JP6816036B2 - ヒストン脱アセチル化阻害剤の結晶形態 - Google Patents

ヒストン脱アセチル化阻害剤の結晶形態 Download PDF

Info

Publication number
JP6816036B2
JP6816036B2 JP2017563542A JP2017563542A JP6816036B2 JP 6816036 B2 JP6816036 B2 JP 6816036B2 JP 2017563542 A JP2017563542 A JP 2017563542A JP 2017563542 A JP2017563542 A JP 2017563542A JP 6816036 B2 JP6816036 B2 JP 6816036B2
Authority
JP
Japan
Prior art keywords
pattern
oxoheptyl
hydroxyamino
carboxamide
chlorophenyl
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.)
Expired - Fee Related
Application number
JP2017563542A
Other languages
English (en)
Japanese (ja)
Other versions
JP2018516946A5 (enExample
JP2018516946A (ja
Inventor
ジョン・エイチ・ヴァン・ドゥーザー
ファルザネー・セイエディ
グイ・リュウ
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 JP2018516946A publication Critical patent/JP2018516946A/ja
Publication of JP2018516946A5 publication Critical patent/JP2018516946A5/ja
Application granted granted Critical
Publication of JP6816036B2 publication Critical patent/JP6816036B2/ja
Expired - Fee Related legal-status Critical Current
Anticipated expiration legal-status Critical

Links

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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07BGENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B2200/00Indexing scheme relating to specific properties of organic compounds
    • C07B2200/13Crystalline forms, e.g. polymorphs

Landscapes

  • Organic Chemistry (AREA)
  • Chemical & Material Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
JP2017563542A 2015-06-08 2016-06-08 ヒストン脱アセチル化阻害剤の結晶形態 Expired - Fee Related JP6816036B2 (ja)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201562172629P 2015-06-08 2015-06-08
US62/172,629 2015-06-08
PCT/US2016/036422 WO2016200919A1 (en) 2015-06-08 2016-06-08 Crystalline forms of a histone deacetylase inhibitor

Publications (3)

Publication Number Publication Date
JP2018516946A JP2018516946A (ja) 2018-06-28
JP2018516946A5 JP2018516946A5 (enExample) 2019-07-04
JP6816036B2 true JP6816036B2 (ja) 2021-01-20

Family

ID=56178492

Family Applications (1)

Application Number Title Priority Date Filing Date
JP2017563542A Expired - Fee Related JP6816036B2 (ja) 2015-06-08 2016-06-08 ヒストン脱アセチル化阻害剤の結晶形態

Country Status (6)

Country Link
US (1) US10464906B2 (enExample)
EP (1) EP3303306B1 (enExample)
JP (1) JP6816036B2 (enExample)
AR (1) AR104935A1 (enExample)
TW (1) TW201718516A (enExample)
WO (1) WO2016200919A1 (enExample)

Families Citing this family (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2013158984A1 (en) 2012-04-19 2013-10-24 Acetylon Pharmaceuticals, Inc. Biomarkers to identify patients that will respond to treatment and treating such patients
JP6873053B2 (ja) 2015-06-08 2021-05-19 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. タンパク質脱アセチル化阻害剤の製造方法
US11298354B2 (en) * 2016-06-09 2022-04-12 Dana-Farber Cancer Institute, Inc. Methods of use and pharmaceutical combinations of HDAC inhibitors with BET inhibitors
ES2929032T3 (es) 2016-08-08 2022-11-24 Acetylon Pharmaceuticals Inc Combinaciones farmacéuticas de inhibidores de histona desacetilasa 6 y anticuerpos inhibidores de CD20 y usos de los mismos
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

Family Cites Families (51)

