CN112955137B - 组合疗法 - Google Patents

组合疗法 Download PDF

Info

Publication number
CN112955137B
CN112955137B CN201980073799.8A CN201980073799A CN112955137B CN 112955137 B CN112955137 B CN 112955137B CN 201980073799 A CN201980073799 A CN 201980073799A CN 112955137 B CN112955137 B CN 112955137B
Authority
CN
China
Prior art keywords
inhibitor
kras
formula
effective amount
therapeutically effective
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
CN201980073799.8A
Other languages
English (en)
Chinese (zh)
Other versions
CN112955137A (zh
Inventor
拉尔斯·丹尼尔·恩斯特龙
露丝·薇·阿兰达
彼得·奥尔森
詹姆斯·盖尔·克里斯滕森
吉尔·哈林
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.)
Mirati Therapeutics Inc
Original Assignee
Mirati Therapeutics 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 Mirati Therapeutics Inc filed Critical Mirati Therapeutics Inc
Publication of CN112955137A publication Critical patent/CN112955137A/zh
Application granted granted Critical
Publication of CN112955137B publication Critical patent/CN112955137B/zh
Active legal-status Critical Current
Anticipated expiration legal-status Critical

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D471/00—Heterocyclic 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
    • C07D471/02—Heterocyclic 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
    • C07D471/04—Ortho-condensed systems
    • 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
    • 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
    • A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
    • 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
    • A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
    • A61K31/5375—1,4-Oxazines, e.g. morpholine
    • A61K31/5377—1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
    • 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
    • A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
    • A61K31/5375—1,4-Oxazines, e.g. morpholine
    • A61K31/5386—1,4-Oxazines, e.g. morpholine spiro-condensed or forming part of bridged ring systems
    • 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
    • A61K31/54—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one sulfur as the ring hetero atoms, e.g. sulthiame
    • A61K31/541—Non-condensed thiazines containing further heterocyclic rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K39/00—Medicinal preparations containing antigens or antibodies
    • A61K39/395—Antibodies; Immunoglobulins; Immune serum, e.g. antilymphocytic serum
    • 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
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K16/00—Immunoglobulins [IGs], e.g. monoclonal or polyclonal antibodies
    • C07K16/18—Immunoglobulins [IGs], e.g. monoclonal or polyclonal antibodies against material from animals or humans
    • C07K16/28—Immunoglobulins [IGs], e.g. monoclonal or polyclonal antibodies against material from animals or humans against receptors, cell surface antigens or cell surface determinants
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K16/00—Immunoglobulins [IGs], e.g. monoclonal or polyclonal antibodies
    • C07K16/18—Immunoglobulins [IGs], e.g. monoclonal or polyclonal antibodies against material from animals or humans
    • C07K16/28—Immunoglobulins [IGs], e.g. monoclonal or polyclonal antibodies against material from animals or humans against receptors, cell surface antigens or cell surface determinants
    • C07K16/2863—Immunoglobulins [IGs], e.g. monoclonal or polyclonal antibodies against material from animals or humans against receptors, cell surface antigens or cell surface determinants against receptors for growth factors, growth regulators
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K2300/00—Mixtures or combinations of active ingredients, wherein at least one active ingredient is fully defined in groups A61K31/00 - A61K41/00

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Epidemiology (AREA)
  • Organic Chemistry (AREA)
  • Immunology (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Biochemistry (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Molecular Biology (AREA)
  • Genetics & Genomics (AREA)
  • Biophysics (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Microbiology (AREA)
  • Mycology (AREA)
  • Hematology (AREA)
  • Oncology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Medicines Containing Antibodies Or Antigens For Use As Internal Diagnostic Agents (AREA)
CN201980073799.8A 2018-09-10 2019-09-09 组合疗法 Active CN112955137B (zh)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201862729189P 2018-09-10 2018-09-10
US62/729,189 2018-09-10
PCT/US2019/050227 WO2020055756A1 (en) 2018-09-10 2019-09-09 Combination therapies

Publications (2)

Publication Number Publication Date
CN112955137A CN112955137A (zh) 2021-06-11
CN112955137B true CN112955137B (zh) 2025-05-13

Family

ID=69778045

Family Applications (1)

Application Number Title Priority Date Filing Date
CN201980073799.8A Active CN112955137B (zh) 2018-09-10 2019-09-09 组合疗法

Country Status (13)

Country Link
US (2) US12336995B2 (enExample)
EP (1) EP3849538A4 (enExample)
JP (2) JP7546548B2 (enExample)
KR (1) KR102871791B1 (enExample)
CN (1) CN112955137B (enExample)
AU (1) AU2019340366B2 (enExample)
CA (1) CA3112043A1 (enExample)
EA (1) EA202190749A1 (enExample)
IL (1) IL281344B2 (enExample)
MX (2) MX2021002805A (enExample)
SG (1) SG11202102377YA (enExample)
WO (1) WO2020055756A1 (enExample)
ZA (1) ZA202102015B (enExample)

Families Citing this family (14)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN114616232A (zh) * 2019-09-06 2022-06-10 正大天晴药业集团南京顺欣制药有限公司 氮杂环庚烷并嘧啶类衍生物及其医药用途
US12122787B2 (en) 2019-09-20 2024-10-22 Shanghai Jemincare Pharmaceuticals Co., Ltd Fused pyridone compound, and preparation method therefor and use thereof
CN112694475B (zh) * 2019-10-23 2025-09-23 苏州泽璟生物制药股份有限公司 环烷基类和杂环烷基类抑制剂及其制备方法和应用
US12479834B2 (en) 2019-11-29 2025-11-25 Taiho Pharmaceutical Co., Ltd. Phenol compound or salt thereof
WO2021219072A1 (zh) * 2020-04-30 2021-11-04 上海科州药物研发有限公司 作为kras抑制剂的杂环化合物的制备及其应用方法
IL299344A (en) 2020-06-25 2023-02-01 Tolremo Therapeutics Ag Combination of a cbp/p300 bromodomain inhibitor and a kras inhibitor for the treatment of cancer
JP7637777B2 (ja) * 2020-12-08 2025-02-28 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
US20240092803A1 (en) * 2021-01-08 2024-03-21 Beigene Switzerland Gmbh Bridged compounds as kras g12d inhibitor and degrader and the use thereof
CN117460737A (zh) * 2021-07-05 2024-01-26 四川科伦博泰生物医药股份有限公司 杂芳环化合物、其制备方法及用途
CN118043075A (zh) * 2021-07-29 2024-05-14 得克萨斯州大学系统董事会 用于治疗kras突变体癌症的方法和组合物
US20240408099A1 (en) * 2021-10-05 2024-12-12 Mirati Therapeutics, Inc. COMBINATION THERAPIES OF KRAS G12D INHIBITORS WITH Pan ErbB FAMILY INHIBITORS
KR20240114793A (ko) 2021-11-05 2024-07-24 프론티어 메디슨즈 코포레이션 Kras g12c 억제제
WO2025085748A1 (en) 2023-10-20 2025-04-24 Merck Sharp & Dohme Llc Small molecule inhibitors of kras proteins
WO2025145207A1 (en) 2023-12-29 2025-07-03 Bristol-Myers Squibb Company Combination therapy of kras inhibitor and treg-depleting agent

Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2016044772A1 (en) * 2014-09-18 2016-03-24 Araxes Pharma Llc Combination therapies for treatment of cancer
WO2017201161A1 (en) * 2016-05-18 2017-11-23 Mirati Therapeutics, Inc. Kras g12c inhibitors

Family Cites Families (293)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CA2417500C (en) 2000-07-28 2008-11-18 Georgetown University Medical Center Erbb-2 selective small molecule kinase inhibitors
MXPA03005854A (es) 2001-01-02 2003-09-10 Hoffmann La Roche Derivados de quinazolona como antagonistas del receptor adrenergico alfa 1a/b.
WO2002088079A2 (en) 2001-05-01 2002-11-07 Bristol-Myers Squibb Company Dual inhibitors of pde 7 and pde 4
US7105667B2 (en) 2001-05-01 2006-09-12 Bristol-Myers Squibb Co. Fused heterocyclic compounds and use thereof
JP2005522514A (ja) 2002-04-10 2005-07-28 ジェネンテック・インコーポレーテッド 抗ｈｅｒ２抗体改変体
CA2567832A1 (en) 2004-06-04 2005-12-15 Astrazeneca Ab Quinazoline derivatives as erbb receptor tyrosine kinases
KR20190126461A (ko) 2004-07-22 2019-11-11 제넨테크, 인크. Ｈｅｒ２ 항체 조성물
US7812022B2 (en) 2004-12-21 2010-10-12 Glaxosmithkline Llc 2-pyrimidinyl pyrazolopyridine ErbB kinase inhibitors
CA2646257A1 (en) 2005-04-14 2006-10-26 Wyeth Use of an epidermal growth factor receptor kinase inhibitor (egfr) in gefitinib resistant patients
PT1951759E (pt) 2005-11-12 2010-04-01 Lilly Co Eli Anticorpos anti-egfr
EP1960371B1 (en) 2005-12-02 2009-09-16 AstraZeneca AB Quinazoleine derivatives used as inhibitors of erbb tyrosine kinase
AR056857A1 (es) 2005-12-30 2007-10-24 U3 Pharma Ag Anticuerpos dirigidos hacia her-3 (receptor del factor de crecimiento epidérmico humano-3) y sus usos
US20080051387A1 (en) 2006-06-09 2008-02-28 Yuelian Xu Tetrahydropyrido[3,4-d]pyrimidines and related analogues
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
ES2399075T3 (es) 2006-08-30 2013-03-25 Genentech, Inc. Anticuerpos multiespecíficos
US8604044B2 (en) 2006-09-11 2013-12-10 Curis, Inc. Quinazoline based EGFR inhibitors containing a zinc binding moiety
US7547781B2 (en) 2006-09-11 2009-06-16 Curis, Inc. Quinazoline based EGFR inhibitors containing a zinc binding moiety
EP2061469B8 (en) 2006-09-11 2014-02-26 Curis, Inc. Quinazoline based egfr inhibitors
US8242080B2 (en) 2006-10-13 2012-08-14 The Regents Of The University Of California Inhibitors of the EGFR kinase targeting the asymmetric activating dimer interface
US20100210649A1 (en) 2006-12-21 2010-08-19 Sloan-Kettering Institute For Cancer Research Pyridazinones and furan-containing compounds
WO2008103470A2 (en) 2007-02-21 2008-08-28 Trustees Of Columbia University In The City Of New York Oncogenic-ras-signal dependent lethal compounds
PT2182948E (pt) 2007-07-24 2013-04-30 Novartis Ag Utilização de imidazoquinolinas para o tratamento de doenças dependentes do egfr ou doenças que adquiriram resistência a agentes que têm como alvo membros da família egfr
US8119616B2 (en) 2007-09-10 2012-02-21 Curis, Inc. Formulation of quinazoline based EGFR inhibitors containing a zinc binding moiety
ES2668831T3 (es) 2007-10-03 2018-05-22 Nippon Steel & Sumitomo Metal Corporation Aceros inoxidables austeníticos
EP2209775A1 (en) 2007-10-09 2010-07-28 UCB Pharma, S.A. Heterobicyclic compounds as histamine h4-receptor antagonists
US8557243B2 (en) 2008-01-03 2013-10-15 The Scripps Research Institute EFGR antibodies comprising modular recognition domains
PL2259800T3 (pl) 2008-03-05 2014-09-30 Novartis Ag Zastosowanie 5-(2,6-dimorfolin-4-ylopirymidyn-4-ylo)-4-trifluorometylopirydyn-2-yloaminy do leczenia niedrobnokomórkowego raka płuca wykazującego nabytą oporność wobec modulatorów receptora dla naskórkowego czynnika wzrostu (EGFR)
KR20110046514A (ko) 2008-07-31 2011-05-04 제넨테크, 인크. 피리미딘 화합물, 조성물 및 사용 방법
US8642991B2 (en) 2008-11-11 2014-02-04 Samsung Electronics Co., Ltd. Photosensitive quantum dot, composition comprising the same and method of forming quantum dot-containing pattern using the composition
US20100143295A1 (en) 2008-12-05 2010-06-10 Auspex Pharmaceuticals, Inc. Quinazoline inhibitors of egfr tyrosine kinase
WO2010099186A1 (en) 2009-02-25 2010-09-02 Merck Sharp & Dohme Corp. Her2 antibody compositions
WO2010120996A1 (en) 2009-04-17 2010-10-21 Wyeth Llc 5,6,7,8-tetrahydropyrido[3,4-d]pyrimidine compounds, their use as mtor kinase and pi3 kinase inhibitors, and their syntheses
RU2549547C2 (ru) 2009-04-22 2015-04-27 Янссен Фармацевтика Нв Азетидинилдиамиды в качестве ингибиторов моноацилглицерин-липазы
JP5918693B2 (ja) 2009-05-05 2016-05-18 ダナ ファーバー キャンサー インスティテュート インコーポレイテッド Ｅｇｆｒ阻害剤及び疾患の治療方法
CA2783743C (en) 2009-12-11 2022-10-04 Wyeth Llc Phosphatidylinositol-3-kinase pathway biomarkers
US8937159B2 (en) 2009-12-16 2015-01-20 Abbvie Biotherapeutics Inc. Anti-HER2 antibodies and their uses
EP2518064A1 (en) 2009-12-25 2012-10-31 Mochida Pharmaceutical Co., Ltd. Novel aryl urea derivative
JP2013516422A (ja) 2009-12-30 2013-05-13 アビラ セラピューティクス， インコーポレイテッド タンパク質のリガンド−指向性共有的修飾
CN102167742B (zh) 2010-02-25 2014-05-14 上海百迈博制药有限公司 一种全人源抗her2单克隆抗体、其制备方法及用途
US20120107304A1 (en) 2010-04-27 2012-05-03 Boehringer Ingelheim International Gmbh Combination therapy in treatment of oncological and fibrotic diseases
WO2011140338A1 (en) 2010-05-05 2011-11-10 Gatekeeper Pharmaceuticals, Inc. Compounds that modulate egfr activity and methods for treating or preventing conditions therewith
CN103153339B (zh) 2010-05-27 2021-05-04 根马布股份公司 针对her2表位的单克隆抗体
