JP6718889B2 - Shp2の活性を阻害するための化合物および組成物 - Google Patents

Shp2の活性を阻害するための化合物および組成物 Download PDF

Info

Publication number
JP6718889B2
JP6718889B2 JP2017565777A JP2017565777A JP6718889B2 JP 6718889 B2 JP6718889 B2 JP 6718889B2 JP 2017565777 A JP2017565777 A JP 2017565777A JP 2017565777 A JP2017565777 A JP 2017565777A JP 6718889 B2 JP6718889 B2 JP 6718889B2
Authority
JP
Japan
Prior art keywords
methyl
amino
hydrogen
mmol
fluoro
Prior art date
Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
Active
Application number
JP2017565777A
Other languages
English (en)
Japanese (ja)
Other versions
JP2018517752A (ja
JP2018517752A5 (enExample
Inventor
チェン,ツォリアン
ガルシア フォータネット,ジョルジ
ガルシア フォータネット,ジョルジ
ジョーク,アンドリアナ
カルキ,ラジェシュ
ジェー. ラマルシュ,マシュー
ジェー. ラマルシュ,マシュー
リウ,ギャン
ジー. パレルモ,マーク
ジー. パレルモ,マーク
ブラス ペレツ,ローレンス
ブラス ペレツ,ローレンス
ジェームス サルバー,パトリック
ジェームス サルバー,パトリック
デイビッド シュルツ,マイケル
デイビッド シュルツ,マイケル
センドツィク,マーティン
トゥーレ,ベーカリー‐バリー
ユ,ビン
Original Assignee
ノバルティス アーゲー
ノバルティス アーゲー
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by ノバルティス アーゲー, ノバルティス アーゲー filed Critical ノバルティス アーゲー
Publication of JP2018517752A publication Critical patent/JP2018517752A/ja
Publication of JP2018517752A5 publication Critical patent/JP2018517752A5/ja
Application granted granted Critical
Publication of JP6718889B2 publication Critical patent/JP6718889B2/ja
Active legal-status Critical Current
Anticipated expiration legal-status Critical

Links

Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic 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
    • C07D401/14Heterocyclic 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 three or more hetero rings
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00Drugs for skeletal disorders
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P21/00Drugs for disorders of the muscular or neuromuscular system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/28Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • A61P35/02Antineoplastic agents specific for leukemia
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic 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
    • 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
    • C07D401/04Heterocyclic 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 directly linked by a ring-member-to-ring-member bond
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D471/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/02Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/10Spiro-condensed systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D491/00Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
    • C07D491/02Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains two hetero rings
    • C07D491/10Spiro-condensed systems
    • C07D491/107Spiro-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D498/00Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D498/02Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
    • C07D498/10Spiro-condensed systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07BGENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B2200/00Indexing scheme relating to specific properties of organic compounds
    • C07B2200/07Optical isomers

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Veterinary Medicine (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Public Health (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Neurology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Biomedical Technology (AREA)
  • Neurosurgery (AREA)
  • Psychiatry (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Hospice & Palliative Care (AREA)
  • Cardiology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Hematology (AREA)
  • Oncology (AREA)
  • 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)
JP2017565777A 2015-06-19 2016-06-15 Shp2の活性を阻害するための化合物および組成物 Active JP6718889B2 (ja)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201562181893P 2015-06-19 2015-06-19
US62/181,893 2015-06-19
PCT/IB2016/053550 WO2016203406A1 (en) 2015-06-19 2016-06-15 Compounds and compositions for inhibiting the activity of shp2

Publications (3)

Publication Number Publication Date
JP2018517752A JP2018517752A (ja) 2018-07-05
JP2018517752A5 JP2018517752A5 (enExample) 2019-07-18
JP6718889B2 true JP6718889B2 (ja) 2020-07-08

Family

ID=56194530

Family Applications (1)

Application Number Title Priority Date Filing Date
JP2017565777A Active JP6718889B2 (ja) 2015-06-19 2016-06-15 Shp2の活性を阻害するための化合物および組成物

Country Status (6)

