CN112368272B - Shp2抑制剂及其用途 - Google Patents

Shp2抑制剂及其用途 Download PDF

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CN112368272B
CN112368272B CN201980031603.9A CN201980031603A CN112368272B CN 112368272 B CN112368272 B CN 112368272B CN 201980031603 A CN201980031603 A CN 201980031603A CN 112368272 B CN112368272 B CN 112368272B
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oxo
ring
amino
optionally substituted
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CN112368272A (zh
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谢益农
L·E·巴比斯
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Chengdu Xinbiao Likang Pharmaceutical Technology Co ltd
Suzhou Puhe Pharmaceutical Technology Co ltd
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    • C07D401/02Heterocyclic 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
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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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  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
CN201980031603.9A 2018-03-21 2019-03-18 Shp2抑制剂及其用途 Active CN112368272B (zh)

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US201862646107P 2018-03-21 2018-03-21
US62/646,107 2018-03-21
PCT/US2019/022717 WO2019182960A1 (en) 2018-03-21 2019-03-18 Shp2 inhibitors and uses thereof

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JP (1) JP7265275B2 (enExample)
KR (1) KR102724968B1 (enExample)
CN (1) CN112368272B (enExample)
AU (1) AU2019239658A1 (enExample)
CA (1) CA3097709A1 (enExample)
RU (1) RU2020133727A (enExample)
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Families Citing this family (72)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US11466017B2 (en) 2011-03-10 2022-10-11 Board Of Regents, The University Of Texas System Heterocyclic inhibitors of PTPN11
US10280171B2 (en) 2016-05-31 2019-05-07 Board Of Regents, The University Of Texas System Heterocyclic inhibitors of PTPN11
JP6916279B2 (ja) 2016-07-12 2021-08-11 レヴォリューション・メディスンズ,インコーポレイテッド アロステリックshp2阻害剤としての2,5−二置換3−メチルピラジンおよび2,5,6−三置換3−メチルピラジン
EP3515916B1 (en) 2016-09-22 2023-06-07 Relay Therapeutics, Inc. Shp2 phosphatase inhibitors and methods of use thereof
TW202500565A (zh) 2016-10-24 2025-01-01 美商傳達治療有限公司 Shp2磷酸酶抑制劑及其使用方法
CN110446709B (zh) 2017-01-23 2023-09-12 锐新医药公司 作为变构shp2抑制剂的二环化合物
WO2018136264A1 (en) 2017-01-23 2018-07-26 Revolution Medicines, Inc. Pyridine compounds as allosteric shp2 inhibitors
US11591336B2 (en) 2017-05-26 2023-02-28 D. E. Shaw Research, Llc Substituted pyrazolo[3,4-b]pyrazines as SHP2 phosphatase inhibitors
WO2019067843A1 (en) 2017-09-29 2019-04-04 Relay Therapeutics, Inc. PYRAZOLO [3,4-B] PYRAZINE DERIVATIVES AS INHIBITORS OF PHOSPHATASE SHP2
WO2019075265A1 (en) * 2017-10-12 2019-04-18 Revolution Medicines, Inc. PYRIDINE, PYRAZINE AND TRIAZINE COMPOUNDS AS ALLOSTERIC INHIBITORS OF SHP2
TW201927791A (zh) 2017-12-15 2019-07-16 美商銳新醫藥公司 作為變構shp2抑制劑的多環化合物
MX2020008754A (es) 2018-03-02 2020-12-07 Otsuka Pharma Co Ltd Compuestos farmaceuticos.
MX2020009782A (es) 2018-03-21 2021-01-20 Relay Therapeutics Inc Inhibidores de la fosfatasa shp2 y métodos para su uso.
