EA202090255A3 - 6,7-дигидро-5h-бензо[7]аннуленовые производные в качестве модуляторов эстрогеновых рецепторов - Google Patents

6,7-дигидро-5h-бензо[7]аннуленовые производные в качестве модуляторов эстрогеновых рецепторов

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EA202090255A3
EA202090255A3 EA202090255A EA202090255A EA202090255A3 EA 202090255 A3 EA202090255 A3 EA 202090255A3 EA 202090255 A EA202090255 A EA 202090255A EA 202090255 A EA202090255 A EA 202090255A EA 202090255 A3 EA202090255 A3 EA 202090255A3
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group
hydrogen atom
estrogen receptors
benzo
modulators
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EA202090255A
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EA202090255A2 (ru
EA038639B1 (ru
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Монсиф Буабула
Морис Бролло
Виктор Серталь
Юссеф Эль-Амад
Брюно Филош-Ромме
Франк Алле
Гари Маккорт
Лоран Шио
Мишель Табар
Коринн Террье
Фабьенн Томсон
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Санофи
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Publication of EA202090255A2 publication Critical patent/EA202090255A2/ru
Publication of EA202090255A3 publication Critical patent/EA202090255A3/ru
Publication of EA038639B1 publication Critical patent/EA038639B1/ru

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Abstract

Изобретение относится к соединениям формулы (I)где R1 и R2 представляют собой атомы водорода или дейтерия; R3 представляет собой атом водорода или -COOH-, -OH- или OPO(OH)-группу; R4 представляет собой атом водорода или атом фтора; R5 представляет собой атом водорода или -OH-группу; где по меньшей мере один из R3 или R5 является отличным от атома водорода; при этом если R3 представляет собой -COOH-, -OH- или -OPO(OH)-группу, то R5 представляет собой атом водорода; если R5 представляет собой -OH-группу, то R3 и R4 представляют собой атомы водорода; и R6 выбран из необязательно замещенной фенильной, гетероарильной, циклоалкильной или гетероциклоалкильной группы. Настоящее изобретение также относится к получению и вариантам терапевтического применения соединений формулы (I) в качестве ингибиторов и средств разрушения эстрогеновых рецепторов, применимых, в частности, в лечении рака.
EA202090255A 2016-02-15 2017-02-14 6,7-дигидро-5h-бензо[7]аннуленовые производные в качестве модуляторов эстрогеновых рецепторов EA038639B1 (ru)

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EA202090255A2 EA202090255A2 (ru) 2020-05-31
EA202090255A3 true EA202090255A3 (ru) 2020-07-31
EA038639B1 EA038639B1 (ru) 2021-09-28

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EA202090255A EA038639B1 (ru) 2016-02-15 2017-02-14 6,7-дигидро-5h-бензо[7]аннуленовые производные в качестве модуляторов эстрогеновых рецепторов
EA201891841A EA034994B1 (ru) 2016-02-15 2017-02-14 6,7-дигидро-5h-бензо[7]аннуленовые производные в качестве модуляторов эстрогеновых рецепторов

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EP3434272A1 (en) * 2017-07-25 2019-01-30 Sanofi Combination comprising palbociclib and 6-(2,4-dichlorophenyl)-5-[4-[(3s)-1-(3-fluoropropyl)pyrrolidin-3-yl]oxyphenyl]-8,9-dihydro-7h-benzo[7]annulene-2-carboxylic acid
WO2019157020A1 (en) * 2018-02-06 2019-08-15 The Board Of Trustees Of The University Of Illinois Substituted benzothiophene analogs as selective estrogen receptor degraders
CA3109090A1 (en) 2018-08-17 2020-02-20 F. Hoffmann-La Roche Ag Diagnostic and therapeutic methods for the treatment of breast cancer
ES2923412T3 (es) 2018-09-07 2022-09-27 Sanofi Sa Sales de 6-(2,4-diclorofenil)-5-[4-[(3S)-1-(3-fluoropropil)pirrolidin-3-il]oxifenil]-8,9-dihidro-7H-benzo[7]anuleno-2-carboxilato de metilo y proceso de preparación de las mismas
EP3699167A1 (en) 2019-02-22 2020-08-26 Sanofi Process for preparing methyl 1-benzosuberone-7-carboxylate
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