JP2017505787A - 治療薬としてのヒトアンドロゲン受容体dna結合ドメイン(dbd)化合物およびそれらを使用する方法 - Google Patents

治療薬としてのヒトアンドロゲン受容体dna結合ドメイン(dbd)化合物およびそれらを使用する方法 Download PDF

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JP2017505787A
JP2017505787A JP2016551163A JP2016551163A JP2017505787A JP 2017505787 A JP2017505787 A JP 2017505787A JP 2016551163 A JP2016551163 A JP 2016551163A JP 2016551163 A JP2016551163 A JP 2016551163A JP 2017505787 A JP2017505787 A JP 2017505787A
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nhch
optionally
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cancer
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JP2017505787A5 (enExample
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トチェルカソフ、アルテム
レニー、ポール・エス.
バン、フチャン
リ、フイファン
ルブラン、エリック・ジョゼフ・ジャン
ダラル、クシュ
トベルドクーレボフ、アントン・ブイ.
バビー、セルジー
ボゴモル、エフゲニーア
ドゥナイェンコ、カテリーナ
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University of British Columbia
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Publication number Priority date Publication date Assignee Title
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Families Citing this family (30)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2016003917A1 (en) * 2014-07-03 2016-01-07 Quanticel Pharmaceuticals, Inc. Inhibitors of lysine specific demethylase-1
EP3555091A1 (en) * 2016-12-19 2019-10-23 H. Hoffnabb-La Roche Ag Ar-v7 inhibitors
WO2019023651A2 (en) 2017-07-28 2019-01-31 Massachusetts Institute Of Technology MODULATORS OF THE SMALL MOLECULE ANDROGEN RECEPTOR
WO2019126739A1 (en) 2017-12-21 2019-06-27 Shepherd Therapeutics, Inc. Pyrvinium pamoate anti-cancer therapies
CN108084171A (zh) * 2017-12-22 2018-05-29 佛山汉方中医医院有限公司 哌嗪噻吩二环腈类化合物、制备方法及其用途
CN108069950A (zh) * 2017-12-22 2018-05-25 佛山汉方中医医院有限公司 一种含噻吩的二环腈类ssao抑制剂、制备方法及其用途
CN108069948A (zh) * 2017-12-22 2018-05-25 佛山汉方中医医院有限公司 一种ssao抑制剂、其制备方法及其用途
CN108003147A (zh) * 2017-12-22 2018-05-08 佛山汉方中医医院有限公司 异丙基哌嗪氟噻吩二环腈类化合物、制备方法及其用途
CN108084170A (zh) * 2017-12-22 2018-05-29 佛山汉方中医医院有限公司 一类含哌嗪烷氧噻吩结构的二环腈类化合物、制备方法及其用途
CN108003146A (zh) * 2017-12-22 2018-05-08 佛山汉方中医医院有限公司 一类含烷氧噻吩的二环腈类ssao抑制剂、制备方法及其用途
