TW202309022A - 用於治療具egfr突變之癌症之胺基取代雜環 - Google Patents

用於治療具egfr突變之癌症之胺基取代雜環 Download PDF

Info

Publication number
TW202309022A
TW202309022A TW111113881A TW111113881A TW202309022A TW 202309022 A TW202309022 A TW 202309022A TW 111113881 A TW111113881 A TW 111113881A TW 111113881 A TW111113881 A TW 111113881A TW 202309022 A TW202309022 A TW 202309022A
Authority
TW
Taiwan
Prior art keywords
optionally substituted
alkyl
pharmaceutically acceptable
tautomer
stereoisomer
Prior art date
Application number
TW111113881A
Other languages
English (en)
Chinese (zh)
Inventor
克里斯汀 林恩 安德魯斯
鮑都恩 傑瑞德
喬許華 克特尼 荷倫
史考特 理查 曼提
亨利 艾夫雷姆 佩里許
馬修 D 夏爾
孫玉婷
亞努龐 譚皮拉恰庫爾
Original Assignee
美商努法倫特公司
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 美商努法倫特公司 filed Critical 美商努法倫特公司
Publication of TW202309022A publication Critical patent/TW202309022A/zh

Links

Images

Classifications

    • 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
    • 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
    • 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
    • A61K31/505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/519Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
    • 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
    • A61K31/535Heterocyclic 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
    • A61K31/53751,4-Oxazines, e.g. morpholine
    • A61K31/53831,4-Oxazines, e.g. morpholine 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
    • 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
    • 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
    • C07D487/10Spiro-condensed systems
    • 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
    • C07D498/12Heterocyclic 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 three hetero rings
    • C07D498/14Ortho-condensed systems

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)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
TW111113881A 2021-04-13 2022-04-12 用於治療具egfr突變之癌症之胺基取代雜環 TW202309022A (zh)

Applications Claiming Priority (8)

Application Number Priority Date Filing Date Title
US202163174177P 2021-04-13 2021-04-13
US63/174,177 2021-04-13
US202163239089P 2021-08-31 2021-08-31
US63/239,089 2021-08-31
US202163242837P 2021-09-10 2021-09-10
US63/242,837 2021-09-10
US202163292605P 2021-12-22 2021-12-22
US63/292,605 2021-12-22

Publications (1)

Publication Number Publication Date
TW202309022A true TW202309022A (zh) 2023-03-01

Family

ID=81392726

Family Applications (1)

Application Number Title Priority Date Filing Date
TW111113881A TW202309022A (zh) 2021-04-13 2022-04-12 用於治療具egfr突變之癌症之胺基取代雜環

Country Status (13)

Country Link
US (2) US12037346B2 (https=)
EP (1) EP4323356A1 (https=)
JP (2) JP7696443B2 (https=)
KR (2) KR20250151577A (https=)
AU (1) AU2022257621A1 (https=)
BR (1) BR112023021111A2 (https=)
CA (1) CA3213079A1 (https=)
CL (1) CL2023003020A1 (https=)
IL (1) IL306100A (https=)
MX (1) MX2023012060A (https=)
PE (1) PE20240327A1 (https=)
TW (1) TW202309022A (https=)
WO (1) WO2022221227A1 (https=)

Families Citing this family (15)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP4051286A1 (en) * 2019-10-29 2022-09-07 Institut National de la Santé et de la Recherche Médicale (INSERM) Methods and compositions for treating uveal melanoma
TW202214641A (zh) 2020-06-30 2022-04-16 美商艾瑞生藥股份有限公司 Her2突變抑制劑
EP4304586A4 (en) 2021-03-10 2025-04-02 Jnana Therapeutics Inc. SMALL MOLECULE INHIBITORS OF MAMMALIAN SLC6A19 FUNCTION
TW202309022A (zh) * 2021-04-13 2023-03-01 美商努法倫特公司 用於治療具egfr突變之癌症之胺基取代雜環
CR20230604A (es) * 2021-06-26 2024-02-19 Array Biopharma Inc Inhibidores de mutación de her2
WO2023081637A1 (en) 2021-11-02 2023-05-11 Enliven Therapeutics, Inc. Fused tetracyclic quinazoline derivatives as inhibitors of erbb2
CN117384162A (zh) * 2022-05-17 2024-01-12 浙江文达医药科技有限公司 选择性her2抑制剂
WO2024027695A1 (zh) * 2022-08-04 2024-02-08 微境生物医药科技(上海)有限公司 作为her2抑制剂的化合物
CN116082335B (zh) * 2023-01-16 2026-02-24 上海凌凯科技股份有限公司 一种二芳基醚化合物的制备方法
CN116789609A (zh) * 2023-03-03 2023-09-22 南京优氟医药科技有限公司 一种(r)-2-(哌嗪-2-基)乙腈盐酸盐的制备方法
WO2024215809A2 (en) * 2023-04-11 2024-10-17 Cogent Biosciences, Inc. Erbb2 inhibitors
WO2025051148A1 (zh) * 2023-09-05 2025-03-13 北京鞍石生物科技股份有限公司 含氮杂芳基化合物及其制备方法和应用
AU2024345242A1 (en) * 2023-09-22 2026-04-09 Hanmi Pharm. Co. Ltd. Novel skeletal derivative effective for her2 mutation, and pharmaceutical composition comprising same
WO2025195327A1 (zh) * 2024-03-19 2025-09-25 北京鞍石生物科技股份有限公司 螺环/桥环化合物及其制备方法和应用
WO2026081108A1 (en) * 2024-10-16 2026-04-23 The Regents Of The University Of California Compositions and methods for inhibiting egfr

