CN108137539B - 取代的苯并咪唑、它们的制备和它们作为药物的用途 - Google Patents

取代的苯并咪唑、它们的制备和它们作为药物的用途 Download PDF

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CN108137539B
CN108137539B CN201680059249.7A CN201680059249A CN108137539B CN 108137539 B CN108137539 B CN 108137539B CN 201680059249 A CN201680059249 A CN 201680059249A CN 108137539 B CN108137539 B CN 108137539B
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cancer
compound
mmol
propyl
alkyl
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CN108137539A (zh
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M.普拉施拉夫
G.贾克奎莫特
S.克拉里奇
M.贝拉克达里安
S.约翰斯顿
J.S.艾伯特
A.格里芬
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Neomed Institute
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    • C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/10—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a carbon chain containing aromatic rings
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    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/4164—1,3-Diazoles
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    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
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CN201680059249.7A 2015-08-12 2016-08-12 取代的苯并咪唑、它们的制备和它们作为药物的用途 Active CN108137539B (zh)

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US201562204178P 2015-08-12 2015-08-12
US62/204,178 2015-08-12
US201662358101P 2016-07-04 2016-07-04
US62/358,101 2016-07-04
PCT/CA2016/050952 WO2017024412A1 (en) 2015-08-12 2016-08-12 Substituted benzimidazoles, their preparation and their use as pharmaceuticals

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US (4) US10703740B2 (https=)
EP (1) EP3334719B1 (https=)
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CN (2) CN108137539B (https=)
AU (2) AU2016305515A1 (https=)
CA (1) CA2994478C (https=)
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Families Citing this family (11)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN108137539B (zh) * 2015-08-12 2022-01-11 尼奥迈德研究所 取代的苯并咪唑、它们的制备和它们作为药物的用途
GB201617627D0 (en) 2016-10-18 2016-11-30 Cellcentric Ltd Pharmaceutical compounds
GB201617630D0 (en) 2016-10-18 2016-11-30 Cellcentric Ltd Pharmaceutical compounds
JP7165501B2 (ja) * 2017-03-15 2022-11-04 住友ファーマ株式会社 新規ベンズイミダゾール化合物からなる医薬
WO2018207882A1 (ja) * 2017-05-12 2018-11-15 武田薬品工業株式会社 複素環化合物
GB201806320D0 (en) 2018-04-18 2018-05-30 Cellcentric Ltd Process
WO2020093162A1 (en) * 2018-11-07 2020-05-14 Neomed Institute Treatment of bet inhibitor-resistant cancers and other diseases responsive to dual bet and cbp/ep300 inhibition therapy
JP2022053557A (ja) * 2019-02-08 2022-04-06 マルホ株式会社 ピリドン誘導体
CN112174945B (zh) * 2019-07-02 2022-06-07 四川大学 具有抗癌作用的吲唑类化合物及其制备方法和用途
CN115232074A (zh) * 2022-08-22 2022-10-25 湖南复瑞生物医药技术有限责任公司 一种1-烷基取代-2-甲基-5-溴苯并咪唑的合成方法
WO2024249796A2 (en) * 2023-06-02 2024-12-05 Epigenetix, Inc. Extended and delayed release compositions of substituted benzimidazoles

Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CA2098243A1 (en) * 1992-06-13 1993-12-14 Werner Mederski Benzimidazole derivatives
CN107635558A (zh) * 2015-04-15 2018-01-26 赛尔基因昆蒂赛尔研究公司 布罗莫结构域抑制剂

