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AR056893A1 - Compuestos heterociclicos fusionados y no fusionados, antagonistas de receptores mineralocorticoides - Google Patents

Compuestos heterociclicos fusionados y no fusionados, antagonistas de receptores mineralocorticoides

Info

Publication number
AR056893A1
AR056893A1 ARP060105810A ARP060105810A AR056893A1 AR 056893 A1 AR056893 A1 AR 056893A1 AR P060105810 A ARP060105810 A AR P060105810A AR P060105810 A ARP060105810 A AR P060105810A AR 056893 A1 AR056893 A1 AR 056893A1
Authority
AR
Argentina
Prior art keywords
group
optionally substituted
formula
represented
optionally
Prior art date
Application number
ARP060105810A
Other languages
English (en)
Inventor
T Ohra
T P Tang
S Fukumoto
N Ohyabu
C Gauthier
N Matsunaga
L A Demeese
C S Siedem
T Hasui
T Motoyaji
Original Assignee
Takeda Pharmaceutical
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 Takeda Pharmaceutical filed Critical Takeda Pharmaceutical
Publication of AR056893A1 publication Critical patent/AR056893A1/es

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—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
    • 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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    • A61P1/04—Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
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Abstract

Composiciones farmacéuticas que los contienen y usos para la profilaxis o tratamiento de hipertension, falla cardiaca y otros. Reivindicacion 1: Un compuesto caracterizado por que posee la formula (1), en donde A es un grupo representado por la formula -X1------X2------X3-, en donde, X1 y X2 son iguales o diferentes y cada uno es un enlace químico, CH2, CH, O, NH, N, S, SO o SO2, X3 es CH2, CH, O, NH, N, S, SO o SO2; y la línea punteada representa un enlace simple o un enlace doble; con la condicion que cuando entre X1 y X2 hay un enlace doble, entonces el enlace entre X2 y X3 es un enlace simple; R y R' son iguales o diferentes y cada uno es un grupo hidrocarburo alifático opcionalmente sustituido, un grupo hidroxilo opcionalmente sustituido, un grupo amino opcionalmente sustituido, un grupo carboxilo opcionalmente esterificado, un grupo carbamoilo opcionalmente sustituido, un átomo halogeno, un grupo nitro, un grupo ciano, un grupo mercapto opcionalmente sustituido o un grupo acilo, o dos R opcionalmente forman un anillo espiro junto con un átomo de carbono al cual están unidos; k es un entero de valor 0 a 4; l es un entero de valor 0 a 3; Xa es CH o N; Xb es CH o N; Xc es CH o N; el círculo notado con "Het" en la formula (1) es un grupo heterocíclico representado por las formulas (2) a (14); en donde en la formula (2), la parte circular constituye el anillo fusionado en el grupo heterocíclico, es un anillo de 5 a 7 miembros que contiene opcionalmente, como miembro constitutivo del anillo, uno o más miembros seleccionados de O, N, S, SO y SO2; R1 y R2 son iguales o diferentes y cada uno es un átomo de hidrogeno, un grupo hidrocarburo de cadena alifática opcionalmente sustituido, un grupo hidroxilo opcionalmente sustituido, un grupo amino opcionalmente sustituido, un grupo carboxilo opcionalmente esterificado, un grupo carbamoilo opcionalmente sustituido, un átomo halogeno, un grupo nitro, un grupo ciano, un grupo mercapto opcionalmente sustituido, un grupo acilo o un grupo cíclico opcionalmente sustituido; R3 y R3' son iguales o diferentes y cada uno es un grupo hidrocarburo de cadena alifática opcionalmente sustituido, un grupo hidroxilo opcionalmente sustituido, un grupo amino opcionalmente sustituido, un grupo carboxilo opcionalmente esterificado, un grupo carbamoilo opcionalmente sustituido, un átomo halogeno, un grupo nitro, un grupo ciano, un grupo oxo, que un imino opcionalmente sustituidos se agrupan, un grupo mercapto opcionalmente sustituido, un grupo acilo o un grupo cíclico opcionalmente sustituido, o dos R3 forman opcionalmente, junto con dos átomos adyacentes a los cuales están unidos, un anillo de 3 a 7 miembros que contiene opcionalmente, como miembro constitutivo del anillo, uno o más miembros seleccionados de O, N, S, SO y SO2; R4 y R5 son iguales o diferentes y cada uno es un átomo de hidrogeno, un grupo hidrocarburo de cadena alifática opcionalmente sustituido, un grupo hidroxilo opcionalmente sustituido, un grupo amino opcionalmente