Family Cites Families (371)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US510A (en) 1837-12-07 soeel
US949A (en) 1838-09-27 Improvement in roller cotton-gins for ginning long-staple and other kinds of cotton
US5861A (en) 1848-10-17 Locking umbrella and parasol
US5863A (en) 1848-10-17 Matthias p
US2779780A (en) 1955-03-01 1957-01-29 Du Pont 1, 4-diamino-2, 3-dicyano-1, 4-bis (substituted mercapto) butadienes and their preparation
GB1051218A (https=) 1963-03-09
US4172896A (en) 1978-06-05 1979-10-30 Dainippon Pharmaceutical Co., Ltd. Methane-sulfonamide derivatives, the preparation thereof and composition comprising the same
GB8827305D0 (en) 1988-11-23 1988-12-29 British Bio Technology Compounds
US5034393A (en) 1989-07-27 1991-07-23 Dowelanco Fungicidal use of pyridopyrimidine, pteridine, pyrimidopyrimidine, pyrimidopyridazine, and pyrimido-1,2,4-triazine derivatives
US5534520A (en) 1990-04-10 1996-07-09 Fisher; Abraham Spiro compounds containing five-membered rings
US5407938A (en) 1990-04-10 1995-04-18 Israel Institute For Biological Research Certain 1-methyl-piperidine-4-spiro-4'-(1'-3'-oxazolines) and corresponding -(1',3' thiazolines)
US5852029A (en) 1990-04-10 1998-12-22 Israel Institute For Biological Research Aza spiro compounds acting on the cholinergic system with muscarinic agonist activity
US5326776A (en) 1992-03-02 1994-07-05 Abbott Laboratories Angiotensin II receptor antagonists
WO1993017682A1 (en) 1992-03-04 1993-09-16 Abbott Laboratories Angiotensin ii receptor antagonists
GB9217295D0 (en) 1992-08-14 1992-09-30 Wellcome Found Controlled released tablets
EP0583861A1 (en) 1992-08-14 1994-02-23 Pioneer Electronic Corporation Organic electroluminescene device
US5455258A (en) 1993-01-06 1995-10-03 Ciba-Geigy Corporation Arylsulfonamido-substituted hydroxamic acids
US5358970A (en) 1993-08-12 1994-10-25 Burroughs Wellcome Co. Pharmaceutical composition containing bupropion hydrochloride and a stabilizer
GB9315856D0 (en) 1993-07-30 1993-09-15 Wellcome Found Stabilized pharmaceutical
US5541231A (en) 1993-07-30 1996-07-30 Glaxo Wellcome Inc. Stabilized Pharmaceutical
EP0647450A1 (en) 1993-09-09 1995-04-12 BEHRINGWERKE Aktiengesellschaft Improved prodrugs for enzyme mediated activation
IL112249A (en) 1994-01-25 2001-11-25 Warner Lambert Co Pharmaceutical compositions containing di and tricyclic pyrimidine derivatives for inhibiting tyrosine kinases of the epidermal growth factor receptor family and some new such compounds
IL112248A0 (en) 1994-01-25 1995-03-30 Warner Lambert Co Tricyclic heteroaromatic compounds and pharmaceutical compositions containing them
US5654307A (en) 1994-01-25 1997-08-05 Warner-Lambert Company Bicyclic compounds capable of inhibiting tyrosine kinases of the epidermal growth factor receptor family
TW414798B (en) 1994-09-07 2000-12-11 Thomae Gmbh Dr K Pyrimido (5,4-d) pyrimidines, medicaments comprising these compounds, their use and processes for their preparation
US5863949A (en) 1995-03-08 1999-01-26 Pfizer Inc Arylsulfonylamino hydroxamic acid derivatives
ES2153031T4 (es) 1995-04-20 2001-05-16 Pfizer Derivados del acido arilsulfonil hidroxamico como inhibidores de mmp y tnf.
US6232312B1 (en) 1995-06-07 2001-05-15 Cell Pathways, Inc. Method for treating patient having precancerous lesions with a combination of pyrimidopyrimidine derivatives and esters and amides of substituted indenyl acetic acides
US6395733B1 (en) 1995-06-07 2002-05-28 Pfizer Inc Heterocyclic ring-fused pyrimidine derivatives
JP3290666B2 (ja) 1995-06-07 2002-06-10 ファイザー・インコーポレーテッド 複素環式の縮合環ピリミジン誘導体
AR004010A1 (es) 1995-10-11 1998-09-30 Glaxo Group Ltd Compuestos heterociclicos
ATE225343T1 (de) 1995-12-20 2002-10-15 Hoffmann La Roche Matrix-metalloprotease inhibitoren
ZA9756B (en) 1996-01-16 1997-07-17 Warner Lambert Co Process for preparing 4,6-disubstituted pyrido[3,4-d]-pyrimidines
DE19608653A1 (de) 1996-03-06 1997-09-11 Thomae Gmbh Dr K Pyrimido[5,4-d]pyrimidine, diese Verbindungen enthaltende Arzneimittel, deren Verwendung und Verfahren zu ihrer Herstellung
DE19629652A1 (de) 1996-03-06 1998-01-29 Thomae Gmbh Dr K 4-Amino-pyrimidin-Derivate, diese Verbindungen enthaltende Arzneimittel, deren Verwendung und Verfahren zu ihrer Herstellung
DE19608588A1 (de) * 1996-03-06 1997-09-11 Thomae Gmbh Dr K Pyrimido [5,4-d]pyrimidine, diese Verbindungen enthaltende Arzneimittel, deren Verwendung und Verfahren zu ihrer Herstellung
JP3195756B2 (ja) 1996-07-04 2001-08-06 公子 吉水 潤滑補助体
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
EA199900021A1 (ru) 1996-07-13 1999-08-26 Глаксо, Груп Лимитед Бициклические гетероароматические соединения в качестве ингибиторов протеинтирозинкиназы
HRP970371A2 (en) 1996-07-13 1998-08-31 Kathryn Jane Smith Heterocyclic compounds
KR20000067904A (ko) 1996-07-18 2000-11-25 디. 제이. 우드, 스피겔 알렌 제이 매트릭스 메탈로프로테아제의 포스피네이트계 억제제
KR20000068248A (ko) 1996-08-23 2000-11-25 디. 제이. 우드, 스피겔 알렌 제이 아릴설포닐아미노 하이드록삼산 유도체
WO1998023613A1 (en) 1996-11-27 1998-06-04 Pfizer Inc. Fused bicyclic pyrimidine derivatives
ZA9711102B (en) 1996-12-16 1998-08-13 Yamanouchi Pharma Co Ltd N-[(substituted 5-membered heteroaryl)carbonyl] guanidine derivative
JP3338064B2 (ja) 1997-01-06 2002-10-28 ファイザー・インク 環状スルホン誘導体
NZ336840A (en) 1997-02-03 2001-01-26 Pfizer Prod Inc Arylsulfonylamino hydroxamic acid derivatives useful in the treatment of tumor necrosis factor and matrix metalloproteinase mediated diseases
JP2000507975A (ja) 1997-02-07 2000-06-27 ファイザー・インク N−ヒドロキシ−β−スルホニルプロピオンアミド誘導体類及びそれらのマトリックスメタロプロテイナーゼ阻害薬としての使用
EP0960098A1 (en) 1997-02-11 1999-12-01 Pfizer Inc. Arylsulfonyl hydroxamic acid derivatives
DE69839355T2 (de) 1997-07-29 2009-06-04 Alcon Laboratories, Inc., Fort Worth Ophthalmische Zusammensetzungen enthaltend Galaktomannanpolymere und Borat
CA2299355C (en) 1997-08-08 2005-09-27 Pfizer Products Inc. Aryloxyarylsulfonylamino hydroxamic acid derivatives
GB9725782D0 (en) 1997-12-05 1998-02-04 Pfizer Ltd Therapeutic agents
WO1999033172A1 (fr) 1997-12-22 1999-07-01 Hitachi, Ltd. Systeme d'amplification de puissance et terminal de communication radio mobile
RS49779B (sr) 1998-01-12 2008-06-05 Glaxo Group Limited, Biciklična heteroaromatična jedinjenja kao inhibitori protein tirozin kinaze
GB9801690D0 (en) 1998-01-27 1998-03-25 Pfizer Ltd Therapeutic agents
AU2483599A (en) 1998-01-29 1999-08-16 Sepracor, Inc. Pharmaceutical uses of optically pure (-)-bupropion
JP4462654B2 (ja) 1998-03-26 2010-05-12 ソニー株式会社 映像素材選択装置及び映像素材選択方法
PA8469501A1 (es) 1998-04-10 2000-09-29 Pfizer Prod Inc Hidroxamidas del acido (4-arilsulfonilamino)-tetrahidropiran-4-carboxilico
PA8469401A1 (es) 1998-04-10 2000-05-24 Pfizer Prod Inc Derivados biciclicos del acido hidroxamico
EP1004578B1 (en) 1998-11-05 2004-02-25 Pfizer Products Inc. 5-oxo-pyrrolidine-2-carboxylic acid hydroxamide derivatives
EP1143957A3 (en) 1998-12-16 2002-02-27 Warner-Lambert Company Treatment of arthritis with mek inhibitors
