ATE540021T1 - Hydroxansäurederivate als inhibitoren der enzymatischen hdac-aktivität - Google Patents
Hydroxansäurederivate als inhibitoren der enzymatischen hdac-aktivitätInfo
- Publication number
- ATE540021T1 ATE540021T1 AT06726980T AT06726980T ATE540021T1 AT E540021 T1 ATE540021 T1 AT E540021T1 AT 06726980 T AT06726980 T AT 06726980T AT 06726980 T AT06726980 T AT 06726980T AT E540021 T1 ATE540021 T1 AT E540021T1
- Authority
- AT
- Austria
- Prior art keywords
- alkyl
- ring
- optionally substituted
- heteroaryl
- aryl
- Prior art date
Links
- 102000003964 Histone deacetylase Human genes 0.000 title abstract 2
- 108090000353 Histone deacetylase Proteins 0.000 title abstract 2
- 230000000694 effects Effects 0.000 title abstract 2
- 239000003112 inhibitor Substances 0.000 title abstract 2
- 239000002253 acid Substances 0.000 title 1
- 230000002255 enzymatic effect Effects 0.000 title 1
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 abstract 4
- 125000003118 aryl group Chemical group 0.000 abstract 4
- 125000001072 heteroaryl group Chemical group 0.000 abstract 4
- 229910052739 hydrogen Inorganic materials 0.000 abstract 4
- 239000001257 hydrogen Substances 0.000 abstract 4
- 125000000623 heterocyclic group Chemical group 0.000 abstract 3
- 125000006413 ring segment Chemical group 0.000 abstract 3
- IJGRMHOSHXDMSA-UHFFFAOYSA-N Atomic nitrogen Chemical compound N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 abstract 2
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 abstract 2
- 101100490437 Mus musculus Acvrl1 gene Proteins 0.000 abstract 2
- 125000002843 carboxylic acid group Chemical group 0.000 abstract 2
- 125000004435 hydrogen atom Chemical group [H]* 0.000 abstract 2
- -1 C3-C7cycloalkyl Chemical group 0.000 abstract 1
- OKTJSMMVPCPJKN-UHFFFAOYSA-N Carbon Chemical compound [C] OKTJSMMVPCPJKN-UHFFFAOYSA-N 0.000 abstract 1
- 102000013392 Carboxylesterase Human genes 0.000 abstract 1
- 108010051152 Carboxylesterase Proteins 0.000 abstract 1
- 206010028980 Neoplasm Diseases 0.000 abstract 1
- 125000002837 carbocyclic group Chemical group 0.000 abstract 1
- 229910052799 carbon Inorganic materials 0.000 abstract 1
- 125000003178 carboxy group Chemical group [H]OC(*)=O 0.000 abstract 1
- 150000001875 compounds Chemical class 0.000 abstract 1
- 125000000753 cycloalkyl group Chemical group 0.000 abstract 1
- 125000004185 ester group Chemical group 0.000 abstract 1
- 230000003834 intracellular effect Effects 0.000 abstract 1
- 125000002950 monocyclic group Chemical group 0.000 abstract 1
- 229910052757 nitrogen Inorganic materials 0.000 abstract 1
- 125000000165 tricyclic carbocycle group Chemical group 0.000 abstract 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C259/00—Compounds containing carboxyl groups, an oxygen atom of a carboxyl group being replaced by a nitrogen atom, this nitrogen atom being further bound to an oxygen atom and not being part of nitro or nitroso groups
- C07C259/04—Compounds containing carboxyl groups, an oxygen atom of a carboxyl group being replaced by a nitrogen atom, this nitrogen atom being further bound to an oxygen atom and not being part of nitro or nitroso groups without replacement of the other oxygen atom of the carboxyl group, e.g. hydroxamic acids
