JP2017528488A - がんの処置のための併用療法 - Google Patents

がんの処置のための併用療法 Download PDF

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Publication number
JP2017528488A
JP2017528488A JP2017515060A JP2017515060A JP2017528488A JP 2017528488 A JP2017528488 A JP 2017528488A JP 2017515060 A JP2017515060 A JP 2017515060A JP 2017515060 A JP2017515060 A JP 2017515060A JP 2017528488 A JP2017528488 A JP 2017528488A
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Prior art keywords
alkyl
compound
inhibitor
kras
additional therapeutic
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JP2017528488A5 (enExample
Inventor
マシュー ロバート ジェーンズ，
マシュー ロバート ジェーンズ，
マシュー ピーター パトリセリ，
マシュー ピーター パトリセリ，
リアンシェン リー，
リアンシェン リー，
ピンダ レン，
ピンダ レン，
イー リウ，
イー リウ，
Original Assignee
アラクセス ファーマ エルエルシー
アラクセス ファーマ エルエルシー
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Publication of JP2017528488A publication Critical patent/JP2017528488A/ja
Publication of JP2017528488A5 publication Critical patent/JP2017528488A5/ja
Priority to JP2022142265A priority Critical patent/JP2022168089A/ja
Priority to JP2024106300A priority patent/JP2024114976A/ja
Priority to JP2024106299A priority patent/JP2024114975A/ja
Withdrawn legal-status Critical Current

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    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495—Heterocyclic 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
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/517—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with carbocyclic ring systems, e.g. quinazoline, perimidine
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/335—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin
    • A61K31/337—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having four-membered rings, e.g. taxol
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435—Heterocyclic 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
    • A61K31/47—Quinolines; Isoquinolines
    • A61K31/4738—Quinolines; Isoquinolines ortho- or peri-condensed with heterocyclic ring systems
    • A61K31/4745—Quinolines; Isoquinolines ortho- or peri-condensed with heterocyclic ring systems condensed with ring systems having nitrogen as a ring hetero atom, e.g. phenantrolines
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495—Heterocyclic 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
    • A61K31/496—Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/18—Drugs for disorders of the alimentary tract or the digestive system for pancreatic disorders, e.g. pancreatic enzymes
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A61P35/02—Antineoplastic agents specific for leukemia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00

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  • Health & Medical Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Epidemiology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Organic Chemistry (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Hematology (AREA)
  • Oncology (AREA)
  • Pulmonology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Measuring Or Testing Involving Enzymes Or Micro-Organisms (AREA)
  • Medicines Containing Antibodies Or Antigens For Use As Internal Diagnostic Agents (AREA)
JP2017515060A 2014-09-18 2015-09-18 がんの処置のための併用療法 Withdrawn JP2017528488A (ja)

Priority Applications (3)

Application Number Priority Date Filing Date Title
JP2022142265A JP2022168089A (ja) 2014-09-18 2022-09-07 がんの処置のための併用療法
JP2024106300A JP2024114976A (ja) 2014-09-18 2024-07-01 がんの処置のための併用療法
JP2024106299A JP2024114975A (ja) 2014-09-18 2024-07-01 がんの処置のための併用療法

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
US201462052332P 2014-09-18 2014-09-18
US62/052,332 2014-09-18
US201562195633P 2015-07-22 2015-07-22
US62/195,633 2015-07-22
PCT/US2015/051030 WO2016044772A1 (en) 2014-09-18 2015-09-18 Combination therapies for treatment of cancer

Related Child Applications (1)

Application Number Title Priority Date Filing Date
JP2022142265A Division JP2022168089A (ja) 2014-09-18 2022-09-07 がんの処置のための併用療法

Publications (2)

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JP2017528488A true JP2017528488A (ja) 2017-09-28
JP2017528488A5 JP2017528488A5 (enExample) 2018-11-01

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Family Applications (4)

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JP2017515060A Withdrawn JP2017528488A (ja) 2014-09-18 2015-09-18 がんの処置のための併用療法
JP2022142265A Withdrawn JP2022168089A (ja) 2014-09-18 2022-09-07 がんの処置のための併用療法
JP2024106300A Pending JP2024114976A (ja) 2014-09-18 2024-07-01 がんの処置のための併用療法
JP2024106299A Pending JP2024114975A (ja) 2014-09-18 2024-07-01 がんの処置のための併用療法

Family Applications After (3)

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JP2022142265A Withdrawn JP2022168089A (ja) 2014-09-18 2022-09-07 がんの処置のための併用療法
JP2024106300A Pending JP2024114976A (ja) 2014-09-18 2024-07-01 がんの処置のための併用療法
JP2024106299A Pending JP2024114975A (ja) 2014-09-18 2024-07-01 がんの処置のための併用療法

Country Status (8)

Country Link
US (2) US10111874B2 (enExample)
EP (1) EP3193851B1 (enExample)
JP (4) JP2017528488A (enExample)
ES (1) ES2835729T3 (enExample)
JO (1) JO3556B1 (enExample)
TW (1) TWI694837B (enExample)
UY (1) UY36307A (enExample)
WO (1) WO2016044772A1 (enExample)

