AR105812A1 - Métodos para la preparación de inhibidores de proteína deacetilasa - Google Patents
Métodos para la preparación de inhibidores de proteína deacetilasaInfo
- Publication number
- AR105812A1 AR105812A1 ARP160101701A ARP160101701A AR105812A1 AR 105812 A1 AR105812 A1 AR 105812A1 AR P160101701 A ARP160101701 A AR P160101701A AR P160101701 A ARP160101701 A AR P160101701A AR 105812 A1 AR105812 A1 AR 105812A1
- Authority
- AR
- Argentina
- Prior art keywords
- compound
- formula
- preparation
- deacetilase
- inhibitors
- Prior art date
Links
- 238000000034 method Methods 0.000 title abstract 2
- 239000003112 inhibitor Substances 0.000 title 1
- 102000004169 proteins and genes Human genes 0.000 title 1
- 108090000623 proteins and genes Proteins 0.000 title 1
- 150000001875 compounds Chemical class 0.000 abstract 9
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 abstract 4
- 238000006243 chemical reaction Methods 0.000 abstract 2
- ZCYVEMRRCGMTRW-UHFFFAOYSA-N 7553-56-2 Chemical group [I] ZCYVEMRRCGMTRW-UHFFFAOYSA-N 0.000 abstract 1
- WKBOTKDWSSQWDR-UHFFFAOYSA-N Bromine atom Chemical group [Br] WKBOTKDWSSQWDR-UHFFFAOYSA-N 0.000 abstract 1
- ZAMOUSCENKQFHK-UHFFFAOYSA-N Chlorine atom Chemical group [Cl] ZAMOUSCENKQFHK-UHFFFAOYSA-N 0.000 abstract 1
- GDTBXPJZTBHREO-UHFFFAOYSA-N bromine Chemical group BrBr GDTBXPJZTBHREO-UHFFFAOYSA-N 0.000 abstract 1
- 229910052794 bromium Inorganic materials 0.000 abstract 1
- 229910052801 chlorine Inorganic materials 0.000 abstract 1
- 239000000460 chlorine Chemical group 0.000 abstract 1
- 229910052731 fluorine Inorganic materials 0.000 abstract 1
- 239000011737 fluorine Substances 0.000 abstract 1
- 125000001153 fluoro group Chemical group F* 0.000 abstract 1
- 229910052740 iodine Chemical group 0.000 abstract 1
- 239000011630 iodine Chemical group 0.000 abstract 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
- C07D239/02—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
- C07D239/24—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members
- C07D239/28—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more 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, directly attached to ring carbon atoms
- C07D239/32—One oxygen, sulfur or nitrogen atom
- C07D239/42—One nitrogen atom
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
- C07D239/02—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
- C07D239/24—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members
- C07D239/28—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more 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, directly attached to ring carbon atoms
- C07D239/30—Halogen atoms or nitro radicals
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Low-Molecular Organic Synthesis Reactions Using Catalysts (AREA)
- Preparation Of Compounds By Using Micro-Organisms (AREA)
- Peptides Or Proteins (AREA)
- Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
Abstract
Reivindicación 1: Un método para la preparación del compuesto de fórmula (1), que comprende los pasos de: la conversión del compuesto de fórmula (2) en el compuesto de fórmula (3); en el que X se selecciona de flúor, cloro, bromo y yodo; Z se selecciona del grupo que consiste en -CN y -CO₂R; y R es alquilo C₁₋₆; y la conversión del compuesto de fórmula (3) en el compuesto de fórmula (1). Reivindicación 20: Una composición que comprende un compuesto de fórmula (4); en la que Z se selecciona del grupo que consiste en CN y -CO₂R; y en la que R es alquilo C₁₋₆; y un compuesto de fórmula (5), en la que Z se selecciona del grupo que consiste en -CN y CO₂R; y en la que R es alquilo C₁₋₆. Reivindicación 24: Un compuesto que tiene la estructura de fórmula (6) en el que Z se selecciona del grupo que consiste en -CN y -CO₂R; y en el que R es alquilo C₁₋₆. Reivindicación 27: Una composición que comprende el compuesto de acuerdo con la reivindicación 24.
