BR112015032113B1 - análogos de (e)-n’-(1-feniletilideno)benzohidrazida substituídos como inibidores de histona demetilase - Google Patents
análogos de (e)-n’-(1-feniletilideno)benzohidrazida substituídos como inibidores de histona demetilase Download PDFInfo
- Publication number
- BR112015032113B1 BR112015032113B1 BR112015032113-5A BR112015032113A BR112015032113B1 BR 112015032113 B1 BR112015032113 B1 BR 112015032113B1 BR 112015032113 A BR112015032113 A BR 112015032113A BR 112015032113 B1 BR112015032113 B1 BR 112015032113B1
- Authority
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- Brazil
- Prior art keywords
- compound
- compounds
- mmol
- disclosed
- cancer
- Prior art date
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Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D295/00—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms
- C07D295/22—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with hetero atoms directly attached to ring nitrogen atoms
- C07D295/26—Sulfur atoms
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D211/00—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings
- C07D211/92—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with a hetero atom directly attached to the ring nitrogen atom
- C07D211/96—Sulfur atom
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D213/00—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
- C07D213/02—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
- C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
- C07D213/60—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom 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
- C07D213/78—Carbon atoms having three bonds to hetero atoms, with at the most one bond to halogen, e.g. ester or nitrile radicals
- C07D213/86—Hydrazides; Thio or imino analogues thereof
- C07D213/87—Hydrazides; Thio or imino analogues thereof in position 3
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D231/00—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings
- C07D231/02—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings
- C07D231/10—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
- C07D231/12—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms
Landscapes
- Organic Chemistry (AREA)
- Chemical & Material Sciences (AREA)
- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Animal Behavior & Ethology (AREA)
- Medicinal Chemistry (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
- Pyridine Compounds (AREA)
- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US13/921,895 | 2013-06-19 | ||
| US13/921,895 US9266838B2 (en) | 2011-08-15 | 2013-06-19 | Substituted (E)-N′-(1-phenylethylidene)benzohydrazide analogs as histone demethylase inhibitors |
| PCT/US2014/043179 WO2014205213A1 (en) | 2013-06-19 | 2014-06-19 | Substituted (e)-n'-(1-phenylethylidene) benzohydrazide analogs as histone demethylase inhibitors |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| BR112015032113A2 BR112015032113A2 (pt) | 2017-03-21 |
| BR112015032113B1 true BR112015032113B1 (pt) | 2019-01-29 |
Family
ID=52105283
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| BR112015032113-5A BR112015032113B1 (pt) | 2013-06-19 | 2014-06-19 | análogos de (e)-n’-(1-feniletilideno)benzohidrazida substituídos como inibidores de histona demetilase |
Country Status (13)
| Country | Link |
|---|---|
| EP (1) | EP3010915B1 (https=) |
| JP (1) | JP6525162B2 (https=) |
| KR (1) | KR102288648B1 (https=) |
| CN (2) | CN110015984A (https=) |