Country Link
US (1) US10287266B2 (enExample)
EP (1) EP3310774B1 (enExample)
JP (1) JP6718889B2 (enExample)
CN (2) CN107922388B (enExample)
ES (1) ES2805232T3 (enExample)
WO (1) WO2016203406A1 (enExample)

Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2021130662A (ja) * 2015-06-19 2021-09-09 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

Families Citing this family (117)

* 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
JO3517B1 (ar) 2014-01-17 2020-07-05 Novartis Ag ان-ازاسبيرو الكان حلقي كبديل مركبات اريل-ان مغايرة وتركيبات لتثبيط نشاط shp2
ES2699354T3 (es) 2014-01-17 2019-02-08 Novartis Ag Derivados de 1-(triazin-3-il/piridazin-3-il)-piper(-azin)idina y composiciones de las mismas para inhibir la actividad de 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
WO2016203406A1 (en) * 2015-06-19 2016-12-22 Novartis Ag Compounds and compositions for inhibiting the activity of shp2
ES2741746T3 (es) 2015-06-19 2020-02-12 Novartis Ag Compuestos y composiciones para inhibir la actividad de SHP2
WO2017210134A1 (en) 2016-05-31 2017-12-07 Board Of Regents, University Of Texas System Heterocyclic inhibitors of ptpn11
EA202092441A1 (ru) * 2016-06-07 2021-05-21 Джакобио Фармасьютикалс Ко., Лтд. Новые гетероциклические производные, применимые в качестве ингибиторов shp2
JP6994474B2 (ja) 2016-06-14 2022-01-14 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
CN116478131A (zh) 2016-07-12 2023-07-25 锐新医药公司 作为变构shp2抑制剂的2,5-双取代型及2,5,6-三取代型3-甲基吡嗪
WO2018057884A1 (en) 2016-09-22 2018-03-29 Relay Therapeutics, Inc. Shp2 phosphatase inhibitors and methods of use thereof
TWI848901B (zh) 2016-10-24 2024-07-21 美商傳達治療有限公司 Shp2磷酸酶抑制劑及其使用方法
CA3048340A1 (en) * 2017-01-10 2018-07-19 Novartis Ag Pharmaceutical combination comprising an alk inhibitor and a shp2 inhibitor
CN110431134A (zh) * 2017-01-23 2019-11-08 锐新医药公司 作为变构shp2抑制剂的吡啶化合物
AU2018210770B2 (en) 2017-01-23 2022-03-24 Revolution Medicines, Inc. Bicyclic compounds as allosteric SHP2 inhibitors
TWI664175B (zh) * 2017-03-23 2019-07-01 大陸商北京加科思新藥研發有限公司 用於作為shp2抑制劑之新穎雜環衍生物
WO2018218133A1 (en) 2017-05-26 2018-11-29 Relay Therapeutics, Inc. Pyrazolo[3,4-b]pyrazine derivatives as shp2 phosphatase inhibitors
TWI852912B (zh) 2017-09-07 2024-08-21 美商銳新醫藥公司 Shp2抑制劑組合物以及治療癌症的方法
TWI851542B (zh) 2017-09-11 2024-08-11 美商克魯松藥物公司 Shp2之八氫環戊烷并[c]吡咯別構抑制劑
WO2019067843A1 (en) 2017-09-29 2019-04-04 Relay Therapeutics, Inc. PYRAZOLO [3,4-B] PYRAZINE DERIVATIVES AS INHIBITORS OF PHOSPHATASE SHP2
KR20200070295A (ko) * 2017-10-12 2020-06-17 레볼루션 메디슨즈, 인크. 알로스테릭 shp2 억제제로서의 피리딘, 피라진 및 트리아진 화합물
CN111433205B (zh) 2017-12-15 2024-01-19 锐新医药公司 作为变构shp2抑制剂的多环化合物
AU2019222026B2 (en) 2018-02-13 2022-05-12 Shanghai Blueray Biopharma Co., Ltd. Pyrimidine-fused cyclic compound, preparation method therefor and application thereof
CA3092011A1 (en) 2018-03-02 2019-09-06 Otsuka Pharmaceutical Co., Ltd. Pharmaceutical compounds
