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

  • Organic Chemistry (AREA)
  • Chemical & Material Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Animal Behavior & Ethology (AREA)
  • Medicinal Chemistry (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Neurology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Biomedical Technology (AREA)
  • Neurosurgery (AREA)
  • Oncology (AREA)
  • Hospice & Palliative Care (AREA)
  • Psychiatry (AREA)
  • Hematology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (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) CN112625028B (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 (109)

* 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
WO2015107493A1 (en) 2014-01-17 2015-07-23 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
CN112625028B (zh) * 2015-06-19 2024-10-29 诺华股份有限公司 用于抑制shp2活性的化合物和组合物
WO2016203404A1 (en) 2015-06-19 2016-12-22 Novartis Ag Compounds and compositions for inhibiting the activity of shp2
WO2017210134A1 (en) 2016-05-31 2017-12-07 Board Of Regents, University Of Texas System Heterocyclic inhibitors of ptpn11
CN109311848B (zh) * 2016-06-07 2022-02-01 北京加科思新药研发有限公司 可用作shp2抑制剂的新型杂环衍生物
RU2744988C2 (ru) 2016-06-14 2021-03-17 Новартис Аг Соединения и композиции для подавления активности shp2
AU2017296289A1 (en) 2016-07-12 2019-01-31 Revolution Medicines, Inc. 2,5-disubstituted 3-methyl pyrazines and 2,5,6-trisubstituted 3-methyl pyrazines as allosteric SHP2 inhibitors
EP3515916B1 (en) 2016-09-22 2023-06-07 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
JP7240319B2 (ja) 2017-01-23 2023-03-15 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阻害剤としての二環式化合物
SMT202400385T1 (it) * 2017-03-23 2024-11-15 Jacobio Pharmaceuticals Co Ltd Nuovi derivati eterociclici utili come inibitori di shp2
EP3630770B1 (en) 2017-05-26 2024-08-28 Relay Therapeutics, Inc. Pyrazolo[3,4-b]pyrazine derivatives as shp2 phosphatase inhibitors
KR20200051684A (ko) 2017-09-07 2020-05-13 레볼루션 메디슨즈, 인크. 암 치료를 위한 shp2 억제제 조성물 및 방법
US10435389B2 (en) 2017-09-11 2019-10-08 Krouzon Pharmaccuticals, Inc. Octahydrocyclopenta[c]pyrrole allosteric inhibitors of SHP2
EP3687997A1 (en) 2017-09-29 2020-08-05 Relay Therapeutics, Inc. Pyrazolo[3,4-b]pyrazine derivatives as shp2 phosphatase inhibitors
EP3694848A1 (en) * 2017-10-12 2020-08-19 Revolution Medicines, Inc. Pyridine, pyrazine, and triazine compounds as allosteric shp2 inhibitors
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
JP7335882B2 (ja) 2018-02-13 2023-08-30 ブルーレイ セラピューティクス (シャンハイ) カンパニー,リミティド ピリミジン縮合環式化合物及びその製造方法、並びに使用
MX2020008754A (es) 2018-03-02 2020-12-07 Otsuka Pharma Co Ltd Compuestos farmaceuticos.
AU2019239658A1 (en) 2018-03-21 2020-11-12 Suzhou Puhe BioPharma Co., Ltd. SHP2 inhibitors and uses thereof
WO2019183364A1 (en) 2018-03-21 2019-09-26 Relay Therapeutics, Inc. Pyrazolo[3,4-b]pyrazine shp2 phosphatase inhibitors and methods of use thereof
US20220315586A1 (en) 2018-03-21 2022-10-06 Relay Therapeutics, Inc. Shp2 phosphatase inhibitors and methods of use thereof
KR20200143417A (ko) 2018-04-10 2020-12-23 레볼루션 메디슨즈, 인크. Shp2 억제제 조성물, 암을 치료하는 방법 및 shp2 돌연변이를 갖는 대상체를 확인하는 방법
US20190336609A1 (en) 2018-05-01 2019-11-07 Revolution Medicines, Inc. C40-, C28-, and C-32-Linked Rapamycin Analogs as mTOR Inhibitors
US10954243B2 (en) 2018-05-02 2021-03-23 Navire Pharma, Inc. Substituted heterocyclic inhibitors of PTPN11
CN115721648A (zh) * 2018-05-09 2023-03-03 北京加科思新药研发有限公司 可用作shp2抑制剂的新型杂环衍生物
MX2021000795A (es) 2018-07-24 2021-04-12 Taiho Pharmaceutical Co Ltd Compuestos heterociclicos para inhibir la actividad de shp2.
