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AR062360A1 - Derivados heterociclicos que modulan la actividad de la estearoil-coa-desaturasa - Google Patents

Derivados heterociclicos que modulan la actividad de la estearoil-coa-desaturasa

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Publication number
AR062360A1
AR062360A1 ARP070103586A ARP070103586A AR062360A1 AR 062360 A1 AR062360 A1 AR 062360A1 AR P070103586 A ARP070103586 A AR P070103586A AR P070103586 A ARP070103586 A AR P070103586A AR 062360 A1 AR062360 A1 AR 062360A1
Authority
AR
Argentina
Prior art keywords
alkyl
cycloalkyl
group
heterocyclyl
heteroaryl
Prior art date
Application number
ARP070103586A
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English (en)
Original Assignee
Novartis Ag
Xenon Pharmaceuticals Inc
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Family has litigation
First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=39864516&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=AR062360(A1) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Novartis Ag, Xenon Pharmaceuticals Inc filed Critical Novartis Ag
Publication of AR062360A1 publication Critical patent/AR062360A1/es

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Abstract

La presente proporciona derivados heterocíclicos que modulan la actividad de la estearoil-CoA-desaturasa. También se abarcan métodos para utilizar estos derivados, con el fin de modular la actividad de la estearoil-CoA-desaturasa, y composiciones farmacéuticas que comprenden estos derivados. Reivindicacion 1: Un compuesto de la Formula (1) en donde: X es N o CH; Y es NH, O, S o N-CH3; Q es un resto del grupo de formulas (2); W se selecciona a partir de -N(R6) C(O)-, -R8-, C(O)N(R6)-, -R8- OC(O)N(R6)-, -N(R6)C(O)O-, -N(R6)C(O)N(R6)-, -O-, -S-, -N(R6)-, -S(O)t-, -N(R6)S(O)t-, -S(O)tN(R6)-, -OS(O)tN(R6)-, -R8-C(O)-, -OC(O)-, -C(O)O-, -N(R6)C(=N(R6a))N(R6)-, -N(R6)((R6a)N=)C-, -C(N(R6a))N(R6)-, o un enlace directo; V se selecciona a partir de -C(O)N(R6)-, -S(O)t-, -S(O)2N(R6)-, -C(O)-, -R8-C(O)O-, -C(=N(R6a))N(R6)-, o un enlace directo; n es 1, 2, o 3; p es 0, 1, 2, hasta 2n; t es 1 o 2; R1 se selecciona a partir del grupo que consiste en halogeno, hidrogeno, alquilo, alquenilo, alquinilo, alcoxilo, hidroxi-alquilo, alcoxi-alquilo, cicloalquilo, cicloalquil-alquilo, arilo, aralquilo, heterociclilo, heterociclil-alquilo, heteroarilo, o heteroaril-alquilo; o R1 es una estructura de multiples anillos que tiene de 2 a 4 anillos, en donde los anillos se seleccionan independientemente a partir del grupo que consiste en cicloalquilo, heterociclilo, arilo, y heteroarilo, y en donde algunos o todos los anillos pueden estar fusionados unos con otros; R2 se selecciona a partir del grupo que consiste en hidrogeno, alquilo, alquenilo, alquinilo, alcoxilo, hidroxi-alquilo, alcoxi-alquilo, cicloalquilo, cicloalquil-alquilo, arilo, halo-alquilo, aralquilo, heterociclilo, heterociclil-alquilo, heteroarilo, o heteroalquil-alquilo; o R2 es una estructura de multiples anillos que tiene de 2 a 4 anillos, en donde los anillos se seleccionan independientemente a partir del grupo que consiste en cicloalquilo, heterociclilo, arilo, y heteroarilo, y en donde algunos o todos los anillos pueden estar fusionados unos con otros; R3 se selecciona a partir del grupo que consiste en hidrogeno, alquilo, alquenilo, alquinilo, alcoxilo, hidroxi-alquilo, alcoxi-alquilo, cicloalquilo, cicloalquil-alquilo, heterociclilo, arilo, aralquilo, heteroarilo, halogeno, halo-alquilo, haloalcoxilo, ciano, o -N(R6)2; R4 y R4a se selecionan independientemente a partir del grupo que consiste en hidrogeno, alquilo, halo-alquilo, hidroxilo, hidroxi-alquilo, alcoxilo, cicloalquil-alquilo, o aralquilo; o R4 y R4a forman juntos un grupo oxo (=O) o un cicloalquilo; R5 se selecciona a partir del grupo que consiste en alquilo, arilo, cicloalquilo, heteroarilo, heterociclilo, hidroxi-alquilo, alcoxilo, cicloalquil-alquilo, aralquilo, -N(R6)C(O)R2, -C(O)N(R6)R2, -OC(O)N(R6)R2, -N(R6)C(O)OR2, -N(R6)C(O)N(R6)R2, -OR2, -SR2-, -N(R6)R2, -S(O)tR2, -N(R6)S(O)2R2, -S(O)2N(R6)R2, -OS(O)2N(R6)R2, -C(O)R2, -OC(O)R2, -(O)OR2, -N(R6)C(=N(R6a))N(R6)R2, - N(R6)C(=S)N(R6)R2, -N(R6)((R6a)N=)CR2, o -C(=N(R6a))N(R6)R2; cada R6 se selecciona independientemente a partir del grupo que consiste en hidrogeno, alquilo, hidroxi-alquilo, cicloalquil-alquilo, arilo, heteroarilo, heterociclilo, o aralquilo; cada R6a se selecciona independientemente a partir del grupo que consiste en hidrogeno, alquilo, cicloalquil-alquilo, o ciano; cada R7 se selecciona independientemente a partir del grupo que consiste en hidrogeno, alquilo, trifluoro-metilo, arilo, cicloalquilo, heteroarilo, heterociclilo, hidroxi-alquilo, cicloalquil-alquilo, oaralquilo; y cada R8 es independientemente un enlace directo, una cadena de alquileno de cadena recta o ramificada opcionalmente sustituida, una cadena de alquenileno de cadena recta o ramificada opcionalmente sustituida, o una cadena de alquinileno de cadena recta o ramificada opcionalmente sustituida; así como un estereoisomero, enantiomero, o tautomero de los mismos, una sal farmacéuticamente aceptable de los mismos, una composicion farmacéutica de los mismos, o un profármaco de los mismos.
ARP070103586A 2006-08-15 2007-08-13 Derivados heterociclicos que modulan la actividad de la estearoil-coa-desaturasa AR062360A1 (es)

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