JP7240319B2 - アロステリックshp2阻害剤としての二環式化合物 - Google Patents

アロステリックshp2阻害剤としての二環式化合物 Download PDF

Info

Publication number
JP7240319B2
JP7240319B2 JP2019539774A JP2019539774A JP7240319B2 JP 7240319 B2 JP7240319 B2 JP 7240319B2 JP 2019539774 A JP2019539774 A JP 2019539774A JP 2019539774 A JP2019539774 A JP 2019539774A JP 7240319 B2 JP7240319 B2 JP 7240319B2
Authority
JP
Japan
Prior art keywords
formula
alkyl
membered
optionally substituted
heterocycle
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
JP2019539774A
Other languages
English (en)
Japanese (ja)
Other versions
JP2020506178A5 (OSRAM
JP2020506178A (ja
Inventor
ブライアン・アール・ブランク
ジェニファー・ピッツェン
ギャング・ワン
ウォルター・エス・ウォン
クリストス・ツィチジロニス
ジエ・ジャック・リー
エレナ・エス・コルトン
ナイン・エーイ
アンドレアス・バックル
ケヴィン・メレム
クリストファー・セムコ
アッシュ・ジョガルカー
ガート・キス
アドリアン・ジル
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Revolution Medicines Inc
Original Assignee
Revolution Medicines Inc
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 Revolution Medicines Inc filed Critical Revolution Medicines Inc
Publication of JP2020506178A publication Critical patent/JP2020506178A/ja
Publication of JP2020506178A5 publication Critical patent/JP2020506178A5/ja
Priority to JP2022187881A priority Critical patent/JP2023018095A/ja
Application granted granted Critical
Publication of JP7240319B2 publication Critical patent/JP7240319B2/ja
Active legal-status Critical Current
Anticipated expiration legal-status Critical

Links

Classifications

    • 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/4353Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems
    • A61K31/437Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/4353Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems
    • A61K31/4375Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a six-membered ring having nitrogen as a ring heteroatom, e.g. quinolizines, naphthyridines, berberine, vincamine
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/4985Pyrazines or piperazines ortho- or peri-condensed with heterocyclic ring systems
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • 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
    • 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
    • C07D491/04Ortho-condensed systems
    • C07D491/044Ortho-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring
    • C07D491/048Ortho-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring the oxygen-containing ring being five-membered
    • 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
    • C07D498/04Ortho-condensed systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D513/00Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00
    • C07D513/02Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00 in which the condensed system contains two hetero rings
    • C07D513/04Ortho-condensed systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D519/00Heterocyclic compounds containing more than one system of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring system not provided for in groups C07D453/00 or C07D455/00

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Medicinal Chemistry (AREA)
  • Public Health (AREA)
  • Epidemiology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Pyridine Compounds (AREA)
JP2019539774A 2017-01-23 2018-01-09 アロステリックshp2阻害剤としての二環式化合物 Active JP7240319B2 (ja)

Priority Applications (1)

Application Number Priority Date Filing Date Title
JP2022187881A JP2023018095A (ja) 2017-01-23 2022-11-25 アロステリックshp2阻害剤としての二環式化合物

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201762449530P 2017-01-23 2017-01-23
US62/449,530 2017-01-23
PCT/US2018/013023 WO2018136265A1 (en) 2017-01-23 2018-01-09 Bicyclic compounds as allosteric shp2 inhibitors

Related Child Applications (1)

Application Number Title Priority Date Filing Date
JP2022187881A Division JP2023018095A (ja) 2017-01-23 2022-11-25 アロステリックshp2阻害剤としての二環式化合物

Publications (3)

Publication Number Publication Date
JP2020506178A JP2020506178A (ja) 2020-02-27
JP2020506178A5 JP2020506178A5 (OSRAM) 2021-02-12
JP7240319B2 true JP7240319B2 (ja) 2023-03-15

Family

ID=61054566

Family Applications (2)

Application Number Title Priority Date Filing Date
JP2019539774A Active JP7240319B2 (ja) 2017-01-23 2018-01-09 アロステリックshp2阻害剤としての二環式化合物
JP2022187881A Pending JP2023018095A (ja) 2017-01-23 2022-11-25 アロステリックshp2阻害剤としての二環式化合物

Family Applications After (1)

Application Number Title Priority Date Filing Date
JP2022187881A Pending JP2023018095A (ja) 2017-01-23 2022-11-25 アロステリックshp2阻害剤としての二環式化合物

Country Status (14)

Country Link
US (2) US11739093B2 (OSRAM)
EP (1) EP3571199A1 (OSRAM)
JP (2) JP7240319B2 (OSRAM)
KR (1) KR102665763B1 (OSRAM)
CN (2) CN117327075A (OSRAM)
AR (1) AR110740A1 (OSRAM)
AU (2) AU2018210770B2 (OSRAM)
BR (1) BR112019015075A2 (OSRAM)
CA (1) CA3051206A1 (OSRAM)
IL (2) IL296456A (OSRAM)
MX (2) MX2019008695A (OSRAM)
SG (1) SG11201906209SA (OSRAM)
TW (1) TWI820013B (OSRAM)
WO (1) WO2018136265A1 (OSRAM)

Families Citing this family (112)

