JP6523303B2 - 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 - Google Patents

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 Download PDF

Info

Publication number
JP6523303B2
JP6523303B2 JP2016547026A JP2016547026A JP6523303B2 JP 6523303 B2 JP6523303 B2 JP 6523303B2 JP 2016547026 A JP2016547026 A JP 2016547026A JP 2016547026 A JP2016547026 A JP 2016547026A JP 6523303 B2 JP6523303 B2 JP 6523303B2
Authority
JP
Japan
Prior art keywords
amino
alkyl
substituted
hydrogen
hydroxy
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
JP2016547026A
Other languages
English (en)
Japanese (ja)
Other versions
JP2017503000A (ja
JP2017503000A5 (enExample
Inventor
ヒウ−タン チェン,クリスティン
ヒウ−タン チェン,クリスティン
チェン,ジョウリン
ガルシア フォータネット,ジョルグ
ガルシア フォータネット,ジョルグ
グルネンフェルダー,デニス
カルキ,ラジェッシュ
充典 加藤
充典 加藤
ジェイ. ラマルシェ,マシュー
ジェイ. ラマルシェ,マシュー
ブラス ペーズ,ローレンス
ブラス ペーズ,ローレンス
マシュー スタムス,トラビス
マシュー スタムス,トラビス
ウィリアムズ,サラ
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 JP2017503000A publication Critical patent/JP2017503000A/ja
Publication of JP2017503000A5 publication Critical patent/JP2017503000A5/ja
Application granted granted Critical
Publication of JP6523303B2 publication Critical patent/JP6523303B2/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
    • C07D401/02Heterocyclic 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
    • 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
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D239/00Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/02Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
    • C07D239/24Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members
    • C07D239/28Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to ring carbon atoms
    • C07D239/46Two or more oxygen, sulphur or nitrogen atoms
    • C07D239/48Two nitrogen atoms
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D241/00Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings
    • C07D241/02Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings
    • C07D241/10Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings having three double bonds between ring members or between ring members and non-ring members
    • C07D241/14Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings having three double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D241/24Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
    • C07D241/26Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals with nitrogen atoms directly attached to ring carbon atoms
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D249/00Heterocyclic compounds containing five-membered rings having three nitrogen atoms as the only ring hetero atoms
    • C07D249/02Heterocyclic compounds containing five-membered rings having three nitrogen atoms as the only ring hetero atoms not condensed with other rings
    • C07D249/081,2,4-Triazoles; Hydrogenated 1,2,4-triazoles
    • C07D249/101,2,4-Triazoles; Hydrogenated 1,2,4-triazoles with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D249/14Nitrogen atoms
    • 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D403/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/04Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D409/00Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/14Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing three or more hetero rings
    • 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
    • C07D471/04Ortho-condensed systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D487/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/04Ortho-condensed systems

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Veterinary Medicine (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • Oncology (AREA)
  • Hematology (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
JP2016547026A 2014-01-17 2015-01-16 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 Active JP6523303B2 (ja)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201461928738P 2014-01-17 2014-01-17
US61/928,738 2014-01-17
PCT/IB2015/050343 WO2015107493A1 (en) 2014-01-17 2015-01-16 1 -pyridazin-/triazin-3-yl-piper(-azine)/idine/pyrolidine derivatives and and compositions thereof for inhibiting the activity of shp2

Publications (3)

Publication Number Publication Date
JP2017503000A JP2017503000A (ja) 2017-01-26
JP2017503000A5 JP2017503000A5 (enExample) 2018-02-22
JP6523303B2 true JP6523303B2 (ja) 2019-05-29

Family

ID=52462361

Family Applications (1)

Application Number Title Priority Date Filing Date
JP2016547026A Active JP6523303B2 (ja) 2014-01-17 2015-01-16 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

Country Status (6)

Country Link
US (4) US10093646B2 (enExample)
EP (1) EP3094627B1 (enExample)
JP (1) JP6523303B2 (enExample)
CN (1) CN105899491B (enExample)
ES (1) ES2699351T3 (enExample)
WO (1) WO2015107493A1 (enExample)