WO2019183364A1 (en) 2018-03-21 2019-09-26 Relay Therapeutics, Inc. Pyrazolo[3,4-b]pyrazine shp2 phosphatase inhibitors and methods of use thereof
IL278297B2 (en) 2018-05-02 2023-12-01 Navire Pharma Inc Substituted heterocyclic inhibitors of ptpn11
EP3827009A4 (en) 2018-07-24 2022-04-27 Taiho Pharmaceutical Co., Ltd. HETEROBICYCLIC COMPOUNDS TO INHIBIT SHP2 ACTIVITY
SG11202100199UA (en) 2018-08-10 2021-02-25 Navire Pharma Inc 6-(4-amino-3-methyl-2-oxa-8-azaspiro[4.5]decan-8-yl)-3-(2,3-dichlorophenyl)-2-methylpyrimidin-4(3h)-one derivatives and related compounds as ptpn11 (shp2) inhibitors for treating cancer
WO2020061101A1 (en) 2018-09-18 2020-03-26 Nikang Therapeutics, Inc. Tri-substituted heteroaryl derivatives as src homology-2 phosphatase inhibitors
WO2020072656A1 (en) 2018-10-03 2020-04-09 Gilead Sciences, Inc. Imidozopyrimidine derivatives
TW202028183A (zh) * 2018-10-10 2020-08-01 大陸商江蘇豪森藥業集團有限公司 含氮雜芳類衍生物調節劑、其製備方法和應用
CN113365617B (zh) 2018-10-16 2025-12-23 乔治亚州立大学研究基金会股份有限公司 用于医学疾病治疗的一氧化碳前药
EP3867238B1 (en) 2018-10-17 2023-06-07 Array BioPharma Inc. Protein tyrosine phosphatase inhibitors
CN113365988B (zh) * 2019-01-31 2023-10-03 贝达药业股份有限公司 Shp2抑制剂及其应用
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
MA55511A (fr) 2019-04-02 2022-02-09 Array Biopharma Inc Inhibiteurs de protéine tyrosine phosphatase
WO2020210384A1 (en) 2019-04-08 2020-10-15 Merck Patent Gmbh Pyrimidinone derivatives as shp2 antagonists
GB201911928D0 (en) 2019-08-20 2019-10-02 Otsuka Pharma Co Ltd Pharmaceutical compounds
BR112022005349A2 (pt) 2019-09-24 2022-06-14 Relay Therapeutics Inc Inibidores de shp2 fosfatase e métodos de produção e uso dos mesmos
CN112724145A (zh) * 2019-10-14 2021-04-30 杭州雷索药业有限公司 用于抑制shp2活性的吡嗪衍生物
EP4620531A3 (en) 2019-11-08 2025-11-26 Revolution Medicines, Inc. Bicyclic heteroaryl compounds and uses thereof
WO2021115286A1 (zh) * 2019-12-10 2021-06-17 成都倍特药业股份有限公司 一种可用作shp2抑制剂的含氮杂原子的六元并五元芳环衍生物
CN113004282B (zh) * 2019-12-19 2024-05-24 首药控股(北京)股份有限公司 取代的炔基杂环化合物
CN114867720B (zh) * 2020-01-16 2024-10-22 浙江海正药业股份有限公司 杂芳基类衍生物及其制备方法和用途
WO2021147879A1 (zh) * 2020-01-21 2021-07-29 贝达药业股份有限公司 Shp2抑制剂及其应用
KR20230042600A (ko) 2020-06-18 2023-03-28 레볼루션 메디슨즈, 인크. Ras 억제제에 대한 획득된 저항성을 지연, 예방, 및 치료하는 방법
WO2021259077A1 (zh) * 2020-06-22 2021-12-30 四川科伦博泰生物医药股份有限公司 取代吡嗪类化合物,包含其的药物组合物及其用途
MX2023002248A (es) 2020-09-03 2023-05-16 Revolution Medicines Inc Uso de inhibidores de sos1 para tratar neoplasias malignas con mutaciones de shp2.
