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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
Authority
AR
Argentina
Prior art keywords
cycloalkyl
alkyl
optionally substituted
heteroaryl
alkynyl
Prior art date
Application number
ARP150102728A
Other languages
English (en)
Inventor
Zhang Rui
Yang Ying
Reddy Vakiti Ramkrishna
Ullah Farman
Saraswat Neerja
Labelle Marc
Dudekula Dastagiri
John Cook Cyril
Boesen Thomas
Original Assignee
Epitherapeutics Aps
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Publication date
Application filed by Epitherapeutics Aps filed Critical Epitherapeutics Aps
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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