UA71945C2 (en) 1999-01-27 2005-01-17 Pfizer Prod Inc Substituted bicyclic derivatives being used as anticancer agents
JP3270834B2 (ja) 1999-01-27 2002-04-02 ファイザー・プロダクツ・インク 抗がん剤として有用なヘテロ芳香族二環式誘導体
DE19911510A1 (de) 1999-03-15 2000-09-21 Boehringer Ingelheim Pharma Bicyclische Heterocyclen, diese Verbindungen enthaltende Arzneimittel, deren Verwendung und Verfahren zu ihrer Herstellung
GB9906566D0 (en) 1999-03-23 1999-05-19 Zeneca Ltd Chemical compounds
IL129299A0 (en) 1999-03-31 2000-02-17 Mor Research Applic Ltd Monoclonal antibodies antigens and diagnosis of malignant diseases
EP1081137A1 (en) 1999-08-12 2001-03-07 Pfizer Products Inc. Selective inhibitors of aggrecanase in osteoarthritis treatment
US8889112B2 (en) 1999-09-16 2014-11-18 Ocularis Pharma, Llc Ophthalmic formulations including selective alpha 1 antagonists
CO5271670A1 (es) 1999-10-29 2003-04-30 Pfizer Prod Inc Antagonistas del factor de liberacion de corticitropina y composiciones relacionadas
DK1234031T3 (en) 1999-11-30 2017-07-03 Mayo Foundation B7-H1, AN UNKNOWN IMMUNE REGULATORY MOLECULE
EP1149583A3 (en) 2000-04-13 2001-11-14 Pfizer Products Inc. Combinations of corticotropin releasing factor antagonists and growth hormone secretagogues
JP3811775B2 (ja) 2000-07-19 2006-08-23 ワーナー−ランバート カンパニー リミティド ライアビリティー カンパニー 4−ヨードフェニルアミノベンズヒドロキサム酸の酸素化エステル
WO2002012227A2 (en) 2000-08-09 2002-02-14 Astrazeneca Ab Indole, azaindole and indazole derivatives having vegf inhibiting activity
US6995162B2 (en) 2001-01-12 2006-02-07 Amgen Inc. Substituted alkylamine derivatives and methods of use
DE60203260T2 (de) 2001-01-16 2006-02-02 Glaxo Group Ltd., Greenford Pharmazeutische kombination, die ein 4-chinazolinamin und paclitaxel, carboplatin oder vinorelbin enthält, zur behandlung von krebs
DE10115921A1 (de) 2001-03-30 2002-10-02 Boehringer Ingelheim Pharma Verfahren zur Herstellung von 4,6-Diaminopyrimido[5,4-d]pyrimidinen
ES2263743T3 (es) 2001-04-13 2006-12-16 Pfizer Products Inc. Derivados de 4-aminopiridopirimidina sustituidos con un grupo biciclico.
US7132438B2 (en) 2001-10-09 2006-11-07 Amgen Inc. Benzimidazole derivatives
JP4505228B2 (ja) 2002-01-10 2010-07-21 バイエル・シェーリング・ファルマ・アクチェンゲゼルシャフト Rho−キナーゼ阻害剤
PT1478648E (pt) 2002-02-01 2014-07-15 Ariad Pharma Inc Compostos contendo fósforo e suas utilizações
CN1653059A (zh) 2002-03-08 2005-08-10 卫材株式会社 用作医药品的大环化合物
KR100984595B1 (ko) 2002-03-13 2010-09-30 어레이 바이오파마 인크. Mek 억제제로서의 n3 알킬화 벤즈이미다졸 유도체
AU2003229305A1 (en) 2002-05-17 2003-12-02 Scios, Inc. TREATMENT OF FIBROPROLIFERATIVE DISORDERS USING TGF-Beta INHIBITORS
IL149820A0 (en) 2002-05-23 2002-11-10 Curetech Ltd Humanized immunomodulatory monoclonal antibodies for the treatment of neoplastic disease or immunodeficiency
AU2003281200A1 (en) 2002-07-03 2004-01-23 Tasuku Honjo Immunopotentiating compositions
US20040146509A1 (en) 2002-07-25 2004-07-29 Zhihe Li Methods for improvement of lung function using TGF-beta inhibitors
EP1575506A4 (en) 2002-07-25 2008-04-23 Scios Inc METHOD FOR IMPROVING LUNG FUNCTION WITH TGF-BETA INHIBITORS
US7488823B2 (en) 2003-11-10 2009-02-10 Array Biopharma, Inc. Cyanoguanidines and cyanoamidines as ErbB2 and EGFR inhibitors
CN101899114A (zh) 2002-12-23 2010-12-01 惠氏公司 抗pd-1抗体及其用途
US20060167026A1 (en) 2003-01-06 2006-07-27 Hiroyuki Nawa Antipsychotic molecular-targeting epithelial growth factor receptor
WO2007038613A2 (en) 2005-09-26 2007-04-05 The Regents Of The University Of California Selective serine/threonine kinase inhibitors
BRPI0410720A (pt) 2003-05-27 2006-06-20 Pfizer Prod Inc quinazolinas e pirido[3,4-d]pirimidinas como inibidores do receptor de tirosina cinase
US6933289B2 (en) 2003-07-01 2005-08-23 Allergan, Inc. Inhibition of irritating side effects associated with use of a topical ophthalmic medication
EP1654002B2 (en) 2003-08-07 2014-01-29 Allergan, Inc. Compositions for delivery of therapeutics into the eyes
US20050059744A1 (en) 2003-09-12 2005-03-17 Allergan, Inc. Methods and compositions for the treatment of pain and other alpha 2 adrenergic-mediated conditions
NZ590160A (en) 2003-11-21 2012-07-27 Array Biopharma Inc AKT protein kinase inhibitors
WO2005080377A1 (ja) 2004-02-20 2005-09-01 Kirin Beer Kabushiki Kaisha TGFβ阻害活性を有する化合物およびそれを含んでなる医薬組成物
WO2005110410A2 (en) 2004-05-14 2005-11-24 Abbott Laboratories Kinase inhibitors as therapeutic agents
US20090155247A1 (en) 2005-02-18 2009-06-18 Ashkenazi Avi J Methods of Using Death Receptor Agonists and EGFR Inhibitors
US20060188498A1 (en) 2005-02-18 2006-08-24 Genentech, Inc. Methods of using death receptor agonists and EGFR inhibitors
JO2787B1 (en) 2005-04-27 2014-03-15 امجين إنك, Alternative amide derivatives and methods of use
DK2439273T3 (da) 2005-05-09 2019-06-03 Ono Pharmaceutical Co Humane monoklonale antistoffer til programmeret død-1(pd-1) og fremgangsmåder til behandling af cancer ved anvendelse af anti-pd-1- antistoffer alene eller i kombination med andre immunterapeutika
GB0510139D0 (en) 2005-05-18 2005-06-22 Addex Pharmaceuticals Sa Novel compounds B1
KR101139038B1 (ko) 2005-06-28 2012-05-02 삼성전자주식회사 피리미도피리미딘 유도체 및 이를 이용한 유기 박막 트랜지스터
PT1907424E (pt) 2005-07-01 2015-10-09 Squibb & Sons Llc Anticorpos monoclonais humanos para o ligando 1 de morte programada (pd-l1)
CA2618218C (en) 2005-07-21 2015-06-30 Ardea Biosciences, Inc. N-(arylamino)-sulfonamide inhibitors of mek
US7880004B2 (en) 2005-09-15 2011-02-01 Bristol-Myers Squibb Company Met kinase inhibitors
US7547782B2 (en) 2005-09-30 2009-06-16 Bristol-Myers Squibb Company Met kinase inhibitors
ATE446294T1 (de) 2005-11-15 2009-11-15 Array Biopharma Inc N4-phenyl-chinazolin-4-aminderivate und verwandte verbindungen als inhibitoren der erbb-typ-i- rezeptortyrosinkinase zur behandlung hyperproliferativer krankheiten
TW200730527A (en) 2005-12-02 2007-08-16 Takeda Pharmaceuticals Co Fused heterocyclic compound
WO2007081517A2 (en) 2005-12-21 2007-07-19 Abbott Laboratories Anti-viral compounds
JO2660B1 (en) 2006-01-20 2012-06-17 نوفارتيس ايه جي Pi-3 inhibitors and methods of use
JP2009527459A (ja) 2006-02-23 2009-07-30 武田薬品工業株式会社 縮合窒素含有複素環化合物
US8129357B2 (en) 2006-04-07 2012-03-06 Academia Sinica Method of making and using an adenosine analogue
US7351434B2 (en) 2006-04-07 2008-04-01 Academia Sinica Therapeutic Gastrodia extracts
US8236950B2 (en) 2006-12-20 2012-08-07 Abbott Laboratories Anti-viral compounds
WO2008086462A2 (en) 2007-01-11 2008-07-17 Wyeth AMINO-SUBSTITUTED QUINAZOLINE DERIVATIVES AS INHIBITORS OF β-CANTENIN/TCF-4 PATHWAY AND CANCER TREATMENT AGENTS
US7776857B2 (en) 2007-04-05 2010-08-17 Amgen Inc. Aurora kinase modulators and method of use
EP1987839A1 (en) 2007-04-30 2008-11-05 I.N.S.E.R.M. Institut National de la Sante et de la Recherche Medicale Cytotoxic anti-LAG-3 monoclonal antibody and its use in the treatment or prevention of organ transplant rejection and autoimmune disease
US9244059B2 (en) 2007-04-30 2016-01-26 Immutep Parc Club Orsay Cytotoxic anti-LAG-3 monoclonal antibody and its use in the treatment or prevention of organ transplant rejection and autoimmune disease
