RU2016136091A - Соединения, воздействующие на днк-связывающий домен (dbd) андрогенового рецептора человека, в качестве терапевтических средств, а также способы их применения - Google Patents

Соединения, воздействующие на днк-связывающий домен (dbd) андрогенового рецептора человека, в качестве терапевтических средств, а также способы их применения Download PDF

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RU2016136091A
RU2016136091A RU2016136091A RU2016136091A RU2016136091A RU 2016136091 A RU2016136091 A RU 2016136091A RU 2016136091 A RU2016136091 A RU 2016136091A RU 2016136091 A RU2016136091 A RU 2016136091A RU 2016136091 A RU2016136091 A RU 2016136091A
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cancer
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Артем ЧЕРКАСОВ
С. РЕННИ Пол
Фуцюйян БАН
Хуэйфан ЛИ
Эрик Жозеф Жан ЛЕБЛАН
Куш ДАЛАЛ
Антон В. ТВЕРДОХЛЕБОВ
Сергей БАБИЙ
Евгения БОГОМОЛ
Катерина ДУНАЕНКО
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Дзе Юниверсити Оф Бритиш Коламбиа
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RU2016136091A 2014-02-14 2015-02-13 Соединения, воздействующие на днк-связывающий домен (dbd) андрогенового рецептора человека, в качестве терапевтических средств, а также способы их применения RU2016136091A (ru)

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Families Citing this family (32)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
FI3511319T3 (fi) * 2014-07-03 2023-07-20 Celgene Quanticel Res Inc Lysiinispesifisen demetylaasi-1:n inhibiittoreita
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
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
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
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
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
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
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
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
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
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
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
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
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
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
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
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
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
US20220106304A1 (en) 2018-10-03 2022-04-07 The University Of British Columbia Transcription Factor BRN2 Inhibitory Compounds as Therapeutics and Methods for Their Use
EP3917916A4 (en) 2019-01-30 2022-12-14 Montelino Therapeutics, Inc. Bi-functional compounds and methods for targeted ubiquitination of androgen receptor
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
CA3150878A1 (en) * 2019-09-12 2021-03-18 Jonathan Bentley Inhibitors of sarm1
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
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

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
WO2002051821A1 (en) * 2000-12-22 2002-07-04 Astrazeneca Ab Therapeutic compounds
US6528223B1 (en) * 2001-11-20 2003-03-04 Nexpress Solutions Llc Magenta-colored toner particles for electrostatographic imaging
EP1478631A1 (en) 2001-11-28 2004-11-24 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
CA2599320A1 (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
JP5388574B2 (ja) * 2005-05-31 2014-01-15 バーテックス ファーマシューティカルズ インコーポレイテッド イオンチャネルのモジュレーターとして有用なヘテロ環式類
SI2656842T1 (sl) 2006-03-27 2016-10-28 The Regents Of The University Of California Modulator androgenih receptorjev za zdravljenje raka prostate in bolezni, povezanih z androgenimi receptorji
CA2662359A1 (en) * 2006-09-21 2008-03-27 Novartis Ag Pyrrole derivatives useful for the treatment of cytokine-mediated diseases
JP5461197B2 (ja) * 2007-02-02 2014-04-02 ベイラー カレッジ オブ メディスン 代謝障害を処置するための組成物および方法
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
ES2491522T3 (es) * 2008-06-19 2014-09-08 Millennium Pharmaceuticals, Inc. Derivados de tiofeno o tiazol y su uso como inhibidores de PI3K
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
US8642632B2 (en) * 2010-07-02 2014-02-04 Radius Health, Inc. Selective androgen receptor modulators
US20140221374A1 (en) * 2011-03-17 2014-08-07 Ruga Corporation Raf kinase inhibitors
WO2012143599A1 (en) * 2011-04-21 2012-10-26 Orion Corporation Androgen receptor modulating carboxamides

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CN106164071A (zh) 2016-11-23
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