Cited By (17)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2018513853A (ja) * 2015-04-10 2018-05-31 アラクセス ファーマ エルエルシー 置換キナゾリン化合物およびその使用方法
JP2020105162A (ja) * 2018-11-19 2020-07-09 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
JP2021505640A (ja) * 2018-10-15 2021-02-18 イーライ リリー アンド カンパニー Ｋｒａｓ ｇ１２ｃ阻害剤
JP2021100960A (ja) * 2016-12-22 2021-07-08 アムジエン・インコーポレーテツド 肺がん、膵臓がん、または大腸がんを治療するためのＫＲＡＳ Ｇ１２Ｃ阻害剤としての、ベンズイソチアゾール、イソチアゾロ［３，４−ｂ］ピリジン、キナゾリン、フタラジン、ピリド［２，３−ｄ］ピリダジンおよびピリド［２，３−ｄ］ピリミジン誘導体
JP2021521194A (ja) * 2018-05-04 2021-08-26 アムジエン・インコーポレーテツド ＫＲａｓ Ｇ１２Ｃ阻害剤及びそれを使用する方法
JP2021532061A (ja) * 2018-05-08 2021-11-25 アストラゼネカ・アクチエボラーグAstrazeneca Aktiebolag 四環式ヘテロアリール化合物
JP2022500385A (ja) * 2018-09-10 2022-01-04 ミラティ セラピューティクス， インコーポレイテッド 組み合わせ療法
JP2022500381A (ja) * 2018-09-10 2022-01-04 ミラティ セラピューティクス， インコーポレイテッド 組み合わせ療法
JP2022500379A (ja) * 2018-09-10 2022-01-04 ミラティ セラピューティクス， インコーポレイテッド 組み合わせ療法
JP2022500384A (ja) * 2018-09-10 2022-01-04 ミラティ セラピューティクス， インコーポレイテッド 組み合わせ療法
JP2022517222A (ja) * 2019-01-10 2022-03-07 ミラティ セラピューティクス， インコーポレイテッド Ｋｒａｓ ｇ１２ｃ阻害剤
JP2022546043A (ja) * 2019-08-29 2022-11-02 ミラティ セラピューティクス， インコーポレイテッド Ｋｒａｓ ｇ１２ｄ阻害剤
JP2023505056A (ja) * 2019-11-27 2023-02-08 ターニング・ポイント・セラピューティクス・インコーポレイテッド ジアリール大環状化合物を含む併用療法
JP2023550028A (ja) * 2020-11-13 2023-11-30 ジェネンテック， インコーポレイテッド 固形腫瘍を治療するためのｋｒａｓｇ１２ｃ阻害剤及びｖｅｇｆ阻害剤を含む方法及び組成物
JP2024500326A (ja) * 2020-12-08 2024-01-09 ジェネンテック， インコーポレイテッド 固形腫瘍を治療するためのｋｒａｓｇ１２ｃ阻害剤及びｅｇｆｒ阻害剤を含む方法及び組成物
JP2024526949A (ja) * 2021-07-23 2024-07-19 セラス， インコーポレイテッド Ｒａｓの阻害のための組成物及び方法
JP7863642B2 (ja) 2019-08-29 2026-05-21 ミラティ セラピューティクス， インコーポレイテッド Ｋｒａｓ ｇ１２ｄ阻害剤

