CN1874768A - 作为mek抑制剂的n3烷基化苯并咪唑衍生物 - Google Patents

作为mek抑制剂的n3烷基化苯并咪唑衍生物 Download PDF

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Publication number
CN1874768A
CN1874768A CNA2004800323322A CN200480032332A CN1874768A CN 1874768 A CN1874768 A CN 1874768A CN A2004800323322 A CNA2004800323322 A CN A2004800323322A CN 200480032332 A CN200480032332 A CN 200480032332A CN 1874768 A CN1874768 A CN 1874768A
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alkyl
aryl
heteroaryl
fluoro
heterocyclic radical
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Chinese (zh)
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伊莱·M.·华莱士
约瑟夫·P.·利希凯托斯
阿莉森·L.·马洛
布赖恩·T.·赫尔利
M·凯文·科克
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Array Biopharma Inc
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Array Biopharma Inc
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    • C07D235/02—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, condensed with other rings condensed with carbocyclic rings or ring systems
    • C07D235/04—Benzimidazoles; Hydrogenated benzimidazoles
    • C07D235/06—Benzimidazoles; Hydrogenated benzimidazoles with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached in position 2
    • A—HUMAN NECESSITIES
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    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
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    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
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    • C07D235/04—Benzimidazoles; Hydrogenated benzimidazoles
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    • C07F9/02—Phosphorus compounds
    • C07F9/547—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom
    • C07F9/645—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom having two nitrogen atoms as the only ring hetero atoms
    • C07F9/6503—Five-membered rings
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    • C07F9/65586—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom containing at least two different or differently substituted hetero rings neither condensed among themselves nor condensed with a common carbocyclic ring or ring system at least one of the hetero rings does not contain nitrogen as ring hetero atom

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  • Inorganic Chemistry (AREA)
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  • Bioinformatics & Cheminformatics (AREA)
  • Pain & Pain Management (AREA)
  • Rheumatology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
CNA2004800323322A 2003-08-29 2004-08-20 作为mek抑制剂的n3烷基化苯并咪唑衍生物 Pending CN1874768A (zh)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US10/652,733 2003-08-29
US10/652,733 US7235537B2 (en) 2002-03-13 2003-08-29 N3 alkylated benzimidazole derivatives as MEK inhibitors

Publications (1)

Publication Number Publication Date
CN1874768A true CN1874768A (zh) 2006-12-06

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CNA2004800323322A Pending CN1874768A (zh) 2003-08-29 2004-08-20 作为mek抑制剂的n3烷基化苯并咪唑衍生物

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Country Link
US (2) US7235537B2 (https=)
EP (1) EP1663210B1 (https=)
JP (1) JP5026076B2 (https=)
KR (1) KR20060121853A (https=)
CN (1) CN1874768A (https=)
AR (1) AR045738A1 (https=)
AU (1) AU2004270166A1 (https=)
BR (1) BRPI0413152A (https=)
CA (1) CA2537098A1 (https=)
ES (1) ES2628959T3 (https=)
IL (1) IL173935A (https=)
IS (1) IS8384A (https=)
MX (1) MXPA06002268A (https=)
NO (1) NO20061432L (https=)
RU (1) RU2006109600A (https=)
TW (1) TW200524879A (https=)
WO (1) WO2005023251A1 (https=)
ZA (1) ZA200602588B (https=)

