JP2022523786A - ピラジン誘導体およびｓｈｐ２の阻害の際のその適用 - Google Patents

ピラジン誘導体およびｓｈｐ２の阻害の際のその適用 Download PDF

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JP2022523786A
JP2022523786A JP2021551865A JP2021551865A JP2022523786A JP 2022523786 A JP2022523786 A JP 2022523786A JP 2021551865 A JP2021551865 A JP 2021551865A JP 2021551865 A JP2021551865 A JP 2021551865A JP 2022523786 A JP2022523786 A JP 2022523786A
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alkoxy
membered
alkyl
halogen
mmol
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JP2022523786A5 (enExample
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スン，ハイフォン
ワン，クイフォン
ジャン，タオ
マー，モンナン
リュー，ジンチャン
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スージョウ ゲンハウス ファーマシューティカル シーオー．，エルティディー
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    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • 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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    • A61K31/495—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
    • A61K31/4985—Pyrazines or piperazines ortho- or peri-condensed with heterocyclic ring systems
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JP2021551865A 2019-03-04 2020-03-02 ピラジン誘導体およびｓｈｐ２の阻害の際のその適用 Pending JP2022523786A (ja)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
CN201910160960.7 2019-03-04
CN201910160960.7A CN111647000B (zh) 2019-03-04 2019-03-04 吡嗪类衍生物及其在抑制shp2中的应用
PCT/CN2020/077391 WO2020177653A1 (zh) 2019-03-04 2020-03-02 吡嗪类衍生物及其在抑制shp2中的应用

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JP2022523786A true JP2022523786A (ja) 2022-04-26
JP2022523786A5 JP2022523786A5 (enExample) 2022-11-02

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US (3) US12338246B2 (enExample)
EP (1) EP3936502A4 (enExample)
JP (1) JP2022523786A (enExample)
KR (1) KR20210135561A (enExample)
CN (2) CN111647000B (enExample)
AU (1) AU2020233038B2 (enExample)
BR (1) BR112021017495A2 (enExample)
CA (1) CA3132395A1 (enExample)
CL (1) CL2021002308A1 (enExample)
CO (1) CO2021013140A2 (enExample)
IL (1) IL286069B2 (enExample)
MX (1) MX2021010625A (enExample)
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Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2023530838A (ja) * 2020-06-22 2023-07-20 スーチュアン・コールン－バイオテック・バイオファーマシューティカル・カンパニー・リミテッド 置換されたピラジン化合物、当該化合物を含む医薬組成物、及びその使用

