AR082391A1 - Inhibidores biciclicos de acetil-coa y usos de los mismos - Google Patents

Inhibidores biciclicos de acetil-coa y usos de los mismos

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Publication number
AR082391A1
AR082391A1 ARP110102709A ARP110102709A AR082391A1 AR 082391 A1 AR082391 A1 AR 082391A1 AR P110102709 A ARP110102709 A AR P110102709A AR P110102709 A ARP110102709 A AR P110102709A AR 082391 A1 AR082391 A1 AR 082391A1
Authority
AR
Argentina
Prior art keywords
alkyl
carbon atoms
amino
alkoxy
independently
Prior art date
Application number
ARP110102709A
Other languages
English (en)
Original Assignee
Novartis Ag
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 Novartis Ag filed Critical Novartis Ag
Publication of AR082391A1 publication Critical patent/AR082391A1/es

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    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/54—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one sulfur as the ring hetero atoms, e.g. sulthiame
    • A61K31/542—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one sulfur as the ring hetero atoms, e.g. sulthiame ortho- or peri-condensed with heterocyclic ring systems
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    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/40—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
    • A61K31/403—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil condensed with carbocyclic rings, e.g. carbazole
    • A61K31/404—Indoles, e.g. pindolol
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    • 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
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Abstract

La presente proporciona un método para la elaboración de los compuestos de la fórmula (1), sus usos terapéuticos, combinaciones con otros de los agentes farmacológicamente activos, y composiciones farmacéuticas.Reivindicación 1: Un compuesto de la fórmula (1), o una sal farmacéuticamente aceptable del mismo, en donde el anillo A es un sistema de anillo bicíclico seleccionado a partir del grupo de fórmulas (2) en donde la línea ondulada indica que el punto de unión de L1 está sobre el anillo A’; y en donde R1 puede reemplazar a un átomo de hidrógeno de cualquier enlace de CH en el anillo A; X1, por cada presentación, es independientemente CH o N; X2 es NR19, O, o S; X3, por cada presentación, es independientemente NR9, CH2, O, o S; r es 1 ó 2; el anillo B es ciclohexilo o fenilo; en el entendido de que, cuando el anillo B es fenilo, el anillo A es de fórmula (3) en donde R1a es hidrógeno, fenilo, fenil-amino, o un heteroarilo de 5 a 10 miembros, en donde R1a puede estar opcionalmente sustituido sobre uno o más átomos de carbono con uno o más R13 independientemente seleccionados; y en donde, cuando R1a es un heteroarilo que comprende uno o más -NH-, el hidrógeno de cada grupo -NH- puede ser opcionalmente reemplazado con R22; Q se selecciona a partir del grupo de fórmulas (4) en donde la línea ondulada indica el punto de unión con el anillo B; X4 es -NR4- u -O-; q y n son cada uno independientemente 0, 1, 2, 3 ó 4; L1 es -NHSO2-, -SO2NH-, -NHSO2NH- o -NHC(O)NH-; R1 puede reemplazar a un átomo de hidrógeno de cualquier enlace de CH en el anillo A y, por cada presentación, es independientemente deuterio, hidroxilo, nitro, halógeno, ciano, carboxilo, formilo, alquilo C1-7, carbociclilo C3-8, alquenilo C2-7, alquinilo C2-7, alcoxilo C1-7, tioalquilo C1-7, cicloalcoxilo C3-8, arilo C6-10, arilo C6-10-alquilo C1-4, ariloxilo C6-10, amino, N-alquilo C1-7-amino, N,N-di-(alquilo C1-7)-amino, N-arilo C6-10-amino, heterociclilo de 3 a 10 miembros, N-(heterociclilo de 3 a 10 miembros)-amino, (heterociclilo de 3 a 10 miembros)-oxilo, heteroarilo de 5 a 10 miembros, (heteroarilo de 5 a 10 miembros)-alquilo C1-4, N-(heteroarilo de 5 a 10 miembros)-amino, (heteroarilo de 5 a 10 miembros)-oxilo, alcanoílo C1-7, alcoxilo C1-7-carbonilo, alcanoiloxilo C1-7, alquilo C1-7-amido, arilo C6-10-amido, (heterociclilo de 3 a 10 