WO2019183364A1 (en) 2018-03-21 2019-09-26 Relay Therapeutics, Inc. Pyrazolo[3,4-b]pyrazine shp2 phosphatase inhibitors and methods of use thereof
US10561655B2 (en) 2018-03-21 2020-02-18 Synblia Therapeutics, Inc. SHP2 inhibitors and uses thereof
EP3768668B1 (en) 2018-03-21 2024-08-28 Relay Therapeutics, Inc. Shp2 phosphatase inhibitors and methods of use thereof
EP3773590A1 (en) 2018-04-10 2021-02-17 Revolution Medicines, Inc. Shp2 inhibitor compositions, methods for treating cancer and methods for identifying a subject with shp2 mutations
CR20240382A (es) 2018-05-01 2025-08-29 Revolution Medicines Inc ANÁLOGOS DE RAPAMICINA A C40, C28 Y C32 COMO INHIBIDORES DE MTOR (Divisional 2020-578)
KR102611661B1 (ko) 2018-05-02 2023-12-08 나비레 파르마, 인코퍼레이티드 Ptpn11의 치환된 헤테로사이클릭 억제제
CN112174935B (zh) * 2018-05-09 2022-12-06 北京加科思新药研发有限公司 可用作shp2抑制剂的杂环衍生物
MA53395A (fr) 2018-07-24 2021-06-02 Otsuka Pharma Co Ltd Composés hétérobicycliques pour inhiber l'activité de shp2
IL307361B2 (en) 2018-08-10 2024-12-01 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
WO2020061103A1 (en) 2018-09-18 2020-03-26 Nikang Therapeutics, Inc. Fused tricyclic ring derivatives as src homology-2 phosphatase inhibitors
WO2020063760A1 (en) 2018-09-26 2020-04-02 Jacobio Pharmaceuticals Co., Ltd. Novel heterocyclic derivatives useful as shp2 inhibitors
AU2019346118B2 (en) * 2018-09-29 2024-05-16 Novartis Ag Manufacture of compounds and compositions for inhibiting the activity of SHP2
JP2022502385A (ja) 2018-09-29 2022-01-11 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の製造方法
EP3860717A1 (en) 2018-10-03 2021-08-11 Gilead Sciences, Inc. Imidozopyrimidine derivatives
EP3863636A1 (en) 2018-10-08 2021-08-18 Revolution Medicines, Inc. Shp2 inhibitor compositions for use in treating cancer
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
IL282179B2 (en) 2018-10-17 2024-10-01 Array Biopharma Inc Protein tyrosine phosphatase inhibitors
CN111138412B (zh) 2018-11-06 2023-09-15 上海奕拓医药科技有限责任公司 一种螺芳环化合物及其应用
CA3120791A1 (en) 2018-11-30 2020-06-04 Tuojie Biotech (Shanghai) Co., Ltd. Pyrimidine and five-membered nitrogen heterocycle derivative, preparation method therefor, and medical uses thereof
CN113164418A (zh) 2018-12-05 2021-07-23 米拉蒂治疗股份有限公司 组合疗法
CN113316574B (zh) * 2019-01-31 2024-01-30 贝达药业股份有限公司 Shp2抑制剂及其应用
WO2020156243A1 (zh) * 2019-01-31 2020-08-06 贝达药业股份有限公司 Shp2抑制剂及其应用
WO2020165732A1 (en) * 2019-02-12 2020-08-20 Novartis Ag Pharmaceutical combination comprising tno155 and a krasg12c inhibitor
KR20210146287A (ko) 2019-03-01 2021-12-03 레볼루션 메디슨즈, 인크. 이환식 헤테로아릴 화합물 및 이의 용도
SG11202109422WA (en) 2019-03-01 2021-09-29 Revolution Medicines Inc Bicyclic heterocyclyl compounds and uses thereof
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
JP7734586B2 (ja) 2019-03-07 2025-09-05 メルク パテント ゲゼルシャフト ミット ベシュレンクテル ハフツング Shp2アンタゴニストとしてのカルボキサミド-ピリミジン誘導体