Families Citing this family (59)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2020051424A1 (en) 2018-09-07 2020-03-12 Pic Therapeutics Eif4e inhibitors and uses thereof
CN112867718B (zh) 2018-09-29 2025-03-04 诺华股份有限公司 用于抑制shp2活性的化合物和组合物的制造
CN111647000B (zh) * 2019-03-04 2021-10-12 勤浩医药（苏州）有限公司 吡嗪类衍生物及其在抑制shp2中的应用
TW202146393A (zh) 2020-03-03 2021-12-16 美商皮克醫療公司 Eif4e抑制劑及其用途
IL299131A (en) 2020-06-18 2023-02-01 Revolution Medicines Inc Methods for delaying, preventing and treating acquired resistance to RAS inhibitors
US12441737B2 (en) 2020-07-08 2025-10-14 Novartis Ag Manufacture of compounds and compositions for inhibiting the activity of SHP2
WO2022006780A1 (en) * 2020-07-08 2022-01-13 Novartis Ag Manufacture of compounds and compositions for inhibiting activity of shp2
US20250195521A1 (en) 2020-09-03 2025-06-19 Revolution Medicines, Inc. Use of sos1 inhibitors to treat malignancies with shp2 mutations
CA3194067A1 (en) 2020-09-15 2022-03-24 Revolution Medicines, Inc. Ras inhibitors
CN116348466B (zh) * 2020-09-23 2025-05-30 上海齐鲁制药研究中心有限公司 吡嗪硫联苯基类化合物及其应用
JP2024516997A (ja) * 2021-05-05 2024-04-18 フヤバイオ インターナショナル，エルエルシー Ｓｈｐ２阻害剤単独療法およびその使用
TW202309052A (zh) 2021-05-05 2023-03-01 美商銳新醫藥公司 Ｒａｓ抑制劑
JP2024516450A (ja) 2021-05-05 2024-04-15 レボリューション メディシンズ インコーポレイテッド 共有結合性ｒａｓ阻害剤及びその使用
KR20240017811A (ko) 2021-05-05 2024-02-08 레볼루션 메디슨즈, 인크. 암의 치료를 위한 ras 억제제
MX2023012929A (es) * 2021-05-05 2023-11-13 Huyabio Int Llc Terapias de combinacion que comprenden inhibidores de shp2 e inhibidores de tirosina cinasa egfr.
IL308222A (en) * 2021-05-05 2024-01-01 Huyabio Int Llc Combination therapies that include SHP2 inhibitors and PD-1 inhibitors
TW202244049A (zh) * 2021-05-12 2022-11-16 大陸商藥雅科技（上海）有限公司 Shp2磷酸酶抑制劑的製備及其應用
CN115340559A (zh) * 2021-05-12 2022-11-15 药雅科技(上海)有限公司 Shp2磷酸酶杂环类抑制剂的制备及其应用
CN115340561A (zh) * 2021-05-14 2022-11-15 药雅科技(上海)有限公司 Shp2磷酸酶稠环类抑制剂的制备及其应用
AU2022274936B2 (en) * 2021-05-13 2025-08-21 Shanghai Institute Of Materia Medica, Chinese Academy Of Sciences Heterocyclic compound for inhibiting shp2 activity, preparation method therefor and use thereof
WO2022259157A1 (en) 2021-06-09 2022-12-15 Novartis Ag A triple pharmaceutical combination comprising dabrafenib, trametinib and a shp2 inhibitor
TW202317100A (zh) 2021-06-23 2023-05-01 瑞士商諾華公司 包含ｋｒａｓ ｇ１２ｃ抑制劑的藥物組合及其用於治療癌症之用途
WO2023280237A1 (zh) * 2021-07-07 2023-01-12 海创药业股份有限公司 一种磷酸酶降解剂的合成和应用
US12157732B2 (en) 2021-08-25 2024-12-03 PIC Therapeutics, Inc. eIF4E inhibitors and uses thereof
CA3229560A1 (en) 2021-08-25 2023-03-02 Christopher L. Vandeusen Eif4e inhibitors and uses thereof
KR20240055778A (ko) 2021-09-01 2024-04-29 노파르티스 아게 Tead 억제제를 포함하는 제약 조합물 및 암의 치료를 위한 이의 용도
AR127308A1 (es) 2021-10-08 2024-01-10 Revolution Medicines Inc Inhibidores ras
CN116063307B (zh) * 2021-10-29 2025-08-19 中国药科大学 Shp2与cdk4/6双靶点抑制化合物合成及其制备方法与应用