* 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
WO2017210134A1 (en) 2016-05-31 2017-12-07 Board Of Regents, University Of Texas System Heterocyclic inhibitors of ptpn11
WO2017216706A1 (en) 2016-06-14 2017-12-21 Novartis Ag Compounds and compositions for inhibiting the activity of shp2
WO2018013597A1 (en) 2016-07-12 2018-01-18 Revolution Medicines, Inc. 2,5-disubstituted 3-methyl pyrazines and 2,5,6-trisubstituted 3-methyl pyrazines as allosteric shp2 inhibitors
WO2018057884A1 (en) 2016-09-22 2018-03-29 Relay Therapeutics, Inc. Shp2 phosphatase inhibitors and methods of use thereof
TW202500565A (zh) 2016-10-24 2025-01-01 美商傳達治療有限公司 Shp2磷酸酶抑制劑及其使用方法
BR112019014527A2 (pt) 2017-01-23 2020-02-27 Revolution Medicines, Inc. Compostos de piridina como inibidores de shp2 alostéricos
AR110740A1 (es) 2017-01-23 2019-05-02 Revolution Medicines Inc Compuestos bicíclicos como inhibidores alostéricos de shp2
WO2018218133A1 (en) 2017-05-26 2018-11-29 Relay Therapeutics, Inc. Pyrazolo[3,4-b]pyrazine derivatives as shp2 phosphatase inhibitors
JP7356414B2 (ja) 2017-09-07 2023-10-04 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 がんを治療するためのshp2阻害剤組成物および方法
MA50245A (fr) 2017-09-11 2020-07-22 Krouzon Pharmaceuticals Inc Inhibiteurs allostériques octahydrocyclopenta[c]pyrrole de shp2
WO2019067843A1 (en) 2017-09-29 2019-04-04 Relay Therapeutics, Inc. PYRAZOLO [3,4-B] PYRAZINE DERIVATIVES AS INHIBITORS OF PHOSPHATASE SHP2
CN111212834B (zh) 2017-10-12 2024-01-19 锐新医药公司 作为变构shp2抑制剂的吡啶、吡嗪和三嗪化合物
BR112020009757A2 (pt) * 2017-12-15 2020-11-03 Revolution Medicines, Inc. compostos policíclicos como inibidores alostéricos de shp2
JP7474709B2 (ja) 2018-02-27 2024-04-25 インサイト・コーポレイション A2a/a2b阻害剤としてのイミダゾピリミジン及びトリアゾロピリミジン
SG11202009245TA (en) 2018-03-21 2020-10-29 Relay Therapeutics Inc Shp2 phosphatase inhibitors and methods of use 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
KR102724968B1 (ko) 2018-03-21 2024-10-31 수조우 푸허 바이오파마 컴퍼니 리미티드 Shp2 억제제 및 이의 용도
EP3787627A4 (en) 2018-05-02 2021-12-01 Navire Pharma, Inc. SUBSTITUTED HETEROCYCLIC INHIBITORS FOR PTPN11
MA52940A (fr) 2018-05-18 2021-04-28 Incyte Corp Dérivés de pyrimidine fusionnés utilisés en tant qu'inhibiteurs de a2a/a2b
AU2019297361B2 (en) 2018-07-05 2024-06-27 Incyte Corporation Fused pyrazine derivatives as A2A / A2B inhibitors
BR112021002327A2 (pt) 2018-08-10 2021-05-04 Navire Pharma, Inc. derivados de 6-(4-amino-3-metil-2-oxa-8-azaespiro[4,5]decan-8-il)-3-(2,3-diclorofenil)-2-metilpirimidin-4(3h)-ona e compostos relacionados como inibidores de ptpn11(shp2) para o tratamento do câncer
US20200115389A1 (en) 2018-09-18 2020-04-16 Nikang Therapeutics, Inc. Fused tricyclic ring derivatives as src homology-2 phosphatase inhibitors
AU2019350592B2 (en) 2018-09-29 2024-09-26 Novartis Ag Process of manufacture of a compound for inhibiting the activity of SHP2
MX2021003460A (es) * 2018-09-29 2021-06-18 Novartis Ag Fabricacion de compuestos y composiciones para inhibir la actividad de shp2.
US11179397B2 (en) 2018-10-03 2021-11-23 Gilead Sciences, Inc. Imidazopyrimidine derivatives
WO2020076723A1 (en) 2018-10-08 2020-04-16 Revolution Medicines, Inc. Shp2 inhibitor compositions for use in treating cancer
US12187721B2 (en) 2018-10-17 2025-01-07 Array Biopharma Inc. Protein tyrosine phosphatase inhibitors
CN117143079A (zh) * 2018-11-06 2023-12-01 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
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
TWI829857B (zh) 2019-01-29 2024-01-21 美商英塞特公司 作為a2a / a2b抑制劑之吡唑并吡啶及三唑并吡啶
MX2021010319A (es) 2019-03-01 2021-12-10 Revolution Medicines Inc Compuestos biciclicos de heteroarilo y usos de estos.
KR20210146288A (ko) 2019-03-01 2021-12-03 레볼루션 메디슨즈, 인크. 이환식 헤테로사이클릴 화합물 및 이의 용도
WO2020181283A1 (en) 2019-03-07 2020-09-10 Merck Patent Gmbh Carboxamide-pyrimidine derivatives as shp2 antagonists
BR112021018664A2 (pt) 2019-04-02 2021-11-23 Array Biopharma Inc Inibidores de proteína tirosina fosfatase
JP7586834B2 (ja) 2019-04-08 2024-11-19 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拮抗薬としてのピリミジノン誘導体
MX2021013146A (es) 2019-05-13 2022-01-24 Relay Therapeutics Inc Inhibidores de receptores del factor de crecimiento de fibroblastos (fgfr) y metodos de uso de los mismos.
EP3991731A4 (en) * 2019-06-28 2022-07-20 Tuojie Biotech (Shanghai) Co., Ltd. FIVE-MEMBERED NITROGEN-CONTAINING HETEROCYCLIC PYRIMIDINE DERIVATIVE, PROCESS FOR ITS PREPARATION AND ITS PHARMACEUTICAL USE
CN111704611B (zh) * 2019-07-25 2022-01-14 上海凌达生物医药有限公司 一类芳基螺环类shp2抑制剂化合物、制备方法和用途
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
US11890281B2 (en) 2019-09-24 2024-02-06 Relay Therapeutics, Inc. SHP2 phosphatase inhibitors and methods of making and using the same
US11566007B2 (en) 2019-11-04 2023-01-31 Revolution Medicines, Inc. Ras inhibitors
EP4054720A1 (en) 2019-11-04 2022-09-14 Revolution Medicines, Inc. Ras inhibitors
US11608346B2 (en) 2019-11-04 2023-03-21 Revolution Medicines, Inc. Ras inhibitors
EP4620531A3 (en) 2019-11-08 2025-11-26 Revolution Medicines, Inc. Bicyclic heteroaryl compounds and uses thereof
JP2023505100A (ja) 2019-11-27 2023-02-08 レボリューション メディシンズ インコーポレイテッド 共有ras阻害剤及びその使用
WO2021115286A1 (zh) * 2019-12-10 2021-06-17 成都倍特药业股份有限公司 一种可用作shp2抑制剂的含氮杂原子的六元并五元芳环衍生物
