AR042653A1 - Derivados sustiuidos de 1- piperidin -3- il- 4- piperidin 4- -il- piperazina y su uso como antagonistas de taquiquininas - Google Patents

Derivados sustiuidos de 1- piperidin -3- il- 4- piperidin 4- -il- piperazina y su uso como antagonistas de taquiquininas

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AR042653A1
AR042653A1 ARP030104779A ARP030104779A AR042653A1 AR 042653 A1 AR042653 A1 AR 042653A1 AR P030104779 A ARP030104779 A AR P030104779A AR P030104779 A ARP030104779 A AR P030104779A AR 042653 A1 AR042653 A1 AR 042653A1
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disorders
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halo
optionally substituted
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Abstract

La presente se refiere a derivados sustituidos de 1piperidin-3-il-4-piperidin-4-il-piperazina que tienen actividad antagonista de las neuroquininas, en particular actividad antagonista de NK1, una actividad antagonista combinada de NK1/NK3, y una actividad antagonista combinada de NK1/NK2/NK3, a su preparación a las composiciones que los comprenden y a su uso como medicamento, en particular para el tratamiento de la esquizofrenia, emesis, ansiedad y depresión, síndrome de intestino irritable (IBS), trastornos de ritmo circadiano, dolor visceral, inflamación neurogénica, asma, desórdenes de la micturación tales como incontinencia urinaria y nocicepción. En vista de su capacidad para antagonizar las acciones de las taquininas por bloqueo de los receptores de neuroquininas, y en particular antagonizar las acciones de la sustancia P, Neuroquinina A y neuroquinina B por bloqueo del receptor NK1, NK2 y NK3, los compuestos de acuerdo con la presente son útiles como medicamentos, en particular en el tratamiento profiláctico y terapéutico de condiciones intermediadas por taquininas, tales como, por ejemplo, trastornos del SNC, en particular desórdenes esquizoafectivos, depresión, trastornos de ansiedad, trastornos relacionados con el estrés, trastornos del sueno, trastornos cognitivos, trastornos de la personalidad, trastornos de la alimentación, trastornos neurodegenerativos, trastornos de adicción, trastornos del ánimo, disfunción sexual, dolor y otras condiciones relacionadas con el SNC; inflamación, trastornos alérgicos; emesis; trastornos gastrointestinales, en particular el síndrome de intestino irritable (IBS); trastornos de la piel; trastornos vasoespásticos; enfermedades fibrosantes y del colágeno; trastornos relacionados con incremento o la supresión inmune y enfermedades reumáticas y control del peso corporal. Reivindicación 1: Un compuesto de acuerdo con la fórmula general (1), sales de adición con ácidos o bases aceptables para uso farmacéutico de los mismos, las formas estereoquímicamente isoméricas de los mismos, la forma de N-óxidos de los mismos y profármacos de los mismos, en donde: n es un número entero, igual a 0, 1 o 2; m es un número entero, igual a 1 o 2, con la condición de que si m es 2, entonces n sea 1; p es un número entero, igual a 1 o 2; q es un entero igual a 0 o 1; 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 H o alquilo; cada R1 independientemente uno del otro se selecciona del grupo de Ar1, Ar1-alquilo y di(Ar1)-alquilo; R2 es Ar2, Ar2-alquilo, di(Ar2)alquilo, Het1 o Het1-alquilo; Y es un enlace covalente o un radical bivalente de fórmula -C(=O)-, -SO2-;>C=CH-R o >C=N-R, donde R es CN o nitro; cada Alk representa, independientemente uno del otro, un enlace covalente; un radical hidrocarbonado saturado o no saturado, lineal o ramificado bivalente que tiene de 1 a 6 átomos de C; o un radical hidrocarbonado cíclico saturado o no saturado que tiene de 3 a 6 átomos de C; donde cada radical está opcionalmente sustituido en uno o más átomos de C con uno o más radicales fenilo, halo, ciano, hidroxi, formilo y amino; L se selecciona del grupo de H, alquilo, alquiloxi, Ar3-oxi, alquiloxicarbonilo, alquilcarboniloxi, mono- y di(alquil)amino, mono- y di(Ar3)amino, Ar3, Ar3-carbonilo, Het2 y Het2-carbonilo; Ar1 es fenilo, opcionalmente sustituido con 1, 2 o 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 o 3 sustituyentes, cada uno independientemente uno del otro seleccionado del grupo de halo, amino, mono- y di(alquil)amino, ciano, alquilo, hidroxi, alquiloxi, carboxilo, alquiloxicarbonilo, aminocarbonilo y mono- y di(alquil)aminocarbonilo; Ar3 es naftalenilo o fenilo, opcionalmente sustituido con 1, 2 o 3 sustituyentes, cada uno independientemente uno del otro seleccionado del grupo de alquiloxi, alquilo, halo, hidroxi, Ar1carboniloxicarbonilo, 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, isotiazolilo, piridinilo, pirimidinilo, pirazinilo y piridazinilo; o un radical heterocíclico bicíclico seleccionado del grupo de quinolinilo, quinoxalinilo, indolilo, benzimidazolilo, benzoxazolilo, bencisoxazolilo, benzotiazolilo, bencisotiazolilo, benzofuranilo y benzotienilo; y 4a,8a-dihidro-2H-cromenil, cada radical heterocíclico puede estar sustituido opcionalmente en cualquier átomo con uno o más radicales seleccionados del grupo de halo, oxo y alquilo; Het2 es un radical heterocíclico monocíclico seleccionado del grupo de tetrahidrofuranilo, pirrolidinilo, dioxolilo, imidazolidinilo, pirrazolidinilo, piperidinilo, morfolinilo, ditianilo, tiomorfolinilo, piperazinilo, imidazolidinilo, tetrahidrofuranilo, 2H-pirrolilo, pirrolinilo, imidazolinilo, pirazolinilo, 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, benzimidazolilo, imidazo[1,2-alfa]piridinilo, benzoxazolilo, bencisoxazolilo, benzotiazolilo, bencisotiazolilo, benzofuranilo y benzotienilo, benzo[2,1,3]oxadiazolilo, imidazo[2,1-b]tiazolilo, 2,3-dihidrobenzo[1,4]dioxilo, y octahidrobenzo[1,4]dioxilo; cada radical puede estar opcionalmente sustituido con uno o más radicales seleccionados del grupo de Ar1, Ar1alquilo, Ar1alquiloxialquilo, halo, hidroxi, alquilo, alquilcarbonilo, alquiloxi, alquiloxialquilo alquiloxicarbonilo; piperidinilo, piridinilo, pirrolilo, tienilo, oxo y oxazolilo; y alquilo es un radical hidrocarbonado saturado o no saturado, lineal o ramificado que tiene de 1 a 6 átomos de C; o un radical hidrocarbonado cíclico saturado que tiene de 3 a 6 átomos de C; opcionalmente sustituido en uno o más átomos de C con uno o más radicales seleccionados del grupo de radicales fenilo, halo, ciano, oxo, hidroxi, formilo y amino.
ARP030104779A 2002-12-23 2003-12-22 Derivados sustiuidos de 1- piperidin -3- il- 4- piperidin 4- -il- piperazina y su uso como antagonistas de taquiquininas AR042653A1 (es)