Families Citing this family (136)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US9745319B2 (en) 2013-03-15 2017-08-29 Araxes Pharma Llc Irreversible covalent inhibitors of the GTPase K-Ras G12C
US9227978B2 (en) 2013-03-15 2016-01-05 Araxes Pharma Llc Covalent inhibitors of Kras G12C
JO3805B1 (ar) 2013-10-10 2021-01-31 Araxes Pharma Llc مثبطات كراس جي12سي
EP3126520B1 (en) * 2014-04-04 2021-06-09 Amgen, Inc. Amg-337 for use in the treatment of cancers having a met amplification
JO3556B1 (ar) 2014-09-18 2020-07-05 Araxes Pharma Llc علاجات مدمجة لمعالجة السرطان
WO2016049568A1 (en) 2014-09-25 2016-03-31 Araxes Pharma Llc Methods and compositions for inhibition of ras
JP2017528498A (ja) 2014-09-25 2017-09-28 アラクセス ファーマ エルエルシー Ｋｒａｓ ｇ１２ｃ変異体タンパク質のインヒビター
EP3283462B1 (en) 2015-04-15 2020-12-02 Araxes Pharma LLC Fused-tricyclic inhibitors of kras and methods of use thereof
MX379383B (es) * 2015-07-21 2025-03-10 Guangzhou Maxinovel Pharmaceuticals Co Ltd Compuesto de pirimidina de anillo fusionado, intermediario y método de preparación, composición y uso del mismo.
US10144724B2 (en) * 2015-07-22 2018-12-04 Araxes Pharma Llc Substituted quinazoline compounds and methods of use thereof
US10689356B2 (en) 2015-09-28 2020-06-23 Araxes Pharma Llc Inhibitors of KRAS G12C mutant proteins
EP3356349A1 (en) 2015-09-28 2018-08-08 Araxes Pharma LLC Inhibitors of kras g12c mutant proteins
EP3356351A1 (en) 2015-09-28 2018-08-08 Araxes Pharma LLC Inhibitors of kras g12c mutant proteins
WO2017058728A1 (en) 2015-09-28 2017-04-06 Araxes Pharma Llc Inhibitors of kras g12c mutant proteins
WO2017058792A1 (en) 2015-09-28 2017-04-06 Araxes Pharma Llc Inhibitors of kras g12c mutant proteins
EP3356354A1 (en) 2015-09-28 2018-08-08 Araxes Pharma LLC Inhibitors of kras g12c mutant proteins
EP3356347A1 (en) 2015-09-28 2018-08-08 Araxes Pharma LLC Inhibitors of kras g12c mutant proteins
WO2017070256A2 (en) 2015-10-19 2017-04-27 Araxes Pharma Llc Method for screening inhibitors of ras
EP3162875B1 (en) * 2015-10-30 2018-05-23 Merck Patent GmbH Polymerisable compounds and the use thereof in liquid-crystal displays
EP3377481A1 (en) 2015-11-16 2018-09-26 Araxes Pharma LLC 2-substituted quinazoline compounds comprising a substituted heterocyclic group and methods of use thereof
WO2017100546A1 (en) 2015-12-09 2017-06-15 Araxes Pharma Llc Methods for preparation of quinazoline derivatives
JP7114076B2 (ja) 2015-12-22 2022-08-08 シャイ・セラピューティクス・エルエルシー がん及び炎症性疾患の処置のための化合物
US10822312B2 (en) 2016-03-30 2020-11-03 Araxes Pharma Llc Substituted quinazoline compounds and methods of use
CN109843856B (zh) 2016-05-18 2023-05-02 米拉蒂治疗股份有限公司 Kras g12c抑制剂
WO2017214468A1 (en) 2016-06-09 2017-12-14 Tien Yang Der Nanodroplet compositions for the efficient delivery of anti-cancer agents
US10646488B2 (en) 2016-07-13 2020-05-12 Araxes Pharma Llc Conjugates of cereblon binding compounds and G12C mutant KRAS, HRAS or NRAS protein modulating compounds and methods of use thereof
EP3519402A1 (en) * 2016-09-29 2019-08-07 Araxes Pharma LLC Inhibitors of kras g12c mutant proteins
US10377743B2 (en) 2016-10-07 2019-08-13 Araxes Pharma Llc Inhibitors of RAS and methods of use thereof
US10898487B2 (en) 2016-12-22 2021-01-26 Boehringer Ingelheim International Gmbh Benzylamino substituted quinazolines and derivatives as SOS1 inhibitors
CN110291089B (zh) 2017-01-17 2022-05-27 海帕瑞吉尼克斯股份有限公司 用于促进肝再生或者减少或预防肝细胞死亡的蛋白激酶抑制剂
US11358959B2 (en) 2017-01-26 2022-06-14 Araxes Pharma Llc Benzothiophene and benzothiazole compounds and methods of use thereof
WO2018140513A1 (en) 2017-01-26 2018-08-02 Araxes Pharma Llc 1-(3-(6-(3-hydroxynaphthalen-1-yl)benzofuran-2-yl)azetidin-1yl)prop-2-en-1-one derivatives and similar compounds as kras g12c modulators for treating cancer
US11136308B2 (en) * 2017-01-26 2021-10-05 Araxes Pharma Llc Substituted quinazoline and quinazolinone compounds and methods of use thereof
EP3573954A1 (en) 2017-01-26 2019-12-04 Araxes Pharma LLC Fused bicyclic benzoheteroaromatic compounds and methods of use thereof
CN110382482A (zh) 2017-01-26 2019-10-25 亚瑞克西斯制药公司 稠合的杂-杂二环化合物及其使用方法
ES2905676T3 (es) 2017-05-22 2022-04-11 Amgen Inc Inhibidores de KRAS G12C y métodos para su uso
CN110869358A (zh) * 2017-05-25 2020-03-06 亚瑞克西斯制药公司 Kras的共价抑制剂
CN110831933A (zh) * 2017-05-25 2020-02-21 亚瑞克西斯制药公司 喹唑啉衍生物作为突变kras、hras或nras的调节剂
JP2020521741A (ja) * 2017-05-25 2020-07-27 アラクセス ファーマ エルエルシー がんの処置のための化合物およびその使用の方法
CA3066939A1 (en) 2017-06-21 2018-12-27 SHY Therapeutics LLC Compounds that interact with the ras superfamily for the treatment of cancers, inflammatory diseases, rasopathies, and fibrotic disease
CN111051306B (zh) 2017-09-08 2023-01-03 美国安进公司 Kras g12c的抑制剂及其使用方法
US10647715B2 (en) 2017-11-15 2020-05-12 Mirati Therapeutics, Inc. KRas G12C inhibitors
