JP2019535746A - ブルトン型チロシンキナーゼ（ｂｔｋ）阻害剤のｅ３リガーゼリガンドとのコンジュゲーションによるｂｔｋの分解および使用法 - Google Patents

ブルトン型チロシンキナーゼ（ｂｔｋ）阻害剤のｅ３リガーゼリガンドとのコンジュゲーションによるｂｔｋの分解および使用法 Download PDF

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JP2019535746A
JP2019535746A JP2019527358A JP2019527358A JP2019535746A JP 2019535746 A JP2019535746 A JP 2019535746A JP 2019527358 A JP2019527358 A JP 2019527358A JP 2019527358 A JP2019527358 A JP 2019527358A JP 2019535746 A JP2019535746 A JP 2019535746A
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alkyl
independently
linker
bifunctional compound
degron
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JP2019535746A5 (enExample
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ナサナエル エス． グレイ
ナサナエル エス． グレイ
デニス ドブロヴォルスキー
デニス ドブロヴォルスキー
ハイ−ツァン ファン
ハイ−ツァン ファン
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デイナ ファーバー キャンサー インスティチュート，インコーポレイテッド
デイナ ファーバー キャンサー インスティチュート，インコーポレイテッド
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    • A—HUMAN NECESSITIES
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    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • 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
    • A61K31/425—Thiazoles
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    • 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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    • A61K31/47—Quinolines; Isoquinolines
    • A—HUMAN NECESSITIES
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    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/4965—Non-condensed pyrazines
    • A61K31/497—Non-condensed pyrazines containing further heterocyclic rings
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    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
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    • 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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JP2019527358A 2016-11-22 2017-11-22 ブルトン型チロシンキナーゼ（ｂｔｋ）阻害剤のｅ３リガーゼリガンドとのコンジュゲーションによるｂｔｋの分解および使用法 Pending JP2019535746A (ja)

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US201662425211P 2016-11-22 2016-11-22
US62/425,211 2016-11-22
PCT/US2017/063027 WO2018098288A1 (en) 2016-11-22 2017-11-22 Degradation of bruton's tyrosine kinase (btk) by conjugation of btk inhibitors with e3 ligase ligand and methods of use

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CN110204532B (zh) * 2019-05-15 2022-03-08 浙江工业大学 一种靶向egfr蛋白降解的化合物及其制备方法和应用
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WO2021058017A1 (en) * 2019-09-29 2021-04-01 Beigene, Ltd. Degradation of androgen receptor (ar) by conjugation of ar antagonists with e3 ligase ligand and methods of use
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US20240246977A1 (en) * 2020-12-31 2024-07-25 Beigene Switzerland Gmbh Degradation of bruton's tyrosine kinase (btk) by conjugation of btk inhibitors with e3 ligase ligand and method of use
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CA3042294A1 (en) 2018-05-31
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US10925967B2 (en) 2021-02-23
US12329821B2 (en) 2025-06-17
EP3544959A1 (en) 2019-10-02
US20190262459A1 (en) 2019-08-29
AU2017363265A1 (en) 2019-05-16
US20210100908A1 (en) 2021-04-08
US11730818B2 (en) 2023-08-22
WO2018098288A1 (en) 2018-05-31
US20230338551A1 (en) 2023-10-26
AU2017363265B2 (en) 2021-11-04

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