WO2023122938A1 (en) * 2021-12-28 2023-07-06 Js Innomed Holdings Ltd. Heterocyclic compounds as shp2 inhibitors, compositions comprising the heterocyclic compound, and methods of use thereof
JP2025510572A (ja) 2022-03-08 2025-04-15 レボリューション メディシンズ インコーポレイテッド 免疫不応性肺癌を治療するための方法
CN116947867B (zh) * 2022-04-18 2025-12-30 上海茂晟康慧科技有限公司 一种嘧啶-4(3h)-酮类杂环化合物的重要中间体的制备方法
WO2023240263A1 (en) 2022-06-10 2023-12-14 Revolution Medicines, Inc. Macrocyclic ras inhibitors
CN115521305B (zh) * 2022-09-20 2024-11-08 中国药科大学 Shp2&nampt双靶向化合物及其药物组合物和用途
WO2024081674A1 (en) 2022-10-11 2024-04-18 Aadi Bioscience, Inc. Combination therapies for the treatment of cancer
CN115677661B (zh) * 2022-10-27 2024-04-19 中国药科大学 杂环硫醚类化合物及其用途和药物组合物
CN118206550A (zh) * 2022-12-15 2024-06-18 江苏威凯尔医药科技有限公司 Shp2抑制剂及其应用
CN120826403A (zh) * 2023-02-24 2025-10-21 深圳真实生物医药科技有限公司 Shp2抑制剂化合物及其应用
AU2024241633A1 (en) 2023-03-30 2025-11-06 Revolution Medicines, Inc. Compositions for inducing ras gtp hydrolysis and uses thereof
AR132338A1 (es) 2023-04-07 2025-06-18 Revolution Medicines Inc Inhibidores de ras
CR20250420A (es) 2023-04-07 2025-11-20 Revolution Medicines Inc Inhibidores macrocíclicos de ras
CN121100123A (zh) 2023-04-14 2025-12-09 锐新医药公司 Ras抑制剂的结晶形式
CN121464140A (zh) 2023-04-14 2026-02-03 锐新医药公司 Ras抑制剂的结晶形式、含有其的组合物及其使用方法
TW202508595A (zh) 2023-05-04 2025-03-01 美商銳新醫藥公司 用於ｒａｓ相關疾病或病症之組合療法
WO2025011568A1 (zh) * 2023-07-11 2025-01-16 勤浩医药（苏州）有限公司 用作shp2抑制剂的杂环化合物、包含其的药物组合物及其制备方法和用途
US20250049810A1 (en) 2023-08-07 2025-02-13 Revolution Medicines, Inc. Methods of treating a ras protein-related disease or disorder
TW202529768A (zh) 2023-09-29 2025-08-01 大陸商德昇濟醫藥（無錫）有限公司 癌症治療的療法
AU2024360465A1 (en) 2023-10-12 2026-04-09 Revolution Medicines, Inc. Macrocyclic ras inhibitors
CN118108707A (zh) * 2024-02-04 2024-05-31 中国药科大学 吡嗪类化合物及其制备方法、药物组合物和应用
WO2025171296A1 (en) 2024-02-09 2025-08-14 Revolution Medicines, Inc. Ras inhibitors
TW202547461A (zh) 2024-05-17 2025-12-16 美商銳新醫藥公司 Ｒａｓ抑制劑
WO2025242126A1 (zh) * 2024-05-22 2025-11-27 上海正大天晴医药科技开发有限公司 一种药物组合及其应用
WO2025255438A1 (en) 2024-06-07 2025-12-11 Revolution Medicines, Inc. Methods of treating a ras protein-related disease or disorder
WO2025265060A1 (en) 2024-06-21 2025-12-26 Revolution Medicines, Inc. Therapeutic compositions and methods for managing treatment-related effects
WO2026015796A1 (en) 2024-07-12 2026-01-15 Revolution Medicines, Inc. Methods of treating a ras related disease or disorder
WO2026015801A1 (en) 2024-07-12 2026-01-15 Revolution Medicines, Inc. Methods of treating a ras related disease or disorder
WO2026015790A1 (en) 2024-07-12 2026-01-15 Revolution Medicines, Inc. Methods of treating a ras related disease or disorder
WO2026015825A1 (en) 2024-07-12 2026-01-15 Revolution Medicines, Inc. Use of ras inhibitor for treating pancreatic cancer
WO2026050446A1 (en) 2024-08-29 2026-03-05 Revolution Medicines, Inc. Ras inhibitors
WO2026072904A2 (en) 2024-09-26 2026-04-02 Revolution Medicines, Inc. Compositions and methods for treating lung cancer