- C07C259/06—Compounds containing carboxyl groups, an oxygen atom of a carboxyl group being replaced by a nitrogen atom, this nitrogen atom being further bound to an oxygen atom and not being part of nitro or nitroso groups without replacement of the other oxygen atom of the carboxyl group, e.g. hydroxamic acids having carbon atoms of hydroxamic groups bound to hydrogen atoms or to acyclic carbon atoms
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D333/00—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom
- C07D333/50—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom condensed with carbocyclic rings or ring systems
- C07D333/52—Benzo[b]thiophenes; Hydrogenated benzo[b]thiophenes
- C07D333/62—Benzo[b]thiophenes; Hydrogenated benzo[b]thiophenes 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 carbon atoms of the hetero ring
- C07D333/68—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen
- C07D333/70—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen attached in position 2
Landscapes
- Organic Chemistry (AREA)
- Chemical & Material Sciences (AREA)
- Health & Medical Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Public Health (AREA)
- Medicinal Chemistry (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Biomedical Technology (AREA)
- Neurology (AREA)
- Neurosurgery (AREA)
- Pain & Pain Management (AREA)
- Rheumatology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Medicines Containing Material From Animals Or Micro-Organisms (AREA)
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| GBGB0509225.9A GB0509225D0 (en) | 2005-05-05 | 2005-05-05 | Inhibitors of enzymatic activity |
| PCT/GB2006/001602 WO2006117548A1 (en) | 2005-05-05 | 2006-05-04 | Hydroxamic acid dervicatives as inhibitors of hdac enzymatic activity |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| ATE540021T1 true ATE540021T1 (de) | 2012-01-15 |
Family
ID=34685157
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| AT06726980T ATE540021T1 (de) | 2005-05-05 | 2006-05-04 | Hydroxansäurederivate als inhibitoren der enzymatischen hdac-aktivität |
Country Status (5)
| Country | Link |
|---|---|
| US (1) | US7973181B2 (de) |
| EP (1) | EP1877366B1 (de) |
| AT (1) | ATE540021T1 (de) |
| GB (1) | GB0509225D0 (de) |
| WO (1) | WO2006117548A1 (de) |
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| CA2596210C (en) | 2005-02-03 | 2014-07-08 | Topotarget Uk Limited | Combination therapies using hdac inhibitors |
| CA2607020C (en) * | 2005-05-05 | 2015-01-13 | Chroma Therapeutics Ltd. | Alpha amino acid ester-drug conjugates hydrolysable by carboxylesterases |
| US8835501B2 (en) * | 2005-05-13 | 2014-09-16 | Topotarget Uk Limited | Pharmaceutical formulations of HDAC inhibitors |
| WO2007054719A2 (en) | 2005-11-10 | 2007-05-18 | Topotarget Uk Limited | Histone deacetylase (hdac) inhibitors (pxdlol) for the treatment of cancer alone or in combination with chemotherapeutic agent |
| GB0619753D0 (en) | 2006-10-06 | 2006-11-15 | Chroma Therapeutics Ltd | Enzyme inhibitors |
| ES2509342T3 (es) | 2006-10-30 | 2014-10-17 | Chroma Therapeutics Limited | Hidroxamatos como inhibidores de histona desacetilasa |