CA3135555C (en) 2019-04-02 2023-09-19 Array Biopharma Inc. Protein tyrosine phosphatase inhibitors
CN113646049B (zh) * 2019-04-08 2024-08-13 默克专利有限公司 作为shp2拮抗剂的嘧啶酮衍生物
EP3772513A1 (en) * 2019-08-09 2021-02-10 C.N.C.C.S. S.c.a.r.l. Collezione Nazionale Dei Composti Chimici e Centro Screening Shp2 inhibitors
CN114787150A (zh) * 2019-08-15 2022-07-22 黑钻治疗公司 炔基喹唑啉化合物
GB201911928D0 (en) 2019-08-20 2019-10-02 Otsuka Pharma Co Ltd Pharmaceutical compounds
US20230010886A1 (en) * 2019-09-23 2023-01-12 Suzhou Puhe BioPharma Co., Ltd. Shp2 inhibitors and uses thereof
AR120082A1 (es) 2019-09-24 2022-02-02 Relay Therapeutics Inc Inhibidores de fosfatasa shp-2 y métodos para fabricarlos y usarlos
US20240139193A1 (en) 2019-10-15 2024-05-02 Amgen Inc. Combination therapy of kras inhibitor and shp2 inhibitor for treatment of cancers
WO2021091982A1 (en) 2019-11-04 2021-05-14 Revolution Medicines, Inc. Ras inhibitors
CN114901366A (zh) 2019-11-04 2022-08-12 锐新医药公司 Ras抑制剂
PH12022550988A1 (en) 2019-11-04 2023-10-09 Revolution Medicines Inc Ras inhibitors
PE20230249A1 (es) 2019-11-08 2023-02-07 Revolution Medicines Inc Compuestos de heteroarilo biciclicos y usos de estos
EP4065231A1 (en) 2019-11-27 2022-10-05 Revolution Medicines, Inc. Covalent ras inhibitors and uses thereof
WO2021142026A1 (en) 2020-01-07 2021-07-15 Revolution Medicines, Inc. Shp2 inhibitor dosing and methods of treating cancer
AU2021226205A1 (en) 2020-02-28 2022-10-20 Novartis Ag A triple pharmaceutical combination comprising dabrafenib, an Erk inhibitor and a SHP2 inhibitor
CN113493440B (zh) * 2020-04-03 2024-08-23 上海翰森生物医药科技有限公司 含氮杂芳类衍生物的盐及其晶型
TW202144334A (zh) * 2020-04-03 2021-12-01 大陸商上海翰森生物醫藥科技有限公司 含氮雜芳類衍生物游離鹼的晶型
CN113754683A (zh) 2020-06-05 2021-12-07 上海奕拓医药科技有限责任公司 同位素取代的螺芳环化合物及其应用
AU2021293228A1 (en) 2020-06-18 2023-02-09 Revolution Medicines, Inc. Methods for delaying, preventing, and treating acquired resistance to RAS inhibitors
CN115667239B (zh) * 2020-06-22 2025-11-18 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
WO2022009098A1 (en) 2020-07-08 2022-01-13 Novartis Ag Manufacture of compounds and compositions for inhibiting the activity of shp2
CN114195799B (zh) * 2020-09-02 2025-01-28 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
CN116209438A (zh) 2020-09-03 2023-06-02 锐新医药公司 使用sos1抑制剂治疗具有shp2突变的恶性疾病
JP2023541916A (ja) 2020-09-15 2023-10-04 レボリューション メディシンズ インコーポレイテッド がんの治療における、ras阻害剤としてのインドール誘導体
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
CN112062699B (zh) * 2020-11-13 2021-02-26 苏州开元民生科技股份有限公司 一种邻氨基苯硫酚的制备方法
WO2022140427A1 (en) 2020-12-22 2022-06-30 Qilu Regor Therapeutics Inc. Sos1 inhibitors and uses thereof
CN113376301B (zh) * 2020-12-25 2022-11-15 上海药坦药物研究开发有限公司 一种2-氨基-3-氯吡啶-4-硫醇钠的检测方法
MX2023011664A (es) * 2021-04-01 2023-10-11 Array Biopharma Inc Forma cristalina de un inhibidor de shp2.
CN118852330A (zh) 2021-05-05 2024-10-29 锐新医药公司 用于治疗癌症的ras抑制剂
