EA202091101A1 - Спироциклические соединения в качестве модуляторов фарнезоидного x-рецептора - Google Patents

Спироциклические соединения в качестве модуляторов фарнезоидного x-рецептора

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Publication number
EA202091101A1
EA202091101A1 EA202091101A EA202091101A EA202091101A1 EA 202091101 A1 EA202091101 A1 EA 202091101A1 EA 202091101 A EA202091101 A EA 202091101A EA 202091101 A EA202091101 A EA 202091101A EA 202091101 A1 EA202091101 A1 EA 202091101A1
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EA
Eurasian Patent Office
Prior art keywords
compounds
receptor
pharnesoid
modulators
fxr
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EA202091101A
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English (en)
Inventor
Джозеф Е. Карпентер
Янтинь Хуанг
Йинь Ван
Гань Ву
Original Assignee
Бристол-Маерс Сквибб Компани
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Publication of EA202091101A1 publication Critical patent/EA202091101A1/ru

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    • C07D417/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing three or more hetero rings
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    • 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
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    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/445—Non condensed piperidines, e.g. piperocaine
    • A61K31/4523—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
    • A61K31/454—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. pimozide, domperidone
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Abstract

В настоящем изобретении предложены соединения формулы (I)или их стереоизомеры, таутомеры или фармацевтически приемлемые соли или сольваты, где все переменные являются такими, как определено в настоящем документе. Эти соединения модулируют активность фарнезоидного Х-рецептора (FXR), например, в качестве агонистов. Данное изобретение также относится к фармацевтическим композициям, содержащим эти соединения, и способам лечения заболевания, расстройства или состояния, связанного с нарушением регуляции FXR, такого как патологический фиброз, отторжение трансплантата, рак, остеопороз и воспалительные расстройства, путем применения этих соединений и фармацевтических композиций.
EA202091101A 2017-11-01 2018-10-31 Спироциклические соединения в качестве модуляторов фарнезоидного x-рецептора EA202091101A1 (ru)

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US201762580068P 2017-11-01 2017-11-01
PCT/US2018/058326 WO2019089672A1 (en) 2017-11-01 2018-10-31 Spirocyclic compounds as farnesoid x receptor modulators

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JP2023504427A (ja) * 2019-11-29 2023-02-03 ▲広▼▲東▼▲東▼▲陽▼光▲薬▼▲業▼有限公司 三環式含窒素化合物の非晶質及びその用途
JP2023510274A (ja) 2020-01-15 2023-03-13 アンセルム（アンスティチュート・ナシオナル・ドゥ・ラ・サンテ・エ・ドゥ・ラ・ルシェルシュ・メディカル） Ｄ型肝炎ウイルスによる感染を処置するためのｆｘｒアゴニストの使用
CN111592557A (zh) * 2020-05-09 2020-08-28 河北合佳医药科技集团股份有限公司 一种7-氨基-3-乙烯基头孢烷酸的一步法环保制备方法
JP2024502673A (ja) 2021-01-14 2024-01-22 ウエヌイグレックオ・ファーマ Ｈｂｖ感染の処置のためのｆｘｒアゴニストとｉｆｎの相乗効果
TW202308629A (zh) 2021-04-28 2023-03-01 法商Ｅｎｙｏ製藥公司 使用fxr激動劑作為組合治療以增強tlr3激動劑之療效
KR20220153888A (ko) * 2021-05-12 2022-11-21 에이치케이이노엔 주식회사 신규한 벤조티아졸 유도체, 이의 제조방법 및 이의 간질환 예방 또는 치료 용도

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