| CN101583599A (zh) * | 2006-12-15 | 2009-11-18 | 安斯泰来制药有限公司 | N-羟基丙烯酰胺化合物 |
| WO2009040517A2 (en) * | 2007-09-25 | 2009-04-02 | Topotarget Uk Limited | Methods of synthesis of certain hydroxamic acid compounds |
| US8716308B2 (en) | 2008-01-11 | 2014-05-06 | Albany Molecular Research, Inc. | (1-azinone)-substituted pyridoindoles |
| GB0803747D0 (en) | 2008-02-29 | 2008-04-09 | Martin | Enzyme and receptor modulation |
| EP2262493B1 (de) * | 2008-03-07 | 2015-02-25 | Topotarget A/S | Behandlungsverfahren mit längerer kontinuierlicher infusion von belinostat |
| WO2009117808A1 (en) * | 2008-03-25 | 2009-10-01 | Methylgene Inc. | Inhibitors of histone deacetylase |
| GB0900555D0 (en) * | 2009-01-14 | 2009-02-11 | Topotarget As | New methods |
| GB0903480D0 (en) | 2009-02-27 | 2009-04-08 | Chroma Therapeutics Ltd | Enzyme Inhibitors |
| US8629158B2 (en) | 2009-07-01 | 2014-01-14 | Albany Molecular Research, Inc. | Azabicycloalkane-indole and azabicycloalkane-pyrrolo-pyridine MCH-1 antagonists, methods of making, and use thereof |
| US9073925B2 (en) | 2009-07-01 | 2015-07-07 | Albany Molecular Research, Inc. | Azinone-substituted azabicycloalkane-indole and azabicycloalkane-pyrrolo-pyridine MCH-1 antagonists, methods of making, and use thereof |
| WO2011003005A1 (en) | 2009-07-01 | 2011-01-06 | Albany Molecular Research, Inc. | Azinone-substituted azepino[b]indole and pyrido-pyrrolo-azepine mch-1 antagonists, methods of making, and use thereof |
| WO2011003012A1 (en) | 2009-07-01 | 2011-01-06 | Albany Molecular Research, Inc. | Azinone-substituted azapolycycle mch-1 antagonists, methods of making, and use thereof |
| WO2011113013A2 (en) | 2010-03-11 | 2011-09-15 | Hemaquest Pharmaceuticals, Inc. | Methods and compositions for treating viral or virally-induced conditions |
| CA2800143A1 (en) * | 2010-05-21 | 2011-11-24 | The Trustees Of Columbia University In The City Of New York | Selective hdac inhibitors |
| WO2012088038A2 (en) | 2010-12-21 | 2012-06-28 | Albany Molecular Research, Inc. | Piperazinone-substituted tetrahydro-carboline mch-1 antagonists, methods of making, and uses thereof |
| US8993765B2 (en) | 2010-12-21 | 2015-03-31 | Albany Molecular Research, Inc. | Tetrahydro-azacarboline MCH-1 antagonists, methods of making, and uses thereof |
| WO2013052110A1 (en) | 2011-10-03 | 2013-04-11 | The Trustees Of Columbia University In The City Of New York | Novel molecules that selectively inhibit histone deacetylase 6 relative to histone deacetylase 1 |
| US20150141470A1 (en) | 2012-05-08 | 2015-05-21 | The Broad Institute, Inc. | Diagnostic and treatment methods in patients having or at risk of developing resistance to cancer therapy |
| GB201211310D0 (en) | 2012-06-26 | 2012-08-08 | Chroma Therapeutics Ltd | CSF-1R kinase inhibitors |
| DK3222616T3 (da) | 2012-10-17 | 2019-08-19 | Macrophage Pharma Ltd | N-[2-{4-[6-amino-5-(2,4-difluorbenzoyl)-2-oxopyridin-1(2H)-yl]-3,5-difluorphenyl}ethyl]-L-alanin og terbutylester deraf |
| CA2933907A1 (en) | 2013-12-23 | 2015-07-02 | The Trustees Of Columbia University In The City Of New York | Selective hdac6 inhibitors |
