AR099890A1 - Inhibidores de histona demetilasas - Google Patents

Inhibidores de histona demetilasas

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Publication number
AR099890A1
AR099890A1 ARP150100947A ARP150100947A AR099890A1 AR 099890 A1 AR099890 A1 AR 099890A1 AR P150100947 A ARP150100947 A AR P150100947A AR P150100947 A ARP150100947 A AR P150100947A AR 099890 A1 AR099890 A1 AR 099890A1
Authority
AR
Argentina
Prior art keywords
cycloalkyl
aryl
heteroaryl
alkynyl
alkenyl
Prior art date
Application number
ARP150100947A
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English (en)
Inventor
Labelle Marc
Zhang Rui
D Martyr Cuthbert
Saraswat Neerja
Boesen Thomas
Original Assignee
Epitherapeutics Aps
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Publication date
Application filed by Epitherapeutics Aps filed Critical Epitherapeutics Aps
Publication of AR099890A1 publication Critical patent/AR099890A1/es

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    • C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
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Abstract

Reivindicación 1: Un compuesto de la fórmula (1) en donde Q se selecciona CO₂H, -CH=NR¹², -W, -CHR²⁰NR²¹R¹³, -CH=O y -CH(OR¹⁷)₂; A se selecciona de -C(R²ᵃ)₂C(O)-, -C(R²)₂C(R²)₂C(O)-, -Z-cicloalquileno C₃₋₁₀, -Z-heterociclileno, -Z-heteroarileno y -Z-arileno, cuyos -Z-cicloalquileno, -Z-heterociclileno, -Z-heteroarileno y -Z-arileno pueden estar opcionalmente sustituidos con uno o varios R³ y pueden formar una estructura cíclica o heterocíclica con Y, en donde dicha estructura cíclica o heterocíclica formada con Y se fusiona opcionalmente con un grupo arilo o heteroarilo opcionalmente sustituido; Z se selecciona de alquileno C₁₋₄, alqueneno C₂₋₅, alquineno C₂₋₅, heterociclileno y cicloalquileno C₃₋₆; cada M se selecciona, de modo independiente, CH o N; Y se selecciona de -H, -NR⁶R⁷, -OR⁷, alquilo C₁₋₈, alquenilo C₂₋₈, alquinilo C₂₋₈, cicloalquilo C₃₋₁₀, heterociclilo, heteroarilo y arilo, cuyos alquilo, alquenilo, alquinilo, cicloalquilo, heterociclilo, heteroarilo y arilo pueden estar opcionalmente sustituidos con uno o varios R³; R¹ se selecciona de -H, alquilo C₁₋₈, alquenilo C₂₋₈, alquinilo C₂₋₈, cicloalquilo C₃₋₁₀, cuyos alquilo, alquenilo, alquinilo y cicloalquilo pueden estar opcionalmente sustituidos con uno o varios seleccionados de -OH, arilo, alcoxi C₁₋₆, heteroarilo, ariloxi, heteroariloxi, -NR⁶R⁷, F y cicloalquilo C₃₋₆; o con mayor preferencia, se selecciona de -H y alquilo C₁₋₄; o con -A-Y forma un nitrógeno que contiene grupo heterocíclico opcionalmente sustituido donde la sustitución opcional puede ser alquilo C₁₋₈, alquenilo C₂₋₈, alquinilo C₂₋₈, cicloalquilo C₃₋₁₀, alcoxi C₁₋₆, hidroxialquilo C₁₋₆, arilo, -C(=O)NR⁶R⁷, -NR⁶R⁷, -OH y halógeno, cuyos alquilo, alquenilo, alquinilo, cicloalquilo y arilo pueden estar opcionalmente sustituidos con uno o varios seleccionados