JP2022507506A - Ｎｌｒｐ活性に関連する状態を治療するための化合物及び組成物 - Google Patents

Ｎｌｒｐ活性に関連する状態を治療するための化合物及び組成物 Download PDF

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JP2022507506A
JP2022507506A JP2021526492A JP2021526492A JP2022507506A JP 2022507506 A JP2022507506 A JP 2022507506A JP 2021526492 A JP2021526492 A JP 2021526492A JP 2021526492 A JP2021526492 A JP 2021526492A JP 2022507506 A JP2022507506 A JP 2022507506A
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alkyl
aryl
membered
alkoxy
cycloalkyl
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JP2022507506A5 (https=
JPWO2020102576A5 (https=
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フランキ，ルイージ
ゴーシュ，ショミアー
グリック，ギャリー
カッツ，ジェイソン
オピパリ，アンソニー，ウィリアム，ジュニア
ルーシュ，ウィリアム
ザイデル，ハンス，マーティン
シェン，ドン－ミン
ヴェンカトラマン，シャンカー
ウィンクラー，デイビッド，グウェンザー
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ノバルティス アーゲー
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    • A61K31/445—Non condensed piperidines, e.g. piperocaine
    • A61K31/451—Non condensed piperidines, e.g. piperocaine having a carbocyclic group directly attached to the heterocyclic ring, e.g. glutethimide, meperidine, loperamide, phencyclidine, piminodine
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    • C07D317/48—Methylenedioxybenzenes or hydrogenated methylenedioxybenzenes, unsubstituted on the hetero ring
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Publication number Priority date Publication date Assignee Title
CA3105521A1 (en) 2018-07-20 2020-01-23 F. Hoffmann-La Roche Ag Sulfonimidamide compounds as inhibitors of interleukin-1 activity
PH12022551767A1 (en) * 2020-01-22 2023-11-29 Hoffmann La Roche Sulfonimidamide compounds as nlrp3 modulators
EP3984535A1 (en) * 2020-10-16 2022-04-20 Albert-Ludwigs-Universität Freiburg Nlrp3 activators for use in the treatment of infectious diseases or cancer by activating nlrp3 inflammasome
CN114539256B (zh) * 2020-11-20 2024-02-02 上海拓界生物医药科技有限公司 三环化合物及其医药用途
CN117279903A (zh) * 2021-02-10 2023-12-22 杭州英创医药科技有限公司 作为nlrp3抑制剂的化合物
US11932630B2 (en) 2021-04-16 2024-03-19 Novartis Ag Heteroaryl aminopropanol derivatives
CN118302415A (zh) * 2021-12-03 2024-07-05 辰欣药业股份有限公司 二甲基亚磺酰亚胺衍生物的制备方法
CN116804018A (zh) * 2022-03-25 2023-09-26 成都百裕制药股份有限公司 酰胺衍生物及其制备方法和在医药上的应用
CN114989058B (zh) * 2022-06-02 2024-04-16 中国科学院成都生物研究所 一种手性氯代砜亚胺类化合物及其衍生物的制备方法
EP4561574A1 (en) * 2022-07-27 2025-06-04 Novartis AG Dosing regimen for a nlrp3 inhibitor
CN115961298B (zh) * 2022-12-31 2024-10-01 广西师范大学 一种电化学介导乙烯基苯胺与醇合成2，3-二烷氧基取代吲哚啉化合物、合成方法及应用
TW202502747A (zh) * 2023-03-17 2025-01-16 美商凡特斯治療美國公司 用於抑制ｎｌｒｐ３之醯胺衍生物及其用途
WO2025153532A1 (en) 2024-01-16 2025-07-24 NodThera Limited Nlrp3 inhibitors and glp-1 agonists combination therapies

Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2017129897A1 (fr) * 2016-01-25 2017-08-03 Galderma Research & Development Inhibiteurs nlrp3 pour le traitement des pathologies cutanées inflammatoires
JP2018510207A (ja) * 2015-02-16 2018-04-12 ザ ユニバーシティ オブ クィーンズランド スルホニル尿素及び関連化合物並びにその使用
JP2021532101A (ja) * 2018-07-20 2021-11-25 エフ.ホフマン−ラ ロシュ アーゲーF. Hoffmann−La Roche Aktiengesellschaft インターロイキン−１活性の阻害剤としてのスルホンイミドアミド化合物

Family Cites Families (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2018225018A1 (en) * 2017-06-09 2018-12-13 Cadila Healthcare Limited Novel substituted sulfoximine compounds
ES2988798T3 (es) * 2017-07-24 2024-11-21 Novartis Ag Compuestos y composiciones para el tratamiento de afecciones asociadas a la actividad de NLRP
EP3692020A1 (en) * 2017-10-03 2020-08-12 Inflazome Limited Novel compounds

Patent Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2018510207A (ja) * 2015-02-16 2018-04-12 ザ ユニバーシティ オブ クィーンズランド スルホニル尿素及び関連化合物並びにその使用
WO2017129897A1 (fr) * 2016-01-25 2017-08-03 Galderma Research & Development Inhibiteurs nlrp3 pour le traitement des pathologies cutanées inflammatoires
JP2021532101A (ja) * 2018-07-20 2021-11-25 エフ.ホフマン−ラ ロシュ アーゲーF. Hoffmann−La Roche Aktiengesellschaft インターロイキン−１活性の阻害剤としてのスルホンイミドアミド化合物

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