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AR054866A1 - Inhibidores de histona deacetilasa - Google Patents

Inhibidores de histona deacetilasa

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Publication number
AR054866A1
AR054866A1 ARP060103038A ARP060103038A AR054866A1 AR 054866 A1 AR054866 A1 AR 054866A1 AR P060103038 A ARP060103038 A AR P060103038A AR P060103038 A ARP060103038 A AR P060103038A AR 054866 A1 AR054866 A1 AR 054866A1
Authority
AR
Argentina
Prior art keywords
alkyl
3alkyl
cycloalkyl
substituted
heterocycloalkyl
Prior art date
Application number
ARP060103038A
Other languages
English (en)
Inventor
Jerome C Bressi
Anthony R Gangloff
Lily Kwok
Original Assignee
Takeda San Diego Inc
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Takeda San Diego Inc filed Critical Takeda San Diego Inc
Publication of AR054866A1 publication Critical patent/AR054866A1/es

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    • C07D231/10—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
    • C07D231/12—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms
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    • A61K31/00—Medicinal preparations containing organic active ingredients
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    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/415—1,2-Diazoles
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    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
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    • C07D209/04—Indoles; Hydrogenated indoles
    • C07D209/10—Indoles; Hydrogenated indoles with substituted hydrocarbon radicals attached to carbon atoms of the hetero ring
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    • C07D231/10—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
    • C07D231/14—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
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    • C07D401/04—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings directly linked by a ring-member-to-ring-member bond
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    • C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
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    • C07D405/04—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings directly linked by a ring-member-to-ring-member bond
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    • C07D405/12—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a chain containing hetero atoms as chain links
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    • C07D471/04—Ortho-condensed systems