de -OH, arilo, alcoxi C₁₋₆, heteroarilo, ariloxi, heteroariloxi, -NR⁶R⁷, F y cicloalquilo C₃₋₆; o dicho nitrógeno que contiene grupo heterocíclico opcionalmente sustituido formado con -A-Y se fusiona opcionalmente con un grupo arilo o heteroarilo opcionalmente sustituido; o con R¹⁸ forma un nitrógeno que contiene grupo heterocíclico opcionalmente sustituido donde la sustitución opcional puede ser alquilo C₁₋₈, alquenilo C₂₋₈, alquinilo C₂₋₈ o cicloalquilo C₃₋₁₀, cuyos alquilo, alquenilo, alquinilo y cicloalquilo pueden estar opcionalmente sustituidos con uno o varios seleccionados de -OH, arilo, alcoxi C₁₋₆, heteroarilo, ariloxi, heteroariloxi, -NR⁶R⁷, F y cicloalquilo C₃₋₆; R² se selecciona de -H, alquilo C₁₋₈, alquenilo C₂₋₈, alquinilo C₂₋₈ y cicloalquilo C₃₋₁₀, cuyos alquilo, alquenilo, alquinilo y cicloalquilo pueden estar opcionalmente sustituidos con uno o varios seleccionados de -OH, arilo, alcoxi C₁₋₆, heteroarilo, ariloxi, heteroariloxi, F y cicloalquilo C₃₋₆, -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; de modo alternativo, R² puede formar una estructura cíclica o heterocíclica con otros R², R¹, R¹⁸ o Y; R²ᵃ se selecciona de -H, alquilo C₁₋₈, alquenilo C₂₋₈, alquinilo C₂₋₈ y cicloalquilo C₃₋₁₀, cuyos alquilo, alquenilo, alquinilo y cicloalquilo pueden estar opcionalmente sustituidos con uno o varios seleccionados de -OH, arilo, alcoxi C₁₋₆, heteroarilo, ariloxi, heteroariloxi, F y cicloalquilo C₃₋₆, -Z-heterociclilo, -Z-arilo, -Z-heteroarilo, -Z-NR⁶R⁷, -Z-C(=O)-NR⁶R⁷, -Z-NR⁶-C(=O)-R⁷, -Z-NR⁶-C(=O)-OR⁷, -Z-C(=O)-OR⁷, -Z-OR⁷, halógeno, -Z-SR⁷, -Z-SOR⁷, -Z-SO₂R⁷, -Z-SO₂NR⁶R⁷ y -Z-COOR⁷; siempre que los dos grupos R²ᵃ son ambos no hidrógeno o uno de R²ᵃ forma un anillo con R¹ o R¹⁸; cada R³ se selecciona, de modo independiente, de alquilo C₁₋₆, fluoroalquilo C₁₋₄, hidroxialquilo C₁₋₄, alquenilo C₂₋₆, alquinilo C₂₋₆, cicloalquilo C₃₋₁₀, -Z-heterociclilo, -Z-arilo, -Z-heteroarilo, -Z-NR⁶R⁷, -Z-C(=O)-NR⁶R⁷, -Z-NR⁶-C(=O)-R⁷, -Z-NR⁶-C(=O)-OR⁷, -Z-C(=O)-R⁷, -Z-OR⁷, halógeno, -Z-SR⁷, -Z-SOR⁷, -Z-SO₂R⁷, -Z-SO₂NR⁶R⁷ y -Z-COOR⁷, en donde cualquier heterociclilo puede estar sustituido con uno o varios R⁴ y en donde cualquier heteroarilo y cualquier arilo puede estar sustituido con uno o varios R⁵; Z se selecciona de un enlace simple, alquileno C₁₋₄, heterociclileno y cicloalquileno C₃₋₆; cada R⁴ se selecciona, de modo independiente, de alquilo C₁₋₆, fluoroalquilo C₁₋₄, hidroxialquilo C₁₋₄, alcoxi C₁₋₄, cicloalquilo C₃₋₁₀, NR⁶R⁷, C(=O)-NR⁶R⁷, NR⁶-C(=O)-R⁷, Z-C(=O)-R⁷, -Z-C(=O)-H, OR⁷, halógeno, SR⁷, SOR⁷, SO₂R⁷, SO₂NR⁶R⁷ y COOR⁷ y -OH; cada R⁵ se selecciona, de modo independiente, de alquilo C₁₋₆, fluoroalquilo C₁₋₄, hidroxialquilo C₁₋₄, alcoxi C₁₋₄, cicloalquilo C₃₋₆, -Z-C(=O)-NR⁶R⁷, -Z-NR⁶-C(=O)-R⁷, -Z-C(=O)-R⁷, -Z-C(=O)OR⁷, -Z-NR⁶C(=O)OR⁷, OR⁷, -CN y halógeno; cada uno de R⁶ y R⁷ se selecciona, de modo independiente, de hidrógeno, donde opcionalmente no son