AR078537A1 - Derivados heterociclicos de indol ligandos del receptor de estrogenos, composiciones farmaceuticas que los contienen y uso de los mismos para el tratamiento de enfermedades asociadas al sistema nervioso central, osteoporosis, canceres y otras patologias - Google Patents

Derivados heterociclicos de indol ligandos del receptor de estrogenos, composiciones farmaceuticas que los contienen y uso de los mismos para el tratamiento de enfermedades asociadas al sistema nervioso central, osteoporosis, canceres y otras patologias

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Publication number
AR078537A1
AR078537A1 ARP100103630A ARP100103630A AR078537A1 AR 078537 A1 AR078537 A1 AR 078537A1 AR P100103630 A ARP100103630 A AR P100103630A AR P100103630 A ARP100103630 A AR P100103630A AR 078537 A1 AR078537 A1 AR 078537A1
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Argentina
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alkyl
group
alkynyl
cycloalkyl
alkenyl
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ARP100103630A
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Karobio Ab
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Priority claimed from GB0917575A external-priority patent/GB0917575D0/en
Priority claimed from GBGB1004377.6A external-priority patent/GB201004377D0/en
Application filed by Karobio Ab filed Critical Karobio Ab
Publication of AR078537A1 publication Critical patent/AR078537A1/es

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Abstract

Reivindicacion 1: Un compuesto de formula (1) o un éster, amida, solvato o sal farmacéuticamente aceptable del mismo, incluyendo una sal de dicho éster o dicha amida, y un solvato de dicho éster, dicha amida o sal, en la cual R1 se selecciona del grupo formado por halogeno, ciano, nitro, ORA, N(RB)2,-C(O)alquilo C1-4, -SO2alquilo C1-4, alquilo C1-6, alquenilo C2-6, alquinilo C2-6, haloalquilo C1-6, dihaloalquilo C1-6, trihaloalquilo C1-6, haloalquenilo C2-6, dihaloalquenilo C2-6, trihaloalquenilo C2-6, cianoalquilo C1-6, alcoxi C1-4alquilo C1-6, cicloalquilo C3-8, cicloalquil C3-8alquilo C1-6, fenilo, bencilo, y heterociclilo de 5-10 miembros, donde dicho grupo fenilo, bencilo o heterociclilo puede estar sin sustituir o sustituido con entre 1 y 3 sustituyentes, estando cada sustituyente seleccionado independientemente del grupo formado por ORA, halogeno, ciano, nitro, -C(O)alquilo C1-4, alquilo C1-6, alquenilo C2-6, alquinilo C2-6, haloalquilo C1-6, dihaloalquilo C1-6 y trihaloalquilo C1-6; R2 se selecciona del grupo formado por ciano, nitro, N(OH)2, -CHO, -CH=N-OH, -C(O)alquilo C1-4 opcionalmente sustituido con entre 1 y 3 halogenos, -SO2alquilo C1-4, -C(O)NH-OH, -C(NH2)=N-OH, -C(CO2H)=N-OH, -C(NH2)=NH, -C(NH2)=N-NH2, -NH-C(NH2)=NH, -NH-C(O)NH2, -N=C(-NH-CH2CH2-NH-), -S-CN, -S-C(NH2)=NH, -S-C(NH2)=N-OH, -CO2H, -CH(OH)CO2H, -C(O)N(RC)2, -SO2alquilo C1-6, SO2N(RC)2, -C(O)-C(O)-NH2, -CH2NH-CONH2, -SO2ORC, -C(O)CO2H, -CH2SO3H y heterociclilo de 5-10 miembros donde dicho grupo heterociclilo puede estar sin sustituir o sustituido con entre 1 y 3 sustituyentes estando cada sustituyente seleccionado independientemente del grupo formado por ORA, halogeno, ciano, nitro, alquilo C1-6, alquenilo C2-6, alquinilo C2-6, haloalquilo C1-6, dihaloalquilo C1-6 y trihaloalquilo C1-6; cada uno de R3, R4, R5, R6, R7, R8, R9 y R10 se selecciona independientemente del grupo formado por hidrogeno, ORA, halogeno, ciano, nitro, alquilo C1-6, alquenilo C2-6, alquinilo C2-6, haloalquilo C1-6, dihaloalquilo C1-6 y trihaloalquilo C1-6; cada RA se selecciona independientemente del grupo formado por hidrogeno, alquilo C1-6, alquenilo C2-6, alquinilo C2-6, cicloalquilo C3-8, cicloalquil C3-8alquilo C1-6, fenilo, bencilo y heterociclilo de 5-10 miembros, cada uno opcionalmente sustituido con entre 1 y 3 átomos de halogeno; y cada RB se selecciona independientemente del grupo formado por hidrogeno, alquilo C1-6, alquenilo C2-6, alquinilo C2-6, cicloalquilo C3-8, cicloalquil C3-8alquilo C1-6, fenilo, bencilo y heterociclilo de 5-10 miembros, cada uno opcionalmente sustituido con entre 1 y 3 átomos de halogeno; y cada RC se selecciona independientemente del grupo formado por hidrogeno y alquilo C1-6.
ARP100103630A 2009-10-07 2010-10-06 Derivados heterociclicos de indol ligandos del receptor de estrogenos, composiciones farmaceuticas que los contienen y uso de los mismos para el tratamiento de enfermedades asociadas al sistema nervioso central, osteoporosis, canceres y otras patologias AR078537A1 (es)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
GB0917575A GB0917575D0 (en) 2009-10-07 2009-10-07 Novel estrogen receptor ligands
GBGB1004377.6A GB201004377D0 (en) 2010-03-16 2010-03-16 Novel estrogen receptor ligands

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AR078537A1 true AR078537A1 (es) 2011-11-16

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US (1) US8710243B2 (es)
EP (1) EP2486010B1 (es)
JP (1) JP5687704B2 (es)
CN (1) CN102791688B (es)
AR (1) AR078537A1 (es)
DK (1) DK2486010T3 (es)
ES (1) ES2744219T3 (es)
IN (1) IN2012DN02555A (es)
TW (1) TW201124404A (es)
WO (1) WO2011042473A2 (es)

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GB201113538D0 (en) 2011-08-04 2011-09-21 Karobio Ab Novel estrogen receptor ligands
CN105960236A (zh) 2013-12-05 2016-09-21 卡罗医药股份公司 用于治疗间皮瘤的雌激素受体β激动剂
CA2959753A1 (en) 2014-09-02 2016-03-10 The Regents Of The University Of California Estrogen receptor ligand treatment for neurodegenerative diseases
WO2016097036A1 (en) * 2014-12-17 2016-06-23 Karo Bio Ab Estrogen receptor ligand for use in treating melanoma
US11624095B2 (en) 2017-09-27 2023-04-11 Case Western Reserve University Method of quantifying HIV reservoirs by induced transcription based sequencing
CN111704648B (zh) * 2020-06-23 2022-02-15 武汉大学 以氧桥双环庚烯类化合物为雌激素受体配体的蛋白水解靶向嵌合体化合物及制备方法与应用

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US20120202861A1 (en) 2012-08-09
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US8710243B2 (en) 2014-04-29
CN102791688B (zh) 2014-11-12
EP2486010B1 (en) 2019-06-12
WO2011042473A3 (en) 2011-06-03
CN102791688A (zh) 2012-11-21
DK2486010T3 (da) 2019-09-23
JP5687704B2 (ja) 2015-03-18
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EP2486010A2 (en) 2012-08-15
IN2012DN02555A (es) 2015-08-28

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