* 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
WO2001070675A2 (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
ES2294190T3 (es) 2001-11-01 2008-04-01 Janssen Pharmaceutica N.V. Derivados de amida como inhibidores de la glucogeno sintasa quinasa 3-beta.
US7154002B1 (en) 2002-10-08 2006-12-26 Takeda San Diego, Inc. Histone deacetylase inhibitors
US7381825B2 (en) 2003-03-17 2008-06-03 Takeda San Diego, Inc. Histone deacetylase inhibitors
CN101010298A (zh) 2004-04-05 2007-08-01 默克Hdac研究有限责任公司 组蛋白脱乙酰酶抑制剂前药
US8999289B2 (en) 2005-03-22 2015-04-07 President And Fellows Of Harvard College Treatment of protein degradation disorders
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
US8222423B2 (en) 2006-02-14 2012-07-17 Dana-Farber Cancer Institute, Inc. Bifunctional histone deacetylase inhibitors
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
KR101325374B1 (ko) 2008-02-19 2013-11-08 가부시키가이샤 오츠까 세이야꾸 고죠 신체 기능의 회복에 유용한 경구 또는 경장 조성물
AU2009274549B2 (en) 2008-07-23 2014-05-01 Dana-Farber Cancer Institute, Inc. Deacetylase inhibitors and uses thereof
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
US20130040998A1 (en) 2010-01-08 2013-02-14 Dana-Farber Cancer Institute, Inc. Fluorinated hdac inhibitors and uses thereof
PH12012501492B1 (en) 2010-01-22 2020-01-24 Acetylon Pharmaceuticals Inc Reverse amide compounds as protein deacetylase inhibitors and methods of use 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
WO2013158984A1 (en) 2012-04-19 2013-10-24 Acetylon Pharmaceuticals, Inc. Biomarkers to identify patients that will respond to treatment and treating such patients
EP2906211A4 (en) 2012-10-12 2016-04-20 Univ Pennsylvania PYRIMIDINHYDROXY AMID COMPOUNDS AS A PROTEIN DEACETYLASE INHIBITOR AND METHOD OF USE THEREOF
US9145412B2 (en) 2012-11-02 2015-09-29 Acetylon Pharmaceuticals, Inc. Selective HDAC1 and HDAC2 inhibitors
US9096549B2 (en) 2013-02-01 2015-08-04 Acetylon Pharmaceuticals, Inc. Selective HDAC3 inhibitors
US9139583B2 (en) 2013-02-01 2015-09-22 Acetylon Pharmaceuticals, Inc. Selective HDAC3 inhibitors
US20140357512A1 (en) 2013-06-03 2014-12-04 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
WO2015054099A1 (en) 2013-10-08 2015-04-16 Acetylon Pharmaceuticals, Inc. Combinations of histone deacetylase inhibitors and either her2 inhibitors or pi3k inhibitors
US9278963B2 (en) 2013-10-10 2016-03-08 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
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
CA2926808A1 (en) 2013-10-11 2015-04-16 Acetylon Pharmaceuticals, Inc. Combinations of histone deacetylase 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
WO2015084905A1 (en) 2013-12-03 2015-06-11 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
JP6952602B2 (ja) 2014-07-07 2021-10-20 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. ヒストンデアセチラーゼ阻害剤による白血病の治療
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
US9937174B2 (en) 2014-12-05 2018-04-10 University of Modena and Reggio Emilia Combinations of histone deacetylase inhibitors and bendamustine
AU2015360270B9 (en) 2014-12-12 2019-12-05 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
JP6873053B2 (ja) 2015-06-08 2021-05-19 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. タンパク質脱アセチル化阻害剤の製造方法

Also Published As

Publication number Publication date
WO2016200919A1 (en) 2016-12-15
US10464906B2 (en) 2019-11-05
TW201718516A (zh) 2017-06-01
AR104935A1 (es) 2017-08-23
EP3303306A1 (en) 2018-04-11
JP2018516946A (ja) 2018-06-28
EP3303306B1 (en) 2020-02-12
US20170001965A1 (en) 2017-01-05