Citations (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2017502993A (ja) * 2014-01-17 2017-01-26 ノバルティス アーゲー Ｓｈｐ２の活性を阻害するためのｎ−アザスピロシクロアルカン置換ｎ−ヘテロアリール化合物および組成物
JP2017502994A (ja) * 2014-01-17 2017-01-26 ノバルティス アーゲー Ｓｈｐ２の活性を阻害するための１−（トリアジン−３−イル／ピリダジン−３−イル）−ピペリジン／ピペラジン誘導体およびその組成物
WO2017216706A1 (en) * 2016-06-14 2017-12-21 Novartis Ag Compounds and compositions for inhibiting the activity of shp2
WO2018013597A1 (en) * 2016-07-12 2018-01-18 Revolution Medicines, Inc. 2,5-disubstituted 3-methyl pyrazines and 2,5,6-trisubstituted 3-methyl pyrazines as allosteric shp2 inhibitors
JP2018517752A (ja) * 2015-06-19 2018-07-05 ノバルティス アーゲー Ｓｈｐ２の活性を阻害するための化合物および組成物
WO2018130928A1 (en) * 2017-01-10 2018-07-19 Novartis Ag Pharmaceutical combination comprising an alk inhibitor and a shp2 inhibitor

Family Cites Families (9)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
MX388576B (es) 2016-06-07 2025-03-20 Jacobio Pharmaceuticals Co Ltd Derivados heterociclicos novedosos utiles como inhibidores de shp2.
EA202190196A1 (ru) * 2017-03-23 2021-08-31 Джакобио Фармасьютикалс Ко., Лтд. Новые гетероциклические производные, применимые в качестве ингибиторов shp2
CA3074690A1 (en) 2017-09-07 2019-03-14 Revolution Medicines, Inc. Shp2 inhibitor compositions and methods for treating cancer
TW201930292A (zh) 2017-10-12 2019-08-01 美商銳新醫藥公司 作為變構ｓｈｐ２抑制劑的吡啶、吡嗪和三嗪化合物
US11110171B2 (en) 2017-12-21 2021-09-07 New York University PD-1 related cancer therapy
WO2019152454A1 (en) 2018-01-30 2019-08-08 Research Development Foundation Shp2 inhibitors and methods of use thereof
RU2020133727A (ru) 2018-03-21 2022-04-21 Сучжоу Пухе Биофарма Ко., Лтд. Ингибиторы shp2 и их применение
MX2020010719A (es) 2018-04-10 2020-11-06 Revolution Medicines Inc Composiciones de inhibidores de shp2, metodos para tratar el cancer y metodos para identificar a un sujeto con mutaciones en shp2.
CN111647000B (zh) * 2019-03-04 2021-10-12 勤浩医药（苏州）有限公司 吡嗪类衍生物及其在抑制shp2中的应用

Patent Citations (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2017502993A (ja) * 2014-01-17 2017-01-26 ノバルティス アーゲー Ｓｈｐ２の活性を阻害するためのｎ−アザスピロシクロアルカン置換ｎ−ヘテロアリール化合物および組成物
JP2017502994A (ja) * 2014-01-17 2017-01-26 ノバルティス アーゲー Ｓｈｐ２の活性を阻害するための１−（トリアジン−３−イル／ピリダジン−３−イル）−ピペリジン／ピペラジン誘導体およびその組成物
JP2018517752A (ja) * 2015-06-19 2018-07-05 ノバルティス アーゲー Ｓｈｐ２の活性を阻害するための化合物および組成物
WO2017216706A1 (en) * 2016-06-14 2017-12-21 Novartis Ag Compounds and compositions for inhibiting the activity of shp2
WO2018013597A1 (en) * 2016-07-12 2018-01-18 Revolution Medicines, Inc. 2,5-disubstituted 3-methyl pyrazines and 2,5,6-trisubstituted 3-methyl pyrazines as allosteric shp2 inhibitors
WO2018130928A1 (en) * 2017-01-10 2018-07-19 Novartis Ag Pharmaceutical combination comprising an alk inhibitor and a shp2 inhibitor

Non-Patent Citations (1)

* Cited by examiner, † Cited by third party
Title
"RN 2170264-93-2ほか", REGISTRY（STN）[ONLINE], JPN7023004092, 11 January 2018 (2018-01-11), ISSN: 0005539516 *

Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2023530838A (ja) * 2020-06-22 2023-07-20 スーチュアン・コールン－バイオテック・バイオファーマシューティカル・カンパニー・リミテッド 置換されたピラジン化合物、当該化合物を含む医薬組成物、及びその使用

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