CN108129470A (zh) * 2017-12-22 2018-06-08 佛山汉方中医医院有限公司 异丙基哌嗪噻吩二环腈类化合物、其制备方法及其用途
CN107936002A (zh) * 2017-12-22 2018-04-20 佛山汉方中医医院有限公司 一种异丙基哌嗪胺基噻吩二环腈类化合物及其用途
CN108069947A (zh) * 2017-12-22 2018-05-25 佛山汉方中医医院有限公司 含二甲胺噻吩和异丙基哌嗪胺基结构的二环腈类化合物及用途
CN108003148A (zh) * 2017-12-22 2018-05-08 佛山汉方中医医院有限公司 异丙基哌嗪噻吩二环腈类化合物、制备方法及其用途
CN108084169A (zh) * 2017-12-22 2018-05-29 佛山汉方中医医院有限公司 一种硝基噻吩的二环腈类化合物及其用途
CN107880032A (zh) * 2017-12-22 2018-04-06 佛山汉方中医医院有限公司 含噻吩的二环腈类ssao抑制剂、制备方法及其用途
CN108148051A (zh) * 2017-12-22 2018-06-12 佛山汉方中医医院有限公司 一种含氟噻吩的二环腈类ssao抑制剂及其用途
CN108084168A (zh) * 2017-12-22 2018-05-29 佛山汉方中医医院有限公司 一种哌嗪噻吩二环腈类化合物、制备方法及其用途
CN108129469A (zh) * 2017-12-22 2018-06-08 佛山汉方中医医院有限公司 一种异丙基哌嗪硝基噻吩二环腈类化合物及其用途
CN108069949A (zh) * 2017-12-22 2018-05-25 佛山汉方中医医院有限公司 烷基取代的哌嗪甲基噻吩二环腈类化合物、制备方法及其用途
CN108047213A (zh) * 2017-12-22 2018-05-18 佛山汉方中医医院有限公司 一种含硫环的氟噻吩的二环腈类化合物及其用途
US11547759B2 (en) 2019-01-30 2023-01-10 Montelino Therapeutics, Inc. Bi-functional compounds and methods for targeted ubiquitination of androgen receptor
US11465998B2 (en) 2019-04-25 2022-10-11 Regents Of The University Of Minnesota Therapeutic compounds and methods of use thereof
EP4153587A4 (en) * 2020-05-18 2024-06-12 Montelino Therapeutics, Inc. BI-FUNCTIONAL COMPOUNDS AND METHODS FOR TARGETED UBIQUITINATION OF THE ANDROGEN RECEPTOR
US20250115595A1 (en) * 2021-08-09 2025-04-10 The Johns Hopkins University Inhibitors of hypoxia-inducible factors
US11981672B2 (en) 2021-09-13 2024-05-14 Montelino Therapeutics Inc. Bi-functional compounds and methods for targeted ubiquitination of androgen receptor
WO2024059951A1 (en) * 2022-09-22 2024-03-28 The University Of British Columbia Inhibitors of the androgen receptor dna-binding domain
WO2024102810A1 (en) 2022-11-08 2024-05-16 Montelino Therapeutics, Inc. Bi-functional compounds and methods for targeted ubiquitination of androgen receptor
CN116768881B (zh) * 2023-06-30 2025-09-09 郑州大学 4-(3-吲哚基)-1,3-噻唑类化合物及其制备方法和应用
WO2025064918A1 (en) * 2023-09-20 2025-03-27 The Board Of Regents Of The University Of Texas System First-in-class phospho-brd4 inhibitors