KR102861303B1 (ko) * 2017-11-15 2025-09-17 미라티 테라퓨틱스, 인크. Ｋｒａｓ ｇ12ｃ 억제제
ES2944306T3 (es) 2017-12-21 2023-06-20 Boehringer Ingelheim Int Piridopirimidinonas sustituidas por bencilamino y derivados como inhibidores de SOS1
GB201801128D0 (en) * 2018-01-24 2018-03-07 Univ Oxford Innovation Ltd Compounds
GB201801130D0 (en) * 2018-01-24 2018-03-07 Univ Oxford Innovation Ltd Compounds
ES2995514T3 (en) 2018-05-04 2025-02-10 Amgen Inc Kras g12c inhibitors and methods of using the same
WO2019217307A1 (en) 2018-05-07 2019-11-14 Mirati Therapeutics, Inc. Kras g12c inhibitors
EP3790886B1 (en) 2018-05-10 2024-06-26 Amgen Inc. Kras g12c inhibitors for the treatment of cancer
AU2019278998B2 (en) 2018-06-01 2023-11-09 Amgen Inc. KRAS G12C inhibitors and methods of using the same
MX2020012204A (es) 2018-06-11 2021-03-31 Amgen Inc Inhibidores de kras g12c para tratar el cáncer.
CA3100390A1 (en) 2018-06-12 2020-03-12 Amgen Inc. Kras g12c inhibitors encompassing piperazine ring and use thereof in the treatment of cancer
BR112021001709A2 (pt) 2018-08-01 2021-05-04 Araxes Pharma Llc compostos espiro heterocíclicos e métodos de uso dos mesmos para o tratamento de câncer
CR20210083A (es) 2018-08-16 2021-04-19 Hoffmann La Roche Compuestos de anillo fusionado
ES3004338T3 (en) * 2018-09-10 2025-03-12 Mirati Therapeutics Inc Combination therapies
TWI831855B (zh) 2018-10-26 2024-02-11 日商大鵬藥品工業股份有限公司 新穎吲唑化合物或其鹽
ES3004042T3 (en) * 2018-11-09 2025-03-11 Hoffmann La Roche Fused ring compounds
JP7516029B2 (ja) 2018-11-16 2024-07-16 アムジエン・インコーポレーテツド Ｋｒａｓ ｇ１２ｃ阻害剤化合物の重要な中間体の改良合成法
CA3117222A1 (en) 2018-11-19 2020-05-28 Amgen Inc. Kras g12c inhibitors and methods of using the same
CA3112129A1 (en) 2018-12-05 2020-06-11 Mirati Therapeutics, Inc. Combination therapies
EP3898609A1 (en) 2018-12-19 2021-10-27 Shy Therapeutics LLC Compounds that interact with the ras superfamily for the treatment of cancers, inflammatory diseases, rasopathies, and fibrotic disease
EP3919483A4 (en) * 2019-01-29 2022-02-09 Brightgene Bio-medical Technology Co., Ltd. HETEROCYCLIC BENZOPYRIDONE COMPOUND AND USE THEREOF
CN111187835B (zh) * 2019-02-02 2023-03-31 中国科学院上海营养与健康研究所 胰腺癌的靶点erbb2及其在诊断和治疗中的应用
US20220152026A1 (en) 2019-02-12 2022-05-19 Novartis Ag Pharmaceutical combination comprising tno155 and a krasg12c inhibitor
CA3134613A1 (en) 2019-04-02 2020-10-08 Aligos Therapeutics, Inc. Compounds targeting prmt5
US12528796B2 (en) * 2019-04-15 2026-01-20 Tosk, Inc. Modulators of RAS GTPase
EP3738593A1 (en) 2019-05-14 2020-11-18 Amgen, Inc Dosing of kras inhibitor for treatment of cancers
EP3972978A4 (en) * 2019-05-20 2023-04-26 California Institute Of Technology KRAS G12C INHIBITORS AND THEIR USES
CN114144414B (zh) 2019-05-21 2025-11-07 美国安进公司 固态形式
US20220227729A1 (en) 2019-05-21 2022-07-21 Bayer Aktiengesellschaft Identification and use of kras inhibitors
EP3972972A1 (en) 2019-05-21 2022-03-30 Amgen Inc. Solid state forms
WO2020239123A1 (zh) * 2019-05-31 2020-12-03 上海翰森生物医药科技有限公司 芳香杂环类衍生物调节剂、其制备方法和应用
CN112552294B (zh) * 2019-09-10 2023-12-19 上海翰森生物医药科技有限公司 含哌嗪杂环类衍生物抑制剂、其制备方法和应用
CN112047948B (zh) * 2019-06-06 2022-08-16 山东轩竹医药科技有限公司 Kras突变体抑制剂
CN112300194B (zh) * 2019-07-30 2022-01-14 上海凌达生物医药有限公司 一类稠环吡啶酮类化合物、制备方法和用途
BR112022005193A2 (pt) * 2019-09-20 2022-08-16 Shanghai Jemincare Pharmaceuticals Co Ltd Composto de piridona fundido, método de preparação do mesmo e uso do mesmo
US12122787B2 (en) 2019-09-20 2024-10-22 Shanghai Jemincare Pharmaceuticals Co., Ltd Fused pyridone compound, and preparation method therefor and use thereof
CN114761012B (zh) 2019-09-24 2025-03-21 米拉蒂治疗股份有限公司 组合疗法
CA3158793A1 (en) 2019-10-28 2021-05-06 Merck Sharp & Dohme Corp. Small molecule inhibitors of kras g12c mutant
CN112778284B (zh) * 2019-11-01 2022-04-05 四川海思科制药有限公司 一种嘧啶并环衍生物及其在医药上的应用
PE20230249A1 (es) 2019-11-08 2023-02-07 Revolution Medicines Inc Compuestos de heteroarilo biciclicos y usos de estos
CN110698378B (zh) * 2019-11-19 2021-03-19 上海皓元生物医药科技有限公司 2-(羟基-(甲基环丙基)苯基氨基)-1-哌嗪基乙酮衍生物的制备方法
TW202133856A (zh) * 2019-11-27 2021-09-16 美商特普醫葯公司 涉及二芳基巨環化合物之組合療法
EP4065231A1 (en) * 2019-11-27 2022-10-05 Revolution Medicines, Inc. Covalent ras inhibitors and uses thereof
US12478621B2 (en) 2019-11-28 2025-11-25 Deutsches Krebsforschungszentrum Substituted aminoquinolones as dgkalpha inhibitors for immune activation
WO2021105116A1 (en) * 2019-11-28 2021-06-03 Bayer Aktiengesellschaft Substituted aminoquinolones as dgkalpha inhibitors for immune activation
WO2021106230A1 (ja) 2019-11-29 2021-06-03 大鵬薬品工業株式会社 新規なフェノール化合物又はその塩
WO2021113595A1 (en) * 2019-12-06 2021-06-10 Beta Pharma, Inc. Phosphorus derivatives as kras inhibitors
RS63719B1 (sr) 2019-12-11 2022-11-30 Lilly Co Eli Kras g12c inhibitori