Cited By (8)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN103764144A (zh) * 2011-08-31 2014-04-30 诺华股份有限公司 Pi3k抑制剂与mek抑制剂的协同组合
CN104507474A (zh) * 2012-07-26 2015-04-08 诺华股份有限公司 CDK4/6抑制剂和B-Raf抑制剂的药物组合
CN105384754A (zh) * 2014-09-02 2016-03-09 上海科州药物研发有限公司 作为蛋白激酶抑制剂的杂环类化合物及其制备方法和用途
WO2016131406A1 (zh) * 2015-02-16 2016-08-25 苏州晶云药物科技有限公司 一种口服丝裂原活化蛋白激酶抑制剂的晶型及其制备方法
CN109336824A (zh) * 2012-10-19 2019-02-15 诺华股份有限公司 Mek抑制剂的制备和包含mek抑制剂的制剂
WO2019096112A1 (zh) * 2017-11-14 2019-05-23 深圳市塔吉瑞生物医药有限公司 一种取代的苯并咪唑化合物及包含该化合物的组合物
CN115490640A (zh) * 2021-06-17 2022-12-20 深圳市塔吉瑞生物医药有限公司 取代的苯并咪唑类化合物及包含该化合物的组合物及其用途
CN116283940A (zh) * 2017-12-07 2023-06-23 哈尔滨珍宝制药有限公司 一种作为fgfr和vegfr抑制剂化合物的盐型、晶型及其制备方法