Family Cites Families (55)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US4550166A (en) 1984-05-21 1985-10-29 American Cyanamid Company (Pyridinyl)-1,2,4-triazolo[4,3-a]pyridines
US4785005A (en) 1986-06-25 1988-11-15 Rorer Pharmaceutical Corporation 6-(6-alkylpyridone)-carbostyril compounds and their cardiotonic uses
US5093330A (en) 1987-06-15 1992-03-03 Ciba-Geigy Corporation Staurosporine derivatives substituted at methylamino nitrogen
US6465484B1 (en) 1997-09-26 2002-10-15 Merck & Co., Inc. Angiogenesis inhibitors
WO2000012089A1 (en) 1998-08-31 2000-03-09 Merck & Co., Inc. Novel angiogenesis inhibitors
US6162804A (en) 1997-09-26 2000-12-19 Merck & Co., Inc. Tyrosine kinase inhibitors
MY139563A (en) 2002-09-04 2009-10-30 Bristol Myers Squibb Co Heterocyclic aromatic compounds useful as growth hormone secretagogues
BRPI0417674A (pt) 2003-12-18 2007-03-20 Pfizer Prod Inc método para tratar a inflamação aguda em animais, com inibidores de quinase map p38
EP1737459B1 (en) 2004-03-19 2009-08-05 Warner-Lambert Company LLC Imidazopyridine and imidazopyrimidine derivatives as antibacterial agents
PE20080403A1 (es) 2006-07-14 2008-04-25 Amgen Inc Derivados heterociclicos fusionados y metodos de uso
WO2008078091A1 (en) 2006-12-22 2008-07-03 Astex Therapeutics Limited Bicyclic heterocyclic compounds as fgfr inhibitors
AU2008219166B2 (en) * 2007-02-16 2013-05-16 Amgen Inc. Nitrogen-containing heterocyclyl ketones and their use as c-Met inhibitors
US8119658B2 (en) 2007-10-01 2012-02-21 Bristol-Myers Squibb Company Triazolopyridine 11-beta hydroxysteroid dehydrogenase type I inhibitors
BRPI0817434A2 (pt) 2007-10-17 2015-06-16 Novartis Ag Composto orgânicos
MY153913A (en) 2009-05-12 2015-04-15 Janssen Pharmaceuticals Inc 7-aryl-1,2,4-triazolo[4,3-a]pyridine derivatives and their use as positive allosteric modulators of mglur2 receptors
GB0919423D0 (en) 2009-11-05 2009-12-23 Glaxosmithkline Llc Novel compounds
EP2501232A1 (en) 2009-11-16 2012-09-26 Merck Sharp & Dohme Corp. Imidazole derivatives and methods of use thereof
SI2651939T1 (sl) 2010-12-13 2015-07-31 Array Biopharma, Inc. SUBSTITUIRANE N-(1H-INDAZOL-4-IL)IMIDAZO(1,2-a)PIRIDIN-3-KARBOKSAMIDNE SPOJINE KOT INHIBITORJI RECEPTORSKE TIROZINSKE KINAZE TIPA III
GB201114103D0 (en) 2011-08-17 2011-09-28 Glaxosmithkline Llc Novel compounds
KR20140075693A (ko) 2011-08-29 2014-06-19 인피니티 파마슈티칼스, 인코포레이티드 헤테로사이클릭 화합물 및 그의 용도
ES2571479T3 (es) * 2012-04-20 2016-05-25 Gilead Sciences Inc Derivados del ácido benzotiazol-6-il acético y su uso para tratar una infección por VIH
US9550737B2 (en) 2012-06-11 2017-01-24 Ucb Biopharma Sprl TNF -α modulating benzimidazoles
JP6215315B2 (ja) 2012-06-12 2017-10-18 アッヴィ・インコーポレイテッド ピリジノンおよびピリダジノン誘導体
KR102092988B1 (ko) 2012-09-28 2020-03-25 벤더르빌트 유니버시티 선택성 bmp 저해제로써 융합된 헤테로 고리 화합물들
US20140094456A1 (en) 2012-10-02 2014-04-03 Intermune, Inc. Anti-fibrotic pyridinones
AR092742A1 (es) 2012-10-02 2015-04-29 Intermune Inc Piridinonas antifibroticas
WO2014095774A1 (de) 2012-12-20 2014-06-26 Bayer Pharma Aktiengesellschaft Bet-proteininhibitorische dihydropyridopyrazinone
AU2013365926B9 (en) 2012-12-21 2019-01-17 Zenith Epigenetics Ltd. Novel heterocyclic compounds as bromodomain inhibitors