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201562172624P | 2015-06-08 | 2015-06-08 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| AR105812A1 true AR105812A1 (es) | 2017-11-15 |
Family
ID=56264043
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ARP160101701A AR105812A1 (es) | 2015-06-08 | 2016-06-08 | Métodos para la preparación de inhibidores de proteína deacetilasa |
Country Status (11)
| Country | Link |
|---|---|
| US (1) | US10144714B2 (es) |
| EP (1) | EP3303304B1 (es) |
| JP (1) | JP6873053B2 (es) |
| CN (1) | CN107922352B (es) |
| AR (1) | AR105812A1 (es) |
| AU (2) | AU2016276573A1 (es) |
| CA (1) | CA2988594C (es) |
| ES (1) | ES2769255T3 (es) |
| MX (1) | MX369349B (es) |
| TW (1) | TWI706937B (es) |
| WO (1) | WO2016200930A1 (es) |
Families Citing this family (7)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN105753739A (zh) | 2010-01-22 | 2016-07-13 | 埃斯泰隆制药公司 | 作为蛋白质去乙酰化酶抑制剂的反向酰胺化合物及其使用方法 |
| US9663825B2 (en) | 2012-04-19 | 2017-05-30 | Acetylon Pharmaceuticals, Inc. | Biomarkers to identify patients that will respond to treatment and treating such patients |
| AR104935A1 (es) | 2015-06-08 | 2017-08-23 | Acetylon Pharmaceuticals Inc | Formas cristalinas de un inhibidor de histona deacetilasa |
| WO2016200930A1 (en) | 2015-06-08 | 2016-12-15 | Acetylon Pharmaceuticals, Inc. | Methods of making protein deacetylase inhibitors |
| WO2017214565A1 (en) * | 2016-06-09 | 2017-12-14 | Dana-Farber Cancer Institute, Inc., | Methods of use and pharmaceutical combinations of hdac inhibitors with bet inhibitors |
| EP3496751B1 (en) | 2016-08-08 | 2022-10-19 | Acetylon Pharmaceuticals Inc. | Pharmaceutical combinations of histone deacetylase 6 inhibitors and cd20 inhibitory antibodies and uses thereof |
| WO2018098168A1 (en) | 2016-11-23 | 2018-05-31 | Acetylon Pharmaceuticals, Inc. | Pharmaceutical combinations comprising a histone deacetylase inhibitor and a programmed death-ligand 1 (pd-l1) inhibitor and methods of use thereof |
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| US6777217B1 (en) | 1996-03-26 | 2004-08-17 | President And Fellows Of Harvard College | Histone deacetylases, and uses related thereto |
| US20030129724A1 (en) | 2000-03-03 | 2003-07-10 | Grozinger Christina M. | Class II human histone deacetylases, and uses related thereto |
| WO2001070675A2 (en) | 2000-03-24 | 2001-09-27 | Methylgene, Inc. | Inhibitors of histone deacetylase |
| US20050119305A1 (en) | 2001-03-21 | 2005-06-02 | Masao Naka | Il-6 production inhibitors |
| US7244853B2 (en) | 2001-05-09 | 2007-07-17 | President And Fellows Of Harvard College | Dioxanes and uses thereof |
| MXPA04004177A (es) | 2001-11-01 | 2004-09-06 | Janssen Pharmaceutica Nv | Derivados de amida como inhibidores de la glicogeno cintasa cinasa 3-beta. |