Families Citing this family (71)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
KR100984595B1 (ko) * 2002-03-13 2010-09-30 어레이 바이오파마 인크. Ｍｅｋ 억제제로서의 ｎ3 알킬화 벤즈이미다졸 유도체
ES2331246T3 (es) * 2003-07-24 2009-12-28 Warner-Lambert Company Llc Derivados de benzamidazol como inhibidores del mek.
US7538120B2 (en) * 2003-09-03 2009-05-26 Array Biopharma Inc. Method of treating inflammatory diseases
US7144907B2 (en) * 2003-09-03 2006-12-05 Array Biopharma Inc. Heterocyclic inhibitors of MEK and methods of use thereof
CN1905873A (zh) 2003-11-19 2007-01-31 阵列生物制药公司 Mek的杂环抑制剂及其使用方法
US7517994B2 (en) * 2003-11-19 2009-04-14 Array Biopharma Inc. Heterocyclic inhibitors of MEK and methods of use thereof
US7732616B2 (en) * 2003-11-19 2010-06-08 Array Biopharma Inc. Dihydropyridine and dihydropyridazine derivatives as inhibitors of MEK and methods of use thereof
NZ590160A (en) * 2003-11-21 2012-07-27 Array Biopharma Inc AKT protein kinase inhibitors
ES2405785T3 (es) * 2005-05-18 2013-06-03 Array Biopharma Inc. Inhibidores heterocíclicos de MEK y métodos de uso de los mismos
SI1934174T1 (sl) 2005-10-07 2011-08-31 Exelixis Inc Inhibitorji MEK in postopki za njihovo uporabo
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
WO2007071951A1 (en) * 2005-12-21 2007-06-28 Astrazeneca Ab Tosylate salt of 6- (4-br0m0-2-chl0r0phenylamin0) -7-fluoro-n- (2-hydroxyethoxy) -3-methyl-3h-benzimi dazole- 5 - carboxamide , mek inhibitor useful in the treatment of cancer
TWI405756B (zh) 2005-12-21 2013-08-21 Array Biopharma Inc 新穎硫酸氫鹽
RU2418790C3 (ru) * 2005-12-21 2022-03-14 Астразенека Аб Новая гидросульфатная соль
GB0601962D0 (en) 2006-01-31 2006-03-15 Ucb Sa Therapeutic agents
CA2656566C (en) 2006-07-06 2014-06-17 Array Biopharma Inc. Dihydrofuro pyrimidines as akt protein kinase inhibitors
US8063050B2 (en) * 2006-07-06 2011-11-22 Array Biopharma Inc. Hydroxylated and methoxylated pyrimidyl cyclopentanes as AKT protein kinase inhibitors
ATE532789T1 (de) 2006-07-06 2011-11-15 Array Biopharma Inc Dihydrothienopyrimidine als akt-proteinkinase- inhibitoren
ATE523499T1 (de) * 2006-07-06 2011-09-15 Array Biopharma Inc Cyclopenta [d]-pyrimidine als akt-proteinkinasehemmer
US8492378B2 (en) 2006-08-03 2013-07-23 Takeda Pharmaceutical Company Limited GSK-3β inhibitor
PE20081354A1 (es) 2006-11-30 2008-11-14 Genentech Inc Compuestos de azaindolilo como inhibidores de mek
PL2101759T3 (pl) * 2006-12-14 2019-05-31 Exelixis Inc Sposoby stosowania inhibitorów MEK
US8846683B2 (en) 2007-07-05 2014-09-30 Array Biopharma, Inc. Pyrimidyl cyclopentanes as Akt protein kinase inhibitors
US9409886B2 (en) 2007-07-05 2016-08-09 Array Biopharma Inc. Pyrimidyl cyclopentanes as AKT protein kinase inhibitors
WO2009006567A2 (en) 2007-07-05 2009-01-08 Array Biopharma Inc. Pyrimidyl cyclopentanes as akt protein kinase inhibitors
CN101918373B (zh) * 2007-07-05 2013-06-05 阵列生物制药公司 作为akt蛋白激酶抑制剂的嘧啶基环戊烷
GB0714384D0 (en) 2007-07-23 2007-09-05 Ucb Pharma Sa theraputic agents
ATE551336T1 (de) * 2007-08-16 2012-04-15 Hoffmann La Roche Substituierte hydantoine
ES2456966T3 (es) 2007-11-12 2014-04-24 Takeda Pharmaceutical Company Limited Inhibidores de MAPK/ERK cinasa
CN101896227A (zh) * 2007-12-12 2010-11-24 阿斯利康(瑞典)有限公司 包含mek抑制剂和极光激酶抑制剂的组合
JP2011506533A (ja) 2007-12-20 2011-03-03 エフ．ホフマン−ラ ロシュ アーゲー Ｍｅｋキナーゼ阻害剤としての置換ヒダントイン
EP2240455B1 (en) * 2008-01-09 2012-12-26 Array Biopharma, Inc. Hydroxylated pyrimidyl cyclopentane as akt protein kinase inhibitor
ES2422733T3 (es) * 2008-01-09 2013-09-13 Array Biopharma Inc Pirimidilciclopentanos hidroxilados como inhibidores de proteínas cinasas AKT
EP2240494B1 (en) 2008-01-21 2016-03-30 UCB Biopharma SPRL Thieno-pyridine derivatives as mek inhibitors
GB0811304D0 (en) 2008-06-19 2008-07-30 Ucb Pharma Sa Therapeutic agents
US20110105521A1 (en) * 2008-07-11 2011-05-05 Novartis Ag Combination of (a) a phosphoinositide 3-kinase inhibitor and (b) a modulator of ras/raf/mek pathway
