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

Info

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
Authority
CN
China
Prior art keywords
compound
acid
reacting
another embodiment
preparing
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
Application number
CN201680046553.8A
Other languages
English (en)
Chinese (zh)
Other versions
CN107922352A (zh
Inventor
F·塞伊迪
J·H·范杜泽尔
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Acetylon Pharmaceuticals Inc
Original Assignee
Acetylon Pharmaceuticals Inc
Priority date (The priority date 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 date listed.)
Filing date
Publication date
Application filed by Acetylon Pharmaceuticals Inc filed Critical Acetylon Pharmaceuticals Inc
Publication of CN107922352A publication Critical patent/CN107922352A/zh
Application granted granted Critical
Publication of CN107922352B publication Critical patent/CN107922352B/zh
Active legal-status Critical Current
Anticipated expiration legal-status Critical

Links

Images

Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D239/00Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/02Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
    • C07D239/24Heterocyclic 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
    • C07D239/28Heterocyclic 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
    • C07D239/32One oxygen, sulfur or nitrogen atom
    • C07D239/42One nitrogen atom
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D239/00Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/02Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
    • C07D239/24Heterocyclic 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
    • C07D239/28Heterocyclic 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
    • C07D239/30Halogen 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)
  • Peptides Or Proteins (AREA)
  • Preparation Of Compounds By Using Micro-Organisms (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)

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

ID=56264043

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 (OSRAM)
EP (1) EP3303304B1 (OSRAM)
JP (1) JP6873053B2 (OSRAM)
CN (1) CN107922352B (OSRAM)
AR (1) AR105812A1 (OSRAM)
AU (2) AU2016276573A1 (OSRAM)
CA (1) CA2988594C (OSRAM)
ES (1) ES2769255T3 (OSRAM)
MX (1) MX369349B (OSRAM)
TW (1) TWI706937B (OSRAM)
WO (1) WO2016200930A1 (OSRAM)

Families Citing this family (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
LT2526093T (lt) * 2010-01-22 2016-10-10 Acetylon Pharmaceuticals, Inc. Grįžtamieji amido junginiai kaip baltymo deacetilazės inhibitoriai ir jų panaudojimo būdai
HK1207403A1 (en) 2012-04-19 2016-01-29 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
WO2016200930A1 (en) 2015-06-08 2016-12-15 Acetylon Pharmaceuticals, Inc. Methods of making protein deacetylase inhibitors
AR109250A1 (es) * 2016-06-09 2018-11-14 Acetylon Pharmaceuticals Inc Métodos de uso y combinaciones farmacéuticas de inhibidores de hdac con inhibidores de proteínas bet
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
JP7090611B2 (ja) 2016-11-23 2022-06-24 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 ヒストン脱アセチル化酵素阻害剤とプログラム細胞死リガンド1(pd-l1)阻害剤とを含む医薬組み合わせ物及びその使用方法