ambos hidrógeno, alquilo C₁₋₈, fluoroalquilo C₁₋₄, perfluoroalquilo C₁₋₄, hidroxialquilo C₁₋₄, alquenilo C₂₋₈, alquinilo C₂₋₈, cicloalquilo C₃₋₁₀, -Z-heterociclilo, -Z-heteroarilo y -Z-arilo, cuyos alquilo, alquenilo, alquinilo, cicloalquilo, heterociclilo, heteroarilo y arilo pueden estar opcionalmente sustituidos con uno o varios R⁸ seleccionados de modo independiente; o, de modo alternativo, R⁶ y R⁷ pueden formar, junto con el átomo de N al que están unidos, un anillo N-heterocíclico opcionalmente sustituido con uno o varios R⁸ seleccionados de modo independiente; cada R⁸ se selecciona, de modo independiente, de alquilo C₁₋₆, fluoroalquilo C₁₋₄, hidroxialquilo C₁₋₄, alquenilo C₂₋₆, alquinilo C₂₋₆, cicloalquilo C₃₋₁₀, -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, cuyos alquilo, alquenilo, alquinilo, cicloalquilo, heterocíclicos, heteroarilo y arilo pueden estar opcionalmente sustituidos con uno o varios seleccionados de alquilo C₁₋₄, fluoroalquilo C₁₋₄, hidroxialquilo C₁₋₄, cicloalquilo C₃₋₆, -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 cualquier heterociclilo puede también estar sustituido con uno o varios R⁴ como se definió con anterioridad y en donde cualquier heteroarilo y cualquier arilo también puede estar sustituido con uno o varios R⁵ como se definió con anterioridad; cada R⁹ se selecciona, de modo independiente, de -H, alquilo C₁₋₈, fluoroalquilo C₁₋₄, hidroxialquilo C₁₋₄, alquenilo C₂₋₈, alquinilo C₂₋₈, cicloalquilo C₃₋₁₀, -Z-heterociclilo, -Z-arilo y -Z-heteroarilo, en donde cualquier heterociclilo puede estar sustituido con uno o varios R⁴ como se definió con anterioridad y en donde cualquier heteroarilo y cualquier arilo puede estar sustituido con uno o varios R⁵ como se definió con anterioridad; cada uno de R¹⁰ y R¹¹ se selecciona, de modo independiente, de -H, alquilo C₁₋₆, fluoroalquilo C₁₋₄, hidroxialquilo C₁₋₄, alquenilo C₂₋₈, alquinilo C₂₋₈, cicloalquilo C₃₋₁₀, heterociclilo, heteroarilo y arilo, en donde cualquier heterociclilo puede estar sustituido con uno o varios R⁴ como se definió con anterioridad y en donde cualquier heteroarilo y cualquier arilo puede estar sustituido con uno o varios R⁵ como se definió con anterioridad, o, de modo alternativo, R¹⁰ y R¹¹ pueden formar, junto con el átomo de N al que están unidos, un anillo N-heterocíclico opcionalmente de 5 a 7 miembros, opcionalmente sustituido con uno o varios R⁴ como se definió con anterioridad; cuando Q es -CH=NR¹², R¹² se selecciona de alquilo C₁₋₁₀, alquenilo C₂₋₁₀, alquinilo C₂₋₁₀, cicloalquilo C₃₋₁₀, -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 y -Z-COOR⁷, cuyos alquilo, alquenilo, alquinilo, cicloalquilo, heterociclilo, heteroarilo y arilo pueden estar opcionalmente sustituidos con uno o varios R³; cuando Q es -CHR²⁰NR²¹R¹³, R¹³ se selecciona de hidrógeno, -C(O)R⁷, -C(O)C(O)R⁷, -C(O)C(O)OR⁷, alquilo C₁₋₈, fluoroalquilo C₁₋₄, perfluoroalquilo C₁₋₄, hidroxialquilo