ES2769255T3 - Métodos para fabricar inhibidores de la proteína desacetilasa - Google Patents
Métodos para fabricar inhibidores de la proteína desacetilasa Download PDFInfo
- Publication number
- ES2769255T3 ES2769255T3 ES16732810T ES16732810T ES2769255T3 ES 2769255 T3 ES2769255 T3 ES 2769255T3 ES 16732810 T ES16732810 T ES 16732810T ES 16732810 T ES16732810 T ES 16732810T ES 2769255 T3 ES2769255 T3 ES 2769255T3
- Authority
- ES
- Spain
- Prior art keywords
- compound
- converting
- acid
- particular embodiment
- mixture
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
- Active
Links
- 0 *=C(c1cnc(N(c2ccccc2)c(cccc2)c2Cl)nc1)NCCCCCCC(NO)=O Chemical compound *=C(c1cnc(N(c2ccccc2)c(cccc2)c2Cl)nc1)NCCCCCCC(NO)=O 0.000 description 7
- IEMKQRSOAOPKRJ-UHFFFAOYSA-N CCOC(c(cn1)cnc1Cl)=O Chemical compound CCOC(c(cn1)cnc1Cl)=O IEMKQRSOAOPKRJ-UHFFFAOYSA-N 0.000 description 1
- UNZANUODCGDKAV-UHFFFAOYSA-N CCOC(c1cnc(N(c2ccccc2)c(cccc2)c2Cl)nc1)=O Chemical compound CCOC(c1cnc(N(c2ccccc2)c(cccc2)c2Cl)nc1)=O UNZANUODCGDKAV-UHFFFAOYSA-N 0.000 description 1
- PBBZQYXRCHGAKJ-UHFFFAOYSA-N CCOC(c1cnc(N(c2ccccc2)c2cccc(Cl)c2)nc1)=O Chemical compound CCOC(c1cnc(N(c2ccccc2)c2cccc(Cl)c2)nc1)=O PBBZQYXRCHGAKJ-UHFFFAOYSA-N 0.000 description 1
- ZUKQDXJKYIIHBW-UHFFFAOYSA-N CCOC(c1cnc(N(c2ccccc2)c2ccccc2)nc1)=O Chemical compound CCOC(c1cnc(N(c2ccccc2)c2ccccc2)nc1)=O ZUKQDXJKYIIHBW-UHFFFAOYSA-N 0.000 description 1
- ZGDNUSLFBDDDJT-UHFFFAOYSA-N CCOC(c1cnc(Nc2ccccc2Cl)nc1)=O Chemical compound CCOC(c1cnc(Nc2ccccc2Cl)nc1)=O ZGDNUSLFBDDDJT-UHFFFAOYSA-N 0.000 description 1
- VGJWPMYIXKPLJU-UHFFFAOYSA-N COC(CCCCCCNC(c1cnc(N(c2ccccc2)c(cccc2)c2Cl)nc1)=O)=O Chemical compound COC(CCCCCCNC(c1cnc(N(c2ccccc2)c(cccc2)c2Cl)nc1)=O)=O VGJWPMYIXKPLJU-UHFFFAOYSA-N 0.000 description 1
- KVCUEYZPPXIXMV-UHFFFAOYSA-N OC(c1cnc(N(c2ccccc2)c(cccc2)c2Cl)nc1)=O Chemical compound OC(c1cnc(N(c2ccccc2)c(cccc2)c2Cl)nc1)=O KVCUEYZPPXIXMV-UHFFFAOYSA-N 0.000 description 1
- VLIUIBXPEDFJRF-UHFFFAOYSA-N ONC(CCCCCCNC(c1cnc(N(c2ccccc2)c(cccc2)c2Cl)nc1)=O)=O Chemical compound ONC(CCCCCCNC(c1cnc(N(c2ccccc2)c(cccc2)c2Cl)nc1)=O)=O VLIUIBXPEDFJRF-UHFFFAOYSA-N 0.000 description 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)
- Peptides Or Proteins (AREA)
- Preparation Of Compounds By Using Micro-Organisms (AREA)
- Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201562172624P | 2015-06-08 | 2015-06-08 | |
| PCT/US2016/036434 WO2016200930A1 (en) | 2015-06-08 | 2016-06-08 | Methods of making protein deacetylase inhibitors |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| ES2769255T3 true ES2769255T3 (es) | 2020-06-25 |
Family
ID=56264043
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ES16732810T Active ES2769255T3 (es) | 2015-06-08 | 2016-06-08 | Métodos para fabricar inhibidores de la proteína desacetilasa |
Country Status (11)
| Country | Link |
|---|---|
| US (1) | US10144714B2 (enExample) |
| EP (1) | EP3303304B1 (enExample) |
| JP (1) | JP6873053B2 (enExample) |
| CN (1) | CN107922352B (enExample) |
| AR (1) | AR105812A1 (enExample) |
| AU (2) | AU2016276573A1 (enExample) |
