AR060173A1 - Derivados de piridina y de pirimidina como antagonistas del mglur2, metodos para su preparacion, composiciones farmaceuticas que los contienen y su uso en la fabricacion de medicamentos para el tratamiento de trastornos del snc. - Google Patents

Derivados de piridina y de pirimidina como antagonistas del mglur2, metodos para su preparacion, composiciones farmaceuticas que los contienen y su uso en la fabricacion de medicamentos para el tratamiento de trastornos del snc.

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Publication number
AR060173A1
AR060173A1 ARP070101287A ARP070101287A AR060173A1 AR 060173 A1 AR060173 A1 AR 060173A1 AR P070101287 A ARP070101287 A AR P070101287A AR P070101287 A ARP070101287 A AR P070101287A AR 060173 A1 AR060173 A1 AR 060173A1
Authority
AR
Argentina
Prior art keywords
alkyl
optionally substituted
group
halogen
alkoxy
Prior art date
Application number
ARP070101287A
Other languages
English (en)
Inventor
Silvia Gatti Mcarthur
Thomas Woltering
Erwin Goetschi
Juergen Wichmann
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
Family has litigation
First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=36862654&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=AR060173(A1) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Hoffmann La Roche filed Critical Hoffmann La Roche
Publication of AR060173A1 publication Critical patent/AR060173A1/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
    • C07D213/24—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 substituted hydrocarbon radicals attached to ring carbon atoms
    • C07D213/28—Radicals substituted by singly-bound oxygen or sulphur atoms
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    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
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Abstract

Compuestos de la formula (1), a un proceso para su obtencion, a su utilizacion para la fabricacion de medicamentos destinados al tratamiento de trastornos del SNC y a composiciones farmacéuticas que los contienen. Reivindicacion 1: Un compuesto de la formula (1) en la que: o bien uno de X o Y es N y el otro es CH, o bien X e Y son, ambos, N; A es arilo o heteroarilo de 5 o 6 eslabones, cada uno de ellos está opcionalmente sustituido por alquilo C1-6; B es H, ciano o, es un arilo opcionalmente sustituido o un heteroarilo de 5 o 6 eslabones opcionalmente sustituido, los sustituyentes se eligen entre el grupo formado por: halogeno; nitro; alquilo C1-6 opcionalmente sustituido por hidroxi, NRaRb, en el que Ra y Rb son con independencia H, alquilo C1-6 o -(CO)-alquilo C1-6; -S-alquilo C1-6; -(SO2)-OH; -(SO2)-alquilo C1-6; -(SO2)-NRcRd, en el que Rc y Rd son con independencia: H, alquilo C1-6 opcionalmente sustituido por hidroxi, haloalquilo C1-6, alcoxi C1-6, -(CO)-alquilo C1-6 opcionalmente sustituido por alcoxi C1-6, -(CH2CH2O)nCHRe, en el que Re es H o CH2OH y n es 1, 2, 3, 4, 5, 6, 7, 8, 9 o 10, -(CH2)m-arilo, en el que m es 1 o 2 y el arilo está opcionalmente sustituido por halogeno o alcoxi C1-6, -(CH2)p-cicloalquilo C3-6, en el que p es 0 o 1, heterocicloalquilo de 5 o 6 eslabones; -(SO2)-NRfRg, en el que Rf y Rg junto con el átomo de nitrogeno al que están unidos forman un anillo heterocicloalquilo de 4, 5 o 6 eslabones que puede contener opcionalmente otro heteroátomo elegido entre nitrogeno, oxígeno, azufre y un grupo SO2, dicho anillo heterocicloalquilo de 4, 5 o 6 eslabones está opcionalmente sustituido por: un sustituyente elegido entre el grupo formado por hidroxi, alquilo C1-6, alcoxi C1-6 que está opcionalmente sustituido por hidroxi y heteroariloxi de 5 o 6 eslabones; NHSO2-alquilo C1-6; NHSO2-NRhRi en el que Rh y Ri son con independencia H, alquilo C1-6, -(CO)O-alquilo C1-6, o Rh y Ri junto con el átomo de nitrogeno al que están unidos forman un anillo heterocicloalquilo de 4, 5 o 6 eslabones que puede contener opcionalmente otro heteroátomo elegido entre nitrogeno, oxígeno y azufre, dicho anillo heterocicloalquilo de 4, 5 o 6 eslabones está opcionalmente sustituido por alquilo C1- 6; R1 es H, halogeno, alquilo C1-6 opcionalmente sustituido por hidroxi, alcoxi C1-6, haloalquilo C1-6, cicloalquilo C3-6; R2 es H, ciano, halogeno, haloalquilo C1-6, alcoxi C1-6, haloalcoxi C1-6, alquilo C1-6 o cicloalquilo C3-6; R3 es halogeno, H, alcoxi C1-6, haloalquilo C1-6, alquilo C1-6, cicloalquilo C3-6, haloalcoxi C1-6, o es NRjRk en el que Rj y Rk se eligen con independencia entre el grupo formado por: H, cicloalquilo C3-8, arilo, heteroarilo que tiene de 5 a 12 átomos en el anillo y alquilo C1-6 que está opcionalmente sustituido por uno o más sustituyentes elegidos entre el grupo formado por halogeno, hidroxi, cicloalquilo C3-8, arilo, heteroarilo que tiene de 5 a 12 átomos en el anillo y -NRlRm, en el que Rl y Rm se eligen con independencia entre el grupo formado por H y alquilo C1-6; o Rj y Rk junto con el átomo de nitrogeno al que están unidos pueden formar un grupo heterocíclico opcionalmente sustituido, que tiene de 5 a 12 átomos en el anillo y puede contener opcionalmente otro heteroátomo elegido entre nitrogeno, oxigeno y azufre, dicho grupo heteroarilo está opcionalmente sustituido por uno, dos, tres, cuatro o cinco sustituyentes elegidos entre el grupo formado por halogeno, hidroxi, alquilo C1-6 y haloalquilo C1-6; o R2 y R3 pueden formar, juntos, un puente dioxo; R4 es H o halogeno; así como sus sales farmacéuticamente aceptables.
ARP070101287A 2006-03-29 2007-03-28 Derivados de piridina y de pirimidina como antagonistas del mglur2, metodos para su preparacion, composiciones farmaceuticas que los contienen y su uso en la fabricacion de medicamentos para el tratamiento de trastornos del snc. AR060173A1 (es)

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JP2009531370A (ja) 2009-09-03
DK2001849T3 (en) 2014-12-15
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IL194039A (en) 2015-01-29
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