US8633186B2 (en) 2007-06-08 2014-01-21 Senomyx Inc. Modulation of chemosensory receptors and ligands associated therewith
BR122017025062B8 (pt) 2007-06-18 2021-07-27 Merck Sharp & Dohme anticorpo monoclonal ou fragmento de anticorpo para o receptor de morte programada humano pd-1, polinucleotídeo e composição compreendendo o referido anticorpo ou fragmento
JP2009046453A (ja) 2007-08-22 2009-03-05 Takeda Chem Ind Ltd 縮合複素環化合物
EP2205242B1 (en) 2007-09-12 2015-04-15 Genentech, Inc. Combinations of phosphoinositide 3-kinase inhibitor compounds and chemotherapeutic agents, and methods of use
EP2044949A1 (en) 2007-10-05 2009-04-08 Immutep Use of recombinant lag-3 or the derivatives thereof for eliciting monocyte immune response
TWI552752B (zh) 2007-10-19 2016-10-11 賽基艾維洛米斯研究股份有限公司 雜芳基化合物及其用途
US7989465B2 (en) 2007-10-19 2011-08-02 Avila Therapeutics, Inc. 4,6-disubstituted pyrimidines useful as kinase inhibitors
JP5348725B2 (ja) 2007-10-25 2013-11-20 ジェネンテック, インコーポレイテッド チエノピリミジン化合物の製造方法
EP2262837A4 (en) 2008-03-12 2011-04-06 Merck Sharp & Dohme PD-1 BINDING PROTEINS
US7829574B2 (en) 2008-05-09 2010-11-09 Hutchison Medipharma Enterprises Limited Substituted quinazoline compounds and their use in treating angiogenesis-related diseases
CN101575333B (zh) 2008-05-09 2011-06-22 和记黄埔医药(上海)有限公司 一种喹唑啉衍生物及其医药用途
AU2009246263B2 (en) 2008-05-14 2014-08-21 Amgen Inc. Combinations VEGF(R) inhibitors and hepatocyte growth factor (c-Met) inhibitors for the treatment of cancer
AR072999A1 (es) 2008-08-11 2010-10-06 Medarex Inc Anticuerpos humanos que se unen al gen 3 de activacion linfocitaria (lag-3) y los usos de estos
JP2012500855A (ja) 2008-08-25 2012-01-12 アンプリミューン、インコーポレーテッド Pd−1アンタゴニストおよび感染性疾患を処置するための方法
TW201014860A (en) 2008-09-08 2010-04-16 Boehringer Ingelheim Int New chemical compounds
AU2009290544B2 (en) 2008-09-12 2015-07-16 Oxford University Innovation Limited PD-1 specific antibodies and uses thereof
US8552154B2 (en) 2008-09-26 2013-10-08 Emory University Anti-PD-L1 antibodies and uses therefor
WO2010042489A2 (en) 2008-10-06 2010-04-15 Emory University Aminoquinoline derived heat shock protein 90 inhibitors, methods of preparing same, and methods for their use
ES2599458T3 (es) 2008-10-14 2017-02-01 Sunshine Lake Pharma Co., Ltd. Compuestos y métodos de uso
JP5444365B2 (ja) 2008-10-29 2014-03-19 デシフェラ ファーマシューティカルズ,エルエルシー 抗癌活性および抗増殖活性を示すシクロプロパンアミドおよび類似物質
EP3255060A1 (en) 2008-12-09 2017-12-13 F. Hoffmann-La Roche AG Anti-pd-l1 antibodies and their use to enhance t-cell function
SG172352A1 (en) 2008-12-23 2011-07-28 Abbott Lab Anti-viral compounds
CN101759683B (zh) 2008-12-25 2011-12-28 哈尔滨誉衡药业股份有限公司 二氢化茚酰胺化合物制备方法、包含其的药物组合物、及其作为蛋白激酶抑制剂的应用
EP2398797B1 (en) 2009-02-17 2013-11-06 Boehringer Ingelheim International GmbH Pyrimido[5,4-d]pyrimidine derivatives for the inhibition of tyrosine kinases
PL2504364T3 (pl) 2009-11-24 2017-12-29 Medimmune Limited Ukierunkowane środki wiążące przeciwko B7-H1
WO2011066342A2 (en) 2009-11-24 2011-06-03 Amplimmune, Inc. Simultaneous inhibition of pd-l1/pd-l2
CN102086211B (zh) 2009-12-08 2013-09-11 广东东阳光药业有限公司 作为蛋白激酶抑制剂的芳杂环化合物
EP2545078A1 (en) 2010-03-11 2013-01-16 UCB Pharma, S.A. Pd-1 antibody
US20110312996A1 (en) 2010-05-17 2011-12-22 Intermune, Inc. Novel inhibitors of hepatitis c virus replication
AU2011262758B8 (en) 2010-06-11 2014-09-04 Kyowa Kirin Co., Ltd. Anti-tim-3 antibody
ES2526124T3 (es) 2010-06-16 2015-01-07 Cymabay Therapeutics, Inc. Agonistas del receptor GPR120 y sus usos
US8299117B2 (en) 2010-06-16 2012-10-30 Metabolex Inc. GPR120 receptor agonists and uses thereof
WO2011159877A2 (en) 2010-06-18 2011-12-22 The Brigham And Women's Hospital, Inc. Bi-specific antibodies against tim-3 and pd-1 for immunotherapy in chronic immune conditions
US8907053B2 (en) 2010-06-25 2014-12-09 Aurigene Discovery Technologies Limited Immunosuppression modulating compounds
ES2598530T3 (es) 2010-07-14 2017-01-27 Betta Pharmaceuticals Co., Ltd. Nuevos derivados heterocíclicos condensados útiles como inhibidores de la tirosina quinasa c-Met
CN102558147B (zh) 2010-12-23 2014-09-17 江苏先声药物研究有限公司 化合物、制备方法及应用
US20130023531A1 (en) 2011-01-27 2013-01-24 Boehringer Ingelheim International Gmbh Pyrimido[5,4-d]pyrimidylamino phenyl sulfonamides as serine/threonine kinase inhibitors
WO2012125668A1 (en) * 2011-03-17 2012-09-20 Merck Sharp & Dohme Corp. TrkA KINASE INHIBITORS, COMPOSITIONS AND METHODS THEREOF
JP6072771B2 (ja) 2011-04-20 2017-02-01 メディミューン,エルエルシー B7−h1およびpd−1に結合する抗体およびその他の分子
WO2013006490A2 (en) 2011-07-01 2013-01-10 Cellerant Therapeutics, Inc. Antibodies that specifically bind to tim3
CA2840018C (en) 2011-07-24 2019-07-16 Curetech Ltd. Variants of humanized immunomodulatory monoclonal antibodies
WO2013033981A1 (zh) 2011-09-06 2013-03-14 江苏先声药物研究有限公司 一类2,7-萘啶衍生物及其制备方法和应用
KR101764096B1 (ko) 2011-11-28 2017-08-02 메르크 파텐트 게엠베하 항-pd-l1 항체 및 그의 용도
CN102516232A (zh) * 2011-12-14 2012-06-27 无锡美克赛医药科技有限公司 一种ErbB2的小分子选择性抑制剂及其应用
TW201336847A (zh) 2012-02-07 2013-09-16 Taiho Pharmaceutical Co Ltd 喹啉基吡咯并嘧啶化合物或其鹽
JP6003976B2 (ja) 2012-02-22 2016-10-05 コニカミノルタ株式会社 光学フィルム、円偏光板および画像表示装置
DK2722332T3 (en) 2012-02-23 2016-06-20 Taiho Pharmaceutical Co Ltd Quinolylpyrrolopyrimidylforbindelse with concentrated ring or salt thereof.
KR20220084444A (ko) 2012-05-31 2022-06-21 소렌토 쎄라퓨틱스, 인코포레이티드 Pd-l1에 결합하는 항원 결합 단백질
UY34887A (es) 2012-07-02 2013-12-31 Bristol Myers Squibb Company Una Corporacion Del Estado De Delaware Optimización de anticuerpos que se fijan al gen de activación de linfocitos 3 (lag-3) y sus usos
CN111499755A (zh) 2012-08-03 2020-08-07 丹娜法伯癌症研究院 抗-pd-l1和pd-l2双结合抗体单一试剂及其使用方法
BR112015007672A2 (pt) 2012-10-04 2017-08-08 Dana Farber Cancer Inst Inc anticorpos anti-pd-l1 monoclonais humanos e métodos de uso
AR093984A1 (es) 2012-12-21 2015-07-01 Merck Sharp & Dohme Anticuerpos que se unen a ligando 1 de muerte programada (pd-l1) humano
US10344088B2 (en) 2013-03-15 2019-07-09 Glaxosmithkline Intellectual Property Development Limited Antigen binding proteins
SMT202100065T1 (it) 2013-05-02 2021-03-15 Anaptysbio Inc Anticorpi diretti contro la proteina della morte programmata (pd-1)
US20140336182A1 (en) 2013-05-13 2014-11-13 Amgen Inc. Aurora Kinase Modulators and Method of Use
WO2014194302A2 (en) 2013-05-31 2014-12-04 Sorrento Therapeutics, Inc. Antigen binding proteins that bind pd-1
US20160145355A1 (en) 2013-06-24 2016-05-26 Biomed Valley Discoveries, Inc. Bispecific antibodies
BR112016003247B1 (pt) 2013-08-22 2022-05-10 Taiho Pharmaceutical Co., Ltd Composto substituído por quinolina, composição farmacêutica compreendendo o referido composto e seu uso
CN112552401B (zh) 2013-09-13 2023-08-25 广州百济神州生物制药有限公司 抗pd1抗体及其作为治疗剂与诊断剂的用途
EP3060581A4 (en) 2013-10-25 2017-06-07 Dana-Farber Cancer Institute, Inc. Anti-pd-l1 monoclonal antibodies and fragments thereof
WO2015081158A1 (en) 2013-11-26 2015-06-04 Bristol-Myers Squibb Company Method of treating hiv by disrupting pd-1/pd-l1 signaling