EP3833670B1 (en) 2018-08-10 2024-04-17 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
US20210393623A1 (en) 2018-09-26 2021-12-23 Jacobio Pharmaceuticals Co., Ltd. Novel Heterocyclic Derivatives Useful as SHP2 Inhibitors
WO2020065452A1 (en) * 2018-09-29 2020-04-02 Novartis Ag Manufacture of compounds and compositions for inhibiting the activity of shp2
MX2021003459A (es) 2018-09-29 2021-06-18 Novartis Ag Proceso de fabricacion de un compuesto para la inhibicion de la actividad de shp2.
EP3860717A1 (en) 2018-10-03 2021-08-11 Gilead Sciences, Inc. Imidozopyrimidine derivatives
WO2020076723A1 (en) 2018-10-08 2020-04-16 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
EP3867238B1 (en) 2018-10-17 2023-06-07 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
WO2020108590A1 (zh) 2018-11-30 2020-06-04 上海拓界生物医药科技有限公司 嘧啶并五元氮杂环类衍生物、其制备方法及其在医药上的应用
WO2020118066A1 (en) 2018-12-05 2020-06-11 Mirati Therapeutics, Inc. Combination therapies
WO2020156242A1 (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
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
CN113382774A (zh) * 2019-02-12 2021-09-10 诺华股份有限公司 包含tno155和krasg12c抑制剂的药物组合
US20230096028A1 (en) 2019-03-01 2023-03-30 Revolution Medicines, Inc. Bicyclic heterocyclyl compounds and uses thereof
US20230148450A9 (en) 2019-03-01 2023-05-11 Revolution Medicines, Inc. Bicyclic heteroaryl 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
US11033547B2 (en) 2019-03-07 2021-06-15 Merck Patent Gmbh Carboxamide-pyrimidine derivatives as SHP2 antagonists
PH12021552227A1 (en) * 2019-04-02 2022-05-30 Array Biopharma Inc Protein tyrosine phosphatase inhibitors
AU2020271838A1 (en) 2019-04-08 2021-08-19 Merck Patent Gmbh Pyrimidinone derivatives as SHP2 antagonists
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
US12435046B2 (en) 2019-08-15 2025-10-07 Black Diamond Therapeutics, Inc. Alkynyl quinazoline compounds
GB201911928D0 (en) 2019-08-20 2019-10-02 Otsuka Pharma Co Ltd Pharmaceutical compounds
WO2021061515A1 (en) * 2019-09-23 2021-04-01 Synblia Therapeutics, Inc. Shp2 inhibitors and uses thereof
CA3154862A1 (en) 2019-09-24 2021-04-01 Relay Therapeutics, Inc. Shp2 phosphatase inhibitors and methods of making and using the same
WO2021076655A1 (en) 2019-10-15 2021-04-22 Amgen Inc. Combination therapy of kras inhibitor and shp2 inhibitor for treatment of cancers
WO2021091967A1 (en) 2019-11-04 2021-05-14 Revolution Medicines, Inc. Ras inhibitors
CN115894606A (zh) 2019-11-04 2023-04-04 锐新医药公司 Ras抑制剂
CA3160142A1 (en) 2019-11-04 2021-05-14 Revolution Medicines, Inc. Ras inhibitors
KR20220100903A (ko) 2019-11-08 2022-07-18 레볼루션 메디슨즈, 인크. 이환식 헤테로아릴 화합물 및 이의 용도
EP4065231A1 (en) 2019-11-27 2022-10-05 Revolution Medicines, Inc. Covalent ras inhibitors and uses thereof
MX2022008305A (es) 2020-01-07 2022-08-08 Revolution Medicines Inc Dosificacion de inhibidores de shp2 y metodos de tratamiento del cancer.