Families Citing this family (127)

* 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
US10189859B2 (en) * 2013-12-21 2019-01-29 Nektar Therapeutics Derivatives of 6-(2,3-dichlorophenyl)-1,2,4-triazin-5-amine
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
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
US9828358B2 (en) 2015-11-05 2017-11-28 Celgene Quanticel Research, Inc. Compositions comprising an inhibitor of lysine specific demethylase-1
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
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
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
AU2019222026B2 (en) * 2018-02-13 2022-05-12 Shanghai Blueray Biopharma Co., Ltd. Pyrimidine-fused cyclic compound, preparation method therefor and application thereof
CN110655520A (zh) * 2018-06-29 2020-01-07 上海青煜医药科技有限公司 嘧啶并环化合物及其制备方法和应用
CN115448923B (zh) * 2018-02-13 2024-03-22 上海青煜医药科技有限公司 嘧啶并环化合物及其制备方法和应用
CA3092011A1 (en) 2018-03-02 2019-09-06 Otsuka Pharmaceutical Co., Ltd. Pharmaceutical compounds
PE20251292A1 (es) 2018-03-08 2025-05-14 Incyte Corp Compuestos diolicos de aminopirazina como inhibidores de pi3k-gamma
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
US11046658B2 (en) 2018-07-02 2021-06-29 Incyte Corporation Aminopyrazine derivatives as PI3K-γ inhibitors
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
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
CN111153901B (zh) * 2018-11-07 2022-01-25 上海凌达生物医药有限公司 一类含氮稠杂环类shp2抑制剂化合物、制备方法和用途
CN111153899B (zh) * 2018-11-08 2023-12-01 四川科伦博泰生物医药股份有限公司 一种取代吡啶化合物、其制备方法和用途
CN113164418A (zh) 2018-12-05 2021-07-23 米拉蒂治疗股份有限公司 组合疗法
CN111484491B (zh) * 2019-01-25 2022-09-02 四川科伦博泰生物医药股份有限公司 取代吡啶并环化合物、其制备方法和用途
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
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
EP3980128A1 (en) * 2019-06-07 2022-04-13 Revolution Medicines, Inc. Solid forms of {6-[(2-amino-3-chloropyridin-4-yl)sulfanyl]-3-[(3s,4s)-4-amino-3-methyl-2-oxa-8-azaspiro[4.5]decan-8-yl]-5-methylpyrazin-2-yl}methanol, an shp2 inhibitor
TWI817018B (zh) 2019-06-28 2023-10-01 美商艾瑞生藥股份有限公司 用於治療braf相關的疾病和失調症之化合物
CN112300160A (zh) * 2019-08-01 2021-02-02 上海奕拓医药科技有限责任公司 一种螺芳环化合物、其制备及应用
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
GB201911928D0 (en) 2019-08-20 2019-10-02 Otsuka Pharma Co Ltd Pharmaceutical compounds
CN114127053B (zh) * 2019-09-06 2023-06-13 四川科伦博泰生物医药股份有限公司 一种取代吡嗪化合物、其制备方法和用途
AR120082A1 (es) 2019-09-24 2022-02-02 Relay Therapeutics Inc Inhibidores de fosfatasa shp-2 y métodos para fabricarlos y usarlos
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
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
US20230348467A1 (en) 2020-01-16 2023-11-02 Zhejiang Hisun Pharmaceutical Co., Ltd. Heteroaryl Derivative, Preparation Method Therefor, And Use Thereof
WO2021143823A1 (zh) * 2020-01-16 2021-07-22 浙江海正药业股份有限公司 吡啶或嘧啶类衍生物及其制备方法和用途
AU2021226205A1 (en) 2020-02-28 2022-10-20 Novartis Ag A triple pharmaceutical combination comprising dabrafenib, an Erk inhibitor and a SHP2 inhibitor
WO2021247836A1 (en) 2020-06-03 2021-12-09 Board Of Regents, The University Of Texas System Methods for targeting shp-2 to overcome resistance
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
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
WO2022140427A1 (en) 2020-12-22 2022-06-30 Qilu Regor Therapeutics Inc. Sos1 inhibitors and uses thereof
