CN107922352B - 制备蛋白质脱乙酰酶抑制剂的方法 - Google Patents
制备蛋白质脱乙酰酶抑制剂的方法 Download PDFInfo
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- CN107922352B CN107922352B CN201680046553.8A CN201680046553A CN107922352B CN 107922352 B CN107922352 B CN 107922352B CN 201680046553 A CN201680046553 A CN 201680046553A CN 107922352 B CN107922352 B CN 107922352B
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- 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
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- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Preparation Of Compounds By Using Micro-Organisms (AREA)
- Peptides Or Proteins (AREA)
- Low-Molecular Organic Synthesis Reactions Using Catalysts (AREA)
- Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201562172624P | 2015-06-08 | 2015-06-08 | |
| US62/172,624 | 2015-06-08 | ||
| PCT/US2016/036434 WO2016200930A1 (en) | 2015-06-08 | 2016-06-08 | Methods of making protein deacetylase inhibitors |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| CN107922352A CN107922352A (zh) | 2018-04-17 |
| CN107922352B true CN107922352B (zh) | 2021-08-06 |
Family
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Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN201680046553.8A Active CN107922352B (zh) | 2015-06-08 | 2016-06-08 | 制备蛋白质脱乙酰酶抑制剂的方法 |
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 |
|---|---|---|---|---|
| CN102933558B (zh) | 2010-01-22 | 2016-03-16 | 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 |
| WO2013158984A1 (en) | 2012-04-19 | 2013-10-24 | Acetylon Pharmaceuticals, Inc. | Biomarkers to identify patients that will respond to treatment and treating such patients |
| EP3303306B1 (en) | 2015-06-08 | 2020-02-12 | Acetylon Pharmaceuticals, Inc. | Crystalline forms of a histone deacetylase inhibitor |
| CA2988594C (en) | 2015-06-08 | 2023-08-15 | Acetylon Pharmaceuticals, Inc. | Methods of making protein deacetylase inhibitors |
| 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 |
| JP7100018B2 (ja) | 2016-08-08 | 2022-07-12 | 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 | ヒストンデアセチラーゼ6阻害剤及びcd20阻害抗体の薬学的組み合わせならびにその使用 |
| US11497746B2 (en) | 2016-11-23 | 2022-11-15 | Acetylon Pharmaceuticals, Inc. | Pharmaceutical combinations comprising a histone deacetylase inhibitor and a programmed death-ligand 1 (PD-L1) inhibitor and methods of use thereof |
Citations (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US8148526B1 (en) * | 2010-01-22 | 2012-04-03 | Acetylon Pharmaceuticals | Reverse amide compounds as protein deacetylase inhibitors and methods of use thereof |
| WO2013048949A2 (en) * | 2011-09-26 | 2013-04-04 | Bristol-Myers Squibb Company | Selective nr2b antagonists |
| WO2015054099A1 (en) * | 2013-10-08 | 2015-04-16 | Acetylon Pharmaceuticals, Inc. | Combinations of histone deacetylase inhibitors and either her2 inhibitors or pi3k inhibitors |
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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 |
| WO2002074298A1 (en) | 2001-03-21 | 2002-09-26 | Ono Pharmaceutical Co., Ltd. | Il-6 production inhibitors |
| US7244853B2 (en) | 2001-05-09 | 2007-07-17 | President And Fellows Of Harvard College | Dioxanes and uses thereof |
| BR0213791A (pt) | 2001-11-01 | 2004-12-07 | Janssen Pharmaceutica Nv | Derivados de amida como inibidores de glicogênio sintase quinase 3-beta |
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| US7381825B2 (en) | 2003-03-17 | 2008-06-03 | Takeda San Diego, Inc. | Histone deacetylase inhibitors |