CR20230165A (es) 2020-09-15 2023-06-02 Revolution Medicines Inc Derivados indólicos como inhibidores de ras en el tratamiento del cáncer
CN115028649A (zh) * 2021-03-05 2022-09-09 四川科伦博泰生物医药股份有限公司 三并环类化合物,包含其的药物组合物及其用途
WO2022235870A1 (en) 2021-05-05 2022-11-10 Revolution Medicines, Inc. Ras inhibitors for the treatment of cancer
WO2022235822A1 (en) * 2021-05-05 2022-11-10 Huabio International, Llc Shp2 inhibitor monotherapy and uses thereof
WO2022235866A1 (en) 2021-05-05 2022-11-10 Revolution Medicines, Inc. Covalent ras inhibitors and uses thereof
WO2022235817A1 (en) 2021-05-05 2022-11-10 Huabio International, Llc Combination therapies comprising shp2 inhibitors and pd-1 inhibitors
BR112023022819A2 (pt) 2021-05-05 2024-01-16 Revolution Medicines Inc Compostos, composição farmacêutica, conjugados e métodos para tratar câncer em um sujeito, para tratar um distúrbio e para inibir uma proteína ras em uma célula
CN113248449B (zh) * 2021-05-06 2022-09-23 中国药科大学 一种含甲脒的芳基螺环类化合物及其制备方法与应用
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
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
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
CN115340545A (zh) * 2021-05-14 2022-11-15 浙江海正药业股份有限公司 双环杂芳基类衍生物及其制备方法和用途
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
EP4368625A4 (en) * 2021-07-09 2025-07-23 Kanaph Therapeutics Inc SHP2 INHIBITOR AND ITS USE
US20240374571A1 (en) 2021-09-01 2024-11-14 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
WO2023172940A1 (en) 2022-03-08 2023-09-14 Revolution Medicines, Inc. Methods for treating immune refractory lung cancer
CN120504682A (zh) 2022-06-10 2025-08-19 锐新医药公司 大环ras抑制剂
EP4573095A1 (en) 2022-08-17 2025-06-25 Treeline Biosciences, Inc. Pyridopyrimidine kras inhibitors
KR20250164828A (ko) 2023-03-30 2025-11-25 레볼루션 메디슨즈, 인크. Ras gtp 가수분해 유도를 위한 조성물 및 이의 용도
AU2024253668A1 (en) 2023-04-07 2025-11-13 Revolution Medicines, Inc. Macrocyclic ras inhibitors
AU2024243852A1 (en) 2023-04-07 2025-11-06 Revolution Medicines, Inc. Macrocyclic ras inhibitors
KR20250172857A (ko) 2023-04-14 2025-12-09 레볼루션 메디슨즈, 인크. Ras 억제제의 결정형
KR20250169290A (ko) 2023-04-14 2025-12-02 레볼루션 메디슨즈, 인크. Ras 억제제의 결정형, 이를 함유하는 조성물 및 이의 사용 방법
AU2024265078A1 (en) 2023-05-04 2025-12-11 Revolution Medicines, Inc. Combination therapy for a ras related disease or disorder
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
TW202528315A (zh) 2023-09-21 2025-07-16 美商樹線生物科學公司 螺環二氫哌喃并吡啶KRas抑制劑
US20250154171A1 (en) 2023-10-12 2025-05-15 Revolution Medicines, Inc. Ras inhibitors
WO2025081291A1 (en) * 2023-10-16 2025-04-24 Canwell Biotech Limited Benzo [c] [1, 2] oxaborol-1 (3h) -ol derivatives as shp2 inhibitors, compositions and methods thereof
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
WO2025245127A1 (en) 2024-05-21 2025-11-27 Treeline Biosciences, Inc. Spirocyclic dihydropyranopyrimidine kras inhibitors
WO2025255438A1 (en) 2024-06-07 2025-12-11 Revolution Medicines, Inc. Methods of treating a ras protein-related disease or disorder

Citations (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2004018469A1 (de) * 2002-08-22 2004-03-04 Boehringer Ingelheim Pharma Gmbh & Co. Kg Neue purinderivate, deren herstelllung und deren verwendung als arzneimittel
