AR101692A1 - Compuestos y métodos para inhibir histonas demetilasas - Google Patents

Compuestos y métodos para inhibir histonas demetilasas

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Publication number
AR101692A1
AR101692A1 ARP150102728A ARP150102728A AR101692A1 AR 101692 A1 AR101692 A1 AR 101692A1 AR P150102728 A ARP150102728 A AR P150102728A AR P150102728 A ARP150102728 A AR P150102728A AR 101692 A1 AR101692 A1 AR 101692A1
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AR
Argentina
Prior art keywords
cycloalkyl
alkyl
optionally substituted
heteroaryl
alkynyl
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ARP150102728A
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English (en)
Inventor
Zhang Rui
Yang Ying
Reddy Vakiti Ramkrishna
Ullah Farman
Saraswat Neerja
Labelle Marc
Dudekula Dastagiri
John Cook Cyril
Boesen Thomas
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Epitherapeutics Aps
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Publication of AR101692A1 publication Critical patent/AR101692A1/es

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Abstract

Los compuestos de la solicitud pueden modular la actividad de histonas demetilasas (HDMEs), y pueden ser útiles para la prevención y/o tratamiento de enfermedades en las cuales la desregulación genómica está involucrada en la patogénesis, por ejemplo, cáncer. Reivindicación 1: Un compuesto de la fórmula (1), caracterizado porque: Q es seleccionado de CO₂H, CO₂R²⁰, -CH=NR¹², -W, -CH₂NHR¹³, -CH=O y -CH(OR¹⁷)₂; M es CH o N; A es seleccionado de -C(R²)₂C(O)-, -C(R²)₂C(R²)₂C(O)-, C₃₋₁₀ alquilo, -Z-C₃₋₁₀ cicloalquileno, -Z-heterociclileno, -Z-heteroarileno y -Z-arileno, en donde el C₃₋₁₀ alquilo, -Z-cicloalquileno, -Z-heterociclileno, -Z-heteroarileno y -Z-arileno se encuentran opcionalmente sustituidos con uno o más R³, o A e Y forman un anillo heterocíclico o C₃₋₁₀ cicloalquilo; Y es seleccionado de -H, y-NR⁶R⁷, -OR⁷, C₁₋₈ alquilo, C₂₋₈ alquenilo, C₂₋₈ alquinilo, C₃₋₁₀ cicloalquilo, heterociclilo, heteroarilo y arilo, en donde el alquilo, alquenilo, y alquinilo, cicloalquilo, heterociclilo, heteroarilo y arilo son opcionalmente sustituidos con uno o más R³; R¹ es seleccionado de -H, C₁₋₈ alquilo, C₂₋₈ alquenilo, C₂₋₈ alquinilo, y C₃₋₁₀ cicloalquilo, en donde el alquilo, alquenilo, alquinilo y cicloalquilo están opcionalmente sustituidos con uno o más sustituyentes seleccionados de -OH, arilo, C₁₋₆ alcoxi, heteroarilo, ariloxi, heteroariloxi, -NR⁶R⁷, -F y C₃₋₆ cicloalquilo; o R¹, junto con A-Y y el átomo de nitrógeno al cual está unido, forma un anillo heterocíclico que contiene nitrógeno opcionalmente sustituido con uno o más sustituyentes seleccionados independientemente de C₁₋₈ alquilo, C₂₋₈ alquenilo, C₂₋₈ alquinilo, y C₃₋₁₀ cicloalquilo, en donde el alquilo, alquenilo, alquinilo y cicloalquilo son opcionalmente sustituidos con uno o más sustituyentes independientemente seleccionados de -OH, arilo, C₁₋₆ alcoxi, heteroarilo, ariloxi, heteroariloxi, -NR⁶R⁷, -F y C₃₋₆ cicloalquilo; o R¹ y R¹⁸, junto con los átomos a los cuales están unidos, forman un anillo heterocíclico que contiene nitrógeno opcionalmente sustituido con uno o más sustituyentes seleccionados independientemente de C₁₋₈ alquilo, C₂₋₈ alquenilo, C₂₋₈ alquinilo, y C₃₋₁₀ cicloalquilo, en donde el alquilo, alquenilo, alquinilo y cicloalquilo están opcionalmente sustituidos con uno o más sustituyentes seleccionados independientemente de -OH, arilo, C₁₋₆ alcoxi, heteroarilo, ariloxi, heteroariloxi, -NR⁶R⁷, -F y C₃₋₆ cicloalquilo; cada R² es seleccionado independientemente de -H, C₁₋₈ alquilo, C₂₋₈ alquenilo, C₂₋₈ alquinilo, y C₃₋₁₀ cicloalquilo, en donde el alquilo, alquenilo, alquinilo y cicloalquilo están opcionalmente sustituidos con uno o más sustituyentes seleccionados independientemente de -OH, arilo, C₁₋₆ alcoxi, heteroarilo, ariloxi, heteroariloxi, -F, C₃₋₆ cicloalquilo, -Z-heterociclilo, -Z-arilo, -Z-heteroarilo, -Z-NR⁶R⁷, -Z-C(=O)-NR⁶R⁷, -Z-NR⁶-C(R=O)-R⁷, -Z-C(=O)-R⁷, -Z-OR⁷, halógeno, -Z-SR⁷, -Z-SOR⁷, -Z-SO₂R⁷, -Z-SO₂NR⁶R⁷ y -Z-COOR⁷; o dos sustituyentes R² sobre átomos de carbono adyacentes, junto con los átomos de carbono a los cuales están unidos, forman un anillo heterocíclico o C₄₋₁₀ cicloalquilo; o dos sustituyentes R² sobre el mismo átomo de carbono, junto con el átomo de carbono al cual están unidos, forman un anillo heterocíclico o C₃₋₁₀ cicloalquilo; o R² e Y, junto con los átomos de carbono a los cuales están unidos, forman un anillo heterocíclico o C₄₋₁₀ cicloalquilo; cada R³ es independientemente seleccionado de C₁₋₆ alquilo, C₁₋₄ fluoroalquilo C₁₋₄ hidroxialquilo, C₂₋₆ alquenilo, C₂₋₆ alquinilo, C₃₋₁₀ cicloalquilo, -Z-heterociclilo, -Z-arilo, -Z-heteroarilo, -Z-NR⁶R⁷, -Z-C(=O)-NR⁶R⁷, -Z-NR⁶-C(=O)-R⁷, -Z-C(=O)-R⁷, -Z-OR⁷, halógeno, -Z-SR⁷, -Z-SOR⁷, -Z-SO₂R⁷, -Z-SO₂NR⁶R⁷ y -Z-COOR⁷, en donde el heterociclilo está opcionalmente sustituido con uno o más R⁴, y en donde los heteroarilo y arilo están opcionalmente sustituidos con uno o más R⁵; o dos R³ sobre el mismo átomo de carbono pueden, junto con el átomo de carbono al cual están unidos, formar un anillo heterocíclico o C₃₋₁₀ cicloalquilo; Z es seleccionado de un enlace sencillo, C₁₋₄ alquileno, heterociclileno y C₃₋₆ cicloalquileno; cada R⁴ es independientemente seleccionado de C₁₋₆ alquilo, C₁₋₄ fluoroalquilo, C₁₋₄ hidroxialquilo, C₁₋₄ alcoxi, C₃₋₁₀ cicloalquilo, -Z-NR⁶R⁷, -Z-C(=O)-NR⁶R⁷, -Z-NR⁶-C(=O)-R⁷, -Z-C(=O)-R⁷, -Z-C(=O)-H, -OR⁷, halógeno, -SR⁷, -SOR⁷, -SO₂R⁷, -SO₂NR⁶R⁷, y -COOR⁷; cada R⁵ es independientemente seleccionado: de C₁₋₆ alquilo, C₁₋₄ fluoroalquilo, C₁₋₄ hidroxialquilo, C₁₋₄ alcoxi, C₃₋₆ cicloalquilo, -CN, -F, -Cl, -Br, -Z-NR⁶R⁷, -Z-C(=O)-NR⁶R⁷, -Z-NR⁶-C(=O)-R⁷, -Z-C(=O)-R⁷, -Z-C(=O)-H, -OR⁷, -SR⁷, -SOR⁷, -SO₂R⁷, -SO₂NR⁶R⁷, y -COOR⁷; cada R⁶ y R⁷ es independientemente seleccionada de -H, C₁₋₈ alquilo, C₁₋₄ fluoroalquilo, C₁₋₄ hidroxialquilo, C₂₋₈ alquenilo, C₂₋₈ alquinilo, C₃₋₁₀ cicloalquilo, -Z-heterociclilo, -Z-heteroarilo y -Z-arilo, en donde el alquilo, alquenilo, alquinilo, cicloalquilo, heterociclilo, heteroarilo y arilo están opcionalmente sustituidos con uno o más R⁸; o R⁶ y R⁷ pueden, junto con el N-átomo al cual están unidos, formar un anillo heterocíclico opcionalmente sustituido con uno o más R⁸; cada R⁸ es independientemente seleccionado de C₁₋₆ alquilo, C₁₋₄ fluoroalquilo, C₁₋₄ hidroxialquilo, C₂₋₆ alquenilo, C₂₋₆ alquinilo, C₃₋₁₀ cicloalquilo, -Z-heterociclilo, -Z-heteroarilo, -Z-arilo, -Z-NR¹⁰R¹¹, -Z-C(=O)-NR¹⁰R¹¹, -Z-OR⁹, halógeno, -CN, -Z-SR⁹, -Z-SOR⁹, -Z-SO₂R⁹ y -Z-COOR⁹, en donde el alquilo, alquenilo, alquinilo, cicloalquilo, heterociclilo, heteroarilo y arilo están opcionalmente sustituidos con uno o más sustituyentes seleccionados independientemente de C₁₋₄ alquilo, C₁₋₄ fluoroalquilo, C₁₋₄ hidroxialquilo, C₃₋₆ cicloalquilo, -Z-heterociclilo, -Z-heteroarilo, -Z-arilo, -Z-NR¹⁰R¹¹, -Z-C(=O)-NR¹⁰R¹¹, -Z-OR⁹, halógeno, -CN, -Z-SR⁹, -Z-SOR⁹, -Z-SO₂R⁹ y -Z-COOR⁹; en donde el heterociclilo está opcionalmente sustituido con uno o más R⁴ y en donde los heteroarilo y arilo están opcionalmente sustituidos con uno o más R⁵; cada R⁹ es independientemente seleccionado de ,-H, C₁₋₈ alquilo, C₁₋₄ fluoroalquilo, C₁₋₄ hidroxialquilo, C₂₋₈ alquenilo, C₂₋₈ alquinilo, C₃₋₁₀ cicloalquilo, -Z-heterociclilo, -Z-arilo, y -Z-heteroarilo, en donde el heterociclilo está opcionalmente sustituido con uno o más R⁴ y en donde los heteroarilo y arilo están opcionalmente sustituidos con uno o más R⁵; cada R¹⁰ y R¹¹ es independientemente seleccionado de -H, C₁₋₆ alquilo, C₁₋₄ fluoroalquilo, C₁₋₄ hidroxialquilo, C₂₋₈ alquenilo, C₂₋₈ alquinilo, C₃₋₁₀ cicloalquilo, heterociclilo, heteroarilo, y C₆₋₁₄ arilo, en donde el heterociclilo está opcionalmente sustituido con uno o más R⁴ y en donde los heteroarilo y arilo están opcionalmente sustituidos con uno o más R⁵; o R¹⁰ y R¹¹ pueden junto con el N-átomo al cual están unidos, formar un anillo heterocíclico de 5 a 7 miembros opcionalmente sustituido con uno o más R⁴; cuando Q es -CH=NR¹², R¹² es seleccionado de C₁₋₁₀ alquilo, C₂₋₁₀ alquenilo, C₂₋₁₀ alquinilo, C₃₋₁₀ cicloalquilo, -Z-heterociclilo, -Z-arilo, -Z-heteroarilo, -Z- NR⁶R⁷, -Z-C(=O)-NR⁶R⁷, -Z-NR⁶-C(=O)-R⁷, -Z-C(=O)-R⁷, -Z-OR⁷, -Z-SR⁷, -Z-SOR⁷, -Z-SO₂R⁷ y -Z-COOR⁷, en donde el alquilo, alquenilo, alquinilo, cicloalquilo, heterociclilo, heteroarilo y arilo están opcionalmente sustituidos con uno o más R³; cuando Q es -CH₂NHR¹³, R¹³ es seleccionado de -H, -C(O)R⁷, -C(O)C(O)R⁷, -C(O)C(O)OR⁷, C₁₋₈ alquilo, C₁₋₄ fluoroalquilo, C₁₋₄ hidroxialquilo, C₂₋₈ alquenilo, C₂₋₈ alquinilo, C₃₋₁₀ cicloalquilo, -Z-heterociclilo, y -Z-heteroarilo-monocíclico, en donde el alquilo, alquenilo, alquinilo, cicloalquilo, heterociclilo y heteroarilo son opcionalmente sustituidos con uno más R⁸, o R¹³ es -CR¹⁴R¹⁵NR⁶R⁷, -CR¹⁴R¹⁵CN, o -CR¹⁴R¹⁵OR⁷, en donde cada R¹⁴ y R¹⁵ es independientemente seleccionado de -H, C₁₋₈ alquilo, C₂₋₈ alquenilo, C₂₋₈ alquinilo, C₃₋₁₀ cicloalquilo, heterociclilo, heteroarilo, y C₆₋₁₄ arilo, en donde el alquilo, alquenilo, alquinilo, cicloalquilo, heterociclilo, heteroarilo y arilo son opcionalmente sustituidos con uno o más R³; o en donde R¹⁴ y R¹⁵ junto con el átomo de carbono interviniente forman un anillo C₅₋₁₀ cicloalquenil o C₃₋₁₀ cicloalquilo opcionalmente sustituido con uno o más R³; cuando Q es W, W es seleccionado de un grupo 1,3-diazacicloalquil-2-il que es N-sustituido con R¹⁶, opcionalmente sustituido a su vez con uno o más R³, y que opcionalmente contienen uno o dos grupos oxo; un grupo 1,3-tiazacicloaquil-2-il que es N-sustituido con R¹⁶, opcionalmente sustituido a su vez con uno o más R³ y que opcionalmente contiene uno o dos grupos oxo; y un grupo 1,3-oxazacicloalquil-2-il que es N-sustituido con R¹⁶, opcionalmente sustituido a su vez con uno o más R³, y que opcionalmente contiene uno o dos grupos oxo, en donde en todas las tres instancias dos R³ sobre el mismo átomo de carbono pueden, junto con el átomo de carbono al cual están unidos, formar un anillo heterocíclico o C₃₋₁₀ cicloalquilo; R¹⁶ es seleccionado de-H, -C(O)R⁷, -C(O)C(O)R⁷ y -C(O)C(O)OR⁷; cuando Q es -CH(OR¹⁷)₂, cada R¹⁷ es independientemente R³; o en donde dos R¹⁷ junto con el -O-CH-O- interviniente forman un anillo heterocíclico opcionalmente sustituido con uno o más R³ y que opcionalmente contienen uno a dos grupos oxo; R¹⁸ es seleccionado de -H, C₁₋₆ alquilo, C₁₋₆ fluoroalquilo, C₁₋₆ hidroxialquilo, C₂₋₇ alquenilo, C₂₋₇ alquinilo, C₃₋₇ cicloalquilo, y C₃₋₇ oxialquilo; o R¹⁸ y A, junto con los átomos a los cuales están unidos, forman un anillo heterocíclico; o R¹⁸ e Y, junto con los átomos a los cuales están unidos, forman un anillo heterocíclico; o R¹⁸ y R¹, junto con los átomos a los cuales están unidos, forman un anillo heterocíclico; R¹⁹ es seleccionado de C₁₋₈ alquilo, C₂₋₈ alquenilo, C₂₋₈ alquinilo, y C₃₋₁₀ cicloalquilo, en donde el alquilo, alquenilo, alquinilo y cicloalquilo son opcionalmente sustituidos con uno o más sustituyentes seleccionados independientemente de arilo, C₁₋₆ alcoxi, heteroarilo, ariloxi, heteroariloxi, C₃₋₆ cicloalquilo, -Z-heterociclilo, -Z-arilo, -Z-heteroarilo, -Z-NR⁶R⁷, -Z-C(=O)-NR⁶R⁷, -Z-NR⁶-C(=O)-R⁷, -Z-C(=O)-R⁷, Z-OR⁷, halógeno, -Z-SR⁷, -Z-SOR⁷, -Z-SO₂R⁷, -Z-SO₂NR⁶R⁷ y -Z-COOR⁷; y puede formar opcionalmente una estructura ciclofano al unir a Y o A; y cuando Q es CO₂R²⁰, R²⁰ es seleccionado de C₁₋₈ alquilo, C₁₋₄ fluoroalquilo, C₁₋₄ hidroxialquilo, C₂₋₈ alquenilo, C₂₋₈ alquinilo, C₃₋₁₀ cicloalquilo, -Z-heterociclilo, -Z-arilo, y -Z-heteroarilo, en donde el C₁₋₈ alquilo, C₃₋₁₀ cicloalquilo y heterociclilo son opcionalmente sustituidos con uno o más R⁴, y en donde los heteroarilo y arilo son opcionalmente sustituidos con uno o más R⁵ como se define con anterioridad; o una sal o solvato farmacéuticamente aceptable del mismo.
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