US9051370B2 (en) 2010-08-10 2015-06-09 Glycotope Gmbh Humanized EGFR antibodies
MY162825A (en) 2010-08-20 2017-07-31 Novartis Ag Antibodies for epidermal growth factor receptor 3 (her3)
CN105412105A (zh) 2010-11-08 2016-03-23 诺华有限公司 2-甲酰胺环氨基尿素衍生物在治疗egfr依赖性疾病或对靶向egfr家族成员的药剂有获得性耐受性的疾病中的应用
EP2637502B1 (en) 2010-11-10 2018-01-10 Celgene CAR LLC Mutant-selective egfr inhibitors and uses thereof
US9834518B2 (en) 2011-05-04 2017-12-05 Ariad Pharmaceuticals, Inc. Compounds for inhibiting cell proliferation in EGFR-driven cancers
US8691231B2 (en) 2011-06-03 2014-04-08 Merrimack Pharmaceuticals, Inc. Methods of treatment of tumors expressing predominantly high affinity EGFR ligands or tumors expressing predominantly low affinity EGFR ligands with monoclonal and oligoclonal anti-EGFR antibodies
EP3608340A1 (en) 2011-11-23 2020-02-12 Medlmmune, LLC Binding molecules specific for her3 and uses thereof
WO2013084147A2 (en) 2011-12-05 2013-06-13 Novartis Ag Antibodies for epidermal growth factor receptor 3 (her3)
BR112014015018A2 (pt) 2011-12-19 2020-10-27 Synimmune Gmbh moléculas de anticorpo biespecífico e seu método de produção, bem como composição farmacêutica e molécula de ácido nucleico
US9034885B2 (en) 2012-01-13 2015-05-19 Acea Biosciences Inc. EGFR modulators and uses thereof
ES2762873T3 (es) 2012-03-29 2020-05-26 Translate Bio Inc Lípidos catiónicos ionizables
WO2013155223A1 (en) 2012-04-10 2013-10-17 The Regents Of The University Of California Compositions and methods for treating cancer
CN102659692B (zh) 2012-05-04 2014-04-09 郑州泰基鸿诺药物科技有限公司 双联厄洛替尼及其制备方法
JP6469567B2 (ja) 2012-05-05 2019-02-13 アリアド・ファーマシューティカルズ・インコーポレイテッド Ｅｇｆｒ発動性がんの細胞増殖阻害用化合物
CN106008511B (zh) 2012-05-14 2018-08-14 华东理工大学 蝶啶酮衍生物及其作为egfr、blk、flt3抑制剂的应用
TWI641619B (zh) 2012-06-25 2018-11-21 美商再生元醫藥公司 抗－ｅｇｆｒ抗體及其用途
US9695133B2 (en) 2012-07-13 2017-07-04 The Trustees Of Columbia University In The City Of New York Quinazolinone-based oncogenic-RAS-selective lethal compounds and their use
US20150166664A1 (en) 2012-07-18 2015-06-18 Glycotope Gmbh Novel therapeutic treatments with anti-her2 antibodies having a low fucosylation
KR20150064205A (ko) 2012-11-08 2015-06-10 에프. 호프만-라 로슈 아게 Her3의 베타-헤어핀에 결합하는 her3 항원 결합 단백질
EP2917242B1 (en) 2012-11-08 2018-05-16 F.Hoffmann-La Roche Ag Anti-her3/her4 antigen binding proteins binding to the beta-hairpin of her3 and the beta-hairpin of her4
WO2014081718A1 (en) 2012-11-20 2014-05-30 Genentech, Inc. Aminopyrimidine compounds as inhibitors of t790m containing egfr mutants
US20170275367A1 (en) 2012-11-21 2017-09-28 Janssen Biotech, Inc. Bispecific EGFR/C-Met Antibodies
SI2922872T1 (sl) 2012-11-21 2019-01-31 Janssen Biotech, Inc., Bispecifična protitelesa EGFR/C-MET
CN103333246B (zh) 2012-12-21 2015-09-16 百奥泰生物科技(广州)有限公司 一种抗egfr受体的肿瘤生长抑制剂及其制备方法和用途
WO2014137577A1 (en) 2013-03-08 2014-09-12 United Technologies Corporation Ring-shaped compliant support
CN105209493B (zh) 2013-03-14 2019-05-03 德克萨斯州大学系统董事会 用于诊断和治疗用途的her3特异性单克隆抗体
JP6473133B2 (ja) 2013-03-15 2019-02-20 アラクセス ファーマ エルエルシー Ｋｒａｓｇ１２ｃの共有結合性阻害剤
US9227978B2 (en) 2013-03-15 2016-01-05 Araxes Pharma Llc Covalent inhibitors of Kras G12C
PT2968588T (pt) 2013-03-15 2019-05-08 Abbvie Inc Formulações de conjugado de fármaco-anticorpo anti-egfr
US9745319B2 (en) 2013-03-15 2017-08-29 Araxes Pharma Llc Irreversible covalent inhibitors of the GTPase K-Ras G12C
EP3052494B1 (en) 2013-06-28 2018-12-26 H. Hoffnabb-La Roche Ag Azaindazole compounds as inhibitors of t790m containing egfr mutants
JO3805B1 (ar) 2013-10-10 2021-01-31 Araxes Pharma Llc مثبطات كراس جي12سي
EP3636639A1 (en) 2013-10-10 2020-04-15 Araxes Pharma LLC Inhibitors of kras g12c
SG11201605449YA (en) 2014-01-10 2016-08-30 Birdie Biopharmaceuticals Inc Compounds and compositions for immunotherapy
NO2718543T3 (enExample) 2014-02-04 2018-01-06
KR102409739B1 (ko) 2014-03-20 2022-06-17 카펠라 테라퓨틱스, 인크. 암 치료용의 ｅｒｂｂ 티로신 키나제 억제제로서의 벤즈이미다졸 유도체
TWI807150B (zh) 2014-03-20 2023-07-01 美商卡佩拉醫療公司 苯并咪唑衍生物及其醫藥組合物及使用方法
ES2800674T3 (es) 2014-03-21 2021-01-04 X Body Inc Polipéptidos biespecíficos de unión a antígeno
TW202330606A (zh) 2014-03-21 2023-08-01 美商艾伯維有限公司 抗-egfr抗體及抗體藥物結合物
PT3789042T (pt) 2014-04-10 2025-01-14 Daiichi Sankyo Europe Gmbh Método para produzir conjugado anticorpo-fármaco anti-her3
WO2015184349A2 (en) 2014-05-30 2015-12-03 The Trustees Of Columbia University In The City Of New York Multivalent ras binding compounds
TWI689520B (zh) 2014-05-30 2020-04-01 漢霖生技股份有限公司 抗表皮生長因子受體（ｅｇｆｒ）抗體
KR102557615B1 (ko) 2014-06-06 2023-07-20 레드우드 바이오사이언스 인코포레이티드 항-her2 항체-메이탄신 컨쥬게이트 및 이것의 사용 방법
SG10201811124YA (en) 2014-06-20 2019-01-30 Abgenomics Int Inc Her2 antibody-drug conjugates
WO2016025650A1 (en) 2014-08-13 2016-02-18 Celgene Avilomics Research, Inc. Combinations of an erk inhibitor and a cdk4/6 inhibitor and related methods
SG11201701623UA (en) 2014-09-12 2017-03-30 Genentech Inc Anti-her2 antibodies and immunoconjugates
CA2944085C (en) 2014-09-16 2018-04-10 Ease Charm Limited Anti-egfr antibody and uses of same
EP3197870B1 (en) 2014-09-25 2020-08-19 Araxes Pharma LLC Inhibitors of kras g12c mutant proteins
WO2016049565A1 (en) 2014-09-25 2016-03-31 Araxes Pharma Llc Compositions and methods for inhibition of ras
WO2016049568A1 (en) 2014-09-25 2016-03-31 Araxes Pharma Llc Methods and compositions for inhibition of ras
KR102073854B1 (ko) 2014-10-13 2020-02-05 주식회사유한양행 Egfr 돌연변이 키나아제 활성을 조절하기 위한 화합물 및 조성물