Similar Documents

Publication Publication Date Title
CN105209437B (zh) 心肌肌球蛋白激动剂的盐和制备盐的方法
TWI882617B (zh) 3-((1r,3r)-1-(2,6-二氟-4-((1-(3-氟丙基)氮雜環丁-3-基)胺基)苯基)-3-甲基-1,3,4,9-四氫-2h-吡啶并[3,4-b]吲哚-2-基)-2,2-二氟丙-1-醇之固體形式及用於製備包含經取代苯基或吡啶基部分之稠合三環化合物之製程,包括其使用方法
JP6816036B2 (ja) ヒストン脱アセチル化阻害剤の結晶形態
JP2018520205A (ja) レンバチニブメシル酸塩の新規結晶形及びその製造方法
CN110650963A (zh) (S)-2-((2-((S)-4-(二氟甲基)-2-氧代噁唑烷-3-基)-5,6-二氢苯并[f]咪唑并[1,2-d][1,4]氧氮杂*-9-基)氨基)丙酰胺的多晶型物和固体形式及其制备方法
BR112019021447A2 (pt) sal fumarato, forma cristalina i do referido sal, métodos para preparação dos mesmos, composição farmacêutica compreendendo o sal e a forma cristalina i e uso do sal fumarato, da forma cristalina i e da composição farmacêutica
WO2011033307A1 (en) Nilotinib dihydrochloride salt
GB2558514A (en) Process for the synthesis of stable amorphous ibrutinib
WO2011023146A1 (en) Imatinib mesylate polymorphs generated by crystallization in aqueous inorganic salt solutions
US9453011B2 (en) Crystal form of dabrafenib mesylate and preparation method thereof
CN111278808B (zh) 2-(5-(4-(2-吗啉代乙氧基)苯基)吡啶-2-基)-n-苄基乙酰胺的固体形式
KR20200024302A (ko) 페닐 피리미돈 화합물의 염, 다형체 및 이의 약학 조성물 및 용도
JP7152122B2 (ja) エダラボン塩
US20220002302A1 (en) Novel polymorphs of acalabrutinib, a bruton's tyrosine kinase inhibitor
CN111499627A (zh) 取代的咪唑并吡啶基-氨基吡啶化合物的盐和多晶型
CN103819461B (zh) N-[3-氯-4-(3-氟苄氧基)苯基]-6-[5-[[2-(甲亚磺酰基)乙基]氨基]甲基]-2-呋喃基]-4-喹唑啉胺多晶型物及其制备方法
JP2020535192A (ja) レナリドミドの結晶形
CN113149998B (zh) 2-吲哚啉螺环酮类化合物或其盐、溶剂合物的无定形形式或结晶形式
TW202604502A (zh) Shp2抑制劑的新的晶型及其用途
WO2026067446A1 (zh) 一种大稠环化合物的盐、多晶型物及其应用
HU231012B1 (hu) Lapatinib sók
CN105732596A (zh) N-[3-氯-4-(3-氟苄氧基)苯基]-6-[5-[[2-(甲亚磺酰基)乙基]氨基]甲基]-2-呋喃基]-4-喹唑啉胺多晶型物及其制备方法
WO2016081538A1 (en) Solid state forms of ceritinib and salts thereof
WO2022199707A1 (zh) 哌马色林药用盐、制备方法、含其的药物组合物及应用
EP1768969B1 (en) Crystalline mycophenolate sodium

Legal Events

Date Code Title Description
A521 Request for written amendment filed

Free format text: JAPANESE INTERMEDIATE CODE: A523

Effective date: 20190527

A621 Written request for application examination

Free format text: JAPANESE INTERMEDIATE CODE: A621

Effective date: 20190527

A977 Report on retrieval

Free format text: JAPANESE INTERMEDIATE CODE: A971007

Effective date: 20200220

A131 Notification of reasons for refusal

Free format text: JAPANESE INTERMEDIATE CODE: A131

Effective date: 20200309

A601 Written request for extension of time

Free format text: JAPANESE INTERMEDIATE CODE: A601

Effective date: 20200608

A521 Request for written amendment filed

Free format text: JAPANESE INTERMEDIATE CODE: A523

Effective date: 20200904

TRDD Decision of grant or rejection written
A01 Written decision to grant a patent or to grant a registration (utility model)

Free format text: JAPANESE INTERMEDIATE CODE: A01

Effective date: 20201124

A61 First payment of annual fees (during grant procedure)

Free format text: JAPANESE INTERMEDIATE CODE: A61

Effective date: 20201223

R150 Certificate of patent or registration of utility model

Ref document number: 6816036

Country of ref document: JP

Free format text: JAPANESE INTERMEDIATE CODE: R150

R250 Receipt of annual fees

Free format text: JAPANESE INTERMEDIATE CODE: R250

LAPS Cancellation because of no payment of annual fees