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)
- Pain & Pain Management (AREA)
- Rheumatology (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Biomedical Technology (AREA)
- Neurology (AREA)
- Neurosurgery (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicines Containing Material From Animals Or Micro-Organisms (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (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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| EP2946810A1 (de) | 2005-02-03 | 2015-11-25 | TopoTarget UK Limited | Kombinationstherapie mit einem HDAC-Hemmer und Vincristin zur Behandlung von Krebs |
| EP1964577B1 (de) * | 2005-05-05 | 2016-04-13 | GlaxoSmithKline Intellectual Property Development Limited | Durch carboxylesterase hydrolysierbare alpha-aminosäureester-arzneikonjugate |
| CN102579417B (zh) | 2005-05-13 | 2014-11-26 | 托波塔吉特英国有限公司 | Hdac抑制剂的药物制剂 |
| EP2361619A1 (de) | 2005-11-10 | 2011-08-31 | TopoTarget UK Limited | Histone Deacetylase (hdac) Inhibitoren (pxd-101) zur Behandlung von hämatologischen Krebserkrankungen |
| GB0619753D0 (en) * | 2006-10-06 | 2006-11-15 | Chroma Therapeutics Ltd | Enzyme inhibitors |
| JP5043120B2 (ja) * | 2006-10-30 | 2012-10-10 | クロマ セラピューティクス リミテッド | ヒストンデアセチラーゼの阻害剤としてのヒドロキサメート |
| US20100069388A1 (en) * | 2006-12-15 | 2010-03-18 | Astellas Pharma Inc. | N-hydroxyacrylamide compounds |
| CA2700173C (en) * | 2007-09-25 | 2016-10-11 | Topotarget Uk Limited | Methods of synthesis of certain hydroxamic acid compounds |
| BRPI0907122B8 (pt) | 2008-01-11 | 2021-05-25 | Albany Molecular Res Inc | compostos de piridoindóis (1-azinona) substituídos, composição farmacêutica compreendendo os referidos compostos, e usos dos mesmos |
| GB0803747D0 (en) | 2008-02-29 | 2008-04-09 | Martin | Enzyme and receptor modulation |
| WO2009109861A1 (en) * | 2008-03-07 | 2009-09-11 | Topotarget A/S | Methods of treatment employing prolonged continuous infusion of 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 |
| 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 |
| WO2011003007A1 (en) | 2009-07-01 | 2011-01-06 | Albany Molecular Research, Inc. | Azabicycloalkane-indole and azabicycloalkane-pyrrolo-pyridine 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 |
| US8637501B2 (en) | 2009-07-01 | 2014-01-28 | Albany Molecular Research, Inc. | Azinone-substituted azepino[b]indole and pyrido-pyrrolo-azepine MCH-1 antagonists, methods of making, and use thereof |
| US20110245154A1 (en) | 2010-03-11 | 2011-10-06 | Hemaquest Pharmaceuticals, Inc. | Methods and Compositions for Treating Viral or Virally-Induced Conditions |
| EP2571352A4 (de) * | 2010-05-21 | 2014-09-17 | Sloan Kettering Inst Cancer | Selektive hdac-hemmer |
| 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 |
| WO2012088124A2 (en) | 2010-12-21 | 2012-06-28 | Albany Molecular Research, Inc. | Tetrahydro-azacarboline mch-1 antagonists, methods of making, and uses thereof |
| CA2850757A1 (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 |
| WO2013169858A1 (en) | 2012-05-08 | 2013-11-14 | 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 |
| CA2888928C (en) | 2012-10-17 | 2020-05-26 | Macrophage Pharma Limited | Tert-butyl n-[2-{4-[6-amino-5-(2,4-difluorobenzoyl)-2-oxopyridin-1(2h)-yl]-3,5- difluorophenyl}ethyl]-l-alaninate or a salt, hydrate or solvate thereof |
