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 PDFInfo
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- 150000001875 compounds Chemical class 0.000 title claims 48
- 239000003814 drug Substances 0.000 title claims 4
- 239000003098 androgen Substances 0.000 title 1
- 229940124597 therapeutic agent Drugs 0.000 title 1
- CBOIHMRHGLHBPB-UHFFFAOYSA-N hydroxymethyl Chemical compound O[CH2] CBOIHMRHGLHBPB-UHFFFAOYSA-N 0.000 claims 30
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 claims 25
- 125000000956 methoxy group Chemical group [H]C([H])([H])O* 0.000 claims 24
- 206010028980 Neoplasm Diseases 0.000 claims 20
- 201000011510 cancer Diseases 0.000 claims 20
- 238000000034 method Methods 0.000 claims 18
- 230000000694 effects Effects 0.000 claims 17
- 206010006187 Breast cancer Diseases 0.000 claims 8
- 208000026310 Breast neoplasm Diseases 0.000 claims 8
- BAVYZALUXZFZLV-UHFFFAOYSA-N Methylamine Chemical compound NC BAVYZALUXZFZLV-UHFFFAOYSA-N 0.000 claims 8
- 208000002874 Acne Vulgaris Diseases 0.000 claims 4
- 201000004384 Alopecia Diseases 0.000 claims 4
- 206010005003 Bladder cancer Diseases 0.000 claims 4
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- 206010033128 Ovarian cancer Diseases 0.000 claims 4
- 206010061535 Ovarian neoplasm Diseases 0.000 claims 4
- 206010060862 Prostate cancer Diseases 0.000 claims 4
- 208000000236 Prostatic Neoplasms Diseases 0.000 claims 4
- 208000007097 Urinary Bladder Neoplasms Diseases 0.000 claims 4
- 206010000496 acne Diseases 0.000 claims 4
- 206010064930 age-related macular degeneration Diseases 0.000 claims 4
- 231100000360 alopecia Toxicity 0.000 claims 4
- 208000002780 macular degeneration Diseases 0.000 claims 4
- 230000001404 mediated effect Effects 0.000 claims 4
- 125000000896 monocarboxylic acid group Chemical group 0.000 claims 4
- 208000025661 ovarian cyst Diseases 0.000 claims 4
- 201000004228 ovarian endometrial cancer Diseases 0.000 claims 4
- 239000008194 pharmaceutical composition Substances 0.000 claims 4
- 201000010065 polycystic ovary syndrome Diseases 0.000 claims 4
- 201000005112 urinary bladder cancer Diseases 0.000 claims 4
- 239000003937 drug carrier Substances 0.000 claims 3
- 238000004519 manufacturing process Methods 0.000 claims 3
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- 239000000546 pharmaceutical excipient Substances 0.000 claims 3
- 208000006155 precocious puberty Diseases 0.000 claims 2
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Classifications
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- C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
- C07D471/04—Ortho-condensed systems
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D513/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00
- C07D513/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00 in which the condensed system contains two hetero rings
- C07D513/04—Ortho-condensed systems
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- Medicinal Chemistry (AREA)
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- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
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- Endocrinology (AREA)
- Ophthalmology & Optometry (AREA)
- Gynecology & Obstetrics (AREA)
- Pregnancy & Childbirth (AREA)
- Diabetes (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Heterocyclic Compounds Containing Sulfur Atoms (AREA)
- Thiazole And Isothizaole Compounds (AREA)
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| US62/023,773 | 2014-07-11 | ||
| PCT/CA2015/000086 WO2015120543A1 (en) | 2014-02-14 | 2015-02-13 | Human androgen receptor dna-binding domain (dbd) compounds as therapeutics and methods for their use |
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| RU (1) | RU2016136091A (https=) |
| WO (1) | WO2015120543A1 (https=) |
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| 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 |
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| 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 |
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| 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 |
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| 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 |
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| 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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| US20170183319A1 (en) | 2017-06-29 |
| MX2016010604A (es) | 2017-04-27 |
| JP2019142880A (ja) | 2019-08-29 |
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| JP2017505787A (ja) | 2017-02-23 |
| WO2015120543A1 (en) | 2015-08-20 |
| US10011573B2 (en) | 2018-07-03 |
| AU2015218140A1 (en) | 2016-09-01 |
| CA2939048A1 (en) | 2015-08-20 |
| CN106164071A (zh) | 2016-11-23 |
| KR20160115999A (ko) | 2016-10-06 |
| EP3105229A1 (en) | 2016-12-21 |
| EP3105229A4 (en) | 2017-12-20 |
| BR112016018691A2 (pt) | 2017-08-08 |
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