EP4039685A1 (en) 2021-02-08 2022-08-10 Irbm S.P.A. Azabicyclic shp2 inhibitors
TWI825637B (zh) 2021-03-31 2023-12-11 美商輝瑞股份有限公司 啶-1,6(2h,7h)-二酮
EP4067358A1 (en) 2021-04-02 2022-10-05 C.N.C.C.S. S.c.a.r.l. Collezione Nazionale Dei Composti Chimici e Centro Screening (s)-1-(5-((pyridin-3-yl)thio)pyrazin-2-yl)-4'h,6'h-spiro[piperidine-4,5'-pyrrolo[1,2-b]pyrazol]-4'-amine derivatives and similar compounds as shp2 inhibitors for the treatment of e.g. cancer
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
AU2022270116A1 (en) 2021-05-05 2023-12-21 Revolution Medicines, Inc. Ras inhibitors
WO2022235866A1 (en) 2021-05-05 2022-11-10 Revolution Medicines, Inc. Covalent ras inhibitors and uses thereof
MX2023014565A (es) 2021-06-09 2024-02-08 Chugai Pharmaceutical Co Ltd Tratamiento conjunto para tratamiento contra el cancer.
WO2022259157A1 (en) 2021-06-09 2022-12-15 Novartis Ag A triple pharmaceutical combination comprising dabrafenib, trametinib and a shp2 inhibitor
CA3216220A1 (en) 2021-06-09 2022-12-15 F. Hoffmann-La Roche Ag Combination of a particular braf inhibitor (paradox breaker) and a pd-1 axis binding antagonist for use in the treatment of cancer
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
WO2023031781A1 (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
WO2023078881A1 (en) 2021-11-04 2023-05-11 F. Hoffmann-La Roche Ag Novel use of quinazolinone compound for the treatment of cancer
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
CN116903581A (zh) * 2022-04-14 2023-10-20 山东大学 Shp2/hdac双靶点抑制剂及其制备方法和应用
CN115611869B (zh) * 2022-05-11 2024-08-09 山东大学 杂环吡嗪衍生物与其在制备shp2抑制剂中的应用
CN120504682A (zh) 2022-06-10 2025-08-19 锐新医药公司 大环ras抑制剂
EP4345101A1 (en) 2022-09-29 2024-04-03 Irbm S.P.A. Azole derivatives as shp2 inhibitors
CN115677828B (zh) * 2022-11-02 2024-10-18 四川大学 一种抗肿瘤的间二氯苯酚衍生物及其制备方法
JP2025541200A (ja) 2022-12-15 2025-12-18 エフ・ホフマン-ラ・ロシュ・アクチェンゲゼルシャフト がん処置のための併用療法
CN116332908B (zh) * 2023-03-21 2024-07-02 杭州医学院 一种shp2变构抑制剂及其制备方法和应用
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
CR20250420A (es) 2023-04-07 2025-11-20 Revolution Medicines Inc Inhibidores macrocíclicos de ras
AU2024253668A1 (en) 2023-04-07 2025-11-13 Revolution Medicines, Inc. Macrocyclic ras inhibitors
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
WO2024218632A1 (en) 2023-04-17 2024-10-24 Array Biopharma Inc. Erk protein kinase inhibitors
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
US20250375445A1 (en) 2024-06-07 2025-12-11 Revolution Medicines, Inc. Methods of treating a ras protein-related disease or disorder
WO2025261943A1 (en) 2024-06-18 2025-12-26 F. Hoffmann-La Roche Ag Anti-cancer combinations comprising mosperafenib and folfox or folfiri
WO2025265060A1 (en) 2024-06-21 2025-12-26 Revolution Medicines, Inc. Therapeutic compositions and methods for managing treatment-related effects
WO2026006747A1 (en) 2024-06-28 2026-01-02 Revolution Medicines, Inc. Ras inhibitors
WO2026015796A1 (en) 2024-07-12 2026-01-15 Revolution Medicines, Inc. Methods of treating a ras related disease or disorder
WO2026015801A1 (en) 2024-07-12 2026-01-15 Revolution Medicines, Inc. Methods of treating a ras related disease or disorder
WO2026015790A1 (en) 2024-07-12 2026-01-15 Revolution Medicines, Inc. Methods of treating a ras related disease or disorder
WO2026015825A1 (en) 2024-07-12 2026-01-15 Revolution Medicines, Inc. Use of ras inhibitor for treating pancreatic cancer

