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 PDF

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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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acid
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preparing
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CN107922352A (zh
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F·塞伊迪
J·H·范杜泽尔
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Acetylon Pharmaceuticals Inc
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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)
CN201680046553.8A 2015-06-08 2016-06-08 制备蛋白质脱乙酰酶抑制剂的方法 Active CN107922352B (zh)

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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

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CN107922352A CN107922352A (zh) 2018-04-17
CN107922352B true CN107922352B (zh) 2021-08-06

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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)

* Cited by examiner, † Cited by third party
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
HK1207403A1 (en) 2012-04-19 2016-01-29 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
ES2769255T3 (es) 2015-06-08 2020-06-25 Acetylon Pharmaceuticals Inc Métodos para fabricar inhibidores de la proteína desacetilasa
TW201803594A (zh) * 2016-06-09 2018-02-01 達納-法伯癌症協會 Hdac抑制劑與bet抑制劑之使用方法及醫藥組合
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
EP3544600A4 (en) 2016-11-23 2020-06-17 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)

* Cited by examiner, † Cited by third party
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

Family Cites Families (54)

* Cited by examiner, † Cited by third party
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
US7288567B2 (en) 2000-03-24 2007-10-30 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
HUP0402330A3 (en) 2001-11-01 2010-03-29 Janssen Pharmaceutica Nv Amide derivatives as glycogen synthase kinase 3-beta inhibitors, process for producing them, pharmaceutical compositions containing them and use thereof
US7154002B1 (en) 2002-10-08 2006-12-26 Takeda San Diego, Inc. Histone deacetylase inhibitors
EP1608628A2 (en) 2003-03-17 2005-12-28 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
WO2005097747A1 (en) 2004-04-05 2005-10-20 Aton Pharma, Inc. Histone deacetylase inhibitor prodrugs
US8999289B2 (en) 2005-03-22 2015-04-07 President And Fellows Of Harvard College Treatment of protein degradation disorders
AU2006284403A1 (en) 2005-08-26 2007-03-01 Methylgene Inc. Benzodiazepine and benzopiperazine analog inhibitors of histone deacetylase
US8222423B2 (en) 2006-02-14 2012-07-17 Dana-Farber Cancer Institute, Inc. Bifunctional histone deacetylase inhibitors
AU2007248656B2 (en) 2006-05-03 2013-04-04 Dana-Farber Cancer Institute, Inc. Histone deacetylase and tubulin deacetylase inhibitors
US20100278782A1 (en) 2006-06-12 2010-11-04 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
US8778410B2 (en) 2008-02-19 2014-07-15 Earnest Medicine Co., Ltd. Oral or enteral composition useful for recovery of physical functions
KR101708946B1 (ko) 2008-07-23 2017-02-21 다나-파버 캔서 인스티튜트 인크. 탈아세틸화제 억제제 및 그것의 용도
EP2429987A4 (en) 2009-05-15 2012-10-03 Korea Res Inst Chem Tech AMIDE COMPOUND, PROCESS FOR PREPARING THE SAME, AND PHARMACEUTICAL COMPOSITION COMPRISING THE SAME
WO2011019393A2 (en) 2009-08-11 2011-02-17 President And Fellows Of Harvard College Class- and isoform-specific hdac inhibitors and uses thereof
US8759366B2 (en) * 2009-12-17 2014-06-24 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
CA2800143A1 (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
EP3067346A1 (en) 2010-11-16 2016-09-14 Acetylon Pharmaceuticals, Inc. Pyrimidine hydroxy amide compounds as protein deacetylase inhibitors and methods of use thereof