WO2015085238A1 (en) 2013-12-05 2015-06-11 The Regents Of The University Of California, A California Corporation Inhibitors of lpxc
ES2750236T3 (es) 2013-12-09 2020-03-25 UCB Biopharma SRL Derivados heteroaromáticos bicíclicos condensados como moduladores de la actividad del TNF
SG10201804945WA (en) 2013-12-12 2018-07-30 Shanghai hengrui pharmaceutical co ltd Pd-1 antibody, antigen-binding fragment thereof, and medical application thereof
PL3094351T3 (pl) 2014-01-15 2022-06-27 Kadmon Corporation, Llc Środki immunomodulujące
TWI681969B (zh) 2014-01-23 2020-01-11 美商再生元醫藥公司 針對pd-1的人類抗體
TWI680138B (zh) 2014-01-23 2019-12-21 美商再生元醫藥公司 抗pd-l1之人類抗體
PE20170255A1 (es) 2014-01-24 2017-03-22 Dana Farber Cancer Inst Inc Moleculas de anticuerpo que se unen a pd-1 y usos de las mismas
HUE057817T2 (hu) 2014-01-28 2022-06-28 Bristol Myers Squibb Co Anti-LAG-3 antitestek haematológiai malignitások kezelésére
IL310627B2 (en) 2014-01-31 2026-04-01 Daiichi Sankyo Co Ltd Anti-HER2 antibody-drug conjugates, compositions containing them and uses thereof
HUE045065T2 (hu) 2014-01-31 2019-12-30 Novartis Ag TIM-3 antitest molekulák és felhasználásaik
KR102442436B1 (ko) 2014-03-14 2022-09-15 노파르티스 아게 Lag-3에 대한 항체 분자 및 그의 용도
JP6568926B2 (ja) 2014-03-20 2019-08-28 カペラ セラピューティクス,インコーポレーテッド 癌の治療のためのerbbチロシンキナーゼ阻害剤としてのベンゾイミダゾール誘導体
JP6468611B2 (ja) 2014-05-13 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 キナーゼ阻害のためのヘテロアリール化合物
JP6666905B2 (ja) 2014-05-29 2020-03-18 スプリング バイオサイエンス コーポレーション Pd−l1抗体及びその使用
EP3778584A1 (en) 2014-06-19 2021-02-17 ARIAD Pharmaceuticals, Inc. Production process of 2-chloro-4-heteroaryl-pyrimidine derivatives
WO2015195163A1 (en) 2014-06-20 2015-12-23 R-Pharm Overseas, Inc. Pd-l1 antagonist fully human antibody
TWI693232B (zh) 2014-06-26 2020-05-11 美商宏觀基因股份有限公司 與pd-1和lag-3具有免疫反應性的共價結合的雙抗體和其使用方法
CN106604742B (zh) 2014-07-03 2019-01-11 百济神州有限公司 抗pd-l1抗体及其作为治疗剂及诊断剂的用途
JO3663B1 (ar) 2014-08-19 2020-08-27 Merck Sharp & Dohme الأجسام المضادة لمضاد lag3 وأجزاء ربط الأنتيجين
EP4245376A3 (en) 2014-10-14 2023-12-13 Novartis AG Antibody molecules to pd-l1 and uses thereof
SI3215532T1 (sl) 2014-11-06 2020-02-28 F. Hoffmann-La Roche Ag Protitelesa proti TIM3 in postopki uporabe
TWI595006B (zh) 2014-12-09 2017-08-11 禮納特神經系統科學公司 抗pd-1抗體類和使用彼等之方法
WO2016111947A2 (en) 2015-01-05 2016-07-14 Jounce Therapeutics, Inc. Antibodies that inhibit tim-3:lilrb2 interactions and uses thereof
WO2016110821A1 (en) 2015-01-08 2016-07-14 Advinus Therapeutics Limited Bicyclic compounds, compositions and medicinal applications thereof
WO2016128908A1 (en) 2015-02-12 2016-08-18 Advinus Therapeutics Limited Bicyclic compounds, compositions and medicinal applications thereof
EP3265486A4 (en) 2015-03-06 2018-11-14 Sorrento Therapeutics, Inc. Antibody therapeutics that bind tim3
FI3277321T3 (fi) 2015-04-01 2024-10-31 Anaptysbio Inc T-soluimmunoglobuliinia ja musiiniproteiini 3:a (tim-3) vastaan suunnattuja vasta-aineita
GB201505658D0 (en) 2015-04-01 2015-05-13 Cancer Rec Tech Ltd Inhibitor compounds
CN104876912B (zh) 2015-04-08 2017-07-21 苏州云轩医药科技有限公司 Wnt信号通路抑制剂及其应用
EP3294712A4 (en) 2015-05-13 2018-11-07 ARIAD Pharmaceuticals, Inc. Heteroaryl compounds for kinase inhibition
WO2016191471A1 (en) 2015-05-27 2016-12-01 Metastat, Inc. Method of use for inhibitors of epidermal growth factor receptor variants ii, iii and vi
TWI703150B (zh) 2015-06-04 2020-09-01 美商庫拉腫瘤技術股份有限公司 用於抑制menin及mll蛋白之交互作用的方法及組合物
KR20240158360A (ko) 2015-10-09 2024-11-04 베링거 인겔하임 인터내셔날 게엠베하 Mdm2-p53 억제제로서의 스피로[3h-인돌-3,2'-피롤리딘]-2(1h)-온 화합물 및 유도체
AU2016342352B2 (en) 2015-10-23 2022-06-02 Sunesis Pharmaceuticals, Inc. Heterocyclic PDK1 inhibitors for use to treat cancer
AU2016379372A1 (en) 2015-12-22 2018-08-02 Incyte Corporation Heterocyclic compounds as immunomodulators
CN108541255B (zh) 2016-02-02 2019-06-14 深圳市塔吉瑞生物医药有限公司 一种甾体类化合物及包含该化合物的组合物及其用途
WO2017148391A1 (zh) 2016-03-01 2017-09-08 上海医药集团股份有限公司 一种含氮杂环化合物、制备方法、中间体、组合物和应用
US11213520B2 (en) 2016-05-23 2022-01-04 Boehringer Ingelheim International Gmbh Phenylpyrazolylacetamide compounds and derivatives as CDK8/CDK19 inhibitors
WO2018079310A1 (ja) 2016-10-31 2018-05-03 大鵬薬品工業株式会社 エクソン20挿入変異型egfr選択的阻害剤
CN108101905A (zh) 2016-11-24 2018-06-01 中国科学院上海药物研究所 嘧啶并[5,4-b]吲嗪或嘧啶并[5,4-b]吡呤化合物、其制备方法及用途
EP3558979B1 (en) 2016-12-22 2021-02-17 Boehringer Ingelheim International GmbH Novel benzylamino substituted quinazolines and derivatives as sos1 inhibitors
JP2020514370A (ja) 2017-03-17 2020-05-21 キュアバック アーゲー 組合せ抗癌療法のためのrnaワクチン及び免疫チェックポイント阻害剤
US20180303821A1 (en) 2017-04-24 2018-10-25 BraneQuest, Inc. Membrane active molecules
FR3066761B1 (fr) 2017-05-23 2020-10-30 Centre Nat Rech Scient Nouveaux composes inhibiteurs des canaux ioniques
CN109020957B (zh) 2017-06-12 2023-01-13 南京天印健华医药科技有限公司 作为mnk抑制剂的杂环化合物
WO2019023621A1 (en) 2017-07-28 2019-01-31 Yale University ANTICANCER DRUGS AND METHODS OF MAKING AND USING THEM
CN111032655B (zh) 2017-08-31 2022-09-02 达纳-法伯癌症研究所股份有限公司 Egfr和/或her2抑制剂和使用方法
TW201920104A (zh) 2017-08-31 2019-06-01 美商馬愈法瑪公司 外核苷酸焦磷酸酶-磷酸二酯酶1(enpp-1)抑制劑及其用途
PL3677266T3 (pl) 2017-09-01 2024-07-01 Taiho Pharmaceutical Co., Ltd. Selektywny inhibitor egfr z mutacją w eksonie 18 i/lub eksonie 21
JP7333313B2 (ja) 2017-09-01 2023-08-24 シャンハイ ファーマシューティカルズ ホールディング カンパニー,リミティド 窒素含有複素環化合物、製造方法、中間体、組成物および使用
CN111868039A (zh) 2017-09-26 2020-10-30 加利福尼亚大学董事会 用于治疗癌症的组合物和方法
WO2019068613A1 (en) 2017-10-02 2019-04-11 Boehringer Ingelheim International Gmbh NOVEL [1,6] NAPHTHYRIDINE COMPOUNDS AND DERIVATIVES AS CDK8 / CDK19 INHIBITORS
EP3700904B1 (en) 2017-10-24 2023-07-19 Bayer AG 4h-pyrrolo[3,2-c]pyridin-4-one derivatives
HRP20230400T1 (hr) 2017-12-21 2023-06-23 Boehringer Ingelheim International Gmbh Benzilamino supstituirani piridopirimidinoni i derivati kao inhibitori sos1
CN108490184B (zh) 2018-01-26 2021-01-08 中国科学院化学研究所 人pot1蛋白在白血病诊断中的用途
CR20250117A (es) 2018-01-26 2025-05-09 Exelixis Inc COMPUESTOS PARA EL TRATAMIENTO DE TRASTORNOS DEPENDIENTES DE CINASAS (Divisional 2020-0355)
TWI798334B (zh) 2018-01-31 2023-04-11 大陸商迪哲(江蘇)醫藥股份有限公司 Erbb/btk抑制劑
JP7313364B2 (ja) 2018-02-21 2023-07-24 ベーリンガー インゲルハイム インターナショナル ゲゼルシャフト ミット ベシュレンクテル ハフツング Egfr阻害剤としての新たなベンズイミダゾール化合物および誘導体
JP2021104931A (ja) 2018-02-22 2021-07-26 大日本住友製薬株式会社 含窒素複素環を有するジベンゾアゼピン誘導体
EP3755323A4 (en) 2018-02-23 2021-11-24 The Regents Of The University Of Michigan EGFR DIMER DISRUPTORS AND THEIR USES
WO2019170088A1 (zh) 2018-03-06 2019-09-12 北京赛特明强医药科技有限公司 一种噁嗪并喹唑啉与噁嗪并喹啉类化合物及其制备方法和应用
WO2019177374A1 (ko) 2018-03-13 2019-09-19 포로노이바이오 주식회사 2, 4, 5-치환된 피리미딘 유도체, 이의 제조방법 및 이를 유효성분으로 포함하는 암 또는 염증질환의 예방 또는 치료용 약학적 조성물
WO2019177375A1 (ko) 2018-03-13 2019-09-19 포로노이바이오 주식회사 2, 4, 5-치환된 피리미딘 유도체, 이의 제조방법 및 이를 유효성분으로 포함하는 암의 예방 또는 치료용 약학적 조성물
WO2019214651A1 (zh) 2018-05-08 2019-11-14 南京明德新药研发有限公司 作为选择性HER2抑制剂的吡咯并[2,1-f][1,2,4]三嗪类衍生物及其应用
TWI858848B (zh) 2018-05-08 2024-10-11 大陸商迪哲(江蘇)醫藥股份有限公司 ErbB受體抑制劑