EP3209334A2 (en) 2014-10-20 2017-08-30 Igenica Biotherapeutics, Inc. Novel antibody-drug conjugates and related compounds, compositions, and methods of use
EP3221309B1 (en) 2014-11-20 2019-11-13 Council of Scientific and Industrial Research Novel benzimidazole based egfr inhibitors
KR20170098865A (ko) 2014-12-11 2017-08-30 베타 파마, 인크. Egfr 조정제로서의 치환된 2-아닐리노피리미딘 유도체
WO2016105525A2 (en) 2014-12-23 2016-06-30 Dana-Farber Cancer Institute, Inc. Novel pyrimidines as egfr inhibitors and methods of treating disorders
CN104530063B (zh) 2015-01-13 2017-01-18 北京赛特明强医药科技有限公司 喹唑啉并杂环类化合物及其制备方法和作为用于治疗癌症的表皮生长因子受体抑制剂的应用
JP2018504441A (ja) 2015-02-03 2018-02-15 トリリウム セラピューティクス インコーポレイテッド 癌の治療に有用なｅｇｆｒ阻害剤としての新規フッ素化誘導体
WO2016125186A1 (en) 2015-02-03 2016-08-11 Council Of Scientific & Industrial Research Novel flavone based egfr inhibitors and process for preparation thereof
US10017540B2 (en) 2015-03-11 2018-07-10 California Institute Of Technology Cyclic peptide binder against oncogenic K-Ras
EP3280708B1 (en) 2015-04-10 2021-09-01 Araxes Pharma LLC Substituted quinazoline compounds and methods of use thereof
EP3283462B1 (en) 2015-04-15 2020-12-02 Araxes Pharma LLC Fused-tricyclic inhibitors of kras and methods of use thereof
WO2016172692A1 (en) 2015-04-24 2016-10-27 H. Lee Moffitt Cancer Center And Research Institute, Inc. Mutant kras inhibitors
EP3091033A1 (en) 2015-05-06 2016-11-09 Gamamabs Pharma Anti-human-her3 antibodies and uses thereof
BR112017023821A2 (pt) 2015-05-06 2018-07-31 Leidos Biomedical Res Inc moduladores de k-ras
US10144724B2 (en) 2015-07-22 2018-12-04 Araxes Pharma Llc Substituted quinazoline compounds and methods of use thereof
AR106135A1 (es) 2015-09-24 2017-12-13 Ionis Pharmaceuticals Inc Moduladores de la expresión del sarcoma de la rata de kirsten (kras)
EP3356354A1 (en) 2015-09-28 2018-08-08 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
EP3356359B1 (en) 2015-09-28 2021-10-20 Araxes Pharma LLC Inhibitors of kras g12c mutant proteins
WO2017058902A1 (en) 2015-09-28 2017-04-06 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
EP3356351A1 (en) 2015-09-28 2018-08-08 Araxes Pharma LLC Inhibitors of kras g12c mutant proteins
US10875842B2 (en) 2015-09-28 2020-12-29 Araxes Pharma Llc Inhibitors of KRAS G12C mutant proteins
EP3364977A4 (en) 2015-10-19 2019-09-04 Araxes Pharma LLC PROCESS FOR SCREENING INHIBITORS OF RAS
US10670605B2 (en) 2015-10-22 2020-06-02 The Scripps Research Institute Cysteine reactive probes and uses thereof
WO2017080980A1 (en) 2015-11-09 2017-05-18 Astrazeneca Ab Dihydropyrrolopyrazinone derivatives useful in the treatment of cancer
WO2017079864A1 (en) 2015-11-12 2017-05-18 Hangzhou Yier Biotech Co., Ltd. Treatment of cancers related to chronically active ras
EA038635B9 (ru) 2015-11-16 2021-10-26 Араксис Фарма Ллк 2-замещенные соединения хиназолина, содержащие замещенную гетероциклическую группу, и способы их применения
US9988357B2 (en) 2015-12-09 2018-06-05 Araxes Pharma Llc Methods for preparation of quinazoline derivatives
US20170283445A1 (en) 2016-04-05 2017-10-05 University Of South Carolina Small Molecule Inhibitors Selective For Polo-Like Kinase Proteins
KR20220130249A (ko) 2016-05-26 2022-09-26 리커리엄 아이피 홀딩스, 엘엘씨 Egfr 억제제 화합물
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
US10377833B2 (en) 2016-07-22 2019-08-13 Beijing Mabworks Biotech Co., Ltd. Bispecific anti-HER2 antibody
CN110167968B (zh) 2016-09-15 2023-11-28 斯图加特大学 针对her3的抗原结合蛋白
WO2018064510A1 (en) 2016-09-29 2018-04-05 Araxes Pharma Llc Inhibitors of kras g12c mutant proteins
WO2018068017A1 (en) 2016-10-07 2018-04-12 Araxes Pharma Llc Heterocyclic compounds as inhibitors of ras and methods of use thereof
CA3082011A1 (en) 2016-11-30 2018-06-07 Bantam Pharmaceutical, Llc Methods of using substituted pyrazole and pyrrole compounds and for treatment of hyperproliferative diseases
MX2019006299A (es) 2016-11-30 2019-11-12 Bantam Pharmaceutical Llc Compuestos de pirazola sustituida y metodos para usarlos para el tratamiento de enfermedades hiperproliferativas.
CA3047125A1 (en) 2016-12-15 2018-06-21 The Regents Of The University Of California Compositions and methods for treating cancer
WO2018115380A1 (en) 2016-12-22 2018-06-28 Boehringer Ingelheim International Gmbh Novel benzylamino substituted quinazolines and derivatives as sos1 inhibitors
PL3558955T3 (pl) 2016-12-22 2021-12-27 Amgen Inc. Pochodne benzoizotiazolu, izotiazolo[3,4-b]pirydyny, chinazoliny, ftalazyny, pirydo[2,3-d]pirydazyny i pirydo[2,3-d]pirymidyny jako inhibitory kras g12c do leczenia raka płuc, trzustki lub jelita grubego
US10344026B2 (en) 2017-01-18 2019-07-09 Nantbio, Inc. Compositions and methods of targeting mutant K-ras
CN110382483A (zh) 2017-01-26 2019-10-25 亚瑞克西斯制药公司 稠合的n-杂环化合物及其使用方法
US11274093B2 (en) 2017-01-26 2022-03-15 Araxes Pharma Llc Fused bicyclic benzoheteroaromatic compounds and methods of use thereof
US11279689B2 (en) 2017-01-26 2022-03-22 Araxes Pharma Llc 1-(3-(6-(3-hydroxynaphthalen-1-yl)benzofuran-2-yl)azetidin-1 yl)prop-2-en-1-one derivatives and similar compounds as KRAS G12C modulators for treating cancer
WO2018140514A1 (en) 2017-01-26 2018-08-02 Araxes Pharma Llc 1-(6-(3-hydroxynaphthalen-1-yl)quinazolin-2-yl)azetidin-1-yl)prop-2-en-1-one derivatives and similar compounds as kras g12c inhibitors for the treatment of cancer
