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AR084474A1 - Compuestos heterociclicos como inhibidores de dgat1 - Google Patents

Compuestos heterociclicos como inhibidores de dgat1

Info

Publication number
AR084474A1
AR084474A1 ARP110103235A AR084474A1 AR 084474 A1 AR084474 A1 AR 084474A1 AR P110103235 A ARP110103235 A AR P110103235A AR 084474 A1 AR084474 A1 AR 084474A1
Authority
AR
Argentina
Prior art keywords
heterocyclyl
aryl
alkyl
cycloalkyl
nrprq
Prior art date
Application number
Other languages
English (en)
Inventor
Rajiv Sharma
Kishorkumar Shivajirao Kadam
Ravindra Dnyandev Jadhav
Shivaji Sadashiv Kandre
Amol Gupte
Original Assignee
Piramal Life Sciences Ltd
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 Piramal Life Sciences Ltd filed Critical Piramal Life Sciences Ltd
Publication of AR084474A1 publication Critical patent/AR084474A1/es

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    • C07D417/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
    • C07D417/04—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings directly linked by a ring-member-to-ring-member bond
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    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/4245—Oxadiazoles
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    • C07D207/02—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D207/30—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having two double bonds between ring members or between ring members and non-ring members
    • C07D207/32—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having two double bonds between ring members or between ring members and non-ring members with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms
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    • C07D231/02—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings
    • C07D231/10—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
    • C07D231/12—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms
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    • C07D263/32—Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms
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  • Gastroenterology & Hepatology (AREA)

Abstract

Procesos de obtención y composiciones farmacéuticas.Reivindicación 1: Un compuesto de la fórmula (1) o un estereoisómero, tautómero, sal farmacéuticamente aceptable, solvato o N-óxido de los mismos; donde, Z se selecciona del grupo de fórmulas (2); - - - indica el punto de fijación; n es un entero seleccionado de 1 - 5; m es 0 ó 1; R1 y R2 se seleccionan independientemente de hidrógeno o alquilo C1-12, o R1 y R2 pueden formar opcionalmente un anillo cicloalquilo C3-7 no sustituido o sustituido; R3 es hidrógeno o alquilo C1-12; R5 se selecciona de hidrógeno, alquilo C1-12, CF3, cicloalquilo C3-7, arilo, o heterociclilo; B es un anillo heteroarilo de 5-miembros representado por una de las estructuras generales del grupo de fórmulas (3), donde los puntos 1 y 2 son puntos de fijación de B a fenilo y a Z respectivamente y R4 se selecciona de hidrógeno, alquilo C1-12 o arilo; o B es un anillo heteroarilo de 6-miembros que contiene 1 ó 2 N-átomos, donde el anillo heteroarilo de 6-miembros puede ser no sustituido o sustituido con uno o más grupos seleccionados de halógeno, hidroxi, alcoxi C1-12, ciano, nitro, alquilo C1-12, alquenilo C2-12, alquinilo C2-12, cicloalquilo C3-12, arilo, ariloxi, heterociclilo u O-heterociclilo; L se selecciona de *NHC(O)NH, *N(CH3)C(O)NH, *NHC(S)NH, *SO2NH, *CONH o *NH(C=NR6)NH, donde * indica el punto de fijación de L a A, y R6 se selecciona de hidrógeno, metilo, ciano o nitro; A se selecciona de alquilo C1-12, cicloalquilo C3-12, arilo o heterociclilo; en donde, el alquilo C1-12 se encuentra no sustituido o sustituido con uno o mas grupos seleccionados de halógeno, hidroxi, alcoxi C1-12, ciano, nitro, cicloalquilo C3-12, arilo, heterocíclico, C(O)Rp, C(O)ORp, NRpRq, C(O)NRpRq, SRp, S(O)Rp o SO2Rp; el cicloalquilo C3-12 se encuentra no sustituido o sustituido por uno o más grupos seleccionados de halógeno, hidroxi, alcoxi C1-12, ciano, nitro, arilo, heterociclilo, C(O)Rp, C(O)ORp, NRpRq, C(O)NRpRq, SRp, S(O)Rp o SO2Rp; el arilo se encuentra no sustituido o sustituido con uno o más grupos seleccionados de halógeno, hidroxi, alcoxi C1-12, ciano, nitro, alquilo C1-12, OCF3, CF3, alquenilo C2-12, alquinilo C2-12, cicloalquilo C3-12, arilo, ariloxi, heterociclilo, O-heterociclilo, C(O)Rp, C(O)ORp, NRpRq, C(O)NRpRq, SRp, S(O)Rp o SO2Rp; o el arilo puede fusionarse con un anillo cicloalquilo de 5 ó 6 miembros no sustituido o sustituido que contenga opcionalmente uno o más heteroátomos seleccionados de O, N o S; el heterociclilo está no sustituido o sustituido con uno o más grupos seleccionados de halógeno, hidroxi, alcoxi C1-12, ciano, nitro, alquilo C1-12, alquenilo C2-12, alquinilo C2-12, cicloalquilo C3-12, arilo, ariloxi, heterociclilo, O-heterociclilo, C(O)Rp, C(O)ORp, NRpRq, C(O)NRpRq, SRp, S(O)Rp o SO2Rp; Rp y Rq son seleccionados independientemente de hidrógeno, alquilo C1-12, arilo, aralquilo o heterociclilo, o Rp y Rq juntos con el N al cual están fijados opcionalmente forman un anillo de 3 a 7 miembros; con la condición de que A no es un grupo metilo.
ARP110103235 2010-09-03 2011-09-05 Compuestos heterociclicos como inhibidores de dgat1 AR084474A1 (es)

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