JP2021523208A (ja) 2018-05-14 2021-09-02 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 ピリミジン誘導体の医薬塩及び障害の処置方法
EP3569618A1 (en) 2018-05-19 2019-11-20 Boehringer Ingelheim International GmbH Antagonizing cd73 antibody
US11485713B2 (en) 2018-05-25 2022-11-01 Essa Pharma, Inc. Androgen receptor modulators and methods for their use
WO2019228403A1 (en) 2018-05-29 2019-12-05 Fronthera U.S. Pharmaceuticals Llc Autotaxin inhibitors and uses thereof
CN112236417A (zh) 2018-06-14 2021-01-15 达纳-法伯癌症研究所股份有限公司 作为her2抑制剂的氰基喹啉酰胺化合物及使用方法
TW202012391A (zh) 2018-07-04 2020-04-01 日商第一三共股份有限公司 二芳基醚型喹唑啉衍生物
US20210347785A1 (en) 2018-08-01 2021-11-11 Shanghai Ennovabio Pharmaceuticals Co., Ltd. Preparation and application of aromatic compound having immunoregulatory function
US11945803B2 (en) 2018-08-07 2024-04-02 Tosk, Inc. Modulators of RAS GTPase
EP3833372A4 (en) 2018-08-10 2022-06-08 Blueprint Medicines Corporation TREATMENT OF EGFR MUTANT CANCER
EP4523755A3 (en) 2018-09-18 2025-06-11 F. Hoffmann-La Roche AG Quinazoline derivatives as antitumor agents
CN113056272A (zh) 2018-09-21 2021-06-29 光谱医药公司 新的喹唑啉egfr抑制剂
JP2022502495A (ja) 2018-09-25 2022-01-11 ブラック ダイアモンド セラピューティクス,インコーポレイティド チロシンキナーゼ阻害剤としてのキナゾリン誘導体、組成物、それらの作製方法、およびそれらの使用
US20220041613A1 (en) 2018-09-25 2022-02-10 Black Diamond Therapeutics, Inc. Tyrosine kinase inhibitor compositions, methods of making and methods of use
CN111171020A (zh) 2018-11-13 2020-05-19 上海轶诺药业有限公司 一类六元并六元杂环化合物及其作为蛋白受体激酶抑制剂的用途
WO2020108613A1 (zh) 2018-11-30 2020-06-04 江苏豪森药业集团有限公司 杂芳类衍生物调节剂、其制备方法和应用
ES3033635T3 (en) 2018-12-28 2025-08-06 Taiho Pharmaceutical Co Ltd L718 and/or l792 mutant treatment-resistant egfr inhibitor for use in the treatment of cancer
KR102809395B1 (ko) 2019-03-15 2025-05-16 더 리전트 오브 더 유니버시티 오브 캘리포니아 암을 치료하기 위한 조성물 및 방법
PT3943491T (pt) 2019-03-19 2025-07-28 Voronoi Inc Derivado de heteroarilo, método para a produção do mesmo e composição farmacêutica que compreende o mesmo como componente eficaz
CN109912572B (zh) 2019-03-29 2020-11-06 武汉德诺美生物医药股份有限公司 Egfr抑制剂及其医药用途
DK3959211T3 (da) 2019-04-24 2026-04-27 Bayer Ag 4h-pyrrol[3,2-c]pyridin-4-on-forbindelser
EP3962908A4 (en) 2019-04-25 2022-10-26 Board of Regents, The University of Texas System HETEROCYCLIC INHIBITORS OF TYROSINE KINASE
CN112079830B (zh) 2019-06-14 2023-12-22 上海翰森生物医药科技有限公司 含并环类衍生物抑制剂、其制备方法和应用
WO2020260252A1 (en) 2019-06-24 2020-12-30 Boehringer Ingelheim International Gmbh New macrocyclic compounds and derivatives as egfr inhibitors
AU2020328598A1 (en) 2019-08-15 2022-03-03 Black Diamond Therapeutics, Inc. Alkynyl quinazoline compounds
WO2021057877A1 (zh) 2019-09-26 2021-04-01 深圳市塔吉瑞生物医药有限公司 取代的芳香稠合环衍生物及其组合物及用途
WO2021062327A1 (en) 2019-09-27 2021-04-01 Jubilant Biosys Limited Fused pyrimidine compounds, compositions and medicinal applications thereof
CN115181104A (zh) 2019-09-29 2022-10-14 深圳市塔吉瑞生物医药有限公司 取代的稠合三环衍生物及其组合物及用途
WO2021127456A1 (en) 2019-12-19 2021-06-24 Rain Therapeutics Inc. Methods of inhibiting epidermal growth factor receptor proteins
WO2021127397A1 (en) 2019-12-19 2021-06-24 Black Diamond Therapeutics, Inc. Nitrogen heterocyclic compounds and methods of use
MX2022007969A (es) 2019-12-23 2022-12-13 Blueprint Medicines Corp Inhibidores de egfr.
EP4100409B1 (en) 2020-02-03 2024-08-28 Boehringer Ingelheim International GmbH [1,3]diazino[5,4-d]pyrimidines as her2 inhibitors
JP7626774B2 (ja) 2020-02-03 2025-02-04 ベーリンガー インゲルハイム インターナショナル ゲゼルシャフト ミット ベシュレンクテル ハフツング HER2阻害薬としての[1,3]ジアジノ[5,4-d]ピリミジン
WO2021164697A1 (zh) 2020-02-18 2021-08-26 深圳市塔吉瑞生物医药有限公司 取代的酰胺衍生物及其组合物及用途
WO2021179274A1 (en) 2020-03-13 2021-09-16 Suzhou Zanrong Pharma Ltd. ErbB RECEPTOR INHIBITORS AS ANTI-TUMOR AGENTS
CN113493439B (zh) 2020-03-20 2022-10-14 深圳市塔吉瑞生物医药有限公司 取代的丙烯酰胺衍生物及其组合物及用途
EP4126861B1 (en) 2020-03-31 2025-06-18 Bayer Aktiengesellschaft 3-(anilino)-2-[3-(3-alkoxy-pyridin-4-yl]-1,5,6,7-tetrahydro-4h-pyrrolo[3,2-c]pyridin-4-one derivatives as egfr inhibitors for the treatment of cancer
US11608343B2 (en) 2020-04-24 2023-03-21 Boehringer Ingelheim International Gmbh Substituted pyrimido[5,4-d]pyrimidines as HER2 inhibitors
EP4146205A4 (en) 2020-05-05 2024-05-29 Nuvalent, Inc. HETEROAROMATIC MACROCYCLIC ETHERS AS CHEMOTHERAPEUTIC AGENTS
IL297832A (en) 2020-05-05 2023-01-01 Nuvalent Inc Macrocyclic heteroaromatic chemotherapeutic agents
KR102860318B1 (ko) 2020-05-07 2025-09-16 삼성디스플레이 주식회사 유기 발광 소자 및 이를 포함한 전자 장치
WO2021231400A1 (en) 2020-05-12 2021-11-18 Accutar Biotechnology, Inc. Bis-aryl ethers containing n-acyl azetidine as egfr/her2 inhibitors
WO2021243596A1 (en) 2020-06-03 2021-12-09 InventisBio Co., Ltd. Aminopyrimidine compounds, preparation methods and uses thereof
CN113861195B (zh) 2020-06-30 2022-11-18 上海和誉生物医药科技有限公司 一种多稠环egfr抑制剂及其制备方法和应用
TW202214641A (zh) 2020-06-30 2022-04-16 美商艾瑞生藥股份有限公司 Her2突變抑制劑
CN113880804A (zh) 2020-07-01 2022-01-04 微境生物医药科技(上海)有限公司 新型苯并咪唑化合物
WO2022006386A1 (en) 2020-07-02 2022-01-06 Enliven Therapeutics, Inc. Alkyne quinazoline derivatives as inhibitors of erbb2
CN116096372B (zh) 2020-07-09 2024-09-03 上海和誉生物医药科技有限公司 一种egfr抑制剂、其制备方法和在药学上的应用
CN113943288A (zh) 2020-07-17 2022-01-18 微境生物医药科技(上海)有限公司 5,6-二氢吡嗪并[2,3-c]异喹啉化合物
CN115836070B (zh) 2020-08-10 2024-08-09 上海和誉生物医药科技有限公司 作为egfr抑制剂的稠环化合物及其制备方法和应用
EP4194443A4 (en) 2020-08-10 2024-10-09 Abbisko Therapeutics Co., Ltd. Efgr inhibitor, preparation method therefor, and application thereof
WO2022033455A1 (zh) 2020-08-13 2022-02-17 上海和誉生物医药科技有限公司 具有egfr抑制活性的三嗪衍生物及其制备方法和应用
TW202220994A (zh) 2020-08-17 2022-06-01 大陸商貝達藥業股份有限公司 雙環化合物,包含其的藥物組合物及其用途
WO2022042755A1 (zh) 2020-08-28 2022-03-03 华东理工大学 抑制突变型egfr的化合物及其应用
WO2022055895A1 (en) 2020-09-08 2022-03-17 Cullinan Pearl Corp. Treatment regimens for exon-20 insertion mutant egfr cancers
MX2023002884A (es) 2020-09-14 2023-03-31 Boehringer Ingelheim Int Vacuna heterologa de estimulo primario.
TW202227425A (zh) 2020-09-18 2022-07-16 南韓商沃若諾伊生物公司 雜芳基衍生物、彼之製法、及包含彼作為活性成份之藥學組成物
KR20230094197A (ko) 2020-09-23 2023-06-27 스코르피온 테라퓨틱스, 인코퍼레이티드 암 치료에 유용한 피롤로[3,2-c]피리딘-4-온 유도체들
WO2022072645A2 (en) 2020-09-30 2022-04-07 Scorpion Therapeutics, Inc. Methods for treating cancer
TW202229282A (zh) 2020-09-30 2022-08-01 美商史考皮恩治療有限公司 治療癌症之方法
WO2022072632A1 (en) 2020-09-30 2022-04-07 Scorpion Therapeutics, Inc. Bicyclic compounds for use in the treatment cancer
CA3194724A1 (en) 2020-10-05 2022-04-14 Dana-Farber Cancer Institute, Inc. Potent and selective inhibitors of her2
WO2022076671A1 (en) 2020-10-08 2022-04-14 Black Diamond Therapeutics, Inc. Method of treating cancers using quinazoline derivatives
KR20230107419A (ko) 2020-10-09 2023-07-14 스코르피온 테라퓨틱스, 인코퍼레이티드 암 치료 방법
JP2023545178A (ja) 2020-10-14 2023-10-26 ベーリンガー インゲルハイム インターナショナル ゲゼルシャフト ミット ベシュレンクテル ハフツング Stingアゴニストと、細胞透過性ペプチド、カーゴ、及びtlrペプチドアゴニストを含む複合体との組合せ
WO2023077259A1 (en) 2021-11-02 2023-05-11 Enliven Therapeutics, Inc. Fused tetracyclic quinazoline derivatives as inhibitors of erbb2
WO2022094271A1 (en) 2020-10-30 2022-05-05 Scorpion Therapeutics, Inc. Methods for treating cancer