US11059819B2 (en) 2017-01-26 2021-07-13 Janssen Biotech, Inc. Fused hetero-hetero bicyclic compounds and methods of use thereof
EP3573964A1 (en) 2017-01-26 2019-12-04 Araxes Pharma LLC Benzothiophene and benzothiazole compounds and methods of use thereof
JOP20190186A1 (ar) 2017-02-02 2019-08-01 Astellas Pharma Inc مركب كينازولين
BR112019021899A2 (pt) 2017-04-20 2020-08-18 The Regents Of The University Of California moduladores de k-ras
ES2928576T3 (es) 2017-09-08 2022-11-21 Amgen Inc Inhibidores de KRAS G12C y métodos de uso de los mismos
US10647715B2 (en) * 2017-11-15 2020-05-12 Mirati Therapeutics, Inc. KRas G12C inhibitors
EP3710439B1 (en) 2017-11-15 2023-02-15 Mirati Therapeutics, Inc. Kras g12c inhibitors
WO2020027202A1 (ja) 2018-07-31 2020-02-06 本田技研工業株式会社 電力予測システム、電力予測装置、電力予測方法、プログラム、及び記憶媒体
EP3849535A4 (en) * 2018-09-10 2022-06-29 Mirati Therapeutics, Inc. Combination therapies
US20220040181A1 (en) * 2018-09-10 2022-02-10 Mirati Therapeutics, Inc. Combination therapies
LT3849537T (lt) * 2018-09-10 2025-02-10 Mirati Therapeutics, Inc. Kompleksinės terapijos
WO2020055760A1 (en) * 2018-09-10 2020-03-19 Mirati Therapeutics, Inc. Combination therapies
CN113038342B (zh) 2018-09-30 2022-10-14 荣耀终端有限公司 音频播放电路和终端
CN111193490B (zh) 2018-11-14 2025-05-13 天津大学 散热结构、带散热结构的体声波谐振器、滤波器和电子设备
SG11202102357RA (en) * 2018-12-05 2021-04-29 Mirati Therapeutics Inc Combination therapies
JP7592601B2 (ja) 2019-01-10 2024-12-02 ミラティ セラピューティクス， インコーポレイテッド Ｋｒａｓ ｇ１２ｃ阻害剤
WO2020163598A1 (en) 2019-02-07 2020-08-13 The Regents Of The University Of California Immunophilin-dependent inhibitors and uses thereof
EP3924687A4 (en) 2019-02-11 2022-11-02 Mesomat Inc. SENSING FIBERS FOR STRUCTURAL STRESS MONITORING
KR102747104B1 (ko) 2019-02-18 2024-12-27 한국과학기술연구원 단백질 키나아제 저해 활성을 갖는 신규한 피리도[3,4-d]피리미딘-8-온 유도체 및 이를 포함하는 암의 예방, 개선 또는 치료용 약학 조성물
CA3130618A1 (en) 2019-02-20 2020-08-27 Fred Hutchinson Cancer Research Center Binding proteins specific for ras neoantigens and uses thereof
GB201902392D0 (en) 2019-02-21 2019-04-10 Cambridge Entpr Ltd Modular binding proteins
US20220313700A1 (en) 2019-02-26 2022-10-06 Cell Response, Inc. Methods for treating map3k8 positive cancers
WO2020177629A1 (zh) 2019-03-01 2020-09-10 劲方医药科技(上海)有限公司 螺环取代的嘧啶并环类化合物，其制法与医药上的用途
AU2019432235B2 (en) 2019-03-05 2024-02-01 Questor Technology Inc. Gas incinerator system
SG11202109451TA (en) 2019-03-05 2021-09-29 Astrazeneca Ab Fused tricyclic compounds useful as anticancer agents
AU2020231218B2 (en) 2019-03-06 2025-09-11 Dana-Farber Cancer Institute, Inc. T cell receptors specific to B-cell maturation antigen for treatment of cancer
US20220160714A1 (en) 2019-03-22 2022-05-26 Icahn School Of Medicine At Mount Sinai Methods for treating colorectal cancer
WO2020205486A1 (en) 2019-03-29 2020-10-08 Kura Oncology, Inc. Methods of treating squamous cell carcinomas with farnesyltransferase inhibitors
AU2020253823A1 (en) 2019-03-29 2021-10-14 Dicerna Pharmaceuticals, Inc. Compositions and methods for the treatment of KRAS associated diseases or disorders
KR102222693B1 (ko) 2019-04-04 2021-03-04 금정제약 주식회사 H-rev107 유래 펩타이드의 신규한 용도
US20220227740A1 (en) 2019-04-15 2022-07-21 Tosk, Inc. Modulators of RAS GTPase
US20200335182A1 (en) 2019-04-16 2020-10-22 Uratim Ltd. Method and apparatus for facilitating the binding of biological macromolecules with the use of gluing molecular agents with applications in RAS mutations and related conditions
KR20220012255A (ko) 2019-04-28 2022-02-03 젠플리트 테라퓨틱스 (상하이) 아이엔씨. 옥사아자퀴나졸린-7(8h)-케톤 화합물, 이의 제조 방법 및 이의 약학적 응용
HUE065486T2 (hu) 2019-05-10 2024-05-28 Deciphera Pharmaceuticals Llc Fenilaminopirimidinamid autophágia inhibitorok és azok felhasználási eljárásai
PE20220592A1 (es) 2019-05-10 2022-04-22 Deciphera Pharmaceuticals Llc Inhibidores de la autofagia de heteroarilaminopirimidina amida y metodos de uso de estos
CA3138123A1 (en) 2019-05-13 2020-11-19 Novartis Ag New crystalline forms of n-(3-(2-(2-hydroxyethoxy)-6-morpholinopyridin-4-yl)-4-methvlphenyl)-2 (trifluoromethyl)isonicotinamide as raf inhibitors for the treatment of cancer
MY208668A (en) 2019-05-14 2025-05-23 Janssen Biotech Inc Combination therapies with bispecific anti-egfr/c-met antibodies and 3rd generation egfr tyrosine kinase inhibitors
EP3738593A1 (en) 2019-05-14 2020-11-18 Amgen, Inc Dosing of kras inhibitor for treatment of cancers
MX2021014177A (es) 2019-05-20 2022-04-25 California Inst Of Techn Inhibidores de kras con la mutacion de glicina a cisteina en el codon 12 (g12c) y usos de los mismos.
EP3972972A1 (en) 2019-05-21 2022-03-30 Amgen Inc. Solid state forms
NZ782284A (en) 2019-05-21 2024-11-29 Amgen Inc Solid state forms
WO2020233592A1 (en) 2019-05-21 2020-11-26 Inventisbio Shanghai Ltd. Heterocyclic compounds, preparation methods and uses thereof
EP3972963A1 (en) 2019-05-21 2022-03-30 Bayer Aktiengesellschaft Identification and use of kras inhibitors
WO2020247914A1 (en) 2019-06-07 2020-12-10 Emory University Kras g12v mutant binds to jak1, inhibitors, pharmaceutical compositions, and methods related thereto
WO2020252353A1 (en) 2019-06-12 2020-12-17 Vanderbilt University Amino acid transport inhibitors and the uses thereof
CN114269715A (zh) 2019-06-12 2022-04-01 范德比尔特大学 作为氨基酸转运抑制剂的二苄基胺
TW202115089A (zh) 2019-07-01 2021-04-16 大陸商江蘇恆瑞醫藥股份有限公司 喹唑啉酮類衍生物、其製備方法及其在醫藥上的應用
EP4011886A4 (en) 2019-08-02 2023-07-26 Shanghai Jemincare Pharmaceuticals Co., Ltd. TETRACYCLIC COMPOUND, METHOD FOR PREPARATION AND USE