| CA (1) | CA2988594C (enExample) |
| ES (1) | ES2769255T3 (enExample) |
| MX (1) | MX369349B (enExample) |
| TW (1) | TWI706937B (enExample) |
| WO (1) | WO2016200930A1 (enExample) |
Families Citing this family (7)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| TW201735926A (zh) | 2010-01-22 | 2017-10-16 | 艾斯特隆製藥公司 | 作為蛋白質去乙醯酶抑制劑之反式醯胺化合物及其使用方法 |
| EP2839037B1 (en) | 2012-04-19 | 2018-12-26 | Acetylon Pharmaceuticals, Inc. | Biomarkers to identify patients that will respond to treatment and treating such patients |
| TW201718516A (zh) | 2015-06-08 | 2017-06-01 | 艾斯特隆製藥公司 | 組蛋白去乙醯酶抑制劑之晶形 |
| TWI706937B (zh) | 2015-06-08 | 2020-10-11 | 美商艾斯特隆製藥公司 | 製備蛋白質去乙醯酶抑制劑之方法 |
| EP3468559B1 (en) * | 2016-06-09 | 2023-11-22 | Dana Farber Cancer Institute, Inc. | Methods of use and pharmaceutical combinations of hdac inhibitors with bet inhibitors |
| US11324744B2 (en) | 2016-08-08 | 2022-05-10 | Acetylon Pharmaceuticals Inc. | Methods of use and pharmaceutical combinations of histone deacetylase inhibitors and CD20 inhibitory antibodies |
| 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 |
Family Cites Families (57)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| 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 |
| CA2404002A1 (en) | 2000-03-24 | 2001-09-27 | Methylgene, Inc. | Inhibitors of histone deacetylase |
| JPWO2002074298A1 (ja) | 2001-03-21 | 2004-07-08 | 小野薬品工業株式会社 | Ｉｌ−６産生阻害剤 |
| US7244853B2 (en) | 2001-05-09 | 2007-07-17 | President And Fellows Of Harvard College | Dioxanes and uses thereof |
| US7183288B2 (en) | 2001-11-01 | 2007-02-27 | Herwig Josephus Margareta Janssen, legal representative | Amide derivatives as glycogen synthase kinase 3-β inhibitors |
| US7154002B1 (en) | 2002-10-08 | 2006-12-26 | Takeda San Diego, Inc. | Histone deacetylase inhibitors |
| US7375228B2 (en) | 2003-03-17 | 2008-05-20 | Takeda San Diego, Inc. | Histone deacetylase inhibitors |
| WO2005007091A2 (en) | 2003-07-07 | 2005-01-27 | Georgetown University | Histone deacetylase inhibitors and methods of use thereof |
| US8227636B2 (en) | 2004-04-05 | 2012-07-24 | Merck Hdac Research, Llc | Histone deacetylase inhibitor prodrugs |
| SG171690A1 (en) | 2005-03-22 | 2011-06-29 | Harvard College | Treatment of protein degradation disorders |
| WO2007022638A1 (en) | 2005-08-26 | 2007-03-01 | Methylgene Inc. | Benzodiazepine and benzopiperazine analog inhibitors of histone deacetylase |
| JP5441416B2 (ja) | 2006-02-14 | 2014-03-12 | プレジデント アンド フェロウズ オブ ハーバード カレッジ | 二官能性ヒストンデアセチラーゼインヒビター |
| CA2654540C (en) | 2006-05-03 | 2017-01-17 | President And Fellows Of Harvard College | 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. |
| KR101433629B1 (ko) | 2006-09-11 | 2014-08-27 | 쿠리스 인코퍼레이션 | 아연 결합 부분을 함유한 티로신 키나아제 억제제 |
| 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 |
| KR101708946B1 (ko) | 2008-07-23 | 2017-02-21 | 다나-파버 캔서 인스티튜트 인크. | 탈아세틸화제 억제제 및 그것의 용도 |
| JP5713999B2 (ja) | 2009-05-15 | 2015-05-07 | コリア リサーチ インスティテュート オブ ケミカル テクノロジー | アミド化合物、その製造方法及びそれを含む薬学組成物 |