KR20220130126A (ko) 2019-12-20 2022-09-26 미라티 테라퓨틱스, 인크. Sos1 억제제
WO2021138391A1 (en) 2019-12-30 2021-07-08 Tyra Biosciences, Inc. Indazole compounds
EP4087840A4 (en) 2020-01-10 2024-01-10 Immuneering Corporation Mek inhibitors and therapeutic uses thereof
TW202140450A (zh) * 2020-02-24 2021-11-01 大陸商泰勵生物科技（上海）有限公司 用於癌症治療的ｋｒａｓ抑制劑
CN111358794A (zh) * 2020-03-13 2020-07-03 南通大学 一种用于治疗非小细胞肺癌的药物或试剂盒
WO2021218110A1 (zh) * 2020-04-29 2021-11-04 上海凌达生物医药有限公司 一类苯并噻唑基联芳基类化合物、制备方法和用途
TW202200563A (zh) * 2020-04-29 2022-01-01 中國商北京泰德製藥股份有限公司 喹喔啉酮衍生物作為kras g12c突變蛋白的不可逆抑制劑
WO2021259331A1 (zh) * 2020-06-24 2021-12-30 南京明德新药研发有限公司 八元含n杂环类化合物
US12286431B2 (en) 2020-09-11 2025-04-29 Mirati Therapeutics, Inc. Crystalline forms of a KRas G12C inhibitor
TWI880049B (zh) 2020-12-04 2025-04-11 美商美國禮來大藥廠 Kras g12c抑制劑
US12398154B2 (en) 2020-12-15 2025-08-26 Mirati Therapeutics, Inc. Azaquinazoline pan-KRas inhibitors
EP4262803A4 (en) 2020-12-16 2025-03-12 Mirati Therapeutics, Inc. Tetrahydropyridopyrimidine pan-kras inhibitors
EP4267250A1 (en) 2020-12-22 2023-11-01 Qilu Regor Therapeutics Inc. Sos1 inhibitors and uses thereof
US20250177399A1 (en) * 2021-01-29 2025-06-05 Mirati Therapeutics, Inc. Combination therapies
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
CN115703775A (zh) * 2021-08-06 2023-02-17 苏州阿尔脉生物科技有限公司 一种kras突变体g12c抑制剂及其制备方法和应用
CN115813930A (zh) * 2021-08-17 2023-03-21 赛诺哈勃药业（成都）有限公司 大环化合物与mek抑制剂联用在用于治疗疾病药物中的用途
CN117858878A (zh) * 2021-08-18 2024-04-09 北京加科思新药研发有限公司 N-环丙基吡啶并[4,3-d]嘧啶-4-胺衍生物及其用途
EP4395769A1 (en) 2021-09-01 2024-07-10 Novartis AG Pharmaceutical combinations comprising a tead inhibitor and uses thereof for the treatment of cancers
MX2024003363A (es) * 2021-09-22 2024-04-04 Sichuan Huiyu Pharmaceutical Co Ltd Derivado de piridina y uso del mismo.
US20250249003A1 (en) 2021-10-05 2025-08-07 Mirati Therapeutics, Inc. Combinations of kras g12d inhibitors with irinotecan and related methods of treatment
WO2023138583A1 (zh) * 2022-01-21 2023-07-27 上海湃隆生物科技有限公司 杂环类化合物、药物组合物及其应用
US20250154170A1 (en) 2022-02-10 2025-05-15 Bayer Aktiengesellschaft Fused pyrimidines as kras inhibitors
CN114456110A (zh) * 2022-03-02 2022-05-10 重庆南松凯博生物制药有限公司 一种7-氯-4-羟基喹啉-3-羧酸的合成方法
WO2023165581A1 (zh) * 2022-03-03 2023-09-07 四川汇宇制药股份有限公司 一种吡啶类衍生物及其用途
WO2023168036A1 (en) 2022-03-04 2023-09-07 Eli Lilly And Company Method of treatment including kras g12c inhibitors and shp2 inhibitors
EP4504209A1 (en) 2022-04-08 2025-02-12 Eli Lilly and Company Method of treatment including kras g12c inhibitors and aurora a inhibitors
WO2023199180A1 (en) 2022-04-11 2023-10-19 Novartis Ag Therapeutic uses of a krasg12c inhibitor
US12600722B2 (en) 2022-07-18 2026-04-14 Incyte Corporation Tetracyclic compounds as DGK inhibitors
US12600723B2 (en) 2022-07-18 2026-04-14 Incyte Corporation Tetracyclic compounds as DGK inhibitors
KR20250060956A (ko) 2022-08-05 2025-05-07 컴쿼트 바이오사이언시즈 인크. 헤테로환 화합물 및 이의 용도
WO2024109233A1 (zh) * 2022-11-22 2024-05-30 四川汇宇制药股份有限公司 一种嘧啶并芳环化合物及其制备方法和用途
CN120882709A (zh) * 2023-03-13 2025-10-31 四川汇宇制药股份有限公司 喹唑啉衍生物的盐型、晶型、其制备方法及应用
CN121219016A (zh) 2023-06-02 2025-12-26 第一三共株式会社 抗-her3抗体-药物缀合物和rasg12c抑制剂的组合
GB2631397A (en) 2023-06-28 2025-01-08 Sevenless Therapeutics Ltd New treatments for pain
WO2025016899A1 (en) 2023-07-19 2025-01-23 Bayer Aktiengesellschaft Spirocyclic compounds for the treatment of cancer
WO2025026903A1 (en) 2023-07-31 2025-02-06 Bayer Aktiengesellschaft Imidazo pyrimidine compounds for the treatment of cancer
GB2633813A (en) 2023-09-21 2025-03-26 Sevenless Therapeutics Ltd New treatments for pain
WO2025067453A1 (zh) * 2023-09-27 2025-04-03 健艾仕生物医药有限公司 一种含kras抑制剂的药物组合、含其的组合物及其应用
WO2025085748A1 (en) 2023-10-20 2025-04-24 Merck Sharp & Dohme Llc Small molecule inhibitors of kras proteins
WO2025083426A1 (en) 2023-10-20 2025-04-24 Sevenless Therapeutics Limited New treatments for pain
WO2025137507A1 (en) 2023-12-22 2025-06-26 Regor Pharmaceuticals, Inc. Sos1 inhibitors and uses thereof
WO2025146548A1 (en) 2024-01-04 2025-07-10 Sevenless Therapeutics Limited Sos1 inhibitors useful to treat pain and cancer
WO2026035947A1 (en) 2024-08-07 2026-02-12 Tesseract Medicines Us, Llc Kras-targeting covalent-induced drug conjugates comprising a topoisomerase payload
WO2026035945A1 (en) 2024-08-07 2026-02-12 Tesseract Medicines Us, Llc Covalent-induced drug conjugates targeting kras and comprising a topoisomerase payload
WO2026064520A1 (en) 2024-09-19 2026-03-26 Tesseract Medicines Us, Llc Covalent-induced drug conjugates targeting kras and comprising a tubulin inhibitor payload
WO2026064527A1 (en) 2024-09-19 2026-03-26 Tesseract Medicines Us, Llc Kras-targeting covalent-induced drug conjugates comprising a tubulin inhibitor payload

Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2013155223A1 (en) * 2012-04-10 2013-10-17 The Regents Of The University Of California Compositions and methods for treating cancer

Family Cites Families (153)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
GB939516A (en) 1961-05-29 1963-10-16 British Drug Houses Ltd Sulphonyl ureas
US3702849A (en) 1967-10-26 1972-11-14 Pfizer 4-(isoquinolin-1-yl) piperazine-1-carboxylic acid esters
US3752660A (en) 1971-03-15 1973-08-14 Allied Chem Chlorophenoxyacetyloxazolidone herbicides and preparation thereof
EP0094498A3 (en) 1982-05-06 1985-04-03 American Cyanamid Company Antiatherosclerotic 1-piperazine derivatives
US4439606A (en) 1982-05-06 1984-03-27 American Cyanamid Company Antiatherosclerotic 1-piperazinecarbonyl compounds
JPS59163372A (ja) 1983-03-09 1984-09-14 Showa Denko Kk ピラゾ−ル誘導体とその製造法及び除草剤
JPS60193955A (ja) 1984-03-13 1985-10-02 Mitsui Toatsu Chem Inc 環式不飽和アミド置換エ−テル化合物及びその製造方法
JPS6143190A (ja) 1984-08-06 1986-03-01 Mitsui Petrochem Ind Ltd ピリドピリミジン誘導体およびその製法
US4911920A (en) 1986-07-30 1990-03-27 Alcon Laboratories, Inc. Sustained release, comfort formulation for glaucoma therapy
FR2588189B1 (fr) 1985-10-03 1988-12-02 Merck Sharp & Dohme Composition pharmaceutique de type a transition de phase liquide-gel
US5033252A (en) 1987-12-23 1991-07-23 Entravision, Inc. Method of packaging and sterilizing a pharmaceutical product
US5052558A (en) 1987-12-23 1991-10-01 Entravision, Inc. Packaged pharmaceutical product
US5010175A (en) 1988-05-02 1991-04-23 The Regents Of The University Of California General method for producing and selecting peptides with specific properties
GB8827305D0 (en) 1988-11-23 1988-12-29 British Bio Technology Compounds
US5925525A (en) 1989-06-07 1999-07-20 Affymetrix, Inc. Method of identifying nucleotide differences
IE66205B1 (en) 1990-06-14 1995-12-13 Paul A Bartlett Polypeptide analogs
US5650489A (en) 1990-07-02 1997-07-22 The Arizona Board Of Regents Random bio-oligomer library, a method of synthesis thereof, and a method of use thereof
DK0495421T3 (da) 1991-01-15 1996-12-09 Alcon Lab Inc Anvendelse af carragenaner i topiske ophthalmiske sammensætninger
US5212162A (en) 1991-03-27 1993-05-18 Alcon Laboratories, Inc. Use of combinations gelling polysaccharides and finely divided drug carrier substrates in topical ophthalmic compositions
US6051380A (en) 1993-11-01 2000-04-18 Nanogen, Inc. Methods and procedures for molecular biological analysis and diagnostics
US6017696A (en) 1993-11-01 2000-01-25 Nanogen, Inc. Methods for electronic stringency control for molecular biological analysis and diagnostics
US5573905A (en) 1992-03-30 1996-11-12 The Scripps Research Institute Encoded combinatorial chemical libraries
US5323907A (en) 1992-06-23 1994-06-28 Multi-Comp, Inc. Child resistant package assembly for dispensing pharmaceutical medications
US5288514A (en) 1992-09-14 1994-02-22 The Regents Of The University Of California Solid phase and combinatorial synthesis of benzodiazepine compounds on a solid support
US5455258A (en) 1993-01-06 1995-10-03 Ciba-Geigy Corporation Arylsulfonamido-substituted hydroxamic acids
US5605798A (en) 1993-01-07 1997-02-25 Sequenom, Inc. DNA diagnostic based on mass spectrometry
US5858659A (en) 1995-11-29 1999-01-12 Affymetrix, Inc. Polymorphism detection
US6045996A (en) 1993-10-26 2000-04-04 Affymetrix, Inc. Hybridization assays on oligonucleotide arrays
US6068818A (en) 1993-11-01 2000-05-30 Nanogen, Inc. Multicomponent devices for molecular biological analysis and diagnostics
US5538848A (en) 1994-11-16 1996-07-23 Applied Biosystems Division, Perkin-Elmer Corp. Method for detecting nucleic acid amplification using self-quenching fluorescence probe
DE69531542T2 (de) 1994-02-07 2004-06-24 Beckman Coulter, Inc., Fullerton Ligase/polymerase-vermittelte analyse genetischer elemente von einzelnukleotid-polymorphismen und ihre verwendung in der genetischen analyse
US5593853A (en) 1994-02-09 1997-01-14 Martek Corporation Generation and screening of synthetic drug libraries
US5539083A (en) 1994-02-23 1996-07-23 Isis Pharmaceuticals, Inc. Peptide nucleic acid combinatorial libraries and improved methods of synthesis
US6309853B1 (en) 1994-08-17 2001-10-30 The Rockfeller University Modulators of body weight, corresponding nucleic acids and proteins, and diagnostic and therapeutic uses thereof
EP0786997A4 (en) 1994-10-27 1998-03-11 Merck & Co Inc MUSCARINE ANTAGONISTS
US5863949A (en) 1995-03-08 1999-01-26 Pfizer Inc Arylsulfonylamino hydroxamic acid derivatives
JP3053222B2 (ja) 1995-04-20 2000-06-19 ファイザー・インコーポレーテッド Ｍｍｐおよびｔｎｆ抑制剤としてのアリールスルホニルヒドロキサム酸誘導体
FR2734816B1 (fr) 1995-05-31 1997-07-04 Adir Nouveaux aryl (alkyl) propylamides, leur procede de preparation et les compositions pharmaceutiques qui les contiennent
DE69638269D1 (de) 1995-06-14 2010-11-18 Univ California Hochaffine humane antikörper gegen tumorantigene
ATE225343T1 (de) 1995-12-20 2002-10-15 Hoffmann La Roche Matrix-metalloprotease inhibitoren
EP0818442A3 (en) 1996-07-12 1998-12-30 Pfizer Inc. Cyclic sulphone derivatives as inhibitors of metalloproteinases and of the production of tumour necrosis factor
CA2260898C (en) 1996-07-18 2002-05-14 Pfizer Limited Phosphinate based inhibitors of matrix metalloproteases
PL331895A1 (en) 1996-08-23 1999-08-16 Pfizer Arylosulphonylamino derivatives of hydroxamic acid
US5777324A (en) 1996-09-19 1998-07-07 Sequenom, Inc. Method and apparatus for maldi analysis
DE69730151T2 (de) 1997-01-06 2005-08-04 Pfizer Inc. Cyclische sulfonderivate
AU721748B2 (en) 1997-02-03 2000-07-13 Pfizer Products Inc. Arylsulfonylamino hydroxamic acid derivatives
GB9702194D0 (en) 1997-02-04 1997-03-26 Lilly Co Eli Sulphonide derivatives
CA2279863A1 (en) 1997-02-07 1998-08-13 Pfizer Inc. N-hydroxy-beta-sulfonyl-propionamide derivatives and their use as inhibitors of matrix metalloproteinases
WO1998034918A1 (en) 1997-02-11 1998-08-13 Pfizer Inc. Arylsulfonyl hydroxamic acid derivatives
