AR123933A1 - ISOXAZOLE DERIVATIVES AS MODULATORS OF THE SEROTONIN 5-HT₂A RECEPTOR USEFUL FOR THE TREATMENT OF DISORDERS RELATED THERETO - Google Patents

ISOXAZOLE DERIVATIVES AS MODULATORS OF THE SEROTONIN 5-HT₂A RECEPTOR USEFUL FOR THE TREATMENT OF DISORDERS RELATED THERETO

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AR123933A1
AR123933A1 ARP210102981A ARP210102981A AR123933A1 AR 123933 A1 AR123933 A1 AR 123933A1 AR P210102981 A ARP210102981 A AR P210102981A AR P210102981 A ARP210102981 A AR P210102981A AR 123933 A1 AR123933 A1 AR 123933A1
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Argentina
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alkylene
alkyl
cycloalkyl
phenyl
independently selected
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ARP210102981A
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Spanish (es)
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Arena Pharm Inc
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Publication of AR123933A1 publication Critical patent/AR123933A1/en

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  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)

Abstract

Se proporciona un compuesto de fórmula (1) o una sal farmacéuticamente aceptable de este, que es un modulador de 5-HT₂A y puede usarse en el tratamiento de enfermedades y trastornos asociados con la expresión y/o actividad del receptor de serotonina 5-HT₂A. Por lo tanto, también se proporcionan métodos de tratamiento de enfermedades y trastornos relacionados con 5HT₂A. Reivindicación 1: Un compuesto de fórmula (1) o una sal farmacéuticamente aceptable de este, en donde: R¹ se selecciona de alquilo C₁₋₆, cicloalquilo C₃₋₆, fenilo, heteroarilo de 5 - 10 miembros, heterocicloalquilo de 5 - 9 miembros, (alquilen C₁₋₃)-(cicloalquilo C₃₋₆), (alquilen C₁₋₃)-fenilo, (haloalquilen C₁₋₃)-fenilo, (alquilen C₁₋₃)-(heteroarilo de 5 - 10 miembros), (alquilen C₁₋₃)-(heterocicloalquilo de 5 - 9 miembros), (alquilen C₁₋₃)-O-(cicloalquilo C₃₋₆) y (alquilen C₁₋₃)-NH-(cicloalquilo C₃₋₆), en donde el alquilo, alquileno, cicloalquilo, fenilo, heteroarilo y heterocicloalquilo están, cada uno, opcionalmente sustituidos con uno o más sustituyentes seleccionados independientemente de halógeno, -CN, -OH, -NH₂, alquilo C₁₋₃, (haloalquilo C₁₋₃), (cicloalquilo C₃₋₆), -O-(alquilo C₁₋₃), (alquilen C₁₋₃)-O-(alquilo C₁₋₃) y fenilo; R² se selecciona de heterocicloalquilo de 4 - 6 miembros, (alquilen C₁₋₃)-(heterocicloalquilo de 4 - 10 miembros) y (alquilen C₁₋₃)-NR²AR²B, en donde el alquileno y heterocicloalquilo están, cada uno, opcionalmente sustituidos con uno o más sustituyentes seleccionados independientemente de halógeno, oxo, -OH, (alquilo C₁₋₃), -O-(alquilo C₁₋₃), (alquilen C₁₋₃)-C(O)OH, -C(O)H, -C(O)OH, -C(O)(alquilo C₁₋₃), -C(O)(alquilen C₁₋₃)-OH, -C(O)C(O)OH y -SO₂(alquilo C₁₋₃); R²A y R²B se seleccionan cada uno independientemente de H, alquilo C₁₋₃, haloalquilo C₁₋₃, cicloalquilo C₃₋₆, (alquilen C₁₋₃)-O-(alquilo C₁₋₃), (alquilen C₁₋₃)-OH, (alquilen C₁₋₃)-(cicloalquilo C₃₋₆), (alquilen C₁₋₃)-S(=O)-(alquilo C₁₋₃), (alquilen C₁₋₃)-SO₂-(alquilo C₁₋₃) y C(=NH)(alquilo C₁₋₃); o R²A y R²B, tomados junto con el nitrógeno al cual están unidos, forman un anillo heterocicloalquilo de 3 - 10 miembros opcionalmente sustituido con