| WO2011019393A2 (en) | 2009-08-11 | 2011-02-17 | President And Fellows Of Harvard College | Class- and isoform-specific hdac inhibitors and uses thereof |
| MX2012007154A (es) * | 2009-12-17 | 2012-08-01 | Merck Sharp & Dohme | Aminopirimidinas como inhibidores de syk. |
| EP2638009A4 (en) | 2010-01-08 | 2014-06-11 | Harvard College | FLUORINATED HDAC HEMMER AND USES THEREOF |
| TW201735926A (zh) | 2010-01-22 | 2017-10-16 | 艾斯特隆製藥公司 | 作為蛋白質去乙醯酶抑制劑之反式醯胺化合物及其使用方法 |
| EP2571352A4 (en) | 2010-05-21 | 2014-09-17 | Sloan Kettering Inst Cancer | SELECTIVE HDAC HEMMER |
| WO2012018499A2 (en) | 2010-08-05 | 2012-02-09 | Acetylon Pharmaceuticals | Specific regulation of cytokine levels by hdac6 inhibitors |
| US8614223B2 (en) | 2010-11-16 | 2013-12-24 | Acetylon Pharmaceuticals, Inc. | Pyrimidine hydroxy amide compounds as protein deacetylase inhibitors and methods of use thereof |
| US9512083B2 (en) | 2011-07-20 | 2016-12-06 | The General Hospital Corporation | Histone deacetylase 6 selective inhibitors for the treatment of bone disease |
| EP2760843B1 (en) * | 2011-09-26 | 2016-03-02 | Bristol-Myers Squibb Company | Selective nr2b antagonists |
| JP5724851B2 (ja) * | 2011-11-30 | 2015-05-27 | 東レ株式会社 | Ｎ−（ヨードフェニル）ピリミジニルアミン誘導体の製造方法 |
| EP2839037B1 (en) | 2012-04-19 | 2018-12-26 | Acetylon Pharmaceuticals, Inc. | Biomarkers to identify patients that will respond to treatment and treating such patients |
| JP2015533173A (ja) | 2012-10-12 | 2015-11-19 | トラスティース・オブ・ザ・ユニバーシティ・オブ・ペンシルバニア | タンパク質脱アセチル化酵素阻害剤としてのピリミジンヒドロキシアミド化合物およびその使用方法 |
| US9145412B2 (en) | 2012-11-02 | 2015-09-29 | Acetylon Pharmaceuticals, Inc. | Selective HDAC1 and HDAC2 inhibitors |
| US9139583B2 (en) | 2013-02-01 | 2015-09-22 | Acetylon Pharmaceuticals, Inc. | Selective HDAC3 inhibitors |
| 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 |
| US20140357512A1 (en) | 2013-06-03 | 2014-12-04 | Acetylon Pharmaceuticals, Inc. | Histone deacetylase (hdac) biomarkers in multiple myeloma |
| EP3046559A4 (en) | 2013-09-20 | 2017-03-22 | Acetylon Pharmaceuticals, Inc. | Treatment of diseases caused by abnormal lymphocyte function with an hdac6 inhibitor |
| EP3054952B1 (en) | 2013-10-08 | 2022-10-26 | Acetylon Pharmaceuticals, Inc. | Combinations of histone deacetylase 6 inhibitors and the her2 inhibitor lapatinib for use in the treatment of breast cancer |
| JP6584391B2 (ja) | 2013-10-10 | 2019-10-02 | 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ｐｉ３ｋ阻害剤との組み合わせ |
| WO2015054474A1 (en) | 2013-10-10 | 2015-04-16 | Acetylon Pharmaceuticals, Inc. | Pyrimidine hydroxy amide compounds as histone deacetylase inhibitors |
| WO2015054197A1 (en) | 2013-10-10 | 2015-04-16 | Acetylon Pharmaceuticals, Inc. | Hdac inhibitors, alone or in combination with btk inhibitors, for treating non-hodgkin's lymphoma |
| KR20160060143A (ko) | 2013-10-11 | 2016-05-27 | 에이스틸론 파마수티컬스 인코포레이티드 | 히스톤 디아세틸라아제 억제제와 면역조절성 약물의 조합물 |
| 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 |
| US9949972B2 (en) | 2013-12-03 | 2018-04-24 | Acetylon Pharmaceuticals, Inc | Combinations of histone deacetylase inhibitors and immunomodulatory drugs |