miembros)-amido, carbamoilo, N-alquilo C1-7-carbamoilo, N,N-di-(alquilo C1-7)-carbamoilo, alcoxilo C1-7-amido, alquilo C1-7-ureido, y arilo C6-10-ureido, en donde R1 está opcionalmente sustituido sobre uno o más átomos de carbono con uno o más R13 independientemente seleccionados; y en donde, cuando R1 comprende un heterociclilo o un heteroarilo que comprende uno o más -NH-, el hidrógeno de cada grupo -NH- puede ser independientemente reemplazado opcionalmente con R22; o dos R1 sobre el mismo átomo de carbono, pueden formar juntos un oxo; o dos R1 sobre el mismo átomo de carbono, junto con el átomo de carbono con el que están unidos, forman un espiro-carbociclilo de 3 a 8 átomos de carbono; o dos R1 sobre átomos de carbono adyacentes, junto con los átomos de carbono con los que están unidos, pueden formar un carbociclilo de 3 a 8 átomos de carbono fusionado o fenilo, el cual puede estar opcionalmente sustituido con uno o más R13; y R2, por cada presentación, se selecciona independientemente a partir del grupo que consiste en hidroxilo, ciano, alquilo C1-7, alcoxilo C1-7, alquenilo C2-7, amino, alquilo C1-7-amino, di-(alquilo C1-7)-amino, alquilo C1-7-amido, alcoxilo C1-7-amido; en donde R2, por cada presentación, puede ser independientemente sustituido opcionalmente con uno o más halógenos; o dos o más grupos R2 sobre átomos de carbono no adyacentes forman juntos un puente de alquileno C1-4; o dos o más grupos R2 sobre átomos de carbono adyacentes, pueden formar un carbociclilo C3-8 fusionado; R3 se selecciona a partir del grupo que consiste en un alquilo C1-7, carbociclilo C3-8, carbociclilo C3-8-alquilo C1-4, arilo C6-10, arilo C6-10-alquilo C1-4, un heteroarilo de 5 a 10 miembros, un (heteroarilo de 5 a 10 miembros)-alquilo C1-4, un heterociclilo de 3 a 10 miembros, y un (heterociclilo de 3 a 10 miembros)-alquilo C1-4, en donde R3 está opcionalmente sustituido sobre uno o más átomos de carbono con uno o más R14; y en donde, cuando R3 comprende un heteroarilo o heterociclilo, el cual comprende uno o más -NH-, el hidrógeno de cada grupo -NH- puede ser independientemente reemplazado opcionalmente con un alquilo C1-7; R4 es hidrógeno, alquilo C1-7, o alcoxilo C1-4-alquilo C1-4; o R3 y R4, junto con el átomo de nitrógeno con el que están unidos, forman un heterociclilo de 3 a 7 miembros, en donde el heterociclilo puede estar opcionalmente sustituido sobre uno o más átomos de carbono con uno o más R15; y en donde, cuando el heterociclilo comprende uno o más -NH-, el hidrógeno de cada grupo -NH- puede ser independientemente reemplazado opcionalmente con R16; R13, por cada presentación, es independientemente deuterio, nitro, halógeno, ciano, hidroxilo, carboxilo, alquilo C1-7, cicloalquilo C3-8, alcoxilo C1-7, arilo C6-10, ariloxilo C6-10, heterociclilo de 3 a 10 miembros, heteroarilo de 5 a 10 miembros, amino, alquilo C1-7-amino, di-(alquilo C1-7)-amino, alcanoílo C1-7, alcoxilo C1-7-carbonilo, alcanoiloxilo C1-7, alquilo C1-7-amido, alcoxilo C1-7-amido, carbamoilo, N-alquilo C1-7-carbamoilo, N,N-di-(alquilo C1-7)-carbamoilo, alquilo C1-7-sulfonilo, alquilo C1-7-sulfoniloxilo, alquilo C1-7-sulfonamido, sulfamoilo, N-alquilo C1-7-sulfamoilo, o N,N-di-(alquilo C1-7)sulfamoilo, en donde R13 está opcionalmente sustituido sobre uno o más átomos de carbono con uno o más R17 independientemente seleccionados; y en donde, cuando R13 es un heterociclilo o un heteroarilo que comprende uno o más -NH-, el hidrógeno de cada grupo -NH- puede ser independientemente reemplazado opcionalmente con R20; o dos R13 sobre el mismo átomo de carbono, pueden formar juntos un oxo o un espiro-carbociclilo C3-8; o dos R13 sobre átomos de carbono adyacentes, junto con los átomos de carbono con los que están unidos, pueden formar un heterociclilo de 3 a 7 miembros, el cual puede estar opcionalmente sustituido sobre uno o más átomos de carbono con uno o más R17, y si el heterociclilo comprende uno o más grupos -NH-, el hidrógeno de cada grupo -NH- puede ser independientemente reemplazado opcionalmente con R20; R14, por cada presentación, es