US8993630B2 (en) 2008-11-10 2015-03-31 Bayer Intellectual Property Gmbh Substituted sulphonamido phenoxybenzamides
CA2776944A1 (en) * 2009-10-12 2011-05-12 F. Hoffmann-La Roche Ag Combinations of a pi3k inhibitor and a mek inhibitor
EP2491014A1 (en) 2009-10-21 2012-08-29 Bayer Pharma Aktiengesellschaft Substituted halophenoxybenzamide derivatives
US20120269803A1 (en) 2009-10-21 2012-10-25 Bayer Intellectual Property Gmbh Substituted benzosulphonamides
EP2491015A1 (en) 2009-10-21 2012-08-29 Bayer Pharma Aktiengesellschaft Substituted benzosulphonamides
CA2807510A1 (en) 2010-08-05 2012-02-09 Case Western Reserve University Inhibitors of erk for developmental disorders of neuronal connectivity
MY170236A (en) 2010-10-06 2019-07-11 Glaxosmithkline Llc Benzimidazole derivatives as pi3 kinase inhibitors
WO2012055953A1 (en) 2010-10-29 2012-05-03 Bayer Pharma Aktiengesellschaft Substituted phenoxypyridines
CN102020651B (zh) 2010-11-02 2012-07-18 北京赛林泰医药技术有限公司 6-芳基氨基吡啶酮甲酰胺mek抑制剂
DK2655375T3 (en) 2010-12-23 2015-03-09 Sanofi Sa PYRIMIDINON DERIVATIVES, PREPARATION AND PHARMACEUTICAL USE THEREOF
WO2012135781A1 (en) 2011-04-01 2012-10-04 Genentech, Inc. Combinations of akt inhibitor compounds and chemotherapeutic agents, and methods of use
RU2013148817A (ru) 2011-04-01 2015-05-10 Дженентек, Инк. Комбинации соединений-ингибиторов акт и мек и способы их применения
EP2714037B1 (en) 2011-05-25 2016-07-13 Université Paris Descartes Erk inhibitors for use in treating spinal muscular atrophy
CN103204825B (zh) 2012-01-17 2015-03-04 上海科州药物研发有限公司 作为蛋白激酶抑制剂的苯并噻唑化合物及其制备方法和用途
NZ629432A (en) 2012-03-14 2017-01-27 Lupin Ltd Heterocyclyl compounds as mek inhibitors
KR102204520B1 (ko) 2012-10-12 2021-01-20 엑셀리시스, 인코포레이티드 암의 치료에 사용하기 위한 화합물의 신규 제조 방법
US9867825B2 (en) * 2012-12-20 2018-01-16 Novartis Ag Pharmaceutical combination comprising binimetinib
MA38522A1 (fr) * 2013-03-21 2017-10-31 Novartis Ag Thérapie de combinaison comprenant un inhibiteur de b-raf et un second inhibiteur.
EP3043822A1 (en) 2013-09-11 2016-07-20 The J. David Gladstone Institutes, A Testamentary Trust Established under The Will of J. David Gladstone Compositions for preparing cardiomyocytes
WO2016009306A1 (en) 2014-07-15 2016-01-21 Lupin Limited Heterocyclyl compounds as mek inhibitors
WO2016035008A1 (en) 2014-09-04 2016-03-10 Lupin Limited Pyridopyrimidine derivatives as mek inhibitors
WO2017033113A1 (en) 2015-08-21 2017-03-02 Acerta Pharma B.V. Therapeutic combinations of a mek inhibitor and a btk inhibitor
FI3463345T3 (fi) * 2016-06-03 2023-01-31 Farmaseuttisia yhdistelmiä
EP4523755A3 (en) 2018-09-18 2025-06-11 F. Hoffmann-La Roche AG Quinazoline derivatives as antitumor agents
US20220040324A1 (en) 2018-12-21 2022-02-10 Daiichi Sankyo Company, Limited Combination of antibody-drug conjugate and kinase inhibitor
US11447482B1 (en) 2019-02-14 2022-09-20 KUDA Therapeutics, Inc. Imidazopyridine and oxazolopyridine derivatives and analogs thereof, methods of preparation thereof, methods of HIF-2A pathway inhibition, and induction of ferroptosis
EA202192575A1 (ru) 2019-03-21 2022-01-14 Онксео Соединения dbait в сочетании с ингибиторами киназ для лечения рака
CN114761006A (zh) 2019-11-08 2022-07-15 Inserm(法国国家健康医学研究院) 对激酶抑制剂产生耐药性的癌症的治疗方法
WO2021148581A1 (en) 2020-01-22 2021-07-29 Onxeo Novel dbait molecule and its use
CN115322105A (zh) * 2021-05-11 2022-11-11 江苏润安制药有限公司 一种合成艾拉莫德关键中间体的方法
US12280055B2 (en) 2021-05-27 2025-04-22 Mirati Therapeutics, Inc. Combination therapies
CA3226162A1 (en) 2021-07-09 2023-01-12 Plexium, Inc. Aryl compounds and pharmaceutical compositions that modulate ikzf2
IL312004A (en) 2021-10-20 2024-06-01 Hoffmann La Roche Crystalline forms of quinazoline derivatives, their preparation, assembly and use
CN116135839A (zh) * 2021-11-18 2023-05-19 江苏润安制药有限公司 一种阿齐沙坦关键中间体的制备方法
WO2025073765A1 (en) 2023-10-03 2025-04-10 Institut National de la Santé et de la Recherche Médicale Methods of prognosis and treatment of patients suffering from melanoma