WO2021142026A1 (en) 2020-01-07 2021-07-15 Revolution Medicines, Inc. Shp2 inhibitor dosing and methods of treating cancer
CN114867720B (zh) 2020-01-16 2024-10-22 浙江海正药业股份有限公司 杂芳基类衍生物及其制备方法和用途
CN111393459B (zh) * 2020-04-16 2022-07-22 南京安纳康生物科技有限公司 Shp2抑制剂及其用途
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
IL298917A (en) * 2020-06-11 2023-02-01 Betta Pharmaceuticals Co Ltd Shp2 inhibitors, compositions and uses thereof
TW202214253A (zh) 2020-06-18 2022-04-16 美商銳新醫藥公司 延遲、預防及治療對ras抑制劑之後天抗性之方法
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
CN111925333A (zh) * 2020-09-01 2020-11-13 济南悟通生物科技有限公司 一种2-氨基-5-甲基吡嗪的制备方法及产品与应用
IL301062A (en) 2020-09-03 2023-05-01 Revolution Medicines Inc Use of sos1 inhibitors to treat malignancies with shp2 mutations
CR20230165A (es) 2020-09-15 2023-06-02 Revolution Medicines Inc Derivados indólicos como inhibidores de ras en el tratamiento del cáncer
TW202233629A (zh) 2020-10-20 2022-09-01 美商安進公司 雜環螺環化合物及使用方法
US20230406860A1 (en) 2020-10-27 2023-12-21 Amgen Inc. Heterocyclic spiro compounds and methods of use
TW202233625A (zh) 2020-11-18 2022-09-01 美商傳達治療有限公司 Fgfr抑制劑及其製造及使用方法
CN112402385B (zh) * 2020-11-30 2022-04-01 北京华氏开元医药科技有限公司 4-羟甲基-1h-吲哚类化合物药物制剂及其制备方法
CN112194652B (zh) * 2020-11-30 2021-03-05 北京华氏开元医药科技有限公司 4-羟甲基-1h-吲哚类化合物、制备方法及应用
AR124449A1 (es) 2020-12-22 2023-03-29 Qilu Regor Therapeutics Inc Inhibidores de sos1 y usos de los mismos
WO2022135568A1 (zh) * 2020-12-25 2022-06-30 江苏恒瑞医药股份有限公司 一种嘧啶并五元氮杂环类衍生物的晶型及其制备方法
EP4039685A1 (en) 2021-02-08 2022-08-10 Irbm S.P.A. Azabicyclic shp2 inhibitors
EP4301756A4 (en) * 2021-03-05 2025-02-26 Nimbus Saturn, Inc. HPK1 ANTAGONISTS AND THEIR USES
US12071442B2 (en) 2021-03-29 2024-08-27 Nimbus Saturn, Inc. Substituted pyrrolo[3,4-c]pyridines as HPK1 antagonists
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
JP2024517693A (ja) 2021-04-29 2024-04-23 アムジエン・インコーポレーテツド 2-アミノベンゾチアゾール化合物及びその使用方法
CN117500811A (zh) 2021-05-05 2024-02-02 锐新医药公司 共价ras抑制剂及其用途
CN118561952A (zh) 2021-05-05 2024-08-30 锐新医药公司 Ras抑制剂
CR20230558A (es) 2021-05-05 2024-01-24 Revolution Medicines Inc Inhibidores de ras para el tratamiento del cáncer
WO2022238816A1 (en) * 2021-05-14 2022-11-17 Bm Pharma Consulting Pty. Ltd Bicyclic heterocyclic compounds for prophylaxis and treatment of viral infections
TW202313041A (zh) 2021-06-09 2023-04-01 瑞士商諾華公司 包含達拉菲尼、曲美替尼和shp2抑制劑之三重藥物組合
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
TW202327569A (zh) 2021-09-01 2023-07-16 瑞士商諾華公司 包含tead抑制劑的藥物組合及其用於癌症治療之用途
AR127308A1 (es) 2021-10-08 2024-01-10 Revolution Medicines Inc Inhibidores ras
WO2023109761A1 (zh) * 2021-12-15 2023-06-22 贝达药业股份有限公司 吡唑并嘧啶酮类化合物及其盐的结晶
KR102681872B1 (ko) * 2022-01-11 2024-07-04 서울대학교산학협력단 신규한 스피로-매크로라이드 화합물, 이의 생산 방법 및 용도
US20250179077A1 (en) 2022-02-16 2025-06-05 Amgen Inc. Quinazoline compounds and uses thereof as inhibitors of mutant kras proteins
US20250163064A1 (en) 2022-02-16 2025-05-22 Amgen Inc. Quinazoline compounds and uses thereof as inhibitors of mutant kras proteins
KR20240153578A (ko) * 2022-02-23 2024-10-23 치아타이 티안큉 파마수티컬 그룹 주식회사 피롤리논 함유 융합 비시클릭 화합물
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
CN114685301A (zh) * 2022-03-31 2022-07-01 山东省药学科学院 一种2-氨基丙二酰胺的生产改良方法
IL316768A (en) 2022-05-25 2025-01-01 Ikena Oncology Inc MEK inhibitors and their uses
EP4536364A1 (en) 2022-06-10 2025-04-16 Revolution Medicines, Inc. Macrocyclic ras inhibitors
EP4568956A1 (en) 2022-08-11 2025-06-18 Relay Therapeutics, Inc. Solid forms of a cdk inhibitor
EP4573095A1 (en) 2022-08-17 2025-06-25 Treeline Biosciences, Inc. Pyridopyrimidine kras inhibitors
EP4345101A1 (en) 2022-09-29 2024-04-03 Irbm S.P.A. Azole derivatives as shp2 inhibitors
AU2024241633A1 (en) 2023-03-30 2025-11-06 Revolution Medicines, Inc. Compositions for inducing ras gtp hydrolysis and uses thereof
AR132338A1 (es) 2023-04-07 2025-06-18 Revolution Medicines Inc Inhibidores de ras
WO2024211712A1 (en) 2023-04-07 2024-10-10 Revolution Medicines, Inc. Condensed macrocyclic compounds as ras inhibitors
KR20250172857A (ko) 2023-04-14 2025-12-09 레볼루션 메디슨즈, 인크. Ras 억제제의 결정형
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
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
TW202528315A (zh) 2023-09-21 2025-07-16 美商樹線生物科學公司 螺環二氫哌喃并吡啶KRas抑制劑
TW202530228A (zh) 2023-10-12 2025-08-01 美商銳新醫藥公司 Ras抑制劑
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
WO2025194054A1 (en) 2024-03-14 2025-09-18 Amgen Inc. Spirocyclic compounds as modulators of kras and uses thereof
WO2025194057A1 (en) 2024-03-14 2025-09-18 Amgen Inc. Macrocyclic compounds as modulators of kras and uses thereof
WO2025217247A1 (en) 2024-04-10 2025-10-16 Amgen Inc. Tethered spiro-heterocyclic inhibitors of kras g12c mutant proteins and uses thereof
WO2025230878A1 (en) 2024-04-29 2025-11-06 Amgen Inc. Macrocyclic compounds as modulators of kras and uses thereof
WO2025240582A1 (en) 2024-05-14 2025-11-20 Amgen Inc. Macrocyclic compounds as modulators of kras and uses thereof
WO2025240847A1 (en) 2024-05-17 2025-11-20 Revolution Medicines, Inc. Ras inhibitors
WO2025245127A1 (en) 2024-05-21 2025-11-27 Treeline Biosciences, Inc. Spirocyclic dihydropyranopyrimidine kras inhibitors
WO2025255438A1 (en) 2024-06-07 2025-12-11 Revolution Medicines, Inc. Methods of treating a ras protein-related disease or disorder

