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AR102851A1 - Compuestos de n-((het)arilmetil)-heteroaril-carboxamidas como inhibidores de calicreína plasmática - Google Patents

Compuestos de n-((het)arilmetil)-heteroaril-carboxamidas como inhibidores de calicreína plasmática

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Publication number
AR102851A1
AR102851A1 ARP150103901A ARP150103901A AR102851A1 AR 102851 A1 AR102851 A1 AR 102851A1 AR P150103901 A ARP150103901 A AR P150103901A AR P150103901 A ARP150103901 A AR P150103901A AR 102851 A1 AR102851 A1 AR 102851A1
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AR
Argentina
Prior art keywords
independently selected
alkoxy
alkyl
alkylb
optionally substituted
Prior art date
Application number
ARP150103901A
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English (en)
Inventor
Teanby Hodgson Simon
Joy Edwards Hannah
Louise Davie Rebecca
Michael Evans David
Original Assignee
Kalvista Pharmaceuticals Ltd
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Publication date
Application filed by Kalvista Pharmaceuticals Ltd filed Critical Kalvista Pharmaceuticals Ltd
Publication of AR102851A1 publication Critical patent/AR102851A1/es

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Abstract

Composiciones que comprenden dichos compuestos; el uso de estos compuestos en una terapia (por ejemplo en el tratamiento o la prevención de una enfermedad o condición en la cual está implicada la actividad de la calicreína plasmática); y métodos de tratamiento de pacientes con dichos compuestos. Reivindicación 1: Un compuesto caracterizado porque de fórmula (1), donde B es (CH₂)ₙ-fenilo, donde n es 0 ó 1 y fenilo está sustituido con 1 a 3 sustituyentes seleccionados entre alquilo, alcoxi, OH, halo, CN, COOR⁸, CONR⁸R⁹, OCF₃, CF₃ y NR⁸R⁹; o B es anillo heterocíclico de 5 ó 6 miembros que contiene uno o dos heteroátomos seleccionados entre N, O y S; dicho anillo heterocíclico puede ser aromático o no aromático y está sustituido con 1 a 3 sustituyentes seleccionados entre alquilo, alcoxi, OH, oxo, halo, CN, COOR⁸, CONR⁸R⁹, OCF₃, CF₃ y NR⁸R⁹; D se selecciona entre CH₂, CH-alquiloᵇ, C(alquilᵇ)₂ y CO; y U se selecciona entre CH₂, CH-alquiloᵇ y C(alquilᵇ)₂; y E se selecciona entre NH, N-alquiloᵇ, CH₂ y O; o U es CH; y E es N; donde U, D y E juntos forman parte de un azacarbociclo; W, X, Y y Z se seleccionan en forma independiente entre C, N, O y S, de manera que el anillo que contiene W, X, Y y Z es un heterociclo aromático de cinco miembros; R⁵, R⁶ y R⁷ en forma independiente están ausentes o se seleccionan en forma independiente entre H, alquilo, alcoxi, halo, OH, arilo, heteroarilo, -NR⁸R⁹, CN, COOR⁸, CONR⁸R⁹, -NR⁸COR⁹, CF₃, y R¹⁶; A se selecciona entre arilo y heteroarilo; R⁸ y R⁹ se seleccionan en forma independiente entre H y alquilo; R¹⁶ es un sistema de anillos monocíclico de 3, 4, 5 ó 6 miembros que contiene carbono que puede ser aromático, saturado o insaturado no aromático y que opcionalmente puede contener 1, 2, 3 ó 4 heteroátomos seleccionados entre N, O y S, donde el sistema de anillos R¹⁶ a su vez está opcionalmente sustituido con sustituyentes seleccionados entre alquilo y oxo; alquilo es un hidrocarburo saturado lineal que tiene hasta 10 átomos de carbono (C₁₋₁₀) o un hidrocarburo saturado ramificado de entre 3 y 10 átomos de carbono (C₃₋₁₀); alquilo