uno o más sustituyentes seleccionados independientemente de halógeno, oxo, -OH, alquilo C₁₋₃, (haloalquilo C₁₋₃), -O-(alquilo C₁₋₃), (alquilen C₁₋₃)-C(O)OH, -C(O)H, - C(O)(alquilo C₁₋₃), -C(O)(alquilen C₁₋₃)-OH, -C(O)C(O)OH y -SO₂(alquilo C₁₋₃), y que opcionalmente contiene un heteroátomo adicional seleccionado del grupo de N, O y S; R³ y R⁴ se seleccionan cada uno independientemente de H, alquilo C₁₋₆ y haloalquilo C₁₋₆; y R⁵ se selecciona de H y alquilo C₁₋₆.There is provided a compound of formula (1) or a pharmaceutically acceptable salt thereof, which is a modulator of 5-HT₂A and can be used in the treatment of diseases and disorders associated with the expression and/or activity of the serotonin 5-HT₂A receptor. . Therefore, methods of treating diseases and disorders related to 5HT₂A are also provided. Claim 1: A compound of formula (1) or a pharmaceutically acceptable salt thereof, wherein: R¹ is selected from C₁₋₆ alkyl, C₃₋₆ cycloalkyl, phenyl, 5-10 membered heteroaryl, 5-9 membered heterocycloalkyl , (C₁₋₃ alkylene)-(C₃₋₆ cycloalkyl), (C₁₋₃ alkylene)-phenyl, (C₁₋₃ haloalkylene)-phenyl, (C₁₋₃ alkylene)-(5-10 membered heteroaryl), ( C₁₋₃ alkylene)-(5-9 membered heterocycloalkyl), (C₁₋₃ alkylene)-O-(C₃₋₆ cycloalkyl) and (C₁₋₃ alkylene)-NH-(C₃₋₆ cycloalkyl), wherein the alkyl, alkylene, cycloalkyl, phenyl, heteroaryl, and heterocycloalkyl are each optionally substituted with one or more substituents independently selected from halogen, -CN, -OH, -NH₂, C₁₋₃ alkyl, (C₁₋₃ haloalkyl), ( C₃₋₆ cycloalkyl), -O-(C₁₋₃ alkyl), (C₁₋₃ alkylene)-O-(C₁₋₃ alkyl) and phenyl; R² is selected from 4-6 membered heterocycloalkyl, (C₁₋₃ alkylene)-(4-10 membered heterocycloalkyl) and (C₁₋₃ alkylene)-NR²AR²B, wherein alkylene and heterocycloalkyl are each optionally substituted with one or more substituents independently selected from halogen, oxo, -OH, (C₁₋₃ alkyl), -O-(C₁₋₃ alkyl), (C₁₋₃ alkylene)-C(O)OH, -C(O)H , -C(O)OH, -C(O)(C₁₋₃ alkyl), -C(O)(C₁₋₃ alkylene)-OH, -C(O)C(O)OH and -SO₂(C₁ alkyl ₋₃); R²A and R²B are each independently selected from H, C₁₋₃ alkyl, C₁₋₃ haloalkyl, C₃₋₆ cycloalkyl, (C₁₋₃ alkylene)-O-(C₁₋₃ alkyl), (C₁₋₃ alkylene)-OH , (C₁₋₃ alkylene)-(C₃₋₆ cycloalkyl), (C₁₋₃ alkylene)-S(=O)-(C₁₋₃ alkyl), (C₁₋₃ alkylene)-SO₂-(C₁₋₃ alkyl) and C(=NH)(C₁₋₃ alkyl); or R²A and R²B, taken together with the nitrogen to which they are attached, form a 3-10 membered heterocycloalkyl ring optionally substituted with one or more substituents independently selected from halogen, oxo, -OH, C₁₋₃ alkyl, (C₁₋ haloalkyl ₃), -O-(C₁₋₃ alkyl), (C₁₋₃ alkylene)-C(O)OH, -C(O)H, -C(O)(C₁₋₃ alkyl), -C(O) (C₁₋₃ alkylene)-OH, -C(O)C(O)OH and -SO₂(C₁₋₃ alkyl), and optionally containing one additional heteroatom selected from the group of N, O and S; R³ and R⁴ are each independently selected from H, C₁₋₆ alkyl, and C₁₋₆ haloalkyl; and R⁵ is selected from H and C₁₋₆ alkyl.

ARP210102981A 2020-10-27 2021-10-27 ISOXAZOLE DERIVATIVES AS MODULATORS OF THE SEROTONIN 5-HT₂A RECEPTOR USEFUL FOR THE TREATMENT OF DISORDERS RELATED THERETO AR123933A1 (en)

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US202063106156P 2020-10-27 2020-10-27

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AR123933A1 true AR123933A1 (en) 2023-01-25

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