Citations (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2003508382A (ja) 1999-08-27 2003-03-04 スージェン・インコーポレーテッド リン酸模倣体およびホスファターゼ阻害剤を用いる治療方法
JP2008503591A (ja) 2004-06-22 2008-02-07 ライジェル ファーマシューティカルズ, インコーポレイテッド ユビキチンリガーゼ阻害剤
WO2010011666A2 (en) 2008-07-21 2010-01-28 University Of South Florida Indoline scaffold shp-2 inhibitors and cancer treatment method
CN103554038A (zh) 2013-06-19 2014-02-05 云南大学 多卤代苯腈喹唑啉酮化合物及其制备方法和用途
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
WO2016203404A1 (en) 2015-06-19 2016-12-22 Novartis Ag Compounds and compositions for inhibiting the activity of shp2

Family Cites Families (123)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US2572728A (en) 1949-01-07 1951-10-23 American Cyanamid Co Hydroxybenzenesulfonamidopyra-zines and preparation of same
US2636882A (en) 1950-08-11 1953-04-28 Quaker Oats Co Preparation of 3-pyridols from 2-acylfurans
BE758503A (fr) 1969-11-07 1971-05-05 Shell Int Research Compositions pesticides
GB1459571A (en) 1974-09-12 1976-12-22 Pfizer Ltd Thiophene-2-sulphonamide derivatives and their use as therapeutic agents sheet orienting apparatus
JPS5762269A (en) 1980-10-03 1982-04-15 Ogawa Koryo Kk 2,3,5-trisubstituted pyrazine derivative
US4513135A (en) 1982-03-05 1985-04-23 Eli Lilly And Company Diaryl-pyrazine derivatives affecting GABA binding
DE3242195A1 (de) 1982-11-15 1984-05-17 Basf Ag, 6700 Ludwigshafen Neue 2-aminopyrazine und verfahren zur herstellung von 2-aminopyrazinen und pyrazinen
JPH0249775A (ja) 1988-05-19 1990-02-20 Nippon Soda Co Ltd 6員環又は7員環を有する複素環化合物及びその製造方法
JPH04112877A (ja) 1990-09-04 1992-04-14 Nippon Soda Co Ltd 新規シアノピラジン誘導体及びその製造方法
EP0579835A4 (en) 1991-11-12 1994-06-01 Nippon Soda Co Wavelength conversion material for agriculture
US5262564A (en) 1992-10-30 1993-11-16 Octamer, Inc. Sulfinic acid adducts of organo nitroso compounds useful as retroviral inactivating agents anti-retroviral agents and anti-tumor agents
GB9504854D0 (en) 1994-03-31 1995-04-26 Zeneca Ltd Nitrogen derivatives
CZ244598A3 (cs) 1996-02-07 1998-10-14 Janssen Pharmaceutica N.V. Pyrazolopyrimidiny jako antagonisty CRF receptoru
AU8071698A (en) 1997-06-13 1998-12-30 Sugen, Inc. Novel heteroaryl compounds for the modulation of protein tyrosine enzyme relatedcellular signal transduction
AU783915B2 (en) 2000-02-16 2005-12-22 Neurogen Corporation Substituted arylpyrazines
EP1448587B1 (en) 2001-10-01 2009-09-02 Mount Sinai School of Medicine Noonan syndrome gene
US6921762B2 (en) 2001-11-16 2005-07-26 Amgen Inc. Substituted indolizine-like compounds and methods of use
MXPA04004714A (es) 2001-11-21 2004-08-19 Upjohn Co Derivados de aril 1,4-pirazina sustituidos.
CA2479744A1 (en) 2002-03-28 2003-10-09 Paul E. Finke Substituted 2,3-diphenyl pyridines
EP1539736A1 (en) 2002-09-12 2005-06-15 Pharmacia & Upjohn Company LLC Substituted 1,4-pyrazine derivatives
WO2004056875A1 (en) 2002-12-23 2004-07-08 Wyeth Antibodies against pd-1 and uses therefor
US7157460B2 (en) * 2003-02-20 2007-01-02 Sugen Inc. Use of 8-amino-aryl-substituted imidazopyrazines as kinase inhibitors
MXPA05012082A (es) 2003-05-09 2006-02-22 Pharmacia & Upjohn Co Llc Compuestos como antagonistas del receptor crf1.
GB0314057D0 (en) 2003-06-18 2003-07-23 Astrazeneca Ab Therapeutic agents
FR2856684B1 (fr) 2003-06-26 2008-04-11 Sanofi Synthelabo Derives de diphenylpyridine, leur preparation et leur application en therapeutique
WO2005028480A2 (en) 2003-09-03 2005-03-31 Neurogen Corporation 5-aryl-pyrazolo[4,3-d]pyrimidines, pyridines, and pyrazines and related compounds
CA2541832C (en) * 2003-10-10 2009-11-24 Pfizer Products Inc. Substituted 2h-[1,2,4]triazolo[4,3-a]pyrazines as gsk-3 inhibitors
EP1678160A1 (en) 2003-10-27 2006-07-12 Astellas Pharma Inc. Pyrazine derivatives and pharmaceutical use thereof
DE102004015954A1 (de) 2004-04-01 2005-11-10 Ina-Schaeffler Kg Umschlingungstrieb
WO2005095384A1 (en) 2004-04-01 2005-10-13 Astellas Pharma Inc. Pyrazine derivatives and pharmaceutical use thereof as adenosine antagonists
ES2375395T3 (es) 2004-12-23 2012-02-29 Mallinckrodt Llc Derivados de pirazina fluorescentes y método de uso de los mismos en la evaluación de la función renal.
JP2008536950A (ja) 2005-04-18 2008-09-11 ニューロジェン・コーポレーション 置換ヘテロアリールのcb1拮抗薬
UA95244C2 (ru) 2005-06-22 2011-07-25 Плексикон, Инк. Соединения и способ модулирования активности киназ, и показания для их применения
US20080274469A1 (en) 2005-10-21 2008-11-06 The Regents Of The University Of California C-Kit Oncogene Mutations in Melanoma
WO2007106142A2 (en) 2006-02-24 2007-09-20 Mallinckrodt Inc. Process for using optical agents
JP2007277097A (ja) 2006-04-03 2007-10-25 Mie Univ 発光化合物、発光方法、及びその製造方法
WO2007117699A2 (en) 2006-04-07 2007-10-18 University Of South Florida Inhibition of shp2/ptpn11 protein tyrosine phosphatase by nsc-87877, nsc-117199 and their analogs