Family Cites Families (31)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5750545A (en) 1993-07-23 1998-05-12 The Green Cross Corporation Triazole derivative and pharmaceutical use thereof
US5525625A (en) 1995-01-24 1996-06-11 Warner-Lambert Company 2-(2-Amino-3-methoxyphenyl)-4-oxo-4H-[1]benzopyran for treating proliferative disorders
UA73073C2 (uk) 1997-04-03 2005-06-15 Уайт Холдінгз Корпорейшн Заміщені 3-ціанохіноліни, спосіб їх одержання та фармацевтична композиція
BR9810385A (pt) 1997-07-01 2000-09-05 Warner Lambert Co Derivados de ácido benzóico 2-(4-bromo ou 4-iodo fenilamino) e sua utilização como inibidores de mek
US6506798B1 (en) 1997-07-01 2003-01-14 Warner-Lambert Company 4-Arylamino, 4-aryloxy, and 4-arylthio diarylamines and derivatives thereof as selective MEK inhibitors
NZ501276A (en) 1997-07-01 2000-10-27 Warner Lambert Co 4-bromo or 4-iodo phenylamino benzhydroxamic acid derivatives and their use as MEK inhibitors in treating proliferative disorders
US6821963B2 (en) 1997-07-01 2004-11-23 Warner-Lambert Company 4-Bromo or 4-iodo phenylamino benzhydroxamic acid derivatives and their use as MEK inhibitors
US6310060B1 (en) 1998-06-24 2001-10-30 Warner-Lambert Company 2-(4-bromo or 4-iodo phenylamino) benzoic acid derivatives and their use as MEK inhibitors
EP1140062B1 (en) 1999-01-07 2005-04-06 Warner-Lambert Company LLC Treatment of asthma with mek inhibitors
WO2000040237A1 (en) 1999-01-07 2000-07-13 Warner-Lambert Company Antiviral method using mek inhibitors
IL144214A0 (en) 1999-01-13 2002-05-23 Warner Lambert Co Benzoheterocycles and their use as mek inhibitors
CA2349180A1 (en) 1999-01-13 2000-07-20 Stephen Douglas Barrett Anthranilic acid derivatives
CA2348236A1 (en) 1999-01-13 2000-07-20 Stephen Douglas Barrett 4-arylamino, 4-aryloxy, and 4-arylthio diarylamines and derivatives thereof as selective mek inhibitors
CA2349832A1 (en) 1999-01-13 2000-07-20 Warner-Lambert Company Benzenesulfonamide derivatives and their use as mek inhibitors
ATE311363T1 (de) 1999-01-13 2005-12-15 Warner Lambert Co Sulfohydroxamsäure and sulfohydroxamate und ihre verwendung als mek-inhibitoren
DE69926914T2 (de) 1999-01-13 2006-06-29 Warner-Lambert Co. Llc 1-heterozyklus-substituierte diarylaminen
GB9910577D0 (en) 1999-05-08 1999-07-07 Zeneca Ltd Chemical compounds
US7030119B1 (en) 1999-07-16 2006-04-18 Warner-Lambert Company Method for treating chronic pain using MEK inhibitors
HUP0202381A3 (en) 1999-07-16 2004-12-28 Warner Lambert Co Method for treating chronic pain using mek inhibitors
KR20020012315A (ko) 1999-07-16 2002-02-15 로즈 암스트롱, 크리스틴 에이. 트러트웨인 Ｍｅｋ 저해제를 사용한 만성 통증의 치료 방법
ES2208364T3 (es) 1999-07-16 2004-06-16 Warner-Lambert Company Llc Procedimiento para tratar dolor cronico usando inhibidores de mek.
PL352835A1 (en) 1999-07-16 2003-09-08 Warner-Lambert Company Method for treating chronic pain using mek inhibitors
MXPA02008103A (es) 2000-03-15 2002-11-29 Warner Lambert Co Diarilaminas sustituidas con 5-amida como inhibidores mek.
EP1339702A1 (en) 2000-03-15 2003-09-03 Warner-Lambert Company 5-amide substituted diarylamines as mek inhibitors
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
SK2072003A3 (en) 2000-08-25 2004-01-08 Warner Lambert Co Process for making N-aryl-anthranilic acids and their derivatives
US7067532B2 (en) 2000-11-02 2006-06-27 Astrazeneca Substituted quinolines as antitumor agents
US20040039208A1 (en) 2001-07-20 2004-02-26 Chen Michael Huai Gu Process for making n-aryl-anthranilic acids and their derivatives
EP1482944A4 (en) * 2002-03-13 2006-04-19 Array Biopharma Inc NZ ALKYL BENZIMIDAZOLE DERIVATIVES AS MEK INHIBITORS
KR100984595B1 (ko) * 2002-03-13 2010-09-30 어레이 바이오파마 인크. Ｍｅｋ 억제제로서의 ｎ3 알킬화 벤즈이미다졸 유도체
ES2331246T3 (es) * 2003-07-24 2009-12-28 Warner-Lambert Company Llc Derivados de benzamidazol como inhibidores del mek.