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BRPI0509803A (pt) 2004-04-13 2007-09-18 Incyte Corp derivados de piperazinilpiperidina como antagonistas de receptor de quimiocina
GB0417702D0 (en) * 2004-08-09 2004-09-08 Merck Sharp & Dohme New uses
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WO2014142761A1 (en) * 2013-03-15 2014-09-18 Nanyang Technological University 3-piperidone compounds and their use as neurokinin-1 (nk1) receptor antagonists
EP3160469B1 (en) 2014-06-25 2021-04-28 Emory University Methods of managing conditioned fear with neurokinin receptor antagonists

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HRP20050554B1 (hr) 2014-02-28
NO20053598L (no) 2005-09-20
KR20050085217A (ko) 2005-08-29
TW200503715A (en) 2005-02-01
NO20053598D0 (no) 2005-07-22
JP4660198B2 (ja) 2011-03-30
CA2509088C (en) 2012-01-24
EA008774B1 (ru) 2007-08-31
CN1728999A (zh) 2006-02-01
WO2004056364A1 (en) 2004-07-08
MXPA05006888A (es) 2005-08-16
DE60317709T2 (de) 2008-10-30
US7572786B2 (en) 2009-08-11
UA83474C2 (uk) 2008-07-25
PL214705B1 (pl) 2013-09-30
DE60317709D1 (de) 2008-01-03
MY134383A (en) 2007-12-31
EA200501040A1 (ru) 2005-12-29
IL169337A (en) 2011-07-31
HRP20050554A2 (en) 2006-06-30
PL376075A1 (en) 2005-12-12
JP2006512348A (ja) 2006-04-13
ES2297275T3 (es) 2008-05-01
US20060252747A1 (en) 2006-11-09
AU2003300578B2 (en) 2009-06-04
CA2509088A1 (en) 2004-07-08
AU2003300578A1 (en) 2004-07-14
PA8593201A1 (es) 2004-07-26
TWI327916B (en) 2010-08-01
HK1087924A1 (en) 2006-10-27
JO2485B1 (en) 2009-01-20
KR101049075B1 (ko) 2011-07-15
CL2003002722A1 (es) 2005-04-08
IL169337A0 (en) 2007-07-04
NO331173B1 (no) 2011-10-24
NZ541036A (en) 2007-07-27

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