sustituido, un grupo carboxilo opcionalmente esterificado, un grupo carbamoilo opcionalmente sustituido, un átomo halogeno, un grupo nitro, un grupo ciano, un grupo mercapto opcionalmente sustituido, un grupo acilo o un grupo cíclico opcionalmente sustituido, o R4 y R5 en combinacion forman opcionalmente un grupo oxo; R6 y R7 son iguales o diferentes y cada uno es un átomo de hidrogeno, un grupo hidrocarburo de cadena alifática opcionalmente sustituido, un grupo hidroxilo opcionalmente sustituido, un grupo amino opcionalmente sustituido, un grupo carboxilo opcionalmente esterificado, un grupo carbamoilo opcionalmente sustituido, un átomo halogeno, un grupo nitro, un grupo ciano, un grupo mercapto opcionalmente sustituido, un grupo acilo o un grupo cíclico opcionalmente sustituido, o R6 y R7 en combinacion opcionalmente forman un grupo oxo; con la condicion que por lo menos uno de un par de R4 y R5 y un par de R6 y R7 debe formar un grupo oxo; m y n son iguales o diferentes y cada uno es un entero de valor 0 a 4; X4 es CH o N; X5 y X6 son iguales o diferentes y cada uno es CH, C o N; X5' y X6' son iguales o diferentes y cada uno es CH2, CH, NH, N, O, S, SO o SO2; X7 es CH2, CH, NH, N, O, S, SO o SO2; X8 es CH o N; X9 es CH2, CH, NH, N, O, S, SO o SO2; X10 es CH2, CH, NH, N, O, S, SO o SO2; X11 es NH, O, S, SO o SO2; X12 es O o S; y la línea punteada es un enlace simple o un enlace doble; con la condicion que, cuando entre X5 y X6 hay un doble enlace, la union entre X6 y X7 debe ser un enlace simple (formula (2)); y cuando entre X5' y X6' hay un enlace doble, la union entre X6' y X7 debe ser un enlace simple (formula (3)); con la condicion que a) cuando el grupo "Het" de la formula (1) es un grupo heterocíclico representado por la formula (3), entonces por lo menos uno de R1 y R2 debe ser un grupo arilo opcionalmente sustituido o un grupo heteroarilo opcionalmente sustituido; b) cuando el grupo "Het" de la formula (1) es un grupo heterocíclico representado por la formula (4) u (8), entonces el átomo de carbono al cual el grupo representado por la formula (15), está enlazado y el átomo de carbono al cual R1 está enlazado deben ser adyacentes entre sí, y R1 debe ser un grupo arilo opcionalmente sustituido o un grupo heteroarilo opcionalmente sustituido; c) cuando el grupo representado por la formula -X1------X2------X3-, es -CH2-O- y el grupo "Het" es un grupo heterocíclico representado por la formula (16), entonces R1 no debe ser fenilo, 4-metoxifenilo, 3,4-dimetoxifenilo y 4-clorofenilo; d) cuando el grupo representado por la formula -X1------X2------X3-, es -CH2-O- y el grupo "Het" es un grupo heterocíclico representado por la formula (10), entonces R1 no debe ser un 2-piridilo opcionalmente sustituido; e) cuando el grupo representado por la formula -X1------X2------X3- es -CH2-O-, y el grupo "Het" es un grupo heterocíclico representado por la formula (10), en donde R1 es un fenilo opcionalmente sustituido, entonces el grupo -NH- en el anillo pirazol tal como fue ilustrado anteriormente debe ser sustituido por R3; f) cuando el grupo representado por la formula -X1------X2------X3- es -O-, -CH2-O- , -CH2-S- o -CH=CH-, y el grupo "Het" es un grupo heterocíclico representado por la formula (4), entonces R1 no debe ser un átomo de halogeno y trifluorometilo; g) cuando el grupo representado por la formula -X1------X2------X3- es -NH- o -CH2-NH-, y el grupo "Het" es un grupo heterocíclico representado por la formula (11), entonces R1 no debe ser un grupo alquilo; h) cuando el grupo representado por la formula -X1------X2------X3- es -CH2-O-, y el grupo "Het" es un grupo heterocíclico representado por la formula (12), entonces R1 debe ser un grupo arilo opcionalmente sustituido o un grupo heteroarilo opcionalmente sustituido; i) cuando el grupo representado por la formula -X1------X2------X3-, es -S- o -CH2-O-, y el grupo "Het" es un grupo heterocíclico representado por la formula (14), entonces R1 no debe ser un átomo halogeno; y j) cuando el grupo "Het" está representado por la formula (5), entonces por lo menos uno de R1 y R2 debe ser un grupo arilo opcionalmente sustituido o un grupo heteroarilo opcionalmente sustituido, o una sal del mismo.
ARP060105810A 2005-12-28 2006-12-27 Compuestos heterociclicos fusionados y no fusionados, antagonistas de receptores mineralocorticoides AR056893A1 (es)

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