| AU (1) | AU2014281398B2 (https=) |
| BR (1) | BR112015032113B1 (https=) |
| CA (1) | CA2915817C (https=) |
| ES (1) | ES2739814T3 (https=) |
| IL (1) | IL243200B (https=) |
| MX (1) | MX366949B (https=) |
| NZ (1) | NZ715331A (https=) |
| SG (2) | SG11201510376QA (https=) |
| WO (1) | WO2014205213A1 (https=) |
Families Citing this family (37)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| BR112015032113B1 (pt) * | 2013-06-19 | 2019-01-29 | University Of Utah Research Foundation | análogos de (e)-n’-(1-feniletilideno)benzohidrazida substituídos como inibidores de histona demetilase |
| JP6602779B2 (ja) | 2014-02-13 | 2019-11-06 | インサイト・コーポレイション | Ｌｓｄ１阻害剤としてのシクロプロピルアミン類 |
| EP3105218B1 (en) | 2014-02-13 | 2019-09-25 | Incyte Corporation | Cyclopropylamines as lsd1 inhibitors |
| EP3105219B9 (en) | 2014-02-13 | 2018-10-03 | Incyte Corporation | Cyclopropylamines as lsd1 inhibitors |
| US9527835B2 (en) | 2014-02-13 | 2016-12-27 | Incyte Corporation | Cyclopropylamines as LSD1 inhibitors |
| US9758523B2 (en) | 2014-07-10 | 2017-09-12 | Incyte Corporation | Triazolopyridines and triazolopyrazines as LSD1 inhibitors |
| WO2016007731A1 (en) | 2014-07-10 | 2016-01-14 | Incyte Corporation | Imidazopyridines and imidazopyrazines as lsd1 inhibitors |
| US9695167B2 (en) | 2014-07-10 | 2017-07-04 | Incyte Corporation | Substituted triazolo[1,5-a]pyridines and triazolo[1,5-a]pyrazines as LSD1 inhibitors |
| US9695180B2 (en) | 2014-07-10 | 2017-07-04 | Incyte Corporation | Substituted imidazo[1,2-a]pyrazines as LSD1 inhibitors |
| WO2016119031A1 (pt) * | 2015-01-29 | 2016-08-04 | Fundação De Amparo À Pesquisa Do Estado De Minas Gerais - Fapemig | Composto, processo de síntese do composto, uso, composição farmacêutica, método de tratamento de inflamações ou de doença neurodegenerativa, forma de dosagem oral e método de inibição de enzima acetilcolinesterase |
| EP3277689B1 (en) | 2015-04-03 | 2019-09-04 | Incyte Corporation | Heterocyclic compounds as lsd1 inhibitors |
| AU2016275702A1 (en) | 2015-06-12 | 2017-12-21 | Oryzon Genomics, S.A. | Biomarkers associated with LSD1 inhibitors and uses thereof |
| WO2017013061A1 (en) | 2015-07-17 | 2017-01-26 | Oryzon Genomics, S.A. | Biomarkers associated with lsd1 inhibitors and uses thereof |
| MY189367A (en) | 2015-08-12 | 2022-02-08 | Incyte Corp | Salts of an lsd1 inhibitor |
| RU2018127657A (ru) | 2015-12-30 | 2020-01-31 | Новартис Аг | Виды терапии на основе иммуноэффекторных клеток с улучшенной эффективностью |
| ES3057783T3 (en) | 2016-03-15 | 2026-03-04 | Oryzon Genomics Sa | Combinations of lsd1 inhibitors for use in the treatment of neoplastic diseases |
| WO2017158136A1 (en) | 2016-03-16 | 2017-09-21 | Oryzon Genomics, S.A. | Methods to determine kdm1a target engagement and chemoprobes useful therefor |
| TWI833686B (zh) | 2016-04-22 | 2024-03-01 | 美商英塞特公司 | Lsd1 抑制劑之調配物 |
| EP3535414A1 (en) | 2016-11-03 | 2019-09-11 | Oryzon Genomics, S.A. | Pharmacodynamic biomarkers for personalized cancer care using epigenetic modifying agents |
| WO2018083189A1 (en) | 2016-11-03 | 2018-05-11 | Oryzon Genomics, S.A. | Biomarkers for determining responsiveness to lsd1 inhibitors |
| CN108727377A (zh) * | 2017-04-14 | 2018-11-02 | 四川大学 | 3-氰基吡唑并[1,5-a]嘧啶衍生物及其制备方法和用途 |
| FI3661510T3 (fi) | 2017-08-03 | 2024-12-18 | Oryzon Genomics Sa | Menetelmiä käyttäytymismuutosten hoitamiseksi |
| WO2019068326A1 (en) | 2017-10-05 | 2019-04-11 | Université D'aix-Marseille | INHIBITORS OF LSD1 FOR THE TREATMENT AND PREVENTION OF CARDIOMYOPATHIES |