EP4334318A4 (en) 2021-05-05 2025-03-05 Huyabio International, LLC COMBINATION THERAPIES WITH SHP2 INHIBITORS AND PD-1 INHIBITORS
WO2022235866A1 (en) 2021-05-05 2022-11-10 Revolution Medicines, Inc. Covalent ras inhibitors and uses thereof
US12390469B2 (en) 2021-05-05 2025-08-19 Huyabio International, Llc SHP2 inhibitor monotherapy and uses thereof
AU2022270116A1 (en) 2021-05-05 2023-12-21 Revolution Medicines, Inc. Ras inhibitors
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
AU2022306911A1 (en) * 2021-07-07 2024-02-22 Hinova Pharmaceuticals Inc. Synthesis and application of phosphatase degrader
WO2023031781A1 (en) 2021-09-01 2023-03-09 Novartis Ag Pharmaceutical combinations comprising a tead inhibitor and uses thereof for the treatment of cancers
CN118019537A (zh) * 2021-09-28 2024-05-10 上海翰森生物医药科技有限公司 Shp2抑制剂联合egfr-tki治疗和预防肿瘤疾病的医药用途
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
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
CN120504682A (zh) 2022-06-10 2025-08-19 锐新医药公司 大环ras抑制剂
WO2024113194A1 (en) * 2022-11-30 2024-06-06 Canwell Biotech Limited Shp2 inhibitors, compositions and methods thereof
TW202504611A (zh) 2023-03-30 2025-02-01 美商銳新醫藥公司 用於誘導ras gtp水解之組合物及其用途
AU2024253668A1 (en) 2023-04-07 2025-11-13 Revolution Medicines, Inc. Macrocyclic ras inhibitors
CR20250420A (es) 2023-04-07 2025-11-20 Revolution Medicines Inc Inhibidores macrocíclicos de ras
WO2024216048A1 (en) 2023-04-14 2024-10-17 Revolution Medicines, Inc. Crystalline forms of ras inhibitors, compositions containing the same, and methods of use thereof
WO2024216016A1 (en) 2023-04-14 2024-10-17 Revolution Medicines, Inc. Crystalline forms of a ras inhibitor
WO2024229406A1 (en) 2023-05-04 2024-11-07 Revolution Medicines, Inc. Combination therapy for a ras related disease or disorder
WO2025034702A1 (en) 2023-08-07 2025-02-13 Revolution Medicines, Inc. Rmc-6291 for use in the treatment of ras protein-related disease or disorder
WO2025034919A1 (en) 2023-08-08 2025-02-13 Quanta Therapeutics, Inc. Combination therapies with kras modulators
TW202530228A (zh) 2023-10-12 2025-08-01 美商銳新醫藥公司 Ras抑制劑
WO2025106901A1 (en) 2023-11-17 2025-05-22 Quanta Therapeutics, Inc. Combination cancer therapies with a kras modulator and an rtk-mapk pathway inhibitor
WO2025137507A1 (en) 2023-12-22 2025-06-26 Regor Pharmaceuticals, Inc. Sos1 inhibitors and uses 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
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
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
WO2026015801A1 (en) 2024-07-12 2026-01-15 Revolution Medicines, Inc. Methods of treating a ras related disease or disorder
WO2026015796A1 (en) 2024-07-12 2026-01-15 Revolution Medicines, Inc. Methods of treating a ras related disease or disorder
CN119039223B (zh) * 2024-10-31 2025-02-25 江苏豪森药业集团有限公司 一种含氮杂芳类衍生物的制备方法及其中间体
CN119798246B (zh) * 2024-12-20 2025-08-05 山东大学齐鲁医院 靶向shp2的荧光探针、制备方法及其应用