puede estar opcionalmente sustituido con 1 ó 2 sustituyentes seleccionados en forma independiente entre C₁₋₆ alcoxi, OH, CN, CF₃, COOR¹⁰, CONR¹⁰R¹¹, fluoro y NR¹⁰R¹¹; alquiloᵇ es un hidrocarburo saturado lineal que tiene hasta 6 átomos de carbono (C₁₋₆) o un hidrocarburo saturado ramificado de entre 3 y 6 átomos de carbono (C₃₋₆); alquiloᵇ puede estar opcionalmente sustituido con 1 ó 2 sustituyentes seleccionados en forma independiente entre C₁₋₆ alcoxi, OH, CN, CF₃ y fluoro; alcoxi es un hidrocarburo lineal unido por O de entre 1 y 6 átomos de carbono (C₁₋₆) o un hidrocarburo ramificado unido por O de entre 3 y 6 átomos de carbono (C₃₋₆); alcoxi puede estar opcionalmente sustituido con 1 ó 2 sustituyentes seleccionados en forma independiente entre OH, CN, CF₃, COOR¹⁰, CONR¹⁰R¹¹, fluoro y NR¹⁰R¹¹; azacarbociclo es un anillo monocíclico de 5 ó 6 miembros que contiene carbono, que comprende uno o dos átomos de nitrógeno en el anillo, y que puede estar opcionalmente sustituido con oxo; arilo es fenilo, bifenilo o naftilo; arilo puede estar opcionalmente sustituido con 1, 2 ó 3 sustituyentes seleccionados en forma independiente entre alquilo, alcoxi, metilendioxi, etilendioxi, OH, OCF₃, halo, CN, heteroarilo, -(CH₂)₀₋₃-O-heteroarilo, ariloᵇ, -O-ariloᵇ, -(CH₂)₁₋₃-ariloᵇ, -(CH₂)₁₋₃-heteroarilo, -COOR¹⁰, -CONR¹⁰R¹¹, -(CH₂)₀₋₃-NR¹⁰R¹¹ y CF₃; ariloᵇ es fenilo, bifenilo o naftilo, que puede estar opcionalmente sustituido con 1, 2 ó 3 sustituyentes seleccionados en forma independiente entre alquilo, alcoxi, OH, halo, CN, -COOR¹⁰, -CONR¹⁰R¹¹, CF₃ y NR¹⁰R¹¹; heteroarilo es un anillo aromático monocíclico o bicíclico de 5, 6, 9 ó 10 miembros, que contiene, donde sea posible, 1, 2 ó 3 miembros del anillo seleccionados en forma independiente entre N, NR⁸, S y O; heteroarilo puede estar opcionalmente sustituido con 1, 2 ó 3 sustituyentes seleccionados en forma independiente entre alquilo, alcoxi, OH, OCF₃, halo, CN, arilo, -(CH₂)₁₋₃-arilo, heteroariloᵇ, -COOR¹⁰, -CONR¹⁰R¹¹, CF₃ y -(CH₂)₀₋₃-NR¹⁰R¹¹; heteroariloᵇ es un anillo aromático monocíclico o bicíclico de 5, 6, 9 ó 10 miembros, que contiene, donde sea posible, 1, 2 ó 3 miembros del anillo seleccionados en forma independiente entre N, NR⁸, S y O; donde heteroariloᵇ puede estar opcionalmente sustituido con 1, 2 ó 3 sustituyentes seleccionados en forma independiente entre alquilo, alcoxi, OH, halo, CN, arilo, -(CH₂)₁₋₃-arilo, -COOR¹⁰, -CONR¹⁰R¹¹, CF₃ y NR¹⁰R¹¹; R¹⁰ y R¹¹ se seleccionan en forma independiente entre H, alquiloᵇ, CONR¹⁴R¹⁵, COR¹⁷, ariloᵇ y heteroarilᵇ; o R¹⁰ y R¹¹ junto con el átomo de nitrógeno al cual están unidos forman un anillo heterocíclico de 4, 5, 6 ó 7 miembros que contiene carbono, que contiene opcionalmente un heteroátomo adicional seleccionado entre N, S y O, que puede ser saturado o insaturado con 1 ó 2 enlaces dobles y que puede estar opcionalmente mono- o di-sustituido con sustituyentes seleccionados entre oxo, alquiloᵇ, alcoxi, OH, halo y CF₃; R¹⁴, R¹⁵ y R¹⁷ se seleccionan en forma independiente entre H o alquiloᵇ; y tautómeros, isómeros, estereoisómeros (incluyendo enantiómeros, diasteroisómeros y mezclas racémicas y escalémicas de los mismos), sales farmacéuticamente aceptables y solvatos del mismo; con la condición de que el compuesto de fórmula (1) no es un compuesto de fórmula (2).
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