y amino; L se selecciona del grupo de hidrógeno, alquiloxi, Ar3-oxi, alquiloxicarbonilo, mono- y di(alquil)amino, mono- y di(Ar3)amino, mono- y di(alquiloxicarbonil)amino, Ar3, Ar3-carbonilo, Het2 y Het2-carbonilo; Ar1 es fenilo, opcionalmente sustituido con 1, 2 ó 3 sustituyentes, cada uno independientemente uno del otro seleccionado del grupo de halo, alquilo, ciano, aminocarbonilo y alquiloxi; Ar2 es naftalenilo o fenilo, cada uno opcionalmente sustituido con 1, 2 ó 3 sustituyente, cada uno independientemente uno del otro seleccionado del grupo de halo, nitro, amino, mono- y di(alquil)amino, ciano, alquilo, hidroxi, alquiloxi, carboxilo, alquiloxicarbonilo, aminocarbonilo y mono- y di(alquil)aminocarbonilo; Ar3 es naftalenilo o fenilo, cada uno opcionalmente sustituido con 1, 2 ó 3 sustituyentes, cada uno independientemente uno del otro seleccionado del grupo de alquiloxi, alquilo, halo, hidroxi, piridinilo, morfolinilo, pirrolidinilo, imidazo[1,2-alfa]piridinilo, morfolinilcarbonilo, pirrolidinilcarbonilo, amino y ciano; Het1 es un radical heterocíclico monocíclico seleccionado del grupo de pirrolilo, pirazolilo, imidazolilo, furanilo, tienilo, oxazolilo, isoxazolilo, tiazolilo, tiadiazolilo, isotiazolilo, piridinilo, pirimidinilo, pirazinilo y piridazinilo; o un radical heterocíclico bicíclico seleccionado del grupo de quinolinilo, quinoxalinilo, indolilo, benzoimidazolilo, benzoxazolilo, benzoisoxazolilo, benzotiazolilo, benzoisotiazolilo, benzofuranilo y benzotienilo; cada radical heterocíclico puede estar sustituido opcionalmente en cualquier átomo por un radical seleccionado del grupo de halo y alquilo; Het2 es un radical heterocíclico monocíclico seleccionado del grupo de pirrolidinilo, dioxolilo, imidazolidinilo, pirrazolidinilo, piperidinilo, morfolinilo, ditianilo, tiomorfolinilo, piperazinilo, imidazolidinilo, tetrahidrofuranilo, 2H-pirrolilo, pirrolinilo, imidazolinilo, pirrazolinilo, pirrolilo, imidazolilo, pirazolilo, triazolilo, furanilo, tienilo, oxazolilo, isoxazolilo, tiazolilo, tiadiazolilo, isotiazolilo, piridinilo, pirimidinilo, pirazinilo, piridazinilo y triazinilo; o un radical heterocíclico bicíclico seleccionado del grupo de benzopiperidinilo, quinolinilo, quinoxalinilo, indolilo, isoindolilo, cromenilo, benzoimidazolilo, imidazo[1,2-alfa]piridinilo, benzoxazolilo, benzoisoxazolilo, benzotiazolilo, benzoisotiazolilo, benzofuranilo y benzotienilo; cada radical opcionalmente sustituido con uno o más radicales seleccionados del grupo de Ar1, Ar1alquilo, halo, hidroxi, alquilo, piperidinilo, pirrolilo, tienilo, oxo, alquiloxi, alquiloxialquilo y alquiloxicarbonilo; y alquilo es un radical hidrocarbonado saturado o no saturado, lineal o ramificado C1-6; o un radical hidrocarbonado cíclico saturado C3-6; opcionalmente sustituido en uno o más átomos de carbono con uno o más radicales seleccionados del grupo de radicales fenilo, halo, ciano, oxo, hidroxi, formilo y amino.
ARP030103649A 2002-10-08 2003-10-07 Derivados sustituidos de 1,4-di-piperidin-4 il-piperazina y su uso como antagonistas de neuroquininas AR041545A1 (es)

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