| WO2017216297A1 (en) | 2016-06-16 | 2017-12-21 | Glaxosmithkline Intellectual Property Development Limited | Dosage regimen |
| EP3484489B1 (de) | 2016-07-15 | 2025-06-18 | Viracta Subsidiary, Inc. | Hdac-hemmer zur verwendung mit therapien auf der basis von nk-zellen |
| GB201713975D0 (en) | 2017-08-31 | 2017-10-18 | Macrophage Pharma Ltd | Medical use |
| CN108084178B (zh) * | 2018-01-04 | 2020-09-01 | 济南大学 | 一类含有四氢-β-咔碄结构的异羟肟酸类化合物的用途 |
| CA3142142A1 (en) | 2019-05-31 | 2020-12-03 | Viracta Subsidiary, Inc. | Methods of treating virally associated cancers with histone deacetylase inhibitors |
| JP7744024B2 (ja) * | 2019-10-03 | 2025-09-25 | テナヤ セラピューティクス， インコーポレイテッド | ５－フルオロニコチンアミド誘導体およびその使用 |
| PH12022551475A1 (en) | 2019-12-20 | 2023-11-29 | Tenaya Therapeutics Inc | Fluoroalkyl-oxadiazoles and uses thereof |
| CN114539110B (zh) * | 2020-11-26 | 2023-02-14 | 东南大学 | 含有ras/raf蛋白干扰基团的hdac抑制剂及其制备方法 |
| CA3216768A1 (en) | 2021-05-04 | 2022-11-10 | Jin Yang | 2-fluoroalkyl-1,3,4-oxadiazol-5-yl-thiazol, hdac6 inhibitors for use in the treatment of metabolic disease and hfpef |
| CN117412950A (zh) * | 2021-06-17 | 2024-01-16 | 钱德拉塞卡·达亚尔·穆达利亚尔 | 用于制备l-草铵膦的中间体的方法 |
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| IT1099355B (it) | 1978-10-12 | 1985-09-18 | Sclavo Inst Sieroterapeut | Composizione adatta alla determinazione in cinetica del glucosio |
| AU650953B2 (en) | 1991-03-21 | 1994-07-07 | Novartis Ag | Inhaler |
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| KR20020059393A (ko) | 1999-09-08 | 2002-07-12 | 제임스 에스. 쿼크 | 새로운 부류의 세포분화제 및 히스톤 데아세틸라아제, 및이의 사용 방법 |
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| GB0003476D0 (en) | 2000-02-16 | 2000-04-05 | British Biotech Pharm | Acetal Hydroxylamine compounds |
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| PE20020354A1 (es) | 2000-09-01 | 2002-06-12 | Novartis Ag | Compuestos de hidroxamato como inhibidores de histona-desacetilasa (hda) |
| GB0023983D0 (en) | 2000-09-29 | 2000-11-15 | Prolifix Ltd | Therapeutic compounds |
| ATE430567T1 (de) | 2000-09-29 | 2009-05-15 | Topotarget Uk Ltd | Carbaminsäurederivate enthaltend eine amidgruppe zur behandlung von malaria |
| EP2292593A3 (de) | 2000-09-29 | 2011-05-25 | TopoTarget UK Limited | Carbamidsäureverbindungen mit einer Sulfonamid enthaltenden Verkettung als HDAC Inhibitoren |
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| WO2002090534A1 (en) * | 2001-05-02 | 2002-11-14 | The Regents Of The University Of California | Method for treating neurodegenerative, psychiatric and other disorders with deacetylase inhibitors |
| US6784173B2 (en) | 2001-06-15 | 2004-08-31 | Hoffmann-La Roche Inc. | Aromatic dicarboxylic acid derivatives |
| WO2003066579A2 (en) | 2002-02-07 | 2003-08-14 | Axys Pharmaceuticals | Novel bicyclic hydroxamates as inhibitors of histone deacetylase |
| EP1482962A4 (de) | 2002-02-15 | 2009-12-23 | Sloan Kettering Inst Cancer | Verfahren zur behandlung von trx-vermittelten erkrankungen |
| ATE395343T1 (de) | 2002-03-13 | 2008-05-15 | Janssen Pharmaceutica Nv | Sulfonylderivate als histone-deacetylase- inhibitoren |
| BR0307607A (pt) | 2002-03-13 | 2004-12-21 | Janssen Pharmaceutica Nv | Derivados de carbonilamino como inibidores de histona desacetilase |