independientemente halógeno, hidroxilo, carboxilo, alcoxilo C1-7-carbonilo, alquilo C1-7, alcoxilo C1-7, cicloalquilo C3-8, arilo C6-10, o heteroarilo de 5 a 10 miembros, en donde R14 puede estar opcionalmente sustituido sobre uno o más átomos de carbono con uno o más R24 independientemente seleccionados; o dos R14 sobre el mismo átomo de carbono, pueden formar juntos un oxo, un espiro-carbociclilo C3-8, o un espiro-heterociclilo de 3 a 7 miembros; o dos R14 sobre átomos de carbono adyacentes, junto con los átomos de carbono con los que están unidos, pueden formar un fenilo, el cual puede estar opcionalmente sustituido sobre uno o más átomos de carbono con uno o más R24; R15, por cada presentación, se selecciona independientemente a partir del grupo que consiste en hidroxilo, carboxilo, alquilo C1-7, alcoxilo C1-7, carbociclilo C3-8, fenilo, y alcoxilo C1-7-carbonilo; en donde R15 puede estar opcionalmente sustituido sobre uno o más átomos de carbono con uno o más sustituyentes independientemente seleccionados a partir de halógeno, hidroxilo, alcoxilo C1-4; o dos R15 sobre el mismo átomo de carbono forman juntos un oxo, o junto con el átomo de carbono con el que están unidos, forman un cicloalquilo C2-8, o un heterociclilo de 3 a 10 miembros; o dos R15 sobre átomos de carbono adyacentes, junto con los átomos de carbono con los que están unidos, pueden formar un fenilo fusionado; R16, por cada presentación, se selecciona independientemente a partir del grupo que consiste en alquilo C1-7, carbociclilo C3-8, alcanoílo C1-7, alcoxilo C1-7-carbonilo, o heteroarilo de 5 a 10 miembros; R17, por cada presentación, se selecciona independientemente a partir de ciano, halógeno, hidroxilo, carboxilo, alquilo C1-7, alcoxilo C1-7, amino, alquilo C1-7-amino, di(alquilo C1-7)-amino, arilo C6-10-amino, arilo C6-10-alquilo C1-4-amino, alcoxilo C1-7-carbonilo, alcanoiloxilo C1-7, heterociclilo de 3 a 10 miembros, en donde R17 puede estar opcionalmente sustituido sobre uno o más átomos de carbono con uno o más de los siguientes independientemente seleccionados: halógeno, amino, alquilo C1-7, alcoxilo C1-7, halo-alquilo C1-7, carboxilo, o alcoxilo C1-7-carbonilo; y en donde, cuando R17 es un heterociclilo, el cual comprende uno o más -NH-, el hidrógeno de cada grupo -NH- puede ser independientemente reemplazado opcionalmente con R23; o dos R17 sobre el mismo átomo de carbono, pueden formar juntos un oxo; R18 es un alquilo C1-7, cicloalquilo C3-8, fenilo o un alcoxilo C1-7-alquilo C1-7; R19, por cada presentación, es independientemente hidrógeno, alquilo C1-7, alcanoílo C1-7, tri-(alquilo C1-7)-sililo, cicloalquilo C3-8, alcoxilo C1-7-carbonilo, cicloalcoxilo C3-8-carbonilo, carbamoilo, N-alquilo C1-7-carbamoilo, N,N-di-(alquilo C1-7)-carbamoilo, o arilo C6-10-alquilo C1-4; en donde R19 está opcionalmente sustituido sobre uno o más átomos de carbono con uno o más R21; R20, R21, R22, y R23, por cada presentación, son independientemente deuterio, halógeno, carboxilo, alquilo C1-7, alcoxilo C1-7, ariloxilo C6-10, arilo C6-10-alcoxilo C1-4, o alcoxilo C1-7-carbonilo; y R24, por cada presentación, es independientemente hidroxilo, halógeno, carboxilo, alquilo C1-7, halo-alquilo C1-7, alcoxilo C1-7, amino, N-alquilo C1-7-amino, N,N-di(alquilo C1-7)-amino, alcoxilo C1-7-carbonilo, alcanoiloxilo C1-7, fosfono-oxilo, alcoxilo C1-7-(hidroxi)-fosforiloxilo o di-(alcoxilo C1-7)-fosforiloxilo; en donde R24 puede estar opcionalmente sustituido sobre uno o más átomos de carbono con un grupo independientemente seleccionado a partir de amino, N-al
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US20140171363A1 (en) 2014-06-19
ES2641833T3 (es) 2017-11-14
EP2598486A1 (en) 2013-06-05
EP2598486B1 (en) 2017-06-28
US20120028969A1 (en) 2012-02-02
JP2013533279A (ja) 2013-08-22
JP5998133B2 (ja) 2016-09-28
CN103339111A (zh) 2013-10-02
WO2012013716A1 (en) 2012-02-02
US9789118B2 (en) 2017-10-17
US8697739B2 (en) 2014-04-15
TW201206907A (en) 2012-02-16
UY33536A (es) 2012-02-29

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