| 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 |
| JP7373991B2 (ja) | 2016-07-15 | 2023-11-06 | ビラクタ セラピューティクス，インク． | 免疫療法で使用するためのヒストン脱アセチル化酵素阻害剤 |
| 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 |
| MX2021014639A (es) | 2019-05-31 | 2022-04-06 | Viracta Subsidiary Inc | Metodos para tratar canceres asociados con virus con inhibidores de la histona deacetilasa. |
| WO2021067859A1 (en) * | 2019-10-03 | 2021-04-08 | Tenaya Therapeutics, Inc. | 5-fluoronicotinamide derivatives and uses thereof |
| CN114980887A (zh) | 2019-12-20 | 2022-08-30 | 特纳亚治疗股份有限公司 | 氟代烷基-噁二唑及其用途 |
| 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 |
| WO2022235842A1 (en) | 2021-05-04 | 2022-11-10 | Tenaya Therapeutics, Inc. | 2-fluoroalkyl-1,3,4-oxadiazol-5-yl-thiazol, hdac6 inhibitors for use in the treatment of metabolic disease and hfpef |
| WO2022264168A1 (en) * | 2021-06-17 | 2022-12-22 | Chandrasekhar Dayal Mudaliar | A process for preparation of an intermediate of l-glufosinate |
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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 |
| US5369108A (en) | 1991-10-04 | 1994-11-29 | Sloan-Kettering Institute For Cancer Research | Potent inducers of terminal differentiation and methods of use thereof |
| MXPA02002505A (es) | 1999-09-08 | 2004-09-10 | Sloan Kettering Inst Cancer | Nueva clase de agentes de citodiferenciacion e inhibidores de histona desacetilasa y metodos de utilizacion de los mismos. |
| CA2391952C (en) | 1999-11-23 | 2012-01-31 | Methylgene Inc. | Inhibitors of histone deacetylase |
| GB0003476D0 (en) | 2000-02-16 | 2000-04-05 | British Biotech Pharm | Acetal Hydroxylamine compounds |
| AU2001248701A1 (en) | 2000-03-24 | 2001-10-03 | Methylgene, Inc. | Inhibitors of histone deacetylase |
| PE20020354A1 (es) | 2000-09-01 | 2002-06-12 | Novartis Ag | Compuestos de hidroxamato como inhibidores de histona-desacetilasa (hda) |
| JP4975941B2 (ja) | 2000-09-29 | 2012-07-11 | トポターゲット ユーケー リミテッド | （ｅ）−ｎ−ヒドロキシ−３−（３−スルファモイル−フェニル）アクリルアミド化合物及びその治療用途 |
| GB0023983D0 (en) | 2000-09-29 | 2000-11-15 | Prolifix Ltd | Therapeutic compounds |
| WO2002026696A1 (en) | 2000-09-29 | 2002-04-04 | Prolifix Limited | Carbamic acid compounds comprising an amide linkage as hdac inhibitors |
| WO2002069947A2 (en) | 2001-01-12 | 2002-09-12 | Methylgene, Inc. | Antisense oligonucleotides and trichostatin analogue histone deacetylase-4 inhibitors against cancer |
| ES2310213T3 (es) * | 2001-05-02 | 2009-01-01 | The Regents Of The University Of California | Procedimiento para tratar trastornos neurodegenerativos, psiquiatricos y otros trastornos con inhibidores de desacetilasa. |
| US6784173B2 (en) | 2001-06-15 | 2004-08-31 | Hoffmann-La Roche Inc. | Aromatic dicarboxylic acid derivatives |
| WO2003066889A2 (en) | 2002-02-07 | 2003-08-14 | Axys Pharmaceuticals, Inc. | Assay for acytyltransferase or deacetylase activity |
| 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 |
| AU2003218737B2 (en) | 2002-03-13 | 2008-04-10 | Janssen Pharmaceutica N.V. | Inhibitors of histone deacetylase |
| ES2306880T3 (es) | 2002-03-13 | 2008-11-16 | Janssen Pharmaceutica Nv | Derivados de sulfonilamino como inhibidores novedosos de la histona desacetilasa. |