EP2063894B1 (en) 2006-04-28 2019-08-28 Northwestern University Formulations containing pyridazine compounds for treating neuroinflammatory diseases
WO2007127448A2 (en) 2006-04-28 2007-11-08 Northwestern University Salts of pyridazine compounds
US7893058B2 (en) * 2006-05-15 2011-02-22 Janssen Pharmaceutica Nv Imidazolopyrazine compounds useful for the treatment of degenerative and inflammatory diseases
WO2007138072A2 (en) * 2006-05-31 2007-12-06 Galapagos N.V. Triazolopyrazine compounds useful for the treatment of degenerative & inflammatory diseases
WO2007145921A1 (en) * 2006-06-06 2007-12-21 Schering Corporation Imidazopyrazines as protein kinase inhibitors
WO2008108944A2 (en) 2007-03-01 2008-09-12 Mallinckrodt Inc. Integrated photoactive small molecules and uses thereof
ATE502940T1 (de) 2007-04-06 2011-04-15 Novartis Ag Ä2,6-ünaphthyridine als proteinkinasehemmer
US8133895B2 (en) * 2007-05-10 2012-03-13 Janssen Pharmaceutica N.V. Fused pyrazine compounds useful for the treatment of degenerative and inflammatory diseases
WO2008138842A1 (en) * 2007-05-10 2008-11-20 Galapagos N.V. Imidazopyrazines and triazolopyrazine for the treatment of joint degenerative and inflammatory diseases
EP2157090A4 (en) 2007-06-21 2011-09-07 Taisho Pharmaceutical Co Ltd PYRAZINAMIDE COMPOUND
US8003797B2 (en) 2007-08-09 2011-08-23 Merck Sharp & Dohme Corp. Pyridine carboxamide orexin receptor antagonists
WO2009025823A1 (en) 2007-08-21 2009-02-26 Amgen Inc. Phosphodiesterase 10 inhibitors
WO2010051238A1 (en) 2008-10-30 2010-05-06 Merck Sharp & Dohme Corp. Pyridazine carboxamide orexin receptor antagonists
SG2014005318A (en) 2009-01-23 2014-03-28 Rigel Pharmaceuticals Inc Compositions and methods for inhibition of the jak pathway
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
WO2010141275A1 (en) 2009-06-01 2010-12-09 Merck Sharp & Dohme Corp. Pyrazine carboxamide orexin receptor antagonists
CA2771190C (en) 2009-08-17 2020-01-21 Memorial Sloan-Kettering Cancer Center Heat shock protein binding compounds, compositions, and methods for making and using same
CA2780713A1 (en) 2009-09-03 2011-03-10 Vancouver Biotech Ltd. Monoclonal antibodies against gonadotropin-releasing hormone receptor
US8673913B2 (en) 2009-11-13 2014-03-18 Case Western Reserve University SHP-2 phosphatase inhibitor
CA2789071C (en) 2010-03-05 2018-03-27 F. Hoffmann-La Roche Ag Antibodies against human csf-1r and uses thereof
TW201200518A (en) 2010-03-10 2012-01-01 Kalypsys Inc Heterocyclic inhibitors of histamine receptors for the treatment of disease
JP5833105B2 (ja) 2010-05-11 2015-12-16 サノフイ 置換n−ヘテロアリールスピロラクタムビピロリジン類、その製造及び治療的使用
US8703768B2 (en) 2010-06-09 2014-04-22 Hoffmann-La Roche Inc. Nitrogen containing heteroaryl compounds
KR101491938B1 (ko) 2010-07-14 2015-02-10 노파르티스 아게 Ip 수용체 효능제 헤테로시클릭 화합물
GB201106829D0 (en) 2011-04-21 2011-06-01 Proximagen Ltd Heterocyclic compounds
US9127000B2 (en) * 2011-02-23 2015-09-08 Intellikine, LLC. Heterocyclic compounds and uses thereof
WO2012149280A2 (en) 2011-04-29 2012-11-01 Abbott Laboratories Novel tricyclic compounds
CN103181918B (zh) 2011-05-04 2014-10-29 厦门大学 脂肪酸类化合物在制备预防和治疗肝癌药物中的应用
US20150005311A1 (en) 2012-01-13 2015-01-01 Novartis Ag IP receptor agonist heterocyclic compounds
JP6374384B2 (ja) * 2012-08-07 2018-08-15 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 プロテインキナーゼ阻害剤としてのピリドピリミジン誘導体
JP5857168B2 (ja) * 2012-11-08 2016-02-10 ファイザー・インク ドーパミンd1リガンドとしての複素芳香族化合物およびその使用
BR112015012366A8 (pt) * 2012-11-29 2019-10-01 Chemocentryx Inc antagonistas de cxcr7, uso dos mesmos, composição farmacêutica, bem como métodos para detectar níveis elevados de cxcr7 em uma amostra e para imagear um tumor, órgão, ou tecido
WO2014113584A1 (en) 2013-01-16 2014-07-24 Rhode Island Hospital Compositions and methods for the prevention and treatment of osteolysis and osteoporosis
CN104995182A (zh) 2013-02-07 2015-10-21 默克专利股份公司 被取代的喹喔啉衍生物及其作为mGluR4的正变构调节剂的用途
CN111139256A (zh) 2013-02-20 2020-05-12 诺华股份有限公司 使用人源化抗EGFRvIII嵌合抗原受体治疗癌症
CA2902026C (en) 2013-03-13 2023-08-29 Prothena Biosciences Limited Tau immunotherapy
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
CA2946759A1 (en) 2014-04-25 2015-10-29 Memorial Sloan-Kettering Cancer Center Treatment of h-ras-driven tumors
WO2016007731A1 (en) * 2014-07-10 2016-01-14 Incyte Corporation Imidazopyridines and imidazopyrazines as lsd1 inhibitors
MY187540A (en) 2014-08-01 2021-09-28 Nuevolution As Compounds active towards bromodomains
CN107106558A (zh) 2014-11-18 2017-08-29 默沙东公司 具有a2a拮抗剂性质的氨基吡嗪化合物
ES2881305T3 (es) 2014-12-17 2021-11-29 Siemens Healthcare Diagnostics Inc Diseño de ensayo sandwich para pequeñas moléculas
US10220036B2 (en) 2014-12-23 2019-03-05 Novartis Ag Triazolopyrimidine compounds and uses thereof