Cited By (15)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN103764144B (zh) * 2011-08-31 2016-07-20 诺华股份有限公司 Pi3k抑制剂与mek抑制剂的协同组合
CN103764144A (zh) * 2011-08-31 2014-04-30 诺华股份有限公司 Pi3k抑制剂与mek抑制剂的协同组合
CN104507474B (zh) * 2012-07-26 2018-01-02 诺华股份有限公司 CDK4/6抑制剂和B‑Raf抑制剂的药物组合
US9700557B2 (en) 2012-07-26 2017-07-11 Novartis Ag Pharmaceutical combinations of a CDK4/6 inhibitor and a B-RAF inhibitor
CN104507474A (zh) * 2012-07-26 2015-04-08 诺华股份有限公司 CDK4/6抑制剂和B-Raf抑制剂的药物组合
CN109336824A (zh) * 2012-10-19 2019-02-15 诺华股份有限公司 Mek抑制剂的制备和包含mek抑制剂的制剂
CN105384754A (zh) * 2014-09-02 2016-03-09 上海科州药物研发有限公司 作为蛋白激酶抑制剂的杂环类化合物及其制备方法和用途
CN105384754B (zh) * 2014-09-02 2018-04-20 上海科州药物研发有限公司 作为蛋白激酶抑制剂的杂环类化合物及其制备方法和用途
WO2016131406A1 (zh) * 2015-02-16 2016-08-25 苏州晶云药物科技有限公司 一种口服丝裂原活化蛋白激酶抑制剂的晶型及其制备方法
WO2019096112A1 (zh) * 2017-11-14 2019-05-23 深圳市塔吉瑞生物医药有限公司 一种取代的苯并咪唑化合物及包含该化合物的组合物
US12116348B2 (en) 2017-11-14 2024-10-15 Shenzhen Targetrx, Inc. Substituted benzimidazole compound and composition comprising same
CN116283940A (zh) * 2017-12-07 2023-06-23 哈尔滨珍宝制药有限公司 一种作为fgfr和vegfr抑制剂化合物的盐型、晶型及其制备方法
CN115490640A (zh) * 2021-06-17 2022-12-20 深圳市塔吉瑞生物医药有限公司 取代的苯并咪唑类化合物及包含该化合物的组合物及其用途
WO2022262699A1 (zh) * 2021-06-17 2022-12-22 深圳市塔吉瑞生物医药有限公司 取代的苯并咪唑类化合物及包含该化合物的组合物及其用途
CN115490640B (zh) * 2021-06-17 2024-11-26 深圳市塔吉瑞生物医药有限公司 取代的苯并咪唑类化合物及包含该化合物的组合物及其用途

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