CA2939048A1 - Human androgen receptor dna-binding domain (dbd) compounds as therapeutics and methods for their use - Google Patents

Human androgen receptor dna-binding domain (dbd) compounds as therapeutics and methods for their use Download PDF

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Publication number
CA2939048A1
CA2939048A1 CA2939048A CA2939048A CA2939048A1 CA 2939048 A1 CA2939048 A1 CA 2939048A1 CA 2939048 A CA2939048 A CA 2939048A CA 2939048 A CA2939048 A CA 2939048A CA 2939048 A1 CA2939048 A1 CA 2939048A1
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ch2ch3
ch2oh
och3
so2ch3
nhch3
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CA2939048A
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English (en)
French (fr)
Inventor
Artem Tcherkassov
Paul S. Rennie
Fuqiang Ban
Huifang Li
Eric Joseph Jean LEBLANC
Anton V. Tverdokhlebov
Evgeniia Bogomol
Kateryna Dunayenko
Sergiy Babiy
Anton V. Tvekjdokhlebov
Kush Dalal
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University of British Columbia
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University of British Columbia
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    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • 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
    • A61K31/42—Oxazoles
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    • C07D207/30—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having two double bonds between ring members or between ring members and non-ring members
    • C07D207/34—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having two double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
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Families Citing this family (32)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EA201891526A3 (ru) * 2014-07-03 2019-05-31 Селджен Квонтисел Рисёрч, Инк. Ингибиторы лизин-специфической деметилазы-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
US10933061B2 (en) 2017-12-21 2021-03-02 Shepherd Therapeutics, Inc. Pyrvinium pamoate therapies and methods of use
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
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
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
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
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
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
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
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
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
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
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
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
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
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
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
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
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
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
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
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
WO2021236695A1 (en) * 2020-05-18 2021-11-25 Montelino Therapeutics, Inc. Bi-functional compounds and methods for targeted ubiquitination of androgen receptor
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
US20240207415A1 (en) 2022-11-08 2024-06-27 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

Family Cites Families (26)

* 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
DE3521406A1 (de) * 1985-06-14 1986-12-18 Bayer Ag, 5090 Leverkusen 2,2-diaryl-chromenothiazole, ihre herstellung und ihre verwendung in aufzeichnungsmaterialien
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
EP1345914A1 (en) 2000-12-22 2003-09-24 AstraZeneca AB Therapeutic compounds
US6528223B1 (en) * 2001-11-20 2003-03-04 Nexpress Solutions Llc Magenta-colored toner particles for electrostatographic imaging
WO2003045930A1 (en) 2001-11-28 2003-06-05 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
CN101103007A (zh) * 2004-11-18 2008-01-09 武田药品工业株式会社 酰胺化合物
GB0503962D0 (en) * 2005-02-25 2005-04-06 Kudos Pharm Ltd Compounds
AU2006217742A1 (en) * 2005-02-25 2006-08-31 Kudos Pharmaceuticals Limited Hydrazinomethyl, HYDR zonomethyl and 5-membered heterocylic compounds which act as MTOR inhibitors and their use as anti cancer agents
WO2006130493A2 (en) * 2005-05-31 2006-12-07 Vertex Pharmaceuticals Incorporated Heterocycles useful as modulators of ion channels
LT2656842T (lt) 2006-03-27 2016-09-26 The Regents Of The University Of California Androgeno receptoriaus moduliatorius, skirtas prostatos vėžio ir su androgeno receptoriumi susijusių ligų gydymui
BRPI0717097A2 (pt) * 2006-09-21 2013-11-26 Novartis Ag Derivados de pirrol úteis para o tratamento de doenças mediadas por citocina
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
JP5596026B2 (ja) * 2008-06-19 2014-09-24 ミレニアム ファーマシューティカルズ， インコーポレイテッド チオフェン又はチアゾール誘導体及びｐｉ３ｋ阻害剤としてのそれらの使用
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
WO2011130515A1 (en) * 2010-04-14 2011-10-20 The United States Of America, As Represented By The Secretary, Department Of Health And Human Services Arylthiazolyl piperidines and related compounds as modulators of survival motor neuron (smn) protein production
US8642632B2 (en) * 2010-07-02 2014-02-04 Radius Health, Inc. Selective androgen receptor modulators
EP2686317A4 (en) * 2011-03-17 2014-08-20 Selexagen Therapeutics Inc RAF KINASE INHIBITORS
ES2541295T3 (es) * 2011-04-21 2015-07-17 Orion Corporation Carboxamidas que modulan el receptor de andrógenos

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