| CN108689960B (zh) * | 2018-06-07 | 2022-03-04 | 济南大学 | 5-苯亚甲基-2-苯基噻唑酮类化合物及其制备和应用 |
| US10968200B2 (en) | 2018-08-31 | 2021-04-06 | Incyte Corporation | Salts of an LSD1 inhibitor and processes for preparing the same |
| US20220151999A1 (en) | 2019-03-20 | 2022-05-19 | Oryzon Genomics, S.A. | Methods of treating attention deficit hyperactivity disorder using kdm1a inhibitors such as the compound vafidemstat |
| LT3941466T (lt) | 2019-03-20 | 2026-02-25 | Oryzon Genomics, S.A. | Vafidemstatas ribinio asmenybės sutrikimo simptomų, nesusijusių su agresija, gydymui |
| CN114341366A (zh) | 2019-07-05 | 2022-04-12 | 奥莱松基因组股份有限公司 | 用于使用kdm1a抑制剂个体化治疗小细胞肺癌的生物标志物和方法 |
| CN110850104B (zh) * | 2020-01-15 | 2020-06-05 | 上海众启生物科技有限公司 | 用于阿尔兹海默症自身抗体检测的蛋白抗原组合及其应用 |
| EP3964204A1 (en) | 2020-09-08 | 2022-03-09 | Université d'Aix-Marseille | Lsd1 inhibitors for use in the treatment and prevention of fibrosis of tissues |
| US20250073232A1 (en) | 2021-04-08 | 2025-03-06 | Oryzon Genomics, S.A. | Combinations of lsd1 inhibitors for treating myeloid cancers |
| US20250295660A1 (en) | 2022-05-09 | 2025-09-25 | Oryzon Genomics, S.A. | Methods of treating nf1-mutant tumors using lsd1 inhibitors |
| EP4522136A1 (en) | 2022-05-09 | 2025-03-19 | Oryzon Genomics, S.A. | Methods of treating malignant peripheral nerve sheath tumor (mpnst) using lsd1 inhibitors |
| CN120529900A (zh) | 2022-11-24 | 2025-08-22 | 奥莱松基因组股份有限公司 | 用于治疗癌症的LSD1抑制剂和Menin抑制剂的组合 |
| CN116444437B (zh) * | 2023-03-08 | 2025-09-16 | 曲靖师范学院 | 抗癌医药达洛鲁胺的合成方法 |
| CN116813569B (zh) * | 2023-07-10 | 2024-07-02 | 衡阳市中心医院 | 一种抗癌药中间体的制备方法和抗癌药的制备方法 |
| WO2025188857A1 (en) * | 2024-03-05 | 2025-09-12 | University Of Florida Research Foundation, Incorporated | Hdac8 degraders and uses thereof |
Family Cites Families (9)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| BRPI0519794A2 (pt) * | 2005-01-07 | 2009-03-17 | Hoffmann La Roche | derivados de [4-(heteroaril)piperazin-1-il]-(fenil 2,5-substituìdo)metanona como inibidores de transportador de glicina 1 (glyt-1) para o tratamento de distúrbios neurológicos e neuropsiquiátricos |
| WO2006136008A1 (en) * | 2005-05-24 | 2006-12-28 | University Health Network | Salicylic acid hydrazones as inhibitors of the erk mapkinase pathway and for the treatment of cancer |
| WO2007008143A1 (en) * | 2005-07-08 | 2007-01-18 | Astrazeneca Ab | Heterocyclic sulfonamide derivatives as inhibitors of factor xa |
| WO2010083314A2 (en) * | 2009-01-14 | 2010-07-22 | Dow Agrosciences Llc | Fungicidal compositions including hydrazone derivatives and copper |
| WO2011058766A1 (en) * | 2009-11-16 | 2011-05-19 | Raqualia Pharma Inc. | Aryl carboxamide derivatives as ttx-s blockers |
| US20110189306A1 (en) * | 2010-01-13 | 2011-08-04 | Norbert Kartner | COMPOUNDS, COMPOSITIONS AND TREATMENTS FOR V-ATPase RELATED DISEASES |
| JP2014500254A (ja) * | 2010-11-09 | 2014-01-09 | セルゾーム リミティッド | Ｔｙｋ２阻害剤としてのピリジン化合物およびそのアザ類似体 |
| SI2744330T1 (sl) * | 2011-08-15 | 2020-11-30 | University Of Utah Research Foundation | Substituirani (E)-N'-(1-feniletiliden) benzohidrazidni analogi kot inhibitorji histon-demetilaze |
| BR112015032113B1 (pt) * | 2013-06-19 | 2019-01-29 | University Of Utah Research Foundation | análogos de (e)-n’-(1-feniletilideno)benzohidrazida substituídos como inibidores de histona demetilase |
-
2014
- 2014-06-19 BR BR112015032113-5A patent/BR112015032113B1/pt not_active IP Right Cessation
- 2014-06-19 WO PCT/US2014/043179 patent/WO2014205213A1/en not_active Ceased