KR20220148847A (ko) 2020-02-28 2022-11-07 노파르티스 아게 다브라페닙, erk 억제제, 및 shp2 억제제를 포함하는 삼중 약학적 조합물
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
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
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
JP2023530351A (ja) 2020-06-18 2023-07-14 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 Ras阻害剤への獲得耐性を遅延させる、防止する、及び、治療する方法
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
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
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
KR20230081726A (ko) 2020-09-03 2023-06-07 레볼루션 메디슨즈, 인크. Shp2 돌연변이가 있는 악성 종양을 치료하기 위한 sos1 억제제의 용도
KR20230067635A (ko) 2020-09-15 2023-05-16 레볼루션 메디슨즈, 인크. 암의 치료에서 ras 억제제로서 인돌 유도체
WO2022063190A1 (zh) * 2020-09-23 2022-03-31 南京明德新药研发有限公司 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
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
EP4333850A4 (en) 2021-05-05 2025-04-09 Huyabio International, LLC SHP2 INHIBITOR MONOTHERAPY AND ITS USES
WO2022235817A1 (en) 2021-05-05 2022-11-10 Huabio International, Llc Combination therapies comprising shp2 inhibitors and pd-1 inhibitors
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
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
EP4395769A1 (en) 2021-09-01 2024-07-10 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
AU2023285116A1 (en) 2022-06-10 2024-12-19 Revolution Medicines, Inc. Macrocyclic ras inhibitors
WO2024113194A1 (en) * 2022-11-30 2024-06-06 Canwell Biotech Limited Shp2 inhibitors, compositions and methods thereof
AU2024241633A1 (en) 2023-03-30 2025-11-06 Revolution Medicines, Inc. Compositions for inducing ras gtp hydrolysis and uses thereof
WO2024211712A1 (en) 2023-04-07 2024-10-10 Revolution Medicines, Inc. Condensed macrocyclic compounds as ras inhibitors
WO2024211663A1 (en) 2023-04-07 2024-10-10 Revolution Medicines, Inc. Condensed macrocyclic compounds as ras inhibitors
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
TW202446388A (zh) 2023-04-14 2024-12-01 美商銳新醫藥公司 Ras抑制劑之結晶形式、含有其之組合物及其使用方法
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
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
WO2025080946A2 (en) 2023-10-12 2025-04-17 Revolution Medicines, Inc. Ras inhibitors
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
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
US3453257A (en) 1967-02-13 1969-07-01 Corn Products Co Cyclodextrin with cationic properties
US3426011A (en) 1967-02-13 1969-02-04 Corn Products Co Cyclodextrins with anionic 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
US4959368A (en) 1986-02-24 1990-09-25 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
CA2369945A1 (en) 1999-04-06 2000-10-12 James L. Kelley 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
EP2090571B1 (de) 2001-10-17 2012-05-16 Boehringer Ingelheim Pharma GmbH & Co. KG Pyrimidinderivate, Arzneimittel enthaltend diese Verbindungen, deren Verwendung und Verfahren zu ihrer Herstellung
ES2485841T3 (es) 2002-02-01 2014-08-14 Ariad Pharmaceuticals, Inc Compuestos que contienen fósforo y usos de los mismos
HRP20040800B1 (en) 2002-03-05 2012-11-30 Merck Frosst Canada & Co Axys Cathepsin cysteine protease inhibitors
TWI275390B (en) 2002-04-30 2007-03-11 Wyeth Corp Process for the preparation of 7-substituted-3- quinolinecarbonitriles
WO2004078750A1 (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
JP4978192B2 (ja) 2004-04-01 2012-07-18 アステラス製薬株式会社 ピラジン誘導体およびその医薬的使用
AU2005249380C1 (en) 2004-04-23 2012-09-20 Exelixis, Inc. Kinase modulators and methods of use
KR20150002863A (ko) 2004-09-02 2015-01-07 제넨테크, 인크. 헤지호그 신호전달에 대한 피리딜 억제제
