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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Publication number
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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compound
acid
reacting
another embodiment
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)
  • 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)
CN201680046553.8A 2015-06-08 2016-06-08 制备蛋白质脱乙酰酶抑制剂的方法 Expired - Fee Related CN107922352B (zh)

Applications Claiming Priority (3)

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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
PL2526093T3 (pl) * 2010-01-22 2017-02-28 Acetylon Pharmaceuticals, Inc. Odwrócone związki amidowe jako inhibitory deacetylazy białkowej oraz sposoby ich stosowania
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
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
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
EP3544600A4 (en) 2016-11-23 2020-06-17 Acetylon Pharmaceuticals, Inc. PHARMACEUTICAL COMBINATIONS WITH A HISTONE DEACETYLAS INHIBITOR AND A PROGRAMMED DEATH LIGAND-1 (PD-L1) INHIBITOR AND METHOD FOR 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
JP2003528074A (ja) 2000-03-24 2003-09-24 メチルジーン インコーポレイテッド ヒストン脱アセチル化酵素の阻害剤
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
AU2002363174B2 (en) 2001-11-01 2008-09-25 Janssen Pharmaceutica N.V. Amide derivatives as glycogen synthase kinase 3-beta 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
EP1644323B1 (en) 2003-07-07 2015-03-18 Georgetown University Histone deacetylase inhibitors and methods of use thereof
CA2561617A1 (en) 2004-04-05 2005-10-20 Aton Pharma, Inc. Histone deacetylase inhibitor prodrugs
SG171690A1 (en) 2005-03-22 2011-06-29 Harvard College Treatment of protein degradation disorders
CA2620414A1 (en) 2005-08-26 2007-03-01 Methylgene Inc. Benzodiazepine and benzopiperazine analog inhibitors of histone deacetylase
WO2008091349A1 (en) 2006-02-14 2008-07-31 The President And Fellows Of Harvard College Bifunctional histone deacetylase inhibitors
WO2007130429A2 (en) 2006-05-03 2007-11-15 The 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.
WO2008033746A2 (en) 2006-09-11 2008-03-20 Curis, Inc. Tyrosine kinase inhibitors containing a zinc binding moiety
TWI478709B (zh) 2008-02-19 2015-04-01 Earnest Medicine Co Ltd A useful oral or enteral composition for the recovery of bodily functions
EP2321264B1 (en) 2008-07-23 2016-05-04 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
US8716344B2 (en) 2009-08-11 2014-05-06 President And Fellows Of Harvard College Class- and isoform-specific HDAC inhibitors and uses thereof
AU2010331927B2 (en) * 2009-12-17 2013-10-10 Merck Canada Inc. Aminopyrimidines as Syk inhibitors
WO2011084991A2 (en) 2010-01-08 2011-07-14 President And Fellows Of Harvard College Fluorinated hdac inhibitors and uses thereof
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
NZ610225A (en) 2010-11-16 2015-08-28 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
HK1207403A1 (en) 2012-04-19 2016-01-29 Acetylon Pharmaceuticals, Inc. Biomarkers to identify patients that will respond to treatment and treating such patients
WO2014059306A1 (en) 2012-10-12 2014-04-17 The Trustees Of The University Of Pennsylvania Pyrimidine hydroxy amide compounds as protein deacetylase inhibitors and methods of use thereof
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
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
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
EP3055299B1 (en) 2013-10-10 2021-01-06 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
PE20161342A1 (es) 2013-10-11 2016-12-31 Acetylon Pharmaceuticals Inc Combinaciones de inhibidores de histona desacetilasa y farmacos inmunomoduladores
EP3060217B1 (en) 2013-10-24 2022-06-08 Mayo Foundation for Medical Education and Research Treatment of polycystic diseases with an hdac6 inhibitor
EP3076973B1 (en) 2013-12-03 2020-04-29 Acetylon Pharmaceuticals, Inc. Combinations of histone deacetylase inhibitors and immunomodulatory drugs
US20150176076A1 (en) 2013-12-20 2015-06-25 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
US20160158231A1 (en) 2014-12-05 2016-06-09 Vib Vzw Pyrimidine hydroxy amide compounds for treating peripheral neuropathy
CN107438436A (zh) 2014-12-05 2017-12-05 摩德纳和雷焦艾米利亚大学 用于治疗淋巴瘤的组蛋白脱乙酰酶抑制剂和苯达莫司汀的组合
CA2970500C (en) 2014-12-12 2023-08-29 Acetylon Pharmaceuticals, Inc. 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
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
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

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

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