C₁₋₄, alquenilo C₂₋₈, alquinilo C₂₋₈, cicloalquilo C₃₋₁₀, -Z-heterociclilo, -Z-arilo y -Z-heteroarilo, cuyos alquilo, alquenilo, alquinilo, cicloalquilo, heterociclilo, arilo y heteroarilo pueden estar opcionalmente sustituidos con uno o varios seleccionados de modo independiente R⁸ o es -CR¹⁴R¹⁵-NR⁶R⁷, -CR¹⁴R¹⁵CN o -CR¹⁴R¹⁵OR⁷, en donde cada uno de R¹⁴ y R¹⁵ se selecciona, de modo independiente, de -H, alquilo C₁₋₈, alquenilo C₂₋₈, alquinilo C₂₋₈, cicloalquilo C₃₋₁₀, heterociclilo, heteroarilo y arilo y en donde R¹⁴ y R¹⁵ junto con el átomo de carbono interviniente pueden designar un anillo cicloalquilo C₃₋₁₀ o cicloalquenilo C₅₋₁₀, cuyos alquilo, alquenilo, alquinilo, cicloalquilo (anillo), anillo cicloalquenilo, heterociclilo, heteroarilo y arilo pueden estar opcionalmente sustituidos con uno o varios R³; R²⁰ y R²¹ son hidrógeno o forman juntos un grupo a 1,3-diaza-C₅₋₇-cicIoalqu-2-ilo que está N-sustituido con R¹⁶ y opcionalmente también sustituido con uno o varios R⁶ y que opcionalmente contiene uno o dos grupos oxo; un grupo 1,3-tiaza-C₅₋₇-cicloalqu-2-ilo que está N-sustituido con R¹⁶ y opcionalmente también sustituido con uno o varios R³ y que opcionalmente contiene uno o dos grupos oxo; un grupo 1,3-oxaza-C₅₋₇-cicloalqu-2-ilo que está N-sustituido con R¹⁶ y opcionalmente también sustituido con uno o varios R⁶ y que opcionalmente contiene uno o dos grupos oxo, en donde en todas las tres instancias, dos R³ en el mismo átomo de carbono pueden formar juntos un grupo espiro; cuando Q es W, W se selecciona de un grupo 1,3-diaza-C₅₋₇-cicloalqu-2-ilo que está N-sustituido con R¹⁶ y opcionalmente también sustituido con uno o varios R³ y que opcionalmente contiene uno o dos grupos oxo; un grupo 1,3-tiaza-C₅₋₇-cicloalqu-2-ilo que está N-sustituido con R¹⁶ y opcionalmente también sustituido con uno o varios R³ y que opcionalmente contiene uno o dos grupos oxo; un grupo 1,3-oxaza-C₅₋₇-cicloalqu-2-ilo que está N-sustituido con R¹⁶ y opcionalmente también sustituido con uno o varios R⁶ y que opcionalmente contiene uno o dos grupos oxo, en donde en todas las tres instancias, dos R³ en el mismo átomo de carbono pueden formar juntos un grupo espiro; R¹⁶ se selecciona de hidrógeno, -C(O)R⁷, -C(O)C(O)R⁷, -C(O)C(O)OR⁷ y -C(O)C(O)NR⁶R⁷; cuando Q es -CH(OR¹⁷)₂, cada R¹⁷ es, de modo independiente, R³ o en donde dos sustituyentes de R¹⁷ junto con el -O-CH(-)-O- interviniente pueden formar un heterociclilo opcionalmente sustituido con uno o varios R³ y que contienen hasta dos grupos oxo; R¹⁸ se selecciona de hidrógeno, alquilo C₁₋₆, fluoroalquilo C₁₋₆, hidroxialquilo C₁₋₆, alquenilo C₂₋₇, alquinilo C₂₋₇, cicloalquilo C₃₋₇, oxialquilo C₃₋₇ y pueden formar una estructura cíclica o heterocíclica con A, Y o R¹; uno de sus isómeros o una mezcla de sus isómeros o una de sus sales o solvatos o profármacos farmacéuticamente aceptables.
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