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 (https=
JPWO2020177653A5 (https=
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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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    • AHUMAN NECESSITIES
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    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic 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
    • A61K31/4965Non-condensed pyrazines
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    • A61K31/495Heterocyclic 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
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    • A61K31/505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
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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 (https=) 2022-11-02
JPWO2020177653A5 JPWO2020177653A5 (https=) 2022-11-02

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US (3) US12338246B2 (https=)
EP (1) EP3936502A4 (https=)
JP (1) JP2022523786A (https=)
KR (1) KR20210135561A (https=)
CN (2) CN111647000B (https=)
AU (1) AU2020233038B2 (https=)
BR (1) BR112021017495A2 (https=)
CA (1) CA3132395A1 (https=)
CL (1) CL2021002308A1 (https=)
CO (1) CO2021013140A2 (https=)
IL (1) IL286069B2 (https=)
MX (1) MX2021010625A (https=)
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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
US12030875B2 (en) 2018-09-07 2024-07-09 PIC Therapeutics, Inc. EIF4E inhibitors and uses thereof
CA3112322A1 (en) 2018-09-29 2020-04-02 Novartis Ag Manufacture of compounds and compositions for inhibiting the activity of 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
AU2021230289A1 (en) 2020-03-03 2022-09-29 PIC Therapeutics, Inc. eIF4E inhibitors and uses thereof
IL299131A (en) 2020-06-18 2023-02-01 Revolution Medicines Inc Methods for delaying, preventing and treating acquired resistance to RAS inhibitors
CN115916786B (zh) 2020-07-08 2025-10-17 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
WO2022006780A1 (en) * 2020-07-08 2022-01-13 Novartis Ag Manufacture of compounds and compositions for inhibiting activity of shp2
MX2023002248A (es) 2020-09-03 2023-05-16 Revolution Medicines Inc Uso de inhibidores de sos1 para tratar neoplasias malignas con mutaciones de shp2.
MX2023003060A (es) 2020-09-15 2023-04-05 Revolution Medicines Inc Derivados indolicos como inhibidores de ras en el tratamiento del cancer.
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
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.
AU2022268962A1 (en) 2021-05-05 2023-12-14 Revolution Medicines, Inc. Ras inhibitors for the treatment of cancer
IL308234A (en) 2021-05-05 2024-01-01 Huyabio Int Llc Monotherapy with an SHP2 inhibitor and its uses
WO2022235866A1 (en) 2021-05-05 2022-11-10 Revolution Medicines, Inc. Covalent ras inhibitors and uses thereof
CA3217393A1 (en) 2021-05-05 2022-11-10 Elena S. Koltun Ras inhibitors
CA3217084A1 (en) * 2021-05-05 2022-11-10 Farbod Shojaei Combination therapies comprising shp2 inhibitors and pd-1 inhibitors
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
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
CN114716448B (zh) * 2021-05-13 2024-01-30 中国科学院上海药物研究所 抑制shp2活性的杂环化合物、其制备方法及用途
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
CN115594666B (zh) * 2021-07-07 2024-05-31 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
JP2024534127A (ja) 2021-08-25 2024-09-18 ピク セラピューティクス, インコーポレイテッド eIF4E阻害剤及びその使用
CA3224341A1 (en) 2021-09-01 2023-03-09 Novartis Ag Pharmaceutical combinations comprising a tead inhibitor and uses thereof for the treatment of cancers
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
CN119136806A (zh) 2022-03-08 2024-12-13 锐新医药公司 用于治疗免疫难治性肺癌的方法
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
WO2024125603A1 (zh) * 2022-12-15 2024-06-20 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
EP4687905A1 (en) 2023-03-30 2026-02-11 Revolution Medicines, Inc. Compositions for inducing ras gtp hydrolysis and uses thereof
KR20260005904A (ko) 2023-04-07 2026-01-12 레볼루션 메디슨즈, 인크. 매크로사이클릭 ras 억제제
CN121263418A (zh) 2023-04-07 2026-01-02 锐新医药公司 大环ras抑制剂
AU2024252105A1 (en) 2023-04-14 2025-10-16 Revolution Medicines, Inc. Crystalline forms of ras inhibitors, compositions containing the same, and methods of use thereof
KR20250172857A (ko) 2023-04-14 2025-12-09 레볼루션 메디슨즈, 인크. Ras 억제제의 결정형
AU2024265078A1 (en) 2023-05-04 2025-12-11 Revolution Medicines, Inc. Combination therapy for a ras related disease or disorder
CN121568944A (zh) * 2023-07-11 2026-02-24 勤浩医药(苏州)股份有限公司 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
IL326136A (en) 2023-08-07 2026-03-01 Revolution Medicines Inc RMC-6291 for use in the treatment of a disease or disorder associated with the RAS protein
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
US20250154171A1 (en) 2023-10-12 2025-05-15 Revolution Medicines, Inc. 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
WO2025240847A1 (en) 2024-05-17 2025-11-20 Revolution Medicines, Inc. Ras inhibitors
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
US20250375445A1 (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
WO2026015825A1 (en) 2024-07-12 2026-01-15 Revolution Medicines, Inc. Use of ras inhibitor for treating pancreatic cancer
WO2026015790A1 (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
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
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
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
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
EA202092441A1 (ru) 2016-06-07 2021-05-21 Джакобио Фармасьютикалс Ко., Лтд. Новые гетероциклические производные, применимые в качестве ингибиторов shp2
KR20240026521A (ko) 2017-03-23 2024-02-28 자코바이오 파마슈티칼스 컴퍼니 리미티드 Shp2 억제제로서 유용한 신규한 헤테로환형 유도체
CA3074690A1 (en) 2017-09-07 2019-03-14 Revolution Medicines, Inc. Shp2 inhibitor compositions and methods for treating cancer
MX2020003579A (es) 2017-10-12 2020-07-22 Revolution Medicines Inc Compuestos de piridina, pirazina, y triazina como inhibidores de shp2 alostericos.
WO2019126736A1 (en) 2017-12-21 2019-06-27 New York University Pd-1 related cancer therapy
US11426422B2 (en) 2018-01-30 2022-08-30 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
SG11202009793TA (en) 2018-04-10 2020-10-29 Revolution Medicines Inc Shp2 inhibitor compositions, methods for treating cancer and methods for identifying a subject with shp2 mutations
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
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
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
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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