WO2021023247A1 (en) 2019-08-07 2021-02-11 Jacobio Pharmaceuticals Co., Ltd. Kras mutant protein inhibitor
WO2021027943A1 (zh) 2019-08-14 2021-02-18 正大天晴药业集团南京顺欣制药有限公司 哒嗪酮并嘧啶类衍生物及其医药用途
CN112390797A (zh) 2019-08-15 2021-02-23 微境生物医药科技(上海)有限公司 新型螺环类K-Ras G12C抑制剂
CN114222743A (zh) 2019-08-16 2022-03-22 劲方医药科技(上海)有限公司 氧代六元环并嘧啶类化合物，其制法与医药上的用途
CN114286676A (zh) 2019-08-22 2022-04-05 密歇根大学董事会 治疗kras相关癌症的方法
WO2021037018A1 (zh) 2019-08-26 2021-03-04 南京创济生物医药有限公司 二氢或四氢喹唑啉类化合物及其中间体、制备方法和应用
WO2021041671A1 (en) 2019-08-29 2021-03-04 Mirati Therapeutics, Inc. Kras g12d inhibitors
CN112771053A (zh) 2019-09-06 2021-05-07 伟迈可生物有限公司 基于生物标志物的治疗组合物
CN114616232A (zh) 2019-09-06 2022-06-10 正大天晴药业集团南京顺欣制药有限公司 氮杂环庚烷并嘧啶类衍生物及其医药用途
CA3149872A1 (en) 2019-09-10 2021-03-18 Eric Alejandro Sweet-Cordero Methods of treating kras mutant cancers
TW202124374A (zh) 2019-09-13 2021-07-01 美商拜歐斯瑞克斯公司 Ras蛋白降解劑、其醫藥組合物及其治療應用
WO2021055728A1 (en) 2019-09-18 2021-03-25 Merck Sharp & Dohme Corp. Small molecule inhibitors of kras g12c mutant
WO2021052499A1 (zh) 2019-09-20 2021-03-25 上海济煜医药科技有限公司 稠合吡啶酮类化合物及其制备方法和应用
WO2021061515A1 (en) 2019-09-23 2021-04-01 Synblia Therapeutics, Inc. Shp2 inhibitors and uses thereof
CA3152025A1 (en) 2019-09-24 2021-04-01 David BRIERE Combination therapies
CN112552295A (zh) 2019-09-25 2021-03-26 北京加科思新药研发有限公司 Kras突变蛋白抑制剂
US20220389021A1 (en) 2019-09-29 2022-12-08 Beigene, Ltd. Inhibitors of kras g12c
WO2021063346A1 (zh) 2019-09-30 2021-04-08 上海迪诺医药科技有限公司 Kras g12c抑制剂及其应用
CN114555586B (zh) 2019-10-10 2023-06-23 信达生物制药(苏州)有限公司 Krasg12c蛋白抑制剂及其制备方法和用途
US20240139193A1 (en) 2019-10-15 2024-05-02 Amgen Inc. Combination therapy of kras inhibitor and shp2 inhibitor for treatment of cancers
JP6754125B1 (ja) 2019-10-15 2020-09-09 学校法人東京理科大学 Ｂｒａｐ２作用増強剤
CN112694475B (zh) 2019-10-23 2025-09-23 苏州泽璟生物制药股份有限公司 环烷基类和杂环烷基类抑制剂及其制备方法和应用
ES3007812T3 (en) 2019-10-23 2025-03-20 Sk Biopharmaceuticals Co Ltd Bicyclic compound and use thereof
MX2022004656A (es) 2019-10-24 2022-05-25 Amgen Inc Derivados de piridopirimidina utiles como inhibidores de kras g12c y kras g12d en el tratamiento del cancer.
CA3158793A1 (en) 2019-10-28 2021-05-06 Merck Sharp & Dohme Corp. Small molecule inhibitors of kras g12c mutant
LT4053118T (lt) 2019-10-30 2024-12-10 Genfleet Therapeutics (Shanghai) Inc. Pakeistas heterociklinis junginys su sujungtais žiedais, jo paruošimo būdas ir naudojimas farmacijoje
JP2023515235A (ja) 2019-10-31 2023-04-12 大鵬薬品工業株式会社 ４－アミノブタ－２－エンアミド誘導体及びその塩
WO2021084765A1 (en) 2019-10-31 2021-05-06 Taiho Pharmaceutical Co., Ltd 4-aminobut-2-enamide derivatives and salts thereof
KR20220109406A (ko) 2019-11-04 2022-08-04 레볼루션 메디슨즈, 인크. Ras 억제제
CN113286794B (zh) 2019-11-04 2024-03-12 北京加科思新药研发有限公司 Kras突变蛋白抑制剂
CA3159561A1 (en) 2019-11-04 2021-05-14 Revolution Medicines, Inc. Ras inhibitors
EP4055028A1 (en) 2019-11-04 2022-09-14 Revolution Medicines, Inc. Ras inhibitors
PE20221323A1 (es) 2019-11-07 2022-09-09 Chugai Pharmaceutical Co Ltd Compuesto de peptidos ciclicos que tiene accion inhibidora de kras
CN112778301A (zh) 2019-11-07 2021-05-11 苏州泽璟生物制药股份有限公司 四氢吡啶并嘧啶类抑制剂及其制备方法和应用
TWI760919B (zh) 2019-11-15 2022-04-11 大陸商四川海思科製藥有限公司 一種嘧啶並環衍生物及其在醫藥上的應用
WO2021108683A1 (en) 2019-11-27 2021-06-03 Revolution Medicines, Inc. Covalent ras inhibitors and uses thereof
US12479834B2 (en) 2019-11-29 2025-11-25 Taiho Pharmaceutical Co., Ltd. Phenol compound or salt thereof
US20230061083A1 (en) 2019-11-29 2023-03-02 Evopoint Biosciences Co., Ltd. Kras g12c inhibitor compound and use thereof
WO2021106231A1 (en) 2019-11-29 2021-06-03 Taiho Pharmaceutical Co., Ltd. A compound having inhibitory activity against kras g12d mutation
JP7480298B2 (ja) 2019-12-02 2024-05-09 シャンハイ インリー ファーマシューティカル カンパニー リミテッド 酸素含有複素環化合物、その製造方法及び使用
WO2021113595A1 (en) 2019-12-06 2021-06-10 Beta Pharma, Inc. Phosphorus derivatives as kras inhibitors
WO2021120045A1 (en) 2019-12-18 2021-06-24 InventisBio Co., Ltd. Heterocyclic compounds, preparation methods and uses thereof
WO2021126799A1 (en) 2019-12-18 2021-06-24 Merck Sharp & Dohme Corp. Macrocyclic peptides as potent inhibitors of k-ras g12d mutant
WO2021121371A1 (zh) 2019-12-19 2021-06-24 贝达药业股份有限公司 Kras g12c抑制剂及其在医药上的应用
JP7644517B2 (ja) 2019-12-19 2025-03-12 ジャコバイオ ファーマスーティカルズ カンパニー リミテッド Ｋｒａｓ突然変異型タンパク質阻害剤
WO2021121397A1 (zh) 2019-12-19 2021-06-24 首药控股(北京)股份有限公司 取代的炔基杂环化合物
TR201920922A2 (tr) 2019-12-20 2020-06-22 Ankara Ueniversitesi 3/4-((2E,6E)-3,7,11-Trimetildodeka-2,6,10-trieniltiyo)benzamid Türevi Bileşikler
AU2020408562A1 (en) 2019-12-20 2022-06-23 Erasca, Inc. Tricyclic pyridones and pyrimidones
CN113045565A (zh) 2019-12-27 2021-06-29 微境生物医药科技(上海)有限公司 新型K-Ras G12C抑制剂
JP2023508482A (ja) 2019-12-27 2023-03-02 ウィゲン・バイオメディシン・テクノロジー・（シャンハイ）・カンパニー・リミテッド スピロ環含有キナゾリン化合物
WO2021139678A1 (zh) 2020-01-07 2021-07-15 广州百霆医药科技有限公司 吡啶并嘧啶类kras g12c突变蛋白抑制剂
CN113087700B (zh) 2020-01-08 2023-03-14 苏州亚盛药业有限公司 螺环四氢喹唑啉
AU2021206240A1 (en) 2020-01-10 2022-08-25 Incyte Corporation Tricyclic compounds as inhibitors of KRAS
EP4092026A4 (en) 2020-01-13 2024-03-06 Suzhou Zelgen Biopharmaceutical Co., Ltd. ARYL OR HETEROARYL PYRIDONE OR PYRIMIDINE DERIVATIVES, PRODUCTION METHOD AND USE THEREOF
KR102382613B1 (ko) 2020-01-15 2022-04-06 한국과학기술연구원 단백질 키나아제 저해 활성을 갖는 7-아미노-3,4-디히드로피리미도피리미딘-2-온 유도체 및 이를 포함하는 치료용 약학 조성물
KR102396930B1 (ko) 2020-01-15 2022-05-12 한국과학기술연구원 피리도[3,4-d]피리미딘 유도체 및 이를 포함하는 치료용 약학 조성물
US11530218B2 (en) 2020-01-20 2022-12-20 Incyte Corporation Spiro compounds as inhibitors of KRAS