GB0510390D0 (en) 2005-05-20 2005-06-29 Novartis Ag Organic compounds
AU2006290715A1 (en) 2005-09-13 2007-03-22 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
DK2137162T3 (en) 2007-03-15 2018-11-26 Novartis Ag Organic compounds and their applications
EP2205242B1 (en) 2007-09-12 2015-04-15 Genentech, Inc. Combinations of phosphoinositide 3-kinase inhibitor compounds and chemotherapeutic agents, and methods of use
JP5348725B2 (ja) 2007-10-25 2013-11-20 ジェネンテック, インコーポレイテッド チエノピリミジン化合物の製造方法
WO2009131687A2 (en) 2008-04-22 2009-10-29 Portola Pharmaceuticals, Inc. Inhibitors of protein kinases
EP2310381A1 (en) 2008-06-13 2011-04-20 Novartis AG 2,4'-bipyridinyl compounds as protein kinase d inhibitors useful for the treatment of ia heart failure and cancer
BRPI0914891A2 (pt) 2008-06-20 2015-11-24 Metabolex Inc agonistas de aril gpr119 e usos dos mesmos
US8168784B2 (en) 2008-06-20 2012-05-01 Abbott Laboratories Processes to make apoptosis promoters
NZ624345A (en) 2008-06-27 2016-07-29 Celgene Avilomics Res Inc 2,4-disubstituted pyrimidines useful as kinase inhibitors
WO2010048149A2 (en) 2008-10-20 2010-04-29 Kalypsys, Inc. Heterocyclic modulators of gpr119 for treatment of disease
US20110306606A1 (en) 2008-12-10 2011-12-15 Jei Man Ryu Novel 2,6-substituted-3-nitropyridine derivative, method for preparing same, and pharmaceutical composition including same
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
MY177250A (en) 2010-06-30 2020-09-10 Fujifilm Corp Novel nicotinamide derivative or salt thereof
WO2012009217A1 (en) 2010-07-13 2012-01-19 Merck Sharp & Dohme Corp. Spirocyclic compounds
CA2806341C (en) 2010-07-29 2020-03-24 Rigel Pharmaceuticals, Inc. Ampk-activating heterocyclic compounds and methods for using the same
WO2012027495A1 (en) 2010-08-27 2012-03-01 University Of The Pacific Piperazinylpyrimidine analogues as protein kinase inhibitors
WO2012052948A1 (en) 2010-10-20 2012-04-26 Pfizer Inc. Pyridine- 2- derivatives as smoothened receptor modulators
JP6082011B2 (ja) 2011-09-12 2017-02-15 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Merck Patent Gesellschaft mit beschraenkter Haftung キナーゼ活性のモジュレーターとして使用するためのアミノピリミジン誘導体
WO2013096093A1 (en) 2011-12-21 2013-06-27 Merck Sharp & Dohme Corp. Compounds as dgat-1 inhibitors
CA2874546A1 (en) 2012-06-07 2013-12-12 F. Hoffmann-La Roche Ag Pyrazolopyrimidone and pyrazolopyridone inhibitors of tankyrase
EP2903985A1 (en) 2012-10-03 2015-08-12 Advinus Therapeutics Limited Spirocyclic compounds, compositions and medicinal applications thereof
US9499522B2 (en) 2013-03-15 2016-11-22 Blueprint Medicines Corporation Compositions useful for treating disorders related to kit
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
JO3517B1 (ar) * 2014-01-17 2020-07-05 Novartis Ag ان-ازاسبيرو الكان حلقي كبديل مركبات اريل-ان مغايرة وتركيبات لتثبيط نشاط shp2
WO2015107493A1 (en) 2014-01-17 2015-07-23 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
US10174032B2 (en) 2014-05-05 2019-01-08 Signalrx Pharmaceuticals, Inc. Heterocyclic compound classes for signaling modulation
JP6878316B2 (ja) 2015-06-19 2021-05-26 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
CN112625028B (zh) * 2015-06-19 2024-10-29 诺华股份有限公司 用于抑制shp2活性的化合物和组合物
WO2016203404A1 (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
JP2018517752A (ja) 2018-07-05
ES2805232T3 (es) 2021-02-11
US20180186770A1 (en) 2018-07-05
CN107922388A (zh) 2018-04-17
EP3310774B1 (en) 2020-04-29
WO2016203406A1 (en) 2016-12-22
EP3310774A1 (en) 2018-04-25
CN112625028A (zh) 2021-04-09
US10287266B2 (en) 2019-05-14
CN107922388B (zh) 2020-12-29
CN112625028B (zh) 2024-10-29

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