| US7154002B1 (en) | 2002-10-08 | 2006-12-26 | Takeda San Diego, Inc. | Histone deacetylase inhibitors |
| JP2006520796A (ja) | 2003-03-17 | 2006-09-14 | タケダ サン ディエゴ インコーポレイテッド | ヒストンデアセチラーゼインヒビター |
| WO2005007091A2 (en) | 2003-07-07 | 2005-01-27 | Georgetown University | Histone deacetylase inhibitors and methods of use thereof |
| CN101010298A (zh) | 2004-04-05 | 2007-08-01 | 默克Hdac研究有限责任公司 | 组蛋白脱乙酰酶抑制剂前药 |
| CA2601706C (en) | 2005-03-22 | 2016-09-20 | Dana-Farber Cancer Institute, Inc. | Treatment of protein degradation disorders |
| WO2007022638A1 (en) | 2005-08-26 | 2007-03-01 | Methylgene Inc. | Benzodiazepine and benzopiperazine analog inhibitors of histone deacetylase |
| CN101400362B (zh) | 2006-02-14 | 2016-10-12 | 哈佛大学校长及研究员协会 | 双官能组蛋白去乙酰化酶抑制剂 |
| AU2007248656B2 (en) | 2006-05-03 | 2013-04-04 | Dana-Farber Cancer Institute, Inc. | Histone deacetylase and tubulin deacetylase inhibitors |
| WO2007144341A1 (en) | 2006-06-12 | 2007-12-21 | Vrije Universiteit Brussel | Differentiation of rat liver epithelial cells into hepatocyte-like cells |
| ES2288802B1 (es) | 2006-07-07 | 2008-12-16 | Universidad De Granada | Nuevos derivados de ftalimida como inhibidores de las histonas desacetilasas. |
| US7888361B2 (en) | 2006-09-11 | 2011-02-15 | Curis, Inc. | Tyrosine kinase inhibitors containing a zinc binding moiety |
| CN101951930A (zh) | 2008-02-19 | 2011-01-19 | 阿奈斯特药品株式会社 | 对身体功能的恢复有用的口服或经肠组合物 |
| WO2010011296A2 (en) | 2008-07-23 | 2010-01-28 | President And Fellows Of Harvard College | Deacetylase inhibitors and uses thereof |
| US8716326B2 (en) | 2009-05-15 | 2014-05-06 | Korea Research Institute Of Chemical Technology | Isoindolinone derivatives, preparation method thereof and a pharmaceutical composition comprising same |
| WO2011019393A2 (en) | 2009-08-11 | 2011-02-17 | President And Fellows Of Harvard College | Class- and isoform-specific hdac inhibitors and uses thereof |
| ES2609040T3 (es) * | 2009-12-17 | 2017-04-18 | Merck Sharp & Dohme Corp. | Aminopirimidinas como inhibidores de Syk |
| WO2011084991A2 (en) | 2010-01-08 | 2011-07-14 | President And Fellows Of Harvard College | Fluorinated hdac inhibitors and uses thereof |
| CN105753739A (zh) | 2010-01-22 | 2016-07-13 | 埃斯泰隆制药公司 | 作为蛋白质去乙酰化酶抑制剂的反向酰胺化合物及其使用方法 |
| WO2011146855A1 (en) | 2010-05-21 | 2011-11-24 | The Trustees Of Columbia University In The City Of New York | Selective hdac inhibitors |
| WO2012018499A2 (en) | 2010-08-05 | 2012-02-09 | Acetylon Pharmaceuticals | Specific regulation of cytokine levels by hdac6 inhibitors |
| CN107011270A (zh) | 2010-11-16 | 2017-08-04 | 阿塞蒂隆制药公司 | 作为蛋白质去乙酰化酶抑制剂的嘧啶羟基酰胺化合物和其使用方法 |
| JP6169076B2 (ja) | 2011-07-20 | 2017-07-26 | ザ ジェネラル ホスピタル コーポレイション | 骨疾患の処置のためのヒストン脱アセチル化酵素６選択的阻害剤 |
