CN109195965B - Wdr5蛋白质-蛋白质结合的抑制剂 - Google Patents

Wdr5蛋白质-蛋白质结合的抑制剂 Download PDF

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CN109195965B
CN109195965B CN201780024229.0A CN201780024229A CN109195965B CN 109195965 B CN109195965 B CN 109195965B CN 201780024229 A CN201780024229 A CN 201780024229A CN 109195965 B CN109195965 B CN 109195965B
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fluoro
phenyl
pyridine
carboxamide
oxo
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CN109195965A (zh
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R·阿瓦尔
C·A·泽佩达-维拉兹奎兹
G·波达
M·艾萨克
D·尤林
B·威尔逊
B·约瑟夫
Y·刘
P·苏布拉马尼安
A·马迈
M·普拉克施
J·K·斯蒂尔
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Propelon Therapeutics
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CN201780024229.0A 2016-03-01 2017-03-01 Wdr5蛋白质-蛋白质结合的抑制剂 Active CN109195965B (zh)

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US201662301673P 2016-03-01 2016-03-01
US62/301,673 2016-03-01
PCT/CA2017/050269 WO2017147700A1 (en) 2016-03-01 2017-03-01 Inhibitors of wdr5 protein-protein binding

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CN109195965B true CN109195965B (zh) 2022-07-26

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JP (3) JP7624690B2 (enExample)
KR (1) KR20180120720A (enExample)
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AU (1) AU2017226004B2 (enExample)
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Families Citing this family (27)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DK3423451T3 (da) 2016-03-01 2022-11-28 Propellon Therapeutics Inc Inhibitorer af wdr5-protein-proteinbinding
WO2017147701A1 (en) 2016-03-01 2017-09-08 Ontario Institute For Cancer Research (Oicr) Inhibitors of wdr5 protein-protein binding
JP2019537585A (ja) 2016-10-28 2019-12-26 アイカーン スクール オブ メディスン アット マウント シナイ Ezh2媒介性がんを治療するための組成物および方法
CA3045037A1 (en) 2016-12-08 2018-06-14 Icahn School Of Medicine At Mount Sinai Compositions and methods for treating cdk4/6-mediated cancer
WO2018176134A1 (en) 2017-03-27 2018-10-04 HYDRO-QUéBEC Salts for use in electrolyte compositions or as electrode additives
WO2019046944A1 (en) * 2017-09-06 2019-03-14 Propellon Therapeutics Inc. INHIBITORS OF PROTEIN BINDING WDR5-PROTEIN
US10501466B2 (en) 2017-09-19 2019-12-10 Vanderbilt University WDR5 inhibitors and modulators
EP3736266A4 (en) * 2018-01-04 2021-01-06 Peking University Shenzhen Graduate School COMPOUND SIMULTANEOUSLY INHIBITING THE LSD1 AND HDAC TARGETS AND ITS APPLICATION
US11472799B2 (en) 2018-03-06 2022-10-18 Icahn School Of Medicine At Mount Sinai Serine threonine kinase (AKT) degradation / disruption compounds and methods of use
CN108715585A (zh) * 2018-04-23 2018-10-30 中国药科大学 苯基联三氮唑类mll1-wdr5蛋白-蛋白相互作用抑制剂
US10844044B2 (en) 2018-06-14 2020-11-24 Vanderbilt University WDR5 inhibitors and modulators
JP2021527666A (ja) * 2018-06-21 2021-10-14 アイカーン スクール オブ メディスン アット マウント シナイ Wd40反復ドメインタンパク質5(wdr5)分解/破壊化合物および使用の方法
US10807959B2 (en) 2018-08-16 2020-10-20 Vanderbilt University WDR5-MLL1 inhibitors and modulators
CN109734674B (zh) 2019-02-26 2022-08-26 中国药科大学 苯胺类wdr5蛋白-蛋白相互作用抑制剂及其制法和用途
CN113543852A (zh) 2019-03-06 2021-10-22 第一三共株式会社 吡咯并吡唑衍生物
CN114423463B (zh) 2019-05-06 2025-09-26 西奈山伊坎医学院 作为hpk1的降解剂的异双功能化合物
CN111039860B (zh) * 2019-12-02 2022-09-13 河北科技大学 2-羟基-n-(4’-氯联苯-2-基)烟酰胺的合成方法及应用
CN113024538B (zh) * 2019-12-24 2022-09-09 南开大学 吡唑酰胺类化合物及其制备和在防治植物病菌病和杀虫中的应用
US12103924B2 (en) 2020-06-01 2024-10-01 Icahn School Of Medicine At Mount Sinai Mitogen-activated protein kinase kinase (MEK) degradation compounds and methods of use
CN114539073A (zh) * 2022-02-18 2022-05-27 郑州萃智医药科技有限公司 3-溴-2-氯-4,6-二氟苯胺的合成方法
JP2025509830A (ja) * 2022-03-14 2025-04-11 フヤバイオ インターナショナル,エルエルシー 血液脳関門を通過するmll1-wdr5タンパク質間相互作用阻害剤化合物及びそれらの使用
AR129265A1 (es) 2022-05-12 2024-08-07 Syngenta Crop Protection Ag Compuestos de alcoxi-heteroaril-carboxamida o tioamida
CN119365449A (zh) * 2022-07-01 2025-01-24 甘李药业股份有限公司 一种用作wdr5抑制剂的化合物或其可药用盐及其应用
EP4554579A2 (en) * 2022-07-14 2025-05-21 Huyabio International, LLC Combination therapies of wdr5 inhibitors and pd-1 inhibitors
CN115974965B (zh) * 2022-08-31 2025-09-12 中国科学技术大学 一种靶向wdr5的多肽抑制剂及其用途
CN119143715B (zh) * 2024-11-12 2025-03-14 天津匠新致成科技有限公司 二芳基团甲基哌嗪类化合物及其制备方法、药物组合物和应用
CN119661474A (zh) * 2024-12-16 2025-03-21 中国药科大学 一类羟肟酸类的双靶点化合物衍生物及其应用