| EP3084446B1 (en) | 2013-12-20 | 2022-12-14 | Acetylon Pharmaceuticals, Inc. | Histone deacetylase 6 (hdac6) biomarkers in multiple myeloma |
| US9464073B2 (en) | 2014-02-26 | 2016-10-11 | Acetylon Pharmaceuticals, Inc. | Pyrimidine hydroxy amide compounds as HDAC6 selective inhibitors |
| 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 |
| CN107205988A (zh) | 2014-07-07 | 2017-09-26 | 埃斯泰隆制药公司 | 利用组蛋白脱乙酰酶抑制剂治疗白血病 |
| US20160137630A1 (en) | 2014-10-08 | 2016-05-19 | Acetylon Pharmaceuticals, Inc. | Induction of gata2 by hdac1 and hdac2 inhibitors |
| JP2017537164A (ja) | 2014-12-05 | 2017-12-14 | ユニヴァーシティ・オブ・モデナ・アンド・レッジョ・エミリア | リンパ腫の治療に使用されるヒストン脱アセチル化酵素阻害剤とベンダムスチンとの組み合わせ |
| WO2016090230A1 (en) | 2014-12-05 | 2016-06-09 | Acetylon Pharmaceuticals, Inc. | Pyrimidine hydroxy amide compounds for treating peripheral neuropathy |
| ES2816641T3 (es) | 2014-12-12 | 2021-04-05 | Regenacy Pharmaceuticals Inc | Derivados de piperidina en calidad de inhibidores de HDAC1/2 |
| 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 |
| TWI706937B (zh) | 2015-06-08 | 2020-10-11 | 美商艾斯特隆製藥公司 | 製備蛋白質去乙醯酶抑制劑之方法 |
| TW201718516A (zh) | 2015-06-08 | 2017-06-01 | 艾斯特隆製藥公司 | 組蛋白去乙醯酶抑制劑之晶形 |
| US11324744B2 (en) | 2016-08-08 | 2022-05-10 | Acetylon Pharmaceuticals Inc. | Methods of use and pharmaceutical combinations of histone deacetylase inhibitors and CD20 inhibitory antibodies |
-
2016
- 2016-06-08 TW TW105118213A patent/TWI706937B/zh active
- 2016-06-08 WO PCT/US2016/036434 patent/WO2016200930A1/en not_active Ceased
- 2016-06-08 CA CA2988594A patent/CA2988594C/en active Active
- 2016-06-08 ES ES16732810T patent/ES2769255T3/es active Active
- 2016-06-08 EP EP16732810.3A patent/EP3303304B1/en active Active
- 2016-06-08 MX MX2017015900A patent/MX369349B/es active IP Right Grant
- 2016-06-08 CN CN201680046553.8A patent/CN107922352B/zh active Active
- 2016-06-08 AU AU2016276573A patent/AU2016276573A1/en not_active Abandoned
- 2016-06-08 JP JP2017563541A patent/JP6873053B2/ja active Active
- 2016-06-08 AR ARP160101701A patent/AR105812A1/es unknown
- 2016-06-08 US US15/176,826 patent/US10144714B2/en active Active
-
2020
- 2020-11-13 AU AU2020267299A patent/AU2020267299B2/en active Active
Also Published As
| Publication number | Publication date |
|---|---|
| EP3303304A1 (en) | 2018-04-11 |
| CA2988594A1 (en) | 2016-12-15 |
| WO2016200930A1 (en) | 2016-12-15 |
| US10144714B2 (en) | 2018-12-04 |
| JP2018518486A (ja) | 2018-07-12 |
| TWI706937B (zh) | 2020-10-11 |
| JP6873053B2 (ja) | 2021-05-19 |
| AU2020267299A1 (en) | 2020-12-10 |
| CN107922352A (zh) | 2018-04-17 |
| AU2016276573A1 (en) | 2018-01-04 |
| US20160355486A1 (en) | 2016-12-08 |
| AU2020267299B2 (en) | 2022-07-07 |
| MX2017015900A (es) | 2018-11-09 |
| CN107922352B (zh) | 2021-08-06 |
| AR105812A1 (es) | 2017-11-15 |
| MX369349B (es) | 2019-11-06 |
| TW201718517A (zh) | 2017-06-01 |
| EP3303304B1 (en) | 2019-11-20 |
| WO2016200930A9 (en) | 2017-02-23 |
| CA2988594C (en) | 2023-08-15 |
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