| CA2531661C (en) | 2003-07-07 | 2013-03-12 | 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 |
| CN101495116A (zh) | 2005-03-22 | 2009-07-29 | 哈佛大学校长及研究员协会 | 蛋白降解病症的治疗 |
| EP1940805A4 (en) | 2005-08-26 | 2009-11-11 | Methylgene Inc | BENZODIAZEPIN AND BENZOPIPERAZINANALOGA AS INHIBITORS OF HISTONDEACETYLASE |
| 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 |
| CN101484156B (zh) | 2006-05-03 | 2015-11-25 | 哈佛大学校长及研究员协会 | 组蛋白脱乙酰基酶和微管蛋白脱乙酰基酶抑制剂 |
| 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. |
| WO2008033746A2 (en) | 2006-09-11 | 2008-03-20 | Curis, Inc. | Tyrosine kinase inhibitors containing a zinc binding moiety |
| EP2255818B1 (en) | 2008-02-19 | 2018-08-22 | Earnest Medicine Co., Ltd. | Oral or enteral composition useful for recovery of physical functions |
| RU2515611C2 (ru) | 2008-07-23 | 2014-05-20 | Президент Энд Феллоуз Оф Гарвард Колледж | Ингибиторы деацетилазы и их применение |
| WO2010131922A2 (en) | 2009-05-15 | 2010-11-18 | Korea Research Institute Of Chemical Technology | Amide compound, preparation method thereof and pharmaceutical composition comprising same |
| US8716344B2 (en) | 2009-08-11 | 2014-05-06 | President And Fellows Of Harvard College | Class- and isoform-specific HDAC inhibitors and uses thereof |
| US8551984B2 (en) * | 2009-12-17 | 2013-10-08 | Merck Sharp & Dohme Corp. | Aminopyrimidines as SYK inhibitors |
| US20130040998A1 (en) | 2010-01-08 | 2013-02-14 | Dana-Farber Cancer Institute, Inc. | Fluorinated hdac inhibitors and uses thereof |
| AU2011255281A1 (en) | 2010-05-21 | 2013-01-10 | Sloan-Kettering Institute For Cancer Research | Selective HDAC inhibitors |
| WO2012018499A2 (en) | 2010-08-05 | 2012-02-09 | Acetylon Pharmaceuticals | Specific regulation of cytokine levels by hdac6 inhibitors |
| NZ710405A (en) | 2010-11-16 | 2017-04-28 | Acetylon Pharmaceuticals Inc | Pyrimidine hydroxy amide compounds as protein deacetylase inhibitors and methods of use thereof |
| EP2734500A4 (en) | 2011-07-20 | 2015-04-08 | Gen Hospital Corp | SELECTIVE HISTONDEACETYLASE-6 INHIBITORS FOR THE TREATMENT OF BONE DISORDERS |
| 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 |
| WO2013158984A1 (en) | 2012-04-19 | 2013-10-24 | Acetylon Pharmaceuticals, Inc. | Biomarkers to identify patients that will respond to treatment and treating such patients |
| HK1213471A1 (zh) | 2012-10-12 | 2016-07-08 | The Trustees Of The University Of Pennsylvania | 作為蛋白脫乙酰基酶抑制劑的嘧啶羥基酰胺化合物及其使用方法 |
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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 |
| US9139583B2 (en) | 2013-02-01 | 2015-09-22 | Acetylon Pharmaceuticals, Inc. | Selective HDAC3 inhibitors |
| WO2014197471A1 (en) | 2013-06-03 | 2014-12-11 | Acetylon Pharmaceuticals, Inc. | Histone deacetylase ( hdac) biomarkers in multiple myeloma |
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| EP3054953B1 (en) | 2013-10-10 | 2020-07-01 | Acetylon Pharmaceuticals, Inc. | Hdac inhibitors in combination with pi3k inhibitors, for treating non-hodgkin's lymphoma |
| 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 |
| EP3054939A4 (en) | 2013-10-11 | 2017-12-13 | 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 |
| KR20160092018A (ko) | 2013-12-03 | 2016-08-03 | 에이스틸론 파마수티컬스 인코포레이티드 | 히스톤 탈아세틸화효소 저해제 및 면역조절 약물의 조합 |
| JP7017309B2 (ja) | 2013-12-20 | 2022-02-08 | 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 | 多発性骨髄腫におけるヒストン脱アセチル化酵素6(hdac6)バイオマーカー |