Family Cites Families (66)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CH445129A (fr) 1964-04-29 1967-10-15 Nestle Sa Procédé pour la préparation de composés d'inclusion à poids moléculaire élevé
US3459731A (en) 1966-12-16 1969-08-05 Corn Products Co Cyclodextrin polyethers and their production
US3426011A (en) 1967-02-13 1969-02-04 Corn Products Co Cyclodextrins with anionic properties
US3453257A (en) 1967-02-13 1969-07-01 Corn Products Co Cyclodextrin with cationic properties
US3453259A (en) 1967-03-22 1969-07-01 Corn Products Co Cyclodextrin polyol ethers and their oxidation products
JPS6041077B2 (ja) 1976-09-06 1985-09-13 喜徳 喜谷 1,2‐ジアミノシクロヘキサン異性体のシス白金(2)錯体
US4235871A (en) 1978-02-24 1980-11-25 Papahadjopoulos Demetrios P Method of encapsulating biologically active materials in lipid vesicles
US4261989A (en) 1979-02-19 1981-04-14 Kaken Chemical Co. Ltd. Geldanamycin derivatives and antitumor drug
FR2567518B1 (fr) 1984-07-11 1987-11-13 Sanofi Sa Nouveaux composes a noyau heterocyclique azote, leur preparation et les medicaments qui en contiennent
US4737323A (en) 1986-02-13 1988-04-12 Liposome Technology, Inc. Liposome extrusion method
EP0799617A3 (en) 1986-02-24 1997-11-12 Mitsui Petrochemical Industries, Ltd. Therapeutic agent for neurological diseases
US5266573A (en) 1989-08-07 1993-11-30 Elf Sanofi Trifluoromethylphenyltetrahydropyridines for the treatment and/or prophylaxis of intestinal motility disorders
KR0166088B1 (ko) 1990-01-23 1999-01-15 . 수용해도가 증가된 시클로덱스트린 유도체 및 이의 용도
DK169008B1 (da) 1990-06-01 1994-07-25 Holec Lk A S Fremgangsmåde og skærm til afskærmning af en strømtransformer samt strømtransformer med en sådan afskærmning
EP0647450A1 (en) 1993-09-09 1995-04-12 BEHRINGWERKE Aktiengesellschaft Improved prodrugs for enzyme mediated activation
IL115849A0 (en) 1994-11-03 1996-01-31 Merz & Co Gmbh & Co Tangential filtration preparation of liposomal drugs and liposome product thereof
WO2000059893A1 (en) 1999-04-06 2000-10-12 Krenitsky Pharmaceuticals Inc. Neurotrophic thio substituted pyrimidines
PE20010306A1 (es) 1999-07-02 2001-03-29 Agouron Pharma Compuestos de indazol y composiciones farmaceuticas que los contienen utiles para la inhibicion de proteina kinasa
GB0018891D0 (en) 2000-08-01 2000-09-20 Novartis Ag Organic compounds
JP4272338B2 (ja) 2000-09-22 2009-06-03 バイエル アクチェンゲゼルシャフト ピリジン誘導体
US6995162B2 (en) 2001-01-12 2006-02-07 Amgen Inc. Substituted alkylamine derivatives and methods of use
EP1438053B1 (de) 2001-10-17 2008-09-10 Boehringer Ingelheim Pharma GmbH & Co.KG Pyrimidinderivate, arzneimittel enthaltend diese verbindungen, deren verwendung und verfahren zu ihrer herstellung
CN100522967C (zh) 2002-02-01 2009-08-05 阿里亚德基因治疗公司 含磷化合物及其应用
DK1482924T3 (da) 2002-03-05 2008-09-29 Merck Frosst Canada Ltd Cathepsin-cystein-protease-inhibotorer
TWI275390B (en) 2002-04-30 2007-03-11 Wyeth Corp Process for the preparation of 7-substituted-3- quinolinecarbonitriles
CA2517422A1 (en) 2003-03-07 2004-09-16 Merck Sharp & Dohme Limited Tetrahydropyran compounds as tachykinin antagonists
US7399865B2 (en) 2003-09-15 2008-07-15 Wyeth Protein tyrosine kinase enzyme inhibitors
CN1938296A (zh) 2004-04-01 2007-03-28 安斯泰来制药有限公司 作为腺苷拮抗剂的吡嗪衍生物及其制药用途
CA2563699C (en) 2004-04-23 2014-03-25 Exelixis, Inc. Kinase modulators and method of use
KR20200019263A (ko) 2004-09-02 2020-02-21 제넨테크, 인크. 헤지호그 신호전달에 대한 피리딜 억제제
GB0510390D0 (en) 2005-05-20 2005-06-29 Novartis Ag Organic compounds
EP1928862A1 (en) 2005-09-13 2008-06-11 Palau Pharma, S.A. 2-aminopyrimidine derivatives as modulators of the histamine h4 receptor activity
US7515405B2 (en) 2006-07-25 2009-04-07 Hewlett-Packard Development Company, L.P. Anti-rotation mechanism for an electronic device
US20090137549A1 (en) 2006-11-09 2009-05-28 Paul John Edward Novel compounds useful for the treatment of degenerative & inflamatory diseases