CN115003668A (zh) 2020-01-21 2022-09-02 南京明德新药研发有限公司 作为kras抑制剂的大环类化合物
GB202001344D0 (en) 2020-01-31 2020-03-18 Redx Pharma Plc Ras Inhibitors
AU2021224733A1 (en) 2020-02-20 2022-09-01 Beta Pharma, Inc. Pyridopyrimidine derivatives as KRAS inhibitors
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
US20230143751A1 (en) 2020-02-24 2023-05-11 Shanghai Zheye Biotechnology Co. Ltd. Aromatic Compound And Use Thereof In Preparing Antineoplastic Drugs
US20210292330A1 (en) 2020-02-28 2021-09-23 Erasca, Inc. Pyrrolidine-fused heterocycles
WO2021175199A1 (zh) 2020-03-02 2021-09-10 上海喆邺生物科技有限公司 一类芳香杂环类化合物及其在药物中的应用
WO2021177721A1 (ko) 2020-03-03 2021-09-10 웰마커바이오 주식회사 Kras 돌연변이 및 활성화된 ron이 존재하는 암의 예방 또는 치료용 약학 조성물
EP4114386A4 (en) 2020-03-05 2024-07-03 The Regents of The University of Michigan INHIBITORS OF EGFR, KRAS, BRAF AND OTHER TARGETS AND THEIR USE
AU2021230372A1 (en) 2020-03-05 2022-09-22 The Regents Of The University Of Michigan Inhibitors of EGFR, KRAS, BRAF, and other targets and use of the same
MX2022011283A (es) 2020-03-12 2022-11-16 D3 Bio Wuxi Co Ltd Compuestos pirimidoheterocíclicos y aplicación de los mismos.
WO2021185233A1 (en) 2020-03-17 2021-09-23 Jacobio Pharmaceuticals Co., Ltd. Kras mutant protein inhibitors
JP7773987B2 (ja) 2020-03-25 2025-11-20 ウィゲン・バイオメディシン・テクノロジー・（シャンハイ）・カンパニー・リミテッド スピロ環含有キナゾリン化合物
KR20220164015A (ko) 2020-04-03 2022-12-12 메드샤인 디스커버리 아이엔씨. 옥타하이드로피라지노디아자나프티리딘 디온 화합물
JP2023521698A (ja) 2020-04-06 2023-05-25 アルヴィナス・オペレーションズ・インコーポレイテッド Ｋｒａｓの標的化分解のための化合物及び方法
TW202144338A (zh) 2020-04-08 2021-12-01 大陸商江蘇恆瑞醫藥股份有限公司 嘧啶并二環類衍生物、其製備方法及其在醫藥上的應用
PH12022552739A1 (en) 2020-04-16 2024-03-25 Incyte Corp Fused tricyclic kras inhibitors
WO2021216770A1 (en) 2020-04-22 2021-10-28 Accutar Biotechnology Inc. Substituted tetrahydroquinazoline compounds as kras inhibitors
EP4138875A4 (en) 2020-04-23 2024-08-28 The Regents of the University of California RAS INHIBITORS AND USES THEREOF
EP4139299B1 (en) 2020-04-24 2025-12-17 Taiho Pharmaceutical Co., Ltd. Kras g12d protein inhibitors
AU2020446002A1 (en) 2020-04-29 2022-12-22 Shanghai Ringene Biopharma Co., Ltd. Benzothiazolyl biaryl compound, and preparation method and use
WO2021219091A2 (zh) 2020-04-29 2021-11-04 北京泰德制药股份有限公司 喹喔啉酮衍生物作为kras g12c突变蛋白的不可逆抑制剂
WO2021219072A1 (zh) 2020-04-30 2021-11-04 上海科州药物研发有限公司 作为kras抑制剂的杂环化合物的制备及其应用方法
US11739102B2 (en) 2020-05-13 2023-08-29 Incyte Corporation Fused pyrimidine compounds as KRAS inhibitors
CN113666923A (zh) 2020-05-15 2021-11-19 苏州泽璟生物制药股份有限公司 烷氧基烷基取代杂环基类抑制剂及其制备方法和应用
WO2021236475A1 (en) 2020-05-18 2021-11-25 Asinex Corporation Compounds that inhibit asparagine synthetase and their methods of use
TWI799871B (zh) 2020-05-27 2023-04-21 大陸商勁方醫藥科技(上海)有限公司 三環并環類化合物，其製法與醫藥上的用途
US20230210852A1 (en) 2020-05-29 2023-07-06 Syros Pharmaceuticals, Inc. Methods of treating cancer in patients with an anomalous kras gene or deletions within chromosome 9
AU2021285032A1 (en) 2020-06-02 2022-12-08 Boehringer Ingelheim International Gmbh Annulated 2-amino-3-cyano thiophenes and derivatives for the treatment of cancer
IL298670A (en) 2020-06-04 2023-01-01 Antengene Discovery Ltd Inhibitors of kras g12c protein and uses thereof
IL298672A (en) 2020-06-04 2023-01-01 Pillai Universal Llc Novel small molecules for targeted unloading of untargetable kras in cancer therapy
WO2021248082A1 (en) 2020-06-05 2021-12-09 Sparcbio Llc Heterocyclic compounds and methods of use thereof
WO2021248083A1 (en) 2020-06-05 2021-12-09 Sparcbio Llc Heterocyclic compounds and methods of use thereof
WO2021248090A1 (en) 2020-06-05 2021-12-09 Sparcbio Llc Heterocyclic compounds and methods of use thereof
WO2021248079A1 (en) 2020-06-05 2021-12-09 Sparcbio Llc Heterocyclic compounds and methods of use thereof
WO2021248095A1 (en) 2020-06-05 2021-12-09 Sparcbio Llc Heterocyclic compounds and methods of use thereof
WO2021252339A1 (en) 2020-06-08 2021-12-16 Accutar Biotechnology, Inc. Substituted purine-2,6-dione compounds as kras inhibitors
WO2021249563A1 (zh) 2020-06-12 2021-12-16 苏州泽璟生物制药股份有限公司 芳基或杂芳基并吡啶酮或嘧啶酮类衍生物及其制备方法和应用
WO2021257828A1 (en) 2020-06-18 2021-12-23 Shy Therapeutics, Llc Substituted thienopyrimidines that interact with the ras superfamily for the treatment of cancers, inflammatory diseases, rasopathies, and fibrotic disease
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
CN115836055A (zh) 2020-06-30 2023-03-21 益方生物科技(上海)股份有限公司 喹唑啉化合物、其制备方法和用途
US20230279025A1 (en) 2020-07-16 2023-09-07 Mirati Therapeutics, Inc. Kras g12d inhibitors
WO2022017339A1 (zh) 2020-07-20 2022-01-27 江苏恒瑞医药股份有限公司 稠合哒嗪类衍生物、其制备方法及其在医药上的应用
JP7584815B2 (ja) 2020-08-02 2024-11-18 上▲海▼▲哲▼▲イェ▼生物科技有限公司 抗腫瘍薬物における芳香族化合物及びその用途
US20230339976A1 (en) 2020-08-04 2023-10-26 Mirati Therapeutics, Inc. Kras g12d inhibitors
WO2022028492A1 (en) 2020-08-05 2022-02-10 Beigene, Ltd. Imidazotriazine and pyrrolopyrimidine derivatives as kras g12c inhibitors
US20230303551A1 (en) 2020-08-13 2023-09-28 Albert Einstein College Of Medicine N-cyclyl-sulfonamides useful for inhibiting raf
CA3190944A1 (en) * 2020-09-11 2022-03-17 Mirati Therapeutics, Inc. Crystalline forms of a kras g12c inhibitor
WO2022087270A1 (en) * 2020-10-23 2022-04-28 Mirati Therapeutics, Inc. Methods for treatment of lung cancers
IL307392A (en) * 2021-04-08 2023-12-01 Mirati Therapeutics Inc Combination therapies with PRMT5 inhibitors for cancer treatment