WO2013013113A2 (en) 2011-07-20 2013-01-24 The General Hospital Corporation Histone deacetylase 6 selective inhibitors for the treatment of bone disease
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
HK1207403A1 (en) 2012-04-19 2016-01-29 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
US9096549B2 (en) 2013-02-01 2015-08-04 Acetylon Pharmaceuticals, Inc. Selective HDAC3 inhibitors
JP2016523236A (ja) 2013-06-03 2016-08-08 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Ａｃｅｔｙｌｏｎ Ｐｈａｒｍａｃｅｕｔｉｃａｌｓ，Ｉｎｃ． 多発性骨髄腫におけるヒストン脱アセチル化酵素（ｈｄａｃ）バイオマーカー
WO2015042418A1 (en) 2013-09-20 2015-03-26 Acetylon Pharmaceuticals, Inc. Treatment of diseases caused by abnormal lymphocyte function with an hdac6 inhibitor
ES2862126T3 (es) 2013-10-10 2021-10-07 Acetylon Pharmaceuticals Inc Compuestos de pirimidín-hidroxiamida como inhibidores de histona desacetilasa
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
ES2818933T3 (es) 2013-10-10 2021-04-14 Acetylon Pharmaceuticals Inc Inhibidores de la HDAC en combinación con los inhibidores de la pi3k, para el tratamiento del linfoma no Hodgkin
WO2015054175A1 (en) 2013-10-11 2015-04-16 Acetylon Pharmaceuticals, Inc. Combinations of histone deactylase inhibitors and immunomodulatory drugs
EP3060217B1 (en) 2013-10-24 2022-06-08 Mayo Foundation for Medical Education and Research Treatment of polycystic diseases with an hdac6 inhibitor
MX2016007251A (es) 2013-12-03 2016-09-07 Acetylon Pharmaceuticals Inc Combinaciones de inhibidores de histona deacetilasa y farmacos inmunomoduladores.
ES2936812T3 (es) 2013-12-20 2023-03-22 Acetylon Pharmaceuticals Inc Biomarcadores de histona desacetilasa 6 (HDAC6) en mieloma múltiple
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
EA201790142A1 (ru) 2014-07-07 2017-07-31 Эситайлон Фармасьютикалз, Инк. Лечение лейкоза ингибиторами гистондеацетилазы
US20160137630A1 (en) 2014-10-08 2016-05-19 Acetylon Pharmaceuticals, Inc. Induction of gata2 by hdac1 and hdac2 inhibitors
AU2015356779A1 (en) 2014-12-05 2017-07-13 University of Modena and Reggio Emilia Combinations of histone deacetylase inhibitors and bendamustine for use in the treatment of lymphoma
WO2016090230A1 (en) 2014-12-05 2016-06-09 Acetylon Pharmaceuticals, Inc. Pyrimidine hydroxy amide compounds for treating peripheral neuropathy
EP3292113B1 (en) 2014-12-12 2020-07-08 Regenacy Pharmaceuticals, LLC Piperidine derivatives as hdac1/2 inhibitors
US20160339022A1 (en) 2015-04-17 2016-11-24 Acetylon Pharmaceuticals Inc. Treatment of neuroblastoma with histone deacetylase inhibitors
US10272084B2 (en) 2015-06-01 2019-04-30 Regenacy Pharmaceuticals, Llc Histone deacetylase 6 selective inhibitors for the treatment of cisplatin-induced peripheral neuropathy
ES2769255T3 (es) 2015-06-08 2020-06-25 Acetylon Pharmaceuticals Inc Métodos para fabricar inhibidores de la proteína desacetilasa
AR104935A1 (es) 2015-06-08 2017-08-23 Acetylon Pharmaceuticals Inc Formas cristalinas de un inhibidor de histona deacetilasa
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

Patent Citations (3)

* Cited by examiner, † Cited by third party
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)

* Cited by examiner, † Cited by third party
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 *

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AU2020267299B2 (en) 2022-07-07
US10144714B2 (en) 2018-12-04
AU2020267299A1 (en) 2020-12-10
US20160355486A1 (en) 2016-12-08
WO2016200930A9 (en) 2017-02-23
TW201718517A (zh) 2017-06-01
EP3303304A1 (en) 2018-04-11
ES2769255T3 (es) 2020-06-25
MX2017015900A (es) 2018-11-09
MX369349B (es) 2019-11-06
WO2016200930A1 (en) 2016-12-15
AU2016276573A1 (en) 2018-01-04
TWI706937B (zh) 2020-10-11
CA2988594A1 (en) 2016-12-15
AR105812A1 (es) 2017-11-15
EP3303304B1 (en) 2019-11-20
JP2018518486A (ja) 2018-07-12
CA2988594C (en) 2023-08-15
CN107922352A (zh) 2018-04-17
JP6873053B2 (ja) 2021-05-19

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