WO2014128655A1 (en) 2013-02-25 2014-08-28 Aurigene Discovery Technologies Limited Substituted imidazo[4,5-c]quinoline derivatives as bromodomain inhibitors
JP6464139B2 (ja) 2013-03-14 2019-02-06 コンバージーン・リミテッド・ライアビリティ・カンパニーＣｏｎｖｅｒｇｅｎｅ Ｌｌｃ ブロモドメイン含有タンパク質の阻害のための方法および組成物
SG11201506687RA (en) 2013-03-15 2015-09-29 Plexxikon Inc Heterocyclic compounds and uses thereof
CA2904364A1 (en) 2013-03-15 2014-09-25 Epigenetix, Inc. Oxazolo[5,4-c]quinolin-2-one compounds as bromodomain inhibitors
US8975417B2 (en) 2013-05-27 2015-03-10 Novartis Ag Pyrazolopyrrolidine derivatives and their use in the treatment of disease
CA2915838C (en) 2013-06-21 2023-04-18 Zenith Epigenetics Corp. Bicyclic bromodomain inhibitors
EP3010918B1 (en) 2013-06-21 2018-08-15 Zenith Epigenetics Ltd. Novel substituted bicyclic compounds as bromodomain inhibitors
HK1221721A1 (zh) 2013-07-09 2017-06-09 Bayer Pharma Aktiengesellschaft Bet蛋白抑制性的改性的二氢喹喔啉酮类化合物和二氢吡啶并吡嗪酮类化合物
US20150051208A1 (en) * 2013-08-14 2015-02-19 Boehringer Ingelheim International Gmbh Pyridinones
WO2015049629A1 (en) 2013-10-01 2015-04-09 Piramal Enterprises Limited Imidazoquinoline compounds as bromodomain inhibitors
EP3290407B1 (en) 2013-10-18 2020-01-01 Celgene Quanticel Research, Inc Bromodomain inhibitors
WO2015081189A1 (en) * 2013-11-26 2015-06-04 Incyte Corporation Bicyclic heterocycles as bet protein inhibitors
US9399640B2 (en) 2013-11-26 2016-07-26 Incyte Corporation Substituted pyrrolo[2,3-c]pyridines and pyrazolo[3,4-c]pyridines as BET protein inhibitors
JP2016539970A (ja) 2013-12-09 2016-12-22 アッヴィ・インコーポレイテッド ブロモドメイン阻害薬として有用なジヒドロピリジノンおよびジヒドロピリダジノン誘導体
GB201321729D0 (en) 2013-12-09 2014-01-22 Ucb Pharma Sa Therapeutic agents
MY190835A (en) 2014-01-09 2022-05-12 Orion Corp Bicyclic heterrocyclic derivatives as bromodomain inhibitors
MX382781B (es) 2014-04-02 2025-03-13 Intermune Inc Piridinonas anti-fibroticas.
EA034972B1 (ru) 2014-04-23 2020-04-13 Инсайт Корпорейшн 1h-пирроло[2,3-c]пиридин-7(6h)-оны в качестве ингибиторов белков bet
CA2966908A1 (en) 2014-11-13 2016-05-19 Convergene Llc Methods and compositions for inhibition of bromodomain and extraterminal proteins
EP3227281A4 (en) 2014-12-01 2018-05-30 Zenith Epigenetics Ltd. Substituted pyridinones as bromodomain inhibitors
HK1245247A1 (zh) 2014-12-17 2018-08-24 恒翼生物医药科技(上海)有限公司 溴结构域的抑制剂
US20190055235A1 (en) 2014-12-17 2019-02-21 Zenith Epigenetics Ltd. Substituted bicyclic compounds as bromodomain inhibitors
GB201503720D0 (en) 2015-03-05 2015-04-22 Glaxosmithkline Ip No 2 Ltd Chemical compound
GB201504689D0 (en) 2015-03-19 2015-05-06 Glaxosmithkline Ip Dev Ltd Chemical compounds
GB201506660D0 (en) 2015-04-20 2015-06-03 Cellcentric Ltd Pharmaceutical compounds
GB201506658D0 (en) 2015-04-20 2015-06-03 Cellcentric Ltd Pharmaceutical compounds
CN108137539B (zh) * 2015-08-12 2022-01-11 尼奥迈德研究所 取代的苯并咪唑、它们的制备和它们作为药物的用途

Patent Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CA2098243A1 (en) * 1992-06-13 1993-12-14 Werner Mederski Benzimidazole derivatives
CN107635558A (zh) * 2015-04-15 2018-01-26 赛尔基因昆蒂赛尔研究公司 布罗莫结构域抑制剂

Non-Patent Citations (1)

* Cited by examiner, † Cited by third party
Title
3(2H)-Pyridazinone, 5-(aminomethyl)-2-methyl-6-(1-methyl-1H-benzimidazol-5-yl)-;Aurora Fine Chemicals;《STN International》;20150617;2-3 *

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