Citations (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN100355751C (zh) * 2000-03-29 2007-12-19 西克拉塞尔有限公司 2-取代的4-杂芳基-嘧啶、其组合物及其用途
CN101679266A (zh) * 2007-03-01 2010-03-24 诺瓦提斯公司 Pim激酶抑制剂及其应用方法
WO2011149874A2 (en) * 2010-05-26 2011-12-01 Schering Corporation N-phenyl imidazole carboxamide inhibitors of 3-phosphoinositide-dependent protein kinase-1
WO2014003124A1 (ja) * 2012-06-28 2014-01-03 富士フイルム株式会社 新規なアミド誘導体またはその塩
CN105175284A (zh) * 2015-07-21 2015-12-23 中国药科大学 酰胺类化合物、制备方法及其医药用途

Family Cites Families (42)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP1247804A1 (en) 1993-11-12 2002-10-09 PHARMACIA &amp; UPJOHN COMPANY Pyrimidine-thioalkyl and alkylether compounds
JPH0959236A (ja) 1995-08-23 1997-03-04 Dai Ichi Seiyaku Co Ltd ベンズアミド化合物
US20010051719A1 (en) 1996-12-19 2001-12-13 Smithkline Beecham P.L.C. Novel compounds
US6362371B1 (en) 1998-06-08 2002-03-26 Advanced Medicine, Inc. β2- adrenergic receptor agonists
DE19952146A1 (de) 1999-10-29 2001-06-07 Boehringer Ingelheim Pharma Arylalkane, Arylalkene und Aryl-azaalkane, diese Verbindungen enthaltende Arzneimittel und Verfahren zu ihrer Herstellung
JP2002193938A (ja) 2000-12-01 2002-07-10 Bayer Ag 4−アリールピリジン誘導体
WO2002088101A2 (en) 2001-04-27 2002-11-07 Vertex Pharmaceuticals Incorporated Inhibitors of bace
GB0215676D0 (en) 2002-07-05 2002-08-14 Novartis Ag Organic compounds
CA2492593A1 (en) 2002-07-15 2004-01-22 Myriad Genetics, Inc. Compounds, compositions, and methods employing same
WO2004022562A1 (en) 2002-09-09 2004-03-18 Cellular Genomics, Inc. 6-ARYL-IMIDAZO[1,2-a]PYRAZIN-8-YLAMINES, METHOD OF MAKING, AND METHOD OF USE THEREOF
GB0412072D0 (en) 2004-05-28 2004-06-30 Syngenta Participations Ag Chemical compounds
CN1960988B (zh) 2004-06-10 2012-01-25 Irm责任有限公司 作为蛋白激酶抑制剂的化合物和组合物
CN101106990B (zh) 2005-01-26 2010-12-08 Irm责任有限公司 用作蛋白激酶抑制剂的化合物和组合物
WO2006124731A2 (en) 2005-05-12 2006-11-23 Irm Llc Compounds and compositions as protein kinase inhibitors
DE102005022977A1 (de) 2005-05-19 2006-12-07 Merck Patent Gmbh Phenylchinazolinderivate
US20070254894A1 (en) 2006-01-10 2007-11-01 Kane John L Jr Novel small molecules with selective cytotoxicity against human microvascular endothelial cell proliferation
BRPI0707666A2 (pt) 2006-02-06 2011-05-10 Irm Llc compostos e composiÇÕes como inibidores de proteÍna cinase
CN102861338A (zh) 2006-04-05 2013-01-09 诺瓦提斯公司 用于治疗癌症、包含bcr-abl/c-kit/pdgf-r tk抑制剂的组合
CN101707863A (zh) 2007-06-15 2010-05-12 Irm责任有限公司 蛋白激酶抑制剂及其使用方法
CN101875617B (zh) 2009-03-23 2015-05-20 中国医学科学院药物研究所 烷氧基取代芳环的氨甲酰基类芳酸化合物及其制法和用途
AU2010244218B2 (en) 2009-05-07 2012-07-19 Astrazeneca Ab Substituted 1-cyanoethylheterocyclylcarboxamide compounds 750
EP2558085B1 (en) 2010-04-16 2017-08-30 Athenex, Inc. Compositions and methods for the prevention and treatment of cancer
WO2011156557A2 (en) 2010-06-11 2011-12-15 Thomas James B Compounds active at the neurotensin receptor