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| MY140390A (en) | 2002-03-13 | 2009-12-31 | Janssen Pharmaceutica Nv | Sulfonylamino-derivatives as novel inhibitors of histone deacetylase |
| ES2309313T3 (es) | 2002-04-03 | 2008-12-16 | Topotarget Uk Limited | Compuestos del acido carbamico que comprenden un acoplamiento de piperacina como hdac inhibidores. |
| TWI319387B (en) | 2002-04-05 | 2010-01-11 | Astrazeneca Ab | Benzamide derivatives |
| GB0209715D0 (en) | 2002-04-27 | 2002-06-05 | Astrazeneca Ab | Chemical compounds |
| RU2005105696A (ru) | 2002-08-02 | 2005-11-10 | Арджента Дискавери Лимитед (Gb) | Замещенные тиенилгидроксамовые кислоты в качестве ингибиторов гистондеацетилазы |
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| DK1611088T3 (da) | 2003-04-07 | 2009-10-19 | Pharmacyclics Inc | Hydroxymater som terapeutiske midler |
| WO2004110989A1 (en) | 2003-05-14 | 2004-12-23 | Bayer Pharmaceuticals Corporation | N-hydroxy-7-(arylamino)heptanamide derivatives useful for treating hyper-proliferative disorders |
| CA2531661C (en) | 2003-07-07 | 2013-03-12 | Georgetown University | Histone deacetylase inhibitors and methods of use thereof |
| WO2005004861A1 (en) | 2003-07-15 | 2005-01-20 | Korea Research Institute Of Bioscience And Biotechnology | A use of novel 2-oxo-heterocyclic compounds and the pharmaceutical compositions comprising the same |
| WO2005014588A1 (en) | 2003-08-01 | 2005-02-17 | Argenta Discovery Limited | Substituted thienyl-hydroxamic acids having histone deacetylase activity |
| JP2007501775A (ja) | 2003-08-07 | 2007-02-01 | ノバルティス アクチエンゲゼルシャフト | 免疫抑制剤としてのヒストンデアセチラーゼ阻害剤 |
| BRPI0410727A (pt) | 2003-08-20 | 2006-06-20 | Axys Pharm Inc | composto, composição farmacêutica, e, uso de um composto |
| PT1663194E (pt) | 2003-08-26 | 2010-07-06 | Merck Hdac Res Llc | Utilizaão de saha para o tratamento de mesotelioma |
| US7781595B2 (en) | 2003-09-22 | 2010-08-24 | S*Bio Pte Ltd. | Benzimidazole derivatives: preparation and pharmaceutical applications |
| AU2004276337B2 (en) | 2003-09-24 | 2009-11-12 | Methylgene Inc. | Inhibitors of histone deacetylase |
| CA2542096A1 (en) | 2003-10-09 | 2005-04-21 | Aton Pharma, Inc. | Thiophene and benzothiophene hydroxamic acid derivatives |
| GB0509223D0 (en) * | 2005-05-05 | 2005-06-15 | Chroma Therapeutics Ltd | Enzyme inhibitors |
| GB0619753D0 (en) * | 2006-10-06 | 2006-11-15 | Chroma Therapeutics Ltd | Enzyme inhibitors |
-
2005
- 2005-05-05 GB GBGB0509225.9A patent/GB0509225D0/en not_active Ceased
-
2006
- 2006-05-04 AT AT06726980T patent/ATE540021T1/de active
- 2006-05-04 EP EP06726980A patent/EP1877366B1/de not_active Not-in-force
- 2006-05-04 US US11/919,048 patent/US7973181B2/en active Active
- 2006-05-04 WO PCT/GB2006/001602 patent/WO2006117548A1/en not_active Ceased
Also Published As
| Publication number | Publication date |
|---|---|
| GB0509225D0 (en) | 2005-06-15 |
| US7973181B2 (en) | 2011-07-05 |
| EP1877366B1 (de) | 2012-01-04 |
| WO2006117548A1 (en) | 2006-11-09 |
| US20090298924A1 (en) | 2009-12-03 |
| EP1877366A1 (de) | 2008-01-16 |
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