AR107934A1 - Sulfonilbencen-ureas asimétricas y usos médicos de las mismas como moduladoras de la actividad del receptor de ghrelina - Google Patents

Sulfonilbencen-ureas asimétricas y usos médicos de las mismas como moduladoras de la actividad del receptor de ghrelina

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Publication number
AR107934A1
AR107934A1 ARP170100694A ARP170100694A AR107934A1 AR 107934 A1 AR107934 A1 AR 107934A1 AR P170100694 A ARP170100694 A AR P170100694A AR P170100694 A ARP170100694 A AR P170100694A AR 107934 A1 AR107934 A1 AR 107934A1
Authority
AR
Argentina
Prior art keywords
alkyl
halo
optionally substituted
atoms
independently
Prior art date
Application number
ARP170100694A
Other languages
English (en)
Inventor
Claudio Pietra
Antoine Daina
Claudio Giuliano
Original Assignee
Helsinn Healthcare Sa
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Filing date
Publication date
Application filed by Helsinn Healthcare Sa filed Critical Helsinn Healthcare Sa
Publication of AR107934A1 publication Critical patent/AR107934A1/es

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    • C07D403/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
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Abstract

Se describen sulfonilbencen-ureas asimétricas. Los compuestos son activos sobre los receptores de ghrelina, en particular tienen actividad agonista inversa; son útiles para prevenir y/o tratar enfermedades mediadas patofisiológicamente por el receptor de ghrelina, como por ejemplo, obesidad, diabetes y abuso de sustancias. También se describen composiciones farmacéuticas que comprenden un compuesto como se describe en la presente y un portador o vehículo farmacéuticamente aceptable. Reivindicación 1: Un compuesto de fórmula (1), o una sal farmacéuticamente aceptable del mismo, en donde: una línea discontinua indica un enlace opcional; W es C, N, u O; X es un enlace, CO, o CR⁷R⁸; k es 0 - 2; R es alquilo C₁₋₆ o Cy¹ en donde dicho alquilo C₁₋₆ o Cy¹ está opcionalmente sustituido con 1 - 3 sustituyentes seleccionados de halo, heteroarilo, alcoxi C₁₋₆, alquilo C₁₋₆, heterocicloalquilo, CO₂(alquilo C₁₋₆), y CO(alquilo C₁₋₆); R¹ y R² son cada uno, independientemente, H, alquilo C₁₋₃, metoxi, halo, o OH; o R¹ y R² tomados junto con los átomos a los cuales ellos están unidos forman un anillo de 5 - 6 miembros; o R¹ y X tomados junto con los átomos a los cuales ellos están unidos forman un anillo de 5 - 6 miembros; o R¹, X y R tomados junto con los átomos a los cuales ellos están unidos forman una estructura bicíclica; R³ es H, alquilo C₁₋₃, metoxi, halo, o -OH, -COOR¹², -CR¹³R¹⁴OH, -CONHR¹⁵, cicloalquilo, heteroarilo; R⁴ es un enlace, NR⁶ o CR⁹R¹⁰; o R³ y R⁴ tomados junto con los átomos a los cuales ellos están unidos forman un anillo de 3 - 6-miembros; R⁵ es Cy², CO(alquilo C₁₋₆,), o alquilo C₁₋₆, en donde dicho Cy², CO(alquilo C₁₋₆), o alquilo C₁₋₆, está opcionalmente sustituido con 1 - 3 sustituyentes seleccionados de halo, alquilamina C₁₋₆, COR¹¹, SO₂R¹¹, heterocicloalquilo, CO₂R¹¹, hidroxialquilo C₁₋₆, heteroarilo, CH₂CO₂R¹¹, alcoxi C₁₋₆, OH, CN, R¹¹, CH₂OSO₃H, bencilo, CH₂SO₃H, CH₂CN, y NHCH₂-cicloalquilo; R⁶ es un enlace, H, o CH₃; R⁷ y R⁸ son cada uno, independientemente, H, alquilo C₁₋₃, o CONH₂, en donde dicho alquilo C₁₋₃ está opcionalmente sustituido con halo; R⁹ y R¹⁰ son cada uno, independientemente, H o alquilo C₁₋₃, en donde dicho alquilo C₁₋₃ está opcionalmente sustituido con halo; R¹¹ es H, NH₂, o alquilo C₁₋₆ opcionalmente sustituido; y R¹², R¹³, R¹⁴ y R¹⁵ son cada uno independientemente H o alquilo C₁₋₃.
ARP170100694A 2016-03-22 2017-03-21 Sulfonilbencen-ureas asimétricas y usos médicos de las mismas como moduladoras de la actividad del receptor de ghrelina AR107934A1 (es)

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EP3390355B1 (en) 2022-12-28
EA201891691A1 (ru) 2019-04-30
ES2940659T3 (es) 2023-05-10
MX2018009128A (es) 2018-11-09
EP3390355A1 (en) 2018-10-24
RS64027B1 (sr) 2023-03-31
AU2017239419A1 (en) 2018-08-09

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