EP3247378B8 (en) 2015-01-09 2023-08-23 Revolution Medicines, Inc. Macrocyclic compounds that participate in cooperative binding and medical uses thereof
KR20170109589A (ko) 2015-02-05 2017-09-29 티르노보 리미티드 암 치료를 위한 irs/stat3 이중 조절제 및 항암제의 조합물
AU2016243939B2 (en) 2015-04-03 2020-09-03 Incyte Holdings Corporation Heterocyclic compounds as LSD1 inhibitors
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
US10287266B2 (en) 2015-06-19 2019-05-14 Novartis Ag Compounds and compositions for inhibiting the activity of SHP2
WO2017011618A1 (en) 2015-07-15 2017-01-19 The Curators Of The University Of Missouri Targeted nanoparticle conjugate and method for co-delivery of sirna and drug
CN105175330B (zh) 2015-08-28 2018-11-13 湖南大学 一种5-位取代硫醚化/硒醚化/碲醚化喹啉类化合物及其制备方法
WO2017059207A1 (en) 2015-10-01 2017-04-06 Warp Drive Bio, Inc. Methods and reagents for analyzing protein-protein interfaces
KR20180094923A (ko) 2015-12-24 2018-08-24 교와 핫꼬 기린 가부시키가이샤 α, β 불포화 아미드 화합물
WO2017156397A1 (en) 2016-03-11 2017-09-14 Board Of Regents, The University Of Texas Sysytem Heterocyclic inhibitors of ptpn11
GB201604970D0 (en) 2016-03-23 2016-05-04 Syngenta Participations Ag Improvements in or relating to organic compounds
CN114539273A (zh) 2016-06-07 2022-05-27 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
WO2017216706A1 (en) 2016-06-14 2017-12-21 Novartis Ag Compounds and compositions for inhibiting the activity of shp2
WO2018013597A1 (en) 2016-07-12 2018-01-18 Revolution Medicines, Inc. 2,5-disubstituted 3-methyl pyrazines and 2,5,6-trisubstituted 3-methyl pyrazines as allosteric shp2 inhibitors
WO2018057884A1 (en) 2016-09-22 2018-03-29 Relay Therapeutics, Inc. Shp2 phosphatase inhibitors and methods of use thereof
TW202500565A (zh) 2016-10-24 2025-01-01 美商傳達治療有限公司 Shp2磷酸酶抑制劑及其使用方法
RU2769132C2 (ru) 2017-01-10 2022-03-28 Новартис Аг Фармацевтическая комбинация, содержащая ингибитор alk и ингибитор shp2
AR110740A1 (es) 2017-01-23 2019-05-02 Revolution Medicines Inc Compuestos bicíclicos como inhibidores alostéricos de shp2
BR112019014527A2 (pt) 2017-01-23 2020-02-27 Revolution Medicines, Inc. Compostos de piridina como inibidores de shp2 alostéricos
HRP20241239T1 (hr) 2017-03-23 2024-12-06 Jacobio Pharmaceuticals Co., Ltd. Novi heterociklički derivati korisni kao shp2 inhibitori
KR20200003803A (ko) 2017-04-05 2020-01-10 레볼루션 메디슨즈, 인크. 협동 결합에 참여하는 화합물 및 그의 용도
KR20240093922A (ko) 2017-04-05 2024-06-24 레볼루션 메디슨즈, 인크. 단백질-단백질 계면을 분석하기 위한 방법 및 시약
WO2018218133A1 (en) 2017-05-26 2018-11-29 Relay Therapeutics, Inc. Pyrazolo[3,4-b]pyrazine derivatives as shp2 phosphatase inhibitors
JP7356414B2 (ja) 2017-09-07 2023-10-04 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 がんを治療するためのshp2阻害剤組成物および方法
CN111212834B (zh) 2017-10-12 2024-01-19 锐新医药公司 作为变构shp2抑制剂的吡啶、吡嗪和三嗪化合物
BR112020009757A2 (pt) 2017-12-15 2020-11-03 Revolution Medicines, Inc. compostos policíclicos como inibidores alostéricos de shp2
CN110156786B (zh) 2018-02-13 2022-06-03 青煜医药研发(上海)有限公司 嘧啶并环化合物及其制备方法和应用
EP3753941B1 (en) 2018-02-13 2024-05-01 Shanghai Blueray Biopharma Co., Ltd. Pyrimidine-fused cyclic compound, preparation method therefor and application thereof
KR102724968B1 (ko) 2018-03-21 2024-10-31 수조우 푸허 바이오파마 컴퍼니 리미티드 Shp2 억제제 및 이의 용도
SG11202009793TA (en) 2018-04-10 2020-10-29 Revolution Medicines Inc Shp2 inhibitor compositions, methods for treating cancer and methods for identifying a subject with shp2 mutations
BR112020022201A2 (pt) 2018-05-01 2021-02-02 Revolution Medicines, Inc. análogos de rapamicina ligada a c40, c28, e c-32 como inibidores de mtor
IL312291A (en) 2018-05-01 2024-06-01 Revolution Medicines Inc C-26-linked rapamycin analogs as MTOR inhibitors
CA3111980A1 (en) 2018-09-10 2020-03-19 Mirati Therapeutics, Inc. Combination therapies
US20200115389A1 (en) 2018-09-18 2020-04-16 Nikang Therapeutics, Inc. Fused tricyclic ring derivatives as src homology-2 phosphatase inhibitors
US11179397B2 (en) 2018-10-03 2021-11-23 Gilead Sciences, Inc. Imidazopyrimidine derivatives
WO2020076723A1 (en) 2018-10-08 2020-04-16 Revolution Medicines, Inc. Shp2 inhibitor compositions for use in treating cancer
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
JP7377679B2 (ja) 2018-11-19 2023-11-10 アムジエン・インコーポレーテツド がん治療のためのkrasg12c阻害剤及び1種以上の薬学的に活性な追加の薬剤を含む併用療法
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
US20220073521A1 (en) 2018-11-30 2022-03-10 Tuojie Biotech (Shanghai) Co., Ltd. Pyrimidine and five-membered nitrogen heterocycle derivative, preparation method therefor, and medical uses thereof
US20200197391A1 (en) 2018-12-21 2020-06-25 Revolution Medicines, Inc. Compounds that participate in cooperative binding and uses thereof
EP4054720A1 (en) 2019-11-04 2022-09-14 Revolution Medicines, Inc. Ras inhibitors