Family Cites Families (68)

* 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
GB9012316D0 (en) * 1990-06-01 1990-07-18 Wellcome Found Pharmacologically active cns compounds
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
GB0300783D0 (en) * 2003-01-14 2003-02-12 Btg Int Ltd Treatment of neurodegenerative conditions
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
EA201290062A1 (ru) 2009-08-17 2013-09-30 Мемориал Слоун-Кеттеринг Кэнсэ Сентр Соединения, связывающие белки теплового шока, композиции и способы получения указанных соединений
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
JP5727276B2 (ja) 2011-03-04 2015-06-03 協同油脂株式会社 グリース組成物及びグリース封入転がり軸受
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
US10189859B2 (en) * 2013-12-21 2019-01-29 Nektar Therapeutics Derivatives of 6-(2,3-dichlorophenyl)-1,2,4-triazin-5-amine
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
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
US10308660B2 (en) 2015-06-19 2019-06-04 Novartis Ag Compounds and compositions for inhibiting the activity of SHP2

Also Published As

Publication number Publication date
JP2017503000A (ja) 2017-01-26
US20180362496A1 (en) 2018-12-20
EP3094627B1 (en) 2018-08-22
US20170204080A1 (en) 2017-07-20
US10774065B2 (en) 2020-09-15
ES2699351T3 (es) 2019-02-08
CN105899491A (zh) 2016-08-24
US10093646B2 (en) 2018-10-09
US20200369643A1 (en) 2020-11-26
US20220348553A1 (en) 2022-11-03
WO2015107493A1 (en) 2015-07-23
CN105899491B (zh) 2019-04-02
EP3094627A1 (en) 2016-11-23
US11401259B2 (en) 2022-08-02

Similar Documents

Publication Publication Date Title
US11401259B2 (en) 1-Pyridazin-/triazin-3-yl-piper(-azine)/idine/pyrolidine derivatives and compositions thereof for inhibiting the activity of SHP2
JP7278359B2 (ja) Shp2の活性を阻害するための化合物および組成物
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
US10301278B2 (en) 1-(triazin-3-yl/pyridazin-3-yl)-piper(-azine)idine derivatives and compositions therefor for inhibiting the activity of SHP2
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: 20180110

A621 Written request for application examination

Free format text: JAPANESE INTERMEDIATE CODE: A621

Effective date: 20180110

A131 Notification of reasons for refusal

Free format text: JAPANESE INTERMEDIATE CODE: A131

Effective date: 20180918

A977 Report on retrieval

Free format text: JAPANESE INTERMEDIATE CODE: A971007

Effective date: 20180913

A521 Request for written amendment filed

Free format text: JAPANESE INTERMEDIATE CODE: A523

Effective date: 20181217

A131 Notification of reasons for refusal

Free format text: JAPANESE INTERMEDIATE CODE: A131

Effective date: 20190122

A521 Request for written amendment filed

Free format text: JAPANESE INTERMEDIATE CODE: A523

Effective date: 20190312

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: 20190416

A61 First payment of annual fees (during grant procedure)

Free format text: JAPANESE INTERMEDIATE CODE: A61

Effective date: 20190425

R150 Certificate of patent or registration of utility model

Ref document number: 6523303

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

R250 Receipt of annual fees

Free format text: JAPANESE INTERMEDIATE CODE: R250