WO2004096806A1 (ja) * 2003-04-30 2004-11-11 Sumitomo Pharmaceuticals Co. Ltd. 縮合イミダゾール誘導体
WO2015175707A1 (en) * 2014-05-13 2015-11-19 Memorial Sloan Kettering Cancer Center Hsp70 modulators and methods for making and using the same
WO2016203405A1 (en) * 2015-06-19 2016-12-22 Novartis Ag Compounds and compositions for inhibiting the activity of shp2
WO2016203404A1 (en) * 2015-06-19 2016-12-22 Novartis Ag Compounds and compositions for inhibiting the activity of shp2

Family Cites Families (42)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JPWO2005053695A1 (ja) * 2003-12-04 2007-12-06 エーザイ・アール・アンド・ディー・マネジメント株式会社 多発性硬化症予防剤または治療剤
US7582631B2 (en) * 2004-01-14 2009-09-01 Amgen Inc. Substituted heterocyclic compounds and methods of use
ES2450566T3 (es) * 2004-11-30 2014-03-25 Amgen Inc. Análogos de quinazolina y quinolinas y su uso como medicamentos para tratar el cáncer
CN101212969B (zh) * 2005-06-07 2013-08-07 药典公司 用于抑郁和应激障碍的嗪酮和二嗪酮v3抑制剂
KR20090031913A (ko) * 2006-06-21 2009-03-30 이 아이 듀폰 디 네모아 앤드 캄파니 세포 증식 억제제로서의 피라지논
WO2008107398A2 (en) * 2007-03-02 2008-09-12 Basf Se Pyrazine compounds
WO2009049098A2 (en) 2007-10-09 2009-04-16 Indiana University Research & Technology Corporation Materials and methods for regulating the activity of phosphatases
NZ713361A (en) * 2009-08-17 2017-06-30 Memorial Sloan Kettering Cancer Center Heat shock protein binding compounds, compositions, and methods for making and using same
CN102080087B (zh) 2010-12-08 2012-05-30 厦门大学 蛋白酪氨酸磷酸酶shp2的核酸适体及其制备方法
US9522881B2 (en) 2013-04-26 2016-12-20 Indiana University Research And Technology Corporation Hydroxyindole carboxylic acid based inhibitors for oncogenic Src homology-2 domain containing protein tyrosine phosphatase-2 (SHP2)
EP3016652A4 (en) 2013-07-03 2017-03-08 Indiana University Research and Technology Corporation Shp2 inhibitors and methods of treating autoimmune and/or glomerulonephritis-associated diseases using shp2 inhibitors
AR097631A1 (es) * 2013-09-16 2016-04-06 Bayer Pharma AG Trifluorometilpirimidinonas sustituidas con heterociclos y sus usos
JP6473457B2 (ja) 2014-01-17 2019-02-20 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
JO3517B1 (ar) 2014-01-17 2020-07-05 Novartis Ag ان-ازاسبيرو الكان حلقي كبديل مركبات اريل-ان مغايرة وتركيبات لتثبيط نشاط shp2
EP3094627B1 (en) 2014-01-17 2018-08-22 Novartis AG 1-pyridazin-/triazin-3-yl-piper(-azine)/idine/pyrolidine derivatives and and compositions thereof for inhibiting the activity of shp2
SG11201609033TA (en) * 2014-05-01 2016-11-29 Celgene Quanticel Res Inc Inhibitors of lysine specific demethylase-1
CN106660987B (zh) * 2014-06-27 2020-11-06 赛尔基因昆蒂赛尔研究公司 赖氨酸特异性脱甲基酶-1的抑制剂
WO2016196591A1 (en) 2015-06-01 2016-12-08 Indiana University Research & Technology Corporation Protein tyrosine phosphatases or shp2 inhibitors and uses thereof
CN107922388B (zh) 2015-06-19 2020-12-29 诺华股份有限公司 用于抑制shp2活性的化合物和组合物
US9932288B2 (en) 2015-12-09 2018-04-03 West Virginia University Chemical compound for inhibition of SHP2 function and for use as an anti-cancer agent