Patent Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2016044772A1 (en) * 2014-09-18 2016-03-24 Araxes Pharma Llc Combination therapies for treatment of cancer
WO2017201161A1 (en) * 2016-05-18 2017-11-23 Mirati Therapeutics, Inc. Kras g12c inhibitors

Also Published As

Publication number Publication date
AU2019340366B2 (en) 2025-01-02
MX2021002805A (es) 2021-07-15
AU2019340366A1 (en) 2021-04-01
EP3849538A4 (en) 2022-06-29
JP2022500379A (ja) 2022-01-04
CN112955137A (zh) 2021-06-11
EP3849538A1 (en) 2021-07-21
KR102871791B1 (ko) 2025-10-15
US20250262213A1 (en) 2025-08-21
SG11202102377YA (en) 2021-04-29
IL281344B2 (en) 2025-09-01
IL281344B1 (en) 2025-05-01
CA3112043A1 (en) 2020-03-19
JP7546548B2 (ja) 2024-09-06
ZA202102015B (en) 2023-05-31
KR20210075981A (ko) 2021-06-23
MX2024008551A (es) 2024-07-19
WO2020055756A1 (en) 2020-03-19
US20220054491A1 (en) 2022-02-24
JP2024133474A (ja) 2024-10-02
US12336995B2 (en) 2025-06-24
EA202190749A1 (ru) 2021-07-09
IL281344A (en) 2021-04-29

Similar Documents

Publication Publication Date Title
CN112955137B (zh) 组合疗法
EP3849534B1 (en) Combination of dasatinib and adagrasib for use in the treatment of non-small cell lung cancer
US20240408099A1 (en) COMBINATION THERAPIES OF KRAS G12D INHIBITORS WITH Pan ErbB FAMILY INHIBITORS
JP2022500384A (ja) 組み合わせ療法
EA020779B1 (ru) СПОСОБ ЛЕЧЕНИЯ РАКА С ИСПОЛЬЗОВАНИЕМ ИНГИБИТОРА cMET И AXL И ИНГИБИТОРА ErbB
US20250177410A1 (en) Combination therapies comprising a sos1 inhibitor and an egfr inhibitor
CA3110658A1 (en) Compounds, compositions and methods for treating or preventing her-driven cancers
JP2024521788A (ja) 併用療法
EP4013421A1 (en) Tetracyclic compounds and their salts, compositions, and methods for their use
CN115038447A (zh) 用于治疗癌症的组合疗法
EP4504197A2 (en) Combination therapies comprising a sos1 inhibitor and a mek inhibitor
HK40055040A (en) Combination therapies
EA048458B1 (ru) Способы комбинированной терапии
CN117615762A (zh) 组合疗法

Legal Events

Date Code Title Description
PB01 Publication
PB01 Publication
SE01 Entry into force of request for substantive examination
SE01 Entry into force of request for substantive examination
REG Reference to a national code

Ref country code: HK

Ref legal event code: DE

Ref document number: 40055040

Country of ref document: HK

GR01 Patent grant
GR01 Patent grant