| US8841301B2 (en) | 2011-09-26 | 2014-09-23 | Bristol-Myers Squibb Company | Selective NR2B antagonists |
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| US9145412B2 (en) | 2012-11-02 | 2015-09-29 | Acetylon Pharmaceuticals, Inc. | Selective HDAC1 and HDAC2 inhibitors |
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| JP2016511237A (ja) | 2013-02-01 | 2016-04-14 | アセチロン ファーマシューティカルズ インコーポレイテッドＡｃｅｔｙｌｏｎ Ｐｈａｒｍａｃｅｕｔｉｃａｌｓ，Ｉｎｃ． | 選択的ｈｄａｃ３阻害剤 |
| EP3004141A4 (en) | 2013-06-03 | 2017-05-31 | Acetylon Pharmaceuticals, Inc. | Histone deacetylase ( hdac) biomarkers in multiple myeloma |
| JP2016531163A (ja) | 2013-09-20 | 2016-10-06 | アセチロン ファーマシューティカルズ インコーポレイテッドＡｃｅｔｙｌｏｎ Ｐｈａｒｍａｃｅｕｔｉｃａｌｓ，Ｉｎｃ． | Ｈｄａｃ６阻害物質を用いた、異常なリンパ球の機能に起因する疾患の治療 |
| US9403779B2 (en) | 2013-10-08 | 2016-08-02 | Acetylon Pharmaceuticals, Inc. | Combinations of histone deacetylase inhibitors and either Her2 inhibitors or PI3K inhibitors |
| JP2016536354A (ja) | 2013-10-10 | 2016-11-24 | アセチロン ファーマシューティカルズ インコーポレイテッドＡｃｅｔｙｌｏｎ Ｐｈａｒｍａｃｅｕｔｉｃａｌｓ，Ｉｎｃ． | 非ホジキンリンパ腫を治療するための、ｈｄａｃ阻害剤単独またはｂｔｋ阻害剤との組み合わせ |
| EP3054953B1 (en) | 2013-10-10 | 2020-07-01 | Acetylon Pharmaceuticals, Inc. | Hdac inhibitors in combination with pi3k inhibitors, for treating non-hodgkin's lymphoma |
| US9278963B2 (en) | 2013-10-10 | 2016-03-08 | Acetylon Pharmaceuticals, Inc. | Pyrimidine hydroxy amide compounds as histone deacetylase inhibitors |
| AU2014332147A1 (en) | 2013-10-11 | 2016-05-05 | Acetylon Pharmaceuticals, Inc. | Combinations of histone deactylase inhibitors and immunomodulatory drugs |
| US10660890B2 (en) | 2013-10-24 | 2020-05-26 | National Institutes Of Health (Nih), U.S. Dept. Of Health And Human Services (Dhhs), U.S. Government Nih Division Of Extramural Inventions And Technology Resources (Deitr) | Treatment of polycystic diseases with an HDAC6 inhibitor |
| BR112016012561A2 (pt) | 2013-12-03 | 2017-08-08 | Acetylon Pharmaceuticals Inc | Combinações de inibidores da histona desacetilase e fármacos imunomoduladores |
| EP3084446B1 (en) | 2013-12-20 | 2022-12-14 | Acetylon Pharmaceuticals, Inc. | Histone deacetylase 6 (hdac6) biomarkers in multiple myeloma |
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| US20150359794A1 (en) | 2014-06-13 | 2015-12-17 | Buck Institute For Research On Aging | Impairment of the large ribosomal subunit protein rpl24 by depletion or acetylation |
| JP6952602B2 (ja) | 2014-07-07 | 2021-10-20 | アセチロン ファーマシューティカルズ インコーポレイテッドＡｃｅｔｙｌｏｎ Ｐｈａｒｍａｃｅｕｔｉｃａｌｓ，Ｉｎｃ． | ヒストンデアセチラーゼ阻害剤による白血病の治療 |
| WO2016057779A2 (en) | 2014-10-08 | 2016-04-14 | Acetylon Pharmaceuticals, Inc. | Induction of gata2 by hdac1 and hdac2 inhibitors |
| WO2016090230A1 (en) | 2014-12-05 | 2016-06-09 | Acetylon Pharmaceuticals, Inc. | Pyrimidine hydroxy amide compounds for treating peripheral neuropathy |