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
ATE489360T1 (de) 2000-03-24 2010-12-15 Methylgene Inc Inhibitoren der histon-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
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
US7169801B2 (en) 2003-03-17 2007-01-30 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
AU2005230682B2 (en) 2004-04-05 2010-10-21 Merck Hdac Research, Llc Histone deacetylase inhibitor prodrugs
EP3354265A1 (en) 2005-03-22 2018-08-01 President and Fellows of Harvard College Treatment of solid tumors
JP2009509923A (ja) 2005-08-26 2009-03-12 メシルジーン、インコーポレイテッド ヒストンデアセチラーゼのベンゾジアゼピン及びベンゾピペラジン類似体阻害薬
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
US8304451B2 (en) 2006-05-03 2012-11-06 President And Fellows Of Harvard College 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.
AU2007296743B2 (en) 2006-09-11 2012-02-16 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
CA2731730C (en) 2008-07-23 2017-06-13 President And Fellows Of Harvard College Deacetylase inhibitors and uses thereof
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
EP2513098B1 (en) * 2009-12-17 2016-11-09 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
JP6041808B2 (ja) 2010-11-16 2016-12-14 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. 蛋白質脱アセチル化酵素抑制剤としてのピリミジン水酸基アミド化合物およびその利用方法
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
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
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
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
WO2014121062A1 (en) 2013-02-01 2014-08-07 Acetylon Pharmaceuticals, Inc. Selective hdac3 inhibitors
WO2014197471A1 (en) 2013-06-03 2014-12-11 Acetylon Pharmaceuticals, Inc. Histone deacetylase ( hdac) biomarkers in multiple myeloma
WO2015042418A1 (en) 2013-09-20 2015-03-26 Acetylon Pharmaceuticals, Inc. Treatment of diseases caused by abnormal lymphocyte function with an hdac6 inhibitor
EP3055299B1 (en) 2013-10-10 2021-01-06 Acetylon Pharmaceuticals, Inc. Pyrimidine hydroxy amide compounds as histone deacetylase inhibitors
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
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
JP2016534069A (ja) 2013-10-24 2016-11-04 メイヨ・ファウンデーション・フォー・メディカル・エデュケーション・アンド・リサーチ Hdac6阻害剤での多嚢胞性疾患の治療
US9949972B2 (en) 2013-12-03 2018-04-24 Acetylon Pharmaceuticals, Inc Combinations of histone deacetylase inhibitors and immunomodulatory drugs
WO2015095632A1 (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
EP3166603B1 (en) 2014-07-07 2020-02-12 Acetylon Pharmaceuticals, Inc. Treatment of leukemia with histone deacetylase inhibitors
EP3204006A4 (en) 2014-10-08 2018-04-04 Regenacy Pharmaceuticals, LLC 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
CA2969790A1 (en) 2014-12-05 2016-06-09 University of Modena and Reggio Emilia Combinations of histone deacetylase inhibitors and bendamustine
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
WO2016200930A1 (en) 2015-06-08 2016-12-15 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
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

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 *

Also Published As

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

Similar Documents

Publication Publication Date Title
CN107922352B (zh) 制备蛋白质脱乙酰酶抑制剂的方法
JP7100125B2 (ja) リボシクリブおよびその塩の改善された調製のためのプロセス
JP6439050B2 (ja) Ask1阻害剤を調製するプロセス
CA2698245C (en) Process and intermediates for preparing integrase inhibitors
KR102396059B1 (ko) 신규 화합물 및 이의 제조방법
JP7157752B2 (ja) Ag-10、その中間体及びその塩の調製方法
US7868207B2 (en) Process for producing 1-(3,4-dichlorobenzyl)-5-octylbiguanide or a salt thereof
EP3412666A1 (en) Process and intermediates for the preparation of bcl-2 inhibitors including venetoclax through reductive amination
US20090137821A1 (en) Method of making dorzolamide hydrochloride
TWI545114B (zh) 製備聯苯基咪唑化合物之方法
US20240262805A1 (en) Method for producing compound or pharmaceutically acceptable salt thereof
KR20250044411A (ko) 빌록사진(viloxazine) 및 기타 2-치환 모르폴린 유도체의 제조 공정 및 중간체
WO2015104602A2 (en) A process for the preparation of anagliptin and its intermediates thereof
CN110498762A (zh) 一种(2s,5r)-5-[(苄氧基)氨基]-哌啶-2-甲酸乙酯的合成方法
JP2008115179A (ja) 光学活性2−[(n−ベンジルプロリル)アミノ]ベンゾフェノン化合物の製造方法
WO2025186427A1 (en) Process for the preparation of deucravacitinib and intermediates thereof and method for purifying deucravacitinib
US20080033181A1 (en) Process for the preparation of Zonisamide and the intermediates thereof
JP2024511422A (ja) 5-{5-クロロ-2-[(3s)-3-[(モルホリン-4-イル)メチル]-3,4-ジヒドロイソキノリン-2(1h)-カルボニル]フェニル}-1,2-ジメチル-1h-ピロール-3-カルボン酸誘導体を合成するための新規な製造方法及び医薬化合物を製造するためのその適用
JP2023033201A (ja) オラパリブの製造方法
WO2022034427A1 (en) An improved process for the preparation of 4-oxoisotretinoin
CN120936603A (zh) 并环化合物的制备方法及其中间体
JP2023513418A (ja) Cdk阻害活性を示すプリン誘導体の調製のための方法

Legal Events

Date Code Title Description
PB01 Publication
PB01 Publication
SE01 Entry into force of request for substantive examination
SE01 Entry into force of request for substantive examination
GR01 Patent grant
GR01 Patent grant