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AR116687A1 - Compuestos y composiciones para tratar condiciones asociadas con la actividad del receptor apj - Google Patents

Compuestos y composiciones para tratar condiciones asociadas con la actividad del receptor apj

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Publication number
AR116687A1
AR116687A1 ARP190102843A ARP190102843A AR116687A1 AR 116687 A1 AR116687 A1 AR 116687A1 AR P190102843 A ARP190102843 A AR P190102843A AR P190102843 A ARP190102843 A AR P190102843A AR 116687 A1 AR116687 A1 AR 116687A1
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AR
Argentina
Prior art keywords
optionally substituted
independently selected
group
ring atoms
disorders
Prior art date
Application number
ARP190102843A
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English (en)
Inventor
Zhe Nie
Sarah Boyce
Michael Hanson
Haifeng Tang
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Annapurna Bio Inc
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Publication date
Application filed by Annapurna Bio Inc filed Critical Annapurna Bio Inc
Publication of AR116687A1 publication Critical patent/AR116687A1/es

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    • C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
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Abstract

Esta descripción presenta entidades químicas (por ejemplo, un compuesto o una sal y/o hidrato y/o profármaco farmacéuticamente aceptable del compuesto) que modulan (por ejemplo, agonizan) el receptor de apelina (también denominado aquí receptor APJ; símbolo de gen “APLNR”). Esta descripción también presenta composiciones que contienen los mismos, así como otros métodos de uso y fabricación del mismo. Las entidades químicas son útiles, por ejemplo, para tratar a un sujeto (por ejemplo, un humano) que tiene una enfermedad, trastorno o condición en la que disminuye la actividad del receptor APJ (por ejemplo, señalización del receptor APJ reprimido o deteriorado; por ejemplo, señalización del receptor de apelina-APJ reprimido o deteriorado) o la sub-regulación de la apelina endógena contribuye a la patología y/o síntomas y/o progresión de la enfermedad, trastorno o condición. Los ejemplos no limitantes de tales enfermedades, trastornos o condiciones incluyen: (i) enfermedad cardiovascular; (ii) trastornos metabólicos; (iii) enfermedades, trastornos y condiciones asociadas con la patología vascular; y (iv) insuficiencia orgánica; (v) enfermedades, trastornos y condiciones asociadas con infecciones (por ejemplo, infecciones microbianas); y (vi) enfermedades, trastornos o condiciones que son secuelas o comórbidas con cualquiera de los anteriores o cualquiera de los aquí descritos. Los ejemplos no limitantes más particulares de tales enfermedades, trastornos o condiciones incluyen hipertensión pulmonar (por ejemplo, PAH); insuficiencia cardíaca; diabetes tipo II; insuficiencia renal; septicemia; e hipertensión sistémica. Reivindicación 1: Un compuesto de fórmula (1), o una sal farmacéuticamente aceptable del mismo; en donde: A¹ es CH o N; cada uno de X¹, X², X³ y X⁴ se selecciona independientemente del grupo que consiste en N y CR³; R¹ es: (i) -(Y¹)ₙ-Y², en donde: n es 0 ó 1; Y¹ es alquileno C₁₋₆, que está opcionalmente sustituido con 1 - 6 Rᵃ; y Y² es: (a) cicloalquilo C₃₋₁₀, que está opcionalmente sustituido con 1 - 4 Rᵇ, (b) arilo C₆₋₁₀, que está opcionalmente sustituido con 1 - 4 Rᶜ; (c) heteroarilo que incluye de 5 - 10 átomos en el anillo, en donde de 1 - 4 átomos en el anillo son heteroátomos, cada uno independientemente seleccionado del grupo que consiste de N, N(H), N(Rᵈ), O y S, y en donde uno o más de los átomos de carbono del anillo heteroarilo están opcionalmente sustituidos con 1 - 4 Rᶜ seleccionado independientemente, o (d) heterociclilo que incluye de 3 - 10 átomos en el anillo, en donde de 1 - 3 átomos en el anillo son heteroátomos, cada uno independientemente seleccionado del grupo que consiste en N, N(H), N(Rᵈ) y O, y en donde uno o más de los átomos de carbono del anillo heterociclilo están opcionalmente sustituidos con 1 - 4 Rᵇ seleccionados independientemente, o (ii) -Z¹-Z²-Z³, en donde: Z¹ es alquileno C₁₋₃, que está opcionalmente sustituido con 1 - 4 Rᵃ; Z² es -N(H)-, -N(Rᵈ)-, -O- o -S-; y Z³ es alquilo C₂₋₇, que está opcionalmente sustituido con 1 - 4 Rᵃ; o (iii) alquilo C₃₋₁₀, opcionalmente sustituido con 1 - 6 Rᵃ seleccionado independientemente; o (iv) -Z⁴-Z⁵-Z⁶-Y² en donde: Z⁴ es alquileno C₁₋₃, que está opcionalmente sustituido con 1 - 4 Rᵃ; Z⁵ es -N(H)-, -N(Rᵈ)-, -O- o -S-; Z⁶ es alquileno C₁₋₄, que está opcionalmente sustituido con 1 - 4 Rᵃ; y Y² es como se definió anteriormente; R² es: (i) arilo C₆₋₁₀, que está opcionalmente sustituido adicionalmente con 1 - 4 Rᶜ; (ii) heteroarilo que incluye de 5 - 10 átomos en el anillo, en donde de 1 - 4 átomos en el anillo son heteroátomos, cada uno independientemente seleccionado del grupo que consiste de N, N(H), N(Rᵈ), O y S, y en donde uno o más de los átomos de carbono del anillo heteroarilo están opcionalmente sustituidos con 1 - 4 Rᶜ seleccionados independientemente; (iii) cicloalquilo C₃₋₁₀, que está opcionalmente sustituido con 1 - 4 Rᵇ; (iv) heterociclilo que incluye de 3 - 10 átomos en el anillo, en donde de 1 - 3 átomos en el anillo son heteroátomos, cada uno independientemente seleccionado del grupo que consiste de N, N(H), N(Rᵈ) y O, y en donde uno o más de los átomos de carbono del anillo heterociclilo están opcionalmente sustituidos con 1 - 4 Rᵇ seleccionados independientemente; o (v) alquilo C₁₋₁₀, que está opcionalmente sustituido con 1 - 6 Rᵃ seleccionado independientemente; cada ocurrencia de R³ se selecciona independientemente del grupo que consiste de -L⁴-R⁴, H y, Rᶜ’; cada ocurrencia de L⁴ se selecciona independientemente del grupo que consiste de: (i) un enlace sencillo; (ii) N(H), N(Rᵈ), o N(R⁴); (iii) -N(H)S(O)₁₋₂- o -N(Rᵈ)S(O)₁₋₂-; (iv) -S(O)₁₋₂N(H)- o -S(O)₁₋₂N(Rᵈ)-; (v) -O-; (vi) -S(O)₀₋₂-; (vii) -C(O)NH- o -C(O)N(Rᵈ); (viii) -N(H)C(O)- o -N(Rᵈ)C(O)-; (ix) -C&
ARP190102843A 2018-10-05 2019-10-07 Compuestos y composiciones para tratar condiciones asociadas con la actividad del receptor apj AR116687A1 (es)

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