US20240051945A1 (en) 2020-10-30 2024-02-15 Blueprint Medicines Corporation Pyrimidine compounds, compositions, and medicinal applications thereof
JP2023549074A (ja) 2020-10-30 2023-11-22 ブループリント メディシンズ コーポレイション ピリミジン化合物、組成物、及びその医薬用途
US12064421B2 (en) 2020-11-02 2024-08-20 Boehringer Ingelheim International Gmbh Substituted 1H-pyrazolo[4,3-c]pyridines and derivatives as EGFR inhibitors
WO2022098992A1 (en) 2020-11-05 2022-05-12 Scorpion Therapeutics, Inc. Use of macrocyclic compounds in methods of treating cancer
EP4244225A1 (en) 2020-11-11 2023-09-20 Bayer Aktiengesellschaft N-[2-({4-[3-(anilino)-4-oxo-4,5,6,7-tetrahydro-1h-pyrrolo[3,2-c]pyridin-2-yl]pyridin-3-yl)oxy)ethyl]prop-2-enamide derivatives and similar compounds as egfr inhibitors for the treatment of cancer
CN114539226B (zh) 2020-11-19 2026-02-13 上海翰森生物医药科技有限公司 一种含吲哚类衍生物自由碱的晶型及其制备方法和应用
TW202222795A (zh) 2020-11-19 2022-06-16 大陸商上海翰森生物醫藥科技有限公司 一種含吲哚類衍生物的鹽、晶型及其製備方法和應用
WO2022105908A1 (zh) 2020-11-23 2022-05-27 上海和誉生物医药科技有限公司 Egfr抑制剂及其制备方法与在药学上的应用
CN115867539B (zh) 2020-12-02 2025-07-22 上海和誉生物医药科技有限公司 2,3-二氢-1H-吡咯并[3,2-b]吡啶衍生物、其制备方法和应用
CN114621207B (zh) 2020-12-11 2025-02-11 广东东阳光药业股份有限公司 一种作为甲状腺激素β受体激动剂的化合物及其用途
WO2022139386A1 (ko) 2020-12-21 2022-06-30 주식회사 비투에스바이오 헤테로아릴 유도체 화합물 및 이의 용도
EP4267137A4 (en) 2020-12-22 2024-11-06 Enliven Inc. HETEROARYL-LACTAM-FUSION PYRIMIDINE DERIVATIVES AS ERBB2 INHIBITORS
KR20220097305A (ko) 2020-12-29 2022-07-07 주식회사 비투에스바이오 헤테로아릴 유도체 화합물 및 이의 용도
PY21113397A (es) 2020-12-29 2022-10-12 Spectrum Pharmaceuticals Inc Tratamiento para tumores sólidos malignos
US20240398805A1 (en) 2021-02-05 2024-12-05 Accutar Biotechnology Inc. Quinazoline derived compounds as egfr inhibitors and their uses thereof
WO2022166916A1 (zh) 2021-02-05 2022-08-11 深圳市塔吉瑞生物医药有限公司 取代的杂芳基衍生物及其组合物及用途
WO2022170052A1 (en) 2021-02-05 2022-08-11 Black Diamond Therapeutics, Inc. Quinazoline derivatives, pyridopyrimidine derivatives, pyrimidopyrimidine derivatives, and uses thereof
CN114907356A (zh) 2021-02-10 2022-08-16 上海医药集团股份有限公司 一种含氮杂环化合物的晶型、其制备方法及应用
EP4304727A1 (en) 2021-03-10 2024-01-17 Blueprint Medicines Corporation Egfr inhibitors
WO2022191664A1 (ko) 2021-03-11 2022-09-15 주식회사 온코빅스 암세포 성장 억제 효과를 나타내는 신규한 피리미딘 유도체
CN117015549A (zh) 2021-03-17 2023-11-07 江苏恒瑞医药股份有限公司 一种喜树碱衍生物的制备方法
WO2022197913A1 (en) 2021-03-18 2022-09-22 Scorpion Therapeutics, Inc. Bicyclic derivatives which can be used to treat cancer
CN115109036B (zh) 2021-03-19 2024-06-11 北京赛特明强医药科技有限公司 一种喹唑啉类化合物、组合物及其应用
US20240217977A1 (en) 2021-03-31 2024-07-04 Blueprint Medicines Corporation Diazepanone-fused pyrimidine compounds, compositions and medicinal applications thereof
WO2022206929A1 (zh) 2021-04-01 2022-10-06 上海医药集团股份有限公司 一种化合物在制备靶向ErbB2突变体的抑制药物中的应用
TW202309022A (zh) 2021-04-13 2023-03-01 美商努法倫特公司 用於治療具egfr突變之癌症之胺基取代雜環
WO2022225238A1 (ko) 2021-04-22 2022-10-27 보로노이 주식회사 헤테로아릴 유도체 화합물 및 이의 용도
EP4335847A1 (en) 2021-05-07 2024-03-13 Voronoi Inc. Heteroaryl derivative, method for preparing same, and pharmaceutical composition comprising same as active ingredient
WO2022237825A1 (zh) 2021-05-13 2022-11-17 上海和誉生物医药科技有限公司 具有egfr抑制活性的氮杂芳基衍生物、其制备方法和应用
CN115667251A (zh) 2021-05-17 2023-01-31 株式会社沃若诺伊生物 杂芳基衍生物化合物、及其用途
JP2024520461A (ja) 2021-05-24 2024-05-24 大鵬薬品工業株式会社 Egfr及び/又はher2に異常を有するがんを有する対象の治療方法
TW202317620A (zh) 2021-06-04 2023-05-01 德商百靈佳殷格翰國際股份有限公司 抗SIRPα抗體
WO2022266458A1 (en) 2021-06-17 2022-12-22 Black Diamond Therapeutics, Inc. 6-heterocycloalkyl-quinazoline derivatives and uses thereof
WO2022266426A1 (en) 2021-06-17 2022-12-22 Black Diamond Therapeutics, Inc. 6-(heterocycloalkyl-oxy)-quinazoline derivatives and uses thereof
WO2022266425A1 (en) 2021-06-17 2022-12-22 Black Diamond Therapeutics, Inc. 3-cyano-quinoline derivatives and uses thereof
WO2022266427A1 (en) 2021-06-17 2022-12-22 Black Diamond Therapeutics, Inc. 4-(aryl-methyl-amino)-quinazoline derivatives and uses thereof
US20240299387A1 (en) 2021-06-22 2024-09-12 Blueprint Medicines Corporation Heterocyclic egfr inhibitors for use in the treatment of cancer
CN117940424A (zh) 2021-06-22 2024-04-26 缆图药品公司 Egfr抑制剂
WO2022271613A1 (en) 2021-06-22 2022-12-29 Blueprint Medicines Corporation Heterocyclic egfr inhibitors for use in the treatment of cancer
CN117858872A (zh) 2021-06-22 2024-04-09 缆图药品公司 用于治疗癌症的杂环egfr抑制剂
JP2024523506A (ja) 2021-06-23 2024-06-28 ブループリント メディシンズ コーポレイション 上皮成長因子受容体阻害剤の塩及び結晶形態
AR126196A1 (es) 2021-06-23 2023-09-27 Blueprint Medicines Corp Proceso para preparar inhibidores de egfr
CR20230604A (es) 2021-06-26 2024-02-19 Array Biopharma Inc Inhibidores de mutación de her2
CA3226006A1 (en) 2021-07-13 2023-01-19 Korea Research Institute Of Chemical Technology Novel pyrimidine-2,4-diamine derivatives, preparation method therefor, and pharmaceutical composition containing same as active ingredient for prevention or treatment of cancer
US20240391931A1 (en) 2021-08-05 2024-11-28 Bristol-Myers Squibb Company Tricyclic fused pyrimidine compounds for use as her2 inhibitors
AU2022322671A1 (en) 2021-08-05 2024-02-29 Industry-Academic Cooperation Foundation, Yonsei University Pyrimidine derivative, method for preparing same, and pharmaceutical composition for preventing or treating cancer comprising same as active ingredient
JP7734995B2 (ja) 2021-08-06 2025-09-08 上海和誉生物医薬科技有限公司 ピリミジンまたはピリジン誘導体およびその製造方法ならびに薬学上の応用
IL310870A (en) 2021-08-24 2024-04-01 Arthrosi Therapeutics Inc Quinazoline compounds for treatment of disease
TW202320768A (zh) 2021-10-01 2023-06-01 美商努法倫特公司 雜芳族大環醚化合物之固體形式、醫藥組成物及製備
CA3231608A1 (en) 2021-10-01 2023-04-06 Amit M. Deshpande Methods of treating solid tumor using heteroaromatic macrocyclic ether compounds
IL312004A (en) 2021-10-20 2024-06-01 Hoffmann La Roche Crystalline forms of quinazoline derivatives, their preparation, assembly and use
WO2023081637A1 (en) 2021-11-02 2023-05-11 Enliven Therapeutics, Inc. Fused tetracyclic quinazoline derivatives as inhibitors of erbb2
US20230227470A1 (en) 2021-12-01 2023-07-20 Boehringer Ingelheim International Gmbh Annulated 2-amino-3-cyano thiophenes and derivatives for the treatment of cancer
WO2023099608A1 (en) 2021-12-01 2023-06-08 Boehringer Ingelheim International Gmbh Annulated 2-amino-3-cyano thiophenes and derivatives for the treatment of cancer
WO2023099624A1 (en) 2021-12-01 2023-06-08 Boehringer Ingelheim International Gmbh Annulated 2-amino-3-cyano thiophenes and derivatives for the treatment of cancer
CN118574835A (zh) 2021-12-01 2024-08-30 勃林格殷格翰国际有限公司 用于治疗癌症的环状2-氨基-3-氰基噻吩及衍生物
WO2023154124A1 (en) 2022-02-09 2023-08-17 Enliven Therapeutics, Inc. Acylated heterocyclic quinazoline derivatives as inhibitors of erbb2
WO2023173083A1 (en) 2022-03-11 2023-09-14 Scorpion Therapeutics, Inc. Tetrahydroindole derivatives as egfr and/or her2 inhibtors useful for the treatment of cancer
CN118715216A (zh) 2022-03-28 2024-09-27 江苏恒瑞医药股份有限公司 含氮杂环类化合物、其制备方法及其在医药上的应用
CA3267358A1 (en) 2022-04-05 2025-03-22 Voronoi Inc. Heteroaryl derivatives for the treatment of her2-related diseases