Patent Citations (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2003508382A (ja) 1999-08-27 2003-03-04 スージェン・インコーポレーテッド リン酸模倣体およびホスファターゼ阻害剤を用いる治療方法
JP2008503591A (ja) 2004-06-22 2008-02-07 ライジェル ファーマシューティカルズ, インコーポレイテッド ユビキチンリガーゼ阻害剤
WO2010011666A2 (en) 2008-07-21 2010-01-28 University Of South Florida Indoline scaffold shp-2 inhibitors and cancer treatment method
CN103554038A (zh) 2013-06-19 2014-02-05 云南大学 多卤代苯腈喹唑啉酮化合物及其制备方法和用途
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
WO2016203404A1 (en) 2015-06-19 2016-12-22 Novartis Ag Compounds and compositions for inhibiting the activity of shp2

Non-Patent Citations (5)

* Cited by examiner, † Cited by third party
Title
Journal of Heterocyclic Chemistry,1988年,Vol. 25, No. 3,Vol. 879-883
Proceedings of the Royal Irish Academy, Section B: Biological, Geological and Chemical Science,1974年,Vol. 74, No. 14,pp. 185-192
REGISTRY(STN)[online],[検索日 2021.11.05],2004年11月10日,CAS登録番号777880-58-7, 777873-58-2, 777873-55-9
REGISTRY(STN)[online],[検索日 2021.11.10],2016年05月26日,CAS登録番号1918848-03-9、1918847-95-6、1918768-32-7
Zhurnal Organicheskoi Khimii,1982年,Vol. 18, No. 3,pp. 656-662