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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 |
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| US9790180B2 (en) | 2014-12-12 | 2017-10-17 | Regenacy Pharmaceuticals, Llc | Piperidine derivatives as HDAC1/2 inhibitors |
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| US10272084B2 (en) | 2015-06-01 | 2019-04-30 | Regenacy Pharmaceuticals, Llc | Histone deacetylase 6 selective inhibitors for the treatment of cisplatin-induced peripheral neuropathy |
| CA2988594C (en) | 2015-06-08 | 2023-08-15 | Acetylon Pharmaceuticals, Inc. | Methods of making protein deacetylase inhibitors |
| EP3303306B1 (en) | 2015-06-08 | 2020-02-12 | Acetylon Pharmaceuticals, Inc. | Crystalline forms of a histone deacetylase inhibitor |
| JP7100018B2 (ja) | 2016-08-08 | 2022-07-12 | 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 | ヒストンデアセチラーゼ6阻害剤及びcd20阻害抗体の薬学的組み合わせならびにその使用 |
-
2016
- 2016-06-08 CA CA2988594A patent/CA2988594C/en active Active
- 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
- 2016-06-08 WO PCT/US2016/036434 patent/WO2016200930A1/en not_active Ceased
- 2016-06-08 TW TW105118213A patent/TWI706937B/zh active
- 2016-06-08 ES ES16732810T patent/ES2769255T3/es active Active
- 2016-06-08 CN CN201680046553.8A patent/CN107922352B/zh active Active
- 2016-06-08 EP EP16732810.3A patent/EP3303304B1/en active Active
- 2016-06-08 AU AU2016276573A patent/AU2016276573A1/en not_active Abandoned
- 2016-06-08 MX MX2017015900A patent/MX369349B/es active IP Right Grant
-
2020
- 2020-11-13 AU AU2020267299A patent/AU2020267299B2/en active Active
Patent Citations (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US8148526B1 (en) * | 2010-01-22 | 2012-04-03 | Acetylon Pharmaceuticals | Reverse amide compounds as protein deacetylase inhibitors and methods of use thereof |
| WO2013048949A2 (en) * | 2011-09-26 | 2013-04-04 | Bristol-Myers Squibb Company | Selective nr2b antagonists |
| WO2015054099A1 (en) * | 2013-10-08 | 2015-04-16 | Acetylon Pharmaceuticals, Inc. | Combinations of histone deacetylase inhibitors and either her2 inhibitors or pi3k inhibitors |
Non-Patent Citations (2)
| Title |
|---|
| "General Preparation of Primary, Secondary, and Tertiary Aryl Amines by the Oxidative Coupling of Polyfunctional Aryl and Heteroaryl Amidocuprates";Vicente del Amo et al.;《ANGEWANDTE CHEMIE-INTERNATIONAL EDITION》;20061120;第45卷(第46期);第7838-7842页 * |
| "Piperidyl amides as novel, potent and orally active mGlu5 receptor antagonists with anxiolytic-like activity";Carsten Spanka et al.;《Bioorganic & Medicinal Chemistry Letters》;20100101;第20卷(第1期);第184-188页 * |
Also Published As
| Publication number | Publication date |
|---|---|
| MX2017015900A (es) | 2018-11-09 |
| TW201718517A (zh) | 2017-06-01 |
| WO2016200930A1 (en) | 2016-12-15 |
| ES2769255T3 (es) | 2020-06-25 |
| AU2020267299A1 (en) | 2020-12-10 |
| AU2020267299B2 (en) | 2022-07-07 |
| MX369349B (es) | 2019-11-06 |
| TWI706937B (zh) | 2020-10-11 |
| AU2016276573A1 (en) | 2018-01-04 |
| CN107922352A (zh) | 2018-04-17 |
| AR105812A1 (es) | 2017-11-15 |
| CA2988594C (en) | 2023-08-15 |
| US10144714B2 (en) | 2018-12-04 |
| WO2016200930A9 (en) | 2017-02-23 |
| JP6873053B2 (ja) | 2021-05-19 |
| EP3303304A1 (en) | 2018-04-11 |
| CA2988594A1 (en) | 2016-12-15 |
| US20160355486A1 (en) | 2016-12-08 |
| EP3303304B1 (en) | 2019-11-20 |
| JP2018518486A (ja) | 2018-07-12 |
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