- 2014-06-19 AU AU2014281398A patent/AU2014281398B2/en not_active Ceased
- 2014-06-19 SG SG11201510376QA patent/SG11201510376QA/en unknown
- 2014-06-19 SG SG10201710543PA patent/SG10201710543PA/en unknown
- 2014-06-19 CN CN201910116764.XA patent/CN110015984A/zh active Pending
- 2014-06-19 JP JP2016521574A patent/JP6525162B2/ja not_active Expired - Fee Related
- 2014-06-19 MX MX2015018032A patent/MX366949B/es active IP Right Grant
- 2014-06-19 CA CA2915817A patent/CA2915817C/en active Active
- 2014-06-19 EP EP14813387.9A patent/EP3010915B1/en not_active Not-in-force
- 2014-06-19 KR KR1020167001538A patent/KR102288648B1/ko not_active Expired - Fee Related
- 2014-06-19 CN CN201480045891.0A patent/CN105555784B/zh not_active Expired - Fee Related
- 2014-06-19 NZ NZ71533114A patent/NZ715331A/en not_active IP Right Cessation
- 2014-06-19 ES ES14813387T patent/ES2739814T3/es active Active
-
2015
- 2015-12-17 IL IL243200A patent/IL243200B/en active IP Right Grant
Also Published As
| Publication number | Publication date |
|---|---|
| JP2016523256A (ja) | 2016-08-08 |
| IL243200A0 (en) | 2016-02-29 |
| AU2014281398B2 (en) | 2018-10-04 |
| EP3010915B1 (en) | 2019-05-08 |
| WO2014205213A1 (en) | 2014-12-24 |
| CN105555784A (zh) | 2016-05-04 |
| JP6525162B2 (ja) | 2019-06-05 |
| CN105555784B (zh) | 2019-03-15 |
| MX366949B (es) | 2019-07-30 |
| NZ715331A (en) | 2019-09-27 |
| BR112015032113A2 (pt) | 2017-03-21 |
| CA2915817C (en) | 2022-12-13 |
| IL243200B (en) | 2020-10-29 |
| ES2739814T3 (es) | 2020-02-04 |
| MX2015018032A (es) | 2016-10-03 |
| CN110015984A (zh) | 2019-07-16 |
| EP3010915A1 (en) | 2016-04-27 |
| SG10201710543PA (en) | 2018-02-27 |
| EP3010915A4 (en) | 2016-12-28 |
| AU2014281398A1 (en) | 2016-01-21 |
| KR20160024929A (ko) | 2016-03-07 |
| CA2915817A1 (en) | 2014-12-24 |
| SG11201510376QA (en) | 2016-01-28 |
| KR102288648B1 (ko) | 2021-08-12 |
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| B65X | Notification of requirement for priority examination of patent application | ||
| B65Y | Grant of priority examination of the patent application (request complies with dec. 132/06 of 20061117) | ||
| B07D | Technical examination (opinion) related to article 229 of industrial property law [chapter 7.4 patent gazette] | ||
| B07E | Notification of approval relating to section 229 industrial property law [chapter 7.5 patent gazette] | ||
| B07A | Application suspended after technical examination (opinion) [chapter 7.1 patent gazette] | ||
| B09A | Decision: intention to grant [chapter 9.1 patent gazette] | ||
| B09X | Republication of the decision to grant [chapter 9.1.3 patent gazette] | ||
| B16A | Patent or certificate of addition of invention granted [chapter 16.1 patent gazette] |
Free format text: PRAZO DE VALIDADE: 20 (VINTE) ANOS CONTADOS A PARTIR DE 19/06/2014, OBSERVADAS AS CONDICOES LEGAIS. |
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| B21F | Lapse acc. art. 78, item iv - on non-payment of the annual fees in time |
Free format text: REFERENTE A 11A ANUIDADE. |
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| B24J | Lapse because of non-payment of annual fees (definitively: art 78 iv lpi, resolution 113/2013 art. 12) |
Free format text: EM VIRTUDE DA EXTINCAO PUBLICADA NA RPI 2832 DE 15-04-2025 E CONSIDERANDO AUSENCIA DE MANIFESTACAO DENTRO DOS PRAZOS LEGAIS, INFORMO QUE CABE SER MANTIDA A EXTINCAO DA PATENTE E SEUS CERTIFICADOS, CONFORME O DISPOSTO NO ARTIGO 12, DA RESOLUCAO 113/2013. |