BR112016018691A2 - Compostos do domínio de ligação ao dna (dbd) de receptor de andrógeno humano como terapêuticos e métodos para seu uso - Google Patents
Compostos do domínio de ligação ao dna (dbd) de receptor de andrógeno humano como terapêuticos e métodos para seu usoInfo
- Publication number
- BR112016018691A2 BR112016018691A2 BR112016018691A BR112016018691A BR112016018691A2 BR 112016018691 A2 BR112016018691 A2 BR 112016018691A2 BR 112016018691 A BR112016018691 A BR 112016018691A BR 112016018691 A BR112016018691 A BR 112016018691A BR 112016018691 A2 BR112016018691 A2 BR 112016018691A2
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- Prior art keywords
- compounds
- dbd
- therapeutics
- substituted
- binding domain
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- C07D277/20—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
- C07D277/32—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings having two or three 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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- 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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- A61K31/425—Thiazoles
- A61K31/426—1,3-Thiazoles
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- A61K31/425—Thiazoles
- A61K31/427—Thiazoles not condensed and containing further heterocyclic rings
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- A61K31/425—Thiazoles
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- A61K31/435—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
- A61K31/4353—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
- 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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- A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
- 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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- A61K31/5375—1,4-Oxazines, e.g. morpholine
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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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- Nitrogen Condensed Heterocyclic Rings (AREA)
Abstract
COMPOSTOS DO DOMÍNIO DE LIGAÇÃO AO DNA (DBD) DE RECEPTOR DE ANDRÓGENO HUMANO COMO TERAPÊUTICOS E MÉTODOS PARA SEU USO. Um composto tendo a estrutura da Fórmula I, em que A é um grupo arila ou heteroarila substituído ou não substituído, D é um grupo heteroarila ou heterociclila de 5 ou 6 membros substituído ou não substituído e E é um grupo arila, heteroarila, cicloalquila ou heterociclila substituído ou não substituído. Os compostos são usados para o tratamento de indicações moduladoras de andrógeno incluindo câncer (câncer de próstata, mama, ovário, endométrio ou bexiga), perda de cabelo, acne, hirsutismo, cistos ovarianos, doença do ovário policístico, puberdade precoce e degeneração macular relacionada à idade. O uso dos compostos para a fabricação de um medicamento para modular a atividade de AR, um método de tratamento usando tais compostos e uma composição farmacêutica e um pacote comercial compreendendo os ditos compostos também são descritos.
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US201461940275P | 2014-02-14 | 2014-02-14 | |
US201462023773P | 2014-07-11 | 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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BR112016018691A BR112016018691A2 (pt) | 2014-02-14 | 2015-02-13 | Compostos do domínio de ligação ao dna (dbd) de receptor de andrógeno humano como terapêuticos e métodos para seu uso |
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US (1) | US10011573B2 (pt) |
EP (1) | EP3105229A4 (pt) |
JP (2) | JP2017505787A (pt) |
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CA (1) | CA2939048A1 (pt) |
MX (1) | MX2016010604A (pt) |
RU (1) | RU2016136091A (pt) |
WO (1) | WO2015120543A1 (pt) |
Families Citing this family (30)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
SI3511319T1 (sl) * | 2014-07-03 | 2023-10-30 | Celgene Quanticel Research, Inc. | Inhibitorji lizin specifične demetilaze-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 |
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 |
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 |
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 |
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 |
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 |
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 |
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 |
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 |
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 |
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 |
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 |
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 |
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 |
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 |
WO2020069625A1 (en) | 2018-10-03 | 2020-04-09 | The University Of British Columbia | Transcription factor brn2 inhibitory compounds as therapeutics and methods for their use |
US11547759B2 (en) | 2019-01-30 | 2023-01-10 | Montelino Therapeutics, Inc. | Bi-functional compounds and methods for targeted ubiquitination of androgen receptor |
EP3917916A4 (en) | 2019-01-30 | 2022-12-14 | Montelino Therapeutics, Inc. | BIFUNCTIONAL COMPOUNDS AND METHODS FOR TARGETING ANDROGEN RECEPTOR UBIQUITINATION |
US11465998B2 (en) | 2019-04-25 | 2022-10-11 | Regents Of The University Of Minnesota | Therapeutic compounds and methods of use thereof |
US20220315568A1 (en) * | 2019-09-12 | 2022-10-06 | Disarm Therapeutics, Inc. | Inhibitors of sarm1 |
EP4153587A4 (en) * | 2020-05-18 | 2024-06-12 | Montelino Therapeutics Inc | BIFUNCTIONAL COMPOUNDS AND METHODS FOR TARGETED UBIQUITINATION OF THE 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 |
Family Cites Families (26)
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 |
US7045539B2 (en) | 2000-12-22 | 2006-05-16 | Astrazeneca Ab | Therapeutic benzoxazole 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 |
RU2007122490A (ru) * | 2004-11-18 | 2008-12-27 | Такеда Фармасьютикал Компани Лимитед (Jp) | Амидное соединение |
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 |
GB0503962D0 (en) * | 2005-02-25 | 2005-04-06 | Kudos Pharm Ltd | Compounds |
WO2006130493A2 (en) * | 2005-05-31 | 2006-12-07 | Vertex Pharmaceuticals Incorporated | Heterocycles useful as modulators of ion channels |
EP2004181B3 (en) | 2006-03-27 | 2023-05-24 | The Regents Of The University Of California | Androgen receptor modulator for the treatment of prostate cancer and androgen receptor-associated diseases |
AU2007299261A1 (en) * | 2006-09-21 | 2008-03-27 | Novartis Ag | Pyrrole derivatives useful for the treatment of cytokine-mediated diseases |
CN101674730B (zh) * | 2007-02-02 | 2014-09-10 | 贝勒医学院 | 用于治疗代谢疾病的组合物和方法 |
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 |
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 |
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 |
EP2686317A4 (en) * | 2011-03-17 | 2014-08-20 | Selexagen Therapeutics Inc | RAF KINASE INHIBITORS |
MX360611B (es) | 2011-04-21 | 2018-11-09 | Orion Corp | Carboxamidas que modulan el receptor de andrógeno. |
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JP2019142880A (ja) | 2019-08-29 |
EP3105229A1 (en) | 2016-12-21 |
WO2015120543A1 (en) | 2015-08-20 |
CN106164071B (zh) | 2019-09-10 |
EP3105229A4 (en) | 2017-12-20 |
AU2015218140A1 (en) | 2016-09-01 |
US20170183319A1 (en) | 2017-06-29 |
KR20160115999A (ko) | 2016-10-06 |
JP2017505787A (ja) | 2017-02-23 |
US10011573B2 (en) | 2018-07-03 |
CA2939048A1 (en) | 2015-08-20 |
MX2016010604A (es) | 2017-04-27 |
RU2016136091A (ru) | 2018-03-19 |
CN106164071A (zh) | 2016-11-23 |
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