US5919626A (en) 1997-06-06 1999-07-06 Orchid Bio Computer, Inc. Attachment of unmodified nucleic acids to silanized solid phase surfaces
AU8253598A (en) 1997-06-17 1999-01-04 Schering Corporation Novel n-substituted urea inhibitors of farnesyl-protein transferase
ID23668A (id) 1997-08-08 2000-05-11 Pfizer Prod Inc Turunan asam ariloksiarilsulfonilamino hidroksamat
GB9725782D0 (en) 1997-12-05 1998-02-04 Pfizer Ltd Therapeutic agents
US6903118B1 (en) 1997-12-17 2005-06-07 Klinge Pharma Gmbh Piperazinyl-substituted pyridylalkane, alkene and alkine carboxamides
GB9801690D0 (en) 1998-01-27 1998-03-25 Pfizer Ltd Therapeutic agents
PA8469401A1 (es) 1998-04-10 2000-05-24 Pfizer Prod Inc Derivados biciclicos del acido hidroxamico
PA8469501A1 (es) 1998-04-10 2000-09-29 Pfizer Prod Inc Hidroxamidas del acido (4-arilsulfonilamino)-tetrahidropiran-4-carboxilico
US7060431B2 (en) 1998-06-24 2006-06-13 Illumina, Inc. Method of making and decoding of array sensors with microspheres
DK1004578T3 (da) 1998-11-05 2004-06-28 Pfizer Prod Inc 5-oxo-pyrrolidin-2-carboxylsyrehydroxamidderivater
US6429027B1 (en) 1998-12-28 2002-08-06 Illumina, Inc. Composite arrays utilizing microspheres
EP1081137A1 (en) 1999-08-12 2001-03-07 Pfizer Products Inc. Selective inhibitors of aggrecanase in osteoarthritis treatment
CA2384838C (en) 1999-09-13 2006-07-18 Nugen Technologies, Inc. Methods and compositions for linear isothermal amplification of polynucleotide sequences
BR0111280A (pt) 2000-06-05 2003-06-10 Dong A Pharm Co Ltd Novos derivados de oxazolidinona e um processo para a preparação dos mesmos
EP1964839A3 (en) 2000-08-18 2008-11-05 Millennium Pharmaceuticals, Inc. Quinazoline derivatives as kinase inhibitors
US6890747B2 (en) 2000-10-23 2005-05-10 Warner-Lambert Company Phosphoinositide 3-kinases
US20020169300A1 (en) * 2001-01-30 2002-11-14 Waterman Marian L. Method of detection and treatment of colon cancer by analysis of beta-catenin-sensitive isoforms of lymphoid enhancer factor-1
ATE449090T1 (de) 2001-07-02 2009-12-15 High Point Pharmaceuticals Llc Substituierte piperazin- und diazepanderivate zur verwendung als histamin h3 rezeptormodulatoren
JP4608852B2 (ja) 2002-10-15 2011-01-12 チッソ株式会社 液晶性ビニルケトン誘導体およびその重合体
CA2516234A1 (en) 2003-02-21 2004-09-02 Pfizer Inc. N-heterocyclyl-substituted amino-thiazole derivatives as protein kinase inhibitors
JP4923380B2 (ja) 2003-12-22 2012-04-25 Ｊｎｃ株式会社 低屈折率異方性化合物、組成物およびそれらの重合体または重合体組成物
JP4932495B2 (ja) 2004-01-23 2012-05-16 アムゲン インコーポレイテッド 化合物及び使用方法
WO2005082892A2 (en) 2004-02-17 2005-09-09 Dr. Reddy's Laboratories Ltd. Triazole compounds as antibacterial agents and pharmaceutical compositions containing them
WO2005095327A1 (ja) 2004-03-31 2005-10-13 Ajinomoto Co., Inc. アニリン誘導体
US20060167044A1 (en) 2004-12-20 2006-07-27 Arnaiz Damian O Piperidine derivatives and their use as anti-inflammatory agents
US20090264415A2 (en) 2004-12-30 2009-10-22 Steven De Jonghe Pyrido(3,2-d)pyrimidines and pharmaceutical compositions useful for medical treatment
GB0428475D0 (en) 2004-12-30 2005-02-02 4 Aza Bioscience Nv Pyrido(3,2-D)pyrimidine derivatives and pharmaceutical compositions useful as medicines for the treatment of autoimmune disorders
JP2007016011A (ja) 2005-06-10 2007-01-25 Nippon Soda Co Ltd 抗酸化活性を有する新規な含窒素ヘテロ環化合物、及び該化合物を含有する抗酸化薬
JP2008543888A (ja) 2005-06-24 2008-12-04 ギリアード サイエンシーズ， インコーポレイテッド ピリド（３，２−ｄ）ピリミジン、およびＣ型肝炎を治療するのに有用な医薬組成物
EP1966132A2 (en) 2005-12-15 2008-09-10 Boehringer Ingelheim International Gmbh Compounds which modulate the cb2 receptor
PE20070978A1 (es) 2006-02-14 2007-11-15 Novartis Ag COMPUESTOS HETEROCICLICOS COMO INHIBIDORES DE FOSFATIDILINOSITOL 3-QUINASAS (PI3Ks)
MX2008012617A (es) 2006-03-31 2008-10-10 Novartis Ag Compuestos organicos.
US20090124636A1 (en) 2006-04-12 2009-05-14 Pfizer Inc. Chemical compounds
JP2009539937A (ja) 2006-06-16 2009-11-19 ハイ ポイント ファーマシューティカルズ，リミティド ライアビリティ カンパニー 置換型ピペリジンカルボキサミドの医薬的使用
US20080039450A1 (en) 2006-06-22 2008-02-14 Jensen Annika J Compounds
FR2903101B1 (fr) 2006-06-30 2008-09-26 Servier Lab Nouveaux derives naphtaleniques, leur procede de preparation et les compositions pharmaceutiques qui les contiennent
WO2008009078A2 (en) 2006-07-20 2008-01-24 Gilead Sciences, Inc. 4,6-dl- and 2,4,6-trisubstituted quinazoline derivatives useful for treating viral infections
CN101679261A (zh) 2007-03-09 2010-03-24 阿斯利康(瑞典)有限公司 哌嗪和哌啶mGluR5增效剂
ES2705599T3 (es) 2007-04-16 2019-03-26 Abbvie Inc Indoles sustituidos en la posición 7 como inhibidores de mcl-1
EP3269824A1 (en) 2008-03-28 2018-01-17 Pacific Biosciences Of California, Inc. Compositions and methods for nucleic acid sequencing
CA2733533C (en) 2008-08-25 2013-12-17 Irm Llc Hedgehog pathway modulators
WO2010087399A1 (ja) 2009-01-30 2010-08-05 第一三共株式会社 ウロテンシンｉｉ受容体拮抗薬
NZ595073A (en) 2009-04-20 2012-11-30 Hoffmann La Roche Proline derivatives as cathepsin inhibitors
AU2010239188B2 (en) 2009-04-22 2016-03-31 Janssen Pharmaceutica Nv Azetidinyl diamides as monoacylglycerol lipase inhibitors
EP2270002A1 (en) 2009-06-18 2011-01-05 Vereniging voor Christelijk Hoger Onderwijs, Wetenschappelijk Onderzoek en Patiëntenzorg Quinazoline derivatives as histamine H4-receptor inhibitors for use in the treatment of inflammatory disorders
KR101256018B1 (ko) 2009-08-20 2013-04-18 한국과학기술연구원 단백질 키나아제 저해활성을 갖는 1,3,6-치환된 인돌 화합물
RU2595718C2 (ru) 2009-09-09 2016-08-27 Селджен Авиломикс Рисерч,Инк. Ингибиторы pi3-киназы и их применение
AU2010339456A1 (en) 2009-12-30 2012-07-05 Celgene Avilomics Research, Inc. Ligand-directed covalent modification of protein
CN102791690B (zh) 2010-01-29 2015-12-02 大塚制药株式会社 作为抗癌药的二取代吡啶衍生物
EP2542893A2 (en) * 2010-03-03 2013-01-09 OSI Pharmaceuticals, LLC Biological markers predictive of anti-cancer response to insulin-like growth factor-1 receptor kinase inhibitors
MX2012010557A (es) 2010-03-16 2012-10-05 Merck Patent Gmbh Morfolinilquinazolinas.
CA2791020A1 (en) 2010-04-28 2011-11-03 Daiichi Sankyo Company, Limited [5,6] heterocyclic compound