Citations (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JPS61291655A (ja) * 1985-06-14 1986-12-22 バイエル・アクチエンゲゼルシヤフト 2,2−ジアリ−ルクロメノチアゾ−ル類
JP2003195570A (ja) * 2001-11-20 2003-07-09 Nexpress Solutions Llc 静電グラフィック画像用マゼンタ色トナー粒子
JP2008531537A (ja) * 2005-02-25 2008-08-14 クドス ファーマシューティカルズ リミテッド 化合物
JP2010504295A (ja) * 2006-09-21 2010-02-12 ノバルティス アーゲー サイトカイン介在疾患の処置に有用なピロール誘導体
US20120004270A1 (en) * 2010-07-02 2012-01-05 Radius Health, Inc. Selective Androgen Receptor Modulators
WO2012125981A2 (en) * 2011-03-17 2012-09-20 Selexagen Therapeutics, Inc. Raf kinase inhibitors
WO2012143599A1 (en) * 2011-04-21 2012-10-26 Orion Corporation Androgen receptor modulating carboxamides

Family Cites Families (19)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DE3509271A1 (de) * 1985-03-15 1986-09-18 Basf Ag, 6700 Ludwigshafen Isothiazol-azofarbstoffe
JPH11209284A (ja) * 1998-01-27 1999-08-03 Sagami Chem Res Center 骨形成促進剤
TW583185B (en) * 2000-06-13 2004-04-11 Novartis Ag N-(substituted glycyl)-2-cyanopyrrolidines and pharmaceutical composition for inhibiting dipeptidyl peptidase-IV (DPP-IV) or for the prevention or treatment of diseases or conditions associated with elevated levels of DPP-IV comprising the same
US6451814B1 (en) * 2000-07-17 2002-09-17 Wyeth Heterocyclic β-3 adrenergic receptor agonists
WO2002051821A1 (en) * 2000-12-22 2002-07-04 Astrazeneca Ab Therapeutic compounds
AU2002353739A1 (en) * 2001-11-28 2003-06-10 Astrazeneca Ab Therapeutic compounds
GB0315111D0 (en) * 2003-06-27 2003-07-30 Cancer Rec Tech Ltd Substituted 5-membered ring compounds and their use
US7384966B2 (en) * 2004-08-31 2008-06-10 Pharminxo Limited 2-arylbenzothiazole derivatives
RU2007122490A (ru) * 2004-11-18 2008-12-27 Такеда Фармасьютикал Компани Лимитед (Jp) Амидное соединение
GB0503962D0 (en) * 2005-02-25 2005-04-06 Kudos Pharm Ltd Compounds
EP1904491A2 (en) * 2005-05-31 2008-04-02 Vertex Pharmaceuticals Incorporated Heterocycles useful as modulators of ion channels
BRPI0709771B1 (pt) 2006-03-27 2022-01-25 The Regents Of The University Of California Composto e composição farmacêutica
EP2120580B1 (en) 2007-02-02 2017-12-27 Baylor College Of Medicine Compositions and methods for the treatment of metabolic disorders
US9085566B2 (en) 2007-02-02 2015-07-21 Baylor College Of Medicine Compositions and methods for the treatment of metabolic and related disorders
DE102007040243A1 (de) 2007-08-25 2009-02-26 Universität des Saarlandes 17Beta-Hydroxysteriod-Dehydrogenase Typ1 Inhibitoren zur Behandlung hormonabhängiger Erkrankungen
CN102066365A (zh) * 2008-06-19 2011-05-18 米伦纽姆医药公司 噻吩或噻唑衍生物和其作为pi3k抑制剂的用途
WO2010118347A2 (en) * 2009-04-10 2010-10-14 Zacharon Pharmaceuticals, Inc. O-linked glycan biosynthesis modulators
DE102010012594A1 (de) * 2010-03-23 2011-09-29 Beiersdorf Ag Kosmetische oder dermatologische Zubereitungen mit einem Gehalt an einem oder mehreren Thiazolderivaten
US20130096160A1 (en) * 2010-04-14 2013-04-18 Secretary, Department Of Health And Human Services Arylthiazolyl piperidines and related compounds as modulators of survival motor neuron (smn) protein production

Patent Citations (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JPS61291655A (ja) * 1985-06-14 1986-12-22 バイエル・アクチエンゲゼルシヤフト 2,2−ジアリ−ルクロメノチアゾ−ル類
JP2003195570A (ja) * 2001-11-20 2003-07-09 Nexpress Solutions Llc 静電グラフィック画像用マゼンタ色トナー粒子
JP2008531537A (ja) * 2005-02-25 2008-08-14 クドス ファーマシューティカルズ リミテッド 化合物
JP2010504295A (ja) * 2006-09-21 2010-02-12 ノバルティス アーゲー サイトカイン介在疾患の処置に有用なピロール誘導体
US20120004270A1 (en) * 2010-07-02 2012-01-05 Radius Health, Inc. Selective Androgen Receptor Modulators
WO2012125981A2 (en) * 2011-03-17 2012-09-20 Selexagen Therapeutics, Inc. Raf kinase inhibitors
WO2012143599A1 (en) * 2011-04-21 2012-10-26 Orion Corporation Androgen receptor modulating carboxamides

Non-Patent Citations (1)

* Cited by examiner, † Cited by third party
Title
DATABASE REGISTRY, JPN7018003563, 10 October 2012 (2012-10-10), ISSN: 0004266733 *

Cited By (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2022504296A (ja) * 2018-10-03 2022-01-13 ザ・ユニバーシティ・オブ・ブリティッシュ・コロンビア 治療薬としての転写因子brn2阻害化合物およびそれらの使用方法
JP2022523916A (ja) * 2019-01-30 2022-04-27 モンテリノ・セラピューティクス・インコーポレイテッド アンドロゲン受容体を標的とするユビキチン化のための二官能性化合物および方法
JP7555938B2 (ja) 2019-01-30 2024-09-25 モンテリノ・セラピューティクス・インコーポレイテッド アンドロゲン受容体を標的とするユビキチン化のための二官能性化合物および方法
JP2022547707A (ja) * 2019-09-12 2022-11-15 ディスアーム セラピューティクス, インコーポレイテッド Sarm1の阻害剤
JP7534390B2 (ja) 2019-09-12 2024-08-14 ディスアーム セラピューティクス, インコーポレイテッド Sarm1の阻害剤

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