WO2017156397A1 (en) * 2016-03-11 2017-09-14 Board Of Regents, The University Of Texas Sysytem Heterocyclic inhibitors of ptpn11
CN107286150B (zh) 2016-04-11 2020-07-07 中国科学院上海有机化学研究所 N-杂环类化合物、其中间体、制备方法、药物组合物和应用
HUE057838T2 (hu) 2016-06-07 2022-06-28 Jacobio Pharmaceuticals Co Ltd SHP2 inhibitorokként hasznos új heterociklusos származékok
PL3468972T3 (pl) 2016-06-14 2020-11-16 Novartis Ag Związki i kompozycje do hamowania aktywności shp2
JP6916279B2 (ja) * 2016-07-12 2021-08-11 レヴォリューション・メディスンズ,インコーポレイテッド アロステリックshp2阻害剤としての2,5−二置換3−メチルピラジンおよび2,5,6−三置換3−メチルピラジン
US10328077B2 (en) * 2016-08-10 2019-06-25 Celgene Corporation Treatment of relapsed and/or refractory solid tumors and non-hodgkin's lymphomas
EP3515916B1 (en) 2016-09-22 2023-06-07 Relay Therapeutics, Inc. Shp2 phosphatase inhibitors and methods of use thereof
TW202500565A (zh) 2016-10-24 2025-01-01 美商傳達治療有限公司 Shp2磷酸酶抑制劑及其使用方法
EP3568204B1 (en) 2017-01-10 2023-08-30 Novartis AG Pharmaceutical combination comprising an alk inhibitor and an shp2 inhibitor
WO2018136264A1 (en) 2017-01-23 2018-07-26 Revolution Medicines, Inc. Pyridine compounds as allosteric shp2 inhibitors
CN108341791B (zh) 2017-01-23 2020-09-29 中国科学院上海药物研究所 苯并噻二唑类化合物、其制备方法及用途
CN110446709B (zh) 2017-01-23 2023-09-12 锐新医药公司 作为变构shp2抑制剂的二环化合物
EP3589647A1 (en) 2017-02-28 2020-01-08 Novartis AG Shp inhibitor compositions and uses for chimeric antigen receptor therapy
SMT202400385T1 (it) 2017-03-23 2024-11-15 Jacobio Pharmaceuticals Co Ltd Nuovi derivati eterociclici utili come inibitori di shp2
US11591336B2 (en) 2017-05-26 2023-02-28 D. E. Shaw Research, Llc Substituted pyrazolo[3,4-b]pyrazines as SHP2 phosphatase inhibitors
EP3678703A1 (en) 2017-09-07 2020-07-15 Revolution Medicines, Inc. Shp2 inhibitor compositions and methods for treating cancer
WO2019067843A1 (en) 2017-09-29 2019-04-04 Relay Therapeutics, Inc. PYRAZOLO [3,4-B] PYRAZINE DERIVATIVES AS INHIBITORS OF PHOSPHATASE SHP2
WO2019075265A1 (en) 2017-10-12 2019-04-18 Revolution Medicines, Inc. PYRIDINE, PYRAZINE AND TRIAZINE COMPOUNDS AS ALLOSTERIC INHIBITORS OF SHP2
CN108113984B (zh) 2017-12-20 2021-05-07 中国科学院成都生物研究所 Shp2抑制剂在制备抗肿瘤的药物中的用途
EP3755699A1 (en) * 2018-02-21 2020-12-30 Relay Therapeutics, Inc. Shp2 phosphatase inhibitors and methods of use thereof
CN108578395B (zh) 2018-06-21 2019-10-25 厦门大学 苯丙烯酸类化合物在制备Shp2特异性抑制剂中的用途及其制药用途
CN109646441A (zh) 2019-01-25 2019-04-19 上海交通大学医学院附属仁济医院 Shp-2抑制剂在制备靶向前神经元型胶质瘤的药物中的应用

Patent Citations (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2004018469A1 (de) * 2002-08-22 2004-03-04 Boehringer Ingelheim Pharma Gmbh & Co. Kg Neue purinderivate, deren herstelllung und deren verwendung als arzneimittel
WO2004096806A1 (ja) * 2003-04-30 2004-11-11 Sumitomo Pharmaceuticals Co. Ltd. 縮合イミダゾール誘導体
WO2015175707A1 (en) * 2014-05-13 2015-11-19 Memorial Sloan Kettering Cancer Center Hsp70 modulators and methods for making and using the same
WO2016203405A1 (en) * 2015-06-19 2016-12-22 Novartis Ag Compounds and compositions for inhibiting the activity of shp2
WO2016203404A1 (en) * 2015-06-19 2016-12-22 Novartis Ag Compounds and compositions for inhibiting the activity of shp2

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