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Abstract

Reivindicacion 1: Un compuesto caracterizado porque comprende la formula (1), en donde: n se selecciona del grupo formado por 0, 1, 2, 3, y 4; A1 se selecciona del grupo formado por cicloalquilo C3-12, hetero-cicloalquiloC3-12, bicicloalquilo C9-12, hetero-bicicloalquiloC3-12, arilo, heteroarilo, bicicloarilo C9-12, y hetero-bicicloariloC4-12, cada uno sustituido o no sustituido; L es un ligador que provee una separacion de 0-6 átomos entre los dos átomos del anillos a los cuales L está unido; J1 se selecciona del grupo formado por -CR7R7'- y -NR19-; J2 se selecciona del grupo formado por -CR20R20' y -NR10-; R1 y R2 se seleccionan cada uno en forma independiente del grupo formado por hidrogeno, hidroxi, alcoxi, ariloxi, heteroariloxi, carbonilo, amino, alquilamino C1-10, sulfonamido, imino, sulfonilo, sulfinilo, alquilo C1-10, halo-alquiloC1-10, carbonil-alquiloC1-3, tiocarbonil-alquiloC1-3, sulfonil-alquiloC1-3, sulfinil-alquiloC1-3, amino-alquiloC1-10, imino-alquiloC1-3, cicloalquilC3-12-alquiloC1-5, hetero-cicloalquilC3-12-alquiloC1-5, aril-alquiloC1-10, heteroaril-alquiloC1-5, bicicloalquilC9-12-alquiloC1-5, hetero-bicicloarilC8-12-alquiloC1-5, cicloalquilo C3-12, hetero-cicloalquiloC3-12, bicicloalquilo C9-12, hetero-bicicloalquiloC3-12, arilo, heteroarilo, bicicloarilo C9-12 y hetero-bicloariloC4-12, cada uno sustituido o no sustituido, o R1 y R2 se pueden tomar juntos para formar un anillo sustituido o no sustituido; R3 se selecciona del grupo formado por hidrogeno, hidroxi, alcoxi, ariloxi, heteroariloxi, carbonilo, amino, alquilamino C1-10, sulfonamido, imino, sulfonilo, sulfinilo, alquilo C1-10, halo-alquiloC1-10, carbonil-alquiloC1-3, tiocarbonil-alquiloC1-3, sulfonil-alquiloC1-3, sulfinil- alquiloC1-3, amino-alquiloC1-10, imino-alquiloC1-3, cicloalquilC3-12-alquiloC1-5, hetero-cicloalquilC3-12-alquiloC1-5, aril-alquiloC1-10, heteroaril-alquiloC1-5, bicicloarilC9-12-alquiloC1-5, hetero-bicicloarilC8-12-alquiloC1-5, cicloalquilo C3-12, hetero-cicloalquiloC3-12, bicicloalquilo C9-12, hetero-bicicloalquiloC3-12, arilo, heteroarilo, bicicloarilo C9-12 y hetero-bicicloariloC4-12, cada uno sustituido o no sustituido; cada R4 se selecciona del grupo formado por hidrogeno, halo, nitro, ciano, tio, hidroxi, alcoxi, ariloxi, heteroariloxi, carbonilo, amino, alquilamino C1-10, sulfonamido, imino, sulfonilo, sulfinilo, alquilo C1-10, halo-alquiloC1-10, carbonil-alquiloC1-3, tiocarbonil-alquiloC1-3, sulfonil-alquiloC1-3, sulfinil- alquiloC1-3, amino-alquiloC1-10, imino-alquiloC1-3, cicloalquilC3-12-alquiloC1-5, hetero-cicloalquilC3-12-alquiloC1-5, aril-alquiloC1-10, heteroaril-alquiloC1-5, bicicloarilC9-12-alquiloC1-5, hetero-bicicloarilC8-12-alquiloC1-5, cicloalquilo C3-12, hetero-cicloalquiloC3-12, bicicloalquilo C9-12, hetero-bicicloalquiloC3-12, arilo, heteroarilo, bicicloarilo C9-12 y hetero-bicicloariloC4-12, cada uno sustituido o no sustituido; R5, R5', R6, R6', R7, R7', R20, y R20' se seleccionan cada uno en forma independiente del grupo formado por hidrogeno, halo, nitro, ciano, oxo, tio, hidroxi, alcoxi, ariloxi, heteroariloxi, carbonilo, amino, alquilamino C1-10, amido, carboxamido, sulfonamido, imino, sulfonilo, sulfinilo, alquilo C1-10, halo- alquiloC1-10, carbonil-alquiloC1-3, tiocarbonil-alquiloC1-3, sulfonil-alquiloC1-3, sulfinil-alquiloC1-3, amino-alquiloC1-10, imino-alquiloC1-3, cicloalquilC3-12-alquiloC1-5, hetero-cicloalquilC3-12-alquiloC1-5, aril-alquiloC1-10, heteroaril- alquiloC1-5, bicicloarilC9-12-alquiloC1-5, hetero-bicicloarilC8-12-alquiloC1-5, cicloalquilo C3-12, hetero-cicloalquiloC3-12, bicicloalquilo C9-12, hetero-bicicloalquiloC3-12, arilo, heteroarilo, bicicloarilo C9-12 y hetero-bicicloariloC4-12, cada uno sustituido o no sustituido, dos cualquiera de R5, R5', R6, R6', R7, R7', R20, y R20' se pueden tomar juntos para formar un anillo sustituido o no sustituido, con la salvedad de que R5, R6, R7 y R20, cada uno en forma independiente están ausentes cuando el C al cual están unidos está unido a L, R5' y R6', 67' y R20', cada uno en forma independiente están ausentes cuando el C al cual están unidos forma parte de un doble enlace; y R8, R10 y R19 se selecciona cada uno en forma independiente del grupo formado por hidrogeno, hidroxi, alcoxi, ariloxi, heteroariloxi, carbonilo, amino, alquilamino C1-10, sulfonamido, imino, sulfonilo, sulfinilo, alquilo C1-10, halo-alquiloC1-10, carbonil-alquiloC1-3, tiocarbonil-alquiloC1-3, sulfonil-alquiloC1- 3, sulfinil-alquiloC1-3, amino-alquiloC1-10, imino-alquiloC1-3, cicloalquilC3-12-alquiloC1-5, hetero-cicloalquilC3-12-alquiloC1-5, aril-alquiloC1-10, heteroaril-alquiloC1-5, bicicloarilC9-12-alquiloC1-5, hetero-bicicloarilC8-12-alquiloC1-5, cicloalquilo C3-12, hetero-cicloalquiloC3-12, bicicloalquilo C9-12, hetero-bicicloalquiloC3-12, arilo, heteroarilo, bicicloarilo C9-12 y hetero-bicicloariloC4-12, cada uno sustituido o no sustituido, o R8 y cualquiera de R5, R5', R6, R6', R7, R7', R20, R20', R10 y R19 se pueden tomar juntos para formar un anillo sustituido o no sustituido, o R10 y cualquiera de R5, R5', R6, R6', R7, R7', R20, R20', R20', y R19, se pueden tomar juntos para formar un anillo sustituido o no sustituido, o R19 y cualquiera de R5, R5', R6, R6', R20, y R20', se pueden tomar juntos para formar un anillo sustituido o no sustituido, con la salvedad de que R8, R10 y R19 cada uno en forma independiente están ausentes cuando el N al cual están unidos está unido a L, y R8, R10 y R19 cada uno en forma independiente están ausentes cuando el N al cual están unidos forma parte de un doble enlace.
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