JP2010518083A (ja) 2007-02-12 2010-05-27 メルク・シャープ・エンド・ドーム・コーポレイション ピペリジン誘導体
AR065718A1 (es) 2007-03-15 2009-06-24 Novartis Ag Compuestos heterociclicos nitrogenados,utiles en el diagnostico y tratamiento de trastornos hiperproliferativos.
BRPI0816769A2 (pt) 2007-09-12 2016-11-29 Hoffmann La Roche combinações de compostos inibidores de fosfoinositida 3-cinase e agentes quimioterapêuticos, e métodos de uso
ES2439705T3 (es) 2007-10-25 2014-01-24 Genentech, Inc. Proceso para la preparación de compuestos de tienopirimidina
AU2009238590A1 (en) 2008-04-22 2009-10-29 Portola Pharmaceuticals, Inc. Inhibitors of protein kinases
EA201100136A1 (ru) 2008-06-13 2011-08-30 Новартис Аг 2,4'-бипиридинилы в качестве ингибиторов протеинкиназы d, применимые для лечения сердечной недостаточности и рака
US8168784B2 (en) 2008-06-20 2012-05-01 Abbott Laboratories Processes to make apoptosis promoters
KR20110026481A (ko) 2008-06-20 2011-03-15 메타볼렉스, 인코포레이티드 아릴 gpr119 작동약 및 이의 용도
TWI458721B (zh) 2008-06-27 2014-11-01 Celgene Avilomics Res Inc 雜芳基化合物及其用途
WO2010048149A2 (en) 2008-10-20 2010-04-29 Kalypsys, Inc. Heterocyclic modulators of gpr119 for treatment of disease
JP2012511567A (ja) 2008-12-10 2012-05-24 ドン ファ ファーム カンパニー リミテッド 新規の2,6−置換−3−ニトロピリジン誘導体、その製造方法及びこれを含む薬学組成物
FR2941696B1 (fr) 2009-02-05 2011-04-15 Sanofi Aventis Derives d'azaspiranyl-alkylcarbamates d'heterocycles a 5 chainons, leur preparation et leur application en therapeutique
WO2010121212A2 (en) * 2009-04-17 2010-10-21 H. Lee Moffit Cancer Center And Research Institute, Inc. Indoline scaffold shp-2 inhibitors and method of treating cancer
WO2011078143A1 (ja) 2009-12-22 2011-06-30 塩野義製薬株式会社 ピリミジン誘導体およびそれらを含有する医薬組成物
SG186877A1 (en) 2010-06-30 2013-02-28 Fujifilm Corp Novel nicotinamide derivatives or salts thereof
JP2013531037A (ja) 2010-07-13 2013-08-01 メルク・シャープ・エンド・ドーム・コーポレイション スピロ環式化合物
SG186850A1 (en) 2010-07-29 2013-02-28 Rigel Pharmaceuticals Inc Ampk-activating heterocyclic compounds and methods for using the same
US8609672B2 (en) 2010-08-27 2013-12-17 University Of The Pacific Piperazinylpyrimidine analogues as protein kinase inhibitors
JP5802756B2 (ja) 2010-10-20 2015-11-04 ファイザー・インク スムーズンド受容体モジュレーターとしてのピリジン−2−誘導体
HRP20171655T1 (hr) 2011-09-12 2017-12-15 Merck Patent Gmbh Derivati aminopirimidina za upotrebu kao modulatori aktivnosti kinaze
WO2013096093A1 (en) 2011-12-21 2013-06-27 Merck Sharp & Dohme Corp. Compounds as dgat-1 inhibitors
BR112014030410A2 (pt) 2012-06-07 2017-06-27 Hoffmann La Roche inibidores de pirazolopirimidona e pirazolopiridona de tanquirase
EP2903985A1 (en) 2012-10-03 2015-08-12 Advinus Therapeutics Limited Spirocyclic compounds, compositions and medicinal applications thereof
WO2014160521A1 (en) 2013-03-15 2014-10-02 Blueprint Medicines Corporation Piperazine derivatives and their use as kit modulators
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
JO3517B1 (ar) * 2014-01-17 2020-07-05 Novartis Ag ان-ازاسبيرو الكان حلقي كبديل مركبات اريل-ان مغايرة وتركيبات لتثبيط نشاط shp2
ES2699354T3 (es) * 2014-01-17 2019-02-08 Novartis Ag Derivados de 1-(triazin-3-il/piridazin-3-il)-piper(-azin)idina y composiciones de las mismas para inhibir la actividad de SHP2
EA036672B8 (ru) 2014-05-01 2021-01-13 Селджен Квонтисел Рисёрч, Инк. Ингибиторы лизин-специфической деметилазы-1
US10174032B2 (en) 2014-05-05 2019-01-08 Signalrx Pharmaceuticals, Inc. Heterocyclic compound classes for signaling modulation
US10308660B2 (en) 2015-06-19 2019-06-04 Novartis Ag Compounds and compositions for inhibiting the activity of SHP2
ES2741746T3 (es) 2015-06-19 2020-02-12 Novartis Ag Compuestos y composiciones para inhibir la actividad de SHP2
WO2016203406A1 (en) * 2015-06-19 2016-12-22 Novartis Ag Compounds and compositions for inhibiting the activity of shp2