Also Published As

Publication number Publication date
JP2024516371A (ja) 2024-04-15
WO2022221227A1 (en) 2022-10-20
IL306100A (en) 2023-11-01
PE20240327A1 (es) 2024-02-22
US20220363696A1 (en) 2022-11-17
AU2022257621A1 (en) 2023-11-23
JP2025134754A (ja) 2025-09-17
EP4323356A1 (en) 2024-02-21
WO2022221227A9 (en) 2023-11-30
KR20250151577A (ko) 2025-10-21
CA3213079A1 (en) 2022-10-20
CL2023003020A1 (es) 2024-03-22
KR102868758B1 (ko) 2025-10-14
KR20230170039A (ko) 2023-12-18
US12037346B2 (en) 2024-07-16
JP7696443B2 (ja) 2025-06-20
BR112023021111A2 (pt) 2023-12-19
US20240327435A1 (en) 2024-10-03
MX2023012060A (es) 2024-01-22

Similar Documents

Publication Publication Date Title
US12037346B2 (en) Amino-substituted heteroaryls for treating cancers with EGFR mutations
AU2020333251B2 (en) Pyrazolo[3,4-b]pyrazine SHP2 phosphatase inhibitors
EP4076450B1 (en) Isoindolinone and indazole compounds for the degradation of egfr
EP4306529B1 (en) Fgfr inhibitors and methods of use thereof
JP2024523839A (ja) 突然変異体brafを分解する療法薬
KR102148681B1 (ko) Pi3 키나제 모듈레이터로서의 헤테로방향족 화합물
ES2788348T3 (es) Derivados heterocíclicos tricíclicos
US20240158418A1 (en) EGFR Degraders to Treat Cancer Metastasis to the Brain or CNS
EP4676602A1 (en) Compounds targeting mutations in p53 and uses thereof
CN118459485A (zh) 用于治疗具有egfr突变的癌症的氨基取代杂环
TW202304925A (zh) (呋喃并嘧啶—4—基)哌𠯤化合物及其用途
HK40080107B (en) Isoindolinone and indazole compounds for the degradation of egfr
HK40080107A (en) Isoindolinone and indazole compounds for the degradation of egfr
HK40070481A (en) Fgfr inhibitors and methods of use thereof
HK40070481B (en) Fgfr inhibitors and methods of use thereof