TW201202230A (en) 2010-05-24 2012-01-16 Mitsubishi Tanabe Pharma Corp Novel quinazoline compound
WO2011153553A2 (en) 2010-06-04 2011-12-08 The Regents Of The University Of California Methods and compositions for kinase inhibition
CN103119439A (zh) 2010-06-08 2013-05-22 纽亘技术公司 用于多重测序的方法和组合物
US8658131B2 (en) 2010-06-21 2014-02-25 Washington University Compounds comprising 4-benzoylpiperidine as a sigma-1-selective ligand
WO2012016082A1 (en) 2010-07-30 2012-02-02 Oncotherapy Science, Inc. Quinoline derivatives and melk inhibitors containing the same
CN103068798A (zh) 2010-09-03 2013-04-24 詹森药业有限公司 作为单酰甘油脂肪酶抑制剂的二-氮杂环丁烷二酰胺
BR112013006953A2 (pt) 2010-09-29 2016-07-26 Intervet Int Bv composto, composições farmacêutica e anti-helmíntica, uso de um composto, kit, e, método de tratamento de uma doença
CN103260703A (zh) 2010-10-22 2013-08-21 詹森药业有限公司 作为单酰甘油脂肪酶抑制剂的哌啶-4-基-氮杂环丁烷二酰胺
WO2012174489A2 (en) 2011-06-15 2012-12-20 The Ohio State University Small molecule composite surfaces as inhibitors of protein-protein interactions
EA201490177A1 (ru) 2011-06-29 2014-08-29 Оцука Фармасьютикал Ко., Лтд. Хиназолины как терапевтические соединения и связанные с ними способы их применения
CN103087077B (zh) 2011-11-03 2016-05-18 上海希迈医药科技有限公司 噻吩并嘧啶和呋喃并嘧啶类衍生物、其制备方法及其在医药上的应用
US9745631B2 (en) * 2011-12-20 2017-08-29 Dana-Farber Cancer Institute, Inc. Methods for diagnosing and treating oncogenic kras-associated cancer
EP2828250B1 (en) 2012-03-19 2021-03-10 Imperial College Innovations Limited Quinazoline compounds and their use in therapy
WO2013155077A1 (en) * 2012-04-09 2013-10-17 Board Of Regents,The University Of Texas System Response markers for src inhibitor therapies
CN104685055A (zh) 2012-05-09 2015-06-03 格兰达利斯有限公司 对单核苷酸KRAS突变特异的双功能短发夹RNA(bi-shRNA)
JO3300B1 (ar) 2012-06-06 2018-09-16 Novartis Ag مركبات وتركيبات لتعديل نشاط egfr
NZ703495A (en) 2012-07-11 2018-02-23 Blueprint Medicines Corp Inhibitors of the fibroblast growth factor receptor
US20150299188A1 (en) 2012-08-24 2015-10-22 Takeda Pharmaceutical Company Limited Heterocyclic compound
WO2014159837A1 (en) 2013-03-14 2014-10-02 Convergene Llc Methods and compositions for inhibition of bromodomain-containing proteins
US9227978B2 (en) * 2013-03-15 2016-01-05 Araxes Pharma Llc Covalent inhibitors of Kras G12C
US9745319B2 (en) 2013-03-15 2017-08-29 Araxes Pharma Llc Irreversible covalent inhibitors of the GTPase K-Ras G12C
TW201524952A (zh) 2013-03-15 2015-07-01 Araxes Pharma Llc Ｋｒａｓ ｇ１２ｃ之共價抑制劑
JP6518656B2 (ja) 2013-06-13 2019-05-22 バイオデシー， インコーポレイテッド 標的生体実体を標的にする生化学実体候補をスクリーニングする方法
CN108440515B (zh) 2013-07-03 2022-05-03 卡尔约药物治疗公司 取代的苯并呋喃基和苯并噁唑基化合物及其用途
WO2015017501A1 (en) 2013-08-02 2015-02-05 Molex Incorporated Power connector
CN104418860B (zh) 2013-08-20 2016-09-07 中国科学院广州生物医药与健康研究院 嘧啶并杂环类化合物及其药用组合物和应用
JO3805B1 (ar) 2013-10-10 2021-01-31 Araxes Pharma Llc مثبطات كراس جي12سي
JP6559123B2 (ja) * 2013-10-10 2019-08-14 アラクセス ファーマ エルエルシー Ｋｒａｓｇ１２ｃの阻害剤
US9376559B2 (en) 2013-11-22 2016-06-28 Exxonmobil Chemical Patents Inc. Reverse staged impact copolymers
WO2015108992A1 (en) 2014-01-15 2015-07-23 Blueprint Medicines Corporation Heterobicyclic compounds and their use as fgfr4 receptor inhibitors
CN105916859A (zh) 2014-02-03 2016-08-31 卡迪拉保健有限公司 杂环化合物
CA3175724C (en) 2014-03-20 2024-01-09 Capella Therapeutics, Inc. Benzimidazole derivatives, and pharmaceutical compositions and methods of use thereof
PE20170331A1 (es) 2014-03-24 2017-04-28 Guangdong Zhongsheng Pharmaceutical Co Ltd Derivados quinolina como inhibidores smo
MA40074A (fr) 2014-05-30 2015-12-03 Univ Columbia Composés liant ras multivalents
JO3556B1 (ar) 2014-09-18 2020-07-05 Araxes Pharma Llc علاجات مدمجة لمعالجة السرطان
WO2016049568A1 (en) 2014-09-25 2016-03-31 Araxes Pharma Llc Methods and compositions for inhibition of ras
JP2017528498A (ja) 2014-09-25 2017-09-28 アラクセス ファーマ エルエルシー Ｋｒａｓ ｇ１２ｃ変異体タンパク質のインヒビター
WO2016049565A1 (en) 2014-09-25 2016-03-31 Araxes Pharma Llc Compositions and methods for inhibition of ras
HK1245677A1 (zh) 2015-01-23 2018-08-31 Aclaris Therapeutics, Inc. 用於治疗炎症和癌症的杂环itk抑制剂
MX382355B (es) 2015-04-10 2025-03-13 Araxes Pharma Llc Compuestos de quinazolina sustituidos y métodos de uso de los mismos.
EP3283462B1 (en) 2015-04-15 2020-12-02 Araxes Pharma LLC Fused-tricyclic inhibitors of kras and methods of use thereof
WO2017015562A1 (en) 2015-07-22 2017-01-26 Araxes Pharma Llc Substituted quinazoline compounds and their use as inhibitors of g12c mutant kras, hras and/or nras proteins
US10144724B2 (en) 2015-07-22 2018-12-04 Araxes Pharma Llc Substituted quinazoline compounds and methods of use thereof
US10689356B2 (en) 2015-09-28 2020-06-23 Araxes Pharma Llc Inhibitors of KRAS G12C mutant proteins
EP3356349A1 (en) 2015-09-28 2018-08-08 Araxes Pharma LLC Inhibitors of kras g12c mutant proteins
WO2017070256A2 (en) 2015-10-19 2017-04-27 Araxes Pharma Llc Method for screening inhibitors of ras
EP3377481A1 (en) 2015-11-16 2018-09-26 Araxes Pharma LLC 2-substituted quinazoline compounds comprising a substituted heterocyclic group and methods of use thereof
WO2017100546A1 (en) 2015-12-09 2017-06-15 Araxes Pharma Llc Methods for preparation of quinazoline derivatives
US10822312B2 (en) 2016-03-30 2020-11-03 Araxes Pharma Llc Substituted quinazoline compounds and methods of use
US10646488B2 (en) 2016-07-13 2020-05-12 Araxes Pharma Llc Conjugates of cereblon binding compounds and G12C mutant KRAS, HRAS or NRAS protein modulating compounds and methods of use thereof
EP3519402A1 (en) 2016-09-29 2019-08-07 Araxes Pharma LLC Inhibitors of kras g12c mutant proteins
US10377743B2 (en) 2016-10-07 2019-08-13 Araxes Pharma Llc Inhibitors of RAS and methods of use thereof

Patent Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2013155223A1 (en) * 2012-04-10 2013-10-17 The Regents Of The University Of California Compositions and methods for treating cancer

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Publication number Priority date Publication date Assignee Title
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