US9233086B2 (en) * 2010-06-16 2016-01-12 The Regents Of The University Of Michigan Inhibition of WDR5 interaction with its binding partners
WO2012066065A1 (en) 2010-11-17 2012-05-24 Novartis Ag Phenyl-heteroaryl amine compounds and their uses
WO2014048878A1 (en) 2012-09-26 2014-04-03 Evotec (Uk) Ltd. Phenyl- or pyridyl- pyrrolo[2,3b]pyrazine derivatives useful in the treatment or prevention of proliferative disorders or dysplasia
WO2014058071A1 (ja) 2012-10-12 2014-04-17 武田薬品工業株式会社 シクロプロパンアミン化合物およびその用途
US9079866B2 (en) 2013-02-04 2015-07-14 Janssen Pharmaceutica Nv Flap modulators
JP6879740B2 (ja) 2013-12-13 2021-06-02 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 リンパ形質細胞性リンパ腫を処置する方法
US9908872B2 (en) 2013-12-13 2018-03-06 Dana-Farber Cancer Institute, Inc. Methods to treat lymphoplasmacytic lymphoma
CN104926801B (zh) * 2014-03-22 2019-06-04 浙江大学 取代氮杂环类衍生物、含其的药物组合物及其在抗肿瘤中的应用
CN105585565B (zh) 2014-10-23 2019-10-01 中国医学科学院药物研究所 含2-苯胺基-4-噻唑基吡啶衍生物及其制法和药物组合物与用途
CN105837575B (zh) 2015-01-13 2019-01-15 四川大学 3-乙炔基吡唑并嘧啶衍生物及其制备方法和用途
DK3423451T3 (da) * 2016-03-01 2022-11-28 Propellon Therapeutics Inc Inhibitorer af wdr5-protein-proteinbinding
IL302705A (en) 2016-03-01 2023-07-01 Immatics Biotechnologies Gmbh Peptides, combinations of peptides, cell-based drugs for use in immunotherapy against bladder cancer and other types of cancer
WO2017147701A1 (en) 2016-03-01 2017-09-08 Ontario Institute For Cancer Research (Oicr) Inhibitors of wdr5 protein-protein binding
WO2017221092A1 (en) 2016-06-20 2017-12-28 Novartis Ag Triazolopyridine compounds and uses thereof
US10160763B2 (en) 2016-09-13 2018-12-25 Vanderbilt University WDR5 inhibitors and modulators
WO2019046944A1 (en) 2017-09-06 2019-03-14 Propellon Therapeutics Inc. INHIBITORS OF PROTEIN BINDING WDR5-PROTEIN
US10501466B2 (en) 2017-09-19 2019-12-10 Vanderbilt University WDR5 inhibitors and modulators
US11999716B2 (en) 2018-10-24 2024-06-04 Vanderbilt University WDR5 inhibitors and modulators
WO2021026672A1 (en) 2019-08-09 2021-02-18 Novartis Ag Heterocyclic wdr5 inhibitors as anti-cancer compounds

Patent Citations (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN100355751C (zh) * 2000-03-29 2007-12-19 西克拉塞尔有限公司 2-取代的4-杂芳基-嘧啶、其组合物及其用途
CN101679266A (zh) * 2007-03-01 2010-03-24 诺瓦提斯公司 Pim激酶抑制剂及其应用方法
WO2011149874A2 (en) * 2010-05-26 2011-12-01 Schering Corporation N-phenyl imidazole carboxamide inhibitors of 3-phosphoinositide-dependent protein kinase-1
WO2014003124A1 (ja) * 2012-06-28 2014-01-03 富士フイルム株式会社 新規なアミド誘導体またはその塩
CN105175284A (zh) * 2015-07-21 2015-12-23 中国药科大学 酰胺类化合物、制备方法及其医药用途

Non-Patent Citations (1)

* Cited by examiner, † Cited by third party
Title
Pharmacological targeting of the Wdr5-MLL interaction in C/EBPa N-terminal leukemia;Florian Grebien et al.;《Nature chemical biology》;20150713;第11卷;第571-578页 *

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