Cited By (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2021130662A (ja) * 2015-06-19 2021-09-09 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
JP7146016B2 (ja) 2015-06-19 2022-10-03 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

Also Published As

Publication number Publication date
US20180186770A1 (en) 2018-07-05
JP2018517752A (ja) 2018-07-05
EP3310774A1 (en) 2018-04-25
EP3310774B1 (en) 2020-04-29
US10287266B2 (en) 2019-05-14
WO2016203406A1 (en) 2016-12-22
ES2805232T3 (es) 2021-02-11
CN107922388B (zh) 2020-12-29
CN112625028B (zh) 2024-10-29
CN107922388A (zh) 2018-04-17
CN112625028A (zh) 2021-04-09

Similar Documents

Publication Publication Date Title
JP7146016B2 (ja) Shp2の活性を阻害するための化合物および組成物
JP6718889B2 (ja) Shp2の活性を阻害するための化合物および組成物
JP7278359B2 (ja) Shp2の活性を阻害するための化合物および組成物
JP6523303B2 (ja) Shp2の活性を阻害するための1−ピリダジン/トリアジン−3−イル−ピペラジン/ピペリジン/ピロリジン誘導体およびその組成物
JP6473457B2 (ja) 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
JP6534389B2 (ja) 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
BR112018075663B1 (pt) Compostos para inibição da atividade de shp2, seu uso, e composição farmacêutica

Legal Events

Date Code Title Description
A521 Request for written amendment filed

Free format text: JAPANESE INTERMEDIATE CODE: A523

Effective date: 20190613

A621 Written request for application examination

Free format text: JAPANESE INTERMEDIATE CODE: A621

Effective date: 20190613

A977 Report on retrieval

Free format text: JAPANESE INTERMEDIATE CODE: A971007

Effective date: 20200423

TRDD Decision of grant or rejection written
A01 Written decision to grant a patent or to grant a registration (utility model)

Free format text: JAPANESE INTERMEDIATE CODE: A01

Effective date: 20200519

A61 First payment of annual fees (during grant procedure)

Free format text: JAPANESE INTERMEDIATE CODE: A61

Effective date: 20200615

R150 Certificate of patent or registration of utility model

Ref document number: 6718889

Country of ref document: JP

Free format text: JAPANESE INTERMEDIATE CODE: R150

R250 Receipt of annual fees

Free format text: JAPANESE INTERMEDIATE CODE: R250

R250 Receipt of annual fees

Free format text: JAPANESE INTERMEDIATE CODE: R250

R250 Receipt of annual fees

Free format text: JAPANESE INTERMEDIATE CODE: R250