| CA2476067C (en) | 2002-03-13 | 2011-09-20 | Janssen Pharmaceutica N.V. | Carbonylamino-derivatives as novel inhibitors of histone deacetylase |
| BR0308908A (pt) | 2002-04-03 | 2005-01-04 | Topotarget Uk Ltd | Composto, composição, uso de um composto, e, métodos para inibir a hdac em uma célula, para o tratamento de uma condição mediada pela hdac, de um condição proliferativa, de câncer e de psorìase |
| TWI319387B (en) | 2002-04-05 | 2010-01-11 | Astrazeneca Ab | Benzamide derivatives |
| GB0209715D0 (en) | 2002-04-27 | 2002-06-05 | Astrazeneca Ab | Chemical compounds |
| JP2005539001A (ja) | 2002-08-02 | 2005-12-22 | アージェンタ・ディスカバリー・リミテッド | ヒストンデアセチラーゼインヒビターとしての置換チエニルヒドロキサム酸 |
| CA2504460A1 (en) | 2002-11-12 | 2004-05-27 | Peter G. Klimko | Histone deacetylase inhibitors for the treatment of ocular neovascular or edematous disorders and diseases |
| US7221775B2 (en) | 2002-11-12 | 2007-05-22 | Intellivid Corporation | Method and apparatus for computerized image background analysis |
| US7244751B2 (en) | 2003-02-14 | 2007-07-17 | Shenzhen Chipscreen Biosciences Ltd. | Histone deacetylase inhibitors of novel benzamide derivatives with potent differentiation and anti-proliferation activity |
| PL1611088T3 (pl) | 2003-04-07 | 2009-11-30 | Pharmacyclics Inc | Hydroksamiany jako środki terapeutyczne |
| WO2004110989A1 (en) | 2003-05-14 | 2004-12-23 | Bayer Pharmaceuticals Corporation | N-hydroxy-7-(arylamino)heptanamide derivatives useful for treating hyper-proliferative disorders |
| EP1644323B1 (de) | 2003-07-07 | 2015-03-18 | Georgetown University | Histondeacetylaseinhibitoren und verfahren zu deren anwendung |
| EP1663201A4 (de) | 2003-07-15 | 2009-10-28 | Korea Res Inst Of Bioscience | Verwendung von neuen 2-oxo-heterozyklischen verbindungen sowie diesen enthaltenden pharmazeutischen zubereitungen |
| WO2005014588A1 (en) | 2003-08-01 | 2005-02-17 | Argenta Discovery Limited | Substituted thienyl-hydroxamic acids having histone deacetylase activity |
| US20060270730A1 (en) | 2003-08-07 | 2006-11-30 | Andreas Katopodis | Histone deacetylase inhibitors as immunosuppressants |
| WO2005019174A1 (en) | 2003-08-20 | 2005-03-03 | Axys Pharmaceuticals, Inc. | Acetylene derivatives as inhibitors of histone deacetylase |
| EP1663194B1 (de) | 2003-08-26 | 2010-03-31 | Merck HDAC Research, LLC | Verwendung von SAHA zur Behandlung von Mesotheliom |
| KR101127201B1 (ko) | 2003-09-22 | 2012-04-12 | 에스*바이오 피티이 리미티드 | 벤즈이미다졸 유도체와 그의 제조방법 및 약학적 적용 |
| CA2539117A1 (en) | 2003-09-24 | 2005-04-07 | Methylgene Inc. | Inhibitors of histone deacetylase |
| US7935724B2 (en) | 2003-10-09 | 2011-05-03 | Merck Hdac Research, Llc | 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 WO PCT/GB2006/001602 patent/WO2006117548A1/en not_active Ceased
- 2006-05-04 US US11/919,048 patent/US7973181B2/en active Active
- 2006-05-04 AT AT06726980T patent/ATE540021T1/de active
- 2006-05-04 EP EP06726980A patent/EP1877366B1/de not_active Expired - Lifetime
Also Published As
| Publication number | Publication date |
|---|---|
| GB0509225D0 (en) | 2005-06-15 |
| US7973181B2 (en) | 2011-07-05 |
| EP1877366A1 (de) | 2008-01-16 |
| EP1877366B1 (de) | 2012-01-04 |
| US20090298924A1 (en) | 2009-12-03 |
| WO2006117548A1 (en) | 2006-11-09 |
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