| WO2016087950A1 (en) | 2014-12-05 | 2016-06-09 | University of Modena and Reggio Emilia | Combinations of histone deacetylase inhibitors and bendamustine for use in the treatment of lymphoma |
| SG11201704759QA (en) | 2014-12-12 | 2017-07-28 | Regenacy Pharmaceuticals Llc | Piperidine derivatives as hdac1/2 inhibitors |
| WO2016168647A1 (en) | 2015-04-17 | 2016-10-20 | Acetylon Pharmaceuticals Inc. | Treatment of neuroblastoma with histone deacetylase inhibotrs |
| US10272084B2 (en) | 2015-06-01 | 2019-04-30 | Regenacy Pharmaceuticals, Llc | Histone deacetylase 6 selective inhibitors for the treatment of cisplatin-induced peripheral neuropathy |
| AR104935A1 (es) | 2015-06-08 | 2017-08-23 | Acetylon Pharmaceuticals Inc | Formas cristalinas de un inhibidor de histona deacetilasa |
| WO2016200930A1 (en) | 2015-06-08 | 2016-12-15 | Acetylon Pharmaceuticals, Inc. | Methods of making protein deacetylase inhibitors |
| EP3496751B1 (en) | 2016-08-08 | 2022-10-19 | Acetylon Pharmaceuticals Inc. | Pharmaceutical combinations of histone deacetylase 6 inhibitors and cd20 inhibitory antibodies and uses thereof |
-
2016
- 2016-06-08 WO PCT/US2016/036434 patent/WO2016200930A1/en not_active Ceased
- 2016-06-08 MX MX2017015900A patent/MX369349B/es active IP Right Grant
- 2016-06-08 ES ES16732810T patent/ES2769255T3/es active Active
- 2016-06-08 CA CA2988594A patent/CA2988594C/en active Active
- 2016-06-08 AU AU2016276573A patent/AU2016276573A1/en not_active Abandoned
- 2016-06-08 AR ARP160101701A patent/AR105812A1/es unknown
- 2016-06-08 TW TW105118213A patent/TWI706937B/zh active
- 2016-06-08 EP EP16732810.3A patent/EP3303304B1/en active Active
- 2016-06-08 US US15/176,826 patent/US10144714B2/en active Active
- 2016-06-08 CN CN201680046553.8A patent/CN107922352B/zh active Active
- 2016-06-08 JP JP2017563541A patent/JP6873053B2/ja active Active
-
2020
- 2020-11-13 AU AU2020267299A patent/AU2020267299B2/en active Active
Also Published As
| Publication number | Publication date |
|---|---|
| AU2016276573A1 (en) | 2018-01-04 |
| TWI706937B (zh) | 2020-10-11 |
| ES2769255T3 (es) | 2020-06-25 |
| MX2017015900A (es) | 2018-11-09 |
| WO2016200930A9 (en) | 2017-02-23 |
| CN107922352B (zh) | 2021-08-06 |
| US20160355486A1 (en) | 2016-12-08 |
| CA2988594C (en) | 2023-08-15 |
| JP2018518486A (ja) | 2018-07-12 |
| EP3303304B1 (en) | 2019-11-20 |
| TW201718517A (zh) | 2017-06-01 |
| US10144714B2 (en) | 2018-12-04 |
| AU2020267299B2 (en) | 2022-07-07 |
| AU2020267299A1 (en) | 2020-12-10 |
| EP3303304A1 (en) | 2018-04-11 |
| WO2016200930A1 (en) | 2016-12-15 |
| MX369349B (es) | 2019-11-06 |
| CN107922352A (zh) | 2018-04-17 |
| CA2988594A1 (en) | 2016-12-15 |
| JP6873053B2 (ja) | 2021-05-19 |
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