Also Published As

Publication number Publication date
JP2023018095A (ja) 2023-02-07
IL268030B2 (en) 2023-02-01
TWI820013B (zh) 2023-11-01
AU2018210770A1 (en) 2019-08-15
RU2019126456A3 (OSRAM) 2021-02-26
MX2019008695A (es) 2019-09-11
WO2018136265A1 (en) 2018-07-26
AR110740A1 (es) 2019-05-02
CA3051206A1 (en) 2018-07-26
TW201827435A (zh) 2018-08-01
AU2018210770B2 (en) 2022-03-24
AU2022204275A1 (en) 2022-07-07
KR20190111079A (ko) 2019-10-01
CN110446709A (zh) 2019-11-12
BR112019015075A2 (pt) 2020-03-10
CN110446709B (zh) 2023-09-12
US20200017511A1 (en) 2020-01-16
RU2019126456A (ru) 2021-02-24
IL268030A (en) 2019-09-26
MX2023004037A (es) 2023-04-27
KR102665763B1 (ko) 2024-05-10
CN117327075A (zh) 2024-01-02
US12365688B2 (en) 2025-07-22
IL296456A (en) 2022-11-01
US11739093B2 (en) 2023-08-29
JP2020506178A (ja) 2020-02-27
US20240199616A1 (en) 2024-06-20
IL268030B (en) 2022-10-01
EP3571199A1 (en) 2019-11-27
SG11201906209SA (en) 2019-08-27

Similar Documents

Publication Publication Date Title
JP7240319B2 (ja) アロステリックshp2阻害剤としての二環式化合物
JP7240320B2 (ja) アロステリックshp2阻害剤としてのピリジン化合物
US11673901B2 (en) Polycyclic compounds as allosteric SHP2 inhibitors
JP7358387B2 (ja) Mtor阻害剤としてのc40-、c28-およびc-32-連結ラパマイシン類似体
CN111448190B (zh) 取代的吲哚化合物
JP7304352B2 (ja) 6-アザインドール化合物
JP2019527728A (ja) アロステリックshp2阻害剤としての2,5−二置換3−メチルピラジンおよび2,5,6−三置換3−メチルピラジン
RU2776846C2 (ru) Бициклические соединения в качестве аллостерических ингибиторов shp2
BR112019000494B1 (pt) 3-metil pirazinas 2,5-dissubstituídas e 3-metil pirazinas 2,5,6- trissubstituídas, composição farmacêutica e seus usos como inibidores de shp2 alostéricos
BR122024024795A2 (pt) 3-metil pirazinas 2,5-dissubstituídas e 3-metil pirazinas 2,5,6- trissubstituídas, composição farmacêutica e seus usos como inibidores de shp2 alostéricos

Legal Events

Date Code Title Description
A521 Request for written amendment filed

Free format text: JAPANESE INTERMEDIATE CODE: A523

Effective date: 20201223

A621 Written request for application examination

Free format text: JAPANESE INTERMEDIATE CODE: A621

Effective date: 20201223

A977 Report on retrieval

Free format text: JAPANESE INTERMEDIATE CODE: A971007

Effective date: 20211125

A131 Notification of reasons for refusal

Free format text: JAPANESE INTERMEDIATE CODE: A131

Effective date: 20211207

A521 Request for written amendment filed

Free format text: JAPANESE INTERMEDIATE CODE: A523

Effective date: 20220302

A02 Decision of refusal

Free format text: JAPANESE INTERMEDIATE CODE: A02

Effective date: 20220726

A521 Request for written amendment filed

Free format text: JAPANESE INTERMEDIATE CODE: A523

Effective date: 20221125

C60 Trial request (containing other claim documents, opposition documents)

Free format text: JAPANESE INTERMEDIATE CODE: C60

Effective date: 20221125

A911 Transfer to examiner for re-examination before appeal (zenchi)

Free format text: JAPANESE INTERMEDIATE CODE: A911

Effective date: 20221207

C21 Notice of transfer of a case for reconsideration by examiners before appeal proceedings

Free format text: JAPANESE INTERMEDIATE CODE: C21

Effective date: 20221213

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: 20230104

A601 Written request for extension of time

Free format text: JAPANESE INTERMEDIATE CODE: A601

Effective date: 20230120

A61 First payment of annual fees (during grant procedure)

Free format text: JAPANESE INTERMEDIATE CODE: A61

Effective date: 20230303

R150 Certificate of patent or registration of utility model

Ref document number: 7240319

Country of ref document: JP

Free format text: JAPANESE INTERMEDIATE CODE: R150