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MX2016010604A - Compuestos de dominio de unión a ácido desoxirribonucleico (dbd a adn) del receptor de andrógeno humano como terapéuticos, y métodos para su uso. - Google Patents

Compuestos de dominio de unión a ácido desoxirribonucleico (dbd a adn) del receptor de andrógeno humano como terapéuticos, y métodos para su uso.

Info

Publication number
MX2016010604A
MX2016010604A MX2016010604A MX2016010604A MX2016010604A MX 2016010604 A MX2016010604 A MX 2016010604A MX 2016010604 A MX2016010604 A MX 2016010604A MX 2016010604 A MX2016010604 A MX 2016010604A MX 2016010604 A MX2016010604 A MX 2016010604A
Authority
MX
Mexico
Prior art keywords
compounds
substituted
heteroaryl
dbd
therapeutics
Prior art date
Application number
MX2016010604A
Other languages
English (en)
Inventor
Tcherkassov Artem
S Rennie Paul
Ban Fuqiang
Li Huifang
Joseph Jean Leblanc Eric
Dalal Kush
V Tverdokhlebov Anton
Babiy Sergiy
BOGOMOL Evgeniia
DUNAYENKO Kateryna
Original Assignee
Univ British Columbia
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Univ British Columbia filed Critical Univ British Columbia
Publication of MX2016010604A publication Critical patent/MX2016010604A/es

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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
    • A61K31/422—Oxazoles not condensed and containing further heterocyclic rings
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    • 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
    • A61K31/425—Thiazoles
    • A61K31/426—1,3-Thiazoles
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    • 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
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    • A61K31/425—Thiazoles
    • A61K31/428—Thiazoles condensed with carbocyclic rings
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    • A61K31/437—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline
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    • A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/4439—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
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  • Endocrinology (AREA)
  • Reproductive Health (AREA)
  • Dermatology (AREA)
  • Pregnancy & Childbirth (AREA)
  • Gynecology & Obstetrics (AREA)
  • Ophthalmology & Optometry (AREA)
  • Diabetes (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Heterocyclic Compounds Containing Sulfur Atoms (AREA)
  • Thiazole And Isothizaole Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)

Abstract

Un compuesto que tiene la estructura de la Fórmula I, en la que A es un grupo arilo o heteroarilo sustituido o no sustituido, D es un grupo heteroarilo o heterociclilo de 5 o 6 miembros sustituido o no sustituido y E es un grupo arilo, heteroarilo, cicloalquilo o heterociclilo sustituido o no sustituido. Los compuestos se usan para el tratamiento de indicaciones moduladas por andrógenos incluyendo cáncer (cáncer de próstata, mama, ovario, endometrio o vejiga), pérdida de cabello, acné, hirsutismo, quistes ováricos, enfermedad de ovarios poliquísticos, pubertad precoz y degeneración macular relacionada con la edad. Se describen también el uso de los compuestos de fabricación de un medicamento modular la actividad de AR, un método de tratamiento usando tales compuestos y una composición farmacéutica y un envase comercial que comprende tales compuestos.
MX2016010604A 2014-02-14 2015-02-13 Compuestos de dominio de unión a ácido desoxirribonucleico (dbd a adn) del receptor de andrógeno humano como terapéuticos, y métodos para su uso. MX2016010604A (es)

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Families Citing this family (32)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
PL3511319T3 (pl) * 2014-07-03 2023-09-11 Celgene Quanticel Research, Inc. Inhibitory lizyno-specyficznej demetylazy-1
JP2020502188A (ja) * 2016-12-19 2020-01-23 エフ・ホフマン−ラ・ロシュ・アクチェンゲゼルシャフト Ａｒ−ｖ７インヒビター
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
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
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
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
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
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
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
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
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
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
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
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
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
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
EP3860994B1 (en) * 2018-10-03 2024-08-14 The University of British Columbia Transcription factor brn2 inhibitory compounds as therapeutics and methods for their use
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
EP4028013A4 (en) * 2019-09-12 2023-10-18 Disarm Therapeutics, Inc. MRSA1 INHIBITORS
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
CN116768881A (zh) * 2023-06-30 2023-09-19 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
US20060106074A1 (en) * 2001-11-28 2006-05-18 Peter Bernstein Er-b-selective ligands
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
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
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
LT3412290T (lt) 2006-03-27 2021-04-26 The Regents Of The University Of California Androgeno receptorių moduliatorius, skirtas prostatos vėžio bei su androgeno receptoriais susijusių ligų gydymui
EP2069333A1 (en) * 2006-09-21 2009-06-17 Novartis Ag Pyrrole derivatives useful for the treatment of cytokine-mediated diseases
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
BRPI0914223A2 (pt) * 2008-06-19 2019-09-24 Millennium Pharm Inc derivados de tiofeno ou tiazol e seus usos como inibidores de p13k
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
WO2012125981A2 (en) * 2011-03-17 2012-09-20 Selexagen Therapeutics, Inc. Raf kinase inhibitors
BR112013026905B1 (pt) * 2011-04-21 2021-09-14 Orion Corporation Compostos de carboxamida moduladora do receptor de andrógeno e seu uso no tratamento e prevenção de câncer de próstata, bem como composições farmacêuticas compreendendo os ditos compostos

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CN106164071A (zh) 2016-11-23
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